Drug Information

  





Itraconazole



   










 

Pharmacokinetics



After oral administration, it
is widely distributed in the body. C.S.F. and saliva contain negligible
amounts of the drug. It is extensively metabolised in liver and the
metabolites are excreted in urine.


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Indication
& Dosage



 

Oral

CANDIDIASIS-ORAL, VAGINAL. SYSTEMIC, CHRONIC MUCOCUTANEOUS.CRYPTOCOCCAL
INFECTIONS INCLUDING MENINGITIS COCCIDIOIDOMYCOSIS AND
PARACOCCIDIOIDOMYCOSIS AND PARACOCCIDIOIDOMYCOSIS. TINEA,  PITYRIASIS,
VERSICOLOR. SEBOPOSRIASIS, ONYCOMYCOSIS. SPOROTRICHOSIS, CHROMOMYCOSIS,
BLASTOMYCOSIS, HISTOPLASMOSIS, ASPERGILLOSIS, FUNGAL KERATITIS. CUTANEIOUS
LEISHMANIASIS:
100-400mg for upto 6 months. Children: Safety not
adequately established but doses of 100mg/day for systemic fngal
infections have been used in 3-16 years old children. Elderly: No change
in dosage. For onychomycosis pulse therapy currently adovacated. See lit

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Action


 



Potent inhibitor of human
fungal pathogens. Susceptible pathogens include dermatophytes (Microsporum,
Tinea, Trichophyton and Epidermophyton species), Yeasts (Candida,
Pityrosporum, Cryptococcus neofromans), dimorphic fungi (Histoplasma,
Blastomyces dermatitidis, Paracocciodes brasiliensis) and others including
Aspergillus fumigatus.

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Interactions

 


Enzyme-inducing drugs
such as rifampicin, carbamazepine, phenytoin, or phenobarbitone
may decrease plasma concentrations of itraconazole. Concomitant
administration of drugs that reduce stomach acidity, such as
antimuscarinics, antacids, proton pump inhibitors, and histamine
H(2)-receptor antagonists, may reduce the absorption of
itraconazole.

Itraconazole may interfere with drugs metabolised by hepatic
microsomal enzymes, especially cytochrome P450 (CYP3A4), hence the
warnings that plasma concentrations of astemizole, cisapride,
cyclosporin, felodipine, statins such as lovastatin or simvastatin,
midazolam, quinidine, terfenadine, triazolam, and warfarin may be
increased. Concentrations of HIV-protease inhibitors such as
indinavir or ritonavir may also be increased; itraconazole plasma
concentrations may be increased in turn. The effects of digoxin
and of vincristine may be increased by itraconazole but the
efficacy of oral contraceptives might be reduced.

There is a risk of cardiac arrhythmias if itraconazole is used
concomitantly with astemizole, cisapride, or terfenadine and such
combinations should be avoided.

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Adverse
Effect & Precautions


 


Nausea, vomiting, skin
rash, dizziness, depression, paraesthesia, vertigo, pedal oedema
and loss of libido.



Precaution: Hepatic impairment. Safety and efficacy in children
has not been established.

Pregnancy: Contraindicated.

Breast Feeding: Contraindicated.

Man: Not recommended.

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Brands available in market :












 

 

 

 


CANDITRAL


Glenmark


CAPS


100mg


4


136.17


ITASPOR


Intas


CAPS


100mg


4


131.50


SPORANOX


Johnson & Johnson


CAPS


100mg


10


173.00

 

 

 

 


Top


    



 






 

     

  
Drug Information
  


Itraconazole
   

 
Pharmacokinetics

After oral administration, it is widely distributed in the body. C.S.F. and saliva contain negligible amounts of the drug. It is extensively metabolised in liver and the metabolites are excreted in urine.

Top
   

Indication & Dosage
 
Oral
CANDIDIASIS-ORAL, VAGINAL. SYSTEMIC, CHRONIC MUCOCUTANEOUS.CRYPTOCOCCAL INFECTIONS INCLUDING MENINGITIS COCCIDIOIDOMYCOSIS AND PARACOCCIDIOIDOMYCOSIS AND PARACOCCIDIOIDOMYCOSIS. TINEA,  PITYRIASIS, VERSICOLOR. SEBOPOSRIASIS, ONYCOMYCOSIS. SPOROTRICHOSIS, CHROMOMYCOSIS, BLASTOMYCOSIS, HISTOPLASMOSIS, ASPERGILLOSIS, FUNGAL KERATITIS. CUTANEIOUS LEISHMANIASIS:
100-400mg for upto 6 months. Children: Safety not adequately established but doses of 100mg/day for systemic fngal infections have been used in 3-16 years old children. Elderly: No change in dosage. For onychomycosis pulse therapy currently adovacated. See lit

Top
  

Action
 

Potent inhibitor of human fungal pathogens. Susceptible pathogens include dermatophytes (Microsporum, Tinea, Trichophyton and Epidermophyton species), Yeasts (Candida, Pityrosporum, Cryptococcus neofromans), dimorphic fungi (Histoplasma, Blastomyces dermatitidis, Paracocciodes brasiliensis) and others including Aspergillus fumigatus.

Top
  

Interactions
 

Enzyme-inducing drugs such as rifampicin, carbamazepine, phenytoin, or phenobarbitone may decrease plasma concentrations of itraconazole. Concomitant administration of drugs that reduce stomach acidity, such as antimuscarinics, antacids, proton pump inhibitors, and histamine H(2)-receptor antagonists, may reduce the absorption of itraconazole.
Itraconazole may interfere with drugs metabolised by hepatic microsomal enzymes, especially cytochrome P450 (CYP3A4), hence the warnings that plasma concentrations of astemizole, cisapride, cyclosporin, felodipine, statins such as lovastatin or simvastatin, midazolam, quinidine, terfenadine, triazolam, and warfarin may be increased. Concentrations of HIV-protease inhibitors such as indinavir or ritonavir may also be increased; itraconazole plasma concentrations may be increased in turn. The effects of digoxin and of vincristine may be increased by itraconazole but the efficacy of oral contraceptives might be reduced.
There is a risk of cardiac arrhythmias if itraconazole is used concomitantly with astemizole, cisapride, or terfenadine and such combinations should be avoided.

Top
    

Adverse Effect & Precautions
 

Nausea, vomiting, skin rash, dizziness, depression, paraesthesia, vertigo, pedal oedema and loss of libido.

Precaution: Hepatic impairment. Safety and efficacy in children has not been established.
Pregnancy: Contraindicated.
Breast Feeding: Contraindicated.
Man: Not recommended.

Top
  

Brands available in market :

 

 

 

 

CANDITRAL

Glenmark

CAPS

100mg

4

136.17

ITASPOR

Intas

CAPS

100mg

4

131.50

SPORANOX

Johnson & Johnson

CAPS

100mg

10

173.00

 

 

 

 

Top
    

 

 

By |2022-07-20T16:42:57+00:00July 20, 2022|Uncategorized|Comments Off on Itraconazole

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