Torezolid Phosphate
Torezolid Phosphate Uses, Dosage, Side Effects, Food Interaction and all others data.
After conversion to its active form by phosphatases, tedizolid exerts its antibacterial activity through inhibition of protein synthesis by binding to the 50S ribosomal subunit of susceptible Gram-positive bacteria. Cross-resistance between other non-oxazolidinone antibacterial drugs is unlikely as it inhibits bacterial protein synthesis through a different mechanism.
Tedizolid is an oxazolidinone antibiotic that works by inhibiting protein synthesis by bacterial ribosomes. However, oxazolidinone antibiotics can also bind to human mitochondrial, but not cytoplasmic, ribosomes. Mitochondrial protein synthesis inhibition is associated with adverse patient effects such as neurological, hematological, and gastrointestinal toxicity, although tedizolid is tolerated better than the related linezolid. Alternative therapies should be considered when treating neutropenic patients with ABSSSI. Clostridium difficile-associated diarrhea has been reported in patients treated with tedizolid.
| Trade Name | Torezolid Phosphate |
| Generic | Tedizolid Phosphate |
| Tedizolid Phosphate Other Names | Tedizolid phosphate, Torezolid phosphate |
| Type | |
| Formula | C17H16FN6O6P |
| Weight | Average: 450.323 Monoisotopic: 450.08529742 |
| Protein binding | Approximately 70 to 90% of tedizolid is bound to human plasma proteins. |
| Groups | Approved |
| Therapeutic Class | Other antibiotic |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tedizolid is an oxazolidinone-class antibacterial drug used for adults for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Tedizolid and other antibacterial drugs, Tedizolid should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria
Torezolid Phosphate is also used to associated treatment for these conditions: Acute Bacterial Skin and Skin Structure Infection (ABSSSI)
How Torezolid Phosphate works
Despite renewed efforts to combat the spread of antimicrobial resistance, multidrug-resistant organisms, including gram-positive bacteria such as methicillin-resistant Staphylococcus aureus, remain a threat. Oxazolidinones represent a relatively new class of antibacterials inhibiting protein synthesis that is generally capable of overcoming resistance to other bacterial protein synthesis inhibitors.
Protein synthesis involves the action of ribosomes, multi-subunit complexes composed of both protein and ribosomal RNA (rRNA) substituents. Translocation along the length of a messenger RNA and concomitant protein synthesis involves the action of the A, P, and E sites of the peptidyltransferase centre (PTC), which accepts charged aminoacyl-tRNAs and catalyzes the formation of peptide bonds between them. The bacterial 70S ribosome comprises a small (30S) and a large (50S) subunit.
Early studies into the mechanism of action of oxazolidinone antibiotics suggested that they inhibit a step in the initiation of protein synthesis. However, this mechanism was inconsistent with mapped resistance mutations, and later studies involving cross-linking and direct structural determination of the binding site revealed that oxazolidinones, including both linezolid and tedizolid, bind in the A site of the PTC by interacting with the 23S rRNA component. The structural studies also revealed that oxazolidinone binding alters the conformation of a conserved nucleotide in the 23S rRNA (U2585 in Escherichia coli), which renders the PTC non-productive for peptide bond formation. Hence, tedizolid exerts its effect through inhibiting bacterial protein synthesis.
Dosage
Torezolid Phosphate dosage
Acute Bacterial Skin and Skin Structure Infection (ABSSSI):
- Intravenous: 200 mg Once daily 1 hour (Infusion Time) for6 days
- Oral: 200 mg Once daily for6 days
No dose adjustment is necessary when changing from intravenous to oral Tedizolid. If patients miss a dose, they should take it as soon as possible anytime up to 8 hours prior to their next scheduled dose. If less than 8 hours remain before the next dose, wait until their next scheduled dose.
Side Effects
The most common adverse reactions (>2%) are nausea, headache, diarrhea, vomiting, and dizziness
Toxicity
Toxicity information regarding tedizolid is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as nausea, headache, dizziness, diarrhea, and vomiting. Symptomatic and supportive measures are recommended.
Precaution
Patients with neutropenia: The safety and efficacy of Tedizolid in patients with neutropenia (neutrophil counts <1000 cells/mm3) have not been adequately evaluated. In an animal model of infection, the antibacterial activity of Tedizolid was reduced in the absence of granulocytes. Consider alternative therapies in neutropenic patients.
Clostridium difficile-associated diarrhea: Evaluate if diarrhea occurs.
Interaction
Tedizolid (when administered orally) can increase the plasma concentrations of orally administered Breast Cancer Resistance Protein BCRP substrates. Monitor for adverse reactions related to the concomitant BCRP substrates if coadministration cannot be avoided
Food Interaction
- Take at the same time every day.
- Take with or without food.
Volume of Distribution
The volume of distribution for tedizolid following a single intravenous dose of 200 mg is between 67 and 80 L. In a study involving oral administration of 200 mg tedizolid to steady-state, the volume of distribution was 108 ± 21 L, while a single 600 mg oral dose resulted in an apparent volume of distribution of 113.3 ± 19.3 L. Tedizolid has been observed to penetrate the interstitial space of both adipose and skeletal muscle tissue and is also found in the epithelial lining fluid as well as in alveolar macrophages.
Elimination Route
Tedizolid reaches peak plasma concentrations within three hours for oral administration and within one hour following intravenous administration; the absolute oral bioavailability is approximately 91%. Food has no effect on absorption. When given once daily, either orally or intravenously, tedizolid reaches steady-state concentrations in approximately three days.
The Cmax for tedizolid after a single dose/at steady-state is 2.0 ± 0.7/2.2 ± 0.6 mcg/mL for oral administration, and 2.3 ± 0.6/3.0 ± 0.7 mcg/mL for intravenous administration, respectively. Similarly, the Tmax has a median (range) of 2.5 (1.0 - 8.0)/3.5 (1.0 - 6.0) hrs for the oral route and 1.1 (0.9 - 1.5)/1.2 (0.9 - 1.5) hrs when given intravenous. The AUC is 23.8 ± 6.8/25.6 ± 8.4 mcg*hr/mL for oral and 26.6 ± 5.2/29.2 ± 6.2 mcg*hr/mL for intravenous.
Half Life
Tedizolid has a half-life of approximately 12 hours.
Clearance
Tedizolid has an apparent oral clearance of 6.9 ± 1.7 L/hr for a single dose and 8.4 ± 2.1 L/hr at steady-state. The systemic clearance is 6.4 ± 1.2 L/hr for a single dose and 5.9 ± 1.4 L/hr at steady-state.
Elimination Route
When given as a single oral dose, approximately 82% of tedizolid is excreted via the feces and 18% in urine. The majority is found as the inactive sulphate conjugate, with only 3% recovered unchanged. Over 85% of the elimination occurs within 96 hours.
Pregnancy & Breastfeeding use
Pregnancy category C. There are no adequate and well-controlled studies of Tedizolid in pregnant women. Tedizolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers: Tedizolid is excreted in the breast milk of rats. It is not known whether tedizolid is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Tedizolid is administered to a nursing woman.
Contraindication
None
Special Warning
Pediatric Use: Safety and effectiveness in pediatric patients below the age of 18 have not been established.
Geriatric Use: Clinical studies of Tedizolid did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. No overall differences in pharmacokinetics were observed between elderly subjects and younger subjects
Acute Overdose
In the event of overdosage, Tedizolid should be discontinued and general supportive treatment given. Hemodialysis does not result in meaningful removal of tedizolid from systemic circulation
Storage Condition
Tablets and injection should be stored at 20°C to 25°C
Innovators Monograph
You find simplified version here Torezolid Phosphate
Torezolid Phosphate contains Tedizolid Phosphate see full prescribing information from innovator Torezolid Phosphate Monograph, Torezolid Phosphate MSDS, Torezolid Phosphate FDA label
FAQ
What is Torezolid Phosphate used for?
Torezolid Phosphate is used to treat skin infections caused by certain types of bacteria in adults and children 12 years of age and older. Torezolid Phosphate is in a class of medications called oxazolidinone antibiotics. It works by stopping the growth of bacteria.
How safe Torezolid Phosphate is?
Clinical safety and tolerability of Torezolid Phosphate in the treatment of acute bacterial skin and skin structure infections.
What are the common side effects of Torezolid Phosphate?
Common side effects may include:
- nausea, vomiting, diarrhea;
- headache;
- dizziness; or.
- pain, swelling, bruising, redness, or a hard lump where a tedizolid injection was given.
How long for Torezolid Phosphate to work?
Concentrations are achieved within approximately 3 hours following oral administration under fasting conditions or at the end of the 1 hour intravenous infusion of Torezolid Phosphate.
Is Torezolid Phosphate safe during pregnancy?
Torezolid Phosphate should only be used during pregnancy if the benefit justifies the potential risk to the fetus. Torezolid Phosphate is known to produce fetal developmental toxicities in animal models.
Is Torezolid Phosphate safe during breastfeeding?
It is not known whether Torezolid Phosphate is excreted in human milk. Torezolid Phosphate is excreted in the milk of lactating rats; therefore, caution should be exercised when Torezolid Phosphate is administered to a breast-feeding woman.
Can I drink alcohol with Torezolid Phosphate?
You should avoid alcoholic beverages while taking Torezolid Phosphate. Side effects may get worse if you take Alcoholic beverages or medicines containing a significant amount of Alcohol.
Can I take Torezolid Phosphate for a long time?
The safety and efficacy of Torezolid Phosphate when administered for periods longer than 6 days have not been established.
How is Torezolid Phosphate eliminated?
Hepatic excretion via bile accounts for the majority of Torezolid Phosphate elimination 80% of the administered dose is eliminated in feces, primarily as a sulfate conjugate.
What are the indications of Torezolid Phosphate?
Torezolid Phosphate is indicated for the treatment of acute bacterial infections of the skin and skin structure . To prevent drug resistance, Torezolid Phosphate should only be used for infections that are caused by susceptible bacteria.
How does Torezolid Phosphate administered?
Torezolid Phosphate is a white to yellow solid and is administered orally or by intravenous infusion.
Can I take overdosage of Torezolid Phosphate?
In the event of Torezolid Phosphate should be discontinued and general supportive treatment given. Hemodialysis does not result in meaningful removal of Torezolid Phosphate from systemic circulation.
