What Is Paroxetine HCl?

Paroxetine hydrochloride tablets, the indication is to treat various types of depression, including depression with anxiety and reactive depression. Common symptoms of depression: fatigue, sleep disturbance, lack of interest and pleasure in daily activities, and loss of appetite. Treatment of obsessive-compulsive neurosis. Common obsessive-compulsive symptoms: Feeling repetitive and persistent thoughts, impulses, or imaginations that can cause significant anxiety, leading to repetitive behaviors or mental activities. Treat panic disorder with or without horror in the square. Common panic attacks: palpitations, sweating, shortness of breath, chest pain, nausea, tingling and dying. Treatment of social phobia / social anxiety. Common symptoms of social anxiety: palpitations, sweating, shortness of breath, etc. It usually manifests as a secondary or significant fear of one or more social situations or performances, leading to avoidance. After the treatment is satisfactory, continued taking this product can prevent the recurrence of depression, panic disorder and obsessive-compulsive disorder.

Paroxetine hydrochloride tablets, the indication is to treat various types of depression, including depression with anxiety and reactive depression. Common symptoms of depression: fatigue, sleep disturbance, lack of interest and pleasure in daily activities, and loss of appetite. Treatment of obsessive-compulsive neurosis. Common obsessive-compulsive symptoms: Feeling repetitive and persistent thoughts, impulses, or imaginations that can cause significant anxiety, leading to repetitive behaviors or mental activities. Treat panic disorder with or without horror in the square. Common panic attacks: palpitations, sweating, shortness of breath, chest pain, nausea, tingling and dying. Treatment of social phobia / social anxiety. Common symptoms of social anxiety: palpitations, sweating, shortness of breath, etc. It usually manifests as a secondary or significant fear of one or more social situations or performances, leading to avoidance. After the treatment is satisfactory, continued taking this product can prevent the recurrence of depression, panic disorder and obsessive-compulsive disorder.

Drug Name

Paroxetine Hydrochloride Tablets

Drug type

Prescription medicines, essential medicines, medicines for medical workers' injuries

Use classification

Selective serotonin reuptake inhibitors

Cautions for Paroxetine Hydrochloride Tablets

Suicidal tendencies and antidepressants Depression and certain mental disorders are themselves associated with an increased risk of suicide. Results of short-term clinical trials of depression (MDD) and other mental disorders show that antidepressants increase suicidal tendency (suicidal ideation and suicidal behavior) in children, adolescents, and young people (24 years) compared to placebo risk. Anyone considering paroxetine hydrochloride tablets or other antidepressants for children, adolescents, and young people ( 24 years of age) must weigh their risks with clinical needs. Short-term clinical trials have not shown that the use of antidepressants in adults older than 24 years compared with placebo increases the risk of suicidal tendencies; and among adults aged 65 and older, suicide after using antidepressants The risk of inclination is reduced. It is necessary to closely observe the deterioration of clinical symptoms, suicidal tendency, and abnormal changes in behavior of patients of all ages after the start of antidepressant treatment. Families and caregivers should be advised to observe closely and communicate with the doctor. Paroxetine hydrochloride tablets are not approved for use in pediatric patients (see [Precautions]-Warning, worsening clinical symptoms and risk of suicide).

Paroxetine hydrochloride tablets ingredients

The chemical name of paroxetine hydrochloride is (-)-trans-4- (4-fluorophenyl) -3-{[3,4 (methyldioxy) phenoxy] methyl} piperidine hydrochloride.
Structural formula:

Molecular formula: C ₁₉ H ₂₀ NO ₃ F · HCl
Molecular weight: 365.84

Properties of Paroxetine Hydrochloride Tablets

This product is a white oval, double-sided raised film-coated tablet.

Specifications of Paroxetine Hydrochloride Tablets

20mg per tablet (calculated based on C ₁₉ H ₂₀ FNO ₃ )

Paroxetine hydrochloride tablets dosage

Take it orally, it is recommended to take it daily at breakfast, swallow the tablets intact and do not chew.
adult:
Depression:
The usual dose is 20 mg daily. After taking 2-3 weeks, according to the response of some patients, some patients need to increase the amount by 10mg per week. According to foreign experience, the maximum daily amount can reach 50mg, which should be prescribed by your doctor.
Obsessive-compulsive neurosis:
The general dose is 40 mg daily, the initial dose is 20 mg daily, and it is increased by 10 mg every week. According to foreign experience, the maximum daily dose can reach 60mg.
Panic disorder:
The general dose is 40mg daily, and the initial dose is 10mg daily. According to the patient's response, it is increased by 10mg every week, and the maximum daily dose can reach 50mg. It is generally believed that the symptoms may be aggravated early in the treatment of panic disorder, so the initial dose is 10 mg.
Social phobia / social anxiety:
The general dose is 20mg per day. If the patient does not respond to 20mg, it can be increased by 10mg per week according to the clinical response of the patient. According to foreign experience, the maximum daily dose can reach 50mg. The dose was changed for at least one week.
As with all antidepressants, the dose should be adjusted according to the condition during treatment. Patients should be treated long enough to consolidate the effect. Maintenance treatment should be maintained for at least several months after the depression is cured. Obsessive-compulsive neurosis and panic disorder require longer maintenance treatment. The withdrawal method is similar to other psychiatric drugs, and it needs to be gradually reduced, and it is not appropriate to stop suddenly.
Discontinuation of Paroxetine <br /> Like other psychotropic drugs, this product should not be discontinued suddenly (see the [Precautions] and [Adverse Effects] section). In the recent clinical trials, the gradual dose withdrawal plan is to gradually reduce the dose at weekly intervals. The daily dose per week is reduced by 10 mg compared to the daily dose last week, and the dose is reduced once a week.
When the daily dose was reduced to 20 mg daily, the patient continued to take the medicine for 1 week at that dose, and then discontinued the medicine. If symptoms of intolerance occur after reduction or discontinuation, consider returning to the previous dose. The doctor can then proceed with the reduction program, but the rate of reduction is slower.
Renal / liver damage:
Due to severe renal impairment (creatinine clearance [30ml / min) or severe liver impairment, the blood concentration of this product is higher than that of healthy people. Therefore, the recommended dose is 20 mg daily, and if the dose needs to be increased, it should also be limited to the lower limit of the medication range.

Adverse reactions of paroxetine hydrochloride tablets

Some of the adverse reactions listed below may be alleviated or reduced over time, and generally do not lead to discontinuation. The adverse drug reactions of each organ system are listed below. The incidence is defined as: very common (1 / 10), common (1 / 100, <1/10), uncommon (1 / 1,000, <1/100), rare (1 / 10,000, < 1 / 1,000), very rare (<1 / 10,000), including individual reports. The incidence of common and infrequent events is generally judged on the safety profile of patients in the paroxetine-treated group (> 8000) in clinical trials, and generally refers to an additional increased incidence compared to placebo. Rare and very rare events are generally judged based on post-marketing information and refer to reporting rates rather than true rates.
Blood and lymphatic system < br Uncommon: abnormal bleeding, mainly seen in the skin and mucous membranes (mostly ecchymosis), anemia, leukopenia, lymphadenopathy, purpura.
Rare: abnormal red blood cells, increased basophils, prolonged bleeding time, excessive eosinophils, hypochromic anemia, iron deficiency anemia, leukocytosis. Lymphedema, abnormal lymphocytes, lymphocytosis, small cell anemia, increased mononuclear cells, normal red blood cell anemia, thrombocytosis, and thrombocytopenia.
Immune system br Uncommon: Allergic reactions (including urticaria and angioedema).
Endocrine system < br rare; diabetes, goiter, hyperthyroidism, hypothyroidism, thyroiditis;
Very rare: syndrome of abnormal antidiuretic hormone secretion (SIADH).
Metabolism and Nutrition Common: Increased cholesterol levels, decreased appetite, and weight gain.
Uncommon: Puffiness. Peripheral edema, elevated SGOT, elevated SGPT, thirst, weight loss;
Rare: elevated alkaline phosphatase, bilirubinemia, elevated BUN, elevated creatinine phosphate kinase, dehydration, elevated Y-globulin, gout, hypercalcemia, hypercholesterolemia, hyperglycemia, high Kalemia, hyperphosphatemia, hypocalcemia, hypoglycemia, hypokalemia, hyponatremia, ketosis, elevated lactate dehydrogenase, and elevated non-protein nitrogen (NPN).
The reported hyponatremia is mainly seen in elderly patients and is sometimes caused by the antidiuretic hormone secretion syndrome (SIADH).
Mental disorders < br Common: drowsiness, insomnia and excitement, abnormal dreams (including nightmares).
Uncommon: blurred consciousness, hallucinations.
Rare: manic response.
These symptoms may be caused by underlying diseases.
Nervous system Common: dizziness, tremor, headache, emotional instability.
Uncommon: extrapyramidal symptoms, abnormal thinking, alcoholism, ataxia, dystonia, dyskinesia, euphoria, hostility, hallucinations, hypertonia, dullness, impaired motor function, inability to coordinate, apathy, increased libido, Manic response, neurosis, paralysis, paranoia.
Rare: convulsions, inability to sit still, restless leg syndrome, abnormal gait, inability to exercise, social disgust, aphasia, choreographer, dyskinesia, delirium, delusion, diplopia, drug dependence, dysphonia , Muscle tremor, epilepsy, convulsions, hyperalgesia, hysterics, manic-depressive reaction, meningitis, myelitis, neuralgia, neuropathy, nystagmus, peripheral neuritis, psychotic depression, psychosis, Reduced reflexes, enhanced reflexes, stiffness, torticollis, closed teeth, withdrawal syndrome.
Very rare: Serotonin syndrome (symptoms may include excitement, confusion, sweating, hallucinations, hyperreflexia, myoclonus, tremor tachycardia, and tremor).
Some patients report extrapyramidal symptoms, including abnormalities in the orofacial muscle tone. These patients are sometimes accompanied by basic dyskinesias or are using neuroleptic drugs.
Eye < br Common: blurred vision.
Uncommon: Dilated pupils (see [Notes]).
Very rare: acute glaucoma.
Cardiovascular system < br Common: hypertension, tachycardia.
Uncommon: sinus tachycardia, orthostatic hypotension, bradycardia, hematoma, hypotension, migraine, orthostatic hypotension,
Syncope:
Rare: Angina pectoris, nodular arrhythmia, atrial fibrillation, bundle branch block, cerebral ischemia, cerebrovascular accident, congestive heart failure, cardiac block, low cardiac output, myocardial infarction, myocardial ischemia, pale , Phlebitis, pulmonary embolism, supraventricular premature contraction, thrombophlebitis, thrombosis, varicose veins, vascular headache, ventricular premature contraction.
Respiratory system, chest, and mediastinum Common: Yawning.
Uncommon: asthma, bronchitis, dyspnea, nosebleeds, hyperventilation, pneumonia, respiratory flu.
Rare: emphysema, hemoptysis, snoring, pulmonary fibrosis, pulmonary edema. Increased sputum volume, wheezing and altered speech.
Digestive system is very common: nausea.
Common: constipation, diarrhea, vomiting, dry mouth.
Uncommon: bruxism, colitis, difficulty swallowing, belching, gastritis, gastroenteritis, gingivitis, glossitis, salivation, abnormal liver function, rectal bleeding, ulcerative stomatitis.
Rare: aphthous stomatitis, bloody diarrhea, excessive appetite, cardiac spasm, gallstone disease, duodenitis, enteritis, esophagitis, fecal impaction, fecal incontinence, bleeding gums, vomiting, hepatitis, ileitis, intestinal obstruction, Intestinal obstruction, jaundice, black faeces, oral ulcers, peptic ulcers, enlarged salivary glands, salivary glands, gastric ulcers, stomatitis, discoloration of the tongue, swelling of the tongue, caries.
Very rare: gastrointestinal bleeding.
Hepatobiliary system br rare: elevated liver transaminase.
Very rare: liver events (such as hepatitis, sometimes with jaundice and / or liver failure).
