Rapid-acting insulin (name 3)
Lispro
Aspart
Glulisine
Rapid-acting insulin (use)
Postprandial glucose control in DM1, 2, GDM
Short-acting insulin (name 1)
regular insulin
Short-acting insulin (3 uses)
- DM1, 2, GDM
- DKA (IV)
- Hyperkalemia (+ glucose)
Intermediate-acting insulin (name 1)
NPH
Long-acting insulin (name 2)
Glargine
Detemir
Long-acting insulin (use)
Basal glucose control in DM1, 2, GDM
Metformin (mechanism)
Biguanides
Alteration of intracellular microsomal enzyme -> decreases hepatic glucose production, increases peripheral insulin sensitivity
Euglycemic and doesn’t cause weight gain
Metformin (use)
1st line in DM2, can use w/out islet fx
Metformin (side effect)
Lactic acidosis -> can’t use in renal&hepatic failure, CHF, alcoholism, sepsis
Tolbutamide (mechanism)
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
Tolbutamide (use)
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
Good in renal dysfx
Tolbutamide (side effects)
1st gen sulfonylureas
Disulfiram-like effects
Chlorpropamide (mechanism)
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
Chlorpropamide (use)
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
Chlorpropamide (side effects)
1st gen sulfonylureas
Disulfiram-like effects, increased risk of hypoglycemia in renal failure, don’t use in CHF
Glyburide (mechanism)
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
Glyburide (use)
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
Glyburide (side effect)
2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure
Glimepiride (mechanism)
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
Glimepiride (use)
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
Glimepiride (side effect)
2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure
Glipizide (mechanism)
Sulfonylureas
Closes K+ channel in beta cells -> depolarization -> increased Ca2+ influx -> insulin release
Short acting
Glipizide (use)
Sulfonylureas
DM2 (useless in DM1 bc requires some islet fx)
Glipizide (side effect)
2nd gen sulfonylureas
Increased risk of hypoglycemia in renal failure
-glitazone (mechanism)
Thiazolidinediones
Binds PPAR-g (INTRACELLULAR RECEPTOR) -> transactivation -> increases insulin sensitivity in peripheral tissue (increasing GLUT-4 transporter expression), also increases level of adiponectin and promotes adipocyte differentiation (PPAR-g regulates FA storage)
Takes days-weeks to take effects
-glitazone (use)
DM2
-glitazone (side effects)
Hepatotoxicity (monitor liver fx), HF, weight gain, edema (fluid retention worse when used w/ insulin)
Don’t use in liver disease, CHF, CAD!
Acarbose (mechanism)
Inhibits brush-border alpha-glucosidase (surface membrane-bound enzyme) -> decreases absorption
Acarbose (use)
DM2
Acarbose (side effect)
GI disturbances -> don’t use in IBS or intestinal blockage
Miglitol (mechanism)
Inhibits brush-border alpha-glucosidase (surface membrane-bound enzyme) -> decreases absorption
Miglitol (use)
DM2
Miglitol (side effect)
GI disturbances
Pramlintide (mechanism)
Amylin analog
Decreases gastric emptying and glucagon
Pramlintide (use)
DM1, 2
Pramlintide (side effects)
Nausea, diarrhea, hypoglycemia
Exenatide, Liraglutide (mechanism)
GLP-1 analog -> acts thru G-protein linked adenylyl cyclase -> increases insulin, decreases glucagon
Exenatide, Liraglutide (use)
DM2
Exenatide, Liraglutide (side effects)
Pancreatitis, n/v
-gliptin (mechanism)
DPP-4 inhibitors -> inhibits metab of GLP-1 -> increases insulin, decreases glucagon
-gliptin (use)
DM2
-gliptin (side effects)
Mild urinary/respiratory infections
Propylthiouracil (mechanism)
Thionamides
Blocks thyroid peroxidase (decreases thyroid synthesis) and 5’-deiodinase (decreases peripheral conversion to T3)
Propylthiouracil (use)
For hyperthyroidism in pregnancy (1st trimester only, see side effects for why -> change to methimazole later in pregnancy)
Propylthiouracil (side effects)
Liver toxicity (why methimazole preferred unless pregnant in first trimester), agranulocytosis, aplastic anemia, skin rash ANCA develops in half the pts taking this med
Methimazole (mechanism)
Thionamides
Blocks thyroid peroxidase (decreases thyroid synthesis). Doesn’t block 5’-deiodinase like propylthiouracil
Methimazole (use)
First line for hyperthyroidism unless pregnant
Methimazole (side effects)
Teratogen and can cause aplasia cutis (only used after 1st trimester), agranulocytosis, aplastic anemia, skin rash
Levothyroxine (mechanism)
T4 analog
Levothyroxine (use)
First line for hypothyroidism
Levothyroxine (side effects)
Signs of hyperthyroidism -> tachycardia, heat intolerance, tremors, arrhythmias
Liothyronine (mechanism)
T3 analog
Liothyronine (use)
Myxedema coma (not routinely used for hypothyroidism, see side effects for why)
Liothyronine (side effects)
Arrhythmogenic and can precipitate HF
Demeclocycline (mechanism)
ADH antagonist
Member of tetracycline family
Demeclocycline (use)
SIADH
Demeclocycline (side effects)
Nephrogenic DI, photosensitivity, abnormality of bone and teeth
Octreotide (mechanism)
Somatostatin analog -> inhibits GH, glucagon, insulin, gastrin, VIP
Octreotide (2 main uses)
eso varices (by reducing splanchnic blood flow by inhibiting hormones responsible for splanchnic vasodilation), conditions characterized by oversecretion of hormones it inhibits (acromegaly, carcinoid, gastrinoma, glucagonoma)
Octreotide (side effects)
Gallbladder disease, pancreatitis, cardiac arrhythmias, hyper or hypothyroidism
Leuprolide (mechanism)
GnRH agonist
Leuprolide (2 uses)
Pulsatile release (mimic normal release) -> increases LH & FSH -> fertility Continuous release -> decreases LH & FSH -> suppress growth of prostate cancer, leiomyomas, endometriosis, and halts precocious puberty
Leuprolide (side effects)
Bone pain, feet/ankle swelling
Somatotropin/Somatotrem (mechanism)
GH analog
Somatotropin/Somatotrem (2 uses)
Dwarfism/short stature
Wasting (assc w/ AIDS or malignancy)
Somatotropin/Somatotrem (side effects)
DM (from decreased insulin sensitivity and hyperglycemia), carpal tunnel syndrome, leukemia, slipped capital femoral epiphyseal plate, edema (hand/foot), thickening of bones
Bromocriptine (mechanism)
D2 agonist
Bromocriptine (2 uses)
Pituitary adenoma (prolactinoma, acromegaly) Parkinson disease (high dose)
Bromocriptine (side effects)
Psychotic sx, dizziness, headache, nausea, confusion
Cabergoline (mechanism)
D2 agonist
Cabergoline (2 uses)
Pituitary adenoma (prolactinoma, acromegaly) Parkinson disease (high dose)
Cabergoline (side effects)
Psychotic sx, dizziness, headache, nausea, confusion
Desmopressin (mechanism)
ADH analog (DDAVP) -> likes V2 receptors (collecting tubules) more than V1 (vascular SMC) Stimulates vWF release from endothelium
Desmopressin (3 uses)
Central DI
vWF disease
Bedwetting
Desmopressin (side effects)
Hyponatremia, headache, flushing
Oxytocin (3 uses)
Induces labor
Decreases postpartum bleeding (by inducing contractions)
Stimulates breast milk letdown
Oxytocin (side effects)
Chest pain, confusion, vaginal bleeding, palpitations, seizures
Iodine (2 uses)
Thyroid storm (inhibits thyroid hormone release when used in large dose) Before thyroidectomy (to prevent thyroid storm)
Radioiodine (2 uses)
Hyperthyroidism
Adjunctive for thyroid cancer
Iodine/Radioiodine (side effects)
Metallic taste, excessive salivation, diarrhea, rash
Alendronate and other “-dronate” (mechanism)
Bisphosphonates
Pyrophosphate analog which is a component of hydroxyapatite -> prevent bone resorption (decreased osteoclast activity)
Alendronate and other “-dronate” (3 uses)
Bisphosphonates
Postmenopausal osteoporosis
Paget disease (reduces bone turnover)
Pt on long-term high-dose glucocorticoid (prevent accelerated bone loss)
Alendronate and other “-dronate” (side effects)
Osteonecrosis of jaw, joint/back pain, GI stuff (heartburn, erosive esophagitis, stomach upset - so take on empty stomach)
Calcitriol (mechanism)
Active vit D
Increases Ca2+ absorption from small intestines
Calcitriol (use)
Hypocalcemia from all causes
Calcitriol (side effects)
Hypercalcemia (so constipation follows), polyuria, weakness, somnolence, headache
Repaglinide (mechanism)
Closes K+ channel in beta cells (at a diff site from sulfonylureas tho) -> depolarization -> increased Ca2+ influx -> insulin release
Unlike sulfonylureas, doesn’t stimulate insulin release when extracellular glucose is low
Repaglinide (use)
DM2 to prevent postprandial hyperglycemia (taken before meals)
CAN use in renal insufficiency (unlike sulfonylureas which have the same mechanism) -> met by liver and excreted by gut
-sone (mechanism)
Glucocorticoids
Also triamcinolone
-sone (2 uses)
Addison disease Immune suppression (inflammation, asthma, etc)
-sone (side effects)
Iaotrogenic Cushing syndrome
Adrenal insufficiency if stopped abruptly after chronic use
Ethinyl estradiol (mechanism)
Estrogen, most common form in OCP
Estrogen (side effects)
Procoagulation, increased risk of endometrial cancer
DES (mechanism)
Estrogen
DES (side effects)
Clear cell adenocarcinoma of vagina in females exposed to DES in utero -> so pulled from market
Mestranol (mechanism)
Estrogen
Clomiphene (mechanism)
SERMs
Anti-estrogen in HYPOTHALAMUS -> increases LH and FSH release
Clomiphene (use)
Infertility due to anovulation (PCOS in women desirous of pregnancy)
Clomiphene (side effects)
Hot flashes, visual disturbances, multiple pregnancies, ovarian enlargement
Tamoxifen (mechanism)
SERMs
Anti-estrogen in BREAST
Agonist in UTERUS and bone
Tamoxifen (use)
ER+ breast cancer (pre-menopausal)
Tamoxifen (side effects)
Endometrial cancer, thrombi
Raloxifene (mechanism)
SERMs
Anti-estrogen in BREAST and UTERUS
Agonist in bone
Raloxifene (2 uses)
ER+ breast cancer (postmenopausal)
Osteoporosis prevention in postmenopausal
Raloxifene (side effects)
Thrombi
Anastrozole (mechanism)
Aromatase inhibitor -> decreases estrogen
Anastrozole (use)
Postmenopausal w/ breast cancer
Exemestane (mechanism)
Aromatase inhibitor -> decreases estrogen
Exemestane (use)
Postmenopausal w/ breast cancer
Progestins (3 uses)
OCP
Endometrial cancer
AUB
Mifepristone/RU-486 (mechanism)
Competitive inhibitor of progestins
Mifepristone/RU-486 (use)
Abortion (used w/ misoprostol - PGE1)
Mifepristone/RU-486 (side effects)
heavy bleeding, GI effects (n/v, anorexia), abd pain
OCP (3 contraindications)
smokers > 35 yo (increased risk of cardiovascular events)
hx of thromboembolism and stroke
hx of estrogen-dependent tumor
Danazol (mechanism)
Partial agonist of androgen
Danazol (2 uses)
Endometriosis
Hereditary angioedema
Danazol (side effects)
Hepatotoxicity, decreased HDL, androgen effects (acne, hirsutism, masculinization), weight gain, edema
Testosterone (2 uses)
Promotes recovery after burn/injury (anabolic effect) Replete testosterone (fix sexual dysfx 2ndary to testosterone deficiency -> like after mumps orchitis)
Testosterone (side effects)
Reduces intratesticular testosterone (neg feedback to LH) -> get gonadal atrophy in males
Premature epiphyseal plate closure
Increases LDL and decreases HDL
Finasteride (mechanism)
5a-reductase inhibitor (so get less conversion from testosterone to DHT)
Finasteride (3 uses)
BPH
Male pattern baldness
Hirsutism
Flutamide (mechanism)
Competitive inhibitor of androgens
Nonsteroidal
Flutamide (2 uses)
Prostate carcinoma
Hirsutism
Ketoconazole (mechanism)
Inhibits 17,20-desmolase -> inhibits steroid synthesis (so affects multiple pathways leading to decreased androgen synthesis)
Spironolactone (mechanism)
Anti-androgen (inhibits steroid binding, 17,20-desmolase, 17a-hydroxylase)
Ketoconazole (use)
PCOS to prevent hirsutism
Spironolactone (use)
PCOS to prevent hirsutism
Ketoconazole (side effects)
Gynecomastia, amenorrhea
Spironolactone (side effects)
Gynecomastia, amenorrhea
-enafil (mechanism)
Inhibits cGMP-specific PDE-5 -> increases cGMP -> SMC relaxation in corpus cavernosum -> erection
-enafil (2 uses)
ED Pulm HTN (prolongs vasodilation)
-enafil (side effects)
Life-threatening hypotension in pts taking nitrates
Impaired blue-green color vision
Headache, flushing, dyspepsia
Fulvestrant (mechanism)
Anti-estrogen
Fulvestrant (use)
ER+ breast cancer (postmenopausal)
Cyproterone (mechanism)
Anti-androgen (at receptor)
Mitotane (mechanism and use)
Adrenocorticolytic drug
For adrenocortical carcinoma
Medroxyprogesterone (use)
Progesterone-only contraceptive IM injection
Pegvisomant (mechanism and use)
GH receptor antagonist
For acromegaly
Podophyllin (mechanism and use)
Inhibits topoisomerase II
Topically for genital warts
“-gliflozin” (mechanism and use)
Canagliflozin and dapagliflozin
Inhibits SGLT2 (transporters in renal tubule lumen) -> urinary glucose loss
For DM2
“-gliflozin” (3 side effects)
UTI, genital mycotic infections
Hypotension
Avoided in pts w/ renal impairment!
Danazole (mechanism and 3 uses)
Androgen used to suppress LH and FSH release by pituitary
Endometriosis, hemophilia, ITP
Nandrolone (mechanism and use)
Anabolic steroids
For anemia caused by kidney failure