THERAPEUTICS

Brands

• Blocadren (oral), Betimol, Betim, Timoptic, Istalol (ocular solution)

Generic?

• Yes

Class

• β-blocker

Commonly Prescribed for

(FDA approved in bold)

• Migraine prophylaxis

• Hypertension

• Myocardial infarction (MI)

• Chronic open-angle glaucoma or ocular hypertension (ocular solution)

• Congestive heart failure (stable)

• Angina pectoris due to coronary atherosclerosis

• Prevention of variceal bleeding

How the Drug Works

• Migraine: proposed mechanisms include inhibition of adrenergic pathway, interaction with serotonin system and receptors, inhibition of nitric oxide production, and normalization of contingent negative variation. Prevention of cortical spreading depression may be one mechanism of action for all migraine preventives

How Long Until It Works

• Migraines: within 2 weeks, but can take up to 3 months on a stable dose to see full effect

If It Works

• In migraine, the goal is a 50% or greater decrease in migraine frequency or severity. Consider tapering or stopping if headaches remit for more than 6 months or if considering pregnancy

If It Doesn't Work

• Increase to highest tolerated dose

• Migraine: address other issues, such as medication overuse, other coexisting medical disorders, such as anxiety, and consider changing to another drug or adding a second drug

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Migraine: for some patients, low-dose polytherapy with 2 or more drugs may be better tolerated and more effective than highdose monotherapy. May use in combination with AEDs, antidepressants, natural products, and non-pharmacological treatments, such as biofeedback, to improve headache control

Tests

• None required

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Antagonism of β receptors

Notable AEs

• Bradycardia, hypotension, hyper or hypoglycemia, weight gain

• Bronchospasm, cold/flu symptoms, sinusitis, pneumonias

• Dizziness, vertigo, fatigue/tiredness, depression, sleep disturbances

• Sexual dysfunction, decreased libido, dysuria, urinary retention, joint pain

• Exacerbation of symptoms in peripheral vascular disease and Raynaud's syndrome