Tigecycline (50mg)

Clinical Pharmacologist's Monograph

⚠️ Prescription Only: This medicine is Schedule H/H1. Do not self-medicate.

1. Clinical Overview

Tigecycline is a broad-spectrum glycylcycline antibiotic, structurally derived from minocycline. It is a bacteriostatic agent with activity against a wide range of Gram-positive, Gram-negative, anaerobic, and atypical bacteria, including many multidrug-resistant (MDR) pathogens. It is a critical reserve antibiotic in the Indian context, used primarily for complicated intra-abdominal infections (cIAI) and complicated skin and skin structure infections (cSSSI) when other alternatives are unsuitable due to resistance or allergy.

OnsetDurationBioavailability
Peak plasma concentrations are achieved within 0.5 to 4 hours post-infusion.The dosing interval is every 12 hours, supported by a long post-antibiotic effect (PAE).Not applicable (Intravenous administration only).

2. Mechanism of Action

Tigecycline inhibits protein synthesis in bacteria by binding reversibly to the 30S ribosomal subunit. This blocks the entry of amino-acyl tRNA molecules into the A site of the ribosome, preventing the incorporation of amino acid residues into elongating peptide chains.

3. Indications & Uses

  • Complicated Intra-abdominal Infections (cIAI) caused by susceptible organisms like E. coli, B. fragilis, Enterococcus faecalis.
  • Complicated Skin and Skin Structure Infections (cSSSI) caused by susceptible organisms like S. aureus (MRSA & MSSA), Streptococcus pyogenes, E. coli, B. fragilis.

4. Dosage & Administration

Adult Dosage: Initial dose: 100 mg IV single dose, followed by 50 mg IV every 12 hours. Duration: 5 to 14 days based on infection severity and clinical response.

Administration: Reconstitute 50 mg vial with 5.3 mL of 0.9% Sodium Chloride or 5% Dextrose to get 10 mg/mL. Further dilute in 100 mL of compatible IV fluid (NS or D5W). Infuse over 30 to 60 minutes. Flush line before/after with same diluent. Incompatible with amphotericin B, chlorpromazine, methylprednisolone, voriconazole.

5. Side Effects

Common side effects may include:

  • Nausea (26-35%)
  • Vomiting (16-20%)
  • Diarrhea (12-14%)
  • Injection site reactions

6. Drug Interactions

DrugEffectSeverity
WarfarinTigecycline may prolong PT/INR; increased monitoring required.Moderate
Oral ContraceptivesPotential reduction in contraceptive efficacy; advise alternative non-hormonal methods.Moderate
Proton Pump Inhibitors (e.g., Omeprazole)Concurrent use may reduce tigecycline absorption if given orally (not relevant for IV).Minor
Live Bacterial Vaccines (e.g., Typhoid, BCG)Antibiotics may diminish therapeutic effect of live vaccines.Moderate

7. Patient Counselling

  • Complete the full prescribed course even if you feel better.
  • Report severe diarrhea, even if it occurs weeks after finishing the antibiotic.
  • Inform all doctors about this medication if you need surgery or dental work.
  • Use effective non-hormonal contraception during treatment if applicable.

8. Toxicology & Storage

Overdose: Expected to be an extension of side effects: severe nausea, vomiting, pancreatitis. No specific antidote.

Storage: Store unopened vials at or below 25°C. Protect from light. Reconstituted solution in vial is stable for up to 6 hours at room temperature or up to 48 hours refrigerated (2-8°C). The fully diluted solution in IV bag is stable for up to 24 hours at room temperature or up to 48 hours refrigerated. Do not freeze.