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PHA 037 - PHARMACOLOGY > SAS 9 - CHOLINERGIC ANTAGONIST > Flashcards

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

A

M4 & M5

22
Q

a prototype of muscarinic antagonist

A

Atropine

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
Q

how many percent of unchanged atropine drug is excreted in the urine?

A

50%

26
Q

what is the MOA of Atropine?

A

reversibly blocks muscarinic receptors

27
Q

what is the effect of atropine blocking the muscarinic receptor?

A

inhibition of IP3 release and inhibition of adenylyl cyclase

28
Q

what are the muscarinic receptors that atropine does not distinguish?

A

M1-M3

29
Q

what is the low dose of scopolamine does to the CNS?

A

Drowsiness and amnesia

30
Q

what is the low dose of scopolamine does to the CNS?

A

Drowsiness and amnesia

31
Q

how does acetylcholine transmission causes parkinson?

A

when acetylcholine production is unbalanced with dopamine production it can lead to impair motor command

32
Q

what is cycloplegia?

A

it is when the ciliary muscle loses its ability to contract - loss of accommodation

33
Q

what are the effects of parasympatholytic drugs in the eyes?

A

> mydriasis
cycloplegia
sandy eyes

34
Q

what is the condition that is fatal for children done by atropine?

A

Atropine fever

35
Q

what is the parasympathetic drug that is effective for motion sickness (increases blood levels over 48-72 hours)

A

Scopolamine

36
Q

what type of administration is best for opthalmoscopic examination?

A

ointment or eyedrops

37
Q

what are the synthetic analog of atropine that is used as an inhalational drug to treat COPD

A

Ipratropium tiotropium, aclidinium, umeclidinium

38
Q

used to relieve bladder spasms after urologic surgery (~M3 receptor)

A

Oxybutynin

39
Q

non-selective and comparable to oxybutynin

A

Trospium

40
Q

more M3 selective and requires only one daily dosing

A

Darifenacin and Solifenacin

41
Q

antimuscarinic agent that is only approved in Europe but not in USA

A

Propiverine

42
Q

What are the contraindications of Muscarinic antagonist

A

> Angle-closure glaucoma
history of prostatic hyperplasia
Gastric ulcer
Children in danger with malignant hyperthermia

43
Q

what is ganglion-blocking drugs?

A

it blocks the ganglion in the sympathetic and parasympathetic

43
Q

what is ganglion-blocking drugs?

A

it blocks the ganglion in the sympathetic and parasympathetic

44
Q

ALL ganglion-blocking drugs are SYNTHETIC AMINES

A

ALL ganglion-blocking drugs are SYNTHETIC AMINES

45
Q

a ganglion-blockers that depolarizes neuromuscular blocking agent

A

Decamethonium

46
Q

what is the MOA of ganglion blocker?

A

binds to nicotinic receptor

47
Q

ganglion blocker can be surmounted

A

ganglion blocker can be surmounted

48
Q

ganglion-blocking drugs are now classified as

A

nondepolarizing competitive antagonist

49
Q

what is the drug in the ganglion-blocking that produces MOST OF ITS BLOCKING ACTION

A

Hexamethonium

50
Q

blocks the nicotinic receptors and be as possible adjunct with the transdermal nicotine patch

A

Mecamylamine

PHA 037 - PHARMACOLOGY (19 decks)

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