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Identification
NamePerhexiline
Accession NumberDB01074  (APRD00107)
TypeSmall Molecule
GroupsApproved
Description2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. [PubChem]
Structure
Thumb
Synonyms
(-)-2-(2,2-Dicyclohexylethyl)piperidine
(+)-2-(2,2-Dicyclohexylethyl)piperidine
2-(2,2-Dicyclohexylethyl)piperidine
Perhexilene
Perhexilina
Perhexiline
Perhexilinum
Perhexilline
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIKU65374X44
CAS number6621-47-2
WeightAverage: 277.4879
Monoisotopic: 277.276950125
Chemical FormulaC19H35N
InChI KeyInChIKey=CYXKNKQEMFBLER-UHFFFAOYSA-N
InChI
InChI=1S/C19H35N/c1-3-9-16(10-4-1)19(17-11-5-2-6-12-17)15-18-13-7-8-14-20-18/h16-20H,1-15H2
IUPAC Name
2-(2,2-dicyclohexylethyl)piperidine
SMILES
C(C(C1CCCCC1)C1CCCCC1)C1CCCCN1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as piperidines. These are compounds containing a piperidine ring, which is a saturated aliphatic six-member ring with one nitrogen atom and five carbon atoms.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPiperidines
Sub ClassNot Available
Direct ParentPiperidines
Alternative Parents
Substituents
  • Piperidine
  • Azacycle
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of severe angina pectoris.
PharmacodynamicsUsed in the treatment of unresponsive or refractory angina. Perhexiline increases glucose metabolism at the expense of free-fatty-acid metabolism, enhancing oxygen efficiency during myocardial ischaemia. Perhexiline also potentiates platelet responsiveness to nitric oxide both in patients with angina and patients with acute coronary syndrome. The predominant mechanism of this particular perhexiline effect is an increase in platelet cGMP responsiveness. Perhexiline also may reduce the potential for nitric oxide clearance by neutrophil-derived oxygen. Perhexiline relieves symptoms of angina, improves exercise tolerance, and increases the workload needed to induce ischaemia when used as monotherapy. The primary therapeutic roles for perhexiline are as short-term therapy (less than 3 months duration) in patients with severe ischaemia awaiting coronary revascularisation or long-term therapy in patients with ischaemic symptoms refractory to other therapeutic measures.
Mechanism of actionPerhexiline binds to the mitochondrial enzyme carnitine palmitoyltransferase (CPT)-1 and CPT-2. It acts by shifting myocardial substrate utilisation from long chain fatty acids to carbohydrates through inhibition of CPT-1 and, to a lesser extent, CPT-2, resulting in increased glucose and lactate utilization. This results in increased ATP production for the same O2 consumption as before and consequently increases myocardial efficiency.
Related Articles
AbsorptionWell absorbed (>80%) from the gastrointestinal tract following oral administration.
Volume of distributionNot Available
Protein bindingPerhexiline and its metabolites are highly protein bound (>90%).
Metabolism

The principal metabolites of perhexiline in man are monohydroxyperhexiline (which is excreted, in part, conjugated with glucuronic acid) and dihydroxyperhexiline that accounts for a relatively small proportion of the total metabolites. Two unidentified metabolites have also been found in the faeces. The pharmacological activity of the metabolites is not known. Hydroxylation of perhexiline is controlled by cytochrome P450 2D6 (CY P450 2D6).

SubstrateEnzymesProduct
Perhexiline
Not Available
cis-Hydroxy PerhexilineDetails
Perhexiline
Not Available
MonohydroxyperhexilineDetails
Route of eliminationNot Available
Half lifeVariable and non-linear. Some reports show a half-life of 2-6 days, others indicate it could be as high as 30 days.
ClearanceNot Available
ToxicityOral LD50 rat: 2150 mg/kg; Oral LD50 Mouse: 2641 mg/kg. Short term adverse effects include nausea, transient dizziness, hypoglycaemia in diabetic patients, and torsade de pointes (rare).
