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Pharmacology FINAL (2nd sem) > C3 > Flashcards

C3 Flashcards

1
Q

Antiprotozoal and antihelminthic drugs

A
  • Antiprotozoal agents:
    • Antimalarials
      • chloroquine
      • mefloquine
      • primaquine
      • quinine
      • artemether
      • atovaquone
      • proguanil
    • Anti-amebic:
      • metronidazole, tinidazole
      • paromomycin
  • Anti-helminthic agents:
    • mebendazole
    • ivermectin
    • niclosamide
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2
Q

DRUGS FOR MALARIA?

A

Chloroquine
Artemether
Quinine
Mefloquine
Primaquine

atovaquone

proguanil

lumefantrine , minimal cardiotoxicity, is now used in fixed combination with artemether

(Coartem) for uncomplicated falciparum malaria.

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3
Q

Chloroquine MOA?

A

prevents polymerization of the hemoglobin breakdown product heme into hemozoin

blood schizonticide

  • Intracellular accumulation
    of heme is toxic to the parasite
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4
Q

Chloroquine PharmacoKinetix?

A

orally

large volume of distribution ( needs a loading dose in lifethreatening infection)

  • Antacids may decrease oral absorption
    of the drug
  • Elimination: unchanged in the urine.
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5
Q

Chloroquine Clinical use?

A

Blood schizonticide

ALL non-resistant malarias

  • autoimmune disorders (rheumatoid arthritis)
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6
Q

Chloroquine Toxicity?

A
  1. GI irritation
  2. skin rash
  3. headaches
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7
Q

what about Artemether?

A
  • metabolized in the food vacuole of the parasite –> toxic free radicals
  • blood schizonticides active against P.falciparum (also MDRs)
  • Adverse effects are mild : GI upset
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8
Q

Quinine MOA?

A
  • form complexes with double-stranded DNA to prevent strand separation –> block of DNA replication and transcription to RNA
  • it is blood schizonticide
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9
Q

Quinine PharmacoKinetix?

A

orally
- metabolized before renal excretion

  • I.V. administration is possible in severe infections
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10
Q

Quinine Clinical use?

A
  • in P.falciparum infections resistant to chloroquine (for those who tolerate oral treatment)
  • should not be used routinely for prophylaxis
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11
Q

Quinine Toxicity?

A
  • cinchonism (GI distress, headache, vertigo, blurred vision, and tinnitus)
  • Severe overdose: disturbances in cardiac conduction
  • Hematotoxic effects: G6PD-deficient
  • Blackwater fever (intravascular hemolysis) is a rare and sometimes fatal complication in quinine-sensitized persons
  • it is contraindicated in pregnancy
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12
Q

Mefloquine, primaquin MOA?

A

unknown :)

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13
Q

Mefloquine PharmacoKinetix?

A

orally because of local irritation

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14
Q

Mefloquine clinical use?

A
  • first-line drug (taken weekly) for prophylaxis
  • daily for infection
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15
Q

Mefloquine Toxicity?

A
  • GI upset
  • skin rash, headache, and dizziness
  • At high doses:
    cardiac conduction abnormality, psychiatric disorders, and seizures
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16
Q

Primaquine MOA?

A
  • unknown mech
  • it is a tissue schizonticide
  • limits malaria transmission by acting as a gametocide
17
Q

Primaquine PharmacoKinetix?

A

Absorption is complete after oral administration

18
Q

Primaquine Clinical use?

A
  • against liver stages of P.Vivax and P.Ovale
  • PCP ( P.jiroveci pneumonia)
  • should be used in conjunction with a blood schizonticide
19
Q

Primaquine Toxicity?

A
  • well tolerated but may cause:
    1. GI distress
    2. headaches
    3. . Blood cytopenias
  • More serious toxicity:
    hemolysis (G6PD-deficients)

*contraindicated in pregnancy*

20
Q

what about Atovaquone ?

A
  • disrupt mitochondrial metabolism ( electron transport in protozoa)

Malarone (Atova + Proguanil) for both chemoprophylaxis (taken daily) and treatment of falciparum malaria

  • rash , fever, GI effects occur at the higher doses
21
Q

DRUGS FOR AMEBIASIS?

A

Metronidazole, tinidazole

Paromomycin

22
Q

Antihelminthic drugs

A
  • Round worms (Nematodes):
    • Mebendazole
    • Ivermectin
    • Albendazole
    • Diethylcarbamazine
  • FLUKES (Trematodes)
    • Praziquantel
  • Tape worm (Cestodes)
    • Albendazole
    • Mebendazole
    • Niclosamide
    • Praziquantel
23
Q

Proguanil MOA, administration

A

Antifolate

-inhibits folate synthesis

oral

24
Q

Proguanil effects

A

Mostly blood schizonticide

25
Q

Proguanil toxicity

A

GI upset

rash (sometimes severe)

cytopenia

26
Q

metronidazole MOA

A

reactive metabolic products

Anti-amebic agents

27
Q

metronidazole clinical uses

A
  • Luminal amebiasis
  • Extra-intestinal amebiasis
  • giardiasis
  • trichomoniasis
28
Q

metronidazole pharmacokinetic

A
  • oral
  • rapid diffusion into all tissues
29
Q

metronidazole toxicity

A
  • Nausea
  • headache
  • paresthesia
  • disulfiram effect
30
Q

Mebendazole MOA

A

Selective inhibiton of microtubule synthesis and glucose uptake in round worms

31
Q

Mebendazole clinical uses

A
  • Ascariasis
  • pinworm
  • whipworm infections
32
Q

mebendazole pharmacokinetics

A
  • less than 10% is absorbed systematically after oral use
  • metabolised by hepatic enzymes

plasma levels can be increased by cimetidine

decreased by carbamazepine or phenytoin

33
Q

mebendazole toxicity

A
  • GI irritation
  • granulocytopenia (high dose)
  • alopecia (high dose)
  • teratogenic ; CI in pregnancy
34
Q

Ivermectin MOA

A
  • intensifies GABA-mediated neurotranmission in round worms
  • causes immobilization of parasite; facilitate their removal by reticuloendothelial system.
  • DOESNT cross BBB
35
Q

Ivermectin clinical use

A
  • Onchocerciasis
  • cutaneous larva migrans
  • stronglodiasis

against round worms

36
Q

Ivermectin SE

A
  • reactions due to dying worms :
    • fever
    • headache, dizziness
    • rash
    • pruritis
    • tachycardia
    • hypotension
    • joint pain
    • muscle pain
    • lymph gland pain
  • controlled with NSAID, Antihistamines
  • CI in pregnancy
37
Q

Niclosamide MOA

A
  • Uncoupling oxidative phosphorylations
  • OR by activating ATPases.
38
Q

Niclosamide Clinical uses

A
  • Beef, pork, fish tapeworm
  • small, large intestinal flukes
39
Q

Niclosamide toxicity

A
  • GI distress
  • headache
  • rash
  • fever

Avoid ethanol consumption 24-48 hres

Pharmacology FINAL (2nd sem) (37 decks)

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