Pharm Final Lecture 3

Front 1

describe malaria and how it is infected ect

Back 1

Plasmodium sporozoites enter the liver, form tissue schizonts, and undergo exoerythrocytic schizogony (blocked by primaquine) to produce merozoitesreleased from the liver invade erythrocytes and form trophozoites that undergo erythrocytic schizogony (antimalarial drugs). Some trophozoites develop into male and female gametocytes, which must subsequently pass back into a mosquito before they can develop into sporozoites

Front 2

Tissue schizonticides

Back 2

Eliminate developing or dormant liver forms (primaquine)

Front 3

Blood schizonticides

Back 3

Act on erythrocytic parasites chloroquine, quinine, mefloquine, pyrimethamine, proguanil

Front 4

Gametocides

Back 4

: Kill sexual stages and prevent transmission to mosquitoes,
primaquine
also quinine does for p vivax and ovale

Front 5

primaquine

Back 5

Anti-malarial (8-aminoquinoline) Unknown mechanism. NOT effective in erythrocytic forms; eliminate liver forms; kill sexual stages prevent transmission ot mosquitoes; pre erythrocytic prevents preleapse due to vivax
Tissue schizonticide and gametocide
ORAL
NOT effective on erythrocytic forms.
Side effects: Well tolerated, except:
AVOID IN: G6PD-deficient pts-hemolysis, Myelosuppressed
, Pregnancy
Max [plasma]=1-2 hrs (FASTEST)
T 1/2 = 3-8 hrs.
Urine excretion

Front 6

chloroquine

Back 6

CQ Anti-malarial (4-aminoquinoline)
Concentrates in the food vacuole; prevents polymeration of heme into hemozoin. (Parasite eats Hb for nutrients, but heme is toxic to it, so it converts it to hemozoin); lysis of parasite and RBC.
**Blood schizonticide -->erythrocytic paracites
ORAL
Malaria (DOC for tx AND prophylaxis)
Used alone for P.falciparum and P.malariae; w/combo of primaquine for P. vivax or P. ovale.
***Increasing drug resistance
***GI distress, N/V
CONTRAINDICATIONS: Psoriasis or porphyria, Retinal abnormalities
, Myopathy
Don't take w/Kaolin or Ca2+/Mg antacids → reduce absorption
Max [plasma]=3 hrs. t1/2 = 1-2 months (LONGEST)
Urine excretion
****Safe in pregnancy and kids

Front 7

pre erythrocytic malarial drug

Back 7

primaquine

Front 8

fastest malrial drug

Back 8

primaquine; 1-2 hours lasts 3-8 hours

Front 9

drugs that causes G6PD deficient pts hemolysis

Back 9

primaquine and MQ

Front 10

DOC for malarial treatment an dprophylaxis

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chlorquine ---P. falciparum P malariae
combo of primauqine for vivax and ovale

Front 11

quinine

Back 11

used for severe malaria
Anti-malarial. From the bark of a cinchona tree
Unknown mechanism.
Blood schizonticide -->NOT active against liver schinzonts.
(all 4 species) Gametocidal (P.vivax & P.ovale)
ORAL
Esp. P.falciparum
Give w/doxycycline or other Ab. to reduce duration to 3 day max.
NOT for prophylaxis (too much toxicity) NOT active on liver stage parasites.
"Cinchonism":- Tinnitus, HA, Nausea/dizziness, flushing, Visual disturbances
Caution w/cardiac =****QT prolongation is common
CONTRAINDICATION: anyone taking or recently took mefloquine (cardiac arrest and convulsions) Max [plasma]=1-3 hrs.
T1/2 = 18 hours
--higher rate in infected pts. due to increased protein binding
Liver metabolism;
urine excretion
2nd choice w/Ab for treatment of malaria. (combine w/any of the following: tetracycline, doxycycline, clindamycine, azithromycin)

Front 12

quinidine

Back 12

not used much due to shorter 1/2 life
Anti-malarial. From the bark of a cinchona tree Unknown mechanism.
Blood schizonticide (all 4 species)
Gametocidal (P.vivax & P.ovale) ORAL Esp. P.falciparum
Give w/doxycycline or other Ab. to reduce duration to 3 day max.
NOT for prophylaxis (too much toxicity) NOT active on liver stage parasites.
"Cinchonism": Tinnitus, HA, Nausea/dizziness, Flushing, Visual disturbances
Caution w/cardiac =QT prolongation is common
CONTRAINDICATION: anyone taking or recently took mefloquine (cardiac arrest and convulsions) Max [plasma]=1-3 hrs.
T1/2 = 18 hours
--higher rate in infected pts. due to increased protein binding
Liver metabolism;
urine excretion
2nd choice w/Ab for treatment of malaria. (combine w/any of the following: tetracycline, doxycycline, clindamycine, azithromycin)

Front 13

mefloquine

Back 13

MQ
Anti-malarial (synthetic 4-quinoline methanol) Unknown mechanism.
Blood schizonticide
ORAL-->local irritation
Tx. of Chloroquine-resistant P.falciparum (last choice for tx)
Prophylaxis for malaria
Not for severe infections; (quinine preferred d/t more rapid activity and less resistance)
NOT for use WITH quinine or quinidine.
Side effects: N/V, dizziness,
Sleep & behavioral disturbances
CONTRAINDICATIONS: epilepsy, phychiatric disorders, cardiac conditions
G6PD deficiency (hemolysis d/t decreased NADPH and GSH) Max [plasma]=18 hrs.
(SLOWEST)
T1/2=20 days (weekly dosing)

Front 14

pyrimethamine

Back 14

Folate reductase inhibitor Inhibition of plasmodial dihydrofolate reductase.
Blood schizonticide--> all four species
***also treats toxoplasmosis
Chemoprophylaxis (in combo w/chloroquine) for malaria -- T 1/2=3.5 days (LONG)

Front 15

proguanil

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Folate reductase inhibitor Inhibition of plasmodial dihydrofolate reductase.
Blood schizonticide-->treats all four species
Chemoprophylaxis (in combo w/chloroquine) for malaria -- T 1/2= 16 hrs. (SHORT)

Front 16

antibodies for malaria?

Back 16

tetracycline, doxylcine, clindamycin, azithromycin

--erythrocyte shizonts all 4 species

Front 17

atovaquone

Back 17

inhibits mitochondrial E transport dec ATP synthesis....for malaria????

Front 18

malarone

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Folate reductase inhibitor Inhibition of plasmodial dihydrofolate reductase + inhibits nucleic acid and ATP in parasite by messing up transport.
Blood schizonticide -- Chloroquine-resistant malaria (Treatment or prophylaxis) -- A combo drug of proguanil + atovaquone

Front 19

2 gametocidal drugs for malaria

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primaquine and quinine (only vavax ovale)

Front 20

2 drugs that can cause hemolysis w/ G6PD def?

Back 20

mefloquine and primaquine

Front 21

what is cinochonism?

Back 21

tinnitius HA nausea/dizzy, flush, visual distubances in quinine malarial drug

Front 22

do not take MQ w/ ?

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quinine or quinidine

Front 23

drug for CQ resistant P falciparum?

Back 23

MQ

Front 24

2 drugs folate reductase inhibitors?

Back 24

pyrimehtamine, proguanil
malarone is proguanil and atovaquone