Pulmicort Flexhaler

Dosage for Budesonide varies significantly based on the condition being treated and the formulation prescribed by your doctor.

• Asthma (Inhalation): The typical starting dose for adults is 360 mcg twice daily. Some patients may start as low as 180 mcg twice daily. The maximum recommended dose is usually 720 mcg twice daily.
• Crohn’s Disease (Oral): For the induction of remission, the standard dose is 9 mg taken once daily in the morning for up to 8 weeks. For maintaining remission, your doctor may prescribe 6 mg once daily for up to 3 months.
• Ulcerative Colitis (Oral): The usual dose is 9 mg once daily in the morning for up to 8 weeks.
• Allergic Rhinitis (Nasal): The standard dose is 1 to 2 sprays in each nostril once daily (32 mcg per spray).

Budesonide is approved for use in children for specific conditions, but dosing must be strictly monitored by a pediatrician.

• Asthma (Nebulized Respules): For children aged 12 months to 8 years, the dose ranges from 0.25 mg to 1.0 mg total daily dose, administered via a jet nebulizer.
• Asthma (Inhaler): For children aged 6 years and older, the starting dose is usually 180 mcg twice daily.
• Crohn’s Disease: For children weighing more than 25 kg with mild-to-moderate Crohn's, a dose of 9 mg daily for 8 weeks followed by a taper is common, though this is often based on clinical judgment.
• Allergic Rhinitis: Approved for children 6 years and older, typically 1 spray per nostril daily.

Renal Impairment

No specific dosage adjustments are typically required for patients with renal (kidney) impairment, as the drug is primarily metabolized by the liver. However, patients should be monitored for systemic corticosteroid effects.

Hepatic Impairment

Since Budesonide is cleared by the liver, patients with moderate to severe hepatic impairment (liver disease) may experience higher levels of the drug in their blood. Your doctor may need to monitor you more closely for signs of 'Cushingoid' symptoms (like a round face or weight gain) and may consider a lower dose.

Elderly Patients

In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

• Oral Capsules/Tablets: These should be swallowed whole in the morning. Do not crush, chew, or break them, as they have a special coating designed to release the medicine in specific parts of the intestine. They can usually be taken with or without food.
• Inhalers: After using a Budesonide inhaler, you MUST rinse your mouth with water and spit it out. This helps prevent 'thrush' (a yeast infection in the mouth). Always use the specific technique (e.g., 'breathe out, then inhale deeply') taught by your pharmacist.
• Nasal Spray: Shake gently before use. Clear your nasal passages before spraying.
• Storage: Store all forms at room temperature (68°F to 77°F), away from moisture, heat, and light.

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and return to your regular schedule. Do not double the dose to catch up. Consistency is key for managing chronic inflammation.

Acute overdosage with Budesonide is unlikely to be life-threatening. However, chronic overdosage (taking too much over a long period) can lead to systemic corticosteroid effects such as hypercorticism and adrenal suppression. Symptoms of chronic overdose include thinning skin, easy bruising, changes in body fat distribution (especially in the face, neck, and waist), and increased acne or facial hair. If you suspect an overdose, contact your local poison control center or seek emergency medical attention.

> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking Budesonide without medical guidance, as sudden discontinuation can lead to a flare-up of your symptoms or withdrawal-like effects.

Common side effects are often related to the specific method of delivery. For inhaled Budesonide, the most frequent issues include:

• Nasopharyngitis: This feels like a common cold, characterized by a sore throat, runny nose, or nasal congestion. It typically lasts a few days as the body adjusts.
• Oral Candidiasis (Thrush): This appears as white patches on the tongue or inside the cheeks. It can cause a cottony feeling in the mouth or loss of taste. Rinsing the mouth after use significantly reduces this risk.
• Headache: Mild to moderate headaches are common when starting oral or nasal Budesonide.
• Upper Respiratory Tract Infection: Increased susceptibility to minor coughs or sinus pressure.

• Dyspepsia and GI Distress: Some patients taking oral Budesonide report nausea, flatulence (gas), or stomach pain.
• Mood Changes: Nervousness, restlessness, or trouble sleeping (insomnia) can occur as corticosteroids can stimulate the central nervous system.
• Skin Changes: Easy bruising (ecchymosis) or acne may develop, particularly with oral forms.
• Muscle Cramps: Some patients report minor muscle aches or tremors.

• Hypersensitivity: This includes rash, itching, or hives.
• Glaucoma or Cataracts: Increased pressure in the eye or clouding of the lens has been reported with long-term use of both inhaled and oral corticosteroids.
• Growth Retardation: In pediatric patients, a slight slowing of growth velocity may occur, though the final adult height is usually not significantly affected if monitored.
• Psychiatric Symptoms: Rare cases of depression, aggression, or anxiety have been noted.

> Warning: Stop taking Budesonide and call your doctor immediately if you experience any of these serious symptoms.

• Anaphylaxis: Signs include difficulty breathing, swelling of the face, lips, or tongue, and severe dizziness. This is a medical emergency.
• Adrenal Insufficiency: This occurs when the body stops producing its own natural cortisol. Symptoms include extreme tiredness, muscle weakness, loss of appetite, weight loss, and feeling lightheaded.
• Severe Infections: Because steroids suppress the immune system, you may develop serious fungal, bacterial, or viral infections (like chickenpox or measles) that become life-threatening.
• Bronchospasm: Occasionally, an inhaler can cause immediate wheezing and chest tightness right after use. Use a rescue inhaler and contact your doctor.
• Vision Changes: Blurred vision, eye pain, or seeing halos around lights.

Prolonged use of Budesonide, particularly the oral forms, can lead to systemic effects despite its design for local action:

• Osteoporosis: Corticosteroids can interfere with calcium absorption, leading to weakened bones and increased fracture risk. Your doctor may recommend Vitamin D and Calcium supplements.
• Cushingoid Features: Long-term high doses can cause a 'moon face,' a 'buffalo hump' (fat deposit between the shoulders), and abdominal weight gain.
• Thinning of the Skin: The skin may become fragile and take longer to heal from cuts or scrapes.
• Immune Suppression: You may find that you get sick more often or that minor infections take longer to resolve.

No FDA black box warnings exist for Budesonide. However, there are significant warnings regarding the transfer of patients from systemic corticosteroid therapy (like oral prednisone) to Budesonide. Because Budesonide has lower systemic activity, it may not provide enough steroid to a body that has become dependent on prednisone, potentially leading to a life-threatening adrenal crisis.

Report any unusual symptoms to your healthcare provider. Your doctor will weigh the benefits of controlling your inflammation against the risks of these side effects.

Budesonide is a powerful medication that requires careful management. It is essential to understand that Budesonide is not a 'rescue' medication. For asthma, it will not stop an ongoing attack; for IBD, it will not provide instant relief. It is designed for long-term control. Patients must also be aware of the 'steroid-sparing' nature of this drug, which means it has fewer side effects than prednisone but is not entirely risk-free.

As of 2026, there are no FDA black box warnings for Budesonide. However, clinical guidelines emphasize that deaths due to adrenal insufficiency have occurred in patients transferring from systemic steroids to less systemically available steroids like Budesonide.

• Immunosuppression: Budesonide can mask signs of infection and make you more susceptible to new infections. Avoid exposure to chickenpox or measles if you have not been vaccinated. If exposed, contact your doctor immediately.
• Adrenal Suppression: If you are under stress (surgery, severe infection, or injury), your body may not be able to produce enough natural cortisol while on Budesonide. You may need supplemental systemic steroids during these times.
• Hypercorticism: Some patients are more sensitive to steroids than others. If you develop a round face, acne, or significant weight gain, your dose may need adjustment.
• Bone Mineral Density: Patients with a history of osteoporosis or those at high risk (e.g., smokers, sedentary lifestyle) should have their bone density monitored, as steroids can decrease bone formation.
• Ocular Effects: Long-term use increases the risk of cataracts and glaucoma. Regular eye exams are recommended for those on long-term therapy.

Your healthcare provider will likely require the following tests while you are taking Budesonide:

• Growth Monitoring: In children, height and weight should be checked regularly to ensure the drug is not significantly impacting growth.
• Eye Exams: Annual or bi-annual checks for intraocular pressure and cataracts.
• Bone Density (DEXA) Scan: Particularly for post-menopausal women or those on long-term oral Budesonide.
• ACTH Stimulation Test: If adrenal suppression is suspected, this test measures how well your adrenal glands are functioning.
• Liver Function Tests: Since the liver metabolizes Budesonide, baseline tests may be required for those with known liver disease.

Budesonide generally does not affect the ability to drive or operate machinery. However, if you experience dizziness or blurred vision as a side effect, you should avoid these activities until you know how the medication affects you.

There is no direct contraindication between Budesonide and alcohol. However, alcohol can irritate the lining of the stomach and intestines. If you are taking oral Budesonide for Crohn's or Ulcerative Colitis, alcohol may worsen your underlying condition or increase the risk of GI side effects.

Do not stop taking Budesonide suddenly, especially if you have been taking it for a long time. Sudden discontinuation can cause a 'rebound' of your inflammatory symptoms or signs of steroid withdrawal (joint pain, fatigue, nausea). Your doctor will provide a tapering schedule to slowly reduce your dose.

> Important: Discuss all your medical conditions, especially any history of tuberculosis, infections, or liver disease, with your healthcare provider before starting Budesonide.

• Strong CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole): These medications block the enzyme that breaks down Budesonide. Using them together can increase the amount of Budesonide in your blood by up to 8-fold, significantly increasing the risk of serious side effects like adrenal suppression.
• Ritonavir and Saquinavir: These HIV medications are extremely potent inhibitors of CYP3A4 and should generally be avoided with Budesonide unless the benefit outweighs the risk of systemic steroid effects.

• Clarithromycin and Erythromycin: These antibiotics can increase Budesonide levels. Your doctor may need to adjust your dose or monitor you for 'Cushingoid' symptoms.
• Cimetidine: This heartburn medication can slightly increase the levels of Budesonide in the blood.
• Live Vaccines (e.g., Measles, Mumps, Rubella): Because Budesonide suppresses the immune system, live vaccines may not work as well or could potentially cause the infection they are meant to prevent. Always consult your doctor before getting any vaccinations.

• Antacids and Proton Pump Inhibitors (PPIs): For oral Budesonide (like Entocort EC), the enteric coating is designed to dissolve at a specific pH (acidity level). Medications that change stomach acidity might cause the coating to dissolve too early, reducing the drug's effectiveness in the lower intestine.
• Estrogens/Oral Contraceptives: These can increase the levels of corticosteroids in the body, potentially enhancing the effects and side effects of Budesonide.

• Grapefruit and Grapefruit Juice: Grapefruit contains compounds that inhibit the CYP3A4 enzyme in the gut. Drinking grapefruit juice while taking oral Budesonide can double or triple the amount of drug absorbed into your bloodstream. You should avoid grapefruit products entirely while on oral Budesonide.
• High-Fat Meals: For certain oral formulations, a high-fat meal can delay the time it takes for the drug to reach peak levels but does not usually change the total amount absorbed.

• St. John’s Wort: This herbal supplement is a potent 'inducer' of CYP3A4. It speeds up the breakdown of Budesonide, which can make the medication less effective at controlling your inflammation.
• Echinacea: Some evidence suggests Echinacea may interfere with the immunosuppressant effects of corticosteroids.

Budesonide may interfere with the results of certain diagnostic tests:

• ACTH Stimulation Test: May show a false-low response, suggesting adrenal insufficiency when it is actually a drug effect.
• Skin Tests: Corticosteroids can suppress the inflammatory response to skin prick tests for allergies, leading to false-negative results. You may need to stop the medication several days before testing.

For each major interaction, the mechanism usually involves the CYP3A4 enzyme system. Inhibition leads to toxicity (too much drug), while induction leads to reduced efficacy (not enough drug). Management usually involves choosing an alternative medication or performing frequent clinical monitoring for steroid side effects.

> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter drugs.

Conditions where Budesonide must NEVER be used include:

• Hypersensitivity: If you have a known severe allergy to Budesonide or any of the ingredients in the formulation (such as milk proteins in some inhalers), you must not use this drug. An allergic reaction can lead to anaphylaxis.
• Status Asthmaticus: Budesonide is contraindicated as the primary treatment for intense, acute episodes of asthma where intensive measures are required. It does not act fast enough to open airways in an emergency.
• Untreated Systemic Infections: If you have a widespread fungal, bacterial, or viral infection that is not being treated, Budesonide can worsen the infection by suppressing your immune response.

These conditions require a careful risk-benefit analysis by your physician:

• Tuberculosis (TB): If you have an active or latent TB infection in the respiratory tract, Budesonide must be used with extreme caution as it can cause the infection to flare up.
• Ocular Herpes Simplex: Steroids can cause a worsening of viral infections in the eye, potentially leading to corneal perforation.
• Liver Cirrhosis: Because the liver is responsible for clearing Budesonide, patients with cirrhosis will have much higher systemic levels of the drug, increasing the risk of side effects.
• Osteoporosis: Patients with significantly reduced bone mineral density should use Budesonide only if the benefits of controlling inflammation outweigh the risk of further bone loss.
• Peptic Ulcer Disease: While Budesonide is 'gut-targeted,' it can still potentially delay the healing of stomach or intestinal ulcers.

Patients who have had allergic reactions to other corticosteroids (such as triamcinolone, fluticasone, or hydrocortisone) may also be sensitive to Budesonide. While not always the case, your doctor should be informed of any previous 'steroid allergies.' Some inhaler formulations contain lactose; patients with severe milk protein allergies (not just lactose intolerance) should avoid these specific brands as they may contain trace amounts of milk proteins that can trigger a reaction.

> Important: Your healthcare provider will evaluate your complete medical history, including any past infections or allergic reactions, before prescribing Budesonide.

Budesonide is generally considered the preferred corticosteroid for the treatment of asthma during pregnancy. According to the FDA and various clinical guidelines, maintaining control of asthma is vital for the health of both the mother and the fetus.

• Risk Category: Historically classified as Category B (animal studies show no risk, or human studies show no risk).
• Data: Large observational studies have not shown an increased risk of congenital malformations when inhaled Budesonide is used during the first trimester.
• Clinical Consideration: While systemic steroids are linked to a slightly higher risk of cleft palate, the low systemic exposure of Budesonide makes this risk much lower. However, oral Budesonide should only be used if the potential benefit justifies the potential risk to the fetus.

Budesonide is excreted in human milk in very small amounts. For inhaled versions, the amount a nursing infant would receive is negligible.

• Safety: Clinical data suggests that use of inhaled Budesonide by a nursing mother is unlikely to result in significant risk to the infant.
• Oral Use: While levels are still low, mothers taking oral Budesonide (9 mg daily) should monitor their infants for signs of adrenal suppression, though this is theoretically unlikely.

Budesonide is widely used in children, but with specific precautions:

• Approved Age: Inhalation suspension (Respules) is approved for children as young as 12 months. Nasal sprays are approved for ages 6 and up.
• Growth Effects: Data from clinical trials show that inhaled corticosteroids may cause a reduction in growth velocity (about 1 cm per year) in pediatric patients. This effect is usually seen in the first year of treatment and is not necessarily linked to final adult height. Doctors should monitor growth regularly.
• Conditions Not Approved: Oral Budesonide for Crohn's is generally not FDA-approved for children under 18, though it is frequently used 'off-label' by pediatric gastroenterologists.

Clinical studies of Budesonide did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

• Considerations: Elderly patients are more likely to have decreased liver function, which can increase Budesonide levels.
• Bone Health: Seniors are at higher risk for osteoporosis; therefore, the effect of Budesonide on bone density should be monitored closely.
• Polypharmacy: Older adults are often on multiple medications (like diltiazem or certain antibiotics) that can interact with Budesonide via the CYP3A4 pathway.

The pharmacokinetics of Budesonide are not significantly altered by kidney disease. No dose adjustment is typically needed for patients with renal failure or those on dialysis. However, since metabolites are excreted renally, monitoring for general steroid side effects is still wise.

Liver function is the most critical factor in Budesonide clearance.

• Mild to Moderate Impairment: Increased systemic exposure is expected.
• Severe Impairment (Child-Pugh Class C): These patients may have significantly elevated levels of Budesonide. Use should be avoided or monitored with extreme caution, as the drug's 'local' advantage is lost when the liver cannot clear the portion that enters the bloodstream.

> Important: Special populations require individualized medical assessment to ensure the safest possible treatment plan.

Budesonide is a potent glucocorticoid with a high ratio of topical anti-inflammatory activity to systemic effects. Its molecular mechanism involves passing through the cell membrane and binding with high affinity to the Glucocorticoid Receptor (GR). This complex then translocates to the nucleus where it binds to DNA.

Specifically, it inhibits the transcription of pro-inflammatory genes that code for cytokines (IL-1, IL-2, IL-4, IL-5, IL-6, IL-8, TNF-alpha), chemokines, and adhesion molecules. It also induces the expression of anti-inflammatory genes like Annexin-1 (which inhibits phospholipase A2, reducing arachidonic acid release) and Mitogen-activated protein kinase phosphatase-1 (MKP-1). This multi-pronged approach reduces airway hyperreactivity in asthma and intestinal mucosal swelling in IBD.

• Onset of Action: For asthma, improvement can be seen within 24 hours, but full effect takes 1-2 weeks. For Crohn's, improvement usually occurs within 2-4 weeks.
• Duration: The anti-inflammatory effects persist for several hours after the drug is cleared from the plasma due to its high tissue binding.
• Dose-Response: There is a clear dose-response relationship for anti-inflammatory effects, but higher doses also increase the risk of HPA (Hypothalamic-Pituitary-Adrenal) axis suppression.

| Parameter | Value |

|---|---|

| Bioavailability | ~10% (Oral), ~20-30% (Inhaled) |

| Protein Binding | 85% to 90% |

| Half-life | 2.0 to 3.6 hours |

| Tmax | 1-2 hours (Inhaled), 3-5 hours (Oral) |

| Metabolism | Hepatic (CYP3A4) |

| Excretion | Renal (60%), Fecal (40%) |

• Molecular Formula: C25H34O6
• Molecular Weight: 430.5 g/mol
• Solubility: Practically insoluble in water; sparingly soluble in ethanol.
• Structure: It is a non-halogenated corticosteroid. It exists as a mixture of two epimers (22R and 22S), with the 22R form being twice as potent as the 22S form.

Budesonide is classified as a Corticosteroid [EPC]. Within this, it is a glucocorticoid. It is related to other medications like fluticasone, mometasone, and beclomethasone, but it is unique due to its exceptionally high first-pass metabolism, making it ideal for targeted local therapy with minimal systemic impact.