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Loracarbef

Drug Nomenclature

Synonyms: KT-3777; LY-163892; Loracarbef; Loracarbefum; Lorakarbef; Lorakarbefi
BAN: Loracarbef
USAN: Loracarbef
INN: Loracarbef [rINN (en)]
INN: Loracarbef [rINN (es)]
INN: Loracarbef [rINN (fr)]
INN: Loracarbefum [rINN (la)]
INN: Лоракарбеф [rINN (ru)]
Chemical name: (6R,7S)-3-Chloro-8-oxo-7-d-phenylglycylamino-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid monohydrate
Molecular formula: C16H16ClN3O4,H2O =367.8
CAS: 76470-66-1 (anhydrous loracarbef); 121961-22-6 (loracarbef monohydrate)
ATC code: J01DC08
Loracarbef

Pharmacopoeias in US

pH of a 10% suspension in water is between 3.0 and 5.5. Store in airtight containers.

Adverse Effects and Precautions

Adverse effects of loracarbef are generally similar to those of other beta lactams (see Benzy (penicillin, and Cefalotin). They include gastrointestinal disturbances, particularly diarrhoea, and hypersensitivity reactions such as skin rashes. Increases in liver enzymes and abnormalities in haematological parameters have been reported. Loracarbef should not be given to patients known to be hypersensitive to it or to other beta lactams because of the possibility of cross-sensitivity. It should be given with caution, with appropriate dosage reduction, in patients with renal impairment.

Interactions

Probenecid decreases the renal excretion of loracarbef thereby increasing its plasma concentrations.

Antimicrobial Action

Loracarbef is bactericidal with antibacterial activity similar to that of cefaclor.

Pharmacokinetics

Loracarbef is well absorbed from the gastrointestinal tract with a bioavailability of 90%. Peak plasma concentrations after 200-and 400-mg doses as capsules are about 8 and 14micrograms/mL respectively at 1.2 hours. Peak concentrations are achieved more rapidly after an oral suspension and a paediatric dose of 15 mg/kg produces a concentration of about 19 micrograms/mL within 40 to 60 minutes. Absorption is delayed by the presence of food. A plasma half-life of about 1 hour has been reported which is prolonged in renal impairment. About 25% is bound to plasma proteins. Loracarbef is excreted largely unchanged in the urine, and therapeutic concentrations are maintained in the urine for up to 12 hours. Probenecid delays excretion. Loracarbef is removed by haemodialysis.

Uses and Administration

Loracarbef is an oral carbacephem antibiotic. The carbacephems are closely related to the cephalosporins, but replacement of the sulfur atom in the 7-aminocephalosporanic acid nucleus by a methylene group is said to enhance stability. It is used similarly to cefaclor in the treatment of susceptible infections of the respiratory and urinary tracts and of skin and soft tissue. For details of these infections and their treatment, see under Choice of Antibacterial, p. 162. Loracarbef should be given 1 hour before food or on an empty stomach. Loracarbef is given as the monohydrate. Doses are expressed in terms of the equivalent amount of anhydrous loracarbef. The usual adult dose is 200 to 400 mg every 12 hours. In uncomplicated urinary-tract infections, a dose of 200 mg daily may be adequate. A dose for children is 7.5 mg/kg every 12 hours for uncomplicated infections or 15 mg/kg every 12 hours for acute otitis media or acute maxillary sinusitis. For details of reduced doses of loracarbef in patients with renal impairment, see below.

Administration in renal impairment

Doses of loracarbef should be reduced in patients with renal impairment; patients with a creatinine clearance of 10 to 49 mL/minute may be given half the usual dose at the usual dosage interval or the full usual dose at twice the usual interval; patients with a creatinine clearance of less than 10 mL/minute may be treated with the usual dose given every 3 to 5 days. Patients on haemodialysis should receive another dose following dialysis.

Preparations

The United States Pharmacopeia 31, 2008: Loracarbef Capsules; Loracarbef for Oral Suspension.

Proprietary Preparations

Germany; Lorafem; Greece: Lorbe; Mexico: Carbac; Lorabid; South Africa: Lorabid; Sweden: Lorabid; Turkey: Lorabid; United States of America (USA): Lorabid.

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