Spasmalgon Effect pills, 30pcs

Composition

1 film-coated tablet contains:

active ingredients:  paracetamol 325.0 mg, naproxen 100.0 mg, caffeine 50.0 mg, drotaverine hydrochloride 40.0 mg, phenyramine maleate 10.0 mg;

excipients:  microcrystalline cellulose 118.6 mg, pregelatinized corn starch 30.0 mg, hyprolose 20.0 mg, croscarmellose sodium 60.0 mg, citric acid 10.0 mg, disodium edetate 0.4 mg, ascorbic acid 20.0 mg, talc 12.0 mg, magnesium stearate 4.0 mg;

film coating:  Opadray fx green 65 F210000 30.0 mg (polyvinyl alcohol 14,100 mg, talc 6,588 mg, macrogol 3,990 mg, pearlescent pigment* 3,000 mg, polysorbate-80 0.810 mg, titanium dioxide 0.750 mg, aluminum varnish based on indigo carmine dye 0.507 mg, aluminum varnish based on quinoline yellow dye 0.255 mg).

* Mother-of-pearl pigment consists of mica and contains 69-75% potassium aluminosilicate (E 555) and 25-31% titanium dioxide (E 171).

Pharmacological action

Combined drug, has analgesic, anti-inflammatory, antispasmodic, antipyretic effect.

Paracetamol is a non-narcotic analgesic, has an antipyretic and analgesic effect due to the blockade of cyclooxygenase (COX) in the central nervous system (CNS) and the effect on the pain centers and thermoregulation.

Naproxen is a nonsteroidal anti-inflammatory drug (NSAID) that has anti-inflammatory, analgesic and antipyretic effects associated with non-selective suppression of COX activity, which regulates prostaglandin synthesis.

Caffeine-causes dilation of blood vessels in skeletal muscles, heart, and kidneys; increases mental and physical performance, helps eliminate fatigue and drowsiness; increases the permeability of histohematic barriers and increases the bioavailability of non-narcotic analgesics, thereby enhancing the therapeutic effect. It has a tonic effect on the blood vessels of the brain.

Drotaverin-has a myotropic antispasmodic effect due to inhibition of phosphodiesterase IV, acts on the smooth muscles of the gastrointestinal tract( GIT), biliary tract, genitourinary system, blood vessels.

Phenyramine – H1-histamine receptor blocker. It has antispasmodic and mild sedative effects, reduces the effects of exudation, and also enhances the analgesic effect of paracetamol and naproxen.

Pharmacokinetics:

Paracetamol

is characterized by high and rapid absorption from the gastrointestinal tract, mainly in the small intestine. The time to reach the maximum concentration in blood plasma (TMAX) is 0.5-1.5 hours after oral use. The maximum concentration in blood plasma (Cmax) is 5-20 mcg/ml. The association with plasma proteins is insignificant-15%. Paracetamol is evenly distributed and penetrates through the blood-brain barrier, as well as into most body tissues. The estimated volume of distribution is 0.95 l / kg. 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 half-life (T 1/2) is 1.5-2.5 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, drug clearance decreases and T 1/2 increases.

Naproxen

Absorption from the gastrointestinal tract of naproxen is fast and complete. Bioavailability – 95%. Food intake practically does not affect either the fullness or the rate of absorption. Tsmakh – 1-2 hours. Binding to plasma proteins is more than 99%. The equilibrium concentration is reached by taking 4-5 doses of the drug (2-3 days). It is metabolized in the liver to dimethylnaproxene with the participation of the CYP2C9. T1/2 isoenzyme – 12-15 hours. Clearance – 0.13 ml / min / kg. It is excreted by the kidneys (98%),10% of which is unchanged; 0.5-2.5% of the dose is excreted in the bile. In case of renal failure, accumulation of metabolites is possible.

Caffeine

Caffeine, which is part of the drug, is almost completely and quickly absorbed, the maximum concentration in the blood plasma is reached in 1 hour. It quickly passes through the blood-brain and placental barriers, enters breast milk, and is excreted (including in the form of metabolites) mainly by the kidneys about 65-80%. The main metabolites are 1-methylxanthine,1-methyluric acid and acetylated uracil derivatives, and a small amount of caffeine is converted to theophylline and theobromine. T1 / 2 – 3.5 hours.

