Experience in using the antispasmodic Buscopan in gynecological practice

Pharmacodynamics and pharmacokinetics

The drug has an antispasmodic effect aimed at the smooth muscles of the gastrointestinal tract, gall bladder, and genitourinary organs. In addition, the secretion of food glands is reduced . In this case, the anticholinergic effect on the nervous system is not manifested.

Thanks to the presence of an additional substance - paracetamol , Buscopan Plus, in addition to its antispasmodic effect, eliminates the cause of pain, providing a muscle-relaxing effect exactly at the site of pain.

The active component, hyoscine butyl bromide, is characterized by insignificant absorption in the gastrointestinal tract. Once inside the body, it is absorbed by 8%, with an average absolute bioavailability of up to 1%. A single use of hyoscine butyl bromide at a dosage of 20-400 mg leads to maximum plasma concentrations after 2 hours.

The active component is predominantly distributed in the muscle cells of the abdominal cavity and pelvis. The interaction of the drug with the movement of choline in the epithelial cells of the human placenta was also noted. The bulk of metabolism is due to hydrolysis of the ester bond. The drug is excreted through urine and feces.

Introduction

Abdominal pain (AP) is one of the most common reasons for seeking medical help (after headaches, back pain and dizziness) and can be associated with both self-limiting disorders and severe, life-threatening conditions requiring immediate medical intervention.
Establishing a correct diagnosis can be difficult due to the presence of multiple organ systems in the abdominal cavity and the fact that AB can cause many diseases. In this regard, AB is treated worldwide by general practitioners/family doctors, surgeons, internists, emergency physicians, pediatricians, gastroenterologists, urologists and gynecologists. AB usually falls into one of the following categories:

1. The process leading to inflammation of the parietal peritoneum and/or associated with inflammation of the parenchymal organs is usually associated with the occurrence of constant, aching pain, intensifying with changes in the tension of the peritoneum due to pressure/squeezing, stretching or changing position. It is often accompanied by defence, a contraction of the abdominal muscles to reduce tension in the peritoneum.

2. Pain associated with obstruction of a hollow organ, often cramping or colicky in nature, which corresponds to the peristaltic movements of the organ aimed at eliminating the obstruction.

3. Pain associated with vascular disorders in the abdominal cavity (thrombosis or embolism) is caused by hypoxia/ischemia of tissue distal to the site of occlusion; may occur suddenly or gradually, be strong or mild.

4. Functional gastrointestinal disorders such as functional dyspepsia and irritable bowel syndrome IBS [1]. 5. AB may be associated with damage to organs not located in the abdominal cavity (for example, lower lobe pneumonia).

In terms of frequency of occurrence, the leading place in the occurrence of AB is inflammation of hollow and parenchymal organs, accompanied by irritation of the peritoneum. Examples include such common diseases as gastritis, gastroesophageal reflux disease (GERD), peptic ulcers, appendicitis, cholecystitis, hepatitis, intestinal obstruction, urethritis colic, cystitis, pyelonephritis and primary dysmenorrhea.

Indications for use of Buscopan

• spasm of the genitourinary and gastrointestinal tract , for example, with renal colic, pyloric spasms, cholecystitis and intestinal colic;
• exacerbation of gastric ulcer and duodenal ulcer;
• dyskinesia of the bile ducts and gallbladder;
• algodismenorrhea and so on.

In addition, indications for the use of Buscopan suppositories for patients before labor were noted.

Contraindications for use

It is not recommended to take tablets:

• patients under 6 years of age;
• if you have hypersensitivity to Buscopan and its components;
• for myasthenia gravis , megacolony , angle-closure glaucoma and pulmonary edema .

Additional contraindications for suppositories are:

• prostate adenoma;
• abnormalities in cardiac activity and cerebral vessels.

Side effects

Taking Buscopan may be accompanied by unwanted effects caused by the anticholinergic properties of the drug. Therefore, they are usually mild in severity and pass quickly without additional intervention.

Patients are especially often concerned about:

• skin peeling , urticaria , itching , irritation;
• dry mouth;
• difficulty breathing;
• tachycardia , arrhythmia;
• problems with urination and so on.

Pharmacological properties of hyoscine butyl bromide

Hyoscine butyl bromide (HBB) is a hyoscine derivative obtained from the leaves of the Duboisia tree, native primarily to Australia. GBB is also known as scopalamine-N-butyl bromide, N-butylscopolammonium bromide and butylscopolamine. The molecular formula is C21H30BrNO4, the molecular weight is 440.37.

GBB contains a nitrogen molecule linked by four different bonds with different chemical groups; thus, it is a quaternary ammonium compound. The GBB molecule is highly polarized and, unlike ammonium and other similar compounds, retains polarity regardless of the pH of the environment. In this regard, when administered orally, only partial absorption of the drug occurs (8%), and systemic bioavailability is less than 1%. However, despite low blood levels immediately after administration, GBB and/or its metabolites are detectable at the sites of action.

The drug does not penetrate the blood-brain barrier and has low binding to plasma proteins. Metabolism is carried out mainly by hydrolysis of the ester bond. After oral administration, excretion of the drug occurs in feces and urine.

As is known, in the parasympathetic nervous system, acetylcholine (ACCh) acts on two types of receptors, muscarinic and nicotinic cholinergic receptors. In most cases, nerve transmission occurs in two stages: upon stimulation, the preganglionic nerve releases ACh into the ganglion, which acts on the nicotinic receptors of postganglionic neurons. The postganglionic neuron then releases ACh to excite muscarinic receptors in the target organ.

Three main types of muscarinic receptors have been well studied:

• M1-muscarinic receptors are found in the nervous system.

• M2-muscarinic receptors, located in the heart.

• M3 muscarinic receptors are located in many parts of the body, especially in the smooth muscle of the blood vessels, bronchi and gastrointestinal tract (GIT), as well as various glands associated with the respiratory tract and GI tract. Stimulation of these receptors leads to indirect vasodilation (via the formation of nitric oxide), bronchoconstriction and increased intestinal motility, as well as increased glandular secretion. M3 receptors are also found in the ciliary body and muscles of the iris, where they are involved in accommodation and allow control of pupil size.

There are also M4 and M5 receptors; the latter are found only in the central nervous system (CNS). The full characteristics of the action and localization of M5 receptors are not fully understood.

Recent studies have also shown that GBB is a potent non-competitive nicotinic receptor blocker in vitro. If such an effect occurs in vivo, it may contribute to the known mechanism of the antispasmodic action of the drug [2].

GBB blocks the action of ACh in the parasympathetic receptors of smooth muscles and secretory glands. This is the basis for both the mechanism of action of GBB and its side effects. Thus, GBB causes a decrease in motility of the gastrointestinal tract and genitourinary tract, and is used to eliminate spasms of these systems, the appearance of which is possible with gastroenteritis, colitis, inflammatory bowel diseases, diverticulitis, biliary colic, cystitis, colic with urethritis and primary dysmenorrhea. It is also used to prevent gastrointestinal spasms before radiological and diagnostic tests, such as endoscopic retrograde cholangiopancreatography and colonoscopy. Based on the mechanisms of action of GBB, side effects/adverse reactions may occur.

The most common of these are: skin reactions (eg, urticaria, rash, erythema, itching) and other types of hypersensitivity, tachycardia, dry mouth, urinary retention. Many of the listed undesirable effects may be associated with the anticholinergic properties of the drug. Anticholinergic side effects are usually mild and self-limiting. It should be noted that, as a quaternary ammonium compound, GBB does not penetrate the blood-brain barrier and therefore does not cause adverse effects from the central nervous system.

Peripheral anticholinergic effects develop due to the ganglion-blocking effect on the walls of internal organs, as well as due to the antimuscarinic effect.

The use of GBB is contraindicated in myasthenia gravis and megacolon/Hirschsprung's disease. In addition, it should not be administered parenterally to patients with uncompensated narrow-angle glaucoma, with tachycardia; prostate hypertrophy with urinary retention; with mechanical stenosis of the gastrointestinal tract.

