Endocrine Drugs Flashcards
(71 cards)
1
Q
Somatotropin
Somatropin
A
- recombinant form of GH that acts through GH receptors to increase IGF-1 production
- restores normal growth and metabolic GH effects in GH-deficient individuals
- increases final adult height in some children with short stature not due to GH deficiency
- Primary Clinical Applications: replacement in GH deficiency; increased final adult height in children with short stature due to certain conditions
- Primary Toxicities (children): pseudotumor cerebri, progression of scoliosis, edema, hyperglycemia, risk of asphyxia and sleep apnea in obese PWS patients
- Primary Toxicities (adults): peripheral edema, myalgias, arthralgias, carpal tunnel syndrome
2
Q
Mecasermin
A
- recombinant form of IGF-1 that stimulates IGF-1 receptors
- improves growth and metabolic IGF-1 in individuals with IGF-1 deficiency due to severe GH resistance
- Primary Clinical Application: replacement in IGF-1 deficiency that is not responsive to exogenous GH
- Toxicity: hypoglycemia
3
Q
Octreotide
Lanreotide
A
- somatostatin (SST) analogs
- agonists at SST receptors
- inhibit production of GH
- Primary Clinical Application: acromegaly caused by GH-secreting tumors
- Toxicities: nausea, vomiting, abd cramps, flatulence, gallstones, sinus bradycardia, conduction disturbances
4
Q
Pegvisomant
A
- GH receptor antagonist
- blocks GH receptors
- ameliorates effects of excess GH production
- Primary Clinical Application: acromegaly
- Toxicity: well tolerated
5
Q
Urofollitropin
Follitropin alpha and beta
A
- FSH analog
- activate FSH receptors
- mimic effects of endogenous FSH
- Primary Clinical Application: controlled ovarian hyperstimulation in women; infertility due to hypogonadotropic hypogonadism in men
- Toxicities: ovarian hyperstimulation syndrome, multiple pregnancies
6
Q
Lutropin alpha
A
- LH analog
- agonist at LH receptors
- mimics effects of endogenous LH
- Clinical Application: used in combination with follitropin alpha in controlled ovarian hyperstimulation procedures for stimulation of follicular development in infertile women with profound LH deficiency
- Toxicities: ovarian hyperstimulation syndrome, multiple pregnancies
7
Q
Choriogonadotropin alpha
A
- hCG analog
- agonist at LH receptors
- mimics effects of endogenous LH
- Clinical Applications: controlled ovarian hyperstimulation in women; infertility due to hypogonadotropic hypogonadism in men
- Toxicities: ovarian hyperstimulation syndrome, multiple pregnancies
8
Q
Leuprolide
A
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
9
Q
Goserelin
A
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
10
Q
Histrelin
A
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
11
Q
Nafarelin
A
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
12
Q
Triptorelin
A
- gondadotropin-releasing hormone (GnRH) analog
- increased LH and FSH secretion with intermittent administration
- reduced LH and FSH secretion with prolonged continuous administration
- Clinical Applications: ovarian suppression during controlled ovarian hyperstimulation procedures; endometriosis; uterine fibroids; prostate cancer; central precocious puberty
- Toxicities (continuous treatment in women): symptoms of menopause, depression, decreased libido, generalized pain, vaginal dryness, breast atrophy, reduced bone density (with prolonged use)
- Toxicities (continuous treatment in men): hot flashes, edema, gynecomastia, decreased libido, decreased hematocrit, reduced bone density, asthenia
13
Q
Ganirelix, Cetrorelix, Degarelix
A
- GnRH antagonist
- blocks GnRH receptors
- reduces endogenous production of LH and FSH
- Clinical Application: prevention of premature LH surges during controlled ovarian hyperstimulation procedures; Degarelix is approved for treatment of symptomatic advanced prostate cancer
- continuous treatment with degarelix causes symptoms of androgen deprivation (e.g. hot flashes, edema)
14
Q
Bromocriptine
A
- dopamine (DA) agonist
- activate dopamine D2 receptors
- suppress pituitary secretion of prolactin
- Clinical Application: treatment of prolactinemia
- Toxicities: nausea, headache, lightheadedness, orthostatic hypotension, fatigue, psychiatric manifestations
- nausea lessened by vaginal administration
15
Q
Cabergoline
A
- dopamine (DA) agonist
- activate dopamine D2 receptors
- suppress pituitary secretion of prolactin; suppresses pituitary secretion of ACTH
- Clinical Application: treatment of prolactinemia; treatment of Cushing’s disease
- Toxicities: nausea, headache, lightheadedness, orthostatic hypotension, fatigue, psychiatric manifestations
- associated with incidence of cardiac valvulopathy
- nausea lessened by vaginal administration
16
Q
Oxytocin
A
- activates oxytocin receptors
- increased uterine contractions
- Clinical Applications: induction and augmentation of labor; control of uterine hemorrhage after delivery
- Toxicities: excessive stimulation of uterine contractions can cause fetal distress, placental abruption, or uterine rupture; inadvertent activation of vasopressin receptors can cause fluid retention, hyponatremia, heart failure, and seizures
17
Q
Vasopressin; Desmopressin
A
- ADH receptor agonists
- relatively selective activation of vasopressin V2 receptors
- antidiuretic effects (decreases water excretion)
- Clinical Application: treatment of diabetes insipidus
- Toxicities: overdose can cause hyponatremia and seizures; vasopressin (but not desmopressin) can cause vasoconstriction and should be used with caution in patients with CAD
18
Q
Hydrocortisone (Cortisol), Cortisone, Prednisone, Prednisolone, Methylprednisolone, Betamethasone, Dexamethasone
A
- glucocorticoids
- act through GC receptors and GC receptor elements on DNA to regulate the transcription of numerous genes
- Effects (metabolic): hyperglycemia, fat deposition in certain anatomical locations
- Effects (catabolic): muscle protein catabolism, wasting in lymphoid and connective tissue, fat, and skin
- Effects (immunosuppressive): inhibit the functions of tissue macrophages and other antigen presenting cells
- Effects (anti-inflammatory): affect distribution and function of leukocytes, suppress inflammatory cytokines and chemokines
- Clinical Application: replacement in primary adrenocortical insufficiency (Addison’s disease); replacement in congenital adrenal hyperplasia
- Toxicities (protein catabolism): growth retardation; osteoporosis; muscle wasting; thinning of skin and purple striae (bruising); poor wound healing
- Toxicities (fat metabolism): fat redistribution with central obesity
- Toxicities (glucose metabolism): hyperglycemia; diabetes mellitus
- Toxicites (other): depression; anxiety; hypomania; insomnia; glaucoma and cataracts; hirsutism; sweating; acne
19
Q
Fludrocortisone
A
- Mineralocorticoid (MC)
- act through MC receptors and MC receptor elements on DNA to regulate gene transcription
- Effects: promote sodium and water retention and secretion of potassium and protons in the distal tubule of the nephron; maintains plasma volume and blood pressure
- Clinical Applications: replacement in primary adrenocortical insufficiency (Addison’s disease); replacement in congential adrenal hyperplasia
- Toxicities: hypertension; hypokalemia; metabolic alkalosis
20
Q
Ketoconazole
A
- inhibitor of adrenal steroid biosynthesis
- non-selectively inhibits the P450C17, C17, 20-lyase, 3-beta-hydroxy-steroid dehydrogenase, and P450C11 enzymes
- inhibit the production of cortisol and aldosterone
- treatment of Cushing’s syndrome/disease
- treatment of PCOS to prevent hirsuitism
- Toxicity: hepatotoxicity, gynecomastia, amenorrhea
21
Q
Metyrapone
A
- inhibitor of adrenal steroid biosynthesis
- selectively inhibits the P450C11 enzyme
- inhibits the production of cortisol and aldosterone
- treatment of Cushing’s syndrome/disease
- Toxicity: salt and water retention, hirsutism
22
Q
Mifepristone
A
- GC receptor antagonist
- competitively inhibits GC receptors
- ameliorates effects of excess cortisol production
- treatment of Cushing’s syndrome/disease
- Toxicity: menstrual abnormalities
23
Q
Pasireotide
A
- somatostatin (SST) receptor agonist
- activates SST receptors
- suppresses pituitary secretion of ACTH
- treatment of Cushing’s disease
