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Identification
NameGallamine Triethiodide
Accession NumberDB00483  (APRD00712)
TypeSmall Molecule
GroupsApproved
DescriptionA synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of tubocurarine, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)
Structure
Thumb
Synonyms
Flaxedil
Gallamin triethiodid
Gallamini Triethiodidum
Triéthiodure de Gallamine
Trietioduro de galamina
External Identifiers
  • F 2559
  • HL 8583
  • RP 3697
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Flaxedil Inj 20mg/mlliquid20 mgintravenousAventis Pharma Inc1951-12-312003-07-22Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
FlaxedilSanofi-Aventis
MyraxanYoo Young
SincurarinaCarlo Erba
TricuranNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIQ3254X40X2
CAS number65-29-2
WeightAverage: 891.5291
Monoisotopic: 891.176873061
Chemical FormulaC30H60I3N3O3
InChI KeyInChIKey=REEUVFCVXKWOFE-UHFFFAOYSA-K
InChI
InChI=1S/C30H60N3O3.3HI/c1-10-31(11-2,12-3)22-25-34-28-20-19-21-29(35-26-23-32(13-4,14-5)15-6)30(28)36-27-24-33(16-7,17-8)18-9;;;/h19-21H,10-18,22-27H2,1-9H3;3*1H/q+3;;;/p-3
IUPAC Name
(2-{2,3-bis[2-(triethylazaniumyl)ethoxy]phenoxy}ethyl)triethylazanium triiodide
SMILES
[I-].[I-].[I-].CC[N+](CC)(CC)CCOC1=CC=CC(OCC[N+](CC)(CC)CC)=C1OCC[N+](CC)(CC)CC
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenol ethers
Direct ParentPhenol ethers
Alternative Parents
Substituents
  • Phenol ether
  • Choline
  • Alkyl aryl ether
  • Quaternary ammonium salt
  • Ether
  • Hydrocarbon derivative
  • Organic iodide salt
  • Organic salt
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Organic zwitterion
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor use as adjuncts to anesthesia to induce skeletal muscle relaxation and to facilitate the management of patients undergoing mechanical ventilation
PharmacodynamicsGallamine Triethiodide is a nondepolarizing neuromuscular blocking drug (NDMRD) used as an adjunct to anesthesia to induce skeletal muscle relaxation. The actions of gallamine triethiodide are similar to those of tubocurarine, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. Muscle groups differ in their sensitivity to these types of relaxants with ocular muscles (controlling eyelids) being most sensitive, followed by the muscles of the neck, jaw, limbs and then abdomen. The diaphragm is the least sensitive muscle to NDMRDs. Although the nondepolarizing neuromuscular blocking drugs do not have the same adverse effects as succinylcholine, their onset of action is slower. They also have a longer duration of action, making them more suitable for maintaining neuromuscular relaxation during major surgical procedures.
Mechanism of actionIt competes with acetylcholine (ACh) molecules and binds to muscarinic acetylcholine receptors on the post-synaptic membrane of the motor endplate. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. It blocks the action of ACh and prevents activation of the muscle contraction process. It can also act on nicotinic presynaptic acetylcholine receptors which inhibits the release of ACh.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8901
Blood Brain Barrier+0.8616
Caco-2 permeable+0.6256
P-glycoprotein substrateSubstrate0.6912
P-glycoprotein inhibitor INon-inhibitor0.8173
P-glycoprotein inhibitor IINon-inhibitor0.8176
Renal organic cation transporterNon-inhibitor0.6818
CYP450 2C9 substrateNon-substrate0.8147
CYP450 2D6 substrateNon-substrate0.6511
CYP450 3A4 substrateSubstrate0.5708
CYP450 1A2 substrateNon-inhibitor0.8002
CYP450 2C9 inhibitorNon-inhibitor0.8613
CYP450 2D6 inhibitorNon-inhibitor0.8874
CYP450 2C19 inhibitorNon-inhibitor0.8815
CYP450 3A4 inhibitorNon-inhibitor0.9296
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6622
Ames testNon AMES toxic0.6156
CarcinogenicityNon-carcinogens0.5724
BiodegradationNot ready biodegradable0.9841
Rat acute toxicity2.8202 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7691
hERG inhibition (predictor II)Inhibitor0.666
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Davis and geck div american cyanamid co
PackagersNot Available
Dosage forms
FormRouteStrength
Liquidintravenous20 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point152-153Fourneau, E.; U.S.Patent 2,544,076; March 6, 1951; assigned to Societe des Usines Chimiques Rhone-Poulenc, France.
