Antihypertensives drugs
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The document classifies drugs used to treat hypertension into 9 categories based on their mechanisms of action. These categories include drugs that act centrally, on autonomic ganglia, on postganglionic sympathetic nerve endings, on adrenergic receptors, directly on vascular smooth muscle, as potassium channel activators, by blocking the renin-angiotensin-aldosterone axis, oral diuretics, and miscellaneous drugs. Examples are provided for each category of antihypertensive drugs.
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Abnormalities in fluid volume and electrolyte composition are common and important clinical disorders. Drugs that block specific transport functions of the renal tubules are valuable clinical tools in the treatment of these disorders. Although various agents that increase urine volume (diuretics) have been described since antiquity, it was not until 1937 that carbonic anhydrase inhibitors were first described and not until 1957 that a much more useful and powerful diuretic agent (chlorothiazide) became available. Technically, a “diuretic” is an agent that increases urine volume, whereas a “natriuretic” causes an increase in renal sodium excretion and an “aquaretic” increases excretion of solute-free water. Because natriuretics almost always also increase water excretion, they are usually called diuretics. Osmotic diuretics and antidiuretic hormone antagonists (see Agents That Alter Water Excretion) are aquaretics that are not directly natriuretic.
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The document discusses different classes of diuretic drugs, including their mechanisms and effects. It describes loop diuretics like furosemide that inhibit sodium chloride reabsorption in the thick ascending limb of Henle's loop, increasing excretion of sodium and chloride in urine. It also discusses thiazide diuretics that act in the early distal tubule by inhibiting carbonic anhydrase and enhancing excretion of magnesium and potassium while inhibiting calcium and uric acid excretion. Finally, it mentions osmotic diuretics like mannitol that cause water retention in the proximal tubule through osmotic effects, resulting in water diuresis.
Antidiuretics
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ACE Inhibitors
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ACE Inhibitors
1. ACE inhibitors work by inhibiting the angiotensin converting enzyme and reducing angiotensin II levels, leading to vasodilation and sodium excretion.
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Hypertension is the most common cardiovascular disease determined by increase blood pressure (pressure exerted by blood against the wall of a blood vessel )in arteries.
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Hello friends, This is Akhila Gundabathini!! Here is the detailed information about antihypertensive drugs. Hope this presentation is helpful for you.. Thank You
Anti-hypertensive drugs
This document provides information about antihypertensive drugs. It defines hypertension as blood pressure higher than 140/90 mmHg according to WHO standards. It then discusses different classes of antihypertensive drugs including diuretics, beta blockers, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, and alpha blockers. For ACE inhibitors specifically, it explains their mechanism of inhibiting the conversion of angiotensin I to angiotensin II, thereby lowering blood pressure by decreasing peripheral vascular resistance. Common ACE inhibitors mentioned are captopril, enalapril, and lisinopril.
Anti hypertensive drugs
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Adrenonegative medications impair nerve impulse transmission in adrenergic synapses. They include adrenoblockers which block postsynaptic alpha-1, alpha-2, beta-1, and beta-2 adrenoreceptors, as well as sympatholytics which impair presynaptic transmission. Adrenoblockers are used to treat hypertension, heart failure, and benign prostatic hyperplasia by dilating blood vessels and reducing cardiac workload. Sympatholytics like guanethidine and reserpine also reduce blood pressure by impairing norepinephrine release from nerve endings. These drugs can cause side effects related to decreased adrenergic tone like weakness, dizziness, and orthostatic
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This document summarizes different types of antihypertensive drugs used to treat hypertension. It discusses sympatholytic agents including centrally acting agents and alpha/beta-adrenergic blockers. It also covers diuretics such as thiazides, loop diuretics, and potassium-sparing diuretics. The document explains vasodilators, calcium channel blockers, and ACE inhibitors as additional classes of antihypertensive drugs. It provides examples of drugs in each class and describes their mechanisms of action in lowering blood pressure.
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1.Introduction
2.Types of Hypertension
3.Risk factors
4.Classification of Anti-hypertensive Drugs
1.Diuretics :-
(a)Thiazides :-
Hydrochlorothiazide, Chlorthalidone, Indapamide
(b)Loop diuretics :-
Furosemide, Bumetanide, Torasemide
(c)Potassium sparing diuretics :- Spironolactone, Amiloride,
2. ACE inhibitors :-
Captopril,, Lisinopril, Enalapril, Ramipril,
3. Angiotensin blockers :-
Losartan, Candesartan ,Valsartan
4. Renin inhibitors :-
Aliskiren , Remikiren
5. β-adrenergic blockers :-
(a)Non selective :- Propranolol, Metoprolol Timolol,
(b)Selective :- Bisoprolol, Metoprolol, Atenolol
6. α-adrenergic blockers :-
(a)Selective :- Prazosin, Terazosin, Doxazosin
(b)Non Selective :- Phentolamine, Phenoxybenzamine
7. α-β, adrenergic blockers :-
Labetalol, Carvedilol
8. Calcium channel blockers :-
(a)L Type –Verapamil, Diltiazem, Efonidipine,
(b)Dihydropyridine -Nifedipine, Nicardipin, Lacidipine
9. Potassium channel openers :-
Minoxidil, Diazoxide,
10. Vasodilators :-
(a)Arteriolar dilator:- Hydralazine, Minoxidil,
(b)Arteriolar venodilator :- Sodium Nitroprusside
11. Centrally acting sympatholytics :-
Clonidine, α- methyldopa,
Anti-Hypertensive Drugs Medicinal Chemistry
Hypertension or high blood pressure is a chronic medical condition in which the blood pressure in the arteries is elevated i.e. 140/90 mmHg systolic /diastolic pressure.
