Misol 14s 100 mg film-coated tablets
- $31.00
MISOL 50
of MISOL 100
the Trade name
of MISOL 50
of MISOL 100
the International unlicensed
name Sertraline Dosage Form
of the Tablet, film coated, 50 mg, 100 mg
Structure
One tablet contains
active agent – sertraline a hydrochloride of 55.954 mg or 111.908 mg, 50.00 mg and 100.000 mg of sertraline respectively,
excipients are equivalent: lactoses monohydrate, sodium of a kroskarmelloz, PVP K30 (Povidone), aerosil 200, cellulose microcrystalline PH 102, magnesium stearate,
structure of film cover No. 1:
Sepifilm LP 770: hydroksipropilmetiltsellyuloz (E464), cellulose microcrystalline (E460), stearic acid (E570), titan dioxide (E171).
OpisanieTabletki, an oval form, film coated white color, biconvex and with risky on one party (for a dosage of 50 mg).
Tablets, oblong shape, film coated white color, biconvex and with risky on one party (for a dosage of 100 mg).
Pharmacotherapeutic group
of Serotonin of the return capture inhibitors selection.
The ATX N06AB06 code
the Pharmacological
Pharmacokinetics At properties intake of sertraline to a dose from 50 to 200 mg once a day within 14 days the concentration of sertraline in plasma reaches peak (Cmax) in 4.5 - 8.4 h after reception. Average elimination half-life of sertraline makes about 26 h. Constant level of sertraline in blood plasma is reached approximately in 1 week of drug treatment (reception of a dose once a day). Cmax and the area under curve (AUC) of sertraline are proportional to a dose from 50 to 200 mg. According to elimination half-life at repeated intake of sertraline in a dose from 50 to 200 mg approximately twofold cumulation of drug in comparison with single dose is observed. At administration of drug at meal time the area under a curve slightly increases, and Cmax – increases by 25% before achievement of time of peak plasma concentration (Tmax), and then decreases from 8 h to 5.5 h.
Sertraline biotransformirutsya actively at the first passing through a liver. Main way of metabolism of N-desmetilirovaniye sertraline. N-desmetilsertralin – the main metabolite found in plasma with elimination half-life of 62 h to 104 h N-desmetilsertralin considerably concedes on activity to sertraline. Sertraline and N-desmetilsertralin are exposed to oxidizing deamination and consecutive restoration, hydroxylation and glyukuronidny conjugation. About 40 - 45% of the entered radioactive sertraline are removed with urine in 9 days. Invariable sertraline is not found in urine. About 40 - 45% of the entered radioactive sertraline are removed with a stake, including 12 - 14% of invariable sertraline.
Sertraline contacts proteins (98%) in concentration from 20 to 500 ng/ml.
The plasma clearance at elderly patients is 40% lower, than at young people.
A pharmacodynamics
the Mechanism of effect of drug MISOL is connected with inhibition of neuronalny serotonin reuptake (5HT). In clinical doses sertraline blocks serotonin reuptake in thrombocytes of the person. Drug is specific inhibitor of neuronalny serotonin reuptake and has very weak impact on the return capture of noradrenaline and dopamine. Has no affinity to adrenergic (an alpha - 1, an alpha - 2, a beta), cholinergic, GAMK-ergichesky, dofaminergichesky, gistaminergichesky, serotonergic (5HT 1A, 5HT 1B, 5HT 2) or to benzodiazepine receptors. Prolonged use leads to decrease of the activity of noradrenalinovy receptors of a brain, other clinically effective antidepressive and antiobsessivny drugs give similar effect. Sertraline does not inhibit a monoaminooxidase.
Does not cause physical and mental dependence.
- treatment of big depressive episodes, prevention of a recurrence of big depressive episodes
- the obsessivno-compulsive disorders (OCD) at adults and children from 6 years
- panic disorders with or without agarofobiya
- posttraumatic stressorny disorders (PTSD)
- social anxiety disorders
the Route of administration and a dosage
of MISOL appoint indications inside, once a day in the morning or in the evening.
Pill MISOL can be taken irrespective of meal.
Initial dose
Depression and ROC: treatment of MISOLOM it is necessary to begin 50 mg/days with a dose.
Panic disorders, PTSD and social anxiety disorders: treatment begin 25 mg/days which is increased in one week up to 50 mg/days with a dose. Use of drug according to such scheme allows to reduce the frequency of the early undesirable effects of treatment characteristic of panic disorder.
Selection of a dose
Depression, ROC, panic disorders, PTSD and social anxiety disorders: at insufficient effect of use of MISOLA for patients in a dose of 50 mg/days, its daily dose can be increased. The dose should be raised with an interval not more often than once a week to the maximum recommended dose making 200 mg/days.
The initial therapeutic effect can be shown within 7 days, however the full effect is usually reached in 2-4 weeks (or even during longer time at ROC).
Maintenance therapy
the Maintenance dose at long-term treatment has to be minimum effective – with its corresponding changes depending on therapeutic effect.
Use for treatment of children
Safety and efficiency of sertraline are established at children with ROC (aged from 6 up to 17 years). At the teenagers (at the age of 13-17 years) suffering from ROC, treatment of MISOLOM it is necessary to begin 50 mg/days with a dose. At children (at the age of 6-12 years) therapy of ROC begin 25 mg/days with a dose, in one week increase it to 50 mg/days. In the subsequent, at insufficient effect the dose can be increased in steps on 50 mg/days up to 200 mg/days as required. In clinical trials at patients with a depression and ROC aged from 6 up to 17 years it was shown that the MISOLA pharmacokinetic profile was similar to that at adults. However, to avoid overdose, at increase in a dose more than 50 mg it is necessary to take into account smaller body weight at children in comparison with adults.
Selection of a dose at children and teenagers
Elimination half-life of sertraline makes about 1 day therefore change of a dose has to happen to an interval not less than 1 week.
Use for treatment of elderly people
At advanced age drug is used in the same range of doses, as at more young people.
Use for patients with insufficiency of function of a liver
of MISOL should be applied with care at patients with liver diseases. At patients with a liver failure it is necessary to use smaller doses or to increase an interval between administrations of drug.
Use for patients with insufficiency of function of kidneys
Sertraline is substantially metabolized in an organism. In not changed view with urine only the insignificant amount of drug is removed. As expected taking into account insignificant renal excretion of sertraline, correction of its dose depending on severity of a renal failure it is not required.
