Tedizolid

Approved Uses

Tedizolid is an oxazolidinone antibiotic primarily used to treat acute bacterial skin and skin structure infections (ABSSSI). These are serious infections that affect the skin and the tissues just beneath it.

Conditions Treated

Healthcare providers prescribe tedizolid for several types of skin-related bacterial infections, including:

• Cellulitis
• Erysipelas
• Major cutaneous abscesses
• Infected wounds

This medication is specifically designed to target Gram-positive bacteria. It is effective against Staphylococcus aureus, including methicillin-resistant strains (MRSA), as well as various Streptococcus species and Enterococcus faecalis.

Tedizolid is only intended to treat infections caused by bacteria; it will not work for viral infections such as the common cold or flu. Using antibiotics when they are not needed increases the risk of getting an infection later that resists antibiotic treatment.

Mechanism of Action

Tedizolid belongs to a class of medications known as oxazolidinone antibiotics. It works by disrupting the internal processes of certain types of bacteria, specifically Gram-positive bacteria. To survive and multiply, bacteria must constantly produce new proteins. Tedizolid binds to a specific part of the bacterial cell called the 50S ribosome, which acts as the protein-making machinery.

By attaching to this site, the medication prevents the bacteria from assembling essential proteins. This action has different effects depending on the specific strain of bacteria involved:

• Bacteriostatic effect: For many types of bacteria, the drug stops them from growing and reproducing, which allows the body's immune system to clear the remaining infection.
• Bactericidal effect: For certain other types of bacteria, such as specific strains of streptococci, the drug may kill the bacteria directly.

Because tedizolid works differently than many older antibiotics, it can often remain effective against bacteria that have developed resistance to other treatments.

Common Side Effects

The most common side effects associated with tedizolid are usually mild and may include:

• Nausea
• Headache
• Diarrhea
• Vomiting
• Dizziness

Serious Side Effects

While less common, some side effects can be serious. Seek medical attention immediately if you notice:

• Allergic reactions: Symptoms such as hives, rash, difficulty breathing, or swelling of the face, lips, tongue, or throat.
• Severe diarrhea: Watery or bloody stools, which may be a sign of a new infection. Do not use anti-diarrhea medicine unless told to do so by a doctor.
• Vision problems: Any changes in vision, including blurred vision or changes in how you see colors.
• Neuropathy: Numbness, tingling, or a pins and needles sensation in the hands or feet.
• Low blood cell counts: Unusual bruising, pale skin, or feeling lightheaded.

In rare cases, tedizolid may interact with other medications to cause serotonin syndrome. Symptoms include confusion, rapid heart rate, sweating, and muscle tremors.

Neutropenia

Tedizolid may lead to a decrease in white blood cell counts, a condition known as neutropenia. This risk is generally higher in individuals who already have low white blood cell levels before starting treatment. Healthcare providers may monitor blood counts if the medication is used for longer than the recommended duration or in patients with pre-existing blood disorders.

Clostridioides difficile-Associated Diarrhea

Like most antibacterial agents, tedizolid can cause Clostridioides difficile-associated diarrhea (CDAD). This condition occurs because the antibiotic alters the normal bacteria in the colon, allowing C. difficile to grow. Symptoms can range from mild diarrhea to life-threatening inflammation of the colon. If severe, watery, or bloody diarrhea occurs during or after treatment, medical attention is required.

Neuropathy

Peripheral and optic neuropathy have been reported in patients treated with the oxazolidinone class of antibiotics, particularly during long-term use. While tedizolid is typically prescribed for a short 6-day course, patients should report any changes in vision, such as blurring or loss of color vision, or physical sensations like tingling or numbness in the hands and feet.

Serotonin Syndrome

Tedizolid is a weak inhibitor of monoamine oxidase (MAO). Although the risk is low during the standard 6-day treatment period, there is a potential for serotonin syndrome if tedizolid is used alongside certain antidepressants or other serotonergic medications. Symptoms of serotonin syndrome may include confusion, rapid heart rate, tremors, or sweating.

Development of Drug-Resistant Bacteria

Prescribing tedizolid in the absence of a proven or strongly suspected bacterial infection is unlikely to provide benefit and increases the risk of the development of drug-resistant bacteria. It is important to complete the full course of therapy as directed by a healthcare provider.

Pregnancy

There is limited information available regarding the use of tedizolid in pregnant women. In animal studies, the medication has shown potential for developmental toxicity when administered at high doses. Because of the lack of human data, it is important to discuss the potential risks and benefits with a healthcare provider if you are pregnant or planning to become pregnant.

Breastfeeding

It is not known whether tedizolid passes into human breast milk. While studies in animals have shown that the drug can be excreted in milk, it is unclear if the same occurs in humans. If you are breastfeeding, consult your healthcare provider to determine the best course of action for you and your infant.

Dosage Forms

Tedizolid is available in the following forms:

• Oral Tablet: A solid form for administration by mouth.
• Intravenous Injection: A sterile powder for solution that is reconstituted and diluted by a healthcare professional for administration as an infusion into a vein.

FDA Approval Status

Tedizolid phosphate was approved by the U.S. Food and Drug Administration (FDA) in June 2014. It is an oxazolidinone-class antibacterial drug available in both oral tablet and intravenous injection forms.

Approved Indications

Tedizolid is FDA-approved for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of specific Gram-positive microorganisms. These include:

• Staphylococcus aureus (including methicillin-resistant [MRSA] and methicillin-susceptible [MSSA] isolates)
• Streptococcus pyogenes
• Streptococcus agalactiae
• Streptococcus anginosus group (including S. anginosus, S. intermedius, and S. constellatus)
• Enterococcus faecalis

The medication is approved for use in adults and pediatric patients 12 years of age and older.

Regulatory Requirements and Safety

The FDA requires that tedizolid be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria to maintain the drug's effectiveness and prevent the development of drug-resistant bacteria. There are no boxed warnings or Risk Evaluation and Mitigation Strategies (REMS) currently mandated for this medication.

FDA Approval Overview

The U.S. Food and Drug Administration (FDA) granted approval for tedizolid in June 2014. It is classified as an oxazolidinone antibacterial drug and is marketed under the brand name Sivextro.

Approved Indications

Tedizolid is indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible Gram-positive bacteria. The FDA approved its use for both adults and pediatric patients who are at least 12 years of age.

The approval covers infections caused by several pathogens, including:

• Staphylococcus aureus (including methicillin-resistant [MRSA] and methicillin-susceptible [MSSA] strains)
• Streptococcus pyogenes
• Streptococcus agalactiae
• Streptococcus anginosus group (including S. anginosus, S. intermedius, and S. constellatus)
• Enterococcus faecalis

Dosage Forms and Administration

The FDA has approved two administration routes for tedizolid, which may allow for a transition from hospital to home care:

• Oral Tablets: 200 mg tablets taken once daily.
• Intravenous (IV) Injection: 200 mg administered via infusion once daily.

The standard duration of treatment approved by the FDA for these infections is six days.