Endocrine Pharmacology Flashcards
Hormones from the Anterior Pituitary
GH
Gonadotropins
Prolactin
Hormones from the Hypothalamus
GnRH
Hormones from the Posterior Pituitary
Oxytocin
Vasopressin
GH Inhibitor
Somatostatin
PRL Inhibitor
Dopamine
Mediator of GH
IGF-1
Mediators of TSH
Thyroxine
Triiodothyronine
Mediators of ACTH
Glucocorticoid
Mineralocorticoid
Androgens
Mediators of FSH/LH
Estrogen
Progesterone
Testosterone
Increases release of IGF1
Hormone for GH deficiency, short stature, Failure to thrive, AIDS wasting
Somatotropin
Drug used for performance enhancement (increases muscle mass), banned by athletics committees
Somatotropin
Somatostatin analog
Suppresses secretion of GH, IGF1, Serotonin and GI peptides
Drug for acromegaly, pituitary adenoma (GH secreting), carcinoid, gastrinoma, glucagonoma, variceal bleeding
Can alter requirements for antidiabetic agents
Octreotide
Lanreotide
In women, FSH directs_____; while FSH and LH collaborate for _________
follicle development
ovarian steroidogenesis
In men FSH regulates______ and LH stimulates_________.
spermatogenesis
androgen production
Ovulation induction can cause ovarian hyperstimulation syndrome with the following triad of Sx:
Ovarian Enlargement
Hypovolemia
Ascites
Possibly Shock
FSH Analog
Drug for controlled ovarian hyperstimulation, infertility due to hypogonadism in men
SE: Ovarian Hyperstimulation syndrome, multiple pregnancies, gynecomastia in men
Follitropin Alfa
Menotropins (hMG), UROFOLLITROPIN (from urine of menopausal women), Follitropin Beta
LH Analog
Drug for controlled ovarian hyperstimulation, hypogonadotropic hypogonadism
SE: Ovarian hyperstimulation syndrome, multiple pregnancies, gynecomastia in men
Choriogonadotropin Alfa (HUMAN CHORIONIC GONADOTROPIN (hCG), Menotropins (hMG), Lutropin
Increased LH and FSH secretion with intermittent administration, reduced LH and FSH with continuous administration
Drug for Controlled ovarian hyperstimulation, endometriosis, myoma uteri, precocious puberty, prostate cancer
SE: Hot flushes, osteoporosis, gynecomastia, temporary exacerbation of precocious puberty or prostate cancer
Leuprolide
LAHAT NG -RELIN
GnRH Antagonist
Drug for Controlled Ovarian Hyperstimulation, Prostate Cancer
SE: Hypersensitivity (Abarelix)
Does not cause tumor flare up when used for prostate cancer
Ganirelix
LAHAT NG -RELIX
Partial D2 receptor agonist
Inhibits GH release
Drug for hyperprolactinemia, Pituitary adenoma (PRL secreting), acromegaly, Parkinson’s
SE: Erythromelalgia, Reynaud’s Phenomenon, Pulmonary infiltrates
Bromocriptine
Pergolide, Carbergoline, Quinagolide
Stimulates uterine contraction and labor
Stimulates milk letdown
Drug for labor induction/augmentation, control of postpartum hemorrhage
SE: Fetal distress, placental abruption, uterine rupture, water intoxication, hypotension
Oxytocin
Contraindications to Oxytocin
Fetal distress Prematurity Abnormal Presentation CPD Predispositions for uterine rupture
Vasopressin V2 receptor agonist
DOC for Central DI
Desmopressin
Vasopressin
Sx of Central DI
Polyuria
Polydipsia
Hypernatremia
Inability to resorb water from the urine
Central DI: deficient _________ of ADH
Nerphrogenic DI: end-organ ________ to ADH
Secretion
Resistance
Antagonist at V1a and V2 receptors
Drug for SIADH
Central Pontine Myelinosis may occur with rapid correction of hyponatremia
Conivaptan
Tolvaptan, Lixivaptan
T3 is about ______ times more potent than T4
10
T___ is converte to T____ in target cells
T4 to T3
Identify if Thyrotoxicosis or Hypothyroidism: Weakness Increased DTR Menstrual Irregularity Decreased Fertility
Thyrotoxicosis
Identify if Thyrotoxicosis or Hypothyroidism: Stiffness Decreased DTR Infertility Decreased Libido Impotence Oligospermia
Hypothyroidism
Thyroid hormone
Activation of nuclear receptors
Drug for Hypothyroidism, Myxedema Coma
SE: Dry skin, nervousness, heat intolerance
