Gi, Endocrine, Repro And Rheum Drugs

Front 1

Cimetidine, ranitidine, famotidine, nizatidine

Back 1

H2 blockers
MECH: reversibly block histamine H2 receptors → ↓H+ secretion by parietal cells
USE: peptic ulcer, gastritis, mild GERD
TOX: Cimetidine: inhibits P-450, antiandrogenic, cross BBB (confusion, dizziness, HA) and placenta; cime- and ranitidine ↓ renal excretion of creatinine

Hint 1

GI

Front 2

Omeprazole, lansoprazole

Back 2

PPI
MECH: irreversibly inhibit H+/K+ ATPase in parietal cells
USE: peptic ulcer, gastritis, GERD, Zollinger-Ellison

Hint 2

GI

Front 3

Bismuth, sucralfate

Back 3

MECH: binds ulcer base providing physical protection and allowing HCO3- secretion to reestablish pH gradient in mucus layer
USE: ↑ ulcer healing, travelers diarrhea, H. pylori triple therapy

Hint 3

GI

Front 4

Misoprostol

Back 4

MECH: PGE1 analog →↑ production and secretion of gastric mucous barrier, ↓acid production
USE: prevention of NSAID-induced pep ulcers; maintenance of PDA; post-coital abortifacient
TOX: diarrhea, abortifacient

Hint 4

GI, Congenital, Repro

Front 5

Pirenzepime, propantheline

Back 5

Muscarinic antagonists
MECH: block M1 receptors on ECL →↓histamine secretion; block M3 on parietal cells →↓H+ secretion
USE: Peptic ulcer
TOX: tachycardia, dry mouth, difficulty focusing

Hint 5

GI

Front 6

Infliximab

Back 6

MECH: monoclonal antibody to TNF-alpha → ↓inflammation
USE: Crohn's dz, RA, ankylosing spondylitis
TOX: respiratory infection, fever, hypotension, TB reactivation

Hint 6

GI, Rheum

Front 7

Sulfasalazine

Back 7

MECH: Combo of sulfapyridine (antibacterial) and mesalamine (anti-inflam)
USE: IBD (Crohns's and UC)
TOX: malaise, nausea, sulfonamide tox, reversible oligospermia

Hint 7

GI

Front 8

Ondansetron

Back 8

Central-acting antiemetic
MECH: 5-HT3 antagonist
USE: Post op vomiting, CA chemotherapy
TOX: HA, constipation

Hint 8

GI

Front 9

Cisapride

Back 9

Pro-kinetic agent
MECH: Acts through seratonin receptors to ↑ACh release at myenteric plexus →↑esophageal tone and ↑ gastroduodenal contractility
USE: no longer used
TOX: torsades de pointes with other drugs (erythromycin, ketoconazole, nefazodone, fluconazole)

Hint 9

GI

Front 10

Metoclopramide

Back 10

Pro-kinetic agent
MECH: D2 receptor antagonist →↑resting tone, contractility, LES tone, motility; does not increase transit time through colon
USE: diabetic and post op gastroparesis
TOX: ↑Parkinson's effects, restlessness, drowsines, fatigue, depression, nausea, constipation

Hint 10

GI

Front 11

Metformin

Back 11

Biguanide
MECH: ↓hepatic glucose output (↓gluconeogensis); sensitizes the liver to insulin.
USE: Oral hypoglycemic
TOX: lactic acidosis; *does not cause hypoglycemia

Hint 11

Diabetes

Front 12

Tolbutamide

Back 12

Sulfonylureas - 1st generation
MECH:Close ATP/ADP K-channel → beta-cell depolarization →↑Ca influx → insulin release
USE: Type 2 DM only (must have some islet function)
TOX: disulfiram-like effects

Hint 12

Diabetes

Front 13

Chlorpropamide

Back 13

Sulfonylureas - 1st generation
MECH:Close ATP/ADP K-channel → beta-cell depolarization →↑Ca influx → insulin release
USE: Type 2 DM only (must have some islet function)
TOX: disulfiram-like effects

Hint 13

Diabetes

Front 14

Glyburide

Back 14

Sulfonylureas - 2nd generation (more potent)
MECH:Close ATP/ADP K-channel → beta-cell depolarization →↑Ca influx → insulin release
USE: Type 2 DM only (must have some islet function)
TOX: hypoglycemia

