Antifungal Drugs: Anti-Infectives and Anti-Inflammatory: Ncm106 - Pharmacology 2 Semester, AY 2020-2021

ANTI-INFECTIVES AND ANTI-INFLAMMATORY:
ANTIFUNGAL DRUGS
NCM106 – PHARMACOLOGY
2ND Semester, AY 2020-2021
Prepared By:
Kandy Anne C. Abuan, MSN
Learning Objectives
At the end of the session, the students will be able to:
1.Discuss the mechanism of action, pharmacokinetics, and pharmacodynamics of
each drug classification, such as:
- Antibacterial
- Antiviral
- Antitubercular
- Antifungal
- Antimalarial, Antiprotozoal, Antihelmintic
- Antiseptic and Disinfectant Agents
- Anti-Inflammatory, Antirheumatic
2.Understand the side and adverse effects of this drugs
3.Identify nursing responsibilities in administering this drugs 2
Antifungal Drugs
 Polyenes
 Flucytosine
 Ketoconazole
 Synthetic Triazoles
 Glucan Synthesis Inhibitors
3
I. Polyenes
 The polyenes include amphotericin B and

nystatin.
 The potency of amphotericin B has made it the
most widely used antifungal drug for severe
systemic fungal infections.
 Nystatin is used only topically or orally to treat
local fungal infections. 4
I. Polyenes
 Amphotericin B is usually administered to

treat severe systemic fungal infections and
meningitis.
 It’s never used for non-invasive forms of
fungal disease because it’s highly toxic.
5
I. Polyenes
Pharmacokinetics
 After IV administration, amphotericin B
is distributed throughout the body and
excreted by the kidneys.
 Oral nystatin undergoes little or no
absorption, distribution, or metabolism. 6
I. Polyenes
Pharmacodynamics
 Amphotericin B
- usually acts as a fungistatic drug
- can become fungicidal if it reaches
high concentrations in the fungi
7
I. Polyenes
Drug Interaction Adverse Reaction
 Amphotericin B when taken with
 Chills
aminoglycosides, cyclosporine, or
acyclovir  Fever
 Corticosteroids, extended-
spectrum penicillins, and digoxin  Nausea and Vomiting
 Amphotericin with digoxin or  Anorexia
thiazide diuretics
 Saline Solution and Electrolyte  Muscle and Joint pain
solutions
 Indigestion 8
I. Polyenes
Nursing Responsibilities
1. Monitor the patient’s pulse, respiratory rate, temperature, and blood
pressure every 30 minutes for at least 4 hours after giving the drug IV
2. Monitor BUN, creatinine (or creatinine clearance), and electrolyte
levels; CBC; and liver function test results at least weekly.
3. Monitor for rhinocerebral phycomycosis, especially in a patient with
uncontrolled diabetes. Leukoencephalopathy may also occur.
4. Monitor pulmonary function.
9
II. Flucystosine
 The only antimetabolite that acts as an

antifungal.
 Flucytosine is a purine and pyrimidine
inhibitor.
 used primarily with another antifungal drug
such as amphotericin B to treat systemic fungal
infections. 10
II. Flucystosine
Pharmacokinetics
 After oral administration, flucytosine is
well absorbed from the GI tract and
widely distributed.
 It undergoes little metabolism and is
excreted primarily by the kidneys. 11
II. Flucystosine
Pharmacodynamics
 Penetrates fungal cells, where

it’s converted to its active
metabolite, fluorouracil.
12
II. Flucystosine
 Cytarabine (may antagonize the  Confusion  Rash
antifungal activity of flucytosine,  Headache  Nausea and
possibly by competitive  Drowsiness vomiting
inhibition)
 Vertigo  Abdominal
Distention
 Hematologic, kidney, and liver  Hallucinations
function (must be closely
 Difficulty
 Diarrhea
monitored during flucytosine breathing  Anorexia
therapy because of the drug’s
 Respiratory arrest
serious risk of toxicity) 13
II. Flucystosine
1. Monitor the patient for adverse CNS reactions.
2. Monitor blood and liver and renal function studies frequently
3. If possible, regularly perform blood level assays of the drug to
maintain flucytosine at therapeutic levels (25 to 120 mcg/mL).
4. Monitor the patient’s hydration status if adverse GI reactions
occur.
14
III. Ketoconazole
 A synthetic imidazole derivative, is an

effective oral antifungal drug with a broad
spectrum of activity.
 Used to treat topical and systemic infections
caused by susceptible fungi, which include
dermatophytes and most other fungi.
15
III. Ketoconazole
Pharmacokinetics
 When given orally, ketoconazole is
absorbed variably and distributed
widely.
 It undergoes extensive liver metabolism
and is excreted in bile and feces. 16
III. Ketoconazole
Pharmacodynamics
 Within the fungal cells, interferes with
sterol synthesis, damaging the cell
membrane and increasing its permeability.
 This leads to a loss of essential intracellular
elements and inhibition of cell growth.
17
III. Ketoconazole
 Ketoconazole use with drugs that  Anaphylaxis
decrease gastric acidity  Joint pain
 Phenytoin with ketoconazole  Chills
 Theophylline with ketoconazole  Fever
 Ketoconazole with cyclosporine  Tinnitus
 Ketoconazole with  Impotence
anticoagulants  Photophobia
 Hepatotoxicity
18
III. Ketoconazole
1. Assess the patient’s fungal infection before therapy and regularly
throughout therapy.
2. Assess for adverse reactions and drug interactions.
3. Risk of serious hepatotoxicity: The drug shouldn’t be used for fungal
infections of the skin or nails.
4. To minimize nausea, divide the daily amount into two doses and give
the drug with meals.
5. Monitor the patient’s hydration status if adverse GI reactions occur. 19
IV. Synthetic Triazoles
 The synthetic triazoles treat various infections:

