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| 2 types of cholinergic receptors and subtypes |
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| muscarinic (G protein link,1-5, M2-heart and smooth muscle, M3- glands and endothelium, M1,4,5-nerves), nicotinic (ion channel-mediated, M-skeletal muscle, N-autonomic ganglion cells). both are activated by acetylcholine ->(acetylcholinesterase) choline and acetic acid |
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| primary neurotransmisster for cholinergic system |
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| muscarinic receptors derived from |
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| nicotinic receptors derived from |
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| excessive amnts of acetylcholine causes |
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| downregulation of amnt released by nerve cells |
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| elicit cholinergic reaction. 2 classes: alkaloids and choline esters, directly activate the acetylcholine receptor |
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| elicit cholinergic reaction, irreversible or reversible, inhibit acetylcholinesterase to prolong the effects of endogenous acetylcholine neurotransmitter |
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| muscarinic receptor activity. Acetylcholine gets released from the nerves and can bind onto this G protein muscarinic receptor. What's illustrated here is the M two receptor. Excessive amount of acetylcholine, besides being activated by acetylcholinesterase, also results in downregulation of acetylcholine being released from the cell from nerve cells. So, therefore, this also slows down the activity of acetylcholine in this muscarinic receptor. |
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| nicotinic receptor activity. acetylcholine bind onto this ion channel, which results in an action potential to occur, which ultimately result in some sort of skeletal muscle action, whether it's muscle contraction, muscle relaxation, so on, so forth |
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| directing acting cholinoreceptor-activating drugs table |
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[image]
acetylcholine is highly susceptible to breakdown and is non-selective, binds to both muscarinic and nicotinic receptors equally, DOA a few sec so not a practical drug to give. methyl choline a lot less susceptible to cholinesterase DOA prolonged, more muscarinic selective |
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| cholinoreceptor-activating, methacholine (met a cool lad and dined), carbachol (carbs and alcohol), bethanechol (bet you won't call), succinylcholine. poorly absorbed in GI tract and CNS (have NH4 component making them charged) |
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| cholinoreceptor-activating, pilocarpine (pill car pine), lobeline (lobe line) (have NH3, not charged, will absorb in GI tract and CNS) |
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| mnemonic to remember what happens when you give someone cholinoceptor-activating drugs |
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Definition
| DUMBBELS- defecation, urination (relaxation of sphincters), Miosis (narrow pupils), bronchospasm, bronchorrea (bronchial smooth muscle contraction, harder to breathe), Bradycardia (lowering heart rate), emesis (vomiting), lacrimation, salivation, secretory (tears and sweats) |
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| activating nicotinic receptors |
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Definition
if activate M subtype N(M)- can either get a disorganized fasciculation of each skeletal muscle motor unit, or have a strong contraction of the entire muscle
if activate N subtype receptor N(N)- nerve, either get excitatory postsynaptic potential activation or inhibitory postsynaptic potential, very unpredictable |
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| Excitatory postsynaptic potentials (EPSPs) |
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| Inhibitory postsynaptic potentials (IPSPs) |
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| cholinesterase-inhibiting drugs |
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Definition
inhibit acetylcholinesterase, prolong effects of endogenous acetylcholine, 3 classes:
-simple alcohol w NH4 (charged)- edrophonium (ed phone him)
-carbamates- not charged: physostigmine (fight or stick me), carbaryl (carry a barrel), charged: neostigmine (new stick me), pyridostigmine (pie rid or stick me)
-organoposphates- echothiophate (echo my fate)(charged), malathion (marathon)(not charged), sarin (sawr him)(not charged)
-highly liposoluble (rapid CNS penetration) except for echothiphate, not charged except for carbaryl
-used for insecticide and biochemical warfare
-organophosphate binds the strongest, then carbamates and edrophonium |
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| more tightly a drug is bound to the receptor.. |
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Definition
| longer duration of action and harder it is to get rid of the drug's effect |
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| cholinesterase inhibitor with longest duration of action |
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Definition
| echothiophate (echo my fate) - 100 hrs, strongest binding |
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| cholinesterase inhibitor with shortest duration of action |
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| edrophonium (ed phone him) - 5-15 min), bound less strongly |
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| how to reverse carbamate effect |
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| how to reverse organophosphate effect |
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Definition
| high-dose prolonged atropine, maybe pralidomine/2-PAM (given to EMT responders in the case of a terrorist attack) |
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| cholinesterase-inhibitor drugs affects |
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| muscarinic effects same as cholinoreceptor-activating drugs, DUMBBELLS. nicotinic effects of cholinesterase-inhibitor drugs causes prolonged effects of acetylcholine: inc muscle tone, while cholinoreceptor-activating drugs cause dec muscle tone and flaccid paralysis due to rapid depolarization causing muscle twitching then leading to flaccid muscle |
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| acetylcholinesterase-inhibiting drugs cause |
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| Myasthenia gravis treatment and what is it (common usage) |
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| (skeletal muscle weakness bc not enough acetylcholine receptors in body) cholinesterase-inhibiting drugs (neostigmine-new stick me and pyridostigmine-pie or stick me (Edrophonium has too short a DOA)(Pysostigmine [not charged, penetrates CNS, not best choice]). acetylcholine-activating drugs wont' work here bc don't have enough functioning cholinergic receptor- Nm) |
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| inducing neuromuscular paralysis drug (common usage) |
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| cholinoreceptor-activating drug: succinylcholine- make skeletal muscle vibrate, send mult action potentials to it then goes flaccid. when pt needs to be intubated |
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| Alzheimer's disease treatment (common usage) |
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| cholinesterase-inhibiting drugs- donepezil (don a present) and galantamine (galantly mine) |
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| uncommon drug usage treatment for reflux esophagitis and agent we use now |
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uncommon- cholinoreceptor-activating drug: inc tone of lower esophageal sphincter and prevent acid from spilling in from the stomach to the esophagus
today- PPIs |
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| uncommon drug usage treatment for glaucoma and agent we use now |
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cholinesterase-inhibiting drugs or cholinoreceptor-activating drug- improves disease by increasing intraocular pressure causing lacrimation
today- topical beta blockers and prostate gland and derivatives |
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| uncommon agent for supraventricular tachyarrythmia |
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Definition
cholinesterase-inhibitor drugs: inc adrenergic, dec acetylcholine activity
agents today: beta blocker and calcium channel blocker |
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| urinary retention uncommon usage drug |
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Definition
| cholinesterase drugs caused sphincter to relax. now use tamulosin |
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| uncommon indication for antimuscarinic drug intoxication |
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| drug enhances acetylcholine effects, replaced by benzodiazepines |
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Definition
cholinergic- parasympathetic
charged- won't absorb well in GI or CNS
muscarinic effects- DUMBELLS, same for cholinoreceptor activators and cholinesterase inhibitors
nicotinic effects- cholinoreceptor activators dec muscle tone and cholinesterase- inhibitors do the opposite |
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