Beclomethasone

Beclomethasone is a synthetic glucocorticoidbelonging to Corticosteroids

Beclomethasone is indicated for the prophylactic management of asthma and as a maintenance treatment for chronic asthma. It may also be used to treat other respiratory disorders, such as chronic obstructive pulmonary disease (COPD), allergic rhinitis, and nasal polyps.

Beclomethasone can be absorbed into the bloodstream through inhalation, nasal administration, or topical application. The rate and extent of absorption depend on the formulation and the site of administration. Beclomethasone is distributed to various tissues in the body, including the liver, kidneys, and lungs. It binds to plasma proteins at a rate of 87-90%. Beclomethasone is metabolized in the liver by the enzyme CYP3A4 to its active metabolite, beclomethasone-17-monopropionate (B17MP). Beclomethasone and its metabolites are excreted in the urine and feces. The elimination half-life of beclomethasone is approximately 2.8 hours, while the elimination half-life of B17MP is approximately 14 hours.

For beclomethasone inhalers, the Tmax is generally between 30 minutes to 1 hour after administration.

For beclomethasone nasal sprays, the Tmax is generally within 30 minutes after administration.

For beclomethasone creams or ointments applied topically to the skin, the systemic absorption is generally low, so the Tmax is not usually relevant.

For beclomethasone inhalers, the Cmax is generally achieved within 5-15 minutes after administration, with a range of 0.2 to 2.2 nanograms per milliliter (ng/mL) for various doses.

For beclomethasone nasal sprays, the Cmax is generally achieved within 30 minutes after administration, with a range of 0.12 to 0.45 ng/mL for various doses.

Beclomethasoneshows common side effects like insomnia, confusion, hallucination, nervousness, disorientation, depression, anxiety, mood changes. Renal and urinary disorders: Crystalluria (high doses).

Beclomethasone is available in tablets.

Beclomethasone is available in India, Germany, Canada, France.

Beclometasone (as diproprionate) is a prodrug w/ potent glucocorticoid and weak mineralocorticoid activity. It controls the rate of protein synthesis, depresses the migration of polymorphonuclear leukocytes, reduces fibroblast activity, and reverses capillary permeability and lysosomal stabilisation at the cellular level to prevent or control inflammation.

Beclomethasone is available in the form of tablets, inhalers, nasal sprays, creams, ointment.

Beclomethasone is indicated for the prophylactic management of asthma and as a maintenance treatment for chronic asthma. It may also be used to treat other respiratory disorders, such as chronic obstructive pulmonary disease (COPD), allergic rhinitis, and nasal polyps.

Betamethasone is a synthetic glucocorticoid that binds to intracellular glucocorticoid receptors, which are present in many different cell types throughout the body. Once bound to these receptors, betamethasone induces a variety of cellular effects, including reducing inflammation, suppressing the immune system, and altering the metabolism of carbohydrates, fats, and proteins. These actions help to reduce swelling, redness, itching, and other symptoms of inflammatory conditions.

Beclomethasone is approved for use in the following clinical indications

Beclomethasone is indicated for the prophylactic management of asthma and as a maintenance treatment for chronic asthma. It may also be used to treat other respiratory disorders, such as chronic obstructive pulmonary disease (COPD), allergic rhinitis, and nasal polyps.

Inhalation/Respiratory

Asthma prophylaxis

Adult: As aerosol or dry powd inhaler: Initially, 100-200 mcg daily for mild cases; 200-400 mcg daily for moderate cases; 400-800 mcg daily for severe cases. All doses are given in 2 divided doses. Usual maintenance dose: 400-800 mcg daily in 2 divided doses, titrated to the lowest effective dose. Max: 800 mcg (up to 2 mg may be necessary in severe cases) daily in divided doses.

Child: ≥6 yr 100 mcg in 2-4 divided doses, titrated to the lowest effective dose for maintenance. Max: 200 mcg daily.

Nasal

Treatment and prophylaxis of allergic and non-allergic rhinitis

Adult: As spray: 100 mcg into each nostril bid, or 50 mcg in each nostril 3-4 times daily. Max: 400 mcg daily. 50 mcg in each nostril bid may be used as prophylaxis.

Child: ≥6 yr Same as adult dose.

Oral

Ulcerative colitis

Adult: As modified-release tab: 5 mg once daily in the morning, before or after breakfast, for mild to moderate cases. Max duration: 4 wk.

Topical/Cutaneous

Corticosteroid-responsive dermatoses

Adult: 0.025% cream: Apply a thin film to affected area(s) 1-3 times daily, or as directed based on severity.

Beclomethasone inhalers: These are available in various strengths, including 40 mcg, 80 mcg, and 160 mcg per inhalation.

Beclomethasone nasal sprays: These are available in various strengths, including 50 mcg and 100 mcg per spray.

Beclomethasone creams or ointments: These are available in various strengths, including 0.025%, 0.05%, and 0.1%.

Beclomethasone is available in the form of tablets, inhalers, nasal sprays, creams, ointment.

• Dosage Adjustment for Pediatric Patients:

Initial doses should be based on previous asthma therapy and disease severity, including current control and risk of future exacerbations:

Age: 4 to 11 years:

• Initial dose: 40 mcg via oral inhalation twice a day
• Maintenance dose: After 2 weeks, may increase dose to 80 mcg twice daily for additional asthma control; after asthma stability has been achieved, titrate to the lowest effective dose to reduce the possibility of side effects
• Maximum dose: 80 mcg twice a day

Age: 12 years or older:

For patients not previously receiving inhaled corticosteroid (ICS): Initial dose: 40 to 80 mcg via oral inhalation twice a day

For patients switching from another ICS: Initial dose selection should be based on the previous ICS strength: 40 to 320 mcg via oral inhalation twice a day

• Maintenance dose: After 2 weeks, may increase dose for additional asthma control; after asthma stability has been achieved, titrate to the lowest effective dose to reduce the possibility of side effects
• Maximum dose: 320 mcg twice a day

Dosing: Kidney Impairment:

Pediatric

• Adolescents ≥17 years:
• CrCl ≥30 mL/minute: No dosage adjustment necessary.
• CrCl <30 mL/minute: Initial: 0.5 mg once daily; maximum maintenance dose: 0.5 mg twice daily.
• End-stage renal disease (ESRD) (receiving hemodialysis): Maximum maintenance dose: 0.5 mg once daily.

Take after eating and with a full glass of water to decrease gastric upset.

Beclomethasone is contraindicated in individuals who have a known hypersensitivity to beclomethasone or any of its components. It is also contraindicated in individuals who are experiencing an acute asthma attack or who have a primary treatment of status asthmaticus, which is a severe and potentially life-threatening asthma attack that does not respond to conventional therapy. In addition, beclomethasone should be used with caution or avoided in individuals who have certain medical conditions, such as tuberculosis, fungal or viral infections of the respiratory tract, ocular herpes simplex, or systemic fungal infections. It should also be used with caution in individuals who have a history of osteoporosis, glaucoma, cataracts, or other conditions that may be exacerbated by long-term use of corticosteroids.

Beclomethasone is a medication that should be used with caution and under the guidance of a healthcare provider. Here are some precautions and warnings to be aware of when using beclomethasone:

• Use only as directed: Beclomethasone should be used only as directed by a healthcare provider, and at the lowest effective dose for the shortest possible duration.
• Risk of respiratory infections: Long-term use of beclomethasone may increase the risk of respiratory infections, such as pneumonia or tuberculosis. It is important to monitor for signs of infection and to use caution when using beclomethasone in individuals with a history of these infections.
• Adrenal suppression: Beclomethasone may suppress the function of the adrenal glands, which can result in a variety of symptoms, including weakness, fatigue, and weight loss. Individuals who have been taking beclomethasone for a prolonged period of time should be gradually weaned off the medication under the guidance of a healthcare provider.
• Ocular effects: Beclomethasone may cause ocular effects such as cataracts or glaucoma. It is important to have regular eye exams while taking beclomethasone, particularly for individuals who are using high doses or have a history of eye problems.
• Growth suppression in children: Long-term use of beclomethasone may suppress growth in children. Children who are taking beclomethasone should be monitored regularly for growth and development.
• Use during pregnancy and breastfeeding: Beclomethasone is classified as a pregnancy category C medication, which means that it may not be safe to use during pregnancy. It is also not known whether beclomethasone passes into breast milk. Women who are pregnant or breastfeeding should talk to their healthcare provider before using beclomethasone.

Beclomethasone may cause liver problems, and using it with substantial quantities of ethanol may increase that risk.

Beclomethasone is present in breast milk.

