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

Stem definition	Drug id	CAS RN
neuromuscular blocking agents with rigid structure	661	96946-42-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: cisatracurium besylate cisatracurium besilate cisatracurium	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:

cisatracurium besylate
cisatracurium besilate
cisatracurium

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)	0.14 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	5.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.62 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.42 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 15, 1995	FDA	ABBVIE

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	373.41	44.55	104	2812	23529	63462577
Anaphylactic reaction	144.05	44.55	67	2849	66033	63420073
Hypotension	99.09	44.55	89	2827	272515	63213591
Mixed liver injury	98.71	44.55	26	2890	4709	63481397
Bronchospasm	98.52	44.55	35	2881	17245	63468861
Cardiac arrest	98.33	44.55	58	2858	92487	63393619
Circulatory collapse	76.38	44.55	31	2885	21907	63464199
Myoclonus	75.02	44.55	28	2888	15840	63470266
Multiple organ dysfunction syndrome	74.84	44.55	41	2875	56711	63429395
Cardiogenic shock	71.69	44.55	28	2888	17904	63468202
Bradycardia	65.14	44.55	41	2875	73186	63412920
Acute generalised exanthematous pustulosis	61.42	44.55	22	2894	11077	63475029
Respiratory failure	52.90	44.55	41	2875	101817	63384289
Sinus tachycardia	50.87	44.55	24	2892	24244	63461862
Post procedural complication	48.89	44.55	21	2895	17053	63469053
Shock	48.56	44.55	23	2893	23440	63462666
Bronchopulmonary dysplasia	46.07	44.55	9	2907	424	63485682
Apnoea	44.75	44.55	16	2900	8006	63478100

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	287.00	34.56	91	3138	15850	34937852
Hyperthermia malignant	177.48	34.56	41	3188	2136	34951566
Anaphylactic reaction	126.59	34.56	61	3168	32240	34921462
Hypertransaminasaemia	113.17	34.56	35	3194	5571	34948131
Drug reaction with eosinophilia and systemic symptoms	101.77	34.56	53	3176	32959	34920743
Rhabdomyolysis	98.31	34.56	67	3162	68096	34885606
Toxic epidermal necrolysis	94.29	34.56	44	3185	21602	34932100
Bronchospasm	76.86	34.56	31	3198	10700	34943002
Shock	66.49	34.56	36	3193	24143	34929559
Hypotension	55.69	34.56	84	3145	221565	34732137
Acute respiratory distress syndrome	50.86	34.56	31	3198	25938	34927764
Cardiac arrest	49.07	34.56	52	3177	96107	34857595
Klebsiella infection	48.79	34.56	21	3208	8510	34945192
Vasoplegia syndrome	47.84	34.56	14	3215	1842	34951860
Serotonin syndrome	47.45	34.56	27	3202	19906	34933796
Septic shock	44.20	34.56	43	3186	71791	34881911
Hypoxia	41.65	34.56	37	3192	55058	34898644
Pseudomonal sepsis	38.93	34.56	14	3215	3533	34950169
Haemodynamic instability	37.26	34.56	18	3211	9505	34944197
Circulatory collapse	35.85	34.56	23	3206	21015	34932687
Multiple organ dysfunction syndrome	34.82	34.56	39	3190	76527	34877175

