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Medication Safety Issues
Avoid the use of meperidine for pain control, especially in elderly and renally-compromised patients (Institute for Safe Medication Practices [ISMP], 2007)
Sound-alike/look-alike issues:
Meperidine may be confused with meprobamate
Demerol® may be confused with Demulen®, Desyrel®, dicumarol, Dilaudid®, Dymelor®, Pamelor®
High alert medication: The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.
Pronunciation
(me PER i deen)
U.S. Brand Names
Index Terms
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Management of moderate-to-severe pain; adjunct to anesthesia and preoperative sedation
Use: Dental
Adjunct in preoperative intravenous conscious sedation in patients undergoing dental surgery; alternate oral narcotic in patients allergic to codeine to treat moderate to moderate-severe pain
Use: Unlabeled/Investigational
Reduce postoperative shivering; reduce rigors from amphotericin
Restrictions
C-II
Pregnancy Risk Factor
C/D (prolonged use or high doses at term)
Pregnancy Considerations
Meperidine is known to cross the placenta, which may result in respiratory or CNS depression in the newborn.
Lactation
Enters breast milk/contraindicated (AAP rates “compatible”)
Breast-Feeding Considerations
Meperidine is excreted in breast milk and may cause CNS and/or respiratory depression in the nursing infant.
Contraindications
Hypersensitivity to meperidine or any component of the formulation; use with or within 14 days of MAO inhibitors; pregnancy (prolonged use or high doses near term)
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• CNS events: Normeperidine (an active metabolite and CNS stimulant) may accumulate and precipitate anxiety, tremors, or seizures; risk increases with renal dysfunction and cumulative dose.
• Hypotension: May cause hypotension; use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics).
Disease-related concerns:
• Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions.
• Adrenal insufficiency: Use with caution in patients with adrenal insufficiency, including Addison's disease.
• Biliary tract impairment: Use with caution in patients with biliary tract dysfunction; acute pancreatitis may cause constriction of sphincter of Oddi.
• CNS depression/coma: Use with caution in patients with CNS depression or coma.
• Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use.
• Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure; exaggerated elevation of ICP may occur.
• Hepatic impairment: Use with caution in patients with hepatic disorders.
• Obesity: Use with caution in patients who are morbidly obese.
• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture.
• Psychoses: Use with caution in patients with toxic psychoses.
• Renal impairment: Avoid use in patients with renal impairment.
• Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages.
• Sickle-cell disease: Use is not recommended; increased risk of normeperidine-induced seizures.
• Tachycardias: Use with caution in patients with supraventricular tachycardias.
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Debilitated patients: Use with caution in debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages.
• Elderly: Avoid use in the elderly.
Dosage form specific issues:
• Sulfites: Some preparations contain sulfites which may cause allergic reaction.
Other warnings/precautions:
• Abuse/misuse/diversion: Healthcare provider should be alert to problems of abuse, misuse, and diversion.
• Acute pain management: Meperidine offers no advantage over other opioids as an analgesic and has unique neurotoxicity. The use of meperidine in this setting should be avoided (American Pain Society [APS], 2003; ISMP, 2007).
• Chronic pain management: Use is not recommended for the management of chronic pain.
• Withdrawal: Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with mu opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.
Adverse Reactions
Frequency not defined.
Cardiovascular: Hypotension
Central nervous system: Fatigue, drowsiness, dizziness, nervousness, headache, restlessness, malaise, confusion, mental depression, hallucinations, paradoxical CNS stimulation, increased intracranial pressure, seizure (associated with metabolite accumulation), serotonin syndrome
Dermatologic: Rash, urticaria
Gastrointestinal: Nausea, vomiting, constipation, anorexia, stomach cramps, xerostomia, biliary spasm, paralytic ileus, sphincter of Oddi spasm
Genitourinary: Ureteral spasms, decreased urination
Local: Pain at injection site
Neuromuscular & skeletal: Weakness
Respiratory: Dyspnea
Miscellaneous: Histamine release, physical and psychological dependence
Metabolism/Transport Effects
Substrate (minor) of CYP2B6, 2C19, 3A4
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alvimopan: Analgesics (Opioid) may enhance the adverse/toxic effect of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation. Risk D: Consider therapy modification
Ammonium Chloride: May increase the excretion of Analgesics (Opioid). Risk C: Monitor therapy
Amphetamines: May enhance the analgesic effect of Analgesics (Opioid). Risk C: Monitor therapy
Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Analgesics (Opioid). Risk C: Monitor therapy
Barbiturates: May enhance the CNS depressant effect of Meperidine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Desmopressin: Analgesics (Opioid) may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
MAO Inhibitors: May enhance the serotonergic effect of Meperidine. This may cause serotonin syndrome. Risk X: Avoid combination
Pegvisomant: Analgesics (Opioid) may diminish the therapeutic effect of Pegvisomant. Risk C: Monitor therapy
Phenytoin: May increase the metabolism of Meperidine. Risk C: Monitor therapy
Protease Inhibitors: May enhance the adverse/toxic effect of Meperidine. Protease Inhibitors may decrease the serum concentration of Meperidine. Concentrations of the toxic Normeperidine metabolite may be increased. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: Analgesics (Opioid) may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk C: Monitor therapy
Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification
Sibutramine: May enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Risk X: Avoid combination
Succinylcholine: May enhance the bradycardic effect of Analgesics (Opioid). Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid or limit ethanol (may increase CNS depression). Watch for sedation.
Herb/Nutraceutical: Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
Storage
Meperidine injection should be stored at room temperature; do not freeze. Protect from light. Protect oral dosage forms from light.
Compatibility
Stable in dextran 6% in dextrose, dextran 6% in NS, D5LR, D51/4NS, D51/2NS, D5NS, D5W, D10W, LR, 1/2NS, NS.
Y-site administration: Compatible: Amifostine, amikacin, ampicillin, ampicillin/sulbactam, atenolol, aztreonam, bumetanide, cefamandole, cefazolin, cefotaxime, cefotetan, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, cefuroxime, chloramphenicol, cisatracurium, cladribine, clindamycin, co-trimoxazole, dexamethasone sodium phosphate, diltiazem, diphenhydramine, dobutamine, docetaxel, dopamine, doxycycline, droperidol, erythromycin lactobionate, etoposide phosphate, famotidine, filgrastim, fluconazole, fludarabine, gatifloxacin, gemcitabine, gentamicin, granisetron, heparin, hydrocortisone sodium succinate, insulin (regular), kanamycin, labetalol, lidocaine, linezolid, magnesium sulfate, melphalan, methyldopate, methylprednisolone sodium succinate, metoclopramide, metoprolol, metronidazole, ondansetron, oxacillin, oxytocin, paclitaxel, penicillin G potassium, piperacillin, piperacillin/tazobactam, potassium chloride, propofol, propranolol, ranitidine, remifentanil, sargramostim, teniposide, thiotepa, ticarcillin, ticarcillin/clavulanate, tobramycin, vancomycin, verapamil, vinorelbine. Incompatible: Allopurinol, amphotericin B cholesteryl sulfate complex, cefepime, cefoperazone, doxorubicin liposome, idarubicin, imipenem/cilastatin, minocycline. Variable (consult detailed reference): Acyclovir, furosemide, nafcillin.
Compatibility in syringe: Compatible: Atropine, atropine with hydroxyzine, atropine with promethazine, butorphanol, chlorpromazine, cimetidine, dimenhydrinate, diphenhydramine, droperidol, fentanyl, glycopyrrolate, hydroxyzine, ketamine, metoclopramide, midazolam, ondansetron, pentazocine, pentazocine with perphenazine, perphenazine, prochlorperazine edisylate, promazine, promethazine, ranitidine, scopolamine. Incompatible: Heparin, morphine, pentobarbital.
Compatibility when admixed: Compatible: Cefazolin, dobutamine, metoclopramide, ondansetron, scopolamine, succinylcholine, triflupromazine, verapamil. Incompatible: Aminophylline, amobarbital, floxacillin, furosemide, heparin, morphine, phenobarbital, phenytoin, thiopental. Variable (consult detailed reference): Sodium bicarbonate.
Mechanism of Action
Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression
Pharmacodynamics/Kinetics
Onset of action: Analgesic: Oral, SubQ: 10-15 minutes; I.V.: ~5 minutes
Peak effect: SubQ.: ~1 hour; Oral: 2 hours
Duration: Oral, SubQ.: 2-4 hours
Absorption: I.M.: Erratic and highly variable
Distribution: Crosses placenta; enters breast milk
Protein binding: 65% to 75%
Metabolism: Hepatic; hydrolyzed to meperidinic acid (inactive) or undergoes N-demethylation to normeperidine (active; has 1/2 the analgesic effect and 2-3 times the CNS effects of meperidine)
Bioavailability: ~50% to 60%; increased with liver disease
Half-life elimination:
Parent drug: Terminal phase: Adults: 2.5-4 hours, Liver disease: 7-11 hours
Normeperidine (active metabolite): 15-30 hours; can accumulate with high doses (>600 mg/day) or with decreased renal function
Excretion: Urine (as metabolites)
Dosage
Note: The American Pain Society (2003) and ISMP (2007) do not recommend meperidine's use as an analgesic.
Children: Pain: Oral, I.M., I.V., SubQ: 1-1.5 mg/kg/dose every 3-4 hours as needed; 1-2 mg/kg as a single dose preoperative medication may be used; maximum 100 mg/dose (Note: Oral route is not recommended for acute pain.)
