Spasm drugs. Antispasmodics

Comparative characteristics antispasmodic drugs used in the practice of a gastroenterologist

Antispasmodics occupy the main place in a number of drugs used for abdominal pain. They play an important role in the pathogenetic therapy of certain diseases of the digestive system. Abdominal pain is a common reason for patients to visit a doctor and the most important symptom that requires careful analysis. Misunderstood the nature of pain and incorrect treatment tactics can have undesirable consequences for the patient. In each case, when the patient complains of pain, the doctor should make a differential diagnosis of diseases of the digestive system, genitourinary system, heart and lung diseases, as well as various metabolic disorders and intoxications. The most common source of pain in the abdomen are the digestive organs. It is fundamentally important to clarify the nature and origin of this symptom. Abdominal pain can be divided into 3 categories: visceral, parietal, radiating. The impact of damaging factors on the internal organs is reflected in the appearance of visceral pain. Pain receptors of the hollow organs of the gastrointestinal tract are localized in the muscular and serous membranes. Visceral pain fibers are sensitive mainly to mechanical stimuli: tension of the peritoneum, stretching (with a fairly rapid increase in intraluminal pressure), or strong muscle contraction of the wall of a hollow organ. Pathological stretching of the walls of the digestive organs can be observed, for example, in violation of the evacuation from the stomach of a functional or organic nature, intestinal obstruction, obstruction of the biliary tract by a stone or a foreign body. Pathological spasm is possible with acute gastritis, enteritis, colitis, functional disorders of the motility of the gastrointestinal tract. Inflammatory changes and ischemia can also provoke visceral pain. This is due to the fact that some inflammatory mediators and biologically active substances help to reduce the threshold of pain sensitivity of mechanoreceptors, excited by stretch and contraction stimuli. Visceral pain is usually dull, not clearly localized. It occurs in the epi-, meso- or hypogastric region and is projected mainly near the midline, which is explained by bilateral sensory innervation. internal organs. Visceral pain is characterized by a combination with vegetative manifestations (sweating, nausea, vomiting, vasomotor reactions). Dysmotility acts as a universal pathophysiological mechanism inherent in diseases of the digestive system of various nature. As a consequence, visceral pain accompanies the bulk of diseases of the digestive system. The contractile activity of smooth muscle cells of the gastrointestinal tract is quite complex. It is influenced by various factors:

What antispasmodics for the intestines are the most effective, it will be interesting to know for everyone who often encounters painful sensations in the abdominal cavity. This phenomenon occurs quite often and can be the result of errors in diet, alcohol abuse, as well as serious diseases.

Antispasmodics for the intestines, they have an analgesic effect, relaxing the muscles. It is important to know which drugs will be the most effective in this case. Not every pain medication has a positive effect in the presence of a spasm.

However, it should be remembered that such remedies do not cure, but only relieve symptoms, so it is very important to identify the root cause and eliminate it. Antispasmodic drugs can mask dangerous ailments. If pain in the intestines occurs frequently, then you should definitely consult with a specialist.

1 Effective drugs

One of the most popular products in this line medicines is No-shpa. It has a relaxing effect on the smooth muscles of the intestines and anesthetizes. No-shpu is often taken for diarrhea, increased gas formation and other similar symptoms. The drug is available in the form of tablets, the main active ingredient of which is drotaverine hydrochloride. No-shpa is contraindicated in people with kidney and liver diseases. It should not be used in heart failure, during pregnancy and during breastfeeding.

An effective antispasmodic is Trimedat. It affects the motility of the gastrointestinal tract. At the same time, it eliminates spasms and pain, accelerating the movement of food through the stomach and intestines. The drug is safe and is used to treat children. Active substance trimebutine has a positive effect on the syndrome and the occurrence of pain in the abdominal cavity. This medicine is excellent for heaviness in the stomach and nausea.

2 Additional funds

1 more effective tool when intestinal spasms occur, Duspatalin is used. It affects smooth muscles, eliminating pain throughout the gastrointestinal tract. Such drugs are prescribed only by a doctor, as they can cause side effects in the form of allergies, nausea and vomiting. The drug is not used during pregnancy, as it can harm the fetus. Each capsule has a prolonged action. This means that there is no need to frequently repeat the drug.

Depending on the mechanism of action, these drugs are divided into 2 groups: neurotropic and myotropic. Neurotropic have an antispasmodic effect by disrupting the transmission of nerve impulses in the autonomic ganglia or nerve endings that stimulate smooth muscles. Myotropic reduce muscle tone by direct impact on biochemical intracellular processes. Myotropic antispasmodics exhibit a certain tropism for individual smooth muscle organs. In accordance with this, bronchodilators, vasodilators, gastrointestinal antispasmodics are isolated. Some myotropic antispasmodics (pinaverium bromide) have a mild M-anticholinergic activity.

The most important neurotropic antispasmodics are M-anticholinergics, or anticholinergics. But some of them, for example, platifillin, also have myotropic properties.

Neurotropic antispasmodics - M-anticholinergics(anticholinergics)

These drugs lower the tone smooth muscle internal organs, including the gastrointestinal tract, biliary tract, bronchi, reduce the secretion of HCl by the glands of the stomach, as well as salivary, mucous, sweat, increase heart rate, cause mydriasis, accommodation paralysis and increased intraocular pressure. According to their chemical structure, M-anticholinergic agents are divided into tertiary ones that penetrate the blood-brain barrier and have a central effect (atropine, scopolamine, buscopan, platifillin, hyoscine butyl bromide), and quaternary ammonium compounds that do not penetrate the blood-brain barrier (methacin).

However, only some of the 18 known anticholinergic drugs have a selective effect on the muscles of the gastrointestinal tract: atropine sulfate, hyoscine butylbromide, platifillin. They lower the tone of the stomach, duodenum, gallbladder, have an antispasmodic effect on the small and large intestines, and exhibit these actions at doses 2-10 times higher than therapeutic ones. And this is accompanied by their poor tolerance due to many side effects. At the same time, the effectiveness of atropine-like drugs in IBS is low - in other words, the danger outweighs the effectiveness, which makes their use very limited and even problematic.

Myotropic antispasmodics

These include drotaverine, no-shpa, mebeverine, papaverine, otilonium bromide, ditsetel (pinaverium bromide), spazmomen, alverine.

Myolytics lower the tone of smooth muscles by direct influence on biochemical intracellular processes. They either lead to an increase in the intracellular content of cyclic adenosine monophosphate (CAMP), a regulator of muscle tone, or to a decrease in intracellular cyclic guanosine monophosphate (CGMP). CAMP activates the release of calcium ions from the cell and their deposition, which inhibits the binding of actin to myosin and reduces the contractility of the cell. CGMP increases contractility by stimulating the release of calcium ions from the depot.
Dicetel (pinaverium bromide) selectively blocks voltage-gated L-type calcium channels in the intestinal musculature and prevents excessive calcium intake. Unlike other calcium antagonists, dicetel acts regardless of the state of calcium channels, which is why it is highly effective and not addictive. Chemical structure the drug limits its passage through cell membranes, so the absolute value of its bioavailability is
Applies and spazmomen (otilonium bromide)- myotropic antispasmodic, which has a selective effect on the smooth muscles of the gastrointestinal tract. Active substance his is otilonium bromide. The drug has a pronounced antispastic effect.
Papaverine - opium alkaloid, has myotropic antispasmodic action on the smooth muscles of the intestines, bile ducts and urinary tract, especially with spasms, unlike other opium alkaloids, does not affect the central nervous system. According to modern concepts, papaverine inhibits phosphodiesterase (PDE) in muscles, which leads to an increase in the concentration of cyclic AMP and the relaxation of smooth muscles associated with its accumulation. But papaverine is also characterized by an action similar to calcium antagonists. It has a maximum antispasmodic effect on the large intestine, then in descending order of effect - on the duodenum and antrum of the stomach.

