Peringatan Keamanan

The LD50 observed by oral administration in a mouse is of 1850 mg/kg.L6403 When an overdose administration is registered, signs of CNS and respiratory depression are rapidly observed. An overdose stage can result in profound sedation, deep respiratory depression, coma, and death.T385 When overdose is observed, it is recommended to administer emergency symptomatic medical support with attention to produce an increase in lorazepam elimination.T388

There is no evidence of carcinogenicity nor mutagenicity. At doses higher than 40 mg/kg there is evidence of fetal resorption and increase in fetal loss.FDA label

Lorazepam

DB00186

small molecule approved

Deskripsi

Lorazepam is a short-acting and rapidly cleared benzodiazepine used commonly as a sedative and anxiolytic.A957 It was developed by DJ Richards, presented and marketed initially by Wyeth Pharmaceuticals in the USA in 1977. The first historic FDA label approval is reported in 1985 by the company Mutual Pharm.L5095

Struktur Molekul 2D

Berat 321.158
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) When administered parentally, the registered half-life of lorazepam is of 14 hours.[T385] Following the administration of 1 mg of lorazepam in healthy adult male volunteers and using a multi-doses equation based on a one-compartment model, the average elimination half-life of lorazepam was estimated to be 11 hours and 8 hours for sublingual and oral doses respectively.[A251115] The absorption half-life was calculated to be 55 minutes for oral doses and 15 minutes for sublingual doses.[A251115]
Volume Distribusi The reported volume of distribution of lorazepam is 1.3 L/kg.[T388] It is important to mention that due to the lipophilicity of lorazepam, it does not redistribute as fast in the brain.[T391]
Klirens (Clearance) _In vivo_ studies with lorazepam have shown a clearance rate of 5.8 ml.min/kg.[A173914]

Absorpsi

Readily absorbed with an absolute bioavailability of 90% when given orally. When intramuscularly administered a dose of 4 mg, lorazepam is completely and rapidly absorbed and achieves a maximal serum concentration of 48 ng/ml in 15-30 minutes. When administered orally, the time to attained maximum concentration is observed to be of 2 hours.T385

Metabolisme

Lorazepam is hepatically metabolized by CYP450 isoenzymes and extensively conjugated to the 3-0-phenolic glucuronide.T385 This is an inactive metabolite and is eliminated mainly by the kidneys.

Rute Eliminasi

When a single 2 mg oral dose is given to healthy subjects, 88% of the administered dose is recovered in urine and 7% was recovered in feces. From the excreted dose in urine, the major form is the glucuronide version that represents 74% while only 0.3% of the dose is recovered as unchanged lorazepam.T388

