You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameDolasetron
Accession NumberDB00757  (APRD00518)
TypeSmall Molecule
GroupsApproved
DescriptionDolasetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. This drug is not shown to have activity at other known serotonin receptors, and has low affinity for dopamine receptors.
Structure
Thumb
Synonyms
Dolasetron
Dolasétron
Dolasetron
Dolasetronum
External Identifiers
  • MDL 73147 EF
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Anzemettablet, film coated50 mg/1oralSanofi Aventis U.S. Llc1997-09-11Not applicableUs
Anzemetinjection500 mg/25mLintravenousSanofi Aventis U.S. Llc1997-09-11Not applicableUs
Anzemettablet, film coated100 mg/1oralSanofi Aventis U.S. Llc1997-09-11Not applicableUs
Anzemettablet50 mgoralSanofi Aventis Canada Inc1997-08-262010-01-01Canada
Anzemetinjection100 mg/5mLintravenousSanofi Aventis U.S. Llc1997-09-11Not applicableUs
Anzemettablet100 mgoralSanofi Aventis Canada Inc1997-08-262014-04-21Canada
Anzemetinjection12.5 mg/.625mLintravenousSanofi Aventis U.S. Llc1997-09-11Not applicableUs
Anzemet Injection 20 mg/mlsolution20 mgintravenousSanofi Aventis Canada Inc1997-09-022011-08-15Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AnemetSanofi-Aventis
ZamanonSanofi-Aventis
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Dolasetron Mesylate
ThumbNot applicableDBSALT000959
Categories
UNII82WI2L7Q6E
CAS number115956-12-2
WeightAverage: 324.38
Monoisotopic: 324.147392512
Chemical FormulaC19H20N2O3
InChI KeyUKTAZPQNNNJVKR-KJGYPYNMSA-N
InChI
InChI=1S/C19H20N2O3/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17/h1-4,9,11-14,20H,5-8,10H2/t11-,12-,13+,14+
IUPAC Name
(1s,3R,5r,7S)-10-oxo-8-azatricyclo[5.3.1.0³,⁸]undecan-5-yl 1H-indole-3-carboxylate
SMILES
[H][C@@]1(C[C@@]2([H])C[C@]3([H])C[C@@]([H])(C1)N2CC3=O)OC(=O)C1=CNC2=C1C=CC=C2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as indolecarboxylic acids and derivatives. These are compounds containing a carboxylic acid group (or a derivative thereof) linked to an indole.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassIndolecarboxylic acids and derivatives
Direct ParentIndolecarboxylic acids and derivatives
Alternative Parents
Substituents
  • Indolecarboxylic acid derivative
  • Quinolizidine
  • Indole
  • Quinuclidone
  • Pyrrole-3-carboxylic acid or derivatives
  • Quinuclidine
  • Piperidinone
  • Piperidine
  • Substituted pyrrole
  • Benzenoid
  • Vinylogous amide
  • Heteroaromatic compound
  • Pyrrole
  • Amino acid or derivatives
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid ester
  • Ketone
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organic oxygen compound
  • Organic nitrogen compound
  • Organooxygen compound
  • Amine
  • Carbonyl group
  • Organic oxide
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, including initial and repeat courses of chemotherapy. Also used for the prevention of postoperative nausea and vomiting. This drug can be used intravenously for the treatment of postoperative nausea and vomiting.
PharmacodynamicsDolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. It is structurally and pharmacologically related to other 5-HT3 receptor agonists. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. It is suggested that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.
Mechanism of actionDolasetron is a selective serotonin 5-HT3 receptor antagonist. In vivo, the drug is rapidly converted into its major active metabolite, hydrodolasetron, which seems to be largely responsible for the drug's pharmacological activity. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
Related Articles
AbsorptionOrally-administered dolasetron is well absorbed
Volume of distribution
  • 5.8 L/kg [adults]
Protein binding69-77%
Metabolism

Hepatic

Route of eliminationHydrodolasetron is eliminated by multiple routes, including renal excretion and, after metabolism, mainly glucuronidation, and hydroxylation.
Half life8.1 hours
Clearance
  • Apparent cl=9.4 mL/min/kg [Healthy volunteers with IV treatment dose up to 5 mg/kg]
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+0.9956
Blood Brain Barrier+0.9403
Caco-2 permeable+0.5119
P-glycoprotein substrateNon-substrate0.5833
P-glycoprotein inhibitor IInhibitor0.5344
P-glycoprotein inhibitor IINon-inhibitor0.5225
Renal organic cation transporterInhibitor0.5
CYP450 2C9 substrateNon-substrate0.8569
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.5387
CYP450 1A2 substrateInhibitor0.5293
CYP450 2C9 inhibitorNon-inhibitor0.6846
CYP450 2D6 inhibitorNon-inhibitor0.9093
CYP450 2C19 inhibitorNon-inhibitor0.7741
CYP450 3A4 inhibitorNon-inhibitor0.8272
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5698
Ames testNon AMES toxic0.6931
CarcinogenicityNon-carcinogens0.9407
BiodegradationNot ready biodegradable0.9963
Rat acute toxicity2.5853 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8902
hERG inhibition (predictor II)Non-inhibitor0.7459
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Sanofi aventis us llc
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous100 mg/5mL
Injectionintravenous12.5 mg/.625mL
Injectionintravenous500 mg/25mL
Tabletoral100 mg
Tabletoral50 mg
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral50 mg/1
Solutionintravenous20 mg
Prices
Unit descriptionCostUnit
Anzemet 100 mg tablet77.77USD tablet
Anzemet 50 mg tablet58.67USD tablet
Anzemet 100 mg Tablet32.16USD tablet
Anzemet 12.5 mg carpuject18.74USD syringe
Anzemet 20 mg/ml2.66USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1329203 No1994-05-032011-05-03Canada
US4906755 No1994-07-022011-07-02Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point278 °CNot Available
water solubilityFreely soluble in waterNot Available
logP2.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.261 mg/mLALOGPS
logP2.41ALOGPS
logP2.33ChemAxon
logS-3.1ALOGPS
pKa (Strongest Acidic)12.18ChemAxon
pKa (Strongest Basic)5.68ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area62.4 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity89.34 m3·mol-1ChemAxon
Polarizability35.02 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Janos Hajko, Tivadar Tamas, Adrienne Kovacsne-Mezei, Erika Molnarne, Csaba Peto, Csaba Szabo, “Production of dolasetron.” U.S. Patent US20070203219, issued August 30, 2007.

US20070203219
General References
  1. Balfour JA, Goa KL: Dolasetron. A review of its pharmacology and therapeutic potential in the management of nausea and vomiting induced by chemotherapy, radiotherapy or surgery. Drugs. 1997 Aug;54(2):273-98. [PubMed:9257083 ]
  2. Gregory RE, Ettinger DS: 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy. Drugs. 1998 Feb;55(2):173-89. [PubMed:9506240 ]
  3. Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. [PubMed:15740177 ]
External Links
ATC CodesA04AA04
AHFS Codes
  • 56:22.20
PDB EntriesNot Available
FDA labelDownload (93.3 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe metabolism of Dolasetron can be decreased when combined with Abiraterone.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Dolasetron.
AlmotriptanDolasetron may increase the serotonergic activities of Almotriptan.
AmantadineAmantadine may increase the QTc-prolonging activities of Dolasetron.
AmiodaroneDolasetron may increase the QTc-prolonging activities of Amiodarone.
AmiodaroneThe metabolism of Dolasetron can be decreased when combined with Amiodarone.
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Dolasetron.
AmitriptylineDolasetron may increase the serotonergic activities of Amitriptyline.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Dolasetron.
AmoxapineDolasetron may increase the serotonergic activities of Amoxapine.
AnagrelideDolasetron may increase the QTc-prolonging activities of Anagrelide.
ApomorphineDolasetron may increase the hypotensive activities of Apomorphine.
ApomorphineApomorphine may increase the QTc-prolonging activities of Dolasetron.
AprepitantThe serum concentration of Dolasetron can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Dolasetron.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Dolasetron.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Dolasetron.
Arsenic trioxideDolasetron may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherDolasetron may increase the QTc-prolonging activities of Artemether.
ArtemetherThe metabolism of Dolasetron can be decreased when combined with Artemether.
AsenapineDolasetron may increase the QTc-prolonging activities of Asenapine.
AtazanavirAtazanavir may increase the QTc-prolonging activities of Dolasetron.
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Dolasetron.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Dolasetron.
BedaquilineDolasetron may increase the QTc-prolonging activities of Bedaquiline.
