Isosorbide Mononitrate | apollo +9191 46 950 950

Isosorbide Mononitrate | apollo +9191 46 950 950

Isosorbide Mononitrate

CAS Number : 16051-77-7

Molecular Formula : C6H9NO6

Molecular Weight : 191.1388 g/mol

Systematic (IUPAC) : (3R,3aS,6S,6aR)-6-hydroxy-hexahydrofuro[3,2-b]furan-3-yl nitrate

Type : small molecule

Description

Isosorbide mononitrate is a drug used principally in the treatment of angina pectoris1 and acts by dilating the blood vessels so as to reduce the blood pressure. It is sold by AstraZeneca under the trade name Imdur.

Isosorbide mononitrate is used to for the the prophylactic treatment of angina pectoris; that is, it is

taken in order to prevent or at least reduce the occurrence of angina. Research on Isosorbide

mononitrate as a cervical ripener to reduce time at hospital to birth is supportive.

Isosorbide mononitrate is an active metabolite of isosorbide dinitrate and exerts qualitatively similar

effects. Isosorbide mononitrate reduces the workload of the heart by producing venous and arterial dilation. By

reducing the end diastolic pressure and volume, isosorbide mononitrate lowers intramural pressure,

hence leading to an improvement in the subendocardial blood flow. The net effect when administering isosorbide

mononitrate is therefore a reduced workload for the heart and an improvement in the oxygen

supply/demand balance of the myocardium.

The adverse reactions which follow have been reported in studies with isosorbide mononitrate:

Very common. Headache predominates (up to 30%) necessitating withdrawal of 2 to 3 % of patients, but the

incidence reduces rapidly as treatment continues .

Common. 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%).

Adverse effects associated with the clinical use of the drug are as expected with all nitrate preparations. They

occur mainly in the early stages of treatment.

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

Categories

Vasodilator Agents

Nitrates and Nitrites

Nitric Oxide Donors

Taxonomy

Kingdom : Organic

Classes

Isosorbides

Carbohydrates

Substructures :

Glycerol and Derivatives

Hydroxy Compounds

Oxoazaniums

Ethers

Esters

Isosorbides

Heterocyclic compounds

Furans

Nitrates

Alcohols and Polyols

Carbohydrates

Pharmacology

Indication : For the prevention of angina pectoris due to coronary artery disease and the treatment of acute

and chronic angina pectoris, hypertension, and myocardial infarction.

Pharmacodynamics : Isosorbide-5-mononitrate, the long-acting metabolite of isosorbide dinitrate, is used as

a vasodilatory agent in the management of angina pectoris. 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.

Mechanism of action : Similar to other nitrites and organic nitrates, Isosorbide Mononitrate is converted to nitric oxide (NO), an 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) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting 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.

Absorption : 100%

Volume of distribution : 0.6 to 0.7 L/kg

Protein binding : 5%

Metabolism : Hepatic

Route of elimination : 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, with 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

Clearance

120–122 mL/min [Single dose of 60 mg PO]

151–187 mL/min [Single dose of extended-release tablet 60 mg PO]

132-151 mL/min [Multiple doses of extended release tablet 60 mg PO]

119-140 mL/min [Multiple doses of extended release tablet 120 mg PO]

Toxicity : Symptoms of overdose include

vasodilatation, venous pooling, reduced cardiac output, and hypotension. There are no data suggesting what

dose of isosorbide mononitrate is likely to be life-threatening in humans. In rats and mice, there is

significant lethality at doses of 2000 mg/kg and 3000 mg/kg, respectively.

Affected organisms : Humans and other mammals

What is isosorbide mononitrate?

Isosorbide mononitrate belongs to a group of drugs called nitrates. It dilates (widens) blood vessels, making it easier for blood to flow through them and easier for

the heart to pump.

Isosorbide mononitrate is used to prevent angina attacks (chest pain).

Isosorbide mononitrate will not treat an angina attack that has already begun.

Isosorbide mononitrate may also be used for purposes not listed in this medication guide.

Drug Class And Mechanism

Isosorbide mononitrate is in the class of drugs called nitrates that are used for treating and preventing angina.

Other nitrates include nitroglycerin (Nitrostat, NitroQuick, Nitrolingual, Nitro-Dur and others) and isosorbide dinitrate (Isordil Titradose, Dilatrate-SR, Isochron). Nitrates are vasodilators (dilators of blood vessels). Blood returning from the body in the veins

must be pumped by the heart through the lungs and into the body's arteries against the high pressure in the

arteries. In order to accomplish this work, the heart's muscle must produce and use energy ("fuel") which requires oxygen brought to the heart by the blood.

