Nasonex
Nasonex - General Information
Nasonex 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. he 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.
Pharmacology of Nasonex
Nasonex 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. Nasonex 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.
Nasonex for patients
PATIENT'S INSTRUCTIONS FOR USE ASMANEX TWISTHALER 220 mcg (mometasone furoate inhalation powder)
FOR ORAL INHALATION ONLY
Please read this leaflet carefully before taking ASMANEX TWISTHALER. This leaflet does not contain the complete information about this medication. If you have any questions about ASMANEX TWISTHALER, ask your healthcare provider or pharmacist.
IMPORTANT POINTS TO REMEMBER ABOUT ASMANEX TWISTHALER
• Your healthcare provider has prescribed ASMANEX TWISTHALER. It contains a medication called mometasone furoate, which is a synthetic corticosteroid. This medication is used as maintenance treatment that helps prevent and control asthma symptoms.
• ASMANEX TWISTHALER is not a bronchodilator. You should not use ASMANEX TWISTHALER when you are having sudden symptoms of shortness of breath. Use an inhaled short-acting bronchodilator such as albuterol to relieve sudden symptoms of shortness of breath.
• Your healthcare provider may prescribe bronchodilators such as albuterol for emergency relief if an acute asthma attack occurs.
• The inhaler delivers your medication as a very fine powder that you may (b)(4) mell or feel. Whether or not you are able to sense of a dose, not take extra ess your healthcare provider has told you to.
• Use the inhaler regularly and at the same time each day as prescribed by your healthcare provider. Maximum benefit may not be achieved for 1 to 2 weeks or longer. If your symptoms do not improve in that time frame or if your condition worsens, contact your healthcare provider.
Do not use the inhaler if you notice that it is not working correctly. Take it to your healthcare provider or pharmacist.
HOW TO USE
Remove the ASMANEX TWISTHALER from its foil pouch and write the date on the cap label. It's important to throw away the inhaler 45 days after this date or when the dose counter reads "00", whichever comes first.
Step 1. Open inhaler
Hold the inhaler straight up with the pink portion (the base) on the bottom. It is important that you remove the cap of the TWISTHALER while it is in this upright position to make sure that you get the right amount of medicine with each dose.
Holding the pink base, twist the cap in a counter- clockwise direction to remove it. As you lift off the cap, the dose counter on the base will count down by one. (If you began with the dose counter reading "30," this action will cause it to now read "29.") This action loads the device with the medicine that you are now ready to inhale.
IT IS IMPORTANT TO NOTE that the indented arrow (located on the white portion of the TWISTHALER, directly above the pink base) is pointing to the dose counter.
Step 2. Inhale dose
Exhale fully. Then bring the TWISTHALER up to your mouth with the mouthpiece facing toward you. Place it in your mouth, holding it in a horizontal position. Firmly closing your lips around the mouthpiece, take in a fast, deep breath. Since the medication is a very fine powder, you may not be able to feel or taste it after inhalation.
Remove the TWISTHALER from your mouth and hold your breath for about 10 seconds, or as long as you comfortably can.
IMPORTANT: DO NOT BREATHE OUT THROUGH THE INHALER.
After you take your medicine, it is important that you wipe the mouthpiece dry, if necessary, and immediately replace the cap, firmly closing the TWISTHALER.
This is the only way to be sure that your next dose is properly loaded. Be sure that the arrow is in line with the dose-counter window. The cap needs to be put back on and turned in a clockwise direction, as you gently press down. You'll hear a distinctive "click" to let you know that the cap is fully closed.
IT IS IMPORTANT TO REPEAT STEPS 1 AND 2 EACH TIME YOU INHALE.
Rinse your mouth after using.
STORING YOUR INHALER
Keep your inhaler clean and dry at all times. If the device needs cleaning, gently wipe the mouthpiece with a dry cloth or tissue as needed. Do not wash the inhaler. Avoid contact with any liquids.
Store in a dry place at 25°C (77F°); excursions permitted to 15-30°C (59-86°F)
Keep your inhaler out of the reach of young children.
HOW TO KNOW WHEN YOUR INHALER IS EMPTY
The inhaler has a dose indicator window on the pink base. It is a dose counter which displays the number of doses remaining. When the unit reads 01, this indicates the last remaining dose. After dose 01, the counter will read 00, and the cap will lock. The unit must then be discarded.
Nasonex Interactions
In clinical studies, the concurrent administration of the ASMANEX TWISTHALER inhaler and other drugs commonly used in the treatment of asthma was not associated with any unusual adverse events. However, ketoconazole, a potent inhibitor of cytochrome P450 3A4, may increase plasma levels of mometasone furoate during concomitant dosing.
Nasonex Contraindications
ASMANEX TWISTHALER therapy is contraindicated in the primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required. Hypersensitivity to any of the ingredients of this preparation contraindicates its use.
Additional information about Nasonex
Nasonex Indication: The inhaler is indicated for the maintenance treatment of asthma as prophylactic therapy. The nasal spray is indicated for the treatment of the nasal symptoms of seasonal allergic and perennial allergic rhinitis.
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. Nasonex 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Mometasone
Synonyms: Not Available
Drug Category: Anti-Allergic Agents; Anti-inflammatory Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Mometasone: Asmanex Twisthaler; Elocom; Elocon; Mometasone furoate; Nasonex;
Absorption: Nasal spray is virtually undetectable in plasma
Toxicity (Overdose): The potential for acute toxic effects following overdose with the mometasone inhaler is low. However, habitual overuse of the product can cause symptoms of steroid overload, including menstrual irregularities, acne, obesity, and muscle weakness. Single oral doses up to 8000 µg have been studied on human volunteers with no adverse events reported.
Protein Binding: 98% to 99% (in a concentration range of 5 to 500 ng/mL).
Biotransformation: Hepatic. Extensive metabolism to multiple metabolites. There are no major metabolites detectable in plasma. Upon in vitro incubation, one of the minor metabolites formed is 6ß-hydroxy-mometasone furoate. In human liver microsomes, the formation of the metabolite is regulated by cytochrome P-450 3A4.
Half Life: 5.8 hours
Dosage Forms of Nasonex: Spray Intrasinal
Ointment Topical
Lotion Topical
Cream Topical
Chemical IUPAC Name: (9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one
Chemical Formula: C22H28Cl2O4
Mometasone on Wikipedia: https://en.wikipedia.org/wiki/Mometasone
Organisms Affected: Humans and other mammals
