Flashcards in topic 15 Deck (21):
What are 2 classes of nematodes? What nematodes are included in each?
In GI tract
Ascaris lumbricoides (roundworm)
Trichuris trichiura (whipworm)
Enterobius vermicularis (pinworm)
Strongyloides stercoralis (threadworm)
Ancylostoma duodenale and Necator americanus
20% of population
Cause systemic infection
Trichinella spiralis (trichinosis)-parasite in GI tract and skeletal muscle.
transmitted through bite of insect vectors
Wuchereria bancrofti (elephantiasis)- parasite in lymph glands
Onchocerca volvulus (river blindness)-parasite located in lymph glands and eye.
What 3 drugs are used to treat GI infections caused by nematodes?
Mebendazole, albendazole, pyrantel pomoate
What is the mech of action of mebendazole and albendazole?
It inhibits uptake of glucose and uncouples oxidative phosphorylation
In addition, it binds b-tubulin and blocks microtubule polymerization.
The result of the drug effect on the parasite is to cause immobilization, death and expulsion from the G.I. tract
What is the absor, admin, of mebendazole?
Mebendazole is poorly absorbed (10-15%) and unabsorbed drug excreted in stool.
What is the absorp, admin, distr of albendazole?
Absorption is good when taken with fatty meal.
CNS levels reach 50% of serum levels.
What is the spectrum of albendazole?
Specificity: Broad spectrum
T. trichiura, A. duodenale, N. americanus, A. lumbricoides, E. vermicularis infections
Drug of choice for treatment of cysticercosis due
What is the absotp, admin, and mech of action of pyrantel pomoate?
This drug is taken orally and poorly absorbed from the GI tract.
Mechanism of Action
It is a depolarizing neuromuscular blocking agent.
It acts as an agonist causing persistent activation of nicotinic acetylcholine receptors.
This results in worm paralysis and removal by gut peristalsis.
What are the side effects of pyrantel pomoate?
If taken in exceptionally large amounts (greater than 1g), enough drug can be absorbed to cause neuromuscular blockade in host.
What is the spectrum of pyrantel pomoate?
It is effective in treating infection by A. lumbricoides. N. americanus and A. duodenale.
It is the drug of choice for treating
E. vermicularis infections.
Which drugs are used to treat systemic infections caused by nematodes (wuchereria bancrofti)
What is the absorp, admin, mech of action of diethylcarbamazine?
The drug is given orally and is readily absorbed from the G.I. tract.
Mechanism of Action
** mechanism unknown but may be hyperpolarization of muscle
The drug appears to sensitize filarial worms to phagocytosis by macrophages.
What are the side effects of diethylcarbamazine?
More serious is a severe inflammatory reaction to released proteins of the phagocytized filarieae called Mazzotti reaction
What is the spectrum of diethylcarbamazine?
Active against filarial infections
Wuchereria bancrofti (given with albendazole)
No longer used for Onchocerca volvulus b/c it caused eye damage.
What is the admin, absorp, and mech of action of ivermectin?
Well absorbed, administer on an empty stomach.
Mechanism of Action
Activates GABA and glutamate-gated chloride channels only in invertebrates causing tonic paralysis of muscles.
What are the side effects of ivermectin?
Side effects and Precautions
Main side effect is Mazzotti reaction with hypotension, fever, pruritis, bone and joint pain (mild in 10-15% in first time users but can be severe in 5%).
At higher doses or in patients with a damaged brain barrier CNS toxicity can occur as indicated by tremors, ataxia and lethargy.
What is the spectrum of ivermectin?
Effective against W. bancrofti (given with albendazole), O. volvulus and S. stercoralis.
What are the different kinds of cestodes (tapeworms) and where are they found in the body? What drug is used to treat them?
Taenia solium (pork tapeworm)-found in GI tract and larvae in tissues (cysticercosis)
Diphyllobothrium latum (fish tape worm)
Taenia saginata (beef tapeworm)
Hymenolepis nana (dwarf tapeworm)
What is the admin, absorp, metab, and mech of action of praziquantel?
80% of oral dose is absorbed and is metabolized by liver p450 enzymes.
Patients with depressed liver function may require adjustment of dosage.
It increases parasite membrane permeability to cations (Ca2+) causing severe muscular contraction.
Praziquantel does not kill cestodes in vivo, but causes the worms to be dislodged from their usual sites of residence in the intestine.
What are the side effects of praziquantel?
Both Albendazole and Praziquantel
are contraindicated in patients with ocular cysticercosis (T. solium infection) due to host response that can damage eye.
What is the spectrum of praziquantel?
Broad spectrum drug which is effective against all types of tape worms: Taenia solium, Diphyllobothrium latum, Taenia saginata and Hymenolepis nana in the GI tract.
Alternative to treat T. Solium cysticercosis when used at high doses. Albendazole is preferred treatment for cysticercosis