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Pharmacology of Hypertension Management by Mind Map: Pharmacology of Hypertension
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Pharmacology of Hypertension Management

Classes of hypertension



check every 2 years




check in one year

stage 1



confirm within 2 months

stage 2



Evaluate within 1 week to 1 month

should be treated at once if BP is greater than 180/110 mm Hg

non-pharmacological therapy

effective (alone) when diastolic BP is between 85 to 94

Reduction in salt intake

Weight reduction

every 1 Kg lower 2.5/1.5

Light physical exercise

30 minutes brisk walking most days of the week reduces B.P by 4-9

dietary approaches to stop hypertension (DASH)

diet high in fruits, vegetables and low fat dairy products

significantly reduces BP in about 8 weeks

diet rich in potassium and calcium, Potassium, direct vasodilator, increases the synthesis of bradykinin and natriuretic peptide, Calcium, enhances the secretion of a vasodilator peptide: Calcitonin Gene Related Peptide (CGRP), reduces the secretion of parathyroid hypertensive factor (PHF)

reduce alcohol intake

Cessation of smoking

Decrease caffeine intake

Psychological methods



Lifestyle modification


if not lowered to target limit within 3 to 6 months of lifestyle changes

start treatment

keep the lifestyle modifications


below 140/85 for non-diabetic

below130/80 in diabetic

British Hypertension Society: August 2011



types, Thiazides, hydrochlorothiazide, chlorthalidone, indapamide, used in mild to moderate hypertension with normal renal function, Loop diuretics, furosemide, might cause deafness (sometimes reversible), bumetanide, ethacrynic acid, used in acute edema due to congestive heart failure, Potassium sparing diuretics, spironolactone, aldersterone antagonist, gynecomastia, triamterene, amiloride, used in hyper aldosteronism and heart failure

mechanism, decreasing vascular resistance because sodium makes smooth muscle more stiff, recent studies, activating ATP-regulated K+ channels in arterioles, leading to membrane hyper polarization, which opposes Ca2+ entry and inhibiting contraction

clinical use, at least as effective as BBs, CCBs, and ACE inhibitors in reducing CV outcomes, particularly effective in preventing stroke and HF, good for elderly, effectively lower B.P in most patients from 10-15, for mild to moderate hypertension

adverse effects, hypokalemia (except for potassium sparing), problematic in patients with arrhythmia or acute MI, prevented with, low doses i.e.12.5 to 25 mg/day, diet rich in potassium, banana, spinach, dried apricot and orange juice, hyponatremia if they have HF, others, hyperuricemia, hypercalcemia, hyperglycemia, male sexual dysfunction

Inhibitors of Renin Angiotensin System

Angiotensin converting enzyme (ACE) inhibitors, types, Sulphydryl group, captopril, can be used for urgency, Dicarboxyl group, enalapril, Phosphorus containing drugs, fosinopril and ceronapril, all are equally effective. differ in potency, pro or active, and pharmacokinetics, other indications, cardiac failure, diabetic nephropathy, left ventricular systolic dysfunction, Mechanism, inhibits conversion of angiotensin I to angiotensin II, lead to accumulation of bradykinin, because angiotensin II degrades it, adverse effects, dry cough, hypotension, skin rash, protein urea, hyperkalemia, aldesterone responsible for secretion of potassium, acute renal failure, especially in patient with renal artery stenosis, Angiotensin II helps maintain adequate glomerular filtration, abnormalities in taste, angioneurotic edema, 0.1 to 0.2%, due to accumulation of bradykinin, or induction of tissue specific auto antibodies, fetal hypotension and renal failure, contraindicated during second and third trimesters of pregnancy, Interactions, NSAIDs, reduce the antihypertensive effect of ACE, by inhibiting bradykinin mediated vasodilatation, reported renal failure with aspirin and captopril use, Antacids (containing aluminum and magnesium hydroxide), reduce the bioavailability of captopril by 40%, azathioprine, reported Leucopenia with captopril, digoxin and lithium, ACE inhibitors may increase their plasma levels, ARBs, hypertension, hyperkalemia, and renal failure

Angiotensin receptor blockers (ARBs), types, losartan, has the highest potential for drug interactions due to P450 enzyme system, non (significant) reported, valsartan, candesartan, Mechanism, blocking the receptor for angiotensin II, Clinical use, if ACE didn't work, or if cough not tolerated, Side effects, hyperkalemia, muscular cramps, GIT complaints, headache and dizziness, Contraindications, hypersensitivity, pregnancy, interactions, lithium, increased renal reabsorption of lithium, toxicity, Digoxin, with Candesartan, monitor digoxin levels, Indomethacin, decreased effectiveness of losartan

