Viscaldix® (Viskaldix®)

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Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceClopamide + PindololClopamide + Pindolol
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  • Viscaldix®
    pills inwards 
    EGIS ZAO Pharmaceutical Plant     Hungary
    • Dosage form: & nbsppills
    Composition:Each tablet contains active substances: 5 mg of clopamid and 10 mg of pindolol, Excipients: lactose monohydrate, corn starch, magnesium stearate.
    Description:White or almost white round, flat tablets with a bevel, with an arcuate engraving "VISKAL"on the same side, odorless or almost odorless. A slight unevenness of the surface of the tablets is allowed.
    Pharmacotherapeutic group:Hypotensive combined agent (beta-blocker + diuretic)
    ATX: & nbsp

    C.07.C.A.03   Pindolol in combination with other diuretics

    Pharmacodynamics:

    The combined preparation contains two active components, complementary to each other's hypotensive effect.

    Pindolol is a lipophilic noncardioselective membrane stabilizing beta blocker- receptors, which has its own sympathomimetic activity (SMA). Pindolol partially excites β1 and β2 receptors, especially strongly affects the β2 receptors. Clopamide is a sulfonamide diuretic.The chemical structure of the clopamid differs from the structure of the thiazides. However, it has the same mechanism of action as thiazide preparations. Klopamid is a weak diuretic.

    Mechanism of action:

    Pindolol is a competitive inhibitor of beta-adrenergic receptors in the heart, bronchi and smooth muscles, with a pronounced intrinsic sympathomimetic activity. The membrane-stabilizing effect of this drug has no clinical significance. In patients with predominant sympathetic activity pindolol reduces heart rate (heart rate) and cardiac output, but only slightly reduces the heart rate at rest.

    It has a moderate effect on exercise-induced acceleration of the heart rate, reduces myocardial contractility, and also slightly slows the atrial-ventricular conduction of the stimulation. Pindolol increases the resistance of the respiratory tract.

    Like other beta-blockers, pindolol reduces blood pressure (BP), heart rate and heart rate, which leads to a decrease in oxygen consumption by the myocardium. By reducing myocardial contractility and diastole lengthening pindolol improves blood supply and oxygenation of areas of the myocardium with disturbed blood flow. Thanks to this action pindolol reduces the frequency of attacks of angina and increases the physical performance of patients.

    In connection with the partial excitatory effect on β2smooth muscle receptors pindolol has a clinically significant vasodilator effect. With arterial hypertension, this drug reduces the increased total vascular peripheral resistance and thus maintains or even improves the blood supply of various organs. Generally pindolol does not have an undesirable effect on the metabolism of fats, even when long-term use of the drug.

    By suppressing the absorption of sodium and chlorine ions in the distal renal tubules, clopamid enhances the secretion of these ions and water.

    Like thiazides, clopamid inhibits the reabsorption of sodium in the cortical segment of the ascending knee of the Henle loop and the distal renal tubules. However, it does not have the same effect in the medullary segment and therefore does not affect the osmotic gradient and the concentration ability of the kidneys. In this regard, since in this segment of the nephron only 3 - 5% sodium, clopamid increases the excretion of sodium and water to a much lesser degree and its diuretic effect is much weaker than the effects of such diuretics (furosemide and ethacrynic acid). Especially at the beginning of the course of treatment, clopamid can cause a significant loss of ionoat sodium, the degree of which can decrease with prolonged therapy. Unlike other diuretics, clopamid enhances the reabsorption of calcium ions.

    Clopamid has a diabetic potential and increases the level of uric acid, cholesterol and triglycerides in the blood plasma. However, the clinical significance of its adverse metabolic effects is significantly different in different patients. During the first 2-3 weeks of taking the drug, the antihypertensive effect of clopamid is mainly associated with a decrease in the volume of extracellular fluid due to the excretion of sodium ions, resulting in reduced venous pressure, reduced cardiac output, and finally reduced blood pressure. In the future - with prolonged intake of the drug - cardiac output returns to the initial level, and peripheral resistance remains reduced. It is believed,that it is partially caused both by the expansion of the vessels in connection with the loss of fluid from the vascular wall, and by the excretion of sodium, which, according to some observations, weakens the contractile response of the glaucomadjam cells on norepinephrine.

