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359 Cards in this Set

  • Front
  • Back
List 3 dysfunctions of blood
Thrombosis
bleeding
anemia
What is the most common abnormality of hemostasis
Thrombosis
Name 4 thrombotic disorders
Acute MI
DVT
PE
Acute ischemic stroke
What class of drugs treat thrombotic disorders
Anticoagulants
Fibrinolytics
Name 2 bleeding disorders involving failure of hemostasis
Hemophilia
Vitamin K deficiency
How is hemophilia treated
Factor VIII transfusion
How is Vit K deficiency treated
Dietary supplements of the vitamin
A clot that adheres to a vessel wall is called ____
Thrombus
Intravascular clot that floats in the blood is termed ____
Embolus
T or F: Arterial thrombosis occurs in medium-sized vessels rendered thrombogenic by surface lesions of endothelial cells caused by atherosclerosis.
True
Does arterial or venous thrombosis consist of platelet rich clot
Arterial
T or F: Venous thrombosis is triggered by blood stasis or inappropriate activation of the coagulation cascade
True
Does venous or arterial thrombosis typically involves a clot that is rich in fibrin, with fewer platelets
Venous
What chemical mediators are synthesized by intact endothelial cells and act as inhibitors of platelet aggreation
Prostacyclin and Nitric Oxide
T or F: Damaged endothelial cells synthesize more prostacyclin
False: Less
T or F: Platelet membrane contains receptors that can bind thrombin, thromboxanes, and exposed collagen
True
In intact, normal vessel, are circulating levels of thrombin and thromboxane low or high
Low
T or F: Endothelium covers the collagen in the subendothelial layers and the platelet receptors are thus unoccupied and remain inactive
True
T or F: When platelet receptors are occupied, each of these receptor types triggers a series of reactions leading to the release into the circulation of intracellular granules by the platelets. This ultimately stimulates platelet aggregation
True
T or F: When endothelium is injured, platelets adhere to and virtually cover the exposed collagen of the subendothelium. this triggers a complex series of chemical rxns resulting in platelet activation
True
During platelet activation, receptors on the surface of the adhering platelets are activated by what?
Collagen of the underlying connective tissue
When platelets go through morphologic changes, what chemical mediators do they release which ultimately bind to receptors of the resting platelets
Adenosine diphoshate (ADP)
Thromboxane A2
Serotonin
Platelet-activation factor
Thrombin
T or F: activation of IIb/IIIa receptors that bind fibrinogen regulate platelet-platelet interaction and thrombus formation
True
What substance simultaneously binds to GP IIb/IIIa receptors on two separate platelets, resulting in platelet cross-linking and platelet aggregation
Fibrinogen
Local stimulation of the coagulation cascade by tissue factors released from the injured tissue and by mediators on the surface of platelets results in formation of what?
Thrombin
Thrombin catalyzes the hydrolysis of ____ to ____, which is incorporated into the plug
Fibrinogen to fibrin
T or F: Cross-linking of the fibrin strands stabilizes the clot and forms a hemostatic platelt-fibrin plug
True
What substance limits the growth of a clot, dissolving the fibrin network as wounds heal
Plasmin
T or F: The last step in the response to vascular trauma depends on a family of membrane GP receptors
True
What is the most GP receptors that regulates platelet-platelet interaction and thrombus formation
IIb/IIIa receptor
What platelet activation agents promote the conformational change necessary for the GP IIb/IIIa receptor to bind ligands, particularly fibrinogen
Thromboxane A2
ADP
Thrombin
Serotonin
Collagen
T or F: Fibrinogen simultaneously binds to GP IIb/IIIa receptors on two separate platelets, resulting in platelet cross-linking and aggregation.
True
Platelet aggregation inhibitors inhibit what 3 receptors, interfering in the signals that promote platelet aggregation
COX-1
GP IIb/IIIa
ADP
Stimulation of platelets by thrombin, collagen and ADP results in activation of platelet membrane phospholipase that liberate what substance
arachidonic acid
Arachidonic acid is first converted to what prostaglandin by COX-1
H2
Prostaglandin H2 is further metabolized to what substance
Thromboxane A2
T or F: Thromboxane A2 produced by the aggregating platelets further promotes the clumping process essential to the formation of a hemostatic plug
True
What drug inhibits thromboxane A2 synthesis from arachidonic acid in platelets by irreversible acetylation of COX-1
Aspirin
Aspirin-induced suppression of thromboxane A2 synthetase results in suppression of platelet aggregation, which lasts for how long?
Life of platelet: 7-10 days
What drug is used as prophylactic tx of transient cerebral ischemia, recurrent MI, and pre and post-MI pts
Aspirin
What is the recommended daily dose of ASA
81-165 mg
Bleeding time is prolonged by ASA tx, this causes an increased incidence of what?
Hemorrhagic stroke and GI bleed, esp in higher doses
What drug, if taken concominantly, can antagonize the platelet inhibition by aspirin
Ibuprofen
T or F: Selective COX-2 inhibitors may contribute to CV events by shifting the balance of chemical mediators in favor of thromboxane A2
True
What 2 drugs block platelet aggregation by interfering with the binding of ADP to its receptors on platelets, thus inhibiting the activation of GP IIb/IIIa receptors
Ticlopidine and Clopidogrel
What two drugs have been effective in preventing cerebrovascular, cardiovascular, and peripheral vascular disease, which are used in stent insertion during an MI
Ticlopidine and Clopidogrel
Most serious adverse effect of ticlopidine
Neutropenia
T or F; Key role of platelet GP IIb/IIIa receptor is platelet aggregation
True
By binding to GP IIb/IIIa, this antibody blocks the binding of fibrinogen, inhibiting aggregation
Abciximab
Through what route is Abciximab administered as an adjunct to percutaneous coronary intervention
IV
What is the mechanism of action of Eptifibatide and tirofiban
blocking the GP IIb/IIIa receptor
T or F: when intravenous infusion is stopped, Eptifibatide and tirofiban are slowly cleared from the plasma
False: rapidly
Is Dipyridamole a vasoconstrictor or a vasodilator
Vasodilator
Dipyridamole is a prophylactic drug used in treating what condition
Angina Pectoris
Dipyridamole results in decreased levels of what molecule
Thromboxane A2
Does the intrinsic, extrinsic, or both systems produce Factor Xa, which converts prothrombin to thrombin
Both
Thrombin is responsible for the generation of what glycoprotein, which is responsible for mesh-like matrix of the blood clot
Fibrin
T or F: If thrombin is not formed or if its function is impeded, coagulation is inhibited
True
Does Heparin or Warfarin inhibit the action of coagulation factors
Heparin
Does heparin or warfarin interfere with the synthesis of the coagulation factors
Warfarin
What drug is used acutely to interfere with the formation of thrombi
Heparin
T or F: unfractionated heparin has a wide range of molecular weights
True
Heparin is used in the prevention of what diseases
venous thrombosis, PE, and MI
What drug is used prophylactically to prevent post-op venous thrombosis in pts having hip replacement and in acute MI
Heparin
What drug is used in extracorporeal devices, such as dialysis machines, to prevent thrombosis
Heparin
What drugs are anticoagulants of choice in pregnant women w/ prosthetic heart valves or venous thromboembolism
Heparin and LMWH
Why is Heparin the DOC for anticoagulation in pregnant women
It doesn't cross the placenta
LMWH, such as Enoxaparin and Dalteparin can be administered through what route, making them useful in outpatient therapy
Sub q
Why is IM administration of LMWH contraindicated
because of hematoma formation
What is the dosage recommendations for Heparin
Bolus IV, followed by continuous infusion for 7-10 days
When administering continuous infusion of heparin, how should you titrate the dose
so that PTT is 1.5 - 2.5 fold the normal
Is it necessary to obtain the same index of PTT in LMWH
No
Are thromboembolic problems less common with LMWH or Heparin
LMWH
What is the chief complication of heparin therapy
Hemorrhage
How is heparin reversed
Protamine sulfate
Heparin preparations are from animal sources and may have the following adverse reactions
Urticaria and anaphylactic shock
T or F: Thrombocytopenia is a common abnormality among hospital pts
True
What type of heparin-induced thrombocytopenia (HIT) is common, not serious, mild decrease in platelet number
Type I
When does Type I HIT occurs
Within the first 5 days of treatment
What dangerous effect does Type II HIT produce
Platelet aggregation which can result in thrombocytopenia and thrombosis
When does Type II HIT occur
Between 5-14 days of treatment
Type 2 HIT can have a platelet drop up to what %?
50%
Is Type I or II HIT relatively rare
Type II
When Type II HIT occurs, heparin tx should be discountinued and replaced with what other anticoagulant
Lepirudin
Heparin is contraindicated in pts with a hx of the following surgeries
Brain, eye, or spinal cord
T or F: Heparin is contraindicated for pts who have bleeding disorders and alcoholics
True
What drug is a direct thrombin antagonist related to hirudin - a thrombin inhibitor from the leech
Lepirudin
T or F: One molecule of lepirudin binds to one molecule of thrombin, resulting in blockade of the thrombogenic activity of thrombin
True
T or F: Lepirudin has large effect on platelet aggregation
False: little effect
T or F: IV Lepirudin is effective in the treatment of HIT, it can prevent further thromboembolic complications
True
What is the major adverse effect of Lepirudin
Bleeding
T or F: Bleeding from Lepirudin can be exacerbated by concomitant thrombolytic tx, w/ streptokinase or alteplase
True
This drug's anti-Factor Xa activity far exceeds its antithrombin activity and is administered sub q
Danaparoid
Danaparoid is effective in what type of HIT
Type II
T or F: Even careful monitoring to keep the PT time at 1.5-2.5 fold longer than normal does not prevent bleeding complications in about 20% of pts taking Warfarin
True
What cofactor do Factors II, VII, IX, and X require for their synthesis by the liver
Vitamin K
What enzyme is inhibited by warfarin
Vitamin K epoxide reductase
Effects of warfarin can be overcome by the administration of what?
Vitamin K
How long does the reversal of warfarin w/ Vit K take
24 hrs
Thrombolytic agents all act to convert ____ to ____
Plasminogen to plasmin
Plasmin is a protease that hydrolyzes ____ and thus dissolves clots
Fibrin
What 2 thrombolytic drugs are unsuccessful about 20 % of the time
Alteplase and Streptokinse
T or F: Clots become resistant to lysis as they age
True
For MI, where is the delivery of thrombolytic agents most reliable in terms of achieving recanalization, but may not be possible in the 2-6 hr "therapeutic window"
Intracoronary
If intracoronary administration of thromboylitcs is not possible, which route is used
IV
What is a major side effect of thrombolytics
Hemorrhage
T or F: Unsuspected lesion such as peptic ulcer may hemorrhage if given thrombolytic tx
True
What are contraindications for thrombolytic agents
Healing wounds
pregnancy
cerebrovascular accident
Mets
What drug has low affinity for free plasminogen in the plasma, but it rapidly activates plasminogen that is bound to fibrin in a thrombus or a hemostatic plug
Alteplase
This drug is said to be "fibrin selective"
Alteplase
What drug acts on free plasminogen and induces a general fibrinolytic state
Streptokinase
Is alteplase or streptokinase superior in dissolving older clots
Alteplase
what drug, when administered w/in 3 hrs of an ischemic stroke significantly improves clinical outcome
Alteplase
What are adverse effects of Alteplase
GI and Cerebral hemorrhage
What drug is a protein purified from culture broths of Group C Beta hemolytic streptococci
Streptokinase
T or F: Streptokinase works by hydrolyzing fibrin plugs and catalyzing degradation of fibrinogen
True
Streptokinase is approved for use in what conditions
Acute PE
DVT
acute MI
Arterial thrombosis
Streptokinase is instituted within how many hours of an MI
4
On discontinuation of streptokinase tx, what drugs may be administered
Heparin or oral anticoagulants
Streptokinase may precipitate bleeding. In the rare instance of life-threatening hemorrhage, what can be administered?
Aminocaproic acid
What needs to be done to prevent potential therapeutic failure of streptokinase
Need sufficient quantities of it to overwhelm the antibodies that may have accumulated in inds who have had a streptococcal infections
Hemophilia is a consequence of a deficiency of what factors
VIII and IX
Concentrations of factors VIII and IX are available from human donors, but they carry what risk
Transferring viral infections
Fibrinolytic states can be controlled by what synthetic agent which inhibits plasminogen activation
Aminocaproic acid
This agent antagonizes the anticoagulant effects of heparin
Protamine sulfate
T or F: Positively charged protamine interacts with the negatively charged heparin, forming a stable complex w/o anticoagulant activity
True
What is another name for vitamin K
Phytonadione
The response to Vitamin K is slow, requiring 24 hrs. If immediate hemostasis is required, what should be used instead
Fresh frozen plasma
This agent stops bleeding by blocking plasmin. It is approved for prophylactic use to reduce perioperative blood loss in pts undergoing bypass surgery
Aprotinin
Iron is stored in intestinal mucosal cells as ____
Ferritin
A negative iron balance produces what type of anemia
Hypochromic microcytic
Supplementation with what substance is required to correct iron deficiency
Ferrous sulfate
What are the most common adverse effects of iron supplements
GI disturbance
What is a primary result of folic acid deficinecy
Megaloblastic anemia
What are the causes of folate deficiency
