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Quiz 2 Drugs and Receptors
Lectures six seven and eight
39
Medical
Professional
11/01/2011
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Term
Bethanechol
 Definition
• Muscarinic
• Hypotonic neurogenic Bladder
• Urinary retention
• Intestinal atony
Term
Methacholine
 Definition
• Mainly cardivascular Muscarinic
• Brachial airway hyperreactivity
• Asthma
Term
M1 ("neural")
 Definition
• Autonomic ganglia, presynaptic nerve terminals, and central nervous system
• Increased IP3
• Modulation of neurotransmission
Term
M2 ("cardiac")
 Definition
• Cardiac tissue (sinoatrial and atrioventricular nodes)
• Increased potassium efflux or decreased cAMP
• Slowing of heart rate and conduction
Term
M3 ("glandular")
 Definition
• Smooth muscle and glands
• Increased IP3
• Contraction of smooth muscles and stimulation of glandular secretions
• Vascular smooth muscle
• Increased cGMP due to nitric oxide stimulation
• Vasodilation
Term
Nicotinic Muscle type
 Definition
• Neuromuscular junctions
• Increased sodium influx
• Muscle contraction
Term
Nicotinic Ganglionic type
 Definition
• Autonomic ganglia
• Increased sodium influx
• Neuronal excitation
Term
Nicotinic CNS type
 Definition
• Central nervous system
• Increased sodium influx
• Neuronal excitation
Term
nAChR
 Definition
 Fast EPSP
Term
Dopaminergic/-adrenergic/ M2 receptors
 Definition
 Slow IPSP
Term
M1 receptors
 Definition
 Slow EPSP
Term
Peptide transmitters R (angiotensin, substance P)
 Definition
 Late Slow EPSP
Term
Direct Acting CHOLINERGIC AGONIST
 Definition
 Achetylcholine
 Bethanechol
 Methacoline
 Pilocarpine
 Succinylcholine
 Nicotine
Term
Indirect Acting (reversible) CHOLINERGIC AGONIST
 Definition
 Edrophonium
 Neostigmine
 Physostigmine
 Pyridostigmine
Term
Indirect Acting (irreversible) CHOLINERGIC AGONIST
 Definition
 Echothiophate
 Isoflurophate
Term
Reactivation of Acetylcholine Esterase CHOLINERGIC AGONIST
 Definition
 Pralidoxime
Term
Muscarinic Receptor Agonists
 Definition
o Clinically used for diagnosis of asthma and miotics
o Structure variation: amphipathic vs. charged
Term
Pilocarpine Tretiary amine
 Definition
• Muscarinic
• Glaucoma
• Miosis induction
• Xerostomia or xerophalmia
Term
pharmacology of the cholinomimetics
 Definition
o The major therapeutic uses:
 Glaucoma (closed angle and wide angle)
• Glaucoma is a disease characterized by increased intraocular pressure.
 Mechanism: Muscarinic stimulants and cholinesterase inhibitors reduce intraocular pressure by causing contraction of the ciliary body so as to facilitate outflow of aqueous humor/diminishing the rate of its secretion.
 Treatment: direct agonists (pilocarpine, emergency treatment ) or cholinesterase inhibitors (echothiophate, isoflurophate longer duration of action).
 For chronic glaucoma, these drugs have been largely replaced by topical -blockers and prostaglandin derivatives.
Term
Albuterol
 Definition
2 agonist) dilate bronchioles selectively
Term
Metoprolol
 Definition
(1 antagonist) selectively decrease heart rate
Term
bethanecol
 Definition
Pharmacological M-agonist bethanecol (GI and urinary tract motility)
Term
atropine
 Definition
M-antagonist atropine (dilate pupils- mydriais/ increase heart rate) action
Term
NN
 Definition
Neuronal- excites neurotransmission

NN: a and b subunits
Term
NM
 Definition
–somatic neuromuscular – excites muscle contraction

NM:5 subunits; 30-50% homology
Term
phentolamine
 Definition
selectively blocks α-adrenoceptors
Term
propranolol
 Definition
selective β-adrenoceptors blocker
Term
 Inhibit synthesis of neurotransmitter
 Definition
• Hemicholinium
• Metyrosine (alpha-methyl-para-tyrosine)
Term
 Prevent vesicular storage of neurotransmitter
 Definition
• Vesamicol*
• Reserpine
Term
 Inhibit release of neurotransmitter
 Definition
• Botulinum toxin
• Bretylium
Term
 Increase release of neurotransmitter
 Definition
• Black widow spider venom (α-latrotoxin)*
• Amphetamine
Term
 Inhibit reuptake of neurotransmitter
 Definition
• Cocaine
Term
 Inhibit metabolism of neurotransmitter
 Definition
• Cholinesterase inhibitors (physostigmine)
• Monoamine oxidase inhibitors (phenelzine)
Term
 Activate postsynaptic receptors
 Definition
• Acetylcholine, bethanechol, and pilocarpine
• Albuterol, dobutamine, and epinephrine
Term
 Block postsynaptic receptors
 Definition
• Atropine and tubocurarine (block muscarinic and nicotinic receptors, respectively)
• Phentolamine and propranolol (block α- and β-adrenoceptors, respectively)
Term
 The α1-adrenoceptors
 Definition
• mediate smooth muscle and glands contraction
Term
 The α2-adrenoceptors
 Definition
• cause transmitter release, contraction
Term
 Activation of β1-adrenoceptors
 Definition
• produces cardiac stimulation
Term
 The β2-adrenoceptors
 Definition
• mediate smooth muscle relaxation
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