- Toxicities: nausea, diarrhea, hyperglycemia, bradycardia, conduction disturbances
24
Q
Spironolactone, Eplerenone
A
- mineralocorticoid receptor antagonsits
- competitively inhibit MC receptors
- diuretic effects
- ameliorates effects of excess aldosterone production
- Spironolactone also inhibits steroid binding, 17-alpha-hydroxylase, and 17,20-desmolase
- treatment of aldosteronism
- Spironolactone also used to treat PCOS
- Toxicities (spironolactone): hyperkalemia, cardiac arrhythmia, menstrual abnormalities, gynecomastia, hirsutism
- Toxicities (eplerenone): hyperkalemia
25
Phenoxybenzamine
- alpha-adrenoreceptor antagonist
- relatively selective antagonists of alpha-1 receptors
- an irreversible antagonist
- lowers blood pressure
- treatment of hypertension associated with pheochromocytoma
- Toxicities: orthostatic hypotension; tachycardia
26
Prazosin; Terazosin; Doxazosin
- alpha-adrenoreceptor antagonist
- relatively selective antagonists of alpha-1 receptors
- competitive antagonist (unlike phenoxybenzamine which is an irreversible antagonist)
- lower blood pressure
- treatment of hypertension associated with pheochromocytoma
- Toxicity: orthostatic hypotension
27
Atenolol; Metoprolol; Propranolol
- beta-adrenoreceptor antagonists
- atenolol and metoprolol are relatively selective antagonists of beta-1 receptors
- propranolol blocks both beta-1 and beta-2 receptors
- lower heart rate and blood pressure
- treatment of elevated heart rate associated with pheochromocytoma
- used only in conjunction with alpha-receptor antagonists (to prevent unopposed alpha)
- Toxicities: bradycardia, fatigue, cold hands
28
Metyrosine
- competitively inhibits tyrosine hydroxylase
- lowers blood pressure
- treatment of hypertension associated with pheochromocytoma
- Toxicities: extrapyramidal symptoms; orthostatic hypotension; crystalluria
29
Levothyroxine (L-thyroxine; L-T4; T4)
- bioavailability: ~100%
- routes: PO or IV
- metabolism: mainly liver, kidneys, brain and muscles
- elimination: 7 days (in hyperthyroidism 3-4 days, in hypothyroidism 9-10 days)
- excretion: feces and urine
- pregnancy category: A
* ** want to increase dose during first 12 weeks of pregnancy because baby is dependent on mothers thyroid hormone during this period... thyroid hormone is very important in fetal brain and skeletal development ***
- synthetically made
- recommended for treatment of hypothyroidism (not T3 or T4/T3 combinations)
- remember: 85% of T3 comes from T4 conversion
- age >60 or cardiac disease: must start at a low dose
- recheck thyroid hormone levels every 4-6 weeks after a dose change
- aim for normal TSH level
30
Medical Situations Where Levothyroxine Dosing May Be Affected
- weight changes (dose is based on weight)
- estrogen (pregnancy, OCP, HRT): need to increase T4 dose because of increased TBG... when TBG goes up, free T4 temporarily decreases and therefore the pituitary makes more TSH and then makes more T4
31
Things That Interfere with T4 Absorption
- iron, calcium, soy
- cholestyramine (cholesterol resin Rx)
- at least 4 hrs between T4 and these drugs
- levothyroxine is taken on an empty stomach about half to an hour before meals in the morning or at bedtime
32
Adverse Effects of Levothyroxine
- long-term suppression of TSH below normal values will frequently cause cardiac side-effects (atrial fibrillation, osteoporosis)
- overdose may cause hyperthyroidism-like effects; heart palpitations, tachycardia, heat intolerance, abdominal pain, nausea, anxiousness, tremors, insomnia, weight loss, and increased appetite
- rare allergic reactions (difficulty breathing, shortness of breath, swelling of the face and tongue
33
Drugs that inhibit production of thyroid hormones
-thioamides (PTU, MMI)
34
Drugs that block iodide uptake
- anionic inhibitors: perchlorate (ClO4-), thiocyanate (SCN-), pertechnetate (TcO4-)
- sodium-iodine symporter blocked by anionic inhibitors
35
Drugs that destroy the thyroid gland
-radioiodide (131-I) or surgery (thyroidectomy)
36
High Iodide and Thioamides
- TPO blocked by high iodide and thioamides
- proteolysis blocked by high iodide
- Iodine in high doses --> Wolff Chaikoff effect