Increased demand (pregnancy)
Poor absorption
Alcoholism
Dihydrofolate reductase inhibitors
Name 2 dihydrofolate reductase inhibitors
Methotrexate
Trimethoprim
What are 2 causes of vit B12 deficiency
low dietary levels or
poor absorption
What causes poor absorption of vit B12
failure of gastric parietal cells to produce intrinsic factor
Failure to produce intrinsic factor results in what type of anemia
Pernicious
T or F: malabsorption syndromes or gastric resection can cause vit B12 deficiency
True
For dietary deficiency of vit B12, how should it be administered
Orally
How should vit B12 be administered for pernicious anemia
IM or Sub q
T or F: Folic acid alone reverses the hematologic abnormality and masks the B12 deficiency, which can then proceed to severe neurologic dysfunction
True
For a pt suffering from pernicious anemia, how long should tx be administered
for life
What glycoprotein is made by the kidney, regulate red cell proliferation and differentiation in bone marrow
Erythropoietin
Human erythropoietin is effective in the treatment of anemia caused by what disease
End-stage renal disease
What other supplement may be required for adequate response in tx of ESRD
Iron
What drug has been shown to relieve the painful clinical course of sickle-cell disease
Hydroxyurea
T or F: In sickle-cell disease, hydroxyurea increases fetal Hgb levels, thus diluting the abnormal HgbS
True
T or F: Polymerization of HgbS is delayed in treated pts, so that painful crises are not caused by sickled cells blocking capillaries and causing tissue hypoxia
True
What corticosteroid has excellent antiemetic properties
Dexamethasone
What are 3 major causative factors of PUD
H. pylori
Increased HCl secretion
Inadequate mucosal defense
Optimal tx for pts w/ PUD who are infected w/ H. Pylori requires what type of treatment
Antimicrobial
What tests are used to diagnoise H. pylori infection
Endoscopic bx of gastric mucosa
Serologic tests
Breath tests for urea
T or F: Eradication of H. pylori results in rapid healing of active peptic ulcers and low recurrence rates
True
What is the typical triple tx of PUD
PPI w/ either Metronidazole or amoxicillin plus clarithromycin
What is the typical quadruple tx of PUD
Bismuth subsalicylate and metronidazole plus tetracycline plus H2 receptor blocker or a PPI
How long are the triple and quadruple therapies for PUD administered
2 weeks
How do Bismuth salts work
increase the secretion of mucus
Does GERD respond to antibiotic tx? Why or why not
No, b/c it is not associated w/ H. pylori
Gastric acid secretion by parietal cells is stimulated by what 3 factors
Acetylcholine
Histamine
Gastrin
What 2 factors diminish gastric acid production
Prostaglandin E2
Somatostatin
What drugs are particularly effective aganst nocturnal acid secretion
H2 receptor antagonists
Name four H2 receptor antagonists used in US that inhibit basal, food-stimulated, and nocturnal secretion of gastric acid
Cimetidine
Ranitidine
Nizatidine
Famotidine
Do H2 receptor antagonists effect H1 receptors
No
T or F: H2 receptor antagonists completely inhibit gastric acid secretion induced by histamine or gastrin; however, they only partially inhibit gastric acid secretion induced by Acetylcholine
True
T or F: The therapeutic use of H2 antagonists has increased with the advent of PPIs
False: decreased
What H2 antagonists are equally effective in promoting healing of duodenal gastric ulcers, but whose recurrence is common after treatment is stopped
Cimetidine
Ranitidine
Nizatidine
Famotidine
T or F: Low dose of H2 antagonists are effective for prevention and tx of heartburn; however, about 50% pf pts do not find benefit and PPIs are now used preferentially
True
H2 receptor antagonists act by stopping acid secretion, but they may not relieve symptoms for how long
At least 45 minutes
How do antacids work
They neutralize secreted acid already in the stomach, but their effects are shorter lasting
What H2 antagonist is inactivated by the liver's microsomal mixed-function oxygenase system and can interfere in the metabolism of many other drugs
Cimetidine
Which drug is longer lasting, Cimetidine or Ranitidine
Ranitidine
Nizatidine is eliminated principally by what route?
By the kidney
What H2 antagonist has endocrine effects such as gynecomastia, galactorrhea, and reduced sperm count
Cimetidine
What H2 antagonist inhibits cytochrome P450 and can slow metabolism, thus potentiating the action of drugs like warfarin
Cimetidine
Except ____, all H2 antagonists inhibit the gastric first-pass metabolism of ethanol
Famotidine
T or F: Drugs such as ketoconazole which depend on an acidic medium for gastric absorption, will not be efficiently absorbed if taken with one of the H2 antagonists.
True
This drug binds to the proton pump of the parietal cell, thereby suppressing secretion of hydrogen ions into the gastric lumen
Omeprazole
Name 4 PPIs that are now available, in addition to Omeprazole
Pantoprazole
Esomeprazole
Rabeprazole
Lansoprazole
T or F: all PPIs inhibit both basal and stimulated gastric acid secretion more than 90%.
True
Acid suppression begins within how many hrs of PPI administration
1-2
what are DOC for tx of erosive esophagitis, active duodenal ulcer, GERD and hypersecretory conditions such as Zollinger-Ellison syndrome
PPIs
These drugs reduce the risk of bleeding from an ulcer caused by ASA and other NSAIDS
PPI's
This PPI interferes in the oxidation of warfarin
Omeprazole
T or F: Drug interactions are a big problem with PPIs
False: not a problem, except for omeprazole
Prolonged tx w/ PPIs and H2 antagonists may result in this deficiency
Vitamin B12
This substance is produced by the gastric mucosa, inhibits secretion of HCL and stimulates secretion of mucus and bicarb (cytoprotective effect)
Prostaglandin E2
Deficiency of prostaglandins is thought to be involved in the pathogenesis of what disease
Peptic ulcers
Name the drug that is an analog of prostaglandin E1, that has cytoprotective actions
Misoprostol
Routine prophylactic use of misoprostol is justified in what pts
Those taking NSAIDS and are at high risk of NSAID induced ulcers, such as the elderly
Like other prostaglandins, misoprostol produces uterine contractions and is contraindicated in whom?
Pregnant women
These drugs are weak bases that react with gastric acid and may have other actions such as reduction of H. pylori colonization and stimulation of prostaglandin synthesis
Antacids
Name 3 commonly used antacids
aluminum hydroxide
magnesium hydroxide
calcium carbonate
Systemic absorption of the following antacid can produce transient metabolic alkalosis, it is not recommended for long term use
Sodium bicarbonate
Calcium carbonate preparations are also used as calcium supplements for the treatment of this disease
Osteoporosis
Which antacid may be constipating
Aluminum hydroxide
Which antacid may produce diarrhea
Magnesium hydroxide
Preparations that combine which 2 antacids aid in normalizing bowel function
Aluminum hydroxide and
Magnesium hydroxide
____ content of antacids is an important consideration in pts w/ HTN or CHF
Sodium
By forming complex gels w/ epithelial cells, this mucosal protective agent creates a physical barrier that impairs diffusion of HCL and prevents degradation of mucus by pepsin and acid
Sucralfate
T or F: Sucralfate stimulates prostaglandin release as well as mucus and bicarb output, thereby effectively healing duodenal ulcers
True
This mucosal protective agent heals peptic ulcers, increase secretion of mucus, and coat and protect the ulcer crater
Colloidal bismuth
What side effects of chemo demand effective management
Nausea and vomiting
Who is more susceptible to nausea and vomiting
Young and women more than older pts and men
Uncontrolled vomiting can produce what side effects
Dehydration
Metabolic imbalances
Nutrient depletion
The chemoreceptor trigger zone is located where in the brainstem?
Area postrema at the caudal end of the 4th ventricle, outside the blood-brain barrier
Where is the vomiting center located
lateral reticular formation of the medulla
What does the vomiting center do
coordinates the motor mechanisms of vomiting
The vomiting center also responds to afferent input from this system
vestibular
The vestibular system functions mainly in this condition
Motion sickness
What 2 chemoreceptors play critical roles in the vomiting center activation
Dopamine receptor type 2
5-HT3
Name an anticholinergic, antiemetic drug
Scopolamine
Name 2 H1 antagonist, antiemetic drugs that are useful in motion sickness but are ineffective against substances that act directly on the chemoreceptor trigger zone
Dimenhydrinate
Meclizine
Prochlorperazine belongs to what class of drugs
Phenothiazines
This drug acts by blocking dopamine receptors, and is effective against low or moderately emetogenic chemotherapeutic agents
Prochlorperazine (phenothiazines)
What is an adverse reaction of Prochlorperazine (phenothiazines)
Extrapyramidal sx
Ondansetron and Granisetron belong to this group of drugs
5-HT3 receptor antagonists
Where in the body do 5-HT3 receptor antagonists work
Periphery (visceral vagal afferent fibers)
Brain (chemoreceptor trigger zone)
T or F: 5-HT3 antagonists have a short duration of action and are cheap
False: long duration and are costly
This drug belongs to the substituted benzamides class
Metoclopramide
T or F: Metoclopramide has antidopaminergic side effects such as extrapyramidal sx
True
name 2 drugs that belong to the Butyrophenones class and act by blocking dopamine receptors
Droperiodol
Domperidone
Lorazepam belongs to what class of drugs
Benzodiazepines
Name the drug whose beneficial effects are due to its sedative, anxiolytic, and amnesic properties. It's useful in treating anticipatory vomiting
Lorazepam (benzodiazepine)
These 2 corticosteroids are effective against mildly to moderately emetogenic chemotherapy. Most frequently, they are used in combination w/ other agents
Dexamethasone and methylprednisolone
what is a potential side effect of corticosteroids
Insomnia and hyperglycemia in pts w/ DM
Dronabinol belongs to what class of drugs, it's seldom used as a first-line antiemetic
Cannabinoids (marijuana derivatives)
Dexamethasone increases its antiemetic activity when given with this 5-HT3 antagonist
Metoclopramide
This antihistamine is administered w/ metoclopramide to reduce extrapyramidal reactions
Diphenhydramine
Increased motility of the GI tract and decreased absorption of fluid are major factors in this condition
Diarrhea
What two antimotility agents are widey used to control diarrhea
Diphenoxylate
Loperamide
T or F: dephenoxylate and loperamide have opioid-like actions on the gut, inhibit acetylcholine release, and decrease peristalsis
True
Diphenoxylate and loperamide can cause what side effect
Toxic megacolon
These adsorbents act by adsorbing intestinal toxins or microorganisms/coating or protecting the intestinal mucosa.
