Torendo kutab instructions for use. Zalasta Ku-Tab: instructions for use of tablets. Terms and conditions of storage

Registration number: P N001049/02 dated 12/12/2007
Trade name: CYCLOFERON®
Dosage form: enteric-coated tablets.

Group name: meglumine acridone acetate

Compound:

One tablet contains: active substance– meglumine acridone acetate in terms of acridone acetic acid – 150.00 mg, obtained according to the following recipe: acridone acetic acid – 150.00 mg, meglumine (N-methylglucamine) – 146.00 mg;
excipients: povidone K 30 - 7.93 mg, calcium stearate - 3.07 mg, hypromellose - 2.73 mg, polysorbate 80 - 0.27 mg;
enteric coating: methacrylic acid and ethyl acrylate copolymer – 23.21 mg, propylene glycol – 1.79 mg.

Description: round biconvex tablets yellow color, covered with an enteric coating. On a cross section, the kernel is yellow.

Pharmacotherapeutic group: immunostimulating agent. ATX code – L03AX

Pharmacological properties

Pharmacodynamics

Cycloferon is a low-molecular-weight interferon inducer, which determines a wide range of its biological activity (antiviral, immunomodulatory, anti-inflammatory, etc.). Cycloferon is effective against herpes viruses, influenza and other pathogens of acute respiratory diseases. Has a direct antiviral effect, suppressing viral reproduction early stages(days 1–5) of the infectious process, reducing the infectivity of the viral progeny, leading to the formation of defective viral particles. Increases the body's nonspecific resistance to viral and bacterial infections.

Pharmacokinetics

When taking a daily dose, the maximum concentration in the blood plasma is reached after 2–3 hours, gradually decreases by the 8th hour, and after 24 hours Cycloferon is detected in trace amounts. The half-life of the drug is 4–5 hours, so its use in recommended doses does not create conditions for accumulation in the body.

Indications for use

In adults in complex therapy:

herpetic infection.

In children starting from four years of age in complex therapy:

influenza and acute respiratory diseases;
herpetic infection.

In children over four years of age for the prevention of influenza and acute respiratory diseases.

Contraindications

Pregnancy, period breastfeeding, childhood up to 4 years (due to imperfect swallowing), individual intolerance to the components of the drug, decompensated cirrhosis of the liver.

Carefully

For diseases of the digestive system in the acute stage (erosion, gastric and/or duodenal ulcers, gastritis and duodenitis) and a history of allergic reactions before taking the drug, be sure to consult your doctor.

During pregnancy and breastfeeding

The use of the drug during pregnancy and breastfeeding is contraindicated.

Directions for use and doses

Orally once a day 30 minutes before meals, without chewing, with ½ glass of water, in age-specific dosages:

children 4–6 years old: 150 mg (1 tablet) per dose;
children 7–11 years old: 300–450 mg (2–3 tablets) per dose;
adults and children over 12 years of age: 450–600 mg (3–4 tablets) per dose.

It is advisable to repeat the course 2–3 weeks after the end of the first course.

In adults:

When treating influenza and acute respiratory diseases, the drug is taken on days 1, 2, 4, 6, 8 (course of treatment - 20 tablets). Treatment should begin at the first symptoms of the disease.
For severe flu, take six tablets on the first day. If necessary, additional symptomatic therapy is carried out (antipyretics, analgesics, expectorants).
For herpes infection, the drug is taken on days 1, 2, 4, 6, 8, 11, 14, 17, 20, 23 (course of treatment - 40 tablets). Treatment is most effective when the first symptoms of the disease appear.

In children from four years of age:

For influenza and acute respiratory diseases, the drug is taken in age-specific doses on days 1, 2, 4, 6, 8, 11, 14, 17, 20, 23. The course of treatment ranges from 5 to 10 doses, depending on the severity of the condition and severity clinical symptoms.
For herpes infection, the drug is taken on the 1st, 2nd, 4th, 6th, 8th, 11th, 14th day of treatment. The course of treatment may vary depending on the severity of the condition and the severity of clinical symptoms.
For emergency nonspecific prevention of influenza and acute respiratory diseases (in direct contact with patients with influenza or acute respiratory infections of another etiology, during an influenza epidemic): on the 1st, 2nd, 4th, 6th, 8th day. Next, take a break of 72 hours (three days) and continue the course on the 11th, 14th, 17th, 20th, 23rd day. The general course is from 5 to 10 doses.

Side effects

According to the World Health Organization, adverse effects are classified according to their frequency as follows:

– very frequent (≥ 1/10);
– common (≥ 1/100 – – uncommon (≥ 1/1000 – – rare (≥ 1/10000 – – very rare ( – frequency unknown (cannot be determined based on available data).
Violations by immune system: very rarely – angioedema.
Disorders of the skin and subcutaneous tissues: very rarely - rash, urticaria.
If any of the undesirable effects indicated in the instructions get worse or you notice any other undesirable effects not listed in the instructions, tell your doctor.

Overdose

There is no information about an overdose of the drug.

Interaction with other drugs

Cycloferon is compatible with all drugs used in the treatment of these diseases (interferons, chemotherapy, symptomatic drugs, etc.). Enhances the effect of interferons and nucleoside analogues. Reduces side effects chemotherapy, interferon therapy.

special instructions

Cycloferon does not affect the ability to drive vehicles.
For diseases of the thyroid gland, consultation with an endocrinologist is necessary.
If the next dose of the drug is missed, then you should, at the first opportunity, without taking into account the time interval and doubling the dosage, continue the course according to the started regimen.
If there is no therapeutic effect, you should consult a doctor.

Release form

Latin name: Zalasta
ATX code: N05AH03
Active substance: Olanzapine
Manufacturer: KRKA POLSKA, Sp.z.o.o (Poland).
Release from the pharmacy: On prescription
Storage conditions: no more than 30 0 C.
Best before date: 36 months.

The medicine Zalasta Ku-Tab is good remedy to restore the nervous system and eliminate its severe disorders. This is an antipsychotic drug that has pronounced antipsychotic effects. Only a doctor should prescribe it, because using it on your own can have a negative impact on your health. But still, you should first carefully study all its important features and rules of use.

