Flashcards in EXAM #2: REVIEW Deck (165):
What drug is used to prevent the adverse effects of high dose methotrexate?
What are the unique adverse effects associated with Methotrexate?
What enzyme does 5-FU inhibit?
What are the unique adverse effects associated with 5-FU?
Oral and GI ulcers
What is Capecitabine?
What is disease is Cytarabine primarily used as a chemotheraputic agent for?
What enzyme does Cytarabine require to be activated?
What enzyme inactivates Cytatabine?
What is the unique syndrome seen with Cytarabine? What are the symptoms?
What enzyme activates Gemcitabine into its active form?
What enzyme does Gemcitabine specifically inhibit?
What enzyme do 6-Mercaptopurine and 6-Thioguanine require for activation?
What enzyme inactivates 6-Mercaptopurine?
Thiopurine Methyltransferase (TPMT)
What diseases are 6-MU and 6-TG commonly used to treat?
AML and ALL
What disease is Fludarabine used to treat?
What enzyme activates Fludarabine?
What enzymes does Fludarabine specifically inhibit?
*****Also inhibits mRNA translation*****
What disease is Cladrabine used to treat?
Hairy Cell Leukemia
What enzyme does Cladrabine specifically inhibit?
What is the mechanism of action of Cyclophosphamine?
Nitrogen mustard DNA alkylating agent
What is the metabolite of Cyclophosphamine that is particularly harmful? What does it cause?
What drug is used to prevent Hemorrhagic cystitis in Cyclophosphamine administration?
What is the mechanism of action of Carmustine? What is it used to treat?
Nitrosurea alkylating agent that is highly lipophilic --> Brain cancer
What two enzymes reduce the efficacy of the DNA alkylating agents?
List the three Platinum compounds. What is their mechanism of action?
These drugs are all non-classical DNA alkylating agents
What are the unique adverse effects associated with Cisplatin?
How is the neprotoxicity associated with Cisplastin prevented?
Co-administration with IV saline
What adverse effect is seen with Carbiplatin?
What is the mechanism of action of Procarbazine? What is it used to treat?
Non-classical alkylating agent used to treat Hodgkins' Disease
What is the mechanism of action of Dacarbazine? What is it used to treat?
Non-classical alkylating agent used to treat Melamona and Sarcoma
What is the mechanism of action of Temozolamide? What is it used to treat?
Non-classical alkylating agent used to treat Glioblastoma and Melanoma
List the Anti-microtubule drugs. What phase of the cell cycle do these agents perturb?
Which of the anti-microtubule drugs inhibit microtubule polymerization?
Vinblastine and Vincristine
Which of the anti-microtubule drugs inhibit microtubule depolymerization?
What is the unique adverse effect seen with Vincristine?
What is the unique adverse effect seen with Paclitaxel?
What drugs are used to prevent the anaphylaxis seen with Paclitaxel?
What drug is given to counteract the myelosuppression seen with Paclitaxel?
Filgrastim, a G-CSF drug
List the Topoisomerase I inhibitors.
List the Topoisomerase II inhibitor.
What is the mechanism of action of Doxorubicin?
This is an antibiotic that:
- Topoisomerase II inhibitor
- Intercalates DNA
- Inhibits DNA polymerase
What is the unique adverse effect seen with Doxorubicin?
How is the cardiomyopathy seen with Doxorubicin prevented?
What is the mechanism of action of Bleomycin?
Small peptide that cause single and double strand DNA breaks in G2
What unique adverse effect is seen with Bleomycin?
What is the mechanism of action of Tamoxifen?
Estrogen receptor antagonist
*****Treats estrogen receptor positive breast cancer
What is the mechanism of action of Anastrazole?
Inhibits aromatase to prevent conversion of Testosterone to estrogen in post-menopausal women with estrogen receptor positive breast cancer
What is the mechanism of action of Leuprolide and Goserelin?
These are GnRH AGONISTS used to treat prostate cancer
What is the mechanism of action of Degarelix?
GnRH ANTAGONIST used to treat prostate cancer
What is the mechanism of action of Trastuzumab?
HER-2 receptor antagonist
What is the unique side effect seen with Trastuzumab?
What is the mechanism of action of Cetuximab?
EGFR antagonist used to treat COLON CANCER
Activating mutation of what proto-oncogene limits the efficacy of Cetuximab?
What is the mechanism of action of Bevacizumab?
What is the mechanism of action of Lapinotab?
EGFR and HER-2blocker (downstream target) used for REFRACTORY BREAST CANCER
What is the mechanism of action of Erlotinib?
