Autonomic Drugs Flashcards

1
Q

Primary neurotransmitter in sympathetic NS and acts on ____

A

Norepinephrine (noradrenaline)

Alpha and beta adrenergic receptors

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2
Q

Sweat glands use ____ receptors

A

muscarinic acetylcholine

Even though its in sympathetic NS

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3
Q

Primary neurotransmitter in parasympathetic NS and acts on ____

A

Acetylcholine

muscarinic ACh receptors

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4
Q

Epinephrine produced in ___.
Activates most ____ receptors.
Synthesis requires ____

A

Adrenal medulla
Adrenergic
phenoethanolamine N-methyltransferase

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5
Q

Catecholamine synthesized from ___.

Rate limiting step:

A

Tyrosine

Tyrosine –> L-Dopa by tyrosine hydroxylase

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6
Q

Catecholamines (3)

A

Dopamine
Norepinephrine
Epineprine

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7
Q

Endogenous agonist for muscarinic and nicotinic receptors

A

Acetylcholine

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8
Q

Muscarinic receptors found on ___.

Mediates: (3)

A

targets of parasympathetic innervation

  1. Slowing cardiovascular function
  2. Increasing secretion
  3. Stimulating intestinal peristalsis
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9
Q

Subtypes of muscarinic receptors:

M1-M5

A
M1: neural
M2: cardiac
M3: glandular/smooth muscle (bladder)
M4: CNS
M5: unclear role
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10
Q

Odd numbered muscarinic receptors act via ___

Mediate:

A

Inositol triphosphase pathway

Parasympathetic vasodilation
Bronchoconstriction
Increased GI tract motility
Increased salivation, sweating and voiding, defecation

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11
Q

Even numbered muscarinic receptors act via ___
Found in:
Mediate:

A

inhibiting adenylyl cycase and reduce cyclic AMP

Heart

slowing heart rate, decreasing contractility

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12
Q

2 Main types of nicotinic receptors

A
  1. Skeletal muscle: mediates contraction

2. Neuronal: found in autonomic ganglia, brain, adrenal medulla

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13
Q

Metabolite of nicotine

A

cotinine

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14
Q

Varenicline =

Use:

A

Partial agonist of neuronal nicotinic receptor that mediates reward effect of nicotine

Treat nicotine dependence

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15
Q

Mivacurium, pancuronium, vecuronium =

Uses:

A

Nicotinic ACh receptor antagonist

Nueromuscular blocker: paralyze muscle in Sx

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16
Q

Clinical uses of AChe Inhibitors

A

Myasthenia gravis: Symptomatic treatment to try to get a lot of ACh in junction to overcome loss of receptor

Alzheimer’s disease: Penetrate CNS to overcome deficiency of cholinergic signaling

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17
Q

Donepezil
Rivastigmine
Galantamine

A

AChE inhibitors used in Alzheimer’s Disease

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18
Q

Pyridostigmine

A

Long acting AChE inhibitor used for Myasthenia gravis

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19
Q

Organophosphate AChE inhibitors cause

A

IRREVSERSIBLE inhibition of AChE

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20
Q

AChE inhibitor poisoning causes:

Symptoms:

A

activation of both muscarinic and nicotinic receptors

“DUMBLESS”: diarrhea, urination, miosis, bronchoconstriction, excitation (mm. and CNS), lacrimation, salivation, sweating

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21
Q

Treatment of AChE poisoning (2)

A

Atropine: blocks overstimulation of muscarinic receptors
Pralidoxime: prevents irreversible inhibition of AChE by organophosphate compound

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22
Q

Bethanechol, carbachol, pilocarpine =

Use:

A

Muscarinic acetylcholine receptor agonist

Topical treatment of glaucoma

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23
Q

Bethanechol =

Use:

A

Muscarinic acetylcholine receptor agonist

Urinary retention

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24
Q

Atropine =

Uses:

A

Muscarinic acetylcholine receptor antagonist
Penetrates CNS, BBB

Severe bradycardia
AChE poisoning

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25
Q

Tropicamide =

Uses:

A

Muscarinic acetylcholine receptor antagonist

Pupil dilation of ophthalmology

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26
Q

Scopolamine =

Uses:

A

Muscarinic acetylcholine receptor antagonist

Motion sickness

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27
Q

Glycopyrrolate =

Uses:

A

Muscarinic acetylcholine receptor antagonist

Dry secretions

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28
Q

Benztropine, diphenhydramine =

Uses:

A

Muscarinic acetylcholine receptor antagonists

Parkinsonism

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29
Q

Ipratropium, tiotropium =

Uses:

A

Muscarinic acetylcholine receptor antagonist

Asthma
Chronic obstructive pulmonary disease

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30
Q

Tolterodine, solifenacin =

Uses:

A

Muscarinic acetylcholine receptor antagonists

Bladder spasm
Urinary incontinence

31
Q

Treatment of antimuscarinic overdose

A

Acetylcholinesterase inhibitors

32
Q

Adrenergic alpha1 receptor actions:

A
  1. Increase inositol triphosphate, diacylglycerol, intracellular Ca2+
  2. Vasoconstriction
  3. Urinary retention: contraction of bladder trigone + sphincter
  4. Mydriasis: dilates pupil
33
Q

Adrenergic alpha2 receptor actions:

A
  1. Inhibit adenylyl cyclase
  2. Constrict smooth muscle
  3. Inhibit Norepi release
34
Q

Adrenergic beta receptors actions:

A
  1. Activate adenylyl cyclase

2. Increase intracellular cAMP

35
Q

Adrenergic beta-1 receptors actions:

A

Mainly in heart –> increased heart rate and contractility

Juxtaglomerular cells –> increase renin secretion

36
Q

Adrenergic beta-2 receptors actions:

A
Relax smooth muscle -->
1. Vasodilation
2. Bronchodilation
3. Uterine relaxation
Skeletal muscle --> uptake of K+
Liver --> glycogenolysis, gluconeogenesis
Pancreas --> insulin, glucagon secretion
Thyroid --> T4 --> T3 conversion
37
Q

Adrenergic beta-3 receptors actions:

A

Lipolysis of adipose tissue

Relaxation of urinary bladder

38
Q

Phenylephrine =

Uses:

A

Alpha-1 agonist

Nasal congestion
Raise blood pressure

39
Q

Clonidine =

Uses:

Adverse effect:

A

Alpha-2 agonist

Inhibitory effect on sympathetic NS (inhibit NE release)
Hypertension

Prone to rebound hypertension

40
Q

Prazosin =

Use:

A

alpha1 specific antagonist

hypertension

41
Q

Doxazosin =

Use:

A

alpha1 specific antagonist

hypertension

42
Q

Terazosin =

Use:

A

alpha1 specific antagonist

BPH

43
Q

Tamsulosin =

Use:

A

alpha1 specific antagonist

BPH

44
Q

All alpha-1 antagonists are capable of causing ____

A

orthostatic hypotension

45
Q

Phenoxybenzamine =

Uses:

A

Non specific alpha antagonist
IRREVERSIBLE

Pheochromocytoma (adrenal medulla tumor): block effects of catecholamines released by tumors

46
Q

Phentolamine =

Use:

A

Non specific alpha antagonist

Pheochromocytoma (adrenal medulla tumor): block effects of catecholamines released by tumors

47
Q

Dobutamine =

Uses:

A

Beta-1 agonist

Cardiogenic shock
Heart failure

48
Q

Albuterol =

Use:

Adverse effect:

A

Short acting Beta-2 agonist

Acute asthma attacks

Tachycardia

49
Q

Salmeterol, formoterol, bambuterol =

Use:

A

Long acting selective Beta 2 agonist

Chronic asthma therapy

50
Q

Terbutaline =

Use:

A

Beta 2 agonist

Prevents premature labor: relaxation of uterine smooth muscle

51
Q

Isoproterenol =

Effect:

