Sertraline

Sertraline is an antidepressant drug belonging to the selective serotonin reuptake inhibitor class.

In the molecular structure of sertraline there are two chiral centers and only the S, S (+) isomer is marketed; the other R, R isomers; R, S; and S, R only slightly inhibit serotonin reuptake.

Sertraline - Chemical Structure

In addition, sertraline also has a weak action on the re-uptake of noradrenaline and dopamine.

Indications

For what it uses

The use of sertraline is indicated for the treatment of:

Depression;
Social anxiety disorder;
Disorder from panic attacks;
Post-traumatic stress syndrome;
Obsessive-compulsive disorder.

Warnings

Depression is often associated with an increase in suicidal thoughts, self-harm and suicide attempts. It is said that an improvement of these symptoms occurs immediately after taking sertraline, indeed it takes a certain period of time before the drug performs its therapeutic action. Therefore, it is necessary to monitor the patients until the aforementioned improvement occurs.

Sertraline can be used in children and adolescents under the age of 18 only for the treatment of obsessive-compulsive disorder.

Care should be taken with the administration of sertraline in patients with epilepsy or with a history of seizure disorders.

As sertraline is mainly metabolised in the liver, caution should be used when administering the drug in patients with pre-existing dysfunctions and / or liver disorders.

Abrupt discontinuation of sertraline therapy should be avoided due to withdrawal symptoms that may occur.

Sertraline should not be used in patients entering a manic phase.

Sertraline can alter the glycemic rate, therefore in patients suffering from diabetes - being treated with the drug - it may be necessary to adjust the dose of insulin and / or oral hypoglycemic agents.

Caution should be used in the administration of sertraline in patients with glaucoma.

Interactions

Sertraline should not be taken concomitantly with IMAO (monoamine oxidase inhibitors, such as - for example - moclobemide or selegiline ) due to the serious side effects that may occur. If it is necessary to start a MAOI-based therapy, a period of at least two weeks must elapse after the last intake of sertraline.

The concomitant use of sertraline and other drugs capable of increasing the serotonin signal (such as tryptophan ) should be avoided due to the serious side effects that may arise.

Concomitant use of sertraline and pimozide (an antipsychotic) should be avoided.

Much attention must be paid to the concomitant administration of sertraline and triptans (drugs used for the treatment of migraine), as they are also able to increase the serotonin signal.

The concomitant administration of sertraline and St. John's wort (or St. John's wort, a plant with antidepressant properties) should be avoided.

Sertraline is bound to plasma proteins, so it is necessary to pay attention to the possible concomitant administration of drugs also capable of binding to plasma proteins.

From some animal studies, it appears that sertraline is able to interact with insulin, therefore caution should be used when administering in diabetic patients.

The concomitant use of sertraline and TCA (tricyclic antidepressants) may increase sertraline plasma concentration up to toxic levels.

Cimetidine (a drug used in the treatment of gastric ulcer) is able to decrease the elimination rate of sertraline, thus causing potentially dangerous effects.

During concomitant administration of sertraline and anticoagulants (such as warfarin ), NSAIDs (non-steroidal anti-inflammatory drugs), acetylsalicylic acid and its derivatives, there may be an increased risk of bleeding.

The co-administration of sertraline and phenytoin (a drug used to treat epilepsy) can cause a decrease in the plasma concentration of the latter, thus favoring the appearance of convulsive crises.

A lot of attention is recommended in the concomitant administration of sertraline and lithium (a drug used to treat bipolar disorders).

A lot of caution should be used when administering sertraline in patients already treated with electroconvulsive therapy (TEC).

The concomitant use of sertraline and alcohol should be avoided.

Sertraline can affect the ability to drive or use machines.

In any case, before starting therapy with sertraline, you need to tell your doctor if you are taking any type of medication.

Side effects

Sertraline can trigger many adverse effects that vary in type and intensity from one patient to another. This is due to the sensitivity that each individual has towards the drug, therefore it is not said that all the side effects occur in the same way in every patient.

Below are the main side effects that may occur during sertraline therapy.

Gastrointestinal disorders

Sertraline therapy can cause nausea, vomiting, diarrhea or loose stools, dyspepsia, constipation, stomach upset, air in the stomach, esophageal problems, difficulty swallowing, increased salivation and mouth and tongue ulceration. Furthermore, sertraline can promote the onset of anorexia.

Pathologies of the central nervous system

Sertraline can cause drowsiness, dizziness, tremors, numbness and tingling, alterations in coordination, excessive movements, akathisia (a psychomotor syndrome characterized by the impossibility of remaining still) and lack of attention. In addition, sertraline can promote the appearance of convulsions.

Psychiatric disorders

Treatment with sertraline can cause various psychiatric disorders, including:

Insomnia;
Sleepwalking;
Depression;
Suicidal thoughts;
Anxiety;
Nervousness;
agitation;
Abnormal and terrifying dreams;
Hallucinations;
Mania;
Hypomania;
Suicidal ideas and behavior;
Excessive feeling of happiness;
Euphoria;
Lack of personal care;
Aggression;
Paranoia.

Renal and urinary disorders

Sertraline therapy can cause urination problems, increased urine excretion, increased urination frequency, nocturia (need to get up many times during the night to rest) or an inability to urinate.

