SAFOЦID
Active material: Azithromycin, Fluconazole, Seknidazol
When ATH: J01FA10
CCF: Combination drug with antiprotozoal, antifungal and antibacterial effect
ICD-10 codes (testimony): A54, A56.0, A56.1, A59, B37.3, N30, N34, N72, N76
When CSF: 06.07.01
Manufacturer: Lyka Labs Ltd.. (India)
Pharmaceutical form, composition and packaging
A set of tablets three species:
Tablets pink, round, Valium, a facet and Valium; on a break - pink (1 PC. in blister).
| 1 tab. | |
| fluconazole | 150 mg |
Excipients: microcrystalline cellulose, calcium phosphate dibasic (anhydrous), sodium croscarmellose, magnesium stearate, colloidal silicon dioxide, dye “пунцовый лак 4R”.
Pills, coated pinks, kapsulovidnoy form, lenticular, with Valium; on a break - a kernel white or nearly white. (1 PC. in blister).
| 1 tab. | |
| azithromycin | 1 g |
Excipients: sodium lauryl, sodium croscarmellose, povidone K-30, magnesium stearate, colloidal silicon dioxide (anhydrous).
The composition of the shell: gipromelloza, diethyl phthalate, talc (magnesium silicate peeled), Titanium dioxide, macrogol 4000, dye “пунцовый лак 4R”.
Pills, coated white or nearly white, kapsulovidnye, lenticular, with Valium; on a break - white or nearly white (2 PC. in blister).
| 1 tab. | |
| seknidazol | 1 g |
Excipients: corn starch, microcrystalline cellulose, colloidal silicon dioxide (anhydrous), sodium starch glycolate, povidone-30, Talcum cleared, magnesium stearate.
The composition of the shell: hydroxypropyl, diethyl phthalate, Talcum cleared, Titanium dioxide, macrogol 4000.
4 PC. – blisters (1) – packs cardboard.
Pharmacological action
Combination set, containing an antifungal drug, antibiotic and antibacterial drug with antiprotozoal activity.
Fluconazole – antifungal agent, triazole derivative, It is a potent selective inhibitor of sterol synthesis in the fungal cells.
Effektiv at opportunističeskih mycosis, incl. caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Also shown activity flukonazola models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.
Azithromycin – broad spectrum antibiotic, a representative subgroup of macrolide antibiotics - azalides. When you create inflammation in high concentrations has a bactericidal effect.
It is active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus Group C, F and G, Staphylococcus aureus, Streptococcus viridans; Gram negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; Some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp., and also Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pale, Borrelia burgdorferi.
Azithromycin are not active against Gram-positive bacteria, erythromycin resistant.
Seknidazol – antimicrobial germicide, synthetic derivative of nitroimidazole.
It is active against obligate anaerobic bacteria (slowly- and nesporoobrazuющih), Some agents of protozoal infections: Trichomonas vaginalis, Giardia lamblia, Entamoeba histolytica.
Seknidazol are not active against aerobic bacteria.
It increases the sensitivity of tumors to radiation, causing sensitization to ethanol (disulfiramopodobnyh action). Interaction with DNA, It is a violation of the spiral structure, break threads, inhibition of the synthesis of nucleic acids and cell death.
Pharmacokinetics
Fluconazole
Absorption
After oral administration fluconazole is well absorbed from the gastrointestinal tract, bioavailability of 90%. In the fasting state at a dose 150 mg Cmax in plasma is 90% the content in the plasma during on / in – 2.5-3.5 mg / l. Simultaneous food intake does not affect the absorption of the drug, ingested. Cmax plasma peaking 0.5-1.5 h after administration. Plasma concentration is directly proportional to the dose.
Distribution
Bolus (first day), in 2 times the normal daily dose, achieves a concentration, appropriate 90% Css, to 2 Day. Before the drug 1 time / day 90% Level Css It is achieved by 4-5 Day Treatment.
Vd It is approaching the total water content in the body. Plasma protein binding – 11-12%.
Fluconazole penetrates well into all body fluids. Drug concentrations in saliva and sputum are similar to its level in plasma. In patients with fungal meningitis, fluconazole content in cerebrospinal fluid reaches 80% of its level in plasma. In the stratum corneum, epidermis, derma and sweat liquid reaches high concentrations, which exceed serum.
Deduction
T1/2 Fluconazole is about 30 no.
About 80% excreted in the urine as unchanged. The clearance of fluconazole is proportional QC. Fluconazole metabolites in peripheral blood has been detected.
Azithromycin
Absorption
After oral administration, azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic medium and lipophilicity. At a dose of 500 mg Cmax azithromycin plasma levels achieved after 2.5-2.96 h and is 0.4 mg / l. Bioavailability is 37%.
Distribution
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (incl. in prostate), in skin and soft tissue. High concentrations in tissues (in 10-15 times higher, than in blood plasma) and a long T1/2 due to low binding of azithromycin from plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrate in medium with low pH, environmental lysosomes. This in turn determines the big Vd – 31.1 l / kg and a high plasma clearance.
