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Pharmacology Exam 2 > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

Methacholine

A
  • Direct cholinergic agonist
  • Methacholine Challenge Test
  • Susceptible to AChE
  • M action only
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2
Q

Carbachol

A
  • Direct cholinergic agonist
  • Contracts iris and ciliary muscle (miosis)
  • Apply locally as ophthalmic drops
  • M and N action
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3
Q

Bethanechol

A
  • Direct cholinergic agonist
  • postop/postpartum non-obstructive urinary retention, atonic neurogenic bladder, gastric atony
  • M action only
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4
Q

Pilocarpine

A
  • Direct cholinergic agonist
  • Contracts iris and ciliary muscle (miosis)
  • Apply locally as ophthalmic drops
  • Xerostomia associated with Sjögren’s syndrome or radiation form head and neck cancers
  • M action only
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5
Q

Cevimeline

A
  • Direct cholinergic agonist
  • Xerostomia associated with Sjörgen’s syndrome or radiation from head and neck cancers
  • M action only
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6
Q

Nicotine

A
  • Cholinergic, N receptor agonist (PANS and SANS)
  • SANS: increase BP/HR, sweating, reduced GI motility, skeletal muscle relaxation
  • CNS: increase alertness in drowsy pt and increase relaxation in tense subject
  • Typically requires gradual reduction in nicotine
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7
Q

Nicotine Replacement Therapy (NRT)

A
  • Cholinergic, N receptor agonist
  • Stimulates the α4ß2 Nn receptors to stimulate DA release
  • Delivers nicotine slower than smoking having fewer positive reinforcing effects/habits
  • Cannot actively smoke
  • Types: gum, lozenge, patch, nasal spray, inhaler
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8
Q

Varenicline (Chantix)

A
  • Cholinergic, N receptor partial agonist
  • Has higher affinity for α4ß2
  • N receptor stimulation is ~30-60%
  • Used for smoking cessation
  • Can initially smoke but need to set a quit date
  • ADR’s: vivid/abnormal dreams, insomnia, N/V, constipation, neuropsychiatric disorders (boxed warning)
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9
Q

Bupropion (Zyban)

A
  • Antidepressant that can be used for smoking cessation
  • Inhibits re-uptake of DA and NE
  • FDA indication for smoking cessation, not sure on the mechanism (increase in NE may decrease withdrawal symptoms and increase of DA may decrease cravings)
  • Can smoke initially
  • ADR’s: agitation, insomnia, dry mouth, nausea, tachycardia, can lower seizure threshold (dosing limitations)
  • Welbutrin
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10
Q

Tacrine

A
  • Indirect cholinergic, AChI

- Removed from market due to hepatotoxicity

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11
Q

Rivastigmine

A
  • Indirect cholinergic, AChI

- Mild-moderate AD

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12
Q

Galantamine

A
  • Indirect cholinergic, AChI

- Mild-moderate AD

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13
Q

Donepezil

A
  • Indirect cholinergic, AChI
  • Mild-moderate AD and moderate-severe AD
  • Longer 1/2 life potentially helps with more severe AD
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14
Q

AChI

A
  • Increases ACh by blocking AChE

- ADR’s: bradycardia (dose-limiting), dizziness, increased urinary frequency, GI: nausea and diarrhea

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15
Q

Edrophonium

A
  • Indirect cholinergic, non-AD AChI
  • MG diagnosis
  • Short-acting (5-15 min duration of action)
  • Edrophonium test: used to distinguish between cholinergic (worsening) and myasthenic (improvement) crises
  • NMB reversal
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16
Q

Neostigmine

A

-Indirect cholinergic, non-AD AChI
-MG treatment
-NMB reversal
-Postop ileus and urinary retention
-0.5-2 hours duration of action
-

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17
Q

Pyridostigmine

A

-Indirect cholinergic, non-AD AChI
-MG treatment
-NMB reversal
-3-6 hour duration of action
-

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18
Q

Physostigmine

A
  • Indirect cholinergic, non-AD AChI
  • Anticholinergic toxidrome
  • Previously used in glaucoma
  • 0.5-2 hours
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19
Q

Ambenonium

A
  • Indirect cholinergic, non-AD AChI
  • MG treatment
  • 4-8 hour duration of action
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20
Q

Organophosphate

A
  • Indirect cholinergic, non-AD AChI
  • Irreversible AChI
  • Pesticides (Malathion and parathion), nerve gas (Sarin), herbicides
  • Covalent bonds to AChE active site and leads to non-specific increase of ACh in peripheral and central M and N receptors
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21
Q

Malathion

A
  • Indirect cholinergic, non-AD AChI
  • Irreversible AChI
  • Used to treat lice and causes lice to have cholinergic toxidrome
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22
Q

Sarin

A
  • Indirect cholinergic, non-AD AChI
  • Irreversible AChI
  • Nerve gas
  • Covalent bonds to AChE and causes for too much ACh
  • Induces cholinergic toxidrome
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23
Q

Pralidoxime (2-PAM)

A
  • Antidote to Sarin
  • Enzyme reactivation prior to aging of enzyme
  • Breaks the phosphorous- enzyme bond created
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24
Q

Atracurium

A
  • Anti cholinergic
  • Non-depolarizing NMB
  • Binds to N receptors on end plate to antagonize ACh and stop depolarization
  • ADR’s: prolonged via diaphragm paralysis
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25
Q

Cistracurium

A
  • Anti cholinergic
  • Non-depolarizing NMB
  • Binds to N receptors on end plate to antagonize ACh and stop depolarization
  • ADR’s: prolonged via diaphragm paralysis
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26
Q

Rocuronium

A
  • Anti cholinergic
  • Non-depolarizing NMB
  • Binds to N receptors on end plate to antagonize ACh and stop depolarization
  • Sugammadex used to reverse
  • ADR’s: prolonged via diaphragm paralysis
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27
Q

Vecuronium

A
  • Anti cholinergic
  • Non-depolarizing NMB
  • Binds to N receptors on end plate to antagonize ACh and stop depolarization
  • Sugammadex used to reverse
  • ADR’s: prolonged via diaphragm paralysis
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28
Q

Pancuronium

A
  • Anti cholinergic
  • Non-depolarizing NMB
  • Binds to N receptors on end plate to antagonize ACh and stop depolarization
  • Longest duration
  • ADR’s: prolonged via diaphragm paralysis
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29
Q

Sugammadex

A

-Forms complex with Rocuronium or vecuronium to render them inactive and prevent N blockade

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30
Q

Succinylcholine

A
  • Anti-cholinergic
  • Depolarizing NMB
  • Competes with ACh for N receptors and mimics ACh to depolarize the end plate
  • Prolonged depolarization
  • Ultra-short acting NMB
  • ADR’s: malignant hyperthermia
  • Treat with dantrolene
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31
Q

Dantrolene

A
  • Skeletal muscle relaxant
  • Directly interferes with Ca2+ ion release from SR in skeletal muscle cells (uncoupling of excitation-contraction process)
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32
Q

Cocaine

A
  • Adrenergic
  • Inhibits NET; increased SANS effect (vasoconstriction, increased alertness, enhanced reward)
  • Stimulates pre-synaptic NE release
  • Central DA reuptake inhibition
  • Acute DA release
  • Therapeutic use: topical local anesthetic (Na channel inhibitor)
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33
Q

Amphetamine

A
  • Central stimulants
  • Amphetamines
  • Promote release of NE (primarily) and DA (lesser extent)
  • Paired with dextroamphetamine: adderall
34
Q

Dextroamphetamine

A
  • Central stimulants
  • Amphetamines
  • Promote release of NE (primarily) and DA (lesser extent)
  • When paired with amphetamine: adderall
  • dexedrine
35
Q

Lisdexamfetamine

A
  • Central stimulants
  • Amphetamines
  • Promote release of NE (primarily) and DA (lesser extent)
  • Prodrug of dextroamphetamine
  • “f” for prodrug
  • Used for binge-eating disorder, “f” for food
36
Q

Methamphetamine

A
  • Central stimulants
  • Amphetamines
  • Promote release of NE (primarily) and DA (lesser extent)
  • Indicated for narcolepsy
37
Q

Methylphenidate

A
  • Central stimulants
  • Non-amphetamines
  • Promote release of DA (primarily) and NE (lesser extent)
  • Less jittery (less of a SANS effect)
  • Slightly less cardiac effect
  • “DA involved in date”
38
Q

Dexmethylphenidate

A
  • Central stimulants
  • Non-amphetamines
  • Promote release of DA (primarily) and NE (lesser extent)
  • Less jittery (less of a SANS effect)
  • Slightly less cardiac effect
  • “DA involved in date”
39
Q

Atomoxetine

A
  • Indirect sympathomimetics
  • Thought to involve NET reuptake inhibition
  • Non-stimulant for treatment of ADHD (for peds)
40
Q

Modafinil

A
  • Indirect sympathomimetics
  • Increases concentrations of NE, DA, 5HT, Glu
  • Decreases concentration of GABA
  • Uses: narcolepsy, circadian rhythm disturbances
41
Q

Midodrine

A
  • Selective Alpha-1 Agonist
  • Prodrug
  • Treatment of orthostatic hypotension
42
Q

Phenylephrine

A
  • Selective Alpha-1 Agonist

- Cough/cold; IV vasopressor (vasoconstrictor)

43
Q

Pseudoephedrine

A
  • Selective Alpha-1 Agonist

- Decongestant for cough/cold

44
Q

Oxymetazoline

A
  • Selective Alpha-1 Agonist
  • Nasal spray, rhinitis medicamentosa
  • Makes hole in nose with over use, only use in low frequency and not too much
45
Q

Naphazoline

A
  • Selective Alpha-1 Agonist

- Eye drops for red eye

46
Q

Doxazosin

A
  • Selective Alpha-1 Antagonist
  • Block all alpha-1 subtypes
  • Use for HTN and/or BPH
  • End in “sin”
  • ADR’s: dizziness, hypotension, reflex tachycardia, first-dose phenomenon
47
Q

Terozosin

A
  • Selective Alpha-1 Antagonist
  • Block all alpha-1 subtypes
  • Use for HTN and/or BPH
  • End in “sin”
  • ADR’s: dizziness, hypotension, reflex tachycardia, first-dose phenomenon
48
Q

Prazosin

A
  • Selective Alpha-1 Antagonist
  • Block all alpha-1 subtypes
  • Use for HTN and/or BPH
  • End in “sin”
  • Used in PTSD nightmares (CNS alpha1 receptors)
  • ADR’s: dizziness, hypotension, reflex tachycardia, first-dose phenomenon
49
Q

Tamsulosin

A
  • Selective Alpha-1 Antagonist
  • More selective for alpha-1A receptors on prostate/urethra
  • End in “sin”
  • ADR’s: dizziness, hypotension, reflex tachycardia, first-dose phenomenon
50
Q

Alfuzosin

A
  • Selective Alpha-1 Antagonist
  • More selective for alpha-1A receptors on prostate/urethra
  • End in “sin”
  • ADR’s: dizziness, hypotension, reflex tachycardia, first-dose phenomenon
51
Q

Silodosin

A
  • Selective Alpha-1 Antagonist
  • More selective for alpha-1A receptors on prostate/urethra
  • End in “sin”
  • Most selective for alpha 1A (BPH)
  • Least hypotensive
  • ADR’s: dizziness, hypotension, reflex tachycardia, first-dose phenomenon
52
Q

Clonidine

A
  • Selective Alpha2 Agonist

- HTN, ADHD, withdrawal, muscle spasticity

53
Q

Tixanidine

A
  • Selective Alpha2 Agonist

- HTN, ADHD, withdrawal, muscle spasticity

54
Q

Guanfacine

A
  • Selective Alpha 2 agonist

- ADHD, older drug for HTN

55
Q

Dexmedetomidine

A
  • Selective Alpha 2 agonist

- IV sedative with sympatholytic/analgesic properties

56
Q

Brimonidine

A
  • Selective Alpha 2 agonist

- Eye drops for glaucoma (dilates and decrease aqueous humor)

57
Q

Apraclonidine

A
  • Selective Alpha 2 agonist

- Eye drops for glaucoma (dilates and decrease aqueous humor)

58
Q

Methyldopa

A
  • Selective Alpha 2 agonist
  • Prodrug
  • Favorable agent for HTN in pregnancy
59
Q

Yohimbine

A
  • Selective Alpha 2 antagonist?
  • Male erectile dysfunction
  • Limited evidence: concern for elevated BP/HR, increased motor activity, and irritability, tremor
60
Q

Phenoxybenzamine

A
  • Non-selective Alpha Antagonists
  • Vasodilates while increasing cardiac output– benefit seen in diagnosis/treatment of pheochromocytoma
  • Oral
  • Treatment of extravasation from IV alpha 1 agonist?
  • ADR’s: nasal congestion, miosis, orthostatic hypotension
61
Q

Phentolamine

A
  • Non-selective Alpha Antagonists
  • Vasodilates while increasing cardiac output– benefit seen in diagnosis/treatment of pehochromocytoma
  • IV/IM
  • Pareternal and has shorter duration of action (more inpatient use)
  • Treatment of extravasation from IV alpha 1 agonist?
  • ADR’s: nasal congestion, miosis, orthostatic hypotension
62
Q

Non-AD AChI’s ADR’s

A
  • Affects both N and M due to decrease in specificity
  • M: salivation, urination, bradycardia, bronchoconstriction, abdominal cramping
  • N: muscle fasciculation/cramping
63
Q

Dobutamine

A
  • Selective beta-1 agonist
  • Positive inotropic effect&raquo_space; chronotropic effects
  • IV (requires dose titration to desired effect)
  • Therapeutic use: short term, cardiogenic shock, septic shock, acute congestive HF
64
Q

Metroprolol succinate

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • Once daily option (outpatient)
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
65
Q

Metroprolol tartrate

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • 3-4 times daily (inpatient)
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
66
Q

Atenolol

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • Only beta blocker that use renal dosing requirements
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
67
Q

Bisoprolol

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • Generally maintains selectivity at higher doses
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
68
Q

Nebivolol

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • Generally maintains selectivity at higher doses
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
69
Q

Esmolol

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
70
Q

Betaxolol

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
71
Q

Acebutolol

A
  • Selective beta-1 antagonist
  • Decrease HR, FOC, and AV conduction
  • Also has ISA: intrinsic sympathomimetic activity, like a partial agonist.
  • Benefit: doesn’t block as potently and can use with a baseline bradycardia
  • ADR’s: will cause up regulation (can’t abruptly stop taking drug otherwise excessive SANS response)
72
Q

Albuterol

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • SABA: rescue inhalers, quick onset and quick offset
  • Local
  • ADR’s: Selective unless given at higher doses and may act on beta-1 (tachycardia)
73
Q

Levalbuterol

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • SABA: rescue inhalers, quick onset and quick offset
  • Local
  • ADR’s: Selective unless given at higher doses and may act on beta-1 (tachycardia)
74
Q

Formoterol

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • LABA: end in terol, long acting, use in COPD setting, daily use, combined with steroid/anticholinergics
  • Local
  • ADR’s: Selective unless given at higher doses and may act on beta-1 (tachycardia)
75
Q

Salmeterol

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • LABA: end in terol, long acting, use in COPD setting, daily use, combined with steroid/anticholinergics
  • Local
  • ADR’s: Selective unless given at higher doses and may act on beta-1 (tachycardia)
76
Q

Olodaterol

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • LABA: end in terol, long acting, use in COPD setting, daily use, combined with steroid/anticholinergics
  • Local
  • ADR’s: Selective unless given at higher doses and may act on beta-1 (tachycardia)
77
Q

Arformoterol

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • LABA: end in terol, long acting, use in COPD setting, daily use, combined with steroid/anticholinergics
  • Local
  • ADR’s: Selective unless given at higher doses and may act on beta-1 (tachycardia)
78
Q

Indacaterol

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • LABA: end in terol, long acting, use in COPD setting, daily use, combined with steroid/anticholinergics
  • Local
  • ADR’s: Selective unless given at higher doses and may act on beta-1 (tachycardia)
79
Q

Terbutaline

A
  • Selective beta-2 agonist
  • Bronchodialtion
  • Oral
  • ADR’s: Selective unless given at higher doses and may act on beta1 (tachycardia)
80
Q

Isoproterenol

A
  • Non-selective beta agonist
  • Old drug
  • Primarily used for beta-1 effect (positive inotrope)
  • Use largely replaced by dobutamine
81
Q

metaproterenol

A
  • Non-selective beta agonist
  • Primarily used for beta-2 effect (bronchodilation)
  • Asthma/COPD; bronchospasm
82
Q

Mirabegron

A
  • Selective beta-3 agonist
  • On the detrusor
  • To treat overactive bladder, urinary incontinence, urgency, and frequency
  • Increases bladder capacity during storage phase
  • ADR’s: BP elevation, tachycardia
  • Alternative to anti-M’s?– is usually the treatment but they have a lot of ADR’s so beta 3 is ideal

Pharmacology Exam 2 (6 decks)

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