Elevated liver transaminase has been reported. Post-marketing reports of liver events (eg, hepatitis, sometimes with jaundice, and / or liver failure) have also been received, and these reports are rare. If liver function tests continue to increase, paroxetine should be discontinued.
Skin and subcutaneous tissues are common: sweating, itching.
Uncommon: rash, acne, hair loss, contact dermatitis, dry skin, bleeding spots, eczema, herpes simplex, light sensitivity, urticaria.
Rare: angioedema, nodular erythema, erythema polymorpha, exfoliative dermatitis, mycotic dermatitis, rickets, shingles, hirsutism, maculopapular rash, seborrhea, skin discoloration, skin hypertrophy, skin ulcers, sweating Reduces and blistering herpes.
Very rare: photosensitivity.
Kidney and genitourinary system < br is very common: sexual dysfunction.
Uncommon: urinary retention, urinary incontinence, amenorrhea, breast pain, cystitis, dysuria, hematuria, excessive menstruation, nocturia, polyuria, pyuria, urgency, vaginitis.
Rare: hyperprolactinemia / galactorrhea, abortion, breast atrophy, breast enlargement, endometrial disease, epididymitis, fibrocystic mastopathy, kidney stones, kidney pain, leucorrhea, mastitis, irregular bleeding, Nephritis, oliguria, salpingitis, urethritis, cast urine, uterine spasm, urinary stones, vaginal bleeding, and vaginal candidiasis.
Systemic and administration site reactions < br Common: weakness, weight gain.
Uncommon: chills, facial swelling, general weakness, and neck pain.
Rare: adrenergic syndrome, cellulitis, candidiasis, stiff neck, pelvic pain, peritonitis, sepsis and ulcers.
Very rare: peripheral edema.
Musculoskeletal system:
Common: Arthralgia.
Uncommon: arthritis, joint disease.
Rare: Bursitis, myositis, osteoporosis, generalized convulsions, tenosynovitis, hand and foot convulsions.
Peculiar feeling:
Common: Tinnitus.
Uncommon: maladjustment, conjunctivitis, ear pain, eye pain, keratoconjunctivitis, dilated pupils, otitis media.
Rare: amblyopia, varying pupil size, blepharositis, cataracts, conjunctival edema, corneal ulcers, deafness, exophthalmos, hemorrhage, glaucoma, auditory allergies, night blindness, external ear inflammation, olfactory insomnia, photophobia, ptosis Bleeding, loss of taste, and loss of vision.
Symptoms of discontinuation of paroxetine <br Common: Dizziness, sensory disturbance, sleep disturbance, anxiety, headache.
Uncommon: Excitement, nausea, tremor, confusion, sweating, diarrhea.
As with many other psychotropic drugs, discontinuation of this product (especially when abruptly discontinued) may cause dizziness, sensory disturbances (including paraesthesia, electrical shock sensation, and tinnitus), sleep disturbances (including intense dreaming), excitement or anxiety , Nausea, headache, tremor, confusion, diarrhea and sweating. In most patients, these events are mild to moderate and self-limiting. No group of patients was found to be at a higher risk of these symptoms, so it is recommended that if the paroxetine treatment is no longer needed, the drug should be gradually reduced (see [Dosage and Administration] and [Cautions]).
Adverse events in clinical studies in children:
In children's clinical studies, at least 2% of patients reported the following adverse events, which occurred at least twice as often as placebo: emotional instability (including self-harm, suicidal thoughts, suicide attempts, crying, and mood swings) , Hostility, loss of appetite, tremor, sweating, cramps, and agitation. Suicidal thoughts and suicidal tendencies are mainly seen in clinical trials in adolescents with major depression. Hostility is more common in children with obsessive-compulsive neurosis, especially children under 12 years of age.
In the trial, a gradual dose reduction regimen was used (increased daily by 10 mg daily to 10 mg daily and continued to be discontinued after one week). During gradual reduction or discontinuation, at least 2% of patients reported the following adverse reactions, which occurred at least twice as often as placebo: emotional instability, nervousness, dizziness, nausea, and abdominal pain (see [Note matter).
Post-marketing report: Since the market launch of the drug, spontaneous reports of adverse events in patients taking this product have been received. Adverse events not listed above that may not be causally related to the drug include. Acute pancreatitis, elevated liver function tests (the most severe cases are deaths due to liver necrosis, and a significant increase in transaminase associated with severe liver dysfunction). Gurbacher syndrome, toxic epidermal necrosis and slackness, abnormal penile erection. Syndrome of abnormal antidiuretic hormone secretion, symptoms of prolactinemia, galactorrhea. Nerve blocker malignant syndrome-like event, serotonin syndrome. Extrapyramidal symptoms include inability to sit still, bradykinesia, gear-like rigidity, dystonia, hypertonia, and oculomotor nerve crisis related to the combined use of piperidine. Shivering and clenching. Status epilepticus, acute renal failure, pulmonary hypertension. Allergic alveolitis, allergic reactions, eclampsia, laryngospasm, optic neuritis, porphyria, ventricular fibrillation, ventricular tachycardia (including apical torsional ventricular tachycardia), thrombocytopenia, hemolytic anemia , Hematopoietic dysfunction adverse events (including aplastic anemia, pancytopenia, bone marrow dysplasia, and agranulocytosis) and vasculitis syndrome (such as allergic purpura). After taking this product and phenytoin simultaneously for 4 weeks, I received a report of an increase in phenytoin blood concentration. There was also a report of severe hypotension after the addition of this product in the long-term treatment of metoprolol.

Contraindications of paroxetine hydrochloride tablets

Those who are known to be allergic to this product and its excipients are contraindicated.
This product cannot be used in combination with monoamine oxidase inhibitors (including the antibiotics linezolid, a reversible, non-selective monoamine button enzyme inhibitor) or within two weeks after the end of treatment with a monoamine oxidase inhibitor. Similarly, do not use monoamine oxidase inhibitors for two weeks after the treatment with this product (see [Drug Interactions] for details).
This product cannot be combined with methiopyrazine. Because it is the same as other drugs that inhibit liver cytochrome P450 isoenzyme CYP450 2D6.
This product can cause an increase in the plasma concentration of methiopyrazine (see [Drug Interactions]). Methidazine alone can lead to prolonged QTc interval. And accompanied by severe ventricular arrhythmias. For example, electrocardiograms show spike-tip phenomena (peak crests) and sudden death.
This product should not be used in combination with pimozide (see [Drug Interactions]).

Precautions for paroxetine hydrochloride tablets

Warn of clinical deterioration and suicide risk:
Adults or children with major depression (MDD), whether or not they take antidepressants. Both may have worsening symptoms of depression and / or suicidal ideation and suicidal behavior (suicidal tendency). This danger persists during illness. Until the disease is significantly relieved. Suicide is a known risk of depression and some other mental illnesses that are themselves the strongest predictors of suicide. It has long been thought that the early stage of antidepressant treatment can induce some patients to worsen their disease and appear suicidal. Short-term antidepressants (SSRls and others). A comprehensive analysis of placebo-controlled clinical trial data shows that in children. In adolescents and young patients (age 18-24), these drugs increase suicidal ideation and suicidal behavior (suicidal tendency) in patients with major depression and other mental illnesses. Short-term clinical trials of antidepressants show. Compared with placebo. The risk of suicide did not increase in adult patients over 24 years of age, but it decreased in the interest of adults over 65 years of age.
In children and adolescents with major depression, obsessive-compulsive disorder, or other mental illness. Comprehensive analysis of placebo-controlled clinical trials. Includes 9 antidepressants. 24 short-term clinical trials in 4,400 patients. In adults with major depression or other psychiatric disorders, a comprehensive analysis of placebo-controlled clinical trials included 11 antidepressants. 295 short-term clinical trials (median duration 2 months) in more than 77,000 patients. Suicide risk differs between different drugs, but the suicide risk of younger patients in almost all trial drugs tends to increase; the absolute suicide risk among different indications is also different, with the incidence of major depression highest. The risk stratification between age stratification and indications (drug and placebo) is relatively stable. These differences are detailed in Table 1 (drug-placebo differences in suicides per 1,000 treated patients).

In any child-related clinical trial. No suicide has occurred, and suicide has occurred in adult clinical trials. But these data are not enough to evaluate the effect of the drug on suicide.
It is not known when the drug is used for a longer period of time (such as more than several months). Whether suicide risk is increased, but data from clinical trials of placebo-controlled maintenance treatments in adults with depression suggest that the use of antidepressants can delay the relapse of depression.
All patients receiving antidepressant medication should be properly monitored to closely observe any deterioration in their condition, suicidal tendency, and abnormal behavior changes, especially during the first few months of the course of treatment, or when changing the dosage (Increase or decrease the dose).

In adults and children treated with antidepressants for major depression and other indications, whether or not they are mentally ill. Subjects have reported the following symptoms: anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsiveness, inability to sit still (difficult meditation), mild mania, mania. Although the causal relationship between these symptoms and clinically worsening depression and / or suicidal risk has not been proven. But these symptoms may be a precursor to suicide.
If the patient's depression continues to worsen, suicidal thoughts / behavior, signs of exacerbation of depression, or signs of suicide appear, especially if these symptoms are severe, sudden, or new. Consideration should be given to changing treatment options, including the possibility of stopping medication.
If you decide to discontinue treatment, the product should be gradually reduced as quickly as possible due to the risk of discontinuation of the product. Pay attention to the sudden occurrence of certain symptoms ( see [Precautions] and [Dosage and Administration]).
In the course of receiving antidepressant medication for major depression or other indications (whether it is a mental illness or not), family members or caregivers should be warned to closely monitor the patient's excitement, irritability, abnormal behavior changes, or other symptoms mentioned above , And suicidal tendencies, etc., should report these symptoms to medical personnel or medical institutions in a timely manner. Family members or caregivers are monitored daily.
In order to reduce the risk of overdose, the minimum dosage tablet should be selected when formulating this product, and it should be matched with good patient management measures.
Screening for patients with bipolar disorder: Major depressive episodes may be the initial manifestation of bipolar disorder, and it is generally believed (though not yet confirmed by controlled clinical trials) that antidepressants are used alone in patients at risk for bipolar disorder. Treating a major depressive episode may increase its likelihood of exacerbating mixed / manic episodes. It is unclear whether the above symptoms will also occur in this way. Before starting antidepressant treatment, patients should be adequately screened to determine whether they are at risk for bipolar disorder: this screening should include a detailed history of mental illness, as well as suicide, bipolar disorder, and depression Family history of the disease. It should be noted that this product has not been approved for the treatment of bipolar disorder.
Possible interactions with monoamine oxidase inhibitors. In patients receiving a serotonin reuptake inhibitor. When combined with monoamine oxidase inhibitors (MAOI), serious and even fatal reactions have been reported. These reactions include fever, stiffness, myoclonus, and autonomic instability with rapid fluctuations in vital signs. Changes in mental state (including development of extreme excitement to delirium and coma). These reactions have also been reported in patients who recently discontinued such drugs and started a monoamine oxidation inhibitor. Some cases are characterized by malignant syndrome similar to neuroblockers. There are no human test data on the interaction of monoamine oxidase inhibitors with this product. Limited animal experimental data suggest that paroxetine is used in combination with monoamine chloride inhibitors. Can play a synergistic role in raising blood pressure and inducing behavioral excitement. Therefore, this product is not recommended for combination with monoamine oxidase inhibitors (including the antibiotic drug linezolid. A reversible, non-selective monoamine oxidase inhibitor), nor is it recommended to use this product within two weeks after discontinuing the monoamine oxidase inhibitor (see [ Taboo]). Monoamine oxidase inhibitors should not be used until this product has been discontinued for at least two weeks.
Serotonin syndrome: in patients treated with SNRls and SSRls (including this product). Life-threatening serotonin syndrome may occur, especially when combined with serotoninergic drugs (including amitriptyline) and drugs that affect serotonin metabolism (including monoamine oxidase inhibitors) are more prone to serotonin synthesis Signs include changes in mental state (such as excitement, hallucinations, coma). Autonomic nervous instability (such as tachycardia, unstable blood pressure, high fever), neuromuscular abnormalities (such as hyperreflexia, ataxia), and / or gastrointestinal symptoms (such as nausea, vomiting, diarrhea).
Contraindications: This product is used in combination with monoamine oxidase inhibitors to treat depression (see [Precautions]).
When this product is combined with a serotonin receptor agonist (amitriptyline), it is necessary to carefully and closely monitor the clinical condition, especially at the beginning of treatment and when increasing the dose (see [Precautions]).
This product is not recommended for combination with serotonin precursor substances (such as tryptophan) (see [Precautions]).
Possible interaction with methiopyrazine: Methiopyrazine alone can prolong the QTc interval. Severe ventricular arrhythmias appear. Such as tip torsional ventricular tachycardia and sudden death. This effect seems to be dose related.
An in vivo test showed. Drugs that inhibit CYP2D6 (such as paroxetine) can increase plasma levels of methiopyrazine, so the combination of paroxetine and methiopyrazine is not recommended (see [Contraindications] and [Cautions]).
Pregnancy medication:
Teratogenic effects: Epidemiological investigations have shown that in infants born to mothers exposed to antidepressants in the first trimester of pregnancy, there is an increased risk of congenital malformations (such as ventricular septal defects (VSDs) and Septal defects (ASDs)), usually, the severity of septal defect lesions. From a symptomatic lesion requiring surgery, to asymptomatic or natural healing. For women who are pregnant during taking paroxetine, the harm that the drug may cause to the fetus should be considered. Only continue to use paroxetine if the benefits of paroxetine treatment outweigh the potential risks. Otherwise, paroxetine should be discontinued and other antidepressants should be selected. Drugs (see [Precautions]). For women planning a pregnancy or in the first trimester of pregnancy, paroxetine should not be started until other available treatment options have been considered.
A clinical trial based on Swedish national registry data evaluated 6,896 infants who were exposed to antidepressants during early pregnancy (5,123 women were exposed to SSRls, of which 815 were exposed to paroxetine) and all registered Compared with the registered population, the risk of cardiovascular malformations (mainly VSDs and ASDs) was increased in infants exposed to paroxetine in early pregnancy (OR 1.8; 95% confidence interval: 1.1-2.8). The proportion of cardiovascular malformations in infants exposed to paroxetine in the first trimester is 2%. The proportion of cardiovascular malformations in all registered population was 1%. In these infants exposed to paroxetine, the overall risk of congenital malformations did not increase.
In a separate retrospective cohort study. 5,956 infants were evaluated using data from the National Institutes of Health. The mother of the infant had used paroxetine or other antidepressants during the first trimester of pregnancy (n = 815 in paroxetine patients). Studies have shown that compared with other antidepressants. Paroxetine has a tendency to increase the risk of cardiovascular malformations (OR 1.5, 95% confidence interval: 0.8-2.9). When using paroxetine and other antidepressants within 3 months of pregnancy. The incidence of cardiovascular malformations was 1.5% and 1%, respectively. Among the 12 infants with cardiovascular malformations who took paroxetine in the first three months of pregnancy, the mother had taken it. There are 9 patients with VSDs. This study also suggests a comparison with other antidepressants. Paroxetine increases the overall risk of major congenital malformations (including cardiovascular defects) (OR: 1.81 95% confidence interval: 1.2 -2.8). In infants who used paroxetine 3 months before the mother's pregnancy. The incidence of all congenital malformations was 4%. In infants who have used other antidepressants within 3 months of pregnancy. The incidence of all congenital malformations was 2%.
