Drug Effect Characteristics

Epinephrine
SNS NT catecholamine -
all alpha and beta
receptor stimulation
increase HR, constrict blood vessels,
dilate vessels to skeletal muscle and
liver, bronchodilator. Used for
Anaphylaxis
Norepinephrine
SNS NT catecholamine -
alpha1/2 and beta 1 fight or flight
Metyrosine
Inhibitor of Tyrosine
Hydroxylase
Inhibits production of all catecholamines
- used in pheochromocytoma where
making excess epi and nor epi
L-Dopa
Precursor to
catecholamine synthesis
Bypasses the RLS and can cross the
BBB easier than dopamine so given as a
therapy for parkinson's disease allowing
brain to make dopamine easier. SNS
side effects throughout body though.
Tyramine
naturally occuring MAO
compound found in foods
that acts as
catecholamine releasing
agent
large intake with MAO inhibitors -
hypertensive crisis
Amphetamine
Indirect General Agonist
CNS stimulant. Releases
stored catecholamines
facilitates release of NE, Epi, DA. Also
blocks reuptake and blocks degradation
by MAO. Used for ADHD and narcolepsy.
High abuse potential - more potent than
cocaine which only blocks reuptake.
Causes tolerance.
Ephedrine
Indirect General Agonist
Releases stored
Catecholamines.
Activates alpha and beta
receptors and increases
catecholamine release
release of Ne into nerve terminal and
weakly stimulates beta receptors =
bronchodilation, increased hr, increased
bp. Found in weight loss drugs and
nasal decongestants. Tolerance
develops. Starting material for synthesis
of methamphetamine.
Cocaine
Indirect General Agonist
Serotonin/epinephrine/no
repinephrine/dopamine
reuptake inhibitor
increases catecholamines in the synapse
so have greater affect. Can cross BBB
and cause addiction by affecting the
mesolimbic reward pathway.
Desipramine
Tri cyclic Norepinephrine
reuptake inhibitor
used as a tri-cyclic anti-depressant,
very selective (Only NE) and potent,
also used for ADHD (underproduction of
norepinephrine has been associated
with ADHD). Does not cause tolerance
because only blocks NE (DA causes
tolerance). Also causes cardiac
arrhythmias.
Selegiline/Phen
elzine
Selective Inhibitor of
MAO-B
because of slectivity, MAO-A can still
continue to metabolize tyramine so
fewer food-drug interactions.
Aminophylline
Competitive non-
selective
phosphodiesterase
(normally removes cAMP
in cell) inhibitor
Increases cAMP leading to
brochodilation (use is for asthmatics
that are also on beta blockers for HTN
treatment so can't use albuterol) - less
potent and shorter acting than
theophylline. But are non-specific so
also get increased heart rate (which
consumes o2) and contactility (other
effects of increased cAMP - D and beta
receptors). not used.
Theophylline
Competitive non-
selective
phosphodiesterase
inhibitor
Increases cAMP leading to
brochodilation (use is for asthmatics
that are also on beta blockers so can't
use albuterol)
Sildenafil (AKA
viagra) Selective PDE-5 inhibitor
increases cGMP which is only found in
certain tissues - smooth muscle in penis
relaxes allowing for erection. Also
decreses resistance in lungs (for
pulmonary HTN) and increases cerebral
blood flow.
Isoproterenol
non selective beta
adrenergic agonist - beta
1 and 2
used for bradychardia/heart block to
increase contractility. Can also be used
for asthma to bronchodilate but not
used for this much
Dopamine
D1 Receptor Agonist
D1>beta1>alpha1
low dose = increase blood flow to
kidneys. Higher dose = beta1 effects =
increase hr and contractility. High dose
= include vasoconstriction. Use in shock
to increase CO via beta1 and preserve
kidney function via D1
Dobutamine
Primarily B1 Receptor
Agonist
increases contractility with no real
change in heart rate. Inotropic. Used to
treat acute but potentially reversible
heart failure
Albuterol Beta 2 selective agonist
leads to bronchodilation via increase in
cAMP - use in asthmatics, inhaled.
Ritodrine Beta 2 selective agonist
leads to bronchodilation, also used to
prevent premature uterine
contractions (good to prevent delivery
before fetal respiratory tract developed)
Propanolol
Non-selective beta
blocker decrease CO
Metoprolol beta1 selective blocker
Treatment of diseases such as
hypertension. Greater exercise tolerance
because beta2 receptors can still
mediate vasodilation. Also
glycogenolysis is less impeded so better
for diabetics.
Pindolol weak beta blocker
Treatment of diseases such as
hypertension. Doesn't slow heart rate as
much but still blocks increase in HR and
CO produced by SNS stimulation so less
likely to cause severe bradychardia in
pts with htn and low hr (athletes). So
better for exercise tolerance.
Carvedilol alpha1 and beta blocker
blocking beta = decreased CO and
blocking alpha = vasodilation. So used
to treat htn. Decreases
mortality/morbidity in pts with heart
failure. Also decreases size of heart wall
and is antioxidant
Labetalol alpha1 and beta blocker used to treat htn in pregnancy.
Phenylephrine selective alpha 1 agonist
causes vasoconstriction of nasal blood
vessels = decongestant, dilates pupil,
increases bp and decreases hr via
baroreceptor reflex. Given as a nasal
spray reduces the systemic side effects
on bp and hr. extended use = rebound
hyperemia and ischemia.
Clonidine
alpha 2a agonist in the
brain
decreases SNS output (NE release) =
decreased bp - used for htn, touretts
syndrome, and drug withdrawal. Works
within the CNS. Can also stimulate post
synaptic alpha 2 receptors causing
vasoconstriction but this is only at high
doses (also why better given orally over
IV). over time the lack of SNS
stimulatio will increase the receptors so
if suddenly go off the drug then htn will
be very bad. is physiologic
effect.Application for hypertension
(especially with renal disease)
Brimonidine
Alpha 2 adrenergic
agonist
Vasoconstriction of blood vessels
leading to reduction in aqueous humor
flow. Lowering of intraocular pressure in
patients with glaucoma or ocular
hypertension.
Phentolamine Alpha1 antagonist Anti-hypertensive.
Phenoxybenzam
ine
Non-selective Irreversible
Alpha antagonist
noncompetitive/irreversible. Alkylates
receptors (including serotonin and
histamine). Not used much. Only to
block catecholamine affects before
surgery to remove pheochromocytoma
Prazosin Alpha1 antagonist
anti-hypertensive. Better than
phentolamine because less reflexive
tachycardia. Orthostatic htn with first
dose though.
Tamsulosin Alpha1 antagonist
treatment of BPH because causes
relaxation of smooth muscle of prostate,
trigone muscle of bladder, and urethra.
Less orthostatic hypotension because is
1A selective.
"-olol" Beta Antagonist suffix
"-terol" Beta 2 Agonist suffix
Aspirin
Effect:
SALICYLATE: Analgesic
and Anti-inflammatory
Characteristics:
Acetaminophen
Effect:
Analgesic only (use in
asthmatics, kids,
pregnant women)
Characteristics:
Ibuprofen
Effect:
PROPRIONIC ACID:
Analgesic and Anti-
inflammatory
Characteristics:
Naproxen
Effect:
PROPRIONIC ACID:
Analgesic and Anti-
inflammatory
Characteristics:
Ketoprofen
Effect:
PROPRIONIC ACID:
Analgesic and Anti-
inflammatory
Characteristics:
Diflunisal
Effect:
SALICYLATE: Analgesic
and Anti-inflammatory
Characteristics:
Sulindac
Effect:
ACETIC ACID: Anti-
Inflammatory Only
Characteristics:
Indomethacin
Effect:
ACETIC ACID: Anti-
Inflammatory Only
Characteristics:
Celecoxib/Celeb
rex
Effect:
COX2 INHIBITOR: Anti-
Inflammatory Only: black
box
Characteristics:
Rofecoxib
Effect:
COX2 INHIBITOR:
Analgesic and Anti-
inflammatory: Removed
from market
Cortisol
Effect:
Short Acting
Glucocorticoid (8-12
hours)
Characteristics:
Cortisone
Effect:
Short Acting
Glucocorticoid (8-12
hours)
Characteristics:
Fludrocortisone
Effect:
Mineralocorticoid (8-12
hours)
Characteristics:
Prednisone
Effect:
Short Acting
Glucocorticoid (8-12
hours)
Characteristics:
Triamcinolone
Effect:
Intermediate Acting
Glucocorticoid (12-36
hours)
Characteristics:
Dexamethasone
Effect:
Long lasting
Glucocorticoid (36-72
hours)
Characteristics:
Aminoglutethimi
de
Effect:
Anti-Steroid
Characteristics:
Blocks initial step of
Metyrapone
Effect:
Anti-Steroid
Characteristics:
Tests the capacity of HPA
Pentobarbital
Effect:
Barbiturate - General
CNS depressant: depress
heart rate, lower bp,
depress respiration
Characteristics:
High GABA affinity but
also blocks calcium and
AMPA receptorssedation
side effects = not used.
Very long t1/2 - 40
hours, knocks patients
out for days
Thiopental
Effect:
Barbiturate - General
CNS depressant: depress
heart rate, lower bp,
depress respiration
Characteristics:
Highly lipophilic -
absorbed quick but
duration of action short.
Induction agent.
Phenobarbital
Effect:
Barbiturate - General
CNS depressant: depress
heart rate, lower bp,
depress respiration
Characteristics:
Used as anti-seizure:
increase GABA affinity =
cl channels open longer.
Vincristine
Effect:
Targets Mitotic Spindle
Characteristics:
Prevents polymerization
of microtubules. TX: HL
Paclitaxel
Effect:
Targets Mitotic Spindle
Characteristics:
Enhances microtubule
formation. TX: Breast CA
(in addition to CMF)
Cyclophosphami
de
Effect:
Alkylating/DNA Cross-
linking
Characteristics:
Pro-Drug: metabolized by
P450 into phosphoramide
mustard (cytotoxic) and
acrolein (causes cystitis).
Co administer with
MESNA to decrease
cystitis side effect.
Decrease in WBC so
monitor. TX: Breast CA
(C in CMF), Hodgkins,
NH, leukemia
Mechlorethamin
e
Effect:
Alkylating/DNA Cross-
linking
Characteristics:
Derived from poison gas.
(The C in CMF). Causes
Immunosuppression.
Cisplatin
Effect:
Alkylating/DNA Cross-
linking
Characteristics:
SIDE EFFECT = Renal
Insufficiency.
Doxorubicin/
Adriamycin
Effect:
Topoisomerase Inhibitor
Characteristics:
causes cardiotoxicity so
must limit LIFETIME dose
(women > men). TX:
Breast CA in AC combo
for those that not
respond to CMF TX
Irinotecan
Effect:
Topoisomerase Inhibitor
Characteristics:
TX: Colon CA with
FOLFIRI combo (FOL =
folinic acid - leucovorin,
F=5-FU, IRI = irinotecan)
5-FU
Effect:
Anti-Metabolite
Characteristics:
inhibits thymidylate
synthase needed for
dUMP to dTMP
competitively = no DNA
synthesis. TX: Breast CA
(F in CMF) and colon CA
(F in FOLFIRI). Increased
cytotoxicity via
metotrexate and
leukovorin
Methotrexate
Effect:
Anti-Metabolite
Characteristics:
Blocks DHFR = not make
dTMP = no DNA
synthesis. TX: Breast CA
(M in CMF). Side effects:
nephrotoxicity,
neurotoxicity, bone
marrow suppression
Leucovorin
Effect:
antidote to methotrexate
toxicity
Characteristics:
Used to rescue normal
cells in the bone marrow
from toxic effects of
methotrexate (in excess
also allows 5-FU to
inhibit more efficientyl)
Trastuzumab
Effect:
mAb - humanized
Characteristics:
Targets HER2 seen in
aggressive Breast CA
(poor prognosis), with
chemo = increase in
survival. Also causes
cardiac toxicity
Cetuximab
Effect:
mAb - chimeric
Characteristics:
targets EGFR in
metastatic colorectal CA.
When used with FOLFIRI
is only benefit if have
wild type Kras. Have GI
and skin side effects
(rash and
vomit/diarrhea)
Rituximab
Effect:
mAb - chimeric
Characteristics:
Destroys B cells and
tehrefore used to treat
disease characterized by
excessive numbers of B
cells. Tx: Lymphomas,
Leukemias, Transplant
rejection, autoimmune
disorders.
Bevacizumab
Effect:
mAb - humanized
Characteristics:
Neutralizes circulating
VEGF receptors which
prevents angiogenesis
but not work and causes
HTN. So only use is in
Macular Degeneration
Gefitinib
Effect:
Small Molecule Kinase
Inhibitor: EGFR
Characteristics:
Target: EGFR receptor.
Side effect = skin toxicity
(present in everyone)
Erlotinib
Effect:
Small Molecule Kinase
Inhibitor: EGFR
Characteristics:
Target: EGFR receptor.
Not work against
mutated T790 gene.
Lapatinib
Effect:
Small Molecule Kinase
Inhibitor: HER2
Characteristics:
very selective for HER2 -
is most selective KI
Imatinib
(Gleevec)
Effect:
Small Molecule Kinase
Inhibitor: Bcr/Abl
Characteristics:
targets the wild type abl
receptor in CML.
Resistance develops
quickly
Sorafenib
Effect:
Small Molecule Kinase
Inhibitor: VEGFR
Characteristics:
Broad Spectrum inhibitor,
but primary target is
VEGFR
Sunitinib
Effect:
Small Molecule Kinase
Inhibitor: VEGFR
Characteristics:
Broad Spectrum inhibitor,
but primary target is
VEGFR
Bortezomib
Effect:
Small Molecule Kinase
Inhibitor: Proteosome
inhibitor
Characteristics:
Inhibits protease by
binding proteosome
machinery (in all cells
though) causing CA cell
apoptosis. Used in
multiple Myeloma. Side
effects are many
including neutropenia
Vemurafenib
Effect:
Small Molecule Kinase
Inhibitor: BRAF
Characteristics:
Specific inhibitor of
mutant BRAF in
Melanoma. A major side
effect is squamous cell
cancer in 12% of patients
Ipilimumab
Effect:
T-Cell Modulator:Blocking
Antibody increases T-cell
reaction
Characteristics:
Enhanced T-cell reaction
and more potent anti-
tumor reaction by
blocking CTLA-4(an
inhibitor receptor). Side
effects of rashes and
diarrhea/colitis
Anti-PD1
Effect:
T-Cell Modulator:Blocking
Antibody results in
preferential T-cell
activation
Characteristics:
Enhanced T-cell reaction
and more potent anti-
tumor reaction by
blocking interaction
between PD-1 and PD-L1
which signal T cells to
apoptose. Side effects of
rashes and
diarrhea/colitis