Clonidine in Prophylaxis of Migraine

Running head: CLONIDINE
Clonidine in Prophylaxis of Migraine
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1CLONIDINE
Introduction
Migraine is a term which is commonly used to describe mild to severe headache. Due to
the physiological changes in the brain, a pain starts to develop which causes migraine associated
headaches and other symptoms. Studies show that migraine headaches have a positive relation
with light, sound and smell. Excessive light, certain disturbing sounds and foul and repugnant
smells often increases the intensity of migraine (1). The probable symptoms include vomiting or
nausea. Some patients complain that they experience pain on just one side of the brain while pain
on both sides of the brain are also reported. The migraine associated pain is often reported as a
throbbing or pounding pain. Designating all types and forms of headaches as migraine is not
appropriate because there is another form of headache which is associated with tension and it
occurs due to muscle contraction of the neck, face and scalp (2).
Boehringer Ingelheim Pharma decided to discover a peripherally active adrenergic
compound for nasal decongestion in the form of nose drops and task was given to to chemist
named Helmut Stahle. It was believed that decongestive agents are derived from imidazoline
structure. He ended up discovering Clonidine by introducing chlorine atoms as substituents in the
2- and 6- positions of the phenyl ring. It was found out that clonidine has more antihypertensive
activity than decongestant (5).
Clonidine is indicated in lowering blood pressure, used in the prophylaxis of vascular
migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms
associated with menopause, in conjunction with benzodiazepines for the treatment of alcohol
withdrawal, to manage nicotine dependence, use in the treatment of open-angle and secondary
glaucoma and attention-deficit hyperactivity (ADHD) is also treated (6).

2CLONIDINE
Clonidine acts by stimulation of the centrally active alpha 2A subtype of alpha adrenergic
receptors in the brainstem, causing decrease in sympathetic outflow of central nervous system.
Clonidine is imidazole derivative and metabolized by cytochrome P450 (CYP). Clonidine is
therapeutically active in lowering blood pressure in conjunction with other drugs. Clonidine is
also used in other conditions like neuropathy, smoking and alcohol cessation, attention deficit
syndrome, vascular headache, menopausal symptoms, diabetic diarrhoea, and restless leg
disorder. Clonidine was first approved in US in 1974 and still widely used for various
indications. Mostly clonidine is indicated in hypertension, but sometime also used for cancer
pain management, attention deficit syndrome and menopausal flushing in some parts of the
world. In NHS clonidine is mainly used for hypertension and menopausal flushing. Unlicensed
use of clonidine includes Tourette syndrome, sedation, migraine, and to alleviate symptoms of
alcohol, nicotine and narcotic withdrawal. Clonidine available in tablet (25mcg, 100mcg) and
injection (150mcg). Clonidine dose in adults is 50-100mcg three times daily, and can be
increased steadily 2nd or 3rd day until control achieved. Main side effects are sedation, fatigue,
bradycardia, dry mouth, headache, dizziness, postural hypotension, male impotence and
gastrointestinal tract disturbance. (1)