C3 Flashcards
1
Q
Antiprotozoal and antihelminthic drugs
A
chloroquine mefloquine quinine lumefantrine artemether primaquine metronidazole atovaquone proguanil mebendazole ivermectin niclosamide
2
Q
DRUGS FOR MALARIA?
A
Chloroquine Artemether Quinine Mefloquine Primaquine
3
Q
Chloroquine MOA?
A
- accumulates in the food
vacuole of plasmodia and prevents polymerization of the hemoglobin
breakdown product heme into hemozoin - Intracellular accumulation
of heme is toxic to the parasite - Resistance in P.falciparum: decreased
intravacuolar accumulation of chloroquine via a transporter
4
Q
Chloroquine PharmacoKinetix?
A
- rapidly absorbed when
given orally - is widely distributed to tissues and have
large volume of distribution - Antacids may decrease oral absorption
of the drug - Elimination: unchanged in the urine.
5
Q
Chloroquine Clinical use?
A
- acute attacks of non-falciparum and sensitive falciparum malaria
- chemoprophylaxis
- autoimmune disorders (rheumatoid arthritis)
6
Q
Chloroquine Toxicity?
A
- Low doses:
1. GI irritation
2. skin rash
3. headaches - High doses:
1. severe skin lesions
2. peripheral neuropathies
3. myocardial depression
4. retinal damage
5. auditory impairment
6. toxic psychosis.
7
Q
what about Artemether?
A
- metabolized in the food vacuole of the parasite –> toxic free radicals
- blood schizonticides active against P.falciparum (also MDRs)
- best used in combination with other agents
- the only drugs reliably effective against quinine-resistant strains
- Adverse effects are mild
8
Q
Quinine MOA?
A
- form complexes with double-stranded DNA to prevent strand separation –> block of DNA replication and transcription to RNA
- it is blood schizonticide
9
Q
Quinine PharmacoKinetix?
A
- bioavailability: rapidly absorbed orally
- metabolized before renal excretion
- I.V. administration is possible in severe infections
10
Q
Quinine Clinical use?
A
- in P.falciparum infections resistant to chloroquine (for those who tolerate oral treatment)
- commonly used with doxycycline or clindamycin to shorten the duration of therapy and limit toxicity
- should not be used routinely for prophylaxis
11
Q
Quinine Toxicity?
A
- cinchonism (GI distress, headache, vertigo, blurred vision, and tinnitus)
- Severe overdose: disturbances in cardiac conduction
- Hematotoxic effects: G6PD-deficient
- Blackwater fever (intravascular hemolysis) is a rare and sometimes fatal complication in quinine-sensitized persons
- it is contraindicated in pregnancy
12
Q
Mefloquine MOA?
A
unknown :)
13
Q
Mefloquine PharmacoKinetix?
A
can only be given orally because of local irritation
14
Q
Mefloquine clinical use?
A
- first-line drug (taken weekly) for prophylaxis
- an alternative drug to quinine in acute attacks and uncomplicated infections resulting from P falciparum.
15
Q
Mefloquine Toxicity?
A
- GI distress
- skin rash, headache, and dizziness
- At high doses:
cardiac conduction defects, psychiatric disorders, and neurologic effects
