Apokyn - General Information
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Apokyn has widespread effects in the central nervous system and on smooth muscle.
Pharmacology of Apokyn
Apokyn is a narcotic pain management agent indicated for the relief of pain in patients who require opioid analgesics for more than a few days. Apokyn 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. In clinical settings, morphine exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Apokyn appears to increase the patient's tolerance for pain and to decrease discomfort, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Opioids also produce respiratory depression by direct action on brain stem respiratory centers.
Apokyn for patients
If clinically advisable, patients receiving ORAMORPH SR brand of morphine sulfate sustained release tablets, should be given the following instructions by the physician:
- Morphine may produce psychological and/or physical dependence. For this reason, the dose of the drug should not be increased without consulting a physician.
- Morphine may impair mental and/or physical ability required for the performance of potentially hazardous tasks (e.g., driving, operating machinery).
- Morphine should not be taken with alcohol or other CNS de-pressants (sleep aids, tranquilizers) because additive effects, including CNS depression, may occur. A physician should be consulted if other prescription and/or over-the-counter medications are currently being used or are prescribed for future use.
- For women of childbearing potential, who become or are planning to become pregnant, a physician should be consulted regarding analgesics and other drug use.
Storage: ORAMORPH SR Tablets should be stored in unopened containers at or below room temperature.
Caution: Federal law prohibits dispensing without prescription. Federal law prohibits the transfer of this drug to any person other than the patient for whom it was prescribed.
Safety and Handling Instructions: ORAMORPH SR is supplied as tablets that pose little risk of direct exposure to health care personnel and should be handled and disposed of in accordance with hospital policy. Patients and their families should be instructed to dispose of ORAMORPH SR tablets, that are no longer needed, down the toilet.
Use with Other Central Nervous System Depressants: The depressant effects of morphine are potentiated by the presence of other CNS depressants such as alcohol, sedatives, antihistaminics, or psychotropic drugs. Use of neuroleptics in conjunction with oral morphine may increase the risk of respiratory depression, hypotension and profound sedation or coma.
Interaction with Mixed Agonist/Antagonist Opioid Analgesics: Agonist/antagonist analgesics (i.e., pentazocine, nalbuphine, butorphanol, or buprenorphine) should NOT be administered to patients who have received or are receiving a course of therapy with a proof opioid agonist analgesic. In these patients, the mixed agonist/antagonist may alter the analgesic effect or may precipitate withdrawal symptoms.
ORAMORPH SR is contraindicated in patients with respiratory depression in the absence of resuscitative equipment, in patients with acute or severe bronchial asthma and in patients with known hypersensitivity to morphine.
ORAMORPH SR is contraindicated in any patient who has or is suspected of having a paralytic ileus.
Additional information about Apokyn
Apokyn Indication: For the relief and treatment of severe pain.
Mechanism Of Action: The precise mechanism of the analgesic action of morphine is unknown. However, specific CNS opiate receptors have been identified and likely play a role in the expression of analgesic effects. 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.
Drug Interactions: Cimetidine Cimetidine increases the effect of the narcotic
Naltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals
Rifampin Rifampin decreases the effect of morphine/codeine
Trovafloxacin IV morphine decreases the absorption of trovafloxacin
Food Interactions: Avoid alcohol.
Take with food.
To avoid constipation: increase your daily intake of fiber (beans, whole grains, vegetables).
Generic Name: Morphine
Synonyms: (-)-Heroin hydrochloride; (-)-Morphine; D-(-)-Morphine; Diacetylmorphine hydrochloride; Diamorphine hydrochloride; Heroin hydrochloride; Heroine hydrochloride; Morphine Sulfate; Morphinum; O,O'-Diacetylmorphine hydrochloride; Morphin; Morphina
Drug Category: Narcotics; Analgesics; Opiate Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Morphine: Apokyn; Astramorph PF; Avinza; Depodur; Dulcontin; Duramorph PF; Duromorph; Epimorph; Kadian; M-Eslon; M.O.S; MS/L; MS/S; MSIR; Meconium; Morfina; Morphia; Morphine Extra-Forte; Morphine Forte; Morphine H.P; Morphinism; Morphitec; Morphium; Moscontin; Ms Contin; Nepenthe; OMS Concentrate; Oramorph SR; Ospalivina; RMS Uniserts; Rescudose; Roxanol; Roxanol 100; Roxanol UD; Statex; Statex Drops; l-Morphine;
Absorption: Bioavailability is approximately 30%.
Toxicity (Overdose): LD50 = 461 mg/kg (rat, oral), 600 mg/kg (mouse, oral). Human lethal dose by ingestion is 120-250 mg of morphine sulfate. Symptoms of overdose include cold, clammy skin, flaccid muscles, fluid in the lungs, lowered blood pressure, "pinpoint" or dilated pupils, sleepiness leading to stupor and coma, slowed breathing, and slow pulse rate.
Protein Binding: 30-40%
Biotransformation: Primarily hepatic (90%), converted to dihydromorphinone and normorphine. Also converted to morphine-3-glucuronide (M3G) and morphine-6-glucuronide. Virtually all morphine is converted to glucuronide metabolites; only a small fraction (less than 5%) of absorbed morphine is demethylated.
Half Life: 2-4 hours
Dosage Forms of Apokyn: Solution Intravenous
Tablet, extended release Oral
Capsule, extended release Oral
Solution / drops Oral
Chemical IUPAC Name: (5α,6α)-Didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol
Chemical Formula: C17H19NO3
Morphine on Wikipedia: http://en.wikipedia.org/wiki/Morphine
Organisms Affected: Humans and other mammals