BetaxololThe metabolism of Dolasetron can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Dolasetron can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Dolasetron can be decreased when combined with Boceprevir.
BortezomibBortezomib may increase the QTc-prolonging activities of Dolasetron.
BosentanThe serum concentration of Dolasetron can be decreased when it is combined with Bosentan.
BromocriptineDolasetron may increase the serotonergic activities of Bromocriptine.
BupropionThe metabolism of Dolasetron can be decreased when combined with Bupropion.
BuserelinBuserelin may increase the QTc-prolonging activities of Dolasetron.
BuspironeDolasetron may increase the serotonergic activities of Buspirone.
CabergolineDolasetron may increase the serotonergic activities of Cabergoline.
CapecitabineThe metabolism of Dolasetron can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Dolasetron can be increased when combined with Carbamazepine.
CelecoxibThe metabolism of Dolasetron can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Dolasetron can be increased when it is combined with Ceritinib.
CeritinibDolasetron may increase the QTc-prolonging activities of Ceritinib.
ChloroquineDolasetron may increase the QTc-prolonging activities of Chloroquine.
ChloroquineThe metabolism of Dolasetron can be decreased when combined with Chloroquine.
ChlorpromazineDolasetron may increase the QTc-prolonging activities of Chlorpromazine.
ChlorpromazineThe metabolism of Dolasetron can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Dolasetron can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Dolasetron can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Dolasetron can be decreased when combined with Cinacalcet.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Dolasetron.
CisaprideDolasetron may increase the QTc-prolonging activities of Cisapride.
CitalopramDolasetron may increase the QTc-prolonging activities of Citalopram.
CitalopramThe metabolism of Dolasetron can be decreased when combined with Citalopram.
ClarithromycinDolasetron may increase the QTc-prolonging activities of Clarithromycin.
ClemastineThe metabolism of Dolasetron can be decreased when combined with Clemastine.
ClobazamThe metabolism of Dolasetron can be decreased when combined with Clobazam.
ClomipramineClomipramine may increase the QTc-prolonging activities of Dolasetron.
ClomipramineDolasetron may increase the serotonergic activities of Clomipramine.
ClotrimazoleThe metabolism of Dolasetron can be decreased when combined with Clotrimazole.
ClozapineDolasetron may increase the QTc-prolonging activities of Clozapine.
ClozapineThe metabolism of Dolasetron can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Dolasetron can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Dolasetron can be decreased when combined with Cocaine.
ConivaptanThe serum concentration of Dolasetron can be increased when it is combined with Conivaptan.
CrizotinibDolasetron may increase the QTc-prolonging activities of Crizotinib.
CrizotinibThe metabolism of Dolasetron can be decreased when combined with Crizotinib.
CyclobenzaprineDolasetron may increase the serotonergic activities of Cyclobenzaprine.
CyclosporineThe metabolism of Dolasetron can be decreased when combined with Cyclosporine.
DabrafenibDabrafenib may increase the QTc-prolonging activities of Dolasetron.
DarifenacinThe metabolism of Dolasetron can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Dolasetron can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Dolasetron can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Dolasetron can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Dolasetron.
DelavirdineThe metabolism of Dolasetron can be decreased when combined with Delavirdine.
DesfluraneDesflurane may increase the QTc-prolonging activities of Dolasetron.
DesipramineDesipramine may increase the QTc-prolonging activities of Dolasetron.
DesipramineDolasetron may increase the serotonergic activities of Desipramine.
DesvenlafaxineDolasetron may increase the serotonergic activities of Desvenlafaxine.
DexamethasoneThe serum concentration of Dolasetron can be decreased when it is combined with Dexamethasone.
DextromethorphanDolasetron may increase the serotonergic activities of Dextromethorphan.
DihydroergotamineThe metabolism of Dolasetron can be decreased when combined with Dihydroergotamine.
DihydroergotamineDolasetron may increase the serotonergic activities of Dihydroergotamine.
DiltiazemThe metabolism of Dolasetron can be decreased when combined with Diltiazem.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Dolasetron.
DisopyramideDolasetron may increase the QTc-prolonging activities of Disopyramide.
DofetilideDolasetron may increase the QTc-prolonging activities of Dofetilide.
DomperidoneDolasetron may increase the QTc-prolonging activities of Domperidone.