Adults: Pain:
Oral: Initial: Opiate-naive: 50 mg every 3-4 hours as needed; usual dosage range: 50-150 mg every 2-4 hours as needed (manufacturers recommendation; oral route is not recommended for acute pain)
I.M., SubQ: Initial: Opiate-naive: 50-75 mg every 3-4 hours as needed; patients with prior opiate exposure may require higher initial doses
Preoperatively: 50-100 mg given 30-90 minutes before the beginning of anesthesia
Note: If use in acute pain (in patients without renal or CNS disease) cannot be avoided, treatment should be limited to ?48 hours and doses should not exceed 600 mg/24 hours.
Elderly:
Oral: 50 mg every 4 hours
I.M.: 25 mg every 4 hours
Dosing adjustment in renal impairment: Avoid use in renal impairment
Dosing adjustment/comments in hepatic disease: Increased narcotic effect in cirrhosis; reduction in dose more important for oral than I.V. route
Dental Usual Dosing
Pain (analgesic): Adults: Oral: Initial: Opiate-naive: 50 mg every 3-4 hours as needed; usual dosage range: 50-150 mg every 2-4 hours as needed (manufacturers recommendation; oral route is not recommended for acute pain)
Administration: Oral
Administer syrup diluted in 1/2 glass of water; undiluted syrup may exert topical anesthetic effect on mucous membranes
Administration: I.V.
Meperidine may be administered I.M., SubQ, or I.V. IVP should be given slowly, use of a 10 mg/mL concentration has been recommended. For continuous I.V. infusions, a more dilute solution (eg, 1 mg/mL) should be used.
Administration: I.V. Detail
pH: 3.5-6.0 (adjusted)
Monitoring Parameters
Pain relief, respiratory and mental status, blood pressure; observe patient for excessive sedation, CNS depression, seizures, respiratory depression
Reference Range
Therapeutic: 70-500 ng/mL (SI: 283-2020 nmol/L); Toxic: >1000 ng/mL (SI: >4043 nmol/L)
Test Interactions
Increased amylase (S), increased BSP retention, increased CPK (I.M. injections)
Patient Education
If self-administered, use exactly as directed; do not increase dose or frequency. Drug 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); or constipation (increased exercise, fluids, fruit, or fiber may help; if unresolved, consult prescriber about use of stool softeners). Report chest pain, slow or rapid heartbeat, acute dizziness or persistent headache; changes in mental status; seizures; swelling of extremities or unusual weight gain; changes in urinary elimination; acute headache; back or flank pain or muscle spasms; blurred vision; skin rash; or shortness of breath. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.
Geriatric Considerations
Meperidine is not recommended as a drug of first choice for the treatment of chronic pain in the elderly due to the accumulation of its metabolite, normeperidine, which leads to serious CNS side effects (eg, tremor, seizures). If used for acute pain, its use should be limited to 1-2 doses.
Anesthesia and Critical Care Concerns/Other Considerations
The 2002 ACCM/SCCM guidelines for analgesia (critically-ill adult) recommend against using meperidine repetitively. The guidelines recommend fentanyl in patients who need immediate pain relief because of its rapid onset of action; fentanyl or hydromorphone is preferred in patients who are hypotensive or have renal dysfunction. Morphine or hydromorphone is recommended for intermittent, scheduled therapy. Both have a longer duration of action requiring less frequent administration.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation). See Dental Comment.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Dental Comment
Meperidine is not to be used as the narcotic drug of first choice. It is recommended only to be used in codeine-allergic patients when a narcotic analgesic is indicated. Meperidine is not an anti-inflammatory agent. Meperidine, as with other narcotic analgesics, is recommended only for limited acute dosing (ie, 3 days or less); common adverse effects in the dental patient are nausea, sedation, and constipation. Meperidine has a significant addiction liability, especially when given long-term.
Mental Health: Effects on Mental Status
Sedation is common; may cause nervousness or confusion; may rarely produce depression, hallucinations, or paradoxical CNS stimulation
Mental Health: Effects on Psychiatric Treatment
Sedation is common; may cause nervousness or confusion; may rarely produce depression, hallucinations, or paradoxical CNS stimulation
Nursing: Physical Assessment/Monitoring
Assess other medications patient may be taking for additive or adverse interactions. Monitor therapeutic effectiveness and adverse reactions or overdose at beginning of therapy and at regular intervals with long-term use. Monitor frequently for need, may cause physical and/or psychological dependence. For inpatients, implement safety measures. Assess knowledge/teach patient appropriate use (if self-administered), adverse reactions to report, and appropriate interventions to reduce side effects. Discontinue slowly after prolonged use.