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+0.9818
Blood Brain Barrier+0.9796
Caco-2 permeable+0.6799
P-glycoprotein substrateNon-substrate0.5484
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.8888
Renal organic cation transporterInhibitor0.6665
CYP450 2C9 substrateNon-substrate0.8539
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.7558
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8779
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8452
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9548
BiodegradationNot ready biodegradable0.8346
Rat acute toxicity2.7630 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7559
hERG inhibition (predictor II)Non-inhibitor0.6082
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility0.0608 mg/LNot Available
logP6.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.72e-05 mg/mLALOGPS
logP5.87ALOGPS
logP5.53ChemAxon
logS-7ALOGPS
pKa (Strongest Basic)10.58ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area12.03 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity87.23 m3·mol-1ChemAxon
Polarizability36.22 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
MSMass Spectrum (Electron Ionization)splash10-001i-9000000000-e8335ba9964dd32ada29View in MoNA
References
Synthesis Reference

Stephen W. Horgan, Frank P. Palopoli, Edward J. Schwoegler, “Process for preparing 2-(2,2-dicyclohexylethyl)piperidine.” U.S. Patent US4069222, issued August, 1950.

US4069222
General ReferencesNot Available
External Links
ATC CodesC08EX02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (25.6 KB)
Interactions
Drug Interactions
Drug
2-HYDROXY-1,4-NAPHTHOQUINONEThe risk or severity of adverse effects can be increased when 2-HYDROXY-1,4-NAPHTHOQUINONE is combined with Perhexiline.
2-mercaptobenzothiazoleThe risk or severity of adverse effects can be increased when 2-mercaptobenzothiazole is combined with Perhexiline.
AbirateroneThe metabolism of Perhexiline can be decreased when combined with Abiraterone.
AlfuzosinAlfuzosin may increase the hypotensive activities of Perhexiline.
AmiodaroneThe metabolism of Perhexiline can be decreased when combined with Amiodarone.
AmobarbitalThe metabolism of Perhexiline can be increased when combined with Amobarbital.
AmorolfineThe risk or severity of adverse effects can be increased when Amorolfine is combined with Perhexiline.
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Perhexiline.
AN2690The risk or severity of adverse effects can be increased when AN2690 is combined with Perhexiline.
AnidulafunginThe risk or severity of adverse effects can be increased when Anidulafungin is combined with Perhexiline.
AprepitantThe serum concentration of Perhexiline can be increased when it is combined with Aprepitant.
ArtemetherThe metabolism of Perhexiline can be decreased when combined with Artemether.
AtazanavirThe metabolism of Perhexiline can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Perhexiline can be decreased when combined with Atomoxetine.
AtosibanThe risk or severity of adverse effects can be increased when Perhexiline is combined with Atosiban.
Atracurium besylatePerhexiline may increase the neuromuscular blocking activities of Atracurium besylate.
Bafilomycin A1The risk or severity of adverse effects can be increased when Bafilomycin A1 is combined with Perhexiline.
BarbitalThe metabolism of Perhexiline can be increased when combined with Barbital.
Benzoic AcidThe risk or severity of adverse effects can be increased when Benzoic Acid is combined with Perhexiline.
BetaxololThe metabolism of Perhexiline can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Perhexiline can be decreased when it is combined with Bexarotene.
BifonazoleThe risk or severity of adverse effects can be increased when Bifonazole is combined with Perhexiline.
BoceprevirThe metabolism of Perhexiline can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Perhexiline can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Perhexiline can be decreased when it is combined with Bosentan.
BupropionThe metabolism of Perhexiline can be decreased when combined with Bupropion.
ButenafineThe risk or severity of adverse effects can be increased when Butenafine is combined with Perhexiline.
ButoconazoleThe risk or severity of adverse effects can be increased when Butoconazole is combined with Perhexiline.
CandicidinThe risk or severity of adverse effects can be increased when Candicidin is combined with Perhexiline.
