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psychomotor stimulants and drugs of abuse
CBN III
44
Medical
Graduate
02/12/2011

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Term
when are psychomotor stimulants used?
Definition
in management of ADHD and to reduce opioid-induced sedation in CA pts
Term
what are other names for ADHD?
Definition
hyperkinetic syndrome, ADD, and minimal brain dysfunction w/hyperactivity
Term
does hyperactivity always occur w/ADHD?
Definition
no
Term
what is the etiology for ADHD?
Definition
unknown - may be related to deficiency in brain catecholamines
Term
what characterizes drug therapy for ADHD?
Definition
~75% successful - by *increasing the ability to concentrate and perform a task, the drug can calm the pt during work projects (increases energy internally to allow parts of brain involved in tasking to be active ).
Term
what are the CNS stimulants which may be used to tx ADHD?
Definition
caffeine, amphetamines, methylphenidate.
Term
what are the "other" agents which may be used to tx ADHD?
Definition
antidepressants: TCAs (imipramine & desipramine have some efficacy but are toxic, atomoxetine may be used), MAOI (good efficacy, but toxic), barbiturates (ineffective +paradoxical excitation), clonidine (useful in limited cases), and modafinil.
Term
what characterizes caffeine as a CNS stimulant?
Definition
caffeine does not appear to be effective in ADHD. at doses > 500 mg/day, caffeinism may occur: anxiety, h/a, insomnia, and increased muscle tension. can also cause unacceptable hyperglycemia in DM pts.
Term
what characterizes amphetamines as CNS stimulants? MOA?
Definition
amphetamine, methamphetamine are powerful CNS stimulants. major MOA: indirect simulation of the CNS via promotion of catecholamine release from pre-synaptic storage sites and inhibition of their re-uptake at the pre-synaptic membrane. minor MOA: direct stimulation of post-synaptic adrenergic receptors and inhibition of MAO. (activate sympathetic system in every way possible)
Term
what are amphetamines used for?
Definition
wt loss (4-8 wks), narcolepsy (excessive sleepiness, sleep attacks, sleep paralysis), and ADHD
Term
what ADRs are associated w/amphetamines?
Definition
acute: tachycardia, elevated BP, insomnia, anorexia, tachyphylaxis, and tourettes (motor/verbal tics). chronic: decreased wt gain (inhibited growth in children), psychological dependence, development of significant tolerance and physical dependence, and toxic psychosis.
Term
what is adderall?
Definition
an immediate release amphetamine
Term
what is adderall xr?
Definition
a 1x/daily extended release single-entity amphetamine - double pulses delivery system. pts on this had significant improvement in symptoms, control, and quality of life with continuous long-term treatment.
Term
what characterizes methylphenidate as a CNS stimulant?
Definition
similar to amphetamine, but less CNS stimulation and less CV activation. major drug of abuse. regarded as ADHD DOC. ADRs: similar to amphetamines, but less intense, less inhibitory effect on growth, and less motor tics.
Term
what are additional uses for methylphenidate?
Definition
depression (geriatric pts/stroke pts) and antagonism of opioid-induced sedation in CA pts.
Term
what is concerta? dexmethylphenidate?
Definition
concerta: extended methylphenidate release formulation. dexmethylphenidate: d-isomer, more potent in treating ADHD (focalin, focalin xr)
Term
what characterizes clonidine as a tx for ADHD?
Definition
this alpha-2 adrenergic agonist at the pre-synaptic membrane causes a decreased release of catecholamines - the opposite effect which appears necessary for pharm ADD management. it can be used alone or w/methylphenidate when prominence of aggressive symptoms, fam hx of tic disorders, and presence of severe conduct disorder. ADRs: sedation, bradycardia, and hypotension.
Term
what characterizes antidepressant therapy for ADHD?
Definition
the TCAs imipramine & desipramine have some efficacy but are toxic. thus they are used in pts unresponsive to stimulant therapy. ADRs: anticholinergic and cardiac arrhythmias. *atomoxetine, a SNRI focuses on blocking NE uptake.
Term
what is modafinil?
Definition
mechanism unknown. may *facilitate glutamate activity and *reduce release of GABA. weak interaction with dopamine transporter, a system that seems necessary for its wake-promoting action; *blocks DA reuptake. it is approved for narcolepsy, but has been prescribed off-label for sleepiness and fatigue from other illnesses, including depression, sleep apnea, parkinson's disease, chronic-fatigue syndrome, and multiple sclerosis. it has been used to improve problems w/shift work in hospitals. limited abuse potential.
Term
what characterizes cocaine?
Definition
cocaine is a stimulant, similar to amphetamine/methamphetamine. it is not a narcotic, but it is one of the most addicting drugs available. it is a free base (non-ionized, highly lipid soluble) which allows extremely rapid absorption from the lungs when smoked and rapid entrance into the brain (crack). smoking crack onset: 1-2 min, snorting cocaine onset: 20-30 min, and IV injection onset 1-2 min. duration of action: 30-60 min. it is rapidly biotransformed by plasma cholinesterase.
Term
how is cocaine tested for?
Definition
present degree of impairment: blood/saliva. determination of previous use: urine (inactive metabolites for 5-10 days) and hair (good for checking to see if it will affect pregnancy).
Term
what is cocaine's MOA?
Definition
blocks reuptake of DA and NE at the presynaptic membrane.
Term
what are the acute pharmacological effects of cocaine?
Definition
euphoria (DA), tachycardia, HTN and hyperthermia (due to vasoconstriction from increased NE action), migraine-like h/a, nervousness, insomnia, anorexia, mydriasis, and constipation.
Term
what characterizes acute toxicity to cocaine?
Definition
CV: MI (constriction of coronaries) and cardiac arrhythmias (sinus tachy, PVCs, ventricular tachy, v-fib, rupture of ascending aorta, CVA). respiratory: rhinorrhea. CNS: assaultive behavior and seizures (death possible).
Term
what characterizes chronic toxicity to cocaine?
Definition
CNS: anxiety, paranoia, delirium, hallucinations, psychosis, and brain atrophy. respiratory: reduced sense of smell, rhinitis, ulceration/perforation of nasal septum, pulmonary edema, and pulmonary hemorrhage. GI: intestinal ischemia. reproductive: ED and delay in orgasm. renal: nephrotoxicity and renal failure. injection related: hepatitis, tetanus, and AIDS risk. other: TB.
Term
does tolerance develop to cocaine?
Definition
yes and there is clinical evidence of physical dependence.
Term
what characterizes withdrawal syndrome w/cocaine?
Definition
general fatigue, depression, prolonged sleep, hyperphagia (increased appetite), intense craving for cocaine (lasts ~7 days), exacerbation of pre-existing psychological disturbances (depression and possible suicide attempts).
Term
what characterizes polyaddiction?
Definition
CNS depressants are often taken concomitantly - so often cocaine abusers will present w/BZD physical dependence as well.
Term
what is tx for acute cocaine intoxication?
Definition
if not severe, may end within 24 hours; treat symptoms. dopamine agonists such as bromocriptine have been used to curb the craving.
Term
what is tx for chronic cocaine intoxication?
Definition
psychotherapy, lithium, antidepressants
Term
how does cocaine use affect pregnancy?
Definition
cocaine induced vasoconstriction probably reduces the blood flow and, consequently, oxygen delivery to the fetus. prenatally, this increases risk of spontaneous abortion/fetal death. postnatally: immediate - decreased head circumference, visual disturbances, increased muscular rigidity, abnormal sleep patterns (apnea, SIDS) and cerebral infarct. at 2 years - sensory/motor difficulties, difficulty in climbing stairs, afraid of quick movements, and difficulty initiating words.
Term
how does cocaine use affect breastfeeding?
Definition
this has been used topically to reduce breast soreness - but infants can ingest enough to get seizures.
Term
what is the etiology of substance abuse?
Definition
*1) experimentation: acute use influenced by peer pressure. *2) dependence - significant factors: low self-esteem, immaturity, inability to solve personal problems, easily frustrated, difficulty in relating to opposite sex, over-dependence on family/friends - insignificant factors: family income, personal income, area of residence, and level of intelligence.
Term
what is the role of family in prevention of substance abuse?
Definition
love, respect and discipline need to be provided.
Term
how should adult family members serve as good role models?
Definition
interaction with spouse, children and friends, proper respect for legitimate drug therapy, responsible social use of alcohol
Term
what is the role of school in preventing substance abuse?
Definition
strengthen values of self, family, friends, life in general. increase awareness of toxic effects of cigarettes, alcohol, and drugs. should provide limited counseling if necessary.
Term
what issue is always present w/impaired healthcare professionals?
Definition
low self-esteem
Term
what are additional issues for healthcare professionals?
Definition
increased number of pts to manage, reduced control of ordering tests/selecting therapeutic procedures/prescribing medications, lowered career satisfaction, decreased income, knowledge of clinical pharmacology, accessibility to drugs, and code of silence.
Term
what are the club drugs?
Definition
MDMA, rohypnol, GHB, and ketamine
Term
what characterizes MDMA (3-4 methylenedioxymethamphetamine)?
Definition
this is a synthetic, psychoactive drug chemically similar to the stimulant methamphetamine and the hallucinogen mescaline. at high doses, MDMA can interfere with the body’s ability to regulate temperature. this can lead to a sharp increase in body temperature (hyperthermia), resulting in liver, kidney, and cardiovascular system failure. b/c MDMA can interfere w/its own metabolism, potentially harmful levels can be reached by repeated drug use at short intervals. research in animals links MDMA exposure to long-term damage to serotonin neurons and can lead to changes in brain function, affecting cognitive tasks and memory with long term use as well as depression.
Term
what characterizes GHB, ketamine and rohypnol?
Definition
these are predominately CNS depressants - often colorless, tasteless, and odorless. thus they are referred to as "date rape" drugs.
Term
what is GHB?
Definition
GHB (gamma hydroxybutyrate) is a CNS depressant which has been abused for its euphoric, sedative, and anabolic (body building) effects. coma and seizures can occur following abuse of GHB. combining use with other drugs such as alcohol can result in nausea and breathing difficulties. GHB may also produce withdrawal effects, including insomnia, anxiety, tremors, and sweating. it has been used by body builders and in poisonings, overdoses, date rapes, and deaths.
Term
what is ketamine?
Definition
ketamine is an anesthetic which can cause dream-like states and hallucinations. in high doses, ketamine can cause delirium, amnesia, impaired motor function, high blood pressure, depression, and potentially fatal respiratory problems.
Term
what is rohypnol?
Definition
aka flunitrazepam, rohypnol is a BZD. when mixed with alcohol, rohypnol can incapacitate victims and prevent them from resisting sexual assault. it can produce “anterograde amnesia,” which means individuals may not remember events they experienced while under the effects of the drug. also, rohypnol may be lethal when mixed with alcohol and/or other depressants.
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