ANTIMALARIAL

Question 1

VECTOR of MALARIA

Answer 1

Anopheles mosquito

FEMALE ONLY

Question 2

CAUSATIVE AGENT of MALARIA

Answer 2

Plasmodium ovale
Plasmodium malariae
Plasmodium falciparum
Plasmodium vivax
Plasmodium knowlesi

Question 3

causative agent of malaria that is considered ZOONOTIC

ZOONITC - animal to animal transmission only

Answer 3

Plasmodium knowlesi

Question 4

2 major stages for malarial cycle

Answer 4

1. exoerythrocytic
2. erythrocytic

Question 5

MOST PATHOGENIC causative agent of MALARIA

Answer 5

P. falciparum

Question 6

DIFFERENT DRUGS FOR MALARIA

Answer 6

• 4-aminoquinolines
• 8-aminoquinolines
• natural anti-malarial

Question 7

MALARIA

Plasmodium is a parasite coined from ____ which means BAD AIR

Answer 7

mala aria

Question 8

other names for MALARIA

Answer 8

Ague
Intermittent fever
Marsh fever
The Fever

Question 9

MALARIA

causative agent that is MILDER; RARELY FATAL

Answer 9

P. malariae

Question 11

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

Answer 11

DR. RONALD ROSS

Question 12

MALARIA

3 potential ways to control malaria

Answer 12

• Vector control
• Drug therapy
• Vaccination

Question 13

MALARIA | CAUSATIVE AGENTS

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

Answer 13

P. falciparum

Question 14

MALARIA | CAUSATIVE AGENTS

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

Answer 14

P. vivax

Question 15

MALARIA | CAUSATIVE AGENTS

• 10%
• RELAPSES are common

Answer 15

P. malariae

Question 16

MALARIA | CAUSATIVE AGENTS

• LEAST common

Answer 16

P. ovale

Question 17

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

Answer 17

QUININE SULFATE

Question 18

CINCHONA ALKALOIDS

QUININE SULFATE:
side effects

Answer 18

abortifacient

Question 19

CINCHONA ALKALOIDS

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

Answer 19

QUINIDINE

Question 20

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

Answer 20

CINCHONISM

Question 21

what is the proposed MOA of quinine and related compounds?

Answer 21

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

Question 22

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

Answer 22

CHLOROQUINE

Question 23

4-AMINOQUINOLINES

CHLOROQUINE:
parenteral

Answer 23

HCl

Question 24

4-AMINOQUINOLINES

CHLOROQUINE:
oral

Answer 24

PO₄
phosphate

Question 25

# **4-AMINOQUINOLINES** * **HIGH PROTEIN BOUND** (remains in the body for **OVER A MONTH**)

Answer 25

Hydroxychloroquine

Question 26

# **4-AMINOQUINOLINES** * **PROPHYLAXIS** for malaria * associated with **higher incidence** of **HEPATITIS** and **AGRANULOCYTOSIS**

Answer 26

Amodiaquine

Question 27

# **4-AMINOQUINOLINES** * **SCHIZONTICIDE** (newest member) * exacerbate **mental disorders** * DOC for **MALARIAL SUPPRESSION**

Answer 27

Mefloquine

Question 28

# **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***

Answer 28

PRIMAQUINE

Question 29

# **8-AMINOQUINOLINES** PRIMAQUINE: **most effective** against parasites in the ____

Answer 29

LIVER

Question 30

# **8-AMINOQUINOLINES** PRIMAQUINE: **NOT** effective against parasites within ____

Answer 30

erythrocytes

Question 31

# **8-AMINOQUINOLINES** PRIMAQUINE **MOA**: disruption of ____

Answer 31

parasites' mitochondria

Question 32

# **8-AMINOQUINOLINES** PRIMAQUINE: **DOC**

Answer 32

acute attack of Plasmodium vivax

Question 33

# **POLYCYCLIC ANTIMALARIAL DRUGS** * a **TETRACYCLINE** that inhibits the pathogen's **PROTEIN SYNTHESIS** * **PROPHYLAXIS** for malaria * CI in **children** and in areas with **greatest sunlight**

Answer 33

DOXYCYCLINE

Question 34

# **POLYCYCLIC ANTIMALARIAL DRUGS** DOXYCYCLINE: **MOA**

Answer 34

inhibits pathogen's PROTEIN SYNTHESIS

Question 35

# **POLYCYCLIC ANTIMALARIAL DRUGS** DOXYCYCLINE: **contraindication**

Answer 35

in children & in areas with greatest sunlight

Question 36

# **POLYCYCLIC ANTIMALARIAL DRUGS** * can **ARREST TISSUE CONDUCTION** in **cardiac muscles**

Answer 36

Halofantrine

Question 37

# **POLYCYCLIC ANTIMALARIAL DRUGS** * proposed MOA: inhibition of **β-hematinin** by forming complex with **hemin**

Answer 37

Lumefantrine

Question 38

# **POLYCYCLIC ANTIMALARIAL DRUGS** * **MOST TOXIC** antimalarial drug * **ACRIDINE DYE** (can cause **YELLOW** color of **skin**, **tissues**, etc.) * tx of malaria and a **SCLEROSING AGENT**

Answer 38

QUINACRINE

Question 39

# **POLYCYCLIC ANTIMALARIAL DRUGS** QUINACRINE: can cause ____ color of **skin**, **tissues**, etc.

Answer 39

yellow

Question 40

# **POLYCYCLIC ANTIMALARIAL DRUGS** ARTEMISININ: * is a **METHYL ETHER** derivative of **dihydroartemesinin**

Answer 40

ARTEMETHER

Question 41

# **POLYCYCLIC ANTIMALARIAL DRUGS** ARTEMISININ: * is a **HEMISUCCINATE** derivative of the active metabolite **dihydroartemisin**

Answer 41

ARTESUNATE

Question 42

# **FIXED COMBINATION** * **PROPHYLAXIS** and treatment of **chloroquine resistant** malaria * MOA: inhibition of **FOLIC ACID** biosynthesis and **DIHYDROFOLATE REDUCTASE**

Answer 42

Sulfadoxine + Pyrimethamine

Question 43

# **FIXED COMBINATION** SULFADOXINE + PYRIMETHAMINE: **MOA**

Answer 43

inhibition of **FOLIC ACID** biosynthesis and **DIHYDROFOLATE REDUCTASE**

Question 44

# **FIXED COMBINATION** * effective against **ERYTHROCYTIC** and **EXOERYTHROCYTIC** plasmodium * used for **RESISTANT MALARIA** * MOA: inhibition of **dihydrofolate reductase** and **damage** to the parasite's **mitochondria**

Answer 44

ATOVAQUONE & PROGUANIL

Question 45

# **FIXED COMBINATION** ATOVAQUONE & PROGUANIL: **MOA**

Answer 45

inhibition of **dihydrofolate reductase** and **damage** to the parasite's **mitochondria**

Question 46

# **FIXED COMBINATION** **PROGUANIL** is a **prodrug** of ____

Answer 46

CYCLOGUANIL

Question 47

# **FIXED COMBINATION** * interfere **HEME metabolism** → interfere parasites in **ERYTHROCYTIC stage** * MOST ESTABLISHED MOA

Answer 47

Artemether & Lumefantrin

Question 48

# **NEW DRUG APPROACHES** * isolated from **Streptomyces fermentation broth** in **1980** * inhibition of **NON-MEVALONATE PATHWAY** & **GLUTATHIONE REDUCTASE** ## Footnote inhibition of glutathion - no antioxidant - increase free radicals - cell death

Answer 48

FOSMIDOMYCIN

Question 49

# **NEW DRUG APPROACHES** FOSMIDOMYCIN: **MOA**

Answer 49

inhibition of NON-MEVALONATE PATHWAY & GLUTATHIONE REDUCTASE