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(Ch 42) Antifungal Drugs Flashcards

1
Q

What is the structure of a fungus?

A

Fungi are eukaryotic organisms with rigid cell walls that contain chitin as well as polysaccharides.

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2
Q

What is a mycosis?

A

Fungal infection which can be divided into

three groups:

  • systemic mycoses,*
  • subcutaneous mycoses,*
  • superficial mycoses.*
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3
Q

Name seven drugs used for

systemic and subcutaneous mycoses.

A
  1. Amphotericin B (Fungizone)
  2. Flucytosine (Ancobon)
  3. Ketoconazole (Nizoral)
  4. Fluconazole (Diflucan)
  5. Itraconazole (Sporanox)
  6. Voriconazole (VFEND)
  7. Caspofungin (Cancidas)
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4
Q

Name the 5 different

CLASSIFICATION OF ANTIFUNGAL DRUGS

A
  1. Polyene Antibiotics
  2. Azole Derivatives
  3. Allylamine Drugs
  4. Echinocandin Drugs
  5. Other Antifungal Drugs
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5
Q

Name all

Polyene Antibiotics

A

Amphotericin B

(ABELCET, AMBISOME, AMPHOTEC)

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6
Q

Name all 6

Azole Derivatives:

A
  1. Clotrimazole (GYNE-LOTRIMIN, MYCELEX)b
  2. Fluconazole (DIFLUCAN)
  3. traconazole (SPORANOX)
  4. Ketoconazole (NIZORAL)
  5. Voriconazole (VFEND)
  6. Posaconazole (NOXAFIL)
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7
Q

Name all

Allylamine Drugs

A

• Terbinafine (LAMISIL)c

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8
Q

Name all

Echinocandin Drugs

A

• Caspofungin (CANCIDAS)d

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9
Q

Name all

“Other Antifungal Drugs”

A
  1. Ciclopirox (LOPROX)
  2. Flucytosine (ANCOBON)
  3. Griseofulvin (GRIS-PEG)
  4. Tolnaftate (TINACTIN)
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10
Q

Systemic mycoses

can cause?

A

Systemic mycoses can cause

signs and symptoms of:

soft tissue infection, urinary tract infection, pneumonia, meningitis, or septicemia

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11
Q

The systemic mycoses are most commonly caused by members of the genera?

A

Aspergillus

Blastomyces

Candida

Coccidioides

Cryptococcus

Histoplasma

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12
Q

Echinocandin Drugs

What is the MOA

Ex. of the drug

A

Cyclic hexapeptide compounds that inhibit

fungal cell wall sysntesis

ex: Caspofungin

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13
Q

AMPHOTERICIN B

What is the classification of this drug?

A

Amphotericin B is a

polyene antibiotic

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14
Q

AMPHOTERICIN B

What is its importance?

A

It is the drug of choice for treating many

systemic mycotic infections.

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15
Q
  • Provide examples of*
  • Systemc mycotic infections:*
A

signs and symptoms of soft tissue infection:

urinary tract infection

pneumonia

meningitis

septicemia

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16
Q

Amphotericin B

How does this drug work?

A

Fungal cells contain ergosterol, a sterol specific to fungal cell membranes.

Amphotericin B binds to ergosterol* and *forms pores or channels within the membrane.

This allows electrolytes to leak from the cell*, which *results in cell death

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17
Q

Does amphotericin B bind to

cholesterol?

A

No.

Only ergosterol is affected by this drug.

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18
Q

Does amphotericin B enter the

CNS?

A

No

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19
Q

Amphotericin B

What is this drug’s antifungal spectrum?

A

Amphotericin B is effective against a broad spectrum of organisms including:

Candida
Histoplasma capsulatum

Cryptococcus neoformans

Blastomyces dermatitidis

Aspergillus
Coccidioides immitis

Mucormycosis

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20
Q

Amphotericin B

What is the route of administration?

A

Usually IV;

however, for fungal meningitis:

intrathecal (inject into spinal cord) administration is required.

-A topical form of amphotericin B also exists.

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21
Q

Amphotericin B

What are its pharmacokinetics?

A

Amphotericin B is poorly absorbed from the gastrointestinal tract.

Bile is the major route of excretion. A small part of the drug, however, is eliminated in the urine.

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22
Q
  • Amphotericin B*
  • How does resistance occur?*
A

ergosterol is replaced with other precursor sterols

for the cell membrane.

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23
Q

Amphotericin B

What are adverse signs to watch for during administration?

A
  1. Renal impairment—80% of patients exhibit a decreased glomerular filtration rat*_e and _*changes in renal tubular function.
  2. This drug can cause a renal tubular acidosis.
  3. Newer liposomal formulations of amphotericin B can help reduce the renal toxicity.
  4. Hypotension
  5. Fever, chills (“shake and bake” syndrome)
  6. Hypochromic normocytic anemia
  7. Neurological effects
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24
Q

FLUCYTOSINE

What type of drug is flucytosine?

A

A synthetic pyrimidine antimetabolite.

It is related in structure to an anticancer drug called 5-fluorouracil (5-FU).

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25
Flucytosine When is it used?
Flucytosine is used *_predominantly in conjunctio_*n with ***amphotericin B*** or ***itraconazole***
26
*_Flucytosine_* *_How does flucytosine work?_*
It enters fungal cells through a ***_cytosine- specific permease_*** and ***_is first converted to 5-FU_***. Subsequently, it is *_converted_* to ***5- fluorodeoxyuridine monophosphate (5- FdUMP***). This *_acid inhibits_* ***thymidylate synthetase***, which is an *essential enzyme* in the *_production of DNA_* . ***NOTE:*** Mammalian cells *_do not convert_* *flucytosine to 5-FU* and therefore are *not affected.*
27
***Flucytosine*** Is its antifungal spectrum broad or narrow?
***Narrow;*** it affects *_only the following:_* ***Candida Cryptococcus neoformans*** *_Agents_* causing ***chromomycosis***
28
How is *flucytosine* usually _administered_?
PO
29
What are the pharmacokinetics of flucytosine?
Flucytosine *_distributes well throughout the tissues*_, including the _*cerebrospinal fluid (CSF)_*. It is *_excreted intac_*t in the ***urine.***
30
***Flucytosine*** *What are the toxicities of this drug?*
***1. Hematological***—reversible bone marrow depression leading to neutropenia and thrombocytopenia 2. ***Elevated hepatic enzymes*** 3. ***Gastrointestinal disturbances***—nausea, vomiting, severe enterocolitis
31
***Ketokonazole*** ***Into what category does this drug fit?***
*Ketoconazole* is the *_prototypical azole*_ used for _*systemic mycoses_*. Other drugs in this category include: ***fluconazole, itraconazole, and voriconazole***. They all have the *_same mechanism of action_* but *_different therapeutic indications*_ and _*pharmacokinetics_*. Their development _provided a way to treat_ ***systemic infections orally.***
32
* Ketokonazole* * azoles MOA?*
They ***block cytochrome P-450***–mediated *lanosterol demethylation to ergosterol*. The *_specific enzyme_* that is _blocked_ is called ***C-14-α demethylase.***
33
What is *ketoconazole’s* spectrum?
It is useful and *mostly used* as a *_second line agent against_* ***Histoplasma, Candida, Cryptococcus, Blastomyces, and dermatophytes***. It has largely been *_replaced by_* ***itraconazole*** for the *_treatment of all_* ***mycoses*** because of *_increased effectiveness and reduced toxicities._*
34
**ketoconazole’s** How is this drug administered?
***PO -ONLY***
35
Ketoconazole * What are its pharmacokinetics?* * Name 2 drugs that impair its absorption.*
*Ketoconazole* *_depends on gastric acidity_* to be *_dissolved and absorbed_*; drugs such as ***cimetidine*** and ***antacids*** *_impair_* its *_absorption_*. Ketoconazole is _*metabolized in the **liver***_ and e*_xcreted through the **bile.**_*
