Basic Info.
Suitable for
Elderly, Children, Adult
Pharmaceutical Technology
Chemical Synthesis
Pharmacological and Toxicology
Aminoglycoside Antibiotic
Character
Colorless or Yellowish Clear Liquid
Usage
Intramuscular Injection or Intravenous Drip
Molecular Formula
C22h43n5o13
Molecular Weight
585.6025
Product Description
Product Description
Amikacin Injection 500mg/2mLDescriptionAmikacin is a semisynthetic aminoglycoside antibiotic derived from kanamycin. Amikacin occurs as a white, crystallinepowder and is sparingly soluble in water. The injection consists of the sulfate salt.Amikacin Injection is a sterile clear, colourless solution, free from specks, lint, or other visible evidence ofcontamination. Each 2 mL vial contains amikacin sulfate equivalent to amikacin activity 500 mg (500,000 I.U.).
PharmacokineticsAbsorptionFollowing IM administration of a single dose of amikacin of 7.5 mg/kg in adults with normal renal function, peakplasma amikacin concentrations of 17-25 micrograms/mL are attained within 45 minutes to 2 hours.Following IV infusion of the same dose given over 1 hour peak plasma concentrations of the drug average 38micrograms/mL immediately following the infusion, 5.5 micrograms/mL at 4 hours, and 1.3 micrograms/mL at 8 hours.DistributionFollowing administration of usual dosages of amikacin, amikacin has been found in bone, heart, gallbladder, and lungtissue. Amikacin is also distributed into bile, sputum, bronchial secretions, and interstitial, pleural, and synovial fluids.EliminationThe plasma elimination half-life of amikacin is usually 2-3 hours in adults with normal renal function and is reported torange from 30-86 hours in adults with severe renal impairment.In adults with normal renal function, 94-98% of a single IM or IV dose of amikacin is excreted unchanged byglomerular filtration within 24 hours. The drug may be completely recovered within approximately 10-20 days inpatients with normal renal function. Terminal elimination half-lives of greater than 100 hours have been reported inadults with normal renal function following repeated IM or IV administration of the drug.In patients with impaired renal function, the clearance of amikacin is decreased; the more severe the impairment, theslower the clearance. Therefore, the interval between doses should be adjusted according to the degree of renalimpairment. Endogenous creatinine clearance rate and serum creatinine which have high correlation with serum half-lifeof amikacin, may be used as a guide for this purpose (see Dossge and Administration - Impaired RenalFunction).IndicationsAmikacin Injection is indicated in the short-term treatment of serious infections caused by susceptible strains of Gramnegativebacteria, (see Microbiology).Staphylococcus aureus, including methicillin-resistant strains is the principal Gram-positive organism sensitive toamikacin.The use of amikacin in the treatment of staphylococcal infections should be restricted to second-line therapy, andshould be confined to patients suffering from severe infections caused by susceptible strains of stapylococcus whohave failed to respond or are allergic to other available antibiotics.Amikacin Injection is indicated in the treatment of neonatal sepsis when sensitivity testing indicates that otheraminoglycosides cannot be used.In certain severe infections such as neonatal sepsis, concomitant therapy with a penicillin type drug may be indicatedbecause of the possibility of infections due to Gram-positive organisms such as streptococci or pneumococci. Ifconcomitant treatment with a penicillin type drug is indicated, then the drugs should be administered separately and atdifferent sites because in-vitro mixing of the two drugs causes inactivation of amikacin.Clinical studies have shown amikacin to be effective in treating bacteraemia, septicaemia including neonatal sepsisand serious infections of the respiratory tract, bones and joints, central nervous system, skin and skin structures(including those resulting from burns), intra-abdominal organs, post-operative infections and complicated and recurrenturinary tract infections, when caused by susceptible organisms.ContraindicationsAmikacin Injection is contraindicated in patients with a known history of hypersensitivity to amikacin, any constituentsof the injection (see Description ) or in patients who may have subclinical renal or eighth nerve damage induced byprior administration of nephrotoxic and/or ototoxic agents, as the toxicity may possibly be additive.Pregnancy (see Use in Pregnancy) ; Lactation (see, Use in Lactation).Use in PregnancyCategory D. Gentamicin and other aminoglycosides cross the placenta. There is evidence of selective uptake ofgentamicin by the foetal kidney resulting in dam ge (probably reversible) to immature nephrons, eighth cranial nervedamage has also been reported following in-utero exposure to some of the aminoglycosides. Because of the chemicalsimilarity, all aminoglycosides must be considered potentially nephrotoxic and ototoxic to the foetus. It should also benoted that therapeutic blood levels in the mother do not equate with safety for the foetus.Use in LactationIt is not known whether amikacin is excreted in breast milk. Since the possible harmful effect on the infant is notknown, it is recommended that if nursing mothers must be given amikacin, the infants should not be breast fed