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Clinical Pharmacology II > Antifungal & Antiparasitic > Flashcards

Antifungal & Antiparasitic Flashcards

1
Q

What are the four major families of Antifungal’s ?

A
  • Polyene Macrolides
    Natural Antifungals
  • Azole Drugs
    Synthetic Antifungals
  • Echinocandins
    Semisynthetic Antifungals
  • Allylamines
    Synthetic Antifungals
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2
Q

What does the fungal cell membrane have and what is its function?

A
  • Ergosterol

- Strength and Fluidity

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3
Q

What does the Fungal cell wall have and what is it’s function?

A
  • B1,3 and B1,6 Glucans
    Strength and Rigidity
  • Glucans
    Link glucose molecules
  • Mannoproteins
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4
Q

What are the two targets for Antifungal agents?

A

1) Ergosterol Syn

2) Glucan Synthesis

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5
Q

What antifngal targets the enzyme Squalene Epoxidase in the fungal cell membrane?

A
  • Terbinafine
    (Allylamines)
  • Prevents Squalene from becoming Squalene Epoxide
  • Prevents Ergosterol Syn
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6
Q

What antifungal targets the CYP450 in fungus in the fungal cell membrane?

A
  • Fluconazole
    (Azoles)
  • Prevents Ergosterol Syn
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7
Q

What antifungal interferes with Ergosterol in the Fungal cell membrane?

A
  • Amphotericin B & Nystatin
    (Polyene Macrolides)
  • Interferes with Ergosterol in cell membrane
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8
Q

What antifungal targets fungal cell wall Beta Glucan syn ?

A
  • Caspofungin

Echinocandins

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9
Q

MOA for Amphotericin B?

A
  • Forms membrane pores via interaction with Ergosterol

- Causes leakage of cellular contents killing the fungi

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10
Q

T of F

Amphotericin B has poor GI absorption?

A
  • True

- Very poor PO GI (Exploited to treat GI infections)

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11
Q

The half life of Amphotericin B is ?

A
  • Long half-life
  • T1/2 > 15 days (2 weeks)
  • Slow kidney excretion
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12
Q

T or F

You can give Amphotericin B IV or Intrathecally?

A
  • True

- Treats CNS infections (Fungal Meningitis)

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13
Q

T or F

Amphotericin B has no impact on Renal or Hepatic impairment?

A
  • True

- 90% serum protein bound

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14
Q

What antifungal has the widest spectrum of coverage and is the initial therapy or empiric therapy for life threatening infections?

A
  • Amphotericin B
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15
Q

What does Amphotericin B treat?

A
  • Pathogenic yeast (Candida; Cryptococcus)
  • Dermatophytes (Dermal / Topical infections)
  • Pathogenic Molds Aspergillis
  • Endemic mycoses for FL and SW US are blastomycosis, coccidiodomycosis, histoplasmosis, and sporotrichoisis
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16
Q

T or F

Amphotericin B can form pores in human cells as well?

A
  • True

- Fungicidal & relatively selectively Toxic (Can form pores in human cells too)

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17
Q

Amphotericin B has a lot of toxicities most common is?

A
  • Infusion Related Reaction (Common)
Chills
Muscle spasms
Vomiting
HA
Hypotension
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18
Q

How do you prevent Amphotericin B infusion toxicities?

A
  • Test Dose Before

or

  • Pretreatments with Antipyretics. Antihistamine, Corticosteroids
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19
Q

How can you minimize Amphotericin B infusion reactions?

A
  • Slow infusion

- Minimize the dosage

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20
Q

What is the Major and Limiting Toxicity of Amphotericin B

A
  • Irreversible Nephrotoxicity
  • Due to Prolonged/High Dose

Hypokalemia
Hypomagnesemia
Renal Tubular Acidosis

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21
Q

The precursor to Ergosterol is lanosterol and it is blocked by Azole drugs by targeting what in the fungus?

A
  • CYP450

- Disrupting Strength and Fluidity

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22
Q

What group of antifugal medications have a Imidazole (2N) 5 member or Triazole (3N) 5 member ring?

