INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION
TINSET PED® suspension

SCHEDULING STATUS:
Schedule 2.

PROPRIETARY NAME
(and dosage form):

TINSET PED^® suspension

COMPOSITION
Each mL contains oxatomide monohydrate 2,6 mg equivalent to oxatomide 2,5 mg. Preservatives: Methylparaben 0,18% m/v; propylparaben 0,02% m/v.

PHARMACOLOGICAL CLASSIFICATION
A.5.7.1 Medicines affecting autonomic functions. Antihistaminics.

PHARMACOLOGICAL ACTION
Pharmacodynamics:
Oxatomide inhibits allergic and other hypersensitivity reactions by decreasing the release and effects of various mediators. Blockade or attenuation of receptor-mediated effects is known for histamine (H₁), serotonin (5-HT₂), leukotrienes (LTC₃, LTC₄) and platelet aggregation factor (PAF). The onset and intensity of allergic reactions is further shifted by oxatomide as a result of a decreased mediator release. Mast cells, which produce and store the allergic mediators, secrete them following mobilization of calcium. This process is inhibited by oxatomide.
Pharmacokinetics:
The absorption of oxatomide from the gastro-intestinal tract is virtually complete in humans. Peak blood concentrations are reached within 2 hours. Oxatomide is metabolised in the liver through aromatic hydroxylation, oxidative N-dealkylation and conjugation. Less than 0,5 % of the dose is excreted unchanged. Excretion of metabolites is mainly via the faeces (60%), especially from the bile and also via the urine.
Oxatomide, which has a half-life of 14 hours, reaches steady-state plasma levels (about 35 ng/mL with a twice daily dose of 30 mg) after 3 days. The plasma protein binding amounts to 98%.

INDICATIONS
TINSET PED is indicated in the symptomatic treatment of allergic rhinitis and chronic urticaria.
TINSET PED relieves the classical nasal and ocular symptoms associated with hay-fever.
In cases of chronic urticaria TINSET PED reduces the severity of the erythema, and pruritus.

CONTRA-INDICATIONS
TINSET PED is contra-indicated in premature infants, neonates and patients with known hypersensitivity to any of the ingredients.
The safety of TINSET PED in pregnant or lactating women has not been established. TINSET PED should not be administered to pregnant or lactating women.

WARNINGS
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.
In infants and children, TINSET PED may act as a cerebral stimulant and symptoms may include convulsions and hyperpyrexia.
Oxatomide is not recommended in the treatment of acute asthma.

DOSAGE AND DIRECTIONS FOR USE
Children:
Initial dose: 0,2 mL (0,5 mg) per kilogram bodyweight twice daily.
Optimal dose range: 0,2 mL (0,5 mg) to 0,4 mL (1 mg) per kilogram bodyweight twice daily.
Directions for use of the pipette in children:

NOTE:

The pipette must not be used for administration of any other medicine. The pipette is specifically calibrated for administration of TINSET PED.

Fig 1: The bottle comes with a child-proof cap, and should be opened as follows:

–	Push the plastic screw cap down while turning it counter clockwise
–	Remove the unscrewed cap.

Fig. 2: Pull the pipette out of its case and insert it into the bottle.
Fig. 3: While holding down the bottom ring, pull the top ring up to the mark corresponding to the child's weight in kilograms.
Fig. 4: Holding the bottom ring, remove the entire pipette from the bottle.
Empty the pipette and fit it back into its case.
Close the bottle.
{illustrated here}

SIDE-EFFECTS AND SPECIAL PRECAUTIONS
Side-effects:
Sedation, varying from slight drowsiness to deep sleep and including inability to concentrate, lassitude, dizziness, hypotension, muscular weakness, and incoordination.
Other side-effects include gastro-intestinal disturbances such as nausea, vomiting, diarrhoea or constipation, and epigastric pain. TINSET PED may produce headache, blurred vision, tinnitus, elation or depression, irritability, nightmares, anorexia, difficulty in micturition, dryness of the mouth, tightness of the chest, dysuria and tingling, heaviness and weakness of the hands.
In babies and young children, dyskinetic neurological reactions have been observed. Epileptiform seizures in patients with focal lesions of the cerebral cortex may be precipitated.
Administration of TINSET PED may cause allergic reactions such as rash, urticaria, angioedema and less frequently anaphylactoid reactions.
Blood disorders, including agranulocytosis and haemolytic anaemia have been reported.
Increased appetite and mass gain have been reported.
Reports from post marketing experience with TINSET PED include convulsions, transaminase elevations and hepatitis.
Precautions:
Caution is recommended in children under six years because of the risk of overdosage phenomena due to increased distribution to the central nervous system.
TINSET PED is not suited for prompt relief of allergic conditions such as asthma attacks. When TINSET PED is prescribed to asthma patients, the existing treatment regimen must not be interrupted abruptly, but its dosage gradually reduced. This is particularly important in patients under corticosteroid treatment.
Because of its hepatic elimination, TINSET PED should be administered carefully to patients who have a liver disorder. If required, the treatment in such patients should preferably start with half the normal dose; the dosing interval may be maintained.
Since TINSET PED has anticholinergic properties, it should be used with care in conditions liable to be exacerbated or otherwise adversely affected by atropine, such as glaucoma and prostatic hypertrophy.
Elderly patients are more susceptible to central nervous system depressant and hypotensive effects.
Interactions:
Patients are warned that TINSET PED may enhance the sedative effect of central nervous system depressants including alcohol, barbiturates, hypnotics, narcotic analgesics, sedatives, and tranquillizers.
The side-effects of anticholinergic drugs such as atropine and tricyclic antidepressants may be enhanced by the concomitant administration of TINSET PED.
TINSET PED may mask warning symptoms of damage caused by ototoxic drugs such as the aminoglycoside antibiotics.
Monoamine oxidase inhibitors may enhance the antimuscarinic effect of TINSET PED.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
Symptoms:
The most commonly reported symptoms after dosing are somnolence, stupor and extrapyramidal symptoms such as dyskinesia, torticollis, oculogyria, dystonia and hypertonia. Hyperexcitability and agitation are less common. Mydriasis, tachycardia as well as bradycardia and generalised muscle spasms have more rarely been reported. Signs of central nervous system stimulation like excitement, hallucinations, muscle tremors, ataxia and convulsions are prominent in infants and children whilst a dry mouth, flushed face, mydriasis and, hyperpyrexia are also not uncommon. Coma and cardiorespiratory collapse tend to be terminal events.
Treatment:
Treatment consists of dose observation of vital signs, administration of activated charcoal and/or gastric lavage, and supportive measures. Extrapyramidal symptoms have been successfully treated with anticholinergic agents. There is no specific antidote.

IDENTIFICATION
Off-White to grey homogenous liquid.

PRESENTATION
Amber glass bottles containing 100 mL of dilute suspension, supplied with a graduated pipette.

STORAGE INSTRUCTIONS
Store below 25°C.
Protect from light.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER
Y/5.7.1/345

NAME AND BUSINESS ADDRESS OF THE APPLICANT
JANSSEN –CILAG
Janssen Pharmaceuticals (Pty) Ltd.
(Reg. No. 80/11122/07)
15th Road, Halfway House, 1685

DATE OF PUBLICATION OF THIS PACKAGE INSERT
4 June 1992

                Code No.: 023196
                        99E
® TRADEMARK
Britepak

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