indication

Used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.

pharmacology

Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity. Oxprenolol is a lipophilic beta blocker which passes the blood-brain barrier more easily than water soluble beta blockers. As such, it is associated with a higher incidence of CNS-related side effects than hydrophilic ligands such as atenolol, sotalol and nadolol. Oxprenolol is an potent beta-blocker and should not be administered to asthmatics because it can cause irreversible airway failure and inflammation.

mechanism of action

Like other beta-adrenergic antagonists, oxprenolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Like propranolol and timolol, oxprenolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. It also blocks beta-2 adrenergic receptors located in bronchiole smooth muscle, causing vasoconstriction. By binding beta-2 receptors in the juxtaglomerular apparatus, oxprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Oxprenolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.

toxicity

Symptoms of overdose include abdominal irritation, central nervous system depression, coma, extremely slow heartbeat, heart failure, lethargy, low blood pressure, and wheezing.

biotransformation

Hepatic.

absorption

Oral bioavailability is 20-70%.

half life

1-2 hours

drug interactions

Acetohexamide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Chlorpropamide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Clonidine: Increased hypertension when clonidine stopped

Dihydroergotamine: Ischemia with risk of gangrene

Dihydroergotoxine: Ischemia with risk of gangrene

Disopyramide: The beta-blocker, oxprenolol, may increase the toxicity of disopyramide.

Epinephrine: Hypertension, then bradycardia

Ergonovine: Ischemia with risk of gangrene

Ergotamine: Ischemia with risk of gangrene

Fenoterol: Antagonism

Formoterol: Antagonism

Gliclazide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Glipizide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Glisoxepide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Glyburide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Glycodiazine: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Ibuprofen: Risk of inhibition of renal prostaglandins

Indomethacin: Risk of inhibition of renal prostaglandins

Insulin Glargine: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Isoproterenol: Antagonism

Lidocaine: The beta-blocker increases the effect and toxicity of lidocaine

Methyldopa: Possible hypertensive crisis

Methysergide: Ischemia with risk of gangrene

Orciprenaline: Antagonism

Pipobroman: Antagonism

Pirbuterol: Antagonism

Piroxicam: Risk of inhibition of renal prostaglandins

Practolol: Antagonism

Prazosin: Risk of hypotension at the beginning of therapy

Repaglinide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Salbutamol: Antagonism

Salmeterol: Antagonism

Terazosin: Increased risk of hypotension. Initiate concomitant therapy cautiously.

Terbutaline: Antagonism

Tolazamide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Tolbutamide: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Treprostinil: Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Verapamil: Increased effect of both drugs