Optiginal - instructions for use, doses, side effects, contraindications

Active substances: sertaconazole nitrate 300 mg, lidocaine hydrochloride 10 mg. Excipients: sodium hydrophosphate 1.44 mg, potassium dihydrogen phosphate 0.038 mg, water for injection 123.522 mg, macrogol-1500 to 2.5 g.

Description:

Suppositories from white to white with a yellowish hue of color of cylindrical shape with a pointed end, homogeneous in the longitudinal section. On the cut, an air rod or a funnel-shaped depression is allowed!

Pharmacotherapeutic group:Antifungal agent

ATX: & nbsp

D Dermatology

Pharmacodynamics:

Sertaconazole is an antifungal drug, an imidazole derivative and a benzothiophene. In therapeutic doses, it exerts a fungistatic and fungicidal action. The mechanism of action is to inhibit the synthesis of ergosterol and increase the permeability of the cell membrane, which leads to lysis of the fungal cell.

It is active against Candida spp. (including Candida albicans, Candida tropicalis, Candida glabra! a and other fungi of the genus Candida).

Lidocaine - a local anesthetic, stabilizes the neuronal membrane, reduces its permeability for sodium ions, which prevents the occurrence and conduct of painful impulses. Expands blood vessels.

Pharmacokinetics:

Systemic absorption of sertaconazole after single intravaginal application is not available. When topical application creates stable high concentrations in the mucous membrane of the vagina.

Lidocaine is rapidly and almost completely metabolized in the liver (in unchanged form with local application with urine, less than 10% of the dose received into the systemic blood flow is excreted). The main pathway of metabolism is oxidative N-dealkylation, with the formation of active metabolites (monoethylglycinexylidine and glycinexylidin) having a half-life (T_1/2) 2 hours and 10 hours, respectively.

With liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value. With chronic renal failure, cumulation of metabolites is possible.

Penetrates through the blood-brain and placental barrier, is secreted with the mother's milk (40% of the concentration in the mother's plasma).

With topical application lidocaine can be absorbed into the systemic circulation in a small amount.

Indications:

Local treatment of infections of the vaginal mucosa caused by fungi of the genus Candida (candidiasis vulvovaginitis).

Contraindications:

Hypersensitivity to sertaconazole, lidocaine, imidazole derivative, benzothiophene and other components of the drug.

Severe violations of kidney and liver function.

Children under 18 years of age (efficacy and safety not defined).

Carefully:

Impaired liver and kidney function. Caution should be exercised when using Optiginal® in patients with reduced hepatic function and / or kidney function.

Other. Genetic predisposition to malignant hyperthermia, local infection in the field of application, trauma of the mucous membrane or skin in the field of application, concomitant acute diseases, weakened patients, advanced age.

Pregnancy and lactation:

Sufficient data on the use of sertaconazole during pregnancy and lactation are absent. Lidocaine penetrates the placenta. Lidocaine was used in a large number of pregnant women and women of childbearing age.Data on the violation of lidocaine reproductive processes (for example, increased frequency of malformations or any direct or indirect effect on the fetus) are not available. However, the risk to humans is not fully established. Studies on animals regarding the effect of lidocaine on pregnancy, embryo-fetal development, childbirth and postnatal development are incomplete. With intravaginal injection, the risk of lidocaine penetration into breast milk is minimal.

Given the single-use method, as well as the lack of systemic action of the components of the drug, its use during pregnancy and lactation is possible if the intended benefit of therapy for the mother exceeds the potential risk to the fetus and the baby.

Dosing and Administration:

The drug is administered intravaginally once. The suppository is injected deep into the vagina, lying on the back, before going to bed.

If clinical symptoms persist, the drug can be re-used after 7 days.

Before using the drug, you need to make a thorough toilet of the external genitalia using neutral soap.

Correction of the dosing regimen

The need for correction of the dosing regimen is decided individually with the attending physician.

Use in special patient groups

Patients with impaired renal function. In patients with reduced renal function, caution should be exercised when prescribing Optiginal®. Decreased kidney function does not affect the pharmacokinetics of lidocaine, but can cause accumulation of metabolites. The need for correction of the dosing regimen is decided individually with the attending physician.