Use:

A

Non selective beta-adrenergic agonist

Lower PVR, increase heart rate, contractility

Symptomatic bradycardia

52
Q

Mirabegron =

Use:

A

Beta 3 agonist

Overactive bladder

53
Q

Norepinephrine action:

Use:

A

Potent: alpha1, 2, beta 1 receptors
Little: beta 2 receptor

Septic shock –> used to increase blood pressure

54
Q

Epinephrine =

Use:

A

Potent agonist of both alpha and beta receptors

Anaphylactic shock: Dilate bronchial smooth muscle and raise blood pressure

55
Q

Effects of epinephrine:

A
  1. Vasoconstriction
  2. Increase heart rate and contraction
  3. Vasodilation of large vessels in skeletal muscle
  4. Dilation of bronchial smooth muscle
  5. Increase systolic, decrease diastolic BP
56
Q

Epinephrine + alpha-adrenergic antagonist =

A

beta agonist effect unopposed –> increase heart rate, prominent vasodilation, decrease mean arterial pressure

57
Q

Adverse effects of beta-blocker

A

Bradycardia
AV conduction block
Hypotension
Sexual dysfunction

58
Q

Non-selective beta-blockers should be avoided in:

A
  1. Asthma patients b/c blocks B2 receptor –> bronchoconstriction
  2. Diabetic patients b/c block glycogenolysis
59
Q

Selective Beta-1 antagonists

A

Atenolol
Metoprolol
Esmolol
Nadolol

60
Q

Non-selective beta blockers

A

Propranolol

Timolol

61
Q

Drugs that block alpha1, beta 1 and 2 receptors

A

Carvedilol

Labetalol

62
Q

Esmolol =

Use:

A

Selective Beta-1 antagonist
Very short half life

Cardiac arrhythmia

63
Q

Nadolol =

Use:

A

Non-selective Beta antagonist
Long half life
Not lipophilic

Cardiac arrhythmia

64
Q

Acebutolol, pindolol =

A

Beta blocker w/ weak partial agonist of beta receptors

Cause less bradycardia

65
Q

Carvedilol =

Use:

A

Beta blocker w/ alpha-adrenergic antagonist

Heart failure

Improves insulin sensitivity

66
Q

Labetalol =

Use:

A

Beta blocker w/ alpha-adrenergic antagonist
ISA+

Vasodilator in HTN –> won’t slow down b/c heart rate not affected
Hypertension in pregnancy
Pheochromocytoma

67
Q

Amphetamines action:

Uses:

A

Increase norepi release from nerve terminals
Increase release of dopamine

ADHD: Adderall
Short-term weight loss
Narcolepsy

68
Q

Cocaine action:

Use:

Metabolite:

A

Blocks norepi and dopamine reuptake

Local anesthetic in ENT surgeries

Benzoylecgonine

69
Q

Pindolol =

A

Nonselective Beta adrenergic antagonist
Block beta receptor w/o slowing heart
Lipophilic –> treat neuogenic syncopy –> low level beta stimulant

Good in healthy people

70
Q

Nebivolol =

A

Selective beta1 adrenergic antagonist

Pulmonary HTN
Produce NO
Heart works better: increased CO, SV, EF, LVEDV

71
Q

Beta-blockers: 1 of the only drugs to

A

Decrease mortality
Cardioprotective mechanisms
Reduce sympathetic NS
Increase ventricular fibrillation in ischemia
Stability of coronary atherosclerotic plaques
Myocardial oxygen consumption by suppressing lipoysis –> metabolize more glucose

72
Q

Verapamil =

Use:

Metabolism:

A

Potent AV nodal blockade

Multifocal atrial tachycardia, idiopathic fascicular ventricular tachycardia
Premature ventricular contraction

Pulmonary friendly
Work synergistic w/ beta blockers

Liver

73
Q

Diltiazem =

Metabolism:

A

AV nodal blockade

Work synergistic w/ beta blockers

Renal