midazolam indications/contra

Stem definitionDrug idCAS RN
diazepam derivatives 1802 59467-70-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • buccolam
  • midazolam
  • mezolam
  • midazolam hydrochloride
  • midazolam HCl
A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.
  • Molecular weight: 325.77
  • Formula: C18H13ClFN3
  • CLOGP: 3.42
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 30.18
  • ALOGS: -4.52
  • ROTB: 1

Drug dosage:

DoseUnitRoute
15 mg O
15 mg P

Approvals:

DateAgencyCompanyOrphan
Dec. 20, 1985 FDA

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
Hypotension 664.95 47.44 245 2686 49269 3333659
Anaphylactic reaction 497.34 47.44 143 2788 12911 3370017
Drug ineffective 495.99 47.44 256 2675 115834 3267094
Oxygen saturation decreased 444.95 47.44 124 2807 9967 3372961
Cardiac arrest 382.27 47.44 140 2791 27179 3355749
Toxicity to various agents 324.59 47.44 145 2786 46909 3336019
Respiratory depression 303.08 47.44 75 2856 3759 3379169
Sedation 250.30 47.44 71 2860 6030 3376898
Bradycardia 249.58 47.44 90 2841 16579 3366349
Agitation 245.74 47.44 93 2838 19613 3363315
Status epilepticus 233.85 47.44 60 2871 3475 3379453
Unresponsive to stimuli 218.53 47.44 68 2863 7940 3374988
Tachycardia 216.58 47.44 89 2842 23282 3359646
Respiratory arrest 210.69 47.44 72 2859 11296 3371632
Respiratory failure 193.75 47.44 82 2849 23059 3359869
Seizure 190.35 47.44 96 2835 40304 3342624
Delirium 190.23 47.44 64 2867 9564 3373364
Hypoxia 189.82 47.44 64 2867 9627 3373301
Procedural complication 187.48 47.44 46 2885 2214 3380714
Blood pressure decreased 167.55 47.44 64 2867 13772 3369156
Cardio-respiratory arrest 160.74 47.44 64 2867 15376 3367552
Drug interaction 154.98 47.44 88 2843 46724 3336204
Depressed level of consciousness 153.17 47.44 57 2874 11408 3371520
Apnoea 143.77 47.44 38 2893 2464 3380464
Intestinal ischaemia 135.47 47.44 34 2897 1793 3381135
Anaphylactic shock 132.72 47.44 43 2888 5696 3377232
Coma 130.47 47.44 52 2879 12500 3370428
Anaesthetic complication 129.66 47.44 28 2903 757 3382171
Dyskinesia 126.50 47.44 44 2887 7241 3375687
Acidosis hyperchloraemic 120.72 47.44 20 2911 117 3382811

Pharmacologic Action:

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SourceCodeDescription
ATC N05CD08 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives
FDA EPC N0000175694 Benzodiazepine
FDA Chemical/Ingredient N0000007542 Benzodiazepines
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000777 Anesthetics
MeSH PA D018681 Anesthetics, General
MeSH PA D018686 Anesthetics, Intravenous
MeSH PA D014151 Anti-Anxiety 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 D006993 Hypnotics and Sedatives
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Feeling agitated indication 24199005
Anxiety indication 48694002
General anesthesia indication 50697003
Sedation indication 72641008
Conscious sedation indication 314271007
Local anesthesia indication 386761002
Sedation in Intubated Patients indication
Induce Anterograde Amnesia indication
Sedation as Adjunct to Anesthesia indication
Preoperative Anxiety indication
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Cirrhosis of liver contraindication 19943007 DOID:5082
Shock contraindication 27942005
End stage renal disease contraindication 46177005 DOID:784
Chronic heart failure contraindication 48447003
Pregnancy, function contraindication 289908002
Coma contraindication 371632003
Angle-closure glaucoma contraindication 392291006 DOID:13550
Hemodynamic instability contraindication 422773005
Peripheral Vasoconstriction contraindication
Insomnia off-label use 193462001
Status epilepticus off-label use 230456007 DOID:1824
Cocaine-Associated Acute Ischemic Heart Disease off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.07 Basic
pKa2 2.36 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-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.74 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.44 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-3/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.26 WOMBAT-PK CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.12 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.61 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.75 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 9.12 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.26 WOMBAT-PK CHEMBL
Multidrug resistance protein 1 Transporter Km 4.35 WOMBAT-PK
Cytochrome P450 3A4 Enzyme Km 6 WOMBAT-PK
Thyrotropin-releasing hormone receptor GPCR ANTAGONIST Ki 5.49 IUPHAR
GABA-A receptor; anion channel Ion channel Ki 8.70 CHEMBL
Translocator protein Membrane receptor Ki 8.70 CHEMBL

External reference:

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IDSource
3342 IUPHAR_LIGAND_ID
4019839 VUID
N0000147927 NUI
C0026056 UMLSCUI
D00550 KEGG_DRUG
CHEMBL655 ChEMBL_ID
DB00683 DRUGBANK_ID
4019839 VANDF
6960 RXNORM
26800000 SNOMEDCT_US
373476007 SNOMEDCT_US
d00301 MMSL
130935 MMSL
24970 MMSL
N0000006704 NDFRT
N0000147927 NDFRT
004585 NDDF
4192 PUBCHEM_CID
CHEMBL1200420 ChEMBL_ID
D008874 MESH_DESCRIPTOR_UI
R60L0SM5BC UNII
4497 INN_ID
59467-96-8 SECONDARY_CAS_RN
CHEBI:6931 CHEBI
08J PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-3566 SYRUP 2 mg ORAL ANDA 14 sections
MIDAZOLAM HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0409-2305 INJECTION, SOLUTION 1 mg INTRAMUSCULAR ANDA 15 sections
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2306 INJECTION, SOLUTION 1 mg INTRAMUSCULAR ANDA 15 sections
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2307 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 15 sections
MIDAZOLAM HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0409-2308 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 15 sections
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2587 INJECTION, SOLUTION 1 mg INTRAMUSCULAR ANDA 15 sections
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0409-2596 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 15 sections
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0574-0150 SYRUP 2 mg ORAL ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6056 INJECTION 1 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6057 INJECTION 1 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6059 INJECTION 1 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6060 INJECTION 5 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6061 INJECTION 5 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6063 INJECTION 5 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6190 INJECTION 5 mg INTRAMUSCULAR ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6209 INJECTION 1 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6210 INJECTION 1 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 0641-6211 INJECTION 5 mg INTRAMUSCULAR ANDA 16 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 17478-523 INJECTION 1 mg INTRAVENOUS ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 17478-524 INJECTION 5 mg INTRAVENOUS ANDA 15 sections
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17856-0205 SYRUP 2 mg ORAL ANDA 12 sections
Midazolam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17856-3566 SYRUP 2 mg ORAL ANDA 13 sections
Midazolam hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 23155-600 INJECTION, SOLUTION 1 mg INTRAMUSCULAR ANDA 14 sections
Midazolam hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 23155-601 INJECTION, SOLUTION 5 mg INTRAVENOUS ANDA 14 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 25021-655 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 25021-656 INJECTION, SOLUTION 5 mg INTRAVENOUS ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 25021-660 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 25021-661 INJECTION, SOLUTION 5 mg INTRAVENOUS ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 47781-588 INJECTION, SOLUTION 2 mg INTRAVENOUS ANDA 15 sections
Midazolam HUMAN PRESCRIPTION DRUG LABEL 1 47781-589 INJECTION, SOLUTION 5 mg INTRAVENOUS ANDA 15 sections