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Aztreonam (Systemic)


General


Pronunciation

(AZ tree oh nam)


Brand Names: U.S.

  • Azactam
  • Azactam in Dextrose

Indications


Use: Labeled Indications

Treatment of patients with urinary tract infections, lower respiratory tract infections, septicemia, skin/skin structure infections, intra-abdominal infections, and gynecological infections caused by susceptible gram-negative bacilli


Contraindications


Hypersensitivity to aztreonam or any component of the formulation


Dosing and Administration


Dosing: Adult

Urinary tract infection: IM, IV: 500 mg to 1 g every 8 to 12 hours

Moderately severe systemic infections: 1 g IV or IM or 2 g IV every 8 to 12 hours. Note: IV route preferred for septicemia, intra-abdominal abscess, or peritonitis; higher doses (8 to 12 g daily) may be needed for patients with cystic fibrosis (Zobell, 2013) or other infections (Solomkin, 2010).

Severe systemic or life-threatening infections (eg, Pseudomonas aeruginosa): IV: 2 g every 6 to 8 hours; maximum: 8 g daily. Note: Higher doses (8 to 12 g daily) may be needed for patients with cystic fibrosis (Zobell, 2013) or other infections (Solomkin, 2010).

Surgical (perioperative) prophylaxis (off-label use): IV: 2 g within 60 minutes prior to surgery. Doses may be repeated in 4 hours if procedure is lengthy or if there is excessive blood loss (Bratzler, 2013).


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Mild-to-moderate infections: Infants ≥9 months, Children, and Adolescents: IV: 30 mg/kg/dose every 8 hours; maximum: 120 mg/kg/day (8 g daily)

Moderate-to-severe infections: Infants ≥9 months, Children, and Adolescents: IV: 30 mg/kg/dose every 6 to 8 hours; maximum: 120 mg/kg/day (8 g daily)

Cystic fibrosis: Infants ≥9 months, Children, and Adolescents: IV: 50 mg/kg/dose every 6 to 8 hours (ie, up to 200 mg/kg/day); maximum: 8 g daily. Note: Higher doses (8 to 12 g daily) may be needed for patients with cystic fibrosis (Zobell, 2013).

Surgical (perioperative) prophylaxis (off-label use): Children ≥1 year and Adolescents: IV: 30 mg/kg within 60 minutes prior to surgery (maximum: 2,000 mg per dose). Doses may be repeated in 4 hours if procedure is lengthy or if there is excessive blood loss (Bratzler, 2013).


Dosing: Renal Impairment

IM, IV: Adults: Following initial dose, maintenance doses should be given as follows:

CrCl 10 to 30 mL/minute: 50% of usual dose at the usual interval

CrCl <10 mL/minute: 25% of usual dosage at the usual interval

Intermittent hemodialysis (IHD): Dialyzable (20% to 50%): Loading dose of 500 mg, 1 g, or 2 g, followed by 25% of initial dose at usual interval; for serious/life-threatening infections, administer 12.5% of initial dose after each hemodialysis session (given in addition to the maintenance doses). Alternatively, may administer 500 mg every 12 hours (Heintz, 2009). Note: Dosing dependent on the assumption of 3 times/week, complete IHD sessions.

Peritoneal dialysis (PD): Administer as for CrCl <10 mL/minute (Aronoff, 2007)

Continuous renal replacement therapy (CRRT) (Heintz, 2009; Trotman, 2005): Drug clearance is highly dependent on the method of renal replacement, filter type, and flow rate. Appropriate dosing requires close monitoring of pharmacologic response, signs of adverse reactions due to drug accumulation, as well as drug concentrations in relation to target trough (if appropriate). The following are general recommendations only (based on dialysate flow/ultrafiltration rates of 1 to 2 L/hour and minimal residual renal function) and should not supersede clinical judgment:

CVVH: Loading dose of 2 g followed by 1 to 2 g every 12 hours

CVVHD/CVVHDF: Loading dose of 2 g followed by either 1 g every 8 hours or 2 g every 12 hours (Heintz, 2009)


Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer 's labeling. Use with caution (minor hepatic elimination occurs).


Reconstitution

IM: Reconstitute vial with at least 3 mL SWFI, sterile bacteriostatic water for injection, NS, or bacteriostatic sodium chloride per gram of aztreonam; immediately shake vigorously.

IV:

Bolus injection: Reconstitute vial with 6 mL to 10 mL SWFI; immediately shake vigorously.

Infusion: Reconstitute vial with at least 3 mL SWFI per gram of aztreonam; immediately shake vigorously. Reconstituted solutions are colorless to light yellow straw and may turn pink upon standing without affecting potency. Further dilute in an appropriate solution for infusion to a final concentration ≤2% (ie, final concentration should not exceed 20 mg/mL).


Administration

Injection: Doses >1 g should be administered IV

IM: Administer by deep injection into large muscle mass, such as upper outer quadrant of gluteus maximus or the lateral part of the thigh

IV: Administer by slow IV push over 3 to 5 minutes or by intermittent infusion over 20 to 60 minutes.


Storage

Vials: Prior to reconstitution, store at room temperature; avoid excessive heat. After reconstitution, solutions for infusion in D5W, LR, NS, or other appropriate solution, with a final concentration of ≤20 mg/mL, should be used within 48 hours if stored at room temperature or within 7 days if refrigerated. Solutions for infusion with a final concentration of >20 mg/mL (if prepared with SWFI or NS only) should also be used within 48 hours if stored at room temperature or within 7 days if refrigerated; all other solutions for infusion with a final concentration >20 mg/mL must be used immediately after preparation (unless prepared with SWFI or NS).

Premixed frozen containers: Store unused container frozen at ≤-20 ‚ °C (-4 ‚ °F). Frozen container can be thawed at room temperature of 25 ‚ °C (77 ‚ °F) or in a refrigerator, 2 ‚ °C to 8 ‚ °C (36 ‚ °F to 46 ‚ °F). Thawed solution should be used within 48 hours if stored at room temperature or within 14 days if stored under refrigeration. Do not freeze.


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Intravenous:

Azactam in Dextrose: 1 g (50 mL); 2 g (50 mL) [sodium free]

Solution Reconstituted, Injection:

Azactam: 1 g (1 ea); 2 g (1 ea) [sodium free]

Generic: 1 g (1 ea); 2 g (1 ea)


Compatibility

Solution for infusion: Stable in D5LR, D51/4NS, D51/2NS, D5NS, D5W, D10W, mannitol 5%, mannitol 10%, LR, NS.

Y-site administration: Incompatible with acyclovir, amphotericin B, amphotericin B cholesteryl sulfate complex, amsacrine, anakinra, azithromycin, chlorpromazine, daunorubicin HCl, ganciclovir, lorazepam, metronidazole, mitomycin, mitoxantrone, prochlorperazine edisylate, streptozocin.


Drug Interactions

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Avoid combination

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Consider therapy modification

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. Consider therapy modification


Monitoring Parameters

Injection: Periodic liver function test; monitor for signs of anaphylaxis during first dose


Lab Test Interferences


Test Interactions

May interfere with urine glucose tests containing cupric sulfate (Benedicts solution, Clinitest); positive Coombs' test


Adverse Reactions


>10%:

Hematologic & oncologic: Neutropenia (children 3% to 11%; adults <1%)

Hepatic: Increased serum transaminases (children, high dose: >3 times ULN: 15% to 20%; children, standard dose: increased serum AST 4%, increased serum ALT 7%)

Local: Pain at injection site (children 12%, adults 2%)

1% to 10%:

Cardiovascular: Phlebitis (intravenous: ≤2%), thrombophlebitis (intravenous: ≤2%)

Dermatologic: Skin rash (children 4%, adults ≤1%)

Gastrointestinal: Diarrhea ( ≤1%), nausea ( ≤1%), vomiting ( ≤1%)

