3P High Stakes Exam Practice

Pharmacology Study Guide –
Antihypertensives (NP Level)

1. ACE Inhibitors (e.g., Lisinopril, Enalapril, Captopril)
Indications

 Hypertension (especially in diabetes or CKD)
 Heart failure with reduced EF
 Post-MI (to reduce remodeling)
 Proteinuric CKD

Pharmacodynamics

 Inhibit conversion of angiotensin I → angiotensin II
 Decrease vasoconstriction, aldosterone secretion, and preload/afterload
 Increase bradykinin (vasodilator effect, but causes cough/angioedema)

Pharmacokinetics

 Mostly renally excreted (dose adjust in renal impairment)
 Onset: 1 hr; Duration: 24 hrs (longer in lisinopril, ramipril)

Safety & Contraindications

 Absolute: Pregnancy, history of angioedema, bilateral renal artery stenosis
 Caution: Renal impairment, hyperkalemia

Monitoring

 Baseline & follow-up: BMP (K+, creatinine, eGFR) within 1–2 weeks of initiation
 Monitor BP response, cough, angioedema

Key Notes

 First-line for HTN in diabetes and CKD
 Dry cough & angioedema = class effects




2. ARBs (e.g., Losartan, Valsartan, Olmesartan)

,Indications

 Hypertension (alternative to ACE if cough/angioedema)
 Heart failure
 Diabetic nephropathy

Pharmacodynamics

 Block angiotensin II receptor (AT1) → vasodilation, ↓ aldosterone
 Do not affect bradykinin (less cough/angioedema than ACEs)

Pharmacokinetics

 Hepatic metabolism (CYP2C9, CYP3A4)
 Mostly once daily dosing

Safety & Contraindications

 Absolute: Pregnancy, bilateral renal artery stenosis
 Caution: Renal impairment, hyperkalemia

Monitoring

 Same as ACEs (BMP: K+, creatinine, eGFR)
 BP response

Key Notes

 Better tolerated than ACEs; useful if ACE-induced cough
 Still risk of hyperkalemia & renal dysfunction




3. Calcium Channel Blockers (CCBs)
Dihydropyridines (Amlodipine, Nifedipine)

 Indications: HTN, angina, Raynaud’s
 MOA: Inhibit Ca2+ influx into vascular smooth muscle → vasodilation
 PK: Oral, hepatic metabolism (CYP3A4)
 Contraindications: Severe hypotension, caution in HF with reduced EF
 Safety: Peripheral edema, headache, flushing, gingival hyperplasia
 Monitoring: BP, HR, edema
 Key Notes: Amlodipine safe in HFrEF, others not preferred

Non-dihydropyridines (Verapamil, Diltiazem)

,  Indications: HTN, angina, rate control in atrial fibrillation
 MOA: Decrease AV node conduction → ↓ HR & contractility
 Contraindications: Severe LV dysfunction, AV block, bradycardia
 Safety: Bradycardia, constipation (esp. verapamil)
 Monitoring: HR, BP, ECG
 Key Notes: Avoid with beta-blockers (risk of brady/heart block)




4. Thiazide Diuretics (Hydrochlorothiazide, Chlorthalidone)
Indications

 First-line for uncomplicated HTN
 Synergistic with ACE/ARB

Pharmacodynamics

 Inhibit Na+/Cl– reabsorption in distal convoluted tubule → mild diuresis, ↓ BP

Pharmacokinetics

 Onset: 2 hrs, Duration: 6–12 hrs (longer for chlorthalidone)

Safety & Contraindications

 Absolute: Sulfa allergy (relative), anuria
 Safety: Hypokalemia, hyponatremia, hypercalcemia, ↑ uric acid (avoid in gout),
hyperglycemia

Monitoring

 BMP (Na+, K+, Ca2+, creatinine, glucose, uric acid)
 BP response

Key Notes

 More effective in Black and elderly patients
 Chlorthalidone stronger, longer acting than HCTZ




5. Beta Blockers (Metoprolol, Atenolol, Carvedilol,
Propranolol)

, Indications

 HTN (not first-line unless compelling indication: CAD, MI, HFrEF, arrhythmias)
 Angina, rate control, heart failure (carvedilol, metoprolol succinate, bisoprolol)

Pharmacodynamics

 Block beta-adrenergic receptors → ↓ HR, ↓ contractility, ↓ renin release

Pharmacokinetics

 Lipophilic (propranolol) vs hydrophilic (atenolol) → affects CNS penetration
 Hepatic metabolism (metoprolol, carvedilol) vs renal (atenolol)

Safety & Contraindications

 Absolute: Severe bradycardia, AV block, decompensated HF, asthma (nonselective)
 Safety: Fatigue, depression, sexual dysfunction, bronchospasm (nonselective)

Monitoring

 HR, BP
 Caution in diabetics (mask hypoglycemia symptoms)

Key Notes

 Not first-line for HTN unless compelling cardiac indication




6. Aldosterone Antagonists (Spironolactone, Eplerenone)
Indications

 Resistant HTN
 HFrEF (mortality benefit)
 Hyperaldosteronism

Pharmacodynamics

 Block aldosterone receptor in distal tubule → Na+ excretion, K+ retention

Pharmacokinetics

 Oral, hepatic metabolism