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

Stem definition	Drug id	CAS RN
	2657	55142-85-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ticlopidine ticlop ticlid tiklyd ticlopidine hydrochloride ticlopidine HCl	An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES. Molecular weight: 263.78 Formula: C14H14ClNS CLOGP: 4.39 LIPINSKI: 0 HAC: 1 HDO: 0 TPSA: 3.24 ALOGS: -4.08 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ticlopidine
ticlop
ticlid
tiklyd
ticlopidine hydrochloride
ticlopidine HCl

An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.

Molecular weight: 263.78
Formula: C14H14ClNS
CLOGP: 4.39
LIPINSKI: 0
HAC: 1
HDO: 0
TPSA: 3.24
ALOGS: -4.08
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.50	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	80 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	15.81 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Oct. 31, 1991	FDA

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
Drug interaction	67.87	30.47	48	1287	229083	63258604
Sopor	52.05	30.47	19	1316	22145	63465542
Hyponatraemic syndrome	44.28	30.47	8	1327	547	63487140
Hyperkalaemia	41.48	30.47	21	1314	54182	63433505
Apraxia	40.21	30.47	9	1326	1812	63485875
Hypochloraemia	39.33	30.47	9	1326	2000	63485687
Hypercreatininaemia	37.61	30.47	7	1328	564	63487123
Cerebral haemorrhage	36.08	30.47	16	1319	30713	63456974
Melaena	33.07	30.47	15	1320	30350	63457337

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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
Drug interaction	56.34	28.00	57	1385	225889	34729600
Sopor	50.71	28.00	19	1423	12117	34943372
Slow speech	48.51	28.00	11	1431	1191	34954298
Intentional self-injury	41.44	28.00	17	1425	13754	34941735
Alcohol interaction	38.85	28.00	11	1431	2902	34952587
Melaena	36.59	28.00	21	1421	35359	34920130
Electrocardiogram QT prolonged	31.24	28.00	20	1422	40932	34914557
Hyponatraemia	30.40	28.00	26	1416	82665	34872824
Mechanical urticaria	29.90	28.00	5	1437	108	34955381
Anaemia	29.87	28.00	42	1400	233293	34722196

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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
Drug interaction	110.29	24.98	104	2890	415079	79326315
Sopor	93.54	24.98	38	2956	32972	79708422
Melaena	65.72	24.98	36	2958	60854	79680540
Intentional self-injury	54.92	24.98	26	2968	32393	79709001
Anaemia	53.39	24.98	74	2920	444941	79296453
Cerebral haemorrhage	51.15	24.98	30	2964	57643	79683751
Hyponatraemic syndrome	48.38	24.98	10	2984	770	79740624
Hyperkalaemia	45.00	24.98	36	2958	114362	79627032
Hyponatraemia	43.99	24.98	43	2951	177805	79563589
Slow speech	41.61	24.98	11	2983	2467	79738927

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B01AC05	BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Platelet aggregation inhibitors excl. heparin
CHEBI has role	CHEBI:48676	fibrin modulating agent
CHEBI has role	CHEBI:50248	hematologic agents
CHEBI has role	CHEBI:50249	anticoagulants
CHEBI has role	CHEBI:50427	platelet aggregation inhibitors
CHEBI has role	CHEBI:68563	ADP receptor subtype P2Y12 antagonists
FDA EPC	N0000175578	Platelet Aggregation Inhibitor
FDA PE	N0000008832	Decreased Platelet Aggregation
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D065689	Cytochrome P-450 CYP2C19 Inhibitors

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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
Percutaneous coronary intervention	indication	415070008
Cerebrovascular Occlusion	indication
Subacute Stent Thrombosis Prevention	indication
Prevention of Cerebral Thrombosis	indication
Obstruction of bile duct	contraindication	30144000
Gastrointestinal ulcer	contraindication	40845000
Hyperlipidemia	contraindication	55822004	DOID:1168
Acute nephropathy	contraindication	58574008
Blood coagulation disorder	contraindication	64779008	DOID:1247
Gastrointestinal hemorrhage	contraindication	74474003

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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	7.18	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
P2Y purinoceptor 12	GPCR	Q9H244	P2Y12_HUMAN	ANTAGONIST			WOMBAT-PK	CHEMBL
Prostaglandin G/H synthase 2	Enzyme	P35354	PGH2_HUMAN		IC50	4.33	WOMBAT-PK
Prostaglandin G/H synthase 1	Enzyme	P23219	PGH1_HUMAN		IC50	4.28	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.85	DRUG MATRIX
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.75	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.86	DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.77	DRUG MATRIX
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	5.20	DRUG MATRIX
Cytochrome P450 2A6	Enzyme	P11509	CP2A6_HUMAN		Ki	6.70	WOMBAT-PK
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	6.18	DRUG MATRIX

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External reference:

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ID	Source
TIC	PDB_CHEM_ID
003610	NDDF
003611	NDDF
10594	RXNORM
108971003	SNOMEDCT_US
2177	MMSL
31069	MMSL
386950000	SNOMEDCT_US
3908	INN_ID
395904008	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ticlopidine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	68151-0079	TABLET, FILM COATED	250 mg	ORAL	ANDA	25 sections

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