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PoD - E4 > Antiparasitic Medications > Flashcards

Antiparasitic Medications Flashcards

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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
Mefloquine - Adverse effects
Causes vivid dreams
26
Pyrimethamine - Mechanism of Action
- Structurally related to TRIMETHOPRIM | - Binds to and reversibly inhibits dihyrofolate reductase
27
Pyrimethamine - Uses
- Formally used in combination with SULFONAMIDE and QUININE for treatment of chloroquine resistant plasmodia - Occasionally used in pregnancy in endemic areas for prophylaxis
28
Pyrimethamine - Adverse Effects
- N/V/D, anorexia - Hypersensitivity reactions - Hematologic reactions - Anemia due to decrease in folic acid - MUST SUPPLEMENT LEUCOVORIN
29
Atovaquone-proguanil (Malarone) - Mechanism of Action
- 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
Atovaquone-proguanil (Malarone) - Uses
- 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
Artemisinin - Uses
- 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
Chemoprophylaxis for malaria
- 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
Treatment of malaria - P. falciparum
- CHLOROQUINE RESISTANT: arteminisinin derivatives, malarone, mefloquine, clindamycin + quinine or quinidine - Doxycycline + quinine or quinidine - CHLOROQUINE SENSITIVE: chloroquine
34
Treatment of malaria - P. vivax
- Malarone - Chloroquine (sensitive areas) - Primaquine (radical cure, also P. ovale) - CHLOROQUINE RESISTANT: malarone, clindamycin + quinine or quinidine, doxycycline + quinine or quinidine
35
Treatment of malaria - other plasmodia
- Chloroquine phosphate or hydroxychloroquine | - Quinidine
36
What is the most common enteric parasite in the US
Giardiasis
37
Furazolidone - Adverse effects
- GI complains | - Mild hemolysis in G6PD deficient patients
38
Metronidazole - Mechanism of Action
- 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
Metronidazole - Uses
- 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
Metronidazole - Adverse Effects
- GI effects - Metallic taste - Disulfiram-like effect (alcohol intolerance)
41
Iodoquinol (diiodohydroxyquine) - Uses
Asymptomatic amebiasis (drug of choice)
42
Iodoquinol (diiodohydroxyquine) - Adverse Effects
- GI complaints - Seizures - Encephalopathy - High iodine content can interfere with TFTs TFT = thyroid function test
43
Paromomycin - Uses
- Aminoglycoside, poorly absorbed after oral administration | - Alternative to iodoquinol for asymptomatic amebiasis
44
Paromomycin - Adverse Effects
- GI complaints - Potentially nephrotoxic - Ototoxic (IV)
45
Leishmaniasis - Treatment
Drug of choice - Antimonial agents - Sodium stibogluconate - Meglumine antimoniate Alternatives: amphotericin B, pentamidine
46
Trypanosomiasis - South American (Chagas Disease) - Treatment
Nifurtimox (drug of choice)
47
Trypanosomiasis - African (Sleeping sickness) - Tsetse fly - Treatment
- DRUGS OF CHOICE: eflornithine, suramin | - ALTERNATIVE: Pentamidine
48
Toxoplasmosis - Treatment
- DRUGS OF CHOICE: pyrimethamine (and leucovorin) + sulfadiazine - ALTERNATIVE: Pyrimethamine (and leucovorin) + clindamycin
49
Enterobiasis (pinworm) - Treatment
- Pyrantel pamoate - Mebendazole - Albendazole
50
Ascariasis (roundworm) - Treatment
- Mebendazole - Pyrantel pamoate - Albendazole
51
Filariasis - Treatment
Diethycarbamazine
52
Trichuriasis (whipworm) - Treatment
- DRUG OF CHOICE: mebendazole | - ALTERNATIVE: albendazole
53
Hookworm - Treatment
- Mebendazole - Pyrantel pamoate - Albendazole
54
Strongyloidiasis - Treatment
- DRUG OF CHOICE: ivermectin | - ALTERNATIVE: thiabendazole
55
Mebendazole - Mechanism of Action
Selectively binds to helminthic tubulin and blocks microtubule assembly in helminthes and inhibits glucose uptake resulting in immobilization and death
56
Mebendazole - Adverse Effects
- Abdominal pain | - Relatively no side effects at normal doses
57
Ivermectin - Mechanism of Action
- 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
Ivermectin - Uses
Drug of choice for strongyloidiasis
59
Ivermectin - Adverse Effects
Minimal - GI complaints and drowsiness
60
Pyrantel Pemoate - Mechanism of Action
Depolarizing neuromuscular blocking agent
61
Pyrantel Pemoate - Uses
Alternative to mebendazole for - Ascariasis - Hookworm - Pinworm
62
Pyrantel Pemoate - Adverse Effects
Minimal - GI complaints, headache, drowsiness
63
Thiabendazole - Mechanism of Action
Inhibits the fumurate reductase of susceptible helminths
64
Thiabendazole - Uses
- Second line agent for strongyloidiasis - TREMATODES (flukes): praziquantel - CESTODES (tapeworms): niclosamide

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