CNS Stimulants
1. Analeptics
2. Anorexiants
3. Antidepressants
4. Serotonin agonists
CNS Stimulants: Adverse effects
• CVS: Palpitation, tachycardia,
hypertension, angina, dyshythmia
• CNS: Nervousness, restlessness, anxiety
• Endocrine: Hypoglycemia, hyperglycemia
• GIT: Nausea, vomiting,diarrhea
Analeptic
• Used to stimulate respiration when natural
reflex is lost
• H-cholinomimetic (reflex analeptic)
• Central analeptic (Aminophyllin,
theophylline,Caffeine, Doxapram)
Did You Know?
• Caffeine is a xanthine alkaloid compound that
acts as a stimulant in humans. Caffeine is
sometimes called guaranine when found in
guarana, mateine when found in mate, and
theine when found in tea. It is found in the
leaves and beans of the coffee plant, in tea,
yerba mate, and guarana berries, and in small
quantities in cocoa, the kola nut and the Yaupon
Holly. Overall, caffeine is found in the beans,
leaves, and fruit of over 60 plants, where it acts
as a natural pesticide that paralyzes and kills
certain insects feeding upon them.
Chemical Properties
Molar Mass = 194.19 g mol−1
Density: 1.2 g/cm³
Phase: Solid
Melting Point: 237 °C
Boiling Point: 178 °C
Uses of Caffeine
• Caffeine is a central nervous system (CNS)
stimulant, having the effect of temporarily
warding off drowsiness and restoring
alertness. Beverages containing caffeine,
such as coffee, tea, soft drinks and energy
drinks enjoy great popularity: caffeine is
the world's most widely consumed
psychoactive substance. In North
America, 90% of adults consume caffeine
daily.
Metabolizing Of Caffeine
• Caffeine is completely absorbed by the stomach and small
intestine within 45 minutes of ingestion. After ingestion it
is distributed throughout all tissues of the body and is
eliminated by first-order kinetics. The half-life of caffeine
varies widely among individuals according to such factors
as age, liver function, pregnancy, some concurrent
medications, and the level of enzymes in the liver needed
for caffeine metabolism. In healthy adults, caffeine's halflife is approximately 3-4 hours. In women taking oral
contraceptives this is increased to 5-10 hours, and in
pregnant women the half-life is roughly 9-11 hours.
Caffeine can accumulate in individuals with severe liver
disease when its half-life can increase to 96 hours.
Caffeine
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AP
Hate rate
Respiratory stimulation
Adjunctive effect
Doxapram
• over dosage of CNS depressant
• COPD (chronic obstructive pulmonary
disease
• Respiratory depression in postoperative
recovery period
Doxapram: Contraindication
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Newborn
Epilepsy
Hypertension
Stroke
Amphetamines
• Produce mood elevation or euphoria,
increase mental alertness and capacity for
work, decrease fatigue and drowsiness,
prolong wakefulness.
Amphetamines usage
• Narcolepsy
• ADHD (attention-deficit/hyperactivity
disorder
Amphetamines
• Tolerance
• Psychological dependence
• High abuse potential (under Control
Substance Act
Methylxanthines
• COPD (chronic obstructive pulmonary
disease
• Respiratory depression in postoperative
recovery period
Anorexants
• Central acting (Benzphetamine,
diethylpropion, Sibutramine)
• Metabolism acting (orlistat)
Antidepressants
• Used to treat depression
• Depression, common feelings
– Pessimism
– Worry
– Intense sadness
– Loss of concentration
– Slowing of mental processes
– Problems with eating and sleeping
Serotonin agonist (Sumatriptan)
• Treatment of migraine
Antidepressants
Common Symptoms of Depression
– Loss of interest in
usual activities
– Low self-esteem
– Self-pity
– Significant weight loss
or gain
– Insomnia or
hypersomnia
– Extreme restlessness
– Loss of energy
– Feelings of
worthlessness
– Diminished ability to
think
– Feelings of guilt
– Recurrent thoughts of
death
– Suicide attempts
Antidepressants
Depression
• Women are affected more often than men
• When men are affected, it is usually later
in life
• Levels of neurotransmitters in the brain
may be a causative factor
Mood Disorders
• Mania
• Bipolar Disorder
• Unipolar Disorder
Mood Disorders
• Mania
Mood of extreme excitement, excessive elation,
hyperactivity, agitation, and increased
psychomotor activity
• Bipolar Disorder
• Unipolar Disorder
Mood Disorders
• Mania
• Bipolar Disorder
Mood swings alternate between major
depression and mania
• Unipolar Disorder
Mood Disorders
• Mania
• Bipolar Disorder
• Unipolar Disorder
Major depression with no previous occurrence
of mania
Treatment for Depression
Electroconvulsive Therapy
• Introduction of brief, but convulsive
electrical stimulation through the brain
• Can induce seizures
• Effective for major and delusional
depression
Antidepressants
• Selective Serotonin Reuptake
Inhibitors (SSRIs)
• Cyclic Antidepressants
• Monoamine Oxidase Inhibitors
(MAOIs)
Antidepressants
Selective Serotonin Reuptake
Inhibitors (SSRIs)
– Block the reuptake of serotonin, with
little effect on norepinephrine
– Fewer side effects than older meds
Treatments
Cyclic Antidepressants
– Two Types
• Tricyclic antidepressants (TCAs)
• Tetracyclic antidepressants
– Prevent reuptake of norepinephrine
and/or serotonin
– Agents in this class differ in adverse
effects, cost, and response
Treatments
Monoamine Oxidase Inhibitors
(MAOIs)
Allows for buildup of norepinephrine at the
synapse
Drug List
SSRIs for Depression
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citalopram (Celexa)
escitalopram (Lexapro)
fluoxetine (Prozac, Sarafem)
fluvoxamine
paroxetine (Paxil)
sertraline (Zoloft)
venlafaxine (Effexor)
Dispensing Issues
Warning!
