Pharmacology > Endocrine System > Flashcards

Endocrine System Flashcards

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1
Q

thyroid and parathyroid glands

A

TH
thyroglobulin
PTH

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2
Q

Pancreas

A

exocrine: trypinogen, chymotrypsin, amylase, lipase
endocrine: insulin, glucagon

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3
Q

adrenal

A
  • cortisol
  • aldosterone
  • estrogens
  • androgens
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4
Q

bone formation

A

PTH: calcium, phosphorous

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5
Q

growth formation

A

estrogens, androgens: testosterone

-growth hormone releasing hormone-GH (somatropin)

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6
Q

metabolic rate control

A

TSH

TH

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7
Q

CHO metabolism

A

insulin

glucagon

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8
Q

blood pressure control

A

cortisol
aldosterone
ADH

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9
Q

bisphosphanates

A
  • used for osteoporosis and Paget’s disease
  • alendronate (fosomax), etidronate (Didronell), pamidronate (Aredia), risedronate (Actonel), tiludronate (Skelid)
  • alendronate, risedronate, ibendronate are used mostly for prevention
  • rational drug selection: high risk: white, Asian, hx of eating disorders
    • correct preexisting vit. D deficiency, hypocalcemia b/4 starting bisphonates
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10
Q

pharmacodynamics of bisphosphanates

A

-inhibits osteoclastic activity and bone resorption thus increases bone density
-bone density mass increases rapidly in first year and plateau’s after 2-3 yrs
ADRs: diarrhea, constipation, n/v, hypocalcemia, hypophosphatemia, dyspenia, esophageal ulcers, arthragia, myalgia, HA, rash, afib
-pathologic fx for tx >3 months
-osteonecrosis (jaw)
-muscular skeletal pain
-caution with patients with renal impairment, hrt failure, liver dz, active GI problems
-drug and food interactions: ranitidine doubles alendronate bioavailability, calcium supplements, antacids

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11
Q

pharmacokinetics of bisphonates

A
  • must be taken with 8 oz of water and fasting
  • pt. must remain upright for 30 minutes or one hour with ibandronate
  • onset 3-6 wks peak 3-6 months
  • half life ten years
  • metabolism-none
  • excretion: urine, feces (unabsorbed drug)
  • most pregnancy category C except pamidronate category D
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12
Q

Human growth hormone

A
  • stimulates growth and metabolism of every cell in body

- used for short stature men

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13
Q

pharmacodynamics of human growth horomone

A
  • initial insulin-like effect
  • simulates growth of linear bones, skeletal muscles and organs
  • simulates erythropoietin
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14
Q

pharmacokinetic human growth hormone

A 
IM and SQ well absorbed
-bioavailability 75% SQ
-metabolism: hepatic renal 90%
excretion: renal
ADRs: antibody development, hyperglycemia, edema, hypothyroidism, arthralgia, ha, dizziness, flu-like sx's
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15
Q

pancreatic enzymes

A

-used for cystic fibrosis and pancreatitis
-monitoring: CF-lifetime
pancreatitis-contraindicated during times of acute illness
hypersensitivity-may need products from vegetable sources
steatorrhea: needs monitoring

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16
Q

pharmacodynamics of pancreatic enzymes

A
  • inactivated by pH values
  • pancreatin (Ku-zyme) pancrealipase (Pancreas)
  • subsititute for pancreatic enzymes
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17
Q

pharmacokinetic of pancreatic enzymes

A

-taken immediately before of with meal
-absorption: none, because it acts locally in GI tract
-excretion: feces
-pancrelipase made from pork, pancreatin is made from pork, cow, or vegetable source-not good for people with gout or renal impairment
-antacids decrease effectiveness, decreases absorption of oral iron
ADRs: skin irritation, rashes, GI: n/v, stomatitis, hyperuicosuria, hyperuricemia

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18
Q

pharmacodynamics of inulin

A
  • total number of receptor sites can be decreased by obesity and long standing hyperglycemia
  • binds at insulin receptor sites on cell membrane allowing glucose to enter cells
  • acts on liver to increase storage of glucose as glycogen, decreases production of urea, catabolic activity and cAMP,
  • promotes protein synthesis on muscle cells
  • reduces circulation of free fatty acids and promotes storage of triglycerides in adipose tissue
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19
Q

types of inslin

A

rapid-acting: Lispro (Humalog), apart (Novolog), or glulisine (Apidra), onset about 5 minutes, peaks in one hour, duration 4-5 hours SQ
short-acting: humulin insulins, sometime used around mealtime; takes 30-45 minutes before eating, peaks in 3-4 hrs. duration 4-ten hours, can give IM off label use
intermediate-acting: NPH is mixed with protamine delaying absorption insulin looks cloudy and has to be mixed before its injected; onset half to hour peak 4 to ten duration twelve 24 hours
long-acting: glargine (Lantus), detemir (levemir) insulin onset 2-4 hours, duration 24 hours with little or no peak
ultra long lasting: Degludec, 42 hour duration

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20
Q

hypothalmic-pituitary system

A
  • thyrotropin-releasing hormone creates TSH
  • GnRh-leads to FSH, LH
  • prolactin releasing hormone-prolactin
  • oxytocin
  • antidiuretic hormone (ADH)
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21
Q

etidronate (Didronel)

A
  • bisphosphanate
  • reduces both bone resorption and formation (coupled together)
  • reduce vertebral fractures
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22
Q

pamidronate and risedronate (Aredia and Actonel)

A
  • bisphosphonate
  • inhibits resorption without inhibiting formation or mineralization
  • pamidronate only available in parenteral form
  • both reduce vertebral fractures
  • risedronate reduces non-vertebral fractures
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23
Q

alendronate (Fosamax)

A
  • bisphosphonate
  • 100-500x more potent then other drugs
  • highly selective inhibitor
  • inhibits osteoclastic activities without interfering with osteoclast recruitment or attachment
  • reduces both vertebral and nonvertebral fractures
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24
Q

tiludronate (Skelid)

A
  • bisphosphonate
  • inhibits osteclastic activity by interfering with osteoclasts attachment to bone surface and inhibiting osteclastic proton pump
  • decreases vertebral fractures
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25
zoledronic acid (Zometa)
- bisphosphonate - inhibits osteoclast activities and induces apoptosis - only IV - reduces vertbral fractures
26
ibandronate (Boniva)
- bisphosphonate - inhibits osteoclastic activity and reduces bone resorption - reduces vertebral fractures - can be given IV every 3 months if po untolerated or unwilling
27
monitoring on bisphosponate
- electrolytes-especially serum calcium | - alkaline phosphatase-increasing positive for paget's dz
28
somatrem and somatropin
-for GH depression -given to stimulate synthesis of somatomedins in growth plate cartilage resulting in increased linear, organ and skeletal growth and increased protein synthesis -insulin-like effect -contraindicated for patients with closed epiphyses, or active tumor growth -close monitoring is needed for patient with thyroid disorders -insulin resistance can occur--cautious with diabetic patients ADRs: hyperglycemia, hypothyroidism, edema to secondary Na+ retention
29
pancreas
- exocrine and endocrine glad - 2 major dz: CF and pancreatitis - both leads to obstruction of ducts resulting in activated digestive enzymes within pancreas and failure of releasing enzymes into duodenum to digest--malabsorption
30
diabetes
type one: destruction of beta cells to produce insulin type 2: insulin resistant -either one-disequilibrium between excess production of glucagon and lack of insulin
31
pharmacokinetics of insulin
-absorption dependent on type, injection site, and volume injected -abdominal absorbs 50% more -metabolism: induces CYP1A2 -excretion: urine ADRs: hypoglycemia, diabetic ketoacidosis, ETOH increases hypoglycemia -drug interactions: beta blks increase insulin resistance and masks hypoglycemic symptoms
32
average dosing for insulin
0.6-0.8 U/kg
33
monitoring for diabetes
- routine glycohemoglobin, renal function and CBC - A1C test x2/yr when under control; once quarterly if tx goals not reached - goal usually is A1C
34
type 2 diabetes
- insulin resistance - 4 primary alterations: insufficient production of endogenous insulin by beta cells, tissue insensitivity to insulin, impaired response of beta cells to BG levels, excessive production of glucose secondary to increased glucagon levels - liver and incretin hormone system is the major organ
35
sulfonyureas
- helps with insufficient production of endogenous insulin by stimulating release from beta cells - improve insulin binding or increase # of receptors but does not improve insulin utilization - second line drug - not used as monotherapy - all potentiate effects of antidiuretic hormone - glipizide (Glucotrol), glyburide (Diabeta), glimeride (Amaryl)-
36
pharmacokinetics of sulfonylureas
- metabolism: liver CYP2C9 - absorption: all with most - protein binding: >95% - excretion: urine and feces
37
pharmacotherapeutics of sulfonylureas
-precautions/contraindications: cross sensitivity with sulfonamides and thiazide diuretics -pregnancy C -older adults more sensitive -pediatric use for 10-18 yrs old but off label ADRs: hypoglycemia, GI, derm rashes, SIDH, hemolytic anemia, leukopenia, thrombocytopenia, wt. gain
38
clinical use/dosing for sulfonyureas
- for type 2 - use either first or second generation--first generation more hypoglycemia, wt. gain, and reduction of efficacy overtime - dose on individual response-titrate every 4-7 days - for neurogenic diabetes insipidus--chlorpropamide off label use
39
rational drug selection/dosing for sulfonylureas
- age: avoid using chlorpropamide and glyburide in older adults--use short acting glipizide - low cost-generic available - with comorbidities: renal impairment use glipizide/tolbutamide or glyburide - concurrent with insulin-only glimepiride by FDA, most 2nd generation
40
monitoring of sulfonylureas
-HbA1C baseline every 6 months if meeting therapy goals or every 3 months if adjusting CBC on onset and every8-ten months -can be taken food except glipizide must be taken 30 minutes prior to meal
41
biguanides
- oral antihyperglycemic drug - first line drug for adults and children over age ten - metformin (glucophage) - monotherapy-lacks hypoglycemic effects, weight neutral, and decreased CVD events
42
pharmacodynamics biguanides