Animal test: During the organogenesis period, paroxetine was given to rats at a dose of 50 mg / kg / day or rabbit at 6 mg / kg / day. These doses are 8 times (rat) and 2 times (rabbit) the maximum human recommended dose (MRHD). No teratogenic effect was found in the test. But when administered in the last three months of pregnancy to lactation. The number of deaths of pups increased 4 days before lactation. When the dose is 1 mg / kg / day or 1 mg / m2, which is close to 1/6 of the maximum recommended human dose (MRHD). This effect can also occur. No invalid dose was determined for one pup death. The cause of death of the pups is also unclear.
Non- teratogenic effects: Newborns exposed to this product and other SSRls, or 5-hydroxytryptamine · norepinephrine reuptake inhibitors (SNRls) within three months of the last trimester. You will need to extend your hospital stay due to complications. Prolong the duration of respiratory support and tube feeding. These complications can occur quickly after birth. Clinical findings in previous reports include respiratory distress, cyanosis, apnea, and seizures. Body temperature fluctuations. Difficult feeding. Vomiting, hypoglycemia. Hypotonia. Hypertonia, hyperreflexia, tremor. trembling. Irritable and keep crying. These characteristics are consistent with the direct toxic effects of SSRls and SNRls. Or may be consistent with a drug withdrawal syndrome. have to be aware of is. In some cases, the clinical manifestations are consistent with serotonin syndrome (see [Notes]).
Newborns exposed to SSRls in late pregnancy. Increased risk of developing persistent pulmonary hypertension (PPHN) in newborns. In the general population, 1-2 cases of PPHN can occur per 1,000 live births. It is also associated with neonatal morbidity and mortality. In a retrospective case-control clinical trial. There were 377 babies born to women who had PPHN at birth. The 836 babies born to women were healthy at birth. Compared with infants who were not exposed to antidepressants during pregnancy. The risk of PPHN in infants exposed to SSRls after the 20th week of pregnancy is almost 6 times higher. There is currently no conclusive evidence that exposure to SSRls during pregnancy is at risk for PPHN. This trial is the first study of this potential risk. In this test. The number of included cases exposed to a single species of SSRls was insufficient. Therefore, it is impossible to determine whether SSRls all have the same PPHN risk level. There are also post-marketing reports of preterm births in pregnant patients exposed to paroxetine or other SSRls. When applied paroxetine in late pregnancy. Physicians should carefully consider potential risks and treatment benefits. The physician should also note. In a prospective longitudinal study. 201 women with a history of major depression had normal mood during early pregnancy. But during pregnancy. Compared with pregnant women who continue with antidepressant treatment. Women who have discontinued antidepressants are more likely to have relapses or worsen their condition.
Mania and bipolar disorder <br /> Major depressive episodes may be the first manifestations of bipolar disorder. It is generally accepted (though not confirmed by controlled trials) that the treatment of such major depressive episodes with antidepressants alone may increase the likelihood of exacerbation of mixed / manic episodes in patients at risk for bipolar disorder. Before starting treatment with antidepressants. Patients should be fully screened. Determine if they are at risk for bipolar disorder. This screening should include a detailed history of mental illness. Including suicide. Family history of bipolar disorder and depression. It should be noted that this product is not approved for the treatment of bipolar disorder. Like all antidepressants, this product should be used with caution in patients with a history of mania,
Fractures: Epidemiological studies on the risk of fractures with antidepressants including SSRls have shown a certain correlation with fractures. This risk occurs during treatment and is greatest early in the treatment. Fractures are thought to occur in patients taking this product.
Meditation cannot: in rare cases. Use of this product or other SSRls may result in meditation. It is characterized by irritable inner feelings and psychomotor excitement. For example, often because of conscious distress. Do not sit or stand quietly. This situation is most likely to occur within the first few weeks of treatment.
Serotonin Syndrome / Antipsychotic Malignant Syndrome < br In rare cases, paroxetine treatment may cause serotonin syndrome or antipsychotic malignant syndrome-like events. Especially when combined with other serotonergic drugs and / or antipsychotics. Because these syndromes can cause potentially fatal problems. So if these events occur (characterized by a combination of symptoms such as high fever, tonicity, myoclonus, autonomic nerve instability, there may be rapid fluctuations in vital signs, changes in mental state, including blurred consciousness, irritability, extreme excitement, progress To delirium and coma). This product should be discontinued and supportive symptomatic treatment should be taken. Paroxetine cannot be used in combination with serotonin precursor substances (such as L-tryptophan, hydroxytryptamine), because the combination of the two is at risk for serotonin syndrome (see [Contraindications] and [Drug Interactions]).
Heart < br Using this product in patients with heart disease should usually be observed.
Epilepsy is the same as other psychiatric drugs. Use with caution in patients with epilepsy.
Seizures <br /> Generally. The incidence of seizures during treatment with this product [0.1%. Patients with seizures should stop taking the medication.
Glaucoma < br Compared with other selective 5-HT reuptake inhibitors (SSRls), this product may cause pupil dilation, and patients with glaucoma with narrowed angles should be used with caution.
Children and adolescents (under 18 years of age)
In children and adolescents with major depressive disorder and other mental illnesses, an increased risk of suicidal ideation and behavior is associated with treatment with antidepressants. In children and adolescent clinical trials of this product. Compared with placebo. Adverse events related to signs of suicide (suicide attempts and suicidal thoughts) and hostility (mainly manifested as aggressiveness, confrontational behavior and anger) were more common in paroxetine-treated patients (see [Adverse Reactions]). There is still a lack of growth for children and adolescents. Long-term safety data on maturity, cognitive and behavioral development.
Adults' clinical condition worsens and suicide risk. <br /> Young adults. Especially young adults with major depressive disorder. During treatment with paroxetine. May increase the risk of suicide. An analysis of adults with mental illness and a placebo-controlled trial showed that young adults (predefined age range 18 to 24 years) treated with paroxetine were more likely to commit suicide than placebo (17 / 776 [2.19%] than 5/542 [0.92%]). Although this difference is not statistically significant. In older age groups (25-64 years old and 65 years or older). No such increase was observed. Adults (all ages) with major depressive disorder are treated with paroxetine. Compared with placebo, the increase in suicidal behavior was statistically significant (118455 [0.32%] than 1/1978 [0.05%] l All events were suicide attempts). However, most of the (8/11) suicide attempts due to paroxetine occurred among young adults aged 18-30. These data on major depressive disorder suggest that the higher suicide rates observed in young adult populations with mental illness may be extended to those over 24 years of age.
Patients with depression, whether or not they take antidepressants. Depression may worsen. And / or suicidal ideation and suicidal behavior (signs of suicide). This danger persists until the condition is significantly relieved. The risk of suicide may increase during the early stages of recovery. This is common clinical experience with all antidepressant medications. Other mental illnesses treated with paroxetine may also increase the risk of suicidal behavior. and. These conditions may also be combined with major depressive disorder. In addition, patients with a history of suicidal behavior or suicidal thoughts. Younger adults and patients who show significant suicidal thoughts before starting treatment are at higher risk for suicidal thoughts or attempts. All patients should be monitored throughout the treatment period for clinical deterioration (including the appearance of new symptoms) and signs of suicide. Especially at the beginning of the course. Or when changing the dosage (increase or decrease). Patients (and their caregivers) should be warned. Pay attention to monitoring the deterioration of the condition (including the emergence of new symptoms) and / or the occurrence of suicidal thoughts / behaviors or self-harm thoughts. Once these symptoms appear. Seek medical advice immediately. You should be aware that the appearance of some symptoms (such as excitement. Meditation or mania) may be related to the underlying disease state or medication (see meditation inability. Mania and bipolar disorder. Adverse reactions).
If the patient has clinical deterioration (including new symptoms). And / or suicidal ideation / behavior, especially those with severe, sudden or emerging symptoms. Consideration should be given to changing treatment options. Includes possible discontinuation of medication.
Electric shock therapy (ECT)
There is currently no clinical experience regarding the combination of this product and electrical shock. however. Rarely, patients who are taking SSRls may report prolonged ECT-induced seizures and / or secondary seizures.
Hyponatremia < br Rarely, hyponatremia has been reported and occurs mainly in elderly patients. Hyponatremia symptoms can usually be reversed after discontinuation.
Signs and symptoms of hyponatremia include headaches, inattention, memory impairments, blurred consciousness, weakness, and unstable standing may cause a fall. In severe or acute cases, signs and symptoms also include hallucinations, syncope, seizures, and coma. Stop breathing and die.
Bleeding < br After taking this product. There have been reports of skin and mucosal bleeding (including gastrointestinal bleeding), so caution should be taken with drugs that increase the risk of bleeding. Patients with known and likely bleeding tendency should use this product.
Monoamine oxidase inhibitors < br After monoamine oxidase (MAO) inhibitor treatment is stopped for at least 2 weeks. Before you begin to use paroxetine with caution. And the dosage of this product should be gradually increased. Until the desired effect is achieved (see [Contraindications] and [Drug Interactions]).
Renal damage / liver damage Patients with severe renal impairment or liver impairment should be used with caution (see [Dosage and Administration]).
Driving / Manipulating Machines < br Clinical experience proves. After taking this product. No effect on cognitive or psychomotor function. However, like all psychoactive drugs. Patients taking medication while driving or operating machinery. Be careful.
Symptoms of discontinuation of paroxetine treatment in adults <br /> clinical trials in adults. Adverse events occurred in 30% of patients treated with paroxetine when discontinued. 20% of patients in the placebo group had adverse events. Symptoms of withdrawal are different from symptoms of drug addiction or dependence caused by substance abuse. dizziness.12(2-3)
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1. Clinical studies have shown that the absorption and pharmacokinetics of paroxetine are not affected by the following factors or have only insignificant effects (that is, such effects are small and do not require changes to the dosing regimen):
Food antacid digoxin propranolol 2. Serotonergic drugs, like other selective 5-HT reuptake inhibitors (SSRIs), are the same as serotonergic drugs (including monoamine oxidase inhibitors, L-tryptophan, triptans, tramadol, linezolid) , SSRIs, lithium and St. John's Wort-St. John's Wort-Forsythia-preparations may cause 5-HT related effects (serotonin syndrome: see [taboo] and [notes].
When these drugs are used in combination with this product, care must be taken and clinical conditions need to be closely monitored.
3 Drug Metabolizing Enzymes: Inducers or inhibitors of drug metabolizing enzymes can affect the metabolism and pharmacokinetics of this product. When this product is used in combination with known drug metabolizing enzyme inhibitors, the lower limit of the dosage range should be considered. When this product is used in combination with known drug metabolizing enzyme inducers (such as carbamazepine, rifampicin, phenobarbital, and phenytoin), there is no need to consider adjusting the initial dose. Subsequent dose adjustments will depend on clinical response (response and tolerability).
Fosamprenavir / ritonavir: When used in combination with Fosamprenavir / ritonavir, it significantly reduces the plasma concentration of paroxetine. Any dose adjustment should be made based on clinical effects (tolerability and effectiveness).
4 Alcohol: Paroxetine does not increase alcohol and cause mental and motor dysfunction, but this product is not recommended for use with alcohol.
5. As with most antidepressants, this product cannot be used in combination with monoamine oxidase inhibitors. Do not use monoamine oxidase inhibitors for two weeks before or after taking this product. Caution should be taken when taking this product two weeks after discontinuing a monoamine oxidase inhibitor, and the dose should be gradually increased.
6. Anticonvulsants: carbamazepine, phenytoin, sodium valproate. The combination of these drugs seems to have little effect on the pharmacokinetic / pharmacodynamic characteristics in patients with epilepsy.
7. Paroxetine inhibits CYP2D6 like other antidepressants (including other SSRIs). Paroxetine inhibits liver cytochrome P450 enzyme CYP2D6. Inhibition of CYP2D6 may lead to increased plasma concentrations of the combined drugs metabolized by this enzyme. These include certain tricyclic antidepressants (eg, amitriptyline, nortriptyline, imipramine, and desipramine), phenothiazine neuroleptics (eg, perphenazine, and thiram Dazine, see [Contraindications], Risperidone, Atoxetine, certain antiarrhythmics of type 1c (eg, propafenone and flukanib), and metoprolol.
CYP3A4
In vivo interaction studies of paroxetine and cytochrome CYP3A4 substrate terfenadine under steady state conditions have shown that paroxetine has no effect on the pharmacokinetics of terfenadine. Similar in vivo interaction studies have found that paroxetine has no effect on the pharmacokinetics of alprazolam, and alprazolam has no effect on the pharmacokinetics of paroxetine. Paroxetine is not harmful in combination with terfenadine, alprazolam, and other drugs as substrates for CYP3A4.
8. Procycladine: Daily administration of paroxetine will significantly increase the plasma concentration of procycladine. If anticholinergic effects are found, the dose of procycladine should be reduced.
9. Pimozide
A single low-dose (2 mg) combination of piperidine and paroxetine showed elevated levels of piperidine. However, the mechanism of interaction between piperidine and paroxetine is unknown, and combined use of piperidine and this product is strictly forbidden due to the narrow indications of piperidine treatment and its known QT interval extension (see [Contraindications]).
10 Tricyclic antidepressants (TCAs)
Because paroxetine can inhibit TCA metabolism, it should be used with tricyclic antidepressants (TCAs) with caution. To reduce the TCA dose when TCA is used in combination with this product, it is necessary to monitor the plasma TCA concentration.
11. Drugs that are highly bound to plasma proteins: Because paroxetine is highly bound to plasma proteins. Patients taking another drug that is highly bound to protein when using this product. The free concentration of other drugs will increase. It may lead to adverse events. In contrast, paroxetine, which is replaced by other proteins that are highly bound to the drug, can also cause adverse reactions.
12. Drugs that affect hemostasis (eg NSAIDs. Aspirin and Warfarin). Platelet release 5. Serotonin plays an important role in hemostasis. Case-control and cohort analysis epidemiological studies have demonstrated that the use of antipsychotic drugs that interfere with serotonin reuptake is associated with upper gastrointestinal bleeding. It has also been shown that combined use of NSAID or aspirin increases the risk of bleeding. When SSRls or SNRls are combined with warfarin. Changes in anticoagulation, including increased bleeding. Patients receiving warfarin when starting or stopping paroxetine. All need to closely observe the patient's condition.

Paroxetine hydrochloride tablets overdose

Existing information shows that this product has a large safety range. There have been reports of overdose of this product at a single dose of 2000 mg or in combination with other drugs (including alcohol). Experience after overdose of this product shows that in addition to those mentioned in the adverse reactions section, nausea, vomiting, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contraction, agitation, anxiety and tachycardia have been reported. Occasional incidents of coma or ECG changes are reported, but are rarely life-threatening, and most often occur in combination with other psychiatric drugs (with or without alcohol).
There is no special antidote, and it can be treated according to the conventional method of overdose of other antidepressants. Patients can be treated according to clinically applicable methods or recommended by the National Poison Control Center.

Pharmacology and toxicology of paroxetine hydrochloride tablets

Pharmacological effects < br Paroxetine hydrochloride is an antidepressant and a potent, highly selective 5-HT reuptake inhibitor. It can increase the concentration of 5-HT in synaptic cleft. Enhance central serotonergic nerve function. Only slightly inhibits the reuptake of norepinephrine and dopamine. Almost no compared with muscarinic receptors or 1, 2, -adrenergic receptors, dopamine receptors (D ₂ ), 5-HT ₁ receptors, 5-HT ₂ receptors and histamine (H ₁ ) receptors Affinity. No inhibitory effect on monoamine oxidase.
Toxicological studies for genotoxicity:
Paroxetine Ames test, mouse lymphoma test, off-program DNA synthesis test. Human lymphocyte chromosome aberration test, mouse micronucleus test and rat dominant lethal test result were all negative.
Reproductive toxicity:
Paroxetine was given at 15 mg / kg / day (calculated as mg / m2, which is 2.9 times the clinically recommended dose for the treatment of depression). The conception rate of rats decreased. In 2 to 52 week toxicity studies. Irreversible damage to the reproductive tract of male rats was found (epidermal vacuoles were seen at 50 mg / kg / day. At 2 Smg / kg / day, the atrophy of the pill tube with atrophy suppression was atrophied). Organogenesis rats and rabbits were given paroxetine 50mg / kg / day and 6mg / kg / day, respectively (calculated as mg / m2. They are equivalent to 8 and 2 times the clinically recommended doses for treating depression, respectively). No teratogenic effect was seen. However, the rats were continuously administered three months after pregnancy and throughout the lactation period. In the first 4 days of lactation, the death of young rats increased. The effect occurred at 1 g / kg / day. The cause of death is unknown. A no-effect dose that caused death in rat pups could not be determined.
Carcinogenicity In carcinogenicity tests administered to rodents for two years. The doses for mice and rats were 25 mg / kg days and 20 mg / kg days, respectively (calculated as mg / m2, which are equivalent to 3.9 times the clinically recommended doses for the treatment of depression). The results showed that the incidence of reticuloma in male rats in the high-dose group increased significantly (control, low, medium, and high-dose groups were 1/0, 0 / 50.0 / 50, and 4/50, respectively). The incidence of lymphatic reticuloendothelial tumors increased in a dose-dependent manner. No effect was seen in female rats. The number of tumors in mice showed a dose-dependent increase. However, the number of mice with tumors showed no drug-related increase. The relevance of these findings to humans is unclear.

Pharmacokinetics of Paroxetine Hydrochloride Tablets

Paroxetine hydrochloride solution is completely absorbed after oral administration. Take this product orally 30mg daily. Take it continuously for 30 days. The mean clearance half-life is about 21 hours (CV 32%). Paroxetine is mainly degraded by metabolism. Its metabolites have no pharmacological activity. It appears as a nonlinear pharmacokinetic process at increasing doses. Paroxetine is partially metabolized by CYP2D6. Metabolites are mainly excreted in urine, and a small amount is excreted in feces. There are no data to evaluate the pharmacokinetics of paroxetine in patients with CYP2D6 deficiency (lack of metabolism).
Absorption and distribution This product can be completely absorbed after oral administration. After absorption, it undergoes first pass metabolism. Normal men take this product 30mg orally daily. Most of them can reach steady state in about 10 days. Very few patients require slightly longer time, Cmax 61.7g / ml at steady state. Tmax was 5.2.hr and Cmax was 30.7ng / ml. 21 hours (CV 32%). Steady-state Cmax and Cmax values are 6-14 times the values predicted by single-dose clinical trials. Based on AUC port. 2. The calculated steady-state drug exposure is 8 times the value predicted by the single-dose clinical trial. Excessive accumulation is the result of rapid saturation of the metabolic enzymes of paroxetine.
Adopt the method of eating Russian and not eating at the same time of single dose administration. The effect of food on paroxetine bioavailability was studied. When serving with food. AUC increased slightly (6%). But Cmax increased more (29%). The peak plasma concentration time was reduced from 6.4 hours to 4.9 hours. 95% of this product is combined with plasma proteins. Distributed throughout the body. Including the central nervous system. Only 1% remains in the systemic circulation.
The elimination half-life of metabolism and excretion is usually 24 hours. This product is metabolized by the liver, mainly excreted by the kidneys, and a small amount is excreted by feces. Its metabolites are inactive.
The main metabolites of paroxetine after oral absorption are polar covalent complexes of oxidation and methylation. Easy to remove. Covalent conjugates with glucuronic acid and sulfate are predominant. Major metabolites have been isolated and identified. The data show that the inhibitory effect of drug metabolites on serotonin reintroduction is less than 1/50 of the parent drug. CYP2D6 is involved in partial metabolism of paroxetine. When clinical dosage. The saturation of this enzyme makes the pharmacokinetic process of paroxetine dose increase and treatment course appear non-linear. The effect of this enzyme on paroxetine metabolism suggests some potential drug-drug interactions (see [Cautions]). 10 days after oral paroxetine solution 30mg dose. Almost 64% is excreted by the urine. 2% of them are parent drugs. 62% are metabolites, and about 36% are excreted by feces (probably via bile). Most of them are metabolites. The parent drug is less than 1%.

Paroxetine Hydrochloride Tablets Storage

Shaded, sealed and stored in a dry place.

Packaging of Paroxetine Hydrochloride Tablets

Aluminum-plastic blister, 7 pieces per plate, 1 plate per box.
Aluminum plastic blister, 10 pieces per plate, 1 plate per box.

Expiration date of paroxetine hydrochloride tablets

36 months

Paroxetine Hydrochloride Tablets

"Chinese Pharmacopoeia" 2010 edition two ^[1]