Peringatan Keamanan

Older patients metabolize delorazepam slower than younger patients and thus suffer from more adverse effects.

Delorazepam

DB01511

small molecule experimental illicit

Deskripsi

Delorazepam is a benzodiazepine which, like other drugs in its class, possesses anxiolytic, skeletal muscle relaxant, hypnotic and anticonvulsant properties. It may have adverse effects such as drowsiness, and cognitive impairments such as short term memory impairment.

Delorazepam is an active metabolite of the benzodiazepine known as cloxazolam. It is a long acting benzodiazepine which makes it superior in this sense to lorazepam which is short acting. Lorazepam is also a major active metabolite of delorazepam.

In addition to be long acting, delorazepam is relatively potent, with 1 mg of delorazepam being the equivalent of 10 mg diazepam. It has been approved for marketing in Italy.

Struktur Molekul 2D

Berat 305.159
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Very long elimination half life of 80-115 hours, varying with age. Elimination is slower as age increases. [1] Liver disease also impacts elimination half life, with impairment resulting in half lives up to 395 hours.
Volume Distribusi 140 L/kg apparent volume of distribution in 11 patients with normal renal function; 47 L/kg in 11 patients with renal failure and on regular hemodialysis. In another study, apparent volume of distribution was 65 L/kg in 8 patients with liver disease and 118.4 L/kg in 12 healthy controls.
Klirens (Clearance) Still detectable 72 hours after dosing in healthy patients. Patients with liver disease experienced a reduction in clearance from 0.13 to 0.25 ng/mLh.

Absorpsi

77-87% oral bioavailability, with a relatively slow absorption rate. Reaches peak plasma levels within 1-2 hours of administration. Food may slow absorption, however other pharmacokinetic variables remain unchanged. After multiple doses delorazepam accumulates, although accumulation is slower in younger patients.

Metabolisme

Delorazepam is metabolized at a relatively slow pace by the liver. The major metabolite (15-34% of the parent drug) is lorazepam. Older patients metabolize delorazepam slower than younger patients.

Rute Eliminasi

Renally eliminated.