A
  • Azole drugs
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23
Q

What are Imidazole (2n) used as?

A
  • Topical Antifungals
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24
Q

What are Triazoles (3n) used as ?

A
  • Systemic Antifungals
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25
Q

Metabolism of Azoles is important because it can also inhibit human CYP450, which ones exactly? Why is it important?

A
  • CYP3A4 (moderate)
    75% of FDA approved drugs
  • CYP2C9 (moderate)
  • CYP2D19 (strong)
  • CYP2C19 (strong)
  • A lot of Drug Drug interactions
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26
Q

What is Fluconazole used to treat?

A
  • Yeasts
    Candida
    Cryptococcus
  • Dermatophytes
    Ringworm
    Jock itch
    Athlete’s foot
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27
Q

T or F

Fluconazole treats Pathogenic Molds as well?

A
  • False
  • Does not treat
    Mucormycosis
    Aspergillus
    Fusarium
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28
Q

T of F

Azole drugs like Fluconazole inhibit CYP450 in fungas but it can inhibit it in humans as well, why is that important?

A
  • True
  • Inhibits 17-alpha-hydroxylase
    (CYP450c17)
  • Blocks Sex hormone
    Testosterone, Estrogen
  • Blocks Glucocorticoids
    Drying and Thinning skin
  • Mineralcorticoids remain intact or elevated
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29
Q

MOA for Caspofungin (Echinocandin)?

A
  • Inhibits the synthesis of β1-3-glucan to prevent cell wall biogenesis
  • Cell wall formation
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30
Q

T or F

Caspofungin (Echinocandin) needs to be dose adjusted for hepatic insufficiency?

A
  • True
  • Extensively metabolized in the liver
  • Peptide hydrolysis
  • N-acetylation
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31
Q

What is the major concern with toxicity with Caspofungin ?

A
  • Hepatotoxcitiy
    Drug Drug reactions
  • Especially with Cyclosporine (Immunosuppressant)
  • Hepatotoxicity
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32
Q

What is Caspofungin ONLY approved to treat?

A
  • Aspergillosis
  • In pt’s who failed to respond to Amphotericin B
  • Treats yeast and mold
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33
Q

Caspofungin treats Cryptococcus?

T or F

A
  • False
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34
Q

MOA of Terinafine?

A
  • Inhibitor of squalene epoxidase (Fungus Enzyme)
    1) Accumulation of toxic squalene
    2) Inhibition of ergosterol formation to kill fungi
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35
Q

What antifugal is Keratinophilic, Only builds up in the cells with Keratine?

A
  • Terbinafine (Lamisil)
  • Effective only against Dermatophytes in the
    Nails
    Skin
    Hiar
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36
Q

What does Terbinafine (Lamisil) treat?

A

Dermatophytes

  • Tenia Pedis
  • Athletes Foot
  • Jock itch
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37
Q

T or F

Large doses of Terbinafine can cause Hepatotoxicity ?

A
  • True

- No Drug Drug interacts

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38
Q

Which antifungal would be the best choice for empiric treatment of a life-threatening systemic infection?

A
  • Amphotericin B

- Broadest spectrum of activity

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39
Q

Which antifungal(s) would be the best choice for treatment of Tinea pedis (athlete’s foot)?

A 
- Terbinafine
Topical imidazole (such as miconazole/Micatin®)
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40
Q

Which antifungal(s) would be the best choice for a systemic Candida infection?

A
  • Fluconazole (Cheaper)

- Caspofungin

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41
Q

What does a mosquito bite produce?

A
  • Sporozoites
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42
Q

What does the Exoerythrocytic stage produce?

A

-Sporozoites infecting the liver hepatocytes

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43
Q

Infected hepatocytes are now called ?

A
  • Tissue Schizonts
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44
Q

Infected Hepatocytes rupture and release what?

A
  • Merozoites
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45
Q

What is the Erythrocytic stage?

A
  • Merozoites infecting RBC’s in the blood called now

- Blood Schizonts aka Erythrocytic Schizonts

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46
Q
  • Blood Schizonts aka Erythrocytic Schizonts have two possibilities now, what are they?
A

1) Produce more Blood Schizonts from infected RBC’s

or

2) Produce Gametocytes that can be taken up by mosquitoes

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47
Q

What are the three antimalarial drugs ?

A

1) Liver Schizonticide
2) Blood Schizonticides
3) Gametocides

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48
Q

T or F

A signal agent can eliminate all forms of parasites ?

A
  • False
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49
Q

Where do most antimalarial drugs target?

A
  • Blood Schizonts
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50
Q

Liver Schizonticides act where?

A
  • Act on the RBC’s parasite which are rapidly dividing (Active disease)
  • Where most drugs target
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51
Q

Where do liver Schizonticides act?

A
  • Interfere with production of Merozites
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52
Q

Where do gametocides act?

A
  • Kills gametocytes

or

  • Prevents transmission to mosquito
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53
Q

Most common parasitic Malarial causing organism in humans?

A
  • Plasmodium Faciparum
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54
Q

T or F

Antimalarial drugs can be Chemoprophylaxis or for used for treatment?

A
  • True
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55
Q

T or F

Tonic contains Quinine, and Quinine is an Antimalarial?

A
  • True
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56
Q

Quinine is a rapid acting, highly active schizonticide against all five species, especially for Falciparum Malaria?

T or F

A
  • True, Blood Schizonticide for all five species
  • Gametocidal only against
    P. Vavax
    P. Ovale
  • Not a Liver Schizonticide for any species
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57
Q

What is the definition of Radical Cure?

A
  • CLEARING ALL forms of the parasites to effectively clear the parasites and eradicate the disease
58
Q

What is Quinine, and what is it used for?

A
  • Natural Antimalarial
  • Blood Shizonticide (All 5)
  • Gametocidal (Only P. Vivax & P. Ovale)
  • No Liver Scizonticide activity
59
Q

How do antimalarial agents work?

A
  • Prevention of heme polymerization to kill off erythrocytic parasites
  • Accumulate in food vacuole inside the parasite
  • Have extremely large volumes of distribution
  • Long Half life
60
Q

Most common antimalarial used ?

A
  • Quinine
61
Q

Quinine adverse effects?

A
  • Cinchonism = Poisoning due to excessive ingestion of cinchona alkaloids
S&S of Cinchonism 
Tinnitus
Nausea
Flushing
Visual disturbances
Double vision
62
Q

T or F

Quinine needs to be used with caution in G6PD deficiency?

A
  • True

- Will cause Hemolysis

63
Q

What is Chloroquine ?

A
  • Syn Quinine
64
Q

MOA Chloroquine antimalarial?

A
  • Chloroquine gets protonated inside food vaculole with low ph
  • Prevents biocrystallization of Ferriprotoporphyrin (toxic heme) into Hemozoin (Nontoxic heme)
65
Q

Chloroquine is the drug of choice for treatment of?

A
  • Non Malarial resistance - Treats Non Falciparum Malaria & Falciparum Malaria
66
Q

What causes Falciparum resistance?

A
  • Mutations in transporter of Choloquine

- Mutated PfCRT transporter

67
Q

T or F

Chloroquine can treat liver dormant parasites?

A
  • False

- Only Blood Schizonticide

68
Q

What does the Plasmodium Parasite (Inside RBC) depends on?

A
  • Breakdown of hemoglobin from RBC’s for their amino acids to continue their life cycle
69
Q

What kind of HEME is toxic to Plasmodium?

A
  • Ferriprotoporphyrin Heme
70
Q

What impairs the absorption of Chloroquine?

A
  • Absorption impaired by Ca2+ or Mg2+ containing antacids

- Because its a Phosphate Salt

71
Q

True or False

Cholorquine has a HUGE volume of distribution (70,000 liters)

A
  • True

- All in the food vacule of the plasmodium

72
Q

T or F

Cholorquine has a very long half life?

A
  • Very Slow

- t/12 = 1 to 2 months

73
Q

Common Adverse effects of Cholorquine?