The ability of azithromycin to accumulate mainly in lysosomes is important for elimination of intracellular pathogens. Proved, that phagocytes deliver azithromycin to the localization of infection, where it is released in the process of phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher, than in healthy tissues (on average 24-34%) and correlate with the degree of inflammatory edema. Despite the high concentration in phagocytes, Azithromycin has no significant effect on their function. Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatments.
Metabolism
It is metabolized in the liver by demethylation, metabolites formed are inactive.
Deduction
Derivation of azithromycin in plasma passes 2 Phase: T1/2 is 14-20 hours, ranging from 8 to 24 hours after dosing and 41 no – in the range of 24 to 72 no, allowing you to use the drug 1 time / day.
Seknidazol
Absorption and distribution
Absorption vыsokaya, bioavailability of 80%. After a single oral dose 2 г Tmax is 4 no.
It penetrates through the placental barrier, excreted in breast milk.
Metabolism and excretion
It is metabolized in the liver.
Excreted in the urine within 72 no (16% dose).
Testimony
Co-infection of the urinary tract, Sexually Transmitted Infections:
- Gonorrhea;
- Trichomoniasis;
- Chlamydia;
- Bacterial vaginosis;
- Fungal Infections;
- Related specific and nonspecific cystitis, uretrity, vulvovaginitises, cervicitы.
Dosage regimen
The drug is taken orally – all at once 4 tab. (1 tab. flukonazola, 1 tab. azithromycin and 2 tab. seknidazola), included in the blister, for 1 hours before meals or 2 hours after a meal once.
Side effect
Cardio-vascular system: rarely – heart rhythm disturbances.
From the digestive system: nausea, vomiting, diarrhea, digestive disorders, stomach ache, flatulence, anorexia.
From the senses: rarely – taste disturbances.
From the hematopoietic system: leukopenia.
Allergic reactions: skin rashes, itch, anaphylactic reactions.
Other: rarely – headache, dizziness, stomatitis.
Contraindications
- Organic diseases of the central nervous system;
- Concurrent use of terfenadine, astemizole or other drugs, prolonging the QT interval;
- Pregnancy;
- Lactation;
- Children's age;
- Hypersensitivity to fluconazole or other azole compounds;
- Hypersensitivity to azithromycin and other macrolides;
- Hypersensitivity to seknidazol and other nitroimidazole.
FROM caution the drug should be used in conjunction with cisapride, rifabutin or other drugs, metabolized by cytochrome P450 isoenzymes.
Pregnancy and lactation
Safotsid is contraindicated during pregnancy and lactation (breast-feeding).
Cautions
Concomitant use of fluconazole and oral hypoglycemic agents in diabetic patients may be, However, the physician should bear in mind the possibility of hypoglycemia.
When concomitant administration of warfarin and azithromycin requires careful monitoring of the prothrombin time.
Overdose
Data on drug overdose Safotsid not provided.
Drug Interactions
Fluconazole
With simultaneous use of fluconazole and warfarin increased the prothrombin time, average, on 12%. In this connection, it is recommended to carefully monitor the performance of prothrombin time in patients, receiving the drug in conjunction with anti kumarinovyh.
Флуконазол увеличивает T1/2 plasma from oral hypoglycaemic agents – sulfonylureas (incl. hlorpropamyd, glibenclamide, glipizide, tolbutamid) in healthy humans. Concomitant use of fluconazole and oral hypoglycemic agents may be, but a doctor should keep in mind the possibility of hypoglycemia.
Patients, receiving high doses of theophylline or who have a chance of developing theophylline intoxication, must be supervised for early detection of the symptoms of an overdose of theophylline, tk. administration of fluconazole reduces the average rate of clearance from the plasma theophylline.
Concomitant use of fluconazole with terfenadiom, astemizole or other drugs, prolonging the QT interval.
With simultaneous use of fluconazole with cisapride, rifabutin or other drugs, metabolized isoenzymes of P450 should be careful.
Azithromycin
Antacids (aluminum and magnesium-), ethanol and food slows down and reduces the absorption of azithromycin.
With simultaneous use of warfarin and azithromycin (at conventional doses) changes in prothrombin time is not revealed, However, the interaction of macrolides and warfarin may increase the anticoagulant effect. You should carefully monitor the prothrombin time in patients.
With simultaneous use of azithromycin with digoxin concentration in blood plasma increases.
With simultaneous use of azithromycin with ergotamine or dihydroergotamine amplified the toxic effect (vasospasm, dysesthesia).
Azithromycin slows down and increases the plasma concentration and toxicity of cycloserine, anticoagulants, methylprednisolone, Felodipine, and drugs, undergoing microsomal oxidation (incl. Carbamazepine, terfenadine, cyclosporine, geksoʙarʙital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemics, Theophylline and other xanthine derivatives), by inhibiting microsomal oxidation in hepatocytes azithromycin.
Linkozaminy weaken, tetracycline and chloramphenicol enhance the efficacy of azithromycin.
Seknidazol
Enhances hypoglycemic effect of insulin and oral hypoglycemic agents. When combined with ethanol development disulfiramopodobnyh reaction (incl. stomach cramps, nausea, vomiting, headache, flushing).
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children, dry, dark place at temperatures not above 30 ° C. Shelf life – 3 year.
