But spa or similar. What is better Drotaverine or No-shpa - comparison of drugs. Instructions for use

The well-known drug “No-shpa” is used when spasms of the smooth muscles of the urinary tract, gastrointestinal tract, internal female genital organs, and brain occur. The range of applications for No-shpa is quite wide, which is why the drug is so popular. “No-shpa” helps due to what it contains. This is what has an antispasmodic effect. The drug is sold both as a solution for intramuscular and intravenous administration. In order to purchase No-shpu, you do not need a prescription.

On average, the price of No-shpa ranges from 150 rubles for 20 tablets with a dosage of 40 mg to 250 rubles per pack of 100 tablets, with the same dosage.

Not suitable for everyone

If the dose is exceeded or if side effects from No-shpa occur, colic may appear, headache, insomnia, constipation.

Instead of "No-shpa"

More expensive analogues of “No-shpa” are “Ple-Spa”, “Spazoverin”, “Spazmonet”, “Spakovin”. Difference expensive analogues from cheap ones in that almost all of them are made at modern equipment foreign manufacturers, so if you doubt the quality of drugs produced by domestic factories, opt for more expensive drugs.

Most cheap analogue“No-shpy”, the cost of which is several times less - “Drotaverine”, it is produced by a domestic manufacturer and contains the same substances. Its main advantage is price.

Other antispasmodics that are not analogues of No-shpa, but also relieve pain, are Spazgan, Bral, Pentalgin, Analgin. They are sold in packs of 10 tablets and have affordable price up to 100 rubles. Buscopan and Galidor are considered expensive antispasmodics, the price of which exceeds 350 rubles for 20 tablets.

“No-spa” is a drug that can relieve pain of various origins. You can purchase this drug or replace it with analogues, the choice is up to you. Be careful not to exceed the dose and be sure to read the instructions.

The basis of this drug is drotaverine, an active substance that helps to effectively relieve spasms and relax the smooth muscles of various organs. In Russian pharmacies, No-shpu can be found in the form of tablets and ampoules. As a rule, these are French-made products.

The description of the medicine states that it is intended to relieve pain in the following cases:

• ailments of the biliary tract (cholecystolithiasis, cholecystitis, etc.);
• pathologies of the urinary system (cystitis, nephrolithiasis, etc.);
• in the form of ampoules - also to reduce the phase of cervical dilation and shorten the duration of labor.

No-shpu is used as an additional medicine:

• to relieve spasms in the gastrointestinal tract (ulcers, gastritis, colitis, enteritis, etc.);
• for the purpose of treating a headache that a person characterizes as “a hoop or belt around the head”;
• with dysmenorrhea - painful sensations during menstruation;
• if we are talking about injections, they are also administered during strong contractions during childbirth.

One tablet or 2 ml ampoule contains 40 mg of drotaverine. Recommended dosages of No-shpa:

1. Single dose for adults – no more than 2 tablets. You can take a maximum of 6 tablets per day in 3 doses.
2. The maximum dose for a child from 6 to 12 years old is 2 tablets per day, but not more than 1 piece. for 1 appointment.
3. Children over 12 years of age are allowed to take no more than 4 tablets, divided into 2-4 times, within 24 hours.
4. In the form of injections for adults - up to 240 mg per day, but not once, but in 2-3 doses.

Attention! There is also No-shpa Forte, which contains 2 times more drotaverine - 80 mg in 1 tablet. Accordingly, the manufacturer has provided other dosages for it.

Some instructions state that the medicine should not be taken by a child under 6 years of age, others - up to 1 year. In practice, doctors sometimes prescribe the drug to children, allowing them to drink half, 1/3 or 1/4 of the tablet at a time. And if about childhood There are disagreements among pharmacists, then it is absolutely impossible for people suffering from kidney, liver or heart failure to be treated with No-shpa. The drug is not prescribed to those who are lactose intolerant (it is available in tablets), as well as to nursing mothers.

If the product is not suitable for you, this will become clear from the side effects:

• decreased blood pressure (therefore, in case of hypotension, No-shpa should be taken with caution);
• headache, dizziness;
• constipation, nausea, vomiting;
• allergic reactions, etc.

If you take No-shpa on your own for 1-2 days, but do not feel any improvement, consult a doctor. If we are talking about using the drug as an additional therapy, you can delay your visit to the hospital for up to 3 days.

How to replace no-shpu. Reviews about the medicine and its analogues

No-shpa can be purchased in packages of 6, 20, 24, 60 or 100 tablets, in liquid form - in boxes containing 5 or 25 ampoules. When expressing their opinion about this drug, users emphasize:

• The medicine relieves spasms well in both adults and children (as prescribed by a pediatrician). A lot of positive feedback from those who suffer from stomach pain;
• No-spa, in comparison with analogues, is more gentle;
• helps maintain pregnancy if the cause of the threat is uterine hypertonicity;
• useful before going through some painful procedures– for example, colonoscopy;
• but taking it can be harmful for prostate adenoma.

The cost of 24 tablets of No-shpa is approximately 190 rubles, the larger the pack, the more profitable it is, of course, in terms of price. However, you can buy cheaper analogues of the drug in pharmacies:

1. Drotaverine. The most popular substitute for No-shpa. Available in the same dosage: 1 tablet - 40 mg of active substance. The cost of a package with 20 pcs. – from about 12 rub. There is also Drotaverine Forte. According to reviews, this drug is absolutely comparable to No-shpa, but has a pleasant bonus in the form of a low price. Therefore, many users note that they are switching to a cheaper analogue.


2. Spasmol. The composition is the same as No-shpa and Drotaverine. According to reviews, it replaces both medications well. Although there are opinions that Spasmol is more of an analogue of papaverine, and can also be harmful during menstruation. The average cost is about 30 rubles. for 20 tablets. True, in Lately The drug can be difficult to find in pharmacies.
3. Spasmonet. Price for 20 tablets is about 70 rubles. Considering that there are cheaper antispasmodics with drotaverine, this medicine may not be the most popular. However, those who have taken it note its high effectiveness for various painful sensations.

It is worth remembering that everything medicines have contraindications and side effects. There is also such a factor as individual intolerance. Therefore, if drugs with drotaverine are not suitable for you, look for another antispasmodic, remembering to consult with your therapist.

Characteristics of the original drug

The drug "No-Shpa" is available in two forms: solution for injection and tablets. The latter type is more popular. The medicine is an over-the-counter drug and is available in almost every pharmacy chain. It produces an antispasmodic effect without affecting the functioning of the nervous system.

Analogue of the drug "No-Shpa"

You should change the medicine if you have contraindications to its use. Patients with adverse reactions the medicine is changed to an alternative one, but with a different composition. Tablets and solution "No-Shpa" have structural and relative analogues. The latter include any painkillers: “Ibuprofen”, “Paracetamol”, “Analgin”, “Nimesil”, “Ketorol”. Such medications should be chosen together with your doctor. Closer in action will be “Papaverine” and “Papazol”.

Absolute structural substitutes for the drug “No-Shpa” include the following analogues: “Drotaverine”, “Spazmonet”, “Spazmol”, “NOSH-BRA”, “Spazoverine” and so on. Let's look at some of them and find out if there is a significant difference between the drugs.

Inexpensive product "Drotaverine"

This drug contains the same active ingredient as the expensive foreign medicine. Tablets and injections "No-Shpa" have a Russian analogue - "Drotaverin". Its cost is approximately 30 rubles for 20 pills. This is much cheaper than the originally announced medicine. According to the instructions for use, “Drotaverine” is prescribed to women in labor during labor to relieve cervical spasms. The drug is used for flatulence. It has much more indications for use than No-Shpa tablets and injections. Analogue with trade name"Drotaverine" is not used for children under 12 years of age. This is an important difference from an expensive substitute.

