Beclomethasone Dipropionate
Beclomethasone Dipropionate Uses, Dosage, Side Effects, Food Interaction and all others data.
Following topical administration into the nasal mucosa, Beclomethasone Dipropionate produces anti-inflammatory and vasoconstrictor effects. The exact mechanism of these actions remain unknown, but may involve reductions in the following: number of mediator cells (basophil, leukocytes and mast cells) at the epithelial level, number of eosinophils, sensitivity of sensory nerves to mechanical stimuli, secretory response to cholinergic receptor stimulation, and fibroblast activity. Other mechanisms may involve inhibition of capillary dilation and permeability, stabilization of lysosomal membranes and subsequent prevention of release of proteolytic enzymes.
Inflammatory conditions, including asthma, dermatoses, and allergic rhinitis, involve the activation of cascades by inflammatory mediators. Inflammation is a primary defense mechanism and the homeostatic response of the immune system; however, a prolonged inflammatory response in certain disorders may lead to tissue damage, pain, and swelling. Beclomethasone Dipropionate works by attenuating the inflammatory responses associated with asthma, allergic rhinitis, nasal polyps, and corticosteroid-responsive dermatoses. It suppresses the actions of inflammatory cells, such as mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils. It also inhibits the release of inflammatory mediators, such as histamine, eicosanoids, leukotrienes, and cytokines. Beclomethasone Dipropionate is reported to exhibit potent topical activity while possessing low systemic effects.
Beclomethasone Dipropionate is a corticosteroid drug with anti-inflammatory and vasoconstrictive effects used to treat chronic inflammatory processes such as asthma, allergic rhinitis, corticosteroid-responsive dermatoses. When inhaled, it improves lung function, decreases airway hyper-reactivity, and reduces the severity of asthmatic symptoms. Although inhaled corticosteroids, including beclomethasone dipropionate, are reported to mainly act locally in the lungs, systemic effects such as disruption of hypothalamic-pituitary-adrenal (HPA) axis function, bone turnover, osteoporosis, and growth suppression may still be observed with chronic use or high dose administration. There were varying findings from clinical studies examining the effect of beclomethasone dipropionate on growth suppression in pediatric patients. It was shown to suppress the hypothalamo-pituitary-adrenal (HPA) axis in a dose-dependent manner. HPA axis is a central hormonal response system to stress and activation of HPA axis leads to the production of endogenous steroid hormone production. Long-term use of high-dose systemic corticosteroids, including those inhaled, was often associated with signs and symptoms of adrenal insufficiency when exposed to stress conditions, such as trauma, surgery, or infections. As corticosteroids work by suppressing the immune system, there may be an increased risk for developing infections. Cases of Candida albicans infection of the mouth and throat have been reported with inhaled beclomethasone dipropionate therapy.
| Trade Name | Beclomethasone Dipropionate |
| Generic | Beclomethasone dipropionate |
| Beclomethasone dipropionate Other Names | Beclometasone dipropionate, Beclometasone dipropionato, Beclomethasone dipropionate |
| Type | |
| Formula | C28H37ClO7 |
| Weight | Average: 521.042 Monoisotopic: 520.222781245 |
| Protein binding | Based on the findings of in vitro studies, the protein binding of the main active metabolite, beclomethasone-17-monopropionate (17-BMP), was 94-96% over the concentration range of 1000 to 5000 pg/mL. |
| Groups | Approved, Investigational |
| Therapeutic Class | Nasal Steroid Preparations |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Prophylaxis and treatment of seasonal & perennial allergic rhinitis including hay fever & non-allergic (vasomotor) rhinitis. Prevention of recurrence of nasal polyps following surgical removal.
Beclomethasone Dipropionate is also used to associated treatment for these conditions: Asthma, Bacterial Sinusitis, Chronic Obstructive Pulmonary Disease (COPD), Chronic Sinusitis, Dermatosis, Fungal skin infection, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis, Vasomotor Rhinitis, Corticosteroid-responsive dermatoses, Recurrent nasal polyps
How Beclomethasone Dipropionate works
Beclomethasone Dipropionate is a corticosteroid and prodrug that is rapidly activated by hydrolysis to the active monoester, 17 monopropionate (17-BMP), which mediates anti-inflammatory actions. 17-BMP has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 13 times that of dexamethasone and 25 times that of beclomethasone dipropionate. Upon binding of the ligand, the glucocorticoid receptors dimerize and translocate into the nucleus, where they subsequently bind to glucocorticoid response elements (GRE) on glucocorticoid-responsive genes, leading to changes in transcription. There are several proposed mechanisms for the anti-inflammatory action of corticosteroids. Corticosteroids may work by increasing the transcription of genes coding for anti-inflammatory proteins, including lipocortin-1 and interleukin-10. Corticosteroids were also shown to inhibit the expression of multiple genes that encode pro-inflammatory factors, such as cytokines, chemokines, and adhesion molecules, that are activated during the chronic inflammatory process. This is thought to be due to the direct inhibitory interaction between activated glucocorticoid receptors and activated pro-inflammatory transcription factors, such as nuclear factor-kappa B and activator protein-1. Chronic inflammation is often characterized by enhanced expression of these transcription factors that bind to and activate coactivator molecules, which then acetylate core histones to switch on gene transcription to further amplify the inflammatory process. Corticosteroids suppress the multiple inflammatory gene expression by promoting histone deacetylation, resulting in tighter coiling of DNA and reduced access of transcription factors to their binding sites.
Dosage
Beclomethasone Dipropionate dosage
Dosage of intranasal Beclomethasone Dipropionate must be carefully adjusted according to individual requirements and response.
Adults: Recommended usual dosage: 02 (two) sprays (50 µgm/spray) in each nostril twice daily. For some patients, 01 (one) spray in each nostril 3 to 4 times daily may be preferred. Total daily doses of 400 µgm (08 sprays) should not generally be exceeded.
Children (6 to 12 years of age): Usual dose: 01 (one) spray in each nostril twice daily. Patients not adequately responding, or those with more severe symptoms may use 02 (two) sprays in each nostril twice daily.
Children under 6 years of age: Not recommended since safety profile studies have not been conducted. After the first few days, patients may be able to reduce their dosage to 100 µg (one spray in each nostril) once daily for maintenance therapy.
Side Effects
Rare instances of nasal septum perforation have been reported following intranasal administration. As with other nasal sprays, dryness and irritation of the nose and throat, unpleasant taste & smell and epistaxis have been reported rarely. Rare instances of wheezing, cataracts, glaucoma and increased intra-ocular pressure have been reported following the intranasal use of Beclomethasone.
Toxicity
The oral LD50 in rats is >3750 mg/kg.
The acute toxicity of beclometasone dipropionate is low. The only harmful effect that follows inhalation of large amounts of the drug over a short period of time is suppression of hypothalamic-pituitary-adrenal (HPA) function. Chronic: The excessive use of beclometasone dipropionate over a long period could lead to adrenal suppression.
Precaution
Care must be taken while transferring patients from systemic steroid to Beclomethasone nasal spray if there is any reason to suppose that their adrenal function is impaired.
Food Interaction
No interactions found.Volume of Distribution
Following intravenous administration, the steady-state volume of distribution was 20 L for beclomethasone dipropionate and 424 L for the active metabolite, beclomethasone-17-monopropionate.
Elimination Route
Following oral inhalation of 320 mcg of beclomethasone dipropionate (BDP), the Cmax was 88 pg/mL and it was reached after 0.5 at post-administration. The mean Cmax of the major and most active metabolite, beclomethasone-17-monopropionate (17-BMP), was 1419 pg/mL at 0.7 hour post-dosing.
In another pharmacokinetic study, the AUC of BDP and 17-BMP were 6660 and 6185 pgxh/mL, respectively. The Cmax was 35356 pg/mL for BDP and 2633 pg/mL for 17-BMP, and and the median time to reach these concentrations (Tmax) was 0.2 hours. In the same study, the AUC of 17-BMP following oral and intranasal administration were 10158 and 3660 pgxh/mL, respectively. The Cmax of 17-BMP following oral and intranasal administration were 703 and 310 pg/mL, respectively, and the Tmax was 4 hours. The total bioavailability of 17-BMP following oral and intranasal administration were 41% and 44%, respectively.
Half Life
Following intravenous administration, the half life of beclomethasone dipropionate was 0.5 hours while the half life of the active metabolite 17-BMP was 2.7 hours. Following oral and intranasal administration, the half life of 17-BMP was 8.8 and 5.7 hours, respectively.
Clearance
Following intravenous administration, the clearance of beclomethasone dipropionate and 17-BMP were 150 L/h and 120 L/h, respectively.
Elimination Route
Regardless of the route of administration, beclomethasone dipropionate and its metabolites are predominantly excreted in the feces, with less than 10% of the drug and its metabolites being excreted in the urine.
Pregnancy & Breastfeeding use
Beclomethasone should be used during pregnancy, if the potential benefit justifies the potential risks to fetus. In addition, as there is natural increase in corticosteroid production during pregnancy, most women will require a lower exogenous corticosteroid dose and many will not need corticosteroid treatment during pregnancy.
As other corticosteroids are excreted in human milk, caution should be exercised when Beclomethasone nasal spray is administered to a nursing woman.
