(Chapter 20 Cholingeric Drugs)

Question 1

Acetylcholine (ACh)

Answer 1

Neurotransmitter responsible for transmission of nerve impulses to effector cells in the parasympathetic nervous system
- essential for learning and memory

Question 2

Acetylcholinesterase (AChE)

Answer 2

Enzymes responsible for the breakdown of ACh

Question 3

Alzheimer’s Disease

Answer 3

A disease characterized by progressive mental deterioration manifested by loss of memory, ability to calculate, and visual-spatial orientations, as well as by confusion and disorientation

• Triggers implicated in the development include genetics, environment, and lifestyle
• Characterized by oid plaques that form between neurons and Neurofibrillary tangles found in neurons
• donepezil (Aricept) in the drugs used

Question 4

Cholingeric drugs

Answer 4

Drugs that stimulate the PSNS by mimicking ACh

• Also called Parasympathomimetics
• Contraindications include brachycarida, allergy, GI or GU obstruction, hyperhtyroidism, hypotension, etc
• Adverse effects include Abdominal cramps, increased secretions, nausea, vomiting, Headache, dizziness, sweating, Bradycardia, hypotension, etc
• SLUDGE (salivation, lacrimation, urination, diapherysis, GI upset, eminis (nausea/vomiting)) - over dose symptoms
• Effects include a increase in the PSNS such as decrease in HR, constriction of the bronchoiles, increased motility and secretion of the GI tract, constriction of the pupil, increased salivation and sweating
• At recommended doses, affects primarily the muscarinc receptors but at high doses it stimulates nicotinic receptors which can causes many adverse effects

Question 5

Direct-acting cholingeric agonists

Answer 5

Drugs that bind directly to cholingeric receptors to activate them
- Really good at decreasing intraocular pressure
Example is bethanechol (Duvoid) which increases motility of the GI tract, relaxes sphincters in the bladder (helpful for post surgery)

Question 6

Indirect-acting cholingeric agonists

Answer 6

Drugs that work indirectly by making more ACh available at the receptor site (inhibits the enzyme that breaks down ACh)
- Cause skeletal muscle contractions, are used for diagnosis and treatment of myasthenia gravis, are used to reverse neuromuscular blocking drugs, and are used to reverse anticholinergic poisoning (antidote)

Question 7

Irreversible cholinesterase inhibitors

Answer 7

Drugs that form a permanent covalent bond with cholinesterase. The body must make more cholinesterase to break this bond.

Question 8

Muscarinic receptors

Answer 8

Effector organ cholingeric receptors located post synaptically in the smooth muscle, heart muscle, and glands supplied by the parasympathetic fibers
- Need to know they are in different places

Question 9

Nicotinic receptors

Answer 9

Cholinergic receptors located in the ganglia of both the PNS and the sympathetic nervous system

• Called ion receptors because they allow sodium in
• Need to know they are in different places

Question 10

Reversible cholinesterase inhibitors

Answer 10

Drugs that bind to cholinesterase for minutes to hours but do not form a permanent bond