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

Stem definition	Drug id	CAS RN
	2717	19794-93-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: trazodone trazodon trazodone hydrochloride trazodone HCl	A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309) Molecular weight: 371.87 Formula: C19H22ClN5O CLOGP: 3.65 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 42.39 ALOGS: -3.11 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

trazodone
trazodon
trazodone hydrochloride
trazodone HCl

A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309)

Molecular weight: 371.87
Formula: C19H22ClN5O
CLOGP: 3.65
LIPINSKI: 0
HAC: 6
HDO: 0
TPSA: 42.39
ALOGS: -3.11
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.30	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	81 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	7.30 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	23.05 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	1.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.52 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 24, 1981	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
Completed suicide	1256.40	10.08	1465	119419	144208	63223930
Drug abuse	549.82	10.08	684	120200	71834	63296304
Sopor	500.02	10.08	381	120503	21783	63346355
Toxicity to various agents	440.04	10.08	1246	119638	246004	63122134
Serotonin syndrome	377.69	10.08	362	120522	28320	63339818
Pemphigus	328.43	10.08	4	120880	183722	63184416
Polycystic ovaries	294.71	10.08	152	120732	4319	63363819
Hand deformity	270.58	10.08	7	120877	159450	63208688
Systemic lupus erythematosus	248.78	10.08	48	120836	208870	63159268
Sensitisation	243.23	10.08	122	120762	3264	63364874

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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	580.72	11.26	708	49325	97460	34809438
Serotonin syndrome	470.87	11.26	315	49718	19618	34887280
Priapism	401.71	11.26	178	49855	4816	34902082
Toxicity to various agents	389.10	11.26	873	49160	199489	34707409
Drug abuse	306.72	11.26	526	49507	98570	34808328
Sopor	277.42	11.26	188	49845	11948	34894950
Intentional overdose	147.05	11.26	241	49792	43433	34863465
Suicidal ideation	137.50	11.26	224	49809	40164	34866734
Suicide attempt	117.28	11.26	205	49828	38911	34867987
Overdose	114.87	11.26	338	49695	90721	34816177

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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	1691.93	10.15	2159	143412	243608	79355209
Serotonin syndrome	785.72	10.15	654	144917	44373	79554444
Toxicity to various agents	766.76	10.15	2083	143488	419457	79179360
Sopor	753.99	10.15	562	145009	32448	79566369
Drug abuse	735.14	10.15	1171	144400	161520	79437297
Priapism	386.88	10.15	181	145390	4324	79594493
Suicide attempt	307.60	10.15	547	145024	82385	79516432
Polycystic ovaries	291.42	10.15	141	145430	3638	79595179
Cardio-respiratory arrest	228.91	10.15	568	145003	107942	79490875
Sensitisation	218.14	10.15	111	145460	3200	79595617

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N06AX05	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:37887	adrenergic blockers
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:50949	SSRI
FDA EPC	N0000175696	Serotonin Reuptake Inhibitor
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D000928	Antidepressive Agents

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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
Major depressive disorder	indication	370143000
Insomnia	off-label use	193462001
Priapism	contraindication	6273006	DOID:9286
Suicidal thoughts	contraindication	6471006
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Hypokalemia	contraindication	43339004
Syndrome of inappropriate vasopressin secretion	contraindication	55004003	DOID:3401
Heart disease	contraindication	56265001	DOID:114
Blood coagulation disorder	contraindication	64779008	DOID:1247

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.98	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
150MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	OLEPTRO	ANGELINI PHARMA	N022411	Feb. 2, 2010	DISCN	TABLET, EXTENDED RELEASE	ORAL	7829120	March 27, 2027	METHOD OF TREATING DEPRESSION
300MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	OLEPTRO	ANGELINI PHARMA	N022411	Feb. 2, 2010	DISCN	TABLET, EXTENDED RELEASE	ORAL	7829120	March 27, 2027	METHOD OF TREATING DEPRESSION

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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
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Kd	6.80	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	6.65	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	7.35	WOMBAT-PK	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.03	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.54	WOMBAT-PK
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Kd	5.07	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.02	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.08	WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	5.75	PDSP
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		IC50	9.55	WOMBAT-PK

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External reference:

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ID	Source
001511	NDDF
004610	NDDF
10737	RXNORM
1504	MMSL
213	IUPHAR_LIGAND_ID
25332-39-2	SECONDARY_CAS_RN
2878	INN_ID
372829000	SNOMEDCT_US
4018812	VANDF
4019954	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0555-0711	TABLET	300 mg	ORAL	ANDA	26 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0555-0711	TABLET	300 mg	ORAL	ANDA	26 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0555-0733	TABLET	300 mg	ORAL	ANDA	26 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-2578	TABLET	50 mg	ORAL	ANDA	31 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-2579	TABLET	100 mg	ORAL	ANDA	31 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8339	TABLET	150 mg	ORAL	ANDA	30 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8339	TABLET	150 mg	ORAL	ANDA	30 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8371	TABLET	50 mg	ORAL	ANDA	30 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8371	TABLET	50 mg	ORAL	ANDA	30 sections
Trazodone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8386	TABLET	100 mg	ORAL	ANDA	30 sections

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