Tedizolid Phosphate: Empowering Skin Health Against Bacterial Onslaughts

Overview

Tedizolid phosphate is an antibiotic predominantly utilized to treat skin infections induced by specific types of bacteria in humans aged 12 and above. It functions by inhibiting the proliferation of microorganisms. It is important to remember that cold, flu and other viral infections cannot be treated with Tedizolid phosphate. The probability of acquiring illnesses in the future that are resistant to antibiotic therapy can be increased by the misuse or overuse of antibiotics. Therefore, it is important to utilize antibiotics carefully. Tedizolid phosphate received the United States Food and Drug Administration approval in 2014.

Drug Group:

Tedizolid phosphate belongs to a group of drugs known as oxazolidinone.

Indications:

The antibiotic Tedizolid phosphate is a member of the oxazolidinone class. It is used to treat certain skin infections brought on by particular bacteria. Acute bacterial skin and skin structure infections (ABSSSI) are the name given to bacterial infections treated with Tedizolid phosphate. Certain gram-positive bacteria, such as Enterococcus faecalis, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus group (which includes Streptococcus anginosus, Streptococcus intermedius, and Streptococcus constellatus), and Methicillin-resistant (MRSA) and Methicillin-susceptible (MSSA) types of Staphylococcus aureus can all be treated with Tedizolid phosphate.

Contraindications:

None.

Dosage Forms and Available Strengths:

There are two dosage options for Tedizolid phosphate: a tablet and an injectable form. The tablet is oval in shape and yellow, with the numbers "TZD" and "200" on opposite sides. The injection is prepared by combining the white to off-white powder with sterile water. Before being injected, it is combined and then diluted with a certain kind of saline solution.

For Patients:

What Is ABSSSI (Acute Bacterial Skin and Skin Structure Infections)?

A bacterial infection that affects the skin and its surrounding tissues is referred to as a skin and skin structure infection (SSSI), and it frequently requires antibiotic therapy. It is classified into complicated and uncomplicated categories.

The U.S. Food and Drug Administration (FDA) defines simple serous abscesses, spontaneous lesions, furuncles (pus-filled, painful lump beneath the skin that is the result of inflamed, infected hair follicles), and cellulitis (bacterial skin infection that results in discomfort, swelling, and redness in the affected area) primarily caused by Staphylococcus aureus and Streptococcus pyogenes as uncomplicated SSSI. On the other hand, complex SSSI refers to infections that require extensive surgical intervention or penetrate deeper soft tissue. These infections can include severe abscesses, burns, infected ulcers, or underlying conditions that impede the effectiveness of treatment. Complicated infections also include superficial infections or abscesses in anatomical locations such as the rectal area that have a higher probability of involvement from anaerobic or gram-negative pathogens.

The USFDA has been referring to these infections as acute bacterial skin and skin structure infections (ABSSSI) since 2008.

How Does Tedizolid Work?

Tedizolid phosphate inhibits the synthesis of proteins in bacteria, just like other oxazolidinones. Tedizolid phosphate binds to the 23S ribosomal ribonucleic acid (rRNA), which is found inside the 50S subunit of the ribosome (responsible for protein synthesis to cause this inhibition. Similar to other drugs in the oxazolidinone class, Tedizolid phosphate exhibits a low rate of spontaneous resistance development.

What Are the Clinical Uses of Tedizolid Phosphate?

Tedizolid phosphate is a drug used to treat skin infections in adults and children 12 years of age and older that are brought on by specific types of bacteria. It is a member of the oxazolidinone antibiotics class of drugs. It functions by halting bacterial growth. For viral illnesses such as colds and the flu, antibiotics like Tedizolid phosphate are ineffective. The chance of developing an infection later on that is resistant to antibiotic treatment rises when antibiotics are used unnecessarily.

How Should Tedizolid Phosphate Be Used?

• Tedizolid phosphate is supplied as a tablet for oral use. Typically, it is taken once daily for six days, with or without food. Tedizolid phosphate must be taken at the same time every day to be effective.

• Patients should carefully adhere to the directions on their prescription label and ask their doctor or pharmacist for clarification if they have any questions. Patients should take Tedizolid phosphate exactly as directed. They should not increase or decrease the dosage, and they should not take it more frequently than recommended.

• Patients on Tedizolid phosphate therapy should anticipate feeling better within the first few days of treatment. But it is best to get in touch with a medical expert right once if symptoms intensify or continue.

• Taking Tedizolid phosphate as directed for the whole prescribed duration is important, even if symptoms subside. Patients should never miss doses or stop taking Tedizolid phosphate abruptly. This is because failing to take the drug as prescribed could lead to an infection that is not fully treated, which could create bacteria that are resistant to antibiotics.

What Are the Side Effects of Tedizolid Phosphate?

Side effects from Tedizolid phosphate are possible, and patients should contact their doctor right once if any of the below-mentioned symptoms worsen or continue:

• Headaches, or dizziness.

• Diarrhea (watery stool).

• Vomiting and nausea.

Tedizolid phosphate can have serious adverse effects that call for emergency medical intervention. The patient must contact the doctor right away if they encounter any of the following symptoms:

• Simple bruises or bleeding (such as nosebleeds, gum bleeding, cuts that bleed for a long time, or blood in the stools or urine).

• Tingling, burning, numbness, or pain in feet or hands.

• Severe diarrhea (bloody or watery stools) could happen up to two months or longer even after the treatment. Fever and stomach cramps may or may not accompany it.

• Loss or change in vision.

What Are the Things to Inform the Doctor Before Taking Tedizolid Phosphate?

• Patients should disclose any allergies, especially to Tedizolid phosphate, other drugs, or any ingredients in Tedizolid phosphate tablets, to their pharmacist and healthcare practitioner before starting Tedizolid phosphate treatment. If needed, patients can ask their pharmacist for an extensive list of ingredients.

• All current prescription and over-the-counter drugs, along with any vitamins, supplements, or herbal products taken or intended to be used, must be disclosed. While taking Tedizolid phosphate with other drugs, such as Methotrexate, Rosuvastatin, and Topotecan, dosage changes or careful monitoring for possible adverse effects may be required. Hence drug history becomes vital.

• Any history of low white blood cell count should be disclosed by the patient to their physician.

• It is crucial to talk to the healthcare professional about pregnancy, plans for pregnancy, or breastfeeding. Patients should contact their doctor right away for additional advice if they become pregnant while taking Tedizolid phosphate.

Dietary Consideration: Patients should stick to their regular diet unless their doctor instructs them otherwise.

Storage: Make sure the drug is securely closed, stored out of children's reach, and kept in its original container. Keep it out of the bathroom and at room temperature, away from light, extreme heat, and moisture.

Disposal: It is important to appropriately dispose of unused drugs to avoid pet or child ingestion. Medication should not be flushed down the toilet. Instead, it should be returned using a medication take-back program, or speak with the pharmacist or waste and recycling department about other disposal choices. All prescriptions must be kept out of the reach and sight of children. Use child-resistant containers and store them in a secure location.

Missed Dose: The patient should take the missed dose as soon as they remember it and take their next dose at the scheduled time if they remember more than eight hours before their next planned dose. On the other hand, skip the missed dose and stick to the usual dosing plan if they remember less than eight hours before their next scheduled dose. Never take two doses to make up for the missed one.

Overdose: It is critical to contact emergency medical services if the person has passed out, had a seizure, is having trouble breathing, or cannot be awakened. These signs may point to a significant medical issue that needs to be treated right now.

For Doctors

Pharmacodynamics: The most accurate indicator of Tedizolid phosphate’s efficacy in animal research was shown to be the AUC (area under the curve) or minimum inhibitory concentration (MIC) ratio. In humans, a dose of approximately 2000 mg/day (milligrams per day) was required to inhibit bacterial growth when these cells were low (neutrophil count less than 100 cells/mL - cells per milliliter). Nevertheless, there is no research done on Tedizolid phosphate’s efficacy or safety in treating people with neutropenia, or low neutrophil counts. Tedizolid phosphate at both the standard dosage of 200 mg (milligrams) and the higher dose of 1200 mg had no discernible impact on heart rate or cardiac electrical activity in investigations on heart rhythm that involved 48 subjects. This indicates that Tedizolid phosphate does not affect the heart's regular beat.

Mechanism of Action: Tedizolid phosphate is a class of medication that, when taken internally, transforms into the antibacterial drug Tedizolid. Tedizolid binds to the 50S subunit of the ribosome, which is a component of bacteria and acts as an antibiotic. The bacteria are unable to produce the proteins necessary for growth and survival as a result of this adhesion. Since Tedizolid functions differently from other antibiotic classes, bacteria resistant to other classes of antibiotics are unlikely to be resistant to Tedizolid. Tedizolid has been demonstrated in laboratory experiments to inhibit the growth of some bacteria, including enterococci, staphylococci, and streptococci. This means that while it stops these bacteria from growing, it does not kill them.

Pharmacokinetics: After being administered orally or intravenously, Tedizolid phosphate, the prodrug, transforms into Tedizolid which is the active component. After multiple once-daily dosages, steady-state concentrations are reached in about three days, and the half-life of Tedizolid is about twelve hours. Tedizolid accumulation is around thirty percent.

• Absorption: After oral administration of Tedizolid phosphate under fasting conditions, or after a one-hour intravenous infusion, peak plasma Tedizolid concentrations are reached in approximately three hours. Since the absolute bioavailability is 91 percent, there is no need to change the dosage for oral and intravenous administration. Oral Tedizolid phosphate can be administered with or without meals because there is no difference in total systemic exposure between feeding (high-fat, high-calorie) and fasting conditions.

• Distribution: Tedizolid is distributed throughout the body, including adipose and skeletal muscle tissue, mostly binding to human plasma proteins (between 70 and 90 percent).

• Metabolism: There are no substantial circulating metabolites in humans, except Tedizolid, which makes up roughly 95 percent of the total radiocarbon AUC in plasma. Since Tedizolid did not degrade in human liver microsomes, it seems doubtful that Tedizolid is a substrate for hepatic CYP450 enzymes.

• Excretion: The liver is primarily responsible for the removal of Tedizolid phosphate after a single oral injection given during a fasting state. Feces and urine contain 82 percent and 18 percent of the dose, respectively. Most Tedizolid removal (greater than 85 percent) occurs in 96 hours. The amount of Tedizolid phosphate that is eliminated undisturbed in urine and feces is below three percent.

• Specific Populations: According to population pharmacokinetic studies, the pharmacokinetics of Tedizolid are not affected by any clinically significant demographic or patient characteristics, such as age, gender, race, ethnicity, weight, body mass index, or measurements of liver or kidney function.

• Drug Interaction Studies: Tedizolid does neither induce nor inhibit CYP enzymes nor does it appreciably alter the metabolism of certain CYP enzyme substrates. Furthermore, it has no clinically meaningful impact on crucial drug transporters. Although Tedizolid is a reversible monoamine oxidase inhibitor in vitro, clinical trials did not assess the drug's interaction with MAO inhibitors. Its potential interactions with serotonergic and adrenergic drugs are unknown, but they may have therapeutic implications.

What Is the Prescribed Dosage and Method of Administration For Tedizolid Phosphate?

• Recommended Dosage: For patients 18 years of age or older, an intravenous (IV) infusion or an oral dose of 200 mg given once a day for six days is the recommended dosage of Tedizolid phosphate.

• Intravenous Solution Preparation and Administration:

  • Tedizolid phosphate is provided in 200 mg single-use vials as a sterile, lyophilized powder for injection. Sterile water for injection must be used to reconstitute each 200 mg vial, and only 0.9 percent sodium chloride Injection, USP should be used for diluting after that.

  • Tedizolid phosphate vials are designed for single use only and do not include any antimicrobial preservatives.

• Compatible Intravenous Solutions: Tedizolid phosphate is suitable for use with USP 0.9 percent sodium chloride Injection.

• Incompatibilities:

  • Any solution containing divalent cations, such as Ca2+ or Mg2+, is incompatible with Tedizolid phosphate for injection; this includes Hartmann's Solution and Lactated Ringer's injection.

  • There is not much information on how well Tedizolid phosphate works with other intravenous drugs, additives, or prescriptions, so it is best to avoid adding them to Tedizolid phosphate single-use vials or infusing them at the same time. When administering multiple medicines sequentially through the same intravenous line, it is recommended to cleanse the line both before and following the infusion of Tedizolid phosphate with 0.9 percent sodium chloride injection, USP.

