Azithromycin | Azithromycin-OBL capsules 250 mg 6 pcs.
Special Price
$15.52
Regular Price
$24.00
In stock
SKU
BID469513
Packaging
6 pcs
Pharmacological action
Pharmacotherapeutic group:
antibiotic-azalide
Pharmacodynamics:
Azithromycin is a broad-spectrum bacteriostatic antibiotic from the group of macrolides-azalides. It has a wide range of antimicrobial effects.
The mechanism of action of azithromycin is associated with inhibition of protein synthesis of microbial cells. By binding to the 50S subunit of the ribosome, it inhibits the peptide translocase at the translation stage and inhibits protein synthesis, slowing the growth and reproduction of bacteria. In high concentrations it has a bactericidal effect.
Has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms.
Microorganisms may initially be resistant to the action of the antibiotic or may become resistant to it.
In most cases, sensitive microorganisms
1. Gram-positive aerobes
Staphylococcusaureus Methicillin-sensitive
Streptococcuspneumoniae Penicillin-sensitive
Streptococcus pyogenes.
2. Gram-negative aerobes
Haemophilus influenzae
Haemophilus parainfluenzae
Legionella pneumophila
Moraxella catarrhalis
Pasteurella multocida
Neisseria gonorrhoeae.
3. Anaerobes
Clostridium perfringens
Fusobacterium spp.
Prevotella spp.
Porphyriomonas spp.
4. Other microorganisms
Chlamydia trachomatis
Chlamydia pneumoniae
Chlamydia psittaci
Mycoplasma pneumoniae
Mycoplasma hominis
Borrelia burgdorferi.
Microorganisms that can develop azithromycin resistance
Gram-positive aerobes
Streptococcuspneumoniae Penicillin-sensitive.
Initially resistant microorganisms
Gram-positive aerobes
Enterococcusfaecalis
Staphylococci (methicillin-resistant staphylococci show a very high degree of resistance to macrolides)
gram-positive bacteria resistant to erythromycin.
Anaerobes
Bacteroidesfragilis.
Pharmacokinetics:
Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic environment and lipophilicity. It is rapidly distributed throughout the body, while high antibiotic concentrations are achieved in the tissues. After oral administration of 500 mg, the maximum concentration of azithromycin in blood plasma is reached after 2.5-2.9 hours and is 0.4 mg / L. Bioavailability is 37.5%.
Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, the prostate gland), into the skin and soft tissues. A high concentration in tissues (10-50 times higher than in blood plasma) and a long half-life are due to the low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a low pH environment surrounding lysosomes. This, in turn, determines a large apparent volume of distribution (31.1 l / kg) and high plasma clearance.
The ability of azithromycin to accumulate primarily in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver azithromycin to the sites of localization of the infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema. Azithromycin persists in bactericidal concentrations for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.
In the liver, demethylates, the resulting metabolites are inactive.
Excretion of azithromycin from blood plasma takes place in 2 stages: The half-life is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours, which allows you to use the drug 1 time / day.
The drug is excreted mainly with bile unchanged, a small part is excreted by the kidneys.
Indications
Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
· Infections of the upper respiratory tract and ENT organs (pharyngitis / tonsillitis, sinusitis, otitis media)
· Infections of the lower respiratory tract, bronchitis, acute bronchitis , including caused by atypical pathogens
· Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses)
· Initial stage of Lyme disease (borreliosis) - migratory erythema (Erythemamigrans)
· Urogenital tract infections caused by Chlamytiatra.
Contraindications
В· Hypersensitivity to antibiotics of the macrolide group
В· Severe impairment of liver and kidney function
В· Children under 12 years of age with body weight less than 45 kg (for this dosage form)
Caution:
- moderate dysfunction of the liver and kidneys
- with arrhythmias or a predisposition to arrhythmias and lengthening of the QT interval
- with the combined use of terfenadine, warfarin, digoxin.
Use during pregnancy and lactation
Use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.
If necessary, the appointment of the drug during lactation should stop breastfeeding (excreted in breast milk).
Special instructions
Do not take with food.
In case of skipping a dose, the missed dose should be taken as soon as possible, and the next with an interval of 24 hours.
It is necessary to observe a break of 2 hours while using antacids.
After withdrawal of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under the supervision of a physician.
Effect on the ability to drive vehicles and mechanisms
Azithromycin does not affect the ability to drive vehicles and mechanisms.
Composition
Composition per capsule:
active substance:
azithromycin dihydrate (in terms of azithromycin) - 250 mg.
excipients:
microcrystalline cellulose,
povidone (low molecular weight polyvinylpyrrolidone medical),
crospovidone,
calcium stearate,
sodium lauryl sulfate.
