Bupropion modified release tablets
- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Modified release tablets containing bupropion hydrochloride
Indicated as an aid to smoking cessation in combination with motivational support in nicotine-dependent patients.
It is recommended that treatment is started whilst the patient is still smoking and a target stop date set within the first two weeks of treatment with bupropion, preferably in the second week.
Bupropion should be used in accordance with current smoking cessation guidelines. The patient's motivation to quit should be assessed before commencing therapy.
Patients should be treated for between 7 to 9 weeks. If at seven weeks no effect is seen, treatment should be discontinued. Although discontinuation reactions are not expected, a tapering-off period may be considered.
The initial dose is 150 mg daily for 6 days, increasing on day 7 to 150 mg twice daily. There should be an interval of at least 8 hours between successive doses. The maximum single dose should not exceed 150 mg and the total daily dose should not exceed 300 mg.
The recommended daily dose is 150 mg as greater sensitivity may be experienced.
Patients with Renal Impairment
Recommended reduced daily dose of 150 mg.
Patients with Hepatic Impairment
Recommended reduced daily dose of 150mg.
Children under 18 years
Within 2 weeks of discontinuing MAOIs
Within 5 weeks of discontinuing fluoxetine or 2 weeks of other SSRIs
Alcohol withdrawal syndrome
Central nervous system neoplasm
History of anorexia nervosa
History of bipolar disorder
History of bulimia nervosa
History of seizures
Precautions and Warnings
History of head trauma
History of psychiatric disorder
Reduced seizure threshold
Reduce dose in patients with hepatic impairment
Reduce dose in patients with renal impairment
Advise patient dizziness may affect ability to drive or operate machinery
Monitor blood pressure pre-treatment and periodically thereafter
Assess patient for predisposing risk factors which lower seizure threshold
Concurrent nicotine replacement therapy: Monitor blood pressure weekly
Discontinue treatment if patient develops seizures
Monitor patient for signs and symptoms of depression
Monitor patients for signs and symptoms of Serotonin Syndrome
Monitor patients with hepatic impairment for toxic effects
Monitor patients with renal impairment for toxic effects
When used with SSRIs, risk of Serotonin syndrome
Advise patients/carers to seek medical advice if suicidal intent develops
Consider discontinuation if psychotic or manic symptoms occur
Consider dose reduction or discontinuation if serotonin syndrome suspected
May affect urine test results
Progressive withdrawal recommended
Consider discontinuing treatment in cases of marked hypertension
Discontinue if hypersensitivity reactions occur
Discontinue treatment if no effect is seen within 7 weeks
Reduce dose in elderly
Advise patient not to take St John's wort concurrently
Advise patient to avoid bedtime doses so as to reduce the risk of insomnia
Patients should not exceed recommended dose
The recommended dose of bupropion must not be exceeded, since it is associated with a dose-related risk of seizures.
There is an increased risk of seizures occurring during treatment in the presence of predisposing risk factors which lower the seizure threshold. Bupropion should not be used in patients with predisposing risk factors unless there is a compelling clinical justification for which the potential medical benefit of smoking cessation outweighs the potential increased risk of seizure. In these patients, a maximum dose of 150 mg daily should be considered for the duration of treatment.
Bupropion is indicated for the treatment of depression in some countries. Studies have shown an increased risk of suicidal thinking and behaviour associated with antidepressant use in patients less than 25 years old.
Discontinue if hypersensitivity or anaphylactic reactions occur (skin rash, pruritus, urticaria, chest pain, oedema or dyspnoea) during treatment. More severe reactions have also been reported: arthralgia, myalgia and fever - in association with rash and other symptoms suggestive of delayed hypersensitivity. These symptoms may resemble serum sickness. In most patients symptoms improve after stopping treatment with bupropion and initiating treatment with antihistamine or corticosteroids, and resolved over time. Symptoms may worsen or return even after discontinuation of bupropion and supportive treatment should continue for a minimum of one week.
Pregnancy and Lactation
Bupropion is contraindicated in pregnancy.
The safety of bupropion for use in human pregnancy has not been established.
In a retrospective study, there was no greater proportion of congenital malformations or to cardiovascular malformation amongst more than a thousand first trimester exposures to bupropion compared with the use of other antidepressants. Also evaluation of experimental animal studies does not indicate direct or indirect harmful effects with respect to the development of the embryo or foetus, the course of gestation and peri- or post-natal development. The potential risk to humans is unknown.
Pregnant women should be advised to quit smoking without the use of pharmacotherapy.
The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Use bupropion with caution in breastfeeding.
Bupropion and its metabolites are excreted in human breast milk. LactMed states limited information indicates that maternal bupropion doses of up to 300 mg daily produce low levels in breastmilk and would not be expected to cause any adverse effects in breastfed infants. If bupropion is required by a nursing mother, it is not a reason to discontinue breastfeeding. However, another drug may be preferred, especially while nursing a newborn or preterm infant. Exclusively breastfed infants should be monitored if this drug is used during lactation, possibly including measurement of serum levels to rule out toxicity if there is a concern.
Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
May cause dizziness or light-headedness. May affect ability to perform tasks that require judgement or motor and cognitive skills. Therefore patients should be advised to exercise caution before driving or using machinery until they are reasonably certain bupropion does not adversely affect their performance.
Advise patients that insomnia can be reduced by avoiding bedtime doses of bupropion (still leaving an interval of 8 hours between doses).
Advise patients not to crush or chew tablets as this may lead to an increased risk of seizures.
Blood glucose disturbances
Exacerbation of psoriasis
Increased blood pressure
Increases in hepatic enzymes
Serum sickness-like reactions
Effects on Laboratory Tests
Bupropion interferes with the assay used in some rapid urine drug screens, which can result in false positive readings, particularly for amphetamines. A positive result should usually be confirmed with a more specific method.
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: May 2015
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.
Medications and Mothers' Milk, Sixteenth Edition (2014) Hale, T and Rowe, H, Hale Publishing, Plano, Texas.
Summary of Product Characteristics: Zyban. GlaxoSmith Wellcome UK Ltd. Revised October 2020
MHRA Drug Safety Update November 2020
Available at: https://www.mhra.gov.uk
Last accessed: 10 March 2021
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 10 March 2021
US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Bupropion Last revised: 10 March 2015
Last accessed: 15 May 2015
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