Beclometasone dipropionate

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Beclometasone dipropionate
Beclometasone dipropionate.png
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Clinical data
Trade names Qvar, Beconase AQ, others
AHFS/Drugs.com Monograph
MedlinePlus a681047
Pregnancy
category
    Routes of
    administration
    inhalation, nasal, topical
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability Converted to beclometasone-17-monopropionate (17-BMP) during absorption
    Protein binding 87% of 17-BMP to albumin and transcortin
    Metabolism By esterase enzymes found in most tissues
    Elimination half-life 2.8 hours
    Excretion Biliary (60%), renal (12%)
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    ChEBI
    ChEMBL
    ECHA InfoCard 100.024.442 Blue pencil.svg
    Chemical and physical data
    Formula C28H37ClO7
    Molar mass 521.042 g/mol g·mol−1
    3D model (JSmol)
     X mark.svgNYes check.svgY  (what is this?)    (verify)

    Beclometasone dipropionate, also spelled beclomethasone dipropionate and sold under the brand name Qvar among others, is a steroid medication. [1] It is available as an inhaler, cream, pills, and nasal spray. [2] The inhaled form is used in the long-term management of asthma. [1] The cream may be used for dermatitis and psoriasis. [3] The pills have been used to treat ulcerative colitis. [4] The nasal spray is used to treat allergic rhinitis and nasal polyps. [5]

    Corticosteroid steroid hormone

    Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones. Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are involved in a wide range of physiological processes, including stress response, immune response, and regulation of inflammation, carbohydrate metabolism, protein catabolism, blood electrolyte levels, and behavior.

    Inhaler medical device

    An inhaler is a medical device used for delivering medication into the body via the lungs. It is mainly used in the treatment of asthma and chronic obstructive pulmonary disease. Zanamivir, used to treat influenza, must be administered via inhaler.

    Nasal spray

    Nasal sprays, are used to deliver medications locally in the nasal cavities or systemically. They are used locally for conditions such as nasal congestion and allergic rhinitis. In some situations, the nasal delivery route is preferred for systemic therapy because it provides an agreeable alternative to injection or pills. Substances can be assimilated extremely quickly and directly through the nose. Many pharmaceutical drugs exist as nasal sprays for systemic administration. Other applications include hormone replacement therapy, treatment of Alzheimer's disease and Parkinson's disease. Nasal sprays are seen as a more efficient way of transporting drugs with potential use in crossing the blood–brain barrier.

    Contents

    Common side effects with the inhaled form include respiratory infections, headaches, and throat inflammation. [1] Serious side effects include an increased risk of infection, cataracts, Cushing’s syndrome, and severe allergic reactions. [1] Long-term use of the pill form may cause adrenal insufficiency. [4] The pills may also cause mood or personality changes. [4] The inhaled form is generally regarded as safe in pregnancy. [6] Beclometasone is mainly a glucocorticoid. [1]

    Respiratory tract infection any number of infectious diseases involving the respiratory tract

    Respiratory tract infection (RTI) refers to any of a number of infectious diseases involving the respiratory tract. An infection of this type is normally further classified as an upper respiratory tract infection or a lower respiratory tract infection. Lower respiratory infections, such as pneumonia, tend to be far more serious conditions than upper respiratory infections, such as the common cold.

    Anaphylaxis Severe allergic reaction

    Anaphylaxis is a serious allergic reaction that is rapid in onset and may cause death. It typically causes more than one of the following: an itchy rash, throat or tongue swelling, shortness of breath, vomiting, lightheadedness, and low blood pressure. These symptoms typically come on over minutes to hours.

    Adrenal insufficiency human disease

    Adrenal insufficiency is a condition in which the adrenal glands do not produce adequate amounts of steroid hormones, primarily cortisol; but may also include impaired production of aldosterone, which regulates sodium conservation, potassium secretion, and water retention. Craving for salt or salty foods due to the urinary losses of sodium is common.

    Beclometasone dipropionate was first patented in 1962 and used medically in 1972. [7] It was approved for medical use in the United States in 1976. [1] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. [8] The wholesale price in the developing world for an inhaler containing 200 doses of medication is about US$3.20 as of 2014. [9] In the United States it costs between 50 and US$100 for a typical month supply of the inhaled form. [10]

    A health system, also sometimes referred to as health care system or as healthcare system, is the organization of people, institutions, and resources that deliver health care services to meet the health needs of target populations.

