Published online by Cambridge University Press: 06 October 2020
THERAPEUTICS
Brands
• Sibelium
Generic?
• Yes
Class
• Calcium channel blocker, antihistamine
Commonly Prescribed for
(FDA approved in bold)
• Migraine prophylaxis
• Hemiplegic migraine prophylaxis
• Vasospasm in subarachnoid hemorrhage
• Adjunctive drug for epilepsy
• Vertigo
• Alternating hemiplegia of childhood
• Gilles de la Tourette syndrome
• Tinnitus
How the Drug Works
• Migraine/cluster: proposed prior mechanisms included inhibition of smooth muscle contraction preventing arterial spasm and hypoxia, prevention of vasoconstriction or platelet aggregation, and alterations of serotonin release and uptake.
• Prevention of cortical spreading depression may be one mechanism of action for all migraine preventives
• May also interact with other neurotransmitters, and may inhibit the synthesis and release of nitric oxide
• The drug also appears to act by blocking dopamine D2 receptors in a manner similar to antipsychotics
How Long Until It Works
• Migraines may decrease in as little as 2 weeks, but can take up to 2 months to see full effect
If It Works
• Migraine: 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 patient 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 agent or adding a second agent
Best Augmenting Combos for Partial Response or Treatment-Resistance
• Migraine: for some patients with migraine, low-dose polytherapy with 2 or more drugs may be better tolerated and more effective than high-dose monotherapy. May use in combination with AEDs, antidepressants, natural products, and non-medication treatments, such as biofeedback, to improve headache control
Tests
• Monitor ECG for PR interval
ADVERSE EFFECTS (AEs)
How the Drug Causes AEs
• Direct effects of calcium receptor antagonism and other CNS receptors. Antihistaminic properties likely cause weight gain and sedation. D2 blockade can cause movement disorders
Notable AEs
• Sedation, depression, weight gain are most problematic
• Nausea, dry mouth, gingival hyperplasia, weakness, muscle aches, and abdominal pain can occur
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