Professional Documents
Culture Documents
Autonomic Pharmacology: Outline
Autonomic Pharmacology: Outline
AUTONOMIC PHARMACOLOGY
Dr. Minerva P. Calimag, MD || August 30, 2019
• Catabolic
• Short preganglionic synapsing with several (one or
more) long postganglionic fibers in the sympathetic
1.1 SOMATIC NERVOUS SYSTEM ganglia
• Regulates activities under conscious control. • preganglionic neurons exit the spinal cord at the
• Acetylcholine (Ach) is the neurotransmitter released thoracolumbar level to synapse with postganglionic
at the neuromuscular junction nerves at the paravertebral ganglia to form the
• Consist of sensory and motor nerve divisions sympathetic trunk
– Sensory Division • all the paravertebral ganglia provide sympathetic
▪ Afferent Division innervation to blood vessels in muscle and skin,
▪ contains neurons and signals from the arrector pili muscles, and sweat glands
tendons, joints, skin, skeletal muscles, eyes, • Sympathetic trunk (22 pairs on each side of the spinal
nose, and many other organs cord)
• Agonist
– binding to receptors trigger a pharmacologic
response (with affinity and intrinsic activity)
• major means of inactivation: degradation by – Full Agonist produces maximum response
(intrinsic activity = 1)
– Partial Agonist cannot produce maximum
response (intrinsic activity < 1)
• Antagonist
• synapses:
– binding to receptors does not trigger a
– all preganglionic fibers outside CNS (sympathetic
pharmacologic response (with affinity, no intrinsic
and parasympathetic)
activity) (intrinsic activity = 0)
– all parasympathetic postganglionic nerve endings
– Competitive Antagonist block of receptor can be
– sympathetic postganglionic nerve endings of sweat
overcome by increasing the concentration of the
glands
agonist
– Somatic: motor neurons innervating skeletal muscle
– Noncompetitive Agonist bock of receptor cannot
be overcome by increasing the concentration of the
3.2 NOREPINEPHRINE agonist
• synthesis: • Inverse Agonist
– ligand binding produces opposite effects to those of
an agonist
– not the same as antagonists which block the effects
of both agonist and inverse agonist.
Receptors with:
● subscript 1 or 3
○ excitatory
○ contraction, constriction, enhanced
secretion
● subscript 2
○ inhibitory
○ relaxation, dilatation, inhibited
secretion
Ephedrine ● Acts indirectly on both alpha & beta receptors ● Used a vasopressor
● Causes release of endogenous
catecholamines (i.e. NE)
Reserpine ● Blocks synthesis & storage of NE ● Used in the management of some types of
HPN
● Adverse effect: Sedation
Betanochol ● Direct Acting: Muscarinic R ● Used for the treatment of GI & bladder atony
➢ Physostigmine
I. Tertiary Tertiary compounds are lipid-soluble and can easily penetrate the brain
Naturally-occuring alkaloids
Synthetic Esters
II. Quaternary Quaternary compounds are water-soluble & do not penetrate the CNS well