Neotigazon: reviews and efficiency, price, instruction manual, analogues

Neotigazone is a pharmacological preparation structurally not different from tretinoin or retinoic acid( a derivative of vitamin A) made synthetically and specialized for the treatment of dermatological pathologies occurring in severe form and stimulating the process of tissue repair( restoration).

Features of the drug

Dosage forms

Producer Neotigazona - pharmaceutical company Actavis Group( Iceland). The drug is available in the form of capsules with an active substance content of 10 or 25 mg, placed in the cells of the contour package of 30, 50 and 100 pieces.

The capsule shell consists of two halves - brown and white-beige. The capsule inscription indicates the amount of drug in milligrams of 10 or 25. The contents are a fine powder substance with small inclusions of light yellow and yellow.

Composition of Neotigazone

Composition of 1 capsule: 10 or 25 mg of active ingredient of acitretin, a substance that stimulates regeneration processes.

Additional ingredients: gelatin, natural polymer - microcrystalline cellulose, food additive - sodium ascorbate( form of vitamin C), and as a thickener - maltodextrin.

Prices

The cost of Neotigazone varies significantly by region, and in different Russian pharmacies in rubles is approximately:

• package with 30 capsules containing 10 mg of acitretin - 3,500-5,500;
• packing of 30 pieces of 25 mg - from 6 000 to 8 000.

Pharmacological action

Pharmacodynamics

Active ingredient - acitretin - is a retinoid( a biological compound similar to vitamin A, affecting the whole body). The mechanism of therapeutic influence has not been fully investigated. It has been established that the use of drugs in the treatment of severe dermatological diseases, which include psoriasis and hyperkeratosis, which do not respond to other means and methods, can significantly improve the skin condition( more than half of patients receiving Neotigazone as a mono drug).

In the course of the study, the main therapeutic effects were established:

• growth regulation, correct differentiation( functional isolation) of skin cells;
• normalization of the keratinization process of the epidermis and keratolytic action aimed at softening and removing excess horny layers( exfoliation);
• suppression of abnormal overgrowth of the epidermis( proliferation) on the background of inflammation due to the activation of enzymes;
• regulation of regenerative mechanisms( recovery, healing);
• elimination of inflammation and strengthening of local protective functions( immunostimulating effect).

After taking the medicine inside, the time interval in which the amount of the active substance in the blood plasma becomes the maximum( TC max) is 1 to 4 hours.

Bioavailability, that is, the ability of a drug to be absorbed in the body( which determines the speed of onset and the severity of the therapeutic effect), becomes optimal if the capsules are taken with food( preferably - with milk).An approximate indicator of the bioavailability of a single dose in 35 to 95 patients out of a hundred is 60%, which is related to the specific features of the individual patient's body. With proteins, the plasma fraction of blood binds almost completely( more than 99%).

Pharmacokinetics

The specificity of acitretin is expressed in a high degree of lipophilicity - the ability to dissolve in fats, which allows easy penetration into tissues. However, this ability allows the active compound to rapidly cross the placenta, penetrating into the fetal bloodstream, and enter into the female milk.

The time interval for which the content of acitretin is reduced by 50%( T 1/2 or half-life) is approximately 50 hours, and T ½ of the main metabolite( intermediate of chemical transformations in the liver) - cis-acitretin - about 60 hours.

At the end of a long treatment, acitretin and its metabolite is excreted in 36 days by the liver( along with bile) and kidneys.

Indications

The doctor may prescribe the use of Neotigazone Capsules to relieve symptoms in cases of severe and often recurring dermatological pathologies with characteristic deviations in the epidermal keratinization process that do not respond positively to other pharmaceuticals and physiotherapy.

These pathologies include:

• psoriasis, and in the pustular form, limited to individual areas, and when the abnormal process spreads to the entire skin;
• erythroderma is ichthyosiform and psoriatic;
• severe hyperkeratosis, including congenital ichthyosis, Darya disease( genetic follicular dyskeratosis), lichen planus, and other pathologies with severe keratinization disorder, especially in cases of their immunity to traditional treatment tactics.

