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AMEBIASIS. 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
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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
Indications: Anaerobe infections C. difficile H. pylori Bacterial vaginosis Trichomonas vaginitis Amebiasis Giardiasis Drug interactions: Ethanol Antacids CyA/tacrolimus Lithium Phenytoin Rifampin Warfarin Metronidazole
Metronidazole: • Uses: • 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
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 Metronidazole
IODOQUINOL EMETINE & DEHYDROEMETINE PAROMOMYCIN SULFATE DILOXANIDE FUROATE
Asymptomatic Intestinal Infection Diloxanide 500 mg tid x 10d or- Iodoquinol 650 mg tid x 21d or- Paromomyin 10 mg/kg tid x 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:- - 2.5mg / 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