PATIENT INFORMATION LEAFLET: INFORMATION FOR THE USER
KANAMYCIN (AS MONOSULFATE) SOLUTION FOR INJECTION
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- This medicine has been prescribed for you. Do not pass it on to others. It may harm them, even if their symptoms are the same as yours.
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- The product solution is filled in the one-point-cut glass ampoule, and snap off the end when use the product.
【Trade name of the preparation】 Kanamycin (as monosulfate) solution for Injection
【Qualitative and quantitative composition】
Kanamycin (as monosulfate) 500mg solution for Injection
Kanamycin (as monosulfate) 1000mg solution for Injection
【Description】Injectable Solution
【Pharmacotherapeutic group】antibiotic-amino glycosides
【Contraindications】Supersensitiveness to kanamycin (including other amino glycosides
in anamnesis), severe chronic kidney disease with azotemia and uremia, neuritis of the VIII
pair of cerebral nerves, pregnancy.
【Pharmacodynamics】 It is an antibiotic with a wide spectrum of a group of amino glycosides. In low concentration it renders bacteriostatic action (by means of damage of protein synthesis in microbial cells), in high concentration it renders bactericidal action (it damages a cytoplasmic membrane of the microbial cell). It penetrates in a microbial cell, interlinks with the specific proteins-receptors on 30S ribosome subunit. It disturbs formation of complex of transport and messenger RNA (30S ribosome subunit) and stops synthetic process of proteins. It is effective in regard to majority of gram-positive and gram-negative microorganisms as well as acid-resistant bacteria: Mycobacterium tuberculosis (including resistant to streptomycin, paraaminosalicylic acid), isoniazid and other antituberculous preparations, except viomycin), Escherichia coli, Shigella spp., Salmonella spp., Proteus spp., Enterobacter spp., Klebsiella pneumoniae, Neisseria gonorrhoeae et meningitidis, Staphylococcus spp.
Strains of those microorganisms resistant to tetracycline, erythromycin, chloramphenicol, benzylpenicillin, streptomycin and others, in most cases preserve sensibility to kanamycin.
It has no effect on Pseudomonas aeruginosa, Streptococcus spp., Bacteroides spp. and other anaerobic bacteria, yeast fungus, viruses and protozoans.
【Pharmacokinetics】
1. Absorption As any other aminoglycoside, kanamycin is weakly absorbed from the gastrointestinal tract. By intramuscular injection Kanamycin is well absorbed into tissues and fluids. Peak serum concentration of kanamycin is reached 1 hour after dosing. One hour after administration of 1g kanamycin, plasma concentration is 10 - 60 mg /ml.
In case of renal impairment, serum kanamycin concentration increases to such levels that they can neurotoxic effect.
2. Distribution Kanamycin is weakly bound to plasma proteins.
The drug diffuses into extracellular fluids, abscesses, ascitic fluids, pericardial fluid, pleural fluid, peritoneal fluid, synovial fluid, lymphatic fluid. Its diffusion is lower into bile, bronchial secretions, saliva, brain and other body fluids.
When the meninges are not inflamed, kanamycin does not penetrate into the cerebrospinal fluid. Kanamycin plasma half-life is approximately 3 hours.
3. Metabolism Aminoglycosides are not metabolized in the liver; they are excreted unchanged in the urine.
4. Elimination Kanamycin is rapidly eliminated in the urine, blood concentration decreases within 6 hours, becoming negligible within 12 - 24 hours. Very little kanamycin is eliminated in the bile.
The largest amount of the dose administered by parenteral route is eliminated within 24 hours in the urine.
The drug is excreted in human milk and the umbilical cord blood circulation.
【Indications to application】
Infectious diseases induced by microorganisms sensitive to kanamycin.
Severe pyogenic-septical diseases: sepsis, meningitis, peritonitis, bacterial endocarditis.
Infectious-inflammatory diseases of respiraltory organs: pneumonia, empyema, lung abscess.
Infections of kidneys and urinary tracts: pyelonephritis, cystitis, urethritis.
Suppurative complications in post-operation period, infected burns and other disease, induce predominantly by gram-negative microorganisms (Escherichia coll, Enterobacter aerogenes, Serratia, Salmonella spp., Klebsiella pneumoniae, Proteus spp., Shigella spp.), resistant to other antibiotics or associations of gram-positive and gram-negative causative agents. Tuberculosis of the lungs and tuberculous damages of other organs (as apart of complex therapy), induced by Koch's bacillus resistant to antituberculous preparation of the I and II lines and other antituberculous preparations, except florimycin.
For treatment with Kanamycin, official local recommendations regarding the proper use of antimicrobial agents must be taken into account.