Angina pectoris (angina) or "heart pain" is due to an inadequate flow of blood (and oxygen) to the muscle of the heart. Nitrates, including isosorbide mononitrate, correct the imbalance between the flow of blood and

oxygen to the heart and the work that the heart must do by dilating the arteries and veins in the body. Dilation of the veins reduces the amount of blood that returns to the

heart that must be pumped. Dilation of the arteries lowers the pressure in the arteries against which the

heart must pump. As a consequence of both effects, the heart works less and requires less blood and oxygen.

Dosing

The recommended dose of isosorbide mononitrate is 20 mg of immediate release tablets twice daily. The two

doses should be administered 7 hours apart in order to avoid tolerance (decreased effect after several doses).

The dose for extended release tablets is 30-240 mg once daily.

Drug Interactions

Sildenafil (Viagra), tadalafil (Cialis) and vardenafil(Levitra) increase the blood pressure lowering

effects of isosorbide mononitrate and may cause excessive reductions in blood pressure. Therefore, patients taking isosorbide mononitrate should not

receive sildenafil, tadalafil or vardenafil.

Severe reductions in blood pressure, especially when changing posture (orthostatic hypotension), may occur when isosorbide mononitrate is combined with calcium channel blockers [for example, diltiazem (Cardizem, Dilacor, Tiazac and several others), verapamil (Calan,

Verelan, Verelan PM, Isoptin, Isoptin SR, Covera-HS)], which also reduce blood pressure.

Uses

Isosorbide mononitrate is used to prevent chest pain (angina) in patients with a certain heart condition

(coronary artery disease). This medication belongs to a class of drugs known as nitrates. It works by relaxing and widening blood vessels so blood can flow more

easily to the heart.This medication will not relieve chest pain once it occurs. It is also not intended to be taken

just before physical activities (such as exercise, sexualactivity) to prevent chest pain. Other medications may be needed in these situations. Consult your doctor for more details.OTHER This section contains uses of

this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition

that is listed in this section only if it has been so prescribed by your health care professional.This medication may also be used with other drugs to

improve the symptoms of heart failure(such as trouble breathing).

How To Use?

Take this medication by mouth, usually twice daily or as directed by your doctor. Take the first dose of the day when you wake up, then take the second dose 7 hours later. It is important to take the drug at the same times

each day. Do not change the dosing times unless directed by your doctor.Use this medication regularly to

get the most benefit from it. Do not stop taking it without consulting your doctor. Some conditions may

become worse when the drug is suddenly stopped. Your dose may need to be gradually decreased.Although

unlikely, when this medication is used for a long time, it may not work as well and may require different dosing. Tell your doctor if this medication stops working well

(for example, you have worsening chest pain or it occurs more often).

Isosorbide is used to prevent or treat chest pain (angina). It works by relaxing the blood vessels to the heart, so the blood and oxygen supply to the heart is

increased.

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

How should this medicine be used?

Isosorbide comes as a regular, sublingual, chewable, and extended-release (long-acting) tablet and extended-

release (long-acting) capsule to be taken by mouth. The tablet usually is taken every 6 hours. The extended-release tablet usually is taken one or two times a day.

The extended-release capsule usually is taken every 8-12 hours. Do not crush, chew, or divide the extended-

release tablets or capsules. The sublingual or chewable tablet is used as needed to relieve chest pain that has already started or to prevent pain before activities

known to provoke attacks (e.g., climbing stairs, sexual activity, heavy exercise, or being outside in cold

weather). The chewable tablet also may be used every 2-3 hours to prevent chest pain. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take isosorbide exactly as directed. Do not take more or

less of it or take it more often than prescribed by your doctor.

Isosorbide controls chest pain but does not cure it. Continue to take isosorbide even if you feel well. Do not stop taking isosorbide without talking to your doctor. Stopping the drug abruptly may cause chest pain.

Isosorbide can lose its effectiveness when used for a long time. This effect is called tolerance. If your angina attacks happen more often, last longer, or are more

severe, call your doctor.

If you are using isosorbide sublingual or chewable tablets for acute chest pain, you should carry the tablets with you at all times. If you are taking isosorbide and

your chest pain is not relieved within 5-10 minutes, take another dose. Call for emergency assistance or go to a

hospital emergency department if pain persists after you have taken three tablets (at 5-10-minute intervals) and

15-30 minutes have passed.

