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Antihypertensive agents

This document discusses antihypertensive agents used to treat hypertension. It begins by defining hypertension as blood pressure above 140/90 mmHg. It then discusses the renin-angiotensin-aldosterone pathway which controls blood pressure. Various classes of antihypertensive agents are described, including beta-blockers, ACE inhibitors, calcium channel blockers, and diuretics. Specific drugs from each class are provided along with their mechanisms and uses for treating hypertension. The mechanisms of action are summarized for each drug class, such as how beta-blockers work by blocking epinephrine to slow the heart rate and lower blood pressure.

Education◦
ANTIHYPERTENSIVE AGENTS BY SWATHI KENCHA ASSISTANT PROFESSOR BANGALORE
HYPERTENSION A condition in which the force of the blood against the artery walls is too high is hypertension. What is Blood Pressure – Blood pressure is pressure of blood exerted on the walls of arteries.
• Hypertension is defined as blood pressure above 140/90,and is considered severe if the pressure is above 180/120. • Hypertension has no serious symptoms but if it is untreated,it can cause health conditions such as heart disease and stroke. • Primary Hypertension – The blood pressure is above normal for which no logical cause is known. • Renal Hypertension – This hypertension may also be induced due to the pathological conditions of the kidney.
SYMPTOMS OF HYPERTENSION • Dizziness • Feeling faint • Fast or irregular heartbeat • Feeling sick • Feeling more thirsty than normal • Blurred vision • Confusion &Tiredness • Breathing very fastly
RENIN-ANGIOTENSIN-ALDOSTERONE PATHWAY • This pathway controls Na⁺ secretion and body fluid volume. Reduced Blood Pressure Lowered sodium excretion Release of Renin Angiotensin Angiotensin-I Angiotensin-II Angiotensin-III B.P ACE
Angiotensin-II Angiotensin-III Vasoconstriction Aldosterone secretion Increased peripheral resistance Increased cardiac output Hypertension
ANTIHYPERTENSIVE AGENTS • Drugs that are used to control or manage the hypertension are called as antihypertensive agents. • Different types of antihypertensive agents to treat hypertension. • They work in different ways to control blood pressure.
CLASSIFICATION 1.β-blockers: Timolol,Propranolol 2.ACE inhibitors : Captopril,Enalapril,Lisinopril,Benazepril,Quinapril 3.Sympathetic agonist(α₂ agonist): Methyldopa,Clonidine, Guanithedine,Guanabenz 4.Vasodilators: Nitroprusside,Diazoxide 5.Diuretics:Hydrochlorthiazide,Spironolactone 6.Calcium channel blockers:Nifedipine,Felodipine,Verapamil 7.Angiotension-II Receptor antagonists: Losartan,valsartan 8.Miscellaneous: Reserpine,Hydralazine,Minoxidil
TIMOLOL Uses: Decreases systemic vascular resistance Used as antihypertensive
PROPRANOLOL Uses:β-blocker used in the treatment of hypertension.
CAPTOPRIL Uses: To treat hypertension,heart failure. To treat post myocardial infarction
LISINOPRIL ENALAPRIL BENAZEPRIL QUINAPRIL HCL
METHYLDOPA Uses:Methyldopa is used to treat high blood pressure It relaxes the blood vessels so that blood flows easily through the body.
CLONIDINE GUANETHIDINEMONOSULPHATE Uses: To treat hypertension α₂ agonist
GUANABENZ ACETATE Uses: To treat hypertension
SODIUM NITROPRUSSIDE DIAZOXIDE Uses: Vasodilators used for the treatment of hypertension
HYDROCHLORTHIAZIDE & SPIRONOLACTONE Uses:Spironolactone is used to treat Hypertension,Hyperaldosterinism and heart failure. Hydrochlorthiazide is used to treat edema because of heart and kidney problems.
NIFEDIPINE FELODIPINE VERAPAMIL Uses:Calcium channel blockers used to treat hypertension
LOSARTAN VALSARTAN Uses: Angiotensin II Receptor antagonists To treat hypertension
RESERPINE Uses:To treat hypertension To treat cardiac arrythmias
MINOXIDIL HYDRALAZINE Uses: Minoxidil used to treat acute hypertension Minoxidil also used for hair growth in alopecia androgenetica. Hydralazine is very useful in the treatment of hypertension.
MOA OF β-BLOCKERS • β-adrenergic blocking agents are drugs that reduce your B.P. • β-blockers work by blocking the effects of the hormone /neurotransmitter –epinephrine. • β-blockers causes heart to beat more slowly and with less force ,which lowers blood pressure. Eg:Timolol,Propranolol
MOA OF ACE INHIBITORS • ACE Inhibitors relaxes veins and arteries to lower blood pressure. • ACE Inhibitors prevents an enzyme(Angiotensin converting enzyme) in the body and blocks the production of angiotensin-II,a substance (peptide) that narrows blood vessels(vasoconstriction). • This narrowing can cause increase in B.P and forces heart to work harder.
VASODILATORS MECHANISM • Vasodilator drugs relaxes the smooth muscle in blood vessels,which causes blood vessels to dilate. • Dilation of arterial blood vessels leads to a reduced systemic vascular resistance . • This leads to fall in arterial blood pressure. Eg: sodiumnitroprusside and diazoxide
MOA OF α₂-AGONISTS • These drugs stimulate α-adrenergic receptors in the brain. • This action results in reduced sympathetic outflow from the CNS and decreases peripheral resistance,renal vascular resistance ,Heart rate and blood pressure. Eg:Methyldopa,clonidine,Guanethidine,Guanabenz
MOA OF DIURETICS • Thiazide diuretics enhance urinary excretion of both Na & H₂O by specifically inhibiting Na reabsorption located in the thick portion of the ascending limb of loop of henle and also in the distal tubule. • They also cause an increase in the excretion of Cl⁻,K⁺ and HCO₃⁻ ions. • Thiazide diuretics also minimizes the glomerular filtration rate. Eg: Chlorthiazide • Spironolactone competes with aldosterone at the specific receptor site located in the distal tubule and causes diuresis.
MOA OF CALCIUM CHANNEL BLOCKERS • Calcium channel blockers inhibits the inward movement(influx) of calcium ions and decreases contractility. Eg: Nifedipine,Felodipine &Verapamil
MOA OF ANGIOTENSIN-II RECEPTOR ANTAGONISTS Valsartan & Losartan INHIBITS
MECHANISM OF RESERPINE • It is an adrenergic blocking agent used to treat mild to moderate hypertension by disrupting norepinephrine vesticular storage. • The antihypertensive action of reserpine is a result by depleting catecholamines from peripheral sympathetic nerve endings.
MECHANISM OF MINOXIDIL • The antihypertensive activity of minoxidil is by opening ATP sensitive potassium channels in vascular smooth muscle and causes vasodilation.
SYNTHESIS OF METHYLDOPA
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