diltiazem indications/contra

Stem definitionDrug idCAS RN
calcium channel blockers, diltiazem derivatives 897 42399-41-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • (+)-Diltiazem
  • dilzem
  • d-Diltiazem
  • d-cis-Diltiazem
  • diltiazem hydrochloride
  • diltiazem malate
  • diltiazem
  • diltiazem HCl
A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
  • Molecular weight: 414.52
  • Formula: C22H26N2O4S
  • CLOGP: 3.65
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 59.08
  • ALOGS: -4.39
  • ROTB: 7

Drug dosage:

DoseUnitRoute
0.24 g O

Approvals:

DateAgencyCompanyOrphan
Nov. 5, 1982 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 4660.25 38.64 1077 3312 30037 3351433
Bradycardia 1560.50 38.64 402 3987 16267 3365203
Toxicity to various agents 1168.11 38.64 407 3982 46647 3334823
Hypotension 1037.43 38.64 378 4011 49136 3332334
Cardiac arrest 878.53 38.64 288 4101 27031 3354439
Poisoning 878.52 38.64 202 4187 4910 3376560
Overdose 793.89 38.64 282 4107 33696 3347774
Drug abuse 635.31 38.64 205 4184 18125 3363345
Drug interaction 622.87 38.64 258 4131 46554 3334916
Intentional overdose 558.86 38.64 178 4211 15047 3366423
Respiratory arrest 380.10 38.64 124 4265 11244 3370226
Intentional product misuse 354.79 38.64 121 4268 12580 3368890
Atrioventricular block complete 347.74 38.64 83 4306 2349 3379121
Drug hypersensitivity 340.12 38.64 156 4233 35524 3345946
Medication error 335.07 38.64 114 4275 11757 3369713
Sinus bradycardia 310.92 38.64 81 4308 3298 3378172
Nodal rhythm 300.46 38.64 58 4331 569 3380901
Atrial fibrillation 300.10 38.64 127 4262 23814 3357656
Dizziness 287.92 38.64 180 4209 76332 3305138
Heart rate decreased 275.15 38.64 81 4308 5197 3376273
Death 272.89 38.64 228 4161 152096 3229374
Acute kidney injury 236.03 38.64 136 4253 49547 3331923
Cardiogenic shock 222.07 38.64 64 4325 3802 3377668
Acute generalised exanthematous pustulosis 215.81 38.64 55 4334 2044 3379426
Exposure via ingestion 208.35 38.64 50 4339 1443 3380027
Syncope 203.53 38.64 99 4290 25534 3355936
Rhabdomyolysis 201.99 38.64 85 4304 15644 3365826
Cardio-respiratory arrest 180.23 38.64 78 4311 15362 3366108
Atrioventricular block 170.91 38.64 46 4343 2118 3379352
Atrioventricular block first degree 164.09 38.64 42 4347 1586 3379884

Pharmacologic Action:

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SourceCodeDescription
ATC C05AE03 CARDIOVASCULAR SYSTEM
VASOPROTECTIVES
AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
Muscle relaxants
ATC C08DB01 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH DIRECT CARDIAC EFFECTS
Benzothiazepine derivatives
FDA MoA N0000000069 Calcium Channel Antagonists
FDA EPC N0000175566 Calcium Channel Blocker
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:35674 antihypertensive agent

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Atrial fibrillation indication 49436004 DOID:0060224
Paroxysmal supraventricular tachycardia indication 67198005
Prinzmetal angina indication 87343002
Angina pectoris indication 194828000
Hyperkalemia contraindication 14140009
Ventricular tachycardia contraindication 25569003
Complete atrioventricular block contraindication 27885002
Acute cerebrovascular insufficiency contraindication 29322000
Sick sinus syndrome contraindication 36083008 DOID:13884
Immunosuppression contraindication 38013005
Angioedema contraindication 41291007 DOID:1558
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Lown-Ganong-Levine syndrome contraindication 55475008 DOID:13087
Aortic valve stenosis contraindication 60573004 DOID:1712
Wolff-Parkinson-White pattern contraindication 74390002 DOID:384
Transplantation contraindication 77465005
Chronic idiopathic constipation contraindication 82934008
Hereditary angioneurotic edema contraindication 82966003 DOID:14735
Cardiogenic shock contraindication 89138009
Hyponatremia contraindication 89627008
Kidney disease contraindication 90708001 DOID:2527
Disorder of connective tissue contraindication 105969002 DOID:65
Second degree atrioventricular block contraindication 195042002
Decompensated cardiac failure contraindication 195111005
Hypertrophic cardiomyopathy contraindication 233873004 DOID:11984
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Left ventricular cardiac dysfunction contraindication 429589006
Hemodialysis with High-Flux Membrane contraindication
Supraventricular arrhythmia off-label use 72654001
Diastolic heart failure off-label use 418304008 DOID:9775

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.63 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
120MG CARDIZEM LA VALEANT INTL N021392 Feb. 6, 2003 RX TABLET, EXTENDED RELEASE ORAL 7108866 Dec. 17, 2019 TREATMENT OF HYPERTENSION AND ANGINA PECTORIS
180MG CARDIZEM LA VALEANT INTL N021392 Feb. 6, 2003 RX TABLET, EXTENDED RELEASE ORAL 7108866 Dec. 17, 2019 TREATMENT OF HYPERTENSION AND ANGINA PECTORIS
240MG CARDIZEM LA VALEANT INTL N021392 Feb. 6, 2003 RX TABLET, EXTENDED RELEASE ORAL 7108866 Dec. 17, 2019 TREATMENT OF HYPERTENSION AND ANGINA PECTORIS
300MG CARDIZEM LA VALEANT INTL N021392 Feb. 6, 2003 RX TABLET, EXTENDED RELEASE ORAL 7108866 Dec. 17, 2019 TREATMENT OF HYPERTENSION AND ANGINA PECTORIS
360MG CARDIZEM LA VALEANT INTL N021392 Feb. 6, 2003 RX TABLET, EXTENDED RELEASE ORAL 7108866 Dec. 17, 2019 TREATMENT OF HYPERTENSION AND ANGINA PECTORIS
420MG CARDIZEM LA VALEANT INTL N021392 Feb. 6, 2003 RX TABLET, EXTENDED RELEASE ORAL 7108866 Dec. 17, 2019 TREATMENT OF HYPERTENSION AND ANGINA PECTORIS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER IC50 7.32 WOMBAT-PK CHEMBL
Voltage-dependent calcium channel gamma-1 subunit Ion channel IC50 6.10 WOMBAT-PK
Cytochrome P450 3A4 Enzyme IC50 5.74 DRUG MATRIX
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel Ki 4.02 WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR Ki 5.62 PDSP
Multidrug resistance protein 1 Transporter IC50 4.37 CHEMBL
Solute carrier family 22 member 1 Transporter IC50 4.91 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.76 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1S Ion channel Ki 6.42 CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 4.35 CHEMBL
5-hydroxytryptamine receptor 3A Ion channel BLOCKER IC50 4.68 IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel IC50 4.52 CHEMBL
Voltage-gated L-type calcium channel Ion channel Ki 7.80 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel IC50 7.34 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel IC50 7.27 CHEMBL
Potassium voltage-gated channel subfamily C member 1 Unclassified BLOCKER IC50 4 IUPHAR
Potassium voltage-gated channel subfamily A member 7 Unclassified BLOCKER IC50 4.20 IUPHAR
5-hydroxytryptamine receptor 3A Ion channel BLOCKER IC50 5.26 IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1F Unclassified BLOCKER IC50 4 IUPHAR

External reference:

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IDSource
DB00343 DRUGBANK_ID
2298 IUPHAR_LIGAND_ID
4020128 VUID
N0000179650 NUI
C0700579 UMLSCUI
D00616 KEGG_DRUG
CHEMBL23 ChEMBL_ID
14Y6444DRP UNII
144604-00-2 SECONDARY_CAS_RN
3443 RXNORM
372793000 SNOMEDCT_US
59941008 SNOMEDCT_US
4019722 VANDF
N0000006682 NDFRT
N0000147814 NDFRT
004514 NDDF
d00045 MMSL
39186 PUBCHEM_CID
CHEMBL1697 ChEMBL_ID
CHEMBL1200805 ChEMBL_ID
D004110 MESH_DESCRIPTOR_UI
3433 INN_ID
CHEBI:101278 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0074-3045 TABLET, EXTENDED RELEASE 120 mg ORAL NDA 12 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0074-3061 TABLET, EXTENDED RELEASE 180 mg ORAL NDA 12 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0074-3062 TABLET, EXTENDED RELEASE 240 mg ORAL NDA 12 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0074-3063 TABLET, EXTENDED RELEASE 300 mg ORAL NDA 12 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0074-3064 TABLET, EXTENDED RELEASE 360 mg ORAL NDA 12 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0074-3069 TABLET, EXTENDED RELEASE 420 mg ORAL NDA 12 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0318 TABLET, FILM COATED 30 mg ORAL ANDA 11 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0319 TABLET, FILM COATED 60 mg ORAL ANDA 11 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0320 TABLET, FILM COATED 90 mg ORAL ANDA 11 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-0321 TABLET, FILM COATED 120 mg ORAL ANDA 11 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5112 CAPSULE, EXTENDED RELEASE 120 mg ORAL ANDA 12 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5117 CAPSULE, EXTENDED RELEASE 180 mg ORAL ANDA 12 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5118 CAPSULE, EXTENDED RELEASE 240 mg ORAL ANDA 12 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5119 CAPSULE, EXTENDED RELEASE 300 mg ORAL ANDA 12 sections
Diltiazem Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0179-0110 TABLET, FILM COATED 120 mg ORAL ANDA 11 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0771 TABLET, COATED 30 mg ORAL NDA 12 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0772 TABLET, COATED 60 mg ORAL NDA 12 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0791 TABLET, COATED 90 mg ORAL NDA 12 sections
Cardizem HUMAN PRESCRIPTION DRUG LABEL 1 0187-0792 TABLET, COATED 120 mg ORAL NDA 12 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0795 CAPSULE, COATED, EXTENDED RELEASE 120 mg ORAL NDA 12 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0796 CAPSULE, COATED, EXTENDED RELEASE 180 mg ORAL NDA 12 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0797 CAPSULE, COATED, EXTENDED RELEASE 240 mg ORAL NDA 12 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0798 CAPSULE, COATED, EXTENDED RELEASE 300 mg ORAL NDA 12 sections
Cardizem CD HUMAN PRESCRIPTION DRUG LABEL 1 0187-0799 CAPSULE, COATED, EXTENDED RELEASE 360 mg ORAL NDA 12 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2045 TABLET, EXTENDED RELEASE 120 mg ORAL NDA 16 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2046 TABLET, EXTENDED RELEASE 180 mg ORAL NDA 16 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2047 TABLET, EXTENDED RELEASE 240 mg ORAL NDA 16 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2048 TABLET, EXTENDED RELEASE 300 mg ORAL NDA 16 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2049 TABLET, EXTENDED RELEASE 360 mg ORAL NDA 16 sections
Cardizem LA HUMAN PRESCRIPTION DRUG LABEL 1 0187-2050 TABLET, EXTENDED RELEASE 420 mg ORAL NDA 16 sections