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FA.Pharm.AutonomicDrugs Flashcards

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1
Q

Nicotinic ACh receptors are….

Nn are found in _____.

Nm are found in _____.

A

Nicotinic ACh receptors are LIGAND-GATED Na+ / K+ channels;

Nn receptors are found in AUTONOMIC GANGLIA

Nm receptors are found in NEUROMUSCULAR JUNCTIONS

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2
Q

What is odd about the adrenal medulla and sweat glands?

A

Both are part of SANS, but are innvervated by cholinergic fibers.

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3
Q

Botulinum toxin _____ the release of _____ at all _______ terminals.

A

Botulinum toxin PREVENTS the release of NEUROTRANSMITTER at all CHOLINERGIC TERMINALS.

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4
Q

Muscarinic ACh receptors:

General mechanism

Subtypes

A

Muscarinic ACh receptors are G-protein–coupled receptors that act thru 2nd MESSENGERS

Subtypes: M1-M5

However, only M1, M2, and M3 are of concern

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5
Q

G-protein–linked 2nd messengers

Receptor:
G-protein class:
Major functions:

A

¶ QISS and QIQ till you’re SIQ of SQS

{ SANS } { PANS }{ Dopa } { Hista }{ ADH }
[A1] [A2] [ß1] [ß2] [M1] [M2] [M3] [D1] [D2] [H1] [H2] [V1] [V2]
[ q ] [ i ] [ s ] [ s ] [ q ] [ i ] [ q ] [ s ] [ i ] [ q ] [ s ] [ q ] [ s ]

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6
Q

Receptor: A1

G-protein class:

Major functions:

A

Receptor: A1

G-protein class: Gq

Major functions:
/\ Vascular smooth muscle contraction,
/\ pupilary dilator muscle contraction (mydriasis),
/\ intestinal and bladder sphincter muscle contraction

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7
Q

Receptor: A2

G-protein class:

Major functions:

A

A2

Gi

\/ sympathetic outflow
\/ insulin release

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8
Q

Receptor: ß1

G-protein class:

Major functions:

A

ß1

Gs

/\ Heart Rate
/\ Contractility
/\ Renin release
/\ Lipolysis

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9
Q

Receptor: ß2

G-protein class:

Major functions:

A

ß2

Gs

Vasodilation
Bronchodilation
/\ Heart rate
/\ Contractility
/\ Lipolysis
/\ INSULIN RELEASE
\/ uterine tone
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10
Q

Receptor: M1

G-protein class:

Major functions:

A

M1

Gq

CNS
Enteric nervous system

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11
Q

Receptor: M2

G-protein class:

Major functions:

A

M2

Gi

\/ Heart rate
\/ contractility of atria ( ø by atropine)

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12
Q

Receptor: M3

G-protein class:

Major functions:

A

M3

Gq

/\ Exocrine gland secretions (sweat, GASTRIC ACID)
/\ Gut peristalsis
/\ Bladder contraction
BronchoCONSTRICTION
/\ Pupillary sphincter muscle contraction (miosis)
Ciliary muscle contraction (accomodation)

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13
Q

Receptor: D1

G-protein class:

Major functions:

A

D1

Gs

Relaxes renal vascular smooth muscle

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14
Q

Receptor: D2

G-protein class:

Major functions:

A

D2

Gi

Modulates transmitter release, especially in the brain

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15
Q

Receptor: H1

G-protein class:

Major functions:

A

H1

Gq

/\ Nasal and bronchial mucus production
/\ Bronchiole contraction
Pruritis (itching)
Pain

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16
Q

Receptor: H2

G-protein class:

Major functions:

A

H2

Gs

/\ Gastric acid secretion

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17
Q

Receptor: V1

G-protein class:

Major functions:

A

V1

Gq

/\ Vascular smooth muscle contraction

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18
Q

Receptor: V2

G-protein class:

Major functions:

A

V2

Gs

/\ H2O permeability and reabsorption in the COLLECTING TUBULES of the kidney

¶ V …2… is found in the …2… kidneys

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19
Q

Gq coupled receptors and their MOA

A

H1, A1, V1, M1, M3

           Gq                                lipids Receptor—>Phospholipase C—>  |      DAG—> Protein Kinase C
                                                  V      /
                                                  PIP2  
                                                          \ 
                                                          IP3 —> /\ [Ca++] in cell

¶ hey cutesy! HAV 1 M&M
q C

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20
Q

Gs and Gi coupled receptors and their MOA

A

Receptor
ß1,ß2,D1 \ Gs
H2,V2 \ (+) ATP /\ [Ca++] in heart
Adenylyl Cyclase—> | /
/ (-) \/ / (+)
/ Gi cAMP—>p.k.A
Receptor \ (-)
M2,A2,D2 \
Myosin light-chain kinase
¶MAD 2’s (smooth muscle)

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21
Q

CHOLINERGIC Neuron

Drug that blocks reuptake of Choline

A

Hemicholinium

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22
Q

CHOLINERGIC Neuron

Drug that blocks ACh from entering vesicles

A

Vesamicol

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23
Q

CHOLINERGIC Neuron

What is needed for NT release from vesicles

A

Ca++

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24
Q

CHOLINERGIC Neuron

What blocks the release of ACh from vessicles?

A

Botulinum toxin

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25
CHOLINERGIC Neuron Postsynaptically, what breaks down ACh, and what does it break it down into?
ACh-esterase ACh —> Acetate + Choline
26
NORADRENERGIC Neuron Drug that blocks Tyrosine Hydroxylase. This drug prevents _____ from becoming ______.
Metyrosine blocks Tyrosine hydroxylase (-) Metyrosine ——| Tyrosine hydroxylase Phenylalanine——>Tyrosine———X———> DOPA /' \, THB DHB
27
NORADRENERGIC Neuron Drug that blocks entry of dopamine into vessicles
Reserpine
28
NORADRENERGIC Neuron Drug that blocks release of NE from vessicles
Guanethidine
29
NORADRENERGIC Neuron Drug that causes NE to be released from vessicles
Amphetamine
30
NORADRENERGIC Neuron 3 drugs that block reuptake of NE at nerve terminal
1. Cocaine 2. TCAs 3. Amphetamine
31
NORADRENERGIC Neuron Name 3 release modifying, presynaptic receptors, and whether they inhibit or stimulate neuron.
1. M2 --- inhibit 2. Angiotensin II --- stimulate 3. A2 --- inhibit All are presynaptic and found in cardiac muscle (SA node)
32
In general, cholinomimetic agents make you…
ooze from every orifice.
33
Drug: Bethanechol Class :: Subclass Clinical applications Action
BethaneCHOL Cholinomimetic, direct agonist Postoperative and neurogenic ileus Urinary retention Activates Bowel and Bladder smooth muscle Resistant to AChE ¶ BETHANY, CALL me if you want to activate your Bowels and Bladder
34
Drug: Carbachol Class :: Subclass Clinical applications Action
CarbACHOL Cholinomimetic, direct agonist Glaucoma Pupillary contraction Relieve of intraocular pressure ¶CARBon copy of acetylcholine
35
Drug: Pilocarpine Class :: Subclass Clinical applications Action
Pilocarpine Cholinomimetic, direct agonist Potent stimulator of SWEAT, TEARS, SALIVA Contracts ciliary muscle of eye (open angle) Contract pupillary sphincter (narrow angle) Resistant to AChE ¶You cry, drool, and sweat on your PILOw
36
Drug: Methacholine Class :: Subclass Clinical applications Action
Methacholine Cholinomimetic, direct agonist Challenge test for DX of ASTHMA Stimulates muscarinic receptors in airway when inhaled
37
Drug: Neostigmine Class :: Subclass Clinical applications Action
Neostigmine Cholinomimetic, INdirect agonist Postoperative and neurogenic ileus Urinary retention Myasthenia gravis Reversal of neuromuscular junction blockade (postoperative) /\ endogenous ACh; no CNS penetration ¶ NEO CNS! = NO CNS
38
Drug: Pyridostigmine Class :: Subclass Clinical applications Action
Pyridostigmine Cholinomimetic, INdirect agonist ``` Myasthenia gravis (b/c long acting) Does NOT penetrate CNS ``` /\ endogenous ACh /\ Strength ¶ Py…RID…ostigmine get …RID… of myasthenia gravis