Overdose

Cases of overdose with Buscopan have not been established, but the occurrence of the symptoms described in the list of side effects should not be excluded.

In such situations, the following treatment procedures are recommended:

• gastric lavage;
• taking activated carbon or other means of similar action;
• use of cholinomimetics intravenously or intramuscularly.

All other complications require symptomatic therapy.

Review of the clinical use of hyoscine butyl bromide

Abdominal pain (nonspecific colic) and IBS

The ability of GBB to eliminate nonspecific colicky ABs is explained by its antimuscarinic effect. Clinically, this effect is manifested by relaxation of the smooth muscles of the gastrointestinal tract, due to which the spasms/colic felt by the patient decrease/disappear. This effect was objectively demonstrated in a study of the electrical and biomechanical activity of the stomach, in which intravenous administration of 20 mg of GBB led to a decrease in mechanical motility by 50.9%, and electrical motility by 36.5% [3].

The main areas of clinical application of GBD in AB were nonspecific abdominal pain of the colic type, IBS, biliary colic and GERD.

The use of GBB in nonspecific AB has been studied in a number of recent studies. A recent large study compared the efficacy and tolerability of 10 mg GBB 3 times daily, 500 mg paracetamol 3 times daily, and a fixed combination of the two compared with placebo in patients with intermittent abdominal cramping pain [4]. All 1637 patients were given a placebo for a week, after which they were randomized to receive one of 4 treatments for 3 weeks. Pain severity (as measured by visual analogue scale and verbal rating scale) was statistically significantly reduced in all treatment groups compared to placebo. Treatment was well tolerated in all groups, and the incidence of side effects did not differ significantly between groups.

Another study of 204 children followed for a week compared GBD with a homeopathic remedy. Both medications were found to provide significant symptomatic relief (severity of spasms, pain/colic, sleep disturbances, difficulty eating and drinking, frequent crying) as assessed by the parent/caregiver, and were well tolerated [5].

Tytgat et al. published two reviews regarding the use of oral/enteral GBD for the treatment of cramping abdominal pain and a number of other clinical scenarios [6, 7]. The first of them contains 10 placebo-controlled studies that examined the effectiveness and safety of oral and rectal use of GBB. The effectiveness of the drug has been established in all studies, which is considered by the authors as evidence in support of the use of the drug for abdominal pain associated with cramps.

The second review provides evidence on the use of GBD for the treatment of colic/spasms; for diagnostic purposes - during visualization; regarding the therapeutic effectiveness and safety of parenteral administration of GBB for the treatment of biliary and renal colic, severe spasms of the genitourinary tract; as well as during childbirth and as palliative treatment. The authors concluded that GBB preparations are fast-acting and highly effective and well tolerated, which supports their use in a number of indications associated with acute abdominal cramps, during childbirth, for palliative treatment, and during diagnostic and therapeutic procedures of the abdominal organs. cavities that can impede spastic contraction [7]. The pharmacological profile of GBB suggests the possibility of its use in conditions accompanied by intestinal irritation. A double-blind, randomized, parallel-group comparative study was conducted, which included 712 patients with IBS. Patients were prescribed: GBB + paracetamol, GBB, paracetamol or placebo for 4 weeks. A visual analogue scale was used to assess symptoms, and by the end of treatment, more than 75% of patients in the GBD group experienced symptom relief [8]. There was also a statistically significant decrease in AB intensity in the GBD group compared to placebo and paracetamol. Other researchers have confirmed the equal effectiveness of GBB and similar drugs, plus their advantage over placebo in the treatment of IBS [9–11].

Renal colic

Renal colic is usually a consequence of the presence of a calculus (stone) in the ureter (less often in the bladder); the severe paroxysmal pain that accompanies this condition is caused by periodic spastic contractions of the blocked hollow organ, aimed at eliminating the blockage. It seems logical that a drug that can eliminate such spasms in the urinary system would have good analgesic effects, which a number of studies have been conducted to evaluate.