    The two active components give a total antihypertensive effect.

    Pharmacokinetics:

    Pindolol

    - Fast and almost complete (> 95 %) absorption and insignificant (13 %) metabolism of the "first passage" cause a high (87 %) bioavailability of pindolol.

    - The maximum concentration of the drug in the blood plasma is reached 1 hour after reception inside.

    - Pindolol has a linear pharmacokinetics in the dose range of 5 -15 mg.

    - Approximately 40% of the absorbed substance binds to blood plasma proteins. Visible volume of distributionI is 2 - 3 l / kg. Due to lipophilic properties pindolol can penetrate the blood-brain barrier.

    - Pindolol metabolized to inactive metabolites in the liver.

    - The final half-life is approximately 3-4 hours. Approximately 30-40% of the administered dose is excreted unchanged by the kidneys, and 60 to 70% is excreted in the form of inactive metabolites through the intestine and kidneys.The clearance of pindolol from the whole organism is 500 ml / min.

    - Pindolol penetrates the placental barrier and in small amounts is excreted in breast milk. The ratio of the concentrations of the substance in the blood of the umbilical cord and the mother's blood is 0.7.

    - The ratio of concentrations of pindolol in milk and blood of the mother is 1.6.

    Clopamid:

    - The complete antihypertensive effect of clopamid is achieved after about 2 to 4 weeks of taking the drug. After oral intake, approximately 90% of the clopamid is absorbed. The maximum concentration in blood plasma is achieved through 1,9-2,5 hours after ingestion. Approximately 45% of the absorbed amount of clopamid binds to plasma proteins. The apparent volume of distribution is 1.5 l / kg.

    - The main pathway of the metabolism of clopamide (42.5%) is hydroxylation to the inactive derivative. Clopamide is excreted by the kidneys (20 - 30% is released unchanged). Half-life - 10 hours.

    - Diuresis and natriuresis begin 1 to 2 hours after taking the drug and reach a maximum after 2 - 4 hours. Depending on the dose, the effect persists for 12-24 hours.

    Indications:

    Arterial hypertension of mild to moderate severity as a monotherapy or (if necessary) in combination with other antihypertensive agents.

    Contraindications:

    - Hypersensitivity to any component of the drug or sulfonamides.

    - Severe renal and / or hepatic impairment.

    Pindolol:

    - Chronic heart failure in the stage of decompensation, resistant to conventional methods of treatment.

    - "Pulmonary" heart.

    - Pronounced bradycardia.

    - Atrioventricular blockade of II - III degree.

    - Bronchial asthma, chronic obstructive pulmonary disease (COPD).

    - Syndrome of weakness of the sinus node.

    - Cardiogenic shock.

    - Arterial hypotension.

    - Stenocardia of Prinzmetal.

    - Severe violations of peripheral circulation, Reynaud's syndrome (see section Special instructions)

    - Simultaneous administration of monoamine oxidase inhibitors (MAO) (see section "Interaction with other drugs").

    - Joint application with parenteral blockers of "slow" calcium channels such as phenylalkylamines (verapamil) or benzothiazepines (diltiazem) (see section "Interaction with other drugs").

    Clopamid:

    - Hypokalemia, hyponatremia, hypochloraemia, hypocalcemia.

    - Acute glomerulonephritis.

    - Addison's disease.

    "Porphyria."

    - Acute attack of gout.

    - Pregnancy and the period of breastfeeding (risk of development of hypersensitivity to sulphonamides in a newborn)

    - Age before 18 years (effectiveand safety are not established).

    - Lactose intolerance.

    Carefully:

    Feohromatsitoma, ischemic heart disease, atrioventricular blockade I degree, violations peripheral blood circulation, diabetes mellitus, bradycardia, connective tissue diseases (including systemic lupus erythematosus), gout.

    Pregnancy and lactation:The drug is contraindicated in pregnancy and lactation.

    In clinical studies of other beta-blockers, no fetotoxic effects were detected.

    If the mother took pindolol, neonates should be placed under close observation for a period of 2 to 5 days because of the possibility of bradycardia and hypoglycemia, presumably associated with blockade of beta-adrenergic receptors.

