Generic
Pethidine Hydrochloride
2 brands available in the market
At a glance
Pethidine Hydrochloride is an opioid analgesic used for short-term (24-36 hours) relief of moderate to severe pain. It can be given via intramuscular, subcutaneous, slow intravenous bolus, intravenous infusion, and patient-controlled analgesia (PCA).
Description
Pethidine is a phenylpiperidine derivative opioid analgesic that acts mainly as a mu-receptor agonist. It mimics endogenous opioids by activating opioid receptors in the central and peripheral nervous system, reducing neurotransmitter release and postsynaptic neuron activity in the spinal cord, thus preventing pain impulse transmission.
Indications
- Moderate to severe pain (short-term 24-36 hours)
- Anaesthetic adjunct
- Obstetric analgesia
- Preoperative medication
- Postoperative pain
Therapeutic class
Opioid analgesics
Pharmacological class
Opioid Agonist (Mu-receptor)
Pharmacology
Pethidine is a phenylpiperidine derivative opioid analgesic that acts mainly as a mu-receptor agonist. It activates opioid receptors in the CNS and peripheral nervous system, reduces neurotransmitter release, and decreases postsynaptic neuron activity in the spinal cord, preventing pain transmission.
Mechanism of action
Prevents pain signal transmission by activating mu-opioid receptors.
Dosage
Adult Dose (Parenteral):
- Analgesia (IM/SC): 25-100 mg every 3-4 hours
- Analgesia (slow IV): 25-50 mg every 3-4 hours
- Obstetric analgesia: 50-100 mg IM/SC; repeat after 1-3 hours if needed; max 400 mg/24 hours
- Preoperative: 25-100 mg IM/SC (1 hour before surgery)
- Postoperative: 25-100 mg IM/SC every 2-3 hours
- IV infusion: 0.3 mg/kg/hr initially
- PCA: 5-20 mg demand dose, 6-20 min lockout interval
- Elderly (>70 years): Half the normal adult dose
- Hepatic/renal impairment: Dose reduction/increased intervals
Pediatric Dose (Parenteral):
- Analgesia (IM/SC): 0.5-2 mg/kg every 4-6 hours (max 100 mg)
- Preoperative: 1-2 mg/kg IM (1 hour before surgery)
- Postoperative: 0.5-2 mg/kg IM every 2-3 hours
- Neonates: Safety not established
Administration
- Administered by healthcare professional; do not self-administer
- Can be given IM, SC, slow IV bolus, or IV infusion
- IV injection should be given very slowly (preferably diluted)
- PCA allows patient-controlled dosing
Missed dose
If you miss a dose, take it as soon as possible; if almost time for next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Sleepiness
- Vomiting
- Headache
- Dizziness
- Nausea
- Constipation
- Hyperhidrosis
- Bizarre feelings
- Confusion
- Hallucinations
Precautions & warnings
- May decrease alertness and cause drowsiness or dizziness; do not drive if these occur
- Avoid alcohol (may cause excessive drowsiness and respiratory depression)
- Caution in respiratory depression, head injury, raised intracranial pressure
- Caution in elderly, hypothyroidism, Addison's disease
- Caution in hepatic/renal impairment (risk of norpethidine toxicity)
- Do not use with or within 2 weeks of MAOIs
- Caution in cardiac arrhythmias, cor pulmonale
Contraindications
- Hypersensitivity to pethidine
- Respiratory depression (acute bronchial asthma, chronic airway disease, severe emphysema, severe chronic bronchitis)
- Head injury, raised intracranial pressure, brain tumor
- Cardiac arrhythmias (especially supraventricular tachycardia), cor pulmonale
- Concurrent use or within 2 weeks of MAOIs
- Pre-eclampsia, eclampsia
- Convulsive states (status epilepticus, tetanus, strychnine poisoning)
- Diabetic acidosis (risk of coma)
- Acute alcoholism or delirium tremens
- Severe liver disease, incipient hepatic encephalopathy
- Low platelet count, coagulation disorders, or anticoagulant treatment
- Continuous IV infusion in renal impairment
- PCA in young children and adults with poor cognitive function
Drug interactions
- Aciclovir, cimetidine, ritonavir: Increased pethidine metabolite levels
- Phenytoin, barbiturates: Reduced analgesic effects
- Alcohol, barbiturates, benzodiazepines, phenothiazines, TCAs, other CNS depressants: Additive sedative and/or respiratory depressive effects
- Potentially fatal: Increased risk of serotonin syndrome with MAOIs, serotonin agonists, serotonin reuptake inhibitors, sibutramine, TCAs
Food interactions
Caution is advised when consuming alcohol with Pethidine Hydrochloride.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects. Pregnancy Category C; may cause respiratory depression in the newborn.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited human data suggests no significant risk. Pethidine is excreted in breast milk; not recommended for nursing mothers.
Pediatric use
Safety not established in neonates; 2 months-12 years: 0.5-2 mg/kg; 12-18 years: 20-100 mg.
Geriatric use
Elderly patients (>70 years): Half the normal adult dose recommended.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; risk of norpethidine accumulation; dose reduction or increased interval recommended; continuous IV infusion and PCA contraindicated in severe renal impairment.
Hepatic Impairment: Caution in liver disease; dose reduction and/or increased intervals recommended; severe liver disease contraindicated.
Overdose effects
Overdose: CNS/respiratory depression, mydriasis, bradycardia, pulmonary edema, chronic tremor, CNS excitability, seizures. Treatment: Symptomatic; naloxone can reverse opioid effects (do not use for pethidine-induced seizures).
Storage conditions
Store at room temperature; do not freeze; protect from light.
Chemical structure
Pethidine Hydrochloride