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104 Cards in this Set
- Front
- Back
3 uses of cholinergic drugs
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1. used in PNS
2. ACh primary neurotransmitter at NMJ 3. important for brain fcxn |
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2 major classes of cholinergic drugs
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1. cholinergic agonists (stimulants, cholinomimetics)
2. cholinergic antagonists (anti-cholinergics or blockers) |
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2 kinds of cholinergic agonists (stimulants)?
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1. direct acting agonists
2. indirect acting cholinergic agonists |
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What are direct acting cholinergic agonists?
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Drugs that bind to cholinergic receptor to activate it (drugs like ACh)
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What are indirect acting cholinergic agonists?
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Drugs that inhibit cholinesterase (AChE) that breaks down ACh while in its synapse (indirectly allows more ACh around in synapse)
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What is an example indirect cholinergic agonist drug?
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Neostignine--indirect cholinergic or cholinesterase inhibitor drug that is helpful in protecting the diaphragm from paralysis initially
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What are 3 true cholinergic agonist drugs that are ACh like?
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1. bethanchol (Duvoid)
2. carbachol (Carbastat) and pilocarpine (Pilocar) |
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Why would it be helpful to have some specificity for a muscarinic receptor using cholinergic agonists?
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Want to have a peripheral effect where there are more muscarinic receptors
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What does bethanechol (Duvoid) do?
When is it good to use? |
Encourages urine activity and increased GI activity
Use after abdominal surgery Cholinergic agonist drug |
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What does carbachol (Carbastat) and pilocarpine (Pilocar) treat?
How are they used? |
Glaucoma
Topically (lots of SE if used systemically) |
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Which are more specific, indirect or direct cholinergic agonists?
What are 2 drugs that are the exception to this rule? |
Direct cholinergic agonists
1. neostigmine (affects muscarinic) 2. tacrine/donepezil (affects brain) |
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What are 6 applications for cholinergic agonists or stimulants?
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1. GI/urinary atonia (increases gut motility and bladder activity if distention)
2. Alzheimer's 3) Myasthenia Gravis 4) Glaucoma 5) Reversal of NM blockers 6) Reversal of anticholinergic effects (CNS toxicity) |
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How does cholinergic agonists affect the gut and bladder? (2)
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1. increases gut motility (decreases intestinal paralysis)
2. increase bladder activity if bladder distention |
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What are direct cholinergic agonists used to do with the autonomic system?
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Increase PNS activity
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What are 2 direct cholinergic agonist applications?
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1. GI/urinary bladder atonia
2. Glaucoma |
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What are 5 indirect cholinergic agonist applications?
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1. Alzheimer's
2. Myasthenia Gravis 3. Glaucoma (can be either direct or indirect) 4. Reversal of NM blockers 5. Reversal of anticholinergic induced CNS toxicity |
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When and how are cholinergic agonists helpful for AD pts?
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Helpful in early stages of AD when ACh is still present in synapse (indirectly prolongs ACh release)
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When are cholinergic agonists not helpful for AD pts?
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In later stages of AD when pt no longer produces ACh
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What is glaucoma? What happens if goes untreated?
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Increased intraocular pressure
Can cause blindness and impaired vision |
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How do cholinergic agonists treat glaucoma?
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Increases aqueous humor outflow to decrease pressure
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What direct cholinergic stimulants or agonists are 1 type of drug used to treat glaucoma?
How are they given? |
Carbachol (Carbastat) and Pilocarpine (Pilocar)
given topically |
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What happens to the cholinergic receptors within a MG pt?
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Decrease in # of functional cholinergic receptors at end-organ (NMJ)
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What are MG pts given initially to treat and what does it alleviate?
Name an example drug name |
Indirect cholinergic agonists or cholinesterase inhibitors to alleviate fatigue and allow ACh to remain in cleft longer (also protects diaphragm from paralysis)
Neostigmine as an example |
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What are MG pts given when their condition is long term?
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Immunosuppressants to react to autoimmune response
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What are NM blockers used for?
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Used in surgery with general anesthesia
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Why are reversal of NM blockers (indirect cholinergic agonist) used?
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May be used to speed up recovery after use of NM blockers during surgery
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What 3 things can overdose of anticholinergic drugs cause?
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1. delirium
2. hallucinations 3. coma |
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What drugs may be used to reverse the effects of an overdose of anticholinergic drugs (delirium, hallucinations and coma)?
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Indirect cholinergic stimulants or agonists (lots of SE in CNS due to non-specificity)
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What are 2 adverse effects of cholinergic agonists or stimulants?
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1. many SE due to non-specificity
2. mimics exaggerated PNS activity |
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What are 5 exaggerated PNS adverse effects from using cholinergic agonists or stimulants?
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1. GI distress (cramping, nausea, vomiting, diarrhea)
2. increased salivation (could choke) 3. bronchoconstriction 4. bradycardia 5. difficulty with visual accommodation (High PNS activity symptoms) |
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How do anticholinergic or cholinergic antagonist drugs function?