Hematologic & oncologic: Eosinophilia (children 6%, adults <1%), thrombocythemia (children 4%, adults <1%)

Local: Erythema at injection site (intravenous: Children 3%, adults <1%), discomfort at injection site (intramuscular: ≤2%), swelling at injection site (intramuscular: ≤2%)

Renal: Increased serum creatinine (children 6%)

Miscellaneous: Fever ( ≤1%)

<1% (Limited to important or life-threatening): Abdominal cramps, anaphylaxis, anemia, angioedema, breast tenderness, bronchospasm, chest pain, Clostridium difficile associated diarrhea, confusion, diaphoresis, diplopia, dizziness, dysgeusia, dyspnea, erythema multiforme, exfoliative dermatitis, flushing, gastrointestinal hemorrhage, hepatitis, hepatobiliary disease, hypotension, increased serum alkaline phosphatase, increased serum ALT (adults), increased serum AST (adults), induration at injection site, insomnia, jaundice, leukocytosis, malaise, myalgia, numbness of tongue, oral mucosa ulcer, pancytopenia, paresthesia, petechia, positive direct Coombs test, prolonged partial thromboplastin time, prolonged prothrombin time, pruritus, pseudomembranous colitis, purpura, seizure, thrombocytopenia, tinnitus, toxic epidermal necrolysis, urticaria, vaginitis, ventricular bigeminy (transient), ventricular premature contractions (transient), vertigo, vulvovaginal candidiasis, weakness, wheezing


Warnings/Precautions


Special Populations: Renal Function Impairment

Serum half-life may be prolonged.


Special Populations: Hepatic Function Impairment

Serum half-life may be prolonged.


Special Populations: Elderly

Serum half-life may be prolonged.


Warnings/Precautions

Concerns related to adverse effects:

- Beta-lactam allergy: Rare cross-allergenicity to penicillins, cephalosporins, or carbapenems may occur; use with caution in patients with a history of hypersensitivity to beta-lactams.

- Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns:

- Renal impairment: Use the injectable formulation with caution in patients with renal impairment; dosing adjustment required.

- Toxic epidermal necrolysis: Use with caution in bone marrow transplant patients with multiple risk factors for toxic epidermal necrolysis (TEN) (eg, sepsis, radiation therapy, drugs known to cause TEN); rare cases of TEN in this population have been reported.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.


Pregnancy Risk Factor

B


Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. Aztreonam crosses the placenta and can be detected in the fetus.


Actions


Pharmacology

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested. Monobactam structure makes cross-allergenicity with beta-lactams unlikely.


Absorption

IM: Well absorbed; IM and IV doses produce comparable serum concentrations


Distribution

Injection: Widely into body tissues, cerebrospinal fluid, bronchial secretions, peritoneal fluid, bile, and bone

Vd: Neonates: 0.26 to 0.36 L/kg; Children: 0.2 to 0.29 L/kg; Adults: 0.2 L/kg

Relative diffusion of antimicrobial agents from blood into CSF: Good only with inflammation (exceeds usual MICs)

CSF:blood level ratio: Meninges: Inflamed: 8% to 40%; Normal: ~1%


Metabolism

Injection: Hepatic (minor %)


Excretion

Injection: Urine (60% to 70% as unchanged drug); feces (~13% to 15%)


Time to Peak

IM, IV push: Within 60 minutes; IV infusion: 1.5 hours


Half-Life Elimination

Injection:

Neonates: <7 days, ≤2.5 kg: 5.5 to 9.9 hours; <7 days, >2.5 kg: 2.6 hours; 1 week to 1 month: 2.4 hours

Children 2 months to 12 years: 1.7 hours

Children with cystic fibrosis: 1.3 hours

Adults: Normal renal function: 1.7 to 2.9 hours

End-stage renal disease: 6 to 8 hours


Protein Binding

56%


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience diarrhea or injection site pain. Have patient report immediately to prescriber signs of Clostridium difficile (C. diff)-associated diarrhea (stomach pain or cramps, very loose or watery stools, or bloody stools) or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes) (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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