A
  • African descent = Pruritus (itchy skin)

- Hemolysis in G6PD deficiency

74
Q

Chloroquine is contraindicated in what pt conditions?

A
  • Psoriasis (Africans)

- Pt’s predisposed to accumulation of heme or precursors/metabolites (Porphyria)

75
Q

Mefloquine MOA?

A
  • Inhibition of HEME polymerization

- Ferriprotoporphyrin Heme toxic heme builds up

76
Q

Mefloquine is a strong blood schizonticidal agent?

T or F

A
  • True

- Not active against Liver Scizonts or Gametocytes

77
Q

Mefloquine has a long half life?

T or F

A
  • True

- Trapped inside food vacuoles

78
Q

Mefloquine is consider safe for Infants / children and pregnant women?

T or F

A
  • True
79
Q

Mefloquine can be used as a __________ and against _______ diseases?

A
  • Prophylaxis (Once a week)

- Active Malarial diseases (Single Dose)

80
Q

What is the black box warning for Mefloquine?

A
  • Potential Neuropsychiatric reactions

- Manic Monday in the military

81
Q

Mefloquine is contraindicated in ?

A
  • Pt’s with Neuropsychiatric disorders
  • Seizures
  • Psychosis
  • Arrhythmias
82
Q

T of F

Mefloquine is given orally because of severe local skin irritations with IM ?

A
  • True
83
Q

What is the liver enzyme in the liver that process Mefloquine?

A
  • CYP3A4
84
Q

Mefloquine half live is ?

A
  • 3 weeks

- Long half life

85
Q

What is Atovaquone + Proguanil (Malarone) and what are they used for?

A
  • Atovaquone
    Electron transport chain inhibitor
  • Proguanil
    DHFR inhibitor
  • Antimalarial
86
Q

Atovaquone + Proguanil (Malarone) can be used for _____________ and _______________.

A
  • Chemoprophylaxis

- Treatment

87
Q

Why is Atovaquone not used alone but instead in combination with Proquanil?

A
  • Rapid resistance

- Powerful activity in combination

88
Q

What does Proguanil (Prodrug) require?

A
  • CYP3A4 activation into Cycloguanil (DHFR inhibitor)

Dihydrofolate reductase (DHFR) catalyzes the NADPH-dependent reduction of dihydrofolate to tetrahydrofolate

  • Potentiates Atovaquone
89
Q

Atovaquone is low and erratic when given PO, must be given with?

A
  • Fatty food to slow down absorption
90
Q

Atovaquone + Proguanil treats what ?

A
  • Liver Schizonts and Blood Schizonts

- 1 week treatment for Chemoprophylactic treatment

91
Q

Atovaquone is heavily protein-bound causing most drug to remain in what compartment?

A
  • Central compartment (Plasma)
92
Q

What do Plasmodium parasite require?

A
  • ETC to produce ATP

- To maintain mitochondrial membrane potential

93
Q

MOA of Atovaquone ?

A
  • Mimics Ubiquinone in Complex III

aka
- Cytochrome Bc1
- coQ
(Cytochrome C Oxidoreductase)

  • But can not carry electrons
94
Q

Atovaquone can carry electrons ?

T or F

A
  • False
  • Can not carry electrons causing Mitochondrial membrane potential collapse
  • NO ATP = Cell death
95
Q

How does Proguanil help Potentiates Atovaquone ?

A
  • Inhibits DHFR
96
Q

What are some important drug drug interactions with Atovaquone + Proguanil ?

A
  • Plasma concentrations of Atovaquone are reduced by 50% when given with;
  • Tetracycline’s
  • Ripampin
97
Q

What causes Amoebiasis ?

A
  • Entamoeba Histolytica
  • Ingestion of Cyst (Food or Water)
  • Cysts hatch in GI tract and release Amoebas
  • Amoebas divide into Trophozoites
  • Invade other parts of body
98
Q

T or F

Asymptomatic Amoebiasis are not generally treated in Endemic Areas?

A
  • True

- Treated depending on clinical presentation

99
Q

Metronidazole (Flagyl) treats ?