    A small amount of pindolol is excreted in breast milk. Although pindolol, falling in this way into the body of a newborn, does not pose a danger to him, caution should be exercised during breastfeeding, as side effects of beta-blockers (bradycardia, etc.) are possible.

    Clopamid can penetrate the placental barrier and increase the concentration of uric acid and creatinine in the amniotic fluid. Changes in the electrolyte balance of the mother can also have a harmful effect on the fetus. If the mother took klopamid in the second half of pregnancy, the newborn may experience perinatal thrombocytopenia.

    For these reasons, Viscaldix is ​​contraindicated in pregnancy.

    The appointment of the drug Viskaldix to women with breastfeeding is also not recommended (this can lead to increased sensitivity to sulfonamides in the child).

    Dosing and Administration:

    The dose should be selected for each patient individually.

    Recommended initial dose - Pabout 1 tablet in the morning. The daily dose can be increased to 2 tablets, and if necessary up to 3 tablets per day, if after 1 - 2 weeks of taking the drug, a satisfactory hypotensive effect is not achieved.

    In case of cancellation of the drug, the dose should be reduced gradually.

    Elderly patients: Adjustment of the dosing regimen is not required.

    For children: Data on the use of the preparation Viskaldix in children before 18 years there.

    NARtheliver and kidney function: When the function is weak or moderate liver and / or kidney correction is not required. The drug is contraindicated in patients with severe hepatic and / or renal insufficiency.

    Side effects:

    Viskaldix usually well tolerated. During the administration of the preparation Viskaldix, the following side effects were described:

    The cardiovascular system: bradycardia, orthostatic hypotension, cardiac heart failure, arrhythmias, Raynaud's syndrome and chest pain. In very rare there may be conduction disturbances. Enhancement of pre-existing violations peripheral circulation, cold extremities.

    The central nervous systemI system: asthenia, fatigue, dizziness, headache, sleep disturbance, less often - depression, hallucinations, sexual dysfunction, impotence, insomnia and nightmares.

    Respiratory system: very rarely - dyspnoea with physical exertion. Even less often - bronchospasm (even in the absence of obstructive pulmonary disease).

    The digestive tract: disorders of the gastrointestinal tract; mainly - nausea, abdominal pain, diarrhea, constipation, dry mouth.

    Musculoskeletal system: muscle spasms and tremors.

    Changes metabolism: hypoglycemia. Decreased glucose tolerance in diabetes mellitus. Activation of latent diabetes mellitus. It is difficult to normalize the blood glucose level. Reduces high-density lipoprotein cholesterol and increases triglyceride levels. Hypokalemia, hypomagnesemia, hyponatremia, hypochloraemia, hypocalcemia, hyperuricemia, acute attack of gout.

    Skin: In rare cases, skin changes, erythema and urticaria are observed. Psoriasis-like skin lesions. Reversible alopecia.

    Changes in laboratory indicators: In special cases, the appearance of antinuclear antibodies is described. In some cases - thrombocytopenia and leukopenia.

    The use of Viskaldix should be discontinued if one of the symptoms listed above is observed continuously and its association with the use of the drug can not be unequivocally rejected.

    Overdose:

    By toxicity pindolol is one of the least toxic beta-blockers. Toxic symptoms were not observed in one patient who took a single dose of 480 mg.

    Symptoms: nausea, vomiting, diarrhea, thirst, hypokalemia, muscle weakness, bradycardia or tachycardia, lowering blood pressure, hypoglycemia, dizziness, insomnia, confusion.

    Other overdose management measures require intensive care and careful monitoring of the patient (control of blood circulation and respiration parameters, kidney function, blood glucose level, blood serum electrolytes) in combination with conventional nonspecific therapy (remove the unsweetened preparation as soon as possible by washing the stomach and taking activated charcoal ), parenteral administration of fluid and electrolytes.

    With a pronounced decrease in blood pressure and bradycardia - intravenous injection of 0.5 - 1 mg of atropine (if necessary, higher doses can be administered); if the desired effect is not achieved, an implantation of a temporary pacemaker is recommended.

    You can try to suppress the effects of a pronounced beta blockade with isoprenaline infusion (0.5-5 μg / min, not more than 30 μg / min) or dobutamine (2.5-10 μg / kg per 1 min, no more than 40 μg / kg per 1 min).

