Pharmacology Drugs Flashcards by Ricky r

Immunosuppressive: -most common DMARD

folate analog, inhibits dihydrofolate reductase
also anti-cancer since DNA synth inhibiting

Methotrexate

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This drug inhibits dihydroorotate dehydrogenase (DHODH) for treatment of R.A.

leflunomide

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Glucocorticoids are anti-inflammatory by inhibiting the enzyme ___________, which inhibits the release of arachidonic acid from the cell membrane and prevents formation of prostaglandins

phospholipase A2

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long term use of prednisone, a glucocorticoid, can lean to _______

osteoporosis
poor wound healing
hyperglycemia
many more…

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Used to treat R.A., this drug released in the 1990’s is thought to inhibit IL-1 & TNF-alpha release. It is ________

sulfasalazine

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The adverse affects of sulfasalazine include ________

neutropenia
rashes
nausea
vomiting
headaches

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This class of drugs: 1. Inhibits phospholipase A2, inhibiting release of arachidonic acid 
2. Inhibits cytokine production preventing induction of COX-2

glucocorticoids

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The most commonly used DMARD is _________

methotrexate

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methotrexate is a _______ analog

folate

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methotrexate inhibits reaction done by ________, an enzyme essential for DNA synthesis

Dihydrofolate reducatase (DHFR)

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This drug is a pyrimidine synthesis inhibitor for the treatment of R.A.

leflunomide

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This class of drugs modifies the effectiveness of pro-inflammatory cytokines generated in R.A.

biological response modifers

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biological response modifers for R.A. are often called ________

Biologic DMARDs

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What does DMARD stand for?

disease modifying anti-rheumatic drug

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A joint replacement surgery is known as a ________

arthroplasty

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These 5 TNF-α antagonists works by binding to TNF-α to prevent it from binding of it’s receptor

Adalimumab
Etanercept
Infliximab
Golimumab
Certolizumab

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Etanercept is administered by twice weekly _____ ______

Subcutaneous injections

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This R.A. drug is a monoclonal chimeric IgG1 antibody against TNF-α (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)

Infliximab

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Which TNF-α antagonist goes by the trade name humira? (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)

Adalimumab

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adalimumab is more convenient than Etanercept because dosing is _______ rather than _______

adalimumab is twice monthly injection rather than twice weekly

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a human monoclonal antibody that binds to membrane soluble TNF-α

Golimumab

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Golimumab is a monoclonal antibody that binds _____

membrane soluble TNF-α

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This TNF-α antagonist carries the risk of serious infections compared to the others including TB and fungal (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)

golimumab

golem’s misshapen form of TB and fungal infections

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how is certulizumab different from gloimumab and adalimumab?

it was conjugated to PEG to delay its elimination

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Which TNF-α antagonist is a chimeric mouse/human hybrid? (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)

infliximab | inflix is a mix

Which TNF-α antagonist is a fully human monoclonal antibody?(Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)

adalimumab | adam was the first human

Which TNF-α antagonist binds to membrane bound soluble TNF-α? (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)

Golimumab | golem creeps along the sides

Which TNF-α antagonist is a humanized antibody bound to PEG to delay metabolism and elimination? (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)

Certolizumab

R.A. treatment: A soluble recombinant human IL-1 receptor antagonist that requires frequent dosing (anakinra/tocilizumab)

anakinra

R.A. treatment: An IL-6 receptor antagonist sold as Actermra (anakinra/tocilizumab)

tocilizumab

This cytokine antagonist carries a risk of infection with TB, fungi, viral and others (anakinra/tocilizumab)

tocilizumab

Name 2 other cytokine agonists for treatment o R.A. hint: interfere with IL-6 and IL-1

anakinra and tocilizumab

Name 2 Co-stimulatory modulators that effect lymphocytes for treatment of R.A.

Atabatacept (t-cells) | Rituximab (b-cells)

This co-stimulatory modulator inhibits t-cell activation and promotes t-cells apoptosis (Atabatacept/Rituximan)

Atabatacept

This co-stimulatory modulator for R.A. has the side effects of 1. headaches and 2. infections (Atabatacept/Rituximan)

Atabatacept

This co-stimulatory modulator for R.A. side effects of 1. infections and 2. hypersensitivity reactions (Atabatacept/Rituximab)

Rituximab

This Co-stimulatory modulator for R.A. is an anti-CD-20 mAb that reduces circulating B-cells (Atabatacept/Rituximab)

Rituximab

This R.A. drug inhibits production of inflammatory mediators by blocking the JAK kinase pathway

Tofacitinib

What type of drug is Tofacitinib?

a signaling pathway inhibitor

What Dz does Tofacitinib treat?

