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PHS 944 > Cholinergic Handout > Flashcards

Cholinergic Handout Flashcards

1
Q

What are cholinergic drugs?

A

Medications that produce the same effects as parasympathetic nervous system.

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2
Q

[True/False] Cholinergic drugs are available OTC?

A

False. They are prescription only.

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3
Q

What are 4 therapeutic uses of cholinergic drugs?

A

Myasthenia Gravis
Glaucoma
Alzheimer’s Disease
Atropine/OP poisoning

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4
Q

A disease that causes severe muscle cramping?

A

Myasthenia Gravis

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5
Q

A disease that is caused by increased pressure inside the eye.

A

Glaucoma

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6
Q

The most common form of dementia among older people.

A

Alzheimer’s Disease

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7
Q

It accelerates the heart rate, constricts the blood vessels, and raises blood pressure.

A

Sympathetic Nervous System

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8
Q

It serves to slow the heart rate, increase the intestinal and gland activity, and relax the sphincter muscles.

A

Parasympathetic Nervous System

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9
Q

Primary neurotransmitter of the PNS?

A

ACh

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10
Q

What are the two types of ACh receptors?

A

Nicotinic and Muscarinic

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11
Q

What two substrates make ACh?

A

Choline and Acetyl CoA

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12
Q

When ACh is broken down by AChE, what is produced?

A

Choline and Acetate

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13
Q

What are the two main forms of cholinesterases in the body?

A

Acetylcholinesterase

Butylcholinesterase

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14
Q

What residue does AChE and BChE both contain?

A

Serine

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15
Q

What two ways can you find AChE and BChE?

A

Bound to a cell membrane or in a soluble form.

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16
Q

Soluble ____ is very important in keeping plasma _____ low.

A

BChE; [AChE]

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17
Q

In regards to BChE, what causes different elimination rates of some drugs?

A

Genetic Variation

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18
Q

What are 3 ways drugs may be designed to influence cholinergic transmission?

A

Acting on ACh receptors

Affecting the availability of compounds involved in the synthesis, release, and uptake of ACh.

Affecting the biochemical pathways and enzymes involved in the synthesis, packaging, release, hydrolysis, and re-uptake of ACh

19
Q

What are two ways cholinergic drugs can act?

A

As an agonist (mimic the effect of ACh)

Antagonist (to block the effect of ACh.

20
Q

How do muscarinic aginsts bind?

A

Heterogeneously to receptors in the brain and peripheral nervous system.

21
Q

What cholinesterase inhibitor that is used to treat Alzheimer’s does not inhibit BChE?

A

Galantamine

22
Q

What drug was approved for the treatment of moderate-severe AD?

A

Memantine (binds to NMDA receptors)

23
Q

What did the first drug used to treat AD have complexed with it?

A

tacrine

24
Q

The rate of hydrolytic regeneration of the phosphorylated enzyme is much slower than that of the carbamylate enzyme.

A

Irreversible Inhibitors (forms a phosphorylated enzyme)

25
Q

Pyridostigmine and Neostigmine are ______ acetylcholine esterase inhibitors.?

A

Reversible.

26
Q

Tabun Nerve Gas, Sarin Gas, and VX Nerve gas are ________ acetylcholin esterase inhibitors.

A

Irreversible

27
Q

What are the antidotes for OP poisoning called?

A

Oximes

28
Q

What are 3 HIV enzymes that are potential site for therapeutic drugs?

A

Reverse transcriptase
Protease
Integrase

29
Q

How does HIV get the proteins it needs to work?

A

It uses HIV Protease to splice up larger proteins.

30
Q

What family of proteases does HIV protease belong to?

A

Apartyl proteases.

31
Q

What are 3 requirements to design an HIV protease therapeutic agent?

A

They must have a Ki value in nanomolar or subnanomolar range

Must not target mammalian aspartyl proteases

Adequate bioavailability

32
Q

What do they base the structure of HIV protease therapeutic agents off of?

A

Physiological peptide substrate

33
Q

How do you increase the stability of HIV protease therapeutic agents?

A

You replace the amide bonds.

34
Q

Most HIV protease inhibitors have a replacement of the peptide bond by a simple _____ _____.

A

Secondary alcohol

35
Q

What is the lead HIV protease inhibitor?

A

Viracept

36
Q

What is the approach used for the development of Viracept?

A

Crystal structure of target enzyme

Computational analysis and ligand design

Organic synthesis of designed ligand

Biochemical evaluation of the ligand

37
Q

_____-based drug design is an integral part of drug discovery today.

A

Structure

38
Q

Why is there drug resistance in HIV?

A

The high mutation rate of HIV due to infidelity of RT.

39
Q

How do you treat HIV drug resistance?

A

Use combination therapy.

40
Q

Are the combination RT and protease therapeutic drugs on the market effective?

A

No, because of HIV’s mutation rate.

41
Q

Where does Maraviroc bind?

A

CCR5 instead of CXCR4

42
Q

What is a new possible therapeutic agent found in green tea and binds to CD4?

A

EGCG

43
Q

How does EGCG work?

A

It prevents the interaction between gp120 and CD4, which could be useful in combination therapy

44
Q

What other disease can EGCG be useful against besides HIV?

A

Cancer

PHS 944 (4 decks)

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