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Pharmacology (Topic C) > C3. Antiprotozoal and antihelminthic drugs. > Flashcards

C3. Antiprotozoal and antihelminthic drugs. Flashcards

1
Q

List the drugs for P. Jiroveci infection(fungi).

A
  1. Cotrimoxazole (TMP-SMX)
  2. Pentamide + Sulfadiazine + folic acid
  3. Pentamide (?)
  4. Primaquine + Clindamycin
  5. Atovaquon
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2
Q

List the Antimalarials.

A
  1. Chloroquine
  2. Quinidine (+ doxycycline/clindamycin)
  3. Quinine
  4. Mefloquine (+/- artesunat)
  5. Primaquine
  6. Halofantrine
  7. Sulfadoxine + pyrimethamine
  8. Atovaquone
  9. Proquanil
  10. Artemisinin
  11. Malaron (proguanil + atovaquone)
  12. Lumefantrine (+arthemeter)
  13. Artesunat (+meflo/doxy/clinda)
  14. Artemotil
  15. Dihydroartemisinin
  16. Doxycycline (+-quinine /artesunat)
  17. Clindamycin (+ quinine /artesunat)
  18. Azithromycin
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3
Q

List the drugs used for Giardiasis:

A
  1. Metronidazole (Nitromidazole)
  2. Tinidazole
  3. Nitazoxanide
  4. Paromomycin
  5. Furazolidon
  6. Quinacrin
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4
Q

List the drugs for Toxoplasmosis?

A
  1. Pyrimethamine + Sulfadiazine
  2. Pyrimethamine + Clindamycin
  3. Spiramycin
  4. Cotrimoxazole (tmp/smx)
  5. (folinic acid)
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5
Q

List the drugs used in Trichomoniasis.

A
  1. Metronidazole (Nitroimidazole)
  2. Tinidazole
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6
Q

List the drugs used in Leishmaniasis.

A
  1. Amphotericin B
  2. Miltefosine
  3. Sodium Stibogluconate
  4. Meglumin
  5. Antimoniat
  6. Pentamidine (Pentavalent antimonials)
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7
Q

List the Amebiasis treatment.

A
  1. Iodoquinol
  2. Diloxanid furoat
  3. Paromomycin
  4. Metronidazole (+Tinidazole)
  5. Tinidazole
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8
Q

List the agents used in Trypanosomiasis.

A

African trypanosomiasis: (T. Brucei)

  1. Eflornithin
  2. Melarsoprol
  3. Pentamidine
  4. Suramin

American trypanosomiasis: (T. cruzi)

  1. Nifurtimox
  2. Benznidazole
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9
Q

List the Antihelminthic agents.

A

Benzimidazoles:

  1. Albendazole
  2. Mebendazole
  3. Triclabendazole (Levamisole)

Others:

  1. Diethylcarbamazine (DEC)
  2. Ivermectin
  3. Pyrantel Pamoate
  4. Praziquantel
  5. Niclosamide
  6. Biothionol
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10
Q

What is the MOA of Chloroquine?

A

MOA: inhibits heme polymerase → heme accumulates and is toxic to blood schizonts

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11
Q

How are Anti-Malarials classified?

A

Medications can be classified according to their efficacy on certain life-cycle stages:

  1. Tissue Schizonticides - act on liver forms; includes primaquine
  2. Blood Schizonticides - act on erythrocyte forms + prevent clinical symptoms; includes chloroquine, quinine
  3. Gametocides - kill gametocytes; includes primaquine
  4. Prophylactics
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12
Q

What is the MOA of Quinine and Quinidine?

A

They are cinchona alkaloids acting on blood schizonts by unknown mech (gametes in P. vivax/ovale).

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13
Q

What is the MOA of Mefloquine?

A

It has a unknown mechanism against blood schizonts + P. vivax/ovale gametes.

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14
Q

What is the MOA of Bithionol?

A

Bithionol inhibits oxidative phosphorylation.

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15
Q

What is the MOA of Pyrantel Pamoate?

