But-shpalgin® (No-Spalgin®)

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Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceDrotaverin + Codeine + ParacetamolDrotaverin + Codeine + Paracetamol
Dosage form: & nbsppills
Composition:

Each No-Shpalgin tablet contains, as active ingredients:

500.0 mg of paracetamol, 40.0 mg of drotaverine hydrochloride and 8.0 mg of codeine phosphate (in the form of hemihydrate).

Excipients: polyvidone, yellow ferric oxide (E172), magnesium stearate, ascorbic acid, crospovidone, talc, corn starch, microcrystalline cellulose, pregelatinized starch.

Description:

light-yellow tablets with impregnations of a lighter and darker color, an elongated shape with a dividing risk on both sides.

Pharmacotherapeutic group:Analgesic combined (analgesic opioid + analgesic non-narcotic + antispasmodic)
ATX: & nbsp

N.02.B.E   Anilides

Pharmacodynamics:

Paracetamol has an analgesic and antipyretic effect mainly by inhibiting the synthesis of prostaglandins in the central nervous system,and to a lesser extent - by peripheral action, by blocking the action of prostaglandins and other substances that stimulate pain receptors.

Drotaverin is an isoquinoline derivative that exhibits spasmolytic effect on smooth muscle by inhibiting the enzyme phosphodiesterase IV (PDE IV). The consequence of this is an increase in the concentration of c-AMP, which inactivating the enzyme-myosinkinase, leads to a relaxation of smooth muscles. Besides, drotaverine has a weak inhibitory effect on calmodulin-dependent calcium channels. Regardless of the type of autonomic innervation, drotaverine Effective in spasms of smooth muscles. It acts on smooth muscles found in the vascular, gastrointestinal, biliary and urogenital systems, but its effectiveness depends on different levels of phosphodiesterase IV, since the content of phosphodiesterase IV in different tissues is different. Codeine is a central antitussive drug that acts through the m and k receptors involved in the transmission of painful impulses in the central nervous system.

Pharmacokinetics:

Paracetamol and codeine do not affect the pharmacokinetics of each other. Their pharmacokinetics also does not change with repeated admission.

There is no interaction between paracetamol and drotaverin in relation to binding to plasma proteins. In the tests in vitro shown, that paracetamol (in the therapeutic range of doses) nonspecifically inhibits the metabolism of drotaverine, increasing the half-life of the drug 2-7 times, that is in vivo it can also inhibit the metabolism of drotaverine.

The change in pharmacokinetic parameters showed that the equilibrium state can be achieved on the 6th day, with a single dose, and on the third day with a double dose.

But-Shpalgin increases the area under the curve and the maximum concentration of drotaverine. The values ​​of the maximum concentration are in the range of 132-171 ng / ml, the area under the curve 0-24 - 463-830.2 ng. h / l. This can be expressed in a more effective analgesic effect with a somewhat longer duration. A similar phenomenon was also shown for paracetamol. But-Shpalgin increases the area under the paracetamol curve, which leads to a significant decrease in clearance.The values ​​of the maximum paracetamol concentration are in the range of 5495-6752 ng / ml, the area under the curve 0-24 21760.8-26524.7 ng.h / l, and the clearance is 365-418 ml / min.

Indications:For relief of pain of mild and moderate intensity of different genesis.
Contraindications:

- Hypersensitivity to any of the components

- Severe renal or hepatic impairment

- Severe heart failure, atrioventricular blockade of MI degree

- Respiratory failure, bronchial asthma

- Treatment with MAO inhibitors (within 14 days)

- Deficiency of glucose-6-phosphate dehydrogenase

- Child age (up to 6 years)

- Chronic alcoholism and drug addiction

- Condition after traumatic brain injury

- Increased intracranial pressure

- Diseases of the blood (thrombocytopenia, leukopenia, granulocytosis)

- Pregnancy and the period of breastfeeding

- Do not use together with other paracetamol-containing drugs

Carefully:

Gilbert's syndrome (constitutional hyperbilirubiliary), advanced age

Pregnancy and lactation:Contraindicated
Dosing and Administration:

With a headache No-Shpalgin recommended to use inside a single dose of 1-2 tablets, if necessary, repeated intake after 8 hours.

With a short (not more than 3 days) course of treatment, the maximum daily dose is 6 tablets, with a long course it should not exceed 4 tablets per day. In the case of continuous administration of the drug, it is recommended to control the number of leukocytes, platelets, and also creatinine and the level of hepatic enzymes in the blood.

To achieve rapid relief of pain, do not take the drug with food.

Children:

At the age of 6-12 years, a single dose 1/2 -1 tablet, which can be administered again after 10-12 hours, the maximum dose of 2 tablets per day.

Elderly patients:

A normal adult dose is recommended if there is no impairment of kidney and liver function.

With severe impairment of kidney and liver function:

If the kidney or liver function is severely impaired, the dose should be reduced. When the glomerular filtration rate is less than 10 ml / min, the time between two doses should be more than 12 hours. Only occasional use of the drug is allowed.

Side effects:

When applying the recommended therapeutic doses, side effects are rare. People with hypersensitivity can experience allergic reactions (rash, flushing of blood to the face).

Seldom can occur a decrease in blood pressure, headache, dizziness, nausea, palpitations, drowsiness, constipation, very rarely - bronchospasm, mucosal edema of the nose or allergic reactions, violation of blood (agranulocytosis, thrombocytopenia).

When taking high doses, mainly in the case of prolonged use, the drug can cause toxic damage to the liver, in very high doses - lethal (irreversible tissue necrosis). The earliest symptoms of these disorders are: pallor of the skin, vomiting, increased sweating, nausea.

Overdose:

Symptoms of overdose and its treatment:

Nausea, vomiting, circulatory disorders and respiratory depression are the main symptoms of codeine overdose. Recommended gastric lavage and the use of salt laxatives. In case of severe damage to the central nervous system, auxiliary ventilation of the lungs and oxygen supply, as well as the administration of naloxone, may be necessary to monitor the condition.

The condition of a patient who has taken an excessively high dose of paracetamol can be satisfactory for the first 3 days, and only after that there are signs of liver damage.Changes that develop in the liver cells as a result of an overdose cause the accumulation of toxic intermediate products of metabolism. In case of an overdose of antidotes (N-acetylcysteine ​​or methionine) show a protective effect on the liver.

Use the drug for longer than 3 days, you can only under the supervision of a doctor.

Interaction:

Due to the content of drotaverine hydrochloride:

when applied together with levodopa, the effect of the latter decreases, i.e. tremor and stiffness may increase.

Because of the content of paracetamol:

When used together with drugs inducing the induction of liver enzymes (salicylamide, barbiturates, antiepileptic, tricyclic antidepressants, alcohol, rifampicin) the level of toxic metabolites of paracetamol increases When applied simultaneously with chloramphenicol, the half-life of the latter increases and its toxicity increases

Simultaneous use with doxorubicin increases the risk of liver function disorders

reduces the effectiveness of uricosuric drugs.

Metoclopramide and domperidone increase absorption of paracetamol, and colestramine it reduces

With prolonged use of the drug, the risk of bleeding increases due to the presence of paracetamol

Because of the content of codeine:

intensifies the effect of sleeping pills, analgesics and sedatives.

If necessary, No-Shpalgin can be used as an analgesic in patients taking indirect long-acting anticoagulants.

Special instructions:

For quick relief of pain, it is not recommended to take the drug with food. Do not exceed the recommended dose. Simultaneous use of other drugs containing paracetamol, Not recommended. When taking the drug, consumption of alcoholic beverages is prohibited. In renal or hepatic insufficiency, the dose should be set individually. When using the drug for more than 3 days and / or high doses, a control of the peripheral blood picture and the functional state of the liver is necessary. Clinical and laboratory symptoms of hepatotoxic effect begin to appear within 48-72 hours after taking in large doses of the drug.

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

Given that No-Shpalgin can in some cases cause drowsiness, and thus affect the ability to drive traffic,work on machine tools. The degree of restriction or prohibition should be established individually.

Form release / dosage:Pills.
Packaging:12 tablets in blisters (6 tablets per blister) of aluminum, in cardboard boxes
Storage conditions:

At a temperature not exceeding 30 ° C, in the original packaging, out of the reach of children.

Shelf life:

3 years

Do not take it after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe
Registration number:P N015036 / 01-2003
Date of registration:23.05.2008
Date of cancellation:2017-10-24
The owner of the registration certificate:HINOIN Pharmaceutical and Chemical Products Plant, ZAO HINOIN Pharmaceutical and Chemical Products Plant, ZAO Hungary
Manufacturer: & nbsp
Representation: & nbspSanofi Russia, JSCSanofi Russia, JSCRussia
Information update date: & nbsp24.10.2017
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