Extencilline (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Aventis Laboratories (France)

Manufactured By

Sandoz, GmbH (Austria)

ATC Code

J01CE08 (Benzathine benzylpenicillin)

Active Substance

Benzathine benzylpenicillin (Rec.INN registered by WHO)

Dosage Forms

	Extencilline	Lyophilized powder for the preparation of an injection solution 1.2 million IU: vial 50 pcs.
		Lyophilized powder for the preparation of an injection solution 2.4 million IU: vial 50 pcs.
		Lyophilized powder for the preparation of an injection solution 600 thousand IU: vial 50 pcs.

Dosage Form, Packaging, and Composition

Lyophilized powder for the preparation of an injection solution from white to cream color.

Excipients: sodium carboxymethylcellulose, sodium citrate, povidone.

Glass vials with a volume of 5 ml (50) – cardboard boxes.

Lyophilized powder for the preparation of an injection solution from white to cream color.

Excipients: sodium carboxymethylcellulose, sodium citrate, povidone.

Glass vials with a volume of 5 ml (50) – cardboard boxes.

Lyophilized powder for the preparation of an injection solution from white to cream color.

Excipients: sodium carboxymethylcellulose, sodium citrate, povidone.

Glass vials with a volume of 15 ml (50) – cardboard boxes.

Clinical-Pharmacological Group

Penicillin antibiotic, destroyed by penicillinase

Pharmacotherapeutic Group

Antibiotic, penicillin

Pharmacological Action

Benzathine benzylpenicillin is a beta-lactam antibiotic from the group of long-acting type G penicillins. It has a bactericidal effect on susceptible microorganisms by inhibiting the synthesis of mucopeptides of the cell wall.

It is effective against Streptococcus pyogenes A and Treponema pallidum, which cause syphilis and yaws.

Pharmacokinetics

Distribution

After intramuscular injection, Benzathine benzylpenicillin is hydrolyzed very slowly, releasing benzylpenicillin. C_max in blood serum is reached 12-24 hours after injection. The long T_1/2 provides a stable and prolonged concentration of the drug in the blood: on the 14th day after administration of 2.4 million IU of the drug, the concentration in serum is 0.12 µg/ml; on the 21st day after administration of 1.2 million IU of the drug, its concentration is 0.06 µg/ml in 89-97.4% of patients (1 IU = 0.6 µg). Diffusion of the drug into fluids is complete, diffusion into tissues is very weak. Plasma protein binding is 40-60%.

Biotransformation

Biotransformation of the drug is insignificant.

Elimination

It is excreted mainly by the kidneys. Extencilline crosses the placental barrier and is excreted in breast milk.

Indications

Treatment of infections caused by bacteria susceptible to the drug, including

• Prevention of exacerbation of articular rheumatism;
• Treatment of syphilis and other diseases caused by treponemes (yaws, pinta).

ICD codes

Dosage Regimen

Prevention of relapses of articular rheumatism 1 intramuscular injection every 15 days

• adults – 2.4 million IU;
• children (depending on age) – 0.6 million IU – 1.2 million IU

Treatment of syphilis 1 intramuscular injection every 8 days

• adults – 2.4 million IU.

Treatment of yaws and pinta (endemic treponematoses) Single intramuscular injection

• adults – 1.2 – 2.4 million IU;
• children (with body weight up to 45 kg) – 0.6 million IU – 1.2 million IU.

The drug is administered only deep intramuscularly. The drug must not be administered intravenously!

Under aseptic conditions, prepare the solution by introducing into the vial

• 2 ml of water for injections for 0.6 million IU,
• 4 ml of water for injections for 1.2 million IU,
• 8 ml of water for injections for 2.4 million IU.

Mix thoroughly before use by rolling the vial between the palms of the hands, trying to avoid the formation of abundant foam.

Benzathine benzylpenicillin in the form of a prepared suspension can be stored in the refrigerator for no more than 24 hours.

Adverse Reactions

Allergic reactions: urticaria, fever, eosinophilia, multiforme erythema, exfoliative dermatitis, angioedema, difficulty breathing, in exceptional cases – anaphylactic shock.

From the digestive system: nausea, vomiting, diarrhea, candidiasis. Isolated cases of pseudomembranous colitis have been described with the use of the drug.

Other side effects of immunoallergic nature have been reported less frequently: moderate transient increase in serum transaminase levels; reversible anemia, leukopenia, thrombocytopenia; acute interstitial nephritis.

The use of high doses of beta-lactam antibiotics, especially in renal failure, can cause the development of encephalopathy (impaired consciousness, motor disorders, convulsions).

In children, the development of local reactions to the administration of the drug is possible.

Contraindications

• Allergy to beta-lactam antibiotics (penicillins and cephalosporins).

The possibility of cross-allergy with cephalosporins should also be considered.

Use in Pregnancy and Lactation

Extencilline crosses the placental barrier and is excreted in breast milk.

Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

It is recommended to discontinue breastfeeding if it is necessary to prescribe the drug.

Use in Renal Impairment

In renal failure, doses are reduced according to CC: with CC from 10 to 50 ml/min, 75% of the daily dose of the drug is administered; with CC less than 10 ml/min, 25-50% of the daily dose of the drug is administered.

Special Precautions

If any allergic reactions occur, it is necessary to stop the administration of the drug and prescribe appropriate treatment.

Severe and sometimes fatal allergic reactions, up to the development of anaphylactic shock, may occur. In this regard, when collecting anamnesis, attention should be paid to the tolerance of previous treatment with penicillin.

If there is a history of allergy to penicillin, the drug is strictly contraindicated.

In 5-10% of cases, allergic reactions to penicillin may be cross-reactive with allergic reactions to cephalosporins. In this regard, if there is a history of allergic reactions to cephalosporins, the prescription of penicillins is contraindicated.

In renal failure, doses are reduced according to CC: with CC from 10 to 50 ml/min, 75% of the daily dose of the drug is administered; with CC less than 10 ml/min, 25-50% of the daily dose of the drug is administered.

The sodium content per 0.6 million IU of the drug is 5.5 mg or 0.24 mmol, which must be taken into account when following a low-salt diet.

Drug Interactions

When prescribing benzathine benzylpenicillin concomitantly with NSAIDs (indomethacin, phenylbutazone, salicylates), allopurinol, probenecid, the possibility of competitive inhibition of the excretion of drugs from the body should be considered.

Storage Conditions

Store at a temperature not exceeding 25°C (77°F) in a place protected from light. Keep out of reach of children!

Shelf Life

Shelf life – 4 years. Do not use after the expiration date indicated on the package!

Extencilline in the form of a prepared suspension can be stored in the refrigerator for no more than 24 hours.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.