Drotaverine

When taken orally, the absorption of drotaverine is high and rapid. Bioavailability – 100%. After presystemic metabolism,65% of the received dose of drotaverine enters the systemic circulation. The time to reach Cmax in the blood is 45-60 minutes. Binding to plasma proteins is 95-97%, mainly with albumin, gamma-and beta-globulins, and high-density lipoproteins. Evenly distributed in the tissues, penetrates into smooth muscle cells. It does not cross the blood-brain barrier. Drotaverine and / or its metabolites may only slightly cross the placental barrier. T1 / 2 – 8-10 hours. It is almost completely metabolized in the liver by O-deethylation. The metabolites are rapidly conjugated with glucuronic acid. The main metabolite is 4′ – desethyldrotaverine, other metabolites are 6-desethyldrotaverine and 4′ – desethyldrotaveraldine. T1 / 2 – 8-10 hours. In 72 hours, it is almost completely eliminated from the body. Mainly (more than 50% of drotaverine) is excreted by the kidneys, mainly in the form of metabolites, to a lesser extent (about 30%) – with bile. Unchanged drotaverine is not detected in the urine.

Phenyramine

The maximum concentration of phenyramine in the blood plasma is reached in about 1-2.5 hours. T1 / 2 – 16-19 hours. 70-83% of the dose taken is eliminated from the body through the kidneys in the form of metabolites or in unchanged form.

Indications

– Pain syndrome of various Genesis, including pain in the joints, muscles; with sciatica, algodismenoree (menstrual pain), neuralgia, dental pain, headaches (including headaches, caused by spasm of the blood vessels of the brain);

– pain associated with spasm of smooth muscles, including chronic cholecystitis, gallstones, postcholecystectomy syndrome, renal colic;

– post-traumatic and postoperative pain, including inflamed;

– colds, accompanied by a febrile syndrome (as symptomatic therapy).

Contraindications

– Hypersensitivity to the components of the drug;

– erosive-ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);

gastrointestinal bleeding;

– complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid or other NSAIDs (including in the anamnesis);

– severe liver failure;

– severe renal failure;

– oppression of bone marrow hematopoiesis;

– status after conducting coronary artery bypass grafting;

– heavy organic cardiovascular disease (including acute myocardial infarction);

paroxysmal tachycardia,

frequent ventricular premature beats;

– severe arterial hypertension;

– hyperkalemia;

– pregnancy and the period of breastfeeding;

– children’s and teenage age up to 18 years.

With caution:

The drug should be used with caution in patients with cerebrovascular diseases, diabetes mellitus, peripheral artery diseases, a history of ulcerative lesions of the gastrointestinal tract, mild or moderate renal and hepatic insufficiency, viral hepatitis, alcoholic liver damage, benign hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), epilepsy, a tendency to convulsive seizures, glucose-6 deficiency-phosphate dehydrogenase, in elderly patients.

In the presence of any of the listed diseases/conditions the patient should consult a doctor before using the drug.

Side effects

Allergic reactions: skin rash, pruritus, urticaria, angioedema.

Hematopoietic disorders: thrombocytopenia, leukopenia, agranulocytosis, anemia, methemoglobinemia.

From the central nervous system: agitation, anxiety, increased reflexes, tremor, headache, sleep disorders, dizziness, decreased concentration.

From the cardiovascular system: palpitations, arrhythmias, increased blood pressure (BP).

From the digestive system: erosive and ulcerative lesions of the gastrointestinal tract, nausea, vomiting, epigastric discomfort, abdominal pain, constipation, impaired liver function.

From the urinary system: impaired renal function.

Sensory disorders: hearing loss, tinnitus, increased intraocular pressure in patients with angle-closure glaucoma.

Other: dermatitis, tachypnea (rapid breathing).

If any of these side effects worsen, or the patient notes any other side effects that are not listed in the instructions, they should inform their doctor.

