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Autonomic Pharmacology Flashcards

0
Q

Muscarinic ACh Receptors

A

Main antigen is acetylcholine
Parasympathetic post ganglionic neurons
M1, M3, M5: IP3 pathway > increase Ca2+ > SM contraction
M2, M4: inhibit adenyly cyclase and reduce cAMP

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1
Q

Adrenergic Receptors

A

Receptor antigen is norepinephrine or epinephrine (adrenaline: synthesized in adrenal medulla via enzyme phenethanolamine N-methyltransferase)
Sympathetic nervous system

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2
Q

Nicotinic ACh Receptors

A

Preganglionic neurons of parasympathetics, somatic muscle neuromuscular junction
Activation via acetylcholine (release inhibited by botulinum toxin (Botox)

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3
Q

Muscarinic activation

A
  • Slows cardiovascular function
  • Increases secretions
  • increases intestinal activity
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4
Q

Cotinine

A

Main metabolite of nicotine in body

Used for laboratory testing to see if someone smokes

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5
Q

Varenicline

A

partial agonist of a4B2 neuronal nicotinic receptors

Used: treat nicotine dependence and reduces the cravings

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6
Q

Mivacurium

A

nicotinic receptor antagonist (competitive)
Use: neuromuscular blocker = paralyzer
Used in surgeries

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7
Q

Pancuronium

A

nicotinic receptor antagonist (competitive)
Use: neuromuscular blocker = paralyzer
Used in surgeries

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8
Q

Vecuronium

A

nicotinic receptor antagonist (competitive)
Use: neuromuscular blocker = paralyzer
Used in surgeries

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9
Q

Three common organophosphate AchE inhibitors in industry

A

pesticides, parathion, chloropyrifos, malathion (insecticide) and nerve gas (sarin, tabun, VX)
Initial binding to AChE can be reversed but after a few hours, phosphorylated enzyme ages (covalent bond formed) > irreversible

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10
Q

Neostigmine

A

AchE inhibitor
Reversal of non-depolarizing neuromuscular blockers
Use: Treatment of myasthenia gravis
SE: Poisoning > activation of both muscarinic and nicotinic receptors > fatal

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11
Q

Pyridostigmine

A

AchE inhibitor

Use: main treatment for myasthenia gravis

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12
Q

Donepezil (Aricept)

A

AChE Inhibitor

Uses: Palliative treatment of Alzheimer’s disease

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13
Q

Galantamine (Razadyne)

A

AChE Inhibitor

Uses: Palliative treatment of Alzheimer’s disease

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14
Q

Rivastigmine (Exelon)

A

AChE Inhibitor

Uses: Palliative treatment of Alzheimer’s disease

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15
Q

Pralidoxime (2-PAM)

A

Prevents irreversible binding of organophosphate AChE inhibitors to AChE if given prior to a few hours

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16
Q

Toxicity effects of acetylcholinesterase inhibitors

A

DUMBELSS: diarrhea, urination, miosis (contraction of sphincter in eye), bronchoconstrictoin, excitation of muscle (most life threatening) and CNS, lacrimation, salivation, sweating
-Overload of skeletal nicotinin Ach receptors > muscle paralysis > death

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17
Q

Atropine (belladonna)

A

Muscarinic antagonist: tertiary amine that can cross BBB (can cause sedation, behavioral excitation and hallucinations)
Uses: Dilate pupils, treat severe bradycardia
Can be given to help relieve AChE inhibitor poisoning to block muscarinic effects (diarrhea)

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18
Q

Bethanechol

A 
muscarinic agonist (agonist for muscarinic receptors not often used)
Use: treatment of urinary retention
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19
Q

Betanechol, carbachol, pilocarpine

A

Muscarinic agonist
Contract pupillary constrictor > allow aqueous humor to drain out of eye
Uses: Acute glaucoma attack (outflow of aqueous humor into canal of Schlemm is blocked)

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20
Q

SE of anti-muscarinic drugs

A

Decreased secretions (dry mouth), mydriasis (dilated pupil), cycloplegia (decreased accommodation), hyperthermia, tachycardia, sedation (BBB), bronchodilation, urinary retention, constipatoin, behavior excitation and hallucinations (BBB)

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21
Q

Scopolamine

A 
Muscarinic antagonist (can cross BBB)
Use: motion sickness due to sedative and amnesiac effects
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22
Q

Glycopyrrolate

A

Muscarinic antagonist

Use: Dry secretions to prevent aspirations of fluids

23
Q

Benztropine

A

Muscarinic antagonist

Use: Parkinsonism (including drug induced)

