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MEDICINAL ORGANIC CHEMISTRY > ANTI-MALARIALS > Flashcards

ANTI-MALARIALS Flashcards

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1
Q

ANTI-MALARIALS

Malaria is caused by ____ parasite

A

Plasmodium

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2
Q

ANTI-MALARIALS

Vector of malaria

A

Female Anopheles Mosquitos

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3
Q

ANTI-MALARIALS

40%, very chronic and reinfection of liver cells

Plasmodium species

A

P. vivax

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4
Q

ANTI-MALARIALS

50%, Most common, severe, and infects 65% of the patient’s erythrocytes

Plasmodium species

A

P. falciparum

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5
Q

ANTI-MALARIALS

10%, relapses are common

Plasmodium species

A

P. malariae

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6
Q

ANTI-MALARIALS

Least common

Plasmodium species

A

P. ovale

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7
Q

ANTI-MALARIALS

Zoonotic

Plasmodium species

A

P. knowlesi

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8
Q

CINCHONA ALKALOIDS

Lethal for all Plasmodium schizonts and gametocytes

A

Quinine Sulfate

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9
Q

CINCHONA ALKALOIDS

Quinidine is primarily indicated for ____.

A

Cardiac Arrhythmia

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10
Q

CINCHONA ALKALOIDS

More potent and toxic anti-malarial that is a stereoisomer of quinine

A

Quinidine

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11
Q

CINCHONA ALKALOIDS

For nocturnal leg cramps

A

Quinine Sulfate

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12
Q

CINCHONA ALKALOIDS

Adverse effect of Quinine Sulfate

A

Abortifacient

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13
Q

CINCHONA ALKALOIDS

For malaria caused by chloroquine-resistant P. falciparum strains

A

Quinine Sulfate

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14
Q

CINCHONA ALKALOIDS

Toxic syndrome characterized by tinnitus, headache, nausea, and disturbed vision.

A

Cinchonism

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15
Q

4-AMINOQUINOLINES

Main antimalarial drug used for both prophylaxis and treatment of malaria

A

Chloroquine

HCl - Parenteral; PO4 - Oral

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16
Q

4-AMINOQUINOLINES

Highly protein bound anti-malarial

A

Hydroxychloroquine

Plaquenil

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17
Q

4-AMINOQUINOLINES

Prophylaxis for malaria that is associated with higher incidence of hepatitis and agaranulocytosis

A

Amodiaquine

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18
Q

4-AMINOQUINOLINES

Drug of choice for malarial suppression

A

Mefloquine

Lariam

19
Q

4-AMINOQUINOLINES

Drug of choice for Erythrocytic falciparum malaria except resistant strains

A

Chloroquine (Aralene)

HCl - Parenteral; PO4 - Oral

20
Q

8-AMINOQUINOLINES

MOA of primaquine

A

Disruption of parasites mitochondria

21
Q

8-AMINOQUINOLINES

Drug of choice for acute attack of Plasmodium vivax that has the narrowest spectrum of activity

A

Primaquine

22
Q

4-AMINOQUINOLINES

A schizonticide that exacerbate mental disorders

A

Mefloquine

Lariam

23
Q

8-AMINOQUINOLINES

Most effective against malarial parasite in the liver, but not effective against parasites within erythrocytes

A

Primaquine

24
Q

POLYCYCLIC

Tetracycline that inhibits the pathogen’s protein synthesis

A

Doxycycline

25
Q

POLYCYCLIC

Drug of choice for Leptospira interrogans

A

Doxycycline

26
Q

POLYCYCLIC

Prophylaxis for malaria that is containdicated in children and in sunny areas

A

Doxycycline

27
Q

POLYCYCLIC

Arrest tissue conduction in cardiac muscles

A

Halofantrine

28
Q

POLYCYCLIC

MOA: Inhibits the formation of B hematin by forming a complex with hemin

A

Lumefantrine

29
Q

POLYCYCLIC

Most toxic anti-malarial drug

A

Quinacrine

30
Q

POLYCYCLIC

Also a sclerosing agent and for varicose veins

A

Quinacrine

31
Q

POLYCYCLIC

An acridine dye which can cause yellow coloration

A

Quinacrine

32
Q

POLYCYCLIC

Methyl ether derivative of dihydroartemesinin

A

Artemether

33
Q

POLYCYCLIC

Hemisuccinate derivative of the active metabolite dihydro-artemisin

A

Artesunate

34
Q

FIXED COMBINATION

Prophylaxis and treatment of chloroquine resistant malaria

A

Sulfadoxine and Pyrimethamine
(Fansidar)

35
Q

FIXED COMBINATION

MOA of Sulfadoxine and Pyrimethamine:
Inhibition of ____ biosynthesis and ____

A
  1. Folic acid
  2. Dihydrofolate reductase
36
Q

FIXED COMBINATION

Effective against erythrocytic and exo-erythrocytic plasmodium

A

Atovaquone + Proguanil
(Malarone)

37
Q

FIXED COMBINATION

For resistant malaria

A

Atovaquone + Proguanil
(Malarone)

38
Q

FIXED COMBINATION

MOA of Atovaquone + Proguanil
(Malarone):
____ inhibition and ____ damage

A
  1. Dihydrofolate reductase
  2. Mitochondria
39
Q

FIXED COMBINATION

Proguanil is a prodrug of ____.

A

Cycloguanil

40
Q

FIXED COMBINATION

Artemether + Lumefantrin interfere with ____ metabolism to disrupt the parasites erythrocytic stage.

A

Heme

41
Q

NEW DRUG APPROACHES

Isolated from a Streptomyces fermentation broth in 1980

A

Fosmidomycin

42
Q

NEW DRUG APPROACHES

MOA OF Fosmidomycin:
1. ____ pathway inhibition
2. ____ reductase inhibition

A
  1. Non-mevalonate
  2. Glutathione
43
Q

NEW DRUG APPROACHES

Fosmidomycin inhibits the enzyme ____.

A

DOXP reductoisomerase

1-deoxy-D-xylulose-5-phosphate

MEDICINAL ORGANIC CHEMISTRY (17 decks)

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