Pharmacy No. 84. Delivery of medicines to your home and office.

Delivery on Sundays and holidays does not work!

Medicines

my basket

Apteka84.kz is an online pharmacy that offers its customers medicines, medicinal and decorative cosmetics, dietary supplements, vitamins, baby food, intimate products for adults, medical equipment and thousands of other medical and cosmetic products at low prices. All data presented on the Apteka84.kz website is for informational purposes only and is not a substitute for professional medical care. Apteka84.kz strongly recommends that you carefully read the instructions for use contained in each package of medicines and other products. If you currently have any symptoms of the disease, you should seek help from a doctor. You should always tell your doctor or pharmacist about all the medicines you take. If you feel you need further help, please consult your local pharmacist or contact our GP online or by telephone.

Paroxetine

Akathisia

Occasionally, treatment with paroxetine or another drug from the group of selective serotonin reuptake inhibitors is accompanied by the occurrence of akathisia, which is manifested by a feeling of internal restlessness and psychomotor agitation, when the patient cannot sit or stand quietly; with akathisia, the patient usually experiences subjective discomfort. The likelihood of akathisia occurring is highest in the first few weeks of treatment.

Serotonin syndrome/neuroleptic malignant syndrome In rare cases, serotonin syndrome or neuroleptic malignant syndrome-like symptoms may occur during treatment with paroxetine, especially if paroxetine is used in combination with other serotonergic drugs and/or antipsychotics. These syndromes are potentially life-threatening and therefore treatment with paroxetine should be discontinued if they occur (they are characterized by groups of symptoms such as hyperthermia, muscle rigidity, myoclonus, autonomic disturbances with possible rapid changes in vital signs, mental status changes including confusion, irritability, extremely severe agitation progressing to delirium and coma), and begin supportive symptomatic therapy. Paroxetine should not be prescribed in combination with serotonin precursors (such as L-tryptophan, oxytriptan) due to the risk of developing serotonergic syndrome.

Mania and bipolar disorder

A major depressive episode may be the initial manifestation of bipolar disorder. It is generally accepted (although not proven in controlled clinical trials) that treating such an episode with an antidepressant alone may increase the likelihood of an accelerated development of a mixed/manic episode in patients at risk for bipolar disorder. Before initiating antidepressant treatment, careful screening should be performed to assess the patient's risk of bipolar disorder; Such screening should include a detailed psychiatric history, including a family history of suicide, bipolar disorder, and depression. Paroxetine is not registered for the treatment of depressive episodes in bipolar disorder. Paroxetine should be used with caution in patients with a history of mania.

Monoamine oxidase inhibitors (MAO)

Treatment with paroxetine should be started cautiously no earlier than 2 weeks after stopping therapy with MAO inhibitors; The dose of paroxetine should be increased gradually until the optimal therapeutic effect is achieved.

Impaired kidney or liver function

Caution is advised when treating patients with severe renal impairment and patients with impaired liver function with paroxetine.

Epilepsy

As with other antidepressants, paroxetine should be used with caution in patients with epilepsy.

Seizures

The incidence of seizures in patients taking paroxetine is less than 0.1%. If a seizure occurs, treatment with paroxetine should be discontinued.

Electroconvulsive therapy

There is only limited experience with the concomitant use of paroxetine and electroconvulsive therapy.

Glaucoma

Like other SSRI drugs, paroxetine causes mydriasis and should be used with caution in patients with angle-closure glaucoma.

Hyponatremia

When treated with paroxetine, hyponatremia occurs rarely and mainly in elderly patients and is leveled off after discontinuation of paroxetine. '

Bleeding

Bleeding into the skin and mucous membranes (including gastrointestinal bleeding) has been reported in patients taking paroxetine. Therefore, paroxetine should be used with caution in patients who are concomitantly receiving drugs that increase the risk of bleeding, in patients with a known bleeding tendency, and in patients with diseases predisposing to bleeding.

Heart diseases

Normal precautions should be taken when treating patients with heart disease.

Symptoms that may occur when treatment with paroxetine is stopped in adults:

Anxiety disorders and experience with paroxetine

Anxiety disorders are extremely common, with 13–25% of the population experiencing anxiety disorders in their lifetime. According to the DSM-IV (Diagnostic and Statistical Manual) classification, anxiety disorders include [10]:

panic disorder;
generalized anxiety disorder;
agoraphobia without panic disorder;
obsessive-compulsive disorder;
social phobia;
specific phobias;
post-traumatic stress disorder;
acute stress disorder.

Many people are familiar with the symptoms of anxiety. They can be divided into general (mental and vegetative) and specific, determining the type of anxiety disorder. Common mental symptoms include restlessness, irritability, anxious thoughts, motor agitation, flinching at sudden sounds, decreased concentration, increased fatigue, impatience, inability to relax, sleep disturbances, and nightmares. The anxious mood is perfectly conveyed in Edvard Munch’s painting “Anxiety” (Fig. 1).

As a rule, mental symptoms of anxiety are accompanied by vivid vegetative symptoms. Thus, the face of the woman depicted in the picture is pale, tense, and her lips are dry. She keeps her hands on her neck. Perhaps this is a feeling of shortness of breath, a coma in the throat and a feeling of chills. Other autonomic symptoms of anxiety include tachycardia, increased sweating with cold, clammy palms, hot flashes or chills, dyspeptic disorders (abdominal pain, flatulence, diarrhea), dizziness, increased urination, increased physiological tremor, and increased muscle tone.

Clinical forms of anxiety disorders

Generalized anxiety disorder (GAD) is one of the most common forms of anxiety, with 4–9.2% of the population experiencing it during their lifetime [20]. The DSM-IV criteria for GAD are the presence of anxiety and restlessness in combination with at least three of the following symptoms:

impatience or feeling on edge;
increased fatigue;
difficulty concentrating or feeling empty in the head;
irritability;
muscle tension;
sleep disorders.

The duration of the disease must be at least 6 months, the symptoms must cause significant distress or affect social, professional and other areas of activity.

Panic disorder is also extremely common: according to epidemiological studies, panic attacks are observed in 1.5–4% of the population [11], although 35.9–46% of the human population have experienced panic at least once in their lives [2]. Panic disorder affects 6% of people seeking primary care [2]. The main clinical manifestation of panic disorder is panic attacks - attacks of severe anxiety, accompanied by somatic and cognitive symptoms. The main diagnostic signs of panic attacks are paroxysmal occurrence, polysystemic vegetative symptoms, and the presence of emotional disorders, the severity of which can range from a feeling of “discomfort” to “panic” [2]. Agoraphobia is very similar to panic disorder and is defined as anxiety that occurs in response to situations in which the solution is difficult or difficult, or when help will not be available if a panic attack develops. If anxiety in panic disorder can be defined as anxiety in anticipation of a subsequent attack, then agoraphobia is characterized by the presence of provoking factors or situations - being alone outside the house, being in a crowd, on a bridge (as in a Munch painting), traveling on public transport, etc. Provoking situations are actively avoided by patients; getting into them is accompanied by significant distress.

Specific phobias are characterized by the connection of anxiety with certain situations (air travel, contact with animals, the sight of blood, etc.), also accompanied by an avoidance reaction. Finding yourself in a phobic situation provokes an anxious reaction, similar to a panic attack. Patients are critical of their experiences, however, phobias have a significant impact on various areas of the patients’ activities. An example of a specific phobia can be found in the famous artist Pablo Picasso. “For a long time he was deathly afraid of getting his hair cut. For months I wore my hair too long and was hesitant to go to the hairdresser. As soon as someone started talking about it, he fell into a real panic. As a rule, it ended with him asking his loved ones to shorten his hair or locking himself in a small room and trying in vain to cut off his hair himself” [3, 11].

Social phobia is characterized by the occurrence of anxiety in social situations - communication and self-presentation (public speaking or even being in public), fear of possible condemnation from others. As with other anxiety disorders, patients actively avoid social situations because the anxiety causes them significant distress. Thus, the Russian critic and publicist V. G. Belinsky writes: “One thing torments me terribly: my timidity and embarrassment do not weaken, but increase in monstrous progression. I can’t show myself in public: my face is flaring up, my voice is trembling, my arms and legs are shaking, I’m afraid of falling. Self-affirmation is carried out in forms that are in every possible way opposed to accepted norms of behavior. Hence the eccentricity, wildness, and absurdity” [7, 11].

Obsessive-compulsive disorder is characterized by the presence of intrusive thoughts (obsessions) that increase anxiety and ritual actions or thoughts aimed at suppressing this anxiety. There are two key characteristics of symptoms in obsessive-compulsive disorder: egodystonia (the patient is unable to ignore or suppress the symptoms, although he is fully aware of their absurdity) and the presence of significant distress for a significant time (more than an hour a day). The most common obsessions are fear of contamination (45%), pathological doubts (42%), somatic obsessions (36%), the need for symmetry (31%), aggressive impulse (28%), sexual impulse (26%) [14]. Among the compulsions, the most common are checking (60%), washing (50%), counting (36%), the need to ask or admit something (31%), the need for symmetry/neatness (28%), hoarding (18%). ). Distinctive features of obsessive-compulsive disorder from other forms of anxiety disorders are an earlier age of onset, equal representation among both sexes (other forms of anxiety are more common in women), and a fairly high resistance to serotonergic drugs.

