Treprostinil 1mg/ml Inj, 20ml
It is used to treat high blood pressure in the lungs.
Drug Class
Antihypertensive, Pulmonary Arterial Hypertension (PAH) agent
Pharmacologic Class
Prostacyclin analogue; Vasodilator; Platelet aggregation inhibitor
Pregnancy Category
Not available
FDA Approved
May 2002
DEA Schedule
Not Controlled
Overview
What is this medicine?
Treprostinil is a medication used to treat pulmonary arterial hypertension (PAH), a condition where blood pressure in the arteries leading to the lungs is too high. It works by relaxing and widening these blood vessels, making it easier for your heart to pump blood through your lungs and improving your ability to exercise.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered continuously into a vein or the fatty part of the skin. Your doctor may instruct you on how to administer it yourself. Before and after handling the medication, wash your hands thoroughly.
If you need to mix this medication with another fluid, make sure you use the correct type of fluid. If you're unsure, consult your doctor or pharmacist. Do not use the medication if the solution appears cloudy, is leaking, or contains particles. Additionally, do not use it if the solution has changed color.
Safe Disposal of Needles and Supplies
Dispose of used needles and other sharp objects in a designated needle/sharp disposal box. Never reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
Store unopened vials of this medication at room temperature.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered continuously into a vein or the fatty part of the skin. Your doctor may instruct you on how to administer it yourself. Before and after handling the medication, wash your hands thoroughly.
If you need to mix this medication with another fluid, make sure you use the correct type of fluid. If you're unsure, consult your doctor or pharmacist. Do not use the medication if the solution appears cloudy, is leaking, or contains particles. Additionally, do not use it if the solution has changed color.
Safe Disposal of Needles and Supplies
Dispose of used needles and other sharp objects in a designated needle/sharp disposal box. Never reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
Store unopened vials of this medication at room temperature.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Do NOT stop this medication abruptly, as it can lead to a rapid worsening of your condition and potentially life-threatening symptoms. Always consult your doctor before making any changes.
- Learn proper infusion techniques and sterile procedures to prevent infection at the infusion site.
- Always have backup supplies (pump, medication, batteries) readily available.
- Avoid activities that could dislodge or damage your infusion catheter.
- Report any signs of infection at the infusion site (redness, swelling, pain, pus, fever) immediately.
- Avoid sudden changes in posture to minimize dizziness or lightheadedness due to blood pressure changes.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Continuous subcutaneous infusion: Initiate at 1.25 ng/kg/min. If tolerated, increase by 1.25 ng/kg/min increments weekly or biweekly. Continuous intravenous infusion: Initiate at 1.25 ng/kg/min. If tolerated, increase by 1.25 ng/kg/min increments weekly or biweekly. Doses are titrated based on clinical response and tolerability.
Dose Range:
1.25 - 40 mg
Condition-Specific Dosing:
Pulmonary Arterial Hypertension (PAH):
Titrate to optimal clinical response and tolerability, typically ranging from 1.25 ng/kg/min up to 40 ng/kg/min or higher.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (used off-label, dose extrapolated from adult data)
Adolescent:
Not established (used off-label, dose extrapolated from adult data)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but monitor closely.
Moderate:
No specific dose adjustment recommended, but monitor closely.
Severe:
No specific dose adjustment recommended, but monitor closely.
Dialysis:
Not well studied; monitor closely for adverse effects.
Hepatic Impairment:
Mild:
Reduce initial dose to 0.625 ng/kg/min for continuous subcutaneous or intravenous infusion. Titrate cautiously.
Moderate:
Reduce initial dose to 0.625 ng/kg/min for continuous subcutaneous or intravenous infusion. Titrate cautiously.
Severe:
Reduce initial dose to 0.625 ng/kg/min for continuous subcutaneous or intravenous infusion. Titrate cautiously.
Pharmacology
Mechanism of Action
Treprostinil is a prostacyclin analogue. It directly dilates pulmonary and systemic arterial beds, and inhibits platelet aggregation. These actions contribute to improved hemodynamics and symptoms in patients with pulmonary arterial hypertension (PAH).
