Lentocilin

The most common undesirable effects of benzylpenicillin are hypersensitivity reactions, especially skin rashes. Anaphylactic reactions occurred occasionally, which have sometimes been fatal. The overall incidence of allergic reactions to penicillin ranges between 1 and 10%. Anaphylactic reactions occur in approximately 0.05% of patients, usually after parenteral administration. The following undesirable effects were observed with benzylpenicillin: Blood and lymphatic system disorders - Eosinophilia and hemolytic anemia (both with immunological basis), leukopenia and thrombocytopenia. These effects are usually reversible after discontinuation of treatment. Immune system disorders - Hypersensitivity reactions to penicillin cause a wide variety of clinical syndromes. Immediate reactions include anaphylaxis, laryngeal edema, angioedema, urticaria and maculopapular rashes. Late reactions include hemolytic anemia and immune complex self-limited sickness-like reactions, characterized by fever, malaise, urticaria, arthralgia, myalgia, lymphadenopathy and splenomegaly. In order to determine which patients will probably develop severe allergic reactions, hypersensitivity skin tests may be used. Jarisch – Herxheimer reaction. Nervous system disorders - Benzylpenicillin is very irritating to the central and peripheral nervous systems. Neurotoxic reactions include anxiety, asthenia, cerebrovascular accident (CVA), confusion, dizziness, euphoria, nervousness, hallucinations, headache, neuropathy, neurovascular injury, localized or generalized seizures, coma, tremor and vasospasm at the administration site, and occur after parenteral administration of benzylpenicillin potassium. These reactions are most common when the benzylpenicillin is given daily in doses of more than 20,000,000 IU intravenously to renal impaired patients. The accidental injection of preparations of benzylpenicillin into or near by the nerves may produce neuromuscular damage, which rarely may be permanent. Rarely, inadvertent intravascular administration of benzathine benzylpenicillin or procaine benzylpenicillin, including direct administration into an artery - or adjacent to an artery - causes occlusion, thrombosis and severe neurovascular injury, especially in children. Deep injection in the glutes gluteal muscles can cause paralysis, dysfunction and painful irritation of the sciatic nerve. Repeated intramuscular injection of benzylpenicillin preparations in the anterolateral side of the thigh of newborns has rarely caused generalized muscular contractions, as well as atrophy and fibrosis of the quadriceps femoris muscle. After intramuscular administration of benzathine benzylpenicillin may occurs Hoigné syndrome may occur, characterized by agitation accompanied by symptoms such as fear of impending death and visual and auditory hallucinations. Transversal myelitis with permanent paralysis, gangrene requiring amputation of fingers and the more proximal regions of the extremities, and necrosis with formation of scars surrounding the site of injection, have occurred after injections in the buttocks, thighs and deltoid muscle. Eye disorders - Blurred vision, transient blindness. Cardiac disorders - Hypotension, palpitations, syncope, tachycardia, vasodilation and vasovagal syndrome characterized by anxiety, sweating, hypotension, peripheral arterial vasodilation and bradycardia. Cardiopulmonary arrest and death due to inadvertent IV administration. Respiratory, thoracic and mediastinal disorders - Apnea, dyspnea, hypoxia, pulmonary embolism and pulmonary hypertension. Gastro-intestinal disorders - Intestinal necrosis, melena, nausea, vomiting, and pseudomembranous colitis, which can arise during or after treatment. Hepatobiliary disorders - Transient increases in SGOT, hepatitis and cholestatic jaundice. Skin and subcutaneous tissue disorders - Diaphoresis, pruritus and urticaria. Musculo-skeletal, connective tissue and bone disorders - Arthritis, arthropathy, myoglobinuria, periostitis and rhabdomyolysis. Renal and urinary disorders - Hematuria, neurogenic bladder, renal impairment, proteinuria and increased serum BUN and creatinine. Reproductive system and breast disorders - Impotence and priapism General disorders and administration site conditions - Parenteral administration of benzylpenicillin preparations may cause dose-related injection site reactions dose-related and are the result of a direct toxic effect of the drug. IM administration of high doses of benzylpenicillin benzathine (in particular more than 600,000 IU of benzylpenicillin) in a single injection site can result in painful tumefaction and endothelial injury on site. IM administration of benzylpenicillin has been associated with the occurrence of the following side effects at the administration site: inflammation, pain, abscess, edema, hemorrhage, cellulitis, atrophy and cutaneous ulceration. It has also been reported cases of fever and fatigue associated with the use of benzylpenicillin.

Hypersensitivity to the active substance, to other penicillin or to any of the excipients. Hypersensitivity to lidocaine or local anesthetics of the amide type.

Lentocilin S suspension for injection is to be EXCLUSIVELY administered by DEEP INTRAMUSCULAR (IM) INJECTION. Deep IM administration of this medicine requires a rigorous technique and should be performed only by experienced health technicians and in places prepared for the emergency treatment of a possible anaphylactic reaction. Posology Adults Group A streptococcal infections - Upper respiratory tract infections: 1,200,000 IUunits in a single dose. Primary, secondary and early latent syphilis: 2,400,000 unitsIU in a single dose (injection at two different sites). Late latent syphilis or of unknown duration: 2,400,000 unitsIU (injection at two different sites) weekly for 3 consecutive weeks. Tertiary syphilis: 2,400,000 unitsIU (injection at two different sites) weekly for 3 consecutive weeks. Yaws, bejel and pinta: 1,200,000 unitsIU in a single dose. Prophylaxis of rheumatic fever: 1,200,000 unitsIU every 4 weeks. In high-risk patients it is recommended administration of 3 inevery 3 weeks. Prevention of diphtheria, including elimination of the asymptomatic carrier state: 1,200,000 unitsIU in a single dose. Newborns aged ≥ 1 month Asymptomatic congenital syphilis: 50,000 unitsIU/kg in a single dose (maximum dose: 2,400,000 unitsIU/dose). Benzathine benzylpenicillin is not recommended in newborns with proven or highly probable congenital syphilis. Children Group A Streptococcal infections - Upper respiratory tract infections: 25,000 - 50,000 unitsIU/kg in a single dose (maximum dose: 1,200,000 IUunits/dose) or weight < 27 kg: 300,000-600,000 IU units in a single dose weight ≥ 27 kg: 1,200,000 unitsIU in a single dose. - Primary, secondary and early latent syphilis: 50,000 unitsIU/kg (maximum dose: 2,400,000 unitsIU/dose) in a single dose. - Late latent syphilis or latent syphilis of unknown duration: 50,000 unitsIU/kg (maximum dose: 2,400,000 unitsIU/dose) weekly for 3 weeks. - Yaws, bejel and pinta: 300,000 unitsIU as a single dose in children aged less than 6 years or 1,200,000 IUunits in a single dose in children aged 6 years and older. -Prophylaxis of rheumatic fever: 25,000 - 50,000 unitsIU/kg in a single dose (maximum dose: 1,200,000 unitsIU/dose) or weight < 27 kg: 300,000 - 600,000 unitsIU in a single dose weight ≥ 27 kg: 1,200,000 unitsIU in a single dose. Prevention of diphtheria (including elimination of the asymptomatic carrier state): - children aged < 6 years (or weight < 30 kg): 600,000 unitsIU in a single dose - children aged ≥ 6 years (or weight ≥ 30 kg): 1,200,000 unitsIU in a single dose. Special populations Elderly - Dose adjustment is not necessary. However, since the elderly have a higher likelihood of decreased renal function, this must be taken into consideration during the selection of the posology and may be useful to monitor renal function. Renal insufficiency - Toxic concentrations of benzylpenicillin following administration of the usually recommended dose are not expected. Liver insufficiency - Dose adjustment is not necessary.

Bacteriostatic antibiotics: Bacteriostatic antibiotics, such as tetracycline, erythromycin and chloramphenicol, may antagonize the bactericidal effect of benzylpenicillin by interfering with active bacterial growth necessary to benzylpenicillin’s effect. Oral contraceptives: The efficacy of oral contraceptives may be impaired in case of concomitant therapy with benzylpenicillin, which may result in an unwanted pregnancy. Women taking oral contraceptives should be alerted to this situation and should be informed about the need to adopt alternative methods of contraception. Methotrexate: Penicillins may reduce the renal excretion of methotrexate causing a potential increase in its toxicity. Probenecid: Probenecid decreases the renal tubular secretion of benzylpenicillin. Its concomitant use with benzylpenicillin can prolong blood levels of benzylpenicillin. Probenecid may be used therapeutically for this purpose.

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Powder and diluent for suspension for injection: 1200000 units carton-vial

Lentocilin Penicillin G Benzathin PENICILLIN G BENZATHINE PENICILLIN G SOYBEAN LECITHIN POLYSORBATE 80 WATER LIDOCAINE HYDROCHLORIDE MONOSODIUM CITRATE

Lentocilin

Penicillin G Benzathin

84383-110

HUMAN PRESCRIPTION DRUG

INTRAMUSCULAR

indications&usage section