Tetralysal

Each capsule contains: Lymecycline (tetracycline base equivalent) 300 mg (Contains 408 mg Lymecycline equivalent to 300 mg Tetracycline base).

Antibacterial.
Pharmacology: Effects on acne: The exact mechanisms by which tetracyclines reduce lesions of acne vulgaris have not been fully elucidated; however, the effect appears to result in part from the antibacterial activity and anti-inflammatory activity of the drugs. Following oral administration, the drugs inhibit the growth of susceptible organisms (mainly Propionibacterium acnes) on the surface of the skin and reduce the concentration of free fatty acids in sebum. The reduction in free fatty acids in sebum may be an indirect result of the inhibition of lipase-producing organisms which convert triglycerides into free fatty acids or may be a direct result of interference with lipase production in these organisms. Free fatty acids are comedogenic and pro inflammatory and are believed to be a possible cause of inflammatory lesions, e.g. papules, pustules, nodules, cysts, of acne. However, other mechanisms also appear to be involved because clinical improvement of acne vulgaris with oral tetracycline therapy does not necessarily corresponds with a reduction in the bacterial flora of the skin or a decrease in the free fatty acid content of sebum.
Tetracyclines provide bacteriostatic action at the available plasma and tissue concentrations and rare effective against intracellular and extracellular organisms. Their mechanism of action is based on an inhibition of ribosomal protein synthesis. Tetracyclines block the access of the bacterial aminoacyl-tRNA to the mRNA-ribosome complex by binding to the 30S subunit of the ribosome, thus preventing the addition of amino acids to the growing peptide chain in protein synthesis. When given at therapeutically attainable concentrations their toxic effects is limited to the bacterial effects.
Pharmacokinetics: Absorption: Absorption is rapid, effective plasma levels are reached within the first hour following drug intake. The peak plasma level is reached within 3 to 4 hours after oral administration. Concurrent milk has not been shown to significantly modify the absorption of lymecycline.
Distribution: Oral administration of 300 mg, in the adult, gives rise to: a peak plasma level of 1.6 to 4 ug/mL, a highly variable residual concentration (0.29 to 2.19 ug/mL), a plasma half-life of approximately 10 hours.
Repeated administration results in a steady mean plasma concentration between 2.3 to 5.8 ug/mL. Wide intra- and extra-cellular diffusion, under normal dosage conditions, results in effective concentrations in most body tissue and fluids, and notable in the lungs, bones, muscles, liver, bladder, prostate, bile and urine.
Excretion/elimination: The product is principally excreted in urine and secondarily in the bile. About 65% of the administered dose are eliminated within 48 hours.

Lymecycline (Tetralysal) contains a broad spectrum antibiotic which is recommended for the treatment of infections due to micro-organisms sensitive to tetracyclines.
Lymecycline (Tetralysal) is also indicated in the treatment of acne.

The recommended dose for acne is 300 mg/day. The usual duration of treatment is 12 weeks.
The usual recommended dose for indications other than acne in adults is 600 mg/day.
Methods of administration: It should be taken with an adequate amount of fluids in order to reduce the risk of esophageal irritation and ulceration. (see PRECAUTIONS).

Acute overdosage is rare with antibiotics and there is no specific treatment. Should this happen gastric emptying should be considered. Supportive measures should be instituted as required and a high fluid intake maintained.

Hypersensitivity to the active substance or, to other tetracyclines or to any of the excipients.
Children under 8 years of age due to the risk of permanent dental staining and enamel hypoplasia.
Concurrent treatment with oral retinoids (see INTERACTIONS).

Solid dosage forms of tetracyclines may cause oesophageal irritation and ulceration. To avoid oesophageal irritation and ulceration, adequate fluids (water) should be taken with this medicinal product (see DOSAGE & ADMINISTRATION).
Caution should be exercised if the product is administered to patients with impaired renal or hepatic functions.
Overdosage of tetracyclines could result in hepatotoxicity.
High dosage of tetracyclines may be nephrotoxic.
Due to the risks of photosensitivity, it is recommended to avoid exposure to direct sunlight and ultraviolet light during treatment which should be discontinued if erythematous cutaneous manifestations occur.
The use of expired tetracyclines can lead to renal tubular acidosis (Pseudo-Fanconi syndrome) readily reversible when treatment is discontinued.
Treatment with Lymecycline (Tetralysal) should be discontinued if any evidence of raised intracranial pressure develops during treatment.
Prolonged use of broad-spectrum antibiotics may result in the appearance of resistant organisms and superinfection.
Tetracyclines in general can cause exacerbation of systemic lupus erythematosus.
Caution should be observed in the treatment of patients with myasthenia gravis who may be at risk of worsening of the condition.
Effects on the Ability to Drive and Use Machines: Not applicable.

Tetracyclines readily cross the placental barrier and are distributed into milk. Therefore, Lymecycline (Tetralysal) should not be administrated to pregnant or breast-feeding women (risk of enamel hypoplasia or dental dyschromia in the infant).

See table.

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*Manifestations of clinical symptoms, including visual disturbances, or headache, should prompt a possible diagnosis of intracranial hypertension. If increased intracranial pressure is suspected during treatment with lymecycline, administration should be immediately stopped. Benign intracranial hypertension has been reported with tetracyclines, with possible symptoms of headache, vomiting, visual disturbances including blurred vision, scotoma, diplopia or permanent loss of vision.
Some adverse effects are reported with tetracycline therapy in general: Dental dyschromia and/or enamel hypoplasia may occur if the product is administered in children younger than 8 years of age.
Haemolytic anaemia, eosinophilia and other hematologic disorders have been reported with tetracycline therapy.
Extra-renal hyperazotemia linked to an anti-anabolic effect which may be intensified by the association with diuretics has been reported with tetracycline therapy.
Systemic Lupus Erythematosus.
Pancreatitis.

Oral Retinoids and Vitamin A (above 10 000 IU/day): risk of intracranial hypertension.
Simultaneous administration of iron preparations and antacids, magnesium/aluminium and calcium hydroxides, oxides, salts and activated charcoal, cholestyramine, bismuth chelates and sucralfate may decrease cycline absorption. Medicinal products which increase gastric pH may reduce the absorption of tétracyclines. Enzyme inducers such as barbiturates, carbamazepine, phenytoin may accelerate the decomposition of tetracycline due to enzyme induction in the liver thereby decreasing its half-life. Consequently, a minimum 2-hour gap is necessary between the two treatments.
The effect of oral coumarin-type anticoagulants could be increased with an increased risk of haemorrhage.
Bacteriostatic medicinal products including Tetralysal may interfere with the bacteriocidal action of penicillin and beta-lactam antibiotics. Therefore, it is advisable that tetracycline-class drugs and penicillin should not be used in combination.
Laboratory tests interferences: Lymecycline could cause false-positive urine glucose determinations. It could also interfere with fluorometric determinations of urine catecholamines resulting in falsely increased values (Hingerty's method).
Tetracyclines and methoxyflurane, when used in combination, have been reported to result in fatal renal toxicity.
Didanosine: the digestive absorption of cyclines is decreased due to the increase in gastric pH (presence of an antacid in the didanosine tablet).
Some adverse effects have been reported with tetracycline therapy when used in combination with lithium; an interaction between lithium and the tetracycline class is a recognized interaction. Specifically, a combination of lymecycline with lithium may cause an increase in serum lithium levels.

Lymecycline (Tetralysal) 300 mg should be stored at a temperature not exceeding 25°C.

Tetracyclines / Acne Treatment Preparations

J01AA04 - lymecycline ; Belongs to the class of tetracyclines. Used in the systemic treatment of infections.

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