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Heterocyclic Drug Design and Development
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Garima Verma, Mohammad Shaquiquzzaman, Mohammad Mumtaz Alam
Smoking deterrents are the agents which prevent an individual from smoking. Bupropion is most commonly used for smoking cessation (Medicinenet. com. Bupropion sustained-release). Smoking deterrents obtained from plants are mentioned in Table 9.20.
Pharmacological Approaches for Tobacco Cessation
Published in Rajmohan Panda, Manu Raj Mathur, Tobacco Cessation, 2019
Binod Kumar Patro, Suravi Patra
Bupropion hydrochloride sustained-release tablet is licensed as a non-nicotine tobacco cessation drug. Bupropion blocks dopamine–norepinephrine reuptake in the mesolimbic system and nucleus accumbens and also has a nicotine receptor blocking activity.9 Its antismoking effect is independent of its antidepressant effect, and acts primarily to decrease nicotine withdrawal symptoms and craving.10 Bupropion is as effective as NRT but less effective than varenicline. Bupropion should be started at least 1 week before the patient's quit date. For the first 3 days, one tablet daily should be taken, on the 4th day, one tablet twice daily should be taken to be continued for at least 7 weeks. In case of no improvement in abstinence, it should be withdrawn. For more information, refer to Table 5.2.
Information on level of drugs into breastmilk
Published in Wendy Jones, Breastfeeding and Medication, 2018
Bupropion was originally developed as an anti-depressant but is rarely used as such in the UK currently. It is, however, used to support smoking cessation attempts. Its use is contra-indicated in patients with a history of seizure and use by mothers whose baby has suffered any form of seizure is best avoided. Bupropion undergoes extensive first-pass metabolism and it has several active metabolites with long half-lives. It is 80% plasma protein bound. It is given as a modified-release preparation in smoking cessation at an initial dose of 150 mg once daily for six days, increasing to 150 mg twice daily on day seven. Treatment is started about one to two weeks before an agreed quit date, to allow steady-state blood levels of bupropion to be reached, and therapy normally continues up to 12 weeks. There is a case report of a 6-month-old baby who suffered seizures three days after the mother initiated 150 mg per day dose of bupropion (Chaudron and Schoenecker 2004). The mother discontinued the drug and no further adverse events were noted.
When is pharmacotherapy necessary for the treatment of seasonal affective disorder?
Published in Expert Opinion on Pharmacotherapy, 2022
Jean-Baptiste Belge, Amber CF Sabbe, Bernard GCC Sabbe
Given the well-known morbidity of a depressive episode and the predictability of these episodes inherent to the SAD diagnosis, preventive treatment may be necessary, especially for those individuals who are known to experience severe depressive episodes. Until today, bupropion extended release (XR) is the only antidepressant with a proven prophylactic efficacy for SAD and is as such approved by the US FDA. Three double-blind randomized controlled trials demonstrated bupropion’s superior prophylactic efficacy to placebo [12,13]. Recurrence of depressive episodes was significantly lower in the bupropion group when started in autumn, before the onset of symptoms and continued until spring [12,13]. However, side-effects of bupropion include headaches, insomnia and nausea and affect around 20–30% of patients [12,13]. While an efficacious intervention for the prevention of recurrence of depressive episodes, the Cochrane working group stated that the numbers needed to treat for additional beneficial outcomes (NNTB) will vary strongly by baseline risks [14]. For a population with a yearly recurrence rate of 30%, the NNTB is 8, while for populations with yearly recurrence rates of 50% and 60%, NNTBs are 5 and 4 [14].
Treatment Outcomes of a Multi-Component Mobile Health Smoking Cessation Pilot Intervention for People with Schizophrenia
Published in Journal of Dual Diagnosis, 2020
Alyssa M. Medenblik, Adam M. Mann, Tiffany A. Beaver, Eric A. Dedert, Sarah M. Wilson, Patrick S. Calhoun, Jean C. Beckham
Pharmacotherapy was offered to all study participants, but not required for study participation. The pharmacotherapy was chosen prior to meta-analyses indicating varenicline was efficacious for smokers with schizophrenia (Tsoi et al., 2013). The study physician provided all pharmacotherapy and screening for pharmacotherapy. All study participants (who assented and for whom it was not contraindicated) were prescribed bupropion, which they started 2 weeks prior to their quit day (150 mg/daily for days 1–7 and 300 mg/daily [administered in two daily doses]). Because bupropion has been shown to improve long-term quit rates in smokers with schizophrenia, 11 participants were asked to continue bupropion for 6 months following the quit date and were provided with enough of the medication to do so. Participants who started bupropion but did not quit during the intervention were not prescribed bupropion through the 6-month follow up. Contraindications for bupropion were assessed by the study physician. Varenicline was offered as an alternative if participants did not quit on their initial quit date due to its efficacy for smokers with schizophrenia (Tsoi et al., 2013). For participants who switched to varenicline, there was a washout period for bupropion and then varenicline was prescribed (0.5 mg once per day for 3 days, 0.5 mg twice per day for 4 days, then 1 mg twice per day up until 6-month follow-up).
Systematic review of preclinical, clinical, and post-marketing evidence of bupropion misuse potential
Published in The American Journal of Drug and Alcohol Abuse, 2019
Andrew C Naglich, E. Sherwood Brown, Bryon Adinoff
Orally dosed bupropion has known side effects including lowered seizure threshold, agitation, gastrointestinal disturbance, and issues with sleep (11). User experiences describing the effects of ingestion of doses between one and six times the maximum recommended daily dose of bupropion detail a variety of adverse reactions including jitteriness and anxiety (3/14), nausea and vomiting (5/14), formication (1/14), and auditory or visual hallucinations (12/14). Erowid users who have orally taken supratherapeutic doses of bupropion frequently report no positive effects (9/14), feelings of euphoria (5/14), or enhanced perception of light and sound (2/14). The number of cases of bupropion use as the sole intoxicant is markedly smaller by the number of reports with caffeine (54) and prescription d-amphetamine (98).