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Halcion and Nefazodone Hydrochloride

Determining the interaction of Halcion and Nefazodone Hydrochloride and the possibility of their joint administration.

Check result:
Halcion <> Nefazodone Hydrochloride
Relevance: 09.11.2022 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Ask your doctor before using triazolam together with nefazodone. This combination should generally be avoided as nefazodone can significantly increase levels of triazolam. This may result in side effects such as dizziness or drowsiness. If you experience dizziness or drowsiness, avoid driving, operating machinery, or performing other hazardous activities. You may need a dose adjustment if you take both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Professional:

CONTRAINDICATED: Coadministration with nefazodone may significantly increase the plasma concentrations of triazolam. The mechanism is nefazodone inhibition of CYP450 3A4, the isoenzyme responsible for the metabolic clearance of triazolam. In healthy male volunteers, administration of triazolam (0.25 mg) with nefazodone (200 mg orally twice a day for 7 days) resulted in a 1.7-fold increase in mean triazolam peak plasma concentration (Cmax), a 3-fold increase in half-life, and a nearly 4-fold increase in systemic exposure (AUC) compared to administration without nefazodone. These changes were associated with increased sedation and impaired psychomotor performance. Triazolam did not affect the pharmacokinetics of nefazodone.

MANAGEMENT: A 75% reduction in the initial dosage of triazolam has been recommended when prescribed with nefazodone. However, because such a small dose is not generally achievable with commercially available formulations of triazolam, coadministration with nefazodone is considered contraindicated. Lorazepam, oxazepam, and temazepam are not metabolized by CYP450 3A4 and may be suitable alternatives in patients requiring nefazodone and a benzodiazepine.

References
  • Barbhaiya RH, Shukla UA, Kroboth PD, Greene DS "Coadministration of nefazodone and benzodiazepines: 2. a pharmacokinetic interaction study with triazolam." J Clin Psychopharmacol 15 (1995): 320-6
  • Kroboth PD, Mcauley JW, Derry CL "Time-dependent sensitization to triazolam? An observation in three studies." J Clin Psychopharmacol 15 (1995): 192-6
  • Riesenman C "Antidepressant drug interactions and the cytochrome p450 system: a critical appraisal." Pharmacotherapy 15 (1995): s84-99
  • Kroboth PD, Folan MM, Lush RM, Chaikin PC, Shukla UA, Barbhaiya R, Salazar DE "Coadministration of nefazodone and benzodiazepines: 1. pharmacodynamic assessment." J Clin Psychopharmacol 15 (1995): 306-19
  • "Product Information. Halcion (triazolam)." Pharmacia and Upjohn, Kalamazoo, MI.
  • Dresser GK, Spence JD, Bailey DG "Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition." Clin Pharmacokinet 38 (2000): 41-57
  • "Product Information. Serzone (nefazodone)." Bristol-Myers Squibb, Princeton, NJ.
Halcion

Generic Name: triazolam

Brand name: Halcion

Synonyms: n.a.

Nefazodone Hydrochloride

Generic Name: nefazodone

Brand name: Serzone

Synonyms: Nefazodone

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

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