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108 terms

Pharmacology to KNOW (Week 5 for Week 6)

Antifungal, Antimalarial/Protozoal/Hemlmintic, Dermatologic, Antiinflammatory/Antigout, Immunosuppressants, Immunizing Drugs, Cancer/Oncologic
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Methotrexate
Anti-metabolite drug

Imitates dihydrofolate (DHF or FH2)

Used in standard breast cancer chemotherapy cocktail, CMF

Blocks dihydrofolate reductase (enzyme in thymidine synthesis, resulting in inhibition of deoxyribonucleotide synthesis)

Will also (minor effect) block purine synthesis
Leucovorin
Anti-metabolite drug

Imitates tetrahydrofolate (THF of FH4); blocks dihydrofolate reductase

Antidote to methotrexate toxicity, but at excess it facilitates 5-FU's action; used with 5-FU and irinotecan in colon cancer (FOLFIRI)
Gemcitabine
Imitates cytidine in pyrimadine synthesis

Blocks thymidylate synthetase, resulting in inhibition of deoxyribonucleotide synthesis
Cyclophosphamide
Used in standard breast cancer chemotherapy cocktail, CMF

Alkylating, DNA cross-linking agent

Prodrug, can be given orally, activated by CYP450

Results in thrombocytopenia and leukopenia, so is also used for leukemia.
Busulfan
Alkylating, DNA cross-linking agent
Mechlorethamine (aka nitrogen mustard, mustargen)
Alkylating, DNA cross-linking agent

Results in thrombocytopenia and leukopenia, so is also used for leukemia

M in MOPP (O=oncovorin, P=procarbazin, P=prednisone) for Hodgkin's
Nitrosourea (NU)
Alkylating, DNA cross-linking agent
Cisplatin
DNA cross-linking agent

Has platinum in structure

Different body distribution from cyclophosphamide (ovarian, lung cancers)

Additional side effect = renal insufficiency
Carboplatin and derivatives
DNA cross-linking agent

Has platinum in structure

Different body distribution from cyclophosphamide (ovarian, lung cancers)

Additional side effect = renal insufficiency
Vincristine (aka oncovorin)
From rosy periwinkle (Vinca rosea)

Inhibits mitotic spindles by inhibiting microtubule formation

Additional dose-dependent side effect = peripheral neuropathy

Used in Hodgkin's (MOPP)
Vinblastine
From rosy periwinkle (Vinca rosea)

Inhibits mitotic spindles by inhibiting microtubule formation

Additional dose-dependent side effect = peripheral neuropathy
Paclitaxel
From pacific yew tree (Taxus brevifolia)

Inhibits mitotic spindles by inhibiting microtubule breakdown into tubulin monomers

Additional dose-dependent side effect = peripheral neuropathy
Bevacizumab
Anti VEGF (soluble vascular endothelial growth factor)

Turned out to be a disappointment because did not decrease recurrence of tumors

Used in macular degeneration

Adverse side effect: HTN
Cetuximab
Anti EGFR (aka HER1)

Used for colorectal cancer in addition to FOLFIRI

Only use on tumors with wild-type KRAS (doesn't work if constitutively active, so patient gets side effects without treatment)

Side effects: skin reactions, infusion related reactions, rash, dermatitis acneiform, diarrhea
Panitumumab
Anti EGFR (aka HER1)

Used for colorectal cancer

Not used very often (IgG2, thus less complement binding and less ADCC)
Trastuzumab
Anti HER2 (aka erbB2)

Used in breast cancer

Cardiac side effects
Rituximab
Anti CD20 (expressed on B cells)

Used for B cell lymphomas in addition to CHOP (cyclophosphamide, hydroxydaunorubicin, oncovorin, prednisone)
Gefitinib
EGF-R kinase small molecule inhibitor

Used in lung cancers

Resistant if T790M mutation in EGF-R kinase exists

Adverse side effect: Skin toxicity
Erlotinib
EGF-R kinase small molecule inhibitor

Used in lung cancers

Resistant if T790M mutation in EGF-R kinase exists

Adverse side effect: Skin toxicity
Lapatinib
HER-2 kinase small molecule inhibitor
Imatinib (Gleevec)
abl small molecule inhibitor (also kit and PDGF-R)

Used in CML

Resistance is quick because leukemic cells replicate very quickly
Sorafenib
Mainly VEGF-R small molecule inhibitor (also kit and PDGF-R)

