Numorphan
Numorphan - General Information
An opioid analgesic with actions and uses similar to those of morphine, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)
Pharmacology of Numorphan
Numorphan 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.
Numorphan for patients
Numorphan Interactions
The concomitant use of other CNS depressants including sedatives, hypnotics, tranquilizers, general anesthetics, phenothiazines, other opioids, tricyclic antidepressants, monoamine oxidase (MAO) inhibitors, and alcohol may produce additive CNS depressant effects. When such combined therapy is contemplated, the dose of one or both agents should be reduced.
Anticholinergics or other medications with anticholinergic activity when used concurrently with opioid analgesics may result in increased risk of urinary retention and/or severe constipation, which may lead to paralytic ileus.
It has been reported that the incidence of bradycardia was increased when oxymorphone was combined with propofol for induction of anesthesia.
In addition, CNS toxicity has been reported (confusion, disorientation, respiratory depression, apnea, seizures) following coadministration of cimetidine with opioid analgesics; no clear-cut cause and effect relationship was established.
Numorphan Contraindications
NUMORPHAN should not be administered to patients who are hypersensitive to oxymorphone hydrochloride or to any of the other ingredients in NUMORPHAN, or hypersensitive to morphine analogs.
NUMORPHAN should not be administered to individuals during an acute asthmatic attack or to patients with severe respiratory depression, upper airway obstruction, or any patient who has or is suspected of having a paralytic ileus. NUMORPHAN should not be used in the treatment of pulmonary edema secondary to a chemical respiratory irritant. Opioid analgesics cause pooling of blood in the extremities by decreasing peripheral vascular resistance. This effect results in decreases in venous return, cardiac work, and pulmonary venous pressure, and blood is shifted from the central to peripheral circulation which would not be beneficial in the treatment of pulmonary edema secondary to a chemical respiratory irritant.
Additional information about Numorphan
Numorphan Indication: For the treatment of moderate-to-severe pain
Mechanism Of Action: Numorphan 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Oxymorphone
Synonyms: Dihydrohydroxymorphinone; Dihydroxymorphinone; Oxymorphine; 14-Hydroxydihydromorphinone; Oximorphonum
Drug Category: Narcotics; Adjuvants; Analgesics; Opiate Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Oxymorphone: Numorphan; Opana;
Absorption: Not Available
Toxicity (Overdose): Oxymorphone 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. In a severe case of overdose, apnea, circulatory collapse, cardiac arrest, and death may occur. Intravenous mouse LD50 is 172 mg/kg.
Protein Binding: Not Available
Biotransformation: Oxymorphone undergoes extensive hepatic metabolism in humans. After a 10 mg oral dose, 49% was excreted over a five-day period in the urine. Of this, 82% was excreted in the first 24 hours after administration. The recovered drug-related products contained the oxymorphone (1.9%), the conjugate of oxymorphone (44.1%), the 6(beta)-carbinol produced by 6-keto reduction of oxymorphone (0.3%), and the conjugates of 6(beta)-carbinol (2.6%) and 6(alpha)-carbinol (0.1%).
Half Life: 1.3 (+/-0.7) hours
Dosage Forms of Numorphan: Suppository Rectal
Chemical IUPAC Name: Not Available
Chemical Formula: C17H19NO4
Oxymorphone on Wikipedia: https://en.wikipedia.org/wiki/Oxymorphone
Organisms Affected: Humans and other mammals
