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PoD - E4 > Antiparasitic Medications > Flashcards

Antiparasitic Medications Flashcards

1
Q

Major types of parasitic disease

A
  • Protozoan (ie malaria, ameibiasis)

- Helminthe (ie ascariasis, enterobiasis)

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2
Q

Types of Treatment - Antiprotozoal Agents

A
  • SUPPRESSIVE THERAPY: elimination of parasite responsible for acute symptoms
  • CLINICAL CURE: removal of all parasites from blood
  • RADICAL CURE: elimination of all parasite forms from the body
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3
Q

Antimalarial agents

A
  • Chloroquine
  • Primaquine
  • Quinine (Cinchona alkaloid)
  • Quinidine (Cinchona alkaloid)
  • Mefloquine
  • Pyrimethamine
  • Atovaquone-proguanil (Malarone)
  • Artemisinin and Derivatives
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4
Q

Antiprotozoal agents - Giardiasis

A
  • Metronidazole

- Furazolidone

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5
Q

Antiprotozoal agents - Amebicidic

A
  • Metronidazole
  • Iodoquinol (diiodohydroxyquine)
  • Paromomycin
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6
Q

Antihelminthic agents

A
  • Mebendazole (Vermox)
  • Ivermection
  • Pyrantel pamoate (Antiminth)
  • Thiabendazole
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7
Q

Chloroquine - Mechanism of Action

A
  • Parasite digests HgB of host red cells
  • HgB degradation product (ferriprotoporphyrin IX) is toxic to parasite membranes and essential enzymes
  • Parasite protects itself from ferri IX with the activity of a heme polymerase
  • CHLOROQUINE IS THOUGHT TO INHIBIT SEQUESTRATION OF HEME AND THIS HEME POLYMERASE
  • Oxidative damage results
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8
Q

Chloroquine - Uses

A

Asexual and erythrocytic forms in susceptible parasites

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9
Q

Chloroquine - Pharmacokinetics

A
  • Half-life: 4 days

- Allows for once weekly prophylaxis

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10
Q

Chloroquine - Resistance

A

Parasites actively transport chloroquine out of acidic digestive vacuole

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11
Q

Chloroquine - Adverse effects

A
  • Headache, N/V, blurred vision, dizziness, fatigue, confusion
  • RARE: depigmentation of hair, corneal opacities, hematological disorders, exacerbation of psoriasis, dose related retinopathy, hemolysis of G6PD deficient patients
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12
Q

Chloroquine - Contraindications

A
  • Psoriasis
  • Retinal disease
  • Epilepsy
  • Myasthenia gravis
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13
Q

Chloroquine - Indications

A
  • Prevention and treatment of malaria
  • Extraintestinal amebiasis (not FDA approved)
  • Inflammatory disease (RA, SLE) (not FDA approved)
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14
Q

Primaquine - Mechanism of Action

A

Interferes with mitochondrial function

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15
Q

Primaquine - Uses

A
  • Only agent available for treating exoerythrocytic hypnozoite forms of P. vivax and P. ovale in liver
  • Some activity against asexual blood stages of P. vivax but this action is not sufficient for prophylaxis
  • RADICAL CURE: P. vivax, P. ovale (prevent of relapse) - used after chloroquine in treatment or shortly before or just after chloroquine prophylaxis ends in persons with known exposure
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16
Q

Primaquine - Adverse effects

A
  • Methhemoglobinemia
  • Abdominal distress
  • Hemolysis in G6PD deficient patients
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17
Q

Quinine (Cinchona alkaloid) - Mechanism of action

A

Similar to chloroquine

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18
Q

Quinine (Cichona alkaloid) - Uses

A
  • Increased due to chloroquine resistance, quinine resistance now a problem
  • Can be used for PARENTERAL THERAPY (not available in US) against chloroquine and multi-drug resistant P. falciparum (in other countries)
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19
Q

Quinine (Cichona alkaloid) - Adverse effects

A
  • POOREST THERAPEUTIC TO TOXIC RATIO OF ALL ANTIMALARIAL AGENTS
  • CINCHONISM: dose related and reversible
  • Tinnitus, decreased hearing, headache, N/V, visual disturbances
  • RARE: hypersensitivity, hypoglycemia, hemolysis in G6PD deficient patients
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20
Q

