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Derm Pharm 2020 > 2 - Systemic Antiparasitic Agents > Flashcards

2 - Systemic Antiparasitic Agents Flashcards

1
Q

Ivermectin is a semisynthetic antihelminthic derived from fermentation products of Streptomyces avermitilis

A

True

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2
Q

Ivermectin has structural similarity to that of macrolide antibacterial agents (erythromycin, clarithromycin, azithromycin)

A

True

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3
Q

Although topical permethrin appears to be the most effective treatment for scabies, ivermectin appears to be an effective oral agent

A

True (data considering both cost and efficacy suggests that benzyl benzoate and ivermectin are most cost-effective for the treatment of scabies)

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4
Q

In patients with crusted scabies, the response to oral ivermectin is variable and oral therapy in combination with topical scabicides and keratolytics are advocated

A

True (ivermectin alone often fails in crusted scabies)

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5
Q

Ivermectin appears comparable or slightly inferior to permethrin in efficacy against non-crusted scabies, but has the convenience of oral dosing

A

True (ivermectin alone fails in crusted scabies)

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6
Q

Ivermectin is primarily metabolised by CYP3A4 in the liver and excreted in the faeces

A

True (ivermectin is a substrate of CYP3A4)

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7
Q

As <1% of the administered ivermectin dose is excreted in the urine (mainly faecal excretion), dose adjustment is needed with biliary obstruction but renal failure is not likely to affect metabolism

A

True (metabolised by the liver and excreted in the faeces)

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8
Q

Bioavailability of ivermectin is increased when the drug is administered with a high-fat meal

A

True

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9
Q

Ivermectin selectively binds to glutamate-gated chloride ion channels found in invertebrate (parasites) nerve and muscle cells, resulting in increased permeability of cell membranes to chloride ions and hyperpolarisation of the nerve/muscle cell causing death of the parasite

A

True

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10
Q

Ivermectin is FDA approved in the treatment of intestinal strongyloides specifically caused by Strongyloides stercoralis, and onchocerciasis (river blindness) caused by Onchocerca volvulus

A

True (scabies is not FDA approved)

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11
Q

Ivermectin is most widely used in dermatology (off label) for the treatment of scabies

A

True (200 ug/kg as a single dose, then repeated in 7-10 days) - addition of topical keratolytics and topical permethrin in crusted scabies

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12
Q

Ivermectin is used in dermatology (off label) to some extent for the treatment of pediculosis (lice)

A

True (400 ug/kg as a single dose on Day 1 and Day 8)

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13
Q

Ivermectin is used in dermatology (off label) to some extent for the treatment of cutaneous larva migrans

A

True

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14
Q

A single dose of Ivermectin has also been used empirically (off label) to reduce the pruritus in homeless populations

A

True

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15
Q

Ivermectin has been used in the control of hospital and institutional outbreaks of scabies, and may be superior to topical treatment in the setting of mass infestation

A

True

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16
Q

Ivermectin is commonly associated with Mazzoti-type reactions (oedema, urticarial rash, systemic symptoms and ophthalmological reactions) when used in the treatment of helminthic infestations

A

True (less common in the setting of scabies)
NB. Mazzoti reactions may be due to allergic and inflammatory responses to the death of microfilariae or to microorganisms within the worms

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17
Q

Ivermectin is commonly associated with pruritus in the setting on helminthic infestation

A

True (less common in the setting of scabies)

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18
Q

Ivermectin is commonly associated with fever in the setting of helminthic infestation

A

True (less common in the setting of scabies)

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19
Q

Ivermectin is commonly associated with lymphadenopathy or lymph node tenderness in the setting of helminthic infestation

A

True (less common in the setting of scabies)

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20
Q

Tachycardia is an infrequent adverse reaction to Ivermectin

A

True

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21
Q

The Mazzoti reactions commonly associated with ivermectin in patients with onchocerciasis may be due to allergic and inflammatory responses to the death of microfilariae or to microorganisms within the worms

A

True (doxycycline can eliminate endosymbiotic bacteria within filarial worms, and reducing the incidence of Mazzoti reactions)

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22
Q

Doxycycline can eliminate endosymbiotic bacteria within filarial worms, and reducing the incidence of Mazzoti reactions in patients with onchocerciasis associated with ivermectin treatment

A

True

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23
Q

Facial oedema is an infrequent adverse reaction to Ivermectin

A

True

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24
Q

Orthostatic hypotension is an infrequent adverse reaction to Ivermectin

A

True

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25
Q

Diarrhoea is an infrequent adverse reaction to Ivermectin

A

True

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26
Q

Nausea is an infrequent adverse reaction to Ivermectin

A

True

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27
Q

CNS symptoms is a rare adverse reaction to Ivermectin

A

True

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28
Q

SJS is a rare adverse reaction to Ivermectin

A

True

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29
Q

Abnormal LFTs is a rare adverse reaction to Ivermectin

30
Q

Ivermectin may enhance the anticoagulant effect of warfarin

31
Q

Australia has shown increasing increasing resistance to both topical permethrin and oral ivermectin in the treatment of scabies due to increased drug metabolism and efflux mechanisms

32
Q

Ivermectin is classified as pregnancy category C and teratogenic effects have been observed in animal studies

33
Q

Ivermectin is not recommended during lactation

A

True (enters breast milk, and safety and efficacy for use in children <15kg have not been established)

34
Q

Ivermectin is not recommended for children under 15kg

35
Q

Mass infestations of scabies are the best setting for the use of ivermectin

36
Q

Albendazole has both antihelminthic and antiprotozoal activity

37
Q

Albendazole has low aqueous solubility and so is poorly absorbed from the GI tract

A

True (oral bioavailability is enhanced when Albendazole is taken with a fatty meal)

38
Q

The systemic antihelminthic activity of Albendazole is attributed to its primary metabolite Albendazole sulfoxide

A

True (Albendazole is rapidly converted to the sulfoxide metabolite before reaching the systemic circulation, such that the plasma levels of Albendazole as the parent drug is negligible in plasma)

39
Q

Biliary elimination is the major route of excretion for Albendazole and its metabolite Albendazole sulfoxide, with <1% excreted in the urine

A

True (biliary obstruction will affect blood levels, but renal failure is unlikely to affect levels)

40
Q

Albendazole sulfoxide (major metabolite of Albendazole) is mainly bound to plasma protein and achieves excellent distribution throughout the body

41
Q

Albendazole inhibits tubulin polymerisation, which causes immobilisation and death of the susceptible organisms

42
Q

Albendazole is FDA approved for the treatment of neurocystocercosis and hydatid disease (tapeworms)

43
Q

Ivermectin is significantly more effective than Albendazole for pediculosis

44
Q

Albendazole has not been adequately studied in children under 1 year of age

45
Q

Albendazole may cause bone marrow suppression with aplastic anaemia and agranulocytosis

46
Q

Bone toxicity may occur in patients on Albendazole with and without underlying hepatic dysfunction and FBC should be monitored

A

True (biliary obstruction affects blood levels as the drug is mainly excreted in the bile)

47
Q

Patients with liver disease on Albendazole appear to be at an increased risk for bone marrow suppression

A

True (biliary obstruction affects blood levels as the drug is mainly excreted in the bile)

48
Q

Other adverse effects of Albendazole include hepatotoxicity

49
Q

Other adverse effects of Albendazole include GI discomfort

50
Q

Other adverse effects of Albendazole include diarrhoea

51
Q

Other adverse effects of Albendazole include headache

52
Q

Other adverse effects of Albendazole include dizziness

53
Q

Hypersensitivity reactions presenting with rash, pruritus or urticaria is rarely associated with Albendazole

54
Q

Albendazole is a CYP1A2 inhibitor

A

True (may inhibit theophylline metabolism as theophylline is a CYP1A2 substrate)

55
Q

Albendazole is classified as pregnancy category C as it is both teratogenic and embryotoxic in animal studies

A

True (pregnancy test should be obtained before starting therapy)

56
Q

Thiabendazole is a broad spectrum antihelminthic that has been used for the treatment of parasitic infestations in humans and animals

57
Q

Thiabendazole is metabolised almost entirely by the liver and the metabolites are substantially excreted by the kidneys

A

True (therefore the drug should be used with caution and the dose may need to be adjusted in patients with impaired hepatic or renal function)

58
Q

Thiabendazole is rapidly absorbed and metabolised almost completely to its 5-hydroxy form in the liver

59
Q

The mechanism of action of thiabendazole is unknown but it may inhibit the helminth-specific fumarate reductase

60
Q

Thiabendazole is indicated for the treatment of strongyloidiasis

61
Q

Thiabendazole is indicated for the treatment of cutaneous larva migrans

62
Q

Thiabendazole is indicated for the treatment of visceral larva migrans

63
Q

Thiabendazole has been used for the treatment of intestinal roundworms infestation

64
Q

Thiabendazole has been associated with hepatotoxicity

65
Q

Thiabendazole has been associated with anorexia and abdominal symptoms such as nausea, vomiting, diarrhoea, and abdominal pain

66
Q

Thiabendazole has been associated with CNS symptoms such as convulsions, confusion, tinnitus and depression

67
Q

Thiabendazole has been associated with SJS

68
Q

Thiabendazole is a CYP1A2 inhibitor

A

True (may increase theophylline and caffeine levels as these 2 are CYP1A2 substrates)

69
Q

Thiabendazole is classified as pregnancy category C as birth defects have been observed in animal studies

70
Q

Ivermectin may rarely cause potentially fatal encephalopathy in patients co-infected with loiasis

Derm Pharm 2020 (47 decks)

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