【Special warnings and precautions for use】
Precautions
This medication should be used carefully in patients with hearing deficit and vestibular abnormalities including impaired eight cranial nerve function.
Kanamycin causes renal and auditory toxicity; consequently, precautions should be taken when using this medication:
In patients with renal impairment, kanamycin can be used only if necessary, the dose should be reduced according to the recommendations concerning renal function
constant renal and auditory monitoring should be performed; if necessary, serum antibiotic concentration should be measured.
concomitant use of diuretics should be carefully considered
close monitoring of renal and hearing functions is necessary if kanamycin is used for a long term period of time, in particular in the case of tuberculosis.
because of the pharmacokinetics of kanamycin, its toxic effects on renal and hearing functions, repeated and/or long-term use of this medication is not recommended especially in the elderly.
If kanamycin is used before surgery, it is necessary to inform the anesthetist-resuscitator.
Tuberculosis treatment
If it is needed for treatment of tuberculosis, the use of kanamycin must comply with guidelines for the treatment of tuberculosis. This medication should not be used, if bacterial tests have not been performed i.e., if there is no antibiotic sensitivity testing indicating that this microbial agent is sensitive to kanamycin or other antibiotics.
To be effective, kanamycin it should be used in combination with one or more medications against tuberculosis. Such a combined treatment is necessary. If necessary, and considering the results of antibiotic sensitivity testing, it may be adjusted.
Renal toxicity effect increases if antibiotics from the aminoglycoside group and cephalosporins are used concomitantly.
For patients presenting with diseases which disturb nerve impulse transmission to muscle fibers (severe myasthenia, Parkinson’s disease, infant botulism), aminoglycoside antibiotics should be used with caution, because the effects aminoglycosides at the neuromuscular junction are similar to the effects of curare. Consequently, this may result in muscular weakness and neuromuscular blockade.
Due to renal immaturity in the neonates, elimination of aminoglycoside antibiotics in this population is slower; consequently, plasma half-life may be longer. Aminoglycoside antibiotics should be used with caution in full-term and premature neonates.
Aminoglycoside antibiotics should be used with caution in the elderly because of a slower elimination process.
【Interaction with other medicinal products and other forms of interaction】
Antibiotics In-vitro incompatibility of aminoglycoside and beta-lactam antibiotics e.g., penicillins has been demonstrated; therefore they should not be mixed in the same syringe.
If combination use of these antibiotics is deemed necessary, they should be injected at different times and at different sites of injection.
If concomitantly used with other antibiotics which may renal and auditory toxicity (gentamicin, streptomycin, neomycin, polymyxin, cephalosporin), the renal and auditory toxicity of kanamycin is increased.
Diuretics If strong diuretics are used concomitantly with kanamycin, in particular loop diuretics, e.g., furosemide, the renal toxicity is increased.
General anesthetics, muscle relaxant agents
Kanamycin can enhance the effect of general anesthetics and muscle relaxant agents which can lead to muscular weakness and neuromuscular blockade causing respiratory paralysis.
【Pregnancy and lactation】
1. Pregnancy Kanamycin crosses the placental barrier. Fetal serum concentrations of kanamycin average 16 to 50% of maternal serum concentrations. There are no well-controlled studies conducted in humans. Experimental studies in rats did not demonstrate any teratogenic effect of kanamycin; however experimental studies in guinea pigs and rats at doses of 200 mg/kg/day led to hearing impairment in the off-spring.
Studies on aminoglycoside antibiotics e.g., gentamicin, demonstrated that the use of this antibiotic in pregnant women may be toxic to the kidney of the fetus.
Studies on streptomycin and tobramycin demonstrated that irreversible, bilateral congenital deafness can occur in the fetus from a woman who used this antibiotic.
Due to the risk of toxic effects to renal, auditory and balance functions, pregnant women can use kanamycin only if absolutely required.
2. Breastfeeding Kanamycin is excreted into breast milk in small amounts. Since kanamycin is poorly absorbed from the gastrointestinal tract (1% absorption of the dose used) negligible amounts of kanamycin pass into the blood circulation of the breastfed infant. Kanamycin can disrupt the intestinal microflora in infant breastfed from mothers treated with kanamycin. Infant may present with diarrhea, fungi can develop on mucous embrane.
Nursing mothers using kanamycin should consider the possibility of stopping breastfeeding.
Effects on ability to drive and use machines
It is necessary to exercise caution when running operations requiring elevated concentrations of attention and quickness of psychomotor action.