High blood pressure has damaging effect on the heart, brain, kidneys and eyes.
Drugs used to lower blood pressure is known as antihypertensive drugs.
Antihypertensive drug therapy has improved remarkably in the last 50 years.
Before 1950, less effective and less tolerated antihypertensive drugs were available.
Veratrum and sodium thiocyanate could lower BP, but were toxic and difficult to use.
The ganglion blockers that were developed in the 1950s were effective, but inconvenient.
Reserpine was a breakthrough, but produced mental depression.
The therapeutic potential of hydralazine was not tapped fully because of the marked side effects when it was used alone
First choice drug in all grade of essential as well as renovascular hypertension (except renal artery stenosis).
This class of medicine works by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart.
Most patient require low doses which are well tolerated.
Example - Captopril, Enalapril, Lisinopril, Ramipril, Perindopril, Benazepril, Fosinopril, Quinapril, Trandolapril.
Large hydrophobic N-heterocyclic ring increase potency.
Ring showed contain –COOH group to mimic ACE substrate.
The Zn2+binding group may be
sulfhydryl (-CH2SH) like captopril
Di-carboxylate like in enalapril, lisinopril and quinapril
Phosphate like fosinopril
Sulfhydryl group shows superior binding to Zn ion and produces side effect like skin rash, taste disturbance etc.
Esterification of carboxylate or phosphate produce orally bioactive prodrug.
Large heterocyclic ring and hydrophobic ring generally N-containing increase potency and alter pharmacokinetic parameter.
Generally pyrrolidine ring is present (E.g. – Captopril, Enalapril)
The N-group must contain –COOH group to mimic the C-terminal carboxylate of ACE substrate.
X is usually methyl to mimic the side chain of aniline . This type of drug do not require prodrug for oral activity.
Drugs are : Losatran, Candesartan, Irbesartan, Valsartan, Telmisartan
The most prominent action of angiotensin II is vasoconstriction.
The two types of angiotensin II receptors are AT1 and AT2 , most of the action of angiotensin II are mediated by AT1 receptor.
Angiotensin receptor blockers do not affect bradykinin production.
Oral bioavibility – 33% (1st pass metabolism) It is partially carbonylated in liver to an active metabolism (E3174).
All ARB prevent and reverse all known effect of angiotensin-II including slow CNS effect, release of catecholamine, secretion of aldosterone, direct and indirect renal effect.
Telmisartan has additional PPAR-ϒ agonistic activity. This activity can help patient with dysglycemia.
There are thee functional groups that are the most important part f
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Antihypertensives drugs
- 1. CLASSIFICATION OF ANTIHYPERTENSIVES DRUGS PRESENTED BY:- Dr Nikhil Bansal J.N.M.C.,Wardha
- 2. The drugs used in the treatment of hypertension act by reducing the cardiac output and/or reducing the total peripheral resistance, without correcting the cause.
- 3. CLASSIFICATION:- 1)Drugs acting centrally. 2)Drugs acting on autonomic ganglia. 3)Drugs acting on the postganglionic sympathetic nerve ending. 4)Drugs acting on the adrenergic receptors. 5)Drugs acting on the vascular smooth muscle. 6)Potassium channel activators. 7)Drugs which block renin-angiotensin-aldosterone axis. 8)Oral diuretics. 9)Miscellaneous.
- 4. Drugs acting centrally:- (a)Alpha2 adrenergic receptor stimulants:- eg:- Clonidine and methyldopa (b) Selective imidazole receptor (I- receptor) Stimulant:- eg:- Moxonidine
- 5. Drugs acting on the autonomic ganglion:- Ganglion blocking agents eg:- Trimethaphan
- 6. Drugs acting on the postganglionic sympathetic nerve endings:- (a) Adrenergic neuron blockers eg:- Guaenethidine, Bethanidine, Debrisoquine, Bretylium. (b) Catecholamine depletors eg:- Reserpine
- 7. Drugs acting on adrenergic receptors :- (a) Alpha-adrenergic blocking agents eg:- Phentolamine, Phenoxybenzamine, Prazosine, Indoramine. (b) Beta-adrenergic blocking agents eg:- Propranol, Atenolol, Metopprolol. (c) Both alpha and beta adrenergic blocking drugs eg:- Labetalol
- 8. Drugs acting directly on the vascular smooth muscle:- (a)Arteriolar vasodilators eg:- Calcium channel blockers, Hydralazine, Diazoxide, Minoxidil (b) Arteriolar-venular vasodilators eg:-Sodium nitroprusside
- 9. . Potassium channel activators:- eg:-Diazoxide, Minoxidil, Pinacidil, Nicorandil.
- 10. Drugs which block renin-angiotensin- aldosterone axis:- (a)Those which block renin release eg:- Beta-adrenergic blockers (b) Those which block the conversion of angiotensin I to angiotensin II:- These drugs act by inhibiting the angiotensin converting enzyme (ACE) eg:- Captopril, Enalapril (c) Those which competitively block angiotensin II vascular receptors (ARB): eg;- Losartan. (d) Those which counterer the action of aldosterone (Aldosterone antagonist):- eg:- Spironolactone.
- 11. Oral diuretics:- eg:-Thiazides Miscellaneous:- eg:- Metyrosine
- 12. It must be emphasized that various antihypertensive drugs may ultimately reduce BP in humans by more than one mechanism.
- 13. THANK YOU