Levothyroxine (T4)
Liothyronine (T3)
T4 dose must be lowered in pxs with __________ or longstanding __________ due to increased cardiosensitivity
Cardiovascular disease
Hypothyroidism
Thioamide
Inhibits Thyroid peroxidase
Blocks peripheral conversion of T4 to T3
Drug for Hyperthyroidism (esp in Pregnant), Thyroid Storm
SE: Fulminant hepatitis, Agranulocytosis
Slow onset of action (3-4 weeks for full effect)
Largely protein bound
PTU
Thioamide
Inhibits Thyroid peroxidase, blocks iodine organification
Drug for hyperthyroidism (DOC in nonpregnant)
SE: Cholestatic jaundice, agranulocytosis
altered sense of taste/smell
Slow onset of action (3-4 weeks for full effect)
Methimazole
Prenatal exposure to Methimazole can lead to this condition
Aplasia Cutis Congenita
Absence of a portion of skin in a localized or widespread area at birth
Sx of Agranulocytosis
Acute severe neutropenia
sore throat or high fever
increased susceptibility to infections
Tx for Agranulocytosis
Give G-CSF to stimulate body to make more WBC
Discontinue medication
Iodide
Emits beta rays causing destruction of thyroid parenchyma
Hyperthyroidism
SE: Permanent hypothyroidism
Preferred treatment for most patients
Contraindicated in pregnant women or nursing mothers
Radioactive Iodine 131I
Iodide
Inhibits iodine organification, reduces size and vascularity of thyroid gland
Drug for thyroid storm, hyperthyroidims, preop thyroidectomy, radiation prophylaxis
SE: Iodism, metallic taste
Prevents radiation induced thyroid damage
Should not be used alone (escape in 2-8weeks)
Potassium Iodide
Lugol’s Solution
Prenatal exposure to Potassium Iodide can cause _____
Fetal Goiter
Identify: Ingestion of Iodine causes Hypothyroidism
Wolf-Chaikoff Effect
Identify: Ingestion of Iodine causes Hyperthyroidism
Jod-Basedow Effect
This drug causes clinical improvement of hyperthyroidism without altering thyroid hormone levels
Class?
Beta Blockers
This beta blocker may be used to treat thyrotoxicosis-related arrhythmia
Esmolol
Enumerate the anti-thyroid drugs that inhibit peripheral conversion of T4 to T3
Propylthiouracil Propranolol Hydrocortisone Contrast with Iodine Methimazole
Granulocyte count of <500cells/mm3
Sudden acute exacerbation of all the symptoms of thyrotoxicosis
Thyroid Storm
Tx of Thyroid Storm
PTU (inhibits conversion of iodide to iodine)
Iodides
Propranolol
Hydrocortisone (protects against shock)
Drugs that can induce Hyperthyroidism
Clofibrate
Amiodarone (can convert T4 to T3, or iodine induced in a person with underlying thyroid disease, or inflammatory causing leakage of thyroid hormone)
Methadone
CAM
Tx for Amiodarone induced Thyroid Disease due to Peripheral Conversion
Levothyroxine
Tx for Amiodarone induced Thyroid Disease due to Iodine-induced mechanism in those with underlying thyroid disease or inflammatory causing leakage of thyroid hormone
Thioamides (PTU/Methimazole)
Corticosteroids
Common Precursor of Corticosteroids
Cholesterol
Short-acting, low potency glucocorticoid
Suppresses inflammation
Drug for adrenal insufficiency, insect bites, contact dermatitis, status asthmaticus, thyroid storm
Hydrocortisone
Low Potency: Desonide
Medium Potency: Fluticasone, Mometasone
High Potency: Desoximetasone, Clobetasol
Glucocorticoid
SE: Adrenal SUPPRESSION
Prednisone
Betamethasone, Triamcinolone, Dexamethasone
This glucocorticoid hastens fetal lung maturation
Betamethasone
Mineralocorticoid
Strong agonist, moderate anti-inflammatory effects
Drug for chronic adrenal insufficiency (Addison’s Disease), Congenital Adrenal Hyperplasia, Adrenal Replacement Therapy Post-Adrenalectomy
SE: Salt and fluid retention, HypoK, Congestive HF
Additive HypoK with Loop diuretics and thiazides
Fludrocortisone
Deoxycorticosterone
Destruction or dysfunction of entire adrenal cortex
Ususally symptomatic only with >90% destruction
Addison Disease
Adrenal Insufficiency is what syndrome?
