Sertraline
When ATH: N06AB06
Characteristic.
The white crystalline powder. Poorly soluble in water and isopropyl alcohol, soluble in ethanol.
Pharmacological action.
Antidepressant.
Application.
Depression, obsessive-compulsive disorder.
Contraindications.
Hypersensitivity, childhood, lactation.
Pregnancy and breast-feeding.
Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)
Side effects.
Impaired consciousness, ataxia, incoordination, Hyper- and paresthesia, hyperkinesis, Hypo- and dyskinesia, generalized seizures, migraine, midriaz, nistagmo, dizziness, ptosis, giporefleksiя, sleep disturbance, aggressiveness, amnesia, apathy, depersonalization, emotional lability, euphoria, hallucinations, paranoid reactions, somnambulism, withdrawal, headache, hypertension or hypotension, tachycardia, kollaptoidnye state, swelling (incl. periorbital), bronchospasm, cough, dyspnoea, dysphagia, irritation of the gastrointestinal mucosa, hyperptyalism, glossitis, gipertrofiya right, ulcerative stomatitis, artralgii, dysmenorrhoea, enlargement and tenderness of the breast, anemia, lymphadenopathy, dizurija, allergic reactions.
Cooperation.
The joint appointment with MAO inhibitors cause hyperthermia, myoclonus, irritability, ažitaciû, disturbance of consciousness, delirium, rolling into a coma. Promotes cumulation (blocks biotransformation) H1-blockers (astemizol, terfenadine, cisapride) with lengthening of the QT interval and the possible development of fatal ventricular arrhythmias such as "pirouette". Increases plasma levels of free fraction (displace from its association with proteins) H2-blockers, tricyclic antidepressants, sulfonylurea derivatives, anxiolytics, varfarina, digoksina.
Overdose.
Symptoms: drowsiness, anxiety, nausea, vomiting, tachycardia, ECG changes.
Treatment: Activated carbon, gastric lavage, diurez, maintaining vital functions.
Dosing and Administration.
Inside, by 50 mg 1 once a day in the morning or evening; with no effect dose gradually (during 8 Sun) increases to a maximum daily - 200 mg per reception.
Precautions.
If the patient is taking antidepressants other groups (MAO inhibitors, tricyclic), the sertraline can be administered only through 2 Weeks after their withdrawal.
Cooperation
| Active substance | Description of interaction |
| Amitriptyline | FKV. FMR. It inhibits CYP2D6 and slows the biotransformation, may increase the plasma concentration of, increases (mutually) effect; the combined appointment is necessary to reduce the dose. |
| Warfarin | FKV. FMR: synergism. Against the background of sertraline (It competes for space due to the proteins) increased plasma levels of free fraction; can increase the effect. |
| Venlafaxine | FKV. It inhibits CYP2D6 and slows the biotransformation, can increase the plasma concentration; joint application requires dose reduction. |
| Diazepam | FKV. Against the backdrop of slowing sertraline biotransformation, increases the time to reach Cmax desmethyldiazepam, reduced clearance. |
| Digoxin | FKV. Against the backdrop of increased plasma levels of sertraline free fraction (It is displaced from its association with proteins), the effect can be enhanced. |
| Zolpidem | FKV. Against the background of sertraline (Night dose) much (in 1,5 times) With increasesmax and decreases (in 2 times) the time to achieve. |
| Imipramine | FKV. Inhibits CYP2D6, slows the biotransformation, may increase plasma concentrations and enhance the (mutually) effects, incl. negative; the combined appointment is necessary to reduce the dose. |
| Clomipramine | FKV. Inhibits CYP2D6, slows the biotransformation, Increases concentration of plasma, increases (mutually) effects, incl. negative; It requires the combined use of dose reduction. |
| Linezolid | FMR. Inhibits MAO and the background of sertraline can cause severe, sometimes fatal effects (delirium, coma); combined use is contraindicated. |
| Lithium carbonate | FKV. Against the backdrop of significant changes in the sertraline plasma levels and renal clearance were observed; It allowed the combined use, but with mandatory monitoring of lithium levels. |
| Lorazepam | FMR: synergism. Against the background of sertraline (It competes for space communications proteins) content increases the free fraction in plasma, dampening effect on the central nervous system. |
| Maprotilin | FKV. Inhibits CYP2D6, slows the biotransformation, Increases concentration of plasma, increases (mutually) effects, incl. negative; It requires the combined use of dose reduction. |
| Mirtazapine | FKV. FMR. Inhibits CYP2D6, slows the biotransformation, increases plasma concentration, increases (mutually) effects, incl. negative; the combined use should decrease the dose. |
| Moclobemide | FMR: synergism. Inhibits MAO and the background of sertraline may lead to severe, life-threatening reactions, including hyperthermia, rigidity, myoclonus, autonomic disorders, delirium and to whom; simultaneous and / or sequential use is contraindicated. |
| Paroxetine | FKV. FMR. Inhibits CYP2D6, slows the biotransformation, increases plasma concentration, increases (mutually) effects, incl. negative; In a joint application should decrease the dose. |
| Procarbazine | FMR: synergism. Inhibits MAO and the background of sertraline may lead to severe, life-threatening reactions, including hyperthermia, rigidity, myoclonus, autonomic disorders, delirium and to whom; simultaneous and / or sequential use is contraindicated. |
| Propafenone | FKV. CYP2D6 inhibitory activity and can increase the plasma concentration; with a joint appointment necessary dose adjustment. |
| Selegiline | FMR: synergism. Inhibits MAO and the background of sertraline can cause severe, sometimes fatal, reaction, including hyperthermia, rigidity, myoclonus, autonomic disorders, extreme agitation, progressing to delirium and to whom; joint and / or sequential use is contraindicated. |
| Sumatriptan | FMR: synergism. Against the background of sertraline may develop (isolated reports) weakness, hyperreflexia, incoordination. |
| Trazodone | FKV. FMR. Slows biotransformation (competes for CYP2D6), Increases concentration of plasma, increases (mutually) effects, incl. negative; with a joint appointment needed dose reduction. |
| Fluvoxamine | FKV. Inhibits CYP2D6, slows the biotransformation, increases plasma levels, increases (mutually) effects, incl. negative; joint application requires dose reduction. |
| Fluoxetine | FKV. Inhibits CYP2D6, slows the biotransformation, increases plasma levels, increases (mutually) effects, incl. negative; joint application requires dose reduction. |
| Citalopram | FKV. Inhibits CYP2D6, slows the biotransformation, increases plasma levels, increases (mutually) effects, incl. negative; joint application requires dose reduction. |
| Ethanol | It reinforces the negative effects; at the time of treatment should abandon spirits. |
