Depressants Flashcards
Depressant Plants
Humulus lupulus L. (Cannabaceae) – Hops
Piper methysticum G. Forst. (Piperaceae) – Kava
Valeriana officinalis L. (Caprifoliaceae) - valerian
Papaver somniferum L. (Papaveraceae) – opium poppy
Alcohol plants:
◦ Grains, grapes, apples, cassava and etc.
Valeriana officinalis L
Caprifoliaceae family Activity: sedative, sleep promoting, spasmolytic, muscle relaxant Chemistry: monoterpenes (isovaltrate- up to 46%, didrovaltrate, valeric acid, and other volatile oils), sesquiterpenes (valerenic acid, hydroxyvalerinic acid), and alkaloids
Opium Poppy
•Papaver somniferum (Papaveraceae) •Long history of use and abuse in international politics • China • Afghanistan •Source of heroine, morphine, and codeine •Extremely addictive •Affects enkaphalin neurotransmitter •2500 BC Sumerians medicinal use •"opion" = poppy juice Greek •paregoric – tincture used for diarrhea •in Europe called "Laudanum" – Paracelsus •Opium trade w/China
Opium and Morphine
•1803 – morphine isolated, w/hyperdermic needle as powerful painkiller and
anaesthetic
•US Civil War- increase morphine addiction in US
•1874 discovery of heroine – morphine w/2 acetyl groups extra
• initially sold by Bayer- much more effective, less-addictive alternative to morphine
•1924 – illegalized in the US, decreased morphine use, but increased heroine use
• by 1996, 2.4 M used heroin, 216,000 using it monthly
•1972 agreement w/Turkey illegalized cultivation
• production moved to Afghanistan, Golden Triangle
Humulus lupulus
TM uses: ◦Insomnia ◦Neuralgia ◦ Excitability Bitter part of oleo-resin ◦ Humulone ◦ Lupulone
Kava or Sakau - Piper methysticum
Cold water infusion of roots of a shrub
Pacific islanders use often to foster sociability and community
identity
◦ Restricted to men in past
◦ Formal social protocols used
◦ Now – widespread access and popularization via “kava bars”
Health impact:
◦ Kavalactones = Anxiolytic and muscle relaxant properties; also used in West to
treat insomnia
Sakau (kvaa)use in Pohnpei
Roots are pounded with stones until a fine macerate is made Water is mixed in, then the material is transferred to the inner bark of Hibiscus tilaceus The roots are transferred to the hibiscus, and then twisted to press the liquid through the bark gaps
Questions of toxicity with Kava?
Reports of toxicity in solvent-extracted kava products in
Europe in 1990s
◦ Product standardized to 70% kavalactones – but what else is in this
extraction?
◦ Water extractions of this plant are drunk at 8 times the “normal”
dose of 300mg in Polynesia with no ill effects
◦ Lesson for translation from the field to the market
Effect and MOA for kava
Produces dose-dependent effects on the CNS. The antiepileptic and neuroprotective
properties of kavalactones have been demonstrated in animal models.
Kavalactones produced centrally mediated skeletal muscle relaxation in vivo and smooth
muscle relaxation in vitro.
Unlike other CNS depressants, kava does not depress cognitive function or
electroencephalographic event-related potentials. However, the ability of kavalactones to
significantly increase barbiturate sleep time has been demonstrated in animals.
Kavalactones also have significant local anesthetic properties. Kawain is equipotent to cocaine
in producing topical anesthesia.
MOA not fully elucidated, but multiple effector sites may be involved
May potentiate γ-aminobutyric acid (GABA) inhibitory neurotransmission