Parasitic Infections Flashcards
Major targets for chemotherapy for parasitic infections:
- Unique essential molecule found only in the parasite
- Similar molecules found in both the host and parasite but indispensable for the parasite only
- Common biochemical functions found in both parasite and host but with different pharmacological properties
Categories of parasites found in humans:
- Macroscopic (ringworm, tapeworm, head louse)
- Microscopic (trichomonas, malaria, beaver fever)
Two examples of taenia species which can affect humans:
- Taenia saginata (beef tapeworm) and taenia solium (pork tapeworm)
How do pigs and cows get infected with tapeworm?
- Parasite eggs get released into environment
- Get infected when ingesting vegetation that has been contaminated
- Oncospheres hatch and penetrate the intestinal wall of the intermediate host
Where does the parasite attach within the host/intermediate host?
- Scolex (worm’s head) attaches to the intestine, matures, produces more eggs
What does praziquantel treat?
Targets and treats parasitic worms
What is praziquantel?
A synthetic isoquinoline derivative
Praziquantel bioavailability after oral dosing?
80%
MOA of praziquantel:
Exact unknown, but it binds to the integument of the parasite and produces focal vacuolization
Drug of choice against cestode infections:
- Praziquantel
Pros of praziquantel:
- Safe and effective
- Single oral dose
- Impairs the function of hooks and suckers at the anterior end of the worm
When is the bioavailability of praziquantel diminished?
When taken concurrently with corticosteroids
Adverse reactions of praziquantel:
Nausea, headaches, abdominal discomfort
What is niclosamide?
Salicylanilide derivative used to treat parasitic worms
MOA of niclosamide:
Rapidly killing scolex and producing segments of adult tapeworms
- Inhibition of mitochondrial anaerobic phosphorylation of ADP results in a decrease in ATP production
What is the second line choice of treatment for parasitic worms?
Niclosamide
Administration of niclosamide:
Single oral dose tablet, chewed thoroughly and swallowed with water
Adverse effects of niclosamide:
GI complaints
- Avoid alcohol for 24 hours
Common name of enterobius vermicularis:
Pinworm
Life cycle of pinworms:
- Eggs on perinanal folds that contain larvae which mature in 4-6 hours
How does a human get infected with pinworms?
- Ingesting embryonated eggs which hatch in the small intestine, adults form in the lumen of the cecum
- Eggs can also contaminate nightclothes and bedding
Drugs of choice for pinworm:
Mebendazole and pyrantel
What is mebendazole?
Broad spectrum drugs effective against parasites
How do you administer mebendazole?
Administered orally
- Less than 10% absorbed
- Absorption can be increased if ingested with a fatty meal
- Twice over a two week interval
MOA of mebendazole:
- Binds to B-tubulin and inhibits polymerisation to microtubules
- This inhibits parasite motility, glucose uptake and cell division
- Once parasite is killed, it is expelled in feces
Do not administer mebendazole if…
Pregnant
Pyrantel class:
Tetrahydropyrimidines
MOA of pyrantel:
- Poorly absorbed within the gut
- Acts selectively at neuromuscular junctions of parasites on nicotinic acetylcholine receptors
- This causes the release of ACh and inhibition of acetylcholinesterase
- Results in paralysis of worms
Differences between pyrantel and mebendazole
Pyrantel has a narrower spectrum of activity than mebendazole
Adverse effects of pyrantel:
Mild, nausea, vomiting, diarrhea
Common name of pediculus capitis:
Head lice
How do head lice grow and mature?
Feeding on human blood
Treatment for head lice:
Permethrin, Malathion
Class of permethrin:
Phyrethroids
MOA of permethrin:
Causes voltage-gated sodium channels to remain open which causes membrane depolarization and rapid paralysis in the parasite
- Absorbed through the skin
Class of malathion
organophosphate