Relidin®
Pethidine
25, 50 and 100 mg Ampoule
Acute pain: Management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate; obstetrical analgesia, preoperative medication.
Mechanism of Action:
Binds to opioid receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression.
Method of Administration:
IM (preferred route), IV: 50 to 150 mg every 3 to 4 hours as needed; maximum daily dose: 600 mg; limit duration to ≤48 hours. If IV administration is required, administer diluted and at a slow rate. Dosing based on severity of pain; start at the lower end of dosing range.
Notes
Contraindications:
Hypersensitivity (eg, anaphylaxis) to meperidine or any component of the formulation; use with or within 14 days of MAO inhibitors; significant respiratory depression; acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment; GI obstruction, including paralytic ileus (known or suspected).
Interactions:
Anticholinergic Agents: May enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor therapy
Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Meperidine. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Meperidine. Risk C: Monitor therapy CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Meperidine. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Meperidine. Risk C: Monitor therapy
Dapoxetine: May enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Do not use serotonergic agents (high risk) with dapoxetine or within 7 days of serotonergic agent discontinuation. Do not use dapoxetine within 14 days of monoamine oxidase inhibitor use. Dapoxetine labeling lists this combination as contraindicated. Risk X: Avoid combination
FentaNYL: Meperidine may enhance the CNS depressant effect of FentaNYL. Meperidine may enhance the serotonergic effect of FentaNYL. This could result in serotonin syndrome. Management: Consider alternatives to this combination. If use is necessary, monitor for signs and symptoms of serotonin syndrome/serotonin toxicity and CNS depression. Risk D: Consider therapy modification
Tricyclic Antidepressants: May enhance the CNS depressant effect of Serotonergic Opioids (High Risk). Serotonergic Opioids (High Risk) may enhance the serotonergic effect of Tricyclic Antidepressants. This could result in serotonin syndrome. Management: Consider alternatives to this drug combination. If combined, monitor for signs and symptoms of serotonin syndrome/serotonin toxicity and CNS depression. Risk D: Consider therapy modification
Pregnancy and Lactation:
Opioids cross the placenta. According to some studies, maternal use of opioids may be associated with birth defects (including neural tube defects, congenital heart defects, and gastroschisis), poor fetal growth, stillbirth, and preterm delivery.
Breast milk exposure to meperidine and normeperidine is consistently associated with neonatal sedation and may interfere with breastfeeding. Nonopioid analgesics are preferred for breastfeeding females who require pain control peripartum or for surgery outside of the postpartum period; meperidine is not recommended if an opioid is needed.
Warning and Precaution:
- CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
- CNS events: Normeperidine (an active metabolite and CNS stimulant) may accumulate and precipitate anxiety, tremors, or seizures; risk increases with preexisting CNS or renal dysfunction, prolonged use (>48 hours), and cumulative dose (>600 mg/24 hours in adults). Oral meperidine should not be used since first-pass metabolism decreases efficacy while increasing normeperidine concentrations (APS 2016). Note: Naloxone does not reverse, and may even worsen, neurotoxicity.
- Constipation: May cause constipation which may be problematic in patients with unstable angina and patients’ post-myocardial infarction (MI). Consider preventive measures (eg, stimulant laxative) to reduce the potential for constipation.
- Hypotension: May cause severe hypotension (including orthostatic hypotension and syncope); use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics). Monitor for symptoms of hypotension following initiation or dose titration. Avoid use in patients with circulatory shock.
- Respiratory depression: Serious, life-threatening, or fatal respiratory depression may occur. Monitor closely for respiratory depression, especially during initiation or dose escalation. Carbon dioxide retention from opioid-induced respiratory depression can exacerbate the sedating effects of opioids. Patients and caregivers should be educated on how to recognize respiratory depression and the importance of getting emergency assistance immediately in the event of known or suspected overdose.
- Serotonin syndrome: May occur with concomitant use of serotonergic agents (eg, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, triptans, tricyclic antidepressants), lithium, St. John’s wort, agents that impair metabolism of serotonin (eg, monoamine oxidase inhibitors [MAOIs]), or agents that impair metabolism of tramadol (eg, CYP2D6 and 3A4 inhibitors). Monitor patients for serotonin syndrome such as mental status changes (eg, agitation, hallucinations, coma); autonomic instability (eg, tachycardia, labile blood pressure, hyperthermia); neuromuscular changes (eg, hyperreflexia, incoordination); and/or GI symptoms (eg, nausea, vomiting, diarrhea).
Adverse Reactions:
Cardiovascular: Bradycardia, cardiac arrest, circulatory depression, flushing, hypotension, palpitations, shock, syncope, tachycardia
Central nervous system: Agitation, confusion, delirium, disorientation, dizziness, drug dependence (physical dependence), habituation, hallucination, headache, increased intracranial pressure, involuntary muscle movements (including muscle twitching, myoclonus), mood changes (including euphoria, dysphoria), sedation, seizure (associated with metabolite accumulation), serotonin syndrome
Dermatologic: Diaphoresis, pruritus, skin rash, urticaria
Gastrointestinal: Biliary colic, constipation, nausea, spasm of sphincter of Oddi, vomiting, xerostomia
Genitourinary: Urinary retention Hypersensitivity: Anaphylaxis, histamine release, hypersensitivity reaction
Local: Injection site reaction (including pain, wheal, and flare)
Neuromuscular & skeletal: Tremor, weakness Ophthalmic: Visual disturbance
Respiratory: Dyspnea, respiratory arrest, respiratory depression
Storage:
Store below 30ºC and protect from freezing