Quinidine (Cinchona alkaloid) - Mechanism of Action

A

Similar to chloroquine

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21
Q

Quinidine (Cinchona alkaloid) - Uses

A
  • PARENTERAL therapy in chloroquine resistant P. falciparum (since quinine not available in US delays in therapy were occuring)
  • Being replaced by ARTEMISININS
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22
Q

Quinidine - Adverse effects

A
  • EKG changes

- Hypotension

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23
Q

Mefloquine - Mechanism of action

A
  • Derived from quinine
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24
Q

Mefloquine - Uses

A
  • Prophylaxis against drug resistant P. falciparum and P. vivax for travelers over extended periods into endemic areas
  • Schizontocidal drug; no effect on exoerythrocytic stage
  • Resistance to mefloquine is increasing in Thailand and West Africa
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25
Q

Mefloquine - Adverse effects

A

Causes vivid dreams

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26
Q

Pyrimethamine - Mechanism of Action

A
  • Structurally related to TRIMETHOPRIM

- Binds to and reversibly inhibits dihyrofolate reductase

27
Q

Pyrimethamine - Uses

A
  • Formally used in combination with SULFONAMIDE and QUININE for treatment of chloroquine resistant plasmodia
  • Occasionally used in pregnancy in endemic areas for prophylaxis
28
Q

Pyrimethamine - Adverse Effects

A
  • N/V/D, anorexia
  • Hypersensitivity reactions
  • Hematologic reactions
  • Anemia due to decrease in folic acid
  • MUST SUPPLEMENT LEUCOVORIN
29
Q

Atovaquone-proguanil (Malarone) - Mechanism of Action

A
  • ATOVAQUONE: mitochondrial toxicant in parasites
  • PROGUANIL: in active form, inhibits dihydrofolate-thymidylate synthase (decrease DNA synthesis)
  • Malarone is a fixed concentration drug containing atovaquone and proguanil with minimal toxicity
30
Q

Atovaquone-proguanil (Malarone) - Uses

A
  • Chemoprophylaxis and the treatment of uncomplicated P. falciparum malaria in children and adults
  • Asexual blood forms and liver stages of P. falciparum (BUT NOT P. vivax)
31
Q

Artemisinin - Uses

A
  • Derived from qing hao or sweet wormwood; parent plus 3 derivatives (dihyrdoartemisinin, artemether, and artesunate)
  • Effective against P. falciparum and asexual erythocytic stages of P. vivax
  • Gametocytocidal activity
  • May produce toxic heme adducts and oxidant stress
  • Generally used in combination with other drugs for treatment of severe P. falciparum malaria; may be given orally or parenterally; not used for chemoprophylaxis
  • NOT USED IN PREGNANCY
32
Q

Chemoprophylaxis for malaria

A
  • ATOVAQUONE-PROGUANIL: all areas
  • MEFLOQUINE: mefloquine sensitive malaria areas
  • CHLOROQUINE or HYDROXYCHLOROQUINE: restricted to areas of chloroquine-sensitive malaria
  • PRIMAQUINE: short stays in areas that are primarily P. vivax; anti-relapse therapy P. vivax and ovale
  • DOXYCYCLINE: all areas
33
Q

Treatment of malaria - P. falciparum

A
  • CHLOROQUINE RESISTANT: arteminisinin derivatives, malarone, mefloquine, clindamycin + quinine or quinidine
  • Doxycycline + quinine or quinidine
  • CHLOROQUINE SENSITIVE: chloroquine
34
Q

Treatment of malaria - P. vivax

A
  • Malarone
  • Chloroquine (sensitive areas)
  • Primaquine (radical cure, also P. ovale)
  • CHLOROQUINE RESISTANT: malarone, clindamycin + quinine or quinidine, doxycycline + quinine or quinidine
35
Q

Treatment of malaria - other plasmodia

A
  • Chloroquine phosphate or hydroxychloroquine

- Quinidine

36
Q

What is the most common enteric parasite in the US

A

Giardiasis

37
Q

Furazolidone - Adverse effects

A
  • GI complains

- Mild hemolysis in G6PD deficient patients

38
Q

Metronidazole - Mechanism of Action

A
  • Nitro group serves as an electron acceptor forming a reduced cytotoxic agent
  • Toxic form can bind to protein and DNA and may generate free radicals
39
Q

Metronidazole - Uses

A
  • Has systemic activity (severe disease or liver abscess)
  • Anaerobic bacteria
  • Entamoeba histolytica
  • E. polecki
  • Enteritis due to Giardia lamblia
  • VAGINITIS DUE TO TRICHOMONAS VAGINALIS (FDA approved)
  • Alternative for blastocystis hominis and balantidium coli
40
Q

Metronidazole - Adverse Effects

A
  • GI effects
  • Metallic taste
  • Disulfiram-like effect (alcohol intolerance)
41
Q

Iodoquinol (diiodohydroxyquine) - Uses

A

Asymptomatic amebiasis (drug of choice)

42
Q

Iodoquinol (diiodohydroxyquine) - Adverse Effects

A
  • GI complaints
  • Seizures
  • Encephalopathy
  • High iodine content can interfere with TFTs

TFT = thyroid function test

43
Q

Paromomycin - Uses

A
  • Aminoglycoside, poorly absorbed after oral administration

- Alternative to iodoquinol for asymptomatic amebiasis

44
Q

Paromomycin - Adverse Effects

A
  • GI complaints
  • Potentially nephrotoxic
  • Ototoxic (IV)
45
Q

Leishmaniasis - Treatment

A

Drug of choice - Antimonial agents

  • Sodium stibogluconate
  • Meglumine antimoniate

Alternatives: amphotericin B, pentamidine

46
Q

Trypanosomiasis - South American (Chagas Disease) - Treatment

A

Nifurtimox (drug of choice)

47
Q

Trypanosomiasis - African (Sleeping sickness) - Tsetse fly - Treatment

A
  • DRUGS OF CHOICE: eflornithine, suramin

- ALTERNATIVE: Pentamidine

48
Q

Toxoplasmosis - Treatment

A
  • DRUGS OF CHOICE: pyrimethamine (and leucovorin) + sulfadiazine
  • ALTERNATIVE: Pyrimethamine (and leucovorin) + clindamycin
49
Q

Enterobiasis (pinworm) - Treatment

A
  • Pyrantel pamoate
  • Mebendazole
  • Albendazole
50
Q

Ascariasis (roundworm) - Treatment

A
  • Mebendazole
  • Pyrantel pamoate
  • Albendazole
51
Q

Filariasis - Treatment

A

Diethycarbamazine

52
Q

Trichuriasis (whipworm) - Treatment

A
  • DRUG OF CHOICE: mebendazole

- ALTERNATIVE: albendazole

53
Q

Hookworm - Treatment

A
  • Mebendazole
  • Pyrantel pamoate
  • Albendazole
54
Q

Strongyloidiasis - Treatment

A
  • DRUG OF CHOICE: ivermectin

- ALTERNATIVE: thiabendazole

55
Q

Mebendazole - Mechanism of Action

A

Selectively binds to helminthic tubulin and blocks microtubule assembly in helminthes and inhibits glucose uptake resulting in immobilization and death

56
Q

Mebendazole - Adverse Effects

A
  • Abdominal pain

- Relatively no side effects at normal doses

57
Q

Ivermectin - Mechanism of Action

A
  • GABA receptor agonist
  • In nematodes and arthropods, GABA controls neurotransmission by sending inhibitory signals to motor neurons
  • Ivermectin potentiates these inhibitory signals and results in paralysis of the organism
58
Q

Ivermectin - Uses

A

Drug of choice for strongyloidiasis

59
Q

Ivermectin - Adverse Effects

A

Minimal - GI complaints and drowsiness

60
Q

Pyrantel Pemoate - Mechanism of Action

A

Depolarizing neuromuscular blocking agent

61
Q

Pyrantel Pemoate - Uses

A

Alternative to mebendazole for

  • Ascariasis
  • Hookworm
  • Pinworm
62
Q

Pyrantel Pemoate - Adverse Effects

A

Minimal - GI complaints, headache, drowsiness

63
Q

Thiabendazole - Mechanism of Action

A

Inhibits the fumurate reductase of susceptible helminths

64
Q

Thiabendazole - Uses

A
  • Second line agent for strongyloidiasis
  • TREMATODES (flukes): praziquantel
  • CESTODES (tapeworms): niclosamide

PoD - E4 (5 decks)

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