【Undesirable effects】
1. Very common: (> 1/10)
Nephrotoxicity (Averages 10-15% incidence). Acute renal failure may be characterized by rising levels of BUN, residual nitrogen, decreased creatinine levels and oliguria, nausea, vomiting. These disorders mostly occurred during prolonged therapy or at high doses, in patients with a history of renal impairment or circulation disorders or those receiving concomitant treatment with drugsknown to induce kidney damage.
These effects are reversible upon discontinuation of the antibiotic.
2. Common: (>1/100 to <1/10)
Ototoxicity (1-5% incidence). The incidence of aminoglycoside-induced cochlear toxicity in neonates has been estimated at around 2%.
3. Uncommon: (> 1/1000 to <1/100)
Vestibular and auditory damage, usually irreversible. Dizziness, nausea, tinnitus and hearing loss. Mostly reported in patients treated with prolonged therapy or at very high doses. This effect is especially common in elderly patients with renal impairment or those receiving concomitant treatment with drugs inducing toxic effects on the hearing and balance organs.
GI intolerance: nausea, vomiting, diarrhea.
Rash. Hypersensitivity reaction: skin rash, hives, itching.
4. Rare: (> 1/10000 to < 1/1000)
Congenital deafness.
Neuromuscular paralysis (most common with large doses administered via intraperitoneal instillation or in patients with myasthenia gravis). Headache, paresthesia, muscle twitching and weakness, convulsions.
Neurtoxicity: headache, paresthesias, and blurred vision. In very rare instances peripheral neuritis, optic neuritis, neuromuscular blockade (with possible respiratory arrest) occurs.
5. Frequency not defined:
Blood and lymphatic system disorders: Changes in blood cell count.
Hepatobiliary disorders: temporary increase in serum transaminases (GOT, GPT), increased serum bilirubin.
Cardiovascular: Edema
Local: Burning, stinging
Respiratory: Dyspnea
【Overdose】
The symptoms of an overdose are the same as those of undesirable effects. Loss of balance and hearing disorders, headache, dizziness, nausea, renal disorders may occur. Toxic doses of kanamycin may block nerve impulse transmission to the muscle and inhibit breathing. In case of neuromuscular blockade, respiratory function needs to be maintained; calcium and neostigmin should be injected.
In the event of overdosage or toxic reaction, hemodialysis or peritoneal dialysis will aid in the removal of kanamycin from the blood.
Posology and method of administration
Standard dose for the patients with normal renal impairment
Intramuscular injection
Kanamycin Acid Sulfate for Injection may be given by deep slow intramuscular injection.
Adults The daily dose of this medication is 15 mg /kg /body weight. If needed, it will be divided into two equal parts (7,5 mg/kg of body weight) and injected every 12 hours.
The maximum daily adult dose is 1.5 g. During the whole course of treatment, the maximum dose which can be used is 15 g kanamycin.
Children The daily dose of this medication is 15 mg /kg/body weight. If needed, it will be divided into two equal parts (7,5 mg/kg/ body weight) and injected every 12 hours.
The maximum daily dose in children is 600 mg. This medication should not be used for more than 6 days.
Infants The daily dose of this medication is 5-15 mg /kg/body weight. If needed, it will be given into two equally divided dosages (7,5 mg/kg/body weight) and injected every 12 hours.
Serum antibiotic concentration should be regularly monitored.
Intravenous injection
Adults and children The dose of this medication by intravenous injection in children and adults is the same as that used for intramuscular injection.
Infants The daily dose of this medication is 15 mg /kg/body weight. If needed, it will be given into two equally divided dosages (7.5 mg/kg/body weight) and injected every 12 hours. Serum antibiotic concentration should be regularly monitored.
Patients with renal impairment
In patients with renal impairment, it is necessary to:
reduce the dose;
regularly check renal, hearing and balance functions;
immediately adjust the dose according to the plasma drug concentration.
The initial dose in adults with oliguria is 1 g. Later, a 500 mg dose every 2-4 days should be used.
Following oliguria or in the case of azotemia or when the glomerular filtration rate is less than 10 ml/min, the initial dose is 1 g. Later, a dose of 500 mg every 1-2 days should be used.
Contraindications
This medication should not be used in the patients with hypersensitivity to antibiotics of the aminoglycoside group.
【Storage conditions】Do not store above 30℃.Protected from light.
Keep out of reach of children. Discard unused portion in accordance with local requirements.
【Shelf life】 24 months.
Do not use after expiration date, specified on the pack.
Pharmacy purchasing terms Prescription medicine.
Manufactured by: Shanghai Harvest Pharmaceutical Co., Ltd.
No. 805, Jinhu Road, China (Shanghai) Pilot Free Trade Zone, China
For any information about this medicinal product, please contact the supplier.
PATIENT INFORMATION LEAFLET: INFORMATION FOR THE USER
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