TRADE NAME: ETAPHYLLINE AMPOULE GENERIC NAME: Acephylline piperazine COMPOSITION: Each 5 ml contain: Active ingredient: Acephylline piperazine 0.5 mg : water Excipients PHARMACEUTICAL FORM: Solution for injection PHARMACOLOGICAL ACTION: 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: For the relief of bronchospasm in asthma ,bronchitis & emphysema . DOSAGE AND ADMINISTRATION: Intramuscular or slow intravenous injection. Dose: as doctor prescribed. 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, cardiovascular diseases & in individuals with underlying seizure disorders (unless receiving appropriate anticonvulsant medication ). UNDESIRABLE 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. Convulsions, cardiac arrhythmias, and hypotension may follow intravenous injection, particulary if the injection is too rapid, and sudden deaths have been reported. The drug is too irritant for intramuscular use. Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via sending e-mail to pv@memphis.com.eg INTERACTION WITH OTHER MEDICINAL PRODUCTS AND OTHER FORMS OF INTERACTION: • 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.