 Fluconazole
- used to treat mouth, throat, and esophageal candidiasis and
serious systemic candidal infections.
- It’s also used to treat cryptococcal meningitis.
 Itraconazole
- used to treat blastomycosis, nonmeningeal histoplasmosis,
candidiasis, aspergillosis, and fungal nail disease. 20
 The synthetic triazoles treat various infections:

 Voriconazole
- used to treat invasive aspergillosis and serious fungal infections
 Posaconazole
- used as prophylaxis against invasive Aspergillus and Candida in
high-risk patients.
- It is also used for the treatment of oropharyngeal candidiasis.
21
Pharmacokinetics
 After oral administration, fluconazole is about 90%
absorbed.
 It’s distributed into all body fluids, and more than
80% of the drug is excreted unchanged in urine.
 Oral bioavailability is greatest for itraconazole and
posaconazole when they are taken with food.
22
Pharmacodynamics
 Interfere with fungal cell wall synthesis

by inhibiting the formation of ergosterol
and increasing cell wall permeability,
making the fungus susceptible to
osmotic instability. 23
Drug Interaction
 Warfarin (increase the risk of bleeding)
 Fluconazole with oral antidiabetic (may increase the
plasma concentration of oral antidiabetic drugs)
 Rifampin and cimetidine (enhance the metabolism of
fluconazole, reducing its plasma level)
24
Adverse Reactions
 Adverse reactions to fluconazole,
 Adverse reactions to
voriconazole, and posaconazole include:
itraconazole include:
a. Abdominal pain
b. Diarrhea a. Dizziness
c. Dizziness b. Headache
d. Headache
c. Hypertension
e. Increase in liver enzymes
f. Nausea and vomiting d. Impaired liver function
g. Rash e. Nausea
25
1. Assess the patient’s fungal infection before therapy and
regularly throughout therapy.
2. Periodically monitor liver function during prolonged
therapy.
3. Assess for adverse reactions and drug interactions.
4. Assess the patient’s and family’s knowledge of drug
therapy. 26
V. Glucan Synthesis Inhibitor
 Drugs in the class Glucan Synthesis

Inhibitors:
a. Caspofungin acetate (Cancidas)
b. Anidulafungin (Eraxis)
c. Micafungin (Mycamine) 27
Pharmacokinetics
 These drugs are given IV and are highly
protein-bound, with little distribution
into RBCs.
 They are slowly metabolized and
excreted in urine and feces. 28
Pharmacodynamics
 Caspofungin, anidulafungin, and

micafungin inhibit the synthesis of
beta (1,3)-Dglucan, an enzyme
present in fungal cells.
29
Drug Interaction
 Patients taking Caspofungin and Tacrolimus (may
need higher doses of tacrolimus because caspofungin
decreases the blood tacrolimus level)
 These drugs should not be given to anyone with a
known hypersensitivity to any glucan synthesis
inhibitors.
30
Adverse Reactions
 Adverse reactions common  Additional adverse reactions
to the group include: specific to caspofungin
include:
a. Nausea
a. Paresthesia
b. Vomiting
b. Tachycardia
c. Diarrhea
c. Tachypnea
d. Pyrexia d. Rash
e. Facial swelling 31
1. Assess the patient’s hepatic function before starting drug therapy.
2. Observe the patient for histamine-mediated reactions (rash, facial
swelling, pruritus, sensation of warmth).
3. Monitor the patient’s laboratory test results carefully for an
increase in liver function test values.
4. Keep in mind that the dosage may need to be adjusted if the patient
has hepatic insufficiency.
32
REFERENCES
Burchum, J., & Rosenthal, L. (2014). Lehne's Pharmacology for Nursing

Care-E-Book. Elsevier Health Sciences.
Scott, W. N., & McGrath, D. (2008). Nursing Pharmacology Made

Incredibly Easy!. Lippincott Williams & Wilkins.
Zerwekh, J. (2018). Mosby's Pharmacology Memory NoteCards-E-Book:

Visual, Mnemonic, and Memory Aids for Nurses. Elsevier Health
Sciences.
33

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ANTI-INFECTIVES AND ANTI-INFLAMMATORY:

 The polyenes include amphotericin B and

 Amphotericin B is usually administered to

 The only antimetabolite that acts as an

 Penetrates fungal cells, where

 A synthetic imidazole derivative, is an

 Theophylline with ketoconazole  Fever

 Ketoconazole with cyclosporine  Tinnitus

 Ketoconazole with  Impotence

 The synthetic triazoles treat various infections:

 The synthetic triazoles treat various infections:

 Interfere with fungal cell wall synthesis

 Drugs in the class Glucan Synthesis

 Caspofungin, anidulafungin, and

Burchum, J., & Rosenthal, L. (2014). Lehne's Pharmacology for Nursing

Scott, W. N., & McGrath, D. (2008). Nursing Pharmacology Made

Zerwekh, J. (2018). Mosby's Pharmacology Memory NoteCards-E-Book:

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