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104 Cards in this Set

  • Front
  • Back
3 uses of cholinergic drugs
1. used in PNS
2. ACh primary neurotransmitter at NMJ
3. important for brain fcxn
2 major classes of cholinergic drugs
1. cholinergic agonists (stimulants, cholinomimetics)
2. cholinergic antagonists (anti-cholinergics or blockers)
2 kinds of cholinergic agonists (stimulants)?
1. direct acting agonists
2. indirect acting cholinergic agonists
What are direct acting cholinergic agonists?
Drugs that bind to cholinergic receptor to activate it (drugs like ACh)
What are indirect acting cholinergic agonists?
Drugs that inhibit cholinesterase (AChE) that breaks down ACh while in its synapse (indirectly allows more ACh around in synapse)
What is an example indirect cholinergic agonist drug?
Neostignine--indirect cholinergic or cholinesterase inhibitor drug that is helpful in protecting the diaphragm from paralysis initially
What are 3 true cholinergic agonist drugs that are ACh like?
1. bethanchol (Duvoid)
2. carbachol (Carbastat) and pilocarpine (Pilocar)
Why would it be helpful to have some specificity for a muscarinic receptor using cholinergic agonists?
Want to have a peripheral effect where there are more muscarinic receptors
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
What does carbachol (Carbastat) and pilocarpine (Pilocar) treat?

How are they used?
Glaucoma

Topically (lots of SE if used systemically)
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)
What are 6 applications for cholinergic agonists or stimulants?
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)
How does cholinergic agonists affect the gut and bladder? (2)
1. increases gut motility (decreases intestinal paralysis)
2. increase bladder activity if bladder distention
What are direct cholinergic agonists used to do with the autonomic system?
Increase PNS activity
What are 2 direct cholinergic agonist applications?
1. GI/urinary bladder atonia
2. Glaucoma
What are 5 indirect cholinergic agonist applications?
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
When and how are cholinergic agonists helpful for AD pts?
Helpful in early stages of AD when ACh is still present in synapse (indirectly prolongs ACh release)
When are cholinergic agonists not helpful for AD pts?
In later stages of AD when pt no longer produces ACh
What is glaucoma? What happens if goes untreated?
Increased intraocular pressure

Can cause blindness and impaired vision
How do cholinergic agonists treat glaucoma?
Increases aqueous humor outflow to decrease pressure
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
What happens to the cholinergic receptors within a MG pt?
Decrease in # of functional cholinergic receptors at end-organ (NMJ)
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
What are MG pts given when their condition is long term?
Immunosuppressants to react to autoimmune response
What are NM blockers used for?
Used in surgery with general anesthesia
Why are reversal of NM blockers (indirect cholinergic agonist) used?
May be used to speed up recovery after use of NM blockers during surgery
What 3 things can overdose of anticholinergic drugs cause?
1. delirium
2. hallucinations
3. coma
What drugs may be used to reverse the effects of an overdose of anticholinergic drugs (delirium, hallucinations and coma)?
Indirect cholinergic stimulants or agonists (lots of SE in CNS due to non-specificity)
What are 2 adverse effects of cholinergic agonists or stimulants?
1. many SE due to non-specificity
2. mimics exaggerated PNS activity
What are 5 exaggerated PNS adverse effects from using cholinergic agonists or stimulants?
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)
How do anticholinergic or cholinergic antagonist drugs function?
Function by blocking the receptor from ACh effects and diminish ACh stimulation to tissues
Are anticholinergic or cholinergic antagonists competitive or non-competitive?
Competitive, they bind and then release from the receptor
What are 2 types of anticholinergic or cholinergic antagonist drugs?
1. anti-nicotinic
2. anti-muscarinic
What are 2 uses for anti-nicotinic drugs?
1. HTN (emergent use)
2. neuromuscular blockers during surgery
What is a prototypical anti-muscarinic drug?
Atropine which makes the eyes dilate
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
What are anti-muscarinic drugs used for? (5)
1. GI disorders (IBS, ulcers)
2. Parkinson's (overactive central cholinergic synapses)
3. CV
4. Motion sickness
5. Decrease bladder tone
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
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!
What are 3 rehab considerations for taking cholinergic drugs?
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
What do adrenergic drugs influence?
SNS
What are 2 major classes of adrenergic drugs?
1. pharmacological agonists
2. pharmacological antagonists
What are adrenergic drugs also called (agonists and antagonists)?
Sympathomimetics (agonists)
Sympatholytics (antagonists)
How are adrenergic drugs categorized?
According to their mode of action or receptors, not by clinical application
What is the primary location for alpha 1 receptors?
Vascular smooth muscle
Response when alpha 1 receptors are stimulated?
Vasoconstricts organs
Use of alpha 1 agonist drug? (3)
1. hypotension
2. nasal congestion
3. types of increased HRs
--paroxysmal
--superventricular
--tachycardia
Use of alpha 1 antagonist drug?
HTN
Primary location for alpha 2 receptors?
CNS symptoms (inhibitory)
Response when alpha 2 receptors are stimulated? (3)
1. inhibit sympathetic signals
2. inhibit interneurons
3. decrease motor excitability
Use of alpha 2 agonist drugs? (2)
1. HTN
2. spasticity
Use of alpha 2 antagonist drugs?
n/a
Primary location of beta 1 receptors?
Heart
Response when beta 1 receptors are stimulated? (2)
1. Increase HR
2. Increase contractility
Use of beta 1 agonist drugs?
Increase cardio fcxn and output
Use of beta 1 antagonists? (5)
1. HTN
2. arrhythmia
3. angina
4. heart failure
5. MI
Primary location of beta 2 receptors?
Bronchioles
Response when beta 2 receptors are stimulated?
Dilation of airways
Use of beta 2 agonist (bronchodilators) drugs?
Prevent bronchospasms
Use of beta 2 antagonists?
n/a
What 3 types of adrenergic receptors can treat HTN?
1. alpha 1 antagonist (smooth muscles)
2. alpha 2 agonist (inhibits CNS sympathetic)
3. beta 1 antagonist (heart)
What are 2 mixed adrenergic agonists?
1. ephedrine
2. epinephrine
How does ephedrine (mixed adrenergic agonist) work and when is it used?
Works on both alpha and betas indirectly

