PELINOL Tablet

For patients who experience side effects with maximal therapeutic doses of either theophylline or salbutamol alone and patients with severe asthma who require more than one drug from any class of bronchodilators.

For oral administration.

The usual starting dose is 1 tablet of PELINOL thrice daily.

Hypersensitivity to xanthine derivatives.

In patients with active peptic ulcer disease, and in individuals with underlying seizure disorders (unless receiving appropriate anti-convulsant medication).

Pre-existing cardiac tachyarrhythmias, and in patients with known hypersensitivity to salbutamol. Although intravenous salbutamol and, occasionally, salbutamol tablets are used in the management of premature labour, they are contraindicated in antepartum haemorrhage or toxaemia of pregnancy.

Immediate hypersensitivity reactions may occur after administration of salbutamol, as demonstrated by rare cases of urticaria, angio-oedema, rash, bronchospasm, and oropharyngeal oedema.

Theophylline

Side effects associated with theophylline are generally mild when peak serum theophylline concentrations are <20ncg/mL and mainly consists of transient caffeine- like adverse effects such as nausea, vomiting, headache, restlessness, and insomnia.

Above 20mcg/mL, side effects such as vomiting, cardiac arrhythmias, and intractable seizures have been reported.

Salbutamol

The adverse reactions to salbutamol are similar in nature to reactions to other sympathomimetic agents. The most frequent adverse reactions to salbutamol are nervousness, tremor, headache, tachycardia, and palpitations. Less frequent adverse reactions are muscle cramps, insomnia, nausea, weakness, dizziness, drowsiness, flushing, restlessness, irritability, chest discomfort, and difficulty in micturition.

Rare cases of urticaria, angio-oedema, rash, bronchospasm, and oropharyngeal oedema have been reported after the use of salbutamol. In addition, salbutamol, like other sympathomimetic agents, can cause adverse reactions such as hypertension, angina, vomiting, vertigo, central nervous system stimulation, unusual taste, and drying or irritation of the oropharynx.

Sympathomimetic agents: Concomitant use is not recommended since such use may lead to deleterious cardiovascular effects.

Monoamine oxidase inhibitors: Salbutamol should be used with caution in patients being treated with these drugs, since the action of salbutamol in the vascular system may be potentiated.

Beta-blockers and salbutamol inhibit the effect of each other. Propranolol increases serum theophylline levels.

Cimetidine, erythromycin, oral contraceptive steroids, and ciprofloxacin increase serum theophylline levels.

Carbamazepine, phenobarbital and rifampin decrease levels of theophylline.

Pregnancy

There are no adequate and well-controlled studies in pregnant women. It is not known whether theophylline can cause foetal harm when administered to pregnant women. PELINOL should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus.

Lactation

It is not known whether salbutamol & theophylline is excreted in human milk. Because of the potential for tumorigenicity shown for salbutamol in animal studies, a decision should be made whether to discontinue lactation or to discontinue the drug, taking into account the importance of the drug to the mother.

Theophylline is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing infants. Serious adverse effects in the infant are unlikely unless the mother has toxic serum theophylline concentrations.

In patients with coronary artery disease, congestive heart failure, hypertension, hyperthyroidism and diabetes.

Frequent clinical cardiac monitoring may be required when treating patients of ischaemic heart disease with myocardial irritability, in presence of hypoxia and electrolyte imbalances, and in patients with congestive cardiac failure and hypertension, who are on routine potassium depleting diuretics.

Care should be exercised in patients requiring additional parenteral therapy with theophylline (intravenous aminophylline injection/infusion) so as to maintain serum theophylline levels between 10-20mcg/mL with frequent therapeutic drug monitoring, if available, or clinical monitoring.

Due to the theophylline component, caution must be exercised in patients with peptic ulcer, as centrally mediated gastrointestinal effects may be associated with serum levels of theophylline over 20mcg/mL. This is, however, unlikely occur with the recommended dosage.

Elderly patients with serum concentrations above 20mcg/mL are more likely to experience serious side effects such as ventricular arrhythmias or convulsions than are younger patients. Less serious signs of theophylline toxicity (i.e., nausea and restlessness) may occur frequently when initiating therapy, but are usually transient.

Theophylline

Theophylline is a bronchodilator, structurally classified as a methylxanthine. Theophylline has two distinct actions in the airways of patients with reversible obstruction; smooth muscle relaxation and suppression of the response of the airways to stimuli. Theophylline also increases the force of contraction of the diaphragmatic muscles.

Salbutamol

Salbutamol is a selective Beta-2-adreneric agonist administered for the symptomatic relief of bronchospasm associated with chronic or acute asthma, bronchitis or other obstructive pulmonary diseases. Because of its relative specificity for beta-2 receptors, salbutamol relaxes smooth muscle of the bronchi, uterus and vascular supply to the skeletal muscle, but generally has much less stimulant action on the heart than does isoproterenol which has powerful action on all beta receptors.