Opana vs Oxycodone

This article features an Opana (oxymorphone hydrochloride, numorphan, numorphone) vs Oxycodone (oxycontin) comparison. The strength, withdrawal effects and overall effects of both drugs in treatment of pain, muscle craps, etc. are compared.

Are you finding it increasingly impossible to walk to the bathroom at night without stifling a yell of pain due to your muscle cramps?

Chronic pain can be extremely depressing and can cause both physical and mental agony.

Luckily, there is a wide array of medications available to counter chronic pain that bothers you twenty four hours a day. A class of drugs popular for treating chronic pain is opioid group of analgesics.

Opioids

Opioids are drugs that have an action on brain similar to that of opiates such as morphine and codeine (1). These are synthetic, commercially produced medications. They are not derived from naturally occurring opium.

Their uses as an analgesic or pain killer are:

Acute pain

Opioids are efficient in treatment of acute pain for example post operative pain. They have also been found to be imperative in analgesic care to help with the severe, chronic, disabling pain that may occur in some terminal conditions such as cancer, and degenerative medical conditions such as rheumatoid arthritis. In many cases opioids are a successful long-term therapy strategy for those with chronic cancer pain. They significantly improve life quality of patient (2).

Chronic non cancer pain

Studies have shown that the adverse effects of opioids are likely greater than their benefits when used for most non-cancer chronic conditions including headaches, back pain and fibromyalgia. Thus they should be used cautiously in chronic non-cancer pain.

Opioids are contraindicated as a first-line treatment for headache because they disturb alertness, bring risk of addiction, and increase the prospect that episodic headaches will become a regular episode. Opioids also can cause increased sensitivity to headache pain (hyperalgesia). When other treatments fail or are unavailable, opioids may be suitable for treating headache if the patient can be scrutinized to prevent the development of chronic headache (3).

Opana

Opana is a semi- synthetic opioid painkiller and commercially available hydrochloride salt of drug oxymorphone.

Composition

Opana consists of the following main substances:

• Oxymorphone hydrochloride
• Lactose monohydrate
• Magnesium stearate
• Pregelatinized starch

Active ingredient

The active ingredient of Opana is oxymorphone. The drug was developed in Germany.

Uses

Opana is used to treat moderate to severe pain. It is usually prescribed to those patients who need pain relief around the clock for a long duration of time.

Oxymorphone is indicated for the relief of moderate to severe pain when other analgesics prove ineffective and also as a medication to decrease apprehension, maintain anesthesia and as an obstetric analgesic before surgical procedures.  It can be used for the treatment of pain in patients with dyspnea associated with acute left ventricular failure and pulmonary edema (4).

Opana extended-release tablets are indicated for the management of long term pain and are indicated only for patients already on a regular schedule of strong opioids for a prolonged period.

The immediate-release Opana tablets are prescribed for management of breakthrough pain for patients on the extended-release version. Oxymorphone is considered, with buprenorphine, oxycodone, dihydrocodeine, morphine and other opioids as a means of extenuating refractory depression (5).

It is a major depressive disorder that does not respond adequately to regular anti depressants.

Mechanism of action

Oxymorphone interacts majorly with the opioid mu-receptor. Opioid receptors are found extensively in brain, spinal cord and digestive tract. These mu-binding sites are unconnectedly distributed in the human brain, with more density in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and some cortical areas.

They are also found on terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. Also, it has been shown that oxymorphone attaches to and inhibits action of  GABA inhibitory interneurons via mu-receptors.

These interneurons generally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can move downstream (6).

It acts to a lesser degree upon delta opiod receptors. Action of oxymorphone is ten times more potent than that of morphine.

Physical and chemical properties

Opana is commercially produced from thebaine, which is found in small amount in opium poppy and in large amounts in oriental poppy (7).

Oxymorphone hydrochloride or opana is an odorless white to off white crystalline powder. It becomes dark in color upon exposure to light.

Adverse effects

Side effects of Opana are as follows (8):

General

Common side effects of opana are:

• Difficulty having a bowel movement.
• Increased sweating.
• Nausea or vomiting.
• Sleepiness and drowsiness.
• Acid or sour stomach.
• Belching.

Gastrointestinal

Gastrointestinal side effects of Opana include:

• Constipation.
• Nausea.
• Vomiting.
• Dry mouth.
• Abdominal distention.
• Flatulence.
• Abdominal pain.
• Diarrhea.
• Dyspepsia.

