A.14

Question 1

β-receptor antagonist

Answer 1

1. Non-selective β-antagonists:
   Propranolol,
   Carvedilol,
   Timolol,
   Sotalol,
   2.β1-selective antagonists:
   Metoprolol,
   Bisoprolol,
   Nebivolol,
   Esmolol

Question 2

Propranolol

Answer 2

MOA: non-selective β-antagonist;
ROA: p.o, parentral;
Effect: HR↓→diastolic perfusion↑→O2 demand↓;
IND: HTN, angina pectoris, antiharrhythmic class II (treatment+prophylaxis), Migraine (prophylaxis), Essential tremor, glaucoma, Pheochromocytoma;
SEs: sedation, sleep disturbances;
Extra: Lipophilic→cross BBB, reduces mortality in patients with stable angina

Question 3

Timolol

Answer 3

MOA: non-selective β-antagonist;
ROA: topical;
Effect: Decreased aqueous humor secretion;
IND: Glaucoma

Question 4

Sotalol

Answer 4

MOA: non-selective β-antagonist + (K+ ch. blocker); ROA: p.o; Effect: ↓HR+AV conduction;
IND: Anti-arrhythmic class III → supraventricular +ventricular tachycardia;
SEs: Torsades-de-Pointes (uncommon ventricular tachycardia)

Question 5

Carvedilol

Answer 5

MOA: α1-antagonist, β-antagonist;
ROA: p.o., i.v;
IND: HTN, CHF, chronic stable angina;
Extra: Antioxidant properties (↓production of free radicals)

Question 6

Metoprolol

Answer 6

MOA: β1-selective antagonist;
Dosage: 2x25-100mg;
Effect: local anesthetic effect (inhibit Na+-channels) ; IND: HTN, chronic stable angina, CHF, ACS, anti-arrhythmic class II;
SEs: Nightmares, lethargy, bradycardia;
Extra: Lipophilic → can cross BBB

Question 7

Bisoprolol

Answer 7

MOA:β1-selective antagonist;
IND: HTN, chronic stable angina, CHF;
Extra: lipophilic→penetrates BBB;
DOA: long- 10-12h

Question 8

Nebivolol

Answer 8

MOA: β1-selective antagonist;
Effect: NO-dependent vasodilation - better for young males;
IND: HTN, CHF;
Extra: lipophilic→can penetrate BBB

Question 9

Esmolol

Answer 9

MOA: β1-selective antagonist;
ROA: i.v infusion;
Effect: ultrashort effect (9 min);
IND: Perioperative HTN/tachycardia, SVT, atrial fibrillation;
Extra: applied in acute cases, does NOT cross BBB