DoxepinDoxepin may increase the QTc-prolonging activities of Dolasetron.
DoxepinDolasetron may increase the serotonergic activities of Doxepin.
DoxycyclineThe metabolism of Dolasetron can be decreased when combined with Doxycycline.
DronedaroneDolasetron may increase the QTc-prolonging activities of Dronedarone.
DronedaroneThe metabolism of Dolasetron can be decreased when combined with Dronedarone.
DroperidolDroperidol may increase the QTc-prolonging activities of Dolasetron.
DuloxetineDolasetron may increase the serotonergic activities of Duloxetine.
DuloxetineThe metabolism of Dolasetron can be decreased when combined with Duloxetine.
EfavirenzThe serum concentration of Dolasetron can be decreased when it is combined with Efavirenz.
EletriptanDolasetron may increase the serotonergic activities of Eletriptan.
EliglustatDolasetron may increase the QTc-prolonging activities of Eliglustat.
EliglustatThe metabolism of Dolasetron can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Dolasetron can be decreased when it is combined with Enzalutamide.
Ergoloid mesylateDolasetron may increase the serotonergic activities of Ergoloid mesylate.
ErgonovineDolasetron may increase the serotonergic activities of Ergonovine.
ErgotamineDolasetron may increase the serotonergic activities of Ergotamine.
EribulinEribulin may increase the QTc-prolonging activities of Dolasetron.
ErythromycinDolasetron may increase the QTc-prolonging activities of Erythromycin.
ErythromycinThe metabolism of Dolasetron can be decreased when combined with Erythromycin.
EscitalopramDolasetron may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Dolasetron can be decreased when it is combined with Eslicarbazepine acetate.
EtravirineThe serum concentration of Dolasetron can be decreased when it is combined with Etravirine.
EzogabineEzogabine may increase the QTc-prolonging activities of Dolasetron.
FamotidineFamotidine may increase the QTc-prolonging activities of Dolasetron.
FelbamateFelbamate may increase the QTc-prolonging activities of Dolasetron.
FentanylDolasetron may increase the serotonergic activities of Fentanyl.
FingolimodFingolimod may increase the QTc-prolonging activities of Dolasetron.
FlecainideDolasetron may increase the QTc-prolonging activities of Flecainide.
FloxuridineThe metabolism of Dolasetron can be decreased when combined with Floxuridine.
FluconazoleFluconazole may increase the QTc-prolonging activities of Dolasetron.
FluorouracilThe metabolism of Dolasetron can be decreased when combined with Fluorouracil.
FluoxetineDolasetron may increase the QTc-prolonging activities of Fluoxetine.
FluoxetineThe metabolism of Dolasetron can be decreased when combined with Fluoxetine.
FlupentixolDolasetron may increase the QTc-prolonging activities of Flupentixol.
FluvastatinThe metabolism of Dolasetron can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Dolasetron can be decreased when combined with Fluvoxamine.
FluvoxamineDolasetron may increase the serotonergic activities of Fluvoxamine.
FormoterolFormoterol may increase the QTc-prolonging activities of Dolasetron.
FosamprenavirThe metabolism of Dolasetron can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Dolasetron can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Dolasetron.
FosphenytoinThe metabolism of Dolasetron can be increased when combined with Fosphenytoin.
FrovatriptanDolasetron may increase the serotonergic activities of Frovatriptan.
Fusidic AcidThe serum concentration of Dolasetron can be increased when it is combined with Fusidic Acid.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Dolasetron.
GalantamineGalantamine may increase the QTc-prolonging activities of Dolasetron.
GemfibrozilThe metabolism of Dolasetron can be decreased when combined with Gemfibrozil.
GemifloxacinDolasetron may increase the QTc-prolonging activities of Gemifloxacin.
GoserelinGoserelin may increase the QTc-prolonging activities of Dolasetron.
GranisetronDolasetron may increase the QTc-prolonging activities of Granisetron.
HaloperidolDolasetron may increase the QTc-prolonging activities of Haloperidol.
HaloperidolThe metabolism of Dolasetron can be decreased when combined with Haloperidol.
HistrelinHistrelin may increase the QTc-prolonging activities of Dolasetron.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Dolasetron.
IbandronateIbandronate may increase the QTc-prolonging activities of Dolasetron.
IbutilideDolasetron may increase the QTc-prolonging activities of Ibutilide.
IdelalisibThe serum concentration of Dolasetron can be increased when it is combined with Idelalisib.
IloperidoneDolasetron may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe metabolism of Dolasetron can be decreased when combined with Imatinib.
ImipramineImipramine may increase the QTc-prolonging activities of Dolasetron.
ImipramineDolasetron may increase the serotonergic activities of Imipramine.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Dolasetron.
IndapamideIndapamide may increase the QTc-prolonging activities of Dolasetron.
IndinavirThe metabolism of Dolasetron can be decreased when combined with Indinavir.
IrbesartanThe metabolism of Dolasetron can be decreased when combined with Irbesartan.
IsavuconazoniumThe metabolism of Dolasetron can be decreased when combined with Isavuconazonium.
IsocarboxazidDolasetron may increase the serotonergic activities of Isocarboxazid.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Dolasetron.
IsoniazidThe metabolism of Dolasetron can be decreased when combined with Isoniazid.
IsradipineIsradipine may increase the QTc-prolonging activities of Dolasetron.
ItraconazoleItraconazole may increase the QTc-prolonging activities of Dolasetron.
IvabradineIvabradine may increase the QTc-prolonging activities of Dolasetron.
IvacaftorThe serum concentration of Dolasetron can be increased when it is combined with Ivacaftor.
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Dolasetron.
LapatinibLapatinib may increase the QTc-prolonging activities of Dolasetron.
LeflunomideThe metabolism of Dolasetron can be decreased when combined with Leflunomide.
LenvatinibDolasetron may increase the QTc-prolonging activities of Lenvatinib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Dolasetron.
LevofloxacinDolasetron may increase the QTc-prolonging activities of Levofloxacin.
LevomilnacipranDolasetron may increase the serotonergic activities of Levomilnacipran.
LinezolidDolasetron may increase the serotonergic activities of Linezolid.
LithiumLithium may increase the QTc-prolonging activities of Dolasetron.
LithiumDolasetron may increase the serotonergic activities of Lithium.
LopinavirDolasetron may increase the QTc-prolonging activities of Lopinavir.
LopinavirThe metabolism of Dolasetron can be decreased when combined with Lopinavir.
LorcaserinDolasetron may increase the serotonergic activities of Lorcaserin.
LorcaserinThe metabolism of Dolasetron can be decreased when combined with Lorcaserin.
LosartanThe metabolism of Dolasetron can be decreased when combined with Losartan.
LovastatinThe metabolism of Dolasetron can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Dolasetron can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Dolasetron can be decreased when it is combined with Lumacaftor.
LumefantrineDolasetron may increase the QTc-prolonging activities of Lumefantrine.
LumefantrineThe metabolism of Dolasetron can be decreased when combined with Lumefantrine.
MaprotilineMaprotiline may increase the QTc-prolonging activities of Dolasetron.
MaprotilineDolasetron may increase the serotonergic activities of Maprotiline.
MefloquineMefloquine may increase the QTc-prolonging activities of Dolasetron.
MequitazineDolasetron may increase the arrhythmogenic activities of Mequitazine.
MethadoneDolasetron may increase the serotonergic activities of Methadone.
MethadoneThe metabolism of Dolasetron can be decreased when combined with Methadone.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Dolasetron.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Dolasetron.
MetoprololThe metabolism of Dolasetron can be decreased when combined with Metoprolol.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Dolasetron.
MifepristoneMifepristone may increase the QTc-prolonging activities of Dolasetron.
MilnacipranDolasetron may increase the serotonergic activities of Milnacipran.
MirabegronMirabegron may increase the QTc-prolonging activities of Dolasetron.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Dolasetron.
MirtazapineDolasetron may increase the serotonergic activities of Mirtazapine.
MitotaneThe serum concentration of Dolasetron can be decreased when it is combined with Mitotane.
MoclobemideDolasetron may increase the serotonergic activities of Moclobemide.
ModafinilThe serum concentration of Dolasetron can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Dolasetron.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Dolasetron.
NafcillinThe serum concentration of Dolasetron can be decreased when it is combined with Nafcillin.
NaratriptanDolasetron may increase the serotonergic activities of Naratriptan.
NefazodoneThe metabolism of Dolasetron can be decreased when combined with Nefazodone.
NefazodoneDolasetron may increase the serotonergic activities of Nefazodone.
