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

Logo TINSET 30 mg tablets.

SCHEDULING STATUS:
Schedule 2.

PROPRIETARY NAME
(and dosage form):

TINSET 30 mg tablets.

COMPOSITION
Each tablet contains
oxatomide 30 mg.

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

CONTRA-INDICATIONS
TINSET is contra-indicated in premature infants, neonates and patients with known hypersensitivity to any of the ingredients.
The safety of TINSET in pregnant or lactating women has not been established. TINSET 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 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
Adults
: 1 tablet (30 mg) twice daily (morning and evening).

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 inco-ordination.
Other side-effects include gastro-intestinal disturbances such as nausea, vomiting, diarrhoea, or constipation, and epigastric pain. TINSET 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 may cause allergic reactions such as rash urticaria, angioedema and less frequently anaphylactoid reactions may occur.
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 include convulsions, transaminase elevations and hepatitis. Exceptional cases of Stevens-Johnson, toxic epidermal necrolysis and erythema multiforme have been reported.
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 is not suited for prompt relief of allergic conditions such as asthma attacks. When TINSET 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 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 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 may enhance the sedative effect of central nervous system depressants including alcohol, barbiturates, hypnotics, narcotic analgesics, sedatives, tranquillizers and anti-epileptics, e.g. carbamazepine.
The side-effects of anticholinergic drugs such as atropine and tricyclic antidepressants may be enhanced by the concomitant administration of TINSET.
TINSET 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.

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 close 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
White circular, slightly arched biconvex tablets, 9 mm in diameter, inscribed "ox" above "30" on one side and "JANSSEN" on the other side.

PRESENTATION
Cartons containing one or more blister packs, each containing 10 tablets.

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

REGISTRATION NUMBER
Q/5.71/35

NAME AND BUSINESS ADDRESS OF THE APPLICANT
JANSSEN - CILAG
Janssen Pharmaceutica (Pty) Ltd.,
(Reg. No.1980/011122/07)
15th Road, HALFWAY HOUSE, 1685

DATE OF PUBLICATION OF THIS PACKAGE INSERT
05 June 2001
        Code No.: 024178
        2002B

Updated on this site: December 2002
Source: Pharmaceutical Industry

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