ENDOCRINE PHARMACOLOGY Flashcards
Dopamine agonist > inhibiting prolactin
Bromocriptine
Pergolide
Cabergoline
Quinagolide
*category B!
Rare disorder seen in px taking Bromocriptine characterized by burning pain and warmth and redness of the extremities
Erythromelalgia
Activates oxytocin receptors > stimulates uterine contraction and labor, milk let down
Oxytocin
Demoxytocin
Agonist of peripheral oxytocin receptors
Carbetocin
Oxytocin-receptor blocker not yet FDA approved due to increase incidence of infant death rates
Atosiban
Selective for V2 receptors
1. Causes insertion of water channels in the CD > water reabsorption
2. Act on extra-renal V2 receptors to increase factor VIII and vWF
ADH agonist
DVT
Desmopressin
Vasopressin
ADH agonist is used in:
Central diabetes insipidus
Antagonist at V1 and V2 receptors > increases renal excretion of water
ADH antagonist
Conivaptan
Tolvaptan
Lixivaptan
Tol and Lixi: more selective to V2
ADH antagonist drugs are used in what condition?
SIADH
May SIADH si Coni :<
2 types of Diabetes Insipidus
- Central DI: deficient secretion of ADH
- Nephrogenic DI: end-organ resistance to ADH effects
GH agonist that increases release of IGF-1 in the liver and cartilage
Somatropin
Recombinant IGF-1
Mecasermin
Blood glucose level in GH agonists:
- Somatropin: HYPERglycemia
- Mecasermin: HYPOglycemia
Somatostatin analogs
Octreotide
Lantreotide
Supresses the release of GH, glucagon, insulin, IGF-1, serotonin, and GIP
Somatostatin (octreotide, lanreotide)
GH receptor antagonist
Pegvisomant
Activates FSH receptors > mimics effects of endogenous FSH
FSH analogs
FOLLItropin
Menotopins
UtoFOLLItropins
FOLLItropin beta
Activates LH receptors > mimics effects of endogenous LH
LH agonists
Choriogonadotropin alfa - recombinant hCG
Lutropin alfa - recombinant LH
Menotropins - mixture of FSH and LH from postmenopausal women
hCG
GNRH agonists
Leu + -relins
Leuprolide
Gonadorelin
Goserelin
Histrelin
Nafarelin
Triptorelin
Administrations of GnRH agonists
- Intermittent: increase LH and FSH secretion
- Prolonged continuous administration: reduced LH and FSH secretion
GnRH antagonists
Ganirelix
Cetrorelix
Abarelex
Degarelix
GnRH inhibitor used for prostate cancer
Degarelix
GnRH used to prevent LH surge in controlled ovulation
Ganirelix
Hyperthyroidism drug preferred during 1st trimester
PTU
Mainstay treatment for postpartum hyperthyroidism
Methimazole
Blocks uptake of iodide by the gland through competitive inhibition of the iodide transport mechanism
Perchlorate
Petechnetate
Thiocyanate
Methimazole is preferred over PTU except in what conditions:
- 1st trimester pregnancy
- Thyroid storm
- Methimazole sensitivity/allergy
S/E seen in both PTU and Methimazole
Agranulocytosis
Causes APLASIA CUTIS CONGENITA if given during 1st trimester
Methimaxole
Emits beta rays causing destruction of thyroid parenchyma
Radioactive iodine
Permanent side effect of RAI
Hypothyroidism
Radiation exposure of thyroid gland may cause
Papillary thyroid Ca
Permanent cure of thyrotoxicosis without surgery
RAI
Contraindications of RAI
Pregnant
Breastfeeding
Inhibits thyroglobulin proteolysis. Used as preparation for surgical thyroidectomy to reduce size and vascularity of thyroid gland
Iodine
Potassium iodine
Lugol’s solution
Potassium iodide saturated solution
Block beta receptors, slows pacemaker activity, inhibits peripheral conversion of T4 to T3
Propanolol
Activation of nuclear receptors results in gene expression with RNA formation and protein synthesis
Levothyroxine
Levothyronine
Liotrix
Prototype glucocorticoid
Hydrocortisone
Glucocorticoid with the highest anti-inflammatory potency
Betamethasone
Glucocorticoid with the highest self-retaining potency
Fludrocortisone
Behavioral changes secondary to steroid use
Steroid rage
Desmolase inhibitor blocking the conversion of cholesterol to pregnenolone
Amino-glutethimide
Glucocorticoid synthesis inhibitor abused by body builders to lower circulating levels of cortisol in the body and prevent muscle loss
Anti-glutethimide
Inhibits cholesterol side-chain cleavage, cytochrome P450 enzymes
Ketoconazole
Alternative to Ketoconazole
Itraconazole
Selective inhibitor of steroid 11-hydroxylation
11-B hydroxylase inhibitor
Metyrapone
Drug of choice for pregnant patients with Cushing’s syndrome
Metyrapone
Used for diagnostic testing for adrenal function
Metyrapone
Competitive inhibitor at GC receptor and progesterone receptor
Mifepristone
Approved abortifacient for medical abortion
Mifepristone
Aldosterone precursor
Deoxycorticosterone
Clear cell vaginal adenocarcinoma in daughters of mothers who took this drug
Diethylstilbestrol (DES)
Progestin used as an appetite stimulant
Megestrol
A synthetic steroid with weak estrogenic, progestognenic, and androgenic activity, and hence is an agonist of the estrogen, progesterone, and androgen receptor. It is primarily used in menopausal hormone therapy, post-menopausal osteoporosis and endometriosis
Tibolone
Activates estrogen and progesterone receptors, inhibits ovulation, effects on cervical mucus gland, uterine tubes, and endometrium lead to decreased fertility
Combined oral contraceptive
Activates progesterone receptors > prevents conception by altering cervical mucus and creating a hostile endometrium
Medroxy-progesterone acetate
Used as emergency contraception / post-coital contraceptive
Levonorgestrel
Ethinyl estradiol + levonorgestrel
Full estrogen receptor antagonist for hormone receptor positive metastatic breast Ca resistant to Tamoxifen
Fluvestrant
Estrogen antagonist that increases bone mineral density and is preferred in patient with history of breast cancer in the management of hot flushes
Raloxifene
Partial agonist of estrogen receptors in pituitary
Clomiphene
Acts as an antagonist to estrogen receptors in the pituitary > inhibit negative feedback mechanism by estrogen > leads to pituitart stimulation causing increase LH and FSH
Reduces estrogen synthesis by inhibiting aromatase thich converts testosterone to estrogen. Used in breast cancers resistant to Tamoxifen
Aromatase inhibitor
ALE
A - anastrozole
L - letrozole
E - exemestane (irreversible inhibitor)
Weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors
Danazol
This type of drugs causes temporary exacerbation of precocious puberty or prostate cancer, apoplexy, and blindness during the irst few weeks of therapy therefore should be co-administered with Flutamide, an androgen receptor antagonists
GNRH agonists
Lueprolide and -relins
Pharmacologic antagonist of glucocorticoid and progesterone receptors
Mifepristone
Androgen receptor antagonist used in prostate cancer and for surgical castration
Flutamide, Bicalutamide, and Nilutamide
Nilutamide (surgical castration)
Inhibits 5a-reductase that converts testosterone to dihydrotestosterone, used in BPH and male pattern baldness
5a-reductase inhibitor
1. Finasteride
2. Dutasteride