Оптигинал®

General characteristics. Structure:

Active ingredients: 300 mg of a sertakonazol of nitrate, 10 mg of lidocaine of a hydrochloride.

Excipients: sodium hydrophosphate, potassium dihydrophosphate, water for injections, a macrogoal.

Pharmacological properties:

Pharmacodynamics. Sertakonazol - antifungal drug, derivative an imidazole and petrolthiophene. In therapeutic doses has fungistatic and fungicidal effect. The mechanism of action consists in oppression of synthesis of ergosterol and increase in permeability of a cellular membrane that leads to a lysis of a cell of a mushroom.

It is active concerning Candida spp. (including Candida albicans, Candida tropicalis, Candida glabra! and and other mushrooms of the sort Candida).

Lidocaine - local anesthetic, stabilizes a neyronalny membrane, reduces its permeability for sodium ions that interferes with emergence and carrying out painful impulses. Expands vessels.

Pharmacokinetics. System absorption of a sertakonazol after single intravaginalny use is absent. At topical administration creates stable high concentration in a mucous membrane of a vagina.

Lidocaine quickly and almost is completely metabolized in a liver (in not changed view at topical administration with urine less than 10% of the dose which came to a system blood stream are removed). The main way of metabolism - oxidizing N-dealkylation, at the same time the active metabolites (моноэтилглицинксилидин and глицинксилидин) having an elimination half-life (T1/2) of 2 h and 10 h respectively are formed.

At liver diseases intensity of metabolism decreases and makes from 50% to 10% of a normal amount. At a chronic renal failure cumulation of metabolites is possible.

Gets through a blood-brain and placental barrier, cosecretes with maternal milk (40% of concentration in mother's plasma).

At topical administration lidocaine can be soaked up in a system blood stream in insignificant quantity.

Indications to use:

Topical treatment of the infections of a mucous membrane of a vagina caused by sort Candida mushrooms (a candidosis vulvovaginitis).

Route of administration and doses:

Drug is used intravaginalno once. Suppository is entered deeply into a vagina, lying on spin, before going to bed.

In case of preservation of clinical symptoms perhaps repeated use of drug in 7 days.

Before use of drug it is necessary to make a careful toilet of external genitals with use of neutral soap.

Correction of the mode of dosing. Need of correction of the mode of dosing is solved individually together with the attending physician.

Use for special groups of patients. Patients with renal failures. At patients it is necessary to be careful with reduced function of kidneys at purpose of the drug Optiginal®. Depression of function of kidneys does not influence lidocaine pharmacokinetics, but can cause accumulation of metabolites. Need of correction of the mode of dosing is solved individually together with the attending physician.

Patients with abnormal liver functions. At patients it is necessary to be careful with reduced function of a liver at purpose of the drug Optiginal®. At patients with reduced function of a liver the elimination half-life can increase in 2 and more times. Need of correction of the mode of dosing is solved individually together with the attending physician.

Patients with genetic predisposition to a malignant hyperthermia. It is necessary to be careful at purpose of the drug Optiginal4 to the patients having genetic predisposition to a malignant hyperthermia.

Children's age. It is contraindicated to use the drug Optiginal® at patients 18 years since clinical trials in this age group were not conducted are younger.

Features of use:

Pregnancy and lactation. Sufficient data about use of a sertakonazol at pregnancy and in the period of a lactation are absent. Lidocaine gets through a placenta. Lidocaine was applied at a large number of pregnant women and women of childbearing age. Data on disturbance by lidocaine of reproductive processes (for example, increase in frequency of malformations either any direct or indirect impact on a fruit) are absent. Nevertheless, the risk for the person is up to the end not established. Researches on animals concerning influence of lidocaine on pregnancy, embrio-fetalis development, childbirth and post-natal development incomplete. At intravaginalny introduction the risk of penetration of lidocaine into breast milk is minimum.

Considering a single route of administration, and also lack of systemic action of components of drug, its use during pregnancy and a lactation is possible if the estimated advantage of therapy for mother surpasses potential risk for a fruit and the child.

Treatment can be carried out to periods time.

