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PHARMACOLOGY > 7 Anti-Protozoal Drugs > Flashcards

7 Anti-Protozoal Drugs Flashcards

0
Q

mixed amebicide

A

metronidazole

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1
Q

what are the 3 types of amebicides?

A
  1. Mixed
  2. luminal
  3. systemic
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2
Q

luminal amoebicide

A

diloxanide furoate

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3
Q

systemic amebicide

A

choloroquine

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4
Q

MOA of metroniazole

A

metronidazole= electron acceptor

amoebas have ferrodoxin like compounds which activate metronidazole which binds to DNA and causes cell death

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5
Q

you use metronidazole in combination with…

A

diloxanide furoate

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6
Q

if you take metronidazole you may develop

A
  1. metallic taste
  2. oral fungus
  3. disulfiram like effects if taken with alcohol
    - ->blocks aldehyde dehydrogenase–> aldehyde accumulation–> sickness
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7
Q

if you see prolonged symptoms of metronidazole (metallic taste) you might ask the pt…

A

have you been taking OTC cimetidine (for heartburn)?

–> its a p450 - and prolongs the plasma half life of metronidazole

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8
Q

you use metronidazole vs…

A

Giardia lamblia
Entamoeba histolytica
Trichomonas vaginalis

Bacteroides
Clostridium–> C. difficile

on the

Metro

Garderella

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9
Q

luminal amebicide

A

diloxanide furoate

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10
Q

if you patient is an asymptomatic passer of cyst you should give them

A

diloxanide furoate

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11
Q

which amebicide is only used for interstinal amebiasis

A

diloxanide furoate

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12
Q

what drugs can you use for systemic amebicide

A
  1. metronidazole
  2. diloxanide furoate
  3. chloroquine

you give as a combination

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13
Q

what are the systemic amebicides and what do they prevent

A

combination of metronidazole, diloxanide furoate, and chloroquine

they prevent amebic liver abscesses–> think abscess=pus

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14
Q

Schizonticides are used vs.

A

malaria

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15
Q

what 2 organisms cause malaria:

A
  1. plasmodium falciparium= deadly

2. plasmodium vivax= milder

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16
Q

if you need to target tissue schizont in a patient with malaria you would use

A

primaquine

*which you will often use in conjugation with a blood schizonticide, due to its lack of activity against the erythrocytic schizonts

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17
Q

what form of malaria does primaquine eradicate?

A

Exo-erythrocytic form= the developmental stage in the liver before RBC become infected
primary forms= P. falciparum and vivax
secondary forms=P. vivax and ovale

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18
Q

if the pt had low levels of glucose-6-phosphate dehydrogenase (G6PD deficiency) primaquine can induce

A

hemolytic anemia

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19
Q

primaquine has…

A

a low incidence of GI side effects

20
Q

what are the blood schizonticides?

A
  1. chloro-quine
  2. quinine
  3. meflo-quine
21
Q

what are the 4 MOA for cholorquine= blood schizonticide

A
  1. enters RBC and interfers with heme polymerase, which the parasites need to survive in RBC
  2. take up by food vacuoles
    chloroquine is basic and when placed in the acidic environment will take up a proton and become trapped, resulting in alkalinization of organelles–> parasite cant carry out hemoglonin digestion
  3. disrupt tertiary structure of nuclei acids–> decreased DNA synthesis
  4. bind to ferri-proto-porphyrin 9= complex that damages membranes and causes lysis of both parasite and RBC
22
Q

chloroquine (blood schizonticide)= DOC for

A

erythrocyte P. falciparum malaria–> except resistant chains

23
Q

side effects of cholorquine

A
  1. electrocardiographic changes
  2. if used chronically
    - -> discoloration of nail beds and visual disturbances
24
Q

when would you use quinine (blood schizonticide)

A

for resistant malarial strains

NEVER 1ST CHOICE DRUG FOR MALARIA–> CAN CROSS PLACENTA

25
Q

what are the effects of overdosing on quinine=cinchonism

A
  1. nausea and vomiting
  2. tinnitus=ringing of the ears
  3. vertigo

THIS IS REVERSIBLE

26
Q

what test is used for hemolytic anemia

A

Coombs test

27
Q

MOA of mefloquine

A

damage parasite membrane

28
Q

characteristic of mefloquine= blood schizonticide

A

long half life

29
Q

BIG side effect of mefloquinine= blood schizonticide

A

CNS ISSUES–> neurotic and psychotic manifestation
-can cause schizophrenia (ppl that come back from iraq and end up killing whole family)

DONT GIVE TO SCUBA DIVERS–> confusion underwater–>death

30
Q

prophylaxis for malaria

A

if sensitive–> use cholorquine

if resistant–> use doxycycline (photosensitive so use sunscreen0

31
Q

what are the 2 organisms for trypanosomiasis

A
  1. Trypanosoma brucei–> African sleeping sickness
  2. Trypanosoma cruzi–> Merican= Chagas’ disease
    - -> invades CNS
32
Q

what are the trypanosomiasis drugs

A
  1. melarsoprol
  2. petamidine isethionate
  3. nifurtimox
33
Q

melarsoprol is the DOC used only for…

A

late stages in african sleeping sickness with CNS involvement for
T. brucei gambiense
T. brucei rhodesiense

34
Q

melarsoprol (for African sleeping sickness= T. brucei) can cause

A

encephalopathy which is sometimes reversible but most times not reversible

35
Q

MOA for pentamidine isethionate= vs trepanosoma

A

binds to parasite DNA and interferes with synthesis of

  1. RNA
  2. DNA
  3. phospholipids
  4. protein of parasite
36
Q

when do you use pentamidine isethionate?

A

for treatment vs .
1. T brucei gambiense
DURING HEMATOLOGICAL STATE
2. Pneumocystis carinii–> seen in HIV pt

-not effective vs. T cruzi

37
Q

why would you not give pentamidine isethionate via IV

A

if you give it IV youll see

  1. tachcardia
  2. sharp fall in BP
38
Q

Pentamidine isethionate is toxic to…

A

beta cells of the pancreas–> can cause type 1 DM

39
Q

what is the only drug used for acute T. cruzi infections

A

nifurtimox (suppressive not curative drug)

40
Q

MOA of nitrofurtimox (for T. cruzi)

A

nitroaromatic compound that get reduced– free electron that attacks molecular O2 and forms:

  1. superoxide
  2. hydroxy radical
  3. H2O2

**requires that the organism lacks catalase

41
Q

what side effects do you see with nifurtimox= for T. cruzi

A

anaphylaxis and delayed hypersensitivity rxns

42
Q

drug used for leishmaniasis

A

sodium stibo-gluconate

43
Q

MOA of sodium stibo-gluconate= vs leishmaniasis

A

inhibits phosphofructokinase (PFK)–> which inhibits glycolysis

44
Q

side effect of sodium stibogluconate= leishmaniasis

A

cardiac arrhythmias

45
Q

DOC for Toxoplasma gondii= cat poop (cats= only animal that can shed oocyst in poop)

A

pyri-methamine

46
Q

MOA of pyrimethamine= DOC for T. gondii

A

inhibits dihydrofolate reductase–> reduced tetra-hydrofolate
–> leads to no purines or pyrimidines

MOA= same as TMP

47
Q

what might you see if you use pyrimethamine vs. T gondii

A

severe hypersensitivity rxns

possible megaloblastic anemia

48
Q

most commonly diagnosed intestinal parasite in the US

A

Giardia lamblia

PHARMACOLOGY (5 decks)

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