Avelox 400mg Bayer treat infections (1 blister x 5 tablets)

Pharmacokological

Pharmacological effects: Quinolon antibiotics, fluoroquinolone.

Mechanism of action

moxifloxacin, 8-methoxyl-fluoroquinolone is a broad-spectrum antibiotic with bactericidal effect. On Vitro Moxifloxacin has a broad spectrum for Gram -positive and negative bacteria, anaerobic bacteria, sustainable bacteria with acids, not typical bacteria such as Mycoplasma spp, Chlammydia spp and Legionella spp.

Dinosurable effect is caused by moxifloxacin to interfere with Men Topoisomerase II and IV, these are the enzymes that need to control DNA geometry and help copy and repair DNA.

The bactericidal effect of moxifloxacin depends on the concentration of the drug. The minimum minimum bactericidal concentration is equivalent to the minimum bacterial inhibition concentration.

moxifloxacin works against beta-lactam and macrolide resistance bacteria. Studies on the animal infection model show that the drug is highly active in Vivo.

Drug resistance

The anti -drug anti -drug mechanisms, penicillin, cephalosporin, aminoglycoside, macrolide and tetracycline do not affect the bactericidal activity of moxifloxacin. There is no cross resistance between moxifloxacin and these drugs. No anti -drugs through plasmid intermediaries so far.

It is found that half of the C8-methoxyl contributes to increased activity and selective reduction of drug resistance mutations for gram-positive bacteria compared to half of the C8-H. The presence of Bicyclamine replacement substance at the C7 position prevents the pumping (EFFLUX) active, a Fluoroquinolone resistance mechanism.

In vitro studies have shown that drug resistance for moxifloxacin grows slowly due to many mutant steps. Only a very low rate of drug resistance is proven (10-7-10-10). When germs are in contact with moxifloxacin at a concentration under the mic, it only increases mic value.

Diagonal resistance between quinolone has also been monitored. However, some Gram -positive and anaerobic bacteria resist other Quinolone but still sensitive to moxifloxacin.

Effects on gastrointestinal bacteria population in humans

In two studies on volunteers, after using moxifloxacin by oral, the following permanent strains have been changed: E.coli, Bacillus spp., Bacteroides Vulgatus, Enterococci and Klebsiella spp as well as other anaerobic bacteria such as Bifidobacterium, Eubacterium and peptostoccus. This change returns to normal after 2 weeks. Clostridium difficile toxicity is not found.

pharmacokinetic pharmacokinetics

After drinking, moxifloxacin tablets are absorbed quickly and almost completely. The absolute bioavailability of the drug reaches about 91%.

The pharmacokinetics of the drug achieved within 50 - 1200mg after taking a single dose or a dose of 600mg once daily for 10 days. Stable concentration is achieved within 3 days. After taking the dose of 400mg, the peak concentration is 3.1mg/l achieved for 0.54 hours. The highest and lowest concentration in plasma (when taking 1 dose of 400mg per day) respectively 3.2 and 0.6mg/l.

Simultaneous use of moxifloxacin with food that extends the time to the peak concentration for approximately 2 hours and slightly reduces the peak concentration in plasma by about 16%. The absorption amount remains unchanged. People often rely on the AUC/Mic ratio to predict Quinolone's bactericidal effectiveness, but it is not commensurate with the clinical effect. Therefore, you can drink Avelox outside meals.

After using a single dose of 400mg intravenously within 1 hour, the peak of plasma peaks reached about 4.1mg/l at the end of the transmission time, an increase of approximately 26% related to oral use. The exposure of the drug, in terms of AUC index is 39mg/h/l after intravenous infusion is only a little higher than 35 mg/h/l after taken, in the condition of the drug is almost completely absorbed and used to 91%.

After the intravenous injection is repeated (intravenous infusion in 1 hour) at a dose of 400mg, the peak and bottom of the plasma is stable, respectively, between 4.1 to 5.9 and 0.43 to 0.84mg/l. At stable concentration, the distribution of the drug in the period between 2 doses is approximately 30% higher after the first dose. In patients, the average stable concentration is 4.4mg/l achieved immediately after intravenous infusion (transmitted within 1 hour).

Distribution

moxifloxacin is quickly distributed to extracellular compartments. The exposure of the drug, based on the AUC (ACCORM = 6kg/h/l), is quite high in terms of distribution at a stable concentration (VSS) approximately 2l/kg. The peak concentration in the salivary glands can be achieved higher than the plasma concentration. In studies on in vitro and body testing, ranging from 0.02 to 2mg/l, it is determined that the amount associated with the protein is approximately 45%, regardless of the concentration of the drug. Moxifloxacin mainly binds to plasma albumin. Due to the low ratio of protein, the peak concentration is high in the form of a high level> 10 times the mic concentration.

moxifloxacin achieves high concentrations in tissues such as lungs (epithelium fluid, alveolar cells, bio -tissue), sinuses (sinus and sinus sinuses, nasal polyps) and inflammatory organizations (burns), where the concentration of the drug exceeds plasma concentrations. A large amount of drugs in the form of free are found in organs containing many fluids (salivary glands, muscles, subcutaneous tissues). Besides, the high concentration of drugs is also seen in tissues and fluids in the abdominal and genital tract of women.

Peak concentrations and ratios between local and plasma concentrations are very different for oral medication or intravenous infusion and a single dose of 400mg.

Metabolism

moxifloxacin undergo phase II biological metabolism and are eliminated through the kidneys and bile in the form of non -metabolic drugs as well as Sulfo complex (M1) and glucuronide (m2). M1 and M2 are metabolites that are meaningful to humans, both are inactive bacterial.

Regardless of whether the test on in vitro or clinical trial phase phase research pharmacokinetics interact with other drugs, the phase biological metabolism process has the participation of the cytochrome P450 enzyme system. Regardless of the medication line, both metabolites M1 and M2 are found in plasma at lower concentrations than the original drug concentration. The corresponding preclinical studies have been conducted with both metabolites and found that they are not at risk of safety and absorption.

Elimination

moxifloxacin is exported from plasma with a half -life of approximately 12 hours. The average body clearance amount after the dose of 400mg is about 179 to 246ml/min. The amount of removal through the kidney is about 24 -53ml/min, showing that the renal tubules may have been re -absorbed in part of the drug in the kidney. Simultaneous use with ranitidin and probenecid does not change the drug's clearance in the kidney.

The balance between the initial amount of drugs and the metabolites through phase II of moxifloxacin has been reabsorbed almost completely, approximately 96 - 98% does not depend on the use line and shows no signs of metabolites of the oxidation process.

Older people

pharmacokinetics is not affected by age.

Gender

There are about 33% with a difference in pharmacokinetics (AUC, CMAX) of moxifloxacin between men and women. The absorption of drugs is not affected by gender. This difference for AUC and CMAX may be due to body weight rather than gender. This has no clinical significance.

Race difference

The race difference is tested on white, Japanese, black and other racial groups. There is no detection of a different dynamic difference related to race.

Children and adolescents

Moxifloxacin pharmacokinetics in children have not been studied.

Renal function

pharmacokinetics are not significantly affected in patients with renal function (even when creatinine clearance

Liver function

Moxifloxacin concentration in plasma in patients with medium to severe liver function.