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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

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

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 391.63 44.41 48 2266 152 90625981
Anaphylactic reaction 351.22 44.41 117 2197 87407 90538726
Anaphylactic shock 303.82 44.41 83 2231 31534 90594599
Bronchospasm 244.36 44.41 64 2250 20645 90605488
Bradycardia 235.29 44.41 86 2228 83761 90542372
Neuromuscular block prolonged 114.85 44.41 19 2295 633 90625500
Cardiac arrest 114.47 44.41 55 2259 104880 90521253
Hypotension 75.65 44.41 64 2250 325333 90300800
Vocal cord dysfunction 69.25 44.41 13 2301 901 90625232
Drug reaction with eosinophilia and systemic symptoms 67.37 44.41 29 2285 42729 90583404
Hypoventilation 60.57 44.41 16 2298 5280 90620853
Clonus 59.26 44.41 16 2298 5734 90620399
Oxygen saturation decreased 54.53 44.41 34 2280 107449 90518684
Muscle twitching 53.75 44.41 21 2293 24181 90601952
Hyperreflexia 52.42 44.41 15 2299 6642 90619491
Maternal exposure during pregnancy 51.24 44.41 54 2260 360009 90266124
Delayed recovery from anaesthesia 49.46 44.41 10 2304 1020 90625113
Fanconi syndrome 48.49 44.41 11 2303 1932 90624201
Angioedema 47.37 44.41 26 2288 64850 90561283
Anaesthetic complication neurological 46.52 44.41 9 2305 732 90625401

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 460.78 52.82 141 1927 42602 42576665
Recurrence of neuromuscular blockade 361.52 52.82 50 2018 228 42619039
Anaphylactic shock 323.93 52.82 94 1974 23423 42595844
Negative pressure pulmonary oedema 226.31 52.82 37 2031 588 42618679
Bronchospasm 197.10 52.82 56 2012 12829 42606438
Cardiac arrest 195.23 52.82 98 1970 109222 42510045
Bradycardia 177.46 52.82 85 1983 85399 42533868
Neuromuscular block prolonged 129.90 52.82 23 2045 596 42618671
Laryngospasm 92.25 52.82 21 2047 1967 42617300
Kounis syndrome 81.24 52.82 21 2047 3347 42615920
Oxygen saturation decreased 78.40 52.82 45 2023 64642 42554625
Delayed recovery from anaesthesia 74.39 52.82 16 2052 1153 42618114
Hypotension 65.66 52.82 71 1997 257560 42361707
Hypoventilation 55.65 52.82 16 2052 3786 42615481

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 693.25 36.68 231 4049 114069 110470950
Anaphylactic shock 586.54 36.68 169 4111 51377 110533642
Recurrence of neuromuscular blockade 581.85 36.68 78 4202 353 110584666
Bradycardia 327.89 36.68 146 4134 155371 110429648
Bronchospasm 311.68 36.68 92 4188 30147 110554872
Cardiac arrest 256.89 36.68 133 4147 196620 110388399
Negative pressure pulmonary oedema 230.36 36.68 37 4243 662 110584357
Neuromuscular block prolonged 215.63 36.68 38 4242 1209 110583810
Delayed recovery from anaesthesia 128.49 36.68 27 4253 2188 110582831
Laryngospasm 118.55 36.68 29 4251 4639 110580380
Oxygen saturation decreased 117.60 36.68 74 4206 156908 110428111
Hypotension 114.83 36.68 120 4160 523729 110061290
Kounis syndrome 111.69 36.68 29 4251 5896 110579123
Hypoventilation 98.25 36.68 28 4252 8053 110576966
Respiratory arrest 68.89 36.68 37 4243 58262 110526757
Blood pressure decreased 63.72 36.68 45 4235 115046 110469973
Vocal cord dysfunction 63.34 36.68 13 4267 937 110584082
Hypoxia 58.96 36.68 45 4235 129470 110455549
Haemodynamic instability 56.13 36.68 24 4256 22864 110562155
Pulseless electrical activity 52.73 36.68 21 4259 16736 110568283
Muscle twitching 49.96 36.68 24 4256 29911 110555108
Clonus 46.12 36.68 16 4264 8700 110576319
Drug interaction 43.59 36.68 73 4207 500110 110084909
Airway complication of anaesthesia 43.50 36.68 9 4271 675 110584344
Respiratory failure 42.81 36.68 47 4233 215285 110369734
Hyperreflexia 41.05 36.68 15 4265 9470 110575549
Anaesthetic complication neurological 39.80 36.68 9 4271 1024 110583995
Respiratory acidosis 38.93 36.68 16 4264 13810 110571209
Drug reaction with eosinophilia and systemic symptoms 38.38 36.68 29 4251 82066 110502953
Angioedema 37.87 36.68 31 4249 98469 110486550
Fanconi syndrome 37.46 36.68 11 4269 3508 110581511
Ventricular fibrillation 37.33 36.68 22 4258 41291 110543728

