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Drug
Aspirin
(acetylsalicylic
acid)
Therapeutic Use
Low dose: protection against
cardiovascular disease
Platelet aggregation
protection (MIs, strokes, etc.)
Mechanism of Action
Non-selective irreversible
inhibitor of COX-1/2.
For COX-1, alters active
binding site to prevent
substrate entry.
Drug/Drug
Interactions
Probenecid blocks
elimination.
Salicylate
See aspirin.
Ibuprofen (Advil)
NSAID
Naproxen (Aleve)
Reversible competitive
inhibitor of COX-1/2.
Inhibition of prostaglandin
synthesis.
Indomethacin
(Idocin)
Adverse Effects
Phys. Disposition
(ADME)
- Contraindicated in
Aspirin hydrolyzed in
children with fever due
plasma to salicylate.
to virus (may cause
Conjugated by
Reyes syndrome).
glutathione, glucoronic
- GI bleeding/uclers
acid, and sulfate
- Analgesic nephropathy, eliminated renally.
progressive renal failure
- Hepatic injury
- Respiratory and
metabolic acidosis if at
toxic levels.
More adverse effects
Metabolized by CYP
than aspirin.
GI discomfort and stress Acidic so well absorbed.
hemorrhage and
perforation.
Renal excretion,
extensively metabolized,
Analgesic nephropathy
undergo EH circulation.
Postpartum hemorrhage
for pregnant users (also
prolonged gestation and
inhibition of labor)
Celecoxib
NSAID
(anti-inflammation)
Inhibits COX-2
Misoprostol
Heparin
Anti-coagulant
Cardiovascular disease
(uncontrolled platelet
aggregation).
Black box warning.
Protamine sulfate
antagonist.
- Bleeding
- Hypersensitivity
(sometimes)
Drug
Therapeutic Use
unstable angina; prevent
thrombosis in extracorporeal
devices
Enoxaparin
(Lovenox)
Anti-coagulant
Prevent DVT,
thromboembolism, Pts with
HIT
Fondaparinux
(Arixtra)
Anti-coagulant
Prevent PE, DVT;
thromboprophylaxis for Pts
undergoing hip/knee surgery,
Pts with HIT
Dabigatran
(PRADAXA)
Anti-coagulant
Rivaroxaban
(Xarelto)
Apixaban
(Eliquis)
Warfarin
(Coumadin)
Anti-coagulant
Anti-coagulant
Anti-coagulant
Mechanism of Action
Drug/Drug
Interactions
- Transient
thrombocytopenia
- Heparin-induced
thrombocytopenia
- Contraindications:
history of
hypersensitivity to
heparins, active
bleeding, threatened
abortion, surgical
procedures in general,
infective endocarditis
- Bleeding
- Hypersensitivity
(sometimes)
- Transient
thrombocytopenia
See above for
contraindications.
- Bleeding
- Hypersensitivity
(sometimes)
- Transient
thrombocytopenia
See above for
contraindications.
Adverse Effects
Phys. Disposition
(ADME)
Does not cross into
placenta.
Must routinely monitor
Pt. because drug is
mixture of
unfractionated peptides.
Subcutaneous injection
Oral dose
Bleeding
Administered as
dabigatran etexilate
(prodrug).
Bleeding
Metabolized by CYP3A4
Bleeding
MANY. See last page.
Bleeding
100% bioavailable;
highly bound to plasma
Drug
Therapeutic Use
Mechanism of Action
Drug/Drug
Interactions
Gla modifications in
clotting factors factors
inactive
Adverse Effects
Pro-cogulative states
(inhibition of protein C
and S)
Can be overcome by
excess Vitamin K.
Phys. Disposition
(ADME)
protein; long half-life.
Extensively metabolized
(CYP-2C9), excreted in
urine.
Crosses placenta can
be teratogen.
Desirudin
Anti-coagulant
Bivalrudin
Anti-coagulant
Agratroban
Anti-coagulant
Clopidogrel
(Plavix)
Anti-coagulant (anti-platelet)
Use with Pt who are allergic
to aspirin or need synergic
effect with aspirin.
Aspirin
Anti-coagulant (anti-platelet)
Abciximab
NSAID
Anti-coagulant (anti-platelet)
Cortisol
Anti-inflammatory steroid;
immuno-suppressant
No TXA2 formation.
No hemostasis (platelet
change initiation).
Ig that inhibits GP2b/3a
receptor on platelets no
fibrinogen binding no
aggregation
- Inhibit phospholipase A2
(AA mobilization) via
increased synthesis of
annexin-1
- Decrease production of
PG and LT
- Inhibit COX-2 upregulation/synthesis
- Decrease TNF-
production by inhibiting
Rash, diarrhea,
abdominal pain,
dyspepsia, bleeding,
thrombotic
thrombocytopenia
Well absorbed;
extensive metabolism by
liver; 8 hr half life; urine
and fecal elimination
See above.
See above.
Needs to get
metabolized to be active.
See above.
May cause
hypertension because
also interacts with
mineralcorticoid
receptor with high
affinity.
(Licorice has
glycyrrhizic acid
which inhibits 11HSD 2 from
Abrupt cessation of
therapy acute adrenal
insufficiency (fever,
myalgia, arthralgia,
malaise).
Inactivated by liver
conjugation into inactive
metabolites, excreted in
liver
Drug
Therapeutic Use
Mechanism of Action
NFB (TNF-
transcription factor)
Prednisolone
Dexamethasone
Aldosterone
Flurocortisone
Chlorpheniramine
(Chlortrimeton)
Diphenhydramine
(Benadryl)
Dimenhydrinate
(Dramamine)
Anti-inflammatory steroid;
immuno-suppressant
Anti-inflammatory steroid;
immuno-suppressant
Diagnose causes of
hypercorticism
Mineralcorticoid (low blood
pressure)
Replacement therapy of
mineralcorticoid (low blood
pressure, aldosterone
deficiency)
Anti-histamine (1
generation)
st
Allergic rhinitis,
conjunctivitis, itching, atopic
& contact dermatitis,
urticaria, drug reactions,
motion sickness, local
Drug/Drug
Interactions
regulating high
cortisol levels.)
See Cortisol.
Adverse Effects
increased susceptibility
to infection, peptic ulcer
disease, osteoporosis,
osteonecrosis,
myopathy,
cataracts,behavior
disturbance, growth
suppression, Cushings
syndrome
See Cortisol.
See Cortisol.
Phys. Disposition
(ADME)
Use the lowest dose
possible to achieve
desired result because
not specific/curative.
See Cortisol.
Active ingredient for
prednisone. If Pt has
hepatic failure,
administer prednisolone
straight.
See Cortisol.
Retains Na+
Retains Na+ (125x
potency)
Inverse agonists to H1
receptor on smooth
muscle, endothelial
vessels, and CNS.
Depression drugs
inhibit MAO more
histamine
accumulation
Moderate glucocorticoid
potency.
Fat soluble, go through
membranes. Well
absorbed.
Hepatic metabolism.
Liposoluble, well
absorbed. Metabolized
by liver. Renal
excretion.
Crosses placenta and
breast milk.
Penetrates BBB anti-
Drug
Therapeutic Use
Mechanism of Action
Drug/Drug
Interactions
Loratadine
(Claritin)
Cetirizine
(Zyrtec)
Fexofenadine
(Allegra)
Anti-histamine (2nd
generation)
Adverse Effects
vision, dry eyes, dry
mouth, urinary retention,
constipation, ED),
fatality in young
children
Inverse agonists to H1
receptor on smooth muscle
and endothelial vessels
Allergic rhinitis,
conjunctivitis, itching, atopic
& contact dermatitis,
urticaria, drug reactions
Depression drugs
inhibit MAO more
histamine
accumulation
Contraindicated for
people with glaucoma,
prostatic hypertrophy,
impaired renal function,
elderly (impairs their
cognition), pregnant and
lactating women,
neonates, infants and
young children.
Even 30x overdose has
not seen any adverse
effects or fatality!
Contraindicated for
pregnant and lactating
women.
Phys. Disposition
(ADME)
Ach and sedation.
Liposoluble, well
absorbed. Metabolized
by liver. Renal
excretion.
Crosses placenta and
breast milk.
Differences:
Does not penetrate BBB,
longer lasting, some
metabolized by CYP3A4
Cetirizine is metabolite
of hydroxyzine.
Fexofenadine excreted
by bile and abs is
inhibited by some fruit
juices.
Cromolyn sodium
(Nasalcrom)