Uploaded by Marco-Antonio Hartmann, Ph.D.

EPPP Pharmacology-Table

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Class
Antidepressant
Subclass
Tricyclics
(TCAs)
Product
Imipramine
/Tofranil,
clomiprami
ne/Anafran
il,
amitriptylin
e/Elavil
Mechanism
block reuptake of
norepinephrine and
serotonin at synapses;
support catecholamine
hypothesis (depression
2/2 lower-than-normal
levels of the
neurotransmitter)
Selective
Serotonin
Reputake
Inhibitors
(SSRIs)
fluoxetine/
Prozac,
sertraline/Z
oloft,
paroxetine/
Paxil
block reuptake of
serotonin at synapses
Monoamin
e Oxidase
Inhibitors
(MAOIs)
phenelzine
/Nardil,
tranylcypro
mine/Parna
te
block action of enzyme
that breaks down
norepinephrine and
serotonin, making
these
neurotransmitters
more available at
synapses
SNRIs
venlafaxine
/Effexor,
duloxetine/
Cymbalta,
desvenlafaz
ine/Pristiq
bupropion/
Wellbutrin/
Zyban
NDRIs
Use
MDD w/
hopelessness, inability
to experience
pleasure, vegetative
sxs (i.e. appetite, sleep
disturbances, anergia);
Dysthymic D/O; Panic
Attacks, Agoraphobia;
OCD
(clomipramine/Anafra
nil);
enuresis (esp.
imipramine/Tofranil);
chronic pain
MDD, Dysthmic D/O;
OCD, Panic D/O, Social
Phobia, binge eating,
premature ejaculation
Side effects
anticholinergic effects (i.e., dry mouth,
constipation, urinary retention, blurred
vision)
GI sxs, impaired sexual funx, drowsiness,
confusion/memory impairment (esp. in
older adults); often effects subside within
few weeks, if not, may be eliminated by
lowering dosage;
serious effects: tachycardia, orthostatic
hypotension, arrhythmia
nausea, loss of appetite, impaired sexual
funx, agitation, headaches, insomnia;
combining w. TCA, MAOI, or other drug
that increases serotonin can cause
serotonin syndrome (i.e., altered
consciousness, agitation, other changes in
metnal status; autonomic changes –
sweating, dilated pupils; tremor, muscle
rigidity, akathaisia – motor restlessness)
Caution
toxicity if OD; caution
w. heart disease or
suicidal patients
Comparison
Relative to TCAs,
quicker
effectiveness,
fewer/less severe
side effects (incl.
anti-cholinergic
effects, sedation,
cognitive
impairment,
cardiovascular
effects), safer in
OD
Atypical or nonresponsive depression
(increased appetite,
hypersomnia,
rejection-sensitivity,
mood reactivity, sxs of
anxiety/hypochondria
sis),
MDD, GAD, Social
Anxiety D/O, Panic
D/O
sleep disturbances, nausea/GI concerns,
sexual dysfunx, headache, elevated blood
pressure
MDD, tobacco
cessation
dry mouth, agitation, insomnia,
itching/skin rash, decreased appetite; can
aggravate pre-existing seizures or
1
psychosis; can cause anaphylaxis (severe
allergic rxn)
Mood
Stabilizers
Lithium
Antiseizure
drugs
lithium
carbonate/
Eskalith,
Lithonat,
Duralith,
lithium
citrate,
Cibalith
Carbamaze
pine/Tegre
tol,
Valproic
acid/Depak
ote
unknown; appears to
effect dopamine,
norepinephrine,
serotonin
Bipolar, stabilizes
mood (depressive and
manic episodes),
redux of mood swings
nausea, diarrhea, metallic taste in mouth,
weight gain, hand tremor, fatigue, mild
cog. Impairment (i.e., confusion,
disorientation)
require monitoring to
avoid lithium toxicity
incl. vomiting,
abdominal pain,
diarrhea, tremor,
slurred speech, ataxia,
seizures, coma, death
useful for tx of
dysphoric mania and
mania w. rapid cycling
altering serotonin
levels
N/V, tremor, visual disturbances, ataxia
monitor blood levels;
liver failure w.
