endocrine Flashcards
Estradiols
estradiol cypionate
Premarin
ethinyl estradiol
biological affection of estradiols
female tract development
secondary sexual characteristic
reduce secretion of gonadotropin from pituitary
increase triglyceride, reduce LDL, increase HDL
increase coagulation of blood protein
diethylstilbestrol
we do not use it anymore
it was use unsuccessfully to prevent miscarriage
it causes severe toxicity
ectopic pregnancy
infertility
vaginal adenocarcinoma
DES daughter
have increase risk of develop breast cancer and cervical caner
DES son
have increase risk of develop cryptorchidism
hypospadias
transgenderism, gender dysphoria
emergency contraception / post coital contraceptive
( morning after pill )
prevent pregnancy if given within 72 hours
can be combination of estrogen and progestin
or progestin only
progesterone only product have fewer side effects
action - inhibit ovulation before LH surge
decrease receptivity in uterine tube endometrium
altered cervical mucous gland function
monophasic or
mulitphasic with placebo week ( sugar pill to get period )
oral estrogen
Non-contraceptive use
Tx for hypogonadism in sound females
Hormone replacement therapy in females with premature ovarian failure or surgical removal
Hormone replacement therapy in postmenopausal females
side effect of oral contraceptive agent / oral estrogen
increase risk of endometrial cancer ( prevented by combining with progestin )
increase risk in breast cancer (postmenopausal women)
increase in CV risk in postmenopausal women
toxicity / overdose effect of oral contraceptive agent / oral estrogen
nausea
great tenderness
migraine
thromboembolic disease
gallbladder disease
Hypertriglyceridemia
hypertension
progestins
progesterone is the major progestin in human
induces secretion of endometrium, healthy endometrium for pregnancy
medroxyprogesterone
prototypical oral synthetic progestin
synthetic progestin doesn’t support pregnancy
inhibit ovulation
in HRT use as adjunct to reduce the risk of endometrium cancer
side effect of progestin
affect carb metabolism
stimulate fat deposits
dec HDL
reduce boen density ( long term)
delayed ovulation after cessation
suppress GnRH and LH, FSH
Selective Estrogen Receptor Modulator ( SERMs)
Tamoxifen, Toremifene
Estrogen receptor antagonist in breast tissue - reduce risk of breast cancer
estrogen receptor agonist in endometrial tissue - promote endometrial hyperplasia
increase risk of endometrial cancer
side effect of SERMs
as antagonist - hot flash
as agonist - increase risk of venous thromboembolism
- increase risk of endometrial cancer
Selective Estrogen Receptor Modulator ( SERMs)
Raloxifene
approved of prevention and treatment of osteoporosis
antagonist effect - reduce breast cancer risk
agonist effect - no estrogenic effect on endometrial tissue ( unlike tamoxifen)
Selective Estrogen Receptor Modulator ( SERMs)
Bazedoxifene
use for menopause symptoms and osteoporosis prevention
Selective Estrogen Receptor Modulator ( SERMs)
Clomiphene
reduces negative feedback in pituitary increase LH and FSH
induce ovulation in anovulatory women
Pure estrogen receptor antagonist
Fulvestrant
use in breast cancer with resistance to tamoxifen
use in women with breast cancer with endometrial risk factor
non-steroidal competitive aromatase inhibitor ( synthesis inhibitors )
anastrozole, letrozole
irreversible aromatase inhibitor
Exemestane
Danazol
inhibits enzyme involve in Gn synthesis
weak partial agonist of progestin, androgen and glucocorticoid receptor
use in tx of endometriosis and fibrocystic breast disease of the breast
Leuprolide
Gonadotropin- releasing hormone analogue
MOA- cont’d stimulation of GnRh receptor suppresses secretion
inhibits ovarian production of estrogen and progesterone
use in Tx of - precocious puberty
- short term tx of endometriosis
- short term tx of fibrosis
Gonadotropin- releasing hormone antagonists
abarelix, degarelix
use in tx of prostate cancer
Mifepristone
estrogen promotes
reproduction : ductal growth in Brest,
thickening of vaginal epithelium
proliferation of uterine epithelium
copious secretion of thicken mucus form endocervical gland
increase vaginal acidity
promote endometrial restoration after menstruation
metabolic : block bone reaborsptlon
promotes epiphyseal closure
lower the risk pf cardiovascular disease
CNS neruprotective
promotes insulin sensitivity and glucose uptake
three cause of insulin resistance
reduce binding of insulin to ties receptor
reduce receptor numbers
reduced receptor responsiveness
criteria for Dx of DM
fasting glucose > 126mg/dl
random glucose > 200mg/dl plus symptoms
oral glucose tolerance test: 2 hr plasma glucose > 200mg/dl or Hemoglobin A1c 6.5 or higher
criteria for Dx of DM
fasting glucose > 126mg/dl
random glucose > 200mg/dl plus symptoms
oral glucose tolerance test: 2 hr plasma glucose > 200mg/dl or Hemoglobin A1c 6.5 or higher
preferred agent to manage DM hypertension
ARB eg losartan
1- initiate life style change plus metformin
2- cont’d step 1 and add a second drug, either thiazolidinedione, a DDP-4 inhibitor, a GLp01 receptor agonist. a sulfonyulurea or basal insulin should be considered if pt doesn’t achieve glucose control goal
3- progress to three drug combination therapy
4
general glycemic treatment target
A1c < 7
peak postal plasma glucose < 180 mg/dl
regular insulin. humulin R , novolin R
onset 30 - 60
peak 1-5
duration 6-10 hr
insulin glargine ( Lantus )
long acting
onset 70 min
peak N/A
duration 18-24 hours
insulin determir (levemir )
long acting
onset 60 - 120 mins
peak 12-24 hrs
duration : depends on dose
0.2 unit / kg 12 hr
0.4 unit / kg 20-24 hr
insulin determir (levemir )
long acting
onset 60 - 120 mins
peak 12-24 hrs
duration : depends on dose
0.2 unit / kg 12 hr
0.4 unit / kg 20-24 hr
NPH ( humbling H)
intermediate
onset 60-120
peak 6-14 hrs
duration 16-24hrs
MOA of Biguanide ( metformin )
decrease glucose production by liver
increase tissue response to insulin
adverse effect of metformin
GI symptom - decrease appetite, Nausea, diarrhea
lactic acidosis
should be held at hospital to prevent adverse accumulation of drug such as can occur with renal impairment in patients with dehydration or exposed to iodine contrast studies during hospital stay.
second gen Sulfonylureas
Glimepir-ide
Glipiz-ide
Glybur-ide
-ide take my sulfonylureas
MOA of sulfonylureas
promote insulin secretion by binding to the K channel
adverse effect of sulfonylureas
hypoglycemia
weight gain
Meglitinides ( Glinides)
Nateglinide
Repaglinide
similar to sulfonylureas but binds to a different site Ca channel instead K )
Meglitinides ( Glinides)
Nateglinide
Repaglinide
adverse effect of Meglitnides
adverse effect of Meglitinides
hypoglycemia
weight gain
Thiazolidinedione (Glitazones )
Pioglitazone
Rosiglitazone
MOA of Thiazolidinedione (Glitazones )
Thiazolidinedione (Glitazones )
increase insulin sensitivity , increase glucose uptake by muscle and adipose tissue and decrease glucose production by the liver
binding to the proliferator activated receptor gamma (PPAR-gamma ) nuclear factor
bring -glita to the PPAR-ty
adverse effect of Thiazolidinedione (Glitazones )
heart failure exacerbation in HF patient due to it increase fluid retention in the kidney
fracture
ovulation –> unintended pregnancy
DPP-4 inhibitors (gliptins)
Sita-gliptin
Saxa-gliptin
Lina-gliptin
DPP-4 inhibitors (gliptins)
Sita-gliptin
Saxa-gliptin
Lina-gliptin
MOA of
MOA of DPP-4 inhibitors (gliptins)
enhance the activity of incretins by inhibiting their breakdown by DPP-4
thereby increase insulin release, reduce glucagon release and decrease hepatic glucose production
adverse effect of DPP-4 inhibitors (gliptins)
upper respiratory tract infection
pancreatitis
sodium - glucose co-transporter 2 inhibitor
Canagliflozin
increase glucose excretion via urien by inhibiting SGLT-2 in the kidney tubule
dec glucose level and inducing weight loss
Adverse effect of SGLT-2
Genital mycotic infection
orthostasis
