Lodge 2

Question 1

Drugs: Prazosin, terazosin, doxazosin, tamsulosin, and alfuzosin

Answer 1

Alpha blockers

Question 2

Responses to Alpha blockers

Answer 2

Vasodilation (blood vessels of the skin, viscera, mucous membranes)

Question 3

Uses for Alpha blockers

Answer 3

• Hypertension

* Benign Prostatic Hyperplasia (enlarged prostate)

Question 4

a1 Adrenergic Antagonists – Hypertension

Answer 4

a1-adrenergic antagonists relax smooth

muscle and decrease TPR.

Question 5

a1 Adrenergic Antagonists – BPH

Answer 5

•Tamsulosin(Flomax): a1-adrenergic antagonists relax smooth muscle in the prostate and bladder neck decreasing the degree of blockage of urine flow (treat symptoms).
• Side effects:
- dizziness when standing (due to vasodilation).
- inhibits ejaculation or causes retrograde ejaculation

Question 6

Side effects of directly-acting antagonists: the alpha blockers

Answer 6

• Orthostatic hypotension
• Tachycardia
• Vertigo
• Sexual dysfunction

Question 7

Uses for B blockers

Answer 7

tx of hypertension, ischemic heart disease, congestive heart failure, and certain arrhythmias

Question 8

Uses for Propranolol – prototypic non selective b Blocker

Answer 8

• Hypertension
• Migraine
• Hyperthyroidism
• Angina pectoris
• Myocardial infarction

Question 9

Side effects of directly-acting antagonists: propranolol – prototypic non selective b Blocker

Answer 9

• Fatigue
• Bronchoconstriction
• Sexual dysfunction
• Arrhythmias

Question 10

Acetylcholine is released from parasympathetic postganglionic neurons as well as ALL _______ neurons

Answer 10

preganglionic & somatic

Question 11

Acetylcholine Synthesis occurs in nerve terminal and ______ is the rate limiting step.

Answer 11

Choline uptake

Question 12

Acetylcholine Inactivation

Answer 12

• Hydrolyzed by acetylcholinesterase (AChE) in the synaptic cleft to form choline
• Recycled
• Terminated by pseudocholinesterase, widely distributed throughout the plasma

Question 13

• Atony of the bladder
• Atony of the GI tract
• Myasthenia gravis (↓ muscle tone) - Intoxication by Ach antagonists
• Glaucoma
• Alzheimer’s Disease

Answer 13

Therapeutic uses of AChE inhibitors

Question 14

Reversible AChE Inhibitors include…

Answer 14

• Physostigmine

- Neostigmine

Question 15

AChE Inhibitors can be used to treat _______ by increasing synaptic ACh.

Answer 15

Myasthenia Gravis

Question 16

______ is a nicotinic agonist that is NOT degraded by Acetyl cholinesterase

Answer 16

Suxamethonium

Question 17

______ (short duration AChE inhibitor) used to distinguish between “myasthenic” and “cholinergic” crisis in patients

Answer 17

Edrophonium

Question 18

AChE Inhibitors can be used to treat _____ by restoring loss of function and not altering progression of the disease.

Answer 18

Alzheimer’s Disease

Question 19

Tacrine, donepezil, rivastigmine, and galantamine

Answer 19

AChE inhibitors

Question 20

Cholinergic Receptors:

• agonist
• as many as 12 sub-types
• ligand-activated cation channels

Answer 20

Nicotinic

Question 21

Cholinergic Receptors:

• agonist
• 5 sub-types
• G-protein coupled (7-TM)

Answer 21

Muscaranic

Question 22

_______ are the principle cholinergic receptor in skeletal muscle and autonomic ganglia (BOTH sympathetic and parasympathetic) and are ligand-gated cation channels

Answer 22

Nicotinic receptors

Question 23

Full agonist at Nicotinic Receptors and has both central and peripheral effects

Answer 23

Nicotine

Question 24

• CNS stimulant 
- Arousal
- Increases mental performance
• Rewarding (activates DA system)
• Addictive

Answer 24

Nicotine Effects (central)

Question 25

- Sympathomimetic (Increase BP and Heart Rate) | - Nicotine stimulates nicotinic receptors on adrenal medulla leading to epinephrine release

Answer 25

Nicotine Effects (periphery)

Question 26

– A partial agonist at central a4b2-nicotinic receptor | – Possesses 50% of the intrinsic activity of nicotine – Prevents the binding of nicotine

Answer 26

varenicline (Chantix)

Question 27

______ are the principle cholinergic receptor at autonomic ganglia (BOTH sympathetic and parasympathetic)

Answer 27

Nicotinic receptors

Question 28

Because ganglonic antagonists block ______ function, the effect of these drugs depends upon the dominant tone in the organ system.

Answer 28

BOTH parasympathetic and sympathetic

Question 29

Nicotinic Receptor Drugs: no longer of use for regulating autonomic functions (non specific)

Answer 29

NN (Ganglion)

Question 30

Nicotinic Receptor Drugs: effects at muscles useful for paralysis during surgery

Answer 30

NM (NMJ)

Question 31

Nicotinic Receptor Drugs: Smoking cessation, also promising advances with SELECTIVE ligands (i.e. Analgesia, Alzheimer's, schizophrenia)

Answer 31

NN (Brain)

Question 32

Muscarinic receptors are localized to ________.

Answer 32

parasympathetic effectors

Question 33

________ are the principle cholinergic receptor in smooth muscle, cardiac muscle and glands.

Answer 33

Muscarinic receptors

Question 34

Muscarinic Agonist examples

Answer 34

- Bethanechol (non-selective) - Cevimeline (M3) - Atropine (non-selective) - Ipratropium/tiotropium (M)

Question 35

Use of Cevimeline

Answer 35

* Muscarinic agonist (mainly M3) * Parasympathetic stimulation increases salivation * Used in dentistry to treat severe Xerostomia (dry mouth)

Question 36

Side effects of Cevimeline

Answer 36

sweating, urination, stuffy nose, lacrimation, and abdominal pain

Question 37

Use of Atropine

Answer 37

Decrease respiratory secretions as an adjunct for anesthesia

Question 38

Effects of Atropine

Answer 38

* **Secretion **– Potently inhibits glandular secretion –particularly salivation (can be used in dental setting) * Eye – Persistent mydriasis (dilation) lasts 7-14 days * GI – Can be used as anti-spasmodic to reduce GI motility. * Urinary – reduce hyper-motility states of the urinary bladder, occasionally used in children. * Cardiovascular – Bimodal. Low doses inhibit presynaptic M1 receptors and increase Ach leading to bradycardia. High doses block M2 in SA node and increases heart rate.

Question 39

Use and effects of Ipratropium/ tiotropium

Answer 39

* Used as second-line therapy for asthma (first line Albuterol– b agonist) * Therapeutic effects are specific due to inhalational application

Question 40

_________ (i.e. Cevimeline) will stimulate salivation, however due to their side effects, muscarinic agonists are not widely used to treat this condition as there are satisfactory masticatory stimulants and artificial saliva products available OTC.

Answer 40

Muscarinic agonists

Question 41

Patients taking parasympathomimetics (e.g., post-operative GI problems or glaucoma) should never be treated with _______ to reduce the flow of saliva.

Answer 41

anti-cholinergic drugs