MAKLOMIST 125
Fluticasone Propionate
What it does
Fluticasone is a corticosteroid used to reduce inflammation in various conditions.
Commonly used for: allergic rhinitis (hay fever), asthma, chronic obstructive pulmonary disease (COPD), skin conditions like eczema and psoriasis
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Medicine sourcing is available in Kenya only. We don't sell or dispense medicines - licensed pharmacies do.
Sourcing - Kenya onlyRegistration & product details
Source: South African Health Products Regulatory Authority · fetched 2026-04-15 21:30:22 · updated 2026-09-16 04:01:14
Drug Interactions
42Severe (1)
Mifamurtide - decreases efficacy
Corticosteroidsarepredictedtodecreasetheefficacyof mifamurtide.Avoid.rTheoretical
Moderate (19)
Corticosteroids - increases exposure
Dronedarone is predicted to increase the exposure to corticosteroids (methylprednisolone). Monitor and adjust dose.
Corticosteroids - increases concentration
Miconazole is predicted to increase the concentration of corticosteroids (methylprednisolone). Monitor and adjust dose.
Corticosteroids - increases exposure
Antifungals, azoles (fluconazole, isavuconazole, posaconazole) are predicted to increase the exposure to corticosteroids (methylprednisolone). Monitor and adjust dose.
Corticosteroids - decreases exposure
Cenobamate is predicted to decrease the exposure to corticosteroids (fluticasone). Adjust dose.
Corticosteroids - decreases efficacy
Mifepristone is predicted to decrease the efficacy of corticosteroids. Use with caution and adjust dose.
Unknown (22)
Aspirin - decreases concentration
Corticosteroids are predicted to decrease the concentration of aspirin (high-dose) and aspirin (high-dose) increases the risk of gastrointestinal bleeding when given with corticosteroids.
Choline Salicylate - decreases concentration
Corticosteroids are predicted to decrease the concentration of cholinesalicylate. Ciclesonide → see corticosteroids Ciclosporin → see TABLE 2 p. 1517 (nephrotoxicity), TABLE 16 p. 1521 (increased seru
Corticosteroids - increases exposure
Cobicistat is predicted to increase the exposure to corticosteroids (beclometasone) (risk with beclometasone is likely to be lower than with other corticosteroids).
Corticosteroids - increases risk of gastrointestinal perforation
Erlotinib is predicted to increase the risk of gastrointestinal perforation when given with corticosteroids.
Corticosteroids - increases exposure
Idelalisib is predicted to increase the exposure to corticosteroids (betamethasone, budesonide, ciclesonide, deflazacort, dexamethasone, fludrocortisone, fluticasone, hydrocortisone, methylprednisolon
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: class
About this medicine
Fluticasone is a corticosteroid used to reduce inflammation in various conditions.
What it treats
- allergic rhinitis (hay fever)
- asthma
- chronic obstructive pulmonary disease (COPD)
- skin conditions like eczema and psoriasis
How it works
Fluticasone works by decreasing inflammation and swelling in the body, helping to relieve symptoms.
Who it's for
This medication is for adults and children who need relief from inflammation-related conditions.
Drug class
Corticosteroids
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Fluticasone
BNF-referencedFluticasone is a synthetic corticosteroid that exhibits anti-inflammatory properties. It is widely used in the management of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD) and for the treatment of nasal inflammatory disorders such as allergic rhinitis and nasal polyps. Fluticasone works by reducing inflammation and suppressing the immune response, thereby improving airway function and alleviating symptoms associated with these conditions.
Indications
- Asthma maintenance therapy
- Chronic obstructive pulmonary disease (COPD)
- Allergic rhinitis
- Nasal polyps
Dosage
Adults: For asthma: 160 micrograms once daily, may be reduced to 80 micrograms once daily if control is maintained; may be increased to 320 micrograms twice daily if necessary. For allergic rhinitis:
Mechanism of action
Fluticasone propionate acts as a highly selective agonist at the human glucocorticoid receptor, exhibiting negligible activity at androgen, estrogen, or mineralocorticoid receptors. It activates glucocorticoid receptors and inhibits nuclear factor kappa B, which plays a crucial role in the inflammatory response. Additionally, fluticasone reduces the number of inflammatory mediator cells in the nasal mucosa and decreases nasal reactivity to allergens, leading to reduced release of inflammatory mediators and proteolytic enzymes.
Pharmacodynamics
Fluticasone's therapeutic effects are primarily local, resulting from the deposition of the inhaled drug on the nasal mucosa or lungs, rather than systemic effects from swallowed portions. Its anti-inflammatory action includes the inhibition of eosinophilia and other inflammatory cell types, contributing to the management of allergic conditions and symptoms of asthma. The drug is associated with vasoconstriction in the skin when used topically.
