Drug information of Pethidine

Pethidine

Drug group:

Opiate agonist; a synthetic phenylpiperidine derivative.

Mechanism of effect

Precise mechanism of action has not been fully elucidated; opiate agonists act at several CNS sites, involving several neurotransmitter systems to produce analgesia.

Pharmacodynamic

Opiate agonists act at specific receptor binding sites in the CNS and other tissues; opiate receptors are concentrated in the limbic system, thalamus, striatum, hypothalamus, midbrain, and spinal cord.

Pharmacokinetics

Oral: Undergoes extensive first-pass metabolism in the liver, with approximately 50–60% of a dose reaching systemic circulation unchanged.
IM: Approximately 80–85% of a dose of the drug is absorbed within 6 hours after intragluteal injection.
Oral, peak analgesia: Within 1 hour and declines gradually over 2–4 hours. Sub-Q, peak analgesia: In about 40–60.
IM, peak analgesia: In about 30–50 minutes. Sub-Q or IM: Analgesia is maintained for 2–4 hours.Crosses the placenta; may accumulate in fetus. Distributes into breast milk.Plasma Protein Binding is Approximately 60–80%.
Metabolism is Principally in the liver.Normeperidine is the active metabolite and exhibits about half the analgesic potency of meperidine but twice the CNS stimulant (e.g., seizure-inducing) potency.Excreted in urine as metabolites and unchanged drug.

Dosage

Usual Adult Dose for Pain
Oral:
50 to 150 mg orally every 3 to 4 hours as needed
Maximum dose: 600 mg per day
Parenteral:
50 to 150 mg IM or subcutaneously every 3 to 4 hours as needed; IM administration is preferred when repeated dose are required .
-May be administered IV, however, lower doses are advised and administration should be very slow, preferably using a diluted solution .
Patient Controlled Analgesia (PCA):
-Initial dose: 10 mg with a range of 1 to 5 mg per incremental dose; Lockout interval: 6 to 10 minutes; adjust dose based on patient response .
For continuous IV infusion, the usual adult dose is 15 to 35 mg per hour
Usual Adult Dose for Anesthesia
For Preoperative Medication:
Usual dose: 50 to 100 mg IM or subcutaneously 30 to 90 minutes before the beginning of anesthesia
For Obstetrical Analgesia:
Usual dose: 50 to 100 mg IM or subcutaneously when pain becomes regular; may repeat at 1 to 3 hour intervals
For Support of Anesthesia:
-Slow IV fractional doses or continuous IV infusion of a dilute (e.g. 1 mg/mL) solution; titrate to needs of patients
Comment:
-This drug should not be administered IV unless a narcotic antagonist and facilities for assisted or controlled respiration are immediately available.
Uses: As a preoperative medication and for support of anesthesia and obstetrical analgesia.
Usual Pediatric Dose for Pain
Oral:
Initial dose: 1.1 to 1.8 mg/kg orally every 3 to 4 hours as needed
Maximum single dose: 50 to 150 mg
Maximum daily dose: 600 mg
Parenteral:
Initial dose: 1.1 to 1.8 mg/kg IM or subcutaneously every 3 to 4 hours as needed; IM administration is preferred when repeated doses are required
Maximum single dose: 50 to 150 mg
-May be administered IV, however, lower doses are advised and administration should be very slow, preferably using a diluted solution.
• Usual Pediatric Dose for Anesthesia
For Preoperative Medication:
Usual dose: 1.1 to 2.2 mg/kg IM or subcutaneously 30 to 90 minutes before the beginning of anesthesia .
Maximum dose: 50 to 100 mg
For Support of Anesthesia:
-Slow IV fractional doses or continuous IV infusion of a dilute (e.g. 1 mg/mL) solution; titrate to needs of patients .

Drug contraindications

severe hypersensitivity reactions

Alerts

• Serotonin syndrome may occur in patients receiving meperidine in conjunction with other serotonergic drugs or drugs that impair serotonin metabolism (e.g., MAO inhibitors). Serotonin syndrome may occur at usual dosages.
• Manifestations may include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile BP, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination, rigidity), and/or GI symptoms (e.g., nausea, vomiting, diarrhea).
• Additive depressant effects may occur with concomitant use of other CNS depressants including other opiates, sedatives or hypnotics, general anesthetics, phenothiazines, tranquilizers, skeletal muscle relaxants, sedating antihistamines, and alcohol. When such combined therapy is contemplated, the dose of one or both agents should be reduced.
• Adrenal insufficiency reported in patients receiving opiate agonists or opiate partial agonists.
• Respiratory depression effects and ability of opiates to increase CSF pressure may be markedly exaggerated in patients with head injury, other intracranial lesions, or preexisting elevation in intracranial pressure; opiate effects may produce cerebral hypoxia and obscure clinical course of patients with head injuries.
• May cause severe hypotension postoperatively or when ability to maintain blood pressure is compromised (e.g., depleted blood volume, concurrent phenothiazine or general anesthetic use).
• Inadvertent IM injection into or near nerve trunks can result in sensory-motor paralysis, which may or may not be transient.
• Some commercially available formulations contain sodium metabisulfite, a sulfite that may cause allergic-type reactions, including anaphylaxis and life-threatening or less severe asthmatic episodes, in certain susceptible individuals.
• Accumulation of toxic normeperidine metabolite can stimulate the CNS and precipitate seizures in patients without a preexisting seizure disorder.
• May increase ventricular response rate through a vagolytic action, therefore use with caution in patients with atrial flutter and other supraventricular tachycardias.

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you have:
• If you have an allergy to meperidine or any other part of meperidine injection.
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
• If you have any of these health problems: Lung or breathing problems like asthma, trouble breathing, or sleep apnea; high levels of carbon dioxide in the blood; or stomach or bowel block or narrowing.
• If you are taking any of these drugs: Buprenorphine, butorphanol, nalbuphine, or pentazocine.
• If you have taken certain drugs used for low mood (depression) like isocarboxazid, phenelzine, or tranylcypromine or drugs used for Parkinson's disease like selegiline or rasagiline in the last 14 days. Taking this medicine within 14 days of those drugs can cause very bad high blood pressure.
• If you are taking any of these drugs: Linezolid or methylene blue.
• Do not take meperidine injection with other strong pain drugs or if you are using a pain patch without talking to your doctor first.
• Do not use more than what your doctor told you to use. Do not use more often or longer than what you were told. Doing any of these things may raise the chance of very bad side effects.
• If you have been taking this medicine for a long time or at high doses, it may not work as well and you may need higher doses to get the same effect. This is known as tolerance. Call your doctor if meperidine injection stops working well. Do not take more than ordered.
• If you have been taking this medicine on a regular basis and you stop it all of a sudden, you may have signs of withdrawal. Do not stop taking meperidine injection all of a sudden without calling your doctor. Tell your doctor if you have any bad effects.

Pregnancy level

C


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