Oxyphone

Oxyphone Uses, Dosage, Side Effects, Food Interaction and all others data.

Oxyphone is a full opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of oxymorphone is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with oxymorphone. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.

The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.

Oxyphone is a semi-synthetic opioid substitute for morphine. It is a potent analgesic. Opioid analgesics exert their principal pharmacologic effects on the CNS and the gastrointestinal tract. The principal actions of therapeutic value are analgesia and sedation. Opioids produce respiratory depression by direct action on brain stem respiratory centers. The mechanism of respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to increases in carbon dioxide tension and to electrical stimulation.

Trade Name Oxyphone
Availability Prescription only
Generic Oxymorphone
Oxymorphone Other Names Dihydrohydroxymorphinone, Dihydroxymorphinone, Oximorfona, Oximorphonum, Oxymorphone, Oxymorphonum
Related Drugs Buprenex, aspirin, acetaminophen, tramadol, naproxen, Tylenol, oxycodone, butorphanol, ropivacaine, Stadol
Weight 10mg, 1 mg/ml
Type Tablet, Injection
Formula C17H19NO4
Weight Average: 301.3371
Monoisotopic: 301.131408101
Groups Approved, Investigational, Vet approved
Therapeutic Class Opioid analgesics
Manufacturer Incepta Pharmaceuticals Limited
Available Country Bangladesh
Last Updated: September 19, 2023 at 7:00 am
Oxyphone
Oxyphone

Uses

Tablet is used for treatment of moderate to severe pain like chronic cancer, arthritis, postoperative & low back pain.

Injection is used for the relief of moderate to severe pain. It is also used for pre-operative & post-operative medication for support of anesthesia, for obstetrical analgesia and for relief of anxiety in patients with dyspnea associated with pulmonary edema secondary to acute left ventricular dysfunction.

Oxyphone is also used to associated treatment for these conditions: Anxiety, Severe Pain, Moderate Pain, Perioperative analgesia, Obstetrical analgesia therapy

How Oxyphone works

Oxyphone interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the 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 binds to and inhibits GABA inhibitory interneurons via mu-receptors. These interneurons normally inhibit the descending pain inhibition pathway. So, without the inhibitory signals, pain modulation can proceed downstream.

Dosage

Oxyphone dosage

Oxyphone Tablet: This may be used as needed in the treatment of acute post-surgical pain with a dose of 5-10 mg every 4 hours. Administer Oxyphone Tablet on an empty stomach at least one hour prior to or two hours after eating.

Oxyphone Injection:

  • Subcutaneous or Intramuscular Administration: Initially 1 mg to 1.5 mg, repeated every 4 to 6 hours as needed.
  • Intravenous: 0.5 mg initially. For analgesia during labor 0.5 mg to 1 mg intramuscularly is recommended.

Conversion from Oral Oxyphone to Oxyphone Injection: Given the absolute oral bioavailability of approximately 10%, patients receiving oral Oxyphone may be converted to Oxyphone Hydrochloride injection by administering one-tenth the patient's total daily oral Oxyphone dose as Oxyphone Hydrochloride injectable in four or six equally divided doses (e.g., total daily oral dose/ [10X4]). For example, approximately 1 mg of Oxyphone Hydrochloride injectable IM every 6 hours (4 mg total IM dose) may be required to provide pain relief equivalent to a total daily dose of 40 mg oral Oxyphone. As with any opioid drug product, it is necessary to adjust the dosing regimen for each patient individually taking into account the patient's prior analgesic treatment experience.

Side Effects

General Disorders: Respiratory depression, Fatigue, Asthenia.

Metabolism and Nutrition Disorders: Anorexia.

Cardiac Disorders: Tachycardia, Bradycardia, Palpitations.

Eye Disorders: Miosis, Diplopia, Blurred vision.

Gastrointestinal Disorders: Vomiting, Constipation.

Psychiatric Disorders: Dysphoria, Euphoric mood, Nervousness, Restlessness, Insomnia, Agitation, Hallucination, Depression.

Vascular Disorders: Hypotension & Flushing.

Toxicity

Oxyphone overdosage is characterized by respiratory depression, extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, and sometimes bradycardia and hypotension. Patients experiencing an overdose may develop apnea, circulatory collapse, and cardiac arrest. Intravenous mouse LD50 is 172 mg/kg.

