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19 Cards in this Set

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Sulfonylureas | 2nd Generation

Glyburide ( Diabeta, Micronase, Glynis’s PresTab)


Glipizide (Glucotrol, Glucotrol XL)


Glimepiride (Amaryl)

Sulfonylureas

Glyburide, Glipizide, Glimepiride


MOA- increase secretion of preformed insulin from beta cells of the pancreas by closing K channels


2ndary- increases insulin receptor sensitivity and decreased hepatic glucose output

Sulfonylureas Adverse Effects

Glipizide, Glimepiride, Glyburide



Hypoglycemia -> most common


Dermatologic réactions: rash, photosensitivity, hypersensitivity


GI - NV , abnormal liver function tests


WEIGHT GAIN

Sulfonylureas

Glyburide, Glimepiride, Glipizide


Metabolism and Excretion


Hepatically Metabolized -use with caution and at reduced doses in patients with hepatic impairment


Rénal Excretion - May accumulate in patients with CrCl <30mL/min

Biguanides

Metformin | Glucophage

Biguanides Contraindications

eGFR <30 mL/min


Rénal impairment


Liver - May decrease the ability to eliminate lactic acid


Hypoxic state- acute or chronic alcohol abuse, elderly, CHF

Biguanides

No hypoglycemia


Weight loss


Decrease triglycerides


NVD

Biguanides

No hypoglycemia


Weight loss


Decrease triglycerides


NVD -> metallic taste

TZD

Rosiglitazone & Pioglitazone


Hepatoxicity and Edema


Fracture risk - caution w/ women with pre existing osteoporosis


Bladder CA - caution against active bladder CA and caution in patients with history

TZD

Rosiglitazone & Pioglitazone


Hepatoxicity and Edema


Fracture risk - caution w/ women with pre existing osteoporosis


Bladder CA - caution against active bladder CA and caution in patients with history

TZD

Rosi, Pio


Exacerbate CHF


Exacerbate CHF

GLP-1 Agonists

ELAD (Exenatide, Liraglutide, Albiglutide, Dulaglutide)


Once or twice daily


Not recommended with CrCl <30 mL/min


Should not be used in patients with a personal or family history of medullary thyroid cancer


NV, HA, Pancreatitis

DPP-4 Inhibitors

SSAL (Sitagliptin, Saxagliptin, Alogliptin, Lingagliptin)


Inhibits DPP-4 enzyme that is responsible for the breakdown on incertum hormones GLP-1


Once daily


FDA: sévère joint pain


AE: well tolerated, pancreatitis (rare) , heart dz ?

Sodium Glucose Cotransporter


(SGLT)2 inhibitors

CDE (Canagliflozin, Dapagliflozin, Empaglifozin)


Reduces réabsorption of filtered glucose, increased urinary excretion of glucose, thereby reducing plasma glucose concentrations

SGLT -2 Advantages

Weight loss


Low risk of hypoglycemia


BP lowering


Rénal protection

SGLT-2 inhibitors CONCERNS

Limp amputation


Électrolyte disturbances


Decreased BP


Bacterial urinary tract infections


Fungal genital infections


Malignancy

Thioureas

Propylthiouracil (PTU)


Methimazole (Tapazole)


MOA: inhibits the iodination of tyrosine and the coupling of iodotyrosines


PTU also inhibits the peripheral conversion of T4 to T3


Does not effect the release of preformed T4 and T3

Thioureas

PTU (protein bound)


Methimazole - bound to protein


Both agents have very short half lives, however, they accumulate in the thyroid gland to exert longer effects


Patient becomes euthyroid over a 1-2 month period

Thioureas Adverse Effects

PTU (Propylthiouracil), Methimazole (Tapazole)


Rash, Fluid Retention , decreased WBC , reverses on dc if caught early