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- Pharmacology For Metronidazole + Nalidixic Acid
Metronidazole + Nalidixic Acid Pharmacology
Metronidazole + Nalidixic AcidAbout Metronidazole + Nalidixic AcidN/AMechanism of Action of Metronidazole + Nalidixic AcidN/APharmacokinets of Metronidazole + Nalidixic AcidN/AOnset of Action for Metronidazole + Nalidixic AcidN/ADuration of Action for Metronidazole + Nalidixic AcidN/AHalf Life of Metronidazole + Nalidixic AcidN/ASide Effects of Metronidazole + Nalidixic AcidN/AContra-indications of Metronidazole + Nalidixic AcidN/ASpecial Precautions while taking Metronidazole + Nalidixic AcidN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Metronidazole + Nalidixic AcidN/AInteractions for Metronidazole + Nalidixic AcidN/ATypical Dosage for Metronidazole + Nalidixic AcidN/ASchedule of Metronidazole + Nalidixic AcidN/AStorage Requirements for Metronidazole + Nalidixic AcidN/AEffects of Missed Dosage of Metronidazole + Nalidixic AcidN/AEffects of Overdose of Metronidazole + Nalidixic AcidN/A
MetronidazoleAbout MetronidazoleA nitroimidazole antibiotic, Anti-infective, Antiprotozoal,amebicide.Mechanism of Action of MetronidazoleMetronidazole is nitro imidazoles which have 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 exerts cytotoxic action by damaging DNA and other critical biomolecules. 3. DNA helix destabilization & strand breakage has been observed.Pharmacokinets of MetronidazoleAbsorption: Well absorbed orally, Distribution: Widely distributed,
Metabolism: Metabolized in liver by oxidation & glucuronide conjugation, Excretion: Excreted in urine.
Onset of Action for Metronidazole1 to 2 daysDuration of Action for Metronidazole8hours.Half Life of Metronidazole8 hours.Side Effects of Metronidazole1.Anorexia.
7.Looseness of stool.
8.Peripheral neuropathy &CNS effects.
16.Thrombophlebitis at site of injection
17.OtotoxicityContra-indications of Metronidazole1.Hypersensitivity to the drug
Special Precautions while taking Metronidazole1.Renal impairment
4.Use cautiously along with other hepatotoxic drugs & In visual field changes
Pregnancy Related InformationUse with caution
First trimester:contra indicatedOld Age Related InformationMay be used.Breast Feeding Related InformationContraindicatedChildren Related InformationUse with caution
Indications for Metronidazole1.Amoebiasis
4.Pseudo membranous enterocolitis
5.Anaerobic bacterial infections after surgery, Brain abscess, & Endocarditis
6.Helicobacter pylori infections
Interactions for MetronidazoleWarfarin & other coumarin anticoagulants: Potentiates the anticoagulant effect resulting in increased prothrombin time.
Alcohol: A disulfiram-like reaction. Abdominal cramps, nausea, vomiting, headache & flushing.
Disulfiram: Acute psychotic reaction or confusional state.
Phenobarbital & Phenytoin: Increased metabolism of metronidazole resulting in decreased efficacy.
Lithium: Increased lithium levels and toxicity.
Flurouracil: Increased toxicity of flurouracil.
Lab tests: May interfere with chemical analysis for AST,SGOT, ALT, SGPT, LDH, triglycerides and hexokinase glucose. Zero values may occur.Typical Dosage for MetronidazoleAdult
Amoebiasis:400 to 800 mg 8hourly for 5 to 10days depending up on the severity of infection
In severe infections and liver abscess: 1gm as slow I.V. infusion followed by 0.5 gm twice daily till oral therapy is started
Giardiasis:200mg 8hourly for 1week or 2gm/day for 3days or I.V.500mg thrice daily
Trichomonas vaginitis: 400mg 8 hourly for a week or 2gm once daily for a week.
