Autonomic Drugs Flashcards
The Nervous System is divided into two categories mainly:
- Central Nervous System
- Peripheral Nervous System
Central Nervous System is composed of
- brain
- spinal cord
Peripheral Nervous System is composed of
- neuronal tissues outside the CNS
In terms of functionality, CNS is divided into two components:
- Somatic
- Autonomic
The ——— is largely independent (autonomous) in that its activities are not under direct conscious control.
autonomic nervous system (ANS)
It is concerned primarily with control and integration of visceral functions necessary for life such as cardiac output, blood flow distribution, and digestion.
Autonomic Nervous System (ANS)
Evidence is accumulating that the ANS, especially what nerve that also influences immune function and some CNS functions such as seizure discharge?
vagus nerve
What nerves can also influence cancer development and progression?
autonomic nerves
The motor portion of somatic subdivision is largely concerned with consciously controlled functions such as (MRP)
movement, respiration, and posture
The nervous system has several properties in common with what system?
endocrine system
The nervous system has several properties in common with what system?
endocrine system
It takes place through the release of small amounts of transmitter substances from the nerve terminals into the synaptic cleft.
Chemical transmission
It takes place through the release of small amounts of transmitter substances from the nerve terminals into the synaptic cleft.
Chemical transmission
The transmitter crosses the cleft by —— and activates or inhibits the postsynaptic cell by binding to a specialized receptor molecule.
diffusion
In a few cases, what transmission may occur from the postsynaptic cell to the presynaptic neuron terminal and modify its subsequent activity.
retrograde transmission
By using—— that mimic or block the actions of chemical transmitters, we can selectively modify many autonomic functions.
drugs
transmitters, we can selectively modify many autonomic functions. These functions involve a variety of effector tissues, including (csvpe)
cardiac muscle, smooth muscle, vascular endothelium, exocrine glands, and presynaptic nerve terminal
transmitters, we can selectively modify many autonomic functions. These functions involve a variety of effector tissues, including (csvpe)
cardiac muscle, smooth muscle, vascular endothelium, exocrine glands, and presynaptic nerve terminal
The ANS lends itself to division on anatomic grounds into two major portions: (SP)
the sympathetic (thoracolumbar) division and the parasympathetic (traditionally “craniosacral) division
The ANS lends itself to division on anatomic grounds into two major portions: (SP)
the sympathetic (thoracolumbar) division and the parasympathetic (traditionally “craniosacral) division
Most thoracic and lumbar sympathetic preganglionic fibers are short and terminate in ganglia located in the ———chains that lie on either side of the spinal column.
paravertebral
Most of the remaining sympathetic preganglionic fibers are somewhat longer and terminate in—————, which lie in front of the vertebrae, usually on the ventral surface of the aorta.
prevertebral ganglia
Most of the remaining sympathetic preganglionic fibers are somewhat longer and terminate in—————, which lie in front of the vertebrae, usually on the ventral surface of the aorta.
prevertebral ganglia
Some preganglionic parasympathetic fibers terminate in parasympathetic ganglia located outside the organs innervated: (COPS)
the ciliary, pterygopalatine, submandibular, and otic ganglia.
Several ——— are innervated by sacral preganglionic nerves
pelvic ganglia
The ————is a large and highly orga- nized collection of neurons located in the walls of the gastrointes- tinal (GI) system
enteric nervous system (ENS)
The primary transmitter at ANS ganglia, at the somatic neuromuscular junction, and at parasympathetic postganglionic nerve endings. A primary excitatory transmitter to smooth muscle and secretory cells in the ENS. Probably also the major neuron-to-neuron (“ganglionic”) transmitter in the ENS.
Acetylcholine (ACh)
Acts as a transmitter or cotransmitter at many ANS-effector synapses.
Adenosine triphosphate (ATP)
Found with substance P in cardiovascular sensory nerve fibers.
- Present in some secretomotor ENS neurons and interneurons.
- A cardiac stimulant.
Calcitonin gene-related peptide (CGRP)
Found with substance P in cardiovascular sensory nerve fibers.
- Present in some secretomotor ENS neurons and interneurons.
- A cardiac stimulant.
Calcitonin gene-related peptide (CGRP)
May act as a cotransmitter in some excitatory neuromuscular ENS neurons.
Cholecystokinin (CCK)
A modulatory transmitter in some ganglia and the ENS. Possibly a postganglionic sympathetic transmitter in renal blood vessels.
Dopamine
A modulatory transmitter in some ganglia and the ENS. Possibly a postganglionic sympathetic transmitter in renal blood vessels.
Dopamine
Present in some secretomotor and interneurons in the ENS. Appear to inhibit ACh release and thereby inhibit peristalsis. May stimulate secretion.
