No-spa Duo pills 40mg + 500mg, 12pcs

Composition

Active ingredients: Drotaverine hydrochloride-40.0 mgParacetamol-500 mg Excipients: corn starch, pregelatinized krazmal, yellow quinoline dye, sodium carboxymethyl starch, magnesium stearate, talc, microcrystalline cellulose PH-102.

Pharmacological action

Pharmacotherapeutic group: Combined analgesic agent (non-narcotic analgesic agent+antispasmodic agent)ATX: N. 02. B. E. 51 Paracetamol in combination with other drugs, excluding psycholeptics Pharmacodynamics :

A combined drug, the action of which is due to the components included in its composition.

Drotaverine is an isoquinoline derivative that has an antispasmodic effect on smooth muscles (inhibition of the enzyme phosphodiesterase IV, an increase in the concentration of cAMP, which, by inactivating the enzyme myosin kinase, leads to relaxation of smooth muscles). Drotaverine also has a weak inhibitory effect on calmodulin-dependent calcium channels. Regardless of the type of autonomic innervation, drotaverine is effective in treating smooth muscle spasms. It acts on smooth muscles located in the vascular, gastrointestinal, biliary and urogenital systems (the content of phosphodiesterase IV in different tissues is different).

Paracetamol has analgesic and antipyretic effects mainly by inhibiting the synthesis of prostaglandins in the central nervous system. In inflamed tissues, cellular peroxidases neutralize the action of paracetamol, which explains the almost complete absence of an anti-inflammatory effect. The absence of a blocking effect on Pg synthesis in peripheral tissues causes paracetamol to have no negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa.

Pharmacokinetics:

Paracetamol is rapidly absorbed in the gastrointestinal tract and distributed to most organs and tissues. Absorption is high, the time to reach the maximum concentration is reached in 0.5-2 hours; the maximum concentration is 5-20 mcg / ml. Binding to plasma proteins is 15%. Penetrates the blood-brain barrier. Less than 1% of the dose of paracetamol taken by a nursing mother passes into breast milk.

It is metabolized in the liver (90-95%): 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which conjugate with glutathione to form already inactive metabolites. When glutathione is deficient, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The CYP2E1 isoenzyme is also involved in drug metabolism.

The elimination half-life is 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% – in unchanged form.

In elderly patients, the clearance of the drug decreases and the half-life increases.

Drotaverine when taken orally is rapidly and almost completely absorbed, absorption is high, the semi-absorption period is 12 minutes. Bioavailability – 100%. Evenly distributed in the tissues, penetrates into smooth muscle cells.

Time to reach the maximum concentration is 2 hours.

Binding to plasma proteins is 95-98%.

The elimination half-life is 1-4 hours. It is mainly excreted by the kidneys, to a lesser extent – with bile.

It does not cross the blood-brain barrier.

Indications

Pain syndrome of mild to moderate intensity (tooth and headache, joint and muscle pain, neuralgia, algodismenorrhea), caused, among other things, by spasms of smooth muscles of internal organs (renal colic, biliary colic, biliary dyskinesia and gallbladder hyperkinetic type, intestinal colic, spastic constipation, spastic colitis, tenesmus).

Use during pregnancy and lactation

Contraindicated.

Contraindications

Hypersensitivity; severe renal and hepatic insufficiency; severe chronic heart failure (NYHA functional class III-IV), grade II-III atrioventricular block, cardiogenic shock; respiratory failure, bronchial asthma; chronic alcoholism; blood diseases (thrombocytopenia, leukopenia, agranulocytosis); glucose-6-phosphate dehydrogenase deficiency; intracranial hypertension; concomitant use of other medications, treatment with monoamine oxidase inhibitors (and for another 14 days after their withdrawal); pregnancy and lactation; children under 6 years of age. With caution: With caution, it is prescribed to patients with benign hyperbilirubinemia (Gilbert’s syndrome), patients with atrioventricular block of the first degree, as well as the elderly.

Side effects

From the central nervous system (usually develops when taking high doses):  dizziness, headache, drowsiness.

From the cardiovascular system:  hypotension, arrhythmia, tachycardia, hot flashes.

From the digestive system: nausea, constipation, rarely (with high doses) – toxic liver damage.

From the side of the hematopoietic organs: with prolonged use in large doses – aplastic anemia, agranulocytosis, thrombocytopenia.

Allergic reactions: skin rash, very rarely – bronchospasm, swelling of the nasal mucosa.

Interaction

Drotaverine reduces the effect of levodopa (tremor and rigidity may increase).

The combined use of paracetamol with chloramphenicol increases the half-life of chloramphenicol and increases its toxicity.

Concomitant use of paracetamol with doxyrubicin increases the risk of developing liver function disorders.

Paracetamol reduces the effect of uricosuric drugs. Metoclopramide and domperidone enhance the absorption of paracetamol, while colestyramine reduces it. Concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (reduced synthesis of procoagulant factors in the liver). Inducers of microsomal oxidation in the liver (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which causes the possibility of severe intoxication even with a small overdose.

Long-term use of barbiturates reduces the effectiveness of paracetamol.

Ethanol contributes to the development of acute pancreatitis.

Microsomal oxidation inhibitors (including cimetidine) reduce the risk of hepatotoxic effects.

Long-term, combined use of paracetamol and other non-specific anti-inflammatory drugs increases the risk of developing” analgesic ” nephropathy and renal papillary necrosis, the onset of end-stage renal failure.

Concomitant long-term use of high-dose paracetamol and salicylates increases the risk of developing kidney or bladder cancer.

Diflunisal increases the plasma concentration of paracetamol by 50% – the risk of developing hepatotoxicity.

Myelotoxic drugs increase the manifestations of paracetamol hematotoxicity.

How to take, course of use and dosage

Inside, with a large amount of liquid 1-2 hours after a meal (taking the drug immediately after a meal leads to a delay in the onset of action).

For children aged 6-12 years, the drug is prescribed in a single dose of 1/2 tablet, Repeated use of the drug is possible after 10-12 hours, the maximum dose is 2 tablets per day.

Adults and adolescents over 12 years of age are recommended to use the drug 1-2 tablets at a time, if necessary, the reception can be repeated after 8 hours. With a short (no more than 3 days) course of treatment, the maximum daily dose is 6 tablets, with a longer course of treatment, it should not exceed 4 tablets per day.

Elderly patients with normal liver and kidney function do not need to adjust the dose of the drug, in patients with hepatic and/or renal insufficiency, the dose of the drug should be reduced and set individually.

The maximum duration of treatment without consulting a doctor is 3 days.

Overdose

Symptoms due to an overdose of paracetamol: during the first 24 hours after ingestion – pallor of the skin, nausea, vomiting, anorexia, abdominal pain; impaired glucose metabolism, metabolic acidosis.

Symptoms of impaired liver function may appear 12-48 hours after an overdose. In severe overdose – liver failure with progressive encephalopathy, coma; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis. The hepatotoxic effect in adults is manifested when taking 10 g or more.

Treatment:  gastric lavage, saline laxatives, use of SN-group donors and glutathione-methionine synthesis precursors 8-9 hours after overdose and N-acetylcysteine – 12 hours after overdose. The need for additional therapeutic measures (further use of methionine, intravenous use of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after taking it. If the central nervous system is severely damaged, artificial ventilation and oxygen therapy may be necessary.

Special instructions

The risk of liver damage increases in patients with alcoholic hepatosis.

In patients with mild to moderate renal and hepatic insufficiency, the dose should be set individually.

When using the drug for more than 3 days and/or high doses, it is necessary to monitor the picture of peripheral blood (the number of white blood cells, platelets) and the functional state of the liver (the activity of “liver” enzymes). Clinical and laboratory symptoms of hepatotoxic effects begin to appear within 48-72 hours after taking large doses of the drug.

Influence on the ability to drive vehicles and mechanisms:During the treatment period, it is necessary to refrain from driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in the original packaging (blister pack), at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 2 years.

Do not use after the expiration date indicated on the package.

Active ingredient

Drotaverine, Paracetamol

Dosage form

Tablets