Fluconazole + Tinidazole Pharmacology

Fluconazole + Tinidazole

About Fluconazole + Tinidazole
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Mechanism of Action of Fluconazole + Tinidazole
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Pharmacokinets of Fluconazole + Tinidazole
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Onset of Action for Fluconazole + Tinidazole
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Duration of Action for Fluconazole + Tinidazole
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Half Life of Fluconazole + Tinidazole
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Side Effects of Fluconazole + Tinidazole
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Contra-indications of Fluconazole + Tinidazole
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Special Precautions while taking Fluconazole + Tinidazole
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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 Fluconazole + Tinidazole
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Interactions for Fluconazole + Tinidazole
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Typical Dosage for Fluconazole + Tinidazole
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Schedule of Fluconazole + Tinidazole
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Storage Requirements for Fluconazole + Tinidazole
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Effects of Missed Dosage of Fluconazole + Tinidazole
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Effects of Overdose of Fluconazole + Tinidazole
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Fluconazole

About Fluconazole
A triazole derivative, A board range Antifungal.
Mechanism of Action of Fluconazole
Fluconazole 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 synthesis
Pharmacokinets of Fluconazole
Absorption: 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 Fluconazole
N/A
Duration of Action for Fluconazole
1 day
Half Life of Fluconazole
N/A
Side Effects of Fluconazole
1.Abdominal pain
2.Nausea
3.Vomiting
4.Diarrhoea
5.Alopecia
6.Headache
7.Rash
8.Alteration in liver enzyme

Contra-indications of Fluconazole
1.Hypersensitivity to Fluconazole and other Azole antifungals
Special Precautions while taking Fluconazole
1. Hepatic dysfunction
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Contraindicated
Children Related Information
CHILDREN below13:Use with caution.
NEONATES:contraindicated
Indications for Fluconazole
1.Oesophageal candidiasis
2.Oropharyngeal candidiasis
3.Vaginal candidiasis
4.Systemic candidiasis
5.Cryptococcal meningitis
6.Coccidioidomycosis
7.Histoplasmosis
8.Prophylaxis in bone marrow transplantation
9.Candidiasis in immunocompromised individuals
10.Peritonitis
Interactions for Fluconazole
Cimetidine: 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 Fluconazole
Adult: 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.
CHILDREN:
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 Fluconazole
N/A
Storage Requirements for Fluconazole
The drug should be stored in room temperature. Keep away from moisture and sunlight.
Effects of Missed Dosage of Fluconazole
Take 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 Fluconazole
Give supportive measures and treatment.

Tinidazole

About Tinidazole
Nitroimidazole antibiotic, Antibacterial, antiprotozoal.
Mechanism of Action of Tinidazole
Tinidazole is 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 Tinidazole
Absorption: Well absorbed orally, Distribution: Widely distributed,
Metabolism: Metabolized in liver by oxidation &glucuronide conjugation, Excretion: Excreted in urine.
Onset of Action for Tinidazole
Within few hours
Duration of Action for Tinidazole
16 hours
Half Life of Tinidazole
12 hours
Side Effects of Tinidazole
1.Anorexia
2.Bitter taste
3.Nausea
4.Vomiting
5.Diarrhoea
6.Fatigue
7.Dry mouth
8.Abdominal distress
9.Headache
10.Dizziness
11.Vertigo
12.Rash
13.Urticaria
14.Angioedema
15.Peripheral neuropathy & CNS effects,
Contra-indications of Tinidazole
1.Hypersensitivity to the drug
2.Blood dyscrasias
3.CNS disorders
Special Precautions while taking Tinidazole
1.Hepatic impairment
2.Alcoholic cirrhosis
3.Obstructive liver diseases
4. Use cautiously along with other hepatotoxic drugs & In visual field changes
5. Avoid alcohol use during therapy
Pregnancy Related Information
Use with caution, but contra indicated in first trimester
Old Age Related Information
N/A
Breast Feeding Related Information
Contraindicated
Children Related Information
N/A
Indications for Tinidazole
1.Amoebiasis
2.Giardiasis
3.Trichomonas vaginitis
4.Anaerobic bacterial infections
5.Prophylactic agent after colorectal surgery
6.H. pylori infections
Interactions for Tinidazole
Alcohol: Disulfiram like reaction.
Ampicillin, Doxycycline and Cotrimoxaole: Synergism with these agents.
Typical Dosage for Tinidazole
Amoebiasis:
Adults: 2gm once daily for 3 days
Children: 30 to 50mg/kg/day or 600mg 12hourly for 5 to 10 days
Trichomoniasis & Giardiasis:
600mg once daily for a week or 2gm single dose
Anaerobic bacterial infections:
2 gm followed by 500mg 12 hourly for 5 days
Prophylaxis after colorectal surgery:
2gm single dose before surgery
H. pylori infections:
0.5gm 12hourly for 7 to14 days in triple combination
Schedule of Tinidazole
H
Storage Requirements for Tinidazole
Store at room temperature at a range of 15 to 30 degree C. Protect from excess heat and moisture.
Effects of Missed Dosage of Tinidazole
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 Tinidazole
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

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