No-shpa solution d/in. 20mg/ml amp. 2ml No. 25

No-Shpa is an antispasmodic drug that has been produced for over 60 years and has many positive reviews from consumers. It is very popular in the CIS countries, Eastern Europe and Asia. According to English-language sources, the main active component of this medicine, drotaverine, is mainly used intravenously to relieve pain during labor. Numerous studies have shown that drotaverine is effective in various situations and take No-Shpu with:

• menstruation;
• stomach cramps;
• headache.

The drug is also completely safe for children. Let's consider all the features of But Shpa : method of use, contraindications, how it affects the body and how it interacts with other medications.

Compound

The main active ingredient contained in the drug is drotaverine. This substance is a modified papaverine, a painkiller made from the opium poppy.

1 tablet of No-Shpa contains:

• drotaverine hydrochloride – 40 mg;
• magnesium stearate – 3 mg;
• talc – 4 mg;
• povidone – 6 mg;
• corn starch – 35 mg;
• lactose monohydrate – 52 mg.

The dosage form of the drug is convex yellow tablets with a greenish or orange tint and “spa” engraving on one side.

Pharmacodynamics

The main component of the drug is drotaverine, which is an isoquinoline derivative. The substance has an antispasmodic effect, reduces the entry of Ca2 into smooth muscle cells, reduces intestinal motility and smooth muscle tone of internal organs, and dilates blood vessels. Does not affect the autonomic nervous system. Unlike papaverine, with which drotaverine is similar in chemical structure and pharmacological properties, it has a strong and long-lasting effect.

Drotaverine has a direct effect on smooth muscles, so it can be used in situations in which drugs from the M-anticholinergic group are contraindicated.

Instructions for use NO-SPALGIN

Paracetamol

has analgesic and antipyretic effects, mainly due to the suppression of the synthesis of prostaglandins in the tissues of the central nervous system and, to a lesser extent, due to the suppression of the synthesis of prostaglandins and other substances that stimulate pain receptors in the periphery.

Drotaverine

is an isoquinolone derivative that has an antispasmodic effect directly on smooth muscles. The decisive mechanism of action is the selective blockade of the enzyme phosphodiesterase IV with a subsequent increase in the level of cAMP, which, by inactivating myosin light chain kinase (MLCK), leads to relaxation of smooth muscles. Its action does not depend on the influence of the autonomic nervous system.

Codeine

is an analgesic of central action, acting on μ and κ receptors involved in the transmission of pain signals in the central nervous system.

Study of the interactions of the active ingredients of the combination

Based on clinical results

One pilot, open-label, randomized, parallel-group phase I clinical trial in healthy male volunteers found that active ingredients used in combination (8 mg codeine, 40 mg drotaverine, and 500 mg paracetamol) and alone were safe and well tolerated . No severe adverse reactions were recorded; We observed 5 cases of non-severe reactions, but only 2 of them were possibly related to taking the drug or taking blood for testing (1 case of a temporarily positive complicated Romberg test and 1 case of superficial phlebitis of the forearm).

During pharmacokinetic measurements, it was shown that when taking the combination, the saturation stage is reached within 6 days with a single daily dose, and within 3 days with a double dose.

The combination of codeine + drotaverine + paracetamol increased the AUC and Cmax of drotaverine,

those. the use of the combination improved the relative bioavailability of drotaverine. According to the results of the study, Cmax values ​​were in the range of 132÷171 ng/ml, and AUC0-24 values ​​were 463.4÷830.2 ng*h/ml.

These data meant more effective

analgesic effect and a slight increase in duration of action.

Similar results were obtained in the case of paracetamol:

the combination increased AUC and significantly decreased clearance at both doses.
According to the results of the study, Cmax values ​​were in the range of 5495÷6752 ng/ml, AUC0-24 values ​​were 21760.8÷26524.7 ng*h/ml, and clearance values ​​were 356-418 ml/min. Previous trials and kinetic studies have shown that codeine
does not interact with either paracetamol or drotaverine.

To compare the effectiveness of the combination with that of paracetamol alone, one comparative, multicenter, randomized, double-blind, double-placebo-controlled, parallel-group phase III study was conducted.

