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
_________ addicts are likely to
have dilated pupils and twitching of muscles
Meperidine
In Europe, addicts who could not be detoxified
and kept free of drugs by any other means have been
given ________ the active ingredient in heroin,
diacetylmorphine,
A randomized trial conducted by Fudala
and colleagues has demonstrated the superiority over
methadone of a combination of ________ AND _______ combined with brief counseling in keeping opioid addicts in treatment and abstinent of abused drugs
buprenorphine and
naloxone
Neuro cx of Opiate use
________, probably
as a result of the toxic effects of quinine in the heroin
mixtures
Amblyopia
Neuro cx of Opiate use
Most instances of this _______ are the result of inhalation of heated heroin vapor in a practice known as “chasing
the dragon.
leukoencephalopathy
An acute generalized _____with myoglobinuria
and renal failure has been ascribed to the intravenous
injection of adulterated heroin
myonecrosis
_________ and ________ are the sequelae of
venous thrombosis resulting from the administration of
heroin and its adulterants by the intramuscular and
subcutaneous routes.
Brawny edema and fibrosing
myopathy (Volkmann contracture)
for barbiturates
T or F
The higher its lipid solubility, the
greater the drug’s central nervous system potency and
the quicker and briefer its action
T
The action of barbiturates is to suppress neuronal
transmission, presumably by__________
at pre- and postsynaptic receptor sites, and to ___________
enhancing GABA inhibition
reduce
excitatory postsynaptic potentials
T or F
Pentobarbital and secobarbital
produce their effects quickly and recovery is relatively
rapid
T
In the case of long-acting barbiturates, such as ____________, the hypnotic-sedative effect lasts 6 h or more after an average oral dose;
with the intermediate-acting drugs such
as ___________, 3 to 6 h;
and with the short-acting drugs,
_________ and______, less than 3 h
phenobarbital and barbital
amobarbital
secobarbital and pentobarbital
The potentially fatal dose of phenobarbital is____g.
The lowest plasma concentration
associated with lethal overdosage of phenobarbital
or barbital has been approximately ______ and
that of amobarbital and pentobarbital, 10 mg/mL.
6 to 10
60 mg/mL`
flaccid coma with small reactive
pupils, hypothermia, and hypotension.
What type of toxicity
barbiturate
Hemodialysis or hemofiltration with charcoal may be
used in comatose patients who have ingested long-acting
barbiturates and these treatments are particularly advisable if _____ or _____has developed
anuria or uremia
B a rbitu rate Abst i n e n ce , o r Withd rawa l ,
Sy n d ro me
Immediately following withdrawal, the patient seemingly
improves over a period of ________, as the symptoms
of intoxication diminish
8 to 12 h
With
chronic phenobarbital or barbital intoxication, withdrawal
symptoms may not become apparent until ___________h after the final dose
48 to
72
In Barbiturate withdrawal
there is a greatly heightened
sensitivity to photic stimulation, to which the patient
responds with _________ or a seizure accompanied by
paroxysmal changes in the EEG
myoclonus
This is the oldest and one of the safest, most effective, and
most inexpensive of the sedative-hypnotic drugs.
chloral hydrate
T or F
Tolerance and addiction to chloral hydrate develops usually
F
_rare
The________ have been prescribed frequently
for the treatment of anxiety and insomnia, and they are
especially effective when the anxiety symptoms are
severe.
benzodiazepines
____________ is particularly
useful in the treatment of delirious patients who require
parenteral medication.
Diazepam
____________has a central place in the treatment o f panic
attacks and other anxiety states, and as an adjunct in
some depressive illnesses
Alprazolam
______a specific pharmacologic antagonist
of the CNS effects of benzodiazepines, rapidly but
briefly reverses most of the symptoms and signs of
benzodiazepine overdose
Flumazenil,
In chronic benzodiazepine users, the gradual tapering
of dosage over a period of _______minimizes the
withdrawal effects.
1 to 2 weeks
MOA of anti-psychotic drugs
blocking the postsynaptic
mesolimbic dopamine receptors of which there
are four subtypes, termed D1 through D4 on neuronal
membranes
The _______receptors are located mainly
in the frontal cortex, hippocampus, and limbic cortex,
and the______ receptors are in the striatum
D2
D1
The newer “atypical” antipsychotic drugs, exemplified
by________ apparently achieve the same degree of D2
and D3 blockade in the temporal and limbic lobes while
exhibiting substantially less antagonistic activity in the
striatum-accounting also for their lesser parkinsonian
side effects.
clozapine,
8 CLASSES OF ANTI-PSYCH
1.
2.
3.
( 4) the rauwolfias alkaloids;
(5) an indole derivative, loxapine, and a unique dihydroindolone, molindone;
(6) a diphenylbutylpiperidine, pimozide;
(7) dibenzodiazepines, typified by ______
(8) a benzisoxazole derivative, _______
1) the phenothiazines;
(2) the thioxanthenes;
(3) the butyrophenones;
clozapine and olanzapine; and
risperidone
they are particularly favored in controlling the
confusion and psychosis of parkinsonian patients
clozapine
_____ may be useful in the treatment
of haloperidol-refractory cases of Gilles de la Tourette
syndrome
Pimozide
This group comprises chlorpromazine (Thorazine), promazine (Sparine), triflupromazine (Vesprin), prochlorperazine (Compazine), perphenazine (Trilafon), fluphenazine (Permitil, Prolixin), thioridazine (Mellaril), mesoridazine (Serentil), and trifluoperazine (Stelazine
Phenoth iazines
The phenothiazines have had their widest application
in the treatment of the major psychoses, namely
_____ and, to a lesser extent, ________
schizophrenia
bipolar psychosis
Side effects of Phenothiazines
cholestatic type of jaundice,
agranulocytosis, seizures, orthostatic
hypotension, skin sensitivity reactions, mental
depression, and, most importantly, immediate or delayed
extrapyramidal motor disorders
The ____________ is the most extreme complication of Phenothiazones
neuroleptic
malignant syndrome
5 EPS syndromes associated with Phenothiazines
- parkinsonian syndrome
- Acute dyskinetic and dystonic reactions
- Akathisia
- Tardive dyskinesias
- neuroleptic malignant syndrome
Suppression of dopamine
in the ____________
is presumably the basis of the parkinsonian signs
striatum (similar to the effect of loss of
doparninergic nigral cells that project to the striatum)