CNS Stimulants Flashcards
What are stimulants?
Drugs that stimulate the CNS and PNS
Most NS stimulants are chemically similar to what? What does this do?
NE
simulate the flight or fright response
What do CNS stimulants decrease
Requirement for sleep and food intake
What are the symptoms of ODing on CNS stimulants?
Convulsions and death
What are the downsides of CNS stimulants on the CNS?
Increased nervousness and anxiety
What is the effect of CNS stimulants on the cardio system?
Increased BP and HR
What is the MOA of doxapram? What type of drug is it? What is it used for?
Analeptics/respiratory stimulant used to counteract respiratory depression by increasing tidal volume and RR.
What are analeptics?
Respiratory stimulants
Is doxapram fast or slow acting? Short or long duration?
Fast
short
What is the MOA of pentylenetetrazol? Use?
GABA (a) antagonist
circulatory and respiratory stimulant
What is the MOA of strychnine? Use?
Glycine antagonist
pesticide–Causes muscular convulsions and death through asphyxia
What is the MOA of bicuculline? Use?
GABA-(A) antagonist
What is the MOA picrotoxin? Use?
GABA-(A) blocker
What are methylxanthines?
Xanthines derivatives used as mild CNS and respiratory stimulants and bronchodilators
What type of drug is caffeine? What is its medical use?
Methylxanthine
Treatment for apnea of prematurity
What is theophylline? Use?
Methylxanthine (adenosine receptors antagonist) that is used to relax bronchial smooth muscle in COPD treatment
What are sympathomimetic amides?
Amphetamines and analogues
What are the 5 sympathomimetic amides?
Methamphetamine Dexamphetamine Methylphenidate cocaine Modafinil
What is the MOA of atomoxetine? What type of drug is it?
NE reuptake inhibitor
Sympathomimetic amide
What is the usual route of CNS stimulants?
Oral
How are CNS stimulants degraded?
MAO(a) and MAO (b)
Liver degradation via MEOS p450 system
How are CNS stimulant metabolites excreted?
urine
What is the duration of action for most of the CNS stimulants? What is the consequence of this?
Short–multiple dosing needed
True or false: CNS stimulants are often given as a prodrug form
True
What is the MOA of analeptic stimulants?
GABA (A) and glycine antagonists
What is the MOA of methylxanthines?
Reduce adenosine activity (adenosine is a CNS depressant)
What is the MOA of amphetamines?
Increase synaptic catecholamine levels by increasing release of DA and NE from presynaptic vesicles
What is the MOA of cocaine?
Inhibition of monoamine reuptake (DA and NE)
What is the MOA of atomoxetine?
Selective NE transporter blockade
What are the clinical uses of methylphenidate?
ADHD
What is the clinical use of doxapram?
treat drug induced post anesthesia respiratory depression
What is the clinical use of caffeine?
Analgesia (used with excedrin (ASA and acetaminophen))
What are the four drugs that are used to treat narcolepsy?
Modafinil
Amphetamine
Dextroamphetamine
Ephedrine
What is the major concern with the clinical use of amphetamines?
Abuse potential
Why were amphetamines used in obesity treatments? What is the major issue with this?
Anorexiants
Tolerance/abuse
What is Orlistat?
Weight loss lipase inhibitor
What schedule is amphetamine?
2
What type of drug is adderall?
Amphetamine
What are the three approved uses of amphetamine?
Narcolepsy
ADHD
Short-term weight loss
What area of the brain does cocaine primarily work on?
Reward circuitry in the Ventral tegmental area
What are the medical uses of cocaine?
Topical anesthesia in eye and nasal surgery
What schedule is cocaine?
II
What is the MOA of cocaine?
Inhibits the dopamine transporter (DAT) and increase synaptic DA
What is the MOA of amphetamine? (2)
Competitively inhibits DAT and interferes with VMATs, causing depletion and release
What is the mesolimbic pathway responsible for? Where is it? What are the neurons that are housed here?
Brain reward circuitry
Ventral tegmental area
Dopamine neurons here
What are the CNS side effects of psychomotor stimulants?
Euphoria
Dysphoria
What are the Cardio side effects of CNS stimulants?
MI
CVA
What are the endocrine/metabolic effects of CNS stimulants?
Anorexia
Weight loss
What are the side effects of modafinil?
Steven-Johnson syndrome
What are the long term effects of CNS stimulants on growth? Tics?
minimal for both
What are the concerning side effects of CNS stimulants on CV in kiddos?
Increased BP and HR
What is the most common developmental neurobehavioral disorder?
ADHD
What is the prevalence of ADHD?
3-5% of children
What is the male:female ratio of ADHD?
4:1
What are the three different ADHD subtypes?
- Hyperactive-impulsive
- Inattentive type
- Combined
What are the symptoms of adult ADHD?
shifts activities
Easily bored
Impatient
Restless
What is the primary part of the brain that is affected in ADHD? What are the three sub-parts of this?
Frontal lobe
- dorsal prefrontal cortex
- Dorsal ACC
- Caudate and putamen
What is the dopamine deficit hypothesis of ADHD?
Dorsolateral prefrontal cortex (PFC) lacks DA, since this projects to the ACC
What are the three CNS stimulants used for ADHD?
- Methylphenidate
- Amphetamine salts
- Dextroamphetamine
What are the four non-stimulants to treat ADHD?
- Atomoxetine
- Clonidine
- Modafinil
- Antidepressants
What is the MOA of clonidine? What is the basis of using this to treat ADHD?
alpha2 agonist–increases blood flow to the prefrontal cortex
What is the MOA of modafinil? What is the basis of using this in treatment of narcolepsy?
Activates histamine neurons in tuberomammillary nucleus of the hypothalamus, increases awakeness
What type of drug is doxapram?
Analeptic
What type of drug is caffeine?
Methylxanthine
What type of drug is theophylline
Methylxanthine
What type of drug is methamphetamine?
sympathomimetic amine
What type of drug is amphetamine?
sympathomimetic amine
What type of drug is methylphenidate?
sympathomimetic amine
What type of drug is cocaine?
sympathomimetic amine
What type of drug is modafinil?
sympathomimetic amine
What type of drug is atomoxetine?
sympathomimetic amine