Isordil - Comprehensive Usage Guide: instructions, indications, composition, side effects
Composition
- Active Ingredient: Isosorbide dinitrate
- Excipients: May include lactose monohydrate, microcrystalline cellulose, maize starch, colloidal anhydrous silica, magnesium stearate, and other inactive ingredients depending on the formulation.
Official Forms
- Isordil is available in various formulations, including:
- Tablets: Available in strengths such as 5 mg and 10 mg.
- Sublingual tablets: Available in strengths such as 2.5 mg and 5 mg.
- Extended-release tablets: Available in strengths such as 40 mg.
- Oral spray: Available in strengths such as 1.25 mg per spray.
Pharmacological Group
- Isordil belongs to the pharmacological group of organic nitrates and nitrites (ATC code: C01D A08).
Pharmacological Properties
- Pharmacodynamics: Isosorbide dinitrate is a vasodilator that relaxes smooth muscles in blood vessels, leading to vasodilation and decreased cardiac preload and afterload. It primarily acts by releasing nitric oxide, which activates guanylate cyclase, resulting in increased cyclic guanosine monophosphate (cGMP) levels and smooth muscle relaxation.
- Pharmacokinetics: Isosorbide dinitrate is rapidly absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver to active metabolites. It has a short half-life of about 1 to 4 hours and is primarily excreted in the urine.
Indications
- Isordil is indicated for the prevention and treatment of angina pectoris (chest pain) due to coronary artery disease. It may also be used in the management of congestive heart failure and acute myocardial infarction (heart attack).
Contraindications
- Isordil is contraindicated in individuals with:
- Hypersensitivity to isosorbide dinitrate or any component of the formulation
- Severe anemia
- Hypotension (low blood pressure)
- Circulatory shock
- Increased intracranial pressure
- Concomitant use with phosphodiesterase-5 (PDE-5) inhibitors such as sildenafil (Viagra), tadalafil (Cialis), or vardenafil (Levitra) due to the risk of severe hypotension
- Concomitant use with riociguat, a soluble guanylate cyclase stimulator, due to the risk of hypotension
- Acute myocardial infarction associated with marked hypotension or volume depletion
Interactions
- Isordil may interact with various medications, including other vasodilators, antihypertensive agents, calcium channel blockers, beta-blockers, tricyclic antidepressants, and alcohol, potentially increasing the risk of hypotension or other cardiovascular effects. Caution is advised when co-administering Isordil with these agents.
Specifics of Use
- Isordil tablets should be taken orally with a full glass of water, preferably on an empty stomach. Sublingual tablets should be placed under the tongue and allowed to dissolve completely. The dosage and frequency of administration depend on the patient’s condition and response to therapy.
Pregnancy and Breastfeeding
- Isordil may be used during pregnancy if the potential benefits outweigh the potential risks to the fetus. However, caution is advised, and the lowest effective dose should be used. It is not known whether Isordil is excreted in human breast milk, so breastfeeding mothers should consult a healthcare professional before using Isordil.
Impact on Motor Functions
- Isordil may cause dizziness or lightheadedness, especially when standing up suddenly from a sitting or lying position. Patients should avoid driving or operating machinery until they know how Isordil affects them.
Dosage and Administration
- The recommended dosage of Isordil varies depending on the formulation and the patient’s condition. For the prevention of angina, the usual starting dose of oral Isordil tablets is 5 mg to 20 mg three to four times daily. Sublingual Isordil tablets are used for the acute relief of angina symptoms, with doses ranging from 2.5 mg to 5 mg as needed.
Overdose
- In case of overdose, supportive measures should be initiated as needed. Symptoms of overdose may include severe hypotension, syncope (fainting), dizziness, headache, and methemoglobinemia. Patients should seek medical attention if overdose is suspected.
Side Effects
- Common side effects of Isordil may include:
- Headache
- Dizziness
- Flushing (warmth, redness, or tingling sensation)
- Hypotension
- Tachycardia (rapid heartbeat)
- Nausea or vomiting
- Serious adverse effects such as methemoglobinemia, rebound angina, and tolerance may occur with long-term use or at high doses.
Storage and Shelf Life
- Isordil should be stored at room temperature (15-30°C) in a dry place, protected from light and moisture. Check the expiration date on the packaging and discard any expired or unused medication.
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