Tigecycline

Intravenous
Community-acquired pneumonia
Adult: Initially, 100 mg, followed by 50 mg 12 hourly via infusion over 30-60 minutes. Treatment duration: 7-14 days, according to the severity, site of infection, and patient's clinical response.
Hepatic impairment: Severe: Initially, 100 mg, followed by 25 mg 12 hourly.
Reconstitution: Reconstitute vial labelled as containing 50 mg with 5.3 mL of NaCl 0.9% inj or dextrose 5% inj to achieve a concentration of 50 mg/5 mL. Gently swirl to dissolve. Further dilute reconstituted vial(s) to a 100 mL infusion bag up to Max final concentration of 1 mg/mL.
Incompatibility: Y-site: Amphotericin B, diazepam, omeprazole, esomeprazole, or any IV solution that may result in a pH above 7.

Intravenous
Complicated intra-abdominal infections
Adult: Initially, 100 mg, followed by 50 mg 12 hourly via infusion over 30-60 minutes. Treatment duration: 5-14 days, according to the severity, site of infection, and patient's clinical response.
Hepatic impairment: Severe: Initially, 100 mg, followed by 25 mg 12 hourly.
Reconstitution: Reconstitute vial labelled as containing 50 mg with 5.3 mL of NaCl 0.9% inj or dextrose 5% inj to achieve a concentration of 50 mg/5 mL. Gently swirl to dissolve. Further dilute reconstituted vial(s) to a 100 mL infusion bag up to Max final concentration of 1 mg/mL.
Incompatibility: Y-site: Amphotericin B, diazepam, omeprazole, esomeprazole, or any IV solution that may result in a pH above 7.

Intravenous
Complicated skin and skin structure infections
Adult: Initially, 100 mg, followed by 50 mg 12 hourly via infusion over 30-60 minutes. Treatment duration: 5-14 days, according to the severity, site of infection, and patient's clinical response.
Hepatic impairment: Severe: Initially, 100 mg, followed by 25 mg 12 hourly.
Reconstitution: Reconstitute vial labelled as containing 50 mg with 5.3 mL of NaCl 0.9% inj or dextrose 5% inj to achieve a concentration of 50 mg/5 mL. Gently swirl to dissolve. Further dilute reconstituted vial(s) to a 100 mL infusion bag up to Max final concentration of 1 mg/mL.
Incompatibility: Y-site: Amphotericin B, diazepam, omeprazole, esomeprazole, or any IV solution that may result in a pH above 7.

Hypersensitivity to tigecycline or tetracycline.

Patient with intestinal perforation. Hepatic impairment. Pregnancy and lactation. Not indicated for the treatment of hospital-acquired or ventilator-associated pneumonia, diabetic foot infections. Reserve the use of tigecycline in situations when alternative treatments are not suitable. Patient Counselling This drug may cause dizziness, if affected, do not drive or operate machinery. Avoid direct exposure to sunlight. Monitoring Parameters Monitor baseline blood coagulation parameters, including fibrinogen; LFT; development of superinfection, at baseline and regularly during treatment. Monitor for signs and symptoms of hypersensitivity reactions during administration.

Significant: Anti-anabolic effects (e.g. increased BUN, azotaemia, acidosis, hyperphosphataemia); coagulopathy (e.g. prolongation of PT and aPTT, decreased fibrinogen); photosensitivity, pseudotumour cerebri; superinfection including C. difficile-associated diarrhoea (prolonged use). Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, dyspepsia, anorexia. General disorders and administration site conditions: Injection site reactions. Hepatobiliary disorders: Jaundice, increased ALT, AST, alkaline phosphatase and bilirubin. Infections and infestations: Abscess. Nervous system disorders: Headache, dizziness. Skin and subcutaneous tissue disorders: Pruritus, rash. Vascular disorders: Thrombophlebitis.
Potentially Fatal: Anaphylaxis and anaphylactoid reactions, acute pancreatitis, hepatic failure.

May increase warfarin serum levels. May decrease efficacy of oral contraceptives.

Tigecycline, a synthetic derivative of minocycline, is a glycylcycline antibiotic which inhibits protein synthesis by binding to the 30s ribosomal of susceptible bacteria. It is generally considered as bacteriostatic agent with bactericidal activity against S. pneumonia and L. pneumophilia. Tigecycline antibacterial activity covers facultative gram-positive and gram-negative bacteria including methicillin-resistant staphylococci.
Distribution: Widely distributed into the tissues; crosses the placenta. Volume of distribution: 7-9 L/kg. Plasma protein binding: 71-89%.
Metabolism: Not extensively metabolised in the liver via glucuronidation, N-acetylation, and epimerisation, resulting in trace amount of glucuronide, N-acetyl metabolite, and tigecycline epimer.
Excretion: Via faeces (59%, mainly as unchanged drug); urine (33%; 22% of the total dose as unchanged drug). Elimination half-life: 27 hours (single dose); 42 hours (following multiple doses).

Intravenous: Unopened vial: Store below 30°C. Reconstituted solution: Store below 25°C for up to 24 hours or between 2-8°C for up to 48 hours.

Tetracyclines

J01AA12 - tigecycline ; Belongs to the class of tetracyclines. Used in the systemic treatment of infections.