endocrine drugs
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| Inhibitor of Na+-I- cotransporter | PERCHLORATE
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| mechanism and main toxicity of perchlorate | Block uptake of iodide (I-), Aplastic Anemia
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| Iodide mechanism | Inhibit organification, Inhibit release of T3 and T4 (via inhibition of proteases), decrease size and vascularity of gland
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| Radioactive Iodine (131I) mechanism | Rapid uptake of Iodine, Emission of radioactive β-particle
Selective destruction of thyroid tissue
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| how toxic is radio active Iodine | little to no toxicity
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| PROPYLTHIOURACIL (PTU) mechanism | Block Organification, inhibit thyroid peroxidase
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| PROPYLTHIOURACIL is a | Thioamide
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| Levothyroxine is | t4 analogue
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| Ketoconazole is | an antifungal
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| ketoconazole mechanism | a non-selective inhibitor of steroid hormone biosynthesis.
It inhibits various enzymes in the biosynthetic pathway of cortisol
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| Ketoconazole interacts with | statins ex: simvastatin
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| Mifepristone | GC receptor antagonist
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| Mitotane | chemically non-selective adrenalectomic agent
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| OXYTOCIN actions | Induces contraction of smooth muscle in reproductive tracts, initiating labor, stimulates lactation
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| DESMOPRESSIN ACETATE is | a long synthetic vasopressin anologue, it has minimal vasoconstrictor effects. The Antidiuretic : Pressor ratio is 4000x higher than native ADH
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| CONIVAPTAN is | ADH ANTAGONISTS: Used in patients with hyponatremia or acute HF. It has a high affinity for V1A and V2 rec
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| Chloropromide and Glyburide desctiption and MOA | its a Sulfonylurea, which inhibits the atpase sensitive k channel
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| Chloropromide and Glyburide effect | INCREASE insulin release from pancreas
DECREASE Glucagon levels (mechanism unclear)
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| Chloropromide and Glyburide TOXICITY/SIDE EFFECTS | Hypoglycemia (Most common side effect)
Weight Gain
Potentially Teratogenic
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| PRAMLINITIDE is | Amylin Analog, a synthetic human amylin
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| MOA and effects | Binds to the Amylin Receptor in specific regions of the brain.
Activation of the amylin receptor cause reductions in glucagon release
Promotes satiety, slows gastric emptying
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| PRAMLINITIDE Drug-Drug Interaction | Contraindicated in patients with disorders of motility or on drugs that decrease gastric motility (i.e. OPIODE ANALGESICS)
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| REPAGLINIDE is | Meglitinides
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| REPAGLINIDE MOA | STIMULATE insulin release from pancreas
Similar mechanism to sulfonylureas
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| NATEGLINIDE is | d-phenylalanine derivative
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| NATEGLINIDE MOA | STIMULATE insulin release from pancreas
Similar mechanism to sulfonylureas
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| NATEGLINIDE and REPAGLINIDE adverse effects | Hypoglycemia, diarrhea, nausea and weight gain
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| Metformin is a | Biguanide that activates ampk
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| METFORMIN effects | Liver: Decreases gluconeogenesis
Skeletal muscle: Increase glucose utilization
(lowers glucose levels)
DOES NOT DEPEND ON FUNCTIONING PANCREATIC BETA CELLS
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| Metformin adverse effects and metabolism | IMPAIRS HEPATIC LACTIC ACID METABOLISM
Lactic acidosis
Muscle pain
Metabolism:
Not metabolized
Excreted unchanged in the urine
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| PIOGLITAZONE | Insulin Sensitizer: Thiazolidinediones (TZD’s)
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| PIOGLITAZONE MOA | acts on PPAR GAMMA
INCREASE INSULIN SENSITIVITY
DECREASE INSULIN RESISTANCE
INCREASE GLUCOSE UTILIZATION
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| PIOGLITAZONE adverse effects | ASSOCIATED WITH BLADDER CANCER
FLUID RETENTION
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| ACARBOSE | ALPHA-GLUCISIDASE INHIBITOR
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| ACARBOSE MOA | Inhibit α-glucosidase in GI tract
Decrease absorption of Glucose
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| Acarbose | GI disturbance
Excess carbohydrates in GI tract lead to increased bacterial digestion of polysaccharides.
