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

Stem definition	Drug id	CAS RN
neuromuscular blocking agents with rigid structure	259	64228-79-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: atracurium tracrium atracurium besylate	A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents. Molecular weight: 929.16 Formula: C53H72N2O12 CLOGP: 3.30 LIPINSKI: 2 HAC: 14 HDO: 0 TPSA: 126.44 ALOGS: -7.63 ROTB: 26 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

atracurium
tracrium
atracurium besylate

A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

Molecular weight: 929.16
Formula: C53H72N2O12
CLOGP: 3.30
LIPINSKI: 2
HAC: 14
HDO: 0
TPSA: 126.44
ALOGS: -7.63
ROTB: 26

Status: OFP

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

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	0	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	8.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.65 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	0.10 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.52 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.31 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Nov. 23, 1983	FDA

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
Anaphylactic shock	652.75	45.94	157	2363	23476	63463026
Anaphylactic reaction	340.29	45.94	119	2401	65981	63420521
Bronchospasm	191.83	45.94	56	2464	17224	63469278
Hypotension	169.82	45.94	115	2405	272489	63214013
Cardiac arrest	100.78	45.94	56	2464	92489	63394013
Patent ductus arteriosus	61.64	45.94	17	2503	4233	63482269
Pulseless electrical activity	56.15	45.94	18	2502	7503	63478999
Tachycardia	55.04	45.94	42	2478	118114	63368388
Circulatory collapse	53.27	45.94	23	2497	21915	63464587
Stress cardiomyopathy	52.11	45.94	18	2502	9432	63477070
Acute respiratory distress syndrome	51.72	45.94	23	2497	23511	63462991
Wrong product administered	51.24	45.94	16	2504	6125	63480377
Anticholinergic syndrome	51.14	45.94	13	2507	2369	63484133

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
Anaphylactic shock	407.74	45.75	109	2051	15832	34938939
Anaphylactic reaction	153.87	45.75	62	2098	32239	34922532
Bronchospasm	150.16	45.75	46	2114	10685	34944086
Leukocytosis	74.14	45.75	34	2126	24031	34930740
Rash maculo-papular	68.71	45.75	34	2126	28417	34926354
Eosinophilia	68.31	45.75	33	2127	26189	34928582
Hepatic cytolysis	66.02	45.75	27	2133	14469	34940302
Hypotension	61.99	45.75	72	2088	221577	34733194
Trigemino-cardiac reflex	50.67	45.75	9	2151	184	34954587
Erythema	49.29	45.75	42	2118	88738	34866033
Cardiac arrest	46.38	45.75	42	2118	96117	34858654

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
Anaphylactic shock	1008.46	37.92	260	4285	35736	79704107
Anaphylactic reaction	474.27	37.92	178	4367	83565	79656278
Bronchospasm	323.90	37.92	99	4446	24760	79715083
Hypotension	204.44	37.92	181	4364	440136	79299707
Cardiac arrest	126.77	37.92	93	4452	172003	79567840
Circulatory collapse	94.27	37.92	45	4500	37623	79702220
Eosinophilia	89.23	37.92	46	4499	45299	79694544
Tachycardia	77.78	37.92	71	4474	177697	79562146
Stress cardiomyopathy	71.17	37.92	26	4519	11140	79728703
Rash maculo-papular	69.54	37.92	42	4503	56036	79683807
Bradycardia	66.93	37.92	58	4487	135499	79604344
Shock	65.58	37.92	37	4508	43511	79696332
Trigemino-cardiac reflex	61.36	37.92	11	4534	258	79739585
Hepatic cytolysis	60.57	37.92	30	4515	27121	79712722
Leukocytosis	60.29	37.92	35	4510	43420	79696423
Acute respiratory distress syndrome	52.04	37.92	32	4513	44035	79695808
Pulseless electrical activity	51.58	37.92	22	4523	14138	79725705
Wrong product administered	46.57	37.92	18	4527	8994	79730849
Allergy test negative	46.46	37.92	9	4536	325	79739518
Erythema	46.01	37.92	60	4485	223230	79516613
Airway complication of anaesthesia	44.40	37.92	9	4536	411	79739432
Type I hypersensitivity	42.59	37.92	14	4531	4384	79735459
Fatigue	41.65	37.92	3	4542	929724	78810119
Anticholinergic syndrome	41.12	37.92	13	4532	3598	79736245
Anaesthetic complication	39.77	37.92	12	4533	2847	79736996
Procedural hypotension	39.27	37.92	11	4534	2012	79737831
Anaphylactoid shock	38.84	37.92	9	4536	772	79739071
Oxygen saturation decreased	38.66	37.92	42	4503	129005	79610838
Haemodynamic instability	38.15	37.92	19	4526	17363	79722480

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	M03AC04	MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS Other quaternary ammonium compounds
CHEBI has role	CHEBI:48878	nicotinic antagonists
CHEBI has role	CHEBI:51371	muscle relaxants
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D018680	Cholinergic Antagonists
MeSH PA	D009465	Neuromuscular Agents
MeSH PA	D009466	Neuromuscular Blocking Agents
MeSH PA	D003473	Neuromuscular Nondepolarizing Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018733	Nicotinic Antagonists
MeSH PA	D018373	Peripheral Nervous System Agents
FDA EPC	N0000175720	Nondepolarizing Neuromuscular Blocker
FDA PE	N0000175732	Neuromuscular Nondepolarizing Blockade

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

Disease	Relation	SNOMED_ID	DOID
Muscle relaxation, function	indication	11977004
General anesthesia	indication	50697003
Skeletal Muscle Relaxation for Endotracheal Intubation	indication
Hypocalcemia	contraindication	5291005
Disorder of lung	contraindication	19829001	DOID:850
Hypokalemia	contraindication	43339004
Low blood pressure	contraindication	45007003
Eaton-Lambert syndrome	contraindication	56989000	DOID:0050214
Hypermagnesemia	contraindication	66978005
Myasthenia gravis	contraindication	91637004	DOID:437
Disorder of electrolytes	contraindication	237840007
Hypothermia	contraindication	386689009
Malignant hyperthermia	contraindication	405501007

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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])	Bioact source	MoA source
Acetylcholine receptor	Ion channel	P02708 P11230 Q07001	ACHA_HUMAN ACHB_HUMAN ACHD_HUMAN	ANTAGONIST	IC50	7.77	WOMBAT-PK	CHEMBL
Neuronal acetylcholine receptor subunit alpha-2	Ion channel	Q15822	ACHA2_HUMAN				WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-7	Ion channel	P36544	ACHA7_HUMAN	ANTAGONIST	IC50	8.25	IUPHAR
Neuronal acetylcholine receptor subunit alpha-3	Ion channel	P32297	ACHA3_HUMAN	ANTAGONIST	IC50	9.05	IUPHAR
Neuronal acetylcholine receptor subunit alpha-4	Ion channel	P43681	ACHA4_HUMAN	ANTAGONIST	IC50	8.10	IUPHAR
Small conductance calcium-activated potassium channel protein 3	Ion channel		KCNN3_RAT		Ki	5.23	CHEMBL

External reference:

ID	Source
2GQ1IRY63P	UNII
4019619	VUID
N0000147713	NUI
D00758	KEGG_DRUG
64228-81-5	SECONDARY_CAS_RN
1218	RXNORM
C0004234	UMLSCUI
CHEBI:2914	CHEBI
CHEMBL1360	ChEMBL_ID
47319	PUBCHEM_CID
DB13295	DRUGBANK_ID
CHEMBL1200527	ChEMBL_ID
D001279	MESH_DESCRIPTOR_UI
9537	IUPHAR_LIGAND_ID
DB00732	DRUGBANK_ID
1341	MMSL
397	MMSL
4228	MMSL
d00173	MMSL
372835000	SNOMEDCT_US
72752006	SNOMEDCT_US
74074008	SNOMEDCT_US
4018778	VANDF
4019619	VANDF
4734	INN_ID
002409	NDDF
013420	NDDF

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1105	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	12 sections
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1105	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	12 sections
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1109	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	12 sections
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1109	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	12 sections
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	25021-659	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	22 sections
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	25021-672	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	22 sections
Atracurium Besylate	Human Prescription Drug Label	1	55150-216	INJECTION, SOLUTION	50 mg	INTRAVENOUS	ANDA	20 sections
Atracurium Besylate	Human Prescription Drug Label	1	55150-216	INJECTION, SOLUTION	50 mg	INTRAVENOUS	ANDA	20 sections
Atracurium Besylate	Human Prescription Drug Label	1	55150-217	INJECTION, SOLUTION	100 mg	INTRAVENOUS	ANDA	20 sections
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	71288-701	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	23 sections
Atracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	71288-702	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	23 sections