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Pharmacology > Antifungals > Flashcards

Antifungals Flashcards

1
Q

What are fungal infections

A

They are slow growing, difficult to treat infections

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2
Q

Where do fungal infections occur

A

In devitalized or avascular tissues such as the skin, nails, hair, etc.

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3
Q

What kind of treatment do fungal infections require?

A

They require prolonged treatment

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4
Q

Which are the Superficial Fungal infections

A

Dermatomycoses: ring worm species
Candidiasis: mucous membrane infections

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5
Q

Examples of Dermatomycoses

A

Tinea Pedis: athletes foot
Tinea corporis: body
Tinea Cruris: groin
Tinea Capitis: scalp
Tinea Unguium: nalis

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6
Q

Places where Candidiasis occur

A

Skin
Mouth: thrush
Vagina

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7
Q

Which are the Systemic Fungal Infections?

A

Systemic Candidiasis
Cryptococcosis: meningitis
Systemic Aspergillosis: respiratory issues in Immunocompromised patients
Blastomycosis: lung infection
Histoplasmosis: lung infection
Emergomycosis: found in immunocompromised patients

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8
Q

Which are the Systemic Antifungals

A

Amphotericin B
Azoles
Echinocandins
Griseofulvin
Terbinafine

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9
Q

Which are the Topical Antifungals

A

Terbinafine
Nystatin
Clotrimazole
Miconazole
Ketoconazole
Econazole

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10
Q

What is Amphotericin B

A

Its a very toxic systemic antifungal with a broad spectrum pof activity

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11
Q

Indications of Amphotericin B

A

Disseminated Candidiasis
Cryptococcosis
Murcomycosis
Histoplasmosis
Blastomycosis
Aspergillus
Emergomycosis
Sporotrichiosis

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12
Q

MOA of Amphotericin B

A

it binds to ergosterol thus altering the permeability of fungal cell by forming pores in the cell membrane–> allows for leakage of cell contents–> interferes with fungal integrity= Fungal Death

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13
Q

Admin of Amphotericin B

A

IV as its absorption from GI tract is negligible

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14
Q

What else can Amphotericin B be used as?

A

as local antifungal for fungi within the lumen of GI tract

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15
Q

Amphotericin B is DOC for

A

most serious systemic infections

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16
Q

How is Amphotericin B used

A

Used as induction therapy than its replaced by the newer azole once fungal burden has been reduced

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17
Q

Elimination of Amphotericin B

A

its eliminated slowly–> over several day period

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18
Q

AEs of Amphotericin B due to Infusion rxns

A

fever
chills
headache
myalgia
NV
Hypotension

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19
Q

AEs of Amphotericin B due to Cumulative Toxicity

A

NEPHROTOXIC
Renal impairment: pre-renal injury, renal tubular acidosis
Renal Tubular acidosis: K and Mg wasting
Anemia: decr. EPO production due to damaged renal cells
Abnormalities in liver function seen

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20
Q

DIs of Amphotericin B

A

Aminoglycosides, Tenofovir, Cyclosporine
Diuretics: worsen Hypokalemia
Digoxin: hypokalemia may worsen Digoxin toxicity

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21
Q

Which are the Azoles used in Fungal infections

A

Imidazoles: topical use
Triazole: systemic use

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22
Q

Name the Imidazoles

A

Ketoconazole
Miconazole
Clotrimazole

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23
Q

Name the Triazoles

A

Itraconazole
Fluconazole
Voriconazole
Posaconazole

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24
Q

Indications of the Azoles

A

Broad spectrum of activity against Dermatophytes and Invasive yeast infections like the Candidiasis and Cryptococcus

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25
Q

MOA of Azoles

A

Inhibit fungal CYP450(14-demethylase) enzymes leading to a reduction in Ergosterol synthesis

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26
Q

Which azoles are more selective

A

Triazoles are more selective than Imidazoles–> Imidazoles have incr. incidence of AEs

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27
Q

AEs of Azoles

A

Hepatotoxicity
NV
Diarrhea
Headache
SKin rash

28
Q

DIs of Azoles

A

Azoles inhibit CYP450=incr. serum conc. of co-administered drugs

29
Q

CIs of Azoles

A

Pregnancy as its Teratogenic
Lactation as its excreted in breast milk

30
Q

Exception to CIs of Azoles

A

females who are at term and have severe vaginal Candidiasis

31
Q

Indication of Voriconazole

A

DOC: Invasive Aspergillosis
Candida spp.: serious ones resistant to fluconazole
Oropharyngeal and Oseophageal Candidiasis

32
Q

AEs of Voriconazole

A

Visual disturbances
Photosensitivity Dermatitis(chronic oral)
Toxicity: rash and raised hepatic enzymes

33
Q

Is Voriconazole effective against UTIs

A

No, as its excreted as an inactive metabolite in the urine

34
Q

Indications of Fluconazole

A

Vaginal and Oropharyngeal Candidiasis not responding to topical treatment
Oesophageal and systemic Candidiasis
Cryptococcal Meningities

35
Q

Fluconazole is administered to whom

A

As prophylaxis to immunocompromised patients to reduce fungal infections
*bone marrow transplant, AIDs patients

36
Q

Effect of Fluconazole on Hepatic Enzymes

A

has the least effect on heaptic enzymes –> less DIs’

37
Q

Indications of Itraconazole

A

Dermatophytosis: tenia species
Onchomychosis: nail infections
Azole of choice in: dimorphic fungi infections
Candidaisis not responding to conventional treatment
Alternative therapy for Aspergillosis not responding to standard therapy

38
Q

Admin of Itraconazole

A

Orally via capsule: absorption incr. by food and low gastric pH
Oral solution preferred in Oropharyngeal/Oesophageal candidiasis

39
Q

DIs of Itraconzaole

A

Avoid antacids as they increase gastric pH–> decr absorption of drug

40
Q

Indications of Posaconazole

A

Most Candida: alternate agent in Oropharyngeal/Oesophageal candidiasis
Aspergillosis: alternative
Murcomycosis

41
Q

Admin of Posaconazole

A

Oral suspension
*fatty meal incr. its absorption

42
Q

Which are the Echinocandins

A

Caspofungin
Anidulafungin
Micafungin

43
Q

MOA of Echinocandins

A

specifically inhibit D-glucan synthesis which is essential to fungal cell wall integrity–> compromises integrity of cell–> cell wall becomes permeable= cell lysis

44
Q

Indications of Caspofungin

A

Candidiasis: invasive O+O
Aspergillus: salvage therapy
Empiric therapy for febril Neutropenia

45
Q

SEs of Caspofungin

A

minor GIT SEs
Flushing

46
Q

Admin of Caspofungin

A

IV ONLY

47
Q

Indications of Micafungin and Anidulafungin

A

Systemic invasive Candidiasis infections

48
Q

MOA of Griseofulvin

A

inhibits fungal mitosis

49
Q

Indications of Griseofulvin

A

limited to Dermatophytic infections of skin, nail and hair
Fungistatic
*not active against Candidia

50
Q

Admin of Griseofulvin

A

Oral
*absorption incr. by fatty food
*avoid mil

51
Q

AEs of Griseofulvin

A

Headaches
Skin Rashes
Altered taste sensation
Dry mouth

52
Q

Griseofulvin have largely been replace by

A

Itraconazole+Terbinafine for systemic treatment of Dermatophytosis

53
Q

MOA of Terbinafine

A

inhibits Squalene Epoxidase which prevents Ergosterol synthesis

54
Q

Indications of Terbinafine

A

Superficial Dermatophytosis of skin, nail and hair
Candida albicans

55
Q

PK of Terbinafine

A

highly lipophilic–> distributes preferentially to hair, skin, nail bed
Fungicidal
Keratophilic

56
Q

Admin of Terbinafine

A

Oral: for 12wks=cures 90% of onychomycosis (more effective than Griseofulvin or Itraconazole)
Topical

57
Q

AEs of Terbinafine

A

GIT upset
Headache
Skin rxns
Arthralgia
Taste disturbances
Hepatotoxicity

58
Q

Indications of Nystatin

A

Oropharyngeal thrush
Vaginal Candidiasis
Intertriginous Candidal infections
*not effective aginst Dermatophyte skin infecrions

59
Q

Admin of Nystatin

A

Cutaneous cream/ointment
Vagina: vaginal tablets
Topical oral suspension: has local or topical effect as its not ansorbed systemically

60
Q

Who can use Nystatin be used in

A

Infants as topical suspension for oral thrush on tongue upper palate
Patients with dentures

61
Q

Indications of Clotrimazole and Miconazole

A

Vulvovaginal Candidiasis
Dermatophytic infections including Tenia species
Oral Candidiasis

62
Q

Topical Antifungals indicated for Dermatophytosis (any tinea)

A

MECK: Cream
Clotrimazole
Econazole
Miconazole
Ketoconazole

63
Q

Topical Antifungals indicated for Vaginal Candidiasis

A

MEC: vaginal cream/tablet
Clotrimazole
Econazole
Miconazole

64
Q

Topical Antifungals indicated for Oral candidasis (oral thrush)

A

MC
Miconazole: oral gel
Clotrimazole: lozenge

65
Q

Topical Antifungals indicated for Pityriasis Versicolor

A

Ketoconazole: shampoo

66
Q

Topical Antifungals indicated for Seborrheic Dermititis

A

Ketoconazole: shampoo

Pharmacology (50 decks)

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