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

Stem definition	Drug id	CAS RN
	2749	84-96-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: alimemazine alimemazine tartrate temaril trimeprazine tartrate trimeprazine alimezine methylpromazine teralene	A phenothiazine derivative that is used as an antipruritic. Molecular weight: 298.45 Formula: C18H22N2S CLOGP: 5 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 6.48 ALOGS: -4.55 ROTB: 4 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

alimemazine
alimemazine tartrate
temaril
trimeprazine tartrate
trimeprazine
alimezine
methylpromazine
teralene

A phenothiazine derivative that is used as an antipruritic.

Molecular weight: 298.45
Formula: C18H22N2S
CLOGP: 5
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 6.48
ALOGS: -4.55
ROTB: 4

Status: OFM

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

Drug dosage:

Dose	Unit	Route
30	mg	O
30	mg	P

ADMET properties:

Property	Value	Reference
S (Water solubility)	100 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
None	FDA	ALLERGAN HERBERT

FDA Adverse Event Reporting System (Female)

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 overdose	1352.03	50.01	428	5601	73724	63409269
Intentional self-injury	1281.12	50.01	326	5703	25361	63457632
Coma	545.91	50.01	211	5818	64153	63418840
Poisoning deliberate	463.43	50.01	123	5906	11095	63471898
Somnolence	264.29	50.01	180	5849	178505	63304488
Toxicity to various agents	175.99	50.01	162	5867	247088	63235905
Depressed level of consciousness	167.30	50.01	92	5937	61986	63421007
Suicide attempt	166.15	50.01	91	5938	60827	63422166
Bradypnoea	156.31	50.01	41	5988	3509	63479484
Tachycardia	155.44	50.01	111	5918	118045	63364948
Electrocardiogram QT prolonged	154.30	50.01	86	5943	59444	63423549
Hepatocellular injury	106.58	50.01	52	5977	27329	63455664
Mydriasis	96.65	50.01	38	5991	11918	63471075
Altered state of consciousness	95.45	50.01	47	5982	25183	63457810
Drug abuse	94.92	50.01	68	5961	72450	63410543
Cardio-respiratory arrest	87.24	50.01	60	5969	59899	63423094
Hypothermia	85.24	50.01	36	5993	13545	63469448
Akathisia	84.36	50.01	32	5997	9114	63473879
Suicidal ideation	71.43	50.01	54	5975	62367	63420626
Hypotension	69.85	50.01	106	5923	272498	63210495
Rhabdomyolysis	66.32	50.01	45	5984	43906	63439087
Miosis	65.20	50.01	25	6004	7328	63475665
Cholestasis	64.07	50.01	38	5991	29396	63453597
Pneumonia aspiration	63.43	50.01	40	5989	34500	63448493
Hyperthermia	63.27	50.01	26	6003	9130	63473863
Hypercapnic coma	59.06	50.01	11	6018	188	63482805
Bladder dilatation	58.17	50.01	14	6015	843	63482150
Asphyxia	54.75	50.01	21	6008	6160	63476833
Drug dependence	54.30	50.01	32	5997	24451	63458542
Extrapyramidal disorder	50.97	50.01	25	6004	13259	63469734

FDA Adverse Event Reporting System (Male)

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
Coma	786.35	37.85	267	3897	45411	34907356
Poisoning deliberate	295.66	37.85	84	4080	7760	34945007
Intentional overdose	244.57	37.85	114	4050	43560	34909207
Intentional self-injury	241.19	37.85	82	4082	13689	34939078
Drug abuse	169.17	37.85	119	4045	98977	34853790
Toxicity to various agents	142.27	37.85	145	4019	200217	34752550
Somnolence	102.33	37.85	93	4071	111023	34841744
Miosis	93.18	37.85	37	4127	9498	34943269
Electrocardiogram QT prolonged	83.42	37.85	55	4109	40897	34911870
Poisoning	68.44	37.85	32	4132	12194	34940573
Pneumonia aspiration	61.36	37.85	46	4118	41857	34910910
Extrapyramidal disorder	60.83	37.85	30	4134	12850	34939917
Hepatocellular injury	58.16	37.85	35	4129	22176	34930591
Suicide attempt	57.40	37.85	43	4121	39073	34913694
Tachycardia	48.57	37.85	55	4109	84717	34868050
Depressed level of consciousness	47.61	37.85	40	4124	42801	34909966
Pulmonary oedema	44.01	37.85	40	4124	47489	34905278
Rhabdomyolysis	43.83	37.85	47	4117	68116	34884651
Altered state of consciousness	42.37	37.85	29	4135	22864	34929903

FDA Adverse Event Reporting System (Geriatric)

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
Coma	1281.96	39.41	470	8940	100179	79634799
Intentional overdose	930.26	39.41	378	9032	105582	79629396
Intentional self-injury	861.30	39.41	264	9146	32155	79702823
Poisoning deliberate	768.11	39.41	214	9196	18614	79716364
Somnolence	362.19	39.41	266	9144	238715	79496263
Toxicity to various agents	290.37	39.41	299	9111	421241	79313737
Drug abuse	232.25	39.41	175	9235	162516	79572462
Electrocardiogram QT prolonged	226.84	39.41	138	9272	90248	79644730
Suicide attempt	191.22	39.41	120	9290	82812	79652166
Tachycardia	164.97	39.41	149	9261	177619	79557359
Hepatocellular injury	157.37	39.41	87	9323	47506	79687472
Miosis	157.36	39.41	62	9348	15727	79719251
Bradypnoea	150.61	39.41	47	9363	6005	79728973
Altered state of consciousness	133.70	39.41	76	9334	43746	79691232
Depressed level of consciousness	133.32	39.41	102	9308	96550	79638428
Pneumonia aspiration	127.53	39.41	86	9324	66881	79668097
Extrapyramidal disorder	117.12	39.41	56	9354	22623	79712355
Mydriasis	114.34	39.41	51	9359	17592	79717386
Hypothermia	110.91	39.41	54	9356	22692	79712286
Cardio-respiratory arrest	106.55	39.41	94	9316	108416	79626562
Rhabdomyolysis	104.59	39.41	91	9319	103040	79631938
Poisoning	94.07	39.41	50	9360	25222	79709756
Asphyxia	82.78	39.41	36	9374	11684	79723294
Akathisia	81.67	39.41	37	9373	13222	79721756
Bladder dilatation	76.77	39.41	22	9388	2097	79732881
Suicidal ideation	68.70	39.41	63	9347	76277	79658701
Hypotension	63.66	39.41	152	9258	440165	79294813
Faecaloma	61.04	39.41	29	9381	11535	79723443
Drug dependence	60.51	39.41	45	9365	40724	79694254
Hypercapnic coma	59.34	39.41	13	9397	411	79734567
Cholestasis	52.80	39.41	46	9364	52063	79682915
Thymus disorder	52.28	39.41	11	9399	286	79734692
Pain	52.17	39.41	10	9400	703792	79031186
Drug ineffective	51.79	39.41	32	9378	1080881	78654097
Hyperthermia	51.54	39.41	30	9380	18007	79716971
Regurgitation	50.41	39.41	17	9393	2770	79732208
Serotonin syndrome	50.22	39.41	42	9368	44985	79689993
Arthralgia	47.16	39.41	6	9404	571797	79163181
Sinus tachycardia	46.58	39.41	37	9373	36871	79698107
Intentional product misuse	43.71	39.41	55	9355	95110	79639868
Overdose	43.57	39.41	78	9332	184128	79550850
Drug interaction	42.33	39.41	126	9284	415057	79319921
Haemodynamic instability	42.11	39.41	26	9384	17356	79717622
Morbid thoughts	41.41	39.41	11	9399	791	79734187
Neuroleptic malignant syndrome	39.95	39.41	30	9380	27529	79707449
Pyramidal tract syndrome	39.63	39.41	10	9400	587	79734391

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R06AD01	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Phenothiazine derivatives
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents

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

Disease	Relation	SNOMED_ID	DOID
Dermatographic urticaria	indication	7632005	DOID:743
Angioedema	indication	41291007	DOID:1558
General anesthesia	indication	50697003
Allergic rhinitis	indication	61582004
Nasal discharge	indication	64531003
Nasal congestion	indication	68235000
Sneezing	indication	76067001
Urticaria	indication	126485001
Itching of skin	indication	418363000
Allergic conjunctivitis	indication	473460002	DOID:11204
Alcoholism	contraindication	7200002
Organophosphate poisoning	contraindication	8260003
Weight gain finding	contraindication	8943002
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003
Chronic disease of respiratory system	contraindication	17097001
Myocardial infarction	contraindication	22298006	DOID:5844
Glaucoma	contraindication	23986001	DOID:1686
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Parkinsonism	contraindication	32798002
Conduction disorder of the heart	contraindication	44808001
Chronic heart failure	contraindication	48447003
Bradycardia	contraindication	48867003
Extrapyramidal disease	contraindication	76349003
Hyperglycemia	contraindication	80394007	DOID:4195
Epilepsy	contraindication	84757009	DOID:1826
Leukopenia	contraindication	84828003	DOID:615
Stupor	contraindication	89458003
Tardive dyskinesia	contraindication	102449007
Prolonged QT interval	contraindication	111975006
Acute disease of cardiovascular system	contraindication	128487001
Angina pectoris	contraindication	194828000
Disease of liver	contraindication	235856003	DOID:409
Metabolic syndrome X	contraindication	237602007	DOID:14221
Hyperprolactinemia	contraindication	237662005	DOID:12700
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Anemia	contraindication	271737000	DOID:2355
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Coma	contraindication	371632003
At risk for aspiration	contraindication	371736008
Visual impairment	contraindication	397540003
Breastfeeding (mother)	contraindication	413712001
Myocardial ischemia	contraindication	414795007	DOID:3393
Obesity	contraindication	414916001	DOID:9970
Congenital long QT syndrome	contraindication	442917000
Carcinoma of female breast	contraindication	447782002

🐶 Veterinary Drug Use

Species	Use	Relation
Dogs	Itching	Indication
Dogs	Inflammation	Indication
Dogs	Adjunctive therapy in various cough conditions	Indication
Dogs	Acute or chronic bacterial infections provided the infection is controlled by appropriate antibiotic or chemotherapeutic agents	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Temaril-P Tablets	Zoetis Inc.	2
Temaril-P Spansule Capsule No. 1, Temaril-P Spansule Capsule No. 2	Zoetis Inc.	2

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.92	Basic
pKa2	3.55	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST				CHEMBL	CHEMBL
FAD-linked sulfhydryl oxidase ALR	Enzyme	P55789	ALR_HUMAN		AC50	5.90		CHEMBL

External reference:

ID	Source
4019960	VUID
N0000148045	NUI
D02245	KEGG_DRUG
4330-99-8	SECONDARY_CAS_RN
4018016	VANDF
4019960	VANDF
C0041031	UMLSCUI
CHEBI:9725	CHEBI
CHEMBL829	ChEMBL_ID
5574	PUBCHEM_CID
DB01246	DRUGBANK_ID
CHEMBL3989885	ChEMBL_ID
CHEMBL1713082	ChEMBL_ID
C031242	MESH_SUPPLEMENTAL_RECORD_UI
7237	IUPHAR_LIGAND_ID
10825	RXNORM
2318	MMSL
5629	MMSL
d00788	MMSL
001535	NDDF
001536	NDDF
387471006	SNOMEDCT_US
52803004	SNOMEDCT_US
8109005	SNOMEDCT_US
D014291	MESH_DESCRIPTOR_UI
706	INN_ID
362NW1LD6Z	UNII

Pharmaceutical products:

None