EGFR receptor blocker used for NON SMALL CELL LUNG CANCER
What is the unique side effect associated with Asparaginase?
What is the mechanism of action of Bortezomib?
Proteasome inhibitor that increases p53
What is the unique adverse effect associated with Bortezomib?
What is the mechanism of action of Temsirolimus?
What are the unique adverse effects seen with Temsirolimus?
Which antineoplastic agents are nephrotoxic?
Which antineoplastic agents are neurotoxic?
Which antineoplastic agents are cardiotoxic?
Which antineoplastic agents cause bladder toxicity?
Which antineoplastic agents cause hypersensitivity reactions/ anaphylaxis?
List the ADP receptor antagonists/ P2Y12 antagonists.
Which ADP receptor antagonists are irreversible?
Which ADP receptor antagonists are reversible?
Which ADP receptor antagonists have been shown to be more efficacious? What is their drawback?
****Despite being more efficacious, also associated with more bleeding****
What CYP enzyme metabolizes Clopidegril?
What is the clinical significance of CYP2C19?
- Highly polymorphic
- Inhibited by omeprazole i.e. omeprazole increases the efficacy of Clopidegril
List the GPIIb/IIIa antagonists. Which of these are a Fab antibody, peptide, and non-peptide small molecule?
Abciximab - Fab antibody
Tirofiban- non-peptide small molecule
What are the adverse effects seen with GPIIb/IIIa administration?
What is the mechanism of action of Voraxapar?
What is the adverse effect associated with Voraxapar?
****Note that this drug is contraindicated in patients with a history of intracranial bleeding
What is dual anti-platelet therapy? Triple?
Dual= ASA and clopidegril
Triple= + Warfarin
List the indirect thrombin/ Factor X inhibitors. What is the difference between these three drugs?
Enoxaparin - LMWH
Fondapainaux - Pentasaccharide
What are the adverse effects associated with Heparin?
What drug reverses Heparin?
List the direct thrombin inhibitors.
Which of the direct thrombin inhibitors is divalent? What does this mean?
"rudins" --> block the active site and E1 site on Thrombin
Which of the direct thrombin inhibitors is monovalent? What does this mean?
"an's" -->block only the active site
List the direct Factor Xa inhibitors.
What enzyme metabolizes Warfarin?
List the fibrinolytic drugs.
What are the unique adverse effects seen with Streptokinase administration?
What drugs can reverse fibrinolytic therapy?
Draw the general pathway of cholesterol metabolism.
What drug blocks NPC1L1?
What is the function of Apo C-II?
Activation of LPL
What is the transporter that get cholesterol from the periphery into HDL?
What disorder is characterized by decreased LPL expression or function?
What is the manifestation of Primary Chylomicronemia?
Increased chylomicrons and VLDL
Which drugs are best at treating Primary Chylomicronemia?
Fibrates and Niacin
What disease is characterized by decreased Apo E function of expression?
What is the manifestation of Dysbetalipoproteinemia?
Increased IDL and chylomicron remnants
What is the best therapy for Dysbetalipoproteinemia?
Fibrates and Niacin
What disease is characterized by decreased apo C-II function or expression?
What is the manifestation of Familial Hypertriglyceridemia ?
Increased Chylomicrons and VLDL
What is the best therapy for Familial Hypertriglyceridemia ?
Fibrates and Niacin
What disease is characterized by decreased LDLR function or expression?
What is the manifestation of Familial Hypercholesterolemia?
What is the best therapy for Familial Hypercholesterolemia?
Bile acid binding resins
What is the effect of decreased Apo-B 100 function of expression?
What is the best treatment for an ApoB-100 defect?
Bile acid binding resins
List the Fibrates.
What is the mechanism of action of the Fibrates?
List the bile acid binding resins.
What is the mechanism of action of Niacin?
Inhibition of adipocyte hormone sensitive lipase
List the statins.
What are the indications for Quinidine?
- Life threatening ventricular arrhythmia
What are the indications for Procainamide?
1) Re-entry SVT
3) A-flutter with WPW
4) Life threatening ventricular arrhythmia
What are the indications for Lidocaine?
- Post MI arrhythmia
- Digitalis induced arrhythmia
What are the indications for Propafenone?
2) Atrial arrhythmia
3) Ventricular arrhythmia in patients WITHOUT heart disease
What are the indications for Amiodarone?
1) Acute conversion of VT or VF
What are the indications for Verapamil?
2) A-fib with RVR
What are the contraindications to Verapamil?
- Conduction block
- WPW + a-fib
- Ventricular Tachycardia
What are the adverse effects seen with Adenosine administration?
