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meperidine (Demerol, pethidine)

 

Classes: Synthetic, Opioids; Opioid Analgesics

Dosing and uses of Demerol, pethidine (meperidine)

 

Adult dosage forms and strengths

syrup: Schedule II

  • 50mg/5mL

tablet: Schedule II

  • 50mg
  • 100mg

injectable solution: Schedule II

  • 25mg/mL
  • 50mg/mL
  • 75mg/mL
  • 100mg/mL

 

Pain

Meperidine is not recommended as a first choice analgesic by The American Pain Society and ISMP (2007); if no other options, limit use in acute pain to ≤48hr; doses should not exceed 600 mg/24hr; oral route is not recommended for treatment of acute or chronic pain

Pain: 50-150 mg PO/IM/SC q3-4hr PRN; adjust dose based degree of response

Preoperatively: 50-150 mg IM/SC q3-4hr PRn

Continuous infusion: 15-35 mg/hr

Obstetrical analgesia: 50-100 mg IM/SC; repeated q1-3hr PRn

 

Dosing Modifications

Renal impairment: Avoid use

Hepatic impairment: Consider lower initial dose intially; increased opioid effect possible in cirrhosis

 

Pediatric dosage forms and strengths

syrup: Schedule II

  • 50mg/5mL

tablet: Schedule II

  • 50mg
  • 100mg

injectable solution: Schedule II

  • 25mg/mL
  • 50mg/mL
  • 75mg/mL
  • 100mg/mL

 

Pain

Meperidine is not recommended as a first choice analgesic by The American Pain Society and ISMP (2007); if no other options, limit use in acute pain to ≤48hr; doses should not exceed 600 mg/24hr; oral route is not recommended for treatment of acute or chronic pain

1-1.8 mg/kg PO/IM/SC q3-4hr PRN; individual dose not to exceed 100 mg

Preoperatively: 1.1-2.2 mg/kg IM/SC 30-90 minutes before initiation of anesthesia

 

Geriatric dosage forms and strengths

 

Pain

50 mg PO q4hr or 25 mg IM q4hr; treatment for acute pain should be limited to 1-2 doses

 

Dosing Considerations

Not drug of choice in elderly patients, because of accumulation of metabolite normeperidine, causing increased central nervous system (CNS) effects

Reduce total daily dose in elderly patients

 

Demerol, pethidine (meperidine) adverse (side) effects

Frequency not defined

Agitation

Angina

Bradycardia

Cardiac arrest

Coma

Constipation

Dizziness

Dry mouth

Dysphoria

Euphoria

Faintness

Hypotension

Mental clouding or depression

Myocardial infarction

Nausea

Nervousness

Palpitation

Physical and psychological dependence

Pruritus, urticaria

QT-interval prolongation

Respiratory arrest

Respiratory/circulatory depression

Restlessness

Sedation

Seizures

Severe cardiac arrhythmias

Shock

ST-segment elevation

Sweating, flushing, warmness of face/neck/upper thorax

Syncope

Tachycardia

Urinary retention

Visual disturbances

Vomiting

Weakness

 

Warnings

Contraindications

Hypersensitivity to drug or component of the formulation

Severe respiratory insufficiency

Within 14 days of taking MAO inhibitors; if linezolid or IV methylene blue (MAOIs) must be administered, discontinue serotonergic drug immediately and monitor for CNS toxicity; may resume 24 hr after last linezolid or methylene blue dose, or after 2 weeks of monitoring, whichever comes first

 

Cautions

Potential for tolerance and drug dependence

Caution in acute abdominal conditions (may obscure diagnosis or clinical course of patient), pseudomembranous colitis, toxin-mediated diarrhea

Narrow therapeutic index in certain patient populations, particularly in combination with CNS-depressant drugs

Cardiac arrhythmias, drug abuse or dependence, emotional lability, gallbladder disease, head injury, increased intracranial pressure, benign prostatic hyperplasia, hepatic or renal impairment, seizures with epilepsy, urethral stricture, urinary tract surgery

Use with caution in following conditions: Sickle cell anemia; pheochromocytoma; acute alcoholism; adrenocortical insufficiency (eg, Addison disease); CNS depression or coma; delirium tremens; debilitated patients; kyphoscoliosis associated with respiratory depression; myxedema or hypothyroidism; prostatic hypertrophy or urethral stricture; head trauma; billiary tract impairment; severe impairment of hepatic, pulmonary, or renal function; toxic psychosis

