No-Spa forte 80mg tab 10 pc

Description

Composition
Active substance:
1 tablet contains: drotaverine hydrochloride – 80 mg ;.
Excipients:
Magnesium stearate, talc, povidone, corn starch, lactose monohydrate.
Description:
Oblong biconvex tablets with a greenish yellow or orange shade, with the engraving “NOSPA” on one side and a fault line on the other side.
Product form:
Tablets 80 mg, Valium planimetric packaging.
Contraindications
Hypersensitivity to drotaverine and / or auxiliary substances included in the preparation.
Severe hepatic or renal failure.
Severe heart failure (decreased cardiac output).
Lactation (see. Section “Pregnancy and lactation”).
Children’s age (clinical trials in children has not been).
Hereditary lactose intolerance, lactase deficiency, galactosemia or malabsorption syndrome glucose / galactose (due to the presence of lactose in the composition preparation) (see. “Special instructions”).
Carefully:
If hypotension.
Pregnant women (see. Section “Pregnancy and lactation”).
Dosage
80 mg
Indications
Spasms of smooth muscle in diseases of the biliary tract: cholecystolithiasis, cholangiolithiasis, cholecystitis, pericholecystitis, cholangitis, an inflammation of duodenal papilla.
Spasms of smooth muscle in diseases of the urinary tract: nephrolithiasis, uretrolitiaz, pyelitis, cystitis, bladder spasms.
As an adjuvant therapy: with smooth muscle spasm of the gastrointestinal tract: gastric ulcer and duodenal ulcer, gastritis, gastric cardia and pyloric spasm, enteritis, colitis, spastic colitis, constipation and irritable bowel syndrome with bloating;
at tensor headaches (tension headaches);
when algodismenoree.
Interaction with other drugs
Since levodopa.
With simultaneous use of drotaverine may weaken the antiparkinsonian effect of levodopa, i.e., to increase rigidity and tremor.
With papaverine, bendazol and other antispasmodics (including with m-holinoblokatorami)
Strengthening antispasmodic action.
With morphine.
Decrease spazmogennoe morphine activity.
With phenobarbital.
Strengthening antispasmodic action Drotaverinum.
Overdose
Overdose Drotaverinum associated with cardiac arrhythmias and conduction, including a total blockade of legs bundle branch block and cardiac arrest, which can be fatal.
In case of overdose, patients should be under medical supervision and, if necessary, they should be carried out is symptomatic and aimed at maintaining the basic functions of the body treated.
pharmachologic effect
Pharmacological group:
Antispasmodic.
Pharmacodynamics:
Drotaverine represents an isoquinoline derivative, the chemical structure and pharmacological properties close papaverine, but having a stronger and prolonged action. Drotaverine has potent antispasmodic effect on smooth muscle by inhibiting the enzyme phosphodiesterase (PDE). Phosphodiesterase enzyme necessary for the hydrolysis of cAMP (cyclic adenosine-3`, 5`-monophosphate) to AMP (adenosine monophosphate 5`). Inhibition of the enzyme phosphodiesterase increases the concentration of cAMP, which triggers the following cascade reaction: high concentrations of cAMP activates cAMP-dependent phosphorylation of myosin light chain kinase (MLCK). Phosphorylation MLCK leads to a decrease of its affinity for Ca2 + -kalmodulinovomu complex, resulting in an inactivated form MLCK supports muscle relaxation. cAMP, in addition, effect on cytosolic Ca2 + ion concentration by stimulating transport Ca2 + into the extracellular space and sarcoplasmic reticulum. This effect of lowering drotaverine tsitozolnoi Ca2 + ion through cAMP explains its antagonistic effect with respect to Ca2 +.
In vitro drotaverin inhibits PDE IV isozyme without inhibiting PDE isoenzymes PDE III and V. Therefore drotaverine efficiency depends on PDE IV concentrations in tissues, the contents of which varies in different tissues. PDE IV is most important to inhibit the contractile activity of smooth muscle, and therefore the selective inhibition of PDE IV can be useful for the treatment of hyperkinetic dyskinesias and various diseases accompanied by spastic conditions of the gastrointestinal tract.
Hydrolysis of cAMP in the myocardium and vascular smooth muscle occurs mainly via isoenzyme PDE III, which explains the fact that at high spasmolytic activity in drotaverine no serious side effects of the heart and blood vessels and marked effects on the cardiovascular system.
Drotaverinum effective in spasms of smooth muscles of both neurogenic and muscular origin. Regardless of the type of the autonomic innervation of drotaverin relaxes the smooth muscles of the gastrointestinal tract, biliary tract, urinary tract, blood vessels.
Due to its vasodilating action Drotaverinum improves blood circulation.
Pharmacokinetics:
Compared with papaverine Drotaverinum when administered more quickly and more completely absorbed from the gastrointestinal tract. Absorption is 100%. However, after metabolic the “first pass through the liver” enters into the systemic circulation of 65% of the dose. Maximum plasma concentration (Cmax) is achieved after 45-60 minutes.
In vitro drotaverin it has a high bond to plasma proteins (95-97%), especially albumin, and y (b- globulins.
Drotaverinum evenly distributed in the body, it enters the smooth muscle cells. It does not cross the blood-brain barrier. Drotaverine and / or its metabolites can slightly penetrate the placenta.
The man Drotaverinum almost completely metabolized in the liver by 0-dezetilirovaniya. Its metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4′-dezetildrotaverin but which have been identified 6 dezetildrotaverin and 4′-dezetildrotaveraldin.
The half-life of drotaverine is 8-10 hours.
72 hours drotaverin almost completely excreted, over 50% of drug is excreted by the kidneys (mainly as metabolites) and about 30% through the gastrointestinal tract (excretion in bile). Drotaverinum unchanged in the urine is detected.
Pregnancy and breast-feeding
For a limited number of historical data on the drug administration in human and animal research data while taking into drotaverine received proof of his teratogenic or embryotoxic effect, as well as adverse effects on pregnancy. Despite this, when using the drug in pregnant women should be careful to prescribe a drug only after careful weighing of benefits and risks for the mother and the relationship of risk to the child.
Studies on excretion in breast milk Drotaverinum been conducted in animals. In the absence of such studies in animals and clinical data, assign Drotaverinum during lactation is not recommended.
Conditions of supply of pharmacies
Without recipe.
side effects
The following side effects in clinical studies that were regarded as at least possibly tied with drotaverin, are according to the following gradation frequency of occurrence: very often (> 1/10), often (> 1/100
special instructions
Use of the drug in patients with arterial hypotension requires increased caution.
Each tablet Nospanum forte contains 104 mg of lactose. At reception according to the recommended dosage regimen for each dose can come to 156 mg of lactose (1.5 tablets Nospanum forte), which may cause in patients suffering from lactose intolerance, disorders of the gastrointestinal tract. This form of product is unacceptable for patients with lactase deficiency, galactosemia or malabsorption syndrome glucose / galactose.
Effects on ability to drive and use other mechanisms
When administered in therapeutic doses of drotaverin did not affect the ability to drive and do work requiring attention. If you notice any side effects issue of driving vehicles or other lesson potentially dangerous activities require individual consideration. In case of vertigo should avoid activities potentially hazardous activities such as driving and operating machinery.
Storage conditions
Store at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
The drug is taken orally. Typically, the average daily dose is 120-240 mg (daily dose is divided into 2-3 doses).
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist