No-shpa and diuretic effect. No-shpa tablets, a fast-acting colic remedy

Medicine no-shpa (INN - drotaverine) belongs to the group of antispasmodics. The ability to suppress the activity of the enzyme phosphodiesterase (PDE), which is necessary for the hydrolysis of cAMP to AMP, gives no-shpu a strong antispasmodic effect on smooth muscles. The exclusion of PDE from the cycle of biochemical transformations leads to an increase in the concentration of cAMP, which automatically triggers a whole cascade of reactions, as a result of which the desired muscle relaxation is potentiated. No-shpa is a world famous brand produced by the Hungarian pharmaceutical plant "Hinoin" since the beginning of the 60s of the last century. Almost immediately, the new super-effective antispasmodic gained worldwide recognition, the strength of which has not decreased one iota at the present time. In Russia, this drug was first registered in 1963, and immediately won the hearts (or rather, excessively toned smooth muscles) of hundreds of thousands of patients and their physicians. Dozens of years of application of no-shpy testify to high efficiency and sufficient security this drug. According to statistics, no-shpa is the most commonly prescribed antispasmodic, the volume of which is growing every year.

Due to the selectivity of its action, no-shpa does not affect cardiovascular system, aiming "attacking" only the spasmodic muscles of the biliary tract, digestive and genitourinary tract.

No-shpa is available in two dosage forms: tablets and solution for intravenous and intramuscular injection. The composition of the tablet form may include 40 or 80 mg of drotaverine (in the latter case, the word "forte" is added to the name of the drug). By general recommendations the daily dose of the drug is from 120 to 240 mg (with a maximum single dose of 80 mg), the frequency of administration is 2-3 times a day. Regarding the reception of no-shpa by patients childhood, then for them the daily dose should be 80 mg in 2 doses (children from 6 to 12 years old) or 160 mg in 2-4 doses (children from 12 years old). The duration of taking the drug without medical supervision should not exceed 1-2 days. If after this period the pain does not subside, then it is necessary to without fail consult a doctor for diagnosis and correction drug therapy. If no-shpa is used as ancillary treatment, then the duration of pharmacotherapy without consulting a specialist may be longer (up to 3 days). In some cases, experienced patients can reliably track their condition and evaluate the effectiveness of treatment. If some time after taking no-shpy in maximum dose the pain decreases slightly or does not remain at the same level, then there is nothing left but to see a doctor.

Pharmacology

Antispasmodic, isoquinoline derivative. It has a powerful antispasmodic effect on smooth muscles due to inhibition of the PDE4 type enzyme (PDE4). Inhibition of PDE4 leads to an increase in the concentration of cAMP, inactivation of myosin light chain kinase, which further causes smooth muscle relaxation. The Ca 2+ ion concentration-reducing effect of drotaverine through cAMP explains the antagonistic effect of drotaverine with respect 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 different tissues. PDE4 is most important for the suppression contractile activity smooth muscle, and therefore selective PDE4 inhibition may be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by a spastic state of the gastrointestinal tract.

Hydrolysis of cAMP in the myocardium and vascular smooth muscles 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 part of the heart and blood 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 autonomic innervation drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, and genitourinary system.

Due to its vasodilating action drotaverine improves tissue blood supply.

Thus, the above mechanisms of action of drotaverine eliminate spasm of smooth muscles, which leads to a decrease in pain.

Pharmacokinetics

Suction

After oral administration, drotaverine is rapidly and completely absorbed from the gastrointestinal tract. After first pass metabolism systemic circulation enters 65% taken dose drotaverine. C max in blood plasma is reached in 45-60 minutes. The action of the drug begins after 30 minutes.

Distribution

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

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

Metabolism

Drotaverine is almost completely metabolized in the liver.

breeding

T 1/2 drotaverine is 8-10 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 gastrointestinal tract (excretion into bile). Drotaverine is mainly excreted as metabolites; unchanged drotaverine is not found in the urine.

Release form

Tablets are yellow with a greenish or orange tint, round, biconvex, engraved with "spa" on one side.

Excipients: magnesium stearate - 3 mg, talc - 4 mg, povidone - 6 mg, corn starch - 35 mg, lactose monohydrate - 52 mg.

6 pcs. - PVC/Aluminum blisters (1) - cardboard packs.
24 pcs. - PVC/Aluminum blisters (1) - cardboard packs.
20 pcs. - blisters Aluminium/Aluminum (laminated with polymer) (2) - packs of cardboard.
60 pcs. - polypropylene bottles (1) with a polyethylene stopper, equipped with a piece dispenser - packs of cardboard.
100 pieces. - polypropylene bottles (1) - cardboard packs.

Dosage

Adults are prescribed 1-2 tablets. at one time 2-3 times / day. The maximum daily dose is 6 tab. (corresponding to 240 mg).

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

In the case of the appointment of the drug No-shpa ® for children aged 6 to 12 years - 40 mg (1 tab.) 1-2 times / day, for children over the age of 12 years - 4 mg (1 tab.) 1 -4 times / day or 80 mg (2 tablets) 1-2 times / day. The maximum daily dose - 160 mg (4 tab.)

When taking the drug without consulting a doctor, the recommended duration of taking the drug is usually 1-2 days. In cases where drotaverine is used as adjuvant therapy, the duration of treatment without consulting a doctor may be longer (2-3 days). If a pain syndrome persists, the patient should consult a doctor.

Efficiency evaluation method

If the patient can easily self-diagnose the symptoms of his illness, because they are well known to him, the effectiveness of the 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 significantly decrease 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 the palm of your hand so that the dosing hole on the bottom does not rest against the palm. Then press on the top of the vial, causing one tablet to fall out of the dosing hole on the bottom.

Overdose

An overdose of drotaverine was associated with disorders heart rate and conductivity, including complete blockade bundle pedicles and cardiac arrest, which can be fatal.

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

Interaction

PDE inhibitors, like papaverine, weaken the antiparkinsonian effect of levodopa. When prescribing the drug No-shpa ® simultaneously with levodopa, it is possible to increase rigidity and tremor.

With the simultaneous use of drotaverine with other antispasmodics, including m-anticholinergics, there is a mutual strengthening of the antispasmodic action.

Side effects

Below are adverse reactions observed in clinical research, divided by organ systems indicating the frequency of their occurrence in accordance with the following gradations recommended by WHO: very often (≥10%), often (≥1%,<10), нечасто (≥0.1%, <1%), редко (≥0.01%, <0.1%), очень редко, включая отдельные сообщения (<0.01%), частота неизвестна (по имеющимся данным частоту определить нельзя).

From the side nervous system: rarely - headache, dizziness, insomnia.

From the side of the cardiovascular system: rarely - a feeling of palpitations, a decrease in blood pressure.

From the digestive system: rarely - nausea, constipation.

From the immune system: rarely - allergic reactions (angioneurotic edema, urticaria, itching, rash).

Indications

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, spasms of the bladder.

As adjuvant therapy:

with 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;
with tension headaches;
with dysmenorrhea (menstrual pain).

Contraindications

severe liver or kidney failure;
severe heart failure (low cardiac output syndrome);
children's age up to 6 years;
breastfeeding period (no clinical data);
hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (for tablets, due to the presence of lactose monohydrate in their composition);
hypersensitivity to the components of the drug.

With caution, the drug should be used for arterial hypotension, during pregnancy, in children.

Application features

Use during pregnancy and lactation

The conducted studies did not reveal teratogenic and embryotoxic effects of drotaverine, as well as adverse effects on the course of pregnancy. However, if it is necessary to use the drug No-shpa ® during pregnancy, care should be taken and the drug should be prescribed only after assessing the ratio of the potential benefit to the mother and the possible risk to the fetus.

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

Application for violations of liver function

Use is contraindicated in severe liver failure.

Application for violations of kidney function

Use is contraindicated in severe renal failure.

Use in children

The drug is contraindicated in children under the age of 6 years.

special instructions

The composition of the 40 mg tablets includes 52 mg of lactose monohydrate, 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 glucose/galactose malabsorption syndrome.

Influence on the ability to drive vehicles and control mechanisms

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

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

To relieve a sudden spasm, to eliminate pain, the hands themselves reach for the first aid kit. There lies No-shpa - a faithful assistant for all family members at any time of the day. This antispasmodic will quickly relax smooth muscles and help relieve spasms of the heart and blood vessels. Someone has a remedy for pain for months and waits in the wings. But as soon as the spasm makes itself felt, small yellow pills quickly neutralize it.

Instructions for use of the drug No-shpa

When buying pills without a doctor's prescription, you need to carefully study the instructions and make sure that there are no serious restrictions on taking the drug. The instructions indicate the composition of the tablets, in which cases they can be used, to whom they are categorically contraindicated. It says what No-shpa helps with, and what dosage is needed for various pains at different ages.

Attention should be paid to the possibility of taking medication for expectant mothers and women who are breastfeeding. The instruction was compiled by specialists, it takes into account all possible reactions to other drugs if they are taken simultaneously with No-shpa. There are special instructions regarding alcohol and driving.

Indications for use, or what helps No-shpa

Antispasmodics are prescribed by doctors of various profiles. Urologists and gynecologists, surgeons and therapists, cardiologists and gastroenterologists.

There are main indications for starting the use of this drug:

Colic of the liver and kidneys;
gastrointestinal diseases;
Various pain sensations in the muscles;
Spasms of the stomach with an ulcer;
Severe headaches and painful periods;
Removal of spasms during the removal of stones from bile.

No-shpa is used by gynecologists during early pregnancy to exclude the possibility of miscarriage. Obstetricians also use the drug to open the uterus during childbirth.

Dosage, or how to use No-shpu correctly

The indications for the use of No-shpy must be followed by a dosage. Depending on how old a person is, the spasm of which organ needs to be eliminated, the number of tablets that can be taken during the day is prescribed.

See also: Instructions for use of the drug.

Method of application for children

If a child is under 6 years old, he is prescribed half a tablet in the morning, at lunchtime and at dinner. From 6 to 12 years old, this may already be 1 or 2 tablets with each meal. When giving the drug to children, you should definitely get a doctor's consultation in order to exclude all contraindications.

Method of application for adults

Children from 12 years of age and adults take an antispasmodic 2 tablets 3 times a day. The dose may be reduced or increased as directed by the physician or depending on the intensity of the spasms.

The tablet should be swallowed without chewing, drinking plenty of water. It is recommended to take No-shpu during or immediately after a meal so that the drug is quickly absorbed into the body.

Intravenous administration

No-shpa in ampoules is prescribed by a doctor in cases where sudden seizures and colic occur during the removal of stones. It is administered intravenously. The dosage is established only in a medical institution. Emergency workers may also administer the drug in solution to quickly relieve pain. The introduction into the vein is done by an experienced specialist only in the supine position, avoiding overdose.

Composition, description and pharmacotherapeutic group

No-shpa has a simple composition: 40 mg of drotaverine, starch, povidone, lactose, magnesium and talc. This drug can be immediately distinguished from others by its yellow color, convex round shape and marking with three letters - “spa”. No-shpa in ampoules and tablets belongs to the group of antispasmodics.

Pharmacokinetics of the drug

As soon as drotaverine enters the stomach with water or food, it is completely absorbed by the intestines. The drug is quickly and evenly distributed over all types of tissues and muscles, penetrates into the cells. Relaxation of spasms and pain relief occurs within 20 minutes after taking the tablets, 5-10 minutes after injection into a vein. The action stops after 6-8 hours. Completely excreted from the body within three days.

Contraindications to the use of tablets and side effects

The indications for the use of No-shpa indicate when this drug is prescribed by a doctor, and when it can be taken independently. But there are a number of diseases in which the use of tablets and injections is strictly prohibited or should be carried out with great care after consulting a doctor.

Renal and hepatic insufficiency of moderate and severe degree;
Low blood pressure, hypotension;
Sensitivity to the components of the drug;
Atherosclerosis, serious eye diseases;
When feeding babies with breast milk;
Pregnancy, except for the necessary doctor's prescriptions;
Serious heart disease.

There are cases of allergy to drotaverine. As soon as a rash appears on the body, itching and slight redness of the skin on the hands begin, taking No-shpa for headaches, coughing, and severe spasms should be stopped immediately. You can resume treatment only if the allergy is not confirmed.

Sometimes patients complain about various reactions of the body after they started taking No-shpu by prescription or on their own. These may be signs of arrhythmia or a slight decrease in pressure. It happens that the head begins to spin, or heat is felt throughout the body. Rare complaints of sweating and drowsiness.

No-shpa: analogues and prices in Russia

No-shpa has analogues in the same way as other basic drugs. Analogues are those that have in their composition the active original substance and the same effect on the body when taken.

The most effective and popular analogues of No-shpa:

and Nosh-bra;
Dolce and No-x-sha;
Nokhshaverin and two more forms of Drotaverin: forte and hydrochloride.

You should not assign an analogue to yourself. Only a qualified doctor can determine which drug to replace the original, if necessary. Both Drotaverine and No-shpa have exactly the same effect on the body of a child and an adult. The difference is only in the manufacturer and the possibility of a fake.

Drotaverine is not faked, because it is much cheaper than No-shpa. When purchasing a drug with a higher cost, you should ask for a certificate from a pharmacist, and also get one tablet to check the labeling. The price of Drotaverin ranges from 50 to 90 rubles. No-shpu in tablets can be purchased from 100 to 250 rubles, in injections - up to 450 rubles.

No-shpa for children: when to give

Starting from 12 months, the drug can be prescribed to children with such diseases and symptoms:

Headache that does not stop within an hour;
High temperature and muscle spasms due to its increase;
Pain with cystitis and kidney stones;
Bowel problems, constipation.

Sometimes parents give No-shpa for coughs or bronchitis to help with expectoration. But doctors cannot say for sure whether the drug has the desired effect in this case.

Tradename: NO-SHPA ®

International (non-proprietary) name: Drotaverine

Dosage form: tablets

Compound:

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.

Description

Round, biconvex tablets, yellow with a greenish or orange tint, spa engraved on one side.

Pharmacotherapeutic group:

Antispasmodic.

ATX code: A03A D02

Pharmacological properties:

Pharmacodynamics

Drotaverine is an isoquinoline derivative that exhibits a powerful antispasmodic effect on smooth muscles by inhibiting the enzyme, phosphodiesterase (PDE). The enzyme phosphodiesterase is required for the hydrolysis of cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). Inhibition of the enzyme phosphodiesterase 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 (MLCK). Phosphorylation of MLCK leads to a decrease in its affinity for the Ca 2+ -calmodulin complex, resulting in the inactivated form of MLCK supporting muscle relaxation. cAMP also affects the cytosolic Ca 2+ ion concentration by stimulating Ca 2+ transport into the extracellular space and sarcoplasmic reticulum. This Ca 2+ ion concentration-lowering effect of drotaverine through cAMP explains the antagonistic effect of drotaverinate with respect to Ca 2+ .

In vitro, drotaverine inhibits the PDE IV isoenzyme without inhibition of the PDE III and PDEV isoenzymes. Therefore, the effectiveness of drotaverine depends on the concentration of PDE IV in tissues, the content of which varies in different tissues. PDE IV is most important for suppressing the contractile activity of smooth muscles, and therefore, selective inhibition of PDE IV may be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by a spastic state of the gastrointestinal tract.

Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly with the help of the PDE III isoenzyme, which explains the fact that with high antispasmodic activity, drotaverine has no serious side effects on the heart and blood 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 autonomic innervation, drotaverine relaxes the smooth muscles of the gastrointestinal tract, biliary tract, and genitourinary system.

Pharmacokinetics

Absorption:

After oral administration, drotaverine is rapidly and completely absorbed. After first pass metabolism, 65% of the accepted dose of drotaverine enters the systemic circulation. The maximum plasma concentration (Cmax) is reached in 45-60 minutes.

Distribution

In vitro, drotaverine has a high association with plasma transactions (95-98%), especially with γ-albumin and β-globumins.

Drotaverine is evenly distributed throughout the tissues, penetrates into smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites may slightly cross the placental barrier.

Metabolism

In humans, drotaverine is almost completely metabolized in the liver by O-deethylation. Its metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4"-deethyldrotaverine, in addition to which 6-deethyldrotaverine and 4"-deethyldrotaveraldine have been identified.

breeding

In humans, a two-chamber mathematical model was used to assess the pharmacokinetics of drotaverine. The terminal half-life of plasma radioactivity was 16 hours.

Indications for use

spasms of smooth muscles 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 adjuvant therapy:

With 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 of "acute abdomen" (appendicitis , peritonitis, ulcer perforation, acute pancreatitis, etc.).
For tension headaches.
With dysmenorrhea.

Contraindications

hypersensitivity to the active substance or to any of the excipients of the drug
Severe liver or kidney failure
Severe heart failure (low cardiac output syndrome)
Children's age up to 6 years
Breastfeeding period (lack of clinical data).
Rare hereditary galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome (due to the presence of lactose in the preparation).

Carefully:

With arterial hypotension.

In children (lack of clinical experience).

In pregnant women (see section "Pregnancy and lactation").

Dosage and administration

adults

Usually the average daily dose in adults is 120-240 mg (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 in children have not been conducted.

In the case of the appointment of drotaverine to children:

For children from 6 to 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 during this period the pain syndrome does not decrease, the patient should consult a doctor to clarify the diagnosis and, if necessary, change therapy. In cases where drotaverine is used as adjuvant therapy, the duration of treatment without consulting a doctor may be longer (2-3 days).

Efficiency evaluation method

If the patient can easily self-diagnose the symptoms of his disease, since they are well known to him, then the effectiveness of the 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 decrease in pain or no decrease in pain, or if the pain does not significantly decrease after taking the maximum daily dose, it is recommended to consult a doctor.

Side effect

Below are the adverse reactions observed in clinical studies, divided by systems, organs, indicating the frequency of their occurrence in accordance with the following gradations: very frequent (≥ 10%), frequent (≥1%,<10); нечастые (≥0,1%, < 1%); редкие (≥0,01%, < 0,1%) и очень редкие, включая отдельные сообщения (< 0,01%), неизвестная частота (по имеющимся данным частоту определить нельзя).

From the side of the cardiovascular system

Rare - increased heart rate, lowering blood pressure.

From the side of the nervous system

Rare - headache, dizziness, insomnia.

From the gastrointestinal tract

Rare - nausea, constipation.

From the side of the immune system

Rare - allergic reactions (angioneurotic edema, urticaria; rash, itching) (see section "Contraindications").

Overdose

There are no data on drug overdose.

In the event of an overdose, patients should be under medical supervision and, if necessary, they should receive symptomatic and supportive treatment, including artificial vomiting or gastric lavage.

Interaction with other drugs

With levodopa

Phosphodiesterase inhibitors, like papaverine, reduce the antiparkinsonian effect of levodopa. When prescribing drotaverine simultaneously with levodopa, it is possible to increase rigidity and tremor. With other antispasmodics, including m-anticholinergics Mutual enhancement of antispasmodic action.

Drugs that significantly bind to plasma proteins (more than 80%)

Drotaverine significantly binds to plasma proteins, mainly albumin,

γ and β-globulins (see section "Pharmacokinetics"). There are 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 protein binding (displacement of one of the drugs by another from the protein bond and an increase in the concentration of the free fraction in the blood of the drug with a less strong binding to the protein), which is hypothetical may increase the risk of pharmacodynamic and/or toxic side effects of this drug.

special instructions

No-shpa® 40 mg tablets contain 52 mg of lactose. It can cause gastrointestinal complaints in individuals suffering from lactose intolerance. This form is unacceptable for patients suffering from lactose deficiency, galactosemia or impaired glucose / galactose absorption syndrome (see section "Contraindications").

Pregnancy and lactation

As shown by animal reproduction experiments and retrospective studies of clinical data, the use of drotaverine during pregnancy does not lead to either teratogenic or embryotoxic effects. However, the use of the drug is recommended only after careful weighing of the benefit/risk ratio.
Due to the lack of necessary clinical data during lactation, it is not recommended to prescribe.

Influence on the ability to drive a car and other mechanisms

When taken orally in therapeutic doses, drotaverine does not affect the ability to drive a car and perform work that requires increased attention. If any side effects appear, the issue of driving vehicles and working with mechanisms requires individual consideration. In the event of dizziness after taking the drug, you should avoid engaging in potentially hazardous activities, such as driving and working with mechanisms.

Release form

Tablets 40 mg.

6, 10 or 20 tablets in PVC/Aluminum blister.

1, 2,4 or 5 blisters of 6 tablets with instructions for use in a cardboard box.

3 blisters of 10 tablets with instructions for use in a cardboard box.

1 blister of 20 tablets with instructions for use in a cardboard box.

10 tablets in an Aluminium/Aluminum blister (laminated with a polymer).

2 blisters with instructions for use in a cardboard box.

60 or 64 tablets in a bottle of polypropylene with a polyethylene stopper,

equipped with a dispenser.

100 tablets in a polypropylene bottle with a polyethylene stopper.

1 bottle with instructions for use in a cardboard box.

Best before date

For Aluminium/Aluminum blister tablets: 5 years. For tablets in PVC/Aluminum blister packs: 3 years.

For tablets in vials: 5 years.

Do not use the drug after the expiration date indicated on the package.

Storage conditions

For Aluminium/Aluminum blister tablets: store at a temperature not exceeding 30 °C.

For tablets in PVC/Aluminum blister packs: store at a temperature not exceeding 25 °C. For tablets in vials: store in a place protected from light at a temperature of 15°C to 25°C. Keep out of the reach of children.

Terms of dispensing from pharmacies

Without recipe

Manufacturer
Hinoin Plant of Pharmaceutical and Chemical Products CJSC, Hungary st. Levai, 5,2112 Veresgyhaz, Hungary.

Claims of consumers should be sent to the address in Russia:

115035, Moscow, st. Sadovnicheskaya, 82, building 2.

No-shpa (NO-SPA) is a popular drug that has a quick antispasmodic effect on smooth muscles. It is applied for:

etiotropic therapy to eliminate spasm of muscle tissue, which is the basis of the pathological condition;
symptomatic treatment of spasm of smooth muscles, which is a symptom of the disease, without affecting its pathogenesis;
premedication during the preparation of patients to some procedures (catheterization of the ureters, urethra, etc.).

Since the drug acts exclusively on smooth muscles, it is practiced in situations where there are contraindications to antispasmodics from the anticholinergic group (prostatic hypertrophy,).

Pharmacological group: myotropic antispasmodic.

Drotaverine or No-shpa

Surely each of us had to take the famous yellow pills with a special aftertaste for various health problems. The composition of the drug contains the active substance drotaverine, and it is under this name that the most popular competitor of No-shpa and its analogue in composition are produced. What is the difference between Drotaverine and No-shpa?

Having studied the instructions for the preparations, it becomes clear that the composition, the principle of action, and the effect they have are similar. Therefore, a reasonable question arises - does it make sense to overpay for No-shpu?
No-shpa is an original drug, a patented dosage form. The presence of a patent is not only an excuse for the high cost of the drug, but also certain obligations that are imposed on the manufacturer: the quality of raw materials, production control, drug safety must be at the highest level. In order to obtain a patent, the drug must meet a number of strict requirements and pass the necessary clinical trials.

Drotaverine is a generic offered to the consumer under an international, and therefore non-proprietary name. The clinical efficacy of generics is not fully proven, since less stringent requirements are put forward for this group of drugs.

It turns out that a patented drug undergoes more testing before it hits the pharmacy counter. However, this does not mean that the generic has a negative effect on health.

Physical and chemical properties, composition, price

The drug is available in two dosage forms - tablets for oral administration and a solution for intramuscular and intravenous administration.

Base substance

Excipients

Physiochemical properties

No-shpa tablets

6, 20, 24 tablets in aluminum blisters. 60, 100 tablets in polypropylene bottles, in cardboard packs.

No. 6: 50-70 rubles;
No. 24: 180-220 rubles.

Drotaverine hydrochloride: 40 mg

Magnesium stearate 3 mg, corn starch 35 mg, talc 4 mg, povidone 6 mg, lactose monohydrate 52 mg.

Yellowish-greenish tablets, round, biconvex, debossed with "spa" on one side.

Solution

2 ml in glass ampoules made of dark glass with a break notch. 5 ampoules per pack, in cardboard packs.

No. 25: 450-480 rubles.

Drotaverine hydrochloride: 20 mg in 1 ml or 40 mg in 1 ampoule

Sodium disulfite 2 mg, 96% ethanol - 132 mg, water for injection - up to a volume of 2 ml.

Clear greenish-yellow solution.

pharmachologic effect

Drotaverine hydrochloride is an isoquinoline derivative with a powerful antispasmodic effect on smooth muscles. This effect is possible due to the inhibition of an enzyme called PDE (phosphodiesterase).

PDE is involved in the hydrolysis of cAMP to AMP. Inhibition of phosphodiesterase is characterized by an increase in the concentration of cAMP, which starts a chain reaction. cAMP in high concentrations is an activator of cAMP-dependent phosphorylation of MLCK (myosin light chain kinase). This leads to a decrease in the affinity of MLCK for the Ca2+-calmodulin complex, and the inactivated form of MLCK creates muscle relaxation.

cAMP affects the cytosolic concentration of the Ca2+ ion, lowering it. This is due to the stimulation of Ca2+ transport into the sarcoplasmic reticulum and extracellular space.

The effectiveness of drotaverine hydrochloride depends on the concentration of the phosphodiesterase enzyme in tissues, which varies significantly.

Hydrolysis of cAMP in the muscle tissue of the heart and vascular smooth muscle is carried out using the PDE3 isoenzyme. This explains the absence of serious adverse reactions from the CCC with high antispasmodic activity.

Selective PDE4 inhibitors, which is drotaverine, can reduce the sensitivity of the uterus to the action of the hormone oxytocin and lead to accelerated relaxation of the muscle tissue of the organ, which makes it possible to stop preterm labor.

In addition to the antispasmodic effect, drotaverine reduces swelling and inflammation in muscle tissue. The elimination of spasm leads to an improvement in the blood supply to the organs. The drug is effective for pain, and also helps to restore the passage of the internal contents of hollow organs.

At the same time, drotaverine does not directly interfere with the mechanism of pain sensitivity and does not erase the symptoms of acute conditions, unlike analgesics.

The effectiveness of drotaverine is high in spasms of smooth muscle tissue of neurogenic and muscular origin. No-shpa relaxes the smooth muscle fibers of the gastrointestinal tract, urinary and biliary tract.

Pharmacokinetics

After ingestion, the active substance is completely and rapidly absorbed, evenly distributed throughout the tissues and penetrates into smooth muscle cells. About 65% of the active substance enters the blood. The maximum concentration in the blood is determined 45-60 minutes after ingestion. Slightly passes through the placental barrier. It does not enter the central nervous system and does not affect the autonomic nervous system.

When administered intravenously or intramuscularly, drotaverine binds to plasma proteins by 95-98% with a maximum effect after 30 minutes.

Metabolism of the substance occurs to the liver cells by O-deethylation reactions. Drotaverine metabolites are conjugated with glucuronic acid.

Excreted by the kidneys (more than 50%) and intestines (30%) as metabolites, complete elimination occurs within 72 hours.

