Drugs

Question 1

Acetylcholine esterase inhibitors

Answer 1

Useful in alzhiemers patients to increase electrical activity in the brain
Prevents the break down of Ach into choline and acetate.
Increases neuronal transmission by increasing the level and duration of neural transmission

Question 2

Adalimumab

Answer 2

Monoclonal antibody
Inhibits the effects of TNFa, prevents binding to p55 and p57 receptors.
Decreases leukocyte migration, decreases epidermal thickness, causes apoptosis in cells with TNF aplpah receptors, inhibits the release of IL-6 and acute phase proteins.
Useful in decreasing inflammation such as in rheumatoid arthiritis

Question 3

Adenosine

Answer 3

Used to decrease HR
Binds to A1 receptors on the heart, this is an inhibitory GPCR, inactivates adenylate cyclase reducing cAMP production this decreases calcium ion influx and increase postassium ion efflux leads to decrease action potential generation in conductile cells
Binds to A2 receptors - antagonist of wake signals
Binds to A2a receptors - agonist of sleep
A2 and A2a are found in the brain

Question 4

Amoxicillin

Answer 4

Is a beta lactam antibiotic
Beta lactam ring mimics D-Ala-D-Ala
Binds to PBP transpeptidase enzyme, inhibits this.
Prevents crosslinking of proteoglycan in bacterial cell walls
Leads to death by osmotic burst as cell wall integrity reduced

Question 5

Anthracycline

Answer 5

End in rubicin
Used in chemotherapy - is a cytotoxic non-specific antibiotic
Intercalated into DNA to destabilise DNA structures, causing DNA breakages, this alters the transcriptomes of the cell and can activate apoptosis if damage accumulates
inhibit topoisomerases 2 enzymes, leading to supercoiling and DNA tangles - unable to be transcribed leading to apoptosis.
Also metabolised into free oxygen radicals leading to DNA damage

Question 6

Asparaginase

Answer 6

Is an induction chemotherapy drug
Acts in the ECF, hydrolyses asparagine to aspartic acid and ammonia.
Tumour cells are dependent of asparagine from the interstitial space, have no intracellular asparagine synthase.
When low supply of essential asparagine as no more in interstisial space, unable to produce protein leading to cell death
Self cells are not affected as contain in intracellular asparinge synthase so are able to produce their own asparagine
Asparagine is a non essential amino acid.
However some rapidly dividing cells such as rbcs can show lower levels of dependence on asparagine in the ECF

Question 7

Aspirin

Answer 7

Is an NSAID
Inhibits COx-1 and Cox-2, prevents conversion of arachidonic acid into prostanoids
Is slightly selective for COX-1, this reduces the amount of thromboxane, this inhibts platelett aggregation
Also reduces prostaglandinds, which can help resolve pain,fever and inflammation, particularly by cox-2 inhibition reducing PE2 and PI2
Used as preventitive medication after a TIA

Question 8

Atorvastatin

Answer 8

Is an antielempic
Acts on herpatocytes
inhibits HMG-CoA reductase enzyme, this reduces the production of myalonic acid a precursor for LDL
This prevents hepatocytes from synthesising cholesterol
Also increases the number of LDL receptors on hepatocytes so takes in more LDL.
This reduces the amount of LDL ‘bad cholesterol’ in systemic circulation.
This imporves cardiovascular health, reduces risk of a heart attack or stroke

Question 9

Azithromycin

Answer 9

Is a macrolide
Is an antibiotic
Inhibits the 23sRNA of the 50s subunit on a bacterial ribosome.
Inhibits translocation of aminoacyl tRNA
This prevents protein elongation, Inhibits translocation leading to no protein production and cell death
Given to treat Chlamydia

Question 10

Benzylpenicillin

Answer 10

Used to treat bacterial meningitis in over 16yrs
Is a beta lactam antibiotic
Beta lactam ring mimics D-Ala-D-Ala
Binds to PBP tranverse peptidase, inhibits this.
Prevents crosslinking of proteoglycan in bacterial cell walls
Leads to death by osmotic burst as cell wall intergiry reduced

Question 11

Champix

Answer 11

Medication to help stop smoking, was previously available on the NHS but has now been withdrawn.
partial agonsit of alpha-4 beta-2 nicotinic acetylcholine receptors - has lesser effects than nicotine whilst preventing nicotine from binding
Helps ease withdrawal symptoms whilst reducing cravings

Question 12

Chondroitin

Answer 12

Used in osteoarthiritis
Is a component of cartilage ECM
Thought to encourage collagen regneration
Inhibits cox-2 preventing inflammation and inhibits NO synthesis reducing cartilage damage
Is not recommended by NICE guidelines