Used for emergent hypotension or as a bronchodilator
How does epinephrine (mixed adrenergic agonist) work?
Works directly on all 4 receptors (alphas and betas)
What type of drug is Phenylephrine (neo-synephrine)?

What is it used for?
Alpha 1 selective agonist

Used for hypotension to vasoconstrict and decongestant
Name an example drug of an alpha 1 selective agonist
Phenylephrine (neo-synephrine) to vasoconstrict and decongestant
What are 3 adverse effects of alpha 1 selective agonist drugs?
1. HTN
2. HA
3. Reflex bradycardia
How does reflex bradycardia occur with using an alpha 1 selective agonist drug?
Drug will increase BP, barorecptors will initiate decrease in HR and cardiac output in response to drug
What are 2 alpha 2 selective agonist drugs and what are they used for?
1. Clonidine (Duraction) for HTN and anxiety
2. Tizanidine (Zanaflex) for spasticity
What does Clonidine (Duraction) do? What does it treat?
Alpha 2 selective agonist that treats HTN and anxiety
What is tizanidine (Zanaflex) and what does it treat?
Alpha 2 selective agonist that treats spasticity
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
What is an example beta 1 selective agonist?

2 indications to use it in treatment?
Dobutamine (Dobutrex)

1. treat shock
2. heart failure
What is an adverse effect of beta 1 selective agonist?
Arrhythmia
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
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
What are 3 adverse effects of beta 2 selective agonists?
1. nervousness
2. restlessness
3. trembling
What is Albuterol (Proventil) and what is it used for?
Beta 2 selective agonist used to treat asthma, bronchitis and emphysema (bronchodilator)
What are 3 adverse effects of Albuterol (Proventil)?
1. nervousness
2. restlessness
3. trembling
What is an adverse effect of using Dobutamine (Dobutrex)?
Arrhythmia
What are 3 adverse effects of using Clonidine (Duraction) and/or Tizanidine (Zanaflex)?
1. dizziness
2. drowsiness
3. dry mouth

(3 serious effects if toxic--breathing difficulty, bradycardia, synscope)
What are 3 adverse effects of using Phenylephrine (neo-synephrine)?
1. HTN
2. HA
3. reflex bradycardia
What are mixed alpha and beta adrenergic agonists?
Drug with agonist activity at all adrenergic receoptors or act as indirect agonists
What are 6 varied indications for mixed alpha and beta agonist?
1. ADD
2. Narcolepsy
3. Hypotension
4. Asthma (inhalers)
5. Anaphylactic shock
6. Anesthesia
What are 2 adverse effects of mixed alpha and beta adrenergic agonists?
1. excess CNS excitation
2. excess stimulation of CV system (HTN, arrhythmias and cardiac arrests)
What can mixed alpha and beta adrenergic agonists do in reference to their receptors?
Any agonist will affect any alpha and beta receptor (SE!)
What do adrenergic antagonists usually end in?
-olol
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
When is Phentolamine (Regitine) an alpha blocker (antagonist) used?
For a surgery when a tumor is secreting too much epinephrine or norepinephrine
What are 2 adverse effects of using Phentolamine (Regitine) an alpha blocker?
1. reflex tachycardia
2. OH
What are 2 adverse effects of using an alpha antagonist?
1. reflex tachycardia
2. OH
How does reflex tachycardia occur when using Phentolamine (Regitine) an alpha blocker?
Drug decreases BP and BR respond with increasing HR and CO
What is an example drug that is an alpha 1 selective antagonist or blocker?
Prazosin (Minipress)
What is Prazosin (Minipress) and what does it treat?
Alpha 1 blocker or antagonist

Treats HTN
What are 2 adverse effects of using Prazosin (Minipress) an alpha 1 blocker?
1. reflex tachycardia
2. OH
What is an example of a beta blocker (antagonist) that is non-selective?
Propranolol (Inderal)
What is Propranolol (Inderal) and what is it used for?
Beta blocker (antagonists) that is non-selective

Treats HTN and angina
What are 2 adverse effects to taking Propranolol (Inderal)?
1. some bronchoconstriction and increased airway resistance
2. excess depression of cardiac function
What are 2 adverse effects to taking a non-selective beta blocker?
1. some bronchoconstriction and increased airway resistance
2. excess depression of cardiac function
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
What is an example drug of a beta 1 selective antagonist or blocker?
Metoprolol (Lopressor)
What is Metoprolol (Lopressor) and what is it used for?
Beta 1 selective blocker or antagonist (caridoselective)

Used for HTN and angina
What is an adverse effect when taking Metoprolol (Lopressor)?
Excess depression of cardiac function
What is an adverse effect when taking a beta 1 selective blocker?
Excess depression of cardiac function