How does telithromycin work?

Telithromycin is in a class of medications called ketolide antibiotics. It works by killing bacteria. Antibiotics such as telithromycin not work for colds, flu, or other viral infections. Taking antibiotics when they are not needed increases your risk of getting an infection later that resists antibiotic treatment.

What is the main indication of telithromycin?

KETEK is indicated for the treatment of community-acquired pneumonia (of mild to moderate severity) due to Streptococcus pneumoniae, (including multi-drug resistant S. pneumoniae [MDRSP1]), Haemophilus influenzae, Moraxella catarrhalis, Chlamydophila pneumoniae, or Mycoplasma pneumoniae, for patients 18 years or older.

How is azithromycin synthesized?

Our synthesis of azithromycin was initiated with the preparation of 2 through the desymmetrization method, asymmetric ethyl addition, and regioselective epoxide openings.

How does azithromycin inhibit protein synthesis?

Macrolide antibiotics inhibit protein synthesis by targeting the bacterial ribosome. They bind at the nascent peptide exit tunnel and partially occlude it. Thus, macrolides have been viewed as ‘tunnel plugs’ that stop synthesis of every protein.

How is telithromycin excreted?

After entering the systemic circulation, telithromycin is eliminated by multiple pathways (7% by biliary and/or intestinal excretion, 13% by renal excretion and 37% by hepatic metabolism). Telithromycin is metabolised via cytochrome P450 (CYP) 3A4 and non-CYP pathways.

Is telithromycin a macrolide?

The ketolides are a new subclass of macrolides, and telithromycin is the first of these agents to be approved. Modifications to the basic macrolide structure result in enhanced activity against penicillin- and erythromycin resistant respiratory pathogens.

What is the composition of azithromycin?

Azithromycin, as the dihydrate, is a white crystalline powder with a molecular formula of C38H72N2O12•2H2O and a molecular weight of 785.0.

What enzyme metabolizes azithromycin?

Azithromycin has been shown to be a weak substrate for CYP3A4, to be minimally metabolized by the enzyme, and to neither induce nor inhibit CYP3A4 activity [16].

What is the mechanism of action of azithromycin?

Azithromycin is a macrolide antibiotic which inhibits bacterial protein synthesis, quorum-sensing and reduces the formation of biofilm.

Why antibiotics inhibit protein synthesis?

Protein synthesis is a complex, multi-step process involving many enzymes as well as conformational alignment. However, the majority of antibiotics that block bacterial protein synthesis interfere with the processes at the 30S subunit or 50S subunit of the 70S bacterial ribosome.

Does telithromycin inhibit cyp3a4?

Like many imidazole-containing drugs, telithromycin is a strong inhibitor of CYP 3A4; therefore, it can affect the efficacy and toxicity profile of medications that are metabolized by this isoenzyme.

Why was telithromycin discontinued?

On March 11, 2016, the FDA announced that Sanofi Aventis discontinued the manufacturing of Ketek (telithromycin) 300 mg and 400 mg tablets. — The decision to discontinue Ketek was due to business reasons. — The last batch of Ketek expires in June 2016. The inventory of Ketek will be available until supply is depleted.

What type of antibiotic is azithromycin?

Azithromycin belongs to the class of drugs known as macrolide antibiotics. It works by killing bacteria or preventing their growth. However, this medicine will not work for colds, flu, or other virus infections. This medicine is available only with your doctor’s prescription.

Does azithromycin inhibit CYP450?

Azithromycin and dirithromycin neither inhibit cytochrome P450 enzymes nor are implicated in clinically significant drug-drug interactions.

What is CYP3A4 enzyme?

Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97) is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body.

What is the function of azithromycin?

Azithromycin is used to treat certain bacterial infections, such as bronchitis; pneumonia; sexually transmitted diseases (STD); and infections of the ears, lungs, sinuses, skin, throat, and reproductive organs.

What is the primary target of azithromycin?

Azithromycin binds to the 23S rRNA of the bacterial 50S ribosomal subunit. It stops bacterial protein synthesis by inhibiting the transpeptidation/translocation step of protein synthesis and by inhibiting the assembly of the 50S ribosomal subunit Label, 5.

Which drug inhibit protein synthesis?

Protein Synthesis Inhibitors

Drug	Drug Description
Tetracycline	An antibiotic used to treat a wide variety of susceptible infections.
Gentamicin	An aminoglycoside used to treat a wide variety of aerobic infections in the body.
Netilmicin	An aminoglycoside used to treat a wide variety of infections in the body.

Which class of drugs inhibit protein synthesis?

antibacterials
Protein synthesis inhibitors represent another major group of clinically useful antibacterials, such as erythromycin, tetracycline, chloramphenicol, and aminoglycosides. They selectively interact with the 70S bacterial ribosome and spare the 80S eukaryotic ribosome particle.

What is synthesis of aspirin?

Synthesis of Aspirin. After the synthesis of aspirin, the product was recrystallized for purification to rid the product of impurities. A major impurity that could be found in the crude product would be unreacted salicylic acid. The crude product and the purified product can be tested using ferric chloride.

What class of drug is telithromycin?

Telithromycin, a semi-synthetic erythromycin derivative, belongs to a new chemical class of antibiotics called ketolides. Ketolides have been recently added to the macrolide-lincosamide-streptogramin class of antibiotics. Similar to the macrolide antibiotics, telithromycin prevents bacterial growth by interfering with bacterial protein synthesis.

What is the role of salicylic acid in the synthesis of aspirin?

This time the hydroxyl group of the salicylic acid acts as the nucleophile to attack the carbonyl group of the acetic anhydride and replace one of the acetyl groups. After the synthesis of aspirin, the product was recrystallized for purification to rid the product of impurities.

How do you make acetylsalicylic acid from aspirin?

The mixture is heated to form the Acetylsalicylic Acid (C9H8O4) and Acetic Acid (C2H4O2). After the reaction takes place, water is water is used to cleanse the excess Acetic Anhydride from the product and cause the Aspirin product to crystallize.