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115 Cards in this Set
- Front
- Back
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Neuropharmacology
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The study of drug that alter processes controlled by the nervous system.
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Neuronpharmacologic agens
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These drugs are very theraputic, very useful, and widely used because all body processes are regulated by the nervous system.
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Neurological Body Functions
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Cardiac output
Gladular function Respirtory function Pain Perception Mood |
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Neurons
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nuerons elict response by nuerons and post synaptic cells. Without neurons there would be no drug benefit because there would be no drug reception.
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How nuerons regulate other cells.
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There are two basic processes by which neurons elicit responses from other cells. 1) axonal conduction and 2) synaptic transmission
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Post synaptic cell
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Could be another neuron, muscle cell, or a cell in a secretory gland.
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Major steps in nueron post-synaptic cell process.
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All three must happen
1) Conduction of action potential along axon of a neuron 2) Release of nuerotransmitter molecule from the axon terminal. 3) Binding of transmitter molecules to receptors on the post-synaptic cell. This is where agonist and antaginist come into play. |
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DRUG
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The drug is dependent on the type of neurotransmitter released, the receptor on the post-synaptic cell and eventst that take place.
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Synaptic CEll
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Changes in synaptic cell determine if the drug has a selective or non selective action
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DRUGS THAT WE WILL LOOK AT
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Most of the drugs that we will look at will be selective MEANING they target the specific cell/organs. THIS IS SYNAPTIC TRANSMISSION
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NON-SELECTIVE DRUGS
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ARE used with the AXON CONDUCTION meaning local anesthetics.
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IMPORTANT
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Receptors are going to influence the abiiity of a neuon to influence the behavior of other cells. This will be based on the neurnons ability to alter recepor activity on the target cell
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STEPS IN SYNAPTIC TRANSMISSION
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Release of neuron transmitter across the synaptic gap. THe ability of a drug to pass a synaptic gap can enhance (quick and easy passage) or reduce (slow) the drug's effect.
1. Sythesis-Molecules are in the AXON. 2. Storage-Neurontransmitter is stored in the axon terminal. 3. Release-Action potential brings release from storage. ONly a small amount of neurotransmitter is released from with each action potential. 4. Receptor binding-The neurontramitter looks for something to bind to. 5. It is terminated--Neurotransmitter is gettin rid by reuptake, breakdown, and diffusion |
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MORT
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THIS IS GENERAL ANESTISHA
All organs are regulated by type a receptors. |
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Merv
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Does not affect others. There is a A organ, B organ and so on.
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ABOUT THE PNS
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1) Know receptor it is on (beta 1 or beta 2, etc)
2) Know normal respones like increased HR, BP, contraction 3) Know whether the drug will increase or decrease receptors activation. |
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OKAY THE PNS
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1) Somatic-VOLUNATORY/Feelings
2) Autonomic 1) Para-Peace 2) Symp-fight or flight |
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Autonomic Nervous System
Resp for |
Cardiac function
secretory glands like salivary, gastric, sweat and bronchial glands. 3) and Smooth muscle function-muscles of bronchi, blood vessals, urogenital, and GI tract. |
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Did you know about the PNS?
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Certain poisions will block the para system (incestides and nerve gas) so you will have high heart rate, bp, etc
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What includes in the Para system
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slows heart rate
increases gastric secretions emptying of bladder, bowel Focus of eye for near vision Constriction of the bronchiole smooth muscle. |
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Sympt Nervous System
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Regulation of cardiov system
Reg of body temp Compensation for loss of blood |
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Homeostatis
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OBJECT: This is the objective of the SNS tring to get peace back in.
Includes- Maintence of blood flow to brain Redistribution of blood flow during exercise Compensation for the loss of blood. |
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HOw is temp regulated?
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Blood flow is brought to the skin to increase or decrease heat loss.
2) Sympathetic nerves to sweat glands promote secretion of sweat when cooling is needed. 3) Erection of body hair when heat conservation is needed. |
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What is fight or flight?
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Increase In hr and bp
shunting of blood away from skin to skeletal muscles. Dilation of bronchi to improve oxygenation. Dilate pupil to increase visula acuity. Also, mobilizes stored energy, therby providing glucose for brain |
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ANS's Para and sym
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intervations help body function properly as a nervous system. THe targeted organ determines what goes into the process of regulation.
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what is Feedback?
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A proces tha tallows for a system to adjust itself by responding to incoming info. Most places in the body involve feedback.
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Feedback-------------
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Let's picture this:
From the Sensor to the brain and then to the spinal cord and then to the effector. SO S-------C-------S--E That is the main component of feedback. |
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Feedback is a
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REFLEX
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The most important phar aspect of body regulation is
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BP and is called the baroreceptor reflux.
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What is autonomic tone?
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This is the involunatary and constantly being scrutized
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What is the automic tone?
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This is involuntary and is scrutiized by the body. It can be by para or symp. IN most ORGANS it is usually the para that provides the predominant tone. Except in the vascular sytem.....where the symp is the dominant automic tone.
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Neurotransmitters of the PNS is??????????
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Two neurotransmitters are nver used at the same time.
The examples are 1. Acetylcholine: Most common Norepinephrine Epinephrine Dopamine |
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ACH is released by
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Para:
ALL preganglionic ALL postganglionic Sympth: All preganglionic Most post but some sympth go to sweat glands. ALL SOMOTOMATIC MOTOR NUERONS GO TO SKELETAL MUSCLES!!!!!!!!!!! |
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OKay now: Cholenergic-Receptors that mediate responses to Ach
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They either block or mimic the actions of ACh
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Nicotonic N
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all autonomic nervous system: Ganglia and adrenal medulla.
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Nicotinic N
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All autonomic Nervous System Ganglia and Adrenal Medulla
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Nicotinic M
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Neuromuscular junction
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Muscarinic
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All para target organs: eye, heart, lung, bladder, GI tract, Sweat Glands, Sex organs, Blood Vessals
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Cholenergic
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Receptors that mediate responses to ACH!!!!!!!
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Adrenergic
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Receptors that mediate responses to norepinephrine and epinephrine!!!!!!!!!!!!!
Examples are Alpha 1 & 2, Beta 1& 2 and Dopamine |
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Okay now to
Norepinephrine |
Responds to Alpha 1, 2 and Beta 1
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Epinephri
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responds to Alpha 1, 2 and Beta 1,2
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Dopamine
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Only binds with dopamine, but can influence the binding of alpha 1 and beta 1.
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Cholenergic Drugs
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Influence cholenergic receptors. They are associated with toxicity because they achieve toxic levels quick.
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Muscarinic Agonists
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Bethanechol
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Muscarinic Antagonists
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Atropine Known as a ANTICHOLENERGIC DRUG
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What is parasypathoneumetic Drug?
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Drugs that bind to muscarinic receptors. They act in similar response when give to parasym nervous system
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Atropine High dose Vs Low dose
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At low dose you get increased salivation and at highest dose you get decrease in stomach acid.
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Bethanechol
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What to know:
Treats non-obstructive urinary retention Take intake/outake to determine efficacy High Risk pop: counterindicated for those w/ peptic ulcer disease, urinary tract obstruction, intest obstruction, corna insuff, hypotension, asthmas and hyperthyoidism |
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More bethanecol
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Route: ORAL
Administer: 1 hour prior to eating or 2 hrs after. Do not admister with food. Evaluation: Insure a bedpan is around. Monitor I/O. Minimize adverse effects: salivation, sweating, urinary urgency, bradycardia, hypotension. Monitor BP and pulse and muscarinic excess. Also, look for toxicity- pt is salivating, sweating, defacation, slow Hr, severe low bp, Treat with ATROPINE and supportive measures. |
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Nicotinic N
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All autonomic Nervous System Ganglia and Adrenal Medulla
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Nicotinic M
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Neuromuscular junction
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Muscarinic
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All para target organs: eye, heart, lung, bladder, GI tract, Sweat Glands, Sex organs, Blood Vessals
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Cholenergic
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Receptors that mediate responses to ACH!!!!!!!
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Adrenergic
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Receptors that mediate responses to norepinephrine and epinephrine!!!!!!!!!!!!!
Examples are Alpha 1 & 2, Beta 1& 2 and Dopamine |
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Okay now to
Norepinephrine |
Responds to Alpha 1, 2 and Beta 1
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Epinephri
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responds to Alpha 1, 2 and Beta 1,2
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Dopamine
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Only binds with dopamine, but can influence the binding of alpha 1 and beta 1.
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Cholenergic Drugs
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Influence cholenergic receptors. They are associated with toxicity because they achieve toxic levels quick.
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Muscarinic Agonists
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Bethanechol
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Muscarinic Antagonists
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Atropine Known as a ANTICHOLENERGIC DRUG
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What is parasypathoneumetic Drug?