A
  • Protozoa (Amoebas)
    Drug of Choice

&

  • Bacteria
    In anaerobic conditions ONLY
100
Q

Metronidazole (Flagyl) MOA?

A
  • Formation of a nitro radical (Electrophillic) wants to react with (N, Sulfur or O2)
  • Nitro radical causes damage to nucleophilic biomolecules
  • DNA protein thiols (Anaerobic Amoeba)
  • Host is protected by oxygen-mediated radical detoxification
  • Oxygen in host cells absorbs the radical = No damage
101
Q

T or F

Metronidazole (Flagyl) must be adjusted for Liver and Kidney dysfunction?

A
  • True
102
Q

T or F

Mild to Moderate, Severe and Extraintestinal Amoebas infections are all treated the same?

A
  • True
  • Metronidazole (Flagyl)
  • 750 mg 3xd for 10 days
103
Q

What are some common adverse effects of Metronidazole (Flagyl) ?

A
  • Metallic taste
  • Nausea
  • Dry mouth
  • HA
  • Disulfiram Effect
104
Q

The Disulfiram effect that Metronidazole induces is caused by drinking _______ and causes what S&S?

A
  • Alcohol
  • Hot flashes
  • Flushing
  • Lightheaded
  • Increased body temp
  • Due to Increase of Acetaldehyde
    (Toxic by product)
105
Q

What does Metronidazole inhibit in the liver?

A
  • CYP2C9

- Caution with pts taking Warfarin

106
Q

T or F

Metronidazole (Flagyl) is a Teratogen?

A
  • True

- Avoid in pregnancy and nursing

107
Q

What can you substitute Metronidazole for in a Pregnant pt or a pt with Hepatic or Renal Disease to treat Amoebas when there is no other option?

A

Antimicrobial Agents

  • Rifampin
  • Tetracycline
  • Amphotericin B
108
Q

What are the three drugs that treat Helminthic infections in the US?

A
  • Albendazole (Benazoles)
  • Ivermectin ( Avermectins)
  • Praziquantel
109
Q

Albendazole (Benazoles) MOA ?

A
  • Inhibit microtubule polymerization

- Component of the Cytoskeleton

110
Q

Ivermectin ( Avermectins) MOA?

A
  • Agonist of Glutamate - Activated channels that paralyze invertebrates
111
Q
  • Praziquantel
A
  • Causes increased permiability of Helminthic cell membranes to Ca2+
  • Triggering hyperpolarization
  • Subsequent paralysis
112
Q

Dynamic polymerization and Depolymerization allows for cytoskeleton remodeling allows for _________ and controls cell _________.

A
  • Mitosis

- Cells polarity

113
Q

Albendazole is a microtubule destabilizers, they bind where?

A
  • Bind to Colchicine site on Beta Tubulin
  • Prevents polymerization
  • Binds parasite > human tubulin
  • Relatively selective toxic
114
Q

Once Albendazole binds Beta Tubulin in a parasite what happens?

A
  • Disrupts EGG development (Disruption of Spindle)
    No eggs hatching
  • Disrupts polarity of Adult parasite cells

Decreased nutrient glucose uptake
Eventually death

115
Q

T or F

Albendazole leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen stores

A
  • True
116
Q

T or F

Albendazole also prevents the formation of spindle fibers needed for cell division, which in turn blocks egg production and development; existing eggs are prevented from hatching.

A
  • True
117
Q

What other effects does the impairment of Beta Tubulin do to parasites?

A
  • Cell motility
  • Maintenance of cell shape
  • Intracellular transport are also disrupted
118
Q

T or F

Taking Albendazole with a fatty meal increases its absorption?

A
  • True increases PO x 5

- Bad PO absorption

119
Q

Albendazole can reach all tissue to include the CNS

T or F

A
  • True

- Its lipophillic

120
Q

Albendazole is a CYP1A2 inducer and substrate meaning?

