PCOL Rationale

• Neuroleptics


  Antipsychotic agents, also known as major tranquilizers/antischizophrenics
• GABA


  The major inhibitory neurotransmitter in the brain
• Glycine


  The major inhibitory neurotransmitter in the spinal cord
• Glutamate


  The major excitatory neurotransmitter in the brain
• Monoamines


  Include epinephrine, norepinephrine, dopamine, serotonin
• Phenobarbital is an anticonvulsant that increases GABA levels and does not affect Na channels
• Amobarbital is an intermediate-acting barbiturate that is used as a hypnotic, not a sedative
• Pharmacokinetics


  What the body does to the drug
• Pharmacodynamics


  What the drug does to the body
• Pharmacotherapeutics


  Study of the rational drug use
• Mannitol facilitates non-target-protein action, through colligative (physical) mechanism
• Na+-K+-ATPase pump


  Targeted by digoxin
• 1. H Pump


  Targeted by PPIs
• COX


  Targeted by NSAIDs
• Beta receptors


  Targeted by beta blockers
• Types of receptors


  • Ionotropic
  • Metabotropic
  • Kinase-linked
  • Gene-transcription
• GABAA receptors


  Type I receptors, linked with Cl ion channels
• Metabotropic receptors


  Also known as G protein-coupled receptors
• Agonist


  Affinity with intrinsic activity
• Efficacy


  Maximum achievable response
• Ceiling dose


  Lowest dose producing maximum effect
• Margin of safety


  Parameter of quantal dose-response
• Slope

  Degree of changes in dose with changes in response
• Mannitol for cerebral edema does not facilitate chemical antagonism, it is a physical interaction
• Chelation (e.g. deferoxamine for iron poisoning) and neutralization (e.g. antacids for hyperacidity) are examples of chemical antagonism
• Efficacy is measured by the level of response, not by a certain amount
• Amlodipine 5 mg tablet

  The most potent, as the lower the dose, the more potent
• Competitive antagonist

  Reversible, surmountable, relatively safer
• Non-competitive antagonists are toxic
• Higher therapeutic index implies that a drug does not require therapeutic drug monitoring
• Nicotinic receptors are ionotropic, unlike the other receptors which are metabotropic
• Morphine for severe pain

  The most effective, as higher efficacy is more useful for severe disorders
• Anatomy and physiology of the autonomic nervous system

  • It contains 2 neurons
  • The first neuron is called the pre-ganglionic neuron
  • It does not have a ganglion
  • The function is mainly vegetative
• Synthesis, storage and release of neurotransmitters

  Observed in the pre-synapse
• Beta-1 receptor activation in the heart does not cause release of renin, that is an effect of beta-1 receptors in the kidneys
• Mechanism of methyldopa


  Metabolic transformation by same pathway as precursor of transmitter
• Mechanism of Guanethedine, Guanardrel, Bretylium (GGB)

  Prevention of release of adrenergic neurotransmitter
• Mechanism of Reserpine


  Blockade of transport system of adrenergic neurotransmitter
• Mechanism of Tyramine, Ephedrine, Amphetamine, Angiotensin II, Methamphetamine (TEAM)


  Promotion of exocytosis or displacement of transmitter from storage sites
• Labetalol is not approved for use in patients with congestive heart failure, unlike bisoprolol, metoprolol succinate, and carvedilol