Linokem

Description

Linokem Tablet (Linezolid)

Manufacturer: Alkem Laboratories Ltd.Generic Name: Linezolid Availability: Available in Nepal

Indications:

• Community-acquired pneumonia
• Skin and skin structure infections (uncomplicated and complicated)
• Nosocomial pneumonia
• Vancomycin-resistant Enterococcus faecium infections
• Methicillin-resistant Staphylococcus aureus (MRSA) infections

Dosage:

Adult Oral Dose:

• Uncomplicated skin and skin structure infections: 400 mg every 12 hours for 10-14 days.
• Vancomycin-resistant Enterococcus faecium: 600 mg every 12 hours for 14-28 days.
• Methicillin-resistant Staphylococcus aureus infections: 600 mg twice daily for 7-21 days.
• Community-acquired pneumonia; Nosocomial pneumonia; Complicated skin and skin structure infections: 600 mg every 12 hours for 10-14 days.
• Elderly: No dosage adjustment needed.
• Hepatic impairment: Mild to moderate: No dosage adjustment needed.

Child Oral Dose:

• Pneumonia, complicated skin infections, vancomycin resistant enterococci:
  • Birth–11 years: 30 mg/kg/day every 8 hours.

  • 11 years: 1,200 mg/day every 12 hours.

• Uncomplicated skin infections:
  • Birth–5 years: 30 mg/kg/day every 8 hours.
  • 5–11 years: 20 mg/kg/day every 12 hours.

  • 11–18 years: 1,200 mg/day every 12 hours.

Renal Dose:

• Renal impairment: No dosage adjustment needed. (Give after haemodialysis. Not known if linezolid or metabolites removed during peritoneal dialysis.)

Administration: May be taken with or without food.

Contraindications:

• Known hypersensitivity to Linezolid or any other product components.
• Concomitant use with or within two weeks of taking any medicinal product that inhibits monoamine oxidases A or B (e.g., phenelzine, isocarboxazid).
• Uncontrolled hypertension.
• Pheochromocytoma.
• Thyrotoxicosis.
• Carcinoid syndrome.
• Concomitant use with directly and indirectly acting sympathomimetic agents (e.g., pseudoephedrine), vasopressive agents (e.g., epinephrine, norepinephrine), dopaminergic agents (e.g., dopamine, dobutamine), serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists (triptans), meperidine, or buspirone.

Precautions:

• Preexisting myelosuppression
• Renal impairment (CrCl < 30ml/min)
• Uncontrolled hypertension
• Phaeochromocytoma
• Carcinoid syndrome
• Untreated hyperthyroidism
• Chronic infection
• History of seizures
• Bipolar depression
• Schizophrenia or acute confusional states
• Pregnancy and lactation
• Monitor complete blood counts weekly.

Pregnancy and Lactation:

• Lactation: Unknown; use caution.
• Pregnancy: Use caution.

Interactions:

• May reduce serum levels with rifampicin and phenytoin.
• May cause hypoglycemia with insulin or oral antidiabetics.
• May increase risk of seizures with tramadol.

Potentially Fatal Interactions:

• Increased risk of serotonin syndrome with MAOIs, TCAs, SNRIs, or other serotonergic drugs (e.g., bupropion, vilazodine, mirtazapine, amoxapine, buspirone, maprotiline, meperidine, trazodone, nefazodone).
• Significant increase in blood pressure with vasopressive agents (e.g., epinephrine, norepinephrine), sympathomimetic agents (e.g., pseudoephedrine) and dopaminergic agents (e.g., dopamine, dobutamine).

Adverse Effects:

>10%:

• Pediatrics: Diarrhea (7.8-10.8%)

1-10%:

• Headache (5.7-8.8%)
• Diarrhea (8.2-8.3%)
• Nausea (5.1-6.6%)
• Vomiting (2-4.3%)
• Dizziness (1.8-2.6%)
• Rash (1.1-2.3%)
• Vaginal moniliasis (1.1-1.8%)
• Taste alteration (1-1.8%)
• Oral moniliasis (0.5-1.7%)
• Abnormal LFTs (0.4-1.6%)
• Fungal infection (0.3-1.5%)
• Localized abdominal pain (1.2-1.3%)
• Tongue discoloration (0.3-1.3%)
• Generalized abdominal pain (0.9-1.2%)
• Pediatrics: Vomiting (2.9-9.4%), Headache (0.9-6.5%), Anemia (5.6%), Thrombocytopenia (4.7%), Nausea (1.9-3.7%), Generalized abdominal pain (0.9-2.4%), Localized abdominal pain (0.5-2.4%), Loose stools (1.6-2.3%), Eosinophilia (0.4-1.9%), Pruritus (other than application site) (0.8-1.4%), Vertigo (1.2%)

<1%:

• Lactic acidosis
• Myelosuppression
• Peripheral neuropathy
• Disorder of optic nerve
• Serotonin syndrome

Potentially Fatal Adverse Effects:

• Reversible myelosuppression (including anaemia, leukopenia, pancytopenia and thrombocytopenia, particularly if using > 10-14 days)
• Transient ischaemic attacks
• Renal failure
• Stevens-Johnson syndrome

Mechanism of Action: Linezolid is a bacteriostatic oxazolidinone that inhibits ribosomal protein synthesis. It is active against Gram-positive bacteria, including vancomycin-resistant enterococci and MRSA. It has limited in vitro activity against Gram-negative bacteria.

Note: This information is not intended for diagnosis, medical advice, or treatment, nor is it intended to be a substitute for the exercise of professional judgment.