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ANS Pharmacology

A Gq receptor that increases phospholipase C -> IP3/DAG or phospholipase A2 -> eicosanoid synthesis. Present on vascular smooth muscle, visceral smooth muscle (sphincters), radial muscle of iris, CNS neurons Alpha-1 adrenergic receptor
Gi protein that decreases cAMP or opens ligand-gated K+ channels or G0 protein blocks L and N Ca ++ vg-channels. Present on some presynaptic terminals, pacreatic islets (B-cells), platelets, ciliary epithelium, smooth muscle, CNS neurons. Alpha-2 adrenergic receptor
Gs protein increasing cAMP or opening L type Ca++ vg-channels. present on Myocardium, juxtaglomerular cells, some presynaptic terminals, adipocytes, CNS neurons. Beta-1 adrenergic receptors
Gs protein that increases cAMP. Present on visceral smooth muscle, vascular smooth muscle, liver, myocardium, skeletal muscle, some presynaptic terminals, CNS neurons Beta-2 adrenergic receptors
Gs protein that increases cAMP. Present in adipocytes Beta-3 adrenergic receptors
Gs protein that increases cAMP. Present on renal and mesenteric vascular smooth muscle, CNS neurons. D-1 dopamine adrenergic receptors
Gi protein that opens K+ lg-channels or Go protein that blocks Ca++ vg-channels. Present on some presynaptic terminals, CNS neurons. D-2 dopamine adrenergic receptors.
Ligand-gated cation channel (Na+ usually). Present on ganglionic neurons, adrenal medulla, some presynaptic cholinergic terminals, CNS neurons Nicotinic neural (Nn)
Ligand-gated cation channel (Na+). Present on skeletal muscle endplates only. Nicotinic muscular (Nm)
Gq protein phospholipase C -> IP3/DAG or closing of K+ channels. Present on ganglionic neurons, presynaptic terminals, CNS neurons. Muscarinic M1
Gi protein that decreases cAMP or opens K+ channels. Present on myocardium, presynaptic terminals, ganglionic neurons, some smooth muscle, CNS neurons. Muscarinic M2
Gq protein that activates phospholipase C -> IP3/DAG. Present on smooth muscle, exocrine glands, vascular endothelium, CNS neurons. Muscarinic M3
Alpha Blockers. Phentolamine, phenoxybenzamine, prazosin, tamsulosin
Non-selective Beta blockers Propanolol, Pindolol, Timolol, Sotalol
Selective Beta blockers Atenolol, Esmolol
Alpha-beta blockers. Labetalol
Indirect acting antiadrenergic drug. Metyrosine
Inhibitory presynaptic receptor regulation in ANS and ENS. M2, a-2, D-2, 5HT-1, 5HT-2, 5HT-3, H3, P1 (adenosine or ATP), delta (enkephalins), EP3 (PGE1, PGE2)
Excitatory presynaptic receptor regulation in ANS and ENS. Nm, B-2, AII-1 (antieotensin II)
Cholinergic receptors of the heart, arterioles, bronchial muscle, lung secretions, copora cavrnosa, uterus. M2 (little effect on the ventricle), M3 (via NO), M3, M3, M3 (via NO), M3
Cholinergic receptors in GI, pancreas exocrine secretion, Pancrease insulin secretion, Urinary detruser, urinary trigone/sphincter, Eye sphincter of iris, ciliary muscle, lacrimal glands, sweat glands, nerve endings M3 for all except M2 for last.
Adrenergic receptors in heart, arterioles in organs, arterioles in skeletal muscle and liver, veins, spleen capsule, bronchial muscle, lung secretions, skin pilomotor muscles, skin apocrine sweat glands, platelets, mast cells, fat cells B-1>>B-2, a-1, B-2, a-1 (constriction)&B-2(dilation), a-1, B-2, a-1 (decrease) B-2 (increase), a-1, a-1, a-2, B-2, B-3 (lipolysis)a-2(decrease lypolysis)
Alpha-beta agonist drugs Epinephrine and Norepinephrine
alpha agonists. phenylephrine, clonidine, apraclonidine, Tizanidine.
Beta agonists. salmeterol, albuterol, dobutamine, isoproterenol.
D-receptor agonists. Dopamine
Mixed acting adrenergic drugs. Methyldopa, Tyramine, cocaine, amphetamine, dopamine.
Epinephrine receptor targets. B-1=B-2=B-3 > a-1=a-2
Norepinephrine receptor targets. B-1 > a-1=a-2
specific alpha-1 receptor agonist. Phenylephrine
Specific alpha-2 receptor agonist. clonidine and apraclonidine
Beta-1, 2, and 3 receptor agonist. isoproterenol
Specific Beta-1 receptor agonist. Dobutamine.
Specific Beta-2 receptor agonists. albuterol and salmeterol
Dopamine-1 and 2 receptor agonist. Dopamine
Used for cases of anaphylaxis/angioedema, cardiopulmonary resuscitation in cardiac arrest, prevention of surgical bleeding (superficial wounds), retard absorption of local anesthetics, laryngotracheobronchitis/asthma (less now), open-angle glaucma. Epinephrine therapies.
Treatment of hypotension and vasodilatory shock (due to spinal trauma/spinal anesthesia/sepsis); can also be added to local anesthetics to retard absorption. Norepinephrine therapies.
Treatment when renal perfusion contributes to cardiogenic, neurogenic and septic shock. IV Dopamine therapy.
Treatment for postural hypotension (due to ANS disorder, endocrine disease, vascular insufficiency, etc.), nasal or ocular decongestant, constrict radial iris muscles (to prevent damage to eye), local vasoconstrictor(epistaxis), prolong local anesthetics Phenylephrine.
Alpha-2 agonist in the nucleus of tractus solitarius and rostral ventrolateral medulla to function in decreasing NE and Epi release. Also imidazoline receptor agonist in the ventrolateral medulla. clonidine and apraclonidine
Treatment of hypertension (second choice), W/D from tobacco/alcohol/opioids, preanesthetic to induce sedation, neuropathic pain, menopausal hot flashes, neuropsychiatric disorders Clonidine
Treatment of open angle glaucoma by increasing production of aqueous humor. Apraclonidine.
Treatment of spinal cord spasticity. Tizanidine.
List the covered direct acting muscarinic agonist choline esters. acetylcholine, carbachol, bethanecol
List the covered direct acting muscarinic agonist natural alkaloids. Pilocarpine and muscarine
List the covered direct acting nicotinic agonists. nicotine (carbachol)
List the covered cholinesterase reactivators. pralidoxime.
List the indirect reversible cholinesterase inhibitors donepezil, phenostygmine, neostygmine, edrophonium
List the indirect irreversible cholinesterase inhibitors. Organophosphates (parathion, others)
List the cholinesterase reactivators. pralidoxime.
Drug that can increase the outflow of aqueous humor by topical aplication, but has a stonger effect on nicotinic receptors than acetylcholine. Carbachol
Drug that is delivered PO or SC, has nicotine blocking activity, but is a powerful M3 and M1 receptor agonist. Bethanechol.
Drug with a tertiary structure that activates M1, M2, and M3 receptos, but does not have nicotinic activity. used to treat open-angle glaucoma when beta blockers are contraindicated or xerostomia. Pilocarpine (muscarine is Quaternary)
Patient comes in drooling with nausea, diarrhea, cold sweat, tachypnea, tachycardia, disturbed hear/vision, and marked weakness. PE reveals multiple patches attached to skin and a large wad of gum in their mouth. What is a likely culprit? Nicotine poisoning.
A monoquaternary oxime that is a cholinesterase reactivator used in cases of organophosphate poisoning (insecticide). Though it cannot reverse central effects. Pralidoxime
Treatment for myasthenia gravis because of both indirect and direct effects related to cholinergic system. neostigmine
A drug that modestly slows the degeneration of cognitive function seen in alzheimers disease due to selective inhibition of acetylcholinesterase in the brain. Donepezil
A nonselective a-1 and a-2 antagonist. Phenoxybenzamine and Phentolamine (ergot alkaloids, neuroleptics, tricyclic antidpressants also have similar property)
Selective a-1 receptor antagonist. Prazosin and Tamsulosin
Nonselective B-1 and B-2 antagonists. Propanolol, Pindolol, Timolol, and Sotalol
Selective B-1 antagonists. Esmolol, Metoprolol, and Atenolol.
a-1, B-1, and B-2 receptor antagonists. Labetalol and Carvediol.
Drug acts by Inhibition of catecholamine synthesis leading to indirect antiadrenergic effects Metyrosine.
List examples of tertiary amines acting as antimuscarinic drugs. Atropine, Scopolamine, Homatropine, Darifenacin (Benztropine)
List examples of quaternary ammonium compounds with antimuscarinic activity. Glycopyrrolate and Ipratropium
List examples of anticholinergic ganglionic blocking drugs. Mecamylamine (Glycopyrrolate and Ipratropium)
Selective M3 receptor antagonist. Darifenacin
Nonselective M1, M2, M3 receptor antagonist with little to no nicotinic activity. Atropine.
Used to induce mydriasis, cycloplegia, decreased bronchial secretions for preoperative use. Treats IBS, biliary colic, sialorrhea, motion sickness, bronchial asthma, and parkinson's disease. Antimuscarinic drugs.
Created by: 45203472
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