Azenil - General Information
A semi-synthetic macrolide antibiotic structurally related to erythromycin. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.
Pharmacology of Azenil
Azenil, a semisynthetic antibiotic belonging to the macrolide subgroup of azalides, is used to treat STDs due to chlamydia and gonorrhea, community-acquired pneumonia, pelvic inflammatory disease, pediatric otitis media and pharyngitis, and Mycobacterium avium complex (MAC) in patients with advanced HIV disease. Similar in structure to erythromycin. azithromycin reaches higher intracellular concentrations than erythromycin, increasing its efficacy and duration of action.
Azenil for patients
Patients should be instructed to take Zmax on an empty stomach (at least 1 hour before or 2 hours following a meal).
Patients should be instructed to immediately contact a physician if any signs of an allergic reaction occur.
Patients who vomit within the first hour should contact their health care provider about further treatment.
Keep bottle tightly closed. Store at room temperature. Use within 12 hours of constitution. Shake bottle well before use. The entire contents of the bottle should be consumed.
Patients should be advised that Zmax may be taken without regard to antacids containing magnesium hydroxide and/or aluminum hydroxide.
Patients should be counseled that antibacterial drugs including Zmax should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). Not taking the complete prescribed dose may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by Zmax or other antibacterial drugs in the future.
Co-administration of nelfinavir at steady-state with a single dose of azithromycin (2 ´600 mg tablets) results in increased azithromycin serum concentrations. Although a dose adjustment of azithromycin is not recommended when administered in combination with nelfinavir, close monitoring for known side effects of azithromycin, such as liver enzyme abnormalities and hearing impairment, is warranted.
Azithromycin did not affect the prothrombin time response to a single dose of warfarin. However, prudent medical practice dictates careful monitoring of prothrombin time in all patients treated with azithromycin and warfarin concomitantly. Concurrent use of macrolides and warfarin in clinical practice has been associated with increased anticoagulant effects.
Drug interaction studies were performed with azithromycin and other drugs likely to be co-administered. When used in therapeutic doses, azithromycin had a modest effect on the pharmacokinetics of atorvastatin, carbamazepine, cetirizine, didanosine, efavirenz, fluconazole, indinavir, midazolam, rifabutin, sildenafil, theophylline (intravenous and oral), triazolam, trimethoprim/sulfamethoxazole or zidovudine. Co-administration with efavirenz or fluconazole had a modest effect on the pharmacokinetics of azithromycin. No dosage adjustment of either drug is recommended when azithromycin is co administered with any of the above agents. Interactions with the drugs listed below have not been reported in clinical trials with azithromycin; however, no specific drug interaction studies have been performed to evaluate potential drug-drug interaction. Nonetheless, they have been observed with macrolide products. Until further data are developed regarding drug interactions when azithromycin and these drugs are used concomitantly, careful monitoring of patients is advised:
Digoxinñelevated digoxin concentrations.
Ergotamine or dihydroergotamineñacute ergot toxicity characterized by severe peripheral vasospasm and dysesthesia.
Cyclosporine, hexobarbital and phenytoin concentrations.
Laboratory Test Interactions
There are no reported laboratory test interactions.
Studies evaluating the use of repeated courses of Zmax have not been conducted.
Zmax is contraindicated in patients with known hypersensitivity to azithromycin, erythromycin or any macrolide or ketolide antibiotic.
Additional information about Azenil
Azenil Indication: For the treatment of patients with mild to moderate infections caused by susceptible strains of the designated microorganisms in the specific conditions: H. influenzae, M. catarrhalis, S. pneumoniae, C. pneumoniae, M. pneumoniae, S. pyogenes, S. aureus, S. agal
Mechanism Of Action: Azenil binds to the 50S subunit of the 70S bacterial ribosomes, and therefore inhibits RNA-dependent protein synthesis in bacterial cells.
Drug Interactions: Anisindione Increases the anticoagulant effect
Cyclosporine The macrolide increases the effect of cyclosporine
Dicumarol Increases the anticoagulant effect
Disopyramide The macrolide increases the effect of disopyramide
Lovastatin Azenil can possibly increase the statin toxicity
Acenocoumarol Increases the anticoagulant effect
Warfarin Increases the anticoagulant effect
Food Interactions: Take on empty stomach: 1 hour before or 2 hours after meals.
Do not take Aluminum or magnesium antacids or supplements while on this medication.
Generic Name: Azithromycin
Synonyms: Aritromicina [Spanish]; Azithramycine; Azithromycin Dihydrate; Azithromycine [French]; Azithromycinum [Latin]
Drug Category: Anti-Bacterial Agents; Other Macrolides
Drug Type: Small Molecule; Approved
Other Brand Names containing Azithromycin: Azenil; Azitromax; Aziwok; Aztrin; Hemomycin; Misultina; Mixoterin; Setron; Sumamed; Tobil; Tromix; Zeto; Zifin; Zithrax; Zithromax; Zitrim; Zitromax; Zitrotek; Vinzam; Zmax; Zitrocin; Azibiot; Azifine;
Absorption: Bioavailability is 37% following oral administration.
Toxicity (Overdose): Potentially serious side effects of angioedema and cholestatic jaundice were reported
Protein Binding: Serum protein binding is variable in the concentration range approximating human exposure, decreasing from 51% at 0.02 µg/mL to 7% at 2 µg/mL.
Biotransformation: Hepatic. In vitro and in vivo studies to assess the metabolism of azithromycin have not been performed.
Half Life: 68 hours
Dosage Forms of Azenil: Powder, for solution Oral
Powder, for solution Intravenous
Powder, for suspension Oral
Chemical IUPAC Name: (2R,3S,4R,5R,8R,10R,11R,13S,14R)-11-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-3,4,10-trihydroxy-13-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one
Chemical Formula: C38H72N2O12
Azithromycin on Wikipedia: http://en.wikipedia.org/wiki/Azithromycin
Organisms Affected: Enteric bacteria and other eubacteria