-
Methacholine
- MAChR Agonist: ^M3
- Dx of Airway Hyperreactivity: Methacholine Challenge with low-dose Provocholine
- No effect on non-asthmatics
-
Bethanachol
- MAChR Agonist:
- Tx: ^GI (postop GIatony, Congenital Megacolon), ^Detrusor (postop retention, spinal injury, non-obstructive)
- Long t1/2: not a substr for AChE
-
Pilocarpine
- MAChR Agonist:
- Tx: Glaucoma, Xerostomia (radiation, Sx, Sjogren's)
- Sides: Diaphoresis, CNS effects (tertiary amine)
-
Carbachol
- NAChR/MAChR Agonist: <NAChR
- Tx: Glaucoma (if pilocarpine uneffective)
- Long t1/2: not a substr for AChE
- Sides: Ganglionic stim.
-
Neostigmine
- AChE Inh:
- Tx: ^SM (GIatony, Detrussor atony), Glaucoma, MG, Reverse NMJ blockers
- Quaternary: no CNS effect
-
Pyridostigmine
- AChE Inh:
- Tx: most common Tx for MG
- Longer t1/2 than neostigmine
- Quaternary: no CNS effect
-
Physostigmine
- AChE Inh:
- Tx: Anticholinergic OD (atropine, antipsychotic/depressant)
- Tertiary: crosses BBB
-
Edrophonium
- AChE Inh:
- Dx of MG: Tensilon Test
- Rapid onset, Short Duration
-
Tacrine (Cognex)
- Long-Acting AChE-Inh: (Cognex)
- Tx: Alzheimer's
-
Donepezil (Aricept)
- Long-Acting AChE-Inh: (Aricept)
- Tx: Alzheimer's
-
Rivastigmine (Exelon)
- Long-Acting AChE-Inh: (Exelon)
- Tx: Alzheimer's
-
Galantamine (Reminyl)
- Long-Acting AChE-Inh: (Reminyl)
- Tx: Alzheimer's
-
Echothiophate
- Irrev. AChE-Inh: Plates AChE, then "ages"
- Tx: Glaucoma (powerful, persistent miosis)
- Quaternary: doesn't penetrate skin
-
OP-toxin
Irrev. AChE-Inh: Plates AChE, then "ages"
-
Pralidoxime (2-PAM)
- 2-PAM: reverses Plation of AChE (OP-toxin, Saran)
- Must be given before "aging"
-
Atropine
- Competitive MACh Antagonist:
- Tx: Retinal Exam (mydriasis), Resp. (bronchD, dries secretion, but inh mucociliary), Heart (trachy after slight brady, post-MI brady, AV block), IBS, OB
- Antidote for "Cholinergic Crises": OP-toxin, Mushroom poison, Saran, excessive stigmine in MG Tx
-
Scopolamine
- Competitive MAChR Antagonist:
- Tx Systemic: Retinal Exam (mydriasis), Resp. (bronchD, dries secretion), Heart (trachy after slight brady, post-MI brady, AV block), IBS, OB
- Tx CNS: Motion sickness, Parkinsonism
- Antidote for "Cholinergic Crises": OP-toxin, Mushroom poison, Saran, excessive stigmine in MG Tx
- Sides: depression, amnesia
-
Ipratropium (Atrovent)
- Competitive MAChR Antagonist: (Atrovent)
- Tx: Asthma/COPD
- Doesn't inh mucociliary clearance
-
Tiotropium (Spiriva)
- Competitive M3 Antagonist: (Spiriva)
- Tx: COPD
- less M2 affinity
- doesn't inh mucociliary clearance
- long t1/2: once-a-day
-
Pirenzepine
- Competitive M1 Antagonist:
- Tx: Peptic Ulcers (inh M1 of parietal cells & PNS ganglia)
-
Tolterodine (Detrol)
- M3 Antagonist: (Detrol)
- Tx: OB
-
Oxybutynin (Ditropan)
- M3 Antagonist: (Ditropan)
- Tx: OB
-
Darifenacin (Enablex)
- M3 Antagonist: (Enablex)
- Tx: OB
-
Solifenacin (Vesicare)
- M3 Antagonist: (Vesicare)
- Tx: OB
-
Varenicline (Chantix)
- Partial CNS NAChR Agonist: (Chantix)
- Tx: smoking cessation
-
Mecamylamine
- Nn Antagonist: Gang blocker (PNS & SNS)
- Tx: AntiHT (last resort)
-
d-Tubocurarine
- Competitive Nm Antagonist: Paralysis for Sx
- Sides: some Nn activity, Histamine release
-
Doxacurium
- Competitive Nm Antagonist: Paralysis for Sx
- less histamine
- longer duration of action
-
Rocuronium
- Competitive Nm Antagonist: Paralysis for Sx
- least potent- high doses
- Rapid onset
- little histamine
-
Atracurium
- Competitive Nm Antagonist: Paralysis for Sx
- little histamine
- intermediate duration of action
- No Renal/Hepatic metab: ideal for kidney/liver disease
-
Mivacurium
- Competitive Nm Antagonist: Paralysis for Sx
- Short Duration
- substr for PseudoChE: beware def.
- some histamine
-
Succinylcholine
- Depolarizing Nm Antagonist: Paralysis for Sx
- Very rapid, Very short (substr for PseudoChE, not AChE)
- Sides: Hyperkalemia (releases Ca: burns, ^arrhythmia), Myalgia, may stim Nn
- Malignant Hyperthermia: in combo w/ anesthetics: rigidity/heat prod., calcium release from SR
- Tx: Dantrolene (inh Ca release from SR) & ice bath
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