Side effects
Very often
- insomnia, drowsiness, dizziness, a headache
- nausea, dryness in a mouth, diarrhea
- disturbance of an ejaculation
- fatigue
Often
- pharyngitis
- loss of appetite, increase in appetite
- a depression, depersonalization, nightmares, alarm, agitation, decrease the libido, a bruxism, paresthesia, a tremor, a hypertension, a dysgeusia, disturbance of attention
- a visual disturbance, tinnit
- heartbeat, inflows, yawning
- abdominal pain, vomiting, dyspepsia, a meteorism, a constipation
- skin rash, a hyperhidrosis
- myalgia
- sexual dysfunction, erectile dysfunction
Infrequently
- upper respiratory tract infections, rhinitis
- hallucinations, euphoria, apathy, disturbance of thinking
- a spasm, involuntary muscular contractions, an incoordination, a hyperkinesia, amnesia, a hypesthesia, speech disorders, confusion of consciousness a hypokinesia, hypotonia, hyporeflexia
- postural dizziness, migraine, ear pain
- tachycardia, hypertensia
- a bronchospasm, dispnoe, cough, epistaxis
- an esophagitis, a dysphagy, hypersalivation, an eructation
- periorbital swelled, a purpura, an alopecia, cold sweat, xeroderma, urticaria
- an osteoarthritis, muscle weakness, a dorsodynia, convulsive twitchings of muscles
- a nocturia, an ischuria, a polyuria, a pollakiuria, urination disorders
- vaginal bleeding, disturbance of sexual function at women
- an indisposition, a fever, temperature increase, thirst
- increase in body weight, decrease in body weight
Is rare
- a diverticulitis, a gastroenteritis
- average otitis
- a neoplasm
- a limfoadenopatiya
- a hypercholesterolemia, a hypoglycemia
- medicinal dependence, psychotic disorders, aggression, paranoid reaction, suicide thoughts / behavior, a hypomania, a mania, a premature ejaculation,
- a coma, a choreoathetosis, dyskinesia, a hyperesthesia
- disturbance of a slezootdeleniye, scotoma, a diplopia, photophobia, a hyphema, a mydriasis, an exophthalmos, a ptosis, conjunctivitis, a nystagmus
- a myocardial infarction, bradycardia, cardial disorders, peripheral ischemia
- a laryngospasm, a hyperventilation, hypoventilation, a stridor, a dysphonia, a hiccups
- stomatitis, language ulcers, a hyperplasia of gums, disturbances from teeth, the aggravated caries, a glossitis, a melena
- abnormal liver functions
- dermatitis, violent dermatitis, follicular rash, disturbance of structure of hair, an abnormal smell of skin, an acne, eczema, a hypertrichosis, decolouration of skin, pustulous rash
- a hyperacusia
- disturbances from bones
- urine incontinence
- a menorrhagia, an atrophic vulvovaginitis, a balanoposthitis, genital discharges, a priapism, a galactorrhoea
- hernia
- decrease in medicinal tolerance, disturbance of gait
- increase in activity of ALT, nuclear heating plant
- a vazodilatation
With an unknown frequency
- a leukopenia, thrombocytopenia, anemia
- anaphylactoid reactions, allergic reactions
- a giperprolaktinemiya
- a hypothyroidism, a syndrome of inadequate secretion of antidiuretic hormone
- a hyponatremia, diabetes, a hyperglycemia
- paranoia, motive disorders, including extrapyramidal symptoms, such as hyperkinesia, hypertension, gnash teeth, disturbance of gait, sinkope
- a serotonergic syndrome or the malignant antipsychotic syndrome in certain cases connected with combined use of serotonergic medicines that includes agitation concern, sweating, diarrhea, fever, hypertensia, tachycardia, rigidity, an akathisia, psychomotor disturbances, a bespokoynost, disorders of vision
- gastrointestinal bleedings, a hamaturia
- pancreatitis
- jaundice, a liver failure
- Stephens-Johnson's syndrome, an epidermal necrolysis, a Quincke's disease, a face edema, photosensitivity, an itching
- an arthralgia, muscular spasms
- a gynecomastia, disturbances of a menstrual cycle
- peripheral swell
- dysfunction of thrombocytes
of the Contraindication
- hypersensitivity to sertraline or other components of drug
- neurologic disturbances (including a delay of intellectual
development)
- maniacal states
- epilepsy
- decrease in body weight
- simultaneous use with inhibitors monoaminooksidaza (IMAO) and with Pimozidum
- intolerance of a galactose, insufficiency of Lappa lactase, malabsorption of a glucose/galactose
- pregnancy and the period of a lactation
- children's age up to 6 years
Medicinal interactions
Combined use of drug MISOL with:
- the drugs contacting proteins of blood plasma (for example, warfarin, digitoxin), can lead to shift in plasma concentration, shown in the form of side reaction in view of the fact that MISOL also strongly contacts proteins of blood plasma. In researches of comparison of a prothrombin time and AUC (the area under a curve) (0-120 h) at intake of warfarin (in a dose of 0.75 mg/kg) to and on the expirations of 21 days after intake of sertraline (50-200 mg/days) or placebo, increase in a prothrombin time by 8% of rather basic line for the sertraline compared to 1% reduction for placebo was observed (r
- Cimetidinum, causes significant increase in AUC (50%), Cmax (24%) and elimination half-life (26%) of sertraline at their combined use. The clinical value of these changes is unknown,
- with diazepam the reduction of clearance of sertraline by 32% of rather basic line of diazepam is observed. The clinical value is unknown,
- lithium drugs, it is recommended to control plasma concentration of lithium at a concomitant use of sertraline and, if necessary, to adjust a dose of drugs of lithium,
Experience of clinical trials which purpose was a definition of the optimum time necessary for the translation of patients from reception of other antidepressive funds for sertraline is limited. It is necessary to be careful upon such transition, especially from drugs of long action, for example, from fluoxetine: the necessary interval between cancellation of one selective serotonin reuptake inhibitor (SSRI) and the beginning of intake of other similar drug is not established,
- with the drugs which are metabolized P450 2D6 (tricyclic antidepressants and antiarrhytmic drugs 1C of a class, such as propafenon and flekainid), MISOL, as well as many other antidepressants, inhibits biochemical activity of enzyme P450 2D6 cytochrome (debrizokvingidroksilaza) and at the expense of it can increase concentration in plasma of other drugs which biotransformirutsya by this enzyme,
- sumatriptany, extremely exceptional cases of emergence of weakness, increase in tendon jerks, confusion of consciousness, alarm and excitement at the patients who were at the same time accepting SIOZS and sumatriptan are celebrated. Observation of patients who have corresponding clinical bases for a concomitant use of a sumatriptan and SIOZS (to tsitalopra, fluoxetine, fluvoksamin, paroksetin) is recommended,
- tricyclic antidepressants, extent of interaction of SIOZS with tricyclic antidepressants (TCA) can cause the clinical problems depending on degree of inhibition and pharmacokinetics of SIOZS. However it is necessary to be careful at co-administration of TCA and drug MISOL as the last can suppress metabolism of TCA. At a concomitant use of TCA and MISOL it is necessary to control plasma concentration of TCA and to reduce TCA dose,
- tolbutamide, MISOL causes considerable reduction (to 16% of the basic line) clearance of tolbutamide. MISOL slightly influences linking with plasma proteins or tolbutamide distribution volume, assuming that the lowered clearance – result of change of metabolism of drug. The clinical value of lowering of clearance of tolbutamide is unknown,
- atenolol, drug MISOL at single dose in a dose of 100 mg
does not affect beta and adrenoceptor blocking activity of atenolol,
- digoxin, reception of MISOL does not affect plasma concentration of digoxin and its renal clearance,
- with Pimozidum, increase in levels of Pimozidum at its single appointment in a low dose (2 mg) was noted. Increase in levels of Pimozidum was not connected with any changes in the ECG. As, the mechanism of this interaction is not known, and Pimozidum differs in the narrow therapeutic index, the concomitant use of Pimozidum and sertraline is contraindicated.
- with monoamine oxidase inhibitors (IMAO) heavy complications at simultaneous use of sertraline and IMAO are noted (including IMAO which are selectively operating (selegilin) and with reversible type of action (moklobemid). Development of a serotoninovy syndrome is possible. Similar complications, sometimes from the death, arise when assigning IMAO against the background of treatment by the antidepressants oppressing neuronalny capture of monoamines or right after their cancellation.
- with selective inhibitors of the return neuronalny serotonin reuptake and IMAO arise: a hyperthermia, rigidity, a myoclonus, lability of the autonomic nervous system (fast fluctuations of parameters of a respiratory and cardiovascular system), changes of the mental status, including acrimony, the significant excitement, confusion of consciousness which in certain cases can pass into a delirious state or a coma.
- with medicines, oppressing the central nervous system and ethanol requires close attention and also consumption of the alcoholic drinks and drugs containing alcohol during treatment by sertraline is forbidden,
- with drugs, influencing serotonergic transfer: when replacing one inhibitor of neuronalny serotonin reuptake by another, there is no need for "the washing period". However it is required to be careful at treatment changes of course. It is necessary to avoid joint prescribing of tryptophane or a fenfluramin with sertraline.
- with induction of microsomal enzymes of a liver sertraline causes the minimum induction of enzymes of a liver. Co-administration of sertraline in a dose of 200 mg and antipyrine leads to small (5%), but to reliable reduction of elimination half-life of antipyrine,
- with glibenclamide and digoxin: at administration of sertraline in a daily dose of 200 mg of medicinal interaction with these drugs it is not revealed.
- with Phenytoinum: prolonged use of sertraline in a dose of 200 mg/days does not make clinically significant impact and does not suppress Phenytoinum metabolism. Despite this, careful observation of Phenytoinum level in blood plasma is recommended from the moment of prescribing of sertraline with the corresponding correction of doses of Phenytoinum.
Special
instructions MISOL should not be applied in a combination with MAO inhibitors or within 14 days after the treatment termination by MAO inhibitor. Similarly, it is possible to appoint MAO inhibitor not earlier, than, at least, in 14 days after cancellation MISOLA.
Other serotonergic means – it is necessary to be careful at co-administration of sertraline with other drugs strengthening serotonergic neurotransmission such as, tryptophane, fenflyuramin or 5-NT-agonisty. Similar joint appointment at an opportunity has to be excluded, considering the probability of pharmakodinamichesky interaction.
During the MISOL drug treatment the intake of alcohol and other alcohol-containing drugs is forbidden.
In the researches conducted at children and adults with a depression and other mental disturbances it is established that antidepressants increase risk of development of suicidal thoughts and behavior. In this regard all patients accepting antidepressants have to be carefully examined regarding clinical deterioration, tendency to suicides and unusual changes in behavior, especially within the first several months of a course of medicinal therapy or during correction of a dose of drug both increase, and reduction. The decision which is usually made in that case leads to change of the therapeutic mode up to drug withdrawal, especially at such patients at whom considerable deterioration in a depression is observed.
Such symptoms as concern, agitation, acute disturbing condition with reaction of panic, insomnia, irritability, hostile aggression, impulsiveness, an akathisia (psychomotor concern), a hypomania, a mania were found in the patients with a depression and other mental disorders accepting antidepressants. Though the causal relationship between manifestations of these symptoms and deterioration in a depression or suicidal impulses is not established yet, such symptoms can already be predecessors of suicidal manifestations.
The family and personnel which are looking after patients with a depression or other mental disorders, accepting antidepressants, have to be in advance warned about need to watch carefully patients, especially at manifestation of symptoms of agitation, irritability, unusual changes in behavior and the symptoms stated above and immediately to note them.
During therapy of the patients with a depression inclined to a suicide, within the first several weeks it can not be observed noticeable improvement in this connection such patients need to be observed carefully. The prescription on MISOL has to be written in the minimum quantity in order to avoid risk of overdose.
If the decision to stop treatment was made, medicinal therapy has to be minimized so quickly as far as it is possible, but with confidence that such sudden cancellation will not be connected with development of certain somatic and psychopathological symptoms.
Depressions of various etiology can be initial manifestation of bipolar disorders. It is usually observed (though it is not established in check tests) when therapy by antidepressants of separate disorders can lead to increase in a likelihood of developing the mixed / maniacal disorders at the patients inclined to bipolar psychoses. In this regard before an initiation of treatment antidepressants patients with symptoms of a depression have to be carefully examined for definition of presence of risk of developing bipolar disorders, such inspection has to include the detailed psychiatric anamnesis, including data on family cases of a suicide, bipolar disorders and depressions. MISOL is not shown for treatment of bipolar disorders.
Safety profile at the MISOL drug treatment is identical at patients with a depression of various etiology, ROC, panic disorders, a PTSD and a social phobia.
Drug MISOL was not studied at patients with a convulsive syndrome therefore it is necessary to avoid its use for patients with unstable epilepsy, and patients with controlled epilepsy should be observed carefully during treatment. At appearance of spasms in all cases drug needs to be cancelled. It should be noted that at the patients who are exposed to electroconvulsive therapy, sufficient experience of use of sertraline is absent. Possible success or risk of the similar combined treatment is not studied.
MISOL promotes reduction in serum of uric acid approximately for 7%. The clinical importance of such weak uricosuric effect is unknown.
The Serotoninovy syndrome and a malignant antipsychotic syndrome
At use of the selective serotonin reuptake inhibitors (SSRI) are described cases of development of a serotoninovy syndrome (CC) and the malignant antipsychotic syndrome (MAS) which risk increases at combination of SIOZS with other serotonergic means (including triptanes) and also the drugs influencing serotonin metabolism (including monoamine oxidase inhibitors), antipsychotic means and other antagonists of dopamine receptors. Changes of the mental status (in particular, agitation, hallucinations, a coma), vegetative lability (tachycardia, fluctuations of arterial blood pressure, a hyperthermia), changes of neuro and muscular transfer (hyperreflexia, a lack of coordination of movements) and/or disturbances from digestive tract (nausea, vomiting and diarrhea) can be manifestations of CC. Some manifestations of CC, including, the hyperthermia, rigidity of muscles, vegetative lability with a possibility of fast fluctuations of parameters of the vital functions and also changes of the mental status, can remind the symptomatology developing at ZNS. Monitoring of patients regarding development of clinical manifestations of CC and ZNS is necessary.
Transition from other selective serotonin reuptake inhibitors (SSRI), antidepressants or antiobsessivny drugs. Experience of clinical trials which purpose was a definition of the optimum time necessary for the translation of patients from reception of other antidepressive and antiobsessivny funds for sertraline is limited. It is necessary to be careful upon such transition, especially with it is long the operating drugs, for example, from fluoxetine. The necessary interval between cancellation of one selective serotonin reuptake inhibitor and the beginning of intake of other similar drug is not established.
