Universal reference book for medicines
Product name: ALEVAL

Active substance: sertraline

Type: Antidepressant

Manufacturer: Sun Pharmaceutical Industries (India)
Composition, form of production and packaging
The tablets covered with a film cover of
blue color, round, biconcave, with risk from one side;
on the kink - the core of white color.
1 tab.

sertraline hydrochloride 28 mg,

which corresponds to the content of sertraline 25 mg

Excipients: calcium hydrophosphate dihydrate, microcrystalline cellulose, corn starch, hypromellose 2910, talc purified, magnesium stearate, silicon dioxide colloidal anhydrous, crospovidone, indigocarmine.

Composition of the film membrane: hypromellose 2910, macrogol 6000, talc purified, titanium dioxide, indigocarmine.

14 pcs.
- Strips (1) - packs of cardboard.
14 pcs.
- Strips (2) - packs of cardboard.
The tablets covered with a film cover of blue color, round, biconcave, with risk from one side;
on the kink - the core of white color.
1 tab.

sertraline hydrochloride 56 mg,

which corresponds to the content of sertraline 50 mg

Excipients: calcium hydrophosphate dihydrate, microcrystalline cellulose, corn starch, hypromellose 2910, talc purified, titanium dioxide, magnesium stearate, silicon dioxide colloid, crospovidone, indigo carmine.

Composition of the film membrane: hypromellose 2910, macrogol 6000, talc purified, titanium dioxide, indigocarmine.

14 pcs.
- Strips (1) - packs of cardboard.
14 pcs.
- Strips (2) - packs of cardboard.
The tablets covered with a film cover of blue color, round, biconcave, with risk from one side;
on the kink - the core of white color.
1 tab.

sertraline hydrochloride 112 mg,

which corresponds to the content of sertraline 100 mg

Excipients: calcium hydrophosphate dihydrate, microcrystalline cellulose, corn starch, hypromellose 2910, talc purified, magnesium stearate, silicon dioxide colloid, crospovidone, indigo carmine.

Composition of the film membrane: hypromellose 2910, macrogol 6000, talc purified, titanium dioxide, indigocarmine.

14 pcs.
- Strips (1) - packs of cardboard.
14 pcs.
- Strips (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2013.

PHARMACHOLOGIC EFFECT

Antidepressant, selective serotonin reuptake inhibitor (5-HT).
Has a very weak effect on the re-uptake of norepinephrine and dopamine. In therapeutic doses, sertraline blocks the seizure of serotonin by human platelets.
Does not have a stimulating, sedative or anticholinergic action.
Sertraline does not have an affinity for m-cholinergic receptors, adrenergic receptors, serotonin, dopamine, histamine receptors, GABA or benzodiazepine receptors.
The antidepressant effect is noted towards the end of the second week of regular sertraline intake, whereas the maximum effect is achieved only after 6 weeks.Sertraline does not cause mental or physical drug dependence.

PHARMACOKINETICS

When ingested suction of sertraline from the gastrointestinal tract is significant, but it is slow.
C max in blood plasma is achieved 4.5-8.4 hours after taking the drug inside. C ss of sertraline in blood plasma is achieved within a week with a single daily intake. When taking the drug during meals, bioavailability increases by 25%, while the time to achieve C max decreases.
Distribution

The total binding of sertraline to plasma proteins is 98%.
V d > 20 l / kg.
Sertraline is excreted in breast milk.
Data on the ability of sertraline to penetrate through the BBB is not available.
Metabolism and excretion

Sertraline is extensively metabolized by "first passage" through the liver, undergoing N-demethylation.
Its main metabolite, N-desmethylsertralin, is less active than the parent compound. Metabolites are excreted in urine and feces in equal amounts. About 0.2% sertraline is excreted in the urine unchanged. T 1/2 of the drug is 22-36 hours and does not depend on age or sex. For N-desmethylsertraline, this value is 62-104 hours.
Pharmacokinetics in special clinical cases

T 1/2 sertraline and AUC increase when liver function is impaired.

Regardless of the severity of renal failure, the pharmacokinetics of sertraline does not change with its constant application.

Sertraline is not dialyzed.

INDICATIONS

- Depression of various etiologies (treatment and prevention);

- obsessive-compulsive disorder (OCD);

- panic disorder (with or without agoraphobia);

- Post-traumatic stress disorder (PTSD).

DOSING MODE

The drug is administered orally, 1 time / day in the morning or evening.
Sertraline tablets can be taken regardless of food intake.
With depression and OCD for adults, the initial dose is 50 mg 1 time / day.
The dose can be gradually increased at intervals not more than once a week to a maximum daily dose of 200 mg.
The initial therapeutic effect may appear within 7 days, but the overall effect is usually achieved in 2-4 weeks (or even for a longer time with OCD).
The maintenance dose for long-term treatment should be minimal effective with appropriate changes depending on the therapeutic effect.
In OCD for children aged 6 to 12 years, the initial dose is 25 mg.
After a week, you can increase the dose to 50 mg.
For children aged 12 to 17 years, the initial dose is 50 mg.
The daily dose can be gradually, not earlier than a week, increase from 50 mg to a maximum of 200 mg.In order to avoid an overdose, less weight should be taken into account in children compared to adults; with an increase in the dose of more than 50 mg / day, careful monitoring of this category of patients is necessary and at the first signs of an overdose, cancel the drug.
For panic disorders and PTSD, the drug is prescribed to adults .
The initial dose is 25 mg. Taking into account the tolerability, the dose can be gradually increased to a maximum value of 200 mg not more often than once a week by 25 mg, until the desired therapeutic effect is achieved.
A satisfactory therapeutic result is achieved usually after 7 days from the start of treatment.
However, in order to achieve the full therapeutic effect, the drug should be taken regularly for 2-4 weeks. The minimum dose providing the therapeutic effect is preserved as a supporting one in the future.
In elderly patients and in patients with impaired renal function, no special dose selection is required.

In patients with severe impairment of liver function , the dose of the drug should be reduced or the intervals between doses should be increased.

SIDE EFFECT

On the part of the digestive system: dyspeptic symptoms (flatulence, nausea, vomiting, diarrhea), abdominal pain, pancreatitis, dry mouth, hepatitis, jaundice, liver failure, decreased appetite until anorexia;
rarely - increased appetite.
From the cardiovascular system: heart palpitations, tachycardia, lowering blood pressure.

From the musculoskeletal system: arthralgia, muscle cramps.

From the side of the central nervous system and the peripheral nervous system: extrapyramidal disorders (dyskinesias, akathisia, gnashing of teeth, gait disturbance), involuntary muscular contractions, paresthesia, fainting, drowsiness, headache, migraine, dizziness, tremor, insomnia, anxiety, agitation, tremor, convulsions , manic disorders, hallucinations, euphoria, nightmares, psychosis, decreased libido, suicide, coma.

From the respiratory system: bronchospasm, yawning.

From the urinary system: enuresis, urinary incontinence or retention.

On the part of the reproductive system: violation of sexual function (delay ejaculation, decreased potency), galactorrhea, gynecomastia, menstrual disorder, priapism.

From the sense organs: visual impairment, mydriasis, periorbital edema, ringing in the ears.

On the part of the endocrine system: giperprolaktinemiya, hypothyroidism, syndrome of inadequate secretion of ADH.

Dermatological reactions: redness of the skin or flushes of blood to the face, alopecia, photosensitivity, purpura, increased sweating;
rarely Stevens-Johnson syndrome, toxic epidermal necrolysis.
Allergic reactions: urticaria, pruritus, anaphylactoid reaction, angioedema, edema of the face.

Laboratory test data: rarely, with prolonged use - there is an asymptomatic increase in the activity of transaminases in the blood serum.
The abolition of the drug in this case leads to a normalization of the activity of the enzymes. Possible development of leukopenia and thrombocytopenia, as well as an increase in the concentration of cholesterol in the serum.
Other: weakness, decrease or increase in body weight, bleeding (including nasal, gastrointestinal or hematuria), peripheral edema.