Interaction

Concomitant use of SPASMALGON EFFECT with barbiturates, tricyclic antidepressants, rifampicin, and alcoholic beverages increases the risk of hepatotoxic effects (these combinations should be avoided).

Paracetamol enhances the effect of indirect anticoagulants and reduces the effectiveness of uricosuric drugs.

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

Concomitant use of paracetamol with ethanol (beverages and drugs containing alcohol) increases the risk of acute pancreatitis.

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

Diflunisal increases the plasma concentration of paracetamol by 50%, which increases the risk of hepatotoxicity.

Naproxen can cause a decrease in the diuretic effect of furosemide, an increase in the effect of indirect anticoagulants, increases the toxicity of sulfonamides and methotrexate, reduces the excretion of lithium and increases its concentration in blood plasma.

With the combined use of caffeine and barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin), it is possible to increase the metabolism and increase the clearance of caffeine; with the simultaneous use of caffeine and cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin-a decrease in the metabolism of caffeine in the liver (slowing its excretion and increasing concentration in the blood).

Concomitant consumption of caffeinated beverages and other CNS-stimulating drugs can lead to excessive CNS stimulation.

When used concomitantly, drotaverine may weaken the antiparkinsonian effect of levodopa.

With the simultaneous use of phenyramine with tranquilizers, sleeping pills, monoamine oxidase inhibitors, alcohol, it is possible to increase the depressing effect on the central nervous system.

How to take, course of use and dosage

The drug is taken orally 1 tablet 1-3 times a day. The maximum daily dose is 4 tablets.

The duration of treatment is no more than 3 days as an antipyretic and no more than 5 days as an analgesic. Continuation of treatment with the drug is possible only after consultation with a doctor.

Do not exceed the indicated dose of the drug!

Overdose

Symptoms: pallor of the skin, anorexia (lack of appetite), abdominal pain, nausea, vomiting, gastrointestinal bleeding, agitation, motor restlessness, confusion, tachycardia, arrhythmia, hyperthermia (increased body temperature), frequent urination, headache, tremor or muscle twitching; epileptic seizures, increased activity of “hepatic” transaminases, hepatonecrosis, increased prothrombin time time limit.

Symptoms of impaired liver function may appear 12-48 hours after an overdose. Severe overdose leads to liver failure with progressive encephalopathy, coma, and death; acute renal failure with tubular necrosis; arrhythmia, pancreatitis. If an overdose is suspected, you should immediately seek medical attention from a doctor.

Treatment: gastric lavage followed by the use of activated charcoal.

A specific antidote for paracetamol poisoning is acetylcysteine. The introduction of acetylcysteine is relevant within 8 hours after taking paracetamol. In case of gastrointestinal bleeding, it is necessary to administer antacids and gastric lavage with an icy 0.9% sodium chloride solution; maintain ventilation and oxygenation; in case of epileptic seizures, intravenous use of diazepam; maintain the balance of fluid and salts in the body.

Special instructions

Avoid concomitant use of SPASMALGON EFFECT with other medications containing paracetamol and / or other NSAIDs, including those used to relieve the symptoms of “colds”, flu, and nasal congestion. When using the drug SPASMALGON® EFFECT for more than 5-7 days, peripheral blood parameters and the functional state of the liver should be monitored. Paracetamol distorts the results of laboratory tests of glucose and uric acid in blood plasma.

If it is necessary to determine 17-ketosteroids, the SPASMALGON® effect should be canceled 48 hours before the study.

Keep in mind that naproxen increases the bleeding time.

The effect of caffeine on the central nervous system depends on the type of nervous system and can be manifested by both excitation and inhibition of higher nervous activity.

During the treatment period, the patient should avoid drinking alcohol.

Influence on the ability to drive vehicles and mechanisms:

In some cases, it is possible to reduce the concentration of attention and the speed of psychomotor reactions, so during treatment, the patient should be careful when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years.

Do not use after the expiration date.

Active ingredient

Drotaverine, Caffeine, Naproxen, Paracetamol, Phenyramine

Dosage form

Tablets