50 Drugs 3rd Year Flashcards

1
Q

Aspirin (Aceytlsalycilic acid)

A

Irreversible inactivation of COX enzyme.
This reduces thromboxane (platelet aggregation) and prostaglandin (noiciception and inflammation) production.

Secondary prevention of thrombotic events.
Pain relief.

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2
Q

Clopidogrel

A

Irreversibly blocks the ADP-receptor on platelet membranes so inhibits formation of the GPIIb/IIIa complex needed for platelet aggregation, so stops thrombus formation.

Used for secondary prevention of thrombotic events.

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3
Q

Tenecteplase/Alteplase

A

Recombinant form of tissue plasminogen activator. Catalyses conversion of plasminogen to plasmin, to promote fibrin clot lysis.

Used acutely for stroke, MI and PE.

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4
Q

Unfractionated Heparin

A

Enhances activity of antithrombin III which inhibits thrombin. Also inhibits multiple other factors of clotting cascade.

Prophylaxis and treatment of thromboembolic disease, and in acute coronary syndromes.

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5
Q

Low Molecular Weight Heparin

A

Enhances activity of antithrombin III which inhibits thrombin. Also inhibits other factors in the coagulation cascade.

Prophylaxis and treatment of thromboembolic disease, and in acute coronary syndromes.

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6
Q

Warfarin

A

Inhibits Vitamin K Epoxide Reductase preventing recycling of vitamin K (after carboxylation of factors 2, 7, 9 and 10).

Treatment of venous thromboembolism, and thromboprophylaxis in AF/metal heart valves/cardiomyopathy.

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7
Q

Dabigatran

A

Direct Thrombin Inhibitor, preventing conversion of fibrinogen to fibrin.

Used for prophylaxis of venous thromboembolism (especially post-op) and thromboprophylaxis in AF.

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8
Q

Rivaroxiban/Apixaban (Factor Xa Antagonist)

A

Inhibits conversion of prothrombin to thrombin, inhibiting fibrin clot formation.

Prophylaxis and treatment of venous thromboembolism (especially post-op), prophylaxis of thromboembolism in AF.

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9
Q

Bisoprolol/Atenolol (B-blocker)

A

Cardioselective Beta-1-adrenoceptor antagonist (blocks beta-1-receptors in cardiac and renal tissue) inhibiting SNS stimulation of heart and renal tissue (including inhibiting renin release).
Blockade of SA node to reduce heart rate and blockade of myocardial receptor to decrease contractility.

Used in hypertension, angina, rate control in AF.

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10
Q

Propanolol/Carvedilol (B-blocker)

A

Propanolol: non-cardioselective beta-1 adrenoceptor antagonist.
Carvedilol: non-selective beta-1, beta-2 and alpha-1 adrenoceptor antagonist.
Inhibits SNS stimulation of the heart and vascular SM.

Used in hypertension, angina, anxiety, post-MI prophylaxis, migraine prophylaxis, heart failure.

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11
Q

Ramipril (ACE Inhibitor)

A

Inhibits conversion of angiotensin I to angiotensin II (a systemic vasoconstrictor), causing inhibition of aldosterone release from the adrenal cortex, reducing sodium and water retention.

Hypertension, heart failure, nephropathy, prevention of cardiovascular events in high risk patients.

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12
Q

GTN - Glyceryl Trinitrate (Nitrates)

A

Converted to nitric oxide and acts as a potent vasodilator. Cardioselective (especially coronary arteries). Reduces cardiac preload and afterload.

Used in angina and severe hypertension.

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13
Q

Verapamil

A

(Rate limiting Ca channel blockers)

Blocks L-type calcium channels reducing calcium entry to cells and reducing myocardial and smooth muscle contractility.
Dilates coronary vessels to reduce afterload.
Anti-dysrythmic drug due to prolonged AV node conduction.

Used in supra-ventricular arrythmias, treatment of angina and hypertension.

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14
Q

Amilodipine/Nefidipine

A

(Non-rate limiting Ca Channel blockers)

L-type calcium channels stopping cellular calcium entry. This decreasing cardiac and vascular SM contractility. Dilate coronary blood vessels and reduce afterload. THIS DOES NOT LOWER HEART RATE.

Used for hypertension and angina.

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15
Q

Simvistatin

A

Competitively inhibits HMG-CoA reductase this increases expression of LDL-receptors on hepatocytes, increasing hepatic uptake of cholesterol. This reduces development of atherosclerotic plaques.

Used in hypercholesterolaemia and prevents cardiovascular events in high risk patients.

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16
Q

Digoxin

A

(Cardiac Glycosides)

Increases vagal parasympathetic activity and inhibits the Na/K pump causing intracellular sodium retention. More calcium moves into the cell via Na/Ca exchangers. More calcium causing increased heart contractility, and reduced conduction rate through the AV node.

Used in heart failure and for rate control in AF.

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17
Q

Amiodarone

A

(Anti-arrhythmic)
Blocks cardiac K+ channels, prolonging repolarisation of the cardiac action potential.
Restore sinus rhythm.
Slows AV conduction.

Used in supraventricular and ventricular arrhythmias.

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18
Q

Flucloxacillin/Amoxicillin/Benzyl Penicillin/Penicillin V

A

(B-lactams - penicillins)

Attaches to penicillin-binding-protein forming on a bacterial cell wall. This inhibits the transpeptidase enzyme which cross-links bacterial cell walls. Failure to cross-link induces cell auto-lysis.

Flucloxacillin: Soft tissue infection, staphylococcal endocarditis, otitis externa.
Amoxicillin: Community acquired pneumonia.

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19
Q

Ceftriaxone

A

(B-lactams - Cephelosporums)

Attaches to penicillin-binding-protein forming on a bacterial cell wall. This inhibits the transpeptidase enzyme which cross-links bacterial cell walls. Failure to cross-link induces cell auto-lysis. Less susceptible to beta-lactamases than penicillins.

Serious infection: Pneumonia, meningitis, septicaemia.

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20
Q

Vancomycin

A

(Glycopeptides)

Bactericidal - inhibits cell wall synthesis in gram-positive bacteria.

Used in infections with suspected MRSA, severe C. diff infection.

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21
Q

Gentamicin

A

(Aminoglycosides)

Binds to 30s ribosomal subunit inhibiting protein synthesis - Bacteriostatic effect.
Bacterocidal effect - on bacterial cell walls resulting in rapid killing.

Used in severe gram negative infections: biliary tract infection, pyelonephritis, hospital acquired pneumonia.
Some severe gram positive infections: endocarditis and soft tissue infections.

22
Q

Ciprofloxacin

A

(Quinlones)

Interferes with bacterial DNA replication and repair.

Broad spectrum, has both gram positive and negative cover.
Respiratory tract infection, upper urinary tract infection, gonorrhoea.

23
Q

Clarithromycin/erythromycin

A

(Macrolides)

Binds to 50s ribosomal subunit and inhibits protein synthesis.

Used in severe CAP, campylobacter, moderate soft tissue infection, otitis media, Lyme disease, to eradicate H. pylori infection.

24
Q

Trimethoprim

A

(Inhibits folate synthesis)

Inhibits folate metabolism pathway causing impaired nucleoside synthesis, so interferes with bacterial DNA replication.

Used in uncomplicated UTI, bronchitis, PCP infection.

25
Q

Aciclovir

A

(Anti-viral)

It is a guanosine derivative converted to triphosphate by infected host cells. Aciclovir triphosphate then inhibits DNA polymerase, inhibiting viral DNA replication.

Used in HSV and VZV.

26
Q

Salbutamol

A

Short acting Beta-2 adrenoceptor agonists (SABA), relaxes bronchial SM. Inhibits pro-inflammatory cytokine release from mast cells and TNF-alpha release from monocytes reducing inflammation. Stimulates cilia action to increase mucus clearance.

Used in asthma and COPD.

27
Q

Salmetrerol

A

Long acting Beta-2 andrenoceptor agonist (LABA)
Relaxes bronchial SM, inhibits inflammatory cytokine release from mast cells, and TNF-alpha from monocytes. Stimulates cilia action to increase mucus clearance.

Used in asthma and COPD.

28
Q

Triotropium/Ipratropium Bromide

A

(Anti-muscarinic bronchodilators)

Muscarinic receptor (M3) antagoist causing bronchodilation and reduced mucus secretion.

Used in Asthma and COPD.

29
Q

Beclamethasone

A

(Inhaled corticosteroid)

Decreases pro-inflammatory cytokine production and up-regulates beta-2 adrenoceptors in airways.

Used in asthma, COPD, oral thrush.

30
Q

Chlopheniramine

A

(anti-histamine)

H1 receptor antagonist, reduces histamine mediated contraction of bronchial SM.

Used in anaphylaxis, hayfever, Urticaria.

31
Q

Levodopa

A

(Dopamine precursor)

Prodrug, that crosses the BBB and is converted to dopamine. Striatal dopaminergic neurotransmission is increased.

Used in Parkinsons disease. Give with dopamine decarboxylase inhibitor/COMT inhibitor to stop peripheral conversion.

32
Q

Apomorphine

A

(Dopamine Agonist)

Stimulates post synaptic dopamine receptors (D1/D2 family)

Used in Parkinsons disease.

33
Q

Entacapone

A

(Catechol-O-Methytransferase inhibitor)

Prevents peripheral break down of levodopa by inhibiting COMT so more dopamine reaches the brain.

Used in Parkinsons Disease.

34
Q

Carbamazipine

A

(Anti-epileptic drug)

Acts on voltage gated Na channels on the pre-synaptic membrane to stop sodium influx to neurons, decreasing their excitability.

Used in epilepsy.

35
Q

Sodium Valporate

A

(Anti-epileptic)

Weak sodium ion channel blocker.
Inhibits GABA degrading enzymes - increased GABA stops action potentials.

Used in epilepsy, bipolar, depression.

36
Q

Phenytoin

A

(Anti-epileptic)

Acts as voltage gated Na+ channel blocker on the presynaptic membrane. This limited action potential transmission, limiting spread of seizure activity.

Used in epilepsy (including status epilepticus).

37
Q

Lamotrigrine

A

(Anti-epileptic)

Acts on pre-synaptic membrane to block Na+ and/or Ca channels to reduce action potentials and excitatory signals.

Used in epilepsy.

38
Q

Levetiracetam

A

(anti-epileptic)

SV2A is a synaptic vesicle protein needed for neurotransmitter release. Levetiracetam blocks this.

Used in epilepsy.

39
Q

Citalopram/Sertraline/Fluoxetine

A

(SSRI)

Inhibits reuptake of serotonin at the serotonin reuptake pump of the synaptic cleft in the CNS.

Used in depression, bullemia, OCD.

40
Q

Amitriptyline

A

(Tricyclic Antidepressants)

Stops reuptake of monoamines by binding to monoamine pump at the presynaptic cleft. Reduces reuptake of noradrenaline/serotonin.

Used in depression and neuropathic pain.

41
Q

Diazepam/Lorazepam

A

(Benzodiazapines)

Increases GABA affinity for GABA receptor. Gaba binding to receptor increases chloride flow through chloride channels, causing hyperpolarisation. This reduces activity of the limbic system, thalamus and hypothalamus.

Used in epilepsy, anxiety, muscle spasm, alcohol withdrawal.

42
Q

Prednisalone/hydrocortisone/dexamethasone

A

(Corticosteroids - Glucocorticoids)

Bind to glucocorticoid receptors and up-regulate anti-inflammatory mediators, and down-regulate pro-inflammatory mediators. This provides immunosuppression.
Can also increase gluconeogenesis.

Used in adrenal insufficiency, post-transplant immunosuppression, eczema, IBD, RA, MS, acute asthma.

43
Q

Etanercept/Infilximab/Adalimumab

A

(Anti-TNF)

Blocks action of TNF and its receptor, reducing inflammation. TNF alpha and beta are produced by macrophages and T cells, which stimulates IL-1, IL-6 and IL-8.

RA, psoriatic arthritis, ankylosing spondylitis.

44
Q

Methotrexate

A

(immunosuppressant)

Disrupts DNA synthesis by stoping the action of the enzyme dihydrofolate.

Used for post-transplant immunosuppression, IBD, vasculitis, paediatric leukaemia.

45
Q

Azathioprine

A

(immunosuppressant)

Stops DNA synthesis by blocking purine synthesis in lymphocytes.

Post-transplant immunosuppression, IBD, vasculitis.

46
Q

Omeprazole

A

(PPI)

Bind to H+/K+ pump on gastric parietal cells to reduce gastric HCl production.

Peptic ulcers, GORD, H. pylori infection, prophylaxis in long term NSAIDS.

47
Q

Cimetidine/Ranitidine

A

(H2 receptor antagonists)

Blocks histamine binding to H2 receptors on gastric parietal cells stimulating gastric acid secretion.

Used in peptic ulcers, GORD.

48
Q

Lactulose/Senna

A

(Laxative)

Reduces water resorption in the intestine. Pulls water into the bowel to increase distention and movement.

Used in contsitpation, used as prophylaxis for opioid analgesia.

49
Q

Cimetidine/Ranitidine

A

(H2 receptor antagonists)

Blocks histamine binding to H2 receptors on gastric parietal cells stimulating gastric acid secretion.

Used in peptic ulcers, GORD.

50
Q

Lactulose/Senna

A

(Laxative)

Reduces water resorption in the intestine. Pulls water into the bowel to increase distention and movement.

Used in constipation, used as prophylaxis for opioid analgesia.

51
Q

Cyclizine

A

(Anti-emetic)

Histamine H1 receptor antagonist which acts on the vomiting region in the medullary region. Mild anti-cholinergic and anti-muscarinic effects.

Nausea, vomiting, prophylaxis in chemotherapy and opiate analgesic use.

52
Q

Bendroflumethiazine

A

(thiazide