Nicotinic acid (niacin)
Niaspan 500 mg is related to B vitamins, but at higher doses (3-5 grams a day) it has a hypolipidemic effect, lowering the equally cholesterol levels (LDL) and triglycerides (TG).
The main indication for nicotinic acid (NA) is hypertriglyceridemia. She also prescribed for moderately elevated cholesterol levels, LDL and low HDL-cholesterol.
According to the results of clinical trials Coronary Drug Project CDP), CLAS, FATS, HDL-Atherosclerosis Treatment Study (HATS) and the Stockholm Ischemic Heart Disease Study showed that treatment of NK reduces nonfatal MI (45), CVD mortality and total mortality.
Mechanisms of action of Niaspan
The main effect of NC on lipid metabolism – Inhibition of synthesis of VLDL in the liver, due to declining revenues of free fatty acids (FFA) from peripheral adipocytes to the liver, which is a substrate for the synthesis of VLDL. Inhibition of VLDL production in the liver leads to a reduction of LDL-cholesterol levels. Compared with other lipid-lowering medications, NC to the greatest degree increases HDL-cholesterol. Raising HDL-cholesterol levels is primarily due to HDL-2 fraction. This effect is due to clearance (disposal) of HDL via receptor SRBI.
Pharmacokinetics Niaspan
60-76% of the dose NC is rapidly absorbed. Peak plasma concentrations are observed within 30-60 minutes after the appointment of the usual forms of TC, and 4-5 hours for sustained-release forms of NC. Up to 90% of ingested per os drug excreted in urine as in the native form and as metabolites. There is some evidence that the effect of NC is more pronounced in women than in men because of the metabolism of this drug, depending on gender.
Hypolipidemic effectiveness of Niaspan
Nicotinic acid in daily doses of 3,0-6,0 gram leads to a lower level:
• total cholesterol and HDL-LDL by 20-25%;
• TG – 20-50%;
• Lipoprotein (a) – 30%;
• Increased HDL-cholesterol levels by 25-50%.
Forms of sustained-release NK somewhat better tolerated, but are less effective in lowering lipids. Raising HDL-cholesterol level depends on its initial concentration in the blood, this effect is maximal at a normal level of LDL-cholesterol. Reduction of Lp (a) is dose-dependent effect, reaching 36%.
Reduction of TG is shown in the first 1-4 days, and total cholesterol and LDL cholesterol, much later, after 3-5 weeks of treatment NC. Described the development of refractoriness to high doses of Nagorno Karabakh.
Adverse events observed during the reception Niaspan
When you receive an NC may develop the following side effects:
Redness of skin;
• Dry and itchy skin;
• acanthosis (acantosis nigrantis);
• Gastritis;
• Hepatitis B;
• Increase of uric acid, gout;
• Hyperglycemia;
• Hypotension and syncope (rarely);
• Supraventricular cardiac arrhythmias (rare);
• Toxic amblyopia (rare).
Reddening of the skin associated with peripheral vasodilatation of skin vessels. Dilatation of dermal blood vessels – a consequence of release of prostaglandins (prostacyclin, prostaglandin D2 and E2). The treatment often arise NC cutaneous side effects: dryness, ichthyosis and acantosis nigrans. In addition, nicotinic acid is a B-vitamins (nicotinamide – Derivative NC) and used for prophylaxis and treatment of beriberi. NC activates the fibrinolytic system. In large doses, NC reduces excretion of uric acid (may cause gout) and impairs tolerance to carbohydrates, especially in patients with diabetes.
Side effects of the liver manifest increased transaminases (3-5% of patients), and in some cases may develop liver failure. Metabolic side effects include disorders of carbohydrate metabolism (10% of patients), increased uric acid levels (5-10% of patients). Myopathy when taking NC rare, and perhaps primarily, in combination therapy with statins and fibrates. Niacin increases the secretion of histamine and gastric motility that may be associated with exacerbation of gastric ulcers, abdominal discomfort. When you receive an NC also possible temporary side effects such as dizziness, headache, fatigue, increased nervous irritability, episodes of panic, nausea, vomiting, cholestasis, toxic amblyopia, loss of central vision, and impotence. In laboratory assays are sometimes recorded increase in prothrombin time, thrombocytopenia, increased concentration of amylase.
The use of Niaspan with certain categories of patients
Nicotinic acid in clinical practice is shown in patients with I, III, IV, V types of DLP and isolated gipoalfalipoproteinemiey. NC can be successfully used in mixed HL with moderately elevated plasma total cholesterol, especially in combination with reduced concentration of LDL-cholesterol. In marked hypercholesterolemia, NC can be assigned to low doses of statins, fibrates or bile acid sequestrants. On the recommendations of the ACC and AHA NC in combination with aspirin, nitrates, beta-blockers and ACE inhibitor indicated for the treatment of patients with stable angina and concomitant increase in HDL-LDL (> 3.4 mmol / l). NC is also shown in the treatment of patients with c DLP and atherosclerosis of the lower extremities. Atsipimoks taken in doses of 750-1200 mg per day, enduratsin – 500-1500 mg per day.
Cautions and contraindications Niaspan
Appointment of Tax contraindicated in gastric ulcer, gastric hemorrhage in history. Particular caution should be exercised when administering to patients with NC rhabdomyolysis, liver disease, unstable angina, haemorrhagic diathesis in history. Relative contraindication to the NC are hypotension, gout, type 2 diabetes. According to the controlled studies have not indicated teratogenic effects of NK women in the first trimester of pregnancy. However, not recommended for NC in pregnant and lactating women. There is currently no conclusive clinical data about the good tolerability and safety receive NC in children younger than 16 years. Forms of sustained-release HK (niaspan, enduratsin) should not be administered to young people under the age of 18 years, and drug Advikor – persons under 21 years old. In elderly patients the efficacy and tolerability of NK in the form of delayed release, the same as in those of younger age.
Prior to his appointment as a Tax lipid-lowering drugs should try to use all non-drug methods to control lipids: a strict diet, weight loss, increased physical activity. In the early treatment of NC need to get a full blood chemistry, paying special attention to indicators of liver enzymes, CPK, bilirubin, uric acid levels and blood sugar. These indicators should be monitored throughout the treatment period, at least 1 time in 3-6 months. Nicotinic acid should be used with caution in persons who abuse alcohol in patients with unstable angina and acute myocardial infarction receiving nitrates, antagonists kaltsevyh channels and beta-blockers.
To minimize side effects and improve adherence to treatment is recommended:
• begin the application ships with small doses (250 mg) and gradually increase the dose to 4 grams with an interval of one week;
• use aspirin to minimize the appearance of feelings of heat and redness;
• Take NC only with food, leading to a gradual absorption of the NC and promotes leveling of adverse events;
• Do not take NC with hot drinks and alcohol;
• Do not take a hot shower (bath) shortly after receiving the Tax Code;
• begin to use short-range products.
Niacin (Niaspan prolonged release)
take 1-2 grams 2-3 times per day. To reduce the risk of hepatotoxicity, long-term treatment of niacin used in small doses.
