ANTIPROTOZOAL AGENTS Flashcards

1
Q

This disease are highly prevalent in tropical third world countries

A

Antiprotozoal Agents

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2
Q

The common protozoal diseases:

A

-malaria
-amebiasis
-giardiasis
-trichomoniasis, toxoplasmosis & as a direct consequence of the AIDS
epidemic, pneumocystis carinii pneumonia

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3
Q

Entamoeba
histolytica

A

Amebiasis

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4
Q

Balantidium coli

A

Balantidiasis

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5
Q

Giardia lamblia

A

Giardiasis

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6
Q

Cryptosporidium
spp

A

Cryptosporidiosis

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7
Q

Trichomonas vaginalis

A

Trichomoniasis

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8
Q

Genital infection

A

Trichomoniasis

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9
Q

Pneumocystis carinii
(opportunistic pathogen)

A

Pneumocystis carinii
pneumonia

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10
Q

Best known for causing blindness in neonates

A

Toxoplasmosis

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11
Q

Leishmania donovani

A

Lieshmaniasis

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12
Q

2-methyl-5-nitroimidazole-1-ethanol

A

Metronidazole (Flagyl)

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13
Q

-Most useful of a group of antiprotozoal nitroimidazole derivatives

-First marketed for topical tx Trichomonas vaginalis vaginitis; effective
orally against both acute & carrier states of disease

-Possess amebicidal activity; effective against both intestinal & hepatic
amebiasis

-Also use in the tx for giardiasis & balantidiasi

A

Metronidazole (Flagyl)

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14
Q

Because of its bactericidal action, it has become an important agent
for treatment of serious infections (septicemia, pneumonia,
peritonitis, pelvic infections, abscesses, meningitis) caused by anaerobic bacteria

A

Metronidazole

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15
Q

Effective against obligate anaerobic bacteria but ineffective against
facultative anaerobes or obligate aerobes

A

Metronidazole

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16
Q

Despite its low water solubility, it is well absorbed following oral administration

A

Metronidazole

17
Q

Is administeres parenterally only via slow infusion

A

Metronidazole

18
Q

are unsuitable for IV administration
because of their extreme acidity

A

Metronidazole

19
Q

-Possessed amebicidal activity in vitro
-Treatment of asymptomatic carriers of E. Histolytica
-Administered orally only as 500 mg tablets

A

Diloxanide Furoate

20
Q

For acute & chronic intestinal amebiasis but not effective in extraintestinal
disease

A

Lodoquinol

21
Q

Relatively high incidence of neuropathy occurs, so it should not be used
routinely for traveler’s diarrhea

A

Lodoquinol

22
Q

-Obtained by separation from extracts of ipecac
 Exert direct amebicidal action on various forms of E. Histolytica

-Protoplasmic poisons that inhibit protein synthesis in protozoal &
mammalian cells by preventing protein elongation

-Used only in combination w/ other agents because their effect in intestinal
amebiasis is solely symptomatic & cure rate only 10%-15%

-Toxic effect limit its usefulness

A

Emetine & Dehydroemetine

23
Q

Causes high frequency of GI distress (nausea & diarrhea), cardiovascular
effects (hypotension & arrhythmia) & neuromuscular effects (pain &
weakness)

A

Emetine & Dehydroemetine

24
Q

Lower incidence of cardiotoxicity w/ dehydroemetine

A

Emetine & Dehydroemetine

25
Q

-Treatment of pneumonia caused by opportunistic pathogenic protozoan P.
Carinii, a frequent secondary invader associated w/ AIDS

-Administered by slow IV infusion or by deep IM injection for PCP

-Aerosol form – used by inhalation for prevention of PCP in high-risk patients
infected w/ HIV

-Both inhalant & parenteral dosage forms are sterile lyophilized powders that
must be made up as sterile aqueous solutions prior to use.

-Sterile water for injection must be used to reconstitute the aerosol, to avoid
precipitation of pentamidine salt

A

Pentamidine Isethionate

26
Q

Cough & bronchospasm

A

Inhalation

27
Q

Hypertension & hypoglycemia

A

Injection

28
Q

-Prophylaxis and treatment of African trypanosomiasis

-Also for treating visceral leishmaniasis

-Prophylactic agent – rapidly disappears from plasma after IV injection and
is distributed to tissues, where it is stored for a long period.

