Paxil sleep. Paxil storage conditions. Anxiety disorders and Paxil

Antidepressant, selective serotonin reuptake inhibitor. It has a bicyclic structure, different from the structure of other known antidepressants.

It has an antidepressant and anxiolytic effect with a fairly pronounced stimulating (activating) effect.

The antidepressant (thymoanaleptic) effect is associated with the ability of paroxetine to selectively block the reuptake of serotonin by the presynaptic membrane, which causes an increase in the free content of this neurotransmitter in the synaptic cleft and an increase in its activity in the central nervous system.

The effect on m-cholinergic receptors, α- and β-adrenergic receptors is insignificant, which determines the extremely weak severity of the corresponding side effects.

Pharmacokinetics

After oral administration, paroxetine is well absorbed from the gastrointestinal tract. Eating does not affect absorption. C ss is established by 7-14 days from the start of therapy.

The main metabolites of paroxetine are polar and conjugated oxidation and methylation products. Due to the low pharmacological activity of metabolites, their effect on therapeutic efficacy is unlikely.

T 1 / 2 averages 16-24 hours. Less than 2% is excreted in the urine unchanged, the rest - in the form of metabolites either in the urine (64%) or in the bile.

Excretion of paroxetine is biphasic.

With long-term continuous administration, pharmacokinetic parameters do not change.

Release form

Film-coated tablets white color, oval, biconvex, engraved with "20" on one side and a notch on the other.

Excipients: calcium hydrophosphate dihydrate - 317.75 mg, sodium carboxystarch type A - 5.95 mg, magnesium stearate - 3.5 mg.

Compound film shell: Opadry white - 7 mg (hypromellose - 4.2 mg, titanium dioxide - 2.2 mg, macrogol 400 - 0.6 mg, polysorbate 80 - 0.1 mg).

10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.

Dosage

When taken orally, the initial dose is 10-20 mg / day. If necessary, depending on the indications, the dose is increased to 40-60 mg / day. The dose increase is carried out gradually - by 10 mg with an interval of 1 week. Reception frequency - 1 time / day. The treatment is long. The effectiveness of therapy is assessed after 6-8 weeks.

For elderly and debilitated patients, as well as for impaired renal and hepatic function, the initial dose is 10 mg / day; maximum dose- 40 mg / day.

Interaction

With simultaneous use with paroxetine, an increase in plasma concentrations of drugs metabolized with the participation of the CYP2D6 isoenzyme of the cytochrome P 450 system (antidepressants, antipsychotics phenothiazine derivatives, class IC antiarrhythmic drugs).

With the simultaneous use of agents that induce or inhibit protein metabolism, changes in the metabolism and pharmacokinetic parameters of paroxetine are possible.

With simultaneous use, the effect of alprazolam is enhanced due to a decrease in its metabolism due to inhibition of CYP3A isoenzymes of the cytochrome P450 system under the influence of paroxetine.

With simultaneous use with warfarin, oral anticoagulants, an increase in bleeding time is possible with unchanged prothrombin time.

With simultaneous use with dextromethorphan, dihydroergotamine, cases of serotonin syndrome are described.

With simultaneous use with interferon, a change in the antidepressant effect of paroxetine is possible.

The simultaneous use of tryptophan can cause the development of serotonin syndrome, manifested by agitation, anxiety, disorders of the gastrointestinal tract, including diarrhea.

With simultaneous use with perphenazine, it increases the side effects from the central nervous system due to inhibition of the metabolism of perphenazine under the influence of paroxetine.

With simultaneous use, the concentration in the blood plasma of tricyclic antidepressants increases, there is a risk of developing serotonin syndrome.

Simultaneous administration of cimetidine increases the concentration of paroxetine in the blood plasma.

Side effects

From the side of the central nervous system: rarely (when used in doses of more than 20 mg / day) - drowsiness, tremor, asthenia, insomnia.

From the side digestive system: rarely (when used in doses of more than 20 mg / day) - nausea, dry mouth; in some cases - constipation.

Others: rarely (when used in doses of more than 20 mg / day) - increased sweating, ejaculation disorders.

Indications

Endogenous, neurotic and reactive depressions.

Contraindications

Simultaneous use of MAO inhibitors and a period of up to 14 days after their withdrawal, hypersensitivity to paroxetine.

Application features

Application for violations of liver function

Application for violations of kidney function

Use in elderly patients

special instructions

Stopping the use of paroxetine should be carried out by gradually reducing the dose, in order to avoid the withdrawal syndrome, which is manifested by dizziness, nausea, vomiting, insomnia, confusion, increased sweating.

During treatment with paroxetine, alcohol is contraindicated.

Use with caution 14 days after the abolition of MAO inhibitors, gradually increasing the dose. MAO inhibitors should not be prescribed within 2 weeks after the complete withdrawal of paroxetine.

When used simultaneously with drugs that inhibit the metabolism of liver enzymes, paroxetine should be used at the lowest recommended doses. When used simultaneously with drugs that induce enzyme metabolism, no change in the initial doses of paroxetine is required.

Use paroxetine with caution with lithium preparations (it is recommended to control the concentration of lithium in the blood plasma), oral anticoagulants.

AT experimental studies the carcinogenic and mutagenic properties of paroxetine have not been established.

Influence on the ability to drive vehicles and control mechanisms

Use with caution in patients whose activities are associated with the need high concentration attention and speed of psychomotor reactions.

Country of origin

Product group

Antidepressant

Release forms

• Tablets of 20 mg - 100 pieces per pack. Tablets 20mg - 30pcs per pack.

Description of the dosage form

• White, film-coated, oval, biconvex tablets, debossed with "20" on one side and a break line on the other.

pharmachologic effect

Pharmacokinetics

Special conditions

Compound

• paroxetine hydrochloride hemihydrate 22.8 mg, which corresponds to the content of paroxetine 20 mg Excipients: calcium dihydrophosphate dihydrate, sodium carboxystarch type A, magnesium stearate. Shell composition: hypromellose, titanium dioxide, macrogol 400, polysorbate 80

Paxil indications for use

• - depression of all types, including reactive depression and severe depression, depression accompanied by anxiety (the results of studies in which patients received the drug for 1 year show that it is effective in preventing relapses of depression); - treatment (including maintenance and preventive therapy) of obsessive-compulsive disorder (OCD). In addition, paroxetine is effective in preventing OCD relapses; - treatment (including supportive and preventive therapy) of panic disorder with and without agoraphobia. In addition, paroxetine is effective in preventing the recurrence of panic disorder; - treatment (including supportive and preventive therapy) of social phobia; - treatment (including maintenance and preventive therapy) of generalized anxiety disorder. In addition, paroxetine is effective in preventing relapses. this disorder; - treatment of post-traumatic stress disorder.

Paxil contraindications

• - simultaneous reception MAO inhibitors and the period of 14 days after their withdrawal (MAO inhibitors cannot be prescribed within 14 days after the end of treatment with paroxetine); - simultaneous reception of thioridazine; - concomitant use of pimozide; - age up to 18 years (supervised clinical researches paroxetine in the treatment of depression in children and adolescents has not been proven effective, so the drug is not indicated for the treatment of this age group). Paroxetine is not prescribed to children under the age of 7 years due to the lack of data on the safety and efficacy of the drug in this category of patients. - hypersensitivity to paroxetine and other components of the drug.

Paxil dosage

• 20 mg 20 mg

Paxil side effects

• The frequency and intensity of some side effects may decrease with continued therapy and usually do not lead to discontinuation of treatment. Determination of the frequency of side effects: very often (> 1/10), often (> 1/100, 1/1000, 1/10 000,

drug interaction

Overdose

Storage conditions

• store at room temperature 15-25 degrees
• keep away from children

Paxil is one of the most commonly used antidepressants. Reviews about the drug among patients and doctors are very different. Your popularity this remedy deserved the ability to cope with various anxiety, stressful conditions, phobias and . The drug does not cause drowsiness, pressure drops, sleep disturbances, depression brain activity which is especially important for working and active patients.

Consider the feedback from patients and doctors about the application this drug in the treatment of various anxiety and depressive disorders.

Patient reviews

“I was prescribed a course of treatment with Paxil. The doctor immediately warned about possible side effects. Started treatment with 10 mg per day.

The first day of therapy was harmless. However, for the next 5-6 days I felt some Strange feeling detachment at home, on the street and even at work. This, of course, alerted me, but the doctor said that this is such a period of adaptation and it needs to be endured. From the second week of treatment, the dose of the drug was prescribed 20 mg. To my surprise, increasing the dose of the drug not only did not cause discomfort, and even eliminated the mild nausea that was observed after taking 10 mg in previous days. With an increase in the dose, the feeling of detachment disappeared, for some time there was even a slight euphoria. I have been taking the drug for the third month now. I feel great."

