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73 Cards in this Set

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What are the two major classes of cholinergic drugs?
chol agonists (cholinomemetics) and anti-cholinergic drugs (cholinergic antagonists)
Why is ACh so important?
It is the primary NT at the NMJ and it is also important in certain brain regions
Name two types of cholinergic agonists (stimulants)
direct acting and indirect acting
What are the types of direct acting cholinergic agonists?
muscarinic and nicotinic
What is the one type of indirect-acting drug that was mentioned in lecture?
neostignine- inhibits cholinesterase and makes sure more ACh binds to receptors
Why is it helpful if there is some specificity for direct acting cholinergic stimulants on muscarinic receptors?
muscarinic receptors are in the periphery and so that is where you want the drug to take action
Direct-acting cholinergic stimulants function similarly to what?
ACh
Name some cholinergic stimulant drugs
bethanechol (Duvoid)

Carbachol (Carbastat) and pilocarpine (pilocar)
What is the function of bethanechol (Duvoid)?
encourages urinary activity and can increase GI activity which is helpful for abdominal surgery
Does Bethanechol attach to nicotinic, muscarinic, or adrenergic receptors?
muscarinic
Carbachol and pilocarpine are used for what medical condition?
glaucoma, used topically
Is the function of indirect acting cholinergic stimulants to potentiate AChE or inhibit AChE?
inhibit AChE causing an increase in ACh in the synaptic cleft
T or F: Indirect acting agents have a higher specificity when compared to direct acting agents
F, relatively low
Name the two exceptions to the low specificty of indirect acting cholinergic stimulants?
neostigmine and tacrine
After surgery there is a lack of smooth muscle tone in the GI or bladder; what are possible uses for direct acting cholinergic stimulants?
increase bladder activity and peristalsis by increasing the parasympathetic activity
How does indirect cholinergic stimulants help treat Alzheimers disease?
In early AD decrease symptoms by prolonging release of endogenous ACh. Causes increase in memory, cognition and other cortical functions
Cholingergic stimulants are used for:
A. AD
B. GI/urinary bladder atonia
C. Glaucoma
D. Myasthenia Gravis
E. All of the above
E. All of the above
How do cholinergic stimulants help treat glaucoma?
increase outflow of aqeous humor thus lowering intraocular pressure
What types of cholinergic stimulants treat glaucoma?
indirect and direct
Myasthenia gravis is a dz that affects NMJ and is treated by immune suppresants and what type of chol stimulant?
indirect such as neostigmine can allow endogenous ACh to stay at the synaptic cleft longer
How do cholinergic stimulants help with myasthenia gravis?
cholinesterase inhibitors alleviate fatigue
How are cholinergic stimulants helpful in the reversal of overdose on anticholinergic drugs?
used to reverse delirium, hallucinations, coma (signs of overdose)
Neuromuscular blockers are used during surgery with general anesthesia, what type of cholinergic stimulants are used and how?
indirect may be used to speed up recovery after use of these drugs
What are the adverse effects of cholinergic stimulants?
GI distress, increase salivation, bronchoconstriction, bradycardia, difficulty with visual accomodation
What is the function of anticholinergic drugs?
block the receptor from ACh effects, diminishing response of tissue to ACh stimulation
Name the two types of anticholinergic drugs
antimuscarinic and antinicotinic
What do antinicotinic drugs treat?
HTN and neuromuscular block
What are antimuscarinic used for?
atropine, synthetic, semisynthetic forms lots of uses for these drugs
Identify the mechanism of action of antimuscarinic drugs and the specificity of these drugs
block postsynaptic cholinergic muscarinic receptor and it is not completely specific so they will affect multiple tissues
Name the applications for antimuscarinic drugs
decreases GI tract stimulation for those with peptic ulcers; Parkinsons, Cardiovascular, motion sickness
Side effects of anticholinergic drugs
dry mouth, blurred vision, urinary retention, constipation, tachycardia
What are the rehab considerations for someone with Alzheimer's or myasthenia gravis taking cholinergic agonists?
