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Neuroscience (1206) > Drugs Modulating ANS Function (Cholinergic and AntiCholinergic Drugs) > Flashcards

Drugs Modulating ANS Function (Cholinergic and AntiCholinergic Drugs) Flashcards

1
Q

What are the two Cholinergic Receptors

A

Nicotinic, Muscarinic

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2
Q

What drug are all muscarinic sites blocked by

A

Atropine

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3
Q

What drug blocks Effector cells of skeletal muscle innervated by somatic nerves

A

Curare

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4
Q

What drug blocks Autonomic ganglion cells of sympathetic & parasympathetic nerves

A

hexamethonium

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5
Q

What drug blocks Adrenal medullary cells and some adrenergic nerve terminals

A

hexamethonium

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6
Q

What are the locations of M1 receptors

A

CNS
Gastric Gland
Salivary Gland

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7
Q

What are the locations of M2 receptors

A

Heart
GIT
CNS

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8
Q

What are the locations of M3

A 
Salivary Gland
Gastric Gland
Eye
GIT
Blood vessels
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9
Q

What drug inhibit Cholinesterase

A

Neostigmine

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10
Q

What drug inhibit AcH release by inhibiting synthesis

A

Hemicholinium- blocks choline uptake

Botulinium, Mg, aminoglycosides- inhibit release mechanism

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11
Q

What drug blocks the action of AcH

A

Atropine, Tubocurarine

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12
Q

What are the two types of Cholinergic Agonists

A

Direct Acting Agonist

Indirect Acting

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13
Q

What type of Cholinergic Agonist inhibit acetylcholinesterase

A

Indirect Acting

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14
Q

What substance may cause respiratory paralysis after large doses due to inhibition of presynaptic release of Ach & post-synaptic sensitization to Ach

A

Aminoglycosides

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15
Q

What are the two types of Cholinoreceptor activating drug

A

Choline ester, Alkaloids

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16
Q

What are the Choline Esters drugs

A

Acetylcholine
Metacholine
Bethanechol

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17
Q

What are the Alkaloid drugs

A

Pilocarpine
Muscarine
Nicotine
Labeline

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18
Q

What are the different types of cholinesterase inhibiting drugs

A

Alcohol
Carbamates
Organophosphates

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19
Q

What are some examples of Organophosphates

A

Therapeutics
Insecticides
Nerve Gases

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20
Q

True or false, the effects of AcH is short lived

A

True

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21
Q

What are the main receptors that acetylcholine act on

A

Muscarinic and nicotinic

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22
Q

Why are nicotinic effects not normally seen

A

Ach does not readily penetrate tissues which surround skeletal m & autonomic ganglia

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23
Q

What are adverse effects of AcH

A 
Diarrhoea and decreased blood pressure
Urination
Miosis
Bronchoconstriction & bradycardia
Excitation of skeletal m
Lacrimation
Salivation & sweating
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24
Q

Nicotinic Effects of Acetylcholine can be protected based stimulation of nicotinic receptors on

A

Sympathetic and Parasympathetic Ganglia
Adrenal Medulla
Skeletal M

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25
Q

What is the therapeutic use of Acetylcholine

A

Miosis during ophthalmic sx

(rarely use b/c of widespread effects & rapid hydrolysis by cholinesterase

26
Q

What are the adverse effects of Acetylcholine

A

Generalized cholinergic stimulation

27
Q

What receptors does Acetylcholine activate

A

M, N

28
Q

What is the therapeutic use of Bethanechol

A

Increases intestinal motility esp after sx. Stimulates detrusor m of bladder →used to treat urinary retention

29
Q

What are the adverse effects of Bethanechol

A

Generalized Cholinergic Stimulation

30
Q

What receptors does Bethanechol activate

A

M and some mild N properties

31
Q

What is the therapeutic use of Methacholine

A

Diagnosis of asthma and bronchial hyperactivity

32
Q

What are some adverse effects of Methacholine

A

Generalized cholinergic stimulation

33
Q

What receptors does Methacholine activate

A

M

34
Q

What is the therapeutic use of Pilocarpine

A

Very good at stimulating miosis & opening of trabecular meshwork around canal of Sclemn► used treatment of glaucoma

35
Q

What are the adverse effects of Pilocarpine

A

Unlike other direct acting agonists, pilocarpine is able to enter brain & cause CNS disturbances -hallucinations, convulsions & generalized cholinergic stimulation

36
Q

What receptors does Pilocarpine activate

A

M

37
Q

Give an example of Cholinesterase inhibiting drug Alcohols

A

Edrophonium

38
Q

Give an example of Cholinesterase inhibiting drug Carbamates : Teritiary Animes

A

Physostigmine

39
Q

Give an example of Cholinesterase inhibiting drug Carbamates: Quaternary Ammoniums

A

Neostigmine

Pyridostigmine

40
Q

Give an example of Cholinesterase inhibiting drug : Organophosphate: Therapeutics

A

Isoflurophate Echothiophate

41
Q

Give an example of Cholinesterase inhibiting drug : Organophosphate Insecticides

A

Malathion

Parathion

42
Q

Give an example of Cholinesterase inhibiting drug : Organophosphate Nerve Gases

A

Sarin

43
Q

What is the therapeutic use of Physostigmine

A

For overdoses of atropine, phenothiazines, tricyclic antidepressants

44
Q

What are the adverse effects of Physostigmine

A

Convulsions
Muscle paralysis secondary to overstimulation
Generalized cholinergic stimulation

45
Q

What is the therapeutic use of Neostigmine

A

Treatment of myasthenia gravis
Treatment of urinary retention & paralytic ileus
Antidote for non-depolarizing neuromuscular blockade as with tubocurarine

46
Q

What are the adverse effects of Neostigmine

A

Excessive cholinergic stimulation

47
Q

True or false, Neostigmine actions are more prominent on CVS and eye than NMJ and GIT

A

False, more prominent on NMJ and GIT than CVS and eye

48
Q

What is the therapeutic use of Endrophonium

A

Used to diagnose myasthenia gravis (MG). Not useful for maintenance therapy – short duration of action ( 5-15 min)
Used to differentiate MG from cholinergic crisis (excessive Ach)

49
Q

True or False, In the test for Myasthenia Gravis, Edrophonium will drastically improve in patients with chollinergic weakness than Myasthenia Gravis

A

False, myasthenic weakness substantially improved by edrophonium; cholinergic weakness is aggravated

50
Q

What is the therapeutic use of Pyridostigmine

A

Long duration of action

Used for long term treatment of myasthenia gravis

51
Q

What is the adverse effects of Pyridostigmine

A

Excessive Cholinergic Stimulation

52
Q

What organophosphate is not highly lipid soluble

A

Echothiophosphate

53
Q

Recovery of enzymatic Activity in organophosphate depends on

A

Synthesis of new enzymes- process that may take weeks

54
Q

What is used to treat organophosphate Toxicity

A

Support respiration
Very high doses of atropine (muscarinic receptor)
Cholinesterase reactivator- Pralidoxime

55
Q

What are the different types of Neuromuscular blocks

A

Neuromuscular
Ganglionic
Muscarinic

56
Q

What are the drugs associated with muscarinic blockers

A 
Atropine
Scopolamine
Homatropine
Cyclopentolate
Tropicamide
Pirenzepine
57
Q

What are the types of Neuromuscular blockers

A

Non-depolarizing

Depolarizing

58
Q

What are the drugs associated with ganglionic blockers

A

Nicotine
Hexamethonium
Trimethaphan

59
Q

What are the therapeutic uses of atropine

A

Treatment of bradycardia
Mydriasis & Cycloplegia
Gastrointestinal spasms
Organophosphate poisoning

60
Q

What are the toxic affects of Atropine

A

Red as a beet , blind as a bat , dry as a bone , hot as a hare & mad as a hatter “
→ Cutaneous vasodilation → atropine flush , blurred vision ,
↓ secretions , hyperthermia ( atropine fever due to ↓ sweat ), delirium & hallucinations

61
Q

What drug classes may have Anticholinergic side effects

A 
Antihistamines 
Antipsychotics
Tricyclic antidepressants
Monoamine oxidase inhibitors ( MAOI )
Lithium

Neuroscience (1206) (17 decks)

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