Alyona

“I was treated with Paxil for depression for about 3 years. Several times I tried to stop taking the pills, but each time the symptoms resumed already on the 3rd day. I feel like a drug addict. However, this is better than that from which the treatment began. ”

Irina

“I was prescribed Paxil two weeks ago. The drug seems to be well tolerated, but I'm very afraid that it will be addictive. However, the doctor says that the abolition of the drug will not bring me any inconvenience if all his recommendations are followed.

Oksana

“Treatment with Paxil was effective for me, but the withdrawal syndrome negates all the advantages of this drug. It was very difficult and took a long time to cancel it. I think it's better to do with other drugs that do not cause such addiction.

Elena

Of course, after reading different reviews about Paxila (often quite unflattering), terribly nervous. I was even ready to attack the doctor with claims about prescribing this drug to me. However, in the morning she pulled herself together. The doctor explained that the remedy is very effective, but requires caution in following the rules of appointment and cancellation. Indeed, I did not feel any unpleasant symptoms, despite my fears. And here is the improvement general condition was noticeable already in the third week of treatment.

Lily

“I was prescribed to take Paxil 20 mg per day. The first two days I tried to somehow endure it, but on the third day I decided that I would no longer take it. Was great weakness, nausea, several times even vomiting, dizziness. For me, it’s better to be in a state of depression than to be treated with such drugs.”

Natalia

“A few years ago, Paxil was also attributed to me. The dose was increased gradually from 10 mg to 20 mg after a week. They also canceled gradually. The course of treatment lasted 9 months. The first two weeks there was a feeling of slight malaise, but soon everything passed. No withdrawal syndrome at the end of the course was observed. I can only say positive things about efficiency. I wanted to live and enjoy life again. There are situations when it is worth asking for help from specialists, and not trying to cope with the problem yourself.

Julia

« Paxil has been familiar to me for several years. This drug was once taken by my mother. After a series of troubles and stresses, I also happened to start taking this remedy. At first I tried to get by with only consultations of a psychotherapist, but without medicines yet it didn't work out. Of course, I was somewhat worried about the fact that certain side effects and even addiction could develop from taking Paxil. However, I did not notice any unpleasant symptoms from the treatment. 7 months of treatment brought me back to life. Now I have almost forgotten about my former depression. The drug is effective and well tolerated."

Alina

“I associate Paxil with the most bad memories. I took it for five days. It seems to me that if before the treatment I had some mental disorders, then while taking these pills, the symptoms only worsened. I decided for myself once and for all that I would not take antidepressants, no matter how bad it was for me.

Hope

“Paxil was prescribed to me for treatment postpartum depression. The course of treatment was about 10 months. Gradually the dose was increased to 30 mg, then reduced. Satisfied with the effect, it is tolerated medicine fine. No serious side effects were observed."

Taisia

“Paxil was prescribed to me after a car accident. It is worth noting that after this event, a lot has changed in my life. And the restoration of the body turned out to be more difficult mentally than physically. Antidepressants were not prescribed to me right away. At first, I thought I could handle stress on my own.

However, as time went on, the situation only worsened. I was tormented by insomnia, when I fell asleep, nightmares arose. I was terribly afraid to walk down the street, nothing made me happy. After the appointment, Paxila experienced some discomfort associated with mild nausea, weakness, dizziness. However, with the beginning of the third week of treatment, everything went away. It is worth noting that in addition to Paxil, other drugs were prescribed to me. The treatment lasted 12 months. Now I feel great, I don’t even remember about past problems. ”

Marina

Reviews of doctors

“Antidepressants should only be prescribed in extreme cases. I believe that treatment of anxiety-depressive disorders should begin with regular consultations with a psychotherapist. Only when they are ineffective can the use of antidepressants be considered.

Anna

“Paxil is a real lifesaver for depressed patients. I would like to note the special effectiveness of the drug in the presence of suicidal tendencies in patients. The drug is excellent for various types mental disorders even if others fail medications. Quite often, if it is necessary to prescribe an antidepressant to patients, I opt for Paxil.

Inna

« The drug Paxil has earned the trust of many doctors due to its availability and high efficiency. Subject to correct mode dosing of the drug at the beginning and end of treatment, the tolerability of the drug is quite good. Side effects or overdose are extremely rare. If the patient has panic attacks, I prefer to combine Paxil with nootropic drugs».

Lydia

“Paxil is one of the few antidepressants that does not have a hypnotic effect on the patient. Also, the drug does not suppress brain activity. Thus, Paxil is suitable for the treatment of a patient who is forced to continue working despite the start of treatment. Another positive property drug is the lack of its effect on heart rate and blood pressure.

Vitaly

Paxil is an excellent drug for the treatment anxiety states and depression. However, the problem of using Paxil in the treatment of such patients lies in its incorrect prescription. Many doctors, due to the lack of regular use of Paxil in practice, do not know how to properly titrate the drug at the beginning and end of the course of treatment (treatment begins with a quarter of a tablet with a gradual transition to a whole). Also, to reduce the likelihood of side effects from Paxil, tranquilizers (benzodiazepine series) are prescribed. From the second week of such treatment, Paxil can be used alone.

Dmitry

“The drug is good, if it is necessary to prescribe an antidepressant, I choose it. Many patients are afraid of addiction to the drug and the withdrawal syndrome. However, I would like to clarify the situation.

There is no addiction to this drug. All unpleasant symptoms that occur when Paxil is canceled are due to the fact that the disturbances in the body have not been completely eliminated, but only the effect of the drug has been temporarily eliminated. Paxil only temporarily eliminates the signs of a mental disorder. However, in the case serious violations, besides it, the appointment of other medications, for example, homeopathic medicines, is required.

Valentine

“I rarely prescribe Paxil to my patients. I prefer to manage with the advice of a psychologist and the appointment of phytopreparations. If these measures are ineffective, I refer the patient for treatment by a psychotherapist.

Evgenia

“Paxil is an excellent drug for eliminating the manifestations of anxiety and depressive states. However, it should be borne in mind that in the presence of serious mental disorders required A complex approach to the treatment of the patient. Subject to the recommendations for the selection of individual effective dose drug, Paxil is an excellent anti-anxiety agent.

Paroxetine hydrochloride hemihydrate 22.8 milligrams (equivalent to 20.0 milligrams paroxetine ), as excipients: calcium dihydrogen phosphate dihydrate , sodium carboxymethyl starch type A, magnesium stearin shell tablets - Opadry white YS - 1R - 7003 (macrogol 400, titanium dioxide, hypromellose, polysorbate 80).

Release form

The drug is available in biconvex tablets, packed in blisters of 10 pieces, one package may contain one, three or ten blisters.

pharmachologic effect

Renders antidepressant action according to the mechanism of specific inhibition by reuptake in functional brain cells - neurons .

Pharmacodynamics and pharmacokinetics

Has a low affinity for muscarinic cholinergic receptors . As a result of the research, data were obtained that:

• On animals anticholinergic properties appear weakly.
• Paroxetine in vitro studies - poor affinity for α1-, α2- and β-adrenergic receptors , including to dopamine (D2), serotonin subtype 5-HT1- and 5-HT2- , including histamine receptors(H1) .
• In vivo studies confirm in vitro results - no interaction with postsynaptic receptors and does not depress the central nervous system and does not cause arterial hypotension .
• Without breaking psychomotor functions , paroxetine does not increase the inhibitory effect ethanol on the central nervous system .
• The study behavioral changes and showed that paroxetine is able to cause a weak activating effect at a dose exceeding the slowing down of serotonin reuptake, while the mechanism is not amphetamine-like .
• On the healthy body paroxetine does not significant changes AD(), heart rate and EKG.

With regard to pharmacokinetics, after oral administration, the drug absorbed and metabolized during the "first pass" of the liver, as a result of which less paroxetine enters than absorbed from the gastrointestinal tract. By increasing the amount of paroxetine in the body (single dose large doses or repeated intake of usual doses) achieve partial saturation metabolic pathway and reduced clearance of paroxetine, resulting in a disproportionate increase in plasma concentrations of paroxetine. This means that the pharmacokinetic parameters are unstable and the kinetics are non-linear. However, non-linearity is usually mild and occurs in patients taking low doses of the drug, which cause low level paroxetine in plasma. It is possible to achieve equilibrium concentration in plasma in 1-2 weeks.

Paroxetine is distributed in tissues, and according to pharmacokinetic calculations, 1% of the total amount of paroxetine that is present in the body remains in plasma. At therapeutic concentrations, approximately 95% of paroxetine in plasma is bound to proteins . There was no relationship between plasma concentrations of paroxetine and clinical effects. adverse reactions. He is able to penetrate breast milk and in embryos .

Biotransformation occurs in 2 phases: including primary and systemic elimination before inactive polar and conjugated products as a result of the process oxidation and . Half-life varies within 16-24 hours. Approximately 64% are excreted in the urine as metabolites, 2% - unchanged; the rest - with feces metabolites and 1% - unchanged.

