Pharmacology Drugs Flashcards
Immunosuppressive: -most common DMARD
- folate analog, inhibits dihydrofolate reductase
- also anti-cancer since DNA synth inhibiting
Methotrexate
This drug inhibits dihydroorotate dehydrogenase (DHODH) for treatment of R.A.
leflunomide
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
long term use of prednisone, a glucocorticoid, can lean to _______
- osteoporosis
- poor wound healing
- hyperglycemia
many more…
Used to treat R.A., this drug released in the 1990’s is thought to inhibit IL-1 & TNF-alpha release. It is ________
sulfasalazine
The adverse affects of sulfasalazine include ________
- neutropenia
- rashes
- nausea
- vomiting
- headaches
This class of drugs: 1. Inhibits phospholipase A2, inhibiting release of arachidonic acid 2. Inhibits cytokine production preventing induction of COX-2
glucocorticoids
The most commonly used DMARD is _________
methotrexate
methotrexate is a _______ analog
folate
methotrexate inhibits reaction done by ________, an enzyme essential for DNA synthesis
Dihydrofolate reducatase (DHFR)
This drug is a pyrimidine synthesis inhibitor for the treatment of R.A.
leflunomide
This class of drugs modifies the effectiveness of pro-inflammatory cytokines generated in R.A.
biological response modifers
biological response modifers for R.A. are often called ________
Biologic DMARDs
What does DMARD stand for?
disease modifying anti-rheumatic drug
A joint replacement surgery is known as a ________
arthroplasty
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
Etanercept is administered by twice weekly _____ ______
Subcutaneous injections
This R.A. drug is a monoclonal chimeric IgG1 antibody against TNF-α (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)
Infliximab
Which TNF-α antagonist goes by the trade name humira? (Etanercept/ Infliximab/ Adalimumab/ Golimumab/ Certolizumab)
Adalimumab
adalimumab is more convenient than Etanercept because dosing is _______ rather than _______
adalimumab is twice monthly injection rather than twice weekly
a human monoclonal antibody that binds to membrane soluble TNF-α
Golimumab
Golimumab is a monoclonal antibody that binds _____
membrane soluble TNF-α
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
how is certulizumab different from gloimumab and adalimumab?
it was conjugated to PEG to delay its elimination
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:
- 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)
- Colchicine
- NSAIDs
- 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: ?
- 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: ?
- start allopurinol
2. consider febuxostat is CrCl is greater than 30mL/min
Dx: Chronic tophaceous gout
Hx: no complications
Rx: ?
- 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:
- clomiphene
2. tamoxiphene