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

Stem definition	Drug id	CAS RN
diazepam derivatives	136	28981-97-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: xanax alprazolam alprozolam alzolam	A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238) Molecular weight: 308.77 Formula: C17H13ClN4 CLOGP: 2.56 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 43.07 ALOGS: -3.98 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

xanax
alprazolam
alprozolam
alzolam

A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238)

Molecular weight: 308.77
Formula: C17H13ClN4
CLOGP: 2.56
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 43.07
ALOGS: -3.98
ROTB: 1

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	88 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	20 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	12 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.80 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.74 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.46 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.29 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.07 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Oct. 16, 1981	FDA	PHARMACIA AND UPJOHN

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 abuse	5867.10	9.71	3586	241084	68932	63175420
Completed suicide	4349.58	9.71	3954	240716	141719	63102633
Sopor	2268.01	9.71	1278	243392	20886	63223466
Toxicity to various agents	2023.89	9.71	3503	241167	243747	63000605
Respiratory arrest	1367.50	9.71	1079	243591	31566	63212786
Suicide attempt	1248.85	9.71	1350	243320	59568	63184784
Poisoning	1157.73	9.71	698	243972	13002	63231350
Intentional overdose	1116.19	9.71	1402	243268	72750	63171602
Cardio-respiratory arrest	975.34	9.71	1179	243491	58780	63185572
Poisoning deliberate	895.15	9.71	551	244119	10667	63233685

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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 abuse	7661.01	10.68	4464	109410	94632	34748425
Toxicity to various agents	2307.32	10.68	3035	110839	197327	34645730
Completed suicide	2187.99	10.68	2101	111773	96067	34746990
Respiratory arrest	1833.64	10.68	1140	112734	26903	34816154
Poisoning	1458.49	10.68	738	113136	11488	34831569
Cardio-respiratory arrest	1087.32	10.68	1107	112767	54166	34788891
Cardiac arrest	863.33	10.68	1297	112577	94862	34748195
Intentional product misuse	781.49	10.68	849	113025	44762	34798295
Drug dependence	771.69	10.68	636	113238	23581	34819476
Sopor	719.03	10.68	464	113410	11672	34831385

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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 abuse	12826.30	9.57	7743	283203	154948	79298494
Completed suicide	6685.09	9.57	6175	284771	239592	79213850
Toxicity to various agents	4258.26	9.57	6368	284578	415172	79038270
Respiratory arrest	3471.11	9.57	2320	288626	55230	79398212
Sopor	2895.94	9.57	1689	289257	31321	79422121
Poisoning	2544.41	9.57	1415	289531	23857	79429585
Cardio-respiratory arrest	2159.63	9.57	2306	288640	106204	79347238
Cardiac arrest	1888.32	9.57	2710	288236	169386	79284056
Suicide attempt	1666.36	9.57	1772	289174	81160	79372282
Intentional overdose	1604.44	9.57	1955	288991	104005	79349437

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05BA12	NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Benzodiazepine derivatives
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:51371	muscle relaxants
CHEBI has role	CHEBI:51373	gamma-aminobutyric acid receptor agonist
FDA CS	M0002356	Benzodiazepines
FDA EPC	N0000175694	Benzodiazepine
MeSH PA	D014151	Anti-Anxiety 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
Generalized anxiety disorder	indication	21897009	DOID:14320
Anxiety	indication	48694002
Mixed anxiety and depressive disorder	indication	231504006
Panic disorder	indication	371631005	DOID:594
Insomnia	off-label use	193462001
Suicidal thoughts	contraindication	6471006
Asthenia	contraindication	13791008
Alcohol intoxication	contraindication	25702006
Depressive disorder	contraindication	35489007
Substance abuse	contraindication	66214007

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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	6.15	Basic
pKa2	4.9	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
GABA-A receptor alpha-5/beta-3/gamma-2	Ion channel	P18507 P28472 P31644	GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	8	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	7.43	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRG2_HUMAN GBRB3_HUMAN GBRA2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	7.92	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRG2_HUMAN GBRB3_HUMAN GBRA3_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	7.16	WOMBAT-PK	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		Ki	3.85	WOMBAT-PK
Platelet-activating factor receptor	GPCR	P25105	PTAFR_HUMAN		Ki	5.46	PDSP
Bromodomain-containing protein 4	Unclassified	O60885	BRD4_HUMAN		Kd	5.61	CHEMBL
Cholecystokinin receptor type A	GPCR		CCKAR_RAT		IC50	4.19	CHEMBL

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External reference:

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ID	Source
08H	PDB_CHEM_ID
001464	NDDF
111127002	SNOMEDCT_US
1327	MMSL
1885	MMSL
202363	RXNORM
2118	PUBCHEM_CID
3426	INN_ID
386983007	SNOMEDCT_US
4018074	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0054-3068	SOLUTION, CONCENTRATE	1 mg	ORAL	ANDA	34 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0054-3068	SOLUTION, CONCENTRATE	1 mg	ORAL	ANDA	34 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2027	TABLET	0.25 mg	ORAL	ANDA	29 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2027	TABLET	0.25 mg	ORAL	ANDA	29 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2027	TABLET	0.25 mg	ORAL	ANDA	29 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2029	TABLET	0.50 mg	ORAL	ANDA	29 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2029	TABLET	0.50 mg	ORAL	ANDA	29 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2029	TABLET	0.50 mg	ORAL	ANDA	29 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2031	TABLET	1 mg	ORAL	ANDA	29 sections
Alprazolam	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2031	TABLET	1 mg	ORAL	ANDA	29 sections

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