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Cholinergics Flashcards

1
Q

Hemicholinium receptor/mechnism

A

Blocks choline transporter CHT1 preventing uptake and synthesis of acetylcholine

Used for research

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2
Q

Vesamicol receptor/mechanism

A

Blocks the vesicular ACh-H+ antiporter VAChT preventing storage of ACh

Used for research

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3
Q

Botulinum Toxin receptor/mechanism

A

Prevents synaptic vesicle fusion inhibiting ACh release (synaptobrevin)

Used in local injection; conditions with excess muscle tone (blepharospasm); wrinkles, HA and pain

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4
Q

Neuromuscular blockers drugs

A

Tubocurarine and Succinylcholine

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5
Q

Tubocurarine receptor/mechanism

A

Non depolarizing
Binds to Nm->competitive inhibition
Prevents depolarization

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6
Q

Tubocurarine indication/effect

A

Anesthesia->muscle weakness and flaccid paralysis

Action can be overcome by AChE inhibitors such as neostigmine or edrophonium

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7
Q

Tubocurarine PK

A

Minimal oral absorption so need to be IV
Poor membrane penetration
Doesn’t cross BBB

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8
Q

Tubocurarine adverse

A

May cause histamine release

May bind M receptors

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9
Q

Succinylcholine receptor/mechanism

A

Depolarizing
Activates Nm causing depolarization -> transient disorganized contraction -> desensitization followed by flaccid paralysis

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10
Q

Succinylcholine indication/effect

A

Useful for ET intubation

Electroconvulsive therapy

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11
Q

Succinylcholine PK

A

continuous IV infusion

Rapid hydrolysis by plasma cholinesterase
Rapid onset (1m) and brief duration (5-10m)
Not metabolized effectively at the synapse

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12
Q

Succinylcholine adverse

A

Malignant hyperthermia an autosomal dominant disorder -> excess release of calcium from the SR; usually when combined with a halogenated anesthetic (Tx dantrolene)

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13
Q

Mecamylamine, Trimethaphan, Hexamethonium receptor/mechanism

A

Antagonize nicotinic receptors in both parasympathetic and sympathetic autonomic ganglia

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14
Q

Mecamylamine, Trimethaphan, Hexamethonium effects

A

Arterioles and veins are under predominant sympathetic control (adrenergic) -> dilation, hypotension, etc alpha 1

Block parasympathetics at the heart, iris and ciliaris muscle -> tachycardia, mydriasis, and cycloplegia (far vision)

GI, urinary bladder and salivary gland lose parasympathetics -> reduced motility, secretions; urinary retention, xerostomia (dry mouth)

Sweat glands lose sympathetics -> anhydrosis

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15
Q

Mecamylamine, Trimethaphan, Hexamethonium adverse

A 
Vasodilation
Venodilation
Hypotension
Tachycardia
Mydriasis
Decreased GI/urinary motility
Xerostomia
Anhydrosis
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16
Q

Mecamylamine, Trimethaphan, Hexamethonium other

A

Historically used to treat HTN, but have been replaced due to many undesirable effect

Dirty drugs

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17
Q

Pralidoxime effect

A

Regenerate cholinesterase after organophosphate poisoning (before aging)

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18
Q

Pralidoxime indication

A

not used for carbamate poisoning which is reversible and short lived

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19
Q

Pralidoxime other

A

Positively charged; it does not enter the CNS -> not effect on central sx

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20
Q

Tolterodine effect

A

Tertiary amine

Relaxes smooth muscle

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21
Q

Tolterodine indication

A

overactive bladder

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22
Q

Muscarinic antagonists

A 
Atropine
Scopolamine
Ipratropium and Tiotropium
Homatropine, Cyclopentolate, Tropicamide
Benztropine, Trihexyphenidyl
Glycopyrrolate
Tolterodine
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23
Q

Glycopyrrolate indication

A

Oral: inhibition of GI motility
Parenteral: prevent bradycardia during surgery

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24
Q

Benztropine and Trihexyphenidyl Effects

A

Restore balance of input after loss of dopaminergic neurons in the nigrostriatal pathway

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25
Benztropine and Trihexyphenidyl Indication
``` Parkinsonism Extrapyramidal effects ( i.e. drug induced movement disorders) of antipsychotic drugs (D2) ```
26
Benztropine and Trihexyphenidyl PK
tertiary amines are able to enter the CNS
27
Homatropine, Cyclopentolate, Tropicamide effects
*Mydriasis and cycloplegia* - preferred over atropine because of shorter duration of action
28
Homatropine, Cyclopentolate, Tropicamide PK
tertiary amines are able to enter the CNS
29
Ipratropium, Tiotropium effects
Bronchodilation (M3)
30
Ipratropium, Tiotropium indication
Inhalation Tx of ***COPD and adjuvant therapy in asthma**
31
Scopolamine effects/indication
***DOC for motion sickness*** | Blocks short term memory (anesthetic procedures)
32
Scopolamine other
Belladonna Alkaloids-Tertiary amines | Greater and longer duration of action in the CNS than atropine
33
Atropine effects
Eye: mydriasis, unreactive to light, cycloplegia (paralysis of ciliaris muscle causing loss of accommodation and adaptation) GI: antispasmodic; decreases motility (HCl production not affected) Urinary: *decreases hypermotility* CVS: low dose -> bradycardia (presynaptic M2) moderate to high dose-> tachycardia (atrial M2) Secretions from salivary, sweat and lacrimal glands are blocked (may increase body temperature)
34
Atropine indication
Antisialagogue prior to surgery decreases respiratory secretions Increased HR or Decrease AV block due to excessive vagal tone *OD of cholinergic drugs (farmer spraying parathion)* Death cap mushroom poisoning Alleviate the muscarinic side effects of AChE drugs
35
Atropine PK
readily absorbed, partially metabolized by the liver, eliminated primarily in the urine
36
Muscarinic antagonists contraindications/adverse effects
"Atropine flush" due to cutaneous vasodilation (especially in upper body) Anti-PS ->dry mouth, blurred vision, sandy eyes, tachycardia, constipation CNS: restlessness, confusion, *hallucinations, delirium, depression* -> shock and death Elderly patients with angle closure glaucoma -> exacerbation and blindness Use with caution in patients with BPH ->decrease detrusor contraction can cause urinary retention Low levels may cause bradycardia and sedation High levels may cause tachycardia and CNS hyper excitation (delirium, hallucinations, and seizures)
37
AChE Inhibitor drugs
``` Edrophonium (Tensilon) Physostigmine Neostigmine Pyridostigmine Echothiophate (obsolete) Malathion, Parathion Tabun, Sarin, Soman Tacrine, Donepezil, Rivastigmine, Galantamine ```
38
Tacrine, Donepezil, Rivastigmine, Galantamine indication
Orally used | Alzheimer's disease
39
Tabun, Sarin, Soman mechanism
Phosphorylate active site (extremely stable) Ageing-strengthening of the bond making it much more difficult to reverse
40
Malathion, Parathion mechanism
Phosphorylate active site (extremely stable) Ageing-strengthening of the bond making it much more difficult to reverse
41
Echothiophate mechanism
Phosphorylate active site (extremely stable) Ageing-strengthening of the bond making it much more difficult to reverse
42
Echothiphate indication
Chronic angle glaucoma | NOT liposoluble-> doesn't enter CNS
43
Malathion, Parathion effects
Activated by conversion to oxygen analogs in the body
44
Malathion, Parathion indications
insecticides (farmer spraying his field...)
45
Malathion, Parathion PK
Fully distributed (including CNS)
46
Malathion, parathion adverse
Organophosphate overdose treated with atropine or Pralidoxime **have to give before ageing** CNS toxicity
47
Tabun, Sarin, Soman adverse
Organophosphate overdose treated with atropine or Pralidoxime **have to give before ageing** CNS toxicity
48
Tabun, Sarin, Soman effects
Nerve agents - most potent synthetic toxic agents known | Used for terrorism
49
Pyridostigmine indication
Treatment of Myasthenia gravis (most common)
50
Pyridostigmine adverse
CNS toxicity
51
Neostigmine mechnism
Covalent bond with AChE and ButyrylChE
52
Pyridostigmine mechanism
Covalent bond with AChE and ButyrylChE
53
Physostigmine mechanism
Covalent bond with AChE and ButyrylChE
54
Physostigmine chemical
carbamate - tertiary amine | Crosses BBB
55
Neostigmine and Pyridostigmine chemical
Carbamates - QAC - does not enter CNS
56
Edrophonium (Tensilon) chemical
simple alcohol QAC
57
Edrophonium (Tensilon) mechanism
*Reversible* binding to active site of AChE and butyrylcholinesterase
58
Neostigmine indications
*Reversal of NMJ block* produced by non depolarizing muscular blockers i.e. tubocurarine Second line treatment for myasthenia gravis Does not enter the CNS Prevention and Tx of urinary retention
59
Neostigmine adverse
``` Hypotension Salivation, flushing Abdominal pain Nausea, diarrhea Bronchospasm ```
60
Physostigmine indications
Tx for *anticholinergic overdose* Intestinal or bladder atony
61
Physostigmine adverse
High dose -> convulsions**, skeletal muscle paralysis, bradycardia **Contraindicated in suspected TCA overdose** -> aggravates depression of cardiac conduction (TCA's block sodium channels)
62
Edrophonium indication
Diagnosis of Myasthenia gravis (rapid increase in muscle strength after dose) Reverse neuromuscular block produced by non depolarizing muscular blockers (can be used for recovery after surgery)
63
AChE inhibitor effects
CNS: convulsion, coma, respiratory arrest PS action in the eye, respiratory, GI and urinary tracts CVS: -ve chronotropic and inotropic effects -> decreased CO and hypotension NMJ: increased contraction in weak muscles
64
Acetylcholine Receptor
N and M
65
Acetylcholine mechanism
Binding to M receptor induces PS activity Nicotinic effects once M receptors are blocked by atropine (high dose)
66
Acetylcholine Effects
M: parasympathetic and sympathetic activity, sweat glands CVS: M3 vasodilation and reflex tachycardia at small doses; hypotension and bradycardia at higher doses N: stimulate all autonomic ganglia, secretion of Epi from adrenal medulla; skeletal muscle increase HR, BP, etc.
67
Acetylcholine indication/use
Small iv-> drop BP with tachycardia Virtually no use except Cataract surgery -> rapid miosis
68
Cholinergic agonist adverse
Muscarinic syndrome Generalized cholinergic stimulation -> sweating, miosis, flushing, salivation, bradycardia, hypotension, bronchospasm ``` DUMBBELLSS-> Diarrhea Urination Miosis Bradycardia Bronchoconstriction Emesis Lacrimation Lethargy Salivation Sweating ```
69
Bethanechol receptor
M
70
Bethanechol mechanism
Parasympathetic
71
Bethanechol effects
Activates bowel and bladder
72
Bethanechol indication/use
``` Urinary retention (post-surgical postpartum) Hypotonic, myogenic, neurogenic bladder ... atony ``` Ileus, gastroparesis, congenital megacolon Cannot cross BBB
73
Carbachol receptor
M and N
74
Carbachol mechanism
parasympathetic
75
Carbachol effects
Miosis and contraction of ciliaris muscle
76
Carbachol indication/use
Intraocular surgery Glaucoma - decrease intraocular pressure (use pilocarpine first) External use only
77
Methacholine receptor
M and little N
78
Methacholine indication/use
*diagnosis of bronchial airway hyperreactivity* in patients without clinically apparent asthma
79
Pilocarpine receptor
Partial M | tertiary amine
80
Pilocarpine effects
Contraction of ciliaris | Secretion from sweat, salivary, lacrimal and bronchial glands
81
Pilocarpine indication/use
Acute close-angle glaucoma Open angle glaucoma -> 2nd line after timolol Included in the regimen for close angle glaucoma with: timolol, apraclonidine, acetazolamide, and mannitol or glycerol
82
Pilocarpine adverse
CNS disturbances Sweating Salivation
83
Nicotine receptor
Nn>Nm | Tertiary amine
84
Nicotine mechanism/effect
Low dose: ganglion deploarization in both sympathetic and parasympathetic CVS: sympathomimetic due to catecholamine release GI and UG: parasympathomimetic -> n/v/d, voiding, salivary and bronchial secretions High dose: *ganglion blockade due to prolonged depolarization* (desensitization)
85
Nicotine indication/use
smoking cessation therapy
86
Nicotine adverse
Acute nicotine poisoning: nausea, salivation, abdominal pain, vomiting, diarrhea, cold sweat, confusion, etc. Hypotension with a rapid and weak pulse Can lead to death respiratory arrest (central or peripheral)

Pharmacology (24 decks)

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