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106 Cards in this Set

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Hypothalamic Agents

What is Somatotropin?
a growth hormone; stimulates the growth & metabolism of almost all cells in the body

recombinant form of human GH, restores normal growth & metabolic GH effects in GH-deficient individuals
Hypothalamic Agents

What happens with a deficiency of somatotropin?

With an excess?
Deficiency = Dwarfism

Excess = Acromegaly (usually caused by a pituitary tumor)
Hypothalamic Agents

What is Octreotide?
a synthetic growth hormone (GH) antagonist structurally related to somatostatin, inhibits acromegaly

Inhibits production of GH & to a lesser extent , of TSH, glucagon, insulin, & gastrin
Hypothalamic Agents

What is Pegvisomant?
newest agent that is GH antagonist, blocks GH receptors

Ameliorates effects of excess GH production, acromegaly
Anterior Pituitary Agents

Agents (5)?
Corticotropin (ACTH, Acthar)
Cosyntropin (Cortosyn)
Somatrem (Protropin)
Somatropin (Genotropin, Humatrope, others)
Thyrotropin [Thyrogen, Thyroid-stimulating hormone (TSH)]
Posterior Pituitary Agents

What is Anti-Diuretic Hormone (ADH)?
conserves H2O in the body

Secreted by the posterior pituitary when the hypothalamus senses low plasma volume or if osmolality is too high
Posterior Pituitary Agents

Agents (2)?
Used for SIADH

Desmopressin Acetate (DDAVP, Stimate) - most common form of ADH in use - intranasal form most common

Vasopressin (Pitressin) - drug for Diabetes Insipidus, potent vasoconstrictor
Thyroid Drugs

What are the two types of cells in the thyroid gland & what do they secrete?
Thyroid gland: consists of two types of cells which secrete different hormones.

Parafollicular cells: secrete calcitonin
Follicular cells: secrete thyroid hormones (T4 & T3)
Thyroid Drugs

What role does iodine play w/Thyroid function?
Iodine is essential for the synthesis of T4 and T3 (provided via intake)
Thyroid Drugs

What is Hashimoto's thyroiditis?
autoimmune thyroiditis - most common presentation of hypothyroidism
Thyroid Drugs (Hypothyroidism)

Agents (3)?
Levothyroxine (Levothroid, Synthroid, others)
Liothyronine (Cytomel, Triostat) - specific for T3
Thyroid (Armour Thyroid, Westhroid)
Antithyroid Drugs

What is the most common presentation of hyperthyroidism?

How much more common in women?

In which age group is it most common?
Grave's disease is the most common presentation

4-8xs more common in women
30-40 year olds most common
Antithyroid Drugs (Hyperthyroidism)

Agents (4)?
Thioamides:
Methimazole (Tapazole)
Potassium Iodide (ThyroShield, SSKI)

Propylthiouracil (PTU)
Radioactive Iodine (I131, RAI)
Antithyroid Drugs

What are concerns about methimazole?
Methimazole (Tapazole) is a thioamide and is pregnancy category D - crosses the placenta more readily.
Antithyroid Drugs

What are concerns about Sodium iodine-131?
Radioactive Iodine (I-131, RAI) destroys follicular cells with radiation (contraindicated in pregnancy)

Used to shrink thyroid prior to surgery
Antithyroid Drugs

What is Lugol's solution?
nonreactive iodine, inhibits organificaiont & hormone release, reduce the size & vascularity of gland
What are the three essential classes of steroids secreted by the adrenal glands?
Glucocorticoids
Mineralcorticoids
Gonadocorticoids
Which two steroids are known as corticosteroids or adrenocortical hormones"?"
Glucocorticoids & mineralocorticoids
95% of the mineralocorticoids secreted by the adrenals are what?
Aldosterone
What is the primary function of Aldosterone?

Aldosterone + Androgen = ??
The primary function of aldosterone is to promote Na reabsorption & K+ excretion by the renal tubules, thus regulating plasma volume.

Aldosterone + Androgen = Mineralocorticoid
What does the kidney due when plasma volume is low?
The kidneys secrete renin --> production of Angiotensin II

Angiotensin II --> aldosterone secretion --> promonts Na & water retention
What is hyperaldosteronism?
condition from excessive aldosterone secretion usually as a result of adrenal tumors, characterized by hypertension and hypokalemia.
How many glucocorticoids are secreted by the adrenal cortex?
More than 30 glucocorticoids are secreted.
What is hydrocortisone?
The most important pharmacologically glucocorticoid. Affects the metabolism of nearly every cell & prepares the body for long term stress.
What are five effects of glucocorticoids?
Increases blood glucose
Increases the breakdown of proteins & lipids & their utilization as energy sources.
Suppresses the inflammatory response
Increases the sensitivity of vascular smooth muscle to norepinephrine & angiotensin II.
Influences the CNS by affecting mood & maintaing normal brain excitability.
What is the first (of four) steps of glucocorticoid secretion?
Secretion begins with corticotropin-releasing hormone (CRF) secreted by the hypothalamus.
What is the second (of four) steps of glucocorticoid secretion?
CRF travels to the pituitary, where it causes the release of ACTH.
What is the third (of four) steps of glucocorticoid secretion?
ACTH then travels through the blood & reaches the adrenal cortex, causing it to release glucocorticoids.
What is the fourth (of four) steps of glucocorticoid secretion?
When the level of cortisol in the blood increases, it provides negative feedback to the hypothalamus and the pituitary to shut off further release of glucocorticoids.
What is adrenal insufficiency?

What is the role of glucocorticoids in relationship to adrenal insufficiency?
Lack of corticosteroid.

Glucocorticoids are used as replacement therapy for adrenal insufficiency and to decrease inflammation and immune responses. Need to taper when d/c to prevent adrenal suppression.
Name the main twelve uses of glucocorticoid?
Adrenal insufficiency
Allergies (seasonal rhinitis)
Chronic inflammatory bowel disease
Asthma & COPD
Edematous states caused by hepatic, neurological & renal disorders
Neoplastic disease
Post-transplant surgery
Rheumatic diseases
Shock
Skin disorders (rash, contact dermatitis, etc.)
Others
How might glucocorticoids interact with

anti-diabetic agents?
Hyperglycemic effects may decrease the effectiveness of the anti-diabetic agents.
How might glucocorticoids interact with

NSAIDs?
Combining with NSAIDs increases the risk for PUD
How might glucocorticoids interact with

non-potassium sparing diuretics?
Administering with non-potassium-sparing diuretics --> hypokalemia & hypocalcemia.
Glucocorticoid prescribing strategies:

dosing?
Keep doses to the lowest possible amount to achieve a therapeutic effect.
Glucocorticoid prescribing strategies:

administration?
Administer every other day to limit adrenal atrophy.
Glucocorticoid prescribing strategies:

for acute conditions?
For acute conditions, prescribe large amounts for a few days, and then gradually decrease the does until discontinued.
Glucocorticoid prescribing strategies:

to decrease systemic effects?
To decrease the possibility of systemic effects, use inhalation, topical or intra-arterial routes.
What does long-term administration of glucocorticoids put a person at risk for?
Cushing's syndrome
Name two short-acting glucocorticoids

What patient would be using this?
Cortisone (Cortistan, Cortone)
Hydrocortisone (Cortef, Hydrocortone, others)

Usually given as a topical for skin irritation.
Name four intermediate acting glucocorticoids

What patient would be using this?
Methylprednisolone (Medrol, others)
Prednisolone (Delta-Cortef, others)
Prednisone (Deltasone, Meticorten, others)

Pt with hives in an urgent care receiving via IV
Prednisone is for COPD or chemo patient.
Name two long-acting glucocorticoids

What pt would be using this?
Betamethasone (Celestone)
Dexamethasone (Decadron, Dexasone, others)

Dexamethasone suppression test - r/o Cushing's
What is the Somogyi Effect & what is the treatment?
Nocturnal hypoglycemia develops stimulating a surge of counter regulatory hormones which raises blood sugar.

