Page 603 - Basic _ Clinical Pharmacology ( PDFDrive )
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CHAPTER 32  Drugs of Abuse     589



                                                                                                 Pharmacokinetics, Toxicities,
                     Subclass, Drug  Mechanism of Action  Effects            Clinical Application  Interactions
                     BENZODIAZEPINES
                       •   Oxazepam,   Positive modulators of the   Enhances GABAergic   Delirium tremens  Half-life 4–15 h • pharmacokinetics not
                        others       GABA A  receptors, increase   synaptic transmission;        affected by decreased liver function
                                     frequency of channel   attenuates withdrawal
                                     opening             symptoms (tremor,
                                                         hallucinations, anxiety) in
                                                         alcoholics • prevents
                                                         withdrawal seizures
                       •  Lorazepam: Alternate to oxazepam with similar properties
                     N-METHYL-d-ASPARTATE (NMDA) ANTAGONIST
                       •  Acamprosate  Antagonist of NMDA   May interfere with forms of   Treatment of alcoholism •   Allergic reactions, arrhythmia, and low
                                     glutamate receptors  synaptic plasticity that   effective only in combination   or high blood pressure, headaches,
                                                         depend on NMDA receptors  with counseling  insomnia, and impotence •
                                                                                                 hallucinations, particularly in elderly
                                                                                                 patients
                     CANNABINOID RECEPTOR INVERSE AGONIST
                       •  Rimonabant  CB 1  receptor inverse agonist  Decreases neurotransmitter   Approved in Europe from   Major depression, including increased
                                                         release at GABAergic and   2006 to 2008 to treat   risk of suicide
                                                         glutamatergic synapses  obesity, then withdrawn
                                                                             because of major side effects
                                                                             • smoking cessation has
                                                                             never been approved, but
                                                                             remains an off-label
                                                                             indication



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                       C ASE  STUD Y  ANSWER

                       When found by his parents, the patient was having visual   exogenous cannabis with endocannabinoids that fine-tune
                       hallucinations of colorful insects. Hallucinations are often   synaptic transmission and plasticity. While probably not
                       caused by a cannabis overdose, especially when hashish is   fulfilling the criteria for addiction at present, the patient is at
                       ingested. The slower kinetics of oral cannabis are more dif-  risk as epidemiologic studies show that drug abuse typically
                       ficult to control compared to smoking marijuana. The poor   begins in late adolescence. The fact that he is not yet using
                       learning performance may be due to the interference of   other drugs is a positive sign.
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