Gemix

Hemix is an antibacterial drug from the quinolone category.

Indications Gemixa

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

• community-acquired pneumonia (also caused by the action of multidrug-resistant strains);
• chronic bronchitis in the acute stage;
• acute stage of sinusitis.

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Release form

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

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Pharmacodynamics

Gemifloxacin is an antimicrobial drug from the fluoroquinolone category. 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 reparation and replication, as well as transcription of microbial DNA – by slowing down the activity of enzymes DNA gyrase (topoisomerase 2), as well as topoisomerase 4, which are required for bacterial growth. Gemifloxacin has high affinity rates with bacterial topoisomerases – II (DNA gyrase) and IV.

Strains of pneumococcus with gene mutations that encode these enzymes are resistant to most drugs from the fluoroquinolone category. But in significant medicinal concentrations, the substance can slow down the altered enzymes. Therefore, individual strains of pneumococcus that are resistant to fluoroquinolones may show sensitivity to gemifloxacin.

The mechanism of therapeutic activity of fluoroquinolones (including gemifloxacin) is somewhat different from the effect 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 of resistance to fluoroquinolones is gene mutations within DNA gyrase with DNA topoisomerase IV. The frequency of occurrence of these mutations is 10-7/10-10 and less.

The component gemifloxacin has therapeutic activity against most bacterial strains – in in vitro procedures, as well as in vivo:

• Gram-positive aerobes: pneumococci (including those resistant to macrolides and penicillin, as well as most of those resistant to ofloxacin or levofloxacin, as well as MDRSP), pyogenic streptococci (including bacteria resistant to macrolides), Streptococcus agalactiae, Streptococcus viridans and Streptococcus anginosa. In addition, Streptococcus constellatus with Streptococcus milleri and Streptococcus mitis, as well as other bacteria from the streptococcal group. Together with them, also Staphylococcus aureus (sensitive to methicillin), Staphylococcus epidermidis, saprophytic staphylococci, hemolytic staphylococci and other microbes from the staphylococcal category. In addition, there are also fecal enterococci, enterococci faecium and other bacteria from the enterococci category;
• Gram-negative aerobes: Influenza bacillus (this also includes microorganisms with the presence of β-lactamase), Haemophilus parainfluenzae and other bacteria from the Haemophilus group. In addition, Moraxella catarrhalis (with positive and negative β-lactamase) and other types of bacteria from the Moraxella category. In addition, Friedlander's bacillus, Klebsiella oxytoca and other types of microbes from the Klebsiella group. Together with them, also gonococci, Escherichia coli, Acinetobacter iwoffi, Acinetobacter calcoaceticus with Acinetobacter anitratus, and in addition Acinetobacter haemolyticus and other forms of bacteria from the Acinetobacter category. This list also includes Citrobacter freundii, Citrobacter koseri, as well as other microbes from the Citrobacter category;
• Shigella with salmonella, Enterobacter aerogenes and other forms of Enterobacter microbes. Serratia marcescens and other forms of Serratia bacteria. Proteus vulgaris, Proteus mirabilis and other types of bacteria from the Proteus category. Providencia, Morgan's bacterium and other types of Morganella, Yersinia, Pseudomonas aeruginosa and other types of bacteria from the Pseudomonas group, as well as Borde-Gengou bacteria and other microbes from the Bordetella category;
• atypical microbes: Coxiella burnetii and other forms of coxiella, mycoplasma pneumoniae and other bacteria from the mycoplasma group, legionella pneumophila and other microbes from the legionella group, as well as chlamydophila pneumoniae and other forms of chlamydia;
• anaerobes: peptostreptococci, Clostridium non-perfringens, Clostridium perfringens and other forms of clostridia, fusobacteria, porphyromonas and prevotella.

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Pharmacokinetics

After oral administration of the drug in doses of 40-640 mg, its pharmacokinetic characteristics remain linear.

Gemifloxacin is rapidly absorbed in the gastrointestinal tract. It takes 0.5-2 hours after taking 1 tablet of the drug to reach peak levels of the substance in the body. With repeated use of 320 mg of the drug, peak levels of the substance in 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/hour/ml, as well as 4.71-20.1 μg/hour/ml.

When using the drug in a course dose of 320 mg once a day, its equilibrium values are noted on the 3rd day of therapy. Hemiks hardly accumulates (less than 30% after taking the drug in a dose of 640 mg for the first week).

Food consumption has almost no effect on the pharmacokinetic parameters of gemifloxacin, which allows the drug to be used without regard to the time of food consumption.

After repeated use of the drug, 55-73% of the active element is synthesized with plasma protein; the patient's age does not affect the proportion of the synthesized fraction.

The level of gemifloxacin in bronchoalveolar lavage is higher than its values in blood plasma. The drug has a high ability to penetrate into the lung tissue.

A small part of the substance undergoes hepatic metabolism. After 4 hours from administration, unchanged gemifloxacin predominates (its part is 65%) over the products of drug metabolism in the blood plasma. The drug is not metabolized with the participation of the hemoprotein P450 system, and does not slow down the rate of its metabolic processes.

Excretion of the drug (unchanged element and metabolic products) occurs through the intestines (in a healthy person, this figure is 61% ± 9.5% of the portion), and in addition, together with urine (in a healthy person, the figure is 36% ± 9.3%). The excretion period of the drug from plasma and urine is approximately 8 and 15 hours, respectively.

During hemodialysis, approximately 20-30% of the gemifloxacin dose is removed from the plasma.

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Dosing and administration

The tablets should be taken orally, washed down with plain water, regardless of meal time. The required dose per day is 320 mg of the drug once.

For the treatment of community-acquired pneumonia, a single dose of 320 mg of the drug per day is required for 1 week.

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

To eliminate acute sinusitis, a course of treatment with a single daily dose of 320 mg of the drug also lasts 5 days.

People with mild to moderate renal impairment (CC values >40 ml/min) do not need to change the dosage. People with severe stages of the disease (CC level <40 ml/min) and those undergoing hemodialysis or regular ambulatory peritoneal dialysis should take 160 mg of the drug once a day.

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Use Gemixa during pregnancy

Hemix is prohibited for use in pregnant women.

Contraindications

Main contraindications:

• the presence of hypersensitivity to gemifloxacin and other components of the drug;
• prolongation of the QT interval during the ECG procedure (this also includes the congenital form of this disorder);
• history of tendon injury due to fluoroquinolone use;
• lactation period;
• persons under 18 years of age.

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Side effects Gemixa

The use of the drug may cause the following side effects:

• manifestations of allergy: sometimes urticaria, itching, signs of hypersensitivity develop. In addition, Stevens-Johnson syndrome or TEN may develop. Pneumonia of an allergic nature and severe photosensitivity are noted sporadically;
• digestive disorders: the appearance of diarrhea and nausea, sometimes the development of vomiting, bloating, abdominal pain and anorexia. Hepatitis or acute liver failure may occur occasionally;
• disorders of the nervous system function: a feeling of anxiety, drowsiness, restlessness or confusion may occur sporadically, as well as tremor, depression, paranoid syndrome and hallucinations. If signs of damage to the central nervous system occur, the use of the drug must be discontinued. In addition, polyneuropathy of a sensory axonal nature may be observed, manifested in the form of hypoesthesia, paresthesia, a feeling of weakness, as well as other sensitivity disorders;
• disorders of the sensory organs: isolated cases of olfactory and gustatory disorders, tinnitus, hearing loss, dizziness, and visual disturbances (such as problems with color perception and diplopia) are observed;
• lesions affecting the hematopoietic system: sometimes leukopenia develops; occasionally thrombocytopenia appears, and occasionally agranulocytosis, pancytopenia, thrombocytopenic purpura and other hematological disorders. In addition, anemia can sometimes be observed (sometimes in aplastic or hemolytic form);
• urinary dysfunction: crystalluria is occasionally observed. Acute renal failure or tubulointerstitial nephritis may develop;
• Laboratory test results: occasionally, an increase in sodium, total bilirubin, and platelet counts is observed, as well as a decrease in potassium, calcium, and blood neutrophils. An increase in CPK and liver transaminase values, and a change in hematocrit values are also noted;
• Others: arthritis or arthralgia, myalgia, tendovaginitis and vasculitis develop sporadically, as well as superinfections (such as pseudomembranous colitis or candidiasis). Tendon ruptures are also possible.

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Overdose

A sign of intoxication is the potentiation of side effects.

In acute poisoning, vomiting should be induced or gastric lavage should be performed, and symptomatic measures should be taken. Hemix has no specific antidote. The patient should drink plenty of fluids and be constantly monitored. During hemodialysis, 20-30% of the gemifloxacin dose is excreted from the blood plasma.

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Interactions with other drugs

Combination of the drug with antacids containing iron sulfate, magnesium or aluminum, and also with sucralfate reduces the level of bioavailability of Hemix. Antacids should be taken at least 3 hours before taking gemifloxacin or at least 2 hours after it. Sucralfate should be used at least 2 hours after using the drug.

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

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

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Storage conditions

Hemiks should be kept in a dry place, out of reach of small children. Temperature indicator – below 25°C.

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Shelf life

Gemiks can be used for 2 years from the date of manufacture of the medicinal product.

Analogues

An analogue of the drug is the drug Faktiv.

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