Details of the Drug

General Information of Drug (ID: DM84ZXF)

Drug Name

Lorazepam

Synonyms

Almazine; Alzapam; Anxiedin; Anxira; Anzepam; Aplacasse; Aplacassee; ApoLorazepam; Aripax; Ativan; Azurogen; Bonatranquan; Bonton; Delormetazepam; Demethyllormetazepam; Donix; Duralozam; Durazolam; Efasedan; Emotion; Emotival; Equitam; Idalprem; Kalmalin; Larpose; Laubeel; Lomesta; Lopam; Lorabenz; Lorafen; Loram; Lorans; Lorapam; Lorat; Lorax; Loraz; Lorazene; Lorazep; Lorazepamum; Lorazin; Lorazon; Lorenin; Loridem; Lorivan; Lorsedal; Lorsilan; Lorzem; Lozepam; Merlit; Nervistopl; Norlormetazepam; Novhepar; Novolorazem; NuLoraz; Orfidal; Punktyl; Quait; Renaquil; Rocosgen; Securit; Sedatival; Sedazin; Sedicepan; Sedizepan; Sidenar; Silence; Sinestron; Somagerol; Stapam; Tavor; Temesta; Tolid; Tranqipam; Trapax; Upan; Vigiten; Wypax; AHP Brand of Lorazepam; Apo Lorazepam; Apotex Brand of Lorazepam; Baxter Brand of Lorazepam; Ct Arzneimittel Brand of Lorazepam; Desitin Brand of Lorazepam; Dolorgiet Brand of Lorazepam; Llorens Brand of Lorazepam; Lorazep von ct; Lorazepam AHP Brand; Lorazepam Apotex Brand; Lorazepam Baxter Brand; Lorazepam Desitin Brand; Lorazepam Dolorgiet Brand; Lorazepam Fabra; Lorazepam Genericon; Lorazepam Intensol; Lorazepam Lannacher; Lorazepam Llorens Brand; Lorazepam Medical; Lorazepam Medical Brand; Lorazepam Medix Brand; Lorazepam Novartis Brand; Lorazepam Novopharm Brand; Lorazepam Riemser Brand; Lorazepam Wyeth Brand; Lorazepam neuraxpharm; Lorazepam neuraxpharm Brand; Lorazepam preservative free; Lorazepam ratiopharm; Lorazepam ratiopharm Brand; Lorazepan Chobet; Lorazepan Richet; Max Pax; Medical Brand of Lorazepam; Medix Brand of Lorazepam; Merck dura Brand of Lorazepam; Nervistop L; Neuraxpharm Brand of Lorazepam; Novartis Brand of Lorazepam; Novo Lorazem; Novopharm Brand of Lorazepam; Nu Loraz; Nu Pharm Brand of Lorazepam; Orfidal Wyeth; Pro dorm; Ratiopharm Brand of Lorazepam; Riemser Brand of Lorazepam; Serra Pamies Brand of Lorazepam; Wyeth Brand of Lorazepam; L1764_SIGMA; WY4036; Wy 4036; Apo-Lorazepam; Ativan (TN); Ct-Arzneimittel Brand of Lorazepam; Lorazepam (Ativan); Lorazepam Nu-Pharm Brand; Lorazepam ct-Arzneimittel Brand; Lorazepam-Efeka; Lorazepam-neuraxpharm; Lorazepam-ratiopharm; Lorazepamum [INN-Latin]; Medical, Lorazepam; Novo-Lorazem; Nu-Loraz; Nu-Pharm Brand of Lorazepam; O-Chlorooxazepam; O-Chloroxazepam; Temesta (TN); Wy-4036; Wyeth, Orfidal; Lorazepam (JP15/USP/INN); Lorazepam [USAN:INN:BAN:JAN]; (+-)-7-Chloro-5-(o-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one; (+/-)-Lorazepam; 7-Chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one; 7-Chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-2H-1,4-benzodiazepin-2-one; 7-Chloro-5-(2-chlorophenyl)-3-hydroxy-1H-1,4-benzodiazepin-2(3H)-one; 7-Chloro-5-(o-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one; 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one

Indication

Disease Entry	ICD 11	Status	REF
Absence epilepsy	N.A.	Approved	[1]
Anxiety	N.A.	Approved	[1]
Anxiety disorder	6B00-6B0Z	Approved	[2]
Nausea	MD90	Approved	[1]
Panic disorder	6B01	Approved	[1]
Vomiting	MD90	Approved	[1]
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Therapeutic Class

