化合物详情

Symptoms of toxicity include alopecia, decreased libido, diarrhea, ejaculation disorder, fatigue, insomnia, somnolence and serotonin syndrome.

Treatment should consist of those general measures employed in the management of overdosage with any antidepressant. 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 large volume of distribution of this drug, forced diuresis, dialysis, hemoperfusion and exchange transfusion are unlikely to be of benefit. No specific antidotes for sertraline are known. (L1712)

Because of its extensive protein binding. Sertraline may cause a shift in plasma concns of other drugs similarly tightly protein bound (eg, warfarin, propranolol). the risk of using sertraline in combination with other CNS adrenergic drugs has not been systematically evaluated. Sertraline appears to induce hepatic microsomal enzymes. Patients receiving a sertraline reuptake inhibitor drug in combination with a monoamine oxidase inhibitor may develop serious, sometimes fatal, reactions including hyperthermia, rigidity, myoclonus, autonomic instability, & mental changes (extreme agitation, delirium, coma). At least 14 days should be allowed after starting sertraline before starting a MAOI.

Likelihood score: B (likely but rare cause of clinically apparent liver injury).

Neonates exposed to sertraline late in the third trimester have been reported with complications requiring prolonged hospitalization, tube feeding, and respiratory support.

The effects of food on the bioavailability of the sertraline tablet and oral concentrate were studied in subjects administered a single dose with and without food. For the tablet, AUC was slightly increased when drug was administered with food but the Cmax was 25% greater, while the time to reach peak plasma concentration (Tmax) decreased from 8 hours post-dosing to 5.5 hours. For the oral concentrate, Tmax was slightly prolonged from 5.9 hours to 7.0 hours with food.

The exact mechanism of action sertraline is not fully known, but the drug appears to selectively inhibit the reuptake of serotonin at the presynaptic membrane. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. It is suggested that these modifications are responsible for the antidepressant action observed during long term administration of antidepressants. It has also been hypothesized that obsessive-compulsive disorder is caused by the dysregulation of serotonin, as it is treated by sertraline, and the drug corrects this imbalance.

Limited data are available regarding the use of sertraline (Zoloft) during pregnancy. The California Teratogen Information Service prospectively ascertained 112 pregnant women taking sertraline and compared outcomes to those of 191 women ascertained for nonteratogenic exposures. The rate of major anomalies did not differ significantly between the groups (3.8% vs. 1.9%). Anomalies in the sertraline group included bilateral choanal atresia, valvular pulmonic stenosis with an atrial septal aneurysm, unilateral clubfoot, and Down Syndrome in a pregnancy that was terminated. Among the 158 infants who received a dysmorphological examination, the frequency of minor anomalies was similar in the two groups. There was a nonsignificant excess of spontaneous abortions in the sertraline group (16.7%...

No indication of carcinogenicity to humans (not listed by IARC).

References: DOI:10.1016/j.drudis.2019.09.022

Recent studies suggest that serotonin (5-HT) may play a role in morphogenesis in the mouse embryo. The possible involvement of 5-HT in early development suggests that substances which interfere with serotonergic activities may have teratogenic potential. Therefore, the ability of sertraline, a selective 5-HT uptake inhibitor, to cause developmental defects was investigated. Mouse embryos, in whole embryo culture, were exposed during gastrulation (day 8; plug day = day 1) or neurulation (day 9) to 5-20 uM sertraline and examined for malformations after 48-60 hours. Dose dependent effects were observed on growth and expansion of the prosencephalon and on development of the first visceral arch, following exposure at both stages. Exposure to 20 uM sertraline at day 9 caused a high incidence...

/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poison A and B/

Some studies have shown that SSRIs might have sexual side effects, like low sexual desire or problems with ejaculation. These side effects might affect a man’s fertility (ability to get a woman pregnant). Having depression might also lower sex drive. A man’s use of sertraline is not expected to increase the chance of birth defects. In general, exposures that fathers or sperm donors have are unlikely to increase risks to a pregnancy. For more information, please see the MotherToBaby fact sheet�Paternal Exposure at https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/.

Reference: Smith, C.D. and Nowell, L.H., 2024. Health-Based Screening Levels for evaluating water-quality data (3rd ed.). DOI:10.5066/F71C1TWP