Pharmocology Flashcards by Beth Norman

Proton Pump Inhibitors:

What do the names of the drugs end in?
What is a prodrug?
What is their protective coating made from?
What cells are they taken up by?
What do they form in the blood?
Why do they last a few days?

Name: ‘zole’
Prodrug: Enters inactive 
Protective coating: H2CO3- to alter pH
Uptake: Parietal cells
Form: Suldenamides in the blood
Long lasting: Irreversibly bind

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Histamine (H2) Antagonists:

What is the normal action of Histamine?
What do H2 antagonists do?
What do the names of the drugs end in?

Action: Binds to H2 receptor –> G protein –> adenylate cyclase –> cAMP –> Protein kinase A –> protein phosphorylation and activation –> increases acid
Antagonists block this
Name: ‘tidine’

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NSAIDS’s:

What is the normal action of the COX1 enzyme?
What is the normal action of the COX2 enzyme?
What do NSAID’s do?

COX1: Prostaglandin increase mucus and decrease acid in the stomach
COX 2: Cause inflammation due to illness
Drugs: Stop the inflammation but also decrease mucus and increase acid in the stomach

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Misoprostal:

What molecule is it a similar shape to?
What does it do in the stomach?

Similar shape to prostaglandin

Maintains mucus

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Muscarinic antagonists:

What do they treat?
What do the names of the drugs end in?
Side effects?

Treat: Motion sickness
Name: ‘cine’
Side effects: Blurred vision, relaxed gut and dry mouth

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Histamine (H1) Antagonists:

What do they treat?
What do the names of the drugs end in?
Side effects?

Treat: Motion and morning sickness
Name: ‘zine’
Side effects: Drowsiness and dry mouth

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What drug which was used for morning sickness was banned and why?

Thalidomine

Developmental problems in the limbs

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5HT3 antagonists:

How do they work?
How can you increase their effectiveness

Target 5HT stimulation

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Other drugs for sickness:

Metaclopramide: How it works and side effects.
Phenothiazides: What do the drugs end in and side effects
Doperidone: What does it act on and what can it not cross?

Metaclopramide:
Acts on the chemoreceptor trigger zone and increases digestive motility.
Side effects: movement+menstruation disorders, fatigue, increased prolactin

Phenothazides:
‘zine’ and neurological effects

Doperidone:
Acts on chemoreceptor trigger zone and the gut
Cannot cross the blood brain barrier

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2 interventions for autoimmune disease

What do these drugs do?
Rituximab
Atabercept
Ipilumumab

Cytokine therapies block the problematic antibody (e.g. anti-TNF/anti-IL1)
Steroids to stop clonal expansion by blocking receptors and signal recognition

Rituximab: Anti B cell antibodies
Atabercept: Inhibits T cell response by blocking positive signals
Ipilumumab: Stimulates antibody causing positive signal and decreased T cell activity

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Name 2 anti-platelet drugs

Aspirin and Clopidogrel

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What 2 things does Aspirin do in the vasculature?

3 uses and one problem

Inhibits COX 1 which is used to activate thromboxane A2
Inhibits COX2 in vasculature endothelial cells causing decreased inflammation
Uses: Angina, heart attacks, stroke (can also cause stroke)

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What type of drug is Clopidogrel?
What does it do?
How is it metabolised?
Side effect?

Clopidogrel:
An ADP receptor antagonis
Inhibits ADP (a platelet agonist released from dense granules)
Metabolised by P450 enzymes 
Side effects: Bleeding

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What do anti-coagulants do?
What are the 2 types?
Name 2 anti-coagulant drugs

Decrease the formation of fibrin by inhibiting the synthesis/activity of clotting factors

Direct thrombin inhibitors / direct factor 10 inhibitors

Heparin and Warfarin

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What are the two types of Heparin and how are they made?

What are the differences between them?

Unfractionated Heparin is a natural polysaccharide which can be fractionated to LMW Heparin

UFH binds to antithrombin and inactivates factor 10 and thrombin by forming a ternary complex
LMWH only inactivates factor 10 as it does not form this complex

Side effects: Immune induced thrombocytopenia, neurological injury

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What clotting factors rely on the reduced form of Vitamin K?

Use and side effects of Warfarin?

7,9,10
Use: Prevents clotting after heart attacks
Side effects: Osteoporosis, bleeding, foetal haemorrhage

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How does high levels of Aspirin increase the risk of a myocardial infarction?

COX 2 produces prostacyclin which switches platelets off and vasodilates; when this is blocked platelets are switched on and the vessels are vasoconstricted –> clots

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How does Aspirin actually work?

Stops platelets from metabolising arachidonate acid to thromboxanes
Arachidonate acid is therefore metabolised to lipoxins which solve the response

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What are ‘coxibs’

Example

COX 2 specific drugs

Celecoxib

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4 side effects when Coxibs and ibuprofen are taken together

Hyponatraemia
Heohrotoxicity
Bleeding
Hyperkalaemia

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What does ‘NO-NSAID’ stand for?

2 positive effects?

Nitric oxide-donating NSAID

Gastric protection and increased anti inflammatory effects

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4 roles of Glucocorticoids

3 example drugs

Decrease inflammation caused by cytokines
Decrease prostaglandins and leukotrines
Decrease emigration of leukocytes from vessels
Increase apoptosis of lymphocytes and eosinophils

Hydrocortisone, Prednisolone, Dexamethasone

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What are the three levels of steroid dose?

How is toxicity affected by these levels?

Topical: Low dose
Acute: Medium dose
Chronic: High dose

Higher dose = higher toxicity

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Side effects of steroids (4)

Decreased response to infection
Decrease in steroid production
Carbohydrate and protein metabolism effects
Cushing’s syndrome

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What do glucocorticoids inhibit? | Why does this lead to such a large effect?

Inhibit phospholipase A | Whole cascade is disrupted

2 examples of sedating antihistamines 2 examples of non-sedating antihistamines How are non-sedating antihistamines different?

Chlorphenamine and Promethazine Cetrizine and Fexofenadine They decrease vascular permeability

What is the mechanism of Basilximab?

Pick up cytokine in blood and prevent it from binding OR bind to the receptor and prevent the cytokine from binding Prevent proliferation by blocking JAK signalling

What is the mechanism of Cyclosporine and Tarcolimus?

Both bind to different primary molecules but then go on to block the same protein which is needed for dephosphorylation of a compound which activates IL2 transcription in the nucleus IL2 activates T cells so without dephosphorylation, T cells are not activates

What is the mechanism for Rapamycin?

Blocks the protein mTOR which activates protein synthesis, cytoskeleton activation and migration of immune cells Also blocks proliferation as mTOR also activates cyclins that help G1-->S phase in the cell cycle

What are DMARDs | 5 examples

Disease modifying anti-rheumatic drugs | Methotrexate, Gold, Sulfasalazine, Penillamide, Chloroalanine

What does the drug Carbamazepine do? | What 2 things does it treat?

Increases the inactivated state of the sodium channel and refractory period Treats nerve pain and epilepsy

What does Tetrodotoxin do? | What does it cause?

Blocks Na ion channels | Respiratory depression

What do local anaesthetics do? | Give 2 examples of esters and 3 examples of amides

Block sodium ion channels Esters: Cocaine and Procaine Amides: Lidocaine, Bupiracaine, Ropivacaine

What are the 4 classes of opioids? | e.g. of each

Natural e.g. morphine Endogenous e.g. endorphin Semi-synthetic e.g. heroin Fully synthetic e.g. pethidine

When should you not give opioids?

Alcoholism | Respiratory depression

What receptors do opioids bind to in the brain?

Mu, Delta, Kappa

Side effects of opioids?

Constipation, drowsiness, hypotension, nausea, respiratory depression and vomiting

``` What are the roles of these 7 opioids? Morphine Sulphate Diamorphine (Heroin) Codeine Fentanyl Pethidine Tramadol ```

Morphine Sulphate: Most common Diamorphine (Heroin): Increased power Codeine: Mild-moderate relief, decreases cough and causes constipation Fentanyl: Anaesthetic properties Pethidine: Moderate-severe relief, obstetric and peri-operative Tramadol: Decreases side effects by enhancing adrenergic and serotenergic pathways

What is the role of Naloxone?

An opioid receptor antagonist to reverse the effects of an opioid overdose

What drug is used to treat motor neurone disease? | What does it do?

Riluzole | Blocks glutamatergic neurotransmission to slow the progression of the disease

What is L-DOPA? | 3 side effects?

Precursor of dopamine | Drug resistance, psychosis and involuntary movements

Side effect of a dopamine agonist?

Sleepiness

What is the treatment for Alzheimer's - why? | 3 examples of drugs

AChE inhibitors as there are decreased neurones in the hippocampus meaning ACh levels are reduced Donepezil, Neostigmine, Physostigmine

What drugs do GABA receptors have binding sites for?

Benzodiazapines, Neurosteroids, Pricrotoxin, Barbiturates

What type of drug is Diazepam? | What does it do?

A anticolytic drug | Increases GABA inhibition--> hyperpolarisation

How does the drug Picrotoxin work?

Stops the GABA ion channel from opening causing convulsion

What does strychine poisoning cause?

Convulsion

What do SSRI's specifically inhibit? | What receptors do they inhibit and where are these receptors found?

SERT receptors | 5-HT1A receptors in brain regions that control mood, cognition and theory

4 examples of SSRI's

Escitalopram Fluoxetine Busprione Citalopram

What neurotransmitters do MAO inhibitors affect?

Prevent serotonin and noradrenaline breakdown

How do tricyclics work?

Block the uptake of serotonin and noradrenaline

What drugs are used to treat chronic pain?

NSAID's Paracetamol Opioids Tricyclic Antidepressants

``` What class of drugs are benzodiazepines? What do they treat? ```

GABA-A agonists | Anxiety

4 examples of Benzodiazepines

Diazepam, Temazepam, Colanezpam, Lorzepam

8 side effects of Benzodiazepines

Addiction, amnesia, confusion, decreased coordination, drowsiness, sedation, muscle relaxation, withdrawal symptoms

How do beta blockers help with anxiety?

Decrease the physical symptoms

How do antipsychotic drugs work? | What symptoms do they treat?

Block D2 receptors in the MESOLIMBIC pathway | + symptoms

3 examples of antipsychotic drugs | Which are 1st and 2nd generation

1st generation: Haloperidol | 2nd generation: Olanzapine and Risperidone

Antipsychotic side effects on: | H1, Muscarinic, Alpha 1 adreno and 5HT2C receptors

H1: Sedation Muscarinic: Dry mouth, blurred vision, decreased bowel and urine movements Alpha 1 adreno: Postural hypotension 5HT2C: Increased appetite

3 general side effects of antipschotic drugs

Cardiovascular and diabetes risk, cholesterol increase

How do tricyclic antidepressants work? | 3 things they treat

Block noradrenaline and serotonin reuptake transporters | Treat depression, pain and anxiety

2 examples of tricyclic antideressants

Aminotryptiline and Lofepramin

Side effects of SSRI's

Nausea, suicide idealaition, sexual dyfunction and withdrawal

Which is the safest anti-depressent to overdose on?

SSRI's

2 examples of MAO

Phenzine and Moclopemide

Which antidepressant does not work on neurotransmitters?

Iprinidole

What do beta blockers stop?

Tachycardia

What is a side effect of a beta blocker?

Sweating

What do botox and nerve gases block? | Where?

Both block cholinesterases | Botox in muscles and nerve gases in ganglia

Give two examples of antidotes for sarin

Atropine and Pyridostigmine

Give 4 examples of anaesthetics

Curare, Atacurium, Paniculonin and Miracurium

What 2 things do nicotinic anaesthetics cause? | Give an example

Tonic paralysis and respiratory depression | Suxamethonium

Is suxamethonium a long or short acting drug?

Short acting

What is another name for hyosine

Scopolamine

Give three examples of muscarinic antagonists

Tropicamide, Hyoscine and Atropine

What type of drug is atropine? | What does it do?

A nicotinic and muscarinic antagonist Nicotinic: Relaxes and dilates eye muscles Muscarinic: Affects secretion, increases brachycardia, increases gut motility and decreases motion sickness

What drug has similar effects as Atropine when it works as a muscarinic antagonist

Hyoscine

Give an example of a muscarinc agonist | What does it do?

Pilocarpine | Iris constriction

What two drugs stimulate the adrenergic neurone?

Caffeine and cocaine

What class of drugs is Isoprenaline and Salbutamol?

Alpha antagonist and beta agonist

Which is the more long term drug: Isoprenaline or Salbutamol?

Isoprenaline: ST as metabolised by CATACOLINOTRANSFERASE Salbutamol: LT as inhibits this enzyme

What do Isoprenaline and Salbutamol affect in the blood?

Blood pressure and peripheral resistance

Give two examples of alpha antagonists

Phenoxybenzamine and Prazonin

Give 2 examples of beta antagonists | Which one only works on beta 1?

Propanalol and Atenolol | Atenolol = beta 1 only

Give 2 examples of beta 1 agonists

Dopamine and Dobutamine

Give 3 examples of beta 2 agonists

Salbutamol, Terbutline and Salmeterol

What does phenoxybenxamine work on?

Adrenal gland tumours that release noradrenaline and adrenaline

What are the two classes of antipsychotic medications? | Which has more side effects?

1st and 2nd generation | 1st generation has more side effects

What class of drugs are antipsychotics?

D2 antagonists

What neurotransmitters does Clozapine also affect aside from dopamine?

Noradrenaline and histamin

Is Olanzapine sedative or not sedative?

Very sedative

side effects of antipsychotics

20 year decrease in life expectancy, Breast enlargement, Cardiac issues, Diabetes, Q-T interval increases, Menstrual cycle changes, Milk leakage, Sedation, Sexual Dysfunction, Tachycardia, Weight increase

One way that antipsychotics cause weight increase aside from by a natural increase in appetite

They increase histamine levels

3 examples of immunosupressants which target transplantation

Cyclosporin, Tarcolimus, Sirolimus

1 example of cytostatics for autoimmune disease

Cyclophosphamide

1 example of cytotoxic (chemotherapy) agents for cancer | Explain how it works

Fluorouracil Similar shape to T and U which leads to blocking Inhibits enzymes causing apoptosis

What drug is used to reduce cough?

AF-219

What is the mechanism of action for the antibiotic Tetracycine?

Blocks tRNA entry to ribosomes

What is the mechanism of action for the antibiotic Chlorampenicol?

Blocks new amino acids from entering the polypeptide chain

What do aminoglycoside antibiotics target?

Ribosomes

What do vaccinations target?

Capsules of bacteria

What does penicillin target?

It disrupts the synthesis of the gram negative cell wall

What do beta-lactam antibiotics target?

The septum formation stage of bacterial replication

Give an example of a beta 1 selective beta blocker

Atenolol

Give 2 examples of non-dihydropyranca channel antagonists

Verapamil | Diltiazem

Explain the mechanism of digoxin

Inhibits the Na/K ATPase so the Na/Ca exchanger is used instead Increased Ca leads to increased cardiac contractility causing a steady beat

How do beta blockers affect the RAAS system?

They decrease renin levels

How do alpha blockers work? | Give a side effect

They cause vasodilation which decreases blood pressure | Postural hypotension

What is the suffix of a calcium antagonist | 2 things it does

'-ipine' | Inhibits muscle and vasodilation

What is the suffix of an ACE inhibitor?

'-pril'

What is the suffix of an AT receptor blocker?

'-sartan'

What drug is used to block Aldosterone?

Spironolacetone