TYLIN

Indications

• Complicated skin and skin structure infections
• Complicated intra-abdominal infections
• Community-acquired pneumonia

Dosage

Children: Refer to the BNF for Children for appropriate dosing in paediatric patients.

Adults: The recommended dose for adults is 100 mg IV as a loading dose, followed by 50 mg IV every 12 hours.

Mechanism of action

Tigecycline exerts its antimicrobial effect by binding to the 30S ribosomal subunit of bacteria, inhibiting protein synthesis. This action disrupts the translation process, ultimately leading to bacterial cell growth inhibition and death. The unique structure of tigecycline allows it to overcome some resistance mechanisms that limit the effectiveness of other tetracyclines.

Pharmacodynamics

Tigecycline has a broad spectrum of activity, effective against a variety of bacteria including both aerobic and anaerobic organisms. It demonstrates time-dependent bactericidal activity, where the duration of exposure above the minimum inhibitory concentration (MIC) is critical for its efficacy. The drug is particularly noted for its effectiveness against certain strains of Gram-positive cocci, including MRSA, and some Gram-negative bacilli.

Pharmacokinetics

Tigecycline is administered intravenously and has a volume of distribution that suggests extensive tissue penetration. It is not significantly metabolized by cytochrome P450 enzymes and is primarily eliminated via biliary excretion. The drug has a half-life of approximately 27 hours, allowing for once or twice daily dosing. Its plasma protein binding is high, around 70-90%, which may affect its distribution and elimination.

Contra-indications

• Hypersensitivity to tigecycline or any of its components
• Pregnancy

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Headache
• Dizziness
• Rash

Interactions

• Carbamazepine: Unknown (decreases exposure)
• Antifungals, azoles: Unknown (increases exposure)
• Verapamil: Unknown (increases exposure)
• Coumarins: Unknown (affects anticoagulant effect)
• Ivacaftor: Unknown (increases exposure)
• Lapatinib: Unknown (increases exposure)
• Macrolides: Unknown (increases exposure)
• Neratinib: Unknown (increases exposure)
• Phenindione: Unknown (increases anticoagulant effect)
• Ranolazine: Unknown (increases exposure)

Precautions

• Use with caution in patients with a history of hypersensitivity to tetracycline antibiotics
• Monitor for signs of superinfection during therapy
• Not recommended for use in patients with liver impairment

Pregnancy

Tigecycline is contraindicated in pregnancy due to potential harm to the fetus.

Breast-feeding

Tigecycline should be used with caution in breastfeeding, as it is not known if it is excreted in human milk.

Storage

Store at 20 to 25 degrees Celsius. Protect from light and moisture.

Formulations

• Intravenous powder for reconstitution