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100% (subcutaneous and intravenous)
Tmax:
3-5 hours (subcutaneous infusion)
FoodEffect:
Not applicable for parenteral administration
Distribution:
Vd:
Approximately 14 L/70 kg
ProteinBinding:
Approximately 91% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
2-4 hours
Clearance:
Approximately 150 mL/min/kg
ExcretionRoute:
Primarily renal (79%), with some fecal excretion (13%)
Unchanged:
<4% (in urine)
Pharmacodynamics
OnsetOfAction:
Rapid (due to continuous infusion)
PeakEffect:
Steady state achieved within 10-15 hours of continuous infusion
DurationOfAction:
Continuous (as long as infusion is maintained)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of bleeding, including:
+ Vomiting or coughing up blood
+ Vomit that resembles coffee grounds
+ Blood in the urine
+ Black, red, or tarry stools
+ Bleeding from the gums
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruises that enlarge
+ Uncontrollable bleeding
Severe dizziness or fainting
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Worsening or new breathing difficulties
Abnormal burning, numbness, or tingling sensations
Anxiety or restlessness
Pain or irritation at the injection site
Arm swelling
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or persist, contact your doctor:
Dizziness or headache
Flushing
Jaw pain
Diarrhea
Upset stomach or vomiting
* Irritation at the injection site
This is not an exhaustive list of potential side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of bleeding, including:
+ Vomiting or coughing up blood
+ Vomit that resembles coffee grounds
+ Blood in the urine
+ Black, red, or tarry stools
+ Bleeding from the gums
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruises that enlarge
+ Uncontrollable bleeding
Severe dizziness or fainting
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Worsening or new breathing difficulties
Abnormal burning, numbness, or tingling sensations
Anxiety or restlessness
Pain or irritation at the injection site
Arm swelling
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or persist, contact your doctor:
Dizziness or headache
Flushing
Jaw pain
Diarrhea
Upset stomach or vomiting
* Irritation at the injection site
This is not an exhaustive list of potential side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe headache, dizziness, or fainting (signs of low blood pressure)
- Unusual bleeding or bruising
- Severe pain, swelling, redness, or pus at the infusion site
- Worsening shortness of breath, chest pain, or fatigue (signs of PAH worsening)
- Nausea, vomiting, or diarrhea that is severe or persistent
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, any of its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have liver disease, as this may affect your ability to take this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, health conditions, and concerns with your doctor. This includes:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Any health problems you have, as they may interact with this medication
To ensure your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication with all your other medications and health conditions.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, any of its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have liver disease, as this may affect your ability to take this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, health conditions, and concerns with your doctor. This includes:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Any health problems you have, as they may interact with this medication
To ensure your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication with all your other medications and health conditions.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
When starting this medication, avoid driving and other activities that require alertness until you understand how it affects you. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying position, and be cautious when climbing stairs.
Be aware that this medication may increase your risk of bleeding. Take precautions to avoid injury, and use a soft-bristled toothbrush and an electric razor for shaving.
Do not abruptly stop taking this medication without consulting your doctor, as this may worsen symptoms of high blood pressure in the lungs, such as shortness of breath, dizziness, or weakness. Discuss any concerns with your doctor.
Receiving this medication intravenously may increase your risk of developing a severe, potentially life-threatening infection. Consult your doctor to understand this risk.
If you experience symptoms of withdrawal or suspect that the medication pump is not functioning correctly, seek immediate medical attention. Always have a backup system readily available in case of emergencies.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
When starting this medication, avoid driving and other activities that require alertness until you understand how it affects you. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying position, and be cautious when climbing stairs.
Be aware that this medication may increase your risk of bleeding. Take precautions to avoid injury, and use a soft-bristled toothbrush and an electric razor for shaving.
Do not abruptly stop taking this medication without consulting your doctor, as this may worsen symptoms of high blood pressure in the lungs, such as shortness of breath, dizziness, or weakness. Discuss any concerns with your doctor.
Receiving this medication intravenously may increase your risk of developing a severe, potentially life-threatening infection. Consult your doctor to understand this risk.
If you experience symptoms of withdrawal or suspect that the medication pump is not functioning correctly, seek immediate medical attention. Always have a backup system readily available in case of emergencies.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Severe headache
- Flushing
- Nausea
- Vomiting
- Diarrhea
- Hypotension (low blood pressure)
- Dizziness
- Syncope
What to Do:
If overdose is suspected, immediately reduce or discontinue the infusion and seek emergency medical attention. Call 1-800-222-1222 (Poison Control Center) or go to the nearest emergency room.
Drug Interactions
Major Interactions
- CYP2C8 inhibitors (e.g., Gemfibrozil): May increase treprostinil exposure, requiring dose reduction.
- CYP2C8 inducers (e.g., Rifampin): May decrease treprostinil exposure, requiring dose increase.
Moderate Interactions
- Anticoagulants (e.g., Warfarin, Heparin): Increased risk of bleeding due to treprostinil's antiplatelet effects.
- Antiplatelet agents (e.g., Aspirin, Clopidogrel): Increased risk of bleeding.
- Antihypertensive agents (e.g., Calcium channel blockers, ACE inhibitors): Additive hypotensive effects; monitor blood pressure closely.
