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Amphotericin B:Amphotericin B is also known as lushanamycin. The molecular composition of amphotericin B is a macrocyclic lactone containing 7 pairs of conjugated double bonds as a ligand and a deoxyamino-hexose of trehalose (mycosamine) as a sugar group. It is a amphoteric substance because of the presence of an amino group and a carboxyl group in the structure. A polyene antifungal antibiotic was isolated from the culture medium of Streptomycesnodosus, which was identical with the Lushanmycin produced by the actinomycin isolated from the soil of Jiangxi Lushan in 1974. It has significant bacteriostatic effect on Cryptococcus neoformans, Bacillus dermatitis, Bacillus brasiliensis, Histoplasmosis capsulatum, lateral spora Schenckella, Candida albicans and some nocardia. Dissolved in dimethyl sulfoxide, slightly dissolved in dimethyl formamide, very slightly dissolved in methanol, and insoluble in water, anhydrous ethanol, chloroform, or ether. Amphotericin B is almost effective to most fungi, and drug-resistant strains are rare and the price is low, which makes it still show high practical Chemicalbook value in clinical application for more than 40 years. However, due to its obvious nephrotoxicity and infusion related toxicity (such as fever, chills, nausea, etc.), the promotion and application of amphotericin B is greatly limited. Salt can be formed in neutral or acidic medium, and its water solubility increases but its antibacterial activity decreases. The deoxycholate compound is a light yellow powder, which can form a colloidal solution in water and can be used for injection. This product can maintain long-term stability under the condition of drying, avoiding light and refrigeration, but its aqueous solution should not be more than 24h at room temperature, and can only be stored for one week at 4℃. The antibacterial effect was strongest at pH6.0 ~ 7.5, and weakened at low pH. Its bacteriostatic mechanism is that it can bind with ergosterol on fungal cell membrane, resulting in cell membrane damage, increased permeability, and cell substances escape and die. Bacterial cell membrane does not contain ergosterol component, so ineffective. This product is not easy to absorb orally, and the effective blood concentration can be maintained for more than 24h after intravenous infusion. It doesn't cross the blood-brain barrier easily.
Amphotericin B uses:Amphotericin B is the first choice for deep fungal infection with a wide range of antifungal spectrum. It has an inhibitory effect on cryptococcus, coccidioides, Candida albicans, blastomyces, etc., and a bactericidal effect at high concentration. It is an effective drug for the treatment of deep fungal infection. The main clinical indications are as follows:
① Amphotericin B for cryptococcosis, North American blastomycosis, disseminated candidiasis, coccidiocosis, histoplasmosis.
② Amphotericin B is used to treat mucormycosis caused by Rhizopus, ploughshares, endocytids and frogfaecal fungi.
③ Amphotericin B for the treatment of sporotrichosis caused by Sporotrichia Schenck.
④ Amphotericin B for the treatment of Aspergillosis caused by Aspergillus fumigatus.
⑤ Topical preparation is suitable for pigmentation mycosis, skin fungal infection after burn, respiratory candida, Aspergillus or cryptococcus infection, fungal corneal ulcer.
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