Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Imdur
Active ingredient: Isosorbide
Available dosage forms: 20, 40, 30, 60 mg
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Isosorbide general information
Isosorbide belongs to a category of drugs referred to as nitrates. This isn’t a comprehensive listing of side consequences. This drug might cause you to get dizzy. Some meds can cause you to feel hungrier.
Data on using isosorbide mononitrate during pregnancy are insufficient in order to appraise the possible harmful effect. Additionally It is excreted unchanged within the urine. Dosage regime ought to be designed based on the clinical response of the individual. The dosage is dependent on your healthcare condition and response to treatment. This medication really should not be used in case you have certain health conditions. The lowest effective dose ought to be used.
Some side effects might occur that usually don’t need medical attention. Some conditions might become worse whenever the drug is suddenly stopped. Other medications might be needed.
The additional weight in formula-fed infants is supposed to be because of excess water retention and also a different composition of body fat. It is normally due to narrowing of your own coronary arteries because of a build-up of the fatty substance called atheroma. Hypotension induced by nitrates may come with paradoxical bradycardia and raised angina. Limit alcoholic beverages and prevent overheating which may aggravate dizziness. Additionally It is not designed to be taken just before physical activities (for example, exercise, sexual activity) to reduce chest pain.
It generally does not undergo a first-pass effect. Don’t crush or chew the tablets, which can destroy the very long action of the drug and can increase negative effects. Doing this can release almost all of the drug at the same time and may raise your risk of side consequences. This particular product may contain inactive ingredients, which may cause allergies or alternative difficulties.
It is important to choose the drug in the very same times every day. Some medicines aren’t suitable for those with certain circumstances, and at times a medicine may just be used if extra care is taken. Animal data usually do not suggest an impact of healing isosorbide mononitrate on male and female fertility. Talk about the risks and advantages with your personal doctor.
Your doctors may would like you to wait until you’ve completely recovered from treatment or any additional health issues you could have. Additionally, your health care professional might be able to let you know about approaches to check or lower a few of these side outcomes. Keep away from the reach of children. Don’t forget to use it at exactly the same time every day.
There are plenty of good reasons to keep a nutritious weight. It is very important to discuss proper weight gain, food regime, and exercise in the initial visit and periodically through the entire pregnancy. Eating healthy meals allow you to obtain the weight you have to present crucial nourishment for your own child. There aren’t any data which can be found on the interaction with food.
Angina happens when the heart muscle isn’t getting enough blood. It relaxes blood vessels within your physique (causing them all to widen) and this lessens the strain on your own heart, making it simpler for your heart to pump blood all around your body. This can result in life-threatening vascular complications.
Tell your physician in case you are breast-feeding a baby. Ask your doctor before breast-feeding. Call your physician for medical advice regarding side effects. Don’t alter the dosing times unless instructed by your doctor. You may well be able enough to switch to some other medication, including one which can even allow you to shed pounds. Although unlikely, when this medication is utilized for a very long time, perhaps it doesn’t work as well and could require different dosing.
Active – active substance / start: isosorbide dinitrate
Aerosonit; Dinisorb; Dinitrosorbilong; Ditrat; Of Poppy (Of Mack retard, spray); Izokard; Izoket (Izoket spray, ointment); Izolong; Isosorbitol (isosorbitol retard); Isosorbide dinitrate; ISDN; Kardiket (Kardiket retard); Kardiks; Kardikep; Kardiogard; Cardona; Nisoperkuten; Nitrosorbid; Nitrosorbid – NS .; Nitrosorbid – rusfar; Nitrosorbid – UWI; Sorbidin; TD – Spray Of Mack; Etidiniz.
isosorbide dinitrate – a highly effective anti-anginal agent from the group of nitrates for treatment of coronary heart disease. Aerosol for oral administration designed for the relief of acute episodes and retard forms with long-acting, long-term treatment and prevention of angina pectoris and myocardial infarction.
Active – active substance:
isosorbide dinitrate / Isosorbide dinitrate.
The tablets (retard tablets).
Capsules retard prolonged action.
metered spray for sublingual use.
The solution for infusion.
An ointment for external use.
Properties / Action:
isosorbide dinitrate – peripheral vasodilator with a primary effect on venous vessels. Antianginal drug. Promotes redistribution of coronary blood flow in the area with a reduced blood supply.
isosorbide dinitrate mechanism of action involves the formation of nitric oxide (NO), which causes the activation of guanylate cyclase increases the level of cGMP and that ultimately leads to smooth muscle relaxation and a decrease in peripheral vascular tone.
Dilation of postcapillary vascular bed leads to venous blood depositary that, in turn, decreases venous return to the heart. As a result, the filling pressure is reduced and left ventricular wall stress is reduced (reduced preload), thereby decreasing the need for myocardial oxygen and energy. Decreased cardiac filling pressure and reduced wall stress contribute to the strengthening of capillary blood flow, and opening previously sealed intramural coronary vessels, as well as improving the supply of oxygen ischemic subendocardial area.