1) Bradycardia/ heart block
4) Hypotension (A2 mediated vasodilation)
What are the indications for Acetazolamide?
2) Acute Mountain Sickness
3) Urinary Alkalization
What are the adverse effects of Acetazolamide?
- Hyperchloremic metabolic acidosis
- Renal stones
- Renal K+ loss
What are the contraindications for Acetazolamide?
What are the indications for osmotic diuretics?
1) Prophylaxis for acute renal failure
2) Cerebral edema
3) Dialysis disequilibrium
4) Acute glaucoma
What are the adverse effects of osmotic diuretics?
- Pulmonary edema
List the loop diuretics.
What are the indications for loop diuretics?
1) Pulmonary edema
3) Acute renal failure
What are the adverse effects of the loop diuretics?
- Hypokalemia, natremia, calcemia, magnesia
List the Thiazide diuretics?
What is unique about the Thiazide diuretics in terms of ion secretion/ absorption?
Stimulation of PTH causes Ca++ REABSORPTION
What are the indications for Thiazide diuretics?
Hypercalciuria/ renal stones
Nephrogenic DM Insipidus
List the K+ sparing diuretics.
What is the MOA of K+ diuretics?
Block epithelial Na+ channels on principal cells; thus, K+ is NOT secreted
What are the indications for the K+ diuretics?
- Hypokalemic alkalosis
- Combination therapy to prevent hypokalemia
List the Aldosterone antagonists.
What are the indications for Aldosterone antagonists?
4) Primary or secondary hyperaldosteronism
What are the adverse effects of the aldosterone antagonists?
- Metabolic acidosis in cirrhosis
- Hormonal effects (gynecomastia, impotence...etc.)
What are the contraindications for ACE inhibitors?
2) Bilateral renal artery stenosis
Under what circumstances will ACE inhibitors have an increase in favorable effects?
- Low K+ or hypokalemia
Under what circumstances will ACE inhibitors have an unfavorable effects?
- High K+ or hyperkalemia
- Volume depletion
What are the adverse effects of ACE inhibitors?
P= potassium (increased)
T= taste change
P= pregnancy--> fetopathic
List the ACE inhibitors.
What are the contraindications for ARB therapy?
Bilateral renal artery stenosis
List the ARBs.
What is the role of DHP Ca++ blockers in HTN?
1) First line or add on therapy for uncomplicated
2) Add on therapy for DM and CAD
When should DHP Ca++ blockers be avoided?
List the DHP Ca++ blockers used in anti-HTN therapy.
Under what circumstances can DHP Ca++ therapy have increased favorable effects?
1) Reynaud Syndrome
2) Elderly patient with isolated systolic HTN
3) Cyclosporine induced HTN
Under what circumstances can DHP Ca++ therapy unfavorable effects?
- Peripheral edema
What is the role of NDPH Ca++ blockers in HTN?
1) First line or add on for uncomplicated HTN
2) Add on for DM
3) Alternative to Beta-blockers in CAD
****These drugs will DECREASE myocardial oxygen consumption*****
When should NDHP Ca++ blockers be avoided?
- AV block
- LV dysfunction
Under what circumstances can NDHP Ca++ therapy have increased favorable effects?
1) Reynaud Syndrome
Under what circumstances can NDHP Ca++ therapy unfavorable effects?
- Peripheral edema
- AV block
When are Thiazide diuretics first-line therapy in HTN?
1) LV dysfunction
2) S/p CVA
When should Thiazide diuretics be avoided?
1) Allergy to Sulfa
5) Pre-DM/ elevated fasting glucose
What comorbid conditions should Thiazide diuretics be used in, if a patient has HTN?
- Osteoporosis b/c of increased Ca++ reabsorption
- Hyperkalemia b/c of K+ excretion
When are Beta blockers first line therapy for patients with HTN?
CAD and LV dysfunction
Are aldosterone antagonists first line therapy or add on therapy?
Add on therapy
What situations should aldosterone antagonists be used as add on therapy?
In addition to their normal use, when is aldosterone antagonist therapy beneficial?
What is the role of alpha-1 antagonists in HTN therapy?
- Used in conjunction w/ diuretics
- Lower cholesterol and trigylcerides
List the central alpha 2 agonists.
What adverse effects are seen with alpha-methyldopa?
2) Positive direct coombs test
What is the mechanism of action of Hydralazine?
- Arterial vasodilation by blocking IP3 induced Ca++ release
- Opens K+ channels to hyperpolarize vascular smooth muscle
What is the role of Hydralazine in HTN therapy?
- Add on for resistant HTN esp. in CKD
- SAFE in pregnancy