Barbiturates
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Barbiturates

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Barbiturates Barbiturates Presentation Transcript

  • MARIA FE SALVADOR NAVARRETE MD BIOLOGICALTHERAPIES
  • Barbiturates and Similarly Acting Drugs  used as sedative-hypnotic agents in 20th century  high abuse and addiction potential,  a narrow therapeutic range with low therapeutic index,  and unfavorable side effects.  The use of barbiturates and similar compounds such as meprobamate (Miltown) has been practically eliminated by the benzodiazepines,  buspirone (BuSpar), and hypnotics such as zolpidem (Ambien) and zaleplon (Sonata), which have a lower abuse potential and a higher therapeutic index than the barbiturates.  the barbiturates and similarly acting drugs still have a role in the treatment of certain mental disorders.
  • Pharmacologic Actions  well absorbed after oral administration.  The binding of barbiturates to plasma proteins is high, but lipid solubility varies.  metabolized by the liver and excreted by the kidneys.  The half-lives of specific barbiturates range from 1 to 120 hours (Table 36.8-1).  Barbiturates may also induce hepatic enzymes (cytochrome P450), thereby reducing the levels of both the barbiturate and any other concurrently administered drugs metabolized by the liver.  The mechanism of action of barbiturates involves the γ- aminobutyric acid (GABA) receptor–benzodiazepine receptor–chloride ion channel complex.
  • Therapeutic Indications: Electroconvulsive Therapy  Methohexital (Brevital) is commonly used as an anesthetic agent for electroconvulsive therapy (ECT).  It has lower cardiac risks  Used intravenously, methohexital produces rapid unconsciousness and, because of rapid redistribution, it has a brief duration of action (5 to 7 minutes)  Typical dosing for ECT is 0.7 to 1.2 mg/kg. Methohexital can also be used to abort prolonged seizures in ECT or to limit postictal agitation.
  • Seizures  Phenobarbital (Solfoton, Luminal), the most commonly used barbiturate for treatment of seizures, has indications for the treatment of generalized tonic-clonic and simple partial seizures.  Parenteral barbiturates are used in the emergency management of seizures independent of cause. Intravenous (IV) phenobarbital should be administered slowly, 10 to 20 mg/kg for status epilepticus.
  • Narcoanalysis  Amobarbital (Amytal) has been used historically as a diagnostic aid in a number of clinical conditions,  including conversion reactions,  catatonia,  hysterical stupor,  and unexplained muteness,  and to differentiate stupor of depression,  schizophrenia, and structural brain lesions.
  • SLEEP  The barbiturates reduce sleep latency and the number of awakenings during sleep, although tolerance to these effects generally develops within 2 weeks.  Discontinuation of barbiturates often leads to rebound increases on electroencephalogram (EEG) measures of sleep and a worsening of the insomnia.