Respiratory

Respiratory side effects of Opana include:

• Hypoxia.
• Dyspnea.
• Atelactasis.
• Bronchospasm.
• Laryngospasm.
• Apnea.

Nervous system

Side effects of Opana on nervous system include:

• Somnolence.
• Dizziness.
• Headache.
• Confusion.
• Amnesia.
• Convulsion.
• Memory impairment.

Cardiovascular

Cardiovascular adverse effects of Opana are as follows:

• Tachycardia.
• Hypotension.
• Edema.
• Hypertension.
• Syncope.
• Orthostatic hypotension.

Psychiatric

Psychiatric side effects of Opana include:

• Anxiety.
• Insomnia.
• Confusion.
• Disorientation.
• Restlessness.
• Nervousness.
• Sudden euphoric mood.
• Hallucination.

Genitourinary

Genitourinary adverse effects of Opana are as follows:

• Urinary hesitation or bladder shyness.
• Urinary retention.
• Oliguria

Dermatological

Dermatological adverse effects of Opana are very common and include:

• Pruritus.
• Increased sweating.

Metabolic

Metabolic side effects of Opana include:

• Decreased appetite.
• Dehydration.
• Anorexia.
• Loss in weight.

Ocular

Adverse effects of Opana on sight and vision are as follows:

• Blurry vision.
• Miosis.
• Diplopia.

Interactions of Opana

Use with CNS Depressants

The simultaneous use of other CNS depressants such as sedatives, hypnotics, tranquilizers, general anesthetics, phenothiazines, other opioids, and alcohol along with opana may produce additive CNS depressant effects.

Opana (oxymorphone hydrochloride), like all opioid analgesics, should be started at ⅓ to ½ of the usual dose in patients who are concomitantly getting treatment with other central nervous system depressants because respiratory depression, hypotension, and intense sedation, coma and death may result and used in small doses as necessary for adequate pain relief.

When joint therapy with any of the above medications is considered, the dose of one or both agents should be decreased to avoid drug interaction.

Interactions with Mixed Agonist/Antagonist Opioid Analgesics

Agonist/antagonist painkillers such as pentazocine, nalbuphine, butorphanol, and buprenorphine should be given carefully to a patient who has received or is receiving a course of treatment with a pure opioid agonist pain reliever such as oxymorphone.

In this situation, mixed antagonist analgesics may decrease the analgesic effect of oxymorphone and may cause. withdrawal symptoms in these patients.

Cimetidine

Cimetidine is a histamine H2-receptor antagonist used to treat ulcers and heartburn.

Central nervous system side effects have been observed such as confusion, disorientation, respiratory depression, seizures and apnea following co administration of cimetidine with opioid analgesics especially Opana.

Anticholinergics

These drugs block activity of acetylcholine and are used to treat asthma, gastrointestinal problems and muscular spasms. Anticholinergics or other medications with anticholinergic activity when used together with opioid pain killers such as opana may result in increased risk of urinary retention and severe constipation, which may lead to paralytic ileus.

MAO inhibitors

Opana (oxymorphone hydrochloride) is not advisable for use in patients who have received MAO inhibitor therapy within 14 days, because severe and unpredictable potentiation by MAO inhibitors has been reported with opioid medication.

No specific interaction between oxymorphone and monoamine oxidase inhibitors has been established, but caution must be exercised while use of any opioid in patients taking this class of drugs.

Opana addiction and abuse

Controlled substance

Opana contains drug oxymorphone, a mu opioid agonist and a Schedule II controlled substance with an abuse capacity akin to that of morphine and other opioids (9). Oxymorphone can be abused and addicts may indulge in criminal activities.

Abuse

All patients undergoing therapy with opioids require careful monitoring for signs of abuse and addiction, since opioid analgesic products carries the risk of addiction even under appropriate medical observance and use.

Addiction is a prime, persistent, neurobiological malady, with genetic, psychosocial, and environmental factors affecting its development and manifestations.

Addiction to Opana has the following symptoms and signs:

• Impaired control over drug use
• Compulsive use
• Use for non-medical purposes or recreational use
• Continued use despite harm.

Drug addiction can be treated and is reversible, using a multidisciplinary approach, but relapse is common after rehab.

Drug seeking behavior

Drug-seeking behavior is very common among addicts and drug abusers.

Drug-seeking tricks and tactics include sudden emergency calls or visits near the end of office hours, refusal to undergo complete examination, testing or referral, claims of loss of prescriptions, tampering with prescriptions, and reluctance to provide previous medical records or contact information of family or other doctors.

