Pharm II - Test 3 Flashcards
Class: Levothyroxine (Synthroid)
Thyroid hormone replacement (synthetic T4)
Indication: Levothyroxine (Synthroid)
Hypothyroidism, TSH suppression in select cases of thyroid nodules and thyroid cancer
Side effects: Levothyroxine (Synthroid) and Thyroid USP (Armour) and Liothyronine (Cytomel)
Palpitations, tachycardia, intolerance to heat, anxiety
Long-term elevation of serum T4 may accelerate cardiac disease and osteoporosis
What is an important contraindication for patients with Addison’s disease and hypothyroidism take Synthroid or Armour thyroid?
Replacing thyroid hormone before replacing cortisol can be fatal.
Equivalent dosing: Armour vs. Synthroid vs. Cytomel
60 mg (1 grain) Armour = 100 mcg of T4 (Levothyroixine/Synthroid) = 25 mcg of T3 (Triiodothyronine/Cytomel)
Indication: Thyroid USP (Armour)
Hypothyroidism
MOA: Thyroid USP (Armour)
Replaces both T4 and T3
Thyroid USP (Armour) is standardized to ___
iodine content (0.2% iodine)
With what population should you use more cautious dosing of thyroid replacement?
Patients over 65 with a history of cardiac disease
Class: Liothyronine (Cytomel)
Thyroid hormone replacement (synthetic T3) dosed in mcg
Indication: Liothyronine (Cytomel)
Hypothyroidism with intolerance to T4 replacement therapy or no improvement on T4 replacement therapy
Myxedema coma
“Wilson’s syndrome”
Condition caused by excess administration of thyroid hormone
Thyroiditis factitia
Thyroid conditions can place patients at greater risk for ___(2).
Osteoporosis
Cardiac disease
What type of drugs are often used to block the signs and symptoms of hyperthyroidism?
Beta blockers
Class: Methimazole (Tapazole)
Thionamide
Indication: Methimazole (Tapazole)
Hyperthyroidism
MOA: Methimazole (Tapazole)
Inhibits transformation of inorganic iodine to organic iodine -> blocks production of thyroxine
Inhibits coupling of iodotyrosine to form T3/T4
Minimal effect blocking peripheral conversion of T4 to T3
Contraindications: Methimazole (Tapazole), Propylthiouracil (PTU)
Pregnancy - Propylthiouracil (PTU) is considered safer (category D)
Class: Propylthiouracil (PTU)
Thionamide
Indication: Propylthiouracil (PTU)
Hyperthyroidism
MOA: Propylthiouracil (PTU)
Inhibits transformation of inorganic iodine to organic iodine -> blocks production of thyroxine
Inhibits coupling of iodotyrosine to form T3/T4
Blocks peripheral conversion of T4 to T3
MOA: Methimazole (Tapazole) vs Propylthiouracil (PTU)
Propylthiouracil (PTU) has a greater effect on blocking peripheral conversion of T4 to T3
Indication: Iodine (SSKI)
Hyperthyroidism, thyroid storm
MOA: Iodine (SSKI)
Large doses of iodine inhibit release of thyroxine from thyroid gland
Beneficial effects of Iodine (SSKI) generally last no more than ___.
2-3 weeks
Indication: Radioactive iodine (131I)
Hyperthyroidism, Selected cases of thyroid cancer, thyroid nodules
Side effects: Radioactive iodine (131I)
Tenderness, swelling during initial week, N/V
transient BM depression and acute leukemia w/ extremely high doses
M - dec sperm, temp. infertility (~2 years)
Preparation for treatment with Radioactive iodine (131I)
Euthyroid state achieved by anti-thyroid drugs or SSKI
Contraindications: Radioactive iodine (131I)
Category X (delay 6-12 mos after tx)
SSx: Thyroid storm
High fever, irritability, delirium, V/D, dehydration, hypotension, vascular collapse
Coma, death
Which population is at risk for thyroid storm unless anti-thyroid medication has been administered?
Patients undergoing surgery for hyperthyroidism
Tx: Thyroid storm
Beta blockade + IV Iodine
Dx: DM
Confirmed fasting blood glucose level of >/= 126 mg/dl
Non-fasting blood glucose of >/= 200 mg/dl in pt presenting w/ sxs or exam findings consistent with DM
Concordance for development in identical twins: Type I vs II diabetes
Type I: 50%
Type II: 90-100%
What antibody testing should be considered in all non-obese adults who present with sxs of type II diabetes (type 1.5)?
