Antibiotic Clarithromycin Raw Materials powder 81103-11-9

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Clarithromycin of Usage and Synthesis.

Clarithromycin is a semi-synthetic macrocyclic lipid antibiotic, which can inhibit the synthesis of bacterial protein and achieve antibacterial effect. It can play a strong antibacterial effect on gram-positive and gram-negative bacteria, and can significantly improve the clinical symptoms of patients. Clinical applications are widely used, including soft tissue infection, skin infection, respiratory system, urinary system infection and eradication of Helicobacter pylori therapy.

1. It can be used to treat pharyngitis and tonsillitis caused by streptococcus pyogenes.

2. It can be used to treat acute otitis media, sinusitis, acute bronchitis, acute onset of chronic bronchitis and pneumonia caused by sensitive bacteria.

3. It can be used to treat skin and soft tissue infection caused by sensitive bacteria.

4. It can be used to treat mycoplasma pneumoniae pneumonia, chlamydia trachomatis caused urethritis and non-specific urethritis (cervicitis).

5. Can be used to treat Legionnaires' disease (Legionella infection).

6. Clarithromycin can also be used in combination with other drugs to treat Mycobacterium avium infection and Helicobacter pylori infection.

Uses of Clarithromycin.

Macrolide antibiotics, which are derivatives of erythromycin, change the OH group on the 6 position of erythromycin A to OCH3, that is, clarithromycin. It is effective against gram-positive and negative bacteria, chlamydia and mycobacterium, and can effectively inhibit almost all respiratory pathogens. Stable to gastric acid, good oral absorption, high blood concentration, long blood half-life. Its use is similar to erythromycin, and it is effective for respiratory tract, urinary tract, skin, ear, nose and throat infections.

It is a macrolide antibiotic for the treatment of upper and lower respiratory tract infections, subcutaneous soft tissue infections, etc.

Pharmacological action of Clarithromycin.

Clarithromycin is a 14-membered macrolide broad-spectrum antibiotic. Its mechanism of action is the same as erythromycin, which is mainly bound to the bacterial 50S ribosome subunit and inhibits the synthesis of bacterial proteins by blocking the peptide transfer and mRNA shift, thus playing an antibacterial role.

Compared with erythromycin, clarithromycin has the characteristics of good oral absorption, fast peak time, high blood concentration, long half-life and small individual difference. Clarithromycin has a slightly stronger antibacterial action against methicillin-sensitive staphylococci and streptococci than erythromycin. The antibacterial activity against influenza bacillus is 2 to 4 times stronger than erythromycin (its metabolites 14-hydroxyclarithromycin and clarithromycin have synergistic antibacterial action against influenza bacillus). The effect on Legionella pneumophila, chlamydia trachomatis and mycoplasma urealyticum was also stronger than erythromycin.

Clarithromycin has antibacterial effect on Staphylococcus aureus and streptococcus. It has bactericidal effect on pneumococcus and influenza bacillus. Clarithromycin has strong antibacterial activity against Staphylococcus aureus, Streptococcus, Haemophilus influenzae, Legionella, gonococcus, catarrania and Helicobacter pylori. It also has antibacterial effect on Mycobacterium avium, Mycobacterium and leprae. In addition, it is also effective against mycoplasma pneumoniae, chlamydia trachomatis and mycoplasma urealyticum.

Erythromycin sensitive bacteria such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, dicoccus pneumoniae obviously superior to erythromycin, streptococcus faecalis and Haemophilus influenzae antibacterial action is the same as erythromycin, with erythromycin cross-resistance. Drug-resistant bacteria can produce an enzyme that methylates RNA, methylating the binding site of the ribosome so that the drug cannot bind to the ribosome. The antibacterial effect of clarithromycin on Staphylococcus aureus, Streptococcus pyogenes, diplococcus pneumoniae and Haemophilus influenzae was 2 ~ 10 times stronger than erythromycin.

Product method of Bulk Clarithromycin Powder.

Using erythromycin as raw material, water deactivates a methyl group on the amino group, then reacts with benzyl chloroformate to protect the hydroxyl group and amino group on the 5-position side chain tetrahydropyran ring, then neutralizes iodomethane with dimethyl sulfoxide and tetrahydrofuran, methylates the hydroxyl group on the 6-position, catalyzes hydrogen deactivates the protective group, reacts with formaldehyde to hydroxymethylate the amino group, and finally reduces to methyl group. That's clarithromycin.

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