Deflazacort + Tamsulosin

Usage

• This combination medication is primarily prescribed for the medical expulsive therapy (MET) of ureteric stones (kidney stones), specifically those ≤10 mm in size located in the distal ureter. It aids in the passage of stones by reducing inflammation and relaxing the muscles of the urinary tract.

• Pharmacological Classification:

  • Deflazacort: Corticosteroid, Anti-inflammatory
  • Tamsulosin: Alpha-1 adrenergic receptor antagonist

• Mechanism of Action:

  • Deflazacort reduces inflammation in the kidneys, which facilitates the passage of stones.
  • Tamsulosin relaxes the smooth muscles in the prostate and bladder neck, easing urine flow and aiding stone expulsion.

Alternate Names

• No widely recognized alternate names for the combination exist. The individual components are sometimes referred to as:

  • Deflazacort: Calcort, Deflazacort, Emflaza
  • Tamsulosin: Flomax, Jalyn

• Brand Names: Defcort TM, TASMULINE DFZ

How It Works

• Pharmacodynamics:

  • Deflazacort: Binds to glucocorticoid receptors, modulating gene expression and suppressing inflammatory pathways.
  • Tamsulosin: Selectively blocks alpha-1A adrenergic receptors in the prostate and bladder neck, causing smooth muscle relaxation.

• Pharmacokinetics:

  • Deflazacort: Well-absorbed orally, metabolized in the liver, excreted primarily in urine.
  • Tamsulosin: Absorbed orally, metabolized in the liver by CYP3A4 and CYP2D6 enzymes. Elimination half-life of 9-13 hours, primarily excreted via urine.

• Mode of Action:

  • Deflazacort: Inhibits inflammatory mediators (cytokines, prostaglandins, leukotrienes) and reduces capillary permeability.
  • Tamsulosin: Decreases smooth muscle tone in the lower urinary tract, relieving obstruction.

• Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Deflazacort: Glucocorticoid receptor agonist. Tamsulosin: Alpha-1A adrenergic receptor antagonist.

• Elimination Pathways: Deflazacort: Primarily renal excretion. Tamsulosin: Hepatic metabolism and renal excretion.

Dosage

Standard Dosage

Adults:

• Tamsulosin 0.4 mg + Deflazacort 30 mg once daily, preferably after a meal. For MET, Deflazacort is often given for a shorter duration (e.g., 10 days) while Tamsulosin can be continued for up to 28 days.

Children:

• Use in children below 18 years is not recommended due to limited safety and efficacy data.

Special Cases:

• Elderly Patients: Dosage adjustments may be necessary. Close monitoring recommended.
• Patients with Renal Impairment: Dose adjustments are necessary. Individualized dosing based on renal function.
• Patients with Hepatic Dysfunction: Caution is advised, as both drugs are metabolized in the liver.
• Patients with Comorbid Conditions: Individualized dosing and close monitoring are essential.

Clinical Use Cases

• Intubation, Surgical Procedures, Mechanical Ventilation, ICU Use, Emergency Situations: Not typically used in these settings for kidney stones.

Dosage Adjustments

• Adjust based on individual patient characteristics, including renal and hepatic function and other medical conditions.

Side Effects

Common Side Effects

• Dizziness, headache, nausea, diarrhea, cold symptoms, runny nose, ejaculation disorder, increased appetite, weight gain, fluid retention, insomnia.

Rare but Serious Side Effects

• Bone degradation, bone fracture, electrolyte imbalance, cataract, depressed mood, severe dizziness or fainting, chest pain, vision problems, high blood pressure, elevated blood sugar levels, signs of infection (e.g., fever, chills, sore throat)

Long-Term Effects

• Prolonged use of corticosteroids like Deflazacort can lead to adrenal suppression, osteoporosis, increased risk of infections, and other systemic effects.

Adverse Drug Reactions (ADR)

• Severe allergic reactions, angioedema, hypotension

Contraindications

• Hypersensitivity to deflazacort or tamsulosin.
• Severe hepatic or renal impairment.
• Systemic fungal infections.
• Use with caution in patients with diabetes, cardiovascular disease, glaucoma, or low bone mineral density.

Drug Interactions

• Alpha-blockers (doxazosin, prazosin, terazosin), antihypertensive medications, antibiotics (clarithromycin, erythromycin), antifungals (ketoconazole, itraconazole), and CYP3A4 inhibitors or inducers.

• Alcohol should be avoided as it can potentiate side effects.

• Grapefruit juice may interact with metabolism.

Pregnancy and Breastfeeding

• The safety of this combination during pregnancy and breastfeeding has not been established. Use only if the potential benefits outweigh the risks. Consult with a physician.

Drug Profile Summary

• Mechanism of Action: Deflazacort: Reduces inflammation. Tamsulosin: Relaxes smooth muscles in the urinary tract.
• Side Effects: Dizziness, headache, nausea, increased infection risk.
• Contraindications: Hypersensitivity, severe hepatic/renal impairment, systemic fungal infections.
• Drug Interactions: Alpha-blockers, antihypertensives, antibiotics, antifungals.
• Pregnancy & Breastfeeding: Consult a physician. Safety not established.
• Dosage: 0.4mg Tamsulosin + 30mg Deflazacort once daily.
• Monitoring Parameters: Renal function, blood pressure, blood sugar, signs of infection.

Popular Combinations

• Not applicable. This combination is itself a common pairing for MET.

Precautions

• Monitor for side effects, especially with long-term use.
• Caution in patients with pre-existing medical conditions.
• Evaluate renal and hepatic function before and during treatment.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Deflazacort + Tamsulosin?

A: The standard adult dosage is Tamsulosin 0.4 mg + Deflazacort 30 mg once daily.

Q2: Can this combination be used in children?

A: It’s not recommended for children under 18 due to insufficient safety data.

Q3: What are the common side effects?

A: Dizziness, headache, nausea, and cold symptoms are common.

Q4: Are there any serious side effects?

A: Yes, rare but serious side effects include bone degradation and increased risk of infections.

Q5: What are the contraindications for this combination?

A: Contraindications include hypersensitivity to either drug, severe liver or kidney disease, and systemic fungal infections.

Q6: Can I take this medication if I am pregnant or breastfeeding?

A: Consult your doctor. Safety in pregnancy and breastfeeding is not well-established.

Q7: How does this combination work for kidney stones?

A: Deflazacort reduces inflammation, and Tamsulosin relaxes the urinary tract muscles to facilitate stone passage.

Q8: What are the potential drug interactions?

A: Interactions can occur with other alpha-blockers, antihypertensives, certain antibiotics and antifungals.

Q9: Can this combination cause weight gain?

A: Yes, weight gain is a possible side effect of deflazacort.

Q10: Should this medicine be taken with food?

A: Yes, it’s recommended to take this medicine after a meal to improve absorption and reduce gastrointestinal side effects.