Renal, Endo and GU Drugs Flashcards
Furosemide
Loop Diuretic:
NKCC2: Thick ascending limb of loop of henle; this channel is used in Tubuloglomerular Feedback thus this drug inhibits TGF.
SEs: K, H+, Mg+, Ca2+ wasting; tinnitus, vertigo, hearing impairment, deafness
Also increases renal PG synth=more diuresis.
SHORT ACTING=USED FOR PULM EDEMA not for HTN management. And CHF (LMNOP=lasix, morphine, nsaids, Oxygen, posture)
TOX: SULFA ALLERGY, ototox, hypoK met alkylosis, hyperuremica, impaired Carb tolerance (hyperurecemia, hypomagnesmia
Ethacrynic Acid
Loop Diuretic:
NKCC2: Thick ascending limb of loop of henle; this channel is used in Tubuloglomerular Feedback thus this drug inhibits TGF.
K, H+, Mg+, Ca2+ wasting.
Also increases renal PG synth=more diuresis.
SHORT ACTING=USED FOR PULM EDEMA not for HTN management.
TOX: NO SULFA ALLERGY BUT MORE OTOTOXICITY, hypoK met alkylosis, hyperuremica, impaired Carb tolerance (hyperurecemia, hypomagnesmia
Acetazolemide
Carbonic Anhydrase Inhibitor (Diamox)–Inhibts bicarb absorption in the Prox tubule causing bicarb diuresis (this causes Bicarb dumping and LACK of H+ secretion from not making more bicarb).
Tx: Glucoma and CNS pressure, and altidude sickenss
Decreases Aqueos Humor Secretion.
CSF becomes acidotic causing CNS induced hyperventilation.
Hypokalemic, hyperchloremic (Aldo induced) met acidosis
AVOID IN HEP CIRRHOSIS from poor ammonia clearance (cuz you’re keeping H, thus you are dumping the NH3 counter ions)
HCTZ
Potassium wasting CALCIUM SPARING diuretic actingin the Distal Convulated tubule by inhibiting NCC.
Used in HTN, HF, Nephrolithiasis, Nephrogenic DI (reduces GFR allowing kidney a chance to absorp)
Inhibited by NSAIDs
Tox: RISK OF SULFA ALLERGY, Hyponatremia (Genetic idiosyncracies), hypokalemia, hyperglycemia, hyperlipidemia, hypomagnesia (in elderly).
Spironolactone and Epleronone
Aldosterone Receptor Antagonist: Potassium Sparing Diuretics, acting in the cortical collecting tubule.
Used in Conn’s Syndrome (hyperaldo)
Spironolactone can cause _Gynecomastia from week Antiandrogen receptor effects (WHY USED IN PCOS for Hirtuism)***; Eplerenone does not have this effect_
Tox: Hyperkalemic–cautionable use with other aldo antagonists (ACEI, ARBs…)
Amiloride
K Sparing diruetic by blocking ENaC channel (Na/K exchanger) on epithelial side of Collecting duct.
Tx: Used to counter hyperaldo, can be used in Diabetes inspidus (counter intuitive–used to dump Na preventing HyperNa and telling body to conserve water)
Tox: Hyperkalemic Met Acidosis
Triamterene
K Sparing diruetic by blocking ENaC channel (Na/K exchanger) on epithelial side of Collecting duct.
Used to counter hyperaldo
Tox: Hyperkalemic Met Acidosis, Kidney stones (not with amiloride)
Mannitol
2 majors SEs?
Osmotic Diuretic, Given IV and freely filtered by the kidney. Most effect on the proximal convulted tubule. _ REDUCES BRAIN VOLUME_ (lower Intracranial pressure and glaucoma tx).
PULM EDEMA: initally from rapid increase in fluid volume causing increase pulm pressure=pulm edema
Used to retain urine flow to remove toxins (ie Rhado/hemolysis)
Can worsen CHF; don’t give to anuric patients–causes HTN by pulling fluid from tissue to blood
Desmopressin
V2R agonist (ADH agonist) causing AC–>cAMP–>insertion of aquaporin channels.
Given paraentarally
ETOH inhibtis release of ADH
Also causes increase in vWF production
Colvaptan/Tolvaptan
“vaptans–like evaporate—to dry out”
ADH ANTAGONISTS–used for SIADH and paraneoplastic syndromes (Small Cell carcinoma)
Colvaptan–l V1a/2
Tolvapatan –lV2R
CAN CAUSE CENTAL PONTINE MYLOSIS from too rapid correction of hyponatremia
Bevacizumab
Anti-VEGF Antibody
Sorafenib
VEGF Inhibitor Small molecule
Sunitinib
VEGF inhibitor small molecule
Somatotropin/Somatropin
Growth Hormone, used to fix short stature in hypoGH kids and restore metabolic effects of GH
Tox: Pseudotumor cerebri, progession of scoliosis, edema, hyperglycemia
SLEEP APENEA in obese pnts.
