Drug information of Grepafloxacin


Grepafloxacin

Drug group:

Grepafloxacin is an oral broad-spectrum quinoline antibacterial agent used to treat bacterial infections. Due to the QTc-prolonging potential, grepafloxacin was withdrawn in the United States.

Mechanism of effect

Grepafloxacin exerts its antibacterial activity by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, essential enzymes for duplication, transcription, and repair of bacterial DNA.

Pharmacodynamic

Grepafloxacin has in vitro activity against a wide range of gram-positive and gram-negative aerobic microorganisms, as well as some atypical microorganisms.

Pharmacokinetics

Absorption: Rapidly and extensively absorbed following oral administration. The absolute bioavailability is approximately 70%.

Protein binding: 50%

Metabolism: Primarily hepatic via CYP1A2 and CYP3A4. The major metabolite is a glucuronide conjugate; minor metabolites include sulfate conjugates and oxidative metabolites. The oxidative metabolites are formed mainly by the cytochrome P450 enzyme CYP1A2, while the cytochrome P450 enzyme CYP3A4 plays a minor role. The nonconjugated metabolites have little antimicrobial activity compared with the parent drug, and the conjugated metabolites have no antimicrobial activity

Half life: 15 ± 3 hours

Dosage

Not available

Interactions

Atomoxetine , Azithromycin , Amitriptyline , Iopamidol , Epirubicin , Adenosine , Erythromycin , Oxaliplatin , Ondansetron , insulin , Imipramine , Betamethasone , Bupropion , Papaverin , Perfenazine , Propafenone , Promethazine , Posaconazole , Pimozide , Tacrolimus , Tetrabenazine , Trazodone , Tramadol , Terbutaline , Trifluoperazine , Triamcinolone , Triptorelin , Trimipramine , Tenofovir , Tizanidine , Thioridazine , Daunorubicin , Desipramine , Deflazacort , Dexamethasone , Doxepin , Doxorubicin , Disopyramide , Repaglinide , Risperidone , Sunitinib , Sertraline , Sotalol , Sorafenib , Sevo flurane , Citalopram , Cisapride , Flutamide , Fludrocortisone , Fluphenazine , Fluoxetine , Fluconazole , Fingolimod , Granisetron , Glimepiride , Lapatinib , Maprotiline , Methadon , Methylprednisolone , Nortriptyline , Nilotinib , Haloperidol , Hydroxyzine , Hydroxychloroquine , Hydrocortisone , Vardenafil , Warfarin , Venlafaxine , Voriconazole , Ketoconazole , Clarithromycin , Chlorpromazine , Clozapine , Clomipramine , Solifenacin , Enzalutamide , Flecainide , Bicalutamide , ritodrine , Leuprolide acetate , escitalopram , Clofazimine , Ranolazine , astemizole , Pentamidine , Quetiapine , lithium , Buprenorphine , Toremifene , Glipizide , Tamoxifen , Metaproternol , Prochlorperazine , Quinidine , Amoxapine , Ziprasidone , Histrelin , rasagiline , propoxyphene , protriptyline , iohexol (Omnipaque) , ISOPROTERENOL , prednisone , cortisone , dronedarone , ritonavir , saquinavir , Mirtazapine , primaquine , Apomorphine , valbenazine , Tolbutamide , glyburide , Tolazamide , Ivabradine , Prednisolone , Mifepristone , Dolasetron , Palonosetron , vandetanib , Lopinavir , Telithromycin , Droperidol , Halothane , Osimertinib , Quinine , Chloroquine , Mesoridazine , Procainamide , Polyethylene glycol , Dicoumarol , Mefloquine , Panobinostat , Ribociclib , Dofetilide , Ibutilide , Eribulin , Inotuzumab‎ , chlorpropamide , Idarubicin , Goserelin , Anagrelide , probucol , Sodium phosphate for bowel , Lumefantrine / artemether , Arsenic trioxide , Efavirenz , EMTRICITABINE , Dolutegravir , Melatonin , Abiraterone , Vasopressin , Halofantrine , Acetohexamide , Triflupromazine , Terfenadine , Metrizamide , Abarelix , Asenapine , Alfuzosin , Paliperidone , Pazopanib , ezogabine , Iloperidone , Perflutren , Pimavanserin , Degarelix , Apalutamide , encorafenib , midostaurin , Triclabendazole , ivosidenib , Crizotinib , Telavancin , Deutetrabenazine , Cabozantinib , Anisindione , Siponimod , gilteritinib , glasdegib , Ceritinib , Nilutamide , rilpivirine , Romidepsin

Alerts

liver disease or

any kind of heart disease or heart problem.

Grepafloxacin may increase the risk of seizures if you have an existing seizure disease.

Points of recommendation

Take grepafloxacin exactly as directed by your doctor.

Take each dose with a full glass of water (8 ounces). Drink several extra glasses of fluid each day to prevent the formation of grepafloxacin crystals in your urine.

Grepafloxacin may be taken with or without food.

Do not take antacids that contain magnesium or aluminum, the ulcer medicine sucralfate or vitamin or mineral supplements that contain iron or zinc for a minimum of 4 hours before or 4 hours after a dose of grepafloxacin. Taking antacids, sucralfate, or vitamin or mineral supplements too close to a dose of grepafloxacin can greatly decrease the effects of the antibiotic.

Take all of the grepafloxacin that has been prescribed for you even if you begin to feel better. Your symptoms may start to improve before the infection is completely treated.

Store this medication at room temperature away from moisture and heat.

Avoid prolonged exposure to sunlight. Grepafloxacin increases the sensitivity of the skin to sunlight, and a severe sunburn may result. If sun exposure is unavoidable, wear protective clothing and use sunscreen. Call your doctor if you experience severe burning, redness, itching, rash, or swelling after exposure to the sun.

Use caution when driving, operating machinery, or performing other hazardous activities. Grepafloxacin may cause dizziness. If you experience dizziness, avoid these activities.

Take the missed dose as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and take only your next regularly scheduled dose. Do not take a double dose of this medication unless otherwise directed by your doctor.

Pregnancy level

Group c - Not adequate studies in pregnant women


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