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When both morphine and nalorphine were given together, intramuscularly, in varying dosages, the resulting effects on the respiration were complex: with 5 mg of morphine, increasing the dose of nalorphine produced greater depression than increasing it with 10 mg morphine. The interaction of the two drugs was regarded as an example of "competitive dualism". The antagonism by nalorphine of the respiratory depression produced by morphine was primarily related to differences in the intrinsic action of each drug, and not simply due to mutually competitive affinities for certain receptor sites.

... Resp depressant actions of nalorphine-type antagonists may add to existing resp depression produced by CNS depressants.

Nalorphine HBR reportedly enhanced depression caused by combination injection of meperidine-levallorphan in pt receiving phenelzine /and other monoamine oxidase inhibitors/ ... /Nalorphine hydrobromide/

/HUMAN EXPOSURE STUDIES/ The effects of nalorphine 5 mg im, a partial opiate antagonist, on circulating levels of PRL, GH, TSH, LH, FSH and cortisol were studied in six healthy men. Nalorphine produced a produced a prompt and sharp increase in serum PRL and a small, delayed rise in serum GH. Serum LH and cortisol decreased after drug administration and no change in serum FSH and TSH was observed.

/HUMAN EXPOSURE STUDIES/ The comparative study of 2 narcotic antagonists, naloxone and nalorphine, was performed in healthy volunteers. The influence of these drugs on the respiratory and cicularoty systems and on the psychical state was compared. The study was carried out in a double-blind, cross-over manner. Increasing doses of naloxone and placebo or nalorphine and placebo, were administered intravenously. Naloxone, even in very high doses, caused no changes in cardivascular system, acid-base balance, sensitivity of respiratory centre to carbon dioxide and psychical state of volunteers. After the administration of nalorphine, even in very small doses, changes in psychical state in all examined subjects were observed. Nalorphine caused /a/ significant change in the ventilatory response to CO2. ...

/HUMAN EXPOSURE STUDIES/ In the control trials on near-term pregnant women before tyhe onset of labor, nalorphine was found to cause a mild respiratory acidosis in the mother and metabolic acidosis in the fetus. ...

/SIGNS AND SYMPTOMS/ Significant percentage experience unpleasant reactions that range from anxiety, "crazy feelings," and vivid, disturbing, "unreal" daydreams to frank hallucinations.

For more Human Toxicity Excerpts (Complete) data for NALORPHINE (8 total), please visit the HSDB record page.

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/

/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/

LD50 Rat sc 474 mg/kg

LD50 Rat iv 226 mg/kg

LD50 Mouse oral 1140 mg/kg

LD50 Mouse ip 492 mg/kg

For more Non-Human Toxicity Values (Complete) data for NALORPHINE (7 total), please visit the HSDB record page.

Nalorphine hydrochloride injection. ... Indications for use. Respiratory and circulatory depression in dogs resulting from overdosage of, or unusual sensitivity to, morphine and certain other narcotics. Not for depression due to any other cause. ... Limitations: Successive doses of the drug gradually lose their analeptic effect and eventually induce respiratory depression equal to that of opiates. Therefore, do not exceed therapeutic dosage. Do not mix drug with meperidine solutions because the buffer will cause precipitation. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

The Generic Animal Drug and Patent Restoration act requires that each sponsor of an approved animal drug must submit to the FDA certain information regarding patents held for the animal drug or its method of use. The Act requires that this information, as well as a list of all animal drug products approved for safety and effectiveness, be made available to the public. Nalorphine hydrochloride is included on this list. /Nalorphine hydrochloride/

Schedule III shall consist of the drugs and other substances, by whatever official name, common or usual name, chemical name, or brand name designated, listed in this section. Each drug or substance has been assigned the DEA Controlled Substances Code Number set forth opposite it. Nalorphine (DEA Code Number: 9400) is included on this list.

Biochemical research tool for studying the mechanism of narcotic action; also as an antidote for acute morphine poisoning.

Therapeutic Category: Narcotic antagonist.

Therapeutic Category (Vet): Narcotic antagonist.

Medication

Medication (Vet)

Diacetylmorphine (heroin) is demethylated with cyanogen bromide and hydrolyzed to normorphine, which is alkylated with allyl bromide to give nalorphine.

Prepd from normorphine.

Allorphine

Anarcon

Anthorphine

Antofin

For more Formulations/Preparations (Complete) data for NALORPHINE (19 total), please visit the HSDB record page.

Nalorphine is listed in schedule iii of controlled substances act.

... allyl derivative of morphine. ... able to "antagonize" or neutralize most of the effects of narcotic drugs (morphine, codeine), but not those of other types of depressants

Nalorphine ... no longer available in the United States.