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Renal > Renal Pharmacology > Flashcards

Renal Pharmacology Flashcards

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
Q

Aztreonam

A

Penicillin analog effective against pyelonephritis

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26
Q

Piperacillin-tazobactam

A

Tazobactam is a beta-lactamase inhibitor so this drug combination works synergistically with broad spectrum activity against gram positive and gram negative organisms

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27
Q

Imipenem

A

Very resistant to chromosomal beta-lactamases so a good drug option
Broken down pretty quickly with toxicity of hypersensitivity

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28
Q

Aminoglycoside

A

Frontline treatment for urinary catheter associated UTI along with a fluoroquinolone or other cephalosporin

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29
Q

MOA of aminoglycoside

A

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

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30
Q

Amikacin

A

Aminoglycoside resistant to lots of enzyme inactivation steps so used pretty widely in hospital setting

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31
Q

Ototoxicity

A

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

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32
Q

Renal toxicity

A

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

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33
Q

Tigacycline

A

Overcomes tetracycline resistance mechanisms of efflux pumps but outdated preps can lead to Fanconi’s
Must be given intramuscular instead of IV

34
Q

Dihydropteroate synthase

A

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
Q

Dihydrofolate reductase

A

Inhibition of this enzyme is from trimethoprim in bacterium prep

36
Q

DNA gyrase

A

What is inhibited by quinolones/fluroquinolones in gram-negative bacteria

37
Q

Topoisomerase IV

A

What is inhibited by quinolones/fluoroquinolones in gram-positive bacteria

38
Q

Methenamine

A

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
Q

Nitrofurantoin

A

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
Q

Praziquantel

A

Anti-protozoal that is effective against schistosoma and causes muscular contraction and paralysis at higher drug-levels

41
Q

Metrifonate

A

Seocnd-line for S. haematobium infection and works by being activated to dichlorovoros which inhibits acetylcholinesterase in the worm

42
Q

Mineralocorticoids

A

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
Q

Spironolactone

A

MR antagonist

Can have some action at androgen receptors so can induce gynecomastia, etc.

44
Q

Fludrocortisone

A

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
Q

Eplerenone

A

MR antagonist other than spironolactone

46
Q

11-beta HSD2

A

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
Q

Calcitriol

A

The only vitamin D analog that should be given in renal failure patients as it has been both 1-hydroxylated and 25-hydroxylated

48
Q

Cinacalcet

A

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
Q

22-oxacalcitriol

A

Suppressor of PTH gene expression and can be used for primary hyperparathyroidism syndrome

50
Q

Sevelamer

A

Phosphate binding polymer that helps to lower phosphate by binding and eliminating it in the gut
Used when you have really bad hyperphosphatemia

51
Q

Colchicine

A

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
Q

Allopurinol

A

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
Q

Febuxostat

A

Nonpurine xanthine oxidase inhibitor that can cause liver function abnormalities, diarrhea, and nausea

54
Q

Probenecid

A

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
Q

Tacrolimus

A

Decreases phosphorylation of NFAT by inhibiting calcineurin phosphatase
Can lead to drug-induced hyperglycemia

56
Q

Mycophenolate mofetil

A

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
Q

Azathioprine

A

Purine antimetabolite that is cleaved to 6-mercaptopurine and works to inhibit de novo purine synthesis
Side effect of myelosuppression

58
Q

Muromanab CD3

A

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
Q

M3 receptor agonists

A

Promote bladder voiding

60
Q

Alpha-1 agonists

A

Examples are ephedrine and psudoephedrine. They can be used for treatment of urinary incontinence to help constrict sphincter.

61
Q

Alpha-1 antagonists

A

Prazosin, terazosin, doxazosin, and tamsulosin

Used for treatment of symptoms of urinary obstruction (i.e. BPH) - helps to relax sphincter tone

62
Q

Carbonic anhydrase inhibitors

A

Acetazolamine, methazolamide, and dichlorphenamide

63
Q

CA inhibitor MOA

A

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
Q

Osmotic agents

A

Mannitol, Isorbide, and Urea

65
Q

Osmotic agent MOA

A

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
Q

Loop diuretics

A

Furosemide, bumetanide, ethacrynic acid, and torsemide

67
Q

Loop diuretic MOA

A

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
Q

Ototoxicity

A

toxicity of loop diuretics due to concentration of inner ear fluid that in turn causes a “ringing” in the ears

69
Q

Thiazide diuretics

A

Chlorothiazide, hydrochlorothiazide, chlorthalidone, indapamide, metolazone, quinethazone, etc.

70
Q

Thiazide MOA

A

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
Q

Potassium sparing diuretics

A

Amiloride, triamterene, spironolactone, and eplerenone

Amiloride and triamterene - Direct ENaC blocker
Spironolactone and eplerenone - aldosterone antagonists

72
Q

Potassium sparing MOA

A

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
Q

Gynecomastia

A

Side effect of spironolactone

74
Q

Brain natriuretic peptide

A

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
Q

CA inhibitor

A

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
Q

Concentrated urine

A

Loop diuretics are the strongest diuretics and lead to electrolyte loss which impairs the ability to make concentrated urine

77
Q

Altitude sickness

A

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
Q

Glaucoma

A

Carbonic anhydrase inhibitors can be used to treat glaucoma as well because aqueous humor formation involves carbonic anhydrase activity

79
Q

Hyponatremia

A

Side effect of thiazide diuretics due to their loss of more sodium than water

80
Q

Foscarnet

A

Pyrophosphate analog that can chelate calcium and promote renal magnesium wasting

Renal (7 decks)

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