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47 Cards in this Set
- Front
- Back
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Cholinergic agonist
Natural alkaloid usually goes in eye (topical) reduces intraocular pressure in certain types of glaucoma |
Pilocarpine
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Cholinergic agonist
choline esters uses: - disorders w/ parasymp tone MOA - acts on muscarinic receptors |
Bethanechol
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Cholinergic agonist
new M3 specific agonist fewer side effects than pilocarpine |
Cevimeline
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how does pilocarpine reduce intraocular pressure
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contracs spincter pupillae (M3) and reduces angle block
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muscarinic agoinists side effects
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diarrhea
diaphoresis miosis nausea slaivation urinary urgency CNS distubances ( w/ thse that cross the BBB, i.e pilocarpine) |
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contraindications for muscarinic agonists
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pts. w/ asthma
Heart disease |
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types of ACH esterases
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Acetylcholine esterase ( "real" AChE
pseudo cholinesterase |
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types of pseudo cholinesterases
where and what are they, and what do they do |
plasma cholinesteras
butyryl colinesterase circualing, non-specific esterase that cleave any ester |
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what class of drug prolongs/enhances actions of acetylcholine by inhibiting something
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AChE inhibiitors
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potentila sites of action for AChE inhibitors
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all effector organs innervated by parasympathetic system
NMJ All autonomic ganglia |
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types of AChE inhibitors ( not drug names but types)
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Reversible
irreversible (long) |
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Reversible AChe Inhibitors (short drugs)
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Edrophonium
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Reversible AChe inhibitors (intermediate drugs)
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Physostigmine
Neostigmine Pyridostigmine Rivastigmine Rivastigmine Galanamine Ambenonium Donepezil Tacrine |
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Irreversible ACheE Inhibitors (synthetic organophospate drugs)
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Ecothiophate
Isofluorophate |
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Irreversible AChE inhibitors (Nerve Gases)
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Sarin
Soman |
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Clinical uses for AChE inhibitors
and the drug that is used for a diagnostic test (name) |
Myasthenia Gravis
Hypotonia of Bladder and GI Glaucoma Alzheimers Edrophonium (diagnostic test for myasthenia Gravis) |
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what is myasthenia Gravis, what type of drug do you use to treat, and what is its MOA
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an autoimmun neuromucular disease where antibodies destroy ACh receptors at the NMJ.
AChE inhibitors are used allows for more ACh to stay inthe cleft of the NMJ longer to react with what receptors are remaining. |
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AChE inhibitor drug that doesn't enter brain and has a greater effect at the NMJ than physostigmine
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Neostigmine
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AChE inhibitor drug tha is a plant alkaloid and tertiary amine that can cross the BBB.
potentiats Ach effest ath muscarinic and nicotinci receptors of the ANS and also Nicotinic at the NMJ |
Physostigmine
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adverse effects of Physostigmine
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diarrhea
nausea sweating, miosis urinary urgency convulsions (high doses) bradycardia (high doses) hypotension (high doses) |
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Muscarinic Receptor Antagonists
Belladona alkaloids |
Atropine
Scopolamine |
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MUscarinic Receptor Antagonists
Synthetic and Semi-synthetic derivatives |
Ipratropium
Tiotropium Tolterodine |
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side effects of Atropine
does dosage amount affect the side effects, if so how |
Dry mouth
Constipation Dilated Pupils (mydrasis Blurred vison due to cycloplegia Hot, dry flushed skin Tachycardia Fever CNS Disturbances from the top of this list is the lower dosages, as the dosage increases, the items at the bottom of the list occure |
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use this drug as a reversal to severe bradycardia, to produce mydriasis and cycloplegia
a Muscarinic Receptor Antagonist used: to treat organophospate insecticide poisoning and to treat mushroom poisoning |
Atropine
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a Muscarinic Receptor Antagonist used:
as a prophylactic for motion sickness and adjunt drug in anesthesia to produce sedation and amnesia drug that crosses the BBB better than atropine |
Scopolamine
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a Muscarinic Receptor Antagonist used: in asthma and COPD as an adjunct to albuterol
has minimal inhibitory effect on mucociliary clearance when compared to atropine reduces broncoconstriction mediated by parasympathetic activity |
Ipratropium Bromide
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a Muscarinic Receptor Antagonist used: with COPD and Asthma that is much more selective at the Bronchioles by haveing a greater affinity for M3 vs. M2
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Tiotropium Bromide
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a Muscarinic Receptor Antagonist used: to treat and overactive Bladder by blocking M3 receptors on detrucer muscle and blocks parasympathetic tone to the spincter and prevents leaks
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Tolterodine
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contraindication for M3 Antagonists
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individuals with urinary retention i.e BPH
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Muscarinic antagonist contraindications
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Glaucoma
Bengn prostatic Hyperplasia kidney condition w/ urination problems Myasthenia Gravis Excessive constipation |
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NMJ blockers ( classes)
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Non-depolarizing blockers
dpolarizing blockers |
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non-depolarizing NMJ Blockers
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Atracurium
Cistracurium Vecuronium Rocurnium Pancuronium Tubocurarine |
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Depolarizing NMJ blockers
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Succinyl Choline
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what do non depolarizing NMJ blockers do, and can it be overcome, if so how
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block the nicotinic receptor at the NMJ and prevent actions of acetylcholine. can be overcome by increasing the amount of Ach in the synaptic cleft
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what do depolarizing NMJ blockers do, both phases
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Phase I initially depolarized the muscle membrane and casues fasiculations, the calcium is removed back tino SR and muscle relaxes causing flaccid paralysis
Phase II membrane is repolarized but the muscle is resistant to further activation by acetylcholine |
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what is different between succinylcholine and acetylcholine
what does this cause |
succinylcholine is not hydorlised by acetylchlinesterase, so it stays in the junction longer, this causes desensitization
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side effects of succinylcholine
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muscle pain post op
hyperkalemia decreased heart rate and increased IOP ( at high doses blocking ganglionic nicotinic receptors) Malignant jyperthermia( serious side effect) |
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Neurotransmitters and receptors
pathway or sympathetic adrenal medulla |
Preganglionic uses ach to a nicotinic receptor on the adrenal medulla, releasing epinephrine which acts on an adrenergic receptor on the effector organ
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Neurotransmitters and receptors
pathway for sympathic to effector organs |
preganglionic - ach
receptor - nicotinic post ganglonic - norepi receptor - adrenergic |
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Neurotransmitters and receptors
pathway for parsympathetic to effector organ |
preganglionic - ach
receptor - nicotinic postganglionic- ach receptor - muscarinic |
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Neurotransmitters and receptors
pathway for somatic |
neurotransmitter - ach
receptor - nicotinic |
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what are the ach receptors subtypes
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muscarinic
Nicotinic |
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what are the muscarinic subtypes
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odd, excitatory (M1, M3, M5)
even, inhibitory (M2, M4) |
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what are the nicotinic receptor sub types
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Neuronal
Skeletal muscle |
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what are the excitatory muscarinic receptors coupled with and do
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Coupled to Gq/11
Activation of PLC |
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what are the inhibitory muscarinic receptors coupled with and do
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coupled to Gi
inhibiton of Adenylate cyclase |
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what are the adrenergic receptors and what do they do
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Alpha 1- Gq simulaton of PLC
Alpha 2 - GI, inhibition of AC Beta 1 - GS, Stimulation of AC Beta 2 - GS, Stimulaton of AC |