Tx: Reduce or omit h.s. dose of insulin
What is the Dawn Phenomenon & what is the treatment?
Results when tissue becomes desensitized to insulin nocturnally - blood glucose becomes progressively elevated throughout the night.

Tx: Add or increase the h.s. dose of insulin
Diabetes Drugs: Biguanides

Agent (1)?
Metformin (Glucophage)
Diabetes Drugs: Biguanides

Indications?
Drug of choice; first line therapy for Type 2 DM, promotes weight loss

Contraindicated in liver disease & renal dysfunction (serum creatinine ≥ 1.5 males & 1.4 females) need to monitor creatinine.
Diabetes Drugs: Biguanides

MOA?
Decreases hepatic gluconeogenesis, improves insulin sensitivity, increases glucose utilization by muscle.

Does not cause insulin secretion, therefore no concern for hypoglycemia.
Diabetes Drugs: Biguanides

Adverse Effects?
Nausea, vomiting, diarrhea, decreased appetite
Rare (but fatal): lactic acidosis (s/s muscle pain).

Stop use for 48 hrs after procedures w/contrast. Need to check creatinine before restarting metformin.
Diabetes Drugs: Insulin Secretagogues, Nonsulfonylureas (Glinides)

Agents (2)?
Nateglinide (Starlix)
repaglinide (Prandin) - affected by renal impairment
Diabetes Drugs: Insulin Secretagogues, Nonsulfonylureas (Glinides)

Indications?
Monotherapy or combination therapy for Type 2 DM

Use with caution in liver dysfunction.
Dose adjustment required for renal dysfunction
Diabetes Drugs: Insulin Secretagogues, Nonsulfonylureas (Glinides)

MOA?
Stimulates insulin release from pancreas

Rapid onset (give w/ meals) & short duration of action (requires TID dosing)
Diabetes Drugs: Insulin Secretagogues, Nonsulfonylureas (Glinides)

Adverse Effects?
Hypoglycemia, diarrhea, arthralgia, headache, sinusitis, upper respiratory infection

Several drug-drug interactions
Diabetes Drugs: Insulin Secretagogues, Sulfonylureas

Agents (6)?
Chlorpropamide (Diabinese) - older agents, disulfiram rxn
Tolazamide (Tolinase) - older agents
Tolbutamide (Tol-Tab) - older agents
Glyburide (Diabeta, Micronase)
Glipizide (Glucotrol)
Glimepiride (Amaryl)
Diabetes Drugs: Insulin Secretagogues, Sulfonylureas

Indications?
Monotherapy or combination therapy for Type 2 DM

Use with caution in liver dysfunction.
Dose adjustment required for renal dysfunction
Diabetes Drugs: Insulin Secretagogues, Sulfonylureas

MOA?
Stimulates insulin release from pancreas, enhances beta cell sensitivity to glucose

Over time, response to therapy may diminish. Possibly desensitizes receptors
Diabetes Drugs: Insulin Secretagogues, Sulfonylureas

Adverse Effects?
Hypoglycemia, nausea, bloating, weight gain, photosensitivity, disulfiram reaction (chlorpropamide)

Several drug-drug interactions
Use caution w/sulfa allergy
Diabetes Drugs: Thiazolidinediones

Indications?
Monotherapy or combination therapy for Type 2 DM - 3rd line agent Reserved when other agents not working

Use with caution (if at all) in liver dysfunction – baseline LFTs & periodically afterwards
Contraindicated in NYHA class III or IV
Diabetes Drugs: Thiazolidinediones

Agents (2)?
Pioglitazone (Actos)
Rosiglitazone (Avandia) – REMS program, no new pts
Diabetes Drugs: Thiazolidinediones

MOA?
Increases receptor sensitivity to insulin, decreases both insulin resistance & hepatic gluconeogenesis. No increase of insulin secretion
Diabetes Drugs: Thiazolidinediones

Adverse Effects?
Hepatotoxicity, weight gain, peripheral edema, rash, macular edema, heart failure exacerbation, increase risk of MI (rosiglitazone)

Several drug-drug interactions, metabolized by liver
May increase risk of osteoporosis
May increase risk of bladder cancer (pioglitazone)
Diabetes Drugs: Alpha-glucosidase Inhibitors

Indications?
Adjunct therapy only for Type 2 DM, esp if post-prandial BS elevated.

