No-shpa - instructions for use, doses, side effects, contraindications

Drotaverin is a derivative of isoquinoline, which exhibits a powerful spasmolytic effect on smooth muscle by inhibiting the enzyme, phosphodiesterase (PDE). The enzyme phosphodiesterase is necessary for the hydrolysis of cyclic adenosine monophosphate (cAMP) to adenosine monophosphate (AMP). Inhibition of the enzyme phosphodiesterase leads to an increase in the concentration of cAMP; which triggers the next cascade reaction: high concentrations of cAMP activate cAMP^g dependent phosphorylation of light chain kinos of myosin (CMLC). Phosphorylation of CMLC leads to a decrease in its affinity, to Ca²⁺- kalmodulin - complex, as a result of which the inactivated form of CLCM supports muscular relaxation. cAMP Besides this affects. cytosolic the concentration of the Ca²⁺ thanks to stimulating transport of Sa²⁺ at extracellular space and sarcoplasmic reticulum. This lowering ion concentration Ca²⁺ the effect of drotaverin through cAMP explains the antagonistic effect of drotaverine in relation to Ca²⁺.

In vitro drotaverin inhibits the isoenzyme PDE IV without inhibiting the isoenzymes PDE III and PDE V. Therefore, the effectiveness of drotaverin depends on the concentration of PDE IV in tissues, the content of which differs in different tissues. PDE IV is most important for suppressing the contractile activity of smooth muscle, and therefore selective inhibition of PDE IV can be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by the spastic state of the gastrointestinal tract. The hydrolysis of cAMP in the myocardium and smooth musculature of the vessels occurs, mainly,with the help of the isoenzyme PDE III, which explains the fact that at high spasmolytic activity in drotaverin there are no serious side effects from the heart and vessels and the expressed effects on the cardiovascular system.

Drotaverine is effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of vegetative, innervation, drotaverine relaxes, smooth muscles, gastrointestinal tract, biliary tract, urogenital system.

Pharmacokinetics:

Absorption: After ingestion, drotaverine quickly and completely absorbed. After pre-systemic metabolism, 65% of the dose of drotaverine is administered to the systemic blood supply. The maximum plasma concentration (C_max) is reached in 45-60 minutes.

Distribution:

In vitro drotaverin has a high association with plasma proteins, (95-98%), especially with albumin and y and in - globulins.

Drotaverin is evenly distributed among the tissues, penetrates into the smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites can penetrate insignificantly through the placental barrier.

Metabolism:

In humans drotaverine almost completely metabolized in the liver by O-de-ethylation. Its metabolites are rapidly conjugated to glucuronic acid.

The main metabolite is 4-desethyltraderin, in addition to which 6-deethyldrothavirin and 4-desethyltrodeterin were identified.

Excretion:

In humans, a two-chamber mathematical model was used to evaluate the pharmacokinetics of drotaverin. The final half-life of plasma radioactivity was 16 hours.

Within 72 hours, drotaverine almost completely eliminated from the body. More than 50% of drotaverin is excreted by the kidneys and about 30% through the gastrointestinal tract (excretion in bile). Drotaverine mainly excreted in the form of metabolites, unchanged drotaverine in the urine is not found.

Indications:

Spasms of smooth muscles with diseases of the bile ducts: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, papillitis.

Spasms of smooth muscles of the urinary tract: nephrolithiasis, urethrolithiasis, pyelitis, cystitis, bladder spasms.

As an auxiliary therapy

With spasms of smooth muscles of the gastrointestinal tract: ulcerative, stomach and duodenal ulcer, gastritis / spasm of cardia and pylorus, enteritis, colitis, spastic, colitis with constipation and irritable bowel syndrome with flatulence after exclusion of diseases manifested by the syndrome of "acute abdomen" ( appendicitis, peritonitis, perforation of the ulcer, acute pancreatitis, etc.).

With headaches, tension.

When dysmenorrhea.

Contraindications:

Hypersensitivity to the active ingredient, or to any of the excipients of the drug.

Severe hepatic or renal insufficiency.

Severe heart failure (low cardiac output syndrome).

Children under 6 years.

Breastfeeding period (lack of clinical data).

Rare inherited intolerance to galactose, lactase deficiency and glucose-galactose malabsorption syndrome (due to presence in the formulation of lactose).

Carefully:

With arterial hypotension.

In children (lack of clinical experience of use).

In pregnant women (see the section "Pregnancy and lactation period").

Pregnancy and lactation:

Pregnancy and lactation

As shown by reproductive studies in animals and retrospective data on the clinical use of drotaverine, the use of drotaverine during pregnancy had neither teratogenic nor embryotoxic effects. Despite this, when applying the drug during pregnancy, the potential benefit to the mother and the possible risk to the fetus should be correlated.

Due to the lack of necessary clinical data, during the lactation period, it is not recommended to prescribe.

Dosing and Administration:

Adults

Usually, the average daily dose in adults is 120-240 mg (the daily dose is divided into 2-3 doses). The maximum single dose is 80 mg. The maximum daily dose is 240 mg.

Children

Clinical studies using drotaverine with the participation of children have not been conducted.

In the case of administering drotaverine to children:

- for children from 6 to 12 years, the maximum, daily dose is 80 mg divided into 2 divided doses.

- for children over 12 years of age, the maximum daily dose is 160 mg, divided into 2-4 admission.

