Drug information of Epoprostenol

Epoprostenol

فارسی

Vasodilator and platelet-aggregation inhibitor; a naturally occurring prostaglandin.

Mechanism of effect

 Epoprostenol has 2 major pharmacological actions: (1) direct vasodilation of pulmonary and systemic arterial vascular beds, and (2) inhibition of platelet aggregation.

Pharmacodynamic

Epoprostenol has two major pharmacological actions: (1) direct vasodilation of pulmonary and systemic arterial vascular beds, and (2) inhibition of platelet aggregation. In animals, the vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume.

The effect of epoprostenol on heart rate in animals varies with dose. At low doses, there is vagally mediated brudycardia, but at higher doses, epoprostenol causes reflex tachycardia in response to direct vasodilation and hypotension. No major effects on cardiac conduction have been observed.

Additional pharmacologic effects of epoprostenol in animals include bronchodilation, inhibition of gastric acid secretion, and decreased gastric emptying. No available chemical assay is sufficiently sensitive and specific to assess the in vivo human pharmacokinetics of epoprostenol.

Pharmacokinetics

Absorption: Not Available

Volume of distribution: 357 mL/kg

Protein binding: Not Available

Metabolism: Epoprostenol is metabolized to 2 primary metabolites: 6-keto-PGF1α (formed by spontaneous degradation) and 6,15-diketo-13,14-dihydro-PGF1α (enzymatically formed), both of which have pharmacological activity orders of magnitude less than epoprostenol in animal test systems. Fourteen additional minor metabolites have been isolated from urine, indicating that epoprostenol is extensively metabolized in humans.

Half life: The in vitro half-life of epoprostenol in human blood at 37°C and pH 7.4 is approximately 6 minutes; the in vivo half-life of epoprostenol in humans is therefore expected to be no greater than 6 minutes.

Drug indications

For the long-term intravenous treatment of primary pulmonary hypertension and pulmonary hypertension associated with the scleroderma spectrum of disease in NYHA Class III and Class IV patients who do not respond adequately to conventional therapy.

Dosage

Usual Adult Dose for Pulmonary Hypertension

Initial dose: 2 ng/kg/min via continuous IV infusion and titrate up in increments of 2 ng/kg/min every 15 minutes or longer until a tolerance limit is established or further increases in infusion rate not clinically warranted.

Alerts

  • Pulmonary edema: Some patients with PAH have developed pulmonary edema during dosing adjustment and acute vasodilator testing (an off-label use), which may be associated with concomitant heart failure (LV systolic dysfunction with significantly elevated left heart filling pressures) or pulmonary veno-occlusive disease/pulmonary capillary hemangiomatosis. If pulmonary edema develops during therapy initiation, discontinue and do not readminister.
  • Rebound pulmonary hypertension: Avoid abrupt interruptions or large sudden reductions in dosage; may result in rebound pulmonary hypertension (eg, dyspnea, dizziness, asthenia). A fatal case occurred following interruption. Immediate access to medication or pump and infusion sets is essential to prevent treatment interruptions.
  • Vasodilation: Epoprostenol is a potent pulmonary and systemic vasodilator and can cause hypotension and other reactions such as flushing, nausea, vomiting, dizziness, and headache. Monitor blood pressure and symptoms regularly during initiation and after dose change.
  • Conditions that increase bleeding risk: Epoprostenol is a potent inhibitor of platelet aggregation. Use with caution in patients with other risk factors for bleeding.

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you have :

  •  If you have an allergy to epoprostenol or any other part of epoprostenol.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have heart failure (weak heart).
  • If you have ever gotten fluid in the lungs with use of epoprostenol.

Avoid driving and doing other tasks or actions that call for you to be alert until you see how epoprostenol affects you.

You may bleed more easily. Be careful and avoid injury. Use a soft toothbrush and an electric razor.

Have your blood pressure checked often. Talk with your doctor.

Do not stop taking epoprostenol all of a sudden without calling your doctor. Signs of high pressure in the lungs like shortness of breath, dizziness, or weakness may get worse. Talk with your doctor.

Always have a backup system close by in case you need to use it.

Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using epoprostenol while you are pregnant.

Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Anticoagulants: Potential for increased risk of bleeding.
Antiplatelet agents: Potential for increased risk of bleeding.
Digoxin: Potential decreased clearance of digoxin; possible digoxin toxicity.
Diuretics: Potential decreased clearance of furosemide. Possible additive hypotensive effect.
Hypotensive agents: Possible additive hypotensive effect.
Vasodilators: Possible additive hypotensive effect

Drug contraindications

excessive sensitivity to the drug or its component

• Epoprostenol is contraindicated in patients with heart failure caused by reduced left ventricular ejection fraction. • Epoprostenol is contraindicated in patients with a hypersensitivity to the drug or any of its ingredients.

Pregnancy level

B

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