Sarotenum

General characteristics. Structure:

Active ingredient: 10 and 25 mg of amitriptyline in the form of Amitriptylini hydrochloridum.

Sarotenum is tricyclic antidepressant with sedation.

Pharmacological properties:

Pharmacodynamics. Equally inhibits the return capture of noradrenaline and serotonin. Has cholinolytic and antihistaminic activity. Renders powerful antidepressive, sedative, anxiolytic and analgesic action.

Pharmacokinetics. Bioavailability of amitriptyline at oral administration makes about 60%. The maximum concentration in blood serum is reached on average in 4 hours. Linkng with proteins of plasma – about 95%. Metabolism of amitriptyline is carried out by means of demethylation and a hydroxylation. The main metabolite of amitriptyline is нортриптилин.

The elimination half-life of amitriptyline averages 25 hours (16 – 40 hour), an elimination half-life of a nortriptilin – about 27 hours. Equilibrium concentration is established in 1-2 weeks. Amitriptyline generally with mochy, and, partially, with a stake is removed. Amitriptyline and нортриптилин get through a placental barrier and in small amounts are allocated with breast milk.

Indications to use:

• Depressions, especially with alarm, agitation and sleep disorders. It is shown at treatment: endogenous depressions mono - and bipolar type, the involutional, masked and climacteric depressions. It can be used at dysphorias and alcoholic depressions, situational depressions and depressive neurosis. At treatment of schizophrenic depressions it is used in a combination with neuroleptics.
• Chronic painful frustration.
• Night enuresis.

Route of administration and doses:

Treatment of depressions. Adults: it is necessary to begin treatment with Sarotenum with 75 mg/days (3 times a day on 25 mg). If necessary the dose can increase in days by 25 mg to 150 mg/days (up to 225 mg/days more rare at the hospitalized patients). After achievement of the expressed improvement the daily dose can be reduced to minimum effective, usually to 50 - 100 mg/days. At therapy of depressions it is recommended to continue use of antidepressants including Sarotenum, after achievement of the expressed effect within 4-6 months. In the maintenance doses having antirecurrent effect, Sarotenum can be accepted is long, up to several years.

Elderly: it is necessary to begin treatment with Sarotenum with 30 mg a day (3 times a day on 10 mg). If necessary the dose can increase to 100 - 150 mg/days gradually daily. After achievement of the expressed improvement the daily dose has to be gradually reduced to minimum effective, usually to 25 - 50 mg/days.

Children: treatment by Sarotenum of children has to be carried out only in the conditions of a psychiatric hospital. The initial daily dose is defined with the child's weight, at the rate of 1,5 mg/kg/days. The daily dose can gradually increase by 1,5 mg/kg/days a week, to maximum – 5 mg/kg/days.

Chronic painful frustration. Adults: it is necessary to begin treatment with purpose of 25 mg for the night. If necessary the dose can be increased to 100 mg for the night.

Elderly: it is necessary to begin treatment with purpose of 10 mg for the night. If necessary the dose can be increased to 50 mg for the night.

Night enuresis. Children of 7-12 years: 25 mg in 1/2-1 hour prior to a dream. Children are more senior than 12 years: 50 mg in 1/2-1 hour prior to a dream.

Features of use:

It is not necessary to appoint amitriptyline along with MAO inhibitors. It is possible to begin treatment using amitriptyline in 14 days after the termination of reception of the MAO irreversible non-selective inhibitors, and also not less than in a day after the termination of administration of drugs of reversible action — a moklobemid and a selegilin.

Treatment using MAO inhibitors can be begun not earlier than in 14 days after the amitriptyline reception termination.

Simultaneous use of these drugs can cause development of a serotoninovy syndrome (a combination of the symptoms including alarming arousing, confusion of consciousness, a tremor, muscular rigidity and a hyperthermia).

At use of drug the probability of development of disturbances of a heart rhythm and heavy arterial hypotension increases in high doses. Development of such states is possible also at use of usual doses for patients with the available heart diseases.

