Metronidazole + Nalidixic Acid Pharmacology

Metronidazole + Nalidixic Acid

About Metronidazole + Nalidixic Acid
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Mechanism of Action of Metronidazole + Nalidixic Acid
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Pharmacokinets of Metronidazole + Nalidixic Acid
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Onset of Action for Metronidazole + Nalidixic Acid
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Duration of Action for Metronidazole + Nalidixic Acid
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Half Life of Metronidazole + Nalidixic Acid
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Side Effects of Metronidazole + Nalidixic Acid
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Contra-indications of Metronidazole + Nalidixic Acid
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Special Precautions while taking Metronidazole + Nalidixic Acid
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Metronidazole + Nalidixic Acid
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Interactions for Metronidazole + Nalidixic Acid
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Typical Dosage for Metronidazole + Nalidixic Acid
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Schedule of Metronidazole + Nalidixic Acid
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Storage Requirements for Metronidazole + Nalidixic Acid
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Effects of Missed Dosage of Metronidazole + Nalidixic Acid
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Effects of Overdose of Metronidazole + Nalidixic Acid
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Metronidazole

About Metronidazole
A nitroimidazole antibiotic, Anti-infective, Antiprotozoal,amebicide.
Mechanism of Action of Metronidazole
Metronidazole 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 Metronidazole
Absorption: Well absorbed orally, Distribution: Widely distributed,
Metabolism: Metabolized in liver by oxidation & glucuronide conjugation, Excretion: Excreted in urine.
Onset of Action for Metronidazole
1 to 2 days
Duration of Action for Metronidazole
8hours.
Half Life of Metronidazole
8 hours.
Side Effects of Metronidazole
1.Anorexia.
2.Metallic taste
3.Nausea
4.Vomiting
5.Diarrhoea
6.Headache
7.Looseness of stool.
8.Peripheral neuropathy &CNS effects.
9.Mutagenesis.
10.Radiosensitisation.
11.Transient leucopenia
12.Dry mouth
13.Abdominal distress
14.Dizziness
15.Vertigo
16.Thrombophlebitis at site of injection
17.Ototoxicity
Contra-indications of Metronidazole
1.Hypersensitivity to the drug
2.Blood dyscrasias
3.CNS disorders
Special Precautions while taking Metronidazole
1.Renal impairment
2.Hepatic impairment
3.Alcoholic cirrhosis
4.Use cautiously along with other hepatotoxic drugs & In visual field changes
Pregnancy Related Information
Use with caution
First trimester:contra indicated
Old Age Related Information
May be used.
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Neonates: Contraindicated
Indications for Metronidazole
1.Amoebiasis
2.Giardiasis
3.Trichomonas vaginitis
4.Pseudo membranous enterocolitis
5.Anaerobic bacterial infections after surgery, Brain abscess, & Endocarditis
6.Helicobacter pylori infections
7.Ulcerative gingivitis
Interactions for Metronidazole
Warfarin & 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 Metronidazole
Adult
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
Children
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 Metronidazole
H
Storage Requirements for Metronidazole
Store in a well closed container in a cool dark place. Keep out of the reach of children.
Effects of Missed Dosage of Metronidazole
Take 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 Metronidazole
Treatment 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 Acid

About Nalidixic Acid
Synthetic quinolone(first generation quinolone) antibiotic.
Mechanism of Action of Nalidixic Acid
Nalidixic 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 Acid
Absorption: 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 Acid
0.5 hour
Duration of Action for Nalidixic Acid
6 hours
Half Life of Nalidixic Acid
8 hours
Side Effects of Nalidixic Acid
1. Nausea
2. Vomiting
3. Diarrhoea
4. Abdominal discomfort
5. Restlessness
6. Dizziness
7. Drowsiness
8. Arthralgia
9. Rash
10. Confusion
11. Insomnia
12. Visual disturbances
13. Diplopia
14. Headache
15. Photosensitivity
Contra-indications of Nalidixic Acid
1. Hypersensitivity to Nalidixic acid and other Fluoroquinolones
2. Epilepsy
Special Precautions while taking Nalidixic Acid
1. 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 Information
Contraindicated in 1st trimester
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
NEONATES : Contraindicated
Indications for Nalidixic Acid
1. Urinary antiseptic
2. Cystitis
3. Prostatitis
4. Pyelonephritis
5. Urithritis
6. Trigonitis
7. Post partum pyelitis
8. Intestinal infections
Interactions for Nalidixic Acid
Anticoagulants (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 Acid
Adults: 4 g / day in 4 divided doses
Children : 55 mg / kg body weight / day in 4 divided doses
Schedule of Nalidixic Acid
H
Storage Requirements for Nalidixic Acid
Store at 15 - 30 degree C in a tightly closed container. Protect away from heat and light.
Effects of Missed Dosage of Nalidixic Acid
Take 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 Acid
Give 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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