Instructions for use:
Etaperazine is an antipsychotic drug that acts primarily on the central nervous system.
The dosage form of Etaperazine is film-coated tablets. 1 tablet of the drug contains 4.6 and 10 mg of perphenazine.
The drug is an antipsychotic - an antipsychotic agent that has antiallergic, sedative, muscle relaxant, antiemetic, weak anticholinergic, hypotensive, antiemetic and hypothermic effects. The effectiveness of Etaperazine is due to the blockade of D2 receptors in the mesocortical and mesolimbic systems.
According to the instructions, Etaperazine has an inhibitory (sedative) effect on the nervous system due to the blockade of adrenergic receptors in the reticular formation of the brain stem, without causing a hypnotic effect (in usual dosages).
The antiemetic effect of the drug is due to the blockade of dopamine receptors in the trigger zone of the vomiting center. The hypothermic effect of Etaperazine is achieved due to the blockade of D2 receptors in the hypothalamus.
Reviews of Etaperazine contain information about a wider spectrum of action of the drug compared to chlorpromazine: Etaperazine is more active this tool, however, is inferior to it in adrenolytic and hypothermic effects, as well as in its ability to enhance the effects of narcotic and pharmaceutical drugs.
The pronounced antipsychotic effect of the drug develops 3-7 days after the start of its use and reaches its maximum after 2-6 months of continuous use.
According to the instructions, Etaperazine is used to treat mental illness(such as exogenous-organic and senile psychoses with hallucinatory phenomena, schizophrenia, psychopathy, itchy skin, hiccups). Judging by the reviews of Etaperazine, the drug is successfully used for uncontrollable vomiting in pregnant women.
In some cases, the drug may cause extrapyramidal disorders (tremor, loss of coordination of movements, decrease in their volume), drowsiness, blurred vision, akathisia, autonomic disorders, lethargy, depression, inhibition of consciousness, decreased motivational activity. From the outside cardiovascular system possible reduction blood pressure, violations heart rate, tachycardia, pronounced changes on the ECG. From the gastrointestinal tract, according to reviews of Etaperazine, side effects such as atony are noted bladder and intestines, abdominal pain, loss of appetite, nausea, vomiting.
Allergic reactions to the drug include contact dermatitis, skin rash, photosensitivity, angioedema.
Side effects of Etaperazine associated with the anticholinergic effect of the drug: accommodation disturbances, dry mouth, difficulty urinating, constipation.
The use of Etaperazine is prohibited for endocarditis, a disease associated with inflammation of the internal cavities of the heart, severe cardiovascular diseases(arterial hypotension, decompensated chronic heart failure), progressive diseases of the spinal cord and brain, severe depression of central function nervous system, comatose states of any origin.
The drug is taken orally, after meals.
At psychotic disorders In patients who have not previously used antipsychotic drugs, the dosage of Etaperazine according to the instructions is 4-16 mg of the drug 2-4 times a day. The presence of a chronic disease causes an increase in dosage to 64 mg/day. Duration of treatment in in this case ranges from 1-4 months.
In case of an overdose of Etaperazine, the appearance of neuroleptic reactions is observed, for example, an increase in body temperature. In severe cases, impairment of consciousness may occur in various forms, including coma. Treatment of drug overdose is carried out using intravenous administration of a solution of dextrose, diazepam, nootropic medicines, vitamins C and B, as well as symptomatic therapy.
As indicated in the instructions for Etaperazine, if intestinal obstruction and a brain tumor are suspected, the use of the drug is not advisable - since vomiting can mask the symptoms of poisoning and complicate diagnosis.
During treatment with Etaperazine, it is recommended to regularly monitor liver and kidney function, prothrombin index, peripheral blood, and also exercise caution when driving vehicles and engaging in activities that require quick reaction and increased concentration.
Reviews of Etaperazine mention the need to avoid skin contact with the liquid form of the drug - in order to prevent possible appearance contact dermatitis.
The drug is stored at a temperature not exceeding 20 degrees Celsius in a dark place out of reach of children. The shelf life of Etaperazine, subject to these conditions, is 3 years. The use of the medicinal product beyond the specified expiration date is prohibited.
Perphenazine
10 pcs. - contour cell packaging (5) - cardboard packs.
1200 pcs. - plastic bags (2) - cardboard boxes.
