Parasympathetic drugs Flashcards
Effects of ACh on the body
- Skeletal muscle contraction
- Convulsions in CNS
- Bladder, uterine contraction
- Miosis
- Emesis - GI contraction
- Bradycardia/bronchoconstriction
- Increased secretions
Direct acting parasympathomimetics
- Bethanechol (important)
- Pilocarpine (important)
- ACh
- Carbachol (old opthalmic drug)
- Muscarine (mushroom poison)
Bethanechol mode of delivery
by mouth (PO)
Bethanechol targets _________ to cause _________
Bethanechol targets M3 muscarinic receptors to cause contraction of the bladder/detrussor muscle.
When do you use bethanechol?
Urinary disorders in which there is bladder atony (no bladder tone). In cases of spinal injury or dysautonomia - malfunction of ANS
When do you not use bethanechol?
- Blocked urethra or GI tract (will stimulate both)
- Overdose leads to excessive urination/defecation or eventual bradycardia.
What type of drug is bethanechol?
Direct acting parasympathomimetic drug acting on the bladder. (M3)
Pilocarpine mode of delivery?
Topical ophthalmic mediation
Pilocarpine is used to stimulate _________
Pilocarpine is used to stimulate mitosis (contraction on the pupil)
Pilocarpine can be used to treat __________
Glaucoma.
Stretching of the iris allows for the aqueous outflow tract to open up, decreasing intraocular pressure.
When do you not use pilocarpine?
Anterior uveitis or anterior lens luxation.
** it can also be irritating and mitosis can last 2-6 hours or become irreversible during chronic use.
What type of drug is Pilocarpine?
DIrect acting parasympathomimetic acting on the eye. (Most likely at M5)
What does indirect acting parasympathomimetics mean?
They impair the function of acetylcholinesterase (anticholinesterases) in which they irreversibly or reversibly bind so that ACh cannot be broken down causing a build up ACh at the synapse.
Name 5 reversible indirect acting parasympathomimetics.
Neostigmine Pyridostigmine Edrophonium Physostigmine Demarcarium
Neostigmine mode of delivery?
Mainly injection, sometimes by mouth.
What is neostigmine used for?
Large animal. Rumen atony, stimulating GI motility in horses, bladder emptying, reverse neuromuscular blockers, and treat myasthenia gravis (not enough ACh receptors for muscle contraction).
How fast is the onset of neostigmine and the duration of neostigmine?
Onset is 10-30 minutes and duration is 4 hours.
What type of drug is neostigmine?
Reversible indirect acting parasympathomimetic acting on acetylcholinesterases at smooth/skeletal muscle.
Pyridostigmine mode of delivery?
By mouth tablet or syrup, or injectable.
What is pyridostigmine used for?
Stimulating GI motility, bladder emptying, reverse neuromuscular blockers, and MAINLY treat myasthenia gravis in small animals (not enough ACh receptors for muscle contraction)
How fast is the onset of pyridostigmne and the duration of pyridostigmine?
Onset is about an hour and duration is 8-10 hours.
What type of drug is pyridostigmine?
Reversible indirect acting parasympathomimetic acting on acetylcholinesterases at smooth/skeletal muscle.
Edrophonium mode of delivery?
Injectible only
What is edrophonium used for?
Diagnosis of myasthenia gravis or determining the a myasthenic crisis from a cholenergic crisis.
How fast is the onset of edrophonium and the duration of edrophonium?
Onset is less than one minute and duration is about 10 minutes.