Module 7 Pharm

Front 1

Which stimulant is the prototype CNS stimulant?

Back 1

Amphetamine

Front 2

Amphetamines produce...?

Back 2

mood elevation
increased wakefulness
increased alertness
increased concentration
increased physical performance

Front 3

Amphetamines are a ___________ controlled drug.

Back 3

Schedule II

High potential for abuse w/ severe liability for psychological and physical dependence.

Front 4

The anorexic effect of amphetamines and related sympathomimetic amines is due to...?

Back 4

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

Front 5

Amphetamine MOA?

Back 5

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

Front 6

Amphetamine adverse effects?

Back 6

peripheral actions mediated through the release of catecholamines cause cardiovascular side effects:

1. increased systolic and diastolic bp

2. tachycardia

Front 7

Amphetamine acute toxicity?

Back 7

**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

Front 8

Amphetamine chronic toxicity?

Back 8

1. marked tolerance and psychological and physiological dependence

2. psychosis --> hallucinations, delusions of persecution, feelings of omnipotence

Front 9

Phentermine?

Back 9

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

Front 10

Monoamine reuptake inhibitor?

Back 10

Sibutramine

Front 11

Sibutramine MOA?

Back 11

Blocks neuronal uptake of NE, 5-HT, and Dopa

Front 12

Sibutramine metabolism?

Back 12

metabolized to active metabolites via CYP3A4

Front 13

Sibutramine side effects?

Back 13

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

Front 14

What "Schedule" category is Sibutramine?

Back 14

Schedule IV (but not an amphetamine)

Front 15

Dosing, use?

Back 15

Once daily dosing; no tolerance to anorexiant effect

Approved by FDA for long-term use in obesity.

Front 16

Clinical presentation of ADHD in preschoolers?

Back 16

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"

Front 17

Clinical presentation of ADHD in school-age children?

Back 17

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

Front 18

Clinical presentation of ADHD in adolescents?

Back 18

Similar to school-age children, but w/ less hyperactivity and greater likelihood of impulse control problems
-- substance abuse
-- alcoholism
-- recklessness

School adjustment problems

Front 19

Clinical presentation of ADHD in adults?

Back 19

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

Front 20

AHDH treatment of choice?

Back 20

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

Front 21

Methylphenidate duration of action?

Back 21

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

Front 22

Slow release methylphenidate?

Back 22

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

Front 23

Methylphenidate MOA?

Back 23

1. release NE and DA from neurons

2. block the reuptake of these catecholamines into their neurons

Front 24

What other drug can be used in place of methylphenidate?

Back 24

Atomoxetine (Strattera)

Front 25

Atomoxetine MOA?

Back 25

selective NE reuptake inhibitor


**Should NOT be administered w/ MAO inhibitor

Front 26

Atomexitine adverse effects?

Back 26

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

Front 27

Characteristics of narcolepsy?

Back 27

Recurrent, uncontrollable, sudden episodes of sleep under conditions normally not conducive to sleep.

Often accompanied by
-- hallucinations
-- cataplexy
-- sleep paralysis

Front 28

Narcolepsy treatment?

Back 28

Modafinil

New amphetamine substitute approved for use in narcolepsy

Claimed to have fewer disadvantages (mood changes, insomnia, abuse potential) than amphetamine

Front 29

Modafinil adverse effects?

Back 29

headache
nausea
nervousness
anxiety
insomnia

rarely reported: increased bp, tachycardia

Front 30

Describe apnea of prematurity.

Back 30

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

Front 31

Preferred apnea treatment in neonates?

Back 31

Theophylline

Front 32

Theophylline MOA?

Back 32

1. inhibition of phosphodiesterases, thereby increasing intracellular cyclic AMP

2. direct effects on intracellular Ca++ concentration

3. antagonism of adenosine receptors

Front 33

Therapeutic action of theophylline in management of Apnea of Prematurity?

Back 33

1. stimulate contraction of skeletal and diaphragmatic muscle

2. stimulate the central respiratory drive centers

3. increase ventilatory center's sensitivity to CO2

Front 34

Theophylline can specifically...?

Back 34

1. eliminate episodes of greater than 20 seconds

2. reduce the number of episodes of shorter duration

Front 35

Theophylline toxicity?

Back 35

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