Lecture 15 CNS Stimulants

Psychomotor stimulants can be used for _____ deficitt disorder or attention deficit hyperactivity disorder.

It can also be used for _______, obesity, sleep apnea, and ____ hypotension.

All CNS stimulants produce a rate _____ effect.

attention; narcolepsy; orthostatic; dependent

Attention-deficit/hyperactivity disorder is characterized by inattentiveness, distractibility, and _____. There is ___ frustration tolerance, frequent ____ of activities, difficulty ____, poor efficiency, and daydreaming.

Dopamine nad ______ play a role in  the control of attention and impulsivity, and thus drugs that affect these. Patients with ADHD have _____ dopamine in parts of the brain.

impulsivity; low; shifting; organizing; norepinephrine; low

Medications used to treat ADHD include:

1. CNS _______

2. Selective norepinephrine ____ inhibitor. 

3. Centrally-acting ____________.

4. Tricyclic ______

stimulants; reuptake; sympatholytics; antidepressents

Narcolepsy is caused by a loss of wake-promoting _____. It is characterized by:

1. Difficulty staying ___.

2. Poor regulation of REM _____. 

3. Disturbed nocturnal sleep

4. Excessive _____ sleepiness.

There are ____ treaments to treat this directly, but ______ stimulants can induce a hyperarousal state allowing for wakefulness during day.

neurons; awake; sleep; daytime; no; psychomotor

Dopamine, NE, and epinephrine are in the class called _____. They have ___ structure and synthesis pathways.

NE and dopamine are synthesized ______, stored in vesicles, and then released upon neuron ____, and bind to both postsynaptic and presynaptic receptors. 

They are then eliminated from the synapse primarily by ____ but they can either be recycle into synaptic vesicles or metabolized into ____ metabolites.

catecholamines; similar; presynaptically; activation; reuptake; inactive

Amphetamine is a _____ release which means it stimulates presynaptic ____ of dopamine and NE, even without an ____ potential. 

It  is used to treat _____, narcolepsy, and obesity.

catecholamine; release; action; ADHD

Lisdexamfetamine is a _____ releaser. It is a ____ of amphetamine meaning there will be a ____ release of amphetamine during the day. It is used to treat ____ and obesity.

catecholamine; prodrug; slow; ADHD

Which drug is a catecholamine releaser and can be used to treat ADHD and narcolepsy?

amphetamine

Which drug is a catecholamine releaser and a prodrug of amphetamine?

lisdexamfetamine

Methylphenidate is a ____ inhibitor. It is a _____ reuptake inhibitor. It is used for ADD and ____ and is preferred for _____.

reuptake; dopamine; ADHD; adolescents

Which drug is a dopamine reuptake inhibitor and is preferred fo adolescents?

methylphenidate

Atomoxetine is a _____ inhibitor. It is a selective _____ reuptake inhibitor. It is marketed as a _____ ADHD stimulant and is used to treat ADHD.

It has ___ dopaminergic effects and more noradrenergic effects than amphetamine.

reuptake; norepinephrine; nonstimulant; fewer

Which drug is a selective NE reuptake inhibitor?

atomoxetine

Bupropion is a ____ inhibitor of both dopamine and ______. It is treated for ____, seasonal depressive disorder, ____ cessation and ADHD (off label).

reuptake; norepinephrine; depression; smoking

What drug is a dopamine and NE reuptake inhibitor?

bupropion

Cocaine is a reuptake _____ inhibitor of dopamine, NE, and _____. It is also a voltage-gated Na channel inhibtor leading to local _____ action.

It is used as topical anesthesia

transporter; serotonin; anesthetic

Which drug is a dopamine, NE, and serotonin reuptake transporter inhibitor?

cocaine

Modafinil is an _____ reuptake inhibitor. This drug allows for little euphoria, lower ____ potential, and fewer ___ effects than other psychomotos.
It can be used for _____, obstructive sleep apnea and is also used by the military to keep soldiers ____.

atypical; addiction; side; narcolepsy; awake

Which drug is an atypical reuptake inhibitor and is used to treat narcolepsy?

modafinil

Effects of stimulants are ____ dependent meaning it becomes more severe as the dose increases. There are two categories of adverse/toxic effects:

1. The _____ effect include headache, dizziness, tremor, insomnia, etc. Acute toxicity can lead to ____ symptoms like paranoia, hallucinations, etc. Insomnia occurs if a person takes the drug at a later ___ causing the effects to persist into bedtime. There is also _____ suppression which lead weight loss and growth suppression in children/adolescents. There should be “drug ____” which are days without meds for children/adolescents. Sympathetic effects include increased ______.