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Drugs that bind to muscarinic receptors. They act in similar response when give to parasym nervous system
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Atropine High dose Vs Low dose
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At low dose you get increased salivation and at highest dose you get decrease in stomach acid.
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Bethanechol
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What to know:
Treats non-obstructive urinary retention Take intake/outake to determine efficacy High Risk pop: counterindicated for those w/ peptic ulcer disease, urinary tract obstruction, intest obstruction, corna insuff, hypotension, asthmas and hyperthyoidism |
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More bethanecol
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Route: ORAL
Administer: 1 hour prior to eating or 2 hrs after. Do not admister with food. Evaluation: Insure a bedpan is around. Monitor I/O. Minimize adverse effects: salivation, sweating, urinary urgency, bradycardia, hypotension. Monitor BP and pulse and muscarinic excess. Also, look for toxicity- pt is salivating, sweating, defacation, slow Hr, severe low bp, Treat with ATROPINE and supportive measures. |
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What is a cholinerterase inhibitor?
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Fuction to prevent degration of Ach. This occurs as a result of Acetylcholinestace. It is non-selective. This inhibits cholinergenic junctions and has limited theraputic potential.
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What is Myasthenia Gravis?
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Neuromusclar disorder leading to fluctuating muscle weakness and predisposition to rapid weaking.
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2 Cholinerterase Inhibitors.
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Helps w/ the breakdown of Ach. MG pts need Ach.
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Reversible
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Moderate duration of effect
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Irreversible
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long lasting effect
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DRUG: Neostigmine
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Trade name: Prostigmine
Non-lipid soluble-does not cross the membrane. Route: Orally or parentally Oral is poorly abosrbed. Side effects: increased glandular secretions, increased motility of the GI, bradycardia, urinary urgency, bronical constriction, changes in pupillary function. |
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What is the theraputic effects of Neostigmine?
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Increased force of muscle contraction with appropriate dosing.
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Toxicity does to Neostigimin?
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Decreases the contraction of muscle.
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AE?
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Excessive musclaric stimulation results in excessive salivation and possibly for neuromuscular blockade which can lead to rapid muscle weakness and paralysis
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What is Neostigimin counterindicated in?
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Pts with pepticdisese , GI and urinary obstr, coronary insuff, hyperthyroidism and asthma
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What is physostigmine
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-This is a chonrinese inhibitor. Only difference is that IT does cross the membrane.
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What is physostigmine treated for?
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Glacoma or treat poisioning by atropine and other drugs that cause muscluar blockade. Usually take 2 mg by IV or IM.
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What is irrersible chorisese inhiibior?
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-Long lasting; causing muscle contraction.
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Example of Irreversible chorisese inhibitor?
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Ecothaphate
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What is Ecothaphate?
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-Used in treatment of glucacoma. Pharm conditions: last long time.
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What is toxicity of Ecothyp to decreahate?
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Pt will present with severe muscle weakness and paralysis
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Treatment of Cholinergic crisis?
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1) First provide mechanical ventilation in case of resp crisis.
2) Next treat with Atropine to decrease muscluaric stimulation. 3) Administer Prolaxidone to reverse the inhibition of cholinestarase. 4) Adminster Diazipam to prevent or treat seizures. |
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What is a myasthenic crisis?
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* when pt are undermedicated for MG.
* Symptoms are indentical to Cholinergic Crisis * Can lead to respitory paralysis. |
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How do determine b/t CC and MC?
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1) administer Cholinesterase inhibitor (ultra-short) name: Edrophonium
If symptoms allivate: it is MG. If symptoms worses it is CC Remember b/c we just did that the risk for paralysis is greater now. |
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What drug do you use to treat muscarinic Antagoist poisoning?
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PHysostigmine: 2mg IM or slow IV injection
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What is a neuromuscular blocking agent?
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Prevent Ach from activating nicotinic M on skeletal muscles. This promotes muscular relaxation. This drug is used during surgery, endo tubing, mech vent, and others
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What is the excitation/Contraction Coupling?
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The process by which an action potential in a motor neuron leads to contraction of a muscle.
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What is depolarization?
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Post charge go inside to circle to be with neg charge
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What is repolarization?
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Post charge moves back outside of cell.
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What is polarization?
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External surface is post and internal is neg. This is the RESTING STAGE.
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What is needed to have a sustained muscle contraction?
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The cycle must be continually repeated.
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How are neuro blocking agents categorized?
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Non-depolarization and depolarization
and time of action (long, immediate, short, ultra short acting) |
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What is a non-depolarizing neuromusclar agent?
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TUBOCURARINE
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Tubocurarine
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* Not lipid soluble
* cannot be given orally * no effect on CNS or baby does not cross B-B barrier * Competes with ACH for nicotine M receptor sites (this drug is an antagoist and does not activate these receptors.) |
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What does tubocurarine do?
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relaxes skeletal muscles, should be gradual, OD can lead to resp paralysis.
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Tubocurarine
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Give IV only
Remember can cause hypotension Normal liver and kidney metabolism, cannot be given orally usual dose is 40-60 units loading does with 20-30 units maintence dose. |
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What are the AE of Tubocurarine?
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Resp arrest, cardi effects, hypotension, bradycardia, dysrhythmias, cariac arrest.
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What are precaustions of Tubocurarine?
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*use very carefully with pat with MG,
*Some abnorm can cause alterations low potass-increase effect high pott-decrease effect |
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What is the toxicity of tubocurarine?
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1. prolonged apnea Manage with resp support and neostigmine to reverse neuromusclar blockade.
2. Massive histamine release,: runny nose, watery eyes. Tx: give antihistamine 3 Cardiovasc Collapse: Assess and treat individually |
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What is a DEPOLARIZIN NEUROMUSUCLAR AGENT?
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Succinylcholine
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Succinylcholine
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ultra short acting only depolarized agent in use clinically *M of Action -Binds to nicoltinic M receptors and causes depolarization. Remains bound and prevents repolarization. It has constant depolarization. Contact Depolarization: Causes paralysis This paralysis remains until levels drop |
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Succinylcholine: Pharm effects?
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Causes Flaccid Paralysis and has no effect on CNS
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What are the pharmacok of succinylcholine?
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peaks in 1 min
paralysis fades in 4-10 min B/c it is found in plasma it is called plasma cholineraterase. Metabolized in PLASMA not hepatic. |
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What are the theraputic uses of succinylcholine?
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*used during endotrach inhib, This drug is less desirable then tubocuranine. Better to be used in short duration.
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What are the AE of succinylcholine?
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PROLONGED APNEA WITH LOW PSEUDOCHOLINESTERASE Activity (b/c of genetics)
MALIGNANT HYPERTHERMIA> rare and fatal muscle ridigity elevation of body temp This is due to excesive and uncontrolled metabolic activity in muscle. POST OPPERATIVE MUSCLE PAIN -Develops 12-24 hrs after surgery HYPERKALEMIA Promotes excess potassium from tissue. Death from Cardiac arrest has developed Most likely w/ pts with burns, multiple trama, upper neuron injury. |
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What are the toxicity of succinylcholine?
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PROLONGED APNEA
NO TREATMENT FOR TOXICITY. |
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How is it administered and what is a typical dose?
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aval in solution or powder
usually IV but can be given IM Typical dose is 25-75 mg in a single IV injection |
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FINALLY FUCK FUCK FUCK I thought we were done with cholergic drugs
What is Ganglionic locking agents |
They lack selectivity so they are not used. Use only for Hypertension. Mecamylamine is the only agent
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What is an adrenrgic agonists?
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produce effect by activating adrenergic receptors. Reffered as sympathomimetics.
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What are the mechanism of Adrenergic Receptor Activation/d
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1) DIRECT RECEPTOR BINDING-Most common mechanism by which drug activate.
2) PROMOTION of NOREPHRINE RELEASE. acting on terminals of sympt nerves to cause NE release 3) INHIBITION of NE REUPTAKE-reuptake of NE is the major mechanism by which adrenergic transmission is terminated. By blocking NE reuptake, drug cause a buildup of NE and increase receptor activation. INHIBITION of NE Inactivation: MAOI increase NE available for release and enhance receptor activation. |
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What are the 2 classes of Adrenergic Agonist?
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Catecholamines
Noncatecholamines |
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What are the 2 differences b/t the two.
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1) oral usbility
2) Duration of action 3) Ability to act on CNS. |
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What is a Catecholamine?
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Epinephrine
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Epinephrine
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* cannot be usued orally; admistered topically, by injection or by inhalation
*alpha 1 and 2, beta 1,2 |
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What are the theraputic uses of Epinephrine?
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1) Delay absorption of anesthetica
2) Control superficial bleeding 3) Reduce nasal congestion 4) Elevate bp 5) Overcome AV heart block 6) Brochodilation 7) Anaphylactic Shock |