Concentrations of Beclomethasone in breast milk increase with supplementation. When used as a dietary supplement, the recommended dietary allowance of Beclomethasone is increased in breastfeeding patients compared to nonbreastfeeding patients. Doses of Beclomethasone for the treatment of dyslipidemias are greater than those used as a dietary supplement. Due to the potential for serious adverse reactions in the breastfed infant (including hepatoxicity), the manufacturer recommends that breastfeeding be discontinued when Beclomethasone is used for treatment of dyslipidemias.

• Common Adverse effects

Irritation in the nose or throat (with nasal spray) Hoarseness or changes in voice (with inhalation) Headache Nausea Cough Sore throat Runny or stuffy nose Sinus pain Dry mouth or throat Skin rash or itching (with topical use)

• Less Common Adverse effects:

Allergic reactions, including hives, itching, or difficulty breathing Eye problems, such as cataracts or glaucoma (with long-term use) Growth suppression in children (with long-term use) High blood sugar levels Increased risk of infections, including fungal infections of the mouth or throat (thrush) Mood changes or behavioral changes, such as agitation or aggression Osteoporosis or bone fractures (with long-term use) Slow wound healing

• Rare Adverse effects

Adrenal suppression (with long-term use) Anaphylaxis (a severe and life-threatening allergic reaction) Cushing's syndrome (with long-term use) Decreased immune system function (with long-term use) Hyperglycemia (high blood sugar levels) Hypokalemia (low levels of potassium in the blood) Hypersensitivity reactions (such as rash or angioedema) Ocular toxicity (such as increased intraocular pressure, cataracts, or glaucoma with long-term use) Psychiatric effects (such as mood changes or suicidal thoughts)

Beclomethasone may interact with other medications, supplements, or herbal products. Some potential drug interactions of beclomethasone include: Drugs that may increase the risk of corticosteroid-induced side effects, such as other corticosteroids, some antibiotics, and certain antifungal medications. Drugs that may decrease the effectiveness of beclomethasone, such as some anticonvulsants, certain antibiotics, and some herbal products. Drugs that may be affected by beclomethasone, such as some anticoagulants, some diabetes medications, and some vaccines.

The common side effects of Beclomethasone include the following :

Irritation in the nose or throat (with nasal spray) Hoarseness or changes in voice (with inhalation) Headache Nausea Cough Sore throat Runny or stuffy nose Sinus pain Dry mouth or throat Skin rash or itching (with topical use).

Symptoms: Tachycardia, tremor, hyperactivity, metabolic effects (e.g. hypokalaemia, lactic acidosis), headache, nervousness, dry mouth, palpitations, dizziness, fatigue, malaise, insomnia, arrhythmias, anginal pain, seizures. Children may experience nausea, vomiting, hyperglycaemia when taken orally.

Management: Symptomatic treatment. Monitor serum K and lactate levels. May give cardioselective β-blocker with caution. May give oral or IV potassium for hypokalaemia as needed.

Pharmacodynamic

Beclomethasone is a corticosteroid medication that is used to reduce inflammation in the body. The mechanism of action of beclomethasone involves its ability to bind to and activate glucocorticoid receptors (GR) in the cells of various tissues. Once beclomethasone binds to the GR, it translocates to the nucleus of the cell and binds to specific DNA sequences known as glucocorticoid response elements (GREs). This process results in the regulation of the transcription of various genes involved in inflammation, immune responses, and other processes. Beclomethasone has potent anti-inflammatory effects that can help reduce the production and release of inflammatory mediators, such as cytokines and leukotrienes, from immune cells, leading to a reduction in inflammation. It can also suppress the immune system and reduce the production of antibodies, which can be useful in the treatment of autoimmune disorders.

Pharmacokinetics

• Absorption: Beclomethasone can be absorbed into the bloodstream through inhalation, nasal administration, or topical application. The rate and extent of absorption depend on the formulation and the site of administration.
• Distribution: Beclomethasone is distributed to various tissues in the body, including the liver, kidneys, and lungs. It binds to plasma proteins at a rate of 87-90%.
• Metabolism: Beclomethasone is metabolized in the liver by the enzyme CYP3A4 to its active metabolite, beclomethasone-17-monopropionate (B17MP).
• Elimination: Beclomethasone and its metabolites are excreted in the urine and feces. The elimination half-life of beclomethasone is approximately 2.8 hours, while the elimination half-life of B17MP is approximately 14 hours.

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