Interaksi Makanan

3 Data
  • 1. Avoid alcohol.
  • 2. Limit caffeine intake.
  • 3. Take with food.

Interaksi Obat

1412 Data
Buprenorphine Lorazepam 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 Lorazepam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.
Hydrocodone Lorazepam 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 Lorazepam.
Magnesium sulfate The therapeutic efficacy of Lorazepam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Lorazepam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.
Mirtazapine Lorazepam 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 Lorazepam.
Orphenadrine Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Lorazepam 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 Lorazepam.
Pramipexole Lorazepam may increase the sedative activities of Pramipexole.
Ropinirole Lorazepam may increase the sedative activities of Ropinirole.
Rotigotine Lorazepam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Lorazepam.
Suvorexant Lorazepam 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 Lorazepam.
Thalidomide Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Clozapine The risk or severity of adverse effects can be increased when Lorazepam is combined with Clozapine.
Loxapine The risk or severity of adverse effects can be increased when Loxapine is combined with Lorazepam.
Methadone Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Olanzapine The risk or severity of adverse effects can be increased when Lorazepam is combined with Olanzapine.
Probenecid The serum concentration of Lorazepam can be increased when it is combined with Probenecid.
Sodium oxybate Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Lorazepam can be increased when it is combined with Teduglutide.
Yohimbine The therapeutic efficacy of Lorazepam can be increased when used in combination with Yohimbine.
Mefloquine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Lorazepam can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Lorazepam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Lorazepam may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Valproic acid The serum concentration of Lorazepam can be increased when it is combined with Valproic acid.
Flumazenil Flumazenil may decrease the sedative activities of Lorazepam.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Lorazepam.
Ethanol Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Lorazepam 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 Lorazepam.
Zimelidine The risk or severity of adverse effects can be increased when Lorazepam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Lorazepam is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Lorazepam is combined with Seproxetine.
Fluvoxamine The risk or severity of adverse effects can be increased when Lorazepam is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Lorazepam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Lorazepam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Lorazepam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Lorazepam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Lorazepam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Lorazepam is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Lorazepam is combined with Escitalopram.
Milnacipran The risk or severity of adverse effects can be increased when Lorazepam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Lorazepam is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Lorazepam is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Lorazepam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Lorazepam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Lorazepam is combined with Alaproclate.
Benzatropine Lorazepam may decrease the excretion rate of Benzatropine which could result in a higher serum level.
Disopyramide Lorazepam may decrease the excretion rate of Disopyramide which could result in a higher serum level.
Cyproheptadine The risk or severity of CNS depression can be increased when Lorazepam is combined with Cyproheptadine.
Propiomazine The risk or severity of CNS depression can be increased when Lorazepam is combined with Propiomazine.
Propantheline Lorazepam may decrease the excretion rate of Propantheline which could result in a higher serum level.
Dicyclomine Lorazepam may decrease the excretion rate of Dicyclomine which could result in a higher serum level.
Cocaine The risk or severity of methemoglobinemia can be increased when Lorazepam is combined with Cocaine.
Tolterodine Lorazepam may decrease the excretion rate of Tolterodine which could result in a higher serum level.
Flavoxate Lorazepam may decrease the excretion rate of Flavoxate which could result in a higher serum level.
Tiotropium Lorazepam may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Fesoterodine Lorazepam may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Lorazepam may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Lorazepam may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Lorazepam may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Lorazepam may decrease the excretion rate of Propiverine which could result in a higher serum level.
Amitriptyline The risk or severity of CNS depression can be increased when Lorazepam is combined with Amitriptyline.
Imipramine The risk or severity of CNS depression can be increased when Lorazepam is combined with Imipramine.
Doxepin The risk or severity of CNS depression can be increased when Lorazepam is combined with Doxepin.
Nortriptyline The risk or severity of CNS depression can be increased when Lorazepam is combined with Nortriptyline.
Desipramine The risk or severity of CNS depression can be increased when Lorazepam is combined with Desipramine.
Zopiclone The risk or severity of adverse effects can be increased when Lorazepam is combined with Zopiclone.
Caffeine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Caffeine.
Dyphylline The therapeutic efficacy of Lorazepam can be decreased when used in combination with Dyphylline.
Pentoxifylline The therapeutic efficacy of Lorazepam can be decreased when used in combination with Pentoxifylline.
Mercaptopurine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Mercaptopurine.
Oxtriphylline The therapeutic efficacy of Lorazepam can be decreased when used in combination with Oxtriphylline.
Theobromine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Theobromine.
Fenethylline The therapeutic efficacy of Lorazepam can be decreased when used in combination with Fenethylline.
8-azaguanine The therapeutic efficacy of Lorazepam can be decreased when used in combination with 8-azaguanine.
7,9-Dimethylguanine The therapeutic efficacy of Lorazepam can be decreased when used in combination with 7,9-Dimethylguanine.
Xanthine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Xanthine.
7-Deazaguanine The therapeutic efficacy of Lorazepam can be decreased when used in combination with 7-Deazaguanine.
Guanine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Guanine.
9-Methylguanine The therapeutic efficacy of Lorazepam can be decreased when used in combination with 9-Methylguanine.
Peldesine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Peldesine.
Hypoxanthine The therapeutic efficacy of Lorazepam can be decreased when used in combination with Hypoxanthine.
9-Deazaguanine The therapeutic efficacy of Lorazepam can be decreased when used in combination with 9-Deazaguanine.
Propentofylline The therapeutic efficacy of Lorazepam can be decreased when used in combination with Propentofylline.
Valomaciclovir The therapeutic efficacy of Lorazepam can be decreased when used in combination with Valomaciclovir.
3-isobutyl-1-methyl-7H-xanthine The therapeutic efficacy of Lorazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
Uric acid The therapeutic efficacy of Lorazepam can be decreased when used in combination with Uric acid.
Doxofylline The therapeutic efficacy of Lorazepam can be decreased when used in combination with Doxofylline.