Results of preclinical safety tests

Results of preclinical safety studies of each active substance separately

Paracetamol

Oral LD50 in mice was 295-1212 mg/kg body weight, in rats - > 4 g/kg. The approximate IV lethal dose of paracetamol is 826 mg/kg and the oral LD50 is 2404 mg/kg. Long-term use of very high doses (1-7 g/kg) caused damage to the liver and kidneys of laboratory animals.

Paracetamol had no effect on reproductive function and was neither mutagenic nor carcinogenic.

Drotaverine

There are no preclinical data that could influence the clinical use of the drug.

Codeine

There are no preclinical data that could influence the clinical use of the drug.

Indications and contraindications

You should use No-Shpu with arterial hypotension especially carefully. One tablet of No-Shpa contains 104 mg of lactose, so people with lactose intolerance should limit their intake of No-Shpa to avoid problems with the gastrointestinal tract. Those suffering from galactosemia, lactose deficiency or glucose/galactose malabsorption syndrome should avoid taking this medicine.

Indications for use

For therapeutic purposes for:

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

As an auxiliary treatment (when the use of the drug in tablet form is not possible) for:

• spasms of smooth muscles of the gastrointestinal tract: gastric and duodenal ulcers, gastritis, cardio- and/or pylorospasm, enteritis, colitis;
• gynecological diseases: dysmenorrhea.

Instructions for use

No spa tablets: instructions for use for adults: take 1-2 tablets at a time 2-3 times a day. The maximum dose of the drug is 6 tablets (240 mg of drotaverine) per day. You can take No-Shpa without a doctor’s prescription for 1-2 days; if it is used for auxiliary therapy, then 2-3 days.

Clinical studies of the active substance with the participation of children have not been conducted. If this drug is prescribed to children, it should be taken as follows:

• From 6 to 12 years – 1 tablet 1-2 times a day, maximum dose – 80 mg of drotaverine (2 tablets).
• 12 years and older - 1 tablet 1-4 times a day or 2 tablets 1-2 times a day, maximum dose of drotaverine - 160 mg (4 tablets).

The pain disappears a few hours after taking No-Shpa. If this does not happen, it is recommended to consult a doctor.

Side effects

The body may react adversely to the components of the drug. Possible symptoms include:

• Nervous system: headache, dizziness, sleep disorder, vertigo.
• Cardiovascular system: decreased blood pressure, palpitations.
• Digestive system: nausea, constipation.
• Immune system: allergic reactions (rash, itching, urticaria).

All side effects of the drug are rarely detected: approximately 1 case in 10,000.

An overdose of No-Spa causes cardiac rhythm and conduction problems, which can lead to drug failure and death. In case of an overdose of the drug, you should immediately consult a doctor and subsequently receive symptomatic treatment under his supervision.

Pregnancy and lactation

Clinical studies have shown that drotaverine does not have a teratogenic or embryotoxic effect, therefore its use during pregnancy is allowed . It is important to be careful and take drotaverine only after weighing the benefits for the mother and the potential risk for the child. There are no preclinical and clinical data on the use of the drug during lactation, therefore, taking No Shpu while breastfeeding is not recommended .

Use during pregnancy or breastfeeding

Pregnancy. As shown by the results of retrospective clinical studies and animal studies, oral administration of the drug did not cause any evidence of any direct or indirect effect on pregnancy, embryonic development, childbirth or postpartum development. However, pregnant women should use this drug with caution. Drotaverine should not be used during childbirth.

Lactation. Due to the lack of data from preclinical studies, administration of the drug during breastfeeding is not recommended.

During menstruation

The peculiarity of drotaverine, which is part of No Shpa, is that it relaxes the smooth muscles of various organs, including the uterus. It relieves spasms and improves blood flow, which helps get rid of painful sensations. The drug is taken 1-2 pills 2-3 times a day for 1-2 days or until the pain disappears. The maximum dosage of no spa is 2 tablets at a time. Note! But Shpu should be taken during menstruation only if you are sure that this is pain during a natural process.

Interaction with other drugs

PDE inhibitors like papaverine, which includes drotaverine, which is part of No-Shpa, weaken the antiparkinsonian effect of the substance levodopa (dihydroxyphenylalanine). Therefore, the combination of No Shpa and drugs containing levodopa can lead to increased tremor and rigidity. In combination with other antispasmodic drugs, No Shpa enhances its analgesic effect. Before combining this drug with other medications, you should consult your doctor.

Note!

