Pronunciation:

(al PROS ta dill)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Prostin VR Pediatric®: 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

Caverject®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology; adjunct in the diagnosis of erectile dysfunction

Edex®, Muse®: Treatment of erectile dysfunction of vasculogenic, psychogenic, or neurogenic etiology

Use - Unlabeled/Investigational:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

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.

Adverse Reactions:

Intraurethral:

>10%: Genitourinary: Penile pain, urethral burning

2% to 10%:

Central nervous system: Headache, dizziness, pain

Genitourinary: Vaginal itching (female partner), testicular pain, urethral bleeding (minor)

<2%: Tachycardia, perineal pain, leg pain

Intracavernosal injection:

>10%: Genitourinary: Penile pain

1% to 10%:

Cardiovascular: Hypertension

Central nervous system: Headache, dizziness

Genitourinary: Prolonged erection (>4 hours, 4%), penile fibrosis, penis disorder, penile rash, penile edema

Local: Injection site hematoma and/or bruising

<1%: Balanitis, injection site hemorrhage, priapism (0.4%)

Intravenous:

>10%:

Cardiovascular: Flushing

Central nervous system: Fever

Respiratory: Apnea

1% to 10%:

Cardiovascular: Bradycardia, hyper-/hypotension, tachycardia, cardiac arrest, edema

Central nervous system: Seizures, headache, dizziness

Endocrine & metabolic: Hypokalemia

Gastrointestinal: Diarrhea

Hematologic: Disseminated intravascular coagulation

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%: Anemia, anuria, bleeding, bradypnea, bronchial wheezing, cerebral bleeding, CHF, gastric regurgitation, hematuria, hyperbilirubinemia, hyperemia, hyperextension of neck, hyperirritability, hyperkalemia, hypoglycemia, hypothermia, jitteriness, lethargy, peritonitis, second degree heart block, shock, stiffness, supraventricular tachycardia, thrombocytopenia, ventricular fibrillation

Overdosage/Toxicology:

Drug Interactions:

Ethanol/Nutrition/Herb Interactions:

Stability:

Caverject® Impulse™: Store at controlled room temperature of 15°C to 30°C (59°F to 86°F). Provided as a duel-chamber syringe with diluent in one chamber. To mix, hold syringe with needle pointing upward and turn plunger clockwise; turn upside down several times to mix. Device can be set to deliver specified dose, each device can be set at various increments. Following reconstitution, use within 24 hours and discard any unused solution.

Caverject® powder: The 5 mcg, 10 mcg, and 20 mcg vials should be stored at or below 25°C (77°F). The 40 mcg vial should be stored at 2°C to 8°C until dispensed. After dispensing, stable for up to 3 months at or below 25°C. Use only the supplied diluent for reconstitution (ie, bacteriostatic/sterile water with benzyl alcohol 0.945%). Following reconstitution, all strengths should be stored at or below 25°C (77°F); do not refrigerate or freeze; use within 24 hours.

Caverject® solution: Prior to dispensing, store frozen at -20°C to -10°C (-4°F to -14°F); once dispensed, may be stored frozen for up to 3 months, or under refrigeration at 2°C to 8°C (36°F to 46°F) for up to 7 days. Do not refreeze. Once removed from foil wrap, solution may be allowed to warm to room temperature prior to use. If not used immediately, solution should be discarded. Shake well prior to use.

Edex®: Store at controlled room temperature of 15°C to 30°C (59°F to 86°F); following reconstitution with NS, use immediately and discard any unused solution.

Muse®: Refrigerate at 2°C to 8°C (36°F to 46°F); may be stored at room temperature for up to 14 days.

Prostin VR Pediatric®: Refrigerate at 2°C to 8°C (36°F to 46°F); prior to infusion, dilute with D5W or NS; use within 24 hours.

Mechanism of Action:

Pharmacodynamics/Kinetics:

Onset of action: Rapid

Duration: <1 hour

Distribution: Insignificant following penile injection

Protein binding, plasma: 81% to albumin

Metabolism: ~75% by oxidation in one pass via lungs

Half-life elimination: 5-10 minutes

Excretion: Urine (90% as metabolites) within 24 hours

Dosage:

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: See table.

Erectile dysfunction::

Alprostadil

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®: Intracavernous: Individualize dose by careful titration; doses >40 mcg (Edex®) or >60 mcg (Caverject®) are not recommended: Initial dose must be titrated in physicians office. 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

Vasculogenic, psychogenic, or mixed etiology: 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 be 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 dose 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

Maintenance: Once appropriate dose has been determined, patient may self-administer injections at a frequency of no more than 3 times/week with at least 24 hours between doses

Muse® Pellet: Intraurethral:

Initial: 125-250 mcg

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

Elderly: Elderly patients may have a greater frequency of renal dysfunction; lowest effective dose should be used. In clinical studies with Edex®, higher minimally effective doses and a higher rate of lack of effect were noted.

Administration:

Monitoring Parameters:

Patient Education:

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

Injection, powder for reconstitution:

Caverject®: 10 mcg, 20 mcg, 40 mcg [contains lactose; diluent contains benzyl alcohol]

Caverject® Impulse™: 10 mcg, 20 mcg [prefilled injection system; contains lactose; diluent contains benzyl alcohol]

Edex®: 10 mcg, 20 mcg, 40 mcg [contains lactose; diluent contains benzyl alcohol; also packaged in kits containing diluent, syringe, and alcohol swab]

Injection, solution: 500 mcg/mL (1 mL)

Caverject® [DSC]: 20 mcg/mL (2 mL)

Prostin VR Pediatric®: 500 mcg/mL (1 mL) [contains dehydrated alcohol]

Pellet, urethral (Muse®): 125 mcg, 250 mcg, 500 mcg, 1000 mcg

International Brand Names: