ILDong Amikacin

Amikacin sulfate.

Each vial contains 250/500 mg (potency) amikacin as the sulfate.
Amikacin sulfate, a semi-synthetic aminoglycoside antibiotic derived from kanamycin has a broad spectrum of antibacterial activity.
Amikacin sulfate resists degradation by most aminoglycoside-inactivating enzymes known to affect gentamicin, tobramycin and kanamycin.
Amikacin sulfate is active in vitro against penicillinase and non-penicillinase producing Staphylococcus species, including methicillin-resistant strains.
Amikacin sulfate combined with a β-lactam antibiotic acts synergistically against many clinically significant Gram-negative organisms.

Pharmacology: Intramuscular Administration: Amikacin is rapidly absorbed after intramuscular administration. In normal adult volunteers, average peak serum concentrations of about 12, 16 and 21 μg/ml are obtained 1 hour after intramuscular administration of 250 mg (3.7 mg/kg), 375 mg (5 mg/kg), 500 mg (7.5 mg/kg), single doses, respectively.
At 10 hours, serum levels are about 0.3 μg/ml, 12 μg/ml and 21 μg/ml, respectively. Tolerance studies in normal volunteers reveal that amikacin is well tolerated 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.
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 mean peak serum concentration of 38 μg/ml at the end of the infusion. 84% of the administered dose was excreted in the urine in 9 hours and about 94% within 24 hours.
Repeat infusions of 7.5 mg/kg every 12 hours in normal adults were well tolerated and caused no drug accumulation.
General: Following administration at the recommended dose, therapeutic levels are found in bone, heart, gallbladder and lung tissue in addition to significant concentrations in urine; bile; sputum; bronchial secretions; interstitial, pleural and synovial fluids.
Spinal fluid levels in normal infants are approximately 10 to 20% of the serum concentrations and may reach 50% when the meninges are inflamed.

The following infections caused by strains of Pseudomonas aeruginosa, Proteus species, Serratia species, Escherichia coli, Klebsiella species, Enterobacter species, Citrobacter species, Providencia species, Acinetobacter species resistant to gentamicin but susceptible to amikacin and Staphylococccus species.
Septicemia, infections associated with bronchiectasis, pneumonia, pulmonary suppuration, serious infections of bones and joints, central nervous system (including meningitis) and skin and soft tissue, peritonitis, burns and postoperative infections, serious complicated and recurrent urinary infections.

Intramuscular Administration: Patients with normal renal function: The recommended dosage for adults, children and older infants with normal renal function is 15 mg (potency)/kg/day divided into 2 or 3 equal doses administered at equally divided intervals.
Treatment of patients in the heavier weight classes should not exceed 15 g (potency)/day. When amikacin is indicated in newborns, it is recommended that a loading dose of 10 mg (potency)/kg be administered initially to be followed with 7.5 mg (potency)/kg every 12 hours.
The usual duration of treatment is 7 to 10 days. The total daily dose by all routes of administration should not exceed 15 mg (potency)/kg/day. At the recommended dosage level, uncomplicated infections due to amikacin-sensitive organisms should respond in 24 to 48 hours. If definite clinical response does not occur within 3 to 5 days, therapy should be stopped and the antibiotic susceptibility pattern of the invading organism should be rechecked. When amikacin is indicated in uncomplicated urinary tract infections, a dose of 250 mg (potency) twice daily may be used.
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 interval.
Intravenous Administration: The dose of amikacin sulfate are identical to the dose recommended for intramuscular administration. The solution for intravenous use is prepared by adding the contents of a 500 mg (potency) vial to 200 ml of sterile diluent such as Normal Saline or 5% Dextrose in Water. The solution is administered by intravenous infusion to adults and pediatric patients over a 30 to 60 minute period. Infants should receive a 1 to 2 hour infusion. Dosage adjustment should be made according to the age and symptoms of the patient.

Patients with a history of hypersensitivity to the ingredient of the product, aminoglycoside antibiotics, or bacitracin.