Antipsychotic drug(neuroleptic), piperazine derivative of phenothiazine. It is believed that the antipsychotic effect of phenothiazines is due to the blockade of postsynaptic dopamine receptors in the mesolimbic structures of the brain. Perphenazine has strong effect, central mechanism which is associated with inhibition or blockade of dopamine D 2 receptors in the chemoreceptor trigger zone of the cerebellum, and peripheral - with blockade of the vagus nerve in the gastrointestinal tract. Has alpha-adrenergic blocking activity. Anticholinergic activity and sedative effect may be mild to moderate in intensity, hypotensive effect weakly expressed. Has a pronounced extrapyramidal effect. The antiemetic effect may be enhanced by anticholinergic and sedative properties. Has a muscle-relaxing effect.
Clinical data on the pharmacokinetics of perphenazine are limited.
Phenothiazines are highly protein bound. They are excreted mainly by the kidneys and partly with bile.
Treatment of psychotic disorders, especially hyperactivity and agitation, schizophrenia; neuroses accompanied by fear and tension. Treatment of nausea and of various etiologies. Skin itching.
Cirrhosis, hepatitis, hemolytic jaundice, nephritis, hematopoietic disorders, myxedema, progressive systemic diseases head and spinal cord, decompensated heart disease, thromboembolic diseases, late stages of bronchiectasis, pregnancy, lactation, hypersensitivity to perphenazine.
For adults and children over 12 years of age, when taken orally, the daily dose is 4-80 mg. In the chronic course of the disease and in resistant cases, the daily dose can be increased to 150-400 mg. The frequency of administration and duration of treatment are determined individually.
Adults and children over 12 years old with intramuscular injection single dose is 5-10 mg. For intravenous administration, a single dose is 1 mg.
Maximum doses: adults and children over 12 years of age with intramuscular administration - 15-30 mg/day, with intravenous administration - 5 mg/day.
From the side of the central nervous system: drowsiness, akathisia, blurred vision, dystonic extrapyramidal reactions, parkinsonian extrapyramidal reactions.
From the liver: rarely - cholestatic jaundice.
From the hematopoietic system: rarely - agranulocytosis.
From the side of metabolism: rarely - melanosis.
Allergic reactions: rarely - skin rash accompanied by contact dermatitis.
Dermatological reactions: rarely - photosensitivity.
Effects due to anticholinergic action: possible dry mouth, accommodation disturbances, constipation, difficulty urinating.
When used simultaneously with drugs that have a depressant effect on the central nervous system, with ethanol and ethanol-containing drugs, increased depression of the central nervous system and respiratory function is possible.
When used simultaneously with anticonvulsants, the threshold may be lowered convulsive readiness; with drugs for the treatment of hyperthyroidism, the risk of developing agranulocytosis increases.
When used simultaneously with drugs that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal disorders is possible.
When used simultaneously with drugs that cause arterial hypotension, severe orthostatic hypotension is possible.
When used simultaneously with drugs that have anticholinergic effects, their anticholinergic effects may be enhanced, while the antipsychotic effect of the antipsychotic may decrease.
When used simultaneously with tricyclic antidepressants, maprotiline, and MAO inhibitors, the risk of developing NMS increases.
With the simultaneous use of antiparkinsonian drugs and lithium salts, the absorption of phenothiazines is impaired.
With simultaneous use, it is possible to reduce the effect of amphetamines, levodopa, clonidine, guanethidine, epinephrine.
When used simultaneously, extrapyramidal symptoms and dystonia may develop.
With simultaneous use, the vasoconstrictor effect of ephedrine may be weakened.
Perphenazine should be used with caution when hypersensitivity to other phenothiazine drugs.
Phenothiazines are used with extreme caution in patients with pathological changes in the blood picture, liver dysfunction, alcohol intoxication, Reye's syndrome, as well as for cardiovascular diseases, predisposition to the development of glaucoma, Parkinson's disease, gastric ulcer and duodenum, urinary retention, chronic respiratory diseases (especially in children), epileptic seizures, vomiting; in elderly patients (increased risk of excessive sedation and hypotensive effects), in depleted and weakened patients.
The development of tardive dyskinesia during the use of perphenazine is more likely in elderly patients, women and those with brain damage. Parkinsonian extrapyramidal reactions are more often observed in elderly patients, dystonic extrapyramidal reactions - in younger people. Symptoms of these disorders may occur in the first few days of treatment or after long-term therapy and may recur even after a single dose.
In case of hyperthermia, which is one of the elements of NMS, perphenazine should be discontinued immediately.
The simultaneous use of phenothiazines with absorbent antidiarrheals should be avoided.
During the treatment period, avoid drinking alcohol.
Impact on the ability to drive vehicles and operate machinery
It should be used with caution in patients engaged in potentially hazardous activities that require a high speed of psychomotor reactions.
Perphenazine is contraindicated for use during pregnancy and lactation.
Preparation Etaperazine- an antipsychotic drug, a neuroleptic that has antiallergic, sedative, muscle relaxant, antiemetic, weak anticholinergic, hypotensive, antiemetic and hypothermic effects. The effectiveness of Etaperazine is based on the ability of the drug to block D2 receptors of the mesolimbic and mesocortical systems. According to the instructions, Etaperazine has an inhibitory (sedative) effect on the nervous system, blocking adrenergic receptors of the reticular formation of the brain stem. When using the drug in normal dosages, it does not appear hypnotic effect. The drug has an antiemetic effect due to the blockade of dopamine receptors in the trigger zone of the vomiting center. The hypothermic effect of Etaperazine is due to the blockade of D2 receptors in the hypothalamus. Reviews of Etaperazine indicate that the drug has a wider spectrum of action compared to chlorpromazine, since Etaperazine exhibits greater activity, but is inferior to chlorpromazine in hypothermic and adrenolytic effects. In addition, Etaperazine, to a lesser extent than chlorpromazine, enhances the effects of drugs and drugs. The pronounced antipsychotic effect of the medication appears after three to seven days from the start of administration, maximum effect observed after two to six months, subject to continuous use of the drug.
| Name: | ETAPERAZINE |
| ATX code: | N05AB03 - |
Latin name: etaperazine
ATX code: N05AB03
Active ingredient: perphenazine
Manufacturer: Tatchimpharmpreparaty, Russia
Release from the pharmacy: By prescription
Storage conditions: up to 25 degrees Celsius
Best before date: 3 years.
Etaperazine is used for a variety of mental disorders.
Taking the drug is indicated in the following cases:
Description of composition: active ingredients perphenazine. Auxiliary components: potato starch, talc, titanium dioxide.
Pills white, covered with a shell. One package contains 50 pieces of ethapazine, 4 mg each.
The average cost in Russia is 340 rubles per package.
The drug etaprazine belongs to the neuroleptics from the group of phenothiazines. The drug has an antiemetic and sedative effect. The medication has a significant effect on the central nervous system. It is an antipsychotic that has a wide range of uses. The main effects are antipsychotic, antiemetic, cataleptogenic, alpha-adrenolytic. You can also note the occurrence of a weak hypotensive and muscle relaxant effect. It is also noteworthy that the sedative effect is simultaneously combined with an exciting one.
A selective effect on deficiency symptoms is also noted. In some cases, pronounced extrapyramidal disorders develop. The drug is well absorbed from the gastrointestinal tract. In some cases, marked fluctuations in maximum plasma concentrations are observed. Pronounced binding to plasma proteins is also observed. The medication is broken down well and mainly in the liver. It is excreted along with bile and urine.
The instructions for use of etaprazine indicate that the initial dosage is 12 mg as recommended by a doctor. In some cases you can increase daily dosage up to 60 mg, and in severe situations up to 120 - 180 mg. One or half a tablet is usually prescribed as antiemetic drug as medicinal dose before surgical procedures or in obstetric and medical practice. The medication should be used 3-4 times a day.
During pregnancy and breastfeeding
Pregnant and nursing mothers should not prescribe this drug, only in extreme situations with severe vomiting.
The drug should not be prescribed for progressive systemic diseases of the spinal cord and brain, liver cirrhosis, hemolytic jaundice, for problems with hematopoiesis, thromboembolism, pregnancy and breastfeeding. Also, you should not use the drug for hepatitis, nephritis, myxedema, heart disease, hypersensitivity or individual intolerance to the active substance, and also not late stages bronchiectasis.
Cross drug interactions
The drug has a depressant effect on the central nervous system and respiratory functions, if combined with alcoholic drinks. If combined with drugs that potentiate extrapyramidal disorders, they intensify, including fluoxetine. Drugs for the correction of thyroid hormones cause agranulocytosis, and anticonvulsants increase the threshold for the onset of convulsive reactions. When used together, antihypertensive drugs significantly potentiate the onset of hypotensive manifestations.
Anticholinergic drugs reduce the effectiveness in terms of antipsychotic properties. If a patient simultaneously takes tricyclic antidepressants and MAO inhibitors, then the risk of side effects increases many times. Medicines to treat Parkinson's reduce the absorption of phenothiazines. Levodopa, amphetamines, guanethidine, clonidine and epinephrine reduce the effectiveness of the drug when used simultaneously. The medicine reduces the vasoconstrictor effect of ephedrine.
