Olfosonide

Olfosonide Uses, Dosage, Side Effects, Food Interaction and all others data.

Olfosonide is a synthetic corticosteroid having potent glucocorticoid activity and weak mineralocorticoid activity. It has approximately a 200-fold higher affinity for the glucocorticoid receptor and a 1000-fold higher topical anti-inflammatory potency than cortisol. Corticosteroids have been shown to have a wide range of inhibitory activities against multiple cell types (e.g., mast cell, eosinophil, neutrophil, macrophage, and lymphocyte) and mediators (e.g., histamine, eicosanoids, leukotriene, and cytokine) involved in allergic mediated inflammation.

Olfosonide is a glucocorticoid used to treat respiratory and digestive conditions by reducing inflammation. It has a wide therapeutic index, as dosing varies highly from patient to patient. Patients should be counselled regarding the risk of hypercorticism and adrenal axis suppression.

Trade Name Olfosonide
Availability Prescription only
Generic Budesonide
Budesonide Other Names Budesónida, Budesonide
Related Drugs Entyvio, Humira, Stelara, Dupixent, Tysabri, Xolair, Zeposia, Colazal, ProAir Digihaler, prednisone
Type
Formula C25H34O6
Weight Average: 430.5339
Monoisotopic: 430.23553882
Protein binding

Corticosteroids are generally bound to corticosteroid binding globulin and serum albumin in plasma. Budesonide is 85-90% protein bound in plasma.

Groups Approved
Therapeutic Class Nasal Decongestants & Other Nasal Preparations, Respiratory corticosteroids
Manufacturer
Available Country Greece
Last Updated: September 19, 2023 at 7:00 am
Olfosonide
Olfosonide

Uses

Olfosonide is a glucocorticoid used for the induction of remission in patients with active, mild to moderate ulcerative colitis.

Olfosonide Nebuliser suspension is used for the maintenance treatment and as prophylactic therapy of asthma.

Olfosonide Nasal Spray is used for-

  • Prophylaxis and treatment of seasonal and perennial allergic rhinitis
  • Prophylaxis and treatment of vasomotor rhinitis
  • Symptomatic relief of nasal polyposis
  • Prevention against nasal polyps after polypectomy

Olfosonide Inhaler is used for the maintenance treatment of asthma as prophylactic therapy in adult and paediatric patients six years of age or older. It is also used for patients requiring oral corticosteroid therapy for asthma, many of those patients may be able to reduce or eliminate their requirement for oral corticosteroids over time. Olfosonide inhaler is not used for the relief of acute bronchospasm.

Olfosonide is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Allergies, Asthma, Chronic Obstructive Pulmonary Disease (COPD), Collagenous Colitis, Crohn's Disease (CD), Nasal Congestion, Oesophagitis, Eosinophilic, Polyps, Nasal, Pruritus, Rhinosinusitis, Ulcerative Colitis, Vasomotor Rhinitis, Corticosteroid-responsive dermatoses, Mild Crohn’s Disease, Moderate Crohn’s Disease

How Olfosonide works

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

Dosage

Olfosonide dosage

Children 3 months to 12 years of age: 0.5 - 1 mg twice daily.Adults and elderly: 1 - 2 mg twice daily.

Side Effects

●headache● nausea● upper abdominal pain● fatigue● acne● flatulence● joint pain● urinary tract infection● abdominal distension● constipation

Toxicity

Acute overdose of corticosteroids is rare, however prolonged high dosing of corticosteroids can lead to hypercorticism and adrenal axis suppression. In the case of overdose, reduce the dosage of corticosteroids temporarily.

A 200mg oral dose is lethal to female mice while a 400mg oral dose is lethal to male mice.

Precaution

● Since budesonide is a glucocorticoid, general warnings concerning glucocorticoids should be followed.

● Risk of impaired adrenal function when transferring from glucocorticoid treatment with higher systemiceffects to glucocorticoid treatment with lower systemic effects, such as budesonide. Taper patients slowly fromsystemic corticosteroids if transferring to budesonide.

● Potential worsening of infections (e.g., chickenpox, measles, existing tuberculosis, fungal, bacterial, viral, orparasitic infection). Use with caution in patients with these infections.

● Reduced liver function affects the elimination of glucocorticoid, and increases systemic availability of oralbudesonide.

Interaction

Avoid Cytochrome P450 3A4 inhibitors (e.g. ketoconazole, grapefruit juice). It may cause increased systemic corticosteroid effects. Olfosonide does not affect the plasma levels of oral contraceptives.

Food Interaction

  • Take with or without food. Food delays drug absorption, but not to a clinically significant extent.

[Moderate] GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations and systemic effects of orally administered budesonide.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.

According to the manufacturer, the systemic exposure of oral budesonide approximately doubles after extensive intake of grapefruit juice.

MANAGEMENT: Patients receiving budesonide should avoid the regular consumption of grapefruits and grapefruit juice to prevent undue increases in plasma budesonide levels and systemic effects.

Volume of Distribution

The volume of distribution of budesonide is 2.2-3.9L/kg.

Elimination Route

Extended release oral capsules are 9-21% bioavailable. A 9mg dose reaches a Cmax of 1.50±0.79ng/mL with a Tmax of 2-8h and an AUC of 7.33ng*hr/mL. A high fat meal increases the Tmax by 2.3h but otherwise does not affect the pharmacokinetics of budesonide.

180-360µg metered inhaled doses of budesonide are 34% deposited in the lungs, 39% bioavailable, and reach a Cmax of 0.6-1.6nmol/L with a Tmax of 10 minutes.

A 1mg nebulized dose is 6% bioavailable, reaching a Cmax of 2.6nmol/L with a Tmax of 20 minutes.

A 9mg oral extended release tablet reaches a Cmax of 1.35±0.96ng/mL with a Tmax of 13.3±5.9h and an AUC of 16.43±10.52ng*hr/mL.

Olfosonide rectal foam 2mg twice daily has an AUC of 4.31ng*hr/mL.

Half Life

Olfosonide has a plasma elimination half life of 2-3.6h. The terminal elimination half life in asthmatic children 4-6 years old is 2.3h.

Clearance

Olfosonide has a plasma clearance of 0.9-1.8L/min. The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min. The clearance in asthmatic children 4-6 years old is 0.5L/min.

Elimination Route

Approximately 60% of a budesonide dose is recovered in the urine as the major metabolites 6beta-hydroxybudesonide, 16alpha-hydroxyprednisolone, and their conjugates. No unchanged budesonide is recovered in urine.

Pregnancy & Breastfeeding use

Pregnancy Category CThere are no adequate and well-controlled studies in pregnant women. Olfosonide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.Nursing mothers

Olfosonide is secreted in human milk. So, a decision should be made whether to discontinue nursing or budesonide taking into account the clinical importance of the drug to the mother.

Use in childrenSafety and effectiveness of budesonide in pediatric patients have not been established.Use in Hepatic Impaired patientsMonitor patients for signs and/or symptoms of hypercorticism.

Contraindication

Hypersensitivity to any of the ingredients of Olfosonide.

Acute Overdose

If glucocorticoids are used at excessive doses for prolonged periods, systemic glucocorticoid effects such as hypercorticism and adrenal suppression may occur.

Symptoms: Decreased motor activity, piloerection, generalised oedema. Management: Immediate gastric lavage or emesis followed by supportive and symptomatic treatment.

Innovators Monograph

You find simplified version here Olfosonide

Olfosonide contains Budesonide see full prescribing information from innovator Olfosonide Monograph, Olfosonide MSDS, Olfosonide FDA label

FAQ

What Olfosonide is used for?

Olfosonide is used to prevent difficulty breathing, chest tightness, wheezing, and coughing caused by asthma.

What are the common side effects of Olfosonide?

Common side effects may include:

  • headache, dizziness;
  • indigestion, nausea, vomiting, stomach pain, bloating, gas, constipation;
  • feeling tired;
  • back pain, joint pain;
  • painful urination;
  • cold symptoms such as stuffy nose, sneezing, sore throat;
  • pain anywhere in your body; or
  • signs of too much steroid medicine in your blood.


Is it safe to use Olfosonide?

You should know that budesonide inhalation sometimes causes wheezing and difficulty breathing immediately after it is inhaled. If this happens, use your fast-acting (rescue) asthma medication . Do not use budesonide inhalation again unless your doctor tells you that you should.

Is Olfosonide safe during pregnancy?

Olfosonide recommended doses are safe to use during pregnancy. Oral corticosteroids, at the doses used to treat asthma exacerbations, do not appear to pose a significant risk to the mother or child.

Is Olfosonide safe during breastfeeding?

Olfosonide recommended doses are safe to use during breastfeeding.Oral corticosteroids, at the doses used to treat asthma exacerbations, do not appear to pose a significant risk to the mother or child.

Can I drink alcohol with Olfosonide?

You can't drink alcohol while taking Olfosonide. Taking corticosteroids like Olfosonide can make it hard for your body to fight infections.

Can I take Olfosonide at night?

Olfosonide is usually taken once a day in the morning. Take Olfosonide at around the same time every day.

What does Olfosonide do to the body?

Olfosonide does control and prevent symptoms (wheezing and shortness of breath) caused by asthma.It works directly in the lungs to make breathing easier by reducing the irritation and swelling of the airways.

How many times a day can I take Olfosonide?

Olfosonide can be repeated every 12 hours for a maximum of 36 hours or until clinical improvement.

Should Olfosonide be taken with or without food?

You can take it with or without food. If it upsets your stomach, take it with food. Take your doses at regular intervals. Do not take your medicine more often than directed.

How long can I safely take Olfosonide?

Olfosonide should take once a day in the morning for up to 8 weeks. Your doctor may adjust your dose as needed.

Is Olfosonide safe for long-term use?

Olfosonide at a mean dose of 4.5 mg/day is an effective and safe long-term maintenance therapy in collagenous colitis, which preserves health-related quality of life.

Does Olfosonide raise blood sugar?

Olfosonide may increase blood sugar levels and so may oppose the blood sugar lowering effects of antidiabetic medicines.

Does Olfosonide cause bone loss?

Bone loss is reduced with Olfosonide, but not completely eliminated.

Can Olfosonide cause liver damage?

The mechanism by which Olfosonide might cause serum aminotransferase elevations or liver injury is not known. 

What happens if I suddenly stop taking Olfosonide?

If you suddenly stop taking the Olfosonide, you may also have withdrawal symptoms such as weakness, weight loss, nausea, muscle pain, headache, tiredness, dizziness.

Does Olfosonide weaken immune system?

If you use this Olfosonide long-term it's can weaken your immune system.

Is Olfosonide a strong steroid?

Olfosonide is a potent steroid that undergoes extensive first-pass metabolism.

*** Taking medicines without doctor's advice can cause long-term problems.
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