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pharma By Cie > Cholinoceptor Activating and Cholinesterase INhibiting drugs > Flashcards

Cholinoceptor Activating and Cholinesterase INhibiting drugs Flashcards

1
Q

Cholinomimetic (direct-acting, muscarinic) that Act on both M and N receptors. Activates M1-M3
receptors in all peripheral tissues.

A

Acetylcholine

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2
Q

no Nicotinic action, resistant to

AChE, just like carbachol and bethanechol)

A

Methacholine

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3
Q

Results to increased secretion, smooth muscle contraction (except in vascular smooth muscles where it causes relaxation) and changes in heart rate; very short-lived duration of action: 5-30sec, rapidly hydrolyzed by AChE

A

Acetylcholine

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4
Q

Cholinomimetic (direct-acting, muscarinic that act on both muscarinic and nicotinic
action

A

Carbachol

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5
Q

Activates muscarinic (M1-M3) receptors. Act on M
receptors only.
It is used for Bladder and bowel atony (post-surgery or spinalcord injury), Congenital megacolon

A

Betanechol

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6
Q

are carbamic acid estersand are resistant to hydrolysis of AChE,

A

Betanechol and Carbachol

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7
Q

used for glaucoma, used as miotic.

A

CArbachol

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8
Q

an indirect acting cholinomimetic and is also

another drug useful for bladder and bowel atony.

A

Neostigmine

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9
Q

Precaution using cholinimimetics

A

you must be certain that your patient doesn’t have mechanical obstruction to outflow. Because administration of cholinomimetics in a patient with bladder and bowel atony will worsen obstruction.

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10
Q

Activates muscarinic (M3) receptors in ciliary muscle
(causing contraction of ciliary body to facilitate
aqueous humor outflow and diminish its rate of
secretion) and salivary glands (increasing salivation)

A

PILOCARPINE

CEVIMELINE [C] (M3 selective)

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11
Q

Treatment Glaucoma, Sjögren syndrome, Sicca syndrome

A

PILOCARPINE

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12
Q

SE of Pilocarpine

A

Miosis, Blurring of vision (due to cyclospasm),

Increased salivation, Hypertension

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13
Q

Interesting exception to the rule for

pilocarpine

A

for Pilocarpine, hypertension maybe seen

after a brief period of hypotension due to the activation of sympathetic postganglionic M1 receptors

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14
Q

What is Sjorgen Syndrome

A

autoimmune disorder characterized by triad of
• Xerostomia (Dry Mouth)
• Xerophthalmia (Dry Eyes)
• Rheumatoid Arthritis

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15
Q

Selective partial agonist at nicotinic

receptors; DOA 12-24h

A

VArenicline

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16
Q

NIcotine as drug

A

MOA: Activates nicotinic Ach receptors (Nn and Nm)
Uses: Smoking Cessation
SE: Generalized ganglionic stimulation (hypertension,
tachycardia, nausea, vomiting, diarrhea)

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17
Q

Type of mushroom that can cause MUscarinic toxicity

A

mushrooms (genus: Inocybe)

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18
Q

Sign and symptoms for Muscarinic toxicity

A

• CNS stimulation
• EYE: miosis, spasm of accommodation
• LUNGS: bronchoconstriction
• GIT/GUT: excessive gastrointestinal and genitourinary smooth muscle activity
• Increased secretory activity (sweat glands, airway,
gastrointestinal tract, lacrimal glands)
• Vasodilation

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19
Q

Treatment for Muscarinic Activity

A

Atropine (Cholinergic antagonist)

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20
Q

Sign and symptoms for Nicotinic toxicity

A

• blockade of neuromuscular end plate depolarization
o leading to fasciculations and paralysis
• CNS toxicity: stimulation (convulsions) followed by CNS depression

Remember sympathetic, parasympathetic and neuromuscular junctions
are ALL affected)

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21
Q

Treatment for Nicotinic TOxicity

A

symptom directed:
•atropine for muscarinic excess,
•diazepam and anticonvulsants for CNS stimulation, •mechanical ventilation if with neuromuscular blockade

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22
Q

Examples of INDIRECT-ACTING CHOLINOMIMETICS

A 
Neostigmine
Pyridostigmine
Physostigmine
AMBENONIUM [C],
DEMECARIUM [CARBAMATES] [C], 
ECHOTHIOPHATE [ORGANOPHOSPHATE]
RIVASTIGMINE [B]
GALANTAMINE [B]
DONEPEZIL [C]
TACRINE [C]
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23
Q

Cholinomimetic (indirect-acting) for diagnosis – Tensilon test. Differentiation of cholinergic crisis and myasthenic crisis (see note below for explanation) , Reversal of neuromuscular blockade

A

Edrophonium

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24
Q 
Myasthenia gravis (treatment) and Reversal of
nondepolarizing neuromuscular blockade
A

Neostigmine

25
Q

Among all indirect acting cholimimetics, which has a good lipid solubility

A

Physostigmine: good lipid solubility: able to enter the CNS because of its tertiary amine structure, DOA: 4-8h

26
Q

When reversing the effects of non-depolarizing neuromuscular blockers with neostigmine or edrophonium, why do we need to coadminister
ATROPINE?

A

To counteract the bradycardia associated with giving an indirect acting cholinomimetic

27
Q

Nerve gases

A

Sarin, Tabun, Soman: Nerve Gases

28
Q

What is myasthenia gravis?

A 
An autoimmune destruction of nicotinic ACh receptors,
characterized by:
• fluctuating muscle
• weakness
• ocular symptoms
• bulbar symptoms
• proximal muscle weakness
29
Q

Myasthenia gravis patients are sensitive to which drug class, that when given, may actually worsen their condition?

A

Nondepolarizing neuromuscular blockers (because the mechanism of the disease and its MOA are similar), Aminoglycoside antibiotics (because these drugs interfere with neuromuscular transmission)

30
Q

Differentiate myasthenic crisis from cholinergic crisis

A

MYASTHENIC CRISIS
• acute worsening of symptoms due to infection, stress or UNDERmedication

CHOLINERGIC CRISIS
• excessive activation of cholinoceptors (skeletal muscleweakness and parasympathetic signs) due to OVERmedication

31
Q

How does EDROPHONIUM differentiate myasthenic crisis from cholinergic crisis?

A
  • IMPROVES muscle strength in myasthenic crisis

* WEAKENS muscle strength in cholinergic crisis

32
Q

Cholinomimetic (indirect-acting) used for Alzheimers

A

•Rivastigmine is available as transdermal patch

•Donepezil is combined with Memantine (NMDA
antagonist) for Alzheimer’s dementia

33
Q

What are the signs and symptoms of organophosphate

poisoning?

A 
Diarrhea 
Urination 
Miosis 
Bradycardia
Bronchospasm 
Excitation (skeletal muscle and CNS)
Lacrimation
Sweating
Salivation
34
Q

NMDA receptor blocker; used for

moderate to severe Dementia

A

Memantine

35
Q

Antidote for organophosphate poisoning (first choice) which completely blocks all muscarinic receptors

A

Atropine

36
Q

Notorious for causing hyperthermia in susceptible

patients (because Atropine suppresses thermoregulatory sweating).

A

Atropine

37
Q

Direct acting Muscarinic Agonist: cholinomimetics big responses are as follows:

A

1) a decrease in heart rate
2) increase in secretion and
3) increase in smooth muscle contraction (e.g. diarrhea and urinary
incontinence)

38
Q

Properties of INdirect Cholinomimetics

A

Acetylcholinesterase inhibitors: Indirect-acing cholinomimetics
• they will not reach the blood vessels (they purely act on innervation)
• they also stimulate nicotinic receptors

39
Q

Muscarinic Antagonists for Parkinsonism

A 
“Tri (try) to Park your BENZ, BIP (beep) here.”
• TRIhexyphenidyl
• BENZtropine
• BIPeriden
• PARK is for Parkinson’s disease
40
Q

Difference between Cycloplegia and Mydriasis

A

C = Cycloplegia = Ciliary muscle paralysis = loss of
Accommodation
Mydriasis = Dilate (or you dilate your mouth when you say mydriasis)

41
Q

Addresses BOTH Nicotinic and Muscarinic symptoms.
Must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs (before the bond has AGED or turned covalent, which is a stronger bond); has oxime group which has high affinity for phosphorus

A

Pralidoxime

42
Q

T/F the role of your cholinergic antagonists in PArkinsons dse is to improve tremors

A

TRUE

43
Q

It is Cholinergic antagonist (muscarinic) which Competitively blocks ALL muscarinic receptors and Antagonizes histamine and serotonin.

It is used in Motion sickness, decrease acid secretion in GIT, Nausea and Vomiting

A

Scopalamine / Hyoscine (transdermal patch )

44
Q

It is an M receptor antagonist which Blocks muscarinic receptors in bronchial smooth muscle and Prevents vagal stimulated bronchoconstriction
Used Acute Asthma, COPD

A

Ipratropium

45
Q

Advantage of Ipratropium compared to SABA

A

Less toxic than beta-agonists (LESS TACHYCARDIA

→ LESS ARRHYTHMIA) in patients with COPD

46
Q

It does not cross the BBB, and consequently has none to few central effects. It may be used as a monotherapy as maintenance for COPD.
It may also be used as an anti-spasmodic and reduce
salivation with some anesthetics

A

GLYCOYRRONIUM [B]

47
Q

Competitively blocks M3 receptors.

Uses IBS, minor diarrhea, decrease acid secretion in GIT

A

DICYCLOMINE [B] HYOSCYAMINE [B], GLYCOPYRROLATE [B]

48
Q

Slightly blocks M3 receptors. Reduces Detrusor
muscle tone.
Used in Urge incontinence, Post-operative spasms

A

Oxybutinin

49
Q

Atropine Toxicity

A
  • Atropine fever (hyperthermia)
  • Atropine flush (cutaneous vasodilation)
  • Decreased secretions
  • Tachycardia
  • Arrhythmias (intraventricular conduction block)
  • Constipation
  • Blurred vision
  • CNS toxicity
50
Q

Treatment of Atropine TOxicity

A

Treatment: Symptomatic
o Temperature control: use of cooling blankets
o Seizure control: Diazepam
o Physostigmine

51
Q

Atropine Toxicity

A
  • HOT as a hare (hyperthermia)
  • DRY as a bone (decreased secretion)
  • RED as a beet (cutaneous vasodilation)
  • BLIND as a bat (cycloplegia)
  • MAD as a hatter (CNS toxicity)
52
Q

CONTRAINDICATIONS TO MUSCARINIC

BLOCKERS

A

• cautious use in infants (since they are sensitive to the
hyperthermic effects of atropine)

  • acute angle-closure glaucoma (since mydriasis can block the normal drainage of aqueous humor)
  • benign prostatic hyperplasia (can precipitate further urinary retention already present in this subgroup because muscarinic antagonists will relax smooth muscle of the ureters and bladder wall)
53
Q 
Cholinergic antagonist (nicotinic)
Competitively blocks Nn nicotinic ACh receptors
Uses Hypertension (obsolete), Hypertensive emergencies
A

HEXAMETHONIUM [D] TRIMETHAPHAN, [D] MECAMYLAMINE [C]

54
Q

Example of Depolarizing Neuromuscular blocker

A

Kapag nakapagDEPOsit ka sa toilet, SUCCess yun!

DEPOlarizing = SUCCinylcholine

55
Q

Exampple of NONDEPOLARIZING Neuromuscular blocker

A

NONDEPOLARIZING (Tubocurarine, Pancuronium,

Atracurium, Vecuronium)

56
Q

Synthesis of Acetylcholine is inhibited by

A

Hemicholinium

57
Q

Storage of Acetylcholine is inhibited by

A

vesamicol

58
Q

Release of Acetylcholine is inhibited by

A

botolinum toxin

pharma By Cie (1 decks)

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