Treprostinil

What is Treprostinil

Treprostinil is a tricyclic benzidine analog of epoprostenol (prostacyclin) approved for patients with pulmonary arterial hypertension (PAH; WHO Group I). Studies that established effectiveness in PAH treatment included predominately patients with New York Heart Association (NYHA) Class II to IV symptoms, Class III symptoms, and Class II to III symptoms for treprostinil injection, oral inhalation, and oral tablets, respectively.

Treprostinil has also been known by the names Uniprost and UT-15. Treprostinil can be administered via oral tablet administration, oral inhalation, or continuous subcutaneous or intravenous infusion and does not require refrigeration during delivery. While the subcutaneous route of administration is preferred for the injectable formulation, treprostinil can also be administered intravenously via a central catheter in patients unable to tolerate continuous subcutaneous infusion due to injection site pain or reactions.

In contrast, epoprostenol (Flolan) must be refrigerated during delivery and is only administered via a central venous catheter due to an extremely short half-life.

Intravenous administration through a central catheter may expose patients to complications such as catheter-related embolism or thrombosis, sepsis, and delivery system malfunction.

Continuous subcutaneous infusion of treprostinil (Remodulin), classified as an orphan drug, was approved by the FDA in May 2002. The intravenous use of treprostinil was approved by the FDA in November 2004.

In March 2006, the FDA approved a dosage regimen for the transition to treprostinil from epoprostenol. The dosage regimen is used in order to minimize clinical deterioration in patients requiring transition to treprostinil from epoprostenol.

The oral inhalational dosage form of treprostinil (Tyvaso) was approved by the FDA in July 2009. The oral extended release tablet formulation (Orenitram) was approved by the FDA in December 2013.

Indications

  • pulmonary hypertension

Side Effects

  1. abdominal pain
  2. angioedema
  3. anorexia
  4. arthralgia
  5. asthenia
  6. bone pain
  7. chest pain (unspecified)
  8. cough
  9. diarrhea
  10. dizziness
  11. dyspepsia
  12. edema
  13. epistaxis
  14. erythema
  15. flushing
  16. GI bleeding
  17. headache
  18. hematoma
  19. hemoptysis
  20. hypokalemia
  21. hypotension
  22. infection
  23. injection site reaction
  24. injection site reaction
  25. maculopapular rash
  26. musculoskeletal pain
  27. myalgia
  28. nasal irritation
  29. nausea
  30. paresthesias
  31. phlebitis
  32. pruritus
  33. rash
  34. syncope
  35. throat irritation
  36. thrombocytopenia
  37. vomiting
  38. wheezing

Monitoring Parameters

  • arterial blood gases (ABGs)
  • blood pressure

Contraindications

  • abrupt discontinuation
  • alcoholism
  • asthma
  • bleeding
  • breast-feeding
  • chronic obstructive pulmonary disease (COPD)
  • diverticulitis
  • geriatric
  • hepatic disease
  • hepatitis
  • hypotension
  • intravenous administration
  • pregnancy
  • pulmonary disease
  • renal disease
  • renal failure
  • renal impairment

Interactions

  • Abciximab
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Alemtuzumab
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Hydrochlorothiazide, HCTZ
  • Alprostadil
  • Amifostine
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Aminosalicylate sodium, Aminosalicylic acid
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Amyl Nitrite
  • Anagrelide
  • Anticoagulants
  • Antithrombin III
  • Apixaban
  • Apraclonidine
  • Argatroban
  • Aripiprazole
  • Asenapine
  • Aspirin, ASA
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Dipyridamole
  • Aspirin, ASA; Omeprazole
  • Aspirin, ASA; Oxycodone
  • Aspirin, ASA; Pravastatin
  • Atenolol; Chlorthalidone
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Azilsartan; Chlorthalidone
  • Baclofen
  • Benazepril; Hydrochlorothiazide, HCTZ
  • Bendroflumethiazide; Nadolol
  • Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Betrixaban
  • Bismuth Subsalicylate
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Bisoprolol; Hydrochlorothiazide, HCTZ
  • Bivalirudin
  • Bortezomib
  • Bosentan
  • Candesartan; Hydrochlorothiazide, HCTZ
  • Cannabidiol
  • Captopril; Hydrochlorothiazide, HCTZ
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Cariprazine
  • Celecoxib
  • Chloroprocaine
  • Chlorothiazide
  • Chlorthalidone
  • Chlorthalidone; Clonidine
  • Choline Salicylate; Magnesium Salicylate
  • Cilostazol
  • Clopidogrel
  • Clozapine
  • Co-Enzyme Q10, Ubiquinone
  • Cocaine
  • Conivaptan
  • Dabigatran
  • Dalteparin
  • Danaparoid
  • Desirudin
  • Dexmedetomidine
  • Dextromethorphan; Quinidine
  • Diclofenac
  • Diclofenac; Misoprostol
  • Diflunisal
  • Dihydroergotamine
  • Diltiazem
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Dipyridamole
  • Duloxetine
  • Edoxaban
  • Enalapril; Hydrochlorothiazide, HCTZ
  • Enflurane
  • Enoxaparin
  • Epoprostenol
  • Eprosartan; Hydrochlorothiazide, HCTZ
  • Eptifibatide
  • Esomeprazole; Naproxen
  • Etodolac
  • Etomidate
  • Famotidine; Ibuprofen
  • Fenoprofen
  • Fluoxetine; Olanzapine
  • Flurbiprofen
  • Fondaparinux
  • Fosinopril; Hydrochlorothiazide, HCTZ
  • Fospropofol
  • Gemfibrozil
  • General anesthetics
  • Haloperidol
  • Halothane
  • Heparin
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Hydrochlorothiazide, HCTZ
  • Hydrochlorothiazide, HCTZ; Irbesartan
  • Hydrochlorothiazide, HCTZ; Lisinopril
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Moexipril
  • Hydrochlorothiazide, HCTZ; Olmesartan
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Quinapril
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Telmisartan
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrochlorothiazide, HCTZ; Valsartan
  • Hydrocodone; Ibuprofen
  • Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
  • Ibuprofen
  • Ibuprofen; Oxycodone
  • Ibuprofen; Pseudoephedrine
  • Iloperidone
  • Iloprost
  • Indomethacin
  • Isoflurane
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Isosorbide Dinitrate, ISDN
  • Isosorbide Mononitrate
  • Ketamine
  • Ketoprofen
  • Ketorolac
  • Lansoprazole; Naproxen
  • Lepirudin
  • Levodopa
  • Lovastatin; Niacin
  • Lurasidone
  • Magnesium Salicylate
  • Meclofenamate Sodium
  • Mefenamic Acid
  • Meloxicam
  • Methohexital
  • Methyclothiazide
  • Metolazone
  • Milrinone
  • Monoamine oxidase inhibitors
  • Nabumetone
  • Naproxen
  • Naproxen; Pseudoephedrine
  • Naproxen; Sumatriptan
  • Nesiritide, BNP
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nimodipine
  • Nitrates
  • Nitroglycerin
  • Nitroprusside
  • Nonsteroidal antiinflammatory drugs
  • Olanzapine
  • Oxaprozin
  • Oxymetazoline
  • Pentosan
  • Pentoxifylline
  • Perindopril; Amlodipine
  • Piroxicam
  • Prasugrel
  • Prazosin
  • Procainamide
  • Procaine
  • Propofol
  • Quinidine
  • Rasagiline
  • Rifampin
  • Risperidone
  • Rivaroxaban
  • Rofecoxib
  • Salicylates
  • Salsalate
  • Sevoflurane
  • Silodosin
  • Sulindac
  • Sympathomimetics
  • Tetrabenazine
  • Tetracaine
  • Thiazide diuretics
  • Thiopental
  • Thiothixene
  • Ticagrelor
  • Ticlopidine
  • Tinzaparin
  • Tirofiban
  • Tizanidine
  • Tolmetin
  • Trandolapril; Verapamil
  • Trazodone
  • Valdecoxib
  • Verapamil
  • Vorapaxar
  • Warfarin
  • Yohimbine
  • Ziprasidone
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