| Flap 1 |
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|
| Flap 2 |
|
|
| alpha-1 |
Gq; increaes vasculr smooth muscle contraction |
| alpha-2 |
Gi; decrease sym outflow; decrease insuline release |
| beta-1 |
Gs; heart- increase HR, contractility; increase renin release, increase lipolysis, maintains aqueous humor formation |
| beta-2 |
Gs; lungs- vasodilation, bronchodilation; heart- increase HR, contractility; increase lipolysis, increase glucagon release |
| M1 |
Gq; in brain; CNS, enteric nervous system |
| M2 |
Gi; decrease HR, contractility |
| M3 |
Gq; increase exocrinie gland secretions, increase gut peristalsis, increase bladder contraction |
| D1 |
Gs; relaxes renal vascular smooth muscle |
| D2 |
Gi; modulates transmitter release, especially in brain |
| H1 |
Gq; increase nasal and bronchial mucus production, contraction of bronchioles, pruritis, pain |
| H2 |
Gs; increase gastric acid secretion |
| V1 |
Gq; increase vascular smooth muscle contraction |
| V2 |
Gs; increase water permeability and reabsorption in the collecting tubles of kidney |
| Gq receptors |
H1, alpha-1, V1, M1, M3 (HAVe 1 M&M) |
| Gs receptors |
B1, B2, D1, H2, V2 |
| Gi receptors |
M2, alpha-2, D2 (MAD 2's) |
| Gq protein MOA |
PLC --> PIP2 --> IP3 and DAG --> increase Ca++ in and PKC |
| Gs protein MOA |
adenylyl cyclase --> cAMP --> PKA |
| Gi protein MOA |
inhib adenylate cyclase -->decreased cAMP --> inhib PKA |
| bethanechol |
direct ACh agonist; activates bowel and bladder |
| carbachol |
direct ACh agonist; used in glaucoma, pupillary contraction, release of intraocular pressure |
| pilocarpine |
direct ACh agonist; stimulates sweat, tears, saliva |
| methacholine |
direct ACh agonist; challenge test for asthma diagnosis |
| neostigmine |
AChE inhibitor; reversal of neuromuscular jxn blockade, MG; NO CNS penetration |
| pyridostigmine |
AChE inhibitor; MG (long-acting) |
| edorphonium |
AChE inhibitor; tensilon test to diagnose MG |
| physostigmine |
AChE inhibitor; glaucoma |
| used in glaucoma; crosses BBB; used to treat atropine OD |
physostigmine |
| AChE inhibitor poisoning |
excess ACh; DUMBBELSS- diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimation, sweating, salivation |
| AChE inhibitor OD antidote |
atropine (anti-muscarinic), parlidoxime (regenerates active AChE) |
| AChE inhibitor for Alzheimer's |
donepezil, galantamine, rivastigmine |
| muscarinic antag; produces mydriasis and cycloplegia |
atropine |
| muscarinic antag; use in Parkinson's |
benztropine |
| muscarinic antag; use for motion sickness |
scopolamine |
| muscarinic antag; used in asthma, COPD |
ipratropium |
| muscarinic antag; use to reduce urgency in mild cystitis and reduce bladder spasms |
oxybutynin |
| muscarinic antag; use for peptic ulcer treatment |
propantheline, methoscopolamine, glycopyrrolate |
| glaucoma drugs |
alpha-agonists (epi, brimonidine), beta-blockers (timolol), cholinergics (pilocarpine), diuretics (acetazolamide, mannitol), PG (latanoprost) |
| 1st line for glaucoma |
latanoprost (PG) |
| glaucoma drug that increases outflow of aqueous humor |
pilocarpine |
| atropine contraindications |
glaucoma, BPH, GI obstruction, dementia, infants with fever |
| atropine |
muscarinic antag; (blocks ACh effects); used to treat cholinesterase inhibitor poisoning (insecticides) |
| parathion |
AChE inhibitor in insecticides --> HIGH amounts of ACh; get DUMBBELS |
| effects of atropine |
muscarinic antag --> decreased ACh effects; increased temp, decrease secretions, peripheral vasodilation, mydriasis, agitation, urinary retention, constipation |
| hexamethonium |
nicotinic antag; blocks both sym and parasym; prevents reflex bradycardia caused by NE |
| epi |
alpha-1, alpha-2, beta-1, beta-2 sympathomimetic |
| NE |
alpha-1, alpha-2 > beta-1 sympathomimetic |
| isoproterenol |
beta-1 = beta-2 sympathomimetic |
| dopamine |
D1 = D2 > B > alpha sympathomimetic |
| dobutamine |
beta-1 > beta-2 sympathomimetic |
| phenylephrine |
alpha-1 > alpha-2 sympathomimetic |
| albuterol |
beta-2 > beta-1 sympathomimetic |
| terbutaline |
beta-2 > beta-1 sympathomimetic |
| ritodrine |
beta-2 sympathomimetic |
| amphetamine |
indirect general agonist; releases stored catecholamines |
| ephedrine |
indirect general agonist; release stored catecholamines |
| cocaine |
indirect general agonist; uptake inhibitor |
| clonidine |
central alpha-2 agonist |
| methyldopa |
central alpha-2 agonist |
| treatment for anaphylaxis, open angle glaucoma |
epi |
| treatment for septic shock |
NE |
| treatment for shock, heart failure |
dopamine |
| treatment for cardiogenic shock |
dobutamine |
| treatement for acute asthma |
albuterol |
| treatement for reducing premature uterine contractions |
terbutaline, ritodrine |
| treatement for narcolepsy, obesity, ADD, MDD |
amphetamine |
| treatment for nasal congestion, urinary incontinence, hypoTN |
ephedrine |
| causes vasoconstriction and local anesthesia |
cocaine |
| treatment for HTN, especially in patients with renal disease |
clonidine, methyldopa |
| phenoxybenamine |
irreversible alpha blocker |
| phentolamine |
reversible alpha blocker |
| used to treat pheochromocytoma |
phenoxybenzamine (irreversible alpha block), phentolamine (reversible alpha block) |
| SE: 1st dose orthostatic hypoTN |
prazosin (alpha-1 blocker) |
| prazosin, terzosin, doxzosin |
alpha-1 blocker |
| use to treat HTN, urinary retention in BPH |
prazosin (alpha-1 blocker) |
| mirtazapine |
alpha-2 blocker |
| use for thin, elderly patient with depression |
mirtazapine (anti-depressant, alpha-2 blocker) |
