Drugs Flashcards

Question

RAMIPRIL: - Class: - Administration: - Mode of action: - Indications: - Side effects: - Contra-indications:

Answer 1

- Class: ACE inhibitor (others = lisinopril, enalopril) - Administration: oral tablet, oral capsule - Mode of action: inhibit ACE activity = less angiotensin II produced = less bradykinin breakdown = relaxation of arterial smooth muscle - Indications: heart failure, hypertension, MI, stroke, nephropathy - Side effects: dry cough, dizziness & fainting, fatigue - Contra-indications: Afro-Caribbean (less likely to respond), renovascular disease, hypovolaemia

Answer 2

- Class: semisynthetic antibiotic - Administration: IV infusion, oral capsule, oral suspension - Mode of action: inhibits bacterial RNA polymerase enzyme – no RNA synthesis - Indications: TB, Leprosy, Legionnaire's, H.influenza - Side effects: hepatotoxicity, fever, GI disturbance - Contra-indications: acute porphyrias, jaundice, liver failure

Answer 3

- Class: DOAC (others = apixaban) - Administration: oral tablet - Mode of action: competitive irreversible inhibition of factor Xa. Prevents thrombin formation - Indications: DVT, PE, stroke - Side effects: diarrhoea, nausea, dizziness, headache, hypotension - Contra-indications: active bleeding, malignancies, oesophageal varices

Answer 4

- Class: beta 2 agonist (LABA) - Administration: aerosol inhaler, powder inhaler - Mode of action: beta 2 stimulation causes relaxation of bronchial smooth muscle - Indications: asthma, COPD - Side effects: dizziness, sinus infections, migraines - Contra-indications: severe pre-eclampsia

Answer 5

- Class: cGMP-specific PDE5 inhibitor - Administration: oral tablet, IV injection - Mode of action: increases cGMP to cause smooth muscle relaxation - vasodilation - Indications: erectile dysfunction, pulmonary hypertension - Side effects: back pain, myalgia, dyspepsia, flushing - Contra-indications: retinal disorders, recent MI/stroke, hypotension

Answer 6

- Class: paralytic - Administration: IV injection - Mode of action: mimics ACh at NM junction, with slow hydrolysis – prolongs depolarisation = NM blockade - Indications: general anaesthesia - Side effects: flushing, hyperkalaemia, myoglobinaemia/uria - Contra-indications: Duchenne MD, FH of malignant hyperthermia, hyperkalaemia

Answer 7

- Class: alpha blocker - Administration: oral tablet - Mode of action: selective A1 antagonist - causes relaxation in smooth muscle = less resistance to urinary flow = less pain in BPH - Indications: benign prostatic hyperplasia - Side effects: allergy, hypotension, retrograde ejaculation - Contra-indications: micturition syncope, postural hypertension

Answer 8

- Class: opioid - Administration: IM injection, IV infusion, oral tablet - Mode of action: agonist of mu-opioid receptors, serotonin & norepinephrine reuptake inhibitor, enhances serotonin release - Indications: moderate to severe pain - Side effects: allergy, hypotension, retrograde ejaculation - Contra-indications: pregnancy and lactation, children/elderly, liver/renal failure, respiratory depression

Answer 9

- Class: calcium channel blocker (others = felodipine) - Mode of action: inhibit influx of calcium ions into vascular smooth muscle cells through L-type calcium channels -\> calcium can't enter muscle cells = vasodilation and decreased BP - Indications: hypertension (1st line in patients \>55 and/or Afro-Caribbean) - Side effects: abdominal pain, dizziness, fatigue, flushing, headache, nausea, oedema, palpitation, sleep disturbances - Contra-indications: caution in the elderly and those with heart failure (avoid if uncontrolled), avoid in unstable angina, severe aortic stenosis and those who have had an MI in the last month

Answer 10

- Class: NSAIDs - Mode of action: reversibly inhibits both the COX-1 and COX-2 enzymes. This results in the inhibition of prostaglandin synthesis (prostaglandins act as signaling molecules in the body, inducing inflammation) - Indications: pain and inflammation in rheumatic disease/MSK disorders, acute gout, acute migraine - Side effects: asthma, diarrhoea, dizziness - Contra-indications: those with a history of hypersensitivity to aspirin or any other NSAID

