FINALS- ANTIMALARIALS

Question 1

caused by a Plasmodium parasite and is transmitted to humans by the Anopheles Mosquito

Answer 1

Malaria

Question 2

Malaria is caused by this parasite

Answer 2

Plasmodium spp.

Question 3

Malaria is transmitted to humans by

Answer 3

Anopheles Mosquito

Question 4

• causes the most severe form of the disease
• infects up to 65% of the patients erythrocytes

Answer 4

Plasmodium falciparum

Question 5

• second most common species
• can be very chronic in recurrence because it can reinfect liver cells

Answer 5

Plasmodium vivax

Question 7

• second most common species
• can be very chronic in recurrence because it can
reinfect liver cells

Answer 7

Plasmodium vivax

Question 8

• although causing only 10% of all malarial cases,
relapses are very common

Answer 8

Plasmodium malariae

Question 9

• the least common species

Answer 9

Plasmodium ovale

Question 10

• derived from “mala aria” or ______

Answer 10

Bad Area

Question 11

• also called ague, intermittent fever, marsh fever and The Fever

Answer 11

Malaria

Question 12

• a nocturnal feeder
• should prevent contact between humans and the insect
• can be eliminated by using insecticides

Answer 12

Anopheles Mosquito

Question 13

Insecticide used to eliminate Anopheles Mosquito

Answer 13

Dichlorodiphenyltrichloroethane (DDT)

Question 14

Diseases spread: Malaria
Which mosquitoes bite?: Pregnant females
When do they bite: Night
Resting position: With abdomen sticking upwards
Location: Predominantly rural
Breeding ground: Bodies of water

Answer 14

Anopheles Mosquito

Question 15

Diseases spread: Dengue, Yellow Fever, Chikungunya, Lymphatic Filariasis
Which mosquitoes bite?: Pregnant females
When do they bite: Day
Resting position: Lies
Location: Predominantly urban
Breeding ground: Shallow water surfaces

Answer 15

Aedes Mosquito

Question 16

Human Mutations that Protect Against Malaria

Answer 16

• Sickling disease (sickle cell anemia)
• G6PD patients
• Hemoglobin C
• Thalassemia
• Increased production of NO
• Pyruvate kinase deficiency

Question 17

• Kill the sporozoites injected by the mosquito and/or prevent the sporozoites from entering the liver
• Kill the schizonts residing in hepatocytes and/or prevent them from becoming merozoites
• Kill the merozoites in the blood and/or prevent them from developing into gametocytes
• Kill the gametocytes before they can enter the mosquito and reproduce into zygotes

Answer 17

Drugs used to Prevent & Treat Malaria

Question 18

• have one common structural feature - a quinoline ring, or a “quinoline with an additional benzene” (an acridine ring)

Answer 18

SAR

Question 19

• derived from Cinchona tree (Cinchona succirubra & Cinchona calisaya)
• has quinuclidine ring

Answer 19

Cinchona Alkaloids

Question 20

• reserved for malarial strains resistant to other agents
• used for Chloroquine-resistant P. falciparum
• used in nocturnal leg cramps
• Category X (abortifacient)

Answer 20

Quinine

Question 21

It inhibits nucleic acid synthesis, protein synthesis, and glycolysis in Plasmodium falciparum and can bind with hemazoin in parasitized erythrocytes.

Answer 21

MOA of Quinine

Question 22

• not indicated for malaria, but a more potent agent than quinine
• more toxic
• used for cardiac arrythmias

Answer 22

Quinidine

Question 23

• a syndrome causing nausea and vomiting, tinnitus and vertigo
• can proceed to involvement of GI tract, nervous and cardiovascular system, and the skin

Answer 23

Cinchonism

Question 24

• closest antimalarials that are bases on quinine structure
• substituted at the same position 4 as quinine and have assymetric carbon equivalent to quinine’s C9
position

Answer 24

7-Chloro-4-Aminoquinolines

Question 25

• DOC in the treatment of erythrocytic falciparum malaria • used for both prophylaxis and treatmant of P. ovale, P. vivax and P. malariae infections • MOA: unknown • not effective against exoerythrocytic parasites • does not prevent relapses of P. vivax and P. ovale • also indicated for the treatment of extraintestinal amebiasis • anti-inflammatory action explains its occasional use in RA and discoid lupus erythematosus • S/E: Retinopathy, hemolysis in patients with G6PD deficiency, muscular weakness, exacerbation of psoriasis and impaired liver function

Answer 25

Chloroquine

Question 26

• remains in the body for over a month • prophylactic dosing is once weekly

Answer 26

Hydroxychloroquine

Question 27

• highly suppressive in P. vivax and P. falciparum • has curative activity against P. falciparum • S/E: hepatitis, agranulocytosis

Answer 27

Amodiaquine

Question 28

• effective single agent for suppressing and curing multi-drug resistant forms of P. falciparum • CI: patients with active depression, a recent history of depression, generalized anxiety disorder, psychosis, schizophrenia and other major psychiatric disorders

Answer 28

Mefloquine

Question 29

• all can cause hemolytic anemia in G6PD deficient patients

Answer 29

8-Aminoquinolines

Question 30

• effective only against the exoerythrocytic stages of malaria • only agent that can lead to radical cures of P. vivax and P. ovale malarias (dormant stages in the liver) • gametocidal for all four plasmodia species, transmission of the disease can be prevented • not used as prophylaxis • MOA: disrupt the parasites mitochondria

Answer 30

Primaquine

Answer 32

9-Aminoacridines

Question 33

• primarily used in the treatment of Giardiasis but is also effective against tapeworm and malaria, and topically against leishmaniasis • should not be given with primaquine because of increased toxicity

Answer 33

Quinacrine

Question 34

• MOA: inhibits the pathogen's protein synthesis by reversibly inhibiting the 30S ribosomal subunit • Use for malaria is limited to prophylaxis against strains of P. falciparum resistant to chloroquine and sulfadoxine-pyrimethamine

Answer 34

Doxycycline

Question 35

• is a schizonticide • MOA: unknown

Answer 35

Halofantrine

Question 36

• a natural product from the dry leaves of Artemisia annua (sweet wormwood)

Answer 36

Artemisinin

Question 37

• schizonticide • Sulfadoxine - interferes with the parasites ability to synthesize folic acid • Pyrimethamine - inhibits the reduction of folic acid to its active tetrahydrofolate coenzyme form • indicated for the prophylaxis and treatment of chloroquine-resistant P. falciparum • active against all the asexual erythrocytic forms

Answer 37

Sulfadoxine & Pyrimethamine

Question 38

• Proguanil - metabolized to cycloguanil • combination is against both erythrocytic and exoerythrocytic Plasmodium • indicated for malaria resistant to chloroquine, halofantrine, mefloquine and amodiaquine

Answer 38

Atovaquone & Proguanil

Question 39

• these two interfere with heme metabolism, thereby stopping development of the parasite in the erythrocyte states

Answer 39

Artemether + Lumefantrine