Careful Administration: It is desirable to avoid using the product in the following patients but, if its use is unavoidable, it should be administered with caution: Patients who or whose blood relatives have deafness due to aminoglycosides or other causes; Patients with renal disorders; Patients with liver disorders; Newborns, prematures; Patients who are not taking adequate oral feedings or are receiving parenteral feeding, elderly patients and patients who are not in good general condition. (Vitamin K deficiency may occur. Close clinical observation is required); Patients with myasthenia gravis; Contains sodium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people.
The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than non-asthmatic people.
General Precautions: It is recommended to confirm the susceptibility and administer only minimum period requiring treatment, in order to prevent the emergence of resistant strains.
In the intravenous infusion, it should be administered over a period of 30 minutes or more, in order to avoid occurrence of adverse reactions. After completion of the infusion, it is desirable to monitor the serum levels.
Use in Elderly: Attention should be paid to the following points in elderly patients. Doses and dosage interval should be adjusted according to the condition of the elderly patients.
1) Amikacin sulfate is excreted primarily in the kidneys, but sometimes elderly patients may have reduced renal function and high serum levels are maintained for a long period. There is a fear of damaging the eighth cranial nerve of the kidneys because of this reason.
2) The bleeding tendency associated with symptoms of vitamin K deficiency may occur.

Use during Pregnancy: There is a fear of damaging the eighth cranial nerve of newborns. The product should be administered only when the expected therapeutic benefit is thought to outweigh any possible risk.
Use in Nursing Mothers: It should be made a decision whether to discontinue nursing or to discontinue the drug.

Shock: Use of the product may rarely cause shock. Close clinical observation is required. If abnormal signs or symptoms occur, therapy should be discontinued and appropriate treatment initiated.
Hypersensitivity: Use of the product may infrequently cause rash or pruritus and rarely cause fever. If such reactions occur, therapy should be discontinued.
Neurologic: Symptoms of eighth nerve disorders such as tinnitus, a closed feeling of the ear, ear pain, vertigo and deafness may occur infrequently. Close clinical observation is required. If symptoms occur, discontinuation of therapy is desirable. If prolongation of therapy is unavoidable, the product should be administered with caution.
Renal: Severe renal disorders such as acute renal failure may occur rarely. Close clinical observation is required. If abnormal signs or symptoms occur, therapy should be discontinued and appropriate treatment initiated.
Hepatic: Elevations in GOT, GPT and/or AL-P levels may occur infrequently. Close clinical observation is required. If abnormal signs or symptoms occur, appropriate treatment including discontinuation of therapy should be initiated.
Hematologic: Symptoms such as leucopenia and eosinophilia may occur rarely.
Gastrointestinal: Symptoms such as diarrhea, nausea and vomiting may occur rarely.
Vitamin deficiencies: Symptoms of vitamin K deficiency (such as hypo-prothrombinemia and bleeding tendency) and vitamin B group deficiency (such as glossitis, stomatitis, anorexia and neuritis) may occur rarely.
Injection sites: Intramuscular use of the product may infrequently cause local pain or induration at the site of injection.
Others: Symptoms such as transient headache and numbness of the lips may occur rarely.

Use of the product may enhance the nephrotoxic effect of blood substitutes such as dextran and sodium alginate, the use of which may cause renal disorders. It is advisable to avoid using the product concomitantly with these blood substitutes.
Respiratory depression due to curare-like effect (neuromuscular blocking effect) may occur. When the product is administered concomitantly with anesthetics or muscle relaxants, careful administration is required.
Concomitant use of the product with loop diuretics such as ethacrynic acid and furosemide may enhance nephrotoxicity and/or ototoxicity.
It is advisable to avoid using the product concomitantly with these diuretics.

Store in a hermetic container at room temperature below 25°C.

Aminoglycosides

J01GB06 - amikacin ; Belongs to the class of other aminoglycosides. Used in the systemic treatment of infections.

POM