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  • Antihypertensive Agents Dr S. O. Olayemi

  • HYPERTENSIONChronically persistent elevated blood pressure>/=140 mm Hg systolic blood pressure and or diastolic >/= 90 mmHg in individual above 18 years of ageControlled BP SBP
  • Expert Committee on non Communicable diseasesOne third of Nigerian adults above 15 years of age are hypertensives, from this one third are aware of the hypertensive status, and one third are on treatment.Control definition?Complex?compliance/cost etc

  • TREATMENT GOALPrevent morbidity and mortality associated with high blood pressure.Achieving control through least intrusive means possibleControl other modifiable cardiovascular risk factors.

  • Ace Inhibitors:Captopril (Capoten) 12.5 150mg dailyEnalapril (Vasotec) 5 40 mg dailyLisinopril (Zestril) 5 40mg dailyRamipril (Tritace) 2.5 10mg dailyPerindopril (Aceon) 4 16 mg dailyFosinopril (Monopril) 5 40mg daily

  • Action: ACEI block conversion of Angiotensin 1 to Angiotensin 11 thereby blocking stimulation of aldosterone.Major site of Angiotensin II production Vessels and not the kidneys. reduce peripheral resistance and salt and water retention.Side Effect: Cough, Rashes, Leukopenia, Hyperkalaemia, Angio-Odema

  • ACE inhibitorsReduce dose in volume depleted pt, elderly(hypotension)May be combined with diuretics Hyperkalaemia CKD pts, potassium sparing diuretics and angiotensin receptor blockers.ARF- renal artery stenosisContraindicated in pregnancy and pt with hx of angioodema.

  • ANGIOTENSIN II RECEPTOR ANTAGONISTSLosartan (Cozaar) 50 100 mg dailyValsartan (Diovan) 80 320 mg dailyTemilsartan (Micardis) 20 80 mg dailyIrbesartan (Avapro) 150 300mg dailyOlmesartan (Benicar) 20 40 mg dailyCandesartan (Atacand) 8 32 mg daily

  • ANGIOTENSIN II RECEPTOR ANTAGONISTS: ARBsAction: They directly block the angiotensin II type 1 (AT1) receptors vasoconstriction, aldosterone release, sympathetic activation, ADH release, constriction of efferent renal arteriolesBeneficial AT2-vasodilation,tissue repair and inhibition of cellular growth in blood vessels (reduce peripheral resistance and salt/water retention)Side Effects: Rashes, Leukopenia,Hyperkalaemia but no cough

  • ARBsReduce dose in volume depleted pt, elderly(hypotension)May be combined with diuretics Hyperkalaemia CKD pts, potassium sparing diuretics and angiotensin receptor blockers.ARF- renal artery stenosisContraindicated in pregnancy Do not induce cough as in ACEIs

  • VASODILATORS ; Hydralazine (Apresoline 20 100 mg daily, Minoxidil (Loniten) 10 40mg daily, Action: They decrease peripheral resistance by dilating arteries/arterioles.Combined with diuretic/B blockers diminish fluid retention/reflex tarchycardia.Side Effect: Hydralazine (Headache, lupus-like syndrome), Minoxidil (Orthostasis, facial hirsutism), Diazoxide (Hyperglycaemia.


    Dihydropyridines :Nifedipine (Adalat/ProcardiA) 20 90 mg dly, I, Felodipine (Plendil) 5 20 mg dly, Amlodipine (Norvasc) 2.5 10 mg dlyNicardipine (Cardene) 60 120 mg dlyPhenylakylamine: Verapamil 100 400 mg dlyBenzothiazepine: Diltiazem 120 480 mg dly.Action: Reduce smooth muscle tone and cause vasodilation: may reduce cardiac output.Verapamil/diltiazem: decrease HR/delay A-V nodal conduction Supra ventricular tachycardia

  • Calcium channel blockersAvoid immediate release nifedipines etcDihydropyridines are more potent peripheral vasodilators compared to non-dihydropyridines.Side effect: Dihydropyridines reflex sympathetic discharge (tarchycardia) Headache, flushing, peripheral oedema.Non dihyropyridines variable heart block

  • DIURETICS Loop diuretics Frusemide (Lasix) 20mg 1 g, Bumetanide (Bumex) 0.5-4mg Torsemide (Demadex) 5mg dly.Site of Action: Loop of Henle, Reduce Na+/K+/Cl- cotransporter: reduce urine concentration; Increase calcium excretion.Preferrably morning/afternoon (avoid nocturnal diuresis)Higher doses in patients with CKD.Side effect: Ototoxicity, Hypokalaemia, Hypotension, Gout.


