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PSYCHOTROPICS

PSYCHOTROPICS.

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PSYCHOTROPICS

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  1. PSYCHOTROPICS This study material is recommended specifically for practical courses from Pharmacology II for students of general medicine and stomatology. These brief notes could be used to prepare for the lesson and as a base for own notes during courses. Addititonal explanations and information are given in single lessons.

  2. PSYCHOTROPICS

  3. PSYCHOFARMAKON (psychoactive drug) DEFINITION:

  4. PSYCHOTROPICS CLASSIFICATION with regard to their influence on psychical function + • VIGILANCE - + II. AFFECTIVITY - + III. PSYCH. INTEGRATION - + IV. MEMORY -

  5. Classification of psychotropics with regard to their main therapeutic effect: Příklady: • drugs for affective disorders • drugs for anxiety disorders • drugs for sleeping disorders • etc

  6. ETOPHARMACOLOGY Desription, principle, use:

  7. ANIMAL MODELS OF BEHAVIOUR Examples:

  8. ANXIOLYTICS Synonyms, characteristics, influence on CNS:

  9. INDICATIONS • anxiety– fear, psychictension • phobia • stagefright (not in allcases) • psychosomaticdiseases • PTSD • etc.

  10. ANXIOLYTICS - benzodiazepines

  11. BZD EFFECTS 1) hypnosedative 2) anxiolytics 3) anticonvulsive 4) myorelxant [ 5) amnestic ]

  12. Mode of Action - specific (receptor) - selectively bind to specific target site on GABAA receptor complex with Cl-channel - increase of affinity of GABA binding sites for GABA (positive allosteric modulation) -increaseofopeningCl-channelfrequency - neuronalmembranehyperpolarization - signaltransductioninhibition

  13. MZD adverse effects

  14. BZD contraindications

  15. Pharmacokinetics • ABSORPTION: • DISTRIBUTION: • BIOTRANSFORMATION: • EXCRETION:

  16. BZD - drugs - chlordiazepoxide (prodrug) - diazepam - oxazepam - bromazepam - lorazepam - alprazolam - tofizopam - ......

  17. - others..... • haimyl hypnotic effect: flunitrazepam, midazolam • myorelxants., enticonvulsive eff., clonazepam,diazepam

  18. Classification with regard to pharmacokinetics • ultra-short acting (3 - 6 hrs) • short acting (less than12 hrs) • long acting (12 – 24 hod) • very long acting (more than 24 hrs)

  19. BZD specificantagonists

  20. Barbituratessimilar mode of action to BZD, today as anxiolytics obsolete

  21. Otheranxiolytics serotonergic system • I. 5 - HT1A rec. partial agonists • II. small doses of antidepressants • III. small doses of antipsychotics • IV. H1- antiHis. • V. beta-block. • VI. propan derivatives

  22. HYPNOTICS, SEDATIVES, HYPNOSEDATIVES Definition: HYPNOTICS: SEDATIVES: Target site:

  23. HYPNOTICS, SEDATIVES, HYPNOSEDATIVES Indications • HYPNOTICS: • SEDATIVES: border between HYPNOTICS and SEDATIVES unclear HYPNOSEDATIVES

  24. Insomnia: • transitory • acute • chronic

  25. Sleepcycles • 1. slow-wawe sleep (NREM) • 2. fast-wave sleep (REM)

  26. HYPNOTICS INDICATIONS Insomnia in casethat:

  27. Requirements for ideal hypnotics • fast induction of sleep with physiological structure • wide therapeutic range • optimal speed of elimination • fast absorption after oral administration • therap. level. maintained for 5-7hrs, without active metabolites • without AE and drug interactions • without risk of addiction

  28. HYPNOTICS I.generation III. generation II. generation

  29. HYPNOTICS I. generation barbiturates – today obsolete nonbarbiturate hypnotics (ob- solete or rarely used)

  30. HYPNOTICS II. generation benzodiazepines

  31. HYPNOTICS III. generationΩ1selectiveagonistsof benzodiazepine receptors (Ω1 rec.= today: BZD1 rec.)

  32. Other drugs used as hypnosedatives I. small doses of suppressive antidepressants II. small doses of antipsychotics III. H1 - antiHis. (I. generation) IV. herbal hypnosedatives

  33. NEW TRENDS IN THE THERAPY OF INSOMNIA ll. influnecing circadial rhytms

  34. HERBAL HYPNOTICS • - Melissa off. • - Valeriana off. • - Humulus lupulus • - Crataegus monogyna • - Passiflora incarnata • - Hypericum perforatum

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