Fluticasone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Inhalation/Respiratory
Asthma prophylaxis
Adult: As fluticasone propionate dry powder or metered dose inhaler: Mild asthma: Initially, 100 mcg bid. Moderate and severe asthma: Initially, 250-500 mcg bid, may be increased up to 1,000 mcg bid based on individual response. As fluticasone propionate nebule: 500-2,000 mcg bid. As fluticasone furoate dry powder inhaler: Initially, 100 mcg once daily, may be increased to 200 mcg once daily if necessary. The dosage may be increased until control is achieved or reduced to the minimum effective dose according to the individual response.
Child: As fluticasone propionate dry powder or metered dose inhaler: 4-16 years Initially, 50-100 mcg bid, may be increased up to 200 mcg bid if nescessary. As fluticasone propionate nebule: 4-16 years 1,000 mcg bid. As fluticasone furoate dry powder inhaler: 5-<12 years 50 mcg once daily. ≥12 years Same as adult dose. The dosage may be increased until control is achieved or reduced to the minimum effective dose according to the individual response.

Nasal
Nasal polyps
Adult: As fluticasone propionate drops: Instill 200 mcg into each nostril 1 or 2 times daily for at least 4-6 weeks.
Child: ≥16 years Same as adult dose.

Nasal
Allergic rhinitis
Adult: As fluticasone propionate 0.05% spray: 100 mcg into each nostril once daily preferably in the morning, may be increased to bid as necessary. Maintenance dose: 50 mcg into each nostril once daily. As fluticasone furoate spray: Initially, 55 mcg into each nostril once daily, may be reduced to 27.5 mcg into each nostril once daily when maximum benefit and symptom control has been achieved. All doses must be titrated down to the lowest effective dose to maintain adequate control of symptoms.
Child: As fluticasone propionate 0.05% spray: 4-11 years 50 mcg into each nostril once daily preferably in the morning, may be increased to bid as necessary. Max: 100 mcg into each nostril daily. >12 years Same as adult dose. As fluticasone furoate spray: 6-11 years Initially, 27.5 mcg into each nostril once daily, may be increased to 55 mcg into each nostril once daily if necessary to control symptoms. Doses may be reduced back to 27.5 mcg into each nostril once daily when adequate symptom control has been achieved. ≥12 years Same as adult dose. All doses must be titrated down to the lowest effective dose to maintain adequate control of symptoms.

Topical/Cutaneous
Corticosteroid-responsive dermatoses
Adult: As 0.05% cream or 0.005% ointment: Apply thinly and rub gently to the affected area 1 or 2 times daily for up to 4 weeks until improvement occurs, then reduce frequency of application or change treatment to a less potent preparation. Re-evaluate treatment and diagnosis if condition worsens or does not improve within 4 weeks.
Child: In patients with atopic dermatitis who are unresponsive to lower potency corticosteroids: As 0.05% cream, 0.005% ointment, or 0.05% lotion: ≥3 months Apply thinly and rub gently to the affected area 1 or 2 times daily for 1-2 weeks. If condition has been controlled, may reduce frequency of application to the lowest effective dose for the shortest possible time. Withdraw treatment and reassess diagnosis if no improvement is seen within 1-2 weeks.
Hướng dẫn pha thuốc
Nebule: May be diluted with sterile 0.9% NaCl solution if necessary.
Chống chỉ định
Oral inhalation: Primary treatment of status asthmaticus or other acute asthma episodes requiring intensive measures. Nasal: Treatment of asthma, current or recent nasal septal ulcers, surgery, injury or trauma that is not fully healed. Topical: Untreated cutaneous infections, rosacea, acne vulgaris, perioral dermatitis, perianal and genital pruritus, pruritus without inflammation; dermatoses including dermatitis and nappy rash in infants <3 months.
Thận trọng
Patients with COPD, diabetes mellitus, ocular disease (e.g. cataracts, glaucoma), major risk factors for decreased bone mineral count (e.g. prolonged immobilisation, family history of osteoporosis, postmenopausal status, tobacco use, advanced age, poor nutrition); infections (e.g. ocular herpes simplex, active or quiescent respiratory tract TB; viral, fungal, bacterial, or parasitic systemic infections); psoriasis, history of local hypersensitivity to other corticosteroids (topical). Avoid abrupt withdrawal. Hepatic impairment. Children. Pregnancy and lactation.
Phản ứng phụ
Significant: Adrenal suppression (e.g. suppression of hypothalamic-pituitary-adrenal axis, hypercortisolism, Cushing’s syndrome), immunosuppression (prolonged use), pneumonia, local oropharyngeal candidiasis, local nasal effects (e.g. epistaxis, nasal septal perforation, ulceration, or erosion), visual disturbances (e.g. blurred vision, increased intraocular pressure, glaucoma, cataract, central serous chorioretinopathy), decreased bone mineral density, growth retardation in children, hyperglycaemia or glycosuria, delayed wound healing, localised reactions (e.g. skin atrophy), rebound of pre-existing dermatoses, withdrawal symptoms (e.g. joint/muscle pain, lassitude, depression). Rarely, vasculitis or other systemic eosinophilic conditions, psychological or behavioural effects in children (e.g. psychomotor hyperactivity, sleep disorders, anxiety, depression, aggression), hypersensitivity reactions (e.g. anaphylaxis, angioedema, bronchospasm, hypotension, contact dermatitis, rash, urticaria).
Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, toothache, dyspepsia.
General disorders and admin site conditions: Fatigue, malaise.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Headache, dizziness, unpleasant taste or smell.
Respiratory, thoracic and mediastinal disorders: Hoarseness, dysphonia, cough, sinusitis, nasopharyngitis, rhinalgia, nasal or throat dryness, irritation, burning and soreness.
Skin and subcutaneous tissue disorders: Pruritus, local skin burning, contusions, skin thinning, erythema, striae, pigmentation changes, hypertrichosis.
Vascular disorders: Hypertension.
Potentially Fatal: Paradoxical bronchospasm, adrenal insufficiency.
Inhalation/Respiratory/Nasal/Topical: C; Nasal: C
Thông tin tư vấn bệnh nhân
Topical: Do not apply on thin or broken skin, large surface area, or on occluded areas of the skin (e.g. intertriginous areas or under occlusive dressings).
MonitoringParameters
Monitor peak flow, FEV1, and other pulmonary function tests, LFTs; growth in children and adolescent via stadiometry. Assess for signs and symptoms of adrenal suppression, ocular changes, nasal ulceration or septal perforation, oral candidiasis (long-term use), skin infections, and possible eosinophilic conditions.
Quá liều
Symptoms: Oral inhalation: Suppression of adrenal function, acute adrenal crisis, hypoglycaemia, decreased consciousness, or convulsions. Topical: Features of hypercortisolism. Management: Gradually reduce the dose, or substitute a less potent corticosteroid.
Tương tác
May increase risk of systemic exposure and side effects with CYP3A4 inhibitors (e.g. ritonavir, cobicistat, ketoconazole, itraconazole).
Tác dụng
Description: Fluticasone belongs to a group of corticosteroid which utilises a fluorocarbothioate ester linkage at the 17 carbon position. It has a potent anti-inflammatory and vasoconstrictive activity. Topical fluticasone exhibits its anti-inflammatory, antipruritic and vasoconstrictive properties by depressing the formation, release and activity of endogenous chemical mediators of inflammation through the induction of phospholipase A2 inhibitory proteins and consequent inhibition of arachidonic acid release.
Onset: Oral inhalation: 1-2 weeks or longer.
Pharmacokinetics:
Absorption: Absorbed systemically primarily via lungs. Bioavailability: 13.9% (oral inhalation); <2% (nasal). Time to peak plasma concentration: 0.5-1 hour (oral inhalation).
Distribution: Volume of distribution: 4.2 L/kg (fluticasone propionate); 608 L (fluticasone furoate). Plasma protein binding: >99%.
Metabolism: Undergoes extensive first-pass metabolism, converted to 17β-carboxylic acid by CYP3A4 isoenzyme.
Excretion: Faeces (as unchanged drug and metabolites); urine (<5% as metabolites).
Đặc tính

Chemical Structure Image
Fluticasone furoate

Source: National Center for Biotechnology Information. PubChem Database. Fluticasone furoate, CID=9854489, https://pubchem.ncbi.nlm.nih.gov/compound/Fluticasone-furoate (accessed on Jan. 21, 2020)


Chemical Structure Image
Fluticasone propionate

Source: National Center for Biotechnology Information. PubChem Database. Fluticasone propionate, CID=444036, https://pubchem.ncbi.nlm.nih.gov/compound/Fluticasone-propionate (accessed on Jan. 21, 2020)

Bảo quản
Dry powder or metered dose inhaler/nebule/nasal spray or drops: Store between 15-30°C. Protect from direct heat or sunlight. Do not refrigerate or freeze. Cream/ointment/lotion: Store below 30°C.
Phân loại ATC
R03BA05 - fluticasone ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, glucocorticoids.
R01AD08 - fluticasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.
R01AD12 - fluticasone furoate ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.
R03BA09 - fluticasone furoate ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, glucocorticoids.
D07AC17 - fluticasone ; Belongs to the class of potent (group III) corticosteroids. Used in the treatment of dermatological diseases.
References
Anon. Fluticasone (Nasal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/08/2019.

Anon. Fluticasone (Oral Inhalation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/08/2019.

Anon. Fluticasone (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/08/2019.

Buckingham R (ed). Fluticasone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/08/2019.

Fluticasone Propionate Lotion (E. Fougera & Co. A Division of Fougera Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/08/2019.

Fluticasone Propionate Spray, Metered (Morton Grove Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/07/2015.

Veramyst Spray, Metered (GlaxoSmithKline LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/07/2015.

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