Isosorbide-5-Mononitrate Pharmacology


About Isosorbide-5-Mononitrate
Alkyl nitrate derivative, a direct vasodilator, Antianginal.
Mechanism of Action of Isosorbide-5-Mononitrate
It is a direct smooth muscle relaxant, which have a prominent action vascular smooth muscles preferentially veins than arteries. It is enzymatically denitrated in the smooth muscle cells to release the reactive free radical nitric oxide which activates cytosolic guanylyl cyclase thus increases cyclic GMP levels which causes dephosphorylation of myosin light chain kinase(MLCK) through a cyclic GMP dependent protein kinase. Reduced availability of phosphorylated (active) MLCK interferes with activation of myosin and myosin fails to interact with actin to cause contraction and consequently relaxation occurs. Elevated levels of cyclic GMP also reduce calcium entry which also contributing to relaxation. It dilates veins more than arteries because veins have greater amount of enzyme that generate nitric oxide from nitrates. It also preferentially dilates epicardial arteries than autoregulatory arteries duo to defferential distribution of nitrate metabolizing enzymes in these vessels.
It causes preload reduction, slight decrease in after load, and preferential relaxation of larger conducting coronary arteries and is used as an effective drug in the management of both angina and congestive heart failure.

Pharmacokinets of Isosorbide-5-Mononitrate
Absorption: Well absorbed orally, bioavailability is about 100%.
Onset of Action for Isosorbide-5-Mononitrate
30 to 60 minutes
Duration of Action for Isosorbide-5-Mononitrate
Half Life of Isosorbide-5-Mononitrate
4 to 6 hours
Side Effects of Isosorbide-5-Mononitrate
1. Headache
2. Weakness
3. Dizziness
4. Methaemoglobinaemia
5. Flushing
6. Palpitation
7. Orthostatic hypotension
8. Sweating
9. Sub lingual burning
10. Rashes

Contra-indications of Isosorbide-5-Mononitrate
1. Myocardial infarction
2. Hypersensitivity to nitrates
3. Severe hypotension
4. Shock
5. Along with phosphodiesterase inhibitors

Special Precautions while taking Isosorbide-5-Mononitrate
1. Gradually withdraw the drug with caution start therapy with lower doses
2. Hypotension
3. Blood volume depletetion
4. Cerebral haemorrhage
5. Glaucoma

Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Indications for Isosorbide-5-Mononitrate
1. Prophylaxis of angina pectoris
2. Adjunctive treatment of heart failure
3. Post myocardial infarction therapy

Interactions for Isosorbide-5-Mononitrate
Alcohol: Severe hypotension and cardiovascular collapse.
Aspirin: Increase serum concentrations of nitrates and their actions.
Antihypertensives, TCAs, Phenothiazine, Calcium channel blockers: Marked symptomatic orthostatic hypotension.
Lab Tests: May interfere with the Zlatkis-Zak colour reaction causing a false report of decreased serum cholesterol.
Typical Dosage for Isosorbide-5-Mononitrate
10 to 20mg two times daily with 7 hours apart; and first dose in morning.
Sustained release forms: 30 to 60mg once daily; Increased to 120mg once daily if required.

Schedule of Isosorbide-5-Mononitrate
Storage Requirements for Isosorbide-5-Mononitrate
Store at a temperature below 25 degree C. Protects from moisture.
Effects of Missed Dosage of Isosorbide-5-Mononitrate
Effects of Overdose of Isosorbide-5-Mononitrate
Treatment is supportive and symptomatic. Remove drug from the body by gastric lavage and administer activated charcoal to reduce absorption. Monitor blood gas measurements and methemoglobin levels. Supportive measures include respiratory support and oxygen administration. Recumbent positioning and passive movements of the extremities aid venous return. Maintain adequate body temperature and administer I.V. fluids. Administer adrenergic agonist like phenylephrine if required. For Methaemoglobinaemia; methylene blue may be given.

Home Delivery for Isosorbide-5-Mononitrate in Your City

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Isosorbide-5-Mononitrate is a generic medicine name and there are several brands available for it. Some of the brands for isosorbide-5-mononitrate might be better known than isosorbide-5-mononitrate itself. If the pharmacy that's willing to deliver medicines to your home doesn't have isosorbide-5-mononitrate in stock, you can ask for one of the branded alternatives for isosorbide-5-mononitrate.