Tigecycline

Trade Names:
Tygacil
- Injection, lyophilized powder for solution 50 mg

Pharmacology

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Tigecycline, a glycylcycline, inhibits protein transportation in bacteria by binding to the 30S ribosomal subunit and blocking entry of amino-acyl tRNA molecules into the A site of the ribosome. This prevents incorporation of amino acid residues into elongating peptide chains.

Pharmacokinetics

Absorption

C _max and AUC _0-24h for 50 mg every 12 h as a 30-min infusion are 0.87 mcg/mL and 4.7 mcg•h/mL, respectively.

Distribution

Plasma protein binding ranges from 71% to 89%. Vd is 7 to 9 L/kg.

Metabolism

Not extensively metabolized.

Elimination

The half-life is approximately 42 h and Cl is approximately 23.8 L/h (multiple dosing). Primary route of elimination is biliary/fecal excretion (59% of dose); glucuronidation and renal excretion are secondary routes (33% of dose excreted in urine, 22% as unchanged tigecycline).

Special Populations

Pharmacokinetics not significantly altered.

Systemic Cl reduced 25% and half-life prolonged 23% in patients with moderate hepatic impairment (Child-Pugh class B); systemic Cl reduced 55% and half-life prolonged 43% in patients with severe hepatic impairment (Child-Pugh class C).

Indications and Usage

Treatment of community-acquired bacterial pneumonia, complicated skin and skin structure infections, and complicated intra-abdominal infections caused by susceptible strains of specific microorganisms.

Contraindications

Standard considerations.

Dosage and Administration

IV Initial dose of 100 mg followed by 50 mg every 12 h for 5 to 14 days (complicated skin and skin structure infections and intra-abdominal infections) or 7 to 14 days (community-acquired bacterial pneumonia).

No dosage adjustment needed.

Initial dose of 100 mg followed by maintenance dose of 25 mg every 12 h.

General Advice

• For IV infusion only. Not for intradermal, subcutaneous, IM, IV bolus, or intra-arterial administration.
• Reconstitute each vial of tigecycline 50 mg with 5.3 mL of sodium chloride 0.9% injection, dextrose 5% injection, or Ringer's lactate (2 vials for 100 mg dose; 1 vial for 50 mg dose). Gently swirl until drug dissolves. Reconstituted solution contains tigecycline 10 mg/mL. Prepare infusion solution by immediately withdrawing 5 mL of reconstituted solution from the vial and adding to 100 mL IV bag for infusion. Max concentration in IV bag should be 1 mg/mL.
• Reconstituted solution should be yellow to orange in color; if not, the solution should be discarded. Do not administer if particulate matter, cloudiness, or discoloration (eg, black, green) is noted.
• Administer prescribed dose over 30 to 60 min through a dedicated IV line or through a Y-site. If IV line is used for sequential infusion of other drugs, flush IV line with sodium chloride 0.9% injection, dextrose 5% injection, or Ringer's lactate before and after infusion of tigecycline.
• The following drugs or diluents are compatible with tigecycline when administered through a Y-site: amikacin, dobutamine, dopamine, gentamicin, haloperidol, lidocaine, morphine, norepinephrine, piperacillin/tazobactam (EDTA formulation), potassium chloride, propofol, ranitidine, Ringer's lactate, theophylline, and tobramycin.
• The following drugs should not be administered simultaneously through the same Y-site as tigecycline: amphotericin B and diazepam.

Storage/Stability

Store unopened vials at 59° to 86°F. Reconstituted solution must be immediately transferred and further diluted for IV infusion. Diluted solution may be stored at room temperature for up to 24 h (up to 6 h in the vial and the remaining time in the IV bag), or refrigerated (36° to 46°F) for up to 48 h after immediate transfer of the reconstituted solution to the IV bag.

Drug Interactions

Coadministration may decrease the effectiveness of the oral contraceptive.

Warfarin Cl may be reduced and plasma levels may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Phlebitis (3%); thrombophlebitis (less than 2%).

CNS

Headache (6%); asthenia, dizziness (3%).

Dermatologic

Rash (3%); pruritus (less than 2%).

EENT

Taste perversion (less than 2%).

GI

Nausea (35%); vomiting (20%); diarrhea (12%); abdominal pain (6%); dyspepsia (2%); abnormal stools, anorexia (less than 2%).

Genitourinary

Leukorrhea, vaginal moniliasis, vaginitis (less than 2%).

Hematologic-Lymphatic

Anemia (4%); eosinophilia, increased INR, prolonged aPTT, prolonged PT, thrombocytopenia (less than 2%).

Hepatic

Jaundice (less than 2%); acute pancreatitis, hepatic cholestasis (postmarketing).

Local

Injection-site edema, inflammation, pain, phlebitis, or reaction (less than 2%).

Metabolic-Nutritional

ALT increased, hypoproteinemia (5%); alkaline phosphatase increased, AST increased (4%); increased amylase, increased BUN (3%); bilirubinemia (2%); hypocalcemia, hypoglycemia, hyponatremia, increased creatinine (less than 2%).

Miscellaneous

Infection (8%); death (5%); abnormal healing (4%); abscess (3%); sepsis/septic shock (2%); allergic reactions, chills (less than 2%); anaphylaxis/anaphylactoid reactions (postmarketing).

Precautions

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy in children younger than 18 yr of age has not been established. Use in patients younger than 8 yr of age is not recommended because of effects on tooth development.

Hypersensitivity

Use with caution in patients with known hypersensitivity to tetracycline class antibiotics.

Hepatic Function

Treat patients with severe hepatic function with caution; reduce dose and monitor for treatment response.

Superinfection

May result in overgrowth of nonsusceptible organisms.

Hepatic effects

Increases in total bilirubin, PT, and transaminases have been seen. Isolated cases of significant hepatic dysfunction and hepatic failure have also been reported.

Intestinal perforation

Use caution when considering tigecycline monotherapy in patients with complicated intra-abdominal infections secondary to intestinal perforation.

Pseudomembranous colitis

Consider possibility in patients who develop diarrhea.

Tetracycline antibiotics

Tigecycline is structurally similar to tetracycline class antibiotics and may have similar adverse effects (eg, anti-anabolic action, pancreatitis, photosensitivity, pseudotumor cerebri).

Tooth discoloration

May cause permanent discoloration of teeth (yellow-gray-brown) if used during tooth development (last half of pregnancy, infancy, and children younger than 8 yr of age). Do not use during tooth development unless other drugs are not likely to be effective or are contraindicated.

Ventilator-associated pneumonia

Efficacy not demonstrated in patients with hospital-acquired pneumonia. Lower cure rates and greater mortality were observed in the subgroup of patients with ventilator-associated pneumonia.

Overdosage

Symptoms

Nausea and vomiting.

Patient Information

• Advise patient or caregiver that medication will be prepared and administered by a health care provider in a health care setting.
• Advise patient to take medication exactly as directed. Skipping doses or not completing therapy may decrease the effectiveness of the treatment.
• Review dosing schedule and prescribed length of therapy with patient. Advise patient that duration of therapy is dependent on site, severity of infection, and response to treatment.
• Advise patient or caregiver to immediately inform health care provider if injection-site pain or redness, skin rash, hives, itching, or shortness of breath occur during treatment.
• Advise patient or caregiver to report signs of superinfection to health care provider: black, “furry” tongue; foul-smelling stools; vaginal itching or discharge; white patches in mouth.
• Warn patient or caregiver that diarrhea containing blood or pus may be a sign of a serious disorder and, if noted after discharge, to seek medical care and not treat at home.

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