Tygacil (tigecycline)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tigecycline, a synthetic derivative of minocycline, is a glycylcycline antibiotic.
Tigecycline, a synthetic derivative of minocycline, is a glycylcycline antibiotic. Tigecycline is structurally related to tetracyclines, differing mainly in the addition of a glycylamido moiety at position 9 of the tetracycline nucleus. Like tetracyclines, tigecycline inhibits protein synthesis in susceptible organisms mainly by reversibly binding to 30S ribosomal subunits, thereby inhibiting binding of aminoacyl transfer-RNA to those ribosomes.
Tigecycline has a broad spectrum of antibacterial activity and usually is bacteriostatic in action. Tigecycline is active in vitro and in clinical infections against various gram-positive aerobic and facultatively aerobic bacteria, including Staphylococcus aureus (including methicillin-resistant (oxacillin-resistant) strains), Streptococcus agalactiae (group B streptococci), S. anginosus group (S. anginosus, S. intermedius, S. constellatus), S. pneumoniae(penicillin-susceptible strains), S. pyogenes (group A beta-hemolytic streptococci), and Enterococcus faecalis (vancomycin-susceptible strains only). The drug also is active in vitro and in clinical infections against various gram-negative aerobic and facultatively aerobic bacteria, including Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (beta-lactamase-negative strains), Klebsiella oxytoca, K. pneumoniae, and Legionella pneumophila, and some anaerobic bacteria, including Bacteroides fragilis, B. thetaiotaomicron, B. uniformis, B. vulgatus, Clostridium perfringens, and Peptostreptococcus micros.
Tigecycline may be active against some bacteria resistant to conventional tetracyclines since susceptibility to the drug is not affected by the 2 major tetracycline resistance mechanisms (i.e., ribosomal protection, efflux). In addition, susceptibility to tigecycline is not affected by many other common resistance mechanisms, including beta-lactamases (e.g., extended-spectrum beta-lactamases (ESBLs)), target site modifications, macrolide efflux pumps, or enzyme target (e.g., gyrase, topoisomerase) changes. Tigecycline resistance in some bacteria (e.g., Acinetobacter calcoaceticus-baumannii complex) is attributed to multidrug-resistant (MDR) efflux pumps.
In vitro studies have demonstrated synergism between tigecycline and some other antibacterials (e.g., colistin) against some Enterobacteriaceae. (See Drug Interactions: Antibacterials.)
Tigecycline is extensively distributed into various tissues, including alveolar cells, epithelial lining fluid, skin blister fluid, gall bladder, lung, colon, synovial fluid, and bone. Tigecycline concentrations in certain tissues (i.e., alveolar cells, gallbladder, lung, colon, epithelial fluid) are substantially higher than concentrations in serum. Animal studies indicate that tigecycline crosses the placenta and is found in fetal tissues.
The drug is approximately 71-89% bound to plasma proteins. Tigecycline is not extensively metabolized; each of the recovered metabolites (a glucuronide, an N-acetyl metabolite, and a tigecycline epimer) constitutes less than 10% of the administered dose. The half-life of tigecycline is 27.1 or 42.4 hours following single or multiple dosing, respectively.
Tigecycline is principally eliminated by biliary and fecal excretion as unchanged tigecycline and metabolites. About 59% of a dose is eliminated by biliary and fecal excretion; 33% is eliminated in urine (22% as unchanged drug).
Tigecycline is used for the treatment of complicated intra-abdominal infections, community-acquired pneumonia, and complicated skin and skin structure infections caused by certain susceptible gram-positive and gram-negative bacteria.