Hint 14

Diabetes

Front 15

Glimepiride

Back 15

Sulfonylureas - 2nd generation (more potent)
MECH:Close ATP/ADP K-channel → beta-cell depolarization →↑Ca influx → insulin release
USE: Type 2 DM only (must have some islet function)
TOX: hypoglycemia

Hint 15

Diabetes

Front 16

Glipizide

Back 16

Sulfonylureas - 2nd generation (more potent)
MECH:Close ATP/ADP K-channel → beta-cell depolarization →↑Ca influx → insulin release
USE: Type 2 DM only (must have some islet function)
TOX: hypoglycemia

Hint 16

Diabetes

Front 17

Rosiglitazone

Back 17

Glitazone
MECH: Activate nuclear receptors (PPAR-γ) →↑insulin sensitivity (↓insulin resistance)
USE: Type 2 DM (monotherapy or combined with other agents)
TOX: Weight gain, edema (CHF), *MI

Hint 17

Diabetes

Front 18

Pioglitazone

Back 18

Glitazone
MECH: Activate nuclear receptors (PPAR-γ) →↑insulin sensitivity (↓insulin resistance)
USE: Type 2 DM (monotherapy or combined with other agents)
TOX: Weight gain, edema (CHF)

Hint 18

Diabetes

Front 19

Acarbose

Back 19

α-glucosidase inhibitor
MECH: Inhibit intestinal brush border α-glucosidases → delayed sugar hydrolysis and glucose absorption → ↓postprandial hyperglycemia
USE: Type 2 DM
TOX: flatulence and diarrhea (limit use)

Hint 19

Diabetes

Front 20

Miglitol

Back 20

α-glucosidase inhibitor
MECH: Inhibit intestinal brush border α-glucosidases → delayed sugar hydrolysis and glucose absorption → ↓postprandial hyperglycemia
USE: Type 2 DM
TOX: flatulence and diarrhea (limit use)

Hint 20

Diabetes

Front 21

Lispro

Back 21

Insulin - Fast acting
MECH: Binds insulin receptor →
Liver: ↑glucose storage (glycogen)
Muscle: ↑glycogen and protein synthesis; K+ uptake
Fat: aids TG storage
USE: Type 1 DM; life-threatening hyperkalemia, stress-induced hyperglycemia
TOX: hypoglycemia

Hint 21

Diabetes

Front 22

Insulin

Back 22

Insulin - Short acting
MECH: Binds insulin receptor →
Liver: ↑glucose storage (glycogen)
Muscle: ↑glycogen and protein synthesis; K+ uptake
Fat: aids TG storage
USE: Type 1 DM; life-threatening hyperkalemia, stress-induced hyperglycemia
TOX: hypoglycemia

Hint 22

Diabetes

Front 23

NPH (“Neutral protamine Hagedorn”)

Back 23

Insulin - intermediate acting (slow solubilization)
MECH: Binds insulin receptor →
Liver: ↑glucose storage (glycogen)
Muscle: ↑glycogen and protein synthesis; K+ uptake
Fat: aids TG storage
USE: Type 1 DM; life-threatening hyperkalemia, stress-induced hyperglycemia
TOX: hypoglycemia

Hint 23

Diabetes

Front 24

Lente

Back 24

Insulin - long acting
MECH: Binds insulin receptor →
Liver: ↑glucose storage (glycogen)
Muscle: ↑glycogen and protein synthesis; K+ uptake
Fat: aids TG storage
USE: Type 1 DM; life-threatening hyperkalemia, stress-induced hyperglycemia
TOX: hypoglycemia

Hint 24

Diabetes

Front 25

Ultralente

Back 25

Insulin - long acting
MECH: Binds insulin receptor →
Liver: ↑glucose storage (glycogen)
Muscle: ↑glycogen and protein synthesis; K+ uptake
Fat: aids TG storage
USE: Type 1 DM; life-threatening hyperkalemia, stress-induced hyperglycemia
TOX: hypoglycemia

Hint 25

Diabetes

Front 26

Orlistat

Back 26

MECH: inhibits pancreatic lipases → altered fat absorption and metabolism
USE: long-term obesity management (with a modified diet)
TOX: Steatorrhea, GI discomfort, reduced absorption of fat-soluble vitamins, HA

Hint 26

endocrine

Front 27

Sibutramine

Back 27

MECH: 5HT & norepi reuptake inhibitor → appetite suppression (centrally acting)
USE: short- and long-term obesity managment
TOX: HTN, tachycardia

Hint 27

endocrine

Front 28

Propylthiouracil

Back 28

MECH: inhibits thyroperoxidase (organification and coupling of thyroid hormone synthesis); ↓ peripheral conversion of T4 to T3
USE: Hyperthyroidism
TOX: skin rash, agranulocytosis, aplastic anemia

Hint 28

endocrine

Front 29

Methimazole

Back 29

MECH: inhibits thyroperoxidase (organification and coupling of thyroid hormone synthesis)
USE: Hyperthyroidism
TOX: skin rash, agranulocytosis (sore throat, fever, arthralgias), aplastic anemia

Hint 29

endocrine

Front 30

Growth Hormone (GH)

Back 30

USE: GH deficiency, Turner's syndrome

Hint 30

endocrine

Front 31

Somatostatin

Back 31

MECH: Inhibits growth hormone, glucagon, insulin, LH, 5HT, gastin VIP
USE: acromegaly, carcinoid, gastrinoma, glucagonoma

Hint 31

endocrine

Front 32

Octreotide

Back 32

Somatostatin analog
MECH: Inhibits growth hormone, glucagon, insulin, LH, 5HT, gastin VIP
USE: acromegaly, carcinoid, gastrinoma, glucagonoma
TOX: long QT

Hint 32

endocrine

Front 33

Desmopressin

Back 33

ADH
USE: central diabetes insipidis

Hint 33

endocrine

Front 34

Oxytocin

Back 34

USE: stimulate labor, uterine contractions

Hint 34

endocrine

Front 35

Levothyroxine

Back 35

MECH: thyroxine replacement
USE: hypothyroidism, myxedema
TOX: tachycardia, heat intolerance, tremors

Hint 35

endocrine

Front 36

Triiodothyronine

Back 36

MECH: thyroxine replacement
USE: hypothyroidism, myxedema
TOX: tachycardia, heat intolerance, tremors

Hint 36

endocrine

Front 37

Glucocorticoids (hydrocortisone, prednisone, triamcinolone, dexamethasone, beclomethasone)

Back 37

MECH:
Anti-inflammatory: inhibit phospholipase A2 →↓ production of leukotrienes and prostaglandins; inhibit release of histamine and 5HT
Immunosuppression: inhibit production of IL-2 and T-lymphocytes
USE: Addison's dz, inflammation, immune suppression, asthma/allergy
TOX: Iatrogenic Cushing's

Hint 37

endocrine, rheum

Front 38

Ketoconazole

Back 38

MECH: inhibits steroid synthesis
USE: Cushing dz
TOX: liver dysfunction, gynecomastia

Hint 38

endocrine

Front 39

Democlocycline

Back 39

MECH: impairs ADH (tetracycline)
USE: SIADH
TOX: binds calcifying tissue

Front 40

Finasteride

Back 40

MECH: 5 alpha-reductase inhibitor →↓conversion of T to DHT
USE: BPH; male-pattern baldness

Hint 40

Male repro

Front 41

Flutamide

Back 41

MECH: nonsteroidal competitive inhibitor of androgens at T receptors
USE: prostate CA

Hint 41

Male repro

Front 42

Leuprolide

Back 42

MECH: GnRH analog with agonist properties when used in a pulsatile fashion; antagonist when used continuously
USE: infertility, prostate cancer, uterine fibroids
TOX: antiandrogen, N/V

Hint 42

Reprp

Front 43

Sildenafil, Vardenafil

Back 43

MECH: inhibit cGMP phosphodiesterase →↑cGMP → smooth muscle relaxation in corpus cavernosum →↑blood flow → erection
USE: erectile dysfunction
TOX: hypotension with nitrates, HA, flushing, dyspepsia, blue-green color conversion.

Hint 43

Male repro

Front 44

Clomiphene

Back 44

MECH: partial agonist of estrogen receptors in pituitary gland → prevents normal feedback inhibition →↑release of LH and FSH → ovulation
USE: infertility
TOX: hot flashes, ovarian enlargment, multiple simultaneous pregnancies, visual disturbances

Hint 44

Female repro

Front 45

Mifepristone (RU-486)

Back 45

MECH: Competitive inhibitor of progestins at progesterone receptors
USE: postcoital abortifacient (prevents implantation)
TOS: heavy bleeding, GI, abdominal pain

Front 46

Opiod analgesis (morphine, fentanyl, codeine, heroine, meperidine)

Back 46

MECH: opioid receptor agonists modulate synaptic transmission
USE: pain, acute pulmonary edema
TOX: addiction, respiratory depression, miosis (pinpoint pupils), additive CNS depression, constipation. Tox treated with naloxone/naltrexone

Front 47

Dextromethorphan

Back 47

MECH: opioid receptor agonists modulate synaptic transmission
USE: cough suppression

Front 48

Methadone

Back 48

MECH: opioid receptor agonists modulate synaptic transmission
USE: maintenance program for addicts
TOX: addiction, respiratory depression, miosis (pinpoint pupils), additive CNS depression, constipation. Tox treated with naloxone/naltrexone

Front 49

Loperamide and diphenoxylate

Back 49

MECH: opioid receptor agonists modulate synaptic transmission
USE: diarrhea

Front 50

Ibuprofen

Back 50

NSAID
MECH: reversibly inhibits COX-1 and-2 →↓ prostaglandin synthesis
USE: antipyretic, analgesic, anti-inflammatory
TOX: renal damage, aplastic anemia, GI distress, ulcers

Hint 50

Rheum

Front 51

Naproxen

Back 51

NSAID
MECH: reversibly inhibits COX-1 and-2 →↓ prostaglandin synthesis
USE: antipyretic, analgesic, anti-inflammatory
TOX: renal damage, aplastic anemia, GI distress, ulcers

Hint 51

Rheum

Front 52

Ketorolac

Back 52

NSAID
MECH: reversibly inhibits COX-1 and-2 →↓ prostaglandin synthesis
USE: antipyretic, analgesic, anti-inflammatory
TOX: renal damage, aplastic anemia, GI distress, ulcers

Hint 52

Rheum

Front 53

Indomethacin

Back 53

NSAID
MECH: reversibly inhibits COX-1 and-2 →↓ prostaglandin synthesis
USE: close PDA
TOX: renal damage, aplastic anemia, GI distress, ulcers

Hint 53

Rheum

Front 54

celecoxib, valdecoxib

Back 54

COX-2 inhibitors
MECH: Reversibly inhibits COX-2, by sparing COX-1 it should allow maintenance of GI mucosa and not cause ulcers/bleeding
USE: RA, osteoarthritis
TOX: ↑risk of thrombosis

Hint 54

Rheum

Front 55

Acetaminophen

Back 55

MECH: reversibly inhibits cyclooxygenase - mostly in CNS because inactivated peripherally
USE: antipyretic, analgesic
TOX: OD → hepatic necrosis (metabolite depletes glutathione and forms toxic tissue adducts); Antidote = N-acetylcysteine → regenerates glutathione

Hint 55

Rheum

Front 56

Colchicine

Back 56

MECH: depolymerizes microtubules impairing leukocyte chemotaxis and degranulation
USE: acute gout
TOX: GI (given orally)

Hint 56

Gout

Front 57

Probenicid

Back 57

MECH: inhibits reabsorption of uric acid; inhibits secretion of penicillin
USE: chronic gout

Hint 57

Gout

Front 58

Allopurinol

Back 58

MECH: inhibits xanthine oxidase →↓conversion of xanthine to uric acid
USE: chronic gout; lymphoma/leukemia to prevent tumor lysis associated urate nephropathy

Hint 58

Gout

Front 59

Etanercept

Back 59

MECH: recombinant TNF receptor that binds TNF-alpha
USE: RA, psoriasis, ankylosing spondylitis

Hint 59

Rheum

Front 60

Cyclosporine

Back 60

MECH: binds cyclophilins → inhibits calcineurin → ↓IL-2 → ↓activation/differentiation of T cells
USE: suppress acute organ rejection after transplantation, autoimmune disorders
TOX: ↑viral infection and lymphoma, nephrotox (preventable with mannitol diuresis)

Hint 60

Rheum

Front 61

Tacrolimus (FK506)

Back 61

MECH: Binds FK-binding protein → ↓ IL-2 and other cytokines
USE: suppress acute organ rejection after transplantation
TOX: significant - nephrotox, peripheral neuropathy, HTN, pleural effusion, hyperglycemia

Hint 61

Rheum

Front 62

Azathioprine

Back 62

MECH: antimetabolite of 6-mercaptopurine that interferes with metabolism and synthesis of nucleic acids → toxic to proliferating lymphocytes
USE: kidney transplant, autoimmune disorders, glomerulonephritis, hemolytic anemia
TOX: bone marrow suppression, metabolized by xanthine oxidase - tox ↑ by allopurinol (xanthine oxidase involved in metabolism)

Hint 62

Rheum