Test 3 Pharm: Antimalarials

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dmatta
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35835
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Test 3 Pharm: Antimalarials
Updated:
2010-10-02 19:44:51
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Malarial meds
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TEST 3 REVIEW OF ANTIMALARIALS
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  1. Malaria signs/symptoms:
    Paroxysm: relapsing or periodic fever

    • Periodicity corresponds to erythrocytic
    • development (24, 48 or 72hours)
    • –benign tertian: P. vivax
    • –malignant tertian : P. falciparum
    • –quartan : P. malariae

    The pattern of intermittent chills/fever mirrors the synchronized parasite development in an infected person’s blood

    • This response is primarily due to toxins released with rupture of RBCs containing
    • schizonts
  2. USE OF ANTIMALARIAL DRUGS
    1. Causal prophylaxis – blocks liver growing stages of parasite

    2. Suppressive prophylaxis – doesn’t block liver stage but as come out into blood blocks parasitemia from developing

    3. Post exposure prophylaxis – prevent recurrence

    4. Intermittent Presumptive Therapy – give ineffective drug once a month to pregnant woman, newborns

    5. Radical cure – kill hypnozodic stages in liver (P. vivax, P. ovale)
  3. Suppressive prophylaxis for P. vivax in travelers: prevents the primary blood stage
    infection, does not prevent relapse from hypnozoite, Rx 28 days after return for doxy and MQ
    • DOXYCYCLINE
    • MEFLOQUINE
    • MALARONE (PROGUANIL AND ATOVAQUONE)
  4. CASUAL PROPHYLAXIS: TARGETS THE GROWING IN THE LIVER STAGES
    • PREVENT/KILL THE PRIMARY LIVER SCHIZONT
    • PREVENT/KILL THE HYPNOZOITE
    • RX 7 DAYS, HAS TO BE TAKEN EVERY 14 DAYS

    PRIMAQUINE
  5. PRESUMPTIVE ANTI-RELAPSE THERAPY (PART)
    TAKE PRIMAQUINE AFTER RETURN
  6. SUPPRESSIVE PROPHYLAXIS: SUPPRESSION OF BLOOD STAGES
    • CHLOROQUINE
    • MEFLOQUINE
    • DOXYCYCLINE
    • MALORONE (PROGUANIL AND ATOVAQUONE)
  7. MAJOR ANTIMALARIAL DRUGS
    • CHLOROQUINE
    • MEFLOQUINE
    • DOXYCYCLINE
    • PRIMAQUINE
    • MALARONE (PROQUANIL AND ATOVAQUONE)
  8. TREATMENT OF ACUTE UNCOMPLICATED MALARIA
    • MALARONE (ATOVOQUONE/PROGUANIL)
    • COARTEM (ARTEMETHER/LUMEFANTRINE)
    • ACT = Artemisinin Combination Therapy. Taken for treatment of malarya, used in combination to prevent resistance
  9. TREATMENT OF SEVERE MALARIA, INCLUDING CEREBRAL MALARIA
    ARTESUNATE IV (COMPASSIONATE USE IND VIA CDC)
  10. PROPHYLAXIS FOR TRAVELERS, MILITARY, PEACE CORPS, ETC
    • MALARONE FIRST CHOICE
    • MEFLOQUINE SECOND CHOICE
  11. POSTEXPOSURE PROPHYLAXIS (PREVENTS RELAPSE)
    PRIMAQUINE
  12. CHLOROQUINE
    • Mech:
    • Blocks the polymerization of soluble heme by plasmodium; soluble heme toxic to pathogen

    • Use:
    • - Clinical cure
    • - Suppressive prophylactic
    • - Highly active against blood stages

    • Toxicity:
    • Dose related retinopathy; hearing issues; cardiac issues; pruritus (itching) of palms, soles, and scalp; nausea and vomiting on empty stomach

    • Metab/kinetics
    • - Well absorbed orally
    • - Can be gicen IM for severe cases
    • - metabolysm: desethylchloroquine is active VS PARASITES!!

    • Interaction/resistance
    • Some falciparum is resistant to chloroquine via PfCRT--> transporter that pumps out chloroquine from digestive vacuole
  13. PRIMAQUINE
    • Mech:
    • Possibly intermediate oxidants form that are toxic to exoerythorcytic forms

    • Use:
    • - Casual prophylaxis and radical cure.
    • - Eradicates hepatic (latent) stages of vivax +ovale

    • Toxicity:
    • - Leucopenia
    • - Agranulocytosis
    • - Hemolysis in pts that are G6PD deficient (hemolytic anemia)
    • - G6PD toxicity

    • Interaction/resistance
    • Falciparum is resistant to primaquine. Can lead to radical cures for P. vivax and P. ovales b/c effective against the exoerythrocytic form in liver. NOTE: Effective against erythrocytic forms


    • Primaquine is the only thing that works to kill the dormant form in the liver.
  14. Mefloquine
    • Mech:
    • Blood schizonticidal activity
    • Not active against gametophytes or hepatic stages of vivax.

    • Use:
    • For chloroquine resistant falciparum
    • Prophylaxis for travelers

    • Interaction/resistance:
    • Contraindicated if: hx of epilepsy (can cause seizures if on anticonvulsive therapy), less than 2 yrs old, taking drugs that alter cardiac condition
  15. Artemisinin
    • Mech:
    • Reduces gametocyte form so can reduce transmission ; artemisinin reduces
    • parasite load after which the partner drug (ex. Mefloquine) can finish off
    • parasite due to being in supratherapeutic levels even if parasite is resistant;
    • MOA is possibly blocking of SERCA Ca2+ pump in parasite or formation of highly
    • active iron-oxo species

    • Use:
    • Can use as Aremisinin combination therapy (ACT); used on multidrug resistant P. falciparum
    • Use for severe malaria, in the US, including cerebral malaria (Artesunate IV)
    • Artesunate IV also used in high levels of parasites in blood

    • Metabolism/kinetics:
    • Obtained from plants; IV artesunate is 35% more efficacious than quinine
    • Used due to lack of timely access to IV quinidine, or if quinidine intolerance or contraindication, or if quinidine failure
  16. MALARONE (Atovaquone/proguanil)
    • Use:
    • Suppressive prophylactic
    • Taken with milk or food to increase absorption
    • Suppression of blood stages; All four types of malaria if uncomplicated and not progressing rapidly
    • Prophylaxis for travelers
    • Acute uncomplicated malaria

    Highly active against blood stages, partly against liver stages

    • Metabolism
    • –Atovaquone
    • »Not metabolized in humans
    • »Excreted via bile

    • –Proguanil
    • »Metabolized to active triazine (cycloguanil)
    • »Affected by CYP2C19 mutations
  17. COARTEM (Artemether/lumefrantine)
    First FDA approved ACT

    • Use:
    • Acute uncomplicated Malaria

    • Contraindications:
    • –Pregnancy or breast-feeding
    • –Heart problems (eg, irregular heartbeat, QT prolongation)
    • –Recent use of halofantrine or other drugs that can cause QT prolongation

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