    Side effects

    Occasionally, it may cause a cough upon inhalation. Deposition on the tongue and throat may promote oral candidiasis, which appears as a white coating, possibly with irritation. [11] [12] [13] This may usually be prevented by rinsing the mouth with water after using the inhaler. Other adverse drug reaction side effects may rarely include: a smell similar to burning plastic, unpleasant taste, hoarseness or nasal congestion, pain or headache, and visual changes. Allergic reactions may occur, but rarely.

    Cough medical symptom, reflex to clear large breathing passages

    A cough is a sudden, and often repetitively occurring, protective reflex which helps to clear the large breathing passages from fluids, irritants, foreign particles and microbes. The cough reflex consists of three phases: an inhalation, a forced exhalation against a closed glottis, and a violent release of air from the lungs following opening of the glottis, usually accompanied by a distinctive sound.

    Tongue mouth organ that tastes and facilitates speech

    The tongue is a muscular organ in the mouth of most vertebrates that manipulates food for mastication, and is used in the act of swallowing. It is of importance in the digestive system and is the primary organ of taste in the gustatory system. The tongue's upper surface (dorsum) is covered by taste buds housed in numerous lingual papillae. It is sensitive and kept moist by saliva, and is richly supplied with nerves and blood vessels. The tongue also serves as a natural means of cleaning the teeth. A major function of the tongue is the enabling of speech in humans and vocalization in other animals.

    Throat anterior part of the neck, in front of the vertebral column

    In vertebrate anatomy, the throat is the front part of the neck, positioned in front of the vertebra. It contains the pharynx and larynx. An important section of it is the epiglottis, which is a flap separating the esophagus from the trachea (windpipe) preventing food and drink being inhaled into the lungs. The throat contains various blood vessels, pharyngeal muscles, the nasopharyngeal tonsil, the tonsils, the palatine uvula, the trachea, the esophagus, and the vocal cords. Mammal throats consist of two bones, the hyoid bone and the clavicle. The "throat" is sometimes thought to be synonymous for the isthmus of the fauces.

    Nasal corticosteroids may be associated with central serous retinopathy. [14]

    Central serous retinopathy

    Central serous retinopathy (CSR), also known as central serous chorioretinopathy, is an eye disease that causes visual impairment, often temporary, usually in one eye. When the disorder is active it is characterized by leakage of fluid under the retina that has a propensity to accumulate under the central macula. This results in blurred or distorted vision (metamorphopsia). A blurred or gray spot in the central visual field is common when the retina is detached. Reduced visual acuity may persist after the fluid has disappeared.

    Names

    Beclometasone dipropionate is the INN modified and beclomethasone dipropionate is the USAN and former BAN. It is a prodrug of the free form, beclometasone (INN).

    United States Adopted Names are unique nonproprietary names assigned to pharmaceuticals marketed in the United States. Each name is assigned by the USAN Council, which is co-sponsored by the American Medical Association (AMA), the United States Pharmacopeial Convention (USP), and the American Pharmacists Association (APhA).

    A British Approved Name (BAN) is the official, non-proprietary, or generic name given to a pharmaceutical substance, as defined in the British Pharmacopoeia (BP).
    The BAN is also the official name used in some countries across the world, because starting in 1953, proposed new names were evaluated by a panel of experts from WHO in conjunction with the BP commission to ensure naming consistency worldwide.

    A prodrug is a medication or compound that, after administration, is metabolized into a pharmacologically active drug. Inactive prodrugs are pharmacologically inactive medications that are metabolized into an active form within the body. Instead of administering a drug directly, a corresponding prodrug might be used instead to improve how a medicine is absorbed, distributed, metabolized,and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects.

    Clenil, Qvar are brandnames for the inhalers. Beconase, Alanase, Vancenase, Qnasl for the nasal spray or aerosol.

    Related Research Articles

    A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal congestion in the upper respiratory tract. The active ingredient in most decongestants is either pseudoephedrine or phenylephrine. Intranasal corticosteroids can also be used as decongestants and antihistamines can be used to alleviate runny nose, nasal itch, and sneezing.

    Salbutamol chemical compound

    Salbutamol, also known as albuterol and marketed as Ventolin among other brand names, is a medication that opens up the medium and large airways in the lungs. It is used to treat asthma, including asthma attacks, exercise-induced bronchoconstriction, and chronic obstructive pulmonary disease (COPD). It may also be used to treat high blood potassium levels. Salbutamol is usually used with an inhaler or nebulizer, but it is also available as a pill and intravenous solution. Onset of action of the inhaled version is typically within 15 minutes and lasts for two to six hours.

    Hydrocortisone the hormone cortisol when supplied as a medication

    Hydrocortisone, sold under a number of brand names, is the name for the hormone cortisol when supplied as a medication. Uses include conditions such as adrenocortical insufficiency, adrenogenital syndrome, high blood calcium, thyroiditis, rheumatoid arthritis, dermatitis, asthma, and COPD. It is the treatment of choice for adrenocortical insufficiency. It can be given by mouth, topically, or by injection. Stopping treatment after long-term use should be done slowly.

    Ipratropium bromide chemical compound

    Ipratropium bromide, sold under the trade name Atrovent among others, is a medication which opens up the medium and large airways in the lungs. It is used to treat the symptoms of chronic obstructive pulmonary disease and asthma. It is used by inhaler or nebulizer. Onset of action is typically within 15 to 30 minutes and lasts for three to five hours.

    Nicotine replacement therapy

    Nicotine replacement therapy (NRT) is a medically-approved way to take nicotine by means other than tobacco. It is used to help with quitting smoking or stopping chewing tobacco. It increases the chance of quitting smoking by about 50% to 70%. Often it is used along with other behavioral techniques. NRT has also been used to treat ulcerative colitis. Types of NRT include the adhesive patch, chewing gum, lozenges, nose spray, and inhaler. The use of more than one type of NRT at a time may increase effectiveness.

    Salmeterol chemical compound

    Salmeterol is a long-acting β2 adrenergic receptor agonist (LABA) used in the maintenance and prevention of asthma symptoms and maintenance of chronic obstructive pulmonary disease (COPD) symptoms. Symptoms of bronchospasm include shortness of breath, wheezing, coughing and chest tightness. It is also used to prevent breathing difficulties during exercise.

    Betamethasone chemical compound: steroid medication

    Betamethasone is a steroid medication. It is used for a number of diseases including rheumatic disorders such as rheumatoid arthritis and systemic lupus erythematosus, skin diseases such as dermatitis and psoriasis, allergic conditions such as asthma and angioedema, preterm labor to speed the development of the baby's lungs, Crohn's disease, cancers such as leukemia, and along with fludrocortisone for adrenocortical insufficiency, among others. It can be taken by mouth, injected into a muscle, or applied as a cream. When given by injection, anti-inflammatory effects begin in around two hours and last for seven days.

    Ketorolac chemical compound

    Ketorolac, sold under the brand name Toradol among others, is a nonsteroidal anti-inflammatory drug (NSAID) and is used as an pain medication. It is considered a first-generation NSAID.

    Nasal congestion symptom

    Nasal congestion is the blockage of the nasal passages usually due to membranes lining the nose becoming swollen from inflamed blood vessels.

    Fluticasone propionate chemical compound

    Fluticasone propionate, sold under the brand names Flovent and Flonase among others, is a steroid medication. When inhaled it is used for the long term management of asthma and COPD. In the nose it is used for hay fever and nasal polyps.

    Pyrantel chemical compound

    Pyrantel is a medication used to treat a number of parasitic worm infections. This includes ascariasis, hookworm infections, enterobiasis, trichostrongyliasis, and trichinellosis. It is taken by mouth.

    Benzylpenicillin chemical compound

    Benzylpenicillin, also known as penicillin G, is an antibiotic used to treat a number of bacterial infections. This includes pneumonia, strep throat, syphilis, necrotizing enterocolitis, diphtheria, gas gangrene, leptospirosis, cellulitis, and tetanus. It is not a first-line agent for pneumococcal meningitis. Benzylpenicillin is given by injection into a vein or muscle. Two long-acting forms benzathine benzylpenicillin and procaine benzylpenicillin are available for use by injection into a muscle.