Indications for use

The drug is used in all types of adults, including reactive and severe, accompanied by anxiety, for supportive and preventive therapy. Children and adolescents 7-17 years old panic disorder with and without agoraphobia, social phobias, generalized anxiety disorders, post-traumatic stress disorder.

Contraindications

Hypersensitivity to paroxetine or other constituents.

Side effects

A decrease in the frequency and intensity of individual side effects of paroxetine occurs as the course of treatment progresses, therefore, do not require discontinuation of the appointment. The frequency gradation is as follows:

• very often (≥1/10);
• often (≥1/100,<1/10);
• sometimes happens (≥1/1000,<1/100);
• rarely (≥1/10,000,<1/1000);
• very rarely (<1/10 000), учитывая отдельные случаи.

Frequent and very frequent occurrence is determined on the basis of generalized data on the safety of the drug in more than 8 thousand patients. Clinical Trials were carried out to calculate the difference in the frequency of side effects in the Paxil group and the second placebo group. The incidence of rare or very rare side effects of Paxil is based on post-marketing information on the frequency of reports, and not the true frequency of these effects.

Side effect rates are stratified by organ and frequency:

• Blood and lymphatic system: rarely happen abnormal (hemorrhage into the skin and mucous membranes). Very rarely possible thrombocytopenia .
• Endocrine system: very rarely - violation of secretion.
• The immune system: very rare allergic reactions type and .
• Metabolism: "often" cases of decrease, sometimes in elderly patients with impaired secretion of ADH - hyponatremia .
• CNS: often occurs or , seizures ; rarely - clouding of consciousness , manic reactions as possible symptoms of the disease itself.
• Vision: very rare exacerbation , but "often" - blurred vision.
• The cardiovascular system: "rarely" noted sinus , as well as a transient decrease or increase in blood pressure.
• Respiratory system, chest and mediastinum: "often" noted yawn .
• gastrointestinal tract : "very often" fixed nausea ; often, or dry mouth ; gastrointestinal bleeding is very rarely recorded.
• Hepatobiliary system: rather "rarely" there was an increase in the level of production hepatic ; very rare cases accompanied by jaundice and/or liver failure .
• Epidermis: often recorded; rare case skin rashes and very rare reactions photosensitivity .
• urinary system: Rarely recorded.
• reproductive system: very often - cases sexual dysfunction ; rare and galactorrhea .
• Among common disorders: often fixed asthenia , and very rarely - peripheral edema.

An approximate list of symptoms that may occur after completion of the course has been established paroxetine : "often" was noted by others sensory disturbances , sleep disturbances, the presence of a feeling of anxiety, ; sometimes - strong emotional arousal , nausea , sweating , as well as diarrhea . Most often, these symptoms in patients are mild and mild, disappear without intervention. Patient groups at increased risk of side effects have not been registered, but if there is no greater need for treatment with paroxetine, the dose is gradually reduced until complete withdrawal.

Paxil tablets, instructions for use (Method and dosage)

Tablets are taken orally, swallowed whole and not chewed. Take once a day in the morning with meals.

Interaction

Paroxetine is not recommended for use with MAO inhibitors , as well as within 2 weeks after the completion of the course; in combination with, because, like other drugs that inhibit activity enzyme CYP2 D6 cytochrome P450 , increases the concentration of thioridazine in plasma. Paxil is able to enhance the effect of alcohol-containing drugs and reduce the effectiveness and Tamoxifen . Microsomal oxidation inhibitors and Cimetidine increase the activity of paroxetine. When used with indirect coagulants or antithrombotic agents, an increase in bleeding is observed.

Terms of sale

On prescription.

Storage conditions

In a dry place, out of the reach of children, protected from light. Permissible temperature is not more than 30 ° Celsius.

Best before date

Keep up to three years.

paxil and alcohol

As a result of clinical studies, data were obtained that the absorption and pharmacokinetics of the active substance - paroxetine does not depend or almost does not depend (that is, dependence does not require dose changes) on and alcohol. It has not been established that paroxetine enhances the negative effect of ethanol on psychomotor , however, it is not recommended to take it with alcohol, since in general alcohol suppresses the effect of the drug - reducing the effectiveness of treatment.

Paxil: instructions for use and reviews

Latin name: Paxil

ATX Code: N06AB05

Active substance: paroxetine (paroxetine)

Manufacturer: GlaxoSmithKline Pharmaceuticals, S.A. (GlaxoSmithKline Pharmaceuticals, S.A.) (Poland); Glaxo Wellcome Production (France); S.C.Europharm S.A. (S.C.Europharm S.A.) (Romania)

Description and photo update: 27.07.2018