SPAZMALGON® EFFECT (Spasmalgon® Effekt)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceDrotaverine + Caffeine + Naproxen + Paracetamol + Pheniramine maleateDrotaverine + Caffeine + Naproxen + Paracetamol + Pheniramine maleate
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  • SPAZMALGON® EFFECT
    pills inwards 
    Balkanfarma - Dupnitsa AD     Bulgaria
    • Dosage form: & nbspTfilm-covered abeys.
    Composition:

    1 tablet, coated with a film jacket, contains:

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

    Excipients: cellulose microcrystalline 118.6 mg, starch corn pregelatinized 30.0 mg, giprolose 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 sheath: Opadry 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 lacquer based on indigo carmine dye 0,507 mg, aluminum dye based on dye quinoline yellow 0.255 mg).

    * Pearlescent pigment consists of mica and contains 69-75% potassium aluminosilicate (E555) and 25-31%% titanium dioxide (E171).

    Description:Oblong, biconvex tablets covered with a film membrane, green with a risk on one side.
    Pharmacotherapeutic group:Analgesic agent (analgesic non-narcotic agent + non-steroidal anti-inflammatory drug + psychostimulating agent + antispasmodic + H1-histamine receptor blocker)
    ATX: & nbsp

    N.02.B.E   Anilides

    Pharmacodynamics:

    The combined preparation has analgesic, anti-inflammatory, antispasmodic, antipyretic effect.

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

    Naproxen - non-steroidal anti-inflammatory drug (NSAID), has anti-inflammatory, analgesic and antipyretic effect associated with nonselective suppression of COX activity regulating the synthesis of prostaglandins.

    Caffeine - causes an expansion of blood vessels of skeletal muscles, heart, kidneys; increases mental and physical performance, helps to eliminate fatigue and drowsiness; increases the permeability of histohematological barriers and increases the bioavailability of non-narcotic analgesics,thereby contributing to the enhancement of the therapeutic effect. Has a tonic effect on the vessels of the brain.

    Drotaverine - has a myotropic antispasmodic effect caused by inhibition of phosphodiesterase IV, acts on smooth muscles of the gastrointestinal tract (GIT), bile ducts, urogenital system, vessels.

    Pheniramine - H1-gistaminovyh receptors blocker. Has spasmolytic and mild sedative effect, reduces the phenomenon of exudation, and also enhances the analgesic effect of paracetamol and naproxen.

    Pharmacokinetics:

    Paracetamol

    It is characterized by high and rapid absorption from the gastrointestinal tract, mainly in the small intestine. Time to reach the maximum concentration in the blood plasma (TCmOh) - 0.5-1.5 hours after ingestion. The maximum concentration in the blood plasma (CmOh) - 5-20 mcg / ml. The connection with plasma proteins is insignificant - 15%. Paracetamol evenly distributes and penetrates the blood-brain barrier, as well as in most body tissues. The estimated volume of distribution is 0.95 l / kg. Metabolised in the liver (90-95%): 80% enters the conjugation reaction withGlucuronic acid and sulfates with formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites, which are conjugated with glutathione with the formation of already inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. In the metabolism of the drug is also involved isoenzyme CYP2E1. The half-life (T1/2) - 1,5-2,5 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, the clearance of the drug decreases and T1/2.

    Naproxen

    Absorption from the digestive naproxen is fast and complete. Bioavailability is 95%. The intake of food practically does not affect either the completeness or the rate of absorption. TSmOh - 1-2 hours. Binding to plasma proteins is more than 99%. Equilibrium concentration is achieved by taking 4-5 doses of the drug (2-3 days). Metabolized in the liver to dimethylnaproxen with the participation of isoenzyme CYP2C9. T1/2 - 12-15 hours. Clearance - 0.13 ml / min / kg. It is excreted by the kidneys (98%), 10% of which - unchanged; with bile excreted 0.5-2.5% of the dose. With renal failure, metabolites can be accumulated.

    Caffeine

    Caffeine, which is part of the drug, is almost completely and quickly absorbed, the maximum concentration in blood plasma is reached after 1 hour. Rapidly passes through the blood-brain and placental barriers, enters the breast milk, is excreted (including in the form of metabolites) mainly in the kidneys of about 65-80%. The main metabolites are 1-methylxanthine, 1-methyl uric acid and acetylated derivatives of uracil, a small amount of caffeine is converted into theophylline and theobromine. T1/2 - 3,5 hours.

    Drotaverine

    When administered orally, the absorption of drotaverin is high and rapid. Bioavailability is 100%. After presystemic metabolism, 65% of the accepted dose of drotaverine enters the systemic circulation. Time to reach CmOh in the blood - 45-60 minutes. Binding to plasma proteins is 95-97%, mainly with albumin, gamma and beta globulins, as well as high-density lipoproteins. Evenly distributed in tissues, penetrates smooth muscle cells. Does not penetrate the blood-brain barrier. Drotaverine and / or its metabolites can penetrate insignificantly through the placental barrier. T1/2 - 8-10 hours. Almost completely metabolized in the liver by O-de-ethylation. Metabolites are rapidly conjugated with glucuronic acid.The main metabolite is 4'-desethyltraderin, the other metabolites are 6-deethyldrothaverin and 4'-deethyldrothaveraldin. T1/2 - 8-10 hours. For 72 hours almost completely eliminated from the body. Basically (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 in the urine is not found.

    Pheniramine

    The maximum concentration of Pheniramine in blood plasma is reached after approximately 1-2.5 hours. T1/2 - 16-19 hours. 70-83% of the accepted dose is excreted 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 radiculitis, algodismenorrhea (menstrual pains), neuralgia, toothache, headache (including headache due to spasm of the cerebral vessels);

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

    - post-traumatic and postoperative pain syndrome, including those accompanied by inflammation;

    - catarrhal diseases accompanied by febrile syndrome (as symptomatic therapy).

    Contraindications:

    - Hypersensitivity to the components of the drug;

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

    - gastrointestinal bleeding;

    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in history);

    - severe hepatic impairment;

    - severe renal insufficiency;

    - oppression of bone marrow hematopoiesis;

    - condition after aortocoronary bypass surgery;

    - severe organic diseases of the cardiovascular system (including acute myocardial infarction);

    - paroxysmal tachycardia;

    - frequent ventricular extrasystole;

    - severe arterial hypertension;

    - hyperkalemia;

    - pregnancy and the period of breastfeeding;

    - children and adolescence up to 18 years.

    Carefully:

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

    Pregnancy and lactation:

    Contraindicated use of the drug during pregnancy and during breastfeeding.

    Dosing and Administration:

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

    Duration of treatment is no more than 3 days as an antipyretic agent and no more than 5 days - as an anesthetic. Continuation of treatment with the drug is possible only after consulting a doctor.

    Do not exceed the indicated doses of the drug!

    Side effects:

    Allergic reactions: skin rash, itching, hives, angioedema.

    On the part of the organs of hematopoiesis: thrombocytopenia, leukopenia, agranulocytosis, anemia, methemoglobinemia.

    From the side of the central nervous system: excitation, anxiety, increased reflexes, tremor, headache, sleep disturbances, dizziness, decreased concentration of attention.

    From the side of 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.

    From the sense organs: hearing loss, tinnitus, increased intraocular pressure in patients with closed-angle glaucoma.

    Other: dermatitis, tachypnea (rapid breathing).

    If any of these side effects are aggravated, or the patient notes any other side effects not listed in the instructions, he should inform the doctor.

    Overdose:

    Symptoms: pallor of the skin, anorexia (lack of appetite), abdominal pain, nausea, vomiting, gastrointestinal bleeding, agitation, motor anxiety, confusion, tachycardia, arrhythmia, hyperthermia (fever), frequent urination, headache, tremor or muscle twitching; epileptic seizures, increased activity of "hepatic" transaminases, hepatonecrosis, an increase in prothrombin time.

    Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose, hepatic failure develops with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis; arrhythmia, pancreatitis. If you suspect an overdose, you should immediately seek medical help from a doctor.

    Treatment: gastric lavage followed by administration of activated charcoal.

    Specific antidote for paracetamol poisoning is acetylcysteine. The introduction of acetylcysteine ​​is important for 8 hours after taking paracetamol. With gastrointestinal bleeding it is necessary to administer antacids and rinse the stomach with an ice-cold 0.9% solution of sodium chloride; maintenance of ventilation and oxygenation; with epileptic seizures - intravenous diazepam; maintaining the balance of fluid and salts in the body.

    Interaction:

    At simultaneous reception of a preparation SPAZMALGON® EFFECT with barbiturates, tricyclic antidepressants, rifampicin, alcohol-containing beverages the risk of hepatotoxic action increases (these combinations should be avoided).

    Paracetamol increases the effect anticoagulants of indirect action and reduces efficiency uricosuric drugs.

    Long-term use barbiturates reduces the effectiveness of paracetamol.

    With the simultaneous use of paracetamol with ethanol (drinks and drugs containing alcohol) increases the risk of acute pancreatitis.

    Inhibitors of microsomal oxidation (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 is able to cause a decrease in diuretic effect furosemide, amplification of effect indirect anticoagulants, increases toxicity sulfonamides and methotrexate, reduces excretion lithium and increases its concentration in the blood plasma.

    With the joint use of caffeine and barbiturates, primidon, anticonvulsants (hydantoin derivatives, especially phenytoin) possibly increased metabolism and increased clearance of caffeine; while taking caffeine and cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increased concentration in the blood).

    Simultaneous use caffeine-containing beverages and other CNS stimulating agents, can lead to excessive stimulation of the central nervous system.

    With simultaneous application drotaverine can weaken the antiparkinsonian effect levodopa.

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

    Special instructions:

    It is necessary to avoid the simultaneous use of the drug SPAZMALGON® EFFECT with other agents containing paracetamol and / or other NSAIDs, including with funds to relieve the symptoms of "colds", flu and nasal congestion.

    When using the drug SPAZMALGON® EFFECT for more than 5-7 days, it is necessary to monitor the parameters of peripheral blood and the functional state of the liver. Paracetamol distorts the results of laboratory studies of glucose and uric acid in the blood plasma.

    If it is necessary to determine 17-ketosteroids, SPASMALGON® EFFECT should be discontinued 48 hours before the test.

    It should be borne in mind that naproxen increases bleeding time.

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

    During treatment, the patient should avoid drinking alcohol.

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

    In some cases, the concentration of attention and the speed of psychomotor reactions may be reduced, so during the treatment the patient should be careful when driving vehicles and taking other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Film-coated tablets.
    Packaging:

    10 tablets in a three-layer blister PVC / PVDX / PVC film or double-layer PVC / PVDC film and aluminum foil.

    For 1, 2 or 3 blisters together with instructions for use in a cardboard bundle.

    Storage conditions:At a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:Without recipe
    Registration number:LP-003690
    Date of registration:20.06.2016
    Expiration Date:20.06.2021
    The owner of the registration certificate:Balkanfarma - Dupnitsa ADBalkanfarma - Dupnitsa AD Bulgaria
    Manufacturer: & nbsp
    Representation: & nbspAktavis, Open Company Aktavis, Open Company
    Information update date: & nbsp18.08.2016
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