Enkephalin and related opioid peptides
Present in secretomotor neurons; may play a role in appetite-satiety mechanisms
Galanin
May have presynaptic effects on excitatory ENS nerve terminals.
- Has some relaxant effect on the gut. Prob- ably not a major transmitter in the ENS.
GABA (γ-aminobutyric acid)
May have presynaptic effects on excitatory ENS nerve terminals.
- Has some relaxant effect on the gut. Prob- ably not a major transmitter in the ENS.
GABA (γ-aminobutyric acid)
Extremely potent excitatory transmitter to gastrin cells. Also known as mammalian bombesin.
Gastrin-releasing peptide (GRP)
- Found in many noradrenergic neurons.
- Present in some secretomotor neurons in the ENS and may inhibit secretion of water and electrolytes by the gut.
- Causes long-lasting vasoconstriction. It is also a cotransmitter in some parasympathetic postganglionic neurons.
Neuropeptide Y (NPY)
- Found in many noradrenergic neurons.
- Present in some secretomotor neurons in the ENS and may inhibit secretion of water and electrolytes by the gut.
- Causes long-lasting vasoconstriction. It is also a cotransmitter in some parasympathetic postganglionic neurons.
Neuropeptide Y (NPY)
A cotransmitter at inhibitory ENS and other neuromuscular junctions; may be especially important at sphincters.
Nitric oxide (NO)
The primary transmitter at most sympathetic postganglionic nerve endings.
Norepinephrine (NE)
An important transmitter or cotransmitter at excitatory neuron-to-neuron junctions in the ENS.
Serotonin (5-HT)
- An important sensory neurotransmitter in the ENS and elsewhere.
- Appear to be excitatory cotransmitters with ACh at ENS neuromuscular junctions.
- Found with CGRP in cardiovascular sensory neurons.
- It is a vasodilator (probably via release of nitric oxide).
Substance P, related tachykinins
- Excitatory secretomotor transmitter in the ENS; may also be an inhibitory ENS neuromuscular cotransmitter.
- A probable cotransmitter in many cholinergic neurons.
- A vasodilator (found in many perivascular neurons) and cardiac stimulant.
Vasoactive intestinal peptide (VIP)
The ENS includes two plexus which are ? (MS)
myenteric plexus and the submucous plexus
myenteric, is plexus of ———
Auerbach
myenteric, is plexus of ———
Auerbach
submucous is plexus of
Meissner
Transmit chemical and mechanical information from the mucuosa and from stretch receptors to motor neurons in the plexuses.
Sensory fibers
It functions in semiautonomous manner and also proviides necessary synchronization of impulses
ENS - Enteric Nervous System
Classic synapses such as —— are relatively “tight”in that the nerve terminates in small bouttons very close to the tissue innervated
- Mammalian neuromuscular junctions and most neuron-neuron synapses
A large number of peripheral ANS fibers synthesize and release acetylcholine
Cholinergic fibers
Most postganglionic sympathetic fibers release ——
- they are noradrenergic (often called simply “adrenergic”) fibers
norepinephrine (also known as noradrenaline
Five key features of neurotransmitter function provide potential targets for pharmacologic therapy: (SSRTR)
synthesis, storage, release, termination of action of the transmitter, and receptor effects.
Vesicles are provided with ——— which serve to align them with release sites on the inner neuronal cell membrane and participate in triggering the release of transmitter.
vesicle-associated membrane proteins (VAMPs)
The release site on the inner surface of the nerve terminal membrane contains ———, which interact with VAMPs. VAMPs and SNAPs are collectively called ——
- synaptosomal nerve-associated proteins (SNAPs)
- fusion proteins
Acetylcholine (ACh) is synthesized in the cytoplasm from acetyl-CoA and choline through the catalytic action of the enzyme ——
choline acetyltransferase (ChAT)
Acetyl-CoA is synthesized in —— , which are present in large numbers in the nerve ending.
mitochondria
Choline is transported from the extracellular fluid into the neuron terminal by a sodium-dependent membrane called
choline transporter
This symporter can be blocked by a group of research drugs called
hemicholiniums
Once synthesized, acetylcholine is transported from the cytoplasm into the vesicles by a vesicle-associated transporter (VAT) that is driven by
proton efflux
The antiporter can be blocked by the research drug
vesamicol
The antiporter can be blocked by the research drug
vesamicol
The antiporter can be blocked by the research drug
vesamicol
Storage of acetylcholine is accomplished by the packaging of —— of acetylcholine molecules (usually ——— molecules in each vesicle).
“quanta”
- 1000–50,000
Most of the vesicular acetylcholine (a positively charged quaternary amine) is bound to negatively charged ——
vesicular proteoglycan (VPG).
