Roaccutane - Instructions For Use, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Roaccutane

Roaccutane: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Drug interactions
11. 11. Analogs
12. 12. Terms and conditions of storage
13. 13. Terms of dispensing from pharmacies
14. 14. Reviews
15. 15. Price in pharmacies

Latin name: Roaccutane

ATX code: D10BA01

Active ingredient: isotretinoin (isotretinoin)

Manufacturer: F. Hoffmann-La Roche Ltd. (Switzerland)

Description and photo update: 2019-16-08

Prices in pharmacies: from 1728 rubles.

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Roaccutane is an anti-seborrheic, anti-inflammatory drug used to treat acne.

Release form and composition

Roaccutane dosage form - capsules: oval, opaque; the contents of the capsules are a suspension of a uniform consistency from dark yellow to yellow; 10 mg each - brown-red, on the surface the inscription "ROA 10" in black ink; 20 mg each - one half brown-red, the other white, on the surface the inscription "ROA 20" in black ink (in blisters of 10 pcs., in a cardboard box of 3 or 10 blisters).

Composition of 1 capsule:

• active substance: isotretinoin - 10 or 20 mg;
• auxiliary components (10/20 mg): yellow beeswax - 7.68 / 15.36 mg, soybean oil - 107.92 / 215.84 mg, hydrogenated soybean oil - 7.68 / 15.36 mg, partially hydrogenated soybean oil - 30.72 / 61.44 mg;
• capsule shell (10/20 mg): gelatin - 75.64 / 120.66 mg, glycerol 85% - 31.275 / 49.835 mg, Karion 83 (mannitol, hydrolyzed potato starch, sorbitol) - 8.065 / 12.86 mg, red dye iron oxide (E172) - 0.185 / 0.145 mg, titanium dioxide (E171) - 1.185 / 1.97 mg;
• ink: shellac, black iron oxide dye (E172); use of ready-made ink Opacode Black S-1-27794 is acceptable.

Pharmacological properties

Pharmacodynamics

Isotretinoin is a stereoisomer of all-trans retinoic acid (tretinoin). The exact mechanism of action of the active component of Roaccutane has not yet been fully determined, but it has been proven that the improvement in the condition of patients with severe forms of acne (a decrease in the severity of symptoms) is explained by the inhibition of the activity of the sebaceous glands and a decrease in their size, confirmed by histological studies. Isotretinoin also has an anti-inflammatory effect on the skin.

The cause of desquamation of corneocytes into the duct of the sebaceous gland and blockage of the latter with excess sebaceous secretion and keratin is hyperkeratosis of epithelial cells of the sebaceous gland and hair follicle. In the future, this leads to the formation of a comedone, and in some cases - the development of an inflammatory process. Isotretinoin is an inhibitor of sebocyte proliferation and acts on acne by normalizing the process of cell differentiation. Sebum is the main substrate for the growth of Propionibacterium acnes, so a decrease in sebum production inhibits bacterial colonization of the duct.

Pharmacokinetics

Since the pharmacokinetic parameters of isotretinoin and its metabolites tend to be linear, its content in plasma during treatment can be predicted based on information obtained after a single dose. This characteristic of Roaccutane also confirms the absence of an effect on the activity of hepatic enzymes involved in the metabolism of drugs.

The absorption of isotretinoin from the gastrointestinal tract may vary. Its absolute bioavailability has not been determined, since Roaccutane is not available in a dosage form intended for intravenous administration to humans. However, extrapolating the results of studies in which dogs have been involved suggests a rather low and variable systemic bioavailability. In patients with acne, the maximum equilibrium plasma concentration of isotretinoin after ingestion of 80 mg of Roaccutane on an empty stomach was 310 ng / ml (the value ranged from 188 to 473 ng / ml) and was reached in about 2–4 hours. The content of isotretinoin in plasma is approximately 1.7 times higher than its content in the blood, which is due to the insignificant degree of penetration of the substance into erythrocytes.

Taking Roaccutane together with food increases bioavailability by 2 times compared to taking the drug on an empty stomach.

The degree of binding of isotretinoin to plasma proteins (mainly albumin) tends to a maximum (99.9%), therefore, in a wide range of recommended doses, the concentration of an unchanged active substance with pharmacological activity does not exceed 0.1% of the dose taken.

The volume of distribution of isotretinoin in humans has not been determined because Roaccutane is not available in an intravenous dosage form.

In patients with severe acne who took 40 mg of the drug 2 times a day, the equilibrium concentrations of isotretinoin in the blood were 120-200 ng / ml. The concentrations of 4-oxo-isotretinoin in these patients were 2.5 times higher than those for isotretinoin. Information on the penetration of the drug into tissues when used in humans is considered insufficient. The content of isotretinoin in the epidermis is 2 times less than in serum.

After oral administration, 3 main metabolites are determined in plasma: 4-oxo-retinoin, tretinoin (all-trans-retinoic acid) and 4-oxo-isotretinoin. The main metabolite is considered to be 4-oxo-isotretinoin, the content of which in blood plasma in an equilibrium state is 2.5 times higher than the content of isotretinoin. Metabolites of lesser clinical significance (for example, glucuronides) have also been identified, but their structure is not precisely established in all cases.

Isotretinoin metabolites are characterized by biological activity proven by several laboratory tests. Therefore, the therapeutic effect of Roaccutane in patients may be due to the pharmacological activity of isotretinoin and its metabolites. Since in vivo isotretinoin and tretinoin (all-trans-retinoic acid) reversibly pass into each other, the metabolism of tretinoin depends on the metabolism of isotretinoin. About 20-30% of the dose of the drug is metabolized by isomerization. The pharmacokinetic parameters of isotretinoin are significantly influenced by enterohepatic circulation.

Studies of metabolic processes in vitro confirm that the conversion of isotretinoin to 4-oxo-isotretinoin and tretinoin is carried out with the participation of several enzymes of the cytochrome P ₄₅₀ (CYP) system. Presumably, none of the forms plays a key role in this. Isotretinoin and its metabolites do not significantly alter the activity of CYP enzymes.

After oral administration of isotretinoin labeled with a radioactive nuclide, it is excreted through the kidneys and through the intestines in approximately equal amounts. In the final phase, the half-life for the unchanged drug in patients with acne is on average 19 hours. The terminal phase elimination half-life for 4-oxo-isotretinoin is probably longer, at about 29 hours.

Isotretinoin is a natural (physiological) retinoid. Endogenous concentrations of retinoids are restored approximately 2 weeks after the end of treatment with Roaccutane.

Since the intake of isotretinoin is unacceptable for liver dysfunctions, it is not possible to determine the pharmacokinetic parameters in patients of this category. Renal failure does not alter the pharmacokinetics of Roaccutane.

Indications for use

• acne in severe forms (conglobate / nodular-cystic or in the presence of a risk of scarring);
• acne if other treatments fail.

Contraindications

• liver failure;
• severe hyperlipidemia;
• hypervitaminosis A;
• combined use with tetracyclines;
• pregnancy (if pregnancy occurs during therapy or within a month after its end, there is a very high probability of giving birth to a child with severe malformations) and lactation;
• age up to 12 years;
• hypersensitivity to the components of the drug.

According to the instructions, Roaccutane should be used with caution in the following conditions / diseases:

• alcoholism;
• diabetes;
• depression (anamnestic data);
• lipid metabolism disorders;
• obesity.

Instructions for the use of Roaccutane: method and dosage

Roaccutane is taken orally, preferably with food.

Frequency of admission - 1-2 times a day.

The doctor selects the dose individually. The effectiveness of therapy and adverse reactions are dose-dependent and vary from patient to patient.

The recommended starting daily dose is 0.5 mg / kg.

In most cases, the daily dose is in the range of 0.5-1 mg / kg, with a very severe course of the disease and in cases of treating acne of the trunk, it may be increased to 2 mg / kg.

The optimal course dose is 120-150 mg / kg (which is the basis for calculating the duration of treatment). Often, complete remission of acne can be achieved within 16-24 weeks of using Roaccutane. With very poor tolerance of the drug, it is possible to reduce the daily dose and increase the duration of the course.

In most cases, after a single course of treatment, acne disappears completely. With obvious relapses, a repetition of the course is indicated. It is prescribed no earlier than 2 months after the end of the first course (the period during which improvement may continue).

In severe renal impairment, therapy should be started at a lower dose (eg, 10 mg per day). In the future, it is increased to 1 mg / kg per day or the highest tolerable.

Side effects

Adverse reactions are usually reversible (after dose reduction / discontinuation of therapy), but in some cases they may persist after discontinuation of Roaccutane. In most cases, violations are dose dependent.

Possible side reactions:

• digestive system: nausea, diarrhea, inflammatory bowel disease (ileitis / colitis), bleeding, pancreatitis (especially with concomitant hypertriglyceridemia above 800 mg / dL, in rare cases - with a fatal outcome), reversible / transient increase in the activity of liver transaminases; in some cases - hepatitis (most often the changes did not go beyond the normal range and in the course of treatment returned to the initial parameters, but sometimes a dose adjustment or treatment cancellation was required);
• central nervous system and mental sphere: headache, depression, behavioral disturbances, seizures, increased intracranial pressure (“pseudotumor of the brain”: visual impairment, headache, vomiting, nausea, optic nerve edema);
• respiratory system: rarely - bronchospasm (more often with a history of bronchial asthma);
• hematopoietic system: neutropenia, accelerated ESR, decreased hematocrit, anemia, leukopenia, change in the number of platelets;
• musculoskeletal system: muscle pain with / without an increase in serum creatine phosphokinase, joint pain, tendinitis, arthritis, hyperostosis, tendon / ligament calcification, other bone changes;
• immune system: systemic / local infections caused by gram-positive pathogens (Staphylococcus aureus);
• sense organs: in some cases - photophobia, visual acuity disturbances, dark adaptation disturbance (decrease in twilight vision); rarely - a violation of color perception (disappears after the cancellation of therapy), conjunctivitis, lenticular cataract, blepharitis, keratitis, edema of the optic nerve (a manifestation of intracranial hypertension), eye irritation, hearing impairment at certain sound frequencies;
• disorders associated with hypervitaminosis A: dry skin, mucous membranes, including cheilitis, nasal bleeding, hoarseness, conjunctivitis, contact lens intolerance, reversible corneal opacity;
• laboratory indicators: lowering the level of high density lipoproteins, hypertriglyceridemia, hyperuricemia, hypercholesterolemia; rarely - hyperglycemia, diabetes mellitus (detected for the first time), increased activity of serum creatine phosphokinase (especially with intense physical exertion);
• dermatological reactions: itching, rash, fulminant acne, facial erythema / dermatitis, paronychia, sweating, pyogenic granuloma, persistent hair thinning, onychodystrophy, increased granulation tissue proliferation, reversible hair loss, photoallergy, hirsutism, photosensitivity, skin hyperpigmentation; at the beginning of therapy, acne may worsen for several weeks;
• others: proteinuria, glomerulonephritis, systemic hypersensitivity reactions, hematuria, lymphadenopathy, vasculitis (Wegener's granulomatosis, allergic vasculitis).

During post-marketing observations, cases of such severe skin reactions as Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis were recorded.

Overdose

An overdose of Roaccutane may be accompanied by symptoms characteristic of hypervitaminosis A. In this case, it is recommended to wash the stomach in the first few hours after taking the drug in high doses.

special instructions

Roaccutane should be prescribed by a physician, preferably a dermatologist, experienced in the use of systemic retinoids and aware of the risk of its teratogenicity. Male and female patients should be informed of this and have a copy of the information brochure.

To avoid the unintentional effect of Roaccutane on the body of other people, it is impossible to take donated blood from patients who receive or received the drug shortly before (within 30 days).

It is recommended to monitor the function of the liver and liver enzymes before starting therapy, after 1 month from the moment of its initiation, and then every 3 months or according to indications. As a rule, the increase in hepatic transaminases is transient and reversible and is within the normal range. If the norm is exceeded, a dose reduction or treatment cancellation is indicated.

Fasting serum lipids should be measured with the same frequency. As a rule, the normalization of lipid concentration occurs after dose reduction, discontinuation of therapy and following diet. A clinically significant increase in triglyceride levels should be monitored. Their rise over 9 mmol / l or 800 mg / dl can lead to acute pancreatitis, in some cases - with a lethal outcome. Therapy is canceled in case of persistent hypertriglyceridemia or with the development of symptoms of pancreatitis.

In rare cases, psychotic symptoms, depression, and very rarely suicidal attempts occur during treatment. Despite the fact that a causal relationship with the use of Roaccutane has not been established, special care must be taken when prescribing the drug to patients with a history of depression. It is also necessary to monitor all patients for the development of depression while taking the drug (consultation with a specialist may be required). If the cancellation of therapy does not lead to the disappearance of symptoms, further observation and treatment by a specialist is necessary.

At the beginning of therapy, in rare cases, an exacerbation of acne was noted, which passes without dose adjustment of Roaccutane for 7-10 days.

Several years after the therapeutic course of dyskeratosis with Roaccutane, with a total course dose and duration of therapy exceeding those recommended for acne therapy, bone changes occurred, including hyperostosis, premature closure of the epiphyseal growth zones, calcification of tendons / ligaments. In this regard, when prescribing Roaccutane to any patient, you must first carefully assess the ratio of benefits to risks.

At the beginning of therapy, to reduce dryness of the mucous membranes and skin, patients are recommended to use moisturizing ointments or body creams, lip balm.

Patients during the period of taking Roaccutane to detect the development of severe skin reactions need careful monitoring (if necessary, treatment is canceled).

Laser treatment and deep chemical dermabrasion procedures during therapy, as well as for 5-6 months after the end of the treatment course, should be avoided (possibly increased scarring in atypical places and the development of hypo- and hyperpigmentation). During the period of taking Roaccutane and within six months after its completion, epilation should not be carried out using wax applications (there is a possibility of epidermis detachment, dermatitis and scarring).

As a rule, corneal opacity, dryness of the conjunctiva of the eyes, keratitis and deterioration of night vision after the withdrawal of Roaccutane disappear. If the mucous membrane of the eyes is dry, it is possible to use moisturizing eye ointments or artificial tear preparations. With dry conjunctiva, monitoring is necessary for the likely development of keratitis. If there are complaints of vision, it is necessary to consult an ophthalmologist (the drug can be canceled). In cases of intolerance to contact lenses during the period of taking Roaccutane, glasses should be used.

During treatment, it is necessary to limit exposure to sunlight / ultraviolet rays. It is recommended to use sunscreens with a high protective factor (at least 15 SPF).

With the development of benign intracranial hypertension, incl. when combined with tetracyclines, Roaccutane is immediately canceled. Also, immediate withdrawal of therapy is indicated in cases of severe hemorrhagic diarrhea.

Patients belonging to a high-risk group (with diabetes mellitus, obesity, chronic alcoholism or fat metabolism disorders) may require more frequent laboratory tests of glucose and lipid levels during therapy. In diabetes (confirmed or suspected), a more frequent measurement of glycemia is recommended.

In some patients, during the period of therapy, there may be a decrease in the acuity of night vision, which in some cases persists even after the end of the course. In this regard, patients are advised to be careful when driving at night (requires careful monitoring of the state of visual acuity).

Application during pregnancy and lactation

Pregnancy is an absolute contraindication for prescribing a course of Roaccutane therapy. If the patient becomes pregnant during treatment or within a month after treatment, the risk of having a baby with severe intrauterine malformations is considered to be quite high.

Isotretinoin has a strong teratogenic effect. In pregnancy that occurs while taking this drug in any dose and even for a short period of time, the likelihood of intrauterine malformations in the fetus is very high (including from the central nervous system, large blood vessels and heart). The frequency of spontaneous miscarriages also increases.

Roaccutane should not be used in women of reproductive age, unless the patient's condition meets all of the following criteria:

• She suffers from severe acne (acne with a high risk of scarring, conglobata or nodular-cystic acne), showing resistance to more gentle treatments;
• She fully understands the need for precautions and is ready to use reliable methods of contraception recommended by a doctor;
• she accurately understands and is determined to follow any prescriptions of a specialist;
• in treatment associated with a relapse of the disease, she undertakes to constantly use the same effective contraceptive methods for one month before starting treatment with isotretinoin, during treatment and for one month after its completion, as well as regularly undergo a reliable test to determine pregnancy;
• she received information from a doctor about the risks inherent in pregnancy that occurred during the course of therapy and within 1 month after its termination, and the need for urgent consultation at the slightest suspicion of pregnancy;
• she undertakes to strictly see the doctor every month;
• she was warned by a specialist about the possible ineffectiveness of contraceptives;
• she should start treatment only on the 2-3rd day of the next normal menstrual cycle;
• she confirmed that she understands the essence of the precautions being taken;
• she has a negative result of the most accurate pregnancy test, obtained within 11 days before starting treatment with isotretinoin; Doctors strongly recommend a pregnancy test to be carried out monthly during the course of therapy and 5 weeks after its completion;
• she understands the need for and continuously uses effective contraception for 1 month before starting Roaccutane, during treatment and for 1 month after its completion; it is desirable to use at least two different methods of contraception, including the barrier method.

The use of contraception in accordance with the above instructions is recommended even for those patients who usually do not use contraceptive methods due to infertility (excluding women who have undergone hysterectomy), lack of sexual activity or amenorrhea.

In accordance with approved clinical practice, a pregnancy test, the sensitivity of which should not be less than 25 mIU / ml, should be performed in the first 3 days of the menstrual cycle.

Before starting treatment to rule out a possible pregnancy, the date and result of the initial pregnancy test are recorded with a specialist before using contraceptives. Women with irregular periods should have a pregnancy test based on their sexual activity. It is usually performed 3 weeks after unprotected intercourse. The doctor is obliged to conduct a conversation with the patient about methods of contraception.

A pregnancy test is performed on the day the drug is prescribed or 3 days before the woman's visit to the doctor. The latter should document the test results. It is allowed to prescribe Roaccutane only to those women who have used effective contraceptives for at least 1 month before starting treatment.

During the course of therapy, mandatory visits to the attending physician are recommended every 28 days. The need for monthly verification of the absence of pregnancy is due to local practice, the sexual activity of the individual patient and previous menstrual irregularities. 5 weeks after the completion of the course of therapy, a test is prescribed to exclude pregnancy.

A prescription for a drug for a woman of reproductive age can only be prescribed for 30 days; if it is necessary to continue therapy, Roaccutane is re-prescribed. It is recommended that the pregnancy test, the prescription and the purchase of the drug in the pharmacy be scheduled on the same day. You can buy Roaccutane in a pharmacy only within 7 days from the date of the prescription by a doctor.

In the case of male patients taking this drug, the available data confirm that the exposure of isotretinoin from the seminal fluid and semen of men into the female body is insufficient for the development of a teratogenic effect. Men should take care to minimize the risk of taking Roaccutane by others, especially women.

When pregnancy occurs, the course of treatment with Roaccutane is interrupted. It is necessary to discuss the feasibility of preserving it with a specialist with extensive knowledge of teratology. There is documented information on the diagnosis of severe intrauterine fetal malformations, provoked by the intake of isotretinoin. These include pathologies of the parathyroid glands, microcephaly, hydrocephalus, malformations of the thymus gland and face (cleft palate), malformations of the cerebellum, cardiovascular anomalies (defects in the septum, transposition of great vessels, tetrad of Fallot), microphthalmia, anomalies of the outer ear (narrowing or absence of the external auditory canal, microtia).

Since isotretinoin is characterized by high lipophilicity, it is most likely to pass into breast milk. Due to possible side effects, Roaccutane is not prescribed during lactation.

Drug interactions

With the combined use of Roaccutane with certain drugs / substances, the following effects may develop:

• vitamin A: increased symptoms of hypervitaminosis A (the combination is not recommended);
• tetracyclines: increased intracranial pressure (the combination is contraindicated);
• progesterone drugs: a decrease in their effectiveness;
• local exfoliative / keratolytic drugs for the treatment of acne: increased local irritation (the combination is contraindicated).

Analogs

Roaccutane analogues are: Retinoic ointment, Verocutane, Erase, Aknekutan, Isotretionin, Retasol.

Terms and conditions of storage

Store in a dark, dry place out of reach of children at temperatures up to 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Roaccutane

According to reviews, Roaccutane (according to experts) is well tolerated with strict adherence to the treatment regimen, and is also highly effective.

For mild to moderate acne vulgaris, the drug is not prescribed. During the course of treatment, patients recommend that it is imperative to monitor the state of the liver and the concentration of lipids (the analysis is done on an empty stomach).

Price for Roaccutane in pharmacies

The average price for Roaccutane with a dosage of 10 mg is 1,678-2,100 rubles, and with a dosage of 20 mg - 2,800-3,600 rubles (the package contains 30 tablets).

Roaccutane: prices in online pharmacies

Drug name Price Pharmacy

Roaccutane 10 mg capsule 30 pcs. 1728 RUB Buy

Roaccutane 10mg capsules 30 pcs. 1756 RUB Buy

Roaccutane 20 mg capsule 30 pcs. 2868 RUB Buy

Roaccutane 20mg capsules 30 pcs. RUB 3113 Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, 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!