Generic Name

Fluticasone

Brand Name

Flutizox®

Dosage Form

Metered-dose inhaler

Strength

50, 125, 250 mcg/dose

Indication

Fluticasone is a corticosteroid indicated in the treatment of corticosteroid responsive dermatoses, asthma, and COPD.
Fluticasone's 2 esters are indicated as inhalers for the treatment and management of asthma by prophylaxis as well as inflammatory and pruritic dermatoses. A 
Fluticasone propionate nasal spray is indicated for managing nonallergic rhinitis while the Fluticasone furoate nasal spray is indicated for treating season and perennial allergic rhinitis.

Recommended Dose:

Dosage of any medicine is determined by your physician.

The recommended dosage of this medicine is as follows:

· Adults and children 16 years or older; 100 - 500 mcg, twice a day.

· Children 4 to 16 years old; 50 – 100 mcg, twice a day.

· Children less than 4 years old; medicine safety for the patient and dosage must be determined by physician.

Missed Dose

If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.

Route of Elimination
Fluticasone furoate is eliminated ≥90% in the feces and 1-2% in the urine.

Fluticasone propionate is mainly eliminated in the feces with <5% eliminated in the urine.

Half- life

15.1 hours for intranasal Fluticasone furoate and 24 hours for the inhaled formulation. A study of 24 healthy Caucasian males showed a half-life of 13.6 hours following intravenous administration and 17.3-23.9 hours followed inhalation.

7.8 hours for intravenous Fluticasone propionate. A study of 24 healthy Caucasian males shows a half-life of 14.0 hours following intravenous administration and 10.8 hours following inhalation.

Clearance

57.8L/h for Fluticasone furoate. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration.

1093mL/min for Fluticasone propionate. A study of 24 healthy Caucasian males showed a clearance of 63.9L/h following intravenous administration.

Toxicity
Fluticasone furoate administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studies. Fluticasone furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanisms. Fluticasone furoate is not associated with carcinogenicity, mutagenicity, or impairment of fertility. There are no well controlled studies in pregnancy or lactation though animal studies have shown teratogenicity and hypoadrenalism in the offspring of treated mothers and other corticosteroids are known to be excreted in breast milk. Generally, there are no reported adverse effects with fluticasone in pregnancy. Pediatric patients should be given the lowest possible dose and monitored for reduction in growth velocity. There is insufficient evidence to determine whether geriatric patients respond differently to other patients. Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patients. Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatment.

Fluticasone propionate's use in specific populations has not been well studied. Fluticasone propionate is not carcinogenic, mutagenic, or clastogenic, nor did it affect fertility in animal studies. Subcutaneous Fluticasone propionate has been shown to produce teratogenic effects in rats though oral administration does not. Generally, there are no reported adverse effects with fluticasone in pregnancy. Fluticasone propionate in human milk may cause growth suppression, effects on endogenous corticosteroid production, or other effects. Pediatric patients treated with Fluticasone propionate ointment experienced adrenal suppression. Geriatric patients treated with Fluticasone propionate did not show any difference in safety or efficacy compared to other patient groups, though older patients may be more sensitive to adverse effects. There is no difference in the clearance of Fluticasone propionate across genders or race. Patients with hepatic impairment should be closely monitored due to the elimination mechanism.

Pregnancy and Lactation

Teratogenic Effects: Pregnancy Category C. Subcutaneous studies in the mouse and rat at 45 and 100 mcg/kg, respectively (approximately 1/10 and 1/2 the maximum human daily inhalation dose based on mcg/m2, respectively), revealed fetal toxicity characteristic of potent glucocorticoid compounds, including embryonic growth retardation, omphalocelecleft palate, and retarded cranial ossification.

In the rabbit, fetal weight reduction and cleft palate were observed following subcutaneous doses of 4 mcg/kg (approximately 1/25 the maximum human daily inhalation dose based on mcg/m2). However, following oral administration of up to 300 mcg/kg (approximately 3 times the maximum human daily inhalation dose based on mcg/m2) of fluticasone propionate to the rabbit, there were no maternal effects nor increased incidence of external, visceral, or skeletal fetal defects. No fluticasone propionate was detected in the plasma in this study, consistent with the established low bioavailability following oral administration.

Less than 0.008% of the administered dose crossed the placenta following oral administration of 100 mcg/kg to rats or 300 mcg/kg to rabbits (approximately 1/2 and 3 times the maximum human daily inhalation dose based on mcg/m2, respectively).

There are no adequate and well-controlled studies in pregnant women. Fluticasone propionate Inhalation Aerosol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Experience with oral glucocorticoids since their introduction in pharmacologic, as opposed to physiologic, doses suggests that rodents are more prone to teratogenic effects from glucocorticoids than humans. In addition, because there is a natural increase in glucocorticoid production during pregnancy, most women will require a lower exogenous glucocorticoid dose and many will not need glucocorticoid treatment during pregnancy.

Interactions with medicines

Interaction reports for fluticasone and the medicines listed below;

· Fluticasone / Salmeterol

· Aspirin

· Diphenhydramine

· Duloxetine

· Fish Oil (omega-3 polyunsaturated fatty acids)

· Atorvastatin

· Pregabalin

· Metoprolol Tartrate (metoprolol)

· Polyethylene glycol 3350

· Albuterol

· Montelukast

· Tiotropium

· Budesonide / Formoterol)

· Levothyroxine)

· Acetaminophen

· Vitamin B12 (cyanocobalamin)

· Vitamin C (ascorbic acid)

· Vitamin D3 (cholecalciferol)

· Cetirizine

Precautions

During withdrawal from oral corticosteroids, some patients may experience symptoms of systemically active corticosteroid withdrawal, e.g., joint and/or muscular pain, lassitude, and depression, despite maintenance or even improvement of respiratory function.

Fluticasone propionate will often permit control of asthma symptoms with less suppression of HPA function than therapeutically equivalent oral doses of prednisone. Since fluticasone propionate is absorbed into the circulation and can be systemically active at higher doses, the beneficial effects of Fluticasone propionate Inhalation Aerosol in minimizing HPA dysfunction may be expected only when recommended dosages are not exceeded and individual patients are titrated to the lowest effective dose. A relationship between plasma levels of fluticasone propionate and inhibitory effects on stimulated cortisol production has been shown after 4 weeks of treatment with Fluticasone propionate Inhalation Aerosol. Since individual sensitivity to effects on cortisol production exists, physicians should consider this information when prescribing fluticasone propionate Inhalation Aerosol.

Because of the possibility of systemic absorption of inhaled corticosteroids, patients treated with these drugs should be observed carefully for any evidence of systemic corticosteroid effects. Particular care should be taken in observing patients postoperatively or during periods of stress for evidence of inadequate adrenal response.

It is possible that systemic corticosteroid effects such as hypercorticism and adrenal suppression (including adrenal crisis) may appear in a small number of patients, particularly when Fluticasone propionate Inhalation Aerosol is administered at higher than recommended doses over prolonged periods of time. If such effects occur, fluticasone propionate inhalation aerosol should be reduced slowly, consistent with accepted procedures for reducing systemic corticosteroids and for management of asthma symptoms.

A reduction of growth velocity in children or teenagers may occur as a result of inadequate control of chronic diseases such as asthma or from use of corticosteroids for treatment. Physicians should closely follow the growth of adolescents taking corticosteroids by any route and weigh the benefits of corticosteroid therapy and asthma control against the possibility of growth suppression if an adolescent s growth appears slowed.

The long-term effects of fluticasone propionate in human subjects are not fully known. In particular, the effects resulting from chronic use of fluticasone propionate on developmental or immunologic processes in the mouthpharynxtrachea, and lung are unknown. Some patients have received fluticasone propionate inhalation aerosol on a continuous basis for periods of 3 years or longer. In clinical studies with patients treated for nearly 2 years with inhaled fluticasone propionate, no apparent differences in the type or severity of adverse reactions were observed after long- versus short-term treatment.

Rare instances of glaucoma, increased intraocular pressure, and cataracts have been reported following the inhaled administration of corticosteroids, including fluticasone propionate.

In clinical studies with inhaled fluticasone propionate, the development of localized infections of the pharynx with Candida albicans has occurred. When such an infection develops, it should be treated with appropriate local or systemic (i.e., oral antifungal) therapy while remaining on treatment with Fluticasone propionate Inhalation Aerosol, but at times therapy with Fluticasone propionate Inhalation Aerosol may need to be interrupted.

Inhaled corticosteroids should be used with caution, if at all, in patients with active or quiescent tuberculosis infection of the respiratory tract; untreated systemic fungalbacterialviral or parasitic infections; or ocular herpes simplex.

Side effects

Common side effects of Flutizox® include:

· Hoarseness,

· Throat irritation,

· Headache,

· Dryness in your mouth/nose/throat,

· White patches or sores inside your mouth or on your lips,

· Stuffy nose,

· Sinus pain,

· Cough

· Deepened voice.

Tell your doctor if you have serious side effects of Flutizox® including:

· Signs of infection (such as fever, chills, persistent sore throat),

· Vision problems,

· Increased thirst or urination,

· Easy bruising or bleeding,

· Mental/mood changes (such as depression, mood swingsagitation), or

· Bone pain.

Contraindications

Fluticasone propionate Inhalation Aerosol is contraindicated in the primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required.

Storage

Store the canister at room temperature, away from heat and direct light. Do not freeze. Do not keep this medicine inside a car where it could be exposed to extreme heat or cold. Do not poke holes in the canister or throw it into a fire, even if the canister is empty.


6.1.7.0
گروه دورانV6.1.7.0