What helps and how to inject no-spa in ampoules for children and adults. "No-spa" intramuscularly: instructions for use, purpose, dosage, composition, indications and contraindications. Is it possible to take a solution of noshpa orally?

How to use No-shpu intramuscularly? Let's find out in this article.

The drug "No-shpa" is a drug based on the substance drotaverine, which is produced in the form of tablets and ampoules. The medicine gives an antispasmodic effect and is used in the treatment of spastic syndrome of the digestive tract, reproductive, hepatobiliary and urinary systems. In addition, this medication relieves spasms of cerebral vessels in case of headaches arising from overexertion as a result of depression and neurosis, and of peripheral vessels in case of Raynaud's disease or endarteritis.

The active substance is a derivative of papaverine. The non-proprietary international name of the drug “No-shpa” is “Drotaverine”. According to the clinical and pharmacological classification, it is classified as a myotropic antispasmodic. In its properties, the substance is very similar to papaverine, but has a longer and more pronounced relaxing effect on muscle fibers.

The effectiveness of the pharmacological agent is due to its ability to have an inhibitory effect on the enzyme phosphodiesterase, which, through a series of chemical reactions, can catalyze the inactivation of myosin chain kinase. This kinase phosphorylates myosin and provokes muscle contraction. When it is relieved, muscle relaxation is maintained. The positive properties of the drug also include selective suppression of only the fourth type of PDE, which does not affect the third type enzyme and does not cause negative side effects from the blood vessels and heart.

Drotaverine causes muscle relaxation when spasms of both neurogenic and myogenic origin occur and, regardless of the type of innervation, relaxation of muscle fibers. The essential advantage of this medication is that there is no stimulating effect on the cholinergic system, as a result of which the drug “No-shpa” can be used in people suffering from a disease such as glaucoma. However, some caution must be exercised when taking it, especially in the presence of prostatic hypertrophy, since symptoms of urinary retention may occur due to relaxation of the detrusor muscle in the bladder. So "No-shpa" intramuscularly is prescribed very often.

Composition and release form

The medical product “No-shpa” for intramuscular administration is produced in glass ampoules containing 2 ml of injection solution. The volume of the active element in 1 ml is 20 mg of drotaverine. Injections can be carried out through intra-arterial, intravenous and intramuscular administration. The solution has a bright yellow-green color.

Indications for use

Indications for the use of the pharmacological agent "No-shpa" intramuscularly are the prevention and treatment of organ functional disorders and pain syndrome caused by:

• muscle spasms digestive organs tract with ulcers, gastritis, dyskinesia, pancreatitis, spastic enteritis, proctitis or colitis, as well as with spasms of the pylorus or cardia, irritable bowel, development of flatulence, spastic constipation, tenesmus;
• dysfunction of the hepatobiliary system inflammatory processes V gallbladder or its ducts, hyperkinetic forms of biliary dyskinesia, cholelithiasis;
• excessive excitability of the uterus during pregnancy;
• spasms of the urinary system with the development of kidney stones, pyelitis, urolithiasis, neurogenic Bladder, pyelonephritis, cystitis;
• spasms of the uterine pharynx during the birth process;
• prolonged opening of the uterine pharynx;
• postpartum contractions;
• the threat of spontaneous miscarriage;
• menstruation.

This is stated in the instructions. “No-spa” is also used intramuscularly when spasms of cerebral and peripheral vessels occur. Effective for postoperative colic due to gas retention, preparation for instrumental studies, postcholecystectomy syndrome.

Use of “No-shpa” injections for children

Children under six years of age are prohibited from injecting the drug intramuscularly. It is important to know that the main substance of the drug is synthesized artificially. In other words, it is not a natural element. Therefore, No-shpu is usually used intramuscularly for children only as prescribed by a specialist.

The medicine is a good antispasmodic, but does not have an analgesic effect like, for example, Analgin and similar drugs. In addition, it has some contraindications for use, which should also be taken into account when treating children.

Instructions for use for No-Spa injections indicate that this medicine is usually prescribed to young patients in the following cases:

• which is accompanied high temperature and coldness of the extremities.
• Spasms due to bronchitis or stenosis, causing coughing.
• Spasms causing headache.
• Renal or intestinal colic.
• Excessive painful gas.
• Smooth muscle spasm during pyelitis or cystitis.
• Spasms due to gastritis or colitis.

Contraindications for the use of No-shpa injections for children are:

• age up to 6 years;
• low blood pressure in a child;
• intolerance to drotaverine;
• vascular diseases;
• bronchial asthma;
• suspicion of intestinal obstruction;
• suspicion of acute appendicitis;
• liver and kidney failure.

In accordance with the instructions for use, No-shpy injections can be carried out during pregnancy.

Use during pregnancy

Among the medicines that are widely used during pregnancy, "No-shpa" plays a special role. Being a powerful antispasmodic, this medicine eliminates any pain associated with temporary dysfunction of the digestive tract in expectant mothers. In addition, during pregnancy, this medication is absolutely safe, it can be used without any concerns.

However, even taking into account these properties of the drug, care should be taken when using it during this period, since it has certain indications for use, contraindications and negative side reactions.

During pregnancy, "No-shpa" intramuscularly can be prescribed for uterine hypertonicity and the threat of preterm birth. At the first symptoms of preterm labor or the threat of spontaneous miscarriage, such as pulling painful sensations in the lower abdomen and a feeling of fullness in this area, a single application of "No-shpa" in most cases completely eliminates uterine hypertonicity and helps to maintain pregnancy.

Another indication for using this pharmacological drug- spasm of the smooth muscles of the uterus and cervix during childbirth. This situation is dangerous because the child is in a clamped state - excessive tension in the myometrial muscles helps expel it from the uterus, but the contracted cervix prevents its movement through the birth canal. In most cases, one dropper with this medicinal solution is enough to restore the normal birth process. The intramuscular dosage of No-shpa must be strictly observed.

Contraindications

• The main contraindication to the use of this medicinal product, like many other drugs, is a manifestation of severe disorders of the liver, kidneys, and heart, due to the insufficiency of their functions.
• In addition, the drug “No-shpa” is not prescribed during breastfeeding, since drotaverine and other representatives of this pharmacological category can pass into breast milk.
• The use of the drug is allowed from 6 years of age, but only in tablet form, since studies of the effects of injection solutions have not been carried out, according to which the use medical product Parenteral administration is contraindicated.
• Taking the medication is contraindicated if you have a high sensitivity to the active element or other substances from its composition.
• This medicinal product can only be used with certain precautions for low blood pressure due to the high likelihood of collapse, as well as during pregnancy.

What is the dosage of No-shpa intramuscularly?

Dosage regimen and methods of administration

A single dosage of the drug "No-shpa" in the form of solutions for intramuscular, intraarterial and intravenous administration depending on medical indications is 1-2 ampoules. The frequency of such injections is 1-3 times a day. How to administer No-shpu intramuscularly is indicated in the instructions.

During labor or after an abortion, it is allowed to administer the drug in an amount of 80 mg with a time interval of at least 2 hours. How long does it take for No-shpa to work? Intramuscular and intravenous injection allows you to get the desired result after 5 minutes. That is why injections of this medication have become widespread.

Side effects

Negative side reactions that can occur when using this pharmacological drug are extremely rare. Most often, its action negatively affects the nervous system, gastrointestinal tract, blood vessels and heart.

1. Nervous system: cephalalgia, dizziness, sleep disturbance.
2. Circulatory system: increased or rapid heartbeat, feeling of heat, irregular heartbeat, decreased blood pressure (sometimes to the point of collapse), atrioventricular blockade.
3. Digestive system: dyspepsia, nausea, stool disorders.

In addition to the above-mentioned negative effects of this medication, there is some information about side effects such as breathing problems, excessive sweating, and allergic reactions. Local redness or burning sensation may occur. Most often this manifests itself when the dosage of No-shpa injections is not observed.

