Dulera inhaler: what you need to know

Indications: Dulera is indicated for the treatment of asthma, including reduction of asthma exacerbations, in adults and children 12 years of age and older. Dulera should be used for patients who are not adequately controlled with inhaled corticosteroids and, for necessary reasons, beta-2 agonists of short duration or whose severity of the disease clearly justifies the initiation of treatment with two maintenance therapies. Dulera inhaler can also be used in patients who are already adequately controlled with inhaled corticosteroids and long-acting beta-2 agonists.

Properties: Pharmacokinetics and pharmacodynamics in humans: Mometasone furoate is a topical glucocorticosteroid with local anti-inflammatory properties and formoterol is a potent, selective beta2-adrenergic stimulant. Glucocorticoids, such as mometasone furoate exert their anti-inflammatory effects through glucocorticoid receptors (GR). Upon entering the glucocorticoid in contact with the GR in the cytoplasm, the hetero-complex dissociates and activates. The GR activated by the ligand moves (translocates) from the cytoplasm to the nucleus. The activated GR can then regulate the transcription of anti-inflammatory genes by binding to specific deoxyribonucleic acid (DNA) sequences; called glucocorticoid response elements.

However, it is more likely to be the ability of glucocorticoids to suppress gene transcription; which provides primary activity to suppress inflammation. In this case, the activated GR interacts with the transcription factors apolipoprotein A-1 (AP1) or with the nuclear factor kappa B (NF-kB) to regulate the expression of the genes. In addition, glucocorticoids have been shown to regulate the expression of an NF-kB inhibitor. Formoterol fumarate is a potent, selective beta2-adrenergic stimulant. This exerts a bronchodilator effect in patients with reversible obstruction of the respiratory tract that lasts 12 hours. Formoterol inhibits the release of histamine and leukotrienes from passively sensitized human lung.

Some anti-inflammatory properties, such as the inhibition of edema and accumulation of inflammatory cells, have been observed in animal experiments.

Pharmacodynamic effects: Mometasone furoate: The binding affinity to GR corresponds to functional activity. Mometasone furoate binds with very high affinity to human GR and this leads to its potent inhibitory effects on cells to reduce the synthesis and release of pro-inflammatory mediators and cytokines. Mometasone furoate significantly inhibits the release of leukotrienes from the leukocytes of allergic patients. In a cell culture, mometasone furoate demonstrated a high potency in inhibiting the synthesis and release of IL-1, IL-5, IL-6, and TNF at; it is also a potent inhibitor of the production of the TH2, IL-4 and IL-5 cytokines, from human T-CD4 + cells. In an analysis of different leukocyte populations of atopic patients, mometasone furoate was a more potent inhibitor of leukotriene production than beclomethasone dipropionate. In preclinical models, it has been shown that mometasone furoate reduces the accumulation of inflammatory cells, including eosinophils, infiltrates the upper and lower respiratory tract and improves lung function after provocation with allergens. Additionally, mometasone furoate reduced the number of lymphocytes and levels of messenger ribonucleic acid (RNA) for the pro-allergic cytokines IL-4 and IL-5. Formoterol fumarate:In vitro studies in guinea pig trachea have indicated that racemic formoterol and its enantiomers (R, R) - and (S, S) are highly selective agonists of beta-2 adrenoreceptors. The enantiomer (S, S) was 800 to 1000 times less potent than the enantiomer (R, R) and did not affect the activity of the enantiomer (R, R) in the smooth muscle of the trachea. A pharmacological basis for the use of one of the two enantiomers in preference to the racemic mixture was not demonstrated.

Sponsor Ads

• Ad Space Available - Rent it Now!

Report this Page

Created on Mar 28th 2019 18:10. Viewed 419 times.

Share on APSense

Comments

Dose Pharmacy  online medicine store Generic medicine are available at buy medication online at lower price now. this is one of the best option to save the money. Jan 23rd 2020 04:40