Little-known "Spazmol"

The next substitute for the drug “No-Shpa” (analogue) is the Russian “Spazmol”. The composition still contains the same drotaverine. Indications for use: treatment and prevention of smooth muscle spasms, cervical spasm during childbirth, painful menstruation, spasms of cerebral vessels. You should not take this medicine in the same situations as the No-Shpa drug. Some sources indicate that this medication is prohibited for use by pregnant and lactating women. But these data are called into question.

"Spasmonet" will eliminate pain

Another analogue of the drug “No-Shpa” with the same active ingredient is “Spazmonet” tablets. Their name speaks for itself. The medicine is used for spasms of smooth muscles of the digestive tract, constipation, stomach ulcers, arterial spasms, and uterine hypertonicity during pregnancy. The manufacturer names low blood pressure and prostatic hyperplasia as additional contraindications to treatment. Children under 6 years of age should not use the drug without medical advice.

What kind of feedback can you hear?

Of all the medicines presented, No-Shpa is the most popular. This medication is prescribed to expectant mothers without much fear. The use of "Drotaverine" among expectant mothers is also practiced. Clinical studies have shown the safety and effectiveness of these medications. While the effect of other analogues is questioned. Consumer reviews of medications vary. Some people praise the drugs, while others criticize them. Everything here is very individual. If pain syndrome is caused by a spasm, then any of the listed remedies will help you. If discomfort is caused by other reasons, all drugs may be powerless.

Buyers are often indignant because of the high cost of No-Shpa tablets. They prefer to choose cheaper analogues. If in alternative means contains the same active ingredient as the prescribed medicine, then you may well give it preference. Mandatory medical consultation is required in situations where No-Shpa is replaced in pregnant and lactating women, persons with chronic diseases and small children.

Conclusion

The article introduced you to the well-known myotropic antispasmodic called “No-Shpa”. Instructions for use, price, analogues of tablets are described for you. Many consumers are trying to find a cheap substitute for an expensive drug. It is worth approaching this issue with full responsibility. It is better to visit the doctor several times to make sure that the chosen medicine is safe, rather than worry about possible unpleasant consequences. Before using any of the described products, read the instructions.

A sharp contraction of one muscle or group is a phenomenon called spasm. Some people mean by this condition only frequent cramps of the limbs, but such a contraction can affect absolutely all muscle groups in the human body and manifest themselves in different ways. The main manifestation of the condition is pain, often of a pulsating nature. The sensations can be very strong, and in order to cope with them you have to resort to special medications - antispasmodics, which help relax the created tension. Patients usually choose proven remedies, which can safely include No-shpu and Drotaverine. Let's find out if there is a difference between these products and how to take them correctly.

Is there a difference in the composition of Drotaverine and No-shpa

Drotaverine hydrochloride is a substance that has an antispasmodic, lowers blood pressure, increases blood flow to important bodies action. This component is active substance both as part of the drug No-shpa and among the ingredients of Drotaverine. It is worth noting that the dosage is no different - 40 mg in each tablet. The products under consideration differ only in some items from the list of auxiliary components:

• Drotaverine tablets contain lactose, povidone, magnesium stearate, crospovidone, potato starch and talc;
• Additional ingredients of No-shpa include magnesium stearate, povidone, talc, corn starch and lactose.

After considering the composition of the tablets, it becomes obvious that there is no difference in their effect on the body, the difference lies only in the cost of the product.

The principle of action of antispasmodics

The active component of the drugs under consideration has antispasmodic activity in relation to the smooth muscles of the digestive, urogenital and biliary systems, as well as in relation to the corresponding layer of blood vessels. The substance relaxes the muscles, due to which existing spastic pains disappear, the lumen of blood vessels expands (pressure decreases). This effect is possible due to the ability of drotaverine to change the cell membrane potential and their permeability.

When the substance enters the body, it has a noticeable effect after 12 minutes, as it is quickly and completely absorbed from the digestive tract. The active component distributes evenly, penetrating smooth muscle cells. Drotaverine hydrochloride has no effect on the central or autonomic nervous system. Excretion occurs in approximately 24 hours in the urine.

