INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo PAX INJECTION 10 mg/2 mL

SCHEDULING STATUS:
S5

PROPRIETARY NAME
(and dosage form):

PAX INJECTION 10 mg/2 mL

COMPOSITION:
Each 2 mL ampoule contains 10 mg of
Diazepam, stabilized with 0,12% m/v benzoic acid, 4,88% m/v sodium benzoate and 1,5% v/v benzyl alcohol.

PHARMACOLOGICAL CLASSIFICATION:
A.2.6 Tranquilizers.

PHARMACOLOGICAL ACTION:
It has been found that the major locus of central nervous system depressant action of diazepam on spinal reflexes is the brain stem reticular system. Drug elimination follows a biphasic pattern, with a rapid phase (plus-minus ½ within 2 to 3 hours) followed by a slow decay with a half-time of 2 to 8 days. Diazepam is metabolized to active products including oxazepam. One third is excreted as oxazepam and 70% of the metabolites appear in the urine. Metabolites have been found in the urine and in the plasma 14 days after a 10 mg dose.

INDICATIONS:
Diazepam is used in the treatment of anxiety in neurotic patients, and for preoperative medication. It may be effective in relieving the acute symptoms of the alcohol withdrawal syndrome, but has no specific usefulness in the treatment of psychotic patients. Diazepam injection can also be used to facilitate labour. It can also be used in status epilepticus.

CONTRA INDICATIONS:
Diazepam is contra-indicated in infants and in patients with known hypersensitivity to diazepam. Caution should be observed when giving diazepam to patients with impaired hepatic or renal function and to patients with closed-angle glaucoma. Elderly and debilitated patients are specially sensitive to side-effects and in patients with obstructive airway disease, respiratory depression may be produced. The effects of diazepam may be enhanced by alcohol, barbiturates, narcotics. MAO inhibitors and other depressants of the central nervous system.

WARNINGS:
When given intravenously in the undiluted form, the injection should be administered at a rate not exceeding 5 mg/minute.

DOSAGE AND DIRECTIONS FOR USE :
Intravenous injections should be given into a large lumen vessel, and the solution should be administered slowly (plus-minus 1 mL per minute) if the risk of thrombophlebitis is to be minimised. Intramuscular injection can lead to rise in serum creatine phosphokinase activity, with a maximum between 12 and 24 hours after the injection. Diazepam should not be combined with other aqueous solutions of medicaments except with intravenous solutions of 5 - 10% dextrose or 0,9% sodium chloride.

In this case the contents of the ampoule must quickly be mixed with the total volume of the infusion. In cases of psychiatric disorders and anxiety states the injection can be administered intramuscularly or intravenously in doses of 10 to 20 mg three times daily until acute symptoms subside. In epilepsy an initial dose of 10 to 20 mg intravenously, followed by 20 mg intramuscularly or by intravenous infusion, as required. In severe spasm of central, peripheral and tetanic origin 10 mg once or twice intravenously relieves the spastic state for about 8 hours. For facilitation of labour 20 mg intramuscularly at 2 - 3 fingers dilation.
For anaesthesia: 10 to 20 mg intravenously.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
The toxic effects most frequently encountered with intravenous diazepam are cardiovascular and respiratory depression. Amnesia may persist for a variable period after intravenous administration and care is necessary with ambulant patients. Large doses may produce syncope. Blood dyscrasias and hepatic dysfunction have occasionally been reported. Care should be taken when administered in obstetrics during labour because of the possible effects of central respiratory depression, hypothermia and hypotonia and an increase in foetal heart rate in the infant. In severely disturbed patients treatment with diazepam may result in paradoxical reactions provoking excitement instead of sedation. There is a risk of dependance of the barbiturate-alcohol type and withdrawal reactions including convulsions have been observed in patients receiving large doses for prolonged periods when the medicine was stopped abruptly. Patients taking diazepam should be cautioned against driving motor vehicles, operating machinery or performing tasks where a loss of mental alertness may lead to accidents.

The adverse effects most commonly encountered are drowsiness and oversedation. Drowsiness is more common in elderly and debilitated patients and in patients receiving high doses. Less commonly, the benzodiazepines may produce depression of mood and affect, disorientation or confusion, lethargy, and ataxia.

Paradoxical reactions such as acute hyperexcitable states with rage have been recorded. If these occur, the medicine should be discontinued.

The benzodiazepines have a moderate potential for abuse. Withdrawal symptoms (including convulsions) have occurred following abrupt cessation especially in patients receiving large doses for prolonged periods.

INJECTIONS:
Respiratory depression due to a depressant effect on the respiratory centre and cardiovascular collapse may occasionally occur following intravenous and intramuscular administration of the benzodiazepines.

the benzodiazepines should be administered with particular care to the following patients:

the elderly and debilitated - who are at particular risk of oversedation, respiratory depression and ataxia. (The initial dosage should be reduced in these patients);

patients with pulmonary disease and limited pulmonary reserve;

patients suffering from impairment of renal or hepatic function, or from hypoalbuminaemia;

patients suffering from anxiety concomitant with an underlying depressive disorder;

patients receiving barbiturates or other central nervous system depressants concomitantly with the benzodiazepines. There is an additive risk of central nervous system depression when these medicines are taken together;

patients should be cautioned regarding the additive effect of alcohol when taken together with the benzodiazepines;

the benzodiazepines should be used judiciously during pregnancy and they are preferably avoided. Given during labour, benzodiazepines cross the placenta and may cause the floppy-infant syndrome characterised by central respiratory depression, hypothermia and poor sucking. The benzodiazepines should not be administered to lactating mothers.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Coma, respiratory and cardiovascular depression.
Treatment: No specific antidote is known. General supportive measures should be employed, such as administration of intravenous infusions.
Adequate air passage control must be observed and oxygen can be administered.

Manifestations of overdosage with the benzodiazepines include somnolence, contusion and coma. Gastric aspiration and lavage should be performed, following with 50 g of activated charcoal which should be administed intragastrically. Careful respiratory and cardiovascular support is mandatory. An adequate airway should be maintained. Hypotension, when it occurs, may be controlled with sympathomimetic agents.

IDENTIFICATION:
Clear colourless to pale yellow solution in 2 mL amber glass ampoules.

PRESENTATION:
Amber glass ampoules of 10 mg diazepam per 2 mL packed in boxes of 10.

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

REFERENCE NUMBERS:
K/2.6/220

NAME AND BUSINESS ADDRESS OF APPLICANT:
INTRAMED (PTY) LTD.
6 Gibaud Road
North End 6001

DATE OF PUBLICATION OF THIS LEAFLET:
May 1978 12-101/2-93
  KOHLER C&P P.E.

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