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20 Cards in this Set
- Front
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Amlodipin, Nifidipine
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CCB Non-Rate Limiting. Targets L-type calcium channels, favouringdepolarised closed Ca2+ channels most commonly found in vascularmuscle cells. They act as an antagonist and inhibit the influx of calcium ionsinto vascular smooth muscle cells.The decreasedintracellular Ca2+ causes decreased arterial smooth musclecontractility, leading to vasodilatation and decreased blood pressure.
Uses: Hypertension (2nd line, 1st in over 55's and black AC), angina Side effects: Tachycardia, flushing, peripheral oedema, heart failure |
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Atenolol, Bisoprolol
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Beta-adrenoreceptor blocker. Inhibits the activation of adenylyl cyclase leading to reduced levelsof cAMP. This is turn leads to a reduced intracellular calcium level whichleads to reduced: contractility of the heart (negative inotropy), heart rate(negative chronotropy), blood pressure and cardiac work.
Uses: Resistant (4th line?) hypertension, angina, stable heart failure, MI Side effects: Fatigue, bradycardia, heart block, hypotension, dizzyness |
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Budesonide, Beclometasone
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Corticosteroid. Glucocorticoid receptor agonist, inducing the synthesis oflipocortin-1 polypeptide which inhibits the production of inflammatorymediators such as prostaglandins and leukotrienes which reduces/preventsinflammation.
Uses: COPD, asthma (prophylaxis of both) Side effects: Oral candidiasis, growth retardation in children |
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Furosemide, Bumetanide, Torasemide |
Loop diuretic. Targets the Na+K+2Cl-cotransporter in the thick ascending limb of nephron andcompetitively inhibits at the chloride binding side of a membrane transportprotein. This prevents the transport of sodium from the lumen to the interstitium, increasing diuresis.
Uses: Congestive heart failure, acute hyperkalaemia, acute renal f. Side effects, Hyponatraemia, hypokalaemia, hypovolaemia, renal tox. |
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Ipratropium Bromide
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SAMA. Competitive antagonist of muscarinic M3 receptors in both bronchial smooth muscles and mucous gland cells. Competes with the ACh, prevents ACh mediated bronchoconstriction. Inhibition of the ACh receptor signal results in smooth muscle relaxation and bronchodilatation as well as reduced mucous secretion.
Uses: COPD, irritant induced asthma/acute bronchospasm Side Effects: Dry mouth, constipation, urinary retention |
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Lisinopril
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A competitive ACE inhibitor, preventing the conversion of angiotensin I -> angiotensin II, a vasoconstrictor. This prevents angiotensin II dep. vasoconstriction which leads to vascular smooth musclerelaxation and vasodilatation. No angiotensin II leads to a decreased aldosterone secretion from the renal cortex, decreasing Na+(natriuresis) and water retention (diuresis) leading to lowered bloodvolume. Used: Hypertension, Heart Failure, Post-MI. Side effects: Dry cough (BK), FD Hypotension, Hyperkalaemia, Renal Fail. |
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Perindopril
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A pro-drug which requiresconversion by enzymes in the liver to the active metaboliteperinodoprilat which is an inhibitorof the enzyme ACE.
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Pindolol
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An example of a partial antagonist, acting at b adrenoceptors (non-selective). Thisinhibits the activation of adenylyl cyclase leading to reduced levelsof cAMP. This is turn leads to a reduced intracellular calcium level whichleads to reduced: contractility of the heart (negative inotropy), heart rate(negative chronotropy), blood pressure and cardiac work.
Uses: Resistant (4th line?) Hypertension, Angina, Stable heart failure, MI Side effects: Fatigue, bradycardia, heart block, hypotension, dizzyness |
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Prazosin, Doxazosin, Terazosin
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A selective antagonistat a1adrenoceptors(alpha-blocker), preventsnorepinephrine from activating (via a G-protein) phospholipase C to makethe secondary messengers IP3 and DAG; as a consequence norepinephrine cannotconstrict vascular smooth muscle.
Uses: 3rd line anti-hypertensive, BPH Side Effects: Dry mouth, headache, postural hypotension |
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Diltiazem, Verapamil
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Rate limiting CCB. Targets L-type calcium channels, favouringhyperpolarised Ca2+ channels most commonly found in cardiac musclecells. Antagonist, inhibiting Ca2+ influx intocardiomyocytes through the L-type Ca2+ channels. Decreased intracellular Ca2+ has a negative inotropic effect, decreasing the cardiaccontractility, and lowering cardiac work and afterload as well asblood pressure via vasodilatation. Uses: Hypertension (1st line in Black AC, and >55's), angina, supra.V Side effects: Tachycardia, flushing, peripheral oedema (verapimil) |
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Losartan, Valsartan, Irbesartan |
Angiotensin Receptor Blocker (ARB).Competitivelyantagonises the stimulation of the angiotensin II AT1 receptorleading to selective inhibition of angiotensin II, a vasoconstrictor. Thisprevents angiotensin II dependant vasoconstriction and leads to vascular smoothmuscle relaxation and vasodilatation. Inhibited angiotensin II also lowers blood volume by decreasing aldosterone release, leading to natriuresis and diuresis. Uses: Hypertension 1st line, post-MI, heart failure, T2Dnephropathy Side effects: First dose hypotension, hyperkalaemia, acute renal f. |
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Glyceryl Trinitrate, Isosorbide Mononitrate, Isosorbide Dinitrate |
Nitrates bind tonitrate membrane receptors in vascular smooth muscle.Thenitrates are metabolised to form an NO group, whichstimulates guanylate cyclase to increase production of cGMP. Thisinhibits the entry of Ca2+ ions into the cell, and increases Ca2+ efflux, reducing intracellular Ca2+. This causesvasodilatation. Improved myocardial O2, reduced preload and O2 demand.
Uses: ISMN; angina prophylaxis. ISDN; angina at rest emergency Side effects: tachycardia, flushing, headache |
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Bendroflumethiazide |
Thiazide Diuretic. Inhibitsthe Na+Cl- cotransporter in the DCTwhich prevents the reabsorption of Na+ and Cl- in the cortical segmentof the DCT. Leads to; diuresis, natriuresis, and a reduction in blood volume andpressure. Uses: Hypertension (3rd line), oedema in HF (after loop diuretic used) Side effects: Hypokalaemia, Hyponatraemia, Hypercalcaemia, Impotence |
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Indapimide, Chlortalidone |
Thiazide-like Diuretic.Inhibitsthe Na+Cl- cotransporter in the DCTwhich prevents the reabsorption of Na+ and Cl- in the cortical segmentof the DCT. Leads to; diuresis, natriuresis, and a reduction in blood volume andpressure. Uses: Hypertension (3rd line), oedema in HF (after loop diuretic used) Side effects: Hypokalaemia, Hyponatraemia, Hypercalcaemia, Impotence |
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Spironolactone |
Aldosterone-dependent, Potassium SparingDiuretic. Targets the intracellular aldosteronereceptorsin the renal tubules and acts as a competitive antagonist. It inhibits the Na+/K+ exchange inthe DCT and collecting ducts, promoting K+retention, and Na+ and water loss, whichresults in weak diuresis and has a hypotensive effect.
Uses: oedema in CHF, primary hyperaldosteronism, acute renal failue Side effects: Impotence, testicular atrophy, hyperkalaemia |
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Amiloride |
Potassium SparingDiuretic – Aldosterone Independent.Itdirectly antagonises/blocks the epithelial sodium channel therefore inhibiting Na+ reabsorption in the late DCT and CD. This promotes the loss of Na+and water from the body, without depleting potassium as it decreases the K+secretion levels which subsequently decreases its excretion.
Uses: CHF with loop diuretic to prevent hypokalaemia Side effects: Hyperkalaemia, nausea, abdominal pain |
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Salbutamol, Salmeterol |
Beta 2 Agonists.Agonisesthe B2 adrenoceptors in bronchial smooth muscles. The activation ofthese receptors stimulates adenylate cyclase enzymes to increase production ofcAMP which causes bronchial muscle relaxation and therefore bronchodilatation. Salmeterol is a long acting "preventer" type medication.
Uses: COPD, asthma Side effects: tremor, muscle cramps, arrhythmias |
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Tiotropium Bromide |
LAMA. Competitive antagonist of muscarinic M3 receptors in both bronchial smooth muscles and mucous gland cells. Competes with the ACh, prevents ACh mediated bronchoconstriction. Inhibition of the ACh receptor signal results in smooth muscle relaxation and bronchodilatation as well as reduced mucous secretion.
Uses: COPD Side Effects: Dry mouth, constipation, urinary retention |
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Theophylline |
Xanthines. Competitive,non-selective phosphodiesterase(degrades cAMP and cGMP) inhibitor. Xanthines raise intracellular cAMP causing bronchial smoothmuscle relaxation.They blockadenosine receptors, which prevents diaphragmatic fatigue and inhibits leukotrienesynthesis therefore decreasing inflammation. Uses: COPD, asthma Side effects: Nausea, CNS stim. (anxiety), tachycardia |
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Montelukast |
Leukotriene ReceptorAntagonist. Bindsto cysteinyl leukotriene receptor CysLT1 in bronchial smooth muscle and acts asan antagonist to block their activation. This inhibits the normal action ofcysteinyl leukotrienes (which is a pro-inflammatory) in airway smooth muscletherefore reducing airway inflammation.
Uses: Asthma, bronchitis Side effects: Abdominal pain, thirst, headache |
