Person centred care: Disease, medicines and patients Flashcards

Question

What does the degeneration of the dopaminergic neurone of the nigrostrital tract lead to ? ( what disease):

Answer 1

Parkinsons

Answer 2

-Tryptophan Which helps to make serotonin and melatonin. melatonin helps regulate sleep cycle serotonin regulates APPETITE, SLEEP, MOOD AND PAIN.

Answer 3

1) Glutamic acid (glutamate) 2) GABA( Gabba amino butyric acid) 3) Glycine

Answer 4

1) NMDA receptors 2) AMPA receptors 3) Kainite

Answer 5

The ability of neurones to strengthen their connections

Answer 6

Controls a ion channel, ion channel is entry of sodium and ca+ ions and exit of K+ ions. - This ion channel requires glycine as a co-agonist. ion channel is inhibitied by Mg 2+ ions

Answer 7

inhibitory important in controlling neural activity, as well as preventing seizures.

Answer 8

Cl - ion channel Divided into 2 different types : Type A and Type B

Answer 9

- When GABBA binds Cl- channel opens.

Answer 10

- Receptor recognises different agonists/ antagonists bringsabout inhibitory effects via G proteins

Answer 11

inhibitory transmitter - Also enhances the effects of NMDA receptors. Located in the spinal cord and lower brain. - Similar to GABBA A receptor.

Answer 12

binds allosterically to GLUTAMATE receptors.

Answer 13

Around 50 qualify as actual neurotransmitters. - most well known are "opiates" in the CNS which bind to receptors in the brain.

Answer 14

A layer of epithelial cells in the brain. Which has tight junctions between the cells. Main function is to prevent entry of harmful toxins into the brain.

Answer 15

will make it harder for them to pass through the BBB

Answer 16

Good if carrying out neurological treatment, bad if carrying out any other type of treatment, as to avoid neurological side effects.

Answer 17

ATP-binding cassette (ABC) transporter.

Answer 18

p-glycoprotein This transporter can eject a lot of molecules, even before therapeutic concentration is reached. ^ not goog famalam

Answer 19

Free nerve endings that are receptors for pain, everywhere except the brain.

Answer 20

Carried out by A-fibres 0.1 seconds after stimulus

Answer 21

carried out by unmyelinated C fibres. 1 second after stimulus.

Answer 22

pain from nociceptors on the skin.

Answer 23

pain in a joint or tendon etc

Answer 24

Pain from organ nociceptors.

Answer 25

Non-steroidal anti-inflammatory drugs.

Answer 26

They work by reversibly blocking action potential being carried along nerves. E.g. by blocking Na+ voltage operated channels. so nociceptor nerves can't carry pain signals. Analgesia occurs

Answer 27

more Na+ ions INSIDE the cell And more K+ ions OUTSIDE the cell

Answer 28

1) Polarisation ( Na+ ion channel opens, Na+ rushes into the cell) 2) Depolarisation (positive charge distributed) 3) Repolarisation ( K+ ion channel opens, K+ rushes out of cell, more negative potential on the inside). Hence, the cell is repolarised

Answer 29

This means that the faster the fire rate of a nerve (normally for smaller diameter neurones), the more efficient the anaesthetic will be at blocking it. This means they are more likely to enter Na+ VOCs that are open.

Answer 30

1) Lipid-soluble hydrophobic AROMATIC group 2) Charged hydrophilic AMIDE group. The bond between these groups determine whether the drug is a (amide or an ester)

Answer 31

The amide bond is stronger than ester linkage ester linkage can be easily broken.

Answer 32

This means that ester drugs are LESS stable and can't be stored for as long as amide drugs. Amide anaesthetics are also more heat stable, and therefore, they can be "autoclaved" (sterilised by heat).

Answer 33

Amides This is because the metabolism of esters produce PABA, which is associated with allergic reactions.

Answer 34

Para-aminobenzoic acid

Answer 35

1) Surface anaesthesia, by topic application to skin or mucous membrane. 2) Infiltration anaesthesia, by subcutaneous injection. 3) Intracerebral anaesthesia 4) Intravenous anaesthesia

Answer 36

By subcutaneous injection, causing nociceptive nerves to be blocked. In dentistry "infilatration" is used more.

Answer 37

Injecting the anaesthetic outside the "spinal dura mater"

Answer 38

Spinal injection into cerebrospinal fluid in the subarachnoid space.

Answer 39

Lidocaine.

Answer 40

Papaver Somniferum was taken orally for 200 years as " Tincture of laudanum".

Answer 41

Anything with "morphine- like actions" including endogenous and synthetic agents.

Answer 42

these drugs are used for opioids. normally addictive drugs which are illegal.

Answer 43

1) mu 2) delta 3) Kappa

Answer 44

G protein coupled receptors, which inhibit adenylyl cyclase reducing the amount of intracellular cAMP (Cyclic AMP).

Answer 45

Affects cell function. stimulated opioid receptors, Are able to inhibit the synaptic functions of neurones. by acting on ion channels.

Answer 46

They cause K+ ion channel to open hyperpolarising the nerve harder to become depolarised Reduction in neuronal excitability.

Answer 47

1) Receptor inactive and unoccupied 2) An opioid agonist binds to the receptor and activates it, and it's g-protein diffuses across the membrane. 3) Activated g protein causes K+ channel to to open, allowing the k+ ions to diffuse out the cells cell loses positive charge, and hence becomes hyperpolarised.

Answer 48

inhibits the opening of N-type Ca2+ channels.

Answer 49

inhibiting the n-type ca2+ channel, will mean fewer vesicles will be released reducing neurotransmission

Answer 50

mu-opioid receptor.

Answer 51

1) Respiratory depression (as respiratory centre becomes less sensitive to co2 in the blood), controlled by mu-receptors in the medulla. 2)Nausea and vomiting 3) Pupillary constriction 4) Constipation 5) Itching, bronchoconstriction, vasodilation, hypotension. 6) Sedation 7) Euphoria, controlled by mu- receptors

Answer 52

Respiratory arrest.

Answer 53

to treat dull, visceral pain. morphine diamorphine fentanyl pethidine

Answer 54

To control mild-moderate pain codeine (20% the potency of morphine)

Answer 55

Swapping from R to S chiral centres and vice versa. Not beneficial

Answer 56

Exists as a natural single enantiomer its unnatural enantiomer has no analgesic effect.

Answer 57

1) cough supressing 2) Anti-diarrhoeal preparations.

Answer 58

Naloxone this has affinity for all opioid receptor sub-types.

Answer 59

To reverse problems such as respiratory depression etc.

Answer 60

In opioid users they may cause unwanted side-effects (dysphoria) However, in non-opioid users there will be very little effect.

Answer 61

These receptors are not blocked by naloxone. not classified as true opioid receptors. - non-opioid drugs are also able to bind to sigma receptors (e.g. phencyclidine) balances euphoric effects, with dysphoric.

Answer 62

Tolerance is the increase in dose needed, to produce a given pharmacological effect.

Answer 63

1) Simple n convenient 2) allows for accurate dosing 3) can be used for both local and systemic treatment 4) cost effective (established manufacturing technologies).

Answer 64

1) may be difficult to administer to very young/elderly patients. 2) slow onset of action 3) Absorption and bioavailability can be difficult.

Answer 65

reduce solubility.

Answer 66

Drug is released after a certain period of time (e.g. 4-6hours). The drug reaches the small intestine, a change in pH causes the API to be released.

Answer 67

Enterically coated tablets (EC). the coating is gastro-resistant, and can withstand acidic conditions.

Answer 68

1) Diluents (fillers): bulk up the API. (e.g.lactose,starch) 2) Binders: Hold particles together (e.g. starch, modified cellulose, sugars) 3) Disintegrants: Break up the tablet into drug particles, to allow dissolution and absorption. (e.g. starch) 4) Glidants: Improve power flowability. (e.g. silicon dioxide) 5) Lubricants: to avoid punch face filming. (e.g. Mg and Ca) 6) Wetting agents: to improve interaction of water molecules with the tablet body and surface during disintegration and dissolution. (e.g. Sodium dodecyl sulphate SDS). 7) Others- ( colouring, sweetener and flavour). - Usually for chewable and effervescent tablets. E.g. Riboflavin (orange) colourant.

Answer 69

- increase palitibility by smoothening the surface - minimise unpleasant tastes - improve visual appearance - anti-counterfeiting measures - contain highly potent compounds in the body. - protect stomach from irritation, to to protect API from acidic stomach environment.

Answer 70

1) film coating ( water based) 2-5% of tablet's weight. 2) Sugar coating (20-50% of tablet's weight) 3) Gelatine 4) Enteric coating

Answer 71

1) Disintegration (tablet breaks up into granules) 2) Deaggregation( granules break up into particles) 3) Dissolution( release of API) At each stage the SA of the particles increases, which means rate of dissolution increases.

Answer 72

Capsule shaped tablets

Answer 73

High sodium carbonate/bicarbonate content. - not usually formulated with a binder.

Answer 74

gabapentin and Pregabalin. can also be used to treat epilepsy.

Answer 75

When nerve fibres become damaged. they send incorrect nerve signals to other pain receptors.

Answer 76

make the actions of GABA more potent. binds to regulatory site, causiing change in shape of the GABAA receptor, allowing it to bind more efficiently, giving a greater effect.

Answer 77

Reduce the release of 5-HT. to try reduce anxiety.

Answer 78

when blood flow is restricted causing the concentration of oxygen to be reduced

Answer 79

Chronic exertional compartment syndrome Usually during exercise. lack of muscle control blood can flow into an area, but can't drain out causing discomfort and swelling

Answer 80

Delayed onset muscle soreness muscle stiffness and muscle tenderness.

Answer 81

Exercise where your muscles act as "brakes" e.g. when you try to slow down whilst running

Answer 82

They lengthen

Answer 83

Eccentric exercise

Answer 84

NSAIDs e.g. ibuprofen

Answer 85

molecules which can alter the functions of other cells. NSAIDs work by interfering with autacoids They inhibit COX

Answer 86

COX it is a derivative of arachidonic acid

Answer 87

COX 1 : involved in homeostatic regulation COX 2: present in low levels normally, but present in high levels during inflammation

Answer 88

Blood flows to the affected area causing increased redness and warmth.

Answer 89

prostaglandalins

Answer 90

They increase post capillary venule permeability causing swelling to be enhanced

Answer 91

Reduced temperature and fever

Answer 92

inhibits both COX-1 and COX-2

Answer 93

reduced mucosal protection of the stomach, And GI ulcers may be formed

Answer 94

Therapeutic effect Due to reduction in prostanoid synthesis

Answer 95

Mainly POM Some may be OTC

Answer 96

binds reversibly This binding, renders platelets unable to produce TxA2. So they are not stimulated and phospholipase C is not stimulated So no inositol triphosphate is produced which means Ca2+ levels does not increase and platelets remain inactive viscosity of the blood DECREASES

Answer 97

yes but only at low doses for mild to moderate pain Also aspirin can bind to cox 1 irreversible

Answer 98

by producing NEW platelets (takes 7-10 days) the only way to bring platelet function back to normal

Answer 99

Anti platelet drugs

Answer 100

- gastric discomfort - nausea vomiting - indigestion (dyspepsia) - skin rashes

Answer 101

Their lung alveoli constricts. may lead to an asthmatic attack. NSAIDs must not be supplied to asthmatic patients

Answer 102

They reduce renal function

Answer 103

inhibition of prostaglandins, Causes renal artery to contract which means blood flow to the kidneys is reduced This may even lead to renal failure Therefore NSAIDs are not supplied to patients with kidney injuries (AKI: Acute kidney injury)

Answer 104

1) Analgesic 2) anti-inflammatory 3) anti pyretic

Answer 105

48 hours as first you want the natural healing mechanism from the "inflammatory pathway" to kick start the healing.

Answer 106

To help remove the unwanted side effects that occurred by "COX-1 inhibition". E.g.(negating the effects COX 1 have on the gastrointestinal mucosa lining, allwoing it to be protected)

Answer 107

COX-2 has a bigger binding site and contains a "side-pocket" COX-1 has a narrow binding site

Answer 108

Can bind to both as they are small enough

Answer 109

They produce PGI which acts against the TxA, that is released by platelets preventing clot formation

Answer 110

Decreases production of PGI, but TxA is still produced by platelet COX-1. which means the balance has shifted towards TxA, increasing the risk of developing thrombosis.

Answer 111

1) Enteric coating (protect from stomach ulceration) 2) Soluble preparations- preventing NSAIDs to be concentrated in one area of the stomach. 3) Suppositories: provides an alternative absorption route.

Answer 112

1) Gelatine (some can be used as a suppository as they are soft) 2) HMPC (Hydroxypropyl methylcellulose) 3) PVA ( polyvinyl alcohol)

Answer 113

High As capsule shells are designed to dissolve rapidly when it comes in contact with GI fluids.

Answer 114

- colourless translucent substance, which is tasteless - readily soluble in biological fluids at body temp - it is brittle when dry - And it is elastic when wet and forms a semi-solid gel. - cost-effective to produce

Answer 115

- very sensitive to heat and moisture so special packaging and storage may be required. - may cause solubility problems with different formulations

Answer 116

1) Gelatine 2) water 3) Colourants 4) Preservatives 5) excipients

Answer 117

1) can make it easier to administer very low doses (micro doses), due to semi-solid formulation. 2) fewer excipients required 3) better oral bioavailability than tablets

Answer 118

1) May be difficult to manufacture 2) capsule production used to be slower than tablet production, until "high speed capsule filling equipment was developed. 3) More costly to develop than tablets 4) Not all drugs can be encapsulated.

Answer 119

1) A good choice for "non-palatable" solutions 2) Great for delivering lipid soluble drugs at low doses 3) Can be immediate, slow or sustained release, also an enteric coat can be added.

Answer 120

1) Restricts formulation that can be encapsulated 2) Hard to optimise manufacturing process 3) If one capsule breaks during manufacturing or whilst in storage, formulation could leak onto others this leads to increase waste. 4) moisture sensitive drugs are incompatible with the "moist nature" of the soft gelatine capsules 5) They are temperature sensitive (contents inside should not exceed 35 degrees Celsius).

Answer 121

Diclomax SR

Answer 122

Nurofen liquid capsules

Answer 123

API as crystalline solids that can be made into finely divided solids.