With the cessation of sertraline treatment, in rare cases - withdrawal syndrome: paresthesia, hypesthesia, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis that can not be distinguished from the symptoms of the underlying disease



CONTRAINDICATIONS

uncontrolled epilepsy;

- joint use with MAO inhibitors and pimozide (when replacing one drug with another, refrain from taking antidepressants within 14 days;

- joint use of sertraline with tryptophan or fenfluramine;

- Children under 6 years of age with depression and OCD;

- children and adolescents under 18 years of age with panic disorder and PTSD;

- Pregnancy;

- the period of lactation (breastfeeding);

- Hypersensitivity to the components of the drug.

With caution should be used in cases of organic brain diseases (including mental retardation), manic conditions, epilepsy, hepatic and / or kidney failure, weight loss, in children older than 6 years with depression and OCD.

PREGNANCY AND LACTATION

Contraindicated use of the drug during pregnancy and lactation (breastfeeding).

There are no controlled results of sertraline in pregnant women.

Women of reproductive age who are expected to be prescribed sertraline, should use effective methods of contraception.

Sertraline is excreted in breast milk.
There are no reliable data on the safety of the drug during the period of breastfeeding. If you need to use the drug during lactation, breastfeeding should be discontinued.
In the case of sertraline during pregnancy and during breastfeeding, some newborns whose mothers were taking antidepressants from the group of selective serotonin reuptake inhibitors, including serotonin, may have symptoms similar to the response to drug withdrawal.

APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be used in cases of kidney failure.

In patients with impaired renal function, no special dose selection is required.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution , use the drug for liver failure.

In patients with severe impairment of liver function, the dose of the drug should be reduced or the intervals between doses should be increased.

APPLICATION FOR CHILDREN

Contraindicated in children under 6 years of age with depression and OCD;
in children and adolescents under the age of 18 with panic disorder and PTSD.
In children and adolescents with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior.
Therefore, when prescribing Aleval or any other antidepressant drugs in children, adolescents and young people under 24, it is necessary to correlate the risk of suicide and the benefits of their use.
APPLICATION IN ELDERLY PATIENTS

In elderly patients, no special dose selection is required.

In elderly patients during treatment with sertraline, transient hyponatremia may occur.
Such a side effect is associated with the syndrome of inappropriate ADH secretion. With the development of symptomatic hyponatremia, sertraline should be withdrawn and an adequate therapy aimed at correcting the concentration of sodium in the blood should be prescribed. Signs and symptoms of hyponatremia include headache, impaired concentration, memory impairment, weakness and instability, which can lead to falls. In more severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest and death may occur.
SPECIAL INSTRUCTIONS

Aleval should not be administered together with MAO inhibitors, and also within 14 days after discontinuation of treatment with MAO inhibitors.
Similarly, after the withdrawal of the drug Aleval within 14 days, MAO inhibitors are not prescribed.
With the use of selective serotonin reuptake inhibitors (SSRIs), cases of the development of serotonin syndrome and NOS have been described, the risk of which increases when SSRIs are combined with other serotonergic agents (including triptans), as well as drugs that affect serotonin metabolism (v. including MAO inhibitors), antipsychotics and other dopamine receptor antagonists.
Manifestations of serotonin syndrome may include changes in mental status (in particular, agitation, hallucinations, coma), autonomic instability (tachycardia, blood pressure fluctuations, hyperthermia), changes in neuromuscular transmission (hyperreflexia, impaired coordination of movements) and / or gastrointestinal disturbances nausea, vomiting and diarrhea). Some manifestations of serotonin syndrome, incl. hyperthermia, rigidity of muscles, autonomic instability with the possibility of rapid fluctuations in the parameters of vital functions, as well as changes in mental status, can resemble the symptoms developing in the NSA.
Care should be taken when concurrently administering sertraline with other drugs that enhance serotonergic neurotransmission, such as tryptophan, fenfluramine or serotonin 5-HT receptor agonists.
Such a joint appointment should, if possible, be deleted, given the likelihood of pharmacodynamic interaction.
The experience of clinical studies, the purpose of which was to determine the optimal time required for transferring patients from taking other antidepressants and the drugs used in OCD to sertraline, is limited.
Care must be taken in this transition, especially with long-acting drugs, for example, with fluoxetine. The necessary interval between the cancellation of one SSRI and the start of taking another similar drug is not established.
It should be noted that in patients undergoing electroconvulsive therapy, there is no sufficient experience with sertraline.
The possible success or risk of such a combined treatment has not been studied.
There is no experience with sertraline in patients with convulsive syndrome, therefore, the use of the drug in patients with unstable epilepsy should be avoided, and patients with controlled epilepsy should be carefully observed during treatment.
When the seizures appear, the drug should be discontinued.
During clinical trials, before introduction of sertraline on the market, manic disorders were observed in approximately 0.4% of patients taking sertraline.
Cases of activation of manic disorders are also described in a small proportion of patients with manic-depressive psychosis receiving other antidepressant drugs or agents used in OCD.
Sertralin is actively biotransformed in the liver.
According to the pharmacokinetic study, with repeated sertraline administration in patients with stable cirrhosis of the liver of the lung course, an increase in T 1/2 of the drug was observed and an increase in C max and AUC was almost 3-fold compared to that in healthy people. There were no significant differences in binding to plasma proteins in the two groups. Use sertralin in patients with liver disease with caution. When appointing a drug to a patient with a violation of liver function, it is necessary to discuss the desirability of reducing the dose or increasing the interval between doses of the drug.
Sertraline in a small amount in unchanged form is excreted in the urine.
In patients with mild to moderate renal insufficiency (CK 30-60 ml / min) and patients with severe renal insufficiency (CK-10-29 ml / min or less), the pharmacokinetic parameters (C max and AUC 0-24 ) of sertraline for his repeated admission did not differ significantly from the control group. In all groups, T 1/2 of the drug was the same, as well as there was no difference in binding to plasma proteins. The results of this study suggest that, as expected with the slight renal excretion of sertraline, correction of its dose depending on the severity of renal failure is not required.
It is advisable to use caution when prescribing SSRIs in combination with drugs with established ability to change the functions of platelets, as well as in patients with hemorrhagic diseases in the anamnesis.

During treatment with sertraline, transient hyponatremia may occur.
It often develops in elderly patients, as well as when taking diuretics or a number of other drugs.Such a side effect is associated with the syndrome of inappropriate ADH secretion. With the development of symptomatic hyponatremia, sertraline should be withdrawn and an adequate therapy aimed at correcting the concentration of sodium in the blood should be prescribed. Signs and symptoms of hyponatremia include headache, impaired concentration, memory impairment, weakness and instability, which can lead to falls. In more severe cases, hallucinations, fainting, convulsions, coma, respiratory arrest and death may occur.
Risk of suicide attempts

Patients with depression are a risk group for suicidal attempts.
This danger persists until the development of remission. Therefore, from the beginning of treatment and until the optimal clinical effect is achieved, patients should be provided with permanent medical supervision.
In children, adolescents and young people under the age of 24 years with depression and other mental disorders antidepressants compared to placebo, increased the risk of suicidal thoughts or suicidal behavior. Therefore, when appointing the drug Aleval or any other antidepressant in children, adolescents and young adults under the age of 24 years should be related to the risk of suicide and benefit from their use. In short-term studies in people older than 24 years, the risk of suicide did not increase, and in people over 65 years is somewhat reduced. Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment with antidepressants of all patients should be monitored for early detection of faults or changes in behavior and suicidal tendencies.
Impact on the ability to drive vehicles and manage mechanisms

During treatment Aleval patients is not recommended to drive vehicles, special equipment or engage in activities associated with an increased risk.
OVERDOSE

Symptoms: severe symptoms of an overdose of sertraline is not revealed even in the appointment of the drug in high doses. However, in simultaneous administration with other drugs or possible severe poisoning with ethanol, up to coma and death. Overdose can cause serotonin syndrome with nausea, vomiting, somnolence, tachycardia, agitation, dizziness, agitation, diarrhea, sweating, myoclonus and hyperreflexia.
Treatment:No specific antidote. It requires intensive supportive care and constant monitoring of vital body functions. Induce vomiting is not recommended. Introduction of activated carbon may be more effective than gastric lavage. It is necessary to maintain airway patency. Sertraline has a large V d , in connection with this increased diuresis, dialysis, hemoperfusion or a blood transfusion may be ineffective.
DRUG INTERACTION

