Neuropsychofarmacology 2404-P-5-NP-NPF

Overview of pharmacology according to the scheme:
1. antipsychotic drugs (neuroleptics):
• first attempts after World War I after unsuccessful treatment of psychoses with comas, shocks and malarial fever
• these are drugs with antidopaminoergic effects (blockade of D2 receptors in the striatum), they eliminate the symptoms of psychosis, hallucinations, delusions and agitation
• 1949 - the first drugs from this group were chlorpromethazine and lithium salts, but they had severe side effects and high mortality
• 1952 - reserpine extract of the medicinal plant Rauwolfia serpentina (known in India as a medicine for viper bites and insomnia)
• 1959 haloperidol, 1988 – risperidone, 1968 – sulpyrid, 1975 – clozapine
2. antipsychotic drugs – mechanism of action:
• act mainly on the dopaminergic system responsible for the "normality" of the mind
• influence the modulation of new reinforcements, rewards, and motivation of behavior
• the release of dopamine regulates the feeling of pleasure and delight
• increasing dopamine increases sensitivity to reward-related stimuli
• antipsychotic drugs - mechanism of action: blocking dopaminergic receptors abolishes the mechanism of sharpening the "superconsciousness", stopping treatment, new stress, psychoactive substances cause or exacerbate psychosis, psychological aspect - return of criticism, cognitive and emotional distance, plasticity of response to the symptoms of psychosis
• the effect of antipsychotic drugs is rapid once a high therapeutic level is reached
3. antidepressants - antidepressants:
• 16th century – Laudanum - tinctures ("arcanum" - parables) Paracelsius
• 19th century Tinctura opii E. Kraeplin
• 1952 the first drug for depression – iproniazid (a drug for tuberculosis)
• 1957 imipramine
• 1960 – tricyclic drugs
• 1970 - valproic acid
• 1980 – SSRIs (Serotoin Selective Reuptake Inhibitors) e.g. fluoxetine (Prozac)
• 1990 - escitalopram, e.g. Mozarin
• 2019- about 30-60 drugs on the market
• antidepressants - mechanisms of action: regulatory effect on serotonergic and noradrenergic neurotransmission: reducing the degradation of monoamines (NA, 5HT), selective or not, e.g. MAO inhibitors - inhibition of NA, 5HT reuptake, direct effects on postsynaptic receptors in a specific neurotransmitter system, effect on transmission of signals inside the neuron (concentration of secondary transmitters, expression of transcription processes), influence on the hypothalamic-pituitary-adrenal axis
• Attention! the therapeutic effect begins after 10 - 14 days and improvement after the next 7 - 14 days
4. anti-anxiety drugs - anxiolytics
• soothe and eliminate somatic and mental anxiety symptoms
• reduce the sense of threat and fear of bad events
• reduce the feeling of helplessness
• eliminate somatic symptoms - muscle tension, tremors, excessive sweating, heart palpitations, urge to urinate, various types of pain
• Attention! have a different effect than neuroleptic sedation, i.e. suppression, apathy, indifference, reduction of life activity
• plant precursors: St. John's wort (Hypericum perforatum), Kava - kava (Piper methysticum), valerian (Valeriana officinalis, ginkgo (Ginko - biloba))
• breakthrough in drug treatment: benzodiazepines
• discovered in the USA in the 1950s as a "happy pill"
• anti-anxiety drugs (anxiolytics) – contraindications:
o there are no indications in clinical situations that anxiety may be involved in the development of disease symptoms
about addiction to psychoactive substances of any kind
o drug hypersensitivity
o respiratory failure (asthma, emphysema, cystic fibrosis, bronchitis and pneumonia)
about poisoning (ethanol)
o myasthenia gravis, glaucoma
o pregnancy, lactation
5. mood stabilizers:
• these are drugs that normalize mood disorders (mood stabilizer, normothymics)
• mainly used in bipolar disorder
• 1963 – first drugs – lithium salts in manic episodes
• 1963 - carbamazepine as an antiepileptic drug
• 1963 – valproic acid
• clozapine and lamotrigine – drugs currently used in the treatment of affective disorders, the mechanism of action is related to the transport of sodium by the sodium-potassium pump in the cell membrane
6. Pro-cognitive drugs and agents – nootropics:
• improve memory functions in people with weakened cognitive sphere
• multi-level actions through complex neurophysiological and chemical processes
• affect mood, emotions, awareness, concentration, attention, motivation
• division criteria, very confusing and unregulated activities
7. Drugs and agents used for sleep disorders:
• sleep is a physiological state of cyclical changes in the brain
• sleep disorders are possible during falling asleep and waking up, NREM to REM transitions during the sleep cycle related to changes in neurotransmitter activity
• sleep regulation depends on the acetylcholine, serotonin, norepinephrine and dopamine systems