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Identification
NameFrovatriptan
Accession NumberDB00998  (APRD00270)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionFrovatriptan (Frova®) is a triptan drug developed by Vernalis for the treatment of migraine headaches, in particular those associated with menstruation. The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe.[1] Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head. It is available as 2.5 mg tablets. Frovatriptan has mean terminal elimination half-life of approximately 26 hours, which is substantially longer than other triptans. Frovatriptan is available only by prescription in the United States, where a secondary New Drug Approval (sNDA) was filed in July 2006[2] and which is currently pending.[3] The FDA anticipates completing its review of this application on or before the current PDUFA (Prescription Drug User Fee Act) review date of August 19, 2007. If the sNDA is approved, Frova® will be the only medication indicated in the U.S. for the short-term prevention of menstrual migraine (MM).
Structure
Thumb
Synonyms
Allergo filmtabletten
Frovatriptan succinate
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Frovatablet, film coated2.5 mg/1oralEndo Pharmaceuticals Inc.2001-11-08Not applicableUs
Frovatablet, film coated2.5 mg/1oralSTAT Rx USA LLC2001-11-08Not applicableUs
Frovatablet2.5 mgoralEndo Pharmaceuticals Inc2008-01-04Not applicableCanada
Frovatablet, film coated2.5 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-08-18Not applicableUs
Frovatablet, film coated2.5 mg/1oralUnit Dose Services2001-11-08Not applicableUs
Frovatriptan Succinatetablet, film coated2.5 mg/1oralQualitest Pharmaceuticals2015-10-05Not applicableUs
Teva-frovatriptantablet2.5 mgoralEndo Pharmaceuticals Inc2015-01-16Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Frovatriptan Succinatetablet, film coated2.5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2016-03-11Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
FrovelanNot Available
MiguardNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIH82Q2D5WA7
CAS number158747-02-5
WeightAverage: 243.3043
Monoisotopic: 243.137162181
Chemical FormulaC14H17N3O
InChI KeyInChIKey=XPSQPHWEGNHMSK-SECBINFHSA-N
InChI
InChI=1S/C14H17N3O/c1-16-9-3-5-13-11(7-9)10-6-8(14(15)18)2-4-12(10)17-13/h2,4,6,9,16-17H,3,5,7H2,1H3,(H2,15,18)/t9-/m1/s1
IUPAC Name
(3R)-3-(methylamino)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamide
SMILES
CN[C@@H]1CCC2=C(C1)C1=C(N2)C=CC(=C1)C(N)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as carbazoles. These are compounds containing a three ring system containing a pyrrole ring fused on either side to a benzene ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassCarbazoles
Direct ParentCarbazoles
Alternative Parents
Substituents
  • Carbazole
  • Indolecarboxylic acid derivative
  • Indolecarboxamide derivative
  • Indole
  • Benzamide
  • Benzoyl
  • Aralkylamine
  • Benzenoid
  • Heteroaromatic compound
  • Pyrrole
  • Primary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Secondary amine
  • Secondary aliphatic amine
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the acute treatment of migraine attacks with or without aura in adults.
PharmacodynamicsFrovatriptan is a second generation triptan 5-HT receptor agonist that binds with high affinity for 5-HT1B and 5-HT1D receptors. It is structurally distinct from, but pharmacologically related to other selective 5-HT1B/1D receptor agonists. Frovatriptan has no significant effects on GABAA mediated channel activity and has no significant affinity for benzodiazepine binding sites. Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in migraine. Research has shown that migraine can be caused by the swelling of blood vessels around the brain. Frovatriptan eases the pain associated with migraine by narrowing these blood vessels. Frovatriptan has one of the highest affinities for the 5-HT1B of the second-generation triptan agonists.
Mechanism of actionThree distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.
Related Articles
AbsorptionFrovatriptan is rapidly absorbed from the duodenum, but has low oral bioavailability.
Volume of distribution
  • 4.2 L/kg [males]
  • 3 L/kg [females]
Protein bindingBinding to serum proteins is low (approximately 15%). Reversible binding to blood cells at equilibrium is approximately 60%.
Metabolism

In vitro, cytochrome P450 1A2 appears to be the principal enzyme involved in the metabolism of frovatriptan to several metabolites including hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, and several other minor metabolites. Desmethyl frovatriptan has lower affinity for 5-HT1B/1D receptors compared to the parent compound. The N-acetyl desmethyl metabolite has no significant affinity for 5-HT receptors. The activity of the other metabolites is unknown.

