Mechanism of effect
interferes with microbial DNA synthesis. The bactericidal action of gemifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.
Pharmacodynamic
Gemifloxacin is a quinolone/fluoroquinolone antibiotic. Gemifloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Gemifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Pharmacokinetics
Rapidly absorbed from the GI tract. Bioavailability is approximately 71%. Protein binding ranges from 55% to 73%. Mean Vd ss is 4.18 L/kg. Metabolized to a limited extent by the liver. 61% in the feces and 36% in the urine as unchanged drug and metabolites. The half-lifeis approximately 7 h
Dosage
Usual Adult Dose for Bronchitis 320 mg orally once a day for 5 days Usual Adult Dose for Pneumonia 320 mg orally once a day for 5 or 7 days. Renal Dose Adjustments CrCl 40 mL/min or less: 160 mg orally every 24 hours
Drug contraindications
hypersensitivity to drug or its components. , hypersensitivity to quinolone antibacterialsSide effects
nausea , Headache , Tachycardia , abdominal pain , dizziness , vomiting , rash , Diarrhea , Erythema , Peripheral edema , syncope , hemorrhage , Increased ALT , Increased AST , Anaphylactic reaction , ECG prolonged QT , renal failure , Tendon ruptureInteractions
Pimozide , Tretinoin , MG , Aluminium MG+simeticone , Aluminium MGS , Aluminium gel , ferric carboxymaltose , Zinc , Sucralfate , Magnesium , Magnesium oxide , Calcium , Salbutamol , Sodium bicarbonate , Selenium , Calcium+D3 , Didanosine , prednisone , Dolasetron , vandetanib , sparfloxacin , Dofetilide , Inotuzumab , Iron , Iron polysaccharide , carbonyl iron , Halofantrine , aminolevulinic acid oral , Aminolevulinic acid topical , Acetohexamide , Aluminium Mg , lenvatinib , Entrectinib , Miglitol , cholera vaccine live , Bepridil , bedaquiline , Iron Dextran Complex , vemurafenib , Typhoid vaccine (live), oralAlerts
1-Gemifloxacin has been associated with an increased risk of tendonitis and tendon rupture in patients of all ages. The risk is increased in patients older than 60 yr of age, in patients taking corticosteroids, and in patients with kidney, heart, or lung transplants. 2-Monitor patient's response to therapy
Points of recommendation
1-Administer gemifloxacin 3 h before or 2 h after sucralfate, antacids containing magnesium or aluminum, didanosine chewable buffered tablets or pediatric powder, or other products containing iron or zinc. 2-Administer prescribed dose with a full glass of water. 3-Administer without regard to meals, but administer with food if GI upset occurs. 4-Remind patient to complete entire course of therapy, even if symptoms of infection have disappeared. 5-Caution patient that drug may cause dizziness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined. 6-Advise patient to discontinue therapy and contact health care provider immediately if skin rash, hives, itching, shortness of breath, palpitations, fainting, pain, tenderness, or rupture of tendon occur 7-Inform patient that gemifloxacin may produce prolongation of the QTc interval on an ECG.
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