levorphanol

Derm: flushing, pruritus, sweating

EENT: diplopia, blurred vision, miosis

GI: constipation, vomiting, dry mouth, nausea

Neuro: confusion, sedation, dizziness, dysphoria, euphoria, floating feeling, hallucinations, headache, unusual dreams

Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA)

Misc: allodynia, opioid-induced hyperalgesia, psychological dependence, physical dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Use with extreme caution in patients receiving MAO inhibitors (may result in unpredictable, severe reactions; decrease initial dose of levorphanol to 25% of usual dose).
Additive CNS depression with alcohol, antihistamines, antidepressants, and sedative/hypnotics.
Administration of partial-antagonist opioid analgesics may precipitate withdrawal in physically dependent patients.
Nalbuphine may ↓ analgesia.

Drug-Natural Products:

Concomitant use of kava, valerian, skullcap, chamomile, or hops can ↑ CNS depression.

Availability ⬆ ⬇

(Generic available)

Tablets: 2 mg; 3 mg

Route/Dosage ⬆ ⬇

Larger doses may be required during chronic use
PO (Adults ≥50 kg): Initial dosing in opioid-naive patients: 4 mg every 6–8 hr.
PO (Adults and Children <50 kg): Initial dosing in opioid-naive patients: 0.04 mg/kg every 6–8 hr (unlabeled for use in children).

Action ⬆ ⬇

Binds to opiate receptors in the CNS, altering perception of and response to pain.
Produces generalized CNS depression.

Therapeutic effects:

Decreased pain.

Classifications ⬆ ⬇

Therapeutic Classification: opioid analgesics

Pharmacologic Classification: opioid agonists

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Extensive.

Metabolism/Excretion: Mostly metabolized by the liver.

Half-Life: 12–16 hr; may be as long as 30 hr with chronic dosing.

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

(analgesic effect)

ROUTE	ONSET	PEAK	DURATION
PO	10–60 min	90–120 min	4–5 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of levorphanol to patient. Instruct them to take medication as directed and when to ask for pain medication. Do not share medication with others, even if they have similar symptoms; may be harmful. Keep out of children's reach. Advise patient to read Patient Informationbefore starting and with each Rx refill in case of changes.
REMS: Instruct patient to take levorphanol as directed. If dose is less effective after a few wks, do not dose without consulting health care professional. Discuss safe use, risks, and proper storage and disposal of opioid analgesics with patients and caregivers with each Rx. The Patient Counseling Guide is available at www.fda.gov/OpioidAnalgesicREMSPCG.
Advise patient that levorphanol is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children and in a location not accessible by others.
Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose. Inform patients and caregivers about various ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines (Rx, direct from pharmacist, or state programs). OTC Narcan nasal spray is available at pharmacies nationwide for overdose or accidental ingestion.
Medication may cause drowsiness or dizziness. Advise patient to call for assistance when ambulating and to avoid driving or other activities that require alertness until response to the medication is known.
Advise patient to change positions slowly to minimize orthostatic hypotension.
Caution patient to avoid concurrent use of alcohol or other CNS depressants.
Advise ambulatory patients that nausea and vomiting may be decreased by lying down.
Encourage patient to turn, cough, and breathe deeply every 2 hr to prevent atelectasis.
Rep: Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Inform patient of potential for neonatal opioid withdrawal syndrome with prolonged use during pregnancy. Monitor neonate for signs and symptoms of withdrawal symptoms (irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, failure to gain weight); usually occur the first days after birth. Monitor infants exposed to levorphanol through breast milk for excess sedation and respiratory depression. Chronic use may reduce fertility in females and males.

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Indications ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