Autonomic System Drugs

Question 1

When thinking about drug selectivity, even though a drug may be selective of certain receptors, it has the potential to affect _____ receptors

Answer 1

similar (Think beta 1 and beta 2 despite a selective beta 1 drug)

Question 2

This receptor is seen in most vascular smooth muscle receptors.

Answer 2

alpha-1b

Question 3

Norepinephrine is normally degraded by ______ ____ and is then eliminated in the urine as ____-_____ ___ and _____

Answer 3

1. Monoamine oxidase (MAO), 2. vanillyl-mandelic acid, (VMA), 3. metanephrines

Question 4

Epinephrine is known as a ____ or is able to raise systemic blood pressure. When used in anaphylactic shock it is __-_____ and can affect different adrenergic receptors, mainly ___ and at high doses ____ and ____

Answer 4

1. vasopressor, 2. non-selective, 3. beta 1, 4. alpha 1, 5. beta 2

Question 5

Dopamine is another vasopressor that has an additional effect that increases _____ blood flow and promotes _______. However at high doses dopamine systemic vasoconstriction can occur and in an IV infusion may cause ____ ____ if extravasation occurs.

Answer 5

1. renal, 2. diuresis, 3. tissue necrosis

Question 6

Norepinephrine is the drug of choice in _____ shock, due to its selectivity for ____ receptors, however may also cause tissue necrosis if extravasation occurs.

Answer 6

1. septic, 2. alpha-1

Question 7

Dobutamine is used in ____ _____ patients by stimulating ____ receptors, however at high doses may also stimulate _____ receptors which can lead to ______ _______

Answer 7

1. heart failure, 2. beta 1, 3. beta 2, 4. reflex vasodilation (hypotension)

Question 8

Vasopressin is the same as _____ ____ and can act as a vasoconstrictor when used with other ______

Answer 8

1. antidiuretic hormone, 2. vasopressors

Question 9

Midodrine is an _____ agonist that is used in patients with _____ _____ due to neurological disorders including Parkinsons disease and diabetic neuropathy. Be aware however that it can cause reflex _____ as well as supine ______ and _____ ____

Answer 9

1. alpha 1, 2. orthostatic hypotension, 3. bradycardia (due to sudden peripheral increase in BP), 4. hypertension, 5. urinary retention

Question 10

Examples of beta 2 agonists include _______, which can be either short or long term acting, and smooth muscle relaxants used to stop _____ ____

Answer 10

1. bronchodilators (albuterol, salmeterol), 2. preamture labor (ritrodine, terbutaline)

Question 11

Some adrenergic drugs can have parodoxical effects when affecting the peripheral nervous system vs. central nervous system. An example drug would be ______ which when active in the CNS is used to treat hypertension and prevent withdrawal symptoms drug/alcohol use

Answer 11

1. Clonidine

Question 12

While beta _ receptors mainly associate with the metabolism of fats, there are also drugs that function as agonists for example in the treatment of ______ ____

Answer 12

1. 3, 2. overactive bladder (Mirabegron)

Question 13

Alpha 1 antagonist drugs mainly cause _____ ______ relaxation, examples of these drugs are Cardura (doxasoin) and prazosin (Minipress). Side effects can include reflex _____ with fast acting versions of these drugs.

Answer 13

1. smooth muscle, 2. tachycardia

Question 14

The antidote for Epinephrine is ______ this is commonly used to treat tissue infiltration during local anesthesia

Answer 14

phentolamine (Regitine)

Question 15

Beta blockers are useful for a variety of cardiac conditions including ischemic cardiovascular disease and post MI by reducing the _____ _____ _____

Answer 15

myocardial oxygen consumption (MVO2)

Question 16

Intrinsic Sympathomimetic activity (ISA) is defined as a drug that may function as a ______ instead of ______ because the drug molecule looks identical to the endogenous version when interacting with receptors.

Answer 16

1. agonist, 2. antagonist

Question 17

Beta blockers are often avoided in diabetics due to the fact that it can hide _______

Answer 17

hypoglycemia

Question 18

It is important to avoid using beta blockers with ____ ____ ____ as it can increase risk of brady arrythmias

Answer 18

1. calcium channel blockers (verapamil and diltiazem)

Question 19

Acetylcholine is composed of _____, which is brought into the cell, and ____-___ which is synthesized inside the mitochonrdia

Answer 19

1. Choline, 2. Acetyl-COA

Question 20

When giving a nitrate drug remember that it will always be converted into ____ ____

Answer 20

Nitric Oxide

Question 21

Myasthenia Gravis is a condition that involves the destruction of _____ receptors, which can be treated by using ______ _____

Answer 21

1. Acetylcholine, 2. Acetylcholinesterase inhibitors

Question 22

An important list of side effects of anticholinergics, which can be exaggerated in the elderly, include: _____, _____ (think glaucoma), ____ (what happened to their bowels?), ____ ______ (BPH?), ______, ______, _____ (dry what?), _______ (steamy), ______ and ______

Answer 22

1. tachycardia, 2. mydriasis (DILATED pupils), 3. ileus, 4. urinary retention, 5. delirium, 6. sedation, 7. xerostomia, 8. hyperthermia, 9. convulsions, 10. confusion

Remember Can’t See, Can’t Pee, Can’t Spit, Can’t Shit

Question 23

When giving a NMBA (neuromuscular blocking agent), it is important to remember that with __-_______ drugs the rapid or _____ muscles are affected first followed by the ____ muscles and the _____. Examples of these drugs include atracurium and rocuronium which function as acetylcholine _______

Answer 23

1.Non-depolarizing 2. smaller, 3. larger, 4. diaphragm, 5. antagonists

Question 24

When reversing the effects of NMBAs, you would want to use _______ _____ to increase acetylcholine levels, however the NMBA will still be present in the body until it is completely eliminated, this process is called _____. Examples of the reversal drugs include neostigmine (Prostigmin) and edrophonium (Tensilon)

Answer 24

1. cholinesterase inhibitors, 2. recurarization

Question 25

Another method of inhibiting NMBAs involve \_\_\_\_\_\_\_, which uses drugs such as suggamadex (Bridion) which bind and surround the NMBA and prevent it from activating.

Answer 25

1. encapsulation

Question 26

Depolarizing NMBAs are different than non-depolarizing where depolarizing competes as an _____ with acetylcholine and also has a higher \_\_\_\_\_. The only example in the US used is succinylcholine (Anectine)

Answer 26

1. agonist, 2. affinity

Question 27

Because Depolarizing NMBAs are metabolized by \_\_\_\_\_\_\_\_\_, an important assessment to make is knowing if a patient has a deficiency for this enzyme or a severe response to the NMBA will occur. In addition, other drugs that affect ion channel activity such as ____ may prolong the action of these NMBAs

Answer 27

1. pseudocholinesterase, 2. lithium

Question 28

Five targets of pharmacologic therapy regarding neurotransmitter function are: \_\_\_\_\_\_, \_\_\_\_\_\_, \_\_\_\_, _____ of \_\_\_\_\_, and _____ effects.

Answer 28

1. storage, 2. synthesis, 3. release, 4. termination of action, 5. receptor

Question 29

The physiologic release of neurotransmitters from vesicle to synpase depends on extracellular ______ and occurs when an _____ \_\_\_\_\_ reaches the terminal and triggers an influx of the said ion into the terminal membrane.

Answer 29

1. calcium, 2. action potential

Question 30

Botulinum Toxin is a useful drug in the treatment of various ______ spasms due to its effect on preventing release of \_\_\_\_\_\_\_

Answer 30

1. muscle, 2. acetylcholine

Question 31

The pathway of synthesizing catecholamines in order starts with \_\_\_\_\_, which turns into \_\_\_\_, then \_\_\_\_\_, which converts into _____ and finally \_\_\_\_\_\_

Answer 31

1. tyrosine, 2. dopa, 3. dopamine, 4. norepinephrine, 5. epinephrine

Question 32

Neurotransmitters, in addition to the negative feedback system, can be modulated in the presynaptic region by special receptors known as ________ or \_\_\_\_\_\_\_

Answer 32

1. autoreceptors, 2. heteroreceptors

Question 33

Nerve receptors may be subject to increased up regulation following denervation known as _____ \_\_\_\_\_\_ which can cause some neurotransmitters to become more potent.

