Pt 713: Ans Drugs, Cholinergic And Adrenergic Drugs

Front 1

What system are cholinergic drugs used in? What is the primary neurotransmitter at the NMJ?

Back 1

parasympathetic system

- ACh

Front 2

What regions of the body is ACh important in?

Back 2

certain brain regions

Front 3

What are 2 major classes of cholinergic drugs?

Back 3

1. agnoists/stimulants/cholinomimetics

2. blockers

Front 4

What does a direct cholinergic agonist/stimulant do?

Back 4

binds directly to the receptor and activate it

Front 5

What does an indirect cholinergic agonist/stimulant do?

Back 5

inhibits cholinesterase (breaks down ACh in synapse so there is increased ACh in synapse to bind)

Front 6

What are 2 examples of direct acting cholinergic agonist/stimulants?

Back 6

1. muscarinic
2. nicotinic

Front 7

What are true cholinergic agonists?

Back 7

direct acting cholinergic stimulants

- they function similiarly to ACh

Front 8

Why is it helpful if there is some specificity for muscarinic receptors?

Back 8

want to affect the meriphery more and this is where muscarinic receptors are located

Front 9

What are specific examples of true cholinergic (direct) agonists?

Back 9

Bethanechol (Duvoid) -- encourages urinary activity and is helpful after GI surgery for GI activity

Carbachol (Carbastat) and pilocarpine (Pilocar)

Front 10

What is the mechanism of action for direct cholinergic stimulants?

Back 10

1. bind to a receptor (either muscarinic or nicotinic)
2. acts like ACh

Front 11

What is the function of indirect acting cholinergic stimulants? What is the function of AChE?

Back 11

inhibit acetylcholinesterase enzyme (AChE)

- AChE normally breaks down ACh in synaptic cleft

Front 12

Which has more specificity, direct or indirect cholinergic agents?

Back 12

indirect acting agents have relatively low specificity when compared to direct acting agents

Front 13

What are some expections to the "indirect have less specificity than direct cholinergic agents" rule of thumb?

Back 13

-neostigmine affects muscarinic

-Tacrine/donepezil have more effects in the brain

**none effect only one tissue, side effects in other places where these mechanisms exist

Front 14

What is the mechanism of action for indirect cholinergic stimulants?

Back 14

it binds with the cholinesterase enzyme to inhibit the break down of ACh in the synaptic cleft

** if this doesn't work then there is more ACh in the cleft

Front 15

How do cholinergic stimulants affect GI/urinary bladder atonia?

Back 15

(lack of smooth muscle tone that occurs after surgery or other trauma to the organs)

- decreased intestinal peristalsis (to allow peristalsis to occur), increase GI motility

- bladder distension (increase bladder activity)

Front 16

What usually affects smooth muscle contraction of the GI/urinary bladder?

Back 16

parasympathetic activity causes smooth muscle contraction

** DIRECT cholinergic agonists are used to increase parasympathetic activity

Front 17

How are Cholinergic stimulants used with Alzheimer's disease?

Back 17

- indirect cholinergic stimulants may decrease some symptoms in early AD

- affects cholinergic neurons important for memory, cognition, and other cortical functions

- indirect, drug treatment prolongs release of endogenous ACh, it does not help once neurons cannot release ACh

Front 18

When are cholinergic stimulants used with Alzheimer's disease?

Back 18

used early when there is still some Ach being released at the synapse (no additonal ACh added so not helpful when there is no ACh at receptor later)

Front 19

What is glaucoma? What happens if it is left untreated?

Back 19

defined by an increase in intraocular pressure

can lead to impaired vision/blindness

Front 20

What does the treatment do for glaucoma?

Back 20

treatment increases the outflow of aqueous humor, thus lowering the pressure

- direct cholinergic stimulants are one drug type used to treat the condition topically

Front 21

What is myasthenia gravis?

Back 21

disease affects skeletal NMJ

- number of functional cholinergic receptors at end-organ is decreased
- autoimmune response

Front 22

How do cholinesterase inhibitors work to help treat Myasthenia gravis?

Back 22

- may help alleviate fatigue
- indirect cholinergic agonists (neostigmine)
- allow endogenous ACh to remain in synaptic cleft longer

Front 23

When are reversal of neuromuscular blockades used?

