カナマイシンA

Pharmaceuticals -> Antibiotics

Pharmaceuticals -> Listed in ZINC15

Crystals from ethanol

Crystals from methanol + ethanol

Breast Feeding; Lactation; Milk, Human; Anti-Infective Agents; Antibacterial Agents; Aminoglycosides

Ophthalmological preparations > Anti-infective agents

When heated to decomposition it emits toxic fumes of nitroxides.

Decomposes over a wide range above 250 °C. /Kanamycin sulfate/

Crystals, MP 172-192 °C (decomposes). Specific optical rotation: +130 deg at 18 °C/D (c = 0.5 in water); +114 deg at 21 °C/D (c = 0.98 in water). Soluble in water, formamide; slightly soluble in chloroform, isopropyl alcohol. Practically insoluble in the common alcohols and nonpolar solvents. /Kanamycin B/

Crystals from methanol + ethanol, decomposes above 270 °C. Specific optical rotation (H2O): +126 deg at 20 °C/D. Soluble in water, slightly soluble in formaldehyde. Practically insoluble in the common alcohols and nonpolar solvents. /Kanamycin C/

Specific optical rotation (0.1N H2SO4): +146 deg at 24 °C/D

White, odorless, crystalline powder. Decompses over a wide range above 250 °C, soluble in water, practically insoluble in methanol and ethanol. /Kanamycin sulfate/

Insoluble in acetone, ethyl acetate, benzene /Kanamycin sulfate/

Irregular prisms, decomposes over a wide range above 250 °C. Freely soluble in water. Practically insoluble in the common alcohols and nonpolar solvents. /Kanamycin A sulfate/

The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including kanamycin sulfate, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Kanamycin sulfate/

The Generic Animal Drug and Patent Restoration act requires that each sponsor of an approved animal drug must submit to the FDA certain information regarding patents held for the animal drug or its method of use. The Act requires that this information, as well as a list of all animal drug products approved for safety and effectiveness, be made available to the public. Kanamycin sulfate is included on this list. /Kanamycin sulfate/

Implantation or injectable dosage form new animal drugs. Kanamycin. ... Indications for use. For the treatment of bacterial infections due to kanamycin sensitive organisms in dogs and cats. ... Limitations. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Ophthalmic and topical dosage form new animal drugs. Kanamycin ophthalmic ointment. ... Indications for use. For the treatment of various eye infections (conjunctivitis, blepharitis, dacryocystitis, keratitis, and corneal ulcerations) due to bacteria sensitive to kanamycin. For prophylaxis in traumatic conditions, removal of foreign bodies, and intraocular surgery. ... Limitations. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Ophthalmic and topical dosage form new animal drugs. Kanamycin ophthalmic solution. ... Indications for use. For the treatment of various eye infections (conjunctivitis, blepharitis, dacryocystitis, keratitis, and corneal ulcerations) due to bacteria sensitive to kanamycin. For prophylaxis in traumatic conditions, removal of foreign bodies, and intraocular surgery. ... Limitations. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.

Concomitant and/or sequential use of an aminoglycoside and other systemic, oral, or topical drugs that have neurotoxic, ototoxic, or nephrotoxic effects (e.g., other aminoglycosides, acyclovir, amphotericin B, bacitracin, capreomycin, certain cephalosporins, colistin, cisplatin, methoxyflurane, polymyxin B, vancomycin) may result in additive toxicity and should be avoided, if possible. /Aminoglycosides/

Because of the possibility of an increased risk of ototoxicity due to additive effects or altered serum and tissue aminoglycoside concentrations, aminoglycosides should not be given concomitantly with potent diuretics such as ethacrynic acid, furosemide, urea, or mannitol. It has been suggested that concomitant use of certain anti-emetics that suppress nausea and vomiting of vestibular origin and vertigo (e.g., dimenhydrinate, meclizine) may mask symptoms of aminoglycoside-associated vestibular ototoxicity. /Aminoglycosides/

Concurrent use of an aminoglycoside with general anesthetics or neuromuscular blocking agents (e.g., succinylcholine, rocuronium, tubocurarine) may potentiate neuromuscular blockade and cause respiratory paralysis. ... Aminoglycosides should be used with caution in patients receiving anesthetics or neuromuscular blocking agents, and patients should be closely observed for signs of respiratory depression. /Aminoglycosides/

In vitro studies indicate that the antibacterial activity of aminoglycosides and beta-lactam antibiotics may be additive or synergistic against some organisms including Enterobacteriaceae, Pseudomonas aeruginosa, enterococci, and viridans streptococci. The synergistic effect of aminoglycosides and beta-lactams is used to therapeutic advantage, especially in the treatment of infections caused by enterococci or Ps. aeruginosa. Although the exact mechanism of this synergistic effect has not been determined, it appears that by inhibiting bacterial cell-wall synthesis the penicillin allows more effective ingress of the aminoglycoside to the ribosomal binding site. Synergism between aminoglycosides and extended-spectrum penicillins generally is unpredictable and antagonism has been reported rarely in vitro when these penicillins were used in conjunction with amikacin, gentamicin, or tobramycin. Therefore, some clinicians suggest that when concomitant therapy is indicated it may be advisable to use appropriate in vitro studies to demonstrate synergism against the isolated organism. Concomitant administration of an extended-spectrum penicillin and an aminoglycoside has resulted in decreased serum aminoglycoside concentrations and elimination half life, especially in patients with renal impairment. Therefore, serum aminoglycoside concentrations should be monitored in patients receiving concomitant therapy, especially when very high doses of an extended-spectrum penicillin are used or when the patient has impaired renal function. /Aminoglycosides/

For more Interactions (Complete) data for Kanamycin A (10 total), please visit the HSDB record page.

IDENTIFICATION AND USE: Kanamycin A is aminoglycoside anti-bacterial agent. Kanamycin injection is indicated in the short-term treatment of serious infections caused by susceptible strains of the designated microorganisms. Kanamycin may be considered as initial therapy in the treatment of infections where one or more of the following are the known or suspected pathogens: E. coli, Proteus species (both indole-positive and indole-negative), Enterobacter aerogenes, Klebsiella pneumoniae, Serratia marcescens, Acinetobacter species. HUMAN EXPOSURE AND TOXICITY: Toxic effects of kanamycin on the eighth cranial nerve can result in partially reversible or irreversible bilateral loss of hearing, loss of balance, or both. Tinnitus or vertigo may or may not be experienced. Cochlear damage is usually manifested initially by small changes in audiometric test results at the high frequencies and may not be associated with subjective hearing loss. Vestibular dysfunction is usually manifested by nystagmus, vertigo, nausea, vomiting, or acute Meniere's syndrome. Serious sensitivity reactions, such as anaphylaxis and dermatologic reactions including exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, angioedema, and Stevens-Johnson syndrome, have been reported rarely in patients receiving aminoglycosides; fatalities have occurred rarely. Cross-sensitivity occurs among the aminoglycosides. ANIMAL STUDIES: Intravitreal injection in rabbits and owl monkeys was tolerated at a dose of 0.5 mg, but 1.5 to 6.0 mg produced cataracts in rabbits. Dosages of 200 mg/kg/day in pregnant rats and pregnant guinea pigs led to hearing impairment in the offspring.

/SIGNS AND SYMPTOMS/ Toxic effects of kanamycin on the eighth cranial nerve can result in partially reversible or irreversible bilateral loss of hearing, loss of balance, or both. Tinnitus or vertigo may or may not be experienced. Cochlear damage is usually manifested initially by small changes in audiometric test results at the high frequencies and may not be associated with subjective hearing loss. Vestibular dysfunction is usually manifested by nystagmus, vertigo, nausea, vomiting, or acute Meniere's syndrome.