Answer 124

Like a powder but bigger particle sizes - big physical aggregates of powder particles. - help to increase "flow" and "compatibility". - easier to handle when exposed to moisture than "powders".

Answer 125

1) Dry granulation 2) Wet granulation

Answer 126

Compaction of powder without water

Answer 127

Addition of water to powder followed by mixing and removal of the water.

Answer 128

1) Bulk powders: Found in large containers 2) Divided powders: Individually packaged pre measured doses.

Answer 129

1) More chemically stable than liquid formulations 2) Easier to dispense in large doses 3) fast absorption rate 4) Advances in packaging tech, means that it is becoming easier to make divided doses easier to separate.

Answer 130

1) Not as convenient as small containers of tablets 2) more difficult to mask unpleasant taste, to mask taste it has to be converted into "effervescent" form. 3) Hard to administer low doses 4) Can not be used for oral administration

Answer 131

- proliferation of synovium -destruction of cartilage between joints, and also bone by "osteoclasts". - inflammation of cytokines.

Answer 132

To function as opsonins -Enhancing the uptake by macrophages and neutrophils.

Answer 133

Antibodies that react with "self-antigens"

Answer 134

Immunoglobulin G Also known as IgG or IgM - found in all Rheumatoid arthritis patients

Answer 135

Actually it can function as BOTH and antigen and an antibody

Answer 136

RA (autoimmune- body immune system cells attack the joints) OA (wear and tear)

Answer 137

DMARDs Disease modifying anti-rheumatic drugs - causes long term reduced swellings and joint pains - causes level of plasma acute phase proteins to decrease.

Answer 138

3 months after slow onset of action - in the mean time NSAIDs may be used to reduce symptoms

Answer 139

"short term bridging treatment" with a corticosteroid - to help control symptoms. whilst waiting for the effects of the DMARD to kick in

Answer 140

Due to adverse effects that may occur - wight gain - mood changes

Answer 141

1) DMARDs that supress rheumatic disease process 2) Cytokine modulators (biologics) derived from antibodies

Answer 142

They supress or modify immune response But this can also mean an increase risk of infections due to interfering with the normal immunological response

Answer 143

Takes 1 month And treatment can then be long term with appropriate monitoring

Answer 144

Once a week ONLY usually by oral admin

Answer 145

- nausea - stomatitis (inflammation of buccal lining) - liver cirrhosis - pneumonitis (inflammation of lung tissue)

Answer 146

NSAIDs may reduce the rate of renal clearance of methotrexate leading to increase risk of toxicity

Answer 147

Trimethoprim - if taken together could lead to agranulocytosis or neutropenia Agranulocytosis- deficiency of granulocytes in the blood, causing an increase in vulnerability to infections. Neutropenia- low number of white blood cells in the blood could be fatal

Answer 148

Folic acid But should only be taken Once a week ONLY and should not be taken on the same day as methotrexate.

Answer 149

It's a prodrug that acts as an immunosuppressant by inhibiting the increase of B and T lymphocytes

Answer 150

To stop rejection from transplanting organs.

Answer 151

- nausea - diarrhoea - vomiting - liver toxicity -bone marrow suppression - increase risk of infections (due to potential over suppression of lymphocytes)

Answer 152

Fewer blood cells being produced in the bone marrow

Answer 153

Sore throat

Answer 154

Drugs with long half lives used to treat mild RA - not as effective as other DMARDs

Answer 155

Eye examination as retinopathy could occur (damage of retina) by taking antimalarials - patients may be advised to wear sunglasses

Answer 156

RA but can mess up taste buds and its enantiomer (L-penicillamine) is toxic as it inhibits the action of pyridoxine.

Answer 157

A DMARD with fewer side effects than other DMARDs reduces lymphocyte proliferation and cytokine production. Treat ulcers and chron’s disease, and inflammation in the bowels.

Answer 158

Enteric coating

Answer 159

1) Mineralocorticoids (regulate salt and water balance) 2) Glucocorticoids ( regulate carbs, fats and proteins in response to stress).

Answer 160

Anti inflammatory and immunosuppressant agents by inhibiting phospholipase A2 and COX-2

Answer 161

1) Glucocorticoid levels rise in the blood 2) this is detected by the hypothalamus 3) Causes pituitary gland to secrete less adrenocorticotrophic hormone (ACTH). 4) Glucocorticoid synthesis is reduced

Answer 162

Kinda decrease the functions of the adrenal gland

Answer 163

Redistribution of body fat - puffy facial cheeks - Thin skin- harder to heal from wounds and injuries. - Osteoporosis (weak bones) caused by excess amount of corticosteroid hormones being released

Answer 164

Cells that reabsorb bone by digging "pits"

Answer 165

Cells that secrete "osteoid" (bone matrix) into the "pits" that osteoclasts dig. - The osteoid is then mineralised, resulting in calcium phosphate crystals being made.

Answer 166

calcium Phosphate protein mesh work

Answer 167

Parathyroid hormone (PTH) PTH is secreted by the parathyroid gland when Ca2+ conc is low.

Answer 168

The reabsorption of Ca2+ ions by the kidney.

Answer 169

-Inhibits "calcium mobilisation" (from bone to blood). -And also decreases reabsorption from the renal tube.

Answer 170

Reduction of minerals in the bone

Answer 171

Reduction in actual bone mass

Answer 172

1) Hormone replacement therapy 2) Selective Oestrogen receptor modulators (SERMs): may help to (E.g. Raloxifene) - increase osteoblast activity -reduce osteoclasts Raloxifene has a low bioavailability but is well distributed around the body. 3) PTH fragments: Help to increase bone mass by stimulating increase in osteoblast numbers. Given subcutaneously. They do this by acting on GPCR activating adenyl cyclase and raise intracellular CA2+ levels 4) Bisphosphates: Promote apoptosis of osteoclasts, causing bone reabsorption to be inhibited. - given orally - due to potential GI irritation caused by food (milk). patient is advised to remain upright for 30 mins after taking drug.

Answer 173

condition that causes the softening of bones. to prevent rickets increase vitamin D intake - In adults rickets is known as "osteomalacia"

Answer 174

Eat oily fish (Salmon and mackerel) eggs margarine cereal sun light can be administered as calcitriol (active form of vitamin D) Or ergocalciferol (inactive form of vitamin D).

Answer 175

joint pain long term condition most common type of arthritis in the uk develops in people over the age 45

Answer 176

Sometimes it can in some situations

Answer 177

Around 10-15 grams - no symptoms occur for 24 hours after overdose. - but irreversible liver damage reaches peak by 72-96 hours.

Answer 178

Ideally N-acetylcysteine should be administered with the first 8-10 hours of overdose. - this helps to speed up the replenishment of "glutathione" - potential liver transplant if damage too severe.

Answer 179

Type of arthritis where crystals of sodium urate form around and inside joints. - acute joint pain in hands or feet due to excess uric acid.

Answer 180

1) Naproxen or NSAID 2) Colchicine - does not cause fluid retention unlike NSAIDs, so can be used in heart patients. - also may be toxic at high doses. 3) Corticosteroids: for people who cant tolerate NSAIDs.

Answer 181

No can inhibit the nephron tubule from uric acid in urine. causing build up of uric acid not gooood.

Answer 182

Allopurinol decreases production of uric acid by non- competitive inhibition of xanthine oxidase. reverses deposition of crystals. - not used for for acute treatment. - painful as reduction in uric acid, causes crystals to dissolve, which escape into joint cavity and inflame the synovium.

Answer 183

1) Administer simple analgesics (paracetamol, ibuprofen) 2) Weak opioids 3) Strong opioids

Answer 184

1) Gabapentin (used first line) 2) Pregabalin ( used second line)

Answer 185

As well as being able to treat neuropathic pain They can also treat "epilepsy".

Answer 186

Potentiate GABA by changing the shape of the "GABA type A receptor", causing it to bind more efficiently to neurotransmitter and give a greater effect. - Also causes chloride channel to open, causing more Cl- ions to flow through the channel giving a greater inhibitory effect.

Answer 187

induce sleep reduced senses mild amnesia reduced muscle tone

Answer 188

To inhibit release of 5-HT - well absorbed - short half life nausea and dizziness are common side effects.

Answer 189

1) D1 type: D1 and D5 linked to ACTIVATION of adenylyl cyclase 2) D2 type: D2,D3,D4 subtypes - linked to INHIBITION of adenylyl cyclase - effective as antipsychotics.

Answer 190

1) typical: first generation drugs - chloromazapine, haloperidol - binds to D1 and D2 receptors - may lead to unwanted side effects 2) atypical: second generation - Clozapine, risperidone -- more selectivity for D2 receptors - May reduce unwanted side effects (by blocking 5-HT2A receptors)

Answer 191

A possibility of "hypertension" occurring for people who each cheese whilst taking a MAOI drug. - caused by an interaction with "tyramine".

Answer 192

To treat the hypertension, "phentolamine" can be given. To treat hypotension, it is not treated with a drug, due to risk of developing "hypertension".

Answer 193

Work by competitively inhibiting the reuptake of neurotransmitter from synapses. - Which means more NA and 5-HT remain in the synapses - Eventually, allowing mood to improve.

Answer 194

- Dry skin ( cant sweat) - Dry mouth - blurred vision To treat administer "activated charcoal" to prevent further GI absorption. Seizures can be supressed with "diazepam"

Answer 195

Selective serotonin reuptake inhibitors Commonly prescribed as antidepressants

Answer 196

-Work by INHIBITING 5-HT reuptake -Causing increase in 5-HT concentrations

Answer 197

Acute treatment: Initially causes “autotecptors” to be activated -to inhibit release of 5-HT. Chronic treatment: -Causes auto receptors to desensitise. - causing an increase in the release of 5-HT.

Answer 198

- reduced antimuscarinic effects - safer overdose than an overdose of TCAs - don’t cause “cheese reaction” with MAOIs

Answer 199

Only treat moderate depression TCAs treat more severe depression

Answer 200

It can initially cause to become Excessively Excited And even aggressive And even insomnia

Answer 201

higher risk of withdrawal effects compared to other anti depressants.

Answer 202

Long term At least 9 months

Answer 203

2-3 weeks following the last MAOI dose. - And MAOIs can not be introduced again for 3 weeks following TCA and SSRI therapy (5 weeks after fluoxetine).

Answer 204

Moclobemide (maoi)

Answer 205

TCAs Except for lofepramine.

Answer 206

The basal ganglia

Answer 207

Imbalance between excitatory and inhibitory inputs.

Answer 208

idiopathic parkinsonism

Answer 209

Neurodegeneration( loss of neurones) of the basal ganglia causing a reduction in dopaminergic cells of the substantia nigra (modulates motor movement). - Also a net increase of INHIBITORY GABAergic output occurs.

Answer 210

slowness of movement symptom of parkinsonism

Answer 211

Shaking Most recognisable symptom of parkinsonism

Answer 212

Affects ability to balance increases risk of falling Symptom of parkinsonism

Answer 213

Co-careldopa Its a pro drug A drug which must undergo metabolic processes before becoming pharmacologically acitve.

Answer 214

No its too polar

Answer 215

levodopa is an amino acid so can take advantage of "protein carrier systems"

Answer 216

It is decarboxylated and converted into dopamine.

Answer 217

Dopa decarboxylase.

Answer 218

Carbidopa Carbidopa inhibits dopa decarboxylase And therefore inhibits transformation of levodopa to dopamine. - causing side effects to be reduced.

Answer 219

Loss of cholinergic neurones in the hippocampus and frontal cortex.

Answer 220

Acetyl-cholinesterase inhibitors to increase conc of Ach

Answer 221

valproate - increases GABA content - effective against both "Grand and Petit Mal seizures". - used in children due to low toxicity

Answer 222

1) Phenytoin: effective for "absence seizures" 2) carbamazepine: Not effective for "absence, atonic or tonic seizures". 3) Pregabalin and gabapentin

Answer 223

Nah They have "smooth muscle tissue" for contraction and to keep air ways open.

Answer 224

Primary Bronchi Secondary and Tertiary Bronchioles Terminal bronchioles ( smallest and final branch of bronchioles) Alveolar sacs

Answer 225

Made up of "alveoli" O2 enters the blood stream through alveolar sacs and Co2 is eliminated.

Answer 226

pseudostratified ciliated columnar epithelial cells.

Answer 227

Secrete mucus to trap particles, irritants and any unwanted pathogens.

Answer 228

To waft mucus away from the tract.

Answer 229

Sympathetic nervous system - causes an increase in bronchiole calibre (bronchodilation)

Answer 230

parasympathetic nervous system

Answer 231

1) smooth muscles in the walls of bronchioles RELAX 2) Allowing airways to open up 3) Decreasing air way resistance, and making it easier to breathe.

Answer 232

bronchoconstriction

Answer 233

When bronchiole calibre constrict Usually during periods of relaxation to avoid inhaling too many small particulates. - Bronchoconstriction, leads to an increase in airway resistance.

Answer 234

Beta2 adrenoreceptors

Answer 235

"Adrenergic receptors" receptors that respond to adrenaline and noradrenaline

Answer 236

Postganglionic parasympathetic fibres.

Answer 237

1) Bronchial smooth muscle for bronchoconstriction 2) Also found on glands to facilitate the secretion of mucus, -M3 receptors are the most pharmologically important receptors of the 3 types of muscarinic receptors.

Answer 238

M1, M2, M3

Answer 239

Located in the ganglia on postsynaptic cells - facilitates nicotinic neurotransmission.

Answer 240

They are "inhibitory auto receptors" - They mediate negative feedback on the release of ACh, from postganglionic parasympathetic fibres.

Answer 241

Reduce release of neurotransmitters.

Answer 242

Receptors located in the the membrane of nerve cells.

Answer 243

"recurrent reversible obstruction of air flow in the air way, due to a stimuli which is not considered noxious (harmful), and would not affect a non-asthmatic patient.

Answer 244

Allergens Such as drugs aspirin house dust mites pollen emotions cold air pollutants in the atmosphere infections

Answer 245

Wheezing coughing tight chest Difficulty breathing

Answer 246

Forced expiratory volume in one second. - This is lower in asthma patients

Answer 247

1) Bronchial hyper responsiveness 2) Inflammation in the airways

Answer 248

1) Immediate bronchospasm (Early phase) 2) Bronchiole inflammation (Blood vessels dilate, oedema forms, excess mucus is produced). (known as "late phase"). - This is caused by eosinophils releasing inflammatory mediators. 3) Bronchiole smooth muscle contracts, lining of airway become inflamed 4) Leading to reduced airflow.

Answer 249

Bronchoconstriction due to contraction of smooth muscle

Answer 250

sensitive to allergens

Answer 251

Activated t cells with t-helper 2 cells (Th2) profile of cytokine production in the the bronchial mucosa.

Answer 252

1) APCs present the antigens of the allergen to CD4 T cells, via MHC class II (major histocompatibility complex). 2) These differentiate into Th0 lymphocytes 3) Th1, and clonal expansion of Th2 lymphocytes. 4) Th2 lymphocytes produce various cytokines

Answer 253

Interleukin 5 Interleukin 4 , Interleukin 13

Answer 254

Promotes differentiation and activation of eosinophils.

Answer 255

Cause B cells and plasma cells to produce and release IgE And allow the expression of IgE receptors on mast cells and eosinophils.

Answer 256

causes the release of spasmogens (mediators of bronchoconstriction) - also causes the release of histamines, PGD2, cysLTs (leukotrienes C4 and D4 (LTC4 and LTD4)). Early phase. Chemotactic mediators are released in late phase. Late phase is mainly just the progression of inflammatory events from the "early phase".

Answer 257

Yes Can also happen in patients with normal levels of IgE. can be triggered by respiratory tract infections.

Answer 258

Not very effective.

Answer 259

By treating with: - Beta2 adrenoreceptor agonists - CysLT receptor antagonists - Theophylline.

Answer 260

Inhibited by Glucocorticoids.

Answer 261

Mast cell degranulation

Answer 262

1) Allergic trigger or non specific trigger 2) Mast cells 3) Bronchoconstrictors and chemotactic mediators (Histamine, cysLT, PGD2) 4) Bronchospasm

Answer 263

1) Infiltration of Th2 cells and their cytokines they produced, and activation of eosinophils 2) mediators of inflammatory response (CysLTs, adenosine, neuropeptides) AND toxic proteins AND growth factors (smooth muscle cell hypertrophy, hyperplasia) 3) Airway inflammation/ air way hyper-reactivity (if epithelial is damaged) 4) Bronchospasm, coughing and wheezing.

Answer 264

Increased size of smooth muscle cells and thickening of smooth muscle around airways.

Answer 265

increased size of tissue or organ due to excessive cell production

Answer 266

Airway hyper reactivity airways become very sensitive -leads to a "steeper slope on the dose response curve" -and also a greater "maximal response " to the agonist.

Answer 267

1) Bronchodilators- help to reverse bronchospasm 2) Anti inflammatory agents- help to prevent or inhibit the inflammatory components and causes of asthma.

Answer 268

G protein coupled receptors They need the help of a "g protein" to go between it and its target.

Answer 269

in bronchial smooth muscle

Answer 270

1) Salbutamol/adrenaline bind to activated b2-adenoreceptor 2) This causes the G protein to activate. 3) The G protein then diffuses across the cell membrane, and comes into contact with "adenyl cyclase" 4) Adenyl cyclase then converts ATP into cAMP (Secondary messenger). 5) cAMP then diffuses into the cell and comes into contact with Protein kinase A (PKA), and activates it. 6) Activated PKA causes phosphorylation of the myosin-light chain kinase (MLCK). 7) This causes smooth muscle contraction of bronchi to be inhibited. Relaxation of smooth muscle. 8) Results in bronchodilation. Reducing asthmatic symptoms.

Answer 271

Increased mucus clearance by an action on cilia in the airway. - inhibit mediators being released from "mast cells" - inhibits release of tissue necrosis factor-alpha.

Answer 272

Too much salbutamol means B2-adenoreceptor occupancy in airways is high so any excess salbutamol will start to bind to other receptors could bind to receptors in the heart - which could cause palpitations or tachycardia. (by binding to B1-adenoreceptors) could bind to receptors in the skeletal muscle by binding to b2-adenoreceptors. This may cause muscle tremor.

Answer 273

1) "Fries rearrangement" of aspirin, causes a ketoacid to be produced 2) The keto acid is then esterified. 3) Bromination of the ketone allows for the introduction of an amino group by nucleophilic substitution. 4) Methyl ester and ketone then undergo reduction, and the N-benzyl group is removed.

Answer 274

Replacing the tert-butyl group with large alkyl groups This lead to the production of the drug "Salmeterol" - twice as potent as salbutamol, and has an extended action of 12 hours. usually given twice a day. Another long duration of action drug is "indacaterol". Usually only given once a day.

Answer 275

To relax bronchiole constrictions mainly used for treating COPD by antagonising M3-muscarinic receptors on bronchial smooth muscle cells to cause relaxation. - may also have inhibitory effects on mucus secretion in asthmatic

Answer 276

Ipratropium - Administered by inhalation. - max effect occurs after 30 mins - lasts for 3-5 hours

Answer 277

May go rogue may not be able to differentiate between muscarinic receptor subtypes. E.g. May bind to M2 instead of M3-muscarinic receptors - causing more Ach to be released - causing more vagally-mediated bronchoconstriction. - This may cause a reduction in M3 antagonism at high doses of ipratropium.

Answer 278

Tiotropium lasts for at least 24 hours time to increase FEV1 ( forced expiratory volume in one second) = 30 mins time to increase to PEAK FEV1 (max effect) = 1.5-3 hours

Answer 279

1) Acetylcholine released from postganglionic parasympathetic nerves and binds to M3 recepetors on bronchial smooth muscle cells 2) Sub unit of the g protein activates phospholipase C, which hydrolyses phosphatidylinositol 4,5-bisphosphate(PIP2) into diacylglycerol(DAG) and inositol 1,4,5-triphosphate (IP3) 3) IP3 binds to IP3 receptor located on he endoplasmic reticulum (ER) 4) Ca2+ released from intracellular stores of the ER 5) Ca2+ binds to calmodulin to activate myosin light chain kinase (MLCK) 6) Smooth muscle contracts when myosin light chain undergoes phosphorylation. - DAG may also stimulate entry of Ca2+ ions.

Answer 280

It's quaternary nitrogen" - Ipratropium also has low systemic absorbance.

Answer 281

Three membered ring containing oxygen.

Answer 282

Epoxide group - very reactive - but hard for nucleophiles to enter "inside" the ring. Not enough space

Answer 283

Bronchodilation

Answer 284

1) Inhibits PDE (phosphodiesterase). - levels of cAMP increase - causes bronchodilation 2) Competitive antagonism at adenosine receptors (A1 and A2 receptors) 3) Activation of histone deacetylase - An enzyme that inhibits the acetylation of core histones, that are required for the transcription of inflammatory genes.

Answer 285

Inhibits acetylation of core histones, required for transcription of inflammatory genes.

Answer 286

1) interfere with sleep patterns 2) vasoconstrict blood vessels but will vasodilate most other vessels 3) GI irritation

Answer 287

1) Increase renal blood flow, therefore increase glomerular filtration rate 2) Cause increased alertness

Answer 288

30-100 micromol >110micromol can cause adverse effects >200 micromol can be lethal can cause serious CNS and cardiovascular effects, and even seizures.

Answer 289

Either orally or sustained release or IV injection, followed by IV infusion

Answer 290

Drugs which ACTIVATE P450 enzymes such as Carbamazepine, phenytoin and rifampicin.

Answer 291

Drugs which INHIBIT p450 enzymes such as Erythromycin, ciprofloxacin, diltiazem, fluconazole.

Answer 292

Arachidonic acid - Leukotriene is a major inflammatory mediators More specifically LTD4 and LTC4 (major mediators of bronchoconstriction)

Answer 293

20 carbon with 4 C=C bonds.

Answer 294

Less than 10% of asthma patients are very sensitive to aspirin which means leukotrienes can not bind to their receptors.

Answer 295

As a 3rd line drug along with inhaled corticosteroids and beta2 agonists - less effective at bronchodilation than salbutamol.

Answer 296

1) montelukast 2) Zafirlukast

Answer 297

Bronchodilators help to reverse early phase of bronchospasm Whereas, Glucocorticoids inhibit the inflammatory effects that occur during both phases.

Answer 298

High so crosses the plasma memmbrane easily

Answer 299

1) Cross plasma membrane 2) binds to intracellular receptors which "dimerise" 3) move towards the nucleus and interact with DNA 4) This causes transcription of genes to be modified 5) This induces synthesis of some proteins, but may also inhibit the synthesis of other proteins.

Answer 300

1) enhance expression of lipocortin - suppressing phospholipase A2 - Reducing formation of arachidonic acid and therefore leukotrienes. - limited evidence of annexin-1 (lipocortin) having therapeutic use in treating asthma. 2) Decrease the formation of Th2 cytokines Inhibits: - Activation of eosinophils - clonal expansion of b cells dividing into plasma cells to produce IgE. 3) Reduce the synthesis of cytokines - supressing early phase response to allergens.

Answer 301

1) Metabolic effects hyperglycaemia (high blood sugar) - thinning of skin- easily bruised. Purple/red stretch marks. - fat redistribution (onto neck shoulders and face) 2) Osteoporosis 3) Reduced growth in kids 4) Reduced ability to heal wounds 5) More susceptible to infection - It's anti-inflammatory function may supress features of immune response.

Answer 302

Cushing's syndrome - too much of the hormone cortisol in the body -fat on chest,tummy, neck or shoulders

Answer 303

Simply by reducing or preventing inflammatory effects.

Answer 304

- patients who require regular bronchodilators, are also considered to take "beclomethasone" along with it (glucocorticoid). - patient with acute asthma may require IV hydrocortisone and oral prednisolone (glucocorticoid) - If severity of clinical condition is deteriorating, a "rescue course" of prednisolone may be administered.

Answer 305

- to gargle after inhaling - to use "spacers" in their inhalation device.

Answer 306

1) slows down aerosolid particles, increasing the amount of fine particles being deposited into the lungs. 2) Helps patients with reduced manual dexterity. Helps patients who find it hard to activate the pMDI by pressing down on the canister. 3) Reduces deposition of larger particles into the mouth and back of the throat.

Answer 307

1) LABA 2) Glucocorticoid

Answer 308

No Some use 3 agents (trim bow)

Answer 309

Yes they do The combination inhaler is just used prevention treatment.

Answer 310

- might be better at controlling symptoms - lower doses of inhaled corticosteroids needed: minimising risk of adverse effects. - More convenient for the patient - May be more cost effective

Answer 311

1) Possible lack of dose flexibility 2) may use inhaler to relieve bronchospasm, which means patient may inhale a much larger amount of steroid than intended.

Answer 312

salbutamol for both acute and chronic asthma

Answer 313

- tremor in hands - nervous tension - headache -cramps, palpitations

Answer 314

1) Emphysema (alveoli) 2) Bronchitis (bronchi)

Answer 315

- Dust - exposure to chemicals - environmental exposures (second hand smoke). - Genetic (deficienccy of alpha-antitypsin)

Answer 316

1-2 % its rare lung function decline is faster for these type of patients than smokers. As there is not enough antitrypsin to inhibit certain enzymes that cause lung damage.

Answer 317

- Breathlessness - Chronic cough - Regular phlegm production 9may require antibacterial treatment). - Bronchitis in the winter - wheezing

Answer 318

When COPD patient gets a cold or flu in the winter. May cause winter bronchitis. - cant maintain normal oxygenation of blood - lips and tongue may be visibly blue - may lead to pulmonary hypertension

Answer 319

- Bronchodilator therapy - as well as treatment usiing a nebuliser - Administering oxygen if needed.

Answer 320

Aminophylline via IV administration.

Answer 321

Short course of oral corticosteroid, such as prednisolone 30mg for 1-2weeks

Answer 322

Short acting beta agonist/short acting antimuscarinic agent. Salbutamol is an example of a short acting beta agonist.

Answer 323

NO As in smokers HDAC activity is inhibited explaining the lack of effect glucocorticoids have

Answer 324

1) Immunised against influenza 2) Antibacterial treatments 3) Oxygen administration - However be cautious for potential co2 retention - only 24% o2 is administered 4) Administration of mucolytic drugs ro reduce plegm production

Answer 325

Afferent nerve stimulation.

Answer 326

H1,H2,H3,H4

Answer 327

involved in the defensive actions of histamine - coupled to Gq, inositol phospholipid metabolism, Ca2+ intracellular signalling pathways - Regulate intracellular Ca2+ - some may be located in the CNS, and help with learning and memory.

Answer 328

Mediate gastric acid secretion -generates cAMP as a secondary messenger - involved in cardiac function

Answer 329

- Involved in cognition and appetite

Answer 330

Located on eosinophils and basophils and mast cells.

Answer 331

causes blood vessels to dilate which leads to vasodilation

Answer 332

Reddening (vasodilation) - increased permeability of post-capillary venules - stimulation of sensory fibres leading to CGRP (sometimes referred to as triple response).

Answer 333

Inverse agonists

Answer 334

reduce the level of activity at h1 receptors and block the effects of histamine.

Answer 335

Ephedrine is a a1-adenoreceptor agonist produces local vasoconstriction causes the opening of the nasal pathway

Answer 336

Topical nasal decongestants

Answer 337

Impaired activity of ciliary in the nasal mucosa - therefore can not be used for more than 7 days

Answer 338

3 first,second,third

Answer 339

1) lipophilic, can cross the BBB 2) may cause drowsiness and psychomotor impairment 3) Produce anti-muscarinic side effects, such as dry mouth, blurred vision, urinary retention, GI irritation.

Answer 340

Cetirizine and loratadine

Answer 341

(non-sedating) - more hydrophilic/more ionised at certain pH. - Can not pass through BBB easily

Answer 342

Active metabolites of second gen antihistamines.

Answer 343

Desloratadine - its an active metabolite of loratadine.

Answer 344

1st gen are absorbed slowly whereas as 2nd gen are absorbed fast from the gut - 1st gen undergo considerable first pass metabolism into inactive compounds - 2nd gen metabolised in the liver into active compounds

Answer 345

New and Old antihistamines

Answer 346

- cross the BBB and cause drowsiness and sedation. - can have antimuscarinic side effects - despite being old, they are still useful )e.g. to treat people who cant fall asleep due to hay fever, or to treat motion sickness).

Answer 347

- does not cross BBB - affects muscarinic receptors - produces fewer side effects

Answer 348

The oropharynx just behind the oral cavity

Answer 349

1) trachea and bronchi )lower respiratory tract) 2) to bronchiole and alveolar region

Answer 350

Fine aerosols distributed on peripheral airways, but deposit less drug per unit surface area. - larger particle aerosols deposit more drug per unit surface area, but on the larger more central airways.

Answer 351

Heterodisperse aerosols containing a wide range of particle sizes.

Answer 352

1) Impaction: -occurs in UPPER respiratory tract. -particles with a diameter greater than 10um. - large particles are swallowed, but this has no therapeutic effect 2)Gravitational sedimentation: - particles with diameter less than 10um - deposited in the LOWER respiratory tract. 3) Gravitational diffusion: - occurs in particles below 0.5um. - any not deposited, are exhaled during exhalation (sometimes even 80% exhaled).

Answer 353

1) Diameter of 5-10um = deposited in UPPER respiratory tract 2) Diameter of 1-5 um = Deposited in the LOWER respiratory tract and alveoli.

Answer 354

1) nebuliser 2) dry powder inhaler 3) meter dose inhaler

Answer 355

1) Jet nebuliser- gas 2) ultra sonic nebuliser- liquid (higher freq = smaller size of droplets produced)

Answer 356

- provide large doses with very little patient co-ordination or skill. - disposable nebulisers are cost effective

Answer 357

- consuming and inefficient - Drug wastage (50%) - however, the actual compressors supplying the air in a nebuliser are not low cost. - most of the drug tends to never reach the lungs (most of it either stays in the nebuliser or is released into the environment when breathing out). - only 10% makes it to the lungs on average.

Answer 358

suspension/solution in a select propellent

Answer 359

1) Small volume of drug is homogenously dispersed in a high vapour pressure propellant. 2) metering chamber is opened through an actuator nozzle (this is achieved by a meter valve) 3) Once open to the atmosphere, the high pressure contents of the metering valve, equilibrate with atmospheric pressure. - Contents are propelled rapidly through the nozzle, causing shear and droplet formation.

Answer 360

1) evaporating 2) propelling 3) shearing Ultimately, to reduce the size of droplets produced

Answer 361

Only 10-20% 50-80% goes to the oropharyngeal region

Answer 362

Means a lower drug deposition into the lungs. (Higher IFR=lower drug deposition

Answer 363

Less deposition of drug into alveoli - as aerosol is more readily deposited by impaction in the bronchiole and oropharyngeal region.

Answer 364

When freezing spray temperature, causes patient to stop inhaling the drug.

Answer 365

- helps to reduce co-ordination difficulties - increased drug deposition into the lungs from 7.2% to 20.8%. - however, they dont improve lung deposition in patients who already have good pmdi technique.

Answer 366

By adding a battery-driven propeller - which helps in the dispersion of the powder. without out too much effort inhaling.

Answer 367

1) susceptibility to hydrolysis 2) Light and heat 3) Presence of complex agents might affect solubility 4) conc near the "solubility limit" may cause precipitation.

Answer 368

Due to degradation of drugs and potential microbial growth.

Answer 369

May induce bronchoconstriction and coughing and irritation of the lung mucosa

Answer 370

May cause drug output to decrease by producing foams this is more common in ultra sonic nebulisers.

Answer 371

1) propellent (inert, quite unreactive, hydrophobic). 2) drugs 3) co-solvents (e.g. ethanol) (semi polar) (sensitive to moisture uptake) 4) surfactants- reduces its surface tension, thereby increasing its spreading and wetting properties

Answer 372

1) force of emission of droplets 2) droplet size 3) where in the lung the drug deposits

Answer 373

The difference in vapour pressure and atmospheric pressure.

Answer 374

To disperse respirable particles in a suspension.

Answer 375

Oleic acid.

Answer 376

To bring the drug into solution - to achieve a homogenous distribution in the propellent.

Answer 377

From a pure drug substance - sometimes blends with lactose are prepared

Answer 378

-To act as a diluent - to help disperse the drug and act as a fluidising agent to assist dispersion. - improves flow properties of the formulation.

Answer 379

Amount of drug that reaches the alveolar region

Answer 380

By increasing the surface roughness of lactose particles. - this increases the emitted dose as the lactose can carry more drug particles.

Answer 381

1) salbutamol is SABA (max effect within 30 mins, duration of 4-6 hours), salmeterol is LABA (duration of 12-24 hours) 2) Salbutamol has faster onset of action than salmeterol. 3) Salbutamol has a smaller chain with no ether bond, whereas salmeterol has a longer chain with an ether bond.

Answer 382

Substance produced by microorganism or by chemical synthesis, that kills or inhibits the growth of other microorganism

Answer 383

Rod-shaped bacteria

Answer 384

Agents that INHIBIT growth of bacteria

Answer 385

Spherical shaped bacteria

Answer 386

A fungal pathogen that causes skin, hair, nails and mucus membranes infections

Answer 387

infection caused by a fungus

Answer 388

Preparation of anti-genetic material that can be used to stimulate the development of antibiotics and therefore cause active immunity against a disease or specific number of diseases.

Answer 389

Treatment of disease using chemical substances

Answer 390

Treatment of infection with chemical substances

Answer 391

1) trimethoprim 2) sulfonamides 3) quinolones 4) rifamycins 5) nitroimidazes 6) nitrofurantoin

Answer 392

Pteridine + (PABA)P-aminobenzoic acid Diphosphate I Dihydropteroic acid I Dihydrofolic acid I Tetrahydrofolic acid I Nucleic acid bases - between PABA and pteridine diphosphate, and dihydropteroic acid 1) enzyme: dihydropteroate synthetase 2) Drug inhibitor: sulphonamides - between dihydrofolic acid and nucleic acid bases 1) enzyme: dihydrofolate reductase 2) drug inhibitor: trimethoprim (inhibits it’s “1)”)

Answer 393

To treat a specific type of pneumonia infection that HIV and cancer patients are susceptible to.

Answer 394

Used to treat UTI’s

Answer 395

Inhibit DNA gyrase - they also prevent “re-sealing” of DNA strands, so the DNA becomes damaged - classed as bacterialcidal

Answer 396

1) fluorine atom (only one): increase activity and cellular uptake 2) basic amine group (piperidine): forms a zwitterion with COOH, Which helps pharmacokinetic aspects (e.g cellular uptake) 3) Cyclopropyl group: increases broad spectrum activity.

Answer 397

Ciprofloxacin

Answer 398

Metronidazole Effective for anaerobic infections Commonly used in dental, skin,GI and GU infections - common side effect of these types of drugs is GI irritation/disturbance.

Answer 399

Avoid alcohol

Answer 400

-Used in the treatment of alcohol dependence Works by inhibiting acetaldehyde dehydrogenase, which makes it so the toxic by-product acetaldehyde accumulates more and more

Answer 401

Metronidazole ( a type of nitroimadazole)

Answer 402

Rifampicin

Answer 403

Prevents RNA transcription by inhibiting RNA polymerase.

Answer 404

Turberculosis (TB)

Answer 405

The nitro group is reduced when the drug enters the bacterial cell wall. - this leads to the formation of a reactive species which destroys the DNA.

Answer 406

A cyclic lipopeptide, that is only active against gram positive bacteria.

Answer 407

-Binds to bacterial membranes of growing and stationary phase cells - this causes depolarisation to occur - leading to rapid inhibition of protein,DNA and RNA synthesis.

Answer 408

Only available as powder or solution for injection or Infusion

Answer 409

Inflammation of the inner lining of the hearts chambers and valves

Answer 410

In the fridge

Answer 411

1) B-lactam antibiotics (penacillin,cephlasporin,carbapenems, monobactams). 2) Glycopeptides 3) Fosfomycin 4) Polymyxins

Answer 412

Long peptidoglycan chains that are cross-linked via pentaglycine bridges.

Answer 413

Make them weaker - This is because the shape of these drugs closely resembles the shape of some bonds that are formed in the cell wall. - also prevents pentaglycine links from forming in bacterial cell walls.

Answer 414

Drug activity - By making sure the drug molecules are the correct size/shape

Answer 415

1) Natural 2) aminopenicillin 3) Anti-staphylococcal 4) Anti pseudomonal penicillin

Answer 416

- Inhibits transpeptidase - Therefore inhibits the final step in the synthesis of cell wall - Inhibits crosslinking of peptidoglycan.

Answer 417

Hydrolyses the peptide bond of the beta-lactam ring. - causing the antibiotic to become ineffective.

Answer 418

Benzylpenicillin (penicillin G) and phenoxymethylpenicillin (penicillin V) directly purified from penicillium mold.

Answer 419

Gram positive - and they are vulnerable to B-lactamases.

Answer 420

Yes - it can react with water under acidic conditions - causing the beta lactam ring to break down in a hydrolysis reaction - stomach acid is not good for this - hence the drug is administered via parenteral administration (injection or infusion.

Answer 421

Examples : Amoxicillin and ampicillin - Contain an amino group to improve physiochemical properties. - Vulnerable to B-lactamase - So are usually combined with a beta-lactamse inhibitor (amoxicillin or clauvulanic acid known as co amoxiclav)

Answer 422

Broad spectrum of activity - Gram positive and gram negative

Answer 423

Amoxicillin as it has better absorption.

Answer 424

Also known as penicillinase-resistant penicillin E.g. flucloxacillin and temocillin analogues which have big R group side chains.

Answer 425

To prevent binding of staphylococcal B lactameses - Allowing them to be at least initially effective against staphyloccoccus. - But resistance to this has developed.

Answer 426

Also known as extended spectrum penicillins examples: Piperacillin and ticarcillin (a carboxypenicillin) - Broad spectrum and are only available with beta lactamase inhibitors (e.g. ticarcillin/clavulonic acid and pipercillin/tazobactam)

Answer 427

Pivmecillinam

Answer 428

1) Cefalexin 2) Cefuroxime

Answer 429

- 3 generations first,second,third - depends on their spectrum of activity.

Answer 430

2nd gen don't penetrate CNS 3rd gen penetrate the cerebrospinal fluid when the meninges are inflamed therefore 3rd gen cephalosporins are used to treat CNS infections, such as meningitis.

Answer 431

1) carbapenems- low bioavailability 2) Monobactams - Only used to treat resistant infections - when other drugs are no longer effective - or just to overall avoid resistance

Answer 432

To deal with B-lactamase and prevent them from producing gram-negative organisms that may be resistant to penicillin.

Answer 433

Gram negative aerobic bacilli - due to an unsual spectrum of activity

Answer 434

Due to similar side chains therefore patients who are allergic to penicillin may also be allergic to cephalosporins.

Answer 435

Aztreonam As it is less immunogenic due to many differences in their structure

Answer 436

Vancomycin

Answer 437

Effects cell wall synthesis - by inhibiting peptidoglycan formation

Answer 438

Can sometimes cause nephrotoxicity(toxicity in the kidney) and ototoxicity( trouble hearing or balancing).

Answer 439

Complex and rigid structure - aromatic rings unable to rotate.

Answer 440

Allows for very specific targeting of bacterial cell walls.

Answer 441

1) peptide backbone is held by 5 hydrogen bonds with the cell wall peptide. 2) Dimerisation of vancomycin, to give a highly stable dimer, which acts as a steric shield 3) Access to transglycoside and transpeptidase enzymes is blocked.

Answer 442

-Due to modification of the cell wall precursors, -D alanine became replaced with D-lactic acid. - the loss of NH and therfore the hydrogen bond between vancomycin and the peptide weakens the binding - causing the antibiotic to become inactive

Answer 443

Teicoplanin - has similar structures to vancomycin - does not dimerise

Answer 444

Its alkyl side chain anchors itself to the cell membrane allowing it to interact with the building blocks for cell wall synthesis.

Answer 445

For serious infections caused by gram positive bacteria.

Answer 446

- inhibits first stage of intracellular bacterial cell wall synthesis by blocking peptidoglycan synthesis -- Used in the treatment of UTI's

Answer 447

- Affect the cell wall - commonly used via nebuliser - polymyxin B is used in a combo with other meds in ear and eye preparations.

Answer 448

1) tetracyclines 2) Aminoglycosides 3) Chloramphenicol 4) Macrolides 5) Oxazolidinones 6) sodium fusidate/fusidic acid.

Answer 449

Via the A site

Answer 450

Where the growing peptide chain is bound to tRNA

Answer 451

30S - And block tRNA molecules from entering the A site - Stopping the peptide chain from growing any longer.

Answer 452

Must not be given with food that contains divalent cations (e.g. Ca2+,Mg2+, Fe2+) This is because, this may cause insoluble complexes to form by chelation in the gut - reducing how efficiently the drug is absorbed

Answer 453

1) Pregnant/lactating 2) children 12 and under

Answer 454

1) Children: Tetracyclines will chelate with Ca2+ ions in bones and teeth, staining teeth yellow 2) Pregnant: Affects skeletal development in the foetus.

Answer 455

Cause the misreading of mRNA - coding for a non-functional peptide

Answer 456

Gentamicin

Answer 457

Nah - its a glycopeptide antibiotic

Answer 458

Slightly alkaline conditions e.g. pH 7.4

Answer 459

1) Ionic interaction between cell membrane and aminoglycosides results in rearrangement. 2) This produces pores, which the drug can pass through. 3) Drug trapped inside cell and it accumulates 4) Leads to selectivity.

Answer 460

1) pupurosamine 2) garosamine 3) 2-deoxystreptamine

Answer 461

- Mainly used for formulating eye drops - Inhibits transpeptidation ( stops peptide bonds form forming between peptide chain and arriving amino acids).

Answer 462

bone marrow aplasia ( cant produce enough blood cells) suppression of white and red blood cells encephalopathy optic neuritis: swelling, damages optic nerve.

Answer 463

23S (Found in the peptidyl transferase centre in the ribosome). on 50S RIBOSOME

Answer 464

- inhibits peptide bond formation by interfering with positioning of the aminoacyl of tRNA in the A site.

Answer 465

Erythromycin, azithromycin, clarithromycin

Answer 466

- inhibit ribosome translocation, stopping peptide synthesis from synthesising any further. - may also inhibit cytochrome p450 enzymes

Answer 467

Nausea/ vomiting

Answer 468

Clarithromycin as it is more stable to acid and has better oral absorption

Answer 469

50S just like chloramphenicol so they should not be administered together otherwise they will compete and be less effective.

Answer 470

Clindamycin

Answer 471

bone and joint infections such as osteomyelitis (inflammation of bone marrow).

Answer 472

Inhibits bacterial protein synthesis - by reversibly binding to isoleucyl tRNA synthase.

Answer 473

To eradicate MRSA from the nose - usually available in topical formulations.

Answer 474

Staphylococcal infections - resistance is common so course length is normally short usually given in combo with other antibiotics

Answer 475

Skin infections treated via topical route of administration

Answer 476

Sodium fusidate

Answer 477

Its functional group ( oxazolidinone ring system) binds to 50S ribosome - preventing protein synthesis from occurring.

Answer 478

Linezolid - only used under special supervision serious side effects: diarrhoea, dizziness, fainting, fever, rash.

Answer 479

1) Production of inactivating enzymes (e.g. beta lactamases) 2) Decreased accumulation of drug 3) Ribosomal alternations: Ribosomal sites become modified so they have no affinity for drugs. 4) Development of alternative metabolic pathways e.g. Sulfonamide and trimethoprim resistance occurs: when modified dihydropteroate synthetase and dihydrofolate reductase enzymes are produced, which have no affinity for drugs.

Answer 480

1) Selection: -In a population there may be resistant bacteria - drug kills all non-resistant bacteria - Resistant bacteria that remains can multiply and colonise the area. 2) Transferred resistance: -Genes that encode for resistance can be transferred and distributed throughout the population. - Resistance genes are carried on plasmids, which are transferred during bacterial conjugation. or the genetic material can be transferred through bacteriophages (which distribute plasmid DNA)

Answer 481

When bacteria transfer genetic material to one another through direct contact.

Answer 482

Eukaryotic

Answer 483

1) mycotoxin production 2) Allergens 3) Inflammation 4) Tissue invasion

Answer 484

1) True yeasts 2) Yeast like fungi 3) Moulds

Answer 485

example: cryptococcus neoformans which causes pulmonary infections and "cryptococcal meningitis". cryptococcal means spreading from lungs to brain.

Answer 486

example: candida albicans cause oral thrush and septicaemia (blood poisoning)

Answer 487

Dermatophytes - digest keratin (athletes foot, ringworm) - Aspergillus fumigatus: grows freely on airway lesions, causing pulmonary aspergillosis (mould forming in the lungs).

Answer 488

By selectively targeting the "ergosterol" that fungi produce.

Answer 489

Some may be toxic

Answer 490

Amphotericin and nystatin - interact with ergosterol in fungal cell membranes forming open pores. - cell contents are then uncontrollably lost through these pores. - fatally damaging the cell (fungicidal)

Answer 491

intravenous infusion.

Answer 492

When the kidneys ca no longer move acid, from the blood into the urine.

Answer 493

deposition of calcium salts into the kidney

Answer 494

Build up of nitrogen, creatine and other waste products in the blood /

Answer 495

1) Take a test dose 2) Carefully observe for signs of anaphylaxis for at least 30 mins.

Answer 496

This is because, it interacts with lipids and sterols of fungal cell membranes to create holes - allowing the cell contents to empty resulting in cell death

Answer 497

Its hydrophobic/hydrophilic nature - allowing a cluster of molecules to come together to create pores. - tunnel is lined with polar OH groups, which helps the polar contents of the cell to drain way.

Answer 498

Nah too toxic

Answer 499

Oral suspension that is held in the mouth for as long as possible. - provides local action to treat oral mycoses

Answer 500

1) Miconazole (powder/spray/oromucosal gel) 2) Clotrimazole( used as pessary) 3) ketoconazole (greatest systemic absorption) 4) Econazole 5) tioconazole - the last 2 are less common in practice.

Answer 501

inhibit synthesis of ergosterol - disrupting the structure of the fungal membrane. - cellular constituents then leak out into the extracellular environment.

Answer 502

Topical administration due to low oral absortipon

Answer 503

Some of the drug may still be absorbed from the Gi tract and even buccal absorption.

Answer 504

ketoconazole - therefore is used to treat systemic mycoses

Answer 505

There is a risk of hepatotoxicity when used orally. - could cause adrenal insufficiency - Ketoconazole no longer has an MA to provided orally.

Answer 506

1) Fluconazole 2) Itraconazole 3) Posaconazole 4) Voriconazole - can be administered orally - less chance of causing adrenal sufficiency than ketoconazole (an imidazole). - but can still cause hepatoxicity

Answer 507

Toxic in pregnant women - may cause heart/liver related problems.

Answer 508

An acidic environment in the stomach.

Answer 509

Label 5: "Do not take indigestion remidies 2 hours before or after you take this medicine"

Answer 510

indigestion remedies may decrease gastric acid, decreasing the absorption of itraconazole.

Answer 511

Take it with a carbonated drink e.g. non-diet cola to increase bioavailability in patients with low amounts of gastric acid ( which may be due to either disease or medication they take). - can only be used with capsule formulation.

Answer 512

Fluconazole - no Cl group so not toxic

Answer 513

Posaconazole and voriconazole - or used if other treatments don't work. - these are rarely seen in practice.

Answer 514

Caspofungin micafungin Anidulafungin

Answer 515

They work by inhibiting 1,2-beta-d-glucan synthase - which is an enzyme essential for production of cell walls in some fungi.

Answer 516

Aspergillus and candida

Answer 517

Only administered parenterally due to their large molecular size, and extensive tissue protein binding not effective against CNS infections -CNS penetration is low

Answer 518

Caspofungin - used for severe cases

Answer 519

it is converted into 5-fluororacil which inhibits DNA synthesis side effects (2): Hepatoxicity and bone marrow suppression. - Only used to treat severe infections. - not used alone due to high probability of resistance.

Answer 520

Terbinafine.

Answer 521

Available as a "nail lacquer" (nail polish) for fungal nail infections.

Answer 522

Organisms that infect other microorganisms - rely on hosts for replication - may be either single/double stranded DNA/RNA - surrounded by a protein coat (capsule/plasmid).

Answer 523

May have a lipoprotein envelope derived from host’s plasma. Membrane - which may also contain some viral glycoprotein.

Answer 524

1) Attach themselves onto host cells by using binding sites on their capsid or envelope protein, to bind to receptors. 2) Once attached, endocytosis then occurs and brings the virus receptor complex into the cell. 3) It is then uncoated by the host’s lysosomal enzymes. - Allowing viral genes to use the host’s cellular structure to produce copies of itself. 4) The mRNA produced is then translated into peptides by host cells. - these peptides can then produce enzymes. 5) RNA polymerase then produces copies of viral RNA. Other enzymes synthesise copies of viral structural proteins. - All this leads to the creation of copies being created of the original virus.

Answer 525

1) RNA retrovirus contains a reverse transcriptase enzyme 2) once inside the host cell, they will synthesise DNA from their RNA template. 3) Newly synthesised DNA is then inserted into a hosts DNA, where it undergoes transcription, to form viral RNA and viral protein coats.

Answer 526

1) Viral DNA gets transcribed into mRNA, via the host's RNA polymerase, leading to the production of viral specific proteins 2) Once viral DNA and protein coats have been produced, - virions will then be released either by lysis of the host cell or budding.

Answer 527

1) Humoral immune response (antibody mediated immunity) 2) Cellular immune response (cell-mediated immunity).

Answer 528

Recognise the same antigens on subsequent exposures. - resulting in a more rapid response, as plasma cells are formed quicker

Answer 529

1) They will proliferate to produce memory cells and cytotoxic t lymphocytes ( CD8/killer t cells), T helper cells(CD4), natural killer t cells(NK) and suppressor t cells. 2) infected cells will present the viral peptides on their surface (APC's). This is complexed with MHC molecules, which are recognised by t lymphocytes.

Answer 530

By inhibiting the presenting of MHC peptide complexes. - However, some natural killer t cells, may still attack cells with abnormal MHC expression.

Answer 531

By inducing expression of a MHC class I homologue, which is very similar to the host's MHC.

Answer 532

Yes - which causes interference with immune responses.

Answer 533

1) inhibiting viral penetration of host cells 2) inhibiting nucleic acid synthesis 3) inhibiting proteolytic enzymes (enzymes that break down proteins) 4) inhibiting viral exit of cells.

Answer 534

Oseltamivir and zanamivir - they are neuraminidase inhibitors. - inhibit influenza virus neuraminidase enzymes, which are glycoproteins found on the surface of virions. - can prevent/reduce symptoms of influenza (if administered within 48 hours of the first signs of infection). - still used to treat influenza, but are normally saved to treat more high risk patients.

Answer 535

DNA polymerase inhibitors NRTIS's (nucleoside reverse transcriptase inhibitors) NNRTI's (nucleoside non reversible transcriptase inhibitors) Protease inhibitors (PI's)

Answer 536

- Guanosine analogues. - Allows it to bind to DNA polymerase and inhibit it. This is due to its structure being so similar to guanosine.

Answer 537

As it lacks the OH group normally present in DNA bases on the 3' carbon position of the sugar ring.

Answer 538

Its a pro drug -So it is converted into it's aciclovir monophosphate by thymidine kinase. - The host cell then converts aciclovir monophosphate into aciclovir tri phosphate - inhibiting DNA polymerase and viral DNA synthesis.

Answer 539

Orally (even though absorption is low) (Valganciclovir) IV ( Side effects most common with IV administration). (Ganciclovir) Topically (skin/eye)

Answer 540

Nausea, headache, rash, nephrotoxicity (caused by drug crystallisation in the kidney).

Answer 541

The one with more polar functional groups which is famciclovir - it undergoes ester hydrolysis, to reveal the alcohol group, which is then phosphorylated. Also the purine ring under goes oxidation.

Answer 542

Low/ lack of enzyme thymidine kinase.

Answer 543

Zidovudine Abacavir (similar to guanosine) Didanosine (Similar to adenosine) Emtricitabine Lamivudine (Similar to cytosine) Stavudine (similar to thymidine) Tenofovir Disoproxil - Used in the treatment of HIV.

Answer 544

NRTI Undergoes phosphorylation into its triphosphate. - This then competes with thymidine triphosphatase as a substrate for reverse transcriptase enzymes.

Answer 545

Twice a day

Answer 546

May be partly caused DNA polymerase. Side effects: Nausea,headaches,anaemia, neutropenia.

Answer 547

Its function is to inhibit the nucleoside reverse transcriptase, which is unique to HIV. - Zidovudine lacks 3' OH group, so once it is incorporated into a DNA chain, - the chain is terminated as no other nucleotide can go on to form a new 3'-5' phosphodiester bond.

Answer 548

- Efavirenz - Etravirine - Nevirapine -Rilpivirine - Also used to treat HIV - orally administered, and have long plasma half lives). Around 50 hours. So is given once a day

Answer 549

Drugs that bind to the active site of reverse transcriptase enzymes and denature them. - These drugs are metabolised by the liver - They also induce cytochrome P450 enzymes.

Answer 550

Rash, nausea, vomiting, abdominal pain, diarrhoea, headache, fatigue, hepatoxicity.

Answer 551

Atazanavir Darunavir Lopinavir (available along with ritonavir) Ritonavir Saquinavir Tipranavir. - Also used to treat HIV

Answer 552

- mRNA is translated into polyproteins that are initially inert. - virus specific proteases then convert these poly proteins into viral proteins. - which cleave the poly proteins at certain points.

Answer 553

Drugs that inhibit the enzyme integrase Makes it so viral dna can not be injected into hosts dna - used in combination with other HIV drugs.

Answer 554

Raltegravir

Answer 555

Vaccines - catching a cold then recovering. - injecting a killed/modified microbe. It is harmless, but still antigenic. - Toxin can also be administered (A toxoid) - If host comes into contact with antigens again, then antibodies are rapidly produced. may take anywhere from a few days to a few weeks to be effective. - booster injections required in order to maintain immunity.

Answer 556

1) Live attenuated: live but weakened organisms that express antigens. 2) Inactivated vaccine: Heat-killed / chemically inactivated pathogens. 3) Absorbed vaccines: Inactivated vaccines, absorbed onto aluminium hydroxide, releasing antigenic material slowly, more antibodies produced.

Answer 557

Administering antibodies harvested from immune human/animal donors, or using in vitro engineering and cloning techniques.

Answer 558

Once adminstered antibodies have degraded naturally. - immunity lasts for around 2 weeks - can be used in emergency situations.

Answer 559

1) Exocrine glands 2) Endocrine glands ( slow to start response and have a long duration of response)

Answer 560

Secrete hormones onto epithelial surfaces via ducts.

Answer 561

Secrete hormones directly into the circulatory system.

Answer 562

In intracellular vacuoles or granules.

Answer 563

Paracrine are hormones that act on a different target cell autocrine are hormones that act on the same cell.

Answer 564

stage 1: low/high level of "thyroid hormones" is detected by the hypothalamus. stage 2: hypothalamus synthesises thyrotropin releasing hormone (TRH), which then passes onto the anterior pituitary stage 3: TRH stimulates the anterior pituitary to release thyroid stimulating hormone (TSH) into the blood. - This is detected by thyroid epithelial cells - production of T3 and T4 increases. - - This is also regulated by TSH. stage 4: Thyroid levels in the blood increase stage 5: Hypothalamus detects increasing levels of thyroid hormones in the blood. production of TRH decreases, thyroid hormone production is reduced.

Answer 565

The enzyme "thyroperoxidase" allows for the incorporation of iodide onto tyrosine residues of thyroglobulin - producing T3 and T4 within the lumen of the thyroid. - this is then endocytosed back into the follicle cell, and secreted into the blood plasma.

Answer 566

in the circulation

Answer 567

mainly found intracellularly.

Answer 568

It is converted into T3 which then interacts with a nuclear receptor, to regulate transcription of genes.

Answer 569

- stimulating metabolism - increased oxygen consumption - increased regulation of growth and development

Answer 570

D2 ( 2-deiodinase) - which is found on the ER

Answer 571

RXR-TR heterodimer (TYPE OF THYROID RECEPTOR)

Answer 572

Over reactive thyroid

Answer 573

- high metabolic rate - high temperature - sweating - tremor - tachycardia - weight loss - increase in appetite

Answer 574

When radioactive iodine is injected and taken up by the thyroid. - the radioactive decay then damages the cells - eventually leading to hypothyroidism. radio-iodine is normally used when the other drugs don't work.

Answer 575

Carbimazole

Answer 576

- reduces iodination of thyroglobulin - therefore decreasing synthesis of thyroid hormones. - works by inhibiting thyroperoxidase

Answer 577

A thyroperoxidase inhibitor - given when carbimazole is not effective.

Answer 578

Works by decreasing vascularity, of the thyroid gland. - also reduces hormone secretion. - not used as long term treatment. - normally given 10-14 days prior to "thyroidectomy"

Answer 579

Propranolol Atenolol - used to treat symptoms.

Answer 580

Type of auto-immune disease. - more immunoglobulins directed at TSH receptor - leading to an increase in thyroxine secretion. - common sign/symptom protruding eye balls.

Answer 581

Either an auto-immune or drug induced condition.

Answer 582

- low metabolic rate - slow speech - lethargic -bradycardia - sensitivity to cold - thick skin

Answer 583

Thyroid hormone deficiency since birth - leads to slow growth

Answer 584

Levothyroxine (T4) - given orally - mechanism of action: mimics the effects of endogenous hormones.

Answer 585

Liothyronine (T3) as an injection - quicker onset by doesn't last as long as T4.

Answer 586

1) Adrenal cortex- outer layer. 2) Adrenal medulla- inner layer.

Answer 587

Adrenocorticosteroids.

Answer 588

1) Glucocorticoid activity- zona fasciculata 2) Mineralocorticoid activity- zona glomerulosa

Answer 589

- they have an effect of the metabolism of carbs and protein. - also have strong anti-inflammatory effects.

Answer 590

- Affect water and electrolyte balance.

Answer 591

1) Gluco - Hydrocortisone (cortisol) 2) Mineralo- Aldosterone.

Answer 592

Cholesterol I Pregnenolone I Aldosterone, Hydrocortisone, Testosterone Oestradiol.

Answer 593

Corticotrophin releasing factor - released from the hypothalamus.

Answer 594

To stimulate the anterior pituitary - to release ACTH(Adrenocorticotrophic hormone). - which them stimulates, glucocorticoid production in the adrenal cortex.

Answer 595

hypothalamo-pituitary-adrenal axis. - process of regulating levels of steroids.

Answer 596

by the renin-angiotensin system.

Answer 597

not enough cortisol being produced to combat sudden stop of prednisolone.

Answer 598

For the production of digestive enzymes.

Answer 599

Synthesising and secreting hormones. - islets of Langerhans.

Answer 600

1) Alpha cells- secrete glucagon 2) Beta cells- secrete insulin - also secretes amylin 3) Delta cells- secrete somatostatin 4) PP cells- Secrete pancreatic polypeptide.

Answer 601

increase blood glucose Break down glycogen into glucose

Answer 602

Decrease blood glucose - by increasing uptake of glucose into tissues. - Promotes synthesis of glycogen to glucose.

Answer 603

Inhibits secretion of glucagon and insulin.

Answer 604

Amyloid peptide - delays gastric emptying (fart) - stimulates the break down of glycogen in striated muscle. ^ as a means to increase blood glucose

Answer 605

protein hormones

Answer 606

To modulate glucose metabolism by stimulating the release of insulin and also inhibiting the release of pancreatic glucagon from alpha cells. also slows down the rate of absorption of digested food (by decreasing gastric emptying).

Answer 607

Can act on muscarinic receptors to stimulate secretion of insulin.

Answer 608

Can act on alpha2 adrenoreceptors to inhibit secretion of insulin.

Answer 609

Following an increase in blood glucose: 1) Glucose enters pancreatic beta cells by the glucose transporter (GLUT2). 2) Glucokinase then phosphorylates glucose into glucose-6-phoshphate, - which is then metabolised by glycolysis and the TCA cycle. -causing an increase in ATP and decrease in ADP. 3) increase in ratio of ATP:ADP, causes the inhibition of ATP sensitive K+ channel. - causes K+ to accumulate within the cell. Slightly increasing the positive charge of the cell. - This leads to partial membrane depolarisation , causing voltage gated Ca2+ channel to open. 4) Ca2+ then moves into the pancreatic beta cells. - an increase in intracellular levels of Ca2+, stimulates EXOCYTOSIS of secretory granules containing insulin via vesicles.

Answer 610

Ultimately, results in movement of nutrients from the blood into tissues. - To meet energy demands for physical movement etc.

Answer 611

- immediate metabolic effects - recruiting glucose transporters (GLUT4) to the plasma membrane, so glucose can move into the cell. - Activation of the enzyme "glycogen synthase" to promote synthesis of glycogen. - gluconeogenesis and break down of glycogen is inhibited.

Answer 612

An insulin sensitive glucose transporter present in muscle and fat cells.

Answer 613

Kinase and phospholipase enzymes.

Answer 614

promotes gene expression - synthesis of enzymes involved in the regulation of blood glucose, cell growth and cell division.

Answer 615

1) Insulin binds to it's receptor on the target cell 2) insulin receptor consists of 2alpha and 2 beta sub units. - the beta sub units have intrinsic tyrosine kinase activity. 3) Insulin binds to alpha sub units on the extracellularly on the membrane - promoting auto phosphorylation of tyrosine residues on the intracellularly. 4) tyrosine phosphorylation of adaptor proteins occurs - examples of adaptor proteins: IRS-1 (insulin receptor substrate) which contains 22 tyrosine residues. 5) Phosphorylated tyrosine residues act as a docking sites for signalling proteins which contain SH2 domains ( such as PI3 kinase). - proteins which contain SH2 domains bind to phospho-tyrosine stuff. 6) - occupied insulin receptors aggregate into clusters, which are then internalised into vesicles. This results in down regulation of the receptor at the membrane. These receptors are then recycled back into the plasma membrane.

Answer 616

phosphorylates PIP2 into PIP3.

Answer 617

Recruits protein kinase B so it can mediate 2 signalling response mechanisms: - maintenance of blood glucose homeostasis - immediate metabolic effects of insulin

Answer 618

1) PKB signalling: to promote movement of GLUT 4 vesicles to the plasma membrane. 2) PKB phosphorylates: deactivates glycogen synthase kinase (GSK-3). - which leads to the activation of the enzyme glycogen synthase and the synthesis of glycogen.

Answer 619

T-cell mediated autoimmune response causes, - the destruction of the pancreatic beta cells that produce insulin.

Answer 620

Osmotic diuresis

Answer 621

- increased urination due to the presence of certain substances (urinary glucose and ketone bodies) in the fluid filtered by the kidney - this fluid then becomes urine - The actual osmosis process causes more water to come into the urine therefore leading to an increase in urine volume.

Answer 622

Product of metabolism of fats. - they are toxic

Answer 623

- weight loss - premature growth in kids. - low insulin levels

Answer 624

Insulin replacement

Answer 625

To avoid ketosis - which could lead to coma or be fatal if untreated - to control maintenance of blood glucose to prevent or delay onset of long term symptoms.

Answer 626

This is because it is a "peptide" and is therefore quickly destroyed in the GI tract.

Answer 627

around 10 mins to break down/ avoid toxic levels accumulating: - as enzymes inactivate it in the liver and kidney. - Also 10% of it is secreted in urine.

Answer 628

Reduces it. - insulin clearance decreases due to renal impairment.

Answer 629

2-4 hours. Note: This is for insulin therapy

Answer 630

1) Rapid acting 2) Short acting 3) Intermediate acting 4) long acting

Answer 631

- Insulin Aspart (novorapid) and insulin lispro (humalog) - onset of action is 15 mins - duration of action: 2-5- hrs - mimics the effects of insulin to cope with a meal. - administered before or after a meal.

Answer 632

- soluble insulin (Actrapid) - Onset of action is 30-60 mins - duration: up to 8 hrs - Administered 15-30 mins before a meal via injection.

Answer 633

- isophane insulin (insulatard, humalin I) - Suspension of insulin with protamine - onset of action: 1-2 hrs, max effects: 4-12 hrs Duration: 16-35 hours injected once or twice daily.

Answer 634

- Insulin zinc suspension: Insulin Glargine (Lanctus) (Injected once a day). Insulin Detemir (Levemir) (Injected twice a day). - Finely divided solids which are injected as a suspension, which insulin is slowly absorbed. - reaches a steady level after 2-4 days.

Answer 635

Rarely used - as it may bind with soluble insulin when mixed in the same syringe.

Answer 636

Either rapid or short acting mixed with intermediate acting insulin Example: NovoMix ( 30% insulin aspart, 70% insulin aspart protamine).

Answer 637

- Sterility - stability ( of API in water) - Isotonicity ( API/excipient concentration). - pH ( if pH isn't right may cause changes at the site of administration such as irritation. - Local effects: May cause "local effects" at the site of injection.

Answer 638

often if solubility isn't great it is overcome using other solvents, to formulate the product as a powder for reconstitution prior to admin.

Answer 639

Lys and pro are switched - allowing it to act rapidly, but for a shorter time than natural insulin.

Answer 640

Asparagine is substituted with a glycine on the A chain. - to provide a constant basal supply off insulin.

Answer 641

Substitution of Pro 28 to Asp. Reduces it's tendency to form hexamers, giving it a higher rate of absorption.

Answer 642

Insulin resistance and impaired insulin secretion

Answer 643

1) Down regulation: loss of insulin receptors from the cell surface. 2) Impaired signalling mechanisms: which recruit GLUT-4 (impaired signalling to glut-4) so glucose can not bind to it and enter cells.

Answer 644

1) high sugar and carbs, causes high levels of insulin. 2) Tissues become unresponsive to insulin due to 2 things: Down regulation and impaired signalling mechanisms. 3) insulin sensitive tissues become unresponsive and resistant to insulin. 4) Pancreatic Beta cells produce more insulin in attempt to increase glucose uptake into cells, resulting in "hyperinsulinemia" 5) Eventually, pancreatic beta cells become depleted of insulin causing impaired insulin secretion.

Answer 645

impaired glucose tolerance Pre diabetic state of hyperglycaemia. Above normal levels of both blood glucose and insulin after a glucose test.

Answer 646

large quantity of glucose given as an oral solution to drink. - level normally observed after 2 hours.

Answer 647

- reduces hepatic glucose production (gluconeogenesis). - also increases uptake of glucose and utilisation in skeletal muscle. - reduces absorption of carbohydrates - reduces levels of LDL and VLDL. low density lipo protein very low density lipo protein

Answer 648

1) Anorexia 2) Diarrhoea 3) Nausea 4) GI-related effects

Answer 649

Lactic acidosis - more likely in patients with reduced drug elimination

Answer 650

Heart patients

Answer 651

- stimulating insulin secretion, reducing plasma glucose. - action on the pancreatic beta cells - so it is only effective if there are functional beta cells available. - not used in t1dm or late type 2

Answer 652

SUR1 receptors present on the ATP sensitive potassium channel in the pancreas. - sulfonylureas block the output of potassium channels. - which results in partial membrane depolarisation, triggering the activation of Ca2+ channels. ^ entry of Ca2+ and exocytosis of secretory granules containing insulin.

Answer 653

- well tolerated - most common side effect is hypoglycaemia ( dependedn ton the specific one given)

Answer 654

Due to their reduced renal function this also applies to patients with renal impairment.

Answer 655

1) Tolbutamide - lowest potency and duration (6-12hrs) 2) Glipizide- medium potency and duration (16-24hrs) 3) Glibenclamide- highest potency and duration (18-24hrs)

Answer 656

1) Pioglitazone- however, associated with increased risk in heart failure so not to be used in heaert patients. 2) Rosiglitazone: the MA for this has been withdrawn.

Answer 657

- bind to the nuclear receptor PPAR ( proliferator activated receptor) - After ligand binding, PPARs form heterodimers with retinoid X receptor alpha (RXR-a). - Then undergo a conformational change, which facilitates binding to "peroxisome proliferative response element (PPRE) in the enhancer regions of target genes.

Answer 658

1) reduce insulin resistance in inuslin sensitive tissue: by increasing transcription of GLUT-4 glucose transporters, therefore ccausing uptake of gluccose to increase. 2) Reduce hepatic glucose output 3) Reduction of fatty acid as an energy source: increases utilisation of glucose. 4) Reduction in small dense LDL - Slow onset of effect maximal effect is around 1-2 months after treatment.

Answer 659

Acts on PPAR in adipocytes, promoting adipogenesis.

Answer 660

-Due to enhanced expression of genes that regulate fat metabolism, and fluid volume unwanted side effects: 1) Weight gain- due to differentiation of adipocytes and increase in lipogenesis. 2) Fluid retention- due to reabsorption of NA+ in the renal collecting ducts. causing plasma vol to increase up to 500ml, and also a reduction in haemoglobin conc.

Answer 661

fat laden cells accumulate as adipose tissue

Answer 662

Metabolic formation of fat from glucose.

Answer 663

Inhibits the enzyme glycoside hydrolase (glucosidase). - leading to delay in absorption of carbs - reducing the increase in blood glucose after a meal.

Answer 664

- loose stool - fart - diarrhoea - abdominal pain/bloat

Answer 665

Example: exenatide incretins are peptides that stimulate pancreatic beta cells to secrete insulin. - incretins also inhibit pancreatic glucagon secretion from alpha cells. - They also slow the rate of absorption of digested foods, by decreasing gastric emptying. administered via injection just like insulin, as it is a peptide

Answer 666

GLP-1 receptor agonists Glucagon-like peptide-1 - also used for management of weight gain. the drug recommended for this is semaglutide

Answer 667

1) Enhancing glucose dependent insulin release from pancreatic B cells 2) inhibiting glucagon from pancreatic alpha cells 3) Slowing gastric emptyinng, delaying absorption of carbs after a meal and metabolism 4) Acting as a appetite suppressant, reducing consumption of carbs.

Answer 668

As they are glucose dependent, so insulin only releases when levels of glucose is high, and less when levels are normal.

Answer 669

Dipeptidylpeptidase-4 inhibitors (DDP4) They are added as agents to orally active drugs and are well tolerated and don't affect weight much.

