Antiparasitic Agents

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Antimalarials - Malaria Mayhem Meds

  • Goal: Eradicate parasites from blood (clinical cure) & liver (radical cure).
  • **Classification (Simplified):
    • Blood Schizonticides: Act on erythrocytic forms. E.g., Chloroquine, Artemisinins, Quinine, Mefloquine.
    • Tissue Schizonticides: Act on liver stages (hypnozoites). E.g., Primaquine.
    • Gametocytocidals: Kill sexual forms. E.g., Primaquine.
  • Key Drugs & Actions:
    • Chloroquine: Inhibits heme polymerase. For sensitive P. vivax/ovale/malariae. Resistance in P. falciparum (PfCRT gene).
    • Artemisinins (Artesunate, Artemether): Endoperoxide; free radical damage. Rapid action. DOC for severe malaria (IV Artesunate) & uncomplicated P. falciparum (as ACTs).
    • Primaquine: Radical cure for P. vivax/ovale. ⚠️ Test for G6PD deficiency (risk of hemolysis).
    • Mefloquine: Prophylaxis & treatment. Neuropsychiatric side effects.
    • Atovaquone-Proguanil (Malarone®): Prophylaxis & treatment.
  • 📌 All Clinicians Treat with ACTs for uncomplicated Falciparum.

⭐ Artemisinin-based Combination Therapy (ACT) is the WHO-recommended first-line treatment for uncomplicated P. falciparum malaria to combat resistance and improve efficacy.

Life Cycle of the Malaria Parasite

Other Antiprotozoals - Protozoa Purge Pills

  • Metronidazole & Tinidazole:
    • MOA: Free radical damage in anaerobes.
    • Uses: Amoebiasis, Giardiasis, Trichomoniasis, anaerobic infections. 📌 GET Anaerobes on the Metro (Giardia, Entamoeba, Trichomonas).
    • AE: Disulfiram-like effect with alcohol, metallic taste, neurotoxicity (rare).
  • Luminal Amoebicides: (For asymptomatic E. histolytica cyst passers)
    • Diloxanide furoate (DOC), Iodoquinol (AE: optic neuritis), Paromomycin.
  • Nitazoxanide:
    • Broad spectrum: Giardia, Cryptosporidium. MOA: Inhibits PFOR enzyme.
  • Leishmaniasis:
    • Sodium Stibogluconate: AE: Cardiotoxicity (QT prolongation), pancreatitis.
    • Amphotericin B (liposomal): DOC for Visceral Leishmaniasis (Kala-azar).
    • Miltefosine: Oral, teratogenic.
  • African Trypanosomiasis (Sleeping Sickness):
    • Hemolymphatic stage: Suramin, Pentamidine.
    • CNS stage: Melarsoprol (arsenical; AE: encephalopathy), Eflornithine.
  • American Trypanosomiasis (Chagas Disease):
    • Nifurtimox, Benznidazole.
  • Pentamidine:
    • Uses: Pneumocystis jirovecii pneumonia (PJP), Leishmaniasis, African Trypanosomiasis (early West African).
    • AE: Pancreatitis, dysglycemia, nephrotoxicity.

⭐ Metronidazole is ineffective against luminal amoebic cysts; requires a luminal agent like Diloxanide furoate for eradication of infection and to prevent carrier state development or relapse after tissue amoebicide therapy for invasive disease.

Anthelmintics - Worm Wipeout Weapons

Anthelmintic drug mechanisms and resistance

  • Benzimidazoles (BZDs): Albendazole, Mebendazole
    • Mech: Inhibit parasite β-tubulin → disrupt microtubule polymerization.
    • Uses: Broad-spectrum - Ascaris, hookworm, whipworm (Trichuris), pinworm (Enterobius).
    • Albendazole: Hydatid disease, neurocysticercosis. Fatty meal ↑ absorption.
  • Praziquantel (PZQ):
    • Mech: ↑ Ca²⁺ influx → tetanic muscle contraction & paralysis.
    • Uses: Trematodes (Schistosomiasis, Clonorchiasis), Cestodes (Taeniasis, Diphyllobothriasis).

    ⭐ Praziquantel is the drug of choice for infections caused by all Schistosoma species.

  • Ivermectin:
    • Mech: Activates glutamate-gated Cl⁻ channels → flaccid paralysis.
    • Uses: Onchocerciasis (DOC), Strongyloidiasis, Filariasis (microfilaricidal for W. bancrofti, B. malayi).
  • Pyrantel Pamoate:
    • Mech: Depolarizing neuromuscular blocker (nicotinic agonist) → spastic paralysis.
    • Uses: Pinworm, Ascaris, Hookworm (alternative).
  • Diethylcarbamazine (DEC):
    • Mech: Alters parasite surface membrane → enhances host immune destruction; inhibits arachidonic acid metabolism.
    • Uses: Lymphatic filariasis (W. bancrofti, B. malayi - DOC for adult worms & microfilariae), Loiasis (DOC), Tropical Pulmonary Eosinophilia.
    • ⚠️ Mazzotti reaction (from dying microfilariae).

High‑Yield Points - ⚡ Biggest Takeaways

  • Metronidazole: DOC for amebiasis, giardiasis, trichomoniasis; disulfiram-like reaction with alcohol.
  • Albendazole/Mebendazole: Inhibit microtubule synthesis; Albendazole for neurocysticercosis, hydatid disease.
  • Praziquantel: DOC for schistosomiasis & most cestodes; increases Ca²⁺ permeability.
  • Chloroquine: For malaria prophylaxis & sensitive strains; risk of retinopathy (chronic use).
  • ACTs (Artemisinin Combination Therapies): First-line for uncomplicated P. falciparum malaria.
  • Ivermectin: DOC for onchocerciasis, strongyloidiasis; acts on glutamate-gated Cl⁻ channels.
  • DEC (Diethylcarbamazine): DOC for lymphatic filariasis, loiasis; can cause Mazzotti reaction.

Practice Questions: Antiparasitic Agents

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Treatment of Neurocysticercosis includes all of the following except -

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Flashcards: Antiparasitic Agents

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Which strain(s) of Plasmodium is chloroquine used to treat?_____

TAP TO REVEAL ANSWER

Which strain(s) of Plasmodium is chloroquine used to treat?_____

Plasmodium vivax/ovale

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