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Identification
NameTreprostinil
Accession NumberDB00374  (APRD01272)
Typesmall molecule
Groupsapproved, investigational
Description

Treprostinil is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension. Treprostinil is marketed as Remodulin®. [Wikipedia]

Structure
Thumb
Synonyms
SynonymLanguageCode
(1R,2R,3aS,9aS)-[[2,3,3a,4,9,9a-hexahydro-2-hydroxy- 1-[(3S)-3-hydroxyoctyl]-1H-benz[f]inden-5-yl] oxy]acetic acidNot AvailableIUPAC
[[(1R,2R,3aS,9aS)-2-Hydroxy-1-[(3S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]naphtalen-5-yl]oxy]acetic acidNot AvailableWHO
TreprostinilFrench/GermanUSAN
TreprostiniloSpanishINN
TreprostinilumLatinINN
UniprostNot AvailableIS
SaltsNot Available
Brand names
NameCompany
OrenitramNot Available
RemodulinUnited Therapeutics
TyvasoUnited Therapeutics
Brand mixturesNot Available
Categories
CAS number81846-19-7
WeightAverage: 390.5131
Monoisotopic: 390.240624198
Chemical FormulaC23H34O5
InChI KeyPAJMKGZZBBTTOY-ZFORQUDYSA-N
InChI
InChI=1S/C23H34O5/c1-2-3-4-7-17(24)9-10-18-19-11-15-6-5-8-22(28-14-23(26)27)20(15)12-16(19)13-21(18)25/h5-6,8,16-19,21,24-25H,2-4,7,9-14H2,1H3,(H,26,27)/t16-,17-,18+,19-,21+/m0/s1
IUPAC Name
2-{[(1R,2R,3aS,9aS)-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H,2H,3H,3aH,4H,9H,9aH-cyclopenta[b]naphthalen-5-yl]oxy}acetic acid
SMILES
[H][C@]12C[C@@H](O)[C@H](CC[C@@H](O)CCCCC)[C@@]1([H])CC1=C(C2)C(OCC(O)=O)=CC=C1
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassBenzenoids
ClassBenzene and Substituted Derivatives
SubclassPhenoxyacetic Acid Derivatives
Direct parentPhenoxyacetic Acid Derivatives
Alternative parentsTetralins; Fatty Alcohols; Phenol Ethers; Alkyl Aryl Ethers; Secondary Alcohols; Cyclic Alcohols and Derivatives; Enolates; Carboxylic Acids; Polyamines
Substituentsfatty alcohol; phenol ether; alkyl aryl ether; cyclic alcohol; secondary alcohol; ether; enolate; polyamine; carboxylic acid; carboxylic acid derivative; alcohol
Classification descriptionThis compound belongs to the phenoxyacetic acid derivatives. These are compounds containing an anisole where the methane group is linked to an acetic acid or a derivative.
Pharmacology
IndicationFor use as a continuous subcutaneous infusion or intravenous infusion (for those not able to tolerate a subcutaneous infusion) for the treatment of pulmonary arterial hypertension in patients with NYHA Class II-IV symptoms to diminish symptoms associated with exercise.
PharmacodynamicsPulmonary arterial hypertension (PAH) is a disease in which blood pressure is abnormally high in the arteries between the heart and lungs. PAH is characterized by symptoms of shortness of breath during physical exertion. The condition can ultimately lead to heart failure. Treprostinil is a potent oral antiplatelet agent. The major pharmacologic actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In animals, the vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume. Other studies have shown that treprostinil causes a dose-related negative inotropic and lusitropic effect. No major effects on cardiac conduction have been observed.
Mechanism of actionThe major pharmacological actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In addition to treprostinil's direct vasodilatory effects, it also inhibits inflammatory cytokine. As a synthetic analogue of prostacyclin, it binds to the prostacyclin receptor, which subsequently induces the aforementioned downstream effects.
AbsorptionRelatively rapid and complete after subcutaneous infusion, with an absolute bioavailability approximately 100%. In patients with mild (n=4) or moderate (n=5) hepatic insufficiency and portopulmonary hypertension following a subcutaneous dose of 10 ng per kg of body weight per min for 150 mins the AUC 0-∞ was increased 3-fold and 5-fold respectively.
Volume of distribution
  • 14 L/70 kg
Protein bindingHuman plasma protein binding is approximately 91% in in vitro concentrations ranging from 330 to 10,000 µ/L.
Metabolism

Substantially metabolized by the liver, but the precise enzymes responsible are unknown. Five metabolites have been described (HU1 through HU5) however, the biological activity and metabolic fate of these are unknown. The chemical structure of HU1 is unknown. The metabolite HU5 is the glucuronide conjugate of treprostinil. The other metabolites are formed by oxidation of the 3-hydroxyoctyl side chain (HU2) and subsequent additional oxidation (HU3) or dehydration (HU4). Study results of in vitro human hepatic cytochrome P450 demonstrates that treprostinil does not inhibit CYP-1A2, 2C9, 2C19, 2D6, 2E1, or 3A. Whether treprostinil induces these enzymes has not been studied.