Indications for use

The instructions for use of No-shpa indicate the following indications for etiotropic therapy:

Spasms of smooth muscle tissue in diseases of the biliary tract: cholangiolithiasis, cholecystolithiasis, pericholecystitis, cholecystitis, cholangitis, papillitis;
Spasms of smooth muscle tissue in pathologies of the urinary system: nephrolithiasis, pyelitis, urethrolithiasis, cystitis, spasms and tenesmus of the bladder;

What else helps No-shpa? As an auxiliary therapy drug (tablets or solution if it is impossible to take tablets):

with spasms of smooth muscle tissue of the gastrointestinal tract: gastritis, gastric ulcer and duodenal ulcer, spasms of the pylorus and cardia of the stomach, colitis, spastic colitis with constipation, enteritis, sphincter of Oddi dysfunction, irritable bowel syndrome;
for tension headaches (tablet form). No-shpa is not effective for headaches associated with migraine or increased ICP;
with dysmenorrhea.

Contraindications

severe degree of renal or heart failure;
children's age up to 6 years (tablets). Nosh-pa is not prescribed for children under 18 years of age in the form of a solution;
lactation period (due to the lack of clinical data on the penetration of the drug into mother's milk);
hereditary intolerance to galactose monosaccharide, glucose-galactose malabsorption syndrome, lactase deficiency (for tablets);
hypersensitivity to sodium disulfite (for solution).

special instructions

With caution, the drug is prescribed for arterial hypotension, since there is a risk of collapse, during pregnancy and in pediatrics. When administered intravenously, people with low blood pressure should be in a supine position.

There may be complaints of gastrointestinal dysfunction when using the drug in people with lactose intolerance (52 mg lactose per 1 tablet).

The tablet form does not affect the ability to perform work that requires a significant concentration of attention, and driving a car. After parenteral administration of No-shpa, one should refrain from precise work and driving a car.

No-shpa during pregnancy

Very often, the drug is prescribed in the early stages of pregnancy with uterine tone to reduce the threat of spontaneous miscarriage.

Animal studies and data from a retrospective analysis of the clinical use of drotaverine in pregnant women indicate that the drug in therapeutic dosages did not have either embryotoxic or teratogenic effects on the fetus. But, since the drug crosses the placenta to some extent, the appointment is justified if there is a real risk of miscarriage.

The drug should not be used during labor, as there is a risk of atonic bleeding in the postpartum period.

Dosage of No-shpy

The duration of treatment is individual. It is allowed to take the drug on its own for 1-3 days.

For tablets

Adult patients: 120-240 mg per day, dividing the dose into 2-3 doses. The maximum dose for a single dose is 80 mg.
Children 6-12 years old: 80 mg per day, divided into 2 doses.
Children over 12 years old: 160 mg per day, divided into 2-4 doses.

For maximum effectiveness, the drug is taken 1 hour after a meal with plenty of water.

For solution

Adult patients: 40-240 mg per day, divided into 1-3 injections. In acute spasmodic pain, the drug is administered intravenously slowly, at a dose of 40-80 mg over 30 seconds. V / m injections are administered without diluting the solution with other drugs.

The effectiveness of the drug can usually be assessed by the patient himself, observing a significant decrease or disappearance of the pain spasmodic syndrome within a few hours after taking the pill or injection.

Side effects

CCC: rarely observed tachycardia or decrease in blood pressure;
Nervous system: insomnia, headache and dizziness are rarely noted;
Gastrointestinal: sometimes there is nausea and constipation;
The immune system: occasionally develop allergic reactions (rash, itching). There have been cases of anaphylactic shock with and without fatal outcome (frequency unknown). In persons with bronchial asthma or allergies, bronchospasm may develop when using the drug solution.
Local reactions: swelling at the injection site.

Overdose

With a significant excess of the therapeutic dose, a violation of cardiac conduction and rhythm develops, up to a complete blockade of the legs of the bundle of His and cardiac arrest. Treatment is inpatient only.

drug interaction

Levodopa - weakening of the antiparkinsonian action, increased rigidity and tremor;
Other antispasmodics- increased antispasmodic action;
Tricyclic antidepressants- increased arterial hypotension (only when combined with No-shpa solution);
Morphine - a decrease in spasmodic activity (only when combined with No-shpa solution);
Phenobarbital - increased antispasmodic effect of No-shpa;
Drugs that bind to plasma proteins- possible pharmacodynamic and toxic effects of these drugs.

Analogues

No-shpa forte, Drotaverin, Drotaverin-Forte, Spazmonet, Drotaverin-sti, Spazmol.

Drotaverine hydrochloride

40 mg. 20 tab. 12-20 rub.

Spazmonet

40 mg. 20 tab. 55-80 rub.

Drotaverine forte

80 mg. 20 tab. 50 rub.

Spasmol

40 mg. 20 tab. 32 rub.

No-shpa is a drug that has an antispasmodic effect. Available in the form of a solution for injection and tablets.

Pharmacological action of No-shpa

According to the instructions for No-shpa, the active ingredient of the drug is drotaverine hydrochloride. Auxiliary substances of the solution are ethanol 96%, sodium metabisulphite, water for injection. Auxiliary components of No-shpa tablets are lactose monohydrate, corn starch, polyvidone, talc, magnesium stearate.

The active substance of the drug is an isoquinoline derivative. When using No-shpa, it has an antispasmodic effect on smooth muscles due to inhibition of the PDE 4 enzyme (phosphodiesterase 4), which leads to an increase in the concentration of cyclic adenosine monophosphate. Due to this effect, the myosin kinase light chain is inactivated, resulting in smooth muscle relaxation.

No-shpa inhibits the PDE 4 enzyme in vitro without blunting the PDE 3 and PDE 5 isoenzymes. The therapeutic effect of the drug depends on the content of PDE 4 in the tissues, since it plays an important role in the contractility of smooth muscles. Therefore, the use of No-shpa is effective in the treatment of hyperkinetic diseases and diseases that have arisen against the background of spastic conditions of the gastrointestinal tract.

The PDE 3 isoenzyme is responsible for the hydrolysis of cyclic adenosine monophosphate in vascular and myocardial smooth muscle cells, due to which No-shpa is highly effective as an antispasmodic, even in the absence of a pronounced effect on the cardiovascular system, as well as with undesirable serious cardiovascular events.

In accordance with the instructions for No-shpa, the active component of the drug actively affects the smooth muscles of the vascular and genitourinary systems, as well as the biliary tract and the gastrointestinal tract.

Thanks to its vasodilating properties, No-shpa normalizes the blood supply to tissues.

The drug is completely and quickly absorbed. The maximum concentration in the blood reaches 40-60 minutes after application. Drotaverine has a high ability to bind to plasma proteins. The drug is metabolized in the liver. The substance is completely eliminated from the body after 72 hours in the form of metabolites through the kidneys.

There are restrictions on the appointment of No-shpa for children.

Indications for use No-shpy

No-shpu is used to eliminate spasms of smooth muscles in diseases of the biliary tract, which include papillitis, cholangitis, pericholecystitis, cholecystitis, cholelithiasis.

A drug is prescribed for the relief of spasms of smooth muscles of the urinary system with bladder tenesmus, cystitis, pyelitis and urolithiasis.

During pregnancy, No-shpu is prescribed to relieve the threat of miscarriage and prevent premature birth. The drug reduces the phase of the opening of the cervix, due to which childbirth is faster.

As an adjuvant therapy, No-shpa is used for headaches, dysmenorrhea and severe labor pains.

Methods of application of No-shpa and dosage

The daily dose of No-shpa tablets is 120-240 mg, which is divided into 2-3 doses. The maximum single dosage of No-shpa tablets is 80 mg, the daily amount should not exceed 240 mg.

Intramuscularly, the solution is administered in a daily dose of 40-240 mg, divided into 3 doses. To eliminate acute colic (renal or biliary), No-shpu is administered intravenously slowly (over 30 seconds) in an amount of 40-80 mg.

During pregnancy, No-shpu is taken at 120-240 mg per day, as soon as the primary symptoms of increased uterine tone appear. To accelerate the opening of the cervix during childbirth, 40 mg of the solution is administered intramuscularly. In the absence of the desired therapeutic effect, it is possible to re-administer the drug after 2 hours.

No-shpu for children from 6 to 12 years old is prescribed in a daily dose of 80 mg, divided into 2 doses. The daily dose of No-shpa for children over the age of 12 should not exceed 160 mg, which are divided into 2-4 doses.

Side effects of No-shpy

In rare cases, the use of No-shpa may cause adverse reactions from the body:

Digestive system: nausea, constipation, vomiting;
Central nervous system: headaches, insomnia, dizziness;
Cardiovascular system: decrease in blood pressure, increase in heart rate.

No-shpa can provoke the occurrence of allergic reactions, accompanied by angioedema, urticaria, skin rash, itching.

Contraindications to the use of No-shpa

According to the instructions, No-shpu is not prescribed to people who have:

severe kidney, heart or liver failure;
Hereditary galactose intolerance;
Glucose-galactose malabsorption syndrome (for No-shpa tablets);
Hypersensitivity to the components of the drug;
Angle-closure glaucoma;
prostatic hypertrophy;
Arterial hypotension.

The use of the tablet form of No-shpa for children under the age of 6 years is contraindicated, as well as No-shpa in the form of a solution for injection - up to 18 years.

The drug should not be taken by women during lactation.

Overdose

If No-shpa is used in quantities significantly higher than recommended, you should consult a doctor for further treatment.

Analogues

According to the chemical composition and therapeutic effect, No-shpa analogues are Tetraspasmin, Nospazin, Nospan, Dihydroetaverin, Diprolene, Drotaverin.