Do not use in renal dysfunction (creatinine > 2.0)
Contraindicated in malabsorption, IBD, or intestinal obstruction.
Diabetes Drugs: Alpha-glucosidase Inhibitors

Agents (2)?
Acarbose (Precose) – baseline LFTs then periodically afterwards
Miglitol (Glyset)
Diabetes Drugs: Alpha-glucosidase Inhibitors

MOA?
Reduces rate & extent of CHO digestion & absorption
Diabetes Drugs: Alpha-glucosidase Inhibitors

Adverse Effects?
Flatulence, diarrhea, abdominal pain, decreased absorption of iron (anemia)

May influence absorption of other drugs.
Glucose (dextrose) is recommended for treating hypoglycemia as sucrose metabolism is inhibited.
Diabetes Drugs: Glucagon-like Peptide-1 Agonists

Indications?
Monotherapy (exenatide) or combination therapy for Type 2 DM; generally considered as adjunct – does not replace insulin. For pts who fail metformin alone, or with glinides or sulfonylureas

Contraindicated in severe renal dysfunction (both), h/o pancreatitis (both), & h/o thyroid CA (liraglutide)
Diabetes Drugs: Glucagon-like Peptide-1 Agonists

Agents (2)?
Exenatide (Byetta)
Liraglutide (Victoza)

REMS program - d/t risk for pancreatitis & thyroid tumors
Diabetes Drugs: Glucagon-like Peptide-1 Agonists

MOA?
Increase insulin release in the presence of elevated glucose concentrations, decrease glucagon secretion in a glucose-dependent manner & delay gastric emptying.
Diabetes Drugs: Glucagon-like Peptide-1 Agonists

Adverse Effects
Nausea, vomiting, diarrhea, headache hypoglycemia, pancreatitis, teratogenic, injection site reactions, renal failure, thyroid tumors

Several drug-drug interactions
Diabetes Drugs: Dipeptidyl Peptidase-4 Inhibitors

Indications?
Monotherapy or combination therapy for Type 2 DM; generally considered as adjunct therapy

Contraindicated in ESRD & dose adjustment in renal impairment (sitagliptin, saxagliptin)
Diabetes Drugs: Dipeptidyl Peptidase-4 Inhibitors

Agents (3)?
Sitagliptin (Januvia)
Saxagliptin (Onglyza)
Linagliptin (Tradjenta)
Diabetes Drugs: Dipeptidyl Peptidase-4 Inhibitors

MOA?
Inhibit the degradation of GiP and GLP-1
Diabetes Drugs: Dipeptidyl Peptidase-4 Inhibitors

Adverse Effects?
Increased risk of infection (URI --> sepsis), headache, hypoglycemia, pancreatitis, hypersensitivity reactions, peripheral edema (saxagliptin)

Several drug-drug interactions (saxagliptin)
Diabetes Drugs: Amylin Receptor Agonists

Indications?
Adjunct therapy for Type 1 & Type 2 DM

Contraindicated in pts with hypoglycemic unawareness or gastroparesis
Black Box warning for individuals while driving
Diabetes Drugs: Amylin Receptor Agonists

Agents?
Pramlintide (Symlin)

When initiating, reduce dose of any secretagogues, reduce insulin dose by at least 50%
Diabetes Drugs: Amylin Receptor Agonists

MOA?
Inhibit the degradation of GiP & GLP-1
Diabetes Drugs: Amylin Receptor Agonists

Adverse Effects?
Abdominal pain, loss of appetite, nausea, vomiting, hypoglycemia, dizziness, headache, cough, fatigue

Severe hypoglycemia with concurrent insulin or oral hypoglycemic agent
Diabetes Drugs: Combination Drugs & Others

Agents
Glipizide/Metformin (Metaglip)
Glyburide/Metformin (Glucovance)
Rosiglitazone/Glimepride (Avandaryl)
Pioglitazone/Metformin (ACTOplusmet)
Rosiglitazone/Metformin (Avandamet)
Insulin Preparations: Rapid Acting

Agents (3)?
Insulin Lispro (Humalog)
Insulin Aspart (NovoLog)
Insulin Glulisine (Apidra)

SQ only
Insulin Preparations: Rapid Acting

Onset of Action?
5-15 minutes

mimics body kinetics the best
Insulin Preparations: Rapid Acting

Peak Action?
30-90 minutes
Insulin Preparations: Rapid Acting

Duration of Action?
< 5 hours
Insulin Preparations: Short Acting

Agents (1)?
Regular insulin (Humulin R)

Can be given SQ or IV
Insulin Preparations: Short Acting

Onset of Action?
0.5-1 hour
Insulin Preparations: Short Acting

Peak Action?
2-4 hours
Insulin Preparations: Short Acting

Duration of Action?
5-7 hours
Insulin Preparations: Intermediate Acting

Agent (1)?
NPH
Insulin Preparations: Intermediate Acting

Onset of Action?
2-4 hours
Insulin Preparations: Intermediate Acting

Peak Action?
4-12 hours
Insulin Preparations: Intermediate Acting

Duration of Action?
12-18 hours
Insulin Preparations: Long Acting

Agents (2)?
Insulin glargine (Lantus)
Insulin detemir (Levemir)

Less peaks & valleys
Insulin Preparations: Long Acting (glargine)

Onset of Action?
1.5 hours
Insulin Preparations: Long Acting (glargine)

Peak Action?
No pronounced peak
Insulin Preparations: Long Acting (glargine)

Duration of Action?
20-24 hours
Insulin Preparations: Long Acting (detemir)

Onset of Action?
0.8-2 hours
Insulin Preparations: Long Acting (detemir)

Peak Action?
Relatively flat
Insulin Preparations: Long Acting (detemir)

Duration of Action?
5.7-23.2 hours
Insulin Preparations

NPH/regular (70/30)
Humulin 70/30
Novolin 70/30
Insulin Preparations

Insulin aspart protamine suspension / insulin aspart (70/30)
NovoLog Mix 70/30
Insulin Preparations

Insulin lispro protamine suspension / insulin lispro (70/25)
Humalog Mix 75/25
Insulin Preparations

Insulin lispro protamine suspension / insulin lispro (50/50)
Humalog Mix 50/50
Endocrine Physiology Review

What is the role of the hypothalamus in the endocrine system?
Hypothalamus secretes releasing hormones to the pituitary gland. These trigger the pituitary to know what hormones are to be released.

Hypothalamus secretes thyrotropin-releasing hormone (TRH) --> pituitary --> secretes TSH --> thyroid hormones
Endocrine Physiology Review

What are the two parts of the pituitary gland?
Anterior (adenohypophysis)
Posterior (neurohypophysis)
Endocrine Physiology Review

What is the adenohypophysis?
The anterior pituitary lobe that consists of glandular tissue & secretes ACTH, TSH, growth hormone, prolactin, FSH & LH
Endocrine Physiology Review

What is the neurohypophysis?
The posterior pituitary lobe that contains nervous tissue rather than glandular. Neurons in the posterior pituitary store ADH & oxytocin (released in response from nerve stimulation in the hypothalamus).
Target tissues for drug therapy for diabetes?
What is the ADA recommendations for glycemic control for most nonpregnant adults with diabetes?
A1C: 7% (5.5-7%/6)
Before meals: 70-130
After meals: < 180