Drug Chart Pharm 3
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Transcript of Drug Chart Pharm 3
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Mechanism of Action Use Adverse Effects
Acyclovir Competitive inhibitor of nucleic
acid polymerases
(when inserted instead of base
missing hydroxyl group so no
phosphodiester bond suicidesubstrate, chain terminator)
HSV, VSV, EBV Generally well tolerated but
high IV dosing can cause
nephrotoxicity and
neurotoxicity
Drug resistance acan dveleop
with mutation in viral TK or
viral DNA pol
Can have as much as 50% in
CSF
Can interact with AZT(severe
lethargy) and nephrotoxic
drugsOseltamivir
Selective Neuraminidase
inhibitor; sialic acid analogues,
inhibit viral neuraminidase,
which cleaves sialic acid residues
to facilitate release from host cell
(stop viral release from cell)
Influenza A and B, treat within
48 hrs of onset, reduces time of
illness
transient mild moderate GI
distress, minimized with food
eliminated primarily
unchanged in the kidneys so
decrease dose in kids and
those with renal impairment
Zidovudine (AZT) Nucleoside/Nucleotide ReverseTranscriptase Inhibitors (NRTI)
Fully phosphorylated forms (i)
compete for RT, and (ii) function
as chain terminators block
viral replication
suppression of HIV infection;elevate CD4 counts, AZT use
during pregnancy reduces HIV
transmission to fetus
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Indinavir (IDV) inhibition of HIV protease, which
essential for the production of
mature, mediates post-
translational processing of viralgene products, cleaves itself then
other products
HIV, combination therapy - metabolized primarily via
cytochrome CYP3A4, other
drugs acted on CYP3A4 may
accumulate to dangerouslevels other drugs inducing
CYP3A4 may increase
metabolism
- resistance develops rapidly,
buffalo hump, due to fat
redistribution
also hyperglycemia,
nephrolithiasis
- absorption of this drug
impaired by high fat meal
Penicillin G lactam ring fused to five
membered thiazolidine ring and
R group; lactams irreversibly
inhibit transpeptidases and
decrease cross-linkage of glycan
strands compromising the cell
wall
less susceptible to lactamase
Bactericidal at therapeutic
concentrations
Generally well tolerated but
10% have allergy to whole
class
GI problems: nausea,
diarrhea vomiting
penicillins work best against
actively growing bacteria,
thus bacteriostatic antibiotics
(chloramphenicol,
macrolides, tetracyclines)
interfere with their activity
low pH, dextrose solns,
aminoglycosides solns:
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inactivate lactam
probenecid (gout) blocks
renal excretion, active lactam in blood longer
Amoxicillin Inhibit cell wall synthesis Superinfection with
Clsotridium difficile;
alteration of normal flora
allows this bacteria to grow;
produces toxin causing
diarrhea
Amoxicilin/Clavulanic
Acid (Augmentin)
Amoxicillin Inhibit cell wall
synthesis and clavulanic acid is a
lactamase inhibitor
broader spectrum activity GI: diarrhea, nausea, vomiting
most common with this
combination drugCeftriaxone Cephalosporin; inihibit cell wall
synthesis
3rd generation, broader
spectrum activity
Prolonged use causes biliary
sludging (pain, nausea,
vomiting) in up to 43%
Ciprofloxacin are bactericidal and target
topoisomerases which increased
the supercoiling of DNA which
impacts DNA replication, repair
and transcription
tolerated by humans well
because the drug has a greater
affinity for bacterial
topoisomerases and bacteria are
actively growing (replicating and
repairing DNA more)
metals chelate quinolones,
block adsorption; many
antacids, some dietary
supplements; take quinolones
2 hrs prior or 2-6 hrs after
digesting metals
Avoid in children,
pregnant/nursing women
(damage growing cartilage)
avoid in patients taking
drugs prolonging QT
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interval, arrhythmias,
fainting
TMP/SMX antifolate Recurrent UTIs, opportunistic
infections in AIDS
antifolate activity in humans,
may be offset withsupplement folic acid;
nephrotoxicity avoid in
renal impaired
Azithromycin Protein synthesis inhibitors;
bacteriostatic
treat infections caused by
Gram-positive bacteria; also
works well against several
Gram-negatives
Contraindication: hepatic
impairment
Antacids lower the serum
level of Azithromycin
GI: cramps, diarrhea, nausea,
vomiting
Erythromycin Protein synthesis inhibitors;
bacteriostatic
treat infections caused by
Gram-positive bacteria
Contraindication: hepatic
impairment
Drug Interactions:
Erythromycin inhibits the
cytochrome P450 System
(CYP3A4); interactions
common with other drugs
metabolized by CYP3A4
stimulates GI motility; GI
intolerance may force switch
of drug
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Cardiotoxicity: arrhythmia,
do not administer wih drugs
that prolong QT interval
Doxycycline Protein synthesis inhibitors;bacteriostatic
Caution: children under 8years; pregnant lactating
(category D); patients with
liver impairment
GI distress in some cases
GERD, Photosensitivity
Skeletal: avoid use in children
as drug binds bones and teeth
Rifampin inhibits DNA-dependent RNA
polymerase, blocks txn binds to
bacterial form with greater
affinity than eukaryotic
counterpart
combo treatments (TB,
leprosy); Also inhibits many G+
and G- bacteria; Prophylaxis of
meningococcal and H.
influenzae meningitis
generally well-tolerated,
minor hepatotoxicity, usually
in patients with prior liver
problems
induces P450 enzymes;
increases metabolism of
drugs processed by P450
enzymes
Isoniazid inhibits mycolic acid (FA)
synthesis, a unique component
of mycobacterial cell walls
Used alone for prophylaxis, in
combo to treat TB
Bactericidal for growing forms
Bacteriostatic for resting forms
hepatotoxicity, peripheral
neuritis can offset with
pyridoxine (vit B6), rash,
convulsions in patients prone
to seizure
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Amphotericin B binds ergosterol and forms pores
on the membrane
most systemic fungal infections,
some protozoa
amphoterrible,
fever and chill (shake and
bake), hypotension,
nausea,nephrotoxicity(80%)
caution with other
nephrotoxic drugs,
arrhythmias
caution in use: renal
impairment
Terbinafine interfere with ergosterolsynthesis (inhibit SQUALENE
EPOXIDASE) accumulate toxic
squalene compromise integrity
of membrane
dermatophytes nail fungus(onychomycosis), jock itch (T.
cruris), athletes foot (T. pedis)
generally well tolerated,avoid if pregnant/nursing or
if liver/kidneys impaired
Itraconazole interfere with ergosterol
synthesis, inhibits Lanosterol -
14- Demetylase, a cytochrome
P450 enzyme
Broad spectrum avoid azoles in pregnancy
Griseofulvin binds microtubules- mitosis
inhibitor (causes multinucleated
cells)
restricted to dermatophyes
(skin, hair and nail infections),
alternate treatment for
onychomycosis (nail),
ringworm caused by
Microsporum, Epidermophyton
Generally well tolerated;
headaches other CNS effects,
photosensitivity and rash
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Sulfadiazine +
Pyrimethamine
DHPS & DHFR inhibitor, resp.;
blocks production of THFA
Toxoplasma, antimalarial,
antibacterial
allergies to sulfa,
pyrimethamine toxicity (bone
marrow suppression), does
not alleviate encysted formMebendazole Inhibits microtubule
polymerization/mitotic spindle
poison; bind worm -tubulin
with higher affinity than
mammalian orthologue
nematodes/roundworms Generally well tolerated
Ivermectin kills larvae in host not effective
against adult worm; induces
paralysis via glutamate gated Cl-
channels found only ininvertebrates
broad spectrum antiparasitic;
nematode, esp. for filariae
causing onchocerciasis (river
blindness)
Can effect mammalian GABA
receptor so contraindicate
when Blood Brain Barrier
is impaired
Praziquantel causes spastic paralysis and
tegument damage
flatworms and cestodes generally well tolerated, GI
distress, CNS effects
Contraindications:ocular
cysticercosis (tapeworm
larvae in eye) as host
response to dead worm
damages eye;
ophthalmologic surgery is
recommended instead
inducers of CYP reduce
bioavailability of drug
Insulin Type 1 DM; IDDM Hypoglycemia;
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impaired neurologic function.
inability to concentrate.
slurred speech, lack of
coordination, staggering
symptoms are often
mistaken as alcohol
intoxication
Glipizide increasing endogenous insulin
secretion;ATP binds to KIR and
blocks the channel
ADP binds to SUR and
activates the channelSUR enhances sensitivity of
KIR to ATP and interacts with
sulfonylureas and
meglitinides
Type 2, NIDDM
Oxidized to inactive metabolites
Half-life - 2 to 4 hours
Potency - High (2.5 to 40
mg/day)
hypoglycemia
Glyburide increasing endogenous insulin
secretion ;ATP binds to KIR
and blocks the channel
ADP binds to SUR and
activates the channel
SUR enhances sensitivity of
KIR to ATP and interacts with
sulfonylureas and
meglitinides
Type 2, NIDDM
Oxidized to weakly active
metabolites
Half-life - 6 hours
Duration of action - 24 hours
Potency - High (1.25 to 20
mg/day)
hypoglycemia
Repaglinide Decrease ATP sensitive K+ Tyoe 2, NIDDM Effect is rapid and brief so
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channel conductance
Act similarly too sulfonylureas
but bind to distinctly different
region of SUR1
reduced risk of long-lasting
hypoglycemia
Metformin Insulin sensitizers;
antihyperglycemics; Correct
elevated hepatic glucose
output
Inhibit hepatic gluconeogenesis
Inhibit glucose-6-phosphatase
activity inhibit glycogenolysis activity of insulin receptors
insulin resistance
Appropriate for obese type 2
diabetics
Doesnt produce lactic
acidosis or hypoglycemia;
Secondarily Reduced
triglycerides, total
cholesterol, LDL
Increased HDL
Weight loss, some reduction
of blood pressurePioglitazone are agonists of -(PPAR)
activation of PPAR alters therate of expression of a number of
genes encoding proteins
involved in regulating lipid and
glucose metabolism, ultimately
increasing sensitivity to
insulin at the target tissues
DM Reduce hepatic glucose
output
Does not increase insulin
secretion
Does not induce weight gain
Acarbose competitive and reversible
inhibitors of a-glucosidase in
the small intestine
Delay carbohydrate digestion
and absorption
Smaller rise in postprandial
glucose
For mild to moderate fasting
hyperglycemia with significant
postprandial hyperglycemia
Gastrointestinal disturbances
Flatulence
Nausea
Diarrhea
Contraindicated for
inflammatory and
obstructive bowel
disease, colonic ulcers
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Diazoxide opens the KATP channel and
inhibits insulin release
Oral agent for hypoglycemia
of various causes, including
insulinomas
Levothyroxine Synthetic T4 hormone Hypothyroidism Rare but excessive dose
produce symptoms of
hyperthyroidism
Propylthiouracil compete with thyroglobulin for
oxidized iodide in the process of
organification and coupling
inhibits T4/T3 conversion
Hyperthyroidism
Propylthiouracil inhibits both
thyroid peroxidase and T4/T3
conversion
Methimazole compete with thyroglobulin for
oxidized iodide in the process oforganification and coupling
Hyperthyroidism
methimazole inhibits only
thyroid peroxidase; more
potent than propylthiouracil
Radioactive iodide results in selective destruction of
thyroid gland
hypothyroidism
Stable Iodide high levels of iodide inhibit
thyroid hormone synthesis and
release (Wolff-Chaikoff effect)Hyperthyroidism
used to block thyroid function
in radiation emergencies
hypothyroidism
Propanolol inhibit peripheral T4/T3
conversion by 5-deiodinase
Hyperthyroidism
Inihibit peripheral thyroid
metabolism
Alendronate inhibit mevalonate pathway in Pagets disease and not to be used in the presence
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osteoclasts, posttranslational
modification
slow or block bone resorption,thus, help to lower serum
calcium levels
postmenopausal osteoporosis
in women
of hypocalcemia, during
pregnancy or lactation, or
with a history of any allergy
to bisphosphonates
should not be given to anyone
who is unable to remain
upright for 30 min after
taking the drug, then to have
a meal serious esophageal
erosion can occur!
Calcitonin binds directly to receptors on
osteoclasts and inhibits bone
resorption;
Antihypercalcemic salmon calcitonin should not
be used with known allergies
to salmon or fish products
caution should be used in
patients with renal
dysfunction could be
exacerbated
flushing of the face and
hands, skin rash, nausea and
vomiting,
urinary frequency, localinflammation at the site of
injection
Calcitrol Increases absorption of dietary
calcium in small intestines
Vit D compound
reatment of
hypoparathyroidism and in
patients undergoing chronic
renal dialysis
should not be used in the
presence of any known
allergy to vitamin D,
hypercalcemia, vitamin D
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mineral resorption in bone, and
re-absorption of calcium and
phosphate from renal tubules
inhibit PTH synthesis and
release
with PTH and calcitonin regulate
calcium homeostasis
toxicity
metallic taste, nausea,
vomiting, dry mouth,constipation, and anorexia
CNS effects: weakness,
headache, somnolence,
irritability
Calcium gluconate a therapy for hypocalcemic
states associated with disorders
such as vitamin D-dependentrickets and
hypoparathyroidism
less venous irritation than
calcium chloride
Parathyroid Hormone increase in bone formation
occurs because PTH acutely
promotes osteoblast
development and stimulates
osteoblast activity
stimulates production of active
vitamin D in the kidney
once-daily subcutaneous
administration of PTH favors
bone anabolism
cannot be taken orally, only
subcutaneously or IV
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Methotrexate Inhibition of dihydrofolate
reductase (DHFR) which leads to
depletion of cofactors required
for synthesis of thymidylate andpurines
ALL in children,
choriocarcinoma, combo
therapy for breast carcinomas,
head and neck, ovary andbladder high dose used for
adjuvant therapy
Also for psoriasis, rheumatoid
arthritis, immunosuppressive
agent
With standard dose
myelosuppression, stomatitis,
enteritis
High dose have conjunctivitis,
renal failure neurotoxicity
and rarely hepatic failure
6-Metacaptopurine Function as analog of natural
purine and inhibit de novo
purine synthesis and become
incorporated into nucleic acids
Myelosuppression, gi and
hepatic toxicity
5-Fluorouracil Inhibition of thymidylate
synthase, reduced production of
TTP increase incorporation of
dUTP into DNA
Potent radiosensitizer
Intense dense and combo
with leucovorin associated
with significant gi toxicity,
myelosuppression
Skin pigmentation and rashes
are common
Rarely cerebellar toxicity
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Gemcitabine Inhibition of ribonucleotide
reductase; inhibit incorporation
of dCTP into DNA by DNA pol
IV administration only Same toxicities as the class
and elevation in liver
transaminases
Potent radiosensitizer, not to
be used with radiotherapy
Vinblastine Bind to tubulin at site that
overlaps with GTP binding
domain and prevents extension
of MTs; chromsomes dont
segregate during mitosis
Lymphomas and second line
therapy for various solid
tumors
Neutropenia; gi side effects
Paclitaxel Bind to beta tubulin at site
distinct from vincas or colchine;
promote polymerization and
prevent depolymerization
arresting cell in mitosis
Treatment of many solid
tumors breats, ovarian and
lung
Peripheral neuropathy,
myalgias, myelosupression
Acute hypersensitivity rxns
occur possibly die to vector
Docetaxel Same as above, arrests cell in
mitosis
Improves survival in men with
metastatic prostate cancer by
2.4 months
Peripheral neuropathy,
myalgias, myelosupression
Cabazitaxel Same as above, arrests cell in
mitosis
Improves survival in men with
metastatic prostate cancer by
4.3 months
Peripheral neuropathy,
myalgias, myelosupression
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Colchine Bind MTs at interface btw alpha
and beta tubulins, and
destabilize
First used as anti-
inflammatory/immune
Used in association withallopurinol for gout
Immune deficiency, diarrhea
Cyclophosphamide Alkalating agent; alkylates DNA
twice inducing crosslinks in the
DNA
Metabolite acrolein, can
cause severe cystitis, fancoli
like syndrome in kidneys
CNS: confusion, drowsiness,
hallucinations
Temozolomide Standard of care for
glioblastomas; lipid soluble candiffuse across BBB
Myelosuppression
TMZ+ O6- Benzyl
Gaunadine
Binds DNA repair and
potentiates effects of other
chemotherapy agenst that
damage DNA
Doxorubicin Intercalate into GC rich regions
of DNA, depress DNA,RNA and
protein synthesis
May metabolize and form free
radicals
Activate apoptosis signaling
pathway
Myelosuppression, alopecia,
GI disturbances, cardiac
toxicity is marked
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Cisplatin Functional groups replaced by
water which is replaced by DNA
base usually G and crosslinking
occurs
Nephrotoxicity common,
highly emetogenic, marked
peripheral neuropathy,
anemiaCarboplatin Functional groups replaced by
water which is replaced by DNA
base usually G and crosslinking
occurs
Nephrotoxicity only in high
doses, mildly emetogenic,
rarely have peripheral
neuropathy,
myelosuppression
Etoposide Cause DNA strand breaks by
trapping and stabilizing top II
Tamoxifen Blocks estrogen receptor Breast cancer
Degaralix Blocks GnRH Breast cancer
Imatinib Philadelphia chromosome CML
Trastuzumab Interferes withHER2/neureceptor
Breast cancer
http://en.wikipedia.org/wiki/HER2/neuhttp://en.wikipedia.org/wiki/HER2/neuhttp://en.wikipedia.org/wiki/Receptor_(biochemistry)http://en.wikipedia.org/wiki/Receptor_(biochemistry)http://en.wikipedia.org/wiki/HER2/neu -
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Tocilizumab IL-6 receptor antagonist
(cytokineinvolved in thedevelopment of immunological
and inflammatory reactions)
Bevacizumab antibody that blocks vascular
endothelial growth factor A
(VEGF-A) which prevents the
establishment of blood supply
and metastatic spread.
RCC, lung cancer, colon cancer
to slow growth and inhibit
spread
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Clomiphene Anti-estrogen , blocks estrogen
inhibition of FSH and LHrelease
Used to treat ovarian failure Possibility for
overstimulation multiplepregnancies
Menotropins/ Urofillitropin Produces follicular stimulation
hCG Mimics LH, After priming with
menotropins for 14 days
give hCG to induce follicle
ovulation
Danazol Synthetic androgen used to
inhibit the output of FSH/LH,
removing hormonal
stimulation
Treatment for
endometriosis
Any sex steroid caninhibit FSH/LH in either
sex
Facial hair, lose hair, and
slight virilization
GnRH Stimuates the release of
LH/FSH
Must administer in a
pulsatile pattern
estradiol Endogenous First pass effect so not
effective orally
Estrone Major endogenous estrogen in
humans
Conjugated estrogens Equillan
Premarin
Purified mixtures of
conjugated steroids with
estrogenic properties
Ethinyl estradiol Slower; orally available
Mestranol Orally effective prodrug;
quickly demethylated to
ethinyl estradiol
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Progesterone Progesterone analogs Progestational activity
medroxyprogesterone Progesterone analogs Progestational activity
Slow release form f injectedprogesterone, once injected
slowly ansorbed into
circulation, once n
circulation they are rapidly
transformed and cleared
aaw
Norethindrone Progestational and androgenic
activity
Drosperinone Anti-androgemic activity and
anti mineralcorticoid activity,
available in combo type oral
contraceptives
Norgesetrel, levonogestrel Progestational and androgenic
activity
Mifepristone RU- 486 abortion pill