Instruction for use: Generolon

Active substance Minoxidil

ATX code D11AX01 Minoxidil

Pharmacological group

dermotropic means

Nosological classification (ICD-10)

L64 Androgenic alopecia

Alopecia androgenic, Androgenetic alopecia, Androgenic alopecia of moderate severity, Severe Androgen-Dependent Alopecia, Male pattern hair loss

L65 Other nerubtsuyuschayasya hair loss

Cronkheta-Canada syndrome, Alopecia, Hair loss, Hair loss due to environmental factors, Diffuse hair loss non-hormonal etiology, Increased hair loss

Composition

Spray for external use 1 ml

active substance:

minoxidil 20 mg

50 mg

auxiliary substances: ethanol (96%) - 571/243 mg; propylene glycol 104/520 mg; water - up to 1 ml

Description of dosage form

Colorless or slightly colored with a yellowish hue, a clear aqueous alcohol solution with the smell of alcohol.

pharmachologic effect

Pharmacological action - stimulating hair growth.

Pharmacodynamics

As a peripheral vasodilator, with topical application, minoxidil enhances microcirculation in the area of the hair follicles. Minoxidil stimulates the growth factor of the vascular endothelium, which, presumably, is responsible for increasing the permeability of capillaries, which indicates a high metabolic activity observed in the anagen phase.

Minoxidil stimulates hair growth in patients with hereditary hair loss (androgenic alopecia) in the initial stage.

The exact mechanism of action of minoxidil for external use in hair loss is not fully understood.

Pharmacokinetics

Suction. With external use, minoxidil is poorly absorbed through intact skin: an average of 1.5% (1-2%) of the total applied dose enters the systemic circulation.

The mean values of AUC and Cmax for a 5% minoxidil solution were approximately 18.71 ng · h / ml and 2.13 ng / ml, respectively, with a 2% minoxidil solution of 7.54 ng · h / ml and 1.25 ng / ml, respectively. Tmax with a 5% solution of minoxidil is 5.79 hours.

The effect of minoxidil on hemodynamics is not expressed until the average serum concentration of minoxidil reaches 21.7 ng / ml.

Distribution. Although it was previously reported that minoxidil does not bind to blood plasma proteins, it was later demonstrated in vitro by its in vitro ultrafiltration that it reversibly binds to human plasma proteins in the 37-39% range. Since only 1-2% of the minoxidil applied externally is absorbed, the degree of its binding to plasma proteins is clinically insignificant.

Metabolism. Approximately 60% of minoxidil is metabolized with the formation of minoxidil glucuronide mainly in the liver.

Excretion. T1 / 2 minoxidil for external use averages 22 hours. 97% of minoxidil and its metabolites are excreted by the kidneys and 3% by the intestine.

After discontinuation of the drug, approximately 95% of the minoxidil applied topically is excreted within 4 days.

Indications for Generolon®

Treatment of alopecia in men and women.

Contraindications

increased sensitivity to minoxidil or other components of the drug;

violation of the integrity of the skin;

dermatosis of the scalp;

simultaneous application of other drugs on the scalp;

pregnancy;

the period of breastfeeding;

age younger than 18 years;

age over 65 years.

With caution: cardiovascular disease and arrhythmia, renal and hepatic insufficiency *.

* Before starting treatment, consult a physician.

pregnancy and lactation

Do not use the drug during pregnancy and during breastfeeding.

Side effects

To indicate the frequency of side effects, the following classification is used: very often (≥1 / 10); often (≥1 / 100 and <1/10); infrequently (≥1 / 1000 and <1/100); rarely (≥1 / 10000 and <1/1000); very rarely (<1/10000), including individual messages; frequency is unknown - can not be estimated from the available data.

From the nervous system: often - headache; very rarely - dizziness.

From the skin and subcutaneous tissues: often - skin itching, rash; rarely - dermatitis, manifested in the form of redness, flaking and inflammation; very rarely - temporary hair loss, hair color change, hair texture disorder, hypertrichosis (unwanted hair growth outside the site of application), reactions at the site of application (can spread to the ears and face, include pruritus, irritation, pain, rash, swelling, dryness skin, erythema, but in some cases, the reactions may be more severe, including exfoliation, dermatitis, blistering, bleeding, ulceration).

From the side of the immune system: very rarely - angioedema (manifestations of which can be swelling of the lips, oral cavity, oropharynx, pharynx and tongue), hypersensitivity (manifestations of which may be generalized erythema, generalized skin itching, face swelling and a feeling of tightness in the throat) , allergic contact dermatitis.

From the side of the organ of vision: very rarely - irritation of the eyes.

From the heart: very rarely - tachycardia, a feeling of palpitations.

From the respiratory system, chest and mediastinum: very rarely - shortness of breath.

From the digestive tract: very rarely - nausea, vomiting.

General disorders and disorders at the injection site: very rarely - peripheral edema, pain in the chest.

From the side of the vessels: infrequently - a decrease in blood pressure.

If any of the side effects listed in the manual are aggravated or any other side effects not indicated in the instructions appear, you should notify the doctor.

Interaction

There is a theoretical possibility of strengthening orthostatic hypotension in patients receiving concomitant treatment with peripheral vasodilators (no clinical confirmation). We can not rule out a very slight increase in the minoxidil content in the blood of patients suffering from hypertension and taking minoxidil orally in the case of the simultaneous use of Generolon®, although relevant clinical studies have not been carried out.

It was found that minoxidil for external use can interact with certain drugs for external use. The simultaneous use of a solution of minoxidil for external use and cream containing betamethasone (0.05%) leads to a decrease in the systemic absorption of minoxidil.

Simultaneous application of cream containing tretinoin (0.05%) leads to increased absorption of minoxidil.

The simultaneous application of minoxidil to the skin and preparations for external use such as tretinoin and dithranol, which cause a change in the protective functions of the skin, may lead to an increase in the absorption of minoxidil.

Dosing and Administration

Locally.

Regardless of the size of the treated area, apply 1 ml of solution with a nebulizer (7 strokes) 2 times a day to the affected areas of the scalp, starting from the center of the problem area. After application, wash hands.

The total daily dose should not exceed 2 ml (the dose does not depend on the size of the affected area). Patients who, when using a 2% solution, do not have satisfactory hair growth, and patients for whom faster hair growth is desired, a 5% solution can be used.

For men, the drug Generolon® is most effective at hair loss on the crown, for women - with hair loss in the middle part.

The drug Generolon® is applied only to the dry skin of the scalp. The solution does not require flushing. For the effectiveness of the drug and the achievement of hair follicles, it is important to apply the drug to the scalp, not to the hair.

The appearance of the first signs of suspension of hair loss and restoration of hair growth is possible after applying the drug 2 times a day for 2-4 months. The beginning and degree of growth of hair, as well as the quality of growing hair, can fluctuate in different patients. To achieve and maintain the achieved effect of restoring hair growth, the patient should not interrupt the use of the drug, otherwise hair loss will resume. An increase in the dose of the drug or its more frequent use will not lead to an improvement in the results of therapy. If, after the use of the drug Generolon® for 16 weeks, hair growth is not increased, then the drug should be discontinued.

After the introduction of the drug Generolon®, increased hair loss can occur. This effect is caused by the influence of minoxidil. It is expressed in stimulating the hair transition from the resting phase (telogen) to the growth phase (anagen). Thus, there is a loss of old hair, on the site of which grow new. Temporary increase in hair loss usually lasts for 2-6 weeks from the start of treatment, and then decreases within 2 weeks. If the increased hair loss continues, then the drug should be discontinued and consult with a doctor.

According to individual reports, within 3-4 months after the cessation of treatment can be expected to restore the original appearance.

The duration of treatment on average is about 1 year.

Special groups of patients. There are no recommendations on dosing of Generolon® for use in patients with renal and hepatic insufficiency.

Preparation for use. Remove the screw cap and fix the measuring pump. On the tube on top of the pump, strengthen the elongated nozzle for spraying. Before the first use, press the spray nozzle 3-4 times to allow the pump to fill with the solution, after which the preparation can be used.

Overdose

Accidental ingestion of the drug Generolon® can cause systemic side effects due to the vasodilating properties of minoxidil (5 ml of a 2% solution contains 100 mg of minoxidil, the maximum recommended dose for adults when ingested for the treatment of hypertension, 5 ml of a 5% solution contains 250 mg of minoxidil, i.e., a dose 2.5 times the maximum recommended daily intake for adults for oral administration in the treatment of hypertension).

