Gopal Flashcards
Spironolactone
Steroid; competitive antagonist; blocks androgen receptor. Decreases testosterone and aldosterone and DHEA. treats Hirsutism (women with facial hair) & prostate cancer. Also manages primary hyperaldosteronism & hypertension.
*RECEPTOR ANTAGONIST
Leuprolide
GnRH analogue; PEPTIDE; desensitizes receptors on the surface of the anterior pituitary. Decreases Gonadotropin (FSH/LH) release. INITIAL FLARE. Treat prostate cancer and endometriosis.
Abarelix
synthetic GnRH ANTAGONIST; PEPTIDE; No initial Flare. Treat prostate cancer & endometriosis.
Finasteride
steroid; DHT blocker. inhibits 5a-reductase. Stops conversion of Testosterone to DHT. Treats prostate cancer and Hirsutism.(«_space;mostly)
Flutamide
non-steroid anilide; blocks the action of testosterone. is Hepatotoxic. Synergistic with Leuprolide and causes NO FLARE. Treats Prostate cancer (with Leuprolide)
Cyproterone
Antiandrogenic Steroid; Potent Progestin. Blocks DHT receptor. (like flutamide) Treats Hirsutism. Mostly Decreases Libido & Aggressiveness in SEX OFFENDERS.
Clomiphene
NON-PEPTIDE/NON-STEROID; Antiestrogen. Increases FSH/LH
Tamoxifen
Non-steroid SERM; Blocks E2 Receptor - treats Breast Cancer.
Raloxifene
Non-steroid SERM; Postmenopausal Osteoperosis
Fulvestrant
Steroid; competitive E2 Antagonist. Treats Breast Cancer
Mifepristone
Steroid; Progesterone/Cortisol Competitive Antagonist; Treats Cushing’s Syndrome. ABORTIFACIENT
*RECEPTOR ANTAGONIST
Testosterone
Steroid; maturation of sex organs. Treas Hypogonadism, Osteoporosis and trauma patients to decrease protein loss . (anabolically rebuild)
Can cause Acne or hepatic Dysfunction (jaundice)
Cretinism
Hypothyroidism in children; mental retardation due to deficient thyroid hormone. (NO MYELINATION)
Hypothyroidism
Low T4 & High TSH
Hyperthyroidism
High T4 & Low TSH
Hashimoto’s disease (primary hypothyroidism)
Primary Hypothyroidism (most common) autoimmune destruction of thyroid cells. High TRH and TSH but low T3 and T4. GOITER. Person is RUNDOWN.
Goiter
lack of iodine
Secondary Hypothyroidsim
anterior pituitary failure; lack of TRH and TSH
Dwarfism
growth hormone deficient.
Myxedema
Hypothyroidism - dry waxy swelling of the skin. NON-PITTING EDEMA. (non persistant indentation)
Levothyroxine
Synthetic T4; hormone replacement to treat all forms of HYPOTHYROIDISM. Converted to its active form in vivo. Due to cardiovascular effects, lower doses should be given to OLDER PATIENTS
Graves’ Disease
abnormal productions of TSI (thyroid stimulating immunoglobulin) TSH is low but TSI mimics TSH and causes overstimulation. GOITER. The person is HIGH STRUNG.
Iatrogenic hyperthyroidism
caused by overdose of (levothyroxine)T4/T3 from hyperthyroidism. Iatrogenic = from previous treatment.
Thyroid storm
severe acute thyrotoxicosis; in HYPERTHYROID patients and can be invoked by stress, surgery, and trauma. LIFE THREATENING
Iodide Salt
Antithyroid agent; inhibits iodination of tyrosine and thyroid hormone release. (SHORT TERM) - before surgery
Treats HYPERTHYROIDISM
Iodinated Radiocontrast Media (IRM)
Suppresses T4-T3 conversion. Gives visual of thyroid.
Radioactive Iodine Therapy (RAI)
uses 131-I (radioiodine) for the destruction of thyroid tissue. MOST POPULAR for thyroid removal. Emits Beta particles. PERMANENT CURE without SURGERY. After treatment iodide salts inhibit the thyroid hormone release. NOT USED IN PREGNANT WOMEN.
Thyroidectomy
surgery; reduce functional tissue mass.
Beta-blockers (treat Hyperthyroidism)
inhibit hypersympathetic function of hyperthyroidism.
Anti-thyroid agents
Propylthiouracil(PTU) and methimazole that inhibit synthesis of T3 and T4.
Inhibit Peroxidase (blocks coupling and iodination)
PTU also inhibits T4 to T3 in the periphery! **
Treat Graves disease
Can cause AGRANULOCYTOSIS or VASCULITIS
PTU (propylthiouracil)
ANTI Hypertensive; also inhibits T4 to T3 in the periphery! (better than methimazole) Treats Graves disease
can cause Agranulocytosis(low WBC count) or Vasculitis & Crosses Placenta and enters Breast Milk (causing cretinism)
What might happen if we treated a pregnant woman aggressively with thiourea - PTU?
fetus could develop cretinism from the lack of T4 and T3.