CarbamazepineThe metabolism of Perhexiline can be increased when combined with Carbamazepine.
CarvedilolCarvedilol may increase the hypotensive activities of Perhexiline.
CaspofunginThe risk or severity of adverse effects can be increased when Caspofungin is combined with Perhexiline.
CelecoxibThe metabolism of Perhexiline can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Perhexiline can be increased when it is combined with Ceritinib.
CeruleninThe risk or severity of adverse effects can be increased when Cerulenin is combined with Perhexiline.
ChloroquineThe metabolism of Perhexiline can be decreased when combined with Chloroquine.
ChloroxineThe risk or severity of adverse effects can be increased when Chloroxine is combined with Perhexiline.
ChlorpromazineThe metabolism of Perhexiline can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Perhexiline can be decreased when combined with Cholecalciferol.
CiclopiroxThe risk or severity of adverse effects can be increased when Ciclopirox is combined with Perhexiline.
CimetidineThe metabolism of Perhexiline can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Perhexiline can be decreased when combined with Cinacalcet.
CitalopramThe metabolism of Perhexiline can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Perhexiline can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Perhexiline can be decreased when combined with Clemastine.
ClobazamThe metabolism of Perhexiline can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Perhexiline can be decreased when combined with Clomipramine.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Perhexiline.
ClopidogrelThe metabolism of Perhexiline can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Perhexiline can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Perhexiline can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Perhexiline can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Perhexiline can be decreased when combined with Cocaine.
ConivaptanThe serum concentration of Perhexiline can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Perhexiline can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Perhexiline can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Perhexiline can be decreased when it is combined with Dabrafenib.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Perhexiline.
DarifenacinThe metabolism of Perhexiline can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Perhexiline can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Perhexiline can be increased when it is combined with Dasatinib.
Decanoic AcidThe risk or severity of adverse effects can be increased when Decanoic Acid is combined with Perhexiline.
DeferasiroxThe serum concentration of Perhexiline can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Perhexiline can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Perhexiline can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Perhexiline can be decreased when it is combined with Dexamethasone.
DihydroergotamineThe metabolism of Perhexiline can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Perhexiline can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Perhexiline can be decreased when combined with Diphenhydramine.
DoxazosinDoxazosin may increase the hypotensive activities of Perhexiline.
DoxorubicinThe metabolism of Perhexiline can be decreased when combined with Doxorubicin.
DoxycyclineThe metabolism of Perhexiline can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Perhexiline can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Perhexiline can be decreased when combined with Duloxetine.
EconazoleThe risk or severity of adverse effects can be increased when Econazole is combined with Perhexiline.
EfavirenzThe serum concentration of Perhexiline can be decreased when it is combined with Efavirenz.
EfinaconazoleThe risk or severity of adverse effects can be increased when Efinaconazole is combined with Perhexiline.
EliglustatThe metabolism of Perhexiline can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Perhexiline can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Perhexiline can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Perhexiline can be decreased when it is combined with Eslicarbazepine acetate.
EtravirineThe serum concentration of Perhexiline can be decreased when it is combined with Etravirine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Perhexiline.
FluconazoleThe serum concentration of Perhexiline can be increased when it is combined with Fluconazole.
FlucytosineThe risk or severity of adverse effects can be increased when Flucytosine is combined with Perhexiline.
FluoxetineThe metabolism of Perhexiline can be decreased when combined with Fluoxetine.
FluvoxamineThe metabolism of Perhexiline can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Perhexiline can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Perhexiline can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Perhexiline.
FosphenytoinThe metabolism of Perhexiline can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Perhexiline can be increased when it is combined with Fusidic Acid.
GlyphosateThe risk or severity of adverse effects can be increased when Glyphosate is combined with Perhexiline.
GriseofulvinThe risk or severity of adverse effects can be increased when Griseofulvin is combined with Perhexiline.
HaloperidolThe metabolism of Perhexiline can be decreased when combined with Haloperidol.
HaloproginThe risk or severity of adverse effects can be increased when Haloprogin is combined with Perhexiline.
