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Fundies test 4-pillion lectures
12/3 antihistamines 12/4 adrenergic 12/5 cholinergic
129
Dentistry
Graduate
12/12/2013

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Term
What does acetylcholine do to the nicotinic acetylcholine receptor?
Definition
Acetylcholine opens up the sodium ion channel, sodium rushes into the nerve, depolarizes and neuron fires
Term
How does the steroid interact with the receptor and how does it bring about a hormone response?
Definition
steroid is usually bound by corticosteroid-binding globulin in blood but enters the cell as free molecule (uncharged), bind to intracellular receptor, enters nucleus, turns on transcription by binding to glucocorticoid response element on regulatory region, protein makes hormone response
Term
True or false: A single cell may only have 1 receptor and signaling system.
Definition
False-A single cell may have multiple receptors and signaling systems
Term
What is it called when continuous stimulation of a receptor often results in loss of response and down-regulation of receptors?
Definition
tachyphylaxis (ex: type II diabetes-insulin receptors become insensitive)
Term
Receptor sensitivity can be (increased or decreased) as a result of withdrawal of the agonist
Definition
Receptor sensitivity can be increased as a result of withdrawal of the agonist. (rebound effect)
Term
How do antihistamines work in terms of a binding to a receptor?
Definition
Antihistamines as an example of a class of drugs that bind to a receptor and inhibit normal ligand action
Term
What type of antagonists must be taken every few hours because they are only effective if they are present at an effective concentration?
Definition
Reversible competitive antagonists (H1 receptors)
Term
Are reversible competitive antagonists of (H1 or H2) receptors used as decongestants?

Is (H1 or H2) used to treat excess stomach acid?
Definition
Reversible competitive antagonists of H1 receptors are used as decongestants

Reversible competitive antagonists of H2 receptors are used to treat excess stomach acid
Term
Where does histamine come from?
Definition
Mast cells (contains mediators that cause inflammation: histamine, enzymes, prostaglandins, leukotrienes, platelet activating factor, cytokines) in the tissue and basophils in the blood
Term
What factors activate mast cells?
Definition
IgE-mediated (allergies) - vasodilation, recruits WBCs
Anaphylatoxins (C5a, C3a)
Direct release by certain drugs (opiates)
Physical stimuli (heat, cold, trauma)
Autoimmune (chronic urticaria)
Term
Does histamine have any clinical application in the treatment of disease?
Definition
Histamine has no clinical application in the treatment of disease
Term
What are the 3 different histamine receptors?
Definition
H1
H2
H3
Term
What are the 3 ways you can reduce histamine effects?
Definition
Epinephrine
Mast cell stabilizers
Antihistamines
Term
What is the physiological antagonist that causes smooth muscle actions (vasoconstriction) opposite of histamine, and is used for anaphylaxis and severe urticaria?
Definition
Epinephrine
Term
What is used in asthma that cause mast cells to not release as much histamine but the mechanism is unknown
Definition
mast cell stabilizers
Term
What is the reversible competitive antagonists of H1 receptors in nasal mucosal tissues?
Definition
antihistamines
Term
What is the difference between 1st and 2nd generation antihistamines?

Why does one cause drowsiness while the other doesn't? How do stop the drowsiness?
Definition
1st generation-Penetrates CNS (side effect=causes drowsiness), older, cheaper, generic

2nd- better, more expensive, 1/2 life or ability to enter CNS is changed

Make the drug charged so it won't go across the blood brain barrier and cause drowsiness
Term
Is (H1 or H2) Gq-protein-mediated activation of phospholipase C to make IP3 and diacyglycerol?

Is (H1 or H2) Gs-protein-mediated activation of adenylyl cyclase to make cAMP?
Definition
H1

H2
Term
Is (H1 or H2) found in the stomach, heart, some smooth muscles (uterus), CNS?

Is (H1 or H2) found in smooth muscles (especially in intestine, blood vessels, bladder, trachea), heart, adrenal medulla, vascular endothelium, CNS
Definition
H2

H1
Term
How many transmembrane domains are there in histamine receptors (both H1 and H2)?
Definition
7
Term
Do (H1 or H2) receptor antagonists Commonly cause sedation, blurred vision, nervousness, dryness of mouth/respiratory passages, urinary retention
Paradoxical effect in some children
Prevent motion sickness
Prevent nausea and vomiting
Suppress effects of tremors associated with antipsychotics
Definition
H1 Receptor Antagonists
Term
Are (1st or 2nd) generation antihistamines Rapidly absorbed, Long duration of action (12-24 hrs), Poor distribution to the CNS, Little to no sedation, Older agents metabolized by CYP450 enzyme system, Combined with pseudoephedrine (vasoconstriction) in some products
Definition
2nd generation
Term
Identify whether these drugs are 1st or 2nd generation drugs of H1 receptors

Chlorpheniramine
Cyclazine
Cetirizine
Cyproheptadine
Dimenhydrinate
Diphenhydramine
Fexofenadine
Hydroxyzine
Loratadine
Promethazine
Definition
Chlorpheniramine-1
Cyclazine-1
Cetirizine-2
Cyproheptadine-1
Dimenhydrinate-1
Diphenhydramine-1
Fexofenadine-2
Hydroxyzine-1
Loratadine-2
Promethazine-1

(cetirizine, loratadine, and fexofenadine-2nd generation! can't enter CNS)
Term
How would you treat allergic conjunctivitis?
Definition
Treatment with a **mast-cell stabilizer and antihistamine
(may attempt to avoid allergens)
Term
Olopatadine (Patanol) drops, Alcaftadine, azelastin, bepotastin, epinastine, are what types of histamine reducers?
Definition
combines both anti-histamine and mast cell stabilizer effects (anti-histamine effects occur rapidly, mast cell stabilizer effects take longer) to treat allergic conjunctivitis
Term
Cimetidine, Ranitine, Famotidine and Nizatidine are (H1 or H2) Receptor Antagonist and what do they treat?
Definition
Histamine H2 Receptor Antagonists

Orally effective, competitive inhibitors of H2 receptors on gastric parietal cells, treats acid reflux, decreases amount of acid secreted into the stomach
Term
Which of the following drugs is least likely to cause sedation?

Diphenhydramine
Hydroxyzine
Cetirizine
Promethazine
Definition
Cetirizine - 2nd generation
Term
Which of the following mediators causes the immediate symptoms observed after IgE is cross-linked by allergens?

Histamine
Prostaglandins
Leukotrienes
Interleukins
Definition
Histamine - causes immediate effect- prompts vasodilation, swelling
Term
Which of the following is not a systemic effect of histamine?

Gastric acid secretion
Constriction of small blood vessels
Bronchoconstriction of bronchiolar smooth muscle
Formation of edema
Definition
Constriction of small blood vessels
Term
What receptors do acetylcholine bind to?

Which one is couple to ion channels on the neurons, very quick?

Which one is coupled to G proteins that increase the formation of diacylglycerol and inositol triphosphate (IP3) by activating phospholipase C (muscles, slower, increases release of calcium)?
Definition
Nicotinic Receptor-coupled to ion channels

Muscarinic Receptors-coupled to G proteins that increase the formation of diacylglycerol and inositol triphosphate (IP3) by activating phospholipase C
Term
What receptors does norepinephrine bind to?
Definition
B1, A1, A2
Term
Which adrenergic receptor is coupled to Gs proteins that increase cAMP and is found primarily in the heart?
Definition
B1
Term
Which adrenergic receptor is coupled to Gs proteins that increase cAMP levels found in the lungs?
Definition
B2 (B2 agonist given to treat asthma)
Term
Which adrenergic receptor is coupled to G proteins that increase the formation of diacylglycerol and inositol triphosphate (IP3) by activating phospholipase C
Definition
A1
Term
Which adrenergic receptor is coupled to G proteins but is located on the neuron itself (other ones located on target cell) and decreases cAMP level by feedback inhibition?
Definition
A2 (slows down heart rate)
Term
Does acetylcholine have an enzyme that degrades it at the synaptic cleft? Why?

Does norepinephrine?
Definition
Yes-acetylcholinesterase has to clear acetylcholine out to depolarize quickly. Acetylcholinesterase inhibitors causes acetylcholine action duration to increase

No
Term
**What does norepinephrine bind to versus what does epinephrine bind to?
Definition
Epinephrine binds to all adrenergic receptors (A1, A2, B1, B2)

Norepinephrine does NOT bind to B2 (found in lungs and cause to dilate-why we don't give NE for asthmatic attack) but binds to A1, A2, B1
Term
Drugs that mimic the actions of the sympathoadrenal system are called?

Drugs that block or reduce these actions are called?
Definition
Sympathomimetics, Adrenomimetics, Sympathetic Agonists

Sympatholytics, Sympathoplegic, Sympathetic Antagonists
Term
What is biosynthesis of neurotransmitters pathway?

What is in the storage vesicles?

How are the contents released?
Definition
Tyrosine -> DOPA -> Dopamine -> NE -> EPI

norepinephrine, ATP, and dopamine beta-hydroxylase (converts dopamine to norepinephrine)

Ca2+ dependent (nerve depolarizes, sodium rushes in, calcium rushes in, vesicles release contents into cleft)
Term
What breaks down norepinephrine?

How is norepinephrine taken up?
Definition
monoamine oxidase and COMT (found in liver)

monoamine transporters (NET), cocaine-sensitive, binds to A2
Term
What does NOT happen when you see a bear enter the room?

you immediately open your eyes wide to find an escape route (mydriasis)
increase your heart rate
redistribute blood flow from your intestines to your skeletal muscles
open your pulmonary bronchioles
decrease your blood glucose
Definition
decrease your blood glucose
Term
*What type of agonist would you use during an eye exam to cause mydriasis?

What type of agonist would you use if you want to increase aqueous humor?
Definition
alpha agonist (mydriatic agent), NE, phenylephrine

beta agonist (use beta-blocker to decrease fluid/treat glaucoma)
Term
Adrenergic innervation of the eye innervates?

What receptors predominate?
Definition
Innervates iris dilator muscle, Mueller’s muscle (upper eyelid), conjunctival vasculature

A1 receptors predominate
Term
Cholinergic innervation of the eye innervates?

What receptors predominate
Definition
Innervates iris sphincter muscle, ciliary body

Muscarinic receptors predominate
Term
What agonist activity constricts pupil (miosis), contracts ciliary muscle, and lowers intraocular pressure
Definition
muscarinic agonist activity (muscarinic antagonist cause midriasis)
Term
In the cardiovascular, what causes vasoconstriction (increase resistance and pressure)?

What causes vasodilation?

What causes increased heart rate, increased force of contraction?
Definition
alpha 1

beta 2

beta 1
Term
True or False: During a bear attack, alpha 1 is stimulated and beta 2 is not
Definition
False

alpha 1 (vasoconstriction) decreases blood flow to the intestine
beta 2 (vasodilation) increases blood to the skeletal muscle at the same time
Term
At low dose of epinephrine, the affinity for which receptors dominate? At high doses of epinephrine what receptors dominate?
Definition
Low doses of Epinephrine - beta1 (cardiac) and beta2 (vasodilation) High doses of Epinephrine - alpha1 (vasoconstriction)
Term
**Which G-protein Couple Receptor activates adenylyl cyclase?

Inhibits adenylyl cyclase?

Activates phospholipase C?
Definition
Gs activates adenylyl cyclase
B1, B2, D1
Gi inhibits adenylyl cyclase
M2, A2, D2
Gq activates phospholipase C
M1, M3, A1
Term
Alpha and beta receptors are sympathetic or parasympathetic?

Muscarinic receptors are sympathetic or parasympathetic?
Definition
sympathetic

Parasympathetic
Term
*What adrenergenic agonist causes vasoconstriction in most vessels except skeletal muscles, increase BP, nasal decongestion, mydriasis: contract radial muscle of iris, receptors located at the post-junctional membrane
Definition
Alpha 1
Term
What adrenergenic agonist causes feedback inhibition of NE release, receptors located at the pre-junctional membrane, decreases BP
Definition
Alpha 2
Term
What is the alpha 2 agonist drug that decreases BP?
Definition
Clonidine
Term
What adrenergic agonist causes cardiac effects: increase heart rate, conduction velocity & force of contraction receptors located at post-junctional membrane
Definition
Beta 1
Term
What adrenergic agonist causes pulmonary effect: dilate bronchioles receptors located on post-junctional membranes
Definition
Beta 2
Term
What are the 3 adrenergic transmitters?

What are the three amine collectively called?
Definition
norepinephrine (NE)
dopamine (DA)
epinephrine (EPI)

catecholamines - bind to several distinct adrenergic receptors in different cell types
Term
What does monoamine oxidase work on?
What does it NOT work on?
Definition
sympathomimetic Amines

Amphetamine (lasts longer in synaptic cleft than NE)
Isoproterenol
Term
How does amphetamine effect the mechanism of reuptake of NE back into the noradrenergic neuron?

Cocaine?

Are these direct or indirect blockers?
Definition
Amphetamine can get into the neuron and vesicles and decrease amount of NE released and can bind to receptors and cause release of NE

Cocaine blocks norepinephrine transporter and inhibits reuptake (massive effect at first, and then diminished effect later)

Indirect blockers
Term
What does dopamine bind to?
Isoproterenol?
Dobutamine?
Phenylephrine?
Clonidine?
Terbutaline & Albuterol?
Definition
Dopamine (A1, A2, B1, D1, D2)
Isoproterenol (B1, B2)
Dobutamine (B1)
Phenylephrine (A1)
Clonidine (A2)
Terbutaline & Albuterol (B2)
Term
Is Amphetamine and Tyramine direct or indirect acting?

Is Ephedrine?
Definition
Amphetamine & Tyramine (indirect)
Ephedrine (mixed agonist and indirect)
Term
What are the advantages of synthetic compounds as therapeutic agents?
Definition
1. Increased selectivity for particular adrenergic receptors
2. Improved oral bioavailability
3. Prolonged duration of action
Term
What agonist would you use to treat nasal congestion, treat hypotension, cause mydriasis (dilation of the pupil for eye exam.), or mix with injected local anesthetic drugs to cause vasoconstriction at the site of injection and slow the rate at which the local anesthetic is removed to not get to the heart?
Definition
Alpha 1
Term
What agonist would you use to treat hypertension (not used much because of rebound effect), is highly lipid soluble, crosses blood-brain barrier, activates receptors in hypothalamus and medulla to decrease NE release, decrease sympathetic action in the heart, but may cause xerostomia, drowsiness, constipation?
Definition
Alpha 2 adrenoceptor agonist
Term
What agonist is used for short term treatment of cardiac decompensation (heart failure), Not recommended for chronic use because of receptor desensitization and down-regulation, and cause undesirable side effects (tachycardia, hypertension and arrhythmias) - used in hospital setting
Definition
Beta 1 agonists
Term
What agonist treats asthma by aerosol spray to lungs to minimize systemic side-effects (tachycardia, hypertension, arrhythmias) and often combined with glucocorticoid therapy
Definition
B2 agonists (too much B2 causes tachycardia because it gets to the heart and interacts with B1 receptors)
Term
What B2 agonists are Fast-acting agents for immediate effect (rescue inhaler) ?

Which is long-acting agents for once/twice daily prophylactic effects ?
Definition
salmeterol

albuterol, terbutaline
Term
Is terbutaline (B1 or B2) selective? Is dobutamine (B1 or B2) selective?
Definition

B2 (bronchodilator)

B1

Term
What is an A2 selective agonist that acts centrally to reduce sympathetic outflow to the periphery. Used for mild to moderate hypertension. Xerostomia, sedation, and constipation are major side effects
Definition
clonidine
Term
What is B1 selective, used for short term therapy of cardia decompensation; chronic use and/or high doses result in tachycardia and arrhythmias
Definition
dobutamine
Term
What is B2 selective, administered as aerosols, first-line therapy for asthma, bronchospasm, and emphysema. Nervousness, headache, tachycardia, palpitations, and skeletal muscle tremors are side effects
Definition
albuterol and terbutaline
Term
What has high A1 selectivity?
Definition
Phenylephrine (mydriasis eye drops) and metaraminol
Term
What does phentolamine block and what would that cause?

What does prazosin block and what would that cause?
Definition
phentolamine- blocks A1 (big cardiac effect) and A2 (lots of NE release)=tachycardia

prazosin- blocks A1 (not A2), so feedback inhibition for A2 is still in place but still big effect on beta 1 receptors = increase heart rate
Term
What does propanolol, Timolol block?

What does it do?
Definition
blocks B1 and B2

decrease aqueous humor production by the ciliary body
(good for stage fright)
Term
What does Atenolol, metoprolol (taken orally) block?

What does it do?
Definition
Blocks B1

brings heart rate down
Term
What does Reserpine block?

Is it a direct blocker or indirect?
Definition
Reserpine blocks Norepi storage & release from neurons

Indirect
Term
What antagonist is good for reducing hypertension (blocks NE) and helping with benign prostatic hyperplasia and urinary obstruction as a side effect?
Definition
A1 antagonist
Term
What 3 antagonist drugs have been shown to reverse prostate smooth muscle contraction (alpha1A) and improve urinary flow?

Which one is less potent, but more selective for alpha1 and has a longer duration of action?

Which one has greatest selectivity for alpha1A
Definition
Prazosin

Terazosin is less potent, but more selective for alpha1 and has a longer duration of action

Tamsulosin has greater selectivity for alpha1A than prazosin and terazosin
Term
What drug is a a good antidote for clonidine toxicity?
Definition
Yohimbine blocks clonidine and norepinephrine binding to the alpha2 receptor
Term
Liver metabolism (First-pass metabolism) is most important for (lipophilic or non-lipophilic drugs)?

Renal excretion is most important for (lipophilic or non-lipophilic drugs)?
Definition
Liver metabolism (First-pass metabolism) : (most important for lipophilic drugs)
*Have to be careful about drug-drug interactions that are metabolized by CYP450

Renal excretion : (most important for non-lipophilic drugs) bad if reduced renal function
Term
Plasma half-life of most beta blockers is? (hours)

What are the once a day beta blockers?

*What is the one beta blocker that has rapid onset and short duration (half-life=9 minutes)?
Definition
3-6 hrs

Bentaxolol (eye drop for glaucoma) and Nadolol

Esmolol
Term
Why is the list of beta blockers so long with so many different ones??
Definition
Because of the way they are metabolized
Term
List the clinical uses of Beta-blockers
Definition
Antihypertensive
Antiarrhythmic (slows heart rate)
antianginal
hyperthyroidism
open-angle glaucoma
anxiety
migraine
Term
How do beta blockers help with hypertension?
Definition
short term : no change in BP
long term : decrease renin release from kidneys -> decrease angiotensin -> decrease angiotensin 2 ->sodium reabsorption
Term
How do beta blockers help with angina?
Definition
Decreases heart rate (like arrhythmia and hyperthyroid) to alleviate pain but doesn't help the occlusion of the vessels that causes pain, just the symptoms
Term
How do beta blockers help with hyperthyroid?
Definition
decreases heart rate, but doesn't cure it
Term
What beta blocker helps with open-angle glaucoma and how does it help?
Definition
Timolol

- decreases aqueous humor production
- decreases ocular pressure
Term
What is NOT a major adverse side effect of Beta-blockers

Bradycardia, heart block, congestive heart failure
Bronchospasms
Tiredness
Diarrhea
Heartburn
hyperglycemia
hallucinations
Definition
hyperglycemia

- potentiates hypoglycemia, especially in patients with insulin-dependent diabetes
Term
What is only condition that you WOULD give a beta-blocker to?

sinus bradycardia
heart block
cardiogenic shock
overt cardiac failure
diabetes
hypertensive
asthma
emphysema
Definition
hypertensive

Any heart condition-don't give
diabetes, asthma, emphysema-might block B2 (bad)
Term
What drug blocks A1 (decreases vasoconstriction=lowers blood pressure), B1 (slows heart rate), and B2(bronchoconstriction)
Definition
labetalol
Term
What drug blocks A1, B1, and B2 and has antioxidant activity (decreases O2 radicals)
Definition
Carvedilol
Term
Metoprolol, Atenolol, and Esmolol are ___ generation beta blockers. What do they block?

