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What are the 2 main classes of cholinoceptor-blocking agents (anticholinergics)
1) Anti-nicotinic - block transmission w/in sympathetic & parasympathetic ganglia

2) antimuscarinic - block transmission between the parasympathetic postgnaglionic fiber and the target organ, e.g., salivary glands, heart, GI tract, etc.
What is an antimuscarinic agent?
Muscarinic receptor blocker
What is the prototype antimuscarinic agent?
Atropine, aka hyoscyamine
How does atropine block muscarinic receptors?
Atropine cause reversible, competitive blockade of muscarinic receptors
What can overcome atropine?
Atropine can be overcome by a greater concentration of acetylcholine (Ach) or equivalent muscarinic agonist
Does atropine affect nicotinic cholinergic receptors (NN) of the autonomic ganglia?
No, atropine has little effect.
Does atropine distinguish among the M1, M2, or M3 muscarinic receptor subtypes?
No, atropine does not distinguish among the M1, M2, or M3 muscarinic receptor subtypes.
Name 2 semisynthetic tertiary ammonium analogues of atropine.
1) dicyclomine (Bentyl)

2) tropicamide (Mydriacil)
What are 3 types of drugs that have side effects similar to antimuscarinics/ anticholinergics?
1) antihistamines

2) tricyclic antidepressants (TCA)

3) antipsychotics
What are the side effects of antimuscarinics?
- dry mouth
- blurred vision
- constipation
Name 2 antihistamines that have side anticholinergic effects.
1) dimenhydrinate (Dramamine)

2) diphenhydramine (Benadryl)
Name a tricyclic antidepressants (TCA) that has anticholinergic side effects.
amitriptyline (Elavil)
Name 2 antipsychotics that have anticholinergic side effects.
1) haloperidol (Haldol)

2) chlorpromazine (Thorazine)
What is mydriasis?
reflex pupil dilation
Why are antimuscarinic drugs called 1) mydriatics or 2) cycloplegics?
Because they 1) dilate the pupils and they 2) paralyze the ciliary body which normally affects visual focus.
Name 3 antimuscarinic drugs used for the fundoscopic exam.
1) tropicamide (Mydriacil)

2) cyclopentolate (Cyclogil)

3) atropine sulfate (Isopto Atropine)
Are antimuscarinic drugs used as primary or adjunct treatment of IBS and/or peptic ulcers?

Histamine H2 receoptor blockers and acid (proton) pump inhibitors are primary now.
Why are quatenary antimuscarinic drugs preferred for IBS and/or peptic ulcer.
Quatenary compounds don't cross the blood-brain barrier so you avoid CNS side effects.

You still may have peripheral side effects (dry mouth, etc.)
Name a quatenary antimuscarinic drug.
glycopyrrolate (Robinul)
Name 3 tertiary antimuscarinic drugs used for IBS and/or peptic ulcer:
1) dicyclomine (Bentyl)

2) hyoscyamine (Levsin)

3) clidinium + chlordiazepoxide (Librax)
How are GERD and peptic ulcer disease related?
Gastric acid is the injurious agent.
What drugs block gastric secretion of gastric acid?
H2 blockers or proton pump inhibitors.
What is GERD?
GERD is gastroesophageal reflux disease. Normal or excessive gastric acid refluxes past a faulty lower esophageal sphincter into the lower (or upper) esophagus and causes burning pain (heartburn).
What is peptic ulcer disease?
The gastric mucosal barrier is faulty, and even normal levels of gastric acid erode the gastric musculature.
Are H2 blockers or proton pump inhibitors classified as anticholinergics?
No. H2 blockers or proton pump inhibitors are NOT classified as anticholinergics.
What is a common drug for traveler's diarrhea and other mild GI tract hypermotility?
atropine + diphenoxylate (opiod) -- Lomotil
What is loperamide used for?
Loperamide is an antidiarrhea drug. It is an opioid. It does NOT contain an antimuscarinic.
Before prescribing Lomotil or Imodium, what disease should you rule out?
Clostridium difficile (C. diff) colitis.
How does C. diff injure the colon?
It releases Toxins A & B.
What does a colonoscopy reveal in a patient with C. diff colitis?
White or yellow plaques adhering to the colonic mucosa.
How are white or yellow plaques adhering to the colonic mucosa diagnosed (what disease)?
Membranous colitis.
How do you definitively diagnose C. diff. colitis?
Lab assay of stool for C. diff. toxins.
How does C. diff usually take over?
A wide spectrum antibiotic kills off most of the commensal bacteria in the colon, allowing C. diff to take over.
What are the 2 drugs of choice for C. diff. colitis?
1) metronidazole (Flagyl)

2) vancomycin (Vancocin)
What 2 drugs are recommended for overactive bladder and urge incontinence?
1) oxybutynin (Ditropan)

2) tolterodine (Detrol LA)
Why were antimuscarinics used in conjunction w/irritant anesthetics such as ether for surgical anesthesia?
Antimuscarinics such as atropine and scopolamine prevented bronchial secretions and laryngospasm.
What side effects did antimuscarinics cause when used w/ether for surgical anesthesia?
Intestinal hypomotility and urinary retention.
What drugs have replaced ether and atropine for surgical anesthesia?
Halothane, enflurane, and isoflurane.
How do antimuscarinics help for asthma and COPD?
Antimuscarinics permit bronchodilation and facilitate breathing (parasympathetic muscarinic activity causes bronchoconstriction).
Why are inhaled antimuscarinics used instead of other forms?
Inhalants provide local delivery and limit systemic antimuscarinic side effects.
Name 3 antimuscarinic inhalant bronchodilators.
1) ipratropium (Atrovent)

2) tiotropium (Spiriva)

3) ipratropium + albuterol (Combivent)
What is the drug of choice today for Parkinson's disease?
Why are antimuscarinics used as adjunctive therapy (in addition to levodopa)?
There is no single drug effective in Parkinson's disease.
What is the primary problem in Parkinson's disease?
Loss of dopaminergic neurons in the substantia nigra which leads to loss of dopaminergic output from the substantia nigra to the globus pallidus
What is the secondary transmitter problem in Parkinson's disease resulting from the imbalance of dopamine, i.e., why are antimuscarinics used as adjuncts?
An overbalance of cholinergic muscarinic activity from the globus pallidus back to the substantia nigra and elsewhere.
Name 3 antimuscarinic adjuncts used for Parkinson's disease?
1) benztropine (Cogentin)

2) trihexyphenidyl (Artane)

3) diphenhydramine (Benadryl inj.)
What are 3 antimuscarinics are used for motion sickness?
1) scopolamine (Transderm Scop)

2) dimenhydrinate (Dramamine)

3) meclizine (Antivert)
How are drugs labeled if they prevent nausea and vomiting?
Antiemetics because they prevent emesis.
Why do severe cholinergic excesses (poisonings) tend to occur in rural communities?
Insectisides are used, and wild poisonous mushrooms may be eaten by mistake.
Why is a tertiary, not quaternary, drug used for poisoning caused by a cholinomimetic agent?
The therapy must treat the effects in both the peripheral and central nervous systems, and quaternary drugs cannot cross the blood-brain barrier.
What 2 systems comprise the autonomic nervous system?
Sympathetic and parasympathetic systems.
What is another name for the sympathetic nervous system?
Craniosacral system
What is another name for the parasympathetic nervous system?
Throacolumbar system
Are the sympathetic and parasympathetic systems mainly sensory or motor?
The sympathetic and parasympathetic systems are mainly motor systems.
What does the ANS control (3 things)?
1) glandular secretions
2) smooth muscle (vascular and GI)
3) heart muscle
What carries pain from the chest and abdomen?
Sympathetic pain afferents.
Is ANS control mostly voluntary or involuntary?
ANS control is mostly involuntary.
What is the one sensation the ANS sends to one's consciousness?
What is the physiologic term for housekeeping?
What system is responsible for homeostasis of the body's internal environment?
The ANS, autonomic nervous system.
What controls the homeostatic functions of the following:

-pupil size & focal length
- salivation
- GI tract motility (peristalsis)
- digestion secretions
- cardiovascular (HR, contractile and constrictive tone of vesse
The autonomic nervous system
Is parasympathetic or sympathetic function more local? More widespread?
Parasympathetic is more local.

Sympathetic is more widespread.
Is parasympathetic or sympathetic related to "fight or fright"?

"Rest and digest"?
Sympathetic is "fight or fright"

Parasympathetic is "rest and digest"
What is called the "head ganglion"?
The hypothalamus
What is the peripheral nervous system (PNS)?
The PNS is the neuronal mass outside the brain and spinal cord.
Which cranial nerves are in the CranioSacral system?
3 - oculomotor
7 - facial
9 - glossopharyngeal
10 - vagus nerve
Which sacral spinal nerves are involved in the CranioSacral system?
S2 through S4
Are parasympathetic fibers found in the CranioSacral or ThoracoLumbar system?

Sympathetic fibers?
Parasympathetic fibers in CranioSacral

Sympathetic fibers in ThoracoLumbar
Which thoracic and lumbar spinal nerves are involved in the ThoracoLumbar system?
T1 through L2
Do parasympathetic fibers have long or short preganglionic fibers?

Postganglionic fibers?
parasympathetic fibers have long pre-ganglionic fibers and short post-ganglionic fibers.
Do sympathetic fibers have long or short preganglionic fibers?

Sympathetic fibers have short pre-ganglionic fibers and long post-ganglionic fibers.
Parasympathetic preganglionic neurotransmission involves which neurotransmitter and receptor?
Ach released on nicotinic receptors. NN.
Parasympathetic postganglionic neurotransmission involves which neurotransmitter and receptor?
Ach released onto muscarinic receptors. M2 or M3
Which preganglionic fibers go all the way to the target organ?
Parasympathetic preganglionic fibers.
Sympathetic preganglionic neurotransmission involves which neurotransmitter and receptor?
Ach released onto nicotinic receptors. NN.
Sympathetic postganglionic neurotransmission involves which neurotransmitter and receptor?
NE (norepinephrine) released onto adrenergic receptors:

alpha 1
alpha 2
beta 1
beta 2
What is another name for the sympathetic chain ganglia?
Paravertebral ganglia
What is another name for collateral ganglia?
Prevertebral ganglia
Where are the sympathetic chain (paravertebral) ganglia found?
Close to both sides of the vertebral column.
Where are the collateral (prevertebral) ganglia found?
Farther peripherally than the sympathetic chain ganglia.
Why is sweating different from other sympathetic functions?
Ach is the postganglionic neurotransmitter at the target organ instead of NE
What is the term for the fibers that control sweating?
Sympathetic cholinergic sudomotor fibers
What is an example of a disease that causes local loss of sweating (anhidrosis)?
Horner's syndrome
What are motor neurons going to skeletal muscle (voluntary) called?
Alpha motor neurons
How do motor neurons reach muscle fibers?
They exit the spinal cord and go directly to muscle fiber w/o going thru ganglia.
What neurotransmitter and receptors are involved with alpha motor neurons?
Ach released onto nicotinic receptors in the motor endplate on muscle fibers.
What spinal nerve serves as path from midbrain to pupillary constrictor & ciliary muscles?
CN3 - oculomotor nerve
What spinal nerve serves as path from pons to lacrimal gland and to submandibular & sublingual glands?
CN7 - facial nerve
What spinal nerve serves as path from medulla to parotid gland?
CN9 - glossopharyngeal
What is the path of sympathetic fibers that activate the pupillary dilator muscle and the vasomotor and sudomotor fibers of the head?
Superior cervical ganglia following the internal carotid artery.
What is the path of sympathetic fibers that activate the vasomotor, sudomotor, and pilomotor fibers of the arm?
Sympathetic fibers exit frojm cord segments T2 thru T6, ascend to the stellate ganglia and middle cervical ganglia, and then go thru the brachial plexus
Do sympathetic or parasympathetic nerves go to the body wall and limbs?
Only sympathetic nerves go to the body wall and limbs.
What is the path of sympathetic nerves to vasomotor, sudomotor, and pilomotor fibers of the lower body wall, legs, and feet?
Fused lower lumbar & sacral chain ganglia (T12 - L3) thru lumbosacral plexus, then travel w/ other peripheral nerves and vessels
What spinal nerve serves as path from medulla to heart, lungs, upper viscera, and abdominal viscera?
CN 10 - vagus nerve
What cord segments and what nerves are involved in activating the distal colon, bladder, genitals, rectum, and anus?
S2, S3, S4 thru pelvic splanchnic nerves
What is the path of sympathetic nerves to the heart?
T1 - T4 -> superior cervical ganglioin -> heart
What is the path of sympathetic nerves to the abdominal viscera?
T5 - T12 ->

thoracic splanchnic nerves ->

synapse in celiac and superior mesenteric collateral ganglia around abdominal aorta ->

follow arteries to abdominal viscera
What is the path of sympathetic nerves to the pelvic viscera?
T12 - L2 ->

lumbar spanchnic nerves ->

synapse in inferior mesenteric ganglion and
hypogastric/pelvic plexi ->

follow arteries to pelvic viscera
What is Auerbach's myenteric plexus
autonomic nerve fibers and ganglia located in the muscle tissue of the intestinal tract
What is the name of the nervous system w/in the walls of the GI tract?
The enteric nervous system
What is the path of the enteric nervous system?
Auerbach's myenteric plexus ->

GI motility and Meissner's submucosal plexus ->

What is the relation between symp and parasymp nerves and the enteric nervous system?
Symp and parasymp nerves synapses with and modulates the enteric nervous system
What is Horner's syndrome?
Horner's syndrome is paresis of sympathetic fibers to the head resulting in miosis, anhydrosis, and ptosis
What are 2 synonyms for cholinomimetics
1) parasymapthomimetics

2) cholinoceptor activating drugs
What effect does Ach have on skeletal muscle fiber at the end of an alpha-motor neuron?
Ach always causes muscle contraction.
What effect do direct-acting cholinomimetics have?
Direct-acting cholinomimetics agonize cholinergic receptors.
What effect does acetylcholinesterase have on Ach?
Acetylcholinesterase degrades Ach in the synaptic cleft and at the neuromuscular junction. Thus, it stops neurotransmission.
What happens to neurotransmission if acetylcholinesterase is inhibited?
Neurotransmission will be enhanced.
What do you call (2 names) a drug that antagonizes acetylcholinesterase?
1) cholinesterase inhibitor

2) anticholinesterase
What are indirect-acting cholinomimetics?
Indirect-acting agents produce their primary effects by inhibiting acetylcholinesterase. They increase the endogenous acetylcholine concentration in synaptic clefts and
neuroeffector junctions, and the excess acetylcholine in turn stimulates cholinoceptors
to evoke increased responses. These drugs act primarily where acetylcholine is
physiologically released and are amplifiers of endogenous acetylcholine.
Are nerve agents (organophosphate poisons) direct or indirect-acting cholinomimetics?
How do nerve agents cause death?
They cause cholinergically driven convulsions.
Where are 3 (receptor) places a drug can agonize cholinergic receptors w/ direct-acting cholinomimetics?
1) nicotinic cholinergic (NN) receptors of the postganglionic cell body

2) muscarinic cholinergic (M2 or M3) receptors on the parasympathetic target organ

3) nicotinic cholinergic (NM) receptors on the skeletal muscle fiber
What 2 effects does Ach have when released at parasympathetic synapses?
1) causes the preganglionic AP (action potential) to be transmitted into the postgang fiber

2) causes transmission of the postganglionic AP into the target organ
Name 3 choline esters that are direct-acting cholinomimetics.
1) Ach (Miochol)

2) bethanechol (Urecholine)

3) carbachol (Miostat)

4) methacholine
What cholinomimetic is used to test for allergic asthma?
What kind of cholinomimetics (direct, indirect-acting) are muscarine, pilocarpine (Pilocar), and nicotine?
What are the 2 main types of glaucoma?
1) acute narrow angle glaucoma

2) chronic open angle glaucoma
What produces the aqueous humor that fills the posterior and anterior chambers of the eye?
The ciliary body
How does the aqueous humor exit the eye?
It is absorbed by a network of trabeculae at the angle formed where the back of the cornea meets the front-peripheral edge of the iris. The trabeculae lead to a conjunctival vein, the canal of Schlemm (aka sinus venosus sclerae) which drains the humor into the conjunctival venous blood.
What causes a "narrow angle" between the back of the cornea and the front-peripheral edge of the iris?
The iris bulging forward.
How can you check for a "narrow angle" in the eye?
Shine a penlight from the lateral side of the eye across the front. If the iris is bulging, it will cast a shadow on the medial side.
What does "narrow angle" do to the pressure in the eye?
It causes a buildup of pressure in the eye.
What happens to the iris when the the pupil dilates, and what is the effect on narrow angle?
The iris contracts and gets fatter and compresses the narrow angle even further.
What % of people older than 35 yo have a narrow angle?
Approx. 1%
What are some causes of significant pupil dilation?
- dark places (movies)
- stress
- eye exam
- pre-op atropine
- antidepressants
- nebulized bronchodilators (beta 2 agonists
How does stress cause the pupil to dilate?
Increase epinephrine secretion and sympathetic tone
Name 2 mydriatic (pupil dilator) drugs used in eye exams.
1) tropicamide (Mydriacyl)

2) cyclopentolate (Cyclogyl)
What are the symptoms felt after hours of pupil dilation?
- acute eye pain
- blurred vision (halos)
- nausea, abdominal pain
- conjunctivitis
- steamy cornea
- pupil unreactive to light
- possible permanent vision loss w/in 2-5 days
How soon should acute narrow angle glaucoma be treated?
Immediately. It is considered a medical emergency.
What is(are) the first step(s) in treating acute narrow angle glaucoma?
Decrease pressure by re-constricting the pupil and re-opening the angle
What 3 types of drugs are used to treat acute narrow angle glaucoma (at the same time)?
1) muscarinic agonist
2) anticholinesterase
both of these cause ciliary muscle contraction, which stretches the trabeculae and enhances drainage

3) carbonic anhydrase inhibitor - to decrease fluid production
What are 2 muscarinic agonists that can be used to treat acute narrow angle glaucoma?
1) pilocarpine (Pilocar) drops

2) carbachol (Isopto-carbachol) drops
What are 3 anticholinesterase drugs that can be used to treat acute narrow angle glaucoma?
1) physostigmine opthalmic ointment

2) echothiophate (Phospholine) drops

3) demecarium (Humorsol) drops)
What is the surgical treatment for acute narrow angle glaucoma, and is it temporary or permanent?
Laser peripheral iridotomy (surgical procedure that makes an incision in the iris of the eye)

It is a permanent treatment.
What are 2 other names for chronic open angle glaucoma?
1) simple glaucoma

2) wide angle glaucoma
What causes the fluid buildup/pressure of chronic open angle glaucoma?
Inadequate trabecular drainage
What is the primary cause of chronic open angle glaucoma?
Unknown. Idiopathic. May be familial or related to diabetes.
Chronic open angle glaucoma may be secondary to what conditions?
- uveitis (inflammation of any of the structures of the uvea, including the iris, ciliary body or choroid)

- trauma

- steroid therapy
What surgeries might help with chronic open angle glaucoma?
- trabeculoplasty (a laser procedure that opens up the drainage angle)

- trabeculotomy (a piece of tissue in the eye's drainage angle is removed to create an opening)
For which glaucoma - open angle chronic or narrow angle - is longterm drug treatment needed?
For open angle chronic glaucoma, simple glaucoma
Are cholinomimetics major or minor players in the treatment of wide angle glaucoma, and how do they help?
Cholinomimetics are minor players. They enhance drainage by causing ciliary muscle contraction, which stretches the trabeculae
What are 2 types (w/examples) of cholinomimetic drugs used to treat simple glaucoma?
1) muscarinic agonists: pilocarpine and carbachol

2) anticholinesterase: physostigmine
How do carbonic anhydrase inhibitors help in simple glaucoma?
They decrease aqueous humor production. They inhibit carbonic anhydrase. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases
aqueous humor secretion by slowing the formation of bicarbonate ions.
Name 2 carbonic anhydrase inhibitors that are used to treat simple glaucoma.
1) acetazolamide (Diamox)

2) brinzolamide (Azopt)
How do prostaglandins help in simple glaucoma?
Prostaglandins increase drainage.
What are 2 prostaglandins used in the treatment of wide angle glaucoma?
1) bimatroprost (Lumigan)

2) unoprostone (Rescula)
How do non-selective alpha agonists help with wide angle glaucoma?

Name 2
They increase drainage.

2)dipivefrin (Propine)
How do alpha-2 agonists help with wide angle glaucoma?

Name 2:
They decrease aqueous humor production:

1) aproclonidine (Iopidine)
2) brimonidine (Alphagan)
How do beta blockers help with wide angle glaucoma?

Name 2:
They decrease aqueous humor production:

1) betaxolol (Betoptic)
2) timolol (Timoptic, Betimol)
What is a post-operative ileus?
A post-operative ileus is an atony or paralysis of the stomach or bowel that occurs after intestinal surgery.
What are 3 conditions in which the GI or UT smooth muscle activity is depressed (no obstruction) and in which cholinomimetics may be used for treatment?
1) post-operative ileus
2) urinary retention
after spinal cord injury
3) reflux esophagitis (GERD)
inadequate esophageal sphincter tone
Give the class and an example of 2 cholinomimetic drugs that may be used to treat conditions in which the GI or UT smooth muscle activity is depressed (no obstruction)?
1) muscarinic agonist: bethanechol (Urecholine)

2) anticholinesterase: neostigmine (Prostigmin)
What type of drugs are used to treat GERD in lieu of cholinomimetics?
H2 blockers are popular
What is vasomotion (one of the homeostatic functions controlled by the ANS)?
Alteration or oscillation in vascular diameter.
Which system serves vegetative functions - sympathetic or para?
Which brain structures influence the ANS?
- parts of cerebral cortex
- limbic system
- cerebellum
- hypothalamus
- brain stem
Which gland is a major integration center for the ANS?
The ANS is part of what other nervous system?
It is part of the PNS - peripheral nervous system.
What is pallesthesia?
sense of vibration
What is anhidrosis?
failure of the sweat glands
What is paresis?
Slight or partial paralysis
What is accommodation reflex?
Ocular convergence. Reflex changes in the eyes that enable an object to be focused on the retina.
What are 2 other names for cholinomimetics?
1) parasympathomimetics

2) cholinoreceptor activating drugs
What are the effects of insecticide anticholinesterases on humans?

Bronchorrhea, Bronchospasm, Bradycardia
Excitation (anxiety, fasciculaions, seizures)
How do organophosphate insectisides kill?
By irreversible or longterm anticholinesterase activity and longterm, excessive parasympathetic vegetative manifestations.
What is status epilepticus?
A condition in which there are continuing epileptic attacks w/o intervals of consciousness. It can lead to brain damage and death.
What are 2 typical antidotes for insecticide or humanocide organophosphate poisoning?
1) atropine - competitively blocks all muscarinic receptors, e.g., M1, M2, M3

2) pralidoxime (Protopam, 2-PAM) - competitively inhibits binding of organophosphates to acetylcholinesterase.

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