International generic name

Amikacin

Drug form and composition

Solution for injection. One ampoule of 2 ml contains: 100 mg Amikacin sulfate (50 mg/ml) equivalent to 100 mg Amikacin; 250 mg Amikacin sulfate (125 mg/ml) equivalent to 250 mg Amikacin; or 500 mg Amikacin sulfate (250 mg/ml) equivalent to 500 mg Amikacin.

Indications

Amikacin is indicated for the treatment of infections of: central nervous system, urogenital system, biliary and intestinal tracts, skin and subcutaneous tissues, intraabdominal infections, pneumonia, caused by Gram-negative microorganisms, secondary infections after combustion, bacterial septicemia, infections of the bones and joints (caused by sensitive to Amikacin microorganisms).

Dosage and administration

In adults and children with normal renal function, Amikacin is administered intramuscularly as an intravenous bolus or by slow intravenous infusion in a dose of 5 mg/kg body weight given every 8 hours or 7.5 mg/kg body weight every 12 hours for a period of 7 to 10 days. Before the infusion 500 mg Amikacin is dissolved in 200 mg saline or other suitable solution. The infusion duration is 30 to 60 minutes. The maximum daily dose should not exceed 15 mg/kg body weight, and the total dose for one treatment course should be bellow 15 g. In newborn and prematurely born infants, the single initial dose of Amikacin is 10 mg/kg body weight. After this dose the treatment continues with a dose of 7.5 mg/kg body weight given every 12 hours during the following 7 to 10 days. Amikacin can be used in a single daily dose of 1 g intramuscularly or 15 mg/kg body weight intravenously. In patients with disturbed renal function, the dose should be reduced and Amikacin is injected at longer intervals to avoid possible cumulation. In these cases, dosage should be determined based on the creatinine clearance and the serum creatinine level.

Contraindications

Hypersensitivity to aminoglycoside antibiotics, pregnancy and breast-feeding.

Special warnings and precautions

In high plasma concentrations of the drug there is an increased risk of ototoxicity and kidney toxicity, because of which a monitoring of the pick plasma concentration is advised Amikacin should be prescribed with increased caution in patients suffering from parkinsonism, diseases of the auditory nerve, myasthenia gravis, severe renal and hepatic insufficiency. In cases of prolonged treatment, regular checks of the state of hearing and creatinine clearance are advised. The treatment should be discontinued in cases of loss of hearing of high frequency sounds.

Drug interactions

Concurrent administration of Amikacin with myorelaxants leads to potentiation of their effects and there is a possibility of cessation of the breathing. The combination with other aminoglycoside antibiotics should be avoided because of the augmentation of their ototoxic and nephrotoxic effects. Concurrent administration of Amikacin with fast acting diuretics increases the risk of ototoxicity in patients with renal failure. Combination with cefalosporins or polymixins increases the risk of nephrotoxicity.

Adverse reactions

After prolonged treatment with Amikacin the most common adverse effects are the nephrotoxicity and the ototoxicity. The manifestations of ototoxicity are vestibular toxic changes (in balance) and cochlear toxic changes (loss of hearing associated with a sensation for pressure and noise in ears and decreased perception of high frequency sounds). After concurrent administration of Amikacin and other nephrotoxic drugs renal failure can be developed. Relatively rare the following adverse effects can be seen: allergic reaction, nausea, vomiting, stomatitis, blood changes, depression of respiration, and muscle pareses.

Pharmacological mechanisms

Amikacin is a semisynthetic antibiotic of the aminoglycoside group. It possesses a broad antimicrobial spectrum, but the greatest activity is against the Gram-negative bacteria (E. coli, Proteus, Klebsiella) etc. The drug is active also against some staphylococcus strains (Staphylococcus epidermidis and aureus). Amikacin has a bactericidal action which is due to the inhibition of the protein synthesis in the cells of the microorganisms. It produces errors in genetic code reading during the process of translation and interferes with the ordering of amine acids in the peptic chain and leads to production of “useless proteins”. The presence of a remnant of -hydroxybutyrate acid in the Amikacin’s molecule makes this drug insensitive to the enzymes, produced by Pseudomonas and enterobacteria, resistant to the other aminoglycosides.

Supplied

10 or 100 ampoules of 2 ml (100 mg). 10 or 100 ampoules of 2 ml (250 mg). 10 or 100 ampoules of 2 ml (500 mg).

Expiry

2years.