3. Psychomotor Stimulants Flashcards
(35 cards)
Attention Deficit Hyperactivity Disorder (ADHD)
Other names: ____ Syndrome
Attention Deficit Disorder (ADD)
Minimal Brain Dysfunction with Hyperactivity
Signs / Symptoms
- increased ____ activity
- impaired ____
- ____ attention span
- easy ____
- ____ behavior
- learning ____
____ does not always occur in ADHD.
hyperkinetic
motor coordination short distractibility impulsive disability
hyperactivity
ADHD
Etiology
Unknown. May be related to deficiency in brain ____.
ADHD estimated to affect 5% of children & 2.5% of US adults.
Association between ADHD and earlier-onset substance abuse; ____ not proven.
catecholamines
causation
ADHD
Drug Therapy
Appears to be successful in approximately ____% of cases.
By increasing the ability to concentrate and perform a task, selected drugs seem to ____ the patient during work projects.
2011: >52 million Rxs ADHD meds / ____% inc from 2010.
75
calm
10
ADHD
CNS Stimulants
Caffeine: ____
Amphetamines = ____ > pemoline
Other:
Antidepressants:
– ____:
imipramine & desipramine have some efficacy but are toxic
– ____ Inhibitors:
efficacy = amphetamine & methylphenidate but are too toxic
Barbiturates: ____ (+ paradoxical ____)
Clonidine: useful in ____ cases
ineffective
methylphenidate
tricyclic
MAO
ineffective
excitation
limited
ADHD
1. Caffeine Does not appear to be \_\_\_\_ in ADHD. At doses > \_\_\_\_ mg / day, 'caffeinism' may occur with symptoms such as: \_\_\_\_ Headache \_\_\_\_ Increased muscle tension
Caution in pts with diabetes: may cause unacceptable ____.
effective
500
anxiety
insomnia
hyperglycemia
ADHD
- Amphetamines
Amphetamine; methamphetamine (DESOXYN).
Powerful ____ stimulants.
____ mg, p.o., will produce a significant increase in CNS activity in the non-tolerant person.
Tmax of dextroamphetamine approximately ____ hrs.
Mechanisms of action: a. Major: \_\_\_\_ stimulation of CNS via: 1) promote release of \_\_\_\_ from pre-synaptic storage sites 2) inhibit re-uptake of released \_\_\_\_ at pre-synaptic membrane
b. Minor
1) ____ stimulation of post-synaptic adrenergic receptors
2) inhibition of ____
CNS 5-10 3.5 indirect catecholamines re-uptake
direct
MAO
Amphetamines
Uses \_\_\_\_: short-term (only 4-8 weeks) \_\_\_\_ Ø excessive sleepiness Ø sleep 'attacks' Ø sleep paralysis \_\_\_\_
weight loss
narcolepsy
ADHD
Amphetamines
ADRS
Acute \_\_\_\_ Elevated blood pressure \_\_\_\_ Anorexia
____
Gilles de la Tourettes Syndrome (involuntary tics): motor: ____, body, limbs
verbal: ____, phrases (may be obscene)
appears to be related to excessive central ____ activity
Chronic
Same as acute plus:
____ weight gain: inhibits growth of children Psychological dependence
Development of significant ____ & physical dependence (addicts may use from 1-2 grams per day!)
Toxic ____
tachycardia insomnia tachyphylaxis head words DA
decreased
tolerance
psychosis
Amphetamines
ADDERALL
____ formulation. Combines neutral sulfate salts of ____ and amphetamine, with the dextro isomer of ____ and d,l-amphetamine aspartate monohydrate.
immediate release
dextroamphetamine
amphetamine saccharate
Amphetamines
ADDERALL XR
____ daily extended-release, single-entity amphetamine product [same as Adderall regular tablets].
Adderall XR capsule contains ____ types of drug-containing beads designed to give a ____-pulsed delivery of amphetamines, which prolongs release of amphetamine from Adderall XR compared to the conventional ADDERALL ® immediate-release) tablet formulation.
once
two
double
Amphetamines
ADDERALL XR
• There are adults with ADHD. Does that mean chronic therapy? ____.
• Amphetamines are not ripping apart tissues. The more that a drug acts like a ____ product,
the less ripping apart. Alcohol degenerates cardiac muscle and skeletal muscle and brain tissue.
- Amphetamines, on the other hand does not have too much ____ damage - Someone could be on these for a ____.
yes
natural
pathologic
lifetime
Lisdexamfetamine dimesylate (Vyvanse®) CII
Prodrug of ____.
Does not bind to ____ reuptake sites.
Converted to dextroamphetamine and l-lysine primarily in ____
due to the hydrolytic activity of ____. Significant hydrolysis
even at low ____ levels (33% of normal).
T1⁄2 < ____ hr
ADHD
Moderate to Severe Binge Eating Disorder (BED)
Safety and effectiveness for Tx of ____ have not been
established.
NOT indicated for ____.
Use of other sympathomimetic drugs for weight loss has been
associated with serious ____ adverse events.
Prior to treatment, assess for presence of ____ disease
Severe renal impairment: Maximum dose is ____ mg/day
End stage renal disease (ESRD):
Maximum dose is ____ mg/day
dextroamphetamine NE and DA blood RBCs hematocrit
1
obesity
weight loss
cardiac
50
30
ADHD Initial dose: \_\_\_\_ mg every morning Titration schedule: \_\_\_\_ mg weekly Recommended dose: \_\_\_\_ mg per day Maximum dose: \_\_\_\_ mg per day
30
10 or 20
30 to 70
70
BED
Initial dose: ____ mg every morning
Titration schedule: ____ mg weekly
Recommended dose: ____ mg per day
Maximum dose: ____ mg per day
30
20
50 to 70
70
Warnings/Precautions
Serious Cardiovascular Reactions: ____ in children and adolescents with serious heart problems, as well as sudden death, stroke, and myocardial infarction in adults reported. Avoid use in patients with known structural cardiac ____,
cardiomyopathy, serious heart ____, or coronary artery
disease.
BP and Heart Rate Increases: Monitor ____ and pulse.
Consider benefits and risks before use in patients for whom ____ increases may be problematic
sudden death
abnormalities
arrhythmia
blood pressure
blood pressure
Psychiatric: May cause ____ or manic symptoms in patients with no prior history, or exacerbation of symptoms in pts with pre-existing psychosis. Evaluate for ____ prior to
stimulant use
Suppression of Growth: Monitor height and weight in pediatric pts during Tx.
Peripheral Vasculopathy, including Raynaud’s phenomenon:
Stimulants assoc with ____, including Raynaud’s phenomenon. Careful observation for ____ changes
necessary during Tx with stimulants
psychotic
bipolar disorder
peripheral vasculopathy
digital
Lisdexamfetamine dimesylate (Vyvanse)
ADRs:
Incidence ≥5% and at rate at least 2x placebo
\_\_\_\_
\_\_\_\_
dec weight
--\_\_\_\_
--dizziness
--dry \_\_\_\_
--irritability
--\_\_\_\_
--N/ V
upper abdominal pain
anorexia anxiety diarrhea mouth insomnia
Lisdexamfetamine dimesylate (Vyvanse)
Acidifying agents: ____ amphetamine blood levels
Alkalinizing agents: ____ amphetamine blood levels.
- You can look at the ____ as one of the ways of helping. Because amphetamines are a weak base, the docs will decide to acidify the urine to cause the amphetamine to be more ionized and more ____ soluble, then will get eliminated.
- Something you would never do in the ER is to alkalinize the urine because again this is a weak base, so it would ____ amphetamine blood levels. As amphetamine comes into the renal system, it is not ionized in an alkaline environment, and it is reabsorbed.
dec
inc
urine
water
inc
Adzenys XR-ODT (Amphetamine Extended-Release Orally disintegrating Tablet) for Tx of ADHD in Pts 6 years and older
First and Only FDA Approved \_\_\_\_ Orally Disintegrating Tablet (ODT) for Tx of ADHD
Bioequivalent to a previously approved mixed ____ extended-release capsule (Adderall XR®1), one of the most commonly prescribed medications for the treatment of ADHD.
Adzenys XR-ODT contains amphetamine loaded onto a mixture of ____ release and ____-coated, delayed-release resin particles; designed to disintegrate in ____.
____-protected; not generic of amphet. mixed salts XR capsules.
Available in six dosage strengths, equivalent to the Adderall XR® dosage strengths, thus allowing healthcare providers to
____ the dose.
extended-release amphetamine salts immediate polymer mouth patent individualize
Adzenys XR-ODTTM (Amphetamine Extended-Release Orally Disintegrating Tablet) for Tx of ADHD in Pts 6 Years and Older
Potential for Overdose Due to Medication Errors:
Med errors, including ____ and dispensing errors with
other amphetamine products could occur, leading to possible ____.
Do not substitute for other amphetamine products on a ____ basis, because of different amphetamine base
____ and differing ____ profiles
substitution
OD
milligram-per-milligram
compositions
pharmacokinetics
Adzenys XR-ODTTM (Amphetamine Extended-Release Orally Disintegrating Tablet) for Tx of ADHD in Pts 6 Years and Older
WARNING: ABUSE AND DEPENDENCE
CNS stimulants, including Adzenys XR-ODT, other amphetamine-
containing products, and methylphenidate, have a high potential
for ____. Assess the risk of abuse prior to
prescribing and monitor for signs of abuse and dependence while
on therapy.
abuse and dependence
Adzenys XR-ODTTM (Amphetamine Extended-Release Orally Disintegrating Tablet) for Tx of ADHD in Pts 6 Years and Older
Contraindications: Pts should not take Adzenys XR-ODT if they are:
• ____ to amphetamine or other ingredients of Adzenys XR-ODT. ____ and anaphylactic reactions have been reported in patients treated with other amphetamine products.
• Taking ____, or have taken an MAOI within the past 14 days. ____ crisis can occur.
hypersensitive
angioedema
monoamine oxidase inhibitors
hypertensive
Adzenys XR-ODTTM (Amphetamine Extended-Release Orally Disintegrating Tablet) for Tx of ADHD in Pts 6 Years and Older
READ ME
Warnings and precautions
- Serious ____ Reactions: Sudden death has been reported in association with CNS stimulant treatment at recommended doses in pediatric patients with structural cardiac abnormalities or other serious heart problems. In adults, sudden death, stroke, and myocardial infraction have been reported. Avoid use in patients with known structural cardiac abnormalities, cardiomyopathy, serious heart arrhythmia, coronary artery disease, and other serious heart problems. Further evaluate patients who develop exertional chest pain, unexplained syncope, or arrhythmias during Adzenys XR-ODT treatment.
- ____ and Heart Rate Increases: CNS stimulants can cause an increase in blood pressure (mean increase about 2-4 mm Hg) and heart rate (mean increase about 3-6 bpm). Monitor all patients for potential tachycardia and hypertension.
- ____ Adverse Reactions: Prior to treatment assess for the presence of bipolar disorder. CNS stimulants may cause psychotic or manic symptoms in patients with no prior history, or exacerbate symptoms of behavior disturbance and thought disorder in patients with pre-existing psychosis.
- Long-Term Suppression of ____: CNS stimulants have been associated with weight loss and slowing of growth rate in pediatric patients. Closely monitor weight and height in pediatric patients treated with Adzenys XR-ODT. Treatment may need to be interrupted in children not growing as expected.
- ____, including Raynaud’s Phenomenon: CNS Stimulants, including ADZENYS XR-ODT, are associated with peripheral vasculopathy, including Raynaud’s phenomenon. Signs and symptoms are usually intermittent and mild; very rare sequelae include digital ulceration and/or soft tissue breakdown. Careful observation for digital changes is necessary during treatment with ADHD stimulants. Further clinical evaluation may be required, including referral.
- ____: Use only if the potential benefit justifies the potential risk to the fetus. Based on animal data, Adzenys XR-ODT may cause fetal harm. Breastfeeding is not recommended during treatment with Adzenys XR-ODT.
cardiovascular blood pressure psychiatric growth peripheral vasculopathy pregnancy and lactation
- Methylphenidate (RITALIN; RITALIN SR)
Similar to amphetamines but less ____ stimulation & less ____ activation.
Major drug of ____
Uses
ADHD: regarded by many physicians as ____
____ mg/kg (low dose) = improved behavior & learning
• not for children < ____ years old
• > ____ mg not recommended for children 6 years & older
ADRs
More likely to occur at ____ mg/kg
Similar actions as amphetamines but less intense Less inhibitory effect on growth
Motor ____
Additional Uses
Depression
Ø in ____ pts as alternate to antidepressants
Ø in ____ pts
Antagonism of ____-induced sedation in cancer pts
CNS
CV
abuse
D.O.C
0.3
6
60
1.0
tics
geriatric
stroke
opioid
