Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Examen 2 Farmaco > Muscarinic Agonist > Flashcards

Muscarinic Agonist Flashcards

1
Q

What is the rate limiting step of Cholinergic Neurotransmission?

A

Choline Acetyltransferase
-from choline and acetyl CoA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Which enzyme degrades ACh?

A

Acetylcholinesterase (AChE)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

True or False: M4 are autoreceptors. (Located on or close to the axon terminal)

A

True
-ACh released from parasympathetic neurons interacts with M4 receptors to inhibit ACh release.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

True or False: ACh influences the release of NE from sympathetic neurons by acting on presynaptic M4 receptors. This is known as an Heteroreceptor.

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Why is ACh’s penetration to the CNS is limited when administered systemically?

A

The presence of butyrylcholinesterase in the blood degrades ACh. This also limits the targets it reaches.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Which organs are the Muscarinic receptors found?

A

M1-CNS
M2-Cardiovascular system (negative chrono and ino; vasodilation by M3)
M3-Periphery (Gq)
-Constriction and secretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What should we know about nitric oxide?

A

Produces relaxation in the endothelial cell and contraction in the smooth muscle cell.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Methacoline

A

-Hydrolyzed by AChE
-Lacks Nicotinic actions
-Poor absorption, does not cross BBB
-For asthma and COPD diagnosis
-Side effect: hypotension and Bradycardia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Carbachol

A

-Not hydrolyzed by AChE
-Muscarinic and Nicotinic actions
-Can cause release of epinephrine from adrenal medulla
-Treat glaucoma and cataract surgery (rarely)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Bethanechol

A

-Not hydrolyzed by AChE
-Lacks Nicotinic actions
-Treats Non-obstructive urinary retention and paralytic ileus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Contraindications of Choline esters

A

-Asthma
-Hyperthyroidism
-Coronary insufficiency
-Acid-peptic disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Parasympathetic activation in ventricular fibrillation in the setting of cardiac ischemia

A

Antiarrhythmic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Pilocarpine

A

-Cross BBB
-Hydrolysis by AChE
-Only Muscarinic actions
-less potent than ACh
-Treat xerostomia (promotes tears)
-Drug of choice in emergencies to reduce intraocular pressure.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Which drug has been shown to have less side effects (sweating) than pilocarpine in patients with sjogrens?

A

Cevimeline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Reversible AChE inhibitors

A

-Hydrolyzed by AChE but much more slowly than ACh,
-Contains Edrophonium and it’s a competitive inhibitor of AChE.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Which compounds are irreversible AChE inhibitors?

A

Organophosphate
-Enhanced by aging

17
Q

Aging of Organophosphate

A

-the loss of one of the alkyl groups in the phosphate group. Cause inactivation of AChE.

18
Q

What can be given before aging to break phosphorus-enzyme bond?

A

Pralidoxime

19
Q

What happens to neuromuscular junctions at low therapeutic concentrations?

A

Increase strength of contraction

20
Q

What happens to neuromuscular junctions at High therapeutic concentrations?

A

Accumulation of ACh causing paralysis.

21
Q

Myasthenia Gravis

A

Enfermedad autoinmune que enlaza anticuerpos a receptores Nicotinicos.
Causa:
-ptosis (no levanta párpado)
-diplopia (tiene visión doble)
-Problemas para hablar y tragar
Diagnóstico: Edrophonium test

22
Q

Medicamentos para Myasthenia Gravis

A

Pyridostigmine, Physostigmine y Neostigmine

23
Q

Edrophonium

A

Short-acting AChE inhibitor
-Diagnosis of Myasthenia Gravis

24
Q

Neostigmine

A

For Atony and Myasthenia gravis
-Cannot cross BBB

It’s like Pyridostigmine but this last one is longer acting and for chronic management of Myasthenia Gravis.

25
Q

Which two Acetylcholine Release Modulators are K Channel Antagonist?

A

Amifampridine and 4-aminopyridine

26
Q

Physiotigmine

A

Intermediate-acting AChE Inhibitor
-to treat glaucoma (stimulates CNS) but pilocarpine is more effective
-treat Anticholinergic overdose (antídoto)
-Overdose can cause Cholinergic syndrome (DUMBELS)
-Its metabolite (eseroline) acts as an opioid agonist.

27
Q

What are AChE inhibitors that treat Alzheimer?

A

Tacrine
Donepezil
Rivastigmine
Galantamine

28
Q

Indirect-acting cholinergic agonist Anticholinesterases (Irreversible)

A

Sarin, Soman, and Tabun
-Many of organophosphates are highly lipid-soluble liquids and is distributed to all the body excepts Echothiophate

29
Q

Echothiophate

A

Action: cholinergic stimulation, paralysis of motor function
-To treat glaucoma provoking intense miosis
-Atropine can reverse its effect

30
Q

Parathion and Malathion

A

Both are prodrugs use as insetcides but parathion is more dangerous.

31
Q

Organophosphates Antidotes

A

-Atropine is an mAChR antagonist
-Reactivators: separate inhibitor from AChE (Dephosphorylate)
-Pralidozime (PAM)

32
Q

Pralidoxime (PAM)

A

Its must be used immediately, no more than 36 hours of exposure

Can reactivate inhibited Acetylcholinesterase before aging except in the CNS since it does not cross it.

Examen 2 Farmaco (11 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions