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Drotaverine-Darnitsa

Drugs for functional gastrointestinal disorders

PACKAGE LEAFLET

for medical use of a medicinal product

DROTADAR-DARNITSA

Qualitative and quantitative composition:

Active substance: drotaverine;

1 tablet contains drotaverine hydrochloride 40 mg;

Excipients: lactose monohydrate, maize starch, cellulose microcrystalline, silica colloidal anhydrous, magnesium stearate.

Pharmaceutical form Tablets.

Basic physical and chemical properties: light yellow or dark yellow with inclusion, flat bevel-edged tablets with a score line on one side.

Pharmacotherapeutic group

Drugs for functional gastrointestinal disorders. Papaverine and derivatives. ATC code А03AD02.

Pharmacological properties

Pharmacodynamic properties

Drotadar-Darnitsa, is a isoquinoline derivative that has a spasmolytic effect on smooth muscles by inhibiting the action of the enzyme phosphodiesterase IV (PDE IV), which leads to an increased concentration of cAMP and, due to the inactivation of myosin kinase light chain (MLCK), to the relaxation of smooth muscles.

In vitro, drotaverine inhibits the action of the PDE ІV enzyme and the phosphodiesterase III (PDE III) and phosphodiesterase V (PDE V) isoenzymes. PDE IV is functionally very important for reducing the contractility of smooth muscles, therefore selective the enzyme inhibitors can be effective fin the treatment of hyperkinetic diseases and different diseases associated with spastic conditions of the gastrointestinal tract.

In the smooth muscle cells of the myocardium and vessels, cAMP is hydrolyzed to a greater extent by the PDE III isoenzyme, therefore, drotaverine is an effective antispasmodic in the absence of a significant adverse effects on the cardiovascular system and a strong therapeutic effect on the system. Drotadar-Darnitsa is effective in spasms of smooth muscles of both nervous and muscular etiology. Regardless of the type of autonomous innervation, Drotadar-Darnitsa acts on the smooth muscles of the gastrointestinal, biliary, urogenital and vascular systems. The medicinal product enhances blood supply to the tissues due to its ability to expand the vessels.

Action of drotaverine is stronger than papaverine. Absorption is faster and more complete. It is less associated with plasma proteins. The advantage of drotaverine is that, unlike papaverine, there is no such adverse effect as stimulation of breathing after its parenteral administration.

Pharmacokinetic properties

Drotadar-Darnitsa is rapidly and completely absorbed after oral administration. It binds highly (95- 98 %) to plasma proteins, especially albumin, gamma and beta globulins. The maximum concentration in the blood after oral administration is reached within 45−60 minutes. 65 % of the administrated dose is released into the bloodstream in unchanged form after the primary metabolism. It is metabolized in the liver. The half-life of drotaverine is 8−10 hours. In 72 hours drotaverine is almost completely excreted from the body, more than 50 % is excreted in the urine and about 30 % with the feces. Basically, drotaverine is excreted in the form of metabolites and it is not found unchanged in the urine.

Clinical particulars

Therapeutic indications

For therapeutic purposes with:

spasms of smooth muscles associated with diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis;

spasms of smooth muscles in diseases of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, tenesmus of the bladder.

As an adjunct treatment for:

spasms of the smooth muscles of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, cardio and/or pylorospasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome, accompanied by flatulence;

tension headache;

gynecological diseases (dysmenorrhea).

Contraindications

Hypersensitivity to drotaverine or to any excipient of the medicinal product; severe hepatic, renal or heart failure (low cardiac output syndrome).

Interaction with other medicinal products and other forms of interaction

With the simultaneous use of the drug with levodopa it may decrease antiparkinsonic effect of the latter. This combination should be used with caution, since the antiparkinsonian effect of levodopa is reduced, and the rigidity and the tremor are intensified.

Special warnings and precautions for use

The drug is used with caution in case of arterial hypotension.

Excipients

Drotadar-Darnitsa contains 64.0 mg of lactose monohydrate, therefore, the medicinal product is not prescribed to patients with rare hereditary forms of intolerance to galactose, lactase deficiency or glucose-galactose malabsorption syndrome.

