GI Pharmacology-B Flashcards
Which Anti-androgenic Agent causes a disulfuram type reaction
Nilutamide
Abiraterone: Drug Class
Anti-androgenic Agent
Abiraterone: Mechanism of action
Selectively and irreversibly inhibits CYP17, an enzyme required for androgen biosynthesis, thus inhibiting the formation of testosterone precursors
Abiraterone: Uses
FDA approved for Tx of metastatic, castration-resistant prostate cancer in patients previously treated with docetaxel (now approved as first line Tx)
Enzalutamide: Drug Class
Anti-androgenic Agent
Enzalutamide: Mechanism of action
It is a pure androgen receptor signaling inhibitor. It has no agonistic properties, It inhibits androgen receptor nuclear translocation, DNA binding, and coactivator mobilization leading to cellular apoptosis
Enzalutamide: Uses
FDA approved for Tx of metastatic, castration-resistant prostate cancer in patients previously treated with docetaxel
Enzalutamide: Side Effects
Peripheral edema, fatigue, headache, hot flashes, diarrhea, neutropenia
Abiraterone: Side Effects
Edema, hypertriglyceridemia, hypokalemia, hypophosphatemia, diarrhea
Which Anti-androgenic Agent must be given with prednisone because it inhibits the production of cortisol
Abiraterone
Fulvestrant: Drug Class
Estrogen Receptor Antagonist
Fulvestrant: Mechanism of action
Steroid compound that competitively binds estrogen receptors. Produces nuclear complex that decreases DNA synthesis and inhibits estrogen effects. No ER agonist activity (pure antagonist). Down-regulates ER and inhibits tumor growth
Fulvestrant: Uses
2nd line therapy in postmenopausal women after disease progression on SERM or AI therapy
Fulvestrant: Side Effects
Hot flashes, nausea, angioedema, weakness, local site reaction
Degarelix: Drug Class
Gonadotropin Releasing Hormone Antagonist
Degarelix: Mechanism of action
LHRH antagonist. Major advantage is immediate down regulation of testosterone; no tumor flare
Degarelix: Uses
Equivalent to leuprolide in decreasing testosterone levels for up to one year and FDA approved for treatment of advanced prostate cancer
Degarelix: Side Effects
Hot flashes, injection site reactions
Cholestyramine: Drug Class
Bile acid resin
Bile acid resins: Mechanism of action
Bind negatively charged bile acids which bind consumed cholesterol and everything is excreted
Bile acid resins: Side Effects
Non-compliance (It tastes bad), Increases HMGCoA activity and triglyceride synthesis (May lead to a transient increase in TG/VLDL), steatorrhea, abdominal bloating
Colestipol: Drug Class
Bile acid resin
Name the two Bile acid resins
Cholestyramine and Colestipol
Ezetimibe: Drug Class
Transport inhibitor
Ezetimibe: Mechanism of action
Blocks absorption of cholesterol in the small intestine
Ezetimibe is contraindicated in what patients
Patients with moderate to severe hepatic insufficiency
Simvastatin + Ezetimibe: Combination drug with what trade name
Vytorin
What advantage does combination therapy like Simvastatin + Ezetimibe (Vytorin) have
It reduces the potential side effects of statins by allowing for lower dose of the statin drug to be used to obtain specific reduction in cholesterol
Fluvastatin: Drug Class
HMG Co A Reductase inhibitor
HMG Co A Reductase inhibitors: Mechanism of action
Inhihibits HMGCoA reductase which catalyzes the conversion of Acetyl CoA to Malvonic acid (a key step in the synthesis of cholesterol). This causes low cholesterol in the liver which responds by increasing hepatic LDL receptors removing LDL from the blood).
Lovastatin: Drug Class
HMG Co A Reductase inhibitor
Pravastatin: Drug Class
HMG Co A Reductase inhibitor
HMG Co A Reductase inhibitors: Mechanism of action
Can cause rhabdomyolysis (rare but may be life threatening), transaminase hepatitis (check liver enzymes)
Simvastatin: Drug Class
HMG Co A Reductase inhibitor
HMG Co A Reductase inhibitors are contraindicated in what patients
Contraindicated in patients with renal failure and patients taking cyclosporine, macrolide antibiotics, various antifungal agents, and cytochrome P-450 inhibitors
Atorvastatin: Drug Class
HMG Co A Reductase inhibitor
Rosuvastatin: Drug Class
HMG Co A Reductase inhibitor
Name the six statins in order from least to most potent
(For Love People Say Anything Really) Fluvastatin < Lovastatin < Pravastatin < Simvastatin < Atorvastatin < Rosuvastatin
Clofibrate: Drug Class
Fibric Acid
Name the two Fibric Acids
Clofibrate and Gemfibrozil
Fibric Acids: Side Effects
Dyspepsia, gallstones, myopathy (particularly in combination with statins)
Gemfibrozil: Drug Class
Fibric Acid
Fibric Acids: Mechanism of action
Inhibits fatty acid synthesis, causes lipoprotein lipase-enhanced hydrolysis, stimulates synthesis of apoA-1
Niacin: Drug Class
Nicotinic Acid
Niacin: Mechanism of action
Inhibits VLDL secretion and increases clearance of VLDL via lipoprotein lipase pathway
Niacin: Side Effects
Intense flushing, and associated pruritis (one aspirin can relieve symptom), nausea, abdominal pain, hyperuricemia, hyperglycemia (acanthosis nigricans associated with insulin resistance), hepatotoxicity (increased transaminase, & ALT, flu-like fatigue)
What is the most effective agent for increasing HDL
Niacin
Niacin is contraindicated in what patients
Contraindicated in patients with peptic ulcer disease
Cimetidine (Tagamet): Function and drug class
Control of Gastric Acid, H2 blocker
Name the four H2 blockers
Cimetidine, Ranitidine, Famotidine, Nizatidine
Which H2 blocker inhibits CYP450 and thus can cause drug-drug interactions
Cimetidine
Ranitidine (Zantac): Function and drug class
Control of Gastric Acid, H2 blocker
Cimetidine (Tagamet) may increase the secretion of what hormone
Prolactin
Famotidine (Pepcid): Function and drug class
Control of Gastric Acid, H2 blocker
Nizatidine (Axid): Function and drug class
Control of Gastric Acid, H2 blocker
H2 blockers are useful in treating what
Gastric and duodenal ulcers, and zollinger-Ellison Syndrome (non-beta islet cell, gastrin-secreting tumor of the pancreas that stimulates the acid-secreting cells of the stomach to maximal activity)
Omeprazole (Prilosec): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
Proton Pump Inhibitors: Mechanism of action
Inhibit the K+/H+ ATPase on parietal cells
Proton Pump Inhibitors are superior to H2 blockers in healing of what
NSAID-induced gastric ulcers
Lansoprazole (Prevacid): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
Name the five proton pump inhibitors
Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole
Long term use of proton pump inhibitors is associated with
Hip fractures and possibly hypomagnesemia
Rabeprazole (Aciphex): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
Pantoprazole (Protonix): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
Esomeprazole (Nexium): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
The transient rebound in stomach acid secretion after withdrawing a proton pump inhibitor is a result of increased gastrin levels and can last up to how long
Up to 4 weeks
Atropine: Function and drug class
Control of Gastric Acid, Antimuscarinic
By what mechanism do antimuscarinics affect acid secretion by parietal cells
They block stimulation of muscarinic receptors on parietal cells. Stimulation of these receptors would normally result in increased intracellular Ca++ and activation of the H+/K+ ATPase that pumps proteins into the lumen
Which two antimuscarinics are used to reduce gastric acid secretion
Atropine and Glycopyrrolate
Glycopyrrolate: Function and drug class
Control of Gastric Acid, Antimuscarinic
Misoprostol: Function and drug class
Control of Gastric Acid, Cytoprotective
Misoprostol is an analogue of what
PGE-1
Misoprostol: Mechanism of action
It stimulates PG receptor leading to increased mucous & bicarbonate secretion, and decreases cAMP which decreases HCL secretion
Misoprostol is only used to treat what
A NSAID-induced ulcer
When is Misoprostol contraindicated
During pregnancy (its an abortifacient)
Sucralfate: Function and drug class
Control of Gastric Acid, Cytoprotective
Sucralfate: Mechanism of action
It polymerizes into a sticky gel under acidic conditions which has affinity for exposed protein in crater of an ulcer and inhibits back diffusion of H+ and reduces pepsin activity
Metronidazole & Tetracycline: Function and drug class
Ulcer repair, Antibiotic
Metronidazole & Tetracycline is administered with what
Bismuth subsalicylate (pepto bismol)
What are the two antibiotic regimens for H. Pylori infection
Metronidazole + Tetracycline and Clarithromycin
Clarithromycin: Function and drug class
Ulcer repair, Antibiotic
Clarithromycin is administered with what
Omeprazole
How long are Metronidazole + Tetracycline or Clarithromycin administered for treatment of H. Pylori
14 days
Metoclopramide: Function and drug class
Prokinetic Agent, Increase Acetylcholine
Metoclopramide: Mechanism of action
It is a cholinomimetic and a D2 receptor blocker. It promotes the release of acetylcholine from myenteric neurons
Metoclopramide is used to treat what
GERD and diabetic gastroparisis
Cisapride: Function and drug class
Prokinetic Agent, Increase Acetylcholine
Cisapride
It promotes the release of acetylcholine from myenteric neurons and acts as a 5-HT4 receptor agonist. Has similar prokinetic effects as metoclopramide
How does Cisapride differ from Metoclopramide
It is not a D2 blocker and so does not have antiemetic properties. It also has greater effect on the colon
Name the two prokinetic agents
Metoclopramide and Cisapride
Diphenoxylate (Lomotil): Function and drug class
Antidiarrheal, Opioid
What is Diphenoxylate administered with to discourage deliberate abuse
Sub-therapeutic dose of atropine
Loperamide (Imodium): Function and drug class
Antidiarrheal, Opioid
Name the two antidiarrheal agents
Diphenoxylate and Loperamide
Bismuth subsalicylate (Pepto): Function and drug class
Antidiarrheal, Salicylate
Bismuth subsalicylate (Pepto) can cause what syndrome
Reyes Syndrome
Thymoglobulin: What drug class [and is it used for induction or maintainance therapy]
Anti-lymphocyte globulin (Rabbit derived) [used as an induction agent]
Thymoglobulin: Mechanism of Action
Complement-mediated cell lysis of circulating T-cells
Cytokine release syndrome, serum sickness, leukopenia, and thrombocytopenia are the side effects of what drug
Thymoglobulin
Basiliximab: What drug class [and is it used for induction or maintainance therapy]
Monoclonal Antibody (against IL-2 receptor) [used as an induction agent]
Basiliximab: Mechanism of Action
It binds to the alpha unit of the IL-2 receptor inhibiting binding of IL-2 thereby preventing activation of lymphocytes
Abdominal pain, dizziness, and insomnia are the side effects of what drug
Basiliximab
Methylprednisolone: What drug class [and is it used for induction or maintainance therapy]
Corticosteroid [used as an induction agent]
Methylprednisolone: Mechanism of Action
Blocks cytokine gene expression resulting in a decreased immune response
Hypertension, fluid retention, hyperglycemia, impaired wound healing, mood disturbances, and vivid dreams are the side effects of what drug
Methylprednisolone
Tacrolimus: What drug class [and is it used for induction or maintainance therapy]
Calcineurin Inhibitor [used as a maintainance agent]
Tacrolimus: Mechanism of Action
Inhibits IL-2 synthesis by blocking calcineurin
Alopecia, hyperglycemia, hyperkalemia, nephrotoxicity, neurologic toxicity are the side effects of what drug
Tacrolimus
Mycophenolate: What drug class and is it used for induction or maintainance therapy
Antimetabolite [used as a maintainance agent]
Mycophenolate: Mechanism of Action
Inhibits proliferation of T and B cells by preventing RNA and DNA synthesis
GI intolerance, bone marrow suppression are the side effects of what drug
Mycophenolate
Sirolimus: What drug class and is it used for induction or maintainance therapy
mTOR Inhibitor [used as a maintainance agent]
Sirolimus: Mechanism of Action
Binds to FKBP-12 forming a complex that inhibits the activation of T cells and B cells by inhibiting their response to interleukin-2 (IL-2)
Anemia, hepatic artery thrombosis, hyperlipidemia, impaired wound healing, proteinuria are the side effects of what drug
Sirolimus
Prednisone: What drug class and is it used for induction or maintainance therapy
Corticosteroid [used as a maintainance agent]
Prednisone: Mechanism of Action
Blocks cytokine gene expression resulting in a decreased immune response
Chronic adrenal insufficiency, GERD, Hyperglycemia, hypertension, and osteoporosis are the side effects of what drug
Prednisone
The effectiveness of which Immunosuppression drug(s) is decreased by CYP450 3A4 inducers
Tacrolimus and Sirolimus
The effectiveness of which Immunosuppression drug(s) is decreased by aluminum & magnesium containing antacids and by cyclosporine
Mycophenolate