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
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 |
---|---|---|---|---|
CARDIZEM | Bausch Health Companies | N-018602 RX | 1982-11-05 | 4 products, RLD |
CARDIZEM CD | Bausch Health Companies | N-020062 RX | 1991-12-27 | 5 products, RLD |
TIAZAC | Bausch Health Companies | N-020401 RX | 1995-09-11 | 6 products, RLD |
CARDIZEM LA | Bausch Health Companies | N-021392 RX | 2003-02-06 | 6 products, RLD, RS |
DILTIAZEM HYDROCHLORIDE IN DEXTROSE 5% | Exela Pharma Sciences | N-215252 PEND | 2021-10-28 | 2 products, RLD |
Show 5 discontinued
Diltiazem malate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
TIAMATE | Merck KGaA | N-020506 DISCN | 1996-10-04 | 3 products |
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Diltiazem malate
+
Enalapril maleate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
TECZEM | Bausch Health Companies | N-020507 DISCN | 1996-10-04 | 1 products |
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Labels
FDA
EMA
Brand Name | Status | Last Update |
---|---|---|
cardizem | New Drug Application | 2020-06-02 |
cartia xt | ANDA | 2022-04-06 |
diltiazem hydrochloride | ANDA | 2023-06-15 |
taztia | ANDA | 2017-10-31 |
tiazac | New Drug Application | 2020-10-01 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
---|---|---|---|
atrial fibrillation | EFO_0000275 | D001281 | I48.0 |
atrial flutter | EFO_0003911 | D001282 | — |
hypertension | EFO_0000537 | D006973 | I10 |
myocardial infarction | EFO_0000612 | D009203 | I21 |
supraventricular tachycardia | HP_0004755 | D013617 | I47.1 |
variant angina pectoris | — | D000788 | I20.1 |
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 disorders | D008881 | EFO_0003821 | G43 | 3 | 1 | 5 | 1 | 1 | 11 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
---|---|---|---|---|---|---|---|---|---|
Migraine without aura | D020326 | EFO_0005296 | G43.0 | 2 | — | 3 | — | — | 5 |
Migraine with aura | D020325 | EFO_0005295 | G43.1 | 2 | — | 3 | — | — | 5 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
---|---|---|---|---|---|---|---|---|---|
Healthy volunteers/patients | — | 5 | 1 | — | — | — | 5 |
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 name | DILTIAZEM |
INN | diltiazem |
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 class | calcium 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-ID | 42399-41-7 |
RxCUI | 3443 |
ChEMBL ID | CHEMBL23 |
ChEBI ID | 101278 |
PubChem CID | 39186 |
DrugBank | DB00343 |
UNII ID | EE92BBP03H (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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