Side effects
Etaperazine instructions indicate that in most cases extrapyramidal disorders develop in adults, vascular reactions and allergic manifestations. Elderly patients do not have specific
Overdose
Accommodation may be impaired if you start to overdo it with the recommended dosages. In large dosages, acute neuroleptic syndrome also often develops. This is usually accompanied by a marked increase in body temperature, and in the most severe situations, loss of consciousness and coma are observed. At the slightest suspicion of overdose, you should immediately stop using the medicine. Diazepam is administered intravenously, nootropic drugs, dextrose, ascorbic acid and vitamins C. Symptomatic therapy is also carried out.
JSC Dalkhimpharm, Russia
Average cost– 30 rubles per package.
Triftazine consists of an active working component - trifluoperazine. This drug used to treat schizophrenia, hallucinations, shock states, nausea, vomiting, psychosis and delirium. The drug has a large list of contraindications and side effects, so it is recommended to prescribe it carefully and in really severe cases. Available in tablet and injection form.
Pros:
Cons:
KRKA, Slovenia
Average cost in Russia – 340 rubles per package.
Moditene is a drug for the treatment of various neuroses, schizophrenic disorders, paranoid states, aggressiveness, manic disorder, fear, nervous tension, psychosis, depressive-hypochondriacal syndrome. Available as an injection oil solution 25 mg in 1 ml ampoule. One package contains 5 ampoules. The drug has a moderate list of contraindications and side effects.
Pros:
Cons:
1 film-coated tablet contains:
Perphenazine dihydrochloride
(Etaperazine) ...................................
- 4.0 mg ................... - 6.0 mg ................ - 10.0 mglactose monohydrate...................- 86.0 mg ............. - 111.0 mg ............. - 125.0 mg
potato starch...............- 9.0 mg ........ - 11.70 mg ............. - 13.50 mg
calcium stearate........................- 1.0 mg...................- 1.30 mg............. - 1.50 mg
Shell excipients:
sucrose .................................... - 61.702 mg ............. - 67.872 mg ............. - 92.553 mg
magnesium hydroxycarbonate......- 34.169 mg ............. - 37.586 mg ............. - 51.254 mg
povidone...................................- 0.669 mg............- 0.736 mg................- 1.004 mg
silicon dioxide
colloid............................. - 2.228 mg................. - 2.451 mg................ - 3.342 mg
tropeolin O ........................... - 0.011 mg................. - ........................... -
titanium dioxide ..................... - 1.073 mg...................- 1.192 mg............... - 1.485 mg
beeswax ...................... - 0.148 mg...................- 0.163 mg............... - 0.220 mg
Description:Film-coated tablets, round, biconvex, dosage 4 mg - from light yellow to yellow, 6 mg - white, 10 mg - yellowish-green to green. On the break of the tablets two layers are visible: with a dosage of 4 mg - a white or white core with a grayish tint and a light yellow to yellow shell, 6 mg - a white or white core with a grayish tint and a white shell, 10 mg - a white core or white with a grayish tint and the shell is yellowish-green to green.
Pharmacotherapeutic group:Antipsychotic (neuroleptic). ATX:N.05.A.B.03 Perphenazine
Pharmacodynamics:Antipsychotic (neuroleptic), phenothiazine derivative; has a sedative effect. antiallergic, weak anticholinergic, antiemetic, muscle relaxant. weak hypotensive and hypothermic effect, eliminates hiccups. Antipsychotic effect caused by blockade of dopamine D2 receptors of the mesolimbic and mesocortical systems. Blockade of D2-dopamine receptors in polyneuronal synapses of the brain causes relief of the productive symptoms of psychosis: delusions and hallucinations. The antipsychotic effect is combined with a pronounced activating effect and a selective effect on syndromes occurring with lethargy, lethargy, apathy, primarily with substuporous phenomena, as well as on apatoabulic states. The sedative effect is due to the blockade of adrenergic receptors in the reticular formation of the brain stem. The severity of the sedative effect is from weak to moderate. Has a strong antiemetic effect. Antiemetic activity is associated with inhibition of the trigger zone of the vomiting center due to blockade of D2-dopamine receptors ( central action) and a decrease in secretion and motility of the gastrointestinal tract (GIT) as a result of blockade of m-cholinergic receptors ( peripheral action). Inhibition of dopamine receptors in the nigrostriatal zone and tubuloinfundibular region can cause extrapyramidal disorders and hyperprolactinemia. The peripheral alpha-adrenergic blocking effect is manifested by a decrease in blood pressure (the hypotensive effect is weakly expressed), and the H1-antihistamine has an antiallergic effect. Hypothermic effect - blockade of dopamine receptors of the hypothalamus. It is superior in antipsychotic activity. The antipsychotic effect develops after 4-7 days and reaches a maximum after 1.5-6 months (depending on the nature of the disease).
Pharmacokinetics:Like all phenothiazine derivatives, it is well absorbed into gastrointestinal tract. Plasma protein binding - 90%. Bioavailability is 40% after oral administration. intensively metabolized in the liver by sulfoxylation, hydroxylation, dealkylation and glucuronidation to form a number of metabolites. Significant variations in maximum plasma concentrations have been observed among patients taking phenothiazine derivatives. Hydroxylation of perphenazine is carried out with the participation of the CYP 2 D 6 isoenzyme of the cytochrome P450 enzyme system and, therefore, depends on genetic polymorphism, that is, from 7% to 10% of the population of the Caucasus and a small percentage of the population of Asia have low activity or its complete absence, the so-called “low” metabolism. Patients who are "low" CYP2D6 metabolizers will metabolize perphenazine more slowly and have higher plasma concentrations of etaperazine compared to patients who are normal or "high" metabolizers.
After ingestion of perphenazine, its maximum concentration in plasma, according to studies, is observed after 1-3 hours, 7-hydroxyperphenazine - 2-4 hours. Equilibrium averages maximum concentrations(Cmax) are 984 pg/ml and 509 pg/ml, respectively. The time to reach equilibrium concentration (Css) when taken orally is 72 hours.
It is excreted mainly by the kidneys and partly with bile. The half-life of perphenazine does not depend on the dose and is 9-12 hours, 7-hydroxyperphenazine 10-19 hours.
Indications:- Schizophrenia in adults.
- Severe nausea and vomiting in adults.
Contraindications:- severe toxic depression of the central nervous system (CNS) function and comatose states any etiology;
- patients taking high doses of drugs that depress the central nervous system (barbiturates, alcohol, anesthetics, analgesics, antihistamines);
- inhibition of bone marrow hematopoiesis;
- hematopoietic disorders;
- severe renal or liver failure;
- decompensated hypothyroidism;
- subcortical brain damage with or without dysfunction of the hypothalamus;
- progressive systemic diseases of the brain and spinal cord;
- late stages of bronchiectasis;
- diseases accompanied by a risk of thromboembolic complications;
- hypersensitivity to the components of the drug;
- cardiovascular diseases in the stage of decompensation;
- violation of intracardiac conduction;
- deficiency of lactase, sucrase/isomaltase;
- intolerance to lactose, sucrose;
- glucose-galactose malabsorption.
With caution:Alcoholism (predisposition to hepatotoxic reactions); pathological changes blood; breast cancer (as a result of the secretion of prolactin induced by phenothiazine derivatives, the potential risk of disease progression and resistance to drugs prescribed to patients with endocrine diseases and metabolic diseases and cytostatic drugs); angle-closure glaucoma; prostatic hyperplasia with clinical manifestations; mild to moderate renal or liver failure; peptic ulcer stomach and duodenum (during exacerbation); diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease (extrapyramidal effects increase); epilepsy; chronic diseases accompanied by breathing problems (especially in children); Reye's syndrome (increased risk of hepatotoxicity in children and adolescents); cachexia; vomiting (the antiemetic effect of phenothiazine derivatives may mask vomiting associated with overdose of other drugs); patients during alcohol withdrawal; depression (possibility of suicide remains); old age.
Pregnancy and lactation:Perphenazine easily crosses the placental barrier and is quickly excreted in breast milk, so the possibility of using the drug is determined by the doctor if the potential benefit to the mother outweighs the potential risk to the fetus or child.
Newborns whose mothers took it late in pregnancy or during labor may show signs of toxicity such as lethargy, tremors, and excessive excitability. In addition, these newborns have a low Apgar score.
With prolonged treatment of the mother, or when using high doses, as well as in the case of prescribing the drug shortly before birth, monitoring the activity of the nervous system of the newborn is justified.
Directions for use and dosage:Inside, after eating. Elderly patients may take it before bedtime.
Doses are selected individually according to the severity of the condition.
Elderly, malnourished and debilitated patients usually require a lower initial dose.
When the maximum therapeutic effect is achieved, the dose is gradually reduced to maintenance.
Schizophrenia: For adults not previously treated with antipsychotic drugs, the initial dose is 4-8 mg 3 times a day. Patients with chronic course diseases, if necessary, the dose is increased to 64 mg/day. The duration of treatment depends on the patient’s condition and the severity of side effects and ranges from 1-4 months or more.