/SIGNS AND SYMPTOMS/ Serious sensitivity reactions, such as anaphylaxis and dermatologic reactions including exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, angioedema, and Stevens-Johnson syndrome, have been reported rarely in patients receiving aminoglycosides; fatalities have occurred rarely. Cross-sensitivity occurs among the aminoglycosides. /Aminoglycosides/

/EPIDEMIOLOGY STUDIES/ Amikacin and kanamycin are mainly used for treating multidrug-resistant tuberculosis (MDR-TB), especially in developing countries where the burden of MDR-TB is highest. Their protracted use in MDR-TB treatment is known to cause dose-dependent irreversible hearing loss, requiring hearing aids, cochlear implants or rehabilitation. Therapeutic drug monitoring and regular audiological assessments may help to prevent or detect the onset of hearing loss, but these services are not always available or affordable in many developing countries. We aimed to compare the cumulative incidence of hearing loss among patients treated for MDR-TB with amikacin or kanamycin-based regimens, and to identify the most-at-risk patients, based on the real-life clinical practice experiences in Namibia. We conducted a retrospective cohort study of patients treated with amikacin or kanamycin-based regimens in four public sector MDR-TB treatment sites in Namibia between June 2004 and March 2014. Patients were audiologically assessed as part of clinical care. The study outcome was the occurrence of any hearing loss. Data were manually extracted from patients' treatment records. We compared proportions using the Chi-square test; applied stratified analysis and logistic regression to study the risk of hearing loss and to identify the most-at-risk patients through effect-modification analysis. A P-value<0.05 was statistically significant. All 353 patients had normal baseline hearing, 46% were HIV co-infected. Cumulative incidence of any hearing loss was 58%, which was mostly bilateral (83%), and mild (32%), moderate (23%), moderate-severe (1%), severe (10%), or profound (15%). Patients using amikacin had a greater risk of developing the more severe forms of hearing loss than those using kanamycin (adjusted odds ratio (OR)=4.0, 95 % CI: 1.5-10.8). Patients co-infected with HIV (OR=3.4, 95 % CI: 1.1-10.6), males (OR=4.5, 95 %1.5-13.4) and those with lower baseline body weight (40-59 kg, OR=2.8, 95 % CI: 1.1-6.8), were most-at-risk of developing hearing loss. Amikacin use in the long-term MDR-TB treatment led to a higher risk of occurrence of the more severe forms of hearing loss compared to kanamycin use. Males, patients with low baseline body weight and those co-infected with HIV were most-at-risk. MDR-TB treatment programs should consider replacing amikacin with kanamycin and strengthen the routine renal, serum therapeutic drug levels and audiometric monitoring in the most-at-risk patients treated with aminoglycosides.

/EPIDEMIOLOGY STUDIES/ Quantitative assessments of vestibular hair cells and Scarpa's ganglion cells were performed on 17 temporal bones from 10 individuals who had well-documented clinical evidence of aminoglycoside ototoxicity (streptomycin, kanamycin, and neomycin). Assessment of vestibular hair cells was performed by Nomarski (differential interference contrast) microscopy. Hair cell counts were expressed as densities (number of cells per 0.01 sq mm surface area of the sensory epithelium). The results were compared with age-matched normal data. Streptomycin caused a significant loss of both type I and type II hair cells in all 5 vestibular sense organs. In comparing the ototoxic effect on type I versus type II hair cells, there was greater type I hair cell loss for all 3 cristae, but not for the maculae. The vestibular ototoxic effects of kanamycin appeared to be similar to those of streptomycin, but the small sample size precluded definitive conclusions from being made. Neomycin did not cause loss of vestibular hair cells. Within the limits of this study (maximum postototoxicity survival time of 12 months), there was no significant loss of Scarpa's ganglion cells for any of the 3 drugs. The findings have implications in several clinical areas, including the correlation of vestibular test results to pathological findings, the rehabilitation of patients with vestibular ototoxicity, the use of aminoglycosides to treat Meniere's disease, and the development of a vestibular prosthesis.

/OTHER TOXICITY INFORMATION/ Aminoglycosides can cause fetal harm when administered to pregnant women. Aminoglycoside antibiotics cross the placenta and there have been several reports of total, irreversible, bilateral congenital deafness in children whose mothers received streptomycin during pregnancy. Although serious side effects to fetus or newborn have not been reported in treatment of pregnant women with other aminoglycosides, the potential for harm exists. /Aminoglycosides/

Drug Induced Liver Injury Rank (DILIrank 2.0)

