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meperidine (Demerol, Isonipecaine, Chlorbycyclen, Centralgin)

Tradename: Demerol. DEA-controlled substance: class 2. Indications: 1) treatment of moderate to severe pain 2) anesthesia-related pain control 3) rigors induced by amphotericin B Contraindications: 1) co-administration of MAO inhibitors 2) renal failure (accumulation of active metabolite normeperidine may induce seizures. Dosage: 1) 50-100 mg IV/IM/SC every 3-4 hours 2) 1-1.8 mg/kg up to 150 mg IM/PO every 3-4 hours 3) 25 mg increments 4) give with 25-50 mg of hydroxyzine a) adjunct in pain relief b) reduces nausea 5) continuous infusion not recommended Tabs: 50 & 100 mg. Syrup: 50 mg/5 mL. Injection: 1) multiple dose vials: 50 mg/mL (30 mL), 100 mg/mL (20 mL) 2) single dose ampules: 25 mg (0.5 mL 1 mL), 50 mg (1 mL) 75 mg (1 mL, 1.5 mL), 100 mg (1 mL) 15-100 mg IM = 10-15 mg of IM morphine or 7 mg IV 100 mg PO = 10 mg morphine PO Synergism: Co-administration of hydroxyzine may decrease nausea & potentiate analgesia. Pharmacokinetics: 1) poor oral absorption 2) analgesic effects with IM or SC administration a) onset of action: within 15 minutes b) peak effect within 1 hour c) duration of action 2-4 hours 3) metabolized by the liver to normeperidine* (active) 4) significant 1st pass metabolism 5) excreted in the urine -> normeperidine may accumulated in renal failure 6) 1/2life 3 hours, increased to 7 hours with liver failure * twice the convulsant properties of parent compound Adverse effects: 1) common (> 10%) - weakness, tiredness, nausea/vomiting, hypotension, drowsiness, dizziness, histamine release, constipation 2) less common (1-10%) - ureteral spasms, pain at injection site, nervousness, headache, restlessness, anorexia, malaise, epigastric cramps, dry mouth, biliary spasms, decreased urination confusion, dyspnea 3) uncommon (< 1%) - paralytic ileus, depression, hallucination, paradoxical CNS stimulation, rash, urticaria, increased intracranial pressure, physical & psychologic dependence 4) other - rash or allergic reactions in sulfite-sensitive patients - tachycardia or bradycardia - increase in systemic vascular resistance (vagolytic) - respiratory depression - dose & tolerance-dependent - greater with IV dosing - myoclonus & seizures with accumulation of normeperidine; naloxone does not reverse CNS toxicity caused by normeperidine & may actually increase neuroexcitability [8] Drug interactions: 1) benzodiazepines, barbiturates, alcohol in combination increases CNS adverse effects 2) MAO-inhibitors - contraindicated, fatal reaction have occurred 3) naloxone: direct antagonist to opiate agonists 4) phenothiazines/tranquilizers in combination may increase the risk of seizures &/or CNS depressant effects 5) isoniazid in combination aggravates many of INH side effects 6) tricyclic antidepressants (TCA) may potentiate the effects of meperidine 7) phenytoin may decreasse the analgesic effects of meperidine 8) phenobarbital may increase meperidine metabolism Laboratory: 1) specimen: serum, plasma (heparin, EDTA) 2) methods: GLC, color, fluorometry 3) interferences: -> nicotine may interfere with colorimetric methods 4) labs with Loincs - meperidine in specimen - meperidine in hair - meperidine in gastric fluid - meperidine in meconium - meperidine in saliva - meperidine in serum/plasma/blood - meperidine in serum/plasma - meperidine in urine Mechanism of action: 1) opiate agonist a) partial opioid mu agonist b) mostly opioid kappa activity 2) its chief pharmacologic effects are on the CNS & neural elements in the bowel 2) alters perception of pain at the level of the spinal cord & higher levels of the central nervous system 3) alters emotional response to pain 4) causes less of an increase in biliary pressure than morphine 5) antimuscarinic activity 6) negative inotropic activity

Interactions

drug interactions drug adverse effects (more general classes)

Related

normeperidine (Norpethidine)

General

opiate opioid receptor agonist (narcotic) piperidine

Properties

MISC-INFO: elimination route LIVER 1/2life 3.6 HOURS therapeutic-range 400-700 NG/ML toxic-range >1000 NG/ML protein-binding 40-60% pregnancy-category C + safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 504
  2. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 5
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  5. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  6. Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
  7. Finley R & Liao S, In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
  8. Medical Knowledge Self Assessment Program (MKSAP) 14, American College of Physicians, Philadelphia 2006

Component-of

meperidine/promethazine