Back 23

- NM blockers often are used during surgery with general anesthesia

- indirect cholinergic stimulants may be used to speed up recovery after use of these drugs

Front 24

What is the reversal of anticholinergic-induced CNS toxicity?

Back 24

- overdose of anticholinergic drug can cause delirium, hallucinations, or coma

- indirect cholingeric stimulants may be used to reverse these effects

Front 25

What are adverse effects of cholinergic stimulants caused by?

Back 25

- due to relative nonspecificity
- both types of drugs' adverse effects mimic exaggerated parasympathetic activity

Front 26

What are adverse effects of cholinergic stimulants?

Back 26

- GI distress (N/V, diarrhea, abdominal cramping)
- increased salivation
- bronchoconstriction
- bradycardia
- difficulty with visual accomodation

Front 27

What are ganglion blockers used for (anticholinergic drugs)?

Back 27

emergent HTN

Front 28

What are NM blockers used for (anticholinergic drugs)?

Back 28

used with surgery and general anesthesia

Front 29

What is the function of anticholinergic drugs?

What are the 2 types?

Back 29

block the receptor from ACh effects, diminishing response of tissue to ACh stimulation

1. antinicotinic
2. antimuscarinic

Front 30

Are anticholinergic drugs competative or noncompetative?

Back 30

usually competative antagonists of the receptor

Front 31

What are 2 functions of antinicotinic drugs?

Back 31

1. NM blocker with surgery
2. HTN

Front 32

What are 2 characteristics of antimuscarinic (anticholinergic) drugs?

HINT: what is the prototypical drug, what are the 3 forms?

Back 32

1. prototypical = atropine
2. synthetic, semisynthetic, and natural forms as well

Front 33

What are 2 functions of anticholinergic drugs?

Back 33

- peptic ulcers (decrease acid secretions)
- IBS

used for overactive GI

Front 34

What are side effects of anticholinergic drugs?

Back 34

decreased bladder tone, dilate eyes

Front 35

What is the mechanism of antimuscarinic drugs?

Back 35

block synaptic cholinergic muscarinic receptors

- some preferentially affect some tissues, some others, d/t different muscarinic receptor subtypes

** not completely specific (all drugs will antagonize cholinergic receptors on multiple tissues)

Front 36

What is the primary use for antimuscarinic drugs?

Back 36

adjuct treatment for GI disorders (decrease GI tract stimulation)

Front 37

What are additional uses for antimuscarinic drugs?

Back 37

- Parkinson's to treat overactivity of central cholinergic synapses

- CV
- motion sickness

Front 38

What are side effects of anticholinergic drugs? (5)

Back 38

if given systemically multiple side effects are possible

- dry mouth
- blurred vision
- urinary retention
- constipation
- tachycardia

Front 39

What are rehab considerations for anticholinergic drugs?

Back 39

Alzheimer's or myasthenia gravis: schedule PT at peak effect time

spastic bladder or incontience: after voiding, during the peak effect

nicotine use (smoking, dipping): depends on comorbities, various sympathetics or parasympathetic responses

Front 40

What are adren, mimics, lytics?

Back 40

- adren -- influence activity in SNS
- mimics -- agonist
- lytics -- antagonist

Front 41

What are the 2 major classes of adrenergic drugs?

Back 41

1. pharmacological agonists
2. pharmacological antagonists

Front 42

What are the other names for adrenergic drugs?

Back 42

sympathomimetics and sympatholytics

** drugs are categorized by their mode of action, not clinical application

Front 43

What is:
1. primary receptor location, 2. response when receptor is stimulated
3. agnoist use(s)
4. anatgonist use(s)

for alpha 1

Back 43

1. vascular smooth muscle
2. organ vasoconstriction (depends on where)
3. hypotension, nasal congestion, paroxysmal superventricular tachycardia
4. HTN

Front 44

What is:
1. primary receptor location, 2. response when receptor is stimulated
3. agnoist use(s)
4. anatgonist use(s)

for alpha 2?What is:
1. primary receptor location, 2. response when receptor is stimulated
3. agnoist use(s)
4. anatgonist use(s)

for alpha 2?

Back 44

1. CNS synapses (inhibitory)
2. inhibits sympathetic signals, inhibits internueorns, decreases motor neuron excitability
3. HTN, spasticity
4. n/a

Front 45

What is:
1. primary receptor location, 2. response when receptor is stimulated
3. agnoist use(s)
4. anatgonist use(s)

for Beta 1?