    In case of circulatory insufficiency, it is possible to use means that increase the intracellular level of cAMP by means of mechanisms that are not connected with beta-adrenergic receptors: I / 10 mg of glitchgit can be repeated after 1 hour and, if necessary, continue by infusion at a rate of 1 to 3 mg / h.

    With a strong bronchospasm, you can enter aminophylline intravenous or beta-agonist (eg, isoprenaline) by iv injection or aerosol inhalation.

    Interaction:

    Never combine with the following:

    - parenteral blockers of "slow" calcium channels such as phenylalkylamines (verapamil) or benzothiazepines;

    - MAO inhibitors (theoretically, the risk of a pronounced decrease in blood pressure persists for 14 days after the abolition of the MAO inhibitor).

    - lithium (reduced excretion of lithium by the kidneys).

    Care should be taken when combining with the following medicines:

    For both components:

    - Other antihypertensive drugs (increased risk of hypotension and / or bradycardia).

    - Glycosides of digitalis (risk of bradycardia, conduction disorders; pindolol does not affect the positive inotropic effect of digitalis, but the digitalis glycosides can increase hypokalemia and cause arrhythmia).

    - Oral hypoglycemic agents and insulin (albeit with a lower probability; pindolol, t.it is a beta-blocker with CMA, can enhance hypoglycemic effects of hypoglycemic agents so that hypoglycemia can be recognized only by excessive sweating). Patients with diabetes who use Viscaldix should learn to recognizeь hypoglycemic episodes on the occurrence of increased sweating. BedbugsMr. can weaken the effects of hypoglycemic agents for oral administration.

    - Systemic non-steroidal anti-inflammatory drugs, corticosteroids. tetrakosaktid (delay sodium and water can weaken the antihypertensive effect: pindolol and clopamid).

    - Substances acting on the central nervous system (eg, hypnotics, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics) and ethanol (risk of hypotension).

    For pindolol

    - Nitrates (risk of arterial hypotension).

    - With the simultaneous use of clonidine and guanfacin with pindolol, they cant provoke more severe withdrawal symptoms; therefore Viskaldix should be canceled first in such combinations.

    - Antiarrhythmic agents, blockers of "slow" calcium channels for oral intake of the type of phenylalkylamines (verapamil) or benzothiazepines (diltiazem), parasympathomimetics (risk of arterial hypotension, bradycardia and atrioventricular blockade).

    - Means that have negative inotropic, chronotropic and dromotropic effects (risk of amplification of such effects).

    - ergot alkaloids (risk of peripheral ischemia).

    - Phenotiazines and beta-blockers in a joint application can increase each other's levels in blood plasma.

    - Means for general anesthesia (oppression of heart function).

    - Alpha- and beta-sympathomimetics (risk of arterial hypertension, severe bradycardia, the possibility of stopping the median).

    - Xanthine derivatives (mutually weaken each other's effects, beta-adrenoblockers can reduce the clearance of theophylline).

    - Inhibitors of enzymes (eg, cimetidine), can increase the level of beta-adrenoblokatorov in blood plasma and enhance their effects by changing their hepatic metabolism.

    - Inductors of enzymes (rifampicin and barbiturates), can weaken the effects of beta-blockers by reducing their concentration in the blood plasma.

    - Baclofen (possibly increasing the antihypertensive effect).

    - Lidocaine (the concentration of lidocaine in the blood plasma may increase, which increases the risk of side effects on the heart and the nervous system).

    - Radiopaque substances containing iodine (pindolol can suppress compensatory cardiovascular reaction in case of possible shock and arterial hypotension caused by radiopaque substances; If possible, interrupt the course of pindolol intake before the procedure; if the administration of pindolol is necessary, during the procedure should be ready for resuscitation).

    - Amifostine (increased risk of severe arterial hypotension).

    - Mefloquine (increased risk of severe bradycardia).

    Ethanol can enhance the sedative effect of beta-blockers.

    For the clopamid

    - Muscle relaxants (possible hypokalemia enhances their effects).

    - Oral anticoagulants (thiazide diuretics can weaken the effects of anti-coagulyanth).

    - Kolestyramine (binds clopamide and reduces its absorption and effects).