A

Pyrantel Pamoate causes ACh release and ACh-ase inhibition → spastic paralysis.

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16
Q

What is the MOA of Niclosamide?

A

Niclosamide inhibits oxidative phosphorylation.

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17
Q

What is the MOA of Praziquantel?

A

Praziquantel increases calcium permeability → spastic paralysis.

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18
Q

What is the MOA of Levamisole?

A

Levamisole causes depolarizing neuromuscular blockade → paralysis.

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19
Q

What is the MOA of Ivermectin?

A

Ivermectin enhances GABA effect in helminths → paralysis.

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20
Q

What is the MOA of the Benzimidazoles?

A

Albendazole, mebendazole and thiabendazole inhibit B-tubulin polymerization → paralysis.

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21
Q

List the classifications of Helminths.

A

Classified into:

  1. Nematodes (roundworms)
  2. Trematodes (flukes)
  3. Cestodes (tapeworms)
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22
Q

What is the MOA of Nifurtimox?

A

Nifurtimox has an unclear mechanism; maybe radical metabolites effective in acute phase.

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23
Q

What is the MOA of Eflornithine?

A

Eflornithine inhibits ornithine decarboxylase.

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24
Q

What is the MOA of Sulfadoxine and pyrimethamine?

A

They inhibit folate synthesis.

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25
Q

Which drugs are used in the visceral form of leishmaniasis?

A

Amphotericin B or Miltefosine (oral)

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26
Q

List the 1st line drugs in Toxoplasmosis.

A

1st line = spiramycin, TMP-SMX or pyrimethamine + clindamycin + folinic acid (↓ sfx)

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27
Q

What is given in Trichomoniasis?

A

Nitroimidazoles, such as metronidazole.

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28
Q

What is the first line treatment of Giardiasis?

A

Nitroimidazoles + Nitazoxanide

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29
Q

What is the MOA for Iodoquinol?

A

Iodoquinol has an unknown mechanism. Perhaps because it has a poor oral absorption → luminal effect.

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30
Q

What is the MOA of Primaquine

A

Primaquine has an unknown mechanism against tissue schizonts in all strains.

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31
Q

What is the MOA of Halofantrine ?

A

Halofantrine has an unknown mechanism against blood schizonts in all strains.

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32
Q

What is the route of administration of Halofantrine?

A

Given orally + absorption enhanced by food.

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33
Q

What are the side effects of Halofantrine?

A

Side Effects:

  1. GI, rash, pruritus
  2. Arrhythmia - causes conduction disturbances (rarely used b/c of this … Lumefantrine has fewer side effects and is given with artemether for uncomplicated P. falciparum)
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34
Q

What is the pharmacokinetics like for Primaquine?

A

oral admin with good absorption

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35
Q

What are the indications of primaquine?

A
  1. Acute vivax or ovale malaria - curative
  2. prophylaxis for all strains P. jirovecii - with clindamycin
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36
Q

what are the side effects of primaquine?

A

well-tolerated, but:

  1. GI effects in high doses
  2. Rarely leukocytopenia, methemoglobinemia and HS reactions.
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37
Q

What is the MOA of Benznidazole?

A

Benznidazole inhibits protein + RNA synthesis.

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38
Q

What is the MOA of Melarsoprol?

A

Melarsoprol contains arsenic and thereby inhibits enzymes. Given as slow infusion.

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39
Q

When is pentamidine given in trypanosomiasis?

A

Pentamidine is given in early phase before CNS involvement.

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40
Q

What is the MOA and DOA of Suramin?

A

Suramin is also used in early phase trypanosomiasis. Unclear mechanism; inhibits protein synth + enzymes. Given IV and has a long half-life (40-50 days).

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41
Q

What is the MOA of Atovaquone?

A

Atovaquone inhibits mitochondria, affecting tissue + blood schizonts.

42
Q

What is the MOA of Artemisinin?

A

Artemisinin and derivatives artemether, artemotil, artesunate, dihydroartemisinin may act through free radical production against blood schizonts.

43
Q

What is the MOA of Proguanil?

A

Proguanil is given with atovaquone. It is a biguanid derivative with an active metabolite that inhibits 2HF reductase thymidylate synthase → ↓ DNA synthesis.

44
Q

What are the kinetics like for Chloroquine?

A

Given orally, accumulates in tissues, half life = 4 days.

45
Q

What are the indications for chloroquine?

A

For suppression and prophylaxis P. falciparum is often resistant!

46
Q

What are the side effects of chloroquine?

A

Chloroquines are well tolerated, however some side effects can occur like:

  1. Pruritus and GI effects
  2. Visual disturbances - rare, due to retinal/corneal deposits
  3. Hemolysis - in G6PD deficiency
47
Q

What is the route of administration of quinine and quinidine?

A

Both are given orally and can be given by slow IV.

48
Q

What are the side effects of quinine and quinidine?

A
  1. Cinchonism - quinine intoxication
  2. GI symptoms: Vomitting/Diarrhea
  3. Visual/hearing disturbance
  4. HS rxn
  5. Overdose can cause cardiotoxicity
49
Q

What are the kinetics like for Mefloquine?

A

Orally administered with slow absorption.

50
Q

What are the side effects of Mefloquine?

A

GI and neuropsychiatric effects

51
Q

What are the indications for Mefloquine?

A
  1. Prophylaxis - if chloroquine resistant P. falciparum (use ↓ due to side effects).
  2. Uncomplicated Malaria - with artesunate.
52
Q

What are the kinetics like for Bithionol?

A

Orally admin with BBB penetration.

53
Q

What are the side effects of Biothionol?

A
  1. GI
  2. CNS (dizziness, HA)
  3. toxic hepatitis
54
Q

What are the indications of biothionol?

A

In fascioliasis (Fasciola hepatica)

55
Q

What are the kinetics like for pyrantel pamoate?

A

Orally admin with poor absorption

56
Q

What are the side effects like for pyrantel pamoate?

A
  1. GI (medium severity)
  2. mild CNS effects
57
Q

What are the indications like for pyrantel pamoate?

A

Various roundworms (Ascaris, Necator, Ancylostoma, and Enterobius)

58
Q

What is the route of administration of Niclosamide?

A

orally admin with poor absorption

59
Q

What is the route of administration of Praziquantel?

A

oral admin and crosses BBB

60
Q

What is the route of administration of Levamisole?

A

orally administered.

61
Q

What are the kinetics like for ivermectin?

A

Orally admin; does not cross BBB.

62
Q

What are the indications for Benzimidazoles?

A

roundworm and tapeworm infections

63
Q

List the drugs targets of Antihelminthic drugs.

A

Drug targets are:

1) Neuromuscular coordination

2) Carbohydrate metabolism

3) Microtubules

64
Q

What is the route of administration of Eflornithine?

A

Given as IV (oral → diarrhea)

65
Q

What is the route of administration and side effects of Nifurtimox?

A
  1. Given orally
  2. Causes GI effects, neuropathy, seizures
66
Q

What are the indications of sulfadoxine and Pyrimethamine?

A

For chloroquine resistant uncomplicated malaria (falciparum often resistant!)

67
Q

List the 2nd line drugs in toxoplasmosis.

A

2nd line = pyrimethamine + sulfadiazine + folinic acid

68
Q

What is the second line therapy for giardiasis?

A
  1. Paromomycin, or…
  2. Furazolidone - a nitrofuran, given orally with GI side effects
  3. Quinacrine - broad-spectrum anti-protozoal; oral, long half-life, GI sfx
69
Q

What are the side effects of melarsoprol?

A
  1. GI effects
  2. hepatotoxic
  3. arrhythmia
  4. encephalopathy (give in severe CNS cases)
70
Q

What is the MOA of Nitroimidazoles?

A

Metronidazole and tinidazole have reactive reduction products that are cytotoxic.

71
Q

What are the indications for the Nitroimidazoles?

