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Isotretinoin is a first-generation retinoic acid, a stereoisomer of all-trans retinoic acid. It has an anti-seborrhoeic effect when taken orally, and has been shown to be particularly effective in severe acne. Yellow or orange-red crystalline powder or crystals, insoluble in water, slightly soluble in ethanol, very slightly soluble in ether, soluble in chloroform.
Uses of Isotretinoin.
It is a vitamin A drug with strong and fast inhibition of the proliferation and differentiation process of skin glandular cells, which is highly effective in severe nodular cystic acne.
This product is better absorbed in the stomach and intestines, while topical application is ineffective. It is used for severe acne, cystic acne, party acne which other medications are ineffective, and is also effective in skin disorders such as rosacea, ichthyosis, keratosis pilaris and pityriasis versicolor.
For severe acne, etc.
For the treatment of severe acne.
Pharmacological Effect of Isotretinoin.
Isotretinoin is a first-generation retinoic acid, a stereoisomer of all-trans retinoic acid. It has anti-oil effect when taken orally and has special therapeutic effect on severe acne. The mechanism of action is as follows:
1. It has the effect of shrinking the sebaceous glands, inhibiting the activity of sebaceous glands, and reducing the secretion of sebaceous glands, thus inhibiting the reproduction of Propionibacterium acnes, which relies on the lipid environment for growth.
2. It has the effects of antikeratinisation, inhibiting the over-proliferation of epidermal cells and promoting their differentiation, which can reduce the keratinisation of the follicular opening and sebaceous gland ducts.
3. It can also affect the function of monocytes and lymphocytes, inhibit the chemotaxis of neutrophils and have anti-inflammatory activity.
4. Selectively binds to retinoic acid nuclear receptors and exerts therapeutic effects. It inhibits the proliferation of Acinetobacter short rod bacillus and has immunostimulatory effect at low dose and immunosuppressive effect at high dose.
5. Inhibits the formation of collagenase and gelatinase in the skin and inhibits the activity of ornithine decarboxylase. Since the induction of ornithine decarboxylase can play a major role in skin mutations, isotretinoin can also inhibit tumourigenesis.
6. When used topically, the mechanism of action of this product is similar to that of retinoic acid, which can induce epidermal cell proliferation, promote the differentiation of the granular layer of epidermal cells to the stratum corneum, and regulate the follicular sebaceous epithelium to keratinise the abnormal process of keratinous plugs, so as to play a therapeutic role.
Product Method of Bulk Isotretinoin Powder.
The reaction of β-violet ketone with ethylmagnesium chloride, followed by reaction with triphenylphosphine to form triphenylengravates, and then with cyclopentenone derivatives, produced isotretinoin and its 8Z isomer. Its 8Z isomer was isolated and isomerised to isotretinoin by the action of palladium nitrate.
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