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Alvesco

Alvesco - General Information

Alvesco is a glucocorticoid used to treat obstructive airway diseases. It is marketed under the brand name Alvesco.

 

Pharmacology of Alvesco

Alvesco is a pro-drug that is enzymatically hydrolyzed to a pharmacologically active metabolite, C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1) following intranasal application. Des-ciclesonide has anti-inflammatory activity with affinity for the glucocorticoid receptor that is 120 times higher than the parent compound. The precise mechanism through which ciclesonide affects allergic rhinitis symptoms is not known. Corticosteroids have been shown to have a wide range of effects on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic inflammation.

 

Alvesco for patients

Patient's Instructions for Use

OMNARIS (ciclesonide) Nasal Spray, 50 mcg
FOR INTRANASAL ADMINISTRATION ONLY

Please read this leaflet carefully before taking OMNARIS Nasal Spray. This leaflet does not contain the complete information about this medication. If you have any questions about OMNARIS Nasal Spray, ask your health care provider or pharmacist.

What you should know about OMNARIS Nasal Spray.

Your healthcare provider has prescribed OMNARIS Nasal Spray. It contains a medicine called ciclesonide, which helps relieve inflammation. This medication is used for the treatment of nasal symptoms associated with seasonal and year-round nasal allergy symptoms in adults and adolescents 12 years of age and older.

The nasal spray delivers your medication as an aqueous spray. Once you begin treatment, use your nasal spray once a day, every day, as prescribed by your health care provider. OMNARIS Nasal Spray may begin to work within 24 hours after the first dose. Further symptom improvements may occur over 1 to 2 weeks for seasonal allergy symptoms and 5 weeks for year-round allergy symptoms. If your symptoms do not improve in that time frame or if your condition worsens, contact your health care provider.

Dosage

The recommended dose is 2 sprays in each nostril once daily.

You should not use more than a total of 2 sprays in each nostril daily.

Preparing For Use
  1. Remove OMNARIS Nasal Spray from its foil pouch. Count 4 months from this date and write this date (that is 4 months from removing the bottle from the foil pouch) on the sticker provided on the carton. Peel off this sticker and place it in the space provided on your nasal spray bottle. It's important to throw away the nasal spray bottle after this date.
  2. Before the first use, shake the bottle gently and prime the pump by pressing downward on the shoulders of the applicator eight times. Read the complete instructions carefully and use only as directed. If you have not used the nasal spray for 4 days, shake the bottle gently and prime the pump again by spraying one time or until a fine mist appears.
Using the Spray

1. Blow your nose to clear your nostrils if needed.

2. Shake the bottle gently and remove the dust cap.

3. Hold the bottle firmly with your index and middle finger on either side of the spray tip while supporting the base of the bottle with your thumb (Figure 1).

 

Omnaris (Clesonide) Figure 1 Illustration

Figure 1

4. Insert spray tip into one nostril, and close the other nostril with your finger (Figure 2).

 

Omnaris (Clesonide) Figure 2 Illustration

Figure 2

5. Tilt your head forward slightly and keeping the bottle upright, press the pump quickly and firmly and inhale through your nose as you spray (Figure 3). Avoid spraying in eyes or directly onto the nasal septum (the wall between the two nostrils).

 

Omnaris (Clesonide) Figure 3 Illustration

Figure 3

6. Repeat steps 3-5 for the second spray in the same nostril and for each spray in the other nostril.

Storage Instructions

Keep your nasal spray clean and dry at all times. Store medication between 59° and 86° F. Do not freeze. Keep out of the reach of young children.

How To Know When Your Nasal Spray Bottle Is Empty

The amount of nasal spray left can be seen through a window on the bottle. Do not use this bottle for more than the labeled number of sprays or after the “discard by date” you wrote on the sticker when you opened the foil pouch. You may want to obtain a refill before your supply runs out if recommended by your health care provider.

Applicator Cleaning Instructions

After daily use of your nasal spray, wipe the applicator tip with a clean tissue and replace the dust cap.

