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Itraconazole; Uses, Dosage, Side Effects, Interactions, Pragnancy

Itraconazole is a synthetic triazole agent with antimycotic properties. Formulated for both topical and systemic use, itraconazole preferentially inhibits fungal cytochrome P450 enzymes, resulting in a decrease in fungal ergosterol synthesis. Because of its low toxicity profile, this agent can be used for long-term maintenance treatment of chronic fungal infections

Itraconazole is an orally administered, triazole antifungal agent used in the treatment of systemic and superficial fungal infections. Itraconazole therapy is associated with transient, mild-to-moderate serum elevations and can lead to clinically apparent acute drug-induced liver injury.

Mechanism of Action of Itraconazole

Itraconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Itraconazole is an imidazole/triazole-type antifungal agent. Itraconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation via the inhibition of the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol and is required in fungal cell wall synthesis. The subsequent loss of normal sterols correlates with the accumulation of 14 α-methyl sterols in fungi and may be partly responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Itraconazole exhibits in vitro activity against Cryptococcus neoformans and Candida spp. Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to Cryptococcus neoformans and for systemic infections due to Candida albicans.

Indications of Itraconazole

Systemic fungal infection
Candida urinary tract infections
Aspergillosis, aspergilloma
Aspergillosis, invasive
Blastomycosis
Candidemia
Coccidioidomycosis
Cryptococcal meningitis, immunosuppressed host
Cryptococcosis
Dermatophytosis
Esophageal candidiasis
Febrile neutropenia
Fungal infection prophylaxis
Histoplasmosis
Microsporidiosis
Onychomycosis, Fingernail
Onychomycosis, toenail
Oral thrush
Paracoccidioidomycosis
Sporotrichosis
Tinea capitis
Tinea versicolor
Vaginal yeast Infection
Aspergillosis
Blastomycosis
Chromomycosis
Coccidioidal meningitis
Dermatomycoses
Esophageal candidiasis
Histoplasmosis
Infections, fungal
Onychomycosis
Oropharyngeal candidiasis
Paracoccidioidomycosis
Penicillium marneffei infection
Pulmonary coccidiosis
Sporotrichosis
Vulvovaginal candidiasis
Disseminated Other specified protozoal diseases

Therapeutic Indications

For the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis.
Psittaciformes, Falconiformes, Accipitriformes, Strigiformes, and Anseriformes:
For the treatment of aspergillosis.
Also for the treatment of candidiasis.
Antimycotic active against infections caused by yeasts and fungi
Treatment of naevoid basal-cell carcinoma syndrome (Gorlin syndrome)
Itraconazole capsules are also indicated for the treatment of the following fungal infections in non-immunocompromised patients: Onychomycosis of the toenail, with or without fingernail involvement, due to dermatophytes (tinea unguium) and Onychomycosis of the fingernail due to dermatophytes (tinea unguium).
Itraconazole capsules are indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: Blastomycosis, pulmonary and extrapulmonary; Histoplasmosis, including chronic cavitary pulmonary disease and disseminated, non-meningeal histoplasmosis and Aspergillosis, pulmonary and extrapulmonary, in patients who are intolerant of or who are refractory to amphotericin B therapy.

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Contra Indications of Itraconazole

Have known hypersensitivity to other azole medicines such as itraconazole;
Are taking terfenadine, if 400 mg per day multidose of fluconazole is administered;
Concomitant administration of itraconazole and quinidine, especially when itraconazole is administered in high dosages;
Take SSRIs such as fluoxetine or sertraline.

Dosage of Itraconazole

Dosages may vary in the differant disease condition

INDICATIONS	DOSE	DURATION OF TREATMENT
Gynecological infections:
– Vulvovaginal candidosis	200 mg b.i.d. or 200 mg o.d.	1 day 3 days
Dematological/ophthalmic indications:
– Pityriasis versicolor	200 mg o.d.	7 days
– Tinea corporis, tinea cruris	100 mg o.d. or	15 days or
	200 mg o.d.	7 days¹
– Tinea pedis, tinea manuum	100 mg o.d.	30 days
– Oral candidiasis	100 mg o.d.	15 days

In some patients with compromised immune systems, such as neutropenic, AIDS or transplant patients, the bioavailability of oral itraconazole may be diminished. In these cases the dose may have to be doubled.

The length of treatment for systemic fungal infections should be dictated by the mycological and clinical response to therapy:

INDICATIONS	DOSE	AVERAGE DURATION	COMMENTS
Aspergillosis	200 mg o.d.	2-5 months	Increase dose to 200 mg b.i.d. in the case of widespread infection
Candidiasis	100-200 mg o.d.	3 weeks-7 months
Non-meningeal cryptococcosis	200 mg o.d.	10 weeks	Maintenance therapy (meningeal cases): 200 mg o.d.
Cryptococcal meningitis	200 mg b.i.d.	2 months – 6 months	Maintenance therapy (meningeal cases): 200 mg o.d.
Histoplasmosis	200 mg o.d.	8 months
	200 mg b.i.d.

Side Effects of Itraconazole

The most common

Abdominal or stomach pain
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
Nausea
liver problems,
stomach pain,
vomiting,
Dizziness
Burning, itching, stinging, redness, or other sign of irritation at the application site ,rash
a headache,
increased intracranial pressure,
meningeal signs,
reversible hair loss or thinning, and
fever.

Common

chills or fever
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
decreased amount of urine

Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
burning,
stinging,
severe pain in your upper stomach spreading to your back, nausea, and vomiting;
signs of congestive heart failure–shortness of breath (even with mild exertion), cough with mucus, fast heartbeats, swelling, rapid weight gain, sleep problems; or.

Drug Interactions of Itraconazole

Many drugs can interact with itraconazole, and some drugs should not be used together. Tell your doctor about all your current medicines and any you start or stop using, especially

an antibiotic;
antipsychotic medicine or a sedative;
an antiviral medicine to treat hepatitis C or HIV/AIDS;
medicine to prevent blood clots;
cancer medicine;
heart or blood pressure medication;
immunosuppressants, or medicine to prevent organ transplant rejection;
medicine to treat high cholesterol;
migraine headache medication;
narcotic (opioid) pain medicine;
seizure medicine; or
steroid medication.

Never take itraconazole if you

are taking any of the medicines listed below. Dangerous or even life-threatening abnormal heartbeats could result:

quinidine
dofetilide
cisapride
pimozide
methadone
levacetylmethadol

are taking any of the following medicines

lovastatin
simvastatin
midazolam
nisoldipine
felodipine
ergot alkaloids

have ever had an allergic reaction to itraconazole or any of the other ingredients in itraconazole. Ask your doctor or pharmacist for a list of these ingredients.

Pregnancy and lactation of Itraconazole

Itraconazole 100mg Capsules, hard must not be used during pregnancy except for life-threatening cases where the potential benefits to the mother outweigh the potential harm to the fetus

There is limited information on the use of itraconazole during pregnancy. During post-marketing experience, cases of congenital abnormalities have been reported. These cases included skeletal, genitourinary tract, cardiovascular and ophthalmic malformations as well as chromosomal and multiple malformations. A causal relationship with itraconazole has not been established.

Lactation

A very small amount of itraconazole is excreted in human milk. The expected benefits of itraconazole capsules therapy should, therefore, be weighed against the potential risk of breastfeeding. In case of doubt, the patient should not breastfeed. Women of childbearing potential taking Itraconazole 100mg Capsules, hard should use contraceptive precautions. Effective contraception should be continued until the menstrual period following the end of Itraconazole 100mg Capsules, hard therapy.