Hemix

Hemix is an antibacterial drug from the category of quinolones.

Indications of the hexix

It is used to eliminate infections, the development of which is provoked by the activity of bacteria sensitive to the drug:

• non-hospital pneumonia (also triggered by the action of multidrug-resistant strains);
• chronic bronchitis at the stage of exacerbation;
• acute stage of sinusitis.

[1], [2]

Release form

The release takes place in the form of tablets, in the amount of 10 pieces inside the blister pack. The box contains 1 such blister.

[3], [4], [5]

Pharmacodynamics

Gemifloxacin is an antimicrobial drug from the category of fluoroquinolones. The substance has a wide range of bactericidal activity against gram-positive and -negative, as well as atypical bacteria and anaerobes.

The medicinal element destroys the processes of repair and replication, as well as the transcription of the microbe DNA - by slowing down the activity of DNA-gyrase enzymes (topoisomerase 2), as well as topoisomerase 4, which are required for bacterial growth. In hemifloxacin, high indices of kinship with bacterial topoisomerases-II (DNA-gyrase) and IV.

Pneumococcal strains with gene mutations that encode these enzymes are resistant to most drugs from the category of fluoroquinolones. But in significant drug concentrations, the substance can slow down the altered enzymes. Therefore, individual pneumococcal strains that are resistant to fluoroquinolones may exhibit sensitivity to hemifloxacin.

The mechanism of the therapeutic activity of fluoroquinolones (including hemifloxacin) is somewhat different from that of macrolides with β-lactam antibiotics, as well as tetracyclines with aminoglycosides.

Cross-resistance between Hemix and these categories of antibiotics is not observed.

The main mechanism for the emergence of resistance to fluoroquinolones are gene mutations within the DNA gyrase with DNA topoisomerase IV. In this case, the frequency of occurrence of these mutations is 10-7 / 10-10 and less.

The hemifloxacin component has therapeutic activity against most bacterial strains - in vitro procedures, and in vivo in addition:

• Gram-positive aerobes: pneumococci (among which are resistant to macrolides and penicillin, and also most resistant to ofloxacin or levofloxacin, and in addition MDRSP), pyogenic streptococci (this includes bacteria that are resistant to macrolides), streptococcus agalactia, Streptococcus viridans and Streptococcus anginosus. In addition, Streptococcus constellatus with Streptococcus milleri and streptococcus mitis, as well as other bacteria from the streptococcus group. Together with them also golden staphylococci (sensitive to methicillin), epidermal staphylococci, saprophytic staphylococci, hemolytic staphylococci and other microbes from the category of staphylococci. In addition, fecal enterococci, enterococci fecium and other bacteria from the category of enterococci;
• Gram-negative aerobes: stick influenza (this includes also microorganisms with β-lactamase), Haemophilus parainfluenzae and other bacteria from the Haemophilus group. In addition to this, moraxel catarrhas (with positive as well as negative β-lactamase) and other types of bacteria from the Moraxella category. In addition, Friedlander's stick, Klebsiella Oxytoca and other microbial species from the Klebsiella group. Together with them also gonococcus, E. Coli, Acinetobacter iwoffi, Acinetobacter calcoaceticus with Acinetobacter anitratus, and in addition Acinetobacter haemolyticus and other bacterial forms from the category Acinetobacter. This list includes both Citroobacter frowni, Citrobacter koseri, and other microbes from the category of citrobacter;
• Shigella with salmonella, enterobacter aerogenes and other forms of microbes enterobacter. Serration of marces and other forms of bacteria serration. Vulgar Proteus, Proteus mirabilis and other types of bacteria from the Proteus category. Providence, Morgan's bacterium and other Morganella species, Yersinia, Pseudomonas aeruginosa and other types of bacteria from the group of pseudomonads, and in addition Borde-Zhangu bacteria and other microbes from the Bordetell category;
• atypical microbes: Coxiella burnetii and other forms of coxiella, mycoplasma pneumonia and other bacteria from the group of mycoplasmas, legionella pneumophila and other microbes from the legionella group, as well as chlamydophile pneumonia and other forms of chlamydia;
• anaerobes: peptostreptococci, Clostridium non-perfringens, clostridium perfringence, and other forms of clostridia, fusobacteria, porphyromonas and preotella.

[6], [7], [8]

Pharmacokinetics

After oral administration of drugs in portions of 40-640 mg, its pharmacokinetic characteristics remain linear.

Gemifloxacin undergoes rapid absorption within the gastrointestinal tract. To achieve peak values of the substance within the body after the use of the 1st tablet of drugs, 0.5-2 hours is needed. With the repeated use of 320 mg of the drug, the peak values of the substance within the blood plasma are 1.61 ± 0.51 μg / ml, as well as 0.70-2.62 μg / ml, and the clearance level is 9.93 ± 3.07 μg / h / ml, as well as 4.71-20.1 μg / h / ml.

When the medicinal product is used for a course of 320 mg once a day, its equilibrium values are noted on the third day of therapy. The hemix  almost does not accumulate (less than 30% after the use of drugs in a dose of 640 mg during the first week).

The use of food almost does not affect the pharmacokinetic parameters of hemifloxacin, which makes it possible to use drugs without starting from the time of eating.

After repeated use of LS 55-73% of the active element is synthesized with a plasma protein; the age of the patient does not affect the fraction of the synthesized fraction.

