33 Anthelminthic drugs Flashcards

1
Q

33.01 ANTHELMINTHIC DRUGS

Mebendazole (similar: tiabendazole, albendazole) - actions

A

anthelminthic agent

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2
Q

33.01 ANTHELMINTHIC DRUGS

Mebendazole (similar: tiabendazole, albendazole) - MOA

A

inhibits microtubule synthesis, impairing microtubule functions such as glucose uptake

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3
Q

33.01 ANTHELMINTHIC DRUGS

Mebendazole (similar: tiabendazole, albendazole) - abs/distrib/elim

A

given orally
poor uptake is improved by fatty foods

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4
Q

33.01 ANTHELMINTHIC DRUGS

Mebendazole (similar: tiabendazole, albendazole) - clinical use

A

thread worm, round worm, whip worm and hookworm infections
albendazole also used for cutaneous larva migrans, cysticercosis, strongyloidiases

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5
Q

33.01 ANTHELMINTHIC DRUGS

Mebendazole (similar: tiabendazole, albendazole) - adverse effects

A

GIT disturbances, rash
rarely convulsions in infants

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6
Q

33.01 ANTHELMINTHIC DRUGS

Mebendazole (similar: tiabendazole, albendazole) - special points

A

mebendazole is considered unsuitable for pregnant women or children <2 years old

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7
Q

33.02 ANTHELMINTHIC DRUGS

Levamisole - actions

A

a narrow-spectrum anthelminthic agent

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8
Q

33.02 ANTHELMINTHIC DRUGS

Levamisole - MOA

A

causes tonic paralysis of the worm by stimulating nicotinic receptors at the neuromuscular junction
the paralysed worms (but not the ova) are expelled in the faeces

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9
Q

33.02 ANTHELMINTHIC DRUGS

Levamisole - abs/distrib/elim

A

given orally
plasma half-life 4h

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10
Q

33.02 ANTHELMINTHIC DRUGS

Levamisole - clinical use

A

common round worm infection

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11
Q

33.02 ANTHELMINTHIC DRUGS

Levamisole - adverse effects

A

mild GIT disturbances

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12
Q

33.02 ANTHELMINTHIC DRUGS

Levamisole - special points

A

drug has been withdrawn from North American market

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13
Q

33.03 ANTHELMINTHIC DRUGS

Piperazine - actions

A

a narrow-spectrum anthelminthic agent

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14
Q

33.03 ANTHELMINTHIC DRUGS

Piperazine - MOA

A

reverses neuromuscular transmission in the worm
the paralysed worms are expelled alive in the faeces

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15
Q

33.03 ANTHELMINTHIC DRUGS

Piperazine - abs/distrib/elim

A

given orally

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16
Q

33.03 ANTHELMINTHIC DRUGS

Piperazine - clinical use

A

common round worm infection

17
Q

33.03 ANTHELMINTHIC DRUGS

Piperazine - adverse effects

A

GIT disturbances
rash, bronchospasm
some patients experience CNS symptoms, e.g. dizziness, paraesthesias

18
Q

33.03 ANTHELMINTHIC DRUGS

Piperazine - special points

A

discontinued in United Kingdom
not suitable for pregnant women or for patients with impaired renal or hepatic function

19
Q

33.04 ANTHELMINTHIC DRUGS

Praziquantel - actions

A

a broad-spectrum anthelminthic agent

20
Q

33.04 ANTHELMINTHIC DRUGS

Praziquantel - MOA

A

increases the calcium permeability of the cell membranes, promoting calcium influx, resulting in prolonged contraction of muscle with eventual paralysis and death

21
Q

33.04 ANTHELMINTHIC DRUGS

Praziquantel - abs/distrib/elim

A

given orally, well absorbed, metabolised to inactive products
plasma half-life 60-90min

22
Q

33.04 ANTHELMINTHIC DRUGS

Praziquantel - clinical use

A

schistosomiasis, cysticercosis

23
Q

33.04 ANTHELMINTHIC DRUGS

Praziquantel - adverse effects

A

few and minor: sometimes GIT disturbances

24
Q

33.04 ANTHELMINTHIC DRUGS

Praziquantel - special points

A

considered safe for pregnant and lactating women

25
Q

33.05 ANTHELMINTHIC DRUGS

Ivermectin - actions

A

a broad-spectrum anthelminthic agent

26
Q

33.05 ANTHELMINTHIC DRUGS

Ivermectin - MOA

A

acts at the worm’s neuromuscular junction, causing paralysis either by intensifying GABA-mediated inhibition or by activating an invertebrate-specific glutamate-gated chloride channel

27
Q

33.05 ANTHELMINTHIC DRUGS

Ivermectin - abs/distrib/elim

A

given orally
half-life 11h

28
Q

33.05 ANTHELMINTHIC DRUGS

Ivermectin - clinical use

A

onchocerciasis (drug of choice)
strongyloidiasis
filarial infections
active against some roundworm, but not hookworms

29
Q

33.05 ANTHELMINTHIC DRUGS

Ivermectin - adverse effects

A

infrequent: itching, rash, GIT disturbances, dizziness, fatigue

30
Q

33.06 ANTHELMINTHIC DRUGS

Diethylcarbamazine - actions

A

anthelminthic drug - piperazine derivative

31
Q

33.06 ANTHELMINTHIC DRUGS

Diethylcarbamazine - MOA

A

removes microfilariae from the blood circulation and has limited effect on the adult worms in the lymphatics
may act by changing the parasite making it susceptible to the host’s normal immune responses or by interfering with helminth arachidonate metabolism

32
Q

33.06 ANTHELMINTHIC DRUGS

Diethylcarbamazine - abs/distrib/elim

A

oral administration
partly metabolised - parent drug and metabolites excreted in urine and cleared from body within 48h

33
Q

33.06 ANTHELMINTHIC DRUGS

Diethylcarbamazine - clinical use

A

filarial infections

34
Q

33.06 ANTHELMINTHIC DRUGS

Diethylcarbamazine - adverse effects

A

GI disturbances, joint pain, headache, general feeling of weakness
allergic effects referable to the products of the dying filariae are common and vary with species of worm

35
Q

33.07 ANTHELMINTHIC DRUGS

Niclosamide - actions

A

anthelminthic

36
Q

33.07 ANTHELMINTHIC DRUGS

Niclosamide - MOA

A

the scolex and a proximal segment of the worm are irreversibly damaged - worm separates from intestinal wall and is expelled
thought to result from uncoupling of phosphorylation or stimulation of ATPase activity

37
Q

33.07 ANTHELMINTHIC DRUGS

Niclosamide - abs/distrib/elim

A

given orally
minimal absorption from GI tract

38
Q

33.07 ANTHELMINTHIC DRUGS

Niclosamide - clinical use

A

tapeworm infections - used together with praziquantel

39
Q

33.07 ANTHELMINTHIC DRUGS

Niclosamide - adverse effects

A

nausea, vomiting, pruritus, light-headedness