Instructions for use Drotaverin-Darnitsa tablets 40 mg No. 20
Composition
active ingredient: drotaverine;
1 tablet contains drotaverine hydrochloride 40 mg;
Excipients: lactose monohydrate, corn starch, microcrystalline cellulose, colloidal anhydrous silicon dioxide, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: tablets of light yellow or dark yellow color with inclusions, flat-cylindrical shape, with a bevel and a score.
Pharmacotherapeutic group
Drugs used for functional gastrointestinal disorders. ATX code A0ZA D02.
Pharmacological properties
Pharmacodynamics.
Drotaverine-Darnitsa is an isoquinoline derivative that has an antispasmodic effect on smooth muscles 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 muscles.
In vitro, drotaverine inhibits the action of the enzyme PDE IV and inhibits the isoenzymes phosphodiesterase III (PDE III) and phosphodiesterase V (PDE V). PDE IV has a great functional importance in 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.
Drotaverin-Darnitsa is effective in spasms of smooth muscles of both nervous and muscular origin. Drotaverin-Darnitsa acts on the smooth muscles of the gastrointestinal, biliary, genitourinary and vascular systems, regardless of the type of their autonomic innervation. The drug enhances blood circulation in the 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 blood plasma proteins. The advantage of drotaverine is also that, unlike papaverine, after its parenteral administration, there is no side effect such as respiratory stimulation.
Pharmacokinetics.
Drotaverine-Darnitsa 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 in the blood after oral administration is reached after 45-60 minutes. After primary metabolism, 65% of the dose enters the bloodstream unchanged. It is metabolized in the liver. The 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; unchanged form is not detected in the urine.
Indication
For therapeutic purposes in:
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 the 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 to other components of the drug; severe hepatic, renal or heart failure (small cardiac output syndrome).
Interaction with other medicinal products and other types of interactions
When used simultaneously with levodopa, the antiparkinsonian effect of the latter may be reduced. This combination should be used with caution, as the antiparkinsonian effect of levodopa is reduced and rigidity and tremor are increased.
Application features
The drug should be used with caution in cases of arterial hypotension.
Excipients.
Drotaverin-Darnitsa contains 64.0 mg of lactose monohydrate, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.
Drotaverine belongs to histamine-liberating drugs and can cause non-allergic (pseudo-allergic) reactions that do not have immunological mechanisms, but mimic allergic symptoms (the phenomenon of mimicry). They are usually associated with non-immune release of histamine, bradykinin, complement activation, induction of leukotriene synthesis, which in turn induces bronchospasm and skin manifestations. The drug should be prescribed with caution to patients with a history of allergic reactions or bronchial asthma. If symptoms of hypersensitivity reactions appear after taking drotaverine (rash, itching, swelling of the tissues of the upper respiratory tract), the drug should be immediately discontinued and therapy should be prescribed. In case of symptoms of angioedema or urticaria, oral antihistamines should be used.
If the patient is known to have asthma, administer an inhaled beta-2-agonist. The patient should be monitored for the next 4 hours. If there is persistent vomiting and/or abdominal pain, consider administering epinephrine intramuscularly.
Use during pregnancy or breastfeeding
Animal studies have shown that oral administration of drotaverine 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 using the drug during pregnancy.
Due to the lack of relevant research data, the use of the drug during breastfeeding is not recommended.
Ability to influence reaction speed when driving vehicles or other mechanisms
If patients experience dizziness after using the drug, they should avoid potentially hazardous activities, such as driving and performing work that requires increased attention.
Method of administration and doses
Drotaverin-Darnitsa is administered orally.
Adults: the average daily dose is 120-240 mg (3-6 tablets), divided into 2-3 doses.
Children aged 6-12 years: the maximum daily dose is 80 mg, divided into 2 doses.
Children over 12 years of age: the maximum daily dose is 160 mg, divided into 2-4 doses.
The duration of treatment is determined individually.
Children
The use of the drug is contraindicated in children under 6 years of age.
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.
Treatment: in case of overdose, the patient should be under close medical supervision and receive symptomatic treatment, including induction of vomiting and/or gastric lavage.
Side effects
Side effects observed during clinical trials and possibly caused by drotaverine are listed by system organ class 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).
Gastrointestinal: Rare: nausea, constipation, vomiting.
Nervous system: Rare: headache, dizziness, insomnia.
Cardiovascular system: Rare: palpitations, hypotension.
Immune system disorders: Rare: allergic reactions, including angioedema, urticaria, rash, itching, skin flushing, fever, chills, increased body temperature, weakness.
Expiration date
3 years.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store out of the reach of children in the original packaging at a temperature not exceeding 25 °C.
Packaging
10 tablets in a blister pack; 2 or 3 blister packs in a pack.
Vacation category
Without a prescription.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