Post-traumatic stress disorder has 17 core symptoms, grouped into three groups: re-experiencing the trauma (instructive thoughts, nightmares, emotional and somatic reactions in response to memories), avoidance of memories associated with the trauma (avoidance of thoughts, feelings, places, acquaintances, inability to remember details of a situation, decreased interest in entertainment, withdrawal from other people, lack of prospects for the future) and agitation (sleep disturbances, irritability, difficulty concentrating, hypervigilance and increased startle reflex).

Difficulties in diagnosing anxiety disorders

The main reasons for underdiagnosis of anxiety disorders are the presence of subsyndromal forms of anxiety, as well as a wide range of comorbid disorders - depression, chronic pain syndromes, and other forms of anxiety disorders.

Diagnostic criteria for anxiety disorders are widely presented in the literature and are known to practicing physicians. However, in their daily practice, neurologists and internists much more often see not developed, but subsyndromal forms of anxiety disorders, when in the clinical picture of the disease it is not the mental, but the somatic or neurological components of anxiety that come to the fore. Thus, in the case of GAD, the DSM-IV diagnostic criteria have a significant drawback - they are mainly focused on the presence of mental symptoms, which can lead to underdiagnosis of the anxiety disorder. In the ICD-10 criteria, to make a diagnosis of GAD, the presence of 4 symptoms out of 22, divided into five groups - vegetative, respiratory or gastrointestinal symptoms, symptoms affecting mental activity, general symptoms and nonspecific symptoms, is required, but internists and doctors It is not always convenient for other specialties to use ICD-10 criteria. Starcevic V. et al. identified the most significant symptoms of GAD from the DSM-IV and ICD-10 classifications. The criteria proposed by the authors are much more convenient to use in everyday practice (

.) [18].

Recent epidemiological studies have shown a high prevalence of subsyndromal panic disorder that does not meet diagnostic criteria. In these cases, panic attacks, although rare, anxiety also significantly affects the lives of such patients [15]. Certain diagnostic difficulties can be caused by atypical panic attacks when clinical phenomena not covered by DSM-IV criteria are observed during an attack—diffuse or local pain syndromes, senestopathies, muscle tension, obsessions and compulsions, etc. [2]. There are 10 atypical, conversion symptoms of panic attacks: (1) feeling of a lump in the throat, (2) feeling of weakness in an arm or leg, (3) visual or hearing impairment, (4) gait disturbance, (5) speech or voice disturbance, ( 6) loss of consciousness, (7) a feeling that the body is arching, (8) cramps in the arms and legs, (9) nausea, vomiting, (10) abdominal discomfort [2].

When making a diagnosis of agoraphobia, it is necessary to remember that in cases where the patient has only one or two anxiety-provoking situations, it is necessary to think about specific phobias, and if the anxiety is associated only with social triggers, then about social phobia.

Another feature of panic disorder and agoraphobia is the presence of permanent autonomic disorders, which can occur predominantly in one system or be multisystem in nature [2]. These disorders can be the reason for contacting specialists of various profiles. Thus, patients can come to see a cardiologist with cardialgia, cardiosenestopathies, arterial hypo- and hypertension, syncope and lipothymic conditions, a feeling of lack of air, a feeling of suffocation, and Raynaud's syndrome. Gastroenterologists may encounter in their practice patients who persistently complain of dyspeptic symptoms, dry mouth, nausea, abdominalgia, constipation or diarrhea. Such patients should always request that their anxiety disorder be excluded.

Like other anxiety disorders, obsessive-compulsive disorder is underdiagnosed. Typically, patients with obsessive-compulsive disorder are embarrassed to talk about mental symptoms, even when asked about them directly. The following 5 questions can help a practitioner diagnose this type of anxiety disorder [19]:

Do you wash or clean things a lot?
Do you check something over and over again?
Do you have thoughts that bother you that you would like to get rid of, but you can’t?
Do your daily activities take up a lot of your time?
Is your attention focused on any order or symmetry?

Depression is an integral accompaniment of anxiety. Anxiety disorders occur in 57% of patients with depression [15]. The combination of anxiety and depression significantly aggravates the course of the disease. This is manifested by more severe symptoms, a tendency to chronicity, mental dysfunction, refusal to work, greater seeking of medical help, a greater risk of suicide and resistance to therapy.

