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PHA 324 > Antihelminthic Drugs > Flashcards

Antihelminthic Drugs Flashcards

1
Q

The helminth life cycle is strongly dependent on the following factors:

A
  1. Neuromuscular coordination for worm feeding movements and for maintaining a
    favourable location within the host.
  2. Carbohydrate metabolism as the source of energy, with glucose as the primary
    substrate.
  3. Microtubular integrity – egg laying and hatching, larval development, glucose
    transport, and enzyme activity and secretion are hindered when microtubules are
    modified.
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2
Q

BENZIMIDAZOLES include

A

mebendazole, thiabendazole and albendazole.

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3
Q

Mebendazole is extensively absorbed when administered orally. True or false?

A

False. Little of an oral dose (10%) is
absorbed by the body, therefore it is relatively free of toxic effects.

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4
Q

Albendazole given orally is rapidly absorbed. True or false?

A

True

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5
Q

BENZIMIDAZOLES are teratogenic. True or false?

A

True

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6
Q

Pyrantel pamoate MOA

A
  • Acts as a depolarizing neuromuscular blocking agent.
  • Causes spastic paralysis.
  • Paralyzed worm is expelled from the host’s intestinal tract.
  • It has some anticholinesterase activity
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7
Q

Pyrantel pamoate indication

A

Used along with mebendazole, it is effective in treatment of infections caused by
roundworms, pinworms and hookworms.

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8
Q

Ivermectin is a drug derived from

A

avermectins, a group of natural substances
derived from actinomycete

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9
Q

Ivermectin is contraindicated in

A

Patients with meningitis (compromised BBB) and in pregnancy.

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10
Q

Praziquantel MOA

A

Increases permeability of helminth cell to calcium → contraction of musculature →
paralysis and death of worm.

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11
Q

Praziquantel distributes into the CSF. True or false?

A

True

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12
Q

Drug of first choice for all spp. of Schistosomes and is effective in cysticercosis.

A

Praziquantel

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13
Q

Drug of choice for most cestode (tapeworm) infections

A

Niclosamide

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14
Q

Niclosamide MOA

A
  • Inhibition of parasites mitochondrial anaerobic phosphorylation of ADP which
    produces usable energy in the form of ATP.
  • Also blocks glucose uptake by intestinal tapeworms.
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15
Q

How is Niclosamide administered by for T. Solium

A

Given in a single dose after a light meal, followed by a purgative 2
hours later (to prevent cysticercosis).

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16
Q

Piperazine MOA

A

Reversibly inhibits neuromuscular transmission in the worm, acting possibly like
GABA on GABA-gated chloride channels → worms paralyzed and expelled alive.

17
Q

Piperazine indications

A

Treatment of infections with common roundworm (Ascaris vermicularis) and
threadworm/pinworm (Enterobius vermicularis).

18
Q

DEC is a derivative of

A

Piperazine derivative

19
Q

Levamisole MOA

A

Nicotinic-like action (stimulate and then block NMJ) → paralysed worm expelled
with faeces by normal peristalsis.

20
Q

Levamisole indication

A

Treatment of infection with common roundworm (Ascaris lumbricoides)

21
Q

Oxamniquine MOA

A

Inhibits DNA, RNA and protein synthesis. Parasite may have a unique enzyme capable of esterifying oxamniquine to form a
reactive metabolite which alkylates helminth DNA.

22
Q

Oxamniquine indications

A

• Active against S. mansoni (mature and immature forms).

23
Q

Metriphonate MOA

A

Paralytic action related to inhibition of parasite cholinesterase.

24
Q

Metriphonate is a pro drug. True or false?

A

True

25
Q

Metriphonate indications

A

Effective against S. haematobium but not S. mansoni (possibly due to difference in drug
accessibility (S. mansoni resides in mesenteric veins whereas S. haematobium live within
veins surrounding the bladder).

26
Q

Suramin MOA

A

Inhibits numerous enzymes of filarial helminthes (most notably lactate
dehydrogenase, malate dehydrogenase, dihydrofolate reductase and various protein
kinases). It is a large polyanion that complexes proteins readily.

27
Q

Only antihelmithic to be given parenterally (IV) is…

A

Suramin

28
Q

Drug of choice against Onchocerca volvulus is

A

Suramin

29
Q

Metronidazole MOA

A

Inhibits nucleic acid synthesis by disrupting DNA of microbial cells.

PHA 324 (9 decks)

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