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

Stem definition	Drug id	CAS RN
	2286	60-87-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: promethazine diphergan proazamine prometazin protazine promethazine hydrochloride promethazine HCl	A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals. Molecular weight: 284.42 Formula: C17H20N2S CLOGP: 4.60 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 6.48 ALOGS: -4.07 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

promethazine
diphergan
proazamine
prometazin
protazine
promethazine hydrochloride
promethazine HCl

A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.

Molecular weight: 284.42
Formula: C17H20N2S
CLOGP: 4.60
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 6.48
ALOGS: -4.07
ROTB: 3

Status: OFP

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

Drug dosage:

Dose	Unit	Route
25	mg	O
25	mg	P
25	mg	R

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	5.03 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	25 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	14 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	14 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	14 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	100 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.09 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
March 29, 1951	FDA	DELCOR ASSET CORP

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
Intentional self-injury	6783.21	10.44	2029	65012	23658	63398323
Intentional overdose	5402.75	10.44	2245	64796	71907	63350074
Akathisia	541.15	10.44	240	66801	8906	63413075
Tachycardia	465.60	10.44	598	66443	117558	63304423
Depressed level of consciousness	384.41	10.44	397	66644	61681	63360300
Cholecystitis chronic	310.24	10.44	171	66870	10190	63411791
Drug ineffective	281.14	10.44	420	66621	1044345	62377636
Mydriasis	279.64	10.44	168	66873	11788	63410193
Contraindicated product administered	210.00	10.44	4	67037	217644	63204337
Anxiety	198.18	10.44	591	66450	216950	63205031

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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
Intentional self-injury	2129.99	12.14	662	24800	13109	34918360
Intentional overdose	1659.05	12.14	749	24713	42925	34888544
Akathisia	163.92	12.14	91	25371	8018	34923451
Depressed level of consciousness	116.99	12.14	150	25312	42691	34888778
Respiratory arrest	90.77	12.14	107	25355	27936	34903533
Tachycardia	89.04	12.14	193	25269	84579	34846890
Sinus tachycardia	71.24	12.14	75	25387	17285	34914184
Drug ineffective	67.14	12.14	146	25316	456605	34474864
Off label use	64.22	12.14	131	25331	419393	34512076
Somnolence	62.15	12.14	200	25262	110916	34820553

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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
Intentional self-injury	5502.25	10.31	1743	67326	30676	79644643
Intentional overdose	4203.96	10.31	1975	67094	103985	79571334
Akathisia	575.58	10.31	264	68805	12995	79662324
Tachycardia	377.00	10.31	604	68465	177164	79498155
Depressed level of consciousness	343.55	10.31	421	68648	96231	79579088
Cholecystitis chronic	287.91	10.31	150	68919	9756	79665563
Mydriasis	226.51	10.31	158	68911	17485	79657834
Drug ineffective	206.87	10.31	390	68679	1080523	78594796
Anxiety	174.56	10.31	542	68527	247970	79427349
Poisoning	174.35	10.31	157	68912	25115	79650204

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FDA Adverse Event Reporting System (Pediatric)

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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
Pleural effusion	47.43	26.23	11	217	11	89553
Pulmonary haemorrhage neonatal	43.10	26.23	10	218	10	89554
Congenital tricuspid valve incompetence	32.89	26.23	10	218	46	89518

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Pharmacologic Action:

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Source	Code	Description
ATC	D04AA10	DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Antihistamines for topical use
ATC	R06AD02	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Phenothiazine derivatives
ATC	R06AD52	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Phenothiazine derivatives
ATC	V03AB05	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:36333	local anesthetics
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:50857	anti-allergic drugs
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:59683	antipruritic drugs

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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
Vasomotor rhinitis	indication	8229003	DOID:4730
Nausea and vomiting	indication	16932000
General anesthesia	indication	50697003
Sedation	indication	72641008
Urticaria	indication	126485001
Seasonal allergic rhinitis	indication	367498001
Allergic conjunctivitis	indication	473460002	DOID:11204

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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	9.19	Basic
pKa2	3.55	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
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	9.62	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	6.61	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.59	DRUG MATRIX
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.92	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		IC50	5.12	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.38	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.83	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.77	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.37	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	8.19	DRUG MATRIX

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External reference:

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ID	Source
001483	NDDF
004459	NDDF
142445	RXNORM
14905007	SNOMEDCT_US
2141	MMSL
372871004	SNOMEDCT_US
4017846	VANDF
4019910	VUID
4019910	VANDF
4927	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Promethazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0927	SOLUTION	6.25 mg	ORAL	ANDA	25 sections
Promethazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0927	SOLUTION	6.25 mg	ORAL	ANDA	25 sections
PROMETHAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9940	INJECTION	25 mg	INTRAMUSCULAR	ANDA	12 sections
PROMETHAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9940	INJECTION	25 mg	INTRAMUSCULAR	ANDA	12 sections
PROMETHAZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9940	INJECTION	25 mg	INTRAMUSCULAR	ANDA	12 sections
Promethazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9941	INJECTION	25 mg	INTRAMUSCULAR	ANDA	12 sections
Promethazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9941	INJECTION	25 mg	INTRAMUSCULAR	ANDA	12 sections
Promethazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9941	INJECTION	25 mg	INTRAMUSCULAR	ANDA	12 sections
Promethazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9942	INJECTION	50 mg	INTRAMUSCULAR	ANDA	12 sections
Promethazine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9942	INJECTION	50 mg	INTRAMUSCULAR	ANDA	12 sections

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