Answer 11

- Class: PPIs (others = lansoprazole) - Mode of action: irreversible inhibitor of H + K + ATPase pump at the secretory surface of gastric parietal cells. Inhibits final transport of hydrogen ions into gastric lumen; thereby inhibiting gastric acid secretion - Indications: treatment of gastric and duodenal ulcers (peptic ulcer disease), prevention and treatment of NSAID-associated ulcers, Helicobacter pylori eradicaton (in combination with two antibiotics - Triple Therapy), GORD, Zollinger-Ellison syndrome - Side effects: GI disturbance, e.g. nausea, vomiting, abdominal pain, flatulence, and headache - Contra-indications: PPIs MAY MASK SYMPTOMS OF GASTRIC CANCER - in patients presenting with ‘alarm features’ (bleeding, dysphagia, recurrent vomiting, weight loss) it is important to rule out malignancy before commencing PPI therapy. Avoid in pregnancy and breast-feeding

Answer 12

- Class: antiplatelet agents - Mode of action: irreversible inhibitor of COX enzymes. Impairs synthesis of thromboxane A2 and prostacyclin within platelets = reduced platelet aggregation - Indications: secondary prevention of cardiovascular disease following: MI/acute coronary syndrome/angina pectoris, stroke - Side effects: GI irritation, ulceration and bleeding, bronchospasm - Contra-indications: avoid in active peptic ulceration, haemophilia and other bleeding disorders and those with known hypersensitivity to aspirin or other NSAIDs

Answer 13

- Class: HMG Co-enzyme A reductase inhibitors (others = atorvastatin) - Mode of action: competitive inhibitor for HMG Co-enzyme A reductase. Inhibition of HMG Co-enzyme A reductase reduces hepatic cholesterol synthesis through the mevalonate pathway. This in turn leads to reduced LDL cholesterol, reduced triglycerides, increased HDL cholesterol - Interactions: treatment of primary hypercholesterolaemia, treatment of homozygous familial hypercholesterolaemia, prevention of cardiovascular events in patients with atherosclerotic cardiovascular disease or diabetes mellitus - Side effects: abnormal LFTs (elevated transaminases); GI disturbance, e.g. constipation, flatulence, myalgia - Contra-indications: caution in patients with risk factors for myositis/rhabdomyolysis (e.g., low body mass, hypothyroidism) and those with history of liver disease. Avoid in active liver disease and pregnancy

Answer 14

- Class: beta blockers (others: cardioselective (beta-1 only) = atenolol, non-cardioselective (beta-1 and beta-2) = carvedilol - Mode of action: competitive antagonist for beta adrenoreceptors. This inhibits binding of noradrenaline released from sympathetic adrenergic neurones. This inhibits activation of adenylyl cyclase enzymes leading to reduced cyclic AMP. This in turn leads to reduced intracellular calcium levels. Overall effect = reduce contractility (negative intropy), reduce heart rate (negative chronotropy), reduce blood pressure, reduce cardiac work - Indications: angina pectoris, myocardial infarction, heart failure, resistant hypertension - Side effects: dizziness, fatigue, cold hands, impotence, headaches - Contra-indications: avoid in asthma, heart block and hypotension

Answer 15

- Class: antiplatelet (others = clopidogrel) - Mode of action: P2Y12 receptor antagonist that prevents ADP-mediated P2Y12 dependent platelet activation and aggregation - Indications: prevention of atherothrombotic events - Side effects: diarrhoea, dizziness, GI disorders - Contra-indications: history of hypersensitivity to aspirin or any NSAID

Answer 16

- Class: nitrates - Mode of action: relaxation of vascular smooth muscle - Indications: angina - Side effects: headaches, nausea, flushing - Contra-indications: aortic stenosis, cardiac tamponade, hypovolaemia, mitral stenosis

Answer 17

- Class: SSRIs (others = citalopram, sertraline) - Mode of action: blocks the reuptake of serotonin into presynaptic serotonin neurons by blocking the reuptake transporter protein (5HT1A) located in the presynaptic terminal - Indications: depression, bulimia nervosa, OCD - Side effects: anxiety, dry mouth, diarrhoea - Contra-indications: poorly controlled epilepsy

Answer 18

- Class: antiepileptics - Mode of action: unclear, but though to: slow recovery of the voltage-gated sodium channels, open potassium channels and promote GABA release - Indications: focal and secondary generalised tonic-clonic seizures, primary generalised tonic-clonic seizures, trigeminal neuralgia, diabetic neuropathy - Side effects: dizziness, drowsiness, dry mouth - Contra-indications: AV conduction abnormalities (if not paced), history of bone marrow depression, acute porphyria and those with known hypersensitivity to tricyclic antidepressants

Answer 19

- Class: nonsteroidal aromatase inhibitors - Mode of action: letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of oestrogen biosynthesis in all tissues - Indications: first line treatment in postmenopausal women with hormone-dependent advanced breast cancer - Side effects: hot flush, nausea, vomiting - Contra-indications: premenopausal women

