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PubMed1983

[Pharmacokinetic basis for using tobramycin and sisomicin in treating pyelonephritis of the transplanted kidney].

The pharmacokinetics of tobramycin and sisomicin in patients after kidney transplantations was studied. A significant variability of the pharmacokinetic parameters of tobramycin and sisomicin under conditions of the changing function of the kidney transplant was shown. This required individual control of the drug serum levels in such patients. Linear correlation between the exponent (beta) and the clearance of endogenous creatinine was observed. On the basis of this correlation a nomogram providing a decrease in the percentage of the errors in determining the dosage intervals was plotted.

Adolescent↗
PubMed1983

[General toxic and organotropic properties of sisomicin sulfate in chronic experiments on animals].

General toxic and organotropic properties of sisomicin sulfate were studied in chronic experiments on different animal species with the use of doses equivalent to therapeutic ones in humans or exceeding them by several times. When sisomicin was injected intramuscularly for 4 weeks in a dose equivalent by the body surface to the average daily dose for humans, no significant effect on the macroorganism was observed. When the dose was 2--4 times higher, a significant increase in the blood serum levels of the urea nitrogen, creatinine, bilirubin and aspartate aminotransferase was shown. Histological examinations revealed focal adiposis of epithelial cells of the convoluted tubules of the kidney and small areas of parenchymal necrosis. Impairment of vestibular and auditory functions was detected in some animals.

Animals↗
PubMed1983

[Simulation of the pharmacokinetics of aminoglycosides in the kidneys: single and continuous intake of sisomicin and gentamicin by rats].

The pharmacokinetics of sisomicin and gentamicin in the cortical and medullary layers of the kidneys was studied on rats. The antibiotics were administered daily in doses of 12.5 and 25 mg/kg a day. The levels of the antibiotics in the cortical layer were much higher than those in the medullary layer. The use of a twice as higher dose in the first case resulted in a less than a two-fold increase in the drug concentration, while in the second case the increase was more than two-fold. Prognosis of the pharmacokinetics of aminoglycosides used for 8-16 days was achieved with the help of the constants of the two-compartmental model. It was shown that the actual levels of sisomicin and gentamicin in the kidney medullary layer did not significantly differ from the estimated ones and the levels of the drugs in the cortical layer were much lower than the predicted ones. The distorted linearity of the aminoglycoside pharmacokinetics must be mainly due to saturation of the cortical layer with the drugs.

Animals↗
PubMed1978

[Pharmacologic studies or aminoglycoside antibiotics (amikacin, gentamicin, sisomicin, tobramycin)].

In a randomized study of 12 healthy subjects, the pharmacokinetics of gentamicin, sisomicin and tobramycin were determined after a one-hour infusion of each drug (1.0 mg/kg body-weight). There were no pharmacokinetic differences of therapeutic significance between the three drugs. The mean serum concentrations at the end of infusion were 3.85 microgram/ml for gentamicin and 4.66 microgram/ml for sisomicin, falling to 0.12 and 0.26 microgram/ml, respectively, after eight hours. The biological half-life varied between 96 and 122 min and the apparent volumes of distribution corresponded closely to the size of the extracellular space.--The pharmacokinetic data of amikacin were determined after a one-hour constant infusion, the mean amikacin serum concentration was 37.5 microgram/ml and, 8 hours later, decreased to an average of 1.3 microgram/ml. The biological half-life amounted to a mean of 114.2 +/- 16.7 min, and the apparent volume of distribution could be calculated with 18.1 +/- 1.81/100 kg body weight.

Adult↗
PubMed1981

[Sisomicin. The mechanism of admixture inactivation and formation].

Inactivation of sisomicin in aqueous solutions was studied under various conditions. At pH 4-10 and a temperature of 60 degrees C the inactivation rate constant was equal to (5-10) X 10(-5) hour-1 and remained stable. At lower pH values the inactivation rate constant increased: 5.5 10(-3) (60 degrees C) at pH 0.5. The activation energy of the inactivation reaction was 27 (pH 0.5) and 32 (pH 4.0) kcal/mol. The study on the behaviour of sisomicin in solutions with different pH values under the environmental conditions and in the atmosphere of nitrogen showed that at low pH values the inactivation was mainly determined by hydrolysis of the glycoside bond. Formation of coloured compounds did not include the oxidation reaction. At pH about 7.0 oxidation of the antibiotic or of the products of its degradation with respect to the double bond played a significant role in the inactivation and formation of the coloured substances.

Disaccharides↗
PubMed1980

[Comparative study of sisomicin and gentamycin action on the cells in a tissue culture].

The cytostatic effect of sisomicin and gentamicin, antibiotics from the group of aminoglycosides was studied comparatively with respect to three types of tripsinized cells of chick embryo (cells of the kidneys, liver and fibroblasts). It was found that epithelial cells and in particular kidney cells were most sensitive to the above antibiotics as compared to fibroblasts. It was also shown that gentamicin had a lower cytostatic effect on the embryonal cells of the kidneys, liver and fibroblasts as compared to sisomicin.

Animals↗
PubMed1976

[Sisomicin treatment of urinary tract infections (author's transl)].

In a study with 30 randomized patients the pharmacokinetics, efficacy and side effects of Sisomicin were determined. Half of the patients received one single intramuscular injection of 75 or 100mg (1.4 mg/kg) Sisomicin/day. The other cases were injected 50 or 75mg (1.9 or 2.1 mg/kg) b.i.d. The serum concentrations determined on the first and last days of treatment 1 hour after the application ranged between 4 and 5.3 mug/ml. After 6 hours the values decreased to 0.7-0.8 mug/ml. The elimination rate within 24 h amounted to 63-77%. Depending on the dosage group, the mean urinary concentrations/24 h amounted to 46-51 mug/ml or 63 to 92 mug/ml, respectively. The highest concentration measured during the first 8 hours amounted to 129 mug/ml after an administration of 1.4 mg/kg. In 18 of 29 cases a "cure" of urologic infections, most of which had been treated previously without success, could be achieved. Furthermore we observed 5 relapses, 3 failures and 3 reinfections, but no superinfection. The local and general tolerance of Sisomicin was good. 5 patients showed toxic reactions of the vestibular organ in the form of dizziness. In 1 case there was an excretion of granulated casts.

Adolescent↗
PubMed2000

Distribution and serum concentration of sisomicin released from fibrin glue-sealed dacron graft in the rat and human.

We investigated whether or not fibrin glue (FG) used as a sealant in vascular prostheses to prevent leakage might be useful as a carrier of antibiotics for the prevention of local graft infection. Sisomicin (SISO) was incorporated into fibrin glue (SISO-FG) and evaluated as to its safety and pharmacokinetics. SISO (1.75 mg) -FG Dacron grafts were implanted subcutaneously in the anterior abdominal region of Sprague-Dawley rats, and then the changes in SISO concentrations in the serum and in the tissue around the implantation sites were compared with those same sites in rats that had had intravenous injection of SISO (1.75 mg). The serum SISO concentrations were significantly lower in the SISO-FG Dacron graft group than they were in the intravenous injection group. However, until 4 h after implantation the SISO concentrations in the tissues around the implantation sites were significantly higher in the SISO-FG Dacron group than they were in the iv injection group, and the peak concentrations during that time were 5.8 times higher for the SISO-FG Dacron group than they were for the intravenous injection group. The ratio of the area under the tissue concentration time curve of SISO (AUC tissue) after implantation of the SISO-FG Dacron graft to that after intravenous injection of SISO was 13.08. Therefore, FG was considered to control the release of SISO into the serum and to maintain a high SISO concentration in the tissue around the implantation site. Clinically, SISO (45 mg) -FG was applied directly to the Dacron grafts implanted in 10 patients who underwent prosthetic vascular reconstruction. No graft infection was observed in any of the patients who received SISO-FG Dacron grafts. The mean serum concentration of SISO was 0.65+/-0.17 microg/mL after 1 h and 0.33+/- 0.21 microg/mL after 3 h. The results of these clinical applications are in close correlation with those of the animal experiment and suggest that FG is useful as a carrier of SISO, allowing its controlled release for the prevention of local infection.