Low specificity (affects many kinases)
Sunitinib
Mainly VEGF-R small molecule inhibitor (also kit and PDGF-R)

Low specificity (affects many kinases)
Bortezomib
Reversible inhibitor of proteasome

Causes tumor cells to undergo apoptosis

Used in multiple myeloma

Expected high toxicity in patients (because proteosome is ubiquitous), but turned out OK (mild effects: GI, sensorineural, neutropenia)
General side effects
Bone Marrow: leukopenia, lymphocytopenia, thrombocytopenia, some anemia,
immunosuppression, and potentially leukemia

GI Tract: ulceration, mucositis, diarrhea, vomiting

Hair Follicles: alopecia

Gonads: premature menopause, reduced spermatogenesis

Wound healing is impaired

Fetal teratogenesis

Injection site reactions and tissue damage
carisoprodol

Muscle Relaxant
Soma
cyclobenzaprine

Muscle Relaxant
Flexeril
methocarbamol

Muscle Relaxant
Robaxin
dantrolene

Muscle Relaxant
Dantrium
adalimumab

NSAID
Humira
indomethacin

NSAID
Indocin
diclofenac-misoprostol

NSAID
Arthrotec
ibuprofen

NSAID
Motrin
Ketorolac

NSAID
Toradol
etodolac

NSAID
Lodine
meloxicam

NSAID
Mobic
Naproxen

NSAID
Naprosyn
piroxicam

NSAID
Feldene
celecoxib

(cox-2) NSAID
Celebrex
Colchicine

Gouty Agent
Colchicine
allopurinol

Gouty Agent
Zyloprim
What are the primary indications for immunosuppresants
1. Prevention of organ rejection in transplant clients
2. Treatment of autoimmune disorders (eg rheumatoid arthritis, SLE, MS)
What are the primary concerns with immunosuppressants
1. increased risk of infection
2. increased risk of neoplasms
What effect can immunosuppressants have on vaccines
reduce their effectiveness
What are the special considerations for administration of immunosuppressants
1. Don't take on an empty stomach to avoid GI upset
2. Don't mix oral solutions in a styrofoam cup because meds can adhere to sides
What special instructions should be given to female patients receiving immunosuppressants
Use contraceptive during treatment and for up to 12 weeks after therapy ends
Name 5 immunosuppressants
1. cyclosporine
2. azathioprine (Imuran)
3. mycophenolate mofetil (Cell Cept)
4. glatiramer acetate (Copaxone)
5. muromonab-Cd3 (Orthoclone OKT3)
What is an allogenic transplant
A transplant between genetically nonidentical individuals of the same species
What is the drug of coice for preventing organ rejection following allogenic transplantation
cyclosporine
What drug is often given in conjuction with cyclsporines and why
glucocorticoids because they are also immunosuppressants so you are doubling up
What is a very common concern with cyclosporines? How can you monitor for it? What can you do if it happens?
1. nephrotoxicity
2. Monitor BUN & creatnine levels
3. it is usually reversible following dosage reduction
How is cyclosporine administered
oral or IV
Why should a patient starting cycloesporine have a baseline oral assessment performed
it can cause gingival hyperplasia
What effect can grapefruit juice have on cyclosporine
It can inhibit metabolism of cyclosporine and which will raise the serum levels and increase the risk of toxicity
2 types of vaccine
killed organism or live, but attenuated
both of these are needed if bitten by animal w. rabies
vaccination and immunization
vaccination is
administer both vaccine/toxoid to elicit antibody response
immunization is
provision of both active/ passive immunity
contraindications of live virus vaccine
immunosupressed and pregnant women
you can not get what from a shot?
influenza!!
ADRs from immunizations are
local reactions, mild fever
only potentially serious ADR of immunization is
acute encephalopathy
MMR( measles, mumps, rubella): is a
live viral vaccine of all 3
MMR is 97% effective and it's ADRs are
local soreness, redness, swelling/ rash, fever
DTaP(diptheria and tetanus) you give an
acellular vaccine (avoid whopping cough)
DTaP is 80-90% effective and it's ADRs are
local reactions, mild fever, and very rare (encephalopathy)
IPV(inactive poliovirus vaccine) 97% and ADRs are
devoid of serious ADRs
HIB(hemophilus influenza) prevents
meningitis, arthritis, pneumonia
HIB is 98% effective and ADRs
well tolerated, local reactions/fever
Varicella is also known as
chicken pox
Varicella is a live attenuated varicella virus that is 97% and ADRs are
local reaction, fever, rash
Hep B surface antigen 85% and ADRs
local reaction, fever
Hep B used in preggers what's neg vs pos?
if mother Hep B neg- newborn gets vaccine if mother Hep B pos- newborn gets vaccine and HBIG
Hep A is the inactive hep A virus 94-100% effective risk dependant on
risk factors, immunization so effective- worth getting, AZ is high risk
Hep A ADRs
mild local reaction, HA, anorexia, malaise
Pneumococcal conjugate vaccine causes
pediatric disease
Pneumococcal is 89% effective and ADRs
easily tolerated- mild local, fever
Meningococcal conjugate vaccine has an old product and a new product
menomune(not T cell dependant) and menactra(T cell dependant good memory)
Influenza inactive or live attentuated and it is
seasonal
Rotavirus vaccine most common cause of
diarrhea
Rotavirus vaccine had an early application that was discontinued because it caused
intussuception: intestine folds up inside itself
Rotavirus has 5 common
serotypes and produce IgA (mucosal surface)
Rotavirus has a new product that is a live vaccine called
Rotarix
Human papillomavirus vacine prevents
genital warts and cervical cancer
Human papillomavirus vacine include two drugs that both have virus-like particles but not live
gardasil and ceravix (not tested on preggers)
Cancer
The uncontrolled growth and spread of abnormal human cells
Leucovorin
Rescue therapy; Some protocols use massive amounts of chemotherapy to kill off cancer cells. This treatment is given over a short period followed by an antidote drug immediately thereafter to spare the normal cells.
Antimetabolites
Mimics a necessary nutrient or blocks a reaction, which synthesizes a necessary nutrient; ex. Fluorouracil (5-FU, Efudex) - gloves should be worn b/c an irratant to skin; Cytarabine (Ara-C, Cytosar); Thioguanine (6-TG, 6-Thioguanine
Alkylating Agents
used to treat leukemia, testicular and ovarian cancers, and bladder cancers; Bind to DNA (the genetic material of the cell) and prevent its relocation
Utilized to a greater extent in cancer cells; ex. Chlorambucil (Leukeran)
Cisplatin (Platinol)
Mechlorethamine (Nitrogen Mustard)
Hormones
To treat hormone dependent cancers such as breast cancer; blocks effect of estrogen in target tissues such as breast; Side Effects - hot flashes; ex. Leuprolide Acetate (Lupron); Medroxyprogesterone Acetate (Depo-Provera); Testolactone (Teslac)
Vinca Alkaloids
Vinblastine (Velban); Vincristine (Oncovin); Vinorelbine (Navelbine); Arrests mitotic division at the metaphase of cell division; side effects: bone marrow suppression, hari loss, vomiting
Asparaginase (Elspar)
Blocks asparagine dependent protein synthesis in tumor cells; side effects: vomiting, depression, bleeding, hypersensitivity, bone marrow sensitivity
Antibiotics
Inhibits nucleic acid synthesis; ex. Bleomycin (Blenoxane)
Doxorubicin (Adriamycin); Mitomycin (Mutamycin); side effects: Bleomycin - pulmonary fibrosis, fever, chills, nausea/vomiting; Doxorubicin - myelosuppression, cardiotoxicity, nausea/vomiting ; Mitomycin - bone marrow toxicity, nausea/vomiting
Chloroquine
inhibits heme polymerase activity leading to toxic bulidup of heme; kills malaria trophozoites in the RBCs only
Primaquine
kills liver schizonts of P. vivax and P. ovale
Quinine
inhibits heme polymerase activity leading to toxic buildup of heme; kills trophozoites in RBCs and gametocytes
Mefloquine
kills erythrocyte form of malaria only
Doxycycline
inhibits ribosome
pyrimethamine/sulfadoxine
inhibits synthesis of Tetrahydrofolate which is needed for pyrimidine synthesis
True/False: All of the antimalarials can be given in oral form
True
What side effect is common to antimalarials?
Gi upset
Which antimalarials are safe for all trimesters of pregnancy?
Chloroquine, pyrimethamine/sulfadoxine, quinine, quinidine
antifungal
amphotericin B ( Fungizone)
antifungal
fluconazole (Diflucan)
antifungal
nystatin (Mycostatin)
antigout
allopurinol (Zyloprim)
antigout
colchicine generic only
antigout
probenecid (Benemid)