Treprostinil 10mg/ml Inj, 20ml
It is used to treat high blood pressure in the lungs.
Drug Class
Antihypertensive, Pulmonary; Antiplatelet Agent
Pharmacologic Class
Prostacyclin Analog
Pregnancy Category
Category B
FDA Approved
May 2002
DEA Schedule
Not Controlled
Overview
What is this medicine?
Treprostinil is a medicine used to treat a serious lung condition called pulmonary arterial hypertension (PAH). It works by relaxing and widening the blood vessels in your lungs, which helps blood flow more easily and reduces the strain on your heart. It also helps prevent blood clots. This injectable form is given continuously, either under the skin (subcutaneously) or into a vein (intravenously), using a small pump.
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.
Disposal and Storage
Dispose of used needles and other sharp objects in a designated needle/sharp disposal box. Do not reuse needles or other items. When the box is full, follow local regulations for proper disposal. If you have any questions, consult your doctor or pharmacist.
Storage Instructions
Store unopened vials 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.
Disposal and Storage
Dispose of used needles and other sharp objects in a designated needle/sharp disposal box. Do not reuse needles or other items. When the box is full, follow local regulations for proper disposal. If you have any questions, consult your doctor or pharmacist.
Storage Instructions
Store unopened vials at room temperature.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Adhere strictly to the prescribed continuous infusion schedule; do not interrupt or abruptly stop the infusion without consulting your doctor.
- Learn proper sterile technique for preparing and administering the infusion, and for caring for your infusion site (if subcutaneous or intravenous).
- Rotate subcutaneous infusion sites regularly to prevent skin reactions.
- Carry backup supplies and a backup pump at all times.
- Avoid activities that significantly increase your risk of bleeding or injury due to the antiplatelet effects.
- Report any new or worsening symptoms, or any infusion site problems, to your healthcare provider immediately.
- Maintain regular follow-up appointments with your healthcare team.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 1.25 ng/kg/min (SC or IV continuous infusion). Titrate by 1.25 ng/kg/min increments per week for the first 4 weeks, then by 2.5 ng/kg/min increments per week or longer. Adjust based on clinical response and tolerability.
Dose Range:
1.25 - 40 mg
Condition-Specific Dosing:
Pulmonary Arterial Hypertension (PAH):
Continuous subcutaneous or intravenous infusion, starting at 1.25 ng/kg/min, titrated upwards based on clinical response and tolerability. Doses typically range from 1.25 ng/kg/min to 40 ng/kg/min or higher.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (limited data, individualized use in severe cases)
Adolescent:
Not established (limited data, individualized use in severe cases)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended, but monitor closely for adverse effects.
Dialysis:
Not significantly removed by dialysis; monitor closely.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
Reduce initial dose to 0.625 ng/kg/min. Titrate cautiously.
Severe:
Reduce initial dose to 0.625 ng/kg/min. Titrate cautiously and monitor closely for adverse effects.
Pharmacology
Mechanism of Action
Treprostinil is a prostacyclin analogue. It directly dilates pulmonary and systemic arterial vascular beds and inhibits platelet aggregation. It produces dose-dependent increases in cardiac index and stroke volume, and decreases in pulmonary vascular resistance, systemic vascular resistance, and mean pulmonary arterial pressure.
Pharmacokinetics
Absorption:
Bioavailability:
100% (subcutaneous)
Tmax:
3-5 hours (subcutaneous)
FoodEffect:
Not applicable for injectable forms.
Distribution:
Vd:
Approximately 14 L/70kg
ProteinBinding:
Approximately 96%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2-4 hours (subcutaneous/intravenous)
Clearance:
Approximately 150 mL/min/70kg
ExcretionRoute:
Primarily urine (79%), followed by feces (13%)
Unchanged:
<4% (in urine)
Pharmacodynamics
OnsetOfAction:
Rapid (within minutes for IV, within hours for SC)
PeakEffect:
Dose-dependent, sustained with continuous infusion
DurationOfAction:
Sustained as long as continuous infusion is maintained; effects diminish rapidly upon discontinuation due to short half-life.
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 experience any of the following symptoms, contact your doctor or seek medical attention immediately:
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 increase in size
+ 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
As with any medication, you may experience side effects. While many people have no side effects or only mild 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 possible 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 experience any of the following symptoms, contact your doctor or seek medical attention immediately:
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 increase in size
+ 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
As with any medication, you may experience side effects. While many people have no side effects or only mild 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 possible 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 lightheadedness, especially when standing up
- Fainting spells (syncope)
- Shortness of breath that worsens
- Chest pain
- Swelling in your ankles, feet, or abdomen
- Unusual bleeding or bruising
- Severe pain, redness, swelling, or infection at the infusion site
- Nausea, vomiting, or severe diarrhea that doesn't go away
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, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health issues.
Remember, do not start, stop, or change the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health issues.
Remember, do not start, stop, or change the dosage of any medication without first consulting your doctor.
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 exercise caution 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 pulmonary hypertension, such as shortness of breath, dizziness, or weakness. Discuss any concerns with your doctor.
If you receive this medication intravenously, you may be at a higher 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 your 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.
Women who are pregnant, planning to become pregnant, or breastfeeding should inform their doctor, as the benefits and risks of this medication to both the mother and the baby need to be carefully discussed.
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 exercise caution 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 pulmonary hypertension, such as shortness of breath, dizziness, or weakness. Discuss any concerns with your doctor.
If you receive this medication intravenously, you may be at a higher 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 your 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.
Women who are pregnant, planning to become pregnant, or breastfeeding should inform their doctor, as the benefits and risks of this medication to both the mother and the baby need to be carefully discussed.