Reproductive system disorders

Sertraline can cause decreased libido and sexual dysfunction in both sexes.

In men it can cause dysfunctions of the erection, alterations of the seminal fluid, redness of the penis and foreskin, delayed ejaculation and priapism (long and painful erection not accompanied by sexual excitement).

In women it can cause vaginal bleeding, vaginal dryness and galactorrhoea, that is the abnormal secretion of milk in women who are not breastfeeding.

Respiratory disorders

Sertraline can cause chest pains, breathing difficulties, wheezing, shortness of breath, bronchospasm and nose bleeds.

Blood and lymphatic system disorders

Treatment with sertraline can affect the hemolymphopoietic system (the system responsible for the synthesis of blood cells). This can cause thrombocytopenia (ie a reduction in the number of platelets in the bloodstream, with consequent increased susceptibility to abnormal bleeding and / or bleeding) and leukopenia (ie a decrease in the number of white blood cells in the bloodstream, with a consequent increased susceptibility to contraction of 'infections).

Furthermore, sertraline can cause purpura (appearance of red spots on skin, mucous membranes and organs due to the rupture of small blood vessels).

Endocrine disorders

Sertraline can cause gynecomastia (breast development in men), hypothyroidism and can favor the onset of the syndrome of inappropriate secretion of the antidiuretic hormone (SIADH).

Skin and subcutaneous tissue disorders

Sertraline therapy may promote the appearance of skin rashes, urticaria, pruritus, alopecia, erythema, photosensitivity reactions and toxic epidermal necrolysis.

Hepatobiliary disorders

Treatment with sertraline can promote the onset of liver failure, hepatitis and jaundice. Furthermore, it can cause changes in blood levels of transaminases.

Vascular pathologies

The intake of sertraline can give rise to tachycardia, hypertension, palpitations, peripheral edema and syncope (transient loss of consciousness).

Suspension symptoms

Following abrupt discontinuation of sertraline therapy, so-called withdrawal symptoms may occur. These symptoms are dizziness, agitation, anxiety, nausea, vomiting, tremor, confusion, palpitations, headache, diarrhea, emotional instability and visual disturbances.

Other side effects

Other side effects that can occur during the intake of sertraline are:

Allergic reactions in sensitive subjects;
Dry mouth;
Increased sweating;
Increased appetite;
Increase or loss of body weight;
Taste alterations;
Fatigue;
Hot flashes;
Temperature;
Myalgia and arthralgia;
Osteoarthritis;
Hemorrhoids;
Dripping nose;
Sore throat;
Ear pain;
Tinnitus (an auditory disorder characterized by the perception of noises such as whistling, buzzing, hissing, etc.);
Vision disorders;
Mydriasis (dilation of the pupil).

Overdose

The main symptoms of sertraline overdose are dizziness, nausea, vomiting, tachycardia, tremors, dizziness and agitation. In some cases, coma may also occur.

There is no specific antidote, so drug treatment is only symptomatic. Activated charcoal, osmotic laxatives and gastric lavage may be useful. In any case, if you suspect you have taken an excessive dose of medication, you must immediately inform your doctor and go to the nearest hospital.

Action mechanism

Sertraline is a selective inhibitor of serotonin reuptake and - as such - is able to inhibit the serotonin reuptake transporter itself (SERT).

Serotonin (5-HT) is synthesized within the presynaptic nerve termination and is released following certain stimuli. Once in the synaptic wall (the space between the presynaptic and postsynaptic termination), 5-HT interacts with its receptors on the postsynaptic termination in order to perform its biological function. After that, serotonin binds SERT and is brought back into the presynaptic termination.

Sertraline binds to SERT instead of 5-HT which therefore remains in the synaptic wall for a longer time. The prolonged permanence in the synaptic space causes serotonin to continue to interact with its postsynaptic receptors, which results in an increase in the serotonergic signal with consequent improvement in the pathologies treated.

Mode of Use - Posology

Sertraline is administered orally in the form of tablets. The tablets are available in different dosages.

The dosage of sertraline must be established by the doctor on an individual basis, depending on the type of pathology that must be treated and according to the patient's clinical picture. It should also be borne in mind that in patients suffering from dysfunctions and / or liver disorders it may be necessary to adjust the dose of the drug administered.

Below are the doses of sertraline usually used.

Depression and obsessive-compulsive disorder

The dose of sertraline usually administered is 50 mg of drug a day, which can be increased up to a maximum of 200 mg a day.

Social anxiety disorder, panic disorder and post-traumatic stress syndrome

The initial dosage of sertraline usually used is 25 mg of drug, which can be increased up to 50 mg. In any case, the daily dose should not exceed 200 mg.

Children and adolescents under the age of 18

In this category of patients, sertraline can be used exclusively for the treatment of obsessive-compulsive disorders. The daily dose usually administered ranges from 25 mg to 50 mg of drug, depending on the age of the patients. The maximum daily dose is 200 mg.

Pregnancy and breastfeeding

Sertraline can be used during pregnancy only if the doctor considers it indispensable. In fact, the drug can cause serious damage to the newborn, especially if it was taken by the mother during the last trimester of pregnancy. The newborn may develop a serious disease called persistent pulmonary hypertension that manifests itself with increased respiratory rate and a bluish complexion of the skin. In addition, symptoms may occur, such as: