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Pharmacology 1 > ANS 1 (Parasympathetic) Cholinergic Agonists > Flashcards

ANS 1 (Parasympathetic) Cholinergic Agonists Flashcards

1
Q

Parasympathetic state/ acetylcholine effect and the muscarinic receptor (involved) of heart

A

Bradycardia; M2 receptor

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2
Q

Parasympathetic state/ acetylcholine effect and the muscarinic receptor (involved) of lungs

A

Bronchoconstriction; M2 receptor

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3
Q

Parasympathetic state/ acetylcholine effect and the muscarinic receptor (involved) of gastric acid secretiond

A

increased gastric secretion; M1 receptor

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4
Q

Influx of what ions causes the vesicles to fused with the plasma membrane and releases ACh

A

Ca

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5
Q

enzyme that breaks down ACh

A

Acetylcholinesterase (AChE) or cholinestrase

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6
Q

Cholinergic Agonist or Cholinergic Antagonist: Pilocarpine

A

Cholinergic Agonist

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7
Q

Cholinergic Agonist or Cholinergic Antagonist: Scopolamine

A

Cholinergic Antagonist

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8
Q

Cholinergic Agonist or Cholinergic Antagonist: Atropine

A

Cholinergic antagonist

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9
Q

Cholinergic Agonist or Cholinergic Antagonist: Succinylcholine

A

Cholinergic antagonist

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10
Q

Two general groups of cholinergic agonists based on MOA

A

Direct and indirect Acting

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11
Q

Brains, spinal cord

A

Central Nervous system

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12
Q

nerves outside the brain and spinal cord

A

Peripheral Nervous System

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13
Q

Composed of sensory neurons

Conducts signals from receptors to CNS

A

Sensory or Afferent Division

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14
Q

Composed of motor neurons

Conducts signals from CNS to effectors

A

Motor or Efferent Division

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15
Q 
conducts voluntary movement
with stimulatory effect only 
1 neuron
Neurotransmitter: ACh/nicotinic
targets skeletal muscles
A

Somatic NS

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16
Q

conducts involuntary or automatic movements
with ganglion (postsynaptic or presynaptic)- 2 neurons
with stimulatory or inhibitory effect (sympathetic or parasymathetic)
Neurotransmitter: ACh/muscarinic or NE/ Alpha or beta
targets smooth muscles glands, adipose tissues

A

Autonomic NS

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17
Q

mobilises body systems
“flight or fight” responses
“catabolic” process
Ganglia: near SPINAL CORD ( short Preganglionic & long Postganglionic fibers)
NT:(pre) ACh, (post) NE, E, dopamine
receptors: (ganglia) nicotinic, (target organ) alpha, beta, dopamine

A

Sympathetic Division/ Adrenergic

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18
Q

conserves energy
“rest and digest” responses
anaboic process
Ganglia: near TARGET ORGAN ( long preganglionic & short postganglionic fibers)
NT: (pre &post) ACh
Receptor: (ganglia) nicotinic, (target organ) muscarinic, nicotinic

A

Parasympathetic Division / Cholinergic

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19
Q

NT:

  • transmits all parasympathetic signals to end organs by binding to M (muscarinic) receptors
  • transmits both sympathetic and parasympathetic impulses fr preganglionic neurons to N (nicotinic) recpetors of postganglionic neurons
A

Acetylcholine (ACh)

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20
Q

Manifestations of Rest and Digest / Parasympathetic

A 
DUMBBELSS
Diarrhea
Urination
Mydriasis
Bradycardia
Bronchoconstriction
Emesis
Lacrimation
Salivation
Sweating

Erection

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21
Q

Enzyme needed for synthesis of ACh

A

choline acetyltransferase (acetyl coa + choline forms ACh)

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22
Q

transporter needed for choline to enter presynaptic cell needed in synthesis of ACh

A

Na-dependent choline transporter

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23
Q

Drug which inhibits ACh to be stored in vesicles

A

Vesamicol

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24
Q

ion needed for the release (exocytosis) of ACh to synapse

A

Calcium

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25
Q

acetylcholine receptor in postsynaptic cell

A

Cholinoceptor

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26
Q

enzyme that degrades ACh to acetate and choline thru hydrolysis

A

Acetylcholinesterase or Cholinesterase

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27
Q

Drug that inhibits transport of choline or synthesis of ACh

A

Hemicholinium

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28
Q 
Drug that blocks the release of ACh to synapse
 Wrinkle treatment (botox)
A

Botulinum toxin (Clostridium botulinum)

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29
Q

Location of M1

A 
exocrine glands (secretion)
autonomic ganglia (inc seizure activity)
CNS ( inc cognitive and function )
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30
Q

Location of M2

A

Heart (cardiac inhibition)
CNS (neural inhibition, inc tremors, hypothermia, analgesia)
smooth muscle (inc contraction)
Peripheral nerves ( neural inh, dec ganglionic transmission)

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31
Q

Location of M3

A 
exocrine glands ( inc secretion)
smooth muscles ( inc contraction) 
eye ( miosis, ocular accommodation)
blood vessels: endothelium ( vasodilation)
CNS
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32
Q

location of M4

A

CNS (enhanced locomotion)

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33
Q

Location of M5

A

CNS
Salivary glands
Iris/ciliary muscle

34
Q

Location of Nn or Ng (nicotinic ganglionic receptor)

A

Ganglion ( stimulation)

CNS ( neurotransmission)

35
Q

Location of Nm (Nicotinic neuromuscular junction)

A

skeletal muscle (contraction)

36
Q

2 divisions of Cholinergic agonists

A

Direct Acting and Indirect acting

37
Q

2 divisions of direct acting cholinergic agonists

A

Choline esters and Alkaloids

38
Q

Drugs under choline esters (choline bound to an acetyl derivative by an ester bond and ester bond is hydrolyzed by cholinesterase or AChE)

A 
"Mag- CAB"
Methacoline
Carbachol
ACh
Bethanecol
39
Q

Drugs under alkaloids

A 
"NAP Muna"
Nicotine
Arecoline
Pilocarpine
Muscarine
40
Q

MOA of direct acting cholinergic agonists

A

drugs directly binds to receptors

41
Q

most potent cholinergic agonist
prototype
employed to cause miosis during cataract surgery
can produce brief 10 min miosis
ester of acetic acid and choline, a quaternary amino alcohol
Muscarinic receptors (M1, M2, M3, M4, m5) and Nicotinic

A

Acetylcholine

42
Q

T/F: Acetylcholine is selective agonist for different types of cholinoreceptors and has no limited therapeutic use.

A

FALSE: ACh has both Muscarinic (1-5) and Nicotininc activity therefore, it has LIMITED therapeutic use due to lack of selectivity as an agonist for different types of cholinoreceptors.

43
Q

T/F: Acetylcholine is rapidly hydrolyzed by cholinesterases.

A

True

44
Q 
Strong muscarinic (1-3) activity (only) 
specific for GIT and bladder
inc intestinal motility after surgery
more resistant to hydrolysis
acute non-obstructive urinary retention
duration: 1hr
A

Bethanechol

45
Q

ester of carbamic acid
has both muscarinic (1-5) and nicotinic activity
tx of pilocarpine-resistant open-glaucoma
more resistant to AChE/hydrolysis
duration: 1hr

A

Carbachol

46
Q

has muscarinic (1-3) and weak nicotinic activity
Methacoline challenge: diagnosis of asthma
reserves for px with Normal Lung Function tests but has Positive asthma symptoms
measures hyperresponsiveness / hypersensitivity of the lungs
Result: admin of initial, secondary and the highest dose
In its highest dose:
no asthma if FEV= 20% or higher
asthma/hypersensitive lungs if FEV> 20%

A

Methacholine (Provocholine)

“provoc” Provoking bronchial asthma

47
Q

T/F: Alkaloids are not metabolized by AChE.

A

TRUE

48
Q

DOC for glaucoma
exhibits muscarinic (1-3) activity
can cross blood-brain barrier

A

Pilocarpine (alkaloid fr Pilocarpus sp.)

49
Q

muscarinic (1-3) ; no therapeutic use

A

Muscarine

50
Q

muscarinic (1-3) and nicotinic activity

Potential for Alzheimer’s

A

Arecoline

51
Q

aqueous humor production exceeds outflow, resulting in increased intraocular pressure
most common type of glaucoma

A

Open-angle Glaucoma

52
Q

(glaucoma-related) ______ causes constriction of the sphicter muscle which surrounds the iris. The iris is drawn away from the Schlemm canal, enhancing outflow of aqueous humor.

A

Acetylcholine

53
Q

M(1-5) and nicotinc receptors

A

ACh,

Carbachol

54
Q

M(1-3) and nicotinic receptors

A

Methacoline,

Arecoline

55
Q

M (1-3) receptors

A

Bethanechol,
Pilocarpine,
Muscarine

56
Q

Divisions under Indirect acting

A

Organophosphates
Carbamates
Quaternary Amine (Edrophonium)

57
Q

highly lipid-soluble liquids
have very high affinity for the active site of AChe forming phosphorylated enzyme
inactivates enzyme (AChE) thru phosphorylation

A

Organophosphates

58
Q

MOA of indirect acting cholinergic agonists

A

cholinesterase inhibitors

59
Q

Drugs under Organophosphates

A

Isofluorophate
Echothiophate
Malathion, Parathion
Tabun, Sarin, Soman

60
Q

Chronic tx of open-angle glaucoma

duration: 1 week
route: eye drops

A

Isofluorophate (DFP: di-isoflurophate)

61
Q

tx of open-angle glaucoma
duration: 3-7 d
Route: eye drops

A

Echothiophate

62
Q

insecticide/pesticides
No clinical use
Active metabolites: Malaoxon, Paraoxon

A

Malathion, Parathion

63
Q

Used in 1945 as delousing powder and used with soldiers to combat the spread of life thratening diseases like typhus and malaria

A

DDT (Dichlorodiphenyltrichloroethane)

64
Q

nerve gases used in chemical warfare
poisons of war
penetrates skin, eyes, lungs
loss of consciousness, seizures , apnea, and death

A

Tabun(GA), Sarin(GB), Soman (GD)

65
Q

antidote for organophosphate toxicity or “cholinergic crisrs”

A

2-PAM (Pralidoxime chloride) ,

Atropine

66
Q

antidote for organophosphate toxicity that inactivates AChE thru dephosphorylation; does not cross the blood brain barrier

A

2-PAM (Pralidoxime chloride)

67
Q

antidote for organophosphate toxicity that is a prototype anticholinergic agent and a muscarinic blocker

A

Atropine

68
Q

Carbamyl ester inhibitors
MOA: carbamyl group prevents ACh from binding to the active site of AChE for a period of min to hours and forms CARBAMYLATED enzyme (can be decarbamlated)

A

Carbamates

69
Q

Drugs under carbamates

A

Physostigmine
Neostigmine
Pyridostigmine
Carbamate Insecticides (CAP)

70
Q

for intestinal and bladder atony (no muscle tone)
mitotic agent for open- angle glaucoma
tx of overdoses of anticholinergic drugs ( atropine, TCA, Phenothiazine)
duration: 6-12 h

A

Physostigmine (Eserine)

71
Q

Physosstigma venenosum
can enter and stimulate the CNS
inhibit AChE in th eCNS
stimulates muscarinic, nicotinic sites of ANS + nicotinic of NMJ

A

Physostigmine (Eserine)

72
Q

tx of Myasthenia Gravis (attacking self tissues) , paralytic ileus, or atony of the urinary bladder
antidote for Tubocurarine poisoning and other neuromuscular blocking agents
direct agonist at NM
more polar and does not enter CNS
duraion: 3-6h

A

Neostigmine (Prostigmin)

73
Q

Symptoms of Myasthenia gravis

A 
drooping eyelid
difficulty in swallowing
slurred speech
weak muscles
weak breathing muscles
74
Q

MOA of Neostigmin tx for MG:

A

AChE inh prevent ACh degradation: which increases the probability that remaining receptors will bind ACh

75
Q

direct agonist activit at NM
tx of MG (other than Neostigmine)
duration: 4h

A

Pyridostigmine (Mestinon)

76
Q

Enumerate: Carbamate insecticides

A 
CAP
Carbaryl
Aldicarb
Propoxur
increases ACh
77
Q

competitive AChE, which contains QUATERNARY ammonium
reversible binding to AChE
used for Myasthenia grvis diagnosis (Tensilon test)
short duration: 1-2h

A

Edrophonium (Tensilon)

78
Q

Effect of Cholinergic antagonist

A

dec ACh

79
Q

3 Divisions of Cholinergic Antagonists

A

Muscarinic Blockers
Ganglion BLockers
Neuromuscular Blockers

80
Q

MOA of Muscarinic BLockers

A

blocks the binding of ACh to muscarinic receptors

Pharmacology 1 (3 decks)

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