Pharm Endocrine Exam Flashcards
1
Q
Bisphosphonates
A
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
2
Q
Bisphosphonates meds
A
Alendronate = Fosamax Risedronate Etidronate Tiludronate Pamidronate Ibandronate Zoledronate
All end in -dronate
3
Q
Calcium carbonate
A
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)
4
Q
Calcitriol Indications
A
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.
5
Q
Calcitriol Contraindications / interactions
A
Contraindications: Hypercalcemia, Vitamin D Therapy, Vitamin D toxicity, Nursing mothers
Interactions
Hypermagnesemia
Magnesium containing antacids
Arrhythmias with digitalis if hypercalcemia occurs
6
Q
Recombinant PTH
A
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
7
Q
MOA of Recombinant PTH
A
Bone = Losing calcium
Small intestine = Absorption of calcium
Kidney = Reabsorption calcium
8
Q
MOA of Calcitriol
A
Increases Ca2+ and PO4- absorption in small intestine
Active form of Vitamin D
9
Q
For patients with significant symptoms of hyperthyroidism or patients with hyperthyroidism complications like elderly, cardiovascular disease
A
First line Beta blockers (atenolol 25-50) (200 max) QD
Along with a thionamide
Specifically Methimazole
10
Q
For women who wish to become pregnant with hyperthyroidism
A
Propylthiouracil (PTU would be the preferred drug during the first trimester of pregnancy and can be continued throughout pregnancy
11
Q
Management of Hyperthyroidism flow chart
A
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
12
Q
Beta Blockers and hyperthyroidism
A
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)
13
Q
Methimazole
A
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
14
Q
Proppylthiouracil
A
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
15
Q
MOA of Thionamides
Methimazole
Propylthiouracil
A
Inhibits thyroid hormone synthesis
Inhibit the oxidation of iodine
PTU: inhibits peripheral conversion of T4 to T3
16
Q
Thyroid Storm
A
Slide 40
17
Q
Hypothyroidism
Primary vs Secondary
A
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
18
Q
Primary hypothyroidism goals
A
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).
19
Q
Treatment of choice for primary hypothyroidism
A
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.
20
Q
Initial dose of Levothyroxine for
Primary Hypothyroidism
A
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)
21
Q
Dosing for Levothyroxine
A
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)
22
Q
Levothyroxine sodium
A
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
23
Q
Thyroiditis
A
Subacute painful
(de Quervain’s, granulomatous, giant cell)
Drug induced
(usually amiodarone)
24
Q
MOA of antidiabetic drugs
Biguanides
Thiazolidines
-diones
A
Liver
Decrease glucose production
= Less glucose in the blood
Helps restore normal glucose level in blood
25
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,
26
MOA of antidiabetic drugs
Meglitinides
Sulfonylureas
Phenylalanine derivatives
insulin
Pancreas
Increase insulin secretion
Helps restore normal glucose level in blood
27
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
28
MOA location
| GLP1 receptor agonists
Gut to pancreas
| Pancreas
29
MOA location
| Colesevelam
Gut
30
MOA location
| Alpha glucosidase inhibitors
Gut
31
MOA location
| Sulphonylureas meglitinides
Pancreas
32
MOA location
Pramlintide
Bromocriptine
Brain
33
MOA location
| Metformin
Liver
34
MOA location
| Thiazolidinediones
Muscle / adipose tissue
35
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)
36
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.
37
Initial treatment for Diabetes Type 2
In the absence of specific contraindications, we suggest metformin as initial therapy in most patients.
We suggest initiating metformin at 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)
38
Metformin Dosage for
| Initial treatment for Diabetes Type 2
The dose of metformin should 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 <30 mL/min/1.73 m2
or conditions otherwise predisposing to lactic acidosis are present.
500 BID initial Dose??????????? (Up to Date)
39
For patients with clinical CVD or high cardiovascular risk who cannot take metformin
Diabetes Type 2
we suggest a glucagon-like peptide-1 (GLP-1) receptor agonist (liraglutide, semaglutide, or dulaglutide)
or
sodium-glucose co-transporter 2 (SGLT2) inhibitor (empagliflozin or canagliflozin)
that has demonstrated cardiovascular benefit
40
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, or pioglitazone.
Each one of these choices has individual advantages and risks
41
For patients presenting with symptomatic (eg, weight loss) or severe hyperglycemia with ketonuria,
Diabetes Type 2
Insulin is indicated for initial treatment.
42
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
43
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 and metformin.
44
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)
45
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
46
Glucagon like peptide 1 receptor agonist
(GLP-1 agonist)
Drugs
-Glutides
liraglutide (Victoza)
Semaglutide (Ozempic)
Dulaglutide (Trulicity)
47
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
48
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)
49
Sodium glucose co transporter 2 (SGLT2) inhibitor
| Drugs
-gliflozin
empagliflozin (Jardiance)
Canagliflozin (Invokana)
50
Sulfonylureas
| Drugs
Glipizide (Glucotrol) Short action
Glimeride (Amaryl) Short action
Glyburide (Diabeta) Long action
Combinations of this drug with metformin include
Glucovance and Metaglip
51
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)
52
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 as glipizide, or glimepiride.
Glyburide and other long-acting sulfonylureas have a higher incidence of hypoglycemia.
53
Dipeptidyl peptidase 4 (DDP-4) inhibitors
-gliptin
sitagliptin (Januvia)
saxagliptin (Onglyza)
linagliptin (Tradjenta)
alogliptin (Nesina)
54
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.
55
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
56
repaglinide
Prandin (glinide)
Adjunct to diet and exercise in type 2 diabetes
Not for treatment of Type 1 or diabetic ketoacidosis
57
thiazolidinedione (TZD)
| Drugs
-glitazone
pioglitazone (Actos)
rosiglitazone (Avandia)
58
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
59
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
60
Misc diabetes meds
Alpha-Glucosidase inhibitors
Acarbose (Precose)
miglitol (glyset)
Bile acid sequestrants (mainly for high lipid panel)
colesevelam
Amylin mimetics
Pramlintide (Symlin)
61
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.
62
Alpha-glucosidase inhibitor MOA / side effects
delays carbohydrate absorption
Sie effects: flatulence
63
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.
64
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.
65
colesevlam (Welchol) MOA
Unknown in diabetes
Mainly used for lipids
66
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).
67
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
68
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 than regular insulin for pre-meal coverage,
while the long-acting analogs have a longer and flatter profile than NPH for basal coverage
69
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.
```
70
Insulin Onset and peak
Lispro (Humalog)
Aspart (Novolog)
Glulisine (apidra)
Onset
3-15 min
Peak
45-75 min
71
Insulin Onset and peak
Humulin-R
(regular)
Onset
30 min
Peak
2-4 hours
72
Insulin Onset and peak
NPH
Humulin - N
Onset
2 hours
Peak
4-12 hours
73
Insulin Onset and peak
Lantus
(Glargine)
Onset
2 hours
Peak
No peak
74
Insulin Onset and peak
Detemir
(Levemir)
Onset
2 hours
Peak
3-9 hours
75
Hoe to prevent lipodystrophy
Rotate injection sites
76
Humalog adverse reaction
Hypoglycemia
77
Regular insulin Contraindications
| novolin R
During episodes of hypoglycemia
78
DKA Management
Managed in the inpatient setting (ICU)
Fix metabolic abnormalities
Restore acid base balance
aggressive IV hydration
Treat related conditions and causative factors
79
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
80
Kussmaul breathing in DKA
Rapid Deep breathing
81
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
```
82
DKA treatment
Continuous IV infusion of regular insulin
| same as HHS
83
HHS treatment
Continuous IV infusion of regular insulin
| same as DKA
84
What is an alert value for hypoglycemia
BGL <70
85
Treatment tor a hypoglycemic patient with impaired consciousness and no IV access
Glucagon
86
Glucagon
| Contra/adverse
Glucagen
Severe hypoglycemia
Contra: pheochromocytoma
Adverse:
N/V,
Allergic reactions
(urticaria, respiratory distress, hypotension)
87
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
88
Which of the following DM medication is associated with Vitamin B12 deficiency?
repaglinide (Prandin)
acarbose (Precose)
metformin (Glucophage)
pioglitazone (Actos)
metformin (Glucophage)
89
Which of the following DM medication is associated with CHF?
repaglinide (Prandin)
acarbose (Precose)
metformin (Glucophage)
pioglitazone (Actos)
pioglitazone (Actos)
90
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)
91
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
92
Insulin forces which of the following electrolytes out of the plasma and into the cells?
Calcium
Magnesium
Phosphorous
Potassium
Potassium
93
Rotating injection sites when administering insulin prevents which of the following complications?
