What helps with abdominal pain: list of antispasmodics and other drugs

Throughout life, a person repeatedly experiences abdominal pain. Under the age of 50, most often the cause of pain is not organic, but functional in nature, when drug therapy is most likely to be effective. The cause may be intestinal colic (in children in the first months of life), irritable bowel syndrome, biliary dyskinesia, dysfunction of the sphincter of Oddi, etc. About a third of cases of functional pain are accompanied by spasm of the smooth muscles of the gastrointestinal tract. This is why antispasmodics are so widely used without a doctor’s prescription. Providing a pronounced analgesic effect and normalizing the functioning of the organ, they, unlike non-narcotic and opioid analgesics, do not interfere with the mechanisms of pain, that is, they do not “erase” the picture of the disease, which is critically important in diagnosis.

Nota bene!

When a client asks for a remedy for abdominal pain, it is necessary to exclude urgent situations in order to send the sufferer to a doctor in time. These include:

Severe pain that prevents you from sleeping or doing anything, lasts longer than 1-2 hours.
Severe abdominal pain is accompanied by vomiting.
Severe pain is accompanied by elevated body temperature - 38.5°C and above.
Severe pain is accompanied by loss of consciousness.
Severe abdominal pain in a pregnant woman.
The abdominal muscles are tense and the stomach is as hard as a board.
Diarrhea mixed with bright red blood.
The stool is dark and tarry.
Vomiting blood.
Abdominal pain is accompanied by vomiting, diarrhea and severe dehydration.

Mechanism of action of painkillers

When tissue damage or inflammation occurs, a signal travels along the nerve endings to the brain. In the damaged area, irritation of the nerve endings occurs. As a result of muscle contraction, a spasm occurs.

Painkillers act as follows:

inhibit nerve impulses that transmit pain;
soothe irritated nerve endings;
relieve muscle spasms.

Depending on the type of pain, painkillers are used.

Cellular mechanism of pain

Smooth muscle cells are mainly found in the large intestine. There are significantly fewer of them in the small intestine. The mechanism of cell contraction depends on the concentration of calcium ions in the cytoplasm. The sources of calcium are the extracellular space, connected to the cytoplasm through calcium (slow) membrane channels, as well as the intracellular depot. The release of calcium causes the muscle cell to contract. The contraction of muscle cells forms a spasm and the person feels pain.

The process of muscle contraction is most often triggered by the mediator acetylcholine, binding to muscarinic cholinergic receptors (M-cholinergic receptors). Thus, blockade of M-cholinergic receptors leads to a decrease in tone and relaxation of smooth muscles (and therefore helps relieve abdominal pain). This, in particular, is the basis for the mechanism of action of a group of drugs called M-anticholinergics.

The interaction of calcium with calmodulin leads to the interaction of actin with myosin and cell contraction. CAMP (cyclic adenosine monophosphate) and cGMP (cyclic guanosine monophosphate) weaken the interaction of calcium with calmodulin and also impede the entry of calcium ions into the cell. The level of cAMP and cGMP is controlled by phosphodiesterase (PDE), which destroys excess of these nucleotides. Thus, if you reduce the activity of PDE, the concentration of calcium ions in the cytoplasm will decrease and the tone of the muscle cell will decrease.

Based on the described mechanisms for regulating the calcium concentration inside the muscle cell, which are disrupted under pathological conditions and lead to spasm, the main groups of antispasmodics have been created:

M-anticholinergics (atropine, hyoscine butyl bromide).
PDE IV inhibitors (drotaverine).
Blockers of calcium release from intracellular stores or sodium channel blockers (mebeverine).
Calcium channel blockers.

M-anticholinergics

M-anticholinergics are one of the oldest groups of drugs.
Atropine has been used in medicinal herbs since the 4th century BC. e. Thus, the ancient Greek naturalist Theophrastus described mandrake as a remedy for treating wounds, gout and insomnia, and also as a “love potion.” The ancient Greek military physician Dioscorides (1st century AD) described mandrake wine as an anesthetic to treat pain or insomnia, to be given before surgery or cauterization. M-anticholinergics most effectively affect the upper gastrointestinal tract. The use of non-selective M-anticholinergics (atropine, platyphylline, metacin) is limited by their prescription, as well as by the fact that they have a systemic effect and have a number of side effects, such as intestinal atony and obstruction.

One of the relatively oldest selective M-anticholinergics is hyoscine butyl bromide (first registered in Germany in 1951). It acts on the M1 and M3 subtypes of receptors, localized mainly in the walls of the upper gastrointestinal tract, gallbladder and biliary ducts. Hyoscine butyl bromide does not penetrate the blood-brain barrier and has a weak systemic effect, unlike atropine. However, it is contraindicated in people with glaucoma, benign prostatic hyperplasia, as well as organic stenosis of the gastrointestinal tract and tachyarrhythmias. Hyoscine butyl bromide accumulates in the smooth muscles of the gastrointestinal tract and is excreted unchanged by the kidneys. The drug is successfully used for sphincter of Oddi dysfunction, biliary dyskinesia and pyloric spasm.

The severity of the effect of hyoscine butylbromide also depends on the patient’s individual sensitivity to this drug. Unfortunately, the antispasmodic effect of hyoscine butyl bromide on the small intestine (except the duodenum) and large intestine can be realized when taking a dose 2–10 times higher than the therapeutic dose, so its use is useless for spasms in the lower abdomen. A large number of restrictions and risks when taking this drug require medical supervision, which is why the M-anticholinergics known to us are currently used less and less abroad. However, hyoscine butyl bromide is still available without a prescription.

Phosphodiesterase inhibitors (PDE) type IV

These are traditionally widely used antispasmodics: drotaverine hydrochloride and papaverine. Their injectable forms are sold with a prescription, while their tablet forms are available without a prescription. PDE IV is widely present in smooth muscle along the entire length of the intestine, as well as in the biliary and urinary tracts. Thus, blocking PDE IV has a universal antispasmodic effect regardless of the severity of the spasm or its cause. In addition, drotaverine has anti-edematous and anti-inflammatory effects. Drotaverine can be used for acute abdominal pain - both to relieve acute spasms and for long-term treatment of biliary dyskinesia, cholelithiasis, chronic intestinal diseases with spastic syndrome, which are accompanied by colicky or bursting pain. Unlike M-anticholinergics, drotaverine can be used in elderly men with prostate pathology, as well as with concomitant pathology and combined use with other drugs. The therapeutic concentration of drotaverine in plasma when taken orally is achieved after 45 minutes.

Prevention of abdominal pain in children

Preventive measures aimed at reducing the severity of pain in children include:

Normalization of nutrition. Restoring the diet, as well as selecting the optimal diet, helps prevent the development of abdominal pain, which can be functional in nature. To do this, you need to adhere to a regular diet with maximum limitation of snacks, as well as the consumption of salty, smoked, spicy and fried foods. Preference should be given to fermented milk products, fruits, vegetables, meat and poultry, as well as various cereals. It is important to avoid long breaks between meals.
Creating a favorable psycho-emotional environment at home. Parents need to provide a psychologically comfortable environment for the child’s life, protecting him from quarrels, scandals, showdowns, as well as other adverse factors.
Regulation of sleep and rest patterns. To prevent the development of pain, prevent a decrease in immunity, it is necessary to restore full sleep, eliminate excessive stress, and also normalize the work and rest regime.
Compliance with personal hygiene rules. A prerequisite for reducing the incidence of abdominal pain is hand washing. This procedure is mandatory before eating, after coming from outside, visiting the toilet, and after contact with animals.
Timely treatment of diseases occurring in acute or chronic form. This will prevent a decrease in immunity.