Kaolin
Pectin
Methylcellulose
Are antimotility agents or adsorbents more effective
Antimotility agents
Bismuth subsalicylate is used for this type of diarrhea
Traveler's
T or F: NSAIDS, such as ASA and indomethacin are effective in controlling diarrhea
True
This irritant is a laxative that increases peristalsis
Castor oil
These 2 irritants stimulate colonic activity
cascara and Senna
Bisacodyl belongs to this class of laxatives
Stimulant of the colon
Hydrophilic colloids belong to this class of laxatives
bulking agents
These drugs form gels in the large intestine causing water retention and intestinal distention, thereby increasing peristaltic activity
Bulking agents
Methylcellulose and bran have similar actions to this bulking agent
hydrophilic colloids
These drugs are nonabsorbable salts that hold water in the intestine by osmosis
Saline cathartics
This drug is a semisynthetic disaccharide that also acts as an osmotic laxative
Lactulose
Name 3 stool softeners that when emulsified with the stool, produce softer feces and ease passage
Docusate sodium
Mineral oil
Glycerin suppositories
What % of pts on chemotx will achieve a cure or prolonged remission
10%
What is the overall 5yr survival rate for CA pts
40%
T or F: CA chemotx acts to cause a lethal cytotoxic event in the cancer cell. This attack is generally directed against metabolic sites essential to cell replication
True
T or F: Ideally, anticancer drugs should interfere only with cellular processes that are unique to malignant cells
True
T or F: most currently available chemo drugs work only against malignant cells
False: against all proliferating cells
T or F: in CA treatment, the neoplastic cell burden is initially debulked either by surgery or radiation
True
When is chemo indicataed
When neoplasms are disseminated and are not amenable to surgery
What cell characteristic influences their susceptibility to chemotx
Growth factor
Are rapidly dividing cells more or less susceptible to chemotx
More
chemotx agents that are only effective against replicating cells are said to be...
cell-cycle specific
Are cell-cycle specific or nonspecific drugs useful against tumors that have low percentage of replicating cells
Nonspecific
Is the growth rate of most solid tumors initially slow or rapid
Rapid
T or F: growth rate increases as the tumor size gets bigger
False: decreases
T or F: reducing the tumor burden through surgery or radiation promotes the recruitment of the remaining cells into active proliferation and increases their susceptibility to chemotx agents
True
This is the term used to describe a given dose of a drug that destroys a constant fraction of cells
log kill
For most bacterial infx, what # of log reductions results in a cure
5-log
T or F: immune cells can destroy the remaining bacterial cells; however, the tumor cells are not as readily eliminated
True
is a single or a combination of chemo drugs more effective
Combo
What are 3 advantages of combination therapy
1. maximal cell killing within the range of tolerated toxicity
2. effective against a broader range of cell lines
3. Delay or prevent the development of resistant cell lines
Does melanoma have inherent or acquired resistance to anticancer drugs
Inherent
T or F: some tumor types acquire resistance by mutating, esp after prolonged administration of low-dose drugs
True
How is chemo drug resistance minimized
By short-term, intensive, intermittant therapy with combinations of drugs
Therapy aimed at killing rapidly dividing cells also affects normal cells undergoing rapid proliferation, such as:
Buccal mucosa
Bone marrow
GI mucosa
Hair
T or F: Most chemotx drugs have a narrow therapeutic index
True
What side effects, to a greater or lesser extent, are seen with all antineoplastic drugs
Vomiting
Stomatitis
Alopecia
T or F: myelosuppression predisposes to infection are common to many chemotx drugs
True
What adverse reaction is seen with doxorubicin
Cardiotoxicity
What adverse reaction is seen with bleomycin
pulmonary fibrosis
T or F: Some toxic reactions may be ameliorated by perfusing the tumor locally, removing some of the pt's marrow prior to intensive tx and then reimplanting it, or intenstive diuresis to prevent bladder toxicities
True
Megaloblastic anemia that occurs with this drug ___ can be counteracted by administering ____
Methotrexate
folinic acid (leucovorin)
What drug is the human granulocyte stimulating factor
Filgrastim
What drug can partially reverse neutropenia caused by chemo drugs
Filgrastim
