Endocrine Pharmacology Flashcards by Tin Hernandez

Hormones from the Anterior Pituitary

GH
Gonadotropins
Prolactin

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Hormones from the Hypothalamus

GnRH

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Hormones from the Posterior Pituitary

Oxytocin

Vasopressin

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GH Inhibitor

Somatostatin

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PRL Inhibitor

Dopamine

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Mediator of GH

IGF-1

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Mediators of TSH

Thyroxine

Triiodothyronine

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Mediators of ACTH

Glucocorticoid
Mineralocorticoid
Androgens

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Mediators of FSH/LH

Estrogen
Progesterone
Testosterone

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Increases release of IGF1

Hormone for GH deficiency, short stature, Failure to thrive, AIDS wasting

Somatotropin

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Drug used for performance enhancement (increases muscle mass), banned by athletics committees

Somatotropin

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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

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In women, FSH directs_____; while FSH and LH collaborate for _________

follicle development

ovarian steroidogenesis

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In men FSH regulates______ and LH stimulates_________.

spermatogenesis

androgen production

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Ovulation induction can cause ovarian hyperstimulation syndrome with the following triad of Sx:

Ovarian Enlargement
Hypovolemia
Ascites
Possibly Shock

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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

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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

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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

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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

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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

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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

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Contraindications to Oxytocin

Fetal distress
Prematurity
Abnormal Presentation
CPD
Predispositions for uterine rupture

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Vasopressin V2 receptor agonist

DOC for Central DI

Desmopressin

Vasopressin

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Sx of Central DI

Polyuria
Polydipsia
Hypernatremia
Inability to resorb water from the urine

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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

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