2. Trypanosomiasis
Human African trypanosomiasis, also known
as sleeping sickness, is a vector-born
parasitic disease.
They are transmitted to humans by tsetse fly
(Glossina genus) bites which have
acquired their infection from human
beings or from animals harbouring human
pathogenic parasites.
5. A. Melarsoprol
derivatative of mersalyl oxide
MOA: drug reacts with
sulfhydryl groups, including
enzymes of organism and
host
Resistance: decrease
permeability of drug
Pharmacokinetic: slowly
administered IV
DOC for T. brucei
rhondesiense
has a very short half-life
rapidly excreted in urine
6. A. Melarsoprol
Adverse Effects:
• CNS toxicity - encephalopathy
• Hypersensitivity reactions - fever
• GI disturbance - severe vomiting and
abdominal pain
• Hemolytic anemia ( patient w/ glucose 6-
phosphate dehydrogenase deficiency)
Contraindication: Patients with influenza
7. B. Pentamidine isethionate
• active against T. brucei gambiense
• tx systemic blastomycosis (Blastomyces
dermatitidis) and infections (Pneumocystis
jiroveci)
• DOC patients with pneumonia (P. jiroveci) who
failed to respond to Trimetoprim-
sulfamethoxazole and those allergic to
sulfonamides
• chemotherapy in immunocompromised patients
• alternative drug to Stibogluconate in tx of
Leishmaniasis
8. B. Pentamidine isethionate
MOA:
• T. brucei concentrates pentamine by an
energy-dependent, high affinity uptake
system.
• Drug binds to parasite's DNA and
interferes w/ synthesis of RNA, DNA,
phospholipid and protein
Resistance:
• Inability of trepanosome to concentrate the
drug
9. B. Pentamidine isethionate
Pharmacokinetics:
• Fresh solutions are
administered IM or
aerosols
• concentrated and stored
in liver and kidney for
long period of time
• Ineffective against
meningoencephalitic
stage of trypanosomiasis
• Excreted slowly in urine
• Half-life : 5 days
10.
11. B. Pentamidine isethionate
Adverse Effects:
• Serious renal dysfunction
• Hypotension
• Dizziness
• Rash
• Toxicity to β cells of pancreas
12. C. Nifurtimox
• tx of acute T. cruzi
infections (Chagas
disease)
• suppresive not
curative
Moa:
• undergoes reduction
and generates
intracellular oxygen
radicals (superoxide
radicals & hydrogen
peroxide)
14. Pharmacokinetic:
• administered orally
• rapidly absorbed and
metabolized to
unidentified products
excreted in urine
Adverse Effects:
• Anaphylaxis
• dermatitis
• icterus
• GI problems - weight
loss
• Peripheral neuropathy
15. D. Suramin
• early treatment and
prophylaxis of African
trypanosomiasis
• inhibits glycerol
phosphate
dehydrogenase
• IV
• binds to plasma for
long time,
accumulating in liver
and proximal tubular
cells of the kidney
16. Adverse Effects:
• Nausea and vomiting
• shock
• loss of consciousness
• acute urticaria
• paresthesia, photophobia, palpebral
edema, hyperesthesia on hands and feet
17. E. Benznidazole
• nitroimidazole derivative,
inhibits protein synthesis
and ribonucleic synthesis
in T. cruzi cells
• alternative treatment of
acute and indeterminate
phases of Chagas
Disease
• prophylaxis for preventing
infections among
hematopoietic stem cell
transplant
• ADR: dermatitis,
peripheral neuropathy,
insomnia, anorexia
18. Eflornithine
• irreversible inhibitor of
ornithine decarboxylase
• IV (first line tx second
stage African stage
Trypanosomiasis)
• Topical (tx unwanted
facial hair in women)
• short half life
• ADR:
– anemia, seizure,
temporary hearing
loss
19. Leishmaniasis
Leishmaniasis is
caused by
parasitic protozoa
of the genus
Leishmania.
Humans are
infected via the
bite of
phlebotomine
sandflies, which
breed in forest
areas, caves, or
the burrows of
small rodents.
20. There are four main types of the
disease:
1. In cutaneous forms, skin
ulcers usually form on
exposed areas, such as
the face, arms and legs.
These usually heal within
a few months, leaving
scars.
22. 3. In mucocutaneous
forms, the lesions can
partially or totally
destroy the mucous
membranes of the
nose, mouth and
throat cavities and
surrounding tissues.
23. • Visceral leishmaniasis, also known as kala azar.
• If left untreated, the disease can have a fatality rate as high as
100% within two years.
24. Leishmaniasis
• it is transmitted from animals to humans
(between humans) by a bite of infected
sandflies.
• Diagnosis is establish by demonstrating
the parasite in biopsy material and skin
lesions
26. A. Life cycle of Leishmania species:
• Sandflies transfers the flagellated promastigote form of the protozoa, which is rapidly
phagocytized by macrophage. In the macrophage, promastigotes rapidly change to
nonflagellated amastigotes and multiplies, killing the cell. The newly released
amastigotes are again phagocytized, and cycle continues
27. B. Sodium stibogluconate
• MOA is not determined
but evidence for inhibition
of glycolysis in the
parasite at the
phosphofructokinase
reaction8
has been found.
• Available parenterally
distributed in
extravascular
compartment
• Minimal metabolism ,
excretion: Urine
28.
29. Adverse effects:
• Pain at the injection site
• Pancreatitis
• elevated liver enzyme
• athralgias
• myalgias
• Gastrointestinal upset
• Cardiac arrhythmias
Renal and hepatic function should be monitored
periodically
30. C. Miltefosine (Impavido)
• First orally active drug
for viceral Leishmaniasis
• MOA: interfere with
phospholipids in
parasitic cell membrane
to induce apoptosis
• ADR: Nausea &
vomiting
• Contraidicated to
pregnacy because
teratogenic
31. VI. Taxoplasmosis
• Taxoplasma gondii
• transmitted to humans when they consume raw
or inadequately cooked, infected meat
• symptoms: flu-like symptoms but most people
affected never develop signs and symptoms
(unaware); damage to the brain, eyes (reduced
vision, blurred vision, pain (often with bright
light), redness of the eye, and sometimes
tearing), or other organs
For infants born to infected mothers and for
people with weakened immune systems,
toxoplasmosis can cause extremely serious
complications.
• Cats - only shed oocysts
35. Chemotheraphy for Taxoplasmosis
• Sulfadiazine and
Pyrimethamine - DOC
• Leucovorin - protect
against folate deficiency
• Pyrimethamine w/
Clindamycin or
Trimethoprim and
Sulfamethoxazole - tx
immunocompromised
patients
Leucovorin
At the first appearance of the rash,
pyrimethamine should be
discontinued because
hypersensitivity of the drug is severe
36. VII. Giardiasis
Infection of the small intestine
Giardia lamblia
ingestion of contaminated drinking water
Contaminated water can be in swimming pools,
spas, and bodies of water, such as lakes. Sources of
contamination include animal feces, diapers, and
agricultural runoff.
