Drugs And Parasympatheitc NS SEM2 Flashcards

1
Q

What is muscarine

A

A direct-acting acetylcholine receptor agonist

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2
Q

What can nicotinic receptors which are ligand gated ion channels be classified into

A

Skeletal NMJ
Ganglionic
Neuronal CNS

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3
Q

What system do muscarinic Ach receptors work with

A

The parasympathetic nervous system (and CNS)

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4
Q

Where does the pre-ganglion neuron start from and what does it release

A

Starts from the spinal cord and releases ACh which activates nicotinic acetylcholine receptors on the parasympathetic ganglion

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5
Q

What is activated following the signal relayed to another neurone in the parasympathetic ganglion

A

ACh released again and activates muscarinic ACh receptors on an effector organ (glands or smooth muscle)

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6
Q

Where does the pre-ganglionic neurone originate from and what does it release

A

Originates at the spinal cord and releases ACh to activate nicotinic ACh receptors in the sympathetic chain ganglion

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7
Q

What occurs after ACh receptors in the sympathetic chain ganglion have been acivated

A

Signal transmitted to another neurone that releases norepinephrine (NA) activating adrenoceptors on target effector organ => fight or flight

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8
Q

What can muscarinic receptors activate

A

Activate phospholipase C leading to the production of IP3 and diacyle glycerol - M1, M2, M3
Activate K+ channels - M2

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9
Q

What can muscarinic receptors inhibit

A

Inhibit adenylate cyclase causing a decrease in the levels of cAMP - M2, M4
Inhibit Ca2+ channels - M2

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10
Q

What do the terms parasympathomimetic and cholinomimetic mean

A

Drugs that mimic the effects of the parasympathetic nervous system

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11
Q

What are properties of direct acting drugs of cholinomimetic drugs

A

Mainly have muscarinic effects at end effectors
Most do not have CNS effects

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12
Q

What are properties of indirect acting drugs of cholinomimetic drugs

A

Increase transmission at all cholinergic junctions therefor have muscarinic, ganglionic and skeletal muscle effects
Have CNS effects

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13
Q

What are properties of indirect reversible acting agonist

A

Reversible inhibitors of ACh-esterase can increase the concentration of ACh and prolong lifetime in the synapse/junction

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14
Q

What are properties of indirect irreversible acting agonists

A

Irreversible inhibitors of ACh-esterase increase concentration of ACh and prolong lifetime in the synapse/junction

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15
Q

What are examples of reversible inhibitors of ACh-esterase

A

Physostigmine
Neostigmine

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16
Q

What are examples of irreversible inhibitors of ACh-esterase

A

Organophosphates

17
Q

What are the therapeutic uses of antimuscarinics

A

Pre-anaesthetic medication
Ophthalmological uses
Gastrointestinal antispasmodic agents
Treatment of poisoning by cholinomimetics

18
Q

What are types of sympathetic neurotransmitters

A

Noradrenaline
Adrenaline

19
Q

What occurs when noradrenaline (NA) travels to thee effector organ

A

NA interacts with adrenoceptors on the effector organ, initiating response typically being:
increasing heart rate
Dilating airways
Mobilising energy stores

20
Q

What occurs during the process of neuronal uptake 1 of noradrenalin re uptake

A

The majority of NA is taken back into the pre-synaptic neurone via a high affinity uptake system known as uptake 1

21
Q

What occurs during the process of extra-neuronal uptake 2 of noradrenalin re uptake

A

NA that escapes uptake 1 can be bysorbed by non-neuronal cells e.g glial cells
Has lower affinity for NA but maximum rate meaning it can handle larger amounts of NA, adrenaline and isoprenaline

22
Q

What occurs during the process of the metabolism of noradrenaline (NA)

A

Monoamine oxidase (MAO) breaks down NA into aldehydes which are further metabolised to acids or non-active forms which can be excreted

23
Q

What is the cellular response of alpha-1 (α1) adrenoceptors

A

IP3 induces the release of calcium ions from intracellular stores leading to the contraction of smooth muscle

24
Q

What is the cellular response of alpha-2 (α2) adrenoceptors

A

The reduced cAMP levels lead to inhibition of transmitter release

25
Q

What is the cellular response of beta ( β 1-3) adrenoceptors

A

β1: increases heart muscle contraction

β2 + β3: relaxation of smooth muscle and glycogenolysis

26
Q

What does guanethidine do when accumilates in veiscles

A

Displaces noradrenaline (NA)

27
Q

What is the result of guanethidine accumilating in the vesicle and displacing NA

A

Displacement of NA leads to guanethidine preventing the release of NA into the synaptic cleft therefor reduces the amount of NA available to activate adrenergic receptors