2011.08.07_Endocrine_Drugs.csv

D2 agonist - binds & stimulates D2 receptors on lactotrophs. Decreases prolactin synthesis & DNA synthesis & tumor growth. Usually 1st-line medication (cabergoline has more side effects but is less effective)

High affinity for D2 receptors. Used for patients with hyperprolactinemia. May be useful in patients who do not respond to bromocriptine. Risk of aortic valve fibrosis in those taking very high doses (not normally doses used for treatment of prolactinoma). May cause nausea; orthostatic hypotension; dyskinesia

Also called Synthroid. Drug of choice for treatment of hypothyroidism. Must be monitored via TSH levels. Same as T4. Those with cardiac disease must be started on very low doses. Pregnant patients will require higher doses

Brand name = sandostatin. Mimics natural somatostatin to inhibit growth hormone. Selective SST2R agonist. May cause GI distress & gallstones. Old formula needed to be administered subcutaneously 3x daily; new formula is administered intramuscularly once every 4 weeks

Occasionally used to treat hypothyroidism. Same as T3. Used in severe acute hypothyroidism

Mixture of T4/T3. Mimics natural ratio of T4/T3. No major advantage over levothyroxine

Thyroid hormone replacements isolated from animals. Many disadvantages. Infrequently used

Includes propylthiouracil and methimazole. Drugs of choice for treatment of hyperthyroidism. Inhibit iodination of thyroglobulin by inactivating thyroid peroxidase. Propylthiouracil also blocks peripheral conversion of T4 to T3. Side effects = itchy rash & slight fever

Contains iodide - shuts down thyroxine production at high levels. Inhibits iodination of thyroglobulin and T3/T4 synthesis/release. Used only in combination with thioureylines and in specific situations - pre-op for thyroidectomy & in thyroid storm. Side effects = salivation; sore teeth/gums; hemorrhage; induction of goiter/myxedema

Used to destroy thyroid tissue - emits beta rays

Hyperthyroidism can imitate sympathetic nervous system activation; beta-blockers can block sympathetic effects. Used in life-threatening thyroid storms (exacerbation of thyrotoxicosis) to prevent or reverse severe effects - tachycardia; fibrillation; shock; heart failure. Used in combination with thioureylines/Lugol's solution

Recombinant human growth hormone; used to treat GH deficiency. May lead to development of anti-GH autoantibodies

Broad-acting ADH analogue; acts on V1 and V2 receptors. Few uses due to broad effects; used for temporary control of GI bleeding. Side effects include skin blanching; abdominal cramps; hypertension

ADH analogue; acts selectively on V2 receptors. Used in diabetes insipidus and mild hemophilia. Side effects include water retention; listlessness; seizures; coma

Competitive aldosterone antagonist blocks the actions of aldosterone at its receptor. May cause hypogonadism due to blockage of testosterone biosynthesis

Aldosterone antagonist blocks the actions of aldosterone at its receptor

Potassium-sparing diuretic that works by blocking ENaC

Cortisol replacement

Mineralocorticoid replacement

Blocks androgen receptor

Antifungal; may cause hypogonadism due to blockage of androgen receptor

GnRH agonist

Estrogen antagonist (NOT a SERM - antagonist in all tissues)

Decreases hepatic glucose production through LKB1 - protein kinase that upregulates AMPK. Only member of biguanide family. Increases insulin-mediated muscle glucose uptake & decreases GI glucose absorption & inhibits adipose tissue lipolysis as well. Promotes some slight weight loss & improves microvascular outcomes. May be used in pre-diabetics to prevent progression. Contraindications = renal insufficiency or severe CHF or chronic liver disease. No risk of hypoglycemia but does carry risk of lactic acidosis

Rh negative mothers - help prevent abortion with threatened spontaneous abortion

Aromatase inhibitor

Nasal spray - GnRH agonist

Very long-acting insulin

Very long-acting insulin

2nd-generation sulfonylurea

Very short-acting insulin

Medium-acting insulin

Enhance insulin sensitivity in muscle & liver & adipose tissue - agonist for nuclear receptor PPAR-gamma (in adipocytes & liver -PPR-gamma regulation of genes involved in adipocyte differentiation & fatty acid uptake. PPAR-gamma acts via transactivation & transrepression). Include rosiglitazone & pioglitazone (Avandia & Actos) - rosiglitazone = severely restricted & not generally used. Side effects = weight gain & edema. Contraindicated in those with CHF. LFTs are necessary during treatment. May be associated w/osteoporosis. Delayed onset (3-6 weeks). Decreases inflammation

Bind to potassium channels on beta-cells - causes membrane depolarization -> calcium influx -> release of stored insulin. Effective but have high yearly failure rate & may cause weight gain & hypoglycemia. Examples include glipizide & glyburide

3rd-generation sulfonylurea

Different structure from sulfonylureas but work in much the same way - bind to potassium receptor (distinct site from sulfonylurea) -> calcium influx -> release of stored insulin. Have more rapid action & shorter duration than sulfonyureas. Produce comperable reductions in HbA1c vs. sufonylureas but do not produce weight gain & cause lower rates of hypoglycemia. Drawback: more expensive than sulfonylureas

Metformin - decreases hepatic glucose production. Increases insulin-mediated muscle glucose uptake & decreases GI glucose absorption & inhibits adipose tissue lipolysis as well. Mainly acts through LKB1 - protein kinase that upregulates AMPK. Promotes some slight weight loss & improves microvascular outcomes. May be used in pre-diabetics to prevent progression. Contraindications = renal insufficiency or severe CHF or chronic liver disease

Inhibits hydrolase enzyme on the brush border of the intestines - delays postprandial carbohydrate absorption. Side effects = bloating & flatulence & diarrhea -> poor compliance. Poor efficacy but does not cause weight gain or hypoglycemia

GLP-1 analogues (injection) & DPP4 blockers (oral)

Potassium channel inhibitor - increases permeability of the K-ATP channel -> closing of calcium channel -> prevention of insulin release. Used for treatment of hypoglycemia due to hyperinsulinism & for malignant HTM (relaxes smooth muscle)

Lispro & Aspart & Glulisine (very short; onset 15-30 mins) & regular insulin (short; onset 0.5-1 hr)

NPH (onset 1-4 hr)

Detemir & Glargine (last 14-22 hrs)

"Stands for ""selective estrogen receptor modulator."" Used for the treatment of infertility in anovulatory women. Includes tamoxifen & raloxifene & toremifene"

Amylin analogue. Slows gastric emptying -> aids in absorption of glucose. Also promotes satiety (similar to GLP-1 agonists) & inhibits glucagon