Question 13

Citalopram

Answer 13

Is an SSRI antidepressant
Inhibits SERT
This prevents the reuptake of seratonin from the synpatic cleft into the pre-synpatic neurone
This increases the concentration fo seratonin in the synpatic cleft so more likley to bind to a seratonin receptor on the post synaptic membrane - this increases the intensity and duration of synaptic signalling
This is thought to decrease depression based on the monoamine hypothesis of depression

Question 14

Co-amoxiclav

Answer 14

Used for gram negative bacteria that produce beta lactamases
Cluvanic acid - is weaker bl than amoxacillin so is used as a suicide substrate
amoxacillin then follows the normal mechanism of action of beta lactams

Question 15

Dexamethasone

Answer 15

Is a glucorticoid
Hydrophobic so difuses straight across the cell membrane
Binds to glucorticoid receptor in the cytoplasm, receptor is dimerised to be activated
Travel to nucleus to act as a transcription factor, alters gene expression
Reduces: vascular permeability, neutrophil migration, pro-inflammatory cytokines
Increases: anti-inflammatory cytokines, apoptosis of lymphocytes

Question 16

Diclofinac

Answer 16

non-selective NSAID

Question 17

Donepezil

Answer 17

Acetylcholineesterase inhibitor
Used in alzhimers treatment

Question 18

Entonox

Answer 18

Gas and air - given for pain relief during pregnancy
High flow oxygen - encourages endorphin release
Nitrous oxides - partial agonist of opioid receptors.

Reduces mild pain, may cause hallucination and nausea

Question 19

Fluoxotine (prozac)

Answer 19

SSRI

Question 20

Glucosamine

Answer 20

Used in osteoarthiritis
Thought to encourage cartilage regneration
Is a precursor for componenet of cartilage, glucosaminoglycans in the ECM.
Reduce NFKb and INFy signalling leading to less inflammation
Is not recommended by NICE

Question 21

Hyaluronic acid injections

Answer 21

Glycosaminoglycan - component of ECM
Acts as a lubricant and shock absorber reducing the burden and friction on cartilage to prevent damage.
Antioxidative, anti-inflammatory and analgesic effects.
Reduce pain and inflammation when injected into the synovium.
Can be bound to be aggrecan, increases the water content and viscotity of the synovial fluid.
Used to decrease pain and increase mobility in OA

Question 22

Ibuporfen

Answer 22

non-selective NSAID

Question 23

Infliximab

Answer 23

Monoclonal antibody
TNFalpha inhibitor, prevents interaction with p55 and p57 receptors

Question 24

Iron supplement

Answer 24

Taken orally absorbed into blood stream,
Aids Hb metabolism in the bone marrow
Reduce aneamia

Question 25

Lansoprazole

Answer 25

PPI Oral pro-drug: able to pass through membranes as uncharged Attracted to acidic area around parietal cells as basic Sulfoxide to sulfenic acid, is now charged so not able to pass through the membrane, leads to an accumulation/high conc of drug trapped in the canaliculi of the parietal cell. Disulfide bond with cystene amino acid in proton pump - this is a covalent change so irreversible Conformational change inhibits the proton pump Reduces H+ conc in stomach Used to prevent acid reflux.

Question 26

Bupivacaine (epidural)

Answer 26

Nerve block from T10 to L1 space No sensation below level of block Used in pregnancy - only administered by an anesthesiologist Blocks voltage gated sodium ion channels. Side effects: prolonged labour

Question 27

Mercaptopurine

Answer 27

Is a maintenance chemotherapy drug. Pro-drug Converted to TIMP inhibits processes involving IMP this inhibits purine synthesis Converted to TGTP - inserted into RNA to prevent elongation Converted to TdGTP - inserted into DNA to prevent semi-conservative replication This inhibits the S stage of interphase, preferntially affects rapidly dividng cells.

Question 28

Metformin

Answer 28

Is an anti-hyperglycemic Enters hepatocytes by OTC-1 channel Inhibits mitochondrial complex 1 - reduces ATP production AMP?ADP: ATP ratio increases Activates AMPKA This inhibits fructose-1,6-biphosphate enzyme. This inhibits gluconeogenesis and promotes glycolysis. Also inhibits acetyl-CoA carboxylase inhibitng fat synthesis Also increases cell sensitivity to insulin Decreases glucose absorption in enteroendocytes in the SI This leads to decreased blood glucose - reduces risk to bv in type 2 diabetics

Question 29

Methotrexate

Answer 29

Is an anti-folate (anti-metabolite) used as an induction chemotherapy drug Inhibitis Dihydrofolate reductase, this prevents the conversion of dihydrofolate into terthydrofolate This inhibits thymine synthesis, inhibits DNA and protein production. Also inhibits AICART (purine synthesis), increased levels of AICAR have anti-inflammatory effects Results in cell death Preferentially targets rapidly dividing cells

