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CHAPTER 11 - Antifungal ○ Key Point: Has good CNS

penetration, making it
Agents effective for fungal
meningitis.
Key Terms 2. Isavuconazonium:
○ Indication: Broad-spectrum
azoles: a group of drugs used to treat antifungal, especially used
fungal infections. for invasive aspergillosis and
Candida: fungus that is normally found on mucormycosis.
mucous membranes; can cause yeast ○ Key Point: Prodrug that
infections or thrush of the gastrointestinal converts to isavuconazole in
(GI) tract and vagina in immunosuppressed the body.
patients. 3. Itraconazole:
ergosterol: steroid-type protein found in the ○ Indication: Effective against
cell membrane of fungi; similar in onychomycosis, systemic
configuration to adrenal hormones and mycoses.
testosterone. ○ Key Point: Avoid in patients
fungus: a cellular organism with a hard cell with heart failure due to risk
wall that contains chitin and many of negative inotropic effects.
polysaccharides, as well as a cell 4. Ketoconazole:
membrane that contains ergosterols. ○ Indication: Less common for
mycosis: disease caused by a fungus. systemic use due to side
tinea: fungus called ringworm that causes effects; used topically for
infections such as athlete’s foot, jock itch, dermatologic infections.
and others. ○ Key Point: Can affect
—------------------------------------------------------- hormone production, leading
to adrenal insufficiency or
Systemic Antifungals gynecomastia.
5. Posaconazole:
Azole Antifungals ○ Indication: Prophylaxis and
treatment of invasive fungal
● General Info: Azoles disrupt fungal infections, especially in
cell membrane formation by immunocompromised
inhibiting ergosterol synthesis, a vital patients.
component of the fungal cell ○ Key Point: Requires a
membrane. high-fat meal for optimal
● Common Uses: Treat systemic and absorption.
superficial fungal infections, 6. Terbinafine:
including those caused by Candida ○ Indication: Primarily for
and Aspergillus species. onychomycosis and tinea
1. Fluconazole: infections.
○ Indication: Often used for ○ Key Point: Has
candidiasis (oral, vaginal, hepatotoxicity risk; liver
systemic).
function monitoring is Other Systemic Antifungals
advised.
7. Voriconazole: 1. Amphotericin B:
○ Indication: Commonly used ○ Indication: Broad-spectrum
for invasive aspergillosis. antifungal, effective against a
○ Key Point: Can cause visual wide range of systemic
disturbances; monitor for fungal infections.
hepatotoxicity. ○ Key Point: Known for
nephrotoxicity; requires close
monitoring of kidney function.
2. Flucytosine:
Echinocandin Antifungals ○ Indication: Often combined
with amphotericin B for
● General Info: These inhibit severe infections, especially
synthesis of β-glucan, an essential cryptococcal meningitis.
component of fungal cell walls. ○ Key Point: Bone marrow
Known for fewer side effects. suppression can occur;
● Common Uses: Used primarily for monitor blood counts.
Candida and Aspergillus infections, 3. Griseofulvin:
especially in patients who cannot ○ Indication: Primarily for
tolerate azoles. dermatophyte infections
1. Anidulafungin: (e.g., tinea capitis).
○ Indication: Primarily for ○ Key Point: Take with a fatty
systemic Candida infections. meal for better absorption;
○ Key Point: Does not require avoid in pregnancy.
dose adjustment in renal 4. Nystatin:
impairment. ○ Indication: Mainly used for
2. Caspofungin: oral or cutaneous
○ Indication: Effective against candidiasis.
Candida and Aspergillus ○ Key Point: Not absorbed
infections. systemically; safe for topical
○ Key Point: May need dose or oral use.
adjustment in hepatic
impairment.
3. Micafungin:
○ Indication: Often used for Topical Antifungals
prophylaxis of Candida
infections in stem cell Azole Topical Antifungals
transplant recipients.
○ Key Point: Generally well ● General Info: Azole topicals are
tolerated, low risk of drug effective for treating localized fungal
interactions. infections, especially in the skin and
mucous membranes.
1. Butoconazole, Clotrimazole,
Econazole, Efinaconazole,
Ketoconazole, Luliconazole, ○
Indication: Commonly used
Miconazole, Oxiconazole, for athlete's foot and jock
Sertaconazole, Sulconazole, itch.
Terbinafine, Terconazole, ○ Key Point: Available over the
Tioconazole: counter; effective for mild
○ Indications: Used for tinea infections.
treating tinea infections (e.g., 6. Undecylenic Acid:
athlete’s foot, jock itch) and ○ Indication: Often used for
vulvovaginal candidiasis. mild athlete's foot.
○ Key Point: Generally safe for ○ Key Point: Less effective
short-term use; follow than other topical antifungals
specific instructions for but used as an alternative for
application area. sensitive skin.

