Thienam (imipenem, cilastatin sodium) powder for solution for infusion 500 mg. vials №10

Description

Thienam (imipenem, cilastatin sodium) powder for solution for infusion 500 mg. vials №10

Composition

active substances: imipenem and cilastatin sodium;

1 vial contains imipenem 500 mg and cilastatin sodium 500 mg;

Excipient: sodium bicarbonate.

Dosage form

Powder for solution for infusion.

Basic physical and chemical properties: powder from white to light yellow color.

Pharmacotherapeutic group

Antibacterial agents for systemic use. Carbapenems.
ATX code J01D H51.

Pharmacological properties

Thienam consists of two components: imipenem and cilastatin sodium – in a weight ratio of 1: 1.

Imipenem, also known as N-formamidoyl-thienamycin, is a semi-synthetic derivative of thienamycin, the parent compound produced by the filamentous bacterium Streptomyces cattleya.

Imipenem has bactericidal activity by inhibiting the synthesis of bacterial cell wall of gram-positive and gram-negative bacteria by binding to penicillin-binding proteins (PBPs).

Cilastatin sodium is an inhibitor that has a competitive, reversible and specific effect on dehydropeptidase-I, a renal enzyme that is metabolized and inactivated by imipenem. It has no natural antibacterial activity and does not affect the antibacterial activity of imipenem.

Indications

It is prescribed for the treatment of infections that affect: the genitourinary system, lower respiratory tract, abdominal cavity, soft tissue skin, bones and joints. Effective in the treatment of septicemia. It is ineffective for meningitis.
The effectiveness of treatment with Thienam is explained by the fact that it consists of a well-chosen combination of two drugs, one of which (imipenem) is a broad-spectrum antibiotic, including antibacterial, the second (cilastatin sodium), due to its properties, is able to increase the concentration of imipenem in the kidneys , which greatly enhances its effect.

Contraindications

Contraindicated in case of allergy to one of the active ingredients of Thienam . Do not administer intramuscularly to patients with renal insufficiency. It is forbidden to use lidocaine hydrochloride as an isotonic solution in combination with Thienam in patients in a state of shock or in patients with heart block.

Application during pregnancy and lactation

There is no recorded data on the complete safety of Thienam for the fetus.

Method of administration and dosage

It is administered intravenously or intramuscularly (deeply penetrating into the muscle) after a test for resistance to Thienam of the patient’s microflora. The introduction is carried out very slowly, for at least 20 minutes, with a dose of 1 gram per dose, the introduction is carried out within 60 minutes.
Average dose: 1-2 grams per day. The daily dose is divided into 3-4 doses. In severe cases, the dose can be increased to a maximum of 4 grams per day, then reduced in stages. In the treatment of urogenital infections, 500 milligrams are injected once into the muscle.
In case of impaired renal function, the dose is reduced to 0.25-0.5 g per dose, administering the drug at intervals of 6 to 12 hours.
For children weighing less than 40 kg, the dosage is prescribed at the rate of 15 micrograms per 1 kg of body weight, administered at intervals of 6 hours. Maximum per day, you can enter 2 grams.

Overdose

There are no accurately recorded data. Hemodialysis is presumably effective. Symptomatic treatment is also recommended.

Side effects

Thienam is generally well tolerated by patients. Side effects are similar with cephalosporins. In particular, allergic reactions, manifestations of rash, pruritus, urticaria, anaphylaxis, erythema, angioedema, candidiasis, toxic epidermal necrolysis are likely.
Possible side effects from the gastrointestinal tract: nausea, vomiting, pseudomembranous colitis, coloring of the tongue and teeth. Signs of eosonophilia, leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hepatitis, polyuria, myoclonus, mental disorders, encephalopathy were rare.