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	632.89	30.39	191	5645	35805	79702747
Anaphylactic reaction	253.21	30.39	123	5713	83620	79654932
Hyperthermia malignant	196.18	30.39	45	5791	2872	79735680
Bronchospasm	169.60	30.39	65	5771	24794	79713758
Hypotension	133.30	30.39	162	5674	440155	79298397
Cardiac arrest	128.87	30.39	104	5732	171992	79566560
Mixed liver injury	119.09	30.39	37	5799	7541	79731011
Hypertransaminasaemia	106.40	30.39	38	5798	11886	79726666
Shock	105.07	30.39	55	5781	43493	79695059
Toxic epidermal necrolysis	101.03	30.39	54	5782	44527	79694025
Circulatory collapse	94.95	30.39	49	5787	37619	79700933
Multiple organ dysfunction syndrome	92.74	30.39	74	5762	120172	79618380
Rhabdomyolysis	91.56	30.39	69	5767	103062	79635490
Drug reaction with eosinophilia and systemic symptoms	90.16	30.39	57	5779	64187	79674365
Acute respiratory distress syndrome	71.74	30.39	43	5793	44024	79694528
Hypoxia	65.95	30.39	57	5779	103186	79635366
Bradycardia	61.77	30.39	62	5774	135495	79603057
Acute generalised exanthematous pustulosis	57.01	30.39	27	5809	17227	79721325
Cardiogenic shock	50.94	30.39	34	5802	41880	79696672
Myoclonus	50.29	30.39	29	5807	27631	79710921
Cyanosis	50.09	30.39	28	5808	25154	79713398
Vasoplegia syndrome	49.86	30.39	16	5820	3614	79734938
Tachycardia	49.60	30.39	63	5773	177705	79560847
Septic shock	48.43	30.39	52	5784	122749	79615803
Propofol infusion syndrome	45.60	30.39	13	5823	1970	79736582
Haemodynamic instability	44.89	30.39	23	5813	17359	79721193
Hepatocellular injury	44.76	30.39	33	5803	47560	79690992
Ventricular fibrillation	43.93	30.39	28	5808	31898	79706654
Metabolic acidosis	43.67	30.39	41	5795	82488	79656064
Klebsiella infection	41.18	30.39	21	5815	15699	79722853
Fatigue	41.14	30.39	9	5827	929718	78808834
Diarrhoea	37.99	30.39	9	5827	880480	78858072
Serotonin syndrome	37.42	30.39	29	5807	44998	79693554
Blood pressure decreased	37.25	30.39	41	5795	99425	79639127
Sinus tachycardia	35.62	30.39	26	5810	36882	79701670
Nausea	35.44	30.39	13	5823	957183	78781369
Cardio-respiratory arrest	34.34	30.39	41	5795	108469	79630083
Skin test positive	32.96	30.39	9	5827	1165	79737387
Toxic skin eruption	31.79	30.39	20	5816	22273	79716279

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	M03AC11	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	D009465	Neuromuscular Agents
MeSH PA	D009466	Neuromuscular Blocking Agents
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
Disorder of lung	contraindication	19829001	DOID:850
Myasthenia gravis	contraindication	91637004	DOID:437
Disorder of electrolytes	contraindication	237840007
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])	Mechanism action	Bioact source	MoA source
Acetylcholine receptor	Ion channel	P02708 P11230 Q07001	ACHA_HUMAN ACHB_HUMAN ACHD_HUMAN	ANTAGONIST	IC50	8		WOMBAT-PK	CHEMBL

External reference:

ID	Source
4020957	VUID
N0000148433	NUI
D00759	KEGG_DRUG
136561	RXNORM
4020957	VANDF
4024019	VANDF
C1096766	UMLSCUI
CHEBI:3721	CHEBI
CHEMBL1201248	ChEMBL_ID
CHEMBL1200641	ChEMBL_ID
DB00565	DRUGBANK_ID
C101584	MESH_SUPPLEMENTAL_RECORD_UI
QX62KLI41N	UNII
62887	PUBCHEM_CID
192613	MMSL
36562	MMSL
4455	MMSL
d03875	MMSL
005186	NDDF
005213	NDDF
108452005	SNOMEDCT_US
108453000	SNOMEDCT_US
372495006	SNOMEDCT_US
7389	INN_ID
96946-41-7	SECONDARY_CAS_RN

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4378	INJECTION	2 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4378	INJECTION	2 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4378	INJECTION	2 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4380	INJECTION	2 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4380	INJECTION	2 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4380	INJECTION	2 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4382	INJECTION	10 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4382	INJECTION	10 mg	INTRAVENOUS	NDA	27 sections
Nimbex	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4382	INJECTION	10 mg	INTRAVENOUS	NDA	27 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9396	INJECTION	2 mg	INTRAVENOUS	ANDA	29 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1098	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1098	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1098	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1103	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1103	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1103	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1208	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1208	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1208	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	28 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-3670	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	30 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-3670	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	30 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-5547	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	30 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-5547	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	30 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-7083	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	30 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0409-7083	INJECTION, SOLUTION	2 mg	INTRAVENOUS	ANDA	30 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0703-2033	INJECTION	10 mg	INTRAVENOUS	ANDA	25 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0703-2033	INJECTION	10 mg	INTRAVENOUS	ANDA	25 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0703-2033	INJECTION	10 mg	INTRAVENOUS	ANDA	25 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0703-2045	INJECTION	200 mg	INTRAVENOUS	ANDA	25 sections
Cisatracurium Besylate	HUMAN PRESCRIPTION DRUG LABEL	1	0703-2045	INJECTION	200 mg	INTRAVENOUS	ANDA	25 sections