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HCID 43815생성일: 2026년 10월 27일

파록세틴

파록세틴 · PAXIL · PAROXETIN HCL · AROPAX · FG 7051 · BRL 29060 · AROPAX 20 · Paloxitene

https://huagongshe.com/ko/chemical/43815

파록세틴 분자 구조식

식별자 및 물리적 특성

CAS No.110429-35-1
분자식C19H20FNO3
평균 분자량329.4 g/mol
단동위원소 질량329.14272172 g/mol
SMILESFc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1
InChIKeyAHOUBRCZNHFOSL-YOEHRIQHSA-N
PubChem CID43815
ChEMBLCHEMBL1708
ChEBICHEBI:7936
EC No.682-717-4
DTXSIDDTXSID3023425
현지명파록세틴

화학 및 물리적 성질

XLogP3.5
극성 표면적39.7
수소 결합 공여자 수1
수소 결합 수용자 수5
회전 가능 결합 수4
무거운 원자 수24
형식 전하0
복잡도402
물질 분류Pharmaceutical
의약품DEA NFLIS-Drug Category -> AntidepressantsPharmaceuticals -> Used in SwitzerlandPharmaceuticals -> Nervous system -> PsychoanalepticsPharmaceuticals -> SSRIs (Selective Serotonin Reuptake Inhibitors)Pharmaceuticals -> Listed in ZINC15
LogP(분배 계수)log Kow = 1.233.64.07
용해도Odorless, off-white powder, mp 147-150 °C . Solubility in water: >1 g/mL/Paroxetine methanesulfonate/In water, 1,131 mg/L at 25 °C8.53e-03 g/L
Human DrugsAntidepressants -> Selective serotonin reuptake inhibitors (SSRI)Breast FeedingLactationMilk, HumanAntidepressive AgentsSerotonin Uptake InhibitorsPharmaceuticals
Endocrine DisruptorsPotential endocrine disrupting compound
끓는 점451.7±45.0451.7±45.0 °C(Predicted)
녹는점120-138Odorless off-white powdermolecular weight: 374.84melting point: 120-138 °C /Hydrochloride hemihydrate/129 - 131 °C114-116°C
Physical DescriptionSolid
Dissociation Constants9.519.90pKa1 = 9.6 /secondary amine/
Collision Cross Section183.8 Ų [M+H]+ [CCS Type: DTBuffer gas: N2Ionization: ESI+Dataset: Antidepressants]183.2 Ų [M+H]+ [CCS Type: TWMethod: Major Mix IMS/Tof Calibration Kit (Waters)]180.32 Ų [M+H]+ [CCS Type: TWMethod: calibrated with polyalanine and drug standards]183.61 Ų [M+H]+
Other Experimental PropertiesCrystalsmelting point: 129-131 °Csolubility in water: 5.4 mg/mL /Paroxetine hydrochloride hemihydrate/Crystals from ethanol-ethermelting point: 136-138 °CSpecific optical rotation for the D (sodium) line: -87 deg (c= 5 in ethanol) /paroxetine maleate/
밀도1.1844 (estimate)
저장 조건under inert gas (nitrogen or Argon) at 2–8 °C
물리적 상태Solid
pKa(산도 계수)pKa 9.51 (Uncertain)
색상Off-white to light yellow
NISTParoxetine(61869-08-7)
EPAParoxetine (61869-08-7)

화학적 성질

White Solid

안전 및 규제

GHS 분류This chemical does not meet GHS hazard criteria for 16.7% (1 of 6) of reports.DangerH302 (66.7%): Harmful if swallowed [Warning Acute toxicity, oral]P203, P264, P270, P273, P280, P301+P317, P318, P330, P391, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 6 reports by companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
FDA 요건The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including paroxetine mesylate, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Paroxetine mesylate/The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including paroxetine hydrochloride, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. /Paroxetine hydrochloride/
Toxic Combustion ProductsSpecial hazards arising from the substance or mixture: Carbon oxides, nitrogen oxides (NOx), Hydrogen chloride gas, Hydrogen fluoride. /Paroxetine hydrochloride hemihydrate/
Hazard Classes and CategoriesAcute Tox. 4 (66.7%)
Hazardous Reactivities and IncompatibilitiesIncompatible materials: Strong oxidizing agents. /Paroxetine hydrochloride hemihydrate/
소화 절차Suitable extinguishing media: Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. /Paroxetine hydrochloride hemihydrate/Advice for firefighters: Wear self contained breathing apparatus for fire fighting if necessary. /Paroxetine hydrochloride hemihydrate/
보관 조건Conditions for safe storage, including any incompatibilities: Keep container tightly closed in a dry and well-ventilated place. /Paroxetine hydrochloride hemihydrate/Store tablets between 15 deg and 30 °C (59 deg and 86 °F). ... Store suspension at or below 25 °C (77 °F).
정리 방법Accidental Release Measures. Personal precautions, protective equipment and emergency procedures: Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust. Environmental precautions: Do not let product enter drains. Methods and materials for containment and cleaning up: Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed containers for disposal. /Paroxetine hydrochloride hemihydrate/

용도

개요

Paroxetine is a new highly selective serotonin reuptake inhibitor, mechanistically similar to fluoxetine, fluvoxamine and sertraline, introduced for the treatment of all types of depressive illnesses including depression associated with anxiety. It is reportedly non-sedating and non-stimulatory and compared to fluoxetine has a shorter duration of action (half-life of 24 hours versus 2 to 3 days). Paroxetine is also being investigated as a treatment for obesity, alcoholism and obsessive-compulsive disorders.

용도

A istopically labelled selective serotonin reuptake inhibitor. Used as an antidepressant

일반 설명

In the structure of paroxetine (Paxil), an amino group, protonatedin vivo could H-bond with the–CH2–O– unshared electrons.A β-arylamine–like structure with an extra aryl groupresults. The compound is a very highly selective SERT. Asexpected, it is an effective antidepressant and anxiolytic.

처리 방법SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.SRP: At the time of review, regulatory criteria for small quantity disposal are subject to significant revision, however, household quantities of waste pharmaceuticals may be managed as follows: Mix with wet cat litter or coffee grounds, double bag in plastic, discard in trash.Product: Offer surplus and non-recyclable solutions to a licensed disposal company. Contact a licensed professional waste disposal service to dispose of this material. Contaminated packaging: Dispose of as unused product. /Paroxetine hydrochloride hemihydrate/
Preventive MeasuresAppropriate engineering controls: Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday. /Paroxetine hydrochloride hemihydrate/Precautions for safe handling: Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed. Normal measures for preventive fire protection. /Paroxetine hydrochloride hemihydrate/Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. /Paroxetine hydrochloride hemihydrate/
Personal Protective Equipment (PPE)Skin protection: Handle with gloves. /Paroxetine hydrochloride hemihydrate/Eye/face protection: Safety glasses with side-shields conforming to EN166 Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). /Paroxetine hydrochloride hemihydrate/Respiratory protection: For nuisance exposures use type P95 (US) or type P1 (EU EN 143) particle respirator.For higher level protection use type OV/AG/P99 (US) or type ABEK-P2 (EU EN 143) respirator cartridges. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). /Paroxetine hydrochloride hemihydrate/Body Protection: Complete suit protecting against chemicals, The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. /Paroxetine hydrochloride hemihydrate/
TreatmentTreatment should consist of those general measures employed in the management of overdosage with any drugs effective in the treatment of major depressive disorder. Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. General supportive and symptomatic measures are also recommended. Induction of emesis is not recommended. Gastric lavage with a large-bore orogastric tube with appropriate airway protection, if needed, may be indicated if performed soon after ingestion, or in symptomatic patients. Activated charcoal should be administered. Due to the large volume of distribution of this drug, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit. No specific antidotes for paroxetine are known. (L1712)
상호 작용Rhodiola rosea (Russian Rhodiola/Golden Root) is a high mountain plant from the arctic regions of Europe and Asia which has the active substance phenylpropanoide. It has sedative, anti-depressive, drive-enhancing and stress-modulated properties stimulating the distribution of dopamine and serotoninin combination with other drugs, an increase of side effects and risk profile has to be expected. A case report is presented in order to illustrate the interaction between Rhodiola rosea and antidepressants. We report the case of a 68-year-old female patient with recurrent moderate depressive disorder with somatic syndrome (ICD-10 F33.11) who developed vegetative syndrome, restlessness feeling and trembling since she began to ingest Rhodiola rosea in addition to paroxetine. Prescribing Rhodiola rosea with paroxetine, pharmacokinetic and -dynamic interactions have to be assumed. The symptoms of the patient can be interpreted as a serotonergic syndrome. Because of its different effects, the plant is widely used. An increase of clinical relevant risks should be considered in the add-on treatments.A 74-year-old man with depressive symptoms was admitted to a psychiatric hospital due to insomnia, loss of appetite, exhaustion, and agitation. Medical treatment was initiated at a daily dose of 20 mg paroxetine and 1.2 mg alprazolam. On the 10th day of paroxetine and alprazolam treatment, the patient exhibited marked psychomotor retardation, disorientation, and severe muscle rigidity with tremors. The patient had a fever (38.2 degrees C), fluctuating blood pressure (between 165/90 and 130/70 mg mm Hg), and severe extrapyramidal symptoms. Laboratory tests showed an elevation of creatine phosphokinase (2218 IU/L), aspartate aminotransferase (134 IU/L), alanine aminotransferase (78 IU/L), and BUN (27.9 mg/ml) levels. The patient received bromocriptine and diazepam to treat his symptoms. 