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MOHDIII - Unit 2 > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

1
Q

Muscarinic receptor agonists

A
  • bethanechol
  • carbachol
  • pilocarpine
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2
Q

Muscarinic receptor antagonists

A

atropine, glycopyrrolate, ipratropium, scopolamine, solifenacin, tolterodine, tropicamide

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3
Q

Sympathetic nervous system (SNS)

A
  • increased heart rate, pupillary dilation, reduced GI perstalsis
  • neurotransmitter: NE, receptor: adrenergic
  • exception: some sweat glands use muscarinic acetylcholine receptor
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4
Q

Parasympathetic nervous system (PNS)

A
  • increased salivation, increased peristalsis, decreased heart rate
  • neurotransmitter: acetylcholine (ACh), receptor: muscarinic
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5
Q

Catecholamine (dopamine, NE, epinephrine) synthesis

A
  • rate limiting step: tyrosine>L-DOPA (tyrosine hydroxylase)
  • epinephrine synthesized in adrenal medulla (PHENETHANOLAMINE-N-METHYLTRANSFERASE) from norepinephrine
  • dopamine effects are in renal smooth muscle
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6
Q

Acetylcholine (Cholinergic) receptors

A
  • muscarinic (certain mushrooms) & nicotinic (tobacco plant)
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7
Q

Muscarinic receptors

A 
M1: neural
M2: cardiac
M3: glandular/smooth muscle
M4: CNS
M5: unclear role in vivo
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8
Q

Odd-numbered (M1,M3,M5) muscarinic receptors

A
  • act via inositol triphosphase (IP3) involved in smooth muscle contract
  • vasodilation, bronchoconstriction, increased GI motility, increased salivation, increased sweating, voiding, defacation
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9
Q

Even numbered (M2,M4) muscarinic receptors

A
  • inhibit adenylyl cyclase & reduce cyclic AMP (cAMP)

- M2: opening of K+ channels & inhibition of Ca2+ channels slowing heart rate and decreasing contractility

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10
Q

Nicotinic acetylcholine receptors

A
  • muscle & neuronal types
  • muscle: skeletal muscle, mediates contraction
  • neuronal: both PNS & SNS
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11
Q

Nicotinic acetylcholine receptor agonists

A
  • prominent actions on neuronal receptors both in brain and autonomic ganglia
  • minimal actions on muscle type receptors
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12
Q

Nicotine pharmacology

A
  • CNS activation of receptors in regions involved w/ cognitive functions and reward
  • autonomic effects: tachycardia, increased atrial pressure, sweating
  • metabolite is cotinine: lab testing can tell smokers from non smokers from nicotine replacement
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13
Q

Varenicline

A
  • partial agonist at the alpha4beta2 subtype of neuronal nicotinic receptor
  • mediates reward effect of nicotine
  • shown to help treat nicotine dependence
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14
Q

Nicotinic acetylcholine receptor antagonists

A
  • antagonists of muscle type receptors used as neuromuscular blocker
  • mivacurium, pancuronium, vecuronium
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15
Q

Acetylcholinesterase inhibitors

A
  • increase amount of ACh in synaptic cleft at both nicotinic and muscarinic synapses
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16
Q

Clinical uses of AChe inhibitors

A
  • neuromuscular reversal agents
  • myasthenia gravis
  • alzheimer’s disease
  • insecticides
  • nerve gases
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17
Q

Myasthenia gravis

A
  • caused by antibodies targeted against muscle type nicotinic acetylcholine receptor resulting in fatigue/muscle weakness
  • treatment: long acting AChE inhibitor pyridostihmine
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18
Q

Alzheimer’s disease

A
  • AChE inhibitors that penetrate CNS
  • donepezil, rivastigmine, galantamine
  • limited effect often with only improvement for less than a year
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19
Q

Toxicologic importance of AChE inhibitors

A
  • insecticides: chlorpyrifos, parathion, malathion
  • nerve gases: VX, sarin, tabun
  • organophasphate insecticide AChE inhibitors can cause irreversible inhibition of AChE after several hours of exposure
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20
Q

AChE inhibitor poisoning

A
  • Diarrhea, Urination, Miosis, Bronchoconstriction (PNS), Excitation (muscle & CNS), Lacrimation, Salivation, Sweating
  • DUMBELSS
  • treatment: respiratory support most important-ATROPINE, if organophasphate AChE poisoning-PRALIDOXIME
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21
Q

