Flucloxacillin (Floxacillin)

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Induces
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Floxapen; Belgium: Floxapen, Staphycid; Denmark: Heracillin; Germany: Fluclox, Flucloxa, Flucloxacillin, Staphylex; Greece: Floxapen; Ireland: Floxapen, Flucillin, Fuclon, Flucloxacillin, Geriflox; Italy: Cloxillin, Fareclox, Flucacid, Flucef, Flucinal, Flucloxacillina, Flucox, Fluxacil, Liderclox, Nepenic, Pantaflux, Recaflux; Malta: Floxapen, Ramaxir; Netherlands: Floxapen, Flucloxacilline; Portugal: Floxapen, Flucloxacilina; Sweden: Flukloxacillin, Heracillin; UK: Floxapen, Flucloxacillin.

Latin America

Mexico: Floxapen T-5.

Drug combinations

Flucloxacillin and Amoxicillin

Chemistry

Flucloxacillin: C~19~H~17~ClFN~3~O~5~S. Mw: 453.87. (1) 4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[[[3-(2-chloro-6-fluorophenyl)-5-methyl-7-oxo-, [2S(2α, 5α, 6β)]; (2) 6-[3-(2-Chloro-6-fluorophenyl)-5-methyl-4-isoxazolecarboxamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid. CAS-5250-39-5 (1972).

Pharmacologic Category

Antibacterials; Penicillinase-resistant Penicillins. (ATC-Code: J01CF05).

Mechanism of action

Bactericidal activity of flucloxacillin results from inhibition of cell wall synthesis, mediated through flucloxacillin binding to penicillin-binding proteins.

Therapeutic use

Indicated for treatment of infections due to sensitive Gram-positive organisms, including β-lactamase-producing Staphylococci and Streptococci. Specific approved indications include: staphylococcal skin infections and cellulitis, including impetigo, otitis externa, folliculitis, boils, carbuncles, and mastitis, pneumonia, osteomyelitis, septic arthritis, septicemia, and empirical treatment for endocarditis. Flucloxacillin also indicated for use as prophylactic agent during major surgical procedures (e.g. cardiothoracic and orthopedic surgery) when appropriate.

Pregnancy and lactiation implications

Use in pregnancy or lactation only when potential benefits outweigh potential risks associated with treatment.

Unlabeled use

Contraindications

Flucloxacillin should not be given in history of hypersensitivity to β-lactam antibiotics (e.g. penicillins, cephalosporins) or excipients. Contraindicated in previous history of flucloxacillin-associated jaundice/hepatic dysfunction.

Warnings and precautions

Before initiating therapy with flucloxacillin, investigate previous hypersensitivity reactions to β-lactams. Serious and occasionally fatal hypersensitivity reactions (anaphylaxis) reported in patients receiving β-lactam antibiotics. Although anaphylaxis is more frequent following parenteral therapy, it has occurred in patients on oral therapy (these reactions are more likely to occur in history of β-lactam hypersensitivity). Use with caution in evidence of hepatic dysfunction, patients >50 years of age and those with serious underlying disease. In these patients, hepatic events may be severe, and in very rare circumstances, deaths reported. Prolonged use may occasionally result in overgrowth of non-susceptible organisms. Flucloxacillin capsules contain approximately 51 mg sodium per g. This should be included in daily allowance of patients on sodium-restricted diets.

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