7 days later, the fever disappeared and the patient's serum CPK levels were normalized (175 IU/L). This patient presented with symptoms of neuroleptic malignant syndrome (NMS), thus demonstrating that NMS-like symptoms can occur after combined paroxetine and alprazolam treatment. The adverse drug reaction score obtained by the Naranjo algorithm was 6 in our case, indicating a probable relationship between the patient's NMS-like adverse symptoms and the combined treatment used in this case. The involvement of physiologic and environmental aspects specific to this patient was suspected. Several risk factors for NMS should be noted in elderly depressive patients whose symptoms often include dehydration, agitation, malnutrition, and exhaustion. Careful therapeutic intervention is necessary in cases involving elderly patients who suffer from depression.Serotonin toxicity is an iatrogenic complication of serotonergic drug therapy. It is due to an overstimulation of central and peripheral serotonin receptors that lead to neuromuscular, mental and autonomic changes. Moclobemide is a reversible inhibitor of monoamine oxidase (MAO)-A, selegiline is an irreversible selective inhibitor of MAO-B, and paroxetine is a selective serotonin reuptake inhibitor. Combined use of these agents is known to cause serotonin toxicity. A 53-year-old woman had been treated with paroxetine and selegiline. After moclobemide was prescribed in place of paroxetine without a washout period, she quickly developed confusion, agitation, ataxia, diaphoresis, tremor, mydriasis, ocular clonus, hyperreflexia, tachycardia, moderately elevated blood pressure and high fever, symptoms that were consistent with serotonin toxicity. Discontinuation of the drugs, hydration and supportive care were followed by remarkable improvement of baseline status within 3 days. This case demonstrates that serotonin toxicity may occur even with small doses of paroxetine, selegiline and moclobemide in combination. Physicians managing patients with depression must be aware of the potential for serotonin toxicity and should be able to recognize and treat or, ideally, anticipate and avoid this pharmacodynamically-mediated interaction that may occur between prescribed drugs.A 69-year-old white female presented to the emergency department with a history of confusion and paranoia over the past several days. On admission the patient was taking carvedilol 12 mg twice daily, warfarin 2 mg/day, folic acid 1 mg/day, levothyroxine 100 microg/day, pantoprazole 40 mg/day, paroxetine 40 mg/day, and flecainide 100 mg twice daily. Flecainide had been started 2 weeks prior for atrial fibrillation. Laboratory test findings on admission were notable only for a flecainide plasma concentration of 1360 ug/L (reference range 200-1000). A metabolic drug interaction between flecainide and paroxetine, which the patient had been taking for more than 5 years, was considered. Paroxetine was discontinued and the dose of flecainide was reduced to 50 mg twice daily. Her delirium resolved 3 days later. ... According to the Naranjo probability scale, flecainide was the probable cause of the patient's deliriumthe Horn Drug Interaction Probability Scale indicates a possible pharmacokinetic drug interaction between flecainide and paroxetine. Supratherapeutic flecainide plasma concentrations may cause delirium. Because toxicity may occur when flecainide is prescribed with paroxetine and other potent CYP2D6 inhibitors, flecainide plasma concentrations should be monitored closely with commencement of CYP2D6 inhibitors.For more Interactions (Complete) data for PAROXETINE (53 total), please visit the HSDB record page.
HepatotoxicityLiver test abnormalities have been reported to occur in up to 1% of patients on paroxetine, but elevations are usually modest and usually do not require dose modification or discontinuation. Rare instances of acute, clinically apparent episodes of liver injury, with marked liver enzyme elevations with or without jaundice, have been reported in patients on paroxetine. The onset of injury is usually within 2 to 16 weeks, but can be more delayed, to up to 1 year. The pattern of serum enzyme elevations varies from hepatocellular to mixed or cholestatic. While most cases are mild-to-moderate in severity, severe cases with hepatic failure have been reported. Autoimmune (autoantibodies) and immunoallergic features (rash, fever, eosinophilia) are uncommon.
생태독성 수치EC50Species: Xenopus laevis (African Clawed Frog) blastulaConditions: freshwater, renewal, 23 °C, pH 6.5-9.0Concentration: 4600 ug/L for 96 hrEffect: development, increased deformation /98% purity/LC50Species: Ceriodaphnia dubia (Water Flea) age <24 hr neonate, 3rd or 4th broodConditions: freshwater, static, 24-26 °C, pH 8.1-8.35, hardness 78-93 mg/L CaCO3, alkalinity 64-78 mg/L CaCO3, dissolved oxygen 5.6-6.8 mg/LConcentration: 580 ug/L for 48 hr /99.86% purity/
환경 거동TERRESTRIAL FATE: Based on a classification scheme(1), a Koc range 8,128 to 2.9X10+5(2) indicates that paroxetine is expected to be immobile in soil(SRC). The pKa of paroxetine is 9.6(3), indicating that this compound will exist almost entirely in the cation form in the environment and cations generally adsorb more strongly to soils containing organic carbon and clay than their neutral counterparts(4). Volatilization from moist soil is not expected because the compound exists as an ation and cations do not volatilize. Paroxetine is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 4.8X10-8 mm Hg at 25 °C(SRC), determined from a fragment constant method(5). Biodegradation data in soil were not available(SRC, 2015).AQUATIC FATE: Based on a classification scheme(1), a Koc range of 8,128 to 2.9X10+5(2) indicates that paroxetine is expected to adsorb to suspended solids and sediment(SRC). A pKa of 9.6(3) indicates paroxetine will exist almost entirely in the cation form at pH values of 5 to 9 and, therefore, volatilization from water surfaces is not expected to be an important fate process(SRC). According to a classification scheme(4), an estimated BCF of 3(SRC), from its log Kow of 1.23(3) and a regression-derived equation(5), suggests the potential for bioconcentration in aquatic organisms is low(SRC). Biodegradation data in water were not available(SRC, 2015).ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), paroxetine, which has an estimated vapor pressure of 4.8X10-8 mm Hg at 25 °C(SRC), determined from a fragment constant method(2), is expected to exist solely in the particulate phase in the ambient atmosphere. Particulate-phase paroxetine may be removed from the air by wet and dry deposition(SRC). Photodegradation first order rate constants of 0.29 and 0.27/hr were reported with half-lives of 2.6 and 2.4 hours, respectively(3).
유해 작용Many of the side effects of paroxetine are dose-dependent. The most common side effects include drowsiness, dry mouth, loss of appetite, sweating, sleep disturbance, and sexual side effects. Clinicians can address sexual side effects medications like sildenafil). Discontinuation syndrome is more common and more severe with paroxetine than with other SSRIsthis may be due in part to the fact that it inhibits its own metabolism. Withdrawal symptoms from discontinuation include dizziness, lethargy, nausea, vomiting, headache, fever, chills, vivid dreams, electric shock-like-sensation, dyskinesia, anxiety, crying, irritability, and depersonalization.
노출 경로Paroxetine hydrochloride is slowly, but completely absorbed following oral administration. Paroxetine mesylate salt is also completely absorbed after oral dosing. The oral bioavailability appears to be low due to extensive first-pass metabolism. Paroxetine hydrochloride oral tablets and suspension are reportedly bioequivalent. Absorption of either salt form is not substantially affected by food. Peak concentrations of Brisbelle (mesylate salt) were reached at 6 hours (3 to 8 hours range). Steady state Cmax was 13.10 ng/mL. The steady state AUC (0-last) was 237 hr*ng/mL. Paroxetine mesylate generally follows non-linear pharmacokinetics because CYP2D6, the enzyme that is part responisible for paroxetine metabolism, is readily saturable.
Milk ConcentrationsEXPERIMENTAL: The study was carried out to quantify the excretion of the selective serotonin reuptake inhibitor paroxetine in breast milk. In 6 lactating women, the concentrations of paroxetine in breast milk and serum were studied at the times for assumed minimum (24 hours after dose intake) and maximum (4-7 hours after dose intake) drug levels in milk. Moreover, a seventh subject was studied with frequent and regular sampling throughout a dose interval of 24 hours at 2 different dose levels. The mean milk/serum concentration ratios in the first 6 subjects ranged from 0.39 to 1.11 (overall mean +/- SD = 0.69 +/- 0.29), and the mean estimated dose to the infants ranged from 0.7% to 2.9% (overall mean +/- SD = 1.4% +/- 0.79%) of the weight-adjusted maternal dose. Based on area-under-the-curve data from the seventh subject, the milk/serum concentration ratio was 0.69 at a dose of 20 mg/day and 0.72 at a dose of 40 mg/daythe estimated relative doses to the infant were 1.0% and 2.0%, respectively. The mean increase in milk paroxetine concentrations from assumed minimum to assumed maximum was 61% (range, 4%-172%p < .01). The mean paroxetine concentration in hindmilk was 78% higher than in foremilk (range, 16%-169%p < .01), an increase that was parallel to the increase in milk triglyceride levels (r = 0.83, p = 0.005). No adverse drug reactions or unusual behaviors were reported in the infants. CONCLUSION: The study indicates that the relative dose to a suckling infant for paroxetine is lower than that reported for fluoxetine and citalopram and higher than that reported for sertraline and fluvoxamine.
