chap 6

• so for today we will be discussing the adreno receptor agonist and sympatho pneumatic drugs so supreme we started discussing the autonomic nervous system and then we had started discussing the cholinergic apart so parasympathetic nervous system apart so cholinergic both cholinergic agonists and so do not forget ham on the guitar cholinergic because it is converted by the neurotransmitter um called acetylcholine and do not forget effect you just have to reverse the dumbbells you will get the you will know the effect of the antagonist
• so this time summit term sympathetic nervous system or otherwise known as the fight or flight system in our body so this is still under the autonomic nervous system part
• for this afternoon we will be discussing the molecular pharmacology underlying the actions of sympathomimetic drugs and then enumerated medicinal chemistry of the sympathematic drugs we will also discuss the organ system effects of those drugs and then identify non-cardiac effects of the sympatho pneumatics so naka separate because most of our drugs na outside the cardiovascular system and then let's apply the basic pharmacology of sympathomimetics to a clinical problem so we will end our discussion with a case study
• sympathetic nervous system again we call it the fight or flight system in our body and this is a very important system that governs virtually all organ systems in the body so the effect is not just for the heart but actually all over our body however um sympathetic nervous system is most crucial when it comes to the regulation of our blood pressure
• sympathetic nervous system is governed by the acetylcholine this time the man's sympathetic nervous system is most likely governed by the north epinephrine so major neurotransmitter for the sympathetic nervous system is the north epinephrine
• Hormones


  Released by endocrine glands, travel through the blood to target cells
• Neurotransmitters


  Released by neurons, travel across the synapse to receptors on the next neuron
• Hormones have slower but longer lasting effects compared to neurotransmitters
• The precursor for norepinephrine is the amino acid tyrosine
• The rate limiting step in the production of norepinephrine is the conversion of tyrosine to dopa by the enzyme tyrosine hydroxylase
• Dopamine is converted to norepinephrine by the enzyme dopamine beta hydroxylase
• Vesicular monoamine transporter (VMAT)


  Transports dopamine into vesicles for storage
• Norepinephrine receptors


  Alpha 1, alpha 2, beta 1, beta 2, beta 3
• Norepinephrine can be metabolized by the enzyme catechol-O-methyl transferase (COMT)
• Norepinephrine can be taken back up into the neuron by the norepinephrine transporter
• Monoamine oxidase (MAO) can metabolize norepinephrine inside the neuron
• Methyl dopa


  Inhibits the conversion of tyrosine to dopa
• Reserpine


  Inhibits the vesicular monoamine transporter (VMAT), preventing storage of norepinephrine
• Cocaine


  Inhibits the norepinephrine transporter, increasing norepinephrine in the synapse
• class assad and this is actually pila palanka slide super it took me more than an hour i mean at least an hour to finish this i really need to finish this until tomorrow paramount chapter 7 next week anyway this one is recorded so if you want to listen to it again i'll be sending the recording after our class remember our precursor is tyrosine so look at the structure so you have the o-h here the benzene ring and the carbons you have two carbons here one two and then the nh2 and then the cooh here and then it will be converted to dopa
• Sympathetic nervous system


  Also called adrenergic system
• Noradrenaline


  Also called norepinephrine, neurotransmitter
• Adrenaline


  Also called epinephrine, neurotransmitter
• During stress


  Body releases epinephrine
• Noradrenaline


  Lacks a methyl group compared to adrenaline
• Norepinephrine transporter


  Responsible for reuptake of norepinephrine from synaptic cleft
• 90% of released norepinephrine is removed from synaptic cleft by norepinephrine transporter
• 10% of released norepinephrine binds to receptors
• Sympathomimetic drugs


  Drugs that bind to and activate adrenergic receptors
• Direct agonist


  Drugs that directly bind to and activate adrenergic receptors, e.g. norepinephrine, epinephrine
• Indirect agonist


  Drugs that indirectly increase adrenergic effects, e.g. by releasing norepinephrine
• Mechanisms of action of sympathomimetic drugs

  1. Displacement of stored catecholamines from nerve endings

  2. Inhibition of catecholamine reuptake

  3. Inhibition of catecholamine metabolism
• Tyramine


  Amino acid found in foods that can displace catecholamines and increase norepinephrine levels
• Tyramine-rich foods


  Can increase blood pressure
• Monoamine oxidase (MAO) inhibitors


  Antidepressant drugs that inhibit the enzyme that metabolizes catecholamines
• MAO inhibitors can interact with tyramine-rich foods and cause hypertensive crisis
• Amphetamine


  Stimulant drug used to treat ADHD
• Amphetamine


  • Increases norepinephrine and dopamine release
  • Can have adverse effects like increased blood pressure and heart rate
• Alpha receptors


  Adrenergic receptors that mediate vasoconstriction
• Beta receptors


  Adrenergic receptors that mediate vasodilation and increased heart rate