But-shpa - instructions for use, analogs, reviews and release forms (tablets 40 mg, 80 mg forte, injections in ampoules for injection) of a drug for the treatment of spasms and pain in adults, children and pregnancy

In this article, you can read the instructions for using the drug But-shpa. There are reviews of visitors to the site - consumers of this medicine, as well as opinions of doctors of specialists on the use of No-shpa in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues No-shpas in the presence of existing structural analogs. Use for treatment and relief of spasmodic pain in adults, children, as well as during pregnancy and lactation.

But-shpa - myotropic antispasmodic, isoquinoline derivative.Has a powerful spasmolytic effect on smooth muscle by inhibiting the enzyme PDE. Enzyme PDE is necessary for the hydrolysis of cAMP to AMP. Inhibition of PDE leads to an increase in the concentration of cAMP, which triggers the following cascade reaction: high concentrations of cAMP activate cAMP-dependent phosphorylation of myosin light chain kinase (CMLC). Phosphorylation of CMLC leads to a decrease in its affinity for the Ca2 + -culmodulin complex, as a result of which the inactivated form of CLCM supports muscular relaxation. In addition, cAMP affects the cytosolic concentration of the Ca2 + ion by stimulating Ca2 + transport into the extracellular space and the sarcoplasmic reticulum. This reducing the concentration of the Ca2 + ion, the effect of Drotaverin (the active substance of the preparation of Ho-shpa) through cAMP explains the antagonistic effect of drotaverin relative to Ca2 +.

In vitro, drotaverin inhibits the isoenzyme PDE4 without inhibiting the isoenzymes PDE3 and PDE5. Therefore, the effectiveness of drotaverine depends on the concentration of PDE4 in the tissues (the PDE4 content varies in different tissues).PDE4 is most important for suppressing the contractile activity of smooth muscle, and therefore selective inhibition of PDE4 can be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by spastic state of the gastrointestinal tract.

The hydrolysis of cAMP in the myocardium and smooth musculature of the vessels is mainly due to the isoenzyme of PDE3, which explains the fact that at high antispasmodic activity in No-shpa there are no serious side effects from the heart and vessels and pronounced effects on the cardiovascular system .

Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of vegetative innervation, drotaverin relaxes the smooth musculature of the digestive tract, the bile duct, the urogenital system.

Pharmacokinetics

After ingestion of No-shpa quickly and completely absorbed. After presystemic metabolism, 65% of the accepted dose of drotaverine enters the systemic circulation. Drotaverin is evenly distributed in tissues, penetrates into smooth muscle cells. Does not penetrate the blood-brain barrier.Drotaverin and / or its metabolites are able to penetrate insignificantly through the placental barrier. Within 72 hours, drotaverin is almost completely eliminated from the body. More than 50% of drotaverin is excreted by the kidneys and about 30% by the intestine (excretion into the bile). Drotaverin is mainly excreted in the form of metabolites, unchanged drotaverine in the urine is not detected.

Indications

• spasms of smooth muscles in diseases of bile ducts: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
• spasms of smooth muscles of the urinary system: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms.

As an auxiliary therapy:

• with spasms of smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, spasms of cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence after exclusion of diseases manifested by the syndrome "acute stomach" (appendicitis, peritonitis, perforation ulcers, acute pancreatitis);
• tension headaches (for oral administration);
• algodismenorea.

Forms of release

Tablets of 40 mg.

Tablets No-shpa forte 80 mg.

Solution for intravenous and intramuscular injection (injections in ampoules for injection).

Instructions for use and dosage

Adults with oral intake of the recommended daily dose is 120-240 mg (2-3 reception). The maximum single dose is 80 mg. The maximum daily dose is 240 mg.

The average daily dose for intramuscular administration to adults is 40-240 mg (divided by 1-3 administration per day). In acute colic (renal or bile), the drug is administered intravenously slowly in a dose of 40-80 mg (duration of administration is approximately 30 seconds).

Clinical studies using drotaverine with the participation of children have not been conducted.

In the case of the No-shpa preparation, the maximum daily intake for children aged 6 to 12 years is 80 mg in 2 divided doses, at the age of 12 years, 160 mg in 2-4 doses.

Duration of treatment without consulting a doctor

When taking the drug without consulting a doctor, the recommended duration of taking the drug is usually 1-2 days. If during this period the pain syndrome does not decrease, the patient should consult a doctor to clarify the diagnosis and, if necessary, change the therapy.In cases where the NO-shpa is used as an adjuvant therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).

Method for evaluating effectiveness

If the patient can easily diagnose the symptoms of his disease, because they are well known to him, then the effectiveness of treatment, namely the disappearance of pain, is also easily identifiable by the patient. In the event that a few hours after taking the drug at the maximum single dose, there is a moderate reduction in pain or no pain reduction, or if the pain does not decrease significantly after taking the maximum daily dose, it is recommended to see a doctor.

Side effect

• cardiopalmus;
• a decrease in blood pressure;
• headache;
• dizziness;
• insomnia;
• nausea;
• constipation;
• itching;
• rash;
• hives;
• angioedema;
• reaction at the site of administration.

Contraindications

• severe renal failure;
• severe hepatic impairment;
• severe heart failure (low cardiac output syndrome);
• children under 6 years (for tablets);
• children's age (for parenteral administration, t.no clinical trials have been conducted in children);
• the period of breastfeeding (no clinical data);
• rare hereditary intolerance to galactose, lactase deficiency, glucose-galactose malabsorption syndrome (for tablets, due to the presence of lactose in their composition);
• hypersensitivity to the components of the drug;
• hypersensitivity to sodium disulfite (for solution for iv and / m administration).

Application in pregnancy and lactation

As shown by studies of reproductive performance in animals and retrospective data on clinical use, the use of No-shpa in pregnancy had neither teratogenic nor embryotoxic effects.

In pregnancy, the drug should be used with caution and only in those cases where the potential benefit of therapy for the mother exceeds the possible risk to the fetus.

Due to the lack of necessary clinical data, the drug is contraindicated during lactation (breastfeeding).

special instructions

The tablet contains 52 mg of lactose, and as a result, complaints can be made by the digestive system in patients who are intolerant of latosis.Therefore, the drug in the form of tablets is not prescribed for patients with lactase deficiency, galactosemia or glucose / galactose impaired absorption syndrome.

The solution for intravenous and intramuscular injection includes sodium bisulfite, which can cause allergic reactions, including anaphylactic and bronchospasm, in sensitive individuals (especially in persons with bronchial asthma or allergic reactions in the anamnesis). With increased sensitivity to sodium metabisulfite, parenteral administration of the drug should be avoided.

With iv administration of the drug to patients with low blood pressure the patient should be in a horizontal position in connection with the risk of developing a collapse.

Impact on the ability to drive vehicles and manage mechanisms

When administered orally in therapeutic doses, drotaverin does not affect the ability to drive vehicles and perform work that requires increased concentration of attention.

In case of any adverse reactions, the issue of driving and working with machinery requires individual consideration. In the case of dizziness after taking the drug, you should avoid engaging in potentially hazardous activities,such as vehicle management and working with mechanisms.

After parenteral administration of the drug, it is recommended to refrain from driving vehicles and practicing other potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Drug Interactions

PDE inhibitors like papaverine weaken the anti-Parkinsonian effect of levodopa. When prescribing No-shpa preparation simultaneously with levodopa, strengthening of rigidity and tremor is possible.

With simultaneous application with drotaverine, the spasmolytic effect of papaverine, bendazole and other antispasmodics, including m-cholinoblockers, increases.

No-shpa increases arterial hypotension caused by tricyclic antidepressants, quinidine and procainamide.

But-shpa reduces the spasmogenic activity of morphine.

Phenobarbital enhances the spasmolytic effect of drotaverine.

Drotaverin is largely associated with plasma proteins, mainly albumin, beta and gamma globulins. Data on the interaction of drotaverine with preparations that significantly bind to plasma proteins are not available.However, we can assume the possibility of their interaction with No-shpa at the level of binding to plasma proteins - displacement of one of the drugs to another of the binding sites and an increase in the concentration of free fraction in the blood of the drug with weaker binding to proteins. This may hypothetically increase the risk of pharmacodynamic and / or toxic side effects of this drug.

Analogues of the drug No-shpa

Structural analogs for the active substance:

• Vero-Drotaverine;
• Droverin;
• Drotaverine;
• Drotaverin forte;
• Drotaverina hydrochloride;
• NOSH-BRA;
• Ple-Spa;
• Spazmol;
• Spasmonet;
• Spasmonet forte;
• Cosporeine;
• Spacock.

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