Ceftaroline fosamil

Drug #2251

Ceftaroline fosamil is broad-spectrum, prodrug antibacterial of cephalosporin class of beta-lactams (ß-lactams). Chemically, the prodrug, ceftaroline fosamil monoacetate monohydrate is (6R,7R)-7-{(2Z)-2-(ethoxyimino)-2-[5- (phosphonoamino)-1,2,4 thiadiazol-3-yl]acetamido}-3-{[4-(1- methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl}8-oxo-5- thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate monoacetate monohydrate. The empirical formula is C22H21N8O8PS4•C2H4O2•H2O.

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Primary Characteristics

It is of Semi Synthetic origin and belongs to Cepahalosporin.

It belongs to Antibiotic (Cell Wall) pharmacological group on the basis of mechanism of action.

Molecular Weight: 762.75 · Non-proprietary name: Ceftaroline fosamil.

Molecular structure of Ceftaroline fosamil

Pharmacokinetics

Distribution: Ceftaroline fosamil has a volume of distribution is 20.3 L (18.3-21.6 L). plasma protein binding is 20%.

Elimination: it is metabolised via by phosphatase enzymes & inactivated by hydrolysis, plasma half-life is 1.60 hour, renal excretion is 88%, 8% in urine and feces.

Indications

Ceftaroline fosamil is primarily indicated in conditions like Bacterial skin infections, Community acquired pneumonia.

Contraindications

Ceftaroline fosamil is contraindicated in conditions like Hypersensitivity to any component of product.

Dosage

Ceftaroline fosamil's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
200 mg	200 mg	Every 12h	IV infusion	(For patient with end-stage renal disease (ESRD), including hemodialysis) IV infusion administered over 1 hour. Constitution time is less than 2 minutes. Mix gently and check that the content has dissolved.
300 mg	300 mg	Every 12h	IV infusion	(For patient with creatinine clearance 15-30 ml/min) IV infusion administered over 1 hour
400 mg	400 mg	Every 12h	IV infusion	(For patient with creatinine clearance 30-50 mL/min ) IV infusion administered over 1 hour
600 mg	600 mg	Every 12h	IV infusion	(For patient with normal renal function) IV infusion administered over 1 hour in adults = 18 years of age
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

None recorded.

Side Effects

Ceftaroline fosamil in overdosage may give rise to further complications which include Hepatitis , Renal failure , Hypersensitivity.

Ceftaroline fosamil is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Anaphylaxis, Anemia, Constipation , Convulsions , Diarrhea, Dizziness, esinophilia, Hepatitis, Hyperglycemia, hyperkalemia, Nausea, Neutropenia, Palpitation, Pyrexia , Rashes , Tachycardia, Thrombocytopenia, Urticaria, Vomiting .

Warnings / Precautions

Exercise caution in patients with known hypersensitivity to beta-lactam antibiotics. Clostridium difficile-associated diarrhea (CDAD) has been reported with nearly all systemic antibacterial agents, including Ceftaroline fosamil. Evaluate if diarrhea occurs. If anemia develops during or after therapy, a diagnostic workup for drug-induced hemolytic anemia should be performed and consideration given to its discontinuation . Use with caution in nursing mother.

Available Brands

None recorded.

Storage Conditions

Ceftaroline fosamil should be stored Injection.

Drug Classification

1.6.2.1.3 — Cephalosporins