SAS 9 - CHOLINERGIC ANTAGONIST Flashcards

1
Q

What are “the” antinicotinic drugs?

A

Ganglion blockers and Neuromuscular junction blockers

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2
Q

Anti-muscarinic drugs is also known as

A

parasympatholytic

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3
Q

Why is anti-muscarinic drug is also called as parasympatholytic?

A

because it has the capability to inhibit the effect of parasympathetic autonomic discharge.

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4
Q

At what plant do Atropine can be found?

A

Atropa belladonna (deadly night shade), Datura stramonium (Jamestown weed, and Sacred Datura,thorn apple)

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5
Q

What is the generic name of the Atropine?

A

hyoscyamine

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6
Q

At what plant do scopolamine is found?

A

Hyoscyamus niger or herbane (its l-stereoisomer)

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7
Q

what is the l-stereoisomer of the hyoscyamus niger?

A

herbane

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8
Q

At what number is the l-stereoisomer alkaloids more potent than d-stereoisomer?

A

100x

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9
Q

How will it take for the atropine to be distributed in CNS?

A

30mins - 1 hour

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10
Q

How long will it take for a fast-acting formulation of atropine to take?

A

2 hours

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11
Q

How long will it take for a long-acting formulation of atropine to take?

A

13 hours

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12
Q

It is the eye that is longer to be affected by alkaloids, how many hours does it last?

A

72 hours or more

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13
Q

What is the MOA of Atropine?

A

It blocks the cholinomimetic actions of muscarinic receptors

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14
Q

What is the effect of cholinergic antagonists for muscarinic receptors?

A

prevents the release of IP3 and inhibition of adenylyl cyclase

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15
Q

Where is the most sensitive tissue that is affected by antimuscarinic drugs? SSB

A

Salivary glands, sweat glands, bronchial

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16
Q

Atropine has little to CNS but at high doses of scopolamine it can cause…

A

Excitability, irritability, hallucinations, and coma

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17
Q

a drug that has fewer adverse effects than atropine in lessening digestion

A

telenzepine

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18
Q

a muscarinic receptor that is found in the CNS neurons, sympathetic postganglionic cell bodies, and many presynaptic sites

A

M1

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19
Q

a muscarinic receptor that is found in the myocardium, smooth muscle organs, and
some neuronal sites

A

M2

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20
Q

a muscarinic receptor that is found in the effector cell membranes, especially
glandular and smooth muscle cells.

A

M3

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21
Q

a muscarinic receptor that plays a greater role in the CNS than in the periphery

22
Q

a prototype of muscarinic antagonist

23
Q

what are the street names of the Datura stramonium?

A

Jamestown weed, sacred Datura, or thorn apple

24
Q

parasympatholytic: NATURAL ALKALOIDS are MOSTLY __________ drugs that are well absorbed in the ______ and __________.

A

> Natural alkaloids are mostly tertiary agents
is well absorbed in the gut and conjunctival membranes.

25
how many percent of unchanged atropine drug is excreted in the urine?
50%
26
what is the MOA of Atropine?
reversibly blocks muscarinic receptors
27
what is the effect of atropine blocking the muscarinic receptor?
inhibition of IP3 release and inhibition of adenylyl cyclase
28
what are the muscarinic receptors that atropine does not distinguish?
M1-M3
29
what is the low dose of scopolamine does to the CNS?
Drowsiness and amnesia
30
what is the low dose of scopolamine does to the CNS?
Drowsiness and amnesia
31
how does acetylcholine transmission causes parkinson?
when acetylcholine production is unbalanced with dopamine production it can lead to impair motor command
32
what is cycloplegia?
it is when the ciliary muscle loses its ability to contract - loss of accommodation
33
what are the effects of parasympatholytic drugs in the eyes?
>mydriasis >cycloplegia >sandy eyes
34
what is the condition that is fatal for children done by atropine?
Atropine fever
35
what is the parasympathetic drug that is effective for motion sickness (increases blood levels over 48-72 hours)
Scopolamine
36
what type of administration is best for opthalmoscopic examination?
ointment or eyedrops
37
what are the synthetic analog of atropine that is used as an inhalational drug to treat COPD
Ipratropium tiotropium, aclidinium, umeclidinium
38
used to relieve bladder spasms after urologic surgery (~M3 receptor)
Oxybutynin
39
non-selective and comparable to oxybutynin
Trospium
40
more M3 selective and requires only one daily dosing
Darifenacin and Solifenacin
41
antimuscarinic agent that is only approved in Europe but not in USA
Propiverine
42
What are the contraindications of Muscarinic antagonist
> Angle-closure glaucoma > history of prostatic hyperplasia > Gastric ulcer > Children in danger with malignant hyperthermia
43
what is ganglion-blocking drugs?
it blocks the ganglion in the sympathetic and parasympathetic
43
what is ganglion-blocking drugs?
it blocks the ganglion in the sympathetic and parasympathetic
44
ALL ganglion-blocking drugs are SYNTHETIC AMINES
ALL ganglion-blocking drugs are SYNTHETIC AMINES
45
a ganglion-blockers that depolarizes neuromuscular blocking agent
Decamethonium
46
what is the MOA of ganglion blocker?
binds to nicotinic receptor
47
ganglion blocker can be surmounted
ganglion blocker can be surmounted
48
ganglion-blocking drugs are now classified as
nondepolarizing competitive antagonist
49
what is the drug in the ganglion-blocking that produces MOST OF ITS BLOCKING ACTION
Hexamethonium
50
blocks the nicotinic receptors and be as possible adjunct with the transdermal nicotine patch
Mecamylamine