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53 Cards in this Set

  • Front
  • Back
Antiprotozoal drugs:

Protozoa are motile, ______ eukaryotic organisms
intracellular
Antiprotozoal drugs:
causative agent of amoebiasis
Entamoeba histolytica
Antiprotozoal drugs: this Disease manifests as severe colitis (dysentery) and sometimes liver abscesses
Amoebiasis
Antiprotozoal drugs:
who are the cheif hosts of amoebiasis
humans
Antiprotozoal drugs:
this Infection follows the ingestion of mature cysts in water or food contaminated by human feces.
In the colon, cysts develop into trophozoites. Trophozoites adhere to colonic epithelial cells and feed, multiply and encyst there. Trophozoite also lyses colonic mucosa, invades the submucosa and can reach liver through portal circulation.
amoebiasis
Antiprotozoal drugs:

Kills trophozoites of E. hystolitica, no effect on cysts
Active against the invasive form of the disease in the gut and liver
metronidazole and tinidazole
Antiprotozoal drugs:MOA: nitro group of drug is reduced by protozoa (and anaerobic bacteria) to a DNA-damaging agent
metronidazole
Antiprotozoal drugs:Has unpleasant taste
Interferes with alcohol metabolism; alcohol should be strictly avoided
metronidazole and tinidazole
Antiprotozoal drugs:similar to metronidazole, slower elimination
Tinidazole
Antiprotozoal drugs:Given orally, its unabsorbed fraction is the active form
Effective against the non-invasive form of the amoebiasis parasyte in the GI
Drug of choice for the asymptomati, infected patient
Also used as a follow-up after the disease has been reversed with metronidazole
No serious adverse effects
diloxanide
Antiprotozoal drugs:Principal disease-causing species in the flagellates group are:
Trypanosoma
Leismania
Trichomona
Giardia
Antiprotozoal drugs:
Trypanosomiasis gamiense and rhodesiense cause ...
sleeping sickness
Antiprotozoal drugs:
trypanosomiasis cruzi causes...
chagas disease
Antiprotozoal drugs:Drugs used for sleeping sickness
suramin, pentamidine
Antiprotozoal drugs: drugs used for chagas disease
none - no effective treatment
Antiprotozoal drugs:Enters the trypanosoniasis parasite by endocytosis and inhibits its enzymes
Relatively toxic drug (nephrotoxicicty, optic atrophy, adrenal insuffciency)
Suramin
Antiprotozoal drugs:

Interacts with Trypanosomiasis parasite’s DNA
Usefullness limited by toxic effects: tachycardia, vomiting, breathlessness, later kidney, liver damage, blood dyscrasias
Pentamidine
Antiprotozoal drugs:
Simple skin infection
Expanded mucocutaneous form
Visceral form (“kala-azar”: parasite sreads throughout blood stream and causes hepatomegaly, splenomegaly, anemia and fever)
Leishmaniasis
Antiprotozoal drugs:
Pentavalent Sb compound
Adverse effects: vomiting, bradycardia, hypotension
main drug to treat visceral form of Leishmaniasis
Na stibogluconate
Antiprotozoal drugs:

Causative agent: Trichomonas vaginalis
Causes inflammation of vagina in females, sometimes inflammation of urethra in males
Trichomoniasis
Antiprotozoal drugs:
main treatment of Trichomoniasis
metronidazole
Antiprotozoal drugs:Intestinal disease
Causative agent: Giardia lamblia
Giardiasis:
Antiprotozoal drugs:
therapy for giardiasis
metronidazole
Antiprotozoal drugs:

what type of protozoa is malaria
sporozoa
Antiprotozoal drugs:
definitive host of malaria
mosquitos
Antiprotozoal drugs:
the sexual cycle of the malaria sporozoa takes place in the _____
mosquito
Antiprotozoal drugs:
the asexual cycle of the malaria sporozoa takes place in the ______
human
Lifecycle of plasmodium parasite in humans:
Bite of a mosquito deposits ______ in blood stream, which within 30 minutes enter the liver
sporozoites
Lifecycle of plasmodium parasite in humans:
During 10-14 days sporozoites develop and multiply, cause rupture of parasitised liver cells and ________ are released
Some sporozoites form hypnozoites (dormant forms)
merozoites
Lifecycle of plasmodium parasite in humans:
Merozoites enter the red blood cell and form ________
Some merozoites differentiate into gametocytes
trophozoites
Lifecycle of plasmodium parasite in humans:
Trophozoites within red cell develop into _______
shizonts
Antiprotozoal drugs:

Symptoms: fever, shivering, pain in the joints, headache, repeated vomiting, generalized convulsions
Periodic episodes of fever result from the synchronized rupture of red cells that release merozoites and debris
Malaria
Antiprotozoal drugs:

causes malignant tertian malaria (incorporates receptors for adhesion molecules on the infected red cell membrane and cells form clusters (rosettes) and adhere to blood vessels interfering with the tissue perfusion (kidney, brain). Does not have exoerythrocytic stage
P. falciparum:
Antiprotozoal drugs:
causes benign tertian malaria. Hypnozoites may persist for years
P. vivax
Antiprotozoal drugs:
causes tertian malaria. Forms hypnozoites
P. ovale:
Antiprotozoal drugs:
causes quartan malaria. No exoerythrocytic stage
P. malariae:
Antiprotozoal drugs:

Effective against erythrocytic forms of all 4 species of malaria
Not effective against sporpozoites, hypnozoites, gametocytes
Uncharged at neutral pH, converted to protonated form in acidic food vacuole of the parasite (ion-trapping)
P. falciparum is becoming resistant in most parts of the world; resistance due to increased efflux of the drug
Given for prophylaxis and for acute attacks
No side effects ar prophylactic doses, at larger doses: nausea, vomiting, dizziness, headache

Uncharged at neutral pH, converted to protonated form in acidic food vacuole of the parasite (ion-trapping)
P. falciparum is becoming resistant in most parts of the world; resistance due to increased efflux of the drug
Given for prophylaxis and for acute attacks
No side effects ar prophylactic doses, at larger doses: nausea, vomiting, dizziness, headache
Chloroquine
Antiprotozoal drugs:MOA: prevents digestion of hemoglobin by malaria parasite, also inhibits the enzyme that converts hemes to non-toxic products
Chloroquine
Antiprotozoal drugs:Alkaloid from the bark of Cinchona tree
Effective against erythrocytic forms of all 4 species of malaria, not effective against hypnozoites or gametocytes
MOA: inhibits heme-polymerase
Not concentrated in the parasite as chloroquine
Has depressant action on the heart, mild blocking action at neuromuscular junction, weak antipyretic effect
High concentrations: “cinhonism”: nausea, dizziness, headache, blurred vision, tinitus, cardiac dysrhythmias, CNS disturbances
Quinine
Antiprotozoal drugs:

Kills erythrocytic forms of P. flaciparum and P. vivax
MOA: inhibits heme polymerase
P. falciparum in South-east Asia is increasingly resistant
GI disturbances common; transient CNS toxicity, rare skin problems
Used for chemoprophylaxis in areas where there is a high probability of acquiring chloroquine resistant P. falciparum, also used in acute attacks, not effective against hypnozoites
Mefloquine
Kills blood shizonts of malaria parasite
Not effective against hypnozoites
MOA: unknown
Adverse effect (common): GI disturbances, headache, transient rise in hepatic enzymes, cough, changes in cardiac rhythm, rarely hemolytic anemia, convulsions
Reserved for infections caused by resistant strains
Halofantrine
Antiprotozoal drugs:

inhibit synthesis of folate (compete with PABA).

Used for chloroquine resistant P. falciparum
Sulfonamides (sulfadoxine
Antiprotozoal drugs:

inhibits dihydrofolate reductase (greatest affinity for the plasmodial enzyme)

Used for chloroquine resistant P. falciparum
Pyrimethamine
Antiprotozoal drugs:
Has little action against the erythrocytic stage malaria parasites
Effective against hypnozoites (used as a radical cure)
It has gametocydal actions (used for the prevention of transmission)
Resistance: rare
Few adverse effects: GI disturbances, hemolysis in individuals with X-linked G6P-dehydrogenase deficiency
Primaquine
Antiprotozoal drugs:
Traditional Chinese remedy for malaria
Active against blood shizonts
Not effective against hypnozoites or gametocytes
MOA: not known
Well tolerated
No known resistance
Artemisin (qinghaosu)
Antiprotozoal drugs:
disease Causes infections in immunocompromised patiens
often the presenting symptom and leading cause of death in AIDS
Pneumocystis carnii
Antiprotozoal drugs:
treatment for Pneumocystis carnii
cotrimoxazole, or trimoethoprim-dapsone
Antihelmintic drugs:
definitive hosts of helminths
humans
Antihelmintic drugs:
route of entry of helminth infection
mouth or skin (contaminated water, undercooked meat)
Antihelmintic drugs:
Inhibit the polymerization of helminth b-tubulin, interfering with many functions (glucose uptake)
Broad-spectrum agents
Fatty food increases absorption of mebendazole, albendazol; tiabendazole absorbed well from GI
Adverse effects: highest with tiabendazole (GI disturbances, headache, dizziness)
Benzimidazoles
Antihelmintic drugs:

Broad-spectrum agent
Drug of choice for schizostomiases
MOA: Binds to voltage-gated Ca channels on parsits and causes influx of Ca (rapid contractions of parasite musculature and eventual paralysis and death of the worm)
Well tolerated
Some disturbances seen in patients with heavy worm load might be due to products released from dead worms
Praziquantel
Antihelmintic drugs:

Active against certain filiarias (round worms)
Adverse effects: common, but transient
Drug effects: GI disturbances, arthralgias, headache
Effects of dying filiarie products: skin reactions, enlargement of lymph glands, dizziness, tachycardia, GI and respiratory disturbances
Modifies parasites so that they become susceptible to host’s defense mechanisms
Diethylcarbamazine
Antihelmintic drugs:

Broad-spectrum agent
First choice for filiarial infections and effective in treatment of onchocerciasis (river blindness)
Opens glutamate-gated Cl channels (only found in worms) and causes motor paralysis
Well tolerated
Ivermectin