Description of the drug No-spa solution d/in. 20mg/ml amp. 2ml No. 25 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Precautionary measures

No-Shpa contains disulfite, a substance that can cause allergic reactions, including anaphylactic symptoms and bronchospasm in people with hypersensitivity, especially in patients with asthma or allergic diseases. If you are sensitive to parenteral disulfite, you should not take the drug. When administering drotaverine intravenously, patients with low blood pressure should be in a horizontal position to minimize the risk of collapse.

Effect on driving

When taken orally in small doses, No-Shpa has no effect on people driving or operating other equipment. However, during treatment with the drug when driving a vehicle or other activities that require increased concentration, you should be careful. If dizziness occurs after taking No-Shpa, then these types of activities should be abandoned. The question of whether it is possible to drive a car and operate machinery if there are side effects from using No-Shpa is decided by the attending physician.

No-spalgin® (No-spalgin®)

Paracetamol

after oral administration, it is quickly and completely absorbed from the small intestine.

Maximum plasma concentration is reached after 30-90 minutes and its plasma half-life is 2 hours.

Paracetamol binds weakly to plasma proteins and red blood cells, its distribution is rapid and uniform. Paracetamol is metabolized in the liver, its metabolites are excreted by the kidneys through glomerular filtration. About 85% of the dose taken is excreted in the form of glucuronides, 2% in the form of sulfates, 3% unchanged. Approximately 10% of the dose taken is neutralized in the liver by conjugation with glutathione.

Codeine

after oral administration, it is quickly absorbed from the gastrointestinal tract.

The maximum plasma concentration of codeine is achieved after 1 hour, and its plasma half-life is 2.5-3.5 hours.

Codeine is moderately bound to plasma proteins and is rapidly distributed, accumulating in the kidneys, lungs, liver and skeletal muscles, while brain tissue is not able to accumulate codeine. Codeine crosses the placental barrier and is excreted into breast milk.

In the liver, codeine is metabolized primarily by glucuronidation to codeine-6-glucuronide. A small portion of codeine undergoes O-demethylation, leading to the formation of morphine, and N-demethylation, leading to the formation of norcodeine, with the formation of normorphine after O- and N-demethylation. Morphine and norcodeine are further conjugated with glucuronic acid. Unchanged codeine and its metabolites are excreted mainly by the kidneys within 48 hours (84.4±15.9% of the dose of codeine taken). O-demethylation of codeine to morphine is catalyzed by the cytochrome P450 isoenzyme CYP2D6, which is characterized by genetic polymorphisms that can affect the efficacy and toxicity of codeine.

Genetic polymorphism of the CYP2D6 isoenzyme is manifested by genotypes with ultra-high, high and low activity of the CYP2D6 isoenzyme.

Drotaverine

after oral administration it is quickly and completely absorbed. The maximum plasma concentration is achieved after 45-60 minutes.

Drotaverine entering the systemic circulation is 95-98% bound to plasma proteins, mainly albumins and air globulins.

The plasma half-life is 2.4 hours, the biological half-life is 8-10 hours.

The metabolism of drotaverine occurs in the liver. More than 50% of the dose taken is excreted in the urine, 30% in feces. Drotaverine penetrates the placental barrier.

Combination paracetamol + drotaverine + codeine

A study of the pharmacokinetics of the combination of paracetamol + drotaverine + codeine showed that the equilibrium concentration (Css) of the active ingredients of the drug is established on the 6th day when using one dose per day and on the 3rd day when using two doses per day.

Both with a single dose and with a course of taking the drug, codeine does not affect the pharmacokinetics of paracetamol and drotaverine, and paracetamol does not affect the pharmacokinetics of codeine. Drotaverine and paracetamol do not interact at the level of binding to plasma proteins.

In in vitro

It has been shown that paracetamol (in the therapeutic dose range) nonspecifically inhibits the metabolism of drotaverine, which increases the half-life of the latter by 2-7 times, so it is possible that
in vivo
it can also inhibit the metabolism of drotaverine.

The combination of paracetamol + drotaverine + codeine increases the values ​​of AUC0-24 (area under the concentration-time curve within 24 hours after administration) and Cmax (maximum concentration) of drotaverine, which are in the range of 463.4-830.2 ng*h/ l and 132-171 ng/ml, respectively, that is, the use of the combination increases the relative bioavailability of drotaverine.