carbamazepine or
valproic acid,
agranulocytosis (low
white blood cell count)
and aplastic anemia w.
carbaamzepine
chlorproma
zine/Thoraz
ine,
thioridazin
e/Mellaril,
haloperidol
/Haldol
block dopamine
receptors in the brain;
dopamine hypothesis
Schizophrenia 2/2
overactivity of
dopamine receptors,
though research
suggests may be 2/2
imbalance of
dopamine and other
neurotransmitters:
Nore, Sero,
Glutamate, GABA.
Anticholinergic effects: dry mouth,
urinary retention, blurred vision,
tachycardia, gastric distress, sexual
dysfunx
Extrapyramidal Side effects: shuffling gait,
stooped posture, slurred speech);
dystonia (sustained muscle contraction or
spasms that cause involuntary movts);
akathisia; tardive dyskinesia (abnormal,
involuntary movt., esp. in face, tongue,
jaw; can be alleviated by gradually
withdrawing drug)
Neuroleptic malignant syndrome (NMS):
rare, life-threatening; muscle rigidity, high
fever, seating, unstable blood pressure,
altered mental status, autonomic dysfunx;
usually develops within 2 wks of drug tx;
onset is rapid, and must be immediately
dc’d to avoid fatality
++ Positive sxs (i.e.,
delusions,
hallucinations,
agitations) of
schizophrenia,
clozapine/C
lozaril,
risperidone
/Risperdal,
effect different
dopamine receptors, as
well as serotonin,
Antipsychotics
Traditional
APsych
Atypical
Antipsycho
tic
schizophrenia, other
psychotic d/o or sxs
little effect on negative
sxs (i.e., affective
flattening, anhedonia,
social withdrawal); also
psychosis, Tourette’s
D/O, acute mania
anticholinergic effects,
sedation, weight gain,
neuroleptic malignant
syndrome; clozapine
alleviate positive
and negative sxs;
less likely to cause
extrapyramidal
2
olanzapine/
Zyprexa,ari
prazole/Abi
lify
norepinephrine, and
glutamate receptors
Benzodiaze
pin
diazepam/
Valium,
alprazolam
/Xanax,
triazolam/
Halcion,
clonazepa
m/Klonopin
enhance activity of
inhibitory
neurotransmitter GABA
anxiety, insomnia,
muscle spasms,
seizures, mod/severe
sxs of etoh withdrawal
Barbituates
thiopental/
Pentothal,
amobarbita
l/Amytal,
secobarbita
l/Seconal
exert effect by affecting
GABA receptors in
reticular activating
system, medulla, and
certain areas of cortex
anesthetic, agitated
pts; short-term tx for
insomnia
secobarbital/Seconal
past: anxiety, but now
use benzo b/c safer
Azaspirone
buspirone/
Buspar
affecting dopamine,
norepinephrine,
serotonin levels
Anxiety disorders, esp.
GAD
can cause
agranylocytosis, which
is why not really rx’d
unless failed others
side effects;
typically effective
for pt w/ poor
response to
traditional
antipsyhotics
drowsiness/sedation
ataxia/incoordination/motor
disturbances, cognitive impairment (i.e.,
poor concentration, anterograde amnesia;
confusion/disorientation in older adults),
anticholinergic effects, sexual dysfunx;
chronic use can lead to
dependence, tolerance,
and withdrawal sxs
(irritability, insomnia,
agitation, dyphoria, GI
distress, rebound
anxiety – more severe
than original sxs; severe
withdrawal sxs –
seizures, delirium,
hallucinations, coma –
if abruptly dc after
taking high dose for
extended period of
time)
combining w. etoh
or other CNS
depressant can be
fatal
drowsiness, dizziness, ataxia,
confusion/cognitive impairment,
paradoxical excitement; regular use leads
to dependence, tolerance, and withdrawal
sxs, and seizures, delirium, or death of
sudden withdrawal; widely abused and
often implicated in accidental deaths and
suicides (fatally suppress respiration)
dizziness, light-headedness, nausea,
headache
combining w. etoh can
be fatal 2/2 effect on
brain structures
controlling breathing
SEDATIVES,
HYPNOTICS,
AND
ANXIOLYTICS
tx of anxiety w.o.
causing sedative,
muscle-relaxant effects,
or addiction
3
Other Drugs
NarcoticAnalgesics
natural
opioids
(opium,
morphine,
codeine),
synthetic,
semisynthetic
(heroin,
methadone
,
oxycodone
/Percodan.
OxyContin,
hydrocodo
ne/Vicodin,
meperidine
/Demerol)
mimick effects of
body’s natural
analgesics (endorphins,
enkephalins)
pre-operative
relaxation/sedation,
acute and chronic
pain;
methodone for heroin
addiction (does not
produce euphoric
effects, but reduces
cravings and
withdrawal sxs)
dry mouth, nausea, pupil constriction,
cough suppression, hypotension, sexual
dysfunx, respiratory depression; chronic
use leads to dependence, tolerance, and
withdrawal sxs, and eventually lose
pleasure from drug and use only to avoid
sxs of withdrawaal;
Widely abused drugs;
Withdrawal sxs: early
sxs like those of bad col
or flu (runny nose,
watery eyes, nausea,
fever, yawning); later
sxs include insomnia,
muscle/joint pain,
abdominal cramps, N/v,
diarrhea, elevated
blood pressure
Psystimulants
methylphe
nidate/Rital
in/Concert
a,
pemoline/C
ylert,
amphetami
nedextroamp
hetamine/
Adderall
atomoxetin
e/Strattera
mimic/potentiate
action of
norepinephrine and
dopamine in brain
ADHD, narcolepsy
insomnia,
decreased appetite/weight loss,
stomachaches, dysphoric mood (anxiety,
irritability, sadness);
can exacerbate tics, so rx w. care for those
w. personal/ family hx
“drug holidays:” during
winter and summer
vacations, can help
reverse growth
suppression
block reuptake of
norepinephrine; nonstimulant
ADHD, ages 6+
decreased appetite, dizziness, fatigue,
irritability; in adults, sexual dysfunx and
menstrual cramps; possibly increase s/I in
children/adolescents
E.g.
propranolol
/Inderal
inhibit activity of
sympathetic nervous
system by blocking
beta-adrenergic
receptors, which then
slow heart rate and
lower blood pressure
HTN, cardiac
arrhythmias, migraine
headaches, essential
tremor; physical sxs of
anxiety (i.e.,
palpitations, tremors,
sweating)
bradycardia, hypotension, sexual dysfunx,
fatigue, nausea, vision changes, dizziness,
depression; avoid abrupt withdrawal
(headaches, tremors confusion, HTN,
cardiac arrhythmia)
Norepinep
hrine
Reuptake
Inhibitors
(NRIs)
Betablockers
also drugs of
abuse, such as
cocaine and
methamphetamin
e
less effective than
benzos for
cognitive sxs of
anxiety (i.e.,
worry,
apprehension)
4
Antialcohol
Drugs
disulfiram/
Antabuse,
naltrexone
(ReViia,
Vivitrol)
disulfiram/Antabuse
inhibits etoh
metabolism; when
taken w. etoh, causes
N/V, SOB, tachycardia,
other unpleasant sxs;
etoh abuse and
dependence
naltrexone/Revia/Vivit
rol: opioid receptor
antagonist; reduces
pleasurable effects
of/craving for etoh
disulfiram/Antabuse (in absence of etoh:
drowsiness, skin rash, headache,
restlessness, impotence; overdose:
seizures, low b.p. chest pain, SOB, death);
naltrexone/ReVila/Vivitrol (stomach pain,
N/V, fatigue, headache, joint/muscle pain;
high dose can cause liver damage)
5
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