A

Pentamidine Isethionate (NebuPent®)

29
Q

-Highly lipophilic, water-insoluble analog of ubiquinone 6, an essential
component of mitochondrial electron transport chain in microorganisms

-Act as an antimetabolite for ubiquinone, thus interfere w/ function of
electron transport enzymes

-Originally developed as antimalarial drug but Plasmodium falciparum
developed rapid tolerance to its action

A

Atovaquone (Mepron)

30
Q

-Recommended alternative to TMP-SMX for tx & prophylaxis of PCP in
patients intolerant to this combination

-Effective in eradicating T. Gondii in preclinical animal studies

-Slow & incomplete oral absorption because of low water solubility of drug

-Aqueous suspensions have better absorption than tablets

-Food (esp. high fat content) increases absorption

A

Atovaquone

31
Q

Half life of Atovaquone is

A

62 to 80 hours

32
Q

Side effects of Atovaquone

A

GI intolerance

33
Q

-Treatment of West African sleeping sickness (Trypanosoma brucei / gambiense)

-Indicated for meningoencephalitic stage of disease

-Myelosuppressive drug that causes high incidences of anemia, leukopenia,
thrombocytopenia

-Monitor CBC during course of therapy

-Irreversible inactivation of ornithine decarboxylase by eflornithine is accompanied
by decarboxylation & release of fluoride ion from inhibitor, suggesting enzymecatalyzed activation of inhibitor

-Administered either IV or orally

-Penetration into CSF is facilitated by inflammation of meninges

A

Elfornithine

34
Q

-In addition to their antibacterial & antifungal properties, also have
antiprotozoal activity w/c led to discovery of particular nitrofurans w/
antitrypanosomal activity

-Effective against T. cruzi (South American)

-Only clinically proven treatment for both acute and chronic forms of disease

-Administered orally

-Oral bioavailability is high but first-pass metabolism occurs

  • Half-life: 2-4 hrs
    -High incidence of n&v, abdominal pain & anorexia
A

Nifurtimox

35
Q

-Nitroimidazole derivative

-Treament of Chagas disease

-Effectiveness similar to that of nifurtimox

-Therapy w/ oral benznidazole requires several weeks

-A/E: peripheral neuropathy, bone marrow depression, allergic-type
reactions

A

Benznidazole (Radanil®, Rochagan®

36
Q

-Prepared by reduction of corresponding pentavalent arsanilate to the trivalent
arsenoxide followed by reaction of latter w/ BAL

-DOC for treatment of later stages of both forms of African trypanosomiasis

-Advantage: excellent penetration into CNS, thus effective against
meningoencephalitic forms of T. gambiense & T. Rhodesiense

-Trivalent arsenicals tend to be more toxic to host than corresponding
pentavalent compounds

-Shares toxic properties of other arsenicals, so its use must be monitored for
signs of arsenic toxicity

A

Melarsopol

37
Q

-Pentavalent antimonial compound

  • Treatment of various forms of leishmaniasis

-10% aqueous solution used for either IM or IV injection has pH of
approximately 5.5

-Low therapeutic index, thus monitor carefully for signs of heavy metal
poisoning

  • Antileishmanial action requires its reduction to trivalent form, w/c is
    believed to inhibit phosphofructokinase in parasite
A

Sodium Stibogluconate

38
Q

-2,3-Dimercapto-1-propanol, BAL, dithioglycerol

  • Developed by British during WWII as antidote for “Lewisite”, hence the
    name British anti-Lewisite
  • Effective topically & systematically as antidote for poisoning caused by
    arsenic, antimony, mercury, gold & lead

-Antidotal properties are associated w/ property of heavy metals to react
w/ sulfhydryl groups in proteins & interfere w/ their normal function

  • Topically as ointment or IM as 5% or 10% sol’n in peanut oil
A

Dimercaprol

39
Q

-High-molecular-weight bisurea derivative containing 6 sulfonic acid groups as
their sodium salts

  • Developed in Germany after WWI as byproduct of research efforts directed
    toward development of potential antiparasitic agents from dyestuffs

-Treatment of early cases of trypanosomiasis

  • Long-term prophylactic agent (effectiveness after single IV injection maintained
    up to 3 months)
  • Tissue penetration of drug does not occur bec. of its high molecular weight &
    highly ionic character.
  • Thus, injected dose remains in plasma for very long period

-Prophylaxis of onchocerciasis

A

Suramin Sodium