Sivextro (Tedizolid) - Uses, Dose, Side effects

By interfering with the bacterial ribosomal subunits and preventing bacterial replication, the drug tedizolid (Sivextro) prevents bacterial protein production.

Tedizolid (Sivextro) Uses:

  • Skin and skin structure infections:

    • It is prescribed for the management of acute bacterial skin and soft tissue infections brought on by pathogens that respond well to the medication.
    • It can be used to treat the following susceptible gram-positive organisms:
      • Staphylococcus aureus (including MRSA and MSSA (methicillin-resistant and methicillin-susceptible) isolates,
      • Streptococcus pyogenes,
      • Streptococcus agalactiae,
      • Streptococcus anginosus group (including Streptococcus anginosus, Streptococcus intermedius, and Streptococcus constellatus), and
      • Enterococcus faecalis

Tedizolid (Sivextro) dose in Adults

Tedizolid (Sivextro) dose for treating Skin and skin structure infections:

  • 200 mg orally or intravenously once a day for 6 days.
  • If a dose is missed:

    • It needs to be given as soon as feasible (and up to 8 hours before the next scheduled dose).
    • If less than 8 hours remain before the next scheduled dose, the dose should be given at the scheduled time.

Tedizolid (Sivextro) use in children

Tedizolid's effectiveness and safety in youngsters have not been determined.

Pregnancy Risk Factor C

  • Studies on animal reproduction have shown negative outcomes for fetuses.It has not been tested in human pregnancies.

Tedizolid use during breastfeeding:

  • It is unknown if the drug will be excreted into breastmilk.
  • Manufacturers recommend weighing the benefits and risks of drug exposure for the infant, as well as treating the mother.

Tedizolid dose in kidney disease.

Adjustment in the dosage is not necessary in patients with renal disease.

Tedizolid dose in liver disease:

Adjustment in the dosage is not necessary in patients with liver disease.

Side Effects of Tedizolid (Sivextro):

  • Cardiovascular:

    • Flushing
    • Hypertension
    • Palpitations
    • Tachycardia
  • Central Nervous System:

    • Headache
    • Dizziness
    • Facial Nerve Paralysis
    • Hypoesthesia
    • Insomnia
    • Paresthesia
    • Peripheral Neuropathy
  • Dermatologic:

    • Dermatitis
    • Pruritus
    • Urticaria
  • Endocrine & Metabolic:

    • Increased Gamma-Glutamyl Transferase
  • Gastrointestinal:

    • Nausea
    • Diarrhea
    • Vomiting
    • Clostridioides Difficile Colitis
    • Oral Candidiasis
  • Hematologic & Oncologic:

    • Decreased Hemoglobin
    • Decreased Platelet Count
    • Anemia
    • Decreased White Blood Cell Count
  • Hepatic:

    • Increased Serum Alanine Aminotransferase
    • Increased Serum Aspartate Transaminase
    • Increased Serum Transaminases
  • Hypersensitivity:

    • Hypersensitivity
  • Infection:

    • Fungal Infection
  • Local:

    • Injection Site Reaction
  • Ophthalmic:

    • Asthenopia
    • Blurred Vision
    • Visual Impairment
    • Vitreous Opacity
  • Miscellaneous:

    • Infusion Related Reaction

Contraindication to Tedizolid (Sivextro):

The manufacturer's labeling does not contain any contraindications.

Warnings and precautions

  • Superinfection
    • Long-term antibiotic use can result in superinfections with fungus or bacteria that are resistant, such as diarrhoea linked to C. difficile.
    • C. difficile-associated diarrhoea and pseudomembranous colitis were documented two months after the end of antibiotic therapy.
  • Neutropenia:
    • Patients with a baseline neutrophil count less than 1000 cells/mm should avoid it.
    • Alternative treatment options may be available for these patients.

Tedizolid: Drug Interaction

Risk Factor C (Monitor therapy)

Amifampridine

Amifampridine may have a stronger neuroexcitatory and/or seizure-potentiating impact when combined with substances with seizure threshold lowering potential.

