lorazepam indications/contra

Stem definitionDrug idCAS RN
diazepam derivatives 1606 846-49-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ativan
  • Wy 4036
  • Wy-4036
  • lorazepam
A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.
  • Molecular weight: 321.16
  • Formula: C15H10Cl2N2O2
  • CLOGP: 2.37
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 61.69
  • ALOGS: -4.26
  • ROTB: 1

Drug dosage:

DoseUnitRoute
2.50 mg O
2.50 mg P
2.50 mg SL

Approvals:

DateAgencyCompanyOrphan
Sept. 30, 1977 FDA VALEANT INTL

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 4350.07 36.96 1149 6492 29965 3348253
Intentional overdose 2190.76 36.96 580 7061 14645 3363573
Toxicity to various agents 2164.78 36.96 742 6899 46312 3331906
Sopor 2107.35 36.96 433 7208 3331 3374887
Drug abuse 2065.60 36.96 576 7065 17754 3360464
Suicide attempt 1922.37 36.96 528 7113 15319 3362899
Overdose 1823.58 36.96 603 7038 33375 3344843
Somnolence 1632.63 36.96 548 7093 31656 3346562
Coma 1032.39 36.96 310 7331 12242 3365976
Agitation 1008.95 36.96 339 7302 19367 3358851
Poisoning 866.97 36.96 223 7418 4889 3373329
Delirium 857.11 36.96 253 7388 9375 3368843
Intentional self-injury 839.49 36.96 218 7423 4967 3373251
Respiratory arrest 786.17 36.96 246 7395 11122 3367096
Cardio-respiratory arrest 774.95 36.96 262 7379 15178 3363040
Tachycardia 744.13 36.96 283 7358 23088 3355130
Confusional state 739.49 36.96 323 7318 37675 3340543
Cardiac arrest 666.78 36.96 273 7368 27046 3351172
Hypotension 654.69 36.96 322 7319 49192 3329026
Sedation 647.58 36.96 184 7457 5917 3372301
Catatonia 502.15 36.96 112 7529 1288 3376930
Drug withdrawal syndrome 486.17 36.96 173 7468 11612 3366606
Fall 472.70 36.96 275 7366 58608 3319610
Unresponsive to stimuli 449.08 36.96 148 7493 7860 3370358
Drug interaction 432.94 36.96 240 7401 46572 3331646
Intentional product misuse 429.27 36.96 161 7480 12540 3365678
Neuroleptic malignant syndrome 426.48 36.96 124 7517 4317 3373901
Loss of consciousness 391.53 36.96 190 7451 27957 3350261
Anxiety 379.40 36.96 208 7433 39421 3338797
Respiratory depression 363.42 36.96 106 7535 3728 3374490

Pharmacologic Action:

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SourceCodeDescription
ATC N05BA06 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
ATC N05BA56 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
FDA EPC N0000175694 Benzodiazepine
FDA Chemical/Ingredient N0000007542 Benzodiazepines
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D000927 Anticonvulsants
MeSH PA D000932 Antiemetics
MeSH PA D001337 Autonomic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018682 GABA Agents
MeSH PA D018757 GABA Modulators
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D006993 Hypnotics and Sedatives
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Myoclonic seizure indication 37356005 DOID:308
Atonic seizure indication 42365007
Anxiety indication 48694002
Absence seizure indication 79631006 DOID:1825
Lennox-Gastaut syndrome indication 230418006
Status epilepticus indication 230456007 DOID:1824
Panic disorder indication 371631005 DOID:594
Sedation as Adjunct to Anesthesia indication
Induce Anterograde Amnesia indication
Suicidal thoughts contraindication 6471006
Hepatic encephalopathy contraindication 13920009 DOID:13413
Alcohol intoxication contraindication 25702006
Depressive disorder contraindication 35489007 DOID:2848
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Substance abuse contraindication 66214007
Sleep apnea contraindication 73430006 DOID:0050848
Decreased respiratory function contraindication 80954004
Open-angle glaucoma contraindication 84494001 DOID:1067
Kidney disease contraindication 90708001 DOID:2527
Hypoalbuminemia contraindication 119247004
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Syncope contraindication 271594007
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
At risk for aspiration contraindication 371736008
Angle-closure glaucoma contraindication 392291006 DOID:13550
Breastfeeding (mother) contraindication 413712001
Chronic lung disease contraindication 413839001
Central nervous system depression contraindication 418072004
Porphyria contraindication 418470004 DOID:13268
Delirium off-label use 2776000
Alcohol withdrawal delirium off-label use 8635005
General anesthesia off-label use 50697003
Seizure disorder off-label use 128613002 DOID:1826
Alcohol withdrawal syndrome off-label use 191480000
Insomnia off-label use 193462001
Spasticity off-label use 221360009
Chemotherapy-induced nausea and vomiting off-label use 236084000
Akathisia off-label use 285145004
Local anesthesia off-label use 386761002
Cocaine-Associated Acute Ischemic Heart Disease off-label use
Sedation in Intubated Patients off-label use
Manic Bipolar Disorder Adjunct Treatment off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.09 acidic
pKa2 11.41 acidic
pKa3 0.63 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR IC50 8.46 WOMBAT-PK CHEMBL
Fatty acid-binding protein, liver Unclassified Ki 4.89 CHEMBL