Pharmacokinetics
Fluticasone is administered via inhalation or intranasal routes, leading to low systemic absorption. Following inhalation, it is rapidly absorbed, with peak plasma concentrations occurring within one to two hours. The drug has a high protein binding rate and is extensively metabolized by the liver, primarily through cytochrome P450 enzymes. The elimination half-life is approximately 3 to 4 hours, with metabolites excreted primarily in feces and urine. Due to its significant first-pass metabolism, systemic exposure is minimized.
Contra-indications
- Hypersensitivity to fluticasone or any excipients
- Severe systemic fungal infections
- Untreated localized infections
Adverse effects
- Oral candidiasis
- Dysphonia
- Cough
- Nasal irritation
- Headache
- Throat irritation
- Nasal bleeding
- Increased risk of pneumonia in COPD patients
Interactions
- Cenobamate: Moderate interaction (decreases exposure)
- Cobicistat: Unknown interaction (increases exposure)
- Idelalisib: Unknown interaction (increases exposure)
- Mitotane: Unknown interaction (decreases exposure)
- Clarithromycin: Unknown interaction (increases exposure)
- Rifampicin: Unknown interaction (decreases exposure)
Precautions
- Caution in patients with tuberculosis, untreated systemic infections, or those with a history of severe allergies
- Monitor for signs of adrenal suppression in long-term use
- Use with caution in patients with hepatic impairment
Pregnancy
Fluticasone should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Consultation with a healthcare provider is recommended.
Breast-feeding
Fluticasone is excreted in breast milk. Caution is advised when administered to breastfeeding women.
Storage
Store at room temperature, away from direct sunlight and moisture. Keep out of reach of children.
Formulations
- Pressurized inhalation aerosol: 320 micrograms/9 micrograms per dose
- Nasal spray: 50 micrograms per actuation
- Dry powder inhaler: 200 micrograms per dose
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Fluticasone
PubChem CID 5311101Molecular formula: C22H27F3O4S
Mechanism of action
[DB08906] and [DB00588] work through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show [DB08906] activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats. [DB00588] performs similar activity but is not stated to affect nuclear factor kappa b. Fluticasone propionate is a highly selective agonist at the human glucocorticoid receptor with negligible activity at androgen, estrogen, or mineralocorticoid receptors. In preclinical studies, fluticasone propionate reportedly exhibited weak progesterone-like activity. However, as plasma concentrations of fluticasone propionate are very low following intranasal administration of the drug in recommended doses, the clinical importance of this finding is not known. The therapeutic effects of fluticasone propionate are thought to result from local actions of the deposited inhaled dose on the nasal mucosa rather than from the systemic actions of the swallowed portion of the dose. The exact mechanism(s) of anti-inflammatory action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in the following: number of mediator cells (basophils, eosinophils, helper-inducer [CD4+, T4] T-cells, mast cells, and neutrophils) in the nasal mucosa, nasal reactivity to allergens, and release of inflammatory mediators and proteolytic enzymes. Following exposure of patients with a history of allergic rhinitis to allergen, eosinophils, basophils, mast cells, T cells, and neutrophils appear to infiltrate nasal secretions and mucosa, releasing inflammatory mediators that generate allergic responses such as pruritus, sneezing, rhinorrhea, and nasal edema. /Corticosteroids/ Other mechanisms by which corticosteroids may improve symptoms of allergic rhinitis may involve inhibition of postcapillary venule dilation and permeability and facilitation of nasomucociliary clearance of nasal secretions. Patients receiving short- and long-term treatment with intranasal fluticasone propionate have demonstrated decreases in nasal turbinate swelling and mucosal inflammation. As inflammatory changes occur during periods of increased nasal hyperresponsiveness, the degree of response to nasal secretory stimuli has been used as an indirect measure of inflammation. In patients with asymptomatic seasonal allergic rhinitis, pretreatment with intranasal fluticasone propionate for 2-6 weeks prior to challenge with allergens or inflammatory mediatorsgenerally reduced the release of tryptase, histamine, eosinophilic cationic protein, and prostaglandin D2 in nasal biopsies or nasal lavage fluid; concentrations of eosinophils or activated eosinophils, CD4+ T-cells, and basophils also were reduced. /Corticosteroids/ Like other topical corticosteroids, fluticasone propionate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Pharmacodynamics
Systemically, in vitro experiments show [DB08906] activates glucocorticoid receptors, inhibits nuclear factor kappa b, and inhibits lung eosinophilia in rats. [DB00588] performs similar activity but is not stated to affect nuclear factor kappa b. [DB00588] as a topical formulation is also associated with vasoconstriction in the skin.
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.
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