SubstrateEnzymesProduct
Frovatriptan
Not Available
desmethyl frovatriptanDetails
Frovatriptan
Not Available
Hydroxylated frovatriptanDetails
Frovatriptan
Not Available
Hydroxylated N-acetyl desmethyl frovatriptanDetails
Frovatriptan
Not Available
N-acetyl desmethyl frovatriptanDetails
Route of eliminationRadiolabeled compounds excreted in urine were unchanged frovatriptan, hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, together with several other minor metabolites. Less than 10% of frovatriptan was excreted in urine after an oral dose.
Half life26 hours
Clearance
  • 220 mL/min [male receiving IV dose of 0.8 mg]
  • 130 mL/min [Female receiving IV dose of 0.8 mg]
ToxicityThere is no direct experience of any patient taking an overdose of Frovatriptan. The maximum single dose of frovatriptan given to male and female patients with migraine was 40 mg (16 times the clinical dose) and the maximum single dose given to healthy male subjects was 100 mg (40 times the clinical dose) without significant adverse events.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3
Gene symbol: GNB3
UniProt: P16520
rs5443 Not AvailableT AlleleBetter response to drug treatment17361120
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9934
Blood Brain Barrier+0.986
Caco-2 permeable-0.5794
P-glycoprotein substrateSubstrate0.602
P-glycoprotein inhibitor INon-inhibitor0.8862
P-glycoprotein inhibitor IINon-inhibitor0.7244
Renal organic cation transporterNon-inhibitor0.6147
CYP450 2C9 substrateNon-substrate0.7785
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5
CYP450 1A2 substrateInhibitor0.6997
CYP450 2C9 inhibitorNon-inhibitor0.8842
CYP450 2D6 inhibitorNon-inhibitor0.8614
CYP450 2C19 inhibitorNon-inhibitor0.6656
CYP450 3A4 inhibitorNon-inhibitor0.5316
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5744
Ames testNon AMES toxic0.7623
CarcinogenicityNon-carcinogens0.9456
BiodegradationNot ready biodegradable0.9406
Rat acute toxicity1.9582 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9878
hERG inhibition (predictor II)Inhibitor0.6428
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Endo pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral2.5 mg
Tablet, film coatedoral2.5 mg/1
Prices
Unit descriptionCostUnit
Frova 9 2.5 mg tablet Box262.31USD box
Frova 2.5 mg tablet33.73USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2113726 No2008-02-192012-06-17Canada
CA2152630 No2005-07-262013-12-16Canada
US5464864 No1995-11-072015-11-07Us
US5827871 No1995-10-272015-10-27Us
US5962501 No1993-12-162013-12-16Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
logP0.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.123 mg/mLALOGPS
logP1.2ALOGPS
logP1.08ChemAxon
logS-3.3ALOGPS
pKa (Strongest Acidic)14.54ChemAxon
pKa (Strongest Basic)10.42ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area70.91 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity71.84 m3·mol-1ChemAxon
Polarizability27.55 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Samir Naik, Anthony Crasto, Narendra Joshi, Sachin Srivastava, “Amorphous frovatriptan succinate and process for the preparation thereof.” U.S. Patent US20070299123, issued December 27, 2007.

US20070299123
General References
  1. Markus F, Mikko K: Frovatriptan review. Expert Opin Pharmacother. 2007 Dec;8(17):3029-33. [PubMed:18001261 ]
  2. Easthope SE, Goa KL: Frovatriptan. CNS Drugs. 2001;15(12):969-76; discussion 977-8. [PubMed:11735616 ]
  3. Balbisi EA: Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine. Ther Clin Risk Manag. 2006 Sep;2(3):303-8. [PubMed:18360605 ]
  4. Balbisi EA: Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine. Int J Clin Pract. 2004 Jul;58(7):695-705. [PubMed:15311727 ]
  5. Elkind AH, Wade A, Ishkanian G: Pharmacokinetics of frovatriptan in adolescent migraineurs. J Clin Pharmacol. 2004 Oct;44(10):1158-65. [PubMed:15342617 ]
  6. Jhee SS, Shiovitz T, Crawford AW, Cutler NR: Pharmacokinetics and pharmacodynamics of the triptan antimigraine agents: a comparative review. Clin Pharmacokinet. 2001;40(3):189-205. [PubMed:11327198 ]
External Links
ATC CodesN02CC07
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (871 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe metabolism of Frovatriptan can be decreased when combined with 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE.
AbirateroneThe serum concentration of Frovatriptan can be increased when it is combined with Abiraterone.
AcepromazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Aceprometazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Acetophenazine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Frovatriptan.
AmisulprideThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Frovatriptan.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Frovatriptan.
AmperozideThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Amperozide.
AripiprazoleThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Aripiprazole.
AsenapineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Asenapine.
AzaperoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Azaperone.
AzithromycinThe metabolism of Frovatriptan can be decreased when combined with Azithromycin.
BenmoxinThe metabolism of Frovatriptan can be decreased when combined with Benmoxin.
BifeprunoxThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Bifeprunox.
BortezomibThe metabolism of Frovatriptan can be decreased when combined with Bortezomib.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Brexpiprazole.
BromocriptineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Bromocriptine.
BromocriptineBromocriptine may increase the vasoconstricting activities of Frovatriptan.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Frovatriptan.
CabergolineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Cabergoline.
CabergolineCabergoline may increase the vasoconstricting activities of Frovatriptan.
CaffeineThe metabolism of Frovatriptan can be decreased when combined with Caffeine.
CarbamazepineThe metabolism of Frovatriptan can be increased when combined with Carbamazepine.
CariprazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Cariprazine.
CaroxazoneThe metabolism of Frovatriptan can be decreased when combined with Caroxazone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Chlorprothixene.
CitalopramThe metabolism of Frovatriptan can be decreased when combined with Citalopram.
CitalopramThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Citalopram.
ClomipramineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Clomipramine.
ClotrimazoleThe metabolism of Frovatriptan can be decreased when combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Clozapine.
CyamemazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Cyamemazine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Frovatriptan.
Cyproterone acetateThe serum concentration of Frovatriptan can be decreased when it is combined with Cyproterone acetate.
DapiprazoleThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Dapiprazole.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Frovatriptan.
DeferasiroxThe serum concentration of Frovatriptan can be increased when it is combined with Deferasirox.
DesipramineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Desipramine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Desvenlafaxine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Frovatriptan.
DihydroergotamineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Dihydroergotamine.
DihydroergotamineDihydroergotamine may increase the vasoconstricting activities of Frovatriptan.
DolasetronDolasetron may increase the serotonergic activities of Frovatriptan.
DoxepinThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Doxepin.
DroperidolThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Droperidol.
DroxidopaFrovatriptan may increase the hypertensive activities of Droxidopa.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Frovatriptan.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Frovatriptan.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Ergoloid mesylate.
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Frovatriptan.
ErgonovineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Ergonovine.
ErgonovineErgonovine may increase the vasoconstricting activities of Frovatriptan.
ErgotamineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Ergotamine.
ErgotamineErgotamine may increase the vasoconstricting activities of Frovatriptan.
EscitalopramThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Escitalopram.
FencamfamineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Fencamfamine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Frovatriptan.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Frovatriptan.
FlupentixolThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Fluspirilene.
FluvoxamineThe metabolism of Frovatriptan can be decreased when combined with Fluvoxamine.
FluvoxamineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Fluvoxamine.
FurazolidoneThe metabolism of Frovatriptan can be decreased when combined with Furazolidone.
GranisetronGranisetron may increase the serotonergic activities of Frovatriptan.
HaloperidolThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Haloperidol.
HydracarbazineThe metabolism of Frovatriptan can be decreased when combined with Hydracarbazine.
IloperidoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Frovatriptan.
IproclozideThe metabolism of Frovatriptan can be decreased when combined with Iproclozide.
IproniazidThe metabolism of Frovatriptan can be decreased when combined with Iproniazid.
IsocarboxazidThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Isocarboxazid.
IsocarboxazidThe metabolism of Frovatriptan can be decreased when combined with Isocarboxazid.
LevomilnacipranThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Levomilnacipran.
LidocaineThe metabolism of Frovatriptan can be decreased when combined with Lidocaine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Frovatriptan.
LithiumThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Lithium.
LorcaserinThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Lorcaserin.
LoxapineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Loxapine.
LurasidoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Lurasidone.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Frovatriptan.
MebanazineThe metabolism of Frovatriptan can be decreased when combined with Mebanazine.
MelperoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Melperone.
MesoridazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Mesoridazine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Frovatriptan.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Methotrimeprazine.
Methylene blueThe metabolism of Frovatriptan can be decreased when combined with Methylene blue.
MetoclopramideThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Metoclopramide.
MexiletineThe metabolism of Frovatriptan can be decreased when combined with Mexiletine.
MilnacipranThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Milnacipran.
MinaprineThe metabolism of Frovatriptan can be decreased when combined with Minaprine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Frovatriptan.
MoclobemideThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Moclobemide.
MoclobemideThe metabolism of Frovatriptan can be decreased when combined with Moclobemide.
MolindoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Molindone.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Frovatriptan.
NefazodoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Nefazodone.
NevirapineThe metabolism of Frovatriptan can be decreased when combined with Nevirapine.
NialamideThe metabolism of Frovatriptan can be decreased when combined with Nialamide.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Frovatriptan.
OctamoxinThe metabolism of Frovatriptan can be decreased when combined with Octamoxin.
OlanzapineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Ondansetron.
OndansetronOndansetron may increase the serotonergic activities of Frovatriptan.
OsanetantThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Osanetant.
OsimertinibThe serum concentration of Frovatriptan can be decreased when it is combined with Osimertinib.
PaliperidoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Paliperidone.
PalonosetronPalonosetron may increase the serotonergic activities of Frovatriptan.
PargylineThe metabolism of Frovatriptan can be decreased when combined with Pargyline.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Frovatriptan.
Peginterferon alfa-2bThe serum concentration of Frovatriptan can be increased when it is combined with Peginterferon alfa-2b.
PerospironeThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Perospirone.
PerphenazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Perphenazine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Frovatriptan.
PhenelzineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Phenelzine.
PhenelzineThe metabolism of Frovatriptan can be decreased when combined with Phenelzine.
PheniprazineThe metabolism of Frovatriptan can be decreased when combined with Pheniprazine.
PhenobarbitalThe metabolism of Frovatriptan can be increased when combined with Phenobarbital.
PhenoxypropazineThe metabolism of Frovatriptan can be decreased when combined with Phenoxypropazine.
PimozideThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Pimozide.
PipamperoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Pipamperone.
PipotiazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Pipotiazine.
PirlindoleThe metabolism of Frovatriptan can be decreased when combined with Pirlindole.
PivhydrazineThe metabolism of Frovatriptan can be decreased when combined with Pivhydrazine.
PrimidoneThe metabolism of Frovatriptan can be increased when combined with Primidone.
ProcarbazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Procarbazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Promazine.
PromethazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Promethazine.
PropericiazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Propericiazine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Frovatriptan.
QuetiapineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Quetiapine.
RasagilineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Rasagiline.
RasagilineThe metabolism of Frovatriptan can be decreased when combined with Rasagiline.
RemoxiprideThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Reserpine.
RifampicinThe metabolism of Frovatriptan can be increased when combined with Rifampicin.
RisperidoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Risperidone.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Frovatriptan.
RopiniroleThe metabolism of Frovatriptan can be decreased when combined with Ropinirole.
SafrazineThe metabolism of Frovatriptan can be decreased when combined with Safrazine.
SelegilineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Selegiline.
SelegilineThe metabolism of Frovatriptan can be decreased when combined with Selegiline.
SertindoleThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Sertraline.
SimeprevirThe metabolism of Frovatriptan can be decreased when combined with Simeprevir.
SulpirideThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Frovatriptan.
TapentadolThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Tapentadol.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Frovatriptan.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Tedizolid Phosphate.
TenofovirThe metabolism of Frovatriptan can be decreased when combined with Tenofovir.
TeriflunomideThe serum concentration of Frovatriptan can be decreased when it is combined with Teriflunomide.
TheophyllineThe metabolism of Frovatriptan can be decreased when combined with Theophylline.
ThioproperazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Thioproperazine.
ThioridazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Thiothixene.
TiclopidineThe metabolism of Frovatriptan can be decreased when combined with Ticlopidine.
ToloxatoneThe metabolism of Frovatriptan can be decreased when combined with Toloxatone.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Frovatriptan.
Trans-2-PhenylcyclopropylamineThe metabolism of Frovatriptan can be decreased when combined with Trans-2-Phenylcyclopropylamine.
TranylcypromineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Tranylcypromine.
TranylcypromineThe metabolism of Frovatriptan can be decreased when combined with Tranylcypromine.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Frovatriptan.
TrifluoperazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Triflupromazine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Frovatriptan.
VemurafenibThe serum concentration of Frovatriptan can be increased when it is combined with Vemurafenib.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Frovatriptan.
VilazodoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Vortioxetine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Ziprasidone.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Frovatriptan.
ZotepineThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Zotepine.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Zuclopenthixol.
