Pharm (Pages 225-248) Flashcards
(155 cards)
α1
G-Protein Class/Major Functions
q
Increase vascular smooth muscle contraction, Increase pupillary dilator muscle contraction (mydriasis), Increase intestinal and bladder sphincter muscle contraction
α2
G-Protein Class/Major Functions
i
Decreases sympathetic outflow, Decreases insulin release, Decreases, lipolysis, Decreases platelet aggregation
β1
G-Protein Class/Major Functions
s
Increase heart rate, Increase contractility, Increase renin release, Increase lipolysis
β2
G-Protein Class/Major Functions
s
Vasodilation, bronchodilation, Increase heart rate, Increase contractility, Increase lipolysis, Increase insulin release, DECREASED uterine tone (tocolysis), ciliary muscle relaxation, q aqueous humor production
M1
G-Protein Class/Major Functions
q
CNS, enteric nervous system
M2
G-Protein Class/Major Functions
i
Decreased heart rate and contractility of atria
M3
G-Protein Class/Major Functions
q
Increased exocrine gland secretions (e.g., lacrimal, salivary, gastric acid), increased gut peristalsis, increased bladder contraction, bronchoconstriction, decreased pupillary sphincter muscle contraction (miosis), ciliary muscle contraction (accommodation)
D1
G-Protein Class/Major Functions
s
Relaxes renal vascular smooth muscle
D2
G-Protein Class/Major Functions
i
Modulates transmitter release, especially in brain
H1
G-Protein Class/Major Functions
q
Increases nasal and bronchial mucus production, Increases vascular permeability, contraction of bronchioles, pruritus, and pain
H2
G-Protein Class/Major Functions
s
Increases gastric acid secretion
V1
G-Protein Class/Major Functions
q
Increases vascular smooth muscle contraction
V2
G-Protein Class/Major Functions
s
Increases H2O permeability and reabsorption in the collecting tubules of the kidney (V2 is found in the 2 kidneys)
Bethanechol
Clinical applications/action
Postoperative ileus, neurogenic ileus, and
urinary retention
Activates bowel and bladder smooth
muscle; resistant to AChE. “Bethany, call
(bethanechol) me, maybe, if you want to
activate your bowels and bladder.”
Direct agonist
Carbachol
Clinical applications/action
Glaucoma, pupillary constriction, and relief of
intraocular pressure
Carbon copy of acetylcholine.
Direct agonist
Pilocarpine
Clinical applications/action
Potent stimulator of sweat, tears, and saliva
Open-angle and closed-angle glaucoma
Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma); resistant to AChE. “You cry, drool, and sweat on your ‘pilow.’ ”
Direct agonist
Methacholine
Clinical applications/action
Challenge test for diagnosis of asthma
Stimulates muscarinic receptors in airway when inhaled.
Direct agonist
Neostigmine
Clinical applications/action
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative)
Increases endogenous ACh.
Neo CNS = No CNS penetration.
Indirect agonist
Pyridostigmine
Clinical applications/action
Myasthenia gravis (long acting); does not penetrate CNS
Increases endogenous ACh; increases strength. Pyridostigmine gets rid of myasthenia gravis.
Indirect agonist
Physostigmine
Clinical applications/action
Anticholinergic toxicity (crosses blood-brain barrier to CNS)
Increases endogenous ACh. Physostigmine “phyxes”
atropine overdose.
Indirect agonist
Donepezil,
rivastigmine,
galantamine
Clinical applications/action
Alzheimer disease
Increases endogenous ACh.
Indirect agonist
Edrophonium
Clinical applications/action
Diagnosis of MG (extremely short acting)
MG is now diagnosed by anti-AChR Ab test
Increases endogenous ACh.
Indirect agonist
With all cholinomimetic agents, watch for:
With all cholinomimetic agents, watch for exacerbation of COPD, asthma, and peptic ulcers when giving to susceptible patients.
Indirect agonist
Cholinesterase inhibitor poisoning
Antidote:
Often due to organophosphates, such as
parathion, that irreversibly inhibit AChE.
Causes Diarrhea, Urination, Miosis,
Bronchospasm, Bradycardia, Excitation
of skeletal muscle and CNS, Lacrimation,
Sweating, and Salivation.
DUMBBELSS.
Organophosphates are components of
insecticides; poisoning usually seen in farmers.
Antidote—atropine (competitive inhibitor) +
pralidoxime (regenerates AChE if given early).