Tigecycline
Indications
Tigecycline is used for:
Complicated intra-abdominal infections; Complicated skin and skin structure infections, Community-acquired pneumonia
Adult Dose
The recommended daily dose is as follows:
Adults: The recommended dosage regimen for Tigecycline is an initial dose of 100 mg, followed by 50 mg every 12 hours. Intravenous (IV) infusions of Tigecycline should be administered over approximately 30 to 60 minutes every 12 hours.
The duration of therapy should be guided by the severity and site of the infection and the patient's clinical and bacteriological progress. The recommended duration of treatment with Tigecycline for complicated skin and skin structure infections or for complicated intra-abdominal infections is 5 to 14 days and for Community-acquired pneumonia is 7-14 days.
Hepatic impairment: Mild to moderate: No dosage adjustment. Severe: 100 mg as a single dose, then 25 mg 12 hrly.
Child Dose
<18 years: Safety and efficacy not established
Renal Dose
Renal impairment: No dosage adjustment needed.
Administration
IV Preparation
Reconstitute each vial with 5.3 mL NS or D5W to achieve a conc of 10 mg/mL
IV Administration
Infuse over 30-60 min
Contra Indications
Hypersensitivity. Hospital-acquired pneumonia and ventilator-associated pneumonia. Use during tooth development.
Precautions
Hypersensitivity to tetracyclines. Use tigecycline in situations when alternative treatments are not suitable. Patients w/ complicated intra-abdominal infections secondary to clinically apparent intestinal perforation. Hepatic impairment. Pregnancy and lactation.
Pregnancy-Lactation
Pregnancy
May cause permanent discoloration of deciduous teeth and reversible inhibition of bone growth when administered during second and third trimesters of pregnancy
There are no available data on risk of major birth defects or miscarriage following use during pregnancy
Advise patients of potential risk to fetus if drug is used during second or third trimester
Animal data
Administration of intravenous tigecycline in pregnant rats and rabbits during period of organogenesis was associated with reduction in fetal weights and an increased incidence of skeletal anomalies (delays in bone ossification) at exposures of 5 and 1 times the human exposure at recommended clinical dose in rats and rabbits, respectively
Lactation
There are no data on presence of drug in human milk; however, tetracycline-class antibacterial drugs are present in breast milk
Not known whether drug has an effect on breastfed infant or on milk production
Drug has low oral bioavailability; therefore, infant exposure is expected to be low
Drug is present in rat milk with little or no systemic exposure to drug in nursing pups as a result of exposure via maternal milk; when drug is present in animal milk, it is likely that the drug will be present in human milk
Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed child from drug or from underlying maternal condition
Because of theoretical risk of dental discoloration and inhibition of bone growth, avoid breastfeeding if receiving therapy for longer than three weeks
A lactating woman may consider interrupting breastfeeding and pumping and discarding breastmilk during administration of therapy and for 9 days (approximately 5 half-lives) after last dose in order to minimize drug exposure to a breastfed infant
Interactions
Increased warfarin serum levels. May decrease efficacy of oral contraceptives.
Adverse Effects
Side effects of Tigecycline :
>10%
Nausea (29.5%), Vomiting (19.7%), Diarrhea (12.7%)
1-10%
Infection (8.3%), Fever (7.1%), Abd pain (6.8%), Headache (5.9%), HTN (4.9%), Anemia (4.2%), Dizziness (3.5%), Dyspnea (2.9%), Pruritus (2.6%), Rash (2.4%), Hypotension (2.3%), Insomnia (2.3%)
Mechanism of Action
Tigecycline is a glycylcycline antibiotic which prevents protein synthesis of the susceptible bacteria by binding to its 30s ribosomal subunit. It is generally considered as bacteriostatic agent; w/ bactericidal activity against S. pneumonia and L. pneumophilia. Tigecycline antibacterial activity covers facultative gm+ve (including MRSA, vancomycin-susceptible Enterococcus faecalis) and gm-ve bacteria, and anaerobic bacteria.