[general name] nitroglycerin solution
[English name] nitroglycerinsolution
【 ingredients 】 the main ingredient of this product is nitroglycerin
[properties] this product is a colorless and clear liquid with the characteristics of ethanol
[role category]
[pharmacology and toxicology] the main pharmacological action is to relax vascular smooth muscle. Nitroglycerin releases nitrogen oxide (no), which is the same as endothelial relaxing factor, activates guanylate cyclase, increases cyclic guanylate (CGMP) in smooth muscle and other tissues, leads to dephosphorylation of myosin light chain, regulates the contraction state of smooth muscle and causes vasodilation. Nitroglycerin dilated arteriovenous vascular bed, mainly dilated vein, and its effect intensity was dose-dependent. Peripheral venous dilatation * causes blood to stay in the periphery, decreases the amount of blood in the heart, and decreases the left ventricular end diastolic pressure (preload). Dilation of the artery reduces peripheral resistance (afterload). Arteriovenous dilation reduces myocardial oxygen consumption and alleviates angina pectoris. It also dilates epicardial coronary artery branches. The therapeutic dose can reduce systolic blood pressure, diastolic blood pressure and mean arterial pressure, and the effective coronary perfusion pressure can often be maintained. However, when the diastolic filling time is shortened due to excessive reduction of blood pressure or rapid heart rate, the effective coronary perfusion pressure decreases. The increased central venous pressure and pulmonary capillary wedge pressure, pulmonary vascular resistance and systemic vascular resistance were reduced. Heart rate usually increases slightly, which is estimated to be a reflex effect of blood pressure decline. Cardiac index can increase, decrease or remain unchanged. Patients with increased left ventricular filling pressure and peripheral resistance and low cardiac index may have increased cardiac index. On the contrary, in patients with normal left ventricular filling pressure and cardiac index, intravenous medication can slightly reduce the cardiac index. There is no long-term animal test to evaluate its carcinogenicity.
[pharmacokinetics] sublingual administration takes effect in about 1 ~ 3 minutes and reaches the maximum effect in 5 minutes. The peak blood concentration is 2 ~ 3ng / ml, the effect lasts for 10 ~ 30 minutes and the half decline is about 1 ~ 4 minutes. It is mainly metabolized in the liver, which is rapid and almost complete. The intermediate products are dinitrate and mononitrate, and the end product is glycerol. Compared with the parent drug, the two main active metabolites 1,2 - and 1,3-dinitrogen have weaker effect and longer half-life. After metabolism, it is excreted through the kidney.
【 indications 】 it can be used for the treatment and prevention of coronary heart disease and angina pectoris, as well as for reducing blood pressure or treating congestive heart failure.
[usage and dosage] solution: 1% solution is administered sublingually, 0.05 ~ 0.1ml once, 2ml a day.
[adverse reaction] ⑴ headache: it can occur immediately after medication, which can be severe pain and persistent. ⑵ dizziness, weakness, palpitation and other postural hypotension may occur occasionally, especially in patients with upright and braking. (3) the treatment dose can produce obvious hypotension reaction, including nausea, vomiting, weakness, sweating, pallor and collapse. (4) syncope, blush, drug rash and exfoliative dermatitis were reported.
[contraindication] it is forbidden to be used in patients with early myocardial infarction (severe hypotension and tachycardia), severe anemia, glaucoma, increased intracranial pressure and known allergy to nitroglycerin. It is also forbidden to use sildenafil citrate (Viagra), which enhances the antihypertensive effect of nitroglycerin.
[precautions] ⑴ the minimum dose that can effectively alleviate acute angina pectoris should be used. Excess may lead to tolerance. ⑵ severe hypotension may occur in small doses, especially in the upright position. When taking medicine under the tongue, the patient should take a seat as far as possible to avoid falling due to dizziness ⑶ it should be used with caution for patients with insufficient blood volume or systolic depression. (4) abnormal bradycardia and aggravation of angina pectoris can be combined when inducing hypotension. (5) it can worsen angina pectoris caused by hypertrophic obstructive cardiomyopathy. (6) tolerance to vascular action and anti angina pectoris can occur. (7) in case of blurred vision or dry mouth, stop the medicine. Excessive dose can cause severe headache.
[medication for pregnant and lactating women] it is unknown whether it will cause fetal damage or affect fertility, so it can only be used for pregnant women when it is necessary. It is also unknown whether it is excreted from human milk, so lactating women should be cautious when taking intravenous drugs.
[medication for children]
[medication for elderly patients] is not clear. (to be supplemented)
[drug interaction] ⑴ moderate or excessive drinking can cause hypotension. ⑵ combined with antihypertensive drugs or vasodilators can enhance the effect of nitrate on postural hypotension. ⑶ aspirin can reduce the clearance of sublingual nitroglycerin and enhance its hemodynamic effect. (4) the use of long-acting nitrate can reduce the therapeutic effect of sublingual medication. (5) sildenafil citrate (Viagra) enhances the antihypertensive effect of organic nitrates. (6) when combined with acetylcholine, histamine and sympathetic amines, the curative effect may be weakened.
[drug overdose] overdose can cause severe hypotension, tachycardia, bradycardia, conduction block, palpitation, circulatory failure, death, syncope, persistent pulsatile headache, vertigo, visual impairment, increased intracranial pressure, paralysis and coma with convulsions, blushing and sweating, bad heart and vomiting, abdominal colic and diarrhea, dyspnea and methemoglobinemia.
[Specification]
[storage]
[prescription or not] {prescription}