Clinical Uses of Adrenergics Flashcards
How do cholinergic agonists compare to cholinesterase inhibitors?
Both have the same net effect, increase amount of Ach at the receptor
Acetyl choline, methacholine, carbachol, bethanechol and pilocarpine all fall under the class of drugs called _
Cholinomimetics
What are the 3 competitive cholinesterase inhibitors provided as examples?
Physostigmine
Neostigmine
Edrophonium
What are the 2 non-competitive cholinesterase inhibitors provided as examples?
Organophosphates
Nerve gas
How do competitive and non-competitive cholinesterase inhibitors interact?
The competitive inhibitors may be used as protective agents against the non-competitives
Among the cholinomimetics, carbachol and pilocarpine differ from methacholine and acetylcholine because _
They are not substrates for cholinesterase (pseudo or acetyl)
How do acetylcholinesterase and pseudocholinesterase affect acetyl choline? methacholine?
Both metabolize acetylcholine
Only acetylcholine metabolizes methacholine
Among the cholinomimetics, which 2 agents can be used topically on the eye? Which is more effective?
Carbachol (more effective)
Pilocarpine
Among the cholinomimetics, which 2 are most “antagonizable” by atropine?
Acetylcholine
Methacholine
Rank the 4 cholinomimetics in order of length of action. Longest first
Pilocarpine
Carbachol
Methacholine
Acetylcholine
What are the 2 insecticides provided as examples of cholinesterase inhibitors? What is malathion used for?
Malathion (Lice)
Parathion
What drug can be used prophylactically to prevent toxicity from large doses of cholinesterase inhibitors? How does it work?
Pyridostigmine
Inhibits approx. 30% of enzymatic activity, preventing 30% of enzyme population from being inactivated
Among the reversible cholinesterase inhibitors physostigmine, neostigmine and edrophonium, which is lipid soluble, therefore useful in treating glaucoma or CNS conditions?
Physostigmine
Among the reversible cholinesterase inhibitors physostigmine, neostigmine and edrophonium, which 2 are useful as curare antagonists?
Neostigmine
Edrophonium
Among the reversible cholinesterase inhibitors physostigmine, neostigmine and edrophonium, which 2 the most effective acetylcholinesterase inhibitor?
Neostigmine (most effective)
Edrophonium
Among the reversible cholinesterase inhibitors physostigmine, neostigmine and edrophonium, which is able to inhibit plasmacholinesterase?
Physostigmine
Among the reversible cholinesterase inhibitors physostigmine, neostigmine and edrophonium, which is used in the treatment of myesthenia gravis?
Neostigmine
What is jimsonweed?
It is an antimuscarinic agent with potential as a drug of abuse
What two antimuscarinic agents have both central and peripheral effects?
Atropine
Scopolamine
Many drug classes have antimuscarinic effects. Name 3 example
H1-antihistamines
Tricyclic antidepressants
Neuroleptics
When referring to the nicotinic receptors, N1 refers to _ and N2 refers to _
N1 - Ganglionic
N2 - Neuromuscular
What is the main agonist of the N1 type receptor? What is its effect on HR and epinephrine?
Nicotine
Increases both HR and epinephrine release
What are 2 N1 antagonists provided as examples?
Trimethaphan
Mecamylamine
What are 2 examples of competitive N2 antagonists? One example of non competitive N2 antagonists?
Competitive - Curare, pancuronium
Non-compet - Succinylcholine
What is the main effect area affected by acute adrenergic syndrome? chronic adrenergic syndrome?
Acute - Cardiovascular
Chronic - CNS
What 2 drugs are associated with chronic adrenergic syndrome?
Amphetamines
Methylphenidate (Ritalin)
Alpha 1 adrenergic agonists are used for the treatment of what 2 conditions? What are their effects?
Nasal decongestion (arteriolar constriction) Blood pressure (increase MAP)
What are 2 major uses of alpha 1 adrenergic antagonists?
Decrease blood pressure
Alter micturition
How does terazosin alter micturition? Where is it working?
It blocks alpha 1 receptors in the neck of the bladder, causing relaxation. Reduces micturition
What is the example of the non-selective beta-adrenergic agonist provided? What is its effect of GI and bronchial muscles? On blood glucose and free fatty acids?
Isoproterenol
Relaxes GI and bronchial muscles
Increase blood glucose and free fatty acids
What is a major use of beta 2 agonists?
Bronchodilation
What is a tocolytic? What class of adrenergic drug is considered a tocolytic?
Tocolytic is a drug that prevents uterine contraction
Beta 2 agonists
What type of drug class will cause the following symptoms? Hypotension Improve congestive heart failure Worsen bronchoconstriction Cloud symptoms of hypoglycemia?
Adrenergic blockers
