Bupropion

Bupropion 화학적 특성, 용도, 생산

• 용도

  enteric coating

• Clinical Use

  Wellbutrin and Zyban (an aid in smoking cessation treatment) are trade name products for bupropion. Therefore, the potential exists for an overdose toxicity in a patient receiving multiple brand name and generic prescriptions containing bupropion for the treatment of depression, smoking cessation, and other off-label uses.
  Besides being used to treat depression, bupropion is a nonnicotine aid in the cessation of smoking. The efficacy of bupropion in smoking cessation is comparable to that of nicotine replacement therapy and should be considered as a second-line treatment in smoking cessation. It possesses a broad spectrum of infrequent adverse effects, however, with potential drug metabolism interactions with TCAs, β-adrenergic blocking drugs, and class Icantiarrhythmics.

• 효소 저해제

  This β-ketoamphetamine-type antidepressant and smoking cessation aid (FW = 239.74 g/mol; CAS 34841-39-9), also known as Wellbutrin?, Zyban?, and (±)-2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-one, is said to be a norepinephrine and dopamine reuptake inhibitor, although its weak effect on dopamine levels calls into question the latter action. Bupropion also acts noncompetitively as a neuronal acetylcholine receptor antagonist. Unlike many antidepressants, however, bupropion shows no serotonergic activity. It also lacks typical antidepressant side effects, e.g., sexual dysfunction, weight gain, and sedation. Pharmacokinetics: Upon oral administration, bupropion is rapidly absorbed with first-order kinetics and subsequently eliminated via biphasic kinetics, with a redistribution t1/2 of ~1 hour and an elimination t1/2 of 11-14 hours. Widely distributed throughout the body, bupropion is extensively metabolized, both oxidatively and reductively, to form as many as six metabolites, of which some are pharmacologically active. While bupropion does not inhibit monoamine oxidase, it exerts no effect on serotonin uptake. It minimally alters the reuptake of norepinephrine at presynaptic sites. Importantly, bupropion does not act on postsynaptic b-adrenergic down-regulation or presynaptic dopamine uptake. Gene variants in CYP2C19 are associated with altered in vivo bupropion pharmacokinetics. Key Pharmacokinetic Parameters: See Appendix II in Goodman & Gilman’s THE PHARMACOLOGICAL BASIS OF THERAPEUTICS, 12th Edition (Brunton, Chabner & Knollmann, eds.) McGraw-Hill Medical, New York.

• Drug interactions

  Inhibition studies with the SSRIs and bupropion suggest that bupropion is a potent CYP2D6 inhibitor. Bupropion hydroxylation was strongly inhibited by, in the following order, paroxetine> fluvoxamine> sertraline> desmethylsertraline> norfluoxetine> nefazodone> fluoxetine and only weakly inhibited by venlafaxine, ODV, citalopram, and desmethylcitalopram. The inhibition of bupropion hydroxylation in vitro by SSRIs suggests the potential for clinical drug interactions. Therefore, coadministration of drugs that inhibit CYP2D6 warrants careful monitoring. Because of its selective inhibition of DA reuptake, pharmacodynamic interactions with dopamine agonists (e.g., levodopa) and antagonists should be anticipated. Coadministration of bupropion with drugs that lower the seizure threshold should be avoided because of the risk of serious seizures.
  Drugs that affect metabolism by CYP2B6 also have the potential to interact with bupropion.

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