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Pharmacology
Cholinergics
109
Health Care
Graduate
07/16/2007

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Term
Aqueous humor outflow is constantly subnormal because of degenerative process in the trabecular meshwork.
Definition
Open Angle Glaucoma
Term
No abnormal resistance to aqueous humor outflow, typically Medical emergency with acute onset
Definition
Closed Angle Glaucoma
Term
Drugs used to Treat Glaucoma include _______, _______, _______, _______, and _______.
Definition
Alpha 2 adrenergic agonists, topical carbonic anhydrase inhibitors, beta blockers, Prostaglandin analogs, Cholinergic agonists (direct, indirect-anticholinesterase agents, sympathomimetics)
Term
Postganglionic nerves contain both sympathetic and parasympathetic _______ receptors.
Definition
Nicotinic
Term
_______ receptors are located in the gut and activate HCl secretion.
Definition
M1
Term
_______ receptors are located on cardiac and certain smooth muscle and cause bradycardia and Smooth muscle inhibition.
Definition
M2
Term
These receptors are located on exocrine glands, and Smooth Muscle cells and cause Secretion and Contraction.
Definition
M3
Term
The exception to the rule in the Sympathetic Nervous system is that Sweat Glands contain _______ receptors
Definition
Muscarinic
Term
_______ blocks muscarinic receptors, and is very effective against M2 and M3 subtypes, but is virtually ineffective against M1 subtypes.
Definition
Atropine
Term
Parasympathetic effects in the eye are _______ and _______.
Definition
Miosis; Contraction of the Ciliary Muscle
Term
The Parasympathetic Affect in the Heart is _______, when _______ receptors are stimulated.
Definition
Bradycardia; M2
Term
The Direct effects of cholinergic agents in the heart are _______ and _______.
Definition
Decreased Cardiac Output; reduced peripheral resistance
Term
Parasympathetic effects in the respiratory system are _______ and _______.
Definition
Contraction of Bronchial Smooth muscle; increased secretory activity
Term
There are _______ receptors in the ventricles and arteries which are noninnervated, therefore giving drugs which activates these receptors causes bradycardia and decreased peripheral vascular resistance.
Definition
M2
Term
The parasympathetic effects in the GI system are _______ and _______, and _______.
Definition
Increase peristalsis; relax sphincters; Increase secretory activity (salivary and gastric)
Term
Parasympathetic effects in the Genitourinary system are _______ and _______.
Definition
detrusor contraction; sphincter relaxation
Term
What is the action of Cholinergic Agonists?
Definition
Act on receptors that are activated by acetylcholine
Term
Cholinergic Agonists can be _______ or _______.
Definition
Direct acting (resemble acetylcholine); Indirect acting (Inhibit acetylcholinesterase)
Term
The Majour therapeutic uses of Cholinergic Agonists are _______, _______ and _______ stimulation, _______, and _______.
Definition
Glaucoma; GI and Urinary tract; Neuromuscular junction (myasthenia gravis; curare-induced neuromuscular paralysis); anticholinergic overdose
Term
What are the general toxic effects of Direct Acting cholinergic agonists? (10)
Definition
Flushing, sweating, bradycardia, Bronchoconstriction, GI distress, belching, nausea and vomiting, diarrhea, salivation, sensation of tightness of the urinary bladder (due to contraction)
Term
Signs of acute intoxication of Anticholinesterases are _______, _______, _______, _______, _______, _______, and _______,
Definition
Miosis (reduction in pupil size); salivation; sweating; bronchial constriction; vomiting and diarrhea, convulsions; coma
Term
Direct Acting Cholinergic Agents include _______, _______, _______ and _______.
Definition
Acetylcholine; Bethanechol; Carbachol; Pilocarpine
Term
Acetylcholine, Bethanechol, and Carbachol are all _______, while Pilocarpine is _______.
Definition
Quaternary ammonium compounds; a Tertiary ammonium
Term
Direct Cholinergic Agonists are also called _______.
Definition
Parasympathomimetics
Term
_______ Cannot cross membranes and is quickly destroyed by acetylcholinesterase so it has limited clinical use.
Definition
Acetylcholine
Term
_______ has a Short duration of action, and is only used during Cataract surgery.
Definition
Miochol E
Term
Bethanechols Duration of action is _______.
Definition
About an hour
Term
Bethanechol is designed to _______.
Definition
NOT be destroyed by acetylcholinesterase
Term
What is Bethanechol's mechanism of Action?
Definition
Contraction of bladder detrusor and relaxation of sphincter.
Term
Bethanechol's indication is _______ and _______.
Definition
Urinary retention after surgery; Postpartum
Term
The adverse Affects of Bethanechol are _______, _______, _______, _______, _______, _______, _______ and _______.
Definition
sweating; salivation; flushing, decreased blood pressure; nausea, abdominal pain; diarrhea; bronchospasm
Term
Physical Obstruction, Asthma, and Peptic Ulcers are all _______ of Bethanechol.
Definition
Contraindications
Term
_______ is Considered a third-line agent when other agents are not effective.
Definition
Carbachol
Term
This drug is only used topically as a miotic to decrease IOP and has Dangerous cardiovascular side effects.
Definition
Carbachol
Term
Carbachol is ______ resistant to cholinesterase than Pilocarpine.
Definition
More
Term
Carbachol can stimulate _______ and _______ receptors.
Definition
BOTH Muscarinic; Nicotinic
Term
Carbachol can _______ release of epinephrine from the Adrenal Medulla.
Definition
Stimulate
Term
Contraction of the ciliary muscle attached to the trabecular meshwork to enhance aqueous humor outflow is the Mechanism of action of _______.
Definition
Pilocarpine
Term
The Primary adverse reaction Pilocarpine is _______. Other adverse reactions include _______ and _______.
Definition
Brow Arches;CNS Disturbances; Miosis with decreased vision
Term
This is the Drug of Choice for EMERGENCY lowering of both wide and narrow angle Glaucoma.
Definition
Pilocarpine
Term
Reversible Cholinesterase Inhibitors (Anticholinesterases) are called _______.
Definition
Indirect Cholinergic Agents
Term
Reversible Cholinesterase Inhibitors (Anticholinesterases) cause _______ and _______.
Definition
Muscarinic; Nicotinic receptor stimulation
Term
What is the Mechanism of Action of Edrophonium?
Definition
Prolongs duration of acetylcholine by binding with acetylcholinesterase.
Term
The Clinical indication of Edrophonium is _______.
Definition
Diagnosis of Myasthenia Gravis
Term
Edrophonium is a _______ compound.
Definition
Quaternary Ammonium Compound
Term
Edrophonium has a _______ and is more _______ than Neostigmine.
Definition
Shorter duration of Action; Rapidly absorbed
Term
Physostigmine is a _______ that enters the CNS.
Definition
Tertiary Amine
Term
What is the Mechanism of Action of Physostigmine?
Definition
Prolongs duration of acetylcholine by binding with acetylcholinesterase
Term
What are the indications of Physostigmine?
Definition
Atony (Increases intestinal and bladder motility); Treatment for anticholinergic overdose (atropine, tricyclics and phenothiazines); glaucoma
Term
An Adverse Reaction of Physostigmine is that it can enter the CNS and may cause _______ in high doses.
Definition
Convulsions
Term
What adverse reactions, in addition to causing convulsion in high doses, can Physostigmine cause?
Definition
vomiting, salivation, bradycardia and respiratory arrest from systemic use; miosis and allergic irritation from ophthalmic use
Term
Reversible Cholinesterase inhibitors include _______, _______, _______, and _______.
Definition
Edrophonium; Physostigmine; Neostigmine; Pyridostigmine
Term
What makes Physostigmine a unique Reversible cholinesterase inhibitor?
Definition
It is a tertiary amine, therefore it can enter the CNS
Term
Irreversible Anticholinesterases (Cholinesterase Inhibitors) include _______, _______, _______ and _______.
Definition
Toxins; poisons; Nerve Agents; insecticides
Term
The Antidote for Irreversible Anticholinesterases are _______ and _______.
Definition
Pralidoxime (which will reactivate cholinesterase if used before aging); Atropine (for muscarinic effects: bronchoconstriction,vomiting, bradycardia, miosis, incontinence)
Term
What are the actions of Echothiophate?
Definition
miosis; muscle paralysis, respiratory arrest; convulsions
Term
What is the Clinical indication of Echothiophate?
Definition
Irreversible anticholinesterases used to treat glaucoma. ONLY used Locally
Term
Donepezil (Aricept) and Tacrine (Cognex) are other agents used to treat Alzheimer's Disease, what is their Mechanism of Action?
Definition
Increase cerebral concentrations of acetylcholine by inhibiting acethlcholinesterase
Term
Tacrine (Cognex) was the first agent approved for treatment of Alzheimer's Disease, but can cause _______.
Definition
elevation in serum alanine aminotransferse (ALT) levels
Term
Cholinergic antagonists block activity at _______.
Definition
Both nicotinic and muscarinic receptors.
Term
Cholinergic Antagonists are also called _______ or _______ drugs.
Definition
cholinergic blockers; anticholinergic
Term
The subcategories of Cholinergic Antagonists are _______, _______ and _______.
Definition
Antimuscarinic; Ganglionic Blockers; Neuromuscular blockers
Term
Muscarinic Antagonists _______ all parasympathetic activity.
Definition
Knock out
Term
Ganglionic Blockers are _______ receptor blockers.
Definition
Nicotinic
Term
What is the Mechanism of Action of Antimuscarinic Agents?
Definition
Block muscarinic receptors on the effector organs of the parasympathetic nervous system and on the sweat glands (exception from sympathetic system)
Term
What is the key reason for the usefulness of Antimuscarinic Agents?
Definition
Their specificity for muscarinic receptors (because they have little effect at the skeletal neuromuscular junction or autonomic ganglia)
Term
What are the general pharmacological effects of Atropine sulfate?
Definition
A belladonna alkaloid competitively blocks muscarinic receptors from acetylcholine. It has the ability to cross the CNS
Term
Atropine is used as an antidote for _______.
Definition
Cholinergic Agonists (Organophosphate overdoses)
Term
The Adverse Reactions of Atropine are: _______, _______, _______, _______ (CNS) _______, _______, and _______.
Definition
(autonomic)-dry mouth, blurred vision, tachycardia, and constipation; (CNS) - restlessness, confusion, and hallucinations
Term
What are the Indications for Atropine Sulfate?
Definition
Eye - Diagnostic use only - Causes mydriasis (pupil dilation) and cycloplegia (inability to focus). Increases intraocular pressure in patients with glaucoma; GI - Antispasmodic agent for GI track and bladder - Reduces motility but not hydrochloric acid; Antidote for cholinergic agonists - organophosphate overdoses
Term
Atropine is used in _______.
Definition
Multiple ACLS Protocols
Term
Atropine Improves Sinus Node and AV Node conduction by _______ vagal activity.
Definition
Inhibiting
Term
Atropine gets rid of the _______ in the heart, therefore the sympathetic system is able to take over.
Definition
Parasympathetic effects (M2)
Term
Anticholinergic contraindications are _______, _______, _______, _______, _______, and _______.
Definition
Narrow angle glaucoma, Tachycardia, GI or GU Obstructive disease, Myasthenia gravis , Asthma (Atropine only)
Term
What are the Anticholinergic Warnings?
Definition
Heat prostration - due to decreased sweating; Diarrhea; Gastric ulcers - These will delay gastric emptying time
Term
Scopolamine is indicated for _______.
Definition
Motion Sickness
Term
Why might Scopolamine be used in surgery?
Definition
To block short-term memory
Term
Both _______ and _______ are used to reduce the flow of saliva (antisialagogue) in surgery.
Definition
Scopolamine; Atropine
Term
Scoploamine is a _______ antimuscarinic Blocker.
Definition
Prototypical antimuscarinic (anticholinergic) blocker.
Term
Scopolamine has _______ CNS penetration and therefore _______ CNS affects than Atropine.
Definition
Greater; Greater
Term
Donnatal will cause _______ and _______.
Definition
drowsiness; anticholinergic side effects (dry mouth, urinary retention, constipation, and increased sensitivity to light)
Term
Donnatals indication is _______, Although it only relieves the symptoms and does nothing to correct the underlying problem.
Definition
A GI Antispasmodic
Term
Dicyclomine (Bentyl) is an _______.
Definition
anticholinergic GI antispasmodic
Term
What is the indication of Dicyclomine (Bentyl)?
Definition
Treatment of functional bowel/irritable bowel syndrome. It can also be used to increase bladder capacity in patients with detrusor hyperreflexia
Term
Dicyclomine (Bentyl) is containdicated in _______.
Definition
Infants less than six months old
Term
Oxybutynin (Ditropan) targets _______ receptors.
Definition
Muscarinic
Term
Oxybutynin (Ditropan) exerts _______ effects on smooth muscle.
Definition
Direct Antispasmodic
Term
What are the indications for Oxybutynin (Ditropan)?
Definition
Bladder instability and overactive bladder
Term
This is the newest anticholinergic indicated for overactive bladder.
Definition
Tolterodine (Detrol)
Term
Ipratropium (Atrovent) is indicated for _______ and _______.
Definition
Bronchospasm associated with COPD; Rhinorrhea
Term
Ipratropium (Atrovent) Acts on _______ receptors.
Definition
Muscarinic
Term
Ipratropium (Atrovent) has both _______ and _______ effects.
Definition
Brochodilation (Effects are localized predominantly in the lungs); Anti-secretory
Term
Compared to Beta agonists (ie. Albuterol) Ipratropium is generally considered _______ in COPD patients but _______ in asthmatic patients.
Definition
Equal or superior; Not as Effective
Term
_______ is an Inhaler containing both ipratropium and albuterol
Definition
Combivent
Term
Several anticholinergics are used to treat _______, where they serve to lower the amount of acetylcholine in the CNS to attempt to keep it in balance with dopamine.
Definition
Parkinsonism
Term
Anticholinergics used to treat Parkinsonism include _______ and _______.
Definition
Benztropine (Cogentin); Trihexyphenidyl (Artane)
Term
_______ drugs Benztropine (Cogentin) and Trihexyphenidyl (Artane) are both anticholinergic drugs used to treat parkinson’s disease.
Definition
Antimuscarinic
Term
Ganglionic Blockers show _______ selectivity block receptors on _______ the parasympathetic and sympathetic ganglia
Definition
NO; Both
Term
Nicotine in _______ doses causes ganglionic stimulation causing euphoria and arousal. It also causes relaxation, and improves attention
Definition
Low
Term
Nicotine in _______ doses creates a ganglionic blockade causing respiratory paralysis and hypotension
Definition
High
Term
Neuromuscular Blocking Drugs block _______ receptors on the neuromuscular skeletal muscle junctions.
Definition
Nicotinic
Term
Nicotinic receptor Antagonists are _______, they sit on the receptor and shut them down.
Definition
Nondepolarizing
Term
Nicotinic receptor Agonists are _______, they overstimulate the nicotinic receptor and desensitize them.
Definition
Depolarizing
Term
Neuromuscular Blocking Drugs are indicated in _______.
Definition
Surgery to produce complete muscle relaxation
Term
Nondepolarizing blockers, such as Turbocurarine are _______, their action can be reversed by increasing concentration of acetylcholine with cholinesterase inhibitors (neostigmine, edrophonium and pyridostigmine)
Definition
Competitive Blockers
Term
In Low Doses Nondepolarizing blockers _______ with receptor and prevent ACh binding. Action can be overcome by increasing concentration of _______.
Definition
Combine; Cholinesterase
Term
In High Doses of Nondepolarizing blockers the ability of cholinesterase reversal is _______ due to the blockage of the end plates
Definition
Reduced
Term
This is an extremely rapidly acting Depolarizing Agent used for rapid intubation.
Definition
Succinylcholine
Term
The Primary adverse effect of Succinylcholine is _______.
Definition
Malignant Hyperthermia
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