Read full story
Isotretinoin is a drug against acne chemically associated with retinoic acid and retinol (vitamin A). The exact mechanism of action is not known, it blocks the sebaceous glands, reduces the production of fat in the skin, and thereby prevents the development of acne. It is sold in many countries of the world and is considered one of the most effective means of fighting acne. In one recent study, 160 volunteers used Accutane for a period of 2-28 weeks. Of 133 patients who remained at the end of the experiment, 127 patients noted complete or almost complete disappearance of acne. That is 95% efficiency, which is very important for any drug. Also, 60% of the patients did not worry about pimples for a whole year after completing the Accutane. Bodybuilders use it for the same purpose to remove one of the most visible external side effects of using AAS-acne.
After taking Isotretinoin (Accutane) (13-cis retinoic acid), the serum concentration in it reaches a maximum within 2-4 hours. The bioavailability of isotretinoin when administered on an empty stomach is approximately 20%; when taken with food, the absorption of the drug is significantly increased. Isotretinoin does not have a local effect. In plasma, the drug is actively associated with albumin, and the concentration of isotretinoin in the blood is usually higher than in tissues.
Isotretinoin (Accutane) in the body reversibly turns into tretinoin, and about 20-30% of isotretinoin is metabolized by this route. With the repeated administration of the drug, its main metabolite, 4-oxoisotretinoin, accumulates in the blood. Metabolites and the starting material (in the form of conjugates with glucuronic acid) are secreted into bile. T1 / 2 isotretinoin is 6-36 hours. With repeated administration, the steady-state serum concentration is reached after 5-7 days. Some metabolites of isotretinoin disappear from the plasma quite slowly. Because of the possible teratogenic effect of retinoids, women are advised to avoid pregnancy for at least 1 month after stopping their intake. The pharmacokinetics of isotretinoin is reviewed by Allen and Bloxham in Symposium, 1989b.
History of Isotretinoin
Isotretinoin (Accutane) was developed by Hoffmann-La Roche, and was first put on the market in 1982. It was sold until 2002 under the patent name Accutane. Now he is on the market under a lot of names. Isotretinoin is a licensed drug, but in recent years its sale has been regulated because of side effects. In particular, women need to make sure that they are not pregnant. The drug carries yellow stickers with a list of possible side effects.
Composition of Isotretinoin (Accutane)
One 10 mg capsule contains: active substance:
- isotretinoin – 10 mg;
- auxiliary substances: soybean oil – 107.92 mg, beeswax yellow – 7.68 mg, soya beans hydrogenated oil – 7.68 mg, soya beans partially hydrogenated oil – 30.72 mg;
- capsule shell: glycerol 85% – 31.275 mg, gelatin – 75.64 mg, Carion 83 (potato hydrolyzed starch, mannitol, sorbitol) – 8.065 mg, iron dye red oxide (E172) 0.185 mg, titanium dioxide (E171) 1.185 mg;
- ink for inscription on the capsule ‘, shellac, iron dye oxide black (E172); it is allowed to use ready-made Opacode Black ink S-l-27794.
One capsule of 20 mg contains:
- active substance: isotretinoin – 20 mg;
- auxiliary substances: soybean oil – 215.84 mg, beeswax yellow – 15.36 mg, soya beans, hydrogenated oil – 15.36 mg, soya beans, partially hydrogenated oil – 61.44 mg;
- capsule shell: glycerol 85% – 49.835 mg, gelatin – 120.66 mg, Carion 83 (potato hydrolyzed starch, mannitol, sorbitol) – 12.86 mg, iron dye red oxide (E172) -0.145 mg, titanium dioxide (E171) – 1.97 mg;
- ink for applying the inscription on the capsule: shellac, iron dye oxide black (E172); it is allowed to use ready-made Opacode Black ink S-l-27794.
Isotretinoin (Accutane) is usually available in the form of gelatin capsules containing 10,20 or 40 mg of the drug.
Isotretinoin (Accutane) is a retinoic acid derivative, 13-cis-retinoic acid.
Pharmachologic effect of Isotretinoin (Accutane)
Retinoid for systemic therapy of acne.
Isotretinoin (Accutane) is a stereoisomer of fully trans-retinoic acid (tretinoin).
The exact mechanism of action of the drug Isotretinoin (Accutane) has not yet been clarified, but it has been established that the improvement of the clinical picture of severe acne forms is associated with suppression of sebaceous gland activity and histologically confirmed decrease in their size. In addition, the anti-inflammatory effect of isotretinoin on the skin has been proven.
Hyperkeratosis of the cells of the epithelium of the hair bulb and the sebaceous gland leads to corneocytes sloughing into the gland duct and to blockage of the latter with keratin and an excess of sebaceous secretion. This is followed by the formation of a comedon and, in some cases, accession
Side effects of Isotretinoin (Accutane)
Isotretinoin (Accutane) is a potent drug with associated side effects. This is a controversial drug. At one time newspapers were rumbling about him, that he can cause fetal defects, depression and cause suicide. Admission during pregnancy can cause serious complications in the development of the fetus. Also, it is somewhat hepatotoxic, can cause inflammation of the intestine, pancreatitis, suppression of good cholesterol and worsen hearing and vision, can also cause psychosis, palpitation, hoarseness, increased intracranial pressure and even deformation of the nasal cartilage if taken after surgery at this site.
Although it is not exactly proven that Isotretinoin (Accutane) can cause depression, psychosis and a propensity for suicide, this possibility can not be taken lightly.
This opportunity was investigated in 2005. 28 people participated in this study, half of them took Isotretinoin (Accutane), and half of them were modern antibiotics. Computed tomography was performed before and after 4 weeks of drug use. They showed changes in the part of the cerebral cortex, in the area that is responsible for depressive conditions. Those taking Isotretinoin (Accutane) in these areas decreased metabolism by 21%, while those taking antibiotics were only 2%.
Hypersensitivity, pregnancy is established and planned (possibly teratogenic and embryotoxic action); lactation period; hypervitaminosis A. For rectal administration – rectum disease. C with caution. Conditions that cause hypertriglyceridemia (including familial hypertriglyceridemia in history, alcoholism, obesity, diabetes mellitus – isotretinoin increases the concentration of triglycerides in the plasma, reduces the content of HDL and increases the risk of cardiovascular disease), hepatic and / or renal failure, chronic pancreatitis, hepatic and / or renal insufficiency, CHF, diabetes mellitus and predisposition to its development.
The usual dosage of Isotretinoin (Accutane) is 0.5-1 mg per kilogram of weight per day, that is, for a 100 kilogram athlete the dose will be 100 mg, every day. In very serious cases, you can increase the dose to 2 mg per kilogram of weight. The daily dose should be divided into two equal doses, which must be taken throughout the day. Isotretinoin should be taken with food, and not on an empty stomach, as food helps this drug to be absorbed. The course of treatment usually lasts 15-20 weeks. Between courses of therapy should take at least 2 months. In case of using bodybuilders without a prescription, the dose should be lowered in order to minimize the possibility of side effects. Duration of application is also reduced to 6-8 weeks. However, many athletes are prone to acne “on the course,” so they may need more than one course of treatment per year.
Showing all 3 results