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I hate DRUGS!! > Drugs with Important actions in Blood, Inflammation and Gout > Flashcards

Drugs with Important actions in Blood, Inflammation and Gout Flashcards

1
Q

23 year old woman is referred by her OB for evaluation of anemia. If this woman has macrocytic anemia, an icnreased serum concentration of transferrin and a normal serum concentration of Vitamin B12, the most likely cause of her anemia is deficiency of_________

A

Folic acid

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2
Q

The laboratory data of your pregannt patient indicate that she does not have macrocytic anemia but rather microcytic anemia. Optimal treatment of normocytic or mild micocytic anemia associated with preganncy uses _____

A

ferrous sulfate tablets

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3
Q

Accidental posioning of ferrous tablet causes ______

A

Necrotizing gastroenteritis, shock, and metabolic acidosis

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4
Q

Immediate treatment for iron tablet toxicity

A

Parenteral deferoxamine

  • Oral defarasirox is effective for chronic iron toxicity
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5
Q

A 45 year old male stomach cancer patient underwent tumor removal surgery. After surgery he developed megaloblastic anemia. His anemia is caused by a deficiency of _____ and can be treated with _______

A

Intrinsic factor

Vitamin B12

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6
Q

Which of the following is most likely to be required by a 5 year old boy with chronic renal insufficiency?

A

Erythropoeitin

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7
Q

In a patient who requires filgastrim (G-CSF) after being treated with anticancer drugs, the therapeutic objective is to prevent

A

Systemic infection

  • Stimulates the production and function of neutrophils, important cellular mediators of the innate immune system that serce as the first line of defense against infection
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8
Q

The megaloblastic anemia that results from vitamin B12 deficiency is due to inadequate supplies ________

A

dTMP

  • Homocysteine and N-methyltetrahydroloate accumulate
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9
Q

Treatment for chemotherapy induced thrombocytopenia

A

Oprelvekin (IL-11)

  • Stimulates platelt production and decreases the number of platelt transfusions
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10
Q

Twenty months after finishing chemotherapy. The woman had a relapse of breast cancer and was now unresponsive to standard doses of chemotherapy. The decion was to use high-dose chemotherapy followed by autologous stemm cell transplantation. Which of the following drugs is most likely to be used to mobilize the peripheral blood stem cells needed for the patient’s autologous stem cell transplantation?

A

Filgrastim (G-CSF)

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11
Q

Ferrous sulfate

A

Required for biosynthesis of heme and heme containing proteins, including hemoglobin and myoglobin

Used in IDA

Complicated endogenous system for absorbing, storing and transporting iron. No mechanism for iron excretion other than cell and blood loss

Acute overdose results in necrotizing gastroenteritis, abdominal pain, bloody diarrhea, shock, lethargy, and dyspnea. Chronic iron overload results in hemochromatosis with damae to the heart, liver and pancreas

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12
Q

Parenteral preparations of iron

A

Iron dextran, iron sucrose complex, sodium ferric gluconate, and ferumoxytol.

  • Can cause pain, hypersensitivity reactions
  • ferumoxytol may interefere with MRI studies
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13
Q

Deferoxamine

A

Chelates excess iron

Used in Acute iron poisoning. inherited or acquired hemochromatosis

Preferred routes of administration: intramuscular or subcutaneous

Rapid IV administration may cause hypotension. Neurotoxicity and increased susceptibility to certain infections has occured with long term use

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14
Q

Vitamin B12

(Cyanocobalamin, hydroxocobalamin)

A

Cofactor required for essential enzymatic reactions that form tetrahydrofolate, convert homocysteine to methionine and metabolize L-methylmalonyl-CoA

Used in Vitamin B12 deficiency, which manifests as megaloblastic anemia and is the basis of pernicious anemia

Parenteral vitamin B12 is required for pernicious anemia and other malabsorption syndromes

No toxicity associtaed with excess B12

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15
Q

Folic Acid

(Folacin/pteroylglutamic acid)

A

Precursor of an essential donor of methyl groups used for synthesis of amino acids, purines and deoxynucleotides

Folic acid deficiency, which manifests as megaloblastic anemia. Prevention of NTD

