MS1, Block 2 Cholinergic Drugs
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Anticholinesterase agents (agents that indirectly increase cholinergic function)
Naturally occurring cholinergic stimulants
Choline ester that is partially refractory to AChase breakdown and is valuable as an experimental tool.
Choline ester that is very refractory AChase breakdown and has mostly nicotinic stimulating effects.
Choline ester with well established clinical utility. Refractory to AChase inactivation and has mostly muscarinic stimulating effects.
Useful in treating post-operative urinary retention and atony of the GI tract.
Naturally occurring cholinergic stimulant that activates all autonomic ganglia and stimulation of skeletal muscle.
Naturally occurring cholinergic stimulant that will stimulate all innervated and non-innervated muscarinic receptors.
Good antidote for rapid onset type (muscarine) poisoning.
Naturally occurring cholinergic stimulant that selectively activates muscarinic receptors. Highly charged and readily crosses membrane barriers.
Cholinergic stimulant used to treat glaucoma.
Reversible AChase inhibitors
(DENT are PPs)
AChase inhibitor that is not highly charged (teritary amine) and can readily enter the CNS.
AChase inhibitor used for treatment of atropine poisoning.
AChase inhibitor that is charged (quaternary amine) and does not readily enter the CNS.
AChase inhibitor used to reverse actions of competitive neuromuscular blocking (curare-like) drugs.
Long-acting AChase inhibitor used to treat myasthenia gravis.
AChase inhibitor with a short duration of action that is valuable for the diagnosis of myasthenia gravis.
CNS acting AChase inhibitors that are used to treat cognitive dysfunction in Alzheimer's patients.
Donepezil and Tacrine
Irreversible AChase inhibitor used to treat glaucoma, but restricted to aphakic eyes due to high incidence of cataract formation.
Irreversible AChase inhibitors that are commonly used as insecticides
Parathion and Malathion
Potent anti-cholinesterase war gases.
Sarin and Soman
AChase reactivator that is used to treat intoxication by organophosphates.
Prototypical muscarinic blocking drug that produces CNS excitation resulting in slight paradoxical bradycardia.
Characteristics of atropine poisoning.
Hot, dry skin. Dilated pupils.Maniacal behavior. (Red as a beet, hot as a pistol, dry as a bone, and mad as a hatter)
Muscarinic blocker that causes CNS depressant effects.
Muscarinic blocker used to treat motion sickness.
Less potent and short-acting muscarinic blocker used to cause mydriasis and cycloplegia for ophthalmological exams.
Synthetic muscarinic antagonists that do not enter the CNS and are used primarily in patients with COPD.
Ipratropium and Tiotropium
Second line drug for treatment of bronchial asthma. Appears to be beneficial when combined with other bronchodilators.
Longer duration of action than Ipratropium and can be used as a once/day drug.
CNS acting muscarinic blocker that is used to relieve symptoms of Parkinson's disease.
Muscarinic blocker used to treat spasms of the bladder after urologic surgery and in some neurological disorders producing bladder hyperactivity.
Prototypic ganglionic blocking drug. Does not compete with ACh at nicotinic receptors at the endplate region of skeletal muscle.
Predominant tone and effect of ganglionic blockade on arterioles
Predominant tone and effect of ganglionic blockade on veins
Predominant tone and effect of ganglionic blockade on the heart
Predominant tone and effect of ganglionic blockade on the iris
Predominant tone and effect of ganglionic blockade on ciliary muscle of the eye
Predominant tone and effect of ganglionic blockade on the GI tract
Reduced tone and motility
Predominant tone and effect of ganglionic blockade on the urinary bladder
Predominant tone and effect of ganglionic blockade on salivary glands
Predominant tone and effect of ganglionic blockade on the sweat glands
MS1, Block 2 Cholinergic Drugs
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