Food Interactions
  • Food does not affect amount of absorption but delays maximal levels by about 1 hour.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 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. Easthope SE, Goa KL: Frovatriptan. CNS Drugs. 2001;15(12):969-76; discussion 977-8. [PubMed:11735616 ]
  3. Comer MB: Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan. Headache. 2002 Apr;42 Suppl 2:S47-53. [PubMed:12028320 ]
  4. Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [PubMed:11152011 ]
  5. Deleu D, Hanssens Y: Current and emerging second-generation triptans in acute migraine therapy: a comparative review. J Clin Pharmacol. 2000 Jul;40(7):687-700. [PubMed:10883409 ]
  6. Jahnichen S, Radtke OA, Pertz HH: Involvement of 5-HT1B receptors in triptan-induced contractile responses in guinea-pig isolated iliac artery. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):54-63. Epub 2004 Jun 8. [PubMed:15185063 ]
  7. Balbisi EA: Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine. Int J Clin Pract. 2004 Jul;58(7):695-705. [PubMed:15311727 ]
  8. Parsons AA, Raval P, Smith S, Tilford N, King FD, Kaumann AJ, Hunter J: Effects of the novel high-affinity 5-HT(1B/1D)-receptor ligand frovatriptan in human isolated basilar and coronary arteries. J Cardiovasc Pharmacol. 1998 Aug;32(2):220-4. [PubMed:9700983 ]
  9. Balbisi EA: Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine. Ther Clin Risk Manag. 2006 Sep;2(3):303-8. [PubMed:18360605 ]
  10. Elkind AH, Wade A, Ishkanian G: Pharmacokinetics of frovatriptan in adolescent migraineurs. J Clin Pharmacol. 2004 Oct;44(10):1158-65. [PubMed:15342617 ]
  11. Buchan P, Wade A, Ward C, Oliver SD, Stewart AJ, Freestone S: Frovatriptan: a review of drug-drug interactions. Headache. 2002 Apr;42 Suppl 2:S63-73. [PubMed:12028322 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 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. Balbisi EA: Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine. Int J Clin Pract. 2004 Jul;58(7):695-705. [PubMed:15311727 ]
  3. Comer MB: Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan. Headache. 2002 Apr;42 Suppl 2:S47-53. [PubMed:12028320 ]
  4. Parsons AA, Raval P, Smith S, Tilford N, King FD, Kaumann AJ, Hunter J: Effects of the novel high-affinity 5-HT(1B/1D)-receptor ligand frovatriptan in human isolated basilar and coronary arteries. J Cardiovasc Pharmacol. 1998 Aug;32(2):220-4. [PubMed:9700983 ]
  5. Easthope SE, Goa KL: Frovatriptan. CNS Drugs. 2001;15(12):969-76; discussion 977-8. [PubMed:11735616 ]
  6. Dodick DW, Sandrini G, Williams P: Use of the sustained pain-free plus no adverse events endpoint in clinical trials of triptans in acute migraine. CNS Drugs. 2007;21(1):73-82. [PubMed:17190530 ]
  7. Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. [PubMed:11152011 ]
  8. Deleu D, Hanssens Y: Current and emerging second-generation triptans in acute migraine therapy: a comparative review. J Clin Pharmacol. 2000 Jul;40(7):687-700. [PubMed:10883409 ]
  9. Markus F, Mikko K: Frovatriptan review. Expert Opin Pharmacother. 2007 Dec;8(17):3029-33. [PubMed:18001261 ]
  10. Balbisi EA: Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine. Ther Clin Risk Manag. 2006 Sep;2(3):303-8. [PubMed:18360605 ]
  11. Elkind AH, Wade A, Ishkanian G: Pharmacokinetics of frovatriptan in adolescent migraineurs. J Clin Pharmacol. 2004 Oct;44(10):1158-65. [PubMed:15342617 ]
  12. Buchan P, Wade A, Ward C, Oliver SD, Stewart AJ, Freestone S: Frovatriptan: a review of drug-drug interactions. Headache. 2002 Apr;42 Suppl 2:S63-73. [PubMed:12028322 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Easthope SE, Goa KL: Frovatriptan. CNS Drugs. 2001;15(12):969-76; discussion 977-8. [PubMed:11735616 ]
  2. Buchan P, Keywood C, Wade A, Ward C: Clinical pharmacokinetics of frovatriptan. Headache. 2002 Apr;42 Suppl 2:S54-62. [PubMed:12028321 ]
  3. Buchan P, Wade A, Ward C, Oliver SD, Stewart AJ, Freestone S: Frovatriptan: a review of drug-drug interactions. Headache. 2002 Apr;42 Suppl 2:S63-73. [PubMed:12028322 ]
  4. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on September 24, 2016 02:15