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Muscarinic and nicotinic blockers Flashcards

1
Q

Nicotinic receptor agonists. Examples

A

Nicotine
Acetylcholine
Choline
Epibatidine
Lobeline
Varenicline
Cytisine

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2
Q

Natural nicotinic agonists (selective)

A

Nicotine(small doses)
Lobeline

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3
Q

Synthetic Nicotinic Agonists (selective)

A

Dimethyl phenyl piperazinium (DMPP)
Tetra methyl ammonium (TMA)

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4
Q

Excessive amounts of selective nicotinic agonists leads to

A

Sustained depolarization
Ganglion block

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5
Q

Non-selective muscarinic agonists

A

ACh
Pilocarpine
Carbachol
Anti-ChE

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6
Q

Nicotine is what type of amine and is derived from

A

Tertiary
Nicotiana tobacum leaves

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7
Q

Overall effects of GANGLIONIC stimulation on Blood vessels (sympathetic)

A

Vasoconstriction
Hypertension
Reduced peripheral blood flow

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8
Q

Effects of Ganglionic stimulation in the heart, GIT, Eye, UT, salivary gland

A

Same as Parasympathetic
Bradycardia, Increased tone, Miosis, Urination, watery salivation

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9
Q

Effect of ganglionic stimulation on sweat gland

A

Increased sweating (sympathetic)

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10
Q

Nicotine is available as transdermal patches for

A

Treating nicotine dependence

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11
Q

Varenicline :

A

Partial agonist
Reduces craving for and pleasurable effects of cigarettes

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12
Q

Vesamicol

A

Inhibits ACh carrier (Vesamicol inhibits acetylcholine uptake in presynaptic vesicles and reduce its release)

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13
Q

Botulinum

A

Presynaptic toxin that inhibits exocytosis of ACh from vesicles

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14
Q

Tubocurarine

A

Non-Depolarizing blocking agent(at synapse). Competitive antagonist of ACh

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15
Q

Suxamethonium

A

Depolarizing blocking agent. Inhibits the Post synaptic ACh receptor

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16
Q

Neostigmine

A

Anticholinesterase (inhibits AChE enzyme)

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17
Q

Hemicholinium

A

Inhibits the reuptake of choline (inhibits the choline carrier)

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18
Q

Action on M1 receptor on gastric gland

A

Histamine release
Acid secretion

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19
Q

Clinically Selective Anticholinergic Drugs (M1)

A

Pirenzepine
Telenzepine
Dicyclomine
Trihexyphenidyl

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20
Q

Function of M2 receptor on atrium

A

Shortening of APD, reduced contractility

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21
Q

Function of M2 receptor and on the CNS

A

tremor, anelgesia

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22
Q

Clinically selective anticholinergic drugs (M2)

A

Tripitamine, Methoctramine

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23
Q

Effects of M3 on visceral smooth muscle

A

Contraction

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24
Q

Effects of M3 on vascular endothelium

A

Release of NO to produce vasodilation

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25
Q

Clinically Selective Anticholinergic drugs (M3)

A

Darifenacin
Solifenacin
Oxybutinin
Tolterodine

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26
Q

When activated, M4 receptors inhibit ACh release in the …………….

A

Striatum

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27
Q

Antagonist drug of M4 receptors

A

Himbacine

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28
Q

List the natural anti muscarinic drugs

A
  1. Atropine (DL-hyoscyamine)
  2. Scopolamine (L-hyoscine)
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29
Q

Synthetic anti muscarinic drugs are divided into

A

Structural analogues of atropine
Structurally non related to atropine

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30
Q

List the tertiary ammonium compounds that are structural analogues of atropine

A

Homatropine

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31
Q

List the anti muscarinic drugs that are quarternary ammonium compounds

A
  1. Atropine methyl nitrate (Amn)
  2. Homatropine methyl bromide (Hmb)
  3. Methscopolamine bromide (Mb)
  4. Ipratropium
  5. Tiotropium
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32
Q

List the Tertiary amines structurally unrelated to atropine (anti muscarinic)

A
  1. Pirenzepine
  2. Dicyclomine
  3. Cyclopentolate
  4. Oxyphancyclimine
  5. Tropicamide
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33
Q

List the quarternary amines structurally unrelated to atropine (Synthetic anti muscarinic)

A
  1. Methantheline
  2. Propantheline
  3. Isopropamide
  4. Glycopyrrolate
34
Q

List the nonselective muscarinic receptor antagonists

A
  1. Atropine
  2. Scopolamine
  3. Homatropine
35
Q

List the selective muscarinic receptor M1 antagonists

A
  1. Pirenzepine
  2. Telenzepine
  3. Trihexyphenidyl
36
Q

List the Selective Muscarinic M2 antagonists

A

Methoctramine

37
Q

List the selective muscarinic M3 antagonists

A
  1. Hexahydrosiladefenidol (HHSiD)
  2. 4-DAMP
38
Q

Selective muscarinic M4 receptor antagonists

39
Q

What is Hyoscine derived from

A

Datura stramonium - THORN APPLE

40
Q

Classify Homatropine

A

Semisynthetic Mydriatic

41
Q

List the Semisynthetic antiasthmatics

A

Iprotropium
Tiotropium bromide

42
Q

List the semisynthetic GI spasmolytics

A

Hyoscine butyl bromide

43
Q

List the synthetic mydriatics

A

Tropicamide
Cyclopentolate

44
Q

List Synthetic Quartenary GI spasmolytics

A
  1. Oxyphenonium
  2. Clidinium
  3. Pipenzolate
  4. Isopropamide
  5. Glycopyrrolate
45
Q

Classify Dicyclomine

A

Synthetic Tertiary GI plasmolytic

46
Q

List the Synthetic Tertiary Antiulcer drugs

A

Pirenzepine
Telenzepine
(M1-blockers)

47
Q

List the Synthetic Tertiary Vasicoselective drugs

A

Flavoxate
Oxybutynin
Tolteridine

48
Q

List the Synthetic Tertiary Antiparkinsonians (central M-cholinolytics)

A
  1. Benztropine
  2. Biperiden
  3. Trihexyphenidyl (benzhexol)
49
Q

Salivary, Lacrimal, Bronchial and sweat glands are inhibited by very high/low doses of atropine

50
Q

In low doses, atropine causes (heart rate)

A

Bradycardia

51
Q

Regarding the eye, Atropine causes

A

Mydriasis and Cycloplegia (dilatation and paralysis of accommodation)

52
Q

Low doses of atropine in the CNS can cause

A

Mild restlessness

53
Q

Higher does of atropine in the CNS can cause

A

Agitation and Disorientation

54
Q

Central effects of atropine could be opposed by

A

Anticholinesterase drugs e.g Physostigmine

55
Q

Low doses of Hyoscine in the CNS cause

A

Mild sedation

56
Q

Hyoscine is useful as an Antiemetic and in motion sickness T/F

57
Q

How do atropine-like drugs affect the extrapyramidal system?

A

By Reducing involuntary movement and rigidity in Parkinson’s disease

58
Q

Atropine produces a much of anaesthetic action on the cornea T/F

59
Q

How is atropine eliminated

A

50% eliminated in the liver. The rest excreted unchanged

60
Q

Hyoscine is more completely metabolized but does not cross the BBB. T/F

A

F. Hyoscine crosses the BBB

61
Q

Half life of Atropine

A

Approximately 4 hours

62
Q

Effects of anti muscarinic anatagonists on the heart

A

Bradycardia at low doses then Tachycardia

63
Q

Symptoms of anticholinergic toxicity

A

Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat
Mad as a hatter

64
Q

Management of anticholinergic toxicity

A
  1. Cold sponges/Ice baths
  2. Physical restraints
  3. Chemical restraints(Benzodiazepines)
  4. Gastric lavage (if ingested)
  5. Physostigmine (1-3)mg
65
Q

Physostigmine arrests both central and peripheral effects. T/F

66
Q

Neostigmine affects only central effects. T/F

A

F. Neostigmine is ineffective for central effects

67
Q

Clinical uses of Anticholinergics

A
  1. As antisecretory
  2. As antispasmodic
  3. Bronchial asthma, COPD
  4. As mydriatic and cycloplegic
  5. As cardiac vagolytic
  6. For central action (Parkinsonism, Motion Sickness, Sedation and Amnesia)
  7. Antidote (Anti ChE, early mushroom poisoning)
68
Q

…………,,,,, is used to produce sedation and amnesia in labour and maniacal states

69
Q

Atropine delays/stimulates gastric emptying and absorption of other drugs

70
Q

…….. interferes with absorption of anticholinergics

71
Q

Other drugs that have anticholinergic properties

A

Antihistamines
Tricyclic antidepressants
Phenothiazines
Disopyramide
Pethidine

72
Q

Antinicotinic drugs are divided as

A

Ganglion blockers
Neuromuscular blockers

73
Q

Examples of ganglion blockers

A

Hexamethonium
Trimetaphan
Mecamylamine
(MTH GANG)

74
Q

Examples of neuromuscular blockers

A

Suxamethonium
Decamethonium
Tubocurarine
Atracurium

75
Q

All ganglion blockers of interest are

A

Synthetic amines

76
Q

List the Competitive ganglion blockers

A

Hexamethonium
Mecamylamine
Trimethaphan

77
Q

List the Non-competitive ganglion blockers

A

Nicotine (large doses)
Acetylcholinesterases (large doses)

78
Q

Effect of Ganglion blockade on the heart

A

Tachycardia

79
Q

Trimethaphan is occasionally used in

A

Treatment of hypertensive emergencies

80
Q

Effects of ganglion blockade

A

Depression, vasodilation, hypotension, Decreased VR, tachycardia, Decreased tone and motility

81
Q

Action of NM blockers

A

Block NM transmission at the NMJ, causing paralysis of the affected skeletal muscles

82
Q

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Pharmacology (11 decks)

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