Clarithromycin (Biaxin, Klacid) is a macrolide antibiotic and a CYP3A4 substrate and inhibitor. Clarithromycin (Biaxin, Klacid) prevents bacteria from growing by interfering with their protein synthesis. Clarithromycin (Biaxin, Klacid) binds to the subunit 50S of the bacterial ribosome and thus inhibits the translation of peptides. Clarithromycin (Biaxin, Klacid) has similar antimicrobial spectrum as erythromycin but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila. Clarithromycin (Biaxin, Klacid) is used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydia pneumoniae or TWAR), skin and skin structure infections. Besides, clarithromycin (Biaxin, Klacid)is a substrate and inhibitor of CYP3A4. Inhibitors of CYP3A4 may increase clarithromycin (Biaxin, Klacid) serum concentrations. Inducers of CYP3A4 substrates may decrease clarithromycin (Biaxin, Klacid) serum concentrations.
| Molecular Weight | 747.95 |
| Formula | C38H69NO13 |
| CAS Number | 81103-11-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] No authors listed. Tuberculosis (Edinb). Clarithromycin
[4] G W Amsden. Erythromycin, clarithromycin, and azithromycin: are the differences real?
[5] F Fraschini, et al. Clarithromycin clinical pharmacokinetics
| Related Cytochrome P450 (e.g. CYP17) Products |
|---|
| Cytochrome P450 reductase
Cytochrome P450 reductase is a NADPH-cytochrome reductase. |
| 20-SOLA
20-SOLA is a water-soluble 20-HETE antagonist. |
| TS-011
TS-011 is a selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis. |
| Dibromo-dodecenyl-methylsulfimide
Dibromo-dodecenyl-methylsulfimide is a selective inhibitor of 20-HETE synthesis and attenuates the vasodilatory response to sodium nitroprusside (SNP). |
| Abiraterone decanoate
Abiraterone decanoate is a novel, long-acting Abiraterone precursor compound that also exhibits high CYP17 cleavage enzyme inhibition selectivity for prostate cancer related studies. |
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