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 296.45 51.36 36 1531 108 63487347
Anaphylactic reaction 203.92 51.36 72 1495 66028 63421427
Anaphylactic shock 143.07 51.36 43 1524 23590 63463865
Bradycardia 142.51 51.36 57 1510 73170 63414285
Bronchospasm 133.49 51.36 38 1529 17242 63470213
Neuromuscular block prolonged 97.48 51.36 16 1551 526 63486929
Drug reaction with eosinophilia and systemic symptoms 71.42 51.36 28 1539 33808 63453647
Cardiac arrest 68.71 51.36 37 1530 92508 63394947
Hypoventilation 62.84 51.36 16 1551 4738 63482717
Clonus 58.32 51.36 15 1552 4621 63482834
Hyperreflexia 54.65 51.36 15 1552 5919 63481536

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
Recurrence of neuromuscular blockade 247.79 59.46 34 1312 191 34955394
Anaphylactic shock 235.54 59.46 64 1282 15877 34939708
Anaphylactic reaction 227.47 59.46 73 1273 32228 34923357
Bronchospasm 157.83 59.46 43 1303 10688 34944897
Negative pressure pulmonary oedema 142.10 59.46 21 1325 212 34955373
Cardiac arrest 132.23 59.46 67 1279 96092 34859493
Bradycardia 107.73 59.46 54 1292 75364 34880221
Neuromuscular block prolonged 84.95 59.46 15 1331 486 34955099
Kounis syndrome 81.51 59.46 19 1327 2499 34953086
Oxygen saturation decreased 81.02 59.46 40 1306 53778 34901807

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
Recurrence of neuromuscular blockade 403.74 43.42 54 2785 265 79741284
Anaphylactic reaction 370.47 43.42 131 2708 83612 79657937
Anaphylactic shock 343.13 43.42 101 2738 35895 79705654
Bradycardia 206.50 43.42 99 2740 135458 79606091
Bronchospasm 203.00 43.42 62 2777 24797 79716752
Cardiac arrest 172.95 43.42 95 2744 172001 79569548
Neuromuscular block prolonged 171.41 43.42 30 2809 1000 79740549
Negative pressure pulmonary oedema 151.06 43.42 22 2817 216 79741333
Oxygen saturation decreased 104.52 43.42 62 2777 128985 79612564
Kounis syndrome 97.67 43.42 24 2815 4258 79737291
Hypoventilation 94.39 43.42 26 2813 7198 79734351
Laryngospasm 64.50 43.42 17 2822 3980 79737569
Hypotension 63.53 43.42 78 2761 440239 79301310
Delayed recovery from anaesthesia 62.53 43.42 14 2825 1659 79739890
Respiratory arrest 50.03 43.42 29 2810 57521 79684028
Blood pressure decreased 48.90 43.42 35 2804 99431 79642118
Clonus 47.09 43.42 15 2824 6825 79734724
Drug reaction with eosinophilia and systemic symptoms 44.54 43.42 28 2811 64216 79677333
Hyperreflexia 44.09 43.42 15 2824 8370 79733179

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 MSD 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 MSD 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 MSD 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 MSD 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 MSD SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS Jan. 22, 2024 REVISIONS TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE PACKAGE INSERT TO INCLUDE THE RESULT OF STUDY P145
EQ 500MG BASE/5ML (EQ 100MG BASE/ML) BRIDION MSD SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS Jan. 22, 2024 REVISIONS TO THE USE IN SPECIFIC POPULATIONS SECTION OF THE PACKAGE INSERT TO INCLUDE THE RESULT OF STUDY P145
EQ 200MG BASE/2ML (EQ 100MG BASE/ML) BRIDION MSD SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS June 25, 2024 NEW PATIENT POPULATION
EQ 500MG BASE/5ML (EQ 100MG BASE/ML) BRIDION MSD 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
6918585 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 0006-5423 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 0006-5425 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 29 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 31722-254 INJECTION 100 mg INTRAVENOUS ANDA 27 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 31722-255 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 27 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 71872-7187 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 71872-7187 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections