Pethidine

Brands of Pethidine in Kenya

Pethidine, Macarthys Laboratories Ltd T/a Martindale Pharmaceuticals
Pethidine HCl Fresenius PF, Fresenius Kabi Manufacturing SA (Pty) Limited


Pethidine in Kenya: Uses, Chemical Structure, Abuse, Prices
Pethidine Chemical Structure

INDICATIONS:

Relief of moderate to severe pain.

Premedication.

Obstetric analgesia.

Enhancement of analgesia

DOSAGE

Adults.

For moderate or severe pain.

Normal single dose (usually not to be repeated more often than 4 hourly)

By intramuscular or subcutaneous injection
By slow intravenous injection
25 – 100 mg.
25 – 50 mg.
For obstetric analgesia.

By intramuscular or subcutaneous injection repeated 1 – 3 hours later. 50 – 100 mg.

Maximum of 400mg in 24 hours.

As a premedication.

By intramuscular injection one hour prior to the operation. 50 – 100mg

For the enhancement of analgesia.

By slow intravenous injection. 10 – 25mg as required.

Elderly or debilitated patients.

Initial doses should not exceed 25mg as this group of patients may be specially sensitive to the central depressant effect of the drug.

Paediatric population

For moderate or severe pain.

By intramuscular injection. 0.5 – 2 mg per Kg of body weight.

As a premedication.

By intramuscular injection one hour prior to the operation. 1 – 2 mg per kg of body weight.

CONTRAINDICATIONS

Hypersensitivity to the active substance or to any of the excipients.

Severe respiratory depression, severe obstructive airways disease or acute asthma.

It should not be administered to patients with severe renal impairment or severe hepatic impairment.

Should be avoided in patients with acute alcoholism, delirium tremens, raised intracranial pressure or in those with convulsive states such as status epilepticus.

It should not be administered to patients receiving monoamine oxidase inhibitors ( including moclobemide, and the monoamine B inhibitors selegiline and rasagiline) or within two weeks of their withdrawal.

Pethidine should not be administered to patients receiving ritonavir.

Use of pethidine should be avoided in patients with supraventricular tachycardia.

Use of pethidine in patients with phaechromocytoma may result in hypertensive crisis.

Use of pethidine should be avoided in patients with diabetic acidosis where there is danger of coma.

In comatose patients

In patients with a risk of paralytic ileus

In patients with head injuries.

DRUG INTERACTIONS

Monoamine Oxidase Inhibitors

The concurrent use of MAOIs (including moclobemide) is contra-indicated as they may result in CNS excitation or depression.

Pethidine should not be administered to patients receiving monoamine oxidase inhibitors or moclobemide or within two weeks of their withdrawal .

CNS depressants

CNS depressants such as alcohol, hypnotics, anxiolytics and sedatives, barbiturates and tricyclic antidepressants may increase the general depressant effects of pethidine and should therefore be used with caution.

Opioid agonists

Additive effects on CNS depression, respiratory depression and hypotension can occur with concomitant use of opioid agonist analgesics.

MAO-B inhibitors

Concomitant use of MAO-B inhibitors such as selegiline or rasagiline is contraindicated  as this may lead to hyperpyrexia and CNS toxicity.

Rasagiline should not be given with pethidine as there is risk of CNS toxicity, its use should be avoided for two weeks after taking rasagiline.

Anticonvulsants

Administration of phenytoin may cause an increase in hepatic metabolism of pethidine and subsequently increased levels of norpethidine (a toxic metabolite).

Antipsychotics

Concomitant use of phenothiazines and pethidine can induce severe hypotension.

Anti-virals

Plasma concentrations of pethidine may be decreased by concomitant administration of ritonavir, however levels of norpethidine (a toxic metabolite) may rise. Concomitant administration of ritonavir and pethidine should be avoided .

Histamine H2 antagonists

Cimetidine can reduce the metabolism of pethidine resulting in increased plasma concentration.

Effects of pethidine on other drugs

Pethidine may have an effect on the activities of other drugs, for example domperidone, as a consequence of reduced gastro-intestinal motility.

The plasma levels of ciprofloxacin may be reduced in the presence of opiate premedicants.

Plasma levels of mexiletine may also be reduced in the presence of opioid analgesics.

Possible increased serotonergic effects when pethidine is given with SSRI’s.

Sedative medicines such as benzodiazepines or related drugs:

The concomitant use of opioids with sedative medicines such as benzodiazepines or related drugs increases the risk of sedation, respiratory depression, coma and death because of additive CNS depressant effect. The dose and duration of concomitant use should be limited

ADVERSE EFFECTS

The most serious adverse effects of pethidine are respiratory depression and hypotension. Rapid intravenous administration of pethidine increases the incidence of these effects and may result in serious respiratory depression and hypotension with tachycardia.

Reporting of suspected adverse reactions:

The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:

 

Clinical | Pharmacokinetic data


Pregnancy Category: C
Routes of Administration: By mouth, IV, IM, IT,SC, epidural
Bioavailability: 50–60% (Oral), 80–90% (Oral, in cases of hepatic impairment)
Protein Binding: 65–75%
Metabolosim: Liver
Onset of Action: Not Available
Elimination Half life: 2.5–4 hours, 7–11 hours (liver disease)
Excretion: Renal

Legal Status | Dosage forms & Strengths


Prescription Category:
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:
Tablets | Injectable

Drug Indentifiers:

CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard


Drug Images

References/ Citation:




What was the patient being treated for
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