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The Journal of Antibiotics Aug 1976A radioimmunoassay (RIA) has been developed using 125I-amikacin. Amikacin was iodinated by a modified BOLTON and HUNTER method. Dextran-charcoal was used to separate... (Comparative Study)
Comparative Study
A radioimmunoassay (RIA) has been developed using 125I-amikacin. Amikacin was iodinated by a modified BOLTON and HUNTER method. Dextran-charcoal was used to separate bound from free drug. The standard curve was linear on a logit-log plot in the range of 0.5 ng to 4 ng amikacin per tube. There was no cross-reactivity of amikacin antisera to the amino-glycosides gentamicin, tobramycin, netilmicin, and sisomicin but a 70% cross-reaction was observed with kanamycin, the compound from which amikacin is synthetically derived. Correlation of the RIA with a microbioassay for the determination of serum amikacin levels in 18 patient samples was excellent (r = 0.94). This new RIA technique is more sensitive, rapid, versatile, and less costly than the RIA using 3H-amikacin, and is far more sensitive and faster than microbioassay.
Topics: Amikacin; Animals; Antibody Specificity; Biological Assay; Immunization; Iodine Radioisotopes; Kanamycin; Methods; Rabbits; Radioimmunoassay
PubMed: 1033175
DOI: 10.7164/antibiotics.29.829 -
Antibiotiki I Khimioterapiia =... 2002
Review
Topics: Amikacin; Anti-Bacterial Agents; Bacteria, Anaerobic; Drug Resistance, Bacterial; Drug Therapy, Combination; Gram-Negative Bacteria; Gram-Positive Bacteria; Humans
PubMed: 12365326
DOI: No ID Found -
Medecine Et Maladies Infectieuses Sep 2016To evaluate the efficacy of amikacin on sputum conversion during initial sputum smear positive tuberculosis treatment. (Comparative Study)
Comparative Study Observational Study
OBJECTIVE
To evaluate the efficacy of amikacin on sputum conversion during initial sputum smear positive tuberculosis treatment.
MATERIAL AND METHODS
Single-center observational cohort study (2012-2013) evaluating time to sputum smear conversion with standard treatment (ST) versus standard treatment+amikacin (IV 15mg/kg/day) for seven days (STamK).
RESULTS
Forty-five patients were included. Median time to smear negative samples was 26.5 days (14-56) for the 30 (66.7%) patients included in the ST group and 48 days (19.5-69.5) for the 15 patients (33.3%) included in the STamK group (P=0.76). Time to negative culture was only known for 27 patients (61.4%): 47.5 days (26-58) for 18 patients in the ST group and 40 days (14-77) for nine patients in the STamK group.
CONCLUSION
Despite our small sample size, the addition of amikacin in active tuberculosis treatment did not seem to impact time to smear conversion or period of contagiousness.
Topics: Adult; Amikacin; Antitubercular Agents; Bacterial Load; Drug Administration Schedule; Drug Therapy, Combination; Female; Humans; Male; Middle Aged; Mycobacterium tuberculosis; Patient Isolation; Sputum; Time Factors; Tuberculosis, Pulmonary
PubMed: 27235009
DOI: 10.1016/j.medmal.2016.04.010 -
Pediatrie 1989A study was carried out to determine amikacin blood levels in 44 neonates who were admitted to a Pediatric Intensive Care Unit. Amikacin was administered by intravenous... (Comparative Study)
Comparative Study Review
A study was carried out to determine amikacin blood levels in 44 neonates who were admitted to a Pediatric Intensive Care Unit. Amikacin was administered by intravenous or intramuscular route. The levels obtained with both methods were similar. The results of our study indicate that amikacin levels should be monitored in neonates to avoid toxic concentrations of this drug. On the basis of this study a new neonatal dosage schedule is proposed.
Topics: Amikacin; Bacterial Infections; Ear; Humans; Infant, Newborn; Injections, Intramuscular; Injections, Intravenous; Intensive Care Units, Neonatal; Kidney; Prospective Studies
PubMed: 2654876
DOI: No ID Found -
Antimicrobial Agents and Chemotherapy Aug 1989Efficacy of liposome-encapsulated amikacin and free amikacin against Mycobacterium avium complex was evaluated in the beige mouse (C57BL/6J-bgJ/bgJ) acute infection... (Comparative Study)
Comparative Study
Efficacy of liposome-encapsulated amikacin and free amikacin against Mycobacterium avium complex was evaluated in the beige mouse (C57BL/6J-bgJ/bgJ) acute infection model. Approximately 10(7) viable M. avium complex serotype 1 cells for which the MIC of amikacin was 8 micrograms/ml were given intravenously. Treatment was started with encapsulated or free amikacin at approximately 110 or 40 mg/kg of body weight 7 or 14 days later. In the former experiment, treatment was given two or three times per week. In the latter experiment, treatment was given daily for 5 days. The animals were sacrificed 5 days after the last dose. Liver, spleen, and lung were homogenized, and viable cell counts were determined on 7H10 agar. An analysis of variance and subsequent Tukey HSD (honestly significant difference) tests indicated that both encapsulated and free amikacin significantly reduced viable cell counts in each of the organs compared with counts in the control group. Compared with free amikacin, encapsulated amikacin significantly reduced viable cell counts in the liver and spleen. Liposome encapsulation of an active agent appears to be a promising therapeutic approach to M. avium complex infection.