Paroxetine in the treatment of anxiety disorders

Drugs of various pharmacological groups are used to treat anxiety disorders. However, antidepressants are currently considered the drugs of choice. Widely used until recently, anxiolytics, most of which are benzodiazepines, are not used as a basic drug, primarily due to frequent complications: sedation, behavioral toxicity, paradoxical reactions, tolerance, addiction, dependence, withdrawal and rebound syndrome, as well as the presence of drugs interactions. Among antidepressants, preference should be given to selective serotonin reuptake inhibitors (SSRIs) as they are effective and the most well tolerated drugs. Among the SSRIs, paroxetine is the most studied drug in the treatment of anxiety disorders.

For GAD, paroxetine has shown its effectiveness both in comparison with placebo and tricyclic antidepressants and benzodiazepines [17]. Thus, among patients receiving paroxetine, remission was achieved in 72%, while among patients receiving placebo, only 34% (p < 0.001). Already at 4 weeks of use, paroxetine significantly improved the level of anxiety on the HAM-A scale by 15.6 points compared to benzodiazepine, which improved the anxiety score by only 11.8 points (p < 0.01). The dose of paroxetine effective for the treatment of GAD is 20–40 mg/day (10–50 mg/day) [17].

Paroxetine is the most studied drug in the treatment of panic disorder and agoraphobia. In a large placebo-controlled study, paroxetine was effective compared with placebo, characterized by the occurrence of an attack-free period, at a dose of 40 mg/day (p < 0.02). Thus, when taking paroxetine, an attack-free period occurred in 86% of patients, and when taking placebo - in 50%. Paroxetine also had a significantly lower relapse rate (5%) compared to placebo (30%), p = 0.002 [16].

Studies have also been conducted on the effectiveness of paroxetine for social phobia and post-traumatic stress disorder. Among patients with social phobia, 55% of patients taking paroxetine and 24% of patients taking placebo were responders. In a study of the effectiveness of paroxetine for post-traumatic stress disorder, the differences with placebo were less significant due to the high placebo effect. In the paroxetine group, 60% of patients were responders, in the placebo group - 49% [19].

Obsessive-compulsive disorder is the most resistant to treatment among anxiety disorders. However, the effectiveness of paroxetine has also been proven in this form of anxiety, although in higher doses (40–60 mg/day). The paroxetine group showed a significant improvement on the Y-BOCS scale compared to placebo. The relapse rate was also significantly lower in the paroxetine group (38%) compared with the placebo group (59%), p < 0.033 [13].

Paroxetine has a favorable safety profile. The main side effects when taking it are headache, nausea and other gastrointestinal disorders, sleep disorders and sexual dysfunction. Side effects are not pronounced and regress on their own during the first weeks of taking the drug. The cardiac safety of paroxetine appears to be proven [12].

There is extensive experience in the use of Rexetine (paroxetine), including in domestic clinical practice. The clinical effects of Rexetine have been most studied in the treatment of anxiety disorders encountered in the practice of a neurologist and internist, although it can also be used in psychiatric clinics. Thus, in a study of the effectiveness of Rexetine at a dose of 20–60 mg/day in the treatment of anxiety and depressive disorders in patients who consulted a psychiatrist, the proportion of responders was 50% [1]. When taking Rexetine in patients with anxiety and depressive disorders against the background of dyscirculatory encephalopathy, remission was observed in 91% of patients [8].

In a neurological hospital, Rexetine was effective not only for panic disorder, but also for other diseases accompanied by anxiety - somatized dysthymia, “masked” depression, migraine, tension headache, and other chronic pain syndromes [4].

In the work of Less Yu. E. et al. [6] studied the effectiveness of Rexetine at a dose of 20 mg/day for GAD, taking into account comorbid anxiety and affective conditions (panic disorder, agoraphobia, obsessive-compulsive disorder, depression). The patients were divided into three groups. The first group consisted of patients with isolated GAD, the second group included patients with GAD accompanied by erased comorbid disorders at the subsyndromal level. The third research group included individuals with extensive, clinically significant comorbid disorders. The study confirmed the high effectiveness of Rexetine for GAD. In 35.9% of patients, a remission level was achieved by the end of the course of therapy, 17.9% were classified as responders, 28.3% as partial responders, and only 17.9% as non-responders. The dynamics of anxiety on the Hamilton scale, assessed in this study, are presented in

According to the dynamics of the total HAM-A score, a significant decrease in anxiety was noted at all time points (7, 14, 21, 28, 35 and 42 days from the start of taking Rexetine). The rate of reduction in symptoms, which was the same in all groups during the first two weeks of therapy, further slowed down in the group of patients with severe comorbid disorders, while in the groups of patients without comorbid disorders and with subclinical comorbid disorders, the therapeutic effect steadily increased, reaching a maximum level by the end of the study. By the time the course of therapy was completed, the regression of anxiety symptoms in the groups of patients without comorbid disorders and with subclinical comorbid disorders was significantly greater than in the group of patients with severe comorbid disorders [6]. Thus, this study confirms the information about the high effectiveness of Rexetine in the treatment of GAD. The anti-anxiety effect of the drug begins to manifest itself from the first days of therapy and gradually increases, reaching a maximum after a month of treatment. A dose of 20 mg appears to be adequate in most cases, but in cases of GAD complicated by comorbid emotional disorders, the dose of Rexetine should apparently be increased [6].

Rexetine has proven to be a highly effective drug for the treatment of specific phobias. With this form of anxiety disorder, a fairly rapid effect of Rexetine was noted. Already in the first week, there is a decrease in the feeling of internal tension, regression of vegetative symptoms (sweating, the intensity of the feeling of “incompleteness” of inspiration has decreased), and sleep improves. The most pronounced reduction in the intensity of anxious experiences and improvement in the well-being of patients was observed during the first 4 weeks of Rexetine therapy. Normalization of well-being to the initial, pre-painful state was observed starting from 3–4 weeks of treatment [9].

There is experience in using Rexetine in patients with somatic diseases and concomitant anxiety and depressive disorders. Thus, Rexetine can be used with antihypertensive, vascular, cardiological, antidiabetic and other drugs that are often necessary for patients for health reasons. It has been established that it does not cause addiction or dependence [5].

Our experience in using Rexetine in patients with anxiety and anxiety-depressive disorders showed that among 20 observed patients, 12 people (> 50%) noted complete remission after 6 months of therapy. In approximately 2/3 of cases (13 patients), comorbidity with depressive spectrum disorders was noted. The most common manifestations were: sad mood, depression, sleep disturbances, pain (in the neck and lower back), slowness of movements and speech. During therapy, a gradual reduction of these manifestations was observed. In the dynamics of anxiety symptoms, such manifestations as anxiety, fatigue, irritability, and muscle tension underwent the greatest regression. It should also be noted the effect of therapy on the presentation of autonomic manifestations of anxiety: tachycardia, hot and cold flashes, cold extremities. In general, according to patient reports, 14 of them (70%) rated the results of treatment as “good” or “excellent”. It should be noted that at the time of therapy, 4 patients were taking pharmacological agents prescribed by internists for concomitant diseases (beta-blockers, antihistamines, vasoactive drugs). In no case were there any signs of drug interactions. In addition, during therapy, one patient noted a decrease in episodes of existing tension-type headaches, in two cases a reduction in insomnia was observed, 4 patients noted a decrease in the intensity of accompanying pain manifestations (pain in the cervical region and lower back) and a decrease in the amount of analgesics consumed while taking Rexetine.

Thus, the proven effectiveness, high safety of Rexetine and extensive experience in its use in the treatment of anxiety disorders allow this drug to be actively used in everyday practice by doctors of various specialties.

