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Etaphylline


Composition:
Each 1 ml contains:
Acefylline Piperazine                   0.1 gm

Properties:
Acefylline is a theophylline derivative which is used as a bronchodilator similarly to theophylline. It relaxes smooth muscle, relieves  
bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear. However, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium.

Indications & Usage:
For the relief of bronchospasm in asthma, bronchitis & emphysema.
Contraindications:
This product is contraindicated in individuals who have shown hypersensitivity to its components. It is also contraindicated in patients with active peptic ulcer disease & in individuals with underlying seizure disorders (unless receiving appropriate anticonvulsant medication).


Side effects:
Etaphylline may cause nausea, vomiting, abdominal pain, diarrhea, gastro-intestinal bleeding, insomnia, headache, palpitations, tachycardia, hyperglycemia, hypotension, potentiation of diuresis, albuminuria and tachypnea, muscle twitching, and alopecia.
Drug interactions:
•    Toxic synergism of Etaphylline with ephedrine & with some other sympathomimetic bronchodilators may occur.
•    High dose of allopurinol, ciprofloxacin, clindamycin, erythromycin, clarithromycin, Troleandomycin, Norfloxacin, Propranolol, oral contraceptives, Cimetidine cause increased serum etaphylline levels.
•    Carbamazepine, phenobarbital, phenytoin & rifampicin cause decreased etaphylline levels.
•    Diazepam, Lorazepam and Midazolam increase CNS adenosine concentration, a potent CNS depressant, while Etaphylline blocks adenosine receptors.
•    Aminoglutethimide increases Etaphylline clearance.
•    Disulfiram, Estrogen, Methotrexate, Pentoxiphylline, Thiabendazole & Verapamil decrease Etaphylline clearance.
•    Etaphylline increases renal excretion of Lithium.
•    Sucralfate reduces absorption of Etaphylline


Warnings & Precautions:
•    Determination of serum etaphylline levels is recommended to assure maximal benefit without excessive risk. Serious side effects such as ventricular arrhythmias and convulsions may appear as the first sign of toxicity without any previous warning.
•    Morphine, curare & stilbamidine should be used with caution in patients with airflow obstruction because they stimulate histamine release & may also suppress respiration leading to respiratory failure.
Alternate drugs should be chosen whenever possible.
•    Halothane anesthesia in the presence of etaphylline may produce sinus tachycardia or ventricular arrhythmias.
•    Because dosages of these drugs are titrated to response, no additives should be made to etaphylline solution for injection.
•    It is advised not to exceed the recommended dose to avoid the occurance of complications in the nervous system especially in patients with impaired renal functions.
•    Caution should be taken in elderly and in neonates.
•    Etaphylline should be given with caution to patients with peptic ulceration, hyperthyroidism, hypertension, cardiac arrhythmias, other cardiovascular diseases or uncontrolled seizure disorders, hypoxemia, liver disease, Cor pulmonale as these conditions may be exacerbated.
•    Intravenous injections of etaphylline must be administered very slowly to prevent dangerous central nervous system & cardiovascular side effects resulting from the direct stimulant effect.
•    Dosage requirements of etaphylline vary widely between subjects, serum concentrations monitoring is necessary to ensure that concentrations are within the therapeutic range.

Pregnancy:
There are no adequate & well controlled studies in pregnant women.

Lactation:
- A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.  

Overdosage:
- Common clinical manifestations following overdosage include agitation, convulsions, hyperventilation, hypokalemia &metabolic acidosis.

Treatment of overdosage:
Hypokalemia should be corrected, convulsions should be controlled by intravenous administration of diazepam. Charcoal hemoperfusion or hemodialysis may be required.

Dosage & Administration:

Intramuscular or slow intravenous injection in doses of 500 mg.

Therapeutic category: Bronchodilator.

Legal category: Prescription only medicine.

Package: Box containing 6 ampoules, each contains 5 ml.

Storage: Store at a temperature below 30º C.

 

THIS IS A MEDICAMENT
Medicament is a product, which affects your health and its consumption contrary to instructions is dangerous for you. Follow strictly the doctor’s prescription, the method of use and the instructions of the pharmacist who sold the medicament.
- The doctor and the pharmacist are the experts in medicines, their benefits and risks.
- Do not by yourself interrupt the period of treatment prescribed.
- Do not repeat the same prescription without consulting your doctor.
- Keep all medicaments out of reach of children.

Council of Arab Health Ministers, Union of Arab Pharmacists.