Autonomic Pharmacology Flashcards

(61 cards)

1
Q

⍺1 Receptors

A

Gq, Stimulatory
Increase IP3, DAG, Ca2+

Vasoconstriction

Mydriasis (pupil dilation)

Contraction, urinary retention

Glycogenolysis (increase blood glucose

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2
Q

⍺2 Receptors

A

Gi, inhibitory
Decrease in cAMP and adenylyl cyclase, causing inhibition of NE release

Decreased insulin secretion

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3
Q

β1 Receptors

A

Gs, increased adenylyl cyclase and cAMP

HEART– increased HR, contractility, AV node conduction

Increased lipolysis

Increased renin release from kidney juxtaglomerular cells, causing increased BP

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4
Q

β2 Receptors

A

Gs, increased adenylyl cyclase and cAMP

Bronchodilation

Vasodilation of vascular smooth muscle and arteries of skeletal muscle

Decreased GI motility, Inhibition of labor

Glycogenolysis, gluconeogensis (increase blood glucose)

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5
Q

β3 Receptor

A

Gs, increased adenylyl cyclase and cAMP

Increased lipolysis

Inhibition of urination

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6
Q

Phenylephrine

A

⍺1 agonist

decrease nasal congestion by vasoconstriction

raises blood pressure for hypotension during surgery

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7
Q

Modafinil

A

⍺1 agonist

treats narcolepsy

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8
Q

Clonidine and Dexmedetomidine

A

⍺2 agonists

stimulation of alpha2 leads to decreased SNS activity

treats hypertension
- transient increase in BP followed by sustained hypotension
- produce sedation and analgesia

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9
Q

Brimonidine

A

Alpha2 agonist

Treats glaucoma

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10
Q

Dobutamine

A

Beta1 agonist

Stimulation of beta1 in the heart– increased cardiac rate and cardiac output

Treats cardiac decompensation after cardiac surgery of CHF

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11
Q

Short Acting Beta Agonists (SABAs)

A

Beta2 agonists

Albuterol, Isoproterenol
- relive acute asthma by bronchodilation

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12
Q

Long Acting Beta Agonists (LABAs)

A

Beta2 agonists

Salmeterol, Formoterol, Indacaterol
- prolonged bronchodilation, prevents asthma attacks

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13
Q

Mirabegron

A

Beta3 agonist

Relieves overactive bladder (decreases urination)

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14
Q

Cocaine, Amphetamine, Tyramine

A

Inhibit reuptake of norepinephrine and dopamine

Stimulate alpha1 and beta1 receptors – increase SNS activity

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15
Q

Mixed Action Agonists

A

Direct binding and release of stored NE

long mechanism of action because they are poor substrates for COMT and MAO

Ephedrine, metaraminol

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16
Q

Ephedrine

A

Alpha1 and beta2 agonist

Vasoconstriction and bronchodilation

Decreased urination (because adrenergic agonists are fight or flight)

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17
Q

Metaraminol

A

Alpha1 direct, Indirect

Elevates blood pressure

Treats hypotension produced by drugs or pheochromocytoma

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18
Q

Dopamine

A

Nonselective Direct Acting Adrenergic Agonist (can act on both alpha and beta receptors)

dilation of renal and mesenteric veins

increased salt excretion

increased water excretion

treats CARDIOGENIC SHOCK

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19
Q

Alpha 1 Blockade (general effect)

A

Smooth muscle relaxation

Causes REFLEX TACHYCARDIA

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20
Q

Alpha 2 Blockade (general effect)

A

Norepinephrine release

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21
Q

T/F: Alpha Blockers affect the sympathetic stimulation of the heart

A

FALSE

Alpha blockers do NOT affect the sympathetic stimulation of the heart

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22
Q

Phentolamine

A

Nonselective Alpha Blocker

Reverses anesthesia in dentistry

treats erectile dysfunction

diagnose pheochromocytoma

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23
Q

Phenoxybenzamine

A

Nonselective Alpha Blocker

Treats pheochromocytoma

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24
Q

Alpha1 Blockers

A

End in “-osin”

Treat peripheral vascular disease (Raynaud’s, Buerger’s)

Prazosin, doxazosin, terazosin (tx hypertension)

Tamsulosin, alfuzosin, silodosin (tx benign prostatic hypertrophy and the painful urination/urinary retention)

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25
Prazosin, Doxazosin, Terazosin
Alpha1 blockers (end in "-osin") treat hypertension
26
Tamsulosin, Alfuzosin, Silodosin
alpha1 blockers (end in "-osin") treat benign-prostatic hypertrophy and the painful urination/urinary retention associated
27
Beta Blockers (generalities)
Competitive inhibitors of beta-adrenergic receptors End in "-lol" Block the effect of catecholamines--> decrease sympathetic effects (mainly on heart)
28
Beta1 Block (generalities)
decreased heart rate delayed conduction through AV node Reduced contractility
29
Beta2 Block (generalities)
Bronchoconstriction DO NOT USE ON ASTHMA AND COPD PATIENTS!!
30
ALL beta blockers are contraindicated for _______
Insulin dependent DIABETICS Hypoglycemia usually causes tachycardia and lets the patient know they should eat something. Beta blockers will block the tachycardia, so the issue may go undetected.
31
Nonselective Beta Blockers (β1, β2)
propanolol, timolol, nadolol
32
Propranolol
Nonselective beta blocker migraine prophylaxis (has high lipid solubility, so it can penetrate the CNS)
33
Timolol
nonselective beta blocker decreases intraocular pressure, treats glaucoma
34
Beta1 Blockers
CARDIOSELECTIVE metoprolol, atenolol, nebivolol DO NOT USE ON PATIENT WITH AV HEART BLOCK
35
You can only block β___ in asthmatic patients
You can only block BETA1 in asthmatic patients Beta1 is cardioselective and will not affect the lungs. If we blocked beta2, there would be increased bronchodilation, which would cause even more breathing trouble in an asthmatic/COPD patient
36
Metoprolol
Beta1 blocker (cardioselective) Tx hypertension, angina may lower risk of death after a heart attack
37
Atenolol
Beta1 blocker (cardioselective) tx hypertension associated with ventricular ectopics in hyperthyroidism
38
Nebivolol
Beta1 blocker (cardioselective) releases NO causing vasodilation
39
Carvedilol and Labetalol
Block β1, β2, ⍺1 Block increases of HR and BP Decreases BP WITHOUT REFLEX TACHYCARDIA Able to reduce both systolic and diastolic BP. You decrease both peripheral resistance and cardiac output.. it acts on both the vessels and the heart itself, so it decreases both systolic and diastolic.
40
Muscarinic Agonists (Parasympathomimetics)
increase PARASYMPATHETIC and sympathetic to SWEAT GLANDS NO EFFECT ON BLOOD VESSELS THERE ARE NO MUSCARINIC RECEPTORS ON SKELETAL MUSCLES NEVER GIVE SYNTHETIC CHOLINE ESTERS VIA IV
41
Muscarinic Antagonists (Parasympatholytics)
increase SYMPATHETIC, decrease sweat glands
42
Acetylcholine
Muscarinic agonist used to test for miosis (pupil constriction) after cataract surgery
43
Metacholine
Muscarinic agonist used to diagnose asthma
44
Carbachol
Muscarinic agonist Tx open angle glaucoma and emergency closed angle glaucoma-- produce mitosis
45
Bethanechol
Muscarinic agonist treat urinary retention and help increase GI tone
46
Cevimeline
Muscarinic agonist tx of xerostomia associated with Sjogren's Syndrome
47
Pilocarpine
Muscarinic agonist Topically for glaucoma and orally for xerostomia
48
Atropine
Muscarinic antagonist ANTIDOTE FOR MUSCARINIC TOXICITY OF CHOLINERGIC DRUGS Pupil dilation Blocks M3 in GI tract-- reduction of motility Decreased gastric acid secretion Blocks M2 on heart-- causes tachycardia (Atropine can help overcome bradycardia) Blocks muscarinic receptors on salivary, sweat, and lacrimal glands
49
Scopolamine
Muscarinic antagonist prevent motion sickness and post operative nausea
50
Ipratropium
Muscarinic antagonist brochodilation and reduced mucous secretion
51
Benztropine, Trihexyphenidyl
Muscarinic antagonist treats Parkinson-like disorders
52
Tropicamide
Muscarinic antagonist Produces short acting mydriasis (pupil dilation) for better eye examination
53
Solifenacin
Muscarinic antagonist treats overactive bladder
54
Glycopyrrolate
Muscarinic antagonist Treats peptic ulcers in adults Can treat chronic drooling from neurologic disorders
55
Nicotine
Ganglionic Blocker stimulates and later depresses cholinergic function Increased release of neurotransmitters (dopamine, serotonin, norepinephrine) Increased GI motility and tone Increased BP and HR (high doses can cause BP to fall) Blood vessel constriction
56
Hexamethonium
Ganglionic blocker Blocks nicotinic receptors
57
Trimethanphan
Ganglionic blocker used for hypertensive urgencies and emergencies blocks nicotinic receptors at both sympathetic and parasympathetic ganglia
58
Neuromuscular Blocking Agents (NMBAs)
Can be Non-depolarizing agents or Depolarizing Agents Acts on acetylcholine receptors (different ways based on depolarizing vs. non-depolarizing)
59
Non-Depolarizing NMBAs
Bind the acetylcholine receptors at the neuromuscular junction so that it cannot depolarize-- this inhibits muscle contraction Cisatracurium Pancuronium Rocuronium and Vecuronium Atracurium
60
Depolarizing NMBAs
mimics acetylcholine-- much more resistant to acetylcholinesterase, so there is persistent depolarization Succinylcholine
61
Succinylcholine
Depolarizing NMBA binds nicotinic receptor that opens sodium channel-- causes depolarization Usually administered via IV, rapid onset of action May cause HYPERKALEMIA due to continued flow of potassium into the extracellular fluid