ceftaroline

Action and Spectrum

Actions and Spectrum:

ceftaroline is a broad-spectrum antibiotic in the cephalosporin class that is used to treat various bacterial infections. It has activity against both gram-positive and gram-negative bacteria, including resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA) and penicillin-resistant Streptococcus pneumoniae.

The mechanism of action of ceftaroline is similar to other cephalosporins, where it interferes with the synthesis of the bacterial cell wall, leading to cell death. However, ceftaroline has some unique structural features that allow it to bind to penicillin-binding protein 2a (PBP2a), a protein that is responsible for the resistance of MRSA to beta-lactam antibiotics.

Drug Interaction

Adverse Reaction

Frequency defined

1-10%

Nausea (4%)

Diarrhea (5%)

Rash (3%)

Vomiting (2%)

Constipation (2%)

Increased transaminases (2%)

Phlebitis (2%)

Hypokalemia (2%)

Black Box Warning

Black Box Warning:

black box warning for ceftaroline due to the risk of allergic reactions, including anaphylaxis, which can be life-threatening.

Contraindication / Caution

Contraindication / Caution:

Allergy: Ceftaroline should not be used in individuals who have a known allergy to cephalosporin antibiotics or any of the other ingredients in ceftaroline.

Renal Impairment: Dose adjustment is necessary in patients with moderate or severe renal impairment, as ceftaroline is primarily eliminated through the kidneys.

Coagulation Disorders: Ceftaroline may increase the risk of bleeding in patients with coagulation disorders or receiving anticoagulant therapy.

Pregnancy and Breastfeeding: Ceftaroline is classified as pregnancy category B, which means it is generally safe to use during pregnancy. However, it should only be used during pregnancy if clearly needed. Ceftaroline is excreted in breast milk, and caution should be exercised when administering ceftaroline to breastfeeding mothers.

Clostridioides difficile Infection: The use of ceftaroline may increase the risk of developing Clostridioides difficile-associated diarrhea (CDAD). If diarrhea develops during or after treatment with ceftaroline, the patient should be evaluated for CDAD.

Pregnancy / Lactation

Pregnancy consideration: N/A

Lactation: N/A

Pregnancy category:

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women.
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women.
• Category N: There is no data available for the drug under this category.

Pharmacology

Pharmacology:

ceftaroline is a semisynthetic cephalosporin antibiotic that has been developed for the treatment of bacterial infections. It works by inhibiting the synthesis of the bacterial cell wall, which leads to bacterial death.

Pharmacodynamics:

ceftaroline works by inhibiting the synthesis of bacterial cell walls through binding to and inhibiting the activity of the penicillin-binding proteins (PBPs), which are enzymes responsible for cell wall synthesis. ceftaroline has a unique mechanism of action compared to other cephalosporins in that it has activity against MRSA (Methicillin-resistant Staphylococcus aureus) due to its increased affinity for PBPs that have low affinity for other cephalosporins.

Pharmacokinetics:

Absorption

ceftaroline is administered intravenously, and it is not available in an oral formulation. The drug is rapidly and completely absorbed following intravenous administration.

Distribution

The volume of distribution (Vd) of ceftaroline is approximately 14 liters, indicating that the drug is distributed throughout the extracellular fluid compartment. The protein binding of ceftaroline is moderate, with approximately 20% to 25% of the drug bound to plasma proteins.

Metabolism

ceftaroline is primarily metabolized via enzymatic hydrolysis of the prodrug ester linkage to the active metabolite ceftaroline M1. This process is primarily mediated by carboxylesterases, which are widely distributed in the body. Ceftaroline is not metabolized by the cytochrome P450 system.

Elimination and excretion

The elimination half-life (t1/2) of ceftaroline is approximately 2.5 hours, and the drug is primarily eliminated unchanged in the urine via glomerular filtration and active tubular secretion. Approximately 88% of the dose is excreted in the urine, with the remainder eliminated in the feces.

Adminstartion

Administration:

ceftaroline is a cephalosporin antibiotic that is used to treat bacterial infections. It is administered intravenously (IV) and must be prepared and given by a healthcare professional.

The dosage of ceftaroline varies depending on the severity and type of infection, as well as the patient’s age, weight, and overall health. It is typically given every 12 hours for a duration of 5 to 14 days, depending on the infection being treated.

Patient Information Leaflet

Patient information leaflet

Generic Name: ceftaroline

Why do we use ceftaroline?

ceftaroline is a cephalosporin antibiotic that is used to treat bacterial infections. It works by inhibiting the growth and spread of bacteria, which helps the body’s immune system to fight the infection.

ceftaroline is primarily used to treat skin and soft tissue infections caused by certain types of bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and Streptococcus pneumoniae. It may also be used to treat community-acquired pneumonia and acute bacterial skin and skin structure infections.