—-------------------------------------------------------

Other Topical Antifungals


● Fungal infections in humans can
1. Butenafine: range from mild (like "athlete’s foot")
○ Indication: Used for tinea to severe (potentially deadly
infections (ringworm, infections).
athlete's foot, jock itch). ● When a fungus causes an infection,
○ Key Point: Similar to azoles it is called a mycosis.
in efficacy but structurally ● Fungi are different from bacteria:
different. ○ Fungi have a hard cell wall
2. Ciclopirox: made of chitin and
○ Indication: Effective against polysaccharides.
tinea and certain yeast ○ They have a cell membrane
infections. with a special protein called
○ Key Point: Also used as a ergosterol.
nail lacquer for ○ This structure makes fungi
onychomycosis. resistant to antibiotics
3. Gentian Violet: (because antibiotics target
○ Indication: Antifungal and bacteria).
antibacterial; used for oral ○ In contrast, bacteria are not
candidiasis and minor skin affected by antifungal
infections. drugs.
○ Key Point: Can stain skin
and fabrics; avoid swallowing
when used in the mouth.
4. Naftifine: Why Fungal Infections Are
○ Indication: Tinea infections. Increasing
○ Key Point: Applied once
daily, generally well tolerated.
5. Tolnaftate:
● More people are getting fungal cause the drug to enter the
infections because of an increase in bloodstream.
immunocompromised patients: ○ Avoid tight diapers or
○ Immunocompromised bandages on affected areas
means weak immune to prevent toxic reactions.
systems, which can’t fight
infections well.
○ People with AIDS, cancer,
transplant patients, and For Adults
some elderly people are at
● Antifungal drugs can be toxic, so
higher risk.
they should only be used if the exact
● For example, a fungus called
fungus is identified.
Candida is usually harmless on
● Over-the-counter (OTC)
mucous membranes.
antifungals are common for skin
○ In people with weak immune
infections.
systems, Candida can cause
○ Patients should follow
thrush in the GI tract and
instructions carefully and
vaginitis in the vagina.
consult a healthcare provider
if the problem persists.
● Pregnant and nursing women:
○ Should only use antifungals
Using Antifungal Drugs by Age
if necessary, as these drugs
Group can affect the fetus or baby.
○ Women who might become
For Children
pregnant should use barrier
● Children are more sensitive to contraceptives (like
antifungal drugs. condoms) when using these
○ They may have stronger drugs.
reactions or side effects. ○ If a fungal infection is severe,
○ Many antifungal drugs aren’t it may risk the mother and
fully tested for safety in baby’s lives, so doctors might
children, so extra caution is recommend antifungal
needed. treatment despite risks.
○ Preferred drugs for children
For Older Adults
include fluconazole,
ketoconazole, terbinafine, ● Older adults may be at a higher risk
and griseofulvin (if the of side effects from antifungal
infection is suitable for these drugs.
drugs). ● Liver and kidney health is
● Topical agents (creams or important when using antifungal
ointments) should: drugs:
○ Not be used on open or ○ Liver: Some antifungals
draining skin, as this can (ketoconazole, itraconazole,
griseofulvin) are hard on the Table 11.1 Drugs in Focus:
liver. Systemic Antifungals
■ If the patient has liver
problems (like from
old age, heavy
Azole Antifungals (Systemic
drinking, or other
medications), the Antifungals)
dose might need to
Azoles are drugs used to treat fungal
be reduced and the
infections. They work by stopping the
patient monitored
fungus from making something essential for
closely.
its cell membrane.
○ Kidneys: Some drugs
(flucytosine, fluconazole, 1. Fluconazole (Diflucan)
griseofulvin) can damage ○ Dosage:
the kidneys. ■ Adult: 200–400 mg
■ In patients with by mouth (PO) or
kidney issues, intravenously (IV) on
antifungal use should day 1, then 100
be careful and mg/day for 2–3
monitored. weeks. For vaginal
Candida, 150 mg as a
—----------------------------------------------------
single dose.
■ Pediatric: 3–6 mg/kg
Key Points to Remember PO or IV (don’t go
over 12 mg/kg).
1. Fungal infections can be minor or
○ Uses: Treats infections like
very serious; they’re called
candidiasis (yeast infection),
mycoses.
cryptococcal meningitis, and
2. Fungi are hard to kill because of
other severe fungal
their unique cell wall and membrane,
infections.
making them different from bacteria.
2. Isavuconazonium (Cresemba)
3. Antifungal drugs must be chosen
○ Dosage:
carefully, especially for children,
■ 372 mg IV or PO
pregnant women, and older
every 8 hours for 6
adults.
doses, then 372 mg
4. Side effects can be severe,
once a day.
especially on the liver and kidneys.
○ Uses: Treats serious fungal
5. Patients should follow instructions
infections like aspergillosis
closely and report any issues to a
and mucormycosis.
healthcare provider.
3. Itraconazole (Sporanox)
○ Dosage:
—----------------------------------------------
■ Adult: 200–400 mg
PO daily.
○ Uses: Treats blastomycosis, These antifungals work by disrupting the
histoplasmosis, and cell wall of the fungus.
aspergillosis.
4. Ketoconazole (Generic) 1. Anidulafungin (Eraxis)
○ Dosage: ○ Dosage:
■ Adult: 200–400 mg ■ 100–200 mg IV on
PO daily, up to 400 day 1, then 50–100
mg in severe cases. mg daily.
○ Uses: Treats conditions like ○ Uses: Used for candidemia
candidiasis, (fungal blood infection) and
coccidioidomycosis, and other invasive infections.
more. Can also be used in 2. Caspofungin (Cancidas)
shampoos for fungal scalp ○ Dosage:
infections. ■ 70 mg IV as a loading
5. Posaconazole (Noxafil) dose, then 50 mg IV
○ Dosage: daily.
■ 100–600 mg PO or IV ○ Uses: Treats infections in
per day, depending patients who cannot tolerate
on infection. or don’t respond to other
○ Uses: Prevents infections in treatments.
patients at high risk due to 3. Micafungin (Mycamine)
weakened immune systems. ○ Dosage:
6. Terbinafine (Lamisil) ■ Adult: 150 mg IV
○ Dosage: daily for 1–3 days.
■ Adult: 250 mg PO ○ Uses: Treats infections in the
daily for 6–12 weeks. esophagus and prevents
○ Uses: Treats nail infections Candida infections.
(onychomycosis) and other
skin infections.
7. Voriconazole (Vfend)
○ Dosage: Other Systemic Antifungals
■ 6 mg/kg IV every 12
These antifungals don’t fit in the other
hours for two doses,
groups but are still used for systemic
then 4 mg/kg IV every
(whole-body) fungal infections.
12 hours.
○ Uses: Treats serious
1. Amphotericin B (Abelcet,
infections like invasive
AmBisome)
aspergillosis.
○ Dosage:
■ 3–5 mg/kg IV based
on infection.
○ Uses: Treats severe
Echinocandin Antifungals
infections like aspergillosis,
leishmaniasis, and
cryptococcal meningitis.
2. Flucytosine (Ancobon) Azole Antifungals
○ Dosage:
■ 50–150 mg/kg PO in ● What are they?
divided doses every 6 Azole antifungals are a group of
hours. medicines that treat fungal
○ Uses: Treats systemic infections. These infections can be
infections caused by Candida systemic (affecting the whole body)
or Cryptococcus. or topical (affecting one part of the
3. Griseofulvin (Generic) body, like skin or nails).
○ Dosage: ● Examples of Azole Antifungals:
■ 500 mg PO daily. ○ Fluconazole (Diflucan)
○ Uses: Treats skin infections ○ Itraconazole (Sporanox)
like ringworm (tinea ○ Ketoconazole (Nizoral)
infections). ○ Posaconazole (Noxafil)
4. Nystatin (Generic) ○ Terbinafine (Lamisil)
○ Dosage: ○ Voriconazole (Vfend)
■ 500,000–1,000,000 ○ Isavuconazonium
units three times daily (Cresemba) – newest drug in
(t.i.d.). this group.
○ Uses: Treats oral, vaginal, ● Effectiveness and Safety:
and skin infections by Azoles are generally less toxic
Candida. (safer) than some other strong
antifungals, like amphotericin B.
—------------------------------------------------------- But they might not be as effective in
very severe and fast-spreading
Summary and Tips for infections.
Memorization

1. Azoles (fluconazole, itraconazole,


ketoconazole, etc.) are mostly taken How Azole Antifungals Work
by mouth or IV. They are used for (Therapeutic Actions and
various fungal infections and often Indications)
have pediatric doses.
2. Echinocandins (anidulafungin, ● Mechanism of Action (How they
caspofungin, micafungin) are mostly kill or stop fungus):
for severe infections like ○ Azoles work by attaching to
candidemia and are given IV only. sterols (a kind of molecule)
3. Other Antifungals include in the fungal cell wall.
amphotericin B and flucytosine for ○ They can cause fungal cell
systemic infections, griseofulvin for death (fungicidal) or stop the
skin infections, and nystatin for oral fungus from growing and
and vaginal infections. dividing (fungistatic),
depending on:
—-------------------------------------------------------
■ Type of fungus being ● Terbinafine:
treated. ○ This drug also blocks
■ Dose of the drug ergosterol formation.
used. ○ It affects an enzyme system
● What Happens to the Fungal Cell? called CYP2D6 (part of the
When azoles attach to sterols, they CYP450 system). This is
change the fungal cell wall so that important for people taking
it can’t hold its shape or function. other medicines that use the
This leads to cell death or stops the CYP450 system for
fungus from replicating (making processing in the liver.
more fungal cells). ○ Extra Info: Terbinafine
comes in a sprinkle form for
children.

Types of Azole Antifungals and —-------------------------------------------------------


Their Specific Actions
Key Points to Remember:
● Ketoconazole, Fluconazole,
Itraconazole: 1. Azole antifungals treat fungal
○ These drugs block sterol infections by changing the fungal
activity in the fungal wall, cell wall.
stopping the fungus from 2. They can either kill the fungus or
working properly. stop it from growing, depending on
○ Side Effect: They might also the fungus and drug dose.
affect human steroids like 3. Different azoles have slightly
testosterone and cortisol different ways of working, but they
(hormones in our body). all target the fungal cell wall.
● Posaconazole, Voriconazole, and 4. Some azoles can affect human
Isavuconazonium: hormones, so they may have side
○ These are called triazole effects related to testosterone and
antifungals. cortisol.
○ They stop the fungus from
making ergosterol (an —-------------------------------------------------------
important part of the fungal
cell wall). Pharmacokinetics of Azole
○ Result: Without ergosterol, Antifungals
the fungus cannot make a
strong cell wall, leading to ● What is Pharmacokinetics?
cell death. This is about how the body
○ Isavuconazonium is special absorbs, processes, and gets rid
because it is a prodrug. This of the drug.
means it needs to change in
the body to become the
active drug, isavuconazole.
How Each Drug is Taken and Works in ○ Absorption: Slowly
the Body absorbed from the stomach.
○ Processing: Broken down
● Ketoconazole, Itraconazole, by the CYP450 system in
Posaconazole, and Terbinafine the liver; leaves through
○ How to take: These drugs urine and feces.
are usually taken orally (by 4. Posaconazole
mouth). ○ Absorption: Works quickly,
○ Other forms: Ketoconazole peaks in 3 to 5 hours.
can also be found as a ○ Processing: Broken down in
shampoo or cream. the liver, leaves in feces.
Terbinafine comes in a 5. Terbinafine
sprinkle form for children. ○ Absorption: Quickly
● Fluconazole, Isavuconazonium, absorbed.
and Voriconazole ○ Processing: Extensively
○ How to take: These can be broken down in the liver,
taken orally (by mouth) or leaves through urine, with a
intravenously (IV) (through long half-life of 36 hours
a vein). (stays in the body for a long
○ Why IV? IV is useful for time).
serious infections because it 6. Voriconazole
works faster. Once the ○ Absorption: Peaks in 1 to 2
patient feels better, they can hours orally; if IV, works right
switch to oral. away.
○ Processing: Broken down in
Absorption and Processing of Each Drug the liver, half-life is 24
hours, leaves through urine.
1. Ketoconazole
7. Isavuconazonium
○ Absorption: Quickly
○ Absorption: Peaks in 2 to 3
absorbed from the stomach,
hours orally; in 1 hour if IV.
reaches peak in 1 to 3
○ Processing: Broken down in
hours.
the liver, leaves through
○ Processing: Broken down in
urine and stool; long
the liver; leaves the body
half-life of 130 hours (stays
through feces (poop).
a very long time).
2. Fluconazole
○ Absorption: Peaks in 1 to 2
hours.
○ Processing: Mostly
Contraindications and Cautions
unchanged in urine (doesn’t
break down much), so be (When to Avoid or Be Careful)
careful if the patient has
● Ketoconazole
kidney problems.
○ Liver Caution: Can cause
3. Itraconazole
serious liver damage, so
avoid in patients with liver ○ QT Interval: Don’t use with
problems. drugs that lengthen the QTc
○ Endocrine Issues: Not interval (heart rhythm
recommended for people measure) because it could
with hormone or fertility make it worse.
issues. ○ Ergot Alkaloids Warning:
● Fluconazole Don’t combine with ergots
○ Liver and Kidney Caution: (another type of drug)
Be careful if the patient has because it could cause a
liver or kidney problems (it serious reaction called
could damage these organs). ergotism.
○ No Endocrine Effect:
Doesn’t affect hormones like —-------------------------------------------------------
ketoconazole does.
● Itraconazole Key Points to Remember:
○ Liver Caution: Linked to
liver failure; avoid in 1. Each drug is absorbed, processed,
patients with serious liver and removed by the body
issues. differently.
● Posaconazole 2. Be cautious with these drugs if the
○ Pregnancy and patient has liver, kidney, hormone,
Breastfeeding: Not known if or pregnancy issues.
safe for 3. Some drugs (like voriconazole and
pregnancy/breastfeeding; isavuconazonium) need to be
use only if absolutely avoided with certain other drugs
necessary. because they can cause harmful
○ Liver Caution: Can cause interactions
liver toxicity; watch for
—-------------------------------------------------------
bone marrow, GI, and liver
toxicity.
● Terbinafine and Isavuconazonium Box 11.2 Focus on Safe
○ Liver Caution: Linked to Medication Administration
severe liver toxicity; don’t
use in people with liver Name confusion has occurred between
failure. Lamisil (terbinafine) and Lamictal
○ Pregnancy and (lamotrigine, an antiepileptic agent). Use
Breastfeeding: Could cross extreme caution if your patient is receiving
the placenta and enter either of these drugs to make sure that the
breast milk. Avoid in correct drug is being used
pregnant/nursing women due —-------------------------------------------------------
to possible risks to the baby.
● Voriconazole and
Isavuconazonium
Adverse Effects (Unwanted Side hypoglycemics (blood
Effects) sugar-lowering drugs),
warfarin, oral
● Main Side Effect: Most of the azole anticoagulants (blood
antifungal drugs can cause liver thinners), and phenytoin.
toxicity. This means they can ○ What to Do: If these drugs
damage the liver if not used must be taken together,
carefully. watch the patient closely.
● Effect on The doses might need
Pregnancy/Breastfeeding: These adjusting to avoid problems.
drugs can also harm a fetus Always consult a drug
(unborn baby) or a nursing baby guide when starting or
(baby who is breastfed), so they stopping these drugs.
should be used carefully in pregnant 2. Itraconazole
or breastfeeding women. ○ Black Box Warning: This
drug has a black box
warning (serious safety
alert) about causing
Clinically Important Drug-Drug dangerous heart effects if
Interactions (Interactions with taken with certain other
drugs.
Other Drugs)
○ Avoid These
● What are Drug Interactions? Combinations: Don’t take it
Sometimes, taking two drugs with lovastatin, simvastatin
together can cause problems. They (cholesterol-lowering drugs),
can change how each other works triazolam, midazolam
in the body, sometimes making them (sedatives), pimozide, or
too strong or too weak. dofetilide (heart rhythm
drugs).
Key Interactions with Azole Drugs 3. Voriconazole, Isavuconazonium,
and Posaconazole
1. Ketoconazole and Fluconazole ○ QTc Interval Warning:
○ CYP450 Enzyme Blockers: These drugs shouldn’t be
These two drugs block the used with other drugs that
CYP450 enzyme system in lengthen the QTc interval (a
the liver. This enzyme helps measure of heart rhythm)
the liver process drugs, so because it can make the
blocking it can lead to higher heart rhythm problem worse.
levels of other drugs in the ○ Ergotism Risk: If taken with
blood, making them stronger ergot alkaloids (a type of
than they should be. drug made from a fungus),
○ Drugs Affected: This these can cause ergotism, a
includes drugs like serious condition with
cyclosporine, digoxin, oral symptoms like cramps,
headaches, and blood vessel
problems.
○ Herbal Warning: Be careful
with herbs like ergot, as they
can dangerously interact with
voriconazole and
posaconazole.

—-------------------------------------------------------

Key Points to Remember

1. Liver and Pregnancy Risks: Azole


drugs can damage the liver and
harm a fetus or baby.
2. CYP450 Blocking: Ketoconazole
and fluconazole block an enzyme in
Echinocandin Antifungals
the liver, making other drugs
● What are Echinocandins?
stronger, which can be dangerous.
Echinocandins are a type of
3. Heart Risk with Itraconazole:
antifungal drug used to treat fungal
Avoid certain drugs with itraconazole
infections. The main drugs in this
because of serious heart risks.
group are:
4. QTc Interval and Ergotism:
○ Anidulafungin (brand name:
Voriconazole, isavuconazonium, and
Eraxis)
posaconazole should not be taken
○ Caspofungin (brand name:
with drugs that affect heart rhythm
Cancidas)
or with ergot alkaloids because they
○ Micafungin (brand name:
can cause severe side effects.
Mycamine)
—-------------------------------------------------------
Box 11.3 Focus on Herbal and
Alternative Therapies Therapeutic Actions and
Indications
Patients being treated with voriconazole or
posaconazole should be cautioned about ● How They Work:
the risk of ergotism if they combine this drug These drugs work by blocking
with ergot, an herb frequently used to treat glucan synthesis.
migraine headache and menstrual ○ Glucan is an enzyme (a kind
problems. If the patient is using either of of chemical) that is important
these drugs, it should be suggested that for making the cell wall in
ergot not be used until the antifungal fungi (the outer layer that
therapy is finished. protects the fungal cell).
—-------------------------------------------------------
○ Human cells don’t have ○ Half-Life: 14–17 hours.
glucan, so these drugs ○ Excretion: Leaves the body
target only fungal cells. through urine.
○ When glucan synthesis is
blocked, the fungal cell wall
can’t form, which kills the
fungal cell. Contraindications and Cautions
(Who Should Be Careful or Avoid
These Drugs)
Pharmacokinetics (How the Drug ● Anidulafungin
Moves Through the Body) ○ Pregnancy and
Breastfeeding: Can cross
1. Anidulafungin the placenta (could affect an
○ Given as: An IV infusion unborn baby) and enter
(injected into the vein) once breast milk (could affect a
daily for at least 14 days. breastfeeding baby). Avoid
○ Action: Works quickly. in pregnant or
○ Metabolism: Broken down breastfeeding women.
by degradation (not through ○ Liver Caution: Be careful in
the liver). people with liver problems
○ Half-Life: 40–50 hours (this because it can harm the
means it takes 40–50 hours liver.
for half of the drug to leave ● Caspofungin
the body). ○ Liver Caution: Can damage
○ Excretion: Leaves the body the liver, so use smaller
through feces. doses in people with liver
2. Caspofungin issues.
○ Given as: An IV drug ○ Pregnancy and
(injected into the vein). Breastfeeding: Shown to
○ Metabolism: Broken down harm embryos in animals
slowly by the liver. (embryotoxic) and can enter
○ Half-Life: Goes through breast milk. Use with great
stages, with times of 9–11 caution during pregnancy
hours, 6–48 hours, and and breastfeeding.
40–50 hours. ● Micafungin
○ Distribution: Spreads ○ Pregnancy and
through the body and binds Breastfeeding: Only use
to protein. during pregnancy or
○ Excretion: Leaves the body breastfeeding if benefits are
through urine. greater than risks because
3. Micafungin it might harm the baby.
○ Given as: An IV drug.
○ Action: Works quickly.
Adverse Effects (Side Effects) ● Amphotericin B (brand names:
Abelcet, AmBisome)
● Anidulafungin and Caspofungin ● Flucytosine (brand name: Ancobon)
○ Liver Toxicity: These drugs ● Griseofulvin (brand name:
can damage the liver. So, Gris-Peg)
it’s important to check liver ● Nystatin (generic)
function closely when using
them.
● Micafungin
○ Serious Allergic Reactions: Therapeutic Actions and
Micafungin can cause Indications (How They Work and
severe allergic When They’re Used)
(hypersensitivity) reactions
in some people. 1. Amphotericin B
● Bone Marrow Suppression: ○ How It Works: This drug
○ Bone Marrow Suppression: attaches to sterols in the
All these drugs can lower fungal cell wall, which
bone marrow function, changes the cell wall’s
which affects blood cell permeability (how easily
production. Patients need to things pass through it). This
be monitored closely for can lead to:
this effect. ■ Cell death (kills the
fungal cell) or
■ Stops reproduction
(stops the fungus
Clinically Important Drug–Drug from multiplying).
Interactions ○ When It’s Used: It has many
unpleasant side effects, so
● Caspofungin and Cyclosporine it’s usually saved for serious,
○ Dangerous Together: Using life-threatening infections.
caspofungin with 2. Flucytosine
cyclosporine is not ○ How It Works: Changes the
recommended because it cell membrane of fungi that
could cause severe liver are sensitive to it, which
injury. They should only be causes cell death.
combined if the benefits ○ When It’s Used: Often
outweigh the risks. chosen because it’s less
toxic than amphotericin B.
3. Griseofulvin
Other Antifungal Agents ○ How It Works: This older
antifungal drug changes cell
Some other antifungal drugs don’t fit into membrane permeability,
specific classes (like azoles or leading to cell death.
echinocandins). These include:

When It’s Used: Used for Drug Interactions: Be very careful with
infections where this action is caspofungin and cyclosporine; they
effective. shouldn’t be used together unless really
4. Nystatin needed.
○ How It Works: Like —-------------------------------------------------------
amphotericin B, nystatin
binds to sterols in the fungal Clinically Important Drug–Drug
cell wall. This changes Interactions for Amphotericin B
membrane permeability,
which causes parts of the cell ● Amphotericin B and Nephrotoxic
to leak out, leading to cell Drugs (Drugs that can damage the
death. kidneys)
○ When It’s Used: Often used ○ Avoid Combining: Patients
for different fungal infections taking amphotericin B should
because of its ability to kill not use other drugs that
fungal cells by changing the can harm the kidneys
cell wall. unless absolutely necessary.
This includes:
—------------------------------------------------------- ■ Nephrotoxic
Antibiotics
Key Points to Remember (antibiotics that can
damage kidneys)
1. Echinocandins Block Glucan: This ■ Antineoplastics
kills fungal cells by stopping the cell (drugs used in cancer
wall from forming. treatment that can be
2. Given Through IV: All these drugs toxic to kidneys)
are given through IV injections. ■ Cyclosporine (a drug
3. Liver Warnings: These drugs, that can affect the
especially caspofungin, can harm immune system and
the liver. Be careful if the person has is hard on kidneys)
liver problems. ■ Corticosteroids
4. Pregnancy and Breastfeeding (steroids that can also
Risks: These drugs might harm a have kidney side
baby, so they should be used effects)
carefully in pregnant or ○ Reason: Using amphotericin
breastfeeding women. B with these drugs raises
the risk of severe kidney
Watch Out for Liver Damage:
damage (renal toxicity).
Anidulafungin and caspofungin can damage
the liver, so liver function needs monitoring. —-------------------------------------------------------
Micafungin Risks: Micafungin can cause
serious allergic reactions.
Bone Marrow Suppression: All these
drugs can lower blood cell production, so
patients need close monitoring.
Nursing Considerations for 2. Nursing Diagnoses
Patients Receiving Systemic
● Common Diagnoses:
Antifungals ○ Acute pain related to the
drug’s effects on the stomach
1. Assessment: History and Examination
(GI), nervous system (CNS),
● Check for Contraindications: or the site of infection.
○ Allergy: Look for any history ○ Disturbed sensory perception
of allergy to antifungals. This (like feeling dizzy) due to
helps avoid allergic CNS effects.
reactions. ○ Lack of knowledge about the
○ Liver or Kidney Problems: drug treatment.
If the patient has liver or
3. Planning
kidney issues, it may affect
how the body processes the ● Goals:
drug. ○ Ensure the patient receives
○ Pregnancy or the best effects from the
Breastfeeding: Certain antifungal.
antifungals can harm the ○ Limit any negative effects
baby or infant. from the treatment.
● Physical Assessment: ○ Educate the patient about the
○ Establish baseline health to drug, possible side effects,
see how well the drug is and how to stay comfortable.
working and to catch any
side effects. 4. Implementation with Rationale
○ Test for alertness and
reflexes to check for effects ● Testing:
on the nervous system ○ Do culture tests before
(CNS). starting treatment to choose
○ Examine the skin for color the right drug.
and any rashes to monitor for ○ Start treatment quickly for
skin problems. serious infections, even if
● Cultures: tests are pending.
○ Take a sample from the ● Medication Administration:
infected area to identify the ○ Complete the full course of
type of fungus and how it the antifungal (may take up
responds to treatment. to 6 months for chronic
● Lab Tests: infections) to ensure
○ Check kidney (renal) and effectiveness.
liver (hepatic) function, and ● Monitoring IV Sites:
complete blood counts to ○ Watch for signs of swelling or
establish baseline health and irritation at the IV site
monitor for toxicity. (phlebitis) and change sites if
needed.
● Kidney and Liver Function: ■ Yellowing skin or eyes
○ Check kidney and liver health (could mean liver
before starting and during issues)
treatment. Stop the drug if ■ Severe nausea and
problems arise. vomiting (could affect
● Comfort and Safety: nutrition).
○ Provide safety measures if
the patient feels dizzy (like 6. Evaluation
using side rails or getting
help moving). ● Monitor Effectiveness:
○ Manage headaches and ○ Check if the fungal infection
fevers with pain relievers and improves.
temperature control. ○ Look for side effects: observe
○ Offer small, frequent meals if alertness, nutritional status,
the patient has stomach skin condition, and
upset. kidney/liver function.
● Nutritional Support: ● Evaluate Teaching:
○ Monitor food intake and ○ Ensure the patient can
consider a dietitian's advice if explain the medication name,
needed. dosage, side effects, and
● Patient Education: safety measures.
○ Teach the patient about their ● Comfort and Compliance:
medication and how to take it ○ Check how well comfort
properly. measures are working and if
the patient is following the
5. Patient Teaching treatment plan.

● Dosage and Safety: —-------------------------------------------------------


○ Follow the prescribed dosage
exactly. Key Points
○ Change positions slowly and
avoid driving if feeling dizzy. ● Fungi: Can cause many infections;
● Diet Tips: they are different from bacteria
○ Take the antifungal with because they have a tough outer
meals to help with stomach wall made of chitin and a specific
issues. cell membrane with ergosterol.
○ If nausea is a problem, try ● Toxicity: Systemic antifungal drugs
smaller meals more often. can be harmful. It’s crucial to use the
● Report Symptoms: correct drug and monitor patients
○ Tell a healthcare provider if carefully.
they notice: ● Drug Interactions: Systemic
■ Sore throat antifungals can interact with other
■ Unusual bruising or medications, especially those
bleeding processed by the liver. Be vigilant
when adding or removing drugs from 3. Common Topical Antifungals
a patient’s treatment plan.
● Azole-Type Antifungals:
—------------------------------------------------------- ○ Butoconazole (Gynazole-1)
○ Clotrimazole (Lotrimin,
Topical Antifungals Mycelex)
○ Econazole (Ecoza)
1. What Are Topical Antifungals? ○ Efinaconazole (Jublia)
○ Ketoconazole (Extina,
● Topical antifungals are medications Nizoral, Xolegel)
applied directly to the skin or ○ Miconazole (Lotrimin AF,
mucous membranes to treat fungal Monistat 3)
infections. ○ Oxiconazole (Oxistat)
● They are used for various skin ○ Sertaconazole Nitrate
conditions and infections. (Ertaczo)
○ Sulconazole (Exelderm)
2. Types of Fungal Infections Treated
○ Terbinafine (Lamisil)
○ Terconazole (Terazol)
● Dermatophytes: Fungi that cause
○ Tioconazole (Vagistat-1)
skin infections called mycoses.
● Other Antifungals:
● Common Mycoses:
○ Butenafine (Mentax)
○ Tinea Infections: Often
○ Ciclopirox (Loprox, Penlac
called ringworm, although
Nail Lacquer)
they are caused by fungi, not
○ Gentian Violet (generic)
worms.
○ Luliconazole (Luzu)
■ Examples:
○ Naftifine (Naftin)
■ Athlete’s
○ Tolnaftate (generic)
Foot: Tinea
○ Undecylenic Acid (Cruex,
pedis
Desenex, Pedi-Dri, Fungoid
(infection on
AF)
feet).
■ Jock Itch:
—-------------------------------------------------------
Tinea cruris
(infection in Table 11.2 Drugs in Focus: Topical
the groin
Antifungals
area).
■ Yeast
Infections: Azole Topical Antifungals
Often caused
Azole antifungals are commonly used to
by Candida,
treat infections caused by fungi, especially
affecting the
yeast infections (like Candida) and various
mouth (oral
skin infections (like tinea or ringworm).
thrush) or
Azoles work by blocking a key component in
vagina.
fungal cell walls, stopping them from ○ Form: Topical solution (brand
growing. name: Jublia)
○ How to Apply: Use a brush
1. Butoconazole to apply to affected toenails
○ Form: Vaginal cream (brand daily for 48 weeks.
name: Gynazole-1) ○ Uses: Treats toenail
○ How to Apply: Apply only infections caused by fungi,
once a day for 4 weeks. specifically due to
○ Uses: Effective for treating Trichophyton species.
vaginal Candida infections ○ Memory Tip: "Efi-" for "Effort
(yeast infections). Every Day for Toenails" –
○ Memory Tip: "Buto-one" for daily application for toenail
“once a day, single daily health.
application." 5. Ketoconazole
2. Clotrimazole ○ Form: Available as a cream,
○ Form: Cream, lotion, or gel, foam, or shampoo
solution (available (brand names include
over-the-counter, brands Nizoral).
include Lotrimin, Mycelex) ○ How to Apply: Use once
○ How to Apply: Apply as a daily for 2–4 weeks.
thin layer twice daily for 2–4 ○ Uses: Treats dandruff,
weeks. seborrheic dermatitis, tinea
○ Uses: Treats both oral and infections, and sometimes
vaginal Candida infections, fungal infections in hair.
and various tinea infections ○ Memory Tip: "Keto" for
(e.g., athlete’s foot, jock itch). "Keep your scalp Clear" from
○ Memory Tip: "Clo-" sounds dandruff and fungi.
like "Clear infections with 6. Luliconazole
Twice Daily application." ○ Form: Cream (brand name:
3. Econazole Luzu)
○ Form: Cream (brand name: ○ How to Apply: Apply daily
Spectazole) for 1–2 weeks on the
○ How to Apply: Apply as a affected area.
thin layer once or twice daily ○ Uses: Effective for treating
for 2 weeks. tinea pedis (athlete's foot),
○ Uses: Treats different types tinea cruris (jock itch), and
of tinea (fungal) infections on tinea corporis (ringworm).
the skin. ○ Memory Tip: "Luli-" for "Light
○ Memory Tip: "Eco" sounds treatment" – a short
like "easy," so it’s a short treatment duration.
application period, once or 7. Miconazole
twice daily. ○ Form: Cream, powder, gel,
4. Efinaconazole spray (available OTC, brand
names include Monistat 3)
○ How to Apply: Apply twice 11. Terbinafine
daily for 2–4 weeks. ○ Form: Cream or gel (brand
○ Uses: Treats several types of name: Lamisil)
fungal infections, including ○ How to Apply: Apply once
athlete's foot, jock itch, daily for 1–4 weeks.
ringworm, and vaginal ○ Uses: Treats tinea infections
Candida infections. like athlete’s foot, jock itch,
○ Memory Tip: "Mico-" for and ringworm.
"Multiple forms for Candida ○ Memory Tip: "Terbi-" for
and Tinea." "Terminate Fungus" in a
8. Oxiconazole short time.
○ Form: Cream, lotion (brand 12. Tioconazole