Generic name: tigecycline
Pronunciation: (TYE-ge-SYE-kleen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Tygacil
Indications
The following indications are listed for Tygacil:
- Bacterial Pneumonia
- Cholecystitis
- Complicated Appendicitis
- Complicated Bacterial Peritonitis
- Complicated Skin And Skin Structure E. Coli Infection
- Complicated Skin And Skin Structure Enterococcus Faecalis Infection
- Complicated Skin And Skin Structure Infection
- Complicated Skin And Skin Structure Klebsiella Pneumoniae Infection
- Complicated Skin And Skin Structure Staphylococcus Aureus Infection
- Complicated Skin And Skin Structure Streptococcus Agalactiae Infection
- Complicated Skin And Skin Structure Streptococcus Pyogenes Infection
- Complicated Skin Infection From Enterobacter Cloacae Bacteria
- Diverticulitis Of Gastrointestinal Tract
- Haemophilus Influenzae Pneumonia
- Infectious Disease Of Abdomen
- Intra-Abdominal Abscess
- Legionella Pneumophila Pneumonia
- Streptococcal Pneumonia
Also known as: Abdominal Abscess, Complicated Bacterial Skin And Skin Structure Infection, Complicated E. Coli Skin And Skin Structure Infection, Complicated Skin And Skin Soft Tissue Enterococcus Faecalis Infection, Complicated Skin And Skin Soft Tissue Infection, Complicated Skin And Skin Soft Tissue Infection Due To Streptococcus Pyogenes, Complicated Skin And Skin Structure Bacterial Infection, Complicated Skin And Skin Structure Escherichia Coli Infection, Complicated Staphylococcus Aureus Skin And Skin Soft Tissue Infection, Complicated Streptococcus Pyogenes Skin And Skin Structure Infection, Diverticulitis Of Gi Tract, H. Flu Pneumonia, H. Influenzae Pneumonia, Hemophilus Influenzae Pneumonia, Influenza Bacillus Pneumonia, Intra-Abdominal Infection, Pfeiffer's Bacillus Pneumonia, Pneumonia Due To Haemophilus Influenzae, Pneumonia Due To Streptococcus Species, Pneumonia Due To Streptococcus Spp..
Dosing
No dosing information is available for this tab.
Tigecycline is administered by IV infusion.
Tigecycline may be administered through a dedicated line or through a Y-site. If the same IV line is used for sequential infusion of several drugs, the line should be flushed before and after infusion of tigecycline with 0.9% sodium chloride, 5% dextrose, or lactated Ringer's injection. Tigecycline should not be administered simultaneously through the same Y-site with amphotericin B, amphotericin B lipid complex, diazepam, esomeprazole, or omeprazole.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to tigecycline or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Nausea, vomiting, and diarrhea are the most common adverse effects reported with tigecycline and have been reported in up to 35% of patients in clinical studies.
Adverse effects reported in 2-8% of patients receiving tigecycline include abdominal pain, abnormal healing, abscess, anemia, asthenia, bilirubinemia, dizziness, dyspepsia, headache, hypoproteinemia, increased ALT or AST concentrations, increased alkaline phosphatase concentrations, increased amylase concentrations, increased BUN, infection, phlebitis, and rash.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of tigecycline have not been established in patients younger than 18 years of age and use in this age group is not recommended. Because of the increased mortality observed in adults receiving tigecycline, clinical trials evaluating safety and efficacy of tigecycline in pediatric patients have not been conducted.
For circumstances when there are no alternative anti-infectives, pediatric dosage has been proposed based on data from pharmacokinetic studies that included limited numbers of pediatric patients. For children 8-11 years of age, a pharmacokinetic simulation showed that a tigecycline dosage of 1.2 mg/kg in this age group would likely result in an area under the plasma concentration-time curve (AUC) similar to that reported in adults receiving the recommended adult dosage. For children and adolescents 12-16 years of age, a tigecycline dosage of 50 mg twice daily would likely result in exposures comparable to those observed in adults receiving the recommended adult dosage. (See Pediatric Dosage under Dosage and Administration: Dosage.)
Because use of tigecycline during tooth development (i.e., in infants and children younger than 8 years of age) may cause permanent discoloration (yellow-gray-brown) of the teeth, the drug should not be used in this age group unless other anti-infectives cannot be used. (See Cautions: Pediatric Precautions in the Tetracyclines General Statement 8:12.24.)
Category D. (See Users Guide.) Tigecycline crosses the placenta and is found in fetal tissues. (See Fetal/Neonatal Morbidity and Mortality under Warnings/Precautions: Other Warnings/Precautions, in Cautions.)
Use of tigecycline during tooth development (last half of pregnancy) may cause permanent discoloration (yellow-gray-brown) of the teeth. (See Cautions: Pediatric Precautions in the Tetracyclines General Statement 8:12.24.)
Tigecycline is distributed into milk in rats. It is not known whether tigecycline is distributed into human milk; caution is advised if the drug is administered in nursing women.
There are no substantial differences in safety and efficacy in patients 65 years of age or older relative to younger adults, but increased sensitivity cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
Search health-plan coverage for this drug by ZIP code.
Choose the first character of a health plan name.
Last reviewed · Source: First Databank (FDB) drug data
On this page
Actions
Sign in to save favorites
Saving this drug requires a free Physicians Office Resource account.