Indications for use of tablets

Tablets are used to relieve spasms and, accordingly, eliminate the pain that was provoked by them. It will be relevant to use for the following diagnoses:

1. cholecystitis;
2. cholelithiasis;
3. ulcerative lesions of the gastric and intestinal mucosa;
4. colitis;
5. intestinal colic due to retention or excessive production of gases;
6. cystitis;
7. pyelitis;
8. with spasms of cerebral vessels;
9. The product is also used in gynecological practice as a drug to relieve uterine spasms in the presence of a threat of miscarriage.

It is worth understanding that No-Spa cannot eliminate the source of the problem itself, and therefore is used as a method of temporary symptomatic treatment. The administration of drotaverine may be necessary both for medicinal purposes and to prepare the body for a certain kind of diagnostic tests.

Instructions for use of Drotaverine and No-shpa

The dosage of drugs depends on the age of the patient:

• an adult can take a maximum of 2 tablets at a time, the maximum amount per day is 3-4 pieces;
• Children aged 6 to 12 years can be given the substance a maximum of two times a day, one tablet;
• Children over 12 years of age impose a limitation in the form of a maximum of one tablet per day, used in several doses.

You should simply take the tablets with a small amount of water.

Contraindications for use

You should not take drugs based on drotaverine, first of all, if you have an individual intolerance to this component or at least one of the auxiliary ones. Contraindications also include:

• renal or liver failure;
• age up to 6 years;
• severe heart failure;
• Due to the lack of relevant research, you should not use the product while breastfeeding.

The use of drotaverine for low blood pressure and during pregnancy is not prohibited, however, such conditions require special caution.

The tablets are usually very well tolerated human body, however, during clinical studies, possible side effects in isolated cases that may occur when using drugs, namely increased heart rate, dizziness and headaches, feelings of heat, sleep disturbances, nausea, etc. To eliminate them, you must urgently stop taking the pills and begin symptomatic treatment of the situation.

Which is better - Drotaverine or No-shpa?

It is simply impossible to say which of the drugs under consideration is better, since they have the same active composition and, accordingly, the nature of the effect on the human body. In fact, No-shpa is the same Drotaverine, only under a different name; they differ only in cost in pharmacies.

What is best to take during pregnancy?

Studies have shown that No-shpa and Drotaverine do not cause harm to either the child’s or the mother’s body. However, the use of drugs is possible only after a doctor’s prescription, since during pregnancy weighing is carried out all the time possible harm for the fetus and benefit for the mother.

Instructions for use. Contraindications and release form.

INSTRUCTIONS
for use of the drug
NO-SHPA

Compound
Solution for intravenous and intramuscular injection 1 amp. (2 ml)
active substance:
drotaverine hydrochloride 40 mg
excipients: sodium disulfite (sodium metabisulfite) - 2 mg, ethanol 96% - 132 mg, water for injection - up to 2 ml

Tablets 1 tablet.
active substance:
drotaverine hydrochloride 40 mg
excipients: magnesium stearate - 3 mg; talc - 4 mg; povidone - 6 mg; corn starch - 35 mg; lactose monohydrate - 52 mg

pharmachologic effect
antispasmodic.

Indications of the drug No-shpa®

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

As adjuvant therapy(if oral therapy is not possible):

• spasms of smooth muscles of the gastrointestinal tract: peptic ulcer stomach and duodenum, gastritis, spasms of the cardia and pylorus, enteritis, colitis;
• gynecological diseases: dysmenorrhea.

40 mg tablets:

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

As an adjuvant therapy:

• 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 syndrome acute abdomen(appendicitis, peritonitis, ulcer perforation, acute pancreatitis);
• tension headaches;
• dysmenorrhea.

Contraindications
Solution for intravenous and intramuscular administration:

• hypersensitivity to sodium disulfite (see section " special instructions»);
• severe chronic heart failure;
• childhood (the use of drotaverine in children has not been studied in clinical studies);
• breastfeeding period (no clinical studies available).

Carefully: arterial hypotension(danger of collapse, see “Special Instructions”); pregnancy (see “Use during pregnancy and lactation”).