Topics: Amikacin; Animals; Culture Media; Liposomes; Liver; Lung; Male; Mice; Mice, Inbred C57BL; Mycobacterium avium-intracellulare Infection; Spleen; Time Factors
PubMed: 2802546
DOI: 10.1128/AAC.33.8.1179 -
JAMA Sep 1982Amikacin sulfate was first used sparingly at our cancer center in 1976; since 1979, it has been the only aminoglycoside used for systemic cancer therapy for patients... (Comparative Study)
Comparative Study
Amikacin sulfate was first used sparingly at our cancer center in 1976; since 1979, it has been the only aminoglycoside used for systemic cancer therapy for patients with granulocytopenia. As the development of resistance has been correlated with antibiotic use over time, we wished to determine if prolonged use of amikacin in our patients had led to increased amikacin resistance. A total of 1,129 strains were recovered from 315 patients during a 13-month period. Each species isolated per patient was considered once. Seven percent of the patients had amikacin-resistant strains (2.7% of isolates), and 10% of patients had gentamicin-resistant strains (4% of isolates). Amikacin resistance was significantly less than in an earlier study. Unrestricted use of amikacin has not led to a concomitant increase in amikacin resistance in gram-negative bacilli.
Topics: Amikacin; Aminoglycosides; Bacterial Infections; Drug Resistance, Microbial; Enterobacteriaceae; Gentamicins; Humans; Kanamycin; Neoplasms; Pseudomonas aeruginosa; Time Factors
PubMed: 6809965
DOI: 10.1001/jama.248.10.1199 -
European Journal of Pharmaceutics and... May 2021The aim was to develop a self-emulsifying drug delivery system (SEDDS) for amikacin via imine bond formation with hydrophobic aldehydes.
AIM
The aim was to develop a self-emulsifying drug delivery system (SEDDS) for amikacin via imine bond formation with hydrophobic aldehydes.
METHODS
Trans-2, cis-6-nonadienal, trans-cinnamaldehyde, citral and benzaldehyde were conjugated to amikacin at pH 8.5. Based on results of precipitation efficiency, Fourier-transform infrared spectroscopy (FTIR) and NMR analysis, amikacin-trans-cinnamaldehyde conjugates were further characterized regarding log P via HPLC. The release of amikacin from the amikacin-trans-cinnamaldehyde conjugates was examined through in vitro incubation with bovine serum albumin (BSA). SEDDS containing the amikacin-trans-cinnamaldehyde conjugates were tested regarding mean droplet size (MDS), polydispersity index (PDI), log D and cell viability.
RESULTS
Trans-cinnamaldehyde formed the most hydrophobic conjugates with amikacin whereas benzaldehyde did not form hydrophobic conjugates at all. Imine bond formation was confirmed by FTIR and NMR analysis. The highest increase in log P was achieved for the amikacin-trans-cinnamaldehyde conjugate in a molar ratio of 1:5, shifting from -8.58 up to 1.59. Incubation of this conjugate with BSA led to the formation of BSA-trans-cinnamaldehyde releasing in turn amikacin. SEDDS based on Capmul MCM, Cremophor EL and propylene glycol containing the conjugate demonstrated a MDS of 61.4 nm and PDI of 0.265. Log D was calculated to be 3.38. Cell viability studies showed very good tolerability of conjugate loaded SEDDS in concentrations of 0.1% - 0.5%.
CONCLUSION
Imine bond formation of amikacin with trans-cinnamaldehyde and the incorporation of the resulting conjugate into SEDDS represents a promising strategy for oral delivery of amikacin.
Topics: Acrolein; Administration, Oral; Amikacin; Benzaldehydes; Caco-2 Cells; Drug Carriers; Drug Liberation; Emulsions; Humans; Hydrophobic and Hydrophilic Interactions; Permeability; Serum Albumin, Bovine; Solubility; Toxicity Tests, Acute
PubMed: 33737147
DOI: 10.1016/j.ejpb.2021.03.001 -
The Journal of Antibiotics Jul 1990The synthesis and biological activity of kanamycin A derivatives with an omega-amino-alpha-fluoroalkanoyl side chain on the 1-amino group are described. The fluorinated...