When the joint application of sertraline and pimozide pimozide concentration showed an increase when it is administered in a single low dose (2 mg). The increase pimozide concentration was not associated with any changes in EKG. Since the mechanism of this interaction is not known, and pimozide different narrow therapeutic range, concomitant use of pimozide and sertraline is contraindicated.
There have been serious complications, while the application of sertraline and MAO inhibitors (including selectively operable selegiline, reversible inhibitor of MAO type of action moclobemide and linezolid). Perhaps the development of serotonin syndrome (hyperthermia, rigidity, myoclonus, the lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), mental status changes, including increased irritability, expressed agitation, confusion, which in some cases can go into delirious state or someone). Similar complications, sometimes fatal, occur in the appointment of MAOI antidepressants during treatment, depressing reverse neuronal capture of monoamines or immediately after their withdrawal.
Combined use of sertraline and drugs that have a depressing effect on central nervous system, require careful monitoring.
During the period of treatment, alcohol is not allowed. There was no potentiation of carbamazepine, haloperidol, or phenytoin, and ethanol on cognitive and psychomotor performance in healthy people.
The joint appointment of indirect anticoagulants (warfarin) with sertraline been a 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.
When replacing one inhibitor of neuronal uptake of serotonin on the other there is no need to "washout period". However, you must be careful when changing the course of treatment. Avoid concomitant administration of tryptophan or fenfluramine with sertraline.
Sertraline causes minimal induction of microsomal liver enzymes. Simultaneous administration of sertraline and phenazone 200 mg leads to a significant decrease in T 1/2 phenazone, though it occurs in only 5% of cases.
If co-administration of sertraline does not alter the beta-adrenoceptor blocking effect of atenolol.
When administered sertraline in a daily dose of 200 mg of drug interaction with digoxin and glibenclamide is not revealed.
With prolonged use of sertraline at a dose of 200 mg / day has no clinically significant impact and does not inhibit the metabolism of phenytoin. In spite of this, we recommend careful monitoring of phenytoin concentrations in the blood plasma from the beginning of treatment with sertraline appropriate correction dose of phenytoin.
There have been very rare cases of weakness, increased tendon reflexes, confusion, anxiety and agitation in patients concurrently treated with sertraline and sumatriptan. We recommend monitoring patients who have clinical grounds related to the simultaneous reception of sertraline and sumatriptan.
Pharmacokinetic interaction
sertraline binds to plasma proteins. It is therefore necessary to consider the possibility of interaction with other drugs that bind to plasma proteins (e.g., diazepam and tolbutamide).
While the use of simultaneous application of cimetidine substantially reduces the clearance of sertraline.
Prolonged treatment with sertraline at a dose of 50 mg / day increases the concentration in plasma simultaneously used drugs in the metabolism which participates isoenzyme CYP2D6 (tricyclic antidepressant, antiarrhythmic drugs of class IC means - propafenone, flecainide).
In experimental studies on in vitro interaction was shown that the beta hydroxylation of endogenous cortisol, which occurs with the participation isozymes CYP3A3 / 4 as well as the metabolism of carbamazepine and terfenadine with prolonged use of sertraline at a dose of 200 mg / day are not changed. The concentration in the blood plasma tolbutamide, warfarin and phenytoin during long-term administration of sertraline in the same dose also varies. Therefore, it is believed that sertraline does not inhibit isoenzyme CYP2C9.
When concomitantly sertraline reduces tolbutamide clearance (necessary control of blood glucose).
Sertraline has no effect on the concentration of diazepam in blood serum, which indicates the absence of inhibition of the isozyme CYP2C19. According to in vitro studies, sertraline has virtually no effect or minimally inhibits isoenzyme CYP1A2.
Pharmacokinetics of lithium is not changed by concomitant administration of sertraline. However, the tremor occurs more often in their joint application. Special care is required in the combined use of sertraline (like other SSRIs) with drugs that affect serotonergic transmission (e.g., lithium).
TERMS OF RELEASE FROM PHARMACY

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