BENZYLPENICILLIN BENZATINICA ®

BENZYLPENICILLIN BENZATINICA ® is a benzatin based benzylpenicillin drug

THERAPEUTIC GROUP: General antimicrobials for systemic use - broad-spectrum penicillins

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

Indications BENZYLPENICILLINE BENZATINICA ® Benzatin Benzylpenicillin

BENZYLPENICILLIN BENZATINICA ® is indicated for the treatment of penicillin-infectious diseases.

Thanks to the long duration of action, this medicine is particularly indicated in the treatment of rheumatic diseases due to Streptococcus and Lue.

Mechanism of action BENZYLPENICILLIN BENZATINICA ® Benzatinic benzylpenicillin

Benzatin benzylpenicillin is one of the most effective delay formulations of penicillin G, created to reduce the frequency of drug administration, often the cause of local adverse reactions and therapy interruptions.

Taken intramuscularly, the benzatinic benzylpenicillin accumulates at the injection site, being subsequently released gradually into the circulatory stream and thus allowing the realization of persistent blood concentrations.

Through the bond with plasma proteins and in particular with albumin, this active ingredient, converted into its active form benzylpenicillin, concentrates at the level of the various biological fluids, carrying out its own microbicidal therapeutic action through the inhibition of the formation of cross-linkages of peptidoglycan.

The lack of synthesis of these cross-linking seriously compromises the structural characteristics of the bacterial wall, thus making the micro-organism particularly susceptible to osmotic gradients and determining its death due to osmotic lysis.

After its activity the benzylpenicillin is mainly excreted in an active form through the urine.

Studies carried out and clinical efficacy

1. THERAPY WITH BENZYLPENICILLIN BENZATINIC AND SELECTION OF RESISTANT STRAINS

Arq Bras Cardiol. 2012 Apr 19.

Interesting work that demonstrates how the administration of benzatin benzylpenicillin for the prophylaxis of rheumatic fever may favor the proliferation and colonization of the oral cavity of penicillin-resistant streptococci, demonstrating how prolonged antibiotic therapy significantly affects the selection of resistant strains.

2 . RESISTANCE TO LACTAMIC BETA AND MICROBIAL PROLFERATION

BMC Microbiol. 2012 Apr 18; 12: 57.

Molecular study that seeks to characterize some of the mechanisms involved in antibiotic resistance. In this case, by studying the expression of PBP proteins in Listeria monocytogenes it was noticed how this protein, classically reputed as the main protagonist of betalactamasic activity, is actually necessary also to guarantee the control of cell division.

3. THE PENICILLINS: THE MOST ANTIBIOTIC DRUGS USED IN EUROPE

J Antimicrob Chemother. 2011 Dec; 66 Suppl 6: vi13-23.

Interesting epidemiological surveillance work that shows how penicillins still represent the main antibiotics used in clinical settings in all 33 participating European countries. These studies assume important meanings especially for the understanding of some biological phenomena such as the diffusion of resistant strains.

Method of use and dosage

BENZYLPENICILLIN BENZATINICA ®

Powder and solvent for solution for injection for intramuscular use at 600, 000 IU and 1, 200, 000 IU

Treatment with BENZYLPENICILLINE BENZATINICA ® should necessarily be supervised by your doctor both for the definition of the dosages and for the correct injection procedure.

The therapeutic schemes vary considerably according to the type of pathology, providing for usually shorter weekly administrations for venereal diseases such as syphilis, and monthly for pathologies such as rheumatic fever.

The administration of the drug must necessarily take place intramuscularly, therefore taking care to pay all the necessary precautions, also considering its chemical-physical nature which increases the risk of embolic pathologies following an accidental vascular injection.

Warnings BENZYLPENICILLIN BENZATINICA ® Benzatin Benzylpenicillin

Known the strong sensitizing power of benzylpenicillin, before starting the therapeutic treatment it would be appropriate to ascertain the absence of hypersensitivity to the drug or to chemically and functionally related active principles.

It is useful to remember that this drug is inactivated by beta-lactamases produced by some drug-resistant strains, thus being ineffective.

Elderly patients or those with kidney diseases should pay particular attention to the use of BENZYLPENICILLIN BENZATINICA ® due to the reduced renal clearance of the drug and the greater susceptibility to potential side effects.

All treatment should be supervised by your doctor in order to verify the effectiveness of the therapy and the absence of side effects.

BENZYLPENICILLIN BENZATINICA ® contains parahydroxybenzoates, excipients with a strong allergenic power.

PREGNANCY AND BREASTFEEDING

The potential toxic and sensitizing effects linked to the prolonged persistence of benzylpenicillin in the circulation make it possible to extend the aforementioned contraindications also to pregnancy and the subsequent period of breastfeeding.

Interactions

The therapeutic treatment with BENZYLPENICILLINE BENZATINICA ® could be compromised by the simultaneous use of:

Probenecid, able to increase the hepatic and renal toxicity of penicillin;
Drugs with bacteriostatic activity, known for the therapeutic effects of benzylpenicillin which occur mainly during the proliferative activity of microorganisms.

It is also useful to recall the lowering of the contraceptive power of oral contraceptives induced by the simultaneous administration of antibiotics.

Contraindications BENZYLPENICILLINE BENZATINICA ® Benzatin Benzylpenicillin

The use of BENZYLPENICILLIN BENZATINICA ® is contraindicated in patients who are hypersensitive to penicillins or their excipients and during pregnancy and lactation.

Undesirable effects - Side effects

The particular chemical-physical consistency of the drug and the need to administer the drug necessarily intramuscularly, could determine the appearance of serious local irritative manifestations following the consumption of BENZYLPENICILLINE BENZATINICA ®.

Furthermore, the lasting plasma concentrations that occur in these cases could increase the risk of hypersensitivity reactions in predisposed patients.

In addition to the aforementioned adverse reactions, the treatment with BENZYLPENICILLINE BENZATINICA ® could determine the appearance of:

Nausea, vomiting and diarrhea;
Tubular and glomerular damage accompanied by urinary anomalies and proteinuria;
Hemolytic anemia, neutropenia, leukopenia and myeloinhibition;
Hypertransaminasemia and hyperbilirubinemia;
Lethargy, spasms, convulsions and various neurological symptoms;
Angioedema, pruritus, urticaria, bronchospasm, hypotension and anaphylactic shock.