Telithromycin

Telithromycin Uses, Dosage, Side Effects, Food Interaction and all others data.

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. Telithromycin binds to the 50S subunit of the 70S bacterial ribosome and blocks further peptide elongation. Binding occurs simultaneously at to two domains of 23S RNA of the 50S ribosomal subunit, domain II and V, where older macrolides bind only to one. It is used to treat mild to moderate respiratory infections.

Telithromycin is a ketolide antibiotic which has an antimicrobial spectrum similar or slightly broader than that of penicillin. It is often used as an alternative in patients who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including mycoplasma. Telithromycin prevents bacterial growth by binding to bacterial 50S ribosomal subunits and interfering with bacterial peptide translocation and elongation.

Telithromycin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Telithromycin
Availability	Discontinued
Generic	Telithromycin
Telithromycin Other Names	Telithromycin, telitromicina
Related Drugs	amoxicillin, prednisone, doxycycline, ciprofloxacin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, cefdinir
Type	Oral
Formula	C₄₃H₆₅N₅O₁₀
Weight	Average: 812.018 Monoisotopic: 811.473143313
Protein binding	60 - 70% bound primarily to human serum albumin
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Telithromycin is an ketolide used to treat community acquired pneumonia of mild to moderate severity.

For the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.

Telithromycin is also used to associated treatment for these conditions: Mild community-acquired pneumonia, Moderate community-acquired pneumonia

How Telithromycin works

Telithromycin acts by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. By binding at domain II, telithromycin retains activity against gram-positive cocci (e.g. Streptococcus pneumoniae) in the presence of resistance mediated by methylases (erm genes) that alter the binding site at domain V. Telithromycin may also inhibit the assembly of nascent ribosomal units. Compared to erythromycin A, telithromycin binds to the 23S rRNA with 10 times greater affinity in erythromycin-susceptible organisms and 25 times greater affinity in macrolide-resistant strains. This increased binding affinity may be conferred by the C11-12 carbamate side chain of telithromycin. The side chain appears to maintain binding at domain II in the presence of resistance mediated by alterations in domain V.

Toxicity

LD50>2000 mg/kg (PO in rats). Adverse effects are similar to those of clarithormycin and erithromycin and include diarrhea, nausea, vomiting, loose stools, abdominal pain, flatulence and dyspepsia. It may also cause dizziness, headache and taste disturbances.

Food Interaction

Take with or without food. The absorption is unaffected by food.

Telithromycin Disease Interaction

Major: colitis, hepatitis, liver disease, myasthenia gravis, QT interval prolongationModerate: hemodialysis, renal dysfunction

Volume of Distribution

2.9 L/kg

Elimination Route

Absolute bioavailability is approximately 57%. Maximal concentrations are reached 0.5 - 4 hours following oral administration. Food intake does not affected absorption.

Half Life

Main elimination half-life is 2-3 hours; terminal elimination half-life is 10 hours

Elimination Route

The systemically available telithromycin is eliminated by multiple pathways as follows: 7% of the dose is excreted unchanged in feces by biliary and/or intestinal secretion; 13% of the dose is excreted unchanged in urine by renal excretion; and 37% of the dose is metabolized by the liver.