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Generic Name: Ceftaroline Fosamil
Class: Fifth Generation Cephalosporins
VA Class: AM119
Chemical Name: 4 - [2 - [[(6R,7R) - 2 - Carboxy - 7 - [[(2Z) - (ethoxyimino)[5 - (phosphonoamino) - 1,2,4 - thiadiazol - 3 - yl]acetyl]amino] - 8 - oxo - 5 - thia - 1 - azabicyclo[4.2.0]oct - 2 - en - 3 - yl]thio] - 4 - thiazolyl] - 1 - methyl - pyridinium, inner salt, monoacetate, monohydrate
Molecular Formula: C22H21N8O8PS4.C2H4O2.H2O
CAS Number: 866021-48-9


Antibacterial; β-lactam antibiotic;1 5 6 7 fifth generation cephalosporin.5 6 7 8 27

Uses for Teflaro

Community-acquired Pneumonia

Treatment of community-acquired bacterial pneumonia (CABP, CAP) caused by susceptible Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible [oxacillin-susceptible] strains only), Haemophilus influenzae, Klebsiella pneumoniae, K. oxytoca, or Escherichia coli.1 3

Skin and Skin Structure Infections

Treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible S. aureus (including methicillin-resistant S. aureus [MRSA; also known as oxacillin-resistant S. aureus, ORSA], S. pyogenes (group A β-hemolytic streptococci), S. agalactiae (group B streptococci), E. coli, K. pneumoniae, or K. oxytoca.1 2

Teflaro Dosage and Administration


Administer by IV infusion.1

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Do not admix with or add to solutions containing other drugs.1

Reconstitution and Dilution

Reconstitute 400- or 600-mg single-use vials of ceftaroline fosamil by adding 20 mL of sterile water for injection, 0.9% sodium chloride, 5% dextrose, or lactated Ringer's injection to provide solution containing approximately 20 or 30 mg/mL, respectively.1 Mix vial gently to ensure complete dissolution;1 reconstitution should take <2 minutes.1

Dilute appropriate dose of reconstituted solution in 50–250 mL of the same diluent used for reconstitution, unless drug was reconstituted with sterile water, in which case any compatible IV infusion solution (see Solution Compatibility under Stability) should be used for further dilution.1 When using a 50-mL infusion bag, remove 20 mL of diluent from bag prior to injecting entire reconstituted contents of 400- or 600-mg vial, to provide infusion solution containing approximately 8 or 12 mg/mL, respectively.1

Reconstituted and diluted solutions appear clear and light to dark yellow.1

Final solution in IV infusion bag should be used within 6 hours when stored at room temperature or within 24 hours when stored in refrigerator at 2–8°C.1

Rate of Administration

Administer by IV infusion over approximately 1 hour.1


Available as ceftaroline fosamil monoacetate monohydrate; dosage expressed in terms of anhydrous ceftaroline fosamil.1


Community-acquired Pneumonia

600 mg every 12 hours for 5–7 days.1

Duration depends on site and severity of infection and patient’s clinical and bacteriologic progress.1

Skin and Skin Structure Infections

600 mg every 12 hours for 5–14 days.1

Duration depends on site and severity of infection and patient’s clinical and bacteriologic progress.1

Special Populations

Hepatic Impairment

Manufacturer makes no specific dosage recommendations;1 hepatic impairment not expected to have a clinically important effect on systemic clearance of the drug.1

Renal Impairment

Adjust dosage in adults with Clcr ≤50 mL/minute, including those undergoing hemodialysis.1 (See Table 1.)

Table 1. Dosage for Adults with Renal Impairment1

Clcr (mL/min)

Recommended Dosage


400 mg every 12 h


300 mg every 12 h

<15 or receiving hemodialysis

200 mg every 12 h; on hemodialysis days, give dose after hemodialysis

Geriatric Patients

Dosage adjustment not required based on age; may be required based on age-related changes in renal function.1 (See Renal Impairment under Dosage and Administration.)

Cautions for Teflaro


  • Known hypersensitivity to ceftaroline or other cephalosporins.1 (See Sensitivity Reactions under Cautions.)


Sensitivity Reactions

Hypersensitivity Reactions

Serious, sometimes fatal, anaphylactic reactions and serious skin reactions reported in patients receiving β-lactam antibiotics.1 Anaphylaxis and anaphylactoid reactions have been reported with ceftaroline.1

Discontinue drug if hypersensitivity occurs.1 Serious acute hypersensitivity (e.g., anaphylaxis) reactions require emergency treatment (e.g., epinephrine, airway management, oxygen, IV fluids, antihistamines, corticosteroids, vasopressors) as clinically indicated.1


Partial cross-sensitivity occurs among β-lactam antibiotics.1 27

Prior to initiation of therapy, make careful inquiry concerning previous hypersensitivity reactions to ceftaroline, other cephalosporins, penicillins, or carbapenems.1 Contraindicated in patients hypersensitive to the drug or other cephalosporins; use with caution in those allergic to penicillin or other β-lactams.1

Clostridium difficile-associated Diarrhea and Colitis (CDAD)

Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile.1 12 13 14 15 16

C. difficile infection (CDI) and C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) have been reported with nearly all systemic anti-infectives, including ceftaroline, and may range in severity from mild diarrhea to fatal colitis.1 12 13 14 15 16 C. difficile produces toxins A and B which contribute to development of CDAD;1 13 12 hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.1

Consider CDAD if diarrhea develops during or after anti-infective therapy and manage accordingly.1 12 13 14 15 16 Obtain a careful medical history since CDAD may occur as late as 2 months or longer after anti-infective therapy is discontinued.1

If CDAD is suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible.1 12 14 15 16 Initiate appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.1 12 13 14 15 16

Hematologic Effects

Seroconversion from negative to positive direct antiglobulin (Coombs’) tests reported in approximately 11% of patients receiving ceftaroline in phase 3 clinical trials; no evidence of hemolytic anemia in these patients.1

Consider drug-induced hemolytic anemia in patients who develop anemia during or after ceftaroline treatment; perform diagnostic studies, including direct antiglobulin test.1 If drug-induced hemolytic anemia is suspected, consider discontinuing ceftaroline and administer supportive treatment (e.g., transfusion) as clinically indicated.1

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of ceftaroline and other antibacterials, use only for treatment of infections proven or strongly suspected to be caused by susceptible bacteria.1

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.1 In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.1

Specific Populations


Category B.1


Not known whether distributed into milk.1 Use caution.1

Pediatric Use

Safety and efficacy not established in patients <18 years of age.1

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.1

Substantially eliminated by kidneys; consider age-related decreases in renal function, select dosage with caution, and consider monitoring renal function.1 (See Renal Impairment under Dosage and Administration.)

Hepatic Impairment

Pharmacokinetics not established; systemic clearance not expected to be altered by hepatic impairment.1

Renal Impairment

Dosage adjustments necessary in adults with Clcr ≤50 mL/minute, including those undergoing hemodialysis.1 (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

GI effects (diarrhea,1 25 nausea,1 25 vomiting,1 constipation1 ), headache,25 rash,1 25 pruritus,25 hypokalemia,1 increased transaminases,1 25 phlebitis.1

Interactions for Teflaro

Does not inhibit CYP1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4 in vitro; does not induce CYP1A2, 2B6, 2C8, 2C9, 2C19, or 3A4/5.1 Pharmacokinetic interactions with drugs metabolized by these isoenzymes unlikely.1

No formal drug interaction studies to date.1

Specific Drugs




Amikacin: In vitro evidence of synergistic antibacterial effects against E. coli and K. pneumoniae that produce extended-spectrum β-lactamases (ESBL-producing), AmpC-derepressed Enterobacter cloacae, and Pseudomonas aeruginosa;22 no evidence of antagonism1 22