Lugol’s solution
iodine and potassium iodide; inhibits iodination of tyrosine and thyroid hormone release. By increasing Iodide secretion and iodination is inhibited by NEGATIVE FEEDBACK. SHORT TERM. Treats Thyroid Storm.
Ipodate
Iodinated radiocontract media (IRM); suppresses 5-deiodinase to inhibit T4 to T3 conversion. Rapidly reduces T3 concentrations is thyrotoxicosis.
Propranolol
B-blocker; non selective to prevent tachycardia and other sympathetic drive. Treats THYROID STORM.
Insulin Sensitizers
Do not change sugar levels; Includes METFORMIN[a Biguanide] (Cisapride not used)
Type 1 Diabetes Mellitus (early onset - Children)
Treated with replacement therapy. animal insulins are no longer used.
Insulin resistance
glucose is being dumped in the urine while skeletal muscles are not getting glucose. They slowly die. Exercise overcomes Resistance.
Insulin Analgues
Aspart - fast insulin (HIGH plasma levels)
Regular - 6-8 hours
NPH - up to 18 hours
Determir - up to 20 hours
Glargine - low and steady for days. (LOW plasma levels)
Degludec - longest acting.
Aspart Insulin
FAST insulin; problem with rapid acting and can sometimes overcorrect to cause Hypoglycemia and a coma. addition of ASP (aspartic acid)
Regular Human Insulin
SHORT acting - longer action if there is a larger dose.
NPH Human Insulin
INTERMEDIATE acting
Glargine Insulin
LONG acting; No peak. Asparagine substituted to Glycine. 2 arginines added. (additions make it last longer)
Detemir Insulin
LONG acting (Glargine is longer) Detemir
Degludec insulin
is a recent SLOW onset LONG acting Analog . Greater than Glargine.
Intensive Insulin Therapy
(current trend) INTERMEDIATE or LONG ACTING preparations. (Glargine, Determir, Degludec). Can be combined with “premeal” rapid onsets such as Lispro, Aspar, or Glulisine) LOW DIABETIC COMPLICATIONS
Conventional Insulin Therapy
(in the past) 2 injections daily of SHORT-ACTING (regular) and INTERMEDIATE-acting insulin. No longer recommended.
Insulin Shock (hypoglycemia)
tachycardia, confusoin, sweating, vertigo Treated with sugar or candy, glucagon or glucose.
Insulin-induced immunologic complication
formed insulin antibodies (insulin resistance) Body sees altered insulins and attacks them . Causes pain, lipodystrophy, Edema/weight gain. **
Nasal Insulin Failure
IGF-1 promote growth and activate lung hypertrophy and could lead to lung cancer.
Sulfonylureas
Insulin secretagogue; release of insulin.
Glyburide (2nd gen)
inhibit K-ATP channels(in B-cells) and Decrease glucagon secretion
increase the number insulin receptors in peripheral tissues.
Glyburide
A Sulfonylurea; secretes insulin . Inhibits K-ATP channels to decrease glucagon release. Increases the number of insulin receptors in periphery. BUT can cause ORAL HYPOGLYCEMIA.
Repaglinide
A miglitinide; Acts like a Sulfonylurea. RAPID ONSET and SHORT action. INNEFECTIVE in patients who lack functional Beta cells in ADVANCED stages of Type 2 DM.
Biguanide: Metformin!
Glucophage; IMPROVES INSULIN SENSITVITY. reduces postprandial and fasting glucose in T2 DM. Reduces gluconeogenesis and stimulates glycolysis in periphery, reduces glucose absorption. NO INSULIN release from B cells. DOES NOT cause Hypoglycemia and no weight gain. Used in INSULIN RESISTANCE, Polycystic ovary syndrome, and NAFLD (Non Alcoholic Fatty Liver Disease)
Can cause GI DISTRESS and Lactic Acidosis.
Thiazolidinedions (TZD)
enhance glucose uptake. HbA1C control. PPAR-y activator. Receptors are in BONE and HEART. Treats Hyperglycemia in damaged insulin receptors.
Troglitazone - hepatatoxic
Risiglatazone - Cardiovascular problems
NOT IN CONGESTIVE HEART FAILURE!
Acarbose
a-glucosidase inhibitor ; inhibits this enzyme in the gut. (needed to breakdown polysaccharides to monosaccharides) SLOWS ABSORPTION and REDUCES Hyperglycemia. NO EFFECT on fasting blood sugar. Can cause flatulence, diarrhea, Cramping.
Incretins
Enhance GIP-1; stimulate glucose-dependent Insulin Output.