Indications. Spasms of smooth muscles of the gastrointestinal tract, spastic dyskinesia of the colon. Well absorbed from the gastrointestinal tract. May accumulate in the liver and adipose tissue. Intensively metabolized in the liver by microsomal enzymes by conjugation with phenol. Further excretion is carried out by the kidneys by 60% in the form of metabolites, the rest is unchanged. Side effects. Nausea, anorexia, diarrhea or constipation, malaise, headache, dizziness, allergic skin reactions, rarely jaundice. When administered parenterally, it disrupts atrioventricular conduction and can cause heart block. Doses. Inside 40-60 mg 3 times a day. Maximum daily dose- 600 mg. Parenterally - subcutaneously 1-2 ml 2-4 times a day.

Drotaverine(no-shpa) (40-80 mg 3 times a day, parenterally - s / c, / m 2-4 ml 1-3 times a day). It is superior in activity to papaverine. The mechanism of action has been studied for many decades. It is associated with a change in the intracellular content of cAMP. Drotaverine blocks the specific enzyme phosphodiesterase (PDE), which destroys cAMP. After oral administration, drotaverine is well and quickly absorbed, bioavailability is 65%, and the maximum concentration in the blood is reached within an hour. The drug actively binds to plasma proteins (95-98%), penetrates well into various tissues: the central nervous system, adipose, myocardium, lungs, kidneys, liver, walls of the urinary and gall bladders, intestines, vascular wall. Elimination is slow: about 25% of the substance is eliminated per day, which is the result of the biliary route of excretion (up to 50%) and the presence of enterohepatic circulation. Drotaverine is completely metabolized in the liver with the formation of numerous metabolites. The half-life is 16 hours. In order to improve the drug, its new dosage form- forte, with a high content of drotaverine hydrochloride (80 mg).

A combination drug has also been proposed Meteospasmil- which contains alverin (myotropic antispasmodic) and simethicone (dimethicone with the addition of silica, which reduces gas formation, the surface tension of mucus). Thus, the drug is effective in IBS patients with symptoms of increased gas formation and abdominal pain. An excellent and good effect was noted in 86.7% of patients when using 1 caps. 2-3 times a day before meals.

Sodium channel blockers
Mebeverin (Duspatalin) - myotropic antispasmodic, selectively acting on intestinal smooth muscle cells. The drug has a dual mechanism of action, prevents sodium ions from entering the cell and the subsequent opening of voltage-dependent Ca + channels, which leads to the elimination of spasm and intestinal hyperperistalsis. Secondly, it limits the release of potassium from the cell and thus does not cause the development of intestinal hypotension, having a normorelaxing effect. mebeverine

(200 mg 2 times a day) is metabolized to inactive metabolites when passing through the intestinal wall and liver. Accordingly, the drug has no systemic effects, since the active principle in the blood plasma is not detected. All of its metabolites are rapidly excreted in the urine. Complete excretion of the administered dose occurs within 24 hours. Mebeverine does not accumulate in the body and dose adjustment is not required for the elderly. There is no anticholinergic effect. The drug is produced in the form of prolonged-release capsules of 200 mg, which contain microspheres coated with an acid-resistant shell. This structure allows mebeverine to be released throughout the intestine, including the colon, which is very important in the treatment of IBS symptoms. The effectiveness of mebeverine is 81-83%.

calcium antagonists - spazmomen, fenoverin, pinaverium bromide (dicetel), otilonium bromide. These drugs also refer to myotropic antispasmodics. They have an antispasmodic effect by blocking slow voltage-gated calcium channels in the smooth muscles of the gastrointestinal tract. Calcium antagonists have little effect on receptor-dependent calcium channels, therefore they mainly act in duodenum. About 40% of tonic contractions of the colon are resistant to calcium antagonists, since they are carried out by mobilizing calcium ions from internal depots, and these drugs cannot block this mechanism. Due to the fact that the most common selective calcium antagonists (verapamil, diltiazem, nifedipine) have a systemic effect and are used mainly in diseases of the cardiovascular system, calcium antagonists with a greater tropism for the effect on the gastrointestinal tract have been created - fenoverine and pinaverium bromide. These are myotropic antispasmodics that block slow calcium channels in the smooth muscle cells of the gastrointestinal tract.

Otilonium bromide (spasmodic) is most effective with increased motor activity of the colon, which is more often observed in IBS, accompanied by diarrhea. Patients tolerate the drug well with prolonged use, unlike other antispasmodics. Assign 40 mg before meals 2-3 times a day.

B. Drugs that increase gastrointestinal motility (prokinetics)

These drugs, which have a stimulating effect on the motility of the gastrointestinal tract, differ in their effect on its different sections (metoclopramide, domperidone, cisapride, trimebutine).

IN. Gastrointestinal motility regulators acting on opiate receptors.

The most widely available drug for the treatment of diarrhea is calcium carbonate. Applies also smecta- a drug of natural origin - having a protective effect on the intestinal mucosa and pronounced adsorbing properties. Smecta is characterized by a high level of fluidity of its components and, due to this, an excellent enveloping ability, which helps protect the gastrointestinal mucosa from the negative effects of hydrogen ions, bile salts, microorganisms, their toxins and other irritants. Smecta normalizes the cyclic activity of the intestine by enhancing the absorption of water and electrolytes. Monotherapy smecta leads to the cessation of diarrhea on the 3rd-5th day of treatment. Smecta also stops flatulence. The drug of choice for IBS with a predominance of diarrhea is loperamide (imodium)- opioid receptor blocker, a synthetic opioid drug that does not penetrate the blood-brain barrier and does not have a central effect. Imodium reduces the peristaltic activity of the intestine and slows down the passage of intestinal contents, increases the absorption of water and electrolytes in the intestine, and increases the tone of the anal sphincter. In studies conducted in accordance with the requirements evidence-based medicine, it is shown that the use of imodium has a positive effect in 64-100% of patients with diarrheal IBS, which significantly exceeds the placebo effect (45%). A promising form of imodium is imodium plus.

plus, which includes simethicone, which is well adsorbing gases in the intestines.

Debridat- refers to stimulants of all types of opioid receptors, is used as a motility regulator with the predominance of intestinal hypotension in the clinic.

The choice of antispasmodics

The drugs should have a high selectivity of action on spasmodic areas of the intestine, without disturbing its peristaltic activity. Of the cholinergic agents, it is recommended to give preference to myotropic antispasmodics and modulators of intestinal motility of an opiate nature. B. Drugs that enhance gastrointestinal motility (prokinetics p. 21)
V. PSYCHOTROPIC DRUGS

Studies of the mental state of patients have shown that in a significant proportion of cases there are phenomena of anxious depression (subdepression) with hypochondriacal reactions, less often a depressive syndrome with elements of melancholy on an asthenic background, sometimes apathy. Patients also complain of sleep disturbance (mainly difficulty falling asleep), a pessimistic attitude, loss of former energy and interests, fatigue, impaired attention, decreased appetite and sexual desire, weakness, anxious thoughts about oncological disease. The chronic course of IBS determines in some patients a tendency to form a hypochondriacal syndrome. Almost all patients have various autonomic disorders, including autonomic crises, mostly mixed. The close relationship between autonomic disorders, functional disorders of the gastrointestinal tract and the state of the neuropsychic sphere is well known. Sometimes an exclusive dependence of IBS on mental stress is revealed. This circumstance underlies the use of psychotropic and vegetotropic properties of psychopharmacological drugs for the treatment of functional gastrointestinal disorders.

The choice of a psychotropic drug is determined by the predominance of one or another syndrome of mental disorders.

When IBS is combined with depression, apply antidepressants, but only according to indications due to the pronounced anticholinergic effect and poor tolerance of these drugs. The therapist or gastroenterologist must agree on their appointment with a neurologist, psychotherapist or psychiatrist.

Most of the drugs in this group are tricyclic antidepressants. These include imipramine and amitriptyline. The main psychotropic effect of tricyclic antidepressants is associated with the blockade of reuptake in synapses and the deposition of neurotransmitters. They also have antiserotonin, antihistamine and anticholinergic effects, most pronounced in amitriptyline.

