Verocutane
Verocutane: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Verocutan
ATX code: D10BA01
Active ingredient: isotretinoin (Isotretinoin)
Manufacturer: Veropharm, JSC (Russia)
Description and photo updated: 2018-29-11
Prices in pharmacies: from 891 rubles.
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Verocutane is a remedy for acne.
Release form and composition
The drug is produced in the form of capsules: gelatinous soft, oblong shape with a longitudinal seam, brown-red (10 mg) or with one half brown-red and the other - white with a yellow tint (20 mg); the contents of the capsules are a homogeneous oily suspension from dark yellow to yellow color (10 pieces in a blister strip packaging, 3 or 10 packs in a cardboard box; 30 pieces in a polymer bottle with a polymer cap with a first opening control with an insert of silica gel, 1 bottle in a cardboard box; each box also contains instructions for the use of Verocutan).
1 capsule contains:
- active substance: isotretinoin - 10 or 20 mg;
- additional components: refined soybean oil, beeswax, hydrogenated soybean oil, disodium edetate (Trilon B), butylhydroxyanisole;
- capsule shell: glycerol, medical gelatin, titanium dioxide, propyl parahydroxybenzoate, methyl parahydroxybenzoate, iron dye red oxide.
Pharmacological properties
Pharmacodynamics
Verocutane is a retinoid used for the systemic treatment of acne. Isotretinoin - the active substance of the drug is a stereoisomer of all-trans retinoic acid (tretinoin). Currently, the exact mechanism of action of the drug is not fully determined, but it has been established that the improvement in the clinical picture of severe forms of acne caused by it is due to the inhibition of the activity of the sebaceous glands and a decrease in their size, histologically confirmed. In addition, the anti-inflammatory effect of isotretinoin on the skin has been found.
Thanks to the action of Verocutane, the terminal differentiation of keratinocytes is normalized, the hyperproliferation of the stratified epithelium lining the excretory ducts of the sebaceous glands is inhibited, the formation of detritus is inhibited and its evacuation is facilitated. As a result, the production of sebum decreases, its composition is normalized and secretion is facilitated, the inflammatory reaction around the glands decreases. With systemic use, Verocutane demonstrates anti-inflammatory, sebostatic, antiseborrheic, kerato- and immunomodulatory effects, as well as enhances the regeneration processes in the skin.
Pharmacokinetics
Due to the fact that the kinetics of isotretinoin and its metabolites is linear, its plasma concentrations during therapy can be predicted based on data obtained after a single dose. This feature of the drug also indicates that it does not affect the activity of hepatic enzymes involved in the metabolism of drugs.
Absorption from the gastrointestinal tract (GIT) is variable. The absolute bioavailability and volume of distribution of isotretinoin in humans have not been determined, since there is no form of release for intravenous (IV) administration. It can be assumed, according to preclinical studies, that the bioavailability of the drug is low and variable. If isotretinoin is used with food, its bioavailability doubles when compared to fasting. After oral administration of Verocutane at a dose of 80 mg, the period of reaching the maximum concentration (T Cmax) of isotretinoin is 2–4 hours, and the maximum concentration (C max) is 310 ng / ml (188–473 ng / ml). The plasma level is 1.7 times higher than in the blood, as a result of the low degree of penetration of the active substance into red blood cells.
The agent almost completely (99.9%) binds to plasma proteins (mainly albumin), as a result of which, in a wide range of therapeutic concentrations, the proportion of the free (pharmacologically active) fraction of the drug is less than 0.1% of its total amount. After oral administration of isotretinoin at a dose of 40 mg 2 times a day, its equilibrium concentration (C ss) is 120-200 ng / ml, C ss of the main metabolite (4-oxo-isotretinoin) is 2.5 times higher than that of the active substance. The level of isotretinoin in the epidermis is 2 times lower than in serum. There is insufficient information on the penetration of the drug into human tissues.
