ANTIMALARIAL Flashcards

1
Q

VECTOR of MALARIA

A

Anopheles mosquito

FEMALE ONLY

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2
Q

CAUSATIVE AGENT of MALARIA

A

Plasmodium ovale
Plasmodium malariae
Plasmodium falciparum
Plasmodium vivax
Plasmodium knowlesi

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3
Q

causative agent of malaria that is considered ZOONOTIC

ZOONITC - animal to animal transmission only

A

Plasmodium knowlesi

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4
Q

2 major stages for malarial cycle

A
  1. exoerythrocytic
  2. erythrocytic
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5
Q

MOST PATHOGENIC causative agent of MALARIA

A

P. falciparum

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6
Q

DIFFERENT DRUGS FOR MALARIA

A
  • 4-aminoquinolines
  • 8-aminoquinolines
  • natural anti-malarial
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7
Q

MALARIA

Plasmodium is a parasite coined from ____ which means BAD AIR

A

mala aria

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8
Q

other names for MALARIA

A

Ague
Intermittent fever
Marsh fever
The Fever

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9
Q

MALARIA

causative agent that is MILDER; RARELY FATAL

A

P. malariae

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10
Q
A
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11
Q

MALARIA

  • he DEBUNKED the idea that YELLOW FEVER and other vector-borne diseases are AIR-BORNE
  • he proposed that HINDI GALING SA HANGIN ang MALARIA; it is carried by a VECTOR
A

DR. RONALD ROSS

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12
Q

MALARIA

3 potential ways to control malaria

A
  • Vector control
  • Drug therapy
  • Vaccination
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13
Q

MALARIA | CAUSATIVE AGENTS

  • 50%, MOST COMMON
  • SEVERE form
  • MOST VIRULENT
  • can infect 65% of the patient’s erythrocytes
A

P. falciparum

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14
Q

MALARIA | CAUSATIVE AGENTS

  • 40%, VERY CHRONIC
  • RECURRENCE is possible
  • can cause REINFECTION of the LIVER cells
A

P. vivax

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15
Q

MALARIA | CAUSATIVE AGENTS

  • 10%
  • RELAPSES are common
A

P. malariae

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16
Q

MALARIA | CAUSATIVE AGENTS

  • LEAST common
A

P. ovale

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17
Q

CINCHONA ALKALOIDS

  • LETHAL for ALL Plasmodium schizonts and gametocytes from P. vivax and P. malariae
  • indicated for malaria caused by chloroquine-resistant P. falciparum strains
  • used for NOCTURNAL LEG CRAMPS
  • SE: abortifacient
A

QUININE SULFATE

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18
Q

CINCHONA ALKALOIDS

QUININE SULFATE:
side effects

A

abortifacient

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19
Q

CINCHONA ALKALOIDS

  • MORE POTENT anti-malarial
  • stereoisomer of quinine but is primary indicated for CARDIAC ARRHYTHMIAS
A

QUINIDINE

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20
Q
  • TOXIC syndrome characterized by: tinnitus, headache, nausea, disturbed vision
A

CINCHONISM

21
Q

what is the proposed MOA of quinine and related compounds?

A

inhibitory effect on ATP (proposed only)
MOA is mysterious – not known

22
Q

4-AMINOQUINOLINES

  • MAIN anti-malarial drug for PROPHYLAXIS and treatment of malaria
  • used also for EXTRA-INTESTINAL AMOEBIASIS
  • DOC for ERYTHROCYTIC FALCIPARUM malaria, EXCEPT RESISTANT STRAIN
  • ADR: retinopathy, hemolysis, muscle weakness, exacerbation of psoriasis, porphyria, impaired liver function
A

CHLOROQUINE

23
Q

4-AMINOQUINOLINES

CHLOROQUINE:
parenteral

24
Q

4-AMINOQUINOLINES

CHLOROQUINE:
oral

A

PO₄
phosphate

25
Q

4-AMINOQUINOLINES

  • HIGH PROTEIN BOUND (remains in the body for OVER A MONTH)
A

Hydroxychloroquine

26
Q

4-AMINOQUINOLINES

  • PROPHYLAXIS for malaria
  • associated with higher incidence of HEPATITIS and AGRANULOCYTOSIS
A

Amodiaquine

27
Q

4-AMINOQUINOLINES

  • SCHIZONTICIDE (newest member)
  • exacerbate mental disorders
  • DOC for MALARIAL SUPPRESSION
A

Mefloquine

28
Q

8-AMINOQUINOLINES

  • NARROWEST spectrum of activity
  • most effective against malarial parasite in the LIVER but NOT effective against parasites within eryhthrocytes
  • MOA: disruption of parasites’ mitochondria
  • DOC: for ACUTE attack of Plasmodium vivax
A

PRIMAQUINE

29
Q

8-AMINOQUINOLINES

PRIMAQUINE:
most effective against parasites in the ____

30
Q

8-AMINOQUINOLINES

PRIMAQUINE:
NOT effective against parasites within ____

A

erythrocytes

31
Q

8-AMINOQUINOLINES

PRIMAQUINE MOA:
disruption of ____

A

parasites’ mitochondria

32
Q

8-AMINOQUINOLINES

PRIMAQUINE:
DOC

A

acute attack of Plasmodium vivax

33
Q

POLYCYCLIC ANTIMALARIAL DRUGS

  • a TETRACYCLINE that inhibits the pathogen’s PROTEIN SYNTHESIS
  • PROPHYLAXIS for malaria
  • CI in children and in areas with greatest sunlight
A

DOXYCYCLINE

34
Q

POLYCYCLIC ANTIMALARIAL DRUGS

DOXYCYCLINE:
MOA

A

inhibits pathogen’s PROTEIN SYNTHESIS

35
Q

POLYCYCLIC ANTIMALARIAL DRUGS

DOXYCYCLINE:
contraindication

A

in children & in areas with greatest sunlight

36
Q

POLYCYCLIC ANTIMALARIAL DRUGS

  • can ARREST TISSUE CONDUCTION in cardiac muscles
A

Halofantrine

37
Q

POLYCYCLIC ANTIMALARIAL DRUGS

  • proposed MOA: inhibition of β-hematinin by forming complex with hemin
A

Lumefantrine

38
Q

POLYCYCLIC ANTIMALARIAL DRUGS

  • MOST TOXIC antimalarial drug
  • ACRIDINE DYE (can cause YELLOW color of skin, tissues, etc.)
  • tx of malaria and a SCLEROSING AGENT
A

QUINACRINE

39
Q

POLYCYCLIC ANTIMALARIAL DRUGS

QUINACRINE:
can cause ____ color of skin, tissues, etc.

40
Q

POLYCYCLIC ANTIMALARIAL DRUGS

ARTEMISININ:
* is a METHYL ETHER derivative of dihydroartemesinin

A

ARTEMETHER

41
Q

POLYCYCLIC ANTIMALARIAL DRUGS

ARTEMISININ:
* is a HEMISUCCINATE derivative of the active metabolite dihydroartemisin

A

ARTESUNATE

42
Q

FIXED COMBINATION

  • PROPHYLAXIS and treatment of chloroquine resistant malaria
  • MOA: inhibition of FOLIC ACID biosynthesis and DIHYDROFOLATE REDUCTASE
A

Sulfadoxine + Pyrimethamine

43
Q

FIXED COMBINATION

SULFADOXINE + PYRIMETHAMINE:
MOA

A

inhibition of FOLIC ACID biosynthesis and DIHYDROFOLATE REDUCTASE

44
Q

FIXED COMBINATION

  • effective against ERYTHROCYTIC and EXOERYTHROCYTIC plasmodium
  • used for RESISTANT MALARIA
  • MOA: inhibition of dihydrofolate reductase and damage to the parasite’s mitochondria
A

ATOVAQUONE & PROGUANIL

45
Q

FIXED COMBINATION

ATOVAQUONE & PROGUANIL:
MOA

A

inhibition of dihydrofolate reductase and damage to the parasite’s mitochondria

46
Q

FIXED COMBINATION

PROGUANIL is a prodrug of ____

A

CYCLOGUANIL

47
Q

FIXED COMBINATION

  • interfere HEME metabolism → interfere parasites in ERYTHROCYTIC stage
  • MOST ESTABLISHED MOA
A

Artemether & Lumefantrin

48
Q

NEW DRUG APPROACHES

  • isolated from Streptomyces fermentation broth in 1980
  • inhibition of NON-MEVALONATE PATHWAY & GLUTATHIONE REDUCTASE

inhibition of glutathion - no antioxidant - increase free radicals - cell death

A

FOSMIDOMYCIN

49
Q

NEW DRUG APPROACHES

FOSMIDOMYCIN:
MOA

A

inhibition of NON-MEVALONATE PATHWAY & GLUTATHIONE REDUCTASE