Alprostadil

What is Alprostadil?

• Alprostadil (Caverject; Caverject Impulse; Edex; Muse) is a prostaglandin E1 agonist used to treat certain types of erectile dysfunction in men.
• Alprostadil injection is also sometimes used in combination with other tests to diagnose erectile dysfunction.
• In infants with congenital heart defects, it is delivered by slow injection into a vein to open the ductus arteriosus until surgery can be carried out.
• By injection into the penis or placement in the urethra, it is used to treat erectile dysfunction.
• It is also known as Prostaglandin E1.

Alprostadil

Alprostadil-BallStick

Alprostadil Structural Formula V1

What are the uses of this medicine?

Alprostadil is used to treat certain types of erectile dysfunction in men. Alprostadil injection is also sometimes used in combination with other tests to diagnose erectile dysfunction. In infants with congenital heart defects, it is delivered by slow injection into a vein to open the ductus arteriosus until surgery can be carried out. By injection into the penis or placement in the urethra, it is used to treat erectile dysfunction.

How does this medicine work?

In Patent ductus arteriosus:

• Alprostadil (prostaglandin E1) is one of a family of naturally occurring acidic lipids with various pharmacologic effects.
• Vasodilation, inhibition of platelet aggregation, and stimulation of intestinal and uterine smooth muscle are among the most notable of these effects.
• Smooth muscle of the ductus arteriosus is especially sensitive to alprostadil, and strips of lamb ductus markedly relax in the presence of the drug.

In erectile dysfunction:

• Alprostadil (PGE1) is a prostaglandin with a wide variety of pharmacological actions including vasodilation and inhibition of platelet aggregation.
• Alprostadil induces erection by relaxation of trabecular smooth muscle and by dilation of cavernosal arteries by binding to its receptors and increasing intracellular cyclic adenosine monophosphate (cAMP) levels via modulation of adenylate cyclase.
• This leads to expansion of lacunar spaces and entrapment of blood by compressing the venules against the tunica albuginea, a process referred to as the corporal veno-occlusive mechanism.
• Alprostadil also attenuates presynaptic noradrenaline release in the corpus cavernosum.

Who Should Not Use this medicine ?

This medicine cannot be used:

• in men who have a known hypersensitivity to the drug.
• in men who have conditions that predispose them to priapism, such as sickle cell anemia or sickle cell trait, multiple myeloma, or leukemia.
• for the treatment of erectile dysfunction in men with fibrotic conditions of the penis, such as anatomical deformation, angulation, cavernosal fibrosis, or Peyronie's disease.
• in men with penile implants.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• anticoagulants ('blood thinners') such as heparin and warfarin (Coumadin)
• appetite suppressants
• medications for allergies, colds, high blood pressure, or sinus problems
• any other treatments for erectile dysfunction.

Is this medicine FDA approved?

• Prostaglandin E1 was isolated in 1957 and approved for medical use in the United States in 1981.

How should this medicine be used?

Recommended dosage: In erectile dysfunction: Recommended dosage of (Caverject; Caverject Impulse) for erectile dysfunction:

• Erectile dysfunction of vasculogenic, psychogenic, or mixed etiology: Initiate dosing with 2.5 mcg.
• Erectile dysfunction of pure neurogenic etiology (spinal cord injury): Initiate dosing with 1.25 mcg.

Recommended dosage of (Edex) for erectile dysfunction:

• The dosage range of edex® for the treatment of erectile dysfunction is 1 to 40 mcg.

Recommended dosage of (Muse) for erectile dysfunction:

• The lower doses of MUSE (125 mcg or 250 mcg) are recommended for initial dosing. If necessary, the dose should be increased.

In Patent ductus arteriosus:

• Begin infusion with 0.05 to 0.1 micrograms alprostadil per kilogram of body weight per minute.
• A starting dose of 0.1 micrograms per kilogram of body weight per minute is the recommended starting dose based on clinical studies.

Administration:

• For Patent ductus arteriosus the preferred route of administration for alprostadil injection is continuous intravenous infusion into a large vein. Alternatively, alprostadil injection may be administered through an umbilical artery catheter placed at the ductal opening.
• For erectile dysfunction alprostadil comes as a powder to be mixed with the liquid provided in the package and injected into the penis and as a urethral suppository (pellet to be placed into the urinary opening of the penis).
• Alprostadil is used as needed before sexual activity.
• An erection may occur within 5 to 20 minutes after using the injection and within 5 to 10 minutes after using the pellet.
• The erection should last approximately 30 to 60 minutes.
• Alprostadil injection should not be used more than three times per week, with at least 24 hours between uses.
• Alprostadil pellets should not be used more than twice in a 24-hour period.
• Your doctor will administer the first dose of alprostadil in his or her office to determine the proper dose for you. After you begin to use alprostadil at home, your doctor may gradually increase or decrease your dose.
• You must be trained by your doctor before using alprostadil at home.
• Do not reuse needles, syringes, cartridges, vials , pellets, or applicators.
• Dispose of used needles and syringes in a puncture-resistant container.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As alprostadil injection.
• As a powder to be mixed with the liquid provided in the package and injected into the penis and as a urethral suppository.

