Propranolol
Beta Blocker, Non-selective
Propranolol
Inderal
Propranolol was the first clinically successful beta blocker, introduced in 1964 by James Black. It is non-selective and lipophilic, it crosses the blood–brain barrier readily, which makes it uniquely useful for conditions with a CNS component (performance anxiety, akathisia, essential tremor, migraine prophylaxis) but also accounts for CNS side effects (vivid dreams, fatigue, depression).
Heart rate, blood pressure
Do not stop abruptly, taper to avoid rebound tachycardia, hypertension, or angina. Use with caution in asthma/COPD. May mask hypoglycemia symptoms in diabetics.
Metoprolol, Bisoprolol, Nebivolol
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Effects
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Pharmacokinetics
Absorption
~25% oral bioavailability due to high hepatic first-pass extraction.Distribution
Highly lipophilic; ~90% plasma protein binding; readily crosses the BBB.Metabolism
Hepatic via CYP2D6, CYP1A2, CYP2C19. Active metabolite: 4-hydroxypropranolol.Elimination
Renal excretion of metabolites; <1% unchanged in urine.Interactions
No interactions reported yet.
Monitoring
Patient counseling
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See also
References
Summary
Classes
Beta Blocker, Non-selective
Common uses
Hypertension0, Migraine prophylaxis0, Performance anxiety0, Essential tremor0, Akathisia0
Pharmacy
Starting dose
10–40 mg (situational anxiety); 40 mg BID (HTN)
Preparations
10, 20, 40, 60, 80 mg tabs; 60/80/120/160 mg ER caps; 1 mg/mL IV
US FDA Max
640 mg/d (HTN); 240 mg/d (migraine)
Pharmacology
Routes
Oral, IV
Onset
1–2 h (PO), immediate (IV)
Duration
6–12 h (IR); 24 h (ER)
Half-life
3–6 h
Bioavailability
~25% (extensive hepatic first-pass)
Pregnancy
Category C
Legal status
Rx-only in US
Purported mechanism
Non-selective competitive antagonist at β1 and β2 adrenergic receptors. Lipophilic; significant blood–brain barrier penetration, accounting for its CNS effects.