Obat Simpatik
Obat Simpatik
Obat Simpatik
POKOK BAHASAN
PENGANTAR OBAT OTOMOM
OBAT AGONIS KOLINERGIK
OBAT ANTAGONIS KOLINERGIK
OBAT ADRENERGIK
OBAT ANTAGONIS ADRENERGIK
PENGANTAR
DEFINISI
meniru, modifikasi, aktivitas SSO
meliputi :
sistem saraf otonom (anatomi)
zat kimiawi (neurotransmiter)
organ efektor (efek obat)
Anatomi
Sistem saraf
Sistem Saraf Tepi
Divisi efferen
Divisi afferen
(sensorik)
Saraf Parasimfatis
Saraf Simfatis
SINTESIS
TRANSPORTASI
NEUROTRANSMITER
IKATAN
DEGRADASI
RESEPTOR
EFEK OBAT
KHASIAT KLINIK
ANTIADRENERGIK
SIMPATOLITIK
&
SUMMARIES
Structure of the Autonomic NS
* two neurons, preganglionic and postganglionic.
* synapse in autonomic ganglia.
* each preganglionic neuron is connected with eight, nine or upto 32 postganglionic neurons.
* The autonomic ganglia are also mini - integrating centers.
* They receive input from the periphery and modulate the outgoing responses.
* Intrinsic neurons secrete dopamine that is inhibitory.
The autonomic signals are transmitted to the body through
* the sympathetic nervous system (thoracolumbar system, fight and flight division)
* the parasympathetic nervous system (craniosacral system, rest and digest division)
* Some authors distinguish also the enteric system.
SYMPATHETIC SYSTEM
* The cell bodies in the intermediolateral horns of the thoracic and lumbar spinal cord.
* The myelinated slowly conducting B fibers (preganglionic) through the gray rami communicantes
pass into the ventral roots and to the sympathetic ganglia (paravertebral chain ganglia).
* postganglionic neuron (between the sympathetic ganglia and the target organs). - mostly
unmyelinated C fibers, end on the visceral neurons.
* The paravertebral sympathetic chains of the ganglia lie on both sides of the spinal column.
* There are also two prevertebral ganglia the celiac ganglion and the hypogastric ganglion.
* The fibers from these ganglia reach the inner organs through the plexuses on the surface of the
blood vessels. Other axons from the sympathetic ganglia reenter the spinal cord and reach the target
organs through the spinal nerves.
* active in emergency situations:
- heart beat is accelerated,
- eye pupils are dilated,
- blood pressure raises,
- blood vessels in the skin are constricted,
- blood glucose increases,
- the state of arousal is induced.
Adrenergic receptors
- The nerve fibers do not form firm junctions on the target
organs.
- Neurotransmitters are secreted from the varicosities along the
nerve fibers.
- all are linked to G proteins.
- distinguished by their sensitivity to epinephrine,
norepinephrine and the drug isoproterenol.
- norepinephrine activates more alpha receptors, epinephrine
activates more beta receptors
Alpha receptors
* increase intracellular calcium levels by opening calcium channels in
the cell membrane, by releasing calcium from intracellular stores, or
both.
* 1 receptors are the most common adrenergic receptors.
- dominate in salivary glands and in the vascular smooth muscle
- induce contraction of arterioles, uterus, bronchioles, sphincters of
the urinary bladder and GI tract, vas efferens and musculus dilator
pupillae.
- respond strongly to norepinephrine and only weakly to
epinephrine.
- through the G proteins, they activate phospholipase C. which
catalyzes the liberation of diacylglycerol which causes a release of
calcium ions.
* 2 receptors are less common, occur in the CNS, kidneys, uterus,
parotid gland, pancreas, mast cells and thrombocytes, GI tract. N
- norepinephrine inhibits adenylcyclase.
Beta receptors
- activate cyclic AMP and trigger phosphorylation of cellular proteins.
* 1 receptors are prominent in the heart. They can raise the level of
intracellular calcium. The mechanism of action involves G proteins.
They are coupled to the adenylcyclase.
- In the SA node, they increase the heart rate.
- In the AV node, they increase conduction velocity.
- In the heart muscle, they increase contractility.
- In the kidney, they increase the secretion of renin.
* 2 receptors are in the areas not innervated by the sympathetic
nervous system, in the vascular smooth muscle of skeletal muscles, in
the walls of GI tract and in the brochioles.
- They are sensitive to different catecholamines.
- activate G proteins,
- stimulate adenyl cyclas
- decrease the level of calcium in the cells.
- cause the vasodilation and dilatation of bronchi,
- stimulation of insulin release,
- increase in lipolysis and glyconeogenesis.