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Pharm Test 5
anemia, immunomodulation, antimycos, allergies, asthma, antifungal
214
Pharmacology
Professional
12/13/2013

Additional Pharmacology Flashcards

 


 

Cards

Term
First line TB drugs?
Definition
RIPES
Rifampin
Isoniazid
Pyrazinamide
Ethambutol
Streptomycin
First line: Start 4 drugs (INH, RIF, PZA, EMB) for 2 months followed by 2 drugs from 4-6 months
Term
Which anti-TB drug inhibits the synthesis of mycolic acid of the cell wall?
Definition
Isoniazid
Term
What anti-TB drug requires catalase peroxidase?
Definition
Isoniazid ---prodrug is activated by catalase peroxidase (katG gene)
Term
Where is INH metabolized? How can this vary among the population?
Definition
N-acetylated in the liver (reduce dosage by half in liver toxicity). Some are rapid, some slow acetylators.
Term
Which anti-TB must be adminisitered with B6/pyridoxine?
Definition
Isoniazid
Term
MOA of Rifampin?
Definition
inhibits DNA-dependent RNA polymerase
Term
MOR to Rifampin?
Definition
Mutations in rpoB gene which produces RNA polymerase B subunit
Term
A patient complains of red body fluids and and flu-like symptoms. What drug have they recently taken?
Definition
Rifampin
Term
Drug interactions with Rifampin?
Definition
reacts with 100+ drugs metabolized by liver microsomal enzymes; impairs OCPs; HIV drug interactions
Term
What TB drug kills ONLY mycobacteria by inhibiting the synthesis of arabinosyl transferase (cell wall synthesis enzyme)?
Definition
Ethambutol
Term
How could a mycobacterium make itself resistant to Ethambutol?
Definition
Point mutation in embB gene encoding arabinosyl transferase
Term
Pharmacokinetics of Ethambutol?
Definition
reduce dose in renal failure, do NOT use in CSF infections
Term
Which drug can cause ocular-retrobulbar neuritis? What are the symptoms?
Definition
Ethambutol --
manifests as red-green colorblindness, blurred vision, central scotomata. Cannot be used in kids who cannot take a visual acuity test.
Term
What anti-TB drug works intracellularly and ONLY works against M. tuberculosis?
Definition
Pyrazinamide
Term
MOR to Pyrazinamide?
Definition
mutuation in pncA gene encoding pyrazinamidase which converts the drug to the active form (pyrazinoic acid)
Term
Which anti-TB drug causes athralgia (due to inc uric acid levels)?
Definition
Pyrazinamide
Term
Which anti-TB drugs cause hepatotoxicity?
Definition
INH (10-20% of pts), Rifampin, Pyrazinamide
Term
Which anti-TB drug can cause Lupus-like syndrome?
Definition
Isoniazid
Term
Which drugs are good for TB meningitis? Which anti-TB should NOT be given?
Definition
Pyrazinamide**, Rifampin

do NOT give Ethambutol
Term
What combo of drugs should be given in a pt with hepatitis and tuberculosis?
Definition
Streptomycin and Ethambutol
Term
MOA of Streptomycin?
Definition
bactericidal by inhibiting protein synthesis by binding to ribosome
Term
What aminoglycosides is streptomycin cross resistant to TB with?
Definition
NONE
Term
What are the two major SE of streptomycin?
Definition
ototoxicity, nephrotoxicity
Term
What drugs are used to treat M Leprae?
Definition
Dapsone and Clofazamine
Term
What drug is used for prophylaxis against PJP?
Definition
Dapsone
Term
What drug can cause hemolysis in G6PD deficient patients?
Definition
Dapsone
Term
What anti-mycobacterial can cause erythema nodosum?
Definition
Dapsone
Term
What drugs are used to treat M avium intracellulare (MAI)?
Definition
Clofazamine, RIF, EMB, Clarithromycin
Term
What drugs are used to treat M. kansasii?
Definition
RIF, EMB, INH for 18 months
Term
Which anti-mycobacterial causes skin pigmentation (look tan)?
Definition
Clofazamine
Term
What 3 drugs are used are used for ORAL iron therapy in anemia?
Definition
FERROUS SALTS = Ferrous sulfate, ferrous gluconate, ferrous fumarate