Instructions for use

General principles of treatment:

1. Medication is allowed for use only in the absence of a positive therapeutic benefit in other therapies.
2. Dosages for each patient and duration of treatment are determined only by a specialist, taking into account the rate of absorption of acitretin, the metabolism, the age, sex and the severity of the symptoms in each particular patient.
3. During the course of the Neotigazone, the patient is recommended to carefully evaluate all changes in the general condition and skin manifestations, in a timely manner informing the doctor about any deviations - local and general.
4. For better absorption, capsules should be taken orally with food or with milk.
5. The dosages of the drug are lower, the more pronounced the inflammatory reaction on the skin.

Adult

Monotherapy

• To provide the initial treatment effect for psoriasis, the daily daily dose: 1 capsule 25 mg or 3 capsules of 10 mg( total 30 mg) for 14 to 30 days.
• The dose for maintaining the result obtained for 2 to 4 weeks of treatment is determined taking into account the tolerability of the medication and its effectiveness for a particular patient. Standard daily dosages for adults vary from 25 to 50 mg. The optimal course is 6 to 8 weeks.
• In severe cases, a dose increase of up to 75 mg per day is allowed.
• When the noticeable improvement in pathological skin manifestations is achieved, the treatment is stopped. If a relapse occurs( exacerbation), the therapy is repeated according to the indicated scheme.
• In hyperkeratoses, it is recommended to reduce the daily dose to the lowest possible value, at which the therapeutic effect is manifested, up to - 20 mg or even less.

Combined treatment of

The doctors consider the most optimal solution for psoriasis and expressed hyperkeratosis not with Neotigazone monotherapy, but with its combination with other medicines. Among them there may be traditionally prescribed external ointments, creams, and pharmaceuticals for internal use, permitted for concurrent use with acitretin.

The following reasons serve as the basis for this recommendation:

1. First, after acitretin is discontinued, a second exacerbation can quickly develop. Therefore, to prevent recurrence, Neotigazone is combined with glucocorticosteroids, vitamin D preparations for application to the skin, physiotherapy and traditional ointments.
2. Secondly, in the case of combination therapy, the doctor can reduce the dose of Neotigazone, taking into account the individual reaction to the drug.

For infants and children

In the treatment of children and newborns, acitretin may be used in exceptional cases of extremely severe psoriasis and other dermatological pathologies, only if other methods are completely ineffective.

Features:

1. Particular caution is required because of the high probability of serious adverse reactions that occur during prolonged treatment, including ossification of the interosseous ligaments, impaired renal, hepatic and epiphyseal function that can slow the child's growth.
2. The younger the patient, the faster the emergence and sharper occurrence of side effects.
3. Given these features, when assigning Neotigazone to children, especially a long course, it is required to accurately measure the degree of possible risks with a possible curative result.
4. Before treatment and already in the process of therapy, once every 14 days, according to laboratory tests, liver and kidney function are evaluated, blood is examined for lipid levels. In infants and children under 10 years, in addition, periodically measure growth.

Dosage:

• The daily dose for a child is determined in strict accordance with the patient's body weight.
• The norm per kilogram of weight per day is: 0.5 mg per kilogram of the baby's weight( with the bullous form of ichthyosiform erythroderma).

In rare cases, a short course( no longer than 4 weeks) is allowed to increase the dose per day to 1 mg per 1 kg. Further, the daily dosage is reduced weekly by 0.15-0.25 mg per kilogram.

• with a non-bullous form of erythroderma - 0.75 mg per kilogram;
• with plate ichthyosis - 1 mg / kg.

The maximum total daily dose in a child of any age can not exceed 35 mg.

• In the long course, to maintain the improvement achieved in a minor patient, the physician must calculate the minimum possible dose sufficient for the therapeutic outcome.
• Newborn babies and infants Neotigazone is prescribed exceptionally rarely and only after a detailed examination of the pediatrician and specialists.
• Norm for newborns: 0.8 mg per kilogram of the baby's weight( 7 days), then the dose is reduced to 0.4 mg / kg.
• After improvement for a period of up to 30 - 90 days pass to a dose of 0.2 mg / kg and gradually withdraw capsules. With a bullous form of erythroderma, the dose is reduced 2-fold.

In pregnancy and lactation

Acitretin, like all retinoids, provokes the development of congenital malformations( teratogenicity) in the embryo and fetus, no matter what the minimum dosage is used, and with the shortest course of use. For this reason, the drug is prohibited and at the stage of bearing the baby, and for 2 years after the end of therapy.

In addition, all patients who are capable of childbearing( from the first menstruation to the menopause period), the use of acitretin is also highly undesirable, since in case of accidental conception the risk of intrauterine pathologies in an infant is extremely high.

For the possibility of assigning Neotigazone to a patient of childbearing age, strict compliance with all the conditions without exception is required:

1. A serious dermatological disease with keratinization disorder( keratinization) is diagnosed, not responding to other medications and methods of therapy.
2. The patient confirms that she will follow all the doctor's instructions, agrees to the required precautions, is warned of the high threat of defects in the fetus and serious consequences if the conception occurs during treatment or after it is completed within 24 months.
3. An absolutely intimate act is practiced with the constant use of reliable contraceptives for 30 days before the appointment of Neotigazone, then for the full course of therapy and the next 24 months after the last capsule is taken. It is desirable to combine the use of combined contraceptive pills and the mechanical method of contraception in parallel( condoms, cervical caps, diaphragms).
4. It is not allowed to use oral contraceptives with a low dosage of only one active ingredient - progesterone( so-called "minipilli"), because they are distinguished by a weak contraceptive effect.
5. The first capsule of the medicine is taken not earlier than the period 2 - 3 of the menstrual cycle, which takes place during the reception of birth control pills.
6. A reliable pregnancy test is required, which should be done 1 to 6 days before the first Neotigazone capsule is received, with confirmation of a negative result( lack of conception).
7. Testing for probable pregnancy is done once a month during the course of treatment, and after its completion - once in 1 - 2 months for up to 24 months.
8. It is forbidden to drink alcoholic beverages and pharmaceuticals with ethanol all the time taking acitretin and another 60 days after the end of treatment.
9. In case of an exacerbation, the repeated course of therapy completely fulfills all the above requirements.

If a woman is breastfeeding a baby, Neotigazone is prohibited.

Contraindications

Medication is contraindicated in the following diseases and conditions:

• pregnancy;
• is a particular hypersensitivity to acitretin, excipients, and other types of retinoids;
• conception planning in the next 24 months;
• any period with the probability of accidental conception;
• Breastfeeding a baby;
• severe kidney and liver pathology;
• chronically elevated blood lipid levels( fats, including cholesterol and triglycerides);
• reception of vitamin A, any retinoids to avoid hypervitaminosis A, as well as Methotrexatom and antibiotics of the tetracycline group.

Relative contraindications:

• the age of fertility( fertility), from the menarche( first month cycle) in young girls to postmenopause, excluding the period of continuous use of reliable combined contraceptives;
• , hepatitis, diabetes, atherosclerosis, pancreatitis, where standard dosages of 1 mg / kg per day can cause complications;
• drinking alcohol to avoid serious liver strain.

Side effects of

General

Different degrees of side effects of unwanted reactions, mainly due to an excess of vitamin A, are observed in most patients. Usually, acitretin-associated adverse reactions decrease significantly with a decrease in dose and completely disappear after discontinuation of therapy, that is, they are temporary and reversible. In isolated cases, at the beginning of the reception of the remedy, the symptoms of the underlying disease increased.

Depending on the dose and duration of taking Neotigazone, the following unpleasant effects can occur:

• inflammation and dry lips and red border( cheilitis), seizures in the corners of the mouth;
• congestion of the sinuses of the nose, mucous and bloody discharge from the nose;
• dryness and irritation of the mucosa and conjunctiva of the eyes, ulceration of the cornea( rarely)
• soreness with contact lens wear, twilight vision disorder( "blindness")
• dryness of the mouth, thirst;
• inflammation of the gingival tissue, development of stomatitis, a disorder of taste sensations;
• more frequent development of candidiasis vulvaginitis( thrush);
• skin peeling( usually on the palms, feet) sometimes - all over the body;
• signs of dermatitis, eczema, itchy skin;
• hair loss, deterioration of their structure,
• layering of nails, inflammation of the tissue on the fingers near the nail plates;
• is rarely a rash with bullous manifestations( with blisters, wet areas);
• photosensitization( sensitivity to ultraviolet);
• tenderness of muscles, joints, bones;
• upset stomach and bowel function;
• an increase in existing and the formation of new foci of calcification of tissues, ligaments and tendons, the development of osteoporosis of the spine and abnormal growth of bone tissue;
• increased muscle tension, convulsive manifestations;
• hot flushes to the upper half of the body, local swelling;
• increase in cholesterol, liver enzymes, triglycerides, rarely - hepatitis, jaundice;
• single cases of headaches, increased intracranial pressure, nausea, vomiting, polyneuropathy( numbness of the skin, muscle weakness, hypersensitivity, soreness).

Overdose of

• If neotigazone is taken in unreasonably high doses, an acute overdose of acitretin may occur, in which the symptoms characteristic of acute vitamin A poisoning are unavoidable, including vomiting, dizziness, and intense headaches.
• The medication is immediately stopped, but given the rather low degree of toxicity of the drug, there is no need for specific treatment.

Special instructions for

Special recommendations should be considered when taking Neotigazone:

1. The administration of the medication, determination of dosages and duration of administration is the exclusive prerogative of the attending physician, clearly representative of the effects of the drug, including its increased teratogenic properties.
2. If acitretin is combined with other medicines and treatments, dosage adjustment is required to decrease.
3. All patients who receive Neotigazone, and also within 24 months after discontinuation, are not eligible to be blood donors, especially if blood transfusion can be prescribed to a woman of childbearing age( from age 12);
4. Analyzes for assessing liver function are performed before taking Neotigazone, then every 7 days for the first 60 days from the start of the procedure, and later every three months. At any deviations from the norm, laboratory tests are done every 7 to 12 days. If liver function tests do not come back to normal, and even more so if the tests worsen, the medication is stopped, but the liver condition is monitored for at least another 3 months.
5. During a long course, it is necessary to regularly monitor the cholesterol, blood sugar, triglycerides, and possible osteoporosis disorders, when they are asked whether to stop or continue treatment with an analysis of the risk of progression of such anomalies.
6. For prolonged therapy with acitretin, children need special monitoring of any abnormalities in bone development and growth rates of the child.
7. The eyesight should be checked regularly. If signs of "night blindness" appear, the patient needs to be extremely careful when being active in poorly lit places and driving at night and at dusk.

Currently, the long-term effects of taking drugs with acitretin have not yet been studied.

Interaction with other drugs and alcohol

• The use of alcoholic beverages and drugs with ethanol together with Neotigazone causes the formation of an intermediate substance of erythinate, which is characterized by a very long half-life( 120 days) and comparable to acitretin, a teratogenic effect on the fetus.
• Already after the termination of therapy the refusal of alcohol is obligatory within 2 months.
• Joint administration of the drug with vitamin A, any retinoid leads to severe intoxication due to hypervitaminosis.
• Parallel use with phenytoin reduces the binding of acitretin to proteins.

Reviews

Analysis of reviews of Neotigazone shows that the therapeutic effect of the drug is more pronounced and longer, the less profound are the pathological changes on the skin.

• Practical all patients note the significant effect of the drug on the severe external manifestations of psoriasis, which subsided or completely disappeared for a period of 2 to 3 to 18 to 24 months.
• In the treatment of exacerbations, the time of remission was reduced.
• In reviews, there are rarely complaints of severe adverse symptoms. The main unpleasant manifestations are associated with dry lips and peeling of the skin on the soles and palms.
• Separately emphasize the absolute negative effect of the drug on the fetus, because of which most women do not use the Neotigazone
• Doctors say that Neotigazone is able to relieve severe symptoms, but does not cure the internal cause of the skin disease. However, the medicine, with proper use under medical supervision, undoubtedly deserves attention as a means leading to a significant reduction in pathological phenomena on the skin, which is noted by almost every patient.

Analogues of

There are no complete analogues of Neotigazone in the pharmacy network, but the following medicinal products are referred to as drugs: Oxoralen, Psoberan, Ammifurin, Beroxan, Psoralen.