TIGECYCLINE
Clinical safety rating: caution
Animal studies have proved adverse effects but may be safe for humans
Tigecycline is a glycylcycline antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, blocking entry of amino-acyl tRNA into the A site, thereby preventing peptide chain elongation.
| Metabolism | Tigecycline is not extensively metabolized. It undergoes minimal hepatic metabolism, primarily via glucuronidation and possibly by amide hydrolysis, but specific CYP450 enzymes are not significantly involved. |
| Excretion | Approximately 59% of the dose is excreted via bile/feces, with 22% eliminated unchanged in urine. The remainder undergoes hepatic metabolism. |
| Half-life | Terminal elimination half-life is approximately 27-42 hours in patients with normal renal function, supporting twice-daily dosing. Half-life may be prolonged in severe hepatic impairment. |
| Protein binding | Tigecycline is primarily bound to plasma proteins, with a binding rate of approximately 71-89% (mainly to albumin and lipoproteins). |
| Volume of Distribution | Volume of distribution is large, ranging from 7-10 L/kg, indicating extensive tissue penetration and distribution beyond plasma volume. |
| Bioavailability | Tigecycline is administered only intravenously; oral bioavailability is negligible due to poor absorption. Absolute IV bioavailability is 100%. |
| Onset of Action | Intravenous administration: Onset of action is rapid, with therapeutic plasma levels achieved within 60 minutes following a 30-60 minute infusion. |
| Duration of Action | Duration of action is approximately 12 hours post-dose, aligning with the recommended dosing interval of every 12 hours. Clinical effect persists for the dosing interval. |
| Molecular Weight | 585.65 |
Loading dose: 100 mg IV once, then 50 mg IV every 12 hours.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for renal impairment, including hemodialysis. Tigecycline is not removed by hemodialysis. |
| Liver impairment | Child-Pugh A and B: No adjustment. Child-Pugh C: Loading dose 100 mg IV once, then 25 mg IV every 12 hours. |
| Pediatric use | For patients aged 8 to 11 years: 1.2 mg/kg IV every 12 hours (maximum dose 50 mg per infusion). For patients aged 12 to 17 years: 50 mg IV every 12 hours. |
| Geriatric use | No specific dose adjustment; monitor for adverse effects, as elderly patients may have increased risk of mortality and gastrointestinal effects. |
| 1st trimester | Avoid; animal studies show fetal harm, no adequate human studies. |
| 2nd trimester | Avoid; potential for fetal toxicity, including skeletal abnormalities. |
| 3rd trimester | Avoid; may cause permanent tooth discoloration and bone growth inhibition. |
Clinical note
Warfarin metabolism may be affected increasing INR Can increase all-cause mortality and is reserved for use when alternatives are not suitable.
| Placental transfer | Crosses placenta; detected in fetal tissues. |
| Breastfeeding | Excreted in breast milk; potential for serious adverse effects in nursing infants; consider alternative agents. |
| Lactation Rating |
■ FDA Black Box Warning
An increase in all-cause mortality was observed in clinical trials with tigecycline compared to comparators. The cause of this increase has not been established. Tigecycline should be reserved for use in patients with limited or no alternative treatment options.
| Common Effects | Nausea |
| Serious Effects |
Hypersensitivity to tigecycline or any tetracyclinePatients with known hypersensitivity
| Precautions | Hypersensitivity reactions including anaphylaxis, Hepatic effects: increased liver enzymes, hepatic dysfunction, Pancreatitis, Fetal harm if used in pregnancy; avoid in pregnant women unless benefit outweighs risk, Tooth discoloration in children <8 years, Use in patients with intestinal perforation: risk of sepsis, Photosensitivity, Superinfection: prolonged use may result in bacterial or fungal overgrowth |
| Food/Dietary |
Loading safety data…
| L4 (Possibly Hazardous) |
| Teratogenic Risk | Tigecycline is classified as FDA Pregnancy Category D. There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience. In animal studies, tigecycline caused reduced fetal weights and minor skeletal abnormalities. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Avoid use in the first trimester if possible. |
| Fetal Monitoring | Monitor for signs of hepatotoxicity and pancreatitis in both mother and fetus. Monitor liver function tests (AST, ALT, bilirubin) and pancreatic enzymes (amylase, lipase) periodically. Assess for fetal growth and well-being via ultrasound if clinical concerns arise. |
| Fertility Effects | Tigecycline has not been studied for effects on fertility in humans. In animal studies, there were no effects on mating or fertility at clinically relevant doses. However, theoretical risks from its anti-anaerobic activity on gut flora may indirectly affect fertility. |
| No specific food restrictions are required. However, tigecycline is administered intravenously and is not affected by oral intake. Alcohol consumption should be avoided due to potential hepatotoxicity and increased adverse effects. |
| Clinical Pearls | Tigecycline is a glycylcycline antibiotic with broad-spectrum activity, including MRSA and VRE. It achieves high tissue penetration but low serum concentrations; thus, it is not recommended for bloodstream infections. Its FDA black box warning notes an increased risk of all-cause mortality (observed in clinical trials), particularly in patients with hospital-acquired pneumonia. Monitor for pancreatitis, hepatic dysfunction, and coagulopathy. Avoid in patients <18 years due to permanent tooth discoloration and bone growth impairment. Dose adjustment is not required for renal impairment but caution in hepatic impairment (Child-Pugh C: reduce maintenance dose by 50% after initial loading dose). Rapid infusion can cause nausea and vomiting; administer over 30-60 minutes. |
| Patient Advice | Take tigecycline exactly as prescribed, usually by intravenous infusion once or twice daily. · Inform your doctor if you have liver disease, pancreatitis, or are pregnant or breastfeeding. · This medication may cause nausea, vomiting, or diarrhea; if persistent or severe, notify your healthcare provider. · Avoid alcohol while on this medication as it may increase the risk of liver injury. · Report any signs of infection (fever, chills) or unusual bleeding/bruising to your doctor. · Do not receive live vaccines (e.g., flu nasal spray) during treatment without consulting your doctor. |