Hypersensitivity reactions

Drotaverine is a histamine liberator and it can cause non-allergic (false allergic) reactions that have no immunological mechanisms, but mimic allergic symptoms (mimicry). They are usually associated with non-immune release of histamine, bradykinin, activation of the compliment, induction of the synthesis of leukotrienes, which in turn induces bronchospasm and skin manifestations. The medicinal product should be carefully prescribed to patients with a history of allergic reactions or asthma. If you experience symptoms of hypersensitivity after taking drotaverine (rash, itching, swelling of the tissues of the upper respiratory tract), you should immediately cancel the medicinal product and prescribe therapy. In case of symptoms of angioedema or urticaria, oral antihistamines should be used.

If it is known about asthma in a patient, use an inhaled beta-2-agonist. It is necessary to monitor the patient for the next 4 hours. If there is continuous vomiting and/or abdominal pain, the possibility of administering epinephrine intramuscularly should be considered.

Fertility, pregnancy and lactation

Pregnancy

Results of animal studies have shown that oral administration of drotaverine did not rise to any direct or indirect effect on pregnancy, embryonic development, childbirth, or postpartum development. However, it is necessary to use the drug with caution during pregnancy.

Breastfeeding

Due to the lack of necessary clinical data, it is not recommended to administer medicinal product during breastfeeding.

Effects on ability to drive and use machines

If dizziness is observed in patients after using the medicinal product, they should refrain from potentially hazardous activities, such as driving and doing work that requires increased attention.

Posology and method of administration

Drotadar-Darnitsa is intended for oral administration.

Adults: the average daily dose is 120−240 mg (3−6 tablets), divided into 2−3 doses.

Children 6−12 years old: the maximum daily dose is 80 mg, divided into 2 doses. Children over 12 years old: the maximum daily dose is 160 mg, divided into 2−4 doses. The duration of treatment is determined individually.

Children

Administration of the medicinal product is contraindicated for children under 6 years old. Use of drotaverine for children has not been evaluated in clinical trials.

Overdose

Symptoms: with a significant overdose of drotaverine, cardiac rhythm and conduction disorders were observed, including a complete blockade of the Gis beam and cardiac arrest, which can be lethal.

Treatment: in case of overdose, the patient should be under the close medical supervision and receive symptomatic and supportive treatment, including induction of vomiting and/or gastric lavage.

Undesirable effects

The undesirable effects observed during clinical trials and may have been caused by drotaverine distributed to organs and the frequency of occurrence: very often (>1/10), common (>1/100< 1/10), uncommon (>1/1000, <1/100), rare (>1/10000, <1/1000), very rare (<1/10000).

Gastrointestinal disorders. Rarely: nausea, vomiting, constipation. Nervous system disorders. Rarely: headache, dizziness, insomnia. Cardiac disorders. Rarely: rapid heartbeat, hypotension.

Immune system disorders. Rarely: allergic reactions, including angioedema, urticaria, skin rash, itching, skin flushing, fever, chills, weakness.

Shelf life

3 years.

Special precaution for storage

Store in the original package at temperature not above 25 °C. Keep out of reach of children.

Nature and contents of container

10 tablets in a blister; 3 blisters in a pack.

Category of release

Non-prescription medicine.

Manufacture

PrJSC “Pharmaceutical firm “Darnitsa”.

The manufacturer's location and address of the place of business

13, Boryspilska Street, Kyiv, 02093, Ukraine.

Date of revision of the text

13.10.2017.

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Drotaverine-Darnitsa is an isoquinoline derivative that exerts antispasmodic action on smooth muscle via inhibition of phosphodiesterase–4 (PDE4), resulting in an increase in the cAMP concentration and leading to smooth muscle relaxation due to inactivation of the myosin light chain kinase (MLCK). In vitro, drotaverine suppresses the action of PDE4 and inhibits isoenzymes phosphodiesterase-3 (PDE3) and phosphodiesterase-5 (PDE5).

For the treatment of:

– Smooth muscle spasms in the biliary tract diseases: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis
– Smooth muscle spasms in the urinary tract diseases: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, vesical tenesmus

As an adjuvant treatment in:

– Smooth muscle spasms in the gastrointestinal tract diseases: gastric and duodenal ulcers, gastritis, cardio- and/or pylorospasm, enteritis, colitis, spastic colitis with constipation and irritable bowel syndrome with flatulence
– Stress headache
– Gynecological diseases (dysmenorrhea)

Drotaverine-Darnitsa is intended for internal use.

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 aged over 12 years: the maximum daily dose is 160 mg divided into 2–4 doses.

The duration of the treatment course should be determined on an individual basis.

Specialized edition for medical institutions and doctors.