Nicotinic acid

Nicotinic acid, also known as niacin or vitamin B3, is one of the eight B vitamins. It plays an important role in the body's metabolic processes, helping to convert food into energy. Niacin is also involved in the functioning of the nervous system, maintaining healthy skin, and maintaining normal blood cholesterol levels.

Nicotinic acid has several key features and uses:

1. Lowering cholesterol: Niacin can effectively reduce high levels of LDL ("bad") cholesterol and triglycerides in the blood, and increase HDL ("good") cholesterol. This makes it useful in preventing atherosclerosis and related cardiovascular diseases.
2. Treatment of pellagra: Niacin deficiency can lead to pellagra, a disease characterized by diarrhea, dermatitis and dementia. Nicotinic acid is used to treat and prevent this disease.
3. Improved overall health: As an important component of the coenzymes NAD and NADP, niacin is essential for a multitude of cellular reactions, including DNA repair, energy production, and cellular metabolism.

Niacin is found in many foods including meat, fish, dairy products, eggs, nuts and green vegetables. It is also available in supplement form and can be prescribed by a doctor in higher doses to treat certain medical conditions, such as high cholesterol.

When taken in high doses, nicotinic acid can cause side effects such as skin redness, itching, dizziness, and gastrointestinal problems. Therefore, it is important to use it under the supervision of a medical professional, especially when used in supplement form to treat medical conditions.

Indications Nicotinic acid

1. Niacin Deficiency: Niacin is an important B vitamin, and its deficiency can lead to a variety of health problems including pellagra.
2. Hypercholesterolemia: Niacin is used as a medication to lower blood cholesterol levels, especially LDL (bad) cholesterol levels, which may reduce the risk of cardiovascular disease.
3. Hypertriglyceridemia: Niacin may also help lower blood triglyceride levels, which is also associated with cardiovascular disease risk.
4. Treatment of Some Forms dermatitis: In some cases, niacin may be used to treat dermatitis associated with inadequate niacin intake or other factors.
5. Cataract Prevention: Some studies suggest that niacin may be helpful in preventing cataracts and other eye diseases.
6. Other Conditions: Niacin can also be used to treat or prevent other conditions such as migraine, arthritis, and even some mental disorders, although the scientific evidence in these areas is not as extensive.

Release form

1. Oral tablets and capsules: This is the most common form of niacin, available in both over-the-counter and prescription versions. Tablets and capsules may contain niacin in an immediate-release form that enters the bloodstream quickly, or in an extended/gradual-release form that minimizes side effects and provides more stable niacin levels throughout the day.
2. Liquid forms: Liquid niacin may be preferred for people who have difficulty swallowing tablets or capsules. This form allows for more precise dosage adjustments.
3. Patches: Some products may offer niacin in patch form, providing a gradual release of niacin through the skin over the course of the day, although this form of release is less common.
4. Intravenous solutions: In medical settings, niacin may be administered intravenously for the treatment of acute conditions associated with niacin deficiency or for other specific purposes under strict medical supervision.

Pharmacodynamics

Nicotinic acid, also known as niacin, is one of the B vitamins essential for maintaining human health. It is widely used in medicine to prevent and treat atherosclerosis due to its ability to reduce low-density lipoprotein (LDL) levels and increase high-density lipoprotein (HDL) levels in plasma. A study has shown that nicotinic acid can inhibit the progression of atherosclerosis in mice through its GPR109A receptor expressed by immune cells, independent of its lipid-modifying effects (Lukasova et al., 2011).

In addition to its direct effects on lipid metabolism, nicotinic acid also exhibits a variety of pharmacological effects through activation of the receptor expressed on adipocytes and immune cells, which allows us to explore its potential application for the treatment of other inflammatory diseases such as multiple sclerosis or psoriasis (Lukasova et al., 2011).

The industrial production of nicotinic acid is mainly carried out by oxidizing 5-ethyl-2-methylpyridine with nitric acid, but this process is accompanied by the formation of nitrogen oxide, which is a greenhouse gas. There is a need to develop new technologies for the production of nicotinic acid that are greener and do not burden the environment (Lisicki et al., 2022).

CONCLUSION: Nicotinic acid is an important B vitamin with a wide range of medical applications, including the treatment and prevention of atherosclerosis, and potential for use in the treatment of inflammatory diseases. There is also a need to develop environmentally friendly methods for its production.

Pharmacokinetics

1. Absorption: Nicotinic acid may be absorbed through the gastrointestinal tract after oral medication or ingested from food. Once absorbed, it is rapidly distributed in body tissues.
2. Distribution: Nicotinic acid is well distributed throughout body tissues, including the liver, kidneys, and muscles.
3. Metabolism: In the body, nicotinic acid undergoes metabolism including hydroxylation, deamination and condensation with adenosine to nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP). About 60% of the nicotinic acid consumed is metabolized in the liver.
4. Excretion: Nicotinic acid and its metabolites are mainly excreted through the urine.
5. Mechanism of Action: Nicotinic acid is an important component of the coenzyme NAD and NADP, which plays a key role in the metabolism of carbohydrates, fats and proteins. It can also affect blood cholesterol levels and has vasodilating properties.

Dosing and administration

The method of use and dosage of nicotinic acid (niacin) depends on the specific purpose of its use, whether it is to lower cholesterol levels, treat niacin deficiency (pellagra), improve skin health, or other medical conditions. It is important to emphasize that any use of niacin should be discussed with a physician, especially if high doses are involved, as side effects may occur. The following are general dosage recommendations, which may vary depending on individual needs and health conditions:

For niacin deficiency (pellagra):

• Adults: The usual dose is 14 to 16 mg of niacin per day in the diet. In cases of niacin deficiency, doses may be significantly higher.
• Children: Recommended dose varies according to age and dietary requirements.

To lower cholesterol:

• The starting dose often begins at 500 mg per day at dinner time for immediate-release niacin, gradually increasing to the desired dose, which may be up to 1.5-2 g per day, spread over several meals to minimize side effects.
• For controlled-release products, dosage may vary and should be taken as directed by your doctor.

General Recommendations:

• Niacin should be taken with meals to reduce the risk of stomach discomfort.
• To minimize side effects such as skin redness or itching, it may be recommended to start with a low dose and gradually increase the dose.
• To avoid toxicity and to control side effects, it is important to follow your doctor's recommendations.

Use Nicotinic acid during pregnancy

Nicotinic acid (niacin, vitamin B3) is generally considered safe for use during pregnancy when taken in recommended doses, as part of multivitamin preparations, or as a stand-alone medication to treat deficiencies of this vitamin. However, as with any medication, the use of nicotinic acid during pregnancy should be discussed with your doctor.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to nicotinic acid or any other ingredients of the drug should not use it because of the possible development of allergic reactions.
2. Peptic ulcerdisease: Nicotinic acid may cause irritation of the gastric mucosa, so its use may be contraindicated in people with peptic ulcer disease or gastritis.
3. Liverdisease: Nicotinic acid may affect liver function, so its use should be cautious in patients with liver disease or while taking other medications that affect the liver.
4. Hyperuricemia: Nicotinic acid may increase uric acid levels in the blood, which may worsen gout symptoms or cause an exacerbation.
5. Diabetes mellitus: Taking nicotinic acid may affect blood glucose levels, so it should be used with caution in patients with diabetes mellitus, especially when monitoring glucose levels.
6. Pregnancy and breastfeeding: Pregnant women and nursing mothers should discuss the use of nicotinic acid with their physician, as safety data are limited.
7. Children: Nicotinic acid may be administered to children only for medical reasons and under the supervision of a physician.

Side effects Nicotinic acid

1. Skin redness (overheating): One of the most well-known side effects of niacin is reddening of the skin on the face, neck and body, known as "overheating". This occurs due to the dilation of capillaries under the influence of niacin.
2. Skin rash and itching: In some people, niacin may cause a skin rash or itching.
3. Headache and dizziness: Some people may experience headache or dizziness when taking niacin.
4. Tachycardia (fast heartbeat): Niacin may cause a fast heartbeat in some people.
5. Gastric pain and discomfort: Some patients may experience stomach pain, nausea, vomiting, or other stomach discomfort.
6. Increased blood sugar: In some people, niacin can increase blood glucose levels, which can be problematic for people with diabetes.
7. Increased uric acid levels: This can lead to gout exacerbation in people with this condition.
8. Hepatotoxicity: In rare cases, niacin can cause liver side effects, including increased liver enzymes and even hepatitis.
9. Other side effects: Include allergic reactions, blood pressure changes, vision problems, and others.

Overdose

1. Skin redness: One of the most common side effects of taking high doses of nicotinic acid is reddening of the skin, especially in the face, neck, and upper body. This is due to the dilation of the capillaries in the skin.
2. Hypotension (decreased blood pressure): An overdose of nicotinic acid may cause a drop in blood pressure, which can cause dizziness, weakness, loss of consciousness, and other symptoms associated with hypotension.
3. Dyspeptic symptoms: Gastrointestinal symptoms such as nausea, vomiting, diarrhea, abdominal pain, etc. May occur.
4. Hepatotoxicity: When taking high doses of nicotinic acid, hepatotoxicity may develop, which is manifested by increased levels of liver enzymes in the blood and other signs of liver damage.
5. Hyperglycemia: Taking large doses of nicotinic acid can cause hyperglycemia in some people, which can be dangerous for patients with or predisposed to diabetes.
6. Other unwanted effects: Other rare unwanted effects such as circulatory problems, allergic reactions and even anaphylactic shock in case of severe allergy are possible.

Interactions with other drugs

1. Cholesterol-lowering drugs: Nicotinic acid may enhance the cholesterol-lowering effect of concomitant use with statins or other lipid-lowering drugs. However, it may increase the risk of side effects such as hepatotoxicity or myopathy.
2. Blood sugar-lowering drugs: Nicotinic acid may increase the hypoglycemic effect of insulin or hypoglycemic agents used in diabetes mellitus. Patients with diabetes may need to adjust the doses of blood sugar-lowering drugs when taking nicotinic acid concomitantly.
3. Hyperuricemia drugs: Nicotinic acid may increase blood uric acid levels, which may increase the risk of gout when used concomitantly with hyperuricemia drugs such as allopurinol.
4. Hypertensive drugs: Nicotinic acid may increase the hypotensive effect of antihypertensive drugs such as calcium antagonists or ACE inhibitors. This may lead to a decrease in blood pressure and an increased risk of hypotension.
5. Drugs metabolized by cytochrome P450: Nicotinic acid may affect the activity of cytochrome P450 enzymes, which may alter the metabolism of other drugs metabolized by these enzymes. This may increase or decrease the blood concentrations of other drugs and alter their effectiveness or safety.