Levorphanol Tartrate

Pronunciation: lee-VORE-fah-nole TAR-trate
Class: Opioid analgesic

Trade Names

Levorphanol Tartrate
- Tablets, oral 2 mg

Pharmacology

Acts at receptors in the gray matter in the brain and spinal cord to alter the transmission and perception of pain.

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Pharmacokinetics

Absorption

Steady-state plasma levels are reached by the third day of dosing. Well absorbed following oral administration, reaching the C max in about 1 h.

Distribution

Vd is 10 to 13 L/kg. Plasma protein binding is 40%.

Elimination

Terminal half-life is about 11 to 16 h; Cl is 0.78 to 1.1 L/kg/h.

Indications and Usage

Management of moderate to severe pain, or as a preoperative medication when opioid analgesia is appropriate.

Contraindications

None well documented.

Dosage and Administration

Adults

PO Recommended starting dose is 2 mg. This may be repeated in 6 to 8 h as needed. If necessary, the dose may be increased to 3 mg every 6 to 8 h. Generally, total oral daily dosages of more than 6 to 12 mg in 24 h are not recommended.

Chronic Pain
Adults

PO When converting a patient from morphine to levorphanol, begin the total daily dose of levorphanol at approximately 1/15 to 1/12 the total daily dose of oral morphine.

Perioperative Use
Adults

Dosage should be based on age, body weight, physical status, underlying pathological condition, other drug usage, type of anesthesia, surgical procedure, and severity of pain.

Respiratory Function Impairment
Adults

Reduce dose by 50% or more.

General Advice

  • Administer prescribed dose without regard to meals. Administer with food if GI upset occurs.
  • If using fixed-scheduled dosing (round the clock), do not escalate dose more often than every 72 h to allow patient to reach new steady-state and reduce risk of excessive sedation caused by drug accumulation.

Storage/Stability

Store between 59° and 86°F.

Drug Interactions

Agonist/Antagonist opioid analgesics (eg, buprenorphine, butorphanol, nalbuphine, pentazocine)

Do not administer to patients receiving levorphanol.

CNS depressants (eg, alcohol, antihistamines, barbiturates, general anesthetics, hypnotics, other opioids, phenothiazines, sedatives, skeletal muscle relaxants, tranquilizers, tricyclic antidepressants)

Additive CNS depressant effects. Respiratory depression, hypotension, profound sedation, or coma may occur.

Adverse Reactions

Cardiovascular

Arrhythmias (including bradycardia and tachycardia), cardiac arrest, extrasystoles, hypotension, palpitations, shock.

CNS

Abnormal dreams, abnormal thinking, amnesia, coma, confusion, convulsions, depression, dizziness, drug withdrawal, dyskinesia, hyperkinesia, hypokinesia, insomnia, lethargy, nervousness, personality disorder, stimulation, suicide attempt.

Dermatologic

Pruritus, rash, sweating, urticaria.

EENT

Abnormal vision, diplopia, pupillary disorder.

GI

Abdominal pain, biliary tract spasm, dry mouth, dyspepsia, nausea, vomiting.

Genitourinary

Difficulty urinating, kidney failure, urinary retention.

Respiratory

Apnea, cyanosis, hypoventilation.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Reduce initial dose 50%.

Special Risk Patients

Use with caution and reduce initial dose in patients who are elderly or debilitated, or those who have severe hepatic or renal impairment, hypothyroidism, Addison disease, toxic psychosis, prostatic hypertrophy, urethral stricture, acute alcoholism, or delirium tremens.

Asthma

Use in acute or severe bronchial asthma is not recommended.

Biliary surgery

May increase pressure in common bile duct when given in analgesic doses; use is not recommended in biliary surgery.

CV effects

Because the effects on heart activity are unknown, limit levorphanol use in patients with myocardial dysfunction, acute MI, or coronary insufficiency.

Drug dependence

Has abuse potential.

Head injury

Respiratory depressant effects may be markedly exaggerated in the presence of head injury, intracranial lesions, or preexisting increased intracranial pressure.

Hypotension

May cause severe hypotension in postoperative patients or in individuals whose ability to maintain BP is compromised (eg, volume depletion). May cause orthostatic hypotension in ambulatory patients.

Liver disease

Use with caution in patients with extensive liver disease.

Respiratory depression

May cause serious or potentially fatal respiratory depression if given in excessive dose, too frequently, or if given in full dosage to compromised patients. Use with caution in patients with impaired respiratory reserve or respiratory depression. Reduce initial dose by 50% or more.

Withdrawal syndrome

Discontinuation after chronic use has been reported to result in withdrawal syndrome.

Overdosage

Symptoms

Apnea, bradycardia, cardiac arrest, circulatory collapse, CNS depression, cold and clammy skin, constricted pupils, CV failure, extreme somnolence progressing to stupor or coma, hypotension, respiratory depression, skeletal muscle flaccidity, death.

Patient Information

  • Caution patients or caregivers that medication may be habit forming, to take as prescribed, and not to stop taking or change the dose unless advised by their health care provider. Advise patients or caregivers to notify their health care provider if medication does not adequately control pain.
  • Advise patient, family, or caregiver that if medication needs to be discontinued after prolonged use, it will usually be slowly withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
  • Advise patients to notify their health care provider if any of the following occur and are bothersome or appear to worsen: dizziness or lightheadedness; sleepiness or drowsiness; upset stomach, vomiting, constipation, or stomach pain; rash; difficulty urinating.
  • Advise patients or caregivers to immediately notify their health care provider if any of the following occur: fainting, slow or shallow breathing, excessive sleepiness.
  • Instruct patients to get up slowly from lying or sitting position and to avoid sudden position changes to prevent postural hypotension. Advise patients to report dizziness with position changes to their health care provider. Caution patients that hot tubs and hot showers or baths may make dizziness worse.
  • Caution patient that drug may cause dizziness or drowsiness and to use caution while driving or performing other tasks requiring mental alertness or coordination until tolerance is determined.
  • Caution patient to avoid alcohol and other CNS depressant medications while using this medication.
  • Advise patient that medication is usually started at a low dose and then gradually increased as tolerated until maximum benefit is obtained.
  • Advise patient that if a dose is missed, to take it as soon as possible unless it is nearing time for the next scheduled dose. If it is nearing time for the next dose, advise patient to skip the missed dose and take the next dose at the regularly scheduled time. Caution patient not to double the dose to catch up.

Copyright © 2009 Wolters Kluwer Health.

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