Tezolid

Indications

Tezolid is an oxazolidinone-class antibiotic indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible bacteria in adult patients.

To help prevent the development of drug-resistant bacteria and preserve the effectiveness of Tezolid and other antibiotics, it should only be used for infections proven or suspected to be caused by susceptible microorganisms.
Consult a registered healthcare provider before use.

Pharmacology

After being converted to its active form by phosphatases, Tezolid works by inhibiting bacterial protein synthesis. It binds to the 50S ribosomal subunit in Gram-positive bacteria, preventing the formation of essential proteins. Tezolid differs from other non-oxazolidinone antibiotics in its mechanism of action, minimizing cross-resistance.

Dosage & Administration

For the treatment of acute bacterial skin and skin structure infections (ABSSSI):

• Intravenous: 200 mg once daily for 6 days (administered over 1 hour).
• Oral: 200 mg once daily for 6 days.

No dose adjustment is necessary when transitioning from intravenous to oral Tezolid. If a dose is missed, it should be taken as soon as possible if it’s within 8 hours of the next dose. If less than 8 hours remain before the next dose, skip the missed dose and take the next dose as scheduled.
Consult a registered healthcare provider before use.

Drug Interactions

Tezolid may increase plasma concentrations of certain Breast Cancer Resistance Protein (BCRP) substrates when taken orally. If coadministration is unavoidable, monitor for potential adverse reactions associated with these drugs.

Contraindications

There are no known contraindications for Tezolid.

Side Effects

The most common side effects of Tezolid include:

• Nausea
• Headache
• Diarrhea
• Vomiting
• Dizziness

Pregnancy & Lactation

• Pregnancy Category C: There are no well-controlled studies of Tezolid in pregnant women. It should be used during pregnancy only if the potential benefits justify the potential risks to the fetus.
• Lactation: Tezolid has been detected in rat breast milk. It is unknown whether Tezolid is excreted in human milk, so caution is recommended if used by nursing mothers.

Precautions & Warnings

• Neutropenia: The safety and effectiveness of Tezolid have not been evaluated in patients with neutropenia (neutrophil count < 1000 cells/mm³). In animal studies, Tezolid’s antibacterial activity was reduced without granulocytes, so alternative treatments should be considered for neutropenic patients.
• Clostridium difficile-associated diarrhea: If diarrhea develops during treatment, consider evaluating for possible Clostridium difficile infection.

Use in Special Populations

• Pediatric Use: The safety and effectiveness of Tezolid in patients under 18 years of age have not been established.
• Geriatric Use: While Tezolid has not been specifically studied in elderly populations, no significant differences in pharmacokinetics have been observed between older and younger adults. However, caution is advised.

Overdose Effects

In the event of an overdose, discontinue Tezolid and provide general supportive care. Hemodialysis is not effective at removing Tezolid from the bloodstream.

Therapeutic Class

Tezolid belongs to the class of other antibiotics.

Storage Conditions

Store Tezolid tablets and injections at 20°C to 25°C (68°F to 77°F), and keep them protected from light.