Mecasermin
Recombinant IGF-1
Improves growth
Tox is Hypolgycemia (cuz IGF-1 has minor insulin activity)
Octreotide/Lanreotide
Somatostain Analogs.
Used to inhibit GH production in acromegaly/ GH tumors. Tx for some diarrheas. STOPS SPLANCHNIC CIRULATION THUS GOOD FOR GI BLEEDING (EG ESOPHAGEAL VARICES)
Tox: Nausea, vomiting, GI isues, Gall stones, Sinus brady
Pegvisomant
GH receptor Antagonist
Used for Acromegaly
Not real tox
“Peggy is short”
Urofollitropin
Follitorpin Alpha/Beta
FSH analogs
Used to control ovarian hyperstimulation (control levels and get feedback loop under control)
Infertility due to hypogonadotropic hypogonadism in men
Can cause multiple pregs
Lutropin Alpha
Choriogonadotropin Alpha
LH Receptor Agonist
Used in combo to stim follicular devo
Leuprolide, Goserlin
“relins”
GnRH agonists
Pulsatile Admin caues increase in FSH/LH
Continous admin cause knock down of FSH/LH
Prostate, Breast, Cehmical Castration, Fibriods and Precocious puberty Tx
Can cause bronchospasms and anaphylaxis type hypersenstivity Rxns
Ganirelix
“-relix”
GnRH receptor ANTAGONISTS
Lowers LH/FSH levels
Helps control female cycle and used for symptomatic advance prostate cancer
Bromocriptine
Cabergoline
D2 Recptor Agonists
Used to supress Prolactin secretion and for PD
Tox: nausea, headache, orthostatic hypotension
CABERGOLINE good because nasuea is lessened (particularly by vaginal administration) but associated with Cardiac Valvulopahty
Pitocin
Oxytocin Agonist (causing increase in Calcium which turns on myosin light chain kinase of myometrial smooth muscle)
Used to induce uterine contraction and control hemorrhage
Raloxifene
SERM: Selective EstroR modulator (antiER in breast/uterus, PROER in Bone)
Indicated for Osteoporosis and Prevention/Tx of Breast Cancer in post menopausal women
Venous thrombosis, and Teratogenic (any estrogen = increased coagulation)
Anastrozole
Reversible Aromatase competitve inhbitor
Used in women with ER+ Breast Cancer
Tox: Osteporosis
Clomiphene Citrate
SERM–inhibits ER of hypothalums thus disregulating E’s negative feedback
Infetility, PCOS, Male secondary hypogonadism (off-label)
Can result in multiple pregnancies
Norethindrone
Progestin pill only. Need to be on strick schedule (need to be within 3 hours each day)
Used for contraception, endometriosis, and abnormal periods.
Thickens Vaginal Fluid. Also stops ovulation in 50% of ppl (idiosyncratic)
Stop LH peak by inhibiting pituitary PR.
SMOKING INCREASES CV events
“Nothing but gestrone; and cuz its only half of the hormones, it stops ovulation in 50% of pnts”
Sprintec
E and P analog.
Used for Acne, decrease heavy/painful periods, decreases risk of ovarian cysts.
PE, MI, Thrombophlebitis, HTN, Gall bladder disease, depression
Increase CV risk w/ Smoking
Levonorgestrel
Plan B. Not effective once implantation has begun.
Synthetic progesterone—Inhibits ovulation by negative feedback on Hypothalamus.
Decreases FSH/LH
Mifepristone
Abortifacient (RU486) for first 49 days. (“mife has F for fuck it”)
PR antagonist (stronger than P4), causing endometrial degeneration and cervical softening and finally trophoblast detachment and uterine contraction–bascially simulating ovulation (via decrease P4).
ALSO competitive inhibitor for glucocorticoid receptor
Vaginal Bleeding***, infection
Tertbutaline
B2 agonist. “Relaxes uterus just like airway”
Used for Preterm Labor by slowing uterine contractions (only for 72 hours). Asthma tx too
Can cause breathing issues, fast pounding irregular heart, chest pain, seizures.
Nifedipine
Calcium channel blocker
Used to treat preterm labor by slowing uterine contractions.
don’t combine with MgS04. Constipation, dizziness, nausea. Prolonged vaignal bleeding.
Indomethacin
NSAID used to decrease PGs that normally produce uterine contractions.
Limitations on Dose due to fetal effects=Causes premature closure of ductus arteriosus (lack of PGE2), and Oligohydramnios (loss of fetal PGs causes dysregulation of kidneys)
Magnesium Sulfate
Thought to block calcium
Used for neuroprotective (Cerbral Palsy) effects in preeclampsia (does not really slow contractions in RCTs)
First sign of trouble is loss of patellar reflex
Misoprostol
Labor induction (“prostol pushes”). PGE1
Miscarriage, teratorgenic, uterine rupture, hyperstimulation, HTN, anaphhylaxis, HTN, MI, Arrhtymias, Thromboembolism
Methergine
(“erg”=ergot) ERGOT alkalyoid used for uterine atony and post partum hemorrhage.
Cramps, Respiratory depression, coma
Carboprost
“prost pushes”
PG2 analog that binds PG E2 rectpeor.
Uterine contractor, post partum hemorrhage, 2nd trimester aborptions.
Transient bronchoconstrictions
Doxycyline
Tetra type antibiotic. Inhibits protein synth by binding to the 30s ribo.
UTI, Acne, gonorhea, chlamydia, lymes, periodonitis
Calcium chelotar (binds to bones/teeth). Can cause RTA** and sever skin reaction
Terconazole
azole. Candida albicans in vagina.
Disrupts fungal Cyp450 inhibiting erogsterol production
Flu like sxs
Valacyclovir
Prodrug converted into acylcovir (purine analog guonsine derivative.)
Tx for HSV1/2, Herpes Zoster
Herpes simplex prophyalxis/reduction of transmission.
Prevention of CMV following an organ transplant
Mono
Herpes B virus exposure
Metronidazole
Flagyl. Reduced in organism causing anion to bind to DNA.
Requires mitochondria or organisms that have PFOR
Acts like Dilsulfiram. Severe skin reactions.
Don’t use with ppl with Severe CNS diseases (neutropenia, pancreatitis, ataxia, encephalopathy)
Insulin Preps
Rapid Acting: 5-15 min: Lispro, aspart, glulisine
Long acting: Glargine and Detemir
Glimperide
Glipizide
Glyburide
Sulfonylureas: inhbit Beta cell potassium channel which increases depolarization and Insulin release
Not indicated for heaptic dieases
Glipizide and glybruide also not indicated for renal disease
Repaglinide
(Prandin) Meglinitides: Fast and brief stim of insulin secration
“Non-sulfonureas”
Nateglinidie (Starlix)
Metformin
Biguianide. Turns on AMPK of liver.
Lowers glucose output of liver and increases liver insulin sensitivity.
Ppl lose weight on it.
GI issues, B12 absorb issues, and SEVERE LACTIC ACIDOSIS
Prioglitazone and Rosiglitazone
“-glitazones get ya in the zone to respond to insulin”
Thiazolidines. Binds PPARgamma increasing insulin responding proteins
Increase glut uptake and fat repatterning
SEs: Weight gain, fluid retention AND CONGESTIVE HEART FAILURE
Exanatide, Laraglutide
“Tides produce a tide of GLP1/GIP”
GLP-1 incretins: LOWER BLOOD SUGAR
1) SLOWS GI tract (less absorption), Promote insulins release and glucogaon inhibtion
Inactived by DDP-4.
SEs: GI, Vomitting, Hypoglycemia
Sitagliptin, Saxagliptin, Linagliptin, Alogliptin
“-Glipins keep GLPs lvls by INhibiting DDP4”
DDP-4 inhibitors preventing the breakdown of GLP-1 and GIPs
Canaglifozin, Dapaglifozin
“glifozin keeps ya whizzin”
Inhibits Kidney SGLT-2 which causes glucose to be in the urine.
Dehyration, UTIs, and Yeast infections
Acarbose
Miglitol
“acarbose makes you A-CARBic”
Alpha glucosidase inhbitors: used to process sugar before GI absorption.
This lowers postprandial gluc levels
SEs: GI Issues
Pramlinitide
“you need PRAMlinitide with your chicken PARM cuz you shotgun it”
Amylin Agonists: Slows stomach emptying, reducing glucagon production.
SEs nausea and hypoglycemia, GI motility issues (no gastroparesis)
Colesevelam
Bile Acid Binding Resins
Bromocriptine
Modestly improves glycemic control at lower doses than for AD/Prolactinoma lvls
Hydrocortisone
Prednisone
Betamethason
Dexamethasone
Lower ones have longer duration of actions.
Corticosteroids acting through the Glucocorticoid receptor (steroid receptor).
1) Cushoiniod Effects: Ups Blood sugar, Central fat depostion, protein catabolism
2) Immunosupressive and antiinflamatory effects: supresses cytokine/chemokine production/response.
Used for: Primary adrenocortical insufficiency (Addison’s Disease), replacement for CAH (can be given to mother if daughter is homorecessive for Cyp21 def to prevent ambigious genitalia).
SEs: Crosses placenta/breast, cushingoid, growth retard, fusing of ephyseal plates (termination of linear growth), osteoporiss, muscle wasting, steroid psycosis
Flucortisone
“Flu–for fluid” Mineralcorticoid Agonist
Works just like Aldo.
Used for primary adrenal insufficiency (WONT NEED IT FOR SECONDARY CUZ RAAS IS STILL INTACT since adrenals themselves are ok (possibly atrophic, depneding on chronicity of condition)). ALso for CAH (3 def, 21 def, don’t need for 11 def cuz there is still minor mineralcoritcoid agents being produced (precurosors).
SEs: HTN, HYPOK, Met alk
Ketaconazole
Inhibitor of Steroid biosynth (fungal CYP450 14 and adrenal cyps)
Inhibits Cyp 17, 3, 11 (so you get nothing from adrenals–but apparently in real life you still get minor aldo)
Tx for Cushings
HEPATOTOXIC
Metryapone
“can still bone on metryapone—cyp 11 inhib thus you still have andro excess and some mineralcoritcoid”
Adrenal Steroid biosyntheis inhibitor
Inhbits Cyp 11 (still get weak mineralcorticoid action)
SEs: Na/H20 retention; Hirtuism
Cabergoline
D2 Recptor agonist causing supression of pituiary ACTH
Treats Cushing’s DISEASE
SEs: Cardiac Valvulopahty, H/A, Ortho HOTN, Fatigue, psych manifesations
Pasireotide
Somatostatin Receptor Agonist causing Pit supresion of ACTH
Tx for Cushing’s DISEASE
SEs: GIs, Hyperglycemia, Bradycardia, conduction disturbances
“-eotide” somatostatin analog
Phenoxybenazmine
Prazosin
Terazosin
Doxazosin
Alpha 1 antagnoists
Phenoxy is irreversible.
zosins are competitive antagonists.
HTN Tx associated with pheo’s
SEs: HOTN; Phenoxy can cause TACHY
Metryosine
Compeitivley inhibits Tyrosine Hydroxylase
Lowers blood pressure via inhibition of catecholamine production.
Tx for pheos
SEs: Extrapyramidal Sxs, ortho HOTN, crystalluria
Levothryoxine
Synthetic T4. Long acting, delayed onset.
When initially dosing you might need to give large dose because of unsaturated TBG.
Liothyronine
Synthetic T3. Short duration and Faster onset of action.
Better used for acute crisis—Myxedema Coma
Liotrix
Synthetic T4/3. 4:1 T4 to T3 Ratio
Propylthiouracil
Blocks TPO and 5’deiodinase.
Less hormone production (TPO) as well as blocking peripheral T4–>T3 conversion (5’)
DOES NOT inhibit the iodide transporter
Use PTU in pregnant women ONLY 1st Trimester
SEs: Teratogenic, Agranulocytosis, hepatotox
RASH, AGRANULOCYTOSiS, APLASTIC CRISIS
Methimazole
Inhibits TPO, NOT iodide tranporter. DOES NOT block peripheral T4–>T3
Longer half life, First line in Non-preggers.
Used to lower thyroid levels presurgery.
If you are going to use in Preggers, use in 2+3 trimesters.
SEs: Teratogenic, Agranulocytosis, hepatotox
RASH, AGRANULOCYTOSiS, APLASTIC CRISIS
Cinacalcet
Increases sensisitivty of CaSR of chief cells of PThyroid Gland.
Tx for Secondary hyperparathryroidism
Furosemide’s Mechanism of Action?
SEs?
Thick ascending limb.
1) Messes up countercurrent mechanism
2) Stims PG release causing vasodilation adding to diruresis (THEREFORE NSAIDS INHIBIT THIS EFFECT AND FUROSEMIDE***)
SEs: ototox, hypoK, dehydration, allergy (sulfas), nephrotox, HYPERURICEMIA
Sickle cell patient presents with gross hematuria…whats going on?
Other causes of this?
Renal Papillary necrosis. (ischemic tubular necrosis is in fluid deprived pnts=oliguria and muddy brown casts)***
Analgesic Nephropathy, DM, Acute pyelonephritis, UTIs
1) Rapid onset hematuria vs 2) oligouria with muddy brown casts?
1) Renal papillary necrosis
2) Acute/Ischemic Tubular Necrosis
Palpable nontender gall bladder with weight loss?
Number 1 risk factor?
Courvoisier sign of Pancreatic Head Adenocarcinoma.
Smoking
