No

Analgesic, Narcotic

Relief of moderate to severe pain; also used parenterally for preoperative sedation and an adjunct to nitrous oxide/oxygen anesthesia; 2 mg levorphanol produces analgesia comparable to that produced by 10 mg of morphine

C-II

B/D (if used for prolonged periods or in high doses at term)

Hypersensitivity to levorphanol or any component

Use with caution in patients with hypersensitivity reactions to other phenanthrene derivative opioid agonists (morphine, hydrocodone, hydromorphone, levorphanol, oxycodone, oxymorphone); respiratory diseases including asthma, emphysema, COPD or severe liver or renal insufficiency; some preparations contain sulfites which may cause allergic reactions; tolerance or dependence may result from extended use; dextromethorphan has equivalent antitussive activity but has much lower toxicity in accidental overdose. Elderly may be particularly susceptible to the CNS depressant and constipating effects of narcotics.

>10%:

Cardiovascular: Palpitations, hypotension, bradycardia, peripheral vasodilation

Central nervous system: CNS depression, fatigue, drowsiness, dizziness

Dermatologic: Pruritus

Gastrointestinal: Nausea, vomiting

Neuromuscular & skeletal: Weakness

1% to 10%:

Central nervous system: Nervousness, headache, restlessness, anorexia, malaise, confusion

Gastrointestinal: Stomach cramps, xerostomia, constipation

Endocrine & metabolic: Antidiuretic hormone release

Gastrointestinal: Biliary tract spasm

Genitourinary: Decreased urination, urinary tract spasm

Local: Pain at injection site

Ocular: Miosis

Respiratory: Respiratory depression

<1%: Paralytic ileus, mental depression, hallucinations, paradoxical CNS stimulation, increased intracranial pressure, rash, urticaria, histamine release, physical and psychological dependence, histamine release

Symptoms of overdose include CNS depression, respiratory depression, miosis, apnea, pulmonary edema, convulsions

Naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg

Increased toxicity: CNS depressants increase CNS depression

Store at room temperature, protect from freezing; I.V. is incompatible when mixed with aminophylline, barbiturates, heparin, methicillin, phenytoin, sodium bicarbonate

Levorphanol tartrate is a synthetic opioid agonist that is classified as a morphinan derivative. Opioids interact with stereospecific opioid receptors in various parts of the central nervous system and other tissues. Analgesic potency parallels the affinity for these binding sites. These drugs do not alter the threshold or responsiveness to pain, but the perception of pain.

Onset of action: Oral: 10-60 minutes

Duration: 4-8 hours

Adults:

S.C.: 2 mg, up to 3 mg if necessary, every 6-8 hours

Dosing adjustment in hepatic disease: Reduction is necessary in patients with liver disease

Alcohol: Additive CNS effects, avoid or limit alcohol; watch for sedation

Food: Glucose may cause hyperglycemia; monitor blood glucose concentrations

Pain relief, respiratory and mental status, blood pressure

Drowsiness and dizziness are common; may cause nervousness, restlessness, or confusion; may rarely cause depression, hallucinations, or paradoxical CNS stimulation

Concurrent use with psychotropics may produce additive sedation

No information available to require special precautions

~10% of patients experience dry mouth (will disappear with cessation of therapy)

If self-administered, use exactly as directed (do not increase dose or frequency); may cause physical and/or psychological dependence. While using this medication, do not use alcohol and other prescription or OTC medications (especially sedatives, tranquilizers, antihistamines, or pain medications) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). May cause hypotension, dizziness, drowsiness, impaired coordination, or blurred vision (use caution when driving, climbing stairs, or changing position - rising from sitting or lying to standing, or when engaging in tasks requiring alertness until response to drug is known); loss of appetite, nausea, or vomiting (frequent mouth care, small frequent meals, chewing gum, or sucking lozenges may help); constipation (increased exercise, fluids, or dietary fruit and fiber may help - if constipation remains an unresolved problem, consult prescriber about use of stool softeners). Report chest pain, slow or rapid heartbeat, acute dizziness, or persistent headache; swelling of extremities or unusual weight gain; changes in urinary elimination; acute headache; back or flank pain or spasms; blurred vision; skin rash; or shortness of breath. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.

Observe patient for excessive sedation, respiratory depression; implement safety measures, assist with ambulation

Injection, as tartrate: 2 mg/mL (1 mL, 10 mL)

Tablet, as tartrate: 2 mg

"Drugs for Pain," Med Lett Drugs Ther, 1998, 40(1033):79-84.

Sinclair JG and Lo GF, "The Blockade of Serotonin Uptake and the Meperidine-Monoamine Oxidase Inhibitor Interaction," Proc West Pharmacol Soc, 1977, 20:373-4.