Six studies involving 755 patients were identified that assessed GBD as adjunctive pain relief with nonsteroidal anti-inflammatory drugs (NSAIDs) [15–18] and other antispastic drugs [19]. In comparison, the combination of GBB and pethidine was more effective than diclofenac sodium alone [15], although both drugs were more than 90% effective in providing pain relief 30 minutes after administration. Studies have shown that GBB monotherapy is effective in relieving pain, although it is inferior in this regard to therapy using dipyrone and diclofenac [17] or dipyrone and tramadol [19]. Similarly, studies conducted to compare the combination of GBB and dipirone with tenoxicam [16] as well as flurbiprofen [18] confirmed that this combination provided significant pain relief.

Thus, the available data support the effectiveness of GBB in the treatment of renal colic, both as monotherapy and in combination with other drugs.

Dysmenorrhea

Two recent studies examined the use of GBD in primary and secondary dysmenorrhea. In the first double-blind crossover study of 120 women, GBB and paracetamol were compared with lysine clonixinate and proprinox and placebo [20]. Both treatment groups showed a significant reduction in subjective pain ratings compared to placebo.

A second, long-term, open-label study examined the combined use of lysine clonixinate and GBB during three consecutive menstrual cycles in 30 women [21]. All women initially reported very severe (10.7%), severe (42.9%) or moderate (46.4%) pain. By the end of the study, moderate pain persisted in one patient.

Childbirth

Only one study was found that examined GBB primarily as an analgesic for pain associated with childbirth. The study observed 104 primigravida women during labor and delivery; It was found that intravenous administration of GBB leads to a 36% reduction in pain compared with placebo [22].

Some authors have studied the effects of GBB as a labor accelerator, with the argument that if labor pain cannot be safely eliminated, it may be possible to safely reduce the duration of labor (and thus the pain). Five similar studies were found, three of which compared the drug with saline or no treatment [22–24]. One study compared GBB with another antispasmodic drug (drotaverine) [25], and another compared GBB with drotaverine and no therapy [26]. The drug was administered intravenously in 4 studies at doses ranging from 20 to 40 mg, and in one study - rectally [23]. The last 4 studies involved 533 women, divided into almost equal groups; the use of GBB led to a statistically and clinically significant reduction in the period between drug administration and delivery in the absence of significant adverse reactions on the part of the mother or newborn.

Discomfort and pain associated with manipulation

GBB has been studied as a tool to facilitate various studies of the gastrointestinal tract and nearby structures.

In 3 studies, the effectiveness of GBB compared with placebo (2 studies; 208 patients) and glucagon (1 study; 100 patients) was assessed during sigmoidoscopy and/or colonoscopy. One study comparing the drug and placebo showed a reduction in procedure time in the group receiving GBB [27].

Magnetic resonance imaging can be used to obtain high-resolution images of the upper gastrointestinal tract. A study conducted by Wagner et al. [30], showed that intramuscular administration of GBB significantly improves image quality on T2-weighted magnetic resonance imaging of the abdominal cavity. In addition, magnetic resonance imaging of the liver and pancreas has been found to be slightly better at suppressing gastrointestinal motility by GBD.

Interaction

The simultaneous use of Buscopan and tricyclic antidepressants, Hindin, antihistamines, amantadine and disopyramide may enhance the anticholinergic effect.

Combined use with dopamine antagonists , for example, metoclopramide , weakens the effect of each drug on the gastrointestinal tract.

Complex treatment with Buscopan and beta-adrenergic drugs often increases tachycardia .

special instructions

Treatment with Buscopan requires special instructions. For example, you need to stop using the drug gradually, since rapid withdrawal can cause nausea , sweating and dizziness .

It is also recommended to refrain from overheating when performing physical activity, in the heat, in the bath and sauna. If dry mouth does not disappear for more than 2 weeks, then the risk of developing damage to tooth enamel, gums, and fungal infections . When treating with Buscopan, you should be careful when driving vehicles and other activities that require high attention.

Analogues of Buscopan

In pharmacology there are no analogues of this drug for the active substance.

