5- Parasympathetic Drugs

b. Dantrolene

1. Which of the ff is the DOC for malignant Hyperthermia cause by a depolarizing SMR?

   a. Atropine

   b. Dantrolene

   c. Pancorunium

   d. Atracurium

a. it blocks the Muscarinic receptor

2. What is the MOA of Atropine

   a. it blocks the Muscarinic receptor

   b. it stimulates the release of aCH

   C. It stimulates alpha-1 receptor

   d. NOTA

a. Ache

3. What degrades Ach

   a. Ache

   b. CHAT

   c. COMT

   d. MAO

a. buspirone

ratio: it is for chronic anxiety

4. Which of the ff is not used as smoking deterrent

   a. buspirone

   b. bupropion

   c. Nicotine

   d. Verenicline

b. urinary retention

5. The ff are effects of ACh, except

   a. diarrhea

   b. urinary retention

   c. salivation

   d. bronchoconstriction

a. Physostigmine

6. Which of the ff is not an anti-cholinergic agent?

   a. Physostigmine

   b. Atropine

   c. Scopolamine

   d. Hyoscine

a. Pilocarpine

7. Which of the ff is approved for the management of Siogren Syndrome

   a. Pilocarpine

   b. Atropine

   c. Amphetamine

   d. Physostigmine

a. Pilocarpine

8. An alkaloid present in Pilocarpus Jaborandi

   a. Pilocarpine

   b. mescaline

   c. physostigmine

   d. atropine

a. Choline acetyl transferase

9. The enzyme required in the synthesis of acetylcholine

   a. Choline acetyl transferase

   b. Acetylcholinesterase

   c. Monoamine oxidase

   d. Catechol-O-methyl transferase

a. Bethanechol

10. Direct-acting cholinergic drug

    a. Bethanechol

    b. Physostigmine

    c. Edrophonium

    d. sarin

Parasympathetic Drugs

Involved in signal transmission (neutrotransmitter or neurotransmission) between the different parts of the body

Somatic NS

Voluntary control

Autonomic NS

Involuntary (reflex) control of: smooth mucles, exocrine glands, cardiac muscles

• Thoracolumbar

• Thoracic + Lumbar

Sympathetic Spinal Cord Location:

• Craniosacral Region

• Sacral

• Cranial Nerves

Parasympathetic Spinal Cord Location:

IX, X, VII, III

Parasympathetic Cranial Nerves:

CN IX

glossopharyngeal

CN X

vagus

CN VII

facial

CN III

oculomotor

Short (ACh)

Sympathetic, Preganglionic produces:

Long (NE)

Sympathetic, Postganglionic produces:

Long (ACh)

Parasympathetic, Preganglionic produces:

Short (ACh)

Parasympathetic, Postganglionic produces:

Fight, Flight, or Fright

Sympathetic Function:

Rest & Digest

paraympathetic Function:

Parasympathetic

Sympathetic or Parasympathetic?

Miosis

Sympathetic

Sympathetic or Parasympathetic?

Mydriasis

Parasympathetic

Sympathetic or Parasympathetic?

increase of salivation

Parasympathetic

Sympathetic or Parasympathetic?

Bradycardia

Parasympathetic

Sympathetic or Parasympathetic?

Bronchoconstriction

Parasympathetic

Sympathetic or Parasympathetic?

increase digestion

Parasympathetic

Sympathetic or Parasympathetic?

increase bile release

Parasympathetic

Sympathetic or Parasympathetic?

diarrhea

Parasympathetic

Sympathetic or Parasympathetic?

Urination

Sympathetic

Sympathetic or Parasympathetic?

decrease of salivation

Sympathetic

Sympathetic or Parasympathetic?

Tachycardia

Sympathetic

Sympathetic or Parasympathetic?

Bronchodilation

Sympathetic

Sympathetic or Parasympathetic?

decrease digestion

Sympathetic

Sympathetic or Parasympathetic?

increase of glucose

Sympathetic

Sympathetic or Parasympathetic?

constipation

Sympathetic

Sympathetic or Parasympathetic?

urinary retention

Sympathetic

Sympathetic or Parasympathetic?

increase of Epinephrine/NE

Enteric Nervous System

Innervated by sympathetic & parasympathetic NS

↑ ENS

Parasympathetic stimulation: __ ENS

↓ ENS

Sympathetic stimulation: __ ENS

• increase motility,

• secretion of gastric acid

Enteric nervous system regulates:

Acetylcholine

Neurotransmitter of Parasympathetic

Cholinergic Receptor (Muscarinic or Nicotinic)

Receptor of Parasympathetic

DUMBELS

Parasympathetic Response:

HEMICHOLINUM

Choline Uptake blocker

CHAT

Choline + Acetyl coA  (Enzyme: ___) -→ ACh

VESAMICOL

Ach Vesicular storage blocker:

LATROTOXIN

Ach is stimulated by __ for the Ach to release via exocytosis

BOTULINUM

Ach is inhibited to release via exocytosis w/:

ORGANOPHOSPHATES

AChE blocker:

ATROPINE

Ach Receptor blocker

M1

They are located in the brain & parietal cells (stomach)

M3

They are located in the Exocrine glands & smooth muscles

M5 & M4

They are located in the brain 

M2

They are located in the Heart

depolarization (excitation)

activating M3 in the skeletal muscles gives:

increase secretion

activating M3 in the exocrine gland gives:

relaxation (vasodilation)

activating M5 in the blood vessel gives:

Gq/Gaq

M1, M3, M5 are G-coupled w/ what protein?

Gi

M2& M4 are G-coupled w/ what protein?

Nn

Ganglion

Nm

Muscle

Choline Esters

quarternary compounds: polar, can’t be distributed

• Choline Esters

• Synthetic Acetylcholine Analogs

• Plant Alkaloids

• Other Drugs (Cevimeline, Varenicline)

Direct-Acting Cholinomimetics:

Direct-Acting Cholinomimetics

mimics the action of ACh to the cholinergic Receptor = DUMBELS

Indirect-Acting Acetylcholine Agonists

blocks the AChE = increase ACh = DUMBELS

Acetylcholine

used as a cataract surgery (if rapid miosis is desired)

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Acetylcholine

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Betanechol

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Carbachol

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Muscarine

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Nicotine

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Pilocarpine

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Cevimeline

Direct-Acting Cholinomimetics

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Varenicline

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Edrophonium

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Physostigmine

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Neostigmine, Pyridostigmine

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Echothiophate & Isoflurophate

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Malathion

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Soman & Sarin

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Donepezil

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Rivastagmine

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Tacrine

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Galantamine      

Indirect-Acting Acetylcholine Agonists

Direct-Acting Cholinomimetics or Indirect-Acting Acetylcholine Agonists

Memantine

Betanechol

• diarrhea & urination

• To increase bladder tone

• Non-obstructive neurogenic urinary retention: Post-operative or Post-pertum

Carbachol

• ophthalmic surgery (cataract surgery and iridectomy)

• no longer used in treating open-angle glaucoma

Muscarine

mushroom | POISON

• Muscarine

• Nicotine

• Pilocarpine

Plant Alkaloids

Nicotine

• activates Nicotinic acetylcholine receptor (alpha-4-beta-2-R) = DOPAMINE RELEASE = GOOD FEELING

• Chewing gums, transdermal patch (smoking deterrent)

BEHAVIORAL THERAPY + NicoDERM CQ PATCH: gradual reduction of dose

Treatment for Nicotine

Pilocarpine

• tertiary amine | Pilocarpus

• 2^nd Line: Glaucoma

Pilocarpine

Tx for Sjogren Syndrome