Indications for use

Before using Zalasta Ku-Tab, you should carefully consider the indications. It is usually used to treat nervous system disorders from the following list:

as part of the treatment of manifestations of schizophrenia. This tool provides beneficial maintenance of improvement in clinical symptoms during long-term treatment therapy in patients who have a positive initial response to the medication;
used in the treatment of moderate and severe manifestations of mania;
in the preventive treatment of mania during bipolar disorder.

Composition and release forms

The action and effect of the drug is ensured due to its composition. It is important to know what components it includes:

The active ingredient of the drug is olanzapine. It is thanks to him that the antipsychic effect occurs;
Auxiliary elements include cellactose, pregelatinized starch powder, colloidal anhydrous silicon dioxide, corn starch, and so on.

Zalasta is produced in tablet form. It is imperative to consider their description - they have a light yellow tint, are covered with a shell with an enteric structure, and have a biconvex shape. There is an inscription “5” at the top. Small inclusions of dark color are allowed on the surface.

Each blister contains 7 tablets. Blisters are placed in packs made of cardboard base. Each pack contains 4 blisters.

Medicinal properties

Zalasta is an antipsychotic medication that has a wide pharmacological spectrum of effects. It is an antipsychotic that can have different effects, which have some important features:

the neuroleptic effect is associated with blocking dopamine D2 receptors included in the mesolimbic and mesocortical systems;
the sedative effect is achieved by blocking the adrenergic receptors of the reticular formation in the brain stem;
the medication has an antiemetic effect. It is achieved by blocking dopamine D2 receptors in the trigger area of the vomiting center;
The hypothermic property is produced as a result of blocking dopamine receptors in the hypothalamus.

When using the medicine, its active component olanzapine inhibits the activity of reproductive symptoms - eliminates the manifestations of delusions and hallucinations. It also prevents the development of negative manifestations of mental states.

Pharmacokinetics

The cost of one package of Zalasta is 1200-1500 rubles.

The main element is capable of exhibiting an increased absorption rate; it does not depend on food consumption. Achieving the maximum concentration of olanzapine in blood plasma after oral administration lasts 5-8 hours.

The binding rate to proteins (albumin and glycoprotein) reaches 93%. The main element enters through histohematic barriers, namely the BBB. Metabolization occurs in the liver. Excretion is carried out mainly by the kidneys. Excreted in urine in the form of metabolites.

Mode of application

Zalasta must be taken orally. The instructions for use recommend taking the tablets correctly; to do this, you should follow these steps:

the medicine should be used once a day;
Usage is not affected by food intake;
the initial dose of medication for schizophrenia should be 10 mg per day;
to eliminate all manifestations of mania, you should take 10-20 mg per day at a time;
the medication is often taken in combination treatment therapy. Take 10 mg at a time.

According to the patient's condition, the dosage of the medication can be adjusted. If it is used as part of preventive therapy for manifestations of bipolar disorders that occur in remission, then the initial dosage of the drug should be 10 mg per day. Discontinuation of medication should be done slowly.

During pregnancy and breastfeeding

Studies on the effect of the active substance olanzapine on the development of pregnancy and the formation of the unborn child have not been conducted. There are facts about the effect the substance has during this period. However, the use of the drug while carrying a baby is allowed provided that the positive effect for the mother is greater possible harm for a child.

Before treatment with Zalasta is prescribed, women should tell their doctor if they are pregnant or planning to become pregnant. In rare cases, therapy using this medication causes tremor. Also, sometimes arterial hypertension, signs of lethargy, and drowsiness may appear in children who were born to mothers who used the medication in the last term.

Numerous studies of the drug have shown that the constituent components pass into breast milk. The average dose that the baby receives when the equilibrium concentration of the active substance is reached should be 1.8% of the total dosage. It is for this reason that Zalasta Ku-Tab is not recommended for use during breastfeeding.

Contraindications and precautions

When using Zalasta medication, you should take into account the following contraindications:

contraindicated for angle-closure glaucoma;
not for teenagers under 18 years of age;
while breastfeeding;
in no case should it be taken if galactose intolerance, lapp lactase deficiency or glucose-galactose malabsorption have been identified;
not used if available increased sensitivity to the constituent elements.

There is a list of conditions for which you should take the medicine with caution:

if you have heart, kidney or liver failure
if signs of prostate hyperplasia are detected
if manifestations of intestinal obstruction in paralytic form are detected
during seizures during epilepsy
if seizures of convulsive syndrome are possible
for leukopenia and neutropenia of different origins
for pathologies with cerebrovascular and cardiovascular nature
patients elderly age no group.

In addition, when using it is worth considering special instructions:

If it is taken by people with diabetes, it is important to constantly monitor blood glucose levels. Sometimes when using the medication, manifestations of hyperglycemia or decompensation of diabetes mellitus occur;
Abrupt withdrawal of medication can rarely cause unpleasant conditions - excessive sweating, sleep disturbances, tremor, anxiety, nausea and vomiting. It is advisable that when discontinuing the use of the medication, the dosage should be reduced gradually;
Zalasta Ku-Tab tablets should not be used in the treatment of psychosis during Parkinson's disease, which is caused by the use of dopaminomimetics. In these situations, manifestations of parkinsonism and hallucinations intensify;
due to the fact that there is a high mortality rate, the medicine is not recommended for use as part of therapeutic therapy during psychosis and behavioral disorders during dementia;
It is imperative to exercise caution when taking it simultaneously with other centrally acting medications and alcohol-containing drinks;
Used with caution by people in the elderly group, they may experience signs of postural hypotension. In patients over 65 years of age, constant monitoring of blood pressure is required;
in very rare situations, the use of medications containing olanzapine causes the development of venous thromboembolism;
You should not drive a car while taking an antipsychotic, or perform work that requires increased attention. The fact is that the medication may slightly reduce concentration.

Cross-drug interactions

When taken as monotherapy, it rarely causes unpleasant symptoms. But if the medication is combined with other medications, unexpected conditions may appear. To avoid this, you should pay attention to the interaction of Zalasta Ku-Tab with other medications:

It is not recommended to take it together with activated carbon. The fact is that when taking Zalasta with this sorbent, the absorption rate of olanzapine drops by 50-60%;
olanzapine reduces the effectiveness of dopamine agonists;
Caution must be exercised during simultaneous use with other medications with central effects;
when using Zalasta with alcoholic drinks the drug may have a depressive effect on the nervous system.

Side effects

Many patients claim that no side symptoms develop while taking the drug, but this is only if you follow all the recommendations indicated in the instructions. But still, do not forget that Zalasta Ku-Tab has a number of side effects:

sometimes arterial hypotension occurs
drowsiness may occur
dizziness
dry mouth
problems with stool
increased appetite
signs of asthenia
weight gain
manifestations of eosinophilia
rashes on the surface of the skin
itching sensation
urticaria symptoms
swelling
problems with gait
body temperature may rise
visual hallucinations.

Overdose

It is necessary to use the drug Zalasta correctly; for this it is recommended to follow all the recommendations indicated in the instructions. If the medicine is used in a high dose, the following conditions may occur:

overexcitement, aggressiveness
extrapyramidal manifestations
tachycardia
decreased consciousness, coma may develop
rarely decreases arterial pressure, the person may fall into a coma, cardiac arrhythmia may occur, and sometimes convulsions may occur
In case of acute overdose, if a dose of 450 mg is taken, death can occur.

During an overdose, it is important to provide symptomatic treatment depending on the symptomatic condition of the patient. It is also important to monitor the functioning of vital organs.

Analogues

Sometimes there are cases when the drug Zalasta Ku-Tab cannot be used. This may be due to contraindications or side symptoms. Also, this medication is not always available in pharmacies. For this reason, it is necessary to know what other antipsychotic drugs are that have a similar composition and effect.

Manufacturer: NOVARTIS PHARMACEUTICALS U.K., Ltd. (Great Britain).

Price: from 990-1700 rubles.

It's a neuroleptic. It has antipsychotic, sedative and antihistamine properties. It is used in the treatment of schizophrenia in patients who are resistant to the effects of other antipsychotics or lack a therapeutic effect. It is also recommended to be taken in therapy to prevent the development of relapses of suicide attempts in patients who have schizoid disorders, when treating manifestations of psychosis.

Pros:

good action
easy application
rarely causes adverse symptoms.

Minuses:

there are contraindications
high price
available by prescription.

Manufacturer: Eli Lilly (UK), Lilly del Caribe Inc. (Puerto Rico), Patheon Italia (Italy).

Price: from 2500 to 5000 rubles.

The medication has a strong antipsychotic effect. The composition contains the main element olanzapine. It is produced in two forms - tablets and powder from which the solution is made. It is recommended for use in the treatment of acute manifestations of schizophrenia, chronic forms of delusional disorders, to eliminate bipolar psychosis, schizoaffective disorders with productive symptoms.

Pros:

several release forms
high efficiency
few side symptoms.

Minuses:

there are contraindications
high price
Sold only upon presentation of a prescription.

Manufacturer: Sun Pharmaceutical Industries Ltd (India).

Price: from 150 to 500 rubles.

Thiodazine is an antipsychotic drug used to treat nervous system disorders. The composition contains the active substance – thioridazine hydrochloride. Its dosage can be different - 10 mg, 25 mg, 50 mg and 100 mg. Available in the form of film-coated tablets. It is recommended to take it for exacerbation of schizophrenia, for chronic schizophrenia, depression, anxiety, psychosomatic disorders and emotional disorders.

Pros:

easy to use
affordable price
high efficiency.

Minuses:

there are contraindications
prescription
many side symptoms.

Be sure to read these instructions for use of MAXICOLD ® tablets and consult a specialist before taking this drug.

Registration number: LP-000077

Trade name of the drug: Maxicold ®

International nonproprietary or generic name: Paracetamol + Phenylephrine + [Ascorbic acid]

Dosage form: film-coated tablets

Composition per tablet

Active substances: paracetamol - 500 mg, phenylephrine hydrochloride - 10 mg, ascorbic acid - 30 mg.

Excipients:
core: croscarmellose sodium - 28.00 mg, calcium hydrogen phosphate - 82.62 mg, ethylcellulose - 0.20 mg, hyprolose (hydroxypropylcellulose) - 35.00 mg, magnesium stearate - 7.00 mg, talc - 7.00 mg, solar dye sunset yellow (E 110) - 0.18 mg;
shell: hypromellose (hydroxypropyl methylcellulose) - 13.200 mg, hyprolose (hydroxypropylcellulose) - 7.701 mg, talc - 6.300 mg, titanium dioxide - 2.750 mg, sunset yellow dye (E 110) - 0.049 mg or OPADRY 20A230018 Orange (OPADRY 20A2 30018 Orange) - 30.00 mg [Hypromellose (hydroxypropylmethylcellulose) - 13.200 mg, hyprolose (hydroxypropylcellulose) - 7.701 mg, talc - 6.300 mg, titanium dioxide - 2.750 mg, sunset yellow dye (E 110) - 0.049 mg].

Description

Tablets, film-coated, pinkish-orange, oval, doubly convex with a score. On a cross section, the tablet is pinkish-orange in color with white and orange splashes.

Pharmacotherapeutic group: a remedy for eliminating the symptoms of acute respiratory diseases (ARI) and “colds” (non-narcotic analgesic + alpha-adrenergic agonist + vitamin).

ATX code:

Pharmacological properties

The combined drug has an antipyretic and analgesic effect, intended to relieve the symptoms of colds and flu.

The effect of the drug is due to the properties of its constituent components.

Paracetamol– a non-narcotic analgesic, has an antipyretic and analgesic effect due to the blockade of cyclooxygenase in the central nervous system and the effect on the centers of pain and thermoregulation. Reduces headaches, muscle pain, and fever.

Phenylephrine– alpha1-adrenergic stimulant, which has little effect on beta-adrenergic receptors of the heart; is not a catecholamine. Causes a narrowing of arterioles, thereby reducing swelling and hyperemia of the nasal mucosa, making breathing through the nose easier.

Ascorbic acid– increases the body’s resistance to infections, replenishes the increased need for vitamin C during colds and flu.

Pharmacokinetics

Paracetamol: well absorbed in the intestine, time to reach maximum concentration (Tmax) is 0.5-2 hours; connection with plasma proteins – 15%. Metabolized in the liver to form both active and inactive metabolites. The half-life (T1/2) is 1-4 hours. It is predominantly excreted by the kidneys in the form of metabolites - glucuronides and sulfates, 3% - unchanged.

Phenylephrine: After oral administration, phenylephrine is poorly absorbed from the gastrointestinal tract (GIT). Metabolized with the participation of monoamine oxidase (MAO) in the intestinal wall and during the “first pass” through the liver. The bioavailability of phenylephrine is low.

Ascorbic acid: Absorbed in the gastrointestinal tract (mainly in the jejunum). Tmax after oral administration – 4 hours. Easily penetrates into leukocytes, platelets, and then into all tissues; the highest concentration is achieved in the glandular organs, leukocytes, liver and lens of the eye; penetrates the placenta. Metabolized primarily in the liver into deoxyascorbic acid and further into oxaloacetic acid and ascorbate-2-sulfate. Excreted by the kidneys, through the intestines, with sweat, breast milk unchanged and in the form of metabolites.

Indications

Symptomatic treatment of infectious and inflammatory diseases (including influenza and other acute respiratory viral infections (ARVI)), accompanied by elevated temperature body, chills, nasal congestion, headache, pain in bones and muscles, in the throat and sinuses.

Contraindications

Hypersensitivity to any component of the drug; severe renal/liver failure; hyperthyroidism (including thyrotoxicosis); heart disease (severe stenosis of the aortic mouth, acute myocardial infarction, tachyarrhythmias); arterial hypertension; simultaneous use of tricyclic antidepressants, beta-blockers, monoamine oxidase inhibitors, incl. within 14 days after cancellation; simultaneous use of other paracetamol-containing drugs and drugs to relieve symptoms of colds, flu and nasal congestion; prostatic hyperplasia; angle-closure glaucoma; children's age (up to 9 years, as well as children weighing less than 30 kg).

Use with caution

With deficiency of glucose-6-phosphate dehydrogenase, with benign hyperbilirubinemia, during pregnancy and lactation, in old age.

Directions for use and doses

Orally, before meals or 1-2 hours after meals, with plenty of liquid.

Adults and children over 12 years of age (body weight over 40 kg): 1-2 tablets every 4-6 hours. The frequency of administration is no more than 4 times a day with an interval of at least 4 hours.

Children aged 9 to 12 years (body weight more than 30 kg): 1 tablet every 4-6 hours. The frequency of administration is no more than 4 times a day with an interval of at least 4 hours.

DO NOT EXCEED THE SPECIFIED DOSE.

Side effect

Allergic reactions are possible (skin rash, skin hyperemia, urticaria, angioedema).

Paracetamol: hematopoietic disorders (anemia, thrombocytopenia, methemoglobinemia). Phenylephrine: headache, nausea or vomiting; angina pectoris, bradycardia, shortness of breath, increased or decreased blood pressure, palpitations, tachycardia, ventricular arrhythmia (especially when used in high doses), irritability, restlessness, allergic reactions.

Ascorbic acid: can cause irritation of the gastrointestinal mucosa; with prolonged use of large doses - nausea, vomiting, diarrhea, hyperacid gastritis, ulceration of the gastrointestinal mucosa; decreased capillary permeability (possible deterioration of tissue trophism, increased blood pressure, hypercoagulation, development of microangiopathies). Thrombocytosis, hyperprothrombinemia, erythropenia, neutrophilic leukocytosis, hypokalemia, glycosuria, and inhibition of the function of the pancreatic insular apparatus are also possible.

With long-term use in doses significantly higher than recommended, the likelihood of renal dysfunction increases (moderate pollakiuria, hyperoxaluria, nephrolithiasis, damage to the glomerular apparatus of the kidneys), increased excitability of the central nervous system, headache, insomnia.
If any unwanted reactions occur, consult your doctor.

Overdose

In case of overdose, seek medical advice immediately medical care even if you feel well, because there is a risk of delayed signs of serious liver damage.

In case of overdose, symptoms are usually caused by exposure to high doses of paracetamol.

Symptoms: during the first 24 hours after administration - pallor of the skin, nausea, vomiting, anorexia, abdominal pain; impaired glucose metabolism, metabolic acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In case of severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis. The hepatotoxic effect in adults occurs when taking 10 g or more.

Treatment: administration of SH-group donors and precursors for the synthesis of glutathione - methionine within 8-9 hours after an overdose and acetylcysteine - within 8 hours. The need for additional therapeutic measures (further administration of methionine, intravenous administration of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Interaction with other drugs

The drug enhances the effects of monoamine oxidase inhibitors, sedatives, and ethanol.

The risk of developing hepatotoxic effects of paracetamol increases with simultaneous intake of ethanol, hepatotoxic medicines, inducers of microsomal oxidation enzymes in the liver (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants, etc.).

Concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (decreased synthesis of procoagulant factors in the liver). Paracetamol reduces the effectiveness of uricosuric drugs.

Long-term use of barbiturates reduces the effectiveness of paracetamol. Metoclopramide and domperidone increase, and cholestyramine reduces the rate of absorption of paracetamol. Inhibitors of microsomal oxidation enzymes (including cimetidine) reduce the risk of hepatotoxic action of paracetamol.

The simultaneous use of ethanol and paracetamol contributes to the development of acute pancreatitis. Long-term combined use of paracetamol and nonsteroidal anti-inflammatory drugs increases the risk of developing “analgesic” nephropathy and renal papillary necrosis, and the onset of end-stage renal failure. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney cancer or Bladder. Diflunisal increases the plasma concentration of paracetamol by 50%, the risk of developing hepatotoxicity. Myelotoxic drugs enhance the hematotoxicity of paracetamol.

Phenylephrine reduces the hypotensive effect of diuretics and antihypertensive drugs (including methyldopa, mecamylamine, guanadrel, guanethidine), and reduces the antianginal effect of nitrates.

Phenothiazines, alpha-blockers (phentolamine), furosemide and other diuretics reduce the hypertensive effect of pheniramine. Monoamine oxidase inhibitors (including furazolidone, procarbazine, selegiline), oxytocin, ergot alkaloids, tricyclic antidepressants, methylphenidate, adrenostimulants enhance the vasoconstrictor effect and arrhythmogenicity of phenylephrine; arterial hypertension is possible against the background of reserpine. Ergometrine, ergotamine, methylergometrine, oxytocin, doxapram increase the severity of the vasoconstrictor effect of pheniramine.

Inhalational anesthetics (including chloroform, enflurane, halothane, isoflurane, methoxyflurane) increase the risk of severe atrial and ventricular arrhythmias. Thyroid hormones increase (mutually) the effect of phenylephrine and the associated risk of coronary insufficiency (especially in coronary atherosclerosis).

Ascorbic acid increases the concentration of benzylpenicillin and tetracyclines in the blood, reduces the effectiveness of heparin and indirect anticoagulants, increases the overall clearance of ethanol, which in turn reduces the concentration ascorbic acid in the body, reduces the therapeutic effect of antipsychotic drugs (neuroleptics) phenothiazine derivatives, tubular reabsorption of amphetamine and tricyclic antidepressants.

When used simultaneously with acetylsalicylic acid, the urinary excretion of ascorbic acid increases and the excretion of acetylsalicylic acid decreases. Acetylsalicylic acid, oral contraceptives, fresh juices and alkaline drinks reduce the absorption and absorption of ascorbic acid.

Ascorbic acid improves the absorption of iron preparations in the intestine; increases the risk of developing crystalluria during treatment with salicylates and short-acting sulfonamides, slows down the excretion of acids by the kidneys, increases the excretion of drugs that have an alkaline reaction (including alkaloids), reduces the concentration of oral contraceptives in the blood, and reduces the chronotropic effect of isoprenaline. With long-term use or use in high doses, it can interfere with the interaction of disulfiram and ethanol; in high doses, it increases the excretion of mexiletine by the kidneys.

Quinoline drugs, calcium chloride, salicylates, and glucocorticoids deplete ascorbic acid reserves when used for a long time. Barbiturates and primidone increase the excretion of ascorbic acid in the urine.

special instructions

Before taking the drug, consult a doctor in case of concomitant use of metoclopramide, domperidone, cholestyramine (due to the fact that metoclopramide and domperidone increase, and cholestyramine reduces the rate of absorption of paracetamol), anticoagulants (since the concomitant use of paracetamol in high doses increases the effect of anticoagulant medicines).

Taking the drug distorts the results of laboratory tests assessing the concentration of glucose and uric acid in plasma.

When using the drug for more than 5-7 days, peripheral blood counts and the functional state of the liver should be monitored.

The use of the drug during pregnancy is possible only as prescribed by a doctor.

TO AVOID TOXIC DAMAGE TO THE LIVER, THE DRUG SHOULD NOT BE COMBINED WITH ALCOHOL BEVERAGES, OR TAKEN BY PERSONS WITH CHRONIC ALCOHOLISM.

The drug does not have a negative effect on the performance of potentially hazardous activities that require special attention and quick reactions.

Release form

Film-coated tablets.

2, 10 or 12 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

1 or 2 blister packs with instructions for use in a cardboard pack.

Storage conditions

In a dry place at a temperature not exceeding 25 °C. Keep out of the reach of children!

Best before date

1 year. Do not use after the expiration date stated on the package.

Excipients: mannitol, basic butyl methacrylate copolymer, microcrystalline cellulose, hyprolose (low-substituted hydroxypropylcellulose LH-21), aspartame, crospovidone, red iron oxide (E172), mint and menthol flavoring, calcium silicate, magnesium stearate.

10 pieces. - blisters (3) - cardboard packs.

pharmachologic effect

Antipsychotic drug (neuroleptic), benzisoxazole derivative. It has a high affinity for serotonin 5-HT 2 and dopamine D 2 receptors. Binds to α 1 -adrenergic receptors and, with slightly lower affinity, to histamine H 1 -receptors and α 2 -adrenergic receptors. Has no affinity for cholinergic receptors. Although risperidone is a potent D 2 -antagonist (which is believed to be the main mechanism for improving the productive symptoms of schizophrenia), it causes less pronounced suppression of motor activity and induces catalepsy to a lesser extent than classical antipsychotics. Due to balanced antagonism to serotonin and dopamine receptors in the central nervous system, the likelihood of developing extrapyramidal side effects is reduced.

Risperidone may induce a dose-dependent increase in prolactin concentrations in the blood.

Pharmacokinetics

After oral administration, risperidone is completely absorbed from the gastrointestinal tract, Cmax in plasma is reached within 1-2 hours. Food does not affect the absorption of risperidone.

C ss of risperidone in the body is achieved within 1 day in most patients. C ss 9-hydroxyrisperidone is achieved within 4-5 days. Plasma concentrations of risperidone are dose proportional (over the therapeutic dose range).

Risperidone is quickly distributed in the body, Vd is 1-2 l/kg. In plasma, risperidone binds to alpha 1-glycoprotein. The binding of risperidone to plasma proteins is 88%, 9-hydroxyrisperidone - 77%.

Risperidone is metabolized in the liver with the participation of the CYP2D6 isoenzyme with the formation of 9-hydroxyrisperidone, which has a pharmacological effect similar to risperidone. The antipsychotic effect is due to the pharmacological activity of risperidone and 9-hydroxyrisperidone. Another route of metabolism for risperidone is N-dealkylation.

After oral administration in patients with psychosis, T1/2 of risperidone from plasma is 3 hours. T1/2 of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours.

After 1 week of use, 70% is excreted in the urine, 14% in feces. In urine, the total content of risperidone and 9-hydroxyrisperidone is 35-45%. The rest is inactive metabolites.

In elderly patients and in patients with renal insufficiency, increased plasma concentrations and delayed elimination of risperidone were observed after a single oral dose.

Indications

Treatment of schizophrenia (including new-onset acute psychosis, acute attack of schizophrenia, chronic schizophrenia); psychotic states with pronounced productive (hallucinations, delusions, thought disorders, hostility, suspicion) and/or negative (blunted affect, emotional and social detachment, poverty of speech) symptoms; to reduce affective symptoms (depression, guilt, anxiety) in patients with schizophrenia; prevention of relapses (acute psychotic states) in chronic schizophrenia; treatment of behavioral disorders in patients with dementia with symptoms of aggressiveness (outbursts of anger, physical violence), disturbances mental activity(agitation, delirium) or psychotic symptoms; treatment of mania in bipolar disorders (as a mood stabilizer as an adjuvant therapy).