The risk of a rupture of barrier contraceptives (condom or diaphragm) from latex increases at their simultaneous use with drug. For prevention of reinfection it is recommended to carry out simultaneous treatment of the sexual partner by means of local or system antifungal drugs. During treatment it is recommended to abstain from sex life.

Not to allow hit of drug on a mucous membrane of eyes, a nose, a mouth, open wounds or in a stomach. At accidental hit of drug in eyes, it is necessary to wash out immediately them water.

To consult with the doctor if improvement does not occur or new symptoms appear.

At development of allergic reaction drug is cancelled.

Influence on ability to manage vehicles and mechanisms. Оптигинал® does not influence performance of potentially dangerous types of activity requiring special attention and bystry reactions (control of vehicles, the machine equipment, etc.).

 

Side effects:

For the description of frequency of side reactions the following categories are used: very often (> 1/10), it is frequent (> 1/100; <1/10), infrequently (> 1/1000; <1/100), it is rare (> 1/10000; <1/1000), it is very rare (<1/10000).

Allergic reactions. Seldom: hypersensitivity reactions (contact dermatitis, local erythema, Quincke's disease and other allergic reactions).

Local reactions. Seldom: a burning sensation, an itch in a vagina.

Interaction with other medicines:

Sertakonazol. Simultaneous use with local contraceptive drugs can lead to weakening of spermicidal action of the last.

Lidocaine. Cimetidinum and propranolol reduce hepatic clearance of lidocaine (decrease in metabolism owing to inhibition of a microsomal oxidation and decrease in a hepatic blood-groove) and increase risk of development of toxic effects (including a condition of an oglushennost, drowsiness, bradycardia, paresthesias, etc.).

Barbiturates, Phenytoinum, rifampicin (inductors of microsomal enzymes of a liver) reduce efficiency (increase in a dose can be required).

At use with Ajmalinum, Phenytoinum, verapamil, quinidine, Amiodaronum strengthening of a negative inotropic effect is possible. Combined use with beta adrenoblockers increases risk of development of bradycardia.

Cardiac glycosides weaken cardiotonic effect, kurarepodobny medicines strengthen a muscular relaxation. Procaineamide increases risk of development of excitement of the central nervous system (CNS), hallucinations.

At simultaneous use of lidocaine and somnolent and sedative medicines strengthening of their oppressing action on TsNS is possible.

At intravenous administration of hexobarbital or thiopental of sodium against the background of effect of lidocaine respiratory depression is possible.

At simultaneous use of lidocaine and polymyxin B strengthening of the oppressing influence on neuromuscular transmission therefore in that case it is necessary to monitor function of breath of the patient is possible.

At intravaginalny introduction the risk of emergence of undesirable medicinal interaction is absent.

Contraindications:

Hypersensitivity to a sertakonazol, lidocaine, derivatives of an imidazole, benzthiophene and other components of drug.

Heavy renal failures and liver.

Children's age up to 18 years (efficiency and safety are not defined).

With care. Abnormal liver function and kidneys. It is necessary to be careful in case of purpose of the drug Optiginal® to patients with reduced function of a liver and/or kidneys.

Other. Genetic predisposition to a malignant hyperthermia, a local infection in a scope, an injury of a mucous membrane or integuments in scopes, the accompanying acute diseases weakened patients, advanced age.

Overdose:

Cases of overdose of the drug Optiginal® are not registered.

At accidental one-time introduction of bigger number of suppositories, than it is offered the doctor, emergence of the following symptoms is possible: hyperhidrosis, pallor of integuments, dizziness, headache, drowsiness, disturbance of sensitivity, tremor, concern, psychomotor excitement, spasms, vision disorder, hypotonia, disturbance of a cordial rhythm, fever, methemoglobinemia. Symptomatic treatment. There is no specific antidote.

Storage conditions:

In the dry place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging

Issue conditions:

According to the recipe

Packaging:

Suppositories vaginal 300 mg / 10 mg. Packaging: on 1 suppository in a blister strip packaging from aluminum foil or a film polyvinyl chloride. On 1 blister strip packaging together with the application instruction in a pack from a cardboard.