Target Protein

Translocator protein TSPO
GABA(A) Receptor GABRA1
GABA(A) Receptor Benzodiazepine Binding Site GABRA1

Referensi & Sumber

Synthesis reference: Igor Lifshitz, "Process for preparing pure crystalline lorazepam." U.S. Patent US20010039340, issued November 08, 2001.
Artikel (PubMed)
  • PMID: 7439058
    Kemper N, Poser W, Poser S: Benzodiazepine dependence: addiction potential of the benzodiazepines is greater than previously assumed (author's transl). Dtsch Med Wochenschr. 1980 Dec 5;105(49):1707-12.
  • PMID: 6144459
    Lader M: Short-term versus long-term benzodiazepine therapy. Curr Med Res Opin. 1984;8 Suppl 4:120-6.
  • PMID: 8625666
    Maltais F, Laberge F, Laviolette M: A randomized, double-blind, placebo-controlled study of lorazepam as premedication for bronchoscopy. Chest. 1996 May;109(5):1195-8.
  • PMID: 238548
    Heisterkamp DV, Cohen PJ: The effect of intravenous premedication with lorazepam (ativan), pentobarbitone or diazepam on recall. Br J Anaesth. 1975 Jan;47(1):79-81.
  • PMID: 3611398
    Milligan DW, Howard MR, Judd A: Premedication with lorazepam before bone marrow biopsy. J Clin Pathol. 1987 Jun;40(6):696-8.
  • PMID: 7388368
    Authors unspecified: Systematic review of the benzodiazepines. Guidelines for data sheets on diazepam, chlordiazepoxide, medazepam, clorazepate, lorazepam, oxazepam, temazepam, triazolam, nitrazepam, and flurazepam. Committee on the Review of Medicines. Br Med J. 1980 Mar 29;280(6218):910-2.
  • PMID: 17989424
    Li C, Liu T, Cui X, Uss AS, Cheng KC: Development of in vitro pharmacokinetic screens using Caco-2, human hepatocyte, and Caco-2/human hepatocyte hybrid systems for the prediction of oral bioavailability in humans. J Biomol Screen. 2007 Dec;12(8):1084-91. doi: 10.1177/1087057107308892. Epub 2007 Nov 7.
  • PMID: 18384456
    Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31.
Menampilkan 8 dari 11 artikel.
Textbook
  • Ghiasi N. and Marwaha R. (2018). Lorazepam.. Treasure Island, FL.
  • Pagliaro L. and Pagliaro A. (1999). Psychologists' psychotropic drug reference. Taylor and Francis.
  • Volpe J. (2008). Neurology of the Newborn (5th ed.). Saunders Elsevier.

Contoh Produk & Brand

Produk: 526 • International brands: 8
Produk
  • Apo-lorazepam
    Tablet • 0.5 mg • Oral • Canada • Generic • Approved
  • Apo-lorazepam
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Apo-lorazepam
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • Ativan
    Tablet • 1 mg/1 • Oral • US • Approved
  • Ativan
    Tablet • 0.5 mg/1 • Oral • US • Approved
  • Ativan
    Injection, solution • 2 mg/1mL • Intramuscular; Intravenous • US • Approved
  • Ativan
    Tablet • 0.5 mg/1 • Oral • US • Approved
  • Ativan
    Tablet • 1 mg/1 • Oral • US • Approved
Menampilkan 8 dari 526 produk.
International Brands
  • Almazine — Psyco Remedies
  • Anxiedin — U-Liang
  • Idalprem — Novartis
  • Lorabenz
  • Lorsilan — Belupo
  • Somagerol
  • Temesta — Wyeth
  • Wypax — Wyeth KK

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul