Oxymorphone / Opana

DESCRIPTION / DEFINITIONS: Opana is an opioid painkiller used for the management of acute pain severe enough to require an opioid painkiller but for which no other painkillers or treatment have been successful. The active ingredient is oxymorphone.

ABUSE: Opana’s high potential for abuse is the reason Opana is only recommended for those for whom no other painkiller has worked or is likely to.

ADDICTION / DEPENDENCE: The risk of addiction and dependence is very high even at recommended doses. See more information below.

SIDE EFFECTS:  Side effects include lightheadedness, loss of appetite, memory impairment, life-threatening respiratory depression, and seizures. See more information below.

WITHDRAWAL SYMPTOMS: Withdrawal symptoms with Opana can include anxiety, anorexia, insomnia, increased blood pressure, heart rate, or respiratory rate, and irregular heart beat. See list of common withdrawal symptoms below.

TREATMENT: Opana should not be stopped abruptly or without medical guidance. Medical detox facilities are available that make quitting Opana safe and more comfortable. See more below.

 

DESCRIPTION / DEFINITIONS

The formulation of Opana currently available is Opana IR (Immediate Release), although you may see it referred to as simply Opana. Opana ER (Extended Release) is also frequently mentioned online and even on government and other sites that specialize in providing detailed information about specific drugs. However, Opana ER was taken off the market in September 2017.

According to the Opana label “Because of the risks of addiction, abuse, and misuse with opioids, even at recommended doses, reserve OPANA for use in patients for whom alternative treatment options [e.g., non-opioid analgesics or opioid combination products]:

  • Have not been tolerated, or are not expected to be tolerated,
  • Have not provided adequate analgesia, or are not expected to provide adequate analgesia”

The label’s black box warnings make it clear that this drug should only be taken with great care:

WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME; INTERACTION WITH ALCOHOL; AND RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS

Addiction, Abuse, and Misuse

OPANA exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death.  Assess each patient’s risk prior to prescribing OPANA, and monitor all patients regularly for the development of these behaviors and conditions.

Life-threatening Respiratory Depression

Serious, life-threatening, or fatal respiratory depression may occur with use of OPANA.  Monitor for respiratory depression, especially during initiation of OPANA or following a dose increase.

Accidental Ingestion

Accidental ingestion of even one dose of OPANA, especially by children, can result in a fatal overdose of oxymorphone.

Neonatal Opioid Withdrawal Syndrome

Prolonged use of OPANA during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts. If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available.

Interaction with Alcohol

Instruct patients not to consume alcoholic beverages or use prescription or non-prescription products that contain alcohol while taking OPANA. The co-ingestion of alcohol with OPANA may result in increased plasma levels and a potentially fatal overdose of oxymorphone.

Risks From Concomitant Use With Benzodiazepines Or Other CNS Depressants

Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death.

Reserve concomitant prescribing of OPANA and benzodiazepines or other CNS depressants for use in patients for whom alternative treatment options are inadequate.

  • Limit dosages and durations to the minimum required.
  • Follow patients for signs and symptoms of respiratory depression and sedation 

ABUSE

Opana is a Schedule II drug, which means it has “a high potential for abuse which may lead to severe psychological or physical dependence.”

It is twice as potent as other opioids.

Opana has a long history of dependence and abuse. Its original extended release formula (Opana ER) could be crushed and snorted (inhaled through the nose) so the drug would have greater, and immediate, impact. When the manufacturer (ENDO) tried to resolve this problem with a new abuse-resistant version, the abuse-resistant formulation did prevent crushing and snorting, but people who were abusing the drug quickly found that the new pills could basically be melted down and injected. The person injecting it got a 12-hour dose all at one time, made even stronger by direct injection into the veins – which increased the potential of dangerous side effects, dependence, addiction, and overdose. Opana injection was also associated with people sharing needles and was accused of causing an HIV epidemic in some areas of the U.S.

The FDA asked that the drug be taken off the market, which it was in September 2017.

The Opana immediate release is still available, but there is no longer an extended release version.

ADDiCTION / DEPENDENCE

Opana is twice as potent as other opioids. The risk of dependence, addiction, abuse, and misuse with Opana – even at recommended doses – is high enough to warrant a Schedule II DEA classification, meaning that it has “a high potential for abuse which may lead to severe psychological or physical dependence.”

According to the Opana label, Opana should be reserved for use with patients for whom all other treatment options [e.g., non-opioid analgesics or opioid combination products] have not been tolerated, or are not expected to be tolerated, have not provided adequate analgesia, or are not expected to provide adequate analgesia. Also, Opana should be used at the lowest possible dose for the shortest period of time. 

HALF LIFE AND METABOLISM

The biological half-life of a substance is the time it takes for a drug to lose half of its pharmacologic activity. This is significant because it affects how soon withdrawal symptoms may appear.

Opana half-life ranges from approximately 9-11 hours after a single oral dose (5-40 mg).

Opana is highly metabolized, principally in the liver, and undergoes reduction or conjugation with glucuronic acid to form both active and inactive products.  The two major metabolites of oxymorphone are oxymorphone-3-glucuronide and 6-OH-oxymorphone.

Although oxymorphone itself does not undergo CYP-mediated metabolism, a portion of the oxycodone dose is metabolized to oxymorphone by CYP2D6.

The CYP enzymes are the major enzymes involved in drug metabolism, and since many drugs may increase or decrease the activity of various CYP isozymes, this is a major source of adverse drug interactions, since changes in CYP enzyme activity may affect the metabolism and clearance of various drugs. For example, if one drug inhibits the CYP-mediated metabolism of another drug, the second drug may accumulate within the body to toxic levels, possibly causing an overdose.

