ALPROSTADIL (Local)

Some commonly used brand names are:

In the U.S.?

• Caverject
• Edex
• Muse
• Prostin VR Pediatric

In Canada?

• Caverject
• Prostin VR

Other commonly used names are PGE ₁ and prostaglandin E ₁.

Category

• Impotence therapy agent
• Diagnostic aid, erectile dysfunction
• Diagnosticaid, penile vasculature imaging

Description

Alprostadil (al-PROS-ta-dil) belongs to a group of medicines called vasodilators thatcan increase blood flow by expanding blood vessels. Alprostadil is used toproduce erections in some men who need treatment for erectile dysfunction(sexual impotence). This medicine causes an erection because it increasesthe blood flow to the penis.

Alprostadil injection should not be used as a sexual aid by men who donot have erectile dysfunction. If the medicine is not used properly, permanentdamage to the penis and loss of the ability to have erections could result.

Alprostadil is used alone or with medical tests to help diagnose erectiledysfunction that may be caused by nerve or blood vessel problems in the penis.

Alprostadil is available only with your doctor's prescription, in the followingdosage forms:

Intraurethral
• Suppositories (U.S.)

Parenteral
• Injection (U.S. and Canada)

Before Using This Medicine

In deciding to use a medicine,the risks of using the medicine must be weighed against the good it will do.This is a decision you and your doctor will make. For alprostadil, the followingshould be considered:

Allergies?Tell your doctor if you have ever had any unusual orallergic reaction to alprostadil. Also tell your health care professionalif you are allergic to any other substances, such as foods, preservatives,or dyes.

Older adults?This medicine has been tested and has not been shownto cause different side effects or problems in older people than it does inyounger adults.

Other medicines?Although certain medicines should not be usedtogether at all, in other cases two different medicines may be used togethereven if an interaction might occur. In these cases, your doctor may want tochange the dose, or other precautions may be necessary. Tell your health careprofessional if you are taking any other prescription or nonprescription (over-the-counter[OTC]) medicine.

Other medical problems?The presence of other medicalproblems may affect the use of alprostadil. Make sure you tell your doctorif you have any other medical problems, especially:

• Abnormal penis, including curved penis and birth defects of the penis?Chanceof problems occurring may be increased

• Bleeding problems?Chance of bleeding at the place of injectionmay be increased

• Infection of penis or
• Red or itchy (inflamed) penis?Conditions may worsen with theuse of alprostadil suppositories. Also, local skin problems and minor bleedingfrom inserting the suppository may occur

• Conditions causing thickened blood or slower blood flow, includingleukemia; multiple myeloma (tumors of the bone marrow); polycythemia, sicklecell disease, or thrombocythemia (blood problems) or

• Priapism (history of)?Patients with these conditions have anincreased risk of priapism (erection lasting longer than 6 hours) while usingalprostadil

Proper Use of This Medicine

Special patientdirections come with the suppositories and some of the injection medicines. Read the directions carefully before using the medicine.

For the injections?There are several alprostadil products that canbe injected. Although the injection method is the same, the mixing proceduresare different. Be sure you know which of these productsyou will be using and the proper way to mix the injection.

• One product called Alprostadil for Injection (brand names Caverject and Edex) is availableas a powder in an injection bottle (vial). Caverject must be mixed with a solution called Bacteriostatic Water for InjectionUSP. Edex must be mixed with a solution calledSodium Chloride Injection USP. The solution for mixing comes with your productand may be already loaded into a syringe or contained in another injectionbottle (vial).
• Another product is called Alprostadil Injection (brand names Prostin VR Pediatric and ProstinVR). Although the medicine is already in solution, it is much too strongto be injected into the penis. The solution must be mixed (diluted) with anotherliquid that is sold as a separate prescription, called 0.9% Sodium ChlorideInjection USP. In most cases, a pharmacist will make this solution for you,giving you the proper strength that you need. Check with your doctor or pharmacistto make sure the solution has been diluted before using it.