*Ferrous form (Fe2+) is absorbed in the duodenum and jejunum and is used to make heme. Ferric iron (Fe3+) is storage iron.
Term
What 3 drugs could you give an iron deficient pt with a GI resection/malabsorption syndromes?
Definition
Iron dextran (most common)
also - iron sucrose and iron gluconate
Term
What molecule in the plasma can be used to measure total body stores of iron?
Definition
ferritin

Note: ferritin goes down in iron deficiency and transferrin goes up
Term
What is Deferoxamine?
Definition
Iron chelating substance given for acute iron toxicity (overdose of iron tablets or necrotizing gastroenteritis)
Term
What is hemochromatosis?
Definition
"Iron overload"
usually a term reserved for a genetic cause
Term
How is Vit B12 absorbed? Transported? Stored?
Definition
B12 complexes with Intrinsic Factor and is absorbed in the distal ileum. Absorbed B12 is bound to plasma Transcobalamin II for distribution. B12 is stored mainly in the liver.
Term
What are cyanocobalamin and hydroxycobalamin?
Definition
Prodrugs of Vit B12 given IM. They take 1-2 months to treat anemia.
Term
A pt has megaloblastic anemia, atrophic glossitis (smooth tongue), "subacute combined degeneration" (degeneration of the posterior and lateral columns of the spinal cord) as well as lower limb parathesias. What is your diagnosis? How do you treat it?
Definition
Vitamin B12 deficiency/pernicious anemia
Treat with Vit B12.
*DO NOT GIVE FOLIC ACID AS TREATMENT TO THIS PT. It will not reverse CNS damage.
Term
Who needs recombinant human EPO therapy (eg. Epoetin alfa, Epogen)?
Definition
Chronic renal failure
aplastic anemia
leukemia
HIV/AIDS
Cancer
Anemia of prematurity
post-phlebotomy
Term
How old is Beyonce?
Definition
32
Term
There is usually an inverse relationship between EPO and Hgb, except for in what condition?
Definition
Chronic Renal Failure
both EPO and Hgb are low
Term
What are the two endogenous myeloid growth factors? which one stimulates proliferation of erythroid and megakaryocytic cells too? which one promotes release of hematopoietic stem cells from bone marrow?
Definition
G-CSF and GM-CSF both stimulate growth/differentiation of myeloid cells.
GM-CSF - erythroid and megakaryocytes
G-CSF - release of HSCs
Term
What are filgastrim and pegfilgastrim? what cell lines do they stimulate?
Definition
recombinant G-CSF
FIL and PEG release babies (HSCs) and stimulate growth/differentiation of myeloid
Term
What is sargramostim? what cell lines does it stimulate?
Definition
recombinant GM-CSF
SARah GRAM stimulates MY MEGA ERection (myeloid, megakaryocytes, erythroid)
Term
Which has more toxicities between G-CSF and GM-CSF?
Definition
GM-CSF, thus G-CSF is more preferred.

GM-CSF causes fever, arthralgia, myalgia, peripheral edema, pleural/pericardial effusion
Term
What therapy would you give a pt after intense myelosuppressive chemo to help replenish neutrophil supplies?
Definition
G-CSF (or GM-CSF)
Term
What is an autologous transplant? What therapy is administered to a pt beforehand?
Definition
An autologous transplant is when a patient receives his or her own bone marrow or stem cells that were collected and frozen before admission for high-dose chemotherapy or radiation. G-CSF is used for the mobilization of peripheral blood stem cells for collection.
Term
What is Oprelvekin? What stem cell line does it promote proliferation of?
Definition
recombinant IL-11
megakaryocytes (inc platelets)
Term
What therapy is used to treat thrombocytopenia after chemo?
Definition
IL-11 (oprelvekin) given for 2-3 weeks or until platelet count >50,000/uL
Term
What "peptibody" treats thrombocytopenia by binding to the thombopoietin receptor (Mp1)?
Definition
Romiplostim
Term
What is Eltrombopag?
Definition
thrombopoietin agonist - literally says it in the name "the thrombop ag"
Term
Can you name the five solo albums Beyonce has produced?
Definition
Dangerously in Love (2003)
B'Day (2006)
I Am... Sasha Fierce (2008)
4 (2011)
Beyoncé (2013)
Term
What drug class is a nonspecific competitor of NF-kB at the promoter?
Definition
corticosteroids
Term
What are the four ways that corticosteroids cause "blanket immunosuppression"?
Definition
1. Dec pro-inflammatory cytokine production by MACs (esp IL-1, 6 and TNF-a)
2. (partial) suppression of antigen presentation
3. Alteration in PMN/lymphocyte cell traffic that reduces their availability at inflammatory sites
4. Impaired chemotaxis of PMNs
Term
At what hour of the day would it theoretically be most effective to give corticosteroids?
Definition
2 am (circadian rhythm dictates cytokine peaks in the early morning)
Term
What are the 6 side effects of corticosteroids?*
Definition
1. High risk of infection due to impaired T cell response and poor neutrophil function.
2. Osteoporosis (dec Ca++ uptake, altered bone cytokine balance)
3. DM (due to inc insulin resistance)
4. CNS - insomnia, depression, emotional lability
5. Obesity and stria
6. HTN (interference with RAAS)
Term
Which immunosuppressant is an "alkylating agent"?
Definition
Cyclophosphamide
Term
Which immunomodulator is used to treat Granulomatous Polyangiitis (Wegener's)?
Definition
Cyclophosphamide
Term
Which immunomodulator is used to treat vasculitis?
Definition
Cyclophosphamide
Term
What is the name of Beyonce's current tour?
Definition
The Mrs. Carter Show World Tour
Term
Which immunomodulator can cause hemorrhagic cystitis, bladder fibrosis and cancer?
Definition
Cyclophosphamide
Term
Which immunomodulator can cause infertility?
Definition
Cyclophosphamide
Term
Which immunomodulator is a prodrug metabolized to 6-mercaptopurine? What genetic polymorphism prolongs its activation?
Definition
Azathioprine
TPMT genetic polymorphism decreases deactivation of active 6-mercaptopurine
Term
What drug should not be given with Azathioprine?
Definition
Allopurinol - causes bone marrow suppression
Term
How is Methotrexate used differently for immunosuppression than oncology?
Definition
Used at high doses in oncology to inhibit DNA synthesis.
Used a low doses as an anti-inflammatory
Term
What immunosuppression drug is used to treat RA?
Definition
Methotrexate
Term
Which immunosuppressive drug has a SE of oral ulcers and hypersensitivity pneumonitis? What should be coadministered to reduce this SE?
Definition
Methotrexate
Folic acid PO may reduce SE
Term
Which immunosuppressive drug inhibits T&B cell proliferation by blocking de novo nucleotide synthesis?
Definition
Mycophenolate mofetil
Term
What immunosuppressive is the DOC for SLE?
Definition
Mycophenolate mofetil
Term
Which immunosuppressive is "steroid sparing", aka helps us to use less corticosteroids?
Definition
Mycophenolate mofetil
Term
Which immunosuppressive is the most teratogenic?
Definition
Leflunomide
(washout with cholestyramine if the pt gets pregnant)
Term
Which immunosuppressive has a very long half life and extensive entero-hepatic recirculation?
Definition
Leflunomide
Term
Which immunosuppressive inhibits de novo pyrimidine synthesis?
Definition
Leflunomide
Term
What are the two calcineurin inhibitors? what is calcineurin? wtf is Signal #1 blocking?
LONG ANSWER, GET READY
Definition
Cyclosporine and Tacrolimus

Calcineurin = Ca-dependent protein phosphatase that dephosphorylates a cystopasmic TF in T cells that then translocates to the nucleus and stimulates growth/differentiation of T cells

