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PHARM 2 > anti-malarials > Flashcards

anti-malarials Flashcards

1
Q

chloroquine

A

tx and prophylaxis

P. vivax and P. ovale - active against blood parasites - NOT liver stage

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2
Q

DOC for p.vivax and ovale

A

chloroquine

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3
Q

DOC in tx in non-falciparum and sensitive uncomplicated falciparum malaria

A

chloroquine

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4
Q

chloroquine MOA

A

concentrates in parasite food vaculoes

prevents biocrystallization of Hgb breakdown product heme to non-toxic hemozin = accum of heme results in lysis of parasite and RBC

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5
Q

chloroquine resistance

A

putative transporter: PfCRT

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6
Q

chloroquine AE

A

fatal = most common drug used for suicide

pruritus

hemolysis - G6PD

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7
Q

chloroquine contraindication

A

psoriasis, porphyria, retinal abnormalities

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8
Q

parenteral tx of severe falciparum

A

quinidine

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9
Q

oral tx of falciparum (alt in chloroquine resistant areas)

A

quinine

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10
Q

first line for severe falciparum

A

quinine/quinidine

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11
Q

quinine/quinidne use

A

good against BLOOd - not liver stages

depresses O2 uptake and carb metabolism

intercalates into DNA = disrupting replication/transcription

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12
Q

quinine/quinidine AE

A

cinchonism - tinnitus, HA, nausea

HS

hematological abnl: thrombocytopenia, agranulocytosis

hypoglycemia - stimulates insulin release

uterine contractions: still used in pregnant pt (benefits outweigh risks)

hypotension

QT prolongation

blackwater fever: likely HS rxn - hemolysis and hemolgobinuria

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13
Q

quinine/quinidine contraindications

A 
visual/auditory problems
cardiac
don't use with mefloquine
can inc levels of warfarin and digoxin
renal insuff (dec dose)

Category C pregancy

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14
Q

mefloquine

A

works against chloroquine resistant strains
related to quinine

MOA: destroys asexual blood forms

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15
Q

only medication recommended for chemoprophylaxis in pregannt women in chloroquine resistant areas

A

mefloquine

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16
Q

mefloquine use

A

effective against most strains of p. falciparum and vivax

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17
Q

what combo is used in uncomplicated malaria in south east asia

A

mefloquine + artesunate

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18
Q

mefloquine AE

A

neuro and psych: ringing, anxiety, depression, hallcuination

weekly dosing: n/v/d, beahviro disturbances

higher dosing: leukocytosis, thrombocytopenia, aminotransferase, arrhythmias

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19
Q

mefloquine contraindications

A

hx of epilepsy, psych disorders, arrhythmia, cardiac conduction defects

DONT GIVE WITH quinine/quinidine, halofantrine

safe in young and pregant

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20
Q

DOC eradication of dormant liver forms in vivax and ovale

A

primaquine

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21
Q

Primaquine use

A

acute vivax and ovale and terminal prophylaxis of vivax and ovale

chemoprophylaxis against falciparum and vivax

22
Q

primaquine MOA

A

not understood - maybe oxidants disrupting mitochondria binding to DNA

23
Q

primaquine AE

A

rare - leukopenia, agranulocytosis, leukocytosis, cardiac arrhtymias

**hemolysis or methemoglbinemia - esp in G6PD pt’s

24
Q

what to test for before administering primaquine

A

G6PD - if deficient, must deal with dormant stages, cannot take at all

25
Q

primaquine contraindications

A

DO NOT USE DURING PREGNANCY - until fetus is born and found if deficient

26
Q

malarone

A

(combo of atovaquone + proguanil)

tx and prophylaxis of falciparum

NOT SAFE IN PREGANCY

27
Q

malarone MOA

A

disrupt mitochondrial electron transport

28
Q

pyrimethamine

A

folate synth inhibitor

29
Q

proguanil

A

folate synth inhibitor

30
Q

sulfadoxine

A

folate synth inhibitor

31
Q

folate synth inhibitor application

A

chemoprophylaxis - only in combo of proguanil + chloroquine (not recommended)

intermittent therapy - high risk pt’s recieve intermittent therapy regardless of infection status

tx chloroquine resistant falciparum - NOT used in severe malaria

32
Q

pyrimethamine + proguanil

A

act slowly against RBC form of malaria

inhibit plasmodial dihydrofolate reductase

33
Q

proguanil active against which form/s

A

only active against some hepatic forms

34
Q

sulfonamides active against which form

A

weakly against RBC schizonts

inhibit dihydropteroate synthase

35
Q

folate synthesis inhibitors AE

A

well tolerated

proguanil - mouth ulcers

pyrimethamine-sulfadoxine = steven johnson

sulfadoxine - blood, GI,CNS,derm, renal toxic

proguanil and pyrimethamine-sulfadoxine = safe in pregancy

36
Q

doxycycline

A

active against RBC schizonts NOT liver stage

complete tx for severe facliparum (alongside quinine) after initial tx

must be taken daily as chemoprophylaxis

37
Q

doxycycline AE

A

photosensitive
discoloration/hypoplasia of teeth
not safe in pregnancy
fatal hepatoxicity (in pregnancy(

38
Q

artemisin

A

artesunate
artemether
dihydroartemesinin (oral only)
coartem (artemether + lumefantrine)

39
Q

artemesin use

A

IV severe falciparum malaria - don’t use alone to protect against resistance

only active in blood stage - not liver stage

40
Q

artemesin MOA

A

binds iron, breaks down peroxide bridges = generates free radicals that damage parasites

very short t 1/2 - IV therapy + logner acting agent

41
Q

artemisin AE

A

neurotoxicity, QT prolongation

safer in 2nd and 3rd trimersters

only use in 1st if severe

42
Q

other antimalarials:

A

clindamycin - doxy alternative

halofantrine (RBC stages, teratogenic)

lumefantrine (RBC stages, minor QT prolongation)

43
Q

DOC chemophrophylaxis in pregnant women

A

chloroquine

if chloroquine resistant: mefloquine

44
Q

DOC SEVERE malaria tx in pregancy 1st trimester

A

quinidine or artesunate

45
Q

DOC SEVERE malaria tx in pregnancy 2-3rd trimester

A

1st: artesunate
2nd: artemether

46
Q

p. falciparum uncomplicated DOC

A

1) chloroquine/hydrochloroquine

chloroquine resistant:

1) atovoquone-proguanil/malarone
2) co-artem
3) quinine+doxycycline
4) mefloquine

47
Q

P. malariae DOC

A

chloroquine/hydroxychloroquine

48
Q

P. vivax/ovale DOC

A

1) chloroquine + primaquine

2) hydroxychloroquine + primaquine

49
Q

P. vivax DOC in chloroquine resistant

A

1) quinine + doxycycline + primaquine
2) atovaquone - progaunil + primaquine
3) mefloquine + primaquine

50
Q

uncomplicated malaria in pregnancy DOC

A

1)chloroquine/hydrochloroquine

  • chloroquine resistant (falciparum)
    1) mefloquine
    2) quinine + clindamycin
  • chloroquine resistant (vivax)
    Mefloquine
51
Q

DOC severe malaria in all species

A

1) Quinidine + doxycycline or clindamycin

2) artesunate, followed by atovaquone-proguanil, clindamycin, or mefloquine

PHARM 2 (18 decks)

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