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Pharmacology 2 > 2 - Endocrine Pharmacology > Flashcards

2 - Endocrine Pharmacology Flashcards

1
Q

What does a lack in iodine in the diet lead to?

A

Excessive secretion of TSH, resulting in thyroid hypertrophy which leads to a goiter

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2
Q

What is considered primary vs secondary hypo/hyperthyroidism?

A
  • Primary - disease of thyroid gland
  • Secondary - disease of pituitary or hypothalamus gland
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3
Q

What are the 2 synthetic thyroid preparations made by industry?

A
  1. Sodium levothroxine (T4 = Synthroid, Levoxyl)
  2. Sodium liothyronine (T3 = Cytomel) - oral absorption
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4
Q

What is the preferred drug for most cases of hypothyroidism?

A

Sodium levothyroxine (T4 = Synthroid, Levoxyl)

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5
Q

What is the use for sodium levothyroxine (T4 = Synthroid)? And how does it work?

A
  1. Replacement or supplement therapy in hypothyroidism
  2. Increases basal metabolic rate
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6
Q

What are the important adverse effects of sodium levothyroxine (T4 = Synthroid)?

A
  • Indicates overdose = hyperthyroidism
  • Palpitations, tachycardia
  • Nervousness, sweating
  • Increased appetite
  • Weight loss
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7
Q

What is propylthiouracil?

A

“PTU” - a palliative treatment of hyperthyroidism in preparation for surgery or radioactive iodine therapy, management of thyrotoxic crisis

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8
Q

What drug blocks iodination reaction (blocks oxidation of iodine) in thyroid gland, and blocks synthesis of T4 and T3?

A

PTU - propylthiouracil

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9
Q

What are the side effects of PTU?

A
  • Skin rash
  • Nausea
  • Agranulocytosis
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10
Q

What does methimazole (Tapazole) do?

A
  • Palliative treatment of hyperthyroidism, returns patient to a normal metabolic state prior to thyroidectomy, control thyrotoxic crisis that may accompany thyroidectomy
  • It blocks iodination reaction in thryoid gland, blocks iodine’s ability to combine with tyrosine to form T3 and T4
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11
Q

Why is methimazole (Tapazole) an undesirable drug?

A
  • Expensive
  • Inconvenient
  • Adverse effects (fever, rash, hematologic disorders)
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12
Q

What is the process of taking Radioactive Iodine I 131?

A
  • Patient swallows iodine “tagged” with radioactive nucleotide
  • Drug binds to iodine receptors and slowly irradiates and destroys thyroid gland (< 3 months)
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13
Q

What are some dental considerations of patients with hypothyroidism?

A
  • Easier from management perspective (than hyper)
  • Cold, tired/fatigued
  • More sensitive to CNS depressents, need to lower dose = sedatives, opiods
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14
Q

What is absolutly contraindicated in patients with active disease of hyperthyroidism?

A

Epinephrine

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15
Q

What are the dental considerations of patients with hyperthyroidism?

A
  • Nervous, increased BP
  • Palpitations and tachycardia
  • May percieve more pain
  • Less sensitive to CNS depressants, may require higher dose of pain meds and sedatives
    • May be mis-labeled as having “drug-seeking” behaviors
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16
Q

What disease results from autoimmune destruction of pancreatic beta cells? And what is the only effective drug in treating this disease?

A
  1. Type 1 Diabetes
  2. Insulin
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17
Q

How was insulin previously prepared and how is it available today?

A
  • Previously - bovine (cows) and porcine (pigs)
  • Now - human-type insulin (recombinant technology)
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18
Q

How is insulin classified?

A

3 ways:

  1. Onset
  2. Peak
  3. Duration of action
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19
Q

Name the short-acting insulin preparations.

A

insulin Regular (Humulin R)

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20
Q

Name the rapid-acting insulin preparations.

A
  • insulin Aspart (NovoLOG)
  • insulin Glulisine (Apidra, Apidra Solostar)
  • insulin Lispro (HumaLOG)
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21
Q

Name the intermediate acting insulin preparations.

A
  • insulin NPH (HumuLIN, NovoLIN N)
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22
Q

Name the intermediate to long-acting insulin preparations.

A
  • insulin Detemir (Levemir)
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23
Q

Name the long-acting insulin preparations.

A
  • insulin Glargine (Lantus, Lantus Solostar)
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24
Q

What is the big risk for oral drug therapy for management of Type 2 Diabetes?

A

Hypoglycemia

25
Q

What are the primary drug classes for oral drugs used in treatment of type 2 diabetes?

A

“BATSI”

  • Biguanides (metformin)
  • Alpha-glucosidase inhibitors
  • Thiazolidinediones (TZDs)
  • Sulfonylureas (“traditional” oral hypoglycemics)
  • Incretins - GLP-1 agonists, DDP-4 inhibitors
26
Q

What type of primary oral drugs for type 2 diabetes are newer (2nd generation) that are more potent but not more effective?

A

Sulfonylureas

27
Q

What are the 1st generation sulfonylureas?

A

All end in “amide”

  • tolbutamide (Orinase) ** oldest in class
  • tolazamide (Tolinase)
  • acetoheamide (Dymelor)
  • chlorpropramide (Diabinese)
28
Q

What are the 2nd generation sulfonylureas?

A

all end in “ide”

  • glypizide (Glucotrol) **
  • glyburide (Diabeta, Glynase, PresTab, Micronase)

10 to 100 times more potent than 1st generation

29
Q

What is the major distinction between 1st gen and 2nd gen sulfonylureas?

A

Potency - 2nd is way more potent that 1st

30
Q

What are the warnings with sulfonylureas?

