Neurological drugs

The partition coefficient and concepts derived from it are particularly important in explaining the mode of action of neurological drugs, such as anticonvulsants (chapter 8, section 8.1.5) and general anesthetics, which must penetrate the blood-brain barrier prior to exerting their biological effect. 

Nobile-Orazio E, Carpo M, Scarlato G. Gangliosides. Their role in chnical neurology. Drugs 1994 47(4) 576-85. 

Agents acting on the central nervous system psychotropic and neurological drugs... 

N Central nervous system Psychotropic drugs, neurological drugs (ex anti-Parkinson drugs) analgesics... 

Substituted y-butyrolactones are attractive synthetic targets because of their importance as neurological drugs as well as synthetic intermediates. Selective reduction of irisubstituted butenolides may represent a convenient entry into substituted y-butyrolactones. Since treatment of a butenolide with an excess of HCOOH/n-BusN in the presence of... 

The barbiturates are contraindicated in patients with known hypersensitivity to the drugs. The barbiturates are used cautiously in patients with liver or kidney disease and those with neurological disorders. The barbiturates (eg, phenobarbital) are used with caution in patients with pulmonary disease and in hyperactive children. When barbiturates are used with other CNS depressants (eg, alcohol, narcotic analgesics, and antidepressants), an additive CNS depressant effect may occur. See Chapter 26 for additional information on the barbiturates. 

Before starting Hie drug Hierapy, Hie nurse performs a physical assessment of the patient to provide a baseline for future evaluaHons of drug Hierapy. It also is important to include an evaluaHon of Hie patient s neurologic status. Display 29-1 describes Hie assessments Hie nurse would make when evaluating Hie neurological status. 

Clinical signs and symptoms of toxicity are related to the overstimulation of muscarinic, nicotinic, and central nervous system receptors in the nervous system. Muscarinic receptors are those activated by the alkaloid drug muscarine. These receptors are under the control of the parasympathetic nervous system, and their hyperactivity results in respiratory and gastrointestinal dysfunction, incontinence, salivation, bradycardia, miosis, and sweating. Nicotinic receptors are those activated by nicotine. Hyperactivity of these receptors results in muscle fasciculations even greater stimulation results in blockade and muscle paralysis (Lefkowitz et al. 1996 Tafliri and Roberts 1987). Hyperactivity of central nervous system receptors results in the frank neurological signs of confusion, ataxia, dizziness, incoordination, and slurred speech, which are manifestations of acute intoxication. Muscarine and nicotine are not... 

Important products derived from amino acids include heme, purines, pyrimidines, hormones, neurotransmitters, and biologically active peptides. In addition, many proteins contain amino acids that have been modified for a specific function such as binding calcium or as intermediates that serve to stabilize proteins—generally structural proteins—by subsequent covalent cross-hnk-ing. The amino acid residues in those proteins serve as precursors for these modified residues. Small peptides or peptide-like molecules not synthesized on ribosomes fulfill specific functions in cells. Histamine plays a central role in many allergic reactions. Neurotransmitters derived from amino acids include y-aminobutyrate, 5-hydroxytryptamine (serotonin), dopamine, norepinephrine, and epinephrine. Many drugs used to treat neurologic and psychiatric conditions affect the metabolism of these neurotransmitters. 

Cui L, Locatelli L et al (1997) Effect of nucleoside analogs on neurite regeneration and mitochondrial DNA synthesis in PC-12 cells. J Pharmacol Exp Ther 280(3) 1228-1234 Dal Pan GJ, Glass JD et al (1994) Clinicopathologic correlations of HIV-l-associated vacuolar myelopathy an autopsy-based case-control study. Neurology 44(11) 2159-2164 Dalakas MC (2001) Peripheral neuropathy and antiretroviral drugs. J Peripher Nerv Syst 6(l) 14-20 Dalakas MC, Semino-Mora C et al (2001) Mitochondrial alterations with mitochondrial DNA depletion in the nerves of AIDS patients with peripheral neuropathy induced by 2 3 -dideoxycytidine (ddC). Lab Invest 81(11) 1537-1544... 

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