36
What are ketoconazole’s major toxicities?
***-Gynecomastia*** and ***decreased libido*** due to *_inhibition of testosterone*_ and _*cortisol synthesis_* -***GI distress***—*nausea, vomiting* ***-Hepatic dysfunction***—*inhibits cytochrome P-450 system* ***-Allergies***
37
***Ketaconazole*** *State _contraindications_ to the use of this drug*
***_Never_*** use ***ketoconazole*** and ***amphotericin B*** *_together_* —*they antagonize each other’s actions*.
38
***Fluconazole*** What are the *major advantage*s of *_fluconazol*_e over _*ketoconazole_*?
***Fluconazole*** *_can enter the CSF in high concentrations*_ and _*is not dependent_* on ***acidic pH*** _for absorption._ It also *_does not caus_*e the ***endocrine dysfunction*** seen with ***ketoconazole***.
39
What are the therapeutic uses of *_fluconazole?_*
*_-Disseminated_* or *_progressive coccidioida_*l *infections such as **meningitis**—**(drug of choice)*** ## Footnote *_-Disseminated histoplasmosis_ Oral, esophageal, and vaginal candidiasis.* * -_Candidemia_ of the nonimmunosuppressed patient.* * -_Prophylaxis_ of **cryptococcal meningitis** in AIDS patients whose infection has been controlled by _amphotericin B_*
40
***Ketoconazole*** How is it administered and excreted?
***Orally** or **IV*** *_Eliminated_ through the* ***kidneys.***
41
*What t**_oxicities_** are associated with* *_Fluconazole_*?
Can *_inhibit the cytochrome P450 system_* responsible for the *metabolism of several other drugs* such as ***cyclosporine, warfarin, and phenytoin*** *Similar to most azoles*, ***do not administer to pregnant women.***
42
43
ITRACONAZOLE What is itraconazole’s therapeutic use?
Itraconazole is the *drug of choice* for *_patients with indolent nonmeningeal infections_* of: ***blastomycosis, histoplasmosis, coccidioidomycosis*** *and* ***cutaneous sporotrichosis.***
44
ITRACONAZOLE Is it effective in *_CNS infections_*?
***No,*** it *does not easily penetrate the* ***blood- brain barrier*.**
45
ITRACONAZOLE How can this drug be *administered*?
***IV*** or ***oral***
46
ITRACONAZOLE Where is it metabolized?
In the ***liver***. ## Footnote *It is a _potent inhibitor_ of the* ***cytochrome P450 system.***
47
What are the adverse effects of ***itraconazole***?
* GI distress, hypertriglyceridemia, rash, hypokalemia, hypertension, and hepatotoxicity.* * It _does not have_ the **endocrinological side effects** of **ketoconazole.***
48
VORICONAZOLE When is ***voriconazole*** used?
This is *one of the newer azoles* with a ***broader spectrum*** than its predecessors. Currently it is *reserved for use* in: *_invasive Aspergillosis,_* *_life-threatening infections with Fusarium_* *_or_* *_Scedosporium apiospermum._*
49
VORICONAZOLE How is it administered?
Oral or IV
50
VORICONAZOLE How is it metabolized?
Through the ***cytochrome P450 system***. Drugs that *_induce*_ or _*inhibit that system*_ can _*cause dramatic changes in plasma concentrations of voriconazole_*. *_Coadministration_* of ***rifampin*** or ***rifabutin*** is ***_contraindicated_*** because of *_increased_ **voriconazole metabolism.***
51
VORICONAZOLE What are its Adverse effects?
*_Transient blurred vision_ or _color perception_ has been reported shortly after administration.* *_Hepatotoxicity_ occurs occasionally.* *_Rash_*
52
CASPOFUNGIN What is it?
This drug is the *_prototype of a class_* of ***antifungals*** called ***echinocandins***.
53
CASPOFUNGIN ## Footnote ***MOA***
It *_inhibits cell wall synthesis_* by *_blocking_* the ***formation of β(1,3)-D-glucan.***
54
CASPOFUNGIN Administration?
***IV- Only***
55
CASPOFUNGIN USE:
*_Invasive Aspergillus infections_* for patients who have *_failed therapy_* with other agents such as ***amphotericin B*** or ***Voriconazole***.
56
Caspofungin *any adverse effects?*
***Yes*** *_phlebitis_* at the *injection site* and *_flushing_ from histamine release*
57
* Identify _six major drugs_* * used to treat* *_superficial mycotic_ infections*
1. Griseofulvin(Fulvicin) 2. Nystatin(Mycostatin) 3. Miconazole(Monistat) 4. Clotrimazole(Canestencream) 5. Econazole(Spectazole) 6. Terbinafine(Limisil)
58
GRISEOFULVIN *What is its mode of action?*
Griseofulvin *enters susceptible fungal cells* and *_inhibits_* ***microtubule function***. With *_long-term therapy (weeks to months),_* this drug *_accumulates_ in the newly synthesized stratum corneum, making these cells undesirable for fungal growth.*
59
GRISEOFULVIN What is the antifungal spectrum of this drug?
It is ***effective*** ***only*** *against* *_dermatophytes,_* including ***Trichophyton, Microsporum, and Epidermophyton***. ***Griseofulvin*** has largely *_been replaced_* by ***terbinafine*** because it *_requires 6 to 9 months of therapy and is more toxic._*
60
GRISEOFULVIN What are the *pharmacokinetics* of this drug?
Griseofulvin is *_absorbed well orally_*, especially with a *_high-fat diet_*, and *_distributed to the keratin-containing_* ***stratum corneum.*** It is *eliminated through the **bile.***
61
GRISEOFULVIN State this drug’s *adverse effects.*
*Headache Hepatotoxicity GI irritation Rarely teratogenic or carcinogenic*
62
NYSTATIN What is the structure of drug?
Nystatin is a ***polyene*** *s_imilar in structure_* to ***amphotericin B***, with the *_same mechanism of action_*. ***It creates pores in the cell membrane of the fungi.***
63
NYSTATIN What is the route of administration?
*Topical for _skin_* and *_mucocutaneous infections_* or *_oral for **thrush**_* ***Note:** Thrush, 0ral candidiasis, is a yeast/fungi infection of the genus Candida that develops on the mucous membranes of the mouth.* *happens most often to toddlers and children but can affect anyone. Antifungal medications, which are generally taken for 10 to 14 days, to treat thrush*
64
NYSTATIN What is nystatin’s therapeutic use?
*Treatment of superficial Candida infections*
65
NYSTATIN What are its adverse effects?
***Bitter taste*** ***nausea***
66
Miconazole-Clotrimazole-Econazole ROA?
***Topical.*** *They are _highly toxic if used systemically._*
67
Miconazole-Clotrimazole-Econazole Are other ***azole drugs*** *used topically?*
***Yes.*** ***Terconazole*** and ***butoconazole*** are two of the *more recently developed drugs,* but *they are all very similar drugs.*
68
Miconazole-Clotrimazole-Econazole What are the indications for use?
*_Superficial infections of the skin_* and *_mucous membranes (vulvovaginitis_*). ## Footnote *_Effective against_ **Candida** and **dermatophytoses***
69
Miconazole-Clotrimazole-Econazole * What are the pharmacological properties* * of these drugs?*
*They are very similar to **ketoconazole** in mechanism of action and spectrum.*
70
Miconazole-Clotrimazole-Econazole *What are the side effects?*
Since they are ***only given topicall***y the *most common adverse effects include* ## Footnote *_itching, erythema, and burning._*
71
TERBINAFINE What is it used for?
Terbinafine is a ***first-line agent*** *used to _treat dermatophyte infections_,* ## Footnote *especially **onychomycosis***
72
TERBINAFINE *What is its route of administration?*
Although it is used to ***treat superficial infections***, it is *given* ***orally*** *or* ***topically***
73
***Terbinafine*** How does it work?
*_Inhibits_ an enzyme* ***(squalene epoxidase***) used to *_synthesize ergostero_*l. ## Footnote ***Accumulation of squalene is toxic to fungi***
74
Terbinafine ***What are the toxic effects?***
* Rash, headache and GI irritation.* * Rarely* *_hepatotoxicity and neutropenia_* may occur. The drug is ***contraindicated in pregnancy.***
75

(MUL) Pharmacology (18 decks)

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