“Doctor shopping” or visiting multiple prescribers to get extra prescriptions is prevalent  among drug abusers and people suffering from untreated addiction.

Abuse and addiction are separate and distinct from physical dependence and tolerance.

Opana like other opioids, may be diverted for non-medical use. Careful record-keeping of prescribing information, including quantity, frequency, and renewal requests is strongly advised.

Opana is meant for oral use only. Abuse of this drug poses a risk of overdose and death. This risk is increased with simultaneous abuse of this medicine with alcohol and other substances. Parenteral drug abuse is frequently coupled with transmission of infectious diseases such as hepatitis and HIV.

Appropriate measures to prevent Opana abuse

Necessary measures to ascertain that patient does not develop tendency to abuse opana are:

• Proper assessment of the patient
• Proper prescribing method
• Periodic re-evaluation of therapy
• Proper dispensing and storage are appropriate measures that help to limit abuse of opioid drugs.

Dependence

Opioid analgesics therapy may lead to physical dependence. Physical dependence results in withdrawal symptoms after sudden discontinuation of a drug or upon use of an opioid antagonist or mixed opioid agonist-antagonist agent.

Withdrawal also may be triggered through use of drugs with opioid antagonist activity, e.g., naloxone, nalmefene, or mixed agonist-antagonist analgesics such as pentazocine, butorphanol, buprenorphine, nalbuphine.

Physical dependence may not occur to a clinically profound degree until after many days to weeks of continuous opioid usage.

Tolerance is the need for increasing doses of opioids to maintain a medicinal  effect such as pain relief. The development of physical dependence or tolerance is not unusual during prolonged opioid therapy for chronic pain.

Opana withdrawal

If opana is suddenly discontinued in a physically-dependent patient, an abstinence syndrome may take place. It is characterized by these signs and symptoms:

• Restlessness
• Lacrimation
• Rhinorrhea. It  is a condition where the nasal cavity is filled with abundant amount of mucus fluid. The condition, commonly known as a runny nose, occurs frequently.
• Yawning
• Perspiration
• Chills
• Myalgia or muscle pain.
• Mydriasis.
• Other symptoms also may develop, including: irritability, anxiety, backache, joint pain, weakness, abdominal cramps, insomnia, nausea, anorexia, vomiting, diarrhea,  elevated blood pressure, respiratory rate, or heart rate.

Babies born to mothers physically dependent on opioids will also be physically dependent and may exhibit respiratory disorders and withdrawal symptoms.

Opana use during pregnancy

It has been assigned category C for use during pregnancy. Studies have shown harmful effects on fetus when mother used opana (10, 11).

Precautions to be aware of when taking Opana

In the following circumstances Opana should be used with great caution (12):

Respiratory depression

Respiratory depression is the main risk of Opana therapy. Respiratory depression may occur more frequently in elderly or incapacitated patients as well as in those suffering from conditions accompanied by hypoxia. Even small doses may trigger respiratory depression sometimes.

Administer Opana with great care to patients with conditions such as hypoxia, hypercapnia, asthma, chronic obstructive pulmonary disease, myxedema, kyphoscoliosis, central nervous system depression or coma.

In these patients, even normal therapeutic doses of opana may decrease respiratory capacity while at the same time increasing airway resistance to the point of apnea. Consider other non-opioid analgesics and use this drug only under careful medical supervision at the lowest effective therapeutic dose in such patients.

Use in patients with head injury and increased intracranial pressure

In case of a head injury, intracranial lesions or a pre existing increase in intracranial pressure, the respiratory depressant effects of opana and its capacity to raise cerebrospinal fluid pressure (resulting from vasodilation following CO2 retention) may be strikingly exaggerated. It can also produce effects on papillary response and consciousness, which may cover neurologic signs of further elevation in intracranial pressure in patients with head injuries.

Prescribe or give Opana with great caution in patients who may be especially vulnerable to the intracranial effects of CO2 retention, such as those with symptoms of increased intracranial pressure or impaired consciousness.

Opana may obscure the clinical course of a patient with a head injury and should be used only if clinically prescribed by a doctor.

Patients with hypotension

Opana like all opioid analgesics, may cause severe lowering of blood pressure  in a patient whose ability to maintain normal levels of blood pressure has been compromised by a depleted blood volume, or after simultaneous therapy with drugs such as phenothiazines or other agents that cause hypotension and compromise vasomotor tone.

Give Opana with caution to patients in circulatory shock, since its vasodilator effect may further lower cardiac output.

