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- Pharmacology For Fluconazole + Ornidazole + Azithromycin
Fluconazole + Ornidazole + Azithromycin Pharmacology
Fluconazole + Ornidazole + AzithromycinAbout Fluconazole + Ornidazole + AzithromycinN/AMechanism of Action of Fluconazole + Ornidazole + AzithromycinN/APharmacokinets of Fluconazole + Ornidazole + AzithromycinN/AOnset of Action for Fluconazole + Ornidazole + AzithromycinN/ADuration of Action for Fluconazole + Ornidazole + AzithromycinN/AHalf Life of Fluconazole + Ornidazole + AzithromycinN/ASide Effects of Fluconazole + Ornidazole + AzithromycinN/AContra-indications of Fluconazole + Ornidazole + AzithromycinN/ASpecial Precautions while taking Fluconazole + Ornidazole + AzithromycinN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Fluconazole + Ornidazole + AzithromycinN/AInteractions for Fluconazole + Ornidazole + AzithromycinN/ATypical Dosage for Fluconazole + Ornidazole + AzithromycinN/ASchedule of Fluconazole + Ornidazole + AzithromycinN/AStorage Requirements for Fluconazole + Ornidazole + AzithromycinN/AEffects of Missed Dosage of Fluconazole + Ornidazole + AzithromycinN/AEffects of Overdose of Fluconazole + Ornidazole + AzithromycinN/A
FluconazoleAbout FluconazoleA triazole derivative, A board range Antifungal.Mechanism of Action of FluconazoleFluconazole is fungicidal or fungistatic depending on the drug concentrations. I t inhibits the conversion of Lanosterol to 14 demethyl Lanosterol by inhibiting the cytochromeP450 enzyme 14 alpha demethylase and impair ergosterol synthesisPharmacokinets of FluconazoleAbsorption: It is well absorbed after oral administration. Distribution: It is widely distributed in the body. Metabolism: It undergoes insignificant metabolism. Excretion: It is excreted mainly through urine.Onset of Action for FluconazoleN/ADuration of Action for Fluconazole1 dayHalf Life of FluconazoleN/ASide Effects of Fluconazole1.Abdominal pain
8.Alteration in liver enzyme
Contra-indications of Fluconazole1.Hypersensitivity to Fluconazole and other Azole antifungalsSpecial Precautions while taking Fluconazole1. Hepatic dysfunctionPregnancy Related InformationContraindicatedOld Age Related InformationUse with caution.Breast Feeding Related InformationContraindicatedChildren Related InformationCHILDREN below13:Use with caution.
NEONATES:contraindicatedIndications for Fluconazole1.Oesophageal candidiasis
8.Prophylaxis in bone marrow transplantation
9.Candidiasis in immunocompromised individuals
Interactions for FluconazoleCimetidine: Decreased efficacy of fluconazole.
Cyclosporine: Increase in serum cyclosporine plasma concentration.
Hydrochlorothiazide: Reduction in renal clearance of fluconazole.
Phenytoin: Efficacy of phenytoin enhanced.
Rifampicin: Efficacy of fluconazole decreased, higher dosage required.
Sulfonylureas: Efficacy of tolbutamide, glyburide and glipizide increased.
Warfarin: Potentiates the anticoagulant effect resulting in increase in prothrombin time.
Typical Dosage for FluconazoleAdult: 200 - 400 mg once daily
Systemic candidiasis: Maximum dose: 400 mg .The drug should be administered 2 more weeks after resolution of symptoms.
Oropharyngeal candidiasis: Initial dose: 200 mg once daily followed by 100 mg once daily. The drug should be administered at least 14 days after resolution of symptoms.
Oesophageal candidiasis: Initial dose: 200 mg once daily followed by 100 mg once daily and dose can be increased to 400 mg. The drug should be administered at least 14 days after resolution of symptoms.
Cryptococcal Meningitis: : Initial dose: 400 mg once daily followed by 200 mg once daily for 2 - 3 month until CSF culture is negative.
Vaginal candidiasis: 150 mg once daily
Peritonitis: 50 - 200 mg once daily.
Before bone marrow transplantation as prophylaxis:400 mg once daily for several days before transplantation and after 7 days after Neutrophil count rises above 1000 cells per cub.mm.
Candidiasis in immunocompromised individuals: 100 -200 mg once daily.
2 - 8 mg / kg body weight /day
Systemic candidiasis: 6 - 12 mg / kg body weight /day
Oropharyngeal candidiasis: Initial dose: 6 mg / kg body weight / day followed by 3 mg / kg body weight / day. The drug should be administered at least 14 days after resolution of symptoms.
Schedule of FluconazoleN/AStorage Requirements for FluconazoleThe drug should be stored in room temperature. Keep away from moisture and sunlight.Effects of Missed Dosage of FluconazoleTake the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose and continue the regular schedule.Effects of Overdose of FluconazoleGive supportive measures and treatment.
