Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
A remedy for acne treatment. Promotes the normalization of terminal differentiation of cells, inhibits the hyperproliferation of the epithelium of the excretory ducts of the sebaceous glands, the formation of detritus and facilitates its evacuation. Due to this, the production of sebum decreases, its isolation is facilitated, the composition is normalized, the inflammatory reaction around the glands is reduced. With external and systemic application it has antiseboric, sebostatic, anti-inflammatory, kerato-and immunomodulatory effects; strengthens the regeneration processes in the skin.
PHARMACOKINETICS
After ingestion isotretinoin absorbed from the gastrointestinal tract, absorption can increase when taken with food. C max in blood plasma is achieved 1-4 h after ingestion.
Bioavailability during ingestion is low, which may be due to parietal metabolism in the intestinal wall and the effect of "first passage" through the liver.
Isotretinoin binds to a high degree of plasma proteins. Metabolised in the liver with the formation of the main metabolite of 4-oxo-isotretinoin, there is also some isomerization of isotretinoin to tretinoin.
Isotretinoin, tretinoin and its metabolites undergo enterohepatic recirculation.
The final T 1/2 tretinoin is 10-20 hours. The equivalent amount is determined in feces, mostly unchanged, and in urine in the form of metabolites.
INDICATIONS
For oral administration: severe forms of nodular-cystic acne, especially with localization on the trunk.
For rectal administration: severe recurrent forms of acne, rash with concomitant seborrheic process.
For external use: papulo-pustular acne, seborrhea, rosacea, perioral dermatitis.
DOSING MODE
For oral administration, the initial dose is 500 mcg / kg / day; the maximum daily dose is applied for a limited time and is 1 mg / kg; maintenance dose - 0.1-1 mg / kg / day; duration of treatment - 16 weeks, repeated course is carried out with an interval of 8 days. Take with food in 1 or more receptions.
Rectal - 0.5-1 mg / kg 1 time / day for the night (in the supine position); course of treatment - 8-12 weeks, intervals between courses - 1-2 months.
Ointment applied a thin layer on the affected skin 2 times / day. Duration of treatment is 4-6 weeks.
SIDE EFFECT
Dermatological reactions: dryness of the mucous membranes, skin rash, dermatitis, itching, cheilitis, erythema (especially on the face), sweating, palmar-plantar peeling, paronychia, nail dystrophy, increased proliferation of granulation tissue in the affected area; rarely - thinning hair, vasculitis, photosensitivity.
From the senses: conjunctivitis, photophobia, decreased night vision, corneal opacity, hearing loss.
From the central nervous system and peripheral nervous system: headache; rarely - depression, convulsive seizures, propensity to suicide; in isolated cases - intracranial hypertension.
On the part of the digestive system: nausea; rarely - colitis, bleeding from the gastrointestinal tract, transient increase in the activity of hepatic transaminases; in isolated cases - hepatitis.
On the part of the hematopoiesis system: anemia, neutropenia, change in the number of platelets, increased ESR.
From the side of metabolism: increased concentration of TG, glucose.
From the musculoskeletal system: pain in the muscles and joints; rarely - hyperostosis.
Other: nosebleeds.
With rectal and external application: during 1-2 weeks of treatment, there may be new rashes, itching, swelling and redness of the skin.
CONTRAINDICATIONS
Pregnancy, established and planned, lactation, hypersensitivity to isotretinoin, simultaneous use of antibiotics of the tetracycline group.
For oral administration: severe violations of the liver and / or kidney function, hypervitaminosis A, a significantly elevated level of lipids in the blood plasma, neoplasms.
For rectal use - rectum disease.
PREGNANCY AND LACTATION
Isotretinoin has a pronounced teratogenic and embryotoxic effect.
Contraindicated with an established and planned pregnancy.
Contraindicated during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Rectally and externally apply with caution in diseases of the kidneys.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Rectally and externally apply with caution in liver diseases.
APPLICATION FOR CHILDREN
Safety of use in children and patients of prepubescent age is not established.
SPECIAL INSTRUCTIONS
Rectally and externally apply with caution in diseases of the liver, kidneys, chronic pancreatitis, cardiac decompensation, chronic intoxications (including alcohol).
When rectal and external application with a sharp exacerbation reaction (at the 1-2 nd week of treatment), it is recommended to cancel the treatment for a few days before it subsides, then the therapy can be resumed.
Ingestion requires regular monitoring of liver function and lipid levels in blood plasma before treatment, 1 month after the start of therapy, and then every 3 months.
With diabetes, obesity, alcoholism or lipid metabolism disorders, more frequent monitoring of laboratory parameters is recommended. When diabetes mellitus or suspected of it, you need to strictly monitor the level of glucose in the plasma.
With prolonged use, it is possible to develop symptoms of chronic hypervitaminosis A.
During the treatment period or for some time after its termination, it is impossible to be donors for women of childbearing age.
On the background of therapy, patients should not be prescribed UV-therapy, patients should avoid direct exposure to sunlight.
During treatment, contact lens intolerance may occur.
Safety of use in children and patients of prepubescent age is not established.
It should avoid simultaneous use of isotretinoin and derivatives of 19-nortestosterone, especially in patients with gynecological / endocrine diseases.
It is not recommended simultaneous use of other drugs that have keratolytic or exfoliative properties (including other retinoids), as well as progesterone in microdoses (including mini-pills).
DRUG INTERACTION
The effect of isotretinoin is weakened by the simultaneous use of progesterone in microdoses.
With the simultaneous use of isotretinoin and vitamin A, it is possible to intensify toxic effects.
With the simultaneous use of isotretinoin and antibiotics of the aminoglycoside group, there is a risk of developing intracranial hypertension.
