Neotigason capsules 10 mg 30 pcs
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Active ingredients
Atsitretin
The brand
Neotigason
Composition
1 caps Acitretin (as a dry spray containing 25% of the active substance) 10 mg. Excipients: microcrystalline cellulose - 50 mg; in the composition of the dry spray (per 1 g): acitretin - 250 mg, gelatin - 270 mg, maltodextrin - 410 mg, sodium ascorbate - 70 mg.
Pharmacological effect
Systemic retinoid. Atsitretin, the active ingredient of the drug Neotigason, is a synthetic aromatic analogue of retinoic acid. In preclinical studies on the tolerability of acitretin, no mutagenic or carcinogenic effect was found; there was also no indication of its direct hepatotoxicity. Atsitretin had a pronounced teratogenic effect on animals. Clinical studies have confirmed that with psoriasis and keratinization disorders, acitretin normalizes the processes of proliferation, differentiation, and keratinization of epidermal cells, and its side effects are, in general, quite tolerable. The action of the drug is purely symptomatic; its mechanism remains largely unknown.
Pharmacokinetics
Absorption: Cmax of atsitretin in plasma is observed in 1-4 h after reception. The best bioavailability of atsitretin is achieved when taking the drug during a meal. The bioavailability of a single dose is about 60%, but it is subject to significant individual fluctuations (36-95%). Distribution: Atsitretin has a pronounced lipophilicity and easily penetrates the tissue. Its binding to proteins exceeds 99%. In animal studies, acitretin passed through the placental barrier in quantities capable of causing fetal malformations. Lipophilic properties of atsitretin force to assume that it in significant quantities gets to breast milk. Metabolism: Acitretin is metabolized by isomerization to the 13-cis isomer (cis-acitretin), as well as by the formation of glucuronides and cleavage of the side chain. Withdrawal: Studies with repeated intake of the drug by patients aged 21 to 70 years have shown that T1 / 2 acitretin is about 50 hours, and its main metabolite in plasma, cis-acitretin, which is also teratogenic, is 60 hours. Given the longest duration T1 / 2 acitretin (96 h) and cis-acitretin (123 h) in these patients, as well as on the basis of their linear kinetics, it can be predicted that more than 99% of the drug will be eliminated from the body within 36 days after the cessation of long-term treatment.Moreover, within 36 days after cessation of treatment, the concentrations of acitretin and cis-acitretin in plasma decreased below the sensitivity limit of the method (less than 6 ng / ml). Atsitretin is excreted exclusively in the form of metabolites, in approximately equal amounts through the kidneys and biliary tract.
Indications
- severe forms of psoriasis, including psoriatic erythroderma, localized or generalized pustular psoriasis - severe dyskeratosis, such as congenital ichthyosis of red hair of Darya, other severe violations of keratinization, resistant to traditional therapies.
Contraindications
- severe hepatic and renal failure - severe chronic hyperlipidemia - pregnancy. Neotigason has a strong teratogenic effect and should not be given to pregnant women. The same applies to all women capable of childbearing, unless they use reliable contraceptives 4 weeks before the start of treatment, during treatment and for two years after its completion - hypersensitivity to the drug (acitretin or excipients) or other retinoids.
Use during pregnancy and lactation
Pregnancy Neotigason high teratogenen. It is contraindicated not only to pregnant women who may become pregnant during treatment or within 2 years after its termination, but also to all women potentially capable of having children. The risk of having a child with developmental defects is especially high if Neotigason is taken before or during pregnancy, regardless of the dose and duration of therapy. The effect of Neotigason on the fetus is always associated with the risk of congenital malformations. Neotigazonone is contraindicated in any woman who is capable of childbearing, unless each of the following conditions is met: 1. The patient suffers from severe keratinization resistant to standard treatments. 2. You can be sure that the patient understands and follows the instructions of the doctor. 3. The patient is able to apply the prescribed contraceptives carefully and continuously. 4. It is absolutely necessary that every woman capable of childbirth use effective contraceptives without interruption for 4 weeks before the start of treatment, during the treatment process and for two years after the completion of the treatment with Neotigason. 5. Treatment should not begin before the 2nd or 3rd day of the next normal menstrual cycle. 6. Two weeks before the start of treatment, a negative pregnancy test should be obtained.During treatment, it is recommended to conduct additional tests for pregnancy at least 1 time / month. 7. Before starting treatment with Neotigason, the doctor should give detailed information, verbally and in writing, to women capable of childbearing about the necessary precautions, the danger of very severe fetal malformations and the possible consequences of pregnancy during Neotygazone treatment or within 2 years after it ends. 8. The same effective and continuous contraceptive measures should be applied each time a course of treatment is repeated, regardless of its duration, and be respected for two years after the end of the course. 9. If, despite all precautions, during the treatment with Neotigason or within 2 years after its termination, pregnancy occurs, there is a great risk of severe fetal malformations (for example, a hernia of the brain). Breastfeeding Neotigason should not be prescribed to nursing mothers.
Dosage and administration
Due to individual differences in absorption and the rate of metabolism of acitretin, the dose must be selected individually. Capsules are best taken once a day with food or with milk. The following are indicative recommendations. Adults Initial daily dose: 25 mg (ie, 1 capsule 25 mg each) or 30 mg / day (3 capsules 10 mg each) for 2-4 weeks. Maintenance dose depends on the clinical efficacy and tolerability of the drug. As a rule, the optimal therapeutic effect is achieved with a daily dose of 30 mg taken as early as 6-8 weeks. In some cases, it is necessary to increase the dose to a maximum equal to 75 mg / day (i.e., 3 capsules, 25 mg each). After sufficient regression of psoriatic lesions, treatment of patients with psoriasis can be stopped. Relapse is treated as above. With dyskeratosis, maintenance therapy is usually required, which is carried out in as small doses as possible. They can be below 20 mg / day and should not exceed 50 mg / day. Children Given the possibility of severe side effects, long-term treatment should carefully compare the possible risk with the expected therapeutic effect. Atsitretin should be prescribed only if all other methods of treatment fail. The daily dose depends on body weight and is about 0.5 mg / kg.In some cases, for a limited time, higher doses may be required, up to I mg / kg / day (no more than 35 mg / day). The maintenance dose should be as low as possible, taking into account possible adverse reactions with long-term treatment. Combination therapy If Neotigason is used in combination with other types of treatment, it is possible to reduce its dose, depending on the individual patient's response. When treating with Neotigas, the usual topical treatment can be continued; it does not affect the action of Neotigason.
Side effects
Adverse reactions occur in most patients taking Neotigason. However, they usually disappear after dose reduction or drug withdrawal. Sometimes at the beginning of treatment there is an aggravation of the symptoms of the disease. The most frequent side effects are symptoms of hypervitaminosis A, for example, dry lips, which can be eliminated by using a rich cream; cheilitis and fissures in the corners of the mouth, dryness and inflammation of the mucous membranes and transitional epithelium; sometimes nasal bleeding, rhinitis and ophthalmic disorders (xerophthalmia, conjunctivitis), as well as intolerance to contact lenses; rarely - corneal ulcers. There were also cases of thirst and dry mouth, sometimes stomatitis, gingivitis and a violation of taste, an increase in the frequency of vulvovaginitis caused by Candida albicans. Thinning and flaking of the skin can occur throughout the body, especially on the palms and soles. Described frequent cases of "stickiness" of the skin, dermatitis, eczema and itching, hair loss, brittle nails and paronychia. There are separate reports of the occurrence of bullous eruptions and changes in the structure of the hair; photosensitivity reactions rarely develop. After the withdrawal of Neotigazona, these side effects are usually reversible. There are separate reports of headaches, although an increase in intracranial pressure is rarely observed. If severe headaches, nausea, vomiting and visual disturbances occur, Neotigason should be canceled immediately and the patient should be referred to a neurologist. Sometimes there was a violation of dark adaptation. Muscle, bone and joint pain may occur. Maintenance therapy can lead to an increase in the already existing hyperostosis of the spine, the emergence of new hyperostosis and soft tissue calcification, as is the case with long-term systemic use of other retinoids.Cases of the appearance of peripheral edema and hot flashes are described, gastrointestinal disorders, hepatitis, jaundice, and a temporary and, as a rule, reversible increase in the activity of aminotransferases and alkaline phosphatase rarely develop. When treating with large doses of Neotigason, a reversible increase in serum triglycerides and serum cholesterol occurred, especially in high-risk patients (with lipid metabolism disorders, diabetes, obesity, and alcoholism). If these disorders persist, an increased risk of atherogenesis cannot be ruled out.
Overdose
In the event of an acute overdose, Neotigason should be discontinued immediately. No other special measures are required, since the acute toxicity of the drug is low. Overdose symptoms are identical to those in acute hypervitaminosis A (headache, dizziness).
Interaction with other drugs
Because of the risk of hypervitaminosis A, the simultaneous use of vitamin A and other retinoids should be avoided. Since both Neotigason and tetracyclines can cause an increase in intracranial pressure, their simultaneous use is contraindicated. There are reports of an increased risk of developing hepatitis with the combined use of methotrexate and Tigason (etretinate), therefore, the use of methotrexate at the same time as Neotigason is also contraindicated. Neotigazone does not affect the binding of coumarin (warfarin) anticoagulants to proteins. If Neotygazone administered simultaneously with phenytoin, it should be noted that Neotigason partially reduces the degree of binding of phenytoin to proteins. Atsitretin can reduce the contraceptive effect of micropiles with progesterone. Therefore, you should not use micropiles with progesterone for contraception. No other interactions between Neotigazone and other drugs (for example, digoxin, cimetidine, estrogen / progestogen combined oral contraceptives) have been found to date. In a study in healthy volunteers, a single dose of acitretin together with ethyl alcohol led to the formation of etretinate (this was previously detected in vitro). In recent studies, the formation of etretinate was also detected in some patients taking Neotigason.Until this phenomenon is fully explained, it is necessary to take into account the pharmacokinetic features of etretinate: since its half-life is approximately 120 days, it is necessary to use contraceptives for two years after the completion of treatment.
special instructions
Neotigason can be prescribed only by doctors who have experience with systemic retinoids and who understand the risk of the teratogenic effect of acitretin. Women of childbearing age should not drink alcohol during treatment with Neotygazone, since there is clinical evidence that, while taking acitretin and alcohol, etretinate can form in the body. The mechanism of this metabolic transformation is not established; therefore, it is unclear whether other substances can participate in it. Reception of ethanol should be avoided for 2 months after cessation of therapy with acitretin. Women of childbearing age should not be blood transfused from patients receiving Neotigason. Consequently, during treatment with Neotigason and during the year after its completion, blood donation is prohibited. Liver function should be monitored prior to the start of Neotigazoi treatment, every 1-2 weeks during the first month after the start of treatment, and then every 3 months. If test results indicate pathology, monitoring should be carried out weekly. If liver function does not return to normal or deteriorates further, Neotigason should be canceled. In this case, it is recommended to continue to monitor liver function for at least 3 more months. It is necessary to control the level of fasting serum cholesterol and triglycerides, especially in patients at risk (lipid metabolism disorders, diabetes, obesity, alcoholism) and with long-term treatment. In patients with diabetes mellitus, retinoids can improve or worsen glucose tolerance, therefore, in the early stages of treatment, the concentration of glucose in the blood should be checked more often than usual. Adults receiving long-term therapy with Neotigazone should regularly conduct appropriate examinations, taking into account the possibility of anomalies of ossification (see "Side Effects"). In the event of such violations should be discussed with the patient the question of continuing treatment, carefully matching the possible risks and benefits of the drug. In children, you need to carefully monitor the parameters of growth and bone development.Because of the possibility of impaired night vision, patients should be warned about the need for caution when driving a car or working with machines and mechanisms at night. Care should be taken to monitor visual impairment. At present, not all the effects of Neotygazone that may occur throughout life are known.