T or F: Antineoplastic agents are mutagens, neoplasms may arise 10 or more yrs after the original cancer was cured
True
Treatment induced neoplasia are esp a problem with these agents
Alkylating
This class of drugs is structurally related to normal compounds within the cell. They generally interfere with the availability of normal purine or pyrimidine nucleotide precursors either by inhibiting their synthesis, or by competing with them in DNA or RNA synthesis
Antimetabolites
Methotrexate belongs to what class of drugs
Antimetabolites
This drug is teratogenic and is an abortifacient, should be avoided in pregnancy
Methotrexate
This class of drugs owes its cytotoxic action to its interaction with DNA, leading to disruption of DNA function
Antibiotics
What drug is one of the most important and widely used anticancer drugs
Doxorubicin
What is an adverse side effect of doxorubicin
Irreversible, dose-dependent cardiotoxicity
Irreversible, dose dependent cardiotoxicity is more common in these two antibiotics
Daunorubicin
Doxorubicin
What is the most serious adverse effect of Bleomycin
Pulmonary toxicity: progressing from rales, cough, and infiltrate to potentially fatal fibrosis
These drugs exert their cytotoxic activity by covalently binding to nucleophilic groups on various cell constituents
Alkylating agents
what is the most commonly used alkylating agent
Cyclophosphamide
Carmustine belongs to what class of drugs
Nitrosureas
Because of their ability to penetrate the CNS, nitrosureas are used primary in the treatment of ____
Brain tumors
Where are microtubule inhibitors derived from
Plants
Name 2 microtubule inhibitors
Vincristine
Vinblastine
This chemo drug has shown good activity against advanced ovarian cancer and metastatic breast cancer
Paclitaxel (taxol)
This drug shows impressive benefits with fewer side effects
Docetaxel
This is a potent, anti-inflammatory corticosteroid with less mineralcorticoid activity than cortisol
Prednisone
This drug is used primarily to induce remission in pts with acute lymphocytic leukemia and in the treatment of Hodgkins and non-Hodgkins lymphoma
Prednisone
This drug can predispose to infx, hyperglycemia, cataract formation, osteoporosis, and change in mood (euphoria or psychosis)
Prednisone
These two drugs are analogs of GnRH and occupy the GnRH receptor in the pituitary which leads to desensitization, and inhibition of release of FSH and LH. Thus, both androgen and estrogen synthesis are reduced
Leuprolide and Goserelin
Response to this drug in prostatic cancer is equivalent to that of orchiectomy
Leuprolide
These drugs have some benefit in pre-menopausal women with advanced breast cancer
Leuprolide and Goserelin
T or F: with the use of GnRH analogs, levels of androgen may initially rise but then fall to castration levels
True
This drug is synthetic, nonsteroidal antiandrogen, used in the treatment of prostate cancer. It competes with the natural hormone for binding to the androgen receptor
Flutamide
T or F: introduction of an allograft can illilcit a damaging immune respone - rejection
True
Earlier immunosuppressive drugs were nonselective, and pts frequently succumbed to infection due to suppression of what part of the immune system
Humoral (antibody mediated)
Cell mediated
Today, the principal approach to immunosuppressive tx is to alter the function of ____ using antibodies against immune proteins
lymphocyte
Name the 3 mechanisms of action by which immunosuppressive drugs are categorized
1. interfere w/ cytokine production
2. disrupt cell metabolism, preventing lymphocyte proliferation
3. mono-and polyclonal antibodies block T cell surface molecules
T or F: Immunosuppresive tx is used in treatment of autoimmune disease
True
What is the name of signaling proteins that bind to cell surface receptors
Cytokines
What molecules are considered cytokines
Interleukins
Interferons
TNFs
Transforming growth factors
Colony-stimulating factors
Which cytokine stimulates proliferation of helper T cell
IL-2
What molecules do helper T cells produce, which in turn activate NK cells, macrophages, and cytotoxic T lymphocytes
IL-2
IFN gamma
TNF-beta
T or F: drugs that interfere with production or activity of IL-2 will significantly dampen the immune response
True
Cyclosporine can be used alone, but is more effective when what other drugs are administered
Glucocorticoids
Cyclosporine is an alternative to what drug for the treatment of severe, active rheumatoid arthritis, and recalcitrant psoriasis
Methotrexate
Cyclosporine preferentially suppresses cell mediated or humoral reactions?