R.A.

Gout is caused by the crystallization of _____ _____ within the joints

uric acid

this dz is sometimes called 'crystal arthritis'

gout

The uric acid crystals that cause gout are a result of ________ metabolism

purine

Two methods to reduce uric acid load:

1. prevent production | 2. increase excretion

what is podagra?

gout in the big toe

What is colchicine used to treat?

acute gouty arthritis

This drug blocks tubulin and prevents leukocyte migrations, phagocytosis and activity

Colchicine

Long term use of colchicine can cause ______ and _______

peripheral neuropathy and neutropenia

Pain relief for acute gouty arthritis can include (3)

1. Colchicine 2. NSAIDs 3. Corticosteroids

Indomethacin and Naproxen are both _______

non-selective NSAIDs

Indomethacin and Naproxen can both cause damage to the GI tract in the form of

gastric and duodenal ulcers

Compete with urate at the anionic transport site of the renal tubule and inhibit urate reabsorption (probenecid/ allopurinol/ febuxostat/ pegloticase)

probenecid

Reduces uric acid synthesis by inhibiting xanthine oxidase (probenecid/ allopurinol/ febuxostat/ pegloticase)

allopurinol

probenecid/ allopurinol/ febuxostat/ pegloticase | what do all these drug treat?

chronic tophaceous gout

a deposit of uric acid crystals is called a _______

Tophus

Which can cause a maculopapular rash (probenecid/ allopurinol/ febuxostat/ pegloticase)

allopurinol

Non-purine, non-competitive antagonist of xanthine oxidase | probenecid/ allopurinol/ febuxostat/ pegloticase

febuxostat

Converts uric acid to allantoin (probenecid/ allopurinol/ febuxostat/ pegloticase)

pegloticase (bound to PEG)

Allopurinol is metabolized to alloxanthine. allopurinol is a competitive inhibitor while alloxanthine is a non-competitive inhibitor of _______ _______

xanthine oxidase

Dx: acute gout attack Hx: No complications Rx: ?

1. NSAIDs | 2. possible corticosteriods injected IA

Dx: acute gout attack Hx: renal insufficiency Rx: ?

systemic corticosteroids

Dx: acute gout attack Hx: peptic ulcer risk Rx: ?

colchicine

Dx: Chronic tophaceous gout w/ uric acid stones Hx: renal insufficiency Rx: ?

1. start allopurinol | 2. consider febuxostat is CrCl is greater than 30mL/min

Dx: Chronic tophaceous gout Hx: no complications Rx: ?

1. allopurinol or if not tolerated, | 2. febuxostat

what are the natural endogenous estrogens called?

E1: Estrone E2: Estradiol E3: Estriol

What is the primary source of estrogen in pre-menopausal women? which estrogen is it?

the ovary | E2: estradiol

What is the major estrogen in postmenopausal women?

E1: Estrone

Aromatase converts testosterone to _______ and androstenedione to ______

testosterone to estradiol | androstenedione to estrone

estrogen circulating in the body is bound to _______

sex hormone binding globulin (SHBG) | and albumin weakly

Diethylstilbestrol (DES) is not used due to the increased risk of ________

adenocarcinoma of the vagina and cervix

synth estrogens estradiol valerate and estradiol cypoinate are (estradiol esters/ conjugated estrogens/ alkyl estrogens)

estradiol esters

synth estrogens estrone sulfate and equilin sulfate are (estradiol esters/ conjugated estrogens/ alkyl estrogens)

conjugated estrogens

synth estrogens ethinyl estradiol and mestranol are (estradiol esters/ conjugated estrogens/ alkyl estrogens)

alkyl estrogens

HRT (increases/decreases) risk of cardio dz, stroke and dvt

increases

2 non-steroidal anti-estrogens are:

1. clomiphene | 2. tamoxiphene

Tamoxiphen has an anti estrogenic effect on the ______ and a pro-estrogenic effect on the _______

anti to the breast | pro to the uterine endometrium and bone

Tamoxiphen binds to the _______ receptor

estrogen receptor (ER)

tamoxiphene has a (low/high) binding affinity

low, a high dose has to be used

clomiphen induces ovulation by binding the estrogen receptor in the _________

hypothalamus (inhibiting negative feedback leading to secretion of gonadotropins and LH)

Name the synthetic progesterones (4)

1. medroxyprogesterone 2. norethindrone 3. norgestrel 4. megestrol

The pharm name for "plan B" is _________

Levonorgestrel

Levonorgestrel's effect is to ________

prevent implantation

Levonorgestrel is most similar to the endogenous hormone _________

progesterone

The pharm name for "the abortion pill" is _________

RU-486 or mifepristone

mifepristone can be taken up to ___ days after fertilization and still be effective

49 days (7 weeks)

The pharm name for viagra is _________

Sildenafil citrate

The pharm name for levitra is ________

Vardenalfil HCl

The pharm name for Cialis is ________

Tadalafil

Tadalafil, vardenafil and sildenafil citrate are all in the class of _______

PDE5 inhibitors

Which has the longer half-life (tadalafil/ vardenafil/ sildenafil)

tadalafil (cialis)

What does APC stand for in colon cancer?

Adenomatous polyposis coli

two competing theories of tumor genesis are:

1. Clonal Evolution | 2. Cancer Stem cells

what do cyclin-CDK complexes do to their targets?

phosphorylate them (kinase)

Cdk2-cyclin A functions in (G1/ S/ G2+M) phase

Cdk1-cyclin B functions in (G1/ S/ G2+M) phase

G2+M

which cyclin-Cdk complexes can phosphorylate Rb? (3)

cyc E cdk 2 cyc D cdk 4 cyc D cdk 6 (E2, D4, D6)

hyperphosphorylation of Rb causes the release of _____

E2F

E2F activates the transcription of genes whose products control progression from ___ to ___ phase

G1 to S phase

Rb releases E2F when it becomes __________ by cyclin-Cdk complexes: E2, D4, D6

hyperphosphoryalted

These are cystine proteases that are activated in response to apoptotic insults such as cancer drugs: ______

Capsases

This is released into the cytosol from the mitochondria during apoptosis: _________

Cytochrome C

Anticancer drug resistance due to dysregulation of the apoptosis promoting genes due to mutations is known as (intrinsic/acquired) resistance

intrinsic

Anticancer Drug resistance due to dysregulation of one or both apoptotic pathways during chemotherapy is (intrinsic/acquired) resistance

acquired resistance (the key is during chemo)

the ABVD drugs are

Doxorubicin (adriamycin) bleomycin vinblastine dacarbazine

the CHOP drugs are

Cyclophosphamide hydroxydoxorubacin Vincristine (Oncovine) Prednisone

the MOPP drugs are

Mechlorethamine Vincristine (oncovine) Procarbazine Prednisone

the CMF drugs are

Cyclophosphamine Methotrexate 5-fluorouracil

the FEC drugs are

5-fluorouracil Epirubicin Cyclophosphamide

What kind of drugs are anakinra and tocilizumab?

cytokine antagonsits for IL-6 and IL-1, a type of biological response modifiers

This class of anti-cancer drugs transfers alkyl groups to DNA

alkylating agents

This alkylating agent is part of the MOPP treatment and is good for hodgkin's lymphoma, ALL, choroicarcinoma, Burkitt and T-cell lymphoma (methotrexate/mechlorethamine)

mechclorethamine

These two alkylating agents are given as pro-drugs and are activated by a liver p450 (mechlorethamine/ cyclophosphamide/ Ifosfamide)

cyclophosphamide and Ifosphamide

this nitrogen mustard is better for sarcoma and testicular cancer (cyclophosphamide/ Ifosphamide)

Ifosamide

this nitrogen mustard is the most widely used and is best for ALL, CLL, non-hodgkin's, breast lung and ovarian cancers (cyclophosphamide/ Ifosphamide)

cyclophosphamide

These two alkylating agents lead to hemorragic cysts and bladder irritation due to the acrolein metabolite (mechlorethamine/ cyclophosphamide/ Ifosfamide)

cyclophosphamide and Ifosphamide

The alkylating agents that are nitrosoureas are (Carmustine + Lomustine/ Dacarbazine + Procarbazine)

Carmustine and Lomustine

Carmustine and Lomustine are good for treating (hodgkin's/ brain tumors/ ovarian cancer)

brain tumors

These drugs are soluble across the BBB (nitrosoureas /platinum analogs/ triazenes)

nitrosoureas | Carmustine and Lomustine

Pick the 3 Triazenes (Dacarbazine/ procarbazine/ ifosamide/ cyclophaphamide/ temozolomide)

dacarbazine procarbazine temozolomide

Since the nitrosoureas Carmustine and Lomustine have good solubilities, they can get into bones and have the side effect of __________

myelosupression

This triazene is part of the ABVD combination regiment (Doxorubicin/ dacarbazine/ procarbazine/ temozolomide)

dacarbazine | doxorubicin is adrimacin, an anthracycline

(dacarbazine/ temozolomide) is administered IV and (dacarbazine/ temozolomide) is administered orally

dacarbazine is IV | temozolomide is oral

this platinum analog is known for its renal toxicity (Cisplatin/ Carboplatin/ Oxaliplatin)

cisplatin

this platinum analog is known for its myelosuppression and thrombocytopenia (Cisplatin/ Carboplatin/ Oxaliplatin)

carboplatin

this platinum analog is known for its neutropenia and eripheral censory loss (Cisplatin/ Carboplatin/ Oxaliplatin)

oxaliplatin

The platinum analogs are (alkylating/ DNA intercalating) agents

alkylating

the platinum analogs are made cytotoxic by reacting with (p450/ water)

water

cyclophosphamide and Ifosphamide are made cytotoxic by reacting with (p450/ water)

p450

platinum analog best for testicular, ovarian, bladder and lung carcinomas (Cisplatin/ Carboplatin/ Oxaliplatin)

cisplatin

platinum analog best for ovarian cancer (Cisplatin/ Carboplatin/ Oxaliplatin)

carboplatin

platinum analog best for gastric and colorectal cancer (Cisplatin/ Carboplatin/ Oxaliplatin)

oxaliplatin

Methotrexate (can/ cannot) penetrate the CNS

cannot, administered intrathecally for meningeal leukemia

5-fluorouracil, cytarabine, gemcitabine are (pyrimidine/ purine) analog

pyrimidine

5-fluorouracil is converted to 5-FdUMP which inhibits _______ synthase

thymidylate synthase

This pyrimidine analog can give hand-foot syndrome with erythema and sensitivity (5-fluorouracil/ cytarabine/ gemcitabine)

5-fluorouracil

This pyrimidine analog is most effective for AML and CML (5-fluorouracil/ cytarabine/ gemcitabine)

cytarabine | cyta for CML and AML

This pyrimidine analog can be made into a topical cream for basal cell carcinoma and face peels (5-fluorouracil/ cytarabine/ gemcitabine)

5-fluorouracil | 5-fluoro for the face

Which is the best for solid tumors in the head, neck, esophagus, and non-small cell lung (5-fluorouracil/ cytarabine/ gemcitabine/ 6-mercaptopurine)

gemcitabine

Which is a pyrimidine analog of cytidine? | 5-fluorouracil/ cytarabine/ gemcitabine/ 6-mercaptopurine

cytarabine and gemcitabine

Which is S phase specific? (5-fluorouracil/ cytarabine/ gemcitabine/ 6-mercaptopurine)

All of them! | 5-fluorouracil/ cytarabine/ gemcitabine/ 6-mercaptopurine

This is our only purine analog (5-fluorouracil/ cytarabine/ gemcitabine/ 6-mercaptopurine)

6-mercaptopurine

This chemotheraputic prodrug must be metabolized by HGRPRT (5-fluorouracil/ cytarabine/ gemcitabine/ 6-mercaptopurine)

6-mercaptopurine

Used to maintain remission in acute ALL (5-fluorouracil/ cytarabine/ gemcitabine/ 6-mercaptopurine)

6-mercaptopurine

Dactinomycin, daunorubicin, doxorubicin, epirubicin, idarubicin are all (Base analogs/ intercalating agents/ antibiotics)

BOTH intercalating agents and antibiotics

Which act in the G2 phase of the cell cycle? (doxorubicin/ epirubicin/ idarubicin/ bleomycin)

bleomycin

What are our 2 microtubule formation inhibiting drugs?

