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diltiazem 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
calcium channel blockers, diltiazem derivatives	897	42399-41-7

Description:

Molecule	Description
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 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.24	g	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	5.60 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	4.10 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	38 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	19.30 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	13 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.18 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Nov. 5, 1982	FDA	VALEANT INTL

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sedation complication	611.73	10.05	346	106534	13476	63368666
Creatinine renal clearance decreased	571.39	10.05	351	106529	15957	63366185
Atrial fibrillation	569.05	10.05	833	106047	115803	63266339
Orthostatic hypotension	525.87	10.05	457	106423	35703	63346439
Completed suicide	505.71	10.05	891	105989	144782	63237360
Hypotension	440.42	10.05	1226	105654	271378	63110764
Blood calcium decreased	410.42	10.05	347	106533	26104	63356038
Sedation	394.28	10.05	402	106478	38407	63343735
Balance disorder	360.52	10.05	567	106313	83855	63298287
Cognitive disorder	335.38	10.05	441	106439	55374	63326768

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Completed suicide	257.61	10.77	503	52786	97665	34805977
Bradycardia	245.22	10.77	424	52865	74994	34828648
Atrial fibrillation	244.49	10.77	561	52728	121832	34781810
Cardiac failure congestive	147.98	10.77	365	52924	82905	34820737
Hypotension	123.47	10.77	664	52625	220985	34682657
Off label use	114.30	10.77	299	52990	419225	34484417
Dyspnoea	101.71	10.77	946	52343	375836	34527806
Mycotic allergy	93.03	10.77	35	53254	573	34903069
Conjunctivitis allergic	89.33	10.77	41	53248	1129	34902513
Mite allergy	88.15	10.77	35	53254	667	34902975

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Completed suicide	701.16	9.65	1409	137488	244358	79361133
Sedation complication	591.16	9.65	358	138539	15311	79590180
Creatinine renal clearance decreased	554.29	9.65	369	138528	18633	79586858
Atrial fibrillation	545.57	9.65	1119	137778	196767	79408724
Hypotension	480.05	9.65	1769	137128	438548	79166943
Bradycardia	427.05	9.65	811	138086	134746	79470745
Orthostatic hypotension	402.73	9.65	493	138404	55671	79549820
Blood calcium decreased	371.24	9.65	361	138536	31458	79574033
Cardiac failure congestive	357.00	9.65	775	138122	141627	79463864
Balance disorder	336.99	9.65	612	138285	98245	79507246

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
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
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38215	calcium channel blockers
FDA EPC	N0000175566	Calcium Channel Blocker
FDA MoA	N0000000069	Calcium Channel Antagonists
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002121	Calcium Channel Blockers

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
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
Anal fissure	off-label use	30037006
Supraventricular arrhythmia	off-label use	72654001
Diastolic heart failure	off-label use	418304008	DOID:9775
Hyperkalemia	contraindication	14140009
Ventricular tachycardia	contraindication	25569003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.63	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Voltage-dependent L-type calcium channel subunit alpha-1C	Ion channel	Q13936	CAC1C_HUMAN	BLOCKER	IC50	7.32	WOMBAT-PK	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	5.74	DRUG MATRIX
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	4.37	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	5.62	PDSP
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN	BLOCKER	IC50	4.68	IUPHAR
Voltage-dependent calcium channel gamma-1 subunit	Ion channel	Q06432	CCG1_HUMAN		IC50	6.10	WOMBAT-PK
Voltage-dependent T-type calcium channel subunit alpha-1H	Ion channel	O95180	CAC1H_HUMAN		Ki	4.02	WOMBAT-PK
Voltage-dependent L-type calcium channel subunit alpha-1S	Ion channel	Q13698	CAC1S_HUMAN		Ki	6.42	CHEMBL
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	4.91	CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	4.35	CHEMBL

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External reference:

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ID	Source
C9F	PDB_CHEM_ID
000711	NDDF
004514	NDDF
007237	NDDF
12218006	SNOMEDCT_US
144604-00-2	SECONDARY_CAS_RN
1547	MMSL
203211	RXNORM
2298	IUPHAR_LIGAND_ID
33286-22-5	SECONDARY_CAS_RN

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cardizem	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0771	TABLET, COATED	30 mg	ORAL	NDA	21 sections
Cardizem	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0772	TABLET, COATED	60 mg	ORAL	NDA	21 sections
Cardizem	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0791	TABLET, COATED	90 mg	ORAL	NDA	21 sections
Cardizem	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0792	TABLET, COATED	120 mg	ORAL	NDA	21 sections
Cardizem CD	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0795	CAPSULE, COATED, EXTENDED RELEASE	120 mg	ORAL	NDA	14 sections
Cardizem CD	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0796	CAPSULE, COATED, EXTENDED RELEASE	180 mg	ORAL	NDA	14 sections
Cardizem CD	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0797	CAPSULE, COATED, EXTENDED RELEASE	240 mg	ORAL	NDA	14 sections
Cardizem CD	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0798	CAPSULE, COATED, EXTENDED RELEASE	300 mg	ORAL	NDA	14 sections
Cardizem CD	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0799	CAPSULE, COATED, EXTENDED RELEASE	360 mg	ORAL	NDA	14 sections
Cardizem LA	HUMAN PRESCRIPTION DRUG LABEL	1	0187-2045	TABLET, EXTENDED RELEASE	120 mg	ORAL	NDA	25 sections

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