Activation of a mania/hypomania. The hypomania and a mania were observed approximately at 0.4% of the patients receiving sertraline. Cases of activation of a mania/hypomania are described also at a small part of the patients with manic-depressive psychosis receiving other antidepressive or antiobsessivny means.
Pathological bleedings / hemorrhages
It is recommended to be careful when prescribing selective serotonin reuptake inhibitors in combination with the drugs having the established ability to change of functions of thrombocytes and also at patients with hemorrhagic diseases in the anamnesis.
The hyponatremia
during treatment by sertraline can arise a tranzitorny hyponatremia. It develops at elderly patients more often and also at intake of diuretics or some other drugs. The similar side effect is connected with a syndrome of inadequate secretion of antidiuretic hormone. At development of a symptomatic hyponatremia sertraline it is necessary to cancel and appoint the adequate therapy directed to correction of level of sodium in blood. Signs and symptoms of a hyponatremia include a headache, disturbance of concentration of attention, memory disturbance, weakness and instability that can lead to falling. In more hard cases there can be hallucinations, a faint, spasms, a coma, an apnoea and death.
A withdrawal
At the treatment termination by sertraline development of a withdrawal, especially is possible if the termination is sharp. Risk of developing a withdrawal can depend on several factors, including duration of therapy and a dose, the period of reduction of a dose. It was reported about cases of development of the following symptoms after the termination of treatment of SIOZS: dizziness, touch disturbances, including paresthesias, sleep disorders, including insomnia, concern, nausea and/or vomiting, a tremor, the increased perspiration, a headache, diarrhea, emotional instability, irritability and visual disorders. Generally some patients had symptoms of moderate weight, however, they were serious intensity. Symptoms usually pass during the first several days after the treatment termination. Patients who carelessly
missed reception of the next dose of drug have very rare messages of symptoms of a withdrawal. In order to avoid a withdrawal the dose of sertraline has to decrease gradually within several weeks or months.
Schizophrenia:
At the patients having schizophrenia psychotic signs can worsen.
Diabetes
At patients with diabetes at use of SIOZS it is regularly necessary to check glucose level in blood. If necessary dose adjustment of insulin or oral hypoglycemic means has to be carried out.
An akathisia / psychomotor concern
Use of sertraline was connected with development of psychomotor concern which can clinically be similar to the akathisia which is characterized subjectively unpleasant or the disturbing restlessness and requirement to move, often accompanied inability to sit or stop. These symptoms are most probable within the first several weeks after administration of drug. To patients at whom these signs, increase in a dose of drug develop can be dangerous.
The liver failure
Sertraline biotransformirutsya actively in a liver. According to a pharmacokinetic research, at multiple dose of sertraline at patients with stable cirrhosis of an easy course the increase in elimination half-life of drug and almost triple increase in AUC (the area under a curve concentration/time) and the maximum concentration of drug in comparison with those at healthy people was observed. Essential differences in linking with proteins of plasma in two groups were not. At patients with a chronic liver failure of an easy course at administration of drug of MISOL the decrease in clearance leading to increase in elimination half-life was observed. Therefore it is necessary to use drug MISOL at patients with liver diseases with care. If drug is appointed to the patient from the liver broken by function, it is necessary to discuss expediency of a dose decline or increase in an interval between administration of drug.
The renal failure
Sertraline is exposed to active biotransformation therefore in not changed view with urine he is brought in insignificant quantity. At patients with a slight and moderate renal failure (clearance of creatinine of 30-60 ml/min.) and patients with moderate or heavy degree with a renal failure (clearance of creatinine of 10-29 ml/min.) pharmacokinetic parameters (AUC0-24 and Cmax) drug at its multiple dose significantly did not differ from group of control. In all groups the elimination half-life of drug was identical, is equal as there were no differences in linking with proteins of plasma. Results of this research demonstrate to what, as expected taking into account insignificant excretion of sertraline, correction of its dose depending on severity of a renal failure is not required.
Use in pediatrics
of ROC the only indication at which appoint MISOL to children. The profile of safety is comparable to that at treatment of adult patients with SURROUNDING. The efficiency of administration of drug of MISOL at children with a depression or panic disorders is not established in controlled researches. The same as at reception of other SIOZS, reception MISOLA causes a loss of appetite and loss of weight. At long purpose of SIOZS children need to control periodically during treatment the body weight and growth of patients. Safety and efficiency of administration of drug at children are younger than 6 years is not established.
Use for elderly people
about 800 elderly people took part In clinical trials of sertraline 65 or 75 years are more senior. Patients of elderly and younger age had an identical profile and frequency of side reactions.
Pregnancy and a lactation
of Controlled results of use of drug MISOL for pregnant women are not present therefore it is possible to appoint drug at pregnancy only if the expected advantage for mother exceeds potential risk for a fruit.
It is unknown whether it is found and if it is found out, then in what quantity, sertraline or its metabolites in breast milk. If prescribing of drug is necessary, then breastfeeding should be stopped.
Features of influence on ability to run vehicles or other potentially dangerous mechanisms
of the Research showed that drug MISOL does not affect psychomotor function. Nevertheless, antidepressive or antiobsessivny means can worsen the intellectual or physical activity necessary for performance of potentially dangerous functions of type of driving of the car or control of mechanisms what it is necessary to warn the patient about. MISOL should not be appointed with benzodiazepines or other tranquilizers to the drivers or persons operating potentially dangerous mechanisms.
Overdose
overdose cases at monotherapy by drug MISOL in a dose up to 6 g Were reported. Death cases at overdose of drug MISOL in combination with other medicines and/or alcohol are known.
Symptoms: uneasiness, drowsiness, changes on the ECG, a mydriasis, nausea, vomiting, tachycardia.
Treatment: there is no specific antidote. Ensuring normal passability of airways (oxygenation and ventilation of the lungs), gastric lavage, purpose of emetic HP, activated carbon with sorbitol is required. Control of function of heart, liver and other vitals and performing symptomatic and maintenance therapy are necessary.
The artificial diuresis, dialysis, hemoperfusion and exchange blood transfusion are ineffective.
Form of release and packing
of the Tablet, film coated 50 mg, 100 mg.
On 10 or 14 tablets (for a dosage of 50 mg) and 5 or 7 tablets (for a dosage of 100 mg) in blister strip packaging from a film of white not transparent PVH/PE/PVDH and aluminum foil.
On 3 (on 10 tablets) or 1 or 2 (on 14 tablets) planimetric packing (for a dosage of 50 mg), 2 or 4 (on 7 tablets) or 6 planimetric packs (on 5 tablets) (for a dosage of 100 mg) together with the instruction for medical use in the state and Russian languages place in a pack cardboard with the hologram of firm – producer.
To Store storage conditions at a temperature not above 25 °C, in the dry, protected from light place.
A period of storage
2 years
Prescription status
According to the prescription
Republic of Kazakhstan JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika Producer
Almaty, Shevchenko St. 162 E.
