tigecycline

Inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit.

Therapeutic effects:

Resolution of infection.

Spectrum:

Active against the following gram-positive bacteria: Enterococcus faecalis (vancomycin-susceptible strains only), Staphylococcus aureus (methicillin-sensitive and methicillin-resistant strains), Streptococcus agalactiae, Streptococcus anginosus, Streptococcus pneumoniae (penicillin-susceptible isolates), and Streptococcus pyogenes.
Also active against these gram-negative organisms: Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Legionella pneumophila, Klebsiella oxytoca, and Klebsiella pneumoniae.
Additionally active against the following anaerobes: Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Clostridium perfringens, and Peptostreptococcus micros.

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Widely distributed with good penetration into gall bladder, lung, and colon.

Metabolism/Excretion: Minimal metabolism; primary route of elimination is biliary/fecal excretion of unchanged drug and metabolites (59%), 33% renal (22% unchanged).

Half-Life: 27.1 hr (after 1 dose); 42.4 hr after multiple doses.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	end of infusion	12 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Diabetic foot infections
;
Hospital-acquired or ventilator-associated pneumonia (↑ risk of mortality and ↓ effectiveness)
;
Pedi: Children.

Use Cautiously in:

Complicated intra-abdominal infections due to perforation;
Severe hepatic impairment (↓ maintenance dose);
OB: Use during pregnancy only if potential maternal benefit outweighs potential fetal risk; may cause permanent teeth discoloration and suppress bone growth in fetus, especially when used during 2nd or 3rd trimester;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Geri: Older adults may be more sensitive to adverse effects.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: photosensitivity, rash, STEVENS-JOHNSON SYNDROME (SJS)

Endo: hyperglycemia, hypoglycemia

F and E: hypocalcemia, hyponatremia

GI: nausea, vomiting, ↑liver enzymes, anorexia, CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), dry mouth, jaundice, PANCREATITIS

GU: ↑serum creatinine

Hemat: hypofibrinogenemia

Local: injection site reactions

Neuro: dysgeusia, intracranial hypertension, somnolence

Resp: pneumonia

Misc: DEATH, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

May ↓ effectiveness of hormonal contraceptives.
Effects on warfarin are unknown; monitoring recommended.
May ↑ trough levels and risk of toxicity of calcineurin inhibitors, including cyclosporine and tacrolimus.

Route/Dosage ⬆ ⬇

IV (Adults ): 100 mg initially, then 50 mg every 12 hr for 5–14 days (skin/skin structure infections and intra-abdominal infections) or 7–14 days (pneumonia).

Hepatic Impairment

IV (Adults ): Severe hepatic impairment: 100 mg initially, then 25 mg every 12 hr.

Availability ⬆ ⬇

(Generic available)

Lyophilized powder for injection: 50 mg/vial

Assessment ⬆ ⬇

Assess for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and during therapy.
Before initiating therapy, obtain a history of tetracycline hypersensitivity; may be cross-reactive and should be avoided with known hypersensitivity to tetracyclines.
Monitor for signs/symptoms of hypersensitivity reaction. If symptoms occur, immediately discontinue tigecycline and treat as indicated. Keep emergency medication and equipment nearby during therapy.
Monitor for signs/symptoms of CDAD (diarrhea, abdominal cramping, fever, bloody stools). If CDAD occurs, discontinue tigecycline and treat as indicated. May begin up to several weeks following cessation of therapy.
Assess for signs/symptoms of pancreatitis (nausea, vomiting, abdominal pain, ↑ serum lipase or amylase) periodically during therapy. If pancreatitis suspected, consider discontinuation of tigecycline.
Monitor patients for development of severe cutaneous adverse reactions, including SJS. Assess for rash, fever, general malaise, fatigue, muscle or joint pain, blisters, oral lesions, and conjunctivitis periodically during therapy. If signs/symptoms of SJS occur, discontinue tigecycline.

Lab Test Considerations:

Obtain specimens for culture and sensitivity before initiating therapy. 1st dose may be given before receiving results.
- Monitor CBC with differential.
- Monitor blood coagulation parameters, including fibrinogen, before and regularly during therapy.
- May ↑ alkaline phosphatase, amylase, bilirubin, LDH, AST, and ALT. If hepatic dysfunction occurs, monitor progression and evaluate risk and benefit of continuing therapy. Hepatic dysfunction may occur after discontinuation of therapy.
- May cause ↑ BUN, azotemia, acidosis, and hyperphosphatemia. If any of these abnormalities occur, discontinue tigecycline.
- May cause hyperglycemia, hypokalemia, hypoproteinemia, hypocalcemia, or hyponatremia.

Implementation ⬆ ⬇

May cause yellow-brown discoloration and softening of teeth and bones if administered prenatally, during lactation, or early childhood through 8 yr.

IV Administration:

Intermittent Infusion: Reconstitute each vial with 5.3 mL of 0.9% NaCl or D5W. Reconstituted solution should be yellow to orange in color. Do not administer if discolored or contains particulates. Concentration: 10 mg/mL. Diluent: Dilute further in 100 mL of D5W, LR, or 0.9% NaCl. Reconstituted solution should be yellow to orange in color. Do not administer if discolored or contains particulates. Infusion is stable for up to 24 hr at room temperature or for up to 48 hr if refrigerated. Concentration: 1 mg/mL.
Rate: Infuse over 30–60 min.
Y-Site Compatibility:
- acetylcysteine
- acyclovir
- allopurinol
- amikacin
- aminocaproic acid
- aminophylline
- amphotericin B liposomal
- ampicillin
- ampicillin/sulbactam
- argatroban
- arsenic trioxide
- atracurium
- azithromycin
- aztreonam
- bivalirudin
- bumetanide
- buprenorphine
- busulfan
- butorphanol
- calcium chloride
- calcium gluconate
- cangrelor
- carboplatin
- carmustine
- caspofungin
- cefazolin
- cefepime
- cefiderocol
- cefotaxime
- cefotetan
- cefoxitin
- ceftazidime
- ceftazidime/avibactam
- ceftolozane/tazobactam
- ceftriaxone
- cefuroxime
- ciprofloxacin
- cisatracurium
- cisplatin
- clindamycin
- cyclophosphamide
- cyclosporine
- cytarabine
- dacarbazine
- dactinomycin
- daptomycin
- daunorubicin
- dexamethasone
- dexmedetomidine
- dexrazoxane
- digoxin
- diltiazem
- diphenhydramine
- dobutamine
- docetaxel
- dopamine
- doxorubicin hydrochloride
- doxorubicin liposomal
- droperidol
- enalaprilat
- ephedrine
- epinephrine
- eptifibatide
- ertapenem
- erythromycin
- esmolol
- etoposide
- etoposide phosphate
- famotidine
- fentanyl
- fluconazole
- fludarabine
- fluorouracil
- foscarnet
- fosphenytoin
- furosemide
- ganciclovir
- gemcitabine
- gentamicin
- glycopyrrolate
- granisetron
- haloperidol
- heparin
- hydrocortisone
- hydromorphone
- ifosfamide
- imipenem/cilastatin
- insulin regular
- irinotecan
- isavuconazonium
- isoproterenol
- ketorolac
- labetalol
- letermovir
- leucovorin
- levofloxacin
- lidocaine
- linezolid
- lorazepam
- magnesium sulfate
- mannitol
- melphalan
- meperidine
- meropenem
- meropenem/vaborbactam
- mesna
- methohexital
- methotrexate
- metoclopramide
- metoprolol
- metronidazole
- midazolam
- milrinone
- mitomycin
- mitoxantrone
- morphine
- moxifloxacin
- mycophenolate
- nafcillin
- nalbuphine
- naloxone
- nitroglycerin
- nitroprusside
- norepinephrine
- octreotide
- ondansetron
- oxaliplatin
- oxytocin
- paclitaxel
- palonosetron
- pamidronate
- pantoprazole
- pemetrexed
- pentamidine
- pentobarbital
- phenobarbital
- phenylephrine
- piperacillin/tazobactam
- plazomicin
- potassium acetate
- potassium chloride
- potassium phosphates
- procainamide
- prochlorperazine
- promethazine
- propofol
- propranolol
- remifentanil
- rocuronium
- sodium acetate
- sodium bicarbonate
- sodium phosphates
- succinylcholine
- sufentanil
- sulbactam/durlobactam
- tacrolimus
- tedizolid
- telavancin
- theophylline
- thiotepa
- tirofiban
- tobramycin
- topotecan
- trimethoprim/sulfamethoxazole
- vancomycin
- vasopressin
- vecuronium
- vinblastine
- vincristine
- vinorelbine
- zidovudine
- zoledronic acid
Y-Site Incompatibility:
- amiodarone
- amphotericin B deoxycholate
- bleomycin
- chloramphenicol
- chlorpromazine
- dantrolene
- diazepam
- epirubicin
- esomeprazole
- hydralazine
- idarubicin
- nicardipine
- phenytoin
- verapamil

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patient to take full course of therapy, even if feeling better. Skipping doses or not completing full course may result in ↓ effectiveness and ↑ risk of bacterial resistance.
Instruct patient to notify health care provider if fever and diarrhea develop, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care provider.
Advise patient to notify health care provider if superinfection (black, furry overgrowth on the tongue; vaginal itching or discharge; loose or foul-smelling stools), rash, pruritus, or urticaria occur.
Pedi: Caution parent that tigecycline use during infancy through 8 yr may cause permanent discoloration of the teeth and reversible bone growth inhibition.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected. Advise women of reproductive potential to use a nonhormonal method of contraception while taking tigecycline and until next menstrual period. Use during the 2nd and 3rd trimesters may cause permanent yellow-gray-brown discoloration of the teeth and reversible inhibition of bone growth in the fetus. Advise patient to avoid breastfeeding during and for 9 days after last dose.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