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Function by blocking the receptor from ACh effects and diminish ACh stimulation to tissues
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Are anticholinergic or cholinergic antagonists competitive or non-competitive?
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Competitive, they bind and then release from the receptor
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What are 2 types of anticholinergic or cholinergic antagonist drugs?
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1. anti-nicotinic
2. anti-muscarinic |
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What are 2 uses for anti-nicotinic drugs?
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1. HTN (emergent use)
2. neuromuscular blockers during surgery |
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What is a prototypical anti-muscarinic drug?
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Atropine which makes the eyes dilate
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What is the mechanism of antimuscarinic drugs?
Are they specific? Why? |
Blocks postsynaptic cholinergic muscarinic receptors
Not specific! All of these drugs will antagonize cholinergic receptors on multiple tissues |
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What are anti-muscarinic drugs used for? (5)
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1. GI disorders (IBS, ulcers)
2. Parkinson's (overactive central cholinergic synapses) 3. CV 4. Motion sickness 5. Decrease bladder tone |
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What are anti-muscarinic drugs primarily used for?
What are their effects? |
Adjunct treatment for GI disorders like IBS and ulcers
Decrease GI tract stimulation and secretions |
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If given systemically, what are 5 most common side effects of anti-muscarinics (anticholinergics)?
What do they all have in common? |
1. dry mouth
2. blurred vision 3. urinary retention 4. constipation 5. tachycardia All sympathetic responses, too much of a decrease in PNS! |
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What are 3 rehab considerations for taking cholinergic drugs?
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1. If pt is taking cholinergic agonists for Alzheimer's or MG, schedule pt therapy at peak time effect
2. If pt is taking muscarinic antagonist for spastic bladder or incontinence, schedule pt after voiding and at peak effect 3. If nicotine use, a pt can experience SNS or PNS responses depending on comorbidities |
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What do adrenergic drugs influence?
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SNS
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What are 2 major classes of adrenergic drugs?
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1. pharmacological agonists
2. pharmacological antagonists |
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What are adrenergic drugs also called (agonists and antagonists)?
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Sympathomimetics (agonists)
Sympatholytics (antagonists) |
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How are adrenergic drugs categorized?
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According to their mode of action or receptors, not by clinical application
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What is the primary location for alpha 1 receptors?
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Vascular smooth muscle
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Response when alpha 1 receptors are stimulated?
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Vasoconstricts organs
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Use of alpha 1 agonist drug? (3)
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1. hypotension
2. nasal congestion 3. types of increased HRs --paroxysmal --superventricular --tachycardia |
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Use of alpha 1 antagonist drug?
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HTN
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Primary location for alpha 2 receptors?
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CNS symptoms (inhibitory)
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Response when alpha 2 receptors are stimulated? (3)
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1. inhibit sympathetic signals
2. inhibit interneurons 3. decrease motor excitability |
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Use of alpha 2 agonist drugs? (2)
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1. HTN
2. spasticity |
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Use of alpha 2 antagonist drugs?
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n/a
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Primary location of beta 1 receptors?
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Heart
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Response when beta 1 receptors are stimulated? (2)
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1. Increase HR
2. Increase contractility |
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Use of beta 1 agonist drugs?
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Increase cardio fcxn and output
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Use of beta 1 antagonists? (5)
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1. HTN
2. arrhythmia 3. angina 4. heart failure 5. MI |
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Primary location of beta 2 receptors?
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Bronchioles
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Response when beta 2 receptors are stimulated?
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Dilation of airways
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Use of beta 2 agonist (bronchodilators) drugs?
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Prevent bronchospasms
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Use of beta 2 antagonists?
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n/a
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What 3 types of adrenergic receptors can treat HTN?
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1. alpha 1 antagonist (smooth muscles)
2. alpha 2 agonist (inhibits CNS sympathetic) 3. beta 1 antagonist (heart) |
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What are 2 mixed adrenergic agonists?
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1. ephedrine
2. epinephrine |
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How does ephedrine (mixed adrenergic agonist) work and when is it used?
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Works on both alpha and betas indirectly
Used for emergent hypotension or as a bronchodilator |
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How does epinephrine (mixed adrenergic agonist) work?
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Works directly on all 4 receptors (alphas and betas)
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What type of drug is Phenylephrine (neo-synephrine)?
What is it used for? |
Alpha 1 selective agonist
Used for hypotension to vasoconstrict and decongestant |
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Name an example drug of an alpha 1 selective agonist
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Phenylephrine (neo-synephrine) to vasoconstrict and decongestant
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What are 3 adverse effects of alpha 1 selective agonist drugs?
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1. HTN
2. HA 3. Reflex bradycardia |
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How does reflex bradycardia occur with using an alpha 1 selective agonist drug?
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Drug will increase BP, barorecptors will initiate decrease in HR and cardiac output in response to drug
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What are 2 alpha 2 selective agonist drugs and what are they used for?
