Friday, 6 May 2011

Introduction into clinical practice ...

The introduction into clinical practice of the modern generation of antidepressants has provided substantial progress in the treatment of depression. One step in this direction was the creation of citalopram. Citalopram, bicyclic derivative ftalana, in some studies is regarded as the standard selectivity of SSRIs. This characteristic is correlated with the actual lack of influence of the drug and its metabolites on dopaminergic and noradrenergic neurotransmitter systems, as well as with minimal affinity for the receptor and enzyme systems (alpha-and beta-adrenergic, histamine-1 receptors, D1 and D2 receptors, 5-HT1A, 5-HT1B and 5-HT2 receptors, benzodiazepine and opioid receptors). Unlike other members of this group of antidepressants (fluvoxamine, fluoxetine, paroxetine), drug and its metabolites have virtually no "secondary" pharmacological properties, ie not associated with a large number of other receptors and enzymes (cytochromes R1A2, and R3A4 R2S19, R2D6, M-cholinergic receptors, nitroksidsintetaza) that can make a positive contribution to the overall clinical effect. Systemic bioavailability of citalopram is close to zero and is 80%. Being fat-soluble compound, citalopram easily (not related to the meal) and rapidly (within 2 - 4 hours) reaches maximum concentration in biological fluids and its lipotropic ensures easy penetration of the active ingredient through the blood-brain barrier. Renal clearance of citalopram in the treatment stays within 20-25% at the expense of alternative ways of final elimination, which, unlike other SSRIs, does not require dose adjustment even when the phenomena of moderate renal insufficiency. Having higher compared with other SSRIs selectivity, the drug retains multivalency and affects not only the wide range of disorders that are determined by pathologically reduced affect, but also to other symptom - anxiety, obsessive-phobic, behavior, etc. The significant trends and indicators of citalopram in outpatient and steady practice is the speed display therapeutic activity. At the clinical level, the lowest latency period between the drug and a marked timolepticheskim action indicated in the first 7 - 10 days of therapy. Study of the effectiveness of citalopram in vascular, particularly multiinfarktnoy, dementia and Alzheimer's disease showed the possibility of reduction of symptoms of emotional dullness (coarsening), depressed mood, irritability and restlessness, inner tension, the propensity to excessive anxiety in normal situations, the formation of fear and the formation of panic attacks and asthenic symptoms, and even confusion. The use of therapeutic doses of citalopram is not accompanied by cardiotoxic effects (changes in blood pressure, occurrence of arrhythmias, or disturbances on ECG), regardless of duration of treatment and the presence of cardiac pathology.

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