Imdur
Imdur
Generic Name
Imdur
Brand Names
for isosorbide mononitrate (IMN), a *nitrate* vasodilator.
Mechanism
Imdur is the brand name for isosorbide mononitrate (IMN), a *nitrate* vasodilator.
• Release & Metabolism: Oral IMN is rapidly hydrolyzed to isosorbide dinitrate and subsequently to nitric oxide (NO) in the bloodstream.
• NO Pathway: NO activates soluble guanylate cyclase → ↑ cyclic‑guanosine monophosphate (cGMP) → dephosphorylation of myosin light chains → smooth‑muscle relaxation.
• Vascular Effects: Predominant venous dilation reduces preload; at higher doses arterial dilation decreases afterload.
• Result: Decreased myocardial oxygen demand and relief of anginal pain.
Pharmacokinetics
| Parameter | Value / Notes |
| Absorption | 85–90 % bioavailability; peak plasma 30–60 min. |
| Distribution | Volume of distribution ≈ 1.8 L/kg; protein binding low. |
| Metabolism | First‑pass hepatic hydrolysis → isosorbide dinitrate → systemic NO; minimal CYP involvement. |
| Elimination | Renal clearance ≈ 0.3 L/h/kg; half‑life 5–7 h (oral), 1–2 h (sublingual). |
| Special Populations | Adjust for severe renal impairment; not dose‑adjusted in mild–moderate hepatic dysfunction. |
Indications
- Stable angina pectoris – prophylaxis and symptom control.
- Pre‑operative angina prophylaxis (short‑term).
- Short‑acting sublingual form (Imdur® Rapid) for acute anginal attacks (≤30 min onset).
Contraindications
- Absolute Contraindications
- Severe hypotension (SBP <90 mm Hg).
- Known hypersensitivity to nitrates.
- Concomitant use of phosphodiesterase‑5 inhibitors (sildenafil, tadalafil, vardenafil) or NO donors (nitroglycerin).
- Relative
- Recent ischemic stroke or intracranial hemorrhage.
- Severe anemia (hematocrit <25 %).
- Acute myocardial infarction (use cautiously, under supervision).
- Warnings
- *Nitrate tolerance*: requires 10–12 h drug‑free interval daily.
- *Orthostatic hypotension*: especially in elderly, dehydrated, or dehydrating diuretic users.
- *Headache*: common, may indicate high dose or rapid titration.
- *Priapism*: rare but severe; avoid if patient uses PDE5 inhibitors.
Dosing
| Form | Initiation | Titration | Maintenance | Max Daily Dose |
| Oral chewable (5 mg) | 5 mg q12h → 5 mg q8h (if tolerated) | Increase by 5 mg q12h every 3–7 days | 10–20 mg q12h | 160 mg |
| Sublingual (Rapid) | 10 mg q15–20 min for acute angina | 10 mg q12h if needed | 10–20 mg q12h | 160 mg |
• Administration Tips
• Take with a meal if GI upset occurs.
• Do not crush sublingual tablets; chew orally or swallow whole.
• Use a 12–24 h nitrate‑free interval to prevent tolerance.
Adverse Effects
- Common
- Headache (≈30 %)
- Flushing, warmth
- Dizziness, light‑headedness
- Nausea, GI upset (rare)
- Serious
- Severe orthostatic hypotension → syncope or falls
- Priapism (especially with concurrent PDE5 inhibitors)
- Nitrate tolerance → breakthrough angina
- Rare: severe rash or hypersensitivity reactions
Monitoring
- Blood pressure: baseline and after each dose titration; check orthostatic BP.
- Heart rate & ECG: to monitor for arrhythmias or ischemic changes.
- Headache frequency/intensity: dose adjustment or adjunctive therapy if persistent.
- Renal & hepatic panels: annually; more frequently if clinically indicated.
- Patient diary: record angina episodes, dose changes, and side effects.
Clinical Pearls
- Titrate Slowly – 5 mg increments every 3–5 days to avoid headache surge and tolerance.
- Nitrate‑Free Window – a 12‑h drug‑free interval (often overnight) is essential; consider evening dose or split the dose to maintain steady plasma levels.
- Sublingual for Acute – use the Rapid form only for brief, episodic angina; it should *not* replace chronic maintenance dosing.
- Avoid Concomitant NO Donors – even topical nitroglycerin patches can precipitate severe hypotension if taken concurrently.
- Watch for Priapism – counsel patients using PDE5 inhibitors to seek immediate medical help if prolonged erection >4 h.
- Use with Antihypertensives – synergistic BP drop; monitor closely, especially in elderly or volume‑depleted patients.
- Switching from Isosorbide Dinitrate – IMN has a lower risk of tolerance and is preferred for long‑term therapy.
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• *Prepared for medical students and clinicians; references include product labeling and major cardiology guidelines (ACC/AHA 2022, ESC 2022).