EXAM #3: CNS STIMULANTS Flashcards
What endogenous molecule are most CNS stimulants chemically similar to?
NE
What will CNS stimulants increase?
1) Alterness
2) Productivity/ motivation
3) Arousal
4) Euphoria
5) Nervousness and anxiety
What will CNS stimulants decrease?
Requirements for:
1) Sleep
2) Food intake
What can overdose on CNS stimulants lead to?
- Convulsions
- Death
What is an Analeptic?
Respiratory stimulants used to reverse drug-induced CNS depression (esp. post-op)
What is the hallmark analeptic?
Doxapram
What is the clinical utility of Doxapram?
This is a stimulant used to counteract anesthesia induced respiratory depression
What is the MOA of doxapram?
Binds to carotid artery chemoreceptors/ medullary respiratory centers
What is the common MOA of the non-doxapram analeptics?
GABA-A antagonists
What is a methylxanthine?
Xanthine derivative CNS/ respiratory stimulant
List the Methylxanthines.
Caffeine
Theophylline
What is the primary clinical indication for caffeine?
Apnea of prematurity
What is the clinical indication for Theophylline?
COPD/Asthma
*Drug has bronchodilator properties
List the Sympathomimetic Amide stimulants.
Amphetamine analogs:
- Methamphetamine
- Dexamphetamine
- Methylphenidate
Cocaine
Modafinil
Atomoxetine
How are the amide psychomotor stimulants metabolized?
1) Monamine oxidase
2) Liver p450
What classes of drugs will have adverse drug-drug interactions with the psychomotor stimulants?
MAOI
SSRI
What is the duration of action of many psychomotor stimulants? What are the clinical implications?
- Short duration
- Multiple dosing or extended release formulas
What is the clinical indication for Modafinil?
Narcolepsy/ sleep disorders
What drug is primarily used to treat ADHD?
Methylphenidate (Ritalin)
What drug was historically used for weight loss?
Amphetamine
How is the drug Orlistat used clinically?
Weight loss
What is the MOA of Orlistat?
Lipase inhibitor that decreases GI fat absorption
What are the three approved clinical uses for amphetamine?
1) Narcolepsy
2) ADHD
3) Short-term weight loss
What risk potential does cocaine have? Why?
Level 5 i.e. highest b/c it stimulates VTA reward pathway
What is the MOA of cocaine?
Inhibits DAT i.e. prevents DA reuptake
What is the MOA of amphetamine?
1) Taken up into pre-synaptic vesicle by DAT (prevent DA reuptake)
2) Binds/ inhibits VMAT to cause DA release
Aside from DAT, what other transporters do cocaine and amphetamine have effects on?
SERT
NET
What are the common CNS related side effects of the psychomotor stimulants?
Euphoria Dysphoria Insomnia Irritability Tremor Headache Anorexia
What are the cardiovascular related side effects of the psychomotor stimulants?
MI
CVA
What percentage of ADHD patients are the predominant hyperactive/impulse subtype?
10%
What percentage of ADHD patients are the predominant inattentive subtype?
30-40%
What percentage of ADHD patients are the combined subtype?
50-60%
What are the symptoms of ADHD that are common in children with the disorder?
1) Motor hyperactivity
2) Aggressive
3) Low frustration tolerance
4) Impulsive
Why are psychomotor stimulants given in ADHD?
Dopamine Deficit Hypothesis of ADHD–esp. in the PFC
What drugs are used to treat ADHD?
Methylphenidate
Amphetamine salts
- Addreall/ Adderall XR
Dextroamphetamine
What are the non-stimulant drugs that are given for ADHD?
1) Atomoxetine (NE-reuptake blockade)
2) Clonidine (alpha-2 agonist–>increase blood flow to PFC)
3) Modafinil (Activates histamine)
Antidepressants
- TCA
- MAOI
- Bupropion
Can Modafinil be used in children? Why or why not?
NO–Rash?
What are the major side effects of ADHD treatment?
- Decreased appetite/ weight loss
- Insomnia
