TETRALYSAL ® Limeciclina

TETRALYSAL ® is a drug based on limeciclina (Tetracycline L-methylenlisine)

THERAPEUTIC GROUP: General antimicrobials for systemic use - Tetracycline

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications TETRALYSAL ® Limeciclina

TETRALYSAL ® is indicated for the treatment of inflammatory and mixed acne of moderate and severe entity.

Mechanism of action TETRALYSAL ® Limeciclina

The limeciclina, active ingredient of TETRALYSAL ®, is a semisynthetic tetracycline belonging to the first generation tetracycline category, obtained by reacting the most common tetracycline with formaldehyde and lysine.

Originally extracted from yeasts belonging to the Streptomyces species, it was decided over time to optimize their efficacy and pharmacokinetic properties with the aid of chemical synthesis processes.

The wide spectrum of active action on Gram positive and negative, aerobic and anaerobic bacteria and generally also resistant to beta-lactam therapy is guaranteed by the characteristic mechanism of action capable of inhibiting the protein synthesis of the microorganism, binding the ribosomal subunit bacterial 30 S and thus preventing access to tRNA.

The particular therapeutic indication of the limecilina, oriented to the treatment of acne vulgaris, is justified by the ability of this active principle, following oral administration, to concentrate in the cutaneous region, inhibiting the proliferation of Proprionibacetrium Acnes in the sebaceous follicle, thus guaranteeing a reduction of the production of free fatty acids (products of the metabolism of these bacteria), partly responsible for the inflammatory and comedogenic lesions typical of acne.

After its therapeutic action, following a plasma half-life of about 10 hours, the limeciclina is eliminated mainly through the kidney, and in small part with the bile.

Studies carried out and clinical efficacy

1 LIMECICLINA IN THE PREVENTION OF PELVIC INFLAMMATORY DISEASES

Eur J Obstet Gynecol Reprod Biol. 1988 Jul; 28 (3): 241-7.

Outdated work, but innovative in its concepts, which demonstrated the efficacy of lemiccycline therapy in preventing pelvic inflammatory diseases in women with a past history of abortions. This action could be justified by the presence of microorganisms such as Chlamydia trachomatis, responsible for both abortions and inflammatory diseases.

2 . EFFECTIVENESS OF LIMECICLIN IN THE TREATMENT OF ACNE

Eur J Dermatol. 2003 Mar-Apr; 13 (2): 130-5.

Clinical trial conducted on 136 patients suffering from acne, which shows how the treatment with limeciclina for 12 weeks, can reduce inflammatory lesions by more than 60%, as done by the more expensive minocycline, without clinically relevant side effects.

3.TETRACICLINE AND ACNE: POSSIBLE EFFECT PLACEBO?

Int J Clin Pharmacol Ther. 2012 Mar; 50 (3): 157-61.

Very interesting study that re-evaluates the real mechanism of action of tetracyclines in the treatment of inflammatory and non-inflammatory acne. More precisely, the absence of dose-related effects could be indicative of a strong placebo effect, responsible for the therapeutic action.

Method of use and dosage

TETRALYSAL ®

Hard capsules for oral use 150 mg - 300 mg of Tetracycline L-methylenlisine (Limeciclina).

Different studies have shown that treating acne with tetracycline can be effective if performed at low dosages for prolonged periods of time.

For this reason the suggested dosage of TETRALYSAL ® is 300 mg of limeciclina per day for 12 weeks.

Warnings TETRALYSAL ® Limeciclina

The administration of TETRALYSAL ® should be preceded by a careful medical examination in order to assess the prescriptive appropriateness and to exclude the possible presence of conditions incompatible with antibiotic therapy.

Particular caution should be reserved for patients in pediatric and geriatric age, in addition to patients suffering from liver and kidney diseases, given the greater susceptibility to side effects.

Prolonged use of TETRALYSAL ® could lead to the spread of tetracycline resistant strains, some of which are responsible for even severe enterocolitis.

The use of tetracycline exposes the patient to the risk of burns, rashes and dermatological reactions due to the photosensitivity induced by the antibiotic.

PREGNANCY AND BREASTFEEDING

Given the possible side effects and the absence of studies able to fully characterize the safety profile of tetracyclines, it would be advisable to limit the use of these antibiotics during pregnancy and in the subsequent period of lactation to cases of real need and always under strict medical supervision.

Particular caution should also be reserved for pediatric patients given the ability of tetracyclines to cause alterations in dental pigmentation.

Interactions

In order to preserve the therapeutic characteristics and the pharmacokinetic properties of the limeciclina, it would be advisable to avoid the simultaneous administration of TETRALYSAL ® e:

Antacid preparations based on calcium, aluminum or magnesium, able to reduce the intestinal absorption of the antibiotic;
Oral anticoagulants, given the increased risk of bleeding;
Penicillins and beta-lactam antibiotics, able to interfere with the normal therapeutic properties of tetracyclines.

Contraindications TETRALYSAL ® Limeciclina

The use of TETRALYSAL ® is contraindicated in patients who are hypersensitive to tetracycline and its excipients.

Undesirable effects - Side effects

The tetracycline antibiotic treatment is not free from side effects that are sometimes relevant from the clinical point of view.

Gastrointestinal reactions such as nausea, vomiting, diarrhea and abdominal pain, haematological reactions such as anemia, thrombocytopenia, eosinophilia and allergic reactions with edema, urticaria, intense pruritus and edema, have been observed with high frequency in patients receiving tetracycline therapy.

Dental dyschromia and enamel hypoplasia were also rarely seen in pediatric patients, headache, dizziness, hyperazotemia and hypertransaminasemia.