Contraindications

Hypersensitivity to risperidone.

Dosage

Individual. When taken orally, the initial dose for adults is 0.25-2 mg/day, on the 2nd day - 4 mg/day. Then the dose can either be kept at the same level or, if necessary, adjusted. Typically, the optimal therapeutic dose, depending on the indications, is in the range of 0.5-6 mg/day. In some cases, a slower dose escalation and lower initial and maintenance doses may be justified.

For schizophrenia, for elderly patients, as well as for concomitant liver and kidney diseases, an initial dose of 500 mcg 2 times a day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times a day.

Maximum dose: When using risperidone at a dose of more than 10 mg/day, there is no increase in effectiveness compared to lower doses, but the risk of developing extrapyramidal symptoms increases. The safety of risperidone in doses greater than 16 mg/day has not been studied, so further excess of the dose is not allowed.

Side effects

From the side of the central nervous system: often - insomnia, agitation, anxiety, headache; possible - drowsiness, fatigue, dizziness, impaired ability to concentrate, impaired vision clarity; rarely - extrapyramidal symptoms (including tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia). Patients with schizophrenia may experience tardive dyskinesia, NMS, thermoregulation disorders, and seizures.

From the outside digestive system: constipation, dyspeptic symptoms, nausea, vomiting, abdominal pain, increased activity of liver enzymes.

From the reproductive system: priapism, erectile dysfunction, ejaculation disorders, orgasm disorders.

From the cardiovascular system: rarely - orthostatic hypotension and reflex tachycardia, arterial hypertension.

From the endocrine system: galactorrhea, gynecomastia, disorders menstrual cycle, amenorrhea, weight gain.

From the hematopoietic system: a slight decrease in the number of neutrophils and/or platelets.

Allergic reactions: rhinitis, skin rash, angioedema.

Others: urinary incontinence.

Drug interactions

With the simultaneous use of inducers of microsomal liver enzymes, a decrease in the concentration of risperidone in the blood plasma is possible.

When used simultaneously with phenothiazine derivatives, tricyclic antidepressants, it is possible to increase the concentration of risperidone in the blood plasma.

When used simultaneously with carbamazepine, the concentration of risperidone in the blood plasma is significantly reduced.

When used concomitantly, risperidone reduces the effects of levodopa and other dopamine receptor agonists.

When used simultaneously with, it is possible to increase the concentration of risperidone in the blood plasma.

special instructions

Use with caution in patients with diseases of the cardiovascular system (including heart failure, myocardial infarction, cardiac muscle conduction disorders), as well as in cases of dehydration, hypovolemia or cerebrovascular disorders. In this category of patients, the dose should be increased gradually.

The risk of developing orthostatic hypotension is especially increased in the initial period of dose selection. If hypotension occurs, dose reduction should be considered.

When using drugs that have the properties of dopamine receptor antagonists, the occurrence of tardive dyskinesia, characterized by involuntary rhythmic movements (mainly of the tongue and/or face), was noted. There are reports that the occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. Risperidone causes extrapyramidal symptoms to a lesser extent than classical antipsychotics. If symptoms of tardive dyskinesia occur, discontinuation of all antipsychotic medications should be considered.

If NMS develops, all antipsychotics, including risperidone, should be discontinued.

Risperidone should be used with caution in patients with Parkinson's disease, as it is theoretically possible that the disease may worsen.

Classical antipsychotics are known to lower the seizure threshold. Given this, risperidone is recommended to be used with caution in patients with epilepsy.

Risperidone should be used with caution in combination with other centrally acting drugs.

When discontinuing other hepatic enzyme inducers, the dose of risperidone should be reconsidered and, if necessary, reduced.

There are no data on the safety of risperidone in children under 15 years of age.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, until individual sensitivity to risperidone is determined, patients should avoid driving vehicles and other activities that require high concentration and speed of psychomotor reactions.

For liver dysfunction

For schizophrenia with concomitant liver diseases, an initial dose of 500 mcg 2 times a day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times a day.

Use in old age

For schizophrenia, an initial dose of 500 mcg 2 times a day is recommended for elderly patients. If necessary, the dose can be increased to 1-2 mg 2 times a day.

Zalasta Ku-tab
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DOSAGE FORMS
lozenges 10 mg

MANUFACTURERS
Krka Polska Sp.zo.o (Poland)

GROUP
Neuroleptics - dibenzodiazepine derivatives

COMPOUND
The active substance is olanzapine.

INTERNATIONAL NON-PROPENTED NAME
Olanzapine

SYNONYMS
Zalasta, Zyprexa, Zyprexa Zidis, Olanzapin-Teva, Parnasan, Egolanza

PHARMACHOLOGIC EFFECT
Antipsychotic drug (neuroleptic) with a wide pharmacological spectrum of action. The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical systems; sedative effect - blockade of adrenergic receptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic effect - blockade of dopamine receptors of the hypothalamus. In addition, it affects muscarinic, adrenergic, histamine H1 receptors and some subclasses of serotonin receptors. Reduces productive (delusions, hallucinations) and negative symptoms (hostility, suspicion, emotional and social autism) of psychosis. Rarely causes extrapyramidal disorders. Absorption of the active substance is high and does not depend on food intake. Tmax in blood plasma after oral administration is 5-8 hours. Metabolized in the liver, no active metabolites are formed, the main circulating metabolite is a glucuronide, does not penetrate the BBB. It is excreted mainly by the kidneys (60%) in the form of metabolites. Smoking, gender and age affect half-life and plasma clearance. In persons over 65 years of age - 51.8 hours and plasma clearance - 17.5 l/h, in persons under 65 years of age - 33.8 hours and plasma clearance - 18.2 l/h.

INDICATIONS FOR USE
For the treatment of schizophrenia (the drug effectively supports the improvement of clinical symptoms with long-term treatment in patients with an initial positive reaction to the drug); for the treatment of moderate or severe episodes of mania; for the prevention of relapses of mania in bipolar disorder (in patients with manic episodes with a good effect of therapy).

