pentobarbital

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Dose	Unit	Route
0.10	g	O
0.10	g	P
0.10	g	R

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	12.61 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	80 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.91 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.47 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.39 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	22 hours	Lombardo F, Berellini G, Obach RS

Property	Description	Value
kinase-safety-class	ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PIK3CD,PRKDC,TEK	20
kinase-selectivity-class	GRK2,TEK	2
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

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
Propofol infusion syndrome	212.85	103.09	33	1283	1306	90625825
Mitochondrial DNA mutation	189.32	103.09	26	1290	432	90626699
Drug ineffective for unapproved indication	185.78	103.09	59	1257	66585	90560546
Gene mutation	149.38	103.09	26	1290	2104	90625027
Multiple-drug resistance	143.55	103.09	31	1285	7745	90619386
Blood gases abnormal	141.12	103.09	22	1294	899	90626232
CSF oligoclonal band present	140.64	103.09	20	1296	431	90626700
Status epilepticus	140.37	103.09	36	1280	18838	90608293
Pleocytosis	124.57	103.09	20	1296	988	90626143

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 ineffective for unapproved indication	278.14	86.66	91	1678	102747	110484783
Propofol infusion syndrome	208.05	86.66	36	1733	2553	110584977
Mitochondrial DNA mutation	185.73	86.66	26	1743	450	110587080
Multiple-drug resistance	149.48	86.66	36	1733	13199	110574331
Status epilepticus	144.67	86.66	42	1727	31529	110556001
CSF oligoclonal band present	137.76	86.66	20	1749	452	110587078
Gene mutation	134.44	86.66	26	1743	3403	110584127
Blood gases abnormal	130.41	86.66	22	1747	1336	110586194
Drug ineffective	129.66	86.66	138	1631	1520402	109067128
Pleocytosis	111.87	86.66	20	1749	1704	110585826
Off label use	106.57	86.66	124	1645	1500061	109087469
Toxicity to various agents	100.23	86.66	73	1696	480482	110107048

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pentobarbital 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products:

Source	Code	Description
ATC	N05CA01	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Barbiturates, plain
MeSH PA	D000759	Adjuvants, Anesthesia
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D006993	Hypnotics and Sedatives
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018682	GABA Agents
MeSH PA	D018757	GABA Modulators
CHEBI has role	CHEBI:35554	cardiovascular drug
CHEBI has role	CHEBI:63726	neuroprotective agent
CHEBI has role	CHEBI:91016	GABA<small><sub>A</sub></small> receptor agonist

Disease	Relation	SNOMED_ID	DOID
General anesthesia	indication	50697003
Severe anxiety (panic)	indication	80583007
Epilepsy	indication	84757009	DOID:1826
Seizure disorder	indication	128613002
Insomnia	indication	193462001
Status epilepticus	indication	230456007	DOID:1824
Cerebral ischemia	indication	287731003
Local anesthesia	indication	386761002
Tetanus Adjunct Treatment	indication
Benign intracranial hypertension	off-label use	68267002	DOID:11459
Apnea	contraindication	1023001
Suicidal thoughts	contraindication	6471006
Alcoholism	contraindication	7200002
Hyperammonemia	contraindication	9360008
Chronic obstructive lung disease	contraindication	13645005	DOID:3083
Hepatic encephalopathy	contraindication	13920009	DOID:13413
Disorder of lung	contraindication	19829001	DOID:850
Depressive disorder	contraindication	35489007
Hypertensive disorder	contraindication	38341003	DOID:10763
Hyperactive behavior	contraindication	44548000
Low blood pressure	contraindication	45007003
Heart disease	contraindication	56265001	DOID:114
Hepatic failure	contraindication	59927004
Substance abuse	contraindication	66214007
Hepatic coma	contraindication	72836002	DOID:12550
Sleep apnea	contraindication	73430006	DOID:0050847
Decreased respiratory function	contraindication	80954004
Kidney disease	contraindication	90708001	DOID:557
Pneumonia	contraindication	233604007	DOID:552
Disease of liver	contraindication	235856003	DOID:409
Sleep automatism	contraindication	247962006
Anemia	contraindication	271737000	DOID:2355
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Respiratory insufficiency	contraindication	409623005
Porphyria	contraindication	418470004
Acute exacerbation of asthma	contraindication	708038006

Species	Use	Relation
Cats	General anesthesia	Indication
Dogs	General anesthesia	Indication
Dogs	Strychnine poisoning	Indication
Dogs	Euthanasia	Indication
Horses	General anesthesia	Indication
Horses	Sedative-relaxant	Indication

Product	Applicant	Ingredients
Somnopentyl Injection	Intervet Inc.	1
Combuthal Powder	Bimeda Animal Health Limited	2
Chloropent	Zoetis Inc.	3
Beuthanasia-D Special	Intervet Inc.	2
Euthasol	Virbac AH Inc.	2
Euthanasia-III Solution	Med-Pharmex Inc.	2
Pentobarbital Sodium and Phenytoin Sodium	Akorn Animal Health Inc.	2

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Gamma-aminobutyric acid receptor subunit beta-3	Ion channel	P28472	GBRB3_HUMAN	POSITIVE ALLOSTERIC MODULATOR	IC50	4.06	CHEMBL	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	4.30	WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	2.55	WOMBAT-PK
GABA A receptor alpha-2/beta-2/gamma-2	Ion channel	P18507 P47869 P47870	GBRG2_HUMAN GBRA2_HUMAN GBRB2_HUMAN		EC50	4.30	CHEMBL
GABA-A receptor; anion channel	Ion channel		GBRP_RAT GBRB1_RAT GBRD_RAT GBRG2_RAT GBRA5_RAT GBRA3_RAT GBRG1_RAT GBRA2_RAT GBRA4_RAT GBRG3_RAT GBRA6_RAT GBRA1_RAT GBRB3_RAT GBRB2_RAT Q91ZM7_RAT GBRE_RAT		IC50	5.77	CHEMBL

ID	Source
4018516	VUID
N0000146838	NUI
D00499	KEGG_DRUG
24876-35-5	SECONDARY_CAS_RN
57-33-0	SECONDARY_CAS_RN
4018036	VANDF
4018516	VANDF
C0030883	UMLSCUI
CHEBI:7983	CHEBI
RAV	PDB_CHEM_ID
CHEMBL448	ChEMBL_ID
DB00312	DRUGBANK_ID
CHEMBL971	ChEMBL_ID
D010424	MESH_DESCRIPTOR_UI
4737	PUBCHEM_CID
703	INN_ID
I4744080IR	UNII
203085	RXNORM
2161	MMSL
3697	MMSL
5253	MMSL
5254	MMSL
71886	MMSL
d00335	MMSL
001411	NDDF
001412	NDDF
33231001	SNOMEDCT_US
372703009	SNOMEDCT_US
66843009	SNOMEDCT_US
5480	IUPHAR_LIGAND_ID

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Pentobarbital Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	17478-181	INJECTION	50 mg	INTRAMUSCULAR	ANDA	25 sections
Pentobarbital Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	24201-010	INJECTION, SOLUTION	50 mg	INTRAMUSCULAR	ANDA	24 sections
pentobarbital sodium	HUMAN PRESCRIPTION DRUG LABEL	1	25021-676	INJECTION, SOLUTION	50 mg	INTRAVENOUS	ANDA	26 sections
Nembutal Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	76478-501	INJECTION	50 mg	INTRAVENOUS	ANDA	25 sections

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.81	acidic
pKa2	9.51	acidic