    Benzathine benzylpenicillin chemical compound

    Benzathine benzylpenicillin, also known as benzathine penicillin G, is an antibiotic useful for the treatment of a number of bacterial infections. Specifically it is to treat strep throat, diphtheria, syphilis, and yaws. It is also used to prevent rheumatic fever. It is given by injection into a muscle.

    Procaine benzylpenicillin also known as penicillin G procaine, is an antibiotic useful for the treatment of a number of bacterial infections. Specifically it is used for syphilis, anthrax, mouth infections, pneumonia, diphtheria, cellulitis, and animal bites. It is given by injection into a muscle.

    Ethinylestradiol/norethisterone, also known as ethinyl estradiol/norethindrone, is a combination birth control pill made up of ethinylestradiol, an estrogen and norethisterone a progestin. It is used for birth control, symptoms of menstruation, endometriosis, and menopausal symptoms. Other uses include acne. It is taken by mouth.

    Budesonide chemical compound

    Budesonide (BUD), sold under the brand name Pulmicort among others, is a medication of the corticosteroid type. It is available as an inhaler, pill, nasal spray, and rectal forms. The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease (COPD). The nasal spray is used for allergic rhinitis and nasal polyps. The pills in a delayed release form and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis and microscopic colitis.

    Ethinylestradiol/levonorgestrel is a combined birth control pill made up of ethinylestradiol, an estrogen and levonorgestrel a progestin. It is used for birth control, symptoms of menstruation, endometriosis, and as emergency contraception. It is taken by mouth.

    Dextran 70 is a type of fluid given by injection into a vein to expand blood volume. Specifically it is used for shock such as that caused by bleeding or burns when blood transfusions are not quickly available. However, it does not carry oxygen.

    References

    1. 1 2 3 4 5 6 "Beclomethasone Dipropionate". The American Society of Health-System Pharmacists. Archived from the original on 2015-12-08. Retrieved Dec 2, 2015.
    2. "List of products: BECLOMETASONE DIPROPIONATE". MHRA. Archived from the original on 8 December 2015. Retrieved 6 December 2015.
    3. "Beclometasone dipropionate 0.25 mg/g Cream" (PDF). MHRA. Archived (PDF) from the original on 8 December 2015. Retrieved 6 December 2015.
    4. 1 2 3 "Clipper" (PDF). MHRA. Archived from the original (PDF) on 2015-12-08. Retrieved 6 December 2015.
    5. "Beclomethasone Dipropionate eent". The American Society of Health-System Pharmacists. Archived from the original on 2015-12-08. Retrieved Dec 2, 2015.
    6. Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 349. ISBN   9781284057560.
    7. McPherson, Edwin M. (2007). Pharmaceutical Manufacturing Encyclopedia (3rd ed.). Burlington: Elsevier. p. 539. ISBN   9780815518563. Archived from the original on 2015-12-08.
    8. "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
    9. "Beclometasone". International Drug Price Indicator Guide. Retrieved 6 December 2015.
    10. Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 451. ISBN   9781284057560.
    11. Willey R, Milne L, Crompton G, Grant I (1976). "Beclomethasone dipropionate aerosol and oropharyngeal candidiasis". Br J Dis Chest. 70 (1): 32–8. doi:10.1016/0007-0971(76)90004-8. PMID   1259918.
    12. Salzman G, Pyszczynski D (1988). "Oropharyngeal candidiasis in patients treated with beclomethasone dipropionate delivered by metered-dose inhaler alone and with Aerochamber". J Allergy Clin Immunol. 81 (2): 424–8. doi:10.1016/0091-6749(88)90911-6. PMID   3339197.
    13. Fukushima C, Matsuse H, Tomari S, Obase Y, Miyazaki Y, Shimoda T, Kohno S (2003). "Oral candidiasis associated with inhaled corticosteroid use: comparison of fluticasone and beclomethasone". Ann Allergy Asthma Immunol. 90 (6): 646–51. doi:10.1016/S1081-1206(10)61870-4. PMID   12839324.
    14. Haimovici R, Gragoudas ES, Duker JS, Sjaarda RN, Eliott D (October 1997). "Central serous chorioretinopathy associated with inhaled or intranasal corticosteroids". Ophthalmology. 104 (10): 1653–60. doi:10.1016/s0161-6420(97)30082-7. PMID   9331207.