Antiemetics (5HT3 Antagonists)

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Antipsychotic Agents

Serotonin modulators might make antipsychotic drugs more harmful or toxic. Serotonin modulators, in particular, may enhance dopamine blockade, potentially raising the risk for neuroleptic malignant syndrome. Serotonin modulators' serotonergic effects may be strengthened by antipsychotic drugs. Serotonin syndrome might occur from this.

BCG Vaccine (Immunization)

Antibiotics may reduce the BCG vaccine's therapeutic effect (Immunization).

BCRP/ABCG2 Substrates

The serum concentration of BCRP/ABCG2 Substrates may rise after using tedizolid.

Betahistine

The serum concentration of betahistine may rise in response to monoamine oxidase inhibitors.

Blood Glucose Lowering Agents

Blood Glucose Lowering Agents' hypoglycemic effects may be strengthened by monoamine oxidase inhibitors.

Brimonidine (Ophthalmic)

Monoamine Oxidase Inhibitors might make brimonidine more harmful or poisonous (Ophthalmic). Brimonidine serum levels may rise in response to monoamine oxidase inhibitors (Ophthalmic).

Brimonidine (Topical)

Monoamine Oxidase Inhibitors might make brimonidine more harmful or poisonous (Topical). Brimonidine serum levels may rise in response to monoamine oxidase inhibitors (Topical).

Cerebrolysin

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Chloramphenicol (Ophthalmic)

Myelosuppressive Agents' poisonous or harmful effects might be amplified.

Chlorphenesin Carbamate

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

CloZAPine

Myelosuppressive drugs may make CloZAPine's harmful or toxic effects worse. Particularly, there may be a higher chance of neutropenia.

Codeine

Monoamine Oxidase Inhibitors might make codeine more harmful or poisonous.

Dihydrocodeine

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Domperidone

Monoamine Oxidase Inhibitors may intensify Domperidone's negative/toxic effects. Monoamine Oxidase Inhibitors may lessen Domperidone's therapeutic efficacy. Monoamine Oxidase Inhibitors' therapeutic effects may be lessened by dolperidone.

EPINEPHrine (Systemic)

Epinephrine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Systemic).

Esketamine

The hypertensive effects of monoamine oxidase inhibitors might be enhanced.

Lactobacillus and Estriol

The therapeutic effects of Lactobacillus and Estriol may be reduced by antibiotics.

Mesalamine

Could make myelosuppressive agents more effective at suppressing myeloid growth.

Metaraminol

Metaraminol's hypertensive effect may be strengthened by monoamine oxidase inhibitors.

Metaxalone

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Methadone

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Metoclopramide

Serotonin modulators may intensify Metoclopramide's harmful or hazardous effects. This could appear as signs of neuroleptic malignant syndrome or serotonin syndrome.

Opioid Agonists

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Promazine

Could make myelosuppressive agents more effective at suppressing myeloid growth.

Serotonin Modulators

Tedizolid might make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this. The exception is nigroline.

Sympathomimetics

The hypertensive effects of sympathomimetics may be increased by tedizolid. The tachycardic impact of sympathomimetics may be increased by tedizolid.

Talazoparib

Talazoparib's serum levels may rise in response to BCRP/ABCG2 inhibitors.

TraMADol

Serotonin modulators may intensify TraMADol's harmful or hazardous effects. Seizures may become more likely. The serotonergic impact of serotonin modulators may be enhanced by TraMADol. Serotonin syndrome might occur from this.

Risk Factor D (Consider therapy modification)

Alpelisib

Alpelisib's serum levels may rise in response to BCRP/ABCG2 inhibitors. Management: Due to the possibility of elevated alpelisib concentrations and toxicities, avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib. If coadministration is unavoidable, keep a watchful eye out for any elevated alpelisib side effects.

Benzhydrocodone

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this. Treatment: Patients on monoamine oxidase inhibitors (MAOIs) or those who have stopped taking MAOIs within 14 days shouldn't use benzhydrocodone.

COMT Inhibitors

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Deferiprone

Myelosuppressive drugs may make Deferiprone's neutropenic effect stronger. Management: Whenever feasible, refrain from using deferiprone and myelosuppressive medications concurrently. Increased attention should be paid to the absolute neutrophil count if this combination cannot be avoided.

DOPamine

DOPamine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors. Treatment: Patients who are taking (or have recently taken) monoamine oxidase inhibitors should start dopamine at no more than one-tenth (1/10) of the typical dose. 

HYDROcodone

Monoamine Oxidase Inhibitors may intensify Hydrocodone's harmful or hazardous effects. Management: When possible, look into alternatives to this pairing.

Iohexol

The negative/toxic effects of iohexol may be amplified by substances with the potential to lower seizure thresholds. More specifically, there may be a higher chance of seizures. Treatment: Stop using medications 48 hours before using intrathecal iohexol that could lower the seizure threshold. To restart using such agents, give the treatment at least 24 hours. Prophylactic anticonvulsants may be used in nonelective surgeries.

Iomeprol

The negative/toxic effect of Iomeprol may be increased by substances with the potential to lower seizure thresholds. More specifically, there may be a higher chance of seizures. Treatment: Stop using medications 48 hours before using intrathecal iomeprol if they could lower the seizure threshold

Iopamidol

The negative/toxic effects of iopamidol may be increased by substances with the potential to lower seizure thresholds. More specifically, there may be a higher chance of seizures. Treatment: 48 hours before using intrathecal iopamidol, stop using any medications that could lower the seizure threshold. To restart using such agents, give the treatment at least 24 hours. Prophylactic anticonvulsants may be used in nonelective surgeries.

Levodopa-Containing Products

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. The emergence of hypertensive responses when levodopa is combined with nonselective MAOI is of special concern. Treatment: It is not advised to take levodopa and nonselective MAO inhibitors (MAOIs) together. Levodopa should be started at least two weeks after stopping the nonselective MAOI. Observe patients who are on levodopa with a selective MAOI.

Lithium

Monoamine Oxidase Inhibitors might make lithium's harmful/toxic effects worse. Management: Use extreme caution when using this combo. When combination treatment is therapeutically necessary, keep a vigilant eye out for any symptoms of serotonin syndrome or toxicity.

OxyCODONE

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this. Management: When possible, look for alternatives. Use of oxycodone/naltrexone should be avoided during and for 14 days following monoamine oxidase inhibitor therapy. Some oxycodone products' non-US labels suggest that such use is not advised.

Pindolol

Pindolol's hypotensive impact may be strengthened by monoamine oxidase inhibitors. Management: Pindolol's Canadian labelling warns against using a monoamine oxidase inhibitor at the same time.

Reserpine

Monoamine Oxidase Inhibitors may intensify Reserpine's harmful or hazardous effects. Adding reserpine to current MAOI medication may have paradoxical effects (e.g., excitation, hypertension). Treatment: When a patient is concurrently getting reserpine, monoamine oxidase inhibitors (MAOIs) should be avoided or used very cautiously.

Sodium Picosulfate

Antibiotics may reduce Sodium Picosulfate's therapeutic impact. Management: If a patient previously used or is currently using an antibiotic, think about utilising an alternative product for bowel cleansing prior to a colonoscopy.

Typhoid Vaccine

The Typhoid Vaccine's therapeutic benefits may be reduced by antibiotics. The only strain impacted is the live attenuated Ty21a strain. Treatment: Patients receiving systemic antibacterial drugs should refrain from receiving the live attenuated typhoid vaccination (Ty21a). 

Risk Factor X (Avoid combination)

Alcohol (Ethyl)

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Apraclonidine

Monoamine Oxidase Inhibitors might make acrolonidine more harmful or poisonous. The concentration of araclonidine in the serum may rise after using monoamine oxidase inhibitors.

AtoMOXetine

Monoamine Oxidase Inhibitors may intensify AtoMOXetine's neurotoxic (central) impact.

Atropine (Ophthalmic)

Atropine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Ophthalmic).

BCG (Intravesical)

Antibiotics may lessen BCG's therapeutic effects (Intravesical).

BCG (Intravesical)

The therapeutic benefit of BCG may be diminished by myelosuppressive agents (Intravesical).

Bezafibrate

Monoamine Oxidase Inhibitors may intensify Bezafibrate's harmful or hazardous effects.

Buprenorphine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

BuPROPion

BuPROPion's ability to raise blood pressure may be enhanced by monoamine oxidase inhibitors.

BusPIRone

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. Increases in blood pressure have specifically been recorded.

CarBAMazepine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. Management: Refrain from using carbamazepine concurrently with monoamine oxidase inhibitor therapy or within 14 days of stopping it.

Cholera Vaccine

The therapeutic benefit of the cholera vaccine may be reduced by antibiotic use. Management: Cholera vaccine should not be administered to individuals taking systemic antibiotics or within 14 days after taking oral or parenteral antibiotics.

Cladribine

Could make myelosuppressive agents more effective at suppressing myeloid growth.

Cyclobenzaprine

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Cyproheptadine

Monoamine oxidase inhibitors may boost Cyproheptadine's anticholinergic effects. The serotonergic impact of monoamine oxidase inhibitors may be lessened by cyproheptadine.

Dapoxetine

Serotonin modulators' harmful or toxic effects could be exacerbated.

Deutetrabenazine

Monoamine Oxidase Inhibitors may make deutetrabenazine's harmful or hazardous effects worse.

Dextromethorphan

Monoamine oxidase inhibitors might improve dextromethorphan's serotonergic effects. It might result in serotonin syndrome.

Diethylpropion

Diethylpropion may have a stronger hypertensive effect when used with monoamine oxidase inhibitors.

Diphenoxylate

The hypertensive effects of monoamine oxidase inhibitors might be enhanced.

Dipyrone

Myelosuppressive Agents' poisonous or harmful effects might be amplified. Particularly, there may be an elevated risk for agranulocytosis and pancytopenia.

Droxidopa

Droxidopa's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors.

EPINEPHrine (Oral Inhalation)

Epinephrine's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors (Oral Inhalation).

FentaNYL

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Guanethidine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Heroin

Monoamine Oxidase Inhibitors might make heroin more harmful or poisonous.

HYDROmorphone

Monoamine Oxidase Inhibitors may intensify HYDROmorphone's harmful or hazardous effects.

Indoramin

Indoramin's hypotensive impact may be strengthened by monoamine oxidase inhibitors.

Iobenguane Radiopharmaceutical Products

Iobenguane radiopharmaceutical products' therapeutic effects may be reduced by monoamine oxidase inhibitors. Treatment: Before administering iobenguane, stop taking any medications that could impede or interfere with catecholamine transport or uptake for at least five biological half-lives. After each dose of iobenguane, wait at least 7 days before administering these medications.

Isometheptene

Monoamine Oxidase Inhibitors might make isotheptene more harmful or poisonous.

Levomethadone

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Levonordefrin

Levonordefrin's ability to increase blood pressure may be enhanced by monoamine oxidase inhibitors.

Linezolid

Monoamine Oxidase Inhibitors may intensify Linezolid's negative/toxic effects.

Maprotiline

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Meperidine

Meperidine's serotonergic action may be enhanced by monoamine oxidase inhibitors. It might result in serotonin syndrome.

Meptazinol

Monoamine Oxidase Inhibitors may intensify Meptazinol's harmful or hazardous effects.

Mequitazine

Mequitazine's anticholinergic effects may be enhanced by monoamine oxidase inhibitors.

Methyldopa

Monoamine Oxidase Inhibitors may intensify Methyldopa's harmful or hazardous effects.

Methylene Blue

Methylene Blue may have a stronger serotonergic impact when taken with monoamine oxidase inhibitors. Serotonin syndrome might occur from this.

Methylene Blue

Could make serotonin modulators' serotonergic effects stronger. Serotonin syndrome might occur from this.

Methylphenidate

Methylphenidate's ability to raise blood pressure may be enhanced by monoamine oxidase inhibitors.

Mianserin

The neurotoxic effect of Mianserin may be increased by monoamine oxidase inhibitors.

Moclobemide

Monoamine Oxidase Inhibitors may intensify Moclobemide's harmful or hazardous effects.

Monoamine Oxidase Inhibitors

Some monoamine oxidase inhibitors have the potential to increase their hypertensive effects. Other monoamine oxidase inhibitors' serotonergic effects may be enhanced by monoamine oxidase inhibitors. Serotonin syndrome might occur from this.

Morphine (Systemic)

Monoamine Oxidase Inhibitors might make morphine more harmful or poisonous (Systemic).

Nefopam

Monoamine Oxidase Inhibitors may intensify Nefopam's harmful or hazardous effects.

Opium

Monoamine Oxidase Inhibitors might make opium more harmful or poisonous.

OxyMORphone

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

PAZOPanib

The serum concentration of PAZOPanib may rise in response to BCRP/ABCG2 Inhibitors.

Pheniramine

Monoamine oxidase inhibitors' anticholinergic effects might be strengthened.

Pholcodine

The serotonergic effects of monoamine oxidase inhibitors may be enhanced. Serotonin syndrome might occur from this.

Pizotifen

Monoamine Oxidase Inhibitors may strengthen Pizotifen's anticholinergic effects.

Reboxetine

Monoamine Oxidase Inhibitors may intensify Reboxetine's harmful or hazardous effects.

Serotonin 5-HT1D Receptor Agonists

Serotonin 5-HT1D Receptor Agonists' metabolism may be slowed down by monoamine oxidase inhibitors. Management: Naratriptan, eletriptan, or frovatriptan may be suitable 5-HT1D agonists to use if MAO inhibitor medication is necessary. Eletriptan, Frovatriptan, and Naratriptan are exceptions.

Solriamfetol

Solriamfetol's ability to raise blood pressure may be enhanced by monoamine oxidase inhibitors.

SUFentanil

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. Particularly, there may be an elevated risk for serotonin syndrome or opioid toxicities (such as respiratory depression or coma). Management: Due to the risk of serotonin syndrome and/or severe CNS depression, fentanyl should not be administered in conjunction with monoamine oxidase (MAO) inhibitors (or within 14 days of discontinuing an MAO inhibitor).

Tapentadol

The negative or hazardous effects of monoamine oxidase inhibitors can be increased. In particular, norepinephrine's cumulative actions could have harmful cardiovascular repercussions. The serotonergic action of monoamine oxidase inhibitors may be enhanced by tapentadol. Serotonin syndrome might occur from this.

Tetrabenazine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Tetrahydrozoline (Nasal)

Monoamine Oxidase Inhibitors may increase Tetrahydrozoline's hypertensive impact (Nasal).

Tianeptine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Topotecan

Topotecan's serum levels may rise in response to BCRP/ABCG2 inhibitors.

Valbenazine

The negative or hazardous effects of monoamine oxidase inhibitors can be increased.

Monitor:

Monitor completed blood counts with differential at baseline and during the treatment (monitor for neutropenia)

How to administer Tedizolid (Sivextro)?

Oral:

  • Administer without regard to food.

Intravenous:

  • It should be administered as an intravenous infusion over one hour. Avoid administering as an IV push or bolus.
  • If other drugs are administered in the same intravenous line, the line should be flushed with normal saline before and after tedizolid administration.
  • Intra-arterial, SubQ, intrathecal, intraperitoneal, SubQ, and Intramuscular administration should be avoided.

Mechanism of action of Tedizolid (Sivextro):

  • Tedizolidphosphate, a bacteriostatic medication that is converted to its active form tedizolid, acts as a bacteriostatic drug.
  • By attaching to the bacterial ribosomal component 50S, it stops enterococci and staphylococci from replicating bacteria.
  • Additionally, this stops the 70S complex from forming, which stops bacteria from synthesising proteins.

It works well absorbedWhen taken orally.

70% to 90% Protein-bound drug

Metabolism: It is metabolized by phosphatases into the active metabolite Tedizolid.

The oral bioavailability is about 91%

Its elimination half-life is approximately 12 hours.

Following oral treatment, it takes approximately 3 hours, however after intravenous administration, it takes 1 to 1.5 hours for the serum concentration to reach its peak.

Excretion:  82% of it is eliminated in the form of inactive sulphate conjugates in the faeces and 18% in the urine. Less than 3% of the medicine is eliminated as parent drug in the urine or faeces.

International Brand Names of Tedizolid:

  • Cubizolid
  • Sivextro
  • Tedimerp
  • Trcarezolid
  • Zolidocyrl

Tedizolid Brand Names in Pakistan:

No Brands Available in Pakistan.