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PPP-3 > Antiparasitic Drugs > Flashcards

Antiparasitic Drugs Flashcards

1
Q

What stages of the malaria life cycle do quinolones affect?

A

Trophozoite, schizont, and gametocyte stages in blood vessels

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2
Q

What are the pharmacokinetics of Quinolone derivatives?

A
  • Quinine is PO and must take 3x a day
  • Quinidine is IV but not used anymore
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3
Q

What are clinical uses of derived quinolines?

A

Quinine: used for treatment of drug resistant P. falciparum infection
Quinidine: is used for severe malarial infection but discontinued

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4
Q

What are adverse effects of quinoline derivatives?

A
  • GI effects (most common)
  • Cardiac effects like QT prolongation (TdP)
  • Cinchonism (tinnitus, headaches, dizziness)
  • Acute hemolytic anemia (in pt w G6PD deficiency)
    CIs: G6PD deficiency for quinine only
    Interactions: inhibits CYP2D5 and PGP
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5
Q

What is the MOA and clinical uses for chloroquine and hydroxychloroquine?

A

MOA: similar to quinine and inhibits hem-polymerase activity leading to a toxic buildup of heme (same MOA for quinine, quinidine, and mefloquine)
Clinical uses: treatment and prophylaxis of non-resistant P. falciparum and P. malariae + can be used in combination w primaquine for eradication of hepatic stages of P. vivax and P. ovale

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6
Q

What are adverse effects of chloroquine and hydroxychloroquine?

A

GI (n/v/d), QT prolongation, pruritus, visual disturbances
CIs: psoriasis or ocular disease

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7
Q

What is the MOA

A
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8
Q

What are clinical uses for mefloquine?

A

Prophylaxis (once week dosing) and treatment for drug resistant P. falciparum

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9
Q

What are adverse effects for mefloquine?

A

GI (n/v/d), QT prolongation, vivid dreams (common), headache, anxiety, psychosis, seizures
CIs: epilepsy, psychosis, schizophrenia, depression, anxiety (all BBW)

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10
Q

What are clinical uses for primaquine?

A
  • Active against hepatic stages of P. vivax and P. ovale (used in combo w chloroquine)
  • Highly gametocidal against all 4 malaria species
  • Only agent active against dormant hypnozoite stages
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11
Q

What stages of the malaria life cycle does primaquine affect?

A

Stages in the hepatocytes where it is in the form of schizont, sporozoite, and hypnozoite

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12
Q

What are adverse effects for primaquine?

A

GI, QT prolongation, hemolysis and hemolytic anemia (high risk if G6PD if deficient so must test) + counsel pts to look for dark colored urine
CIs: G6PD deficiency and pregnancy
Interactions: Induces CYP1A2 so caution w drugs like warfarin

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13
Q

What drugs are artemisinin and/or derivatives?

A

Artesunate, artemether, and dihydroartemisinin
Characteristics: potent and acts fast so VERY effective and bonus bc many formulations

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14
Q

What is the MOA of artemisinin and/or derivatives

A

Binds iron, breaks down peroxide bridges–> produces free radicals that can damage parasite

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15
Q

What stages of the malaria life cycle do artemisinin and/or derivatives affect?

A

Affects trophozoite, schizont, and gametocyte stages in blood vessels

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16
Q

What are clinical uses for artemisinin and/or derivatives?

A
  • Treatment of uncomplicated falciparum malaria and used in combo (artemether-lumefantrine)
  • Treatment of complicated falciparum malaria (artesunate and artemether)
17
Q

What are side effects of artemisinin and/or derivatives?

A
  • GI (n/v/d), dizziness
    CIs: first trimester of pregnancy and children < 5kg
18
Q

What are general characteristics of antifolates?

A
  • Used as combination regimens (atovaquone and proguanil aka Malarone)
19
Q

What antifolates are used for treatment of malaria?

A

Atovaquone and proguanil

20
Q

What is the MOA of malarone?

A

Atovaquone: disrupts mitochondrial electron transport in parasite and affects nucleotide synthesis
Proguanil: DHFR inhibitor

21
Q

What stage of the malaria life cycle does malarone affect?

A

Liver: schizont and sporozoite stages
Blood vessels: schizont and merozoite stages

22
Q

What are clinical uses of antifolates (malarone) and adverse effects?

A
  • Used for treatment and prophylaxis of chloroquine resistant P. falciparum
  • Adverse effects are abdominal pain, n/v/d, elevated liver enzymes
    CI: pregnancy
23
Q

What else can be used to treat and prevent malaria?

A

Antibiotics like tetracycline, doxycycline, and clindamycin as they inhibit protein synthesis in parasite apicoplast (affects schizont and merozoite stage in blood vessel)
- Used alone for prophylaxis and in combo w quinine for tx

24
Q

Metronidazole clinical use

A

Treats amebiasis (w or w/o extraintestinal issues), giardiasis, and trichomoniasis

25
Q

Tinidazole clinical use

A

Amebiasis, giardiasis, and trichomoniasis

26
Q

Paromomycin (amninoglycoside) clinical use

A

Amebiasis (for asymp and together w metronidazole for intestinal disease) and giardiasis

27
Q

Iodoquinol clinical uses and special adverse effects

A

Used to treat Amebiasis and can have mild diarrhea and enlargement of thyroid

28
Q

T/F: Using paromomycin to treat giardiasis is safer in a pregnant patient

A

True

29
Q

Nitazoxanide clinical use and adverse effects

A

Giardiasis and can cause abdominal pain w diarrhea

30
Q

What drugs have a luminal action?

A

Paromomycin and iodoquinol

31
Q

What drug is a benzimidazole, how does it work, and what can it be used for?

A

Albendazole that is very broad spectrum but mainly GI helminths (nematodes) and cysticercosis or invasive cestodes
MOA: interferes w microtubule synthesis (inhibits cell replication) and microtubule-dependent glucose uptake
- Give w high fat meals

32
Q

What are side effects seen in albendazole?

A

GI and elevation of liver enzymes
CIs: pregnancy and hepatic disease

33
Q

What is the MOA, clinical use, and adverse effects for pyrantel pamoate?

A

MOA: neuromuscular blocking agent that increases Ach release and causes paralysis to the worm
Clinical use: intestinal helminths (roundworms, pinworm, hookworm)
Adverse effects: GI, dizziness, and elevation of liver enzymes

34
Q

What is the MOA, clinical use, and adverse effects for ivermectin?

A

MOA: Increases Cl ions and causes hyperpol then death to parasite
Clinical use: severe intestinal nematodes (not hookworm)
Adverse effects: diarrhea, pruritus
CI in pregnancy

35
Q

What is the MOA, clinical use, and adverse effects for praziquantel?

A

MOA: increased membrane permeability to calcium causes contraction which leads to paralysis
Clinical use: schistosomiasis (DOC), cysticercosis and many other intestinal tapeworms
Adverse effects: n/v/d, headache, dizziness, pruritus

36
Q

What MOA does albendazole have?

A

Starve the worm

37
Q

What MOA does ivermectin, pyrantel pamoate, and praziquantel share?

A

They all paralyze the worm

PPP-3 (21 decks)

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