The list of analogues by pharmacological group includes: Atrovent, Atropine, Gastrocepin, Gastrozem, Driptan, belladonna extract, Midriacil, Novitropan, Spazmex, Trigan and others. Moreover, the price of analogues may vary depending on the manufacturer, the active substance and the number of doses in the package. To change treatment, you must consult a doctor.

How to use Buscopan: instructions

The drug is approved for use by patients over the age of 6 years. It can be used once: for spontaneous spasms of unknown origin, or in short courses: for exacerbations of pathologies, regular painful conditions.

The tablets are taken orally, without chewing, with plenty of clean still water. It is recommended to take 30 minutes before meals or 1.5 hours after, since food can slow down the absorption of the active substance and the development of the pharmacological effect. Daily doses depend on the severity and nature of the spasms:

• for moderately painful symptoms and in childhood, it is enough to take 1 tablet twice a day;
• for severe cramps, the dosage is increased to 6 tablets per day: 2 pcs. three times a day.

Suppositories are used rectally, inserted into the anus for similar symptoms and in appropriate doses:

• children under 12 years of age and adults with mild spasms: 1 suppository 2-3 times a day, keeping a break between administrations of 5-6 hours;
• in case of severe pain, double the dose, using 2 suppositories.

It is noted that the effect of suppositories for spasms in the pelvic organs occurs faster than after taking tablets. For diseases of the small intestine, gallbladder or stomach, it is best to use the oral form of the drug.

Reviews of Buscopan

Discussions of this drug are found on various thematic forums dedicated to pregnancy . As reviews of Buscopan show, suppositories are often prescribed before childbirth, which help prepare the cervix for labor. Most patients, leaving reviews of Buscopan suppositories during pregnancy, note that its effectiveness is not always evident. Some users know that suppositories are prescribed during childbirth, and are interested in what the pills help with. There are also reports that the use of medicine in the treatment of pain and colic can quickly eliminate the problem.

When is Buscopan indicated?

The drug is prescribed to eliminate painful spasms:

• with exacerbation of gastritis, ulcerative pathology of the stomach, duodenum, pancreatitis, cholecystitis, inflammation of the bile ducts, impaired liver function;
• colic in the intestines, kidneys;
• abdominal pain;
• with painful menstruation: at the first signs of cramps, during the period of discharge;
• in other conditions accompanied by painful muscle contractions.

In some cases, Buscopan is used to facilitate cervical dilatation during the prenatal period. Suppositories and tablets are also used in the complex treatment of complications of osteochondrosis.

Buscopan price, where to buy

On average, the price of Buscopan in Moscow pharmacies can vary from 275 to 369 rubles. At the same time, the price of Buscopan candles is higher.

In Ukrainian pharmacies, tablets or suppositories can be purchased for 225-263 UAH.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Buscopan rectal suppositories 10 mg 10 pcs. Boehringer/Instituto de Angeli Srl
  478 RUR order
• Buscopan tablets p.p.o. 10 mg 20 pcs Delpharm Reims

  RUR 507 order

Pharmacy Dialogue

• Buscopan tablets 10 mg No. 20Boehringer Ingelheim

  RUR 538 order

• Buscopan suppositories 10 mg No. 10 Boehringer Ingelheim

  RUR 507 order

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Pharmacy24

• Buscopan 10 mg No. 6 suppositories Istituto de Angeli S.r.l., Italy
  41 UAH.order
• Buscopan 20 mg/ml 1 ml No. 5 solution Boehringer Ingelheim Espana, CA, Spain

  90 UAH order

• Buscopan 10 mg No. 20 tablets Delpharm Reims, France

  54 UAH order

PaniPharmacy

• Buscopan ampoule Buscopan solution d/in. 20mg amp. 1ml No. 5 Spain, Boehringer Ingelheim Espana

  127 UAH order

• Buscopan suppository Supp. buscopan 10 mg No. 10 Italy, Instituto de Angeli

  49 UAH order

• Buscopan tablets Buscopan etc. 10 mg No. 20 France, Delpharm Reims

  62 UAH.order

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