Amitriptyline with care is appointed to patients with a convulsive syndrome, an urination delay, a prostatauxe, a hyper thyroidism, paranoid states, a heavy abnormal liver function or chronic diseases of cardiovascular system.

At depressions the risk of suicide attempts remains. Such risk can exist up to the moment of approach of permanent remission and arise spontaneously throughout a therapy course. Persons with suicide bents should not appoint drug in high doses. Against the background of treatment by antidepressants it is necessary to watch carefully a condition of patients, especially at the beginning of therapy, rather clinical deterioration and/or emergence of suicide thoughts and behavior.

Patients with tendency to a suicide should not have access to a large amount of medicine.

The special attention is necessary in case of purpose of amitriptyline for patients with a hyperthyroidism or accepting drugs of thyroid hormones as development of arrhythmia of heart is possible.

Patients of advanced age are especially inclined to development of postural hypotension during treatment by amitriptyline.

At patients with maniac-depressive frustration transition of a disease to a maniacal phase is possible; from the moment of the beginning of a maniacal phase of a disease it is necessary to stop therapy by amitriptyline.

At use of amitriptyline in connection with a depressive component of schizophrenia strengthening of psychotic symptoms is possible. It is necessary to appoint amitriptyline in a combination with neuroleptics.

Patients with reduction have depths of an anterior chamber of an eye and by narrowing of its corner attacks of acute glaucoma owing to a mydriasis can be observed.
Use of anesthetics against the background of therapy три-/tetracyclic antidepressants can increase risk of arrhythmias and arterial hypotension. It is whenever possible necessary to stop use of amitriptyline several days prior to surgical intervention. In need of an urgent operative measure it is necessary to inform surely the anesthesiologist on treatment by amitriptyline.

Also, as well as other psychotropic drugs, amitriptyline it is capable to change tolerance of an organism to insulin and glucose that demands correction of antidiabetic therapy from patients with a diabetes mellitus; besides, actually depressive disease can be shown by changes of balance of glucose in the patient's organism.

It is reported about hyper pyrexia cases against the background of use of tricyclic antidepressants in case of appointment along with anticholinergic or antipsychotic medicines, especially in the period of hot weather.

The sudden termination of therapy after long treatment can become the reason of emergence of symptoms of cancellation in the form of a headache, an indisposition, sleeplessness and irritability. Such symptoms are not signs of medicamentous dependence.

Excipients: tablets of drug contain monohydrate of lactose in the structure. Patients with a rare inherited disorder in the form of intolerance of a galactose, insufficiency of lactase or malabsorption of glucose galactose should not accept this medicine.

Period of pregnancy and feeding by a breast. Amitriptyline is not appointed during pregnancy if only the expected advantage for mother does not exceed theoretical risk for a fruit. Purpose of tricyclic antidepressants in high doses throughout the III trimester of pregnancy can cause neurobehavioural disturbances in newborns. At newborns, according to messages, drowsiness cases as result of influence of amitriptyline and an ischuria, as result of influence of a nortriptilin (an amitriptyline metabolite) are established if drug was appointed to women during childbirth.

Drug gets into breast milk in low concentration therefore its influence on the baby at use of therapeutic doses by mother is improbable. The dose received by the child makes about 2% of a dose of mother concerning the mass of the child (mg/kg). On condition of clinical need throughout therapy by amitriptyline feeding by a breast can be continued, but observation of a condition of the child of chest age, especially in the first 4 weeks after the birth is recommended.

Children and teenagers aged up to 18 years. Amitriptyline is not recommended for treatment of a depression at children and teenagers aged up to 18 years in connection with insufficiency of data on its safety and efficiency. Treatment by amitriptyline is connected with risk of cardiovascular by-effects in all age groups.

Apply at children of 7-12 years to treatment of night enuresis on condition of absence of organic pathology.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Sarotenum, Sarotenum Retard are medicines with sedation. At the patients receiving psychotropic drugs it is possible to expect disturbance of the general attention and ability to concentration that is dangerous and prohibits control of vehicles and work with exact mechanisms.

