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35 Cards in this Set

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Which stimulant is the prototype CNS stimulant?
Amphetamine
Amphetamines produce...?
mood elevation
increased wakefulness
increased alertness
increased concentration
increased physical performance
Amphetamines are a ___________ controlled drug.
Schedule II

High potential for abuse w/ severe liability for psychological and physical dependence.
The anorexic effect of amphetamines and related sympathomimetic amines is due to...?
1. specific depressant effect on appetite (site of action is lateral hypothalamus)

2. psychological stimulation

3. increased energry expenditure due to physical activity and/or peripheral adrenergic receptor stimulation
Amphetamine MOA?
1. indirect acting sympathomimetics

2. acts to release catecholamines (norepi and dopa) from their intraneural stores

3. acts to block monoamine reuptake, thus prolonging action of monoamines at the synapse
Amphetamine adverse effects?
peripheral actions mediated through the release of catecholamines cause cardiovascular side effects:

1. increased systolic and diastolic bp

2. tachycardia
Amphetamine acute toxicity?
**With i.v. use in particular

1. marked CNS stimulation

2. paranoid psychosis

3. hypertensive crisis, tachycardia, arrhythmias

4. hyperthermia

5. convulsions, coma

6. formication --> believe insects under skin; will try to cut them out
Amphetamine chronic toxicity?
1. marked tolerance and psychological and physiological dependence

2. psychosis --> hallucinations, delusions of persecution, feelings of omnipotence
Phentermine?
Amphetamine derivative

1. lower abuse potential than amphetamine

2. classified as Schedule IV controlled substances

3. same MOA as amphetamine

4. approved by FDA for short-term use in trtmt of obesity
Monoamine reuptake inhibitor?
Sibutramine
Sibutramine MOA?
Blocks neuronal uptake of NE, 5-HT, and Dopa
Sibutramine metabolism?
metabolized to active metabolites via CYP3A4
Sibutramine side effects?
No CNS depression, abuse potential, drug dependence or valvular pathology

1. tachycardia
2. PVCs
3. HTN
4. headache
5. dry mouth
6. insomnia
7. constipation
8. short duration of sleep
What "Schedule" category is Sibutramine?
Schedule IV (but not an amphetamine)
Dosing, use?
Once daily dosing; no tolerance to anorexiant effect

Approved by FDA for long-term use in obesity.
Clinical presentation of ADHD in preschoolers?
1. excessive motor activity

2. difficulty paying attention

3. not listening

4. not responding to normal praise and punishment

5. aggression

6. "can't play alone"

7. "is into everything"
Clinical presentation of ADHD in school-age children?
1. short attention span
2. distractibility
3. restlessness
4. poor impulse control
5. poor peer relations
6. aggression
7. poor socialization
8. learniing disabilities
9. academic underachievement
10. low self-esteem
11. low frustration tolerance
Clinical presentation of ADHD in adolescents?
Similar to school-age children, but w/ less hyperactivity and greater likelihood of impulse control problems
-- substance abuse
-- alcoholism
-- recklessness

School adjustment problems
Clinical presentation of ADHD in adults?
1. short attention span
2. restlessness or fidgetiness
3. quick or excessive temper
4. poor impulse control
5. mood abnormalities
6. poor organization w/ inability to complete tasks
7. low stress tolerance
AHDH treatment of choice?
Methylphenidate (Ritalin)

Therapeutic action referred to as "paradoxical" because they act to increase persistence, attentiveness and concentration, and decrease excessive motor activity in ADHD children
Methylphenidate duration of action?
4-5 hours, so second dose usually required around noon in order to control behavior at school in afternoon

Give DRUG HOLIDAY on weekend and summer to allow linear growth
Slow release methylphenidate?
Duration of action is 12h so lasts entire school day

1. Outer coat contains small, readily bioavb dose which rapidly achieves therapeutic conc

2. remainder of dose released at constant rate from reservoir inside hard shell of tablet
Methylphenidate MOA?
1. release NE and DA from neurons

2. block the reuptake of these catecholamines into their neurons
What other drug can be used in place of methylphenidate?
Atomoxetine (Strattera)
Atomoxetine MOA?
selective NE reuptake inhibitor


**Should NOT be administered w/ MAO inhibitor
Atomexitine adverse effects?
CHILDREN:
-- headache
-- aggression
-- irritability

ADULTS:
-- palpitations
-- insomnia
-- urinary retention

Required to carry "black box" warning label for increased risk of suicidal throughts among children and adolescents
Characteristics of narcolepsy?
Recurrent, uncontrollable, sudden episodes of sleep under conditions normally not conducive to sleep.

Often accompanied by
-- hallucinations
-- cataplexy
-- sleep paralysis
Narcolepsy treatment?
Modafinil

New amphetamine substitute approved for use in narcolepsy

Claimed to have fewer disadvantages (mood changes, insomnia, abuse potential) than amphetamine
Modafinil adverse effects?
headache
nausea
nervousness
anxiety
insomnia

rarely reported: increased bp, tachycardia
Describe apnea of prematurity.
All premature neonates, as well as most full-term neonates, have apnea --> pauses in their breathing pattern

PATHOLOGICAL APNEA:
-- apnea exceeding 20sec duration OR
-- apnea less than 20sec if accomp by bradycardia or oxygen desaturation

Contributed to neuronal immaturity of the brain; tends to resolve
Preferred apnea treatment in neonates?
Theophylline
Theophylline MOA?
1. inhibition of phosphodiesterases, thereby increasing intracellular cyclic AMP

2. direct effects on intracellular Ca++ concentration

3. antagonism of adenosine receptors
Therapeutic action of theophylline in management of Apnea of Prematurity?
1. stimulate contraction of skeletal and diaphragmatic muscle

2. stimulate the central respiratory drive centers

3. increase ventilatory center's sensitivity to CO2
Theophylline can specifically...?
1. eliminate episodes of greater than 20 seconds

2. reduce the number of episodes of shorter duration
Theophylline toxicity?
1. B/C rapid i.v. infusion can result in severe toxicity or sudden death, drug should be injected slowly over 20-40min period

2. plasma conc should be monitored during therapy

Symptoms include:
headache
tachycardia
severe restlessness
nausea
emesis
abdominal pain

Focal and generalized seizures can occur w/o prior signs of toxicity