In case of liver disease

Patients with mild or severe hepatic impairment are advised against using Opana.

Labor and delivery

Opioids cross the placenta and may produce respiratory depression in neonates. Opana is contraindicated for use in women during and immediately before labor, when use of shorter acting analgesics or other analgesic techniques are more appropriate.

Before using oxymorphone

Tell your doctor or pharmacist if you have any medical conditions and your complete medical history, especially if any of the following apply to you:

• If you are pregnant, planning to become pregnant, or are a nursing mother.
• If you are using any herbal preparation, or dietary supplement.
• If you have allergies to certain medicines, food items or other substances
• If you have a history or a patient of chronic obstructive pulmonary disease (COPD) or other lung or breathing problems such as asthma, emphysema, bronchitis, sleep apnea,  kyphoscoliosis, heart problems, low levels of oxygen in the blood (hypoxia), low blood pressure, dehydration, or low blood volume.
• If you have extreme drowsiness, suffered a recent head injury, increased pressure in the brain or a history of seizures.
• If you have liver or kidney disease, thyroid problems, adrenal gland disorder such as Addison disease, stomach pain, stomach or bowel inflammation, gallbladder or pancreas disease, difficulty in urinating, constipation or if you have had recent stomach or bowel surgery.
• If you drink alcohol, have symptoms of alcohol withdrawal or have a record of suicidal thoughts or attempts. Especially if you are a heavy drinker.
• If you or a family member has a history of mood or mental problems (eg, anxiety, depression, hallucinations) or substance abuse history.

Use of Opana

Use Opana strictly according to instructions of your doctor. Check label for complete instructions. It is available for oral use in form of 5 mg or 10 mg tablets. Do not miss a dose. Should not be used while driving and operating heavy machinery due to its adverse effects on nervous system such as confusion. Keep away from children and from any family member with history of drug abuse.

Oxycodone

Oxycodone is an opioid analgesic and narcotic. It is used to relieve moderate to severe ranging pain. It is found in opium and Persian poppy (13).

Uses

Oxycodone is not prescribed for short term use. It is used for chronic pain and for around the clock administration. It has been in use since 1916 for improving quality of life of patients suffering from chronic pain (14).

Mechanism of action

Oxycodone (oxycontin) exerts its analgesic effect by acting on k-opioid receptors. It increases tolerance to pain.  After it binds to the opioid receptor, a G-protein complex is released, which blocks the release of neurotransmitters by the cell by reducing the amount of cAMP produced, closing the calcium channels, and opening the potassium channels (15).

Side effects of oxycodone

Side effects of oxycodone therapy include (16, 17):

General

Most common side effects of oxycodone include:

• Constipation
• Nausea
• Somnolence
• Dizziness
• Vomiting
• Pruritis
• Headache
• Dry mouth
• Sweating
• Pyrexia

Gastrointestinal

Gastrointestinal adverse effects of Oxycodone include:

• Nausea
• Vomiting
• Constipation
• Anorexia
• Abdominal discomfort and pain
• Dyspepsia
• Dysphagia
• Glossitis

Nervous system

Adverse effects of Oxycodone on nervous system include:

• Headache
• Dizziness
• Confusion
• Neuralgia
• Tremor
• Migraine

Respiratory

Respiratory side effects of Oxycodone are as follows:

• Apnea
• Respiratory arrest
• Bronchitis
• Dyspnea
• Pharyngitis

Cardiovascular

Cardiovascular side effects of Oxycodone include:

• Heart failure
• Hemorrhage
• Palpitation
• Tachycardia

Oxycodone interactions

Neuromuscular blocking agents

Oxycodone, as well as other opioid analgesics, may elevate the neuromuscular blocking action of skeletal muscle relaxants and produce an increased degree of respiratory depression.

CNS depressants

Patients receiving narcotic pain killers, general anesthetics, phenothiazines, other tranquilizers, sedative-hypnotics or other CNS depressants including alcohol in tandem with Oxycodone hydrochloride may display an additive central nervous system depression.

Interactive effects resulting in respiratory depression, hypotension, sedation, or coma may result if these drugs are taken in combination with the regular dosage of Oxycodone hydrochloride. When such combined therapy is being considered, the dose of one or both agents should be reduced.

Mixed agonist/antagonist opioid analgesics

Agonist-antagonist analgesics such as pentazocine, nalbuphine, butorphanol and buprenorphine should be administered with extreme care to patients who have received or are receiving a course of therapy with a pure opioid agonist pain killer Oxycodone.