NelfinavirNelfinavir may increase the QTc-prolonging activities of Dolasetron.
NetupitantThe serum concentration of Dolasetron can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Dolasetron can be decreased when combined with Nevirapine.
NicardipineNicardipine may increase the QTc-prolonging activities of Dolasetron.
NilotinibDolasetron may increase the QTc-prolonging activities of Nilotinib.
NilotinibThe metabolism of Dolasetron can be decreased when combined with Nilotinib.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Dolasetron.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Dolasetron.
NortriptylineDolasetron may increase the serotonergic activities of Nortriptyline.
OctreotideOctreotide may increase the QTc-prolonging activities of Dolasetron.
OfloxacinDolasetron may increase the QTc-prolonging activities of Ofloxacin.
OlanzapineOlanzapine may increase the QTc-prolonging activities of Dolasetron.
OlaparibThe metabolism of Dolasetron can be decreased when combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Dolasetron.
OmeprazoleThe metabolism of Dolasetron can be decreased when combined with Omeprazole.
OndansetronDolasetron may increase the QTc-prolonging activities of Ondansetron.
OsimertinibThe serum concentration of Dolasetron can be increased when it is combined with Osimertinib.
OxytocinOxytocin may increase the QTc-prolonging activities of Dolasetron.
PalbociclibThe serum concentration of Dolasetron can be increased when it is combined with Palbociclib.
PaliperidoneDolasetron may increase the QTc-prolonging activities of Paliperidone.
PanobinostatDolasetron may increase the arrhythmogenic activities of Panobinostat.
PanobinostatThe metabolism of Dolasetron can be decreased when combined with Panobinostat.
ParoxetineParoxetine may increase the QTc-prolonging activities of Dolasetron.
ParoxetineDolasetron may increase the serotonergic activities of Paroxetine.
PasireotidePasireotide may increase the QTc-prolonging activities of Dolasetron.
PazopanibDolasetron may increase the QTc-prolonging activities of Pazopanib.
Peginterferon alfa-2bThe serum concentration of Dolasetron can be decreased when it is combined with Peginterferon alfa-2b.
PentamidinePentamidine may increase the QTc-prolonging activities of Dolasetron.
PentobarbitalThe metabolism of Dolasetron can be increased when combined with Pentobarbital.
PerflutrenPerflutren may increase the QTc-prolonging activities of Dolasetron.
PethidineDolasetron may increase the serotonergic activities of Pethidine.
PhenelzineDolasetron may increase the serotonergic activities of Phenelzine.
PhenobarbitalThe metabolism of Dolasetron can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Dolasetron can be increased when combined with Phenytoin.
PimozideDolasetron may increase the QTc-prolonging activities of Pimozide.
PosaconazolePosaconazole may increase the QTc-prolonging activities of Dolasetron.
PrimaquineDolasetron may increase the QTc-prolonging activities of Primaquine.
PrimidoneThe metabolism of Dolasetron can be increased when combined with Primidone.
ProcainamideDolasetron may increase the QTc-prolonging activities of Procainamide.
ProcarbazineDolasetron may increase the serotonergic activities of Procarbazine.
PromazineDolasetron may increase the QTc-prolonging activities of Promazine.
PromazineThe metabolism of Dolasetron can be decreased when combined with Promazine.
PromethazinePromethazine may increase the QTc-prolonging activities of Dolasetron.
PromethazineDolasetron may increase the serotonergic activities of Promethazine.
PropafenoneDolasetron may increase the QTc-prolonging activities of Propafenone.
PropofolPropofol may increase the QTc-prolonging activities of Dolasetron.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Dolasetron.
ProtriptylineDolasetron may increase the serotonergic activities of Protriptyline.
PyrimethamineThe metabolism of Dolasetron can be decreased when combined with Pyrimethamine.
QuetiapineDolasetron may increase the QTc-prolonging activities of Quetiapine.
QuinidineDolasetron may increase the QTc-prolonging activities of Quinidine.
QuinidineThe metabolism of Dolasetron can be decreased when combined with Quinidine.
QuinineDolasetron may increase the QTc-prolonging activities of Quinine.
QuinineThe metabolism of Dolasetron can be decreased when combined with Quinine.
RanolazineRanolazine may increase the QTc-prolonging activities of Dolasetron.
RasagilineDolasetron may increase the serotonergic activities of Rasagiline.