Imipramine is prescribed at 0.05-0.1 g per day, amitriptyline - at 0.025-0.1 g per day.

Currently widely represented non-tricyclic antidepressants related to selective serotonin reuptake inhibitors (fluoxetine, sertraline). Their value in the treatment of IBS is under study.

With a neurasthenic symptom complex with irritability, imbalance, decreased performance, sleep disturbance, antipsychotics mild action in small doses. Of these drugs, sulpiride has the greatest value in the treatment of gastrointestinal disorders. Doses: parenterally (in / m and / in) 0.1-0.3 g in 2-3 injections for 1-2 weeks, then orally 0.05 g 3 times a day.

From tranquilizers benzodiazepine derivatives (phenazepam, temazepam, diazepam, oxazepam and a number of others) are most commonly used.

The molecular substrate of the action of benzodiazepines is specific receptors located in the cortex and other parts of the brain, as well as in the spinal cord, the mediator for which is gamma-aminobutyric acid (GABA). There are 2 types of GABA receptors: A and B. The first are sensitive to benzodiazepines (they are called benzodiazepine receptors). The latter are not sensitive to them. There are 3 known types of GABA-A receptors ( 1,  2  3), the first and second are located in different parts of the central nervous system (some of them are responsible for the anti-anxiety and anticonvulsant, others for the calming effect of benzodiazepine drugs), the third are located mainly in peripheral tissues . Almost all the effects of benzodiazepines are due to their central action. The most significant of them are tranquilizing (sedative), anxiolytic, hypnotic, muscle relaxant, anticonvulsant effects. Only two pharmacological effects are the result of action on peripheral tissues: the expansion of the coronary vessels with intravenous administration of drugs and neuromuscular blockade, the cause of which is the use of very high doses. Despite some differences in chemical structure, all benzodiazepines have a similar pharmacodynamic profile. However, the severity of their effects according to the data clinical research not always the same.

To select a drug, it is necessary, first of all, to take into account the degree of its anti-anxiety effect, necessarily in comparison with the severity of side effects.

The anti-anxiety effect is enhanced in this order: phenazepam > diazepam > chlordiazepoxide temazepam oxazepam > nitrazepam > clonazepam.

Frequency and intensity unwanted effects concomitant treatment is reduced as follows: oxazepam
In addition to psychotropic tranquilizers, they also have vegetotropic properties, which should also be taken into account. The most effective in this sense are phenazepam, diazepam and lorazepam. They also find application in IBS. Each drug has a number of features that distinguish it from others. For example, phenazepam is effective in the treatment of paroxysmal vegetative disorders of the functional and mixed structure and has little effect in permanent vegetative disorders. Unlike phenazepam, diazepam relieves vegetative crises, mainly of a functional origin, and is also effective in permanent long-term vegetative disorders.

Spasmolytics are called a separate group medicines that affect the body when the most severe attacks of pain and spasms occur. Such pain may result from various diseases and pathologies in the human body, manifesting itself in the area of ​​smooth muscle, gastrointestinal tract, bile and genitourinary systems. Statistical seizures can occur in pregnant women, as well as in girls in anticipation of the onset menstrual cycle. In these and many other cases, it is antispasmodics that tend to relax the muscles, relieve acute attacks of spasms, reduce pain and stimulate cardiac activity.

Classification of antispasmodics

Since the appearance and progression of spasms throughout the patient's body and in the intestines in particular is associated with a prolonged inflammatory process, then, based on this, all antispasmodics are divided into three main groups:

1. Neurotropic agents
2. Myotropic agents
3. Neuromiotropic agents

Spasmolytic drugs of a neurotropic nature are drugs whose direct function is to activate the transmission of impulses to the nerve endings. Thanks to this process, the muscles of the organ that gives pain signals are stimulated. This group of antispasmodics includes the so-called M-cholinergic blockers - a combination of atropine sulfate, scopolamine, aprofen, metocinium and other medications.

