No-spa is one of the most common and frequently used antispasmodics in pediatric practice. Antispasmodics are drugs that relax the smooth muscles of many internal organs, thereby relieving excess spasm (contraction) of smooth muscle cells. The mechanisms of action of these agents are different. We will not go into deep detail, but will only say that there are neurotropic and myotropic antispasmodics. Complex terms, the essence of which we will now explain. The mechanism of action of neurotropic antispasmodics is the blockade and disruption of the conduction of impulses from the nervous system to the muscles. In turn, the mechanism of action of myotropic antispasmodics is a direct effect on smooth muscle cells by changing the biochemical processes in them.
As you know, smooth muscle is found in many organs and systems of the body, for example, in the gastrointestinal tract, urinary and reproductive systems, respiratory system (especially in the bronchi) and others. Thus, the spectrum of action and indications for which antispasmodics can be used are quite extensive. One of the most common causes of pain is spasm (contraction) of muscle cells. Antispasmodics, eliminating spasms, have a pronounced analgesic effect.
In this article we will pay much attention to drotaverine, known as “No-shpa”. We will tell you about its release forms, price category, indications and contraindications, dosages, unwanted side reactions. We will also talk about other myotropic antispasmodics that can be used in children.
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.
No-spa solution for injection 20 mg/ml ampoules 25 pcs. in Moscow
Injection:
transparent liquid of greenish-yellow color.
Pills:
round, biconvex, yellow, with a greenish or orange tint, with “spa” engraved on one side.
Absorption.
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 plasma is reached after 45–60 minutes.
Distribution. In vitro
drotaverine has a high binding to plasma proteins (95–98%), especially albumin, γ and β-globulins.
Drotaverine is evenly distributed throughout the tissues and penetrates smooth muscle cells. Does not penetrate the BBB. Drotaverine and/or its metabolites may 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.
Excretion.
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 gastrointestinal tract (excretion into bile). Drotaverine is mainly excreted in the form of metabolites; unchanged drotaverine is not found in the urine.
Drotaverine is an isoquinoline derivative. Shows a powerful antispasmodic effect on smooth muscles due to inhibition of the phosphodiesterase enzyme (PDE). The enzyme PDE is necessary for the hydrolysis of cAMP to AMP. Inhibition of PDE leads to an increase in the concentration of cAMP, which triggers the following cascade reaction: high concentrations of cAMP activate cAMP-dependent phosphorylation of myosin light chain kinase (MLCK), phosphorylation of MLCK leads to a decrease in its affinity for the Ca2+-calmodulin complex, as a result of which the inactivated form of MLCK maintains muscle relaxation. cAMP also affects the cytosolic concentration of Ca2+ ion by stimulating the transport of Ca2+ into the extracellular space and the sarcoplasmic reticulum. This Ca2+-lowering effect of drotaverine via cAMP explains the antagonistic effect of drotaverine on Ca2+.
In vitro
drotaverine inhibits the PDE4 isoenzyme without inhibiting the PDE3 and PDE5 isoenzymes. Therefore, the effectiveness of drotaverine depends on tissue concentrations of PDE4, which vary from tissue to tissue. 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.
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.
Indications and contraindications
No-shpa is most often used in pediatric gastroenterology. Indications for prescribing the drug are:
- Diseases of the gallbladder and bile ducts . The pathology of these organs is often accompanied by spasms. Such diseases include: inflammation of the gallbladder (cholecystitis) and bile ducts (cholangitis), cholelithiasis (calculous cholecystitis, cholangiolithiasis, cholecystocholangitis). It is worth noting that with the development of acute colic, a solution is used for intramuscular and intravenous administration. No-shpa is often used for inflammatory diseases of the stomach and intestines: gastritis, peptic ulcer, enteritis, colitis.
- Diseases of the urinary system . The need to use drugs in this case is also associated with spasms of smooth muscles. These diseases include: inflammation of the kidneys (pyelonephritis), inflammation of the bladder (cystitis), urolithiasis, etc. It is worth noting that with the development of renal colic, preference is given to a solution for intramuscular and intravenous administration, which makes it possible to achieve the desired concentration of the drug in a shorter time. drugs in the blood.
- It is used as an adjuvant in gynecology for dysmenorrhea . Dysmenorrhea is a pathological process in which girls experience severe pain in the lower abdomen during menstruation. In addition to pain, girls often experience nausea, dizziness, headaches, bloating, increased body temperature and other symptoms.
- Quite often, no-shpa is used as an antipyretic at fever . The fact is that there are two types of fevers in children: “pale” and “pink”. "Pink" is more favorable. “Pale” fever is accompanied by symptoms of microcirculation disorders, which are clinically manifested by pallor and “marbling” of the skin. The children's limbs are cold. There is a pronounced feeling of cold and chills. In order to eliminate such fever, you will need no-spa or another antispasmodic for parenteral (intravenous or intramuscular) administration. In addition to analgin, a solution of drotaverine (“No-shpa”) is administered at a dose of 0.1 ml per 1 year of life. The dosage of this product is given for informational purposes only. The choice of medication, as well as its dosage, should be made by the attending physician.
No-shpa is often used as an antipyretic.
Like any other medicine, no-spa has its contraindications:
- Severe liver, kidney, heart failure.
- The period of breastfeeding (lactation).
- Hypersensitivity to the active substance and other excipients included in its composition.
- Children's age up to 6 years. It is worth noting that in pediatric practice this drug is used at an earlier age.
- Malabsorption syndrome associated with lactose and galactose intolerance. Malabsorption is a malabsorption of a substance in the small intestine. As a rule, it is associated with a deficiency of a substance or enzyme that takes part in the absorption of this substance.
Buy No-spa solution intravenously and intramuscularly 40mg/2ml 2ml No. 5 in pharmacies
Instructions for use No-spa solution IV and IM 40 mg/2 ml 2 ml No. 5
Dosage forms injection solution 20mg/ml 2ml
Synonyms Droverin Nosh-bra Spazmol Spazmonet Group Antispasmodics - isoquinoline derivatives International nonproprietary name Drotaverine Composition Active substance - Drotaverine. Manufacturers Hinoin (Hungary), Hinoin Pharmaceutical and Chemical Products Plant A.O. (Hungary), Hinoin Pharmaceutical and Chemical Products Plant CJSC (Hungary) Pharmacological action Antispasmodic, myotropic, vasodilator, hypotensive. Quickly and completely absorbed into the gastrointestinal tract. It is evenly distributed throughout the tissues and penetrates smooth muscle cells. Excreted by the kidneys. Pronouncedly and for a long time expands the smooth muscles of internal organs and blood vessels, reduces blood pressure, and increases cardiac output. It has virtually no effect on the autonomic nervous system and does not penetrate the central nervous system. Side effects: Feeling of heat, dizziness, arrhythmias, hypotension, palpitations, sweating (more often with parenteral administration), allergic dermatitis. Indications for use Spasm of smooth muscles of internal organs (cardio- and pylorospasm), chronic gastroduodenitis, peptic ulcer of the stomach and duodenum, cholelithiasis (hepatic colic), chronic cholecystitis, postcholecystectomy syndrome, hypermotor dyskinesia of the biliary tract, spastic intestinal dyskinesia, intestinal colic due to gas retention after surgery, colitis, proctitis, tenesmus, flatulence, urolithiasis (renal colic), pyelitis, spasm of cerebral vessels, coronary and peripheral arteries, the need to weaken uterine contractions and relieve cervical spasm during childbirth, smooth muscle spasm during childbirth time of instrumental interventions Contraindications Hypersensitivity, glaucoma. Overdose AV blockade, cardiac arrest, paralysis of the respiratory center. Interaction Enhances (especially with intravenous administration) the effect of other antispasmodics (including m-anticholinergics), hypotension caused by tricyclic antidepressants, quinidine, novocainamide. Phenobarbital increases the reliability of eliminating spasms. Reduces the spasmogenic activity of morphine and the antiparkinsonian properties of levodopa. Special instructions Restrictions on use. Prostate adenoma, severe atherosclerosis of the coronary arteries. Storage conditions List B. In a place protected from light at room temperature.
Dosage of the drug
Parents often ask questions: “Is it possible to give no-shpa to children? How much to give no-shpa to a child? How to give? According to the instructions for the drug, no-spa is used in children over 6 years of age. From 6 to 12 years it is recommended to take one tablet (40 mg) 1-2 times a day. In children over 12 years of age, it is possible to use one tablet (40 mg) 1-4 times a day.
As mentioned earlier, no-shpa is also used in children under 6 years of age (from 1 year). At the same time, doctors monitor the baby’s condition.
The optimal dosage regimen is determined by the attending physician. It is necessary to strictly observe the compliance of the dosage form of no-shpa with the indications for its use and dosage regimen.
It is necessary to strictly observe the indications for use and dosage regimen.
Other antispasmodics used in pediatrics
In addition to no-shpa, antispasmodics such as:
- Riabal. The active ingredient is profinium bromide. Riabal is the drug of choice in young children.
- Dicetel.
- Mebeverine.
- Papaverine.
No-spa is the most common antispasmodic. Like any other drugs, it has its own indications and contraindications. The advantage of this drug is the availability of oral and parenteral forms, which allow it to be used as emergency treatment for many conditions in children. Do not self-medicate; if your child experiences pain or discomfort, consult your pediatrician.
