Pethidine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Moderate to severe acute pain 50-150 mg 4 hrly. IV Adjunct to anesth 10-25 mg. IV/IM/SC Moderate to severe acute pain 25-100 mg IM/SC inj or 25-50 mg by slow IV inj repeated after 4 hr. IM/SC Obstetric analgesia 50-100 mg as soon as contractions occur at regular intervals; repeat after 1-3 hr if needed. Max: 400 mg/24 hr. Pre-op medication 25-100 mg 1 hr pre-op. Post-op pain25-100 mg 2-3 hrly if needed.
Dosage Details
Intravenous
Adjunct to anaesthesia
Adult: As hydrochloride: 10-25 mg by slow IV inj.

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.

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.

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.

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.

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.
Reconstitution
Intravenous:
Dilute with water for inj to a concentration of 5-10 mg/ml.
Parenteral:
Moderate to severe acute pain: 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
Intravenous:
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.
Parenteral:
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.
Special 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.
Epidural/IM/IV/Parenteral/PO/SC: C
Overdosage
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.
Food Interaction
Increased CNS depression with valerian, St John's wort, kava kava, gotu kola.
Action
Description: 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.
Pharmacokinetics:
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
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.
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Pethidine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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