propofol indications/contra

Stem definitionDrug idCAS RN
2302 2078-54-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • propofol
  • ampofol
  • diprivan
  • disoprofol
  • pofol
An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.
  • Molecular weight: 178.28
  • Formula: C12H18O
  • CLOGP: 3.93
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 1
  • TPSA: 20.23
  • ALOGS: -3.05
  • ROTB: 2

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Oct. 2, 1989 FDA FRESENIUS KABI USA

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
Propofol infusion syndrome 1897.03 55.74 265 5983 17 3379594
Anaphylactic shock 1672.96 55.74 372 5876 5367 3374244
Hypotension 1502.85 55.74 545 5703 48969 3330642
Cardiac arrest 1050.77 55.74 360 5888 26959 3352652
Rhabdomyolysis 996.17 55.74 303 5945 15426 3364185
Bronchospasm 929.88 55.74 219 6029 4075 3375536
Anaphylactic reaction 806.58 55.74 247 6001 12807 3366804
Bradycardia 731.09 55.74 243 6005 16426 3363185
Post procedural complication 695.91 55.74 179 6069 4838 3374773
Delayed recovery from anaesthesia 634.40 55.74 104 6144 211 3379400
Oxygen saturation decreased 627.19 55.74 192 6056 9899 3369712
Circulatory collapse 574.33 55.74 160 6088 5889 3373722
Hyperthermia malignant 523.72 55.74 96 6152 458 3379153
Metabolic acidosis 486.11 55.74 153 6095 8625 3370986
Respiratory depression 483.85 55.74 127 6121 3707 3375904
Tachycardia 483.23 55.74 196 6052 23175 3356436
Ventricular fibrillation 435.82 55.74 120 6128 4213 3375398
Blood pressure decreased 432.77 55.74 157 6091 13679 3365932
Shock 400.96 55.74 125 6123 6812 3372799
Acute kidney injury 375.13 55.74 208 6040 49475 3330136
Pyrexia 344.39 55.74 235 6013 80880 3298731
Chills 323.12 55.74 145 6103 21877 3357734
Pulseless electrical activity 314.21 55.74 76 6172 1572 3378039
Drug interaction 304.66 55.74 178 6070 46634 3332977
Product contamination microbial 303.30 55.74 50 6198 106 3379505
Ventricular tachycardia 286.43 55.74 93 6155 5769 3373842
Blood creatine phosphokinase increased 285.17 55.74 114 6134 12899 3366712
Respiratory arrest 271.51 55.74 106 6142 11262 3368349
Drug use disorder 257.88 55.74 58 6190 860 3378751
Anaesthetic complication 250.19 55.74 55 6193 730 3378881

Pharmacologic Action:

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SourceCodeDescription
ATC N01AX10 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, GENERAL
Other general anesthetics
CHEBI has role CHEBI:38877 intravenous anaesthetic
CHEBI has role CHEBI:35717 sedative
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:35623 anticonvulsant
FDA PE N0000175975 General Anesthesia
FDA EPC N0000175681 General Anesthetic
MeSH PA D000777 Anesthetics
MeSH PA D018681 Anesthetics, General
MeSH PA D018686 Anesthetics, Intravenous
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D006993 Hypnotics and Sedatives

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
General anesthesia indication 50697003
Sedation in Intubated Patients indication
Sedation as Adjunct to Anesthesia indication
Apnea contraindication 1023001
Asthenia contraindication 13791008
Hypovolemia contraindication 28560003
Low blood pressure contraindication 45007003
Cerebral arteriosclerosis contraindication 65312002
Decreased respiratory function contraindication 80954004
Epilepsy contraindication 84757009 DOID:1826
Myocardial dysfunction contraindication 233928007
Disorder of lipid metabolism contraindication 267431006
Hypoxia contraindication 389086002

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.8 acidic

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-2/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 4.95 CHEMBL CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 5.39 CHEMBL CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 5.70 CHEMBL CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 5.22 DRUG MATRIX
Cytochrome P450 2C9 Enzyme IC50 4.91 WOMBAT-PK
Carbonic anhydrase 1 Enzyme IC50 4.71 WOMBAT-PK
Carbonic anhydrase 2 Enzyme IC50 4.01 WOMBAT-PK
Fatty-acid amide hydrolase 1 Enzyme IC50 4.28 WOMBAT-PK
Prostaglandin G/H synthase 1 Enzyme IC50 5.42 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.03 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 5.46 DRUG MATRIX
Arachidonate 15-lipoxygenase Enzyme IC50 5.12 DRUG MATRIX
Fatty-acid amide hydrolase 1 Enzyme IC50 4.85 CHEMBL
GABA-A receptor; anion channel Ion channel IC50 5.40 CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 Ion channel BLOCKER IC50 5.20 IUPHAR

External reference:

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IDSource
CHEBI:44915 CHEBI
4019500 VUID
N0000147620 NUI
C0033487 UMLSCUI
5464 IUPHAR_LIGAND_ID
D00549 KEGG_DRUG
CHEMBL526 ChEMBL_ID
DB00818 DRUGBANK_ID
4019500 VANDF
14179 MMSL
8782 RXNORM
387423006 SNOMEDCT_US
74674007 SNOMEDCT_US
5372 MMSL
d00933 MMSL
N0000006386 NDFRT
N0000147620 NDFRT
003528 NDDF
D015742 MESH_DESCRIPTOR_UI
YI7VU623SF UNII
5073 INN_ID
4943 PUBCHEM_CID
PFL PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
PROPOFOL HUMAN PRESCRIPTION DRUG LABEL 1 0409-4699 INJECTION, EMULSION 10 mg INTRAVENOUS ANDA 14 sections
Propofol HUMAN PRESCRIPTION DRUG LABEL 1 0591-2136 INJECTION, EMULSION 10 mg INTRAVENOUS ANDA 14 sections
propofol HUMAN PRESCRIPTION DRUG LABEL 1 25021-608 INJECTION, EMULSION 10 mg INTRAVENOUS ANDA 15 sections
Anesthesia S/I-50 HUMAN PRESCRIPTION DRUG LABEL 2 49836-023 KIT 10 mg None NDA 17 sections
Anesthesia S/I-60 HUMAN PRESCRIPTION DRUG LABEL 2 49836-024 KIT 10 mg None NDA 18 sections
Anesthesia S/I-40 HUMAN PRESCRIPTION DRUG LABEL 2 49836-025 KIT 10 mg None NDA 15 sections
Diprivan HUMAN PRESCRIPTION DRUG LABEL 1 52584-269 INJECTION, EMULSION 10 mg INTRAVENOUS NDA 11 sections
Propofol HUMAN PRESCRIPTION DRUG LABEL 1 52584-699 INJECTION, EMULSION 10 mg INTRAVENOUS ANDA 12 sections
Diprivan HUMAN PRESCRIPTION DRUG LABEL 1 63323-269 INJECTION, EMULSION 10 mg INTRAVENOUS NDA 14 sections
Propofol HUMAN PRESCRIPTION DRUG LABEL 1 63323-270 INJECTION, EMULSION 10 mg INTRAVENOUS NDA 13 sections