Oral is well absorbed; need for parenteral administration is rare

Not toxic in overdose, but large amounts can mask vitamin B12 deficiency

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16
Q

Epoetin alfa

A

Agonist of erythropoietin receptors expressed by red cell progenitors

Used in anemia, especially associated with CKDm HIV infection, cancer, and prematurity. Prevention of need for transfusion in patients undergoing certain types of elective surgery

Intravenous or subcutaneous adminsitration 1-3 x per week

SE: Hypertension, thrombotic complications and very rarely, pure red cell aplasia. To reduce risk of serious CVD, hemoglobin should be maintained <12 g/dL

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17
Q

Long acting glycosylated erythropoiesis-stimulating agents (ESAs)

A

Darbepoetin alfa

  • Methoxy polyethylene glycol-epoetin beta: adminsitered 1-2x per month
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18
Q

G-CSF

(filgrastim)

A

Stimualtes G-CSF receptors expressed on mature neutrophils and their progenitors

Used in neutropenia associated with congenital neutorpenia, cyclic neutropenia, myelodysplasiam and aplastic anemia. Secondary prevention of neutropenia in aptients undergoing cytotoxic chemotherapy. Mobilization of peripheral blood cells in preparation for autologous and allogenic stem cell transplantation

Daily subcutaneous adminsitration

SE: bone pain. rarely, splenic rupture

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19
Q

long acting form of filgastrim that is covalently linked to a type of polyethylene glycol

A

Pegfilgrastim

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20
Q

Myeloid growth factor that acts through a distinct GM-CSF receptor to stimulate proliferation and differentiation of early and late granulocytic progenitor cells, and erythroid and magakaryocyte progenitors.

A

GM-CSF (sargramostim)

More likely to cuase fever, arthralgia, myalgia, and capillary leak syndrome

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21
Q

Antagonist of CXCR4 receptor used in combiantioon with G-CSF for mobilixation of peripheral blood cells prior to autologous transplantation in patients with multiple myeloma and non-Hodgkin’s lymphoma who responded suboptimally to G-CSF alone

A

Plerixafor

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22
Q

Oprelvekin (IL-11)

A

Recombinant form of an endogenous cytokine. activates IL-II receptors

USed in secondary prevention of thrombocyrtopenia in patients undergoing cytotoxic chemotherapy for nonmyeloid cancers

Daily SQ adminsitration

SE: Fatigue, headache, dizziness, anemia, fluid accumulation in the lungs, and transient atrial arrythmias

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23
Q

genetically engineered protein in which the Fc components of ahuman antibody are fused to multiple copied of a peptide that stimualtes the thrpombopoetin receptors

A

Romiplostim

Approved for treatment of ITP

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24
Q

Orally active agonist of thrombopoetin receptor; restricted use because of risk of hepatotoxicity and hemorrhage

