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Active ingredients
Nicergolin
Release form
Pills
Composition
1 tablet contains: nicergoline 10 mg. Auxiliary substances: calcium hydrogen phosphate dihydrate - 94.3 mg, microcrystalline cellulose - 22.4 mg, magnesium stearate - 2 mg, sodium carboxymethylcellulose - 1.3 mg. Sugar composition: sucrose - 33.4 mg, talc - 10.9 mg, acacia resin - 2.7 mg, sandarak resin - 1 mg, magnesium carbonate - 0.7 mg, titanium dioxide (E171) - 0.7 mg, rosin - 0.6 mg, carnauba wax - 0.06 mg.
Pharmacological effect
Sertralin is a potent and selective serotonin reuptake inhibitor (5HT). In clinical doses, sertraline blocks serotonin uptake in human platelets. Sertralin does not have an affinity for muscarinic (cholinergic), serotonin, dopamine, histamine, benzodiazepine, and adrenergic receptors. It does not enhance the activity of the sympathetic nervous system. Unlike tricyclic antidepressants, it does not increase body weight.
Pharmacokinetics
When administered sertralina in doses of 50-200 mg 1 time / day. within 14 days, Cmax in plasma is reached after 4.5-8.4 hours. The average T1 / 2 in young and elderly men and women is 22-36 hours. Accordingly, the half-life is approximately double cumulation of the active substance until an equilibrium state is reached after 1 week of treatment. Plasma protein binding is about 98%, Vd - 20 l / kg. Intensively metabolized during the first passage through the liver. The main metabolite found in plasma, N-desmethyl sertraline, has poor pharmacological activity. T1 / 2 N-desmethyl sertraline varies from 62-104 hours. It is mainly excreted through the intestines and in the urine in equal amounts as metabolites, less than 0.2% is eliminated with urine unchanged.
Indications
Acute or chronic vascular or metabolic cerebral insufficiency: atherosclerosis. Thrombosis or embolism of cerebral vessels. transient cerebral ischemic seizures. Acute or chronic peripheral vascular insufficiency: obliterating vascular diseases of the extremities. Raynaud's syndrome. other syndromes characterized by impaired peripheral circulation. Headache.
Contraindications
Acute bleeding. Acute myocardial infarction. Orthostatic hypotension. Increased sensitivity to nicergoline.
Precautionary measures
It is used with caution in the abuse of drugs or dependence on them in history, abnormal liver function, renal dysfunction, epileptic seizures, weight loss. It should not be used in patients undergoing electroshock therapy. The use of sertraline is possible no earlier than 14 days after discontinuation of MAO inhibitors. During the period of treatment to prevent the use of alcohol. Safety of use in pediatrics has not been established.
Use during pregnancy and lactation
Adequate and well-controlled studies of the safety of sertraline during pregnancy have not been carried out, so use is possible only in cases where the expected benefit to the mother outweighs the possible risk to the fetus. It is not known whether sertraline is excreted in breast milk, so use during lactation is not recommended. Separate studies have shown that sertraline in infants whose mothers received sertraline during the feeding period is insignificant or undetermined, while the concentration in breast milk exceeds the concentration in the mother’s blood. Women of childbearing age should be used during sertraline treatment. reliable methods of contraception. In experimental studies, no teratogenic and mutagenic action of sertraline was detected. However, in doses approximately 2.5-10 times higher than the maximum daily clinical doses, sertraline caused a delay in ossification of the fetal bone tissue, possibly as a result of the effect on the maternal individual. With the introduction of sertraline in doses of about 5 times the maximum clinical dose, a decrease in the survival rate of newborns was observed.
Dosage and administration
Inside the drug is prescribed for 5-10 mg 3 times / day with the same intervals between doses for a long period of time. To improve the absorption of the drug should be taken in between meals. In some cases, it is advisable to start treatment with parenteral administration of the drug (Sermion por.iof.d / in. 4 mg fl. 4 ml [with p-lem] pack. 4 Pfizer) with the subsequent transition to oral administration during the period of maintenance therapy. For convenience of dosing you can use the drug Sermion tab.s. 5 mg pack. 30 Pfizer.
Side effects
On the part of the cardiovascular system rarely - feeling the heat and flushing to the face. On the side of the central nervous system rarely - drowsiness, insomnia. On the part of the digestive system rarely - mild gastric disorders.
Overdose
Severe symptoms of an overdose of sertraline were not detected even with the administration of the drug in large doses. Overdose symptoms: tremor, disorientation, restlessness, muscle hypertonia, hyperreflexia, myoclonic jerking first in the feet, then spread throughout the body, abdominal cramps, flatulence, diarrhea, nausea, vomiting, dyspepsia. Treatment of overdose: no specific antidotes. To reduce the absorption possible gastric lavage, the use of activated carbon. It is necessary to ensure normal airway, oxygenation and ventilation of the lungs. The functions of vital organs should be monitored, and symptomatic and supportive therapy should be carried out.
Interaction with other drugs
When applied simultaneously with anticoagulants of coumarin derivatives, the prothrombin time is significantly increased. When used simultaneously, sertraline may displace other drugs from the association with plasma proteins, as a result, the concentration of the corresponding active substance in the plasma increases and the risk of side effects increases. which occurs with the participation of the CYP2D6 isoenzyme, it is possible to increase the plasma concentration of these drugs due to and flexing of the isoenzyme CYP2D6 under the influence of sertraline. With simultaneous use of MAO inhibitors (including selegiline, moclobemide), serotonin syndrome may develop (hyperthermia, muscle rigidity, myoclonus, as well as manifestations of instability in the mental and physiological state of the body, up to the development of delirium and coma ). With simultaneous use with lithium salts may increase tremor. With simultaneous use with desipramine, it is possible to increase the concentration of desipramine in the blood plasma; with cimetidine - a significant reduction in sertraline clearance.
special instructions
Serlift should not be prescribed in conjunction with an MAOI, and also within 14 days after stopping the treatment of MAOI.After canceling Serlift within 14 days do not prescribe IMAO. During treatment with Serlift, care must be taken when driving vehicles and potentially hazardous activities that require increased concentration and psychomotor speed.