    - Epinephrine and norepinephrine - their effects can be weakened.

    - Quinidine - its excretion may slow down.

    - Amount diuretic effects observed at simultaneous introductionebupamide and furosemide.

    Special instructions:

    In patients with chronic heart failure, the compensation stage should be achieved before starting the preparation of Viskaldix.

    In the acute stage of myocardial infarction or in patients with a history of myocardial infarction, the parameters of hemodynamics should be carefully monitored while taking pindolol. Due to its own sympathomimetic activity (SMA), pindolol Viscaldix does not have a significant effect on respiration in patients predisposed to bronchospasm or suffering from obstructive respiratory diseases. However, such effects can not be completely ruled out, as in the case of the use of other beta-blockers. Therefore, Viscaldix should not be given to patients with bronchial asthma or other obstructive pulmonary disease in a history. If breathing disorders occur, the use of Viscaldix should be stopped immediately and the bronchoconstriction eliminated by appropriate therapy (β2-agonists, derivatives of theophylline). Before surgery, an anesthesiologist should be warned that the patient is taking pindolol, since the cardiodepressor effects of heart-depressing common anesthetics (for example, halothane) may increase.

    If prior to surgery, general anesthesia, or for another reason, it is necessary to interrupt the use of the preparation Viskaldix,dose reduction should be done gradually - ideally for 1 to 2 weeks - and, if necessary, give a replacement drug, as a sharp discontinuation of Viscaldix (especially in patients with coronary heart disease) can worsen a patient's condition and provoke an attack of angina or even myocardial infarction due to increased activity of beta-receptors).

    Despite the fact that due to its own sympathomimetic activity (CMA), the undesirable effect of pindolol on the peripheral circulation is less pronounced than that of other beta adrenoblockers without SMA, Viscaldix should not be given to patients with severe obliterating peripheral vascular lesions and Raynaud's syndrome. Symptoms (paresthesias and cold extremities) of the existing (possibly latent) insufficiency of peripheral circulation may worsen during the administration of Viscaldix. Regular monitoring of blood pressure, glucose and uric acid in the blood, as well as electrolytes of blood serum should be regularly monitored. It may be necessary to introduce additional potassium.

    Treatment of patients with diabetes or on a diet requires special care, since pindolol can cause hypoglycemia and mask some of its symptoms (for example, tachycardia), and the only sign of hypoglycemia sometimes remains sweating. When prescribing a drug for people with diabetes mellitus, there may be a need for a new correction of carbohydrate metabolism.

    In patients with pheochromocytoma, Viscaldix always followst combine with alpha-blockers.

    The patient's existing atrial-ventricular arrhythmias can progress to atrioventricular block. Therefore, caution is needed when prescribing Viscaldix to patients with stage I atrioventricular block. In patients predisposed to anaphylactic reactions to various antigens, Viscaldix may increase sensitivity to allergens and enhance anaphylactic reactions. It may be necessary to increase the dosage of pressor amines. The dose of the drug should be reduced when the heart rate at rest becomes below 50 - 55 beats / min, and this is accompanied by clinical symptoms. β-adrenoconjugators increase the symptoms of psoriasis.

    In predisposed patients, clopamid may contribute to the development and / or exacerbation of systemic lupus erythematosus.

    Athletes should be warned that one of the active ingredients of the drug (pindolol) can give a positive result with some doping tests. Each tablet contains 96,8 mg lactose, what should be consider sick with intolerance to lactose.

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

    The drug may have a negative effect on the ability of the patient to drive vehicles or mechanisms, especially at the beginning of the course of treatment and with the concomitant use of alcohol. Therefore, the degree of the corresponding restrictions is determined for each patient individually.

    Form release / dosage:

    Tablets 5 mg +10 mg.

    Packaging:10 tablets in blisters from PVDC / al. foil. 2 blisters together with instructions for use in a cardboard box.
    Storage conditions:

    At a temperature of no higher than 25 ° C in a dark place. Keep out of the reach of children!

    Shelf life:

    5 years. Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013484 / 01
    Date of registration:26.12.2007 / 05.02.2015
    Expiration Date:Unlimited
    Date of cancellation:2017-12-14
    The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Manufacturer: & nbsp
    Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Information update date: & nbsp14.12.2017
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