OPIOID INDUCED HYPERALGESIA

There is increasing medical research showing that taking opioids like Opana for longer than six months will create a condition called Opioid Induced Hyperalgesia. This is a condition where the opioids actually make the pain receptors more sensitive and, therefore, the pain greater. A person with this condition is required to take more and more of the opioid to try to address the pain but finds that the pain actually increases.

As the person takes more of the drug – not aware that the drug is now actually causing the pain – their risk for dependence, side effects, and overdose increases.

 

SIDE EFFECTS

Side effects from Opana can be mild or severe. You should seek emergency medical attention immediately if any are severe, especially if you experience slow or shallow breathing, fainting, seizures, severe drowsiness, difficulty waking up, or signs of an allergic reaction such as rashes, itching and swelling, severe dizziness, and trouble breathing.

Other side effects include:

  • abdominal distention
  • adrenal insufficiency
  • agitation
  • allergic reactions
  • amnesia
  • anaphylaxis – an acute allergic reaction that prompts the immune system to respond. The symptoms can include fainting, lightheadedness, low blood pressure, dizziness, or flushing, difficulty breathing, rapid breathing, shortness of breath, or wheezing, hives, swelling under the skin, blue skin from poor circulation, or rashes, nausea or vomiting, fast heart rate, feeling of impending doom, itching, tongue swelling, difficulty swallowing, facial swelling, mental confusion, nasal congestion, or impaired voice.
  • androgen deficiency – lower levels of male sex hormones, particularly testosterone, than is needed for health
  • angioedema – swelling of the lower layer of skin and tissue just under the skin or mucous membranes. The swelling may occur in the face, tongue, larynx, abdomen, or arms and legs.
  • anxiety
  • appetite decreased
  • bradycardia – abnormally slow heart action
  • central nervous system depression
  • clamminess
  • confusion
  • constipation
  • convulsion
  • dehydration
  • depressed level of consciousness
  • depression
  • dermatitis
  • diarrhea
  • difficult micturition – the discharge of urine from the bladder
  • difficulty swallowing
  • difficulty urinating
  • disorientation
  • dizziness
  • drowsiness
  • dry mouth
  • dyspepsia – indigestion
  • dysphoria – a state of unease or generalized dissatisfaction with life
  • dyspnea – difficult or labored breathing
  • edema
  • euphoric mood
  • fatigue
  • feeling jittery
  • flatulence
  • flushing
  • hallucinations
  • headache
  • heartbeat too fast or slow
  • hot flashes
  • hypersensitivity
  • hypotension
  • hypoxia – the deprivation of oxygen to the brain
  • ileus – a painful obstruction of the ileum or other part of the intestine
  • insomnia
  • interactions with benzodiazepines and other central nervous system (CNS) depressants
  • lethargy
  • life-threatening respiratory depression
  • lightheadedness
  • loss of appetite
  • memory impairment
  • mental impairment
  • mental status changes
  • mild itching
  • miosis – excessive constriction of the pupil of the eye.
  • mood changes
  • nausea
  • Neonatal Opioid Withdrawal Syndrome – the potentially life-threatening reaction in a newborn whose mother has been taking opioids during pregnancy.
  • nervousness
  • oxygen saturation decreased
  • palpitation
  • postural hypotension – A drop in blood pressure (hypotension) due to a change in body position (posture) when a person moves to a more vertical position: from sitting to standing or from lying down to sitting or standing.
  • pruritus – severe itching of the skin
  • pyrexia – fever
  • respiratory depression
  • respiratory distress
  • respiratory rate decreased
  • restlessness
  • sedation
  • seizures
  • serotonin syndrome – serotonin syndrome is a group of side effects that include high body temperature, agitation, increased reflexes, tremor, sweating, dilated pupils, and diarrhea, associated with serotonergic drugs. Serotonergic drugs are used to treat migraine, depression and other mood disorders.
  • severe hypotension
  • somnolence
  • stomach or abdominal pain
  • sweating increased
  • syncope –
    temporary loss of consciousness caused by a fall in blood pressure.
  • tachycardia-abnormally rapid heart rate
  • unusual tiredness
  • urinary retention
  • urticaria – a rash of round, red welts on the skin that itch intensely, sometimes with dangerous swelling, caused by an allergic reaction, typically to specific foods.
  • vision blurred
  • visual disturbances
  • vomiting
  • weakness
  • weight loss

 

WITHDRAWAL SYMPTOMS

The symptoms of Opana withdrawal may be relatively mild or severe, depending on how long you’ve been taking the drug, at what dosage, and how you personally react to the drug and to coming off it. Even when taken for a short period of time – a week or two – a doctor should always be consulted about the proper way to stop taking Opana. If someone is dependent on the drug (or addicted to it) withdrawal will be more difficult. Many people are so uncomfortable trying to quit Opana they start back on it before they’ve gotten through withdrawal. Here are some of the withdrawal symptoms:

  • abdominal cramps
  • anorexia
  • anxiety
  • backache
  • breathing hard
  • chills
  • diarrhea
  • increased blood pressure
  • increased heart rate
  • increased respiratory rate
  • insomnia
  • irregular heart beat
  • irritability
  • joint pain
  • lacrimation – tearing up
  • myalgia – muscle pain
  • nausea
  • perspiration
  • pupil dilation
  • restlessness
  • rhinorrhea – runny nose
  • vomiting
  • weakness
  • yawning

TREATMENT

Quitting Opana on your own can be dangerous as well as uncomfortable and painful. It  should not be done without medical supervision. Not only is it dangerous to attempt withdrawal without medical advice, it is estimated that over 95% of the people who attempt to withdraw from opioids or opiates on their own will not succeed because of the pain of the withdrawal. A medical detoxification can help a person stop taking Opana by making withdrawal safe and more comfortable. Call us to talk to a Detox Advisor.