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Pharm block 5
hormone therapy
88
Pharmacology
Graduate
02/13/2013

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Term
Somatropin
Definition
[recombinant DNA human growth hormone]
-replacement therapy
SE: hyperglycemia, neutralizing Ab, carpal tunnel, fatality with PWS, interact w/glucocorticoids, hypothyroidism
Term
Tesamorelin
Definition
[GHRH analog]
-reduce excess abdominal fat in HIV+ w/lipodystrophy
-category X drug
Term
Mecasermin
Definition
[insulin like growth hormone]
-children w/ IGF-1 deficiency, neutralizing Ab from GH treatment, or defective GH receptor
SE: hypoglycemia (given w/small meals)
Term
Bromocriptine
Definition
[DA2 agonist]
-Tx for excess GH in acromegaly, hyperprolactinemia, PD
-dec fasting and post-prandial glucose levels
-oral, taken in morning
SE: nausea, HA, orthostatic hypotension, fatigue
Term
Octreotide
Definition
[somatostatin analog]
-inhibits Ca2+ influx
-2-3x daily
-sulfonylurea overdose (blocks Ca2+ induced insulin release downstream)
SE: bradycardia, conduction problems
Term
Lanreotide
Definition
[somatostatin analog]
-dose once every 2 weeks
SE: nausea, ab cramps
Term
Pasireotide
Definition
[somatostatin analog]
-multiligand (blocks GH and ACTH)
-cushing's disease
SE: hyperglycemia, inc liver enzymes
Term
Pegvisomant
Definition
[GH receptor antag]
-opioids dec its effects
SE: inc liver enzymes, flu-like symptoms
Term
Menotropins
Definition
[LH and FSH-like cmpnds]
-induce ovulation
-multiple births
SE: ovarian hyperstimulation syndrome (enlargement, ascites, hypovolumia)
Term
FSH
Definition
-induce ovulation
-in vitro fertilization
SE: ovarian hyperstimulation syndrome (enlargement, ascites, hypovolumia)
Term
LH
Definition
-induce ovulation
SE: ovarian hyperstimulation syndrome (enlargement, ascites, hypovolumia)
Term
HCG
Definition
[LH -like activity secreted by placenta]
-induce ovulation
-multiple births
SE: ovarian hyperstimulation syndrome (enlargement, ascites, hypovolumia)
Term
Clomiphene
Definition
-induces ovulation, oral agent*
-blocks E2 receptors in hypothalamus
-prevents normal feedback, inc LH and FSH release*
SE: multiple births, hot flashes, visual disturbances
Term
Gonadorelin
Definition
[GnRH agonist]
-short t1/2
SE: HA, dizziness, hot flashes
Term
Leuprolide
Definition
[GnRH agonist]
-continuous for cancer
-pulsatile for infertility
SE: HA, dizziness, hot flashes
Term
Centrorelix, Granirelix, Degarelix
Definition
[GnRH antagonist]
-dec release of LH and FSH
-for cancer, controlled ovarian hyperstimulation (in vitro fertilization), endometriosis*
Term
Synthetic oxytocin
Definition
-stimulate vasopressin R's and cause water retention
-milk ejection, uterine smooth muscle contraction
Term
Atosiban
Definition
[oxytocin antagonist]
-preterm labor
Term
Demeclocycline
Definition
[ADH antagonist]
-tx for SIADH (impairs cAMP action)
SE: nephrogenic diabetes insipidus, polyuria, nephrotoxic w/ pts in liver failure
Term
Natural vasopressin
Definition
[ADH]
-short t1/2
SE: water intoxication, excessive vasoconstriction
Term
Desmopressin
Definition
[ADH analog]
-long t1/2, less V1 side effects
-tx nephrogenic diabetes insipidus, hemophilia A (releases factor VIII), trauma induced bleeding, pre-op
SE: fluid retention, hyponatremia, seizures
Term
Conivaptan
Definition
[ADH receptor blocker]
-blocks V1 and V2
-euvolemic or hypervolemic hyponatremia (inc free water excretion BUT doesn't inc Na excretion)
-inhibits CYP3A4
Term
Tolvaptan
Definition
[ADH receptor blocker]
-blocks V2
-PKD, euvolemic/hyperV hyponatremia, SIADH
-inc Na quickly, causes ODS (osmotic demyelination syndrome)
-can be used in CHF
SE: liver toxicity
Term
Amiodarone, iodinated contrast media, BB, corticosteroids
Definition
[5'-deiodinase inhibitor: T4-->T3]
-tx for hyperthyroidism
Term
Levothyroxine
Definition
[hypothyroidism tx]
-T4
Term
Liothyronine
Definition
[hypothyroidism tx]
-T3
Term
Liotrix
Definition
[hypothyroidism tx]
-T4 and T3
Term
Iodine
Definition
[hyperthyroidism tx]
-suppresses TH release, dec iodide uptake
Term
Radioactive iodine
Definition
[hyperthyroidism tx]
-contraindicated in pregnancy, delayed hypothyroidism
Term
Propylthiouracil
Definition
[hyperthyroidism tx]
-inhibits peroxidase and 5'-deiodinase *(blocks syn of TH by interfering w/ incorporation of I into tyrosyl residues)
-tx for alcoholic liver disease
-takes 2-4 weeks to work*
SE: skin rashes, altered taste/smell, agranulocytosis, aplastic anemia
Term
Methimazole
Definition
[hyperthyroidism tx]
-inhibits peroxidase only
-longer t1/2
-crosses placenta
Term
Cortisol, cortisone, prednisone, prenisolone, methylprednisolone
Definition
[corticosteroids]
-some Na+ retention
Term
Triamcinolone, betamethasone, dexamethasone
Definition
[corticosteroids]
-NO Na+ retention
-for CHF (bc don't want to retain H2O and Na+)
Term
Aminoglutethimide
Definition
[adrenocortical antagonist: affects all 3]
-inhibits conversion of cholesterol to prenenolone
-"medical adrenectomy"
SE: blurred vision, drowsiness
Term
Ketoconazole
Definition
[adrenocortical antagonist: affects all 3]
-inhibits side chain cleavage of cholesterol (steroid hormone syn)
Term
Metyrapone
Definition
[adrenocortical antagonist: affects gluco and mineralo]
-inhibits 11-B hydroxylase
-only one used in pregnancy* (sex steroids not affected!)
Term
Abiraterone
Definition
[adrenocortical antagonist: affects all 3]
-blocks 17-alpha hydroxylase and 17,20 lyase
-tx for prostate cancer
-prodrug
Term
Mifepristone
Definition
[nonspecific adrenocortical antagonist: progestin and glucocorticoid]
-termination of pregnancy, induce labor after fetal death (w/ misprostol)
-dec endometrial blood supply, detach blastocyst (w/ methotrexate), softens cervix
SE: prolongs QT, hypertension, heavy bleeding, nausea, ab pain
Term
Spironolactone
Definition
[mineralocorticoid antagonist]
-primary aldosteronism, K+ sparing diuretic
-nonselective: also affects androgen R's (competes w/DHT)
-effect lasts 2-3 days after discontinuation
Term
Eplerenone
Definition
[mineralocorticoid antagonist]
-selective
-metabolized via CYP3A4
Term
Drospirenone
Definition
[mineralocorticoid antagonist]
-progestin
-aldosterone and androgen R antag
SE: may inc risk for blood clots
Term
Ulipristal
Definition
[selective progestin receptor modulator]
-blocks/delays ovulation, must start within 120 hrs post sex
-alters endometrium
-metabolized via CYP3A4
Term
Paroxetine
Definition
[SSRI]
-reduces menopausal hot flashes
Term
Gabapentin, Clonidine, exercise, soy
Definition
-reduces menopausal hot flashes
Term
Medroxyprogesterone acetate
Definition
[progesterone]
-added during the last part of the cycle
Term
Estren
Definition
[estrogen-like compound]
-reverses bone loss without affecting reproductive tissues
Term
Tibolone
Definition
-synthetic steroid w/3 metabolites: 2 estrogen properties, 1 progesterone and androgen
Term
Bisphosphates
Definition
-osteoporosis
Term
Teriparatide
Definition
-(PTH) osteoporosis*
Term
Raloxifene, tamoxifen, toremifene, droloxifene
Definition
[selective estrogen receptor modulator/ SERM]
-dec. LDL (no HDL effect)
-estrogen blocker in breast and uterus (antagonist)
-tx for osteoporosis (agonist)
-DOES NOT reduce menopausal hot flashes
SE: toremifine inc QT
Term
Danazol
Definition
[weak androgen, progestin, glucocorticoid activity]
-tx. for endometriosis, fibrocystic breast disease (suppresses ovarian function via LH and FSH inhibition)
SE: liver problems, jaundice (androgen like effects)
Term
Oxytocic
Definition
-stimulates uterine contraction --> labor
-control postpartum bleeding
-abortion
Term
Tocolytic
Definition
-suppresses uterine contractions
-inhibits preterm labor
Term
Magnesium sulfate
Definition
[uterine relaxant for preterm labor]
-inhibits Ca2+ entry and Ach release (weakness, resp arrest)
-crosses placenta
Term
Nifedipine
Definition
[uterine relaxant for preterm labor]
-blocks Ca2+ entry into uterine smooth muscle
Term
Terbutaline
Definition
[uterine relaxant for preterm labor]
-Beta-2 selective agonist relaxes smooth muscle
Term
Indomethacin
Definition
[uterine relaxant for preterm labor]
-inhibits PG syn
-premature closure of DA
Term
Hydroxyprogesterone
Definition
[uterine relaxant for preterm labor]
-dec expression of genes that encode contraction (proteins in myometrium)
-for women w/ at least 1 spontaneous preterm birth
Term
Dinoprostone, misoprostol
Definition
[promote cervical ripening]
-activates collagenase
-causes cervix to shorten, soften, and dilate (use w/ oxytocin)
Term
Finasteride
Definition
[5-alpha reductase inhibitor]
-inhibits ONE isoenzyme in prostate
-shorter t1/2
-tx for BPH, hirsutism, alopecia
-metabolized in liver
Term
Dutasteride
Definition
[5-alpha reductase inhibitor]
-inhibits TWO isoenzymes in prostate, skin, liver
-longer t1/2
Term
Flutamide
Definition
[anti-andronergic, R inhibitor for prostate cancer]
-blocks binding of DHT
-short t1/2
SE: hepatotoxicity, fewer effects than using GHRH antags
Term
Bicalutamide
Definition
[anti-andronergic, R inhibitor for prostate cancer]
-analog of flutamide but more selective
-once a day
Term
Cyproterone
Definition
[anti-andronergic, R inhibitor for prostate cancer]
-progestin
-competitive antag of DHT
Term
Insulin aspart, glulisine, Lispro
Definition
[Synthetic insulin: ultra short]
-onset 10-15 mins, duration 3-5 hrs
(glulisine pregnancy category C)
Term
NPH
Definition
[Synthetic insulin: intermediate]
-onset 1-2 hrs, duration 10-14 hrs
-only insulin that can be combined w/ others in the same syringe (draw up shorter acting first)
Term
Insulin detemir
Definition
[Synthetic insulin: long]
-onset 1-3 hrs, duration 14-23 hrs
-bound to albumin
Term
Insulin glargine
Definition
[Synthetic insulin: intermediate]
-onset 1-4 hrs, duration 16-28 hrs
-pH 4 neutralized and forms microprecipitates
Term
Insulin degludec
Definition
[Synthetic insulin: ultra long]
-duration >24 hrs
-no peak activity
-3x week
Term
Tolbutamide, Tolazamide, Chlorpropamide
Definition
[1st generation sulfonyureas]
-metabolized in liver
SE: disulfuram effects w/alcohol, hypoglycemia, weight gain

tolbutamide, tolazamide --> short
chlorpropamide --> long
Term
Glyburide, Glipizide, Glimepiride
Definition
[2nd generation sulfonyureas]
-metabolized in liver
SE: hypoglycemia, weight gain
Term
Diazoxide
Definition
[sulfonylurea overdose- 2nd line drug]
-ATP dependent K+ channel opener
Term
Repaglinide
Definition
[Meglitinide]
-bind ATP dep K+ channels, short acting
-vary amount needed by caloric intake
SE: hypoglycemia
Term
Nateglinide
Definition
[Meglitinide]
-bind ATP dep K+ channels (more selective), shorter acting
Term
Metformin
Definition
[Biguanide]
-dec. glucose production, inc glucose uptake, dec insulin resistance
-also tx for POS, ovarian cancer
SE: GI effects (diarrhea), contraindicated w/kidney impairment, lactic acidosis
Term
Rosiglitazone
Definition
-inc. insulin sensitivity, inc glucose transporters by PPAR gamma
SE: heart failure, worsen macular edema, inc risk of osteoporosis, liver tox, weight gain
Term
Pioglitazone
Definition
-inc. insulin sensitivity, inc glucose transporters by PPAR gamma
-some effect on PPAR alpha (dec TGs)
-weak CYP3A4 inducer
SE: bladder cancer, inc risk of osteoporosis, liver tox, weight gain
Term
Acarbose
Definition
[Glucosidase inhibitor]
-dec postprandial hyperglycemia
-not much systemic absorption
-given w/ each meal
SE: gas, ab bloating
Term
Miglitol
Definition
[Glucosidase inhibitor]
-dec postprandial hyperglycemia
-some systemic absorption
Term
Exenatide
Definition
[Incretin hormone/ GLP-1 receptor agonist]
-binds alpha cells --> dec hepatic glucose production in postprandial state
-slows gastric emptying, satiety
-subcutaneous or injection (not oral)
SE: hypoglycemia, N/V, diarrhea, fetal abnormalities
Term
Liraglutide
Definition
[Incretin hormone/ GLP-1 analog]
-once daily
SE: thyroid tumors
Term
Sitagliptin
Definition
[DPP-4 inhibitor]
-oral, pregnancy category B
-renal excretion
-tablets may not dissolve completely
SE: hypoglycemia
Term
Saxagliptin
Definition
[DPP-4 inhibitor]
-oral, pregnancy category B
-half metabolized via CYP3A4
SE: hypoglycemia
Term
Linagliptin
Definition
[DPP-4 inhibitor]
-oral, pregnancy category B
-metabolized via CYP3A4, excreted unchanged in urine
SE: hypoglycemia
Term
Alogliptin
Definition
[DPP-4 inhibitor]
-oral, pregnancy category B
-metabolized via CYP3A4, excreted unchanged in urine
-once a day
SE: hypoglycemia
Term
Canaglifozin
Definition
[SGLT2 inhibitor]
-lowers renal threshold for glucose
-once a day
SE: CV risk
Term
Pramlintide
Definition
[synthetic analog of human amylin]
-delay gastric emptying, inhibit glucagon release
-injected
SE: hypoglycemia, dec, appetite, nausea
Term
Colesevelam
Definition
[bile resin]
-inc incretin (GLP-1) secretion
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