Linezolid 600 mg Tablet

Do not take ATMOLINE or give to your child before you talk to your doctor or pharmacist if you or your child:

Are allergic to linezolid or any of the other ingredients listed.
Some of the symptoms of an allergic reaction may include: shortness of breath, wheezing or difficulty breathing, swelling of the face, lips, tongue or other parts of the body, rash, itching or hives on the skin

Have uncontrolled high blood pressure

Have pheochromocytoma (a type of tumour of the adrenal gland)

Have thyrotoxicosis (an overactive thyroid gland)

Have flushing or other symptoms caused by a carcinoid tumour

Any cold or flu medicine containing pseudoephedrine

Adrenaline, a medicine used to treat severe allergic reactions

Any other medicine that increases blood pressure (e.g., noradrenaline, dopamine, dobutamine)

Tricyclic antidepressants, which are medicines to treat depression (e.g., amitriptyline, clomipramine, dothiepin, doxepin, imipramine, nortriptyline, trimipramine)

Some medicines to treat migraine (e.g.naratriptan, sumatriptan, zolmitriptan)

Pethidine, a medicine to treat pain.

Buspirone, a medicine to treat anxiety.

Linezolid should not be used in patients taking any medicinal product which inhibits monoamine oxidases A or B (e.g. phenelzine, isocarboxazid, selegiline, moclobemide) or within two weeks of taking any such medicinal product.
Unless there are facilities available for close observation and monitoring of blood pressure, linezolid should not be administered to patients with the following underlying clinical conditions or on the following types of concomitant medications:

Patients with uncontrolled hypertension, phaeochromocytoma, carcinoid, thyrotoxicosis, bipolar depression, schizoaffective disorder, acute confusional states.

Patients taking any of the following medications: serotonin re-uptake inhibitors tricyclic antidepressants, serotonin 5-HT1 receptor agonists (triptans), directly and indirectly acting sympathomimetic agents (including the adrenergic bronchodilators, pseudoephedrine and phenylpropanolamine), vasopressive agents (e.g. epinephrine, norepinephrine), dopaminergic agents (e.g. dopamine, dobutamine), pethidine or buspirone.

Animal data suggest that linezolid and its metabolites may pass into breast milk and, accordingly, breastfeeding should be discontinued prior to and throughout administration.

Linezolid may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

Diarrhea

Headache

Vomiting

Nausea

Stomach pain

Difficulty falling asleep or staying asleep

Dizziness

White patches in the mouth

Change in color of the tongue

This is Preferred Dosage:
Tablets: The recommended dose for adults and adolescents 12 years and older is one 600mg tablet twice daily (every 12 hours).

Disclaimer:To be taken only after consulting with the doctor.

PHARMACOLOGY

Mechanism of Action

Linezolid is a synthetic antibacterial agent. It inhibits bacterial protein synthesis by binding to bacterial 23S ribosomal RNA of the 50S subunit. This prevents the formation of a functional 70S initiation complex that is essential for the bacterial translation process. Linezolid is bacteriostatic against enterococci and staphylococci and bactericidal against most strains of streptococci.

Pharmacokinetics

Absorption:Rapidly and extensively absorbed after oral dosing. Maximum plasma concentrations are reached approximately 1 to 2 hours after dosing, and the absolute bioavailability is approximately 100%. Therefore, linezolid may be given orally or intravenously without dose adjustment.
Distribution: Linezolid readily distributes to well-perfused tissues. The plasma protein binding of linezolid is approximately 31% and is concentration-independent. The volume of distribution of linezolid at steady-state averaged 40 to 50 liters in healthy adult volunteers.
Metabolism: Hepatic via oxidation of the morpholine ring, resulting in two inactive metabolites (aminoethoxyacetic acid, hydroxyethyl glycine); does not involve CYP.
Bioavailability: 100%
Elimination: Half-life elimination in adults 4-5 hours. Time to peak in adults, oral is 1-2 hours.

INTERACTIONS

Linezolid is a reversible, nonselective inhibitor of MAO. Serotenergic agents (e.g., TCA‚s, venlafaxine, trazodone, sibutramine, meperidine, dextromethorphan, and SSRIs) may cause a serotonin syndrome (eg, agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, tachycardia, hyperpyrexia, cognitive dysfunction) when used concomitantly. Adrenergic agents (eg, phenylpropanolamine, pseudoephedrine, sympathomimetic agents, vasopressor or dopaminergic agents) may cause hypertension. Tramadol may increase the risk of seizures when used concurrently with linezolid. Myelosuppressive medications may increase risk of myelosuppression when used concurrently with linezolid.

Information for Patients:
Ask to read the manufacturer‚s printed information leaflet. It will give you more information about linezolid and will provide a full list of the side-effects which you may experience from taking it. Your doctor may also give you some additional printed information - it is important that you read all the information you are given.
Take linezolid exactly as your doctor tells you to. You will be asked to take two doses each day, 12 hours apart. This will usually mean taking a dose each morning and evening. You can take linezolid before or after meals.
Try to remember to take your doses at the correct times, and not to miss any. If you do forget to take a dose, take it as soon as you remember and then take the next dose 12 hours afterwards. Continue to take a dose every 12 hours. Do not take two doses together to make up for a forgotten dose.
It is usual for a course of treatment to last for 10-14 days. Even if you feel your infection has cleared up, keep taking the antibiotic until the course has finished (unless your doctor tells you otherwise). This is to prevent the infection from coming back and being more difficult to treat.

Formal Name: N-[[(5S)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide

Molecular Formula: C16H20FN3O4