It is not recommended to appoint Sarotenum during pregnancy and feeding a breast.

Side effects:

The side effects connected with anticholinergic action: dryness and/or acid-bitter taste in a mouth, nausea, vomiting, stomatitis, it is rare – cholestatic jaundice; the vision disorder, increase in intraocular pressure, tachycardia, locks and is much more rare – an urination delay. Arise usually in an initiation of treatment, then, as a rule, decrease.

From cardiovascular system: tachycardia, arrhythmias, orthostatic hypotonia, the disturbances of endocardiac conductivity registered only on an ECG, but which are not shown clinically.

From TsNS: drowsiness, weakness, disturbance of concentration of attention, headaches, dizzinesses. These disturbances which are quite often arising at the beginning of therapy by amitriptyline decrease in the course of treatment. More rare, especially when high initial doses are applied, there can be a somnolention, a disorientation, conditions of confusion of consciousness, excitement, hallucinations, extrapyramidal disturbances, a tremor and spasms, is rare - alarm.

Allergic reactions: skin rash, an itch are possible.

Others: there can be nausea, the increased sweating, increase in weight, decrease in a libido.

Interaction with other medicines:

Amitriptyline can strengthen effect of alcohol, barbiturates and other substances, the oppressing TsNS.

Combined use with MAO inhibitors can lead to hypertensive crisis. As amitriptyline strengthens effect of anticholinergic drugs, it is necessary to avoid co-administration with them.

Strengthens action of sympathomimetics of adrenaline, noradrenaline, etc. thereof it is not necessary to apply the local anesthetics containing these substances along with amitriptyline.

Can reduce anti-hypertensive effect of a clonidine, betanidin and guanetidin.

At joint appointment with neuroleptics it is necessary to consider that tricyclic antidepressants and neuroleptics mutually inhibit metabolism of each other, reducing a threshold of convulsive readiness.

At simultaneous use with Cimetidinum amitriptyline metabolism delay, increase in its concentration in a blood plasma and development of toxic effects is possible.

Contraindications:

Recently postponed myocardial infarction, disturbance of endocardiac conductivity, acute alcoholic poisoning, barbiturates or opiates, closed-angle glaucoma, use together with MAO inhibitors and within 2 weeks after their cancellation, hypersensitivity to amitriptyline.

Precautionary measures. Sarotenum has to be appointed with care to patients with convulsive disorders, an urination delay, prostatauxe, a serious illness of a liver or cardiovascular system, hyperfunction of a thyroid gland.

Having sedative effect, can influence ability of driving and other mechanisms. The patients accepting amitriptyline have to be in advance warned by the doctor about this aspect of effect of drug.

Overdose:

Symptoms. Oppression or excitement of TsNS. The expressed manifestations anticholinergic (tachycardia, dryness of mucous membranes, an urination delay) and cardiotoxic (arrhythmias, hypotension, heart failure) actions. Convulsive frustration. Hyperthermia.

Treatment. Is symptomatic. It has to be carried out in a hospital. At oral administration of amitriptyline it is necessary to carry out as soon as possible a gastric lavage and to appoint absorbent carbon. Measures have to be taken for maintenance of activity of respiratory and cardiovascular systems. Monitoring of cordial activity within 3 – 5 days is desirable. Adrenaline should not be appointed in similar cases. At convulsive frustration diazepam can be applied.

Storage conditions:

List B. Tablets of Sarotenum have to be stored at a temperature not above 25 °C. On each packaging expiry date of the validity is specified. To store in places, inaccessible to children.

Issue conditions:

According to the recipe

Packaging:

Each film coated tablet contains Amitriptylini hydrochloridum in quantity, the corresponding 10 and 25 mg of amitriptyline. Packaging: 10 mg - 50 pieces; 25 mg - 50 pieces.