It is important to follow several steps to prepare your alprostadil injectioncorrectly. Before drawing up the medicine into the syringe:

• Wash your hands with soap and water.
• Set the bottles on a clean surface. Wipe the top of the injectionbottles with an alcohol swab. Do not wipe the needle. Throw away the alcohol swab.
• You may need to attach the needle to the syringe. Do not take thecap off yet.

How to mix Caverject:

• If the syringe already contains the Bacteriostatic Water for InjectionUSP, then you need only add the plunger to the syringe. To do this:
  • Pick up the rod-like plunger and place it within the barrel of thesyringe until it touches the rubber piece. Gently screw the plunger into therubber piece until it seems secure. Do not use a lot of force.
  • Hold the syringe by the barrel (not the plunger) and take the capoff the needle.
  • You are now ready to mix the water and the powder. Skip to the directionsunder the title, ? To mix the water and powder.?
• If the syringe does not already contain the Bacteriostatic Waterfor Injection USP, you must withdraw 1 milliliter (mL) of it from the bottleprovided. To do this:
  • Pick up the syringe and take the cap off the needle.
  • Pull the plunger back to the 1-mL mark on the syringe. This pullsair into the syringe. Insert the needle into rubber top of the bottle whileit is upright and inject the 1 mL of air into the bottle.
  • Turn the bottle upside down using one hand. Be sure the tip of theneedle is covered by solution.
  • With your other hand, pull the plunger back slowly to withdraw 1mL of solution into the syringe. Remove the needle and skip to the directionsunder the title, ? To mix the water and powder.?
• To mix the water and powder:
  • Insert the needle into the bottle of alprostadil and inject 1 milliliterof Bacteriostatic Water for Injection USP from your syringe into the bottleof alprostadil.
  • Remove the needle from the bottle, holding the barrel of the syringe.
  • Gently swirl the bottle to mix the powder into the solution, turningit upside down to wet all the powder in the bottle.
  • Follow the directions below, ? How to drawyour dose into the syringe.?

How to mix Edex:

• The syringe already contains the Sodium Chloride Injection USP. Youneed only attach the needle to the syringe and add the plunger. To do this:
  • Remove the needle from its package. Do not remove the needle cap.Gently screw the needle into place on the syringe tip.
  • Pick up the rod-like plunger and place it within the barrel of thesyringe until it touches the rubber piece. Gently screw the plunger into therubber piece until it seems secure. Do not use a lot of force.
  • Hold the syringe by the barrel (not the plunger) and take the capoff the needle.
  • You are now ready to mix the Sodium Chloride Injection USP and thepowder.
  • Insert the needle into the bottle of alprostadil and inject 1.2 millilitersof the Sodium Chloride Injection USP from your syringe into the bottle ofalprostadil.
  • Remove the needle from the bottle, holding the barrel of the syringe.
  • Gently swirl the bottle to mix the powder into the solution, turningit upside down to wet all the powder in the bottle.
  • Follow the directions below, ? How to drawyour dose into the syringe.?

How to mix Prostin VR or Prostin VR Pediatric:

• You will need to get exact mixing instructions from your doctor orpharmacist if you are given two solutions to be mixed. Follow them carefully,asking the pharmacist or doctor any questions that you might have before injectingthe medicine.
• After you or the pharmacist has mixed these solutions, follow thedirections below, ? How to draw your dose into thesyringe.?

How to draw your dose into the syringe (for all injectionproducts):

• Check the solution to make sure it is clear. Do not use the mixture if you can see anything solid in the solution or ifthe solution is cloudy or colored.
• After the alprostadil solution is mixed and the needle is insertedinto the alprostadil bottle, turn the bottle with the syringe as a unit upsidedown in one hand. Be sure the tip of the needle is covered by the solution.With your other hand, pull the plunger back slowly to draw the correct doseof the medicine into the syringe.
• Hold the syringe with the measuring scale at eye level to see thatthe proper dose is withdrawn and to check for air bubbles. To remove air bubbles,tap gently on the measuring scale of the syringe to move any bubbles to thetop of the syringe near the needle.
• If your dose measures too low in the syringe, withdraw more solutionfrom the bottle. If there is too much medicine in the syringe, put some backinto the bottle. Then check your dose again.
• Remove the needle from the bottle, holding the barrel of the syringe,not the plunger.
• Place the cover back on the needle. You are now ready to inject yourdose. Follow the directions below, ? How to givethe alprostadil injection.?

