INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION
Q-MED PETHIDINE Injection 25 mg/1 mL
Q-MED PETHIDINE Injection 50 mg/1 mL
Q-MED PETHIDINE Injection 100 mg/2 mL

SCHEDULING STATUS:
S7

PROPRIETARY NAME
(and dosage form):

Q-MED PETHIDINE Injection 25 mg/1 mL
Q-MED PETHIDINE Injection 50 mg/1 mL
Q-MED PETHIDINE Injection 100 mg/2 mL

COMPOSITION:
1 mL Ampoules containing 25 mg pethidine hydrochloride.
1 mL Ampoules containing 50 mg pethidine hydrochloride.
2 mL Ampoules containing 100 mg pethidine hydrochloride.

PHARMACOLOGICAL CLASSIFICATION:
A 2.9 Other Analgesics

PHARMACOLOGICAL ACTION:
Pethidine is predominantly a mu receptor agonist. It exerts its main pharmacological action on the central nervous system and the neutral elements in the bowel. The rate of absorption may be erratic after intramuscular injection. Pethidine is metabolised mainly in the liver with a half-life of about 3 hours.

INDICATIONS:
Pethidine is indicated for the relief of severe pain. It is particularly useful for the relief of postoperative pain. It may be used to relieve labour pain.

CONTRA-INDICATIONS:
Hypersensitivity to pethidine. Pethidine is contra-indicated in respiratory depression, especially in the presence of cyanosis and excessive bronchial secretion, chronic lung disease, renal and hepatic insufficiency. It should be given with caution to patients with supra-ventricular tachycardia or a history of convulsive disorders. It is also contra-indicated in the presence of acute alcoholism, head injuries, and conditions in which intracranial pressure is raised. Pethidine should not be given to patients who are being treated with monoamine oxidase inhibitors, or within 2 weeks of the discontinuation of such treatment. It should not be given during an attack of bronchial asthma or in heart failure secondary to chronic lung disease.

WARNINGS:
Prolonged use of pethidine may lead to dependence.
Cross-tolerance and cross-dependence can be expected between opioids acting at the same receptors.

DOSAGE AND DIRECTIONS FOR USE:

Children:	0,5 mg to 2 mg per kg body-mass may be given by intramuscular injection.
Adults:	25 mg to 100 mg by subcutaneous or intramuscular injection and by slow intravenous injection in doses of 25 mg to 50 mg.
Obstetric Analgesia:	50 mg to 100 mg may be given by intramuscular or subcutaneous injection as soon as contractions occur at regular intervals. This dose may be repeated after 1 to 3 hours if necessary.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects:
In normal doses the commonest side-effects of pethidine are nausea, vomiting, constipation, drowsiness and confusion. Micturition may be difficult and there may be uretic or biliary spasm; t        here is also an anti-diuretic effect. Dry mouth, sweating, facial flush vertigo, bradycardia, palpitations, orthostatic hypotension, hypothermia, restlessness, changes of mood, hallucinations and miosis also occur. Raised intracranial pressure occurs in some patients. The euphoric activity of pethidine has led to their abuse.
Larger doses produce respiratory depression and hypotension, with circulatory failure and deepening coma. Convulsions may occur in infants and children. Death may occur from respiratory failure.
Due to the histamine-releasing effect, reactions such as urticaria pruritus, as well as hypotension and flushing occur in some individuals. Pain and irritation may occur on injection. Anaphylactic reactions, following intravenous injection of pethidine have been reported as well as muscle rigidity.
The administration of pethidine during labour may cause respiratory depression in the newborn infant.
The intravenous administration of pethidine may result in increased heartrate.

Special Precautions:
The dosage should be reduced in elderly and debilitated patients.
It should be given with caution or in reduced doses to patients with hypothyroidism, adrenocortical insufficiency, impaired kidney or liver function, prostatic hypertrophy, or shock. It should be used with caution in patients with obstructive bowel disorders. Opioid analgesics should be used with caution in patients with myasthenia gravis. The depressant effects of pethidine are enhanced by depressants of the central nervous system such as alcohol, anaesthetics, hypnotics and sedatives, tricyclic antidepressants, and phenothiazines.
It should be used with extreme caution in patients with decreased respiratory reserve.
Pethidine should be used with caution in patients with phaeochromocytoma.
Pethidine crosses the placenta and is excreted in breast milk.

Interactions:
Barbiturates:
Opioid analgesics and barbiturates can be expected to have additive central nervous system (CNS) depressant effects.

Histamine H2antagonists:
Cimetidine reduces the clearance and volume of distribution of pethidine.

Phenothiazines:
Prochlorperazine prolongs the respiratory depressant effect of pethidine in healthy subjects.

Phenytoin:
The hepatic metabolism of pethidine appears to be enhanced by phenytoin.

KNOWN SYMPTOMS OF OVERDOSAGE AND ITS TREATMENT
See "Side-effects" for symptoms.
Intensive supportive therapy may be required to correct respiratory failure and shock. In addition, the specific antagonist naloxone hydrochloride is used to counteract very rapidly the severe respiratory depression and coma produced by excessive doses of opioid analgesics. A dose of 0,4 mg to 2 mg is given intravenously, repeated at intervals of 2 to 3 minutes if necessary, up to 10 mg. Naloxone may also be given by subcutaneous or intramuscular injection. The effect of naloxone may be of shorter duration than that of the opioid analgesic and additional doses may be required to prevent relapses. Respiration assistance may be necessary.
Circulation should be maintained with infusions of dextrose injection and suitable electrolyte solutions.

IDENTIFICATION:
Clear, colourless solution in clear, colourless glass ampoules.

PRESENTATION:
Boxes of 10 x 1 mL Ampoules –25 mg/1 mL
Boxes of 10 x 1 mL Ampoules –50 mg/1 mL
Boxes of 10 x 2 mL Ampoules –100 mg/2 mL

STORAGE INSTRUCTIONS:
Store below 25°C.
Keep out of reach of children.
Protect from light.

REGISTRATION NUMBERS:
25 mg/1 mL: 31/2.9/0083
50 mg/1 mL: 31/2.9/0084
100 mg/2 mL: 31/2.9/0085

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Quatromed Limited
10 Lindley Street
BETHLEHEM 9701

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
4 December 1996                Pro-Print PPE0191/1-97
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