External reference:

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IDSource
DB00186 DRUGBANK_ID
4017848 VUID
N0000146205 NUI
C0024002 UMLSCUI
5884 IUPHAR_LIGAND_ID
D00365 KEGG_DRUG
CHEMBL580 ChEMBL_ID
2104 MMSL
6470 RXNORM
19225000 SNOMEDCT_US
387106007 SNOMEDCT_US
4995 MMSL
4017848 VANDF
N0000007094 NDFRT
N0000146205 NDFRT
001460 NDDF
d00149 MMSL
3958 PUBCHEM_CID
D008140 MESH_DESCRIPTOR_UI
O26FZP769L UNII
2809 INN_ID
CHEBI:6539 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0054-3532 SOLUTION, CONCENTRATE 2 mg ORAL ANDA 13 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0121-0770 LIQUID 2 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0179-0131 TABLET 0.50 mg ORAL ANDA 11 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0179-0148 TABLET 0.50 mg ORAL ANDA 11 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0179-0163 TABLET 1 mg ORAL ANDA 11 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0179-0185 TABLET 1 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0179-0186 TABLET 0.50 mg ORAL ANDA 12 sections
Ativan HUMAN PRESCRIPTION DRUG LABEL 1 0187-0063 TABLET 0.50 mg ORAL NDA 14 sections
Ativan HUMAN PRESCRIPTION DRUG LABEL 1 0187-0064 TABLET 1 mg ORAL NDA 14 sections
Ativan HUMAN PRESCRIPTION DRUG LABEL 1 0187-0065 TABLET 2 mg ORAL NDA 14 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-2321 TABLET 0.50 mg ORAL ANDA 13 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-2457 TABLET 1 mg ORAL ANDA 13 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-2777 TABLET 2 mg ORAL ANDA 13 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-1539 INJECTION, SOLUTION 4 mg INTRAMUSCULAR ANDA 15 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-1985 INJECTION, SOLUTION 2 mg INTRAMUSCULAR ANDA 15 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-6778 INJECTION, SOLUTION 2 mg INTRAMUSCULAR ANDA 15 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-6779 INJECTION, SOLUTION 4 mg INTRAMUSCULAR ANDA 15 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-6780 INJECTION, SOLUTION 2 mg INTRAMUSCULAR ANDA 15 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-6781 INJECTION, SOLUTION 4 mg INTRAMUSCULAR ANDA 15 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0591-0240 TABLET 0.50 mg ORAL ANDA 14 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0591-0241 TABLET 1 mg ORAL ANDA 14 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0591-0242 TABLET 2 mg ORAL ANDA 14 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0603-4246 TABLET 0.50 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0603-4247 TABLET 1 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0603-4248 TABLET 2 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-7805 TABLET 0.50 mg ORAL ANDA 11 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-8003 TABLET 0.50 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-8004 TABLET 1 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-8050 TABLET 2 mg ORAL ANDA 12 sections
Lorazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-8075 TABLET 0.50 mg ORAL ANDA 12 sections