This medicine is available in fallowing brand namesː

• Caverject; Caverject Impulse; Edex; Muse

What side effects can this medication cause?

The most common side effects of this medicine include:

• penile pain
• headache
• back pain
• skin problems
• vision problems

Alprostadil may cause serious side effects, including:

• priapism
• penile fibrosis
• hypotension
• injection site bleeding
• increased risk of heart problems
• needle breakage

What special precautions should I follow?

• Apnea is experienced by about 10 to 12% of neonates with congenital heart defects treated with alprostadil injection. Apnea is most often seen in neonates weighing less than 2 kg at birth and usually appears during the first hour of drug infusion. Therefore, respiratory status should be monitored throughout treatment, and alprostadil injection should be used where ventilatory assistance is immediately available.
• Prolonged erection and priapism have occurred in patients receiving CAVERJECT. To minimize the chances of this occurring, titrate CAVERJECT slowly to the lowest effective dose. Advise patients to seek immediate medical assistance for an erection that persists longer than 4 hours.
• Penile fibrosis has occurred in patients receiving CAVERJECT. Follow patients regularly to detect signs of penile fibrosis. Discontinue in patients who develop penile angulation or cavernosal fibrosis.
• Injections of CAVERJECT can lead to increased peripheral blood levels of alprostadil, especially in patients with significant corpora cavernosa venous leakage. Avoid use in patients with known cavernosal venous leakage.
• Injection site bleeding may occur in patients taking anticoagulants, such as warfarin or heparin. Compress the site of injection with an alcohol swab or sterile gauze for 5 minutes.
• Underlying treatable medical causes of erectile dysfunction should be diagnosed and treated prior to initiation of therapy.
• Safety and efficacy of combinations of CAVERJECT and other vasoactive agents have not been systematically studied. Use of such combinations is not recommended.
• CAVERJECT uses a superfine needle and cases of needle breakage have been reported. Careful instruction in proper patient handling and injection techniques may minimize this risk.
• Serious and fatal adverse reactions can occur in neonates and low birth weight infants treated with benzyl alcohol-preserved formulations in infusion solutions, including CAVERJECT. CAVERJECT is not indicated in neonates and infants.
• Counsel patients about the protective measures necessary to guard against sexually transmitted disease including the Human Immunodeficiency Virus (HIV).

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• fainting
• dizziness
• blurred vision
• nausea
• pain in the penis that does not go away
• erection lasting longer than 6 hours

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Treatment of any systemic symptoms (e.g., hypotension) would be appropriate.

Can this medicine be used in pregnancy?

• Alprostadil is not indicated for use in females.

Can this medicine be used in children?

• Safety and effectiveness for erectile dysfunction have not been established in pediatric patients.
• In infants with congenital heart defects, it is delivered by slow injection into a vein to open the ductus arteriosus until surgery can be carried out.

What are the active and inactive ingredients in this medicine?

CAVERJECT:

• Active ingredient: alprostadil
• Inactive ingredients: alpha cyclodextrin, lactose, sodium citrate, benzyl alcohol (contained in the final solution) and hydrochloric acid and/or sodium hydroxide for pH adjustment.

Who manufactures and distributes this medicine?

CAVERJECT;CAVERJECT IMPULSE:

• Pharmacia & Upjohn Company LLC
• Division of Pfizer Pharmaceuticals LLC.

Alprostadil injection USP Distributed by:

• Teva Pharmaceuticals USA, Inc.
• Parsippany, NJ

Edex: Distributed by:

• Endo Pharmaceuticals Inc.
• Malvern, PA

Muse: Distributed by:

• MEDA PHARMACEUTICALS®
• Somerset, New Jersey

What should I know about storage and disposal of this medication?

• Store alprostadil vials and cartridges at room temperature and away from excess heat and moisture (not in the bathroom).
• Alprostadil pellets should be stored in the original package in the refrigerator, but may be kept at room temperature for up to 14 days before use.
• Do not expose the medication to high temperatures or place it in direct sunlight since this will make it ineffective.

• Dailymed label info on Alprostadil
• FDA Alprostadil

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