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Carroll Pharm Lect 3
Physiology of the Peripheral NS
| Question | Answer |
|---|---|
| What are the divisions of the NS? | CNS (Brain & spinal cord); PNS: Somatic (Voluntary), Autonomic (Involuntary) – Parasympathetic, Sympathetic |
| What are the 3 functions of the autonomic NS? | Regulates the: heart, secretary glands, and smooth muscles |
| What are the 7 regulatory fxns of the parasympathetic NS? | -Housekeeping -Slowing of HR -Increased gastric secretion -Emptying of bladder/bowel -Focusing of the eye -constriction of pupil -contraction of bronchi |
| What are the fxns of the sympathetic NS? | -Fight or flight -increased HR/BP -mobilization of stored energy -dilation of pupils -dilation of bronchi -shunt blood from skin to muscle (cold with fear) |
| What are the three types of control the autonomic NS (ANS) has? | Opposition (HR) , complementary, or one division (blood vessels) |
| What is the anatomy of the PSNS? | Spinal cord --> preganglionic neuron --> ganglion --> postganglionic neuron --> various organs |
| What are the transmitters that occur at the various parts of the PSNS? | Spinal cord --> preganglionic neuron --> (ACh) ganglion --> postganglionic neuron -->(ACh) various organs |
| What are the locations of the receptor subtypes for: the PSNS? | Spinal cord --> preganglionic neuron --> (ACh) (N-N) ganglion --> postganglionic neuron -->(ACh) (M) various organs |
| What is the anatomy of the SNS?(2) | 1) Spinal cord --> preganglionic neuron --> ganglion --> postganglionic neuron --> various organs 2) Spinal cord --> preganglionic neuron --> Adrenal medulla --> various organs |
| What are the transmitters that occur at the various parts of the SNS? | 1) Spinal cord --> preganglionic neuron --> ganglion (ACh) --> postganglionic neuron --> (NE) various organs 2) Spinal cord --> preganglionic neuron --> ganglion (ACh) --> postganglionic neuron --> (ACh) sweat glands 3) Spinal cor |
| What are the locations of the receptor subtypes for: SNS? | 1) Spinal cord --> preganglionic neuron --> (ACh) (N-N) ganglion --> postganglionic neuron --> (NE) (Alpha or Beta) various organs 2) Spinal cord --> preganglionic neuron --> (ACh) (N-N) ganglion --> postganglionic neuron -->(ACh) (M) vari |
| What is the anatomy of the somatic motor system? | Spinal cord --> motor neuron --> skeletal muscle |
| What are the transmitters that occur at the various parts of the Somatic motor system? | Spinal cord --> motor neuron --> (ACh) skeletal muscle |
| What are the locations of the receptor subtypes for: Somatic motor system? | Spinal cord --> motor neuron --> (ACh) (N-M) skeletal muscle |
| What neurotransmitters are used in the PNS? | All ACH except after andrenal medulla = Epi, and the SNS for the various organs = NE |
| What are the two types of neurotransmitters? | Cholinergic (ACh) & Adrenergic (Epi & NE) |
| What are the three receptors for Cholinergic? | Nicotinin-N, Nicotinic-M, Muscarinic |
| What are the receptors for Andrenergic? | Alpha-1, Alpha-2, Beta-1, Beta-2, dopamine (only to dopamine) |
| Where is the location of the nicotinic-n receptor? | All ANS ganglia and the adrenal medulla |
| What is the response to receptor activation of the nicotinic-n receptor? | Stimulation of parasympathetic and sympathetic postganglionic nerves and release of Epi from the adrenal medulla |
| Where is the location of the nicotinic-M receptor? | Neuromuscular junction |
| What is the response to receptor activation of the nicotinic-m receptor? | Contraction of skeletal muscle |
| Where is the location of the muscarinic receptor? | All parasympathetic target organs: eyes, heart, lung, bladder, GI tract, Sweat glands, sex organs, blood vessels |
| What is the response to receptor activation of the muscarinic receptor? | Eyes: contracton of the ciliary muscle focuses the lens for near vision, contraction of the iris sphincter muscle causes decreased pupil diameter; heart: decreased rate; lung: Constriction of bronchi, promotion of secretions; bladder: Voiding |
| Where is the location of the Alpha-1 receptor? | Eye, arterioles (skin, viscera, mucous memb), veins, sex organs (male), bladder neck and prostatic capsule |
| What is the response to receptor activation of the Alpha-1 receptor? | Eye: Contraction of the radial muscle of the iris causes dilated pupils; Arterioles: Constriction; veins: Constriction; Sex organs (male): Ejaculation; Bladder neck and prostatic capsule: Contraction |
| Where is the location of the Alpha-2 receptor? | Presynaptic nerve terminals |
| What is the response to receptor activation of the Alpha-2 receptor? | Inhibition of transmitter release (not with an organ, works with feedback to tell to stop making if have enough) |
| Where is the location of the Beta-1 receptor? | Heat, kidney |
| What is the response to receptor activation of the Beta-1 receptor? | Heart: increased rate, force of contraction, AV conduction velocity; Kidney: rennin release |
| Where is the location of the Beta-2 receptor? | Arterioles (heart, lung, skeletal muscle), Bronchi, Uterus, Liver, Skeletal muscle |
| What is the response to receptor activation of the Beta-2 receptor? | Arterioles: Dilation Bronchi: Dilation Uterus: Relaxation Liver: Glycogenolysis Skeletal muscle: Enhanced contraction, glycogenolysis |
| Where is the location of the dopamine receptor? | kidney |
| What is the response to receptor activation of the dopamine receptor? | Dilation of kidney vasculature |
| What receptors does Epinephrine bind to? | Binds to all alpha and beta, no dopamine |
| What receptors does Norepinephrine bind to? | Binds to all alpha and beta-1, no beta-2 or dopamine |
| What receptors does Dopamine bind to? | Binds to dopamine & alpha-1, Beta-1, NO alpha 2 or beta-2 |
| What are the dominant receptors for the heart and lungs? | Heart: Beta-1; Lungs: Beta-2 |
| What are the receptor classifications for ACh? | Cholinergic Receptor--> Muscarinic OR Nicotinic |
| What are the receptor classifications for NE? | Adrenergic receptor --> Alpha OR Beta (including subclasses of 1 and 2) |
| What is the lifecycle of ACh? | Choline + acetyl CoA --> stored --> destroyed by acetylcholenssterase --> Uptake of choline |
| What is the lifecycle of NE? | Precursors --> Vesicles --> Reuptake (so no enzyme) --> converted to Epi from NE *important for Parkinson's |
| What are the 6 categories of Cholinergic drugs? | Muscarinic agonists, muscarinic antagonists, Ganglionic stimulating agents, ganglionic blocking agents, neuromuscular blocking agents, Cholinesterase inhibitors |
| What do Muscarinic agonists target | What is an example |
| What can Muscarinic antagonists cause | Where does this come from? What are some examples of what is seen with this? |
| What is an example of a Muscarinic antagonist | What are the uses and side effects? |
| What are some drug interactions to be aware of with Atropine? | Antihistamines, antipsychotics, antidepressants (all have Muscarinic affects anyways so get additive effects) |
| What occurs with low doses of atropine | High doses? |
| What are some side effects of Muscarinic poisoning? | Hot, dry, red, blind, crazy |
| What is used to treat Muscarinic poisoning? | Physostigmine – inhibitor of acetylcholinesterase |
| What are cholinesterase inhibitors? | Prevents degeneration of ACh by enzymes acetylCoA, reversible and irreversible |
| What is Neostigmine | Uses? Side effects? |
| What are the drug interactions to be aware of with Neostigmine? | Muscarinic antagonist, neuromuscular blockers |
| What is Myasthenia Gravis | Sx? |
| What is a neuromuscular blocking agent? | Blocks nicotinic-M |
| What is a ganglionic blocking agent? | Blocks nicotinic-N (largely replaced by newer drugs) |
| What are some char'cs of neuromuscular blocking agent? | Blocking nicotinic-M results in muscle relaxation Excitation-Contraction coupled : Depol – positive charge in, repol – pumps (+) out and relaxes muscle |
| What is an example of a non-depol Neuromuscular Blocking Agent | Mechanism of action? Uses |
| What are the drug interactions to be aware of with Tubocurarine? | Anesthetics & antibodies (intensity effects), and cholinesterase inhibitors (decs effects) |
| What is the mechanism of action of a depolarizing Neuromuscular blocking agent? | Binds to nicotinic-M receptors & remains bound resulting in constant depolarization |
| What therapy are neuromuscular blocking agents used and what for? | -Muscle relaxation during surgery (req anesthesia for unconsciousness) -Mechanical ventilation (req anesthetics, stop mov't to fight respirator) -Electroconvulsive Rx (Prevent convulsive mov't) -Endotracheal intubation (Prevent gag reflex) |
| What are some char'cs of Ganglionic blocking agents? | Lack selectivity, competes with ACh for binding to nicotinic-N receptors, controlled hypertension in surgery, side effects are dry mouth & blurred vision |
| What are some uses of Adrenergic Agonists? | Sympathomimetics – work on SNS -direct receptor binding -Promotion of NE release (indirect) -inhibition of NE uptake (indirect, termination) -Inhibition of NE inactivation (Indirct, MAO) |
| What are the two categories of Adrenergic Agonists? | Catecholamines & Noncatecholamines |
| What are some examples and char'cs of Catecholamines? | Adrenergic agonists – Epi, Isoproterenol, Dopamine -not given orally, MAO & COMT – both degrade so not orally -cannot cross the BBB -Shorter duration of action |
| What are some examples and char'cs of Noncatecholamines? | Adrenergic agonists – Ephedrine & Terbutaline -given orally -penetrate BBB, so longer duration of action |
| What is seen with activation of the receptor: Alpha-1? Uses? | -Vasoconstriction – hemostaisis (Epi) -Nasal decongestion (Phenylephrine & Ephedrine) -delay of anesthetic absportion (epi) -elevation of BP -pupil dilation |
| What are the side effects of Alpha-1 activation? | Hypertension, necrosis, bradycardia – mostly due to inc BP |
| What is seen with activation of the receptor: Alpha -2? Uses? | Peripheral-inhibits NE release (little clinical value) CNS-reduce stimulation of adrenergic receptor, indirect acting antiadrenergic agents |
| What is seen with activation of the receptor: Beta-1? Uses? | Cardiac arrest (get contraction in heart going again), heart failure, Shock, AV heart block |
| What are the side effects of Beta-1 activation?? Altered heart rate or rhythm, angina | |
| What is seen with activation of the receptor: Beta-2 | Uses? |
| What are the side effects of Beta-2 activation? | Hyperglycemia (breakdown glucogen to glucose), tremor |
| What is seen with activation of the receptor: Dopamine | Uses? |
| What are the three Sx of anaphylactic shock | What is used to treat it? |
| Receptors, use, side effects, drug interactions of: Epinephrine? | Alpha-1& 2, Beta -1&2…. Anaphylactic shock, delay absorption of anesthetics, homeostasis, overcome AV heart block, pupil dilation, asthma… SE: Hypertensive crisis, dysrhythmias, angina, necrosis, hyperglycemia…. DI:MAO inhibitors (intensify), Tricyclic an |
| Receptors, use, side effects, drug interactions of: Norepinephrine?? Alpha-1&2, beta-1, NO beta-2…. Uses: Hypotension & cardiac arrest…. SE: Same as epi by no hyperglycemia….. DI: Same as Epi | |
| Receptors, use, side effects, drug interactions of: Isoproterenol? | Beta-1&2…. Use: AV Heart block, asthma, bronchospasm….. SE: dysrhythmias, angina, hyperglycemia, and decr fever….. DI: Same as Epi |
| Receptors, use, side effects, drug interactions of: Dopamine? | Dopamine, beta-1, beta-2…. Use: Shock, heart failure, acute renal failure…. SE: tachycardia, dysrhythmias, angina, necrosis…. DI: same as epi |
| What are examples of noncatecholamines? | Terbutaline & Ephedrine |
| Receptors, use, side effects, of: Terbutaline? | Beta-2… uses: asthma, delay of preterm labor…. SE: Tremor |
| Receptors, use, side effects of: Ephedrine? | Alpha-1 & 2, Beta-1&2… mixed drug (direct activation of alpha & beta, indirect activation by releasing NE)…. Uses: Nasal congestion, narcolepsy… SE: Same as Epi + insomnia (crosses BBB) |
| Use, and side effects of: Alpha-Adrenergic Antagonists? | Use: Hypertension, reversal of alpha-1 agonist toxicity, BPH, Raynauds…. SE: Orthostatic hypotension, reflex tachycardia, nasal congestion |
| What is the receptor, use, and side effects of Prazosin? | Alpha-Adrenergic antagonist…. Alpha-1, hypertension, BPH… SE: orthostatic hypotension, reflex tachycardia, nasal congestion |
| What is the receptor, use, and side effects of Phentolamine? | Alpha-adrenergic antagonist…. Alpha-1&2…. Pheochromocyoma…. SE: Same as Prazosin (orthostatic hypotension, reflex tachycardia, nasal congestion) |
| What are the uses and side effects of Beta-adrenergic antagonists? | Use: Angina pectoris, hypertension, dysrhythmias, MI, Heart failure….. SE: Beta-1, Bradycardia, heart failure, AV heart block…. Beta-2, bronchoconstriction, inhibits glycogenolysis (diabetic depend on for too much insulin) |
| What are the receptors, uses, side effects, contraindications, and drug interactions for Propranolol? | Beta-Adrenergic Antagonist… Beta-1&2…. Uses: hypertension, angina, MI… SE: bradycardia, heart failure, inhib of glycogenolysis, bronchoconstriction, CNS effects…. Contra: Diabetics, severe allergic reaction, heart failure, asthma, depression….. DI: Calci |
| What are receptors, uses, side effects, and contraindications for Metopholol? | Beta-1 blocker (diabetics can use b/c of no Beta-2)…. Use: Hypertension, pts with asthma or diabetes & angina or MI…. SE: Bradycardia, AV heartblock… Contra: Heart failure, sinus bradycardia |
| What is an example of an adrenergic neuron-blocking agent… mechanism of action, uses, side effects? | Reserpine… suppresses NE synthesis & displaces NE from vesicles…. Use: Hypertension… SE: Depression, bradycardia, orthostatic hypotension |
| What are two examples of centrally acting alpha-2 agonist? | Clonidine & Methyldopa |
| What are mech of action, uses, and side effects of Clonidine? | Activates alpha-2 receptors to decrease transmitter release… uses: Hypertension, severe pain…. SE: Drowsiness, dry mouth, rebound hypertension |
| What are mech of action, uses, and side effects of Methyldopa? | Similar to clonidine except must be converted to methyINE…. Uses: hypertension…. SE: Hemolytic anemia & liver toxicity |
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