INAPSIN® injection

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

INAPSIN® injection

SCHEDULING STATUS:
Schedule 5

PROPRIETARY NAME
(and dosage form) :

INAPSIN^® injection

COMPOSITION :
Each mL contains 2,5 mg of the active ingredient, droperidol.

PHARMACOLOGICAL CLASSIFICATION:
A.2.6.5. Central nervous system depressants. Miscellaneous structures.

PHARMACOLOGICAL ACTION :
Inapsin is a neuroleptic agent producing marked tranquillization and sedation. It reduces anxiety and provides a state of mental detachment and indifference while allowing the patient to respond to verbal commands.

Inapsin lowers the incidence of nausea and vomiting. Inapsin produces mild alpha-adrenergic blockade, peripheral vascular dilatation and reduction of the pressor effect of epinephrine. It can produce hypotension and decreased peripheral vascular resistance. It may decrease pulmonary arterial pressure.

The onset of action of single intramuscular and intravenous doses is from three to ten minutes following administration, although the peak effect may not be apparent for up to 30 minutes.

Tranquillizing and sedative activity diminish within two to four hours, although alteration of alertness may persist for up to twelve hours.

INDICATIONS:
Inapsin is indicated:

a)	for premedication and as an adjunct during induction and in the maintenance of general and regional anaesthesia;
b)	in neuroleptanalgesia in which Inapsin injection is given concurrently with a narcotic analgesic, to aid in producing tranquillity and decreasing anxiety;
c)	to produce tranquillization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures;
d)	as an anti-emetic for nausea and vomiting associated with cancer chemotherapy;
e)	as a tranquillizer in psychiatry in the treatment of excitation, agitation, aggressive tension, anxiety, turbulence and manic states.

CONTRA-INDICATIONS:
Inapsin is contra-indicated in severely depressed patients and in patients with a known intolerance to the drug.

WARNINGS:
Since Inapsin is metabolised in the liver, care should be taken in patients with hepatic disease. Minor central effects can, in some cases, persist for up to 48 hours after administration of Inapsin and when early discharge is envisaged the patient should be advised not to drive a car or operate machinery on the day following intravenous or intramuscular administration. Inapsin can increase the central nervous system depression produced by other CNS-depressant drugs, and respiratory depression may occur, especially when used with opiates. Inapsin may antagonise the action of adrenaline and other sympathomimetic agents.

DOSAGE AND DIRECTIONS FOR USE:
Inapsin can be administered to both adults and children. The following dosage regimen is recommended:

Children’s Dosage
For children 2 to 12 years 1,0 to 1,5 mg (0,4 - 0,6 mL) per 10 kg body mass is recommended for premedication or for induction of anaesthesia.

Adult Dosage
Psychoses: Severe agitation or aggression: 2,5 to 12,5 mg usually intramuscularly.

Premedication: To allay anxiety and calm the patient in preparation for operation 2,5 to 10,0 mg (1,0 to 4,0 mL) may be administered intramuscularly or intravenously 30 to 60 minutes pre-operatively. The doses should be adjusted according to the age and physical status of the patients.

Induction: To help provide smooth induction 2,5 mg (1,0 mL) per 10 kg body mass may be given (usually intravenously) along with an analgesic and/or general anaesthetic.

Maintenance: To help maintain the desired plane of anaesthesia, to provide smooth emergence and to help reduce the incidence of post-operative nausea and vomiting, additional 1,25 to 2,5 mg (0,5 to 1,0 mL) doses may be administered (usually intravenously).

Use without a general anaesthetic in diagnostic procedures: Administer the usual I.M. premedication 2,5 to 10 mg (1 to 4 mL) 30 to 60 minutes before the procedure. Additional 1,25 to 2,5 mg (0,5 to 1 mL) amounts of Inapsin may be administered, usually intravenously.

Note
When Inapsin is used in certain procedures, such as bronchoscopy appropriate topical anaesthesia is still necessary.

Adjunct to regional anaesthesia 2,5 to 5 mg (1 to 2 mL) may be administered intramuscularly or slowly intravenously when additional sedation is required.

As an agent for chemotherapy-induced nausea and vomiting 1 to 10 mg usually intravenously 30 to 60 minutes prior to chemotherapy, followed by 1,0 to 2,5 mg per hour for up to six hours. Inapsin may be used in combination with high-dose steroids for chemotherapy-induced nausea and vomiting.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects that have been reported are dizziness, chills and shivering, laryngospasm, bronchospasm and hallucinatory episodes (sometimes associated with transient periods of mental depression), extra pyramidal side-effects.
Safety in pregnancy has not been established.
Inapsin is not recommended for breast feeding women.
Gastro-intestinal symptoms, nausea, vomiting, loss of appetite, photosensitive skin reactions, tardive dyskinesia, hyperprolactinaemia, galactorrhoea, gynaecomastia, oligomenorrhoea and amenorrhoea may occur. Pain has been reported at the site of injection.
Severe dystonic reactions have followed the use of Inapsin; it should therefore be used with extreme care in susceptible patients, such as children, adolescents and the elderly. Neurotoxic reactions may occur in patients with hyperthyroidism.
Inapsin must be used with extreme caution in patients receiving lithium.
Inapsin injections must be administered in reduced dosage (as low as 1/2 the dosage usually recommended) when other central nervous depressants are prescribed concomitantly to avoid the possibility of potentiation.
Since droperidol is capable of blocking the response to pressor amines, the potential exists for the precipitation of severe hypotension in the immediate post-operative period. If fluid therapy does not correct the hypotension the administration of pressor agents other than adrenaline should be considered. Inapsin injection should be used with caution in patients with liver and kidney dysfunction.
Inapsin may impair the anti-Parkinson effects of levodopa. The dosage of anti-convulsants may need to be increased to take account of the lowered seizure threshold.
Enhanced CNS-effects when combined with methyldopa, have been reported for Inapsin.
Acute withdrawal symptoms, including nausea, vomiting and insomnia, have been described after abrupt cessation of high doses of Inapsin. Relapse may also occur and gradual withdrawal is advisable.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
The therapeutic ratio of Inapsin is high and in the event of overdose, treatment of possible extrapyramidal effects with anti-Parkinson drugs is usually all that will be required.

Injection overdosage
In the presence of apnoea, a patent airway may be maintained through the use of an oropharyngeal airway or endotracheal tube. Oxygen should then be administered and respiration should be assisted. The patient should be carefully observed during the first 24 hours. Body warmth and adequate fluid intake should be maintained. Hypotension and/or shock may be counteracted by use of fluids and vasopressor drugs (other than adrenaline) if necessary.

CONDITIONS OF REGISTRATION:
Advertising to the professions only.

IDENTIFICATION:
A clear, colourless solution in 2 mL glass ampoules.

PRESENTATION:
Inapsin injection 2 mL (2,5 mg/mL) is supplied in 2 mL clear glass ampoules packed in boxes of 5 and 30 ampoules.

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

REGISTRATION NUMBER:
B/2.6.5/1012.

NAME AND BUSINESS ADDRESS OF APPLICANT:
JANSSEN
PHARMACEUTICA
Janssen Pharmaceutica (Pty) Ltd. (Reg. No. 80/11122/07)
15th Road, Halfway House, 1685
© JANSSEN PHARMACEUTICA (Pty) Ltd.
SOUTH AFRICA

DATE OF PUBLICATION:

29 April 1987

® Trademark

Code No.: 020925
95D