Instructions for No-Spa Forte 80 mg No. 10
Composition
active ingredient: drotaverine;
1 tablet contains drotaverine hydrochloride 80 mg;
excipients: magnesium stearate, talc, povidone, corn starch, lactose monohydrate.
Dosage form
Pills.
Main physicochemical properties: convex oblong tablets of yellow color with a greenish or orange tint; on one side there is a marking “NOSPA”, on the other side there is a dividing line.
The length of the tablet is approximately 13 mm, the width is approximately 6 mm, and the height is approximately 3.8 mm.
Pharmacotherapeutic group
Drugs used for functional gastrointestinal disorders. ATX code A0ZA D02.
Pharmacological properties
Pharmacodynamics
Drotaverine, an isoquinoline derivative, has an antispasmodic effect 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 inhibit 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.
The remedy enhances 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. Another advantage of drotaverine is that, unlike papaverine, after its parenteral administration, there is no side effect such as respiratory stimulation.
Pharmacokinetics
Drotaverine is rapidly and completely absorbed after oral administration. It is highly (95–98%) bound to plasma proteins, especially albumin, gamma- and beta-globulins. The maximum concentration is reached within 45–60 minutes after oral administration. After primary metabolism, 65% of the dose enters the bloodstream unchanged.
Metabolized in the liver. Half-life 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
For therapeutic purposes in:
smooth muscle spasms associated with biliary tract diseases: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;
smooth muscle spasms in urinary tract diseases: nephrolithiasis, ureterolithiasis, 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;
gynecological diseases (dysmenorrhea).
Contraindication
Hypersensitivity to drotaverine or any component of the drug. Severe hepatic or renal failure. Heart failure (low cardiac output syndrome).
Interaction with other medicinal products and other types of interactions
Phosphodiesterase inhibitors (NO-ShPA® forte, papaverine) reduce the antiparkinsonian effect of levodopa.
Caution should be exercised when using NO-SPA® forte simultaneously 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. Clinical studies with drotaverine in children have not been conducted.
One tablet of NO-ShPA® forte contains 104 mg of lactose. When used in accordance with the recommended doses, up to 156 mg of lactose may enter the body per dose, which may lead to gastrointestinal complaints in patients with lactose intolerance.
Do not use for the treatment of patients with lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome.
Use during pregnancy or breastfeeding
Retrospective clinical and animal studies have shown that oral administration of the drug does not cause any indication of 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.
Due to the lack of relevant research data, the use of the drug during breastfeeding is not recommended.
Fertility
There is no information on the effect on human fertility.
The ability to influence the reaction speed when driving or working with other mechanisms
If dizziness occurs after using the drug, you should avoid driving a car and performing work that requires increased attention.
Method of administration and doses
The NO-ShPA® forte tablet can be divided in half.
Adults: The usual average dose is 120–240 mg per day in 2–3 divided doses.
Children over 12 years of age: if necessary, as prescribed by a doctor, the maximum daily dose is 160 mg (1/2 tablet 2–4 times a day).
The duration of treatment is determined by the doctor individually.
Children
The use of the drug for the treatment of children under 12 years of age is contraindicated. The use of drotaverine in children has not been evaluated in clinical studies.
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 closely monitored by a physician and receive symptomatic and supportive treatment. It is recommended to induce vomiting and/or perform gastric lavage.
Side effects
Side effects observed during clinical studies and possibly caused by drotaverine are distributed by organ system and frequency of occurrence: very common (> 1/10), common (> 1/100, <1/10), uncommon (> 1/1000, <1/100), rare (> 1/10000, <1/1000), very rare (<1/10000).
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 the original packaging at a temperature not exceeding 25 °C.
Packaging
No. 10: 10 tablets in a blister, 1 blister in a cardboard box.
No. 24: 24 tablets in a blister, 1 blister in a cardboard box.
Vacation category
Without a prescription.
Producer
Opel Helskea Hungeri Kft.
Opel Helskea Poland Sp. with o.o.
Location of manufacturers and addresses of their places of business.
Levai 5, Veresedház, 2112, Hungary.
Lubelska St. 52, 35-233 Rzeszow, Poland.
Applicant
Opela Healthcare Ukraine LLC, Ukraine.
Location of the applicant and/or the applicant's representative.
Ukraine, 01033, Kyiv, Zhylyanska St., 48-50A.
