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

Logo PAX®-2 TABLET
PAX®-5 TABLET
PAX®-10 TABLET

SCHEDULING STATUS:
S5

PROPRIETARY NAME
(and dosage form):

PAX®-2 TABLET
PAX
®-5 TABLET
PAX
®-10 TABLET

COMPOSITION:
Each tablet contains 2 mg (5 mg, 10 mg)
Diazepam.

PHARMACOLOGICAL CLASSIFICATION:
A 2.6 Tranquillisers.

PHARMACOLOGICAL ACTION:
It has been found that the major locus of CNS depressant action of diazepam on spinal reflexes is the brain stem reticular system. After oral administration peak plasma concentrations are reached in 1 to four hours. Drug elimination follows a biphasic pattern, with a rapid phase (half-life = 2 to 3 hours) followed by a slow decay with a half-life 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. Diazepam is extensively bound to plasma proteins (99%).

INDICATIONS:
Diazepam is used in the treatment of anxiety in neurotic patients and for pre-operative 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 is only indicated when the disorder is severe, disabling or subjecting the individual to extreme stress.

CONTRA-INDICATIONS:
Diazepam is contra-indicated in infants and in patients with known hypersensitivity to diazepam. Pre-existing CNS depression or coma is normally a contra-indication. Caution should be observed when giving diazepam to patients with impaired hepatic or renal function. In elderly and debilitated patients and patients with impaired obstructive airways disease large doses may produce syncope. The effects of diazepam may be enhanced by alcohol, barbiturates, narcotics, MAO inhibitors and other depressants of the central nervous system. The response to treatment with oral anticoagulants may be variable in patients taking diazepam.
Avoid in porphyria as diazepam is considered unsafe although there is conflicting evidence of porphyrogenicity.
Use of diazepam in the first trimester of pregnancy has been associated with various congenital malformations in the infant and in the last trimester it has been associated with drowsiness, respiratory depression and intoxication in the new born infant. For these reasons diazepam is contra-indicated in pregnancy.
Diazepam is excreted in breast milk and is contra-indicated in nursing mothers because of the side-effects it can cause in the breastfed infant such as drowsiness, slow heartbeat and breathing problems.

WARNING:
This medicine may lead to drowsiness or impaired concentration, which may be aggravated by simultaneous intake of alcohol or other central nervous system depressant agents. Patients should not drive or operate machinery where loss of attention might be hazardous.
KEEP OUT OF REACH OF CHILDREN

DOSAGE AND DIRECTIONS FOR USE:
The usual dose for mild anxiety states in ambulant patients is 2 mg thrice daily and in severe anxiety and other psychiatric disorders 15 mg to 30 mg daily in divided doses.
For sleep disturbances 5 mg to 30 mg should be given in the evening. Elderly and debilitated patients with obstructive airways disease should be given one-half the usual adult dose.
Treatment should be as short as possible. The patient should be reassessed regularly and the need for continued treatment should be evaluated, especially in case the patient is symptom free. The overall duration of treatment generally should not be more than 8 –12 weeks, including a tapering off process.
In certain cases extension beyond the maximum treatment period may be necessary; if so, it should not take place without re-evaluation of the patients status.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
The side-effects most frequently encountered with diazepam are drowsiness, oversedation, dizziness, light-headedness; mental depression, fatigue, apathy, constipation, irritability. Less frequently gastro-intestinal disturbances such as diarrhoea, indigestion, changes in libido, tremor, visual disturbances such as blurred vision, urinary retention or incontinence, slurred speech or dysarthria, changes in salivation, depression of mood and affect, disorientation or confusion, lethargy and ataxia, jaundice and occasional blood disorders have been reported. The benzodiazepines can also cause amnesia. Paradoxical reactions such as acute hyperexcitable states with rage and hostility may occur. If these occur, the medicine should be discontinued.
Respiratory depression and hypotension are rare or absent at usual doses but may occasionally occur with high dosage. Large doses may produce syncope. Other side-effects occasionally reported are skin rashes, headaches, nausea and menstrual irregularities. Hepatic dysfunction has occasionally been reported. When diazepam is administered in obstetrics during labour, special care should be taken, since it may cause central respiratory depression and both hypothermia and hypotonia in the infant. It may also increase the foetal heart-rate.
Drowsiness is more common in elderly and debilitated patients and in patients receiving high doses. In severely disturbed patients treatment with diazepam may result in paradoxical reactions provoking excitement instead of sedation. If these occur, the medicine should be discontinued. There is a risk of dependence of the barbiturate - alcohol type and withdrawal reactions including convulsions have been observed in patients receiving large doses for prolonged periods when the drug was stopped abruptly.

Special Precautions:
Particular caution should be exercised with:
1. The elderly and debilitated patient - who are at particular risk of oversedation, respiratory depression and ataxia. (The initial oral dosage should be reduced in these patients).
2. Patients with pulmonary disease and limited pulmonary reserve.
3. Patients suffering from impairment of renal, hepatic or respiratory function.
4. Patients suffering from anxiety accompanied by an underlying depressive disorder.
5. Patients receiving barbiturates or other central nervous system depressants. There is an additive risk of central nervous system depression when these medicines are taken together.
6. Patients should be cautioned regarding the additive effect of alcohol.
7. Patients with myasthenia gravis on account of the pre-existing muscle weakness.
8. Patients with organic brain changes particularly arteriosclerosis.
Given during labour it crosses the placenta and may cause the floppy-infant syndrome characterised by central respiratory depression, hypothermia and poor sucking. Diazepam is not recommended for the primary treatment of psychotic illness. Diazepam should not be used alone to treat depression or anxiety with depression (suicide may be precipitated in such patients). Diazepam should be used with extreme caution in patients with history of alcohol or drug abuse.

Dependence
There is a potential for abuse and the development of physical and psychic dependence, especially with prolonged use and high doses. The risk of dependence is also greater in patients with a history of alcohol or drug abuse. Once physical dependence has developed, abrupt termination of treatment will be accompanied by withdrawal symptoms. These may consist of headaches, muscle pain, extreme anxiety, tension, restlessness, confusion and irritability.
In severe cases the following symptoms may occur: derealisation, depersonalisation, hyperacusis, numbness and tingling of extremities, hypersensitivity to light, noise and physical contact, hallucinations or epileptic seizures.

Rebound effects
A transient syndrome whereby the symptoms that led to treatment with diazepam recur in an enhanced form may occur on withdrawal of treatment. It may be accompanied by other reactions including mood changes, anxiety and restlessness. Since the risk of withdrawal phenomena/rebound phenomena is greater after abrupt discontinuation of treatment it is recommended that the dosage is decreased gradually.

Duration of treatment
The duration of treatment should be as short as possible (see Dosage), but should not exceed eight to twelve weeks in case of anxiety, including tapering off process. Extension beyond this period should not take place without re-evaluation of the situation. It may be useful to inform the patient when treatment is started that it will be of limited duration and to explain precisely how the dosage will be progressively decreased. Moreover it is important that the patient should be aware of the possibility of rebound phenomena, thereby minimising anxiety over such symptoms, should they occur while the product is being discontinued.

INTERACTIONS WITH OTHER MEDICINES:
Refer to contra-indications.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
The most prominent symptom of overdosage is sedation which usually follows symptoms of dizziness, fatigue, apathy or irritability. Large doses may produce syncope.
Manifestations of overdosage include somnolence, confusion, coma, respiratory and cardiovascular depression and hypotension.
The stomach should be emptied by aspiration and lavage, There is no specific treatment and recovery usually follows symptomatic and supportive therapy, with particular attention being paid to the maintenance of cardiovascular, respiratory and renal functions, and to the maintenance of electrolyte balance.

IDENTIFICATION:
2 MG: Pink, flat bevelled edge tablet, bisected and engraved "D1 " on the one side and with a Lennon logo (mortar and pestle) on the other side.
5 mg: Pale orange bisected tablets, engraved with the Lennon logo (mortar and pestle).
10 mg: Blue bisected tablets, engraved with the Lennon logo (mortar and pestle).

PRESENTATION:
2 MG: Securitainers of 30's and 500's.
5 mg: Blister packs of 30's and securitainers of 500's.
10 mg: Blister packs of 30's and securitainers of 500's.

STORAGE INSTRUCTIONS:
Store below 25°C, in well-closed containers.
Protect from light.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBERS:
2 MG:         J/2.6/257
5 mg:         J/2.6/267
10 mg:         J/2.6/250

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Pharmacare Limited
7 Fairclough Road
PORT ELIZABETH
6001

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
20 April 1977

                D190
        A & S PRINTERS

Updated on this site: May 2000
Current: September 2004
Source: Community Pharmacy

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