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Pronunciation |
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(kan
a MYE
sin) |
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U.S. Brand
Names |
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Kantrex® |
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Generic
Available |
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Yes |
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Synonyms |
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Kanamycin Sulfate |
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Pharmacological Index |
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Antibiotic, Aminoglycoside |
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Use |
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Oral: Preoperative bowel preparation in the prophylaxis of infections and
adjunctive treatment of hepatic coma (oral kanamycin is not indicated in the
treatment of systemic infections); treatment of susceptible bacterial infection
including gram-negative aerobes, gram-positive Bacillus as well as some
mycobacteria
Parenteral: Rarely used in antibiotic irrigations during surgery
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Pregnancy Risk
Factor |
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D |
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Contraindications |
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Hypersensitivity to kanamycin or any component or other
aminoglycosides |
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Warnings/Precautions |
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Use with caution in patients with pre-existing renal insufficiency,
vestibular or cochlear impairment, myasthenia gravis, conditions which depress
neuromuscular transmission |
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Adverse
Reactions |
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Percentage unknown: Edema, neurotoxicity, drowsiness, headache, pseudomotor
cerebri, skin itching, redness, rash, photosensitivity, erythema, nausea,
vomiting, diarrhea (most common with oral form), malabsorption syndrome with
prolonged and high-dose therapy of hepatic coma; anorexia, weight loss,
increased salivation, enterocolitis, granulocytopenia, agranulocytosis,
thrombocytopenia, burning, stinging, weakness, tremors, muscle cramps,
ototoxicity (auditory), ototoxicity (vestibular), nephrotoxicity,
dyspnea |
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Overdosage/Toxicology |
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Symptoms of overdose include ototoxicity, nephrotoxicity, and neuromuscular
toxicity
The treatment of choice following a single acute overdose appears to be the
maintenance of good urine output of at least 3 mL/kg/hour. Dialysis is of
questionable value in the enhancement of aminoglycoside elimination. If
required, hemodialysis is preferred over peritoneal dialysis in patients with
normal renal function. Careful hydration may be all that is required to promote
diuresis and, therefore, the enhancement of the drug's elimination.
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Drug
Interactions |
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Increased toxicity:
Penicillins, cephalosporins, amphotericin B, diuretics may increase
nephrotoxicity; polypeptide antibiotics may increase risk of respiratory
paralysis and renal dysfunction
Neuromuscular blocking agents with oral kanamycin may increase neuromuscular
blockade; a small increase in warfarin's effect may occur due to decreased
absorption of vitamin K
Decreased toxicity: Methotrexate with kanamycin (oral) may be less well
absorbed as may digoxin (minor) and vitamin A |
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Stability |
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Darkening of vials does not indicate loss of potency |
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Mechanism of
Action |
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Interferes with protein synthesis in bacterial cell by binding to ribosomal
subunit |
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Pharmacodynamics/Kinetics |
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Absorption: Oral: Not absorbed following administration
Relative diffusion of antimicrobial agents from blood into cerebrospinal
fluid (CSF): Good only with inflammation (exceeds usual MICs)
Ratio of CSF to blood level (%): Normal meninges: Nil; Inflamed meninges: 43
Half-life: 2-4 hours, increases in anuria to 80 hours
End-stage renal disease: 40-96 hours
Time to peak serum concentration: I.M.: 1-2 hours
Elimination: Entirely in the kidney, principally by glomerular filtration
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Usual Dosage |
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Children: Infections: I.M., I.V.: 15 mg/kg/day in divided doses every 8-12
hours
Adults:
Infections: I.M., I.V.: 5-7.5 mg/kg/dose in divided doses every 8-12 hours
(<15 mg/kg/day)
Preoperative intestinal antisepsis: Oral: 1 g every 4-6 hours for 36-72 hours
Hepatic coma: Oral: 8-12 g/day in divided doses
Intraperitoneal: After contamination in surgery: 500 mg diluted in 20 mL
distilled water; other irrigations: 0.25% solutions
Aerosol: 250 mg 2-4 times/day (250 mg diluted with 3 mL of NS and nebulized)
Dosing adjustment/interval in renal impairment:
Clcr 50-80 mL/minute: Administer 60% to 90% of dose or administer
every 8-12 hours
Clcr 10-50 mL/minute: Administer 30% to 70% of dose or administer
every 12 hours
Clcr <10 mL/minute: Administer 20% to 30% of dose or administer
every 24-48 hours
Hemodialysis: Dialyzable (50% to 100%) |
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Monitoring
Parameters |
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Serum creatinine and BUN every 2-3 days; peak and trough concentrations;
hearing |
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Reference Range |
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Therapeutic: Peak: 25-35 mg/mL; Trough: 4-8
mg/mL; Toxic: Peak: >35
mg/mL;
Trough: >10 mg/mL |
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Mental Health: Effects
on Mental Status |
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May cause drowsiness or dizziness; case reports of delirium and psychosis
with aminoglycosides |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause agranulocytosis; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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It is important to maintain adequate hydration (2-3 L/day of fluids unless
instructed to restrict fluid intake). Report change in hearing acuity, ringing
or roaring in ears, alteration in balance, vertigo, feeling of fullness in head;
pain, tingling, or numbness of any body part; change in urinary pattern or
decrease in urine; signs of opportunistic infection (eg, white plaques in mouth,
vaginal discharge, unhealed sores, sore throat, unusual fever, chills); pain,
redness, or swelling at injection site; skin rash; or other adverse reactions.
Pregnancy precautions: Do not get pregnant during therapy with this
medication; use appropriate barrier contraceptive measures. |
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Nursing
Implications |
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Aminoglycoside levels in blood taken from Silastic®
central catheters can sometime give falsely high readings. Administer
around-the-clock rather than 4 times/day, 3 times/day, etc, (ie, 12-6-12-6, not
9-1-5-9) to promote less variation in peak and trough serum levels; modify
dosage in patients with renal impairment; I.M. doses should be administered in a
large muscle mass (ie, gluteus maximus). |
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Dosage Forms |
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Capsule, as sulfate: 500 mg
Injection, as sulfate:
Pediatric: 75 mg (2 mL)
Adults: 500 mg (2 mL); 1 g (3 mL) |
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References |
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Begg EJ and Barclay ML, "Aminoglycosides - 50 Years On," Br J Clin
Pharmacol, 1995, 39(6):597-603.
Cunha BA, "Aminoglycosides: Current Role in Antimicrobial Therapy,"
Pharmacotherapy, 1988, 8(6):334-50.
"Drugs for Tuberculosis," Med Lett Drugs Ther, 1993, 35(908):99-101.
Iseman MD, "Treatment of Multidrug-Resistant Tuberculosis," N Engl J
Med, 1993, 329(11):784-91.
Kristensen M, Molholm HJ, Kampmann J, et al,
"Letter: Drug Elimination and Renal Function," J Clin Pharmacol, 1974,
14(5-6):307-8.
Yasuhara H, Kobayashi S, Sakamoto K, et al,
"Pharmacokinetics of Amikacin and Cephalothin in Bedridden Elderly Patients,"
J Clin Pharmacol, 1982, 22:403-9.
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