Antiamoebitic drugs

Question 1

Antiamoebitic drugs split into types

Answer 1

INT, - intestinal
INT and Ext INT,
Ext INT - extraintestinal

Question 2

INT and Ext INT Drugs

Answer 2

Nitroimidazoles

Emitins and Dehydroemetins (DHEs)

Question 3

Nitroimidazoles

Answer 3

Metronidazole - effective against anaerobic bacteria, E histolytica, T. vaginalis, G. lamblia
Omidazole
Imidazole
Sahamidazole

Question 4

Nitroimidazoles - MoA

Answer 4

-> Converted by protozoal enzyme reducing nitrogen gorup of nitroimidazole and convert to active mtabolite which is cytotoxic to protozoa and damages DNA

Question 5

Method of dose - Nitroimidazoles

Answer 5

Orally, IV

Question 6

Side Effects - Metronidazoles

Answer 6

• mild GI issues
• Allergic rxns
• CNS toxicity
• Disuliform effect
• Metallic taste

Question 7

Advantage - Omidazoles and Imidzoles

Answer 7

–Both longer acting and better tolerated

Question 8

Advantage - Sahamidazole

Answer 8

–No disulfide effect

Question 9

Emetins - type

Answer 9

Emitins - Alkaloid - natural source

Question 10

Emetins - MoA

Answer 10

Kill trophozoite

Question 11

DHEs type

Answer 11

Semi synthetic

Question 12

DHEs MoA

Answer 12

Kill trophozoite

Question 13

Emetins and DHEs side effects

Answer 13

EMETINE
E - emesis
M - muscle weakness
E - ECG changes
T - tachycardia
I - itching
N - nausea 
E - eczema lesions

Question 14

Only INT drugs

Answer 14

Amides, Antibiotics

Question 15

Amides

Answer 15

Diloxinide furoate, Nitazoanide, Iodoquinol

Question 16

Diloxinide furoate MoA

Answer 16

–kill troph in lumen by splitting into diloxinite and furoate, furoate has the antiamoebic property.

Drug of choice (DOC) for carriers

Mixed with tissue amoebicidal to completely eradicate infection

Question 17

Side effects of Diloxinide furoate

Answer 17

• Flatulence
• Nausea
• Rash

Question 18

Nitazoanide (tizoxanide)

Answer 18

-Used in amoebiasis and giardiasis

Question 19

Iodoquinol is very toxic (T/F)

Answer 19

True

Question 20

Side effects of Iodoquinol

Answer 20

-Thyroid enlargement, neurotoxicity

Not used

Question 21

Antibiotics - Antiamoebic

Answer 21

Tetracyclines, Parromycin

Question 22

Tetracyclines MoA

Answer 22

Reach colon and destroy flora fed on by E histolyitica

Not safe for pregnancy

Question 23

Parromycin not safe for pregnancy (T/F)

Answer 23

False, it is given as alternative to Tetracycline which isn’t safe for pregnancy.

Question 24

Ext INT

Answer 24

ChloroAquine,

Millefosine, Na stibogluconate, Pentamidine, Suramin, Melarosoprol, Pyrimethin

Question 25

ChloroAquine MoA

Answer 25

(hepatic amoebiasis)

• Good gut absorption
• Absorbed in upper GIT -> gets concentrated in liver where it acts

Question 26

Millefosine - used in?

Answer 26

–Visceral leishmaniasis

Question 27

Na stibogluconate - used in?

Answer 27

• -Cutaneous leishmaniasis

- -Mucocutaneous leishmaniasis

Question 28

Pentamidine - used in?

Answer 28

• -Leishmania

- -P.jiroveci

Question 29

Suramin - used in?

Answer 29

• -DOC for African sleeping sickness (before CNS involvement)
• -Neurological complications

Question 30

Melarosoprol - used in? MoA? administration? Side effect?

Answer 30

• -Penetrates CNS
• -Af. sleeping sickness
• -IV
• -Side effect: fatal encephalopathy

Question 31

Pyrimethrin - used in?

Answer 31

-Toxoplasmosis