Treprostinil

Treprostinil is a prescription medication used to treat pulmonary arterial hypertension (PAH). It is also used to switch those taking Flolan (epoprostenol) to treprostinil. Treprostinil belongs to a group of drugs called vasodilators, which help to relax the blood vessels within and around the lungs. This helps increase your ability to breathe, especially during exercise. It also acts as a blood thinner, which decreases the chance of a blood clot.

This medication is available in an injectable form to be given directly into a vein (IV) or just under the skin (subcutaneously) by a healthcare professional.

This medication also comes as an inhalant that is to be used 4 times a day, at least 4 hours apart per inhalation.

Treprostinil is also available as extended release tablets. It is usually taken 2 or 3 times a day with food. Swallow tablets whole, do not crush, divided or chew tablets.

Common side effects of treprostinil injectable include diarrhea, jaw pain, and pain at the site of injection. It can also cause dizziness. Do not drive or operate heavy machinery until you know how treprostinil affects you.

Common side effects of treprostinil inhalant include headache, nausea, and flushing. It can also cause dizziness. Do not drive or operate heavy machinery until you know how treprostinil affects you.

Common side effects of treprostinil tablets include headache, nausea, and diarrhea. 

Treprostinil is a prescription medication used to treat pulmonary arterial hypertension. The injectable form may also used to switch those taking Flolan (epoprostenol) to treprostinil. 

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Treprostinil may be found in some form under the following brand names:

• Orenitram

• Remodulin

• Tyvaso

Serious side effects have been reported with treprostinil.

Injectable:

Common side effects of treprostinil injectable include the following:

• pain at site of injection
• headache
• diarrhea
• nausea
• jaw pain
• dizziness
• body swelling
• itching
• low blood pressure

Inhalational:

Common side effects of treprostinil inhalational include the following:

• cough
• headache
• nausea
• dizziness
• flushing
• throat irritation
• throat pain
• diarrhea

Oral:

Common side effects of treprostinil extended release tablets include the following:

• headache
• nausea
• diarrhea
• flushing
• jaw pain
• pain in extremities
• low levels of potassium in the blood
• stomach discomfort

This is not a complete list of treprostinil side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• diuretics such as
  • acetazolamide (Diamox)
  • amiloride (Midamor)
  • bumetanide (Bumex)
  • chlorothiazide (Diuril)
  • chlorthalidone (Thalitone)
  • ethacrynic acid (Edecrin)
  • furosemide (Lasix)
  • hydrochlorothiazide (Microzide, HCTZ)
  • metolazone (Zaroxolyn)
  • torsemide (Demadex)
  • triamterene (Dyrenium, Dyazide, Maxzide)
• angiotensin-converting enzyme (ACE) blockers such as
  • benazepril (Lotensin, Lotensin HCT)
  • captopril (Capoten, Capozide)
  • enalapril (Vasotec, Vaseretic)
  • fosinopril (Monopril, Monopril HCT)
  • lisinopril (Prinivil, Prinzide, Zestril, Zestoretic)
  • moexipril (Univasc, Uniretic)
  • quinapril (Accupril, Accuretic, Quinaretic)
  • ramipril (Altace)
  • trandolapril (Mavik, Tarka)
• angiotensin receptor II blockers such as
  • azilsartan (Edarbi)
  • candesartan (Atacand)
  • irbesartan (Avapro)
  • losartan (Cozaar)
  • olmesartan (Benicar)
  • telmisartan (Micardis, Twynsta)
  • valsartan (Diovan)
• beta blockers such as
  • metoprolol (Toprol XL, Lopressor)
  • carvedilol (Coreg)
  • bisoprolol (Zebeta)
  • betaxolol (Kerlone)
  • nebivolol (Bystolic)
  • propranolol (Inderal)
• calcium channel blockers such as
• nifedipine (Adalat, Nifedical, Procardia)
• amlodipine (Norvasc)
• verapamil (Calan, Isoptin, Covera, Verelan)
• diltiazem (Cardizem)
• vasodilators such as
  • doxazosin (Cardura)
  • prazosin (Minipress)
  • terazosin (Hytrin)
  • clonidine (Catapres)
  • hydralazine (Bidil, Hydra-Zide)
  • minoxidil

• medications that affect your platelets such as clopidogrel (Plavix), aspirin, prasugrel (Effient), ticagrelor (Brilinta), ticlopidine (Ticlid), abciximab (ReoPro), eptifibatide (Integrilin), tirofiban (Aggrastat), and cilostazol (Pletal)
• anticoagulant (blood thinner) medications such as warfarin (Coumadin, Jantoven), heparin, enoxaparin (Lovenox), fondaparinux (Arixtra), rivaroxaban (Xarelto), and apixaban (Eliquis) 
• alcohol

This is not a complete list of all drug interactions. Ask your doctor or pharmacist for more information.

Serious side effects have been reported with this medication, and certain precautions should be followed:

Injectable:

• Long-term (chronic) infusions of treprostinil injectable are delivered using a central venous catheter. This catheter is a long, soft, thin, hollow 
  tube that is placed into a large vein. There is an increased risk of blood stream infections and sepsis (widespread inflammation of the body). This could be fatal if it occurs.
• This medication can cause dizziness. Do not drive or operate heavy machinery until you know how treprostinil affects you.
• Do not take this medication if you are allergic to it or to any of the inactive ingredients.

