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11 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Cholinergic drugs
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- they are agents that influence the activity of cholinergic receptors
- most mimic or block the actions of acetylcholine - cholinesterase inhibitors ( indirect prevent the breadown of acetylchone. |
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MUSCARINI
Receptor location: - sweat gland - blood vessels - all organs regulated by the parasympathetic nervous system |
Effects of Receptors Activation
(Many include) -lower heart rate - increase gland secretion - smooth muscle contraction |
receptor agonist: Bethanechol (selective)
receptor antagonist : Atropine |
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NICOTINIC N
Receptor location: -all ganglia of the autonomic nervous system |
Effects of Receptors Activation
promotes ganglionic transmission |
receptor agonist: Nicotine
receptor antagonist: Mecamylamine |
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NICOTINIC M
Receptor location - Neuromuscular junction (NMJs) |
Effects of Receptors Activation
Skeletal muscles contraction |
receptor agonist: +++ Nicotine
receptor antagonist : d-Tubocurarine, succinylcholine |
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Indirect- acting cholinomimetics
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cholinesterase inhibitors ( Physostigmine, neostigmine, and other cholinesterase inhibitors)
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can activate all cholinergic receptors by causing accumulation of acetylcholine at cholinergic junctions.
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other muscarinic agonists
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cevimeline,
pilocarpine= glaucoma , acetylcholine = miosis. |
muscarine = present in poisonous mushrooms.
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overactive bladder OAB
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disease :
-urinary urgency - urinary frequency - nocturia - urge incontinence( detrusor instability and involuntary contraction) |
solutions :
- behavioral therapy - drug therapy if ineffective percutaneous tibial nerve stimulation (PTNS) may be tried. |
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Drugs used in OAB are Anticholinergic
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specific anticholinergic :
- Oxybutynin ( Ditropan, Oxytrol, Gelnique) a) syrup b) extended-release tablets c) transdermal patch and gel -Darifenacin -solifenacin -Tolterodine a) immediate-release tablets b) extended-release capsules - trospium -Fesoterodine |
other drugs
-scopolamine - ipratropium bromide - antisecretory anticholinergics -dicyclomine - pirenzepine and telenzepine -mydriatic-cycloplegic centrally acting anticholinergics |
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chp 15
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cholinesterase inhibitors and their use in Myasthenia Gravis
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Cholinesterase Inhibitors
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are
-drugs that prevent the degradation of acetylholine Ach by acetylcholinesterase -viewed as indirect- acting cholinergic agonists - lac selectivity (muscarinic ganglionic, and neuromuscular) - limited therapeutic applications |
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"reversible" Cholinesterase inhibitors
- Neostigmine (Prostigmin) *cannot readily cross mbranes * absobe poorly if oral * minimal effects on brain and fetus * poor substrate for cholinesterase ChE |
M.of A.
*neuromusculareffect - therapeutic dose: increases force of contraction in sckeletal muscle - toxic levels: decrease force of contration *Central nervous system |
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