Drug Interactions:

• Monoamine Oxidase Inhibition: In lab studies, the active component of Tedizolid phosphate, Tedizolid, has been shown to momentarily suppress a particular enzyme known as monoamine oxidase (MAO). However, because those on MAO-affecting medications were excluded from the trials, its possible interactions with those drugs could not be assessed.

• Adrenergic Agents: Adrenergic agents affect blood pressure and heart rate. Clinical investigations evaluated Tedizolid phosphate’s potential interactions with these agents. When participants used Tedizolid phosphate together with some adrenergic drugs, no appreciable changes in heart rate or blood pressure were seen; however, some experienced palpitations.

• Serotonergic Drugs: Tedizolid showed no discernible effects on serotonergic drugs, which affect serotonin levels in the brain, in animal research or clinical trials, even at doses far greater than those used in humans. To reduce the possibility of interactions, participants on such medications were not allowed to participate in the trials.

Clinical Studies: The studies, which involved 1315 individuals, showed that for treating acute bacterial skin and skin structure infections (ABSSSI), Tedizolid phosphate 200 mg once daily for six days was just as effective as Linezolid 600 mg every 12 hours for ten days. Compared to patients treated with Linezolid, patients treated with Tedizolid phosphate had higher response rates across all age categories, good clinical responses, and the resolution or near-resolution of infection-related signs and symptoms. Tedizolid phosphate showed efficacy against several bacteria, such as Streptococcus species and Staphylococcus aureus, frequently linked to ABSSSI. Furthermore, Tedizolid phosphate was generally well-tolerated by patients in both studies, and no significant safety issues were reported.

Warnings and Precautions:

• Neutropenia Patients: Patients with very low numbers of neutrophils, a type of white blood cell, have not been adequately researched about Tedizolid phosphate, a medicine used to treat specific bacterial infections. When these white blood cells were lacking, Tedizolid phosphate did not function as well in animal tests. Therefore, while treating patients with specific skin infections who have low neutrophil counts, physicians should think about other options.

• Clostridium Difficile-Associated Diarrhea (CDAD): Following the use of certain antibiotics, such as Tedizolid phosphate, diarrhea due to Clostridium difficile (CDA) can range in severity from moderate to severe. Antibiotics can upset the normal bacterial balance in the stomach, which permits C. difficile to proliferate and create toxins that result in diarrhea. Even if diarrhea occurs months after taking antibiotics, doctors still need to be aware of CDAD while treating patients with diarrhea. Doctors should think about halting medications that are ineffective against C. difficile if they detect CDAD. Managing fluids and electrolytes, giving certain proteins, using antibiotics that target C. difficile, and maybe surgery are all possible treatments for CDAD.

• Development of Drug-Resistant Bacteria: Patients may not benefit from the use of Tedizolid phosphate when it is not required or for preventative measures, and it may even cause bacteria to develop resistance to the medication. This implies that when the drug is required to treat bacterial infections in the future, it could not function as well. As a result, medical professionals must utilize Tedizolid phosphate sparingly and only in cases of confirmed or highly suspected bacterial infection.

Use in Specific Populations:

• Pregnancy: Given its classification as pregnancy category C, Tedizolid phosphate’s effects during pregnancy are not well understood. It is only advised when the mother's advantages outweigh any possible risks to the developing fetus. Even at the highest tested dose, Tedizolid phosphate treatment of mothers throughout pregnancy and lactation did not cause any negative effects in trials conducted on rats. However, when considering the usage of Tedizolid phosphate during pregnancy, caution is suggested.

• Nursing Mothers: It is unknown if Tedizolid finds its way into human breast milk, despite its presence in rat milk. To prevent drug transfer, care should be used when giving Tedizolid phosphate to nursing moms.

• Use in Pediatrics: The effectiveness and safety of Tedizolid phosphate in children under the age of 18 have not been shown. As a result, unless more research is done, using it in this age group is not advised.

• Use in Geriatrics: There were not enough senior participants in Tedizolid phosphate studies to ascertain whether their responses differed from those of younger persons. Nonetheless, there were no appreciable variations in drug use between younger and older people.