Verapamil for cluster headache. Clinical pharmacology and possible mode of action.

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Tfelt-Hansen P, Tfelt-Hansen J

Verapamil for cluster headache. Clinical pharmacology and possible mode of action.

Headache. 2009 Jan;49(1):117-25. doi: 10.1111/j.1526-4610.2008.01298.x.

PubMed ID

19125880 [ View in PubMed

]

Abstract

Verapamil is used mainly in cardiovascular diseases. High-dose verapamil (360-720 mg) is, however, currently the mainstay in the prophylactic treatment of cluster headache. The oral pharmacokinetics are variable. The pharmacodynamic effect of verapamil, the effect on blood pressure, also varies considerably among subjects. The dose of verapamil used for cluster headache is approximately double the dose used in cardiovascular disease, most likely because verapamil is a substrate for the efflux transporter P-glycoprotein in the blood-brain barrier. The access of verapamil to the central nervous system is therefore limited. The clinical use of verapamil in cluster headache is reviewed and several relevant drug interactions are mentioned. Finally, its possible mode of action in cluster headache is discussed. The effect of verapamil in cluster headache most likely takes place in the hypothalamus.Verapamil is an L-type calcium channel blocker but it is also a blocker of other calcium channels (T-, P-, and possibly N- and Q-type Ca(2+) channels) and the human ether-a-go-go-related gene potassium channel. With so many different actions of verapamil, it is impossible at the present time to single out a certain mode of action of the drug in cluster headache.

DrugBank Data that Cites this Article

Drugs

Verapamil

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Verapamil	Potassium voltage-gated channel subfamily H member 2	Protein	Humans	Unknown	Inhibitor	Details
Verapamil	Voltage-dependent L-type calcium channel subunit alpha-1C	Protein	Humans	Yes	Inhibitor	Details

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Verapamil	P-glycoprotein 1	Protein	Humans	Unknown	Substrate Inhibitor	Details