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Index
»
PHARMACOLOGY 1
»
CHAPTER 5 - CHOLINERGIC ANTAGONISTS
»
Level 2
level: Level 2
Questions and Answers List
Basic & Clinical Pharmacology of the Ganglion-Blocking Drugs
level questions: Level 2
Question
Answer
MOA: unknown MOA in CNS Effects: Reduces vertigo, post-operative nausea CA: Prevention of motion sickness and postoperative N & V
SCOPOLAMINE
Competitively BLOCK THE ACTION of acetylcholine and similar agonists at nicotinic receptors of both parasympathetic and sympathetic autonomic ganglia
Ganglion-Blocking Drugs
• Low dose – depolarizes autonomic ganglia – stimulation • High dose – ganglionic blockade – blood pressure falls and GIT & bladder musculature ceases
NICOTINE
1 Nicotine LOW DOSE: 2 Nicotine HIGH DOSE:
1 depolarizes autonomic ganglia – stimulation 2 ganglionic blockade – blood pressure falls and GIT & bladder musculature ceases
• the FIRST TO BE RECOGNIZED but has a very short duration of action Ganglion-Blocking Drug
Tetraethylammonium (TEA)
• was developed and introduced clinically as the FIRSTS DRUG effective for the management of HYPERTENSION
Hexamethonium
• "C10" analog of hexamethonium • a depolarizing neuromuscular blocking agent
DECAMETHONIUM
• a secondary amine • was developed to IMPROVE THE DEGREE AND EXTENT OF ABSORPTION from the GI tract because the quaternary amine ganglion blocking compounds were poorly and erratically absorbed after oral administration • advocated as a possible ADJUNCT with the transdermal nicotine patch to reduce nicotine craving in patients attempting to quit smoking
MECAMYLAMINE
• a short-acting ganglion blocker • is INACTIVE ORALLY and given via IV infusion Occasionally used in the treatment of HYPERTENSIVE emergencies and dissecting AORTIC ANEURYSM
TRIMETHAPHAN
MOA: unknown MOA in CNS Effects: Reduces vertigo, post-operative nausea CA: Prevention of motion sickness and postoperative Nausea & Vomiting Motion Sickness Drug
SCOPOLAMINE
MOA: competitive antagonist at M3 receptor Effects: Reduces smooth muscle and secretory activity of the gut CA: Irritable bowel syndrome, minor diarrhea For Gastrointestinal Disorders
DICYCLOMINE (Bentyl®)
Longer Duration of Action (google: It works by decreasing the motion of the stomach and intestines and the secretion of stomach fluids, including acid.)
HYOSCYAMINE
similar to dicyclomine
GLYCOPYRROLATE
MOA: competitive antagonist at all M receptors Effects: mydriasis and cycloplegia Clinical Application: RETINA EXAMINATION Contraindication: Glaucoma (OPTHALMOLOGY)
ATROPINE
MOA: Competitive, non-selective antagonist at M receptors Effects: Reduces/prevents bronchospasm CA: Prevention & relief of acute episodes of bronchospasms For RESPIRATORY (Asthma, COPD)
IPRATROPIUM (Atrovent)
MOA: non-selective muscarinic antagonist Effects: Reduces detrusor smooth muscle tone, spasms CA: Urge incontinence, post-operative SPASMS FOR URINARY
OXYBUTININ (Ditropan®)