Kanamycin

vNo-DILI-concern

0

No match

DOI:10.1016/j.drudis.2016.02.015

/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Aminoglycosides nephrotoxicity limits their use in clinical practice. Growth hormone-releasing peptide-6 (GHRP6) and epidermal growth factor (EGF) have proven cytoprotective effects in various tissues, including the kidney. This study aimed to determine the cytoprotective effect of EGF and GHRP6 on glomerular, proximal tubular, and interstitial morphology in rats treated with an overdose of kanamycin. Forty-four male Wistar adults rats were submitted to treatment for 20 days with sodium phosphate saline buffer (control group), kanamycin (kanamycin group), kanamycin and EGF (EGF group), kanamycin and GHRP6 (GHRP6 group), kanamycin, EGF, and GHRP6 (EGF-GHRP6 group). The kidneys were studied both during acute kidney injury (n = 19) and recovery phases (n = 25). The percentages of glomerular damage, tubular damage (reversible and irreversible changes), and interstitial damage were quantified in 10 histological fields per kidney using paraffin-embedded sections. The damage in the glomeruli, proximal tubules, and interstitium was less in the groups treated with the cytoprotective treatments than in kanamycin group during acute kidney injury. During the recovery phase, normal structure of several glomeruli and the interstitium was appreciated in the EGF and GHRP6 groups, although tissue repair was not as complete as it in the EGF-GHRP6 group. In the recovery phase, cytoprotective treatments accelerated the recovery of tubular damage and reversible tubular changes prevailed. These results confirm the cytoprotective properties of EGF and GHRP6 alone and in combination and suggest the possibility of using these agents to accelerate kidney tissue repair after aminoglycoside-induced renal damage.

/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ The aim of the present study was to assess the ototoxicity of kanamycin sulfate (KM) in adult rats and its underlying mechanism. Forty male Sprague-Dawley rats (6-7 weeks old) were randomly divided into the experimental group and the control group. The animals in the experimental group were injected subcutaneously with KM (500 mg/kg per day) for two weeks, and the control group received equal volume of normal saline. To assess the ototoxicity of KM, the auditory brainstem response (ABR) was recorded to monitor the changes in hearing thresholds, and the density of spiral ganglion cells (SGCs) and morphology of cochlea were observed using surface preparations and frozen sections of cochlea. The results showed that the hearing threshold of rats in the experimental group was elevated by more than 60 dB across all the frequencies two weeks after the first administration of KM. And in the experimental group, the density of SGCs became lower, and organ of Corti suffered loss of hair cells. The loss of outer hair cells (OHCs) was more severe than that of inner hair cells (IHCs), correlated with the density decrease of SGCs. We conclude that the ototoxicity of KM in the adult rats was apparent and the underlying mechanism is associated with the loss of SGCs and hair cells.

/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ We investigated the time course of the plasticity in fusiform cell (FC) and at auditory nerve (AN) synapse on FC (AN/FC synapse) following chronic kanamycin-induced deafness. Guinea pigs were treated with kanamycin sulfate by subcutaneous injection at dose of 500 mg/kg/day for 7 days. Ultrastructural changes in FC and AN/FC synapse were observed, and local insulin-like growth factor 1 (IGF-1) mRNA was quantified using quantitative real time PCR at 1, 7, 14, 28, 70 and 140 days after kanamycin treatment. The average threshold was 46.46+/-3.45, 80.63+/-5.95 and 103.95+/-6.59 dB SPL respectively at 1, 7 and 14 days, and the threshold was statistically unchanged at 28, 70 and 140 days in comparison with the 14 day group. Mitochondrial swelling in FC and at AN/FC synapse was progressive at 7, 14 and 28 days. Moreover, the thickness of the postsynaptic densities increased at 1, 7 and 14 days. Finally, there was a persistent upregulation in local IGF-1 mRNA at 7, 14, 28 and 70 days. These changes in the ultrastructure of AN/FC synapse and FC, and upregulation of local IGF-1 mRNA were no longer present at 140 days. Our results indicate that the effects of kanamycin on the ultrastructure of FC and AN/FC synapse are progressive. However, FC and AN/FC synapse are capable of reviving and remodeling after kanamycin-induced lesion and incomplete deafferentation. Additionally, local IGF-1 might play a role in the lesion- and deafness-induced plasticity in FC and at AN/FC synapse following chronic kanamycin-induced deafness.

