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MPT > Final Part 1 > Flashcards

Final Part 1 Flashcards

1
Q

What is the principle cholinomimetic?

A

Acetylcholine

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2
Q

What enzyme creates acetyl choline by adding an acetyl group onto choline from Acetyl CoA?

A

Choline acetyltransferase

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3
Q

What is the limiting factor for choline acetyltransferase?

A

Choline

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4
Q

What enzyme inactivates ACh?

A

Acetylcholinesterase (AChE)

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5
Q

What amino acid must be attached to AChE to be activated?

A

Serine and Histidine

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6
Q

What process inactivates ACh?

A

Transesterification

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7
Q

What binds to AChE?

A

Serine and Histidine

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8
Q

What are the two types of cholinergic receptors?

A

Muscarinic and Nicotinic

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9
Q

What drug is selective to M1 receptors and was the only muscarinic antagonist to block gastric acid secretion and did not block other agents?

A

Pirenzapine

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10
Q

What do M1 receptors inhabit?

A

Neuronal tissue
Brain
presynaptic of autonimic ganglia
Exocrine glands

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11
Q

What disease is related to M1 receptors?

A

Alzheimer’s Disease
Memory and learning

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12
Q

Where are M2 receptors in the body?

A

Postganglionic membranes in ANS
Smooth Muscle
Heart
Exocrine Glands

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13
Q

What are M2 receptors known to do?

A

Decrease heart rate and contractility of the heart

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14
Q

Where are M3 receptors located in the body?

A

Brain
Smooth muscle and secretory glands

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15
Q

What do M3 receptors do?

A

Decrease neurotransmitter release
Contraction and secretion

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16
Q

Where are M4 receptors located?

A

Smooth muscle
Secretory glands

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17
Q

What do M4 receptors do?

A

Inhibit Calcium channels

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18
Q

Where are M5 receptors located?

A

Brain
Peripheral tissue

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19
Q

What are the two main requirements for SAR of Muscarinics?

A

Esteratic site
Anionic site

Accomodates the acetyl ester Oxygen through H bonding
Quat amine

20
Q

What must at least two of the 4 side groups be on the quat amine of muscarinics?

21
Q

What are the four classes of Cholinergis and anticholinergics?

A

Muscarinic agonist
Acetycholinesterase Inhibitors
Muscarinic agonists
Muscarinic antagonists

22
Q

What is the pKa of a phenol?

23
Q

Is a phenol acidic or basic?

A

Weakly acidic

24
Q

What is the pKa of carboxylic acid?

25
Q

Is a carboxylic acid basic or acidic?

A

Acidic strong

26
Q

What is the pKa of a thiol?

27
Q

Is a thiol acidic or basic?

A

Mildly acidic

28
Q

What is the pKa of a sulfonamide?

A

4-11

Acidic

29
Q

What is the pKa of a sulfonylurea?

A

5-6

Acidic

30
Q

What is the pKa of an alkyl amine?

A

9-11

Basic

31
Q

What is the pKa of an aromatic amine?

A

2-5

Weakly basic

32
Q

What is the pKa of a pyrrole?

A

1-3

Very weak base

33
Q

What is the pKa of an indole?

A

2

Weak base

34
Q

What is the pKa of an imidazole?

A

13-14

Strong base

35
Q

What is the pKa of a pyridine?

A

5-6

Weak base

36
Q

What is the pKa of an amidine?

A

10-11

Strong base

37
Q

What is the pKa of guanidine?

A

12-13

Very basic

38
Q

What kind of interaction is between carbons?

A

Vander waals

39
Q

What are vanderwaals forces caused by?

A

Momentarily uneven charge

40
Q

What kind of interaction can aromatic rings do?

A

Pi pi stacking

41
Q

What is stronger, dipole dipole interaction or Dipole-induced dipole interaction?

A

Dipole dipole

42
Q

What is stronger dipole induced dipole or pipi stacking

A

Dipole induced dipole

43
Q

Know rule of 9s for a base

A

1above=90% ionized, 10% unionized
2above= 99% ionized, 1% unionized
1 below = 90% unionized, 10% ionized

acid is the opposite

44
Q

Where do hydrophillic drugs go in the body?

A

To the plasma

Plasma is mostly water

45
Q

Where do hydrophobic drugs go in the body?

A

Albumin
High distribution and low excretion

MPT (5 decks)

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