Aged↗
PubMed1975

Antistaphylococcal activity of sisomicin and four other aminoglycosides against strains sensitive and resistant to methicillin.

Five aminoglycosides were tested for inhibitory activity on 91 strains of Staphylococcus aureus, 39 of which were methicillin-resistant. The antistaphylococcal activity of these antibiotics was independent of the methicillin-resistance. Their order of decreasing effectiveness was: gentamicin greater than tobramycin = sisomicin greater than amikacin greater than kanamycin. Resistant strains were only found for the latter.

Aminoglycosides↗
PubMed1980

[Pharmacokinetic and clinical studies with sisomicin in paediatrics (author's transl)].

Pharmakokinetic and clinical investigations were carried out with sisomicin, one of the newer aminoglycoside antibiotics, in 40 children aged from seven days to ten years. Serum concentrations were determined in 35 children 1/2, 1, 2, 4 and 6 hours after i. m. injection of 1.0 mg sisomicin/kg body weight. The average peak serum levels were 2.48 mg/l in children under three months and 3.58 mg/l in children between seven months and ten years. Renal elimination in newborns is delayed in comparison to older infants and children; the distribution volume of the central compartment diminishes with increasing age. The effect of these two counteracting tendencies is that renal clearance remains constant in the age groups investigated, however the frequency of drug administration must be adjusted according to age. During an average treatment period of ten days adequate serum concentrations between 3.1 mg/l and 6.2 mg/l one hour after injection could be achieved with dosages adjusted to age and body weight. Clinical results were good: 18 out of 20 children could be cured clinically, and 20 out of 21 isolated infectious agents were eliminated. There were no problems in local and systemic tolerance.

Bacterial Infections↗
PubMed1978

Binding of sisomicin and streptomycin to human albumin.

The aminoglycosides of the kanamycin and neomycin series are displaced from their protein binding by very low Ca++ ion concentrations, whereas streptomycin is displaced only by very high Ca++ ion concentrations. For streptomycin, therefore, the binding mechanism must differ from that for the other aminoglycosides. The displacing reaction cannot be described by the law of mass action, combining the binding equations. Several possible reasons, such as complex formation and changes in the conformation of albumin, are discussed. Complex formation between sisomicin and the lanthanide ion Nd+++, which has the same ionic radius as the Ca++ ion, could be excluded by recording the difference absorption spectrum. The displacement of the aminoglycosides from their protein binding by Ca++ ions (as well as the pH dependence of the protein binding) suggests that ionic bonds are involved in the interactions between aminoglycosides and serum proteins.

Calcium↗
PubMed1976

Sisomicin in urinary tract infection: Tolerance and efficacy study.

Twenty-one patients with gram-negative urinary tract infections were treated with sisomicin, a new aminoglycoside antibiotic. Bacteriologic cure was achieved in 62 per cent of patients, and improvement in another 33 per cent. Mild transient elevation of serum creatinine occurred in 3 patients. No other toxicity was observed. Further clinical trials with more frequent dose administration and in combination with other antibiotics is suggested.

Adult↗
PubMed1993

Neuronal degeneration of primary cochlear and vestibular innervations after local injection of sisomicin in the guinea pig.

