Prophylactic prevention of angina pectoris due to coronary artery disease
Treatment of acute and chronic angina pectoris, hypertension, and myocardial infarction
20 - 120 mg
VOD 0.6 to 0.7 L/kg
5 % protein bound
Similar to other nitrites and organic nitrates, Isosorbide Mononitrate is converted to nitric oxide (NO)
Active intermediate compound which activates the enzyme guanylate cyclase (Atrial natriuretic peptide receptor A).
This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP)
This activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells
Eventually results in the dephosphorylation of the myosin light chain of the smooth muscle fiber.
The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.
By dilating the vessels, it lowers the blood pressure and reduces the left ventricular preload and afterload, therefore, leads to a reduction of myocardial oxygen requirement
Isosorbide mononitrate is primarily metabolized by the liver, but unlike oral isosorbide dinitrate, it is not subject to first-pass metabolism.
Isosorbide mononitrate is cleared by denitration to isosorbide and glucuronidation as the mononitrate
96% of the administered dose excreted in the urine within 5 days and only about 1% eliminated in the feces
At least six different compounds have been detected in urine, with about 2% of the dose excreted as the unchanged drug and at least five metabolites.
Half-life 5 hours
Headache predominates (up to 30%) necessitating withdrawal of 2 to 3 % of patients, but the incidence reduces rapidly as treatment continues .
Tiredness, sleep disturbances (6%) and gastrointestinal disturbances (6%) have been reported during clinical trials with isosorbide mononitrate modified release tablets, but at a frequency no greater than for placebo.
Hypotension (4 to 5%), poor appetite (2.5%), nausea (1%).
Hypotension (4%) with symptoms such as dizziness and nausea (1%) have been reported.
These symptoms generally disappear during long-term treatment.
Other reactions that have been reported with isosorbide mononitrate modified release tablets include tachycardia, vomiting, diarrhoea, vertigo and heartburn