Term
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Definition
| Agonist at all AChRs (duh.) Limited clinical use: used intraocularly to produce miosis, intracoronary use causes vasodilation, can be used to diagnose vasospastic angina. |
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Term
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Definition
| Can be used to diagnose asthma through a challenge test. Inhalation of this drug causes bronchoconstriction by acting at muscarinics. Must be used very carefully. |
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Term
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Definition
| Treatment for wide-angle glaucome when other cholinomimetics have failed. Causes pupillary contraction and relief and relief of intraocular pressure. |
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Term
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Definition
| Used postoperatively to reduce bladder/bowel distension (BBB). Can be used as an alternative to pilocarpine for treatment of xerostomia. |
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Term
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Definition
| Potent stimulator of sweat, tears and saliva. Used for wide-angle glaucoma and to treat xerostomia. Also used for emergency treatment of narrow-angle glaucoma with an AChE inhibitor (although this condition requires immediate surgical attention). Prolonged use can cause reduced night vision and difficulty in focusing on far objects. |
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Term
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Definition
| Quaternary amine with brief duration (1-5 mins). Used to test for myasthenia gravis where IV administration causes a brief improvement of strength. Also used to judge correct dosage: if brief improvement is seen with use that patient may benefit from a higher dose of carbamate. |
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Term
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Definition
| Crosses BBB into CNS, used for treatment of wide-angle glaucoma, often with pilocarpine. Used to treat atropine overdose ('PHYxes' atropine overdose). Can adversely facilitate formation of cataracts. |
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Term
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Definition
| Short lasting (0.5 - 2hr). Used to treat loss of tone in GI tract and bladder (urinary retention) either from disease or from postoperative recovery from anesthesia. Also used for myasthenia gravis. No CNS penetration ('NEO' CNS penetration). |
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Term
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Definition
| Used to treat myasthenia gravis, longer duration (3-6hr) than neostigmine. |
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Term
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Definition
| Similar to pyridostigmine but even longer acting (4-8hr). |
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Term
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Definition
| Used to treat glaucoma, only clinically useful organophosphate. |
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Term
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Definition
| Insecticides responsible for many cases of farm poisonings. Converted to malaoxon and paraoxon, respectively, which are more toxic compounds. Detoxified in mammals and birds via plasmaesterases. |
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Term
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Definition
| 'Nerve gases' that are potent inhibitors of AChE, among the most toxic agents known. |
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Term
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Definition
| Used in treatment of Alzheimer's. Long acting (once-a-day dosing), CNS penetrant, good oral absorption. |
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Term
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Definition
| Carbamate similar to physostigmine used to treat Alzheimer's. Requires twice-a-day dosing. |
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Term
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Definition
| Long-acting drug for Alzheimer's. Not only a AChE-I but also a potent allosteric enhancer of CNS nicotinic receptors. |
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Term
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Definition
| Anti-muscarinic. Uses: mydriasis for eye exam (outdated); induce cycloplegia (ciliary muscle paralysis) in children for determination of refractive error; sinus bradycardia and AV block; reduction of salivary and resp. secretions and to prevent airway obstruction in patients under anesthesia (outdated); reduce intestinal spasms and pain; reduce gastric acid secretion (outdated); reverse muscarine or AChE-I poisoning; prevent muscarinic side effects in patients receiving neostigmine or AChE-I; as an antidiarrheal |
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Term
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Definition
| Anti-muscarinic. Used for motion sickness, sedative. Applied as a patch. |
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Term
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Definition
| Fast but short-acting mydriatic agent. |
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Term
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Definition
| Fast but short-acting mydriatic agent. |
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Term
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Definition
| Fast but short-acting mydriatic agent. |
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Term
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Definition
| Quaternary amine anti-muscarinic. Taken by inhalation, causes bronchodilation, used in COPD. |
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Term
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Definition
| Quaternary amine anti-muscarinic. Taken by inhalation, causes bronchodilation, used in COPD. Similar to Ipratropium but longer-acting. |
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Term
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Definition
| Anti-muscarinic. Used to manage overactive bladder, relaxes detrusor to allow for more filling. Contraindicated for patients with narrow-angle glaucoma. |
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Term
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Definition
| Anti-muscarinic. Relaxes intestinal smooth muscle. Used for irritable bowel. |
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Term
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Definition
| Anti-muscarinic. Low doses used to inhibit secretions (e.g. to make intubation easier). Used to prevent excessive generalized sweating and to prevent muscarinic side effects in patients receiving neostigmine (used preferentially over atropine for this use). |
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Term
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Definition
| Anti-muscarinic. Used to relieve extrapyramidal symptoms in Parkinson's patients or patients taking antipsychotics. |
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Term
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Definition
| Non-depolarizing ganglionic blocker. Was used as an anti-hypertensive. |
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Term
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Definition
| Non-depolarizing ganglionic blocker. Was used for aortic dissection as it lowers BP and prevents the sympathetic reflex. |
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Term
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Definition
| Non-depolarizing ganglionic blocker. Was used for hypertension, can be used to improve GI absorption. Recent interest for use in Tourette Syndrome. |
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Term
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Definition
| Depolarizing competitive AChR agonist. Phase I: fasiculations; Phase II: desensitization. |
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Term
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Definition
Short-acting, rapid-onset.
Autonomic ganglia: No effect
Histamine release: Low
Cardiac mAChR: None
Metabolism: plasmaChE |
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Term
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Definition
Medium-acting, rapid-onset.
Autonomic ganglia: no effect
Histamine release: none
Cardiac mAChR: slight
Metabolism: Liver |
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Term
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Definition
Medium-acting, slow-onset.
Autonomic ganglia: no effect
Histamine release: none
Cardiac mAChR: none
Metabolism: Liver (and kidney) deacetylation |
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Term
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Definition
Medium-acting, slow-onset.
Autonomic ganglia: no effect
Histamine release: low
Cardiac mAChR: none
Metabolism: spontaneous hydrolysis |
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Term
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Definition
Medium-acting, slow-onset.
Autonomic ganglia: no effect
Histamine release: slight
Cardiac mAChR: none
Metabolism: Spontaneous hydrolysis |
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Term
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Definition
Long-acting, slow-onset.
Autonomic ganglia: blockade
Histamine release: high
Cardiac mAChR: none
Metabolism: Kidney excretion |
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Term
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Definition
Long-acting, slow-onset.
Autonomic ganglia: blockade
Histamine release: moderate
Cardiac mAChR: none
Metabolism: Kidney excretion |
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Term
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Definition
Long-acting, slow-onset.
Autonomic ganglia: no effect
Histamine release: none
Cardiac mAChR: moderate block (also called 'vagolytic effect': tachycardia)
Metabolism: Kidney deacetylation |
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Term
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Definition
Long-acting, slow-onset.
Autonomic ganglia: no effect
Histamine release: none
Cardiac mAChR: none
Metabolism: Kidney deacetylation |
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Term
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Definition
Long-acting, slow-onset.
Autonomic ganglia: no effect
Histamine release: none
Cardiac mAChR: no effect
Metabolism: Kidney excretion |
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