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ANTI-HYERTENSIVE DRUGS: Therapeutic overview

This therapeutic overview by Dr. Busari A.A. provides detailed information on hypertension, including its definition, epidemiology, physiology of blood pressure, different classes of anti-hypertensive drugs, and non-pharmacological treatment options. The classification of drugs is discussed, along with their pharmacology and potential drug targets. This comprehensive guide is a valuable resource for healthcare professionals and researchers in the field of nephrology and hypertension.

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ANTI-HYERTENSIVE DRUGS: Therapeutic overview

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  1. ANTI-HYERTENSIVE DRUGS: Therapeutic overview DR BUSARI. A.A (MB.BS, M.Sc., MMCP, FWACP) Consultant Nephrologist & Lecturer Dept. Of Pharmacology, Therapeutics and Toxicology

  2. Outline • What is hypertension? • Epidemiology, Types and Classification • Physiology of Blood pressure • Classes of anti-hypertensive • Pharmacology of individual drugs. • Non- pharmacological treatment of hypertension • Conclusion

  3. What is hypertension? • Hypertension; Systemic arterial hypertension (HTN) • Defined as sustained elevated Blood Pressure(BP) ≥ 140/90mmHg. • Most common cardiovascular dx. • Asymptomatic in most cases. • Untreated, usually lead to complications such as stroke, heart failure, kidney failure, ischaemic heart dx and death.

  4. Epidemiology • Prevalence is increasing world wide. • 25% of adult population in the U.S. More prevalent in Nigeria 25- 30%. • Affect all races and gender. • Mainly 2 types • Primary (Essential) HTN – 90%, idiopathic, but associated risk factors • Secondary HTN – “RENVA”.

  5. Classification

  6. Physiology of Blood pressure • BP = Cardiac Output X Peripheral Vascular Resistance. • Arterial pressure affected by: • – the autonomic nervous system (fast) • – the renin-angiotensin system (hours or days) • – the kidneys (days or weeks)

  7. Physiology of Blood pressure

  8. Classification of anti-hypertensive by site or mechanism of action A. Sympatholylic drug • ß Adrenergic receptor antagonist (Beta blockers): • atenolol • metoprolol • nadolol • nebivolol • oxprenolol • pindolol • propranolol • timolol

  9. Classification of anti-hypertensive by site or mechanism of action 2. α Adrenergic receptor antagonist (alpha blockers): • Doxazosin • phentolamine • indoramin • phenoxybenzamine • prazosin • terazosin • tolazoline

  10. Classification of anti-hypertensive by site or mechanism of action 3. Mixed adrenergic antagonist: • carvedilol • labetalol • Bucindolol 4. Centrally acting agent/ α2 receptor agonist: • α -methyldopa • clonidine • guanabenz • guanfacine • Moxonidine 5. Adrenergic neuron blockers: • Reserpine • Guanadrel

  11. Classification of anti-hypertensive by site or mechanism of action B. Calcium channel blockers 1.dihydropyridines: • amlodipine • cilnidipine • felodipine • isradipine • lercanidipine • levamlodipine • nicardipine • nifedipine • nimodipine • nitrendipine 2. Non-dihydropyridines: • diltiazem • verapamil

  12. Classification of anti-hypertensive by site or mechanism of action C. Angiotensin-converting enzyme Inhibitors(ACEI): • captopril • enalapril • fosinopril • lisinopril • perindopril • quinapril • ramipril • trandolapril • benazepril

  13. Classification of anti-hypertensive by site or mechanism of action D. Angiotensin II receptor antagonists • candesartan • eprosartan • irbesartan • losartan • olmesartan • telmisartan • valsartan

  14. Classification of anti-hypertensive by site or mechanism of action E. Vasodilators • Aterialvasodialators • Hydralazine • Minoxidil • diazoxide 2. venous vasodialators • Sodium nitroprusside

  15. Classification of anti-hypertensive by site or mechanism of action F. Diuretics 1.Loop diuretics: • furosemide • bumetanide • ethacrynic acid • Torsemide 2. Thiazide diuretics: • epitizide • hydrochlorothiazide • bendroflumethiazide

  16. Classification of anti-hypertensive by site or mechanism of action 4. Thiazide-like diuretics: • indapamide • chlorthalidone • metolazone 5. Potassium-sparing diuretics: • amiloride • triamterene • spironolactone

  17. Potential drug targets: • Potential drug targets: • • CNS, ANS: decrease sympathetic tone • • Heart: decrease cardiac output • • Veins: dilate => decrease preload • • Arterioles: dilate => decrease afterload • • Kidneys: increase diuresis; inhibit RAA system

  18. Potential drug targets:

  19. Potential drug targets:

  20. Rational pharmacotherapy of hypertension. 1.Reduce LV systolic performance (reduce the ESPVR): negative inotropes (betablockers (metoprolol, atenolol, propranolol) and calcium channel blockers (verapamil, diltiazem)). 2. Reduce blood volume and thus drop LVEDV: diuretics (thiazide – hydrochlorothiazide, loop diuretics – furosemide, bumetanide and potassium sparing diuretics – spironolactone, amiloride, triamterene).

  21. Rational pharmacotherapy of hypertension. • 3.Reduce venous tone and thus venous return: Central sympatholytics such as clonidine act to reduce overall sympathetic tone. • 4. Reduce arterial tone (i.e. resistance) and thus reduce Ea: Effective arterial dilators include angiotensin converting enzyme inhibitors (ACE inhibitors – lisinopril, captopril), angiotensin receptor blockers (ARB’s – valsartan, losartan), calcium channel blockers (nifedipine, amlodipine), potassium channel openers (minoxidil), nitric oxide donors (nitroprusside), alpha1 blockers (prazosin, terazosin, doxazosin), and mixed alpha and beta-blockers (labetalol)

  22. THANK YOU

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