Severe nausea and vomiting:
adults are prescribed 8-16 mg 2-4 times a day as an antiemetic drug. Side effects:Not all of the following side effects have been reported with perphenazine. However, pharmacological similarities with other phenothiazine derivatives require that each be taken into account. Many of these side effects can be avoided by reducing the dose.
From the nervous system and sensory organs:
extrapyramidal disorders (especially dystonic) - spasm of the muscles of the back and neck, face, tongue, tonic spasm of the masticatory muscles, difficulty speaking and swallowing, a feeling of stiffness in the throat, oculogyric crises, spasm and pain in the limbs, stiffness of the arms and legs, hyperreflexia, akathisia . parkinsonism, ataxia; drowsiness, lethargy, lethargy, muscle weakness, decreased motivation, dizziness, miosis, mydriasis, blurred vision, glaucoma, pigmentary retinopathy, deposits in the lens and cornea, paradoxical reactions - exacerbation of psychotic symptoms, catalepsy, catatonic-like states, paranoid reactions, lethargy, lethargy , paradoxical arousal, anxiety, hyperactivity, nighttime confusion, strange dreams, sleep disturbance. Their frequency and severity usually increase with increasing dose, but there are significant individual differences in a tendency to develop such symptoms. Extrapyramidal symptoms are usually corrected by the simultaneous use of effective antiparkinsonian drugs or dose reduction. In some cases, however, these extrapyramidal reactions may persist after perphenazine treatment is discontinued.Tardive dyskinesia: rhythmic, involuntary movements of the tongue, face, mouth, and jaw (eg, tongue thrusting, cheek puffing, mouth pucker, chewing movements). Sometimes this may be accompanied involuntary movements limbs. Doesn't exist effective remedy for the treatment of tardive dyskinesia. There is evidence that worm-like movements of the tongue may be an early sign of the syndrome and if treatment is stopped, this syndrome may not develop.
From the cardiovascular system: increase and decrease in blood pressure. orthostatic hypotension, changes in heart rate, tachycardia (especially with an unexpected significant increase in dose), bradycardia, cardiac arrest, weakness and dizziness, arrhythmia, fainting, changes in the electrocardiogram, nonspecific (quinidine-like effect).
Blood disorders (hematopoiesis, hemostasis): leukopenia, agranulocytosis, eosinophilia, hemolytic anemia, thrombopenic purpura, pancytopenia.
From the gastrointestinal tract: nausea, vomiting, diarrhea, constipation, anorexia, increased appetite and body weight, polyphagia, abdominal pain, dry mouth, increased salivation, liver damage (bile stasis), cholestatic hepatitis, jaundice.
Allergic reactions: skin rash, urticaria, erythema, eczema, exfoliative dermatitis, itching. hyperhidrosis, skin photosensitivity, bronchial asthma, fever, anaphylactoid reactions, laryngeal edema and Quincke's edema, angioedema.
Other: pallor, perspiration, intestinal and bladder atony, urinary retention. frequent urination or urinary incontinence, polyuria, nasal obstruction, kidney damage, increased intraocular pressure, skin pigmentation, photophobia, unusual secretion of breast milk, breast enlargement and galactorrhea in women, gynecomastia in men, menstrual irregularities, amenorrhea, changes in libido, decreased ejaculation, syndrome of inappropriate secretion of antidiuretic hormone, false-positive pregnancy test, hyperglycemia, hypoglycemia, glucosuria. peripheral edema, systemic lupus erythematosus syndrome.
Neuroleptic malignant syndrome: hyperthermia, muscle rigidity, change mental status, autonomic instability (irregular pulse and blood pressure fluctuations, tachycardia, sweating and cardiac arrhythmia). Overdose:In case of an overdose of the drug, acute neuroleptic reactions may occur. An increase in body temperature, which may be one of the symptoms of neuroleptic malignant syndrome, should be especially alarming. In severe cases, overdose may occur various shapes disturbances of consciousness, up to coma. Exceeding therapeutic dosages of perphenazine may be accompanied by extrapyramidal reactions, changes in the electrocardiogram - prolongation of the QTc interval, expansion of the QRS complex.
