Composition, form of production and packaging
? Vaginal suppositories are yellowish in color, flat with a rounded end in the form of a truncated ellipse.
1 supp.
thioconazole 100 mg
tinidazole 150 mg
Excipients: Witepsol 2250.0 mg.
7 pcs. - Packings without cell contour (1) from PVC / LDPE, complete with 7 disposable fingertips - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
The drug Gainomax is a combination of thioconazole and tinidazole. Tioconazole is a synthetic antifungal agent with a high activity against yeast-like and other fungi (dermatophytes). It is also effective against bacterial pathogens: Gardnerella vaginalis, Bacteroides spp., Some Gram-positive bacteria (including Staphylococcus and Sreptococcus spp.).
The mechanism of action of thioconazole is to increase the permeability of the fungal cell membrane by inhibiting the synthesis of ergosterol, its main component.Increasing the permeability of the cell membrane disrupts the intracellular ion balance, which leads to cell death. In clinical studies, it was shown that tioconazole is more effective than miconazole both in clinical terms (98% and 78%, respectively), and microbiologically (eradication of the pathogen in 76% and 67% of cases, respectively). In addition, the use of thioconazole compared with miconazole was subjectively two times more comfortable for patients.
Tinidazole is effective against both protozoal pathogens (Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia) and most anaerobic bacteria (Gardnerella vaginalis, Bacteroides fragilis, Bacteroides melaninogenicus, Bacteroides spp., Clostridium spp., Eubacterium spp., Peptostreptococcus spp., And Veillonella spp.).
The mechanism of action of tinidazole is not fully understood. The reduction of the nitro group is mediated by the ferredoxin system and a low oxidation-reduction potential, produced only by anaerobic bacteria. This fact may be the reason that the absorption of tinidazole is more active in anaerobes than in aerobes, although tinidazole penetrates the cell membranes of both, and others. In the course of the reduction reaction, active intermediate substances are formed and the diffusion gradient increases, which enhances the absorption of tinidazole.
Despite the fact that cross-resistance is typical for the group of 5-nitroimidazoles, 65-70% of strains of Trichomonas vaginalis, highly resistant to metronidazole, have an increased sensitivity to
Tinidazole.
According to clinical studies, the efficacy of the combination of thioconazole with tinidazole for intravaginal administration is 90-100%, with a microbiological recovery of 85%.
PHARMACOKINETICS
With intravaginal application, both thioconazole and tinidazole are slightly absorbed. Thus, the absorption of the two drugs in combination should be low.
INDICATIONS
- treatment of vaginitis caused by pathogens of genera Candida, Trichomonas and Gardnerella (vaginal candidiasis, trichomonas vulvovaginitis, gardnerellevic vaginitis, unspecific vaginitis), as well as mixed infection.
DOSING MODE
Intravaginal.
The drug is prescribed for 1 vaginal suppository at night for 7 days. Alternative scheme of admission: 1 vaginal suppository 2 times a day (morning and night) for 3 days.
Vaginal suppositories should be injected deep into the vagina with disposable fingertips contained in the package.
Elderly patients
When prescribing the drug, elderly patients (over 65 years of age) do not need to change the dosage regimen.
SIDE EFFECT
Side effects according to the results of clinical studies. In clinical trials, combinations of tinidazole 150 mg with thioconazole 100 mg in the form of a cream or vaginal tablets, clinical and microbiological indicators were evaluated in total in 348 patients, both regimens were evaluated (3 or 7 days).
According to the results of the studies, the safety of this combination was assessed as high. The following side effects were observed: allergic reactions (in 3.3-4.5% of cases), local itching (1.9%) and burning sensation (1.7%). In most cases, the side effects were of moderate severity, only 0.75% of patients interrupted treatment due to allergic reactions.
Postmarketing experience of application.
In the postmarketing practice of the drug, additional adverse events were reported:
Local reactions: rarely - edema, irritation of the mucous membrane of the vagina.
From the side of the central nervous system and peripheral nervous system: rarely - headache,
fatigue. .
From the side of the urinary system: rarely - darkening of urine.
Allergic reactions: rarely - skin rash, hives, in some cases - angioedema.
Although no cases of transient leukopenia were observed with intravaginal application of the combination of thioconazole and tinidazole, cases of this symptom associated with neurologic or gastrointestinal symptoms associated with systemic administration of tinidazole were described.
CONTRAINDICATIONS
- organic diseases of the nervous system at present or in the anamnesis;
- leukemia, violations of hemopoiesis;
- I trimester of pregnancy, lactation period;
- virginity, age till 18 years;
- Hypersensitivity to the active components or their derivatives, other components of the drug.
PREGNANCY AND LACTATION
Tinidazole penetrates the fetoplacental barrier, as well as into breast milk. Effects of the components of this drug on the development of the fetus and the newborn are not known.
Gainomax is contraindicated in the first trimester of pregnancy. At the time of treatment of drugs Gainomax should stop breastfeeding. The use of the drug Gainomax in the III trimester of pregnancy should be evaluated by the attending physician in terms of the ratio of the potential benefit to the mother and the possible risks to the fetus.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years of age, virgins.
APPLICATION IN ELDERLY PATIENTS
When prescribing the drug, elderly patients (over 65 years of age) do not need to change the dosage regimen.
SPECIAL INSTRUCTIONS
Despite the fact that in the clinical trials there were no stable hematologic abnormalities on the background of the drug, tinidazole can not be taken in patients with diseases of the hematopoiesis system (leukemia, hemopoiesis disorders) at the present time or in the anamnesis.
The drug Gainomax should not be used simultaneously with the means of mechanical contraception (condoms, contraceptive caps or diaphragms), because the suppository base can react with the latex base of these agents.
Alcohol intake should be excluded during the administration of the drug, and also within 2 days after the last dose. The drug should not be stored in the refrigerator.
Impact on the ability to drive vehicles and manage mechanisms
The intake of the drug Gainomax does not affect the ability to drive vehicles and mechanisms.
OVERDOSE
If a large amount of the drug is ingested orally, a gastric lavage is performed. There is no specific antidote, they carry out symptomatic therapy.
DRUG INTERACTION
Simultaneous reception of alcohol and tinidazole in a dosage form for systemic action can cause intestinal colic, nausea and vomiting, and reddening of the skin.
Despite the fact that the use of tinidazole in the vaginal suppositories minimizes the intake of the drug in the systemic circulation, interaction with alcohol must be taken into account when prescribing the drug.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
Store at a temperature not exceeding 25 В° C. Keep out of the reach of children. Shelf life - 2 years.
