Barbiturates: Chapter 5 Flashcards
troduction of Thiopental (1934):
- Rapid-acting barbiturate.
- Enabled quick general anesthesia induction.
- Replaced slower, riskier diethyl ether induction.
Thiopental’s Import/Export Issues:
- Previously imported from overseas.
- Export to U.S. stopped due to use in lethal injections.
Current Relevance of Barbiturates:
- Possibility of resuming shipments.
- Still used by some anesthesiologists outside U.S.
- Serves as prototype for IV anesthetic comparison.
Barbiturates Significance in Drug Development:
Essential for understanding newer IV anesthetics.
Propofol, etomidate, midazolam compared to barbiturates.
Origin of Barbiturates:
Derived from barbituric acid.
Substitutions on Barbiturates:
Affect properties and pharmacokinetics.
Influence potency and effects.
Oxybarbiturates
Examples: Pentobarbital, secobarbital.
Contain oxygen at the second position.
Thiobarbiturates:
Examples: Thiopental, thiamylal.
Sulfur replaces oxygen.
Greater lipid solubility and hypnotic potency.
Phenyl Group Addition:
Example: Phenobarbital.
Increases anticonvulsant, not hypnotic potency
Methyl Group on Nitrogen:
Example: Methohexital.
Heightens hypnotic potency.
Lowers seizure threshold.
Causes myoclonus during induction