Direct dilatation of the coronary vessels and eccentric coronary stenoses, as well as a slight decrease in their resistance to cause an improvement in myocardial perfusion and supply it with oxygen without the development of “steal syndrome”.
Thus, the effect of isosorbide dinitrate is mainly due to a decrease in myocardial oxygen demand by reducing preload and afterload, as well as direct action koronarorasshiryayuschee.
isosorbide dinitrate improves exercise tolerance in patients with coronary heart disease, angina.
In heart failure, isosorbide dinitrate promotes the unloading of the myocardium.
The decrease in blood flow to the right atrium helps reduce the pressure in the pulmonary circulation, which in turn leads to the regression of pulmonary edema symptoms.
Retard forms of isosorbide dinitrate:
The onset of action of the drug observed after 30 – 50 minutes, the maximum effect of approximately 1.5 – 2 hours, the duration of action of the drug 4 – 6 hours.
Aerosol isosorbide dinitrate sublingual application:
Each time the dispenser equal amount of solution is sprayed in the form of tiny droplets. It easily penetrates through the buccal mucosa and into the bloodstream in seconds. When used in the form of sublingual isosorbide dinitrate spray relieves angina for 2 – 3 minutes, the effect lasts for about 1 hour.
Absorption after administration of isosorbide dinitrate into high. After absorption from the gastro – intestinal tract is exposed to the drug effect “first pass” through the liver where it is metabolized to 2 – active metabolites (isosorbide – 5 – mononitrate and isosorbide – 2 – mononitrate). The maximum concentration is achieved after 1 hour serum after oral administration and is maintained, in the case of prolonged forms of the drug for several hours. Bioavailability is about 22%. The half-life of isosorbide – 5 – mononitrate is 4.5 – 6 hours, and isosorbide – 2 – mononitrate – 1.5 – 3 h. Isosorbide – 5 – mononitrate displayed in an inactive form in the form of isosorbide mononitrate, and glucuronate izosorbitola. Excreted in the urine.
isosorbide dinitrate aerosol delivery provides more active substances into the bloodstream than other oral dosage forms. Absorption isosorbide dinitrate through the oral mucosa occurs to a greater extent than in sublingual tablet formulation. The area of absorption much more – all the oral mucosa. Fewer active material forms a thin layer over the entire surface due to absorption hydrophilicity aerosol. The effect of “first pass through the liver” is not carried out; absorption by the mucous membrane of the drug takes place before it can be swallowed. Aerosol provides a more rapid absorption of isosorbide dinitrate as compared to the tablet form, respectively and – achieving a more rapid clinical effect. Aerosol has a long duration of action compared to nitroglycerin th.
For intake: long-term treatment of coronary heart disease, prevention of angina attacks, rehabilitation treatment after myocardial infarction. Chronic heart failure (in combination therapy), some forms of pulmonary hypertension, pulmonary heart (in a combination therapy with cardiac glycosides and / or diuretics).
For use aerosol: relief and prevention of angina attacks; as a means of first aid for acute myocardial infarction and acute left ventricular failure in the prehospital phase. Prevention or treatment of coronary artery spasm during cardiac catheterization. Increased tolerance to ischemia during balloon catheterization.
For intravenously the introduction: acute myocardial infarction, including complicated by acute left ventricular failure; unstable angina; pulmonary edema.
To apply the ointment: the prevention of angina attacks.
drugs isosorbide dinitrate is sometimes prescribed for endarteriite and other diseases accompanied by spasms of peripheral vessels.
Dosage and administration:
In the oral administration of isosorbide dinitrate dosage depends mainly on the stage of the disease and individual needs in nitrates. Multiplicity of reception is determined by the dosage form of the drug.
Tablets for oral use:
Take before meals. Treatment should be started with the lowest dose, gradually increasing the dose to the required. For relief of angina is necessary to chew and hold in the mouth (sublingual) 1 tab. 5 or 10 mg or 1.2 pi. 20 mg. For the prevention of strokes administered in an initial dose of 10 mg of 4 – 5 times a day. In inefficiency with 3 – 5 – day treatment dose can be increased up to 60 – 120 mg per day. In the combined therapy of chronic heart failure, pulmonary hypertension when administered at 10 – 20 mg 3 – 4 times a day. To prevent strokes or heart failure treatment tablets should be swallowed whole. The duration of treatment is determined individually in each case.
Retard forms for oral administration (tablets, capsules):
retard tablets or capsules should be taken after meals, with liquid squeezed small amount of liquid. It is necessary to select a dose according to the individual needs of the patient in consultation with a doctor.
When you assign more than one pill per day. In view of the rapidly developing tolerance, the drug should be used in two daily doses, approximately every 14 hours, a second tablet can be taken at least 8 hours after the first to ensure the full effect of the drug.
In the long-term treatment and the absence of other regulations recommend the following dosage:
Spray for oral use:
The first time you need to spray the drug in the air. If the spray has not been used more than one day, the manipulation is repeated so that subsequent dose has been clinically complete.
unit dosage treatment of angina attack comprises injecting into the mouth of one to three doses used with 30 – second intervals. The simultaneous use of 3 doses may be carried out on special indications.
Prior to physical or emotional stress, which can trigger an attack, you need to inject an aerosol into the mouth 1 – 3 times at intervals of 30 seconds between injections.
Acute myocardial infarction / acute heart failure. Begin with 1 – 3 injections with a 30 – second intervals. If no effect after 5 minutes still need an extra dose of the drug. If during the next 10 minutes no improvement, under the control of blood pressure spray applied again.
For the prevention of coronary artery spasm during catheterization. During the diagnostic or therapeutic measures koronarospazm can be prevented if the catheter before use 1 – 2 doses of aerosol.
If necessary, the injection can be repeated under the control of hemodynamic parameters.
The ointment and spray for external use:
The initial dose is 1 g of ointment (2 unit doses). In the evening before going to bed; if necessary, in the morning. Apply the ointment on the chest, the inner surface of the forearm or abdomen; wait a few minutes; then you can get dressed. The minimum surface area of application of the ointment should be 20 x 20 cm. In case of insufficient clinical response the drug can also be used in the morning.
cutaneous spray applied to the skin from a distance of 20 cm to spray 1 – 2 doses of the drug.
The solution for infusion:
When i / v infusion of the drug solution with a concentration of 100 ug / ml or 200 ug / ml is administered with an initial rate of 3 – 4 drops per minute or 1 – 2 drops per minute, respectively. If necessary, the introduction of the speed can be increased every 5 minutes to 2 – 3 drops provided continuous monitoring of blood pressure, heart rate, ECG and urine output. Maximal administration rate – 33 drops per minute (at a concentration of 100 ug / ml) and 17 drops per minute (at 200 ug / ml concentration). The duration of administration can be from a few hours to several days, depending on the hemodynamic and clinical situation.
Use during pregnancy and lactation
Although experimental studies in animals did not reveal any damaging effects of isosorbide dinitrate on the fetus during pregnancy and breast-isosorbide dinitrate ipolzovat be extremely cautious. During pregnancy and lactation use of the drug is possible only when the intended benefits to the mother outweighs the potential risk to the fetus or child. The drug should not be taken in the first three months of pregnancy without a doctor’s recommendation.
In the early treatment of isosorbide dinitrate may appear headache ( “nitrate headache”), but experience shows that usually after a few days, with incessant taking the drug, she passes.
may include the lowering blood pressure (including orthostatic hypotension with cerebral ischemia and collapse) and an increase in heart rate (reflex tachycardia), especially in the first days of treatment. Very rarely observed kollaptoidnye state, accompanied by bradycardia, and syncope.
In rare cases, the increase in symptoms of angina (paradoxical reaction) may be observed with a strong drop in blood pressure.
Other possible side effects may be nausea, vomiting, erythema (skin redness), sensation of heat.
In some cases, especially at the beginning of treatment, there may be a reduced capacity for rapid mental and motor reactions, somnolence, dizziness, and weakness.
If during treatment the patient takes alcohol can worsen the side effects and reduced therapeutic effect of the drug.
When using oral spray may cause burning sensations easy language.
Special instructions and precautions:
Retard forms of isosorbide dinitrate are not suitable for the treatment of acute attacks of angina. If during treatment occurs angina, it should be fast to stop taking nitrates (An opportunity use oral spray of isosorbide dinitrate).
Do not use retard form slow release in people with malabsorption syndrome.
During therapy with necessary blood pressure control and heart rate, especially during the period of gradually increasing doses.
particularly careful medical supervision is necessary when:
To apply caution in patients who have recently had a hemorrhagic stroke.
To apply caution in the elderly, given the more likely the development of their orthostatic reactions: slow recommended a gradual transition from a horizontal position, or sitting in a vertical position. In some cases, hypotension may be a symptom of an overdose of nitrates.
drug with caution is indicated for: hypertrophic obstructive cardiomyopathy, constrictive pericarditis, aortic and / or mitral stenosis, cerebrovascular disorders.
People with “night” angina nitrates should be used before going to bed. The duration of treatment takes a doctor. Cancelling nitrates should be carefully and gradually to avoid aggravation of coronary artery disease.
During the period of treatment should be deleted alcohol.
If during treatment with ointment angina occurs, it should be to stop taking nitrates fast. After using the ointment, wash your hands; in contact with the mucous membranes of the eyes, nose or mouth causes a feeling of cold.
With a constant continuous treatment with high doses of isosorbide dinitrate may develop tolerance to other nitropreparatov, in connection with what is recommended after 3 – 6 weeks of regular administration of the drug to make a break for 3 – 5 days, replacing the time isosorbide dinitrate other antianginal means.
Dispensed by prescription.