Endocrine Flashcards
onset 5-15 min
Rapid Acting Insulin
peak 45 min - 3 hrs
Rapid Acting Insulin
duration 3-5 hrs
Rapid Acting Insulin
onset 15-30 min
Short Acting Insulin
peak 2-4 hrs
Short Acting Insulin
duration 5-8 hrs
Short Acting Insulin
onset 1-2 hrs
Intermediate Acting Insulin
peak 4-12 hrs
Intermediate Acting Insulin
duration 18-24 hrs
Intermediate Acting Insulin
onset 1-2 hrs
Long Acting Insulin
peak 0-4 hrs (Levemir)
Long Acting Insulin
duration 24 hrs
Long Acting Insulin
onset 30 min
Intermediate Acting/ Combination Insulin
peak 30 min-12 hrs
Intermediate Acting/ Combination Insulin
duration up to 24 hrs
Intermediate Acting/ Combination Insulin
Rapid Acting Insulins
“Rapid HANs”
lispro (-H-umalog)
glulisine (-A-pidra)
aspart (-N-ovoLog)
Short Acting Insulins
“Short Regular NOVice HUMans”
Regular = Humulin R and Novolin R
Intermediate Acting Insulins
“Intermediate Not so PHast Novice Humans”
NPH = Humulin N and Novolin N
long acting insulin that does not have a peak and is NEVER MIXED with other insulins
Lantus
this type of insulin is usually given QD but can be given BID if glucose levels are difficult to control
Long Acting Insulin
Long Acting Insulins
“Long-Acting will always LANd LEVEl”
glargine (Lantus)
detemir (Levemir)
\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_ Insulins: Humalog Mix 50/50 Humalog Mix 75/25 Novolog Mix 70/30 Humulin 70/30 Novolin 70/30
Intermediate Acting/ Combination
type of insulin most often used in pumps
rapid-acting
insulin pump absorption onset, peak, and duration
onset 30 to 60 minutes
peak 1 to 5 hours
duration up to 10 hours
Advantages of __________:
Eliminates multiple injections
Delivers greater accuracy
Improves HgA1c
Results in fewer large swings both up and down in blood glucose level
Allows the patient to exercise without having to eat large amounts of carbohydrates
Insulin Pump
Disadvantages of ___________:
Can cause weight gain
Diabetic ketoacidosis (DKA) if the catheter comes out
Can be expensive/needs insurance approval
Insulin Pump
type of insuline that has a faster peak concentration in serum and more rapid metabolism than injectables
Insulin Inhaler
start treatment with _____________ when oral agent & a GLP1-receptor agonist are unable to keep the A1C <9%.
insulin
________ is not bioavailable when given orally (broken down by stomach acids)
insulin
Complications of __________:
HYPO-glycemia
HYPO-kalemia
Lipohypertrophy (accumulation of SQ fat)
Insulin
SE of ____________:
weight gain
intense well-controlled BS may increase risk for low BS and mortality
Insulin
D2D Interactions of ___________:
Hypoglycemic agents
Hyperglycemic agents (oral steroids, sympathomimetics, thiazides)
Beta Blockers: can delay drug awareness & response to hypoglycemia by masking the stimulation of the sympathetic nervous system that hypoglycemia causes (ex. tachycardia, palpitations, shaking).
Insulin
Indications for ___________:
Type 2DM
Off-label: PCOS, GDM, antipsychotic-induced wt. gain
Type 2DM prevention
Metformin
MOA of ____________:
hepatic glucose production
🠉 insulin sensitivity in target tissues (skeletal muscles & fat) thus 🠉 glucose uptake
🠋intestinal absorption of carbohydrates
Metformin
Contraindications for ____________:
severe renal dysfunction (eGFR<30)
acute/chronic metabolic acidosis including DKA w/ or w/o coma
Hypersensitivity
Metformin
SE of \_\_\_\_\_\_\_\_\_\_\_: diarrhea flatulence N/V, metallic taste in mouth (GI-related, subside over time) HYPER-glycemia if combined with a Sulfonylurea B12 Deficiency w/ long term use
Metformin
Good things about __________:
🠋CV & microvascular complications
🠋triglycerides, free fatty acid concentrations, LDL levels 🠉HDL
May help w/ weight loss (weight neutral drug)
Metformin
Education for __________:
SE resolve but may return w/ dose adjustment
Take with meals
Metformin
Metformin is excreted by the:
kidneys
BBW for __________:
May cause Lactic Acidosis (“MET me in LA”)
Metformin
S/S of \_\_\_\_\_\_\_\_: malaise myalgias N/V severe abdominal pain respiratory distress/SOB somnolence mental status changes tachypnea tachycardia abnormal heartbeat severe loss of strength and energy severe dizziness feeling cold low BG? HA shaking confusion increased hunger sweating ---If left untreated: wheezing chest tightness fever itching, bad cough, blue skin color, seizures, or swelling of face, lips, tongue, or throat hypothermia persistent bradyarrhythmias hypotension death
Lactic Acidosis
Treatment for Lactic Acidosis caused by Metformin use
D/C Metformin and Hemodialysis
Risk Factors for \_\_\_\_\_\_\_\_\_\_\_\_: HF renal impairment ETOH abuse age >65yrs old use of contrast dye surgery hepatic impairment hypoxic states serious acute illness Hx of condition severe infection with decreased tissue perfusion
Lactic Acidosis
D2D Interactions of __________:
Tagamet: 🠉 in metformin blood levels = 🠉 risk of hypoglycemia & LA
ETOH: 🠉 risk of LA
Metformin
Sulfonylureas
Glyburide
Glipizide
Sulfonylureas:
____ Generation are safe in pregnancy
____ Generation NOT safe in pregnancy
2nd = safe 1st = NOT safe
MOA of ____________:
bind to K+ channels in B-cells
stimulate release of insulin
🠉 insulin sensitivity in target tissues (1st & 2nd Gen)
2nd Gen: greater potency + less D2D interactions
Sulfonylureas
SE of \_\_\_\_\_\_\_\_\_\_: *usually well tolerated* *loses effectiveness over time* HYPO-glycemia=most common nausea skin reaction weight gain abnormal LFTs
Sulfonylureas
Sulfonylureas are most effective in patients with __________ weight or __________ weight
normal or increased
Sulfonylureas with longer ½ lives can be dosed _______ but are higher in risk for HYPO-glycemia
daily
________ Sulfonylureas are best for the elderly due to decreased HYPO glycemia risk
Short Acting
D2D Interactions of \_\_\_\_\_\_\_\_\_\_\_: Tagamet NSAIDs ETOH Beta-adrenergic blockers: can 🠋 efficacy Sulfonamide ABX (try to avoid)
Sulfonylureas
MOA of _________:
acts on incretin system and stimulates insulin release
inhibits glucagon release resulting in a 🠋 of the BG
Glucagon-Like Peptide (GLP)-1 Receptor Agonist:
exenatide (Byetta)
Liraglutide (Victoza)
Caution: in cases of acute pancreatitis
Glucagon-Like Peptide (GLP)-1 Receptor Agonist:
exenatide (Byetta)
Liraglutide (Victoza)
BBW: possible risk of thyroid tumors, seen in animal studies
Glucagon-Like Peptide (GLP)-1 Receptor Agonist:
exenatide (Byetta)
Liraglutide (Victoza)
MOA:
lowers BS by improving insulin sensitivity w/o 🠉 insulin production by the pancreas
needs insulin to work
Thiazolidinedione (TZDs):
pioglitazone (Actos)
Contraindications: symptomatic HF or Class 3 and 4 HF
Thiazolidinedione (TZDs):
pioglitazone (Actos)
Caution: Risk for Hepatocellular Injury!
*Report abd pain, N/V, anorexia, jaundice, or dark urine. Check LFTs prior to initiation & monitor if concerned about liver disease
Thiazolidinedione (TZDs):
pioglitazone (Actos)
BBW: Heart Failure - may cause or exacerbate HF (due to fluid retention
**Educate: report ANY weight gain (rapid or not)
and any dyspnea
Thiazolidinedione (TZDs):
pioglitazone (Actos)
MOA: inhibits degradation of incretins causing:
🠉 insulin secretion
🠋 glucagon secretion
Leads to 🠋 in hepatic glucose production
Dipeptidyl Peptidase (DPP-4) Inhibitor “Gliptins”
“Incretin Enhancers”:
Saxagliptin (Onglyza)
Contraindications: Pancreatitis Hx
Dipeptidyl Peptidase (DPP-4) Inhibitor “Gliptins”
“Incretin Enhancers”:
Saxagliptin (Onglyza)
Caution: impaired renal function
Dipeptidyl Peptidase (DPP-4) Inhibitor “Gliptins”
“Incretin Enhancers”:
Saxagliptin (Onglyza)
Can 🠋 appetite and may help w/ weight loss (or weight neutral)
Dipeptidyl Peptidase (DPP-4) Inhibitor “Gliptins”
“Incretin Enhancers”:
Saxagliptin (Onglyza)
MOA: inhibits SGLT2 preventing kidneys from reabsorbing glucose
results in 🠉 urinary excretion of glucose
(newest drug available)
Sodium-glucose cotransporter 2 (SGLT2) inhibitors - gliflozins
BBW: increased risk of limb amputation (possibly due to vasoconstriction)
“Saying Goodbye To my Limbs”
Sodium-glucose cotransporter 2 (SGLT2) inhibitors - gliflozins
Rationale for _____________:
Glucose becomes glycogen, amino acids assemble into proteins, fatty acids are incorporated into triglycerides
Insulin
Rationale for \_\_\_\_\_\_\_\_\_\_\_\_\_: Lowers fasting Bgl by 20% Lowers Triglycerides, fatty acids, and LDL; Raises HDL; ↓ microvascular complications; Helps with weight regulation
Biguanides: Metformin (Glucophage)
Rationale for _____________:
Lowers BG by 20%
Best for normal or slightly overweight.
Short-acting in elderly
Sulfonyureas
Rationale for __________:
Weight neutral
Third-line therapy in patients with A1C >9%
DPP-4 Inhibitors “-gliptins”
Saxagliptin
(Onglyza)
Rationale for ___________:
Redistributes fat from visceral to SubQ; visceral fat is associated with insulin resistance
Thiazo-lidinediones “-glitazones”
Pioglitazone (Actos)
Rosiglitazone (Avandia)
Safety for __________:
Liver damage is reversible if stopped.
Newer meds have lower incidence
Thiazo-lidinediones “-glitazones”
Pioglitazone (Actos)
Rosiglitazone (Avandia)
MOA: Stimulate pancreas to release insulin from beta cells
- often used with Metformin
- Weight neutral/possible gain
- 3rd line med
Meglitinides:
Repaglinide (Prandin)
Rationale for_____________:
Good for erratic meal schedules, patient w/ normal fasting BG and high postprandial (after meal) BG
Meglitinides:
Repaglinide (Prandin)
Safety: Rapid onset and short half-life
Low risk of hypoglycemia
Meglitinides:
Repaglinide (Prandin)
SE: bloating, abdominal cramps, diarrhea, gas
Meglitinides:
Repaglinide (Prandin)
MOA: Inhibit alpha-glucosidase which converts dietary starch and carbs into simple sugars
Causes a decrease in intestinal secretion of glucose
Alpha-Glucosidase Inhibitors:
Acarbose (Precose)
Miglitol (Glyset)
Rationale:
Slows absorption of glucose after meals
Works in the gut so little risk of hypoglycemia
**Rarely used due to intolerable S/E
Alpha-Glucosidase Inhibitors:
Acarbose (Precose)
Miglitol (Glyset)
Safety: Take with first bite of meal TID to decrease postprandial BG
Alpha-Glucosidase Inhibitors:
Acarbose (Precose)
Miglitol (Glyset)
Education:
Better tolerated if client also decreases sugar intake
May cause gas and diarrhea
Alpha-Glucosidase Inhibitors:
Acarbose (Precose)
Miglitol (Glyset)
Drugs not often used for DM due to _________________________________:
Bile acid sequestrant colesevelam (Welchol)
Dopamine Agonists bromocriptine (Cycloset)
SE and lack of efficacy
MOA: Mimic hormones that help regulate BG
Stimulates GLP-a receptors which stimulate insulin release-
Inhibiting postprandial glucagon release
Slows gastric emptying
GLP-1 Agonists/ Incretin Mimetics
Exenatide (Byetta)
Liraglutide (Victoza)
SE: nausea, hypoglycemia, and possible weight loss
GLP-1 Agonists/ Incretin Mimetics
Exenatide (Byetta)
Liraglutide (Victoza)
MOA: Slows gastric emptying leading to feeling of early satiety
Decreases postprandial glucagon secretion
Amylin Analog:
Pramlintide (Symlin)
Rationale for ____________:
Non-injectable hypoglycemic agent
Used as adjunct to insulin
Amylin Analog:
Pramlintide (Symlin)
Safety: Can cause hypoglycemia, weight loss, and nausea
Amylin Analog:
Pramlintide (Symlin)
Education: May promote weight loss
**3rd line therapy due to lack of efficacy in lowering BG
Amylin Analog:
Pramlintide (Symlin)
Rationale:
Slows absorption of glucose after meals
Works in the gut so little risk of hypoglycemia
**Rarely used due to intolerable S/E
Alpha-Glucosidase Inhibitors:
Acarbose (Precose)
Miglitol (Glyset)
Safety: Take with first bite of meal TID to decrease postprandial BG
Alpha-Glucosidase Inhibitors:
Acarbose (Precose)
Miglitol (Glyset)
Education:
Better tolerated if client also decreases sugar intake
May cause gas and diarrhea
Alpha-Glucosidase Inhibitors:
Acarbose (Precose)
Miglitol (Glyset)
Drugs not often used for DM due to _________________________________:
Bile acid sequestrant colesevelam (Welchol)
Dopamine Agonists bromocriptine (Cycloset)
SE and lack of efficacy
MOA: Mimic hormones that help regulate BG
Stimulates GLP-a receptors which stimulate insulin release-
Inhibiting postprandial glucagon release
Slows gastric emptying
GLP-1 Agonists/ Incretin Mimetics
Exenatide (Byetta)
Liraglutide (Victoza)
SE: nausea, hypoglycemia, and possible weight loss
GLP-1 Agonists/ Incretin Mimetics
Exenatide (Byetta)
Liraglutide (Victoza)
MOA: Slows gastric emptying leading to feeling of early satiety
Decreases postprandial glucagon secretion
Amylin Analog:
Pramlintide (Symlin)
Sulfonyurea with cimetidine (Tagamet) =
intensifies ___________ response
hypoglycemic
Safety: Can cause hypoglycemia, weight loss, and nausea
Amylin Analog:
Pramlintide (Symlin)
Education: May promote weight loss
**3rd line therapy due to lack of efficacy in lowering BG
Amylin Analog:
Pramlintide (Symlin)
Weight Neutral DM Drugs
“no GAIM or loss”
Metformin GLP-1 agonists/Incretin Mimetics Amylin Analogs DPP-4 Inhibitors (Gliptins) G: gliptins, A: Amylin Analogs, I: Incretin Mimetics, M: Metformin)
Weight Gain DM Drugs
“gain SIM weight”
Sulfonylureas
Insulin
Meglitinides
Metformin with ETOH = increased risk of __________
lactic acidosis
Metformin with cimetidine (Tagamet) =
increases level of ________
increased risk of _________
Metformin
Hypoglycemia
Metformin with Sulfonyurea or Insulin =
increased risk of ___________ in patients w/ impaired renal function
lactic acidosis
Sulfonyurea with ETOH = ___________ reaction
Disulfiram-Like Reaction
flushing, palpitations, nausea
**possible hypoglycemia
Sulfonyurea with Beta Blocker =
decreases efficacy of ____________ because Beta Blockers suppresses insulin release
Sulfonyurea
In CVD, decrease dose of _____________ as low as 12.5 mcg/day especially if patient is frail
Levothyroxine (T4)
Production of __________ (hormone that promotes hyperglycemia) increases 3X in pregnancy
cortisol
Teaching:
Take at the same time every day
Take after rising on empty stomach with full glass of water
Do not eat for at least 1 hour after taking
Or take 4 hours after eating and wait for 1 hour before eating again
Levothyroxine (T4)
Levothyroxine is highly ____________
protein-bound
converted to T3 in the body (so T3 supplementation is unnecessary)
Levothyroxine (T4)
Dosing;
75-125 mcg (or about 1.6 mcg/kg/dl of ideal body weight)
Levothyroxine (T4)
Adjust Levothyroxine (T4) ___ to ____ mcg/day every 4 to 8 weeks based on clinical response and serum TSH.
12 to 25
elderly dose of Levothyroxine (T4) is ____% less than regular adult dose
75%
Monitor: onset of cardiac sx (angina)
Levothyroxine (T4)
In CVD, decrease dose of _____________ as low as 12.5 mcg/day especially if patient is frail
Levothyroxine (T4)
Once TSH is stabilized on Levothyroxine (T4), check TSH on __ month intervals then ___ month intervals
6 then 12
Drugs that reduce absorption of _____________:
PPIs
Calcium and Iron Supplements
Aluminum containing antacids
Histamine H2 receptor blockers -Cimetidine (Tagamet)
Levothyroxine (T4)
Drugs that accelerate metabolism of ____________:
Warfarin: effects are increased
***accelerates the degradation of Vitamin K-dependent clotting factors
Levothyroxine (T4)
If thyroid replacement is started when patient is taking _______, the dose of _______ may need to be reduced
warfarin
Meds that induce \_\_\_\_\_\_\_\_\_\_ dysfunction: ● Lithium ● Amiodarone ● Interferon "AILs the Thyroid"
Thyroid
Insufficiency of thyroid hormone in pregnancy can lead to fetal __________
brain abnormalities
If a pregnant patient is already taking _____________ in pregnancy, the dose needs to be increased significantly and TSH level monitoring is necessary
Levothyroxine (T4)
has 5-6 drug half-lives, a recommended testing interval post adjustment change is 6-8 weeks
Levothyroxine (T4)
may increase the requirements of Insulin & Digoxin
Levothyroxine (T4)
Use: Treats symptoms of tachycardia, tremor, and anxiety until a euthyroid state is achieved.
Beta Blocker: propanolol (Inderal)
AE of _____________:
BP increases = increase the risk of major adverse CV events
Serious pulmonary oil microembolism (POME) reactions
Testosterone
SE: **Nonselective (blocks beta1 and beta2 receptors) bradycardia decreased AV conduction reduced contractility hypotension reduced cardiac output depression insomnia bizarre dreams sexual dysfunction bronchoconstriction bronchospasm
Beta Blocker: propanolol (Inderal)
One advantage of _________ for hyperthyroidism is that they work quickly, unlike PTU, methimazole, and 131I.
Beta Blockers
In thyrotoxic crisis, in the absence of contraindications (e.g., asthma, heart failure), all patients should receive this immediately. Administration may be oral or IV.
Beta Blockers
MOA: Emits a combination of beta particles and gamma rays
Destruction of thyroid tissue is produced primarily by emission of beta particles which do not travel outside of the thyroid d/t low ability to penetrate any type of physical barrier
Reduction of thyroid gland is gradual
Initial effects become apparent in days or weeks. Full effects develop in 2 to 3 months
Radioactive Iodine 131 “I”
Indication: Graves Disease, Thyroid CA, hyperthyroidism, inadequate response to antithyroid drugs or subtotal thyroidectomy
Radioactive Iodine 131 “I”
Contraindications: Pregnancy, Lactation, very young children (risk of CA)
Radioactive Iodine 131 “I”
BBW: Secondary exposure (transdermal gel, transdermal solution): Virilization has been reported in children who were secondarily exposed to topical gel and solution. Children should avoid contact with unwashed or unclothed application sites in men using topical gel.
Testosterone
Contraindications: Nitrates
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
Indication: Increase quality of life, increase libido, enhance mood, improve bone and muscle mass
Testosterone
Precautions:
Prostate and breast CA are absolute contraindications!
Breast cancer: long term use (>10 yrs) for male hypogonadism may increase risk for BR CA
CVD: Should not be commenced or 3-6 months in patient with PMH of cardiovascular events
Dyslipidemia: may alter serum lipid profile; caution with Hx of MI or CAD
Increases risk of gynecomastia, BPH, prostate CA, VTE, DVT, PE
Testosterone
Erectile Dysfunction is a risk marker for underlying _________________
CV disease
Indications: BPH and ED (off-label - Raynaud’s)
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
D2D Interactions of \_\_\_\_\_\_\_\_\_\_\_\_\_: Potentiate the hypotensive effects of: Nitrates Alpha blockers Anti-hypertensives
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
Education:
Take PO ½ to 4 hours before sexual intercourse and no more than once daily
None of these are affected by alcohol ingestion, although alcohol ingestion is associated with erectile dysfunction
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
has a half-life that is three times the length of the other PDE 5 inhibitors with duration of effect up to 36 hours
Tadalafil (Cialis)
Contraindications: Nitrates
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
Precautions: Recent history of stroke/MI (MI - past 3 months) significantly low or uncontrolled high BP active peptic ulcer predisposed to priapism unstable angina cardiac failure severe liver impairment end-stage renal disease requiring dialysis
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
SE: HA flushing dyspepsia dizziness nausea nasal congestion rhinitis altered vision back pain myalgia
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
Preventitive Strategies for ____________:
regular bone-strengthening exercise
calcium (1200-1500mg daily)
vitamin D (800-1000 IU daily) supplementation PRN
Reduction in modifiable risk factors such as: smoking, ETOH 2/day, high caffeine, low Ca+ and Vit D, physical inactivity
Osteoporosis
Causes of \_\_\_\_\_\_\_\_\_\_\_\_\_: chronic steroids androgen deficiency hypogonadism anorexia bulimia gastric bypass celiac disease hyperthyroidism ankylosing spondylitis
Secondary Osteoporosis
Drugs for \_\_\_\_\_\_\_\_\_\_: Bisphosphonates hormone therapy (HT) selective estrogen receptor modulators (SERMs) rank ligand inhibitors calcitonin Parathyroid hormone is antiresorptive
Osteoporosis
MOA: activation of osteoblasts
Osteoporosis Meds
MOA: binds to RANK Ligand, inhibiting osteoclast formation, function & survival, preventing osteoclasts from resorbing bone
Rank Ligand Inhibitors: Denosumab (Prolia)
Indication: Osteoporosis given via injection q6 months
Rank Ligand Inhibitors: Denosumab (Prolia)
Contraindications: Low Ca+, Low GFR
Biophosphonates
Precautions: Recent history of stroke/MI (MI - past 3 months) significantly low or uncontrolled high BP active peptic ulcer predisposed to priapism unstable angina cardiac failure severe liver impairment end-stage renal disease requiring dialysis
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
SE: HA flushing dyspepsia dizziness nausea nasal congestion rhinitis altered vision back pain myalgia
Phosphodiesterase type 5 Inhibitors: Tadalafil (Cialis)
Preventitive Strategies for ____________:
regular bone-strengthening exercise
calcium (1200-1500mg daily)
vitamin D (800-1000 IU daily) supplementation PRN
Reduction in modifiable risk factors such as: smoking, ETOH 2/day, high caffeine, low Ca+ and Vit D, physical inactivity
Osteoporosis
Short-term or intermittent exposure to ___________ (single SQ injection), leads to a predominance of osteoblast-mediated bone formation
PTH Analog: Teriparatide (Forteo): Injectable
Drugs for \_\_\_\_\_\_\_\_\_\_: Bisphosphonates hormone therapy (HT) selective estrogen receptor modulators (SERMs) rank ligand inhibitors calcitonin Parathyroid hormone is antiresorptive
Osteoporosis
MOA: activation of osteoblasts
Osteoporosis Meds
Alendronate (Fosamax) Risedronate (Actonel) Ibandronate (Boniva) - not recommended to reduce nonvertebral or hip fracture risk Zoledronic acid (Reclast) - annual IV "FABZulous"
Biophosphonates
Indications: First line for postmenopausal women with low bone mineral density, preventative and treatment for osteoporosis
Continue treatment for 3-5 yrs; stop by 5 yrs due to risk of atypical fractures. Positive benefits typically last longer
Biophosphonates
Contraindications: Low Ca+, Low GFR
Biophosphonates
Raloxifene (Evista) - Estrogen Agonist
Selective Estrogen Receptor Modulator (SERM)
MOA: Binds to estrogen receptors, creates an agonist or antagonist effect at the site; exact MOA is unknown; reduce osteoclast activity while reducing estrogenic effect on breast and endometrial tissue (thereby reducing risk of breast CA); Prevents spine fractures
Selective Estrogen Receptor Modulator (SERM)
Indication: Prevention/Treatment of osteoporosis
Risk reduction for invasive breast CA for women 50-60 yrs old with high risk (reduces risk if taken up to 5 years);
Selective Estrogen Receptor Modulator (SERM)
SE: hot flashes, weight gain, flu-like s/s, arthralgias, infections
Selective Estrogen Receptor Modulator (SERM)
BBW: Thromboembolic events!!!
Contraindicated with PMH of VTE, DVT, PE, Retinal vein thrombosis; risk vs. benefit analysis for women with PMH of heart failure or active malignancy; risk for DVT, PE, and superficial thrombophlebitis higher during first 4 months of treatment.
Selective Estrogen Receptor Modulator (SERM)
MOA: binds to RANK Ligand, inhibiting osteoclast formation, function & survival, preventing osteoclasts from resorbing bone
Rank Ligand Inhibitors: Denosumab (Prolia)
Indication: Osteoporosis given via injection q6 months
Rank Ligand Inhibitors: Denosumab (Prolia)
SE:
Infections of the abdomen, urinary tract, and ear
atypical femur fractures have been seen
Risk of hypocalcemia (greatest w/ severe renal dysfunction)
Rank Ligand Inhibitors: Denosumab (Prolia)
MOA: reduce risk of fractures and osteoporosis in specific populations of postmenopausal women
Hormone Therapy: Estrogen and Progestin
Increases risk of heart disease, DVT, breast and endometrial CA
Hormone Therapy: Estrogen and Progestin
MOA: promotes bone formation for men and women; decreases osteoporosis-related fractures; stimulates osteoblast function, increasing GI calcium absorption and renal tubular reabsorption of calcium
**Approved for 48 months
PTH Analog: Teriparatide (Forteo): Injectable “Forteo Fortifies”
Short-term or intermittent exposure to ___________ (single SQ injection), leads to a predominance of osteoblast-mediated bone formation
PTH Analog: Teriparatide (Forteo): Injectable
While PTH analogs stimulate __________ bone formation, they also stimulate _______________ bone breakdown
osteoblast-mediated
osteoclast-dependent
Ideal agent for treatment of ______________ would be purely anabolic, stimulating bone formation without stimulating resorption
osteoporosis
Continuous or high _______________, leads to a predominance of osteoclast-mediated bone resorption and consequent net bone loss
PTH (primary hyperparathyroidism)
reserve this drug for extreme cases for high risk of fractures
PTH Analog: Teriparatide (Forteo): Injectable
BBW: Osteosarcoma
PTH Analog: Teriparatide (Forteo): Injectable
Education:
○ Take with full glass of water after rising
○ Do not lay down for at least 60 minutes after taking (can lead to esophageal ulceration)
○ Take on empty stomach or 4 hours after eating and do not eat or take other medications for at least 30-60 minutes after taking.
Biophosphonates
Risks:
Possible damage to GI tract including throat, esophagus, and stomach
atypical fractures of the femur
esophageal cancer
osteonecrosis of the jaw d/t reduction in blood supply to the jaw (patients may be unable to have dental implants on this med and should tell their dentists about it)
Biophosphonates
Education: Take with a full glass of water after food at same time per day and keep doses to 20 mg or less at a time. May need to dose more than two times per day to avoid GI upset.
Glucocorticoids
Adverse Effects:
○ Altered Metabolism–may lead to hyperglycemia with short-term use, and protein wasting and increased lipid deposition with long-term use.
○ Altered immune response–this may be one of the medication goals, yet this effect will also mask signs of infection.
○ Impaired bone health–will cause calcium to leach out of the bones and could increase risk for osteoporosis with long-term use.
○ Skin–may thin (atrophy) skin with topical use on a daily basis. Chronic use may exacerbate acne.
○ Neurological impacts–cranial nerve palsy, mood instability–may cause tremor, hunger, and agitation, aggression.
○ Cardiac–may increase hypertension due to fluid retention associated with its impact on excretion of potassium and retention of sodium and water.
○ Ocular–angle-closure glaucoma and cataracts with long-term use, cataracts, exophthalmos, papilledema.
○ Chronic Use:
● Hypothalamic Pituitary Adrenal Axis (HPA) suppression
● Cushing’s syndrome
● Osteoporosis
● Immunosuppression
● Skin changes including atrophy, striae, telangiectasia, and acne
Glucocorticoids
First-line for RA; Folic acid antagonist; affects leukocyte suppression, decreasing inflammation caused by by-products of cell degradation; highly effective, 70-75% improvement within 3-8 weeks. Contraindicated in pregnancy and breastfeeding w/leukopenia
Rheumatoid Arthritis (RA) and Disease Modifying Antirheumatic Drugs (DMARDS): Methotrexate (Rheumatrex)
BBW: ■ Use Appropriately: Because of the possibility of serious toxic reactions, use only in life-threatening neoplastic diseases or in patients with severe psoriasis or RA.
Bone marrow suppression, Renal impairment (monitor for toxicity), Hepatotoxicity, Pneumonitis (evaluate for any coughing), Gastrointestinal toxicity, Secondary malignancy, Dermatologic toxicity, Opportunistic infections, Severe toxic reactions, including embryo-fetal toxicity.
Rheumatoid Arthritis (RA) and Disease Modifying Antirheumatic Drugs (DMARDS): Methotrexate (Rheumatrex)
Neurotransmitter that is the main satiety hormone
Serotonin
SE: HA, hypoglycemia (monitor diabetics), back pain, URIs, abnormal lymphocytes. Can raise prolactin levels.
Contraindications/Warnings: Serotonin syndrome, CNS depression, Worsening depression. Contraindicated during pregnancy
Lorcaserin (Belviq)- Anorexiant, Serotonin Receptor Agonist (Controlled Substance IV)
BBW: suicidal thinking
Caution: acute opioid withdrawal, can elevate the heart rate and blood pressure, can cause neuropsychiatric effects, hepatotoxicity, seizures, and hypoglycemia in diabetics from weight loss.
Naltrexone & Bupropion- Anorexiant, Antidepressant, Dopamine/Norepinephrine-Reuptake Inhibitor, Opioid Antagonist
causes fat-soluble vitamin deficiency so take a MVI but separate from this drug by 2 hrs
Orlistat
Contraindications: Pregnancy, chronic malabsorption syndrome, cholestasis; may increase risk for cholelithiasis, hepatotoxicity, and increased urinary oxalate levels may lead to kidney stones.
Orlistat
SE: HA, N/V, confusion, dry mouth, and dizziness
Weight loss drugs that affect neurotransmitters, such as Lorcaserin and Bupropion/Naltrexone
Warnings: Serotonin syndrome, CNS depression, worsening depression BUT No BBW.
Lorcaserin (Belviq)
Calcium absorption is reduced after ________ surgery
bariatric
__________ surgery could make oral contraceptive pills ineffective.
bariatric
2nd gen sulfonylureas - maybe
propylthiouracil (PTU) - safest (Risk vs Benefit)
Synthroid
Betamethasone (24-36.6 weeks @ risk of PTL w/in 1 wk)
Topical corticosteroids (less than 2 weeks)
Prednisolone (severe PUPPS)
Insulin
Metformin
Safe in Pregnancy
● 1st Gen Sulfonylureas ● Phentermine ● Belviq ● Orlistat ● Methotrexate (w/ leukopenia) ● Radioactive Iodine
Not Safe in Pregnancy
● propylthiouracil (PTU) - safest ● Methimazole ● Synthroid ● Prednisone ● Topical low-dose steroids ● NPH & Regular Insulin- may help prevent T1DM
Safe in Breastfeeding
Sulfonylureas
High potency topical steroid on nipple, face, genitals
Phentermine
Aspart, detemir, glargine, glulisine, lispro - caution
Methotrexate (w/leukopenia)
Radioactive Iodine
Not Safe in Breastfeeding
in type ___ DM; these patients produce no endogenous insulin and are therefore very sensitive to dosing adjustments.
1
“Have you MET my KIDS?”
METformin is a stressor to the KIDneys
If there is cross-reactivity between sulfonamide antibiotics (sulfonylarlamines) and other non-arylamine sulfonamides (sulfonylureas) (there should not be…), it is due to the _______________ of the patient rather than a true cross-reactivity.
allergic susceptibility
BBW: May cause or exacerbate heart failure
Thiazolidinediones
drugs that promote insulin secretion
Meglitinides
drugs that delay carbohydrate digestion and absorption
Alpha-Glucosidase Inhibitors
drugs that are contraindicated during pregnancy due to fetal hyperinsulinemia
1st Generation Sulfonylureas
NPH and regular human insulin are considered safe with ___________
breastfeeding
There are no reported adverse reactions and newborn exposure to _______ in breast milk may help prevent type 1 diabetes in these infants
insulin
Aspart, detemir, glargine, glulisine, lispro: While they are probably safe, caution is advised for the use of the newer biosynthetic insulins with breastfeeding due to limited studies
bf
treatment for ___________________: surgical ablation of thyroid tissue, radioactive dye, or antithyroid medications to destroy the overactive thyroid tissue.
Hyperthyroidism
clinical diagnosis of _________________ is only made when patients have low total levels combined with symptoms and/or signs
testosterone deficiency
Men with _________________ who are interested in fertility should have a reproductive health evaluation performed prior to treatment.
testosterone deficiency
Prior to offering ___________ therapy, clinicians should measure hemoglobin and hematocrit and inform patients regarding the increased risk of polycythemia.
testosterone
clinicians should counsel patients that, at this time, it cannot be stated definitively whether ___________ therapy increases or decreases the risk of cardiovascular events (e.g., myocardial infarction, stroke, cardiovascular-related death, all-cause mortality)
testosterone
propylthiouracil (PTU) and methimazole–both are category ____. Nonetheless, endocrinologists will prescribe ______ due to the client and the fetal risks associated with untreated hyperthyroidism.
D; PTU
Zoledronic acid (Reclast) is given via:
IV annually
“Likely effective” when treating type 2DM by lowering BS levels
Berberine
When prescribing tx for ED, what condition is contraindicated with PDE 5 inhibitors
Nitrates
Dosage for ____________:
Pregnancy - 1st trimester increased dose but lower in 2-3rd trimester, baby is dependent on it
Levothyroxine T4
basal insulins
Lantus and Levemir
basal insulin duration (Lantus and Levemir)
24hrs - long acting
peak of basal insulins (Lantus and Levemir)
Lantus no peak
Levemir doesn’t have much of a peak (gradual)
I stimulate insulin secretion, I require some beta cells to work, I can be tricky with antibiotics, I can cause weight gain, My effectiveness wears out.
Sulfonylureas
I am often referred to as an Insulin Sensitizer, I have been known to cause or exacerbate heart failure, I might hurt your liver.
TZD
I am often chosen first, I increase Insulin’s actions in the peripheral tissues, I inhibit glucose production from the liver, I can cause weight loss.
Biguanides- Metformin
- GI side effects (will go away after time)
- MOA: they delay the absorption of carbohydrates
- I only affect the postprandial glucose levels
- I must be taken with the first bite of a meal.
Alpha-Glucosidase Inhibitor
patients with DM actually have a change of their microbiome in their gut, causing _____________
GI SE
a. BBW can cause virilization in kids (Use caution with contaminated clothing)
b. It can raise the blood pressure
c. Pulmonary micro-embolisms
d. Contraindicated in Prostate & Breast Cancer
Testosterone
Why are nitrates with PD5 Inhibitors such a concern?
the vasodilatory effects are enhanced and prolonged
Take these medications first thing in the morning 30-60min before food or other medications.
- TAKE IT WITH A BIG GLASS OF WATER!
- Do not lay down after taking (30-60min)
- They are associated with the risk for atypical fractures after 5yrs, so stop taking them. Longer than 5yrs can cause atypical hip & femur fracture. The drug can continue to keep working for years after - effects are longer lasting (possibly decades)
- Take calcium & Vitamin D to maximize their effectiveness
- They can lead to osteonecrosis of the jaw.
Biphosphonate (Fosamax)
I have a BBW for thromboembolic events, I can cause hot flashes, weight gain, and flu-like symptoms, I bind to the estrogen receptors and reduce the osteoclast activity
Selective estrogen receptor modulator (SERMS)
I inhibit the absorption of dietary fats by 30%; I am contraindicated in pregnancy, cholestasis, and malabsorption syndrome; Take me within 1 hour of a fatty meal; I AM:
Orlistat (Alli)
DO NOT take this if you have NOT eaten a fatty meal! Take vitamins ADEK
Orlistat (Alli)
_____________ patients need to take:
Vitamin B12, calcium, & ADEK; May also reduce effectiveness of oral contraceptives
Gastric bypass/surgery
I am an opioid antagonist; I inhibit dopamine and norepinephrine; I can be associated with suicidal ideations; I can cause HA and sleep disorders; I AM
Naltrexone and Bupropion (Contrave)
