By Antoine Bourrillon
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B. C. D. E. None 25 mg 50 mg 75 mg 100 mg 2. Drugs that are administered IV are A. B. C. D. E. Rapidly absorbed Subject to first-pass metabolism 100% bioavailable Rapidly excreted by the kidneys Rapidly metabolized by the liver 3. Drugs that are highly bound to albumin: A. B. C. D. E. Effectively cross the BBB Are easily filtered at the glomerulus Have a large Vd Often contain quaternary nitrogens Can undergo competition with other drugs for albumin binding sites 4. Most drugs gain entry to cells by: A.
An important anatomic difference between the SANS and PANS is that the ganglia of the former lie in two paraventral chains adjacent to the vertebral column, whereas most of the ganglia of the PANS system are located in the organs innervated. Figure II-1-1 highlights the major features of the ANS and the somatic systems and also shows the location of the major receptor types. These are: l N Nicotinic receptors are located on cell bodies in ganglia of N both PANS and SANS and in the adrenal medulla.
Com Autonomic Pharmacology Acetylcholinesterase Inhibitors Clinical Correlate Alzheimer Disease Late-onset dementia with progressive memory loss and cognitive decline. Neuropathology includes neurofibrillary tangles, amyloid plaques, and loss of ACh neurons in Meynert’s nucleus— rationale for clinical use of AChE inhibitors. Table II-2-5. Properties of Indirect-Acting Cholinomimetics Drug Characteristics Clinical Uses Edrophonium Short-acting Dx—myasthenia Physostigmine Tertiary amine (enters CNS) Rx—glaucoma; antidote in atropine overdose Neostigmine, pyridostigmine Quaternary amines (no CNS entry) Rx—ileus, urinary retention, myasthenia, reversal of nondepolarizing NM blockers Donepezil, rivastigmine Lipid-soluble (CNS entry) Rx—Alzheimer disease Organophosphates Lipid-soluble, irreversible inhibitors Note: used as insecticides (malathion, parathion) and as nerve gas (sarin) Toxicity of AChE Inhibitors As insecticides l l l Long-acting irreversible inhibitors (both carbamates and organophosphates) Wide use in agriculture as insecticides Examples: malathion and parathion Inactive Classic Clue AChE inhibitor poisoning: “Dumbbeelss” Parathion Malathion Diarrhea Humans: Insects: Urination P450 Active Paraoxon Malaoxon Slow Fast P450 Fast Slow Figure II-2-2.