Cholinergic and Anticholinergic drugs Flashcards
What type of drug is Dabigatran Etexilate?
Anticoagulant. It is a prodrug, converted to Dabigatran after GIT absorption and conversion by plasma and liver esterases.
How does P- Glycoprotein affect Dabigatran Etexilate ?
During aborption in the GIT, it interacts with the drug limiting its entry into blood.
What body system do cholinergic and anticholinergic drugs act on ?
On the Autonomic Nervous System.
What is the function of the Autonomic Nervous System?
Involuntary, visceral motor and sensory functions.
encompasses the sympathetic and parasympathetic division.
Where do Cholinergic drugs act specifically?
On the Parasympathetic Division. This is rest and digest.
What are the effector cells of the autonomic nervous system?
Smooth and cardiac muscle.
Exocrine gland
What is the primary neurotransmitter of the parasympathetic nervous system?
ACh (Acetylcholine)
What are the primary neurotransmitters of the sympathetic nervous system?
acetylcholine and norepinephrine.
Effects of parasympathetic nerves.
- Constricts pupils and airways
- Stimulate saliva, stomach activity and intestinal activity
- Slows heartbeat
- Inhibit glucose release which stimulates gallbladder
- Contracts bladder
- Promote genital erection
What are the side effects of the cholinergic drugs.
DUMBELLS
Diarrhea
urination
miosis
bradycardia and bronchoconstriction
emesis
lacrimation
lethargy
salivation
What are the steps of neurotransmission at cholinergic neurons?
- acetylcholine is made
- taken into vesicle to prevent degradation.
- release by presynaptic receptor
- binds and activates postsynaptic receptor
- rapidly hydrolysed into choline and acetate by acetylcholine esterase in the synaptic cleft
- Choline taken up by neuron to recycle.
What is the rate limiting step of neurotransmission at cholinergic neurons?
The uptake of choline.
What are the two cholinergic receptors? How can you distinguish them?
muscarinic and nicotinic receptors.
By their affinity for agents that mimic acetylcholine action.
What are the types of muscarinic receptos?
M1 M2 M3 M4 M5
Why are they called muscarinic receptors?
They recognise muscarine and acetylcholine
Location and Function of M1recepto