Answer 670

Potentiate incretins by competitively inhibiting an enzyme that breaks down incretins.

Answer 671

Sodium glucose transporter 2 inhibitor.

Answer 672

Inhibits SGLT-2 in the proximal convoluted tubule of the kidney, preventing reabsorption of glucose and also helping it's excretion of glucose in urine. Glucose is excreted, causing plasma level to decrease.

Answer 673

This is because their mode of action relies upon normal glomerular-tubular function.

Answer 674

In patients with renal impairment.

Answer 675

Sever lack of insulin levels. - cant use glucose as an energy source - so fat stores are used instead. - Also causing ketones to be released.

Answer 676

1) Na+/K+ ATPase pump removes Na+ from S1 segment renal proximal tubule. 2) SGLT-2 causes Na+ to move down it's concentration, causing glucose to move into S1 segment renal proximal tubule. 3) Glucose is then reabsorbed into the blood via GLUT-2. 4) SGLT-2 inhibitors then inhibit SGLT-2 in the proximal convoluted tubule of the kidney, to prevent reabsorption of glucose and facilitate excretion of glucose in urine. 5) As glucose is excreted in urine, levels of plasma glucose decreases.

Answer 677

1) Oestrogen 2) Progesterone

Answer 678

- They passively diffuse into the cell and bind to their cognate receptors either in the cytoplasm or nucleus.

Answer 679

1) ER alpha 2) ER beta - they have different tissue distributions.

Answer 680

1) PR-A 2) PR-B

Answer 681

- interacts with nuclear receptors - upon ligand binding, receptors dimerize and translocate to the nucleus, causing transcription of target genes. - also non genomic actions.

Answer 682

Hypothalamic-pituitary-gonadal-axis.

Answer 683

When the superficial layer of the endometrium is shed.

Answer 684

1) Menstruation 2) Follicular phase 3) Proliferative phase 4) Luteal phase

Answer 685

- endometrium regenerates after menstrual flow stops. - Gonadotrophin releasing hormone (GnRH) is secreted from the hypothalamus, which stimulates the anterior pituitary to release follicle stimulating hormone (FSH) and luteinising hormone (LH). - FSH and LH then act upon ovaries, causing a small group of follicles to form (each contain an ovum (egg)) . - One follicle develops faster than the rest, this is known as the "graafian follicle" (GF) - which then secretes oestrogen.

Answer 686

- Oestrogen help regenerate the endometrial ( from day5/6 - mid cycle). - thickness and vascularity of the endometrium then increases. - at peak oestrogen levels, there is a cervical secretion of mucus (which contains high amounts of proteins and carbs, facilitating entry of sperm into ovum). - high secretion of oestrogen just before mid-cycle, then stimulates the release of LH. - causing rapid swelling and rupture of graafian follicle, causing ovulation. - if fertilisation occurs at this stage, then the fertilised ovum passes down the fallopian tube to the uterus.

Answer 687

Swelling and rupture of graafian follicle. due to release of oestrogen and LH

Answer 688

- The ruptured graafian follicle proliferates and develops into the corpus luteum, which then secretes progesterone. - Progesterone then acts on oestrogen primed endometrium, allowing it to become suitable for implantation of fertilised ovum. Cervical mucus thickens to hinder sperm. - Progesterone then exerts negative feed back on the hypothalamus and pituitary, causing release of LH to decrease.

Answer 689

Progesterone secretion stops at the end of the cycle, triggering menstruation. - Also the corpus luteum keeps on secreting progesterone causing negative feed back: preventing further ovulation.

Answer 690

combo of synthetic oestrogen with synthetic or natural progesterone. - high levels of synthetic oestrogen and progesterone, prevent the exact cycle of hormonal events of the menstrual cycle occurring.

Answer 691

Combined oral contraceptive pill

Answer 692

- 2nd gen has lower oestrogen count than the 1st gen.

Answer 693

They contain modified progestogens ( which have less adrenergic activity). examples: desogestrel, gestodene

Answer 694

2nd gen safer as 3rd gen has a greater risk of thromboembolism than 2nd gen. - which is a blood clot forming in a vein.

Answer 695

for 21 days in a row ( out of 28 days) - then pill free until the 28th day ( to enable withdrawal menstrual bleed).

Answer 696

When there are placebo pills to be taken from day 22-28

Answer 697

Oestrogen Inhibits the release of FSH Progesterone inhibits the release of LH. - Lack of follicle development, causes cervical mucus to become inhospitable to sperm.

Answer 698

Weight gain nausea - reversible hypertension- due to an increase in plasma renin due to oestrogen production. - blood pressure monitoring is advised. - Thromboembolism (3rd gen pill)

Answer 699

- decrease chance of irregular periods and inter-menstrual bleeding. - reduces heavy menstrual bleeding and pain.

Answer 700

Progesterone only pill - Makes cervical mucus thicker and more hostile to sperm. - also development of endometrium

Answer 701

POP taken every day with no break.

Answer 702

POP as it is less reliable at low doses. - Also irregular bleeding is more common

Answer 703

When they can develop risk of hypertension, cardiac related problems, thromboembolism.

Answer 704

- metabolised slower than natural oestrogen/ progesterone - have a longer half life - greater bioavailability - they are also less susceptible to first-pass metabolism.

Answer 705

Cytochrome p450

Answer 706

movement of bile acid from liver to small intestine and then back to the liver.

Answer 707

It is ideal to minismise the dose of oestrogen ( to avoid thromboembolism) - HOwever increase in clearnace of COCP or POP may lead to contraception fail. - symptoms of increased clearance of COCP/POP : vomitting, diarrhoea

Answer 708

- reduced efficacy and also contraceptive fail

Answer 709

- anti-convulsant - anti-retroviral - antibiotics This is because they increase they are "enzyme inducing drugs", that increase the potency of cytochrome p450 enzymes, and therefore the clearance of COCP/POP.

Answer 710

No longer suitable to bear a child, - generally occurs when there is no period bleeding for a year.

Answer 711

Process of change that leads to menopause.

Answer 712

low levels of oestrogen due to depletion of ovarian follicles. - progesterone levels also decrease if ovulation does not occur.

Answer 713

- hot flushes - night sweats - osteoperosis

Answer 714

Tibolone - also prevents osteroperosis and bone loss. - but can cause menstrual bleeding - so not used within 12 months of last period.

Answer 715

Synthetic compound with weakly oestrogenic and androgenic properties.

Answer 716

Selective oestrogen receptor modulator

Answer 717

Raloxifene induces anti-oestrogenic effects on breast tissue and uterus - but is pro-oestrogenic on the bone and lipid metabolism. - helps to prevent osteoporosis.

Answer 718

Hormonal replacement therapy - involves continuous administration of low doses of one or more oestrogens, with/without a progesterone - progesterone prevents endometrial associated risks as well as ovarian cancer. - helps treat the vasomotor symptoms associated with meno pause(sweating, hot flushes) - however does not reduce risk of coronary heart disease or abnormalities in cognitive function.

Answer 719

Stroke thromboembolism (venous) Endometrial cancer ( that can be treated with progesterone) breast cancer, ovarian cancer - increased risk of coronary heart disease if HRT is started 10 years after menopause

Answer 720

kisspeptin neurokinin B (NKB) Dynorphin - interact to affect pulsatile release of GnRH

Answer 721

Stimulates the release of FSH and LH

Answer 722

can cause an increase in the neuronal size of kisspeptin and gene expression and hypertrophy of arcuate nucleus also increase in NKB expression in post menopausal peeps.

Answer 723

increase in number and size of muscle cells

Answer 724

less negative feed back from osestrogen, causes increased kisspeptin and NKB signalling - resulting in hypersecretion of GnRH.

Answer 725

- KNDy neurons project axons to the MnPO (median preoptic area of hypothalamus) - Then receiving and projection of input is directed to the thermoregulatory pathway via the MnPO nucleus.

Answer 726

A hub for thermoregulation receiving input and projecting input to thermoregulatory pathway. - Also expresses the primary receptor for NKB

Answer 727

Fezolinetant (Veozah) given once daily as a non-hormonal pill

Answer 728

Antagonises NKB at neurokinin-3 receptors

Answer 729

To process food and water and extract nutrients and get rid of waste

Answer 730

API in a liquid vehicle for oral administration

Answer 731

1) Great patient compliance 2) Great absorption 3) Less GI irritation 4) No "drying step" required in the manufacturing process (lower cost) 5) Solutions do not undergo phase separation.

Answer 732

1) Doesn't mask taste well 2) susceptible to microbial contamination 3) Dose uniformity issues (emulsions, suspensions) 4) Hydrolysis of API 5) Not as convenient as tablets or capsules 6) Hard to transport large bottles of liquid - and hard to pack glass bottles (risk of breaking)

Answer 733

A solution is a homogenous mixture that usually contains one or more solutes, dissolved in a suitable solvent ( such as water).

Answer 734

This is because solutions do not have to undergo disintegration and dissolution whereas tablets have to

Answer 735

1) API 2) vehicle 3) Co-solvent ( to improve solubility) 4) Buffer ( form maintaining optimum temperature 5) Sweeteners, colours, taste masking and flavouring agents 6) Preservatives 7) Anti-oxidants

Answer 736

Aqueous solutions which contain high quantity of sugar/ sweetner

Answer 737

85% or more

Answer 738

Resistant to microorganism due to low water content.

Answer 739

- Preservatives are kept to a minimum due to osmotic effects or high sugar conc. And reduce crystallisation - polyhydric alcohols may be used to maintain solubility acting as co-solvents.

Answer 740

1) Sorbitol 2) Glycerol 3) Propylene glycol

Answer 741

This is to avoid microorganism growth.

Answer 742

Crystallisation can form around the cap - this can form a solid plug stopping the syrup from flowing . - To minimise crystallisation of syrups: - polyhydric alcohols are used as well as invert syrup (glucose fructose mixture)

Answer 743

A sweetened solution of API in a mixture of water and ethanol ( 12-15%).

Answer 744

Elixirs have a lower conc of sugar than syrups. They are also less viscous - however less able to mask taste.

Answer 745

Alcholic or hydroalcoholic solutions containing API or extracts from plant materials. Alcohol content is roughly 15-80% - They are flammable - also avoid high temps

Answer 746

- often used when API is hydrophobic, when API is unstable in aqueous solution. - unpleasant taste and feel in mouth - However oil based solutions help prolong drug release

Answer 747

Due to high mobility Decreased potency of drugs as well as chance of less toxicity.

Answer 748

A dispersion of solid within a liquid of gas used for low soluble drugs

Answer 749

1) Course suspension (particles greater than 1um) 2) colloidal dispersion (Particles lower than 1 um).

Answer 750

1) API 2) Wetting agent 3) Suspending agents 4) Flocculating agents 5) Preservatives 6) Sweeteners 7) Flavours 8) Colourants

Answer 751

Form a coating around the API and act to reduce surface tension and facilitate wetting and therefore dispersion/ dissolution. This is because drugs with hydrophobic surfaces are difficult to disperse in aqueous medium

Answer 752

INcrease viscosity of the medium and slow down sedimentation. usually gums, cellulose derivatives.

Answer 753

prevent flocculation and neutralise the high charge density of certain particles

Answer 754

Due to large surface area of dispersed particles

Answer 755

When particles of a liquid suspension form relatively weak bonds to create loose, light fluffy flocs, held together by weak van der waal forces of attraction. - overtime these vdw forces of attraction will thicken to form a thick layer of sediment.

Answer 756

When particles of a liquid suspension are held together by strong inter-particle forces and aggregate - Aggregation leads to crystallisation, forming a thin solid layer of precipitate (cake/caking)

Answer 757

The ones that aggreagete - the ones that floc are cool tho

Answer 758

1) Increase API bioavailability 2) Increased drug stability compared to aqueous solutions 3) Prolonged drug action: Oil reserve acts as a reservoir, where API slowly partitions into aqueous phase for absorption.

Answer 759

1) Thermodynamically unstable, leading to possible flocculation, coalescence or breaking 2) more complex to formulate than other solutions

Answer 760

in a pharmacy energy is added via trituration (mixing and grinding components) In manufacturer this is done by a homogeniser (mixer)

Answer 761

1) oil in water emulsion 2) Water in oil emulsion 3) Multiple emulsions: Water in oil in water oil in water in oil

Answer 762

An emulsion is a system, that consists of two immiscible liquids (where one phase is polar and one phase is non polar), where on liquid is dispersed within the other liquid as small globules, and usually stabilised by an emulsifier.

Answer 763

1) Ability to formulate hydrophobic API into a liquid. 2) more stable than solutions 3) Prolonged drug action- as api slowly partitions into the aqueous phase.

Answer 764

1) Thermodynamically unstable 2) Harder to formulate than formulating a solution.

Answer 765

An agent added to an emulsion to stabilise it

Answer 766

1) coalescence 2) Flocculation 3) Creaming 4) Breaking (cracking)

Answer 767

Dispersed droplets merge together to form large particles. irreversible process and leads to breaking

Answer 768

Dispersed particles form weak interactions with each other, forming flocs within the continuous phase.

Answer 769

Upwards movement of dispersed droplets, leading to phase separation. reversible by gentle mixing.

Answer 770

Could cause an increase in coalescence

Answer 771

complete separation of an emulsion into its component phases.

Answer 772

Weight / height ^2

Answer 773

Nasogastric administration or if not possible than either oesophageal surgery or a peg or pej

Answer 774

Iv administration of a nutritionally balanced and physiochemically stable and sterile combination of the six main groups of nutrients with water (fatty acids, amino acids, glucose, vitamins and electrolytes, trace elements).

Answer 775

IV admin via a central vein allowing the nutrients to be delivered into the superior vena cava or the right atrium.

Answer 776

1) Passes directly into systemic circulation. 2) Bypasses the GI tract and avoids first pass metabolism by the liver.

Answer 777

1) when there is intestinal failure 2) patients with fever 3) underweight infants

Answer 778

1) Triglyceride 2) Sterols 3) phospholipids

Answer 779

A,D,E,K water soluble vitamins: C,B

Answer 780

- large blood supply - haemorrhoidal veins drain into the inferior vena cava, avoiding first pass metabolism.

Answer 781

it melts at body temp dissolution of suppository base in surrounding fluids dispersion of suppository base in surrounding fluids.