39
Drug: Edrophonium Class :: Subclass Clinical applications Action
Edrophonium Cholinomimetic, INdirect agonist DIAGNOSIS (not Tx) of myasthenia gravis (extremely short acting) /\ endogenous ACh ¶ I called my friend EDRO on the PHONE to see if he has myasthenia gravis
40
Drug: Physostigmine Class :: Subclass Clinical applications Action
Physostigmine Cholinomimetic agent, INdirect agonist Glaucoma (b/c it crosses blood-brain barrier —> CNS) Atropine OD /\ endogenous ACh ¶ PHY…sostigmine PHY…xes atropine OD ¶ PH-YS…ostigmine is for your eyes (Fuh-yh-eyes-ostigmine): glaucoma. Did I see an ECHO? (echothiophate also for glaucoma)
41
Drug: Echothiophate Class :: Subclass Clinical applications Action
Echothiophate Cholinomimetic, INdirect agonist Glaucoma /\ endogenous ACh ¶ Fuh-yh-eyes-ostigmine. Did i see an ECHO? Echo is also for glaucoma
42
Drug: Donepezil Class :: Subclass Clinical applications Action
Donepizil Cholinomimetic, INdirect agonist Alzheimer's Dz (only transient, NOT a cure) /\ Endogenous ACh ¶ DONE with al…Z…heimers. donepe…Z…il
43
When given to susceptible px, all cholinomimetics carry risk of exacerbating…
COPD Asthma Peptic Ulcers
44
Drug: Parathion Class :: Subclass Clinical applications Action
Parathion Organophosphate, cholinesterase inhibitor POISON Commonly used as pesticide: case will probably involve FARMER Antidote — ATROPINE + PRALIDOXIME (regenerates active AChE, must use within a few hours before toxin "ages" [ leaves phosphate on receptor, R group is hydrolyzed — irreversable] Causes Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and cns, Lacrimation, Sweating, and Salivation (oozing from every oriface) ¶ DUMBBELSS
45
Drug: Atropine Class Organ system Clinical applications
Atropine Muscarinic antagonist ``` Eye————————— /\ Pupil dilation, cycloplegia Airway———————-- \/ Secretions Stomach——————— \/ Acid secretion Gut————————— \/ Motility Bladder———————- \/ Urgency in cystitis ``` Used to Tx BRADYcardia, and for ophthalmic applications Produces MYDRIASIS and CYCLOPLEGIA ¶Blocks DUMBBELSS
46
Atropine TOXICITY
``` /\ Body temp (due to \/ sweating) Rapid Pulse Dry Mouth Dry, flushed skin Cycloplegia Constipation Disorientation ¶think about Alz Dz with \/ ACh ``` Can cause acute ANGLE CLOSURE glaucoma in elderly, Urinary retention in men with BPH Hyperthermia in infants ¶ Hot as a hare…Dry as a bone…Red as a beet…blind as a bat… Mad as a hatter
47
Name a plant toxicity that mimics that of atropine
Jimson weed
48
Drug: Homatropine Class :: Subclass Clinical applications Action
Homatropine Muscarinic antagonists Produces MYDRIASIS and CYCLOPLEGIA (paralysis of ciliary muscle --> ø accommodation) EYE
49
Drug: Tropicamide Class :: Subclass Clinical applications Action
TROPicamide (like aTROPine) Muscarinic antagonist Produces mydriasis and cycloplegia Eye
50
Drug: Benztropine Class :: Subclass Clinical applications Action
benzTROPINE Muscarinic antagonist Parkinson's disease ¶ PARK my BENZ CNS
51
Drug: Scopolamine Class :: Subclass Clinical applications Action
Scopolamine Muscarinic antagonist Motion sickness ¶ Think about riding in a gyroSCOPE CNS
52
Drug: Ipratropium Class :: Subclass Clinical applications Action
Ipratropium Muscarinic antagonist Asthma, COPD ¶ I PRAy i can breathe again Respiratory
53
Drug: Oxybutynin Class :: Subclass Clinical applications Action
Oxybutynin (same use as Glycopyrrolate) Muscarinic antagonist Reduces urgency in mild cystitis and reduces bladder spasms Genitourinary ¶ GLYCO PYRO's can't pee because they have an OXY BUTT
54
Drug: Glycopyrrolate Class :: Subclass Clinical applications Action
Glycopyrrolate (same use as Oxybutynin) Muscarinic antagonist Reduce urgency in mild cystitis and reduce bladder spasms Genitourinary ¶GLYCO PYRO's can't pee because they have an OXY BUTT
55
Drug: Methscopolamine Class :: Subclass Clinical applications Action
Methscopolamine (along with Pirenzepine, and Propantheline) Muscarinic antagonist Peptic ulcer treatment Gastrointestinal [methscopolamine] [pirenzepine] ¶ use your METH SCOPE to PEER IN ZE gastric ulcer to see the PROPAN (proton) pump, and block the muscarinic receptor
56
Drug: Pirenzepine Class :: Subclass Clinical applications Action
PirenzePINE (similar to Methscopolamine, and propantheline) [atroPINE] Muscarinic antagonist Peptic ulcer treatment Gastrointestinal
57
Drug: Propantheline Class :: Subclass Clinical applications Action
Propantheline (along with Methscopolamine and Pirenzepine) Muscarinic antagonist Peptic ulcer disease Gastrointestinal
58
Drug: Epinephrine Class :: Subclass Clinical applications Action
Epinephrine Direct sympathomimetic Anaphylaxis Glaucoma (open angle) Asthma Hypotension [ a1 ][ a2 ][ ß1 ][ ß2 ][ D1 ] + + + + + + + + + + + + + +
59
Drug: Norepinephrine Class :: Subclass Clinical applications Action
Norepinephrine Direct sympathomimetic Hypotension (but \/ renal perfusion [esp. when given w/ NSAIDS] [ a1 ][ a2 ][ ß1 ][ ß2 ][ D1 ] + + + + + + + + + + +
60
Drug: Isoproterenol Class :: Subclass Clinical applications Action
ISOproterenol Direct sympathomimetic AV block (rare) Isolated ß agonist ß1, ß2
61
Drug: Dopamine Class :: Subclass Clinical applications Action
Dopamine Direct sympathomimetic Shock (renal perfusion) Heart failure: inotropic chronotropid D1 > ß > a D1 ---- low dose ß ------ medium dose a ------ high dose
62
Drug: Dobutamine Class :: Subclass Clinical applications Action
Dobutamine Direct sympathomimetic Heart failure Cardiac stress testing Inotropic AND chronotropic a1 a2 ß1 ß2 D + + + + + + +
63
Drug: Phenylephrine Class :: Subclass Clinical applications Action
Phenylephrine Direct sympathomimetic ``` Pupilary dilation (w/o cycloplegia) Vasoconstriction Nasal decongestion ``` a1 a2 ß1 ß2 D1 + + + + + +
64
Drug: Metaproterenol Class :: Subclass Clinical applications Action
Metaproterenol ¶ MAST \_______________________/ Direct sympathomimetic Acute asthma a1 a2 ß1 ß2 D1 + + + + + +
65
Drug: Albuterol Class :: Subclass Clinical applications Action
Albuterol ¶ MAST \__________________/ Direct sympathomimetic Acute asthma a1 a2 ß1 ß2 D1 + + + + + +
66
Drug: Salmeterol Class :: Subclass Clinical applications Action
Salmeterol ¶ MAST \____________________/ Direct sympathomimetic LONG TERM tx of ASTHMA a1 a2 ß1 ß2 D1 + + + + + +
67
Drug: Terbutaline Class :: Subclass Clinical applications Action
Terbutaline ¶ MAST \______________________/ Direct sympathomimetic \/ Premature uterine contraction a1 a2 ß1 ß2 D1 + + + + + +
68
Drug: Ritodrine Class :: Subclass Clinical applications Action
Ritodrine Direct sympathomimetics \/ Premature uterine contractions a1 a2 ß1 ß2 D1 + + + +
69
Drug: Amphetamine Class :: Subclass Clinical applications Action
Amphetamine INdirect sympathomimetic Narcolepsy Obesity Attention deficit disorder Indirect general agonist RELEASES stored catecholamine
70
Drug: Ephedrine Class :: Subclass Clinical applications Action
Ephedrine INdirect sympathomimetic Nasal decongestion Urinary incontinence Hypotension Indirect general agonist Releases stored catecholamines
71
Drug: Cocaine Class :: Subclass Clinical applications Action
Cocaine INdirect sympathomimetic Vasoconstriction Local anethesia TOX: Stroke, nasal septum perforation Indirect general agonist ø uptake
72
Drug: Clonidine Class :: Subclass Clinical applications Action
Clonidine Sympatheplegics Hyptertension (esp. w/ renal dz) NO \/ in blood flow to kidney Centrally acting a2-agonists \/ Central adrenergic outflow
73
Drug: a-methyldopa Class :: Subclass Clinical applications Action
a-methyldopa Sympathoplegic Hypertension (like Clonidine: esp. w/ kidney dz b/c no \/ in blood to kidney Centrally acting a2-agonists \/ Central adrenergic outflow
74
Drug: Phenoxybenzamine Class :: Subclass Clinical applications Action
Phenoxybenzamine (irreversible) Nonselective alpha blocker PHEOCHROMOCYTOMA (use this drug before removing tumor, since high levels of released catecholamine will never overcome block) TOX: Orthostatic hypotension Reflex TACHYcardia
75
Drug: Phentolamine Class :: Subclass Clinical applications Action
Phentolamine (reversible) Nonselective alpha-blocker Give to patients on MAO inhibitors who eat TYRAMINE-containing foods TOX: Orthostatic hypotension Reflex TACHYcardia
76
Drug: Prazosin, Terazosin, Doxazosin Class :: Subclass Clinical applications Action
-ZOSIN ending a1 selective blocker Hypertension Urinary retention in BPH TOX: 1st dose orthostatic hypotension Dizziness Headache
77
Drug: Mirtazapine Class :: Subclass Clinical applications Action
Mirtazapine a2 selective blocker Use for DEPRESSION Tox: Sedation /\ Serum cholesterol /\ appetite
78
Name drug that causes /\ blood pressure that can be reversed (cause \/ pressure) after Phentolamine administration
Epinephrine Alpha-blockade causes unmasking of the ß2 vasodilatory fx
79
Name drug that causes an /\ BP but whose effect can be cancelled after phentolamine administration.
Phenylephrine A selective alpha-agonist. Alpha blockade cancels its physiological effect.
80
ß-blockers end in…
-olol ex. Acebutolol
81
ß-blockers clinical applications… (6)
1. Hypertension \/ Cardiac output \/ RENIN secretion (due to ß block of JGA cells) 2. Angina pectoris \/ Heart rate / contractility '--> \/ O2 consumption 3. MI \/ mortalitly 4. SVT Class II anti-arrhythmic (Propranolol & Esmolol) \/ AV conduction vel. 5. CHF Slows progression of chronic failure 6. Glaucoma \/ secretions of aqueous humor (timolol eye drops)
82
ß blocker TOX (5)
1. Impotence 2. Exacerbation of asthma/COPD 3. Adverse CARDIAC fx › Bradycardia › AV block › CHF 4. Adverse CNS fx › Sedation › Sleep alterations 5. Use with caution in DIABETICS
83
ß1 selective antagonists… What px would benefit most from these as opposed to non selective ß blockers?
ß1 selective antagonists ¶Begin with letters A-M ``` Acebutolol (partial agonist) Betaxolol ) Esmolol ) > Short acting Atenolol Metoprolol ``` ¶ A BEAM of ß1 blockers Good for px with pulmonary dz!!!
84
Nonselective ß antagonists
Begin with letters N-Z ¶ Please Try Not ßeing Picky / / / / Propranolol--------------' / / / Timolol-----------------------------' / / Nadolol---------------------------------' / Pindolol--------------------------------------------'
85
Nonselective (vasodilatory) | a- and ß-antagonists
Carved…ILOL Labet…ALOL ¶ The weird one's that don't end in -OLOL
86
Partial ß-Agonists
Pindolol ------. Acebutolol-----\------------------. \ \ ¶ …P…artial ß …A…gonists ¶ PAPA

Pharmacology (6 decks)

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