Sathrocin ES 400 mg Tablet
Pink, oblong film-coated tablet with characteristic markings containing Erythromycin Ethyl Succinate equivalent to Erythromycin 400 mg per tablet.
Erythromycin is a macrolide antibiotic with a broad and essentially bacteriostatic action against many Grampositive and to a lesser extent some Gram-negative bacteria, as well as other organisms including mycoplasma, spirochaetes, chlamydias, and rickettsias.
Erythromycin bind reversibly to the 50S subunit of the ribosome, resulting in blockage of the transpeptidation or translocation reactions, inhibition of protein synthesis, and hence inhibition of cell growth. Its action is predominantly bacteriostatic, but high concentrations are slowly bactericidal against the more sensitive strains. Because of the ready penetration of macrolides into white blood cells and macrophages there has been some interest in their potential synergy with host defense mechanisms
in vivo. Its actions are increased at moderately alkaline pH (up to about 8.5), particularly in Gram-negatives species, probably because of the improved cellular penetration of the nonionised form of the drug.
Erythromycin base is unstable in gastric acid, and absorption is therefore variable and unreliable. In consequence, the base is usually administered in film-or enteric-coated preparations, or one of the more acidstable salts or ester is employed.
Food may reduce the absorption of the base or the state, although this depends to some extent on the formulation, but the esters are generally more reliably and quickly absorbed and their absorption is little affected by food, obviating any need to take them before food. Peak plasma concentrations generally occur between 1 and 4 hours after administration.
Around 70 to 75% of the base is protein bound, but after administration as the estolate the propionate ester is stated to be about 95% protein bound. Erythromycin croses the placenta: foetal plasma concentrations are variously stated to be 5 to 20% of those in the mother. It is distributed into breast milk.
Erythromycin is widely distributed throughout body tissues and fluids, although it does not cross the blood brain barrier well and concentrations is CSF are low. It is excreted in high concentrations in the bile and 2 to 5% of an oral dose is excreted in the urine.
Erythromycin is used in the treatment of :
- Upper respiratory tract infections (tonsillitis, pharyngitis, sinusitis, secondary bacterial infections).
- Lower respiratory tract infections ( pneumonia, bronchitis, primary atypical pneumonia legionnaire's disease )
- Skin and soft tissue infections (furunculosis, erysipelas).
- Other infections - Diphtheria carriers and cases as an adjunct to antitoxin, syphilis and Gonorrhoea ( in cases of penicillin allergy ), subacute bacterial endocarditis, otitis media.
Erythromycin is contraindicated in the patients with a known hypersensitivity to erythromycin and its component and patients taking terfenadine. Concurrent use of astemizole and terfenadine with erythromycin is contraindicated. It may increase the risk of cardiotoxicity such as torsades de pointes and ventricular tachycardia, and death. Risk benefit should be considered for patients with impaired hepatic function.
Serious adverse effects are rare generally well tolerated. The most frequent side effects of oral erythromycin preparations are gastrointestinal disturbances and are dose-related. They include nausea, vomiting, abdominal discomfort and cramp, diarrhoea and anorexia. Suprainfection with resistant organisms may occur and pseudomembranous colitis has been reported after antibiotic treatment. There have been reports of hepatic dysfunction, with or without jaundice occurring in patients receiving oral erythromycin products.
Occasional case reports of cardiac arrhythmias, e.g. ventricular tachycardia have been documented in patients receiving erythromycin therapy. There have been isolated reports of other cardiovascular symptoms, e.g. chest pain, dizziness and palpitations; however, a cause and effect relationship has not been established.
There have also been reports of transient central nervous system side effects including confusion, hallucinations, seizures and vertigo; however, a cause and effect relationship has not been established.
Hearing loss is more likely to occur with administration of high doses (≥ 4 grams per day) in patients with renal or hepatic diseases and/or in elderly patients.
PRECAUTIONS / WARNING
Erythromycin and its derivative should be avoided in those known to be hypersensitive to it. Caution should be exercised in those with impaired hepatic function. Repeated courses of erythromycin for longer than 10 days increase the risk of hepatotoxicity. It has been suggested that erythromycin should be used with care in patients with a history of arrhythmias or prolonged QT interval.
During prolonged or repeated therapy, there is a possibility of overgrowth of non-susceptible bacteria or fungi and superinfection. If such infections occur, the drug should be discontinued and appropriate therapy instituted. The use of erythromycin can lead to the development of severe colitis as a result of colonization with C. difficile, a toxin producing organisms. In the patient who is unable to take erythromycin by mouth or in severely ill patients in whom it is necessary to attain an immediate high blood concentration, oral
erythromycin ethyl succinate is not an antibiotic of choice as erythromycin is given intravenously in the form of one of it's more soluble salts such as the gluceptate or the lactobionate.
Use in Pregnancy and Lactation:
Erythromycin crosses the placenta, resulting in low foetal plasma concentrations (5 to 20% of maternal plasma concentrations). Safety of erythromycin for use during pregnancy has not been established. Erythromycins are distributed into breast milk. However, problems in humans have not been documented.
Drug interactions of theophylline may be associated with an increase in serum theophylline levels and potential theophylline toxicity. In case of theophylline toxicity and/or elevated serum theophylline levels, the dose of theophylline should be reduced while the patient is receiving concomitant erythromycin therapy. Concomitant administration of erythromycin and digoxin has been reported to result in elevated digoxin serum levels.
There have been reports of increased anticoagulant effects when erythromycin and oral anticoagulants were used concomitantly. Increased anticoagulant effects due to this drug may be more pronounced in the elderly. Concurrent use of erythromycin and ergotamine or dihydroergotamine has been associated in some patients with acute ergot toxicity characterised by severe peripheral vasopasm and dysesthesia.
Erythromycin has been reported to decrease the clearance of triazolam and midazolam and thus may increase the pharmacologic effect of these benzodiazepines. Concurrently used with Lovastatin may increase the risk of rhabdomyolysis. Erythromycin may inhibit carbamazepine metabolism; it is recommended that erythromycin be used with caution if at all in patients receiving carbamazepine.
There have been reports that there is a rise in serum levels of cyclosporine phenytoin and hexobarbital (drugs metabolised by the cytochrome P450) during concomitant administration of erythromycin. Erythromycin may produce false elevations of urinary catecholamines because of interference with the fluorometric determination.