name: Oxistat) ○ Form: Vaginal ointment
○ How to Apply: Apply once or (brand name: Vagistat-1)
twice daily for 2–4 weeks. ○ How to Apply: One
○ Uses: Treats tinea infections single-dose treatment; apply
on the skin (up to 4 weeks of with an applicator at bedtime.
treatment). ○ Uses: Treats recurrent
○ Memory Tip: "Oxi-" sounds vaginal Candida infections.
like "Apply Once or twice for ○ Memory Tip: "Tio-" sounds
infections." like "One Time Only" –
9. Sertaconazole Nitrate single-dose treatment.
○ Form: Topical cream (brand
name: Ertaczo)
○ How to Apply: Apply
between toes and Other Topical Antifungals
surrounding skin twice a day
for 4 weeks. These are antifungal drugs that work
○ Uses: Specifically targets differently from azoles and can be used for
tinea pedis (athlete’s foot). various fungal infections on the skin, nails,
○ Memory Tip: "Serta-" for and more.
"Specific to Toes" – twice
1. Butenafine
daily for athlete’s foot.
○ Form: Topical cream (brand
10. Sulconazole
name: Mentax)
○ Form: Cream (brand name:
○ How to Apply: Apply in a
Exelderm)
thin layer once or twice daily.
○ How to Apply: Use for
○ Uses: Treats tinea infections,
athlete's foot; apply once or
like athlete’s foot, jock itch,
twice daily for 4–6 weeks.
and ringworm.
○ Uses: Treats tinea infections,
○ Memory Tip: "Bute" sounds
especially athlete's foot.
like "Both morning and
○ Memory Tip: "Sulco" sounds
night."
like "Sport" – suitable for
2. Ciclopirox
athlete's foot.
○ Form: Gel, cream, lotion, ○
Form: Powder, cream, gel,
suspension, shampoo and spray (brand name:
(brands: Loprox, Penlac Nail Tinactin)
Lacquer) ○ How to Apply: Twice a day
○ How to Apply: Apply twice for 2–4 weeks.
daily for 4 weeks. ○ Uses: Treats athlete’s foot,
○ Uses: Used for treating tinea jock itch, and ringworm.
infections, nail infections, and ○ Memory Tip: "Tol" for
seborrheic dermatitis. "Topical on Toes."
○ Memory Tip: "Ciclo-" for 7. Undecylenic Acid
"Cleans the Layers" of skin ○ Form: Powder, cream, or
and nails. ointment (brand names
3. Gentian Violet include Cruex, Desenex)
○ Form: Solution ○ How to Apply: Use as
○ How to Apply: Applied twice needed.
a day to the affected area. ○ Uses: Treats athlete’s foot,
○ Uses: Treats fungal ringworm, jock itch, diaper
infections on the skin and rash, and chafing.
oral thrush. ○ Memory Tip: "Unde-" for
○ Memory Tip: "Violet" – "Under Toes" – fights foot
remember the purple color it fungi.
leaves on the skin.
4. Naftifine —-------------------------------------------------------
○ Form: Cream or gel (generic
available) Key Takeaways
○ How to Apply: Apply once
daily for up to 4 weeks. ● Azoles are the main class for
○ Uses: Treats severe fungal treating fungal infections. They are
infections on the skin. often applied in cream form and
○ Memory Tip: "Naf-" for "No work by stopping fungi from growing.
Fungus" after 4 weeks. ● Application Methods: Some drugs
5. Tavaborole are used daily (e.g., econazole),
○ Form: Solution for toenails while others only need a single dose
(brand name: Kerydin) (e.g., tioconazole).
○ How to Apply: Apply daily to ● Other Antifungals (like butenafine,
toenails for up to 48 weeks. ciclopirox) have unique applications
○ Uses: Treats fungal for nails, feet, and severe skin
infections of the toenails infections.
(onychomycosis).
—-------------------------------------------------------
○ Memory Tip: "Tava" for
"Toenail Care" over time.
6. Tolnaftate
Topical Antifungals: Therapeutic very toxic if absorbed, so do
Actions and Information not use near open wounds.
○ Naftifine, Oxiconazole,
1. Therapeutic Actions Sertaconazole Nitrate: Use
for no longer than 4 weeks to
● How They Work: prevent problems and
○ Topical antifungal drugs resistance.
change how the fungus's cell ○ Sulconazole: Use for no
works. longer than 6 weeks to
○ This stops the fungus from prevent problems and
growing and leads to its resistance.
death. ○ Terbinafine: Use for no
● Uses: longer than 4 weeks; stop if
○ They are used for local the infection improves or if
treatment of fungal infections irritation occurs.
(mycoses). ○ Efinaconazole: Use with the
○ Common infections treated special brush applicator
include tinea infections (like provided.
athlete's foot and jock itch).
4. Adverse Effects
2. Pharmacokinetics
● Local Effects: When applied as
● Absorption: creams, lotions, or sprays, you may
○ These drugs do not enter the notice:
bloodstream, meaning they ○ Irritation
only work where they are ○ Burning sensation
applied. ○ Rash
○ They do not get broken down ○ Swelling
or removed by the body. ● Effects from Suppositories or
Troches: If taken in these forms,
3. Contraindications and Cautions possible side effects include:
○ Nausea
● Limitations: ○ Vomiting
○ Main issues to consider are: ○ Liver issues (due to some
■ Known allergy to any absorption)
topical antifungal. ○ Frequent urination
■ Open wounds or ○ Burning sensation
lesions on the skin. ○ Changes in sexual activity
● Specific Drugs: (due to local absorption in
○ Econazole: Can cause the vagina)
severe burning or irritation;
stop using if it gets bad.
○ Gentian Violet: Stains skin
and clothes bright purple;
treatment’s effectiveness and
check for any local side
effects.

