Angiotensin converting enzyme (ACE) inhibitors are commonly used to treat hypertension by preventing the formation of angiotensin II and aldosterone, both of which raise blood pressure. ACE inhibitors are considered first-line treatment for hypertension and are especially useful for patients with diabetes, renal disease, or heart failure. While generally well-tolerated, ACE inhibitors can cause side effects like dry cough, hyperkalemia, and the rare but potentially severe angioedema.
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Pharmacology Notes
Angiotensin converting enzyme (ACE) inhibitors are commonly used to treat hypertension by preventing the formation of angiotensin II and aldosterone, both of which raise blood pressure. ACE inhibitors are considered first-line treatment for hypertension and are especially useful for patients with diabetes, renal disease, or heart failure. While generally well-tolerated, ACE inhibitors can cause side effects like dry cough, hyperkalemia, and the rare but potentially severe angioedema.
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ANTIHYPERTENSIVE DRUGS
Hypertension is an elevation of systolic
and/ordiastolicBP above 140/90 mm of Hg It is a common cardiovascular condition. Hypertension may be primary (essential) hypertension-where the cause is not known or secondary-when it is secondary to other conditions like renal, endocrine or vascular disorders. Based on the degree of severity, hyper- tension can be graded as in Table 6.5: Table 6.5: Grading of blood pressure
Category SBP mmHg DBP mmHg
Normal <120 and <80
Prehypertension 120-139 or 80-89
Hypertension Stage1 140-159 or 90-99
Hypertension Stage 2 2160 or 2100
Abbreviations: SBP-systolic blood pressure;
DBP-diastolic blood pressure
Blood pressure is determined by
cardiac output (CO) and total peripheral vascular resistance (PVR),5 Blood pressure iscontroled by baroreceptor retlexes acting through autonomic nervous system along with the renin-angiotensin-aldosterone System. System, renin-angi0 sodium and water balancee channels or Chabr Sup plasma volume). DD Classification Diuretics Thiazides: Hydrochlorothiazide, chlorthalidone, etc. 11cal Loop diuretics: Furosemide, bume- tanide Po K'Sparing diuretics: Spironolactone, amiloride, triamterene 2Drugs acting on renin angiotensin system A P Angiotensin converting enzyme in- hibitors: Captopril, enalapril, lisinoo- Alu pril, ramipril, fosinopril, benazepril. Angiotensinl receptor antagonist: Losartan, candesartan, valsartan irbesartan, olmesartan. Renin inhibitor: Aliskiren. Agren 3. Sympathelytics Centoa Centrally acting drugs: Clonidine, methyldopa Arud Ganglion blockers: Trimethaphan Arud
Muhr9Adrenergic receptor blockers:
B-blockers: -
etc. Propranolol, atenolol
a-blockers: Prazosin Mixed a- and carvedilot. B-blockers: Labetalol 4/ Vasodilators (Arteriolar dilators:Hydralazine, minoxidilkdiazOxide Arteriolar and venular Sodium nitroprusside dilators: Renin Angiotensin System Drugs Acting on
Afgiotensin Converting Enzyme (ACE)
Kibitors powerful vasoconstrictor. Angiotensin II is a
Aldosterone also raises the BPby increasing
the plasma volume Fig. 6.4). ACE inhibitors prevent the formation of angiotensin II Angiotensinogen Renin 24 Angiotensin I ACE ACE inhibitors Vasoconstriction Angiotensin ll oso BP Angiotensin lll Salt Aldosterone and water t Blood volume retention Fig. 6.4:Renin-angiotensin system Uses (HC M Sc) 1 Hypertension ACE inhibitors are useful in the treatment of hypertension ofall grades due to all causes. Addition of a diuretic potentiates their efficacy. They are presently the first line anti- hypertensives. (Table 6.7). They are spe- cially indicated as antihypertensives in: Patients with diabetes as ACE-Tslow the development of nephropathy) Renal diseases-ACE inhibitors slow the progression. Left ventricular hypertrophy -is gradually reversed by ACE inhi- itos CCEÁCE inhibitors.are the first line drugs (Cuptop0l CMpml 3 Myocardial infarction ACE inhibitorsenala started within 24 hours andgiven for ph severalweeks prevent the development of CCF and reduce mortality 4 Coronary artery disease: In patients who are at a high-risk of ischemic cardiovascular conditions like MI and stroke, ACEinhibitors afford significant benefit by reducing the risk of MI strokeand sudden death 5. Chronic renal failure: In patients with diabetic nephropathyand chronicrenal failure, ACE inhibitors delay the pro gression of renal disease 6.Scleroderma renal crisis: ACE inhi- bitors may be life-saving in these patients. Adverse effects:/ ACE inhibitors are well- tolerated. Adverse effects include dry cough (due to raised bradykininpersistent levels) hyperkalemia, alteration of taste sensation, skin rashes, hypotension, headache, nausea, abdominal pain andblood disorders Angioedema though rare can be severel At thefirst sign of angioedema ACE inhibitors should be stopped.