TYGACIL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TYGACIL (TYGACIL).
Tigecycline is a glycylcycline antibiotic that binds to the 30S ribosomal subunit, inhibiting protein synthesis by blocking the entry of amino-acyl tRNA molecules into the A site of the ribosome.
| Metabolism | Tigecycline is not extensively metabolized. It undergoes minimal hepatic metabolism, primarily via glucuronidation and amide hydrolysis, and is not significantly metabolized by CYP450 enzymes. |
| Excretion | Biliary/fecal: ~59% unchanged; renal: ~15% unchanged; total recovery: ~74%. |
| Half-life | Terminal half-life: 42.7 hours. Prolonged in renal impairment and severe hepatic impairment; clinically significant for dosing interval adjustments. |
| Protein binding | ~71-89% bound to plasma proteins (mainly albumin and lipoproteins). |
| Volume of Distribution | Vd: 7-9 L/kg; large distribution indicates extensive tissue penetration, including skin, soft tissue, and gastrointestinal tract. |
| Bioavailability | IV only; oral bioavailability negligible (not administered orally). |
| Onset of Action | IV: Rapid distribution; clinical effect typically within hours. |
| Duration of Action | Dosing every 12 hours maintains therapeutic concentrations; prolonged Vd/t1/2 supports twice-daily dosing. |
| Action Class | Tetracyclines |
| Brand Substitutes | Tgkem 50mg Injection, Teglin 50mg Injection, Tigi 50mg Injection, Tagbact 50mg Injection, Tiziren 50mg Injection |
100 mg IV loading dose, then 50 mg IV every 12 hours
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for renal impairment or hemodialysis. |
| Liver impairment | For severe hepatic impairment (Child-Pugh C): initial loading dose of 100 mg, then 25 mg IV every 12 hours. No adjustment for Child-Pugh A or B. |
| Pediatric use | For patients 8 years and older: 1.2 mg/kg IV every 12 hours, not to exceed 50 mg per dose. For patients under 8 years: not recommended. |
| Geriatric use | No specific dose adjustment recommended based on age alone. Monitor renal function as elderly may have reduced clearance; caution with concurrent hepatotoxic drugs. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TYGACIL (TYGACIL).
| Breastfeeding | Excreted in rat milk; unknown in humans. M/P ratio not established. Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for tigecycline and potential adverse effects on the breastfed infant. Infant exposure likely low due to high protein binding (71-89%); however, caution advised. |
| Teratogenic Risk | FDA Pregnancy Category D. Tigecycline crosses the placenta. Animal studies show reduced fetal weight and skeletal ossification delays. There are no adequate human studies; use only if benefit outweighs risk. First trimester: potential for teratogenicity unknown. Second and third trimesters: risk of fetal growth impairment and bone development issues. |
■ FDA Black Box Warning
An increase in all-cause mortality has been observed in clinical trials with tigecycline compared to comparator drugs. The cause of this increase has not been established. Tigecycline should be reserved for use in patients with limited treatment options.
| Serious Effects |
["Hypersensitivity to tigecycline or any component of the formulation"]
| Precautions | ["Hypersensitivity reactions, including anaphylaxis","Hepatic effects: acute pancreatitis, hepatic failure","Increased mortality risk in clinical trials","Pseudomembranous colitis due to Clostridioides difficile","Prothrombin time prolongation and hypoprothrombinemia","Photosensitivity potential","Use in pregnancy: fetal harm based on animal data","Tooth discoloration in children <8 years","Potential for resistance development"] |
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| Fetal Monitoring | Monitor liver function tests, renal function, and complete blood count. Assess for signs of pancreatitis and superinfection. Fetal monitoring: consider ultrasound to assess growth and skeletal development with prolonged use. |
| Fertility Effects | Animal studies show no impairment of fertility at clinically relevant doses. No human data on fertility impact. |