Histamine Effects of activating H1 - answerH1 receptors, it activates a G-protein-linked
second-messenger system that activates phosphatidylinositol, and the transcription
factor cFOS, and results in normal wakefulness
H2 - answerHistamine _____ receptors, best known for their actions in gastric acid
secretion and the target of a number of anti-ulcer drugs, postsynaptic receptors also
activate a G-protein second-messenger system with cyclic adenosine monophosphate
(cAMP), phosphokinase A (PKA), and the gene product CREB.
H3 - answerHistamine _____ receptors are presynaptic and function as autoreceptors.
H3 receptors are not bound by histamine, the molecular gate is open and allows
histamine release. When histamine binds to the H3receptor, the molecular gate closes
and prevents histamine from being released.
Blocking H1 - answerinterferes with the wake-promoting actions of histamine, and thus
can cause sedation, drowsiness, or sleep
Produces sedation and drowsiness—this is why first-generation antihistamines are used
as sleep aids.
Blocking H2 - answerDecreased arousal, promote modest sedative effect, H2 blockade
may modestly reduce arousal.
Blocking H3 - answerResults in disinhibition of histamine release, which can
paradoxically enhance wakefulness
tuberomamillary nucleus (TMN) of the hypothalamus. - answerLocation in brain where
histamine is produced solely
Orexin - answer_______, produced in the lateral hypothalamus, plays a key role in
stabilizing wakefulness by activating multiple arousal systems.
Deficiency in ______ is linked to narcolepsy
orexin (hypocretin) - answerNorepinephrine and serotonin from build up and release
onto neurons in the lateral hypothalamus, causing negative feedback inhibiting the
release of _______
Without ______ - VLPO and GABA take charge and suppress all the arousal
neurotransmitters ______ levels rapidly decline during first hour of sleep, plateau, then
steadily rise before awakening
, Homeostatic Drive to Sleep - answerThe _________ _____ __ _____ refers to the
body's accumulating need for sleep as wakefulness is prolonged. It acts as a "sleep
pressure" mechanism that gradually increases the propensity to fall asleep over time.
Adenosine, GABA, Meltonin - answerHomeostatic drive to sleep chemicals involved
(3)
Adenosine - answeran endogenous neuromodulator—builds up in the brain. Elevated
levels inhibit wake-promoting neurons and help to promote sleep by facilitating inhibitory
processes. This accumulation is central to creating the "sleep pressure" that eventually
leads to sleep onset.
GABA - answerReleased from the ventrolateral preoptic nucleus (VLPO) during sleep;
Adenosine's effects contribute to increased ____, the primary inhibitory neurotransmitter
in the brain, is essential in suppressing arousal systems.
Melatonin - answerhomeostatic sleep drive increases via adenosine accumulation, the
circadian system; secreted from the pineal gland
Doxepin (Sinequan) - answerWhen first‐line agents such as diphenhydramine
(Benadryl) and melatonin fail to achieve sufficient improvement - caution in older adults
due to anticholinergic effects
Addicting, rebound insomnia, next day drowsiness - answerSleep Aid GABA enhancers
caution due to
Suvorexant - answerOrexin receptor antagonists
Ramelteon (Rozerem) - answerMelatonin receptor agonist
Shift workers, jet lag, older patients - answerMelatonin receptor agonist good for
circadian rhythm disorders and who (Three)?
Next day drowsiness, high costs - answerSuvorexant side effects
Armadofinil, modafinil - answerNarcolepsy drugs 1st line
Histamine - answerNeurotransmitter that keeps you awake and effects can be blocked
by diphenhydramine
Orexin - answerNeurotransmitter also known as hypocretin, acts as on/off switch for
wakefulness, deficiency causes narcolepsy
Dopamine, Acetylcholine, Norepinephinrine, Serotonin - answer4 other key
neurotransmitters that aid in wakefulness