ITRACONAZOLE CAPSULES USE
Solution formulation. Most studies examining the efficacy of itraconazole solution have been in patients with impaired immunity. 13,55,56,57,58,59,60,61 Two large comparative studies with fluconazole (Table III) were in HIV-positive patients with oral (n = 244),57 or oropharyngeal (n = 190)58 candidosis: 14 days of itraconazole solution was at least as effective as fluconazole in effecting a clinical response (≥87%). In a further study of 126 immunocompromised patients with oesophageal candidosis, itraconazole solution and fluconazole led to a clinical response in 94% and 91% of cases, respectively.60 A comparative study examining the prophylactic use of itraconazole solution and fluconazole in 445 patients who were expected to be neutropenic following chemotherapy demonstrated that both agents prevent fungal infections in most cases (>97%).59
Peak plasma concentrations of itraconazole are reached within 2 to 5 hours following oral administration. As a consequence of non-linear pharmacokinetics, itraconazole accumulates in plasma during multiple dosing. Steady-state concentrations are generally reached within about 15 days, with Cmax values of 0.5 μg/mL, 1.1 μg/mL and 2.0 μg/mL after oral administration of 100 mg once daily, 200 mg once daily and 200 mg b.i.d., respectively. The terminal half-life of itraconazole generally ranges from 16 to 28 hours after single dose and increases to 34 to 42 hours with repeated dosing. Once treatment is stopped, itraconazole plasma concentrations decrease to an almost undetectable concentration within 7 to 14 days, depending on the dose and duration of treatment. Itraconazole mean total plasma clearance following intravenous administration is 278 mL/min. Itraconazole clearance decreases at higher doses due to saturable hepatic metabolism.
Its use in dogs, small mammals, and some exotics to treat fungal infections is 'off label' or 'extra label'. Use of the human version of this drug is 'off label' or 'extra label' in both cats and dogs. Many drugs are commonly prescribed for off label use in veterinary medicine. In these instances, follow your veterinarian’s directions and cautions very carefully as their directions may be significantly different from those on the label.
It has been experimentally demonstrated that as the pellets in each unit increase, the dissolution rate also increases. Pellet number within a capsule would directly depend on the pellet size and determines the surface area presented for absorption in the gastrointestinal (GI) tract. Thus, smaller pellets would result in larger pellet numbers as seen in our analysis (r = −0.848, P < 0.0001). On the same lines, we observed a significant difference (with P < 0.0001) in average pellet size of brands with >500 pellets versus those with <300 pellets, with significantly smaller pellets in the former . A similar statistically significant difference was also found in the average sizes of pellets among the brands with 300–500 pellets and those with <300 pellets. Brands 7 and 16 had unusually big pellets (1571 and 1845 μm) leading to very low pellet counts of 121 and 135, respectively.
Itraconazole was found to cause a dose-related increase in maternal toxicity, embryotoxicity, and teratogenicity in rats at dosage levels of approximately 40-160 mg/kg/day (5-20 times the MRHD), and in mice at dosage levels of approximately 80 mg/kg/day (10 times the MRHD). Itraconazole has been shown to cross the placenta in a rat model. In rats, the teratogenicity consisted of major skeletal defects; in mice, it consisted of encephaloceles and/or macroglossia.
If you suspect an overdose or an adverse reaction to the medication, call your veterinary office immediately. If they are not available, follow their directions in contacting an emergency facility.
This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). Alcohol may also increase the risk of serious liver problems.
ITRACONAZOLE belongs to a class of drugs called antifungals used to treat fungal infections of the mouth, throat, toenails, fingernails or lungs. Fungal infection is a disease in which a fungus attacks the tissue and causes infection. Fungal infections may be contagious (spread from one person to another).
As per the cost, nine brands had a per-capsule price of more than Rs. 20 rupees, whereas 11 were between Rs. 10 and 20 and only 2 below Rs. 10. Considering a dosage of 100 mg once a day, the cost of a standard 15 day treatment would fall between Rs. 180 and Rs 1215. And the treatment dosages and durations being given by many are much higher than the approved doses. Furthermore, use of 200 mg and higher dose capsule formulations (amply available in the Indian market) in this regard may produce suboptimal response. This is because keeping the same pellet size and technology, a 200-mg drug load formulation would require a much larger capsule size. The change in pellet size by altering the drug–polymer ratio or removing PEG 20000 layer leads to instable formulations with a negative impact on bioavailability.
Many things can affect the dose of a medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.
Special patient populations. The volume of distribution and clearance of fluconazole are greater in children than in adults;19 a relatively high mg/kg dose of fluconazole is therefore necessary in young patients. For those aged greater than 4 weeks, once daily dosing is appropriate. Neonates (aged ≤4 weeks) excrete fluconazole slowly, and less frequent dosing is therefore desirable. 19,20 The pharmacokinetics of fluconazole in the elderly are similar to those in non-elderly adults.15 Immune status has no effect on the pharmacokinetics of fluconazole in either adultsor children. 7,21,22
Itraconazole showed no evidence of carcinogenicity potential in mice treated orally for 23 months at dosage levels up to 80 mg/kg/day (approximately 10 times the maximum recommended human dose ). Male rats treated with 25 mg/kg/day (3.1 times the MRHD) had a slightly increased incidence of soft tissue sarcoma. These sarcomas may have been a consequence of hypercholesterolemia, which is a response of rats, but not dogs or humans, to chronic itraconazole administration. Female rats treated with 50 mg/kg/day (6.25 times the MRHD) had an increased incidence of squamous cell carcinoma of the lung (2/50) as compared to the untreated group. Although the occurrence of squamous cell carcinoma in the lung is extremely uncommon in untreated rats, the increase in this study was not statistically significant.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how the medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.
Dosage Guidelines & TipsHow to take Itraconazole (Sporanox)?Use Itraconazole (Sporanox) exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.Do not share this medicine with another person, even if they have the same symptoms you have.The itraconazole capsule should be taken with food.Swallow the capsule whole and do not crush, chew, break, or open it.Take itraconazole oral solution (liquid) on an empty stomach, at least 1 hour before or 2 hours after a meal. Swish the liquid in your mouth for several seconds before swallowing it.Measure liquid medicine carefully. Use the dosing syringe provided, or use a medicine dose-measuring device (not a kitchen spoon).The Sporanox PulsePak has a special dosing schedule that includes not taking the medicine for several days in a row.
Follow all dosing instructions carefully.Itraconazole capsules should not be used in place of itraconazole oral solution (liquid) if that is what your doctor has prescribed. Avoid medication errors by using only the form and strength your doctor prescribes.If you also take a stomach acid reducer (Tagamet, Pepcid, Axid, Zantac, and others), take itraconazole with an acidic drink such as non-diet cola.Use this medicine for the full prescribed length of time, even if your symptoms quickly improve. Skipping doses can increase your risk of infection that is resistant to medication. Itraconazole will not treat a viral infection such as the flu or a common cold.You may need frequent medical tests.Store at room temperature away from moisture, heat, and light.What should I do if I missed a dose of Itraconazole (Sporanox)?Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.