A

Given in combination for intestinal/extraintestinal infection (amebiasis)

72
Q

What is the MOA of Paromomycin?

A

Paromomycin is a protein synthesis inhibitor (aminoglycoside) used as a 2nd line for extra-/intestinal amebiasis.

73
Q

What are the side effects of Iodoquinol?

A

GI upset

74
Q

What are the indications for Iodoquinol?

A
  1. Asymptomatic intestinal amebiasis - as a monotherapy
  2. Intestinal / extraintestinal amebiasis - in combination
75
Q

What is the MOA of Diloxanide Furoate?

A

Diloxanide Furoate has an unknown mechanism. Perhaps it is its metabolite diloxanide that is absorbed that has some effect. (?)

76
Q

What are the side effects of Diloxanide Furoate?

A

GI upset

77
Q

What are the indications of Diloxanide Furoate?

A

It’s an alternative for asymptomatic amebiasis.

78
Q

What is the route of administration of Benznidazole?

A

oral admin

79
Q

What are the side effects of Benznidazole?

A
  1. GI effects
  2. neuropathy
  3. psychosis
80
Q

What are the side effects of Suramin?

A
  1. Kidney impairment
  2. Dermatitis
  3. Neuropathy
81
Q

What are the indications of atovaquone?

A
  1. Given with proguanil as treatment/prophylaxis in chloroquine-resistant strains (falciparum usually sensitive!)
  2. P. jirovecii - alternative treatment for infection.
82
Q

What is the route of administration of Artemisinin?

A

Artemisinin can be given oral, IV or IM

83
Q

What are the side effects of Artemisinin?

A

Artemisinin is well-tolerated however there are some GI effects.

84
Q

What are the indications of Artemisinin?

A

Given in combination for uncomplicated malaria (w/ mefloquine or lumefantrine)

85
Q

What are the side effects of Niclosamide?

A

GI, dizziness

86
Q

What are the indications for Niclosamide?

A

Taenia species (solium and saginata)

87
Q

What are the side effects of praziquantel?

A

GI, dizziness

88
Q

What are the indications for Praziquantel?

A

Against flukes and tapeworms (Schistosoma, F. hepatica, and Taenia)

89
Q

What are the side effects of Levamisole?

A
  1. GI
  2. Mild neurological symptoms
90
Q

What are the indications for Levamisole?

A

Certain roundworms (A. lumbricoides, A. duodenale, and N. americanus)

91
Q

What are the side effects of Ivermectin?

A

Mild, due to worm disintegration (fever, HA, dizziness, itching, joint pain).

92
Q

What are the indications of Ivermectin?

A

Certain roundworms (Loa loa, A. lumbricoides, A. duodenale and T. trichiura)

93
Q

What is the route of administration for Benzimidazoles?

A

Oral administration

94
Q

What are the side effects of Benzimidazoles?

A
  1. GI
  2. Hepatotoxic
  3. Visual disturbances
  4. Teratogenic
95
Q

What are the side effects of Eflornithine?

A

GI effects, seizures and marrow suppression (give in severe CNS cases)

96
Q

What is the 1st line therapy for P. jiroveci infection?

A

1st line = TMP-SMX

97
Q

What is the route of administration of Pentavalent antimonials?

A

Pentavalent antimonials such as sodium stibogluconate or meglumine antimoniate given IV as first choice in mucocutaneous form; few side effects

98
Q

What is the 2nd line therapy for P.jiroveci therapy?

A

2nd line = pentamidine or clindamycin plus primaquine or atovaquone

99
Q

What is the MOA of Pentamidine?

A

Pentamidine is reserve compound for antimonial resistance, which also has fungicidal effect. It has an unclear MOA. May inhibit DHFR or protein synthesis.

100
Q

What is the route of administration of Pentamidine?

A

given parenterally

101
Q

What are the side effects of Pentamidine?

A
  1. Arrhythmia
  2. Liver / Kidney disturbance
  3. Stevens-Johnson Syndrome

Pharmacology (Topic C) (20 decks)

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