Monoamine oxidase inhibitors (MAOIs)

Monoamine Oxidase Inhibitors have been reported to exaggerate the effects of oxycodone causing anxiety, confusion and significant depression of respiration or coma. Therapy of Oxycodone hydrochloride is not advisable for patients taking MAOIs or within 14 days of stopping such treatment (18).

Precautions related to Oxycodone use

Respiratory depression

Respiratory depression is the foremost threat from all opioid agonist preparations. Respiratory depression occurs mostly in aged patients, usually following large preliminary doses in non-tolerant patients, or when opioids are given in combination with other agents that  bring about respiratory depression.

Oxycodone hydrochloride should be administered with great care in patients with significant chronic obstructive pulmonary disease or cor pulmonale, and in patients having considerably decreased respiratory reserve, hypoxia, hypercapnia, or already present respiratory depression.

In such patients, even usual therapeutic doses of Oxycodone hydrochloride may diminish respiratory drive to the point of apnea. In these patients alternative non-opioid analgesics should be considered, and opioids should be used only under careful medical supervision at the lowest effective dose.

Tolerance and physical dependence

Physical dependence and tolerance are common during chronic opioid therapy. Mention worthy tolerance should not occur in most patients treated with tlowest doses of Oxycodone.

It should be expected, however, that some patients will develop some degree of tolerance and require progressively higher dosages of Oxycodone hydrochloride to keep up pain relief during chronic treatment. The dosage should be assigned keeping in view the patient's individual analgesic response and ability to tolerate side effects.

Drug abuse

Like other opioids, oxycodone is highly addictive and the patient may develop a drug abuse habit. Physician and family members should closely observe patient during therapy for signs of drug abuse.

Pregnancy

As far as pregnancy and Oxycodone use is conerned, Oxycodone has been classified as B pregnancy safety category. This means that it may only be used during pregnancy if potential benefits justify potential risks to the fetus.

Neonates whose mothers have taken Oxycodone chronically may display respiratory depression and withdrawal symptoms, either at birth or sometime after.

It should not be used prior to or during pregnancy as it may prolong labor and reduce strength of uterine contractions.

How to use Oxycodone

Before using oxycodone consult your doctor and brief him completely about your medical record. Do not leave anything out.

You should not use oxycodone if you are allergic to it, or if you have:

• Severe asthma or breathing disorder
• A blockage in your stomach or intestines
• An allergy to any narcotic analgesic such as methadone, morphine, Oxycontin, Darvocet, Percocet, Vicodin, Lortab or narcotic cough medicine that has codeine, hydrocodone, or dihydrocodeine.
• You should not use oxycodone unless you are already using a similar opioid medicine and have tested tolerance to it. Consult your doctor if you are not sure you are opioid-tolerant.
• Oxycodone may be habit forming and addictive. Never share this medicine with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot have access to it. Selling or giving oxycodone to anyone else is against the law.

To make sure oxycodone is safe for you to use, tell your doctor if you have:

• Any type of breathing problem or pulmonary disease.
• History of head injury, brain tumor, or seizures.
• History of substance abuse, over drinking, or mental illness.
• Urination problems.
• Liver or kidney damage.
• Addison's disease or any other adrenal gland disorder.
• Problems with your gallbladder, pancreas, or thyroid function.

Inform your doctor if you are pregnant.

If you use oxycodone while you are pregnant, your baby could become dependent on the drug.

This may cause life-threatening withdrawal symptoms in the baby after birth. Babies born dependent on addictive medicine may need medical treatment for several weeks.

Oxycodone can pass into breast milk and may harm a nursing baby. You should not breast-feed during oxycodone therapy.

Do not give this medicine to a child.

Opana vs Oxycodone - final comparison

Both drugs are potent opiates used as analgesics and are narcotics. Their analgesic action is exerted by acting on different receptors.

Opana (Oxymorphone) is stronger than Oxycodone and this is why it is usually prescribed in smaller doses (Opana is about two times stronger than Oxycodone, e.g. when you take 15 mg of Opana you may get the same effect with 30 mg of Oxycodone). However you should always ask your doctor about the actual regimen and let him or her decide on what is best for you.

Never use any of these drugs in self treatment!

Withdrawal symptoms of both drugs tend to be quite similar. Both are highly addictive and their user is prone to developing drug abuse habit. Both these drugs may cause respiratory distress and hypotension.

In general Oxycodone tends to be a more addictive narcotic than Opana and that is why it is illegal to give any of these drugs to another person.