Gazospazm

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT GAZOSPAZAMÒ (GAZOSPAZAMÒ)

Composition:

Active substances: simethicone, dicycloverine hydrochloride;

1 tablet contains simethicone 125 mg, dicycloverine hydrochloride 20 mg;

Excipients: magnesium-aluminum silicate, lactose monohydrate, microcrystalline cellulose, calcium hydrogen phosphate, stearic acid, colloidal anhydrous silicon dioxide, crospovidone, povidone K29/32, Opadry II 85G 54275 pink: iron oxide red (E 172), lecithin, polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide (E 171).

Pharmaceutical form. Coated tablets.

Main physico-chemical properties: oval, biconvex, smooth on both sides coated tablets of pink color.

Pharmacotherapeutic group.

Spasmolytics and anticholinergics in combination with other drugs. Spasmolytics in combination with other agents.

ATC code: A03ED.

Pharmacological Properties

Pharmacodynamics

Gasospazam® is a combination medication containing two active ingredients: dicycloverine hydrochloride and simethicone.

Dicycloverine hydrochloride exerts a spasmolytic effect (relieves smooth muscle spasm in the gastrointestinal tract and associated abdominal pain due to this spasm or distension of the gastrointestinal wall) and antisecretory effects on exocrine glands. The action of dicycloverine is achieved through its specific anticholinergic (antimuscarinic) activity on acetylcholine receptors, as well as a direct spasmolytic effect on smooth muscles. Studies have shown that dicycloverine is equally effective against spasms induced by acetylcholine and barium chloride. In contrast, the effect of atropine is 200 times weaker in barium chloride-induced spasm than in acetylcholine-induced spasm. The mydriatic effect of dicycloverine and its effect on salivary gland secretion are negligible compared to those of atropine (1/500 and 1/300, respectively).

Simethicone is a surfactant and an antifoaming agent. Its mechanism of action is based on reducing the surface tension of gas bubbles, facilitating the free elimination of gases from the gastrointestinal tract or their absorption through the intestinal wall. Simethicone improves the quality of X-ray and ultrasound images and ensures better distribution of contrast agents on the intestinal mucosa.

Pharmacokinetics

Dicycloverine hydrochloride is rapidly absorbed from the gastrointestinal tract following oral administration. Maximum plasma concentration is reached within 60–90 minutes. It is primarily excreted in urine (79.5% of the administered dose) and partially in feces (8.4%). The mean elimination half-life is 1.8 hours. The mean volume of distribution is 3.65 L/kg.

Simethicone is physiologically and chemically inert. It is not absorbed and is excreted unchanged after passing through the gastrointestinal tract.

Clinical characteristics.

Indications.

Treatment of conditions associated with smooth muscle spasm of the gastrointestinal tract and meteorism, as well as abdominal pain related to these conditions. Treatment of spastic conditions of the gastrointestinal tract, including colitis, intestinal colic, irritable bowel syndrome, spastic constipation. As adjunctive therapy in organic gastrointestinal diseases such as colitis, diverticulitis, enteritis, gastritis, and peptic ulcers.

Contraindications.

Hypersensitivity to components of the drug.

Obstructive gastrointestinal disorders, paralytic ileus, pyloric stenosis of the gastrointestinal tract with obstruction, severe ulcerative colitis or toxic megacolon, reflux esophagitis.

Obstructive biliary tract disorders.

Renal insufficiency, obstructive urinary tract disorders, benign prostatic hyperplasia with urinary retention.

Glaucoma.

Myasthenia gravis.

Thyrotoxicosis.

Cardiac failure, unstable cardiovascular status during acute hemorrhage.

Interaction with other medicinal products and other types of interactions.

Amantadine, class I antiarrhythmic agents (e.g., quinidine), antihistamines, antipsychotic agents (e.g., phenothiazines), benzodiazepines, monoamine oxidase inhibitors, narcotic analgesics (e.g., meperidine), nitrates and nitrites, sympathomimetics, tricyclic antidepressants, corticosteroids, and other agents with anticholinergic activity may enhance the effect or adverse effects of dicycloverine.

Anticholinergic agents may neutralize the effect of antiglaucoma drugs; therefore, the drug should be administered with caution in patients with elevated intraocular pressure and during concomitant use of corticosteroids.

Anticholinergic agents enhance the effect of digoxin, salicylic acid, pyrazolone, codeine, caffeine, and other cholinolytic agents (e.g., atropine sulfate); therefore, concomitant use with dicycloverine hydrochloride is not recommended.

Dicycloverine may neutralize the effect of drugs affecting gastrointestinal motility, such as metoclopramide. It potentiates the effect of spasmolytics.

Since antacids may reduce the absorption of anticholinergic agents, their concomitant use should be avoided.

The inhibitory effect of anticholinergic agents on gastric hydrochloric acid secretion may be neutralized by drugs used in the treatment of achlorhydria and in studies of gastric secretion.

