Term
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Definition
| Cholinergic agonist of the choline ester family. Increases parasympathetic muscle tone --> treats urinary and GI hypotonia. Don't administer if bowel is obstructed but used to restart digestion after surgery. |
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Term
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Definition
M3 specific cholinergic agonist
Treat dry mouth symptom of Sjogrens syndrome
Fewer side effects than pilocarpine |
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Term
| Pilocarpine (aka ocusert, pilocar) |
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Definition
Natural alkaloid chokingeric agonist
Used in treatment of glaucoma (primarily), dry mouth (xerostomia) and reverse effects of atropine. |
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Term
| Side effects associated with muscarinic agonists |
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Definition
| Diarrhea, diaphoresis, miosis, nausea, salivation, urinary urgency, and some CNS disturbances if crosses BBB. |
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Term
| Contraindications for prescribing muscarinic agonists |
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Definition
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Term
| Why can't oral Ach be used as an effective treatment? |
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Definition
| Rapidly degraded by CIRCULATING pseudo-cholinesterases |
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Term
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Definition
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Term
| Name Reversible (short term) AchE inhibitors |
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Definition
| Edrophonium, phystigmine, neostigmine, pyridostigmine, rivastigmine, galantamine, ambenonium, donepezil, tacrine. |
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Term
| irreversible (long term) AchE inhibitors |
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Definition
Organosphospates: Ecothiophate and isoflourophate
Nerve Gases: Sarin, soman |
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Term
Myasthenia gravis
Mechanism of disease?
Mechanism of treatment?
Drugs used to treat? |
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Definition
Autoimmune Ab block/destroy Ach postsynaptic receptors in muscles.
Treated by AchE inhibitors such as neostigmine (can't cross BBB) |
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Term
Neostigmine
Drug class?
Disease used for and side effects? |
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Definition
AchE inhibitor
used in myasthenia gravis b/c it can't cross the BBB and concentrates and the NMJ. Side effects are generalized cholinergic stimulation and drop in BP. Overdose -> cholinergic crisis and paralysis |
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Term
Physostigmine
Class?
Effect?
used for treatment of what? |
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Definition
plant alkaloid and tertiary amine (means it can cross BBB).
increases Ach effect at nicotinic and muscarinic receptors.
Antidote for anticholinergic drugs such as atropine.
Treats glaucoma via reduction of IOP. |
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Term
What is the mnenonic for organosphosphate poisining symptoms?
What pattern do they exhibit? |
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Definition
SLUD
Salivation
Lacrimation
Urination
Defecation
organosphosphates are long term AchE inhibitors so symptoms are all hyperactive parasympathetic responses due to activation of muscarinic and nicotinic receptors. |
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Term
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Definition
| it is when phosphorylated AchE remains inactived for a long period of time (2 hours) and becomes permanently inactivated. |
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Term
| How do you treat organophosphate/nerve gas poisoning? |
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Definition
pyridostigmine prophylactically.
Post exposure administer atropine, scopolamine and pralidoxime |
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Term
| What are atropine and scopolamine? What class do they belong to? |
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Definition
| muscarinic receptor antagonists that are belladona alkaloids. |
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Term
| What are ipratropium, tiotropium, and tolterodine? |
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Definition
| muscarinic receptor antagonists that are synthetic or semi-synthetic. |
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Term
| Clinical uses of atropine? |
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Definition
reversal of severe bradycardia (before epi)
produce mydriasis and cycloplegia (loss of accomadation)
Antispasmodic, suppress respiratory secretions, mushroom and AchE poisining. |
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Term
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Definition
| dry mouth, constipation, dilated pupils, blurry vision (from cycloplegia), hot flushed skin, tachycardia, fever, CNS disturbances. |
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Term
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Definition
| prophylactic for motion sickenss, used in anesthesia for amnesia and sedation, mydriasis |
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Term
| Clinical uses for Ipratropium Bromide and MOA |
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Definition
asthma and COPD to cause bronchodilation along with albuterol.
Used alone if a pt can't use adrenergic agonsits
MOA: blocks muscarinic receptors and thus blocks bronchcoconstriction |
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Term
| another name for Ipratropium Bromide? |
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Definition
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Term
| Spiriva (tiotropium bromide) |
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Definition
| used in COPD and Asthma that is selective for the bronchioles M3 receptor. |
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Term
| Tolterodine (aka ??) and its clinical uses |
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Definition
Aka Detrol
used to treat overactive bladder by blocking the M3 receptor on the detrusor muscle. also blocks PNS input to sphincter preventing leaks |
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Term
| When would an M3 antagoinst be contraindicated? General muscarinic antagonist contraindications? |
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Definition
| most common contraindication is slow voiding and urinary retention as commonly seen in BPH general muscarinic antagonist contraindications: glaucoma, BPH, Mysasthenia Gravis, constipation |
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Term
| What are nicotinic antagonists generally used for? Name 2 |
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Definition
Ganglionic blockers.
Hexamethonium and Trimethophan |
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Term
| Clinical use for NMJ blockers? |
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Definition
| Used to provide complete skeletal muscle relaxation before surgery/anesthesia |
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Term
| What are the two classes of NMJ blockers? |
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Definition
| non-depolarizing and depolarizing blockers |
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Term
| Name the Non-Depolarizing blockers |
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Definition
| Atracurium*, cistracurium, vecuronium, rocuronium, pancuronium, and tubocurarine |
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Term
| What does the suffix -curonium mean? |
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Definition
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Term
| Name a depolarizing NMJ blocker |
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Definition
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Term
| MOA of non-depolarizing NMJ blockers |
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Definition
| competitive blockers of nicotinic receptor preventing Ach from binding. |
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Term
| MOA of succinyl choline including degrading enzymes. |
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Definition
Phase 1:SC is an agonist of nicotinic receptors and initially depolarizes and causes fasciculations, after Ca is sequestered back into SR --> paralysis.
Phase II: membrane repolarizes but SC remains in the NMJ b/c not degraded and therefore resists further depolarization
made of two Achs linked end to end.
Metabolized by plasma cholinesterases and NOT AchE in the NMJ. |
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Term
| Succinyl choline side effects |
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Definition
| Muscle pain post-op, hyperkalemia, bradycardia, increase IOP, malignant hyperthermia (serious) |
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