Each mL contains: Amikacin Sulfate equivalent to Amikacin 50 mg, 125 mg, and 250 mg, respectively.
Amikacin Sulfate is a semisynthetic aminoglycoside antibiotic derived from kanamycin. It is C22H43N5O13·2H2SO4, D-Streptamine, 0-3-amino-3-deoxy-a-D-glucopyranosyl - (1-+6)-) (6-amino-6-deoxy-a-d-glucopyranosyl(1-+4)-N1-(4-amino-2-hydroxyl-oxobuty)2-deoxy-, (S)-, sulfate (1 :2) (salt).
Pharmacology: Pharmacokinetics: Intramuscular Administration: Amikacin is rapidly absorbed after intramuscular administration. In normal adult volunteers, average peak serum concentrations about 12, 16 and locally, following repeated intramuscular dosing, and when given at maximally recommended doses, no ototoxicity or nephrotoxicity has been reported.
There is no evidence of drug accumulation with repeated dosing for 10 days when administered according to recommended doses.
With normal function, 91.9% of the intramuscular dose is excreted unchanged in the urine in the first 8 hours, and 98.2% within 24 hours. Mean urine concentrations for 6 hours are 563 mcg/ml following a 250mg dose. 697 mcg/ml following a 375-mg dose, and 832 mcg/ml, following a 500-mg dose.
Preliminary intramuscular studies in newborns of different weights (less than 1.5 Kg, 1 .5 to 2.0 Kg) at dose of7.5 mg/Kg revealed that like other aminoglycosides, serum half-life values were correlated inversely with post natal age and renal clearances of amikacin. The volume of distribution of amikacin, like other aminoglycosides, remains primarily in the extracellular fluid space in neonates. Repeated dosing every 12 hours in all the above groups did not demonstrate accumulation after 5 days.
Intravenous Administration: Single doses of 500 mg (7.5 mg/kg) administered to normal adults as an infusion over a period of 30 minutes produced a peak serum concentration of 38 mcg/ml at the end of the infusion, and levels of 24 mcg/ml, 18 mcg/ml and 0.75 mcg/ml at 30 minutes, 1 hour, and 10 hours, post infusion, respectively.
Eighty four percent of the administered dose was excreted in the urine in 9 hours and about 94% within 24 hours. Repeated infusions of 7.5 mg/Kg every 12 hours in normal adults were tolerated and caused no drug accumulation.
General: Pharmacokinetic studies in normal adult subjects reveal the mean serum half-life to be slightly over 2hours with a mean total apparent volume of distribution of 24 liters (28% of the body weight). By the ultrafiltration technique, reports of protein binding range from 0 to 11 %. The Mean serum clearance rate is about100 ml/min and the renal clearance rate is 94 ml/min. in subjects with normal renal function.
Amikacin is indicated in short-term treatment of serious infection 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, Seratia species and Acinetobacter (mima-Herella) species.
Amikacin is effective in bacterial septicemia (including neonatal sepsis); serious infection of the respiratory tract, bones, joints, central nervous system (including meningitis) and skin and soft tissue intra abdominal infections(including peritonitis); and in burns and post-operative infections (including postvascular surgery).
Aminoglycosides are not indicated in the uncomplicated initial episodes of urinary tract infection, unless the causative organisms are not susceptible to antibiotics having less potential toxicity.
Amikacin is also effective in staphylococcal disease such as, severe infections, where the causative organisms may either Gram negative (-) bacterium or a staphylococcus, infections due to susceptible strains of staphylococci in patients allergic to other antibiotics, and in mixed staphylococcal/Gram negative (-) infections.
The patient's pre-treatment body weight should be obtained for calculation of correct dosage. Amikacin may be given intramuscularly or intravenously.
Intramuscular Administration for patients with Normal Renal Function: Recommended dosage for adults, children and other infant: 15 mg/kg/day divided into 2 to 3 equal doses administered at equally divided intervals i.e., 7.5 mg/kg every 12 hours or 5 mg/kg every 8 hours. Treatment of patients in the heavier weight classes should not exceed 1.5 g/day. When amikacin is indicated in newborns, it is recommended that a loading dose of 10 mg/kg, be administered initially to be followed with 7.5 mg/kg every 12 hours.
The usual duration of treatment is 7 to 10 days. It is desirable to limit the duration of treatment to short term whenever feasible.
Intramuscular Administration for patients with Impaired Renal Function: Whenever possible, serum amikacin concentrations should be monitored by appropriate assay procedures.
Doses may be adjusted in patients with impaired renal function either by administering normal doses at prolonged intervals or by administering reduced doses at a fixed intervals.
Intravenous Administration: The individual dose, the total daily dose, and the total cumulative dose of Amikacin are identical to the dose recommended for intramuscular administration. The solution for intravenous use is prepared by adding the contents of a 500 mg vial to 100 or 200 ml of sterile diluent such as Normal Saline or 5% Dextrose in Water or any of the compatible solutions listed below.
The solution is administered to adults over 30 to 60 minutes period. The total daily dose should not exceed 15 mg/kg/day and may be divided into, either 2 to 3 equally divided doses at equally divided intervals.
A history of hypersensitivity to amikacin is contraindicated for its use. A history of hypersensitivity of serious toxic reactions to aminoglycosides may contraindicate the use of any other aminoglycosides, because of the known cross-sensitivities of patients to drugs in this class.
Patients treated with parenteral Aminoglycosides should be under close clinical observation because of the potential ototoxicity and nephrotoxicity associated with their use.
Neurotoxicity manifested as vestibular and permanent bilateral auditory ototoxicity can occur in patients with preexisting renal damage and in patients with normal renal function treated with higher doses and for those longer than recommended.
Aminoglycosides are potentially nephrotoxic. The risk of nephrotoxicity is greater in patients with impaired renal function and in those who receive higher doses or prolonged therapy.
This product contains Sodium Metabisufite, which may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible persons.
Stability in IV Fluids: Amikacin is stable for 24 hours at room temperature at concentrations of 0.25 and 5.0 mg/ml in the following solutions; 5% Dextrose Injection, 5% Dextrose Solution and 0.2% Sodium Chloride Injection, 5% Dextrose Solution and 0.45% Sodium Chloride Injection, 0.9% Sodium Chloride Injection, Lactated Ringer's Injection, Normosol R in 5% Dextrose Injection.
In the above solutions with amikacin concentrations of 0.25 and 5.0 mg/ml, solutions aged for 60 days at 4°C and then stored at 25°C had utility time of 24 hours.
At the same concentrations, solutions frozen and aged for 30 days at -15°C and stored at 25°C had utility time of 24 hours.
Store at temperatures not exceeding 30°C.
J01GB06 - amikacin ; Belongs to the class of other aminoglycosides. Used in the systemic treatment of infections.
Soln for inj (vial) 50 mg/mL x 2 mL. 125 mg/mL x 2 mL x 10's. 250 mg/mL x 2 mL.