HexetidineThe risk or severity of adverse effects can be increased when Hexetidine is combined with Perhexiline.
HexobarbitalThe metabolism of Perhexiline can be increased when combined with Hexobarbital.
IdelalisibThe serum concentration of Perhexiline can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Perhexiline can be decreased when combined with Imatinib.
ImipramineThe metabolism of Perhexiline can be decreased when combined with Imipramine.
IndinavirThe metabolism of Perhexiline can be decreased when combined with Indinavir.
IndoraminIndoramin may increase the hypotensive activities of Perhexiline.
IsavuconazoniumThe metabolism of Perhexiline can be decreased when combined with Isavuconazonium.
IsoconazoleThe risk or severity of adverse effects can be increased when Isoconazole is combined with Perhexiline.
IsoniazidThe metabolism of Perhexiline can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Perhexiline can be decreased when combined with Isradipine.
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Perhexiline.
IvacaftorThe serum concentration of Perhexiline can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Perhexiline can be decreased when combined with Ketoconazole.
LabetalolLabetalol may increase the hypotensive activities of Perhexiline.
LopinavirThe metabolism of Perhexiline can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Perhexiline can be decreased when combined with Lorcaserin.
LovastatinThe metabolism of Perhexiline can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Perhexiline can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Perhexiline can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Perhexiline can be decreased when combined with Lumefantrine.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Perhexiline is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Perhexiline is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Perhexiline is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Perhexiline is combined with Magnesium Sulfate.
MethadoneThe metabolism of Perhexiline can be decreased when combined with Methadone.
MethohexitalThe metabolism of Perhexiline can be increased when combined with Methohexital.
MethotrimeprazineThe metabolism of Perhexiline can be decreased when combined with Methotrimeprazine.
MethylphenobarbitalThe metabolism of Perhexiline can be increased when combined with Methylphenobarbital.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Perhexiline.
MetoprololThe metabolism of Perhexiline can be decreased when combined with Metoprolol.
MevastatinThe risk or severity of adverse effects can be increased when Mevastatin is combined with Perhexiline.
MicafunginThe risk or severity of adverse effects can be increased when Micafungin is combined with Perhexiline.
MiconazoleThe risk or severity of adverse effects can be increased when Miconazole is combined with Perhexiline.
MifepristoneThe metabolism of Perhexiline can be decreased when combined with Mifepristone.
MiltefosineThe risk or severity of adverse effects can be increased when Miltefosine is combined with Perhexiline.
MirabegronThe metabolism of Perhexiline can be decreased when combined with Mirabegron.
MitotaneThe serum concentration of Perhexiline can be decreased when it is combined with Mitotane.
MivacuriumPerhexiline may increase the neuromuscular blocking activities of Mivacurium.
ModafinilThe serum concentration of Perhexiline can be decreased when it is combined with Modafinil.
MonensinThe risk or severity of adverse effects can be increased when Monensin is combined with Perhexiline.
MyxothiazolThe risk or severity of adverse effects can be increased when Myxothiazol is combined with Perhexiline.
NafcillinThe serum concentration of Perhexiline can be decreased when it is combined with Nafcillin.
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Perhexiline.
NatamycinThe risk or severity of adverse effects can be increased when Natamycin is combined with Perhexiline.
NefazodoneThe metabolism of Perhexiline can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Perhexiline can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Perhexiline can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Perhexiline can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Perhexiline can be decreased when combined with Nicardipine.
NilotinibThe metabolism of Perhexiline can be decreased when combined with Nilotinib.
NitroprussidePerhexiline may increase the hypotensive activities of Nitroprusside.
NitroxolineThe risk or severity of adverse effects can be increased when Nitroxoline is combined with Perhexiline.
NystatinThe risk or severity of adverse effects can be increased when Nystatin is combined with Perhexiline.
OlaparibThe metabolism of Perhexiline can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Perhexiline can be increased when it is combined with Osimertinib.