Myotropic drugs include drugs that affect the state of smooth muscle cells, inside which biochemical and mechanical processes occur. The basis of such antispasmodics is drotaverine (popularly called No-Shpa), as well as bendazol, halidor, gimecromon and nitroglycerin. Among the most common tablets in this group are Nosh-Bra, Spazmol, Spazmoverin, Kombispasm, Niaspam and Plantex.

Neuromyotropic antispasmodics are drugs that are a combination of the first two types of drugs. They combine their best qualities, being a powerful base for pain suppression.

In addition, based on the origin of the substances, antispasmodics are divided into natural remedies (marsh calamus leaves, henbane and tansy, chamomile and lily of the valley fruits, mint, Chernobyl and oregano) and artificial drugs (drugs produced in artificially created conditions).

Form of release of drugs

All antispasmodics can be produced in the following forms:

Pharmacological group

These types of drugs belong to antispasmodics, the action of which leads to the activation of the antispasmodic effect when required level muscle contractions. The drugs eliminate the slightest suspicion of spasm attacks in the area of ​​​​smooth muscle cells, which leads to a direct blocking of impulses transmitted to the nerve endings.

Instructions for use

For newborns

The main requirement for the removal of painful spasms with the help of antispasmodics is to take them in accordance with the instructions of the health worker. Do not engage in self-diagnosis, as a rather unpleasant disease can be hidden behind regularly occurring pain. Especially when it comes to a newborn baby or a child under the age of twelve. In this case, the reception of almost all funds is strictly prohibited. There is only a small list of names that pediatricians allow children to take. These include the M-holinoblokator, which in certain cases relieves spasms and reduces pain. Newborn babies who have not reached the age of three months are prescribed antispasmodics in the form of a syrup of 1-2 milliliters every 6-10 hours. For six-month-old babies, experts recommend giving this syrup 2-3 milliliters every 5-6 hours, for children from six months to a year - 3-4 milliliters every 5-6 hours, and from a year to three years - 5 milliliters every 4-6 hours . In addition, doctors strongly recommend the use of natural antispasmodics in the form of herbal preparations, infusions, potions and decoctions.

For pregnant women

If we talk about pregnant women, then for them taking antispasmodics is limited to those cases where there is a real absence of a threat to the fetus. Most often, pregnant women take mild antispasmodic drugs, but, of course, they should not be abused. The same applies to mothers during their lactation.

With menstruation

During the period of a painful menstrual cycle, any girl can also resort to the help of antispasmodics. In this case, the most effective are drugs made on the basis of drotaverine and herbal substances. On such days, patients need to spend more time in bed, since it is a passive lifestyle that can help alleviate disease-causing attacks and improve blood circulation.

For the elderly

Elderly people should use antispasmodics with special care and caution. After consulting with a specialist in advance, it is also necessary to take into account the reception of other medications, which can both positively and negatively affect the effectiveness of painkillers.

For pain in the intestines and colitis

To resolve the inflammatory processes that have arisen in the intestines, experts recommend taking Mebeverine or Plantacid. With colitis, gastritis, as well as other diseases of the gastric tract, Papaverine or Drotaverine can help patients. Antispasmodics of this group have the most effective result, reducing the level of acidity and lowering secretion.

Contraindications for use

• all stages of development of tuberculosis;
• intestinal diseases caused by the ingestion of pathogenic viruses and microbes into the patient's body;
• some types of acute colitis;
• a critical increase in the size of the colon;
• Crohn's disease;
• the presence of individual contraindications to taking medications.

Before directly taking any of the types of antispasmodics, it is necessary to consult a therapist. You should not engage in conscious self-medication, as this can cause an overdose or rejection of the medicine by the body. At the appointment with a specialist, focus on the available allergic reactions and general intolerance to certain substances. Store drugs in dry and cool enough places, and carefully read the instructions on the package. Please note that in case of an overdose of antispasmodics, the patient develops nausea, swelling of the face, rash, slight urticaria, increased flatulence and diarrhea.

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