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
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• Azilsartan; Chlorthalidone
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• Cannabidiol
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• Carbidopa; Levodopa
• Carbidopa; Levodopa; Entacapone
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• Chloroprocaine
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• Chlorthalidone
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• Enflurane
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• Fenoprofen
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• Flurbiprofen
• Fondaparinux
• Fosinopril; Hydrochlorothiazide, HCTZ
• Fospropofol
• Gemfibrozil
• General anesthetics
• Haloperidol
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• Heparin
• Hydralazine; Hydrochlorothiazide, HCTZ
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• 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
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