With a one-time infusion of a solution of 400 mg, lasting 1 hour, the peak value reaches at the end of the procedure and is approximately 4.1 mg / L. This corresponds to an increase in the drug's level relative to its level with oral intake on average by 26%.
The AUC is 39 mg / hr and only slightly above the level after oral administration (35 mg · h / l). The bioavailability of the drug is approximately 91%.
After multiple infusions of medication intravenously (at a dosage of 400 mg) for 1 hour once a day, the minimum values, as well as the peak of the equilibrium plasma level are located in the gap, respectively, 4.1-5.9, and 0.43-0.84 mg / l. And with equilibrium indices, the drug AUC in the dosing interval is about 30% higher than the value after the first dose.
The average equilibrium value reaches 4.4 mg / l, and this value is observed at the end of infusion, lasting 1 hour.
The active ingredient passes a rapid distribution in the internal space of the body, outside the vessels. The drug level of AUC (normal value is 6 kg · h / l) is quite high at equilibrium values of the distribution volume (2 l / kg). The results revealed in in vitro tests, as well as ex vivo, showed values in the range of 0.02-2 mg / l.
Synthesis with blood protein (usually albumin) reaches 45%, and this ratio is not affected by drug concentrations. Although this is a fairly low level, the free component has high peak values (10 · IPC).
Moxifloxacin has high enough indices inside the tissues (for example, in the lungs - macrophages of the alveoli and epithelial fluid), and also inside the paranasal sinuses (polyps of the nose, latticular, and maxillary sinuses) and inflammatory foci in which the total values exceed the concentrations obtained inside plasma. Inside the intercellular fluid (in the subcutaneous and muscular tissues, and also in the saliva), the drug is found in large concentrations and in a free form that is not synthesized with the protein. Along with this, large medicinal values can be observed inside the fluids and tissues of the peritoneal organs, as well as inside the female genital organs.
The peak level, as well as the ratio of the indices inside the plasma and the infusion site, for the individual target tissues demonstrate similar data for each of the routes of use after using a single dosage of drugs (400 mg).
There is also biotransformation (phase 2) of moxifloxacin, followed by renal excretion (in addition, with bile / feces - unchanged or in the form of inactive elements M1 (sulfo compound), as well as M2 (glucuronides)).
In vitro experiments, and in addition, during clinical tests of the 1st phase, no metabolic interaction was observed with respect to pharmacokinetic parameters with other drugs, which take part in the biotransformation of the first phase using enzymes of the hemoprotein system P450.
Regardless of the method of administration, the decay products (M1 with M2) are observed inside the plasma at values lower than the unchanged element. In pre-clinical tests, both components were tested in commensurate sizes, so that the possible impact on the tolerability and safety of drugs was excluded.
Half-life is approximately 12 hours. The average level of total clearance when using 400 mg LS is in the range of 179-246 ml / minute. The clearance in the kidneys is approximately 24-53 ml / minute, from which it can be concluded that in the body there is a partial reabsorption of the drug - from the kidneys through the tubules.
Simultaneous administration of probenecid with ranitidine does not lead to a change in the values of the clearance of drugs in the kidneys.