OxiconazoleThe risk or severity of adverse effects can be increased when Oxiconazole is combined with Perhexiline.
pafuramidineThe risk or severity of adverse effects can be increased when pafuramidine is combined with Perhexiline.
PalbociclibThe serum concentration of Perhexiline can be increased when it is combined with Palbociclib.
PanobinostatThe metabolism of Perhexiline can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Perhexiline can be decreased when combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Perhexiline can be decreased when it is combined with Peginterferon alfa-2b.
PentamidineThe risk or severity of adverse effects can be increased when Pentamidine is combined with Perhexiline.
PentobarbitalThe metabolism of Perhexiline can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Perhexiline can be increased when combined with Phenobarbital.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Perhexiline.
PhenytoinThe metabolism of Perhexiline can be increased when combined with Phenytoin.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Perhexiline.
PrazosinPrazosin may increase the hypotensive activities of Perhexiline.
PrimidoneThe metabolism of Perhexiline can be increased when combined with Primidone.
PromazineThe metabolism of Perhexiline can be decreased when combined with Promazine.
QuazepamThe serum concentration of Perhexiline can be increased when it is combined with Quazepam.
QuinidineThe metabolism of Perhexiline can be decreased when combined with Quinidine.
QuinineThe metabolism of Perhexiline can be decreased when combined with Quinine.
RadicicolThe risk or severity of adverse effects can be increased when Radicicol is combined with Perhexiline.
RanolazineThe metabolism of Perhexiline can be decreased when combined with Ranolazine.
RapacuroniumPerhexiline may increase the neuromuscular blocking activities of Rapacuronium.
RifabutinThe metabolism of Perhexiline can be increased when combined with Rifabutin.
RifampicinThe metabolism of Perhexiline can be increased when combined with Rifampicin.
RifapentineThe metabolism of Perhexiline can be increased when combined with Rifapentine.
RitonavirThe metabolism of Perhexiline can be decreased when combined with Ritonavir.
RolapitantThe metabolism of Perhexiline can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Perhexiline can be decreased when combined with Ropinirole.
Salicylhydroxamic AcidThe risk or severity of adverse effects can be increased when Salicylhydroxamic Acid is combined with Perhexiline.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Perhexiline.
SaquinavirThe metabolism of Perhexiline can be decreased when combined with Saquinavir.
SecobarbitalThe metabolism of Perhexiline can be increased when combined with Secobarbital.
SertaconazoleThe risk or severity of adverse effects can be increased when Sertaconazole is combined with Perhexiline.
SertralineThe metabolism of Perhexiline can be decreased when combined with Sertraline.
SildenafilThe metabolism of Perhexiline can be decreased when combined with Sildenafil.
SilodosinSilodosin may increase the hypotensive activities of Perhexiline.
SiltuximabThe serum concentration of Perhexiline can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Perhexiline can be increased when it is combined with Simeprevir.
SinefunginThe risk or severity of adverse effects can be increased when Sinefungin is combined with Perhexiline.
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Perhexiline.
SorafenibThe metabolism of Perhexiline can be decreased when combined with Sorafenib.
St. John's WortThe serum concentration of Perhexiline can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Perhexiline can be increased when it is combined with Stiripentol.
SulconazoleThe risk or severity of adverse effects can be increased when Sulconazole is combined with Perhexiline.
SulfisoxazoleThe metabolism of Perhexiline can be decreased when combined with Sulfisoxazole.
TamsulosinTamsulosin may increase the hypotensive activities of Perhexiline.
TavaboroleThe risk or severity of adverse effects can be increased when Tavaborole is combined with Perhexiline.
TelaprevirThe metabolism of Perhexiline can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Perhexiline can be decreased when combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Perhexiline.
TerbinafineThe risk or severity of adverse effects can be increased when Terbinafine is combined with Perhexiline.
TerconazoleThe risk or severity of adverse effects can be increased when Terconazole is combined with Perhexiline.
ThiamylalThe metabolism of Perhexiline can be increased when combined with Thiamylal.
