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Slides Anti-Infectives Antimicrobials
Antiparasitic Agents
Amebicides Trematodes
Cestodes
Mechanism of resistance
• Malaria organisms develop membrane transporters
to eject intracellular heme.
High doses
• Severe skin reactions
• Peripheral neuropathies, toxic psychosis,
retinal and auditory damage
• Myocardial depression
• May precipitate porphyria attacks
Ute Frevert and Margaret Shear, https://commons.wikimedia.org/wiki/File:Malaria.jpg, CC-BY 2,5
Anubhav Mishra, anmishra013@gmail.com
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Antimalarial Agents Drugs Derived From Artemisinin
Blood schizonticide
• Combines with dsDNA, prevents strand
separation
• Blocks replication and transcription
• Used in chloroquine resistant P. falciparum
• Often combined with doxycycline or
clindamycin
• Used to shorten duration and limit
toxicity
Ute Frevert and Margaret Shear, https://commons.wikimedia.org/wiki/File:Malaria.jpg, CC-BY 2,5
Anubhav Mishra, anmishra013@gmail.com
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Antimalarial Agents Quinine
Blood schizonticide
Toxicity
• Cinchonism (gastrointestinal distress,
headache, vertigo, blurred vision, tinnitus)
• Hemolysis in G6PD deficient patients
• Blackwater Fever: intravascular hemolysis
Blood schizonticide
• Chemically related to quinine
• First line agent; taken weekly (four
weeks before, one week after)
Mechanism of action
• Creates toxic heme particles in food
vacuoles
Blood schizonticide
Toxicity
• GI distress, skin rash, headache,
dizziness
• Nightmares
• May cause cardiac conduction
defects, seizures at high doses
Mechanism of action
• Forms quinolinequinone metabolites that act as oxidants
Toxicity
Mechanism of action
• Antimetabolites; block folic acid synthesis
Toxicity
• Skin rash, gastrointestinal distress
• Contraindicated in pregnancy
Toxicity
• Hematological: agranulocytosis and aplastic anemia
Erythrocide
Malarone R is atovaquone plus proguanil
• Used as treatment and as once daily prophylaxis
• Is an alternative treatment for P. jiroveci infection
Mechanism of action
• Disrupts mitochondrial electron transport
Erythrocide
Toxicity
• Abdominal pains
• GI effects
Erythrocide
• Active against erythrocytic forms of all 4 malaria organisms
• Not used as a chemoprophylactic agent
• High potential for cardiotoxicity; prolonged QT interval
• Embryotoxic; contraindicated in pregnancy
Principles of prevention
• Chloroquine remains first choice in
areas without resistant P. falciparum
Emetine, dehydroemetine
Mechanism of action
• Blocks ribosomal movement along
mRNA
• Inhibits protein synthesis
Mechanism of action
• Bio activation by anaerobes to form cytotoxic products
• Nitro group reduced by ferredoxin
Toxicity
• Headaches, dizziness, rashes, arthralgia
Mechanism of action
• Inhibits microtubule assembly
• Ovicidal in: ascariasis, ancylostomiasis,
trichuriasis
• Larvicidal in: ascariasis, cysticercosis
(pork tapeworm), hookworm, hydatid
disease
Toxicity
• Short duration of therapy; toxicity is
rare
• Reversible leukopenia, elevated liver
enzymes with prolonged use
Mechanism of action
• Immobilizes microfilariae by
unknown mechanism
Toxicity
• Reactions to proteins of dying
filariae include fever, rash, ocular
damage
Mechanism of action
• Single dose
• Intensifies γ-aminobutyric acid (GABA)
neurotransmission in nematodes
• Causes spasm and immobilization of
parasites
• Used in cutaneous larva migrans,
strongyloidiasis, filariasis
Toxicity
Mechanism of action
• Less than 10 % absorbed
systemically
• Inhibits microtubule synthesis and
glucose uptake in nematodes
Mechanism of action
• Absorbed systemically; much more systemic side effects
Toxicity
• GI irritation, intrahepatic cholestasis, liver failure, headache, dizziness, drowsiness
Intravitreal cysticercosis presenting as neovascular glaucoma, Dhanashree Ratra, Chekitaan Phogat, Maneesh Singh, Nikhil S Choudhari,
Scienceopen.com CC-BY 4.0
Anubhav Mishra, anmishra013@gmail.com
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Trematodicidal Agents Praziquantel
Mechanism of action
Toxicity
• Headache, dizziness, drowsiness
Intravitreal cysticercosis presenting as neovascular glaucoma, Dhanashree Ratra, Chekitaan Phogat, Maneesh Singh, Nikhil S Choudhari,
Scienceopen.com CC-BY 4.0
Anubhav Mishra, anmishra013@gmail.com
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Cestodicidal Agents Niclosamide
Mechanism of action
• Uncouples oxidative phosphorylation, causing
paralysis
Toxicity
• Gastrointestinal distress
• Headache
• Rash
• Fever
A. Chloroquine
B. Dihydroartemisinin
C. Quinine
D. Halofantrine
E. Sulfonamides
A. Chloroquine
B. Dihydroartemisinin
C. Quinine
D. Halofantrine
E. Sulfonamides
A. Diloxanide furoate
B. Iodoquinol
C. Paromomycin
D. Metronidazole
A. Diloxanide furoate
B. Iodoquinol
C. Paromomycin
D. Metronidazole
A. Diloxanide furoate
B. Iodoquinol
The principle behind amebicidal therapy is understanding where each drug
works. The first three drugs are luminal amebicides; they stay in the lumen
C. Paromomycin
of the gut and work very well if the infestation is at the luminal surface.
Once the organism
D. Metronidazole becomes systemic, metronidazole would be a logical
choice, as it is activated by anaerobes and very effective in hepatic tissue.
A. Niclosamide
B. Praziquantel
C. Mebendazole
D. Albendazole
Intravitreal cysticercosis presenting as neovascular glaucoma, Dhanashree Ratra, Chekitaan Phogat, Maneesh Singh, Nikhil S Choudhari,
Scienceopen.com CC-BY 4.0
Anubhav Mishra, anmishra013@gmail.com
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© www.lecturio.com | This document is protected by copyright.
While on mission with Medecins sans Frontières® (Doctors Without Borders®),
you see a young boy with a strange lump in his retina. It is a small cyst with a
hard centre. What would be the appropriate treatment?
A. Niclosamide
B. Praziquantel
C. Mebendazole
D. Albendazole
Intravitreal cysticercosis presenting as neovascular glaucoma, Dhanashree Ratra, Chekitaan Phogat, Maneesh Singh, Nikhil S Choudhari,
Scienceopen.com CC-BY 4.0
Anubhav Mishra, anmishra013@gmail.com
Powered by TCPDF (www.tcpdf.org)
© www.lecturio.com | This document is protected by copyright.
While on mission with Medecins sans Frontières® (Doctors Without Borders®),
you see a young boy with a strange lump in his retina. It is a small cyst
with a hard centre. What would be the appropriate treatment?
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