Is There a Connection Between Sertraline and Dizziness?

Sertraline hydrochloride (Zoloft) is a white film-coated tablet with a white core and an antidepressant. Sertraline is used to treat symptoms associated with depression, including depression with anxiety, with or without a history of mania. After the effect is satisfactory, continuing to take sertraline can effectively prevent the recurrence and recurrence of depression. Sertraline is also used to treat OCD. After the effect is satisfactory, continuing to take sertraline can effectively prevent the recurrence of the initial symptoms of obsessive-compulsive disorder.

Sertraline Hydrochloride Tablets (Zoloft)

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Sertraline Hydrochloride Tablets (Zoloft)

In March 2006, Health Canada issued a message warning against the use of serotonin reuptake inhibitors (

In a multiple-dose controlled clinical study of sertraline and placebo in the treatment of depression, common adverse reactions compared to placebo

Gastrointestinal tract: diarrhea / poor stools, dry mouth, indigestion and nausea.

Metabolism and nutrition: anorexia. Nervous system: dizziness, drowsiness, and tremor.

Spirit: insomnia. Reproductive system and breast: sexual dysfunction (mainly delayed male ejaculation).

Skin and subcutaneous tissue: sweating.

The adverse effects observed in double-blind, placebo-controlled trials in patients with obsessive-compulsive disorder were similar to those observed in clinical trials in patients with depression.

Sertraline has received spontaneous reports of adverse events in patients taking sertraline after it was marketed. This includes:

Blood and lymphatic system: neutrophil deficiency and platelet deficiency.

Heart: palpitations and tachycardia. Ears and labyrinths: tinnitus.

Endocrine: Hyperprolactinemia, hypothyroidism, and ADH secretion disorder syndrome.

Ophthalmology: enlarged pupils and abnormal vision. Gastrointestinal tract: abdominal pain, constipation, pancreatitis and vomiting.

Whole body and administration site: weakness, chest pain, peripheral edema, fatigue, fever and discomfort.

Hepatobiliary system: Severe liver diseases (including hepatitis, jaundice, and liver failure) and asymptomatic elevated serum transaminase (SGOT and SGPT).

Immune system: allergic reactions, allergies and allergic reactions.

Examination: abnormal clinical test results, changes in platelet function, increased serum cholesterol, weight loss and weight gain.

Metabolism and nutrition: increased appetite and hyponatremia.

Musculoskeletal and connective tissue: joint pain and muscle spasms.

Nervous system: coma, convulsions, headaches, hypoesthesia, migraine, dyskinesias (including symptoms of extrapyramidal side reactions such as hyperactivity, increased muscle tone, molars and gait abnormalities), involuntary muscle contraction, paresthesia, and syncope.

There are also symptoms and signs related to serotonin syndrome, such as anxiety, confusion, sweating, diarrhea, fever, high blood pressure, myotonia, and tachycardia caused by the simultaneous use of serotoninergic drugs.

Mental: Aggressive reactions, agitation, anxiety, depressive symptoms, euphoria, hallucinations, female libido, male libido, nightmares and mental illness.

Kidney and urinary system: urinary incontinence and urinary retention.

Reproductive system and mammary glands: galactorrhea, male mammary overgrowth, irregular menstruation and abnormal penile erection.

Respiration, chest, and mediastinum: bronchospasm and yawning.

Skin and subcutaneous tissue: alopecia, angioedema, facial edema, puffiness around the eyes, skin photoreaction, pruritus, purpura, rash (rare peeling dermatitis, such as polymorphous erythema: Stevens-Johnson syndrome, epidermal necrolysis) And urticaria.

Blood vessels: abnormal bleeding (such as epistaxis, gastrointestinal bleeding, or hematuria), hot flashes, and hypertension.

Other: Symptoms after sertraline discontinuation have been reported to include anxiety, anxiety, dizziness, headache, nausea, and paresthesia.

This product is contraindicated in people allergic to sertraline.

Prohibition of use with monoamine oxidase inhibitors

Precautions

Sertraline should be carefully considered in combination with drugs that increase serotonin nerve conduction such as tryptophan or fenfluramine to avoid possible pharmacodynamic interactions. The best time to switch to sertraline treatment from other serotonin reuptake inhibitors, antidepressants, or anti-obsessive-compulsive drugs is inexperienced. When switching treatments, especially long-acting drugs such as fluoxetine, care should be taken and careful pharmacodynamic evaluation and monitoring should be performed. The washout period for switching from a selective serotonin reuptake inhibitor to another drug treatment has not yet been determined. Mania / hypomania activation: About 0.4% of patients treated with sertraline experienced hypomania or mania during the pre-market trial. When other marketed antidepressants or anti-obsessive-compulsive medications are used to treat affective disorders, a small number of patients have reported mania or mild mania. Both antidepressants and antiobsessive-compulsive drugs have the potential to induce seizures. Seizures occurred in approximately 0.08% of all trials with sertraline for depression; no seizures were reported in sertraline trials for panic disorder. Of the approximately 1,800 OTC patients treated with sertraline, 4 (approximately 0.2%) experienced seizures, of which 3 were adolescents, 2 had epilepsy, and 1 had a family history of epilepsy. None of the four patients received antiepileptic drugs. All seizures have not been determined to be directly related to sertraline treatment. Sertraline has not been evaluated in patients with epilepsy and should be avoided in patients with unstable epilepsy. Patients with controlled epilepsy should be closely monitored, and any patients with seizures while taking sertraline should stop administration. Because patients with depression may have suicidal attempts and may persist until clinically significant remission, patients at risk for suicide should be closely monitored early in treatment. Because OCD and depression have often been shown to co-exist, patients with OCD should also be monitored for suicidal tendencies. Women of childbearing age should use adequate contraceptive safety when using sertraline. Although clinical pharmacological studies have shown that sertraline has no effect on psychomotor activity. However, antidepressants or anti-obsessive-compulsive drugs can affect the energy and physical performance necessary to perform potentially dangerous work such as driving or operating machinery. Therefore, sertraline should be taken with caution in such patients. Patients with liver dysfunction: Sertraline should be used with caution in patients with liver disease. Patients with liver impairment should reduce the dosage or frequency of administration. Patients with renal insufficiency: There is no need to adjust sertraline doses according to the degree of renal impairment.

[Medication for pregnant and lactating women]

There are not enough good controlled studies of pregnant women. Pregnant women should only take medicine if the advantages outweigh the disadvantages. Sporadic studies of small sample sizes of lactating mothers and infants suggest that although sertraline concentration in milk is higher than serum concentration, sertraline concentration in infant serum is extremely low or undetectable. Breastfeeding women should only use it if the advantages outweigh the disadvantages. Taking sertraline during pregnancy and / or lactation, doctors should pay attention to the symptoms mentioned in the post-marketing report, mothers taking serotonin antidepressants including sertraline, and symptoms similar to withdrawal withdrawal in newborns have been reported .

[Child medication]

Although sertraline is slightly metabolized by pediatric patients, in order to avoid excessive blood concentrations, it is recommended to use lower doses for pediatric patients, especially lighter children aged 6-12 years.

[Medicine for the elderly]

The dosage range for elderly patients is the same as for young patients. More than 700 elderly patients (> 65 years of age) participated in clinical trials demonstrating the efficacy of sertraline in this part of the population. The form and incidence of adverse reactions in elderly patients is similar to that in young patients.

medicine interactions

Monoamine oxidase inhibitors (MAOI): Sertraline is combined with monoamine oxidase inhibitors, including the selective monoamine oxidase inhibitor selegiline and the reversible monoamine oxidase inhibitor moclobemide, which has severe side effects and is sometimes fatal. Some cases have symptoms similar to serotonin syndrome, including: fever, stiffness, muscle spasms, autonomic dysfunction with rapid fluctuations in vital signs; changes in mental status include mental disorders, irritability, and extreme agitation until the development of delirium and coma. Therefore, sertraline cannot be taken when taking a monoamine oxidase inhibitor or within 14 days after discontinuing the monoamine oxidase inhibitor; similarly, it takes more than 14 days after sertraline is discontinued to start treatment with a monoamine oxidase inhibitor.

Pimozide: In a single low-dose pimozide (2 mg) study in combination with sertraline, it was confirmed that taking both drugs can increase the plasma concentration of pimozide. Elevated levels did not cause changes in EKG. The mechanism of this drug interaction is not clear. Sertraline and pimozide are not allowed to be co-administered due to the narrow therapeutic window of pimozide.

CNS inhibitors and alcohol: Simultaneous sertraline 200 mg daily does not increase the effects of ethanol, carbamazepine, haloperidol, or phenytoin on cognitive function and psychomotor activity in healthy subjects, but Sertraline is not recommended for use with alcohol.

Lithium: In a placebo-controlled trial of normal volunteers, the combination of sertraline and lithium did not significantly change the pharmacokinetic parameters of lithium, but the tremor increased compared to placebo, indicating that there is a drug between the two drugs The possibility of ergonomic interaction. Sertraline should be monitored when used in combination with other serotonergic drugs such as lithium.

Phenytoin: In placebo-controlled studies of healthy volunteers, long-term administration of sertraline at 200 mg daily did not significantly inhibit phenytoin metabolism. However, if it is required to be combined with sertraline, the serum concentration of phenytoin should be monitored when sertraline is started, and the dose of phenytoin should be adjusted appropriately. In addition, combination with phenytoin can cause sertraline blood concentration to decrease.

Sumatriptan: After sertraline was marketed, there have been individual reports of the combination of sertraline and sumatriptan in patients with frailty, hypertonic reflexes, ataxia, confusion, anxiety, and agitation. Patients should be closely monitored if sertraline is actually needed in combination with the drug in clinical practice. Protein-bound drugs: Because sertraline binds to plasma proteins, attention should be paid to the possibility of interaction between sertraline and other plasma protein-bound drugs. However, in three formal studies of sertraline interacting with diazepam, tolbutamide, and warfarin, sertraline has not been shown to have a significant effect on the protein-binding rate of these drugs.

Warfarin: Sertraline 200 mg / day in combination with warfarin can cause a small but statistically significant increase in prothrombin time, and its clinical significance is not clear. Therefore, prothrombin time should be closely monitored when sertraline is combined with warfarin or discontinued.

Interactions with other drugs: Studies on the interactions between sertraline and other drugs have been performed. Sertraline 200 mg daily in combination with diazepam or tolbutamide can cause some small but statistically significant changes in pharmacokinetic parameters. Combined with cimetidine can significantly reduce sertraline clearance. The clinical significance of these changes is unknown. Sertraline has no effect on the -adrenergic blockade of atenolol. There was no interaction between sertraline 200 mg daily and glipizide or digoxin. Electroshock Therapy (ECT): There have been no clinical trials examining the advantages or risks of sertraline combined with electroshock therapy.

Cytochrome P450 (CYP) 2D6 metabolized drugs: Antidepressants have varying degrees of inhibition of the drug metabolism isoenzyme CYP 2D6. Its clinical significance depends on the degree of inhibition and the therapeutic index of the combined drug. CYP 2D6 substrates with narrow therapeutic indices include tricyclic antidepressants such as propafenone, flcainide, and class 1C antiarrhythmic drugs. Existing drug interaction studies have shown that long-term administration of sertraline at 50 mg daily can slightly increase the steady-state plasma concentration of desipramine (a marker of CYP 2D6 isoenzyme activity) (average 30 -40%).

Other cytochrome (CYP) enzyme metabolism drugs (CYP 3A3 / 4, CYP 2C9, CYP 2C19, CYP 1A2):

CYP 3A3 / 4: In vivo drug interaction tests show that long-term administration of sertraline 200 mg / day does not inhibit CYP 3A3 / 4-mediated hydroxylation of endogenous cortisol or metabolism of carbamazepine and terfenadine effect. In addition, long-term administration of 50 mg of sertraline per day did not inhibit CYP 3A3 / 4-mediated alprazolam drug metabolism. The data indicate that sertraline is not an inhibitor of CYP 3A3 / 4.

CYP 2C9: Sertraline 200 mg / day has no significant effect on the plasma concentrations of tolbutamide, phenytoin, and warfarin. This indicates that sertraline is not a clinically relevant inhibitor of CYP 2C9.

CYP 2C19: Long-term administration of sertraline 200 mg / day has no significant effect on the blood concentration of diazepam, indicating that sertraline is not an inhibitor of CYP 2C19.

CYP 1A2: Sertraline has no significant inhibitory effect on CYP 1A2 in vitro. Other serotoninergic drugs: Sertraline and drugs that enhance serotonin neurotransmission, such as tryptophan or fenfluramine, should be carefully considered to avoid possible pharmacodynamic interactions.

[Drug overdose]

There is evidence that sertraline still has a large safety margin when overdose. Sertraline has been reported to have taken over 13.5 g alone. Deaths from sertraline overdose have been reported, but most often occur in combination with other drugs and / or alcohol.

Therefore, any overdose should be actively treated. Symptoms of overdose include adverse reactions due to serotonin such as drowsiness, gastrointestinal upsets (such as nausea and vomiting), tachycardia, tremor, agitation, and dizziness. Rarely reported coma. Sertraline has no specific antidote. Open and keep the airways open to ensure adequate oxygen and ventilation. Activated carbon can be used with laxatives, and may be as effective or even more effective as emetic or gastric lavage. At the same time as symptomatic treatment and supportive therapy, it is recommended to monitor the heart and vital signs. Because sertraline has a large distribution volume, forced diuresis, dialysis, hemoperfusion, and transfusion therapy have no significant meaning.

[Drug toxicology]

Pharmacological effects Sertraline hydrochloride is a selective serotonin reuptake inhibitor. Its mechanism of action is related to the inhibition of serotonin reuptake by central neurons. Sertraline blocks serotonin uptake by human platelets at clinical doses. Studies suggest that sertraline is a potent and selective neuronal serotonin reuptake inhibitor with only a slight effect on norepinephrine and dopamine.

In vitro studies show that sertraline has an effect on adrenergic receptors (1, 2, ), cholinergic receptors, GABA receptors, dopaminergic receptors, histamine receptors, 5HT1B, 5HT2) or benzodiazepine receptors have no significant affinity. Antagonism of these receptors is believed to be related to the sedative effects, anticholinergic effects and cardiotoxicity of other psychiatric medications. Long-term administration of sertraline in animals can down-regulate norepinephrine receptors in the brain, which is consistent with the clinical effect of other antidepressants. Sertraline has no inhibitory effect on monoamine oxidase.

Clinical trials Depressive Disorders: A study was performed in patients who participated in an 8-week sertraline 50-200 mg / day open-label trial and treated effective depression clinics. These patients (N = 295) were randomized to sertraline 50-200 mg / day group or placebo group, and the 44-week double-blind trial was continued. The relapse rate of patients in the sertraline group was significantly reduced compared to the placebo group. Patients who completed the study had an average dose of 70 mg / day.

Obsessive-compulsive disorder: In a long-term study, patients who were enrolled in a 52-week single-blind trial of sertraline 50-200 mg / day and treated effectively were eligible for DSM-III-R diagnostic criteria for obsessive-compulsive disorder. These patients (n = 224) were randomly assigned to sertraline or placebo to continue treatment for 28 weeks, and the proportion of patients who fell off due to relapse or poor efficacy were observed. During the 28 weeks of continued treatment, the proportion of patients who relapsed or fell off due to poor response was significantly lower in the sertraline group than in the placebo group. This feature is shown in both male and female patients.

Toxicological studies of genotoxicity: bacterial mutation test, mouse lymphoma mutation test, in vivo mouse bone marrow and in vitro human lymphocyte genetic test results show that sertraline does not show genotoxicity with or without metabolic activation .

Reproductive toxicity: At a dose of 80 mg / kg (in mg / m2, 4 times the maximum human recommended dose of MRHD), a reduction in fertility was observed in one of two rat trials. Reproductive toxicity studies were performed in rats and rabbits at doses of 80 mg / kg / day and 40 mg / kg / day, respectively (approximately 4 times the maximum recommended human dose in mg / m2). No teratogenic effects were found at the doses. Fetal ossification was observed when sertraline was administered to pregnant rats and rabbits at doses of 10 mg / kg and 40 mg / kg, equivalent to 0.5 and 4 times the MRHD in mg / m2, respectively. delay. Sertraline was administered to female rats during late pregnancy and lactation, and the number of stillborn pups at a dose of 20 mg / kg and the number of pups died in the first 4 days after birth was increased. The weight of the pups was also reduced in the first 4 days after birth. The unaffected dose for young rats was 10 mg / kg. The reduction in the survival rate of the young rats is caused by sertraline exposure in the uterus. But the clinical significance of these effects is unclear.

Carcinogenicity: Carcinogenicity studies were performed on CD-1 mice and Long-Evans rats at doses of up to 40 mg / kg / day (in mg / m2, equivalent to approximately 1 and 2 times the MRHD, respectively) . At a dose of 10-40 mg / kg, male mice showed a dose-related increase in hepatic adenomas. No increase in hepatic adenomas or liver was observed in female mice or rats treated with the same administration. Increase in cell carcinoma. The spontaneous rate of hepatic adenoma in CD-1 mice is volatile, and the significance of this result to humans is unclear. 40 mg / kg female rats showed increased thyroid follicular adenoma without accompanying thyroid hyperplasia. Compared with the control group, the uterine adenoma of the rats in the 10-40 mg / kg administration group increased, but the correlation between the results and the drug was not clear.

Dependence: Animal studies have not shown the excitatory effect of this product or the potential for barbiturate-like (central inhibitor) abuse.

Pharmacokinetics

Sertraline is orally administered once daily to 50-200 mg in men. Sertraline exhibits pharmacokinetic characteristics that are directly proportional to the dose. After continuous administration for 14 days, the blood concentration of the human body reaches the peak (Cmax) for 4.5-8.4 hours. There were no significant differences between the pharmacokinetic parameters of adolescents and the elderly and adults from the age of 18-65. Sertraline has an average half-life of 22-36 hours. Consistent with the terminal elimination half-life, it was administered once a day and reached a steady-state concentration after 1 week. During this process, the concentration was doubled. Sertraline has a plasma protein binding rate of 98%. Animal experiment results show that sertraline has a large distribution volume. Sertraline is mainly metabolized first by the liver. The main metabolite N-desmethylsertraline in plasma has a significantly lower pharmacological activity in vitro than sertraline, which is about 1/20 of sertraline. There is no evidence to suggest that The antidepressant model has pharmacological activity in vivo, and its half-life is 62-104 hours. The final metabolites of sertraline and N-desmethylsertraline are excreted in equal amounts from feces and urine, and only a small amount (<0.2%) sertraline is excreted from the urine in its original form. Food had no significant effect on the bioavailability of sertraline tablets.

[Storage] Sealed and stored below 30 ° C.

[Packaging] box

[Validity] 60 months