Renin Inhibitors, Aliskiren

Calcium Channel Blockers

Types, Phenyl alkyl amines, verapamil, good for supraventricular arrhythmias, angina, Dihydropyridines, nifedipine, Immediate-release nifedipine not approved for hypertension due to increased CV risk, amlodipine, felodipine, cause reflex tachycardia, Benzothiazepines, diltiazem, vasodilator of the coronary arteries, All CCBs produce peripheral vasodilation and negative inotropic effect -> equally effective in lowering BP

Mechanism, blocking L type Ca+2 channels in blood vessels and myocardium, in smooth muscles, after Ca enters, it forms complex with protein calmodulin, calmodulin activates myosin light chain kinase (MLCK), activated MLCK causes phosphorylation of MLC, phospholyrated MLC initiates interaction between myosin and actin filaments leading to contraction, in cardiac cells, Ca++ troponin complex initiates contraction, Ca+ is important for initiating contraction, but still the cells have stores inside, block contractile process, dilate arterioles, reduce peripheral vascular resistance and myocardial force of contraction, lowering the blood pressure

Clinical use, not first line for hypertension, but they're effective especially in African-American patients., better used if you have CAD risks and diabetes

Side effects, constipation, flushing, edema, dizziness, headache and nausea, cough and wheezing, DHP produce reflex tachycardia

Interaction, digoxin and verapamil, digoxin toxicity, cimetidine, increased levels, cyclosporine, levels increased by Amlodipine and Diltiazem, CCBs inhibit the enzyme CYP 3A4 responsible for metabolism of cyclosporine, antifungal agents: itraconazole, fluconazole and ketoconazole, increase levels of CCBs, Cigarette smoke, reduce effects of nifedipine and verapamil, Rifampicin, increase CCB metabolism -> reduce efficacy, NSAIDs and oral anticoagulant, monitor symptoms of GIT haemorrhage

Sympatholytics or Sympathoplegic Agents

Centrally acting agents, types, methyldopa, with pregnancy first choice, clonidine hydrochloride, only used in particular situations due to potential adverse effects, during pregnancy, hypertensive urgency, adverse effects, sedation, dry mouth, mental depression, may cause sleep disturbances including nightmares

Ganglionic blocking agent, trimethaphan, only used in particular situations due to potential adverse effects, hypertensive emergencies

α Adrenergic Antagonist, types, prazosin, doxazosin, terazosin, phenoxybenzamine, management of pheochromocytoma before surgery in non malignant cases., indication, Use with with coexisting hyperlipidemia, benign prostatic hyperplasia, side effects, postural hypotension, nasal stuffiness, headache, failure of ejaculation in male

β Adrenergic Antagonists, types, propranolol, atenolol, metoprolol, indication, chronic hypertension associated with angina pectoris, first-line agents when there is coexisting coronary risk, MI, or heart failure, side effects, depression, sexual dysfunction, masking symptoms of hypoglycaemia in diabetes, selective β blockers are better in this aspect

Mixed Adrenergic Antagonists, labetalol, for urgency


Arterial vasodilators, hydralazine, mechanism, activation of potassium channels in arterial blood vessels (hyperpolarization of the cell membrane), release of endothelium derived relaxing factor (EDRF), which in turn activates guanylate cyclase, thereby increasing cyclic GMP, which relaxes smooth muscles., indication, preeclampsia first choice, hypertensive emergency in pregnancy, repeat in 30 minutes, IV in the dose of 10-20mg or I/M 10-50mg, heart failure and renal failure, used with isosorbide dinitrate, side effects, headache, nausea, flushing, hypotension, reflex, tachycardia and dizziness., immunological reactions e.g. lupus syndrome, occurs after 6 months of continuous use, minoxidil, mechanism, activation of potassium channels in arterial blood vessels (hyperpolarization of the cell membrane), Prodrug: require metabolic conversion by the enzyme sulphotransferase, formation of Minoxidil sulfate, more lipophilic and penetrates the vascular smooth muscles more easily, Indication, In men, side effects, hypertrichosis, increased hair growth that occurs on the face, arms, back and chest., Diazoxide, mechanism, activation of potassium channels in arterial blood vessels (hyperpolarization of the cell membrane), indication, hypertensive emergencies such as malignant hypertension, eclampsia, hypertensive encephalopathy, dose, initial 50 to 150mg than the dose repeat after an interval of 10-15 minutes, side effects, salt and water retention, tachycardia, hyperglycemia, all cause reflex tachycardia

Balanced vasodilator, sodium nitroprusside, for emergency, prazosin + ACEI