Atenolol
Atenolol
Tenormin
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Summary
Common uses
Hypertension (FDA, though displaced from first-line by JNC8 and contemporary guidelines)0, Angina pectoris (FDA)0, Post-myocardial-infarction secondary prevention (FDA)0, Atrial fibrillation rate control (off-label)0, Supraventricular tachycardia (off-label)0
Pharmacy
Starting dose
25-50 mg PO once daily; titrate to 100 mg/day
Preparations
Tablets 25, 50, 100 mg
US FDA Max
100-200 mg/day depending on indication
Pharmacology
Routes
Oral
Onset
BP effect within hours; full effect over 1-2 weeks
Duration
24 hours (once-daily dosing supported by long elimination)
Half-life
6-9 hours (substantially longer in renal impairment due to renal elimination)[1]
Bioavailability
~50% (oral)[1]
Pregnancy
Documented fetal growth restriction with chronic exposure; avoid in pregnancy if alternative β-blockers are appropriate. The β-blocker most consistently associated with intrauterine growth concerns[1]
Legal status
Rx-only in US
Purported mechanism
Selective β1-adrenergic receptor antagonist with minimal β2 activity at therapeutic doses, giving lower bronchoconstriction risk than non-selective β-blockers. Hydrophilic (unlike lipophilic propranolol and metoprolol), so it has very limited CNS penetration, giving much less CNS adverse-effect burden (depression, fatigue, vivid dreams) but correspondingly less migraine prophylactic efficacy compared to lipophilic β-blockers. Renally eliminated, so accumulates in renal impairment and requires dose adjustment by creatinine clearance.0 Contemporary hypertension guidelines (JNC8 and onward) have moved atenolol away from first-line antihypertensive use based on trial data showing inferior cardiovascular outcomes versus other antihypertensive classes, particularly in older patients[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Tenormin (atenolol), AstraZeneca/various, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018240s031lbl.pdf