2. ORAL ANTIFUNGAL
MICONAZOLE
• Overview
• Miconazole (Nitrate) is imidazole-type antifungal. When miconazole was first
released, it was hoped it would replace amphotericin B as a parenteral antifungal
agent. It was soon discovered, however, that miconazole not only failed to offer the
same efficacy as amphotericin B, but also possessed intrinsic toxicities after IV
administration.
• While miconazole is still marketed in a parenteral formulation, it most commonly is
used topically and intravaginally. Miconazole was approved by the FDA in 1974it
was one of the first azole antifunfal agent to become widely used for treating
mycoses. Miconazole (Nitrate) is a topically used azole.
• Like other azole antifungals, miconazole exerts its effect by altering the fungal cell
membrane. Miconazole inhibits ergosterol synthesis by interacting with 14a
demethylase, a cytochrome P-450 enzyme that is necessary for the conversion of
lanosterol to ergosterol, an essential component of the membrane. Inhibition of
ergosterol synthesis results in increased cellular permeability, causing leakage of
cellular contents. Miconazole does not appear to have the same effect on human
cholesterol synthesis.
3. • Miconazole is the derivative of Miconazole
(Nitrate)Miconazole is the derivative of Miconazole
(Nitrate) It is of Synthetic origin and belongs to
Azole. It belongs to Antifungals pharmacological
group.
• Indications
• Miconazole (Nitrate) is primarily indicated in
conditions like Balanitis, Candidosis, Fungal
infection, Vulvo-vaginal candidosis.
4. • Contraindications
• Miconazole (Nitrate) is contraindicated in conditions like Hypersensitivity
to any component of product.
• Side Effects
• The severe or irreversible adverse effects of Miconazole (Nitrate), which
give rise to further complications include Cardiac arrhythmias, Hepatitis,
Cardiac arrhythmias, Phlebitis, Pruritis, Arachnoiditis.
• Miconazole (Nitrate) produces potentially life-threatening effects which
include Cardiac Arrest, Cardiac arrest, Anaphylaxis. which are
responsible for the discontinuation of Miconazole (Nitrate) therapy.
• The signs and symptoms that are produced after the acute overdosage of
Miconazole (Nitrate) include Vomiting, Diarrhea, Arrhythmias.
• The symptomatic adverse reactions produced by Miconazole (Nitrate) are
more or less tolerable and if they become severe, they can be treated
symptomatically, these include Drowsiness, Anorexia, Rashes, GI upset,
Flushing, Nausea and vomiting, Local irritation.
5. • Dosage
• Miconazole (Nitrate)'s dosage details are as
follows: Dose Single Dose Frequency Route
Instructions
• Adult Dosage
• 2 % As recommended.OphthalmicAs
required.250 mg 6 hourly PO 100 mg24 hourly
Rectal For 14 days.2 % 24 hourly Topical
Once daily
6. • Storage Conditions
• Cream, Vag Supositories, Powder
• Store Below 40°C. Do not Freeze. Protect
from Sunlight and Moisture.
7. ITRACONAZOLE
• Overview
• Itraconazole is a broad-spectrum antifungal agent for oral
treatment of vulvovaginal candidiasis, pityriasis versicolor and
dermatophytoses.itraconazole is a substituted triazole
derivetive.itraconazoleactive against many Candida species,
endemic mycoses and dermatophytes.
• Itraconazole is the most potent of available azoles, but effectiveness
can be limited by reduced bioavailabilty. The requirement for
intravenous administration and the toxicity of the older antifungal
agents created a need for antifungal agents with a better therapeutic
profile.
• The relatively non-toxic oral azole medications represent the first
major advance in this direction. Since their introduction in the
1980s, these medications have played an increasingly important role
in the systemic therapy of fungal disease.
8. • Primary Characterstics
• Itraconazole also known as Oriconazole. Itraconazole also known as
Oriconazole. It is of Synthetic origin and belongs to Triazole. It belongs to
Antifungals pharmacological group.
• Indications
• Itraconazole is primarily indicated in conditions like Advanced breast or
prostate cancer, Antifungal prophylaxis, Candidiasis, Cryptcoccal
meningitis, Dermatophytic infections, Histoplasmosis, Oculomycoses,
Onychomycoses, Oral candidiasis, Oropharangeal candidiasis,
Orophyrangeal candidiasis, Pityriasis versicolor, Sporotrichosis, Superficial
candidiasis, Systemic mycoses, Tinea pedis, Tinae manuum, To reduce
intestinal secretions and vomiting, To reduce intestinal secretions and
vomiting (palliative care), and can also be given in adjunctive therapy as an
alternative drug of choice in Cushing`s syndrome due to malignant disease,
Fungal keratitis, Leishmaniasis, Vulvo-vaginal candidosis.
9. • Side Effects
• The severe or irreversible adverse effects of Itraconazole, which give rise to
further complications include Hypotension, Hepatitis, Hypotension.
• Itraconazole produces potentially life-threatening effects which include
Dysrhythrics. which are responsible for the discontinuation of Itraconazole
therapy.
• The signs and symptoms that are produced after the acute overdosage of
Itraconazole include Constipation, Gastritis, Depression.
• The symptomatic adverse reactions produced by Itraconazole are more or
less tolerable and if they become severe, they can be treated
symptomatically, these include Dizziness, Vertigo, Headache, Fatigue,
Nausea, Vomiting, Diarrhea, Abdominal pain, Pruritus, Hallucination,
Somnolence, Hair loss, Edema, Photophobia, Vasculitis, dizziness.
10. • Dosage
• Itraconazole's dosage details are as follows:
Dose Single Dose Frequency Route
Instructions
• Adult Dosage
• 200 mg 24 hourlyPO For a Week
11. • Warning / Precautions
• Itraconazole should be used with caution in patients with allliver
disease, heart rhythm disorders (arrhythmias) and of any drug
ergies. It should be used with caution while engaging in activities
requiring alertness because this medication causes dizziness or
drowsiness. It should be used only when clearly needed during
pregnancy or lactation.
• Safe use of itraconazole in the children under the age 16 has not
been established. The drug should be used with caution in the
patients with azole hypersensitivity. Patients who develop abnormal
liver function tests during itraconazole therapy should be monitored
and therapy discontinued if symptoms of the liver disease develop.
Should not be administered to treat onchonycosis in pateints with
ventricular dysfurution.
12. • Storage Conditions
• Caps
• Store Between 15°C-30°C. Protect from
Sunlight, Moisture and Heat.
• Soln
• Store at room temperature, Below 25°C. Do
not Freeze. Protect from Sunlight and Heat.
13. Voriconzaole
• Overview
• Voriconazole is a triazole antifungal agent.
Voriconazole is designated chemically as (2R,3S)-
2-(2,4-difluorophenyl)-3-(5-fluoro-4
pyrimidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol.
• It is available as a lyophilized powder for solution
for intravenous infusion, film-coated tablets for
oral administration, and as a powder for oral
suspension.
14. • Primary Characterstics
• It is of Synthetic origin and belongs to
phenylpropylamines. It belongs to Antifungals
pharmacological group.
• Indications
• VORICONAZOLE is primarily indicated in
conditions like candidemia, Candidiasis,
Invasive aspergillosis.
15. • Side Effects
• The symptomatic adverse reactions produced
by VORICONAZOLE are more or less
tolerable and if they become severe, they can
be treated symptomatically, these include
Headache, Nausea, Vomiting, Fever,
Tachycardia, Chills, Hallucination, Visual
disturbances, Rash, Tachycardia.
16. • Dosage
• VORICONAZOLE's dosage details are as
follows: Dose Single Dose Frequency Route
Instructions
• Adult Dosage
• 0 to 6 mg/kg 2 hourly IV100 mg 2 hourlyPO
less than 40 kg 200 mg 2 hourly PO (40 kg or
more)
17. • Warning / Precautions
• Hepatic Toxicity: Serious hepatic reactions reported. Evaluate liver
function tests at start of and during voriconazole therapy. Visual
Disturbances (including optic neuritis and papilledema): Monitor visual
function if treatment continues beyond 28 days.
• Embryo-Fetal Toxicity: Do not administer to pregnant women unless the
benefit to the mother outweighs the risk to the fetus. Inform pregnant
patient of hazard.
• Patients with Hereditary Galactose Intolerance Lapp Lactase Deficiency or
Glucose-Galactose Malabsorption: Do not use. Arrhythmias and QT
Prolongation: Correct potassium, magnesium and calcium prior to use;
caution patients with proarrhythmic conditions. Infusion Related Reactions
(including anaphylaxis): Stop the infusion. Dermatological Reactions:
Discontinue for exfoliative cutaneous reactions or phototoxicity. Avoid
sunlight due to risk of photosensitivity.Skeletal Events: Fluorosis and
periostitis with long-term voriconazole therapy. Discontinue if these events
occur
