ELICASAL OINTMENT

Indications

• Management of asthma in adults and adolescents not adequately controlled with inhaled corticosteroids and short-acting beta-2 agonists
• Allergic rhinitis
• Nasal polyps

Dosage

Children: For children aged 12-17 years, initially 400 micrograms daily in 1-2 divided doses, single dose to be inhaled in the evening, reduced to 200 micrograms once daily if control is maintained.

Adults: 1 inhalation once daily; dosage may be increased to 400 micrograms twice daily if necessary.

Mechanism of action

Mometasone furoate works by binding to glucocorticoid receptors, leading to the modulation of gene expression. This results in the inhibition of pro-inflammatory cytokines and chemokines, thereby reducing inflammation in the airways and nasal passages. It also inhibits the activation of inflammatory cells such as eosinophils and mast cells, contributing to its therapeutic effects.

Pharmacodynamics

As a corticosteroid, mometasone furoate exhibits significant anti-inflammatory effects, which are crucial in the management of asthma and allergic conditions. The drug reduces airway hyper-responsiveness and decreases mucus production, leading to improved airflow and decreased symptoms such as wheezing and shortness of breath. Its rapid onset of action is beneficial for acute symptom relief.

Pharmacokinetics

Mometasone furoate is well-absorbed when administered by inhalation or nasal spray. It undergoes extensive first-pass metabolism in the liver, resulting in low systemic bioavailability. The drug is primarily excreted via the feces, with a small percentage eliminated through the urine. The half-life of mometasone furoate is approximately 5.8 hours, allowing for once-daily dosing in many cases.

Adverse effects

• Candida infection
• Nasal ulceration
• Throat irritation
• Headache
• Cough

Interactions

• Corticosteroids
• Beta2 agonists

Precautions

• Use with caution in patients with active or quiescent tuberculosis infections
• Monitor for signs of infection
• Use in hepatic impairment requires caution

Pregnancy

Use only if potential benefit outweighs risk-limited information available.

Breast-feeding

Avoid-present in milk in animal studies.

Storage

Store below 30°C. Protect from light and moisture.

Formulations

• {'form': 'Inhalation powder', 'strength': '200 micrograms per dose', 'brand': 'Asmanex Twisthaler'}
• {'form': 'Aqueous nasal spray', 'strength': '50 micrograms per dose', 'brand': 'Flixonase'}

Indications

• Asthma
• Allergic rhinitis
• Skin conditions (e.g., eczema, dermatitis)

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing guidelines.

Adults: Refer to the specific BNF guidelines for adult dosing, which may vary based on the condition being treated.

Mechanism of action

Mometasone exerts its anti-inflammatory effects by crossing cell membranes and binding with high affinity to specific cytoplasmic glucocorticoid receptors. This interaction diminishes the release of leukocytic acid hydrolases, prevents macrophage accumulation at inflamed sites, interferes with leukocyte adhesion to capillary walls, reduces capillary membrane permeability, and inhibits the release of histamine and kinin. Additionally, mometasone inhibits the formation of scar tissue and acts through phospholipase A2 inhibitory proteins, known as lipocortins, which control the synthesis of potent inflammatory mediators like prostaglandins and leukotrienes.

Pharmacodynamics

Mometasone demonstrates medium potency as a corticosteroid, effectively reducing inflammation without significant systemic absorption due to extensive hepatic metabolism. Its local effects are favored over systemic effects, making it suitable for chronic conditions like asthma, where immediate symptom relief is not expected. The onset of action may take 1 to 2 weeks for maximum improvement in asthma symptoms following inhalation. Discontinuation of mometasone may allow for sustained asthma stability for several days.

Pharmacokinetics

Mometasone is extensively metabolized in the liver, resulting in a low systemic bioavailability. Its pharmacokinetic profile includes rapid absorption and distribution, with a half-life that supports once-daily dosing in many cases. The lack of active metabolites contributes to its safety profile, minimizing systemic effects while providing effective local action.

Interactions

• cobicistat+mometasone: Unknown (increases exposure)
• idelalisib+mometasone: Unknown (increases exposure)
• clarithromycin+mometasone: Unknown (increases exposure)

Pregnancy

Mometasone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution should be exercised when administering mometasone to nursing mothers, as it is not known whether it is excreted in human milk.

Storage

Store at room temperature, away from light and moisture. Do not freeze.

Formulations

• Mometasone furoate nasal spray
• Mometasone furoate inhalation aerosol
• Mometasone furoate cream
• Mometasone furoate ointment
• Mometasone furoate lotion

Indications

• Acne vulgaris
• Psoriasis
• Warts
• Seborrheic dermatitis
• Dandruff
• Hyperkeratosis

Dosage

Adults: For topical application, salicylic acid is typically applied once or twice daily, depending on the formulation and condition being treated. Specific dosing guidelines should be followed as per the BNF.

Mechanism of action

Salicylic acid exerts its effects by penetrating the skin and exfoliating the stratum corneum through keratolytic action, which helps in the dissolution of keratin and the removal of dead skin cells. This action facilitates the clearance of pores and can reduce acne lesions. Additionally, salicylic acid has anti-inflammatory properties that can help to decrease swelling and redness associated with various skin conditions. The compound is also known to inhibit the activity of enzymes involved in the synthesis of prostaglandins, which are mediators of inflammation.

Pharmacodynamics

The pharmacodynamics of salicylic acid involve its ability to enhance the turnover of skin cells and reduce the cohesiveness of keratinocytes in the stratum corneum. This leads to increased desquamation and a reduction in the formation of microcomedones in acne. Its anti-inflammatory effects are mediated through the inhibition of cyclooxygenase enzymes, leading to decreased production of pro-inflammatory mediators. This contributes to the reduction of inflammation and pain in affected areas.

Pharmacokinetics

Salicylic acid is absorbed percutaneously when applied topically, with systemic absorption increasing with higher concentrations and prolonged application. Once absorbed, it is metabolized predominantly in the liver to various conjugates, which are then excreted by the kidneys. The elimination half-life can vary based on the formulation and concentration used. For topical applications, significant first-pass metabolism may occur, limiting systemic exposure and reducing potential systemic side effects.

Pregnancy

Salicylic acid is classified as pregnancy category C. Its use should be avoided during pregnancy unless the potential benefits outweigh the risks.

Breast-feeding

Salicylic acid is excreted in breast milk, and caution is advised when using it during breastfeeding.

Storage

Store in a cool, dry place away from direct light.

Mechanism of action

Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. Inflammation is decreased by diminishing the release of leukocytic acid hydrolases, prevention of macrophage accumulation at inflamed sites, interference with leukocyte adhesion to the capillary wall, reduction of capillary membrane permeability, reduction of complement components, inhibition of histamine and kinin release, and interference with the formation of scar tissue. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A₂ inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Mometasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone.

Pharmacodynamics

Mometasone is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. Studies in asthmatic patients have demonstrated that mometasone provides a favorable ratio of topical to systemic activity due to its primary local effect along with the extensive hepatic metabolism and the lack of active metabolites. Though effective for the treatment of asthma, glucocorticoids do not affect asthma symptoms immediately. Maximum improvement in symptoms following inhaled administration of mometasone furoate may not be achieved for 1 to 2 weeks or longer after starting treatment. When glucocorticoids are discontinued, asthma stability may persist for several days or longer. Mometasone has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone. The clinical significance of these findings is unknown.