Opana ER

Keep all appointments with your doctor.

This prescription is not refillable. If you are taking oxymorphone to control your pain on a long term basis, be sure to schedule appointments with your doctor regularly so that you do not run out of medication. If you are taking oxymorphone on a short term basis, call your doctor if you continue to have pain after you finish the medication.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Mechanism of Action

Opioid agonist; inhibits ascending pain pathways, thus altering response to pain; produces analgesia, respiratory depression, and sedation  

Absorption

Bioavailability: 10% (PO)

Onset: 5-10 min

Duration: 3-6 hr

Distribution

Protein bound: 10-12%

Vd: IV, 1.94-4.22 L/kg

Metabolism

Metabolized in liver via conjugation

Elimination

Half-life: Immediate release, 7-9 hr; extended release, 9-11 hr

Excretion: Urine, feces

Opana ER is a prescription medication used to treat moderate to severe pain. Opana ER belongs to a group of drugs called called opiate (narcotic) analgesics. These work by changing the way the body responds to pain.

This medication comes in an extended release tablet form and is taken every 12 hours (twice daily). It is taken on an empty stomach, at least 1 hour before or 2 hours after meals. 

Do not crush, chew, or break tablets. Swallow Opana ER tablets whole. 

Common side effects include constipation, nausea, and headache.

Opana ER can also cause drowsiness and dizziness. Do not drive or operate heavy machinery until you know how it affects you.

Opana ER is part of the drug class:

• Natural opium alkaloids

If you will be taking this medicine for a long time, it is very important that your doctor check you at regular visits for any problems or unwanted effects that may be caused by this medicine.

This medicine may cause serious allergic reactions, including anaphylaxis and angioedema. Anaphylaxis can be life-threatening and requires immediate medical attention. Call your doctor right away if you have a rash, itching, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth while you are using this medicine.

Oxymorphone may increase your risk of having serious breathing problems. Check with your doctor right away if you are having difficult or troubled breathing, irregular, fast, slow, or shallow breathing, pale or blue lips, fingernails, or skin, or shortness of breath.

Do not use more of this medicine or take it more often than your doctor tells you to. This can be life-threatening. Symptoms of an overdose include extreme dizziness or weakness, slow heartbeat or breathing, seizures, trouble breathing, and cold, clammy skin. Call your doctor right away if you notice these symptoms.

This medicine will add to the effects of alcohol and other CNS depressants (medicines that can make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for hay fever, other allergies, or colds, sedatives, tranquilizers, or sleeping medicine, other prescription pain medicine or narcotics, medicine for seizures or barbiturates, muscle relaxants, or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the other medicines listed above while you are using this medicine.

This medicine may be habit-forming. If you feel that the medicine is not working as well, do not use more than your prescribed dose. Call your doctor for instructions.

Oxymorphone may cause some people to become drowsy, dizzy, or lightheaded, or to feel a false sense of well-being. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy, not alert, or lightheaded.

Dizziness, lightheadedness, or even fainting may occur when you get up suddenly from a lying or sitting position. Getting up slowly may help lessen this problem. Also, lying down for a while may relieve dizziness or lightheadedness.

Check with your doctor right away if you have anxiety, restlessness, a fast heartbeat, fever, sweating, muscle spasms, twitching, nausea, vomiting, diarrhea, or see or hear things that are not there. These may be symptoms of a serious condition called serotonin syndrome. Your risk may be higher if you also take certain other medicines that affect serotonin levels in your body.

Using this medicine for a long time can cause severe constipation. To prevent this, your doctor may direct you to take laxatives, drink a lot of fluids, or increase the amount of fiber in your diet. Be sure to follow the directions carefully, because continuing constipation can lead to more serious problems.

Before having any kind of surgery (including dental surgery) or emergency treatment, tell the medical doctor or dentist in charge that you are using this medicine. Serious side effects can occur if your medical doctor or dentist gives you certain other medicines without knowing that you are using oxymorphone.

If you have been using this medicine regularly for several weeks or more, do not change your dose or suddenly stop using it without first checking with your doctor. Your doctor may want you to gradually reduce the amount you are taking before stopping it completely. Withdrawal side effects may occur when the medicine is stopped suddenly because your body has become used to this medicine.

Tell your doctor if you are pregnant or plan to become pregnant while taking this medication. Using this medicine while you are pregnant may cause neonatal withdrawal syndrome in your newborn baby, which can be life-threatening. Tell your doctor right away if your baby has the following symptoms: abnormal sleep pattern, diarrhea, high-pitched cry, irritability, shakiness or tremor, weight loss, vomiting, or failure to gain weight.

Using too much of this medicine may cause infertility (unable to have children). Talk with your doctor before using this medicine if you plan to have children.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

• Tell all of your health care providers that you take Opana ER. This includes your doctors, nurses, pharmacists, and dentists.
• Avoid driving and doing other tasks or actions that call for you to be alert until you see how this medicine affects you.
• To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
• Do not take more than what your doctor told you to take. Taking more than you are told may raise your chance of very bad side effects.
• Do not take Opana ER (oxymorphone extended-release tablets) with other strong pain drugs or if you are using a pain patch without talking to your doctor first.
• Do not stop taking this medicine all of a sudden without calling your doctor. You may have a greater risk of signs of withdrawal. If you need to stop Opana ER, you will want to slowly stop it as ordered by your doctor.
• Allergic reactions have happened with this medicine. Rarely, some reactions can be very bad or life-threatening. Talk with the doctor.
• If you have been taking Opana ER for a long time or at high doses, it may not work as well and you may need higher doses to get the same effect. This is known as tolerance. Call your doctor if this medicine stops working well. Do not take more than ordered.
• Long-term use of an opioid drug like Opana ER may lead to lower sex hormone levels. This may lead to signs like change in sex ability in men, no menstrual period in women, lowered interest in sex, or fertility problems. Call your doctor if you have any of these signs.
• This medicine may raise the chance of seizures in some people, including people who have had seizures in the past. Talk to your doctor to see if you have a greater chance of seizures while taking this medicine.
• If you are 65 or older, use Opana ER with care. You could have more side effects.
• This medicine may cause harm to the unborn baby if you take it while you are pregnant. If you are pregnant or you get pregnant while taking this medicine, call your doctor right away.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Hard stools (constipation).
• Dizziness.
• Feeling sleepy.
• Dry mouth.
• Gas.
• Headache.
• Itching.
• Upset stomach or throwing up.
• Sweating a lot.
• Feeling tired or weak.
• Belly pain.
• You may see the tablet shell in your stool. This is normal and not a cause for concern.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Extended Release Tablets 5 mg:  pink, round, film-coated, biconcave extended-release tablet debossed with an “E” on one side and a “5” on the other side.

Extended Release Tablets 7.5 mg:  gray, round, film-coated, biconcave extended-release tablet debossed with an “E” on one side and a “7 ½” on the other side.

Extended Release Tablets 10 mg: light orange, round, film-coated, biconcave extended-release tablet debossed with an “E” on one side and a “10” on the other side.

Extended Release Tablets 15 mg: white, round, film-coated, biconcave extended-release tablet debossed with an “E” on one side and a “15” on the other side.

Extended Release Tablets 20 mg: light green, round, film-coated, biconcave extended-release tablet debossed with an “E” on one side and a “20” on the other side.

Extended Release Tablets 30 mg: red, round, film-coated, biconcave extended-release tablet debossed with an “E” on one side and a “30” on the other side.

Extended Release Tablets 40 mg: light yellow to pale yellow, round, film-coated, biconcave extended-release tablet debossed with an “E” on one side and a “40” on the other side.

Opana ER extended-release tablets are for oral use and contain oxymorphone, an opioid agonist.  Opana ER extended-release tablets are supplied in 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg, 30 mg, and 40 mg tablet strengths for oral administration.  The tablet strength describes the amount of oxymorphone hydrochloride per tablet.

The tablets contain the following inactive ingredients: hypromellose, polyethylene oxide, polyethylene glycol, α-tocopherol, citric acid, polyvinyl alcohol, titanium dioxide, macrogol and talc.

In addition, the 5 mg, 7.5 mg and 30 mg tablets contain iron oxide red. The 7.5 mg tablets contain iron oxide black, and iron oxide yellow. The 10 mg tablets contain FD&C yellow No. 6. The 20 mg tablets contain FD&C blue No. 1, FD&C yellow No. 6, and D&C yellow No. 10. The 40 mg tablets contain FD&C yellow No. 6, and D&C yellow No. 10.

The structural formula for oxymorphone hydrochloride is as follows: 

13.1  Carcinogenesis and Mutagenesis and Impairment of Fertility

Carcinogenesis

No evidence of carcinogenic potential was observed in long-term animal studies in mice and rats.  Oxymorphone hydrochloride was administered to Sprague Dawley rats (2.5, 5, and 10 mg/kg/day in males and 5, 10, and 25 mg/kg/day in females) for 2 years by oral gavage.  Systemic drug exposure (AUC) at the highest doses tested in male and female rats was 4.8 times and 21.2 times the human exposure at a dose of 20 mg/day, respectively.  Oxymorphone hydrochloride was administered to male and female CD-1 mice (10, 25, 75 and 150 mg/kg/day) for 2 years by oral gavage.  Systemic drug exposure (AUC) at 150 mg/kg/day in male and female mice was 205 times and 243 times the human exposure at a dose of 20 mg/day, respectively.

Mutagenesis

Oxymorphone hydrochloride was not mutagenic when tested in the in vitro bacterial reverse mutation assay (Ames test), or in an in vitro mammalian cell chromosome aberration assay performed with human peripheral blood lymphocytes.  Oxymorphone hydrochloride tested positive in both the rat and mouse in vivo micronucleus assays.  An increase in micronucleated polychromatic erythrocytes occurred in mice given doses ≥250 mg/kg and in rats given doses of 20 and 40 mg/kg.  A subsequent study demonstrated that oxymorphone hydrochloride was not aneugenic in mice following administration of up to 500 mg/kg.  Additional studies indicate that the increased incidence of micronucleated polychromatic erythrocytes in rats may be secondary to increased body temperature following oxymorphone administration. Doses associated with increased micronucleated polychromatic erythrocytes also produce a marked, rapid increase in body temperature. Pretreatment of animals with sodium salicylate minimized the increase in body temperature and prevented the increase in micronucleated polychromatic erythrocytes after administration of 40 mg/kg oxymorphone.

Impairment of Fertility

Female rats were treated with oxymorphone hydrochloride beginning 14 days prior to mating through Gestation Day 7 via oral gavage doses of 5, 10, or 25 mg/kg/day (2.4, 4.9, or 12.2 times the human daily dose of 20 mg/day based on body surface area, respectively).  Male rats were treated via oral gavage with the same oxymorphone hydrochloride doses beginning 28 days prior to and throughout mating.  In female rats, an increase in the length of the estrus cycle and decrease in the mean number of viable embryos, implantation sites and corpora lutea were observed at 4.9 times the human dose of 20 mg/day.  No adverse effects of oxymorphone on male reproductive function or sperm parameters were observed.