levobunolol (Betagan, Gotensin, Vistagan)

Introduction

Tradename: Betagan.

Indications

• open-angle glaucoma
• increased intraocular pressure

Contraindications

Caution:

• bronchial asthma
• sinus bradycardia
• 2nd & 3rd degree AV block
• heart failure

pregnancy category = c

safety in lactation = -

Dosage

• 0.5%: 1 drop OU QD-BID
• 0.25%: 1-2 drops OU BID

Solution: 0.25% (5 mL), 0.5% (5 mL, 10 mL, 15 mL).

Pharmacokinetics

• initial reduction of intraocular pressure in 1 hour
• maximal reduction of intraocular pressure in 2-6 hours
• duration of action: 24 hours

Adverse effects

• common (> 10%)
  • stinging/burning of eye
• less common (1-10%)
  • bradycardia, arrhythmias, hypotension, dizziness, headache, empyema, blepharitis, conjunctivitis, bronchospasm, alopecia
• uncommon (< 1%)
  • visual disturbances, keratitis, rash, pruritus

• drug adverse effects of beta-adrenergic receptor antagonists
• drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
• drug adverse effects of antihypertensive agents

Mechanism of action

• non-selective beta blocker
• reduces aqueous humor production
• may increase aqueous humor outflow
• produces reductions of intraocular pressure of 25-40%

More general terms

• non-specific beta-adrenergic receptor antagonist

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=39468
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3914
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=441415
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=34060
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5284409