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Pharmacology > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

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
Q

Prazosin, Doxazosin, Terazosin

A

Alpha1 blockers (end in “-osin”)

treat hypertension

26
Q

Tamsulosin, Alfuzosin, Silodosin

A

alpha1 blockers (end in “-osin”)

treat benign-prostatic hypertrophy and the painful urination/urinary retention associated

27
Q

Beta Blockers (generalities)

A

Competitive inhibitors of beta-adrenergic receptors

End in “-lol”

Block the effect of catecholamines–> decrease sympathetic effects (mainly on heart)

28
Q

Beta1 Block (generalities)

A

decreased heart rate

delayed conduction through AV node

Reduced contractility

29
Q

Beta2 Block (generalities)

A

Bronchoconstriction

DO NOT USE ON ASTHMA AND COPD PATIENTS!!

30
Q

ALL beta blockers are contraindicated for _______

A

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
Q

Nonselective Beta Blockers (β1, β2)

A

propanolol, timolol, nadolol

32
Q

Propranolol

A

Nonselective beta blocker

migraine prophylaxis (has high lipid solubility, so it can penetrate the CNS)

33
Q

Timolol

A

nonselective beta blocker

decreases intraocular pressure, treats glaucoma

34
Q

Beta1 Blockers

A

CARDIOSELECTIVE

metoprolol, atenolol, nebivolol

DO NOT USE ON PATIENT WITH AV HEART BLOCK

35
Q

You can only block β___ in asthmatic patients

A

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
Q

Metoprolol

A

Beta1 blocker (cardioselective)

Tx hypertension, angina

may lower risk of death after a heart attack

37
Q

Atenolol

A

Beta1 blocker (cardioselective)

tx hypertension associated with ventricular ectopics in hyperthyroidism

38
Q

Nebivolol

A

Beta1 blocker (cardioselective)

releases NO causing vasodilation

39
Q

Carvedilol and Labetalol

A

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
Q

Muscarinic Agonists (Parasympathomimetics)

A

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
Q

Muscarinic Antagonists (Parasympatholytics)

A

increase SYMPATHETIC, decrease sweat glands

42
Q

Acetylcholine

A

Muscarinic agonist

used to test for miosis (pupil constriction) after cataract surgery

43
Q

Metacholine

A

Muscarinic agonist

used to diagnose asthma

44
Q

Carbachol

A

Muscarinic agonist

Tx open angle glaucoma and emergency closed angle glaucoma– produce mitosis

45
Q

Bethanechol

A

Muscarinic agonist

treat urinary retention and help increase GI tone

46
Q

Cevimeline

A

Muscarinic agonist

tx of xerostomia associated with Sjogren’s Syndrome

47
Q

Pilocarpine

A

Muscarinic agonist

Topically for glaucoma and orally for xerostomia

48
Q

Atropine

A

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
Q

Scopolamine

A

Muscarinic antagonist

prevent motion sickness and post operative nausea

50
Q

Ipratropium

A

Muscarinic antagonist

brochodilation and reduced mucous secretion

51
Q

Benztropine, Trihexyphenidyl

A

Muscarinic antagonist

treats Parkinson-like disorders

52
Q

Tropicamide

A

Muscarinic antagonist

Produces short acting mydriasis (pupil dilation) for better eye examination

53
Q

Solifenacin

A

Muscarinic antagonist

treats overactive bladder

54
Q

Glycopyrrolate

A

Muscarinic antagonist

Treats peptic ulcers in adults

Can treat chronic drooling from neurologic disorders

55
Q

Nicotine

A

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
Q

Hexamethonium

A

Ganglionic blocker

Blocks nicotinic receptors

57
Q

Trimethanphan

A

Ganglionic blocker

used for hypertensive urgencies and emergencies

blocks nicotinic receptors at both sympathetic and parasympathetic ganglia

58
Q

Neuromuscular Blocking Agents (NMBAs)

A

Can be Non-depolarizing agents or Depolarizing Agents

Acts on acetylcholine receptors (different ways based on depolarizing vs. non-depolarizing)

59
Q

Non-Depolarizing NMBAs

A

Bind the acetylcholine receptors at the neuromuscular junction so that it cannot depolarize– this inhibits muscle contraction

Cisatracurium
Pancuronium
Rocuronium and Vecuronium
Atracurium

60
Q

Depolarizing NMBAs

A

mimics acetylcholine– much more resistant to acetylcholinesterase, so there is persistent depolarization

Succinylcholine

61
Q

Succinylcholine

A

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

Pharmacology (2 decks)

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