Nicospan

Pharmacodynamics and pharmacokinetics

Taking Nikospan helps improve microcirculation and collateral circulation. The effect of this drug is determined by the substances included in its composition. Once in the body, nicotinic acid is converted into nicotinamide adenine dinucleotide or dinucleotide phosphate. They are necessary for electron transfer and tissue respiration. High dosages of the drug have a beneficial effect on the composition of fats in the blood , as well as in the treatment of hyperlipidemia in combination with other lipid-regulating drugs. Drotaverine hydrochloride has an antispasmodic effect on smooth muscles, causing them to relax.

Inside the body, the drug undergoes rapid absorption from the gastrointestinal tract and widespread distribution in tissues. Penetration of active substances into breast milk has been noted. As a result of metabolism, several metabolites : N-methylnicotinamide, nicotine-uric acid, derivatives of 2-pyridone and 4-pyridone. The drug binds tightly to blood proteins. Its maximum concentration is detected in serum after 45-60 minutes. Nikoshpan is excreted in urine and feces, in metabolites and a small part unchanged.

Description and instructions for the drug Nikoshpan

Nikoshpan is another remedy that dilates blood vessels.
Its action is based on a combination of two active components: drotaverine and vitamin PP (nicotinic acid). The first substance is widely used both as an independent drug and as the basis of such a well-known medicine as No-shpa. It reduces the intensity of calcium entry into smooth muscle cells, which provide the tone of internal organs, including blood vessels, intestines, bile ducts, and so on. As a result, this muscle relaxes and the tension in the vascular walls, intestinal walls and other organs subsides. Blood pressure decreases and spasms go away. The second component – ​​nicotinic acid – protects and restores vascular health, normalizes the concentration of fats in the blood, and reduces its clotting. Thus, blood flow in the system of the smallest vessels improves, tissue nutrition is optimized. Nikoshpan is used for:

• Various vascular diseases. For example, endarteritis, vasospasm, and so on;
• Headache caused by vascular damage;
• Brain circulatory disorders;
• Other circulatory disorders associated with vascular diseases.

Nikoshpan is produced in tablet form. This remedy can be used for a long time, until the alarming symptoms completely disappear. The instructions for the drug recommend taking it three times a day.

Nikoshpan is contraindicated for:

Noticeable dysfunction of the liver, kidneys, heart.

Indications for use

Indications for prescribing Nikospan are:

• angiospastic manifestations accompanied by atherosclerotic and hypertensive encephalopathy;
• cerebral vasospasm;
• atherosclerosis of the coronary arteries;
• obliterating endarteritis;
• vasospasms caused by menopause or migraine.

Directions for use and dosage

Nikoshpan tablets are taken 1 tablet 3 times a day. For vasospasm and migraine, the tablets are taken on an empty stomach, in other cases - after meals.

Nikoshpan for injection is administered intramuscularly or subcutaneously, 1-2 ml 1-2 times a day. If necessary, intra-arterial or intravenous administration of the drug may be prescribed. The solution is injected slowly into the vein. For thromboangiitis obliterans, Nikoshpan is injected into the femoral artery.

For menopausal symptoms and angiospastic conditions, the drug is used for a long period until the symptoms are completely eliminated.

Side effects

When treated with Nikospan, side effects may develop in the form of: facial flushing, feelings of heat, dizziness, headache, skin rash, itching, nausea, dyspepsia, and so on.

In rare cases, the following are noted: arterial hypotension, dizziness, irregular heartbeat, sleep problems, constipation, fainting, and more.

Contraindications to taking Nicospan

There are often disputes in the medical community about whether the sale of this drug without a prescription is permissible. The fact is that there are a number of serious contraindications to its use. “Nikospan” cannot be used in the treatment of those patients who have problems with the kidneys, heart, liver, if the level of cholesterol in the blood is elevated, or if there is a predisposition to thrombosis, which the patient may not be aware of.

In addition, “Nikoshpan” is contraindicated; there is a tendency to arterial hypertension, that is, for those who often have high blood pressure. It can be tracked only with constant monitoring of readings. That is, before you start a course of taking Nicoshpan, you need to make sure that your blood pressure is normal.

This drug is also contraindicated for those who are intolerant to lactose or other components included in the Nikoshpan tablets. Allergy sufferers must carefully read the instructions for the drug, especially the section that describes the composition of the tablets. If the list contains a substance that can cause an attack, you should refuse therapy with this antispasmodic.

Interaction

Combination with oral hypoglycemic agents and contraceptives reduces their effect. The simultaneous use of nicotinic acid and statins increases the risk of myopathy, acute necrosis of the skeletal muscles. The combined use of drotaverine hydrochloride and Levodopa reduces its antiparkinsonian effect.

Instructions for use of Nikoshpan

For effective and safe treatment, it is necessary to carefully study the instructions for use of the drug, dosing principles and possible side effects.

Indications and contraindications for use

The medicine is prescribed for:

• cerebral vasospasm;
• encephalopathy of a hypertensive and atherosclerotic nature;
• obliterating endarteritis;
• migraines;
• vasospasms that appear during menopause.

Obliterating endarteritis
The drug is not used for:

• heart failure;
• kidney and liver diseases;
• hypersensitivity to drotaverine hydrochloride or niacin;
• arterial hypertension.

In addition, this medicine is not recommended for use by women who are breastfeeding or those who are at any stage of pregnancy. It should be remembered that before using Nikospan it is recommended to consult a doctor.

Dosage and method of administration

The instructions for using this product indicate that it can be taken both after meals and on an empty stomach:

• for migraines and vascular spasms - before meals;
• in all other cases - after.

Migraine attack
As a rule, one to three tablets of the drug per day are prescribed. The maximum daily dose of this medicine is 150 mg. Nikoshpan can be used one-time or in courses. The second option is acceptable for cerebral vascular spasms, as well as during menopause.

When using the drug, you need to take into account its compatibility with other drugs:

1. When Levodopa is used together with drotaverine hydrochloride in patients, the antiparkinsonian effect will be reduced.
2. Acute skeletal muscle necrosis and an increased risk of myopathy may occur when statins are used concomitantly with niacin.
3. Nikoshpan can significantly reduce the effect of contraceptives and oral hypoglycemic drugs.

Possible side effects

Some groups of patients may experience side effects such as:

• dizziness;
• rapid heartbeat;
• increased acidity;
• facial redness;
• nausea, sometimes turning into vomiting;
• itching;
• skin rashes;
• sensations of heat.

In some cases, tachycardia, constipation, insomnia, loss of consciousness and fainting may occur. Those patients who suffer from lactose intolerance may experience complaints of intestinal and stomach disorders after taking Nikospan.

Reviews about Nikoshpan

In most cases, reviews of Nikoshpan are found on women's forums for pregnant women. Users are actively discussing this drug and its effectiveness. However, it does not help everyone and not always.

As a rule, women expecting a baby experience various changes in the body, which are often accompanied by discomfort and unpleasant symptoms. Many are worried about headaches, numbness of the limbs and general weakness , but during such a period you need to strictly monitor the intake of medications, as they may be contraindicated.

Nikoshpan is one of the few drugs that can be taken during pregnancy , subject to maximum compliance with the dosage and treatment regimen. It helps reduce the manifestation of unwanted symptoms associated with changes in the functioning of the cardiovascular system, for example: headaches, pressure problems, swelling, and so on. At the beginning of pregnancy, the drug helps improve the tone of the uterus and eliminate the threat of miscarriage .

According to experts, this drug helps well with mild disorders and in combination therapy. However, it is not recommended to take it on your own; you need to consult a doctor who can prescribe adequate treatment.

Composition, properties and release form of the drug Nikoshpan

The basis of Nikoshpan tablets is drotaverine hydrochloride, a common and relatively safe broad-spectrum antispasmodic. The second active substance is nicotinic acid (vitamin PP). Without it, the human body is unable to function properly. Most people use them as auxiliary components when forming tablets.

• talc and magnesium stearate,
• povidone and lactose,
• starch.

Drotaverine, entering the human body, has a direct effect on smooth muscles and the walls of blood vessels, relaxes them, thereby eliminating pain. Nicotinic acid accelerates microcirculation of all fluids in the body, including blood, normalizes the balance of their components, against which the general condition of a person improves and tone increases.

“Nikoshpan” goes on sale in plastic jars placed in a cardboard box. One transparent plastic bottle usually contains 50 tablets.

General information about the drug

Nikoshpan is included in the medicinal group of vasodilating agents. It improves peripheral and cerebral circulation. The main effects after using this product are increased cellular respiration, relief of spasm, pain and improvement of lipid metabolism in the body. The international nonproprietary name of Nikoshpan has not been established; it is included in the Comb drug group (combined drugs).

Release forms, composition and prices for the drug in Russia

The medicine is available in the form of tablets in a package of 50 pieces. Each of them contains 78 g of drotaverine hydrochloride and 22 mg of niacin. The following auxiliary components are used: lactose, magnesium stearate starch, talc and polyvidone. The average cost of Nikoshpan in Russia is presented in the table below (Table 1).

Table 1 – Cost of Nikoshpan

The price of such a medicine in pharmacies will depend on the region of sale. The highest cost for Nikoshpan is in the Far East, St. Petersburg and Moscow.

Pharmacodynamics

Nicotinic acid (water-soluble vitamin PP) is involved in tissue respiration and electron transfer in the respiratory chain. This substance is used for hyperlipidemia in combination with other drugs that regulate lipid metabolism. In high dosages, it allows you to control the amount of fats in the blood and promotes their elimination.

Niacin has its effect due to the formation of coenzymes in the body (the result of the processing of NAD+ and NADP), which take part in the transport of electrons in the respiratory chain and in tissue respiration.

Mechanism of action

Another component of this product is drotaverine hydrochloride, an isoquinoline derivative. The substance has an antispasmodic effect on vascular smooth muscle. The effectiveness of such a substance is determined by the suppression of PDE 4 (without suppression of PDE 3 and 5) and an increase in the level of cAMP, which, through the suppression of the enzyme myosin light chain kinase (MLCK), leads to relaxation of smooth muscles.

The influence of drotaverine extends to the smooth muscles of the genitourinary system, gastrointestinal tract, as well as biliary and vascular muscles. The vasodilating effect allows you to increase blood supply to tissues, which has a beneficial effect on the functioning of organs.

Pharmacokinetics

Vitamin PP is quickly distributed in the tissues of the body after it is absorbed from the gastrointestinal tract. It is excreted from the body mainly with feces and partly with urine. You should be aware that it can pass into breast milk, so Nikoshpan is contraindicated in pregnant women. This component is capable of being metabolized into uric acid and its derivatives.

Drotaverine hydrochloride is rapidly absorbed after both oral and parenteral administration. It binds to alpha lipoproteins, gamma globulins and albumin. In addition, it is able to bind to plasma proteins. The maximum concentration of this component in the blood serum is achieved 65 or 75 minutes after the tablet enters the patient’s body.

Characteristics of drotaverine

Drotaverine is metabolized in the liver. Already two days after use, it is almost completely eliminated from the human body in the form of metabolites with feces (partially - 30%) and urine (50%) unchanged. Currently, manufacturers do not have information about the interaction of drotaverine with niacin.