To develop
of MISOL 100
the Trade name
of MISOL 50
of MISOL 100
the International unlicensed
name Sertraline Dosage Form
of the Tablet, film coated, 50 mg, 100 mg
Structure
One tablet contains
active agent – sertraline a hydrochloride of 55.954 mg or 111.908 mg, 50.00 mg and 100.000 mg of sertraline respectively,
excipients are equivalent: lactoses monohydrate, sodium of a kroskarmelloz, PVP K30 (Povidone), aerosil 200, cellulose microcrystalline PH 102, magnesium stearate,
structure of film cover No. 1:
Sepifilm LP 770: hydroksipropilmetiltsellyuloz (E464), cellulose microcrystalline (E460), stearic acid (E570), titan dioxide (E171).
OpisanieTabletki, an oval form, film coated white color, biconvex and with risky on one party (for a dosage of 50 mg).
Tablets, oblong shape, film coated white color, biconvex and with risky on one party (for a dosage of 100 mg).
Pharmacotherapeutic group
of Serotonin of the return capture inhibitors selection.
The ATX N06AB06 code
the Pharmacological
Pharmacokinetics At properties intake of sertraline to a dose from 50 to 200 mg once a day within 14 days the concentration of sertraline in plasma reaches peak (Cmax) in 4.5 - 8.4 h after reception. Average elimination half-life of sertraline makes about 26 h. Constant level of sertraline in blood plasma is reached approximately in 1 week of drug treatment (reception of a dose once a day). Cmax and the area under curve (AUC) of sertraline are proportional to a dose from 50 to 200 mg. According to elimination half-life at repeated intake of sertraline in a dose from 50 to 200 mg approximately twofold cumulation of drug in comparison with single dose is observed. At administration of drug at meal time the area under a curve slightly increases, and Cmax – increases by 25% before achievement of time of peak plasma concentration (Tmax), and then decreases from 8 h to 5.5 h.
Sertraline biotransformirutsya actively at the first passing through a liver. Main way of metabolism of N-desmetilirovaniye sertraline. N-desmetilsertralin – the main metabolite found in plasma with elimination half-life of 62 h to 104 h N-desmetilsertralin considerably concedes on activity to sertraline. Sertraline and N-desmetilsertralin are exposed to oxidizing deamination and consecutive restoration, hydroxylation and glyukuronidny conjugation. About 40 - 45% of the entered radioactive sertraline are removed with urine in 9 days. Invariable sertraline is not found in urine. About 40 - 45% of the entered radioactive sertraline are removed with a stake, including 12 - 14% of invariable sertraline.
Sertraline contacts proteins (98%) in concentration from 20 to 500 ng/ml.
The plasma clearance at elderly patients is 40% lower, than at young people.
A pharmacodynamics
the Mechanism of effect of drug MISOL is connected with inhibition of neuronalny serotonin reuptake (5HT). In clinical doses sertraline blocks serotonin reuptake in thrombocytes of the person. Drug is specific inhibitor of neuronalny serotonin reuptake and has very weak impact on the return capture of noradrenaline and dopamine. Has no affinity to adrenergic (an alpha - 1, an alpha - 2, a beta), cholinergic, GAMK-ergichesky, dofaminergichesky, gistaminergichesky, serotonergic (5HT 1A, 5HT 1B, 5HT 2) or to benzodiazepine receptors. Prolonged use leads to decrease of the activity of noradrenalinovy receptors of a brain, other clinically effective antidepressive and antiobsessivny drugs give similar effect. Sertraline does not inhibit a monoaminooxidase.
Does not cause physical and mental dependence.
- treatment of big depressive episodes, prevention of a recurrence of big depressive episodes
- the obsessivno-compulsive disorders (OCD) at adults and children from 6 years
- panic disorders with or without agarofobiya
- posttraumatic stressorny disorders (PTSD)
- social anxiety disorders
the Route of administration and a dosage
of MISOL appoint indications inside, once a day in the morning or in the evening.
Pill MISOL can be taken irrespective of meal.
Initial dose
Depression and ROC: treatment of MISOLOM it is necessary to begin 50 mg/days with a dose.
Panic disorders, PTSD and social anxiety disorders: treatment begin 25 mg/days which is increased in one week up to 50 mg/days with a dose. Use of drug according to such scheme allows to reduce the frequency of the early undesirable effects of treatment characteristic of panic disorder.
Selection of a dose
Depression, ROC, panic disorders, PTSD and social anxiety disorders: at insufficient effect of use of MISOLA for patients in a dose of 50 mg/days, its daily dose can be increased. The dose should be raised with an interval not more often than once a week to the maximum recommended dose making 200 mg/days.
The initial therapeutic effect can be shown within 7 days, however the full effect is usually reached in 2-4 weeks (or even during longer time at ROC).
Maintenance therapy
the Maintenance dose at long-term treatment has to be minimum effective – with its corresponding changes depending on therapeutic effect.
Use for treatment of children
Safety and efficiency of sertraline are established at children with ROC (aged from 6 up to 17 years). At the teenagers (at the age of 13-17 years) suffering from ROC, treatment of MISOLOM it is necessary to begin 50 mg/days with a dose. At children (at the age of 6-12 years) therapy of ROC begin 25 mg/days with a dose, in one week increase it to 50 mg/days. In the subsequent, at insufficient effect the dose can be increased in steps on 50 mg/days up to 200 mg/days as required. In clinical trials at patients with a depression and ROC aged from 6 up to 17 years it was shown that the MISOLA pharmacokinetic profile was similar to that at adults. However, to avoid overdose, at increase in a dose more than 50 mg it is necessary to take into account smaller body weight at children in comparison with adults.
Selection of a dose at children and teenagers
Elimination half-life of sertraline makes about 1 day therefore change of a dose has to happen to an interval not less than 1 week.
Use for treatment of elderly people
At advanced age drug is used in the same range of doses, as at more young people.
Use for patients with insufficiency of function of a liver
of MISOL should be applied with care at patients with liver diseases. At patients with a liver failure it is necessary to use smaller doses or to increase an interval between administrations of drug.
Use for patients with insufficiency of function of kidneys
Sertraline is substantially metabolized in an organism. In not changed view with urine only the insignificant amount of drug is removed. As expected taking into account insignificant renal excretion of sertraline, correction of its dose depending on severity of a renal failure it is not required.
