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.
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.
Almont, 98 pcs., 5 mg, chewable tablets
In patients concomitantly receiving phenobarbital, the AUC of montelukast decreased by approximately 40%, but no dosage adjustment is required in such patients.
Since montelukast is metabolized by CYP3A4, caution should be exercised, especially in children, if montelukast is co-administered with CYP3A4 inducers such as phenytoin, phenobarbital and rifampicin.
Montelukast can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma and/or allergic rhinitis.
Montelukast at the recommended therapeutic dose did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethinodrel 35/1), terfenadine, digoxin and warfarin.
in vitro studies
Montelukast has been found to be a strong inhibitor of the CYP2C8 isoenzyme.
However, when studying the in vivo
between montelukast and rosiglitazone (a marker substrate, a representative of drugs primarily metabolized by the CYP2C8 isoenzyme), no confirmation of inhibition of the CYP2C8 isoenzyme by montelukast was obtained. Thus, in clinical practice, the effect of montelukast on CYP2C8-mediated metabolism of a number of drugs, incl. paclitaxel, rosiglitazone, repaglinide.
In vitro studies
showed that montelukast is a substrate of the CYP2C8 isoenzyme, and to a lesser extent, the CYP2C9 and 3A4 isoenzymes. Data from a clinical drug interaction study regarding montelukast and gemfibrozil (an inhibitor of both CYP2C8 and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times.
Co-administration of itraconazole, a strong inhibitor of the CYP3A4 isoenzyme, with gemfibrozil and montelukast did not lead to an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic exposure of montelukast may not be considered clinically significant based on safety data when used at doses greater than the approved dose of 10 mg in adults (eg, 200 mg/day in adults for 22 weeks and up to 900 mg/day in patients taking the drug for approximately 1 week, no clinically significant negative effects were observed). Thus, when co-administered with gemfibrozil, no dose adjustment of montelukast is required.
Based on in vitro
, no clinically significant drug interactions are expected with other known inhibitors of the CYP2C8 isoenzyme (for example, trimethoprim).
In addition, coadministration of montelukast with itraconazole alone did not significantly increase the effect of systemic exposure to montelukast.
Combination treatment with bronchodilators
Almont is a reasonable addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. After achieving a therapeutic effect from treatment with Almont, you can begin to gradually reduce the dose of bronchodilators.
Combined treatment with inhaled corticosteroids
Treatment with Almont provides an additional therapeutic effect in patients using inhaled corticosteroids. Once the condition has stabilized, you can begin to gradually reduce the dose of GCS under the supervision of a physician. In some cases, complete abolition of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Almont is not recommended.
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.
Oral tablets Zaditen
Instructions for medical use of the drug
Description of pharmacological action
Stabilizer of mast cell membranes, has moderate H1-histamine-blocking activity, suppresses the release of histamine, leukotrienes from basophils and neutrophils, reduces the accumulation of eosinophils in the respiratory tract and the reaction to histamine, suppresses early and late asthmatic reactions to the allergen. Prevents the development of bronchospasm, does not have a bronchodilator effect. Inhibits PDE, resulting in an increase in cAMP content in adipose tissue cells. The therapeutic effect is fully manifested after 1.5-2 months from the start of therapy.
Indications for use
Prevention of allergic diseases: atopic bronchial asthma, allergic bronchitis, hay fever, allergic rhinitis, allergic dermatitis, urticaria, allergic conjunctivitis.
Release form
Tablets 1 mg; pack 30; Tablets 1 mg; blister contour packaging 10 box (box) 3;
Pharmacodynamics
Inhibits the release of histamine and other mediators (slowly reacting substance of anaphylaxis, lymphokines, etc.) from mast cells and basophils. Non-competitively blocks H1-histamine receptors, inhibits phosphodiesterase, increases the level of cAMP in cells. Suppresses the sensitization of eosinophils by recombinant human cytokines and their accumulation in the respiratory tract. Prevents the development of symptoms of airway hyperresponsiveness caused by platelet activating factor or exposure to allergens. Prevents the development of bronchospasm (does not have a bronchodilator effect). The clinical effect develops after 6–8 weeks. Depresses the central nervous system.
Pharmacokinetics
After oral administration, it is absorbed almost completely. Bioavailability is approximately 50%, due to the “first pass” effect through the liver. The time to reach Cmax in plasma is 2–4 hours, binding to plasma proteins is 75%. Passes through the BBB and passes into breast milk. Metabolized in the liver; the main metabolite (ketotifen-N-glucuronide) is practically inactive. Excretion from the body occurs in two phases: with T1/2 3–5 hours and 21 hours, respectively. Within 48 hours, the main part of the dose taken is excreted in the urine: 1% unchanged and 60–70% in the form of metabolites.
Use during pregnancy
Contraindicated. FDA category of effect on the fetus is C. Breastfeeding should be discontinued during treatment.
Contraindications for use
Hypersensitivity, pregnancy, lactation. With caution. Epilepsy, liver failure.
Side effects
From the nervous system: drowsiness, dizziness, slow reaction speed (disappear after a few days of therapy), sedation, feeling of fatigue; rarely - anxiety, sleep disturbances, nervousness (especially in children). From the digestive system: dry mouth, increased appetite, nausea, vomiting, gastralgia, constipation. Urinary disorders: dysuria, cystitis. Other: thrombocytopenia, weight gain, allergic skin reactions.
Directions for use and doses
Orally, during meals, adults - 1 mg 2 times a day in the morning and evening. If necessary, the dose is increased to 2 mg 2 times a day. The duration of treatment is at least 3 months. Cancellation of therapy is carried out gradually, over 2-4 weeks.
Overdose
Symptoms: drowsiness, confusion, disorientation, bradycardia or tachycardia, decreased blood pressure, shortness of breath, cyanosis, convulsions, increased excitability, coma. Treatment: gastric lavage (if a little time has passed since administration), symptomatic treatment, with the development of convulsive syndrome - short-acting barbiturates and benzodiazepines. Dialysis is ineffective.
Interactions with other drugs
Strengthens the effect of sleeping pills, antihistamines, ethanol. In combination with hypoglycemic drugs, the likelihood of developing thrombocytopenia increases.
Precautions for use
Not intended to relieve an attack of bronchial asthma. It is not recommended to immediately cancel previous therapy with beta-agonists, glucocorticoids, ACTH (cancellation is carried out for at least 2 weeks, gradually reducing the dose). Use with caution while working for vehicle drivers and people whose profession involves increased concentration. In patients concomitantly receiving oral hypoglycemic agents, the platelet count in the peripheral blood should be monitored.
Special instructions for use
Abrupt cancellation of previous treatment with beta-adrenergic stimulants, corticosteroids, ACTH in patients with bronchial asthma and bronchospastic syndrome after joining ketotifen therapy is undesirable; cancellation is carried out for at least 2 weeks, gradually reducing the dose. Treatment is stopped gradually, over 2-4 weeks (relapse of asthmatic symptoms is possible). For persons sensitive to sedation, the drug is prescribed in small doses in the first 2 weeks. Not intended to relieve an attack of bronchial asthma. In patients simultaneously receiving oral hypoglycemic drugs, the number of platelets in the peripheral blood should be monitored. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Storage conditions
List B.: At a temperature not exceeding 25 °C.
Best before date
24 months
ATX classification:
R Respiratory system
R06 Antihistamines for systemic use
R06AX Other antihistamines for systemic use
R06AX17 Ketotifen
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.