Insulin edema
Insulin lipodystrophy
Insulin resistance
Systemic allergic reaction
Insulin lipodystrophy
94
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
95
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
96
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)
97
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)
98
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)
99
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.
100
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.
101
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
102
desmopressin
DDAVP (Vasopressin (synthetic))
Contraindications:
Moderate to severe renal impairment
(CrCl <50mL/min).
Hyponatremia, or history of.
103
Diabetes insipidus drugs
| Carbamazepine
Stimulates the releases of vasopressin from the pituitary gland
May act directly on the renal tubules
104
Diabetes insipidus drugs
| Thiazides
Inhibits co transport of sodium and chloride
| inducing natriuresis
105
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
106
Vasopressin antagonists for SIADH
-Vaptans
```
Conivaptan
Tolvaptan
Lixivaptan
Relcovaptan
Satavaptan
Mozavaptan
SSR-149415
```
107
Vasopressin agonists for Diabetes insipidus
-pressins
Felypressin
Lypressin
Desmopressin
Terlipressin
108
Drugs that act on the Hypothalamus
Somatostatin analogs
octreotide
Dopamine agonists (D2)
Bromocriptine
Cabergoline
109
Drugs that act on the Anterior pituitary
Recombinant GH
Somatropin
Insulin like growth factor 1
Mecasermin
GH antagonists
Pegvisomant
110
Drugs that act on the Posterior pituitary
Oxytocin
Antidiuretic hormone and analogs
Vasopressin
Desmopressin
Vasopressin antagonists
Conivaptan
****Pressins and vaptans
111
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
112
Dopamine agonist MOA
Suppress GH levels via direct activation of dopamine receptors
113
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
114
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
115
pegvisomant MOA
| Slide 229 ????
Blocks the GH binding site
causing a G120K mutation in binding site
Peg polymer
Stops the JAK/STAT signaling
116
Octreotide and 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
117
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
118
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
119
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
120
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
121
Addison's disease (adrenal crisis)
| In a patient without a previous diagnosis of adrenal insufficiency what is initial treatment?
Dexamethasone, which is not measured in cortisol assays, should be used rather than hydrocortisone while biochemical testing is performed
122
Addison's disease (adrenal crisis)
| After initial treatment and testing
The vast majority of patients with primary adrenal insufficiency eventually require mineralocorticoid replacement with fludrocortisone.
We suggest adjusting the fludrocortisone dose to lower the plasma renin activity to the upper normal range
123
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
124
Steroid withdrawal syndrome
Adrenal insufficiency with too rapid withdrawal of corticosteroids after prolonged therapy
```
Fever
Myalgia
Arthralgia
Malaises
Itchy skin nodules
Rhinitis
Conjunctivitis
```
125
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
126
Cushing Syndrome Treatment
In patients with Cushing’s disease who were not cured by pituitary surgery,
medical therapy targeting the corticotroph tumor
such as cabergoline or pasireotide
------------------------------------------------
Metastatic or occult ectopic ACTH-secreting tumors may respond to
somatostatin analog treatment, adrenal enzyme inhibitors or mitotane
127
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
128
Mitotane
Lysodren
Inoperable adrenal cortical carcinoma
Interactions
Concomitant oral anticoagulants
129
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
130
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)
131
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
132
Which thyroid medication is safe for pregnant females with hyperthyroidism?
Methimazole (Tapazole)
Propylthiouracil (PTU)
Radioactive iodine
Levothyroxine (Synthroid)
Propylthiouracil (PTU)
133
Which drug is not considered a cause of primary hypothyroidism?
Amiodarone (Cardarone)
Amoxicillin (Amoxil)
Lithium (Lithobid)
Levothyroxine (Synthroid)
Amoxicillin (Amoxil)
| Levothyroxine (Synthroid)
134
Which of the following is the initial dose for healthy younger people who have been hypothyroid for a few months?
1. 4 mcg/kg/day
1. 5 mcg/kg/day
1. 6 mcg/kg/day
1. 7 mcg/kg/day
1.6 mcg/kg/day
135
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
136
Which of the following is considered a somatostatin analog?
Carbergoline
Somatropin
Pegvisomant
Octreotide
Octreotide
137
Which of the following is considered a mineralocorticoid medication?
Hydrocortisone
Fludrocortisone
Dexamethasone
Prednisone
Fludrocortisone