The metabolic transformation of the drug proceeds with the formation of the following three main biologically active metabolites: 4-oxo-isotretinoin (the main metabolite), tretinoin (completely trans-retinoic acid), 4-oxo-retinoin. Also, as a result of biotransformation of isotretinoin, less significant metabolites, including glucuronides, arise, but the structure of all metabolic products is not determined.
Plasma levels of 4-oxo-isotretinoin at steady state are 2.5 times higher than those of the parent drug. Due to the fact that in vivo isotretinoin and tretinoin are reversibly converted into each other, the biotransformation of tretinoin is associated with the metabolism of isotretinoin. By isomerization, 20-30% of the dose of the active ingredient Verocutane is metabolized. In the pharmacokinetics of an active substance in humans, enterohepatic circulation is of particular importance. The main role in the metabolism of isotretinoin is assigned to isoenzymes of the CYP system.
In urine and feces after oral administration of radioactively labeled isotretinoin, approximately equal amounts of this substance are detected. In patients with acne, the terminal phase half-life (T ½) for unchanged drug is approximately 19 hours. For 4-oxo-isotretinoin, the T ½ of the terminal phase is probably greater and averages 29 hours.
Isotretinoin is a natural (physiological) retinoid. After completion of therapy, endogenous concentrations of retinoids are restored on average after 2 weeks.
Renal failure does not affect the pharmacokinetic parameters of isotretinoin.
Indications for use
Verocutane is recommended for the treatment of severe acne, such as acne conglobata, nodular-cystic acne, or acne at risk of scarring that does not respond to other therapies.
Contraindications
Absolute:
- hypervitaminosis A;
- liver failure;
- simultaneous treatment with tetracyclines;
- severe hyperlipidemia;
- established / planned pregnancy;
- lactation period;
- age up to 12 years;
- hypersensitivity to any component of the drug.
Verocutane should be used with caution in such diseases / conditions as lipid metabolism disorders, obesity, diabetes mellitus, a history of depression, alcoholism.
Verocutane, instructions for use: method and dosage
Verocutane capsules are taken orally with food, 1 or 2 times a day.
The therapeutic effect of isotretinoin and its adverse reactions are dose-dependent and vary from patient to patient. As a result, an individual dose selection is required during treatment.
The initial daily recommended dose is 0.5 mg / kg, in most patients the dose may be 0.5–1 mg / kg. In severe lesions or in the presence of trunk acne, a daily dose of up to 2 mg / kg may be prescribed.
The optimal course dose is 120-150 mg / kg, the duration of administration is individual for each patient and varies depending on the daily dose. Often, complete remission of acne can be achieved within 16-24 weeks of therapy. If the patient tolerates the recommended dose very poorly, Verocutane can be continued at a lower dose, but the treatment will take longer.
Acne completely disappears in most patients after a single course of therapy. With a pronounced relapse, a repeated course of treatment is prescribed in the same daily and course doses as during the first. Since after the cancellation of Verocutane, the condition can improve for 8 weeks, a second course should be prescribed only after this period.
In patients with severe chronic renal failure (CRF), the initial daily dose of Verocutane needs to be reduced to 10 mg with a further increase, but not more than the maximum allowable daily dose of 1 mg / kg. It is recommended to round the daily dose down to the next lower number of whole capsules.
Side effects
Most of the unwanted effects of isotretinoin are dose dependent. Violations caused by the drug are reversible and disappear after changing the dose or discontinuing therapy, but some may also occur after discontinuation of Verocutane.
Possible side reactions:
- symptoms caused by hypervitaminosis A: dry skin / mucous membranes, including nasal cavity (bleeding), lips (cheilitis), pharynx, larynx (hoarseness), eyes (contact lens intolerance, reversible corneal opacity, conjunctivitis);
- skin and subcutaneous fat: sweating, itching, rash, reversible hair loss, persistent thinning of hair, hyperpigmentation, photoallergy, photosensitization, facial erythema / dermatitis, paronychia, pyogenic granuloma, onychodystrophy, increased growth of granulation tissue, acupuncture forms, hirsutism peeling of the skin of the palms and soles, slight trauma to the skin; at the beginning of the course for several weeks, an exacerbation of acne is possible, which passes without changing the dose of Verocutane;
- nervous system: headache, behavioral disorder, dizziness, sleep disturbance, drowsiness, lethargy, nervousness, anxiety, paresthesia, convulsions, syncope, excessive fatigue, weakness, increased intracranial pressure (pseudotumor of the brain: nausea, vomiting, headache, visual edema nerve, visual impairment);
- sensory organs: eye irritation, photophobia, decreased acuity of twilight vision, impaired color perception (disappears after discontinuation of therapy), impaired visual acuity, xerophthalmia, conjunctivitis, blepharitis, keratitis, optic edema (as a symptom of intracranial hypertension), lenticular cataract, hearing impairment certain sound frequencies;
- mental disorders: emotional lability, aggression, depression, psychosis, suicidal thoughts / attempts, suicide;
- digestive system: dryness of the oral mucosa, diarrhea, nausea, inflammation of the gums, bleeding from the gums, colitis, ileitis, esophagitis, bleeding, esophageal ulcers; pancreatitis, especially with concomitant hypertriglyceridemia above 800 mg / dl, including with a fatal outcome (with the development of symptoms of pancreatitis or with persistent hypertriglyceridemia, Verocutane should be abandoned); an increase in the activity of hepatic transaminases is transient and reversible (in most cases, it does not go beyond the normal range and returns to the initial indicators during treatment), hepatitis;
- musculoskeletal system: muscle / joint pain, arthritis, hyperostosis, calcification of ligaments and tendons, other bone changes, including a decrease in bone density, tendinitis, premature closure of the epiphyseal growth zones (with a total course dose and duration of treatment exceeding the recommended ones);
- respiratory organs: bronchospasm, mainly with a history of bronchial asthma;
- reproductive system: menstrual irregularities;
- hematopoietic organs, blood system: a decrease in the number of neutrophils, leukocytes, anemia, an increase / decrease in the number of platelets, a decrease in hematocrit, an acceleration of the erythrocyte sedimentation rate (ESR);
- immune system: local / systemic infections caused by gram-positive pathogens (Staphylococcus aureus);
- others: back pain, hematuria, lymphadenopathy, proteinuria, glomerulonephritis, vasculitis (allergic vasculitis, Wegener's granulomatosis), systemic hypersensitivity reactions;
- laboratory parameters: an increase in the level of triglycerides (TG), uric acid, cholesterol, hyperglycemia, a decrease in the plasma level of high density lipoproteins (HDL) in the blood, cases of newly diagnosed diabetes mellitus; increased activity of creatine phosphokinase, mainly with intense physical activity.
Against the background of treatment with isotretinoin in the process of post-marketing observation, cases of severe skin reactions in the form of toxic epidermal necrolysis, Stevens-Johnson syndrome, and exudative erythema multiforme were recorded. These serious complications can lead to disability, hospitalization, life-threatening conditions, or death. Careful observation of patients is necessary for the timely detection of severe skin reactions and a decision on the withdrawal of Verocutane.
Overdose
Symptoms of an overdose of Verocutane may be signs of hypervitaminosis A - drowsiness, dizziness, headache, irritability, nausea, vomiting. For the first few hours after an overdose, gastric lavage may be required. In most cases, these disorders are reversible and do not require treatment.
special instructions
Verocutane can only be prescribed by doctors (preferably dermatologists) who have experience with the use of systemic retinoids and who are aware of the risk of teratogenicity of the drug.
The drug should not be used for the treatment of mild to moderate acne vulgaris. During the period of therapy and within 30 days after its completion, it is necessary to completely exclude blood sampling from potential donors in order to avoid the risk of getting this blood into pregnant women due to the high probability of developing teratogenic and embryotoxic effects.
When prescribing Verocutane, it is recommended to monitor the activity of hepatic transaminases, as well as serum lipid concentration before the start of the course, 1 month after its start, and then every 3 months or according to indications. If the activity of liver enzymes exceeds the norm, you need to reduce the dose of the drug or stop taking it. Lipid levels also usually return to normal after dose reduction or discontinuation of treatment.
More frequent monitoring of glucose concentration should be carried out with existing diabetes mellitus or suspicion of it.
In patients taking isotretinoin, rare cases of depression, psychotic symptoms, and extremely rare suicidal attempts were recorded. The causal relationship of their development with the use of Verocutane has not been determined, however, special care must be taken when taking the drug in patients with a history of depression. During treatment with the drug, it is required to observe all patients for the development of depression and, if necessary, refer them to the appropriate specialist.
When receiving isotretinoin, it is recommended to use moisturizing ointments or body creams and lip balm in order to reduce dry skin and mucous membranes at the beginning of the course.
It is necessary to avoid laser treatment and the implementation of deep chemical dermabrasion while taking Verocutane, as well as for 5-6 months after its termination due to the risk of increased scarring in atypical places and the development of hyper- and hypopigmentation. In the course of treatment and for six months after it, it is impossible to perform epilation using wax applications due to the aggravation of the risk of epidermal detachment, scarring and dermatitis.
In case of dryness of the mucous membrane of the eyes while taking Verocutan, it is recommended to use the application of an artificial tear preparation or a moisturizing eye ointment. Patients with dry conjunctiva need to be monitored for possible keratitis. If you develop intolerance to contact lenses during the course, you should use glasses.
It is required to limit exposure to sunlight and ultraviolet (UV) rays, and, if necessary, apply a sunscreen with a protective factor value of at least 15 SPF.
Influence on the ability to drive vehicles and complex mechanisms
While taking Verocutane, some patients may experience a decrease in the acuity of twilight vision, and therefore, care must be taken when driving vehicles and managing any other complex equipment. If a patient experiences such undesirable reactions as dizziness, headache, impaired visual acuity, drowsiness during the period of therapy, it is recommended to refuse to perform the above activities.
Application during pregnancy and lactation
Isotretinoin is a drug with a strong teratogenic effect, and therefore pregnancy is an absolute contraindication for Verocutane therapy. If pregnancy occurs during drug treatment (with any dose of isotretinoin and even with a short course), there is a high probability of having a baby with developmental defects.
The use of isotretinoin in women of childbearing age is allowed only if they have a severe form of acne that is resistant to conventional methods of treatment, and the following requirements are met: the patients understand and strictly adhere to the instructions of the attending physician; know about the danger of pregnancy during treatment with isotretinoin and within one month after its completion and about the need for urgent consultation if pregnancy is suspected; are aware of the possible ineffectiveness of contraception; confirm their understanding of the essence of precautionary measures, realizing the danger of the teratogenic effect of the drug; understand the need for continuous use of effective methods of contraception for 1 month before the course of drug treatment,during therapy and within 1 month after its completion (it is advisable to use simultaneously 2 different methods of contraception, including barrier).
The use of contraceptives during the treatment period is recommended even for those women who do not usually use contraceptive methods due to infertility (with the exception of patients after hysterectomy) and amenorrhea, as well as those who claim that they are not sexually active.
A pregnancy test with a minimum sensitivity of 25 mME / ml, according to current practice, should be carried out in the first 3 days of the menstrual cycle. The result and date of the first pregnancy test must be recorded by a specialist before the course of treatment and prior to the use of contraception to exclude a possible pregnancy. If the patient has irregular menstruation, the time of the test is set depending on sexual activity and is prescribed 3 weeks after unprotected intercourse. The patient should be informed by the doctor about the methods of contraception.
Before starting therapy, a pregnancy test is performed on the first day of using Verocutane or three days before a woman's visit to the doctor. Test results must be recorded by a specialist. Drug therapy can only be started if the patient receives effective contraception for at least one month before starting.
During treatment, you need to visit a doctor every 28 days. The need for monthly pregnancy testing is determined by local practice, taking into account sexual activity and the presence of recent menstrual irregularities (amenorrhea, lack of frequency, abnormal menstruation). With the available indications, a pregnancy test is recommended to be carried out three days before the visit to the doctor and on the day of the visit, the test results are recorded.
A final test is performed 5 weeks after the end of therapy to rule out pregnancy.
For a patient of reproductive age, a prescription for Verocutane is prescribed only for 30 days of treatment, continuation of therapy requires a new prescription of the drug by the doctor. Pregnancy testing, prescription and drug administration are recommended within one day. At the pharmacy, Verocutane should be dispensed only within 7 days from the date of the prescription.
Available data indicate that in women, exposure to the drug from the semen and seminal fluid of men taking oral isotretinoin is insufficient for the occurrence of teratogenic effects of the latter.
In the case when, despite the precautions taken, during the period of therapy or within 1 month after its completion, pregnancy nevertheless occurred, the risk of severe severe fetal malformations (for example, from the heart, large blood vessels, central nervous system) is significantly aggravated. … The threat of spontaneous miscarriages is also increasing. When pregnancy is diagnosed against the background of therapy, the drug is discontinued, the question of the advisability of maintaining the pregnancy must be resolved with the attending physician. Verocutane therapy in a pregnant woman can lead to documented severe congenital malformations of the fetus such as cerebellar malformations, microcephaly, hydrocephalus, external ear abnormalities (narrowing / absence of the external auditory canal, microtia), cardiovascular anomalies, microphthalmia,pathology of the parathyroid glands, malformations of the face (cleft palate), thymus.
During lactation, taking Verocutane is contraindicated. Isotretinoin can pass into breast milk because it is highly lipophilic.
Pediatric use
Patients under 12 years of age should not take Verocutane capsules.
With impaired renal function
In the presence of a severe form of chronic renal failure (CRF), the initial daily dose of Verocutane must be reduced to 10 mg with a further increase, but not more than the maximum permissible daily dose - 1 mg / kg. It is recommended to round the daily dose down to the next lower number of whole capsules.
For violations of liver function
In case of violations of the liver, taking Verocutane is contraindicated.
Drug interactions
- other retinoids (retinol, acitretin, tretinoin, adapalene, tazarotene): the threat of hypervitaminosis A is aggravated;
- local keratolytic drugs for the treatment of acne: may increase local irritation; it is not recommended to combine these drugs with isotretinoin;
- tetracyclines (including minocycline): the threat of increased intracranial pressure increases; combined use is contraindicated;
- progesterone preparations: their effectiveness may be weakened, and therefore contraceptives containing small doses of progesterone should not be used.
Analogs
The analogues of Verokutane are: Retasol, Aknekutan, Erase, Roaccutane, Retinoic ointment.
Terms and conditions of storage
Store out of the reach of children, protected from moisture and light, at a temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Verokutana
There are very few reviews about Verokutana. Experts point to the effectiveness of the drug in the treatment of youthful acne and acne of adults of moderate to severe degree, as well as its good tolerance. Adverse reactions from the skin and mucous membranes are recorded during therapy quite often, but they are transient, respond well to treatment with local agents with a moisturizing effect and do not require discontinuation of treatment. It is noted that the cost of a course dose of Verocutane is 1.5–2 times lower than that of its analogues. Some patients complain about the lack of the drug in pharmacies.
Price for Verocutane in pharmacies
The price of Verocutane can be: 10 mg capsules - 750-950 rubles, 20 mg capsules - 1100-1450 rubles. per package containing 30 pcs.
Verocutane: prices in online pharmacies
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Drug name Price Pharmacy |
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Verocutane 10 mg capsules 30 pcs. 891 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
