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First Aid: Pharmacology

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What are the 3 cholinergic direct agonists?
BCP - Bethanechol, Carbachol, Pilocarpine
What are the clinical applications and actions of Bethanechol?
Clin: postoperative and neurogenic ileus and urinary retention; Action: activates bowel and bladder smooth muscle
What are the clinical applications and actions of Carbachol?
Clin: glaucoma; Action: activates ciliary muscle of eye (open angle), pupillary sphincter (narrow angle)
What are the clinical applications and actions of Pilocarpine?
Clin: glaucoma; Action: activates ciliary muscle of eye (open angle), pupillary sphincter (narrow angle)
What are the 5 cholinergic indirect agonists?
NPEPE - Neostigmine, Pyridostigmine, Edrophonium, Physostigmine, Echothiophate
What is another term for a cholinergic indirect agonist?
Anticholinesterase
What are the clinical applications and actions of Neostigmine?
Clin: Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative); Action: + endogenous ACh
What are the clinical applications and actions of Pyridostigmine?
Clin: Myasthenia gravis; Action: + endogenous ACh, + strength
What are the clinical applications and actions of Edrophonium?
Clin: Diagnosis of myasthenia gravis (very short-acting); Action: + endogenous ACh
What are the clinical applications and actions of Physostigmine?
Clin: Glaucoma (crosses BBB -> CNS) and atropine overdose; Action: + endogenous ACh
What are the clinical applications and actions of Echothiophate?
Clin: Glaucoma; Action: + endogenous ACh
What are the symptoms of cholinesterase inhibitor poisoning?
DUMBBELSS - Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation (and abdominal cramping)
Which are the reversible cholinergic indirect antagonists?
PENP - Physostigmine, Edrophonium, Neostigmine, Pyridostigmine
What is an antidote to cholinesterase inhibitor poisoning and how does it work?
Pralidoxime - it regenerates active cholinesterase
Name an important muscarinic blocker.
Atropine
What can be one cause of cholinesterase inhibitor poisoning?
Exposure to organophosphates
What are the clinical applications of muscarinic antagonists?
Pupil dilation, - acid secretion in acid-peptic disease, - urgency in mild cystitis, - GI motility, - airway secretions, treat organophosphate poisoning. Also causes + body temp, rapid pulse, dry mouth, dry/flushed skin, disorientation, mydriasis with cycloplegia, and constipation.
What are the actions of muscarinic antagonists?
Blocks SLUD - Salivation, Lacrimation, Urination, Defecation.
Name a nicotinic antagonist and its action.
Hexamethonium - a ganglionic blocker.
What are the side effects of atropine as a block of the PNS?
Blind as a bat, Red as a beet, Mad as a hatter, Hot as a hare, Dry as a bone
Name 4 antimuscarinic drugs.
BSAI - Benzotropine, Scopolamine, Atropine (homatropine, tropicamide), Ipratropium
Name the target organ system and application of Benzotropine.
CNS; Parkinson's disease
Name the target organ system and application of Scopolamine.
CNS; Motion sickness
Name the target organ system and application of Atropine.
Eye; Produce mydriasis and cycloplegia
Name the target organ system and application of Ipratropium.
Respiratory; Asthma and COPD
What is the mechanism of action for Dantrolene?
Prevents the release of Ca++ from the sarcoplasmic reticulum of skeletal muscle.
What are the clinical applications of Dantrolene?
Used to treat malignant hyperthermia, which is caused by the concomitant use of inhalation anesthetics (except N2O) and succinylcholine. Also used to treat neuroleptic malignant syndrome (a toxicity of antipsychotic drugs).
What are the clinical applications of neuromuscular blocking drugs?
Used for muscle paralysis in surgery or mechanical ventilation.
Give an example of a depolarizing neuromuscular blocking drug.
Succinylcholine
Name the 2 phases of depolarizing neuromuscular blockades and possible antidotes.
Phase I (prolonged depolarization) - no antidote. Block is potentiated by cholinesterase inhibitors. Phase II (repolarized but blocked) - antidote consists of cholinesterase inhibitors (eg. neostigmine).
What are 6 examples of nondepolarizing neuromuscular blocking drugs?
TAMPVR - Tubocurarine, Atracurium, Mivacurium, Pancuronium, Vecuronium, Rapacuronium.
How can nondepolarizing neuromuscular blockades be reversed?
Neostigmine, Edrophonium, and other cholinesterase inhibitors.

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