How to give the alprostadil injection:

• Choose a spot on your penis as directed by your doctor where youwill give the injection.
• Clean the injection site with alcohol. Sitting upright or slightlyreclined, hold your penis against the side of your thigh so that it cannotmove.
• Remove the cover from the needle and hold the needle at a 90-degreeangle to the place of injection.
• Insert the needle until almost all of the metal part of the needleis inserted into the penis.
• Do not inject the medicine just under the surface of the skin, atthe top or head of the penis, or at the base of the penis near the scrotumor testes. Avoid injecting the medicine into blood vessels that you can see.
• Press the plunger down slowly, taking 5 to 10 seconds to releasethe dose into the penis.
• The injection is usually not painful. If the injection is very painfulor if you notice bruising or swelling at the place of injection, that meansyou are injecting the medicine under the skin. Stop, withdraw the needle,and reposition it properly before continuing with the injection.
• Remove the needle and recap it.
• After you have completed the injection, put pressure on the placeof injection for about 5 minutes or until any bleeding stops. This will preventbruising. Then massage your penis as instructed by your doctor. This helpsthe medicine spread to all parts of the penis, so that the medicine will workbetter.

Choose a different place of injection each time you use the medicine toprevent skin problems. This includes switching the place of injection fromthe right side of the penis for one injection to the left side for the nextinjection.

After a single-use injection is mixed, the medicine must be used immediately.Throw away any unused mixture in the syringe. It cannot be stored for a laterinjection.

Do not reuse your needles.

How to throw away the syringes and bottlessafely:

Dispose of your materials properly. Caverjectcomes in a plastic case that can be permanently locked with the red lockingdevice that is included with the packaging. When the case label is removed,you can see a hole in the center of the case. The red locking device can beinserted and, by firmly pressing it down with your thumb, you will permanentlylock the case. The locked case is safe to be thrown away.

If you do not have the plastic case or are using Prostin VR or Prostin VR Pediatric injection,unscrew the needle from the barrel of the syringe. Then bend, break, or cutthe needle into two pieces with wire cutters. The pieces can be placed ina heavy plastic container, such as a bleach container, and thrown away. Oryou may give them to a health care professional to throw away. If you haveany questions about disposing of the syringe and needles, ask your healthcare professional.

For suppositories?Before inserting the suppository,you should urinate. The small amount of urine normally left in yoururethra will help dissolve the suppository after it is inserted.

How to insert suppositories:

• Remove the delivery device containing the suppository from the foil.Remove the cap from the applicator stem.
• Stretch your penis upward to extend its length, pressing your penistop and bottom. Gently insert the delivery stem up to its collar into yoururethra (located at the top of the penis). If you havepain or a pulling feeling in the penis, withdraw the device and start again.
• Press the button down slowly as far as it will go. This releasesthe suppository into the urethra. After holding the delivery device withinyour penis still for 5 seconds, carefully rock the penis and delivery deviceas a unit from side to side. This helps remove the suppository from the device.
• Remove the delivery device while your penis is upright. Look at thedevice to make sure that the suppository was completely released.
• Repeat the process if a part of the suppository remains in the device.
• After the suppository is completely released, roll your penis betweenyour hands for 10 seconds. This helps to dissolve the suppository. If youfeel any stinging, continue this motion to help stop it.
• Sitting, standing, or walking for 10 minutes while an erection isdeveloping helps increase the blood flow to your penis to gain a proper erection.