A similar phenomenon has also been shown for paracetamol. This combination increases the AUC0-24 values ​​of paracetamol and significantly reduces its clearance. The values ​​of Cmax, AUC0-24 and paracetamol clearance were in the range of 5495-6752 ng/ml, 21760.8-26524.7 ng*h/l, 365-418 ml/min, respectively. This may provide greater pain relief with a slightly longer duration.

Package

No-Shpa is available in the form of pills and solution for intravenous administration. Tablets of 40 or 80 mg are packaged in plastic blisters of 20 pieces. Each such tablet of medicine, along with instructions, is placed in a cardboard box. The packaging varies depending on the number of tablets inside:

• No. 12: 12 tablets per plate. 1 record per package.
• No. 24: 24 tablets per strip, 1 strip per package.
• No. 60: 60 tablets in a dosing container with protective tape, 1 container per box.
• No. 100: 100 ballet shoes per bottle, 1 bottle per package with a tamper-evident sticker.

The solution for injection is a clear, colorless liquid, which is collected in dark-colored ampoules of 2 ml, which are packed in 5 pieces in a plastic contour package.

Release forms and price category

No-spa is available in the form of tablets, as well as in ampoules for intramuscular and intravenous administration. The dosage of one tablet is 40 mg of drotaverine hydrochloride. The tablets have a yellowish-greenish color and are bitter to taste. On one side there is a marking with the inscription “spa”. There are blisters of 6 and 24 pieces. For larger quantities, bottles with stoppers are used, which have 60, 64, 100 pieces. Ampoules are available in two milliliters. The amount of drotaverine per 1 ml of solution is 20 mg; only 2 ml of solution contains 40 mg of drotaverine hydrochloride. The ampoules are made of dark glass and have a marked break point for ease of opening.

No-spa is available in the form of tablets and ampoules.

The drug is affordable. It all depends on the manufacturer, but in any case, no-silo can be classified as a budget drug.

Reviews

I was diagnosed with a stomach ulcer quite a long time ago, because of which I often have to suffer from pain in the stomach area. In such cases, I almost always use No-shpa - it is inexpensive and helps quickly - almost always everything goes away in 30 minutes. I did not find any side effects during use. I usually take 2 tablets after meals; if there are any special circumstances, I call my doctor, he will advise me on how to calculate the dosage.

Andrey, 37 years old

Excellent medicine, I have been using it for many years, I always have it on hand. When I take a severe headache along with analgin, they get along well, there are no side effects, and all the symptoms go away. In general, all relatives, when any pain or spasms appear, take noshpa, even my grandmother drinks for high blood pressure.

Irina, 29 years old

I most often take it for headaches, although it also helps with stomach and back pain. A doctor prescribed No-shpa to a friend for prostatitis, and my sister takes it for vegetative-vascular dystonia. It starts to work in about half an hour, not always the effect that we would like, but in terms of price/quality ratio it’s simply top!

Oleg, 26 years old

Question answer

Unlike analgesics, No-shpa eliminates the spasm that causes pain. The medicine has a high safety profile and is well tolerated by various groups of people.

The manufacturer does not indicate the time of taking the drug, so it is most often taken after meals. In order to relieve acute pain, No-shpa can be drunk outside, regardless of meals.

the manufacturer of the original drug has registered the official trademark NO-SHPA, therefore any analogues produced as domestic analogues are fakes. The original packaging of No-shpa contains a holographic image confirming its originality. Another one is to purchase medications from large, reputable chain pharmacies.

Alcohol in large quantities can cause side effects of the drug: headache, dizziness, nausea, heart palpitations, etc. During the course of treatment, you must stop drinking alcohol. It is strictly forbidden to treat hangover syndrome with No-shpa.

Advantages

Antispasmodics affect smooth muscles and relieve pain caused by spasms. The antispasmodic drug drotaverine is used in gastroenterology, therapy, urology and gynecology in many countries around the world.

• Gastroenterology. In this area, the drug is prescribed for spastic pain accompanying pathology of the biliary tract - cholelithiasis, acute or chronic cholecystitis, cholangitis, etc.
• Urology. Inflammatory processes in the urinary organs (cystitis, pyelitis) can also lead to spasms, so the use of drotaverine for these diseases is completely justified.
• Tension headaches. Drotaverine can also be used to treat tension headaches, since in this case there are muscular and vascular components.

The favorable safety profile has been confirmed by numerous clinical studies.