Schedule rehab at peak plasma concentration/effect
When should PT happen if a pt is taking muscarinic antagonists for spastic bladder or incontinence?
after they void or when they are not likely to void again which makes treatment more effective
What are the two major classes of adrenergic drugs? Also named what?
pharmacological agonists and antagonists; sympathomimetics and sympatholytics
How are adrenergic drugs classified?
according to mode of action not clinical application
Alpha 1 - name primary receptor location and response when stimulated
vascular smooth muscle, organs will have vasoconstriction
Alpha2 - primary receptor location and response when receptor is stimulated
CNS synapses (inhibitory); inhibit sympathetic signals and inhibit interneurons
Alpha1 - agonists uses and antagonists uses
Hypotension, nasal congestion, paroxysmal superventricular tachycardia; HTN
Alpha2- agonist uses
HTN and spasticity
Beta1 - primary receptor location and response when receptor is stimulated
heart, increase HR and contractility
Beta1 - agonist uses and antagonists uses
agonist- used to increase cardiac function/CO;
antagonist- HTN, arrhythmia, angina, heart failure, MI
Beta2- primary receptor location and response when receptor is stimulated
bronchioles; bronchodilation
Beta2 - agonists uses
prevent bronchospasm
Which receptor types have no antagonist uses?
Alpha 2 and beta2
Beta antagonists are also know as what?
Beta blockers
Adrenergic agonists are split into direct and indirect acting name the 3 types of direct acting receptor drugs
alpha agonists, beta agonists, mixed agonists
Name drug for a1 selective agonists
phenylephrine (Neo-Synephrine)
What are the adverse effects of phenylephrine (Neo-Synephrine)?
HTN, HA, reflex bradycardia
How does phenylephrine (neo-synephrine) cause reflex bradycardia?
internal feedback loops try to combat the increase in BP so it does this by increase HR and baroreceptor initiates a decrease in CO; net result is bradycardia
Identify two drugs that are classified as a2-selective agonists
tizanidine (Zanaflex) and clonidine (Duraclon) for HTN
What are the adverse effects of a2-adrenergic agonists?
dizziness, dry mouth, drowsiness with more serious effects being bradycardia, difficulty breathing
Identify drug that is classified as b1 selective agonist
dobutamine (Dobutrex)
How is dobutrex administered?
IV so plasma conc is constant
What are the indications for giving Dobutamine?
heart failure, treat shock
What are the adverse effects of Dobutrex?
arrhythmia
Name b2 selective agonist drug?
albuterol (Proventil)
What are the indications for administering Proventil?
asthma, bronchitis, emphysema
Adverse effects of albuterol?
nervousness, restlessness, trembling
Define the characteristics of alpha and beta mixed agonists
agonist activity at all adrenergic receptors, or act as indirect agonists with varied indications b/c affect a number of different subtypes
What are the adverse effects of alpha and beta mixed agonists?
excess CNS excitation, excess stimulation of CV system
Note: Any agonist at high enough concentration will affect what?
any alpha and beta receptor
What are two types of adrenergic antagonists?
alpha and beta blockers
Alpha blockers have non selective and a1 selective drug types, give an example of each
blocker/nonselective: phentolamine (Regitine)

a1 selective: prazosin
Beta blockers have non selective (antagonists) and b1 selective antagonists, give an example of each
antagonist: propanolol (Inderal)

b1 selective: metoprolol (lopressor
What are the adverse effects of phentolamine (regitine)
reflex tachycardia, OH
How is regitine administered?

a) IV
b) intramuscularly
c) orally
d) a and b
d)
What are the adverse effects of prazosin (minipress)?
reflex tachycardia, OH
Prazosin treats what and is given how?
HTN, given orally
What are adverse effects of propanolol (inderal)?
some bronchoconstriction and increased airway resistance; excess depression of cardiac function
Who should not take beta blockers?
COPD or asthmatic people
How are beta blockers or propanolol given?
orally or IV
what are the adverse effects of metoprolol (lopressor)?
excess depression of cardiac function
How is Lopressor administered?
orally or IV