- Diuretics: May enhance hypotensive effects.
Monitoring
Baseline Monitoring
Diagnosis of Pulmonary Arterial Hypertension (PAH)
Rationale: Confirm appropriate indication for therapy.
Timing: Prior to initiation
Liver and Renal Function Tests (LFTs, RFTs)
Rationale: Assess baseline organ function, especially liver due to hepatic metabolism and potential need for dose adjustment in impairment.
Timing: Prior to initiation
Blood Pressure (BP) and Heart Rate (HR)
Rationale: Establish baseline and monitor for hypotensive effects.
Timing: Prior to initiation
Routine Monitoring
Clinical symptoms of PAH (e.g., dyspnea, fatigue, exercise tolerance)
Frequency: Regularly, during dose titration and ongoing therapy
Target: Improvement or stabilization of symptoms
Action Threshold: Worsening symptoms may indicate need for dose adjustment or re-evaluation of therapy.
Blood Pressure (BP) and Heart Rate (HR)
Frequency: Regularly, especially during dose titration
Target: Maintain within acceptable limits, avoid symptomatic hypotension
Action Threshold: Symptomatic hypotension or significant bradycardia/tachycardia may require dose reduction or discontinuation.
Infusion site assessment (for subcutaneous infusion)
Frequency: Daily
Target: Absence of pain, erythema, induration, or infection
Action Threshold: Severe pain, swelling, skin breakdown, or signs of infection require immediate attention and site rotation.
Signs of bleeding
Frequency: Regularly, especially if on concomitant anticoagulants/antiplatelets
Target: Absence of unusual bruising, petechiae, or overt bleeding
Action Threshold: Any signs of bleeding should be investigated.
Symptom Monitoring
- Dyspnea (shortness of breath)
- Fatigue
- Chest pain
- Syncope (fainting)
- Dizziness
- Headache
- Nausea
- Vomiting
- Diarrhea
- Flushing
- Jaw pain
- Infusion site pain, erythema, induration, rash, or infection
Special Patient Groups
Pregnancy
Treprostinil was previously classified as Pregnancy Category B. Current guidelines suggest using treprostinil during pregnancy only if the potential benefit justifies the potential risk to the fetus. PAH itself poses significant risks during pregnancy.
Trimester-Specific Risks:
First Trimester:
Animal studies have shown some evidence of developmental toxicity at high doses, but human data are limited. Risk of PAH worsening is high.
Second Trimester:
Risk of PAH worsening is high.
Third Trimester:
Risk of PAH worsening is high, especially around delivery. Monitor closely.
Lactation
It is unknown if treprostinil is excreted in human milk. Due to the potential for serious adverse reactions in a breastfed infant, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Unknown; caution advised. Monitor for adverse effects if breastfeeding.
Pediatric Use
Safety and efficacy have not been established in pediatric patients. However, treprostinil is used off-label in pediatric PAH patients, often with dose extrapolation from adult data and careful titration.
Geriatric Use
No specific dose adjustment is required based on age alone. However, elderly patients may have reduced hepatic or renal function, or concomitant diseases, which may necessitate careful monitoring and dose adjustment based on individual patient response and tolerability.
Clinical Information
Clinical Pearls
- Abrupt discontinuation of treprostinil can lead to rapid clinical deterioration and rebound pulmonary hypertension, which can be fatal. Always ensure continuous infusion and have backup systems.
- Infusion site pain and reactions are very common with subcutaneous administration and can be a major limiting factor for patients. Strategies include site rotation, local anesthetics, and patient education.
- Dose titration is critical and highly individualized, requiring close monitoring of symptoms, hemodynamics, and tolerability.
- Patients and caregivers must be thoroughly educated on pump operation, sterile technique, and emergency procedures.
- Treprostinil is a potent vasodilator; monitor for systemic hypotension, especially during initiation and dose increases.
Alternative Therapies
- Epoprostenol (Flolan, Veletri) - IV prostacyclin
- Iloprost (Ventavis) - Inhaled prostacyclin
- Selexipag (Uptravi) - Oral prostacyclin receptor agonist
- PDE5 inhibitors (e.g., Sildenafil, Tadalafil)
- Endothelin Receptor Antagonists (ERAs) (e.g., Bosentan, Ambrisentan, Macitentan)
- Soluble Guanylate Cyclase (sGC) stimulators (e.g., Riociguat)
Cost & Coverage
Average Cost:
Highly variable, typically several thousands to tens of thousands USD per month
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization and often specialty pharmacy distribution)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. Be prepared to provide detailed information about the incident, including the medication taken, the amount, and the time it occurred.