Drugs for ANS

Question 1

ACh

Answer 1

Cholinergic (Muscarinic +
Nicotinic)

Choline Esters

Question 2

Dopamine

Answer 2

Catecholamine:

Direct Agonist

D1

Renal Vasodilation (Used to TX cardiogenc shock, septic shock, heart failure and adjunct to fluid administration in hypovolemic shock)

B1

Cardiac Stimulation (Used to TX cardiogenc shock, septic shock, heart failure and adjunct to fluid administration in hypovolemic shock)

a1

Increase BP (Used to TX cardiogenc shock, septic shock, heart failure and adjunct to fluid administration in hypovolemic shock)

Question 3

Albuterol

Answer 3

Non-catecholamine

β2

Direct Agonist

Bronchodilation (used in asthma)

Question 4

Terbutaline

Answer 4

Non-catecholamine

β2

Direct Agonist

Bronchodilation and uterine relaxation (used to Tx asthma and premature labor (tocolytic))

Question 5

Isoproterenol

Answer 5

Catecholamine

Direct Agonist

β2 :
bronchodilation (Used to TX asthma,

β1:
cardiac stimulation (Used to TX asthma, AV block and bradycardia)

Question 6

Dobutamine

Answer 6

Catecholamine

β1

Direct Agonist

Highest affinity for B1 receptor
Less activity at a1 receptor
Used to Tx cardiogenic shock, cardiac arrest and heart failure

Question 7

Epinephrine

Answer 7

Catecholamine

Direct Agonist

can bind to ALL the adrenergic receptors, used in anaphylactic shock and cardiac arrest

β1:
Cardiac Stimualtion (used in anaphylactic shock and cardiac arrest) 

β2:
Bronchodilation & skeletal muscle vasodilation (used in anaphylactic shock and cardiac arrest)

a1:
Vasoconstriction & Increase BP (used in anaphylactic shock and cardiac arrest)

Question 8

Atenolol, Metoprolol

Answer 8

Selective

β1

Direct Antagonist

Selective for β1 receptors (primarily in cardiac tissue) Aka cardioselective β-blockers “olol”
Produce less bronchoconstriction and other β2 receptor mediated effects
TX HTN, angina, MI

Question 9

Propranolol, Nadolol, Timolol

Answer 9

Non-selective

β

Direct Antagonist

Nonselective: “olol” Block β1 receptors in heart and β2 in smooth muscle, liver and other tissues
β1 blockade - decrease BP , decrease cardiac output, decrease renin release and decrease aqueous humor secretion
β2 blockade – bronchoconstriction, decrease glycogenolysis, mask signs of hypoglycemia
TX HTN, angina, arrhythmias, MI, migraine, glaucoma

Question 10

Clonidine

Answer 10

Non-catecholamine

α2

Direct Agonist

Inhibits NE release from nerve terminal of postganglionic neuron (feedback inhibition)
Used to treat chronic hypertension
Can have effects in CNS (sedation)

Question 11

Phenylephrine

Answer 11

Non-catecholamine

α1

Direct Agonist

Vasoconstriction, Increases BP and mydriasis (Used as nasal decongestant, ocular decongestant and maintenance of BP during surgery)

Question 12

Carbachol

Answer 12

Choline Esters

Muscarinic + Nicotinic

Direct Agonists

For chronic open-angle glaucoma, produce miosis during ophthalmic surgery (Ophthalmic drops)

Question 13

Donepezil

Answer 13

Cholinesterase Inhibitors

Reversible Agent

Muscarinic + Nicotinic

Indirect Agonists

Tx of Alzheimer’s Disease

Question 14

Edrophonium

Answer 14

Cholinesterase Inhibitors

Reversible Agents

Muscarinic + Nicotinic

Indirect Agonists

very short DOA. Used in Dx of Myasthenia Gravis

Question 15

Neostigmine

Answer 15

Cholinesterase Inhibitors

Reversible Agent

Muscarinic + Nicotinic

Indirect Agonists

Tx of Myasthenia Gravis. Antidote for skeletal muscle relaxants.

Question 16

Physostigmine

Answer 16

Cholinesterase Inhibitors

Reversible Agents

Muscarinic + Nicotinic

Indirect Agonists

Tx for overdoses of drugs with anticholinergic effects (i.e. atropine, TCAs)

Question 17

Pyridostigmine

Answer 17

Cholinesterase Inhibitors

Reversible Agent

Muscarinic + Nicotinic

Indirect Agonists

Tx of Myasthenia Gravis

Question 18

Ecothiopate

Answer 18

Cholinesterase Inhibitors

irreversible Agent

Muscarinic + Nicotinic

Indirect Agonists

Question 19

Pesticides (Palathion, Malathion)

Answer 19

Irreversible Agents (Organophosphates)

Question 20

Soman (Chemical Warfare Agent)

Answer 20

Irreversible Agents (Organophosphates):

Question 21

Bethanechol

Answer 21

Choline Esters

Muscarinic

Direct Agonists

stimulates bladder w/o significant effects on HR/BP, Tx of Urinary rentention post-op & post partum

Question 22

Methacoline

Answer 22

Choline Esters

Muscarinic

Direct Agonists

not commercially available

Question 23

Muscarine

Answer 23

Choline Esters

Muscarinic

Direct Agonists

No current medical use

Question 24

Pilocarpine

Answer 24

Choline Esters

Muscarinic

Direct Agonists

higher affinity for muscarinic receptor, Treats glaucoma: stimulate contraction of ciliary muscle fibers ->increase aqueous humor outflow->Decrease Intraocular pressure

Question 25

Cevimeline

Answer 25

Choline Esters Muscarinic Direct Agonists Treat dry mouth associated with Sjogren's syndrome (autoimmune disease that attacks exocrine glands)

Question 26

Atropine, scopolamine, hyoscyamine

Answer 26

BellaDonna Alkaloids: Muscarinic Direct Antagonists Atropine- Sinus bradycardia & AV block, mydriasis scopolamine- mydriasis, motion sickness by blocking cholinergic transmission from vestibular apparatus to vomiting center

Question 27

ipratropium, tolterodine, oxybutynin, propantheline, dicyclomine, benztropine, etc

Answer 27

BellaDonna Alkaloids: Muscarinic Direct Antagonists ipratropium-COPD, emphysema, bronchitis dicyclomine-TX of intestinal spasms/pain oxybutynin/tolterodine-TX of dysuria & urinary incontinence benztropine- TX of Parkinson’s Disease -

Question 28

Nicotine

Answer 28

Choline Esters Nicotinic Direct agonists smoking cessation

Question 29

Succinylcholine

Answer 29

Neuromuscular Blocking Agents Depolarizing Nicotinic Direct Agonists Causes “persistent” depolarization Used for surgery Effects not reversed by cholinesterase inhibitors therefore not antidote if an overdose

Question 30

Trimethaphan

Answer 30

Ganglionic Blockers Nicotinic Direct Antagonists used rarely for hypertensive emergency

Question 31

Atracurium, pancuronium, vecuronium

Answer 31

Neuromuscular Blocking Agents: Nondepolarizing aka curariforms Nicotinic Direct Antagonists Competitive antagonist of ACH at nicotinic muscle receptors Causes muscle relaxation and paralysis (by preventing depolarization) Effects reversed by cholinesterase inhibitors Used for surgery - patient can still blink/use small facial muscles

Question 32

Doxazosin, Prazosin, Terazosin Tamsulosin , Alfuzosin – only for BPH not for HTN

Answer 32

Selective a1 Direct antagonist Selective: "azosin" Relax vascular smooth muscle and smooth muscle in bladder and prostate. Produce vasodilation and Decrease BP Used to treat hypertension and urinary retention due to benign prostatic hyperplasia (BPH) Agents include: Doxazosin, Prazosin, Terazosin Tamsulosin , Alfuzosin – only for BPH not for HTN

Question 33

Phentolamine

Answer 33

Non-Selective: Block α1 and α2 receptors α Direct Antagonist Competitive, reversible DX and TX hypertensive episodes from pheochromocytoma Tx necrosis and ischemia from extravasations of epinephrine

Question 34

Phenoxybenzamine

Answer 34

Non-Selective: Block α1 and α2 receptors α Direct Antagonist Noncompetitive, irreversible TX hypertensive episodes associated w/ pheochromocytoma (tumor in adrenal medulla that secretes Catecholamines)

Question 35

Labetalol

Answer 35

Block both α and β receptors Adrenergic Direct antagonist Tx HTN

Question 36

Carvedilol

Answer 36

Block both α and β receptors Adrenergic Direct antagonist Tx HTN and CHF

Question 37

Pseudoephedrine

Answer 37

Adrenergic Mixed action agonist Nasal Decongestant, Cause vasoconstriction by binding to α1, Increase release of NE from SNS neurons

Question 38

Amphetamine

Answer 38

Adrenergic Indirect Agonists Increase the release of NE & DA from SNS neurons Vasoconstriction and increase in BP (α1) and cardiac stimulation (β) Penetrates CNS - CNS stimulation (increases mood and alertness but decreases appetite)

Question 39

Cocaine

Answer 39

Adrenergic Indirect Agonists Local anesthetic Simulates SNS by blocking reuptake of NE & DA in the PNS & SNS – similar effects as amphetamine

Question 40

Tyramine

Answer 40

Adrenergic Indirect Agonists Normal by-product of tyrosine metabolism in body Found in high concentrations in fermented foods such as certain cheeses, beers, red wine, certain cured meats (salami & pepperoni) Indirect sympathomimetic b/c it causes the release of stored catecholamines. Normally metabolized by MAO. So if taking an MAO inhibitor must avoid tyramine-containing foods.

Question 41

Norepinephrine

Answer 41

Adrenergic Direct Agonist Catecholamine a1: vasoconstriction, increase blood pressure ``` b1: cardiac stimulation (used in hypotension and shock- NOT anaphylactic shock) ```