- decreases glucose in liver - decreases GI glucose absorption and improves insulin sensitivity by increasing peripheral glucose uptake and utilization - does not stimulate insulin from beta cells - inhibits platelet aggregation and reduces blood viscosity
43
pharmacokinetics of biguanides
- absorption: 50-60% after po dose; food decreases and delays absorption - no hepatic metabolism - excreted by kidneys - ETOH potentiates drug's effect on lactate metabolism
44
pharmacotherapies for biguanides-
precautions/contraindications - renal dz/dysfunction - metabolic acidosis - hepatic dz - withhold 48 hrs prior to test with iodine contrast - monitor pt. with b 12 deficiency - category B-not recommended - not for use of children
45
rational drug selection/dosing of biguanides
- IR v. ER-can safely switch btwn both.-just monitor glucose - start 500 mg BID with max of 2550 mg/day - if pts not responded after 4 weeks consider adding other oral agents like sulfonylurea - part of metabolic syndrome treatment protocol - monitoring: renal function, ketones, and HbA1C
46
Alpha-glucosdiase inhibitors
- acarbose (Precose) - migitrol (glyset) - NOT monotherapy *can be for pre-diabetes
47
pharmacodynamics of alpha-glucosidase inhibitors
- inhibits absorption of CHO from GI tract high lowers BG after meals - no hypoglycemia effect
48
pharmacokinetics of alpha-glucosidase inhibitors
-
49
Pharmacotherapies of alpha-glucosidase inhibitors
Precautions/contraindications -not given to patients with IBS, possible bowel obstruction or renal impairment -not for pregnant patients ADRs: flatulance, diarrhea, abdominal pain -drug interactions: acarbose and digoxin and miglitol and propanolol and ratadine
50
Clinical use/dosing of alpha-glucosidase inhibitors
- initial dose 25 mg TID titration 4-8 weeks | - take with first bite of meal
51
pharmacodynamics of thiazolidinediones
- pioglitazone (Actos), rosiglitazone (Avandia) - improves target cell response to insulin - increases utilization of insulin by liver and muscle cells - reduces liver glucose production - modest impact on lipids - no hypoglycemic effects - higher risk of bladder ca - increased risk of of HF - weight gain
52
pharmacokinetics of thiazolidinediones
- rapidly absorbed after po dose - metabolized by liver CYP2C8 and 3A4 - 99% protein bound - excrete through urine and feces as metabolites
53
pharmacotherapies of thiazolidinediones
precautions/contraindications -chronic liver dz-increased concentrations of metabolites -fluid retention-exacerbates HF -restriction of use of rosiglitizone d/t increased risk of MI ADRs: edema, URI, headache, fatigue drug interactions: oral contraceptives need higher doses; -any drug metabolized by CYP3A4-corticosteroids, ketoconazole
54
meglitinides
- short acting insulin secretagogues - add-on therapy - repalinide (Prandin), nateglinide (Starlix) - used in place of sulfonylurea - expensive
55
pharmacodynamics of meglitinides
- increases insulin release from beta cells by closing K+ channels leading to opening of Ca+ channels which then releases insulin - short time in plasm
56
pharmacokinetics of meglitinides
- absorbed rapidly and completely - metabolized in liver by CYP3A4 and CYP2C8 - excreted within 96 hours; mostly in feces some in urine
57
pharmacotherapies of meglitinides
precautions/contraindications -liver impairment-higher concentrations of substrate -pregnancy cat C -not approved for pediatrics ADRs: hypoglycemia drug interactions: any drugs metabolized by CYP 3A4 or CYP 2C9 -antifungals and antimicrobials inhibit metabolism--increasing risk of hypoglycemia
58
dosing for meglitinides
- patient's with HbAC 8 initial one mg before each meal | - titrate every 2 weeks for maximum of sixteen mg/24 hours
59
dipeptidyl peptidase-4 inhibitors
- "gliptins" - newest class of antidiabetic agents - sitagliptin (Januvia) and saxaglipin (Onglyza) - different mechanism of action: works on incretin hormone system - add-on therapy-*can be used as monotherapy but more effective in combination - once a day
60
pharmacodynamics of dipeptidyl peptidase-4 inhibitors
- inhibits DPP-4 which breaksdown GLP and GIP which are released in response to meals - increases secretion of insulin - suppresses release of glucagon from pancreas - promotes pre/post prandial glucose - slows gastric emptying - promotes weight loss - well tolerated
61
pharmacotherapies for dipeptidyl peptidase-4 inhibitors
precautions/contraindications -renal dysfunction-dependence on renal system for elimination -pregnancy cat B -not approved for pediatrics ADRs: GI, headaches drug interactions: ace inhibitors-increased risk for angioedema