CONTRAINDICATIONS
Angle-closure glaucoma; children under 18 years of age (efficacy and safety have not been established); lactation period; galactose intolerance, lapp lactase deficiency or glucose-galactose malabsorption; hypersensitivity to olanzapine or other components of the drug. With caution: renal failure, liver failure, prostatic hyperplasia, paralytic ileus, epilepsy, history of convulsive syndrome, leukopenia and/or neutropenia of various origins, myelosuppression of various origins, incl. myeloproliferative diseases, hypereosinophilic syndrome, cardiovascular and cerebrovascular diseases or other conditions predisposing to hypotension, congenital prolongation of the QT interval on the ECG (increased QTc on the ECG), or in the presence of conditions that can potentially cause prolongation of the QT interval (for example, concomitant use of drugs prolonging the QT interval, congestive heart failure, hypokalemia, hypomagnesemia), old age, as well as concomitant use of other centrally acting drugs; immobilization, pregnancy.

SIDE EFFECT
From the central nervous system and peripheral nervous system: very often - drowsiness; often - dizziness, akathisia, parkinsonism, dyskinesia; rarely - convulsive syndrome (usually against the background of a history of convulsive syndrome); very rarely - neuroleptic malignant syndrome, dystonia (including oculogyric crisis) and tardive dyskinesia. When olanzapine is abruptly discontinued, symptoms such as sweating, insomnia, tremor, anxiety, nausea or vomiting are very rarely observed. From the cardiovascular system: often - arterial hypotension (including orthostatic); infrequently - bradycardia with or without collapse; very rarely - increased QTc interval on ECG, ventricular tachycardia/fibrillation and sudden death, thromboembolism (including embolism pulmonary arteries and deep vein thrombosis). From the digestive system: often - transient anticholinergic effects, incl. constipation and dry mouth, transient, asymptomatic increase in the level of liver transaminases (ALT, AST), especially at the beginning of treatment; rarely - hepatitis (including hepatocellular, cholestatic or mixed liver damage); very rarely - pancreatitis, increased levels of alkaline phosphatase and total bilirubin. Metabolism: very often - weight gain; often - increased appetite; very rarely - hyperglycemia and/or decompensation of diabetes mellitus, sometimes manifested by ketoacidosis or coma, including fatal outcome; hypertriglyceridemia, hypercholesterolemia, hypothermia. From the hematopoietic organs: often - eosinophilia; rarely - leukopenia; very rarely - thrombocytopenia, neutropenia. From the musculoskeletal system: very rarely - rhabdomyolysis. From the outside genitourinary system: very rarely - urinary retention, priapism. From the skin and subcutaneous tissue: rarely - photosensitivity reactions. Allergic reactions: rarely - skin rash; very rarely - anaphylactoid reactions, angioedema, itchy skin or hives. Other: often - asthenia, peripheral edema; very rarely - alopecia. Laboratory indicators: very often - hyperprolactinemia, but clinical manifestations (for example, gynecomastia, galactorrhea and breast enlargement) are rare. In most patients, prolactin levels spontaneously normalized without discontinuation of therapy. Uncommon: increased levels of creatine phosphokinase (CPK). In older patients with dementia, studies have shown a higher incidence of death and cerebrovascular events (stroke, transient ischemic attacks). Very often, this category of patients experienced gait disturbances and falls. Pneumonia, fever, lethargy, erythema, visual hallucinations, and urinary incontinence were also common. Among patients with drug-induced (while taking dopamine agonists) psychoses associated with Parkinson's disease, worsening of parkinsonian symptoms and the development of hallucinations were often recorded. There is evidence of the development of neutropenia (4.1%) during combination therapy with valproic acid in patients with bipolar mania. Long-term therapy (up to 12 months) to prevent relapses in patients with bipolar disorder was accompanied by an increase in body weight.

INTERACTION
Metabolized by the enzyme CYP1A2, therefore inhibitors or inducers of cytochrome P450 isoenzymes that exhibit specific activity against CYP1A2 may affect the pharmacokinetic parameters of olanzapine. CYP1A2 inducers: The clearance of olanzapine may be increased in patients who smoke or when taking carbamazepine concomitantly, resulting in decreased plasma concentrations. Clinical observation is recommended because some cases require increasing the dose of the drug. CYP1A2 inhibitors: fluvoxamine, a specific CYP1A2 inhibitor, significantly reduces clearance. The average increase in maximum concentration after taking fluvoxamine in non-smoking women was 54%, and in smoking men - 77%. The average increase in AUC in these patient categories was 52% and 108%, respectively. In patients taking fluvoxamine or any other CYP1A2 inhibitor (eg, ciprofloxacin), it is recommended that olanzapine therapy be initiated at lower doses. A dose reduction may also be required if CYP1A2 inhibitors are added to therapy. Activated charcoal reduces oral absorption by 50-60% and should be taken at least 2 hours before or after dosing. Fluoxetine (a CYP450 inhibitor), single doses of magnesium or aluminum-containing antacids, or cimetidine do not affect the pharmacokinetics of olanzapine. May weaken the effect of direct and indirect dopamine agonists. In vitro, olanzapine does not inhibit major CYP450 isoenzymes (eg, 1A2, 2D6, 2C9, 2C19, 3A4). In vivo, no inhibition of the metabolism of the following active substances was found: tricyclic antidepressants (CYP2D6), warfarin (CYP2C9), theophylline (CYP1A2) and diazepam (CYP3A4 and 2C19). No interaction was detected when used simultaneously with lithium or biperiden. Therapeutic monitoring of plasma valproic acid levels showed that no changes in valproic acid doses are required when administered concomitantly with olanzapine. Caution should be exercised when using other centrally acting drugs simultaneously. Although a single dose of alcohol (45 mg/70 kg) does not have a pharmacokinetic effect, taking alcohol with olanzapine may be accompanied by an increased depressive effect on the central nervous system.

METHOD OF APPLICATION AND DOSAGE
The drug is prescribed orally, 1 time per day. For schizophrenia, the recommended initial dose of the drug is 10 mg per day. For episodes of mania, the initial dose is 15 mg in 1 dose with monotherapy or 10 mg as part of combination therapy. To prevent relapses in bipolar disorder, the recommended initial dose of the drug in remission is 10 mg per day. The daily dose of the drug for the treatment of schizophrenia, a manic episode or the prevention of relapses of bipolar disorder can be 5-20 mg, depending on the clinical condition of the patient.

OVERDOSE
Symptoms: very common in 10% are: tachycardia, agitation/aggression, dysarthria, various extrapyramidal symptoms, decreased level of consciousness from lethargy to coma; in less than 2% of cases the following occur: delirium, convulsions, coma, neuroleptic malignant syndrome, respiratory depression, aspiration, increased or decreased blood pressure, cardiac arrhythmias; in very rare cases - cardiopulmonary failure. The minimum dose for an acute overdose with a fatal outcome is 450 mg; the maximum dose for an overdose with a favorable outcome (survival) is 1500 mg. Treatment: There is no specific antidote. It is not recommended to induce vomiting. It is necessary to perform gastric lavage, take activated carbon(reduces the bioavailability of olanzapine by 60%), symptomatic treatment under the control of vital functions, including treatment of arterial hypotension and vascular collapse, maintaining respiratory function. The use of epinephrine, dopamine or other sympathomimetics with beta-adrenomimetic activity is not recommended, because the latter can aggravate arterial hypotension. To identify possible arrhythmias, monitoring of cardiovascular activity is necessary. The patient should be under continuous medical supervision until complete recovery.

SPECIAL INSTRUCTIONS
There are very rare reports of the development of hyperglycemia and/or decompensation of diabetes mellitus, sometimes accompanied by the development of ketoacidosis or ketoacidotic coma, incl. there are reports of several fatal cases. In some cases, there was an increase in body weight preceding decompensation, which could become a predisposing factor. In patients with diabetes mellitus and risk factors for the development of this disease, regular clinical monitoring and monitoring of blood glucose levels is recommended. If lipid levels change, therapy adjustments are required. If you abruptly stop taking the drug, very rarely (less than 0.01%) the following symptoms may develop: sweating, insomnia, tremor, anxiety, nausea or vomiting. When discontinuing the drug, a gradual dose reduction is recommended. Since clinical experience with the use of the drug in people with concomitant diseases is limited, the drug should be prescribed with caution to patients with prostatic hyperplasia and paralytic ileus. Experience with the use of olanzapine in patients with psychosis in Parkinson's disease caused by taking dopaminomimetics. Not recommended for the treatment of psychosis in Parkinson's disease caused by dopaminomimetics. Symptoms of parkinsonism and hallucinations increase. At the same time, the effectiveness of treating psychosis was not superior to placebo. Not indicated for the treatment of psychosis and/or behavioral disorders in dementia, due to increased mortality and increased risk of cerebrovascular disorders (stroke, transient ischemic attacks). The increase in mortality is independent of dose or duration of therapy. Risk factors predisposing to increased mortality include: age over 65 years, dysphagia, sedation, malnutrition and dehydration, lung diseases (for example, pneumonia, including aspiration), concomitant use of benzodiazepines. However, the increased incidence of death in the olanzapine groups compared with placebo was independent of these risk factors. With antipsychotic therapy, improvement in the patient's clinical condition occurs within a period of several days to several weeks. During this period, the patient needs careful monitoring. At the beginning of therapy, an asymptomatic increase in liver transaminases (ALT and AST) is possible. In patients with initially elevated AST and/or ALT levels, liver failure, and conditions potentially limiting functionality liver, as well as those taking hepatotoxic drugs medications, caution should be exercised when prescribing the drug. If ALT and/or AST increase during drug therapy, medical monitoring of the patient and, possibly, a reduction in the dose of the drug are recommended. When diagnosing hepatitis (including hepatocellular, cholestatic or mixed), the drug must be discontinued. The drug should be used with caution in patients with leukopenia and/or neutropenia of any origin, myelosuppression of drug origin, as well as during radiation or chemotherapy, due to concomitant diseases, in patients with hypereosinophilic conditions or myeloproliferative diseases. Neutropenia has often been observed with concomitant use of olanzapine and valproic acid. NMS is a potentially life-threatening condition associated with treatment with antipsychotic drugs (neuroleptics), incl. olanzapine. Clinical manifestations NMS: fever, muscle rigidity, impaired consciousness, autonomic disorders (unstable pulse or labile blood pressure, tachycardia, increased sweating, arrhythmias). Additional symptoms of NMS: increased CPK, myoglobinuria (against the background of rhabdomyolysis) and acute renal failure. With the development of symptoms of NMS, as well as an increase in body temperature without visible reasons, it is necessary to cancel all antipsychotics, incl. olanzapine. It should be used with caution in patients with a history of seizures or the presence of factors that lower the seizure threshold. Seizures were rarely reported while taking olanzapine. Therapy was accompanied by a significantly lower incidence of tardive dyskinesia compared with haloperidol. The risk of developing tardive dyskinesia increases with increasing duration of treatment. If signs of this condition occur in a patient taking olanzapine, the drug should be discontinued or the dose reduced. Symptoms of dyskinesia may temporarily increase after discontinuation of the drug. Caution should be exercised when using other centrally acting drugs and alcohol simultaneously. Postural hypotension is uncommon in older adults. In patients over 65 years of age, it is recommended to periodically monitor blood pressure. Caution should be used in patients with an established increase in the QTc interval, especially the elderly, with congenital long QT syndrome, congestive heart failure, myocardial hypertrophy, hypokalemia and hypomagnesemia. When taking the drug, very rarely (less than 0.01%) cases of venous thromboembolism have been reported. A cause-and-effect relationship between therapy and venous thrombosis has not been established. Because patients with schizophrenia often have acquired risk factors for venous thrombosis, all possible other factors (eg, immobilization) should be identified and preventive measures taken. The tablets contain lactose. The drug should not be taken by patients with rare hereditary problems of galactose intolerance, lapp lactase deficiency or glucose-galactose malabsorption. Influence on the ability to drive vehicles and operate machinery. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

STORAGE CONDITIONS
The drug should be stored out of the reach of children, at a temperature not exceeding 30 C.