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Examen 2 Farmaco > Cholinergic System Caro > Flashcards

Cholinergic System Caro Flashcards

1
Q

The neurotransmitter of the parasympathetic nervous system

A

Acetylcholine (ACh)

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2
Q

Cholinergic and Cholinomimetic

A

Cholinergic
-neurons that release ACh and/or have receptors on which ACh synapses upon
Cholinomimetic
-Compounds that stimulate the parasympathetic nervous system

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3
Q

What are the two types of Cholinergic nerves?

A

Nicotinic
-ability to bind nicotine (ionotropic) Muscarinic
-ability to bind muscarine (metabotropic)

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4
Q

Muscarinic cholinergic agents

A

Compounds that interact with Muscarinic Acetylcholinergic Receptors (mAChR) used for:
-treat glaucoma
-treat cognitive disorders (Alzheimer’s)
-re-establish smooth muscle tone of the GI and urinary tract after surgery

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5
Q

Anticholinergic agents (mAChR antagonist)

A

Ability to reduce smooth muscle spasm
-used to treat overactive bladder

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6
Q

mAChR Stimulation

A

-leads to inhibition of adenylyl cyclase
-activation of phospholipase C (which generate secondary messengers)

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7
Q

What chemical structure should a cholinergic agent have?

A

A quaternary ammonium group (a ionic site) and a ester functional group (esteratic site)

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8
Q

Ing’s rule of 5

A

No more than 5 atoms between quaternary N and terminal H. (Esta regla no aplica a todo compuesto)

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9
Q

mAChRs subtypes and G-proteins interactions

A

-odd numbered mAChRs (M1, M3, M5) are coupled to with Gq protein (excitatory)
-even numbered mAChRs (M2 M4) are coupled to with Gi and Go proteins (Inhibitory)

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10
Q

Nicotinic Receptors (nAChRs)

A

-Found in neuromuscular junctions, adrenal medulla, and autonomic ganglia
-Play important role in myasthenia gravis
-Ionotropic that have two ACh binding sites which shows positive cooperativity

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11
Q

Acetylcholinesterase (AChE)

A

Break down ACh. Elimina el grupo Ester

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12
Q

Why can’t choline cross the Blood-Brain Barrier but its phosphate counterparts can?

A

Colina es muy soluble en agua por su carga, tamaño y logP. Para cruzar, se observar la estrategia de prodroga.

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13
Q

Which structure of ACh is more stable?

A

Antiperiplanar (trans)

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14
Q

Why is ACh not able to be administered orally?

A

ACh receptors are found in different organs and can interact with Nicotinic and Muscarinic receptors (no selectivity) causing uncontrollable activation to undesired receptors.

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15
Q

Muscarinic agonist SAR

A

Methacoline
-Metilacion en carbono beta
Carbachol
-presencia de un carbamato en el grupo Ester
Bethanchol
-Metilacion en carbono beta
-presencia de un carbamato en el grupo Ester

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16
Q

non-Specific Muscarinic Agonist

A

Miostat
-acts as an agonist to mAChRs and nAChRs
-Treatment of glaucoma and ocular surgery
-Carbamate este makes it less labios to hydrolysis (long duration)

17
Q

Provocholine (methacholine chloride)

A

Specific Muscarinic agonist
-bronchial challenge test (diagnosis of asma)
-Metilacion en beta

18
Q

Urecholine (bethanecol chloride)

A

Specific Muscarinic Agonist
-used for post-surgical
-orally administrated to avoid cholinergic crisis (sobre dosis)
-carbamato y Metilacion en beta

19
Q

Salogen or Isopto Carpine (pilocarpene HCL)

A

Specific Muscarinic Agonist (M3)
-treat glaucoma and xerostomia
-hidrolisis por el Ester y no cumple regla de Ig

20
Q

Evoxac (Cevimeline Hydrochloride)

A

Specific Muscarinic Agonist
-treat xerostomia
-quinuclidine derivative
-la presencia de azufre hace que se oxide
-Metabolizado por CYP

21
Q

Acetylcholinesterase (AChE) inhibitors

A

Inhibe esta enzima por lo que se acumula ACh.
-improve muscle strength in myasthenia gravis and treat Alzheimer’s.

22
Q

AChE Structure and Function

A

-Esteratic site = serine hydrylase (Ser, his, glu)
-Anionic site = N cation binds (Trp)

23
Q

What happens when AChE is acylated?

A

It is inactive

24
Q

Carbamylated AChE

A

Reversible AChE Inhibitors
-regeneration to an active AChE by hydrolysis is much slower

25
Q

Irreversible AChE inhibitors

A

Phosphate esters inactivate AChE but if aging process occur, the functional group will be anionic and it will never me activated

26
Q

mAChR antagonist (anticholinergic agents)

A

Decrease contraction of smooth muscles, dilation of pupils, decrease secretion.

27
Q

Atropine and Scopolamine

A

Anticholinergic agents
-tiene efecto en CNS por ser lipofilicos

Examen 2 Farmaco (11 decks)

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