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

Stem definition	Drug id	CAS RN
psychoactive	1613	1977-10-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: loxapine loxapin oxilapine loxapine succinate cloxazepine loxitane adasuve loxapine hydrochloride loxapine HCl loxipine maleate	An antipsychotic agent used in SCHIZOPHRENIA. Molecular weight: 327.81 Formula: C18H18ClN3O CLOGP: 3.68 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 28.07 ALOGS: -3.50 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

loxapine
loxapin
oxilapine
loxapine succinate
cloxazepine
loxitane
adasuve
loxapine hydrochloride
loxapine HCl
loxipine maleate

An antipsychotic agent used in SCHIZOPHRENIA.

Molecular weight: 327.81
Formula: C18H18ClN3O
CLOGP: 3.68
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 28.07
ALOGS: -3.50
ROTB: 0

Status: OFP

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

Drug dosage:

Dose	Unit	Route
9.10	mg	Inhal.powder
0.10	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	30 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.02 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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Approvals:

Date	Agency	Company	Orphan
Feb. 25, 1975	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
Poisoning deliberate	434.26	37.30	110	4396	11108	63473408
Coma	398.38	37.30	155	4351	64209	63420307
Neuroleptic malignant syndrome	244.12	37.30	71	4435	11985	63472531
Extrapyramidal disorder	182.23	37.30	58	4448	13226	63471290
Hepatocellular injury	144.68	37.30	59	4447	27322	63457194
Cholestasis	130.58	37.30	56	4450	29378	63455138
Oculogyric crisis	124.38	37.30	28	4478	1693	63482823
Intestinal obstruction	118.29	37.30	53	4453	30846	63453670
Somnolence	117.96	37.30	99	4407	178586	63305930
Altered state of consciousness	102.08	37.30	45	4461	25185	63459331

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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
Coma	387.57	38.28	189	7096	45489	34904157
Antipsychotic drug level below therapeutic	373.07	38.28	90	7195	2457	34947189
Therapeutic product effect variable	360.83	38.28	87	7198	2369	34947277
Disinhibition	356.86	38.28	91	7194	3135	34946511
Akathisia	331.00	38.28	105	7180	8004	34941642
Obsessive-compulsive disorder	329.75	38.28	96	7189	5468	34944178
Euphoric mood	302.14	38.28	90	7195	5551	34944095
Increased appetite	277.73	38.28	90	7195	7339	34942307
Poisoning deliberate	191.19	38.28	69	7216	7775	34941871
Suicide attempt	185.12	38.28	110	7175	39006	34910640

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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
Coma	794.55	33.35	344	10162	100305	79633577
Poisoning deliberate	599.50	33.35	181	10325	18647	79715235
Neuroleptic malignant syndrome	397.95	33.35	146	10360	27413	79706469
Extrapyramidal disorder	315.72	33.35	117	10389	22562	79711320
Hepatocellular injury	265.06	33.35	128	10378	47465	79686417
Somnolence	213.89	33.35	206	10300	238775	79495107
Rhabdomyolysis	191.59	33.35	136	10370	102995	79630887
Intestinal obstruction	187.39	33.35	98	10408	42922	79690960
Hypothermia	186.04	33.35	80	10426	22666	79711216
Miosis	178.43	33.35	70	10436	15719	79718163

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AH01	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Diazepines, oxazepines, thiazepines and oxepines
CHEBI has role	CHEBI:35476	neuroleptics
CHEBI has role	CHEBI:48561	dopaminergic antagonists
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018492	Dopamine Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic 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
Bipolar disorder	indication	13746004	DOID:3312
Schizophrenia	indication	58214004	DOID:5419
Alcoholism	contraindication	7200002
Neuroleptic malignant syndrome	contraindication	15244003	DOID:14464
Senile dementia	contraindication	15662003
Glaucoma	contraindication	23986001	DOID:1686
Disorder of cardiovascular system	contraindication	49601007	DOID:1287
Tardive dyskinesia	contraindication	102449007
Seizure disorder	contraindication	128613002
Hyperprolactinemia	contraindication	237662005	DOID:12700

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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	7.59	Basic
pKa2	3.24	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
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	8.62	CHEMBL	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	7.68	CHEMBL	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.27	PDSP
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.82	PDSP
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.24	PDSP
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.61	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	8	IUPHAR
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	7.82	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.51	PDSP
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.97	PDSP

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External reference:

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ID	Source
001522	NDDF
001523	NDDF
001524	NDDF
1308	MMSL
1346	MMSL
1364415	RXNORM
196711	MMSL
1971003	SNOMEDCT_US
205	IUPHAR_LIGAND_ID
2610	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Adasuve	HUMAN PRESCRIPTION DRUG LABEL	1	51097-001	AEROSOL, POWDER	10 mg	RESPIRATORY (INHALATION)	NDA	31 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1394	CAPSULE	5 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1394	CAPSULE	5 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1395	CAPSULE	10 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1395	CAPSULE	10 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1396	CAPSULE	25 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1396	CAPSULE	25 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1397	CAPSULE	50 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1397	CAPSULE	50 mg	ORAL	ANDA	20 sections
Loxapine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0369	CAPSULE	5 mg	ORAL	ANDA	20 sections

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