There are also special instructions which should be strictly adhered to when using the drug “No-shpa”:

1. It is necessary to observe increased precautions when treating patients who suffer from atherosclerosis coronary arteries or reduced blood pressure.
2. The medicine is approved for use in complex therapy hypertensive crisis.
3. The issue of driving a vehicle while using the drug is decided on an individual basis, especially if its negative effects occur. In this case, it is advisable to refrain from driving and activities associated with the use of complex mechanisms, when using an antispasmodic in injection forms. If dizziness occurs after administration of No-shpa, it is prohibited to perform these types of work intramuscularly.
4. According to clinical studies, this medication does not have embryotoxic or teratogenic effects. However, it is necessary to remember the possible risk to the fetus and use the medication only for strict medical indications and with caution. The use of medication during pregnancy in the form of injections is undesirable.
5. The use of an antispasmodic during labor can cause the development of postpartum atonic bleeding.
6. IN pharmacological agent it contains metabisulfite (sodium disulfite) as an auxiliary element, which must be taken into account if you have hypersensitivity to it.
7. When administering this medication parenterally, patients suffering from hypotension should take a horizontal body position due to the high likelihood of collapse.

What else does the instruction to "No-shpe" (intramuscularly) tell us?

Drug interactions

Drotaverine, like other papaverine derivatives that inhibit PDE enzymes, can reduce the antiparkinsonian properties of levodopa, as well as increase muscle rigidity and tremor. With simultaneous therapy with other antispasmodic medications, mutual potentiation of antispasmodic effects may be observed. This pharmacological drug in injection form enhances the decrease in blood pressure caused by the use of antidepressants, quinidine or procainamide. This is confirmed by the instructions for use of No-shpa injections intramuscularly.

This medication reduces the spasmogenic effectiveness of morphine. When using phenobarbital, the antispasmodic effect of the drug “No-shpa” increases. Taking into account high level binding to plasma proteins (more than 80%) does not exclude the possibility of competition of this drug with medications that have the same feature. Taking this fact into account, if a combination of such drugs is used, the toxic effect of the medications taken may be enhanced.

Analogues

The medical product "No-spa" in the form of injection solutions has many analogues that have the same composition, but different bioequivalence and bioavailability. These medications include:

1. “Nosh-bra” is a medicine from the category of myotropic antispasmodics. By pharmacological properties and chemical structure is close to papaverine, but has a longer and stronger effect. Reduces the level of calcium ions entering smooth muscle cells (suppresses phosphodiesterase, promotes the accumulation of intracellular cAMP). Reduces muscle tone of organs and peristalsis, dilates blood vessels. Has no effect on autonomic nervous system, does not penetrate the central nervous system. The presence of a direct effect on smooth muscles allows the use of this drug as an antispasmodic in situations where medications of the M-anticholinergic class are contraindicated (prostatic hyperplasia, angle-closure glaucoma).
2. “Spazmol” is a medicine that is an antispasmodic with myotropic effects. A distinctive feature of this pharmacological drug is the presence of a long-lasting effect. The medicine affects not only smooth muscles internal organs, but also on the walls blood vessels. It can be taken to prevent the development of spasms or their presence in colitis, cholelithiasis, to eliminate spasms of the gastrointestinal tract, brain, to reduce the tone of the uterus, dilate blood vessels, and reduce peristalsis in the intestines.
3. “Spakovin” is an antispasmodic with myotropic effectiveness, similar in properties to papaverine, but superior to it in effectiveness and duration of action. Reduces the tone of internal organs, their motor activity and has a vasodilating effect.

Other analogues of the drug “No-shpa” are:

• "Drotaverine hydrochloride";
• "Papaverine";
• "Drotaverine Forte";
• "Spazgan";
• "Kuplaton";
• "Niaspam";
• "Spazmolysin";
• "Disflatil";
• "Kidakol";
• "No-h-sha";
• "Spasmomen."

Price

The cost of this medication in the form of ampoules No. 5 ranges from 70 to 190 rubles per package, in the form of ampoules No. 25 - up to 320 rubles. It depends on the region and pharmacy chain.

Transparent liquid of yellow-green color.

Pharmacotherapeutic group

Drugs for the treatment of functional disorders gastrointestinal tract. Papaverine and its derivatives.

ATX code: A03AD02.

Pharmacological properties

Pharmacodynamics

Mechanism of action

Drotaverine is an isoquinoline derivative that exhibits an antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase IV (PDE IV). Inhibition of the PDE IV enzyme results in increased concentrations of cAMP, which inactivates myosin light chain kinase and leads to smooth muscle relaxation.

Drotaverine inhibits PDE IV in vitro without inhibiting PDE III and PDE V isoenzymes. To reduce smooth muscle contractility, PDE IV is functionally very important, and its selective PDE IV inhibitors may be useful in the treatment of hyperkinetic diseases and various symptoms caused by spastic conditions of the gastrointestinal tract.

Drotaverine has no side effects on cardiovascular system, because the smooth muscle cells of the myocardium and blood vessels mainly contain the PDE III isoenzyme.

The PDE III isoenzyme hydrolyzes cAMP in myocardial and vascular smooth muscle and this explains the fact that drotaverine is an effective antispasmodic agent without serious cardiovascular side effects and strong cardiovascular therapeutic activity.

The drug is effective for spasms of smooth muscles of both nervous and muscular etiology. Regardless of the type of autonomic innervation, drotaverine acts on smooth muscles located in the gastrointestinal, biliary, urogenital and vascular systems.

Thanks to its vasodilating effect, it enhances tissue blood circulation. Its effect is stronger than that of papaverine, and absorption is faster and more complete; it binds less to plasma proteins. The advantage of drotaverine is that it does not have a stimulating effect on respiratory system observed after parenteral administration of papaverine.

Pharmacokinetics

Absorption

Drotaverine is quickly and completely absorbed, both after oral administration and after intramuscular administration.

Distribution

Drotaverine is highly bound to human plasma proteins (95-98%), especially albumin, gamma and beta globulins. Maximum plasma concentrations are achieved 45 to 60 minutes after oral administration.

Biotransformation and excretion

Drotaverine is metabolized in the liver, its half-life is 8-10 hours. After the first passage through the liver, 65% of the dose is unchanged in the circulation. Within 72 hours, drotaverine is almost completely eliminated from the body, more than 50% is excreted in the urine and about 30% in feces. Drotaverine is excreted mainly in the form of metabolites; the original compound is not detected in the urine.

Indications for use

Smooth muscle spasms associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis. spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus.

As an adjuvant treatment (if the patient cannot take pills):

With spasms of smooth muscles of gastrointestinal origin: peptic ulcer stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis in gynecology: dysmenorrhea.

Directions for use and dosage

Unless otherwise directed by the physician, the usual average dose for adults is 40 to 240 mg of drotaverine hydrochloride (divided into 1 to 3 doses per day) intramuscularly daily.

In acute colic (biliary and urolithiasis) 40-80 mg intravenously.

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Side effect

During clinical trials, the following side effects were reported by investigators as being associated with drotaverine and presented the following incidence rates: very common (> 1/10); common (> 1/100,< 1/10); нераспространённые (> 1/1000, < 1/100); редкие (> 1/10000, < 1/1000; очень редкие (< 1/10000) и классифицированные по следующим системам органов:

Gastrointestinal Disorders:

rarely: nausea, constipation

Disorders of the nervous system:

rarely: headache, dizziness, insomnia

Cardiovascular Disorders:

rare: palpitations, hypotension

Immune System Disorders:

rarely: allergic reaction (angioneurotic edema, urticaria, pruritus rash) ( see section "Contraindications"),

not known: fatal and non-fatal anaphylactic shock have been reported in patients using the injectable formulation.

General diseases and local reactions:

reactions at the injection site.

If side effects occur, you must stop taking the drug:

When the listed adverse reactions or a reaction not mentioned in the leaflet, consult a doctor!

Contraindications

Increased sensitivity to active substance or any of the excipients of the drug (especially sodium metabisulfite)). severe liver, kidney or heart failure (low cardiac output syndrome).

Overdose

An overdose of drotaverine can cause cardiac arrhythmia and conduction disturbances, including complete bundle branch block and cardiac arrest, which can be fatal.

In case of overdose, the patient should be monitored and receive symptomatic and supportive treatment.

Special instructions and precautions

Clinical studies on the use of the drug in children have not been conducted.

With low blood pressure, the use of the drug requires caution.

When administering drotaverine intravenously - due to the danger of loss of consciousness - the patient must lie down!

Sodium metabisulfite may cause allergic reactions, including anaphylactic symptoms and bronchospasm, especially in patients with asthma or allergies. In case of hypersensitivity to sodium metabisulfite, parenteral use of the drug should be avoided.

Caution should be exercised when taking the drug parenterally by pregnant women.

Pregnancy, breastfeeding and fertility

According to retrospective clinical studies and animal studies, oral administration of drotaverine during pregnancy does not have direct or indirect harmful effects on the course of pregnancy, embryonic development, childbirth and postnatal development. However, caution is required when prescribing the drug during pregnancy. Drotaverine should not be used during childbirth.

Due to the lack of necessary clinical data, it is not recommended to prescribe during breastfeeding.

Conditions for dispensing from pharmacies

No-spa is an antispasmodic drug, an isoquinoline derivative.

Release form and composition

No-shpa is available in the following forms:

• Tablets: yellow, with an orangish or greenish tint, biconvex, round, on one side with an engraving “spa” (6 or 24 pieces in PVC/Aluminum blisters, 1 blister in a cardboard pack; 20 pieces in Aluminum/blisters). Aluminum (laminated with polymer), 2 blisters in a cardboard pack; 60 pieces in polypropylene bottles with a polyethylene stopper equipped with a piece dispenser, 1 bottle in a cardboard pack; 100 pieces in polypropylene bottles, 1 bottle in a cardboard pack);
• Solution for intravenous and intramuscular administration: transparent, greenish-yellow (2 ml in dark glass ampoules with a broken point, 5 ampoules in blister plastic packages, 1 package in a cardboard box).

Active ingredient: drotaverine hydrochloride - 40 mg per 1 tablet; 20 mg in 1 ml solution.

Auxiliary components:

• Tablets: povidone, talc, corn starch, magnesium stearate, lactose monohydrate;
• Solution: ethanol 96%, sodium disulfite (sodium metabisulfite), distilled water.

Indications for use

• Spasms of smooth muscles of the urinary system: spasms of the bladder, pyelitis, nephrolithiasis, cystitis, urethrolithiasis; tenesmus of the bladder (in the form of injections);
• Smooth muscle spasms in diseases of the biliary tract: cholecystitis, cholangitis, cholecystolithiasis, pericholecystitis, cholangiolithiasis, papillitis.

As an auxiliary therapeutic agent, No-shpu is used for the following diseases and conditions:

• Tension headaches (by mouth);
• Spasms of smooth muscles of the gastrointestinal tract: gastritis, colitis, enteritis, spasms of the pylorus and cardia, peptic ulcer of the duodenum and stomach, spastic colitis with irritable bowel syndrome with flatulence and constipation after excluding diseases that manifest themselves as “ acute abdomen"(ulcer perforation, appendicitis, acute pancreatitis, peritonitis);
• Dysmenorrhea.

If it is impossible to use No-shpa tablets, the drug is administered parenterally.

Contraindications

• Severe renal and/or liver failure;
• Severe heart failure;
• Children's age (for solution, since there are no data from clinical studies in this age group);
• Children up to six years of age (for tablets);
• Lactation period (no clinical data);
• Glucose-galactose malabsorption syndrome, lactase enzyme deficiency, lactose intolerance (for tablets);
• Hypersensitivity to the main or auxiliary components of the drug.

No-shpa is used with caution in cases of arterial hypotension (since there is a danger of collapse), in children (for tablets) and pregnant women.

Directions for use and dosage

Pills

The drug in the form of tablets is taken orally. Recommended doses:

• Adults: 120-240 mg per day, divided into 2-3 doses. The maximum single dose - 80 mg, daily - 240 mg;
• Children over 12 years old: 160 mg per day, divided into 2-4 doses;
• Children 6-12 years: 80 mg per day, divided into 2 doses.

Without consulting a doctor, No-shpa is taken no more than 1-2 days. If there is no improvement during treatment, you should consult a doctor to clarify the diagnosis and change therapy if necessary. When using drotaverine as an adjuvant, the duration of treatment without medical advice can be 2-3 days.