Answer 20

- Class: short acting beta 2 agonist (others = terbutaline) - Mode of action: activation of β2 adrenoceptors stimulates adenylate cyclase enzymes to increase production of cAMP = bronchial smooth muscle relaxation and bronchodilatation - Indications: asthma - Side effects: arrhythmias, headache, palpitations, tremor - Contra-indications: caution in diabetes mellitus, hyperthyroidism and cardiovascular disease, e.g. hypotension, arrhythmias

Answer 21

- Class: angiotensin receptor blocker (others = losartan, valsartan) - Mode of action: selective inhibition of potent vasoconstrictor peptide angiotensin II leading to vascular smooth muscle relaxation and vasodilatation = reduced blood pressure - Indications: hypertension, heart failure, post-MI, TYPE II DIABETIC NEPHROPATHY - Side effects: (first dose) hypotension, dizziness, hypotension - Contra-indications: avoid in pregnancy + breast-feeding

Answer 22

- Class: aldosterone antagonist - Mode of action: competitive antagonist, blocks adosterone-MR translocation into the nucleus reducing the production of aldosterone induced proteins. Inhibits Na+ /K+ exchange in the distal tubule and collecting ducts, promoting potassium retention and sodium and water loss - Indications: oedema in congestive heart failure – shown to improve survival, ascites, primary hyperaldosteronism, nephrotic syndrome - Side effects: GI upset, hyperkalaemia - Contra-indications: avoid in hyperkalaemia, hyponatraemia, anuria and Addison's disease

Answer 23

- Class: vitamin K antagonist - Mode of action: depletion of active clotting factors II, VII, IX and X; this produces a potent anticoagulant effect - Indications: prophylaxis of embolisation in rheumatic heart disease and atrial fibrillation, prophylaxis after insertion of prosthetic heart valve, prophylaxis and treatment of venous thrombosis and pulmonary embolism, TIA - Side effects: haemorrhage and bruising - Contra-indications: avoid in pregnancy, peptic ulcer disease, severe hypertension and those with hepatic impairment

Answer 24

- Class: histamine 2 receptor antagonist - Mode of action: prevent binding of histamine to its H2 receptor on the gastric parietal cell reducing stimulation of gastric acid secretion - Indications: GORD, peptic ulcer disease, dyspepsia - Side effects: diarrhoea, headache, dizziness - Contra-indications: avoid in pregnancy. H2 receptor antagonists MAY MASK THE SYMPTOMS OF GASTRIC CANCER - in patients presenting with ‘alarm features’ (bleeding, dysphagia, recurrent vomiting, weight loss) it is important to rule out malignancy before commencing therapy

Answer 25

- Class: corticosteroid (others = dexamethasone) - Mode of action: prednisolone and other corticosteroids mimic the action of the endogenous mediator cortisol at steroid receptors. Binding of a corticosteroid to the cytoplasmic steroid receptor exposes a DNA binding domain on the receptor. This allows the steroid-receptor complex to associate with glucocorticoid response elements present in the promoter regions of target genes - Indications: suppression of inflammatory and allergic disorders, IBD, severe asthma (step 5), immunosuppression, rheumatic disease - Side effects: moon face with plethoric cheeks, central fat distribution with striae, hypertension - Contra-indications: caution in pregnancy

Answer 26

- Class: monoclonal antibody - Mode of action: interferes with interleukin-5 receptor binding, thereby reducing the survival and activity of eosinophils - Indications: severe eosinophilic asthma - Side effects: anaphylactic reaction, myalgia - Contra-indications: hypersensitivity reactions, pre-existing helminth infection

Answer 27

- Class: tumor necrosis factor-alpha (TNF-alpha) inhibitors - Mode of action: binds to soluble and transmembrane forms of TNF-α with high affinity to disrupt the pro-inflammatory cascade signalling - Indications: Crohn's, UC, RA, ankylosing spondylitis, psoriatic arthritis - Side effects: headaches, nausea, fever - Contra-indications: moderate or severe heart failure, severe infections

Answer 28

- Class: alkylating agents - Mode of action: selectively suppress regulatory T cells (Tregs). This effect can be used to counteract immunosuppression in cancer - Indications: RA, used in combination with other agents to treat a wide range of malignancies - Side effects: anaemia, sperm abnormalities, thrombocytopenia - Contra-indications: avoid in acute porphyrias

Answer 29

- Class: aminosalicylates (others = mesalazine) - Mode of action: precise mechanism of action is unknown. Thought to inhibit mucosal production of arachidonic acid metabolites such as prostaglandins - Indications: Crohn's disease, UC, RA - Side effects: GI upset (diarrhoea, nausea, vomiting, abdominal pain) - Contra-indications: caution in those with G6PD deficiency

