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20-September-2008 09:55:50 - Treprostinil Treprostinil Systematic IUPAC name 1R,2R,3aS,9aS-2,3,3a,4,9,9a-hexahydro-2-hydroxy- 1-3S-3-hydroxyoctyl-1H-benzfinden-5-yl oxyacetic acid monosodium salt Identifiers CAS number ? ATC code B01AC21 PubChem 6918140 Chemical data Formula C23H33NaO5 Mol. mass relative molecular weight is 412.49 g/mol. Pharmacokinetic data Bioavailability approximately 100% Metabolism Treprostinil is substantially metabolized by the liver, but the involved enzymes are not currently known. Five metabolites HU1 through HU5 have been identified thus far. Half life 4 hours Excretion Urine 4% as unchanged drug, 64% as metabolites; feces 13% Therapeutic considerations Pregnancy cat. B Legal status ? Routes Subcutaneous or intravenous infusion Treprostinil is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension. Treprostinil is marketed as Remodulin. Clinical pharmacology As an analogue of prostacyclin PGI2, treprostinil effects vasodilation, which in turn lowers the blood pressure. Treprostinil also inhibits platelet aggregation, though the role this phenomenon may play in relation to pulmonary hypertension has yet to be determined. Dosage and administration Treprostinil is administered via a small infusion pump that the patient must wear at all times. Treprostinil is preferentially given subcutaneously using an infusion set, but may be given intravenously via a central venous catheter if the patient is unable to tolerate the potential pain and discomfort of subcutaneous administration. Treprostinil, under the trademark Remodulin, is supplied in 20 mL vials, ranging in concentrations of 1 mg/mL, 2.5 mg/mL, 5 mg/mL, and 10 mg/mL. Treprostinil can be administered subcutaneously as supplied. It must be diluted for intravenous infusion with either sterile water or a 0.9% sodium chloride solution prior to administration. The infusion rate is normally initiated at 1.25 ng/kg/min for new patients, but may be reduced to 0.625 ng/kg/min if the normal rate provokes unwanted side effects in the patient. The infusion rate of trepostinil should be increased no more than 1.25 ng/kg/min per week for the first month, then no more than 2.5 ng/kg/min per week for the remaining duration of infusion. The infusion rate should ideally be high enough to improve symptoms of pulmonary hypertension, while minimizing unpleasant side effects. Oral and inhaled forms of treprostinil are currently undergoing clinical trials. Important safety information Precautions: Since treprostinil is a vasodilator, its antihypertensive effect may be compounded by other medications that affect the blood pressure, including calcium channel blockers, diuretics, and other vasodilating agents. Because of treprostinil's inhibiting effect on platelet aggregation, there is an increased risk of bleeding, especially among patients who are also taking anticoagulants. It is not known whether treprostinil is excreted in breast milk. Caution is advised when administering this medication to nursing women. Caution is advised when administering treprostinil to patients who have impaired kidney or liver function. Common side effects: 85% of patients report pain or other reaction at the infusion site. Other side effects may include headache, diarrhea, nausea, rash, jaw pain, vasodilatation, dizziness, edema swelling, pruritus itching, and hypotension. Warnings: Abrupt interruption of the treprostinil infusion can lead to worsening of pulmonary hypertension symptoms, and should be avoided. v d e Antithrombotics thrombolytics, anticoagulants and antiplatelet drugs B01 Antiplatelet drugs Glycoprotein IIb/IIIa inhibitors Abciximab Eptifibatide Tirofiban ADP receptor/P2Y12 inhibitors Clopidogrel Ticlopidine Prasugrel Prostaglandin analogue PGI2 Beraprost Prostacyclin Iloprost Treprostinil COX inhibitors Acetylsalicylic acid/Aspirin Aloxiprin Carbasalate calcium Other Ditazole Cloricromen Dipyridamole Indobufen Picotamide Triflusal Anticoagulants Vitamin K antagonists inhibit II, VII, IX, X Acenocoumarol Clorindione Coumatetralyl Dicoumarol Dicumarol Diphenadione Ethyl biscoumacetate Phenprocoumon Phenindione Tioclomarol Warfarin Heparin group Antithrombin III Danaparoid Sulodexide low molecular weight heparin Bemiparin, Dalteparin, Enoxaparin, Nadroparin, Parnaparin, Reviparin, Tinzaparin Direct thrombin II inhibitors Argatroban Bivalirudin Dabigatran Desirudin Hirudin Lepirudin Melagatran Ximelagatran Factor Xa inhibitors Apixaban Otamixaban Rivaroxaban oligosaccharides Fondaparinux, Idraparinux Other Defibrotide Dermatan sulfate Ramatroban Thrombolytic drugs/ fibrinolytics plasminogen activators: TPA Alteplase, Reteplase, Tenecteplase UPA Urokinase, Saruplase Streptokinase Anistreplase Monteplase other serine endopeptidases: Ancrod Drotrecogin alfa/Protein C Fibrinolysin Brinase Non-medicinal Citrate EDTA Oxalate v d e Medications used in the management of pulmonary arterial hypertension B01, C02 Prostacyclin analogues Beraprost, Epoprostenol, Iloprost, Treprostinil Endothelin receptor antagonists Ambrisentan, Bosentan, Sitaxsentan PDE5 inhibitors Sildenafil, Tadalafil Adjunctive therapy Calcium channel blockers, Diuretics, Digoxin, Oxygen therapy, Warfarin v d e Eicosanoids: prostaglandins Endogenous/series 2 D2 - E2 Dinoprostone - F2 Dinoprost - H2 - I2 Prostacyclin Prostaglandin analogues E: Alprostadil - Enprostil - Misoprostol F: Bimatoprost - Carboprost - Latanoprost - Travoprost I: Beraprost - Epoprostenol - Iloprost - Treprostinil Retrieved from http://en..org/wiki/Treprostinil Categories: Prostaglandins Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Español This page was last modified on 29 May 2008, at 13:55
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