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
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:74518 anti-obesity agent
CHEBI has role CHEBI:90753 antidote to organophosphate poisoning
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

V03AB Antidotes 28 drugs
4-dimethylaminophenolacetylcysteineamyl nitriteandexanet alfaatropinecopper sulfatedimercaprolethanolflumazenilfomepizoleglutathionehydroxocobalamin show all 28 →

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 Dec. 12, 2027 NEW PATIENT POPULATION
EQ 500MG BASE/5ML (EQ 100MG BASE/ML) BRIDION MSD SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS Dec. 12, 2027 NEW PATIENT POPULATION
EQ 200MG BASE/2ML (EQ 100MG BASE/ML) BRIDION MSD SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS June 12, 2028 PEDIATRIC EXCLUSIVITY
EQ 500MG BASE/5ML (EQ 100MG BASE/ML) BRIDION MSD SUB MERCK N022225 Dec. 15, 2015 RX SOLUTION INTRAVENOUS June 12, 2028 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

None

External reference:

IDSource
D05940 KEGG_DRUG
4035288 VANDF
C1700695 UMLSCUI
CHEBI:90953 CHEBI
CHEMBL2111107 ChEMBL_ID
CHEMBL2107374 ChEMBL_ID
D000077122 MESH_DESCRIPTOR_UI
DB06206 DRUGBANK_ID
8528 INN_ID
343306-79-6 SECONDARY_CAS_RN
361LPM2T56 UNII
6918585 PUBCHEM_CID
1726987 RXNORM
159483 MMSL
26064 MMSL
31376 MMSL
31381 MMSL
350855 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 28 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 0006-5425 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 0264-8200 INJECTION 200 mg INTRAVENOUS ANDA 30 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 0781-3468 INJECTION, SOLUTION 200 mg INTRAVENOUS ANDA 27 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 0781-3469 INJECTION, SOLUTION 500 mg INTRAVENOUS ANDA 27 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 25021-619 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 31 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
SUGAMMADEX SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 42023-830 SOLUTION 200 mg INTRAVENOUS ANDA 18 sections
SUGAMMADEX SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 42023-935 SOLUTION 500 mg INTRAVENOUS ANDA 18 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 43598-924 INJECTION, SOLUTION 200 mg INTRAVENOUS ANDA 27 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 43598-925 INJECTION, SOLUTION 500 mg INTRAVENOUS ANDA 27 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 66794-256 INJECTION, SOLUTION 100 mg INTRAVENOUS unapproved drug other 29 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 66794-257 INJECTION, SOLUTION 100 mg INTRAVENOUS unapproved drug other 29 sections
sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 70069-892 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 26 sections
sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 70069-893 INJECTION, SOLUTION 100 mg INTRAVENOUS ANDA 26 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 70710-1650 INJECTION, SOLUTION 200 mg INTRAVENOUS ANDA 24 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 70710-1651 INJECTION, SOLUTION 500 mg INTRAVENOUS ANDA 24 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 70771-1856 INJECTION, SOLUTION 200 mg INTRAVENOUS ANDA 1 sections
Sugammadex HUMAN PRESCRIPTION DRUG LABEL 1 70771-1857 INJECTION, SOLUTION 500 mg INTRAVENOUS ANDA 1 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 71872-7187 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 28 sections
SUGAMMADEX SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 82449-241 SOLUTION 200 mg INTRAVENOUS ANDA 18 sections
SUGAMMADEX SODIUM HUMAN PRESCRIPTION DRUG LABEL 1 82449-242 SOLUTION 500 mg INTRAVENOUS ANDA 18 sections
BRIDION HUMAN PRESCRIPTION DRUG LABEL 1 84549-423 INJECTION, SOLUTION 100 mg INTRAVENOUS NDA 29 sections