Bupropion
Drug Name: Generic Zyban ( Bupropion equivalent)
Zyban Bupropion is a tablet used to help quit smoking. Research has shown that this anti antidepressant medication approximately doubles the chances of quitting smoking at 3 months from quit date. Zyban is started before quitting smoking, with
a target date usually in the second week of taking Zyban. The generic version of zyban is a popular medication worldwide due to its price, affect and success history.
Drug Uses:
Zyban - Bupropion is widely used by smokers trying to quit the habbit. Research has shown that Zyban -
Bupropion is highy affective and doubles the chances of a smoker who want to stop smoking.
Drug Class Mechanism:
Zyban has an antidepressant action. However, its effect on quitting smoking may not be directly related to its antidepressant effects 2. Possible theories for how it works include blocking the effects of nicotine, reducing withdrawal or helping depressed mood.
How Taken:
ZYBAN - Bupropion should be swallowed whole and not crushed, divided, or chewed. Treatment with ZYBAN - Bupropion should be initiated while the patient is still smoking, since approximately 1 week of treatment is required to achieve steady-state blood levels
of bupropion. Patients should set a “target quit date” within the first 2 weeks of treatment with ZYBAN - Bupropion, generally in the second week.
Indications:
Zyban Tablets are indicated for the treatment of nicotine addiction as smoking cessation support.
Therapeutic action - Zyban - Bupropion tablets:
Pharmacodynamic properties:
Bupropion is a selective inhibitor of neuronal reabsorption of catecholamines (norepinephrine and dopamine) with minimal effect on reabsorption indolaminelor (serotonin), and does not inhibit monoamine oxidase. The mechanism by which bupropion enhances the
ability of patients to abstain from smoking is unknown. However, it is assumed that this action is mediated by noradrenergic mechanism and / or dopamine. In clinical trials, treatment with bupropion reduced the symptoms due to smoking cessation compared with
placebo and also showed evidence of a reduction in the need to smoke compared to placebo.
Pharmacokinetics:
Absorption following oral administration of bupropion tablets in healthy people volunteer, the peak plasma concentration of bupropion was reached in 3 hours. Bupropion and its metabolites show a linear kinetics, following chronic administration of 150-300 mg
/ day. Absorption bupropion is not significantly influenced by the ingestion of food.
Cast:
Bupropion is widely distributed with an apparent volume of distribution of approximately 2000 L. Bupropion and hydroxybupropion are moderately bound to plasma proteins (84% and 77%). Protein binding of the metabolite is about half that treohidrobupropion
of bupropion.
Metabolism:
Bupropion is extensively metabolised in the body. Were identified three pharmacologically active metabolite in plasma: hydroxybupropion and amino-alcohol isomers, and eritrohidrobupropion treohidrobupropion. They may have clinical importance, given that their
plasma concentrations are the same or higher as of bupropion. Peak plasma concentrations are achieved treohidrobupropion hydroxybupropion and approximately 6 hours after a single dose of Zyban. Eritrohidrobupropion can not be measured in plasma after only
one dose of Zyban. Active metabolites are further metabolised to inactive metabolites and excreted in the urine. In vitro studies indicate that bupropion is metabolised to the active metabolite hydroxybupropion mainly by CYP2B6, while cytochrome P450s involved
in the formation is not treohidrobupropion (see Drug Interactions and other forms of interaction). Bupropion and hydroxybupropion are relatively weak inhibitors of CYP2D6, with Ki values of 21, 13.3 mol respectively. Persons known to voluntary intense metabolism
of CYP2D6, coadministration of bupropion and desipramine resulted in increases of 2 and 5 times the Cmax and AUC of desipramine respectively. This effect persisted for at least 7 days after the last dose of bupropion. Since bupropion is not metabolised by
CYP2D6, it is anticipated that influence the pharmacokinetics of bupropion desipramine. Zyban with caution in the administration of CYP2D6 substrates (see Drug Interactions and other forms of interaction). Following an oral dose of 150 mg bupropion, have not
observed differences in Cmax, half-life, Tmax, AUC, or clearance of bupropion or its metabolites mainly between smokers and nonsmokers. Bupropion has been shown to induce its own metabolism in animals when administered subchronic. In humans, there is no evidence
of enzyme induction of bupropion and hydroxybupropion in volunteers or patients receiving recommended doses of bupropion for 10-45 days.
Elimination:
Following oral administration of 200 mg of 14C-bupropion in humans, 87% and 10% of the radioactive dose was observed in urine and faeces respectively. Only 0.5% of the bupropion dose was excreted unchanged. Less than 10% of the 14C dose was recovered in urine
as active metabolite. The apparent clearance after oral administration of bupropion is approximately 200 l / h and the average half-life of bupropion is approximately 20 hours. The half-life of hydroxybupropion is approximately 20 hours and reported the area
under the plasma concentration time curve (AUC) at steady state is about 17 times that of bupropion. Half-lives of treohidrobupropion and eritrohidrobupropion are higher (37 and 33 hours) and AUC values at steady state are 8 and 1.6 times that of bupropion.
Steady state of bupropion and its metabolites is reached in 8 days.
Patients with renal impairment:
the effect of renal disease on the pharmacokinetics of bupropion has not been studied. Elimination of the main metabolites of bupropion may be affected by reduced renal function (see Precautions for use).
Patients with liver damage:
half-life of hydroxybupropion is prolonged in individuals with liver disease due to alcohol, compared to healthy subjects of same age and weight (32.2 + / - 13.5 to 21.2 reported + / - 4.9 hours). Differences in half-life of bupropion and other metabolites
in the two patient groups were minimal.
Elderly:
Pharmacokinetic studies in elderly patients have shown variable results. A clinical trial of single dose pharmacokinetics showed that bupropion and metabolites of the elderly patients did not differ from that in young adults. Other pharmacokinetic studies with
single or multiple dose, has suggested that accumulation of bupropion and metabolites may be greater in elderly patients. Clinical experience has not identified differences in tolerability between elderly and younger patients, but greater sensitivity of older
patients can not be ignored.
Dosage and administration - Zyban - Bupropion tablets:
Adults:
It is recommended that treatment begin while the patient gave up smoking, with a date off target in the first two weeks of treatment with Zyban, preferably in the second week. The initial dose is 150 mg daily for three days, increasing to 150 mg twice a day.
There must be an interval of at least 8 hours between two successive doses. The maximum dose administered once should not exceed 150 mg and total daily dose should not exceed 300 mg. Patients should receive treatment at least 7 weeks. Discontinuation should
be considered if the patient has made progress towards stopping smoking until the seventh week of treatment, it is unlikely to quit during this attempt. Bupropion hydrochloride Systematic evaluation of 300 mg / day to prevent relapse demonstrated that treatment
up to 1 year is well tolerated and effective in preventing relapses. Since a large number of patients who have tried to quit smoking had numerous relapses, the need to continue taking Zyban for a long time to be determined on an individual basis. Recommended
dosage does not require modification if used in combination with Zyban Nicotine Transdermal Systems for nicotine dependence.
Children and adolescents:
safety and efficacy of Zyban tablets in patients under 18 have not been established.
Contra - Zyban - Bupropion tablets:
Zyban is contraindicated in patients with hypersensitivity to bupropion or any of the components of the preparation. Zyban is contraindicated in patients with seizures. Zyban is contraindicated in patients with previous or current diagnosis of bulimia or anorexia
nervosa, given the high incidence of seizures observed in patients after administration of bupropion. Concomitant administration of Zyban with monoamine oxidase inhibitors is contraindicated. Must pass at least 14 days between discontinuation of MAOI and initiation
of treatment with Zyban. Zyban tablets contain bupropion and should not be administered to patients currently treated with any preparation containing bupropion, given that the incidence of seizures is dose dependent.
Precautions - Zyban - Bupropion tablets:
The recommended dose of Zyban should not be exceeded, given that bupropion is associated with a risk of seizures depending on the dose. At doses up to the maximum recommended daily (150 mg Zyban twice daily), the incidence of seizures is approximately 0.1%
(1 / 1000). The risk of seizures when taking Zyban is closely related to the presence of predisposing factors. Thus, Zyban should be used with utmost caution in patients who have one or more conditions predisposing to lower seizure thresholds. These include:
history of head injury, tumors of the central nervous system (CNS), history of seizures, concomitant medications known to lower seizure threshold. In addition, attention to clinical circumstances associated with an increased risk of seizures. These include
alcohol abuse, alcohol and sedative abrupt end, hypoglycaemic or insulin-treated diabetes and the use of stimulants or anorectal products. Zyban should be discontinued in patients who have hypersensitivity or anaphylactic reactions (eg.'s Facial rash, itching,
hives, chest pain, swelling or shortness of breath) during treatment (see ADVERSE REACTIONS). Bupropion is extensively metabolised in the liver to active metabolites, which are then metabolized and excreted by the kidneys. Thus, treatment of patients with
kidney or liver disease should be initiated with a low dose, given the possibility of accumulation of metabolites in a higher than normal. The patient should be monitored because of the possibility of toxic effects due to increased blood and tissue levels
of bupropion and metabolites. Clinical experience has not identified differences in tolerability between patients and elderly adults. However, it can not be excluded greater sensitivity of some older patients. They are likely to show a decreased renal function,
making it necessary to administer the reduced frequency. Since the pharmacology of bupropion is similar to antidepressants, there is a risk that Zyban to precipitate manic episodes in bipolar patients with severe depression phase and can activate a latent
psychosis in susceptible patients. Before treatment with Nicotine Transdermal combination System (NTS), the physician should consult the prescribing information for NTS. When using combination therapy is recommended for emergency treatment to increase blood
pressure.
