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Therapeutics > Cholinergics > Flashcards

Cholinergics Flashcards

1
Q

Cholinoreceptors

A

-nicotinic (NM, NN)
-muscarinic (M1, M2, M3)

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2
Q

Nm receptor

A

-skeletal muscle

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3
Q

NN receptor (neural)

A

-postganglionic
-adrenal medulla

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4
Q

Nicotinic receptor responses

A

-depolarization
-ligand opening of Na/K

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5
Q

Muscarinic receptor responses

A

QIQ

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6
Q

M1 receptor

A

-postganglionic
-depolarization
-GQ mech

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7
Q

M2 receptor

A

-heart
-inhibition
-G1 activation

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8
Q

M3 receptor

A

-smooth muscles (contract)
-exocrine glands (secrete)
-endothelium (relax)
-Gq activation

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9
Q

acetylcholine has higher affinity for which receptor

A

muscarinic

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10
Q

acetylcholine biosynthesis and neurotransmission

A
  1. choline transported to presynaptic nevere terminal by CHT
  2. Ach synthesize from choline and acetyl-CoA by ChAT
  3. ACh transported to storage vesicle by VAT
  4. action potential opens gated channels and increases calcium, fusion of vesicles with the surface membrane results in the release of ACh
    -ACh binds to cholinoreceptors on post synaptic cell
  5. ACh action terminated by metabolism by AChE
  6. auto receptors and receptors on presynaptic nerve end transmitter release
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11
Q

sodium-dependent choline transporter (CHT)

A

-transport choline to presynaptic nerve terminal
-inhibited by hemicholinium

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12
Q

choline acetyltransferase (ChAT)

A

-forms ACh from choline and acetyl coA

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13
Q

vesicle-associated transporter (VAT)

A

-carries ACh to storage vesicle
-inhibited by vesamicol

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14
Q

botulinum toxin

A

-botox
-block release of ACh

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15
Q

acetylcholinesterase (AChE)

A

-metabolizes ACh

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16
Q

Cholinergic agents

A

-acetylcholine
-parasympathetic

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17
Q

Parasympathetic direct agonist

A

-activate cholinoceptors
-muscarinic receptor agonists
-choline esters and alkaloids

18
Q

PSNS indirect agonist

A

-stimulate ACh release
-inhibit AChE
-reversible or irreversible

19
Q

PSNS antagonists

A

-direct or indirect
-many drug side effects

20
Q

Muscarinic AGONIST effect on heart

A

-M2
-DECREASE HR, conduction, and force

21
Q

muscarinic agonist effect on exocrine glands

A

-M3 increase secretion
-lachrymal, tracheobronchial, salivary, digestive, sweat

22
Q

muscarinic agonist effect on smooth muscles

A

-M3 increase contraction
-M2 inhibit relaxation

23
Q

muscarinic agonist effect on sphincters

A

-M3
-relaxation

24
Q

Muscarinic Agonist effects on CNS

A

-not all agonist can access CNS
-mostly M1 receptor
-tremor, hypothermia, increased locomotor activity, improved cognition

25
Q

Direct acting cholinergic receptor agonists: esters

A

-ACh
-methacholine
-carbachol
-bethanechol

26
Q

Direct acting cholinergic receptor agonists: alkaloids

A

-muscarine
-pilocarpine

27
Q

Mushroom poisoning (muscarinic agonists)

A

-bradycardia
-nausea, cramps
-bronchoconstriction
-salivation
-visual disturbances
-sweating (SNS)
-hypotension (SNS)

28
Q

charged muscarine

A

does not cross BBB well

29
Q

Pilocarpine

A

-promote sweating, urine, salivation
-treat gluacoma (outflow aq humor = decrease pressure)

30
Q

Xerostomia

A

-dry mouth
-treat with pilocarpine (M3)

31
Q

Sjogren’s syndrome

A

-autoimmune disorder mostly women
-reduced salivary gland secretions

32
Q

Muscarinic effect on cardiovascular

A

-fall in BP, HR
-M2

33
Q

muscarinic agonist effect on M3

A

-GI (muscle contract, sphincter relax)
-bladder
-eye (miosis)
-sweating (increase)

34
Q

ACh clinical use

A

-Muscarinic and nicotinic receptors
-cholinesterase sensitive
-use for miosis during surgery

35
Q

Carbachol clinical use

A

-muscarinic and nicotinic receptor
-use for miosis during surgery and gluacoma

36
Q

Pilocarpine clinical use

A

-muscarinic receptor
-glaucoma
-dry mouth

37
Q

bethanechol

A

-muscarinic receptor
-urinary retention
-GI stimulation

38
Q

Varencicline clinical use

A

-nicotinic receptor
-smoking cessation

39
Q

Side effects of muscarinic agonists

A

-Diarrhea
-Urination
-Miosis
-Bradycardia
-Bronchoconstriction
-Emesis
-Lacrimation
-Salivation + Sweating (SNS effect)

40
Q

Methacholine clinical use

A

-provacative test for hyperactive airways

Therapeutics (78 decks)

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