24
Tropicamide
Muscarinic antagonist | Use: dilate pupils (shorter acting than atropine), more effective in clinical ophthalmology visit
25
Ipratropium
Muscarinic antagonist Use: treat asthma and COPD Combined with albuterol (B-agonist) as an inhaler
26
Tolerodine
Muscarinic antagonist | Use: treat bladder spasm and urinary incontinenct
27
Solifenacin
Muscarinic antagonist | Use: treat bladder spasm and urinary incontinenct
28
Tiotropium (Spiriva)
Muscarinic antagonist Use: treat COPD Capsuled form that is pierced > aerosolized and inhaled
29
Treatment of urinary incontinence and overactive bladder
Tolterodine, oxybuynin, solifenacin | Muscarinic antagonists
30
Amitriptyline (Elavil)
Tricylic antidepressant with antimuscarinic properties | Overdose > fatal due to antimuscarinic effects (cardiac arythmias)
31
How do you treat anti-muscarinic overdose
AChE inhibitors
32
How do you treat AChE overdose
Atropine
33
alpa Adrenergic receptors
a1: increase IP3, diacylglycerol and intraellular Ca+ > SM contraction (determinant of systemic BP) a2: inhibit adenylyl cyclase > decreased calcium influx > decreased release of norepinephrine (located at presynaptic terminals > inhibit neurotransmitter release > reduce central adrenergic effects)
34
Beta adrenergic receptors
All activate adenylyl cyclase + increase intracellular cAMP B1: expressed in heart > increase HR B2:dilate/relax SM>vasodilation, bronchodilation and uterine relaxtation B3: lipolysis of adipose tissue + relaxation of urinary bladder
35
alpha1-adrenergic receptor activation
mydriasis (pupil dilation), vasoconstriction, contraction of bladder trigone + sphincter (urinary retention), SM contraction of prostate
36
Phenylephrine
alpha1-adrenergic receptor agonist | Use: treat nasal congestion (constrict vessels), IV > raise BP in acute setting
37
Clonidine
alpha2-agonist UsE: treat hypertension > reduce central norepinephrine release SE: rebound hypertension if stopped abruptly
38
Prazosin
alpha1-adrenergic receptor antagonist (specific) | Use: treatment of hypertension via vasodilation
39
Terazosin
alpha1-adrenergic receptor antagonist (specific) | Use: treatment of benign prostatic hypertrophy > relaxes prostate capsular SM
40
Phenoxybenzamine
Non-specific (a1+a2) alpha-adrenergic antagonist | Use: manage pheochromocytoma (tumor that secretes catecholamines)
41
Phentolamine
Non-specific (a1+a2) alpha-adrenergic antagonist | Use: manage pheochromocytoma (tumor that secretes catecholamines)
42
B1-adrenergic receptor activation
Increased heart rate (SA node), increased conduction velocity (AV node), increased force of contraction (atrial + ventricular muscle)
43
Dobutamine
B-1 adrenergic receptor agonist | Use: treat cardiogenic shock and heart failure
44
B-blockers (B-1adrenergic receptor antagonist) action
Treat angina, hypertension, arrhythmias
45
B2-adrenergic receptor effects
vasodilation (all vessels), decreased pre-load, muscle tremor, glycogenolysis, uterine relaxation, bronchodilation
46
Albuterol
B2-adrenergic receptor agonist Use: shorta acting inhaler for acute asthma attacks SE: also activates B1 > tachycardia
47
Salmeterol
B2-adrenergic receptor agonist (selective) Use: long acting (not used for asthma attacks) for chronic asthma SE: increased risk of asthma death
48
Formoterol
B2-adrenergic receptor agonist (selective) Use: long acting (not used for asthma attacks) for chronic asthma SE: increased risk of asthma death
49
Bambuterol
B2-adrenergic receptor agonist (selective) Use: long acting (not used for asthma attacks) for chronic asthma SE: increased risk of asthma death
50
Terbutaline
B2- adrenergic receptor agonist | Use: no longer (black box) fast-acting bronchodilator and also use in uterine relaxation to stop premature labor
51
Isoproterenol
non-selective B-adrenergic agonist Use: treatment of bradycardia (effects blocked by B-blockers) Mechanism: B2 effect = lower vascular resistance B1 effect = increase HR and contractility
52
Mirabegron
B3-adrenergic receptor agonist Use: treatment of overactive bladder Relax urinary bladder SM + enhance lipolysis
53
Norepinephrine
a+B adrenergic receptor agonist (B1 more than B2) Use: Increase BP Effects: Increase SBP, DBP > vagal response > slow HR, increase peripheral vascular resistance
54
Epinephrine
a+B-adrenergic receptor agonist Use: cardiac arrest, anaphylaxis, severe asthma (results in increase SBP, decrease DBP = increase MAP, accelerated HR) Effects: vasoconstriction of vascular beds (precapillary vessels, a1), increase HR (B1), increase contraction (B1), bronchodilation (B2), vasodilation of large vessels in skeletal muscle (B2)

Medications (3 decks)

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