Question 30

Metronidazole

Answer 30

Antimicrobial for anaerobic bacteria and parasites - typically used against a C.Diff infection The nitro group is reduced the ferrodoxin or falvodoxin enzyme only found in target organism This creates free nitrile radicals that are able to bind to and oxide DNA This damages DNA, prevents DNA replication and has cidal acitivity

Question 31

Naproxen

Answer 31

NSAID

Question 32

Omeprazole

Answer 32

PPI

Question 33

Oseltamivir

Answer 33

Inhibits neuraminidase catalysed cleavage Prevents influenza viruses from leaving the infected host cell

Question 34

Oxytocin

Answer 34

Used to induce labour or prevent pph and the mothering hormone Negative feedback to reduce levels of progesterone Binds to receptors to trigger/strengthen uterine muscle contractions, by increasing intracellular calcium in uterine myofibrils. Increased by positive feedback until parturition finshed Is also produced naturally by the body, concerns that may cause too fast labour

Question 35

Paracetamol

Answer 35

NSAID Acts centrally not peripherally Thought to inhibit cox-3 preventing conversion of arachadonic acid into prostanoids. INhibits Cox1 and cox2 to increase the pain threshold Leads to reduced fever and pain. Exact mechanism is unknown

Question 36

Pethidine

Answer 36

Intramuscular Opiod used to relieve pain during labour Binds to receptor on presynaptic neurone - inhibitor GPCR prevents calcium ion influx Binds to receptor on postsytnaptic neurone - activatory GPCR leads to increase K+ efflux Results in hyperpolarisation of membrane Reduces the probability of an action potential being triggered, closes the pain gate

Question 37

Picolax

Answer 37

Laxative - used to clear the bowel before colonectomy. Contains sodium picosulfate and magneisum citrate which are converted into active forms by sulfatases in the gut Increases water secretion and inhibits electrolye and water absorption Increases peristalsis of the colon - faster expulsion of more watery stools.

Question 38

PrEP

Answer 38

Used to prevent HIV infection Typically contains tenofovir - inhibits reverse transcriptase Emtricitabine - reverse trasncriptase Creates a protective barrier around lymphocytes to stop from being invaded by HIV particles and prevents HIV from replicating Must be taken daily and before HIV infection occurs Is a preventative medication

Question 39

Propranolol

Answer 39

Is a beta blocker Antagonist of beta adrenergic receptors B1 - inhibiting decrease heart rate B2 - inhibiting causes vasodilation B2 in lungs, inhibitng can cause bronchspasm, therefore not given to asthmatics of COPD patients as unable to dilate Is a structural analogue of adrenaline Inhibits adenylate cyclase - reducing intracellular calcium so reduces muscle contractility.

Question 40

Thrombolysis

Answer 40

Medication to beak down blood clots Alteplase - is a human made form of a plasminogen activator. Binds to fibrin and plasminogen, converts plasminogen to plasmin (fibrin is a catalyst) Plasmin degrades the fibrin matrix of thrombus promoting dissolving of the clot.

Question 41

Vincristine

Answer 41

Is an induction chemotherapy treatment Binds to beta tubulin, prevents dimerizing with alpha tubulin. Unable to form the polymer component of microtubules Spindle apparatus does not form Mitosis inhibited at metaphase Leads to cell death Preferentially affects rapidly dividing cells.

Question 42

Zyban

Answer 42

Norepinehprine and dopmaine reuptake inhibitor (major depressive disorder and to aid smoking cesssation) Inhibits NET and DAT Interferes with dopamine reuptake in the reward pathway - reduce addiction Acts as a low dose nicotine substitute Antagonism of nicotinic acetycholinergic receptors

Question 43

Nitrominidazole

Answer 43

Nitroimidazole antimicrobials nitro group is converted to active compound by enzymes only found in the target organism (ferrodoxin or falvodoxin) Nitrile free radicals damage DNA - impedes DNA replication and activates apoptosis pathway Anaerobic bacteria and parasites

Question 44

Rosehip extract

Answer 44

Contains polyphenols - increase endorphin production and act as an anti-toxin Vitamin c - anti-toxin Inhibits NF B signalling and decreases levels of CRP leading to reduced inflammation.

Question 45

Curcumin

Answer 45

Inhibits cox-2, Inhibits NF-B signalling reduces inflammatory mediators

Question 46

What are the three branches of prostanoid production?

Answer 46

Prostacyclin PGI2 : involved in vasodilation and decreases platelet aggregation Thromboxane: causes platelet activation and vasoconstriction - can lead to a thrombus formation Prostaglandins E2 and I2: Can lead to pain, inflammation and gastric protection.