Aminocin

(Amikacin Sulphate)
100, 250, 500mg / 2ml Injection

PHARMACOLOGICAL ACTION

AMINOCIN (AMIKACIN SULPHATE) is a semi-synthetic aminoglycoside antibiotic which is active against a broad spectrum of Gram-negative organisms, including Pseudomonas and some Gram-positive organisms. Chemically, the medicine consists of 2 amino sugars glycosidically linked to deoxy-streptamine whose 1-amino group has been acylated by S-4-amino-2-hydroxy-butyric acid.

AMINOCIN (AMIKACIN SULPHATE) is rapidly absorbed after intramuscular administration. In normal adult volunteers, average peak serum concentrations of about 12 and 21 micrograms/mL are obtained 1 hour after intramuscular administration of 250 mg (3,7 mg/kg) and 500 mg (7,5 mg/kg), single doses, respectively. At 10 hours, serum levels are about 0,3 micrograms/mL and 2,1 micrograms/mL, respectively. Mean urine concentrations for 6 hours are 563 micrograms/mL following a 250 mg dose and 832 micrograms/mL following a 500 mg dose.

General

Pharmacokinetics studies in normal adult subjects reveal mean serum half-life to be slightly over 2 hours with a mean total apparent volume of distribution of 24 litres, approximately 28% of the body weight. By the ultrafiltration technique, reports on serum protein binding range from 0 to 11%. The mean serum clearance rate is about 100 mL/min and the renal clearance rate is 94 mL/min in subjects with normal renal function.

Amikacin is excreted primarily by way of glomerular filtration. Following administration at the recommended dose, therapeutic levels are found in significant concentrations in urine, bile, bronchial secretions, interstitial, pleural, and synovial fluids and peritoneal cavity.

Spinal fluid levels in normal infants are approximately 10 to 20% of the serum concentrations and may reach 50% when the meninges are inflamed. AMINOCIN (AMIKACIN SULPHATE) has been demonstrated to cross the placental barrier and yield significant concentrations in amniotic fluid.

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INDICATIONS

AMINOCIN

(AMIKACIN SULPHATE)

AMINOCIN (AMIKACIN SULPHATE)is indicated in the short-term treatment of serious infections due to susceptible strains of Gram-negative bacteria, including Pseudomonas species, Escherichia coli, species of indole-positive and indole-negative Proteus, Providencia species, Klebsiella-Enterobacter-Serratia species, and Acinetobacter (formerly Mima-Herellea) species and Citrobacter freundii.