Injection

The drug in the form of a solution is intended for parenteral administration. The average daily dose is 40-240 mg, divided into 1-3 injections, intramuscularly.

For acute renal and/or gallstone colic, 40-80 mg of drotaverine is administered intravenously.

During physiological labor, to shorten the dilatation phase of the cervix, the drug is administered intramuscularly at the beginning of the stretching period at a dose of 40 mg, and if the effect is unsatisfactory, the injection is repeated once within 2 hours.

Side effects

• Gastrointestinal tract: rarely - nausea, constipation;
• Cardiovascular system: rarely - decreased blood pressure, increased heart rate;
• Nervous system: rarely - dizziness, headache, insomnia;
• Immune system: rarely - allergic reactions (itching, rash, urticaria, angioedema); frequency unknown - anaphylactic shock (fatal and non-fatal);
• Local reactions: rarely - reactions at the injection site.

special instructions

Intravenous injections in patients with low blood pressure should be performed with the patient lying down due to the risk of collapse.

The drug in tablet form (when taken in recommended doses) does not affect the ability to drive vehicles or operate other potentially dangerous mechanisms. After administering No-shpa parenterally, it is advisable to refrain from activities that require increased concentration and speed of mental reactions.

Drug interactions

Drotaverine weakens the antiparkinsonian effect of levodopa; when administered simultaneously, tremor and rigidity may increase.

When used with other antispasmodics (including m-anticholinergics), the antispasmodic effect is mutually enhanced.

Drotaverine for intramuscular and intravenous administration reduces the spasmogenic activity of morphine, and also increases arterial hypotension caused by procainamide, quinidine and tricyclic antidepressants.

Phenobarbital increases the antispasmodic effect of No-shpa.

Drotaverine binds to plasma proteins (mainly β- and γ-globulins and albumin), but there is no data on the interaction of No-shpa with other drugs that significantly bind to plasma proteins. However, this effect should be taken into account when used simultaneously with such drugs due to the risk of toxic and/or pharmacodynamic side effects.

Terms and conditions of storage

Store in a place protected from light at a temperature of 15-25 °C (tablets in polypropylene bottles and solution for injection), no more than 25 °C (tablets in PVC/Aluminium blisters), no more than 30 °C (tablets in Aluminum/Aluminum blisters ). Keep away from children.

The shelf life of tablets in PVC/Aluminum blister packs is 3 years; in Aluminum/Aluminium blisters, in polypropylene bottles and in the form of an injection solution - 5 years.

pharmachologic effect

Myotropic antispasmodic.
Reduces the tone of the smooth muscles of internal organs, reduces their motor activity, and moderately dilates blood vessels.
It is superior to papaverine in terms of severity and duration of antispasmodic action. Does not affect the autonomic nervous system and central nervous system.
Due to the fact that No-shpa acts directly on smooth muscles, it can be used as an antispasmodic in cases where contraindications medicines from the group of anticholinergics (glaucoma, prostatic hypertrophy).
When administered intravenously, the effect of the drug appears within 2-4 minutes. The maximum effect develops after 30 minutes.

Pharmacokinetics

Suction
When taken orally, drotaverine hydrochloride is quickly absorbed from the gastrointestinal tract, the half-absorption period is 12 minutes. Bioavailability is about 100%. Cmax in serum is reached after 45-60 minutes.
Distribution
Drotaverine hydrochloride does not penetrate the BBB.
Metabolism
Drotaverine hydrochloride is biotransformed in the liver.
Removal
After 72 hours, it is practically excreted from the body in the form of metabolites - 50% in urine and 30% in feces.

Indications

– prevention and treatment of functional conditions and pain syndrome caused by spasm of smooth muscles (including spasms of the gastrointestinal tract, urinary tract associated with cholelithiasis, cholecystitis, gastric ulcer, duodenal ulcer; spasm of the pyloric and cardiac part of the stomach; spastic constipation, spastic colitis; proctitis, tenesmus; postoperative colic due to gas retention; due to nephrolithiasis, pyelitis; due to instrumental interventions);
- algomenorrhea;
– to reduce the excitability of the uterus during pregnancy; with spasm of the uterine pharynx during childbirth, prolonged opening of the pharynx, postpartum contractions, threatened abortion;
– spasms of peripheral vessels (including with endarteritis);
– prevention of smooth muscle spasm during instrumental research methods.

