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

Stem definitionDrug idCAS RN
4233 343306-71-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sugammadex
  • bridion
  • sugammadex sodium
  • ORG 25969
Sugammadex is a modified gamma cyclodextrin which is a Selective Relaxant Binding Agent. It forms a complex with the neuromuscular blocking agents rocuronium or vecuronium in plasma and thereby reduces the amount of neuromuscular blocking agent available to bind to nicotinic receptors in the neuromuscular junction. This results in the reversal of neuromuscular blockade induced by rocuronium or vecuronium.
  • Molecular weight: 2002.12
  • Formula: C72H112O48S8
  • CLOGP: -11.90
  • LIPINSKI: 3
  • HAC: 48
  • HDO: 24
  • TPSA: 769.76
  • ALOGS: -1.88
  • ROTB: 40

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.18 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.28 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.53 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 25, 2008 EMA MERCK SHARP & DOHME LIMITED
Dec. 15, 2015 FDA ORGANON USA INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Recurrence of neuromuscular blockade 178.85 51.37 22 1161 81 50603860
Anaphylactic reaction 158.87 51.37 56 1127 53999 50549942
Bronchospasm 104.49 51.37 30 1153 14824 50589117
Bradycardia 103.37 51.37 43 1140 64383 50539558
Anaphylactic shock 99.65 51.37 31 1152 20124 50583817
Neuromuscular block prolonged 71.02 51.37 12 1171 499 50603442
Clonus 60.72 51.37 15 1168 4160 50599781
Hyperreflexia 57.68 51.37 15 1168 5103 50598838
Maternal exposure during pregnancy 54.39 51.37 38 1145 159740 50444201
Hypoventilation 51.57 51.37 13 1170 3908 50600033

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Anaphylactic reaction 171.62 69.86 55 946 27518 29546008
Anaphylactic shock 163.55 69.86 45 956 13291 29560235
Recurrence of neuromuscular blockade 147.45 69.86 20 981 118 29573408
Negative pressure pulmonary oedema 137.85 69.86 20 981 203 29573323
Bronchospasm 106.50 69.86 30 971 9579 29563947
Cardiac arrest 99.35 69.86 51 950 85540 29487986
Neuromuscular block prolonged 88.09 69.86 15 986 448 29573078
Bradycardia 81.52 69.86 41 960 65588 29507938
Kounis syndrome 78.67 69.86 17 984 1812 29571714

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Anaphylactic reaction 292.73 46.96 103 2069 68561 64427999
Recurrence of neuromuscular blockade 230.08 46.96 31 2141 173 64496387
Anaphylactic shock 228.05 46.96 70 2102 30258 64466302
Bradycardia 153.33 46.96 76 2096 118143 64378417
Neuromuscular block prolonged 147.67 46.96 26 2146 951 64495609
Bronchospasm 145.79 46.96 46 2126 21636 64474924
Negative pressure pulmonary oedema 137.49 46.96 20 2152 207 64496353
Cardiac arrest 128.96 46.96 74 2098 153990 64342570
Oxygen saturation decreased 82.90 46.96 49 2123 107127 64389433
Kounis syndrome 80.53 46.96 19 2153 3006 64493554
Hypoventilation 72.17 46.96 20 2152 5986 64490574
Delayed recovery from anaesthesia 59.01 46.96 13 2159 1515 64495045
Hypotension 55.59 46.96 66 2106 380908 64115652
Maternal exposure during pregnancy 51.88 46.96 35 2137 95849 64400711
Clonus 49.70 46.96 15 2157 6052 64490508
Laryngospasm 48.50 46.96 13 2159 3432 64493128
Hyperreflexia 47.27 46.96 15 2157 7133 64489427

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AB35 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Antidotes
FDA CS M0081434 gamma-Cyclodextrins
CHEBI has role CHEBI:51372 neuromuscular agent

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

DiseaseRelationSNOMED_IDDOID
Reversal of neuromuscular blockade indication 241703000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.58 acidic
pKa2 7.94 acidic
pKa3 8.0 acidic
pKa4 8.0 acidic
pKa5 8.0 acidic
pKa6 8.0 acidic
pKa7 8.0 acidic
pKa8 8.0 acidic
pKa9 13.29 acidic
pKa10 13.65 acidic
pKa11 13.89 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MG BASE/2ML (EQ 100MG BASE/ML) BRIDION ORGANON SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS RE44733 Jan. 27, 2026 REVERSAL OF DRUG-INDUCED NEUROMUSCULAR BLOCK
EQ 500MG BASE/5ML (EQ 100MG BASE/ML) BRIDION ORGANON SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS RE44733 Jan. 27, 2026 REVERSAL OF DRUG-INDUCED NEUROMUSCULAR BLOCK

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 200MG BASE/2ML (EQ 100MG BASE/ML) BRIDION ORGANON SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS June 9, 2023 REVISIONS TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE PACKAGE INSERT TO INCLUDE THE RESULT OF STUDY P146 TO FULFILL THE REQUIREMENTS OF PMR 3003-4
EQ 500MG BASE/5ML (EQ 100MG BASE/ML) BRIDION ORGANON SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS June 9, 2023 REVISIONS TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE PACKAGE INSERT TO INCLUDE THE RESULT OF STUDY P146 TO FULFILL THE REQUIREMENTS OF PMR 3003-4
EQ 200MG BASE/2ML (EQ 100MG BASE/ML) BRIDION ORGANON SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS June 25, 2024 NEW PATIENT POPULATION
EQ 500MG BASE/5ML (EQ 100MG BASE/ML) BRIDION ORGANON SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS June 25, 2024 NEW PATIENT POPULATION

Bioactivity Summary:

None

External reference:

IDSource
D05940 KEGG_DRUG
343306-79-6 SECONDARY_CAS_RN
4035288 VANDF
C1700695 UMLSCUI
CHEBI:90953 CHEBI
CHEMBL2111107 ChEMBL_ID
CHEMBL2107374 ChEMBL_ID
D000077122 MESH_DESCRIPTOR_UI
DB06206 DRUGBANK_ID
8528 INN_ID
361LPM2T56 UNII
6918584 PUBCHEM_CID
1726987 RXNORM
159483 MMSL
26064 MMSL
31376 MMSL
31381 MMSL
d07361 MMSL
012914 NDDF
012915 NDDF
1172425006 SNOMEDCT_US
442340006 SNOMEDCT_US
442379000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 0006-5423 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 29 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 0006-5423 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 29 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 0006-5425 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 29 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 0006-5425 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 29 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 71872-7187 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections