Nicotinic acid in ampoules is widely used in medicine for the treatment of cardiac diseases, pathologies of the musculoskeletal system; the drug also has a beneficial effect on the condition of the skin and hair. The advantage of the injection form of drug administration is the simplicity and accuracy of the dosage, the speed of onset of the effect, and the absence of unwanted reactions from the gastrointestinal tract. Doctors advise injecting nicotinic acid according to a regimen that is developed taking into account the patient’s general well-being and the presence of concomitant pathologies.
In this article you will learn about the pharmacokinetics and pharmacodynamics of niacin when administered parenterally, indications and contraindications for prescribing the drug, dosage rules and injection techniques. The following provides information about possible side effects of the drug, signs of overdose, compatibility with vitamins and other medications.
Pharmacodynamics and pharmacokinetics
Vitamin PP (nicotinic acid) is a vitamin that takes part in a large number of oxidative reactions occurring in living cells.
The drug has a specific anti-pellagric effect and is used to improve the activity of blood vessels .
The administration of nicotinic acid preparations makes it possible to normalize the permeability of vascular walls and, accordingly, reduce tissue swelling, improve the state of tissue (in particular, nitrogen and carbohydrate) metabolism and microcirculation, expand the lumen of blood vessels (a vasodilating effect is noted at the level of small blood vessels, including the vessels of the brain brain), increase the fibrinolytic activity of blood plasma and reduce platelet aggregation by suppressing the synthesis of TxAj (thromboxane A2), a mediator of their aggregation and degranulation.
In the body, vitamin PP is biotransformed into nicotinamide , which binds to the hydrogen-transferring coenzymes NAD and NADP. Regulates oxidation-reduction reactions, takes part in synthetic processes, metabolism of amino acids , fats , purines , proteins , as well as in glycogenesis and tissue respiration .
Reduces the rate of VLDL synthesis and inhibits lipolysis (fat degradation) in adipose tissue. Helps normalize blood lipid composition: reduces the concentration of LDL, triglycerides and total cholesterol , while increasing the content of HDL in the blood. Shows antiatherogenic and detoxification properties .
Ensures the conversion of the trans-form of retinol into cis-retinal, which is used in the synthesis of the visual pigment rhodopsin, stimulates the release of histamine and promotes the activation of kininogenesis.
Vitamin B3 is well absorbed in the pylorus of the stomach and the upper parts of the duodenum . With the participation of pyridoxine and riboflavin, it can be produced by the bacterial flora of the intestine from tryptophan , which comes with food. tryptophan required to form a milligram of the substance is 60 mg.
Metabolization occurs in the liver. Nicotinic acid and its metabolic products are excreted by the kidneys; when taken in high doses, the substance is excreted primarily in pure form.
Pharmacological properties
Vitamin B3 is part of the coenzymes NAD and NADP, which are responsible for the transfer of hydrogen and ensure the normal course of redox reactions in the body. Coenzymes are also used for tissue respiration processes, regulation of lipolysis in adipose tissue and carbohydrate metabolism. The drug helps reduce plasma cholesterol levels and normalizes the rheological properties of blood. Niacin has a powerful vasodilating effect.
Injectable medications are made in the form of vitamin solutions with a concentration of the main substance of 1%, which corresponds to 10 mg/ml.
Nicotinic acid can be administered subcutaneously, into the venous bed or intramuscularly. After injection, the substance is evenly distributed in the bloodstream and undergoes metabolic reactions in the liver parenchyma. It is excreted from the body mainly through the kidneys in unchanged form.
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Indications for use
Indications for the use of Nicotinic acid are:
- hypo- and avitaminosis caused by insufficient intake of vitamin B3 from food, exclusively parenteral nutrition, malabsorption syndrome (including against the background of pancreatic ), Hartnup disease, rapid weight loss, gastrectomy , diseases of the digestive system ( persistent diarrhea , including tropical , celiac enteropathy , Crohn's disease );
- conditions accompanied by an increased need for vitamin PP (diseases of the hepatobiliary system, prolonged fever, hyperthyroidism , prolonged stress, chronic infections, pregnancy, lactation, cancer);
- hyperlipidemia (including triglyceridemia and hypercholesterolemia );
- atherosclerosis;
- obliterating diseases of the vessels of the lower extremities (for example, Raynaud's disease );
- ischemic cerebral circulatory disorders;
- spasm of the urinary and biliary tract, vessels of the extremities;
- microangiopathy;
- diabetic polyneuropathy;
- hypoacid gastritis;
- colitis and enterocolitis ;
- facial nerve neuropathy;
- trophic ulcers and non-healing wounds.
Contraindications
Categorical contraindications for both dosage forms of the drug are serious liver dysfunction, bleeding, cerebral hemorrhage, hypersensitivity to nicotinic acid.
Nicotinic acid tablets should also not be taken during periods of exacerbation of peptic ulcer disease and in children under 2 years of age (as an anti-sclerotic agent ).
Additional contraindications to the administration of Nicotinic acid in ampoules are: atherosclerosis , hyperuricemia , severe arterial hypertension , gout , childhood.
Side effects
The drug stimulates the release of histamine , which in some cases may be accompanied by:
- redness of the skin (mainly the upper half of the body and face) with a burning and tingling sensation;
- hypotension;
- orthostatic hypotension (with rapid injection into a vein);
- increased secretion of gastric juice;
- dyspepsia;
- dizziness;
- feeling of a rush of blood to the head;
- hives;
- itching.
Side effects associated with long-term use of high doses of vitamin B3 are expressed as:
- anorexia;
- impaired liver function and obesity;
- vomiting;
- diarrhea;
- irritation of the mucous membrane of the digestive canal;
- ulceration (ulceration) of the gastric mucosa;
- transient increase in the activity of alkaline phosphatase, aspartate aminotransferase, lactate dehydrogenase;
- paresthesia;
- arrhythmias;
- decreased glucose tolerance;
- hyperglycemia.
Instructions for use of Nicotinic acid
Nicotinic acid injections: instructions for use
The route of administration and dose depend on the indications. For ischemic stroke and pellagra, the solution is recommended to be injected slowly into a vein. For pellagra, it is also possible to give injections intramuscularly or subcutaneously.
Antipellagric therapy involves a single or double dose of 50 mg intravenously or 100 mg intramuscularly. The duration of treatment is 10-15 days.
For ischemic stroke, the drug is administered in a dose varying from 10 to 50 mg.
Injections can be given in three ways:
- 1 ml of a one percent solution into the muscle;
- intradermally (to replenish the need for vitamin);
- into a vein, 1-5 ml of a one percent solution, previously diluted in 5 ml of physiological solution.
IM and subcutaneous injections of the drug are quite painful and may be accompanied by a burning sensation. Intravenous injection may cause skin redness and a feeling of heat.
Such a reaction of the body is normal. On the contrary, the absence of redness may indicate the presence of certain problems with blood circulation.
Instructions for tablets
The tablets are taken after meals.
The prophylactic dose for adults varies from 12.5 to 25 mg per day, for children - from 5 to 25 mg per day.
For pellagra, adult patients are prescribed to take 100 mg of nicotinic acid 2 to 4 times a day. Course duration is 2-3 weeks. Children are given the drug 12.5-50 mg two or three times a day.
For vascular lesions of atherosclerotic origin, patients are recommended to take 2 to 3 grams of vitamin PP .
The starting dose for dyslipidemia is 50 mg per day in one dose. Subsequently, if the therapy does not provoke adverse reactions, the frequency of applications is increased to 2-3 times a day. The duration of the course is from one month. Intervals should be maintained between repeated courses.
In all other cases, the daily dose for adults is from 20 to 50, for children - from 12.5 to 25 mg. In some cases, the doctor may increase the daily dose to 100 mg for an adult patient. Depending on the indications, tablets are taken 2 or 3 times a day.
Injection schedule (intramuscular)
Most often, nicotinic acid injections are given intramuscularly, since this method of administering the drug entails the least number of possible adverse reactions.
IMPORTANT! The standard location for the injection is the upper outer quarter of the buttock (there are the fewest anatomical structures such as nerve trunks or large arteries).
Scheme of drug administration:
- Before giving the injection, be sure to thoroughly clean the skin with a cotton swab soaked in a 70% alcohol solution.
- Take the syringe with the substance in your right hand.
- Insert the syringe needle into the skin at a right angle so that approximately 5–7 mm of the needle remains above the surface of the skin after insertion.
- Press the plunger slowly with your left hand, introducing the substance gradually.
- Once the syringe is empty, pull the needle out of the muscle in one short but sharp movement.
- Immediately apply a cotton swab soaked in alcohol to the injection site.
Interaction
N. acid enhances the effect of vasoactive drugs (in particular, ganglion blockers), which may be accompanied by attacks of orthostatic hypotension .
Bile acid sequestrants (for example, colestipol or cholestyramine ) reduce the bioavailability of acidic drugs, including n. acid, so the drug should be taken at least one hour before or no earlier than four hours after taking these medications.
When conducting an analysis to determine the level of glucose in urine, the drug may provoke a false-positive reaction with Benedict's reagent (copper sulfate solution).
N. acid has hyperglycemic potential and can significantly reduce the activity of acarbose, which can cause the development of decompensation of diabetes mellitus .
Due to the ability of N. acids cause hyperglycemia , patients who are prescribed the drug in combination with “ metformin + saxagliptin ” or “metformin + sitagliptin ” should constantly monitor their glycemic control parameters.
In patients taking nadroparin calcium, it is necessary to keep hemocoagulation parameters under control.
With simultaneous use of n. acids and combinations “ amlodipine + atorvastatin ”, n. acid and simvastatin , n. acid and lovastatin may increase the risk of developing myopathy . Combination n. acid with simvastatin can also provoke rhabdomyolysis .
Myopathy and rhabdomyolysis are also possible when using the combination “n. acid in lipid-lowering doses and Simvastatin + Ezetimibe .”
The risk of developing myopathy also increases when lipid-lowering (exceeding 1 gram per day) doses of n. acids in combination with Rosuvastatin . In this regard, treatment with Rosuvastatin should be started at 5 mg/day.
The combination “Nicotinic + Ascorbic acid ” should be used with caution.
The possibility of drug interaction with sodium heparin .
High doses n. acids reduce the effectiveness of the combination “ Glibenclamide + Metformin ”, the hypoglycemic effect of Gliclazide and the effectiveness of the combination “ Gliclazide + Metformin ”, as well as the hypoglycemic effect of Glimepiride .
When used simultaneously with n. acid reduces the effect:
- Glipizide;
- hypoglycemic effect of Gliquidone ;
- Insulin Lispro (including biphasic);
- Metformin;
- Repaglinide;
- hypnotic effect of Phenobarbital .
It is forbidden to mix n in one syringe. acid and Thiamine .
Despite the fact that the simultaneous use of n. acids with HMG-CoA reductase inhibitors can provoke myopathy , with simultaneous administration of the drug with Fluvastatin , the bioavailability of the latter, as well as the bioavailability of n. acid does not change. However, this combination should be used with caution.
Drug compatibility
Nicotinic acid can be injected together with lidocaine, novocaine and other anesthetics that reduce local pain after injection. The combination of the drug with methionine, which protects liver cells from fatty degeneration, works well. You cannot mix niacin with vitamins B1, B6 and B12 in the same syringe, since mutual destruction of these nutrients occurs.
There is evidence of drug interactions between vitamin B3 and other medications:
- Antibiotics increase the feeling of heat and skin flushing after nicotinamide injections.
- It is not advisable to combine lipid-lowering drugs from other groups with nicotine, as this can lead to adverse reactions.
- Injections of nicotinic acid drugs reduce the benefit of hypoglycemic drugs, which requires a revision of their dosages.
- The simultaneous use of vitamin PP with beta blockers and other antihypertensive drugs can cause a sharp uncontrolled decrease in blood pressure.
special instructions
What is vitamin PP?
Wikipedia answers the question “what is nicotinic acid” that it is a white powdery substance, odorless and slightly sour in taste. The powder dissolves poorly in cold water, ethanol, ether and slightly better in hot water.
The gross formula of the substance is C₆H₅NO₂. It was first obtained in 1867 by the oxidation of nicotine with H2CrO4 (chromic acid).
The benefits and harms of vitamin B3
Pure vitamin B3 can strengthen the immune system so much that the human body acquires natural protection against Staphylococcus aureus and a number of other, no less serious, viruses.
Scientists are confident that very high doses can even stop HIV infection and bacterial infections, against which most existing drugs are powerless.
In addition, vitamin B3 has detoxifying .
The body of an adult man requires from 16 to 28 mg of vitamin B3 , the body of a woman - from 14 to 20 mg.
The need for the vitamin will increase during intense nervous and mental activity, increased physical activity, in people working in a hot shop, in a hot climate and in the Far North, during pregnancy and during breastfeeding, in people whose diets include vegetable proteins over animals (including people fasting and people on a low-protein diet).
Nicotinic acid is necessary for the release of energy from fats and carbohydrates, as well as for the normal course of protein metabolism. It normalizes the functioning of the pancreas and stomach, and is also part of the enzymes that ensure cellular respiration.
The vitamin has a beneficial effect on the heart, blood vessels, nervous system, maintains healthy mucous membranes of the oral cavity and intestines, and skin; takes part in ensuring normal vision, reduces high blood pressure and improves blood circulation.
Some scientists are inclined to believe that vitamin B3 prevents the cancerous degeneration of cells.
A lack of this substance in the body is accompanied by apathy, lethargy, fatigue, headaches, dizziness, dry and pale skin, insomnia, irritability, decreased appetite and body weight, constipation, palpitations, and decreased resistance to infections.
If a person does not receive enough nicotinic acid, he develops the disease pellagra . The first signs of the disease are:
- frequent, watery stools (3 or more times a day, without blood or mucus);
- poor appetite, heaviness in the stomach;
- belching and heartburn;
- redness of the oral mucosa;
- salivation , burning in the mouth;
- swelling and cracking of lips;
- protrusion of the papillae of the tongue with red dots;
- the appearance of deep cracks in the tongue and red spots on the face, hands, elbows and neck;
- swelling of the skin (which may hurt, itch, or form blisters);
- noise in ears;
- severe weakness;
- headache;
- crawling sensation and numbness;
- pressure fluctuations;
- unsteady gait.
Excess vitamin in turn can cause skin rashes, itching and fainting.
Products containing vitamin B3
To prevent hypovitaminosis PP , it is preferable to adjust the diet so that vitamin B3- containing foods are present in the diet.
Where is niacin found? In foods, the greatest amount of vitamin B3 can be found in liver, egg yolk, yeast, nuts, fish, milk, chicken, green vegetables, meat, legumes, ground nuts, buckwheat and any other food containing the α-amino acid tryptophan .
Heat treatment does not affect the amount of vitamin.
Why is Nicotinic acid needed in cosmetology?
Despite the fact that the instructions do not contain recommendations regarding the use of Nicotinic acid for hair growth or facial skin, this product is quite often used in beauty salons.
The rejuvenating effect of the drug is based on the ability of nicotinic acid to dilate blood vessels in the peripheral part of the circulatory system, increase the supply of oxygen to tissues, enhance the outflow and removal of aggressive waste and free radicals from skin cells.
As a result, the skin smoothes out, becomes more hydrated and acquires a beautiful and even color.
Nicotinic acid is also used for hair growth. One course usually requires at least 30 ampoules of solution.
After opening the ampoule, the solution is transferred with a syringe into a small container, after which it is distributed with your fingers (or a syringe without a needle) over the entire scalp: first at the temples and along the hairline, then along the partings. Typically, 1 ml of solution is sufficient for one procedure (this corresponds to the contents of 1 ampoule).
It is very important that your hair is clean, since a build-up of dust and grease will prevent the product from being absorbed into the scalp. Before using the drug, you should not use shampoos with silicones to wash your hair, as they will create a barrier for the drug to penetrate into the tissue.
Nicotinic acid is destroyed quite quickly in air, so the procedure should be performed as quickly as possible. An open ampoule cannot be stored.
Normal reactions to the drug are a slight burning sensation, a crawling sensation, redness and burning of the skin.
The appearance of hives, rashes, itching, and headaches indicate intolerance to nicotinic acid. If these symptoms occur, you should wash your hair and stop using the product further.
If, after using Nicotinic acid for hair, the scalp becomes dry or appears, it is recommended to dilute the solution with water in a 1:1 ratio. Such reactions are a consequence of skin sensitivity. Aloe juice can also be used as an alternative to water .
Once the solution is completely applied, the procedure is considered complete. Repeat it daily for a month. There is no need to wash off the drug.
After completing the course, almost all girls note hair growth of 3 cm.
An injection solution of Nicotinic acid has also found use as a remedy for cellulite. Before the procedure, the contents of one ampoule are diluted in 3 ml of water. Then a wide bandage is moistened in the resulting solution and tightly - but not tightly! - wrap it around problem areas.
This method is most effective in getting rid of cellulite on the thighs and abdomen, since these are the areas of the body that are most convenient to bandage. But to eliminate cellulite on the buttocks, it is recommended to use other means.
The bandages are wrapped in cling film and a towel (for insulation). Instead of a towel, you can use a blanket or blanket.
The duration of the first procedure should not exceed 15 minutes. If the skin responds well to the drug and there are no side effects, the time may be increased in the future.
Precautionary measures
It should be borne in mind that nicotinic acid injections are painful.
During treatment, it is necessary to constantly monitor liver function, especially if the patient is prescribed high doses of vitamin B3 .
To prevent hepatotoxicity, it is recommended to introduce a sufficient amount of methionine- foods into the patient’s diet (milk, dairy products, buckwheat, legumes, fish) or prescribe him to take lipotropic drugs (including methionine ).
Nicotinic acid, given its ability to irritate the mucous membrane, is used with caution for peptic ulcer disease (in remission) and hyperacid gastritis . If it is necessary to prescribe the drug in these cases, taking large doses is contraindicated.
To reduce the irritating effect on the mucous membrane of the digestive tract, it is recommended to take the tablets with milk.
Due to the likelihood of hepatotoxicity, taking high doses of vitamin B3 is also contraindicated for liver diseases (including hepatitis and cirrhosis ) and diabetes mellitus .
The use of the drug for the correction of dyslipidemia in diabetes mellitus is inappropriate.
Nicotinic acid for weight loss
Nicotinic acid stimulates metabolic processes, and it is this property that makes it advisable to use the drug for weight loss.
The effect does not develop due to burning excess fat, but due to balancing the concentration of cholesterol in the blood and detoxifying the body.
To achieve more pronounced results, taking the tablets should be combined with reasonable physical activity, a balanced diet and drinking enough water. To speed up your metabolism as much as possible, it is best to take the tablets immediately after meals.
It should be remembered that people with high acidity of gastric juice are recommended to take the drug with warmed milk or mineral water.
Signs of overdose
When niacin is administered intravenously, as well as intramuscularly (at large dosages), the patient may experience some symptoms of an excess of the compound in the body. Most often, an overdose manifests itself as follows:
- redness of the skin appears on the face and torso;
- nausea occurs;
- vomit;
- heartburn;
- diarrhea;
- severe skin itching;
- dizziness;
- fainting;
- darkening of the eyes;
- lack of air;
- paresthesia appears;
- cholestatic jaundice.
IMPORTANT! If any of the listed symptoms appear, you should immediately stop using the drug and consult your doctor for symptomatic treatment.
Nicotinic acid has long been actively used in medical practice. This substance helps eliminate pain and inflammation in diseases of the musculoskeletal system, improve metabolic processes and blood circulation, and activate regenerative processes in the skin. However, niacin should be used carefully, following the developed injection schedule. This will help avoid the appearance of adverse symptoms or signs of overdose.
Reviews about Nicotinic acid
Reviews of Nicotinic acid tablets, as well as reviews of Nicotinic acid injections, are in most cases positive.
The drug has extensive indications for use and is effective for osteochondrosis of various parts of the spinal column, circulatory disorders in the brain and lower extremities, pellagra , decreased visual acuity, dyslipidemia , migraines , obesity, alcohol, occupational or drug intoxication, atherosclerosis and a number of other conditions.
Negative reviews are mainly due to the fact that after taking the tablets or administering the injection solution, the patient experienced a feeling of heat and severe redness of the skin. However, the instructions indicate that such phenomena are a normal physiological reaction of the body.
Reviews of Nicotinic acid for hair are also quite optimistic. The product helps strengthen the roots, improves blood circulation in the scalp, perfectly moisturizes the hair, eliminates dandruff, accelerates hair growth and prevents hair loss.
Cosmetologists recommend Nicotinic acid to improve complexion and skin condition, as well as to strengthen nails. In addition, Nicotinic acid is one of the most affordable and effective remedies for cellulite.
The metabolic effect of the drug allows it to be used to accelerate the breakdown of fats in programs aimed at reducing excess weight.
Despite the huge number of beneficial properties, nicotinic acid is a rather serious drug, the thoughtless use of which can lead to negative consequences for the body.
The advisability of prescribing a drug in one form or another can only be determined by a doctor.
Analogs
Vitamin B3 has a special mechanism of action, so it is quite difficult to replace this drug in the treatment of vitamin deficiency. There are other drugs on the pharmacological market based on nicotinic acid solution, which contain lower concentrations of the substance and therefore have fewer side effects. The most famous of them:
- Apelagrin;
- Niacin;
- Nicoden;
- Liplit.
If the drug was prescribed as part of complex therapy for various diseases, then it can be replaced with drugs with similar pharmacological effects. For osteochondrosis, Actovegin and Trental can be prescribed to improve microcirculation. Various vasodilators are beneficial for the treatment of peripheral circulatory disorders.
Injections of nicotinic acid are recommended for patients to relieve the symptoms of pellagra, treat atherosclerosis and other vascular diseases, reduce subjective symptoms during exacerbation of osteochondrosis, and accelerate hair growth. When administered by injection, the drug has a rapid effect on the body; the standard course of administration lasts about 2 weeks. When using the medicine, side effects may occur, to reduce which it is recommended to dilute the solution for intravenous administration or mix nicotinamide with lidocaine for an intramuscular injection. It is necessary to strictly follow your doctor's recommendations about where and how often to administer nicotinic acid so as not to cause overdose symptoms.
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