ThiopentalThe metabolism of Perhexiline can be increased when combined with Thiopental.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Perhexiline.
ThioridazineThe metabolism of Perhexiline can be decreased when combined with Thioridazine.
ThiotepaThe metabolism of Perhexiline can be decreased when combined with Thiotepa.
ThymolThe risk or severity of adverse effects can be increased when Thymol is combined with Perhexiline.
TiclopidineThe metabolism of Perhexiline can be decreased when combined with Ticlopidine.
TioconazoleThe risk or severity of adverse effects can be increased when Tioconazole is combined with Perhexiline.
TipranavirThe metabolism of Perhexiline can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Perhexiline can be decreased when it is combined with Tocilizumab.
TolnaftateThe risk or severity of adverse effects can be increased when Tolnaftate is combined with Perhexiline.
TranylcypromineThe metabolism of Perhexiline can be decreased when combined with Tranylcypromine.
TrimazosinTrimazosin may increase the hypotensive activities of Perhexiline.
TrimetrexateThe risk or severity of adverse effects can be increased when Trimetrexate is combined with Perhexiline.
VenlafaxineThe metabolism of Perhexiline can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Perhexiline can be decreased when combined with Verapamil.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Perhexiline.
ZiprasidoneThe metabolism of Perhexiline can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Carnitine o-palmitoyltransferase activity
Specific Function:
Catalyzes the transfer of the acyl group of long-chain fatty acid-CoA conjugates onto carnitine, an essential step for the mitochondrial uptake of long-chain fatty acids and their subsequent beta-oxidation in the mitochondrion. Plays an important role in triglyceride metabolism.
Gene Name:
CPT1A
Uniprot ID:
P50416
Molecular Weight:
88366.92 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. Kennedy JA, Kiosoglous AJ, Murphy GA, Pelle MA, Horowitz JD: Effect of perhexiline and oxfenicine on myocardial function and metabolism during low-flow ischemia/reperfusion in the isolated rat heart. J Cardiovasc Pharmacol. 2000 Dec;36(6):794-801. [PubMed:11117381 ]
  4. Unger SA, Kennedy JA, McFadden-Lewis K, Minerds K, Murphy GA, Horowitz JD: Dissociation between metabolic and efficiency effects of perhexiline in normoxic rat myocardium. J Cardiovasc Pharmacol. 2005 Dec;46(6):849-55. [PubMed:16306812 ]
  5. Kennedy JA, Unger SA, Horowitz JD: Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by perhexiline and amiodarone. Biochem Pharmacol. 1996 Jul 26;52(2):273-80. [PubMed:8694852 ]
  6. Ashrafian H, Horowitz JD, Frenneaux MP: Perhexiline. Cardiovasc Drug Rev. 2007 Spring;25(1):76-97. [PubMed:17445089 ]
  7. 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:
Carnitine o-palmitoyltransferase activity
Specific Function:
Not Available
Gene Name:
CPT2
Uniprot ID:
P23786
Molecular Weight:
73776.335 Da
References
  1. Kennedy JA, Kiosoglous AJ, Murphy GA, Pelle MA, Horowitz JD: Effect of perhexiline and oxfenicine on myocardial function and metabolism during low-flow ischemia/reperfusion in the isolated rat heart. J Cardiovasc Pharmacol. 2000 Dec;36(6):794-801. [PubMed:11117381 ]
  2. Unger SA, Kennedy JA, McFadden-Lewis K, Minerds K, Murphy GA, Horowitz JD: Dissociation between metabolic and efficiency effects of perhexiline in normoxic rat myocardium. J Cardiovasc Pharmacol. 2005 Dec;46(6):849-55. [PubMed:16306812 ]
  3. Kennedy JA, Unger SA, Horowitz JD: Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by perhexiline and amiodarone. Biochem Pharmacol. 1996 Jul 26;52(2):273-80. [PubMed:8694852 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. 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 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 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 ]
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. 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 August 17, 2016 12:23