levorphanol


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levorphanol

 [lēv-or´fah-nol]
a potent synthetic opioid analgesic with properties and actions similar to those of morphine; used as the bitartrate salt as an analgesic and an anesthesia adjunct, administered orally, subcutaneously, intramuscularly, or intravenously.
Miller-Keane Encyclopedia and Dictionary of Medicine, Nursing, and Allied Health, Seventh Edition. © 2003 by Saunders, an imprint of Elsevier, Inc. All rights reserved.

levorphanol

(lee-vor-fan-ole) ,

Levo-Dromoran

(trade name)

Classification

Therapeutic: opioid analgesics
Pharmacologic: opioid agonists
Pregnancy Category: C

Indications

Moderate to severe pain.

Action

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

Therapeutic effects

Decreased pain.

Pharmacokinetics

Absorption: Well absorbed following oral and subcut administration.
Distribution: Extensive.
Metabolism and Excretion: Mostly metabolized by the liver.
Half-life: 12–16 hr; may be as long as 30 hr with chronic dosing.

Time/action profile (analgesic effect)

ROUTEONSETPEAKDURATION
PO10–60 min90–120 min4–5 hr
Subcutunknown60–90 min4–5 hr
IVunknownwithin 20 min4–5 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Obstetric / Lactation: Avoid chronic use during pregnancy or lactation.
Use Cautiously in: Head trauma; Increased intracranial pressure; Severe renal, hepatic, or pulmonary disease; Hypothyroidism; Adrenal insufficiency; Alcoholism; Undiagnosed abdominal pain; Prostatic hyperplasia; Geriatric: Geriatric or debilitated patients (dose ↓ suggested).

Adverse Reactions/Side Effects

Central nervous system

  • confusion (most frequent)
  • sedation (most frequent)
  • dysphoria
  • euphoria
  • dizziness
  • floating feeling
  • hallucinations
  • headache
  • unusual dreams

Ear, Eye, Nose, Throat

  • blurred vision
  • diplopia
  • miosis

Respiratory

  • respiratory depression

Cardiovascular

  • hypotension (most frequent)
  • bradycardia

Gastrointestinal

  • constipation (most frequent)
  • dry mouth
  • nausea
  • vomiting

Genitourinary

  • urinary retention

Dermatologic

  • flushing
  • sweating
  • pruritis

Miscellaneous

  • physical dependence
  • psychological dependence
  • tolerance

Interactions

Drug-Drug interaction

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 or pentazocine may decrease analgesia.Concomitant use of kava, valerian, skullcap, chamomile, or hops can increase CNS depression.

Route/Dosage

Larger doses may be required during chronic use
Oral (Adults ≥50 kg) Initial dosing in opioid-naive patients—4 mg q 6–8 hr.
Oral (Adults and Children <50 kg) Initial dosing in opioid-naive patients—0.04 mg/kg q 6–8 hr (unlabeled for use in children).
Subcutaneous Intravenous (Adults ≥50 kg) Initial dosing in opioid-naive patients—2 mg q 6–8 hr. Preoperative use—1–2 mg subcut 90 min prior to procedure.
Subcutaneous Intravenous (Adults and Children <50 kg) Initial dosing in opioid-naive patients—0.02 mg/kg mg q 6–8 hr (unlabeled for use in children).

Availability (generic available)

Tablets: 2 mg
Solution for injection: 2 mg/mL

Nursing implications

Nursing assessment

  • Assess type, location, and intensity of pain prior to and 90–120 min following PO, 60–90 min following subcut, and 20 min (peak) following IV administration. When titrating opioid doses, increases of 25–50% should be administered until there is either a 50% reduction in the patient’s pain rating on a numerical or visual analogue scale or the patient reports satisfactory pain relief. A repeat dose can be safely administered at the time of the peak if previous dose is ineffective and side effects are minimal.
  • An equianalgesic chart (see ) should be used when changing routes or when changing from one opioid to another.
  • Assess BP, pulse, and respirations before and periodically during administration. If respiratory rate is <10/min, assess level of sedation. Dose may need to be decreased by 25–50%. Initial drowsiness will diminish with continued use.
  • Assess bowel function routinely. Prevention of constipation should be instituted with increased intake of fluids and bulk and with laxatives to minimize constipating effects. Stimulant laxatives should be administered routinely if opioid use exceeds 2–3 days, unless contraindicated.
  • Prolonged use may lead to physical and psychological dependence and tolerance. This should not prevent patient from receiving adequate analgesia. Most patients who receive levorphanol for pain do not develop psychological dependence. Progressively higher doses may be required to relieve pain with long-term therapy.
  • Lab Test Considerations: May ↑ plasma amylase and lipase concentrations.
  • If an opioid antagonist is required to reverse respiratory depression or coma, naloxone (Narcan) is the antidote. Dilute the 0.4-mg ampule of naloxone in 10 mL of 0.9% NaCl and administer 0.5 mL (0.02 mg) by direct IV push every 2 min. For children and patients weighing <40 kg, dilute 0.1 mg of naloxone in 10 mL of 0.9% NaCl for a concentration of 10 mcg/mL and administer 0.5 mcg/kg every 2 min. Titrate dose to avoid withdrawal, seizures, and severe pain.

