Drug treatments Human Parasites and Zoonoses
Part 2: protozoa
Parasite Drug Notes
E. histolytica Luminal action:
- Idoquinol, diiodohydroxyquin Competes for iron in GIT
- Paromomycin Interferes w/ protein synth.
Systemic action:
- (Dihydro-)emetine For pregnant women
- Chloroquine Interferes w food vacuole & digestion of RBC
Luminal + systemic action:
- Nitro-imidazoles (metronidazole) Prod. of ROS & mutagenic to parasite
B. coli Metronidazole Prod. of ROS & mutagenic to parasite
G. intestinalis Metronidazole Prod. of ROS & mutagenic to parasite
T. vaginalis Metronidazole Prod. of ROS & mutagenic to parasite
T. brucei Suramin: stage 1 Polysulfonated naphthylamine: inhibition of
rhodesiense - Haemo-lymphatic stages, cidal glycolysis
Melarsoprol: stage 2 Inhibits glycolysis
- Arsenic derivate: 5-10% mortality
T. brucei Pentamidine: stage 1 Inhibits DHF-reductase: folate pathway
gambiense - Haemo-lymphatic stages, cidal (protection against ROS)
Eflornithine / DFMO: stage 2
- Often combinated with Inhibits ornithine-decarboxylase: polyamine
Nifurtimox (NECT): preferred synthesis (ROS)
treatment Gambiense stage 1 & 2
Fexinidazole: both stages Oral drug: no hospitalization
- Very late stage: better NECT Activation by nitro-reductase: induces DNA
- Chance of resistance damage.
T. cruzi Etiological: nifurtimox or benznidazole Nifurtimox: GI not well tolerated
Symptomatix: analgetics, corticosteroids, Benznidazole: nitro-imidazole
B-blockers
Leishmania Pentavalent antimony Lot of resistance in India. Depletes parasite
of glutathiones (protects them from ROS)
Miltefosine: oral treatment! Oral treatment. Interferes with
- High relapse numbers mitochondrial activity.
Amphotericin-B = drug of choice at this Binds ergosterol in lipid membrane: disturbs
moment (cold chain needed). Actually an integrity. Esp. useful as liposome: more
antifungal drug accumulation in macrophage. Cells in bone
marrow not necessary targeted: some
parasites may remain
Paromycin Interferes with protein synthesis
Pentamidine Interrupts folic pathway
Allopurinol Veterinary importance in dogs. Treatment
for life for dogs.
Part 2: protozoa
Parasite Drug Notes
E. histolytica Luminal action:
- Idoquinol, diiodohydroxyquin Competes for iron in GIT
- Paromomycin Interferes w/ protein synth.
Systemic action:
- (Dihydro-)emetine For pregnant women
- Chloroquine Interferes w food vacuole & digestion of RBC
Luminal + systemic action:
- Nitro-imidazoles (metronidazole) Prod. of ROS & mutagenic to parasite
B. coli Metronidazole Prod. of ROS & mutagenic to parasite
G. intestinalis Metronidazole Prod. of ROS & mutagenic to parasite
T. vaginalis Metronidazole Prod. of ROS & mutagenic to parasite
T. brucei Suramin: stage 1 Polysulfonated naphthylamine: inhibition of
rhodesiense - Haemo-lymphatic stages, cidal glycolysis
Melarsoprol: stage 2 Inhibits glycolysis
- Arsenic derivate: 5-10% mortality
T. brucei Pentamidine: stage 1 Inhibits DHF-reductase: folate pathway
gambiense - Haemo-lymphatic stages, cidal (protection against ROS)
Eflornithine / DFMO: stage 2
- Often combinated with Inhibits ornithine-decarboxylase: polyamine
Nifurtimox (NECT): preferred synthesis (ROS)
treatment Gambiense stage 1 & 2
Fexinidazole: both stages Oral drug: no hospitalization
- Very late stage: better NECT Activation by nitro-reductase: induces DNA
- Chance of resistance damage.
T. cruzi Etiological: nifurtimox or benznidazole Nifurtimox: GI not well tolerated
Symptomatix: analgetics, corticosteroids, Benznidazole: nitro-imidazole
B-blockers
Leishmania Pentavalent antimony Lot of resistance in India. Depletes parasite
of glutathiones (protects them from ROS)
Miltefosine: oral treatment! Oral treatment. Interferes with
- High relapse numbers mitochondrial activity.
Amphotericin-B = drug of choice at this Binds ergosterol in lipid membrane: disturbs
moment (cold chain needed). Actually an integrity. Esp. useful as liposome: more
antifungal drug accumulation in macrophage. Cells in bone
marrow not necessary targeted: some
parasites may remain
Paromycin Interferes with protein synthesis
Pentamidine Interrupts folic pathway
Allopurinol Veterinary importance in dogs. Treatment
for life for dogs.
