Autonomic Pharmacology 1 Flashcards by Scott Stauffer

What is the major nuerotransmitter for the parasympathetic nervous system?

Acetylcholine

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What are the major neurotransmitters for the sympathetic nervous system?

Acetylcholine & Norepinephrine

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How can drugs modify ANS activity?

Synthesis
Storage
Release
Receptor interaction
Disposition

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What are the 4 drugs that alter the autonomic nervous system?

Parasympathetic (PANS) stimulatory
Parasympathetic (PANS) inhibitory (blocking)
Sympathetic (SANS) stimulatory
Sympathetic (SANS) inhibitory (blocking)

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What is a drug that acts at the location where acetylcholine is released termed?

Cholinergic

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What is a drug that acts at the location where norepinephrine is released termed?

Adrenergic

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Drugs that act at the location where the PANS acts has the prefix?

Parasympatho…

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A drug that acts at the location where the SANS acts has the prefix?

Sympatho…

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Drugs that acta at the location where a division of the ANS acts and produces the same effect as the neurotransmitter has the suffix?

…mimetic

“Mimics” neurotransmitters - aka agonist drug

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Drugs that act at the location where a division of the ANS acts and blocks the action of the neurotransmitter has the suffix?

-lytic or -blocker

aka antagonist drugs

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What are the parasympathetic PANS drugs?

Stimulatory
- cholinergics
- parasympathomimetics
Inhibitory
- anticholinergics
- parasympatholytics
- cholinergic blockers

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What are the sympathetic SANS drugs?

Stimulatory
- adrenergics
- sympathomimetics
Inhibitory
- adrenergic blockers
- sympathetic blockers
- sympatholytics

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What are the 2 types of cholinergic agonists?

Direct acting
- agonists
Indirect acting
- cholinesterase inhibitors - causes accumulation of ACH = stimulating PANS

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Why do we use direct acting cholinergic drugs?

Longer duration of action
More selective in the effects produced
Stimulate the PANS

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In order to be an effective mediator, ACH must do what?

Fit both physically and chemically at the receptor

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What are the pharmacologic effects of cholinergic drugs (sympathetic effects)?

Cardiovascular
- bradycardia, decreased BP and CO
Eye
- Miosis, lowers intraocular pressure
GI
- Increase in activity, motility and secretion

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What are the primary indications for use of cholinergic drugs?

Glaucoma
Myasthenia gravis (autoimmune disorder)
GI disorders
Reverse urinary retention after surgery

What are some examples of direct acting cholinergic agonists?

cevimeline (Evoxac) - Sjogren’s syndrome
**pilocarpine (Salagen) - glaucoma, Sjogren’s **
acetylcholine (MIochol) - eye surgery
bethanechol (Urecholine) - urinary retention
carbachol (Miostat) - glaucoma

What does pilocarpine (Salagen) used for, do?

Used in eye for treatment of glaucoma
Causes pupil constriction, allows for drainage of fluid from eye
Decreases intraocular pressure
Stimulate salivary secretions in patients with xerostomia

What do indirect-acting cholinergic drugs do?

Stop the breakdown of acetylcholine - build up of acetylcholine = same results/effects of cholinergics

Produce PANS stimulation

What are the primary indications for indirect-acting cholinergic agonists (choilnesterase inhibitors)?

Myasthenia gravis
Glaucoma
Postoperatice urinary retention
Paralytic ileus
Antidotes to agents that produce nondepolarizing neuromuscular blockade (poisons)

How are indirect-acting cholinergic drugs divided?

Into groups based on degree of reversibility with which they are bound to the enyme
- Reversible (includes centrally-acting drugs)
- Irreversible

What are reversible indirect-acting cholinergic drugs used to treat and how do they do it?

Myasthenia gravis and glaucoma, and dementia with Alzheimer’s disease
Cause skeletal muscle activation followed by blockade = no muscle contraction

What are the examples of reversible indirect-acting cholinergic drugs?

edrophonium (Enlon)
physostigmine - reverses toxic life-threatening delirium caused by overdoses of anticholinergic drugs (like Benadryl)
pyridostigmine (Mestinon)

What is an example of a reversible indirect-acting cholinergic drug that is used to treat dementia with Alzheimers?

donepezil (Aricept)

What do irreversible acetylcholinesterase inhibitors do?

Raise Acetylcholine = too much POISONS!!

What are used as insecticides (organophosphates) and nerve gases \*sarin, Soman, tabun" for chemical warfare?

Irreversible Acetylcholinesterase Inhibitors

If poisoned (overdose) with insecticides or organophophates, what do you use?

* **pralidoxime (2-PAM, Protopam)** - regenerates the irreversibly bound ACH receptor sites that are bound by the inhibitors * **atropine (antimuscarinic)** - competitively blocks muscarinic effects of excess ACH

What are the side effects of cholinergic drugs?

SLUD * Salivation * Lacrimation * Urination * Defecation All mimics the parasympathetic nervous system

What are the cholinergic antagonists?

Anticholinergics = antimuscarinics Nueromuscular blocking agnets Ganglionic blocking agents

What do anticholinergic drugs (parasympatholytics) do?

* Prevent action of ACT at postganglionic PANS nerve endings * Blocker drugs or **antagonists** * **Block the receptor site for acetylcholine** * AKA **antimuscarinic drugs **

With anticholinergic drugs - acetylcholine cannot act on receptors where?

In smooth muscle, glands or the heart

What are the major pharmacologic effects of anticholinergic drugs (reduce PANS)?

* CNS = effects determined by dose * Sedation, motion sickness (scopolamine) * Stimulation, delirium, hallucinations, coma (atropine in high doses) * Exocrine glands * Dries up secretions * Used in dentistry to decrease salivation and create dry field for bonded restorations and impressions (atropine) * Smooth Muscle * Bronchodilators * GI tract * Decrease gut motility * Eye * Mydriasis, cycloplegia, drops used for opthalmologic examination -GRRR

What are the clinical uses of anticholinergic drugs?

* Preoperative medications - stops salivation, blocks slowing of heart rate caused by general anesthesia * GI disorders - that produce excess secretion and increased gut motility, stops excess acid secretion, stops diarrhea & cramping * Eye Exam - pupil dilation * Parkinson's disease - Reduces tremors * GU disorders - overactive bladder

How are anticholinergic drugs used in dentistry?

Atropine - to maintain a dry field

What do atropine and pilocarpine do?

* atropine - anticholinergic - dries saliva * pilocarpine - cholinergic - salivation

What is scopolamine and opratropium (Atrovent) used for?

* scopolamine - patch used for motion sickness * ipratropium (Atrovent) - emphysema = stops bronchial secretion

What are the contraindications to anticholinergic drugs?

* **Glaucoma** - cause an acute rise in intraocular pressure * **Prostatic** **hypertrophy** - cause urinary retention, may need catheterization * **Intestinal or urinary obstruction or retention** - slow GI motility and cause urinary retention * **Cardiovascular disease** - drugs can block the vagus nerve, tachycardia can result

What are the adverse reactions to anticholinergic drugs?

Extensions of their pharmacologic effects - too much of what they typically do..

What are the side effects for atropine toxicity?

* Dry as a bone (lack of sweating) * Red as a beet (flushed skin) * Blind as a bat (blurred vision, mydriasis, cycloplegia) * Mad as a hatter (delirium, hallucinations)