Literature

Bobrov AC, Petrunko OB, Kovaleva AB, Pavlova O. N. Rexetine in the treatment of depressive states // Journal of Neurology and Psychiatry named after. S. S. Korsakova. 2005. No. 11.
Vein A. M., Dyukova G. M., Vorobyova O. V., Danilov A. B. Panic attacks. M.: Eidos Media. 2004. 408 p.
Gaev G. Geniuses in private life. M.: Kron-press. 1999.
Dmitriev O.V. Experience of using the drug Rexetine in a neurological hospital // Breast Cancer. 2005. T. 13. No. 22.
Enikolopov S. Anxiety and hypertension. Vicious circle // Ukrainian Rheumatology Journal. 2008. No. 2 (32). pp. 27–28.
Less Yu. E., Malygin Ya. V., Chakhava V. O. Efficacy of the drug Rexetine in patients with generalized anxiety disorder // Breast Cancer. 2005. T. 13. No. 22.
Pietsukh V. A. Literary dreams of V. G. Belinsky. A comment. M.: Moscow worker. 1989.
Retyunsky K. Yu., Khmelnova I. V., Malkova E. B. Therapeutic effectiveness of rexetine in vascular depression // Psychiatry and psychopharmacotherapy. 2005. T. 7. No. 6.
Rumyantseva G.M., Stepanov A.L., Levina T.M. Clinical effectiveness of the drug “Rexetine” (paroxetine) for anxiety spectrum disorders // Psychiatry and psychopharmacotherapy. 2005. T. 7. No. 6.
Smulevich A. B. Depression in general medical practice. M., 2000. 160 p.
Shuvalov A.V. Psychiatry, narcology, sexopathology. New classification of ICD-10. M.: Soviet sport. 2001.
DeVane CL Pharmacokinetics, drug interactions and tolerability of paroxetine and paroxetine CR // Psychopharmacology Bulletin. 2003. V. 37 (Suppl1). P. 29–41.
Ninan TP Obsessive-compulsive disorder: implications of the efficacy of an SSRI, paroxetine // Psychopharmacology Bulletin. 2003. V. 37 (Suppl. 1). P. 89–96.
Nutt D., Ballenger J. Anxiety disorders. Generalized anxiety disorder, obsessive-compulsive disorder and post-traumatic stress disorder // Blackwell Publishing. 2005. 242 p.
Nutt D., Feeney A., Argyropolous S. Anxiety disorders comorbid with depression: panic disorder and agoraphobia // Martin Dunitz. 2002. 111 p.
Pollack MH, Doyle AC Treatment of panic disorder: focus on paroxetine // Psychopharmacology Bulletin. 2003. V. 37 (Suppl. 1). P. 53–63.
Sheehan DV, Mao CG Paroxetine treatment of generalized anxiety disorder // Psychopharmacology Bulletin. 2003. V. 37 (Suppl. 1). P. 64–75.
Starcevic V., Bogojevic G. The concept of generalized anxiety: disorder between the too narrow and too wide diagnostic criteria // Psychopathology. 1999. V. 32. P. 5–11.
Stein DJ, Hollander E. Anxiety disorders comorbid with depression: social anxiety disorder, post-traumatic stress disorder, generalized anxiety disorder, obsessive-compulsive disorder // Martin Dunitz. 2002. 72 p.
Walley EJ, Beebe DK, Clark JL Management of common anxiety disorders // Am Fam Physician. 1994. V. 50. P. 1745–1753.

G. R. Tabeeva Yu. E. Azimova

MMA im. I. M. Sechenova, Moscow

Table.

Rice. 2.

Paroxetine, 30 pcs., 20 mg, film-coated tablets

Paroxetine is an antidepressant. It is a selective inhibitor of serotonin (5-hydroxytryptamine, 5-HT) reuptake by brain neurons, which determines its antidepressant effect and effectiveness in the treatment of obsessive-compulsive (OCD) and panic disorder.

Paroxetine has low affinity for m-cholinergic receptors (has a weak anticholinergic effect), α1-, α2- and β-adrenergic receptors, as well as dopamine (D2), 5HT1-like, 5HT2-like and histamine H1 receptors. Paroxetine does not disrupt psychomotor functions and does not potentiate the inhibitory effect of ethanol on them.

Behavioral and EEG studies show that paroxetine exhibits weak activating properties when administered at doses above those required to inhibit serotonin uptake. Does not cause significant changes in blood pressure, heart rate and EEG levels.

Pharmacokinetics

Suction

After oral administration, paroxetine is well absorbed from the gastrointestinal tract and undergoes first-pass metabolism through the liver.

Distribution

Css is achieved 7-14 days after the start of therapy. With increasing dose and/or duration of treatment, a nonlinear dependence of the pharmacokinetic parameters on the dose is observed.

Paroxetine is extensively distributed in tissues, only 1% of it is present in plasma.

95% protein bound.

Metabolism

Metabolized in the liver to form inactive metabolites. It is an inhibitor of the CYP2D6 isoenzyme.

The main metabolites of paroxetine are polar and conjugated oxidation and methylation products that are quickly eliminated from the body, have weak pharmacological activity and do not affect its therapeutic effect. When paroxetine is metabolized, the selective uptake of serotonin by neurons due to its action is not impaired.

Removal

About 64% of paroxetine is excreted in the urine (2% unchanged, 64% as metabolites); approximately 36% is excreted in bile through the intestines, mainly in the form of metabolites, less than 1% - unchanged.

The elimination of paroxetine metabolites is biphasic, initially as a result of first-pass metabolism through the liver, and then it is controlled by systemic elimination. T1/2 of paroxetine varies, but averages 24 hours.

Pharmacokinetics in special clinical situations

The concentration of paroxetine in the blood plasma increases with impaired liver and kidney function, as well as in the elderly.

Reviews

Mikhail M .: “I took paroxetine for three months. The drug helped me, there were no special side effects. For the holiday I decided to drink a little alcohol, but I didn’t stop taking the pills. Despite the fact that I used to tolerate alcohol well, this time after drinking alcohol, my stomach on the right began to hurt. Doctors diagnosed me with hepatitis, it turned out that this medicine cannot be taken with alcohol.”

Psychiatrist : “Many patients suffering from anxiety and depression look for solutions to their problems “at the bottom of the bottle.” Before starting treatment with paroxetine, we warn them that either take medication and become a healthy person, or continue to drink alcohol, but this may end badly. Patients who try to combine both cause significant harm to their health, and sometimes end up in intensive care.”

Content

Paroxetine tablet p/o film 20mg 30 pcs bfz

Children and adolescents (under 18 years of age) Paroxetine should not be used in children and adolescents under 18 years of age. Treatment with antidepressants in children and adolescents with moderate to severe depressive episodes, recurrent depressive disorder, and other mental illnesses is associated with an increased risk of suicidal thoughts and behavior. In clinical studies, adverse reactions associated with suicide attempts and suicidal ideation, hostility (mainly aggression, deviant behavior and anger) were observed more often in children and adolescents receiving paroxetine than in patients in this age group who received placebo. There are currently no data on the long-term safety of paroxetine in children and adolescents regarding the effects of this drug on growth, maturation, cognitive and behavioral development.

Clinical worsening and suicidal risk in adults Young patients, especially those with major depressive disorder, may be at increased risk of suicidal behavior during paroxetine therapy. An analysis of placebo-controlled studies in adults suffering from mental illness indicates an increase in the frequency of suicidal behavior in young patients (aged 18-24 years) while taking paroxetine compared with the placebo group (2.19% to 0.92%, respectively ), although this difference is not considered statistically significant. In patients of older age groups (from 25 to 64 years and over 65 years), an increase in the frequency of suicidal behavior was not observed. In adults of all age groups suffering from major depressive disorder, there was a statistically significant increase in the incidence of suicidal behavior during treatment with paroxetine compared with the placebo group (incidence of suicide attempts: 0.32% to 0.05%, respectively). However, the majority of these cases with paroxetine (8 of 11) were reported in young patients aged 18 to 30 years. Data obtained from a study of patients with major depressive disorder may indicate an increase in the incidence of suicidal behavior in young patients, which may persist in patients over 24 years of age suffering from various mental disorders. In patients with depression, worsening symptoms of the disorder and/or the emergence of suicidal thoughts and behavior (suicidality) may occur regardless of whether they are receiving antidepressants. This risk persists until significant remission is achieved. The patient's condition may not improve in the first weeks of treatment or more, and therefore the patient's condition should be monitored for timely detection of clinical exacerbation and suicidality, especially at the beginning of the course of treatment, as well as during periods of dose changes, whether increasing or decreasing them. Clinical experience with all antidepressants suggests that the risk of suicide may increase in the early stages of recovery. Other mental disorders for which paroxetine is used may also be associated with an increased risk of suicidal behavior. In addition, these disorders may represent comorbid conditions associated with major depressive disorder. Therefore, when treating patients suffering from other mental disorders, the same precautions should be taken as when treating major depressive disorder. Those most at risk for suicidal ideation or suicide attempts are patients with a history of suicidal behavior or suicidal ideation, young patients, and patients with severe suicidal ideation before treatment and should therefore all receive special attention during treatment. Patients (and those caring for them) should be warned to monitor for worsening of their condition (including the development of new symptoms) and/or the emergence of suicidal ideation/behavior or thoughts of self-harm throughout the course of treatment, especially at the beginning of treatment , or during changes in the dose of the drug (increase and decrease). If these symptoms occur, you should seek immediate medical attention. It must be remembered that the appearance of symptoms such as agitation, akathisia or mania can be associated both with the underlying disease and as a consequence of the therapy used. If symptoms of clinical deterioration (including the development of new symptoms) and/or suicidal thoughts/behavior occur, especially if they appear suddenly, increase in severity, or if they were not part of the patient's previous symptom complex, it is necessary to reconsider the treatment regimen until before discontinuing the drug.

Akathisia Rarely, treatment with paroxetine or another SSRI drug is accompanied by the occurrence of akathisia, which is manifested by a feeling of internal restlessness and psychomotor agitation, when the patient cannot sit or stand quietly; with akathisia, the patient usually experiences subjective discomfort. The likelihood of akathisia occurring is highest in the first few weeks of treatment.

Serotonin syndrome, neuroleptic malignant syndrome In rare cases, serotonin syndrome or neuroleptic malignant syndrome-like symptoms may occur during treatment with paroxetine, especially if paroxetine is used in combination with other serotonergic drugs and/or antipsychotics. These syndromes may be potentially life-threatening and therefore treatment with paroxetine should be discontinued if they occur (they are characterized by clusters of symptoms such as pyrexia, muscle rigidity, myoclonus, autonomic disturbances with possible rapid changes in vital signs, mental status changes including confusion consciousness, irritability, extremely severe agitation progressing to delirium and coma), and begin supportive symptomatic therapy. Paroxetine should not be used in combination with serotonin precursors (such as L-tryptophan, oxytriptan) due to the risk of developing serotonergic syndrome.

Mania and Bipolar Disorder A major depressive episode may be the initial manifestation of bipolar disorder. It is generally accepted (although not proven in controlled clinical trials) that treating such an episode with an antidepressant alone may increase the likelihood of an accelerated, mixed, or manic episode in patients at risk for bipolar disorder. Before initiating antidepressant treatment, careful screening should be performed to assess the patient's risk of bipolar disorder; Such screening should include a detailed psychiatric history, including a family history of suicide, bipolar disorder, and depression. Paroxetine is not registered for the treatment of depressive episodes in bipolar disorder. As with other antidepressants, paroxetine should be used with caution in patients with a history of mania.

Diabetes mellitus In patients with diabetes mellitus, treatment with SSRI drugs may affect glycemic control. Dosage adjustments of insulin and/or oral hypoglycemic medications may be required.

Monoamine oxidase inhibitors (MAOIs) Treatment with paroxetine should be initiated cautiously 2 weeks after discontinuation of treatment with irreversible MAOIs or 24 hours after discontinuation of treatment with reversible MAOIs. The dose of paroxetine should be increased gradually until the optimal therapeutic effect is achieved.

Renal or hepatic impairment Caution is advised when treating patients with severe renal impairment or patients with impaired liver function with paroxetine.

Epilepsy Like other antidepressants, paroxetine should be used with caution in patients with epilepsy.

Seizures The incidence of seizures in patients taking paroxetine is less than 0.1%. If a seizure occurs, treatment with paroxetine should be discontinued.

Electroconvulsive therapy There is only limited experience with the concomitant use of paroxetine and electroconvulsive therapy.

Glaucoma Like other SSRI drugs, paroxetine can cause mydriasis and should be used with caution in patients with angle-closure glaucoma.

Hyponatremia When treated with paroxetine, hyponatremia occurs rarely and mainly in elderly patients and is leveled off after discontinuation of paroxetine.

Bleeding Bleeding into the skin and mucous membranes (including gastrointestinal and gynecological bleeding) has been reported in patients taking paroxetine.

Therefore, paroxetine should be used with caution in patients who are concomitantly receiving drugs that increase the risk of bleeding, in patients with a known bleeding tendency, and in patients with diseases predisposing to bleeding.

Heart Disease The usual precautions should be taken when treating patients with heart disease.

Symptoms that may occur when stopping treatment with paroxetine in adults: In clinical trials in adults, the incidence of adverse reactions when discontinuing paroxetine was 30%, while the incidence of adverse reactions in the placebo group was 20%. The occurrence of withdrawal symptoms does not mean that the drug is abused or addictive, as is the case with narcotics and psychotropic substances.

Withdrawal symptoms reported include dizziness, sensory disturbances (including paresthesias, electric shock sensations, and tinnitus), sleep disturbances (including vivid dreams), agitation or anxiety, nausea, tremor, confusion, sweating, headache, and diarrhea. palpitations, emotional lability, irritability and visual disturbances. These symptoms are usually mild or moderate, but in some patients they can be severe.

They usually occur in the first few days after stopping the drug, but in very rare cases they occur in patients who accidentally missed just one dose. Typically, these symptoms resolve spontaneously and disappear within 2 weeks, but in some patients they can last much longer (2-3 months or more).

It is recommended that the dose of paroxetine be reduced gradually over several weeks or months before discontinuing it completely, depending on the needs of the individual patient.

Bone fractures Based on the results of epidemiological studies of the risk of bone fractures, a connection between bone fractures and the use of certain antidepressants, including SSRI drugs, has been identified. The risk was observed during the course of treatment with antidepressants and was greatest at the beginning of the course of therapy. The possibility of bone fractures should be considered when using paroxetine.

Tamoxifen Some studies have shown that the effectiveness of tamoxifen, as measured by the risk of breast cancer recurrence and mortality, may be reduced when coadministered with paroxetine as a result of irreversible inhibition of CYP2D6. The risk may increase with coadministration over a long period of time. When treating or preventing breast cancer, the use of alternative antidepressants that do not affect the CYP2D6 isoenzyme or have a lesser effect should be considered.

Although paroxetine does not increase the negative effects of alcohol on psychomotor functions, it is not recommended to use paroxetine and alcohol simultaneously.

Effects on the ability to drive vehicles and operate machinery Clinical experience with paroxetine indicates that it does not impair cognitive and psychomotor functions. However, as with treatment with any other psychotropic drugs, patients should be especially careful when driving a car and operating machinery.