Anti Protozoal Drugs (part1/2) - Maleria lifecycle and it's treatment 🦟

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 Amebiasis

infection of intestinal tract by Entamoeba histolytica 

Lifecycle of Entamoeba histolytica 

Two forms…

1. Cyst: survive out of the body…2.Labile/Invasive: cannot survive out of thebody….Cyst ingested through feces-contaiminated food…pass into the lumen… 

where Trpohozites liberated,multiply,invade/ulcerate Mucosa of Large Intestine… 

Amoeba‟s major food intestinal flora…slowly carried toward Rectum,converted into cyst & excreted in feces 

Large no. of Trophozoites within Colon wall lead to systemic invasion.

Maleria, lifecycle, kadzung, lipincott, screening test review , pharmacist

Mixed amoebicides 

Metronidazole

DOC in Amoebic infection, Pseudomembraneous colitis…Nitroimidazole Active for both Luminal & Systemic amoeba

MOA:

 Nitrogen of Metronidazole converted Nitro Radical…Act as electron Acceptor… 

form reduced cytotoxic compound….bind to Ferodoxin-Like low redox potential ELECTRON-TRANSPORT PROTEIN…cell death 

S.E

Metallic taste, Oral moniliasis…

Tinidazole= sec-generation Nitro-imidazole 

Luminal Amebicide Iodoquinol=Halogenated 8-hydroxy Quinolone….Effective for both luminal &cyst form.. 

S.E

Rash, rare Optic neuritis 

Paromomycin= Aminoglycoside antibiotic... 

against only for Intestinal (Luminal) form 

of E.histolytica & Tapeworm….also reduce intestinal flora & leakage of cells from cell memb….

Systemic Amoebicide 

Chloroquine= in combination with Metronidazole & Diloxanide furoate to treat Amoebic liver abscess 

Emetine & DehydroEmetine

Ď´ protein synthesis by blocking chain Elongation… 

Ipecac alkaloid …t1/2 is 5day….

Malaria 

 acute infectious caused by four plasmodium specie

Plasmodium parasite transmitted through Anopheles Mosquito

Plasmodium falciparum most dangerous cause persistent high fever, Orthostatic Hypotension, massive Erythrocytosis, Swollen, reddish limb,capillary obstruction death

Plasmodium vivax cause mild malaria

Plasmodium malaria common to tropical region

Plasmodium ovale rarely encountered

Life cycle of Malarial Parasite

  • When infected mosquito bite
  • inject Plasmodium Sporozoites into blood…
  • Sporozoite migrate from blood to liver….
  • in liver form Merozoites…
  • Merozoite release & invade RBCs using Hb as a nutrient..
  • Infected cell rupture and release thousands of Merozoite& Heme, invade other RBCs…
  • Some Merozoite become Gametocyte, picked-up by Female mosquito

Tissue Schizonticide: 

Primaquine 8-aminoquinine…

👍eradicatePrimary Exoerythrocytic form of P.falciparum, P.vivax…

👍eradicate Secondary Exerythrocytic form of P.vivax & P.ovale remain in liver in form of cyst after erythrocytic form eliminated …

đź‘ŤGametocytic form of all four plasmodium eradicated 

MOA

 produce Oxidant destroy Schizontocide & Hemolysis, Methemoglobinemia toxicity 

S.E

Hemolytic anemia……contra in pregnancy

Blood Schizontocide: 

Chloroquine 

4-aminoquinoline….DOC in Erythrocytic P.falciparum…used in Rheumatoid arthritis

MOA

 đź‘ŤParasite digests Hb to obtain essential Amino Acids…toxic Heme release… 

đź‘ŤParasite polymerizes Heme to nontoxic Hemozoin sequestered into food vacuole… 

đź‘ŤChloroquine Ď´ polymerization…↑Heme cause cell death of parasite 

P.K

Chloroquine Diprotic weak base…↑Vd Excretion↑in Acidified urine

S.E

Discoloration of Nail & mucous memb, Blurred vision, Pruritis, 

Blood Schizontocide: Mefloquine 

For P.falciparum…t1/2 is 17days….↑ECG & Cardiac arrest

Blood Schizontoside: Quinine 

S.E

 Cinchonism: “nausea, vomiting, Tinnitus, vertigo”…Black water fever, +VeCoomb's test for hemolytic anemia, Fetotoxic, ↑Digoxin &NM blocker level

Blood Schizontoside: Artemisnin 

👍From Qingaosu plant …Produce free radical within Plasmodium‟s food vacuole…

đź‘ŤAlso covalently bind to & damage malarial protein 

S.E

 QT-interval prolong, Neurotoxicity 

Blood Schizontoside & Sporonticide: Pyrimethamine 

MOA= Blood Schizonticide…plus A Sporonticide ingest in Mosquito‟s gut…

ϴFH2 reductase… ϴFH4 synthesis….

S.E

 Megaloblastic anemia



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