DPP4 inhibitors
increase GLP-1 release –> increase insulin relase and decreased glucagon release; Sitagliptin & saxagliptin REDUCE HYPERGLYCEMIA
Sitagliptin
inhibit degradation of Incretins (release insulin from GLP-1) delay gastric emptying and reduce food intake.
Pramlintide
Amylin Analog (minor player) decreases gastric emptying and postprandial blood glucose. improve in HbA1C.(blood glucose test) Only for overweight insulin taking patients. INJECT 3 TIME DAILY. (Problem)
Bromocriptine -
treats T2 DM. decreases morning surges of Dopamine, Seritonin, and Norepinephrine to decrease hepatic Glycogenolysis. (increase Dopamine to Decrease sympathetic response.)
Dapagliflozin
SGLT2- Inhibitor; inhibits the reabsorption of glucose by SGLT2 in the proximal tubules of the kidney. Glucose levels decrease and no hypoglycemia. Effective in T2 DM. DO NOT cause weight gain. Increases insulin sensitivity and secretion.
Can cause GLYCOSURIA and GENITAL INFECTIONS (urinary too)
Cinnamon
should NOT be used for glycemic control
Order of Diabetes treatment:
Diet
OAD monotherapy
OAD combination (Metformin+ SU + DPP4-Inh)
OAD + basal insulin (dont want to have to)
complex insulin
Insulin Secretagogues
Glyburide and Repaglinide - increase insulin secretion
Order of OAD treatment choice: (7 of them)
Insulin secretagogues Biguanides (metformin) TZD a-gluc Inhibitor (Acarbose) DDP4-I (Sitagliptin) SGLT-2 inhibitor Bromocriptine
Adverse Effects of Insulin
Hypoglycemia, sweating, weight gain, lipodystrophy
Adverse effects of Sulfonylureas
glyburide
Gi distrubances & Hypoglycemia
Adverse Effects of Repaglinide
drug levels altered when taken with other agents
Adverse Effects of Biguanides (metformin)
Lactic Acidosis, GI Disturbances
Adverse Effects of Thaizolidinediones(TZDs)
Rosiglitazone
CV problems : increased MI , heart attack, Edema, HIP FRACTURE, redistribution of Fat.
Adverse effects of a-Glucosidase Inhibitor (Acarbose)
abdominal pain, diarrhea, Flatulence
Adverse Effects of DPP-4 (Sitagliptin)
nausea and GI disturbances
Adverse Effects of SGLT-2 Inhibitors
Glycosuria, Increased genital and urinary infections
Adverse Effects of Bromocriptine
Nausia and vomitting.
Syndrome X - Triad
Hyperlipidemia, Hyperinsulinemia, Hypertension. Characterized with obesity and high insulin response.
Glucocorticoid receptor
high affinity for cortIsol but a low affinity for aldosterone
Mineralcorticoid receptor
high affinity for both aldosterone and cortisol
CBG (corticosteroid binding globulin)
binds corticosteroids
Cortisol
SHORT ACTING glucocorticoid that opposes insulin action at its target sites. Circadian rhythm (High in AM low around Midnight) Has anti-inflammatory effects by inhibiting cytokine production etc.
Muscle cells - break down protein
Liver cell - release glucose(hyperglycemia)
Fat cell - lipolysis (fat breakdown) cushins
can cause OSTEOPOROSIS and PEPTIC ULCERS
Aldosterone
major natural mineralcorticoid; regulates Na-K balance, blood volume, and Blood pressure.
Prednisone & Triamcinolone
Intermediate-acting corticosteroid agonist
Dexamethasone & Betamethasone
Long-acting corticosteroid agonist
Corticosteroid RECEPTOR Antagonists
Mifepristone & Spironolactone
Corticosteroid SYNTHESIS INHIBITORS
ketoconazole & Aminoglutethimide
Prednisone
Mainly anti-inflammatory;
Fludrocortisone
Topical ANTI-INFLAMMATORY but technically a mineralcorticoid. (salt only at large quantities)
Addison’s disease
treated by cortisol, Prednisone, Fludrocortisol.; adrenal insufficiency. LIFE THREATENING. Infection & trauma
Secondary Adrenal insufficiency
lack of pituitary ACTH. Follows after prolonged steroid therapy and RAPID WITHDRAWL. Iatrogenic (caused from treatment)
Congenital Adrenal Hyperplasia
deficiencies that impair biosynthesis of cortisol and aldosterone. Elevated ACTH causing hyperplasia of adrenocortical cells with no final product.
Non-endocrine diseases that can be treated with potent corticosteroids:
severe inflammation as immunosuppressant autoimmune disease suppression severe asthma myeloproliferative disease nausea & vomitting sickness at high altitude Lung maturation in fetus
Cushing’s syndrome
hypersecretion of glucocorticoids due to ACTH from a Pituitary adenoma (Most common) or Adrenal adenoma.
Treated with surgery OR Adrenal steroid synthesis or Mifepristone.
Symptoms INCREASED APPETITE
Ketoconazole
ANTIFUNGAL agent ; high doses block glucocorticoid & mineralcorticoid biosynthesis. For metastases (spreading cancer) Treats cancers(adrenal), hirsutism, breast cancer
Aminoglutethimide
blocks RATE LIMITING STEP of ACTH. Blocks conversion of Cholesterol to Pregnenalone. s
Prokinetic Agents
promote Upper GI motility- enhance contraction of the gastric antrum and the duodenum. Drugs: Metoclopramide Domperidone Cisapride Erythromycin ***Treats GERD
Ranitine
H2 receptor Antagonist; reduces gastric acid secretion. Most popular* over the counter drug (at low does) Treats ZES (Zollinger-Ellison syndrome) and has less side effects than Cimetidine.
Omeprazole
Proton Pump Inhibitor (PPI) IRREVERSIBLY ; reduce gastric acid secretion from parietal cells. TAILOR MADE DRUG. However it does cause decreased absorption of VIT B12 and HIP FRACTURES for long term use. Long term use.
Pirenzipine
M1 selective muscarinic antagonist; reduce gastric acid secretion
Antacids
agents that nutralize acids. chemical NEUTRALIZATION to bugger the acid in the stomach. Immediate relief. but SHORT duration and REBOUND GASTRIC AID SECRETION.
NaHCO3
antacid. high neutralizer and very soluble. can cause Hypertension. (salt)
CaCO3
antacid moderate neutralizer; and moderate solubility. Can cause hypercalemia and nephrolithiasis (kidney stones)
AlOH3
antacid. high neutralizer , low solubility. can cause CONSTIPATION. Drug absorption reduces its bioavailability.
MgOH2
antacid high neutralizer, and low solubility. Can cause DIARRHEA and be taken LONG TERM. May also cause HYPERMAGNESEMIA. (in patients with renal insufficiency) can kill you if injected. Euthanasia
Cimetidine
H2 receptor antagonist. Reduces gastric acid secretion but has several side effects and no longer is used. Ranitidine is better. (used to be used to treat ZES)
Sucralfate
Cytoprotective mucosal defensive agent that provides a protective MUCUS COATING in the stomach by producing PGE1 and absorbing PEPSIN.
However, the coating decreases GIT MOTILITY. Causes CONSTIPATION & DRYMOUTH.
Misopristol
Methyl PGE1 analong. Mimics PGE1 and enhances production of mucus and HCO3. Cytoprotective and Effective in treating DRUG INDUCED PEPTIC ULCERS by NSAIDS and corticosteroids. But can cause DIARRHEA and CAN’T BE USED IN PREGNANCY.
Bismuth (Bismuthsubsalicylate)
Cytoprotective ; protective coating due to Mucus and PGE1 production. ERADICATES H. PYLORI.
H. Pylori
gram negative bacteria that leads to gastritis and peptic ulcers. Treated with a PPI + Antibacterial.
- PPI
- Amoxycillin/Clarithromycin
- Metronidazole
- Bismuth (if you want the quad treatment)
Zollinger-Ellison Syndrome (ZES)
Gastrinoma of the Duodenum. 2/3rd are malignant. Treated with high dose of PPI (omeprazole) until resorting to surgery or chemotherapy for tumor removal.
Cisapride
PROKINETIC; 5HT4-R Activation to INCREASE ACh release. Blocks cardiac K+ channels and causes ventricular arrhythmias. (LONG QT SYNDROME) not used. CARDIOTOXICITY when combined with Clarithromycin. DDIs
Erythromycin
PROKINETIC & Antibiotic; Activate Motilin receptor. INCREASE ACh release. Enhance duodenal and Colonic motility. Relieves CONSTIPATION by promoting watery diarrhea.
Metoclopramide
PROKINETIC; D2 selective antagonist; INCREASE ACh release (prevents inhibition)
*crosses the BBB
BUT can cause Hyperprolactinemia, Parkinsonian symptoms. (drug induced - Iatrogenic)
Why can’t we use Cholinomimetics and Anticholinesterases to promote gastrinal transit?
non specific effects may cause undesirable muscarinic effects. (salivation, gastric secretion & diarrhea) use Dopamine(D2) blockers , Seritonin4 and Motilin agonists instead.
Domperidone
D2 selective antagonist. DOES NOT cross the BBB. no CNS related symptoms. Still causes Hyperprolactinemia. (posterior pituitary is outside BBB) Effective antiemetic.
Prucalopride
NEW PROKINETIC 5HT4 selective Agonst that promotes ACh release. Treats GERD! & chronic constipation when laxatives fail.
