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Learning objectives
Classify antiamoebic drugs according to the
targeted form of E. histolytica
Describe the pharmacological properties of
nitroimidazoles
Describe the pharmacological properties of
diloxanide furoate
List antibiotics used as adjuvant to antiamoebic
drugs
Describe the principles of treatment of amoebiasis
and giardiasis
1.
2.
Dichloroacetamides
Diloxanide Furoate
Antibiotics: Tetracyclines
Metronidazole (prototype)
Most commonly used agent
Mixed tissue amebicide (Intestinal & extra
Intestinal)
Kills only trophozoites in intestinal wall but not the
cysts of E. histolytica.
Pharmacokinetics:
Oral, I/V infusion, topical gel, cream.
Absorption: Almost complete from GIT, some unabsorbed
drug reaches colon.
PPL:1- 3 hrs
Distribution: widely Distributed to all tissues & high
concentrations in body fluids CSF & brain. Also in Vaginal
secretions ,saliva etc.
t : 7.5 hrs
Prep:
Mechanism of action
Metronidazole kills protozoa & is bactericidal for anaerobic
bacteria.
Metronidazole is a pro drug requiring reductive activation of
Antimicrobial Spectrum
Kills anaerobic protozoa & bacteria
Entameba Histolytica (Trophozoits only)
Trichomona Vaginalis
Giardia Lamblia
Clostridia C . difficile
Bacteroides fragilis
Helicobacter pylori
Therapeutic Uses
Versatile drug
1. Amebiasis: DOC in all tissue infections
Adverse Effects
GIT:
Dry mouth, metallic taste --- most common.
Nausea, vomiting, abdominal cramps , Diarrhea.
Oral thrush--stomatitis
Neurotoxicity: Headache, Insomnia, numbness or
paraesthesias, weakness , dizziness.
Others: Disulfiram like action with alcohol.
Dysuria ,Dark urine.
Hypersensitivity reactions (rash, neutropenia)
Drug interactions
- Potentiate Anticoagulant effect of Warfarin.
- Metabolism of Metronidazole induced by
Phenytoin & Phenobarbitone &
Cimetidine may inhibit it.
- Metronidazole increases Lithium toxicity.
Contraindications
Patient with active disease of the CNS.
Hepatic Disease/Renal disease, dose
adjustment should be done.
Pregnancy/ Nursing Mothers.
Tinidazole :
Second- generation Nitroimidazole.
Congener of Metronidazole similar to
Metronidazole
Longer acting once daily dose.
Short course 2gm single dose orally X 3 days.
Secnidazole: Longer acting (t1/2 24 h)
2gm orally for 3 days
Chloroquine
Tissue Amebicide specially against
Amoebic Hepatitis & Liver Abscess.
Concentrated in liver; kills trophozoits
of E. histolytica
Th.use: Hepatic amebiasis / abscess;
not responding to Metronidazole
Therapeutic uses
Drug of choice for Asymptomatic Luminal
Amoebiasis (cyst passers)
Alongwith tissue amebicide in severe intestinal &
extra intestinal amebiasis.
Adverse effects
Flatulence
Nausea, abdominal cramps
Skin rashes rarely.
Precautions: Pregnancy
Tetracyclines
Used as Luminal amebicide.
Does not kill bacteria directly but disturbs the
symbiosis between normal intestinal flora & E
.histolytica . The amebae grow at expense of
normal intestinal flora .
Tetracyclines are broad spectrum antibiotics & kill
these flora leading to death of E .histolytica also.
Thank you