Cholinergic Agonist Flashcards

1
Q

Name the neurons which use Ach as neurotransmitter

A
  1. Preganglionic fibres terminating in Adrenal Medulla.
  2. The autonomic ganglia ( both parasympathetic and sympathetic)
  3. The post ganglionic fibers of the parasympathetic division.
  4. The postganglionic sympathetic division of sweat glands.
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2
Q

Name Direct acting Cholinergic Agonists

A
Ach
Bethanechol
Carbachol
Cevimeline
Pilocarpine

(Aisay beth Kr sewiyan pilo)

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3
Q

Indirect Cholinergic Agonists reversible

A
Ambenonium
Donepezil
Galantamine
Neostigmine
Pyridostigmine
Physostigmine
Rivastigmine 
Tacrine

(Aam do, galay nai paro, phr rivaj takrain.)

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4
Q

Indirect Cholinergic Agonist irreversible.

A

Echothiophate

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5
Q

Reactivation of Acetylcholinesterase

A

Pralidoxime

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6
Q

Cholinergic neurons also innervate the muscles of -

____ cells

A

Somatic

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7
Q

Patients with Alzheimer disease have a significant loss of ______ neurons in the temporal lobe and entorhinal cortex.

A

Cholinergic

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8
Q

Most of the drugs to treat Alzheimer’s disease are

A

Acetylcholinesterase inhibitors

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9
Q

Neurotransmitter in Cholinergic neurons involve six sequential steps:

A
  1. Synthesis
  2. Storage
  3. Release
  4. Binding of Ach to receptor
  5. Degradation of neurotransmitter in the synaptic cleft
  6. Recycling of choline and acetate
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10
Q

What is the synaptic cleft?

A

The space b/w nerve endings and Adjacent receptors located on nerves or effector organs

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11
Q

____ is transported from the extracellular fluid into the cytoplasm of the cholinergic neuron by energy dependant carrier system that co transports Sodium.

A

Choline

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12
Q

Drug that can inhibit the transport of Choline

A

Hemicholinium

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13
Q

Choline has a quaternary nitrogen and carries a permanent ____ charge

A

Positive

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14
Q

The uptake of chine is a _____ step in Ach synthesis.

A

Rate limiting step

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15
Q

________ catalyzes the reaction of choline with acetyl coenzyme A (CoA) to from ACh in cytosol

A

Choline acetyl transferase

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16
Q

Acetyl Coa is derived from mitochondria and produced by:

A

Pyruvate Oxidation

Fatty acid Oxidation

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17
Q

ACh is packed and stored into _______ by an active transport process coupled to the efflux of protons.

A

Presynaptic Vesicles

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18
Q

The neurotransmitter in vesicles appear as beadlike structures, known as

A

Vericosities

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19
Q

Explain release of ACh

A
  1. Action potential propagated by voltage sensitive sodium channel arrives at nerve ending
  2. Voltage sensitive Calcium channels on presynaptic membrane open.
  3. Increase in intracellular Calcium conc.
  4. Elevated Ca levels promote fusion of synaptic vesicles with cell membrane.
  5. ACh released in synaptic space.
20
Q

Release of ACh can be blocked by

A

Botulinum Toxin

21
Q

Toxin in black widow venom causes:

A

causes all ACh stored in synaptic vesicles to empty into synaptic gap

22
Q

Post synaptic Cholinergic receptors on irgan surface are divided into:

A

Muscarinic rec

Nicotinic rec

23
Q

AChE decomposes ACh to

A

Acetate & Choline

24
Q

Butyryl cholinesterase

A

Pseudocholinesterase

Does not play significant role in ACh termination

25
Q

What is recycling of Choline

A

Choline may be captured by a sodium coupled high affinity uptake system that takes the molecule back into the neuron. They are again acetylated to ACh

26
Q

Muscarinic receptors belong to _____ of protein Coupled Receptors.

A

Class G

27
Q

In addition to ACh, Muscarinic rec also show affinity for

A

Muscarine

An alkaloid, in certain poisonous mushrooms

28
Q

Muscarinic rec show weak affinity for

A

Nicotine

29
Q

classes of Muscarinic receptors

A
M1
M2
M3
M4
M5
29
Q

classes of Muscarinic receptors

A
M1
M2
M3
M4
M5
30
Q

All 5 classes of M rec are found on

A

Neurons

31
Q

M1 rec is specifically found on:

A

Gastric Parietal Cells

32
Q

M2 rec found on

A

Cardiac cells & Smooth muscles

33
Q

M3 rec found on

A

Bladder
Exocrine Gland
Smooth Muscle

34
Q

At High conc. Muscarinic drugs may show some activity on

A

Nicotinic receptor

35
Q

Pirnzepine is ______receptor antagonist

A

M2

36
Q

On rapid infusion , Pirenzepine produces the following side effect

A

Reflex Tachycardia

37
Q

Darifenacin is a competitive M3 antagonist used for

A

Overactive Bladder

38
Q

At present no clinically important agents interact solely with:

A

M4 & M5

39
Q

Nicotinic receptor is composed of ___ units

A

5

40
Q

Nicotinic rec function as a

A

ligand gated ion channel

41
Q

Nicotine at low concentration ____ and at high concentration ____ the nicotinic rec.

A

Stimulates,

Block

42
Q

Nicotinic rec are located in

A

CNS
Adrenal Medulla
Autonomic ganglia
Neuromuscular junction NMJ

43
Q

Ganglionic rec are selectively blocked by

A

Hexamethonium

44
Q

NMJ rec are specifically blocked by

A

Tubocurarine