budesonide rectal

Action and Spectrum

Actions and Spectrum: 

Mechanism of Action: 

• Anti-Inflammatory action: budesonide rectal exerts its therapeutic effects through its potent anti-inflammatory action. It is a glucocorticoid that binds to glucocorticoid receptors in the cells, leading to the modulation of gene expression. This inhibits pro-inflammatory cytokines, chemokines, and other inflammatory mediators, which helps reduce the inflammation in the rectal area. 
• Local Effects: budesonide rectal is designed to act locally in the colon and rectum. After administration, it coats the inflamed mucosa, allowing direct contact with the affected tissues. This localized action helps minimize systemic absorption of the medication, reducing the potential for systemic side effects associated with oral corticosteroids. 

Spectrum of Activity: budesonide rectal is primarily indicated for treating ulcerative colitis, a form of IBD that affects the colon and rectum. It is not typically used to treat Crohn’s disease involving other parts of the digestive tract. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Decreased blood cortisol (17%) 

1-10% 

Nausea (2%) 

Adrenal insufficiency (4%) 

<1% 

Sleep disorder (0.4%) 

Depression (0.4%) 

Insomnia (0.4%) 

Acne (0.4%) 

Hyperglycemia (0.4%)  

Post-marketing reports 

Peripheral edema 

Benign intracranial hypertension 

Maculopapular rash 

Hypertension 

Pyrexia 

Dizziness 

Pruritus 

Allergic dermatitis 

Mood Swings 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

Hypersensitivity 

Caution: 

• Systemic Effects: Although budesonide rectal is designed to act locally and minimize systemic absorption, some absorption into the bloodstream may still occur.  
• Infections: Corticosteroids, including budesonide, can suppress the immune system and increase the risk of infections. If you have an active bacterial, viral, or fungal infection in the rectal area, budesonide rectal should be used with caution.  
• Hypersensitivity: Individuals with known hypersensitivity or allergy to budesonide or its components should avoid using budesonide rectal. 
• Pre-existing Conditions: budesonide rectal should be used cautiously in individuals with certain pre-existing medical conditions, such as diabetes, hypertension, osteoporosis, glaucoma, cataracts, and peptic ulcers.  
• Drug Interactions: budesonide rectal may interact with other medications, including some antifungal agents (e.g., ketoconazole), which can inhibit the metabolism of budesonide, leading to increased systemic exposure. 

Pregnancy / Lactation

Pregnancy consideration: Use cautiously if the benefits outweigh the risks. 

Pregnancy Category: C 

Lactation: Excretion of the drug in human breast milk is known in low concentrations 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

budesonide exerts its pharmacological effects through binding to glucocorticoid receptors within cells. Once bound, the budesonide-glucocorticoid receptor complex is translocated to the cell nucleus, influencing gene expression. This leads to various anti-inflammatory and immunomodulatory effects, including: 

• Inhibition of Pro-inflammatory Cytokines: budesonide suppresses the production and release of pro-inflammatory cytokines, such as interleukin-1 (IL-1), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α). By reducing these inflammatory mediators, budesonide helps to decrease inflammation in the colon and rectum. 
• Inhibition of Phospholipase A2: budesonide inhibits the enzyme phospholipase A2, which releases arachidonic acid from cell membranes. By reducing the availability of arachidonic acid, budesonide indirectly inhibits the synthesis of pro-inflammatory eicosanoids, such as prostaglandins and leukotrienes. 

Pharmacodynamics: 

• Anti-inflammatory action: budesonide rectal exerts potent anti-inflammatory effects locally in the colon and rectum. It inhibits the release of pro-inflammatory cytokines, such as interleukin-1 (IL-1), interleukin-6 (IL-6), and tumor necrosis factor-alpha (TNF-α). By reducing these inflammatory mediators’ production, budesonide helps suppress the immune response and decrease inflammation in the affected area. 
• Immunosuppressive Effects: budesonide rectal acts as an immunosuppressant by inhibiting various immune cell functions. It reduces the migration and activation of inflammatory cells, such as neutrophils, eosinophils, and monocytes, to the inflamed mucosa. This immunosuppressive action helps to control the excessive immune response and subsequent tissue damage associated with IBD. 
• Mucosal healing: budesonide rectal promotes mucosal healing in the colon and rectum. It helps regenerate and repair the damaged epithelial lining, restoring standard tissue structure and function. 
• Localized Effects: budesonide rectal is designed to act locally with minimal systemic absorption. This localized effect helps to reduce the risk of systemic side effects associated with systemic corticosteroids while providing targeted treatment to the affected area. 

Pharmacokinetics: 

Absorption 

budesonide is absorbed after rectal administration, although the specific absorption parameters were not mentioned in the provided data. 

Distribution 

budesonide is highly protein-bound, approximately 85-90% bound to plasma proteins. The volume of distribution (Vd) of budesonide ranges from 2.2 to 3.9 L/kg, indicating extensive distribution throughout the body. 

Metabolism 

budesonide undergoes significant first-pass metabolism in the liver. The primary metabolic pathway of budesonide involves biotransformation by the enzyme CYP3A4 in the liver. The significant metabolites produced are 6-beta-hydroxy budesonide and 16-alpha-hydroxy prednisolone. The glucocorticoid activity of these metabolites is negligible compared to the parent compound. 

Elimination and Excretion 

budesonide has a plasma clearance ranging from 0.9 to 1.8 L/min. The metabolites of budesonide are primarily eliminated in the urine and feces. 

Adminstartion

Administration: 

• Not for oral usage; only for rectal administration  
• Go to the toilet to clear your bowels before administration.  
• Lubricant is already applied to each applicator, although extra lubrication may be achieved using petrolatum or petroleum jelly. 
• Before use, shake the canister briskly for 10 to 15 seconds while warming it in your hands. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: budesonide rectal 

Why do we use budesonide rectal? 

budesonide rectal is primarily used to treat inflammatory bowel diseases (IBD), specifically ulcerative colitis. It is indicated for managing active disease and maintaining remission in patients with mild to moderate distal ulcerative colitis. Here are the primary uses of budesonide rectal: 

• Induction of Remission: budesonide rectal is used to induce remission in patients with active mild to moderate distal ulcerative colitis. It helps reduce inflammation in the rectum and colon, leading to symptom relief and improvement in disease activity. 
• Maintenance of Remission: Once remission is achieved, budesonide rectal may be used as a maintenance therapy to prevent flare-ups and maintain a stable disease state. It helps reduce the risk of disease recurrence and prolongs the time between relapses. 
• Localized Treatment: budesonide rectal is specifically designed for local administration in the colon and rectum. It provides targeted treatment to the affected area, minimizing systemic exposure and reducing the risk of systemic side effects associated with systemic corticosteroids.