DISORDERS IN THE CNS CAUSED BY DRUGS Flashcards
The common drug and toxin transformations
involve ___________, which enhance their solubility and elimination
mainly by the kidney
hydroxylation, deamination, oxidation, and
dealkylation
The process of movement from plasma to brain is by
_______ or by_______
diffusion through capillaries
facilitated transport
The terms opioid and narcoticanalgesic
designate drugs with actions similar to those of
_______
morphine.
Opioids activate G-coupled transmembrane
receptors, meaning they influence neuronal activity
through the intermediate of cAMP; the receptor types are
denomina.te as______, _______, ______
mu, delta, and kappa
Clinical effects of opioids
knowledge that these receptors are concentrated in the
thalamus and dorsal root ganglia (mu receptors,_______),
amygdala (________) and brainstem raphe (_________), and Edinger-Westphal nuclei _______
pain
affect
alertness
(pupillary miosis
Receptors
in the brainstem, also of the ________type, are involved
in modulating respiratory responses to hypoxia and
hypercarbia (respiratory suppression).
mu
Pts susceptible to Morphine side effects
myxedema,
Addison disease, chronic liver disease, and pneumonia
___________, _________, ___________, ________, ___________ are the
we.ll-reognized clinical manifestations of acute opioid
pmsonmg.
Unresponsiveness, shallow respirations, slow respiratory rate (e.g., 2 to 8 per min) or periodic breathing, pinpoint pupils, bradycardia, and hypothermia
In pts with Opiate toxicity,
The immediate cause of death is usually ________
respiratory
depression with consequent asphyxia
This consists of the support of ventilation and administration of ______ or the longer-acting
______ both specific antidotes to the opiates and also
to the synthetic analgesics
naloxone (Narcan),
nalmefene,
The dose of naloxone in adults
is usually ______ and repeated in larger increments (the
second dose is typically 2 mg) every 2 min to a dose of
_______ intravenously.
The
improvements in ____ and _________ and reversal
of miosis are usually dramatic.
0.05 mg
15 mg
circulation and respiration
Naloxone has less direct effect on _________
however, and the patient may remain drowsy for man;
hours
consciousness
Although nalmefene has a plasma half-life
of _______ compared to ______for naloxone, it has no
clear advantage in emergency practice
11 h,
60 to 90 min
an antidote must be used with great caution in an addict
who has taken an overdose of opioid, because in this
circumstance, it may precipitate ______
withdrawal phenomena
Nausea and severe abdominal pain, presumably because
of _________ are
other troublesome symptoms of opiate use or withdrawal
pancreatitis (from spasm of the sphincter of Oddi),
The onset of opioid use is usually in adolescence,
with a peak at 17 to 18 years; fully two-thirds of
addicts start using the drugs before the age of_______
21
Opioid addiction consists of three recognizable phases: 1 2 3
(1) intoxication, or “euphoria,”
(2) pharmacogenic dependence or drug-seeking behavior (addiction), and
(3) the propensity to relapse after a period of abstinence
the administration of opioids
produces a sense of unusual well-being, a state that has
traditionally been referred to as ________
morphine euphoria.
The
latter refers to the symptoms and signs that become
manifest when the drug is withdrawn following a period
of continued use
physical dependence
opioids
activate an opioid antinociceptive system ________, ________, _________ which are opioid receptors and
are located at many different levels of the nervous system
(enkephalins,
dynorphins, endorphins),
The desensitization of opioid receptors, probably mainly the ________, accounts for tolerance through a mechanism of uncoupling of the receptor from the G-protein complex.
mu type
With morphine,
the majority of individuals receiving______ daily for
30 days or more will show moderately severe abstinence
symptoms following withdrawal
240 mg
___________ the equivalent of emotional or
psychologic dependence, refers to the substitution of drugseeking
activities for all other aims and objectives in life.
Habituation,
Abstinence symptoms from _______
are less intense than those from morphine and do not
become evident until 3 or 4 days after withdrawal; for
these reasons THIS can be used in the treatment
of morphine and heroin dependency
methadone