Pills:

• hypersensitivity to the active substance or any of excipients drug;
• severe liver or kidney failure;
• severe heart failure (low cardiac output syndrome);
• children under 6 years of age;
• breastfeeding period (no clinical studies);
• rare hereditary galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the drug).

With caution: arterial hypotension; pediatric patients (lack of clinical experience applications); pregnancy (see “Use during pregnancy and lactation”).

Use during pregnancy and breastfeeding
As shown by reproductive studies in animals and retrospective studies of clinical data, the use of drotaverine during pregnancy had neither teratogenic nor embryotoxic effects. Despite this, when using the drug in pregnant women, caution should be exercised and the drug should be prescribed only after carefully weighing the benefit-risk ratio.
Due to the lack of necessary clinical data, it is not recommended to prescribe during lactation.

Side effects
Below are the adverse reactions observed in clinical studies, divided by organ system, indicating the frequency of their occurrence in accordance with the following gradation: very often (≥10%), often (≥1.<10%); нечасто (≥0,1, <1%); редко (≥0,01, <0,1%); очень редко, включая отдельные сообщения (<0,01%); неизвестная частота (по имеющимся данным частоту определить нельзя).
From the cardiovascular system: rarely - rapid heartbeat, decreased blood pressure.
From the side of the central nervous system: rarely - headache, dizziness, insomnia.
From the gastrointestinal tract: rarely - nausea, constipation.
From the immune system: rarely - allergic reactions (angioedema, urticaria, rash, itching) (see section "Contraindications").
Local reactions (solution for intravenous and intramuscular administration): rarely - reactions at the injection site.

Interaction
Solution for intravenous and intramuscular administration
Levodopa. PDE inhibitors like papaverine reduce the antiparkinsonian effect of levodopa. When prescribing drotaverine simultaneously with levodopa, increased rigidity and tremor may occur.
Papaverine, bendazole and other antispasmodics (including m-anticholinergics). Drotaverine enhances the antispasmodic effect of papaverine, bendazole and other antispasmodics, including m-anticholinergics.
Tricyclic antidepressants, quinidine and procainamide. Increases hypotension caused by tricyclic antidepressants, quinidine and procainamide.
Morphine. Reduces the spasmogenic activity of morphine.
Phenobarbital. Strengthening the antispasmodic effect of drotaverine.
Pills
Levodopa. PDE inhibitors like papaverine reduce the antiparkinsonian effect of levodopa. When prescribing drotaverine simultaneously with levodopa, increased rigidity and tremor may occur.
Other antispasmodics, including m-anticholinergics. Mutual enhancement of antispasmodic action.
Drugs that are significantly bound to plasma proteins (more than 80%). Drotaverine binds significantly to plasma proteins, mainly albumin, γ- and β-globulins (see “Pharmacokinetics”). There is no data on the interaction of drotaverine with drugs that significantly bind to plasma proteins, however, there is a hypothetical possibility of their interaction with drotaverine at the level of binding to protein (displacement of one of the drugs by another from binding to the protein and an increase in the concentration of the free fraction in the blood of the drug with a less strong binding to protein), which could hypothetically increase the risk of pharmacodynamic and/or toxic side effects of this drug.

Directions for use and doses
Solution for injection: IM, IV, slowly. Adults: the average daily dose is 40–240 mg, divided into 1–3 intramuscular injections. For acute renal and gallstone colic - 40–80 mg IV, slowly (duration of administration is about 30 s).
Tablets: orally.
Adults. Typically, the average daily dose in adults is 120–240 mg (the daily dose is divided into 2–3 doses). The maximum single dose is 80 mg. The maximum daily dose is 240 mg.
Children. Clinical studies using drotaverine have not been conducted in children.
In case of prescribing drotaverine to children:
- for children 6–12 years old, the maximum daily dose is 80 mg, divided into 2 doses.
- for children over 12 years of age, the maximum daily dose is 160 mg, divided into 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 pain does not decrease during this period, the patient should consult a doctor to clarify the diagnosis and, if necessary, change therapy. In cases where drotaverine is used as an adjuvant therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).
Method for assessing effectiveness. 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 maximum single dose there is a moderate reduction in pain or no reduction in pain, or if the pain does not significantly decrease after taking the maximum daily dose, it is recommended to consult a doctor.

Overdose
There are no data on drug overdose.
Treatment: In case of overdose, patients should be under medical supervision and, if necessary, treated symptomatically and aimed at maintaining basic body functions (including induction of vomiting or gastric lavage).

special instructions
Injection
Contains sodium disulfite, which may cause allergic-type reactions including anaphylactic symptoms and bronchospasm in sensitive individuals, especially those with a history of asthma or allergic diseases. In case of hypersensitivity to sodium disulfite, parenteral use of the drug should be avoided (see “Contraindications”). When administering drotaverine intravenously in patients with low blood pressure, the patient should be in a horizontal position due to the risk of collapse.
Impact on the ability to drive a car or perform work that requires increased speed of physical and mental reactions.
During the treatment period, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Pills
Contains 52 mg of lactose in each tablet. This may cause gastrointestinal disturbances in patients suffering from lactose intolerance. The tablets are not suitable for patients suffering from lactose deficiency, galactosemia or impaired glucose/galactose absorption syndrome (see “Contraindications”).
Impact on the ability to drive a car or perform work that requires increased speed of physical and mental reactions
When taken orally in therapeutic doses, drotaverine does not affect the ability to drive a car or perform work that requires increased attention. If any side effects 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.

Conditions for dispensing from pharmacies
Solution for intramuscular and intravenous administration. On prescription.
Pills. Over the counter.

Storage conditions for No-shpa®
At temperatures below 30 °C.
Keep out of the reach of children.

Shelf life of the drug No-shpa®
5 years.

pharmachologic effect

Antispasmodic agent, 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 Ca 2+ -calmodulin complex, as a result of which the inactivated form of MLCK maintains muscle relaxation. In addition, cAMP affects the cytosolic concentration of Ca 2+ ion by stimulating the transport of Ca 2+ into the extracellular space and the sarcoplasmic reticulum. This lowering Ca 2+ ion concentration effect of drotaverine through cAMP explains the antagonistic effect of drotaverine in relation to Ca 2+.

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 suppressing the contractile activity of smooth muscles, 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, drotaverine 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

Suction

After oral administration, drotaverine is quickly and completely absorbed. After first-pass metabolism, 65% of the administered dose of drotaverine enters the systemic circulation. Cmax in blood plasma is reached in 45-60 minutes.

Distribution

In vitro, drotaverine is highly bound to plasma proteins (95-98%), especially albumin, β- and γ-globulins.

Drotaverine is evenly distributed in tissues and penetrates smooth muscle cells. Does not penetrate the BBB. Drotaverine and/or its metabolites are able to slightly penetrate the placental barrier.

Metabolism

In humans, drotaverine is almost completely metabolized in the liver by O-desethylation. Its metabolites quickly conjugate with glucuronic acid. The main metabolite is 4"-desethyldrotaverine, in addition to which 6-desethyldrotaverine and 4"-desethyldrotaveraldine have been identified.

Removal

In humans, a two-chamber mathematical model was used to assess the pharmacokinetics of drotaverine. The final T1/2 of plasma radioactivity was 16 hours.

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; bladder tenesmus (parenteral).

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, ulcer perforation, acute pancreatitis);

- tension headaches (for oral administration);

- dysmenorrhea.

When used as an adjuvant, the drug is administered parenterally if it is not possible to use tablets.

Dosage regimen

Clinical studies using drotaverine involving children was not carried out.

If the drug No-shpa ® is prescribed, the maximum daily dose when taken orally for children inages 6 to 12 years is 80 mg (divided into 2 doses), for childrenover 12 years of age- 160 mg (divided into 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 pain does not decrease during this period, the patient should consult a doctor to clarify the diagnosis and, if necessary, change therapy. In cases where drotaverine is used as an adjuvant 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.

When using a bottle with a polyethylene stopper equipped with a piece dispenser: Before use, remove the protective strip from the top of the bottle and the sticker from the bottom of the bottle. Place the bottle in your palm so that the dispensing hole on the bottom does not rest against your palm. Then press on the top of the bottle, causing one tablet to fall out of the dispensing hole at the bottom.

Side effect

Below are the adverse reactions observed in clinical studies, divided by organ system, indicating the frequency of their occurrence in accordance with the following gradations: very common (≥10%), common (≥1%,<10), нечастые (≥0.1%, <1%), редкие (≥0.01%, <0.1%), очень редкие, включая отдельные сообщения (<0.01%), частота неизвестная (по имеющимся данным частоту определить нельзя).

From the cardiovascular system: rare – increased heart rate, decreased blood pressure.

From the nervous system: rare – headache, dizziness, insomnia.

From the gastrointestinal tract: rare – nausea, constipation.

From the immune system: rare - allergic reactions (angioedema, urticaria, itching, rash); frequency unknown - fatal and non-fatal anaphylactic shock has been reported.

Local reactions: rare - reactions at the injection site.

Contraindications for use

- 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).

WITH caution the drug is used for arterial hypotension (due to the risk of collapse), during pregnancy; in children (for tablets).

Use during pregnancy and breastfeeding

As studies of reproduction in animals and retrospective data on the clinical use of drotaverine have shown, the use of drotaverine during pregnancy had neither teratogenic nor embryotoxic effects. Despite this, when prescribing drotaverine to pregnant women, caution should be exercised and it should be used only in cases where the potential benefit to the mother outweighs the potential risk to the fetus, while prescribing the injectable dosage form of the drug No-shpa ® in pregnant women should be avoided.

The drug should not be used during childbirth (potential risk of developing postpartum atonic hemorrhage).

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

Use in children

Parenteral use in children is contraindicated.

Taking the drug orally is contraindicated for children under 6 years of age.

Overdose

Drotaverine overdose has been associated with cardiac rhythm and conduction disturbances, including complete bundle branch block and cardiac arrest, which can be fatal.

Treatment: in case of overdose, patients should be under medical supervision. If necessary, symptomatic treatment aimed at maintaining basic body functions should be carried out, including artificial induction of vomiting or gastric lavage.

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.

With the simultaneous use of drotaverine with other antispasmodics, including m-anticholinergics, a mutual enhancement of the antispasmodic effect occurs.

Drotaverine for IM and IV administration increases arterial hypotension caused by tricyclic antidepressants, quinidine and procainamide.

Drotaverine for IM and IV administration reduces the spasmogenic activity of morphine.

Phenobarbital enhances the antispasmodic effect of drotaverine.

Drotaverine binds significantly to plasma proteins, mainly albumin, β- and γ-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 drotaverine at the level of binding to plasma proteins - the 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.

Conditions for dispensing from pharmacies

The drug in tablet form is approved for use as an over-the-counter product.

The drug in the form of a solution for intravenous and intramuscular administration is available with a prescription.

Storage conditions and periods

Tablets in PVC/Aluminum blisters should be stored at a temperature not exceeding 25°C. Shelf life - 3 years.

Tablets in Aluminum/Aluminium blisters should be stored at a temperature not exceeding 30°C. Shelf life - 5 years.

Tablets in polypropylene bottles and solution for intravenous and intramuscular administration should be stored in a place protected from light at a temperature of 15° to 25°C. Shelf life - 5 years.

The drug should be stored out of the reach of children.

Use for liver dysfunction

Use is contraindicated in severe liver failure.

Use for renal impairment

Use is contraindicated in severe renal failure.

special instructions

The 40 mg tablets contain 52 mg of lactose, as a result of which complaints from the digestive system are possible in patients with lactose intolerance. This form is not intended for 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 individuals (especially in individuals with bronchial asthma or a history of allergic reactions). 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 a 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 working with machinery.

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.