PCOL

• Sedative-Hypnotic Drugs


  Class of rugs na pampakalma and pampatulog
• Anxiolytic Drugs


  • Class of drugs that decreases anxiety
  • Some have sedative or hypnotic effects, some don't
• Neurotransmitter


  • Chemical messenger that enable neurons to communicate with one another
  • Stored in neuronal vesicles until released to the synapse
  • Action potential and calcium influx causes release
  • Terminated by reuptake or metabolism

  
• Action Potential
• Major Neurotransmitters and Their Receptors in the Central Nervous System

  • Acetylcholine
  • Amino Acids (GABA, Glutamate, Glycine)
  • Biogenic Amines (Dopamine, Norepinephrine, Serotonin, Histamine)
  • Neuropeptides (Opioid peptides, Tachykinins)

  
• Acetylcholine Receptors

  • Muscarinic (M1,M3,M5 - excitatory, M2,M4 - inhibitory)
  • Nicotinic - excitatory
• GABA Receptors


  • GABAA - inhibitory, ligand-gated ion channel site of action of sedative hypnotics, alcohol, general anesthetics
  • GABAB - inhibitory, modulates motor neuron excitability

  
• Glutamate Receptors


  • NMDA, AMPA, KA - excitatory
  • mGlu1, mGlu5 - excitatory
  • mGlu2-mGlu4, mGlu6-mGlu8 - inhibitory
• Glycine Receptors


  • Strychnine-sensitive - inhibitory
  • Strychnine-insensitive - excitatory, obligate coagonist for NMDA receptor
• Dopamine Receptors


  • D1, D5 - excitatory
  • D2, D3, D4 - inhibitory
• Norepinephrine Receptors


  • α1 - excitatory
  • α2 - inhibitory
  • β1, β2 - excitatory
• Serotonin (5-HT) Receptors


  • 5-HT1 - inhibitory
  • 5-HT2 - excitatory
  • 5-HT3 - excitatory
  • 5-HT4 - excitatory
• Histamine Receptors


  • H1 - excitatory
  • H2 - excitatory
  • H3 - inhibitory
• Opioid Peptide Receptors


  • Mu, delta, kappa - inhibitory
• Tachykinin Receptors


  • NK1, NK2, NK3 - excitatory
• Neurotransmitters can be excitatory or inhibitory, regulating themselves
• Excitatory Neurotransmitter (Glutamate)


  Causes arousal and seizures when dominant
• Inhibitory Neurotransmitter (GABA)


  Causes sleepiness and depression when dominant
• Anxiety


  Decrease GABA (Inhibitory NT), Increase 5HT, D, NE
• Psychosis


  Increase Glutamate (Excitatory NT), Increase D
• Depression


  Decrease NE, 5HT, D
• Mood Disorder


  Imbalance in NT (D, NE)
• Seizures


  Increase neuron firing, Increase 5HT, NE, D
• Parkinson's


  Decrease D, Increase ACH (Contraction/Movement)
• Alzheimer's


  Increase ACH
• CNS Drugs


  • Only correct an imbalance in neurotransmitter or their receptors
  • Only relieve symptoms, don't necessarily correct underlying diseases
  • Lipophilic to cross blood-brain barrier
  • Only 20% of brain understood, psychopharmacological drugs are hypotheses
• Mechanism of CNS Drugs

  • Synthesis, Storage, and release
  • Reuptake and degradation
  • Receptor activation and blockade
• SEDATIVE-HYPNOTIC-ANXIOLYTIC DRUGS
• Sleep


  Reversible state of reduced consciousness with characteristic EEG changes

  
• Rapid Eye Movement (REM) Sleep


  Sleep characterized by darting eye movements, brain waves similar to wakefulness, body relaxed but can have jerky movements, dreams are fantasy-like

  
• Non-REM (NREM) Sleep


  Subdivided into 4 stages, dreams are more conceptual, constitutes 75-80% of total sleep time

  
• 5 Distinct Patterns of Brain Wave Activity During Sleep

  • Stage 1 (transitional)
  • Stage 2 (deep relaxation)
  • Stage 3 & 4 (deep/slow-wave sleep)
  • Stage 5 (REM)

  
• Insomnia


  Difficulty falling asleep or staying asleep, irregular sleep pattern

  
• Insomnia Treatment


  • Self-limiting if caused by acute stress or minor illness
  • Psychotherapy (CBT) if caused by medical conditions
  • Sedative-hypnotic drugs (BZD, barbiturates) to induce sleep
  • Benzodiazepines (triazolam, estazolam, temazepam, quazepam, flurazepam)
  • Non-pharmacological interventions (good sleep habits, sleep hygiene)
• Psychotherapy (CBT) is first line treatment for insomnia
• When hypnotics are appropriate, they must be used judiciously
• magkaraoon ng vivid dremas, however your body is essentially paralyzed
• INSOMNIA


  Difficult to go to sleep or to stay asleep during night; awaken too early in the morning
• Insomnia


  • Pattern of sleep; irregular, longer latency to fall asleep, frequent awakenings

  
• Insomnia symptoms


  Very transient, can only be associated by identifiable events such as family or work situation