Varenicline overdose in a teenager

Hedlund, Amy Joy; Broderick, Molly; Shah, Nilofar; Cantrell, Lee

doi:10.1080/15563650701787987

Cited by 4 publications

(3 citation statements)

References 3 publications

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“…9 A case report describes a teenager who ingested thirty 0.5-mg tablets of varenicline tartrate. 10 Apart from vomiting, she experienced no other symptoms, and her physical examination after ingestion was unremarkable. Therefore, there are no a priori reasons to expect any safety issues if the varenicline dose is increased in patients not experiencing any drug adverse effects.…”

mentioning

confidence: 95%

Increasing Varenicline Dose in Smokers Who Do Not Respond to the Standard Dosage

et al. 2015

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mentioning

confidence: 95%

Increasing Varenicline Dose in Smokers Who Do Not Respond to the Standard Dosage

et al. 2015

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“…In fact, with high doses of varenicline (> 3 mg/day) the rapid onset of emesis limits the systemic exposure of varenicline [32]. Overdosing is therefore not expected to result in excessive systemic exposures that could potentially cause nicotinic toxic effects, as illustrated by a recently reported overdose case [51,52].…”

Section: Safety and Tolerability Of Vareniclinementioning

confidence: 99%

Pharmacodynamic and pharmacokinetic profiles of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, a smoking cessation aid

Faessel

Rollema

2016

J Pediatr Biochem

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This review describes the role of ?4?2 containing nicotinic acetylcholine receptors in the mesolimbic reward pathway in the neurobiology of nicotine addiction and discusses the rationale for targeting this receptor with partial agonists as novel smoking cessation agents. Varenicline is a ?4?2 nicotinic acetylcholine receptor partial agonist that is a smoking cessation aid with a dual mechanism of action: relief of craving and withdrawal symptoms, as well as attenuation of nicotine reinforcement. The pharmacological profile of varenicline is consistent with that of a potent and selective partial agonist at the target receptor, both in in vitro and in vivo neurochemical and behavioral models. Varenicline was nominated for full clinical development in 1997, and later approved in the US and Europe as a smoking cessation aid in 2006. The recommended dose of varenicline is 1 mg BID for 12 weeks after an initial titration week in adult smokers motivated to stop smoking. The pharmacokinetics of varenicline is linear and consistent regardless of smoking status, age, gender or ethnic background. Varenicline is largely eliminated unchanged in the urine, and consequently a dose adjustment is warranted for patients with severe renal insufficiency. Although varenicline is currently not approved for use in smokers under age 18, its pharmacokinetic and tolerability profile in adolescents appeared generally similar to adults. Several large clinical trials have consistently shown the efficacy, tolerability and safety of varenicline in various ethnic smoking populations and in adult smokers with co-morbid chronic pulmonary or cardiovascular disease. Additional clinical studies in special patient populations are currently ongoing.

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“…1 Data from phase 1 clinical trials showed rapid vomiting responses after high doses of varenicline. 2,3 Maximum plasma concentrations after a single 10-mg dose, at which all subjects vomited, were found to range from 4.1 to 18 ng/mL, similar to those observed after a single 3-mg dose.…”

Section: To the Editormentioning

confidence: 99%