chemical structure of clonidineClonidine tablets and transdermal patch
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Clonidine

Clonidine is a centrally acting antihypertensive (to lower high blood pressure) agent, used mainly for this purpose in the past. It has found new uses, including treatment of some types of neuropathic pain, opioid detoxification, and, off-label, to counter the side effects of stimulant medication such as Methylphenidate. It is also increasingly becoming a more accepted alternative to fight insomnia as the drug is less addictive than most prescription sleep aids. more...

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Because of the above effects, Clonidine is increasingly used in conjunction with stimulants to treat attention-deficit hyperactivity disorder ADHD where it's given late afternoon and/or evening for sleep and because it sometimes helps moderate ADHD associated impulsive and oppositional behavior and may reduce tics ref.

Mechanism of action

Clonidine is a centrally-acting alpha-2 agonist. It selectively stimulates receptors in the brain that monitor catecholamine levels in the blood. These receptors close a feedback loop that begins with descending sympathetic nerves from the brain that control the production of catecholamines (epinephrine, also known as adrenaline, and norepinephrine) in the adrenal medulla. By fooling the brain into believing that catecholamine levels are higher than they really are, clonidine causes the brain to reduce its signals to the adrenal medulla, which in turn lowers catecholamine production and blood levels. The result is a lowered heart rate and blood pressure, with side effects of dry mouth and fatigue.

An analogy would be the lowering the temperature of a house by holding a lit match under the thermostat connected to the furnace.

Administration

Clonidine is typically available as tablets (Catapres®, Dixarit®), as a transdermal patch (Catapres-TTS®), or as an injectable form to be given epidurally, directly to the central nervous system.

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Clonidine Reduces Tamoxifen-Induced Hot Flushes - Brief Article
From American Family Physician, 11/1/00 by Richard Sadovsky

Hot flushes, a set of vasomotor symptoms including a feeling of warmth, redness of the face and upper body, sweating and dizziness, are frequent postmenopausal symptoms. These symptoms are also the most common side effects associated with use of the antiestrogen agent tamoxifen. The symptoms can be severe and may interfere with daily activities and sleep, and may cause discontinuation of tamoxifen therapy. Now that tamoxifen is being used for longer periods in the treatment of early-stage breast cancer, hot flushes are becoming more pronounced. Clonidine hydrochloride is a centrally acting alpha-adrenergic agonist that reduces vascular reactivity and is currently used for treatment of hypertension. It has been shown to control hot flushes thought to be caused by nonadrenergic hyperactivity.

Pandya and associates performed a randomized, controlled trial to study the effect of clonidine on hot flushes in women taking tamoxifen for breast cancer. Postmenopausal women who had been receiving adjuvant tamoxifen therapy for breast cancer for at least one month and reported at least one hot flush per day were included. Patients with coronary artery insufficiency or symptomatic cardiac disease, syncope or symptomatic hypotension were excluded. Patients were randomized to receive oral clonidine, in a dosage of 0.1 mg daily, or placebo at bedtime for eight weeks. Self-report diaries were kept by participants of hot flush symptoms. A side effect checklist was also made available to all participants.

Both groups reported milder hot flush symptoms during treatment, but the reduction was greater in the clonidine group. A significant difference was seen in the mean changes in quality-of-life score at week 8. Difficulty sleeping was the only potential side effect reported significantly more often by the clonidine group.

The authors conclude that oral clonidine can reduce the frequency of tamoxifen-induced hot flushes in postmenopausal women with breast cancer for at least eight weeks. Baseline frequency of hot flushes did not influence patient response to clonidine treatment. The toxicity of oral clonidine was low at the dosage of 0.1 mg daily. Continued use of clonidine for longer periods would probably provide similar benefit, but this step requires further research.

COPYRIGHT 2000 American Academy of Family Physicians
COPYRIGHT 2000 Gale Group

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