2. The _____ effects which includes chilld, cardiac arrhythmia, chest pain/angina. Acute toxicity leads to increased ____ (acronym) and HR as it directly targets B-1 adrenergic receptors. There is also xerostomia or ___ mouth due to a combination of vasoconstriction and lack of salivation. This also leads to risk of ___ decay.

dose; CNS; psychotic; time; appetite; holidy; sweating; cardiovascular; BP; dry; tooth

Psychomotor stimulants are contraindicated with monomaine _____ inhibitors (MAOIs) because it decreases ____ of NE and dopamine causing an increase of NT levels which can lead to _____.

oxidase; metabolism; toxicity

Tolerance to psychomotor stimulants are generally ___, but you end up developing tolerance to mood ____ and appetite suppressant.

Patients treated for narcolepsy with modfinil do ___ demonstrate tolerance.

mild; enhancing; not

Many of the psychomotor stimulatns are extensive psychological dependence meaning they are highly _____. These are regulated as schedule ____ substances.

Physical withdrawal is generally ____, and treatment is not necessarily required. These symptoms include ____ (negative feeling of self), depression, sleepiness. 

The major problem is to help the patient resist the urge or ____ to restrart compulsive use.

addictive; 2; mild; dysphoria; craving

Methylxanthenes are _______ stimulants. These inhibit the enzyme _______ OR is an adenosine receptor ____. 

Overall this leads to CNS ____ and smooth muscle ____. 

This drug has______ dependent effects. At ____ doses it can lead to headache, nausea, vomiting. At ____ doses it can lead to cardiac arrythmia and seizures.

Withdrawal symptoms include lethargy, ____, and headache.

nonpsychomotor; phosphodiesterase; antagonist; stimulation; relaxation; dose; moderate; high; irritability

Theophylline is a ________. It is ____ acting and is found in tea. It is available as orally or as an ___.

It can be off-labeled used for ____ obstruction, bradycardia, and acute cardiac ____.

methylxanthene; long; IV; airflow; decompensation

Which drug is a methylxanthene and is long acting?

theophylline

Caffeine is a _____. It is ____ acting and is found in coffee. It is used recreationally for ___ effects but therapeutically can be used for headaches, ____ relief, and hypotension.

methylxanthene; intermediate; stimulant; migraine

Which drug is a methylxanthene and is intermediate acting?

caffeine

Nicotine is a source of reinforcement of ____ products. It is an ___ for the nicotinic acetylcholine receptor and produces -___ effects. It has a ____ duration of action. 

It is marked with tolerance and behavioral/physical _____. 

Withdrawal symptoms includes irritability, impatience, ____, anxiety, depressed ___, difficulty ____.

tobacco; agonist; stimulant; short; dependence; hostility; mood; concentrating 

To treat smoking cessation or to nicotine abstinence you can do replacement therapy in which it is available as an _____, a nasal spray, gum, lozenge, and a transdermal ____.

It provides nicotine via different ____ of administration but they do have a high ____ rate. 

inhaler; patch; route; relapse

Bupropion is part of the ____ abstinence therapies. It is indicated for ____ associated with cessatoin. 

It is a ___ release formulation with modest effects. There is an increased risk fo ____ and is offered orally.

nicotine; cravings; sustained; seizures

Which drug is indicated for cravings associated with smoking?

bupropion

Varenicline is a ___ agonist of the nicotinic acetylcholine receptors. It is indicated for ____ cessation and produces less euphoric effects and ____ effective nicotine replacement.

Adverse effects include ____ effects like headache, insomnia, abnormal dreams, etc.

partial; smoking; more; CNS

Which drug is a partial agonist for nicotinic acetylcholine receptors?

varenicline