Instructions for No-Spa tablets 40 mg bottle No. 100
Composition
active ingredient: drotaverine;
1 tablet contains drotaverine hydrochloride 40 mg;
excipients: magnesium stearate, talc, povidone, corn starch, lactose monohydrate.
Dosage form
Pills.
Main physicochemical properties: convex tablets of yellow color with a greenish or orange tint; engraved with "spa" on one side.
Pharmacotherapeutic group: Drugs used in functional gastrointestinal disorders. ATC code: A03A D02.
Pharmacological properties
Pharmacodynamics
Drotaverine is an isoquinoline derivative that exerts an antispasmodic effect directly on smooth muscle by inhibiting the action of the enzyme phosphodiesterase IV (PDE IV), which causes an increase in the concentration of cAMP and, due to the inactivation of myosin light chain kinase (MLCK), leads to relaxation of smooth muscle.
In vitro, drotaverine inhibits the action of the enzyme PDE IV and does not affect the action of the isoenzymes phosphodiesterase III (PDE III) and phosphodiesterase V (PDE V). PDE IV is of great functional importance for reducing the contractile activity of smooth muscles, therefore, selective inhibitors of this enzyme may be useful for the treatment of diseases accompanied by hypermotility, as well as various diseases in which gastrointestinal spasms occur.
In myocardial and vascular smooth muscle cells, cAMP is hydrolyzed mainly by the PDE III isoenzyme, therefore drotaverine is an effective antispasmodic that does not have significant side effects on the cardiovascular system and has a strong therapeutic effect on this system.
Drotaverine is effective in smooth muscle spasms of both nervous and muscular origin. Drotaverine acts on the smooth muscles of the gastrointestinal, biliary, genitourinary and vascular systems, regardless of the type of their autonomic innervation.
It increases blood circulation in tissues due to its ability to dilate blood vessels.
The effect of drotaverine is stronger than that of papaverine, absorption is faster and more complete, it binds less to serum proteins. The advantage of drotaverine is also that, unlike papaverine, after its parenteral administration, there is no such side effect as respiratory stimulation.
Pharmacokinetics
Absorption. Drotaverine is rapidly absorbed both after oral administration and after parenteral administration.
Distribution: It is highly bound to plasma albumin (95-98%), alpha and beta globulins. Peak serum concentrations are reached within 45-60 minutes after oral administration.
Biotransformation. After primary metabolism, 65% of the administered dose enters the bloodstream unchanged. Metabolized in the liver.
Excretion. The half-life of biological existence is 8-10 hours. Within 72 hours, drotaverine is almost completely excreted from the body, more than 50% is excreted in the urine and approximately 30% in the feces. Drotaverine is mainly excreted in the form of metabolites, it is not detected in unchanged form in the urine.
Indication
Smooth muscle spasms associated with biliary tract diseases: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.
Spasms of smooth muscles in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder tenesmus.
As an adjunctive treatment:
- for spasms of smooth muscles of the gastrointestinal tract: gastric and duodenal ulcers, gastritis, cardio- and/or pylorospasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome accompanied by flatulence;
- tension headache;
- for gynecological diseases: dysmenorrhea.
Contraindication
Hypersensitivity to drotaverine or any component of the drug. Severe hepatic, renal or heart failure (small cardiac output syndrome).
Special safety measures.
Use with extreme caution in cases of arterial hypotension.
Each tablet of No-Spa contains 52 mg of lactose. Do not use in patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption.
Interaction with other medicinal products and other types of interactions
Phosphodiesterase inhibitors, such as papaverine, reduce the antiparkinsonian effect of levodopa. Caution should be exercised when No-Spa is used concomitantly with levodopa, as the antiparkinsonian effect of the latter is reduced and rigidity and tremor are increased.
Application features
Use with extreme caution in cases of arterial hypotension.
Each tablet of No-Spa contains 52 mg of lactose. Do not use in patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption.
Use during pregnancy or breastfeeding
Pregnancy: Retrospective clinical and animal studies have shown that oral administration of the drug does not indicate any direct or indirect harmful effects with respect to pregnancy, embryonic development, parturition or postnatal development. However, caution should be exercised when prescribing the drug to pregnant women.
Breastfeeding. Due to the lack of data, the use of the drug during breastfeeding is not recommended.
Fertility.
There are no data on the effect on human fertility.
Ability to influence reaction speed when driving vehicles or other mechanisms
If patients experience dizziness after using the drug, they should avoid potentially dangerous activities, such as driving a car and performing work that requires increased attention.
Method of administration and doses
Adults: the recommended dose is 120-240 mg per day in 2-3 doses.
Children: The use of drotaverine in children has not been studied in clinical trials; if the use of drotaverine is necessary, then:
for children aged 6-12 years, 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).
There is no data on the use of the drug in children under 6 years of age.
Before using No-Shpa tablets in the dosing container, it is necessary to remove the protective tape under the lid and the protective sticker on the bottom of the container.
Children
The use of the drug is contraindicated in children under 6 years of age.
Clinical studies on the use of the drug in children have not been conducted.
Overdose
Symptoms: with a significant overdose of drotaverine, cardiac rhythm and conduction disturbances have been observed, including complete bundle branch block and cardiac arrest, which can be fatal.
In case of overdose, the patient should be under close medical supervision and receive symptomatic treatment, including inducing vomiting and/or gastric lavage.
Adverse reactions
Adverse reactions observed during clinical trials and possibly caused by drotaverine are listed by system organ class and frequency: very common (> 1/10), common (> 1/100, < 1/10), uncommon (> 1/1000, < 1/100), rare (> 1/10000, < 1/1000), very rare (< 1/10000), frequency unknown: cannot be estimated from the available data.
Immune system disorders: Rare: allergic reactions, including angioedema, urticaria, rash, itching, skin flushing, fever, chills, increased body temperature, weakness.
Cardiovascular system: Rare: palpitations, hypotension.
Nervous system: Rare: headache, dizziness, insomnia.
Gastrointestinal: Rare: nausea, constipation, vomiting.
Expiration date
3 years.
Storage conditions
Keep out of reach of children.
Store in original packaging at a temperature below +25 °C.
Packaging
No. 12: 12 tablets in a blister, 1 blister in a cardboard box.
No. 24: 24 tablets in a blister, 1 blister in a cardboard box.
No. 60: 60 tablets in a dosing container, closed with a lid with a protective tape against opening, 1 dosing container in a cardboard box.
No. 100: 100 tablets in a bottle, 1 bottle in a cardboard box with a sticker on the box to control the first opening.
Vacation category
Without a prescription.
Manufacturers
Opel Helskea Hunger Kft.
Opel Helskea Poland Sp. with o.o.
Location of manufacturers and their business addresses
Levai 5, Veresedház, 2112, Hungary.
Lubelska St. 52, 35-233 Rzeszow, Poland.
Applicant
Opela Healthcare Ukraine LLC, Ukraine.
Location of the applicant and/or applicant's representative
Ukraine, 01033, Kyiv, Zhylyanska St., 48-50A.
