Universal reference book for medicines
Product name: OPTIGINAL (OPTIGINAL)

Active substance: lidocaine, sertaconazole

Type: Antifungal agent for topical application

Manufacturer: BIOKAD (Russia)

Composition, form of production and packaging
Suppositories vaginal
from white to white with a yellowish hue of color, cylindrical, with a pointed end, uniform in the longitudinal section;
On the cut, an air rod or a funnel-shaped depression is allowed.
1 supp.

sertaconazole nitrate 300 mg

lidocaine hydrochloride 10 mg

Excipients: sodium hydrophosphate - 1.44 mg, potassium dihydrogen phosphate - 0.038 mg, water d / and - 123.522 mg, macrogol 1500 - up to 2.5 g.

1 PC.
- packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

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 glabrata 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 glycinexylidine) having T 1/2 2 h and 10 h 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 blood stream in an insignificant amount.

INDICATIONS

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

DOSING MODE

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 Optiginol. 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 Optiginol. 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.
Children's age .
It is contraindicated to use the drug Optiginal in patients younger than 18 years, because clinical studies in this age group were not conducted.
SIDE EFFECT

To describe the frequency of adverse reactions, the following categories are used: 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 - a burning sensation, itching in the vagina.

CONTRAINDICATIONS

- hypersensitivity to sertaconazole, lidocaine, imidazole derivative, benzothiophene and other components of the drug;

- severe impairment of renal and hepatic function;

- Children's age under 18 years (efficiency and safety are not defined).

Carefully:

- impaired liver and kidney function.
Caution should be exercised in the case of prescribing the Optiginal to patients with reduced hepatic function and / or kidney function;
- genetic predisposition to malignant hyperthermia;

- Local infection in the field of application;

- trauma of the mucous membrane or skin in the area of ​​application;

- concomitant acute diseases;

- Weakened patients;

- elderly 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.

APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be used when prescribing Optiginal to patients with reduced renal function


APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Caution should be used when prescribing Optiginal to patients with reduced hepatic function


APPLICATION FOR CHILDREN

Contraindicated in children under the age of 18 years (efficacy and safety not determined).

APPLICATION IN ELDERLY PATIENTS

With caution should prescribe the drug to elderly patients


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.

Influence on ability to drive vehicles and work with mechanisms

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

OVERDOSE

Cases of an overdose of the Optiginal preparation 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.
DRUG 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 hepatic clearance of lidocaine (decreased metabolism due to inhibition of microsomal oxidation and decreased hepatic blood flow) and increase the risk of toxic effects (including the state of stun, drowsiness, bradycardia, paresthesia, etc.).

Barbiturates, phenytoin, rifampicin (inducers of microsomal liver enzymes) decrease the effectiveness (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 excitation of the central nervous system (CNS), 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.

TERMS OF RELEASE FROM PHARMACY

Released by prescription


TERMS AND CONDITIONS OF STORAGE

In dry, dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children. Shelf life - 2 years.
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