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Lecture Notes
Glaucoma and ANS Drugs
- Beta blockers (Timolol): aqueous humor↓
- Blood vessels are not affected by the parasympathetic nervsous system since there is no inveration or circulating ACh.
- Sweat Glands are activated by the sympathetic system via muscarinic receptor and are cholinergic
- Acetylcolinesterase breaks down ACh into Choline (product 1) and Acetate (product 2), respectively
----------------------------------------------------------------------------------------------
Parasymathetic System: Urinary Bladder
- Contraction of the Detrusor Muscle
- Relaxation of the Sphincer Muscle
- Parasympathetic activation of muscarinic receptors on smooth muscles cause contraction except for the sphincter.
----------------------------------------------------------------------------------------------
Clinical Uses of Muscarinic Agnoists
Pilocarpine
- Oral: Dry Mouth
- Eye Drop: Glaucoma (aqueous humor drainage)
Methacholine
- Bronchial Challenge (asthma test - bronchioconstriction & secretion)
Bethanechol
- Helps with urination and defacation (rest & digest)
----------------------------------------------------------------------------------------------
Cholinoreceptor Blockers: Effects
- Increases heart rate
- Loss of miosis
- Loss of accommodation
- Loss of eye drainage
- Blood vessels not blocked since there is no sympathetic innervation
- Bronchodilation
- Decrease in urinary retention
----------------------------------------------------------------------------------------------
Cholinoreceptor Blockers: Drugs
Atropine (most common exam distractor)
- Blocks Accomadation
- Prototype muscarinic blocker
Scopolamine
- Motion Sickness
Ipratropium
- COPD (quaternary)
- Designed to locally remain in bronchial smooth muscle and not go to brain.
----------------------------------------------------------------------------------------------
Anticholinergic/Muscarinic Poisoning: Symptoms
1) Blind as a Bat: Unable to accomodate
2) Mad as a Hatter: CNS affected
3) Dry as a Bone: Unable to sweat/Dry mouth
4) Hot as Hell: Hot since can't sweat
5) Red as a Beet: body tries to compensate so you turn red.
- Children are especially sensitive to hyperthermia in anticholinergic poisoning.
- Atropine causes Tachycardia since M2 receptor is blocked which suppresses heart rate
- Bronchodilation is expected with anti-cholinergic drugs.
----------------------------------------------------------------------------------------------
Anticholinergic/Muscarinic Poisoning: Diagnosis
- Anticholinergic poisoning, is usally diagnosed by symptoms, but can be tested using methacholine which is unable to act as agonist due to blockers.
----------------------------------------------------------------------------------------------
----------------------------------------------------------------------------------------------
Nicotinic Receptors
- Ion Channels
- Found in all ganglia, Adrenal Medulla, and NMJ
- Phase 1 Depolarizing Blockade because there is too much agonist
- Phase II receptors don't even respond
----------------------------------------------------------------------------------------------
Parasympathetic Drugs: Nicotinic Receptors
- Succinylcholine is both a nicotinic agonist and a NMJ blocker (if there is too much)
- Curare is an NMJ blocker that causes non-depolarization blockade
- Curare has poor oral bioavailability so hunted meat can be eaten
- Nicotinic agonist increase predominant tone initially but then leads to subsequent suppression
- Toxic doses of nicotinic agonist can cause respiratory depression and paralysis
----------------------------------------------------------------------------------------------
Ganglionic Blockers & Effects
- Mecamylamine and Trimethaphan are competative antagonist that blocks predominant tone
- Postural Hypotension: due to vasodilation
----------------------------------------------------------------------------------------------
Drug Class: Indirect Cholinomimetics/Cholinesterase Inhibitors
- Reversible carbamate inhibitors (~hrs) stuck in carbamulated-AChE
- Irreversible organophosphates (~days) stuck in phosphorylated-AChE (insectasides & nerve gases)
- Noncovalent Inhibitors: Edrophonium and Donepezil
- Reversible Carbamate Inhibitors: Neostigmine and Physostigmine
- Irreversible Organophosphates: Echothiophate
----------------------------------------------------------------------------------------------
Indirect Chlinomimetics Symptoms
Reversible Carbamate Inhibitors
- Neostigmine can't cross the BBB since it's positively charged
- Physostigmine can cross the BBB (used for alzheimers)
----------------------------------------------------------------------------------------------
Anticholinesterase Poisoning: Treatment
- Atropine to block muscarinic effects only
- Pralidoxime reactivates AChE and only used for organophosphate poisoning
----------------------------------------------------------------------------------------------
Anticholinergic Poisoning: Treatment
- Treat symptoms
- Benzodiazepines for delirium/convulsions
- Temperature control/cooling blankets
- Physostigmine/anti-cholinesterase
----------------------------------------------------------------------------------------------
Glaucoma and ANS Drugs
- Beta blockers (Timolol): aqueous humor↓
- Beta blockers (Timolol): aqueous humor↓
- Cholinomimetics (Pilocarpine): outflow↑
- Pilocarpine causes a rapid reduction in IOP
- Alpha agonists: humor↓, outflow↑
- Epinephrine cannot be used in closed angle glaucoma
- Muscarinic blockers are contraindicated since it blocks drainage
- Scopolamine is bad for glaucoma
________________________________________________________- Scopolamine is bad for glaucoma
- Blood vessels are not affected by the parasympathetic nervsous system since there is no inveration or circulating ACh.
- Sweat Glands are activated by the sympathetic system via muscarinic receptor and are cholinergic
- Acetylcolinesterase breaks down ACh into Choline (product 1) and Acetate (product 2), respectively
----------------------------------------------------------------------------------------------
Parasymathetic System: Urinary Bladder
- Contraction of the Detrusor Muscle
- Relaxation of the Sphincer Muscle
- Parasympathetic activation of muscarinic receptors on smooth muscles cause contraction except for the sphincter.
----------------------------------------------------------------------------------------------
Clinical Uses of Muscarinic Agnoists
Pilocarpine
- Oral: Dry Mouth
- Eye Drop: Glaucoma (aqueous humor drainage)
Methacholine
- Bronchial Challenge (asthma test - bronchioconstriction & secretion)
Bethanechol
- Helps with urination and defacation (rest & digest)
----------------------------------------------------------------------------------------------
Cholinoreceptor Blockers: Effects
- Increases heart rate
- Loss of miosis
- Loss of accommodation
- Loss of eye drainage
- Blood vessels not blocked since there is no sympathetic innervation
- Bronchodilation
- Decrease in urinary retention
----------------------------------------------------------------------------------------------
Cholinoreceptor Blockers: Drugs
Atropine (most common exam distractor)
- Blocks Accomadation
- Prototype muscarinic blocker
Scopolamine
- Motion Sickness
Ipratropium
- COPD (quaternary)
- Designed to locally remain in bronchial smooth muscle and not go to brain.
----------------------------------------------------------------------------------------------
Anticholinergic/Muscarinic Poisoning: Symptoms
1) Blind as a Bat: Unable to accomodate
2) Mad as a Hatter: CNS affected
3) Dry as a Bone: Unable to sweat/Dry mouth
4) Hot as Hell: Hot since can't sweat
5) Red as a Beet: body tries to compensate so you turn red.
- Children are especially sensitive to hyperthermia in anticholinergic poisoning.
- Atropine causes Tachycardia since M2 receptor is blocked which suppresses heart rate
- Bronchodilation is expected with anti-cholinergic drugs.
----------------------------------------------------------------------------------------------
Anticholinergic/Muscarinic Poisoning: Diagnosis
- Anticholinergic poisoning, is usally diagnosed by symptoms, but can be tested using methacholine which is unable to act as agonist due to blockers.
----------------------------------------------------------------------------------------------
----------------------------------------------------------------------------------------------
Nicotinic Receptors
- Ion Channels
- Found in all ganglia, Adrenal Medulla, and NMJ
- Phase 1 Depolarizing Blockade because there is too much agonist
- Phase II receptors don't even respond
----------------------------------------------------------------------------------------------
Parasympathetic Drugs: Nicotinic Receptors
- Succinylcholine is both a nicotinic agonist and a NMJ blocker (if there is too much)
- Curare is an NMJ blocker that causes non-depolarization blockade
- Curare has poor oral bioavailability so hunted meat can be eaten
- Nicotinic agonist increase predominant tone initially but then leads to subsequent suppression
- Toxic doses of nicotinic agonist can cause respiratory depression and paralysis
----------------------------------------------------------------------------------------------
Ganglionic Blockers & Effects
- Mecamylamine and Trimethaphan are competative antagonist that blocks predominant tone
- Postural Hypotension: due to vasodilation
----------------------------------------------------------------------------------------------
Drug Class: Indirect Cholinomimetics/Cholinesterase Inhibitors
- Reversible carbamate inhibitors (~hrs) stuck in carbamulated-AChE
- Irreversible organophosphates (~days) stuck in phosphorylated-AChE (insectasides & nerve gases)
- Noncovalent Inhibitors: Edrophonium and Donepezil
- Reversible Carbamate Inhibitors: Neostigmine and Physostigmine
- Irreversible Organophosphates: Echothiophate
----------------------------------------------------------------------------------------------
Indirect Chlinomimetics Symptoms
DUMBBELSS (Diarrhea, Urination, Miosis,
Bronchoconstriction, Bradycardia, Excitation CNS/NMJ, Lacrimation, Salivation,
Sweating)
----------------------------------------------------------------------------------------------Reversible Carbamate Inhibitors
- Neostigmine can't cross the BBB since it's positively charged
- Physostigmine can cross the BBB (used for alzheimers)
----------------------------------------------------------------------------------------------
Anticholinesterase Poisoning: Treatment
- Atropine to block muscarinic effects only
- Pralidoxime reactivates AChE and only used for organophosphate poisoning
----------------------------------------------------------------------------------------------
Anticholinergic Poisoning: Treatment
- Treat symptoms
- Benzodiazepines for delirium/convulsions
- Temperature control/cooling blankets
- Physostigmine/anti-cholinesterase
----------------------------------------------------------------------------------------------
Glaucoma and ANS Drugs
- Beta blockers (Timolol): aqueous humor↓
- Cholinomimetics (Pilocarpine): outflow↑
- Pilocarpine causes a rapid reduction in IOP
- Alpha agonists: humor↓, outflow↑
- Epinephrine cannot be used in closed angle glaucoma
- Muscarinic blockers are contraindicated since it blocks drainage
- Scopolamine is bad for glaucoma
----------------------------------------------------------------------------------------------- Scopolamine is bad for glaucoma
Missed Questions
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Pathoma
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Boards and Beyond
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First Aid
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Sketchy
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Sketchy 2
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Sketchy Extra
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Picmonic
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Pixorize
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Physeo
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Bootcamp
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OME
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Additional Resources
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One by one
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