Neuromuscular Blockers Med Chem Flashcards

1
Q

What are the general properties of Spasmolytic agents? (Select All)

A. The exact MOA of spasmolytic medications is not completely known.

B. They are all typically Uncharged and as a result they are orally absorbed and can penetrate the BBB more easily

C. They all exhibit a common pharmacophore (common structure and MOA)

D. Act at the spinal cord and not the brain

E. Have drug interactions with opiod analgesics, benzodiazepines and barbituates and can cause respiratory depresion

A

A, B, D, E

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2
Q

Spasmolytics are centrally acting agents at the spinal cord and can have DDIs with opiod analgesics, barbituates and benzodiazepines. Which of the following statements is true when spasmolytics are used with these agents?

A. Patient must be monitored closely for respiratory depression

B. Dosages will not need to be adjusted from either medication

C. Patients should avoid alcohol and other CNS depressants with spasmolytics

D. Dose reduction may be needed for one or both drugs

A

A, C, D

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3
Q

Baclofen is known as a _____.

A. GABA-A analog

B. GABA-B analog

A

B

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4
Q

Which structure of the following statements is true?

I: The structure circled in blue increases lipophilicity

II: The structure circled in green is an amino acid

III: The structure circled in green is Gamma-Aminobutyric Acid (GABA)

A. I only

B. II only

C. II and III

D. I and III

E. I, II, and III

A

D

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5
Q

All of the following statements are true about Baclofen EXCEPT:

A. GABA-B analog

B. GABA-A analog

C. High BBB penetration due to the P-Chloro group

D. Can be given intrathecally in the case of sever spasms

E. Eliminated unchanged in the urine and as a result its dose must be renally adjusted

A

B

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6
Q

What is the name of the moeity circled in Carisoprodol?

A. Thioethester

B. Alkanediol

C. Glycerol

D. Diesterpropane

A

B

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7
Q

In the drug Carisoprodol what is the name of the moeity circled in red?

A. Ester

B. Amide

C. Carbamate

D. none of the above

A

C

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8
Q

What enzyme is responsible for metabolizng Carisoprodol to it’s active metabolite Meprobamate?

A. CYP2C19

B. CYP2C9

C. CYP3A4

D. None of the above

A

A

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9
Q

If CYP2C19 metabolizes Carisoprodol to Meprobamate what what will you see in patients that are poor CYP2C19 metabolizers?

A. Increased levels of Meprobamate

B. Decreased levels of Meprobamate and increased levels of Carisoprodol

C. Identical levels of meprobamate and carisoprodol

D. No change in metabolism

A

B

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10
Q

What kind of reaction is happening with the metabolism of Carisoprodol to Meprobamate?

A. N-Dealkylation

B. Methylation

C. Ester Hydrolysis

D. None of the above

A

A

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11
Q

Which of the following statements is true regarding Carisoprodol? (Select All)

A. Metabolized by CYP2C9

B. Metabolized by CYP2C19

C. Drug and its metabolite have sedative, anxiolytic effect (Abuse potential)

D. Bioavailability of the drug will be affected by CYP2C19 inhibitors and inducers

A

B, C, D

She has the cyp enzyme and abuse potential in red so its important

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12
Q

What is the name of the structural moeity in Chlorzoxazone (Paraflex)?

A. Benzoimide

B. Benzopurine

C. Benzoxazolone

D. None of the above

A

C

Blue: Benz

Red: Oxazole

Green: ketone=”one

Benzoxazolone

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13
Q

Which of the following side effects are seen with Chlorzoxazone (Paraflex)?

A. Idiosyncratic Hepatotoxicity

B. Dermatologic reactions

C. Uticaria, Erythma, Pruritus

D. All of the above

A

D

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14
Q

Cyclobenazaprine HCL (FLexeril, Amrix) has a ____ moeity that makes it similar to _____.

A. Bicyclic, Bicyclic antidepressants

B. Tricyclic, Tricyclic antidepressants

A

B

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15
Q

Which of the following statements is true regarding Cyclobenzaprine HCl (Flexeril, Amrix)?

A. Long Plasma half life of 1-3 days

B. Accumulates on multiple dosing

C. Causes high incidence of sedation

D. All of the above

A

D

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16
Q

Cyclobenzaprine HCl (Flexeril, Amrix) should not be taken with ____ within ____ days of each other

A. MAO inhibitors, 14

B. MAO inhibitors, 7

A

A

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17
Q

T/F Even though Cyclobenzaprine HCl (Flexeril, Amrix) is structurally identical to a tricyclic antidepressant it does not have the efficacy of an antidepressant

A

T

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18
Q

Diazepam (Valium) is a has the ____ structural moeity.

A. Benzodiazepine

B. Benzomonazepine

C. Benzotriazepine

D. None of the above

A

A.

Benzo- Benzene ring

Diaz- meaning two nitrogens

Pine- 7-membered ring

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19
Q

When Diazepam is metabolized it creates an ____ drug known as ____.

A. Inactive, Desmethyldiazepam

B. Active, Desmethyldiazepam

A

B

Des-meaning one less

Desmethyl- meaning one less methyl group

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20
Q

The desmethyldiazepam metabolite has a half-life of ___ hours

A. 1

B. 10

C. 100

D. 1000

A

C

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21
Q

Metaxolone (Skelaxin) has the ___ moeity, just as Carisoprodol has.

A. Alkanediol

B. Alkanetriol

C. Alkenediol

D. None of the above

A

A

Alkane-3 carbon chain

Diol- two alcohols

Alkanediol

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22
Q

Metaxolone has a very large volume of distribution of ____ L

A. 8

B. 80

C. 800

D. 8000

A

C

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23
Q

T/F Metaxolone causes muscle relaxation without excessive sedation and is NOT associated with abuse

A

T

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24
Q

Metaxolone bioavailability can be increased if taken with ____.

A. Grapefruit juice

B. Fatty foods

C. Low-fat containing foods

D. On an empty stomach

A

B

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25
Q

Methocarbamol (Robaxin) contains the ____ moeity.

A. Glyceroldiether

B. Glyceroltriether

C. Glycerolmonoether

D. Glycerol

A

C

It has a glycerol backbone but one ether connection (the other is an ester) so it can be called a glycerolmonoether

26
Q

Methocarbamol (Robaxin) should be used with caution in patietns that have____

A. Parkinsons

B. Myasthenia gravis

C. Multiple Sclerosis

D. Flaccid paralysis

A

B

27
Q

Orphenadrine Citrate (Norflex) contains the ____ moeity.

A. Ethanolamine ether

B. Ethanolamine Ester

C. Propanolamine ether

D. Propanolamine Ester

A

A

Ethan- Two carbons (on the right of the oxygen)

Ol- Oxygen in the middle

Amine- Nitrogen on the right

Ether- ether in the middle

Ethanolamine ether

28
Q

T/F Orphenadrine Citrate (Norflex) resembles an H1 antagonist Diphenhydramine HCl

A

T

29
Q

Tizanidine (Zanaflex) is structurally similar to clonidine. Because of this it can exhibit ____effects.

A. Hypertensive

B. Hypotensive

A

B

30
Q

(Information Slide) The structure shown here is acetyl choline and certain paralytic drugs will contain this structure.

A
31
Q

Which of these Paralytic medications is a Depolarizing Neuromuscular Blocking Agent (NMBA)?

A. Pancuronium (Pavulon)

B. Vecuronium (Norcuron)

C. Rocuronium (Zemuron)

D. Atracurium (Tracrium)

E. Succinylcholine chloride

A

E

32
Q

Which of these Paralytic medications are Amino Steroid-based medications? (Select All)

A. Pancuronium (Pavulon)

B. Atracurium (Tracrium)

C. Mivacurium (Mivacron)

D. Rocuronium (Zemuron)

E. Vecuronium (Norcuron)

A

A, D, E

Remember: Steroid based= Curonium

33
Q

Which of these Paralytic medications is NOT Tetrahydroisoquinoline-based?

A. Pancuronium (Pavulon)

B. Atracurium (Tracrium)

C. Cisatracurium (Nimbex)

D. Mivacurium (Mivacron)

E. Doxacurium (Nuromax)

A

A

Remember: Tetrahydroisoquinoline based= Curium

34
Q

Which of the following are general properties of Paralytic agents? (Select All)

A. Typically given parenterally due to polarized nature

B. Generaly polar in nature

C. Does not cross BBB

D. Extensive CNS side effects

E. Great oral bioavailability

A

A, B, C

35
Q

When comparing Paralytic NMBAs and Spasmolytic medications, which of the following are true? (Select All)

A. Both typically act centrally in the body

B. Both typically act peripherally in the body

C. Spasmolytic medications generally are able to penetrate the BBB and as a result can exhibit CNS side effects

D. Paralytic NMBAs do not penetrate the BBB and as a result act more at the muscle (peripherally) instead of the brain and spinal cord (centrally)

E. Paralytic NMBAs agents tend to be more non-polar and uncharged molecules while Spasmolytic agents tend to be more polar and charged.

A

C, D

36
Q

In the Paralytic medication succinylcholine, what are the two structures circled in blue?

A. Acetylcholine (ACh)

B. Acetylcholinesterase (AChE)

C. Succinic Acid

D. None of the above

A

A

37
Q

In the Paralytic medication Succinylcholine (Anectine) what is the name of the group circled?

A. Acetylcholine

B. Acetylcholinesterase

C. Succinic Acid

D. None of the above

A

C

38
Q

Which of the following statements about Succinylcholine are true? (Select All)

A. Resitant to AChE but succeptable to Butyrlcholinesterase

B. Rapid onset of 45-50 sec and short DOA of 6-10 min

C. Rapid onset of 45-50 sec and long DOA of 80-120 min

D. Dimer of acetylcholine

E. Will cause an initial fasiculation (twitch) and then flaccid paralysis

A

A, B, D, E

39
Q

What is the MOA of Paralytic Non-Depolarizing NMBAs?

A. Competes with ACh at the cholinergic receptor by acting as a competitive antagonist to cause paralysis

B. Competes with ACh at the cholinergic receptor by acting as a cometitive agonist to cause paralysis

C. Permanently blocks cholinergic receptors and causes them to be recycled

D. none of the above

A

A

Non-depolarizng agents are actually preferred since they do not cause that initial fasiculation

40
Q

Answer the following question provided

A

A

41
Q

When looking at the Paralytic Non-depolarizing NMBA Pancuronium Bromide (Pavulon) the two structures outlined are:

A. Succinylcholine

B. Acetylcholine (ACh)

C. Succinic acid

D. none of the above

A

B

42
Q

On the Paralytic NMBA Pancuronium Bromide (Pavulon) what the left Ring A (blue) will bind to ____ receptors and the right Ring D will bind to ____ receptors.

A. Muscarinic, Nicotinic

B. Nicotinic, Muscarinic

A

A

How to remember which side Ring D is one:

Derecho= “Right” in spanish so Ring D is on the right side.

43
Q

Since Pancuronium (pavulon) has two rings that have ACh and one of those rings (Ring A) can block muscarinic receptors what kinds of side effects might you see?

A. Increased heart rate (Tachycardia)

B. Increased BP (HTN)

C. Decreased PNS activation

D. All of the above

A

D.

Tachycardia= RIng A blocks muscarinic receptors so if you block those on the heart then SNS will take over and increase heart rate

Increased BP= Since HR is now elevated then BP will also increase with it

Increased SNS= Since the drug blocks muscarinic receptors which are PNS dominated, there will be more SNS activity instead.

44
Q

What is true regarding Pancuronium (Pavulon)? (Select all)

A. Time of onset 45-50 sec and DOA of 6-10 min

B. Time of onset 4-6 min and DOA of 120-180 min

C. Long-acting agent

D. Short-Acting agent

E. Has Ring A and Ring D that both contain ACh

A

B, C, E

45
Q

Rocuronium bromide (Zemuron) is a Paralytic NMBA that also has a Ring A and Ring D structure. Which of it’s Rings contains acetylcholine?

A. Ring A

B. Ring D

C. Both

D. Neither

A

B

An acetylcholine structure needs a positively charged amine and an acetyl group at the end. Only the structure outlined in Ring D has this ACh functionality. Ring A does not.

46
Q

Based on the structure of Rocuronium, do you expect it to have any adverse cardiovascular side effects such as Increased BP and heart rate like Pancuronium does?

A. Yes

B. No

A

B

Acetylcholine in Ring A is what binds to Muscarinic receptors but since Rocuronium does not have the ACh in Ring A there should not be CV side effects like there are in Pancuronium

47
Q

Which of the following statements is true regarding Rocuronium (Zemuron)? (Select All)

A. Time of onset 45-60 sec and DOA of 45 min

B. Time of onset 4-6 min and DOA of 80-120 min

C. No CV side effects in comparison to Pancuronium

D. Exhibits CV side effects like Pancuronium does

A

A, C

48
Q

When looking at the Vecuronium Bromide (Norcuron) structure we can conclude that:

A. It will present CV side effects

B. it will not present CV side effects

C. It will bind to Muscarinic receptors

D. It will not bind to Nicotinic receptors

A

B

49
Q

When comparing the structure of Pancuronium bromide to Vecuronium bromide we can infer that: (Select All)

A. Vecuronium is the Desmethyl analog of Pancuronium

B. Both will exhibit CV side effects

C. Pancuronium will exhibit CV side effects

D. Vecuronium will not exhibit CV side effects

A

A, C, D

Pancuronium has one less methyl on its ring A, making it a “desmethyl” analog and also giving it a charged amino group. Which resembles ACh (hence the CV side effects)

50
Q

Which of the following statements is true regarding Vecuronium bromide (Norcuron)?

A. Does not have any CV side effects

B. All metabolites (3-hydroxy/ 17-hydroxy and 3,17 hydroxy) are active

C. Time of onset of 75-90 sec and DOA of 35-45 min

D. All of the above

A

D. All of da above

51
Q

(Information Slide) The following picture shows the common Tetrahydroisoquinoline structure that will be seen in certain Paralytic agents. Notice that the carbon is moved over one more position and the ring on the right is completely saturated with hydrogens (no double bonds)

A
52
Q

This picture shows the general structure of Paralytic Tetrahydroisoquinoline-based NMBAs. Which groups do they contain?

A. Two Quartenary ammonium atoms

B. Diesters (Two esters)

C. Alkyl chain connecting the two esters

D. Two Tetrahydroisoquinoline structures

E. All of the above

A

E

53
Q

T/F In the following structure Atracurium Besylate (Tracrium) the four cicled groups are Chiral Atoms

A

T

54
Q

All of the following statements is true regarding Atracurium besylate (Tracrium) EXCEPT:

A. Can be eliminated by Hofmann elimination

B. Creates an inactive Laudanosine metabolite that can be CNS toxic and causg convulsions. (Base catalyzed decomposition)

C. Since it can undergo Hofmann elimination it is useful for patients with hepatic and renal disease

D. Time of onset 2-4 min and DOA of 30-40 min (intermediate acting)

E. Considered to be an Amino-steroid derivative

A

E

55
Q

The following picture shows the metabolism of Atracurium through the ester hydrolysis and Hofmann metabolism. Judging by Laudanosine’s structure, why would it have adverse CNS side effects such as convulsions?

A. Very polar-charged molecule that will act in the periphery and cause CNS side effects

B. Very polar-charged molecule that will act centrally (penetrate BBB) and cause CNS side effects

C. Very non-polar (uncharged) molecule that will act centrally (penetrate BBB) and cause CNS side effects.

D. Laudanosine is not associated with any side effects.

A

C

56
Q

When comparing Cisatracurium to Atracurium all of the following statements are true except:

A. Cisatracurium requires a lower therapeutic dose

B. CIsatracurium is 3x more potent than atracurium

C. Cisatracurium has lower Cmax and lower amounts of Laudanosine formed in comparison to atracurium

D. Cisatracurium will have ;ess histamine release in comparison to Atracurium

E. Cisatracurium is available in many different isomers in comparison to Atracurium only have 2 different isomers

A

E.

In order to remember which of these has the better effects just know that cisatracurium is better than atracurium

57
Q

After a surgery or any procedure requiring the administration of a paralytic medication, what class of medications should be used to reverse the paralysis?

A. Acetylcholine esterase Inhibitors

B. Depolarizing-NMBAs

C. Non-Depolarizing NMBAs

D. None of the above

E. Any one of the above

A

A

58
Q

Which of these medications is an Acetylcholinesterase inhibitor? (Select All)

A. Neostigmine bromide (Prostigmine)

B. Succinylcholine

C. Endrophonium Chloride (Enlon, Reversol)

D. Vecuronium (Norcuron)

E. Atracurium (Tracrium)

A

A, C

59
Q

Which of the following statements is true regarding Acetylcholin esterase inhibitors

A. Reversible inhibition of AChE

B. Irreversible inhibition of AChE

C. Used post-operatively to reverse neuromuscular blockade by non-depolarizing agents

D. Used to induce paralysis in a patient

A

A, C

60
Q

Acetylcholine esterase inhibitors are meant to reverse paralysis of Non-Depolarizing NMBAs. Can they reverse paralysis of succinylchloine?

A. Yes

B. No

C. Yes but only in stage 1

D. Yes but onlly in stage 2

A

D