duringtherapy.Interactions with Other DrugsIf possible, do not give amikacin in conjunction with athacrynic acid, frusemide or other potent diuretics which maythemselves cause ototoxicity or enhance aminoglycoside toxicity by altering antibiotic concentrations in serum andtissue.Potent diuretics:Other neurotoxic and/or nephrotoxic agents:If possible, avoid concurrent or sequential use of other neurotoxic and/or nephrotoxic antibiotics, including otheraminoglycosides, polymyxin B, colistin, cisplatin, vancomycin, amphotericin B, clindamycin and cephalosporins.Anaesthetics/neuromuscular blocking agents or medications with neuromuscular blocking activity:Concurrent use of amikacin with agents with neuromuscular blocking activity e.g. succinylcholine, tubocurarine,decamethonium, halogenated hydrocarbon inhalation anaesthetics, opioid analgesics and massive transfusions withcitrated anticoagulated blood, should be carefully monitored; neuromuscular blockade may be enhanced, resulting inskeletal muscle weakness and respiratory depression or paralysisi (apnea); caution is recommended when thesemedications and amikacin are used concurrently during surgery or in the postoperative period, especially if there is apossibility of incomplete reversal of neuromuscular blockade postoperatively; treatment with anticholinesterase agentsor calcium salts may help to reverse the blockade.Penicillins:Aminoglycosides are inactivated by solutions containing penicillins. This inactivation is brought about by the opening ofthe beta-lactam ring and combination of the penicillin with an amino group of the aminoglycoside to form a biologicallyinactive amide. For this reason, amikacin and penicillins should not be combined in intravenous injections/infusions.The inactivation of some aminoglycosides by penicillins has been reported in vivo, especially in patients with renalfailure who maintain a higher level of the penicillin for a longer period of time compared to patients with normal renalfunction. Therefore, when amikacin and penicillins are used together in patients with renal failure, the time ofadministration of each drug should be staggered so that several hours separate each infusion.CompatibilitiesAmikacin sulfate is stable for 24 hours at room temperature in the presence of light at 5 mg/mL and 0.25 mg/mL in0.9% Sodium Chloride Intravenous Infusion B.P. and 5% Glucose Intravenous Infusion B.P. solutions.Adverse ReactionsAmikacin induced hepatotoxicity is not a common side effect, however it may occur. Increased serum transaminases(ALT, AST) increased serum bilirubin, hepatomegaly, and hepatic necrosis have been reported.The percentages below refer to incidence in clinical trials.Dosage and AdministrationUncomplicated infections due to sensitive organisms should respond to treatment within 24 to 48 hours at therecommended dosage. If no improvement occurs within three to five days, the use of amikacin sulfate should be reeveluatedand consideration be given to alternative therapy. Failure of the infection to respond may be due toresistance of the organism or to the presence of septic foci requiring surgical drainage.Whenever possible, and especially in patients with impaired renal function, peak and trough amikacin serumconcentrations should be determined and dosage adjusted where necessary to maintain desired serumconcentrations. In general, desired peak cone ntrations are between 15 to 30 micrograms/e mL, and troughconcentrations should not exceed 5 to 10 micrograms/mL. An increased risk of toxicity may be associated withprolonged peak amikacin serum concentrations greater than 30 to 35 micrograms/mL.Intramuscular or Intravenous AdministrationThe intramuscular route is preferred for most infections, but in life-threatening infections or when an intramuscularinjection is not feasible, an intravenous infusion (0.25% over 30 to 60 minutes) may be used.The compatible diluents for intravenous use if required are as follows: 5% Glucose Intravenous Infusion B.P. in Waterfor Injections B.P. and Sodium Chloride Intravenous Infusion B.P. (0.9%). Use solutions for I.V. administration within 12hours after preparation.DosageDosage of amikacin sulfate is expressed in terms of amikacin and calculated on a body weight basis. Dosage isidentical for both routes of administration.The usual recommended dose of amikacin is 15mg/kg daily given in two or three equally divided doses.Dosage given for patients with normal renal function. Initiate treatment with a loading dose of 10 mg/kg followed by 7.5mg/kg every 12 hours. The maximum total daily dose should not exceed 15 mg/kg. Solution infusions via the I.V. routeshould be given over a 1 to 2 hour period.Insufficient clinical use has not enabled firm dosage guidelines to be established for the use of amikacin in prematureinfants.Adults and Children:Neonates and Premature Infants:OverdosageManagementIn the event of overdosage or toxic reactions peritoneal dialysis or haemodialysis should be conside ed. Theseprocedures are of particular importance in patients with impaired renal function. In the newborn infant, exchangetransfusion may also be considered.Clinical featuresLikely signs and symptoms include tinnitus, vertigo, reversible or irreversible deafness, skin rash, drug fever,headache, paraesthesia, reduced renal function or renal failure.
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