Aspek Farmakokinetik

Absorbsi :

Bioavaibilitas : 90 %.

Durasi: Variabel, tergantung pada dosis dan frekuensi (PO [aksi hipnosis]); 15-60 mnt (IV [tindakan
sedatif]).

Waktu plasma puncak: 30-90 mnt (PO), 5-90 mnt (PR).

Konsentrasi plasma puncak: 373 ng / mL (awal pada 45 menit); 447 ng / mL (puncak kedua pada 70
menit).

Distribusi

Protein terikat: 98%.

Vd: 0,8-1L/Kg.

Metabolisme

Dimetabolisme oleh enzim P450 hati CYP2C19, CYP3A4.

Metabolit: N-desmethyldiazepam, 3-hydroxdiazepam, oxazepam.

Eliminasi

Waktu paruh: 20-70 jam (metabolit aktif).

Pembersihan ginjal: 20-30 mL / mnt.

Ekskresi: Urin.

Penyimpanan :

Wadah tertutup hindari cahaya.

Interaksi Obat :

Diazepam + Cimetidine : meningkatkan konsentrasi diazepam dalam plasma karena metabolisme

diazepam oleh enzim hati /usus CYP3A4 diinhibisi oleh cimetidine.

Tatalaksana : menurunkan dosis diazepam.

Diazepam + Dexametason : menurunkan konstentrasi diazepam dalam plasma karena metabolisme

diazepam oleh enzim hati/usus CYP3A4 diinduksi oleh dexametason sehigga mempercepat
metabolisme diazepam.

Sumber (AHFS 2011, Medscape, Drugs.com)

Interaksi

Depresan SSP

Potensi interaksi farmakologis (depresi aditif SSP) dengan alkohol dan depresan SSP lainnya (mis.,
Hipnotik, obat penenang, obat penenang).

Gangguan Uji Laboratorium

Antihistamin dapat menekan uji inhalasi-tantangan dengan histamin atau antigen serta reaksi whare
dan flare terhadap pengujian kulit antigen.

Obat Khusus

Interaksi Obat

Inhibitor MAO Inhibitor MAO memperpanjang dan mengintensifkan efek antikolinergik dari
antihistamin

diphenhydrAMINE ↔ Alcohol (Ethanol)

Moderate Drug Interaction

GENERALLY AVOID: Use of anticholinergic agents with alcohol may result in sufficient
impairment of attention so as to render driving and operating machinery more hazardous. In addition,
the potential for abuse may be increased with the combination. The mechanism of interaction is not
established but may involve additive depressant effects on the central nervous system. No effect of
oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when
administered before ingestion of a standard ethanol load. However, one study found impairment of
attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.
MANAGEMENT: Alcohol should generally be avoided during therapy with anticholinergic agents.
Patients should be counseled to avoid activities requiring mental alertness until they know how these
agents affect them.