OSPRONIM® INJECTION 30 mg/mL

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

OSPRONIM® INJECTION 30 mg/mL

SCHEDULING STATUS:
S6

PROPRIETARY NAME
(and dosage form):

OSPRONIM^® INJECTION 30 mg/mL

COMPOSITION:
Each 1 mL ampoule contains 30 mg pentazocine as lactate.

PHARMACOLOGICAL CLASSIFICATION:
A2.7 Narcotic Analgesics

PHARMACOLOGICAL ACTION:
The major effect of Ospronim^® (Pentazocine) is exerted on the CNS and smooth muscle. The CNS effects correspond to those of the opioids, namely analgesia, sedation and respiratory depression. The agonistic effects of Ospronim^® (Pentazocine) are presumably exerted at the k and d receptors. Ospronim^® (Pentazocine) also demonstrates a weak opioid antagonistic activity. Ospronim^® (Pentazocine) unlike other morphine-like opioids, causes an increase in blood pressure and heart rate, in high doses. In patients with coronary artery disease (intravenously administered) Ospronim^® (Pentazocine) elevates the mean aortic pressure, left ventricular enddiastolic and mean pulmonary artery pressures, resulting in an increase in cardiac work. This is probably because of the rise in catecholamine concentrations in the plasma. Low doses of Ospronim^® have the same effects on the gastro-intestinal tract as those of the opioids, with less elevation of biliary pressure than equianalgesic doses of morphine.
Ospronim^® (Pentazocine) is well absorbed from the gastrointestinal tract, subcutaneous and intramuscular sites. Peak values after intramuscular administration are reached after 15 to 60 minutes and the plasma half-life is 2 to 3 hours. Extensive metabolism in the liver and the individual variation in metabolism could account for variability of analgesic response.

INDICATIONS:
Post operative pain.
Chronic moderate to severe pain.

CONTRA-INDICATIONS:
Children under three years of age: Since clinical experience in children is limited, administration to children is not recommended.
Ospronim^® (Pentazocine) is contra-indicated in respiratory depression, especially in the presence of cyanosis and excessive bronchial secretions. It is also contra-indicated in acute alcoholism, after biliary operations, in heart failure due to chronic lung disease.
Ospronim^® (Pentazocine) should be given with caution to patients prone to seizures. In cases of liver disease or cirrhosis there is an enhanced availability and the dose should be decreased. May precipitate withdrawal symptoms in patients who have recently used narcotic analgesics. Ospronim^® (Pentazocine) should be used with care in patients with increased intracranial pressure and/or head injuries, or in patients with porphyria.

WARNINGS:
Ospronim^® (Pentazocine) may cause physical and psychological dependence. Patients with a history of dependence should be closely supervised. Withdrawal symptoms may occur, even in newborns after prolonged administration during pregnancy.
Because of the possibility of incompatibility it should not be mixed with diazepam, aminophyllin, chlordiazepoxide or soluble barbiturates.
Ospronim^® (Pentazocine) should be used with caution in shock, in reduced doses in elderly and debilitated patients, in hypothyroidism, adrenocortical insufficiency, impaired liver function and prostatic hypertrophy.

It should further be used with caution in patients with inflammatory bowel disorders, patients using monoamine-oxidase inhibitors or within 14 days of stopping such treatment. It should also be used with caution during labour, especially in women delivering premature infants, as Ospronim^® (Pentazocine) may cause respiratory depression in the new-born.

The use of this medicine may lead to drowsiness and impaired concentration which may be aggravated by simultaneous intake of alcohol or other central nervous system depressant agents. Patients should be warned against taking charge of vehicles or machinery or performing potentially hazardous tasks where loss of concentration may lead to accidents.

DOSAGE AND DIRECTIONS FOR USE:

Adults:	30 to 60 mg I.M. or S.C. every 3 to 4 hours, 30 mg I.V. Not more than 360 mg should be given daily to adults.
Children:	(6 to 12 years) 1 mg per kg body-mass I.M. or S.C. every 3 to 4 hours, 500 µg/kg body-mass I.V.

SIDE EFFECTS AND SPECIAL PRECAUTIONS:
The most common side-effects are sedation followed by sweating, dizziness and light-headedness. Nausea, vomiting, dry mouth, constipation, headache, flushing of the skin, disorientation, raised intracranial pressure, transient hypertension, mood changes, nightmares, anxiety, weird thoughts, hallucinations, paraesthesia, pruritus, biliary tract spasm and urinary retention have also been reported at doses above 60 mg. Marked respiratory depression with increased blood pressure and tachycardia may occur. Other side effects are changed uterine contractions, insomnia, vision disturbances, transient eosinophilia, chills and allergic reactions. Injection site should be varied as multiple doses may cause extensive fibrosis of subcutaneous and muscular tissue. Large intravenous doses may cause grand mal convulsions.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
See side effects and special precautions. Respiratory depression is antagonized by naloxone –400 µg given I.V., I.M. or S C. and repeated at intervals of 2 to 3 minutes if necessary. Assisted respiration may be necessary. Other treatment should be symptomatic and supportive.

IDENTIFICATION:
A clear colourless to pale straw coloured solution in 1 mL clear glass ampoules.

PRESENTATION:
Clear ampoules in containers of 10.

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

REGISTRATION NUMBER:
W/2.7/165

NAME AND BUSINESS ADDRESS OF APPLICANT:
INTRAMED (PTY) LTD
6 Gibaud Road
Korsten
PORT ELIZABETH
6001

DATE OF PUBLICATION OF THIS PACKAGE INSERT:

March 1989	12-290/6-94
	Tradepak PE