Description

Compound:

Each capsule contains:

Isotretinoin

Auxiliary components:

yellow beeswax, hydrogenated soybean oil, partially hydrogenated soybean oil, refined soybean oil;

capsule shell: gelatin, glycerol, dry substance Karion, mannitol, hydrogenated hydrolyzed starch, titanium dioxide.

Properties:

Pharmacological action – anti-inflammatory, anti-seborrheic, dermatoprotective, A-vitamin-like, anti-acne.

Normalizes the terminal differentiation of cells, inhibits the proliferation of the epithelium of the ducts of the sebaceous glands, the formation of detritus, facilitates its evacuation. Reduces production and facilitates the secretion of sebum. When taken orally, absorption is variable, bioavailability is low and variable; taking with food increases bioavailability by 2 times. Tmax – 2-4 hours. Plasma protein binding (mainly albumin) – 99.9%. It is metabolized to form three main biologically active metabolites – 4-oxo-isotretinoin (the main metabolite), tretinoin and 4-oxo-retinoin, as well as less significant metabolites, including glucuronides. Since isotretinoin and tretinoin are reversibly converted into each other in vivo, the metabolism of tretinoin is associated with the metabolism of isotretinoin. 20-30% of a dose of isotretinoin is metabolized by isomerization. Enterohepatic circulation may play a significant role in the pharmacokinetics of isotretinoin in humans. In vitro studies have shown that isoenzymes CYP2C8, CYP2C9, CYP3A4 and CYP2B6 of cytochrome P450 are involved in the metabolism of isotretinoin. T1 / 2 isotretinoin – 19 hours, 4-oxo-isoretinoin – 29 hours. It is excreted by the kidneys and bile in approximately equal amounts.

Indications:

For oral administration: severe forms of acne (nodular cystic, conglobate, acne with a risk of scarring); acne, not amenable to other types of therapy.

Dosage and administration:

The optimal dosage regimen is selected by the doctor after the examination.

Inside taken with meals, the initial dose is 0.5 mg / kg per day, which is divided into two parts, used for 16 – 24 weeks. Usually, patients take 0.5-10 mg / kg / day. In case of damage to the trunk or severe disease – 2 mg / kg per day. In severe chronic renal failure, the initial dose should be reduced to 10 mg per day. Depending on the severity of adverse reactions and / and response to treatment, dose adjustment is carried out. If in 16-24 weeks the number of rashes has decreased by 70% or more, then the therapy is stopped. A second course of treatment is carried out upon confirmation of a recurrent or persistent course of the disease with an interval of at least 2 months.

Contraindications:

Hypersensitivity, for oral administration: pregnancy, established or planned (possibly teratogenic and embryotoxic effects), breastfeeding period, liver failure, hypervitaminosis A, severe hyperlipidemia, concomitant tetracycline therapy.

Precautionary measures:

During therapy, it is necessary to control the level of lipids, glucose, and liver function. Patients with diabetes are advised to conduct more frequent monitoring of blood glucose levels. Women of reproductive age should use reliable contraceptive measures 4 weeks before, during and for 1 month after the end of treatment. If pregnancy occurs, it should be terminated for medical reasons. In the event of colitis, visual disturbances and symptoms of a pseudotumor of the brain, treatment is stopped. If a brain pseudotumor is suspected, a neurological examination is performed. Do not prescribe isotretinoin to patients receiving other drugs from the group of retinoids (to avoid hypervitaminosis A). It is necessary to avoid increased insolation, incl. UV therapy. Treatment with isotretinoin may reduce contact lens tolerance. Patients wearing contact lenses, in case of side effects from the eyes, should use glasses.

Side effects:

From the nervous system and sensory organs: excessive fatigue, headache, increased intracranial pressure (pseudotumor of the brain: headache, nausea, vomiting, blurred vision, swelling of the optic nerve), convulsive seizures, xerophthalmia, isolated cases of impaired visual acuity, photophobia, violation of dark adaptation (decrease in the sharpness of twilight vision);

On the part of the digestive tract: dryness of the oral mucosa, bleeding from the gums, inflammation of the gums, nausea, diarrhea, inflammatory bowel disease (colitis, ileitis), bleeding, pancreatitis;

On the part of the hematopoietic system: anemia, a decrease in hematocrit, leukopenia, neutropenia, an increase or decrease in the number of platelets, an acceleration of ESR.

From the respiratory system: rarely – bronchospasm (more often in patients with a history of bronchial asthma).

From the musculoskeletal system: muscle pain with or without elevated serum CPK levels, joint pain, hyperostosis, arthritis