Central nervous system depressent activity

Indolizine derivatives have been studied for their psychotropic anti-inflammatory, analgesic, antimicrobial, antiexudative and hypoglycemic activity. Mannich bases of indolizines (see Section 3.08.3.1.3) have been found to possess central nervous system depressant activity <78AHC(23)103, 77HC(30)117, 77HC(30)179>. 

Dimethoxanate [477-93-0] (47) and pipazethate [2167-85-3] (48) are related phenothiazine derivatives that have shown antitussive activity. Unlike many phenothiazines, these do not produce central nervous system depression or analgesia at therapeutic doses. They are both somewhat less potent than codeine. It has been suggested that the unique side chain that is similar to, but shorter than, the one on benzonatate, may be at least pardy responsible for the antitussive effects. Both dimethoxanate and pipazethate are the result of molecular modifications of classical phenothiazines, such as promethazine [60-87-7], which possess antitussive activity in addition to central nervous system depressant activity. Dimethoxanate can be prepared by the reaction of phenothiazine- 10-carboxylic acid chloride with p-dimethylaminoethoxyethanol (66). 

Introduction During 1966, several new types of chemical structures were reported to have central nervous system depressant activity, and further studies were described of compounds previously classified in this area. The problem of defining further the type of activity to predict whether a given depressant will be of clinical application as an antipsychotic, anti-anxiety agent, sedative, hypnotic, anti-convulsant or anesthetic continues to occupy the attention of many investigators. 

In order to evaluate the analgesic and central nervous system depressant activity and to find out acute toxicity, four Teucrium species... 

Akbar, S., M. Nisa, and M. Tariq. 1985. Central nervous system depressant activity of Cuscuta chinensis. Int.. Crude Drug Res. 23(2) 91-94. 

Tani J, Yamada Y, Oine T, Ochiai T, Ishida R, Inoue I (1979) Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3/f)-quinazolinone derivatives. J Med Chem 22 95-99... 

Cu deficit, excess of Mo and SO Pre-Caucasian plain, Caspian low plain, West Siberian Steppe ecosystems Meadow-Steppe, Eustric Chernozems, Solonchaks, Arenosols The reducing Cu content in the central nervous systems, depressed function of oxidation ferments and activation of catalase, demielinization of the central nervous systems, disturbance of motion, convulsions. Endemic ataxia. Lamb disease is predominant... 

Several semisynthetic derivatives of yohimbine alkaloids show interesting pharmacological activity. For example, 17-methylthiomethoxyyohimbane stereoisomers (612 and 613) are valuable central nervous system depressants (349) and several hydrazides of yohimbinecarboxylic acid (614 and 615-type compounds) are useful cardiac stimulants, respiratory analeptics, and antihypertensives (350-353). 

Certain tricyclic compounds are found to be powerful stimulants, or antidepressants, to the central nervous system. Depressed individuals may respond with an elevation of mood, increased physical activity, mental alertness, and an improved appetite. Imipramine and amitriptyline hydrochlorides are good examples. 

JAP77148076). Some other oxathiazoline derivatives (279) have central nervous system (CNS) activity, as tranquilizers and ataraxics with low toxicity (68SAP6804299) and some dioxazoline derivatives (280) have a modest CNS depressant activity (77JPS772). 

Nearly all central nervous system depressants have some capacity to suppress seizures by virtue of their depressant activity on the brain and spinal cord. Clonazepam and diazepam are two benzodiazepines that depress epileptiform activity and are used in the treatment of epilepsy and seizure disorders (see Chapter 32). 

Mechanism of Action Abarbiturate that binds at the GABA receptor complex, enhancing GABA activity. Therapeutic Effect Depresses central nervous system (CNS) activity and reticular activating system. 

Tetrachloroethane causes central nervous system depression and is highly hepatotoxic in mice and dogs it produced embryotoxic effects and a low incidence of malformations in mice. A single oral dose (437 mg/kg bw) of 1,1,2,2-tetrachloroethane decreased the activity of some hepatic cytochrome P450-dependent monooxygenases and, to a smaller extent, that of UDP-glucuronosyl transferase (lARC, 1979). 

Note The most commonly used emetics are ipecac and apomorphine. Induced emesis is the preferred means of emptying the stomach in awake patients who have ingested a toxic substance or have recently taken a drug overdose. Emesis should not be induced if there is central nervous system depression or ingestion of certain volatile hydrocarbons and caustic substances. Ipecac syrup is prepared from the dried rhizome and roots of Cephaelis ipecacuanha or of C. accuminata, plants from Brazil and Central America, in which the alkaloid emetine is its active principal ingredient. 

Tranquilizers are agents that suppress or inhibit some aspects of central nervous system (CNS) activity—the brain, spinal cord, and the nerves from both— and are thus referred to as CNS depressants. Used primarily to treat insomnia as well as a wide variety of anxiety disorders, tranquilizers are among the most com-... 

Most of the sedative-hypnotics are capable of inhibiting the development and spread of epileptiform activity in the central nervous system. Some selectivity exists in that some members of the group can exert anticonvulsant effects without marked central nervous system depression (although psychomotor function may be impaired). Several benzodiazepines—including clonazepam, nitrazepam, lorazepam, and diazepam—are sufficiently selective to be clinically useful in the management of seizure states (see Chapter 24 Antiseizure Drugs). Of the barbiturates, phenobarbital and metharbital (converted to phenobarbital in the body) are effective in the treatment of generalized tonic-clonic seizures. 

FLUOXETINE, FLUVOXAMINE, PAROXETINE BZDs - ALPRAZOLAM, DIAZEPAM, MIDAZOLAM t in plasma concentrations of these BZDs. Likely t sedation and interference with psychomotor activity Alprazolam, diazepam and midazolam are subject to metabolism by CYP3A4. Fluvoxamine, fluoxetine and possibly paroxetine are inhibitors of CYP3A4 sertraline is a weak inhibitor. SSRIs are relatively weak compared with ketoconazole, which is possibly 100 times more potent as an inhibitor Warn patients about risks associated with activities that require alertness. Consider use of alternatives such as oxazepam, lorazepam and temazepam, which are metabolized by glucuronidation >- For signs and symptoms of CNS depression, see Clinical Features of Some Adverse Drug Interactions, Central nervous system depression... 

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