Interaction with mixed agonist/antagonist opioid analgesics (eg, pentazocine, nalbuphine, butorphanol, buprenorphine) may precipitate withdrawal symptoms

May cause less smooth muscle spasm and constipation than equipotent doses of morphine

Chronic high-dose therapy or administration to patients with renal impairment may result in accumulation of active metabolite normeperidine, leading to agitation and seizures

 

Pregnancy and lactation

Pregnancy category: B; use for prolonged periods or near term not established

Lactation: Drug excreted in breast milk

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Demerol, pethidine (meperidine)

Mechanism of action

Narcotic agonist-analgesic of opiate receptors; inhibits ascending pain pathways, thus altering response to pain; produces analgesia, respiratory depression, and sedation

 

Absorption

Bioavailability: 50-60%; hepatic impairment, 80-90%

Onset: Rapid

Duration: PO/SC, 2-4 hr

Peak plasma time: SC, 40-60 min; IM, 30-50 min

 

Distribution

Protein bound: 65-75%

 

Metabolism

Metabolized in liver via hydrolysis, partial conjugation with glucuronic acid, N-demethylation

Metabolites: Meperidinic acid, normeperidine (active)

 

Elimination

Half-life: 2.5-4 hr (adults); 7-11 hr (liver disease)

Excretion: Urine (primarily)

 

Administration

IV Incompatibilities

Additive: Aminophylline, amobarbital, floxacillin, furosemide, heparin, morphine, phenobarbital, phenytoin, sodium bicarbonate(?)

Syringe: Heparin, morphine, pentobarbitaL

Y-site: Acyclovir(?), allopurinol, amphotericin B cholesteryl sulfate, cefepime, cefoperazone, doxorubicin, furosemide (may be compatible at lower concentrations), idarubicin, imipenem-cilastatin, minocycline, nafcillin(?)

Not specified: Diazepam

 

IV Compatibilities

Solution: Most common solvents

Additive: Cefazolin, dobutamine, metoclopramide, ondansetron, scopolamine, triflupromazine, verapamiL

Syringe: Atropine, butorphanol, chlorpromazine, cimetidine, dimenhydrinate, diphenhydramine, droperidol, fentanyl, glycopyrrolate, hydroxyzine, ketamine, metoclopramide, midazolam, ondansetron, papaveretum, pentazocine, pentazocine with perphenazine, perphenazine, prochlorperazine, promazine, promethazine, promethazine with atropine, ranitidine, scopolamine

Y-site: Amifostine, amikacin, ampicillin, ampicillin-sulbactam, atenolol, aztreonam, bivalirudin, bumetanide, cefamandole, cefazolin, cefotaxime, cefotetan, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, cefuroxime, chloramphenicol, cisatracurium, cladribine, clindamycin, dexamethasone, dexmedetomidine, diltiazem, diphenhydramine, dobutamine, docetaxel, dopamine, doxycycline, droperidol, erythromycin, etoposide phosphate, famotidine, fenoldopam, filgrastim, fluconazole, fludarabine, gatifloxacin, gemcitabine, gentamicin, granisetron, heparin, 6% hetastarch in lactated electrolyte injection (Hextend), hydrocortisone, insulin, kanamycin, labetalol, lidocaine, linezolid, magnesium sulfate, melphalan, methyldopate, methylprednisolone, metoclopramide, metoprolol, metronidazole, ondansetron, oxacillin, oxytocin, paclitaxel, penicillin G, piperacillin, piperacillin-tazobactam, potassium chloride, propofol, propranolol, ranitidine, remifentanyl, sargramostim, teniposide, thiotepa, ticarcillin, ticarcillin-clavulanate, tobramycin, trimethoprim, vancomycin, verapamil, vinorelbine

Not specified: Epinephrine

 

IV/IM Administration

IM: Inject into large muscle mass; when repeated injection is needed, IM is preferred to SC

IV injection: Inject 10 mg/mL very slowly; opiate antagonist and facilities for administration of oxygen and control of respiration should be available during and immediately after administration

Continuous IV infusion: 15-35 mg/hr

Drug has been injected or infused epidurally