Question

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 in 1985 and marketed under the name 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 which, when ingested, releases hydrochloride at a constant, gradual rate into the body. Because of this altered mechanism of delivery, incidence of seizure with .buy.blogopt.com]-SR[/url] is comparable to, and in some cases, lower than that of other antidepressants.
In 1997, HCl was approved by the FDA for use as a smoking cessation aid. Because the name was still associated with high seizure risk, Glaxo subsequently marketed the drug under the name to help people by reducing the severity of withdrawal symptoms. It can be used in combination with nicotine replacement therapies. 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
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 \'s action is not known, but it is thought to be due to the effects on dopaminergic and noradrenergic mechanisms.
Pharmacokinetics
is metabolised in the liver. It has at least three active metabolites: hydroxy, threohydro and erythrohydro. These active metabolites are further metabolised to inactive metabolites and eliminated through excretion into the urine. The half-life of is 20 hours as is hydroxy\'s. Threohydro\'s half-life is 37 hours and erythrohydro\'s 33 hours.
Chronic hepatotoxicity in animals
In rats receiving large doses of chronically, there was an increase in incidence of hepatic hyperplastic nodules and hepatocellular hypertrophy. In dogs receiving large doses of 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 . 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 or , caused drug-seeking behaviour (animal experiments) and was recognized as an amphetamine-like drug by the humans. In a scale ranging from on the lower side to benzedrine, it was given an intermediate score indicating moderate likelihood of abuse. In clinical practise, 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. is not a controlled substance.
Limitation to tobacco withdrawal
In some countries is approved only as a smoking cessation aid and not for treatment of depression.
Influence on sexual function/
An advantage of over most conventional antidepressants is that it causes no sexual dysfunction in men and may even increase . According to a recent study, does also increase 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.

Answer

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 in 1985 and marketed under the name 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 which, when ingested, releases hydrochloride at a constant, gradual rate into the body. Because of this altered mechanism of delivery, incidence of seizure with .buy.blogopt.com]-SR[/url] is comparable to, and in some cases, lower than that of other antidepressants.
In 1997, HCl was approved by the FDA for use as a smoking cessation aid. Because the name was still associated with high seizure risk, Glaxo subsequently marketed the drug under the name to help people by reducing the severity of withdrawal symptoms. It can be used in combination with nicotine replacement therapies. 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
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 \'s action is not known, but it is thought to be due to the effects on dopaminergic and noradrenergic mechanisms.
Pharmacokinetics
is metabolised in the liver. It has at least three active metabolites: hydroxy, threohydro and erythrohydro. These active metabolites are further metabolised to inactive metabolites and eliminated through excretion into the urine. The half-life of is 20 hours as is hydroxy\'s. Threohydro\'s half-life is 37 hours and erythrohydro\'s 33 hours.
Chronic hepatotoxicity in animals
In rats receiving large doses of chronically, there was an increase in incidence of hepatic hyperplastic nodules and hepatocellular hypertrophy. In dogs receiving large doses of 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 . 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 or , caused drug-seeking behaviour (animal experiments) and was recognized as an amphetamine-like drug by the humans. In a scale ranging from on the lower side to benzedrine, it was given an intermediate score indicating moderate likelihood of abuse. In clinical practise, 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. is not a controlled substance.
Limitation to tobacco withdrawal
In some countries is approved only as a smoking cessation aid and not for treatment of depression.
Influence on sexual function/
An advantage of over most conventional antidepressants is that it causes no sexual dysfunction in men and may even increase . According to a recent study, does also increase 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.