Epoprostenol
Epoprostenol Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Epoprostenol is a brand name. Its generic name is Epoprostenol.
Epoprostenol
Epoprostenol (brand name Flolan) is a drug used to treat people with severe pulmonary arterial hypertension (PAH). It is a prostaglandin analog administered by continuous intravenous (IV) infusion through a catheter placed near the heart. It works by relaxing and widening blood vessels, resulting in increased oxygen supply to the lungs and other organs. While it markedly improves prognosis and survival time, there are some associated risks with taking epoprostenol.
Uses of Epoprostenol
Epoprostenol is prescribed for the long-term treatment of PAH, and is indicated for people not responding to other treatments. It also can be used on a short-term basis to stabilize patients whose conditions are acute and deteriorating. In addition, Epoprostenol may improve exercise capacity in those with PAH by increasing blood supply to the heart and lungs.
Mechanism of Action
Epoprostenol works by activating the enzyme adenylate cyclase in the cells, which causes an increase in intracellular cyclic AMP (cAMP). cAMP activates a protein called protein kinase A, which leads to an increase in cell membrane permeability and smooth muscle relaxation. This action results in vasodilation, thereby reducing pulmonary arterial resistance, improving blood flow to the lungs and other organs, and improving oxygenation levels.
How Long Does it Take to Work?
The effects of epoprostenol are usually felt within minutes of the initial dose. However, the full sustained effects may not be felt for several days.
Absorption
It is administered directly into the bloodstream via IV infusion, and thus is not absorbed into the body. Its effects are seen immediately as it is administered.
Route of Elimination
Epoprostenol is eliminated from the body via the kidneys and liver. The majority is excreted unchanged in the urine.
Dosage
The recommended epoprostenol dosage for patients with PAH is an initial dose of 5 ng/kg/min (0.6 mcg/kg/min) administered continuously by IV infusion. This initial dose can be adjusted in increments of 2.5 ng/kg/min (0.3 mcg/kg/min) to a maximum dose of 40 ng/kg/min (4.8 mcg/kg/min). The optimal dose is usually determined by measuring the patient’s response to treatment.
Administration
Epoprostenol is administered as an IV infusion via an implanted catheter with an external pump. The external pump is programmed and adjusted according to the prescribed dose and the patient’s response.
Side Effect
The most common side effects of epoprostenol includes headache, nausea and vomiting, flushing, chest pain, irregular heartbeat, low blood pressure, difficulty breathing, and fluid retention. It may also cause abnormal liver enzyme levels, skin rash, hives and itching. In rare cases, epoprostenol may cause an allergic reaction leading to anaphylaxis or death.
Toxicity
Epoprostenol is relatively safe and well tolerated. No significant drug interactions have been reported. The drug is generally not toxic at the recommended dose, but can cause an increase in the risk of thromboembolism.
Precaution
Epoprostenol should be used with caution in patients with known allergies to prostaglandins, or in those with renal impairment, liver disease, or other medical conditions. It may also reduce the efficacy of other medications taken at the same time, and should not be used with warfarin, heparin, or other anticoagulants.
Interactions
Epoprostenol may interact with other drugs, including antibiotics, antifungals, calcium channel blockers, certain antidepressants, diuretics, and anticonvulsants. It is also known to interact with some over-the-counter and herbal medications. It is important to discuss any medication changes with a doctor before starting epoprostenol.
Disease Interaction
It is recommended that epoprostenol be used with caution in people with other lung diseases, including asthma, emphysema, and chronic obstructive pulmonary disease (COPD). It is also known to interact with some heart conditions, diabetes, and HIV/AIDS.
Drug Interactions
Epoprostenol may interact with other drugs, including antibiotics, antifungals, calcium channel blockers, certain antidepressants, diuretics, and anticonvulsants. It is also known to interact with some over-the-counter and herbal medications. It is important to discuss any medication changes with a doctor before starting epoprostenol.
Food Interactions
Epoprostenol should not be taken with dairy products, orange juice, grapefruit juice, tomatoes, and other acidic foods, as these may reduce the absorption of epoprostenol.
Pregnancy Use
Epoprostenol is classified as a Pregnancy Category B drug. It is not known if epoprostenol is harmful to an unborn fetus. However, it is known that PAH can be dangerous to pregnant women, and treatment with epoprostenol may be necessary. Women who are pregnant should discuss the benefits and risks of using epoprostenol with a doctor.
Lactation Use
It is not known if epoprostenol is secreted in human milk, and use during breastfeeding is not recommended.
Acute Overdose
If an overdose of epoprostenol is suspected, seek immediate medical attention. Symptoms of an overdose include dizziness, nausea, hypotension, and difficulty breathing. Treatment is supportive and may include reducing the dose and increasing fluid intake.
Contraindication
Epoprostenol is contraindicated in patients with known hypersensitivity to prostaglandins. It is also contraindicated in patients with blood clotting disorders or recent thromboembolism and in those taking anticoagulants.
Use Direction
Epoprostenol should be administered as an intravenous infusion. The dose should be adjusted according to the patient’s response to treatment. It should be discontinued if the patient experiences any serious side effects.
Storage Condition
Epoprostenol must be stored at room temperature, between 59°F to 86°F (15°C to 30°C). Keep away from light and moisture. Do not freeze.
Volume of Distribution
Epoprostenol has a volume of distribution of 3.5 L/kg.
Half Life
The half-life of epoprostenol is estimated to be between 10 minutes and 5 hours.
Clearance
Epoprostenol is cleared from the body by both renal and hepatic pathways. The renal clearance is 0.6 L/hour.
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