2. Nursing Diagnoses

● Possible nursing problems include:


○ Acute Pain: Pain related to
how the drug works on the
skin.
○ Deficient Knowledge: The
patient may not know enough
about the drug therapy.
○ Risk for Impaired Skin
Nursing Considerations for Integrity: There is a risk that
the skin may get damaged.
Patients Receiving Topical
Antifungals 3. Planning

1. Assessment: History and Examination ● Goals for the patient include:


○ Getting the best results from
● Check for Allergies: the drug treatment.
○ Look for any known allergies ○ Experiencing few side effects
to topical antifungal drugs to from the drug.
avoid allergic reactions ○ Understanding the drug
(hypersensitivity). treatment, possible side
● Physical Assessment: effects, and how to reduce
○ Check the patient’s overall discomfort.
condition to gather basic
information. This helps to see 4. Implementation with Rationale
how well the treatment is
working and to spot any side ● Before Treatment:
effects. ○ Take samples from the
● Culture and Sensitivity Testing: infected area to identify the
○ Take samples from the fungus causing the problem.
infected area to find out ● Complete Drug Regimen:
which fungus is causing the ○ Make sure the patient
infection and which finishes the full course of
antifungal will work best. treatment to achieve the best
● Inspect the Application Area: results.
○ Look at the skin where the ● Instruct on Administration:
medicine will go for changes ○ Troches: Dissolve slowly in
in color, temperature, and the mouth.
any skin problems (lesions). ○ Vaginal
This helps to monitor the Suppositories/Creams:
Insert them high into the ○ Tell them to report any
vagina; stay lying down for severe irritation, burning, or
10 to 15 minutes after use. worsening of the infection to
○ Topical Creams and a healthcare provider.
Lotions: Rub gently into the
clean, dry area after washing 5. Evaluation
with soap and water. Avoid
using tight bandages over ● Monitor Patient Response:
the area. ○ Check if the signs and
● Stopping Treatment: symptoms of the fungal
○ Advise the patient to stop infection are getting better.
using the drug if they get a ● Watch for Adverse Effects:
severe rash, especially with ○ Look out for any rashes,
blisters or if irritation and pain irritation, or burning in the
get worse. This may mean area being treated.
they are allergic to the drug ● Evaluate Teaching Effectiveness:
or their condition is ○ Make sure the patient can
worsening. name the drug, dosage,
● Patient Teaching: possible side effects, and
○ Show the patient how to ways to avoid side effects.
apply the medication ● Comfort and Safety Measures:
correctly. ○ Monitor how well the patient
○ Explain how long they will is following the treatment
need to treat the infection. plan and if the comfort
○ Suggest wearing clean, dry measures are working.
socks for athlete’s foot to
—-------------------------------------------------------
help get rid of the infection.
○ Advise keeping the infected
area clean with mild soap
Key Points
and water, and to pat it dry.
1. Types of Local Fungal Infections:
○ Warn against scratching the
○ Vaginal and oral yeast
infected area; using cool
infections (caused by
compresses can help with
Candida).
itching.
○ Tinea infections, including:
○ Tell them not to use tight
■ Athlete’s foot.
dressings since they can
■ Jock itch.
increase absorption into the
2. What Are Topical Antifungals?
body.
○ Medications that treat local
○ Do not apply drugs near
fungal infections.
open wounds or sores
○ Not designed for use in the
because these drugs are not
whole body (systemically).
meant to enter the
3. Proper Use:
bloodstream.
○ Correct administration of effects, which may include
topical antifungals makes liver and kidney failure.
them more effective. ● Local Fungal Infections Revisited:
○ Important: Do not use them ○ Include vaginal and oral
near open wounds or lesions. yeast infections (from
4. Possible Side Effects: Candida) and various tinea
○ Can cause serious local infections (like athlete's foot
irritation, burning, and pain. and jock itch).
○ If these symptoms occur, the ● Topical Antifungals’ Purpose:
medication should be ○ Designed to treat skin and
stopped. mucosal infections locally.
● Administration Tips:
○ Proper use increases
effectiveness, and they
Summary should not be used near
open wounds or lesions.
● What is a Fungus? ● Side Effects Reminder:
○ A fungus is a type of cell that ○ Can lead to serious irritation,
has a hard outer layer (cell burning, and pain; stop use if
wall) made of chitin and these happen.
polysaccharides, and a
membrane that includes —-------------------------------------------------------
ergosterols.
● Mycosis: TO BE CONTINUE….
○ An infection caused by a
fungus is called a mycosis.
○ Systemic fungal infections
can be life-threatening,
especially in people with
weakened immune systems.
● How Do Systemic Antifungals
Work?
○ They change how cells allow
substances to pass in and
out (cell permeability).
○ This causes the cells to leak
important components,
preventing them from
replicating and leading to cell
death.
● Monitoring Patients:
○ Systemic antifungals can be
very toxic, so patients must
be watched closely for side

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