Oncology: Vesicant
No
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Injection, solution, as hydrochloride [ampul]: 25 mg/0.5 mL (0.5 mL); 25 mg/mL (1 mL); 50 mg/mL (1 mL, 1.5 mL, 2 mL); 75 mg/mL (1 mL); 100 mg/mL (1 mL)
Injection, solution, as hydrochloride [prefilled syringe]: 25 mg/mL (1 mL); 50 mg/mL (1 mL); 75 mg/mL (1 mL); 100 mg/mL (1 mL)
Injection, solution, as hydrochloride [for PCA pump]: 10 mg/mL (30 mL, 50 mL, 60 mL)
Injection, solution, as hydrochloride [vial]: 25 mg/mL (1 mL); 50 mg/mL (1 mL, 30 mL); 75 mg/mL (1 mL); 100 mg/mL (1 mL, 20 mL) [may contain sodium metabisulfite]
Solution, oral, as hydrochloride: 50 mg/5 mL (500 mL)
Syrup, as hydrochloride:
Demerol®: 50 mg/5 mL (480 mL) [contains benzoic acid; banana flavor] [DSC]
Tablet, as hydrochloride: 50 mg, 100 mg
Demerol®, Meperitab®: 50 mg, 100 mg
Pricing: U.S. (www.drugstore.com)
Solution (Meperidine HCl)
50 mg/5 mL (30): $8.99
100 mg/mL (1): $33.99
Tablets (Demerol)
50 mg (30): $45.56
100 mg (20): $54.97
Tablets (Meperidine HCl)
50 mg (20): $18.66
100 mg (20): $26.66
References
“American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,” Pediatrics, 2001, 108(3):776-89.
American Academy of Pediatrics Committee on Drugs, “Reappraisal of Lytic Cocktail/Demerol®, Phenergan®, and Thorazine® (DPT) for the Sedation of Children,” Pediatrics, 1995, 95(4):598-602.
Armstrong PJ and Bersten A, “Normeperidine Toxicity,” Anesth Analg, 1986, 65(5):536-8.
Buchanan JF and Brown CR, “Designer Drugs: A Problem in Clinical Toxicology,” Med Toxicol Adverse Drug Exp, 1988, 3(1):1-17.
Clark RF, Wei EM, and Anderson PO, "Meperidine: Therapeutic Use and Toxicity," J Emerg Med, 1995,13(6):797-802.
Cole TB, Sprinkle RH, Smith SJ, et al, “Intravenous Narcotic Therapy for Children With Severe Sickle Cell Pain Crisis,” Am J Dis Child, 1986, 140(12):1255-9.
Ferrell BA, “Pain Management in Elderly People,” J Am Geriatr Soc, 1991, 39(1):64-73.
Golembiewski J, "Safety Concerns With Meperidine," J Perianesth Nurs, 2002, 17(2):123-5.
Institute for Safe Medication Practice, “High Alert Medication Feature: Reducing Patient Harm From Opiates,” ISMP Medication Safety Alert, February 22, 2007. Available online at http://www.ismp.org/Newsletters/acutecare/articles/20070222.asp.
Jacobi J, Fraser GL, Coursin DB, et al, “Clinical Practice Guidelines for the Sustained Use of Sedatives and Analgesics in the Critically Ill Adult,” Crit Care Med, 2002, 30(1):119-41. Available at: http://www.sccm.org/pdf/sedatives.pdf. Accessed August 2, 2003.
Kyff JV and Rice TL, “Meperidine-Associated Seizures in a Child,” Clin Pharm, 1990, 9(5):337-8.
Latta KS, Ginsberg B, and Barkin RL, "Meperidine: A Critical Review," Am J Ther, 2002, 9(1):53-68.
Miller RR and Jick H, “Clinical Effects of Meperidine in Hospitalized Medical Patients,” J Clin Pharmacol, 1978, 18(4):180-9.
Mokhlesi B, Leikin JB, Murray P, et al, “Adult Toxicology in Critical Care: Part II: Specific Poisonings,” Chest, 2003, 123(3):897-922.
Olkkola KT, Hamunen K, and Maunuksela EL, “Clinical Pharmacokinetics and Pharmacodynamics of Opioid Analgesics in Infants and Children,” Clin Pharmacokinet, 1995, 28(5):385-404.
Pokela ML, Olkkola KT, Koivisto ME, et al, “Pharmacokinetics and Pharmacodynamics of Intravenous Meperidine in Neonates and Infants,” Clin Pharmacol Ther, 1992, 52(4):342-9.
“Principles of Analgesic Use in the Treatment of Acute Pain and Chronic Cancer Pain,” 5th ed, Glenview, IL: American Pain Society, 2003.
Stone PA, Macintyre PE, and Jarvis DA, “Norpethidine Toxicity and Patient Controlled Analgesia,” Br J Anaesth, 1993, 71(5):738-40.
International Brand Names
Lexi-Comp.com
Last full review/revision August 2008
Content last modified August 2008
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