This paper reports on a dynamic study of the morphological changes within the cochlear and vestibular ganglia of the guinea pig after local application of Sisomicin in the inner ear. The treatment leads to a rapid, complete and irreversible destruction of the sensory cells in the cochlear and vestibular neuroepithelia. A progressive degeneration of the type I and type II afferent neurons, presenting a decreasing gradient from the base towards the apex of the cochlea, is rapidly observed and becomes almost complete as early as 15 days after the peripheral injury. Five months after the treatment the spiral ganglion cells have almost completely disappeared. At this time the vestibular ganglion cell density appears normal but the neurons exhibit important signs of alteration. Such damage to the cochlear and vestibular afferent neurons may result from either retrograde neuronal degeneration and/or direct neurotoxic effect of the drug. Thus the combination of the two mechanisms could lead to neuronal losses in spiral and Scarpa's ganglia after the local aminoglycoside intoxication of the inner ear. The difference in the time course of degeneration for these two afferent ganglia could be due to their specific susceptibilities or to their different anatomical locations.

Animals↗
PubMed2004

ATP, histidine or magnesium ions can protect DNA against sisomicin-induced damage, following stray Cu(II) binding.

The oxidative DNA damage by the cupric complexes of sisomicin was investigated in the presence of varying amounts of histidine, ATP, Mg(II) ions or phosphates. We found that by very low concentrations, the amino acid is able to inhibit the cleavage totally. This occurs both by its competition with antibiotic for copper(II) binding, what was proved by spectroscopic measurements, as well as by ROS scavenging by the imidazole ring. ATP and magnesium also exert an influence on the yield of the DNA destruction by decreasing the amount of the single strand breaks, however only their significant excess is able to break this process. The influence of ATP on the plasmid damage has in this case a similar chemical mechanism to that one observed for histidine. Mg(II) ions, however, interact with DNA and thus prevent the complex binding. Only phosphate anions, in the range of their physiological concentrations, exert no influence on the cleavage process.

Adenosine Triphosphate↗
PubMed2004

Acid-base versus structural properties of an aminoglycoside antibiotic--sisomicin: NMR and potentiometric approach.

Aminoglycoside antibiotics constitute a class of the drugs of high interest, whose therapeutic action is based upon the electrostatic interaction with the variety of RNA molecules. The positive charge of these drugs molecules, located at their amino functions, has a prevailing influence on this process. The potentiometry and (1)H NMR spectroscopy are applied hereby to achieve the characteristics of the acid-base properties of particular protonating groups. We found that the pK values of deprotonation processes cover a wide values range 6-9.8. The correlation spectra of sisomicin, both COSY and TOCSY, allowed attributing unambiguously individual signals to the corresponding protons. These spectra involve a lot of the cross-peaks originating from the B and C rings protons, while the analogous signals originating from A rings protons are less numerous. Molecular modeling provided that the methylated amino group of A ring is located too far from the protonated functions of the remaining rings to affect their pK values. The phenomena observed herein are discussed in line of strength of the analogous processes observed for other aminoglycosides. As the result, four types of amino groups consisted within these antibiotics are distinguished.

Acid-Base Equilibrium↗
PubMed1977

[Investigation of the c. s. fluid levels of two newer antibiotics; cefazolin and sisomicin (author's transl)].

In ten patients continuous estimations of the C.S.F. and serum levels were performed after the administration of a Cephalosporin derivative (Cefazolin - 4 cases) and a new alpha-amino-glycoside antibiotic (Sisomicin - 6 cases). After the evaluation of the results some doubts must be cast on the value of both these antibiotics for the treatment of meningitis or for per-operative chemo-prophylaxis in neurosurgical procedures. The values found were compared with those well-known in the literature, regarding the cephalosporins and the alpha-amino-glycoside Gentamycin.

Adolescent↗
PubMed1995

Prevention of vascular graft infection by sisomicin incorporated into fibrin glue.

To examine the efficacy of sisomicin (SISO) incorporated into fibrin glue (FG) for the prevention of graft infection in animal models, the susceptibility to infection of Dacron grafts (control) and SISO-FG Dacron grafts following the inoculation of Staphylococcus aureus or S. epidermidis was compared. The results showed that SISO-FG Dacron grafts displayed resistance to graft infection.

Animals↗