quit_smoking
Dołączył: 26 Gru 2005
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 Wysłany: Pon 16:13, 26 Gru 2005 Temat postu: Still smoking? This help you to quit! |
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History
[link widoczny dla zalogowanych] was first synthesized by Burroughs Research in 1966, and patented by Burroughs-Wellcome (later Glaxo-Wellcome, and, as of 2000, GlaxoSmithKline) in 1974. It was approved by the [link widoczny dla zalogowanych] in 1985 and marketed under the name [link widoczny dla zalogowanych] as an antidepressant, but clinical trials indicated that incidence of seizure was two to four times greater than other antidepressants and the drug was quickly pulled from the market. Glaxo, realizing that seizure risk was a function of dosage, then developed and marketed a sustained-release (SR) version of [link widoczny dla zalogowanych] which, when ingested, releases [link widoczny dla zalogowanych] hydrochloride at a constant, gradual rate into the body. Because of this altered mechanism of delivery, incidence of seizure with [link widoczny dla zalogowanych].buy.blogopt.com][link widoczny dla zalogowanych]-SR[/url] is comparable to, and in some cases, lower than that of other antidepressants.
In 1997, [link widoczny dla zalogowanych] HCl was approved by the FDA for use as a smoking cessation aid. Because the name [link widoczny dla zalogowanych] was still associated with high seizure risk, Glaxo subsequently marketed the drug under the name [link widoczny dla zalogowanych] to help people [link widoczny dla zalogowanych] by reducing the severity of withdrawal symptoms. It can be used in combination with nicotine replacement therapies. [link widoczny dla zalogowanych] treatment course lasts for seven to twelve weeks, with the patient halting the use of tobacco around ten days into the course.
Mode of action
[link widoczny dla zalogowanych] is a selective catecholamine (norepinephrine and dopamine) reuptake inhibitor. It has only a small effect on serotonin reuptake. It does not inhibit MAO. The actual mechanism behind [link widoczny dla zalogowanych]\'s action is not known, but it is thought to be due to the effects on dopaminergic and noradrenergic mechanisms.
Pharmacokinetics
[link widoczny dla zalogowanych] is metabolised in the liver. It has at least three active metabolites: hydroxy[link widoczny dla zalogowanych], threohydro[link widoczny dla zalogowanych] and erythrohydro[link widoczny dla zalogowanych]. These active metabolites are further metabolised to inactive metabolites and eliminated through excretion into the urine. The half-life of [link widoczny dla zalogowanych] is 20 hours as is hydroxy[link widoczny dla zalogowanych]\'s. Threohydro[link widoczny dla zalogowanych]\'s half-life is 37 hours and erythrohydro[link widoczny dla zalogowanych]\'s 33 hours.
Chronic hepatotoxicity in animals
In rats receiving large doses of [link widoczny dla zalogowanych] chronically, there was an increase in incidence of hepatic hyperplastic nodules and hepatocellular hypertrophy. In dogs receiving large doses of [link widoczny dla zalogowanych] chronically, various histologic changes were seen in the liver, and laboratory tests suggesting mild hepatocellular injury were noted.
Indications
management of depression
adjunctive in tobacco withdrawal
attention deficit disorder
Contraindications
epilepsy and other conditions that lower the seizure-threshold (alcohol withdrawal, active brain tumors etc.)
concomitant treatment with MAO-Inhibitors
caution with the concomitant use of sympathomimetic drugs (e.g. Ephedrine)
active liver damage (e.g. cirrhosis)
anorexia, bulimia
severe kidney disease
severe hypertension
anxiety disorders (caution), agitated patients
pediatric patients (see below)
use considerable caution in treating patients where suicide may be a risk
Interactions
Quite a great number of drugs show clinically significant interactions with [link widoczny dla zalogowanych]. Study the packing insert carefully and ask your prescribing physician in any case of doubt.
Abuse liability
In animal studies and small studies with persons having experience with the use of [link widoczny dla zalogowanych] or [link widoczny dla zalogowanych], [link widoczny dla zalogowanych] caused drug-seeking behaviour (animal experiments) and was recognized as an amphetamine-like drug by the humans. In a scale ranging from [link widoczny dla zalogowanych] on the lower side to benzedrine, it was given an intermediate score indicating moderate likelihood of abuse. In clinical practise, [link widoczny dla zalogowanych] has been shown that the dose required for significant abuse would cause seizures in most patients. Abuse has not become a significant problem in clinical usage, but the drug should be given with caution to patients with a history of drug or alcohol abuse or dependence. [link widoczny dla zalogowanych] is not a controlled substance.
Limitation to tobacco withdrawal
In some countries [link widoczny dla zalogowanych] is approved only as a smoking cessation aid and not for treatment of depression.
Influence on sexual function/[link widoczny dla zalogowanych]
An advantage of [link widoczny dla zalogowanych] over most conventional antidepressants is that it causes no sexual dysfunction in men and may even increase [link widoczny dla zalogowanych]. According to a recent study, [link widoczny dla zalogowanych] does also increase [link widoczny dla zalogowanych] in women with \"hypoactive sexual desire disorder\" but without signs of depression. It is too early to come to conclusive evidence whether to treat these women or not. Further controlled studies are required.
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