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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
Cistracurium
- Anti cholinergic - Non-depolarizing NMB - Binds to N receptors on end plate to antagonize ACh and stop depolarization - ADR's: prolonged via diaphragm paralysis
26
Rocuronium
- 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
27
Vecuronium
- 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
28
Pancuronium
- 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
29
Sugammadex
-Forms complex with Rocuronium or vecuronium to render them inactive and prevent N blockade
30
Succinylcholine
- 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
31
Dantrolene
- Skeletal muscle relaxant - Directly interferes with Ca2+ ion release from SR in skeletal muscle cells (uncoupling of excitation-contraction process)
32
Cocaine
- 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)
33
Amphetamine
- Central stimulants - Amphetamines - Promote release of NE (primarily) and DA (lesser extent) - Paired with dextroamphetamine: adderall
34
Dextroamphetamine
- Central stimulants - Amphetamines - Promote release of NE (primarily) and DA (lesser extent) - When paired with amphetamine: adderall - dexedrine
35
Lisdexamfetamine
- 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
Methamphetamine
- Central stimulants - Amphetamines - Promote release of NE (primarily) and DA (lesser extent) - Indicated for narcolepsy
37
Methylphenidate
- 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
Dexmethylphenidate
- 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
Atomoxetine
- Indirect sympathomimetics - Thought to involve NET reuptake inhibition - Non-stimulant for treatment of ADHD (for peds)
40
Modafinil
- Indirect sympathomimetics - Increases concentrations of NE, DA, 5HT, Glu - Decreases concentration of GABA - Uses: narcolepsy, circadian rhythm disturbances
41
Midodrine
- Selective Alpha-1 Agonist - Prodrug - Treatment of orthostatic hypotension
42
Phenylephrine
- Selective Alpha-1 Agonist | - Cough/cold; IV vasopressor (vasoconstrictor)
43
Pseudoephedrine
- Selective Alpha-1 Agonist | - Decongestant for cough/cold
44
Oxymetazoline
- 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
Naphazoline
- Selective Alpha-1 Agonist | - Eye drops for red eye
46
Doxazosin
- 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
Terozosin
- 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
Prazosin
- 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
Tamsulosin
- 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
Alfuzosin
- 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
Silodosin
- 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
Clonidine
- Selective Alpha2 Agonist | - HTN, ADHD, withdrawal, muscle spasticity
53
Tixanidine
- Selective Alpha2 Agonist | - HTN, ADHD, withdrawal, muscle spasticity
54
Guanfacine
- Selective Alpha 2 agonist | - ADHD, older drug for HTN
55
Dexmedetomidine
- Selective Alpha 2 agonist | - IV sedative with sympatholytic/analgesic properties
56
Brimonidine
- Selective Alpha 2 agonist | - Eye drops for glaucoma (dilates and decrease aqueous humor)
57
Apraclonidine
- Selective Alpha 2 agonist | - Eye drops for glaucoma (dilates and decrease aqueous humor)
58
Methyldopa
- Selective Alpha 2 agonist - Prodrug - Favorable agent for HTN in pregnancy
59
Yohimbine
- Selective Alpha 2 antagonist? - Male erectile dysfunction - Limited evidence: concern for elevated BP/HR, increased motor activity, and irritability, tremor
60
Phenoxybenzamine
- 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
Phentolamine
- 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
Non-AD AChI's ADR's
- Affects both N and M due to decrease in specificity - M: salivation, urination, bradycardia, bronchoconstriction, abdominal cramping - N: muscle fasciculation/cramping
63
Dobutamine
- Selective beta-1 agonist - Positive inotropic effect >> chronotropic effects - IV (requires dose titration to desired effect) - Therapeutic use: short term, cardiogenic shock, septic shock, acute congestive HF
64
Metroprolol succinate
- 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
Metroprolol tartrate
- 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
Atenolol
- 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
Bisoprolol
- 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
Nebivolol
- 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
Esmolol
- 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
Betaxolol
- 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
Acebutolol
- 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
Albuterol
- 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
Levalbuterol
- 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
Formoterol
- 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
Salmeterol
- 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
Olodaterol
- 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
Arformoterol
- 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
Indacaterol
- 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
Terbutaline
- Selective beta-2 agonist - Bronchodialtion - Oral - ADR's: Selective unless given at higher doses and may act on beta1 (tachycardia)
80
Isoproterenol
- Non-selective beta agonist - Old drug - Primarily used for beta-1 effect (positive inotrope) - Use largely replaced by dobutamine
81
metaproterenol
- Non-selective beta agonist - Primarily used for beta-2 effect (bronchodilation) - Asthma/COPD; bronchospasm
82
Mirabegron
- 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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