Contraindicated in people with Inflammatory Bowel Disease
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| EXENATIDE | GLUCAGON-LIKE PEPTIDE-1 (GLP-1) RECEPTOR AGONISTS
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| EXENATIDE effects | promotes: STIMULATES INSULIN PRODUCTION
REDUCES APPETITE
INDUCES β-CELL GROWTH
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| EXENATIDE adverse effects | GI disturbance
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| SITAGLIPTIN | DIPEPTIDYL PEPTIDASE-4 (DPP-4) INHIBITOR
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| sitagliptin effects | INCREASE CIRCULATING GLP-1
INCREASE INSULIN LEVCELS
DECREASE GLUCAGON LEVELS
Adverse effects:
GI disturbance
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| CANAGLIFLOZIN | Sodium-Glucose transporter inhibitor (SGLT-2 inhibitor)
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| Canagliflozin MOA | Inhibits the reabsorbtion of glucose
Results in loss of glucose (glycosuria) and water (osmotic diuresis)
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| Canagliflozin Adverse effects | Increased urination
Increased urinary tract infections
Possible hypotension
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| SIMVASTATIN is | a prodrug, absorbed in the small intestine, and activated in the liver
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| DRUGS THAT INTERFERE WITH STATIN OXIDATION | Macrolide antibiotics: e.g. Erythromycin
Azole antifungals: e.g. Itraconazole
Cyclosporine (immunosuppressant)
Nefazodone (a phenylpiperazine antidepressant)
HIV protease inhibitors
Amiodarone (Antiarrhythmic agent)
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| Adverse effects of statins (simvastatin) | MYOPATHY
The major adverse effect associated with statin use
Statin-induced rhabdomyolysis
Risk increased in proportion to dose and plasma concentrations
Associated with factors inhibiting statin catabolism
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| CHOLESTYRAMINE | Bile-Acid Sequestrant
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| CHOLESTYRAMINE MOA | Positively charged compounds
IONIC BOND with negatively charged bile acids
Block reabsorbtion and enhance excretion of cholesterol
ENHANCES bile acid synthesis
reduces hepatic cholesterol → INC LDL-R synthesis
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| CHOLESTYRAMINE adverse | Relatively safe
Interfere with absorption of other drugs
FUROSEMIDE, THIAZIDE DIURETICS,PROPRANOLOL, DIGOXIN, WARFARIN
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| niacin MOA | Inhibits hormone-sensitive lipase
DECREASES hepatic TG synthesis
Decreases VLDL production and release
Decreases HDL breakdown
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| Niacin ADVERSE EFFECTS | Cutaneous vasodilation (flush)
A prostaglandin dependent phenomena
Treated with NSAIDs, salicylate-containing creams (i.e. Aspercreme™) and aspirin
Dyspepsia
May increase insulin resistance
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| CLOFIBRATE MOA | Act as PPARα ligands
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| Clofibrate effects | Increased FFA OXIDATION
Increased expression and release of ApoA1
INC expression of LPL
↓ HEPATIC VLDL SECRETION, ↓ TGs, modest ↓ LDL, ↑ HDL
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| Clofibrate adverse effects | Displace oral anticoagulants from protein binding sites.
Myopathy when combined w/ statins (gemfibrozil only)
Gemfibrozil blocks OATP1B1 transporter
Associated w/ gallstone formation
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| EZETIMIBE MOA | Inhibits luminal cholesterol uptake in the SMALL INTESTINE
Decreases cholesterol uptake into chylomicrons
Reduces cholesterol in liver
Increases LDL-Receptor expression
Inc plasma LDL clearance
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| Ezetimibe interactions | BILE ACID SEQUESTRANTS INHIBIT ABSORBTION (ex: cholestyramine)
CONTRAINDICATED
No other interaction reported
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| ALIROCUMAB is | a pcsk9 inhibitor. ( PCSK9 inhibitors have been shown to reduce LDL levels by up to 60 percent from baseline levels, (including in statin-intolerant)
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| ALIROCUMAB MOA | Binds and inactivates PCSK9
Inhibits degradation of LDL-R
Increases LDL-R number
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| ALIROCUMAB adverse effect | Itching and swelling at site of injection
Flu-like symptoms
Hypersensitivity-type reactions
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| Somatotropin | is Identical to human GH
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| Mecasermin | recombinant human IGF-I (rh IGF-I)
- Used for treatment of GH-resistant IGF-I deficiency
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| Octreotide | Somatostatin analog
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| Pegvisomant | GH receptor anatgonist, Binds only to one GH receptor, will stop dimerization
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