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Betaxolol

KERLONE

Pronunciation: be-TAX-oe-loel

Betaxolol ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Betaxolol ballicule

What it isBeta-1-selective antagonist; hypertension and pressure lowering in open-angle glaucoma.

Why this oneIt is the most cardioselective ophthalmic beta blocker, making bronchospasm less likely than with timolol.

What limits itEye drops still cause systemic bradycardia or bronchospasm, while pressure reduction is weaker than with timolol.

Betaxolol molecular structure (skeletal formula)
Molecular structure: Betaxolol

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
HypertensionAdults10 mg QD10-20 mg QD40 mg QD (studied; no added benefit >20 mg)
HypertensionSevere renal impairment / dialysis5 mg QDincrease by 5 mg/day q2wk20 mg/day
HypertensionElderly5 mg QD

Titration Wait 7-14 days before doubling dose; in renal impairment increase every 2 weeks

Renal Severe renal impairment/dialysis: initial 5 mg QD, titrate by 5 mg/day q2wk to max 20 mg/day

Hepatic No adjustment needed

Instructions

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy Category C — use only if potential benefit justifies risk; beta-blockers may reduce placental perfusion

Lactation Undefined

Cost

Betaxolol (KERLONE)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $/moCostPlus
10 mgtab30 qd$17.98not offered
20 mgtab30 qd$23.85offered

Generic entry1999

NO BOXED WARNINGS

Principal riskSystemic beta blockade; weaker than timolol

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

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