A
  • Albendazole is a prodrug that is activated by the liver CYP1A2
  • Its activated into it’s primary active substrate (Active Drug) Albendazole Suloxide
121
Q

What will inhibitors of CYP1A2 do to concentrations of Albendazole in the plasma ?

A
  • Reduce plasma concentrations of its active substrate
  • Decreasing the therapy of the pt
  • Can cause Liver damage
122
Q

What medications will inhibit CYP1A2 decreasing the effects of Albendazole ?

A
  • Phenytoin
  • Dexamethasone
  • Praziquantel
  • Ritonavir
123
Q

T or F

Albendazole should not be given to pt’s with Cirrhosis and if Pregnant ?

A
  • True
124
Q

What must be monitored in pt’s taking Albendazole?

A
  • Blood counts

- LFT’s

125
Q

What is Ivermectin an agonist of?

A
  • Glutamate Gated Chloride Channel (GluCl)

- In invertebrates

126
Q

T or F

Humans have GluCl channels ?

A
  • False

- But Ivermectin has off target affinity to GABAergic receptors

127
Q

What invertebrates have GLucl channels which Ivermectin can target?

A
  • Strongyloidiasis (DOC)
  • Onchocerciasis (River blindness) Kills larva (Microfilaria) NOT ADULT worms
  • Roundworms (Nematodes)
  • Scabies
  • Lice
  • Bed Bugs
  • Fleas
  • Tics
  • Heartworms
128
Q

Ivermectin MOA?

A
  • Forces the opening of GluCl
  • Causes hyperpolarization of nerve and muscle cells
  • Flooding the cells with Chloride
  • leads to paralysis and death for parasites
129
Q

What are the Toxicities of Ivermectin (not produced by the drug)

A
  • Result from rapid killing of microfilariae (larva)

- Due to pt’s having a high parasite burden

130
Q

S&S of the Ivermectin induced toxicity?

A
  • Fever
  • Lymphadenitis
  • Lymphangitis
  • Hypotension
  • Tachycardia
  • Peripheral edema
131
Q

How can you counter the Ivermectin induced toxicity?

A
  • Corticosteroids and Control immune response
132
Q

T or F

Ivermectin is taken on an empty stomach?

A
  • True
133
Q

What are some off target effects (Contraindications) of Ivermectin due to it enhancing its effect?

A
  • Off-target activity against vertebrate GABA channels
  • Contraindicated in pts taking GABA agonists
  • Barbiturates
  • Valium
  • Benzodiazepines
  • Valproic acid (anticonvulsant)
134
Q

Praziquantel is the DOC for ?

A
  • All Schistosome infections (Blood Fluke Trematodes)
  • Effective against Larva and Adult stages
  • Very safe even for children
135
Q

T or F

Praziquantel is very safe and highly effective with just one dose?

A
  • True
136
Q

Praziquantel MOA?

A
  • Causes increased permeability of helminthic cell membranes to Ca2+
  • Triggering hyperpolarization and subsequent paralysis
137
Q

What are the two ways to affect Praziquantel absorption?

A
  • High-Carb meal
    Increases plasma concentrations
  • Antiepileptics
    Decrease bioavailabilty
138
Q

Metabolism of Praziquantel can be affected during first pass because?

A
  • Praziuantel is a CYP3A4 substrate

- Inducers of CYP3A4 are contraindicated, reduces Praziuantel serum concentration

139
Q

What are some CYP3A4 inducers that are contraindicated with Praziquantel CYP3A4 substrate ?

A
  • St. Johns Worth
  • Barbiturates
  • Phenytoin
  • Rifampin
140
Q

T or F

Pts taking Praziquantel can drive very easily after taking medication?

A
  • False
  • Causes drowsiness and dizziness
  • Pts should not drive
141
Q

Adverse side effects of Praziquantel?

A
  • Immune response
  • Results from killing of worms
  • Fever, lymphadenitis, lymphangitis, hypotension, tachycardia, peripheral edema.
142
Q

Praziquantel immune response can be counter with ?

A
  • Corticosteroids

- Even though corticosteroids reduce plasma levels ≈ 50%

Clinical Pharmacology II (5 decks)

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