If doses exceeding the recommended levels are applied to large areas of the body or other parts of the body other than the scalp, an increase in the systemic absorption of minoxidil may be possible, which may lead to the development of undesirable events.

Symptoms: fluid retention, decreased blood pressure, tachycardia, dizziness.

Treatment: diuretics may be prescribed to eliminate fluid retention if necessary; for the treatment of tachycardia - beta-blockers. For the treatment of arterial hypotension, a 0.9% solution of sodium chloride should be administered. Do not prescribe sympathomimetic drugs, such as norepinephrine and epinephrine, which have excessive cardiostimulating activity.

special instructions

Apply Generolon® should only be applied to the healthy scalp skin. You can not use it for inflammation, infection, irritation, soreness of the skin, and also at the same time as other medicinal products applied to the scalp.

The drug Generolon® should be applied only on the dry skin of the scalp after bathing or wait about 4 hours after applying the drug before bathing.

Do not let your head get wet earlier than 4 hours after application.

After applying the drug, you should wash your hands thoroughly.

Wash hair with the drug Generolon® is recommended in the usual mode.

Before starting treatment with Generolon®, patients should undergo a general examination, including the collection and study of medical history. The physician should make sure that the scalp skin is healthy.

Minoxidil can be absorbed in small amounts in small amounts, and there is a risk of systemic side effects such as water and salt retention, generalized and local edema, pericardial effusion, pericarditis, pericardial tamponade, tachycardia, angina pectoris, increased orthostatic hypotension, caused by certain antihypertensive agents, for example, guanethidine and its derivatives. The use of generolon ® in patients with hypertension receiving treatment with guanethidine or its derivatives, or minoxidil, is possible only under conditions of medical observation. Patients should undergo periodic examinations to identify possible signs of systemic side effects of minoxidil. Patients with a history of cardiovascular disease should be warned that treatment with Generolon® can exacerbate these diseases.

When systemic side effects or severe skin reactions occur, patients should cancel the drug and consult a doctor.

During the period of using the drug Generolon®, you can use hair spray and other hair care products. Before applying hair care products, first apply Generolon® and wait until the treated area of the skin is completely dry. Data that hair coloring, perming or using hair softeners can reduce the effectiveness of the drug, are absent. However, to prevent possible irritation of the skin of the scalp, you need to make sure that the product has been completely washed off from the hair and scalp before using these chemicals.

The preparation generolon® includes ethyl alcohol, which can cause inflammation and eye irritation. In case of contact with sensitive surfaces (eyes, irritated skin, mucous membranes), rinse the area with plenty of cold water.

The drug will not be effective when using a hair dryer immediately after applying the product to the scalp; hair care products that can cause scarring, as well as deep scalp burns; methods of hair care, requiring a strong pulling hair from the scalp (for example braiding tight braiding (brading) or a horse-tail hair).

Do not use generolon ® in cases of sudden hair loss, focal alopecia, when alopecia develops after birth, in case of baldness caused by taking drugs, malnutrition (iron deficiency, vitamin A), as a result of hair styling in tight hair, and also in the case where the cause of hair loss is unknown.

If blood pressure drops or if chest pain, rapid heartbeat, weakness or dizziness, sudden unexplained weight gain, edema of the hands or feet, persistent redness or irritation of the scalp, discontinue use and consult a doctor.

Accidental ingestion of the drug inside can lead to the development of serious adverse events from the heart. Therefore, this product should be stored in places inaccessible to children.

Avoid inhalation during spraying.

Impact on the ability to manage vehicles and mechanisms. In connection with the possible development of headache, dizziness, eye irritation, care should be taken when driving vehicles and engaging in certain activities that require increased concentration of attention and rapid motor reaction. When these undesirable phenomena appear, one should refrain from performing these activities.

Form of issue

Spray for external use, 2% and 5%. 60 ml of the solution in a white bottle of HDPE with a screw cap of polypropylene white, equipped with a plastic ring of the first opening control. 1 or 2 fl. complete with 1 plastic measuring pump and 1 nozzle for spraying in a protective bag are placed in a cardboard box. 3 fl. complete with 2 plastic measuring pumps and 2 nozzles for spraying in a protective bag are placed in a cardboard box.

Conditions of leave from pharmacies

Without recipe.

storage Conditions

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life of Generolon®

spray for external use 2% - 3 years.

spray for external use 5% - 4 years.

Do not use after the expiry date printed on the package.