Back 45

1. heart
2. increased HR, increased force of contractility
3. used to increase cardiac function/CO
4. HTN, arrhythmia, angina, heart failure, MI (beta blockers)

Front 46

What is:
1. primary receptor location, 2. response when receptor is stimulated
3. agnoist use(s)
4. anatgonist use(s)

for Beta 2?

Back 46

1. bronchioles
2. bronchodilation (too small of bronchioles), decreased uterine contractions (old use, many effects)
3. prevent bronchospasm
4. n/a

Front 47

What is ephedrine? What is it used for and in what situations?

Back 47

alpha and beta agonist and indirect agonist used for severe/emergent hypotension or as a bronchodilator

Front 48

What is epinephrine and what receptors does it effect?

Back 48

endogenously produced, direct to all 4 receptors (mixed agonist)

Front 49

What are B2 selective adrenergic agonist used for?

Back 49

bronchodilation with heart problem

Front 50

What do Beta 1 selective adrenergic agonists do?

Back 50

increase the work of the heart

Front 51

What are examples of alpha 1 selective agonists?

Back 51

phenylephrine (neo-synephrine)

Front 52

What are adverse effects of alpha 1 selective agonists?

Back 52

HTN, HA, reflux bradycardia

Front 53

How does reflex bradycardia happen with alpha 1 selective antgonists?

Back 53

internal feedback loops try to control the increase in BP, increased HR baroreceptor initiates a decrease in CO, the baroreflex will then decrease HR.

net result = bradycardia

Front 54

What are examples of alpha 2 selective agonists and what are they used for?

Back 54

clonidine (Duraclon): for HTN (central acting)

tizanidine (Zanaflex): for spasticity

Front 55

What are adverse effects of alpha 2 selective agonists?

Back 55

dizziness, drowsiness, dry mouth

- more serious effects (difficulty breathing, bradycardia, syncopy ) lkely due to toxicity

Front 56

What are examples of beta 1 selective agonists? What are indications for use?

Back 56

dobutamine (Dobutrex)

treat shock, heart failure

Front 57

What are adverse reactions for beta 1 selective agonists?

Back 57

arrhythmia

** increase the work of the heart

Front 58

What are examples of beta 2 selecive agonists? What are indications for use?

Back 58

albuterol (Proventil)

treat asthma, bronchitis, emphysema

Front 59

What are adverse effects of beta 2 selective agonists?

Back 59

nervousness, restlessness, trembling

** patients with bronchodilation with heart problem

Front 60

What are mixed alpha and beta agonists?

Back 60

drugs with agonist activity at all adrenergic receptors, or act as indirect agonsists

Front 61

What are indications for using mixed alpha and beta agonists?

Back 61

it can affect a number of different subtypes

- ADD
- narcolepsy
- hypotension
- asthma (inhalers)
- anaphylactic shock
- anesthesis

Front 62

What are adverse effects of using mixed alpha and beta agonists?

Back 62

- excess CNS excitement
- excess stimulation of CV system

Front 63

What are mixed alpha and beta agonists used for?

Back 63

treating HTN, arrhythmias

any agonist at high enough concetnration will act as mixed (epinephrine and ephedrine)

Front 64

What do beta blockers end in?

Back 64

tend to end in -olol

- decreased heart rate
- decreased force of contraction

Front 65

What are examples of alpha antagonists? How are they administered?

Back 65

phentolamine (Regitine)

IV or IM (specifically when tumor is secreting too much EP)

**nonspecific

Front 66

What are adverse effects of alpha antagonists?

Back 66

reflex tachycardia, OH
(decreased BP, baroreflex initiates increased BP by increasing the HR)

Front 67

What are examples of alpha 1 selective antagonists?

Back 67

prazosin (Minipress)

Front 68

What are adverse effects of alpha 1 selective antagonists?

Back 68

reflex tachycardia, OH

Front 69

What are examples of beta antagonists?

Back 69

propanolol (Inderal)

Front 70

What are adverse effects of beta antagonists?

Back 70

- bronchoconstriction and increased airway resistance
- excess depression of cardiac function

** asthmatic or COPD should not take this drug

Front 71

What are examples of beta 1 selective antagonists?

Back 71

metoprolol (Lopressor)

** cardioselective

Front 72

What are adverse effects of beta 1 selective antagonists?

Back 72

excess depression of cardiac functions