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PHARMACOLOGY > Antiprotozoal drugs > Flashcards

Antiprotozoal drugs Flashcards

1
Q

Only one cycle of liver cell invasion and multiplication
occurs, and liver infection ceases spontaneously in
less than 4 weeks

A

PLASMODIUM FALCIPARUM AND P.

MALARIAE INFECTIONS

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2
Q

Eradication of both erythrocytic and hepatic parasites
is required to cure these infections and usually
requires two or more drugs

A

PLASMODIUM VIVAX AND P. OVALE

INFECTIONS

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3
Q

§ For eradication of vivax and ovale, it is important to
give a drug that would eradicate dormant liver form
such as

A

primaquine and tafenoquine

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4
Q

eliminate developing

dormant liver forms seen in P. ovale and vivax

A

Tissue schizonticides

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5
Q

act on erythrocytic parasite

A

blood schizonticides

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6
Q

kill sexual stages and prevent

transmission to mosquitoes

A

Gametocides

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7
Q
  • eliminate both hepatic and erythrocytic

stages

A

Radial cure

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8
Q

drugs that prevent heme detoxification

A

Quinine, chloroquine, mefloquine, Primaquine

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9
Q

Folic acid synthesis inhibitors

A

Pyrimethamine, Proguanil, Dapsone, Sulfadoxin

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10
Q

Protein Synthesis Inhibitors

A

Doxycycline

Clindamycin

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11
Q

Inhibit mitochondrial function

A

Atovaquone,

Tafenoquines

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12
Q

Generate free radicals and damages protein and lipids

A

Artemisinin

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13
Q

active against asexual
blood stages; will treat/prevent clinically symptomatic
malaria since signs and symptoms of malaria occur
where there is erythrocytic invasion of malaria

A

CAMPQST (Chloroquine, Artemisinin,
Mefloquine, Pyrimethamine, Quinine/Quinidine,
Sulfadoxin, Tetracyline)

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14
Q

target asexual
erythrocytic form and liver stages of falciparum. They
shorten several days required for post op
chemoprophylaxis

A

Atovaquone

Proguanil

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15
Q

effective against

primary and latent liver stages as well as gametocytes;

A

Primaquine and tafenoquine

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16
Q

§ They are optimized for the treatment of severe falciparum
§ They are effective against asexual erythrocytic stage
of vivax

A

Artemisinin and its derivatives

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17
Q

generate free radicals

that alkylate and oxidize macromolecules in the parasite

A

Artemisinin

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18
Q

Toxicity and contraindications (Artemisinin)

A
  • inc transaminase levels
  • decreases in reticulocyte count and neutrophil counts
  • x for 1st trimester of pregnancy
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19
Q

recommended during the first trimesters of pregnancy

A

Quinine plus clindamcyin or Mefloquine

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20
Q

recommended for the tx of severe malaria during all stages of pregnancy

A

IV artesunate

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21
Q

is well absorbed orally without
important food effect. It has excellent efficacy
against falciparum and vivax, It is well tolerated

A

Pyronaridine

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22
Q

toxicities of artesunate

A

hepatic and agranulocytosis

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23
Q

ACT with longest half-life: 5 weeks

A

Piperaquine - Dihydroartemisnin (artekin)

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24
Q

o It acts by concentrating in parasite food
vacuoles à preventing the biocrystallization of the hemoglobin
breakdown product, heme, into hemozoin à
eliciting parasite toxicity due to the buildup
of free heme

A

Chloroquine

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25
Q

Drug of choice for treatment and chemoprophylaxis of
falciparum malaria
- synthetic 4-aminoquinolone

A

Chloroquine

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26
Q

Chloroquine
Rapidly and almost completely absorbed
from the GIT, reaches maximum plasma
concentration in about _ hrs

A

3 hrs

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27
Q

Chloroquine resistance can be reversed by

A

verapamil, desipramine, chlorphreniramine

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28
Q

most common AE of chloroquine

A

Pruritus

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29
Q

Blood AE of chloroquine

A

Hemolysis g6pd

agranulocytosis

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30
Q

AE chloroquine long term administration

A

Irreversible ototoxicity, retinopathy,

myopathy, peripheral neuropathy

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31
Q

Chloroquine inhibits

A

CYP2d6

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32
Q

Chloroquine Increases risk of ventricular arrhythmia when

co-administered with

A

amiodarone and

halichondrin

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33
Q

T or F

Chloroquine should not be given with mefloquine because of increased risk of seizures

A

T

34
Q

T or F

Chloroquine is safe in pregnancy and young children

A

T

35
Q

associates with intraerythrocytic hemozoin,
suggesting similarities to the mode of action of
chloroquine

A

Mefloquine

36
Q

mefloquine resistance

A

Increased PFRMD1

37
Q

Effective therapy for chloroquine-resistant

strains of falciparum

A

Mefloquine

CYP3A4

38
Q

mefloquine half life

A

20 days

39
Q

AE mefloquine

A 
§ Neurological and psychiatric adverse effects
§ Epigastric pain
§ Diarrhea
§ Abdominal pain
§ Headache
§ Rash
§ Alter cardiac conduction
§ Leukocytosis, thrombocytopenia, aminotransferases 
elevation have also been reported
40
Q

T or F
Pregnancy should be avoided for 3 months after
mefloquine use because of the prolonged half-life

A

T

41
Q

T or F
treatment with or after halofranine or
within 2 months of prior mefloquine administration is
contraindicated

A

T

42
Q

Considered safe in young children and it is the only
chemoprophylactic agent other than chloroquine
approved for children weighing less than 5 kg

A

Mefloquine

43
Q

1ST line therapies for severe falciparum, but its
indication for P. falciparum is no longer used due to
its adverse effects newer drugs are now used

A

Quinine and quinidine

44
Q

dextrorotatory stereoisomer of quinine

A

Quinidine

45
Q

“General parasitic poison”

A

Quinine

46
Q

T or F
Quinine is effective against all four species of
Plasmodium (blood schizonticide)

A

T

47
Q

It does decrease DNA strand separation and
transcription, thereby inhibiting protozoal protein
synthesis.