Cell mediated
What is the end result of cell mediated suppression with cyclosporine
decreased IL-2
T or F: Infections in pts taking cyclosporine are common and may be life-threatening
True
What type of infections are prevalent in pts taking cyclosporine (CsA)
Viral infx due to herpes and CMV
An ointment preparation of cyclosporine has been approved for what condition
Atopic dermatitis
This macrolide is approved for use in renal transplantation
Sirolimus (SRL)
What drug coats stents, ultimately inhibiting restenosis of the blood vessels by reducing proliferation of endothelial cells
Sirolimus (SRL)
T or F: SRL inhibits proliferation of cells in the graft intimal areas and is effective in halting graft vascular disease
True
Antimetabolite agents are usually used in combination with what other drugs
Glucocorticoids
What drug has been the cornerstone of immunosuppressive therapy during the last several decades
Azathioprene
What cells are predominantly affected by cytotoxic effects of azathioprene
Lymphocytes
What is azathioprene's major non-immune toxicity
Bone marrow suppression
Azathioprene is being replaced by what drug
Mycophenolate Mofetil
T or F: Mofetil, like 6-MP, deprives the proliferating T and B cells of a key component of nucleic acids
True
These compounds are prepared either by immunization of rabbits or horses with human lymphoid cells (producing a mixture of polyclonal antibodies directed against a number of lymphocyte antigens)
Antibodies
What drugs were the first pharmacologic agents to be used as immunosuppressive in transplantation and in various autoimmune disorders
Glucocorticoids
These drugs are the mainstay for attenuating rejection episodes
Glucocorticoids
What are the most common agents for transplantation
Prednisone
Methylprednisone
What drugs are employed for autoimmune conditions
Prednisone
Prednisolone
Glucocorticoids mostly affect these cells
T cells
T or F: steroids rapidly reduce lymphocyte populations by lysis or redistribution
True
T or F: efforts are being made to reduce or eliminate the use of steroids in the maintanance of allografts
True
What method of GERD dx is superior to endoscopy
2 week course of PPI. This offers sensitivity and specificity equivalent to pH monitoring
T or F: doses of H-2 blocking agents may have to be doubled to be effective
True
Should PPIs be taken before or after meals
Before, to stimulate activation of proton pumps
What 2 anti-diarrheals are used for symptomatic tx of IBD
Loperamide
Diphenoxylate
This drug is most useful in maintaining remissons of Crohn's and UC
Sulfasalazine
This drug is used in rectal or left sided disease, it's 5ASA coated in Eudragit resin
Mesalamine
This drug is effective in 1st 12 weeks of acute UC
Balsalazide
What antibiotic is the most extensively studied for tx of active Crohn's
Metronidazole
How is achalasia treated today
Botulinum toxin
Until recently, most cases of Achalasia were treated how
Dilation or surgical myotomy
These 3 class of drugs treat diffuse esophageal spasm
Long acting nitrates
CCB
Balloon dilation
What drugs should be avoided in someone w/ IBS and depression
Antidepressants with strong anti-cholinergic effects in pts w/ constipation
This drug is a 5HT-3 antagonist that delays colonic transit and reduces colonic sensation, useful in diarrhea predominant IBS
Alosetron (Lotronex)
This drug is a HT-4 agonist, that stimulates gastric emptying, approved for tx of constipation predominant IBS
Tegaserod (Zelnorm)
3 treatments of ascites
Sodium restriction
fluid restriction
diuretic therapy
-furosemide, amiloride, spironolactone
This drug decreases ammonia diffusion across gut wall and may lead to increased utilization by gut bacteria, used in tx of encephalopathy
Lactulose
Combination tx of what 2 drugs is effective in tx encephalopathy in pts who fail to respond to either agent alone
Neomycin
Lactulose
What drug is a sclerotherapeutic agent used in management of esophageal varicies
Sodium tetradecyl sulfate
This drug is a nonselective vasoconstrictor that reduces portal pressure by constriction of mesenteric and splanchnic arteries and portal veins, thus managing esophagesal varicies
Vasopressin
This drug is a long acting synthetic octapeptide analog of somatostatin, used in managing esophageal varicies
Octreotide