Budecort

budecort or budesonide is a corticosteroid that is used as antiinflammotry drug in asthma and chronic obstructive pulmonary diseases.

1. DRUG PRESENTATION BUDECORT PRESENTER :- RITU CHAHAL 2017033

2. INTRODUCTION Budesonide  ( BUD ), 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 .

3. CLASS Budesonide belongs to CORTICOSTEROID.

4. CLASSIFICATION Natural- M ineralocorticoid & glucocorticoid aldosterone hydrocortisone • Synthetic- 1. Short acting : (8-12hrs)hydrocortisone, Cortisone 2. Intermediate acting :(12-36hrs) prednisolone, triamcinolone 3 . Long acting: (36-72hrs) dexamethasone, betamethasone 4. Inhalation : fluticasone, budesonide , beclamethasone 5. Topical: clobetasol, mometasone desonide 6. Mineralocorticoid : fludrocortisone

5. THERAPEUTIC ACTIONS ANTI-INFLAMMATORY EFFECTS , Glucocorticoid steroids such as cortisol or  budesonide  have potent anti-inflammatory  actions  that reduces inflammation and hyper-reactivity (spasm) of the airways caused by asthma. When used as an inhaler, the  budesonide  goes directly to the inner lining of the inflamed airways to exert its  effects . TRADE NAME : Budecort , Plumicort CHEMICAL NAME : Budesonide

6. MECHANISM OF ACTION Corticosteroids binds to the glucocorticosteroid receptor mediate change in gene expression. Glucocorticoid inhibit neutrophil apoptosis and demargination , they inhibit phospholipase A2. Decrease the formation of arachidonic acid derivatives. They inhibit inflammatory transcription factors They promote anti-inflammatory genes like INTERLEUKIN-10

7. PHARMACOKINETICS Onset of action: Nebulization: 2–8 days; Inhalation: 24 hours; Nasal: 10 hours Protein binding : 85% to 90% Half-life elimination: 2–3.6 hours

8. CONT… Absorption: Orally inhaled budesonide is rapidly absorbed in the lungs and peak concentration is typically reached within 20 minutes. After oral administration of budesonide, peak plasma concentration was achieved in about 1–2 hours and the absolute systemic availability was 6–13%, due to extensive first-pass metabolism. Distribution: C rosses placenta, may enter breast milk. Metabolism: In vitro  studies with human liver homogenates have shown that budesonide was rapidly and extensively metabolized. Excretion/Elimination: B udesonide was preferentially cleared by the liver with systemic clearance. Budesonide was excreted in urine(60%) and feces in the form of metabolites.  

9. DOSE AND ADMINISTRATION Adults (including elderly) and Children over 12 Years 200-1,600 mcg daily, in divided doses. 200 mcg twice daily, in the morning and in the evening. During periods of severe asthma the daily dosage can be increased up to 1600 mcg. In less severe cases and children over 12 years of age, 200 - 800 micrograms daily, in divided doses, may be used. In patients whose asthma is well controlled, the daily dose may be reduced below 400 mcg but should not go below 200 mcg.

10. CONT… Children (5 – 12 Years) 200-800 mcg daily, in divided doses. The dose should be reduced to the minimum needed to maintain good asthma control. Patients should be maintained on the lowest dose that will effectively control symptoms.

11. AVAILABLE FORMS Spray Dry Powder Capsules Inhalation Suspension

12. INDICATIONS Rhinocort Aqua: Management of symptoms of seasonal or personal allergies rhinitis in adults and children 6year and older. Respules / Flexhaler : Maintenance treatment of asthma as prophylactic therapy in adults and children 6 yr and for patients requiring corticosteroids for asthma. Inhalation suspension: Maintenance treatment and prophylaxis therapy of asthma in children 1-8 yr. Oral: Treatment and maintenance of clinical remission for upto 3 month of mild to moderate active Crohn’s disease involving the ileum or ascending colon. Unlabeled use: Eosinophilic esophagitis in children.

13. CONTRAINDICATIONS Budesonide is contraindicated as a primary treatment of  status asthmaticus   or other acute episode of asthma where intensive measures are required.  It is also contraindicated for patients who have hypersensitivity to budesonide or any of the excipients. Use cautiously with TB, systemic infection, lactation.

14. DRUG INTERACTION Those taking tablets or capsules orally should avoid grapefruit and grapefruit juice and  echinacea . Grapefruit juice may double  bioavailability  of oral budesonide. Echinacea diminishes bioavailability. Also, high-fat meals delay absorption but do not impede absorption.

15. ADVERSE EFFECTS CNS: Headache, dizziness, lethargy, fatigue, paresthesis , nervousness Dermatologic: rash, edema, pruritis, alopecia. Endocrine: HPA suppression, Cushing’s syndrome with overdose and systematic absorption. GI: Nausea, dyspepsia, dry mouth. Local: nasal irritation, fungal infection. Respiratory; Epistaxis, rebound congestion, pharyngitis, cough. Other: Chest pain, asthenia, moon face, acne, bruising, back pain.

16. NURSING RESPONSIBILITIES Assessment History: Untreated local nasal infections, nasal trauma, septal ulcers, recent nasal surgery, lactation Physical: BP, P, auscultation; R, adventitious sounds; examination of nares Interventions Nasal inhalation Prime pump eight times before first use. If not used for 2 consecutive days, reprime with 1 spray or until fine mist appears. If not used for more than 14 days, rinse applicator and reprime with 2 sprays or until fine mist appears.

17. CONT… Oral Make sure patient does not cut, crush, or chew capsules; they must be swallowed whole. Administer the drug once each day, in the morning; do not administer with grapefruit juice. Encourage patient to complete full 8 week of drug therapy.

18. NURSING TEACHING Inhalation Do not use more often than prescribed; do not stop without consulting your health care provider. It may take several days to achieve good effects; do not stop if effects are not immediate. Use decongestant nose drops first if nasal passages are blocked. Prime unit before use for  Pulmicort Turbuhaler ; rinse mouth after each use. Store  Respules  upright, protect from light; discard open envelopes after 2 weeks; gently shake before use. You may experience these side effects: Local irritation (use your device correctly), dry mouth (suck sugarless lozenges). Report sore mouth, sore throat, worsening of symptoms, severe sneezing, exposure to chickenpox or measles, eye infections.

19. CONT… Oral Take the drug once a day in the morning. Do not cut, crush, or chew the capsules, they must be swallowed whole. If you miss a day, take the capsules as soon as you remember them. Take the next day’s capsules at the regular time. Do not take more than three capsules in a day. Take the full course of the drug therapy (8 weeks in most cases). Do not take this drug with grapefruit juice; avoid grapefruit juice entirely while using this drug. Store  respules  upright, protected from light; discard open envelopes after 2 weeks. Shake before use. You may experience these side effects: Dizziness, headache (avoid driving or operating dangerous machinery if these effects occur); nausea, flatulence (small, frequent meals may help; try to maintain your fluid and food intake). Report chest pain, ankle swelling, respiratory infections, increased bruising.