CNS Stimulants Flashcards
CNS stimulus - main characteristics:
1) increase
- alertness/awareness
- productivity and motivation
- arousal, locomotion, HR, BP
- euphoria
- nervousness and anxiety
2) decrease requirement for sleep and food
3) overdose = convulsions and death
Name the analeptic and respiratory stimulant drug?
Doxapram
Doxapram
- what type of drug?
- does what to body?
- MOA?
- analeptic & Resp stimulant drug
- *-respiratory stimulant used to counteract postanasthetic respiratory depression
- binds to carotid chemoreceptors and medullary respiratory centers to increase tidal volume and respiratory rate
methylxanthine- list drugs?
caffeine
theophylline
Taking patient off a ventillator give what drug to help with breathing?
doxapram
general effects of methylxanthines?
- -mild CNS and respiratory stimulants
* *-bronchodilators - for asthma
caffeine
- what type of drug?
- *-primary treatment for?
- some effects?
- methylxanthine - CNS stimulant
- **-tx for apnea of premature infants or breathing cessation in premature infants
- fighs off drowsiness/restores alertness
Theophylline
- what type of drug?
- *-Use?
- methylxanthine - CNS stimulant
* *-used for COPD, asthma, and apnea of prematurity
Name the sympathomimetic amide drugs? (psychomotor stimulants)
1) amphetamine & derivatives
a) methamphetamine
b) dexamphetamine
c) methylphenidate
2) cocaine
3) modafinil
4) atomoxetine (NE reuptake inh)
What is MOA for atomoxetine?
NE reuptake inh
Name the stimulant drugs used to treat ADHD?
- methylphenidate
- amphetamine salts
- dextroamphetamine
Name the non-stimulant drugs used to treat ADHD?
- atomoxetine
- clonidine
- modafinil
- Antidepressants (TCAs, MAOIs, bupropion)
metabolism of CNS stimulants
- what enzyme?
- where?
- anything interesting about metabolites?
- uses MAO_A and MAO_B
- liver degredation
- many precursor drugs metabolized into active drugs
What drugs should you not give with CNS stimulants?
(antidepressants) MAOIs and SSRI = results in increased levels monoamines
How are most CNS stimulants excreted?
urine
How long does effect of CNS stimulants last? What is dosing like?
duration time is short
requires multiple doses or extended release formulas
Analeptic stimulant drugs - MOA?
- depression of inhibitory neurotransmission (DISINHIBITION)
- GABA_A and glycine antagonists (dec Cl influx = hyperpolarization)
Methylxanthine drugs - MOA?
- inh of CNS suppressnat
- reduce adenosine activity (CNS suppressany-neuroprotective) by A1 receptor antagonism
Amphetamine drugs -MOA?
- COMPETITIVELY INH DAT AND INC SYNAPTIC DA
- INTERFERE WITH VESICULAR MONOAMINE TRANSPORTER (VMAT) = VESICLES ARE DEPLETED AND SYNAPTIC DA INCREASES
- enhancement of excitatory transmission
- stimulate pre synaptic release from storage vesicles (DA,NE)=inc synaptic catecholamine levels
cocaine - MOA?
INH DOPAMINE TRANSPORTER (DAT) AND INC SYNAPTIC DA
- enhancement of excitatory transmission
- inh of monoamine uptake via blockade of DA, NE and 5-HT transporters (DAT,NET,SERT)=affect reward circuitry similar to amphetamines
Atomoxetine drugs -MOA?
- enhancement of excitatory transmission
- selective NE transport blockade
**Whcih drug used for narcolepsy and sleep disorders?
**modafinil
Which drug used for ADHD?
methylphenidate
**Drug used to treat obesity?
**orlistat
Why are CNS stimulants used in obesity?
anorexia side effect- suppressed appetites (anorexiants)
Orlistat MOA?
lipase inh = dec GI fat absorption
results in GI effects- steatorrhea, fecal incontinence, flatulence
3 legal uses of amphetamine:
- narcolepsy
- ADHD
- short-term weight loss
What “schedule” controlled substance is amphetamine?
schedule II
What “schedule” controlled substance is cocaine?
schedule II
What area of the brain does the cocaine effect?
Ventral tegmental area (VTA) –> reward circuitry of the brain (HOME OF DA NEURONS)
***PSychomotor stimulants: CNS side effects
euphoria dysphoria insomnia iritability tremor headache loss of appetitie
**Psychomotor stimulants: Cardiovascular side effects:
- MI
- cerebrovascular accident (CVA) =stroke
**Psychomotor stimulants: Endocrine/metabolic side effects?
anorexia
severe weight loss
***Which drug has an uncommon side effect of inc suicide risk esp in children?
atomoxetine
Uncommon side effect for modanafil?
skin rash
stevens-johnson syndrome
Which drugs impairs liver function?
atomoxetine
Long term safety of psychomotor stimulants?
- some effect of growth in males
- sometimes get more tics in susceptible patients (tourettes or other)
- cardiovascular-sometimes inc BP and HR
two diagnostic/symptoms for ADHD?
Present for at least 6 months
1) inattention
2) impulsivity/hyperactivity
3 types of ADHD diagnoses:
1) ADHD predominantly hyperactive
2) ADHD predominantly inattentive
3) ADHD combined type
**shift in symptoms for kids to adults:
kids:
- motoric hyperactivity
- aggressiveness
- low frustration tolerance
- impulsiveness
adults: -shifts activities -easily bored -impatient restlessness
Pathophys of ADHD - which brain lobe is affected?
-frontal lobe dysfunction (executive function area)
What is the dopamine deficit hypothesis of ADHD?
Mutliple possibilities! environ/genetic/neurochem/CNS insults…
- dorsal lateral prefrontal cortex (PFC) lacks DA
- the PFC projects to anterior cingulate cortex = integration of inattentiveness and regulation of emotions
**ADHD CNS Stimulant drugs? **Which is main?
- methylphenidate (MAIN)
- amphetamine salts
- dextroamphetamine
Second line drugs to treat ADHD?
- atomoxetine - no abuse potential
- clonidine
- modafinil
- antidepressants (TCAs, MAOI, bupropion)
**Drug approved for narcolepsy?
modafinil - not to be used in children
also can use methylphenidate (ADHD drug)
Atomoxetine
- used for?
- mechanism?
- second line ADHD
- selective NE re-uptake block
Clonidine
- used for?
- MOA?
- second line ADHD
- alpha2 agonist = inc blood flow to prefrontal cortex
Modafinil
- used for?
- mechanism?
- second line ADHD (not in children - bc of skin rash/Stevens johnson syndrome)
- sleep disorders (narcolepsy)
-activates histamine neurons in tuberomammillary nucleus (TMN) of hypothalamus
side effects of ADHD treatment?
decreased appetite
WL
insomnia