37
Beta-Blockers and Treatment of Hyperthyroidism
- modify tissue responses (propranolol)
| - treat hyperadrenergic symptoms
38
Treatment of Thyroiditis
- ASA
- NSAIDS
- corticosteroids (+/-)
39
Propylthiouracil (PTU)
- blocks thyroperoxidase enzyme
- TPO's ability to oxidize the anion iodide (I-) to iodine and to add iodine to tyrosine residues on thyroglobulin are blocked in the presence of PTU
- inhibits 5' deiodinase activity (can't convert T4 to T3) (methimazole does not do this)
- 1/2 life 1-1.5 hrs
- side effects: agranulocytosis, rash, liver failure
- drug of choise during FIRST TRIMESTER pregnancy
40
Methimazole (MMI)
- blocks thyroperoxidase enzyme
- TPO's ability to oxidize the anion iodide (I-) to iodine and to add iodine to tyrosine residues on thyroglobulin are blocked in the presence of PTU
- 1/2 life 5-6 hours
- Side Effects: agranulocytosis, rash, less liver failure than PTU
- first line drug of choise to treat hyperthyroidism (EXCEPT DURING FIRST TRIMESTER OF PREGNANCY, THEN USE PTU)
- aplasia cutis if used during 1st trimester pregnancy
41
Hormonal Contraceptive
- typically contain a prosestin alone or combo of an estrogen and a progestin
- suppress the release of FSH and LH from the anterior pituitary, thereby inhibiting follicular development and preventing ovulation
- contraceptive activities of combination agents also include thickening of the cervical mucus and decreased ovum motility in the uterine tubes
42
Oral Contraceptives (combinations)
- monophasic: constant dosage of both components during the cycle
- biphasic: dosage of one or both components changes once during the cycle
- triphasic: dosage of one or both components changes twice during the cycle
- quite effective when taken according to directions, with risk of contraception being very small (0.3%)
- contraceptive failure has been observed in patients when one or more doses are missed, and due to interactions with other drugs
- product containing the smallest effective amounts of hormones should be used, to minimize the potential for the undesirable physiologic effects that are common with most hormone preparations
43
Adverse Effects of Oral Contraceptives (Mild)
- nausea, mastalgia, breakthrough bleeding and edema (related to amt estrogen - switch to a preparation with a smaller amt of estrogen)
- headache is mild and often transient, but exacerbation of migraine has been reported (discontinue in such a case)
- withdrawal bleeding sometimes fails to occur on "off" days
44
Adverse Effects of Oral Contraceptives (Moderate)
- breakthrough bleeding is a common problem with progestin-only contraceptives, but less so with combo
- weight gain and exacerbation of acne and hirstism can occur with combo agents containing androgen-like progestins (e.g. levonorgestrel)
- ureteral dilation has been reported, and bacteriuria is more frequent
- vaginal infections are more common and more difficult to treat in pts receiving oral contraceptives
- following cessation of contraceptive administration, amenorrhea occurs in some pts (sometimes lasting for several years) (many such pts are also galactorheic)
45
Adverse Effects of Oral Contraceptives (Severe)
- venous thromboembolic disease: approx 3-fold higher risk than in women not taking oral contraceptives
- myocardial infarction: slightly higher risk in women who are obese, have hyperlipoproteinemia or diabetes, or have a hx of HTN (risk increases further w/ smoking)
- cerebrovascular disease: risk of stroke is concentrated in women over the age of 35 who are current (but not past) users of oral contraceptives
- GI disorders: cholestatic jaundice has been reported in a number of patietns taking progestin-containing agents, which is reversible upon cessation (predisposition appears to be genetically based)
- depression: depression of sufficient degree to require cessation of therapy occurs in ~6% of pts treated with some preparations (many hormones have CNS effects)
46
Contraindications and Cautions of Oral Contraceptives
- pts with cardiovascular and cerebrovascular disorders or past hx of these conditions