    Thiazides: Chlorthalidone (Hygroton) 6.25 25mg dly, Hydrochlorothiazides (Esidrix) 12.5 50mg dly Bendrofluazide 2.5 5mg dlySite of Action: Early distal tubule, they reduce NaCl reabsorption thereby reducing the diluting capacity of nephron. Decrease Calcium excretion.Dose in Morning (avoid noctunal diuresis)More effective antihypertensives than loops except in CKD (GFR

  • Potassium sparing diureticsAldosterone antagonist: Spironolactone (Aldactone) 25 50 mg dly, Epleronone (Inspra) 50 100 mg dlySite of Action: Cortical collecting tubule, They block Na+ channelsSide effects: Hyperkalemia, Sexual dysfunctionPotassium Sparing: Amiloride/hydrothiaz-Moduretic 5 10/50 100 mg dly, Triamterene/hydrothiaz 37.5 75/25 50 mg dlyAldosterone antagonist : Gynaecomastia.Action: Reduce extracellular fluid volume and thereby reduce vascular resistance

  • CENTRALLY ACTING DRUGS: Methyl dopa (Aldomet) 250mg 1g dly, Clonidine (Catapres) 0.1-0.8mg dly, Action:They inhibit Sympathetic Nervous System via Central Alpha 2 Adrenergic Receptors.Clonidine withdrawal Rebound BP elevationSide Effects : Somnolence, Orthostasis, Impotence, Rebound Hypertension RESERPINE (0.05-0.25mg) dly- Combined with diuretics-reduce fluid retention

  • BETA BLOCKERS Selective Cardioselective: Atenolol (Tenormin) 25 100 mg dly, Metropolol (Lopressor) 50 200mg dly, Bisprolol (Zebetal) 2.5-10mg dly Bexalolol (Kerlone) 5-20 mg dly.Non Selective: Propranolol (Inderal) 40-320mg dly, Nadolol(Corgard) 40 120mg dly, Timolol Blocaden) 10 40 mg dly.Intrinsic Sympathomimetic activity: Pindolol (Visken) 10 60mg dly, Penbutolol(Levatol) 10 40mg dly, Acebutolol (Sectral) 200 800 mg dly.Alpha and Beta Blockers: Labetalol (Trandate 200-800 mg dly, Carvedilol (Coreg) 12.5 50mg dly).

  • Beta BlockersActions: They reduce cardiac contractility and Rennin release.Additional benefit-Tarchyarrythmias,essential tremor, migraine headache and thyrotoxicosisSide Effect: Bronchospasm ( in severe asthma), bradycardia (A-V Block), Congestive Heart Failure exacerbation, impotence, fatigue, depression.Abrupt withdrawal-rebound hypertension.

  • Antihypertensive Medications indicated in specific Patient Population Diabetes with proteinuriaAce Inhibitors (ACEI)Congestive Heart FailureACEI, Diuretics +/-Beta BlockersIsolated systolic HypertensionDiuretics preferred: long acting dihyropyridine calcium channel blockers

  • CONTDMIBeta Blockers without intrinsic sympathomimetic activity, ACEIOsteoporosisThiazide diureticsBPHAlpha antagonistsPregnancyMethyldopa, Beta blockers, Labetalol, Hydralazine +/-calcium antagonists

  • Antihypertensives in pregnancyMethyldopa-preferred based on safety dataB Blockers- Safe, but IUGR reportedLabetalol-preffered over methyldopa because of fewer side effectsClonidine- Limited data availableCCBs-Limited data available, no teratogenicity with exposureDiuretics-not first line agents but probably safe in low dosesACEIs/ARBs- major teratogenicity on exposure

  • JNC 7 MANAGEMENT OF HYPERTENSIONPrehypertension 120-139/80-89- Life style modification.Stage 1 140-159/90-99-Thiazides, may consider ACEI,ARB, B Blockers Calcium blockers or a combinationStage 2 >160/>100 Two drug combination (usually a thiazide diuretic+an ACEI, an ARB, a B blocker, or calcium blocker



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