Instructions for use / dosage

Inside, p / c and / in. SC or IM, adults: 40-240 mg in 1-3 doses per day; to relieve acute nephrolithiasis and/or gallstone colic: 40-80 mg IV, slowly;
other abdominal spastic pain: 40-80 mg IM or SC, if necessary, up to 3 times a day (no more), followed by switching to oral administration of 120-240 mg;
spasm of the cardia or esophagus: 80 mg IM.

Orally, adults: 120-240 mg in 2-3 divided doses. Children: from 1 to 6 years old - 40-120 mg in 2-3 divided doses, over 6 years old - 80-200 mg in 2-5 divided doses.

Side effect

Maybe: dizziness, palpitations, feeling hot, increased sweating.
At intravenous introduction There have been cases of a decrease in blood pressure (up to collapse), the development of AV blockade, the appearance of arrhythmias, and depression of the respiratory center.

Contraindications

– hypersensitivity to the drug.

Pregnancy and lactation

Use the drug No-shpa with caution during pregnancy and lactation (breastfeeding).

special instructions

Caution should be exercised when prescribing the drug to patients with severe atherosclerosis of the coronary arteries.
No-spa can be used as part of combination therapy to relieve a hypertensive crisis.
In the treatment of gastric and duodenal ulcers, No-shpu is used in combination with anticholinergics.

Overdose

To date, no cases of overdose of the drug No-shpa have been reported.

Drug interactions

With simultaneous use, No-shpa can reduce the antiparkinsonian effect of levodopa.

Storage conditions and periods

The drug should be stored in a place protected from light, in tightly closed packaging at a temperature of 15° to 25°C. Shelf life - 5 years.

In this article you can read the instructions for use of the drug No-shpa. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of No-shpa in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of No-shpa in the presence of existing structural analogues. Use for the treatment and relief of spasmodic pain in adults, children, as well as during pregnancy and breastfeeding.

No-shpa- myotropic antispasmodic, isoquinoline derivative. It has a powerful antispasmodic effect on smooth muscles due to inhibition of the PDE enzyme. The enzyme PDE is necessary for the hydrolysis of cAMP to AMP. Inhibition of PDE leads to an increase in cAMP concentration, which triggers the following cascade reaction: high concentrations of cAMP activate cAMP-dependent phosphorylation of myosin light chain kinase (MLCK). Phosphorylation of MLCK leads to a decrease in its affinity for the Ca2+-calmodulin complex, as a result of which the inactivated form of MLCK maintains muscle relaxation. In addition, cAMP affects the cytosolic concentration of Ca2+ ion by stimulating the transport of Ca2+ into the extracellular space and the sarcoplasmic reticulum. This lowering the concentration of Ca2+ ion effect of drotaverine (the active ingredient of the drug No-shpa) through cAMP explains the antagonistic effect of drotaverine in relation to Ca2+.

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

The hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the PDE3 isoenzyme, which explains the fact that with high antispasmodic activity, No-shpa has no serious side effects on the heart and blood vessels and no pronounced effects on the cardiovascular system .

Drotaverine is effective against smooth muscle spasms of both neurogenic and muscular origin. Regardless of the type of autonomic innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, and genitourinary system.

Pharmacokinetics

After oral administration, No-Spa is quickly and completely absorbed. After first-pass metabolism, 65% of the administered dose of drotaverine enters the systemic circulation. Drotaverine is evenly distributed in tissues and penetrates smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and/or its metabolites are able to slightly penetrate the placental barrier. Within 72 hours, drotaverine is almost completely eliminated from the body. More than 50% of drotaverine is excreted by the kidneys and about 30% through the intestines (excretion into bile). Drotaverine is mainly excreted in the form of metabolites; unchanged drotaverine is not found in the urine.

Indications

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

As an adjuvant therapy:

• for spasms of smooth muscles of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence after excluding diseases manifested by the “acute abdomen” syndrome (appendicitis, peritonitis, perforation ulcers, acute pancreatitis);
• tension headaches (for oral administration);
• algodismenorrhea.

Release forms

Tablets 40 mg.

Tablets No-shpa forte 80 mg.

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

Instructions for use and dosage

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

Clinical studies with the use of drotaverine have not been conducted in children.

When prescribing the drug No-shpa, the maximum daily dose when taken orally for children aged 6 to 12 years is 80 mg in 2 divided doses, for those over 12 years old - 160 mg in 2-4 divided 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 pain syndrome does not decrease, the patient should consult a doctor to clarify the diagnosis and, if necessary, change therapy. In cases where NO-spa is used as an auxiliary therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).

Performance Evaluation Method

If the patient can easily independently 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 assessed by the patient. If within a few hours after taking the drug at the maximum single dose there is a moderate decrease in pain or no decrease in pain, or if the pain does not decrease significantly after taking the maximum daily dose, it is recommended to consult a doctor.

Side effect

• cardiopalmus;
• decrease in blood pressure;
• headache;
• dizziness;
• insomnia;
• nausea;
• constipation;
• rash;
• hives;
• angioedema;
• reactions at the injection site.

Contraindications

• severe renal failure;
• severe liver failure;
• severe heart failure (low cardiac output syndrome);
• children under 6 years of age (for tablets);
• children's age (for parenteral administration, since clinical studies have not been conducted in children);
• breastfeeding period (no clinical data);
• rare hereditary galactose intolerance, 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 intravenous and intramuscular administration).

Use during pregnancy and breastfeeding

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

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

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

special instructions

The tablets contain 52 mg of lactose, which may result in complaints from digestive system in patients with lactose intolerance. Therefore, the drug in tablet form is not prescribed to patients with lactase deficiency, galactosemia or impaired glucose/galactose absorption syndrome.

The solution for intravenous and intramuscular administration contains sodium bisulfite, which can cause allergic reactions, including anaphylactic and bronchospasm, in sensitive persons (especially in persons with bronchial asthma or allergic reactions in the anamnesis). In case of hypersensitivity to sodium metabisulfite, parenteral use of the drug should be avoided.

When administering the drug intravenously to patients with low blood pressure, the patient should be in horizontal position due to the risk of collapse.

Impact on the ability to drive vehicles and operate machinery

When taken orally in therapeutic doses, drotaverine does not affect the ability to drive vehicles or perform work that requires increased concentration.

If any adverse reactions occur, the issue of driving and operating machinery requires individual consideration. If dizziness occurs after taking the drug, you should avoid engaging in potentially hazardous activities such as driving vehicles and work with mechanisms.

After parenteral administration of the drug, it is recommended to refrain from driving vehicles and engaging in other potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Drug interactions

PDE inhibitors like papaverine reduce the antiparkinsonian effect of levodopa. When No-shpa is prescribed simultaneously with levodopa, rigidity and tremor may increase.

When used simultaneously with drotaverine, the antispasmodic effect of papaverine, bendazole and other antispasmodics, including m-anticholinergics, is mutually enhanced.

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

No-shpa reduces the spasmodic activity of morphine.

Phenobarbital enhances the antispasmodic effect of drotaverine.

Drotaverine binds significantly to plasma proteins, mainly albumin, beta and gamma globulins. There are no data on the interaction of drotaverine with drugs that are significantly bound to plasma proteins. 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 by the other from the binding sites and an increase in the concentration of the free fraction in the blood of the drug with weaker binding to proteins. This could hypothetically increase the risk of pharmacodynamic and/or toxic side effects of this drug.

Analogues of the drug No-shpa

Structural analogues of the active substance:

• Vero-Drotaverine;
• Droverin;
• Drotaverine;
• Drotaverine forte;
• Drotaverine hydrochloride;
• NOSH-BRA;
• Ple-Spa;
• Spasmol;
• Spasmonet;
• Spasmonet forte;
• Spazoverine;
• Spakovin.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.