Drug interactions and other forms of interaction:
Physiological changes due to smoking cessation, with or without treatment with Zyban, may affect the pharmacokinetics of concomitant medications. In vitro research has shown that bupropion is metabolised to the main active metabolite hydroxybupropion, primarily
by cytochrome P450 IIB6 (CYP2B6) (see Pharmacokinetics). Attention, therefore, the concomitant use of Zyban with other medicines known to affect the CYP2B6 isoenzyme (eg. Orphenadrine, cyclophosphamide, ifosfamide). Although bupropion is not metabolized by
CYP2D6, in vitro studies conducted on humans have shown that bupropion and hydroxybupropion are inhibitors of CYP2D6 pathway. In pharmacokinetic studies conducted in humans, bupropion administration increased plasma levels of desipramine. This effect persisted
for at least 7 days after the last dose of bupropion. Concomitant use of Zyban with other drugs metabolized by CYP2D6 has not been studied. Thus, concomitant treatment with these drugs predominantly metabolised by this isoenzyme (such as beta blockers, antiarrhythmics,
SSRIs, TCA, antipsychotics) should be started in low dose. If Zyban is inserted into the treatment regimen of a patient who is given drugs metabolised by CYP2D6 should be considered lower initial dosage of drugs, especially for drugs with limited therapeutic
index (see Pharmacokinetics). Since bupropion is extensively metabolized, coadministration of drugs which induce metabolism (eg. Carbamazepine, phenobarbital, phenytoin) or inhibit metabolism might affect clinical work. Limited clinical data suggest an increased
incidence of adverse effects in patients treated with levodopa. Administration in patients receiving levodopa Zyban should be monitored carefully.
Pregnancy and Lactation:
The safety of Zyban during pregnancy has not been established. Evaluation of experimental animal studies do not indicate direct or indirect harmful effects on embryonic and fetal development, the course of pregnancy and prenatal or postnatal development. A
fertility study in rats showed no evidence of impaired fertility. However, animal reproduction studies are not always predictive of human responsiveness, so that Zyban should be used during pregnancy only if the beneficial effect is greater than the potential
risks. Since bupropion and its metabolites are excreted in breast milk, mothers should be advised not to breast feed while taking Zyban.
Effects on ability to drive and use machines:
As with other CNS-acting drugs, bupropion may affect ability to perform actions that require discernment or motor or cognitive skills. Before driving or using equipment, patients should check carefully whether Zyban does not adversely affect performance.
Overdosage has been reported Acute ingestion of doses 10 times the maximum therapeutic dose. In addition to the side effects listed, can appear symptoms including drowsiness, hallucinations and unconsciousness.
Treatment:
In the event of an overdose, hospitalization is recommended. Provide airway, oxygenation and adequate ventilation. Gastric lavage may be indicated if performed soon after ingestion. Using an activated charcoal may also be recommended. There is no known specific
antidote for bupropion .
Side effects - Zyban - Bupropion tablets:
The list below provides information on adverse reactions identified during clinical experience, by system. Corp. (general): fever, chest pain, asthenia.
Cardiovascular: tachycardia, vasodilation, postural hypotension, increased blood pressure, flushing, syncope.
CNS: Depression of seizures (see Precautions for use), insomnia, tremor, concentration disturbance, headache, dizziness, depression, confusion, agitation, anxiety.
Endocrine and metabolic: Anorexia.
Gastrointestinal: dry mouth, gastrointestinal damage, including nausea and vomiting, abdominal pain, constipation.
Skin / Hypersensitivity: Rash, pruritus, sweating. Hypersensitivity reactions from urticaria to angioedema, dyspnoea / bronchospasm and rarely anaphylactic shock. Arthralgia, myalgia and fever have also been reported in association with rash
and other symptoms suggesting Delayed hypersensitivity. Erythema multiforme and Stevens-Johnson syndrome have also been rarely observed.
Senses: tinnitus, impaired vision, impaired taste.
Storage:
Zyban - Bupropion like most medication pills require a dry cool storage to guaranty drugs quality for best results.
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