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Adrenergic & Cholinergic Drugs Flashcards

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1
Q

Acetylcholine

A

Direct nicotinic and muscarinic agonist, choline ester, quaternary ammonium, rapidly hydrolyzed by Ach-ase.

Used to obtain rapid miosis in cataract surgery.

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2
Q

Methancholine

A

Direct muscarinic agonist. Choline ester, quaternary ammonium. More resistant to Ach-ase.

Used to diagnose bronchial airway hyperreactivity.

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3
Q

Bethanechol

A

Direct muscarinic agonist. Choline ester, quaternary ammonium. More resistant to Ach-ase.

Used to treat atony of post-op urinary retention and atony of the bladder.

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4
Q

Pilocarpine.

A

Direct partial muscarinic agonist. natural alkaloid. Tertiary amine. Resistant to ach-ase.

Used to treat glaucoma and dry mouth after radiotherapy.

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5
Q

Nicotine

A

Direct nicotinic receptor agonist. Natural alkaloid. Tertiary amine.

At low dose it will stimulate both sympa and parasympa ganglions by depolarization. At high doses it will cause ganglionic and neuromuscular blockade.

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6
Q

Edrophonium

A

Choline-esterase inhibitor. (indirect-acting cholinergic agent). Short-lived reversible inhibition. Quaternary ammonium, does not enter CNS.

Used to diagnose Myasthenia Gravis. Used to reverse neuromuscular block produced by non-depolarizing muscular blockers.

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7
Q

Phyostigmine

A

Choline esterase inhibitor (indirect cholinergic agent). Tertiary amine. Can enter and act in CNS. Carbamate- forms covalent bond with ach-ase.

Used to treat overdoses of anticholinergic drugs.

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8
Q

Neostigmine

A

Choline esterase inhibitor (indirect cholinergic agent). Quaternary ammonium, can’t enter CNS. Carbamate- forms covalent bond with ach-ase.

Used to treat urinary retention, myasthenia gravis, and reverse effects of non-depolarizing neuromusc blockers afer surgery.

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9
Q

Pyridostigmine

A

Choline esterase inhibitor (indirect cholinergic agent). Quaternary ammonium, can’t enter CNS. Carbamate- forms covalent bond with ach-ase.

Used to treat myasthenia gravis.

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10
Q

Organophosphates

A

Phosphorylate Ach-ase. Disables ach-ase for a while. Synthetic and extremely toxic.

Malathion: insecticide
Sarin: nerve agent

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11
Q

Atropine

A

Muscarinic Antagonist. Belladonna Alkaloid. Reversible competitive. Tertiary amine. both CNS and PNS

Used to block respiratory tract secretions prior to surgery. Antidote for cholinergic agonists.

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12
Q

Scopolamine

A

Muscarinic Antagonist. Belladonna Alkaloid.

Treats motion sickness

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13
Q

Ipatropium

A

Muscarinic Antagonist. Synthetic quaternary ammonium.

Used to treat COPD and asthma.

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14
Q

Tropicamide

A

Muscarinic antagonist. Synthetic tertiary amine.

Used to induce mydriasis with cycloplegia (lens muscle paralysis)

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15
Q

Hexamethonium

A

Nicotinic antagonist. Ganglion blocker.

Was used to treat hypertension in the past.

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16
Q

Tubocurarine

A

Neuromuscular blocker. Nondepolarizing, competitive antagonist.

Used as an adjuvant in anaesthesia to relax skelet muscle.

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17
Q

Succinylcholine

A

Neuromuscular blocker. Depolarizing agonist. Leads to rapid receptor desensitization and flaccid paralysis.

Used for rapid endotracheal intubation. Also electroconvulsive therapy.

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18
Q

Botulinum Toxin

A

Presynaptic acetylcholine release inhibitor.

Treats muscle spasms also used cosmetically for wrinkles.

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19
Q

Epinephrine

A

Agonist at both alpha and beta receptors. Endogenous catecholamine. At low concentrations mainly acts on b1 and b2. At higher concentrations, a1 effects are more pronounced.

Used for anaphylactic shock, acute asthmatic attacks, cardiac arrest.

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20
Q

Norepinephrine

A

Agonist at a1, a2 and b1 receptors. Little action on b2 receptors. Endogenous catecholamine.

Used to treat shock because it increases blood pressure via peripheral vasoconstriction.

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21
Q

Isoproterenol

A

Non-selective Beta agonist. Activates B1 and B2 receptors.

B1 effect- increases heart rate contractility. B2 effect- dilates arterioles in skelet muscle, also bronchodilates. Sys bp stays the same, dia bp falls.

Used in emergencies to stimulate heart rate in bradycardic or heart block patients.

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22
Q

Dobutamine

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A

Beta-1 selective agonist.

Produces moderate hr increase and moderate pvr decrease, but less than isopreterenol. Mild vasodilation.

Used in the dobutamine stress echocardiogram because it increases myocardial o2 consumption. Also used to manage acute heart failure and cardiogenic shock.

