Zoloft: instructions for using the medicine, structure, Contraindications, how to use
Active material: Sertraline
When ATH: N06AB06
CCF: Antidepressant
ICD-10 codes (testimony): F31, F32, F33, F40, F41.0, F41.2, F42, F43
When CSF: 02.02.04
Manufacturer: PFIZER {Italy}
Zoloft: dosage form, composition and packaging
Pills, coated white, oblong, embossed with the inscription “Pfizer” one side, risks and embossed inscription “ZLT50” – the other side of the tablet.
| 1 tab. | |
| sertraline (the hydrochloride) | 50 mg |
Excipients: calcium phosphate, microcrystalline cellulose, hydroksypropyltsellyuloza, sodium starch glycolate, magnesium stearate, hydroxypropyl, polyethylene glycol, polysorbates, Titanium dioxide (E171).
14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
Pills, coated white, oblong, embossed with the inscription “Pfizer” on the one hand and “ZLT100” – the other side of the tablet.
| 1 tab. | |
| sertraline (the hydrochloride) | 100 mg |
Excipients: calcium phosphate, microcrystalline cellulose, hydroksypropyltsellyuloza, sodium starch glycolate, magnesium stearate, hydroxypropyl, polyethylene glycol, polysorbates, Titanium dioxide (E171).
14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
Zoloft: pharmachologic effect
Antidepressant, specific reuptake inhibitor (5-NT) neurons. It has very little effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, blocks the uptake of serotonin in human platelets. He has no incentive, sedative or anticholinergic action. Due to the selective inhibition of 5-HT capture, sertraline does not enhance adrenergic activity. Sertraline does not possesses kin muskarinovym holinoreceptoram, serotonin, dopamine, histamine, GABA-, benzodiazepinovыm and adrenoceptor.
Sertraline does not cause drug dependence, It does not cause an increase in body weight during chronic administration.
Zoloft: pharmacokinetics
Absorption
Is absorbed completely, but with a slower speed. At the same time taking the drug with food increases the bioavailability to 25%, Cmax increases by 25% and Tmax decreases.
In humans, sertraline at a dose of 50 to 200 mg 1 times / day for 14 days Cmax achieved through 4.5-8.4 h after administration. Cmax AUC and proportional dose of 50-200 mg sertraline 1 times / day for 14 days, thus revealed linear dependence pharmacokinetic.
Distribution
Plasma protein binding is about 98%.
Before the equilibrium through 1 week of treatment (welcome dose 1 time / day) there is approximately two-fold drug accumulation.
Metabolism
Sertraline undergoes biotransformation in the active “first pass” through the liver. The major metabolite, detected in plasma, – N-desmethylsertraline – significantly inferior (about 20 time) sertraline in vitro activity, and in fact is not active in models of depression in vivo.
Sertraline and N-desmethylsertraline actively biotransformiruyutsya.
Deduction
Average T1/2 sertraline for young and elderly men and women is 22-36 no. T1/2 N-desmetilsertralina varies 62-104 no. The metabolites are excreted in the feces and urine in equal amounts. Only a small portion of the drug (less 0.2%) excreted in the urine as unchanged.
Pharmacokinetics in special clinical situations
The pharmacokinetic profile in adolescents and the elderly is not significantly different from that of patients aged 18 to 65 years.
Displaying, pharmacokinetics of sertraline in children with OCD is similar to that of adults (Although in children the metabolism of sertraline is somewhat more active). However, given a lower weight in children (especially aged 6-12 years), the drug is recommended at a lower dose, to avoid excessive levels in plasma.
In patients with liver cirrhosis increased T1/2 drug and AUC compared with those in healthy individuals.
According to pharmacokinetic study, when multiple dose of sertraline in patients with stable cirrhosis easy flow, an increase in T1/2 drug and almost threefold increase in AUC (area under the concentration / time curve) and Cmax formulation as compared with those in healthy individuals. There were no significant differences in plasma protein binding in the 2 Group did not have.
In patients with renal insufficiency of mild to moderate severity (CC 30-60 ml / min) and patients with severe renal insufficiency (CC 10-29 ml / min) Pharmacokinetic Parameters (AUC0-24 and Cmax) sertraline with repeated his admission were not significantly different from control. In all the groups T1/2 the drug was similar, as well as there were no differences in plasma protein binding.
Zoloft: testimony
- depression of various etiologies (Treatment and Prevention);
- obsessive-compulsive disorder (OCD);
- panic disorder;
- post-traumatic stress disorder (PTSD);
- social phobia.
Zoloft: dosing regimen
Zoloft™ appointed 1 time / day morning or evening. Tablets can be taken regardless of the meal.
At Depression and OCD treatment is initiated with dosages 50 mg / day.
Treatment panic disorders, PTSD, and social phobia start with a dose 25 mg / day, which increased after 1 the week before 50 mg / day. Use of the drug for such a scheme can reduce the incidence of early adverse effects of treatment, characteristic of panic disorder.
With little effect use of sertraline in patients at a dose of 50 mg / day daily dose can be increased. The dose should be increased at intervals of not more than 1 once a week up to a maximum recommended dose, component 200 mg / day.
The initial effect can be observed through 7 days after treatment, However, the full effect is usually achieved through 2-4 of the week (or even for longer periods of time in OCD).
At conducting long-term maintenance therapy the drug is prescribed in the lowest effective dose, which subsequently is varied depending on the clinical effect.
In Children and adolescents 13-17 years, OCD sufferers, Zoloft treatment™ should start with a dose of 50 mg / day. In children 6-12 years OCD treatment starts with a dose of 25 mg / day, through 1 week it increased to 50 mg / day. Subsequently, with little effect dose can be increased in steps of 50 mg / day to 200 mg / day as needed. To avoid overdose, by increasing the dose more 50 mg is necessary to take into account the smaller body weight in children compared with adults. Change the dose at intervals of not less than 1 of the week.
IN old age The drug is used in the same doses, and that younger patients.
Patients with impaired liver function you should use lower doses or increase the interval between doses of the drug.
Patients with impaired renal function correction dose based on the severity of renal failure, does not require.
Zoloft: side effects
From the central and peripheral nervous system: headache, dizziness, tremor, insomnia (rarely – drowsiness), alarm, ažitaciâ, hypomania, craze, gait disturbance, blurred vision, extrapyramidal disorder (dyskinesias, akathisia), paresthesia, convulsions. Movement disorders were more common in patients with indications of their presence in history or concomitant use of antipsychotics.
When stopping treatment with sertraline are described rare cases of withdrawal. May appear paresthesia, gipestezii, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or psychotic symptoms, It is indistinguishable from the symptoms of the underlying disease.
From the body as a whole: increased perspiration, reduction or increase in body weight, weakness.
From the digestive system: decreased appetite (rarely – increase), up to anorexia, dry mouth, dyspepsia (flatulence, nausea, vomiting, diarrhea), abdominal pain.
On the part of the reproductive system: sexual dysfunction (delayed ejaculation, decreased libido, reduced potency, anorgazmija).
Cardio-vascular system: redness or flushing, bleeding (incl. Nasal), heartbeat.
Allergic reactions: hives, itch.
Dermatological reactions: skin rash; rarely – Stevens-Johnson syndrome, epidermal necrolysis.
On the part of the endocrine system: menstrual irregularities, galactorrhea, hyperprolactinemia.
From the laboratory parameters: transient hyponatremia (often develops in elderly patients, and when receiving diuretics or other drugs series. This side effect is associated with the syndrome of inappropriate secretion of ADH); rarely (prolonged use) – asymptomatic increase in transaminase activity in serum (removal of the drug leads to normalization of the activity of enzymes).
Zoloft: Contraindications
- simultaneous appointment of MAO inhibitors and pimozide;
- pregnancy;
- lactation (breast-feeding);
- Children up to age 6 years;
- hypersensitivity to sertraline.
FROM caution – with organic brain diseases (incl. mental retardation), epilepsy, hepatic and / or renal failure, marked reduction in body weight.
Zoloft: Pregnancy and lactation
Controlled application of the results of sertraline in pregnant women is not, therefore prescribe Zoloft™ Pregnancy can only, if the expected benefit to the mother outweighs the potential risk to the fetus.
Women of reproductive age during treatment with sertraline should use effective methods of contraception.
Sertraline found in human milk, therefore the use of Zoloft™ lactation is not recommended. Reliable data on safety of its use in this case no. If the use of the drug is necessary, then breastfeeding should be discontinued.
Zoloft: Special instructions
Zoloft™ It can be administered no earlier than 14 days after discontinuation of MAO inhibitors. MAO inhibitors may also be administered no earlier, than 14 days after discontinuation of Zoloft™.
Be careful while appointing Zoloft™ with other drugs, enhancing serotonergic neurotransmission, such as tryptophan, fenfluramine or 5-HT-agonistы. This joint appointment with the possibility to be ruled out, given the likelihood of pharmacodynamic interaction.
Caution should be used Zoloft™ with drugs, CNS depressants. Drinking alcohol and drugs, containing ethanol, during treatment with sertraline is prohibited.
Experience in clinical trials, the purpose of which was to determine the optimal time, required to transfer patients taking other antidepressant and antiobsessivnye funds for sertraline, limited. Care must be taken in such a transition, especially long-acting preparations, e.g. fluoxetine. The required interval between the cancellation of a selective serotonin reuptake inhibitor, and start taking a similar drug is not installed.
It should be noted, that patients, undergoing electroconvulsive therapy, sufficient experience with sertraline missing. Possible success or risk of such combined treatment has not been studied.
No experience in the application of sertraline in patients with convulsive disorders, so avoid its use in patients with unstable epilepsy, and patients with controlled epilepsy should be carefully monitored during treatment. When seizures drug should be discontinued.
Sick, Depressed, They are at risk for suicide attempts. This risk persists until remission of. Therefore, from the beginning of the treatment and to achieve optimal clinical response of the patients should establish a permanent medical supervision.
During clinical trials hypomania and mania have been observed in approximately 0.4% patients, sertraline. Cases activation of mania / hypomania have also been described in a small proportion of patients with manic-depressive psychosis, treated with antidepressant or other means antiobsessivnye.
Apply Zoloft™ in patients with liver disease should be cautious; is necessary to adjust the dosing regimen.
Use in Pediatrics
The safety and efficacy of sertraline established in children with OCD (aged 6 to 17 years).
Effects on ability to drive vehicles and management mechanisms
Appointment sertraline, usually, not accompanied by a violation of psychomotor functions. However, its use in conjunction with other drugs may impair attention and motor coordination. Therefore, during treatment with sertraline drive vehicles, special equipment or engage in activities, associated with an increased risk of, not recommended.
Zoloft: overdose
Severe symptoms of an overdose of sertraline were found even when using the drug in high doses. However, simultaneous administration with other drugs or alcohol may occur severe poisoning.
Symptoms: symptoms of serotonin syndrome: nausea, vomiting, drowsiness, tachycardia, ažitaciâ, dizziness, psychomotor agitation, diarrhea, increased perspiration, myoclonus and hyperreflexia.
Treatment: No specific antidotes. Require intensive supportive care, and constant monitoring of vital body functions. Induce vomiting is not recommended. Introduction of the activated carbon may be more effective, than gastric lavage. It is necessary to maintain an open airway. At the large volume of distribution of sertraline, In this regard, increased diuresis, dialysis, hemoperfusion or blood transfusions may be inconclusive.
Zoloft: drug interaction
In a joint application of sertraline and pimozide was an increase in pimozide levels when administered in a single low dose (2 mg). Increased pimozide levels were not associated with any ECG changes. Since the mechanism of this interaction is not known, and pimozide different narrow therapeutic index, concomitant use of sertraline and pimozide is contraindicated.
There have been severe complications, while the use of sertraline and MAOIs, including selective effect (selegiline) and reversible type of action (moclobemide). Perhaps the development of serotonin syndrome: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), altered mental status, including increased irritability, expressed excitement, confusion, which in some cases can go into delirious state, or who.
When coadministered with warfarin sertraline noted slight, but statistically significant increase in prothrombin time – In these cases, it is recommended to monitor the prothrombin time at the beginning of treatment with sertraline and after its cancellation.
Pharmacokinetic interactions
Sertraline is bound to plasma proteins. It is therefore necessary to consider the possibility of interactions with other drugs, binds to a protein (eg, diazepam and tolbutamide).
Concomitant use of cimetidine significantly reduces the clearance of sertraline.
Long-term treatment at a dose of sertraline 50 mg / day increases the concentration in plasma simultaneously used drugs, in the metabolism of which involved CYP2D6 isoenzyme (tricyclic antidepressants, antiarrhythmic drugs of class IC – propafenone, flekainid).
The experiments on the interaction in vitro have shown, What is being done isozymes CYP3A3 / 4 betagidroksilirovanie endogenous cortisol, as well as the metabolism of carbamazepine and long-term administration of terfenadine with sertraline dose 200 mg / day are not changed.
Plasma concentrations of tolbutamide, phenytoin and warfarin with long-term administration of sertraline in the same dose also varies. Thus, it can be concluded, that sertraline does not inhibit CYP2C9 isozyme.
However, while taking sertraline reduces the clearance of tolbutamide – requires monitoring of blood glucose.
Sertraline not affect the diazepam concentration in serum, which indicates the absence of inhibition of isoenzyme CYP2C19. According to in vitro studies, sertraline has virtually no effect or minimally inhibits the CYP1A2 isoenzyme.
The pharmacokinetics of lithium is not changed by concomitant administration of sertraline. However, the tremor occurs more often in their joint application. The combined use of sertraline medicine, affecting serotonergic transmission (eg, lithium), requires increased caution.
When replacing one inhibitor of neuronal uptake of serotonin on the other there is no need to “washout period”. However, caution is required when changes in treatment. Avoid concomitant administration of tryptophan or fenfluramine with sertraline.
Sertraline is a minimal induction of liver enzymes. Co-administration of sertraline at a dose of 200 mg antipyrine and results in a slight (5%), but significant decrease in the half-life of antipyrine.
If co-administration of sertraline does not alter beta-adrenoceptor blocking effect of atenolol.
When administered in a daily dose of sertraline 200 mg drug interactions with glibenclamide, and digoxin were found.
Long-term use of sertraline at a dose of 200 mg / day has no clinically significant effect and inhibits the metabolism of phenytoin. Despite this, we recommend careful monitoring of phenytoin levels in plasma of the appointment of sertraline with a corresponding adjustment of doses of phenytoin.
There have been very rare cases of weakness, increase of tendon reflexes, confusion, anxiety and agitation in patients concurrently treated with sertraline and sumatriptan. It is recommended to monitor patients, who have relevant clinical reasons for the simultaneous reception of sertraline and sumatriptan.
Zoloft: terms of dispensing from pharmacies
The drug is released under the prescription.
Zoloft: terms and conditions of storage
List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 5 years.
