Exam 1: Chapter 20: Cholinergic Drugs Flashcards
Parasympathetic Nervous System
receives innervation from cell bodies located in the cranial nerve nuclei and sacral region of the spinal cord (craniosacral division)
Cholinergic Drugs
- aka parasympathomimetics
- mimics effects of PSNS neurotransmitter acetylcholine (ACh)
- stimulates PSNS
Two Types of Cholinergic Receptors
Based on location and action once stimulated
- Nicotinic Receptors
- Muscarinic receptors
Nicotinic Receptors
located in the ganglia of both the PSNS and SNS
named nicotinic because they can be stimulated by the alkaloid nicotine
Muscarinic Receptors
- located postsynaptically in the effector organs of the PSNS (smooth and cardiac muscle, glands)
- named muscarinic because they can be stimulated by the alkaloid muscarine
Cholinergic Drugs (Direct-acting cholinergic agonists): MOA
bind to cholinergic receptors, activating them
Cholinergic Drugs (Indirect-acting cholinergic agonists): MOA
Inhibits the enzyme acetylcholinesterase, which breaks down ACh
Results in more ACh available at the receptors
Indirect-Acting (Cholinesterase Inhibitors)
Reversible: binds to cholinesterase for a period of minutes to hours
Irreversible: binds to cholinesterase and form a permanent covalent bonds. (body must make new cholinesterase to break these bonds)
Drugs Effects
Stimulates intestine and bladder Stimulates pupils Increased salivation and sweating Cardiovascular effects Respiratory effects
How do cholinergic drugs affect the intestine and bladder?
increases gastric secretions
increases gastrointestinal motility
increases urinary frequency
How do cholinergic drugs affect the pupils?
constriction (miosis)
reduces intraocular pressure
What cardiovascular effects do cholinergic drugs have?
decreased heart rate
vasodilation
What respiratory effects do cholinergic drugs have?
bronchial constriction
narrowed airways
At recommended doses, cholinergics primarily affect
muscarinic receptors
At high doses, cholinergics stimulate
nicotinic receptors
Desired effects are from
muscarinic receptor stimulation
Many undesirable effects are caused by stimulation of
nicotinic receptors
Contraindications for Cholinergic Drugs
Drug Allergy GI or GU tract obstruction Bradycardia Hyperthyroidism Epilepsy Hypotension COPD
Indications for Direct-acting drugs
- reduce intraocular pressure
- useful for glaucoma and intraocular surgery (echothiophate, carbachol, pilocarpine)
- topical application because of poor oral absorption
Bethanechol
direct-acting drug
oral dose or SQ
How does bethanechol work?
increases tone and motility of bladder and GI tract
relaxes sphincters in bladder and GI tract, allowing them to empty
Bethanechol is helpful for
postsurgical atony of the bladder and GI tract
Cevimeline
direct acting drug
used to treat excessively dry mouth resulting from a disordeer known as Sjogrens syndrome
Succinylcholine
direct acting drug
used as a neuromuscular blocker in general anesthesia