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1. Clonidine (Duraction) for HTN and anxiety
2. Tizanidine (Zanaflex) for spasticity |
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What does Clonidine (Duraction) do? What does it treat?
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Alpha 2 selective agonist that treats HTN and anxiety
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What is tizanidine (Zanaflex) and what does it treat?
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Alpha 2 selective agonist that treats spasticity
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What are 3 adverse effects of alpha 2 selective agonists?
3 more serious effects due to toxicity? |
1. dizziness
2. drowsiness 3. dry mouth more serious effects due to toxicity: 1. difficulty breathing 2. bradycardia 3. synscope |
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What is an example beta 1 selective agonist?
2 indications to use it in treatment? |
Dobutamine (Dobutrex)
1. treat shock 2. heart failure |
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What is an adverse effect of beta 1 selective agonist?
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Arrhythmia
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What is Dobutamine (Dobutrex) and what is it used for?
Treats for? |
Beta 1 selective agonist to increase heart function/output
Treats heart failure and shock |
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What is an example drug of a beta 2 selective agonist?
What is it used for? (3) |
Albuterol (Proventil)
1. treat asthma 2. bronchitis 3. emphysema |
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What are 3 adverse effects of beta 2 selective agonists?
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1. nervousness
2. restlessness 3. trembling |
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What is Albuterol (Proventil) and what is it used for?
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Beta 2 selective agonist used to treat asthma, bronchitis and emphysema (bronchodilator)
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What are 3 adverse effects of Albuterol (Proventil)?
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1. nervousness
2. restlessness 3. trembling |
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What is an adverse effect of using Dobutamine (Dobutrex)?
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Arrhythmia
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What are 3 adverse effects of using Clonidine (Duraction) and/or Tizanidine (Zanaflex)?
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1. dizziness
2. drowsiness 3. dry mouth (3 serious effects if toxic--breathing difficulty, bradycardia, synscope) |
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What are 3 adverse effects of using Phenylephrine (neo-synephrine)?
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1. HTN
2. HA 3. reflex bradycardia |
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What are mixed alpha and beta adrenergic agonists?
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Drug with agonist activity at all adrenergic receoptors or act as indirect agonists
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What are 6 varied indications for mixed alpha and beta agonist?
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1. ADD
2. Narcolepsy 3. Hypotension 4. Asthma (inhalers) 5. Anaphylactic shock 6. Anesthesia |
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What are 2 adverse effects of mixed alpha and beta adrenergic agonists?
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1. excess CNS excitation
2. excess stimulation of CV system (HTN, arrhythmias and cardiac arrests) |
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What can mixed alpha and beta adrenergic agonists do in reference to their receptors?
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Any agonist will affect any alpha and beta receptor (SE!)
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What do adrenergic antagonists usually end in?
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-olol
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What drug is an example of an alpha blocker or antagonist that is non-selective?
How is it given? |
Phentolamine (Regitine)
Given IV or IM |
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When is Phentolamine (Regitine) an alpha blocker (antagonist) used?
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For a surgery when a tumor is secreting too much epinephrine or norepinephrine
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What are 2 adverse effects of using Phentolamine (Regitine) an alpha blocker?
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1. reflex tachycardia
2. OH |
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What are 2 adverse effects of using an alpha antagonist?
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1. reflex tachycardia
2. OH |
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How does reflex tachycardia occur when using Phentolamine (Regitine) an alpha blocker?
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Drug decreases BP and BR respond with increasing HR and CO
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What is an example drug that is an alpha 1 selective antagonist or blocker?
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Prazosin (Minipress)
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What is Prazosin (Minipress) and what does it treat?
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Alpha 1 blocker or antagonist
Treats HTN |
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What are 2 adverse effects of using Prazosin (Minipress) an alpha 1 blocker?
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1. reflex tachycardia
2. OH |
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What is an example of a beta blocker (antagonist) that is non-selective?
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Propranolol (Inderal)
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What is Propranolol (Inderal) and what is it used for?
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Beta blocker (antagonists) that is non-selective
Treats HTN and angina |
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What are 2 adverse effects to taking Propranolol (Inderal)?
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1. some bronchoconstriction and increased airway resistance
2. excess depression of cardiac function |
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What are 2 adverse effects to taking a non-selective beta blocker?
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1. some bronchoconstriction and increased airway resistance
2. excess depression of cardiac function |
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What type of pt should not take Propranolol (Inderal) when treating HTN? Why?
What should they take? |
Asthmatic or COPD pt b/c not selective to beta 2 receptors
Should take beta 1 selective antagonist or blocker |
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What is an example drug of a beta 1 selective antagonist or blocker?
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Metoprolol (Lopressor)
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What is Metoprolol (Lopressor) and what is it used for?
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Beta 1 selective blocker or antagonist (caridoselective)
Used for HTN and angina |
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What is an adverse effect when taking Metoprolol (Lopressor)?
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Excess depression of cardiac function
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What is an adverse effect when taking a beta 1 selective blocker?
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Excess depression of cardiac function
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