Male partner should be concurrently treated with the drug
Pseudo membranous enterocolitis:800 mg 8hourly
Anaerobic bacterial infections after surgery, Brain abscess, & Endocarditis:400 to 800 mg 8hourly
In severe cases: 15mg/kg I.V. infusion for 1hour followed by 7.5mg/kg 4 times daily till oral therapy is substituted
Helicobacter pylori infections:400mg 8hourly along with amoxicillin/clarithromycin and a proton pump inhibitor
Ulcerative gingivitis:200 to 800mg 8hourly
Amoebiasis: 30 to 50mg/kg/day for 5to10 days.
Giardiasis:10 to 15mg/kg/day thrice daily
Children (below 12years): 7.5mg/kg I.V.Schedule of MetronidazoleHStorage Requirements for MetronidazoleStore in a well closed container in a cool dark place. Keep out of the reach of children.Effects of Missed Dosage of MetronidazoleTake the missed dose as soon as noticed and 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 MetronidazoleTreatment is supportive & symptomatic. Drug is removed by induced emesis, gastric lavage, and administration of activated charcoal & use of cathartics. For controlling seizures diazepam & phenytoin may be used.
Nalidixic AcidAbout Nalidixic AcidSynthetic quinolone(first generation quinolone) antibiotic.Mechanism of Action of Nalidixic AcidNalidixic acid is a bacteriostatic at low concentration and bactericidal at high concentration. It act by inhibiting the enzyme DNA gyrase (Topoisomerase 2) and Topoisomerase 4. DNA gyrase helps in the formation of a highly condensed three dimensional structure of the DNA by its nicking and closing activity and also by introducing negative supercoil in to the DNA double helix. Nalidixic acid inhibits DNA gyrase which results in abnormal linkage between opened DNA and gyrase and negative supercoiling is impaired. This will inhibits transcription of DNA in to RNA and subsequent protein synthesis.Pharmacokinets of Nalidixic AcidAbsorption: They are absorbed after oral administration.
Distribution: It is distributed widely in the body.
Metabolism: It undergoes partial metabolism in the liver.
Excretion: Drug is excreted mainly through urine.
Onset of Action for Nalidixic Acid0.5 hourDuration of Action for Nalidixic Acid6 hoursHalf Life of Nalidixic Acid8 hoursSide Effects of Nalidixic Acid1. Nausea
4. Abdominal discomfort
12. Visual disturbances
Contra-indications of Nalidixic Acid1. Hypersensitivity to Nalidixic acid and other Fluoroquinolones
Special Precautions while taking Nalidixic Acid1. Hepatic impairment
2. Renal impairment
3. G6PD deficiency
4. Avoid exposure to sun light
5. Prolonged therapy
6. Caution while driving the vehicle, operating machine or involved in any hazardous activities.
Pregnancy Related InformationContraindicated in 1st trimesterOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with caution
NEONATES : ContraindicatedIndications for Nalidixic Acid1. Urinary antiseptic
7. Post partum pyelitis
8. Intestinal infections
Interactions for Nalidixic AcidAnticoagulants (Warfarin or Dicoumarol): Effects of anticoagulants enhanced.
Probenecid: Reduces excretion of nalidixic acid.
Melphalan: Serious Gastro Intestinal toxicity.
Lab tests: False positive urinary glucose results with Benedicts or Fehling?s solution or Clinic test reagent tablets. Falsely elevated urinary 17-keto and ketogenic steroids.
Typical Dosage for Nalidixic AcidAdults: 4 g / day in 4 divided doses
Children : 55 mg / kg body weight / day in 4 divided doses
Schedule of Nalidixic AcidHStorage Requirements for Nalidixic AcidStore at 15 - 30 degree C in a tightly closed container. Protect away from heat and light.Effects of Missed Dosage of Nalidixic AcidTake the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose.Effects of Overdose of Nalidixic AcidGive supportive measures and symptomatic treatment. Gastric lavage has to be done. Give plenty of water to promote the excretion of the drug.
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