Pethidine

Indications
 Oral
Moderate to severe acute pain
Adult: As hydrochloride: 50-150 mg every 4 hr if needed.
Child: As hydrochloride: Children 2 mth to 12 yr: 0.5-2 mg/kg; 12-18 yr: 50-100 mg. Repeat dose every 4-6 hr if necessary.
Elderly: As hydrochloride: 50 mg every 4 hr.
Renal impairment: Dose reductions may be necessary.
Hepatic impairment: Dose reductions may be necessary.
Parenteral
Moderate to severe acute pain
Adult: As hydrochloride: 25-100 mg IM/SC inj or 25-50 mg by slow IV inj repeated after 4 hr.
Child: As hydrochloride: SC/IM: 2 mth to 12 yr: 0.5-2 mg/kg; 12-18 yr: 20-100 mg. Repeat dose every 4-6 hr if needed. IV inj: Neonates and children ≥12 yr: 0.5-1 mg/kg IV inj every 10-12 hr if needed in those up to 2 mth and every 4-6 hr if needed in older children. 12-18 yr: 25-50 mg every 4-6 hr if needed. Alternatively, ≥1 mth: Loading dose: 1 mg/kg by IV inj followed by 100-400 mcg/kg/hr via continuous IV infusion adjusted according to response.
Elderly: 25 mg every 4 hr.
Renal impairment: Dose reductions may be necessary.
Hepatic impairment: Dose reductions may be necessary.
Parenteral
Obstetric analgesia
Adult: As hydrochloride: 50-100 mg by IM/SC inj as soon as contractions occur at regular intervals; repeat after 1-3 hr if needed. Max: 400 mg in 24 hr.
Renal impairment: Dose reductions may be necessary.
Hepatic impairment: Dose reductions may be necessary.
Parenteral
Preoperative medication
Adult: As hydrochloride: 25-100 mg IM/SC given 1 hr before surgery.
Child: As hydrochloride: 1-2 mg/kg given IM 1 hr before surgery.
Renal impairment: Dose reductions may be necessary.
Hepatic impairment: Dose reductions may be necessary.
Parenteral
Postoperative pain
Adult: As hydrochloride: 25-100 mg IM/SC inj every 2-3 hr if necessary.
Child: As hydrochloride: 0.5-2 mg/kg IM every 2-3 hr if necessary.
Renal impairment: Dose reductions may be necessary.
Hepatic impairment: Dose reductions may be necessary.
Intravenous
Adjunct to anaesthesia
Adult: As hydrochloride: 10-25 mg by slow IV inj.
Renal impairment: Dose reductions may be necessary.
Hepatic impairment: Dose reductions may be necessary.

Reconstitution: IV infusion: Dilute with glucose 5% or sodium chloride 0.9% to required volume. IV inj: Dilute with water for inj to a concentration of 5-10 mg/ml.
Incompatibility: Y-site incompatible with idarubicin, imipenem/cilastatin, minocycline, allopurinol, amphotericin B cholesteryl sulfate complex, cefepime, cefoperazone, doxorubicin liposome. Admixture incompatibility: Aminophylline, amobarbital, floxacillin, furosemide, heparin, morphine, phenobarbital, phenytoin, thiopental, pentobarbital. Syringe incompatibility: Pentobarbital, heparin, morphine.
Warnings / Precautions
 May impair ability to drive or operate machinery. Hypovolaemia, CV disease; adrenal insufficiency; biliary tract disorder; CNS depression or coma; history of drug abuse or acute alcoholism; head injury, intracranial lesions, elevated intracranial pressure; hepatic or renal impairment; morbidly obese; prostatic hyperplasia; toxic psychoses; pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive airway disease; sickle-cell disease; supraventricular tachycardia; thyroid dysfunction. Elderly and debilitated patients. Withdraw gradually. Pregnancy (avoid prolonged use or high doses at term) and lactation.
Adverse Reactions
 Hypotension; fatigue, drowsiness, dizziness, nervousness, headache, restlessness, malaise, confusion, depression, hallucinations, tremors, muscle twitches, increased intracranial pressure, seizure, serotonin syndrome; rash, urticaria; nausea, vomiting, constipation, anorexia, stomach cramps, xerostomia, biliary spasm, paralytic ileus, sphincter of Oddi spasm; ureteral spasms, decreased urination; pain at inj site; weakness; dyspnoea; histamine release, physical and psychological dependence.
Overdose Reactions
 Symptoms: CNS/respiratory depression, mydriasis, bradycardia, pulmonary oedema, chronic tremor, CNS excitability, seizures. Treatment: Symptomatic. Naloxone can be used to reverse opioid effects. Do not use naloxone for pethidine-induced seizures.
Drug Interactions
 Increased pethidine metabolite levels with aciclovir, cimetidine, ritonavir. Reduced analgesic effects with phenytoin, barbiturates. Additive sedative and/or respiratory depressive effects with alcohol, barbiturates, benzodiazepines, phenothiazines, TCAs, other CNS depressants.
Potentially Fatal: Increased risk of serotonin syndrome with MAOIs (not be given concurrently or within 14 days of their discontinuation), serotonin agonists, serotonin reuptake inhibitors, sibutramine, TCAs.
See Below for More pethidine Drug Interactions
Food Interactions
 Increased CNS depression with valerian, St John's wort, kava kava, gotu kola.
Mechanism of Actions
 Pethidine is a phenylpiperidine derivative opioid analgesic. It acts mainly as mu-receptor agonist. Like most, opioid analgesics, it mimics endogenous opioids by activating opioid receptors in the central and peripheral nervous system. It reduces the release of neurotransmitter substances and also reduces the activity of postsynaptic neurons in the spinal cord thus preventing transmission of pain impulse.
Absorption: Absorbed from the GI tract; only 50% reaches the circulation due to 1st-pass effect. Peak plasma concentrations after 1-2 hr (oral). Variable absorption (IM).
Distribution: Crosses the placenta; enters breast milk; appears in CSF. Protein-binding: 60-80%.
Metabolism: Extensively hepatic via hydrolysis to pethidinic acid and norpethidinic acid and via demethylation to norpethidine.
Excretion: Via urine (small amounts as unchanged drug); elimination half-life: 3-5 hr (unchanged drug), 20 hr (norpethidine).
Storage Conditions
 Intravenous: Store at room temperature. Do not freeze and protect from light. Oral: Protect from light. Store at room temperature. Parenteral: Store at room temperature. Do not freeze and protect from light.
ATC Classification
 N02AB02 - pethidine ; Belongs to the class of phenylpiperidine derivative opioids. Used to relieve pain.
Storage
 Intravenous: Store at room temperature. Do not freeze and protect from light. Oral: Protect from light. Store at room temperature. Parenteral: Store at room temperature. Do not freeze and protect from light.
Available As
  • Pethidine 50 mg

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