meperidine (Demerol, Isonipecaine, Chlorbycyclen, Centralgin)
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Introduction
Tradename: Demerol. DEA-controlled substance: class 2.
Indications
- treatment of moderate to severe pain
- anesthesia-related pain control
- rigors induced by amphotericin B
Contraindications
- co-administration of MAO inhibitors
- renal failure (accumulation of active metabolite normeperidine may induce seizures.
Dosage
- 50-100 mg IV/IM/SC every 3-4 hours
- 1-1.8 mg/kg up to 150 mg IM/PO every 3-4 hours
- 25 mg increments
- give with 25-50 mg of hydroxyzine
- continuous infusion not recommended
Tabs: 50 & 100 mg.
Syrup: 50 mg/5 mL.
Injection:
- multiple dose vials: 50 mg/mL (30 mL), 100 mg/mL (20 mL)
- 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
Synergism: Co-administration of hydroxyzine may decrease nausea & potentiate analgesia.
Pharmacokinetics
- poor oral absorption
- analgesic effects with IM or SC administration
- onset of action: within 15 minutes
- peak effect within 1 hour
- duration of action 2-4 hours
- metabolized by the liver to normeperidine* (active)
- significant 1st pass metabolism
- excreted in the urine
- normeperidine may accumulated in renal failure
- 1/2life 3 hours, increased to 7 hours with liver failure
* twice the convulsant properties of parent compound
elimination via liver
1/2life = 3.6 hours
protein binding = 40-60 %
Adverse effects
- common (> 10%)
- weakness, tiredness, nausea/vomiting, hypotension, drowsiness, dizziness, histamine release, constipation
- 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
- uncommon (< 1%)
- paralytic ileus, depression, hallucination, paradoxical CNS stimulation, rash, urticaria, increased intracranial pressure, physical & psychologic dependence
- 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 adverse effects of opiates
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- benzodiazepines, barbiturates, alcohol in combination increases CNS adverse effects
- MAO-inhibitors - contraindicated, fatal reaction have occurred
- naloxone: direct antagonist to opiate agonists
- phenothiazines/tranquilizers in combination may increase the risk of seizures &/or CNS depressant effects
- isoniazid in combination aggravates many of INH side effects
- tricyclic antidepressants (TCA) may potentiate the effects of meperidine
- phenytoin may decreasse the analgesic effects of meperidine
- phenobarbital may increase meperidine metabolism
- drug interaction(s) of benzodiazepine with opiates
- drug interaction(s) of Z-drugs with opiates
- drug interaction(s) of alcoholic beverage with opiates
- drug interaction(s) of pregabalin with opiates
- drug interaction(s) of gabapentin with opiates
Laboratory
- specimen: serum, plasma (heparin, EDTA)
- methods: GLC, color, fluorometry
- interferences:
- nicotine may interfere with colorimetric methods
- labs with Loincs
Mechanism of action
- opiate agonist
- its chief pharmacologic effects are on the CNS & neural elements in the bowel
- alters perception of pain at the level of the spinal cord & higher levels of the central nervous system
- alters emotional response to pain
- causes less of an increase in biliary pressure than morphine
- antimuscarinic activity
- negative inotropic activity
More general terms
Additional terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 504
- ↑ Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 5
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
- ↑ Finley R & Liao S, In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
- ↑ 8.0 8.1 Medical Knowledge Self Assessment Program (MKSAP) 14, American College of Physicians, Philadelphia 2006