OrnidazoleAbout OrnidazoleA nitro imidazole derivative, Antiprotozoal antibiotic,Antimicrobial.Mechanism of Action of OrnidazoleOrnidazole is a nitro imidazole which has broad spectrum cidal activity against Protozoa and some anaerobic bacteria. Its selective toxicity to anaerobic microbes involves 1. Drug enters the cell by diffusion, 2. Nitro group of drug is reduced by redox proteins present only in anaerobic organisms to reactive nitro radical which excerts cytotoxic action by damaging DNA and other critical biomolecules. 3. DNA helix destabilization &strand breakage has been observed.
Pharmacokinets of OrnidazoleAbsorption: Well absorbed orally, Distribution: Widely distributed,
Metabolism: Metabolized in liver by conjugation, Excretion: Excreted in urine and small portion is excreted in bile
Onset of Action for OrnidazoleWithin 2 hoursDuration of Action for Ornidazole14hoursHalf Life of Ornidazole12 to 14 hoursSide Effects of Ornidazole1.Abdominal pain
12.VertigoContra-indications of Ornidazole1.Hypersensitivity to the drug or other imidazolesSpecial Precautions while taking Ornidazole1.Vertigo
Pregnancy Related InformationUse with caution
First trimester: contra indicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationMay be usedChildren Related InformationUse with cautionIndications for Ornidazole1.Amoebiasis
4.Anaerobic bacterial infections
Interactions for OrnidazoleN/ATypical Dosage for OrnidazoleAmoebiasis:
Adults: 1gm daily in 2 divided doses for 7 to 10 days
Children: 10 to 25mg/kg once daily for 3days
Adults: 1.5gm once daily for 3 days
Children: 40mg/kg once daily for 3 days
Adults: 1.5gm single daily dose or 0.5gm 12hourly for 5 days,
Male partner should be concurrently treated.
Children: 25mg/kg as a single dose
Adults: 1 to 1.5gm once daily for 2days
Children: 40mg/kg for 2days
Bacterial vaginosis: 1.5gm once or 500mg once daily for 5 to7 days
Schedule of OrnidazoleHStorage Requirements for OrnidazoleStore at cool dry place. Protect from heat and light. Keep out of the reach of children.Effects of Missed Dosage of OrnidazoleTake the missed dose as soon as noticed. If it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.Effects of Overdose of OrnidazoleTreatment is supportive & symptomatic. Drug is removed by induced emesis, gastric lavage, and administration of activated charcoal &use of cathartics.
AzithromycinAbout AzithromycinAn Azalide, macrolide antibiotic.
Mechanism of Action of AzithromycinAzithromycin is a member of macrolide antibiotic. It binds to the 50S sub unit of bacterial ribosome and inhibits translocation.ie: they: interfere with the transfer of the newly formed peptide chain from the A site to the P site and fails to expose the A site .So that A site is unable to bind with the next aminoacyl t RNA complex. This leads to premature termination of amino acid chain and there by inhibits protein synthesis.Azithromycin is active against both gram positive and gram negative aerobic and anaerobic bacteriaPharmacokinets of AzithromycinAbsorption: Azithromycin is completely absorbed after oral administration. Distribution: It is widely distributed in the body .Metabolism: It is not metabolized in the body. Excretion: It is primarily excreted through bile and a very small amount excreted through urine.Onset of Action for Azithromycin1-2 hours.Duration of Action for AzithromycinN/AHalf Life of Azithromycin68 hourSide Effects of Azithromycin1. Nausea
Contra-indications of Azithromycin1.Hypersensitivity to Azithromycin and other macrolideSpecial Precautions while taking Azithromycin1.Renal impairment
Pregnancy Related InformationUse with caution.Old Age Related InformationUse with caution.Breast Feeding Related InformationUse with caution.Children Related InformationUse with cautionIndications for Azithromycin1.Pneumonia
9.Prevention of disseminated Mycobacterium avium complex infection
14.Skin and soft tissue infections
Interactions for AzithromycinAluminium & Magnesium containing Antacids: Decrease peak serum levels.
Theophylline: Serum concentration of Theophylline increased.
Warfarin: Anticoagulant effects enhanced.
Digoxin & Cyclosporine: Increase in their serum concentration.
Carbamazepine: Toxicity occurs which may require hospitalization.
Triazolam: Increases serum levels of Triazolam leading to toxicity.
Ergot Alkaloids: Acute ergotism manifested as peripheral ischaemia.
Food: Absorption reduced by as much as 52% (should be taken 1 hr before or 2 hrs after meal).
Typical Dosage for AzithromycinAdult:
500 mg once daily for 1 day followed by 250 mg once daily for 4 days.
For the treatment of urethritis and cervicitis: 1 - 2 g as a single dose
Prophylaxis of MAC: 1200 mg once weekly
Chancroid: 1000 mg as a single dose
Children: 10 mg / kg body weight once daily on 1 day followed by 5 mg / kg body weight once daily for 4 days.
Schedule of AzithromycinHStorage Requirements for AzithromycinStore in a cool dark place. Keep away from heat and moisture.Effects of Missed Dosage of AzithromycinTake the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose.Effects of Overdose of AzithromycinGive supportive measures and symptomatic treatment
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