Answer 30

- Class: osmotic laxative - Mode of action: it causes water to be retained in the bowel instead of being absorbed into the body. This increases the water content and volume of the stools in the bowel, making them softer and easier to pass, as well as improving gut motility - Indications: chronic constipation - Side effects: flatulence, GI discomfort, nausea, vomiting - Contra-indications: intestinal obstruction, intestinal perforation, toxic megacolon

Answer 31

- Class: antimuscarinic drug - Mode of action: exerts a spasmolytic action on the smooth muscle of the gastrointestinal, biliary and genito-urinary tracts - Indications: symptomatic relief of gastro-intestinal or genito-urinary disorders characterised by smooth muscle spasm, IBS - Side effects: constipation, dizziness, drowsiness - Contra-indications: GI obstruction, severe UC, toxic megacolon

Answer 32

- Class: beta-lactam antibiotic - Mode of action: inhibit cross-linking of NAMA/NAG peptide chains in the peptidoglycan bacterial cell wall = weakening of bacterial cell wall leading to lysis (bacteriocidal) - Indications: broad spectrum - respiratory infections, UTIs, otitis media - Side effects: crystalluria, hypersensitivity vasculitis, dizziness - Contra-indications: hypersensitivity (important in all penicillins!)

Answer 33

- Class: leukotriene receptor antagonists - Mode of action: block the action of cysteinyl leukotrienes (pro-inflammatory eicosanoids released from mast cells and eosinophils) in airway smooth muscle = reduce the airway inflammation seen in asthma and rhinitis - Indications: management of persistent poorly controlled asthma (step 4 in the BTS guidelines), symptomatic relief of seasonal allergic rhinitis in asthma patients - Side effects: abdominal pain, headache, hyperkinesia (in young children); thirst - Contra-indications: caution in the elderly and those with renal impairment, avoid in hepatic impairment

Answer 34

- Class: antithyroid drugs - Mode of action: precise mechanism of action unclear, it is thought to inhibit the iodination of tyrosyl residues in thyroglobulin, which inhibits coupling of iodotyrosine molecules. This reduces output of thyroid hormones T3 and T4 from the thyroid gland, leading to a gradual reduction in hyperthryoid signs and symptoms - Indications: hyperthyroidism - either alone as part of a block regimen to restore euthyroid status or in combination with levothyroxine as the block component of a ‘block and replace’ regimen - Side effects: GI disturbance, arthritis, fever, rash, pruritus, jaundice - Contra-indications: caution in hepatic impairment (avoid if severe) and during pregnancy, avoid in patients with severe blood disorders, discontinue if patient develops clinical or laboratory evidence of neutropenia

Answer 35

- Class: local anaesthetics - Mode of action: blockade of voltage-gated sodium channels (VGSCs) leading to a reversible block of action potential propagation - Indications: anaesthesia, CPR (if amiodarone is not available) - Side effects: temperature sensation altered, tinnitus, vomiting - Contra-indications: - IV use: all grades of atrioventricular block,severe myocardial depression, sino-atrial disorders - With topical use: application to the middle ear (can cause ototoxicity); should not be applied to damaged skin

Answer 36

- Class: antiepileptics - Mode of action: inhibit inactivation of inhibitory neurotransmitter GABA and block its reuptake into neurones = increased GABA levels within the brain = interruption of seizure activity - Indications: epilepsy (but give LAMOTRIGINE in females of childbearing potential for all except myoclonic (levetiracetam) and absence (ethosuximide)) - Side effects: anaemia, confusion, headache - Contra-indications: avoid in active liver disease, hepatic impairment, pregnancy and in patients with family history of severe hepatic dysfunction

Answer 37

- Class: (drugs used in gout) - Mode of action: binds to tubulin. Inhibits polymerisation of neutrophil microtubules by preventing addition of dimers, leading to impaired cell motility and decreases phagocytosis = dampens inflammatory response - Indications: acute gout - Side effects: GI disturbances: nausea, vomiting, abdominal pain, DIARRHOEA - Contra-indications: caution in the elderly, hepatic impairment, renal impairment (avoid if severe) and those with GI or cardiac disease, avoid in pregnancy

Answer 38

- Class: thyroid hormones - Mode of action: agonist of thyroid nuclear receptor. Stimulates nuclear transcription of target genes, increasing mRNA and protein synthesis - restores euthyroid state through synthetic replacement of deficient endogenous thyroid hormone - Indications: hypothyroidism, 'replace' component of block and replace regimen for hyperthyroidism, diffuse non-toxic goitre, Hashimoto’s thyroiditis, thyroid carcinoma - Side effects: usually at excessive dosage, mimic symptoms and signs of hyperthyroidism, e.g. diarrhoea, tachycardia, sweating, restlessness etc. - Contra-indications: avoid in patients with thyrotoxicosis, caution in diabetes insipidus and mellitus + those with cardiovacular disease

Drugs Flashcards

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