AMEBIASIS

I.Emetine group : e.g. Emetine, dehydroemetine and its resinate. II. Quinoline derivatives: Halogenated hyroxyquinolines: Diiodohydroxyquinoline, iodochloroquine 4 – aminoquinolines: Chloroquine. III. Imidazole derivatives: Metronidazole, tinidazole, secnidazole, ornidazole IV. Antibiotics: Tetracyclines, paromomycin. V. Miscellaneous: Diloxanide furoate and kurchi.

Metronidazole: Reductive activation by intracellular transport proteins Reduced by the pyruvate:ferredoxin oxidoreductase system in the mitochondria of obligate anaerobes, which alters its chemical structure. Reduced intermediate particle interacts with intracellular targets — Cytotoxic intermediate particles interact with host cell DNA, resulting in DNA strand breakage and fatal destabilization of the DNA helix

Metronidazole Mechanism of action: –Enters bacteria via cell diffusion –Activated via single reduction step by bacteria  forms radicals  reacts with nucleic acid  cell death Spectrum of activity: –Anaerobic bacteria –Microaerophilic bacteria –Protozoa Resistance: –Rare –Mechanism: decreased activation (↓ red ox reaction) of drug

Metronidazole Indications: –Anaerobe infections –C. difficile –H. pylori –Bacterial vaginosis –Trichomonas vaginitis –Amebiasis –Giardiasis Drug interactions: –Ethanol –Antacids –CyA/tacrolimus –Lithium –Phenytoin –Rifampin –Warfarin

Metronidazole: Uses: 1)T vaginalis 2g single dose, 0.7% gel, 500mg – 1g suppository 2) Amoebiasis 3) Giandaisies 4) Anerobic infections – Bactericides, clostridium, fusobacterium, peptococcus, peptosirgstococcus, Eubacterium, H. pyloris. 5) Polymicrobial infections.

6) Prophylaxis of postop mixed bacterial infection 7) Bacterial vaginosis 8) Pseudomembranous colitis 9) Crohns disease with perianal fistulas

Metronidazole Distribution into tissue Therapeutic levels: PMNs Unobstructed biliary tract Pancreas CSF Empyema fluid Peritoneal fluid Hepatic abscess Pelvic tissues Vaginal/seminal fluid Adverse Effects: –GI: N, V, epigastric distress –Metallic taste –Darkening of urine –Peripheral neuropathy –Pancreatitis –Hepatitis –Fever –Reversible neutropenia

IODOQUINOL EMETINE & DEHYDROEMETINE PAROMOMYCIN SULFATE DILOXANIDE FUROATE

Asymptomatic Intestinal Infection Diloxanide500 mgtidx 10d or- Iodoquinol650 mgtidx 21d or- Paromomyin 10 mg/kg tidx 7d

Mild to Moderate Intestinal Infection Metronidazole 750mg tid x 10d or- Tinidazole 2g od x 3d Plus- Luminal agent

Mild to Moderate Intestinal Infection Alternative: Luminal agent Plus either- Tetracycline 250mg tid x 10d or- Erythromycin 500 mg qid x 10d

Severe Intestinal Infection Metronidazole 750mg tid (500mg IV every 6 h) or Tinidazole plus Luminal agent Alternative: Luminal agent plus either Tetracycline or Dehydroemetine 1mg /kg SC/IM x 3-5d

Hepatic / Extra intestinal Same as above Alternative: Dehydroemetine 1mg /kg S.C/IM x 3-5d Followed by (liver abscess only) Chloroquine 500mg bd x 2d, then 500mg od x21d Plus Luminal agent

PENTAMIDINE: Pnenmocytosis sleeping sickness leishmaniasis Parenteral omebahized powder,

LEISHMANIASIS:- 1) Liposonal anyrhotencin 2) Pentroalent antimonish. Sodium stibozhconate meglumine antimonite 3) Miltefosine 4) Pent amidine isethionate 5) paromorycin

CUTANEOUS: 1) Pentacalant antimoniab 2) As above 3)Antifungals, allopunol

TOPICAL: 1) Iutratesional antimony 2) Paromomycin oint 3) Cryotherapy 4) local heat 5) surgical removal

SODIUM STIBOGLUCONATE:- IV / IM. Iutial t1/ 2 – 2 h Terminal t1/ 2 – 24 h 20 mg / kg 1d x 20 d

ADR: G.I headache, arthralgia, rash - IM – Stenile abscers - ECG - Hemolytic anemia - LFT, renal effects,

NITAZOXANIDE: General. Lanbia C. Parvum E. histohytica A. Iumbricoides Several tapumorns Increase Tizoxamide

MILTEFOSINE: mg / kg / d x 28 d - Single dose amp B + 7 – 14 d miltepoine - G. I. - Decrease LFT - Not in Pregnancy - Resistance is a problem. Combination

PAROMOMYCIN:- 11mg / kg x 21 d IM - ADR as with AGI