Contraindication
Contraindicated in patients with a history of hypersensitivity to any of its components. Infections of the nasal passages and paranasal sinuses should be appropriately treated but do not constitute a specific contraindication to treatment with Beclomethasone nasal spray.
Acute Overdose
Inhalation of excessive doses over a short time period may suppress hypothalamic pituitary adrenal (HPA) function, and no special emergency action need to be taken, rather treatment should be continued at recommended dose. HPA function recovers within one or two day
Storage Condition
Store at a temperature not exceeding 30˚ C. Protect from light & moisture. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Beclomethasone Dipropionate
Beclomethasone Dipropionate contains Beclomethasone dipropionate see full prescribing information from innovator Beclomethasone Dipropionate Monograph, Beclomethasone Dipropionate MSDS, Beclomethasone Dipropionate FDA label
FAQ
What is Beclomethasone Dipropionate used for?
Beclomethasone Dipropionate is used to prevent difficulty breathing, chest tightness, wheezing, and coughing caused by asthma in adults and children 5 years of age and older. Beclomethasone Dipropionate is available as an inhaler, cream, pills, and nasal spray. The inhaled form is used in the long-term management of asthma.
How safe is Beclomethasone Dipropionate?
Beclomethasone Dipropionate is not suitable for some people. To make sure it's safe for you, tell your doctor if you: have had an allergic reaction to Beclomethasone Dipropionate or any other medicines in the past.
How does Beclomethasone Dipropionate work?
Beclomethasone Dipropionate works by reducing the swelling of the airways in the lungs to make breathing easier.
What are the common side effects of Beclomethasone Dipropionate?
Common side effects of Beclomethasone Dipropionate are include:
- headache.
- sore throat.
- runny or stuffy nose.
- back pain.
- nausea.
- cough.
- difficult or painful speech.
Is Beclomethasone Dipropionate safe during pregnancy?
The prevalence of congenital malformations is within the normal range and shows that treatment with Beclomethasone Dipropionate is safe during pregnancy when recommended doses are used.
Is Beclomethasone Dipropionate safe during breastfeeding?
Beclomethasone Dipropionate has not been well studied during breastfeeding after systemic or topical use. Systemic Beclomethasone Dipropionate is best avoided in favor of one of the shorter-acting and better studied alternatives because of its potency and low protein binding which would favor its passage into milk.
Can I drink alcohol with Beclomethasone Dipropionate ?
Yes, you can drink alcohol while using Beclomethasone Dipropionate.
When should be taken of Beclomethasone Dipropionate?
taken twice a day. It's important to use your Beclomethasone Dipropionate inhaler regularly to manage your condition. Keep using it, even if you do not have any symptoms. After using your inhaler, always put the lid back on to keep it clean.
How long does it take Beclomethasone Dipropionate to work?
This is because it takes a few days for to take full effect. Tell your doctor if you feel no better after using the spray for 7 days. For some people it can take 2 weeks or more to get the maximum benefits.
How often can I take Beclomethasone Dipropionate?
The usual dose is 1 or 2 puffs, taken twice a day.
How long does Beclomethasone Dipropionate stay in my system?
Most inhaled steroids have a beneficial effect for 12 hours.
How quickly does Beclomethasone Dipropionate inhaler work?
Beclomethasone Dipropionate inhaler does not work straight away. You'll usually start to wheeze less after using Beclomethasone Dipropionate for 3 to 7 days.
How long can I use Beclomethasone Dipropionate?
Do not use it continuously for more than 1 month without speaking to your doctor. If your symptoms get worse after reducing your dose, you may want to increase it again.
Who should not take Beclomethasone Dipropionate?
You should not use this medicine if your asthma attack has already started. Your doctor will prescribe another medicine for you to use in case of an acute asthma attack.
What happen If I stop taking Beclomethasone Dipropionate?
Some conditions may become worse when the drug is suddenly stopped. If you suddenly stop taking the Beclomethasone Dipropionate, you may also have withdrawal symptoms (such as weakness, weight loss, nausea, muscle pain, headache, tiredness, dizziness).
What happens if I miss a dose?
Use the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not use two doses at one time.
What happen if I take too much Beclomethasone Dipropionate?
Adults taking high doses (either using an inhaler, or as tablets to help control more severe symptoms) have an increased risk of getting adrenal gland problems or weak bones (osteoporosis) over time. This is because more of the corticosteroid gets into your system.
What should if I overdose on Beclomethasone Dipropionate?
If someone has overdosed and has serious symptoms such as passing out or trouble breathing, Otherwise, call a poison control center right away.
Can Beclomethasone Dipropionate cause shortness of breath?
This Beclomethasone Dipropionate may cause Beclomethasone Dipropionate, which means your breathing or wheezing will get worse. This may be life-threatening.
