|
|
|
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. |
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
| |