23
Q

Albuterol

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A

Beta-2 selective agonist. Causes bronchodilation.

Used in asthma (drug of choice)

24
Q

Phenylephrine

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A

Alpha-1 selective agonist. Causes vasoconstriction (a1 effect).

Used as a nasal decongestant and mydriatic. Can be used in combination with tropicamide for mydriasis.

25
Clonidine
Alpha-2 selective agonist. Partial agonist. Used as an antihypertensive. Acts centrally on presynaptic alpha-2 receptors. Reduces overall sympathetic outflow.
26
Amphetamine
Releasing Agent. Indirect-acting adrenergic agonist. Causes norepinephrine release from presynaptic terminals. Potentiate effects of endogenous norepi. Central stimulant, increases blood pressure by alpha action on vasculature and beta action on heart. Used to treat ADHD and Narcolepsy.
27
Tyramine
Releasing Agent. Indirect-acting adrenergic agonist. Causes norepinephrine release from presynaptic terminals. Potentiate effects of endogenous norepi. Not really a medication, but found in fermented foods such as cheese and wine. Can be dangerous to people taking MAO inhibitors by creating vasopressor episodes.
28
Cocaine
Uptake Inhibitor. Indirect-acting adrenergic agonist. Blocks monoamine reuptake.
29
Ephedrine
Mixed-acting Adrenergic Agonist. Induce norepinephrine release. Penetrates the CNS. Isn't removed by MAO or COMT - long action. Used as a pressor agent during spinal anesthesia.
30
Pseudoephedrine
Mixed-acting Adrenergic Agonist. Induce norepinephrine release. Enantiomer of Ephedrine. Available OTC as a decongestant.
31
Phenoxybenzamine
Non-selective alpha antagonist. Irreversible antagonist. Doesn't reduce hypertension. Used to treat pheochromocytoma prior to surgical removal of the tumor.
32
Phentolamine
Non-selective alpha antagonist. Reversible antagonist. Used to treat pheochromocytoma induced hypertension prior to surgical removal of the tumor. Used to treat hypertensive crisis due to stimulant overdose.
33
Prazosin
Alpha 1 selective blocker. Lowers blood pressure by relaxing vascular smooth muscle. Used to treat hypertension but NOT drug of choice. Used as symptom relief for BPH- drug of choice. Relaxes smooth muscle in bladder neck, prostate capsule and urethra.
34
Propranolol
Non selective Beta blocker. Slows heart rate and decreases heart contractility (b1 blockage). Can cause respiratory crisis in patients with COPD and asthma (b2 blockade). Decreases glycogenolysis and Glucagon secretion (b2 blockade)
35
Atenolol
Beta 1 selective blocker. Used as a hypertensive in patients with impaired pulm function or diabetes.
36
Pindol
Partial Beta Agonist. Preferred in individuals with diminished cardiac reserve or propensity to bradycardia.
37
Carbachol
Muscarinic & Nicotinic Agonist Obtain Miosis during surgery & reduce intraocular pressure after surgery
38
Echothiophate
Organophosphate Quaternary ammonium Rarely used for open-angle glaucoma
39
Pralidoxime
Reactivates inhibited ache by splitting phosphate bond. Doesn't enter CNS so can't reverse CNS effects of OP poisoning.
40
Donepizil
Centrally acting AchE inhibitor Treat alzheimers
41
Rivastigmine
Centrally acting AchE inhibitor Treat alzheimers
42
Galantamine
Centrally acting AchE inhibitor Treat alzheimers
43
Tiotropium
Muscarinic Antagonist Used to treat COPD and asthma
44
Cyclopentolate
Muscarinic Antagonist. Tertiary Amine Produce Mydriasis with Cycloplegia
45
Homatropine
Muscarinic Antagonist. Tertiary Amine Produce Mydriasis with Cycloplegia
46
Benztropine
Muscarinic Antagonist Tertiary Amine Treat Parkinsonism & extrapyramidal effects of antipsychotics
47
Trihexyphenidyl
Muscarinic Antagonist Tertiary Amine Treat Parkinsonism & extrapyramidal effects of antipsychotics
48
Glycopyrrolate
Muscarinic Antagonist Quaternary ammonium Reduce secretions & prevent bradycardia in surgery. Treat COPD & adjunct treatment for peptic ulcer.
49
Oxybutynin
Muscarinic Antagonist Treat overactive bladder
50
Tolterodine
Muscarinic Antagonist Treat overactive bladder
51
Dantrolene
Blocks release of Calcium from muscle sarc-reticulum. Treat malignant hyperthermia caused by succinylcholine.
52
Hemicholinium-3
Acetylcholine Synthesis Inhibitor Blocks choline transporter thus inhibiting synthesis. Used as a research tool.
53
Vesamicol
Acetylcholine Storage Inhibitor Blocks Ach-H antiporter which packages Ach into vesicles. Used as a research tool.

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