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Pharmacology of Midodrine; Definition, Mechanism of action, Pharmacokinetics, Uses, Effect
🧠 Midodrine Pharmacology Overview
Midodrine is a prodrug alpha-1 adrenergic agonist used primarily to treat symptomatic orthostatic hypotension (OH)—a condition where blood pressure drops upon standing, causing dizziness or fainting. It’s marketed under names like ProAmatine and Orvaten.
⚡ Mechanism of Action
Prodrug activation: Midodrine is converted to desglymidodrine, its active metabolite.
Alpha-1 receptor agonism: Desglymidodrine stimulates arteriolar and venous alpha-1 receptors, increasing vascular tone and blood pressure.
Peripheral selectivity: Minimal central nervous system penetration due to poor blood-brain barrier diffusion.
💊 Pharmacokinetics
Parameter Value
Bioavailability ~93% (as desglymidodrine)
Peak plasma time Midodrine: ~30 min; Desglymidodrine: ~1–2 hrs
Half-life Midodrine: ~25 min; Desglymidodrine: ~3–4 hrs
Excretion ~80% via urine (active renal secretion)
Metabolism Deglycination in tissues and liver
🧬 Pharmacodynamics
Blood pressure elevation: Increases standing systolic BP by ~15–30 mmHg within 1 hour of a 10 mg dose.
Duration: Effects persist for 2–3 hours.
No significant effect on heart rate or cardiac beta receptors.
💊 Therapeutic Uses
Indication Role of Midodrine
Orthostatic hypotension First-line treatment
Refractory ascites (off-label) Adjunct to diuretics
Hepatorenal syndrome (off-label) Combined with octreotide & albumin
Vasovagal syncope (off-label) Symptom reduction
Dialysis-induced hypotension Pre-dialysis BP support
⚠️ Safety & Side Effects
Common: Paresthesia, piloerection, chills, urinary retention, scalp itching.
Serious:
Supine hypertension (BP Greater than 200 mmHg)—monitor closely3
Bradycardia, especially with other heart rate-lowering drugs
Urinary retention
Contraindications: Pheochromocytoma, thyrotoxicosis, acute renal disease, severe heart disease
🧪 Chemical Profile
Property Value
Molecular Formula C₁₂H₁₈N₂O₄
Molecular Weight 254.28 g/mol
Drug Class Alpha-1 adrenergic agonist (prodrug)
Structure Type Ethanolamine derivative
#Midodrine
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