Answer 782

1) Systemic absorption 2) Can be used in unconscious patients, or patients nil by mouth 3) no GI irritation, and first pass metabolism.

Answer 783

1) Unacceptable to some patients, or they may refuse 2) Difficult to administer to certain types of patients, such as elderly

Answer 784

1) Fatty hydrophobic bases 2) Water- soluble hydrophilic bases.

Answer 785

1) Must melt at body temp 2) able to dissolve in rectal fluid 3) should have a narrow melting point 4) must be chemically and physically stable 5) should be compatible with api

Answer 786

1) Viscosity enhancer 2) Surfactants

Answer 787

An enma used to stimulate bowels to treat constipation - vol reaches up to 2 litres - should be warmed to body temp b4 admin

Answer 788

An dosage formed retained in the rectum, for to either provide treatment locally or systemically. - vol not higher than 100ml

Answer 789

1) Parietal cells secrete HCl into the lumen of the stomach. 2) H+/K+ ATPase pump, pumps H+ ions into the stomach lumen. This proton pump is regulated by ACh, gastrin and histamine

Answer 790

1) Vagus nerve releases ACh, stimulating m1 muscarinic receptors on parietal cells 2) Food enters stomach, and proteins in the stomach wall trigger the release of gastrin from G cells. 3) Gastrin stimulates its receptors on parietal cells, 4) This causes an increase in intracellular concentration of Ca2+ ions, causing H+/K+ ATPase pump to activate. 5) Stimulation of muscarinic and gastrin receptors on paracrine cells cause the release of histamine. 6) This stimulates h2-histamine receptors on parietal cells, increasing the intracellular concentration of cyclic AMP.

Answer 791

Hyperacidity, indigestion, bloating, heart burn

Answer 792

- When lower oesophageal sphincter does not close properly - HCl could affect the linin of the oesophagus, causing a burning sensation. usually treated using antacids

Answer 793

Neutralise gastric acid in the stomach lumen causing pH to increase. - also less gastric production, could cause more gastric acid to be produced. (acid rebound)

Answer 794

1) Sodium bicarbonate: 2) Magnesium hydroxide 3) Aluminium hydroxide

Answer 795

- rapid action - CO2 it prooduces, stimulates the relase of gastrin. - NaHCO3 can cause sytemic alkalosis, and is not receommended for patients trying to cut down on sodium intake.

Answer 796

- insoluble in water unlike sodium bicarbonate - rapid reacts with hcl - low chance of alkalosis - can produce a laxative effect

Answer 797

- not well absorbed from the intestines - tendency to cause constipation - slowly reacts with hcl

Answer 798

Magnesium hydroxide and aluminium hydroxide

Answer 799

- increases mucus viscosity - increasing it's adherence to intestines mucosa -

Answer 800

Proton pump inhibitor Histamine h2 antagonist (cimetidine and ranitdine)

Answer 801

- dizziness - diarrhoea - rashes

Answer 802

lansoprazole omeprazole they are pro drugs that activate are low ph

Answer 803

-Reversibly bind to histamine h2 receptors on gastric parietal cells -inhibiting activity of histamine -reducing gastric acid secretion.

Answer 804

-Irreversibly bind to proton pumps -inhibiting proton pumps on parietal cells -precenting gastric acid secretion,

Answer 805

- once it enters acid environment the drug becomes protonated - This protonation triggers an acid catalysed conversion, which activates the drug. - then binds irreversibly to cysteine residues. Blocking pump, preventing release of HCl, to stop PPI's from being further activated.

Answer 806

Attaches to a sugar molecule in stomach and uses mucus layer as protection.

Answer 807

1) Uses flagella to migrate through alkaline mucus. 2) settles in antrum of stomach, where there is no parietal cells. 3) produces urease, breaking down urea, to produce ammonia. Ammonia then neutralises HCl.

Answer 808

by producing inflammatory toxins, that break down the gastric mucosal barrier - causing a greater chance of pepsin and gastric acid to come into contact, causing stomach wall damage.

Answer 809

Proton pump inhibitor along with 2 antibiotics for one week

Answer 810

if not given on an empty stomach they would react with dietary proteins and will not function effectively

Answer 811

1) blacken teeth 2) blacken tongue 3) blacken faeces 4) nausea, vomiting

Answer 812

- diarrhoea - abdominal cramps - uterine contractions.

Answer 813

Form protective barrier over an ulcer, preventing it from being damaged by gastric acid.

Answer 814

1) Bulk forming laxatives: bulks out intestinal contents with polysacchrides, inducing peristaltic movement. 2) Osmotic laxatives: bulk out intestinal contents with water, helps soften stool. Keep hydration levels up with this 3) Stimulant laxatives: Stimulate mucosa to produce intestinal movements. side effects: intestinal cramps/damage 4) Faecal softeners: soften faeces

Answer 815

As an attempt to flush out microbes, more fluid and electrolytes are being lost than they are absorbed. - leading to dehydration, and electrolyte imbalance.

Answer 816

oral rehydration therapy

Answer 817

Oral solutions of glucose and electrolytes are administered - Works by absorbing na+ ions and glucose, and water follows these absorbed ions by osmosis.

Answer 818

- lipophilic - slowly absorbed - prone to me - can not cross BBB

Answer 819

kaolin - adsorbs microbes and toxins - and coat and protect intestinal mucosa - or adsorb excessive fluid in the bowel, to reduce diarrhoeal symptoms.

Answer 820

As an oral suspension or as a mixture with other drugs like morphine.

Answer 821

Orlistat inhibits lipids and fat from being digested reduces lipid absoprtion reducing calorie intake.

Answer 822

Increase excretion of fat in faeces. abdominal cramps bloating

Answer 823

feel like gonna vomit

Answer 824

Chemoreceptor trigger zone

Answer 825

Detects stimulus of by communicating with the "vomit centre" vomit and monitors chemical composition of blood - also receives signals from eyes and ears

Answer 826

1) Limbic cortex 2) nucleus solitarius: involved with gag reflex 3) Spinal cord: involved with nausea due to physical injury.

Answer 827

1) Reversal of peristalsis in small intestine, intestinal contents and bile enters stomach 2) glottis closes 3) Breath held 4) Oesophagus and gastric sphincter relax 5) Contraction of abdominal muscle to eject stomach contents.

Answer 828

Drugs given to prevent vomit These include: 1) Antimuscarinic 2) H1-histamine receptor antagonists 3)Dopamine d2 receptor antagonists 4)5-hydrroxytryptamine receptor antagonists 5) Cannabinoids 6) Substance P antagonists 7) Glucorticoids

Answer 829

No drugs given to prevent harm to foetus

Answer 830

Antagonises muscarine receptors on the vomiting centre. - prevent/reduce motion sickness example: Hyoscine (scopolamine)

Answer 831

Cyclizine (promethazine) antagonises h1 receptors on the vomit centre. - treat nausea and vomit and motion sickness.

Answer 832

Phenothiazines (prochlorperazine, metoclopramide, domperidone). - block dopamine d2 receptors on the CTZ. - and antagonise muscarinic and histamine receptors.

Answer 833

Yes - so could cause centrally mediated side-effects.

Answer 834

reduces cytoxic induced vomiting - drowsiness -hypotension

Answer 835

1) Abdominal pain and cramping 2) Change in bowel habits: constipation, diarrhoea 3) bloating 4) flautulence 5) incomplete bowel emptying.

Answer 836

1) Chron's disease: affects GI tract 2) Ulcerative colitis: affects large bowel (rectum and colon)

Answer 837

- diarrhoeal symptoms treated with anti-diarrhoeas. - and advised to eat low fat diet - glucocorticoids used to induce remission.

Answer 838

- 5- aminosalicylate (e.g. sulfasalazine). - if no response to this, then immosupressants (methotrexate, azathioprine).

Answer 839

- treated with amino salicylate. - steroids can be administered in combo with amino salicylates.

Answer 840

involves IV admin of hydrocortisone and ciclosporin.

Answer 841

suppository

Answer 842

Arterial disease where arteriosclerotic plaque develops in luminal walls.

Answer 843

1) Endothelial cell is damaged, monocytes form macrophages in arterial walls. 2) This causes free radicals to be produced, these free radicals oxidise LDL. 3) macrophages take up this oxidised LDL forming foam cells, which causes the release of inflammatory cytokines. 4) Foam cells form fatty streaks releasing growth factors. 5) Causes smooth muscle to develop, forming plaque. 6) Rupture of plaque causes thrombosis.

Answer 844

Hmg CoA reductase

Answer 845

Hmg Co A - > mevalonic acid -> farnesol -> cholesterol Hmg CoA reductase

Answer 846

atorvastatin lovastatin simvastatin - lower cholesterol

Answer 847

Inhibits hmg co a reductase prevents substrate from binding, inhibiting the conversion of HMG Co A reductase to mevalonic acid, preventing synthesis of cholesterol

Answer 848

Headache Dizziness Nausea Muscle pain Rashes

Answer 849

usually at night to reduce peak cholesterol synthesis during the day

Answer 850

Reduce LDL and increase HDL Stimulating lipase, reducing triglyceride content o VLDL’s.

Answer 851

Clofibrate

Answer 852

Nauase Upset stomach Diarrhoea

Answer 853

Colestipol (divided powders)

Answer 854

1) bind to bile, preventing reabsorption 2) cholesterol, causes more bile acid to be produced 3) increases demand of cholesterol, increases hepatic LDL receptor expression 4) causes increase in LDL cholesterol clearance

Answer 855

- interfere with absorption of fat soluble viatamins - GI irritation

Answer 856

Reduces delivery of cholesterol to the liver Promoting synthesis of LDL receptors with low levels of LDL-C.

Answer 857

Stomach pain Diarrhoea Muscle pain Joint pain

Answer 858

Thickening of ,muscle layer of arterial walls, narrowing arteries

Answer 859

Build up fat cholesterol and plaque in arterial walls, narrowing arteries.

Answer 860

Under 55: ACE inhibitor Over 55: calcium channel blocker Then A + C Then A,C +D Then: thiazide like diuretic or alpha/beta blocker.

Answer 861

Could cause diabetes

Answer 862

Lower BP vasodilation

Answer 863

Anything ending in @opril@ - captopril - perindopril

Answer 864

Prevents formation of angiotensin’s 2 - preventing blood vessels from being narrowed - lowering bp

Answer 865

- dry cough - hyperkaelaemmia - dizziness - headache

Answer 866

As ace inhibitors inhibit break down of bradykinin Causing it to accumulate in lungs Causing dry cough. - so ARBs may be given instead

Answer 867

Losartan Valsartan

Answer 868

Does not inhibit breakdown of bradykinin

Answer 869

Blocks action of angiotensin 2 Lowering bp

Answer 870

Hyper kaelaemia Dizziness Diarrhoea Headache Cough

Answer 871

Amlodipine Diltiazem

Answer 872

Blocks calcium channel Decreasing vascular force Less calcium to react with cal modules Peripheral resistance decreases Lower bp

Answer 873

Headache Dizziness Arrythmia Nausea Chest pain Constipation

Answer 874

- slows down sa and increases av node contraction - slowing heart rate

Answer 875

To avoid Brady cardia and hypotension

Answer 876

Doxazosin Prazosin

Answer 877

Blocks alpha 1 receptors so norepinephrine can not bind to them. Causing vasodilation Lowering bp

Answer 878

Blocks alpha 1 receptors so norepinephrine can not bind to them. Causing vasodilation Lowering bp

Answer 879

Dizziness Headache Postural hypotension- due to impaired arteriolar vasoconstriction when standing up.

Answer 880

Minoxidil, hydralazine ^ Vasodilator Side effects: tachycardia

Answer 881

Beta blockers

Answer 882

Beta blockers

Answer 883

Co = Hr x sv

Answer 884

Non selective: propranolol: blocks b1,b2 Selective: atenolol, bisoprol: blocks b1

Answer 885

Block adrenaline and noradrenaline Reducing peripheral resistance

Answer 886

Dizziness Cold hands/ feet Nausea

Answer 887

Carvedilol - avoided for diabetes patients, as may affect carbs metabolism - amide group- increases water solubility

Answer 888

- bronchospasm - bradycardia - fatigue -

Answer 889

Methyldopa

Answer 890

Increase urine of vol produced More water excreted Circulatory volume decreases

Answer 891

Indapamide Chlorthalidone

Answer 892

Large vol of blood in veins

Answer 893

Morning To avoid sleep disturbance

Answer 894

- increased cholesterol levels - impaired glucose tolerance

Answer 895

Inhibit salt absorption in the thick ascending limb of loop of henle

Answer 896

Furosemide - reduces oedema

Answer 897

Low k+- hypokaelamia High ca2+- hypercaelaecim

Answer 898

Blocks Na+ channel - reducing an+ absorption, preventing hypokaelamia

Answer 899

Amiloride Triamterene - ACE and Arbs not used with these - as it reduces aldosterone levels - leading to adrenal insufficiency

Answer 900

Stable and unstable angina

Answer 901

Less blood flow to myocardium Low supply of o2 to cardiac muscle

Answer 902

Less blood flow to myocardium Low supply of o2 to cardiac muscle

Answer 903

Predictable Stable levels of coronary blood supply during rest Unstable levels during exercise - supply of blood does not meet demand, causing ischaemia

Answer 904

Acute coronary syndrome (ACS) - rapid onset - pain occurs at rest - longer duration and more severe sysmptoms Caused by atherosclerosis plaque, leads to thrombosis.

Answer 905

Chest pain

Answer 906

Chest pain Tight chest Shortness of breath Sweating

Answer 907

Nitrates: nitroglycerin Glyceral trinitrate (GTN): to treat chest pain Sublingual tablet/spray- duration 30 mins

Answer 908

Nitrates cause venodialtion - less venous return - reduced cardiac pressure loading, work load on heart and o2 demand.

Answer 909

Venous pooling of blood

Answer 910

1) nitrates convert into nitrous oxides 2) guanylyl cyclise converts GTP into cGMP 3) causes Ca2+ ions to be taken up into sacroplasmic reticulum.

Answer 911

Air: air tight containers Heat: not put in trousers Moisture: packaged with a desiccant Light: amber glass bottles.

Person centred care: Disease, medicines and patients Flashcards

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