AMIKACIN
Amikacin is a broad spectrum antibiotic used in dogs, cats, horses and cows for gram negative, gram positive bacteria, pseudomonas, mycoplasma etc. infections.
Amikacin is a semi synthetic extended spectrum aminoglycoside antibiotic. It is resistant to drug inactivating enzymes.
CATEGORY
MECHANISM OF ACTION
Aminoglycoside antibiotic. Action is to inhibit bacteria protein synthesis via binding to 30S ribosome and disrupt the outer membrane in gram-negative bacteria. Amikacin is bactericidal with a broad spectrum of activity except against streptococci and anaerobic bacteria. Amikacin has activity against many bacteria, especially gram negative bacilli, that are resistant to other drugs. Amikacin may be more active than gentamicin against many gram-negative bacteria, especially enteric species, because it is less susceptible to drug-degrading enzymes produced by bacteria. It is one of the most active of all the aminoglycoside group of antibacterial agents.
In most animals, the half-life is short (1–2 hours), and volume of distribution reflects extracellular body water (e.g., 200–250 mL/kg). Amikacin is not absorbed from oral administration. It is eliminated almost exclusively by renal clearance
CLINICAL USES
Amikacin is indicated in bacterial infections, especially for treatment of serious infections caused by gram-negative bacteria. When resistance to gentamicin is anticipated, amikacin is often used in place because bacteria resistant to gentamicin are still susceptible to amikacin. In horses, amikacin is also used for local administration as an intrauterine lavage to treat metritis and other infections of the genital tract caused by gram-negative bacteria. For this purpose, it has been used as an intrauterine flush. In horses, amikacin is also used for regional limb perfusion.
SIDE EFFECTS
Nephrotoxicity is the most dose-limiting toxicity in animals. Ensure that pets have adequate fluid and electrolyte balance during therapy. Ototoxicity and vestibulotoxicity are also possible with amikacin.
CONTRAINDICATIONS
Amikacin should not be used in animals with renal insufficiency or renal failure. Also not in dehydrated animals.
DRUG INTERACTIONS
Amikacin should not be mixed in a vial or syringe with other antibiotics. Amikacin is incompatible with other drugs and compounds when mixed in the same vial or syringe. This effect is particularly important when mixing with other antibiotics. When used with anesthetic agents, neuromuscular blockade is possible.
PRECAUTIONS
Once daily doses are designed to maximize peak-to-minimum inhibitory concentration (MIC) ratio, Consider therapeutic drug monitoring to decrease the risk of renal toxicosis. Activity against some bacteria (e.g., Pseudomonas) may be enhanced when combined with a beta lactam antibiotic, but this action is controversial. Nephrotoxicity is increased with persistently high trough concentrations.
MONITORING
Clinical and Laboratory Standards Institute (CLSI) MIC breakpoint is ≤ 4 mcg/mL for dogs and horses and ≤ 2 mcg/mL for foals. The canine breakpoint can also be applied to bacterial isolates from cats. Monitor BUN, serum creatinine, and urine for evidence of renal toxicity. Plasma or serum drug concentrations can be monitored to measure for problems with systemic clearance. When monitoring trough levels in patients during once-daily administration, the trough levels should fall below the limit of detection. Alternatively, the half-life and clearance can be measured from samples taken at 1 hour and 2–4 hours post-dosing. Clearance in most animals should be above 1.0 mL/kg/min, and half-life should be less than 2 hours.
FORMULATIONS
Injectables:
Amikacin is available in 50 mg/mL and 250 mg/mL injections.
Tablets:
No tablets available for amikacin.
Syrup/Suspensions:
No syrup/suspension available for amikacin.
Other formulations:
No listed other formulation available for amikacin.
STORAGE
Amikacin should be stored in a tightly sealed container, protected from light, and at room temperature. Amikacin will be unstable if mixed with other drugs.
DOSE RATE
Dose rates for various animals are listed below. Adjust the dose rates according to the pathophysiology and conditionNo of each case.
Dogs
- 15 mg/kg q24h IV, IM, or SQ
Cats
- 10 mg/kg q24h IV, IM, or SQ
Horses
- Adult: 10 mg/kg q24h IV or IM
- Foal: 20 mg/kg q24h IV
- Intrauterine use: Administer 2 g (8 mL) diluted in 200-mL sterile saline solution in uterus once per day for 3 days.
- Regional limb perfusion: Doses have ranged from 125 to 500 mg per limb, diluted in 60 mL of saline.
Cattle
- Adult: 10 mg/kg q24h IM, IV, or SQ
- Calf (younger than 2 weeks of age): 20 mg/kg q24h IV or IM
ADMINISTRATION
Amikacin typically administered via intravenous (IV), intramuscular (IM), subcutaneous (SC) routes. It is essential to check the label for specific preparation instructions since certain formulations may be designated for specific routes of administration.
ORAL BIOAVAILABILITY
Amikacin is very poor bioavailable by oral route and not available in oral tablet.
PROTEIN BINDING
Protein binding for amikacin is less than 10%.
ELIMINATION HALF LIFE
The elimination half-life of amikacin is approximately 2 hours.
METABOLISM
Metabolism of amikacin is not happen, it excreted without metabolism.
EXCRETION
Excretion of amikacin takes place in the Kidneys.
ANTIDOTE
No specific antidote.
NOTES
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