Cholinergic drugs Flashcards
Cholinergic Drugs what is it?
Drugs that stimulate the parasympathetic nervous system (the opposing system to the sympathetic nervous system), Also known as cholinergic agonists or parasympathomimetics
Mimic effects of the parasympathetic nervous system neurotransmitter acetylcholine (ACh)
what are the two types of cholinergic receptors?
Nicotine receptors and muscarinic receptors.
what are the two types of cholinergic receptors determined by?
- location
- Action once stimulated.
Nicotinic Receptors are?
Located in the ganglia of both systems
Named nicotinic because they can be stimulated by the alkaloid nicotine.
Cholinergic Drugs: Mechanism of Action, Direct-acting cholinergic agonists
Bind to cholinergic receptors, activating them
Cholinergic Drugs: Mechanism of Action, Indirect-acting cholinergic agonists
Also known as cholinesterase inhibitors
Inhibit the enzyme acetylcholinesterase, which breaks down ACh
Results in more ACh available at the receptors
Indirect-Acting (Cholinesterase Inhibitors) - reversible
Bind to cholinesterase for a short period of time
Indirect-Acting (Cholinesterase Inhibitors) - Irreversible
Bind to cholinesterase for a long period of time
Bind to cholinesterase and form a permanent covalent bond
The body must make new cholinesterase to break these bonds.
Drug Effects
Effects seen when parasympathetic system is stimulated
This system is the “rest and digest” system.
Sympathetic nervous system: “flight or fight”
Drug Effects - stimulates intestine and bladder
Increased gastric secretions
Increased gastrointestinal motility
Increased urinary frequency
Drug effects - stimulates pupils
Constriction (miosis)
Reduced intraocular pressure
whats another drug effects
Increased salivation and sweating
Cholinergic Drug Effects - Cardiovascular effects
Decreased heart rate
Vasodilation
Cholinergic Drug Effects - Respiratory effects
Bronchial constriction, narrowed airways
Cholinergic Drug Effects
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.
Indications - Direct-acting drugs
Reduce intraocular pressure
Useful for glaucoma and intraocular surgery
Indications - Direct-acting drugs
pilocarpine
Indications
Topical application because of poor oral absorption
what does direct acting bethanechol do?
Increases tone and motility of bladder and gastrointestinal (GI) tract
Relaxes sphincters in bladder and GI tract, allowing them to empty
Helpful for postsurgical atony of the bladder and GI tract
Oral dose or subcutaneous injection
Indications - Direct-acting drug succinylcholine do?
Used as a neuromuscular blocker in general anaesthesia
Intravenous
Indications - Indirect-acting drugs
Increase ACh concentrations at the receptor sites, which leads to stimulation of the effector cells
Cause skeletal muscle contractions
Used for diagnosis and treatment of myasthenia gravis
Used to reverse neuromuscular blocking drugs
Used to reverse anticholinergic poisoning (antidote)
Example
physostigmine
Indications - Indirect-acting anticholinesterase drugs, and what drug is it.
Used for treatment of mild to moderate Alzheimer’s disease. donepezil (Aricept®)
Indications - memantine (Ebixa®)
Not a cholinergic drug
Also used in the treatment of Alzheimer’s disease