Signal #1 = normal calcineurin activation after antigen binding to T cell receptor.
Cylcosporine binds to cyclophilin A and then together they bind calcineurin and kill its signal pathway.
Tacrolimus does the same shiz with FKBP.
No Calcineurin activation = no progression to G1.
Term
How many days til Christmas?
Definition
9
Term
Which 2 immunosuppressive drugs are given synergistically after transplants to prevent rejection?
Definition
CNIs (Cyclosporine, Tacrolimus)
and RAP (mTOR/rapamycin/sirolimus)
Term
Which immunosuppressive drug is given for diseases that are primarily T-cell mediated? (eg. ulcerative colitis, uveiitis)
Definition
CNIs (Cyclosporine, Tacrolimus)
Term
Which immunosuppressive drug has a narrow therapeutic window and wide intra/interindividual metabolism?
Definition
CNIs (Cyclosporine, Tacrolimus)
Term
Which immunosuppressive drug is metabolized by P450 enzymes? What happens when given with drugs that activate or suppress this system?
Definition
CNIs (Cyclosporine, Tacrolimus)

This is super important in allograft transplants. Don't be a dipshit and give drugs that ACTIVATE P450 system like phenytoin, dilantin, barbiturates, rifampin because the patient will lose an organ.

ALSO be careful when giving with drugs that INHIBIT P450 like macrolides (erthyromycin, clarithromycin) and the antifungal conazoles. IT CAUSES TOXIC LEVELS of CNIs leading to HTN, HYPERCHOLESTOROLEMIA and NEPHROTOXICITY (cyclo) and NEUROTOXICITY AND DIABETES (tacro). BUT IF YOU'RE SMART, you can actually use this principle to the pts benefit to reduce daily dose of CNI saving them money.
Term
Which immunosuppressive drug needs to be monitored through checking serum blood levels?
Definition
CNIs (Cyclosporine, Tacrolimus)
Term
What does mTOR stand for? What is this drug also called?
Definition
mammalian target of rapamycin
aka sirolimus
Term
How does mTOR/rapamycin/sirolimus work?
Definition
RAP blocks signal #2 (co-stimulation) which prevents cytokine receptor signalling pathways (signal #3). This is mainly IL2/ILR mediated.
Recall: CNIs block signal #1 - TCR activation by Ag.
Term
Which immunosuppressant is anti-fibrinogenic and can also be used on coronary artery stents to prevent re-stenosis?*
Definition
mTOR/RAP
Term
Which immunosuppressant inhibits expression of bcl and is therefore pro-apoptotic?
Definition
mTOR/RAP
Term
Which immunosuppressant can cause hypertriglyceridemia (by decreasing LPL and IGF)?
Definition
mTOR/RAP
Term
Why are monoclonal antibodies that are CD28 blockers "beautiful drugs to use in transplant"?
Definition
T cells are activated when TCR binds to MHCII AND costimulatory CD28 binds to CD80/86. A monoclonal ab called Abatacept (not important to know name) is a CTLA IgG that binds to the CD 80/86 on APC and inhibits CD28 activation. T cells cannot be activated to attack graft. Additionally, you "tolerize" the cell, making the T cell tolerant to the graft.
Term
Which monoclonal antibody works "beautifully" against B cell lymphomas? What is its MOA?
Definition
Rituximab depletes B cells by binding CD20 which makes cells disappear into spleen where they are destroyed. Relatively few side effects. Dr. Robinson's "favorite drug".
Term
What is a "good, transient way" to block an immune response if you don't know what type of immune dz the person has when they come into the hospital?
Definition
IVIG
Term
What is a side effect of IVIG due to its anti-TNF properties?
Definition
Fungal infections, especially histoplasmosis , and progressive multifocal leukencephalopathy
Term
What cytokine would you want to block with a mab in hyper-eosinophilic syndromes?
Definition
IL-5
Term
What mab is used to treat osteoporosis?
Definition
anti-rankL

rankL activates osteoclasts and is overproduced in osteoporosis
Term
What is the generic name for Benadryl?
Definition
Diphenhydramine
Term
What are the 2 first generation H1 Receptor Antagonists?
Definition
Diphenhydramine
Chlorpheniramine
Term
H1 antagonists with strong anti-cholingergic activity (eg. diphenhydramine) are contraindicated in what type of patient?
Definition
COPD, esp during acute attacks, because its anticholinergic activity thickens secretions and decreases expectoration.
Term
Which H1 Receptor Antagonist has anti-motion sickness activity?
Definition
Diphenhydramine
Term
Which H1 Receptor Antagonist treats allergic rhinitis?
Definition
all of first and second generations
Term
All of the H1 receptor antagonists are slight sedatives except for which one?
Definition
Loratidine
Term
Which H1 receptor antagonist is not to be used in cold medicines for children under 4yrs?
Definition
Diphenhydramine
Term
Which H1 receptor antagonists are cxdx in glaucoma?
Definition
Diphenhydramine and Fexofenadine
Term
What are the second generation H1 receptor antagonists?
Definition
Fexofenadine
Loratidine
Cetirizine
Term
What is the generic name for Allegra?
Definition
Fexofenadine
Term
What is the generic name for Claritin?
Definition
Loratidine
Term
What is the generic name for Zyrtec?
Definition
Cetirizine
Term
Which H1 receptor antagonist should not be given with hydroxyzine (a 1G H1 antagonist)?
Definition
Cetirizine
Term
Where are H1 receptors found?
Definition
smooth muscle, endothelium
Term
Where are H2 receptors found?
Definition
gastric mucosa (parietal cells), cardiac muscle, vascular smooth muscle
Term
Where are H3 receptors found?
Definition
presynaptic
Term
Where are H4 receptors found?
Definition
blood cells in bone marrow and circulation - mediate chemotaxis of eosinophils and mast cells
Term
Which two histamine receptors affect the heart? What are the pathways?
Definition
H1 (endothelium) -- Ca --> NO --> sGC --> cGMP --> vasodilation of arterioles
H2 (smooth muscle) -- AC --> cAMP --> relaxation of precapillary sphincters
Term
Which histamine receptor is responsible for gastric secretion? which is responsible for contraction of GI smooth muscle?
Definition
H2 - secretions
H1 - contractions
Term
Which histamine receptor can cause bronchoconstriction?
Definition
H1
Term
What is the triple response to histamine in the skin?
Definition
1. Reddening (dilation of small vessels)
2. Red irregular flare with itching, stimulation of nerve endings.
3. Edematous wheal
Term
Which H1 receptor antagonist is cxdx during pregnancy and lactation?
Definition
Loratidine
Term
Which H1 receptor antagonist is cxdx with MAO inhibitors?
Definition
Fexofenadine
Term
What is the most potent anti-histamine available? 800x more potent than diphenhydramine
Definition
tricyclic anti-depressant Doxepin
Term
Which H1 receptor antagonist has reduced bioavailability if taken with antacids and fruit juices?
Definition
Fexofenadine
Term
Which H1 receptor antagonist is cxdx in a pt with urinary retention?
Definition
Fexofenadine
Term
Which H1 receptor antagonist also inhibits histamine release by reducing degranulation of mast cells?
Definition
Cetirizine
Term
What percentage of asthma is due to allergy?
Definition
30%
Term
What immediate phase spasmogens are released in asthma?
Definition
histamine, platelet-activating factor (PAF) and leukotrienes C4 and D4
Term
What late phase spasmogens are released in asthma?
Definition
leukotriene B4 and PAF
Term
What are the two main categories of anti-asthmatic drugs?
Definition
bronchodilator drugs and anti-inflammatory drugs
Term
What is normal FEV1?
mild obstruction?
severe obstruction?
Definition
normal = 3.9 L
mild obstruction = 3.0 L
severe = 0.9L
Term
What is Beyonce's net worth?
Definition
$350 million
Term
Which B2-agonist is the standard inhaled B-2 agonist for bronchospasm in asthma?
Definition
Albuterol
Term
Which B2-agonist can be administered subQ?
Definition
Terbutaline
Term
Which B2-agonist has the quickest onset?
Definition
Metaproterenol
Term
Which B2-agonist has a unique metabolism?
Definition
Bitolterol is a PRODRUG. Lung esterases hydrolyze hitolterol to terbutylnorepinephrine which is the active form of the drug.
Esterases that hydrolyze the drug are present in higher concentrations in the lung compared to the heart.
Term
Which B2-agonist has the longest duration of action, but should only be used for maintenance treatment of asthma?
Definition
Salmeterol
Term
What are the side effects of b2-agonists?
Definition
skeletal muscle tremor (most common), anxiety, restlessness, tachycardia
Term
What is the MOA for B2-agonists?
Definition
bind to B2 G protein. Activate AC--> cAMP --> PKA --> dec intracellular Ca (decreases contractility)
Term
What 3 ways does theophylline treat asthma?
Definition
1. Inhibition of smooth muscle cAMP phosphodiesterase to maintain high levels of cAMP (smooth muscle relaxant)
2. Antagonism of smooth muscle cell surface receptors for adenosine (bronchoconstrictor in asthmatics)
3. Interference with uptake and sequestration of Ca2+ by the SR in striated muscle to inc cytoplasmic conc - increase cardiac/skeletal muscle contraction
Term
Which methylxanthine is given IV for acute, severe asthma?
Definition
aminophylline
Term
How does smoking affect the half-life of theophylline?
Definition
decreases t1/2
Smoking induces hepatic enzymes that degrade theophylline.
Smoking adults half life = 5 hours.
Non-smoking adults = 9 hours.
Term
How does hepatic dysfunction (as in cirrhosis or decreased blood flow to liver in CHF) affect the half-life of theophylline?
Definition
increases t1/2 (theophylline is hydroxylated and demethylated in the liver)
Term
How does obesity affect the half-life of theophylline?
Definition
increases t1/2
Term
How do OCPs affect the half-life of theophylline?
Definition
increases t1/2
Term
How does a viral upper resp tract infection affect the half-life of theophylline?
Definition
increases t1/2
Term
Why do serum conc of theophylline need to be monitored?
Definition
NARROW therapeutic window = 5-15 micrograms/ml
Interindividual variability of clearance
Dose-related toxicities above 35ug/ml-- CNS: fasciculations, convulsions that are refractory to standard anticonvulsant therapy; Cardiac: tachycardia, arrhythmias, circulatory collapse; elevation in body temp in kids; relaxation of bladder muscle
Term
How is theophylline administered?
Definition
short-acting oral, prolonged oral or iv ...but it CANNOT BE INHALED
Term
Which asthma treatment is a muscarinic antagonist? Why do anticholinergics work for asthma?
Definition
Ipratropium bromide
Asthma can be assoc with vagal-mediated stimulation of bronchial smooth muscle causing bronchospasm and mucus hypersecretion.
Term
What is the MOA of ipratropium bromide?
Definition
inhibits the effect of Ach released from airway vagal nerves by antagonizing muscarinic receptors in bronchial smooth muscles --> dec IP3 --> dec Ca2+ --> relaxation of bronchial sm
Term
What drug should be given with b2-agonists if additional bronchodilitation is needed?
Definition
ipratropium bromide
Term
What drug do you give when B2-agonists and/or theophylline is not well tolerated in asthmatic pts?
Definition
ipratropium bromide
Term
What is the DOC for chronic bronchitis or emphysema in non-asthmatic pts?
Definition
Tiotropium (24 hr anticholinergic bronchodilator)
Term
What minor side effects are assoc with ipratropium bromide?
Definition
dry mouth and pupil dilation (just need to close eyes when inhaling)
Term
How to adrenal corticosteroids help treat asthma? What is the pathway?
Definition
Treats the underlying inflammation which inc airway diameter.

Inc synthesis of lipomodulin --> inhibits phospholipase A2 --> suppresses release of arachidonic acid --> inhibits release of leukotrienes and prostaglandins = bronchodilation
Term
What drug is used to treat Scaptia beyonceae?
Definition
Scaptia beyonceae is not an infectious entity. It is the species of horse fly named after Beyonce in 2011.
Term
What asthma treatment can cause oropharyngeal candidiasis?
Definition
corticosteroids
Term
What is the only asthma adrenal corticosteroid treatment available orally?
Definition
prednisone
Term
What adrenal corticosteroid is used iv as emergency treatment in status asthmaticus?
Definition
methylprednisolone
Term
What adrenal corticosteroids for asthma are inhaled?
Definition
beclomethasone, flunisolide, triamcinolone
Term
Should adrenal corticosteroids be considered as a first line prophylactic therapy in all cases of asthma?
Definition
yes
Term
SE of short-term oral adrenal corticosteroids?
Definition
hyperglycemia, edema, rounding of facial contour
Term
SE of long-term oral adrenal corticosteroids?
Definition
osteoporosis, cataracts, myopathy, HPA axis suppression, psychological depression
Term
SE of inhaled adrenal corticosteroids?
Definition
oropharyngeal candidiasis, dysphonia, dryness of mouth and throat, coughing
Term
What is Symbicort?
Definition
Long acting B-agonist + glucocorticoid combination therapy
Term
What NSAID is used to prevent asthma attacks, including exercise or cold-induced asthma?
Definition
cromolyn sodium
Term
What asthma therapy inhibits degranulation of mast cells?
Definition
cromolyn sodium
Term
What 3 ways does cromolyn sodium prevent asthma?
Definition
inhibits degranulation of mast cells, inhibits recruitment of PMNs and eosinophils to pulmonary epithelium, attenuates the ability of PAF to cause airway hyperreactivity
Term
What is Zafirlukast?* How must it be taken?
Definition
leukotriene inhibitor used in the treatment of asthma by competing with LTD4 (most potent leukotriene) at its cysteinyl LT1 receptor site on airway target cells. Must be taken on empty stomach. 12 years or older.
Term
What drugs are used to treat aspirin-induced asthma?
Definition
any of the Leukotriene inhibitors-- Zafirlukast, Montelukast sodium, Zilueton
Term
Which asthma drug increases PT time when taken with Warfarin?
Definition
Zafirlukast because it inhibits cytP450 degradation of Warfarin
Term
Which leukotriene inhibitor should not be used in breast feeding women?
Definition
Zafirlukast
Term
What drug inhibits leukotriene synthesis by blocking 5' lipooxygenase?*
Definition
Zileuton
Term
What asthma treatment has a side effect of increasing alanine transaminase (ALT)? What is the treatment for that?
Definition
Zileuton; discontinue drug and ALT levels return to normal
Term
What is omalizumab?
Definition
anti-IgE mab which lowers serum free IgE preventing release of histamine and leukotrienes from mast cells. Given subQ. Prophylactic for chronic asthma.
Term
What is the most broad spectrum anti-fungal?
Definition
Amphoteracin B
Term
What is the MOA of Ampho B?
Definition
binds ergosterol in cell wall, forms pores for osmotic fragility
Term
What 2 fungi does Ampho B not treat?
Definition
Candida lusitiniae and Pseudallerischeri boydii
Term
What is the DOC for zygomycosis/mucormycosis?
Definition
Ampho B
Term
Which antifungal should be given in a pregnant/breastfeeding woman?
Definition
Ampho B
Term
What drug should be used to treat fungal infections in immunosuppressed pts?
Definition
Ampho B
Term
What the side effects related to iv infusion of Ampho B?
Definition
fever, chills, muscle spasms, vomiting, HA, hypotension
Term
What antifungal enters the cell via a cytosine-specific permease not found in mammalian cells?
Definition
5-Flucytosine
Term
What happens to 5-Flucytosine once inside the cell?
Definition
It is converted to 5-fluorouracil by cytosine deaminase (not expressed in mammalian cells) and then to 5-FdUMP (inhibits thymidylate synthase - a key enzyme in nucleotide/DNA synthesis) and 5-FUTP (inhibits RNA synthesis)
Term
What drug given with Flucytosine increases its cell permeability?
Definition
Ampho B
Term
What 3 drugs are used to treat Candidal, Cryptococcal or Coccidioidal meningitis?
Definition
Ampho B + Flucytosine (induction)
Fluconazole (consolidation/maintenance)
Term
How many number 1 singles has Beyonce had?
Definition
"Bills, Bills, Bills" (1999)
"Independent Women Part I" (2000)
"Say My Name" (2000)
"Bootylicious" (2001)
"Crazy in Love" feat. Jay-Z (2003)
"Baby Boy" feat. Sean Paul (2003)
"Check On It" feat. Slim Thug (2005)
"Irreplaceable" (2006)
"Single Ladies" (2008)
Term
What is the MOA for azoles?
Definition
inhibit 14a-sterol demethylase, a fungal CYP450 enzyme involved in the conversion of lanesterol into ergosterol
FUNGISTATIC
Term
What is the order of SOA for the azole antifungals?
Definition
Posaconazole (broadest)
Voriconazole
Itraconazole
Fluconazole (narrowest)
Term
What is the prototype for azole antifungals? What are its side effects?
Definition
Ketoconazole (rarely used, replaced by itraconazole)
SE: dec cortisol and testosterone (due to inhibition of CYP450 enzymes involved in adrenal and gonadal steroid synthesis) leads to gynecomastia, dec libido, impotence, menstrual irregularities, hypotension, fatigue
Term
Which azole can be used in pregnancy?
Definition
NONE, they can cause fetal abnormalities
Term
What antifungals should you not use statins with due to the risk of rhabdomyolysis?
Definition
Itraconazole and Voriconazole
Term
What antifungal drugs act on the plasma membrane?
Definition
Polyenes -- Ampho B and Nystatin
Term
What antifungal drug inhibits DNA/RNA synthesis?
Definition
Flucytosine
Term
What antifungal drugs act on the ER, inhibiting ergosterol synthesis?
Definition
azoles, terbinafine
Term
What antifungal drug acts on the microtubules of the mitotic spindle?
Definition
griseofulvin
Term
What antifungal drugs act on the cell wall?
Definition
Echinocandins
Term
What are the 3 side effects of all azole drugs?
Definition
GI distress, hepatotoxicity, teratogenic
Term
What is the only azole that needs renal dose adjustment in renal insufficiency?
Definition
Fluconazole
It is eliminated 80% unchanged by the kidney
Term
What antifungal has a minor side effect of alopecia that is reversible?
Definition
Fluconazole
Term
What is the DOC for non-meningeal endemic dimorphic fungal infections (blastomyces, histoplasmosis, sporothrix, coccidioidomycosis, oral dermatophytes)
Definition
Itraconazole
Term
What is the triad of SE seen with Itraconazole use?
Definition
HTN, hypokalemia, peripheral edema
Term
When is Itraconazole Cxdx?
Definition
CHF and ventricular dysfunction
also with statins
Term
What is the TOC for invasive aspergillus?
Definition
Voriconazole
Term
Which antifungal can cause periostitis?
Definition
Voriconazole
Term
Which antifungal can cause changes in color vision (in 30% of pts)?
Definition
Voriconazole
Term
Which antifungal can cause visual/auditory hallucinations, seizures, and phososensitivity/rash?
Definition
Voriconazole
Term
Which antifungal has non-linear metabolism?
Definition
Voriconazole
Term
Which antifungal is an inhibitor of CYP34A AND CYP2C9, CYP2C19?
Definition
Voriconazole
(other azoles inhibit just CYP3A4, voriconazole has the most potential for drug interaction)
Term
What is the only azole active against zygomycosis/mucormycosis?
Definition
Posaconazole (this would be given if Ampho B didn't work/couldn't be given)
Term
What is Posaconazole primarily used to treat?
Definition
invasive fungal infections
Term
What are the 3 echinocandins?
Definition
Caspofungin, Micafungin, Anidulafungin
Term
What antifungal targets B(1,3)-D-glucan synthase complex in the cell wall?
Definition
Echinocandins
Term
What are the echinocandins two major uses?
Definition
1. treatment of severe disease candidiasis (NOT in meningitis).
2. given for Aspergillus if Ampho B/Voriconazole don't work
Term
SOA for Griseofulvin? what is its clinical use?
Definition
only dermatophytes (epidermophyton, microsporum, trichophyton)
Used to treat superficial skin/nail infection with dermatophytes. 6 month treatment.
Term
Which antifungal inhibits squalene epoxidase, increasing the levels of squalene (toxic to fungus)?
Definition
Terbinafine
Term
What is the most effective treatment for tinea capitis, corpis, cruris, pedis and onchomycosis?
Definition
Oral Terbinafine
Term
Which antifungal has extensive first pass metabolism?
Definition
Oral Terbinafine
Term
What is the MOA for Nystatin?
Definition
Nystatin is a polyene like Ampho B but is used topically. It binds ergosterol and forms pores.
Term
What drug is used in a "swish and swallow" way to treat oral candidiasis?
Definition
Nystatin
Term
What is used to treat oral and vulvovaginal candidiasis?
Definition
Topical azoles - clotrimazole, miconazole, terconazole
Term
What is Butenafine?
Definition
a topical benzylamine used to treat mild cases of tinea cruris, corporis, pedis
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