Alita

COMPOSITION

Each capsule contains

Itraconazole                             100mg

DISCRIPTION

Itraconazole is a fungistatic with broader spectrum of activity than ketocanazole or fluconazole including some moulds like aspergillus & mucor.

PHARMACOLOGY

Mechanism of action:-

Itraconazole impairs the synthesis of ergosterol, an integral part of fungal membrane by selectively binding to the fungal cytochrome P-450 14α demethylase enzyme, which is essential for converting lanosterol into ergosterol. Thus, ALITA inhibits fungal cell growth & replication.

Pharmacokinetics  :-

After oral administration rapidly absorbed, widely distributed in the body. CSF & salvia contains negligible amounts of the drug. It is extensively metabolized in liver & the metabolites are excreted in urine. Absorption rate is increased when taken with or just after fatty meal.

 After multiple dosing steady state concentrations reached in 14 days.Duration of action 3 – 4 days. Elimination half-life after single dose:  20hrs. multiple doses 30hrs.

Highest concentration in adipose tissue, skin, nails & vagina. Low levels in saliva, urine & CSF. Itraconazole is concentrated in the skin & nails secondary to its highly lipophilic nature. Absorption is promoted by a high fat content of administrated meal.Undergoes extensive hepatic metabolism. Plasma half life  20 – 60 hrs.

Plasma Protein binding  is 99.8%

Indication:-        

  Susceptible pathogens include

                                            1. Dermatophytes:-

i.              Microsporum

ii.                    Tinea

iii.                  Trichophyton

iv.                  Epidermophytone Species

             2. Yeasts:-

i               Candida

ii.                    Pityrosporum

iii.                  Cryptococcus neoformans

               3. Dimorphic fungi:-

i.              Histoplasma

ii.                    Blastomyces dermatitidis

iii.                  Paracocciodes brasiliensis

                                           

               4. Others including:-

i.                     Aspergillus fumigatus

5. As a prophylaxis:-

Itraconazole is also used in prophylaxis against opportunistic mycoses in HIV infected patients & those on imunosuppressant therapy.

Dosage  :-   General recommended dosage is 100 to 400mg for up to 6 month.

Oropharyngeal/Esophageal Candidiasis:- 100mg daily for 15 days. For AIDS or Neutropenia patient – 200mg daily for 15 days

Chronic Mucocutaneous Candidiasis:- 200mg daily for 6 months.

Invasive & Disseminative Candidiasis:- 200mg once or twice daily until disease is  controlled.

Vulvovaginal Candidiasis :- 200mg twice daily for 1 day.

Recurrent Vaginal Candidiasis:- 200mg for 3 days &  also on first day of    menses for 6  cycles.     

ALITA is the obvious choice over Fluconazole in vaginal candidiasis. Rapidly reaches the vaginal tissue & stay there.

Offers 96% cure rate in case of vaginal candidiasis whereas fluconazole has only 83% success rate.

Tinea Corporis & Tinea Cruris:-

          Either

              i. 100mg daily for 15 days.

                  Or

ii.                    200mg daily for 7 days

Tinea Pedis & Tinea manuum:-

Either

                      i. 100mg daily for 2 to 4 weeks (30 days)

            Or

ii. 200mg daily for 1 week per month for 3 to 4 months.

Regimens can be chosen & modified according to the severity of disease & degree of clinical response.

Onychomycosis:-

           Either 

i. 200mg OD for 3 months.

           Or

ii. An intermittent pulse regimen of 200mg BD for 7 days & subsequent course repeated after 21 days interval. For fingernails 2 pulses (courses) & for toenails 3 courses are sufficient.

Tinea Capitis:-

 3 to 5mg/kg/day for 4 to 6 weeks can be used to treat children with tinea capitis. Most children requires Alita 100mg cap per day for 4 to 6 weeks to achieve clinical & mycological cure.

Pityriasis Versicolor:-  200mg OD for 7 days.

Histoplasmosis:- 200mg. 1-2 times/days. Maintenance in AIDS patients 200mg OD, increased to 200mg BD if low plasma Itraconazole concentration.

Cryptococcosis including Criptococcal Meningitis:- 200mg twice daily for 6 weeks consolidation therapy and then 200mg once daily as maintenance therapy.

Aspergillosis:- 200mg thrice daily for 4 days as loading dose. And then 200mg twice daily for 4 months to 1 year as maintenance therapy.

Prophylaxis:-

Neutropenia:- 200 mg twice daily until symptoms are resolved and immune system  recovery has occurred.

Immunosuppressant therapy     200mg twice daily until                                  

          Chemotherapy                        

Transplant Recipients

 

Contraindications :- Pregnancy, Azole hypersensitivity, co-administration of Terfenadine or Astemazole with Itraconazole is contraindicated.

Special Precautions   :-         Lactation,hepatic impairment, safety & efficacy in children has not been established.

Adverse effects          :-                         

Nausea, vomiting, skin rash, dizziness (feeling of unsteadiness, usually accompanied by anxiety), depression, paraesthesia (abnormality of sensation), vertigo, pedaloedema, pruritus, fever & loss of libido. In higher doses may cause hypertension, gynaecomastia.

Drug Interactions    :-

Oral absorption of Itraconazole is reduced by antacids, H₂ Blockers and proton pump inhibitors. Rifampicin Phenobarbitone, Phenytoin & Carbamazepine induce Itraconazole metabolism and reduce its efficiency. Isoniazid reduces plasma levels. Effect of oral Hypoglycaemics increased. Corticosteroid bioavailability increased & clearance decreased resulting in toxicity. Increased level of cyclosporine-A leads to nephrotoxicity. Facial flushing & nausea seen with concomitant ingestion of alcohol.