Endocrine Drugs Flashcards
What drug is used in management of short stature that acts by increasing release of IGF-1 in the liver and cartilage, stimulating skeletal muscle growth, amino acid transport, protein synthesis and cell proliferation?
Somatropin
Growth hormone
What drug is used as performance-enhancing drug that is banned by athletic committees?
Somatropin
What is the somatostatin analog used in treatment for acromegaly, pituitary adenoma, carcinoid, gastrinoma, glucagonoma, variceal bleeding?
Octreotide
Drug used to activate FSH receptors for controlled ovarian hyperstimulation and for management of infertility due to hypogonadism in men
Follitropin Alfa
LH analog
Choriogonadotropin alfa
HCG
Menotropins
Lutropin
GnRH analog which increases LH and FSH with intermittent administration and reduces LH and FSH with prolonged continuous administration.
Used for the treatment of endometriosis, myoma uteri, precocious puberty and prostate cancer
Leuprolide
GnRH antagonist used in prostate cancer and prevention of premature LH surge
Ganirelix Cetrorelix Abarelix Degarelix Note: does not cause a tumor flare up when used for treatment of advanced prostate cancer
Dopamine agonist but a partial agonist at dopamine D2 receptors in the brain to inhibit prolactin release
Bromocriptine
Pergolide
Carbergoline
Quinagolide
What is the side effect of bromocriptine other than erythromelalgia and pulmonary fibrosis?
raynaud phenomenon
What is the drug of choice for treatment of pregnant hyperthyroid patients which has a slow onset of action (3-4 weeks to take full effect)
Propylthiouracil
Drug class: Thioamide
What is the mechanism of action of propylthiouracil?
It inhibits thyroid peroxidase reactions
It inhibits iodine organification and peripheral conversion of T4 and T3
What is the treatment of choice for Myxedema coma (progressive weakness, stupor, hypothermia, hypoventilation, hypoglycemia, hyponatremia, water intoxication, shock and death due to severe hypoglycemia)
IV loading dose of Levothyroxine 300-400 mcg
What are the side effects of Propylthiouracil?
Agranulocytosis, Urticaria, Fulminant Hepatitis, Lupus-like syndrome, vasculitis, Hypoprothrombinemia, Exfoliative dermatitis, Polyserositis, Arthralgia
Prenatal exposure to Methimazole results to?
Aplasia cutis congenita
What is the treatment that reduces the size and vascularity of thyroid gland. MOA includes inhibiting iodine organification and hormone release?
Lugol’s solution
Potassium Iodide
What do you call the phenomenon in which the ingestion of iodine causes hypothyroidism?
Wolf-Chaikoff effect
What do you call the phenomenon in which the ingestion of iodine causes hyperthyroidism?
Jod-Basedow effect
What is the drug that cause clinical improvement without altering thyroid hormone levels. It inhibits peripheral conversion of T4 and T3
Propranolol
What are the three drugs that inhibits peripheral conversion of T4 to T3
Propylthiouracil
Propranolol
Hydrocortisone
What is the drug of choice for thyroid storm?
Propylthiouracil then Iodides to retard release of thyroid hormones
Give three drugs that induces hyperthyroidism?
Clofibrate
Amiodarone
Methadone
What drug induces hypo and hyperthyroidism?
Amiodarone
- Has the ability to block the peripheral conversion of T4 to T3 (Tx: Levothyroxine)
- Iodine induced mechanism in persons with an underlying disease or through an inflammatory mechanism that causes leakage of thyroid hormone
(tx: Thioamides or corticosteroids)
What glucocorticoid synthesis inhibitor that inhibits desmolase and reduced synthesis of all hormonally active steroids used in the treatment of breast cancer and cushing syndrome?
Aminogluthemide
Note: Used by body builders to lower circulating levels of cortisol in the body and prevent muscle loss
Which among the azole antifungals inhibits cholesterol side-chain cleavage, cytochrome P450 and other enzymes necessary for synthesis of all steroids? Used in the treatment of adrenal carcinoma, hirsutism, breast cancer, prostate cancer, cushing’s syndrome and fungal infections
Ketoconazole
What glucocorticoid synthesis inhibitor that selectively inhibits steroid 11-hydroxylation used in the diagnostic testing for Cushing’s syndrome? This is also the drug of choice for pregnant patients with cushing’s syndrome
Metyrapone
Examples of progestins
Norgestrel Norethindrone Ethynodiol Megestrol Desogestrel Norelgestromin Norgestimate Etonorgestrel
What are the side effects of progestins?
Decreased HDL and Weight gain
What progestin is used as an appetite stimulant
Megestrol
What is the drug used as an emergency contraception
Levonorgestrel
YUZPE regimen
What is the drug used as a progestin-only pill?
Medroxyprogesterone acetate
IM: Devo-Provera
What is the selective estrogen receptor modulator (SERM) that has an antagonistic effect on the breast tissue and CNS but has an agonist effect in uterus, liver and bone?
Tamoxifen
Toremifene
Side effect of tamoxifen
Increases the risk of endometrial cancer
Note: It prevents osteoporosis and decreases risk of atherosclerosis
SERM that has an antagonist effect in breast tissue, uterus and CNS but has an agonistic effect on the liver and bone. Used in the prevention of breast cancer and increases bone mineral density
Raloxifene
Note: no estrogenic effcts on endometrial cancer
SERM which has a partial agonist in the pituitary. Reduces negative feedback by estriol and Increases FSH and LH output. Used in induction of ovulation
Clomiphene
Note: increases risk of low-grade ovarian cancer with long-term use
Estrogen synthesis inhibitors which acts by inhibiting aromatase and used in the treatment of breast cancer and precocious puberty. Effective in breast cancer which becomes resistant to Tamoxifen
Anastrozole
Letrozole
Exemestane
Antiandrogen that acts as a weak cytochrome P450 and partial agonist of progestin and androgen receptors used in the treatment of endometriosis, fibrocystic disease, hemophilia, angioneurotic edema
Danazol
What are the side effects of danazol
Weight gain
Hirsutism
Note: Contraindicated during pregnancy and breast feeding
What drug is a glucocorticoid receptor antagonist and progesterone receptor used in medical abortion and treatment for Cushing’s syndrome
Mifepristone (RU-486)
What drug activates androgen receptors and is used as an illegal performance enhancement drug in atheletes
Oxandrolone
What is an androgen competitive antagonist which is used in the treatment of prostate cancer and in surgical castration?
Flutamide
Bicalutamide
Nilutamide (surgical castration)
Which drug should be administered with flutamide to avoid tumor-flare up in prostate cancer?
Leuprolide
Which androgen antagonist that has a marked progestational effect that suppresses the feedback enhancement of LH and FSH? It has an orphan drug status and is used for treatment of hirsutism and it decreases sexual drive in men
Cyproterone
What is the androgen synthesis inhibitor that acts by inhibiting 5-alpha reductase and is used in the treatment for BPH
Finasteride
Dutasteride
Examples of Rapid acting Insulins
Lispro
Aspart
Glulisine
What is an androgen competitive antagonist which is used in the treatment of prostate cancer and in surgical castration?
Flutamide
Bicalutamide
Nilutamide (surgical castration)
Which drug should be administered with flutamide to avoid tumor-flare up in prostate cancer?
Leuprolide
Which androgen antagonist that has a marked progestational effect that suppresses the feedback enhancement of LH and FSH? It has an orphan drug status and is used for treatment of hirsutism and it decreases sexual drive in men
Cyproterone
What is the androgen synthesis inhibitor that acts by inhibiting 5-alpha reductase and is used in the treatment for BPH
Finasteride
Dutasteride
Example of Short acting insulin
Regular Insulin (Humalog)
Examples of Intermediate acting insulin
NPH
Lente
Example of Long acting insulin
Ultralente
Examples of ultra-long acting insulin
Glargine
Detemir
Lantus
Happens when the evening dose of intermediate insulin is high and hypoglycemia develops around 3:00 AM. As a result, counter-regulatory hormones are produced, resulting in pre-breakfast hyperglycemia
Somogyi effect
When the evening dose of intermediate insulin is low, hyperglycemia will be present both at 3:00AM and 7:00 AM
Waning of insulin dose
Insulin sensitivity becomes low between 6:00 AM and 7:00 AM due to the growth hormone spike. As a result, mild hyperglycemia occurs in the early morning but the 3:00 Am glucose levels will be normal.
Dawn Phenomenon
Increases insulin secretion from pancreatic beta cells by closing ATP sensitive K+ channels
Sulfonylureas
Examples of 1st generation Sulfanylurea
Chlorpropamide
Tolbutamide
Tolazamide
Examples of 2nd generation Sulfanylureas
Glipizide Glimepiride Glyburide Glibenclamide Gliclazide
Which class of drugs that increases target tissue sensitivity to insulin by activating the peroxisome proliferator receptor gamma nuclear receptor (PPAR-gamma)? This reduces fasting and postprandial hypoglycemia
Thiazolidenedione
(Pioglitazone, Troglitazone, Rosiglitazone)otoxicity
Which class of antidiabetics acts as an insulin secretagogue but is used in postprandial hyperglycemia and in patients with sulfa allergies
Class: Meglitinide
Repaglitinide, Nateglinide, Mitiglinide
Which among the meglitinides has the least incidence of hypoglycemia and may be used in CKD patients?
Nateglinide
Which class of antidiabetics that activates AMP-stimulated protein kinase leading to inhibition of hepatic and renal gluconeogenesis? This reduces postprandial and fasting glucose levels.
Biguanides (Metformin)
Which class of drugs that increases target tissue sensitivity to insulin by activating the peroxisome proliferator receptor gamma nuclear receptor (PPAR-gamma)? This reduces fasting and postprandial hypoglycemia
Thiazolidenedione
What are the side effects of thiazolidenediones
Fluid retention, weight gain, CHF, macular edema and dyslipidemia
What is an incretin modulator that inhibits dipeptidyl peptidase-4 that degrades GLP-1 and other incretins
Sitagliptin
What thiazolidenedione reduces mortality and macrovascular events?
Pioglitazone
What drug is an amylin analog that suppresses glucagon release, delays gastric emptying, stimulates CNS to reduce appetite (anorectic effect)?
Pramlintide
What is an incretin modulator (GLP-1 agonist) that augments glucose-stimulated insulin release from pancreatic B cells, retards gastric emptying and inhibits glucagon secretion, and produces satiety?
Exenatide
What is an incretin modulator that inhibits dipeptidyl peptidase-4 that degrades GLP-1 and other incretins
Sitagliptin
What antiobesity drug that inhibits gastrointestinal and pancreatic lipases and reduces absorption of fats
Orlistatn
Side effects of orlistat?
steatorrhea
rebound weight gain upon discontinuation
What antiobesity drug that inhibits norepinephrine and serotonin reuptake in the CNS and reduces appetite?
Sibutramine
Note: withdrawn due to increased risk of cardiovascular events and strokes
What antiobesity drug that selectively blocks cannabinoid-1 (CB-1) receptor that reduces appetite and is used in obesity, smoking cessation and drug addiction?
Rimonabant
What thyroid hormone acts as a calcitonin and is administered as a nasal spray
Salcitonin
Example of a recombinant parathyroid hormone
Teripatide
Inactive form of Vitamin D
Ergocalciferol
Cholecalciferol
What drug is an active Vitamin D used in the treatment of psoriasis
Calcipotriene
What thyroid hormone acts as a calcitonin and is administered as a nasal spray
Salcitonin
Examples of bisphosphanates
Alendronate Etidronate Ibandronate Pamidronate Risedronate Tiludronate Zoledronic acid
What are the side effects of bisphosphanates
Adynamic bone
Esophagitis
Osteonecrosis of the jaw
Renal impairment
Phosphate binding resin which is used in the treatment for hyperphosphatemia in CKD, Hypoparathyroidism, Vitamin D intoxication
Sevelamer
What is one of the effects of phosphate binding resins
Can significantly reduce uric acid levels