The synthesis and biological activity of kanamycin A derivatives with an omega-amino-alpha-fluoroalkanoyl side chain on the 1-amino group are described. The fluorinated amino acids (4) for the side chain were prepared by fluorination of the alpha-hydroxy esters (2) with diethylaminosulfur trifluoride (DAST) with accompanying the Walden inversion. The reaction products varied with the amino protective groups employed, chain length of the alkanoic acids and the presence or absence of base. The fluorinated side chain was introduced to 1-free-NH2 kanamycin A (12) by the conventional active ester method and subsequent deblocking reactions afforded the desired final products (13-17). Of the derivatives prepared, 1-N-[(S)-4-amino-2-fluorobutyryl]kanamycin A (2'''-deoxy-2'''-fluoroamikacin, 14) showed the best overall activity profile, nearly the same as that of amikacin. Preparation and antibacterial activity of several aminoglycoside antibiotics with the 1-N-(S)-4-amino-2-fluorobutyryl side chain are also discussed.
Topics: Amikacin; Animals; Bacteria; Chemical Phenomena; Chemistry; Diethylamines; Fluorine; Indicators and Reagents; Mice; Molecular Conformation; Molecular Structure
PubMed: 2387779
DOI: 10.7164/antibiotics.43.858 -
Journal of Clinical Pharmacology 1984The concentrations of amikacin in serum, gallbladder, and common duct bile, and gallbladder tissue in patients undergoing surgery of the biliary tract were investigated....
The concentrations of amikacin in serum, gallbladder, and common duct bile, and gallbladder tissue in patients undergoing surgery of the biliary tract were investigated. Patients received 500 mg amikacin intravenously or intramuscularly from 1 to 11 hours before surgery. Another group had T-tubes inserted and blood and bile levels were studied serially postoperatively. One half hour after 500 mg amikacin, serum levels were high and bile levels were 30 per cent of the serum levels, with tissue levels less than 19 per cent of the serum levels. At 6 hours, serum levels were 37 per cent of the 1-hour levels; however, bile levels were 34 per cent of the simultaneous serum levels. At 11 hours, both postdose serum and bile amikacin levels were low. However, simultaneous bile levels were higher than serum levels. No patient suffered from any side effects from amikacin.
Topics: Adult; Aged; Amikacin; Bile; Biliary Tract; Body Fluids; Female; Humans; Infusions, Parenteral; Injections, Intramuscular; Kanamycin; Kinetics; Liver Function Tests; Male; Middle Aged
PubMed: 6747021
DOI: 10.1002/j.1552-4604.1984.tb02781.x -
Journal of Liposome Research Dec 2013The radiolabeling of the liposome surface can be a useful tool for in vivo tracking of therapeutic drug loaded liposomes. We investigated radiolabeling therapeutic drug...
The radiolabeling of the liposome surface can be a useful tool for in vivo tracking of therapeutic drug loaded liposomes. We investigated radiolabeling therapeutic drug (i.e. an antibiotic, amikacin) loaded liposomes with (99m)Tc, nebulization properties of (99m)Tc-labeled liposomal amikacin for inhalation ((99m)Tc-LAI), and its stability by size exclusion low-pressure liquid chromatography (LPLC). LAI was reacted with (99m)Tc using SnCl2 dissolved in ascorbic acid as a reducing agent for 10 min at room temperature. The labeled products were then purified by anion exchange resin. The purified (99m)Tc-LAI in 1.5% NaCl solution was incubated at 4 °C to assess its stability by LPLC. The purified (99m)Tc-LAI was subjected to studies with a clinically used nebulizer (PARI eFlow®) and the Anderson Cascade Impactor (ACI). The use of ascorbic acid at 0.91 mM resulted in a quantitative labeling efficiency. The LPLC profile showed that the liposomal peak of LAI detected by a UV monitor at both 200 nm and 254 nm overlapped with the radioactivity peak of (99m)Tc-LAI, indicating that (99m)Tc-LAI is suitable for tracing LAI. The ACI study demonstrated that the aerosol droplet size distribution determined gravimetrically was similar to that determined by radioactivity. The liposome surface labeling method using SnCl₂ in 0.91 mM ascorbic acid produced (99m)Tc-LAI with a high labeling efficiency and stability that are adequate to evaluate the deposition and clearance of inhaled LAI in the lung by gamma scintigraphy.
Topics: Administration, Inhalation; Amikacin; Anti-Bacterial Agents; Chromatography, Gel; Chromatography, High Pressure Liquid; Liposomes; Organotechnetium Compounds; Particle Size; Spectrophotometry, Ultraviolet
PubMed: 23879241
DOI: 10.3109/08982104.2013.819889