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Antiprotozoal drugs Flashcards

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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
Drug of choice for treatment and chemoprophylaxis of falciparum malaria - synthetic 4-aminoquinolone
Chloroquine
26
Chloroquine Rapidly and almost completely absorbed from the GIT, reaches maximum plasma concentration in about _ hrs
3 hrs
27
Chloroquine resistance can be reversed by
verapamil, desipramine, chlorphreniramine
28
most common AE of chloroquine
Pruritus
29
Blood AE of chloroquine
Hemolysis g6pd | agranulocytosis
30
AE chloroquine long term administration
Irreversible ototoxicity, retinopathy, | myopathy, peripheral neuropathy
31
Chloroquine inhibits
CYP2d6
32
Chloroquine Increases risk of ventricular arrhythmia when | co-administered with
amiodarone and | halichondrin
33
T or F | Chloroquine should not be given with mefloquine because of increased risk of seizures
T
34
T or F | Chloroquine is safe in pregnancy and young children
T
35
associates with intraerythrocytic hemozoin, suggesting similarities to the mode of action of chloroquine
Mefloquine
36
mefloquine resistance
Increased PFRMD1
37
Effective therapy for chloroquine-resistant | strains of falciparum
Mefloquine | CYP3A4
38
mefloquine half life
20 days
39
AE mefloquine
``` § Neurological and psychiatric adverse effects § Epigastric pain § Diarrhea § Abdominal pain § Headache § Rash § Alter cardiac conduction § Leukocytosis, thrombocytopenia, aminotransferases elevation have also been reported ```
40
T or F Pregnancy should be avoided for 3 months after mefloquine use because of the prolonged half-life
T
41
T or F treatment with or after halofranine or within 2 months of prior mefloquine administration is contraindicated
T
42
Considered safe in young children and it is the only chemoprophylactic agent other than chloroquine approved for children weighing less than 5 kg
Mefloquine
43
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
Quinine and quinidine
44
dextrorotatory stereoisomer of quinine
Quinidine
45
“General parasitic poison”
Quinine
46
T or F Quinine is effective against all four species of Plasmodium (blood schizonticide)
T
47
It does decrease DNA strand separation and transcription, thereby inhibiting protozoal protein synthesis.
Quinine
48
AE of quinine/quinidine
Cinchonism Hypoglycemia Blackwater fever
49
T or F | Quinine causes mild uterine contractions when given in 3rd trimester of pregnancy
T
50
T or F | Quinine should not be given concurrently with mefloquine
T
51
Primaquine and tafenoquine are classified under ______
tissue schintocides
52
§ Drug of choice for eradication of dormant liver forms of P. vivax and P. ovale § For chemoprophylaxis against all malarial species.
PRIMAQUINE AND TAFENOQUINE
53
o Medications for P. jiroveci
§ Trimethoprim Sulfamethoxazole § Atovaquone § Pentamidine and Primaquine
54
The drug of choice in P. jirovecii
TMZ | Trimethoprim Sulfamethoxazole
55
Primaquine More serious adverse effect may include:
o Leukopenia o Agranulocytosis o Leukocytosis o Cardiac arrhythmias
56
§ In Tafenoquine, reported adverse effect may include:
o Headache o Diarrhea o Dizziness
57
§ Component of Malarone
Atovaquone 250 mg +proguanil 100 mg
58
Treatment and chemoprophylaxis of | falciparum
Atovaquone
59
MOA of Atovaquone
o Inhibition of mitochondrial electron transport | system in protozoa
60
Atovaquone half life
2-3 days
61
Resistance to pyrimethamine:
mutations is dihydrofolate reductase that decrease the binding affinity of pyrimethamine
62
AE DIAMINOPYRIDINES SULFADOXINEPYRIMETHAMINE
§ Occasional skin rashes and reduced hematopoiesis § Excessive doses can produce a megaloblastic anemia § Erythema multiforme, Steven-Johnson’s syndrome, or toxic epidermal necrolysis
63
fansidar is a combination of _____ and _____
sulfadoxine and | pyrimethamine
64
Treatment of Chloroquine Resistant Falciparum | malaria
sulfadoxine and | pyrimethamine
65
inhibiting protein synthesis in a plasmodial prokaryote-like organelle, the apicoplast.
Tetracycline/Doxycycline, clindamycin, Azithromycin
66
For drugs other than primaquine,
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
For P falciparum, P knowlesi, and other | species not identified
admit the patient and | monitor for disease progression
68
For P falciparum acquired in area with no chloroquine resistance
chloroquine or | hydroxychloroquine (DOC)
69
For P falciparum acquired in areas with chloroquine resistance
Artemether-lumefantrine (preferred) or Atovaquone-proguanil or Quinine + tetracycline/doxycycline/clindamycin or Mefloquine
70
For P falciparum acquired in areas with mefloquine resistance
Artemether-lumefantrine (preferred) or Atovaquone-proguanil or Quinine + tetracycline/doxycycline/clindamycin
71
DOC is Chloroquine or | hydroxychloroquine
P. malaria
72
P vivax and P ovale acquired without | chloroquine resistance
chloroquine or | hydroxychloroquine (DOC)
73
o P vivax acquired in areas with chloroquine | resistance
Artemether-lumefantrine or Atovaquone-proguanil or Quinine + tetracycline/doxycycline/clindamycin or Mefloquine.
74
To treat dormant liver form you | can add ______
primaquine/tafenoquine
75
Pregnant women diagnosed with uncomplicated malaria caused by chloroquine-resistant P. falciparum infection in the 2nd and 3rd trimesters can be treated with
artemether-lumefantrine.
76
In addition, pregnant women of all gestational ages | can be treated with
mefloquine or a combination of | quinine sulfate and clindamycin
77
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
T
78
DOC for amebiasis
Metronidazole
79
characteristic stool of patient with amebiasis
bloody mucoid stool
80
o Luminal amebicides
§ Diloxanide § Paromomycin § Iodoquinol
81
o Systemic amebicides
§ Chloroquine | § Dehydroemetine
82
o Mixed amebicides (luminal and systemic)
§ Metronidazole | § Tinidazole

PHARMACOLOGY (13 decks)

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