AMIKACIN
BRAND NAME:- AMICIN , MIKACIN, MIKAJECT 100mg ,250mg,500mg in 2ml inj.
AMIKACIN it is a semisynthetic derivative of KANAMYCIN to which it resembles in pharmacokinetics,dose and toxicity. The outstanding feature of AMIKACIN is its resistance to bacterial aminoglycoside inactivating enzymes. Thus, it has to the widest spectrum of activity, including many organisms resistant to other aminoglycoside. However, relatively higher doses are needed for pseudomonas, Proteus and Staph. Infections.
The range of condition in which AMIKACIN can be used is the same as for gentamicin. It is recommended as a reserve drug for empirical treatment of hospital acquired gram-negative bacillary infections where gentamicin/tobramycin resistance is High. It is effective in tuberculosis,but used only for multidrug resistant infection.More hearing loss than vestibular disturbances occurs in toxicity.
Pharmacodynamic:-
Amikacin is an aminoglycoside antibiotic. Aminoglycosides bind to the bacteria, causing misreading of t-RNA, leaving bacteria unable to synthesize proteins vital to their growth. Aminoglycosides are useful mainly in the treatment infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, however, other antibiotics may be more potent and less toxic to humans.Label,
Pharmacokinetics:-
Amikacin is not absorbed orally and thus must be administered parenterally. It reaches peak serum concentrations in 0.5–2 hours when administered intramuscularly. Less than 11% of the amikacin actually binds to plasma proteins. It is distributed into the heart, gallbladder, lungs, and bones, as well as in bile, sputum, interstitial fluid, pleural fluid, and synovial fluids. It is usually found at low concentrations in the cerebrospinal fluid, except when administered intraventricularly. In infants, amikacin is normally found at 10–20% of plasma levels in the spinal fluid, but the amount reaches 50% in cases of meningitis.It does not easily cross the blood–brain barrier or enter ocular tissue.
While the half-life of amikacin is normally two hours, it is 50 hours in those with end-stage renal disease.
The majority (95%) of amikacin from an intramuscular or intravenous dose is secreted unchanged via glomerular filtration and into the urine within 24 hours. Factors that cause amikacin to be excreted via urine include its relatively low molecular weight, high water solubility, and unmetabolized state.
Mechanism of action:-
The primary mechanism of action of amikacin is the same as that for all aminoglycosides. It binds to bacterial 30S ribosomal subunits and interferes with mRNA binding and tRNA acceptor sites, interfering with bacterial growth. This leads to disruption of normal protein synthesis and production of non-functional or toxic peptides. Other actions have been postulated for drugs of this class.Label, Amikacin, as well as the rest of the aminoglycosides, are generally bacteriocidal against gram-positive and gram-negative bacteria.
USE:-
Common used as a infection, urinary tract infection. It is effective in tuberculosis. Used for multidrug resistant infection.is also used for the treatment of multidrug-resistant tuberculosis. It is used by injection into a vein using an IV or into a muscle.
Side Effects:-
Kidney damage , Ototoxicity, Nausea, vomiting, stomach upset, or loss of appetite may occur. Pain/irritation/redness at the injection site may rarely occur .
DOSE:- 15mg/kg /day in 1-3doses; urinary tract infection 7.5mg/kg/day. As directed by your doctor.
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