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Diltiazem
Cardizem, Teczem, Tiamate, Tiazac (diltiazem) is a small molecule pharmaceutical. Diltiazem was first approved as Cardizem on 1982-11-05. It is used to treat atrial fibrillation, atrial flutter, hypertension, myocardial infarction, and supraventricular tachycardia amongst others in the USA. The pharmaceutical is active against voltage-dependent L-type calcium channel subunit alpha-1S. In addition, it is known to target potassium voltage-gated channel subfamily A member 5, 5-hydroxytryptamine receptor 3A, voltage-dependent L-type calcium channel subunit alpha-1C, potassium voltage-gated channel subfamily A member 1, cyclic nucleotide-gated cation channel alpha-3, voltage-dependent L-type calcium channel subunit alpha-1F, voltage-dependent L-type calcium channel subunit alpha-1D, cGMP-gated cation channel alpha-1, cyclic nucleotide-gated cation channel beta-3, cyclic nucleotide-gated olfactory channel, potassium voltage-gated channel subfamily A member 2, potassium voltage-gated channel subfamily C member 1, and potassium voltage-gated channel subfamily A member 7.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
cardiovascular diseasesD002318
signs and symptoms pathological conditionsD013568
Trade Name
FDA
EMA
Cardizem, Tiazac (generic drugs available since 1995-05-31, discontinued: Dilacor, Dilt-cd, Diltzac, Tiamate)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Diltiazem hydrochloride
Tradename
Company
Number
Date
Products
CARDIZEMBausch Health CompaniesN-018602 RX1982-11-05
4 products, RLD
CARDIZEM CDBausch Health CompaniesN-020062 RX1991-12-27
5 products, RLD
TIAZACBausch Health CompaniesN-020401 RX1995-09-11
6 products, RLD
CARDIZEM LABausch Health CompaniesN-021392 RX2003-02-06
6 products, RLD, RS
DILTIAZEM HYDROCHLORIDE IN DEXTROSE 5%Exela Pharma SciencesN-215252 PEND2021-10-28
2 products, RLD
Show 5 discontinued
Diltiazem malate
Tradename
Company
Number
Date
Products
TIAMATEMerck KGaAN-020506 DISCN1996-10-04
3 products
Hide discontinued
Diltiazem malate
+
Enalapril maleate
Tradename
Company
Number
Date
Products
TECZEMBausch Health CompaniesN-020507 DISCN1996-10-04
1 products
Hide discontinued
Labels
FDA
EMA
Brand Name
Status
Last Update
cardizemNew Drug Application2020-06-02
cartia xtANDA2022-04-06
diltiazem hydrochlorideANDA2023-06-15
taztiaANDA2017-10-31
tiazacNew Drug Application2020-10-01
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
atrial fibrillationEFO_0000275D001281I48.0
atrial flutterEFO_0003911D001282
hypertensionEFO_0000537D006973I10
myocardial infarctionEFO_0000612D009203I21
supraventricular tachycardiaHP_0004755D013617I47.1
variant angina pectorisD000788I20.1
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
C: Cardiovascular system drugs
C05: Vasoprotectives
C05A: Agents for treatment of hemorrhoids and anal fissures for topical use
C05AE: Muscle relaxants for treatment of hemorrhoids and anal fissures for topical use
C05AE03: Diltiazem
C08: Calcium channel blockers
C08D: Selective calcium channel blockers with direct cardiac effects
C08DB: Benzothiazepine derivative selective calcium channel blockers with direct cardiac effects
C08DB01: Diltiazem
HCPCS
No data
Clinical
Clinical Trials
17 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Migraine disordersD008881EFO_0003821G433151111
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Migraine without auraD020326EFO_0005296G43.0235
Migraine with auraD020325EFO_0005295G43.1235
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients515
Indications Phases 1
No data
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameDILTIAZEM
INNdiltiazem
Description
Diltiazem is a 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. It has a role as a calcium channel blocker, a vasodilator agent and an antihypertensive agent. It is a conjugate base of a diltiazem(1+). It is an enantiomer of an ent-diltiazem.
Classification
Small molecule
Drug classcalcium channel blockers (diltiazem type)
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1
Identifiers
PDB
CAS-ID42399-41-7
RxCUI3443
ChEMBL IDCHEMBL23
ChEBI ID101278
PubChem CID39186
DrugBankDB00343
UNII IDEE92BBP03H (ChemIDplus, GSRS)
Target
Agency Approved
CACNA1S
CACNA1S
Organism
Homo sapiens
Gene name
CACNA1S
Gene synonyms
CACH1, CACN1, CACNL1A3
NCBI Gene ID
Protein name
voltage-dependent L-type calcium channel subunit alpha-1S
Protein synonyms
Calcium channel, L type, alpha-1 polypeptide, isoform 3, skeletal muscle, calcium channel, voltage-dependent, L type, alpha 1S subunit, dihydropyridine receptor alpha 1 subunit, dihydropyridine-sensitive L-type calcium channel alpha-1 subunit, Voltage-gated calcium channel subunit alpha Cav1.1
Uniprot ID
Mouse ortholog
Cacna1s (12292)
voltage-dependent L-type calcium channel subunit alpha-1S (Q99240)
Alternate
KCNA5
KCNA5
HTR3A
HTR3A
CACNA1C
CACNA1C
KCNA1
KCNA1
CNGA3
CNGA3
CACNA1F
CACNA1F
CACNA1D
CACNA1D
CNGA1
CNGA1
CNGB3
CNGB3
CNGA2
CNGA2
KCNA2
KCNA2
KCNC1
KCNC1
KCNA7
KCNA7
Organism
Homo sapiens
Gene name
KCNA5
Gene synonyms
NCBI Gene ID
Protein name
potassium voltage-gated channel subfamily A member 5
Protein synonyms
cardiac potassium channel, HPCN1, insulinoma and islet potassium channel, potassium channel 1, potassium channel, voltage gated shaker related subfamily A, member 5, potassium voltage-gated channel, shaker-related subfamily, member 5, Voltage-gated potassium channel HK2, voltage-gated potassium channel protein Kv1.5, Voltage-gated potassium channel subunit Kv1.5
Uniprot ID
Mouse ortholog
Kcna5 (16493)
potassium voltage-gated channel subfamily A member 5 (Q9Z1R6)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 13,467 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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616 adverse events reported
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