How to throw away the suppository delivery device safely:

• Replace the cap on the delivery device. After storing it in the foil,fold and throw away.

For injections or suppositories?This medicine usually begins to workin about 5 to 10 minutes. You should attempt intercourse within 10 to 30 minutesafter using the medicine. An erection may continue after ejaculation.

Dosing?The dose of alprostadil will be different fordifferent patients. Follow your doctor's orders or thedirections on the label. The following information includes only theaverage doses of alprostadil. If your dose is different,do not change it unless your doctor tells you to do so.

• For the treatment of erectile dysfunction:
  • For injection dosage form:
    • Adults?1.25 to 60 micrograms (mcg) as a single dose once aday. Your exact dose will be determined by your doctor. Inject this medicinevery slowly into your penis as shown to you by your doctor ten to thirty minutesbefore intercourse. Allow five to ten seconds to completely inject the dose.Do not inject more than one dose within twenty-four hours. Also, do not usethis medicine for more than two days in a row or more than three times a week.
  • For suppository dosage form:
    • Adults?125, 250, 500, or 1000 mcg as a single dose once a day.Your exact dose will be determined by your doctor. Insert this medicine intothe urethra of your penis as shown to you by your doctor ten to thirty minutesbefore intercourse. Do not insert more than two doses within twenty-four hours.

Storage?To store this medicine:

• Keep out of the reach of children.
• Refrigerate Alprostadil Injection USP. Keep the medicine from freezing.
• Alprostadil for Injection while in the powder form can be storedat room temperature (between 15 and 25 ?C or 59 and 77 ?F) for 3 months.After it is mixed, the solution must be used immediately.
• Refrigerate alprostadil suppositories. Keep from freezing. They maybe stored at room temperature for 14 days.
• Do not keep outdated medicine or medicine no longer needed. Be surethat any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

Do not use alprostadil if you have a penile implant unless advisedby doctor.

If using the alprostadil suppository, use a condomwhen having sexual intercourse with a pregnant female. Although harmto the fetus is unlikely, using a condom will protect the fetus from exposureto this medicine. If a woman can become pregnant, useof contraceptive methods is recommended because the effects of thismedicine on early pregnancy are not known.

Use alprostadil exactly as directed by your doctor. Do not use more of it and do not use it more often than your doctorordered. If too much is used, the erection lasts too long and does not reversewhen it should. This condition is called priapism. If the erection is notreversed, the blood supply to the penis may be cut off and permanent damagemay occur.

Contact your doctor immediately if the erection lastslonger than 4 hours or if it becomes painful. This may be a sign ofpriapism and must be treated right away to prevent permanent damage.

If you notice bleeding at the place where you injected the medicine, putpressure on the spot until the bleeding stops. If it doesn't stop within 10minutes, check with your doctor.

Side Effects of This Medicine

Along with its needed effects, a medicine may cause some unwanted effects.Although not all of these side effects may occur, if they do occur they mayneed medical attention.

Check with your doctorimmediately if the following side effects occur:

Rare

Curving of penis with pain during erection; erection continuing for 4 to 6 hours; erection continuinglonger than 6 hours with severe and continuing pain of the penis; swelling in or pain of the testes

Symptoms of too much medicine being absorbed into the body

Dizziness; faintness; pelvic pain; flu-like symptoms

Other sideeffects may occur that usually do not need medical attention. These side effectsmay go away during treatment as your body adjusts to the medicine. However,check with your doctor if any of the following side effects continue or arebothersome:

More common

Bleeding at place of injection, short-term; mild bleeding or spotting from urethra (suppository only); pain at place of injection; painful erection; stinging of urethra (suppository only)

Rare

Bruising or clotted blood in penis at place of injection, usuallycaused by an incorrect injection

Female partners may experienceitching or stinging of vagina when you first begin using the alprostadil suppository.These side effects may not be caused from the medicine but may result if femalepartner has not had frequent or recent sexual intercourse.

Other side effects not listed abovemay also occur in some patients. If you notice any other effects, check withyour doctor.