Interaksi Obat

821 Data
Buprenorphine Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Hydrocodone Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Magnesium sulfate The therapeutic efficacy of Delorazepam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Delorazepam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Mirtazapine Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Orphenadrine Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Pramipexole Delorazepam may increase the sedative activities of Pramipexole.
Ropinirole Delorazepam may increase the sedative activities of Ropinirole.
Rotigotine Delorazepam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Delorazepam.
Suvorexant Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Thalidomide Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Clozapine The risk or severity of adverse effects can be increased when Delorazepam is combined with Clozapine.
Methadone Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Olanzapine The risk or severity of adverse effects can be increased when Delorazepam is combined with Olanzapine.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Delorazepam.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Delorazepam.
Sodium oxybate Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Delorazepam can be increased when it is combined with Teduglutide.
Mefloquine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Delorazepam can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Delorazepam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Delorazepam may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Delorazepam.
Ethanol Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Delorazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Delorazepam.
Fluvoxamine The risk or severity of adverse effects can be increased when Delorazepam is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Delorazepam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Delorazepam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Delorazepam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Delorazepam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Delorazepam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Delorazepam is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Delorazepam is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Delorazepam is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Delorazepam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Delorazepam is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Delorazepam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Delorazepam is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Delorazepam is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Delorazepam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Delorazepam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Delorazepam is combined with Alaproclate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Delorazepam.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Delorazepam.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Delorazepam.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Delorazepam.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Delorazepam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Delorazepam.
Cocaine The risk or severity of methemoglobinemia can be increased when Delorazepam is combined with Cocaine.
Quinidine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Quinidine.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Delorazepam.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Delorazepam.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Delorazepam.
Pizotifen The risk or severity of CNS depression can be increased when Delorazepam is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Delorazepam is combined with Dosulepin.
Zopiclone The risk or severity of adverse effects can be increased when Delorazepam is combined with Zopiclone.
Caffeine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Caffeine.
Theophylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Theophylline.
Dyphylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Dyphylline.
Pentoxifylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Pentoxifylline.
Mercaptopurine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Mercaptopurine.
Aminophylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Aminophylline.
Oxtriphylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Oxtriphylline.
Theobromine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Theobromine.
Fenethylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Fenethylline.
8-azaguanine The therapeutic efficacy of Delorazepam can be decreased when used in combination with 8-azaguanine.
7,9-Dimethylguanine The therapeutic efficacy of Delorazepam can be decreased when used in combination with 7,9-Dimethylguanine.
Xanthine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Xanthine.
7-Deazaguanine The therapeutic efficacy of Delorazepam can be decreased when used in combination with 7-Deazaguanine.
Guanine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Guanine.
9-Methylguanine The therapeutic efficacy of Delorazepam can be decreased when used in combination with 9-Methylguanine.
Peldesine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Peldesine.
Hypoxanthine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Hypoxanthine.
9-Deazaguanine The therapeutic efficacy of Delorazepam can be decreased when used in combination with 9-Deazaguanine.
Propentofylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Propentofylline.
Valomaciclovir The therapeutic efficacy of Delorazepam can be decreased when used in combination with Valomaciclovir.
3-isobutyl-1-methyl-7H-xanthine The therapeutic efficacy of Delorazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
Uric acid The therapeutic efficacy of Delorazepam can be decreased when used in combination with Uric acid.
Doxofylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Doxofylline.
6-O-benzylguanine The therapeutic efficacy of Delorazepam can be decreased when used in combination with 6-O-benzylguanine.
Lisofylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Lisofylline.
Lobucavir The therapeutic efficacy of Delorazepam can be decreased when used in combination with Lobucavir.
Cafedrine The therapeutic efficacy of Delorazepam can be decreased when used in combination with Cafedrine.
Theodrenaline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Theodrenaline.
Bamifylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Bamifylline.
Proxyphylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Proxyphylline.
Acefylline The therapeutic efficacy of Delorazepam can be decreased when used in combination with Acefylline.

Target Protein

GABA(A) Receptor GABRA1
GABA(A) Receptor Benzodiazepine Binding Site GABRA1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2875955
    Bareggi SR, Nielsen NP, Leva S, Pirola R, Zecca L, Lorini M: Age-related multiple-dose pharmacokinetics and anxiolytic effects of delorazepam (chlordesmethyldiazepam). Int J Clin Pharmacol Res. 1986;6(4):309-14.
  • PMID: 7589052
    Bareggi SR, Pirola R, Potvin P, Devis G: Effects of liver disease on the pharmacokinetics of intravenous and oral chlordesmethyldiazepam. Eur J Clin Pharmacol. 1995;48(3-4):265-8.
  • PMID: 6130594
    Cazzato G, Gioseffi M, Torre P, Coppola N: Prevention and therapy of delirium tremens with tiapride and chlordesmethyldiazepam. Riv Neurol. 1982 Nov-Dec;52(6):331-42.
  • PMID: 6796270
    Scarone S, Strambi LF, Cazzullo CL: Effects of two dosages of chlordesmethyldiazepam on mnestic-information processes in normal subjects. Clin Ther. 1981;4(3):184-91.
  • PMID: 1782980
    Sennesael J, Verbeelen D, Vanhaelst L, Pirola R, Bareggi SR: Pharmacokinetics of intravenous and oral chlordesmethyldiazepam in patients on regular haemodialysis. Eur J Clin Pharmacol. 1991;41(1):65-8.

Contoh Produk & Brand

Produk: 0 • International brands: 15
International Brands
  • Delorazepam Almus — Almus
  • Delorazepam Alter — Alter
  • Delorazepam Aurobindo — Aurobindo
  • Delorazepam DOC — DOC Generici
  • Delorazepam EG — EG
  • Delorazepam Germed — Germed Pharma
  • Delorazepam Hexal — Hexal
  • Delorazepam Mylan — Mylan
  • Delorazepam Pensa — Pensa Pharma
  • Delorazepam Ranbaxy — Ranbaxy Italia

Sekuens Gen/Protein (FASTA)

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