Route of eliminationNot Available
Half lifeTerminal elimination half-life is approximately 2 to 4 hours. Plasma half-life is 34 and 85 minutes for intravenous and subcutaneous infusion of the drug, respectively.
ClearanceNot Available
ToxicitySymptoms of overdose are extensions of its dose-limiting pharmacologic effects and include flushing, headache, hypotension, nausea, vomiting, and diarrhea. Most events were self-limiting and resolved with reduction or withholding of treprostinil.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.994
Blood Brain Barrier + 0.5541
Caco-2 permeable + 0.5838
P-glycoprotein substrate Substrate 0.7733
P-glycoprotein inhibitor I Non-inhibitor 0.719
P-glycoprotein inhibitor II Non-inhibitor 0.7518
Renal organic cation transporter Non-inhibitor 0.8064
CYP450 2C9 substrate Non-substrate 0.7811
CYP450 2D6 substrate Non-substrate 0.8144
CYP450 3A4 substrate Substrate 0.6538
CYP450 1A2 substrate Inhibitor 0.7312
CYP450 2C9 substrate Non-inhibitor 0.8496
CYP450 2D6 substrate Non-inhibitor 0.9127
CYP450 2C19 substrate Non-inhibitor 0.6214
CYP450 3A4 substrate Non-inhibitor 0.6587
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6885
Ames test Non AMES toxic 0.8716
Carcinogenicity Non-carcinogens 0.9452
Biodegradation Not ready biodegradable 0.7495
Rat acute toxicity 2.0749 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9588
hERG inhibition (predictor II) Inhibitor 0.7664
Pharmacoeconomics
Manufacturers
  • United therapeutics corp
Packagers
Dosage forms
FormRouteStrength
SolutionIntravenous
Prices
Unit descriptionCostUnit
Remodulin 10 mg/ml vial737.0USDml
Remodulin 5 mg/ml vial368.5USDml
Tyvaso inhalation starter kit185.8USDml
Remodulin 2.5 mg/ml vial184.25USDml
Tyvaso 1.74 mg/2.9 ml solution174.55USDml
Tyvaso inhalation refill kit165.68USDml
Remodulin 1 mg/ml vial73.7USDml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States65212121998-11-132018-11-13
United States51532221994-10-062014-10-06
Properties
Statesolid
Experimental Properties
PropertyValueSource
water solubilityInsoluble at 25°CNot Available
logP4.1Not Available
Predicted Properties
PropertyValueSource
water solubility7.31e-03 g/lALOGPS
logP3.53ALOGPS
logP4ChemAxon
logS-4.7ALOGPS
pKa (strongest acidic)3.76ChemAxon
pKa (strongest basic)-1.3ChemAxon
physiological charge-1ChemAxon
hydrogen acceptor count5ChemAxon
hydrogen donor count3ChemAxon
polar surface area86.99ChemAxon
rotatable bond count10ChemAxon
refractivity108ChemAxon
polarizability45.74ChemAxon
number of rings3ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleNoChemAxon
MDDR-like ruleYesChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Hitesh Batra, Raju Penmasta, Vijay Sharma, Sudersan M. Tuladhar, David A. Walsh, “TREPROSTINIL PRODUCTION.” U.S. Patent US20110319641, issued December 29, 2011.

