TripSit · Bupropion

正文中文为机器翻译，仅供参考；专业内容以折叠的原文为准。

详情

别名

wellbutrin zyban amfebutamone

分类

兴奋剂

后遗时间

1-6 小时

剂量

口服

常规

150-300mg/day

重剂量

450mg+/day

轻度

150mg/day

强效

300-450mg/day

起效时间

15-90 分钟

名称

bupropion

通用名

Bupropion

属性

adverse-effects

Agitation, dry mouth, insomnia, headache/migraine, nausea/vomiting, constipation, tremor, dizziness, excessive sweating, blurred vision, tachycardia, confusion, rash, hostility, cardiac arrhythmia, and auditory disturbance

后遗效应

1–6 小时.

别名

wellbutrin zyban amfebutamone

分类

兴奋剂

chemistry

IUPAC: (±)-2-(tert-Butylamino)-1-(3-chlorophenyl)propan-1-one | Formula: C13H18ClNO | Molecular Mass: 239.74 g/mol

contraindications

Seizure disorder, current or prior diagnosis of bulimia or anorexia nervosa, abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and anti-epileptic drugs, and MAOIs

持续

Parent: 11–21 小时 | Metabolites: 20–37 小时

效应

Mild - moderate increase in motor activity and agitation/excitement

legal

Australia: Prescription Only (S4) | Canada: ℞-only | United Kingdom: POM | United States: ℞-only

起效

15–90 分钟.

overdose-symptoms

Seizure, hallucinations, loss of consciousness, sinus tachycardia, ECG changes, bradycardia, cardiac failure, cardiac arrest, and death

pharmacokinetics

Protein Binding: 84% (bupropion), 77% [hydroxybupropion (active metabolite)], 42% [threohydrobupropion (active metabolite)] | Metabolism: hepatic, primarily CYP2B6-mediated hydroxylation; both bupropion and hydroxybupropion (active metabolite) are CYP2D6 inhibitors | Excretion: renal (87%; 0.5% unchanged) and faecal (10%)

pharmacology

NDRI (Norepinephrine-Dopamine Reuptake Inhibitor); NDRA (Norepinephrine-Dopamine Releasing Agent); α3β2, α3β4, α4β2, and α7 nACh receptor antagonist

摘要

A frequently prescribed atypical antidepressant. Occasionally prescribed as an aid to smoking cessation. May lower seizure threshold in predisposed individuals. Poorly understood mechanism of action, probably an NDRI. Avoid combination with other drugs.

warning

Bupropion lowers the seizure threshold in a dose-dependent manner. Seizure risk increases significantly at total daily doses above 450 mg, with immediate-release formulations, rapid dose escalation, or when tablets are crushed or altered. Risk is further increased when combined with other substances that lower the seizure threshold, including CNS stimulants, alcohol (especially during withdrawal or binge use), theophylline, systemic corticosteroids, and certain antidepressants.

来源

general

Evaluation of a Potential Metabolism-Mediated Drug-Drug Interaction Between Atomoxetine and Bupropion in Healthy Volunteers. http://www.ncbi.nlm.nih.gov/pubmed/27518170 dosing information for Bupropion https://www.mayoclinic.org/drugs-supplements/bupropion-oral-route/description/drg-20062478