Propranolol hydrochloride is a nonselective β-adrenergic blocking agent (β-blocker). Propranolol inhibits response to adrenergic stimuli by competitively blocking β-adrenergic receptors within the myocardium and within bronchial and vascular smooth muscle.
藥動學
Propranolol is almost completely absorbed from the GI tract. Propranolol is widely distributed into body tissues including lungs, liver, kidneys, and heart. Propranolol readily crosses the blood-brain barrier and the placenta. The drug is distributed into milk. Propranolol is almost completely metabolized in the liver and at least 8 metabolites have been identified in urine. Only 1–4% of an oral or IV dose of the drug appears in feces as unchanged drug and metabolites. The half-life during the initial phase (t?α) was 10 minutes and that during the terminal phase (t?β) was 2.3 hours.
禁忌症
Second to third degree heart block, bronchial asthma, cardiogenic shocks, sinus bradycardia, allergic rhinitis during the pollen season, hypoglycemia, metabolic acidosis.
懷孕分類
C
哺乳分類
Avoided, milk levels of propanolol with milk/plasma ratios from 0.2-1.5.
副作用
Severe bradycardia, congestive heart failure, hypotension, bronchospasm.
劑量和給藥方法
PO 10-40mg TID or QID, maintenance dose: 160-480mg/day. For emergency of cardiac arrhythmia: IV 1-3mg (less than 1mg/min), maximum dose: 10mg.
小兒調整劑量
Hemangioma, infantile; proliferating :
Infants and Children <5 years : Oral: Initial: 1 mg/kg/day in 2 or 3 divided doses, increase by 1 mg/kg/day at weekly intervals to maintenance dose; usual daily maintenance dose: 1 to 3 mg/kg/day in 2 or 3 divided doses; optimal duration not defined, duration ranged from 3 to 12 months; discontinuation of therapy may be gradually tapered over 1 to 3 weeks to prevent rebound sinus tachycardia.
腎功能調整劑量
No dosage adjustment necessary for any degree of kidney dysfunction ; use with caution, particularly in patients with more advanced kidney impairment.
肝功能調整劑量
Indications other than variceal hemorrhage prophylaxis:
Child-Turcotte-Pugh class A: IV, Oral: No dosage adjustment necessary.
Child-Turcotte-Pugh class B and C :
Initial: In general, administer 50% of the indication-specific dose no more frequently than twice daily; adjust dose based on response and tolerability no more frequently than every 3 to 5 days unless patient is under continuous medical supervision (eg, hospital admission), not to exceed the usual indication-specific recommended dose or dose interval; use with caution.
Variceal hemorrhage prophylaxis :
Child-Turcotte-Pugh class A to C: Oral: No dosage adjustment necessary
安定性
should be stored in a tightly sealed container, below 25°C, away from light and out of reach of children.