/LABORATORY ANIMALS: Chronic Exposure or Carcinogenicity/ Intravitreal injection in rabbits and owl monkeys was tolerated at a dose of 0.5 mg, but 1.5 to 6.0 mg produced cataracts in rabbits.

For more Non-Human Toxicity Excerpts (Complete) data for Kanamycin A (9 total), please visit the HSDB record page.

Aminoglycosides should be used with caution in prematures and neonates because of the renal immaturity of these patients and the resulting prolongation of serum half-life of these drugs.

Kanamycin has the potential to induce auditory and sometimes vestibular toxicity, renal toxicity, and neuromuscular blockade. The risks are higher for patients with a present or past history of renal impairment (especially if hemodialysis is required) ... .

The risk of ototoxicity and nephrotoxicity is greatest in patients with past or present histories of renal impairment, dehydration, or previous exposure to ototoxic drugs and in those who receive high dosage or prolonged treatment. In addition, patients with preexisting tinnitus, vertigo, or subclinical high-frequency hearing loss are especially susceptible to ototoxicity and should be carefully observed for signs of eighth cranial nerve damage during aminoglycoside therapy. /Aminoglycosides/

Aminoglycosides should be used with caution in patients with neuromuscular disorder such as myasthenia gravis or parkinsonian syndrome, since the drugs may aggravate muscle weakness as a result of their potential to produce neuromuscular blockade. If signs of respiratory paralysis occur during aminoglycoside therapy, respiration should be assisted and the drug discontinued. /Aminoglycosides/

In the event of overdosage or toxic reaction, hemodialysis or peritoneal dialysis will aid in the removal of kanamycin from the blood. In the newborn infant, exchange transfusion may also be considered.

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/

/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W TKO /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/

LD50 Rat iv 437 mg/kg

LD50 Rabbit iv 150 mg/kg

LD50 Mouse iv 115 mg/kg

LD50 Mouse sc 1350 mg/kg

For more Non-Human Toxicity Values (Complete) data for Kanamycin A (7 total), please visit the HSDB record page.

The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including kanamycin sulfate, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Kanamycin sulfate/

The Generic Animal Drug and Patent Restoration act requires that each sponsor of an approved animal drug must submit to the FDA certain information regarding patents held for the animal drug or its method of use. The Act requires that this information, as well as a list of all animal drug products approved for safety and effectiveness, be made available to the public. Kanamycin sulfate is included on this list. /Kanamycin sulfate/

Implantation or injectable dosage form new animal drugs. Kanamycin. ... Indications for use. For the treatment of bacterial infections due to kanamycin sensitive organisms in dogs and cats. ... Limitations. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Ophthalmic and topical dosage form new animal drugs. Kanamycin ophthalmic ointment. ... Indications for use. For the treatment of various eye infections (conjunctivitis, blepharitis, dacryocystitis, keratitis, and corneal ulcerations) due to bacteria sensitive to kanamycin. For prophylaxis in traumatic conditions, removal of foreign bodies, and intraocular surgery. ... Limitations. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

Ophthalmic and topical dosage form new animal drugs. Kanamycin ophthalmic solution. ... Indications for use. For the treatment of various eye infections (conjunctivitis, blepharitis, dacryocystitis, keratitis, and corneal ulcerations) due to bacteria sensitive to kanamycin. For prophylaxis in traumatic conditions, removal of foreign bodies, and intraocular surgery. ... Limitations. Federal law restricts this drug to use by or on the order of a licensed veterinarian.

S - Sensory organs

J - Antiinfectives for systemic use

A - Alimentary tract and metabolism

QJ - Antiinfectives for systemic use

QA - Alimentary tract and metabolism

QS - Sensory organs

Kanamycin is an aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses.

Aminoglycosides like kanamycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Kanamycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.

Kanamycin, an aminoglycoside, acts by inhibiting the synthesis of protein in susceptible microorganisms. It is bactericidal in vitro against Gram-negative bacteria and certain Gram-positive bacteria.

