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121 Cards in this Set

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What type of autonomic receptors are on the cardiac and smooth muscle, gland cells, and nerve terminals coming out of the medulla?
Ach and M
What type of autonomic receptors are on the sympathetic sweat glands?
Ach and M
What type of autonomic receptors on the cardiac and smooth muscle, gland cells, and nerve terminals coming out of the spinal cord?
NE, alpha, beta
What type of autonomic recepttors on the renal vascular smooth muscle?
D, D1
What are the local mediator chemical signals?
Histamine + prostaglandins
What are the neurotransmistters?
1. NE, 2. Ach, 3. dopamin, 4. serotonin, 5. histamine, 6. Gamma-aminobutyric acid (GABA)
What drug interferes w/the CHT(choline transporter) transporter?
Hemicholinums - no choline is getting into nerve terminal to make Ach
What drug interferes w/the VAT(vesicular) transporter?
Vesamicol - inhibit vesical transporter -> Ach is formed but cannot be put into vesicle.
What drug interferes w/SNAPs transporters in a cholinergic axon?
Botulinum toxin - prevents receptors to bind w/pre-synapse membrane(Thus no Ach Release)
What drug interferes w/NET
Cocaine, tricyclic anti-depressants
What drug interferes w/VMAT?
Reserpine
What drug interferes w/SNAPS in an adrenergic axon?
Bretylium, guanethidine
What drug interferes w/tyrosine hydroxylase
Methyrosine
Receptors coupled to ion channels
NT binds to ion channel -> allows influx of ions to induce change in membrane potential
Receptors coupled to adenylcyclase
Hormone/NT -> Gs/Gi -> adenylcyclase (on or off)
Receptors coupled to diacylglycerol and inositol triphosphate
Hormone/NT -> Gq -> phospholipase C -> DAG/IP3 -> ↑ [Ca2+]
What are the ways of post-synaptic regulation
1. Normal transmission, 2. up-regulation(aka sensitization), 3. down-regulation (desensitization)
How does up-regulation of post-synaptic receptors work?
Normal amount of NT is release but there is an Antagonist that blocks a lot of receptors thus you lose signal. The body upregulates more receptors to bring back normal amount of response to NT. Thus now w/o antagonist there is much more response to a normal [NT]
How does down-regulation of post-synaptic receptors work?
Normal amount of NT is released but there is an agonist that binds to the receptors. The body down regulates the receptors because it want to keep the signal transmission the same as it was. Thus now w/o the agonist there is a decreased response to a normal [NT]
What is the sympathetic NT on the effector organs?
Norepinephrine
What is the parasympathetic NT on the effector organs?
acetylcholine
What is the function of sympathetic nervous system?
1. ↑ heart rate, 2. ↑ blood pressure, 3. mobilize energy stores, 4. ↑ blood flow to skeletal muscles and heart, 5. dilates pupils/bronchioles
What is the function of sympathetic NS?
Fight or flight
Function of parasympathetic nervous system
Maintains essential bodily functions - digestive processes, elimination of waste, rest and digest
What is the function of vagal parasympathetic innv
Slows HR
What is the function of sympathetic innv
Increases HR
What are the only organs that have sympathetic innv
1. Adrenal medulla, 2. kidney, 3. pilomotor muscles, 4. sweat glands, 5. control of BP
Which direction is feedback control?
Afferent impulses (towards)
What is the function of muscarinic receptors?
Its effects are the same as the parasympathetic NS.
Which direction is reflex arcs?
Efferent impulses (away)
What is the MOA of the body when it detects a decrease in BP?
Afferent signal (senses ↓ BP) -> efferent response (↑ CO) -> ↑ BP
What type of receptor is used in muscarinic-cholinergic receptors?
7-transmembrane domains coupled to G-protein coupled receptors
Location of M4 and M5
CNS
What is M1-M3?
Functionally characterized
What is the function of nicotinic-cholinergic receptors?
Ligand-gated ion channel- binds 2 Ach molecules -> allows Na+ entry -> depolarization of cell; NOTE: Ach stimulates receptor -> then blocks
M1 receptor - location, features, mechanism
Location = nerves, Featuers = 7Transmembrane + Gq, Mechanism = IP3 + DAG
M2 receptor - location, features, mechanism
Location = heart, nerves, Smooth muscle, features = 7Transmembrane receptor + Gi/o, Mechanism = inhibition of cAMP production, activation of K+ channels
M3 receptor - location, features, mechanism
Location = glands, smooth muscle, endothelium, features = 7 transmembrane receptors + Gq, mechanism = IP3 + DAG
What are the 2 ways for cholinergic activation?
1. Direct acting (alkaloids or choline esters), 2. indirect acting (reversible or irreversible)
What are the choline esters we need to know?
1. Acetylcholine, 2. methacholine, 3. carbachol, 4. bethanechol
What are the characteristics of direct-acting cholinergics?
1. Insoluble in lipids, 2. hydrolyzed in GI tranct, 3. IV bolus has brief effect, 4. Intramuscular and subcutaneous injections produce local effects
What are the alkaloid drugs we need to know
Pilocarpine, nicotine, muscarine
How are alkaloids taken?
Liquid nicotine -> absorbed transdermally, muscarine is incompletely absorbed from gut -> but can be toxic when ingested
What type of pH urine ↑ clearance of pilocarpine and nicotine?
Acidification of urine accelerates clearance of pilocarbine and nicotine
How does Ach work in the parasympathetic system?
Ach -> activates muscarinic receptors on effector cells -> inhibits the release of their neurotransmitters (acts indirectly)
What is the MOA of direct acting nicotinic receptor?
Channel opens Na+ and K+ ions to diffuse -> cellular depolarization -> causes skeletal muscle depolarization -> thus contraction of muscle
What is the MOA of depolarizing blockade of nicotinic receptor?
Long term agonist occupies the receptor -> postganglionic neuron stops firing -> skeletal musclerelaxes even though the membrane potential is back to normal
What are the different types of organophosphates?
1.echothiophate, 2. soman
What are the different thiophosphates?
1. Parathione, 2. malathion
Why are acting cholinomimetics dangerous?
Lipid soluble ->
What are some unique characterisitcs of edrophonium and neostigmine?
Poor absorbtion of conjunctiva, skin, and lungs -> thus hard to get toxic effects
What are some unique characteritiscs of physostigmine
Well absorbed on all sites + used on the eye
What is the MOA of organophosphate?
Cholinesterase inhibitors are well absorbed skin, lung, gut, and conjuctiva -> dangerous to humans and highly effective as insecticides
What is the MOA of thiophosphate insecticides
Malathion are lipid soluble and rapidly absorbed -> must be activated in the body to the oxygen analogs (kills insects fast)
What is the MOA of indircet-acting cholinomimetics
1. Inhibis acetylcholinesterase -> ↑ [Ach], 2. butyrylcholinesterase inhibited
What is the duration of quaternary alcohols
Edrophonieum - 2-10 mins
What is the duration of carbamate esters
Phisostigmine - 30 mins -> 6 hrs
What is the duration of organoshosphates
irreversible
What is the process of "aging"
The longer the duration of action the harder it is to release an ethyl group
What reactivates the inhibited acetylcholinesterase?
Pralidoxime - displaces phosphate group and regenerates the enzyme
What are the systemic effects of activation of muscarinic receptors - eye? Secretory? Gastrointestinal? Genitourinary? Respiratory? Cardiovascular?
Activation of parasympathetics = eye = miosis, secretory = sweat, lacrimal, and nasopharyngeal glands, GI = ↑ motor activity,
What is unique about bethanechol
Structurally related to Ach and Not hydrolyzed by acetylcholinesterase -> thus activates the receptor for 1hr -> stimulates an atonic bladder -> neurotonic atony + megacolon is cured
What drug mimics Ach in the eye?
carbachol
What is the drug pilocarpine used for?
Produces rapid miosis and contraction of ciliary muscle
What drug is used to treat sjogren syndrome?
Oral Pilocarpine - dry mouth, lack of tears
What is the cure to overdose of anti-cholinergic drugs (atropine, phenothiazines, tricyclic anti-depressants)
physostigmine
What is the treatment of open angle glaucoma?
echothiophate
What drug is used to diagnose myasthenia gravis? Treatment?
Edrophonium = diganose, treatment = pyridostigmine
What are they Achase inhibitors used in alzheimers disease?
Tacrine, donepezil, rivastigmine, galantamine
What is the cure to chronic nicotine toxicity(smoking)
Veranicline - partial nicotinic receptor agonist and antagonist
Where are the major sources of Achase inihibitor toxicity?
Pesticides in agriculture + the home (RAID)
What are the treatments of Achase inhibitor toxicity?
Atropine + pralidoxime
What are the symptoms seen with parasympathetic NS activation?
DUMB-BELSS = Diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation (CNS), lacrimatino, salivation, sweating
What are the antimuscarinic drugs?
Atropine
What are the antinicotinic drugs
Ganglionic blockers and Neuromuscular junction blockers
What is unique about antimuscarinic MOA?
Its an inverse agonist -> receptor w/constituative activity that is switched off w/the agonist
What are the systemic effects of antimuscarinic agents(atropine) - CNS, EYE, Cardiovascular, Respiratory
CNS = sedative, Eye = Mydriasis, cardiovascular = SA + AV node is blocked + blocked vasodilation, Respiratory = bronchodilation and reduced secretion
What is a side effect of antimuscarinic drugs in the skin
Sweat lands - suppresed thermoregulatory sweating - "atropine fever" = contrainidcated in infants + children
What is the function of pilocarpine on the eye? Atropine on the eye?
Pilocarpine = miosis, atropine = mydriasis
What is the MOA of atropine(antimuscarinic dugs)?
Binds competitively to receptor -> preventing Ach binding; duration =4 hrs
What is the antidose for cholinergic agonists - OD on choliensterase inhibitor insecticides, mushroom poisoning, blocks effects of excess Ach from acetylcholinesterase inhibitors?
atropine
What drug do u use to treat motion sickness?
Scopolamine patch
What are the action of scopolamine
Therepeutic lvl = sedation, high doses = excitation, anti-motion sickness, blocks short-term memory
What drug is a synthetic analog to atropine?
Ipratropium
What are you treating when using ipratropium?
Treating asthma + COPD (inpatients who are unable to take beta-2 receptor agonists)
Where in the body does scopolamine work?
CNS - treats motion sicknes
Where in the body does ipratropium work?
Respiratory -treats COPD
Where in the body does atropine work?
Cardiovascular - treats vasodilation
What drugs are used to treat an over active bladder
Solifenacin
What drugs are used to treat adults w/urinary incontinence
tolterodine
Which G-protein coupled receptor is stimulatory?
Gs
Which G-protien coupled receptor is inhibitory
Gi
Which G-protien is coupled w/adrenorecepotr to phospholipase C
Gq/11
Which receptor is present on the post synaptic membrane and is coupled w/Gq -> phosphoplipase C?
Alpha-1 arenorecepotor
Which receptor is present on pre-synaptic nerve endings, beta-cell of pancrease, on vascular smooth muscle -> coupled w/Gi -> inhibits adenylate cyclase
Alpha -2 adrenoreceptor
What are the drugs that bind to alpha-adrenoreceptors
Epinephrine, norepinephrine, isoproterenol
What happens when u activate the alpha-2-adrenoreceptor?
NE binds -> activates alpha-2-receptor -> turns off adenylyl cyclase -> ↓ [cAMP] -> ↓ NE release
If pt w/vasodilation, bronchodilation, and relaxed smooth muscle
Exposed to beta-2 agonist
What is the location of alpha-1-receptors?
Vascular beds -> dleads to areril and venoconstriction
What is the location of alpha-2-receptors
Vasculature -> leads to vasoconstriction
What is the location ob beta-1 recepotrs
Heart and vasculature -> ↑ cardiac output (due to ↑ contractility and stimulation of the SA node -> thus ↑ HR)
What si the location of the beta-2-receptors
Vascular beds -> ↓ peripheral resistance -> vasodilation
What effect does activation of beta-2-receptors in the respiratory system do?
Smooth muscle bonchodilation
What drug favors alpha-1 over alpha-2 receptor?
Phenylephrine -> causes mydirasis + nasal decongestant
What are the direct acting adrenergic agonists that are alpha-1-receptor selective?
1. Phenylephrine, 2. methoxamine, 3. midodrine
What drug causes mild stimulation of CNS -> improves athletic performance
ephedrine
What is the MOA of amphetamine
CNS = stimulant, periphery = blocks reuptake of NE + releases of stored catecholamines
MOA of cocaine
Blocks the norepinephrine transporter - > NE accumulates in the symaptic cleft
What is the side effect of MAOI in the presence of cheese metabolites
↑ blood pressure
What is the treatment for anaphylaxis
Epinephrine injection (IM)
What is the cytochrome system that metabolizes metoprolol
CYP2D6 - poor metabolizers = higher plasma concentration
What drugs do u use to treat pheochromocytoma?
Phenoxybenzamine (Alpha-receptor antagonist )- b/c in pheochromocytoma the tumor produces too much EPI/NE
What are the beta-receptor antagonist drugs we need to know?
Propranolol, nadolol, metorpolol
Which beta-blocker is a partial beta-agonist and is useful in hypertension, angina
Pindolol + acebutolol
Which beta-blocker is a reversible antagonist (also has alpha-1-receptor antagonist properties)
Labetalol
Which beta-block is a non-selective beta-receptor antagonist + has some capacity to block-alpha-receptors and has antioxidant properties
Carvedilol
What drug is an ultra-short acting - beta-1 antagonist?
esmolol
What drug is used to treat stage fright?
propranolol
What is the drug used to treat thyroid storm?
Propranolol -> treats hyperthyroidism ("thyroid storm")
What should never be done w/beta-antagonists?
Should never be abruptly stopped -> to avoid acute tachycardia, hypertension, and/or ischemia
What are the sympathetic symptoms?
Hot, blind, dry, red, mad, bloated