Antianxiety Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

321.2

Logarithm of the Partition Coefficient (xlogp)

2.4

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 2.5 mcg/L [3]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 7 h [3]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [4]
Bioavailability: The bioavailability of drug is 29% [3]
Clearance: The clearance of drug is 5.8 mL/min/kg [5]
Elimination: 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 []
Half-life: The concentration or amount of drug in body reduced by one-half in 14 hours [6]
Metabolism: The drug is metabolized via the hepatic []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.4448 micromolar/kg/day [7]
Unbound Fraction: The unbound fraction of drug in plasma is 0.09% [6]
Vd: The volume of distribution (Vd) of drug is 1.3 L/kg []
Water Solubility: The ability of drug to dissolve in water is measured as 0.08 mg/mL [4]

Chemical Identifiers

Formula: C15H10Cl2N2O2
IUPAC Name: 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one
Canonical SMILES: C1=CC=C(C(=C1)C2=NC(C(=O)NC3=C2C=C(C=C3)Cl)O)Cl
InChI: InChI=1S/C15H10Cl2N2O2/c16-8-5-6-12-10(7-8)13(19-15(21)14(20)18-12)9-3-1-2-4-11(9)17/h1-7,15,21H,(H,18,20)
InChIKey: DIWRORZWFLOCLC-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 3958
ChEBI ID: CHEBI:6539
CAS Number: 846-49-1
DrugBank ID: DB00186
TTD ID: D0E0OG
INTEDE ID: DR0978
ACDINA ID: D00375

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Translocator protein (TSPO)	TTPTXIN	TSPO_HUMAN	Modulator	[8]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 2B7 (UGT2B7)	DEB3CV1	UD2B7_HUMAN	Substrate	[9]
UDP-glucuronosyltransferase 2B15 (UGT2B15)	DENZ6B1	UDB15_HUMAN	Substrate	[10]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Lorazepam (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Sodium bicarbonate	DMMU6BJ	Minor	Altered absorption of Lorazepam due to GI dynamics variation caused by Sodium bicarbonate.	Acidosis [5C73]	[11]
Oliceridine	DM6MDCF	Major	Additive CNS depression effects by the combination of Lorazepam and Oliceridine.	Acute pain [MG31]	[12]
Nitazoxanide	DMOWLVG	Moderate	Increased plasma concentration of Lorazepam and Nitazoxanide due to competitive binding of plasma proteins.	Bowel habit change [ME05]	[13]
Dihydrocodeine	DMB0FWL	Major	Additive CNS depression effects by the combination of Lorazepam and Dihydrocodeine.	Chronic pain [MG30]	[14]
Morphine	DMRMS0L	Major	Additive CNS depression effects by the combination of Lorazepam and Morphine.	Chronic pain [MG30]	[12]
Olopatadine	DMKMWQG	Moderate	Additive CNS depression effects by the combination of Lorazepam and Olopatadine.	Conjunctiva disorder [9A60]	[15]
Propofol	DMB4OLE	Moderate	Additive CNS depression effects by the combination of Lorazepam and Propofol.	Corneal disease [9A76-9A78]	[16]
Alfentanil	DMVO0UB	Major	Additive CNS depression effects by the combination of Lorazepam and Alfentanil.	Corneal disease [9A76-9A78]	[12]
Remifentanil	DMZTXCH	Major	Additive CNS depression effects by the combination of Lorazepam and Remifentanil.	Corneal disease [9A76-9A78]	[12]
Methadone	DMTW6IU	Major	Additive CNS depression effects by the combination of Lorazepam and Methadone.	Cough [MD12]	[12]
Ethanol	DMDRQZU	Moderate	Additive CNS depression effects by the combination of Lorazepam and Ethanol.	Cystitis [GC00]	[17]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Lorazepam and Esketamine.	Depression [6A70-6A7Z]	[18]
SODIUM CITRATE	DMHPD2Y	Minor	Altered absorption of Lorazepam due to GI dynamics variation caused by SODIUM CITRATE.	Discovery agent [N.A.]	[11]
Mephenytoin	DM5UGDK	Moderate	Increased metabolism of Lorazepam caused by Mephenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[19]
Phenytoin	DMNOKBV	Moderate	Increased metabolism of Lorazepam caused by Phenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[19]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Lorazepam caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[19]
Ethotoin	DMXWOCP	Moderate	Increased metabolism of Lorazepam caused by Ethotoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[19]
Brimonidine	DMQLT4N	Moderate	Additive CNS depression effects by the combination of Lorazepam and Brimonidine.	Glaucoma [9C61]	[20]
Digoxin	DMQCTIH	Moderate	Increased plasma concentration of Lorazepam and Digoxin due to competitive binding of plasma proteins.	Heart failure [BD10-BD1Z]	[21]
Bumetanide	DMRV7H0	Moderate	Additive hypotensive effects by the combination of Lorazepam and Bumetanide.	Heart failure [BD10-BD1Z]	[22]
Didanosine	DMI2QPE	Minor	Altered absorption of Lorazepam due to GI dynamics variation caused by Didanosine.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Metoprolol	DMOJ0V6	Minor	Decreased metabolism of Lorazepam caused by Metoprolol.	Hypertension [BA00-BA04]	[23]
Probenecid	DMMFWOJ	Minor	Decreased metabolism of Lorazepam caused by Probenecid.	Inborn purine/pyrimidine/nucleotide metabolism error [5C55]	[24]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Lorazepam caused by PF-06463922 mediated induction of UGT.	Lung cancer [2C25]	[18]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Lorazepam and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[25]
Propranolol	DM79NTF	Minor	Decreased metabolism of Lorazepam caused by Propranolol.	Migraine [8A80]	[23]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Lorazepam and Lasmiditan.	Migraine [8A80]	[26]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Lorazepam and Flibanserin.	Mood disorder [6A60-6E23]	[27]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Lorazepam and Thalidomide.	Multiple myeloma [2A83]	[28]
Droperidol	DM0DXA8	Major	Increased risk of prolong QT interval by the combination of Lorazepam and Droperidol.	Nausea/vomiting [MD90]	[29]
Teduglutide	DMYOAKS	Moderate	Altered absorption of Lorazepam caused by Teduglutide.	Neonatal malabsorption syndrome [KB89]	[30]
Levomethadyl Acetate	DM06HG5	Major	Additive CNS depression effects by the combination of Lorazepam and Levomethadyl Acetate.	Opioid use disorder [6C43]	[14]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Lorazepam and Apraclonidine.	Optic nerve disorder [9C40]	[20]
Pentazocine	DM1XBHS	Major	Additive CNS depression effects by the combination of Lorazepam and Pentazocine.	Pain [MG30-MG3Z]	[12]
Dextropropoxyphene	DM23HCX	Major	Additive CNS depression effects by the combination of Lorazepam and Dextropropoxyphene.	Pain [MG30-MG3Z]	[31]
Butorphanol	DM5KYPJ	Major	Additive CNS depression effects by the combination of Lorazepam and Butorphanol.	Pain [MG30-MG3Z]	[12]
Oxymorphone	DM65AGJ	Major	Additive CNS depression effects by the combination of Lorazepam and Oxymorphone.	Pain [MG30-MG3Z]	[12]
Levorphanol	DMGS80V	Major	Additive CNS depression effects by the combination of Lorazepam and Levorphanol.	Pain [MG30-MG3Z]	[12]
Hydromorphone	DMHP21E	Major	Additive CNS depression effects by the combination of Lorazepam and Hydromorphone.	Pain [MG30-MG3Z]	[12]
Dezocine	DMJDB0Y	Major	Additive CNS depression effects by the combination of Lorazepam and Dezocine.	Pain [MG30-MG3Z]	[12]
Codeine	DMJX6ZG	Major	Additive CNS depression effects by the combination of Lorazepam and Codeine.	Pain [MG30-MG3Z]	[12]
Nalbuphine	DMOSQGU	Major	Additive CNS depression effects by the combination of Lorazepam and Nalbuphine.	Pain [MG30-MG3Z]	[12]
Buprenorphine	DMPRI8G	Major	Additive CNS depression effects by the combination of Lorazepam and Buprenorphine.	Pain [MG30-MG3Z]	[32]
Hydrocodone	DMQ2JO5	Major	Additive CNS depression effects by the combination of Lorazepam and Hydrocodone.	Pain [MG30-MG3Z]	[12]
Tramadol	DMRQD04	Major	Additive CNS depression effects by the combination of Lorazepam and Tramadol.	Pain [MG30-MG3Z]	[12]
Meperidine	DMX4GND	Major	Additive CNS depression effects by the combination of Lorazepam and Meperidine.	Pain [MG30-MG3Z]	[12]
Oxycodone	DMXLKHV	Major	Additive CNS depression effects by the combination of Lorazepam and Oxycodone.	Pain [MG30-MG3Z]	[12]
Fentanyl	DM8WAHT	Major	Additive CNS depression effects by the combination of Lorazepam and Fentanyl.	Sensation disturbance [MB40]	[12]
Tizanidine	DMR2IQ4	Moderate	Additive CNS depression effects by the combination of Lorazepam and Tizanidine.	Tonus and reflex abnormality [MB47]	[33]
Cetirizine	DMOMP9U	Moderate	Additive CNS depression effects by the combination of Lorazepam and Cetirizine.	Vasomotor/allergic rhinitis [CA08]	[34]
Amiodarone	DMUTEX3	Minor	Potentiate the pharmacologic effects by the combination of Lorazepam and Amiodarone.	Ventricular tachyarrhythmia [BC71]	[35]
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⏷ Show the Full List of 51 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Sodium stearyl fumarate	E00545	23665634	lubricant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Hypromellose	E00634	Not Available	Coating agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Lorazepam 0.5 mg tablet	0.5 mg	Oral Tablet	Oral
Lorazepam 1 mg tablet	1 mg	Oral Tablet	Oral
Lorazepam 2 mg tablet	2 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Lorazepam FDA Label
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5884).
3	Matzke GR, Zhanel GG, Guay DR: Clinical pharmacokinetics of vancomycin. Clin Pharmacokinet. 1986 Jul-Aug;11(4):257-82. doi: 10.2165/00003088-198611040-00001.
4	BDDCS applied to over 900 drugs
5	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.
6	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
7	Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
8	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
9	Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clin Pharmacol Ther. 2008 Apr;83(4):595-600.
10	Effect of the UGT2B15 genotype on the pharmacokinetics, pharmacodynamics, and drug interactions of intravenous lorazepam in healthy volunteers. Clin Pharmacol Ther. 2005 Jun;77(6):486-94.
11	Chun AH, Carrigan PJ, Hoffman DJ, Kershner RP, Stuart JD "Effect of antacids on absorption of clorazepate." Clin Pharmacol Ther 22 (1977): 329-35. [PMID: 19188]
12	US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
13	Product Information. Alinia (nitazoxanide). Romark Laboratories L.C., Tampa, FL.
14	US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
15	Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]
16	Gill SS, Wright EM, Reilly CS "Pharmacokinetic interaction of propofol and fentanyl: single bolus injection study." Br J Anaesth 65 (1990): 760-5. [PMID: 2265045]
17	Divoll M, Greenblatt DJ, Lacasse Y, Shader RI "Benzodiazepine overdosage: plasma concentrations and clinical outcome." Psychopharmacology (Berl) 73 (1981): 381-3. [PMID: 6789361]
18	Cerner Multum, Inc. "Australian Product Information.".
19	Backman JT, Olkkola KT, Ojala M, Laaksovirta H, Neuvonen PJ "Concentrations and effects of oral midazolam are greatly reduced in patients treated with carbamazepine or phenytoin." Epilepsia 37 (1996): 253-7. [PMID: 8598183]
20	Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
21	Castillo-Ferrando JR, Garcia M, Carmona J "Digoxin levels and diazepam." Lancet 2 (1980): 368. [PMID: 6105500]
22	Andrews C, Pinner G "Postural hypotension induced by paroxetine." BMJ 316 (1998): 595. [PMID: 9518913]
23	Hawksworth G, Betts T, Crowe A, et al "Diazepam/beta-adrenoceptor antagonist interactions." Br J Clin Pharmacol 17 Suppl 1 (1984): s69-76. [PMID: 6146341]
24	Abernethy DR, Greenblatt DJ, Ameer B, Shader RI "Probenecid impairment of acetaminophen and lorazepam clearance: direct inhibition of ether glucuronide formation." J Pharmacol Exp Ther 234 (1985): 345-9. [PMID: 4020675]
25	Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
26	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
27	Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
28	Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ.
29	Canadian Pharmacists Association.
30	Product Information. Gattex (teduglutide). NPS Pharmaceuticals, Bedminster, NJ.
31	Hansen BS, Dam M, Brandt J, et al "Influence of dextropropoxyphene on steady state serum levels and protein binding of three anti-epileptic drugs in man." Acta Neurol Scand 61 (1980): 357-67. [PMID: 6998251]
32	Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200]
33	Product Information. Zanaflex (tizanidine). Acorda Therapeutics, Hawthorne, NY.
34	Product Information. Zyrtec (cetirizine). Pfizer US Pharmaceuticals, New York, NY.
35	Kerin NZ, Aragon E, Faitel K, Frumin H, Rubenfire M "Long-term efficacy and toxicity of high- and low-dose amiodarone regimens." J Clin Pharmacol 29 (1989): 418-23. [PMID: 2661600]