When an attack occurs, sit down. If you use chewable tablets, chew a tablet thoroughly and swallow it. To use the sublingual tablets, place a tablet under your tongue or between your cheek and gum and allow it to dissolve. Do not swallow the tablet. Try not to swallow saliva too

often until the tablet dissolves.

Other uses for this medicine

Isosorbide tablets are also used with other drugs to treat congestive heart failure. Talk to your doctor about the possible risks of using this drug for your condition.

What special precautions should I follow?

Before taking isosorbide,

tell your doctor and pharmacist if you are allergic to isosorbide; nitroglycerin tablets, patches, or ointment;

or any other drugs.

tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially aspirin; beta blockers such as atenolol (Tenormin), carteolol (Cartrol), labetalol (Trandate, Normodyne),

metoprolol (Lopressor), nadolol (Corgard), propranolol (Inderal), sotalol (Betapace), and timolol (Blocadren); calcium channel blockers such as amlodipine (Norvasc), diltiazem (Cardizem), felodipine (Plendil), isradipine (DynaCirc), nifedipine (Procardia), and verapamil (Calan, Isoptin); dihydroergotamine (D.H.E. 45);

sildenafil (Viagra); tadalafil (Cialis); vardenafil (Levitra); and vitamins.

tell your doctor if you have or have ever had low red blood cell counts (anemia), glaucoma, or recent head

trauma.

tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant

while taking isosorbide, call your doctor.

if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking isosorbide.

you should know that this drug may make you drowsy or dizzy. Do not drive a car or operate machinery until you

know how it affects you.

tell your doctor if you consume large amounts of alcohol regularly and ask about the safe use of alcoholic

beverages while you are taking isosorbide. Alcohol can make the side effects from isosorbide worse.

What special dietary instructions should I follow?

Take isosorbide tablets on an empty stomach (at least 1 hour before or 2 hours after meals) with a full glass of

water.

What should I do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

What side effects can this medication cause?

Side effects from isosorbide are common. Tell your doctor if any of these symptoms are severe or do not go

away:

headache

rash

dizziness

upset stomach

headache

flushing (feeling of warmth)

If you experience any of the following symptoms, call your doctor immediately:

blurred vision

dry mouth

chest pain

fainting

What storage conditions are needed for this

medicine?

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Keep sublingual and chewable

tablets in the original container. Do not open a container of sublingual or chewable isosorbide until you need a dose. Do not use tablets that are more than 12 months old. Throw away any medication that is outdated or no

longer needed. Talk to your pharmacist about the proper disposal of your medication.

What other information should I know?

Keep all appointments with your doctor and the laboratory.

Isosorbide regular and extended-release tablets or capsules should not be used for acute angina attacks. Continue to use isosorbide sublingual or chewable tablets to relieve chest pain that has already started.

If headache continues, ask your doctor if you may take acetaminophen. Your isosorbide dose may need to be adjusted. Do not take aspirin or any other medication for headache while using isosorbide unless you doctor

tells you to.

The tablets may cause a sweet, tingling sensation when placed under your tongue. This sensation is not an accurate indicator of drug strength; the absence of a tingling sensation does not mean that the drug is not

working.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your

prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such

as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of

emergencies.

Important information about isosorbide mononitrate

Do not use isosorbide mononitrate if you are taking sildenafil (Viagra, Revatio). Serious, life-threatening side effects can occur if you take this medicine while you are using sildenafil. You should not use this medication if you are allergic to isosorbide mononitrate, isosorbide

dinitrate, (Isordil, Dilatrate, Isochron), or nitroglycerin, or if you have early signs of a heart attack (chest pain or heavy feeling, pain spreading to the arm or shoulder,

nausea, sweating, general ill feeling).

Before taking isosorbide mononitrate, tell your doctor if you have congestive heart failure, low blood pressure, or

kidney disease.

Isosorbide mononitrate can cause severe headaches, especially when you first start using it. These headaches may gradually become less severe as you continue to use

the medication. Do not stop taking isosorbide mononitrate. Ask your doctor before using any headache

pain medication.

Isosorbide mononitrate will not treat an angina attack that has already begun.

Use this medicine regularly to prevent an angina attack. Get your prescription refilled before you run out of

medicine completely.

Do not stop taking isosorbide mononitrate suddenly. Stopping suddenly could cause a severe angina attack.

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