Look-Alike Drugs
– Prozac and Proscar (urinary drug)
– Zoloft and Zocor (high cholesterol)
– Celexa and Cerebyx (seizures) and
Celebrex (arthritis)
SSRI
Dispensing Issues
Warning!
• Do not discontinue abruptly
• Alcohol consumption should be avoided
while taking these medications
fluoxetine (Prozac)
• Indicated for major depression and
obsessive-compulsive disorder (OCD)
• Anorexia is a possible adverse effect
• Take in the morning to avoid insomnia
paroxetine (Paxil)
• Indicated for depression, obsessivecompulsive disorder, and panic disorder
venlafaxine (Effexor)
• Blocks reuptake of serotonin and
norepinephrine
• Indicated for depression
• May cause increase in blood pressure and
blurred vision
sertraline (Zoloft)
• Indicated for depression and obsessivecompulsive disorder
• Primary side effect is nausea
• May also cause drowsiness
citalopram (Celexa)
• Indicated for depression and obsessivecompulsive disorder
• Minimal drug interactions
escitalopram (Lexapro)
• Similar to Celexa
• More potent with fewer side effects
Drug List
Cyclic
Antidepressants
Tricyclic
• amitriptyline (Elavil)
• clomipramine (Anafranil)
• desipramine (Norpramin)
• doxepin (Sinequan)
• imipramine (Tofranil)
Drug List
Cyclic
Antidepressants
Tricyclic
• nortriptyline (Aventyl, Pamelor)
• protriptyline (Vivactil)
• trimipramine (Surmontil)
Tetracyclic
• maprotiline
Tricyclic Antidepressants
Dispensing Issues
Warning!
• Improvements are usually seen in
10 to 21 days
• Can be cardiotoxic in high doses
• May cause postural hypotension
Tricyclic Antidepressants
Dispensing Issues
Warning!
Do not discontinue abruptly.
Cyclic Antidepressants Side Effects
• Sedation is
common, but
tolerance usually
occurs
• Have many
anticholinergic
effects
Discussion
Why would cyclic
antidepressants be prescribed
for bed wetting in children?
Discussion
Why would TCAs be prescribed for bed
wetting in children?
Answer
They may be prescribed
because of their anticholinergic
side effects.
Drug List
MAOIs
• phenelzine (Nardil)
• selegiline (Eldepryl)
• tranylcypromine (Parnate)
MAOI
Dispensing Issues
Warning!
Be cautious of many interactions with
foods such as aged cheeses,
concentrated yeast extracts, pickled
fish, sauerkraut, broad bean pods,
chocolate, and alcohol.
MAOI
Dispensing Issues
Warning!
If changing to another class of
antidepressant, patient must have a
two-week “wash out” period before
starting the new medication.
Drug List
Other
Antidepressants
• bupropion (Wellbutrin, Zyban)
• mirtazapine (Remeron)
• trazodone (Desyrel)
trazodone (Desyrel)
• Prevents reuptake of serotonin and
norepinephrine
• Has a better side effect profile than TCAs
• Caution: possible interaction with Ginkgo
bupropion (Wellbutrin, Zyban)
• Dopamine-uptake inhibitor
• Does not cause sedation, blood pressure
changes, or ECG changes
• Do not discontinue abruptly
• Approved in the aid of smoking cessation
Other Antidepressant
Dispensing Issues
Warning!
• Wellbutrin SR = BID dosing
• Wellbutrin XL = QD dosing
Bipolar Disorders
Signs or Symptoms
– Decreased need for sleep
– Elevated or irritable mood
– Excessive involvement in pleasurable
activities with a big potential for painful
consequences
– Grandiose ideas
– Pressure to keep talking
– Racing thoughts
Discussion
What is the drug of choice for
treating bipolar disorders?
Discussion
What is the drug of choice for treating
bipolar disorders?
Answer
Lithium
Discussion
What is the two-fold objective of
drug therapy for bipolar
disorder?
Discussion
What is the two-fold objective of drug
therapy for bipolar disorder?
Answer
Treat acute episodes
Prevent subsequent attacks
Drug List
Drugs to Treat Bipolar
Disorders
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carbamazepine (Epitol, Tegretol)
divalproex (Depakote)
lithium (Eskalith, Lithobid)
olanzapine-fluoxetine (Symbyax)
valproic acid (Depakene)