Antiparasitic Drugs

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Lumen & Tissue Protozoacides - Gut & Glory Guys

  • Nitroimidazoles (Metronidazole, Tinidazole):
    • Targets: Giardia, Entamoeba (invasive), Trichomonas. 📌 "GET on the Metro!"
    • MOA: Prodrugs; form free radicals → DNA damage in anaerobes.
    • SE: Metallic taste, disulfiram-like reaction with alcohol, neurotoxicity.
    • Use: Trichomoniasis (single 2g dose), Giardiasis, Amoebic dysentery/abscess.
  • Lumenal Amebicides (E. histolytica cysts):
    • Diloxanide furoate (DOC: asymptomatic carriers).
    • Iodoquinol (SE: Optic neuritis).
    • Paromomycin (Aminoglycoside; Giardia in pregnancy, Cryptosporidiosis).
  • Nitazoxanide:
    • Broad-spectrum: Giardia, Cryptosporidium, E. histolytica.
    • MOA: Inhibits PFOR enzyme pathway.

⭐ Metronidazole: DOC for symptomatic amebiasis; combine with lumenal agent for E. histolytica.

Hemoflagellate & Sporozoa Slayers - Blood & Tissue Terminators

  • Leishmaniasis:
    • Pentavalent Antimonials (SSG): Cardiotox.
    • Amphotericin B (Visceral): Nephrotoxic. Kala-azar gold std.
    • Miltefosine: Oral; teratogenic.
  • Trypanosomiasis:
    • African (Sleeping Sickness):
      • Early: Suramin (East), Pentamidine (West; hypoglycemia).
      • Late (CNS): Melarsoprol (arsenical, encephalopathy!), Eflornithine (West).
      • 📌 "Early birds get SuP (Suramin/Pentamidine), Late comers get MEl (Melarsoprol/Eflornithine)."
    • American (Chagas): Nifurtimox, Benznidazole. (Chronic: low efficacy)
  • Toxoplasmosis:
    • Pyrimethamine + Sulfadiazine + Folinic acid (myelosuppression rescue).

    Sulfadiazine (Toxo regimen) causes crystalluria; hydrate.

  • Babesiosis:
    • Atovaquone + Azithromycin.
    • Severe: Quinine + Clindamycin.

Antimalarial Agents - Malaria Mashers

Targets: Blood schizonts (active infection), Liver schizonts (incl. hypnozoites for relapse), Gametocytes (transmission). Key drugs:

  • Blood Schizonticides:
    • Artemisinins (Artesunate, Artemether): Rapid acting. Backbone of ACT. For uncomplicated & severe falciparum.

      ⭐ ACT (Artemisinin Combination Therapy) is 1st line for uncomplicated P. falciparum.

    • Chloroquine: For sensitive P. falciparum, P. vivax/ovale/malariae. SE: Retinopathy (long-term).
    • Quinine/Quinidine: For severe/resistant malaria. SE: Cinchonism, hypoglycemia.
    • Mefloquine: Prophylaxis, treatment. SE: Neuropsychiatric.
  • Tissue Schizonticides (Liver Stage):
    • Primaquine: Eradicates hypnozoites (P. vivax/ovale). Gametocidal. ⚠️ Test G6PD (hemolysis).
  • Prophylaxis:
    • Mefloquine
    • Doxycycline
    • Atovaquone-Proguanil (Malarone)

Plasmodium life cycle stages and drug targets

Anthelminthic Drugs - Worm Whackers

  • Benzimidazoles (Albendazole, Mebendazole)
    • MOA: Inhibit β-tubulin polymerization. 📌 "Bend the Worms".
    • Spectrum: Broad (nematodes, some cestodes & trematodes).
    • Albendazole: Systemic; better with fatty meal. Mebendazole: Intraluminal; poor absorption.
    • SE: GI upset, ↑LFTs, bone marrow suppression (prolonged use).
  • Praziquantel
    • MOA: ↑Ca²⁺ influx → spastic paralysis.
    • Spectrum: Trematodes (Schistosoma), Cestodes (Taenia).
    • SE: Dizziness, headache, GI upset.
  • Ivermectin
    • MOA: Glutamate-gated Cl⁻ channel activator → flaccid paralysis.
    • Spectrum: Nematodes (Onchocerca, Strongyloides), ectoparasites.
    • SE: Mazzotti reaction (in onchocerciasis).
  • Pyrantel Pamoate
    • MOA: Neuromuscular blocker → spastic paralysis.
    • Spectrum: Pinworm, roundworm, hookworm.
  • Diethylcarbamazine (DEC)
    • MOA: Alters surface membrane → immune attack.
    • Spectrum: Filariasis (Wuchereria, Brugia), Loa loa.
    • SE: Mazzotti reaction.

⭐ Praziquantel is the drug of choice for schistosomiasis and neurocysticercosis.

High‑Yield Points - ⚡ Biggest Takeaways

  • Metronidazole: DOC for amoebiasis, giardiasis, trichomoniasis; damages DNA.
  • Albendazole/Mebendazole: Treat nematodes, hydatid, neurocysticercosis by inhibiting microtubule synthesis.
  • Praziquantel: DOC for schistosomiasis, tapeworms, flukes; causes parasite paralysis via Ca²⁺ influx.
  • Chloroquine: For sensitive malaria (inhibits heme polymerase); risk of retinopathy.
  • Artemisinin Combination Therapies (ACTs): First-line for uncomplicated P. falciparum malaria.
  • Ivermectin: DOC for onchocerciasis, strongyloidiasis; activates glutamate-gated Cl⁻ channels.
  • Liposomal Amphotericin B: For visceral leishmaniasis; liposomal form reduces nephrotoxicity.

Practice Questions: Antiparasitic Drugs

Test your understanding with these related questions

An Englishman travels to a place which is resistant to chloroquine and mefloquine. What should he take as prophylaxis?

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Flashcards: Antiparasitic Drugs

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Which strain(s) of Plasmodium produce dormant hypnozoites in the liver?_____

TAP TO REVEAL ANSWER

Which strain(s) of Plasmodium produce dormant hypnozoites in the liver?_____

Plasmodium vivax

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