A
  • Increased cardiac mortality
  • Sulfonamide allergy - contraindicated
  • Caution with use if severe hepatic disease
31
Q

What is a serious drug interaction with sulfonylureas?

A

Aspirin - it may enhance the hypoglycemic response to the sulfonylurea

= Hypoglycemia

32
Q

What are the 2 mechanisms taking aspirin with sulfonylureas can cause hypoglycemia?

A
  • Aspirin displaces the sulfonylurea from plasma proteins causing increased blood levels of sulfonylurea
  • Salicylate inhibition PGE increases the insulin response and enhances the response to sulfonylureas
33
Q

What is the most popular drug for Type 2 Diabetes? And what class of drug is it?

A
  • metformin (Glucophage)
  • Biguanide
34
Q

What are the characteristics of metformin (Glucophage)?

A
  • Inhibits absorption of glucose from the gut
  • Decreases hepatic glucose production
  • Increases insulin sensitivity at receptor sites
  • Increases peripheral glucose uptake and utilization
35
Q

What are the benefits of metformin?

A
  • More effective for reducing glycemic level
  • No weight gain
  • Reduces all-cause and cardiovascular mortality
  • **Reduces rates of cancer **in patients with type 2 diabetes
36
Q

What are the risks of taking metformin?

A
  • Lactic acidosis if renal impairment
  • Avoid alcohol - hepatic impairment, acute CHF
  • Gastrointestinal side effects
37
Q

What type of drugs inhibit an enzyme responsible for degrading complex carbs in the gut? And what are the preparations of this drug?

A
  • Alpha-glucosidase inhibitors
  • acarbose (Precose)
  • miglitol (Glyset)

** There is a delay in blood glucose concentrations after a meal when taking these drugs **

38
Q

How do thiazolidinediones work?

A
  • Lower blood glucose by improving target cell response to insulin without increasing pancreatic insulin secretion
  • Reduces insulin resistance
  • Activity depends on the presence of insulin for activity
39
Q

What are the common preparations of thiazolidinediones?

A

end with “zone”

  • pioglitazone (Actos)
  • rosiglitazone (Avandia)
40
Q

What is rosigltiazone (Avanida) associated with (side effects)?

A
  • >30 deaths due to liver failure**
  • Increased risk of heart failure
    • ​Contraindicated in pts with serious heart failure
41
Q

What are the 2 types of incretin mimetics “Incretins”?

A
  • GLP-1 receptor agonist (glucagonlike peptide -1)
  • DPP-4 inhibitors - these drugs end in “liptin”
42
Q

What is the “new” concern for the Incretins?

A
  • That these drugs cause inflammation and possible pre-cancerous changes of pancreas
43
Q

What is the nomal and fasting blood sugar ranges?

A
  • Normal - 70-120 mg/dL
  • Fasting - 70-110 mg/dL
44
Q

What is the gold standard for measuring diabetes?

A

Glycataed Hemoglobin (HbA1c)

  • Measures glycemic control for 6-12 weeks
  • Normal <6%
  • Diabetes diagnosis >6.5%
  • Diabetics goal: <7%
45
Q

What are the American College of Physicians clinical practice guidelines for diabetes?

A
  1. Add drug therapy when lifestyle changes fail to improve hyperglycemia
  2. Initial monotherapy with metformin (drug of choice)
  3. Add 2nd drug if hyperglycemia persists
46
Q

What is a steroid produced and secreted by the ovary?

A

estradiol - natural estrogen

47
Q

What is used for Estrogen Replacement Therapy (ERT)?

A

ethinyl estradiol - orally active

48
Q

Up to the 1990’s only 2 benefits of hormone replacement therapy have been clinically proven, what are they?

A
  1. Hormones relieve menopausal symptoms
  2. Hormones stave off bone loss
49
Q

What are the different Estrogen Replacement drugs (HRT)?

A
  • _Conjugated equine estrogens _
    • Premarin
  • _Esterified estrogens _
    • Estratab, Menest
  • Estradiol preps
    • Estraderm, transdermal patch, Estraderm cream, Climara transdermal patch, Estrace cream
50
Q

What conjugated equine estrogens are effective in treatment of vasomotor symptoms of menopause?

A

Premarin

51
Q

What are some common side effects of Conjugated equine estrogens (Premarin)?

A
  • Peripheral edema
  • Breast tenderness
  • Bloating
  • Headache
52
Q

What is one serious side effect noted in women with an intact uterus that take conjugated equine estrogens (Premarin)?

A
  • Increased risk for endometrial (uterine) cancer

Taking estrogen (such as Premarin) after menopause may also increase risk for breast cancer

53
Q

What drug has the same effects as Premarin at half the dose?

A

Esterified estrogens (Estratab, Menest)

54
Q

What are combination drugs used for?

A
  • Estrogen with progesterone (Prempro)
  • Adding progesterone to the preparation reduces risk for endometrial cancer
55
Q

In the HERS study, women taking estrogen for 4 years noticed what?

A
  • Cholesterol levels went down
  • Increases in blood clots
  • No reduction in heart disease
56
Q

What is the HRT current thinking?

A
  • Estrogen in combination with progestin may increase risk of stroke
  • This outweighs long term use to prevent osteoporosis
57
Q

What are the risks of Prempro?

A

Increased risks of:

  • Heart disease
  • Stroke
  • Pulmonary embolism
  • Invasive breast cancer
58
Q

What is hormone replacement therapy used for today?

A
  • Short term use only = less than 5 years
  • Treat symptoms of menopause

Pharmacology 2 (21 decks)

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