Intestinal absorption of levothyroxine may be impaired when administered concomitantly with simethicone.

Special precautions for use

In conditions of high ambient temperature during treatment with the drug, there is a risk of overheating (elevated body temperature and heat stroke due to reduced sweating). If such symptoms occur, the drug should be discontinued and medical advice sought immediately.

Diarrhea may be an early sign of incomplete intestinal obstruction, particularly in patients with ileostomy or colostomy. In such cases, the drug should not be used.

In individuals with individual hypersensitivity to anticholinergic agents, the drug may cause central nervous system effects such as confusion, disorientation, ataxia, increased fatigue, or, conversely, euphoria, excitement, insomnia, and affective disturbances. These symptoms usually resolve within 12–24 hours after discontinuation of the drug.

Gasospazam® should be used with caution in patients with autonomic neuropathy, hepatic or renal disease, ulcerative colitis (administration of high doses may cause paralytic ileus and development or exacerbation of a serious complication such as toxic megacolon), arterial hypertension, ischemic heart disease, congestive heart failure, tachyarrhythmias, tachycardia, hiatal hernia, and prostate hyperplasia.

Excipients. The drug contains lactose. If you have been diagnosed with an intolerance to certain sugars, consult your doctor before taking this medication.

Use during pregnancy or breastfeeding.

The safety of treatment with dicycloverine and simethicone during pregnancy has not been established; therefore, the drug should not be used during pregnancy.

Since dicycloverine hydrochloride is excreted in breast milk, the drug should not be used during breastfeeding.

Ability to influence reaction rate while driving or operating machinery.

Dicycloverine hydrochloride may cause drowsiness and blurred vision. Therefore, it is not recommended to drive or operate complex machinery requiring high attention and rapid psychomotor reactions during treatment with this drug.

Dosage and Administration.

Adults and children aged 12 years and older: 1 tablet up to 4 times daily.

The maximum daily dose is 4 tablets.

The medication should be taken before or after meals. The medication is not recommended for use longer than 5 days.

Children.

Do not use in children under 12 years of age.

Overdose.

Overdose is characterized by a biphasic course: initially, central nervous system stimulation occurs, manifested by restlessness, illusions, hallucinations, persistent mydriasis, tachycardia, and arterial hypertension. This is followed by depression of the central nervous system, progressing to a comatose state.

Symptoms: headache, nausea, vomiting, abdominal pain, loss of appetite, pallor of the skin, increased intraocular pressure, dizziness, blurred vision, dilated pupils, hot and dry skin, dry mouth, difficulty swallowing, central nervous system excitation, tachycardia, and changes in respiratory rate.

Curare-like effects (neuromuscular blockade, sensation of muscle weakness, and paralysis) may also occur.

Treatment: symptomatic therapy. Within the first hours, induce vomiting, perform gastric lavage, and administer adsorbents.

For relief of psychomotor agitation, diazepam (0.5% solution, 2 ml) may be used.

Adverse reactions.

The adverse effects listed below relate to the group of anticholinergic medicinal products; not all of them have been observed during administration of dicycloverine hydrochloride:

Gastrointestinal disorders: dry mouth, taste disturbances, anorexia, nausea, vomiting, dyspepsia, bloating, abdominal pain, constipation.

Central nervous system disorders: tinnitus, headache, drowsiness, weakness, nervousness, psychosis, numbness, dizziness, coma, confusion and/or excitement (especially in elderly patients), dyskinesia, insomnia, disorientation, transient memory loss, hallucinations, dysarthria, ataxia, euphoria, inadequate emotional responses (symptoms subside within 12–24 hours after dose reduction).

Eye disorders: blurred vision, diplopia, mydriasis, cycloplegia, increased intraocular pressure (transient atropine-like effects which resolve after discontinuation of dicycloverine).

Skin and hypersensitivity reactions: hypersensitivity reactions including allergic dermatitis, pruritus, rash, urticaria, erythema, drug-induced idiosyncrasy, angioneurotic edema, anaphylactic shock.

Urinary system disorders: dysuria, urinary retention.

Cardiovascular disorders: tachycardia, palpitations.

Respiratory system disorders: asthma, apnea, nasal congestion.

Other effects: decreased sweating, sneezing, edema of the pharyngeal mucosa, suppression of lactation.

Shelf life.

2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

7 tablets in a blister; 2 blisters per cardboard pack.

15 tablets in a blister; 1, 2, or 4 blisters per cardboard pack.

Classification.

Over-the-counter (without prescription).

Manufacturer.

LLC "KUSUM PHARM".

Manufacturer's address and place of business.

40020, Ukraine, Sumy region, Sumy city, Skryabina Street, 54.

or

Manufacturer.

LLC "GLEDPHARM LTD".

Manufacturer's address and place of business.

40020, Ukraine, Sumy region, Sumy city, Hryhoriya Davydovskoho Street, 54.