RifabutinThe metabolism of Dolasetron can be increased when combined with Rifabutin.
RifampicinThe metabolism of Dolasetron can be increased when combined with Rifampicin.
RifapentineThe metabolism of Dolasetron can be increased when combined with Rifapentine.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Dolasetron.
RisperidoneRisperidone may increase the QTc-prolonging activities of Dolasetron.
RitonavirRitonavir may increase the QTc-prolonging activities of Dolasetron.
RizatriptanDolasetron may increase the serotonergic activities of Rizatriptan.
RolapitantThe metabolism of Dolasetron can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Dolasetron can be decreased when combined with Ropinirole.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Dolasetron.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Dolasetron.
SaquinavirDolasetron may increase the QTc-prolonging activities of Saquinavir.
SecobarbitalThe metabolism of Dolasetron can be increased when combined with Secobarbital.
SelegilineDolasetron may increase the serotonergic activities of Selegiline.
SertralineSertraline may increase the QTc-prolonging activities of Dolasetron.
SertralineDolasetron may increase the serotonergic activities of Sertraline.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Dolasetron.
SildenafilThe metabolism of Dolasetron can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Dolasetron can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Dolasetron can be increased when it is combined with Simeprevir.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Dolasetron.
SorafenibSorafenib may increase the QTc-prolonging activities of Dolasetron.
SotalolDolasetron may increase the QTc-prolonging activities of Sotalol.
St. John's WortThe serum concentration of Dolasetron can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Dolasetron can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Dolasetron can be decreased when combined with Sulfadiazine.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Dolasetron.
SulfisoxazoleDolasetron may increase the QTc-prolonging activities of Sulfisoxazole.
SulfisoxazoleThe metabolism of Dolasetron can be decreased when combined with Sulfisoxazole.
SumatriptanDolasetron may increase the serotonergic activities of Sumatriptan.
SunitinibSunitinib may increase the QTc-prolonging activities of Dolasetron.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Dolasetron.
TapentadolDolasetron may decrease the analgesic activities of Tapentadol.
Tedizolid PhosphateDolasetron may increase the serotonergic activities of Tedizolid Phosphate.
TelaprevirThe metabolism of Dolasetron can be decreased when combined with Telaprevir.
TelavancinDolasetron may increase the QTc-prolonging activities of Telavancin.
TelithromycinDolasetron may increase the QTc-prolonging activities of Telithromycin.
TerbinafineThe metabolism of Dolasetron can be decreased when combined with Terbinafine.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Dolasetron.
TetrabenazineDolasetron may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazineDolasetron may increase the QTc-prolonging activities of Thioridazine.
ThioridazineThe metabolism of Dolasetron can be decreased when combined with Thioridazine.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Dolasetron.
TicagrelorThe metabolism of Dolasetron can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Dolasetron can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Dolasetron can be decreased when combined with Tipranavir.
TizanidineTizanidine may increase the QTc-prolonging activities of Dolasetron.
TocilizumabThe serum concentration of Dolasetron can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Dolasetron can be decreased when combined with Tolbutamide.
TolterodineTolterodine may increase the QTc-prolonging activities of Dolasetron.
ToremifeneDolasetron may increase the QTc-prolonging activities of Toremifene.
TramadolDolasetron may decrease the analgesic activities of Tramadol.
TranylcypromineDolasetron may increase the serotonergic activities of Tranylcypromine.
TranylcypromineThe metabolism of Dolasetron can be decreased when combined with Tranylcypromine.
TrazodoneTrazodone may increase the QTc-prolonging activities of Dolasetron.
TrazodoneDolasetron may increase the serotonergic activities of Trazodone.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Dolasetron.
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Dolasetron.
TrimipramineTrimipramine may increase the QTc-prolonging activities of Dolasetron.
TrimipramineDolasetron may increase the serotonergic activities of Trimipramine.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Dolasetron.
Valproic AcidThe metabolism of Dolasetron can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Dolasetron can be decreased when combined with Valsartan.
VandetanibDolasetron may increase the QTc-prolonging activities of Vandetanib.
VardenafilVardenafil may increase the QTc-prolonging activities of Dolasetron.
VemurafenibDolasetron may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Dolasetron.
VenlafaxineDolasetron may increase the serotonergic activities of Venlafaxine.
VerapamilThe metabolism of Dolasetron can be decreased when combined with Verapamil.
VilanterolVilanterol may increase the QTc-prolonging activities of Dolasetron.
VilazodoneDolasetron may increase the serotonergic activities of Vilazodone.
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Dolasetron.
VorinostatVorinostat may increase the QTc-prolonging activities of Dolasetron.
VortioxetineDolasetron may increase the serotonergic activities of Vortioxetine.
ZafirlukastThe metabolism of Dolasetron can be decreased when combined with Zafirlukast.
ZiprasidoneDolasetron may increase the QTc-prolonging activities of Ziprasidone.
ZiprasidoneThe metabolism of Dolasetron can be decreased when combined with Ziprasidone.
ZolmitriptanDolasetron may increase the serotonergic activities of Zolmitriptan.
ZuclopenthixolDolasetron may increase the QTc-prolonging activities of Zuclopenthixol.
Food Interactions
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Voltage-gated potassium channel activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Gene Name:
HTR3A
Uniprot ID:
P46098
Molecular Weight:
55279.835 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Conroy T, Cappelaere P, Fabbro M, Fauser AA, Splinter TA, Spielmann M, Schneider M, Chevallier B, Goupil A, Chauvergne J, et al.: Acute antiemetic efficacy and safety of dolasetron mesylate, a 5-HT3 antagonist, in cancer patients treated with cisplatin. European Dolasetron Study Group. Am J Clin Oncol. 1994 Apr;17(2):97-102. [PubMed:8141114 ]
  3. Reith MK, Sproles GD, Cheng LK: Human metabolism of dolasetron mesylate, a 5-HT3 receptor antagonist. Drug Metab Dispos. 1995 Aug;23(8):806-12. [PubMed:7493546 ]
  4. Eisenberg P, Figueroa-Vadillo J, Zamora R, Charu V, Hajdenberg J, Cartmell A, Macciocchi A, Grunberg S: Improved prevention of moderately emetogenic chemotherapy-induced nausea and vomiting with palonosetron, a pharmacologically novel 5-HT3 receptor antagonist: results of a phase III, single-dose trial versus dolasetron. Cancer. 2003 Dec 1;98(11):2473-82. [PubMed:14635083 ]
  5. Monaca-Charley C, Stojkovic T, Duhamel A, De Seze J, Ferriby D, Vermersch P: Double-blind crossover study with dolasetron mesilate, a 5-HT3 receptor antagonist in cerebellar syndrome secondary to multiple sclerosis. J Neurol. 2003 Oct;250(10):1190-4. [PubMed:14586600 ]
  6. Boeijinga PH, Galvan M, Baron BM, Dudley MW, Siegel BW, Slone AL: Characterization of the novel 5-HT3 antagonists MDL 73147EF (dolasetron mesilate) and MDL 74156 in NG108-15 neuroblastoma x glioma cells. Eur J Pharmacol. 1992 Aug 14;219(1):9-13. [PubMed:1397053 ]
  7. Balfour JA, Goa KL: Dolasetron. A review of its pharmacology and therapeutic potential in the management of nausea and vomiting induced by chemotherapy, radiotherapy or surgery. Drugs. 1997 Aug;54(2):273-98. [PubMed:9257083 ]
  8. Hui YF, Ignoffo RJ: Dolasetron. A new 5-hydroxytryptamine3 receptor antagonist. Cancer Pract. 1997 Sep-Oct;5(5):324-8. [PubMed:9341357 ]
  9. Gregory RE, Ettinger DS: 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy. Drugs. 1998 Feb;55(2):173-89. [PubMed:9506240 ]
  10. Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. [PubMed:15740177 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Sanwald P, David M, Dow J: Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of dolasetron. Comparison with other indole-containing 5-HT3 antagonists. Drug Metab Dispos. 1996 May;24(5):602-9. [PubMed:8723743 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Janicki PK: Cytochrome P450 2D6 metabolism and 5-hydroxytryptamine type 3 receptor antagonists for postoperative nausea and vomiting. Med Sci Monit. 2005 Oct;11(10):RA322-8. Epub 2005 Sep 26. [PubMed:16192915 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Sanwald P, David M, Dow J: Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of dolasetron. Comparison with other indole-containing 5-HT3 antagonists. Drug Metab Dispos. 1996 May;24(5):602-9. [PubMed:8723743 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23