Tienam

Tienam is a systemic antibacterial drug.

Indications of the tienama

It is used to eliminate infectious skin lesions, the lower part of the respiratory system, joints with soft tissues, and in addition to these organs in the pelvic area. Also used in the treatment of sepsis, infections that have arisen inside the peritoneum, nosocomial infections, endocarditis of the bacterial type, and in addition, with infectious processes of mixed type and for the prevention of inflammation in the post-surgical period.

Release form

The release occurs as a lyophilizate for a solution used for intravenous injections. The glass bottle contains 1 g of lyophilizate (0.5 g of imipenem and sodium cilastatin). Inside the package - 1 bottle of powder.

Pharmacodynamics

The active elements of the drug are imipenem with cilastatin. The medicine has a large range of antimicrobial effects. Tienam has bactericidal action against flora of gram-negative species, gram-positive microbes, as well as aerobes and anaerobes. Acts by inhibiting the binding processes inside the cell walls of bacteria.

Imipenem is included in the category of carbapenems, and is also a derivative of the thienamycin component.

Sodium cilastatin slows down the activity of the enzyme that imipens the renal metabolism, increasing its values within the system of urination in unchanged form. Cilastatin does not affect the activity of microbial β-lactamase, nor does it have its own antibacterial effect.

The medicine has an effect on staphylococci with streptococci, as well as enterobacteria, Neisseria, Campylobacteria, Mycobacteria, Yersinia with Gardnerella, and Listeria with Klebsiella. The drug actively affects the flora, which has resistance to aminoglycosides with penicillins, as well as cephalosporins. Synergic effect is observed when combined with aminoglycosides - in relation to Pseudomonas aeruginosa (in vitro tests).

[1]

Pharmacokinetics

When the solution was injected with 1% lidocaine (0.5 g each), the peak plasma values of imipenem were observed after 2 hours and their average value was 10 μg / ml. In comparison with the / in the form of drugs, imipenem demonstrated approximately 75% bioavailability. Absorption of the component from the site of administration occurred within 6-8 hours, as a result of which the imipenem index inside the plasma was more than 2 μg / ml in the period of about 6 hours after the injection. Administration of the drug in a dose of 0.5 g every 12 hours caused a weak accumulation of the substance. Values of imipenem in the urine were greater than 10 μg / ml for 12 hours after the IM injection of the solution. The average excretion of the component together with the urine was 50%.

The maximum plasma values of cilastatin with LS in / m method at a dosage of 0.5 g on average were 24 μg / ml and were noted after 1 hour. Bioavailability of the substance in comparison with intravenous injection was approximately 95%. Absorption of the substance from the site of administration almost ended after 4 hours. When using the solution 2 times a day (in a dose of 0.5 g), there was no accumulation of the substance. The average level of excretion of cilastatin along with urine is 75%.

Cilastatin is a specific inhibitor of the enzyme dehydropeptidase-I. The substance effectively inhibits the metabolism of imipenem, which allows for the combined use of these components to obtain drug-effective antibacterial values of imipenem in the plasma in the urine. Peak plasma indices of cilastatin 20 minutes after the administration of the solution (0.5 g) ranged from 21-55 μg / ml. The plasma half-life of cilastatin is approximately 1 hour. About 70-80% of the dosage of the substance after 10 hours after administration is excreted in the urine unchanged. Further cilastatin is not observed inside the urine. About 10% was observed in the form of a decay product, a substance of N-acetyl having a suppressive effect on dehydropeptidase (it can be compared with a similar action of the parent component).

Combination of the drug with probenecid doubles the plasma index and the half-life of cilastatin, but does not affect its excretion in the urine. Cilastatin is synthesized with whey protein by approximately 40%.

Dosing and administration

The solution can be administered both in / m and / in the method. A day is allowed to enter no more than 4000 mg of the drug (calculated by the ratio of 50 mg / kg). You can change the dosage, taking into account the kidney function, the severity of the disease and the weight of the patient.

When preventing the development of complications after surgical procedures: injected in / in the solution solution at a dose of 1000 mg (before that an anesthetic is necessarily administered), and then, after 3 hours it is injected again.

Injections of the substance in the / m method are carried out at a rate of 500-750 mg, the procedure is performed twice per day (the maximum allowed daily dose is 1.5 g).

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Use of the tienama during pregnancy

The use of Tienam in pregnant women has not been adequately studied, and therefore it is only possible to apply it in this period if it is confident that the benefit from its administration exceeds the possible complications of the fetus.

Imipenem penetrates into the mother's milk, so when using drugs it is necessary to temporarily refuse to breast-feed the baby.

Contraindications

The main contraindications:

• hypersensitivity to carbapenems or β-lactam type antibiotics;
• infants less than 3 months of age;
• severe renal disease;
• the intramuscular solution made with the addition of lidocaine is forbidden to be used for hypersensitivity to local amide anesthetics (cardiac conduction disorder occurs and the shock state develops).

Caution is required when appointing elderly people, as well as persons with CNS diseases. Also in this case, a preliminary consultation with a dedicated doctor is necessary.

Side effects of the tienama

Injections of the solution can cause the appearance of such side effects:

• lesions of the urogenital system: occasionally there is the appearance of polyuria, oliguria, as well as kidney failure in acute degree and anuria;
• disorders of the NA: the occurrence of hallucinations, paresthesias, mental disorders, the development of myoclonia, epileptic seizures, and sensation of confusion;
• violations of the function of the gastrointestinal tract: occasionally they mark hepatitis of a medicamentous type, and besides this, vomiting, PMK, nausea and diarrhea;
• lesions of hemostasis and hematopoietic system: development of agranulocytosis, eosinophilia, lymphocytosis, basophilia, monocytosis or leuko-, thrombocyto- or neutropenia. There may also be a positive response from the Coombs test, a decrease in hemoglobin and prolongation of the PTV level;
• changes in the values of laboratory studies: an increase in creatinine with bilirubin, and in addition urea nitrogen and liver enzymes AST with ALT;
• allergy symptoms: development of Quincke edema, TEN, urticaria, skin rashes, erythema polyformiformis, pruritus, fever, and in addition to this exfoliative form of dermatitis and manifestations of anaphylaxis;
• Other: Candidiasis, skin hyperemia, pain due to the formation of an infiltrate at the injection site, and in addition thrombophlebitis and a disorder of taste buds can occur.

[2]

Interactions with other drugs

Tienam is not allowed to combine with other antibiotics, as well as salt of lactate.

There may be a cross-allergic reaction in the case of combination with penicillins, as well as cephalosporins.

Demonstrates antagonism towards other β-lactams (such as monobactams, and in addition penicillins and cephalosporins).

As a result of simultaneous use with ganciclovir, convulsions of generalized type arise.

The drug-blockers of tubular secretion can increase the antibiotic indices inside the blood, and also prolong the half-life of imipenem.

[4], [5]

Storage conditions

Tienam is required to be kept in a place that is not accessible to children. The temperature should not exceed 25 ° C.

Special instructions

Reviews

Tienam is considered to be a fairly effective medication, based on the reviews of most patients. But it must be taken into account that it has a very powerful effect, so it is forbidden to apply it independently, without the doctor's control.

Shelf life

Tienam can be used in the period of 3 years from the date of release of the drug.