The level of hemifloxacin inside bronchoalveolar lavage is higher than its values inside the blood plasma. The drug has a high ability to pass into the lung tissue.

A small part of the substance undergoes hepatic metabolism. After 4 hours after use, hemifloxacin is unchanged in its unchanged form (65% of it) over the metabolic products of drugs inside the blood plasma. The medication is not metabolized with the help of the hemoprotein P450 system, nor does it slow the rate of its metabolic processes.

Excretion of the drug (unchanged element and metabolic products) occurs through the intestine (in a healthy person this figure is 61% ± 9.5% of the dose), and in addition to urine (in a healthy person the indicator is 36% ± 9.3%). The time of excretion of drugs from plasma and urine is approximately 8 and 15 hours, respectively.

During hemodialysis, about 20-30% of the hemifloxacin dose is removed from the plasma.

[9], [10], [11], [12], [13], [14], [15],

Dosing and administration

You need to take the pill orally, squeezed with plain water, not relying on the time of eating. For a day it is required to take single 320 mg of the drug.

In the treatment of non-hospital pneumonia, a single dose of 320 mg of LS is required per day, during the first week.

In the case of exacerbation of chronic bronchitis, it is necessary to take 320 mg of medicament once daily for 5 days.

To eliminate the acute form of sinusitis, a course with a single use of 320 mg of medicine per day also lasts 5 days.

People with kidney failure in mild or moderate form (CC values> 40 ml / minute) do not need to change the dosage. Persons with severe stages of pathology (CC level is <40 ml / minute), and in addition to those who undergo hemodialysis or regular outpatient peritoneal dialysis, one day 160 mg of the drug should be consumed per day.

[21]

Use of the hexix during pregnancy

Hemix is prohibited for pregnant women.

Contraindications

The main contraindications:

• the presence of hypersensitivity to hemifloxacin and other elements of the drug;
• prolongation of the level of the QT-interval in the ECG procedure (this includes the congenital form of the disorder);
• presence in the anamnesis of damages in the field of tendons which have arisen because of use of fluoroquinolones;
• lactation period;
• persons under 18 years of age.

[16]

Side effects of the hexix

Use of the drug may cause such side effects:

• manifestations of allergy: sometimes develop hives, itching, signs of hypersensitivity. In addition, Stevens-Johnson syndrome or TEN can develop. Individual pneumonia of an allergic nature is noted and strong light sensitization;
• digestive disorders: the appearance of diarrhea and nausea, sometimes the development of vomiting, swelling, abdominal pain and anorexia. There is a single hepatitis or liver failure in an acute degree;
• disorders of the function of the NS: a single feeling of anxiety, drowsiness, anxiety or confusion of consciousness occurs, as well as tremors, depression, paranoid syndrome and hallucinations. If there are signs of a CNS lesion, it is necessary to cancel the use of drugs. In addition, polyneuropathy of a sensory axonal character can be noted, manifested in the form of hypoesthesia, paresthesia, sensation of weakness, as well as other sensitivity disorders;
• disorders of sensory function: there is a single violation of olfactory and taste buds, ear noise, hearing impairment, dizziness, as well as visual disorders (such as problems with color perception and diplopia);
• lesions affecting the hematopoietic system: sometimes leukopenia develops; occasionally there is thrombocytopenia, and individually - agranulocytosis, pancytopenia, purpura of thrombocytopenic nature and other hematologic disorders. In addition, from time to time one can observe the appearance of anemia (sometimes in aplastic or hemolytic form);
• disorders of the urinary function: occasionally there is crystalluria. Possible development of acute renal insufficiency or tubulointerstitial nephritis;
• results of laboratory tests: occasionally an increase in the level of sodium, total bilirubin and the number of platelets, and in addition a decrease in the parameters of potassium, calcium and blood neutrophils. There is also an increase in the values of CKK and liver transaminases, and changes in hematocrit;
• others: there is a single development of arthritis or arthralgia, myalgia, tendovaginitis and vasculitis, and also superinfection (such as pseudomembranous form of colitis or candidiasis). Tendon tendon ruptures are also possible.

[17], [18], [19], [20]

Overdose

A sign of intoxication is the potentiation of adverse symptoms.

In acute forms of poisoning, induce vomiting or perform gastric lavage, as well as symptomatic measures. Hexix does not have a specific antidote. The patient needs to drink a lot of fluids, he needs to be constantly watched. During hemodialysis, 20-30% of the hemifloxacin portion is excreted from the blood plasma.

[22], [23]

Interactions with other drugs

Combination of drugs with antacids, which contain iron sulfate, magnesium or aluminum, and also with sucralfate reduces the level of bioavailability of the Gemix. It is necessary to use antacids at least 3 hours before receiving hemifloxacin or at least 2 hours after it. Sucralfate should be used at least 2 hours after using the drug.

Oral contraceptive estrogen-progesterone type slightly reduces the bioavailability of the drug.

Course use of drugs does not affect the pharmacokinetic parameters of contraceptive drugs - derivatives of levonorgestrel or ethinyl estradiol.

[24], [25], [26]

Storage conditions

Hexix is required to be kept in a dry place, where there is no access for young children. The temperature is below 25 ° C.

[27], [28], [29], [30]

Shelf life

The hemix is allowed to be used for 2 years from the date of manufacture of the drug.

Analogues

The analogue of the drug is the drug FACT.

[31], [32], [33], [34], [35], [36], [37],