62
glucagon-like peptide 1 agonists
- new drug of antidiabetic agents - exenatide (Byetta) - SQ injection twice daily; can be given weekly - given 60 minutes before meals - dose 6 hours apart - very expensive - add on therapy
63
pharmacodynamics of glucagon-like peptide-1 agonists
- promotes insulin release from beta cells when glucose level rises - decreases glucagon secretion - increases satiety
64
pharmacotherapies of glucagon-like peptide agonists
``` Precautions/contraindications -severe GI dz-colitis, crohns -pregnancy cat C -renal dz ADRs: n/v/d, pancreatitis drug interactions: increased INR if given with warfarin, digoxin ```
65
amylin agonists
- pramlintide (Symlin) - adjunct therapy for type one and type 2 - co-administered with insulin - lowers glucose by acting on glucagon secretion and slowing gastric emptying - via SQ injections
66
pharmacodynamics of amylin
- slows gastric emptying - suppresses glucagon secretion leading to decreased endogenous glucose - centrally mediated modulation of appetite--potential weight loss
67
pharmacotherapies of amylin
precautions/contraindications -high risk of hypoglycemia since administer with insulin -pregnancy cat C ADRs: GI drug reactions: acetaminophen pharmacokinetics altered--must administer separately
68
glucagon
- considered antidote: used for diabetic patients who have hypoglycemia d/t insulin overdose - SQ, IM, IV
69
pharmacodynamics of glucagon
- stimulates hepatic gluconeogensis and glycogenolysis leading to increased BG - BG rises within ten minutes of injection with maximal effect after 30 minutes - hepatic stores necessary for glucagon to produce antihypoglycemic effect
70
pharmacotherapies of glucagon
precautions/contraindications -pregnancy cat B -use caution with pt suspected having phenochromocytoma or insulinoma ADRs: n/v drug interactions: increased anticoagulant effects of po anticoagulants
71
patient education on glucagon
- educate family members/roommates on to administer IM - pt given supplemental CHO when awake and can swallow - lifestyle management
72
thyroid hormones
- levothyroin (T4), liothyronine (T3), liotrix (mixture of T3 and T4) - hypothalamus-pituitary-thyroid-hormone begins with secretion of TRH from hypotalamus in response to cold, stress, decreased levels of T4 - TRH leads to secretion of TSH which: releases stored thyroid hormone, increases iodine uptake and utilization, increases synthesis of T3 and T4, increases synthesis of prostaglandins - create negative feedback loop to inhibit TRH and TSH - synthetic hormones produces feedback loop to stop secretion of TSH - levothyroxine drug of choice d/t longer half life
73
pharmacokinetics of thyroid hormones
- absorption is erratic with po and decreases with age, food, health of GI tract - majority is protein bound - excreted by bile/feces
74
pharmacotherapies of thyroid hormones
precautions/contraindication -contraindicated after acute MI or thyrotoxiocosis -pregnancy cat A -may need higher doses when pregnant ADRs: symptoms of hyperthyroidism, long term use associated with decreased bone density in hips/spine drug interactions: bile-acid sequestrants, iron salts, antacid decrease absorption; estrogen decrease response; warfarin, digoxin, and beta blockers may decrease action
75
hypothyroidism
- tx indicated with TSH>ten or btwn 5-ten if goiter or anit-thyroid peroxidase - thyroxin replacement is lifelong - levothyroxine drug of choice
76
levothyroxine dosing
pts with CV: initial dose 50 mcg/day 2-4 wks may titrate -average full replacement one hundred -one hundred twenty five mcg/day pt>50 with CV or lifelong disease: initial dose twelve.5 to 25 mcg/day, titrate monthly
77
antithyroid agents
-propylthiouracil (PTU), methimazole (Tapazole) pharmacodynamics: -blocks synthesis of thyroxine and trilodothyronine -does not treat underlying pathology in hyperthyroidism
78
pharmacokinetics of antithyroid agents
-rapidly absorbed after po dosing peaking within one hour 75-80% protein bound--except methimazole is NOT protein bound -short half life -excreted through urine
79
pharmacotherapies of antithyroid agents
``` precautions/contraindications -pregnancy cat D -high concentrations in breast milk -PTU not recommended for children ADRs: agranulocytosis, drowsiness, headache, alopecia, skin rashes, renal/hepatic failure drug reaction: lithium, warfarin ```
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