Help: stopping therapy with antipsychotics, prescribing correctors, intravenous administration diazepam, glucose solution, symptomatic therapy. Interaction:When using Etaperazine simultaneously with other drugs, it is possible:
-
with drugs that have a depressant effect on the central nervous system (anesthetics, narcotic analgesics, and drugs containing it, barbiturates, tranquilizers, etc.) increased depression of the central nervous system, as well as respiratory depression;-
with tricyclic antidepressants, maprotiline or monoamine oxidase inhibitors - the sedative and anticholinergic effects may be prolonged and intensified, and the risk of developing neuroleptic malignant syndrome may increase.- with anticonvulsants - it is possible to lower the threshold of convulsive readiness;
- with drugs for the treatment of hyperthyroidism - the risk of developing agranulocytosis increases;
- with other drugs that cause extrapyramidal reactions - an increase in the frequency and severity of extrapyramidal disorders is possible;
- With antihypertensive drugs- severe orthostatic hypotension is possible;
- with ephedrine - the vasoconstrictor effect of ephedrine may be weakened. Concomitant use with tricyclic antidepressants, selective inhibitors serotonin reuptake agents, such as fluoxetine, sertraline and paroxetine. which inhibit the isoenzyme cytochrome P450 2 D 6 (CYP 2 D 6), can sharply increase plasma concentrations of phenothiazine derivatives and other antipsychotic drugs. When prescribing these drugs to patients already receiving antipsychotic therapy, careful monitoring is essential and dose reduction may be necessary to avoid side effects and toxicity. The administration of alpha and beta adrenergic agonists () and sympathomimetics () can lead to a paradoxical decrease in blood pressure. The antiparkinsonian effect of levodopa is reduced due to blocking of dopamine receptors. may suppress the effect of amphetamines, clonidine, guanethidine.
Perphenazine enhances the m-anticholinergic effects of other drugs, while the antipsychotic effect of the antipsychotic may decrease.
When used simultaneously with prochlorperazine, which is related in chemical structure, prolonged loss of consciousness may occur.
When used together with antiparkinsonian drugs and lithium preparations, absorption in the gastrointestinal tract decreases. When used simultaneously with lithium preparations, the rate of excretion of lithium salts by the kidneys increases and the severity of extrapyramidal disorders increases. Early signs intoxication with lithium salts (nausea and vomiting) may be masked by the antiemetic effect of perphenazine.
Aluminum- and magnesium-containing antacid drugs or antidiarrheal adsorbents reduce the absorption of perphenazine.
Perphenazine may increase blood sugar and impair diabetes control. Dose adjustment of antidiabetic drugs is necessary.
Reduces the effect of anorexigenic drugs (with the exception of fenfluramine).
Reduces the effectiveness of the emetic effect of apomorphine, enhances its inhibitory effect on the central nervous system.
Increases plasma concentrations of prolactin and interferes with the action of bromocriptine. Probucol, . cisapride, disopyramide, pimozide, and contribute to an additional prolongation of the Q-T interval, which increases the risk of developing ventricular tachycardia.
When used together with thiazide diuretics, increased hyponatremia. Combination with beta-blockers enhances hypotensive effect, the risk of developing irreversible retinopathy, arrhythmias and tardive dyskinesia increases. Medicines that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.
Special instructions:Elderly patients with dementia-related psychosis treated with antipsychotic drugs have an increased risk of death.
Extrapyramidal disorders occur more often when taking high doses. Tardive dyskinesia occurs more often in older patients, especially women, while dystonia occurs more often in younger people. If signs or symptoms of tardive dyskinesia occur, discontinuation of antipsychotic treatment should be considered (however, some patients may require continued treatment despite the presence of the syndrome).
Perphenazine may lower the seizure threshold, so caution should be exercised when using the drug in patients with a predisposition to seizure disorders and during alcohol withdrawal. With simultaneous treatment with perphenazine and anticonvulsants, an increase in the dose of the latter may be required.
During therapy with perphenazine, alcohol intake should be avoided, because Additive effects and hypotension may occur. The risk of suicide and the risk of antipsychotic overdose may be increased in patients who abuse alcohol during treatment due to the potentiation of the depressive effect of the drug on the central nervous system.
Caution should be exercised when prescribing the drug to patients with depression. The possibility of suicide in such patients remains during treatment, so it is necessary to exclude them from access to a large number medications during treatment until complete remission occurs.
Use with caution in patients with a history of serious side effects while taking other phenothiazines. Some of the adverse reactions of perphenazine occur more often when taking high doses. should be used with great caution by persons exposed to heat or cold, as phenothiazine derivatives suppress the mechanism of temperature regulation and, depending on temperature environment, can lead to hyperthermia and heatstroke or hypothermia and respiratory failure. A significant increase in body temperature can be caused by individual hypersensitivity. If hyperthermia occurs, treatment should be discontinued immediately. increases the body's sensitivity to action sunlight. Recommended to use sunscreens, especially if patients light skin and wear protective clothing while staying outdoors, and also avoid prolonged exposure to the sun, visiting solariums and using ultraviolet lamps.
Should be used with caution in patients suffering from disorders respiratory system in connection with the possible development of acute pulmonary infection, as well as in chronic respiratory diseases such as bronchial asthma or emphysema.
Antipsychotic drugs increase the concentration of prolactin in the blood, which persists with long-term use. Symptoms may include breast enlargement, dysmenorrhea, decreased libido, or nipple discharge.
Caution should be exercised when prescribing the drug to patients receiving or similar drugs, as well as those who have contact with phosphorus-containing insecticides (an additive anticholinergic effect is possible).
During treatment, liver and kidney functions (with long-term therapy), peripheral blood patterns, and prothrombin index should be monitored. If signs or symptoms of blood dyscrasia occur, treatment should be discontinued and appropriate therapy instituted. Treatment should also be stopped if there are abnormalities in liver tests or if the blood urea nitrogen level is abnormal. Most cases of agranulocytosis were observed between 4 and 10 weeks of therapy. During this period, patients should be especially careful to monitor for sore throat or symptoms of infection. If the number of leukocytes decreases significantly, the drug should be discontinued and appropriate therapy should be started.
Jaundice that develops (rarely) during treatment (between 2 and 4 weeks of therapy) is usually considered a hypersensitivity reaction. In this case, the clinical picture is similar to that of infectious hepatitis, but the results of liver function tests are characteristic of obstructive jaundice. It is usually reversible, but cases of chronic jaundice have been reported.
Sudden death has been rarely reported in patients receiving phenothiazines. In some cases, the cause of death was cardiac arrest, in others it was asphyxia due to a deficiency of the cough reflex.
The antiemetic effect may mask symptoms of toxicity caused by overdose of other drugs and make it difficult to diagnose diseases such as intestinal obstruction, Reye's syndrome, brain tumors, or other encephalopathies.
Patients with diabetes mellitus It should be taken into account that the carbohydrate content in one single dose of the drug (1 tablet) corresponds to: dosage 4 mg - 0.012 XE, dosage 6 mg - 0.015 XE. dosage 10 mg - 0.018 XE.
Caution should be exercised when using perphenazine in older adults because they may be more sensitive to the effects of the drug and the development of side effects such as extrapyramidal symptoms and tardive dyskinesia. Neuroleptic malignant syndrome (NMS), the development of which is possible while taking any classical antipsychotic drugs, is a potentially fatal complex of symptoms. Diagnosing patients with this syndrome is difficult. At differential diagnosis it is important to identify cases where the clinical picture includes serious medical diseases(eg, pneumonia, systemic infection, etc.), other extrapyramidal symptoms, central anticholinergic toxicity, heat stroke, drug fever, and primary central nervous system pathologies. Management of NMS should include: 1) immediate discontinuation of antipsychotic medications and other concomitant medications as needed; 2) intense symptomatic therapy and medical control; 3) treatment of any associated serious problems health problems that require specific procedures. There are no generally accepted specific pharmacological treatment regimens.
It is recommended to closely monitor patients who are taking large doses of phenothiazine derivatives and who are undergoing surgical operations and interventions due to possible development hypotensive phenomena.
With long-term therapy with phenothiazine derivatives, one should keep in mind the possibility of damage to the liver, cornea and the development of irreversible tardive dyskinesia. For patients requiring long-term therapy, the minimum dose should be adjusted if possible. the shortest duration of treatment while maintaining clinical
Efficiency. The need for continued treatment should be reassessed periodically.
Immediate discontinuation of perphenazine therapy may lead to the development of withdrawal symptoms (dizziness, nausea, vomiting, stomach upset, tremors), so the dose of the drug should be reduced gradually until complete cessation.
Impact on the ability to drive vehicles. Wed and fur.:During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities, working with machinery, or driving a car, because may weaken mental and/or physical performance, and also cause drowsiness (especially in the first 2 weeks of treatment).
Release form/dosage:Film-coated tablets 4 mg, 6 mg and 10 mg.
10 tablets of 4 mg or 10 mg in a blister pack.
5 blister packs with instructions for use are placed in a cardboard pack.
To form military first aid kits, 6 mg tablets, 1.2 kg each, in plastic film bags. 2 bags of 1.2 kg each in a cardboard box.
Storage conditions:In a place protected from light, at a temperature not exceeding 25 ° C.
Keep out of the reach of children.
Best before date:3 years. Do not use after the expiration date stated on the package.
Conditions for dispensing from pharmacies: By prescription Registration number: P N001399/01 Registration date: 17.06.2008 Owner of the Registration Certificate:TATHIMPHARMPREPARATY, JSC Russia Manufacturer: Information update date: 30.08.2015 Illustrated instructions
