Cholinergic drugs Flashcards Preview

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Flashcards in Cholinergic drugs Deck (114):
1

Acetylcholine (Miochol)

Direct-Acting cholinergic agonist

2

Bethanechol (Urecholine)

Direct-Acting muscarinic agonist

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Pilocarpine (Isopto Crpine; Pilocar)

Direct-Acting muscarinic agonist

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Cevimeline (Evoxac)

Direct-Acting muscarinic agonist

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Nicotine

Direct-Acting nicotinic agonist

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Varenicline (Chantrix)

Direct-Acting nicotinic agonist

7

Neostigmine (Prostigmin)

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

8

Edrophonium (Tensilon)

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

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Physostigmine (Eserine)

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

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Echothiophate

Cholinesterase Inhibitor. Organophosphate.

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Donepezil (Aricept)

Cholinesterase Inhibitor

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Organophosphate Pesticides

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

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Pralidoxime (2-PAM)

Cholinesterase Inhibitor.

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Atropine (generic)

Cholinergic Antagonist

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Scopolamine (TransDerm Scop)

Cholinergic Antagonist

16

Glycopyrrolate (Robunil)

Cholinergic Antagonist

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Dicyclomine (Bentyl)

Cholinergic Antagonist

18

Tolterodine (Detrol)

Cholinergic Antagonist

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Fesoterodine (Toviaz)

Cholinergic Antagonist

20

Darifenacin (Enablex)

Cholinergic Antagonist

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Solifenacin (Vesicare)

Cholinergic Antagonist

22

Oxybutynin (Ditropan)

Cholinergic Antagonist

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Ipratropium (Atrovent)

Cholinergic Antagonist

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Diphenoxylate-atropine (Lomotil)

Cholinergic Antagonist

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Tropicamide (Mydriacyl)

Cholinergic Antagonist

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Homatropine (Isoptohomatropine )

Cholinergic Antagonist

27

d-Tubocurarine

Non-Depolarizing Neuromuscular Blockers

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Vecuronium (Norcuron)

Non-Depolarizing Neuromuscular Blockers

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Cisatracurium (Nimbex)

Non-Depolarizing Neuromuscular Blockers

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Succinylcholine (Anectine)

Depolarizing Neuromuscular Blockers

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Mecamylamine (Inversine)

Ganglion blocker

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Hexamethonium

Ganglion blocker

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Cholinergic stimulants

cholinergic agonists and cholinesterase inhibitors

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Acetylcholine MOA

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

35

Bethanechol (Urecholine) MOA

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

36

Pilocarpine (Pilocar) MOA

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

37

Cevimeline MOA

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

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Nicotine MOA

Stimulates nicotinic receptors.

39

Varenicline MOA

Stimulates nicotinic receptors.

40

Varenicline Uses

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

41

Muscarinic Agonists MOA

either interact with Gq or Gi

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Muscarinic Agonists effect on the eye

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

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Muscarinic Agonists effect on the heart

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

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Muscarinic Agonists effect on Respiratory system

Bronchoconstriction especially in asthmatics

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Methacholine uses

Diagnosis of asthma

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Muscarinic Agonists effect on GI system

Increased secretions and peristalsis. Sphincters are relaxed.

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Muscarinic Agonists effect on Glands

Increases salivation, lacrimation and nasopharyngeal glands.

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Muscarinic Agonists effect on GU

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

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Muscarinic Agonists effect on Brain

M1 muscarinic receptors in the brain are involved in memory.

50

Use for pilocarpine

Glaucoma DOC. Dry mouth but can cause profound sweating.

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Uses for Bethanechol

Stimulates peristalsis and treats urinary retention

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Uses for cevimeline

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

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Muscarinic Agonist Side effects

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

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Muscarinic Agonist contraindications

Peptic ulcers, coronary insufficiency, asthma.

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Nicotinic Agonsits MOA

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

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Nicotinic Agonists Central effects

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

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Nicotinic Agonists effect on the heart

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

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Nicotinic Agonists effect on GI

PNS. Vomiting, diarrhea and urination.

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Nicotinic Agonists effect on the neuromuscular junction

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

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Nicotinic Agonists Side Effects

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

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Nicotine poisoning treatment

Atropine, anticonvulsants and mechanical respiration

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Cholinesterase inhibitors MOA

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.

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Cholinesterase inhibitors carbamates

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

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2-PAM uses

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

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Cholinesterase inhibitors effect on the brain

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

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Cholinesterase inhibitors effect on the eye

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

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Cholinesterase inhibitors effect on the respiratory system

PNS. Bronchoconstriction and increased mucus secretion.

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Cholinesterase inhibitors effect on the GI tract

PNS. Increased perastilis and relaxation of the sphincters.

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Cholinesterase inhibitors effect on the heart

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

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Cholinesterase inhibitors effect on the NMJ

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

71

Neostigmine uses

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

72

Physostigmine uses

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

73

Donepezil uses

Alzheimer's disease. Absorbed into the CNS.

74

Edrophonium uses

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.

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Echothiophate uses

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

76

Irreversible cholinesterase inhibitor toxicity symptoms

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

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Irreversible cholinesterase inhibitor toxicity treatment

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

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Muscarinic antagonists MOA

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

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Atropine on the CNS

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

80

Scopolamine on the CNS

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

81

Scopolamine uses

Prevents motion sickness. Administered as a patch.

82

Benztropine uses

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

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Muscarinic antagonists effects on the eye

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

84

Muscarinic antagonists contraindications

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

85

Tropicamide uses

Mydriasis and cycloplegia for eye examinations

86

Homatropine uses

Mydriasis and cycloplegia for eye examinations

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Muscarinic antagonists side effects

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

88

Muscarinic antagonists effect on the heart

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

89

Glycopyrrolate uses

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

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Atropine uses

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

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Muscarinic antagonists Effect on respiratory system

Bronchodilation, inhibit secretions and decrease laryngospasm.

92

Ipratropium uses

Bronchodilation in COPD

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Muscarinic antagonists effect on the GI tract

Inhibits motility and GI secretions

94

Dicyclomine uses

Antispasmodic for GI tract

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Diphenoxylate-atropine (Lomotil) uses

antispasmodic to decrease diarrhea with a decrease opioid abuse potential.

96

Muscarinic antagonists effect on the GU system

relaxes bladder wall to reduce urge to void.

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Tolterodine uses

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

98

Oxybutynin uses

Prevents bladder spasm during prostate surgery.

99

Muscarinic antagonists effect on glands

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

100

Atropine poisoning symptoms

"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

Atropine poisoning treatment

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

102

Non-depolarizing NMJ blockers MOA

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

Non-depolarizing NMJ blockers order of paralysis

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

Depolarizing NMJ blockers MOA

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

Succinylcholine side effects

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.

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Succinylcholine contraindications

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

107

Succinylcholine uses

Quick procedures such as tracheotomy or intubation.

108

NMJ blockers uses

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

109

Ganglion blockers MOA

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

Ganglion blockers effect on the eye

Cycloplegia with Mydriasis

111

Ganglion blockers effect on vasculature

SNS tone. Vasodilation. Orthostatic hypotension.

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Ganglion blockers effect on heart

Tachycardia and reduced contractility due to reduces vagal tone.

113

Ganglion blockers effect on GU

Urinary retention is common.

114

Ganglion blockers effect on sweating

reduced but temperature is maintained by vasodilation.