Muscarinic acetylcholine receptor agonists

A
  • used to treat glaucoma, urinary retention, dry mouth (xerostomia)
  • bethanechol, carbachol, pilocarpine used topically for glaucoma
  • bethanechol used to manage urinary retention
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22
Q

Muscarinic acetylcholine receptor antagonists

A
  • ATROPINE, tricyclic antidepressants (amitriptyline & diphenhydramine)
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23
Q

Effects of anti-muscarinic drugs

A
  • decreased secretions (dry mouth), mydriasis (dilated pupils), cycloplegia (decreased accommodation), hyperthermia, tachycardia, bronchodilation, urinary retention & constipation
  • sedation, behavioral excitation & hallucinations seen with drugs that cross blood brain barrier
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24
Q

Clinical applications of antimuscarinics

A
  • sever bradycardia: atropine
  • acetylcholinesterase poisoning: atropine
  • pupil dilation for ophthalmology: tropicamide
  • motion sickness: scopolamine
  • dry secretions: glycopyroolate
  • parkinsonism: benztropine & diphenhydramine
  • asthma & COPD: ipratropium, tiotropium
  • bladder spasm, urinary incontinence: tolterodine, solifenacin
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25
Toxicity of antimuscarinic agents
- hyperthermia, tachycardia, cardiac arrhythmias, sedation, behavioral excitation, hallucinations - AChE inhibitors used in management
26
Adrenergic receptors
- alpha1, alpha2, beta1, beta2, beta3
27
Alpha 1 adrenergic receptor
- increase inositol triphosphate (IP3), diacylglycerol, intracellular Ca2+ - contract smooth muscle leading to vasoconstriction - urinary retention, dilates pupils
28
Alpha 2 adrenergic receptors
- inhibit adenylyl cyclase - constrict vascular smooth muscle - presynaptic receptors in CNS that inhibit NE release
29
Beta adrenergic receptors common effect
- activate adenylyl cyclase & increase intracellular cAMP
30
Beta 1 adrenergic receptor
- predominately in the heart | - increased heart rate & contractility
31
Beta 2 adrenergic receptor
- dilate or relax smooth muscle, causing vasodilation, bronchodilation, and uterine relaxation
32
Beta 3 adrenergic receptor
- lipolysis of adipose tissue & relaxation of urinary bladder
33
Alpha 1 adrenergic agonists
- mydriasis (dilated pupils), vasoconstriction, urinary retention, contraction of smooth muscle of prostate gland - specific alpha 1 agonist is PHENYLEPHRINE: used to treat nasal congestion by limiting blood flow to nasal mucosa, & when given through IV in hospital to raise blood pressure
34
Alpha 2 adrenergic agonists
- CLONIDINE is specific alpha 2 agonist that activates presynaptic receptor that has an inhibitory effect on SNS - clonidine prone to cause REBOUND HYPERTENSION if drug is stopped abruptly
35
Alpha 1 specific antagonists
- prazosin, doxazosin, terazosin, tamsulosin - prazosin & doxazosin used to treat HTN - terazosin & tamsulosin used to treat BPH - all can cause orthostatic hypotension especailly prazosin
36
Alpha 2 specific antagonists
- yohimbine | - not used clinically but is purported to have aphrodisiac effects
37
Non-specific antagonists of alpha adrenergic receptors
- phenoxybenzamine (IRREVERSIBLE) & phentolamine | - management of PHENOCHROMOCYTOMA to block catecholamines released by these tumors
38
Acetylcholinesterase inhibitors
- donepezil - insecticides - neostigmine - pyridostigmine - rivastigminea
39
Beta 1 adrenergic agonists
- dobutamine: used to treat cardiogenic shock and heart failure
40
Beta 2 adrenergic agonists
- used to treat asthma and rarely to stop premature labor
41
Albuterol
- short acting B2 agonist used for asthma attacks | - also activates B1 receptors and can cause tachycardia
42
Salmeterol, formoterol, bambuterol
- LONG ACTING selective B2 agonists used for chronic asthma therapy - association of these drugs w/ increased risk of asthma death
43
Terbutaline
- B2 agonist that can be used to halt premature labor - B2 agonists cause relaxation of uterine smooth muscle - safety concerns so terbutaline is now discouraged
44
Isoproterenol
- NON SELECTIVE Beta adrenergic agonist that lowers PVR (B2) and increases heart rate & contractility (B1) - used primarily for symptomatic bradycardia - effects blocked by non selective B-blocker like propranolol/nadolol
45
Beta 3 adrenergic agonists
- MIRABEGRON: used to treat overactive bladder
46
Agonists of both alpha and beta receptors
- norepinephrine | - epinephrine
47
Norepinephrine
- potent a1,a2, & B1 but little action at B2 - used in septic shock to increase BP through increased PVR & HR - systolic and diastolic pressure increase, which triggers compensatory vagal action to slow heart rate, PVR increases while cardiac output is unchanged or decreased
48
Epinephrine
- potent agonist at both alpha and beta receptors - dilate bronchial smooth muscle & raise blood pressure - management of anaphylactic shock
49
Epinephrine blood pressure effects
- modest rise in arterial pressure - increase in systolic pressure and a decrease in diastolic pressure - pulse rate increases
50
Epinephrine combined with alpha adrenergic antagonist
- B agonist effect are now unopposed - increased heart rate (B1) & vasodilation (B2) & drop in MAP - this is called EPINEPHRINE REVERSAL
51
Beta antagonist (B blockers) clinical uses
hypertension, cardiac arrhythmias, heart failure, angina, anxiety, muscle tremors, hyperthyroidism, glaucoma
52
Non selective beta blocker
- propranolol: used to treat anxiety, muscle tremors, hyperthyroidism because B2 receptors are involved in these disorders
53
Glaucoma treatment
- timolol: topically used to reduce aqueous humor secretion
54
Adverse effects of B-blockers
- bradycardia, AV conduction block, hypotension, sexual dysfunction * *non-selective B-blockers should be avoided in asthma patients due to bronchoconstriction caused by B2 receptors. non selective agents can also cause problems in diabetic patients blocking glycogenolysis (B2 effect)
55
Selectivity of B-blockers
- selective B1: atenolol, metoprolol, esmolol
56
Carvedilol & labetalol
- block a1, B1, & B2 - carvedilol: manage heart failure - labetalol: hypertension in pregnancy
57
Esmolol
- selective B1 blocker - IV administration w/ short duration of action (minutes) - acute management of cardiac arrhythmias
58
Nadolol duration of action
- long acting | - half life of ~24 hours
59
Acebutolol & pindolol
- B blockers w/ partial agonist effect - INTRINSIC SYMPATHOMIMETIC ACTIVITY - act as antagonist when there is high adrenergic activity - theoretic advantage is that they should cause less bradycardia
60
Amphetamine effects
- increase norepinephrine release from nerve terminals - increase release of dopamine (schizophrenic like symptoms) - NO ANTIDOTE
61
Amphetamine & amphetamine like drugs (related to ephedrine and pseudoephedrine)
- amphetamine (adderall) - methamphetamine - MDMA/ecstasy - MDA - bath salts
62
Amphetamine clinical uses
- ADHD - amphetamine mixed salts (adderall) - lisdexamfetamine (vyvanse): prodrug, lysine linked to dextroamphetamine - short term weight loss & narcolepsy
63
Methamphetamine
- abused drug is d-methamphetamine - levo (l-) isomer marked as Vicks vapor inhaler - only one prescription form on market (desoxyn): limited use for obesity and ADHD - smoking or injecting meth associated w/ binge use
64
Bath salts
- misleading name for illicit amphetamine like drugs - related to cathinone and amphetamines: mephedrone, MDPV, methylone - causes hallucinations and panic attacks
65
Cocaine
- blocks norepinephrine & dopamine reuptake - schedule II drug w/ limited use as local anesthetic in ENT surgeris - NO ANTIDOTE
66
Cocaine metabolism
- half life varies from 30 min (chronic users) to 11 hrs (newborn) - diagnostic metabolite is BENZOYLECGONINE (drug test target) - traces remain in body for weeks
67
Health complications of cocaine
- myocardial infarct, strokes, brain hemorrhage, seizures, birth defects, placental abruption (constricts placental vessels) - increased risk of birth defects, stimulates uterine contractions - crack cocaine: crack mixed with bicarbonate
68
Cocaine facts
- fatal cocaine use: death not related to blood levels, large hearts found with chronic users - perforated septum is common, burns on hands, lips, injection sites - dopamine effects: euphoria & paranoia

MOHDIII - Unit 2 (23 decks)

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