A

Quinine

48
Q

AE of quinine/quinidine

A

Cinchonism
Hypoglycemia
Blackwater fever

49
Q

T or F

Quinine causes mild uterine contractions when given in 3rd trimester of pregnancy

A

T

50
Q

T or F

Quinine should not be given concurrently with mefloquine

A

T

51
Q

Primaquine and tafenoquine are classified under ______

A

tissue schintocides

52
Q

§ Drug of choice for eradication of dormant liver forms of P. vivax and P. ovale
§ For chemoprophylaxis against all malarial species.

A

PRIMAQUINE AND TAFENOQUINE

53
Q

o Medications for P. jiroveci

A

§ Trimethoprim Sulfamethoxazole
§ Atovaquone
§ Pentamidine and Primaquine

54
Q

The drug of choice in P. jirovecii

A

TMZ

Trimethoprim Sulfamethoxazole

55
Q

Primaquine More serious adverse effect may include:

A

o Leukopenia
o Agranulocytosis
o Leukocytosis
o Cardiac arrhythmias

56
Q

§ In Tafenoquine, reported adverse effect may include:

A

o Headache
o Diarrhea
o Dizziness

57
Q

§ Component of Malarone

A

Atovaquone 250 mg +proguanil 100 mg

58
Q

Treatment and chemoprophylaxis of

falciparum

A

Atovaquone

59
Q

MOA of Atovaquone

A

o Inhibition of mitochondrial electron transport

system in protozoa

60
Q

Atovaquone half life

A

2-3 days

61
Q

Resistance to pyrimethamine:

A

mutations is
dihydrofolate reductase that decrease the binding
affinity of pyrimethamine

62
Q

AE DIAMINOPYRIDINES SULFADOXINEPYRIMETHAMINE

A

§ Occasional skin rashes and reduced
hematopoiesis
§ Excessive doses can produce a megaloblastic
anemia
§ Erythema multiforme, Steven-Johnson’s syndrome,
or toxic epidermal necrolysis

63
Q

fansidar is a combination of _____ and _____

A

sulfadoxine and

pyrimethamine

64
Q

Treatment of Chloroquine Resistant Falciparum

malaria

A

sulfadoxine and

pyrimethamine

65
Q

inhibiting protein
synthesis in a plasmodial prokaryote-like organelle,
the apicoplast.

A

Tetracycline/Doxycycline, clindamycin, Azithromycin

66
Q

For drugs other than primaquine,

A

begin 1-2 weeks
before departure (except 2 days before for
Doxycycline and Malarone) and continue for 4
weeks after leaving the endemic area (except 1
week for Malarone).

67
Q

For P falciparum, P knowlesi, and other

species not identified

A

admit the patient and

monitor for disease progression

68
Q

For P falciparum acquired in area with no chloroquine resistance

A

chloroquine or

hydroxychloroquine (DOC)

69
Q

For P falciparum acquired in areas with chloroquine resistance

A

Artemether-lumefantrine (preferred) or Atovaquone-proguanil or Quinine +
tetracycline/doxycycline/clindamycin or Mefloquine

70
Q

For P falciparum acquired in areas with mefloquine resistance

A

Artemether-lumefantrine (preferred) or Atovaquone-proguanil or Quinine + tetracycline/doxycycline/clindamycin

71
Q

DOC is Chloroquine or

hydroxychloroquine

A

P. malaria

72
Q

P vivax and P ovale acquired without

chloroquine resistance

A

chloroquine or

hydroxychloroquine (DOC)

73
Q

o P vivax acquired in areas with chloroquine

resistance

A

Artemether-lumefantrine or
Atovaquone-proguanil or Quinine +
tetracycline/doxycycline/clindamycin or
Mefloquine.

74
Q

To treat dormant liver form you

can add ______

A

primaquine/tafenoquine

75
Q

Pregnant women diagnosed with uncomplicated
malaria caused by chloroquine-resistant P.
falciparum infection in the 2nd and 3rd trimesters can
be treated with

A

artemether-lumefantrine.

76
Q

In addition, pregnant women of all gestational ages

can be treated with

A

mefloquine or a combination of

quinine sulfate and clindamycin

77
Q

T or F
Quinine treatment should continue for 7 days for P.
falciparum infections acquired in Southeast Asia and
for 3 days for infections acquired elsewhere

A

T

78
Q

DOC for amebiasis

A

Metronidazole

79
Q

characteristic stool of patient with amebiasis

A

bloody mucoid stool

80
Q

o Luminal amebicides

A

§ Diloxanide
§ Paromomycin
§ Iodoquinol

81
Q

o Systemic amebicides

A

§ Chloroquine

§ Dehydroemetine

82
Q

o Mixed amebicides (luminal and systemic)

A

§ Metronidazole

§ Tinidazole

PHARMACOLOGY (13 decks)

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