Propranolol, Timolol, and Nadolol are ___ generation beta blockers. What do they block?
Definition
2nd (B1 selective)

1st (B1 and B2)

(as generations go on, the more selective the drugs become)
Term
Does adrenergic (agonist or antagonist) and cholinergic (agonist or antagonist) cause mydriasis?

Does adrenergic (agonist or antagonist) and cholinergic (agonist or antagonist) cause miosis?
Definition
adrenergic agonist and cholinergic antagonist

adrenergic antagonist and cholinergic agonist
Term
What drug is a competitive inhibition of A1 receptors in iris dilator muscle, Used clinically to reverse iatrogenically dilated pupils, Reverses phenylephrine-induced dilation in ~ 30-45 min, Reverses tropicamide (cholinergic receptor)-induced dilation in ~ 2-3 hr
Definition
Dapiprazole HCl (causes red eyes)
Term
If you were given acetylcholine, what would be the effects?

If you were to block acetylcholine action, what would the effect be?
Definition
miosis, low heart rate, increase secretions

heart rate goes up, midriasis
Term
What toxin prevents proteins found in vesicle membrane and cell membrane from hooking up so inhibits ACh release from vesicles --> paralyzes muscles
Definition
botulinum toxin
Term
What happens after choline gets taken up?
Definition
binds with acetyl-Coa to form acetylcholine and gets taken up into vesicle.

Cell depolarizes -> vesicles goes into synaptic cleft

It can bind to muscarinic or nicotinic receptors (you can block=paralyze muscles), or broken down by acetylcholinesterases to be taken back up, or bind to acetylcholine auto receptor to turn off release
Term
How can you treat myasthenia gravis?
Definition
blocke acetylcholinesterase so acetylcholine will be around longer because they have fewer acetylcholine receptors (indirect agonists)
Term
What are drugs that look like acetylcholine that bind to the receptor?

What are drugs that look like acetylcholine that bind to the receptor and block acetylcholine binding?

What are drugs that are acetylcholinesterase inhibitors?
Definition
cholinergic agonists

antagonist

indirect agonists
Term
Which muscarinic receptor is found in the CNS neurons, sympathetic postganglionic neurons and forms IP3 and DAG that increases intracellular calcium?
Definition
M1
Term
Which muscarinic receptor is found in the myocardium, smooth muscle, CNS and opens potassium channels and inhibits adenylyl cyclase (slows down heart)
Definition
M2
Term
Which muscarinic receptor is found on exocrine glands, vessels, CNS and forms IP3 and DAG that increases intracellular calcium?
Definition
M3
Term
Which muscarinic receptor is found in the CNS neurons, possibly vagal nerve endings that opens potassium channels and inhibits adenylyl cyclase?
Definition
M4
Term
Which muscarinic receptor is found in vascular endothelium, especiall cerebral vessels and CNS neurons and forms IP3 and DAG that increases intracellular calcium?
Definition
M5
Term
Where are nicotinic receptors found and what is the result of ligand binding?
Definition
Found in postganglionic neurons and skeletal muscles

2 molecules of ACH bind to open Na+/K+ channels and cause depolarization (sends signal to target cell=excitatory)
Term
which muscarinic receptors are excitatory, increase phospholipase C?
Definition
M1
M3
M5
Term
Which muscarinic receptors are inhibitory, inhibits adenylyl cyclase activity?
Definition
M2
M4
Term
2 ways drugs activate Cholinergic responses:

(Direct or indirect) resemble acetylcholine in structure but it is a false substrate for acetylcholinesterase (inhibits) and causes ACh levels to increase above normal?

(Direct or indirect) resembles ACh in structure, binds to ACh receptors to activate ACh signalling pathways
Definition
Indirect cholinomimetic drugs (binds BOTH muscarinic and nicotinic receptors)

Direct cholinomimetic drugs
Term
What are the acetyl choline derivatives (cholinergic agonists)?

What is good about the derivatives?
Definition
Methacholine (Muscarinic)
Bethanecol (Muscarinic)
Carbachol (Muscarinic and Nicotinic)

They have longer half-lifes than acetyl choline
Term
What are the muscarinic plant alkaloids

What are the nicotinic plant alkaloids
Definition
Muscarinic: Muscarine, Pilocarpine

Nicotinic: Nicotine, Lobeline
Term
What happens when the vagus nerves releases ACh onto organs like GI tract and heart?
Definition
it binds to M2 receptors (linked to Gi protein) so it decreases cAMP and decreases protein kinase A (opposite effect of NE binding to B1)

opens up K+ channel, K+ leaks out and causes hyperpolarization so more difficult to fire
Term
What does ACh do at a nicotinic receptor?
Definition
opens up Na channel and allow Na to enter --> depolarization gets an action potential

(muscarinic receptor decreases firing (K+ flow outs), Nicotinic receptor increases firing)
Term
What enzyme normally reduces ACh in synaptic cleft, responsible for termination of ACh action, allows nerve terminal to recover after depolarization, is necessary for normal nerve function, and is localized on post-synaptic membrane
Definition
Acetylcholinesterase
Term
Acetylcholinesterase is transiently acetylated as _____ is hydrolyzed.
Definition
Enzyme is transiently acetylated as ACh is hydrolyzed
Term
*List the Acetylcholinesterase inhibitors (indirect cholinergic mimetics)
Definition
Neostigmine (charged)
Physostigmine (uncharged)
Edrophonium (used to diagnose Myasthenia Gravis)
Insecticides (irreversible)
Neurotoxins
Term
If given Neostigmine, what effects does it have on your eye, intraocular pressure, heart rate?
Definition
Miosis, lower IOP, lower heart rate (Neostigmine=acetylcholinesterase inhibitor, elevates acetyl choline)
Term
What kind of chemical would inhibit Acetylcholinesterase?
Definition
One that looks like acetyl choline (binds to acetylcholinesterase and doesn't let go as quickly)
Term
What effect would an Acetylcholinesterase inhibitor have on different organs?
Definition
if we gave someone ACh we would get same effects
Term
Would an Acetylcholinesterase inhibitor gain access to the Central Nervous System?
Definition
Depends if charged (doesn't get in in CNS) or uncharged (gets in CNS)
Term
What is the best type of drug we have to slow down Alzheimer's Disease?
Definition
Oral Acetyl cholinesterase inhibitors
Term
*A farmer accidentally gets an organophospahte insectide on his clothing. It penetrates his skin. He collapses and is brought to the emergency room. What happened and how do you treat it?
Definition
Insecticide poisoning (irreversible inhibition)- excessive sweating, lungs fill up with fluid, heart stops beating, diaphragm stops contracting

Treat with pralidoxime (PAM) within 24 hrs - prevents irreversible inhibition of acetylcholinesterase (aging)

Atropine to relieve symptoms of excess ACh (acetylcholine antagonist)
Term
What is the drug that inhibits choline reuptake (looks like 2 acetylcholine molecules put together) to deplete acetylcholine?
Definition
Hemicholinium
Term
What is the drug that inhibit ACh uptake into vesicles to deplete acetylcholine released?
Definition
Vesamicol
Term
What anticholinergic drug blocks ACh binding to Muscarinic drugs (ex:bella donna plant)?
Definition
Atropine
Term
Atropine analogs with (shorter or longer) half-lives have been developed.

(short or long) duration of effect makes it less attractive for routine use.
Definition
shorter

long
Term
What are the atropine analogs? Are they cholinergic activators or inhibitors?
Definition
Tropicamide: Mydriasis & Cycloplegia
Ipratropium: Bronchodilator
Benztropine: Parkinson’s disease therapy
Scopolamine: Motion sickness relief

Cholinergic inhibitors
Term
Which atropine analog causes mydriasis and cycloplegia (paralysis of the lens)

Tropicamide:
Ipratropium:
Benztropine:
Scopolamine
Definition
Tropicamide
Term
Which atropine analog is bronchodilator?

Tropicamide:
Ipratropium:
Benztropine:
Scopolamine
Definition
Ipratropium
Term
Which atropine analong is given orally for Parkinson's disease therapy?

Tropicamide:
Ipratropium:
Benztropine:
Scopolamine
Definition
Benztropine
Term
Which atropine analog is used for motion sickness relief (goes to stomach, not the CNS)?

Tropicamide:
Ipratropium:
Benztropine:
Scopolamine
Definition
Scopolamine
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