Because Blessington said this pharm test sucks ass. Flashcards
What are the three available treatment styles for osteoporosis?
- Lifestyle modifications (tobacco, exercise, nutrition, caffeine avoidance)
- Supplements (Calcium and Vitamin D)
- Pharm (Catabolic Inhibitors and Anabolic stimulants)
How much oral calcium is absorbed?
30-40%
What is the ceiling dose of calcium?
3 times per day
At what age does the daily dose of calcium change from 1,000 mg to 1,200 mg in women?
50
Tell me about the three types of calcium supplements…
- Calcium carbonate (cheap - cannot take with food)
- Calcium citrate (better absorbed)
- Calcium Gluconate (Expensive)
What calcium supplement should you take with a PPI?
Calcium Citrate
What is the dosing range for OTC Vitamin D supplement?
700-800IU (controversial)
When is estrogen therapy helpful in osteoporosis?
In peri-menopausal causes – prevents further break down
Not therapeutic so calcium and vitamin D also need to be given
How does estrogen work?
Reduces levels of cytokines, TNF-alpha, IL-1, and IL-6, which stimulate osteoclasts and directly modulate osteoclast activation
Why isn’t estrogen help in senile osteoporosis?
Because in senile, there is decreased osteoblast activity, NOT increased osteoclast activity
When is estrogen therapy cautioned?
Past history/family history of BC, endometrial cancer or history of thromboembolic disorder
Adverse effects of estrogen therapy?
Breakthrough bleeding, breast tenderness, increase risk of cancer - because of this, it is no longer recommended
What is Raloxifene [Evista]?
Selective Estrogen Receptor Modulators (SERM’s)
What does Raloxifene [Evista] do?
Estrogen-like effect on bone and lipids - decreasing bone resorption
Thought not to stimulate endometrium and breast tissue
When is Raloxifene [Evista] used?
Prevention and treatment of osteoporosis
What are the side effects of Raloxifene?
Flu-like syndrome, hot flashes, arthralgias, peripheral edema, headache, weight gain, vaginal bleeding
Who should not take Raloxifene?
History of venous thrombosis and caution when on thyroid medications - may decrease its absorption.
Do you cycle progesterone with Raloxifene?
Negatory.
What do bisphosphates do?
Suppress osteoclast activity with no negative effect on mineralization (except Etidronate)
When should you take bisphosphonates?
On an empty stomach with 8oz of fluids in the AM - sit upright for 30 minutes after to avoid esophagitis.
Who should avoid taking bisphosphonates?
Renal failure patients
What is a side effect of bisphosphonates?
Osteonecrosis of the jaw
Tell me about the 4 formulations of bisphosphonates and what do they do?
- Risedronate - reduces vertebral fractures (not hip)
- Etidronate - used in Paget’s disease only - inhibits mineralization
- Alendronate - most common -reduces both hip and vertebral fractures
- Zolendronic Acid - used in post-hip fractures (IV only - every 12 months)
What is Aldendronate’s MOA?
Decreases rate of bone resorption
What are the side effects of Alendronate?
Esophagitis, hypophosphatemia, myalgia
Who should not take Alendronate?
Esophageal abnormalities
What drugs interact with Alendronate?
Antacids
How often is Alendronate taken?
Daily/weekly
What is Calcitonin?
Hormone - administered in osteoporosis, Paget’s disease and hypercalcemia
What does Calcitonin do?
Decreases osteoclast activity (binds to osteoclast receptors) by antagonizing impact of PTH and possible analgesic effect
Side effects of Calcitonin?
Rhinitis, epistaxis, nasal mucosal ulcerations…
Because inhaled in the nose
How is Calcitonin administered?
IM or nasal spray (hence the SE’s we just talked about)
Alternate nostrils daily
What does Calcitonin reduce the risk of?
Vertebral fractures
Anabolic therapies for osteoporosis?
Testosterone, fluoride, Teriparatide [Forteo]
Does testosterone supplementation help men with osteoporosis?
No
Why is fluoride not a good treatment?
Increases bone mass but the new bone is poorly mineralized and brittle
When is Teriparatide used?
Moderate to severe cases with previous hip/vertebrae fractures not responding to bisphosphonates
How does Teriparatide work?
Injection of low dose recombinant form of PTH - stimulates osteoblast activity causing new bone formation
Must give as low dose injections in order for it to stimulate osteoblasts
Max time frame to take Teriparatide?
2 years
Can you take Teriparatide in combination with bisphosphonates?
No - but bisphosphonates may be started after 2 years of discontinuing Teriparatide
What is Levothyroxine?
T4 replacement
When is Levothyroxine given?
Hypothyroidism
How does Levothyroxine work?
Replacement T4 converted to T3 in peripheral tissues, travels to nuclear receptors, causes protein synthesis, metabolic rate, promotes gluconeogenesis
When should we take Levothyroxine?
In AM 30 minutes before eating
What is a major drug to drug interaction with Levothyroxine?
Iodide
How should hypothyroidism be monitored once on drug?
TSH - 6 to 8 weeks until normalized, 8-12 weeks after dose change
What drugs decrease TSH level?
Corticosteroids and dopamine
What drug increases TSH?
Metoclopramide - no one knows why… well, at least I don’t.
If patient pharmacy swtiches brands of Levo, what should be done?
Curb stomp a bitch.
And then check TSH in 6-8 weeks
As patients age, does their dose change?
It may - typically decreases with age
What is Liothyronine?
T3 replacement (rarely needed)
When is Liothyronine indicated?
Hypothyroidism unresponsive to Levo or treatment for myxedema coma
What percent of hypothyroid patients need Liothyronine?
Roughly 15% - genetic deaminase deficiency so they cannot convert T4 to T3
How does Liothyronine work?
T3 in peripheral tissues to nuclear receptors to cause protein synthesis, metabolic rate, promote gluconeogenesis
How often should Liothyronine be dosed?
BID or TID because short half life
Why is thyroid USP not used anymore?
Don’t even know what this is but it has unpredictable hormone amounts, causing potential T3 toxicity
This probably isn’t important.
What is Liotrix?
Synthetic T4 and T3 in a 4:1 ratio - seldom use
What is Sasha eating right now?
Mac and cheese
Does depression happen with hypothyroidism or hyperthyroidism?
Both!
Starting dosing regimen for Levo?
12.5 to 25 micrograms
What drugs reduce thyroid hormone synthesis?
Anti-thyroid drugs - duh.
Propylthiouracil, methimazole and radioactive iodine
What does radioactive iodine do?
Thyroid ablation - concentrates in thyroid gland and kills off gland cells over 6-8 weeks
Can pregnant women take radioactive iodine?
No
How does methimazole work?
Oxidation of iodine in thyroid gland preventing iodine combining with tyrosine to for T3 and T4
Does Methimazole inactivate circulation T3 and T4?
Nope.
How does Prednisone work?
Suppresses adrenal function at high dose - decreases leukocyte migration - enters cell nucleus to alter synthesis of proteins
Half life of prednisone?
12-26 hours
Side effects of long term use of Prednisone?
HPA-axis suppression
Decreased Ca++ absorption
Hypercorticolism
Can someone on prednisone get live vaccines?
No way Jose
Where is prednisone metabolized to active form?
Liver
Active form = Prenisilone
After how long does a person need to be down titrated when coming off prednisone?
2 weeks of therapy or more
What makes Dexamethasone different from Prednisone?
Longer half life of 48+ hours
8-10 times more potent
Less dose required
What is Fludrocortisone?
Mineralocorticoid - used for Addion’s disease and resistant orthostatic hypotension
What is Fludrocortisone’s MOA?
Promotes increased distal renal tubule absorption of Na+ and loss of K+
What drug interacts with Fludrocortisone?
Diuretics - increase levels of loops
What is Glipizide?
Sulfonylurea - used in type 2 DM
MOA of Glipizide?
Stimulates pancreatic B cells to release insulin
Why is there controversy on using sulfonylureas as first line?
May increase rate of B cell burn out
Weight gain
Side effects of Glipizide?
HYPOGLYCEMIA
Weight gain
Contraindications of Glipizides?
Sulfa allergy
Type 1 DM
Drug-drug interactions with Glipizide?
Beta blockers - decrease hypoglycemic effect/symptoms
What is Repaglinide?
Non-sulfonylurea secreatgogue
When do we use Repaglinide?
To reduce post-prandial glucose levels - used in patients with sulfa allergies that cannot take Glipizide
How does Repaglinide work?
Binds to adjacent receptor on sulfonylurea receptor on beta cell to stimulate insulin release
How much does Repaglidine decrease post prandial glucose levels?
65-70 mg/dL
When should Repaglidine be taken?
15 minutes prior to meals TID
Can Repaglidine be used as monotherapy?
Yes - but also in combo with Metformin and TZD
What is the amylin mimetic?
Pramlintide
Is Pramlintide used in type 1 or type 2 DM?
Both - used to lower post prandial glucose levels
What else does Pramlintide do?
Decreases gastric emptying, glucagon secretion and appetite
How is Pramlintide administered?
Subcutaneously 15 minutes pre-meal - DO NOT MIX WITH INSULIN
What is Exantide [Byetta]?
Incretin-synthetic analog of GLP-1
When do we use Exantide?
Type 2 DM with Metformin +/- Sulfonylurea to lower post prandial glucose levels
Side effects of GLP-1?
Necrotizing, hemorrhagic pancreatitis
Can cause hypoglycemia if used with insulin secretagogue
How is Exantide administered?
SubQ BID up to 60 minutes pre meal
When should someone stop Exantide therapy?
If they develop antibodies to the drug
What is Liraglutide?
Incretin-synthetic analog of GLP-1 used to Type 2 DM with Metformin +/- Sulfonylurea to lower post prandial glucose levels
How does Liraglutide work?
Increases insulin release, decreases glucagon release, slows gastric emptying, decreases appetite, *increases beta cell growth/replication
What is Sitagliptin?
DPP-4 inhibitor used in type 2 DM
How does Sitagliptin work?
Inhibits DPP-4 to reduce degradation of GLP-1 - increases levels of GLP-1
What is Metformin?
Biguanide
Is Metformin the first line drug for Type 2 DM?
Yes!
How does Metformin work?
Unknown - decreases hepatic glucose production, decreases renal gluconeogenesis, slows intestinal absorption glucose, increase glucose conversion to lactate by enterocytes, etc.
Side effects of Metformin?
N, V, D, farting
What drugs interact with Metformin?
Iodinated IV contrast
What should you watch for on patients taking Metformin that have renal failure?
Lactic acidosis
Is hypoglycemia seen in patients with Metformin?
No, not typically
Metformin should be started at low doses and titrated up to avoid what side effect?
Diarrhea
If someone needs IV contrast, what should they do with taking their Metformin?
Hold 48 hours
What is Pioglitazone?
TZD (Thiazolidinedione)
Is Pioglitazone used in Type 1 or Type 2 DM?
Type 2
How does Pioglitazone work?
Decreases insulin resistance - it is the most potent insulin sensitizer
Contraindications of Pioglitazone?
Macular edema, diabetic retinopathy
What is Rosiglitazone?
TZD - no longer used due to severe CV side effects (CHF and AMI)
What hormone does Pioglitazone require for activity?
Insulin - because it sensitizes insulin! Duh!
What should be monitored while on Pioglitazone?
Regular eye exams
What is acarbose?
Alpha-glucosidase inhibitor
Is Acarbose used in type 1, type 2 DM, or both?
Both!
How does Acarbose work?
Reduces post prandial glucose levels by inhibition of intestinal alpha-glucosidase conversion polysaccharides to monosaccarides
Side effects of Acarbose?
Farting, diarrhea, abdominal pain - people hate these
When should Acarbose be taken?
Before each meal
What is Colesevelam?
Bile Acid Sequesterant
What is Colesevelam used for?
Hypercholesteremia
Type 2 DM in adjunct with Metformin/Sulfonylurea/Insulin
MOA of Colesevelam?
Decreases intestinal glucose absorption
What does Colsevelam do to triglycerides?
Elevates them
Caution if >200mg/dL
Discontinue if >500mg/dL
How should Colsevelam be taken?
3 tabs prior to meal BID
What is desmopressin?
Vasopressin receptor agonist
What is desmopressin used to treat?
Diabetes insipidus
How does desmopressin work?
Increases permeability of renal tubular cells to water reabsorption causing decreased urine volume
What is the rapid-acting insulin?
Insulin lispro
What is the short acting insulin?
Regular insulin
Intermediate acting insulin?
Neutral Protamine
Long acting?
Insulin Glargine
Which type of insulin is inhaled?
Exubra
What drug interacts with insulin?
Alcohol - increases hypoglycemia risk
Onset, peak, duration for Lispro?
Onset = 5-15 minutes Peak = 1-1.5 hours Duration = 3-5 hours
Onset, peak, duration of Regular?
Onset = 0.5-1 hour Peak = 2-4 hours Duration = 5-8 hours
Onset, peak, duration of Neutral Protamine?
Onset = 2-4 hours Peak = 4-10 hours Duration = 10-24 hours
Onset, peak, duration of Glargine?
Onset = 2-4 hours
Does not peak
Duration = 20-24 hours
Do not mix with other insulins in the same syringe
What kind of doing is used in type 1 DM?
Short acting (with meals) and intermediate/long acting (basal levels)
What kind of dosing of insulin in used in type 2 DM?
Long acting (basal) +/- short acting
At what A1C level is therapy initiated?
8.5% - single drug therapy may suffice - Metformin or Sulfonylurea
Over 9% - typically needs multiple drugs to work on different mechanisms
