Kanamycin Sulfate

(rINNM)
Synonyms: Kanamicin-monoszulfát; Kanamicino monosulfatas; Kanamycin A Sulphate; Kanamycin monosulfát monohydrát; Kanamycin Monosulphate; Kanamycin Sulphate de; Kanamycine, Sulfate de; Kanamycini monosulfas; Kanamycini Monosulfas Monohydricus; Kanamycini Sulfas; Kanamycinmonosulfat; Kanamycyny siarczan; Kanamysiinimonosulfaatti; Sulfato de kanamicina. 6O-(3-Amino-3-deoxy(6-amino-6-deoxyphate monohydrate.
Cyrillic synonym: Канамицина Сульфат.

💊 Chemical information

Chemical formula: C18H36N4O11,H2SO4,H2O = 600.6.
CAS — 59-01-8 (kanamycin); 25389-94-0 (anhydrous kanamycin sulfate).
ATC — A07AA08; J01GB04; S01AA24. ATC Vet — QA07AA08; QJ01GB04; QS01AA24.

Pharmacopoeias.

In Eur. and US. Jpn includes the anhydrous substance.

Ph. Eur. 6.2

(Kanamycin Monosulphate; Kanamycin Sulphate BP 2008). The sulfate of an antimicrobial substance produced by the growth of certain strains of Streptomyces kanamyceticus. A white or almost white, crystalline powder containing not less than 750 units/mg and 15.0 to 17.0% of sulfate, calculated with reference to the dried material. Soluble 1 in about 8 of water; practically insoluble in alcohol and in acetone. A 1% solution in water has a pH of 6.5 to 8.5.

USP 31

(Kanamycin Sulfate). A white, odourless crystalline powder. It has a potency equivalent to not less than 750 micrograms of kanamycin per mg, calculated on the dried basis. Freely soluble in water; insoluble in acetone, in ethyl acetate, and in benzene. pH of a 1% solution in water is between 6.5 and 8.5. Store in airtight containers.

Incompatibility.

For discussion of the incompatibility of aminoglycosides such as kanamycin with beta lactams, see under Gentamicin Sulfate. Kanamycin is also reported to be incompatible with various other drugs including some other antimicrobials as well as with some electrolytes.

💊 Adverse Effects, Treatment, and Precautions

As for Gentamicin Sulfate. For patients given standard regimens, peak plasma concentrations of kanamycin greater than 30 micrograms/mL, and trough concentrations greater than 10 micrograms/mL, should be avoided. Auditory (cochlear) toxicity is more frequent than vestibular toxicity. Local pain and inflammation, as well as bruising and haematoma, have been reported at the site of intramuscular injections. Gastrointestinal disturbances and a malabsorption syndrome, similar to that seen with oral neomycin, have occurred after oral kanamycin. Oral kanamycin should be avoided in patients with gastrointestinal ulceration.

Breast feeding.

Although kanamycin is distributed into breast milk1 the American Academy of Pediatrics states that no adverse effects have been seen in breast-fed infants whose mothers were receiving kanamycin, and therefore considers2 that its use is usually compatible with breast feeding.
1. Chyo N, et al. Clinical studies of kanamycin applied in the field of obstetrics and gynecology. Asian Med J 1962; 5: 265–75
2. American Academy of Pediatrics. The transfer of drugs and other chemicals into human milk. Pediatrics 2001; 108: 776–89. Correction. ibid.; 1029. Also available at: http://aappolicy.aappublications.org/cgi/content/full/ pediatrics%3b108/3/776 (accessed 27/05/04)

💊 Interactions

💊 Antimicrobial Action

As for Gentamicin Sulfate. It is active against a similar range of organisms although it is not active against Pseudomonas spp. Some strains of Mycobacterium tuberculosis are sensitive. Resistance has been reported in strains of many of the organisms normally sensitive to kanamycin, and at one time was widespread, but a decline in the use of kanamycin has meant that resistance has become somewhat less prevalent. Cross-resistance occurs between kanamycin and neomycin, framycetin, and paromomycin, and partial cross-resistance has been reported between kanamycin and streptomycin.
1. Ho YII, et al. In-vitro activities of aminoglycoside-aminocyclitols against mycobacteria. J Antimicrob Chemother 1997; 40: 27–32.

💊 Pharmacokinetics

As for Gentamicin Sulfate. Less than 1% of an oral dose is absorbed, although this may be significantly increased if the gastrointestinal mucosa is inflamed or ulcerated. After intramuscular injection peak plasma concentrations of kanamycin of about 20 and 30 micrograms/mL are attained in about 1 hour following doses of 0.5 and 1 g respectively. A plasma half-life of about 3 hours has been reported. Absorption after intraperitoneal instillation is similar to that from intramuscular doses. Kanamycin is rapidly excreted by glomerular filtration and most of a parenteral dose appears unchanged in the urine within 24 hours. It has been detected in cord blood and in breast milk.

💊 Uses and Administration

Kanamycin is an aminoglycoside antibacterial with actions similar to those of gentamicin. It has been used in the treatment of susceptible Gram-negative and staphylococcal infections, including gonorrhoea and neonatal gonococcal eye infections, although its use has declined in many centres because of the development of resistance. As with gentamicin it may be used with penicillins and with cephalosporins; the injections should be given at separate sites. Kanamycin has also been used as a second-line drug in tuberculosis, but other, safer drugs are usually preferred. The sulfate or acid sulfate salts are often used: in the USA, preparations containing the bisulfate (C18H36N4011,2H2SO4), but referred to as the sulfate, are available. Doses are expressed in terms of kanamycin base; 1.2 g of kanamycin sulfate, and 1.34 g of kanamycin acid sulfate, are each equivalent to about 1 g of kanamycin. It is usually given by intramuscular injection, and in acute infections adults may be given 15 mg/kg daily, to a maximum of 1.5 g daily, in 2 to 4 divided doses. The same doses may be given by intravenous infusion of a 0.25 to 0.5% solution over 30 to 60 minutes; in the UK, up to 30 mg/kg daily has been given in 2 or 3 divided doses by this route. Similar doses are used in children. Treatment of acute infections should preferably not continue for longer than 7 to 10 days or exceed a cumulative dose of 10 g kanamycin. A dose of 3 to 4 g weekly, given as 1 g on alternate days or as 1 g twice daily on 2 days each week, has been suggested in the UK for chronic bacterial infections, up to a maximum cumulative dose of 50 g, but prolonged use increases the risk of nephrotoxicity and is not generally recommended. A single intramuscular dose of 2 g of kanamycin has been used in the treatment of penicillin-resistant gonorrhoea. In the treatment and prophylaxis of neonatal gonococcal infections in infants born to mothers with gonorrhoea, 25 mg/kg, up to a maximum of 75 mg, may be given as a single intramuscular dose. Peak plasma concentrations greater than 30 micrograms/mL and trough concentrations greater than 10 micrograms/mL should be avoided. It is recommended that dosage should be adjusted in all patients according to plasma-kanamycin concentrations, and this is particularly important where factors such as age, renal impairment, or prolonged therapy may predispose to toxicity, or where there is a risk of subtherapeutic concentrations. For discussion of the methods of calculating aminoglycoside dosage requirements, see Administration and Dosage, under Gentamicin. Kanamycin has been used orally similarly to neomycin, for the suppression of intestinal flora. For pre-operative use, 1 g may be given every hour for 4 hours, then 1 g every 6 hours for 36 to 72 hours. In the management of hepatic encephalopathy, 8 to 12 g daily in divided doses may be given. Kanamycin has also been given in doses of 250 mg as a nebulised inhalation, 2 to 4 times daily. Solutions of kanamycin 0.25% have been used for the irrigation of body cavities. Kanamycin tannate has also been used.

💊 Preparations

USP 31: Kanamycin Injection; Kanamycin Sulfate Capsules.

Proprietary Preparations

Arg.: Cristalomicina; Ger.: Kan-Ophtal; Kana-Stulln; Kanamytrex; India: Kancin; Kaycin; Indon.: Kanabiotic; Kanarco; Kanoxin; Ital.: Keimicina; Malaysia: Kancin; Mex.: Cancina; Kanacil†; Kanadrex†; Kanapat; Kantrex; Randikan†; Solkan; Sulmyn; Singapore: Kancin-L; Kancin†; Spain: Kantrex†; Thai.: Anbikan; Kan-Mycin†; Kancin; Kangen; KMH; USA: Kantrex; Venez.: Kanacyl†; Kantrex. Multi-ingredient: Arg.: Cristalomicina; Fr.: Sterimycine†; Ital.: Dermaflogil; S.Afr.: Kantrexil; Spain: Kanafosal; Kanafosal Predni; Kanapomada; Naso Pekamin; Thai.: KA-Cilone; Venez.: Kanasone†; Monosulpa; Rinomax.
Published April 06, 2019.