Duration of treatment without consulting a doctor

When you receive preparation without consulting with a doctor the recommended duration, taking the drug is usually 1-2 days.If during this period the pain syndrome does not decrease, the patient should consult a doctor to clarify the diagnosis and, if necessary, change the therapy. In cases where drotaverine Used, as an auxiliary therapy, the duration of treatment without consulting a doctor can be longer (2-3 days).

When using a bottle with a polyethylene stopper equipped with a unit dispenser: Before use, remove the protective strip from the top of the vial and sticker from the bottom of the vial. Place the bottle in the palm of your hand in such a way that the metering hole on the bottom does not rest on the palm of your hand. Then press on top of the vial, as a result of which one tablet will drop out of the metering hole on the bottom.

Method for evaluating effectiveness

If the patient can easily diagnose the symptoms of their disease, as they are well known to him, then the effectiveness of treatment, namely the disappearance of pain, is also easily evaluated by the patient. If, within a few hours after taking the maximum single dose, there is a moderate reduction in pain or no pain reduction,or if the pain does not decrease significantly after taking the maximum daily dose, it is recommended to consult a doctor.

Side effects:

Below are the adverse reactions observed in clinical trials, divided by systems, organs, indicating the frequency of their occurrence in accordance with the following grades: very frequent (> 10%), frequent (> 1%, <10); infrequent (> 0,1%, <1%); rare (> 0.01%, <0.1%) and very rare, including individual messages (<0.01%), unknown frequency (according to the available data, the frequency can not be determined).

From the side of the cardiovascular system

Rare - increased heart rate, lower blood pressure.

From the nervous system

Rare - headache, dizziness, insomnia.

From the gastrointestinal tract

Rare - nausea, constipation

From the immune system

Rare - allergic reactions (angioedema, urticaria, rash, itching) (see section "Contraindications").

Overdose:

Overdose of drotaverine was associated with cardiac rhythm and conduction disorders, including complete blockade of the legs of the fasciculus and cardiac arrest, which can be fatal.

In case of an overdose, patients should be under medical supervision; and if necessary they should be symptomatic and aimed at maintaining the basic functions of the body treatment, including artificial vomiting or gastric lavage.

Interaction:

FROM levodopa

Phosphodiesterase inhibitors like papaverine reduce antiparkinsonian action levodopa. When administering drotaverine concomitantly with levodopa, there may be an increase in rigidity and tremor.

FROM other antispasmodic agents, including m-holinoblokatory

Mutual increase of spasmolytic effect.

Drugs that significantly bind to plasma proteins (more than 80%)

Drotaverine significantly bind to plasma proteins, mainly albumin, y-globulin and p (cm. "Pharmacokinetics" section).

No data on the interaction of drotaverine with drugs significantly bind to plasma proteins, but there is a hypothetical possibility of their interaction with the drotaverine-level communication with the protein (the displacement of one of the drugs other of the linkages to the protein and increasing the concentration of the free fraction of drug in the blood with less severe; bond with protein),which hypothetically may increase the risk of pharmacodynamic and / or toxic side effects of this drug.

Special instructions:Tablets No-shpa® 40 mg contain 52 mg of lactose. This can cause gastrointestinal complaints in persons suffering from intolerance to lactose. This form is unacceptable for patients suffering from lactose deficiency, galactosemia, or glucose / galactose impairment syndrome (see the "Contraindications" section).

Effect on the ability to drive transp. cf. and fur:

When administered orally in therapeutic doses drotaverine does not affect the ability to drive and perform work requiring increased attention. If any side effects occur, the issue of driving and working with machinery requires individual consideration.

In the case of dizziness after taking the drug, you should avoid engaging in potentially hazardous activities such as driving and working with machinery.

Form release / dosage:Tablets of 40 mg.

Packaging:By 6, 10, 12, 20 or 24 pills in a blister PVC / Aluminum.
For 1, 2, 4 or 5 blisters for 6 tablets with instructions for use in a cardboard box.
3 blisters for 10 tablets with instructions for use in a cardboard box.
2 blisters with 12 tablets each with instructions for use in a cardboard box.
By 1 blister to 20 or 24 tablets with instructions for use in a cardboard box.
10 tablets per blister Aluminum / Aluminum (laminated polymer).
2 blisters with instructions for use in a cardboard box.
For 60 tablets per vial of polypropylene with polyethylene stopper, equipped with a unit dispenser.
1 bottle with instructions for use in a cardboard box.
100 tablets per bottle of polypropylene with polyethylene stopper.
1 bottle with instructions for use in a cardboard box.

Storage conditions:

For tablets in blisters Aluminum / Aluminum: Store at temperatures not exceeding 30 ° C.

For tablets in PVC blisters / Aluminum: Store at a temperature of no higher than 25 ° C. For tablets in vials: Store in a dark place at a temperature of 15 ° C to 25 ° C.

Keep out of the reach of children.

Shelf life:

For tablets in blisters Aluminum / Aluminum: 5 years.

For tablets in PVC blisters / Aluminum: 3 years.

For tablets in vials: 5 years.
Do not use the drug after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N011854 / 02

Date of registration:23.07.2010 / 28.03.2016

The owner of the registration certificate:HINOIN Pharmaceutical and Chemical Products Plant, ZAO HINOIN Pharmaceutical and Chemical Products Plant, ZAO Hungary

Manufacturer: & nbsp

CHINOIN Pharmaceutical and Chemical Works, Co. Ltd. Hungary

Representation: & nbspSanofi Russia, JSCSanofi Russia, JSCRussia

Information update date: & nbsp05.07.2013

Illustrated instructions

Instructions

No-spa® (No-Spa®)