Answer 33

1. denervation supersensitivity

Question 34

Atropine and Scopolamine are examples of drugs where the ________ form is 100 times more potent than the ________ form but are easily racimized.

Answer 34

1. Levorotary, 2. dextrorotary

Question 35

Most tertiary (3D) antimuscarinic drugs are well absorbed in the ___ and _____ membranes

Answer 35

1. gut, 2. conjunctival

Question 36

Because quaternary antimuscarinic drugs are less _____ soluble, they tend to exhibit less CNS effects.

Answer 36

lipid

Question 37

atropine is the prototype drug of anti cholinergic drugs, one feature of it is that drug effects on the parasympathetic system decline quickly except when used in the _____ or _____ \_\_\_\_ which can last over 72 hours

Answer 37

1. iris, 2. ciliary muscle

Question 38

Antimuscarinic agents typically are moderately to not very ______ and in most tissue these drugs block _____ given cholinergic agonits more effectively than \_\_\_\_\_\_\_

Answer 38

1. selective (Atropine is not very selective), 2. exogenously, 3. endogenously (natural AcH)

Question 39

This receptor is responsible for control of the pupillary constrictor muscle. When blocked, this leads ____ due to unopposed sympathetic activity as well as eliminating the ability to focus near vision

Answer 39

1. M3 (Muscarinic), 2. mydriasis

Question 40

While at normal doses atropine can cause tachycardia, at lower doses there is initially _____ due to blocking __ receptors on vagal postganglionic fibers which normally inhibit ______ release in the sinus node.

Answer 40

1. bradycardia, 2. M1, 3. acetylcholine

Question 41

When giving doses of atropine to children, remember that one function of the drug is to suppress _____ sweating and even with regular dosing there can be a development of _____ \_\_\_\_\_

Answer 41

1. thermoregulatory, 2. atropine fever

Question 42

Atropine may have limited activity in treating patients with COPD due to its ______ nature, essentially blocking __ receptors which are autoinhibitory will inhibit bronchodilation, which is controlled by ___ receptors

Answer 42

1. nonselective, 2. M2, 3. M3

Question 43

Anti muscarinic drugs should never be used solely for the purpose of ____ unless cycloplegia or prolonged action is needed.

Answer 43

Mydriasis

Question 44

Anti muscarinic drugs used to treat overactive bladder such as \_\_\_\_\_\_\_\_, primarily target ___ receptors, however ___ receptors are also active in this process.

Answer 44

1. Oxybutynin, 2. M3, 3. M2

Question 45

Muscarinic effects can be reversed by administering a _____ drug preferably _____ which can treat toxic CNS and peripheral effects.

Answer 45

1. tertiary, 2. atropine

Question 46

These agents competitively block the action of acetylcholine as well as ______ receptors present in the autonomous nervous system.

Answer 46

1. ganglion-blocking agents, 2. nicotinic

Question 47

Because muscarinic drugs are considered ______ , ______ of the urine will increase clearance of these drugs.

Answer 47

1. alkaloids, 2. acidification

Question 48

Muscarinic agonists are able to moderate the activation of adenylyl cyclase and decrease cAMP concentrations caused by \_\_\_\_\_, therefore the effects of these agonists can also _____ the physiologic response of organs to stimulatory hormones.

Answer 48

1. catecholamines, 2. reduce

Question 49

In cases of prolonged agonist activity at nicotinic receptors, the effector response (contraction) is ______ and skeletal muscle cells \_\_\_\_, this can cause the receptor to become more resistive to reversal and can be exploited to cause _____ \_\_\_\_\_\_

Answer 49

1. abolished, 2. relax, 3. muscle paralysis

Question 50

Muscarinic agonists can be beneficial in treating eye disorders such as _____ due to its mechanism of causing ____ of the iris as well as the ciliary muscle which is stimulated by the __ receptor. This in turn increases aqueous humor outflow through the ____ of \_\_\_\_\_\_\_\_

Answer 50

1. glaucoma, 2. miosis (contraction), 3. M3, 4. canal of Schlemm

Question 51

Acetylcholine can affect the cardiovascular system due to its effects in producing ______ and decreasing _______ conduction velocity (Think high K, low Ca influxes and delayed hyperpolarization) in addition to _______ which are mediated by __ receptors. This response however can be opposed by a reflex _______ discharge invoked by low ___ \_\_\_\_\_\_

Answer 51

1. bradycardia, 2. atrioventricular, 3. hypotension, 4. sympathetic, 5. blood pressure

Question 52

Acetylcholine is capable of inducing vaso\_\_\_\_\_ due to activation of __ receptors. However, this requires an intact ________ or otherwise can act on arterial smooth muscle causing vaso\_\_\_\_\_\_

Answer 52

1. vasodilation, 2. M3, 3. endothelium, 4. vasoconstriction

Question 53

Studies have found nicotinic receptors on various immune cells including macrophages and astrocytes that can be induced by acetylcholine to ____ the release of inflammatory cytokines.

Answer 53

reduce

Question 54

Organophosphates are a group of cholinesterase inhibtors that are known for being _____ soluble and can be distributed to all areas of the body. The most dangerous aspect of this is its increased risk of ______ \_\_\_\_\_\_ _____ toxicity

Answer 54

1. lipid. 2. central nervous system

Question 55

The most prominent effects from cholinesterase inhibitors involve the ____ and ____ systems as well as the ___ and ____ \_\_\_\_\_ ________ \_\_\_\_

Answer 55

1. cardiovascular, 2. gastrointestinal, 3. eyes, 4. skeletal muscle neuromuscular junction

Question 56

high doses of cholinesterase inhibitors can potentially cause \_\_\_\_\_, followed by ____ and _____ \_\_\_\_\_

Answer 56

1. convulsions, 2. coma, 3. respiratory arrest

Question 57

Cholinesterase inhibitors cause these cardiovascular effects:

Answer 57

1. bradycardia, 2. increased vascular resistance (^ blood pressure), 3. decreased cardiac output

Question 58

The drug of choice used to illicit a response in myasthenia gravis patients is \_\_\_\_\_\_\_. First a 2mg dose is injected IV followed by an additional 8mg after 45 seconds if no reaction has occurred. Muscle strength improvement within 5 minutes is a positive sign.

Answer 58

Edrophonium

Question 59

When giving cholinesterase inhibitors, it is important to remember that at high doses ______ of muscle fibers may occur

Answer 59

fibrillation

Question 60

alpha blocking drugs are primarily used for _____ and ___ \_\_\_\_ \_\_\_\_\_, the main adverse effect to watch out for is ______ \_\_\_\_\_\_\_

Answer 60

1. hypertension, 2. benign prostate hypertrophy, 3. orthostatic hypotension

Question 61

An important side effect in non selective beta blockers, although not well understood, is the inhibition of ______ metabolism which can cause ________ events in diabetic patients.

Answer 61

1. carbohydrate, 2. hypoglycemic

Question 62

It is dangerous to administer beta blockers with ____ \_\_\_\_\_ blockers due to increased risk of hypotension, bradycardia, heart failure and conduction abnormalities.

Answer 62

1. calcium channel blockers

Question 63

If a patient is suffering from malignant hyperthermia due to an anesthetic complication the drug of choice to reverse this would be

Answer 63

Dantrolene

Question 64

The two main types of NMBAs are \_\_\_-\_\_\_\_\_\_, which blocks acetylcholine, and _____ \_\_\_ which produces an excess amount of acetylcholine.

Answer 64

1. non-depolarizing, 2. depolarizing agonist

Question 65

One feature of NMBAs are that they have limited entry into the CNS due to being poorly _____ soluble

Answer 65

lipid

Question 66

Because NMBAs are metabolized by the \_\_\_\_, the effect is often short but because of drug metabolites (3-Hydroxy) having a longer ____ \_\_\_\_, if the parent drug is given over an extended period of time then there may be prolonged paralysis.

Answer 66

1. Liver, 2. half life

Question 67

Depolarizing NMBAs are known for fast onset of effect and metabolism, the amount of ________ will usually determine this length of effect

Answer 67

cholinesterase

Question 68

The ______ \_\_\_\_\_ is a test that can determine how well the patient can metabolize ________ and often may have familial genetic components

Answer 68

1. dibucaine number, 2. succinylcholine

Question 69

When giving a non-depolarizing NMBA, one should be careful when admistering electrical rapid stimulation to an effected nerve as it can cause a giant release of \_\_\_\_\_\_\_\_\_\_\_

Answer 69

acetylcholine

Question 70

When administering succinylcholine and any anesthetic, particularly halothane, there is an increased risk of _____ \_\_\_\_\_\_\_, although this can be countered by administering a \_\_\_\_\_-\_\_\_\_\_\_\_\_\_ drug

Answer 70

1. cardiac arrhythmias, 2. anti-cholinergic

Question 71

Adrenoceptors are characterized by their affinity to certain catecholamines. For example alpha receptors are more potent to \_\_\_\_\_\_\_, ________ then ______ with the former being the most potent. With beta receptors the order is \_\_\_\_\_\_\_\_, ________ and _______ where the former is once again the most potent in descending order.

Answer 71

1. epinephrine, 2. norepinephrine, 3. isoproterenol, 4. isoproterenol, 5. epinephrine, 6. norepinephrine

Question 72

With dopamine receptors, __ is known to activate adenylyl cyclase while ___ inhibits it.

Answer 72

1. D1, 2. D2

Question 73

Normally catecholamines are not activated _____ due to the presence of -OH groups which makes them subjected to inactivation by \_\_\_\_\_\_-\_-\_\_\_\_\_\_

Answer 73

1. orally, 2. catechol-O-methyltransferase (COMT)

Question 74

Alpha receptor drugs that affect blood pressure are counter-acted in terms of net effect due to the ________ mechanism that usually lowers ____ \_\_\_\_\_. As a result if this is suppressed, then the drugs may stay active longer.

Answer 74

1. baroreflex, 2. heart rate

Question 75

Alpha 2 receptors typically ____ blood pressure when activated by the _____ nervous system. They can however increase blood pressure when given _____ rapidly or in very high ____ doses

Answer 75

1. decreases, 2. central, 3. intravenously, 4. oral

Question 76

D\_ receptors promote vasodilation of renal, sphlanic, coronary, cerebral and vessels as well as _____ in renal vasculature

Answer 76

1. 1, 2. natriuresis

Question 77

An important distinction between adrenoceptors and cholinergic receptors are the activation of ______ and ______ sweat glands respectively activated at these receptors as well as adrenoceptor stimulation is due to ________ stress and not _________ stress

Answer 77

1. apocrine (sweaty hands), 2. eccrine, 3. psychological, 4. thermoregulatory

Question 78

Alpha __ agonists can potentially cause urinary ______ despite it being used in situations where this is desirable in some drugs but a side effect in others like ______ (blood pressure medication)

Answer 78

1. 1, 2. retention, 3. midodrine

Question 79

Although the main modulator of insulin is \_\_\_\_\_\_, beta receptor agonists may _____ insulin secretion while alpha ___ receptor agonists may ____ insulin

Answer 79

1. glucose, 2. increase, 3. 2, 4. decrease

Question 80

Renin is moderated by beta __ receptor agonists and alpha __ receptor agonists where the former _____ renin release and the latter ______ it.

Answer 80

1. 1, 2. 2, 3. increases, 4. inhibits