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