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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
Q

Which drug accelarates the conversion of plasminogen to plasmin

A

Reteplase

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26
Q

If a fibrinolytic drug is used for treatment of acute MI, which of the following adverse drug effects is most likely to occur

A

Hemorrhagic stroke

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27
Q

Mechanism of action of clopidogrel?

A

Thea ctive metaboliye of clopidogrel binds to an inhibits the platelet ADP receptors

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28
Q

Dabigatran is a ______________

A

Direct inhibitor of thrombin

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29
Q

Sudden discontinuance of apixaban can lead to?

A

stroke

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30
Q

Which test would provide accurate information about the coagulation status of patient taking apixaban?

A

Factor X test

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31
Q

Relative to unfractionated heparin, enoxaparin ______

A

can be used without monitoring the patient’s aPTT

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32
Q

TO prevent severe hemorrhage caused by excessive warfarin, what can be given?

A

Vitamin K

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33
Q

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 ________

A

Bivalirudin

  • Direct thrombin inhibitors such as bivalirudin and argatroban provide parenteral anticoagulation similar to that achieved with heaprin.
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34
Q

Unfractionated heparin

A

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

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35
Q

Rivaroxiban

A

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

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36
Q

Direct thrombin inhibitors

(Bivalirudin, argatoban, dabigatran)

A

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)

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37
Q

Warfarin

A

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

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38
Q

Alteplase, recombinant human tissue plasminogen activator

A

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
Q

Bacterial protein that forms a complex with plasminogen that rapidly converts plasminogen to plasmin. Subject to inactivating antibodies and allergic reactions

A

Streptokinase

40
Q

Aspirin

A

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
Q

Abciximab

A

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
Q

Eptifibate, tirofiban

A

reversible GP IIb/IIIa inhibitors of smaller size than abciximab

43
Q

Clopidogrel

A

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
Q

older ADP receptor antagonist with more toxicity, particularly leukopenia and TTP

A

Ticlodipine

45
Q

Newer drug, similar to clopidogrel with less variable kinetics, activation primarily by CYP3A4

A

Prasugrel

46
Q

Reversible ADP receptor antagonist that does not require activation

A

Ticagrelor

47
Q

Dipyridamole

A

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
Q

Vitamin K

(ohytonadione)

A

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
Q

vasopressin V2 receptor agonist increases concentrations of vWF and factor VIII

A

Desmopressin

50
Q

Aminocaproic acid

A

Competitively inhibits plasminogen activation

Used in exxcessive fibrinolysis

Oral and parenteral administration

SE: thrombosis, hypotension, myopathy, diarrhea

Tranexamic acid : analog of aminocaproic acid

51
Q

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

A

HMG-CoA reducatase inhibitors

52
Q

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?

A

Niacin

53
Q

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?

A

Cholestyramine

54
Q

Cholesterol lowering drug contraindicated in pregnancy

A

HMG-CoA reductase inhibitors

55
Q

Major mechanism of action of gemfibrozil

A

Increased TG hydrolysis by lipoprotein liapse

56
Q

Major toxicity by gemfibrozil

A

Cholelithiasis

57
Q

Consumption of alcohol is associated with what changes in lipid concentration?

A

Increased TG

Increased VLDL

58
Q

If aptient has gout, what lipid lowering drug will exacerbate it?

A

Niacin

59
Q

The 2 primary adverse effects of HMG-CoA reductase?

A

Hepatotoxicity adn myopathy

60
Q

Major recognized effct of ezetimibe

A

Inhibition of absorption of cholesterol in the intestine

61
Q

Statins

(Atorvastatin, Simvastatin, rosuvastatin, pitavastatin)

A

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
Q

FIbrates

(Gemfibrozil, fenofibrate)

A

PPAR-alpha agonist

Used in hypertriglyceridemia (VLDL), low HDL cholesterol

Oral adminsitration

Myopathy, heaptic dysfunction, cholestasis

63
Q

Bile acid binding resins

(Colestipol)

A

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
Q

Sterol absorption inhibitor

(Ezetimibe)

A

Reduces intetsinal uptake of cholesterol by inhibiting sterol transporter NPC1L1

Used in elevated LDL cholesterol, phytosterolemia

Oral administration

Rarely, heaptic dysfunction, myositis

65
Q

Niacin

A

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
Q

PCSK9 inhibitors

(Evolucumab, alirocumab)

A

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
Q

Lomipatide

A

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
Q

Mipomersen

A

An antisense oligonucleide that targets apo B-100, mainly in the liver.

69
Q

Among NSAIDs, aspirin is unique because it

A

Irreversibly inhibits its target enzyme

70
Q

Analgesic and antipyretic drug that lacks an anti inflammatory action

A

Acetaminophen

71
Q

ASpirin overdose

A

Hypethermia, metabolic acidosis, dehydration, coma

72
Q

What drug is most likely to increase serum concentrtions of conventional dose of methotrexate, a weak acid that is primarily cleared in the urine?

A

Probenecid

  • competes with the methotrexate for binding to the proximal tubule transporter and thereby decreases the rate of clearance of methotrexate
73
Q

The main advantage of ketorolac over aspirin is that ketorolac is _______________

A

Availbale in a parenteral formulation that can be injected IM or SQ

74
Q

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?

A

Liver failure

75
Q

Many physicians prefer to treat acute gout with a corticosteroid or indomethacin because, high doses of colchicine are likely to cause

A

Severe diarrhea

76
Q

In treating chronic gout, What drug could be used to decrease rate of production of uric acid?

A

Allopurinol

77
Q

Most compelling reason for avoiding celecoxib in the treatment of arthritis

A

History of Myocardial infarction

78
Q

Parenterally administered DMARD whose mechanism of anti inflamatory action is antagonism of TNF alpha

A

Etenercept

79
Q

Anti IL1 drugs

A

anakinra, rilonacept, canakinumab

80
Q

Anti-IL6 drug

A

tocilizumab

81
Q

Inhibits B-lymphocyte stimulator

A

Belimubab

82
Q

Janus kinase inhibitor

A

Tofacitinib

83
Q

Aspirin

A

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
Q

Aspirin dosages

A
  • 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
Q

Ibuprofen

A

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
Q

Celecoxib

A

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
Q

Acetaminophen

A

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
Q

Methotrexate

A

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
Q

Infliximab

A

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
Q

Colchicine

A

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
Q

Probenecid

A

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
Q

Allopurinol

A

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
Q

Pegloticase

A

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

I hate DRUGS!! (26 decks)

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