Sodium channel blockers

These drugs block intracellular calcium stores through a cascade of reactions. The most famous drug is a derivative of veratric acid - mebeverine. Unlike anticholinergics, it does not cause hypotension of the colon. Most often, this drug is prescribed for functional disorders of the gastrointestinal tract or as an adjuvant for organic diseases of the gastrointestinal tract. Mebeverine is used only for course treatment. Mebeverine is most effective in combination with other pathogenetic drugs. Mebeverine is mainly available by prescription, but there is a dosage form in tablets that does not require a doctor's prescription.

We will not dwell on calcium channel blockers in more detail, since these drugs do not have any over-the-counter forms.

The over-the-counter myotropic antispasmodic trimebutine stands apart. Trimebutine acts on the enkephalinergic system of the intestine and peripheral opiate receptors - µ, κ and δ. Having an affinity for receptors that enhance and suppress peristalsis, it stimulates the contraction of intestinal smooth muscles in hypokinetic conditions and is an antispasmodic in hyperkinetic conditions. Trimebutine reduces the tone of the esophageal sphincter, promotes gastric emptying and increased intestinal motility, as well as the response of the smooth muscles of the colon to food irritants. It is used for various functional disorders of the gastrointestinal tract.

Functional pain—how to help your child?

The development of functional pain is common in children aged 7 to 15 years. This condition is accompanied by a pronounced deterioration in well-being, but even with a thorough diagnosis and a complete examination of the patient, the cause cannot be determined. Their appearance is not associated with the presence of pathology of a surgical or infectious nature.

Suspected causes that may cause functional pain include:

Overwork.
Exposure to severe stress or nervous tension.
Functional dyspepsia or impaired stomach function, accompanied by painful digestion.
Irritable bowel syndrome, which is associated with disruption of the digestive tract without organic pathology.
Abdominal migraine. The appearance of pain is accompanied by a sharp deterioration in health with the development of nausea, vomiting and pallor of the skin.

Ask and choose

How can a pharmacy client choose an over-the-counter antispasmodic from the extensive list of drugs for abdominal pain? Guiding questions will help:

Does a person have a chronic organic gastrointestinal disease - peptic ulcer of the stomach or duodenum, chronic cholecystitis, chronic pancreatitis, biliary colic, biliary dyskinesia? As a rule, the patient already knows what helps him or what drug the doctor recommended for him during an exacerbation.
Patient's age? Selective M-anticholinergics are not suitable for the elderly due to the risk of developing intestinal obstruction. Also, antispasmodics have age restrictions for children: mebeverine can be used from twelve years of age, hyoscine butylbromide and drotaverine - from six, trimebutine - from three.
For women - pregnancy, lactation? The use of antispasmodics during pregnancy is possible only as prescribed by a doctor. PDE inhibitors and trimebutine are contraindicated during lactation. Anticholinergics and sodium channel blockers can be used during lactation.
Pain in the upper abdomen, possibly accompanied by nausea or vomiting? A selective M-anticholinergic drug is suitable for adults, in the absence of contraindications described in the instructions for a particular drug.
Pain in the lower abdomen? Type IV PDE inhibitors and sodium channel blockers are suitable.

Sources

Abdominal pain syndrome in the practice of general practitioner T. M. Benz “News of medicine and pharmacy.” Gastroenterology (239), 2008.
Pchelintsev M. V. “Anspasmodics: from clinical pharmacology to pharmacotherapy.” Attending Physician 7 (2008): 74–77.
Mikhailov I. B. Clinical pharmacology (textbook for students of medical universities) - 5th ed., revised. and additional - St. Petersburg: publishing house "Sotis-Med", 2013. - 588 p.
Yakovenko E. P., et al. "Opiate receptor agonist trimebutine in the treatment of functional disorders of the gallbladder and sphincter of Oddi." Journal "Attending Physician" 2–2014 (2017): 56.
Tytgat GN. Hyoscine butylbromide: a review of its use in the treatment of abdominal cramping and pain. Drugs 2007; 67:1343–57.