No

Prostaglandin

Temporary maintenance of patency of ductus arteriosus in neonates with ductal-dependent congenital heart disease until surgery can be performed. These defects include cyanotic (eg, pulmonary atresia, pulmonary stenosis, tricuspid atresia, Fallot's tetralogy, transposition of the great vessels) and acyanotic (eg, interruption of aortic arch, coarctation of aorta, hypoplastic left ventricle) heart disease; diagnosis and treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology; adjunct in the diagnosis of erectile dysfunction

X

Hyaline membrane disease or persistent fetal circulation and when a dominant left-to-right shunt is present; respiratory distress syndrome; hypersensitivity to the drug or components; conditions predisposing patients to priapism (sickle cell anemia, multiple myeloma, leukemia); patients with anatomical deformation of the penis, penile implants; use in men for whom sexual activity is inadvisable or contraindicated; pregnancy

Use cautiously in neonates with bleeding tendencies; apnea may occur in 10% to 12% of neonates with congenital heart defects, especially in those weighing <2 kg at birth; apnea usually appears during the first hour of drug infusion; when used in erectile dysfunction: priapism may occur; patient must be instructed to report to physician or seek immediate medical assistance if an erection persists greater than 4 hours. Treat immediately to avoid penile tissue damage and permanent loss of potency; discontinue therapy if signs of penile fibrosis develop (penile angulation, cavernosal fibrosis, or Peyronie's disease). When used in erectile dysfunction (Muse®), syncope occurring within 1 hour of administration, has been reported; the potential for drug-drug interactions may occur when Muse® is prescribed concomitantly with antihypertensives; some lowering of blood pressure may occur without symptoms, and swelling of leg veins, leg pain, perineal pain, and rapid pulse have been reported in <2% of patients during in-clinic titration and home treatment.

>10%:

Cardiovascular: Flushing

Central nervous system: Fever

Genitourinary: Penile pain

Respiratory: Apnea

1% to 10%:

Cardiovascular: Bradycardia, hypotension, hypertension, tachycardia, cardiac arrest, edema

Central nervous system: Seizures, headache, dizziness

Endocrine & metabolic: Hypokalemia

Gastrointestinal: Diarrhea

Genitourinary: Prolonged erection (priapism), penile fibrosis, penis disorder, penile rash, penile edema

Hematologic: Disseminated intravascular coagulation

Local: Injection site hematoma, injection site bruising

Neuromuscular & skeletal: Back pain

Respiratory: Upper respiratory infection, flu syndrome, sinusitis, nasal congestion, cough

Miscellaneous: Sepsis, localized pain in structures other than the injection site

<1%: Cerebral bleeding, congestive heart failure, second degree heart block, shock, supraventricular tachycardia, ventricular fibrillation, hyperemia, hyperirritability, hypothermia, jitteriness, lethargy, hypoglycemia, hyperkalemia, gastric regurgitation, anuria, balanitis, urethral bleeding, penile numbness, yeast infection, penile pruritus and erythema, abnormal ejaculation, anemia, bleeding, thrombocytopenia, hyperbilirubinemia, hyperextension of neck, stiffness, hematuria, bradypnea, bronchial wheezing, peritonitis, leg pain, perineal pain

Symptoms of overdose when treating patent ductus arteriosus include apnea, bradycardia, hypotension, and flushing

If hypotension or pyrexia occurs, the infusion rate should be reduced until the symptoms subside, while apnea or bradycardia requires drug discontinuation; if intracavernous overdose occurs, supervise until any systemic effects have resolved or until penile detumescence has occurred

Ductus arteriosus: Refrigerate ampuls; protect from freezing; prepare fresh solutions every 24 hours; compatible in D₅W, D₁₀W, and NS solutions

Erectile dysfunction: Refrigerate at 2°C to 8°C until dispensed; after dispensing, stable for up to 3 months at or below 25°C; do not freeze; use only the supplied diluent for reconstitution (ie, bacteriostatic/sterile water with benzyl alcohol 0.945%)

Causes vasodilation by means of direct effect on vascular and ductus arteriosus smooth muscle; relaxes trabecular smooth muscle by dilation of cavernosal arteries when injected along the penile shaft, allowing blood flow to and entrapment in the lacunar spaces of the penis (ie, corporeal veno-occlusive mechanism)

Onset of action: Rapid

Duration: <1 hour

Distribution: Nonsignificant amounts distribute peripherally following penile injection

Protein binding, plasma: 81% to albumin

Metabolism: ~75% metabolized by oxidation in one pass through the lungs

Half-life: 5-10 minutes

Elimination: Metabolites excreted in urine (90% within 24 hours)

Patent ductus arteriosus (Prostin VR Pediatric®):

I.V. continuous infusion into a large vein, or alternatively through an umbilical artery catheter placed at the ductal opening: 0.05-0.1 mcg/kg/minute with therapeutic response, rate is reduced to lowest effective dosage; with unsatisfactory response, rate is increased gradually; maintenance: 0.01-0.4 mcg/kg/minute

PGE₁ is usually given at an infusion rate of 0.1 mcg/kg/minute, but it is often possible to reduce the dosage to 1/2 or even 1/10 without losing the therapeutic effect. The mixing schedule is as follows. Infusion rates deliver 0.1 mcg/kg/minute:

• For a concentration of 2 mcg/mL, add 500 mcg* to 250 mL; infuse at 0.05 mL/kg/minute (72 mL/kg/24 hours)
• For a concentration of 5 mcg/mL, add 500 mcg* to 100 mL; infuse at 0.02 mL/kg/minute (28.8 mL/kg/24 hours)
• For a concentration of 10 mcg/mL, add 500 mcg* to 50 mL; infuse at 0.01 mL/kg/minute (14.4 mL/kg/24 hours)
• For a concentration of 20 mcg/mL, add 500 mcg* to 20 mL; infuse at 0.005 mL/kg/minute (7.2 mL/kg/24 hours)

*500 mcg equals 1 ampul

Therapeutic response is indicated by increased pH in those with acidosis or by an increase in oxygenation (pO₂) usually evident within 30 minutes

Erectile dysfunction

Caverject®, Edex®:

Vasculogenic, psychogenic, or mixed etiology: Individualize dose by careful titration; usual dose: 2.5-60 mcg (doses >60 mcg are not recommended); initiate dosage titration at 2.5 mcg, increasing by 2.5 mcg to a dose of 5 mcg and then in increments of 5-10 mcg depending on the erectile response until the dose produces an erection suitable for intercourse, not lasting >1 hour; if there is absolutely no response to initial 2.5 mcg dose, the second dose may increased to 7.5 mcg, followed by increments of 5-10 mcg

Neurogenic etiology (eg, spinal cord injury): Initiate dosage titration at 1.25 mcg, increasing to a doses of 2.5 mcg and then 5 mcg; increase further in increments 5 mcg until the dose is reached that produces an erection suitable for intercourse, not lasting >1 hour

Note: Patient must stay in the physician's office until complete detumescence occurs; if there is no response, then the next higher dose may be given within 1 hour; if there is still no response, a 1-day interval before giving the next dose is recommended; increasing the dose or concentration in the treatment of impotence results in increasing pain and discomfort

Muse® Pellet: Intraurethral: Administer as needed to achieve an erection; duration of action is about 30-60 minutes; use only two systems per 24-hour period

Arterial pressure, respiratory rate, heart rate, temperature, degree of penile pain, length of erection, signs of infection

May cause dizziness; rarely may produce irritability

May cause seizures; use caution with clozapine and bupropion

No information available to require special precautions

No effects or complications reported

Use only as directed, no more than 3 times/week, allowing 24 hours between injections. Store in refrigerator and dilute with supplied diluent immediately before use. Use alternate sides of penis with each injection. Dispose of syringes and needle and single dose vials in a safe manner (do not share medication, syringes, or needles). Note that the risk of transmitting blood-borne disease is increased with use of alprostadil injections since a small amount of bleeding at injection site is possible. Stop using alprostadil and contact prescriber immediately if signs of priapism occur, erections last more than 4 hours, or you experience moderate to severe penile pain. Report penile problems (eg, nodules, new penile pain, rash, bruising, numbness, swelling, signs of infection, abnormal ejaculations); cardiac symptoms (hypo- or hypertension, chest pain, palpitations, irregular heartbeat); flushing, fever, flu-like symptoms; difficulty breathing, or wheezing; or other adverse reactions. Refer to prescriber every 3 months to ensure proper technique and for dosage evaluation. Pregnancy precautions: This drug will cause severe fetal defects. Consult prescriber for appropriate barrier contraception education for you and your sexual partner(s). Do not give blood while taking this medication and for 1 month following discontinuance.

Ductus arteriosus: Monitor arterial pressure; assess all vital functions; apnea and bradycardia may indicate overdose, stop infusion if occurring; infuse for the shortest time and at the lowest dose that will produce the desired effects. Flushing is usually a result of catheter malposition; central line preferred for I.V. administration.

Erectile dysfunction: Use a 1/2 ", 27- to 30-gauge needle; inject into the dorsolateral aspect of the proximal third of the penis, avoiding visible veins; alternate side of the penis for injections; if the patient is going to be self-injecting at home, carefully assess their aseptic technique for injection and knowledge of proper disposal of the syringe, needle and vial; observe for signs of infection, penile fibrosis, and significant pain or priapism

Injection:

Caverject®: 5 mcg, 10 mcg, 20 mcg

Edex® Injection: 5 mcg, 10 mcg, 20 mcg, 40 mcg

Prostin VR Pediatric®: 500 mcg/mL (1 mL)

Pellet, urethral: 125 mcg, 250 mcg, 500 mcg, 1000 mcg

Peled N, Dagan O, Babyn P, et al, "Gastric-Outlet Obstruction Induced by Prostaglandin Therapy in Neonates," N Engl J Med, 1992, 327(8):505-10.

Weesner KM, "Hemodynamic Effects of Prostaglandin E₁ in Patients With Congenital Heart Disease and Pulmonary Hypertension," Cathet Cardiovasc Diagn, 1991, 24(1):10-5.

Williams G, Abbou CC, Amar ET, et al, "The Effect of Transurethral Alprostadil on the Quality of Life of Men With Erectile Dysfunction, and Their Partners. MUSE Study Group," Br J Urol, 1998, 82(6):847-54.

Woo K, Emery J, and Peabody J, "Cortical Hyperostosis: A Complication of Prolonged Prostaglandin Infusion in Infants Awaiting Cardiac Transplantation," Pediatrics, 1994, 93(3):417-20.