water solubilitySolubleNot Available
logP3.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility4.65e-06 mg/mLALOGPS
logP-0.38ALOGPS
logP-7.7ChemAxon
logS-8.3ALOGPS
pKa (Strongest Basic)-4.5ChemAxon
Physiological Charge3ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area27.69 Å2ChemAxon
Rotatable Bond Count21ChemAxon
Refractivity189.98 m3·mol-1ChemAxon
Polarizability63.43 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Fourneau, E.; U.S.Patent 2,544,076; March 6, 1951; assigned to Societe des Usines Chimiques Rhone-Poulenc, France.

General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (28.5 KB)
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with 1,10-Phenanthroline.
4-AndrostenedioneThe risk or severity of adverse effects can be increased when 4-Androstenedione is combined with Gallamine Triethiodide.
AcebutololGallamine Triethiodide may increase the bradycardic activities of Acebutolol.
AcetylcholineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Acetylcholine.
AclidiniumAclidinium may increase the anticholinergic activities of Gallamine Triethiodide.
AclidiniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Aclidinium.
AlclometasoneThe risk or severity of adverse effects can be increased when Alclometasone is combined with Gallamine Triethiodide.
AldosteroneThe risk or severity of adverse effects can be increased when Aldosterone is combined with Gallamine Triethiodide.
AlfentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Alfentanil.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Alphacetylmethadol.
AlprenololGallamine Triethiodide may increase the bradycardic activities of Alprenolol.
AmbenoniumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Ambenonium.
AmcinonideThe risk or severity of adverse effects can be increased when Amcinonide is combined with Gallamine Triethiodide.
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Anisotropine Methylbromide.
ArecolineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Arecoline.
ArotinololGallamine Triethiodide may increase the bradycardic activities of Arotinolol.
AtenololGallamine Triethiodide may increase the bradycardic activities of Atenolol.
Atracurium besylateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Atracurium besylate.
AtropineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Atropine.
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Gallamine Triethiodide.
BefunololGallamine Triethiodide may increase the bradycardic activities of Befunolol.
BenactyzineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Benactyzine.
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Gallamine Triethiodide.
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Gallamine Triethiodide.
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Gallamine Triethiodide.
BetaxololGallamine Triethiodide may increase the bradycardic activities of Betaxolol.
BethanecholThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Bethanechol.
BevantololGallamine Triethiodide may increase the bradycardic activities of Bevantolol.
BezitramideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Bezitramide.
BiperidenThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Biperiden.
BisoprololGallamine Triethiodide may increase the bradycardic activities of Bisoprolol.
BopindololGallamine Triethiodide may increase the bradycardic activities of Bopindolol.
Botulinum Toxin Type AGallamine Triethiodide may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BGallamine Triethiodide may increase the anticholinergic activities of Botulinum Toxin Type B.
BudesonideThe risk or severity of adverse effects can be increased when Budesonide is combined with Gallamine Triethiodide.
BufuralolGallamine Triethiodide may increase the bradycardic activities of Bufuralol.
BupranololGallamine Triethiodide may increase the bradycardic activities of Bupranolol.
BuprenorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Buprenorphine.
ButorphanolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Butorphanol.
CarbacholThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Carbachol.
CarfentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Carfentanil.
CarteololGallamine Triethiodide may increase the bradycardic activities of Carteolol.
CarvedilolGallamine Triethiodide may increase the bradycardic activities of Carvedilol.