Addison
ADDrenal insuficiency
Adrenal Excess is what syndrome?
Conn
exCess
Most common cause of Iatrogenic Cushing Syndrome
Exogenous Steroid Intake
Most common cause of Adrenal Cushing Syndrome
Cortisol Secreting Adrenal Adenoma
Most common cause of Pituitary Cushing Syndrome
ACTH-secreting Pituitary Adenoma
Most common cause of Ectopic Cushing Syndrome
Paraneoplastic ACTH production from lung tumors
Glucocorticoid Synthesis Inhibitor
Inhibits DESMOLASE, blocking conversion of cholesterol to prenenolone
Drug for breast cancer, cushing syndrome
Abused by body builders to lower circulating cortisol in the body and prevent muscle loss
Aminoglutethamide
Glucocorticoid synthesis inhibitor, Antifungal
Inhibits cholesterol side chain cleavage
Drug for fungal infection
SE: Hepatotoxicity, Gynecomastia, GI disurbances
Inhibitor of CYP450
Ketoconazole
Glucocorticoid Synthesis Inhibitor
Inhibits 11-hydroxylation
Drug for diagnostic testing, Cushing syndrome
DOC for pregnant patients with cushing’s syndrome
Metyrapone
This hormone derived from horses is used for HRT
Premarin
Estrogen
SE: Breakthrough bleeding, breast tenderness, HyperTG, HPN
Increases risk for endometrial CA and breast CA (prevented by combining with progestin)
Ethinyl Estradiol
Mestranol, Estradiol Cypionate
Synthetic estrogen (nonsteroid) Drug for metastatic prostate cancer SE: Increased incidence of Clear Cell Adenocarcinoma in daughters of mothers who took this drug
Diethylstilbestrol
Progestin
SE: Decreased HDL, Weight gain, Reversible decrease in bone mineral density
Prevents estrogen induced endometrial cancer when used in combination
Norgestrel
(Megestrol, Ethynodiol, Desogestrel, Etonogestrel)
LAHAT NG MAY NOR-
Type of Oral Contraceptive:
Taken in constant dosage
Monophasic
Progestin or Estrogen Dosage changes during the month
Biphasic or Triphasic
Contraceptives may be given within ______ hours after unprotected intercourse
72hours
MOA of Combination Hormonal Contraceptives
Inhibition of Ovulation
COC
Activates estrogen and progesterone receptors
SE: Breakthrough bleeding, DVT, Breast CA
Estradiol + Norethindrone
(Ethinyl Estradiol PLUS: Desogestrel/Norgestrel, Drospirenone, Norgestimate
Does not protect against STDs
Pills
POP
Alters cervical mucus and creates a hostile endometrium
SE: Breakthrough bleeding, Delayed return of fertility, Osteoporosis
Medroxyprogesterone Acetate
IM preparation (Depo-provera)
Post coital contraceptive
SE: Severe nausea, dizziness
Must be taken within 72 hours of unprotected sexual intercourse
Levonorgestrel
_____ Regimen is for emergency contraception
Yuzpe
4 tabs OCP then 4 tabs again after 12 hours
Mixed estrogen agonists that have agonist effects in some tissues and antagonists in others
Class?
SERMs
Estrogen antagonist in breast tissue and CNS
Estrogen agonist in uterus
Drug for Hormone Responsive Breast CA (ER+/PR+)
Prevents osteroporosis and decreases risk of atherosclerosis at the risk of causing endometrial CA
Drug?
Tamoxifen
TAnggal Mammary Mo = TAMOxifen
Estrogen Antagonist in Breast, Uterus and CNS
DDrug for Osteoporosis and Breast CA PREVENTION
Reduces risk of Breast CA in those who are VERY HIGH RISK
No estrogenic effects on endometrial tissue
Raloxifene
Partial estrogen agonist in pituitary Reduces negative feedback by estradiol Increases FSH and LSH output Drug for induction of Ovulation SE: Ovarial enlargement, multiple pregnancies
Clomiphene
Clone Me Phlease
Aromatase inhibitor
Drug for Breast CA, Precocious puberty
Effective to tamoxifen resistant Breast CA
Anastrozole
(Letrozole, Exemestane)
Aromatase inhibits Testosterone to Estrogen
Partial agonist of Progestin and Androgen receptors
Drug for Endometriosis, Fibrocystic disease
SE: Weight gain
Contraindicated during pregnancy and breast-feeding
Danazol
Anti-androgen
Antagonist of glucocorticoid and progesterone receptors
Drug for medical abortion
Combination with Misoprostol results in abortion of 95% of early pregnancies
May cause sepsis from unusual organisms
Mifepristone (RU-486)
Organisms like Clostridium Sordeli
Active form of Testosterone in Prostate
DHT
DIhydrotestosterone
Stimulate RBC production in certain anemias
Promotes weight gain
Performance enhancement in athletes
Drug?
Testosterone
Androgen
Increases muscle bulk and RBC production
Drug for male hypogonadism, wasting syndromes in AIDS
SE: Virilization in females, paradoxical feminization in males
Contraindicated in pregnant women and patients with prostate cancer
Testosterone
LAHAT NG MAY -TERONE
Anabolic steroid androgen
Increases ratio of anabolic to androgenic activity
Drug for performance enhancement
SE: Virilization in females, Paradoxical feminization in males, Cholestatic jaundice, Elevated liver enzymes, HCC
Oxandrolone
LAHAT NG MAY -ANDROLONE
Androgen antagonist
Drug for prostate cancer (prevention of acute flare up), surgical castration (Nilutamide)
Flutamide
(Bicalutamide, Nilutamide)
Fake Androgen: Flutamide
Less hepatotoxicity with which androgen antagonists?
Bicalutamide
Nilutamide
Must be co-administered with Leuprolide to prevent prostate cancer flare up
Flutamide
Fake Androgen: Flutamide
Androgen antagonist
Drug for hirsutism, decreases sexual drive in men
Currently an orphan drug
Cyproterone
Cyproterone Acetate
Androgen synthesis inhibitor
Inhibits 5alpha-reductase converting testosterone to DHT
Drug for BPH, male pattern baldness, hirsutism
SE: Impotence
Controversial use in prostate cancer
Finasteride
LAHAT NG -ASTERIDE
FinAsteRIde: Five Alpha Reductase Inhibitor
C peptide is used to:
differentiate Type 1 and Type 2 DM
Diagnose MEN
Rule out factitious hypoglycemia
Assess insulin resistance
MOA of Insulin
Binds to tyrosine kinase receptor
Activates phosphatidylinositol-3-kinase and MAP kinase
Translucation of glucose transporters
Rapid Insulin, duration is 3-4 hours
Lispro
Aspart
Glulisin
mabiLIS!
Short Acting Insulin, duration is 5-7 hours
Regular
Intermediate-Acting Insulin, duration is 18-24 hours
NPH
Lente
Long-Acting Insulin, duration is 18-24 hours
Ultralente
Ultralong Acting Insulin, duration is >24 hours
Glargine : go LARGe!
Detemir
Lantus: LANTa na sa sobrang tagal
Paradoxical improvement f Diabetes in ESRD is due to?
Prolonged half-life of insulin due to decreased clearance
These symptoms are results of CNS deprivation
Neuroglycopenic Symptoms
Thes symptoms are results of CNS mediated sympathoadrenal discharge
Neurogenic (or Autonomic) Symptoms
Patients who are more prone to developing hypoglycemia with insulin:
Advanced renal disease
Elderly
Children below 7 years
Identify Effect and Tx:
Evening dose is High
3AM is low
7AM is high
Somogyi
Decrease Insulin
Identify Effect and Tx:
Evening dose is Low
3AM is high
7AM is high
Waning
Increase Insulin
Identify Effect and Tx:
3AM is Normal
7AM is high (mild)
Dawn Phenomenon
Insulin sensitivity becomes low between 6am and 7am due to GH spike
Identify Effect and Tx:
Evening dose is High
3AM is high
7AM is higher
Waning + Dawn Phenomenon
Increase Insulin
Period when exogenous insulin requirements decrease due to an increase in endogenous production of insulin
This is followed by a TOTAL LACK of endogenous insulin
Honeymoon Period
Most physiologic strategy for Insulin Therapy
Basal Bolus
Long acting BASAL + Short acting BOLUS with every meal
Amount of short-acting insulin is varied depending on pre-prandial CBG
Sliding Insulin Scale
Only routes for administration of Insulin
Subcutaneous
IV
Inhalational seems promising
MOA of insulin Secretagogues
closure of K channels in Pancreatic B cell membrane
Not effective in Pxs who lack functional pancreatic B cells
Requires Islet Cell Function
1st Generation Sulfonylurea
SE: Hypoglycemia, Weight Gain, Disulfiram Reaction, Dilutional Hyponatremia
Drugs that compete for protein binding may enhance hypoglycemic effects
Requires islet cell function
Chlorpropamide
LAHAT NG -AMIDE
Except Gibenclamide
2nd Generation Sulfonylurea
SE: Hypoglycemia (less), Weight Gain, Cholestatic Jaundice (Glibenclamide)
Contraindicated with hepatic impairment and renal insufficiency
Requires Islet cell function
Glipizide
LAHAT NG GLI-
Meglitinide
Insulin Secretagogue
For Postprandial hyperglycemia
SE: Hypoglycemia (least), Upper Respiratory Tract Infections
Used in Diabetics with Sulfa Allergies
Nateglinide has the least Incidence of hypoglycemia and may be used in CKD patients
Requires islet cell function
Repaglinide
LAHAT NG -GLINIDE
MOA of Biguanides
Reduces fasting and postprandial glucose levels
inhibition of hepatic and renal gluconeogenesis
stimulates glucose uptake and glycolysis in peripheral tissues
First line for T2DM (esp Obese)
Inhibits hepatic and renal gluconeogenesis
SE: Weight loss, Lactic acidosis, Vit B12 malabsorption
Contraindicated in pxs with renal disease, alcoholism, hepatic disease, or conditions with tissue anoxia
Metformin
MOA of Thiazolidinediones
Increases target tissue sensitivity to insulin
Reduces fasting and post-prandial glucose
Increases glucose uptake in muscle and adipose
Inhibits hepatic gluconeogenesis
Thiazolidinedione
Regulates gene expression, binds to PPAR-gamma
SE: Fluid retention, congestive heart failure, Dec HDL, Inc LDL, Inc TG
Contraindicated in pregnancy, chronic liver disease, Congestive heart failure
Pioglitazone
LAHAT NG -GLITAZONE
Anti-diabetes drug that reduces mortality and macrovascular events (MI/Stroke)
Pioglitazone
MOA of Alpha Glucosidase Inhibitors
Important for the conversion of complex carbs to monosaccharides
Reduction of post-prandial hyperglycemia
Lacks an effect on Fasting Blood Sugar
Reduces risk of Diabetes on High Risk Pxs
Inhibits Intestinal Alpha Glucosidases
Drug for Diabetes prevention
SE: GI disturbance, Flatulence, Hypoglycemia with sulfonylureas
Minor glucose lowering benefit
Contraindicated in pxs with renal impairment
Acarbose
(Miglitol, Voglibose)
Adjunct therapy only
Novel Diabetic Agents
Pramlintide
Exenatide
Sitagliptin
Amylin analog
Suppresses glucagon release, delays gastric emptying, reduces appetite
Administered as injectable solution with insulin
Pramlintide
Incretin modulator, GLP-1 Agonist
Retards Gastric Emptying, Inhibits glucagon secretion, Produces SATIETY
SE: Hypoglycemia
Administered as an injectable preparation used in combination with metformin or a sulfonylurea
Exenatide
Incretin modulator, DPP-4 Inhibitor (degrades GLP1)
Administered orally as monotherapy or in combination with metformin
Sitagliptin
Inhibits GI and pancreatic lipase, reduces fat absorption
Drug for Obesity and T2DM
SE: Weight loss, Steatorrhea
Rebound weight gain, contraindicated in pregnancy, malabsorption
Orlistat
Inhibits NE and serotonin reuptake in the CNS, reduces appetite
Drug for Obesity
SE Anticholinergic effects
Withdrawn due to increased risk of cardiovascular events and strokes
Sibutramine
Reductil
Selectively blocks cannabinoid 1 receptors, reduces appetite
Drug for Obesity
SE: Suicidality, depression, nausea
Withdrawn due to increased risk of suicides, depression
Rimonabant
Contents of Bangkok Pills and adverse effect
Ephedrine
Fenfluramine
Phentermine
Adverse effect: Valvular Heart Disease
MOA of Glucagon
Catabolic
Increases heart rate and force of contraction
increases hepatic glycogenolysis and gluconeogenesis
Relaxes smooth muscles
Activates glucagon receptors
Drug for severe hypoglycemia, beta blocker overdose
Glucagon
These tumors present with decreased AA in blood, anemia, diarrhea, weight loss and NECROLYTIC MIGRATORY ERYTHEMA
Glucagonoma
MOA of PTH
Increase bone turnover, hypercalcemia, hyperphosphatemia
This electrolyte regulates the synthesis and secretion of PTH
Free Ionized Calcium
Recombinant PTH
Drug for Osteoporosis
Must be administered in low intermittent dses to stimulate bone formation
Teriparatide
Sx of excess Parathyroid Hormone
Painful bones
Renal stones
Abdominal groans
Psychiatric overtones
Effect of PTH on Phos
Phosphate
Thrashing
Hormone
IIndirectly increases calcium and phosphate absorption in the intestine via Increasing Vit D metabolites
Decreased calcium excretion, increase Phos excretion in the kidne
Increased Ca and Phos resorption in bone
Serum calcium increased, serum phosphate decreased
PTH
Increased calcium and phosphate absorption
Increased resorption of calcium
Increase Ca and Phos resorption, promoting mineralization
Serum Ca and Phos both increased
Active Vit. D Metabolytes
Inactive Vit D
Stimulates INtestinal Ca absorption, bone resorption, renal Ca and Phos reabsorption
Drug for Vit D deficiency
This is added to dairy products
Ergocalciferol
LAHAT NG -CALCIFEROL
Active Vit D
Drug for secondary hyperparathyroidism in CKD, Psoriasis
This is required in CKD, liver disease and hypoparathyroidism
Calcitriol
Hormone secreted by Parafollicular C cells in the Thyroid Gland
Decreases Serum Ca and Phos by inhibiting bone resorption and inhibiting renal excretion of Ca and Phos
Calcitonin
Tones down Calcium, Reverses PTH
Drug for Paget Disease of Bone, Hypercalcemia, Osteoporosis, Tumor marker of thyroid cancer
Given as nasal spray
Calcitonin
LAHAT NG - TONIN
Excessive bone resorption leading to formation of weaker bones
Paget Disease of Bone
Bisphosphonate
Suppresses Osteoclast activity
Drug for Paget disease of bone, hypercalcemia, osteoporosis
SE: Adynamic bone, Esophagitis, Osteonecrosis of the jaw
Alendronate
LAHAT NG -DRONATE / -DRONIC ACID
Take this drug with large quantities of water
Contraindicated in renal impairment, esophageal motility disorder and PUD
Alendronate
Phosphate binding resin
Binds to dietary phosphate and prevents absorption
Drug for hyperphosphatemia in CKD
Can reduce Uric Acid levels
Contraindicated in HYPOphosphatemia and bowel obstruction
SEVELAMER
Tablets rapidly expand