If the nasal applicator is clogged or requires more thorough cleaning, use the following cleaning instructions (Do not try to unblock the tiny spray hole on the nasal applicator with a pin or other sharp object):

  1. Remove the dust cap and then gently pull upwards to free the nasal applicator.
  2. Wash the dust cap and applicator with warm water.
  3. Dry and replace the nasal applicator.
  4. Prime the unit with one spray or until a fine mist appears.
  5. Replace the dust cap.
Further Information

Avoid spraying in eyes or directly onto the nasal septum (the wall between the two nostrils).

This leaflet does not contain the complete information about your medicine. If you have any questions or are not sure about something, then you should ask your doctor or pharmacist.

You may want to read this leaflet again. Please DO NOT THROW IT AWAY until you have finished your medicine.

 

Alvesco Interactions

Based on in vitro studies in human liver microsomes, des-ciclesonide appears to have no inhibitory or induction potential on the metabolism of other drugs metabolized by CYP 450 enzymes. The inhibitory potential of ciclesonide on CYP450 isoenzymes has not been studied. In vitro studies demonstrated that the plasma protein binding of des-ciclesonide was not affected by warfarin or salicylic acid, indicating no potential for protein binding-based drug interactions.

In a drug interaction study, co-administration of orally inhaled ciclesonide and oral erythromycin, an inhibitor of cytochrome P450 3A4, had no effect on the pharmacokinetics of either des-ciclesonide or erythromycin. In another drug interaction study, co-administration of orally inhaled ciclesonide and oral ketoconazole, a potent inhibitor of cytochrome P450 3A4, increased the exposure (AUC) of des-ciclesonide by approximately 3.6-fold at steady state, while levels of ciclesonide remained unchanged. Therefore, ketoconazole should be administered with caution with intranasal ciclesonide.

 

Alvesco Contraindications

OMNARIS Nasal Spray is contraindicated in patients with a hypersensitivity to any of its ingredients.

 

Additional information about Alvesco

Alvesco Indication: For the treatment of nasal symptoms associated with seasonal and perennial allergic rhinitis in adults and adolescents 12 years of age and older.
Mechanism Of Action: Glucocorticoids such as ciclesonide can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of glucocorticoids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Alvesco reduces inflammatory reaction by limiting the capillary dilatation and permeability of the vascular structures. These compounds restrict the accumulation of polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive kinins. Recent research suggests that corticosteroids may inhibit the release of arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins. Alvesco is a glucocorticoid receptor agonist. On binding, the corticoreceptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing an increase or decrease in expression of specific target genes, including suppression of IL2 (interleukin 2) expression.
Drug Interactions: Itraconazole Increased effects/toxicity of ciclesonide
Ketoconazole Increased effects/toxicity of ciclesonide
Nelfinavir Increased effects/toxicity of ciclesonide
Ritonavir Increased effects/toxicity of ciclesonide
Food Interactions: Not Available
Generic Name: Ciclesonide
Synonyms: Not Available
Drug Category: Anti-Allergic Agents; Glucocorticoids
Drug Type: Small Molecule; Approved
Other Brand Names containing Ciclesonide: Alvesco;
Absorption: Ciclesonide and des-ciclesonide have negligible oral bioavailability (both less than 1%) due to low gastrointestinal absorption and high first-pass metabolism. The intranasal administration of ciclesonide at recommended doses results in negligible serum concentrations of ciclesonide.
Toxicity (Overdose): Not Available
Protein Binding: The percentage of ciclesonide and des-ciclesonide bound to human plasma proteins averaged ≥ 99% each, with ≤ 1% of unbound drug detected in the systemic circulation.
Biotransformation: Des-ciclesonide undergoes metabolism in the liver to additional metabolites mainly by the cytochrome P450 (CYP) 3A4 isozyme and to a lesser extent by CYP 2D6.
Half Life: Not Available
Dosage Forms of Alvesco: Aerosol, metered Nasal
Aerosol, metered Respiratory (inhalation)
Chemical IUPAC Name: Not Available
Chemical Formula: C32H44O7
Ciclesonide on Wikipedia: http://en.wikipedia.org/wiki/Ciclesonide
Organisms Affected: Humans and other mammals