Exam 2: Endocrine Pharmacology Flashcards
Name the 3 thyroid diseases
- Lack of iodine in diet
- excessive secretion of TSH, resulting in thyroid hypertrophy (Goiter)
- Primary hypo/hyperthyroidism = disease of thyroid gland
- Secondary hypo/hyperthyroidism = disease of pituitary or hypothalamus gland
What is the precursor to making synthetic thyroid hormones T4 and T3?
L-tyrosine
Which chemical is required for synthesis of thyroid hormones?
Iodine
- without iodine, build-up of TH precursor, resulting in goiter
- americans obtain iodine from iodized salt
2 synthetic thyroid preparations are made by industry:
- Sodium levothyroxine (T4 = Synthroid, Levoxyl)
2. Sodium liothyronine (T3 = Cytomel)
What is the preferred drug for most cases of hypothyroidism?
Sodium levothyroxine (Synthroid, Levoxyl)
Use for Sodium levothyroxine (T4 = Synthroid)
replacement or supplement therapy in hypothyroidism
Mechanism of action for Sodium levothyroxine
- Affects DNA transcription and stimulates protein synthesis
- Promotes gluconeogenesis
- Mobilizes glycogen stores
- **Increases basal metabolic rate
Important adverse effects of Sodium levothyroxine
Overdose…
- Palpitations, tachycardia
- Nervousness, sweating
- Increased appetite
- Weight loss
Name the drugs used to treat Hyperthyroidism
- Propylthiouracil
- Iodides
- methimazole (Tapazole)
- Radioactive Iodide I 131
Use of Propylthiouracil (PTU)
treatment of hyperthyroidism in preparation for surgery or radioactive iodine therapy
Mechanism of Propylthiouracil (PTU)
Blocks iodination reaction in thyroid gland; blocks synthesis of T4 and T3
Side effects of PTU
skin rash
nausea
agranulocytosis
What are Iodides
saturated solution of potassium iodide
Mechanism of action of Iodides
Not clear…
Probably reduces secretion of thyroid hormone
Use of Iodides
Used in conjunction with propylthiouracil to prepare patients for surgery
Use of Methimazole (Tapazole)
Hyperthyroidism
Return patient to a normal metabolic state prior to thyroidectomy
Mechanism of action of methimazole (Tapazole)
Blocks iodination reaction in thyroid gland
Blocks iodine’s ability to combine with tyrosine to form T3 and T4
Which of the hypertensive drugs is considered undesirable
methimazole (Tapazole)
- expensive, inconvenient, adverse effects
Oral side effects of methimazole (Tapazole)
Taste alteration
Salivary gland swelling
How does Radioactive iodide I 131 work?
Patient swallows iodine tagged with radioactive nucleotide = drug binds to iodine receptors and slowly irradiates and destroys thyroid gland (
Dental considerations of patients with hypothyroidism
- Easier from management perspective
- Cold, tired/fatigued
- MORE sensitive to CNS depressants
- lower dose
Dental considerations of patients with hyperthyroidism
- Nervous; may have increased blood pressure
- May be sensitive to epinephrine
- if active disease, ABSOLUTE contraindication to epinephrine
- Palpitations and tachycardia
- May perceive more pain
- Less sensitive to CNS depressants
Type I diabetes results from what?
autoimmune destruction of the pancreatic beta cells.
What is the only effective drug in treating Type 1 diabetes?
Insulin
Structure of Insulin
2 chains connected via disulfide bridges
T or F, Insulin preparations currently used are from animal sources
False, no longer used. Current insulin is available as human-type insulin
How is insulin administered?
All insulins are injected subcutaneously (SC)
Insulin is classified in what 3 ways?
- Onset
- Peak
- Durations of action
Name the short-acting insulin preparations
Insulin Regular (HumuLIN R)
Name the rapid-acting insulin preparations
Insulin Aspart (NovoLOG) Insulin Glulisine (Apidra, Apidra Solostar) Insulin Lispro (HumaLOG)
Name the intermediate acting insulin preparations
Insulin NPH (HumuLIN, NovoLIN N)
Name the intermediate to long-acting insulin preparations
Insulin Detemir (Levemir)
Name the long-acting insulin preparations
Insulin Glargine (Lantus, Lantus Solostar)
Use of Lantus Solostar (insulin glargine)
Treatment of type 1 diabetes and type 2 diabetes to improve glycemic control.
Oral complications of Lantus Solostar
Numbness of mouth
General idea behind drugs that work to fix Type 2 diabetes
Target cells become insensitive to insulin. So, more insulin is needed to elicit response in resistant cells.
Name the goals of oral drug therapy for management of Type 2 Diabetes
- Increase insulin secretion in glucose-dependent manner
- Suppress hepatic gluconeogenesis
- Improve insulin sensitivity
Risk of Oral Drug Therapy for Type 2 diabetes
hypoglycemia
Name the Primary drugs for Type 2 diabetes
- sulfonylureas (traditional oral hypoglycemias)
- Biguanides (Metformin)
- Alpha-glucosidase inhibitors
- Thiazolidinediones (TZDs)
- Incretins - GLP-1 agonists, DD-4 inhibitors
Name the 1st generation Sulfonylureas
- tolbutamide (Orinase)
others not in bold…
Name the 2nd generation Sulfonylureas
- glipizide (Glucotrol)
one more but not in bold
What is the major distinction between 1st and 2nd generations of Sulfonylureas
Potency
-2nd generation are more potent but not more effective
3 warnings with Sulfonylureas
- Increased cardiovascular mortality
- Sulfonamide allergy
- Caution with use if severe hepatic disease
Describe a very serious drug interaction with Sulfonylureas
Aspirin
- simultaneous administration may enhance the hypoglycemic response to the sulfonylurea
What is the result of a drug interaction between aspirin and sulfonylurea?
hypoglycemia