A

Eltrombopag

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25
Which drug accelarates the conversion of plasminogen to plasmin
Reteplase
26
If a fibrinolytic drug is used for treatment of acute MI, which of the following adverse drug effects is most likely to occur
Hemorrhagic stroke
27
Mechanism of action of clopidogrel?
Thea ctive metaboliye of clopidogrel binds to an inhibits the platelet ADP receptors
28
Dabigatran is a \_\_\_\_\_\_\_\_\_\_\_\_\_\_
Direct inhibitor of thrombin
29
Sudden discontinuance of apixaban can lead to?
stroke
30
Which test would provide accurate information about the coagulation status of patient taking apixaban?
Factor X test
31
Relative to unfractionated heparin, enoxaparin \_\_\_\_\_\_
can be used without monitoring the patient's aPTT
32
TO prevent severe hemorrhage caused by excessive warfarin, what can be given?
Vitamin K
33
A patient develops severe thrombocytopenia in response to treatment with unfractionated hepatin and still requires parenteral anticoagulation. The patient is most likely to be treated with \_\_\_\_\_\_\_\_
Bivalirudin * Direct thrombin inhibitors such as bivalirudin and argatroban provide parenteral anticoagulation similar to that achieved with heaprin.
34
Unfractionated heparin
Complexes with ATIII. irreversibly inactivated the coagulation factors thrombin and factor Xa Used in venous thrombosis, PE, MI, unstable angina, adjuvant to PCI and thrombolytics Parenteral administration SE: bleeding (monitor with aPTT, protamine is reversal agent). Thrombocytopenia, osteoporosis with chronic use
35
Rivaroxiban
Binds to the active site of factor Xa and inhibits its enzymatic action Used in venous thrombosis, pulmonary embolism, prevention of stroke in patients with nonvalvular atrial fibrillation Oral administration. Fixed dose, no routine monitoring (factor Xa test) SE: bleeding. no specific reversal agent
36
Direct thrombin inhibitors | (Bivalirudin, argatoban, dabigatran)
Bind to thrombin's active site and inhibit its enzymatic action Anticoagulation in patients with Heparin induced thrombocytopenia Bivaluridin and argatroban: IV adminsitration, Dabigatran: oral administration SE: Both: bleeding(monitor with aPTT). Idarucizumab (Fab fragment binds and reverses effect of dabigatran)
37
Warfarin
Inhibits Vitamin K epoxide reducatase and therby interferes with production of functional vitamin K-dependent clotting and anticlotting factors Used in venous thrombosis, PE, prevention of thromboembolic complications of aFIb or cardiac valve replacement Oral adminsitration. delayed onset and offset of anticoagulant activity. many drug interactions SE: bleeding (monitor with PT, vitamin K is a reversal agent). Thrombosis early in therapy due to protein C deficiency. Teratogen
38
Alteplase, recombinant human tissue plasminogen activator
Converts plasminogen to plasmin, which degrades the fibrin in thrombi Used in coronary artery thrombosis, ischemic stroke, PE Parenteral administration SE: bleeding, especially cerebral hemorrhage
39
Bacterial protein that forms a complex with plasminogen that rapidly converts plasminogen to plasmin. Subject to inactivating antibodies and allergic reactions
Streptokinase
40
Aspirin
Nonselective, irreversible COX inhibitor. reduces platelet production of thromboxane A2, a potent stimulator of platelet aggregation Used in prevention and treatment of arterial thrombosis Dose required for antithrombotic effect is lower than anti-inflammatory dose. Duration of activity is longer than pharmokinetic half-life due to irreversible action SE: GI toxicity, nephrotoxicity, hypersensitivity reaction due to increased leukotrienes; tinnitus, hyperventilation metabolic acidosis, hyperthermia, coma in overdoe
41
Abciximab
GP IIB/IIIa inhibitor Inhibits platelet aggregation by interfering with GP IIb/IIIa binding to fibrinogen and other ligands Used during PCI to prevent restonsis. ACS Parenteral adminsitration SE: Bleeding, thrombocytopenia with prolonged use
42
Eptifibate, tirofiban
reversible GP IIb/IIIa inhibitors of smaller size than abciximab
43
Clopidogrel
Prodrug: active metbolite by CYP2C9 and CYP2C19 irreversible inhibits platelet ADP receptor ACS, prevention of restenosis after PCI, prevention and treatment of arterial thrombosis Oral administration SE: Bleeding, GI disturbances, hematologic abnormalities
44
older ADP receptor antagonist with more toxicity, particularly leukopenia and TTP
Ticlodipine
45
Newer drug, similar to clopidogrel with less variable kinetics, activation primarily by CYP3A4
Prasugrel
46
Reversible ADP receptor antagonist that does not require activation
Ticagrelor
47
Dipyridamole
Inhibits adenosisne uptake and inhibits PDE enzymes that degrade cAMP, cGMP used in prevention of thromboembolic complciations of cardiac valce repalcement. Combined with aspirin for for secondary prevention of ischemic stroke Oral administration SE: headache, palpitations, contraindicated in congestive heart failure
48
Vitamin K | (ohytonadione)
Increase supply of reduced vit. K, which is required for synthesis of functional vitamin K dependent clotting and anticlotting factors Used in Vit. K deficiencym reversal of excessiv warfarin anticlotting activity Oral or parenteral administration SE: severe infusion reaction when given IV or IM
49
vasopressin V2 receptor agonist increases concentrations of vWF and factor VIII
Desmopressin
50
Aminocaproic acid
Competitively inhibits plasminogen activation Used in exxcessive fibrinolysis Oral and parenteral administration SE: thrombosis, hypotension, myopathy, diarrhea Tranexamic acid : analog of aminocaproic acid
51
Pj is a year old boy. AT his checkup. noted cutaneous xanthoma. Serum cholesterol of \>936. Further testing confirms diagnosis of homozygous familial hypercholesterolemia. What is the least effective drug class for this
HMG-CoA reducatase inhibitors
52
A 46 year old patient had this lipid profile * Before treaments * TG: 1000 TC: 640 LDL: 120 VLDL 500 HDL 20 * 6 months after * TG: 300 TC: 280 LDL: 90 VLDL 150 HDL 40 What is the most likely drug given to the patient?
Niacin
53
A patient is a diagnosed case of familial combined hyperlipidemia. He has elevated total cholesterol, LDL cholesterol, and TG. her HDL is somewhat reduced What drug is most likelyto increase TG and VLDL when used as monotherapy?
Cholestyramine
54
Cholesterol lowering drug contraindicated in pregnancy
HMG-CoA reductase inhibitors
55
Major mechanism of action of gemfibrozil
Increased TG hydrolysis by lipoprotein liapse
56
Major toxicity by gemfibrozil
Cholelithiasis
57
Consumption of alcohol is associated with what changes in lipid concentration?
Increased TG Increased VLDL
58
If aptient has gout, what lipid lowering drug will exacerbate it?
Niacin
59
The 2 primary adverse effects of HMG-CoA reductase?
Hepatotoxicity adn myopathy
60
Major recognized effct of ezetimibe
Inhibition of absorption of cholesterol in the intestine
61
Statins (Atorvastatin, Simvastatin, rosuvastatin, pitavastatin)
Inhibits HMG-CoA reductsae Used in atherosclerotic vascular doisease (primary and secondary prevention). Acute coronary syndromes Oral adminsitration. P450-dependent metabolism (CYP3A4, CYPC9) interacts with P450 inhibitors/competitors SE: myopathy, hepatic dysfunction, teratogen
62
FIbrates | (Gemfibrozil, fenofibrate)
PPAR-alpha agonist Used in hypertriglyceridemia (VLDL), low HDL cholesterol Oral adminsitration Myopathy, heaptic dysfunction, cholestasis
63
Bile acid binding resins | (Colestipol)
Prevents reabsorption of bile acids from the GI tract Used in elevated LDL cholesterol, pruritus Oral administration. Interferes with absorption of some drugs and vitamins. SE: constipation, bloating
64
Sterol absorption inhibitor | (Ezetimibe)
Reduces intetsinal uptake of cholesterol by inhibiting sterol transporter NPC1L1 Used in elevated LDL cholesterol, phytosterolemia Oral administration Rarely, heaptic dysfunction, myositis
65
Niacin
Decreases catbolism of apo A-1 reduces VLDL secretion from liver. Icnreases HDL cholesterol USed in low HDL cholesterol, elevated VLDL and LDL Oral administration SE: GI irritation, flushing, heaptic toxicity, hyperuricemia, may reduce glucose tolerance
66
PCSK9 inhibitors | (Evolucumab, alirocumab)
Complexes PCSK9. Inhibits catabolism of LDL receptor Used in familial or ther resitant hypercholesterolemia not responsive to oral therapy Parenteral SE: injection site reactions, nasopharyngitis, flu-like symptoms
67
Lomipatide
Microsomal triglcyeride transfer protein (MTP) inhibitor * MTP plays an essential role in accretion of TG to nascent VLDL in liver and to chylomicrons in the intestine. * Its inhibition decreases VLDL secretion and consequently the accumulation of LDL in plasma
68
Mipomersen
An antisense oligonucleide that targets apo B-100, mainly in the liver.
69
Among NSAIDs, aspirin is unique because it
Irreversibly inhibits its target enzyme
70
Analgesic and antipyretic drug that lacks an anti inflammatory action
