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Renal Pharmacology Flashcards

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1
Q

Finasteride

A

An androgen receptor complex antagonist that is mostly used in benign prostatic hyperplasia to decrease the rate of growth
It’s actually a 5 alpha reductase inhibitor

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2
Q

Luteinizing hormone

A

Released by the pituitary in response to stimulation by GnRH to act on the testes to increase testosterone synthesis

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3
Q

Leuprolide/goserelin

A

GnRH agonists that have modifications that make them last longer and increase their affinity for synthetic agonists.
Given in intramuscular formulation
Agonists are effective in that after they are administered for 2-4 weeks, they down-regulate the GnRH receptors on the pituitary
However, still releasing LH during this timeframe so an AR-antagonist is administered during this time frame to stop “androgen flare”

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4
Q

Degarelix

A

GnRH antagonist with six amino acid substitutions which make it an antagonist; does not have androgen flare so do not need to use an AR-antagonist with it

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5
Q

Bicalutamide

A

Nonsteroidal androgen receptor antagonist that is preferred for use to block androgen flair in association with GnRH agonists

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6
Q

Nilutamide

A

Nonsteroidal androgen receptor antagonist that has the toxicity of alcohol intolerance and diminished ocular adaptation to darkness.
Slightly less diarrhea seen here with these patients in comparison with bicalutamide

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7
Q

Cyproterone

A

Steroidal androgen receptor antagonist
Has partial agonist activity at large doses so that it acts as a steroid agonist
Associated with liver toxicity

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8
Q

Sipuleucel-T

A

Used as an autologous cellular immunotherapy for treatment of asymptomatic/symptomatic metastatic and hormone-refractory prostate cancer
Use it early when you first see signs and symptoms

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9
Q

Cabazitaxel

A

Binds to and stabilizes tubulin so that the spindle does not depolarize to inhibit tumor cell proliferation
Leads to cell cycle arrest and growth stoppage
Used with prednisone

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10
Q

Docetaxel

A

Antagonizes microtubule spindle disassembly with toxicity of neutropenia and nephrotoxicity
Can cause an infusion reaction

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11
Q

Bacillus Calmette-Guerin

A

Attenuated live vaccine which causes a granuloma-like reaction in the bladder wall to damage and kill the cancel cells; also damages bladder wall but not that much

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12
Q

Mitomycin

A

Intravesicular agent that is not absorbed at all so effective ocally

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13
Q

Thiotepa

A

Activated by CYP450 to form an alkylator with DNA cross-links to lead to DNA damage
Causes immunosuppression and neurotoxic at high doses

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14
Q

Cisplatin

A

Chemo contraindicated in patients who have renal disease in combination with bladder cancer

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15
Q

Valrubicin

A

Synthetic analog of doxorubicin and used only for intravesicular reaction for BCG-resistant bladder cancer

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16
Q

Interleukin-2

A

Activates lymphocytes and can cause adverse effects like hypertension, arrythmias, peripheral edema, etc.
Only 15-40% effective and works to enhance the body’s anti tumor effects
Toxicities in relation to it activating cytotoxic lymphocytes which can cause other bad toxicities

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17
Q

Sunitinib

A

Oral inhibitor of ATP to intrinsic tyrosine kinase domain of VEGF-R2
Also inhibits other tyrosine kinases
Reduces proliferation and angiogenesis

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18
Q

Sorafenib

A

Oral inhibitor of VEGF tyrosine kinases within tumor cells to reduce proliferation and angiogenesis

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19
Q

Bevacuzimab

A

Humanized monoclonal antibody against VEGF that actually binds to the ligand to prevent it binding to the receptor
Commonly given with interferon alpha in renal cell carcinoma treatment

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20
Q

P13K

A

Pathway by which temsirolimus and everolimus inhibit through acting on the mTOR enzyme complex

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21
Q

mTORC1

A

Enzyme complex that temsirolimus and everolimus act on which is made up of mTOR and FKB12
These drugs bind to the FKB12 part of the enzyme complex
Enzyme normally phosphorylates S6 kinase and relieves inhibitory action of 4EBP to overall promote protein synthesis and metabolism

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22
Q

mTORC2

A

Mechanism of resistance to temsirolimus and everolimus - this enzyme complex can be used instead of mTORC1

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23
Q

Cefepime

A

Fourth-generation cephalosporin that is the best mechanism by which to treat extremely ill UTI patients

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24
Q

Levofloxacin

A

Fluoroquinolone that previously was front-line treatment for UTI’s and pyelonephritis
Recently resistance has developed, so utilize Bactrim more commonly instead
Given in IV format for complicated pyelo patients (nausea, vomiting, etc.) but can be given orally as well
Resistance can be overcome with high doses of the drug

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25
Aztreonam
Penicillin analog effective against pyelonephritis
26
Piperacillin-tazobactam
Tazobactam is a beta-lactamase inhibitor so this drug combination works synergistically with broad spectrum activity against gram positive and gram negative organisms
27
Imipenem
Very resistant to chromosomal beta-lactamases so a good drug option Broken down pretty quickly with toxicity of hypersensitivity
28
Aminoglycoside
Frontline treatment for urinary catheter associated UTI along with a fluoroquinolone or other cephalosporin
29
MOA of aminoglycoside
Bind at start codon during mRNA translation to inhibit mRNA binding When mRNA does bind, leads to misreading Blocks further translation of the transcript or allows for incorporation of incorrect amino acid
30
Amikacin
Aminoglycoside resistant to lots of enzyme inactivation steps so used pretty widely in hospital setting
31
Ototoxicity
Most damaging of the amino glycoside toxicities Usually from progressive damage to vestibular and cochlear sensory cells and is usually irreversible High-pitched tinnitus is usually the first sign associated with this toxicity
32
Renal toxicity
Aminoglycosides cause renal impairment in 26% of patients receiving them May manifest as just decreased GFR or could lead to severe ATN Most important result of renal toxicity is reduced excretion of the drug which can predispose to ototoxicity
33
Tigacycline
Overcomes tetracycline resistance mechanisms of efflux pumps but outdated preps can lead to Fanconi's Must be given intramuscular instead of IV
34
Dihydropteroate synthase
Enzymatic step that is inhibited via sulfamethoxazole in Bactrim What makes them so specific for bacteria because this step is not present in humans
35
Dihydrofolate reductase
Inhibition of this enzyme is from trimethoprim in bacterium prep
36
DNA gyrase
What is inhibited by quinolones/fluroquinolones in gram-negative bacteria
37
Topoisomerase IV
What is inhibited by quinolones/fluoroquinolones in gram-positive bacteria
38
Methenamine
Urinary antiseptic that is excreted unchanged in urine, but low urinary pH activates it to formaldehyde which can kill bacteria - most effective against E. coli Can be given as prophylaxis for UTI's
39
Nitrofurantoin
When given with macro crystals, able to be more available Low pH makes it more effective to give it a higher antimicrobial activity - BUT it is not activated by the low urinary pH. Instead it is just made better Effective against gram-positive enterococci and gram-negative E. coli
40
Praziquantel
Anti-protozoal that is effective against schistosoma and causes muscular contraction and paralysis at higher drug-levels
41
Metrifonate
Seocnd-line for S. haematobium infection and works by being activated to dichlorovoros which inhibits acetylcholinesterase in the worm
42
Mineralocorticoids
Can act at the mineralocorticoid receptor to increase amount of ENaC's and Na ATPase to increase Na levels Favors potassium excretion and elimination
43
Spironolactone
MR antagonist | Can have some action at androgen receptors so can induce gynecomastia, etc.
44
Fludrocortisone
used for aldosterone deficiency as it has a much higher sodium retaining potency than anti-inflammatory action at glucocorticoid receptor Very strong MR agonist
45
Eplerenone
MR antagonist other than spironolactone
46
11-beta HSD2
Enzyme that inactivates cortisol to cortisone which is an inactive form that cannot interact with MR or GR Aldosterone escapes inactivation by this enzyme Black licorice induces this enzyme so can induce hypertension in this way
47
Calcitriol
The only vitamin D analog that should be given in renal failure patients as it has been both 1-hydroxylated and 25-hydroxylated
48
Cinacalcet
Calcium sensor mimetic that mimics stimulatory effect of calcium on calcium-sensing receptor to inhibit PTH secretion by parathyroid glands Lowers the concentration of calcium at which PTH secretion is suppressed
49
22-oxacalcitriol
Suppressor of PTH gene expression and can be used for primary hyperparathyroidism syndrome
50
Sevelamer
Phosphate binding polymer that helps to lower phosphate by binding and eliminating it in the gut Used when you have really bad hyperphosphatemia
51
Colchicine
Used for treatment of gout Interferes with mitotic spindle formation to arrest cell division in G1 Greatest effect seen in cells that have a high turnover
52
Allopurinol
Inhibits xanthine oxidase to prevent synthesis of urate from hypoxanthine and xanthine Can be used with impaired renal function patients Increases the half life of probenecid to make it a synergistic reaction
53
Febuxostat
Nonpurine xanthine oxidase inhibitor that can cause liver function abnormalities, diarrhea, and nausea
54
Probenecid
Highly lipid soluble benzoic acid derivative inhibits uric acid renal tubular reabsorption Synergistic with allopurinol - allopurinol increases its half life Increases concentration of irate in urine so not good for use in patients prone to urate stones Blocks penicillin secretion
55
Tacrolimus
Decreases phosphorylation of NFAT by inhibiting calcineurin phosphatase Can lead to drug-induced hyperglycemia
56
Mycophenolate mofetil
Inhibits inosine monophosphate dehydrogenase to decrease de novo purine biosynthesis Noncompetitive reversible inhibitor of IMP which is an important pathway in B and T lymphocytes
57
Azathioprine
Purine antimetabolite that is cleaved to 6-mercaptopurine and works to inhibit de novo purine synthesis Side effect of myelosuppression
58
Muromanab CD3
Used for an acute rejection episode treatment. It works to block T-cell function and decrease T-cell number. Initial stimulation leads to cytokine release syndrome which can be prevented by pretreatment with prednisone.
59
M3 receptor agonists
Promote bladder voiding
60
Alpha-1 agonists
Examples are ephedrine and psudoephedrine. They can be used for treatment of urinary incontinence to help constrict sphincter.
61
Alpha-1 antagonists
Prazosin, terazosin, doxazosin, and tamsulosin | Used for treatment of symptoms of urinary obstruction (i.e. BPH) - helps to relax sphincter tone
62
Carbonic anhydrase inhibitors
Acetazolamine, methazolamide, and dichlorphenamide
63
CA inhibitor MOA
Leads to defective reabsorption of NaHCO3 But there's a ton of carbonic anhydrase located in the proximal tubule, so takes some time to inhibit enough to see an effect with electrolyte levels Not potassium sparing because leads to increased sodium delivery to the distal nephron Sulfonamide derivatives so can induce a hypersensitivity reaction Alkalinizes the urine Triggers tubuloglomerular feedback so a weaker diuretic because of this Toxicities inc: metabolic acidosis (loss of bicarb), hypokalemia (secretion of K), and renal stone formation
64
Osmotic agents
Mannitol, Isorbide, and Urea
65
Osmotic agent MOA
Undergo limited reabsorption so are freely filtered. Limit reabsorption of sodium and water Nonspecific diuretics that increase the excretion of all electrolytes Do not give long term because expand the ECF volume which can lead to hypertension, pulmonary edema, and eventually CHF (so also would go to show that you don't want to give these diuretics to patients with HTN because they can cause HTN!)
66
Loop diuretics
Furosemide, bumetanide, ethacrynic acid, and torsemide
67
Loop diuretic MOA
Inhibits the NKCC2 in the TAL of the loop of Henle Also blocks macula densa so does not trigger tubuloglomerular feedback (no dec. GFR) Is not potassium sparing - more sodium delivery to distal tubule, more potassium secretion
68
Ototoxicity
toxicity of loop diuretics due to concentration of inner ear fluid that in turn causes a "ringing" in the ears
69
Thiazide diuretics
Chlorothiazide, hydrochlorothiazide, chlorthalidone, indapamide, metolazone, quinethazone, etc.
70
Thiazide MOA
Blocks the Na-Cl symport in the DCT Can cause hypokalemia because also increasing sodium delivery downstream Directly activate calcium reabsorption channels as well so that there is decreased calcium reabsorption leading to the side effect of hypercalcemia Front-line diuretic treatment for increased blood pressure in patients
71
Potassium sparing diuretics
Amiloride, triamterene, spironolactone, and eplerenone Amiloride and triamterene - Direct ENaC blocker Spironolactone and eplerenone - aldosterone antagonists
72
Potassium sparing MOA
Works to block ENaC channels in the late distal tubule and collecting duct This leads to decreased potassium secretion because it decreases the transepithelial voltage in that works to secrete potassium Thus, will have decreased potassium excretion with these Aldosterone antagonists work to stop aldosterone's effect of decreasing the production and insertion of ENaC's as well as Na-K ATPase; with less channels formed, the better able to secrete more sodium
73
Gynecomastia
Side effect of spironolactone
74
Brain natriuretic peptide
Binds to specific receptors via c-GMP signaling to inhibit sodium reabsorption in the IMCD to increase sodium excretion Also inhibits renin-angiotensin pathway
75
CA inhibitor
This drug class can be used to increase the alkalinity of the urine and thus to increase the solubility of uric acid leading to increased irate secretion
76
Concentrated urine
Loop diuretics are the strongest diuretics and lead to electrolyte loss which impairs the ability to make concentrated urine
77
Altitude sickness
Carbonic anhydrase inhibitors can be use to treat this since signs of altitude sickness is attributable to metabolic alkalosis; however, can lead to hyperammonemia which can cause problems in people with liver disease
78
Glaucoma
Carbonic anhydrase inhibitors can be used to treat glaucoma as well because aqueous humor formation involves carbonic anhydrase activity
79
Hyponatremia
Side effect of thiazide diuretics due to their loss of more sodium than water
80
Foscarnet
Pyrophosphate analog that can chelate calcium and promote renal magnesium wasting

Renal (7 decks)

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