Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Medicinal chemistry > CCBs > Flashcards

CCBs Flashcards

You may prefer our related Brainscape-certified flashcards:
AP® Chemistry flashcards Periodic Table flashcards Chemistry 101 flashcards Organic Chemistry 101 flashcards
1
Q

How many types of Ca channels are there?

A

4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are L-channels responsible for?

A

inward movement of Ca into skeletal, cardiac and smooth muscle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What do CCBs treat?

A

angina
hypertension
AF

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What do CCBs block?

A

block the flow of Ca ions into heart muscle cells and arteries

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Classes of CCBs

A
  • 1,4-Dihydropyridine
  • Benzothiazepines
  • Phenylalkylamines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

How do they block Ca ion flow?

A

they bind at specific sites in the open form of the channel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Is there structural similarity between classes?

A

no

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Example of a benzothiazepine drug

A

diltiazem

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Phenylalkylamine drug

A

verapamil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

1,4-Dihydropyridine drug

A

amlodipine

nifedipine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What does each contain?

A

an amine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What does the amine allow for?

A

oral administration

because it can form water soluble hydrochloride salt

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Does first pass metabolism take place?

A

yes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What first pass metabolism happens to amlodipine?

A

aromatic hydroxylation

dihydropyridine oxidation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What first pass metabolism happens to verapamil?

A

N and O demethylation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What first pass metabolism happens to diltiazem?

A

hydrolysis

17
Q

Where are 1,4-dihydropyridine Ca channels located?

A

vascular smooth muscle

18
Q

Where are benzothiazepine Ca channels located?

A

cardiac muscle

19
Q

Where are phenylalkylamine Ca channels located?

A

cardiac muscle

20
Q

What 2 CCBs have an synergistic effect?

A

dihydropyridines and benzothiazepines

21
Q

Plasma half life of nifedipine

A

1.5 - 2 hrs

22
Q

What metabolic transformation occurs in nifedipine?

A

oxidation

gives a pyridine, loses 2 Hs

23
Q

What is amlodipine administered as?

A

as a racemate

maleate salt

24
Q

Which isomer of amlodipine is x1000 more active?

A

S isomer

25
Q

What reduces activity at N1 on 1,4-dihydropyridine?

A

substitution

26
Q

What can be added to C 2/6 on dihydropyridine to add to activity?

A

small groups
CH3
CHO
CN

27
Q

What decreases activity on C 2/6 on dihydropyridines?

A

H or Ph

28
Q

What is essential at C4 in dihydropyridine?

A

phenyl ring

29
Q

What needs to be at C3 on dihydropyridines?

A

ester group

30
Q

What adds lipophilicity at C5 on duhyfropyridines?

A

ester

31
Q

How many chiral centers in diltiazem?

A

2

32
Q

Which from is x10 more active in diltiazem?

A

cis form

33
Q

What can diltiazem also be prescribes as?

A

inhibitor of CTP3A4

34
Q

What is verapamil administered as?

A

a racemate

hydrochloric salt

35
Q

What is the active metabolite of verapamil?

A

norverapamil

Medicinal chemistry (1 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions