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Pharmacology > Cholinergic drugs > Flashcards

Cholinergic drugs Flashcards

1
Q

Acetylcholine (Miochol)

A

Direct-Acting cholinergic agonist

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2
Q

Bethanechol (Urecholine)

A

Direct-Acting muscarinic agonist

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3
Q

Pilocarpine (Isopto Crpine; Pilocar)

A

Direct-Acting muscarinic agonist

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4
Q

Cevimeline (Evoxac)

A

Direct-Acting muscarinic agonist

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5
Q

Nicotine

A

Direct-Acting nicotinic agonist

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6
Q

Varenicline (Chantrix)

A

Direct-Acting nicotinic agonist

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7
Q

Neostigmine (Prostigmin)

A

Cholinesterase Inhibitor. Carbamate. Quaternary amine. Not absorbed well orally and can’t cross the BBB.

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8
Q

Edrophonium (Tensilon)

A

Cholinesterase Inhibitor. Must be injected. No CNS penetration. Binds reversibly with a short duration of action (5-10 mins).

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9
Q

Physostigmine (Eserine)

A

Cholinesterase Inhibitor. Carbamate. Tertiary amine. Can cross the BBB.

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10
Q

Echothiophate

A

Cholinesterase Inhibitor. Organophosphate.

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11
Q

Donepezil (Aricept)

A

Cholinesterase Inhibitor

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12
Q

Organophosphate Pesticides

A

Cholinesterase Inhibitor. Lipid soluble. Phosphorylate AchE with a long lasting bond that ages and increases in strength (can be fatal).

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13
Q

Pralidoxime (2-PAM)

A

Cholinesterase Inhibitor.

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14
Q

Atropine (generic)

A

Cholinergic Antagonist

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15
Q

Scopolamine (TransDerm Scop)

A

Cholinergic Antagonist

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16
Q

Glycopyrrolate (Robunil)

A

Cholinergic Antagonist

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17
Q

Dicyclomine (Bentyl)

A

Cholinergic Antagonist

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18
Q

Tolterodine (Detrol)

A

Cholinergic Antagonist

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19
Q

Fesoterodine (Toviaz)

A

Cholinergic Antagonist

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20
Q

Darifenacin (Enablex)

A

Cholinergic Antagonist

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21
Q

Solifenacin (Vesicare)

A

Cholinergic Antagonist

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22
Q

Oxybutynin (Ditropan)

A

Cholinergic Antagonist

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23
Q

Ipratropium (Atrovent)

A

Cholinergic Antagonist

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24
Q

Diphenoxylate-atropine (Lomotil)

A

Cholinergic Antagonist

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25
Q

Tropicamide (Mydriacyl)

A

Cholinergic Antagonist

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26
Q

Homatropine (Isoptohomatropine )

A

Cholinergic Antagonist

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27
Q

d-Tubocurarine

A

Non-Depolarizing Neuromuscular Blockers

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28
Q

Vecuronium (Norcuron)

A

Non-Depolarizing Neuromuscular Blockers

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29
Q

Cisatracurium (Nimbex)

A

Non-Depolarizing Neuromuscular Blockers

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30
Q

Succinylcholine (Anectine)

A

Depolarizing Neuromuscular Blockers

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31
Q

Mecamylamine (Inversine)

A

Ganglion blocker

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32
Q

Hexamethonium

A

Ganglion blocker

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33
Q

Cholinergic stimulants

A

cholinergic agonists and cholinesterase inhibitors

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34
Q

Acetylcholine MOA

A

Stimulates both nicotinic and muscarinic receptors. Causes PNS stimulation. Metabolized rapidly. No clinical use.

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35
Q

Bethanechol (Urecholine) MOA

A

Stimulates muscarinic receptors especially in the urinary and GI tract. No CNS penetration.

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36
Q

Pilocarpine (Pilocar) MOA

A

Stimulates muscarinic receptors. Sweat and salivary glands are extremely sensitive.

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37
Q

Cevimeline MOA

A

Stimulates M3 receptors. Less side effects than Pilocarpine (Pilocar).

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38
Q

Nicotine MOA

A

Stimulates nicotinic receptors.

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39
Q

Varenicline MOA

A

Stimulates nicotinic receptors.

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40
Q

Varenicline Uses

A

Smoking cessation. Partial agonist for the nicotinic receptors in the brain to reduce cravings. Side effects include: nausea, vomiting, constipation, sleep distrubance, anxiety.

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41
Q

Muscarinic Agonists MOA

A

either interact with Gq or Gi

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42
Q

Muscarinic Agonists effect on the eye

A

Miosis. Contraction of the ciliary muscle for near vision. Decreases intraocular pressure.

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43
Q

Muscarinic Agonists effect on the heart

A

Decreases AV conduction. Inhibits NE release. Increases NO causing vasodilation. But overall very few cardiovascular effects.

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44
Q

Muscarinic Agonists effect on Respiratory system

A

Bronchoconstriction especially in asthmatics

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45
Q

Methacholine uses

A

Diagnosis of asthma

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46
Q

Muscarinic Agonists effect on GI system

A

Increased secretions and peristalsis. Sphincters are relaxed.

47
Q

Muscarinic Agonists effect on Glands

A

Increases salivation, lacrimation and nasopharyngeal glands.

48
Q

Muscarinic Agonists effect on GU

A

Stimulate detrusor muscle and relaxes the sphincter. Increases urge to void.

49
Q

Muscarinic Agonists effect on Brain

A

M1 muscarinic receptors in the brain are involved in memory.

50
Q

Use for pilocarpine

A

Glaucoma DOC. Dry mouth but can cause profound sweating.

51
Q

Uses for Bethanechol

A

Stimulates peristalsis and treats urinary retention

52
Q

Uses for cevimeline

A

Dry mouth. Selective for M3 receptors (doesn’t cause sweating).

53
Q

Muscarinic Agonist Side effects

A

Nausea, vomiting, diarrhea, abdominal cramps, belching, salivation, sweating, cutaneous vasodilation, bronchoconstriction, bladder tightness, blurred vision.

54
Q

Muscarinic Agonist contraindications

A

Peptic ulcers, coronary insufficiency, asthma.

55
Q

Nicotinic Agonsits MOA

A

Increases permeability to calcium and sodium. Located in the autonomic ganglia, brain and skeletal muscle. Immediate action followed by rapid desensitization. .

56
Q

Nicotinic Agonists Central effects

A

Increases alertness and attention. At higher doses and cause tremors, vomiting and increased respiration.

57
Q

Nicotinic Agonists effect on the heart

A

Mostly sympathetic. Increased BP (reflex bradycardia), increased HR.

58
Q

Nicotinic Agonists effect on GI

A

PNS. Vomiting, diarrhea and urination.

59
Q

Nicotinic Agonists effect on the neuromuscular junction

A

Initially cause contraction then desensitize the NMJ leaded to weakness and flaccid paralysis.

60
Q

Nicotinic Agonists Side Effects

A

Vomiting, convulsions, coma, respiratory arrest, paralysis, hypertension and cardiac arrhythmias.

61
Q

Nicotine poisoning treatment

A

Atropine, anticonvulsants and mechanical respiration

62
Q

Cholinesterase inhibitors MOA

A

Inhibit the breakdown of Ach in the synaptic cleft. Useful when cholinergic inputs have been decreased or there is a decreased responsiveness. Effect muscarinic and nicotinic receptors.

63
Q

Cholinesterase inhibitors carbamates

A

Neostigmine and physostigmine. Covalently bind and last 30 mins- 6 hours.

64
Q

2-PAM uses

A

Treats exposure to organophosphate pesticides to inhibit the “aging” process. Contraindicated for carbamate pesticides but still used in emergency protocol.

65
Q

Cholinesterase inhibitors effect on the brain

A

Improves memory by stimulating M1 and Nn receptors. High doses can lead to desensitization (convulsions and respiratory arrest).

66
Q

Cholinesterase inhibitors effect on the eye

A

PNS. Miosis. Ciliary muscle contraction for near vision. Decreased intraocular pressure.

67
Q

Cholinesterase inhibitors effect on the respiratory system

A

PNS. Bronchoconstriction and increased mucus secretion.

68
Q

Cholinesterase inhibitors effect on the GI tract

A

PNS. Increased perastilis and relaxation of the sphincters.

69
Q

Cholinesterase inhibitors effect on the heart

A

PNS. Bradycardia, decreased contractility. Desensitization of ganglionic nicotinic receptors will decrease sympathetic stimulation.

70
Q

Cholinesterase inhibitors effect on the NMJ

A

Low concentrations will increase the force of contraction at higher concentrations a neuromuscular blockade may occur due to desensitization.

71
Q

Neostigmine uses

A

Myasthenia gravis because it may have a direct stimulatory effect on the NMJ. Also used to reverse NMJ blockade after surgery.

72
Q

Physostigmine uses

A

Applied directly to the eye to treat glaucoma. Not used orally except to t treat muscarinic antagonist overdose.

73
Q

Donepezil uses

A

Alzheimer’s disease. Absorbed into the CNS.

74
Q

Edrophonium uses

A

diagnosis of myasthenia gravis (due to it’s short acting effects) and to determine the correct dosing of neostigmine. Can also reverse the NMJ blockade after surgery.

75
Q

Echothiophate uses

A

Emergency treatment of closed angle glaucoma. Used along with pilocarpine.

76
Q

Irreversible cholinesterase inhibitor toxicity symptoms

A

SLUDGE (salivation, lacrimation, urination, defecation, gastric distress, emesis). Miosis, sweating, bronchoconstriction, bradycardia, hypotension. Paralysis eventually occurs due to desensitization.

77
Q

Irreversible cholinesterase inhibitor toxicity treatment

A

Atropine (until pupils dilate), 2-PAM (prevents enzyme aging), mechanical respiration.

78
Q

Muscarinic antagonists MOA

A

Bind muscarinic receptors to block the effect of Ach. Antagonize the effects of the PNS.

79
Q

Atropine on the CNS

A

Little effect but can cause confusion and coma at toxic levels.

80
Q

Scopolamine on the CNS

A

Crosses the BBB at low doses. Causes drowsiness and amnesia. At toxic levels will cause agitation, hallucinations and coma.

81
Q

Scopolamine uses

A

Prevents motion sickness. Administered as a patch.

82
Q

Benztropine uses

A

Can restore the balance between Ach and DA which can occur due to antipsychotics and parkinson’s drugs.

83
Q

Muscarinic antagonists effects on the eye

A

Mydriasis. Cycloplegia (loss of accomodation for near vision). Increased intraocular pressure.

84
Q

Muscarinic antagonists contraindications

A

Narrow angle glaucoma, benign prostatic hyperplasia (urinary retention).

85
Q

Tropicamide uses

A

Mydriasis and cycloplegia for eye examinations

86
Q

Homatropine uses

A

Mydriasis and cycloplegia for eye examinations

87
Q

Muscarinic antagonists side effects

A

Dry eyes, dry mouth, decreased bronchial secretions, tachycardia, mydriasis, cycloplegia, decreased GI motility, urinary retention, hot/dry skin.

88
Q

Muscarinic antagonists effect on the heart

A

Blocks M2 receptors and cause tachycardia (especially in those with high vagal tone). Used to reverse the effect of reflex vagal discharge.

89
Q

Glycopyrrolate uses

A

In surgery to prevent vagal responses due to visceral organs being handled. Also is a second line drug to decrease muscarinic side effects.

90
Q

Atropine uses

A

Reverses bradycardia and increased BP produced by muscarinis agonists or cholinesterase inhibitors (organophosphate pesticides). Used in MI to decrease bradycardia and/or AV block.

91
Q

Muscarinic antagonists Effect on respiratory system

A

Bronchodilation, inhibit secretions and decrease laryngospasm.

92
Q

Ipratropium uses

A

Bronchodilation in COPD

93
Q

Muscarinic antagonists effect on the GI tract

A

Inhibits motility and GI secretions

94
Q

Dicyclomine uses

A

Antispasmodic for GI tract

95
Q

Diphenoxylate-atropine (Lomotil) uses

A

antispasmodic to decrease diarrhea with a decrease opioid abuse potential.

96
Q

Muscarinic antagonists effect on the GU system

A

relaxes bladder wall to reduce urge to void.

97
Q

Tolterodine uses

A

M3 receptor antagonist that decreases overactive bladder and has little CNS side effects

98
Q

Oxybutynin uses

A

Prevents bladder spasm during prostate surgery.

99
Q

Muscarinic antagonists effect on glands

A

Decreases sweating (can lead to overheating) and decreases salivary secretion.

100
Q

Atropine poisoning symptoms

A

“dry as a bone, blind as a bat, mad as a hatter, red as a beet” Dry mouth, mydriasis, tachycardia, hot/flushed skin, agitation and delirium. Atropine is in TCAs, antihistamines, phenothiazine antipsychotics, mushrooms and jimson weed. Also seen with scopolamine poisoning.

101
Q

Atropine poisoning treatment

A

Cholinesterase inhibitor, diazepam (seizures), ice bags, ethanol.

102
Q

Non-depolarizing NMJ blockers MOA

A

Highly ionized, so much be injected, have no CNS effects. Competitive antagonists. Also block pre junctional sodium channels which interferes with sodium mobilization of Ach. Adding more Ach will overcome the block. Can be reversed using cholinesterase inhibitors.

103
Q

Non-depolarizing NMJ blockers order of paralysis

A

small muscle (eye) followed by limbs and larger muscles. The diaphragm and intercostal muscles are the last to be paralyzed. Recovery occurs in the opposite order.

104
Q

Depolarizing NMJ blockers MOA

A

Succinylcholine. Results in initial stimulation and contraction followed by desensitization and blockade. Onset and recovery occur quickly. Hydrolyzed by plasma pseudocholinesterase (genetic differences) addition of cholinesterase inhibitor will delay recovery.

105
Q

Succinylcholine side effects

A

Cardiac arrest: as sodium influx increases, potassium efflux increases and can cause arrest. Malignant hyperthermia: due to uncontrolled release of calcium from the SR causing muscle rigidity and high temperatures.

106
Q

Succinylcholine contraindications

A

extensive soft tissue damage, rhabdomyolysis, SCI, muscular distrophy. Children younger than 8.

107
Q

Succinylcholine uses

A

Quick procedures such as tracheotomy or intubation.

108
Q

NMJ blockers uses

A

surgery, ventilation, orthopedics (bone setting), intubation, convulsions (ECT).

109
Q

Ganglion blockers MOA

A

Non depolarizing competitive antagonist. Very rarely used because they block all ANS ganglion so inhibit PNS and SNS the effect depends on the predominant tone to that organ.

110
Q

Ganglion blockers effect on the eye

A

Cycloplegia with Mydriasis

111
Q

Ganglion blockers effect on vasculature

A

SNS tone. Vasodilation. Orthostatic hypotension.

112
Q

Ganglion blockers effect on heart

A

Tachycardia and reduced contractility due to reduces vagal tone.

113
Q

Ganglion blockers effect on GU

A

Urinary retention is common.

114
Q

Ganglion blockers effect on sweating

A

reduced but temperature is maintained by vasodilation.

Pharmacology (24 decks)

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