Hard gelatin capsules No. 1:
titanium dioxide,
dye blue patented (patent blue V),
diamond black,
crimson dye [Ponceau 4R],
azorubine,
gelatin.
Dosage and Administration
Inside, 1 time per day, at least 1 hour before or 2 hours after a meal.
Adults (including older people) and children over 12 years old with body weight over 45 kg.
For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues
500 mg (2 capsules) 1 time per day for 3 days (course dose - 1.5 g).
For infections of the skin and soft tissues - 1 g / day on the first day for 1 dose, then 0.5 g / day daily from 2 to 5 days (course dose - 3 g).
With migratory erythema
1 time per day for 5 days: 1st day - 1.0 g (4 capsules), then from 2nd to 5th day - 500 mg (2 capsules) (course dose 3 , 0 g).
For urinary tract infections caused by Chlamydiatrachomatis (urethritis, cervicitis)
Uncomplicated urethritis / cervicitis - 1 g (4 capsules) once.
Prescription for patients with impaired renal function
For patients with moderate impaired renal function (creatinine clearance> 40 ml / min), dose adjustment is not necessary.
Side effects
Allergic reactions: itching, skin rashes, angioedema, urticaria, anaphylactic reaction, including edema (in rare cases, fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrosis.
From the circulatory and lymphatic systems: thrombocytopenia, neutropenia.
From the central nervous system: dizziness / vertigo, headache, cramps, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness.
From the sensory organs: tinnitus, reversible hearing loss up to deafness (when taking high doses for a long time), impaired perception of taste and smell.
From the cardiovascular system: rarely - palpitations, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia.
From the digestive system: nausea, vomiting, diarrhea, abdominal pain / cramping, loose stools, flatulence, digestive upset, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory parameters of liver functions, liver dysfunction, liver necrosis (possibly fatal).
From the musculoskeletal system: arthralgia.
From the genitourinary system: nephritis, acute renal failure.
Other: vaginitis, candidiasis, photosensitivity.
Drug Interactions
Antacids do not affect the bioavailability of azithromycin, but reduce the maximum concentration in the blood by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and food.
Azithromycin does not affect blood concentrations of carbamazepine, didanosine, rifabutin, and methylprednisolone when used together.
With parenteral administration, azithromycin does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, trimethoprim / sulfamethoxazole in the blood when used together, however, the possibility of such interactions with the appointment of azithromycin for oral administration should not be ruled out.
Azithromycin does not affect theophylline pharmacokinetics, however, when taken together with other macrolides, theophylline concentration in blood plasma may increase.
If it is necessary to use it together with cyclosporine, it is recommended to control the content of cyclosporin in the blood. Despite, that there is no data on the effect of azithromycin on changes in the concentration of cyclosporin in the blood, other representatives of the macrolide class are able to change its level in blood plasma.
With the combined use of digoxin and azithromycin, it is necessary to control the level of digoxin in the blood, since many macrolides increase the absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma.
With the combined use of warfarin and azithromycin, careful monitoring of prothrombin time is recommended.
It was found that the simultaneous administration of terfenadine and macrolide antibiotics causes arrhythmia and lengthening of the QT interval. Based on this, the above complications cannot be excluded with the combined use of terfenadine and azithromycin.
Since it is possible to inhibit the CYP3A4 enzyme with azithromycin in parenteral form when co-administered with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs whose metabolism involves this enzyme, one should take into account the possibility of such interaction for azine ingestion.
When co-administered with azithromycin and zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or the excretion of its glucuronide metabolite by its kidneys. Nevertheless, the concentration of the active metabolite, phosphorylated zidovudine, in the mononuclear cells of peripheral vessels increases. The clinical significance of this fact is not clear.
With the simultaneous administration of macrolides with ergotamine and dihydroergotamine, their toxic effects may occur.
Overdose
Symptoms: nausea, dizziness, cyanosis, tachycardia, marked decrease in blood pressure, redness of the skin, fever (agitation), agitation, areflexia, tonico-clonic, symptomatic therapy.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 РC.
The product should be stored out of the reach and sight of children.
Shelf life
2 years.
Deystvuyushtee substance
Azithromycin
Terms and conditions
prescription
dosage form
capsules
Prescribing
Prescribing
Prescribing
Nursing mothers as prescribed by the doctor, For adults, Children over 12 years old, Berem nym on doctor's prescription
Obolensky AF Russian
Submit your review to Earn 10 Reward Points click here to login
Write Your Own Review