Patients with impaired hepatic function. In patients with reduced liver function, caution should be exercised when prescribing Optiginal®. In patients with reduced liver function, the half-life may increase by 2 or more times. The need for correction of the dosing regimen is decided individually with the attending physician.

Patients with a genetic predisposition to malignant hyperthermia. Caution should be exercised when prescribing Optiginal® to patients who have a genetic predisposition to malignant hyperthermia.

Childhood. Contraindicated to use the drug Optiginal ® in patients under 18 years of age, becauseclinical studies in this age group were not conducted.

Side effects:

The following categories are used to describe the frequency of adverse reactions: very often (≥ 1/10), often (≥ 1/100; <1/10), infrequently (≥ 1/1000; <1/100), rarely (≥ 1/10000 ; <1/1000), very rarely (<1/10000).

Allergic reactions:

Rarely: hypersensitivity reactions (contact dermatitis, local erythema,

angioedema and other allergic reactions).

Local reactions:

Rarely: burning sensation, itching in the vagina.

Overdose:

Cases of overdose of Optiginal® are not registered.

If you randomly inject more suppositories than prescribed by your doctor, you may experience the following symptoms: hyperhidrosis, pale skin, dizziness, headache, drowsiness, disturbance of sensitivity, tremor, anxiety, psychomotor agitation, seizures, visual impairment, hypotension, cardiac rhythm disturbance , chills, methemoglobinemia. Treatment is symptomatic. There is no specific antidote.

Interaction:

Sertaconazole. Simultaneous use with local contraceptive drugs may lead to a weakening of the spermicidal effect of the latter.

Lidocaine. Cimetidine and propranolol reduce liver lidocaine clearance (decrease in metabolism due to inhibition of microsomal oxidation and decrease in hepatic blood flow) and increase the risk of toxic effects (including the state of stupor, drowsiness, bradycardia, paresthesia, etc.). Barbiturates, phenytoin, rifampicin (inducers of microsomal liver enzymes) reduce efficacy (an increase in dose may be required). When used with aymalin, phenytoin, verapamil, quinidine, amiodarone, an increase in the negative inotropic effect is possible. Joint use with beta-blockers increases the risk of bradycardia. Cardiac glycosides weaken the cardiotonic effect, curare-like drugs enhance muscle relaxation. Procainamide increases the risk of developing central nervous system (CNS) excitation, hallucinations. With the simultaneous use of lidocaine and hypnotics and sedatives, it is possible to intensify their inhibitory effect on the central nervous system. With intravenous injection of hexobarbital or thiopental sodium on the background of the action of lidocaine, respiratory depression is possible.With the simultaneous use of lidocaine and polymyxin B, it is possible to increase the inhibitory effect on neuromuscular transmission, so in this case it is necessary to monitor the function of the patient's breathing.

With intravaginal administration, there is no risk of unwanted drug interactions.

Special instructions:

Treatment can be done during menstruation.

The risk of rupture of barrier contraceptives (condoms or diaphragms) from latex increases with their simultaneous use with the drug. To prevent reinfection, simultaneous treatment of the sexual partner with local or systemic antifungal agents is recommended. During treatment it is recommended to abstain from sexual activity.

Do not allow the drug to enter the mucous membrane of the eyes, nose, mouth, open wounds or into the stomach. In case of accidental ingestion in the eyes, immediately wash them with water.

Consult your doctor if there is no improvement or new symptoms appear.

With the development of an allergic reaction the drug is canceled.

Effect on the ability to drive transp. cf. and fur:

Optiginal® does not affect the performance of potentially hazardous activities requiring special attention and quick reactions (management of vehicles, machinery, etc.).

Form release / dosage:

Vaginal suppositories 300 mg / 10 mg.

Packaging:

1 suppository in a contour cell box made of aluminum foil or PVC film.

On 1 contour acheikova packing together with the instruction on application in a pack from a cardboard.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package

Terms of leave from pharmacies:On prescription

Registration number:LP-002697

Date of registration:06.11.2014

Expiration Date:06.11.2019

The owner of the registration certificate:BIOCAD, CJSC BIOCAD, CJSC Russia

Manufacturer: & nbsp

BIOCAD, CJSC Russia

Information update date: & nbsp10.06.2017

Illustrated instructions

Instructions

Optiginal® (Optiginal)