Vesicles are concentrated on the inner surface of the nerve terminal facing the synapse through the interaction of so called SNARE proteins on the vesicle (a subgroup of VAMPs called v-SNAREs, especially—— )
synaptobrevin
On the inside of the terminal
cell membrane (SNAPs called t-SNAREs, especially ——).
syntaxin and SNAP-25
Calcium interacts with the VAMP — — on the vesicle membrane and triggers fusion of the vesicle membrane
synaptotagmin
The acetylcholine vesicle release process is blocked by———— through the enzymatic cleavage of two amino acids from one or more of the fusion proteins.
botulinum toxin
The acetylcholine vesicle release process is blocked by———— through the enzymatic cleavage of two amino acids from one or more of the fusion proteins.
botulinum toxin
After release from the presynaptic terminal, acetylcholine molecules may bind to and activate an acetylcholine receptor called ——
cholinoceptor
After release from the presynaptic terminal, acetylcholine molecules may bind to and activate an acetylcholine receptor called ——
(cholinoceptor)
Adrenergic neurons transport the precursor amino acid —— into the nerve ending, convert it to ——, and then synthesize a catecholamine transmitter
tyrosine - dopa - dopamine/
norepinephrine or epinephrine
In most sympathetic postganglionic neurons,—— is the final product.
norepinephrine
In most sympathetic postganglionic neurons,—— is the final product.
norepinephrine
Several processes in these nerve terminals are potential sites of drug action. One of these, the conversion of tyrosine to dopa by tyrosine hydroxylase, is the rate-limiting step in—— synthesis.
catecholamine transmitter
Tyrosine hydroxylase can be inhibited by the tyrosine analog ——
metyrosine
A high-affinity antiporter for catecholamines located in the wall of the storage vesicle (vesicular monoamine transporter, VMAT) can be inhibited by the ————
reserpine alkaloids
A high-affinity antiporter for catecholamines located in the wall of the storage vesicle (vesicular monoamine transporter, VMAT) can be inhibited by the ————
reserpine alkaloids
Reserpine and related drugs such as ———— cause depletion of transmitter stores.
tetrabenazine, deutetrabenazine
Reserpine and related drugs such as ———— cause depletion of transmitter stores.
tetrabenazine, deutetrabenazine
Another transporter called ——— carries norepinephrine and similar molecules back into the cell cytoplasm from the synaptic cleft
norepinephrine transporter, NET
NET is also commonly called —— and is partially responsible for the termination of synaptic activity.
uptake 1 or reuptake 1
NET can be inhibited by——— , resulting in an increase of transmitter activity in the synaptic cleft
cocaine and certain antidepressant drugs
NET can be inhibited by——— , resulting in an increase of transmitter activity in the synaptic cleft
cocaine and certain antidepressant drugs
Indirectly acting and mixed-action sympathomimetics ———— are capable of releasing stored transmitter from noradrenergic nerve endings by a calcium-independent process. (TAE)
tyramine, amphetamines, and ephedrine
Indirectly acting and mixed-action sympathomimetics ———— are capable of releasing stored transmitter from noradrenergic nerve endings by a calcium-independent process. (TAE)
tyramine, amphetamines, and ephedrine
inhibit monoamine oxidase and have other effects that result in increased norepinephrine activity in the synapse
Amphetamines
The primary acetylcholine receptor subtypes were named after the alkaloids originally used in their identification: muscarine and nicotine,————
muscarinic and nicotinic receptors.
The primary acetylcholine receptor subtypes were named after the alkaloids originally used in their identification: muscarine and nicotine,————
muscarinic and nicotinic receptors.
the term adrenoceptor is widely used to describe receptors that respond to catecholamines such as ——
norepinephrine
By analogy, the term cholinoceptor denotes receptors (both muscarinic and nicotinic) that respond to ——
acetylcholine
The general class of adrenoceptors can be further subdivided into ———— types on the basis of both agonist and antagonist selectivity and on genomic grounds.
α - adrenoceptor, β-adrenoceptor, and dopamine-receptor
The general class of adrenoceptors can be further subdivided into ———— types on the basis of both agonist and antagonist selectivity and on genomic grounds.
α - adrenoceptor, β-adrenoceptor, and dopamine-receptor
What cholinoceptor is located at CNS neurons, sympathetic postganglionic neurons, some presynaptic sites?
Muscarinic M1
What cholinoceptor can be found at Myocardium, smooth muscle, some presynaptic sites; CNS neurons
Muscarinic M2
What cholinoceptor can be found at Exocrine glands, vessels (smooth muscle and endothelium); CNS neurons
Muscarinic M3
What cholinoceptor is located at CNS neurons; possibly vagal nerve endings
Muscarinic M4
What cholinoceptor is located at CNS neurons; possibly vagal nerve endings
Muscarinic M4
What cholinoceptor is located at Vascular endothelium, especially cerebral vessels; CNS neurons?