Inhalational:

• This medication may increase the risk of bleeding, particularly if you are taking blood thinners. 
• This medication can cause dizziness. Do not drive or operate heavy machinery until you know how treprostinil affects you.
• Do not take this medication if you are allergic to it or to any of the inactive ingredients.

Oral:

• There is an Increased risk of bleeding, particularly in you are taking blood thinners.
• Do not take this medication if you are allergic to it or to any of the inactive ingredients.
• Do not take this medication if you have severe liver impairment (specifically Child Pugh Class C)

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of this medication, there are no specific foods that you must exclude from your diet when receiving this medication.

Before taking treprostinil, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to it or to any of the inactive ingredients
• have liver problems
• have kidney problems
• have diverticulosis
• have low blood pressure or high blood pressure
• have had a stroke
• have stomach ulcers
• are pregnant or are breastfeeding

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Injectable/Inhalational:

• Tell your doctor if you are pregnant or plan to become pregnant.
• The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.
• This medication falls into category B. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Oral:

• Tell your doctor if you are pregnant or plan to become pregnant.
• The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.
• This medication falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if treprostinil crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using treprostinil.

Injectable:

• Treprostinil injectable is infused continuously through a subcutaneous (under the skiN) or surgically placed indwelling central venous catheter
• Therapy with this medication will be needed for prolonged periods, possibly years.
• In order to reduce the risk of infection, proper technique must be used.

Inhalational:

• Take exactly as your healthcare provider tells you to take it.
• You should be properly trained on how to use treprostinil inhalational and the Tyvaso (treprostinil) Inhalation System device.
• To avoid potential interruptions in drug delivery because of equipment malfunction, you should have access to a back-up Tyvaso Inhalation System device 
• If a dose is missed or interrupted, therapy should be resumed as soon as possible
• Avoid skin or eye contact with this medication. If it comes in contact with the skin or eyes, rinse immediately with water.

Oral:

• Take exactly as your healthcare provider tells you to take it.
• Your healthcare provider will slowly increase your dose to find the dose of that is right for you.
• Do not change your dose or suddenly stop taking this medication without first talking to your healthcare provider. Stopping this medication suddenly may cause worsening of your PAH symptoms.
• Tablets are usually taken every 12 hours, but may be taken three times daily (approximately every 8 hours). If you have side effects, your healthcare provider may tell you to change your dose or when you take this medication.
• Take with food.
• Swallow tablets whole. Do not split, chew, crush, or break your tablets. Do not take tablets that are damaged or broken. If tablets are not taken whole, they may release too much medicine at one time. This can lead to side effects.
• You may see the tablet shell in your stools (bowel movements). This is usually normal. The tablet shell is not digested. If you have diverticulosis, the tablet shell may get stuck in a blind pouch or diverticulum in your intestine.
• If you miss your dose of this medication, take the dose as soon as possible with food.
• If you miss two or more doses of this medication, call your healthcare provider to see if you need to change your dose.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication
• your weight
• your height
• your age
• your gender

Injectable:

The recommended starting dose dose for those new to prostacyclin infusion therapy: 1.25 ng/kg/minute (or 0.625 ng/kg/minute if not tolerated). Your dose may be increased according to response to therapy and/or adverse effects.

Inhalational:

• Take undiluted (do not mix with any other liquid).
• Take in 4 separate treatment sessions each day approximately 4 hours apart (during waking hours).
• Starting dose: 3 breaths [18 mcg] per session. If 3 breaths are not tolerated, reduce to 1 or 2 breaths.
• Dose may be increased by an additional 3 breaths at about 1-2 week intervals, if tolerated.
• Increase to target maintenance (long-term) dose of 9 breaths [54 mcg] per session as tolerated.

Oral:

• The starting recommended dose is 0.25 mg twice daily.
• Your doctor may increase your dose by 0.25 mg or 0.5 mg twice daily or 0.125 mg three times daily, not more than every 3 to 4 days as tolerated.
• The maximum dose is determined by tolerability.

If you take too much this medication, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If this medication is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

Inhalational:

• Store ampules in the unopened foil pack between 59°F to 86°F (15°C to 30°C) until ready to use.
• When the foil pouch is opened, ampules should be used within 7 days.
• This medication is sensitive to light. The unopened ampules should be stored in the foil pouch.
• After an ampule is opened and put into the medicine cup in the Tyvaso Inhalation System, this medication can be kept in the medicine cup for no more than 1 day (24 hours).
• Treprostinil inhalational that is left in the medicine cup at the end of the day must be thrown away.
• The Tyvaso Inhalation System can be stored in the carrying case when not in use (example: between treatment sessions or overnight). If storing between treatment sessions, ensure that the plugs are firmly in place in the dome assembly to prevent spillage of this medication.
• Keep this and all medications out of the reach of children.

Oral:

• Store Orenitram at room temperature, between 68°F to 77°F (20°C to 25°C).
• Keep this and all medications out of the reach of children.