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Pharm - Autonomics 1
Autonomic Drugs (Part 1) from First Aid 2013
Question | Answer |
---|---|
What is the acronym for remembering the G-protein classes of the autonomic receptors? | QISS QIQ SIQ SQS aabb M123 DHV |
Alpha-1 functions? (Gq) | Vascular constriction Pupil dilation (mydriasis) Sphincter contraction |
Alpha-2 functions? (Gi) | Negative feedback on sympathetic NE outflow Decrease insulin and lipolysis Increase platelet aggregation |
Beta-1 functions? (Gs) | Increase heart rate and contractility Increase renin Increase lipolysis |
Beta-2 functions? (Gs) | Vasodilation Bronchodilation (asthma) Increase heart rate and contractility Increase insulin Increase lipolysis Decrease uterine tone (tocolysis) Ciliary muscle relaxation after accomm. Increase aqueous humor |
M1 functions? (Gq) | CNS and enteric nervous system |
M2 functions? (Gi) | Decreased heart rate and contractility |
M3 functions? (Gq) | Bronchoconstriction Increase exocrine secretions Increase gut peristalsis Increase bladder contraction Pupil constriction (miosis) Ciliary muscle contraction, accomm. |
D1 functions? (Gs) | Relax renal vascular smooth muscle |
D2 functions? (Gi) | Modulate transmitter release in the brain |
H1 functions? (Gq) | Increases mucus production, bronchiole constriction, pruritis, and pain. |
H2 functions? (Gs) | Increases gastric acid secretion. |
V1 functions? (Gq) | Vascular smooth muscle contraction. |
V2 functions? (Gs) | Increase H2O permeability and reabsorption in the collecting ducts. |
Direct cholinergic/parasympathetic agonists | Bethanechol, Carbechol, Pilocarpine, Methacholine |
Bethanechol: MOA, Use | Activates bowel and bladder. "Bethany, call me if you want to activate your bowels and bladder." |
Carbachol: MOA, Use | "Carbon copy of acetyl-Choline" Use for glaucoma, pupillary contraction, and relief of intra-ocular pressure (opposite of beta-2). |
Pilocarpine: MOA, Use | Exocrine glands: "you CRY, SWEAT, and DROOL on your PILLOW" Treats both kinds of glaucoma. |
Methacholine: MOA, Use | Stimulates muscarinic receptors in the airway when inhaled: asthma challenge test. |
Indirect cholinergic agonists (anticholinesterases) | Neostigmine, Pyridostigmine, Edrophonium, Physostigmine, Donepezil |
Neostigmine: Uses | Reverse post-operative NMJ block, neurogenic ileus or urinary retention. Myasthenia gravis. NO CNS penetration. |
Pyridostigmine: Uses | Myasthenia gravis - LONG ACTING Does not penetrate CNS. |
Edrophonium: Uses | Diagnosis of Myasthenia gravis - very short acting |
Physostigmine: Uses | Treat anti-cholinergic toxicity: "Physostigmine PHYxes atropine overdose." DOES cross CNS! |
Donepizil: Uses | Increase Ach in Alzheimer's disease. |
General side effects of cholinomimetic agents? | Exacerbation of COPD, asthma, and peptic ulcers. |
Cholinesterase inhibitor poisoning | Usually due to organophosphates that irreversibly inhibit AChE: DUMB BELSS Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation (of muscles), Lacrimation, Sweating, and Salivation |
What is the antidote for cholinesterase inhibitor poisoning? | Atropine + pralidoxime (regenerates Ach) |
Muscarinic antagonists | Atropine, homatropine, tropicamide Benztropine Scopolamine Ipratropium, tiotropium Oxybutynin Glycopyrrolate |
Atropine: Uses, Tox | Treats bradycardia, dilates pupils, decreases secretions, decreases stomach acid, decreases gut motility, decreases urgency in cystitis Treats DUMBELSS in agonist O/D. Tox: Hot as a hare, Dry as a bone, Red as a beet, Blind as a bat, Mad as a hatter |
Benztropine: Use | CNS - Parkinson's dz |
Scopolamine: Use | CNS - motion sickness |
Ipratropium, tiotropium: Uses | Resp - COPD, asthma. "I pray I can breathe soon." |
Oxybutinin: Use | GU - reduce urgency, spasms in cystitis |
Glycopyrrolate: Use | GI - treat drooling and peptic ulcers Resp - reduce airway secretions post-op |