Look Up > Drugs > Meperidine
Meperidine
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Restrictions
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Reference Range
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(me PER i deen)

U.S. Brand Names
Demerol®

Generic Available

Yes


Synonyms
Isonipecaine Hydrochloride; Meperidine Hydrochloride; Pethidine Hydrochloride

Pharmacological Index

Analgesic, Narcotic


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

Medical: Management of moderate to severe pain; adjunct to anesthesia and preoperative sedation


Restrictions

C-II


Pregnancy Risk Factor

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


Contraindications

Hypersensitivity to meperidine or any component; patients receiving MAO inhibitors presently or in the past 14 days


Warnings/Precautions

Use with caution in patients with pulmonary, hepatic, renal disorders, or increased intracranial pressure; use with caution in patients with renal failure or seizure disorders or those receiving high-dose meperidine; normeperidine (an active metabolite and CNS stimulant) may accumulate and precipitate twitches, tremors, or seizures; some preparations contain sulfites which may cause allergic reaction; not recommended as a drug of first choice for the treatment of chronic pain in the elderly due to the accumulation of normeperidine; for acute pain, its use should be limited to 1-2 doses; tolerance or drug dependence may result from extended use


Adverse Reactions

>10%:

Cardiovascular: Hypotension

Central nervous system: Fatigue, drowsiness, dizziness

Gastrointestinal: Nausea, vomiting, constipation

Neuromuscular & skeletal: Weakness

Miscellaneous: Histamine release

1% to 10%:

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

Gastrointestinal: Anorexia, stomach cramps, xerostomia, biliary spasm

Genitourinary: Ureteral spasms, decreased urination

Local: Pain at injection site

Respiratory: Dyspnea, shortness of breath

<1%: Mental depression, hallucinations, paradoxical CNS stimulation, increased intracranial pressure, rash, urticaria, paralytic ileus, physical and psychological dependence


Overdosage/Toxicology

Symptoms of overdose include CNS depression, respiratory depression, mydriasis, bradycardia, pulmonary edema, chronic tremors, CNS excitability, seizures

Treatment of an overdose includes support of the patient's airway, establishment of an I.V. line, and administration of naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg.


Drug Interactions

CYP2D6 enzyme substrate

Increased toxicity: May aggravate the adverse effects of isoniazid; MAO inhibitors, fluoxetine, and other serotonin uptake inhibitors greatly potentiate the effects of meperidine; acute opioid overdosage symptoms can be seen, including severe toxic reactions; CNS depressants, tricyclic antidepressants, phenothiazines may potentiate the effects of meperidine


Stability

Meperidine injection should be stored at room temperature and protected from light and freezing; protect oral dosage forms from light


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

Oral, S.C., I.M.:

Onset of analgesic effect: Within 10-15 minutes

Peak effect: Within 1 hour

Duration: 2-4 hours

I.V.: Onset of effects: Within 5 minutes

Distribution: Crosses the placenta; appears in breast milk

Protein binding: 65% to 75%

Metabolism: In the liver

Bioavailability: ~50% to 60%; increased with liver disease

Half-life:

Parent drug: Terminal phase: Neonates: 23 hours; range: 12-39 hours; Adults: 2.5-4 hours; Adults with liver disease: 7-11 hours

Normeperidine (active metabolite): 15-30 hours; is dependent on renal function and can accumulate with high doses or in patients with decreased renal function


Usual Dosage

Doses should be titrated to appropriate analgesic effect; when changing route of administration, note that oral doses are about half as effective as parenteral dose

Adults: Oral, I.M., I.V.: S.C.: 50-150 mg/dose every 3-4 hours as needed

Elderly:

Oral: 50 mg every 4 hours

I.M.: 25 mg every 4 hours

Dosing adjustment in renal impairment:

Clcr 10-50 mL/minute: Administer at 75% of normal dose

Clcr <10 mL/minute: Administer at 50% of normal dose

Dosing adjustment/comments in hepatic disease: Increased narcotic effect in cirrhosis; reduction in dose more important for oral than I.V. route


Dietary Considerations

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

Food: Glucose may cause hyperglycemia; monitor blood glucose concentrations


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

amylase (S), BSP retention, CPK (I.M. injections)


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


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

1% to 10% of patients experience dry mouth


Patient Information

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; changes in mental status; 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 be pregnant. Do not breast-feed.


Nursing Implications

If I.V. administration is required, inject very slowly using a diluted solution; administer over at least 5 minutes; intermittent infusion: dilute to 1 mg/mL and administer over 15-30 minutes; dilute to less than or equal to 10 mg/mL for intermittent I.V. use


Dosage Forms

Injection, as hydrochloride:

Multiple-dose vials: 50 mg/mL (30 mL); 100 mg/mL (20 mL)

Single-dose: 10 mg/mL (5 mL, 10 mL, 30 mL); 25 mg/dose (0.5 mL, 1 mL); 50 mg/dose (1 mL); 75 mg/dose (1 mL, 1.5 mL); 100 mg/dose (1 mL)

Syrup, as hydrochloride: 50 mg/5 mL (500 mL)

Tablet, as hydrochloride: 50 mg, 100 mg


References

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.

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.

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

Ferrell BA, "Pain Management in Elderly People," J Am Geriatr Soc, 1991, 39(1):64-73.

Kyff JV and Rice TL, "Meperidine-Associated Seizures in a Child," Clin Pharm, 1990, 9(5):337-8.

Miller RR and Jick H, "Clinical Effects of Meperidine in Hospitalized Medical Patients," J Clin Pharmacol, 1978, 18(4):180-9.

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.

Stone PA, Macintyre PE, and Jarvis DA, "Norpethidine Toxicity and Patient Controlled Analgesia," Br J Anaesth, 1993, 71(5):738-40.


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