Overdose Information
Overdose Symptoms:
- Severe headache
- Nausea
- Vomiting
- Diarrhea
- Flushing
- Hypotension (low blood pressure)
- Dizziness
- Fainting
What to Do:
Immediately reduce or discontinue the infusion. Call 911 or your local emergency number. For general poison control, call 1-800-222-1222.
Drug Interactions
Major Interactions
- CYP2C8 inhibitors (e.g., gemfibrozil): May increase treprostinil exposure and adverse effects. Consider dose reduction of treprostinil.
- CYP2C8 inducers (e.g., rifampin): May decrease treprostinil exposure and efficacy. Consider dose increase of treprostinil.
Moderate Interactions
- Anticoagulants (e.g., warfarin, heparin): Increased risk of bleeding due to treprostinil's antiplatelet effects. Monitor for signs of bleeding.
- Antihypertensives (e.g., diuretics, vasodilators, beta-blockers, ACE inhibitors): Additive hypotensive effects. Monitor blood pressure.
- Diuretics: Additive hypotensive effects. Monitor blood pressure.
Monitoring
Baseline Monitoring
Diagnosis of Pulmonary Arterial Hypertension (PAH)
Rationale: Confirm indication for therapy.
Timing: Prior to initiation
Liver and Renal Function Tests (LFTs, RFTs)
Rationale: Assess baseline organ function, especially liver due to metabolism and potential for dose adjustment in hepatic impairment.
Timing: Prior to initiation
Complete Blood Count (CBC)
Rationale: Assess baseline hematologic status, especially platelet count due to antiplatelet effects.
Timing: Prior to initiation
Vital Signs (Blood Pressure, Heart Rate)
Rationale: Establish baseline and monitor for hypotensive effects.
Timing: Prior to initiation
Functional Status (e.g., 6-minute walk distance)
Rationale: Establish baseline for assessing treatment efficacy.
Timing: Prior to initiation
Routine Monitoring
Vital Signs (Blood Pressure, Heart Rate)
Frequency: Daily initially, then regularly during dose titration and stable therapy
Target: Individualized, maintain within acceptable limits
Action Threshold: Significant hypotension or tachycardia; adjust dose or manage symptoms.
Symptoms of PAH (dyspnea, fatigue, chest pain, syncope, edema)
Frequency: Daily, ongoing
Target: Improvement or stabilization of symptoms
Action Threshold: Worsening symptoms; consider dose adjustment or alternative therapy.
Infusion Site Reactions (pain, erythema, induration, swelling)
Frequency: Daily, ongoing (for SC infusion)
Target: Minimal to no reaction
Action Threshold: Severe or persistent reactions; consider site rotation, pain management, or switch to IV.
Functional Status (e.g., 6-minute walk distance)
Frequency: Every 3-6 months or as clinically indicated
Target: Improvement or stabilization
Action Threshold: Decline in functional status; re-evaluate treatment.
Liver Function Tests (LFTs)
Frequency: Periodically, especially with dose changes or signs of hepatic dysfunction
Target: Within normal limits
Action Threshold: Significant elevation; re-evaluate dose or investigate cause.
Symptom Monitoring
- Headache
- Jaw pain
- Flushing
- Nausea
- Diarrhea
- Dizziness
- Hypotension
- Edema
- Rash
- Infusion site pain/reaction (for SC infusion)
- Bleeding (e.g., epistaxis, bruising)
Special Patient Groups
Pregnancy
Category B. Animal studies have shown no evidence of harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed and the potential benefits outweigh the potential risks to the fetus.
Trimester-Specific Risks:
First Trimester:
Low risk based on animal data, but human data limited.
Second Trimester:
Low risk based on animal data, but human data limited.
Third Trimester:
Low risk based on animal data, but human data limited.
Lactation
It is not known whether treprostinil is excreted in human milk. Treprostinil was excreted in the milk of lactating rats. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from treprostinil, 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:
Moderate risk (L3) - potential for adverse effects, but human data limited. Monitor infant for diarrhea, flushing, or other signs of drug exposure.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use in children is generally individualized for severe cases of PAH, often based on extrapolation from adult data and close monitoring.
Geriatric Use
No specific dose adjustment is required based on age alone. However, elderly patients may have reduced hepatic or renal function, which could affect drug clearance. Monitor closely for adverse effects and adjust dose as needed based on individual tolerability and response.
Clinical Information
Clinical Pearls
- Treprostinil is a life-sustaining medication for many PAH patients; abrupt discontinuation can lead to rapid clinical deterioration and rebound pulmonary hypertension.
- Infusion site pain and reactions are very common with subcutaneous administration and are a frequent reason for switching to intravenous delivery.
- Patients on continuous infusion require extensive education on pump operation, sterile technique, and emergency procedures.
- Dose titration is a slow, individualized process, often taking weeks to months to reach an optimal therapeutic dose.
- Patients should be advised to carry a medical alert card or wear medical identification indicating their condition and medication.
Alternative Therapies
- Epoprostenol (Flolan, Veletri) - IV prostacyclin
- Iloprost (Ventavis) - Inhaled prostacyclin
- Selexipag (Uptravi) - Oral prostacyclin receptor agonist
- Bosentan (Tracleer) - Endothelin Receptor Antagonist (ERA)
- Ambrisentan (Letairis) - ERA
- Macitentan (Opsumit) - ERA
- Sildenafil (Revatio) - PDE5 Inhibitor
- Tadalafil (Adcirca) - PDE5 Inhibitor
- Riociguat (Adempas) - Soluble Guanylate Cyclase (sGC) Stimulator
Cost & Coverage
Average Cost:
Extremely high (e.g., thousands to tens of thousands USD per month) per vial/month
Generic Available:
Yes
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high co-pays or co-insurance)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to consult with your pharmacist. If you have any questions or concerns about this medication, do not 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 emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.