Pharm Endocrine Exam Flashcards
Bisphosphonates
Prevent loss of bone density and decrease the risk of fractures
Decrease in osteoclast mediated bone reabsorption
MOA
Stimulates osteoclast apoptosis
decreases the number of osteoclasts
decrease in bone reabsorption
2nd/3rd generation
Inhibit Cholesterol synthetic pathway
Decrease in osteoclast function
Decrease in bone reabsorption
Bisphosphonates meds
Alendronate = Fosamax Risedronate Etidronate Tiludronate Pamidronate Ibandronate Zoledronate
All end in -dronate
Calcium carbonate
Calcium carbonate is cheapest and therefore a good first choice
Absorption is better when taken with meals
(calcium citrate is better fasting)
Calcium carbonate is poorly absorbed in patients on PPI’s or H2 blockers.
(use Calcium citrate)
Calcitriol Indications
Rocaltrol (Vitamin D Analog)
Indications
Secondary hyperparathyroidism
and resultant metabolic bone disease in predialysis patients (CrCl 15–55mL/min).
Hypocalcemia and resultant metabolic bone disease in patients on chronic renal dialysis.
Hypocalcemia in hypoparathyroidism
pseudohypoparathyroidism.
Calcitriol Contraindications / interactions
Contraindications: Hypercalcemia, Vitamin D Therapy, Vitamin D toxicity, Nursing mothers
Interactions
Hypermagnesemia
Magnesium containing antacids
Arrhythmias with digitalis if hypercalcemia occurs
Recombinant PTH
Natpara (hormone)
Adjunct to calcium and vitamin D to control hypocalcemia in hypoparathyroidism
Warning: Osteosarcoma
Interactions:
alendronate, digoxin: monitor serum calcium, digoxin levels, and for digitalis toxicity
Adverse reactions:
Paresthesia, hypocalcemia, headache, hypercalcemia, nausea
MOA of Recombinant PTH
Bone = Losing calcium
Small intestine = Absorption of calcium
Kidney = Reabsorption calcium
MOA of Calcitriol
Increases Ca2+ and PO4- absorption in small intestine
Active form of Vitamin D
For patients with significant symptoms of hyperthyroidism or patients with hyperthyroidism complications like elderly, cardiovascular disease
First line Beta blockers (atenolol 25-50) (200 max) QD
Along with a thionamide
Specifically Methimazole
For women who wish to become pregnant with hyperthyroidism
Propylthiouracil (PTU would be the preferred drug during the first trimester of pregnancy and can be continued throughout pregnancy
Management of Hyperthyroidism flow chart
Control symptoms with Beta blockers
(*asthma)
Stop @ euthyroid
Control hyperthyroid with Thionamides or PTU
(*agranulocytosis)
Remission in 50% cases of GD After 6-18 months
Radioactive iodine
(*pregnancy, incontinence, breastfeeding)
Euthyroid or hypothyroid in 90% cases after first dose
Surgery
(*Hypoparathyroidism, Bleeding, Laryngeal nerve palsy
Hypothyroidism, possibly Hypocalcemia
Beta Blockers and hyperthyroidism
End in -lol
Atenolol 50-100 QD
Propranolol 20-40 TID
Help reduce symptoms quickly until other treatments can take effect
(help with tremors, Tachycardia and nervousness)
(don’t stop thyroid hormone production)
(usually feel better within hours)
Methimazole
Tapazole (antithyroid)
For Hyperthyroidism
Not for nursing mothers
Warnings:
Discontinue if agranulocytosis, aplastic anemia, exfoliate dermatitis, hepatitis, elevated liver enzymes
Interactions: Potentiates anti coagulants
Adverse: Arthralgia, paresthesia, hair/taste loss, agranulocytosis, aplastic anemia, liver dysfunction, lupus like syndrome
Proppylthiouracil
PTU
Hyperthyroidism
Warning: Hepatic reactions (injury, failure, transplant)
Interactions:
May potentiate anti coagulants,
May need to reduce beta blockers and digitalis
Caution with drugs that also cause agranulocytosis
Adverse: Arthralgia, paresthesia, hair/taste loss, myalgia, lupus like syndrome
MOA of Thionamides
Methimazole
Propylthiouracil
Inhibits thyroid hormone synthesis
Inhibit the oxidation of iodine
PTU: inhibits peripheral conversion of T4 to T3
Thyroid Storm
Slide 40
Hypothyroidism
Primary vs Secondary
Primary: Iodine deficiency Excess iodide intake Thyroid ablation Hashimotos Sub acute thyroiditis Genetic abnormalities Goiterogenic food Drugs: Lithium, Amiodarone, Antithyroid agents
Secondary:
Adenoma
Ablative therapy
Pituitary destruction
Primary hypothyroidism goals
The goals of therapy are improvement of symptoms,
normalization of TSH secretion,
reduction in size of goiter (if present),
and avoidance of overtreatment (iatrogenic thyrotoxicosis).
Goal to keep serum TSH within the normal range (approximately 0.5 to 5.0 mU/L).
Treatment of choice for primary hypothyroidism
Synthetic T4
Levothyroxine
Either a generic or a brand-name formulation is acceptable.
If a switch from one manufacturer to another is made
Measure a serum TSH six weeks after changing to verify TSH is still within the therapeutic target.
Initial dose of Levothyroxine for
Primary Hypothyroidism
Young healthy patients = Full dose
1.6mcg/kg/day
Taken on empty stomach 30-60 mins before breakfast
T4 serum should be reevaluated in 6 weeks
(adjust if needed)
Symptoms begin to resolve in 2-3 weeks
Regular concentrations are not achieved for 6 weeks)
Dosing for Levothyroxine
Initial = 1.6mcg/kg/day (a few months)
Adjust dose in 12.5-25mcg increments
every 4-6 weeks until TSH returns to normal (euthyroid
Normal TSH = 0.5-5.0)
Levothyroxine sodium
Synthroid (synthetic T4)
Take 30-60 mins before breakfast
Contra: uncorrected adrenal insufficiency
Warning: Not for obesity or weight loss
Underlying cardiovascular disease,
arrhythmias during surgery in CAD patients
Adverse: Arrhythmias, MI, Dyspnea, Muscle spasms
Thyroiditis
Subacute painful
(de Quervain’s, granulomatous, giant cell)
Drug induced
(usually amiodarone)
MOA of antidiabetic drugs
Biguanides
Thiazolidines
-diones
Liver
Decrease glucose production
= Less glucose in the blood
Helps restore normal glucose level in blood
MOA of antidiabetic drugs
Alpha-glucosidase inhibitors
Intestine
Delay glucose absorption in gut
= Less glucose in the blood
Helps restore normal glucose level in blood
***delay carb absorption,
MOA of antidiabetic drugs
Meglitinides
Sulfonylureas
Phenylalanine derivatives
insulin
Pancreas
Increase insulin secretion
Helps restore normal glucose level in blood
MOA of antidiabetic drugs
Biguanide
Thiazolidinediones
Adipose tissue / Muscle
Peripheral Glucose uptake
More glucose leaves the blood and goes into tissue
Helps restore normal glucose level in blood
MOA location
GLP1 receptor agonists
Gut to pancreas
Pancreas
MOA location
Colesevelam
Gut
MOA location
Alpha glucosidase inhibitors
Gut
MOA location
Sulphonylureas meglitinides
Pancreas
MOA location
Pramlintide
Bromocriptine
Brain
MOA location
Metformin
Liver
MOA location
Thiazolidinediones
Muscle / adipose tissue
Type 2 Diabetes treatment
Patients with newly diagnosed diabetes
Comprehensive diabetes self-management education
includes nutrition and eating pattern, physical activity, optimizing metabolic control, and preventing complications.
Weight reduction through diet (for patients with overweight or obesity),
exercise, and behavioral modification can all be used to improve glycemic control,
(the majority of patients with type 2 diabetes will require medication over the course of their diabetes)
A1C target in Diabetes type 2 patients
should be tailored to the individual,
balancing the anticipated reduction in microvascular complications over time with the immediate risks of hypoglycemia.
A reasonable goal of therapy might be an A1C value of ≤7.0 percent (53.0 mmol/mol) for most patients.
Initial treatment for Diabetes Type 2
In the absence of specific contraindications, we suggestmetforminas initial therapy in most patients.
We suggest initiatingmetforminat the time of diabetes diagnosis, along with consultation for lifestyle intervention.
However, for those patients who have clear and modifiable contributors to hyperglycemia and who are motivated to change them
(eg, commitment to reduce consumption of sugar-sweetened beverages) or an A1C near target (ie, <7.5 percent),
a three- to six-month trial of lifestyle modification prior to initiation of pharmacologic therapy is reasonable.
Lifestyle mods, Metformin (after 3-6 months)
Metformin Dosage for
Initial treatment for Diabetes Type 2
The dose ofmetforminshould be titrated to its maximally effective dose
(usually 2000 mg per day in divided doses)
over one to two months, as tolerated.
Metformin should not be administered when estimated glomerular filtration rate (eGFR) is <30mL/min/1.73 m2
or conditions otherwise predisposing to lactic acidosis are present.
500 BID initial Dose??????????? (Up to Date)
For patients with clinical CVD or high cardiovascular risk who cannot takemetformin
Diabetes Type 2
we suggest a glucagon-like peptide-1 (GLP-1) receptor agonist (liraglutide,semaglutide, ordulaglutide)
or
sodium-glucose co-transporter 2 (SGLT2) inhibitor (empagliflozinorcanagliflozin)
that has demonstrated cardiovascular benefit
For patients without clinical CVD and with A1C levels <9 percent
Diabetes Type 2
(in addition to insulin or GLP-1 receptor agonists) include sulfonylureas, SGLT2 inhibitors, DPP-4 inhibitors,repaglinide, orpioglitazone.
Each one of these choices has individual advantages and risks
For patients presenting with symptomatic (eg, weight loss) or severe hyperglycemia with ketonuria,
Diabetes Type 2
Insulin is indicated for initial treatment.
For patients presenting with severe hyperglycemia but without ketonuria or spontaneous weight loss, in whom type 1 diabetes is not likely,
(fasting plasma glucose >250 mg/dL [13.9 mmol/L],
random glucose consistently >300 mg/dL [16.7 mmol/L],
A1C > 9 to 10 percent [74.9 to 85.8 mmol/mol])
Diabetes Type 2
we suggest insulin or a GLP-1 receptor agonist
If inadequate control is achieved (A1C remains >7.0 percent [53.0 mmol/mol] or an alternative patient-specific target level)
Diabetes Type 2
Another medication should be added within two to three months of initiation of the lifestyle intervention andmetformin.
Metformin
Glucophage (Biguanide)
Adjunct to diet and exercise for DM type 2
Monotherapy = 500 BID or 850 QD (with food)
Contra
Sever renal impairment (GFR <30)
Metabolic Acidosis, Diabetic Ketoacidosis
Warning: Lactic acidosis
Interactions:
Increased risk of lactic acidosis with topiramate
Adverse:
N/V/D, flatulence, Asthenia, indigestion, Abdominal discomfort, Lactic acidosis (may be fatal)
MOA of Metformin
Oral diabetic drug Biguanide class (only drug in this class)
Activates the enzyme AMP dependent protein kinase
Primary action; Inhiibts Gluconeogenesis in liver
Decreasing glucose production
(metformin does not cause release of insulin)
Other actions:
Increases glucose uptake insulin sensitivity, fatty acid oxidation
Decreases intestinal glucose absorption
Glucagon like peptide 1 receptor agonist
(GLP-1 agonist)
Drugs
-Glutides
liraglutide (Victoza)
Semaglutide (Ozempic)
Dulaglutide (Trulicity)
Liraglutide (Victoza)
Dose
Give by SC inj in abdomen, thigh, or upper arm once daily.
Initially 0.6mg/day for 1 week,
then increase to 1.2mg/day;
may increase to 1.8mg/day after ≥1 week if additional control is required
GLP-1 Agonist MOA
Food enters small intestine
Small intestine secrets GLP-1 in response to food
GLP-1 slows gastric emptying from stomach
and
goes to pancreas which stimulates insulin secretion
(and suppresses glucagon secretion from pancreas)
Sodium glucose co transporter 2 (SGLT2) inhibitor
Drugs
-gliflozin
empagliflozin (Jardiance)
Canagliflozin (Invokana)
Sulfonylureas
Drugs
Glipizide (Glucotrol) Short action
Glimeride (Amaryl) Short action
Glyburide (Diabeta) Long action
Combinations of this drug with metformin include
Glucovance and Metaglip
Sulfonylureas MOA
Sulfonylureas bind to the sulfonylurea receptor on the adenosine triphosphate (ATP)-sensitive potassium channel (K-ATP channel) of the pancreatic beta cells,
This causes the pancreas to increase insulin secretion
(Insulin secretogogues)
(like an oral insulin)
(can cause hypoglycemia)
Sulfonylureas
Which ones to start with
When a decision has been made to treat with a sulfonylurea,
we suggest a shorter-duration sulfonylurea or one with relatively lower risk for hypoglycemia, such asglipizide,orglimepiride.
Glyburideand other long-acting sulfonylureas have a higher incidence of hypoglycemia.
Dipeptidyl peptidase 4 (DDP-4) inhibitors
-gliptin
sitagliptin (Januvia)
saxagliptin (Onglyza)
linagliptin (Tradjenta)
alogliptin (Nesina)
sitagliptin
(Januvia) (Dipeptidyl peptidase-4 (DPP-4) inhibitor)
Adjunct to diet and exercise in type 2 diabetes, as monotherapy or combination therapy.
Warnings:
Assess renal function before starting therapy and periodically thereafter.
DDP-4 inhibitor MOA
GLP-1 stimulates insulin and suppresses Glucagon
DDP-4 inactivates GLP-1
DDP-4 inhibitors inhibit the DDP-4 enzyme allowing GLP-1 to activate pancreas and lower glucose levels
repaglinide
Prandin (glinide)
Adjunct to diet and exercise in type 2 diabetes
Not for treatment of Type 1 or diabetic ketoacidosis
thiazolidinedione (TZD)
Drugs
-glitazone
pioglitazone (Actos)
rosiglitazone (Avandia)
pioglitazone
Actos (thiazolidinedione) (TZD)
Adjunct to diet and exercise in type 2 diabetes, as monotherapy or in combination with metformin, insulin, or a sulfonylurea.
Not for treating type 1 diabetes or diabetic ketoacidosis.
Contra: NYHA class 3 or IV Heart Failure
Warning:
Congestive Heart Failure
thiazolidinedione (TZD)
MOA
Ligand of the nuclear receptor
peroxisome proliferator activator receptor-y (PPAR-Y)
in liver, muscle and adipose tissue
PPAR-Y receptors in the nucleus
Regulates genes related to glucose and lipid metabolism
Increases insulin sensitivity
Increase insulin mediated glucose uptake by 30-50%
Requires the presence of insulin to work
Other actions: (PPAR-Alpha)
Decreases triglycerides
Increased HDL cholesterol
Decrease in plasma fatty acid level
Misc diabetes meds
Alpha-Glucosidase inhibitors
Acarbose (Precose)
miglitol (glyset)
Bile acid sequestrants (mainly for high lipid panel)
colesevelam
Amylin mimetics
Pramlintide (Symlin)
acarbose
Precose (Alpha-glucosidase inhibitor)
Adjunct to diet in type 2 diabetes, alone or with insulin, metformin, or a sulfonylurea
Take with first bite of each main meal
Contraindications:
Ketoacidosis. Cirrhosis. Inflammatory bowel disease.
Contra:
Transient flatulence, diarrhea, abdominal pain.
Alpha-glucosidase inhibitor MOA / side effects
delays carbohydrate absorption
Sie effects: flatulence
colesevlam
Welchol (Bile acid sequestrant)
Adjunct to diet and exercise in type 2 diabetes mellitus.
Not for the treatment of type 1 diabetes or diabetic ketoacidosis
Contraindications:
History of bowel obstruction. Serum TG>500mg/dL. History of hypertriglyceridemia-induced pancreatitis.
Adverse:
Constipation, dyspepsia, nausea; dysphagia, pancreatitis.
colesevlam (Welchol) Dose
Take with a meal and liquid.
3 tabs twice daily or 6 tabs once daily.
Susp: one 3.75g pkt once daily.
Empty contents into a glass or cup, add 8oz of water, fruit juice, or diet soft drinks; stir and drink.
Do not take susp in its dry form.
colesevlam (Welchol) MOA
Unknown in diabetes
Mainly used for lipids
pramlintide
Symlin (Amylin analogue/amylinomimetic)
Adjunctive treatment in patients with type 1 or type 2 diabetes who use mealtime insulin and who have failed to achieve blood glucose control despite optimal insulin therapy.
Contraindications:
Gastroparesis. Hypoglycemia unawareness.
Warning:
Severe hypoglycemia.
Increased risk of severe hypoglycemia with insulin (esp. type 1 diabetics).
pramlintide Symlin MOA
Liver:
Suppresses the release of glucagon
Stomach:
Slows the food moving from stomach to small intestine
Brain:
Makes you feel full at meals which make you eat less
insulin
The insulin analogs (lispro, aspart, glulisine, glargine, detemir, degludec) were developed to provide more physiologic insulin profiles.
The rapid-acting insulin analogs (insulin lispro, aspart, faster aspart, and glulisine)
have both faster onset and shorter duration of action thanregular insulinfor pre-meal coverage,
while the long-acting analogs have a longer and flatter profile than NPH for basal coverage
Effective use of insulin requires
An understanding of the major variables that affect the degree of glycemic control:
insulin preparation, injection site, injection technique, the size of the subcutaneous depot, and subcutaneous blood flow.
Insulin Onset and peak
Lispro (Humalog)
Aspart (Novolog)
Glulisine (apidra)
Onset
3-15 min
Peak
45-75 min
Insulin Onset and peak
Humulin-R
(regular)
Onset
30 min
Peak
2-4 hours
Insulin Onset and peak
NPH
Humulin - N
Onset
2 hours
Peak
4-12 hours
Insulin Onset and peak
Lantus
(Glargine)
Onset
2 hours
Peak
No peak
Insulin Onset and peak
Detemir
(Levemir)
Onset
2 hours
Peak
3-9 hours
Hoe to prevent lipodystrophy
Rotate injection sites
Humalog adverse reaction
Hypoglycemia
Regular insulin Contraindications
novolin R
During episodes of hypoglycemia
DKA Management
Managed in the inpatient setting (ICU)
Fix metabolic abnormalities
Restore acid base balance
aggressive IV hydration
Treat related conditions and causative factors
HHS Management
Managed in the inpatient setting (ICU)
Assertive rehydration with IV fluids
Monitoring electrolyte balance
Correct hypoglycemia
Correct electrolyte disturbance
Treat related conditions and causative factors
Kussmaul breathing in DKA
Rapid Deep breathing
DKA vs HHS
DKA: (Type 1) Polyuria/Polydipsia Dyspnea Abdominal pain N/V Moderate/severe dehydration Develops in less than 1 day
HHS: (Type 2) Polyuria +/- polydipsia Confusion/ lethargy Severe/Profound dehydration Develops in longer than 1 day
DKA treatment
Continuous IV infusion of regular insulin
same as HHS
HHS treatment
Continuous IV infusion of regular insulin
same as DKA
What is an alert value for hypoglycemia
BGL <70
Treatment tor a hypoglycemic patient with impaired consciousness and no IV access
Glucagon
Glucagon
Contra/adverse
Glucagen
Severe hypoglycemia
Contra: pheochromocytoma
Adverse:
N/V,
Allergic reactions
(urticaria, respiratory distress, hypotension)
Glucagon MOA
Brain:
decreased food intake, appetitie
increased feeling of fullness (satiety)
Pancreas:
Increased insulin secretion
Liver:
Increased glucose production, lipid breakdown
Decreased glucose breakdown, lipid production
Increased ketone body production, AA breakdown
Brown adipose tissue:
Increased resting energy expenditure
Heart:
Increased HR and contractility
Which of the following DM medication is associated with Vitamin B12 deficiency?
repaglinide (Prandin)
acarbose (Precose)
metformin (Glucophage)
pioglitazone (Actos)
metformin (Glucophage)
Which of the following DM medication is associated with CHF?
repaglinide (Prandin)
acarbose (Precose)
metformin (Glucophage)
pioglitazone (Actos)
pioglitazone (Actos)
Which of the following is considered a long-acting insulin
Insulin glargine (Lantus) Insulin lispro (Humalog) Insulin regular (Humulin R) Insulin NPH (Humulin N)
Insulin glargine (Lantus)
A PA administers NPH insulin to a patient who has diabetes at 6:00 AM. When will the patient be at highest risk of experiencing hypoglycemia?
7AM
8AM
9AM
10AM
10AM
Insulin forces which of the following electrolytes out of the plasma and into the cells?
Calcium
Magnesium
Phosphorous
Potassium
Potassium
Rotating injection sites when administering insulin prevents which of the following complications?
Insulin edema
Insulin lipodystrophy
Insulin resistance
Systemic allergic reaction
Insulin lipodystrophy
Which of the following should be taken for a patient who complains of nausea and vomits one hour after taking his glyburide (DiaBeta)?
Give subcutaneous insulin and monitor blood glucose
Monitor blood glucose closely, and look for signs of hypoglycemia
Monitor blood glucose, and assess for signs of hyperglycemia
Give Orange juice immediately
Monitor blood glucose closely, and look for signs of hypoglycemia
When a patient is in diabetic ketoacidosis, the insulin that would be administered is:
vHuman NPH insulin
Human regular insulin
Insulin lispro injection
Insulin glargine injection
Human regular insulin
A patient with diabetes mellitus visits a health care clinic. The patient’s diabetes previously had been well controlled with glyburide (Diabeta), 5 mg PO daily, but recently the fasting blood glucose has been running 180-200mg/dl. Which medication, if added to the clients regimen, may have contributed to the hyperglycemia?
Prednisone (Deltasone)
Atenolol (Tenormin)
Phenelzine (Nardil)
Allopurinol (Zyloprim)
Prednisone (Deltasone)
Which of the following DM medications has a black box warning of the risk of thyroid C-cell tumors?
sitagliptin (Januvia) (DPP4)
colesevelam (Welchol)
liraglutide (Victoza) (GLP-1)
canogliflozin (Invokana) (SGLT2)
liraglutide (Victoza) (SGLT2)
Diabetes Insipidus vs SIADH
DI: High urine output Low levels of ADH Hypernatremia Dehydrated Lose too much fluid
SIADH: Low urinary output High levels of ADH Hyponatremia Overhydrated Retain too much fluid
(Both will present with excessive thirst)
testosterone gel
Androgel
Schedule 3
Warning:
Secondary exposure to testosterone.
Virilization has been reported in children who were secondarily exposed to topical testosterone producrs
Children should avoid contact with unwashed or unclothed application sites
Adverse Reactions:
Acne, prostate disorders, increased PSA, emotional lability, hypertension, gynecomastia, virilization in children.
tolvaptan
Samsca (Selective vasopressin V2-receptor antagonist)
Contraindications:
Autosomal dominant polycystic kidney disease (ADPKD)
Warning:
Initiate and re-initiate in a hospital and monitor serum sodium.
Tolvaptan MOA
Vasopressin attaches to the V2 receptors
This increases the permeability of the aquaporins
Vaptans are a V2 receptor antagonist
They block the V2 receptor so vasopressin cant bind
This causes
dilute urine
Increased free water clearance
Raises serum sodium
Anti vasopressin, increased dilute urine output, increased sodium retention
desmopressin
DDAVP (Vasopressin (synthetic))
Contraindications:
Moderate to severe renal impairment
(CrCl <50mL/min).
Hyponatremia, or history of.
Diabetes insipidus drugs
Carbamazepine
Stimulates the releases of vasopressin from the pituitary gland
May act directly on the renal tubules
Diabetes insipidus drugs
Thiazides
Inhibits co transport of sodium and chloride
inducing natriuresis
Diabetes insipidus drugs
Amiloride
Blocking of ENaA with amiloride reduces the lithium induced down regulation of AQP2 expression and protects the cellular composition of the collecting duct
Vasopressin antagonists for SIADH
-Vaptans
Conivaptan Tolvaptan Lixivaptan Relcovaptan Satavaptan Mozavaptan SSR-149415
Vasopressin agonists for Diabetes insipidus
-pressins
Felypressin
Lypressin
Desmopressin
Terlipressin
Drugs that act on the Hypothalamus
Somatostatin analogs
octreotide
Dopamine agonists (D2)
Bromocriptine
Cabergoline
Drugs that act on the Anterior pituitary
Recombinant GH
Somatropin
Insulin like growth factor 1
Mecasermin
GH antagonists
Pegvisomant
Drugs that act on the Posterior pituitary
Oxytocin
Antidiuretic hormone and analogs
Vasopressin
Desmopressin
Vasopressin antagonists
Conivaptan
**Pressins and vaptans
cabergoline
Dostinex (Dopamine agonist)
Hyperprolactinemic disorders, either idiopathic or due to pituitary tumors.
Uncontrolled hypertension. Sensitivity to ergot alkaloids.
Adverse Reactions:
GI upset, dizziness, fatigue, postural hypotension
Dopamine agonist MOA
Suppress GH levels via direct activation of dopamine receptors
pegvisomant
Somavert (GH receptor antagonist)
Treatment of acromegaly when response to surgery and/or radiation therapy and/or other medical therapies is inadequate or inappropriate.
Interactions:
May need to reduce dose of inulin & oral hypoglycemics
Adverse:
Infection, pain, N/V/D, Elevated LFT’s, Flu syndrome
pegvisomant
Somavert (GH receptor antagonist)
Treatment of acromegaly when response to surgery and/or radiation therapy and/or other medical therapies is inadequate or inappropriate.
Interactions:
May need to reduce dose of inulin & oral hypoglycemics
Adverse:
Infection, pain, N/V/D, Elevated LFT’s, Flu syndrome
pegvisomant MOA
Slide 229 ????
Blocks the GH binding site
causing a G120K mutation in binding site
Peg polymer
Stops the JAK/STAT signaling
Octreotideand other long acting analogues of somatostatin, have a number of established clinical indications including
The treatment of
secretory diarrhea,
gastrointestinal bleeding,
inhibition of tumor growth,
and imaging neuroendocrine and other solid tumors.
***Diarrhea, GI bleed, Tumor inhibition
Octreotide
Sandostatin (somatostatin analog)
Acromegaly unresponsive to or cannot be treated with surgical resection
Warnings:
Diabetes, Hypothyroidism, CVD
Interaction:
Potentiates bromocriptine
Adverse:
Gallbladder abnormalities (gallstones, biliary sludge)
GI upset, bradycardia
Growth Hormone
Hypothalamus secretes
GHRH (growth hormone releasing factor
Which goes to anterior pituitary
Anterior pituitary secretes
GH (growth hormone)
Which goes to liver
Liver secretes IGF-1
Which goes to bone, muscle and fat tissues
Somatropin recominant
Nutropin
Treatment of children with growth failure due to growth hormone deficiency (GHD), idiopathic short stature (ISS),
Contraindications:
Acute critical illness due to surgical complications or multiple accidental trauma or those with acute respiratory failure. Children with closed epiphysis. Active malignancy.
Warnings/Precautions:
Increased mortality in those with acute critical illness
Cortisol control mechanism
Hypothalamus secretes CRH CRH stimulates Anterior pituitary Anterior pituitary secretes ACTH ACTH stimulates Adrenal cortex Adrenal cortex secretes cortisol
As cortisol increases it is a negative feedback to control the release of CRH and ACTH
Addison’s disease (adrenal crisis)
In a patientwithouta previous diagnosis of adrenal insufficiency what is initial treatment?
Dexamethasone, which is not measured in cortisol assays, should be used rather thanhydrocortisonewhile biochemical testing is performed
Addison’s disease (adrenal crisis)
After initial treatment and testing
The vast majority of patients with primary adrenal insufficiency eventually require mineralocorticoid replacement withfludrocortisone.
We suggest adjusting the fludrocortisone dose to lower the plasma renin activity to the upper normal range
Steroids for Addison’s Disease
Glucocorticoids
Prednisone 3-5mg QD
Hydrocortisone 15-25mg divided into 2-3 doses QD
Dexamethasone 05.mg QD
Mineralocorticoids
Fludrocortisone .05 - .2 mg QD
Androgen
DHEA 25-50 mg QD
Steroid withdrawal syndrome
Adrenal insufficiency with too rapid withdrawal of corticosteroids after prolonged therapy
Fever Myalgia Arthralgia Malaises Itchy skin nodules Rhinitis Conjunctivitis
Dexamethasone Suppression test
Dexamethasone acts like cortisol, lowers the amount of ACTH released by the pituitary gland
Normal
Pituitary makes less ACTH
Adrenals make less Cortisol
Cushing’s syndrome
Give Dexamethasone
Pituitary makes less ACTH
Adrenals still make cortisol
Cushing Syndrome Treatment
In patients with Cushing’s disease who were not cured by pituitary surgery,
medical therapy targeting the corticotroph tumor
Metastatic or occult ectopic ACTH-secreting tumors may respond to
somatostatin analog treatment, adrenal enzyme inhibitors ormitotane
pasireotide
Signifor (somatostatin analog)
Patients with Cushing’s disease for whom pituitary surgery is not an option or has not been curative
Interactions:
Caution with antiarrhythmics or other drugs that may prolong the QT interval
Adverse Reactions:
Diarrhea, nausea, hyperglycemia, cholelithiasis, QT prolongation
Mitotane
Lysodren
Inoperable adrenal cortical carcinoma
Interactions
Concomitant oral anticoagulants
Which of the following is not a MOA of bisphosphonates?
Stimulate osteoclast apoptosis
Increase in osteoclast-mediated bone resorption
Decrease in osteoclast function
Inhibit cholesterol synthetic pathway
Increase in osteoclast-mediated bone resorption
Which of the following hypoparathyroidism medications has a boxed warning of a potential risk of osteosarcoma?
Recombinant PTH (Natpara)
Alendronate (Fosamax)
Calcitriol (Rocaltrol)
Vitamin D
Recombinant PTH (Natpara)
Which of the following is not a MOA of PTH?
Increase calcitriol formation in kidney
Release calcium via bones
Decreases absorption of dietary phosphorus in small intestine
Decreases excretion of calcium in kidney
Decreases absorption of dietary phosphorus in small intestine
Which thyroid medication is safe for pregnant females with hyperthyroidism?
Methimazole (Tapazole)
Propylthiouracil (PTU)
Radioactive iodine
Levothyroxine (Synthroid)
Propylthiouracil (PTU)
Which drug is not considered a cause of primary hypothyroidism?
Amiodarone (Cardarone)
Amoxicillin (Amoxil)
Lithium (Lithobid)
Levothyroxine (Synthroid)
Amoxicillin (Amoxil)
Levothyroxine (Synthroid)
Which of the following is the initial dose for healthy younger people who have been hypothyroid for a few months?
- 4 mcg/kg/day
- 5 mcg/kg/day
- 6 mcg/kg/day
- 7 mcg/kg/day
1.6 mcg/kg/day
Which of the following type of thyroiditis is associated with supportive treatment involving ASA and no steroids?
Subacute thyroiditis
Fibrous (Reidel) thyroiditis
Hashimoto thyroiditis
Suppurative thyroiditis
Subacute thyroiditis
Which of the following is considered a somatostatin analog?
Carbergoline
Somatropin
Pegvisomant
Octreotide
Octreotide
Which of the following is considered a mineralocorticoid medication?
Hydrocortisone
Fludrocortisone
Dexamethasone
Prednisone
Fludrocortisone