1. Vinblastine | 2. Vincristine

Which is part of ABVD therapy (Vinblastine/ Vincristine)

Vinblastine

Which has dose limiting neurotoxicity (Vinblastine/ Vincristine)

Vincristine

What are our 2 microtubule degradation inhibiting drugs?

1. Paclitaxel | 2. Docetaxel

Vinca alkaloids prevent microtubule (polymerization/depolymerization) and Taxanes prevent microtubule (polymerization/depolymerization)

Vinca prevent polymerization | Taxanes prevent depolymerization

This enzyme works to relieve torsional strain on DNA stands

Topoisomerase

Etoposide and teniposide both inhibit (topoisomerase I/ topoisomerase II)

topoisomerase II

Tamoxifen is used for anti-________ therapy

Estrogen

use of tamoxifen increases the risk of ________

endometrial cancer | and thromboembolic events

What are SERDs?

selective estrogen downregulators

Name a SERD

Fluvestrant

Anastrozole, Letrozole and Exemestane all do the same thing. They are _________ inhibitors

aromatase inhibitors

Leuprolide and Goserelin both do the same thing, bind and block the _________ receptor

bind and block the GnRH receptor

If Leuprolide and Goserelin block the GnRH receptor, ____ and _____ wont be released

FSH and LH are not released

What are the two non-steriodal androgen-receptor blockers?

Leuprolide and Goserelin

Hydroxyurea inhibits the enzyme _______

ribonucleotide reductase

What drug can treat myeloproliferative neoplasms, polycythemia vera, essential thrombocytopenia and SICKLE CELL?

Hydroxyurea

These drugs induce terminal differentiation in malignant immature promyelocytes for treatment of APL

Retinoids

This drug can treat multiple myeloma but historically caused birth defects in children

Thalidomide

Imatinib, Gefitinib, Erlotinib are all in the class of ____ _____ _____

tyrosine kinase inhibitors

Arsenic trioxide can be used to treat relapse of ____ ________ _______

Acute promyelocystic anemia

Imatinib inhibits (Abl kinase /PDGFR/ c-kit/ EGFR)

Abl kinase, PDGFR and c-kit

Gefitinib and erlotinib inhibit (Abl kinase /PDGFR/ c-kit/ EGFR)

EGRF for NSCLC

What drug is a monoclonal antibody against HER2/neu for breast cancer treatment?

Trastuzumab (Herceptin)

Which id a monoclonal antibody against EGRF1 (ErbB1) for treatment of EGFR-positive colon cancer (Gefitinib/ Erlotinib/ Cetuximab)

Cetuximab

Which inhibits DHODH which is required for pyrimidine synth (methotrexate/leflunomide)

Leflunomide

This drug inhibits a renal ion transporter and increases excretion of uric acid

Probenecid

Doxorubicin and cisplatin work by activating the cell protein ______

p53

This drug binds the Bcl-Abl tyrosine kinase at the site where ATP normally binds. It is ________

Imatinib

Imatinib is metabolized by ________

cytochrome p450(3A4)

the BRAF mutation is characteristic of about 50% of this type of cancer: ______

melanomas

Generally, the best drug for a malignant melanoma without BRAF v600e/k is _______

dacarbazine | a triazine alkylating agent

Ipilimumab is used to treat (CML/ALL/Melanoma)

melanoma

Ipilimumab is an inhibitor of ______

CTLA-4

Which will absorb a drug faster? (IM/Sub Q)

IM, muscles are more vascular

The ErbB# family is has an equivalent name, _____. So ErbB2 is the same as ______

HER# | ErbB2 is HER2/neu

The 3 drugs for melanoma are:

Dabrafenib Vemurafenib Trametineb

This drug for melanoma inhibits Mitogen activated extracellular kinase (MEK) (Dabrafenib/ Vemurafenib/ Trametineb)

Trametinib

These two drugs treat NSCLC:

Erlotinib | Gefitinib

The CYP enzymes do (phase I/ phase II) reactions

phase I

codeine is converted to morphine by CYP____

CYP 2D6

clopidogrel is a prodrug and is activated by CYP___

2C19

Warfarin is metabolized for elimination by CYP___

2C9