US20110319641
General ReferenceNot Available
External Links
ResourceLink
ChEBI50861
ChEMBLCHEMBL1237119
Therapeutic Targets DatabaseDAP001214
PharmGKBPA164768801
Drug Product Database2246552
RxListhttp://www.rxlist.com/cgi/generic/remodulin.htm
Drugs.comhttp://www.drugs.com/cdi/treprostinil-inhalation-solution.html
WikipediaTreprostinil
ATC CodesB01AC21
AHFS Codes
  • 24:12.92
PDB EntriesNot Available
FDA labelshow(223 KB)
MSDSshow(17.4 KB)
Interactions
Drug Interactions
Drug
AbciximabThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Abciximab. Monitor for increased bleeding during concomitant thearpy.
AcebutololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
AcenocoumarolThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Acenocoumarol. Monitor for increased bleeding during concomitant thearpy.
AcetazolamideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Acetylsalicylic acidThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Acetylsalicylic acid. Monitor for increased bleeding during concomitant thearpy.
AliskirenAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
AmilorideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Aminosalicylic AcidThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Aminosalicylic acid. Monitor for increased bleeding during concomitant thearpy.
AmlodipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Amyl NitriteAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
AnagrelideThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Anagrelide. Monitor for increased bleeding during concomitant thearpy.
ApraclonidineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ArgatrobanThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Argatroban. Monitor for increased bleeding during concomitant thearpy.
AtenololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
BenazeprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
BendroflumethiazideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
BetaxololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
BisoprololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
BivalirudinThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Bivalirudin. Monitor for increased bleeding during concomitant thearpy.
BrimonidineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
BumetanideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
CandesartanAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
CaptoprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
CarteololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
CarvedilolAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
CelecoxibThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Celecoxib. Monitor for increased bleeding during concomitant thearpy.
CeliprololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ChlorothiazideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ChlorthalidoneAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
CilazaprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
CilostazolThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Cilostazol. Monitor for increased bleeding during concomitant thearpy.
CitalopramThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Citalopram. Monitor for increased bleeding during concomitant thearpy.
ClevidipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ClonidineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ClopidogrelThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Clopidogrel. Monitor for increased bleeding during concomitant thearpy.
CyclandelateAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
DexmedetomidineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
DiclofenacThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diclofenac. Monitor for increased bleeding during concomitant thearpy.
DiclofenamideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
DiflunisalThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diflunisal. Monitor for increased bleeding during concomitant thearpy.
DiltiazemAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
DipyridamoleThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Dipyridamole. Monitor for increased bleeding during concomitant thearpy. Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
DoxazosinAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
DrospirenoneAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Drotrecogin alfaThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Drotrecogin alfa. Monitor for increased bleeding during concomitant thearpy.
EnalaprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
EnoxaparinThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Exoxaparin. Monitor for increased bleeding during concomitant thearpy.
EplerenoneAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
EprosartanAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
EptifibatideThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Eptifibatide. Monitor for increased bleeding during concomitant thearpy.
EscitalopramThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Escitalopram. Monitor for increased bleeding during concomitant thearpy.
EsmololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ethacrynic acidAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
EtodolacThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Etodolac. Monitor for increased bleeding during concomitant thearpy.
FelodipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
FenoprofenThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Fenoprofen. Monitor for increased bleeding during concomitant thearpy.
FluoxetineThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluoxetine. Monitor for increased bleeding during concomitant thearpy.
FlurbiprofenThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Flurbiprofen. Monitor for increased bleeding during concomitant thearpy.
FluvoxamineThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluvoxamine. Monitor for increased bleeding during concomitant thearpy.
FosinoprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
FurosemideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
GuanabenzAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
GuanfacineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
HeparinThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Heparin. Monitor for increased bleeding during concomitant thearpy.
HydralazineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
HydrochlorothiazideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
HydroflumethiazideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
IbuprofenThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ibuprofen. Monitor for increased bleeding during concomitant thearpy.
IndapamideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
IndomethacinThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Indomethacin. Monitor for increased bleeding during concomitant thearpy.
IrbesartanAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isosorbide DinitrateAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isosorbide MononitrateAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
IsradipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
KetoprofenThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketoprofen. Monitor for increased bleeding during concomitant thearpy.
KetorolacThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketorolac. Monitor for increased bleeding during concomitant thearpy.
LabetalolAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
LepirudinThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Lepirudin. Monitor for increased bleeding during concomitant thearpy.
LevobunololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
LisinoprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
LosartanAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
LumiracoxibThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Lumiracoxib. Monitor for increased bleeding during concomitant thearpy.
MannitolAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Meclofenamic acidThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meclofenamate. Monitor for increased bleeding during concomitant thearpy.
Mefenamic acidThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Mefenamic acid. Monitor for increased bleeding during concomitant thearpy.
MeloxicamThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meloxicam. Monitor for increased bleeding during concomitant thearpy.
MethazolamideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
MethyclothiazideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
MetipranololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
MetolazoneAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
MetoprololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
MinoxidilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
MoexiprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NabumetoneThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Nabumetone. Monitor for increased bleeding during concomitant thearpy.
NadololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NaproxenThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Naproxen. Monitor for increased bleeding during concomitant thearpy.
NebivololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NesiritideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NicardipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NifedipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NimodipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NisoldipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NitrendipineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NitroglycerinAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
NitroprussideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
OlmesartanAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
OxaprozinThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Oxaprozin. Monitor for increased bleeding during concomitant thearpy.
OxprenololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
PapaverineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ParoxetineThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Paroxetine. Monitor for increased bleeding during concomitant thearpy.
PenbutololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
PerindoprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
PhenoxybenzamineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
PhentolamineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
PindololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
PiroxicamThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Piroxicam. Monitor for increased bleeding during concomitant thearpy.
PolythiazideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
PrazosinAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
QuinaprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
RamiprilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ReserpineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
RivaroxabanThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Rivaroxaban. Monitor for increased bleeding during concomitant thearpy.
SalsalateThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Salsalate. Monitor for increased bleeding during concomitant thearpy.
SertralineThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Sertraline. Monitor for increased bleeding during concomitant thearpy.
SotalolAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
SpironolactoneAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
SulindacThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Sulindac. Monitor for increased bleeding during concomitant thearpy.
TelmisartanAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TerazosinAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tiaprofenic acidThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Tiaprofenic acid. Monitor for increased bleeding during concomitant thearpy.
TiclopidineThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Ticlopidine. Monitor for increased bleeding during concomitant thearpy.
TimololAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TirofibanThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Tirofiban. Monitor for increased bleeding during concomitant thearpy.
TizanidineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TolazolineAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TolmetinThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Tolmetin. Monitor for increased bleeding during concomitant thearpy.
TorasemideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TrandolaprilThe prostacyclin analogue, Treprostinil, may increase the hypotensive effect of Trandolapril.
TriamtereneAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TrichlormethiazideAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
UreaAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
ValsartanAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
VerapamilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
WarfarinThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Warfarin. Monitor for increased bleeding during concomitant thearpy.
Food InteractionsNot Available

Targets

1. Prostacyclin receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Prostacyclin receptor P43119 Details

References:

  1. Falcetti E, Hall SM, Phillips PG, Patel J, Morrell NW, Haworth SG, Clapp LH: Smooth Muscle Proliferation and Role of the Prostacyclin (IP) Receptor in Idiopathic Pulmonary Arterial Hypertension. Am J Respir Crit Care Med. 2010 Jul 9. Pubmed
  2. Sprague RS, Bowles EA, Hanson MS, DuFaux EA, Sridharan M, Adderley S, Ellsworth ML, Stephenson AH: Prostacyclin analogs stimulate receptor-mediated cAMP synthesis and ATP release from rabbit and human erythrocytes. Microcirculation. 2008 Jul;15(5):461-71. Pubmed
  3. Olschewski H, Rose F, Schermuly R, Ghofrani HA, Enke B, Olschewski A, Seeger W: Prostacyclin and its analogues in the treatment of pulmonary hypertension. Pharmacol Ther. 2004 May;102(2):139-53. Pubmed
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Peroxisome proliferator-activated receptor delta

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Peroxisome proliferator-activated receptor delta Q03181 Details

References:

  1. Ali FY, Egan K, FitzGerald GA, Desvergne B, Wahli W, Bishop-Bailey D, Warner TD, Mitchell JA: Role of prostacyclin versus peroxisome proliferator-activated receptor beta receptors in prostacyclin sensing by lung fibroblasts. Am J Respir Cell Mol Biol. 2006 Feb;34(2):242-6. Epub 2005 Oct 20. Pubmed

3. P2Y purinoceptor 12

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
P2Y purinoceptor 12 Q9H244 Details

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
  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

Enzymes

1. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Gotzkowsky SK, Dingemanse J, Lai A, Mottola D, Laliberte K: Lack of a pharmacokinetic interaction between oral treprostinil and bosentan in healthy adult volunteers. J Clin Pharmacol. 2010 Jul;50(7):829-34. doi: 10.1177/0091270009351173. Epub 2010 Feb 4. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:10