Precaution

Do not stop abruptly; taper gradually to stop treatment. Use caution in patients with acute pancreatitis, Addison disease, benign prostatic hyperplasia, cardiac arrhythmias, central nervous system (CNS) depression, drug abuse or dependence, emotional lability, gallbladder disease, gastrointestinal (Gl) disorder, pseudomembranous colitis, Gl surgery, head injury, hypothyroidism or untreated myxedema, intracranial hypertension, brain tumor, toxic psychosis, urethral stricture, urinary tract surgery, seizures, acute alcoholism, delirium tremens, shock, cor pulmonale, chronic pulmonary disease, emphysema, kyphoscoliosis, severe obesity, renal or hepatic impairment, elderly or debilitated patients.

Avoid alcohol. Reduce dosage if drug is coadministered with other CNS depressants. Thrombocytopenia purpura resulting in kidney failure or death has been reported when extended-release tablets are dissolved and injected IV. May obscure diagnosis of abdominal conditions.

Risk of opioid addiction, abuse, and misuse, which can lead to overdose and death Assess each patient's risk prior to prescribing and monitor all patients regularly for the development of these behaviors or conditions Life-threatening respiratory depression, life-threatening, or fatal respiratory depression may occur

Monitor for respiratory depression, especially during initiation or following a dose increase

Interaction

Clinical drug interaction studies with Oxyphone showed no induction of CYP450 3A4 or 2C9 enzyme activity indicating that no dose adjustment for CYP 3A4 or 2C9 mediated drug-drug interactions is required.

Food Interaction

  • Avoid alcohol. Ingesting alcohol has unpredictable effects on the pharmacokinetics of oxymorphone. Alcohol may also potentiate the CNS depressant effects of oxymorphone.
  • Take on an empty stomach. Take oxymorphone at least one hour before or two hours after eating as food may increase the absorption of oxymorphone.

Oxyphone Alcohol interaction

[Moderate] GENERALLY AVOID:

Ethanol may potentiate the central nervous system (CNS) depressant effects of opioid analgesics.

Concomitant use may result in additive CNS depression and impairment of judgment, thinking, and psychomotor skills.

In more severe cases, hypotension, respiratory depression, profound sedation, coma, or even death may occur.

Concomitant use of opioid analgesics with ethanol should be avoided.

Half Life

1.3 (+/-0.7) hours

Elimination Route

Oxyphone is highly metabolized, principally in the liver, and undergoes reduction or conjugation with glucuronic acid to form both active and inactive products. Because oxymorphone is extensively metabolized, <1% of the administered dose is excreted unchanged in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category C. The safety of using Oxyphone in pregnancy has not been established with regard to possible adverse effects on fetal development. The use of Oxyphone in pregnancy, in nursing mothers, or in women of child-bearing potential requires that the possible benefits of the drug be weighed against the possible hazards to the mother and the child.

Contraindication

  • Significant respiratory depression
  • Acute or severe bronchial asthma or hypercarbia
  • Known or suspected paralytic ileus
  • Moderate and severe hepatic impairment
  • Hypersensitivity (e.g. anaphylaxis) to oxymorphone

Special Warning

Pediatric use: Safety and effectiveness of Oxyphone Hydrochloride tablet and injection in pediatric patients below the age of 18 years have not been established.

Geriatric use: Oxyphone Hydrochloride tablet and injection should be used with caution in elderly patients. These adverse events included dizziness, somnolence, confusion and nausea.

Acute Overdose

Signs and Symptoms: Acute overdosage with Oxyphone is characterized by respiratory depression, extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils and sometimes bradycardia and hypotension.

Treatment: In the treatment of Oxyphone overdosage, primary attention should be given to the re-establishment of a patient airway and institution of assisted or controlled ventilation. Supportive measures (including oxygen and vasopressors) should be employed in the management of circulatory shock and pulmonary edema accompanying overdose as indicated. The opioid antagonist naloxone hydrochloride is a specific antidote against respiratory depression that may result from overdosage or unusual sensitivity to opioids including Oxyphone

Storage Condition

Tablet: Store in a cool and dry place, protect from light.

Injection: Store at 25°C, protect from light.

Innovators Monograph

You find simplified version here Oxyphone

Oxyphone contains Oxymorphone see full prescribing information from innovator Oxyphone Monograph, Oxyphone MSDS, Oxyphone FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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