Islet cell, insulin, and glutamic acid decarboxylase antibodies
MOA: Metformin vs. Sulfonylureas/Meglitinides vs. Alpha-glucosidase inhibitors vs. Thiazolidinediones (Glitazones) vs. DPP-4 inhibitors
Metformin = inhibits hepatogluconeogenesis, dec insulin resistance
Sulfonylureas/Meglitinides = inc secretion of insulin (secretagogues)
Alpha-glucosidase inhibitors = delay absorption of glucose by intestines
Thiazolidinediones (Glitazones) = dec insulin resistance (via PPAR-gamma)
DPP-4 inhibitors = promote release of insulin from pancreas after eating a meal (via GLP-1)
Class: Metformin (Glucophage)
Biguanides
MOA: Metformin (Glucophage)
Dec hepatic glucose production, inc insulin sensitivity in skeletal muscle
Pregnancy and Metformin (Glucophage)
Category B
Side effects: Metformin (Glucophage)
Abdominal cramping, N, metallic taste, inc risk for B12 deficiency
Lactic acidosis (rare)
Contraindications: Metformin (Glucophage)
Do not use in pts w/ impaired renal fxn (serum creatinine >1.5 mg/dl in M or >1.4 in F)
MOA: Sulfonylureas
Interaction w/ ATP-sensitive K channel in the beta cell membrane -> inc. insulin production from intact beta cells (secretagogues)
What is the MC side effect of sulfonylureas?
Weight gain
In general, sulfonylureas become ineffective within ___.
5-10 years
Contraindications: Sulfonylureas
Patients w/ sulfa allergy
2nd-generation sulfonylureas (3)
Glipizide (Glucotrol)
Glyburide (Micronase, Diabeta)
Glimepiride (Amaryl)
MOA: Meglitinides
Interaction w/ ATP-sensitive K channel in the beta cell membrane -> Inc. insulin release from beta cells (secretagogues)
Meglitinides (2)
Nateglinide (Starlix)
Repaglinide (Prandin)
Which meglitinide has been shown to be equally effective to the sulfonylureas?
Repaglinide (Prandin)
Side effects: Sulfonylureas, Meglitinides
Hypoglycemia, weight gain
Contraindication: Meglitinides
Do not combine with sulfonylurea drugs due to increased risk for hypoglycemia
MOA: Thiazolidinediones / Glitazone
Affect gene expression of PPAR gamma -> dec. peripheral insulin resistance, dec. hepatic glucose production
What is the only glitazone approved for concurrent use with insulin?
Pioglitazone (ACTOS)
TZDs/Glitazones (2)
Rosiglitazone (Avandia)
Pioglitazone (ACTOS)
Side effects: TZDs/Glitazones
Increased risk of CHF, MI(?), bone fractures, weight gain, ALT elevation
Alpha-glucosidase inhibitors (2)
Acarbose (Precose)
Miglitol (Glyset)
MOA: Alpha-glucosidase inhibitors
Inhibit alpha-glucosidase -> delays absorption of glucose and other monosaccharides
Alpha-glucosidase inhibitors can increase the risk for hypoglycemia when combined with ___.
Sulfonylureas
Contraindications: Alpha-glucosidase inhibitors
Pts w/ chronic intestinal dz, IBD, colonic ulceration, intestinal obstruction
Pregnancy: Alpha-glucosidase inhibitors
Category B
MOA: Sitagliptin (Januvia)
Dipeptidyl peptidase 4 (DPP-4) inhibitor -> prevent breakdown of GLP-1 and GIP -> potentiate secretion of insulin, suppress glucagon release -> normalize blood glucose
Side effects: Sitagliptin (Januvia)
Hypoglycemia
Inc. risk of acute/chronic pancreatitis
Indication: Pramlintide (Symlin)
Type 1 or 2 diabetes pts who are not achieving their A1c goal levels
First drug for type I since 1920s
Contraindication: Pramlintide (Symlin)
Cannot be combined with insulin
Side effect: Pramlintide (Symlin)
NAUSEA, modest weight loss
No hypoglycemia or weight gain
Rapid-acting insulin
Lispro (Aspart)
Humulog (Novalog)
Short-acting insulin
Regular Insulin (Humulin R)
Intermediate-acting insulin
NPH (Humulin N)
Long-acting insulin
Glargine (Lantus)
Insulin type for sleeping hours
Glargine (Lantus)
Insulin type before meals
Lispro (Aspart)
Side effects: Insulin
Weight gain, hypoglycemia (seizures, coma, death), hypokalemia, fibrotic/atrophic injection sites