- should be avoided or used with caution in pts with migraines, HTN, diabetes, liver disease, asthma
- liver metabolizes the hormones, so if you have liver disease then the hormonal levels will build up and it will unmask the adverse rxns
- interactions with other drugs (particularly antimicrobials) can reduce contraceptive efficacy
- antimicrobial drugs interfere with normal GI flora, which in turn, decreases enterohepatic cycling (and bioavailability) of estrogens
- drugs that induce hepatic metabolism can increase liver metabolism of estrogens and progestins
47
Beneficial Effects of Oral Contraceptives
- reduce risk of ovarian cysts, ovarian and endometrial cancer, and benign breast disease
- lower incidence of ectopic pregnancy
- iron deficiency and rheumatoid arthritis are less common
- premenstrual sxs, dysmenorrhea, and endometriosis may be ameliorated with use
- acne and hirsutism may also be ameliorated, provided the contraceptive does not contain an androgenic progestin
48
Transdermal Patch (Ortho Evra)
- combination of the synthetic estrogen ethinyl estradiol and the synthetic progestin norelgestromin in a 20 cm patch
- delivers 0.035 mg of ethinyl estradiol and 0.150 mg of norelgestromin per day
- 28 day cycle in which a new patch is applied each week for the first 3 weeks
- 4th week is patch-free
- hormones are very lipid soluble and this is why the patch is so effective (like nicotine patch)
49
Vaginal Ring (NuvaRing)
- flexible plastic ring containing a combination of ethinyl estradiol and etonogestrel
- delivers 0.015 mg of ethinyl estradiol and 0.120 mg of etonogestrel per day
- pts insert the ring into the vagina for 3 weeks, with the 4th week being ring-free
50
Subdermal Implant (Implanon, Nexplanon)
- flexible plastic rod that contains the synthetic progestin etonogestrel
- peak serum concentrations are attained in first few weeks, and effective ovulation suppression is maintained for 3 years
- rod is inseted subdermally on the inside of the upper arm
- implant should be removed after 3 years
51
Injectable Oral Contraceptives (Depo Provera)
- 3 month duration
- 3% typical use failure rate
- advantages: estrogen-free, long-acting, safe in breast feeding, decreased menses
- disadvantages: weight gain, menstrual irregularities, depression, BMD decrease, slow return of menses after stopping use
52
Postcoital Contraceptives (mifepristone)
- pregnancy can be prevented following coitus by administration of estrogens alone, progestins alone, or a combination of both
- the pregesterone receptor antagonist mifepristone has a luteolytic effect, and is also an effective postcoital contraceptive
- treatment is 99% effective if initiated within 72 hours
- the hormones are often co-administered with antiemetics, since 40% of patients experience nausea and vomiting
53
Levonogestrel (Plan B)
- postcoital contraceptive
| - 0.75 mg BID for 1 day
54
Clomiphene
- ovulation-inducing agent
- selective estrogen receptor modulator (SERM)
- acts as a partial agonist at estrogen receptors
- effectively inhibits the actions of stronger estrogens... in humans, this activity leads to an increase in the secretion of gonadotropins and estrogens by inhibiting estradiol's negative feedback effect
- pharmacologic importance of clomiphene rests on its ability to stimulate ovulation in women with oligomenorrhea and amenorrhea and ovulatory dysfunction
- a single course of therapy typically induces a single ovulation, and the patient must be treated repeatedly until pregnancy is achieved
- a 5-day course of therapy induces an initial rise in plasma LH and FSH after several days, which is ten followed by a 2nd rise in gonadotropin levels just prior to ovulation
55
Adverse Effects of Comiphene
- most common effects are hot flashes resembling those experienced by menopausal pts (disappear when drug is discontinued)
- other reported sxs include nausea and vomiting, nervous tension, depression, fatigue, breast soreness, heavy menses, and weight gain
- these appear to be result from the hormonal changes associated with an ovulatory menstrual cycle rather than from the medication
- incidence of multiple pregnancy is ~10%
56
Leuprolide and Other GnRH Agonists
- generally reserved for anovulatory women who fail to respond to other less complicated forms of treatment (e.g. clomiphene)
- they are most commonly used for controlled ovarian hyperstimulation (COH) in assisted reproductive procedures, such as in IVF
57
Ceftriaxone
- treatment of PID
- 3rd generation cephalosporin
- cephalosporins are beta-lactam antibiotics that inhibit the biosynthesis of the bacterial cell wall
- this activity results in bacterial cell death (it is bactericidal)
- inhibitor of cell wall synthesis
58
Azithromycin and Doxycycline
- treatment of PID
- azithromycin is a macrolide antibiotic and doxycycline is a tetracycline analog
- both are long-acting, orally bioavailable agents
- both agnest inhibit bacterial protein synthesis resulting in the inhibition of bacterial growth (they are bacteriostatic)
- azithromycin inhibits translocation step, while doxycycline inhibits elongation step
59
Acyclovir
- acyclic guanosine derivative
- requirement for viral kinase means activation occurs only in infected cells
- inhibits viral DNA synthesis
- indicated for HSV
- shortens the duration of sxs and viral shedding
- shortens time for lesions to heal
- topically is not effective for genital herpes
- long term suppression of HSV can be effective for frequent recurrances
- IV is DOC for herpes encephalitis
60
Valacyclovir
- L-vallyl ester of acyclovir
- converted to acyclovir after oral administration
- dose: similar to IV acyclovir
- more expensive, but can be taken just once/day
- common adverse effects: nausea, vomiting, rash
- when taken in high doses can cause hallucinations and seizures
61
Metronidazole
- broad spectrum antibiotic
- effective against anaerobes and protozoa
- requires activation via reduction to anion radial
- binds to proteins and DNA leading to loss of fxn
- DNA strand breakage
- inhibition of replication
- requires strong reducing conditions which are prevalent in anaerobes
- drugs are preferentially activated by pathogens
- reduced ferredoxin is the electron donor
- requires the pyruvate-ferredoxin oxidoreductase (PFOR) found in anaerobes
- protozoa affected by metronidazole lack mitrochondria and have PFOR
62
Metronidazole (Adverse Effects and Cautions)
- common: nausea, headache, dry mouth
- infrequent: vomiting, diarrhea especially with EtOH, insomnia, weakness, dizziness
- rare: neutropenia, CNS toxicity (ataxia, encephalopathy), pancreatitis
- use with caution in patients with CNS disease
63
Raloxifene
- agonist on bone
- antagonist at uterus
- increases risk of thromboembolic events
- decreases resorption of bone
- used to treat osteoporosis
64
Anastrozole/Exemestane
-aromatase inhibitors used in postmenopausal women with breast cancer
65
Terbutaline
- beta-2 agonist that relaxes the uterus
| - used to decrease contraction frequency in women during labor
66
Danazol
- synthetic androgen that acts as partial agonist at androgen receptors
- used for endometriosis and hereditary angioedema
- toxicity: weight gain, edema, acne, hirsutism, masculinization, decreased HDL levels, hepatotoxicity
67
Finasteride
- 5-alpha reductase inhibitor
- decreased conversion of testosterone to DHT
- useful in BPH
- also promotes hair growth-used to treat male-pattern baldness
68
Tamoxifen
- competitive partial agonist inhibitor of estradiol at the estrogen receptor
- used in the treatment of breast cancer in postmenopausal women and is approved for chemoprevention of breast cancer in high-risk women
- given orally
- excreted by liver
- hot flushes, nausea, vomiting occur in 25% of pts, and many other minor AEs are observed
- slight agonist in the endometrium
- agonist in bone
69
Anastrozole
- aromatase inhibitor
- suppress plasma estrogen levels in postMP women
- inhibit aromatase, the enzyme responsible for the synthesis of estrogens from androgenic substrates
- they have no partial agonist activity
70
Raloxifene
- similar to Tamoxifen
- used for osteoporosis
- selective estrogen receptor modifiers (partial agonist; blocks estradiol)
71
Herceptin
-targeted antibody towards HER2 receptor