Aminoglycosides are usually bactericidal in action. Although the exact mechanism of action has not been fully elucidated, the drugs appear to inhibit protein synthesis in susceptible bacteria by irreversibly binding to 30S ribosomal subunits. /Aminoglycosides/

... Aminoglycosides are aminocyclitols that kill bacteria by inhibiting protein synthesis as they bind to the 16S rRNA and by disrupting the integrity of bacterial cell membrane. Aminoglycoside resistance mechanisms include: (a) the deactivation of aminoglycosides by N-acetylation, adenylylation or O-phosphorylation, (b) the reduction of the intracellular concentration of aminoglycosides by changes in outer membrane permeability, decreased inner membrane transport, active efflux, and drug trapping, (c) the alteration of the 30S ribosomal subunit target by mutation, and (d) methylation of the aminoglycoside binding site. ... /Aminoglycosides/

2.5 hours

The plasma elimination half-life of kanamycin is 2-4 hours in adults with normal renal function, but may be prolonged in geriatric patients. In neonates 1-7 days of age, half-life averaged 4.3-5.1 hours. In premature infants, the elimination half-life of kanamycin reportedly averages 9 hours. In patients with severe burns, plasma half-life and plasma concentrations of the drug may be decreased. Plasma concentrations are higher and the elimination half-life of kanamycin is prolonged in patients with renal impairment. In those with severe renal impairment, the plasma half-life of kanamycin may range from 27-80 hours.

RUC37XUP2P

KANAMYCIN

Established Pharmacologic Class [EPC] - Aminoglycoside Antibacterial

Chemical Structure [CS] - Aminoglycosides

Kanamycin is an Aminoglycoside Antibacterial.

Compounds which inhibit the synthesis of proteins. They are usually ANTI-BACTERIAL AGENTS or toxins. Mechanism of the action of inhibition includes the interruption of peptide-chain elongation, the blocking the A site of ribosomes, the misreading of the genetic code or the prevention of the attachment of oligosaccharide side chains to glycoproteins.

Substances that inhibit the growth or reproduction of BACTERIA.

Kanamycin is rapidly absorbed after intramuscular injection and peak serum levels are generally reached within approximately one hour. Poor oral and topical absorption except with severe skin damage.

In one study in premature infants, peak plasma kanamycin concentrations averaging 17.5 ug/mL were attained within 1 hour following IM administration of a single kanamycin dose of 6.3-8.5 mg/kg; plasma concentrations of the drug averaged 5.8 ug/mL at 12 hours. In neonates 1-7 days of age, peak serum concentrations 30 minutes after a 7.5-mg/kg or 10-mg/kg IM dose were 21.8 or 26.8 ug/mL, respectively. When these doses were given by IV infusion over 20 minutes, serum concentrations at 30 minutes were 21.4 or 29.3 ug/mL, respectively.

Kanamycin is poorly absorbed from the GI tract.

In one study, intraperitoneal instillation of 500 mg of kanamycin diluted in 20 mL of 0.9% sodium chloride resulted in peak plasma kanamycin concentrations of 19 ug/mL within 15 minutes.

Kanamycin is rapidly absorbed after IM injection. Following IM administration of a single 7.5-mg/kg dose of kanamycin in adults with normal renal function, peak plasma kanamycin concentrations are attained within approximately 1 hour and average 22 ug/mL;1 at 8 hours after the dose, plasma concentrations of the drug average 3.2 ug/mL.1 Similar plasma concentrations of kanamycin are attained when the same dose is administered by IV infusion over 1 hour.

For more Absorption, Distribution and Excretion (Complete) data for Kanamycin A (11 total), please visit the HSDB record page.

MEDICATION

MEDICATION (VET)

Anti-Bacterial Agents; Protein Synthesis Inhibitors

Use (kg; approx.) in Germany (2009): >10

Table: Kanamycin Sulfate Preparations [Table#4440]

Grade: USP. /Kanamycin sulfate/

D-Streptamine, O-3-amino-3-deoxy-.alpha.-D-glucopyranosyl-(1.fwdarw.6)-O-[6-amino-6-deoxy-.alpha.-D-glucopyranosyl-(1.fwdarw.4)]-2-deoxy-: ACTIVE

Kanamycin (8063-07-80) is an antibiotic complex produced by Streptomyces kanamyceticus and consists primarily of kanamycin A and two minor components, one of which is designated kanamycin B.