CeliprololGallamine Triethiodide may increase the bradycardic activities of Celiprolol.
CevimelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Cevimeline.
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Gallamine Triethiodide.
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Chlorphenoxamine.
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Gallamine Triethiodide.
CiclesonideThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Gallamine Triethiodide.
CimetropiumGallamine Triethiodide may increase the anticholinergic activities of Cimetropium.
Clobetasol propionateThe risk or severity of adverse effects can be increased when Clobetasol propionate is combined with Gallamine Triethiodide.
ClocortoloneThe risk or severity of adverse effects can be increased when Clocortolone is combined with Gallamine Triethiodide.
CodeineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Codeine.
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Gallamine Triethiodide.
CoumaphosThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Coumaphos.
CyclopentolateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Cyclopentolate.
DarifenacinThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Darifenacin.
DecamethoniumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Decamethonium.
DehydroepiandrosteroneThe risk or severity of adverse effects can be increased when Dehydroepiandrosterone is combined with Gallamine Triethiodide.
dehydroepiandrosterone sulfateThe risk or severity of adverse effects can be increased when dehydroepiandrosterone sulfate is combined with Gallamine Triethiodide.
DemecariumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Demecarium.
DesloratadineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Desloratadine.
DesoximetasoneThe risk or severity of adverse effects can be increased when Desoximetasone is combined with Gallamine Triethiodide.
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Desoxycorticosterone acetate is combined with Gallamine Triethiodide.
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Gallamine Triethiodide.
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Dexamethasone isonicotinate is combined with Gallamine Triethiodide.
DexetimideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dexetimide.
DextromoramideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dextromoramide.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dextropropoxyphene.
DezocineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dezocine.
DichlorvosThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Dichlorvos.
DicyclomineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dicyclomine.
DiflorasoneThe risk or severity of adverse effects can be increased when Diflorasone is combined with Gallamine Triethiodide.
DifluocortoloneThe risk or severity of adverse effects can be increased when Difluocortolone is combined with Gallamine Triethiodide.
DifluprednateThe risk or severity of adverse effects can be increased when Difluprednate is combined with Gallamine Triethiodide.
DihydrocodeineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dihydrocodeine.
DihydroetorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dihydroetorphine.
DihydromorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dihydromorphine.
DiphenoxylateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Diphenoxylate.
DipyridamoleThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Dipyridamole.
DonepezilThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Donepezil.
DPDPEThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with DPDPE.
DronabinolGallamine Triethiodide may increase the tachycardic activities of Dronabinol.
EchothiophateThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Echothiophate.
EdrophoniumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Edrophonium.
EluxadolineGallamine Triethiodide may increase the constipating activities of Eluxadoline.
EPIBATIDINEThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with EPIBATIDINE.
EquileninThe risk or severity of adverse effects can be increased when Equilenin is combined with Gallamine Triethiodide.
EquilinThe risk or severity of adverse effects can be increased when Equilin is combined with Gallamine Triethiodide.
EsmololGallamine Triethiodide may increase the bradycardic activities of Esmolol.
EstroneThe risk or severity of adverse effects can be increased when Estrone is combined with Gallamine Triethiodide.
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Gallamine Triethiodide.
EthylmorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Ethylmorphine.
EtorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Etorphine.
FentanylThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Fentanyl.
FenthionThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Fenthion.
FesoterodineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Fesoterodine.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Gallamine Triethiodide.
FlumethasoneThe risk or severity of adverse effects can be increased when Flumethasone is combined with Gallamine Triethiodide.
FlunisolideThe risk or severity of adverse effects can be increased when Flunisolide is combined with Gallamine Triethiodide.
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Fluocinolone Acetonide is combined with Gallamine Triethiodide.
FluocinonideThe risk or severity of adverse effects can be increased when Fluocinonide is combined with Gallamine Triethiodide.
FluocortoloneThe risk or severity of adverse effects can be increased when Fluocortolone is combined with Gallamine Triethiodide.
FluorometholoneThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Gallamine Triethiodide.
FluprednideneThe risk or severity of adverse effects can be increased when Fluprednidene is combined with Gallamine Triethiodide.
FluprednisoloneThe risk or severity of adverse effects can be increased when Fluprednisolone is combined with Gallamine Triethiodide.
FlurandrenolideThe risk or severity of adverse effects can be increased when Flurandrenolide is combined with Gallamine Triethiodide.
Fluticasone furoateThe risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Gallamine Triethiodide.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Gallamine Triethiodide.
GalantamineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Galantamine.
Ginkgo bilobaThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Ginkgo biloba.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Glucagon recombinant.
GlycopyrroniumThe risk or severity of adverse effects can be increased when Glycopyrronium is combined with Gallamine Triethiodide.
GlycopyrroniumGallamine Triethiodide may increase the anticholinergic activities of Glycopyrronium.
GTS-21The risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with GTS-21.
HeroinThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Heroin.
HexamethoniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Hexamethonium.
HomatropineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Homatropine.
Huperzine AThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Huperzine A.
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Gallamine Triethiodide.
HydrocodoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Hydrocodone.
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Gallamine Triethiodide.
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Gallamine Triethiodide.
HydromorphoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Hydromorphone.
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Gallamine Triethiodide.
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Gallamine Triethiodide.
IndenololGallamine Triethiodide may increase the bradycardic activities of Indenolol.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Gallamine Triethiodide.
IsoflurophateThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Isoflurophate.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Gallamine Triethiodide.
KetobemidoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Ketobemidone.
LabetalolGallamine Triethiodide may increase the bradycardic activities of Labetalol.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Levomethadyl Acetate.
LevorphanolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Levorphanol.
LobelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Lobeline.
LofentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Lofentanil.
MalathionThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Malathion.
MecamylamineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Mecamylamine.
MedrysoneThe risk or severity of adverse effects can be increased when Medrysone is combined with Gallamine Triethiodide.
MefloquineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Mefloquine.
MelengestrolThe risk or severity of adverse effects can be increased when Melengestrol is combined with Gallamine Triethiodide.
MemantineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Memantine.
MethacholineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methacholine.
MethadoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methadone.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methadyl Acetate.
MethanthelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methantheline.
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Gallamine Triethiodide.
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Gallamine Triethiodide.
MetixeneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Metixene.
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Gallamine Triethiodide.
MetoprololGallamine Triethiodide may increase the bradycardic activities of Metoprolol.
MianserinMianserin may increase the anticholinergic activities of Gallamine Triethiodide.
MinaprineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Minaprine.
MirabegronThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Mirabegron.
MivacuriumGallamine Triethiodide may decrease the neuromuscular blocking activities of Mivacurium.
MometasoneThe risk or severity of adverse effects can be increased when Mometasone is combined with Gallamine Triethiodide.
MorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Morphine.
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with N-butylscopolammonium bromide.
NabiloneGallamine Triethiodide may increase the tachycardic activities of Nabilone.
NadololGallamine Triethiodide may increase the bradycardic activities of Nadolol.
NalbuphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Nalbuphine.
NeostigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Neostigmine.
NicotineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Nicotine.
Nicotine bitartrateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Nicotine bitartrate.
NormethadoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Normethadone.
NVA237The risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with NVA237.
OpiumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Opium.
OrphenadrineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Orphenadrine.
OxprenololGallamine Triethiodide may increase the bradycardic activities of Oxprenolol.
OxybutyninThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Oxybutynin.
OxycodoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Oxycodone.
OxymorphoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Oxymorphone.
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Gallamine Triethiodide.
PancuroniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pancuronium.
ParamethasoneThe risk or severity of adverse effects can be increased when Paramethasone is combined with Gallamine Triethiodide.
PenbutololGallamine Triethiodide may increase the bradycardic activities of Penbutolol.
PentazocineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pentazocine.
PentoliniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pentolinium.
PethidineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pethidine.
PhysostigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Physostigmine.
PilocarpineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pilocarpine.
PindololGallamine Triethiodide may increase the bradycardic activities of Pindolol.
PipecuroniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pipecuronium.
PirenzepineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pirenzepine.
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Gallamine Triethiodide.
Potassium ChlorideGallamine Triethiodide may increase the ulcerogenic activities of Potassium Chloride.
PractololGallamine Triethiodide may increase the bradycardic activities of Practolol.
PramlintidePramlintide may increase the anticholinergic activities of Gallamine Triethiodide.
PrednicarbateThe risk or severity of adverse effects can be increased when Prednicarbate is combined with Gallamine Triethiodide.
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Gallamine Triethiodide.
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Gallamine Triethiodide.
PregnenoloneThe risk or severity of adverse effects can be increased when Pregnenolone is combined with Gallamine Triethiodide.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Gallamine Triethiodide.
PropanthelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Propantheline.
PropranololGallamine Triethiodide may increase the bradycardic activities of Propranolol.
PyridostigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Pyridostigmine.
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Gallamine Triethiodide.
QuinidineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Quinidine.
RamosetronGallamine Triethiodide may increase the constipating activities of Ramosetron.
RapacuroniumGallamine Triethiodide may decrease the neuromuscular blocking activities of Rapacuronium.
RemifentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Remifentanil.
RimexoloneThe risk or severity of adverse effects can be increased when Rimexolone is combined with Gallamine Triethiodide.
RivastigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Rivastigmine.
ScopolamineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Scopolamine.
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Scopolamine butylbromide.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Gallamine Triethiodide.
SolifenacinThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Solifenacin.
SotalolGallamine Triethiodide may increase the bradycardic activities of Sotalol.
SuccinylcholineThe serum concentration of Succinylcholine can be increased when it is combined with Gallamine Triethiodide.
SufentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Sufentanil.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Gallamine Triethiodide.
TacrineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Tacrine.
TapentadolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tapentadol.
TimololGallamine Triethiodide may increase the bradycardic activities of Timolol.
TiotropiumGallamine Triethiodide may increase the anticholinergic activities of Tiotropium.
TiotropiumThe risk or severity of adverse effects can be increased when Tiotropium is combined with Gallamine Triethiodide.
TixocortolThe risk or severity of adverse effects can be increased when Tixocortol is combined with Gallamine Triethiodide.
TolterodineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tolterodine.
TopiramateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tramadol.
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Gallamine Triethiodide.
TrichlorfonThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Trichlorfon.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Gallamine Triethiodide.
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Gallamine Triethiodide.
TrimethaphanThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Trimethaphan.
TropicamideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tropicamide.
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Gallamine Triethiodide.
TubocurarineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tubocurarine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Gallamine Triethiodide.
UmeclidiniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Umeclidinium.
VareniclineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Varenicline.
VecuroniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Vecuronium.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Huang XP, Prilla S, Mohr K, Ellis J: Critical amino acid residues of the common allosteric site on the M2 muscarinic acetylcholine receptor: more similarities than differences between the structurally divergent agents gallamine and bis(ammonio)alkane-type hexamethylene-bis-[dimethyl-(3-phthalimidopropyl)ammonium]dibromide. Mol Pharmacol. 2005 Sep;68(3):769-78. Epub 2005 Jun 3. [PubMed:15937215 ]
  2. De Vries B, Roffel AF, Kooistra JM, Meurs H, Zaagsma J: Effects of fenoterol on beta-adrenoceptor and muscarinic M2 receptor function in bovine tracheal smooth muscle. Eur J Pharmacol. 2001 May 11;419(2-3):253-9. [PubMed:11426849 ]
  3. Cembala TM, Forde SC, Appadu BL, Lambert DG: Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors. Eur J Pharmacol. 2007 Aug 13;569(1-2):37-40. Epub 2007 May 22. [PubMed:17588565 ]
  4. Ten Berge RE, Krikke M, Teisman AC, Roffel AF, Zaagsma J: Dysfunctional muscarinic M2 autoreceptors in vagally induced bronchoconstriction of conscious guinea pigs after the early allergic reaction. Eur J Pharmacol. 1996 Dec 27;318(1):131-9. [PubMed:9007524 ]
  5. Spina D, Minshall E, Goldie RG, Page CP: The effect of allosteric antagonists in modulating muscarinic M2-receptor function in guinea-pig isolated trachea. Br J Pharmacol. 1994 Jul;112(3):901-5. [PubMed:7522861 ]
  6. Redka DS, Pisterzi LF, Wells JW: Binding of orthosteric ligands to the allosteric site of the M(2) muscarinic cholinergic receptor. Mol Pharmacol. 2008 Sep;74(3):834-43. doi: 10.1124/mol.108.048074. Epub 2008 Jun 13. [PubMed:18552124 ]
  7. Maier-Peuschel M, Frolich N, Dees C, Hommers LG, Hoffmann C, Nikolaev VO, Lohse MJ: A fluorescence resonance energy transfer-based M2 muscarinic receptor sensor reveals rapid kinetics of allosteric modulation. J Biol Chem. 2010 Mar 19;285(12):8793-800. doi: 10.1074/jbc.M109.098517. Epub 2010 Jan 18. [PubMed:20083608 ]
  8. Ehlert FJ, Griffin MT: Two-state models and the analysis of the allosteric effect of gallamine at the M2 muscarinic receptor. J Pharmacol Exp Ther. 2008 Jun;325(3):1039-60. doi: 10.1124/jpet.108.136960. Epub 2008 Feb 27. [PubMed:18305010 ]
  9. Elsinghorst PW, Cieslik JS, Mohr K, Trankle C, Gutschow M: First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. J Med Chem. 2007 Nov 15;50(23):5685-95. Epub 2007 Oct 18. [PubMed:17944454 ]
  10. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serine hydrolase activity
Specific Function:
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name:
ACHE
Uniprot ID:
P22303
Molecular Weight:
67795.525 Da
References
  1. Radic Z, Taylor P: The influence of peripheral site ligands on the reaction of symmetric and chiral organophosphates with wildtype and mutant acetylcholinesterases. Chem Biol Interact. 1999 May 14;119-120:111-7. [PubMed:10421444 ]
  2. Radic Z, Taylor P: Peripheral site ligands accelerate inhibition of acetylcholinesterase by neutral organophosphates. J Appl Toxicol. 2001 Dec;21 Suppl 1:S13-4. [PubMed:11920914 ]
  3. Robaire B, Kato G: Effects of edrophonium, eserine, decamethonium, d-tubocurarine, and gallamine on the kinetics of membrane-bound and solubilized eel acetylcholinesterase. Mol Pharmacol. 1975 Nov;11(6):722-34. [PubMed:1207670 ]
  4. Seto Y, Shinohara T: Structure-activity relationship of reversible cholinesterase inhibitors including paraquat. Arch Toxicol. 1988 Aug;62(1):37-40. [PubMed:3190453 ]
  5. Bourgeois JP, Betz H, Changuex JP: [Effects of chronic paralysis of chick embryo by flaxedil on the development of the neuromuscular junction]. C R Acad Sci Hebd Seances Acad Sci D. 1978 Mar 13;286(10):773-6. [PubMed:417864 ]
  6. Elsinghorst PW, Cieslik JS, Mohr K, Trankle C, Gutschow M: First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. J Med Chem. 2007 Nov 15;50(23):5685-95. Epub 2007 Oct 18. [PubMed:17944454 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Drug binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name:
CHRNA2
Uniprot ID:
Q15822
Molecular Weight:
59764.82 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Aoshima H, Inoue Y, Hori K: Inhibition of ionotropic neurotransmitter receptors by antagonists: strategy to estimate the association and the dissociation rate constant of antagonists with very strong affinity to the receptors. J Biochem. 1992 Oct;112(4):495-502. [PubMed:1337082 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23