In vitro evidence of indifferent antibacterial effects against ESBL-producing E. coli and K. pneumoniae, AmpC-derepressed E. cloacae, and Ps. aeruginosa;22 no evidence of synergism22 or antagonism1 22


Meropenem: In vitro evidence of synergistic antibacterial effects against ESBL-producing E. coli and indifferent antibacterial effects against ESBL-producing K. pneumoniae, AmpC-derepressed E. cloacae, and Ps. aeruginosa;22 no evidence of antagonism1 22

Other anti-infectives

No in vitro evidence of antagonism between ceftaroline and azithromycin, daptomycin, levofloxacin, linezolid, tigecycline, or vancomycin1

Teflaro Pharmacokinetics


Ceftaroline is administered as ceftaroline fosamil, a prodrug that is inactive until converted in vivo to ceftaroline by a plasma phosphatase.1 4

Plasma Concentrations

In healthy adults, peak plasma concentrations and AUC increase approximately in proportion to dose following single IV doses of 50–1000 mg of ceftaroline fosamil.1

No appreciable accumulation reported when 600-mg doses are given by IV infusion over 1 hour every 12 hours for up to 14 days in adults with normal renal function.1

Special Populations

In healthy adolescents 12–17 years of age, peak plasma concentrations and AUC after a single 8-mg/kg IV dose (600 mg in those weighing >75 kg) are 10 and 23% lower, respectively, compared with healthy adults who received a single 600-mg IV dose.1



Limited data available regarding tissue distribution; animal data indicate ceftaroline is distributed into kidneys, skin, and lungs.4 9

Not known whether distributed into milk.1

Plasma Protein Binding

Approximately 20%;1 decreases slightly with increasing concentrations >1–50 mcg/mL.1



Ceftaroline fosamil is rapidly converted in vivo to ceftaroline by a plasma phosphatase, principally during IV infusion.1 4 In addition, the β-lactam ring of ceftaroline is hydrolyzed to an inactive, open-ring metabolite (ceftaroline M-1).1

Ceftaroline is not a substrate of CYP isoenzymes.1

Elimination Route

Ceftaroline and its metabolites principally eliminated in urine by glomerular filtration.1 Following a single 600-mg IV dose of ceftaroline fosamil, approximately 88% is eliminated in urine (approximately 64% as unchanged drug, and 2% as ceftaroline M-1) and 6% is eliminated in feces within 48 hours.1

Removed by hemodialysis.1


Adults: 2.7 hours.1

Special Populations

Pharmacokinetics in patients with hepatic impairment not established.1

AUC and half-life increased in patients with renal impairment.1 4




Powder for IV Infusion

2–8°C.1 May be stored at room temperature (≤25°C) for ≤7 days.1

Following reconstitution and dilution, may be stored in IV infusion bag for up to 6 hours at room temperature or up to 24 hours when refrigerated at 2–8°C.1


For information on systemic interactions resulting from concomitant use, see Interactions.


Solution Compatibility1 HID


Dextrose 2.5 or 5% in water

Ringer’s injection, lactated

Sodium chloride 0.45 or 0.9%

Drug CompatibilityHID
Y-Site Compatibility


Acyclovir sodium

Amikacin sulfate


Amiodarone HCl



Calcium chloride

Calcium gluconate


Cisatracurium besylate

Clindamycin phosphate



Dexamethasone sodium phosphate


Diltiazem HCl

Diphenhydramine HCl

Dopamine HCl



Esomeprazole sodium


Fentanyl citrate



Gentamicin sulfate

Granisetron HCl

Haloperidol lactate

Heparin sodium

Hydrocortisone sodium succinate

Hydromorphone HCl

Hydroxyzine HCl

Insulin, regular


Lidocaine HCl



Meperidine HCl

Methylprednisolone sodium succinate

Metoclopramide HCl

Metoprolol tartrate


Midazolam HCl

Milrinone lactate

Morphine sulfate

Moxifloxacin HCl


Norepinephrine bitartrate

Ondansetron HCl

Pantoprazole sodium

Potassium chloride

Promethazine HCl


Ranitidine HCl

Remifentanil HCl

Sodium bicarbonate

Tobramycin sulfate




Amphotericin B

Caspofungin acetate



Labetalol HCl

Potassium phosphates

Sodium phosphates


Dobutamine HCl

Magnesium sulfate

Actions and Spectrum

  • Based on spectrum of activity, classified as a fifth generation cephalosporin.5 6 7 8 27

  • Like third and fourth generation cephalosporins, ceftaroline has an expanded spectrum of activity that includes both gram-positive and gram-negative bacteria.4 5 6 7 17 21 27 Unlike first, second, third, and fourth generation cephalosporins, ceftaroline has activity against methicillin-resistant S. aureus (MRSA; also known as oxacillin-resistant Staphylococcus aureus, ORSA).4 5 6 7 17 27

  • Usually bactericidal.1 4 17 22

  • Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.1

  • Spectrum of activity includes many gram-positive and gram-negative aerobic bacteria1 4 17 18 19 20 21 24 27 and some anaerobic bacteria.23

  • Gram-positive aerobes: Active in vitro against S. aureus (including MRSA, vancomycin-resistant S. aureus [VRSA], and daptomycin-nonsusceptible S. aureus),1 4 17 21 24 27 coagulase-negative staphylococci (including methicillin-resistant [oxacillin-resistant] strains),4 21 27 Streptococcus pneumoniae (including penicillin- or cefotaxime-resistant S. pneumoniae or multidrug-resistant S. pneumoniae [MDRSP]),1 4 18 19 20 21 24 27 S. pyogenes (group A β-hemolytic streptococci),1 4 21 27 S. agalactiae (group B streptococci),1 4 21 27 viridans streptococci,4 21 27 and S. dysgalactiae.1 Has only limited activity against Enterococcus faecalis; E. faecium are resistant.4 21

  • Gram-negative aerobes: Active in vitro against Escherichia coli,1 21 27 Klebsiella pneumoniae,1 21 27 K. oxytoca,1 and Haemophilus influenzae (including β-lactamase-producing strains).1 4 21 27 Also active in vitro against Citrobacter koseri,1 C. freundii,1 21 27 Enterobacter cloacae,1 21 27 E. aerogenes,1 27 Moraxella catarrhalis (including β-lactamase-producing strains),1 4 21 27 Morganella morganii,1 21 Pasteurella multocida,21 Proteus mirabilis,1 21 27 and H. parainfluenzae.1 Inactive against Pseudomonas aeruginosa4 27 .

  • Gram-negative bacteria that produce extended-spectrum β-lactamases (ESBLs) from the TEM, SHV or CTX-M families, AmpC cephalosporinases, class B metallo-β-lactamases, or serine carbapenemases are resistant.1 4 21 27

  • Although cross-resistance may occur between ceftaroline and other cephalosporins, some bacteria resistant to other cephalosporins may be susceptible to ceftaroline.1

Advice to Patients

  • Advise patients that antibacterials (including ceftaroline) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold).1

  • Importance of completing full course of therapy, even if feeling better after a few days.1

  • Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with ceftaroline or other antibacterials in the future.1

  • Advise patients that diarrhea is a common problem caused by anti-infectives and usually resolves when the drug is discontinued.1 Importance of contacting a clinician if watery or bloody diarrhea occurs.1

  • Importance of informing clinicians of prior hypersensitivity reactions to ceftaroline, other cephalosporins, other β-lactam antibiotics, or other allergens.1 Importance of discontinuing the drug and immediately informing clinician if an allergic or hypersensitivity reaction occurs.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Ceftaroline Fosamil


Dosage Forms


Brand Names



For injection, for IV infusion

400 mg



600 mg



AHFS DI Essentials. © Copyright, 2016, American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814. Review Date: September 06, 2016.


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