Anti-hypertensive Medications Flashcards
Antihypertensive therapy
- Diuretics
- ACEI / AT1-R antagonist
- Ca-blocker
- Beta-blocker
Examples of ACEI
- Captopril
- Enalapril
- Ramipril
- Lisinopril
MOA of ACEI
Mechanism of action: inhibition of ACE → ↓ conversion of angiotensin I to angiotensin II
Main effects:
- ↓ Angiotensin II
- ↓ Vasoconstriction → ↓ blood pressure
- ↓ Secretion of aldosterone → ↓ reabsorption of Na+ and water → ↓ blood pressure
- Dilation of efferent arteriole → ↑ renal plasma flow → ↓ GFR → ↓ filtration fraction
- ↑ Renin secretion (due to lack of feedback inhibition) → ↑ angiotensin I - ↓ Breakdown of bradykinin → ↑ production of arachidonic acid metabolites → ↑ vasodilation → ↓ blood pressure
Clinical uses of ACEI
- Hypertension
- Cardiac failure
- Following myocardial infarction
- Renal insufficiency
Adverse effects of ACEI
- severe hypotension
- acute renal failure
- hyperkalemia
- angioedema & dry cough
Contraindication of ACEI
pregnancy
Examples of Ang II Receptor (AT1) blockers (ARB)
- Lorsartan
- Valsartan
- Candesartan
- Eprosartan
- Irbesartan
- Telmisartan
MOA of ARB
Mechanism of action: inhibition of angiotensin II receptor type 1 (AT1 receptor)
Main effects:
- ↓ Vasoconstriction → ↓ blood pressure
- ↓ Secretion of aldosterone → ↓ reabsorption of Na+ and water → ↓ blood pressure
- ↑ Renin secretion (compensatory) → ↑ angiotensin I → ↑ angiotensin II
Adverse effects of ARB
Less/no dry cough (unlike in ACEI)
Contraindication of ARB
Pregnancy
Examples of non-selective beta-blockers
- Proponolol
- Pindolol
- Carvedilol
Examples of cardioselective beta-blockers
- Atenolol
- Bisoprolol
- Metoprolol
Beta-blockers approved to treat heart failure
- Bisoprolol
- Metoprolol
- Carvedilol
Clinical uses of beta-blockers
- Hypertension
- Cardiac failure
- Following myocardial infarction
- Abnormal heart rhythm
- Anxiety disorders
Adverse effects of beta-blockers
- Hypotension
- Bradycardia
- AV nodal block
- Reduced exercising capacity
- Bronchoconstriction (esp. asthmatics)
- CNS: vivid dreams, clinical depression
MOA of beta-blockers
- Anti-ischemic effect: β1 blockade → ↓ heart rate and ↓ cardiac contractility → ↓ blood pressure (BP) and ↓ oxygen consumption by the heart → anti-ischemic effect
- Antiarrhythmic effect: β1 blockade → ↓ AVN conduction, ↑ AVN refractory time, and ↓ heart rate → anti-arrhythmic effect
- Anti-remodeling effect
Examples of Calcium Channel Blockers
- Nifedipine (DHP)
- Amlodipine (DHP)
- Verapamil
- Diltiazem
MOA of DHP CCB
CCBs bind to and block L-type calcium channels in cardiac and vascular smooth muscle cells → decreased frequency of Ca2+ channel opening in response to cell membrane depolarization → decreased transmembrane Ca2+ current
Effects of decreased Ca2+ influx:
1. Vascular smooth muscle relaxation → vasodilation → decreased peripheral vascular resistance → decreased afterload → decreased blood pressure
- Decreased cardiac muscle contractility (negative inotropic action) → decreased cardiac output → decreased blood pressure
- Decreased SA node discharge rate (negative chronotropic action) → decreased heart rate (bradycardia) → decreased cardiac output → decreased blood pressure
- Decreased AV node conduction (negative dromotropic action) → termination of supraventricular arrhythmias
Clinical use of CCB
- Antiarrhythmic (Class IV), anti-angina, anti-hypertension
- Anti-HTN: all equally effective
Vasodilator: Nifedipine (preferred choice for vasopastic angina) > diltiazem > verapamil - Cardiac depressant: verapamil > diltiazem > nifedipine
Adverse effects of CCB
- Hypotension
- Heart failure
- Myocardial infarction