Potential Nursing Diagnoses

Acute pain (Indications)
Disturbed sensory perceptionvisual, auditory (Side Effects)
Risk for injury (Side Effects)

Implementation

  • high alert: Accidental overdosage of opioid analgesics has resulted in fatalities. Before administering, clarify all ambiguous orders; have second practitioner independently check original order, dose calculations, and infusion pump settings.
  • Explain therapeutic value of medication prior to administration to enhance the analgesic effect.
    • Regularly administered doses may be more effective than prn administration. Analgesic is more effective if given before pain becomes severe.
    • Coadministration with nonopioid analgesics may have additive analgesic effects and permit lower opioid doses.
    • Medication should be discontinued gradually after long-term use to prevent withdrawal symptoms.
  • Oral: May be administered with food or milk to minimize GI irritation.
  • Intravenous: Subcutaneous: Patients receiving parenteral therapy should be lying down and remain recumbent to minimize side effects for at least 30–60 min.
  • Intravenous Administration
  • Diluent: May be administered undiluted.
  • Rate: Administer slowly, over 3–5 min. Rapid administration may lead to increased respiratory depression, hypotension, and circulatory collapse.
  • Syringe Compatibility: glycopyrrolate
  • Y-Site Compatibility: aminocaproic acid, amphotericin B liposome', bleomycin, carboplatin, cisplatin, cyclophosphamide, cytarabine, dactinomycin, dexmedetomidine, docetaxel, doxacurium, doxorubicin hydrochloride, epirubicin, eptifibitide, etoposide, etoposide phosphate, fenoldopam, fludarabine, fluorouracil, idarubicin, ifosfamide, irinotecan, levofloxacin, methchlorethamine, methotrexate, mitoxantrone, oxaliplatin, paclitaxel, pamidronate, propofol, quinupristin/dalfopristin, rituximab, rocuronium, sodium acetate, tacrolimus, vincristine, vinorelbine
  • Y-Site Incompatibility: pantoprazole, trastuzumab

Patient/Family Teaching

  • Instruct patient on how and when to ask for pain medication.
  • Instruct patient to take levorphanol as directed. If dose is less effective after a few weeks, do not increase dose without consulting health care professional.
  • Medication may cause drowsiness or dizziness. Advise patient to call for assistance when ambulating or smoking. Caution patient 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.

Evaluation/Desired Outcomes

  • Decrease in severity of pain without a significant alteration in level of consciousness or respiratory status.
Drug Guide, © 2015 Farlex and Partners
References in periodicals archive ?
([section]) Short and long acting opioid drugs in this study included buprenorphine, butorphanol, codeine, dihydrocodeine, fentanyl, hydrocodone, hydromorphone, levorphanol, meperidine, methadone, morphine, naltrexone, nalbuphine, naloxone, oxycodone, oxymorphone, pentazocine, propoxyphene, tapentadol, and tramadol.
Opioid medications included the following: Codeine, Fentanyl, Hydrocodone, Hydro-morphone, Levorphanol, Meperidine, Morphine, Oxycodone, Oxymorphone, Pentazocine, Propoxyphene, Tapentadol and Tramadol.
Novel therapies company Relmada Therapeutics (Other OTC:RLMD) reported on Wednesday that it has been granted a patent (EP 2 448 406 B1) from the European Patent Office (EPO) for compositions and methods of use for its extended release oral levorphanol (3-hydroxy-N-methylmorphinan).
They focused on schedule II opioid prescriptions containing oxycodone, fentanyl, hydrocodone, morphine, methadone, hydromorphone, oxymorphone, meperidine, codeine, opium, or levorphanol (JAMA Intern Med.
The prescribed drugs included codeine, dihydrocodeine, meperidine, morphine, oxycodone, hydrocodone, hydromorphone, fentanyl, oxymorphone, propoxyphene, methadone, tramadol, and levorphanol, said Dr.
Opioids should not be withheld if indicated for acute pain, although the best choice of opioid is a pure opioid agonist or mu receptor agonist, such as morphine, methadone (Dolophine[R]), codeine, fentanyl, oxycodone, levorphanol, oxymorphone (Opana[R]), or hydromorphone (Pasero et al., 2011).
Relmadaa[euro](tm)s chief executive Sergio Traversa said that the firm intends to finalise the needed steps to move LevoCap ER, its once daily formulation of levorphanol, into Phase III development, d-methadone, its NDMA receptor antagonist for diabetic painful neuropathy (DPN), to enter Phase IIb, MepiGel and BuCap to commence the pilot PK studies and to prepare the company for a public transaction in the first half of next year.
These include morphine, alfentanil, tramadol, fentanyl, hydromorphone (Dilaudid), methadone, and levorphanol.
The opiates, along with their semi-synthetic opioid derivatives (heroin, hydrocodone, hydromorphone, nalbuphine, oxycodone, oxymorphone) and the increasing number of completely synthetic opioids (propoxyphene, levorphanol, meperidine, diphenoxylate, butorphanol, methadone, fentanyl derivatives, tramadol, buprenorphine, tapentadol) have a long and checkered history in medicine.
Doctors extracted 63 capsules containing a beige coloured substance,later found to be a mixture of codeine, levorphanol and diazepam.
Dextromethorphan is the d-isomer of the codeine analogue of levorphanol which mimics morphine.