Autonomic Drugs

Question 1

Primary neurotransmitter in sympathetic NS and acts on ____

Answer 1

Norepinephrine (noradrenaline)

Alpha and beta adrenergic receptors

Question 2

Sweat glands use ____ receptors

Answer 2

muscarinic acetylcholine

Even though its in sympathetic NS

Question 3

Primary neurotransmitter in parasympathetic NS and acts on ____

Answer 3

Acetylcholine

muscarinic ACh receptors

Question 4

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

Answer 4

Adrenal medulla
Adrenergic
phenoethanolamine N-methyltransferase

Question 5

Catecholamine synthesized from ___.

Rate limiting step:

Answer 5

Tyrosine

Tyrosine –> L-Dopa by tyrosine hydroxylase

Question 6

Catecholamines (3)

Answer 6

Dopamine
Norepinephrine
Epineprine

Question 7

Endogenous agonist for muscarinic and nicotinic receptors

Answer 7

Acetylcholine

Question 8

Muscarinic receptors found on ___.

Mediates: (3)

Answer 8

targets of parasympathetic innervation

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

Question 9

Subtypes of muscarinic receptors:

M1-M5

Answer 9

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

Question 10

Odd numbered muscarinic receptors act via ___

Mediate:

Answer 10

Inositol triphosphase pathway

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

Question 11

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

Answer 11

inhibiting adenylyl cycase and reduce cyclic AMP

Heart

slowing heart rate, decreasing contractility

Question 12

2 Main types of nicotinic receptors

Answer 12

1. Skeletal muscle: mediates contraction

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

Question 13

Metabolite of nicotine

Answer 13

cotinine

Question 14

Varenicline =

Use:

Answer 14

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

Treat nicotine dependence

Question 15

Mivacurium, pancuronium, vecuronium =

Uses:

Answer 15

Nicotinic ACh receptor antagonist

Nueromuscular blocker: paralyze muscle in Sx

Question 16

Clinical uses of AChe Inhibitors

Answer 16

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

Question 17

Donepezil
Rivastigmine
Galantamine

Answer 17

AChE inhibitors used in Alzheimer’s Disease

Question 18

Pyridostigmine

Answer 18

Long acting AChE inhibitor used for Myasthenia gravis

Question 19

Organophosphate AChE inhibitors cause

Answer 19

IRREVSERSIBLE inhibition of AChE

Question 20

AChE inhibitor poisoning causes:

Symptoms:

Answer 20

activation of both muscarinic and nicotinic receptors

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

Question 21

Treatment of AChE poisoning (2)

Answer 21

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

Question 22

Bethanechol, carbachol, pilocarpine =

Use:

Answer 22

Muscarinic acetylcholine receptor agonist

Topical treatment of glaucoma

Question 23

Bethanechol =

Use:

Answer 23

Muscarinic acetylcholine receptor agonist

Urinary retention

Question 24

Atropine =

Uses:

Answer 24

Muscarinic acetylcholine receptor antagonist
Penetrates CNS, BBB

Severe bradycardia
AChE poisoning

Question 25

Tropicamide = Uses:

Answer 25

Muscarinic acetylcholine receptor antagonist Pupil dilation of ophthalmology

Question 26

Scopolamine = Uses:

Answer 26

Muscarinic acetylcholine receptor antagonist Motion sickness

Question 27

Glycopyrrolate = Uses:

Answer 27

Muscarinic acetylcholine receptor antagonist Dry secretions

Question 28

Benztropine, diphenhydramine = Uses:

Answer 28

Muscarinic acetylcholine receptor antagonists Parkinsonism

Question 29

Ipratropium, tiotropium = Uses:

Answer 29

Muscarinic acetylcholine receptor antagonist Asthma Chronic obstructive pulmonary disease

Question 30

Tolterodine, solifenacin = Uses:

Answer 30

Muscarinic acetylcholine receptor antagonists Bladder spasm Urinary incontinence

Question 31

Treatment of antimuscarinic overdose

Answer 31

Acetylcholinesterase inhibitors

Question 32

Adrenergic alpha1 receptor actions:

Answer 32

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

Question 33

Adrenergic alpha2 receptor actions:

Answer 33

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

Question 34

Adrenergic beta receptors actions:

Answer 34

1. Activate adenylyl cyclase | 2. Increase intracellular cAMP

Question 35

Adrenergic beta-1 receptors actions:

Answer 35

Mainly in heart --> increased heart rate and contractility | Juxtaglomerular cells --> increase renin secretion

Question 36

Adrenergic beta-2 receptors actions:

Answer 36

``` 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 ```

Question 37

Adrenergic beta-3 receptors actions:

Answer 37

Lipolysis of adipose tissue | Relaxation of urinary bladder

Question 38

Phenylephrine = Uses:

Answer 38

Alpha-1 agonist Nasal congestion Raise blood pressure

Question 39

Clonidine = Uses: Adverse effect:

Answer 39

Alpha-2 agonist Inhibitory effect on sympathetic NS (inhibit NE release) Hypertension Prone to rebound hypertension

Question 40

Prazosin = Use:

Answer 40

alpha1 specific antagonist hypertension

Question 41

Doxazosin = Use:

Answer 41

alpha1 specific antagonist hypertension

Question 42

Terazosin = Use:

Answer 42

alpha1 specific antagonist BPH

Question 43

Tamsulosin = Use:

Answer 43

alpha1 specific antagonist BPH

Question 44

All alpha-1 antagonists are capable of causing ____

Answer 44

orthostatic hypotension

Question 45

Phenoxybenzamine = Uses:

Answer 45

Non specific alpha antagonist IRREVERSIBLE Pheochromocytoma (adrenal medulla tumor): block effects of catecholamines released by tumors

Question 46

Phentolamine = Use:

Answer 46

Non specific alpha antagonist Pheochromocytoma (adrenal medulla tumor): block effects of catecholamines released by tumors

Question 47

Dobutamine = Uses:

Answer 47

Beta-1 agonist Cardiogenic shock Heart failure

Question 48

Albuterol = Use: Adverse effect:

Answer 48

Short acting Beta-2 agonist Acute asthma attacks Tachycardia

Question 49

Salmeterol, formoterol, bambuterol = Use:

Answer 49

Long acting selective Beta 2 agonist Chronic asthma therapy

Question 50

Terbutaline = Use:

Answer 50

Beta 2 agonist Prevents premature labor: relaxation of uterine smooth muscle

Question 51

Isoproterenol = Effect: Use:

Answer 51

Non selective beta-adrenergic agonist Lower PVR, increase heart rate, contractility Symptomatic bradycardia

Question 52

Mirabegron = Use:

Answer 52

Beta 3 agonist Overactive bladder

Question 53

Norepinephrine action: Use:

Answer 53

Potent: alpha1, 2, beta 1 receptors Little: beta 2 receptor Septic shock --> used to increase blood pressure

Question 54

Epinephrine = Use:

Answer 54

Potent agonist of both alpha and beta receptors Anaphylactic shock: Dilate bronchial smooth muscle and raise blood pressure

Question 55

Effects of epinephrine:

Answer 55

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

Question 56

Epinephrine + alpha-adrenergic antagonist =

Answer 56

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

Question 57

Adverse effects of beta-blocker

Answer 57

Bradycardia AV conduction block Hypotension Sexual dysfunction

Question 58

Non-selective beta-blockers should be avoided in:

Answer 58

1. Asthma patients b/c blocks B2 receptor --> bronchoconstriction 2. Diabetic patients b/c block glycogenolysis

Question 59

Selective Beta-1 antagonists

Answer 59

Atenolol Metoprolol Esmolol Nadolol

Question 60

Non-selective beta blockers

Answer 60

Propranolol | Timolol

Question 61

Drugs that block alpha1, beta 1 and 2 receptors

Answer 61

Carvedilol | Labetalol

Question 62

Esmolol = Use:

Answer 62

Selective Beta-1 antagonist Very short half life Cardiac arrhythmia

Question 63

Nadolol = Use:

Answer 63

Non-selective Beta antagonist Long half life Not lipophilic Cardiac arrhythmia

Question 64

Acebutolol, pindolol =

Answer 64

Beta blocker w/ weak partial agonist of beta receptors Cause less bradycardia

Question 65

Carvedilol = Use:

Answer 65

Beta blocker w/ alpha-adrenergic antagonist Heart failure Improves insulin sensitivity

Question 66

Labetalol = Use:

Answer 66

Beta blocker w/ alpha-adrenergic antagonist ISA+ Vasodilator in HTN --> won't slow down b/c heart rate not affected Hypertension in pregnancy Pheochromocytoma

Question 67

Amphetamines action: Uses:

Answer 67

Increase norepi release from nerve terminals Increase release of dopamine ADHD: Adderall Short-term weight loss Narcolepsy

Question 68

Cocaine action: Use: Metabolite:

Answer 68

Blocks norepi and dopamine reuptake Local anesthetic in ENT surgeries Benzoylecgonine

Question 69

Pindolol =

Answer 69

Nonselective Beta adrenergic antagonist Block beta receptor w/o slowing heart Lipophilic --> treat neuogenic syncopy --> low level beta stimulant Good in healthy people

Question 70

Nebivolol =

Answer 70

Selective beta1 adrenergic antagonist Pulmonary HTN Produce NO Heart works better: increased CO, SV, EF, LVEDV

Question 71

Beta-blockers: 1 of the only drugs to

Answer 71

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

Question 72

Verapamil = Use: Metabolism:

Answer 72

Potent AV nodal blockade Multifocal atrial tachycardia, idiopathic fascicular ventricular tachycardia Premature ventricular contraction Pulmonary friendly Work synergistic w/ beta blockers Liver

Question 73

Diltiazem = Metabolism:

Answer 73

AV nodal blockade Work synergistic w/ beta blockers Renal