Muscarinic M5
What cholinoceptor is located at Postganglionic neurons, some presynaptic cholinergic terminals; pentameric receptors typically contain α- and β-type subunits only?
Nicotinic NN
What cholinoceptor can be found at Skeletal muscle neuromuscular end plates; receptors typically contain two α1- and β1-type subunits in addition to γ and δ subunits?
Nicotinic NM
What adrenoceptor is located at post synaptic effector cells, especially smooth muscle?
Alpha1
What adrenoceptor is located at
Presynaptic adrenergic nerve terminals, platelets, lipocytes, smooth muscle?
Alpha2
What adrenoceptor is located at
Postsynaptic effector cells, especially heart, lipocytes, brain; presynaptic adrenergic and cholinergic nerve terminals, juxtaglomerular apparatus of renal tubules, ciliary body epithelium
Stimulation of adenylyl cyclase, increased cAMP
Beta1
What adrenoceptor is located at Postsynaptic effector cells, especially smooth muscle and cardiac muscle
Beta2
What adrenoceptor is located at Postsynaptic effector cells, especially smooth muscle and cardiac muscle
Beta2
What adrenoceptor is located at Postsynaptic effector cells, especially lipocytes; heart
Beta3
What adrenoceptor is located at Postsynaptic effector cells, especially lipocytes; heart
Beta3
What dopamine receptors are located at Brain; effector tissues, especially smooth muscle of the renal vascular bed
D1 (DA1), D5
What dopamine receptors are located at Brain; effector tissues, especially smooth muscle of the renal vascular bed
D1 (DA1), D5
what dopamine receptor is located at Brain; effector tissues, especially smooth muscle; presynaptic nerve terminals
D2 (DA2)
What dopamine receptor is located at brain?
D3
What dopamine receptor is located at brain?
D3
What dopamine receptor is located at Brain and, cardiovascular system?
D4
A neurotoxin derived from chili peppers, can cause the release of transmitter (especially substance P) from such neurons and, if given in high doses, destruction of the neuron.
Capsaicin
A neurotoxin derived from chili peppers, can cause the release of transmitter (especially substance P) from such neurons and, if given in high doses, destruction of the neuron.
Capsaicin
In the small intestine, for example, these neurons contain one or more of the following:
nitric oxide synthase (which produces nitric oxide, NO), calcitonin gene-related peptide, cholecystokinin, dynorphin, enkephalins, gastrin-releasing peptide,
5-hydroxytryptamine (5-HT, serotonin), neuropeptide Y, somatostatin, substance P, and vasoactive intestinal peptide (VIP)
In the small intestine, for example, these neurons contain one or more of the following:
nitric oxide synthase (which produces nitric oxide, NO), calcitonin gene-related peptide, cholecystokinin, dynorphin, enkephalins, gastrin-releasing peptide,
5-hydroxytryptamine (5-HT, serotonin), neuropeptide Y, somatostatin, substance P, and vasoactive intestinal peptide (VIP)
nitric oxide synthase (which produces nitric oxide, NO), calcito- nin gene-related peptide, cholecystokinin, dynorphin, enkeph- alins, gastrin-releasing peptide, 5-hydroxytryptamine (5-HT, serotonin), neuropeptide Y, somatostatin, substance P, and vaso- active intestinal peptide (VIP)
parasympathetic system is a —— (leading to growth) used to “rest and digest”
trophotropic
parasympathetic system is a —— (leading to growth) used to “rest and digest”
trophotropic
sympathetic system is a —— (leading to energy expenditure), which is activated for “fight or flight”
ergotropic
Primary controlled variable in cardiovascular function is called ——
mean arterial pressure
Increase in peripheral vascular resistance, increases mean arterial pressure that often ———
a slowing of heart rate
It is the reflex compensatory response elicited by norepinephrine
Bradycardia
Presynaptic receptors that respond to the primary transmitter substance released by the nerve ending are called —— that ate usually inhibitory
autoreceptors
The ——— is a cranial nerve that connects the brain to the body’s organs. It’s part of the autonomic nervous system, which regulates involuntary bodily functions.
- carry signals between heart, brain snd digestive system
vagus nerve
Regulatory receptors that respond to many other substances are called
heteroreceptors
Marked contraction of the ciliary muscle, which often occurs with cholinesterase inhibitor intoxication is called
cyclospasm
Marked contraction of the ciliary muscle, which often occurs with cholinesterase inhibitor intoxication is called
cyclospasm