독성 요약IDENTIFICATION AND USE: Paroxetine is an odorless off-white powder formulated into an oral suspension, extended-release film-coated tablets, or film-coated tablets. Paroxetine a second generation selective serotonin-reuptake inhibitor is used for the treatment of major depressive disorder, obsessive and compulsive disorder, panic disorder, social anxiety disorders, general anxiety disorders, and posttraumatic stress disorder. Paroxetine has more recently been approved for use in the treatment of moderate to severe vasomotor symptoms (VMS) associated with menopause. HUMAN EXPOSURE AND TOXICITY: Spontaneous cases of deliberate or accidental overdosage during paroxetine treatment have been reportedsome of these cases were fatal and some of the fatalities appeared to involve paroxetine alone. Commonly reported adverse reactions associated with paroxetine overdosage include somnolence, coma, nausea, tremor, tachycardia, confusion, vomiting, and dizziness. Other notable signs and symptoms observed with overdoses involving paroxetine (alone or with other substances) include mydriasis, convulsions (including status epilepticus), ventricular dysrhythmias (including torsades de pointes), hypertension, aggressive reactions, syncope, hypotension, stupor, bradycardia, dystonia, rhabdomyolysis, symptoms of hepatic dysfunction (hepatic failure, hepatic necrosis, jaundice, hepatitis, and hepatic steatosis), serotonin syndrome, manic reactions, myoclonus, acute renal failure, and urinary retention. During premarketing testing, seizures occurred in 0.1% of patients treated with paroxetine. During premarketing testing, hypomania or mania occurred in approximately 1.0% of paroxetine-treated unipolar patients. In a subset of patients classified as bipolar, the rate of manic episodes was 2.2% for paroxetine and 11.6% for the combined active-control groups. Stevens-Johnson syndrome and toxic epidermal necrolysis have also been reported in paroxetine-treated patients. Epidemiological studies have shown that infants exposed to paroxetine in the first trimester of pregnancy have an increased risk of congenital malformations, particularly cardiovascular malformations. Perinatal adverse effects, including respiratory distress and neonatal adaptation problems are common in exposed infants, and an increased risk for persistent pulmonary hypertension of the newborn (PPHN) has been observed. Also, some neonates exposed to paroxetine and other selective serotonin-reuptake inhibitors (SSRIs) or selective serotonin- and norepinephrine-reuptake inhibitors (SNRIs) late in the third trimester of pregnancy have developed complications that occasionally have been severe and required prolonged hospitalization, respiratory support, enteral nutrition, and other forms of supportive care in special care nurseries. Clinical findings reported to date in the neonates have included respiratory distress, cyanosis, apnea, seizures, temperature instability or fever, feeding difficulty, dehydration, excessive weight loss, vomiting, hypoglycemia, hypotonia, hypertonia, hyperreflexia, tremor, jitteriness, irritability, lethargy, reduced or lack of reaction to pain stimuli, and constant crying. Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Genotoxicity tests for cytogenetic aberrations in vitro in human lymphocytes were negative. ANIMAL STUDIES: Two-year carcinogenicity studies were conducted in rodents given paroxetine in the diet at 1, 5, and 25 mg/kg/day (mice) and 1, 5, and 20 mg/kg/day (rats). There was a significantly greater number of male rats in the high-dose group with reticulum cell sarcomas (1/100, 0/50, 0/50, and 4/50 for control, low-, middle-, and high-dose groups, respectively) and a significantly increased linear trend across dose groups for the occurrence of lymphoreticular tumors in male rats. Female rats were not affected. Although there was a dose-related increase in the number of tumors in mice, there was no drug-related increase in the number of mice with tumors. The relevance of these findings to humans is unknown. Reproduction studies in rats receiving oral paroxetine dosages of 50 mg/kg daily and in rabbits receiving 6 mg/kg daily during organogenesis have been conducted. Although these studies have not revealed evidence of teratogenicity, an increase in pup deaths was observed in rats during the first 4 days of lactation when dosing occurred during the last trimester of gestation and continued throughout lactation. This effect occurred at a dose of 1 mg/kg daily. A reduced pregnancy rate was found in reproduction studies in rats at a dose of paroxetine of 15 mg/kg/day. Irreversible lesions occurred in the reproductive tract of male rats after dosing in toxicity studies for 2 to 52 weeks. These lesions consisted of vacuolation of epididymal tubular epithelium at 50 mg/kg/day and atrophic changes in the seminiferous tubules of the testes with arrested spermatogenesis at 25 mg/kg/day. Paroxetine produced no genotoxic effects in a battery of in vitro and in vivo assays that included the following: Bacterial mutation assay, mouse lymphoma mutation assay, unscheduled DNA synthesis assay, and tests for cytogenetic aberrations in vivo in mouse bone marrow and in a dominant lethal test in rats.Though it is rarely lethal in overdose by itself, patients can develop somnolence, nausea, tremor, heart rhythm disturbances, confusion, vomiting, dizziness, and mydriasis. During toxicity, a patient’s airway, oxygenation, and ventilation require evaluation first. The treatment for overdose includes symptomatic supportive treatment. There is no specific treatment for paroxetine toxicity.Paroxetine is a potent and highly selective inhibitor of neuronal serotonin reuptake. Paroxetine likely inhibits the reuptake of serotonin at the neuronal membrane, enhances serotonergic neurotransmission by reducing turnover of the neurotransmitter, therefore it prolongs its activity at synaptic receptor sites and potentiates 5-HT in the CNSparoxetine is more potent than both sertraline and fluoxetine in its ability to inhibit 5-HT reuptake. Compared to the tricyclic antidepressants, SSRIs have dramatically decreased binding to histamine, acetylcholine, and norepinephrine receptors. The mechanism of action for the treatment of vasomotor symptoms is unknown.
생태독성 발췌/AQUATIC SPECIES/ Selective serotonin reuptake inhibitors (SSRIs) are neurologically active drugs that can contaminate surface waters and have the potential to negatively affect aquatic organisms. In this investigation, the 48 hr acute toxicity of mixtures (binary and quaternary) of four common SSRIs (fluoxetine [Prozac], sertraline [Zoloft], paroxetine [Paxil], and citalopram [Celexa]) were determined in the daphnid Ceriodaphnia dubia. Logistic regression was used to model mortality data and to investigate the applicability of concentration addition and independent action models to explain observed mortality. The concentrations estimated to induce 50% mortality in 48 hr for the individual SSRIs sertraline, fluoxetine, paroxetine, and citalopram were 0.48 to 0.66, 1.23 to 1.84, 2.23 to 3.57, and 10.47 to 14.53 uM, respectively. Concentration addition was a better predictor of mixture effects than independent action and suggested that the tested SSRIs have a similar mechanism of action. Results indicate that environmental hazard assessments should be conservative and consider that acutely toxic effects in aquatic organisms can be additive for each SSRI in a mixture./AQUATIC SPECIES/ ...In this investigation, the acute and chronic toxicity of five /selective serotonin reuptake inhibitors/ (SSRIs) (fluoxetine, Prozacfluvoxamine, Luvoxparoxetine, Paxilcitalopram, Celexaand sertraline, Zoloft) were evaluated in the daphnid Ceriodaphnia dubia. For each SSRI, the 48 hr median lethal concentration (LC50) was determined in three static tests with neonate C. dubia, and chronic (8 day) tests were conducted to determine no-observable-effect concentrations (NOEC) and lowest-observable-effect concentrations (LOEC) for reproduction endpoints. The 48 hr LC50 for the SSRIs ranged from 0.12 to 3.90 mg/L and the order of toxicity of the compounds was (lowest to highest): Citalopram, fluvoxamine, paroxetine, fluoxetine, sertraline. Mortality data for the 8 day chronic tests were similar to the 48 hr acute data. The SSRIs negatively affected C. dubia reproduction by reducing the number of neonates per female, and for some SSRIs, by reducing the number of broods per female. For sertraline, the most toxic SSRI, the LOEC for the number of neonates per female was 0.045 mg/L and the NOEC was 0.009 mg/L. Results indicate that SSRIs can impact survival and reproduction of C. dubiahowever, only at concentrations that are considerably higher than those expected in the environment./AQUATIC SPECIES/ ...In the present study, ... the toxicities of five SSRIs (citalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline) as single substances and of citalopram, fluoxetine, and sertraline in binary mixtures /were tested/ in two standardized bioassays. Test organisms were the freshwater algae Pseudokirchneriella subcapitata and the freshwater crustacean Daphnia magna. In algae, test median effect concentrations (EC50s) ranged from 0.027 to 1.6 mg/L, and in daphnids, test EC50s ranged from 0.92 to 20 mg/L, with sertraline being one of the most toxic compounds. ...
Signs and SymptomsComa, dizziness, drowsiness, facial flushing, nausea, sweating, tremor, vomiting
Effluent ConcentrationsParoxetine was not detected in 84 samples of wastewater from treatment plants at the Spanish Mediterranean area of Valencia. Sampling occurred in June 2008, January 2009, April 2009, and October 2009detection limit range = 0.17 to 0.27 ug/L(1). Paroxetine was analyzed for but not detected in effluents from 90 European wastewater treatment plants, sampled in 2010(2). The compound was not detected in sewage from Tromso Norway(3).
운송 번호(UN)3249
포장분류III
위험 등급6.1(b)
유해 물질 데이터61869-08-7(Hazardous Substances Data)