Acetaminophen
71
ASpirin overdose
Hypethermia, metabolic acidosis, dehydration, coma
72
What drug is most likely to increase serum concentrtions of conventional dose of methotrexate, a weak acid that is primarily cleared in the urine?
Probenecid * competes with the methotrexate for binding to the proximal tubule transporter and thereby decreases the rate of clearance of methotrexate
73
The main advantage of ketorolac over aspirin is that ketorolac is \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
Availbale in a parenteral formulation that can be injected IM or SQ
74
An 18 month old boy dies from an accidental overdose of acetaminophen. Which of the following is the msot likely cause of this patient's death?
Liver failure
75
Many physicians prefer to treat acute gout with a corticosteroid or indomethacin because, high doses of colchicine are likely to cause
Severe diarrhea
76
In treating chronic gout, What drug could be used to decrease rate of production of uric acid?
Allopurinol
77
Most compelling reason for avoiding celecoxib in the treatment of arthritis
History of Myocardial infarction
78
Parenterally administered DMARD whose mechanism of anti inflamatory action is antagonism of TNF alpha
Etenercept
79
Anti IL1 drugs
anakinra, rilonacept, canakinumab
80
Anti-IL6 drug
tocilizumab
81
Inhibits B-lymphocyte stimulator
Belimubab
82
Janus kinase inhibitor
Tofacitinib
83
Aspirin
Acetylation of COX-2 and COX-2 results in decreased prostaglandin syntheis Used in analgesia, antipyretic, antiinflamamtory and antithrombotic (low dose) Duration of activity is longer than pharmacokinetic halflife of drug due to irreversible COX inhibition. SE: GI toxicity, nephrotoxicity, and icnreased bleeding time at therapeutic levels. Bronchonstrictor raction due to increased leukotrienes. Tinnitus, hyperventilation, metabolic acidosis, hyperthermia, coma in overdose
84
Aspirin dosages
* Low range (\<300 mg/d) * reducing platelet aggregation * Intermediate dose (300-2400 mg/d) * antipyretic and analgesic effects * High dosaes (2400-4000 mg/d) * anti-inflamatory effect At low dose - first order at high dose - zero order kinetics
85
Ibuprofen
Reversible inhibition of COX-1 and COX-2 results in decreasd prostaglandin synthesis Used in analgesia, antipyretic, and anti-inflammatory. CLosure of patent ductus arteriosus Rapid metabolism and renal elimination SE: GI toxicity, nephrotoxicity. Reaction due to increased leukotrienes. Interfere with aspirin's antithrombotic action
86
Celecoxib
Selective, reversible inbition of COX-2 results in decreased prostaglandin synthesis Used in analgesia, antipyreticm and anti-inflammatory Hepatic metabolism Nephrotoxicity, Reaction die to increased leukotrienes. Less risk of GI toxicity than nonselective NSAIDs. greater risk of thrombosis than nonselective NSAIDs
87
Acetaminophen
Mechanism unknown, Weak COX inhibitor Analgesia, antipyretic Hepatic conjugation Hepatoxicity in overdose (antidote is acetylcysteine). Hepatotoxicity more likely with chronic alcohol consumption which induces P450 enzymes
88
Methotrexate
DMARD conventional syntehtic cytotoxic to rapidly dividing immune cells due to inhibition of dihydrofolate reductase Anticancer, Rheumatic disorders Renal elimination SE: nausea, mucosal ulcers, hematotoxicity, hepatotoxicity, teratogenicity
89
Infliximab
Biologic (b) anti-TNF alpha Used in rheumatoid arthritis SE: opportunistic infections and reactivation of latent TB and HBV. Increased risk of skin cancer
90
Colchicine
Inhibition of mictorubile assembly decreases macrophage migration and phagocytosis Used in chronic and acute gout, familial mediterranean fever Oral drug SE: diarrhea, severe liver and kidney damage in overdose
91
Probenecid
Inhibition of renal reabsorption of uric acid. Chronic gout, prolongation of antimicrobial drug action, Oral drug SE: exacerbation of acute gout, hypersensitivity reactions, inhibits renal tubular secretion of weak acids such as MTX
92
Allopurinol
Active metabolite irreversibly inhibits xanthine oxidase and lowers production of uric acid Chronic goutm adjunct to cancer chemotherapy Activated by xanthine oxidase, oral drug GI upset, hypersensitivity reactions, bone marrow suppression
93
Pegloticase
Recombinant mammalian uricase converts uric acid to the soluble allantoin USe din chronic refractory gout IV SE: Rapid change in uric acid levels can precipitate gout flare. Prophylaxis with NSAIDs or colchicine

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