Side effects
Very often
- insomnia, drowsiness, dizziness, a headache
- nausea, dryness in a mouth, diarrhea
- disturbance of an ejaculation
- fatigue
Often
- pharyngitis
- loss of appetite, increase in appetite
- a depression, depersonalization, nightmares, alarm, agitation, decrease the libido, a bruxism, paresthesia, a tremor, a hypertension, a dysgeusia, disturbance of attention
- a visual disturbance, tinnit
- heartbeat, inflows, yawning
- abdominal pain, vomiting, dyspepsia, a meteorism, a constipation
- skin rash, a hyperhidrosis
- myalgia
- sexual dysfunction, erectile dysfunction
Infrequently
- upper respiratory tract infections, rhinitis
- hallucinations, euphoria, apathy, disturbance of thinking
- a spasm, involuntary muscular contractions, an incoordination, a hyperkinesia, amnesia, a hypesthesia, speech disorders, confusion of consciousness a hypokinesia, hypotonia, hyporeflexia
- postural dizziness, migraine, ear pain
- tachycardia, hypertensia
- a bronchospasm, dispnoe, cough, epistaxis
- an esophagitis, a dysphagy, hypersalivation, an eructation
- periorbital swelled, a purpura, an alopecia, cold sweat, xeroderma, urticaria
- an osteoarthritis, muscle weakness, a dorsodynia, convulsive twitchings of muscles
- a nocturia, an ischuria, a polyuria, a pollakiuria, urination disorders
- vaginal bleeding, disturbance of sexual function at women
- an indisposition, a fever, temperature increase, thirst
- increase in body weight, decrease in body weight
Is rare
- a diverticulitis, a gastroenteritis
- average otitis
- a neoplasm
- a limfoadenopatiya
- a hypercholesterolemia, a hypoglycemia
- medicinal dependence, psychotic disorders, aggression, paranoid reaction, suicide thoughts / behavior, a hypomania, a mania, a premature ejaculation,
- a coma, a choreoathetosis, dyskinesia, a hyperesthesia
- disturbance of a slezootdeleniye, scotoma, a diplopia, photophobia, a hyphema, a mydriasis, an exophthalmos, a ptosis, conjunctivitis, a nystagmus
- a myocardial infarction, bradycardia, cardial disorders, peripheral ischemia
- a laryngospasm, a hyperventilation, hypoventilation, a stridor, a dysphonia, a hiccups
- stomatitis, language ulcers, a hyperplasia of gums, disturbances from teeth, the aggravated caries, a glossitis, a melena
- abnormal liver functions
- dermatitis, violent dermatitis, follicular rash, disturbance of structure of hair, an abnormal smell of skin, an acne, eczema, a hypertrichosis, decolouration of skin, pustulous rash
- a hyperacusia
- disturbances from bones
- urine incontinence
- a menorrhagia, an atrophic vulvovaginitis, a balanoposthitis, genital discharges, a priapism, a galactorrhoea
- hernia
- decrease in medicinal tolerance, disturbance of gait
- increase in activity of ALT, nuclear heating plant
- a vazodilatation
With an unknown frequency
- a leukopenia, thrombocytopenia, anemia
- anaphylactoid reactions, allergic reactions
- a giperprolaktinemiya
- a hypothyroidism, a syndrome of inadequate secretion of antidiuretic hormone
- a hyponatremia, diabetes, a hyperglycemia
- paranoia, motive disorders, including extrapyramidal symptoms, such as hyperkinesia, hypertension, gnash teeth, disturbance of gait, sinkope
- a serotonergic syndrome or the malignant antipsychotic syndrome in certain cases connected with combined use of serotonergic medicines that includes agitation concern, sweating, diarrhea, fever, hypertensia, tachycardia, rigidity, an akathisia, psychomotor disturbances, a bespokoynost, disorders of vision
- gastrointestinal bleedings, a hamaturia
- pancreatitis
- jaundice, a liver failure
- Stephens-Johnson's syndrome, an epidermal necrolysis, a Quincke's disease, a face edema, photosensitivity, an itching
- an arthralgia, muscular spasms
- a gynecomastia, disturbances of a menstrual cycle
- peripheral swell
- dysfunction of thrombocytes
of the Contraindication
- hypersensitivity to sertraline or other components of drug
- neurologic disturbances (including a delay of intellectual
development)
- maniacal states
- epilepsy
- decrease in body weight
- simultaneous use with inhibitors monoaminooksidaza (IMAO) and with Pimozidum
- intolerance of a galactose, insufficiency of Lappa lactase, malabsorption of a glucose/galactose
- pregnancy and the period of a lactation
- children's age up to 6 years
Medicinal interactions
Combined use of drug MISOL with:
- the drugs contacting proteins of blood plasma (for example, warfarin, digitoxin), can lead to shift in plasma concentration, shown in the form of side reaction in view of the fact that MISOL also strongly contacts proteins of blood plasma. In researches of comparison of a prothrombin time and AUC (the area under a curve) (0-120 h) at intake of warfarin (in a dose of 0.75 mg/kg) to and on the expirations of 21 days after intake of sertraline (50-200 mg/days) or placebo, increase in a prothrombin time by 8% of rather basic line for the sertraline compared to 1% reduction for placebo was observed (r
- Cimetidinum, causes significant increase in AUC (50%), Cmax (24%) and elimination half-life (26%) of sertraline at their combined use. The clinical value of these changes is unknown,
- with diazepam the reduction of clearance of sertraline by 32% of rather basic line of diazepam is observed. The clinical value is unknown,
- lithium drugs, it is recommended to control plasma concentration of lithium at a concomitant use of sertraline and, if necessary, to adjust a dose of drugs of lithium,
Experience of clinical trials which purpose was a definition of the optimum time necessary for the translation of patients from reception of other antidepressive funds for sertraline is limited. It is necessary to be careful upon such transition, especially from drugs of long action, for example, from fluoxetine: the necessary interval between cancellation of one selective serotonin reuptake inhibitor (SSRI) and the beginning of intake of other similar drug is not established,
- with the drugs which are metabolized P450 2D6 (tricyclic antidepressants and antiarrhytmic drugs 1C of a class, such as propafenon and flekainid), MISOL, as well as many other antidepressants, inhibits biochemical activity of enzyme P450 2D6 cytochrome (debrizokvingidroksilaza) and at the expense of it can increase concentration in plasma of other drugs which biotransformirutsya by this enzyme,
- sumatriptany, extremely exceptional cases of emergence of weakness, increase in tendon jerks, confusion of consciousness, alarm and excitement at the patients who were at the same time accepting SIOZS and sumatriptan are celebrated. Observation of patients who have corresponding clinical bases for a concomitant use of a sumatriptan and SIOZS (to tsitalopra, fluoxetine, fluvoksamin, paroksetin) is recommended,
- tricyclic antidepressants, extent of interaction of SIOZS with tricyclic antidepressants (TCA) can cause the clinical problems depending on degree of inhibition and pharmacokinetics of SIOZS. However it is necessary to be careful at co-administration of TCA and drug MISOL as the last can suppress metabolism of TCA. At a concomitant use of TCA and MISOL it is necessary to control plasma concentration of TCA and to reduce TCA dose,
- tolbutamide, MISOL causes considerable reduction (to 16% of the basic line) clearance of tolbutamide. MISOL slightly influences linking with plasma proteins or tolbutamide distribution volume, assuming that the lowered clearance – result of change of metabolism of drug. The clinical value of lowering of clearance of tolbutamide is unknown,
- atenolol, drug MISOL at single dose in a dose of 100 mg
does not affect beta and adrenoceptor blocking activity of atenolol,
- digoxin, reception of MISOL does not affect plasma concentration of digoxin and its renal clearance,
- with Pimozidum, increase in levels of Pimozidum at its single appointment in a low dose (2 mg) was noted. Increase in levels of Pimozidum was not connected with any changes in the ECG. As, the mechanism of this interaction is not known, and Pimozidum differs in the narrow therapeutic index, the concomitant use of Pimozidum and sertraline is contraindicated.
- with monoamine oxidase inhibitors (IMAO) heavy complications at simultaneous use of sertraline and IMAO are noted (including IMAO which are selectively operating (selegilin) and with reversible type of action (moklobemid). Development of a serotoninovy syndrome is possible. Similar complications, sometimes from the death, arise when assigning IMAO against the background of treatment by the antidepressants oppressing neuronalny capture of monoamines or right after their cancellation.
- with selective inhibitors of the return neuronalny serotonin reuptake and IMAO arise: a hyperthermia, rigidity, a myoclonus, lability of the autonomic nervous system (fast fluctuations of parameters of a respiratory and cardiovascular system), changes of the mental status, including acrimony, the significant excitement, confusion of consciousness which in certain cases can pass into a delirious state or a coma.
- with medicines, oppressing the central nervous system and ethanol requires close attention and also consumption of the alcoholic drinks and drugs containing alcohol during treatment by sertraline is forbidden,
- with drugs, influencing serotonergic transfer: when replacing one inhibitor of neuronalny serotonin reuptake by another, there is no need for "the washing period". However it is required to be careful at treatment changes of course. It is necessary to avoid joint prescribing of tryptophane or a fenfluramin with sertraline.
- with induction of microsomal enzymes of a liver sertraline causes the minimum induction of enzymes of a liver. Co-administration of sertraline in a dose of 200 mg and antipyrine leads to small (5%), but to reliable reduction of elimination half-life of antipyrine,
- with glibenclamide and digoxin: at administration of sertraline in a daily dose of 200 mg of medicinal interaction with these drugs it is not revealed.
- with Phenytoinum: prolonged use of sertraline in a dose of 200 mg/days does not make clinically significant impact and does not suppress Phenytoinum metabolism. Despite this, careful observation of Phenytoinum level in blood plasma is recommended from the moment of prescribing of sertraline with the corresponding correction of doses of Phenytoinum.
Special
instructions MISOL should not be applied in a combination with MAO inhibitors or within 14 days after the treatment termination by MAO inhibitor. Similarly, it is possible to appoint MAO inhibitor not earlier, than, at least, in 14 days after cancellation MISOLA.
Other serotonergic means – it is necessary to be careful at co-administration of sertraline with other drugs strengthening serotonergic neurotransmission such as, tryptophane, fenflyuramin or 5-NT-agonisty. Similar joint appointment at an opportunity has to be excluded, considering the probability of pharmakodinamichesky interaction.
During the MISOL drug treatment the intake of alcohol and other alcohol-containing drugs is forbidden.
In the researches conducted at children and adults with a depression and other mental disturbances it is established that antidepressants increase risk of development of suicidal thoughts and behavior. In this regard all patients accepting antidepressants have to be carefully examined regarding clinical deterioration, tendency to suicides and unusual changes in behavior, especially within the first several months of a course of medicinal therapy or during correction of a dose of drug both increase, and reduction. The decision which is usually made in that case leads to change of the therapeutic mode up to drug withdrawal, especially at such patients at whom considerable deterioration in a depression is observed.
Such symptoms as concern, agitation, acute disturbing condition with reaction of panic, insomnia, irritability, hostile aggression, impulsiveness, an akathisia (psychomotor concern), a hypomania, a mania were found in the patients with a depression and other mental disorders accepting antidepressants. Though the causal relationship between manifestations of these symptoms and deterioration in a depression or suicidal impulses is not established yet, such symptoms can already be predecessors of suicidal manifestations.
The family and personnel which are looking after patients with a depression or other mental disorders, accepting antidepressants, have to be in advance warned about need to watch carefully patients, especially at manifestation of symptoms of agitation, irritability, unusual changes in behavior and the symptoms stated above and immediately to note them.
During therapy of the patients with a depression inclined to a suicide, within the first several weeks it can not be observed noticeable improvement in this connection such patients need to be observed carefully. The prescription on MISOL has to be written in the minimum quantity in order to avoid risk of overdose.
If the decision to stop treatment was made, medicinal therapy has to be minimized so quickly as far as it is possible, but with confidence that such sudden cancellation will not be connected with development of certain somatic and psychopathological symptoms.
Depressions of various etiology can be initial manifestation of bipolar disorders. It is usually observed (though it is not established in check tests) when therapy by antidepressants of separate disorders can lead to increase in a likelihood of developing the mixed / maniacal disorders at the patients inclined to bipolar psychoses. In this regard before an initiation of treatment antidepressants patients with symptoms of a depression have to be carefully examined for definition of presence of risk of developing bipolar disorders, such inspection has to include the detailed psychiatric anamnesis, including data on family cases of a suicide, bipolar disorders and depressions. MISOL is not shown for treatment of bipolar disorders.
Safety profile at the MISOL drug treatment is identical at patients with a depression of various etiology, ROC, panic disorders, a PTSD and a social phobia.
Drug MISOL was not studied at patients with a convulsive syndrome therefore it is necessary to avoid its use for patients with unstable epilepsy, and patients with controlled epilepsy should be observed carefully during treatment. At appearance of spasms in all cases drug needs to be cancelled. It should be noted that at the patients who are exposed to electroconvulsive therapy, sufficient experience of use of sertraline is absent. Possible success or risk of the similar combined treatment is not studied.
MISOL promotes reduction in serum of uric acid approximately for 7%. The clinical importance of such weak uricosuric effect is unknown.
The Serotoninovy syndrome and a malignant antipsychotic syndrome
At use of the selective serotonin reuptake inhibitors (SSRI) are described cases of development of a serotoninovy syndrome (CC) and the malignant antipsychotic syndrome (MAS) which risk increases at combination of SIOZS with other serotonergic means (including triptanes) and also the drugs influencing serotonin metabolism (including monoamine oxidase inhibitors), antipsychotic means and other antagonists of dopamine receptors. Changes of the mental status (in particular, agitation, hallucinations, a coma), vegetative lability (tachycardia, fluctuations of arterial blood pressure, a hyperthermia), changes of neuro and muscular transfer (hyperreflexia, a lack of coordination of movements) and/or disturbances from digestive tract (nausea, vomiting and diarrhea) can be manifestations of CC. Some manifestations of CC, including, the hyperthermia, rigidity of muscles, vegetative lability with a possibility of fast fluctuations of parameters of the vital functions and also changes of the mental status, can remind the symptomatology developing at ZNS. Monitoring of patients regarding development of clinical manifestations of CC and ZNS is necessary.
Transition from other selective serotonin reuptake inhibitors (SSRI), antidepressants or antiobsessivny drugs. Experience of clinical trials which purpose was a definition of the optimum time necessary for the translation of patients from reception of other antidepressive and antiobsessivny funds for sertraline is limited. It is necessary to be careful upon such transition, especially with it is long the operating drugs, for example, from fluoxetine. The necessary interval between cancellation of one selective serotonin reuptake inhibitor and the beginning of intake of other similar drug is not established.
Activation of a mania/hypomania. The hypomania and a mania were observed approximately at 0.4% of the patients receiving sertraline. Cases of activation of a mania/hypomania are described also at a small part of the patients with manic-depressive psychosis receiving other antidepressive or antiobsessivny means.
Pathological bleedings / hemorrhages
It is recommended to be careful when prescribing selective serotonin reuptake inhibitors in combination with the drugs having the established ability to change of functions of thrombocytes and also at patients with hemorrhagic diseases in the anamnesis.
The hyponatremia
during treatment by sertraline can arise a tranzitorny hyponatremia. It develops at elderly patients more often and also at intake of diuretics or some other drugs. The similar side effect is connected with a syndrome of inadequate secretion of antidiuretic hormone. At development of a symptomatic hyponatremia sertraline it is necessary to cancel and appoint the adequate therapy directed to correction of level of sodium in blood. Signs and symptoms of a hyponatremia include a headache, disturbance of concentration of attention, memory disturbance, weakness and instability that can lead to falling. In more hard cases there can be hallucinations, a faint, spasms, a coma, an apnoea and death.
A withdrawal
At the treatment termination by sertraline development of a withdrawal, especially is possible if the termination is sharp. Risk of developing a withdrawal can depend on several factors, including duration of therapy and a dose, the period of reduction of a dose. It was reported about cases of development of the following symptoms after the termination of treatment of SIOZS: dizziness, touch disturbances, including paresthesias, sleep disorders, including insomnia, concern, nausea and/or vomiting, a tremor, the increased perspiration, a headache, diarrhea, emotional instability, irritability and visual disorders. Generally some patients had symptoms of moderate weight, however, they were serious intensity. Symptoms usually pass during the first several days after the treatment termination. Patients who carelessly
missed reception of the next dose of drug have very rare messages of symptoms of a withdrawal. In order to avoid a withdrawal the dose of sertraline has to decrease gradually within several weeks or months.
Schizophrenia:
At the patients having schizophrenia psychotic signs can worsen.
Diabetes
At patients with diabetes at use of SIOZS it is regularly necessary to check glucose level in blood. If necessary dose adjustment of insulin or oral hypoglycemic means has to be carried out.
An akathisia / psychomotor concern
Use of sertraline was connected with development of psychomotor concern which can clinically be similar to the akathisia which is characterized subjectively unpleasant or the disturbing restlessness and requirement to move, often accompanied inability to sit or stop. These symptoms are most probable within the first several weeks after administration of drug. To patients at whom these signs, increase in a dose of drug develop can be dangerous.
The liver failure
Sertraline biotransformirutsya actively in a liver. According to a pharmacokinetic research, at multiple dose of sertraline at patients with stable cirrhosis of an easy course the increase in elimination half-life of drug and almost triple increase in AUC (the area under a curve concentration/time) and the maximum concentration of drug in comparison with those at healthy people was observed. Essential differences in linking with proteins of plasma in two groups were not. At patients with a chronic liver failure of an easy course at administration of drug of MISOL the decrease in clearance leading to increase in elimination half-life was observed. Therefore it is necessary to use drug MISOL at patients with liver diseases with care. If drug is appointed to the patient from the liver broken by function, it is necessary to discuss expediency of a dose decline or increase in an interval between administration of drug.
The renal failure
Sertraline is exposed to active biotransformation therefore in not changed view with urine he is brought in insignificant quantity. At patients with a slight and moderate renal failure (clearance of creatinine of 30-60 ml/min.) and patients with moderate or heavy degree with a renal failure (clearance of creatinine of 10-29 ml/min.) pharmacokinetic parameters (AUC0-24 and Cmax) drug at its multiple dose significantly did not differ from group of control. In all groups the elimination half-life of drug was identical, is equal as there were no differences in linking with proteins of plasma. Results of this research demonstrate to what, as expected taking into account insignificant excretion of sertraline, correction of its dose depending on severity of a renal failure is not required.
Use in pediatrics
of ROC the only indication at which appoint MISOL to children. The profile of safety is comparable to that at treatment of adult patients with SURROUNDING. The efficiency of administration of drug of MISOL at children with a depression or panic disorders is not established in controlled researches. The same as at reception of other SIOZS, reception MISOLA causes a loss of appetite and loss of weight. At long purpose of SIOZS children need to control periodically during treatment the body weight and growth of patients. Safety and efficiency of administration of drug at children are younger than 6 years is not established.
Use for elderly people
about 800 elderly people took part In clinical trials of sertraline 65 or 75 years are more senior. Patients of elderly and younger age had an identical profile and frequency of side reactions.
Pregnancy and a lactation
of Controlled results of use of drug MISOL for pregnant women are not present therefore it is possible to appoint drug at pregnancy only if the expected advantage for mother exceeds potential risk for a fruit.
It is unknown whether it is found and if it is found out, then in what quantity, sertraline or its metabolites in breast milk. If prescribing of drug is necessary, then breastfeeding should be stopped.
Features of influence on ability to run vehicles or other potentially dangerous mechanisms
of the Research showed that drug MISOL does not affect psychomotor function. Nevertheless, antidepressive or antiobsessivny means can worsen the intellectual or physical activity necessary for performance of potentially dangerous functions of type of driving of the car or control of mechanisms what it is necessary to warn the patient about. MISOL should not be appointed with benzodiazepines or other tranquilizers to the drivers or persons operating potentially dangerous mechanisms.
Overdose
overdose cases at monotherapy by drug MISOL in a dose up to 6 g Were reported. Death cases at overdose of drug MISOL in combination with other medicines and/or alcohol are known.
Symptoms: uneasiness, drowsiness, changes on the ECG, a mydriasis, nausea, vomiting, tachycardia.
Treatment: there is no specific antidote. Ensuring normal passability of airways (oxygenation and ventilation of the lungs), gastric lavage, purpose of emetic HP, activated carbon with sorbitol is required. Control of function of heart, liver and other vitals and performing symptomatic and maintenance therapy are necessary.
The artificial diuresis, dialysis, hemoperfusion and exchange blood transfusion are ineffective.
Form of release and packing
of the Tablet, film coated 50 mg, 100 mg.
On 10 or 14 tablets (for a dosage of 50 mg) and 5 or 7 tablets (for a dosage of 100 mg) in blister strip packaging from a film of white not transparent PVH/PE/PVDH and aluminum foil.
On 3 (on 10 tablets) or 1 or 2 (on 14 tablets) planimetric packing (for a dosage of 50 mg), 2 or 4 (on 7 tablets) or 6 planimetric packs (on 5 tablets) (for a dosage of 100 mg) together with the instruction for medical use in the state and Russian languages place in a pack cardboard with the hologram of firm – producer.
To Store storage conditions at a temperature not above 25 °C, in the dry, protected from light place.
A period of storage
2 years
Prescription status
According to the prescription
Republic of Kazakhstan JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika Producer
Almaty, Shevchenko St. 162 E.
To develop
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