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Trade Names:
Flolan
- Powder for reconstitution 0.5 mg
- Powder for reconstitution 1.5 mg

Mechanism of Action

Pharmacology

Direct vasodilation of pulmonary and systemic arterial vascular beds; inhibition of platelet aggregation.

Pharmacokinetics

Metabolism

Rapidly hydrolyzed at neutral pH in blood and also undergoes enzymatic degradation. Metabolized to 2 primary active metabolites and several inactive metabolites.

Elimination

The t _½ is approximately 6 min. Excreted mostly in the urine and a small amount in the feces.

Indications and Usage

Treatment of primary pulmonary hypertension (PPH) and pulmonary hypertension associated with scleroderma spectrum of disease in New York Heart Association (NYHA) class III and class IV patients.

Contraindications

Chronic use in patients with CHF caused by severe left ventricular systolic dysfunction; hypersensitivity to structurally related compounds or to the drug or any component of the product.

Dosage and Administration

IV Initiate infusion at 2 ng/kg/min and increase in increments of 2 ng/kg/min every 15 min or longer until dose-limiting pharmacologic effects are elicited or until a tolerance limit to the drug occurs. If dose-limiting pharmacologic effects occur, then decrease the infusion rate to an appropriate chronic infusion rate that is tolerated. If the initial infusion rate is not tolerated, identify a lower dose that is tolerated.

Increase infusion by 1 to 2 ng/kg/min increments at intervals sufficient to allow assessment of clinical response (15 min or more).

Gradually make 2 ng/kg/min decrements every 15 min or longer until dose-limiting effects resolve.

General Advice

• Reconstitute as directed using sterile diluent for epoprostenol. Do not reconstitute or mix with any other parenteral medications or solutions.
• Must be administered through a central venous catheter only. Temporary peripheral IV infusions may be used until central access is established.
• Inspect for particulate matter and discoloration prior to administration.
• Consider increments in dose if symptoms of pulmonary hypertension persist or recur after improving.

Storage/Stability

• Store unopened vials at 59° to 77°F. Protect from light.
• Reconstituted medication may be stored for up to 40 h in refrigerator (36° to 46°F). Do not freeze. Protect from light.
• Discard any solution that has been refrigerated for more than 48 h or has been frozen.
• A single dose can be administered over 8 h at room temperature, and then must be discarded.
• Store vials of diluent at 59° to 77°F.
• Cold pouch administration can be used up to 24 h.
• Do not expose to direct sunlight. Insulate solution from temperatures higher than 77°F and lower than 32°F.
• Do not reconstitute or mix with any other parenteral medications or solutions prior or during administration.

Drug Interactions

May increase risk of bleeding.

May cause additional reductions in BP.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Tachycardia (35%); heart failure (31%); hypotension (16%); syncope (13%); bradycardia (5%).

CNS

Dizziness, headache (83%); anxiety/nervousness/tremor (21%); hyperesthesia/hypesthesia/paresthesia (12%); agitation (11%); dizziness (8%).

Dermatologic

Flushing (58%); sweating (1%).

GI

Nausea/vomiting (67%); diarrhea (37%); abdominal pain (5%); dyspepsia (1%).

Musculoskeletal

Jaw pain (54%); myalgia (44%); nonspecific musculoskeletal pain (35%); musculoskeletal pain (3%); back pain (2%).

Respiratory

Hypoxia (25%); dyspnea (2%).

Miscellaneous

Chills/fever/flu-like symptoms/sepsis (25%); chest pain (11%); anemia, hypersplenism, hyperthyroidism, pancytopenia, splenomegaly (postmarketing).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use caution in dose selection, reflecting greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Abrupt withdrawal

May result in symptoms associated with rebound pulmonary hypertension, including asthenia, dizziness, and dyspnea.

Pulmonary edema

May result during dose ranging in patients with PPH. If this occurs, discontinue medication.

Overdosage

Symptoms

Diarrhea, flushing, headache, hypotension, nausea, tachycardia, vomiting.

Patient Information

• Instruct patient and family that therapy for PPH may be required for months and even years and that commitment is required for drug reconstitution, drug administration, and proper care of the permanent central venous catheter.
• Instruct patient that the medication is infused continuously through a permanent indwelling central venous catheter by an infusion pump.
• Warn patient that even brief interruptions in the delivery of the medication will result in rapid return of symptoms.
• Provide appropriate instructions for home administration (eg, mixing, administration, rate, catheter care).
• Advise patient that this therapy is added to, and does not replace, other therapy that has been prescribed for PPH.
• Advise patient to not change the dose or discontinue therapy unless advised by health care provider.