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83 Cards in this Set
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Cromolyn and Nedocromyl sodium MAO and Administration
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only by inhalation
inhibit degranulation of mast cells Used as a prophylactic for exercise induced and antigen induced asthma. Not everyone responds |
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Anti-inflammatory prophylactic agents in asthma
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cromolyn and nedocromyl sodium
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If an asthmatic develops tolerance to B2 agonists, what is the next line of therapeutics?
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corticosteroids
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List antiiflammatory drugs in asthma (steroids)
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beclamethasone
fluticasone flunisolide triamcinolone budesonide |
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SE of corticosteroids
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oral thrush
reduced growth in children osteoporosis |
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Most effective drugs as a tx for asthma
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corticosteroids
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MAO of corticosteroids in asthma
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reduce eicosanoid synthesis
reduce vascular permeability reduce accumulation of phagocytes in lung tissue modulation of cytokine synthesis Can increase and restore the responsiveness of the bronchial smooth muscle to beta 2 adrenergic agonists |
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compare effectiveness of dexamethasone vs prednisolone in tx of asthma
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1 dose of IM dexamethasone is as effective as 5 days of oral prednisolone
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LMWH MAO
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similar to nedocromyl sodium and cromolyn
also reduce activity of beta adrenergic receptor kinase, which leads to preservation of beta adrenergic receptors |
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methylxanthines mao
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increase cAMP by inhibiting phosphodiesterase
inhibit neural transmission in cns at ganglia where adenosine plays a role block adenosine A1 receptor at bronchial smooth muscle |
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Theyophylline with corticosteroids
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antagonistic, resulting in a worsening of lung function
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theophylline dosing effects on cns
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5-20 mg/L therapeutic range, with n and v at the high end
20-40 anorexia headache abdominal discomfort anxiety 40 and above all of the above plus seizures and arrhythmias |
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methylxanthines ddi
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increase clearance: rifampin, oral contraceptives, phenytoin, barbiturates
decrease clearance: cimetidine and erythromycin |
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beta adrenergic agonists for asthma : short acting
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terbutaline
albuterol pirbuterol bitolterol levalbuterol |
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beta adrenergic agonists for asthma: long acting
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salmeterol
formoterol |
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AE of beta agonists for asthma
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tachycardia
hypokalemia tachyphylaxis muscle tremor |
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First step in asthma therapy
Second step |
inhaled corticosteroids
short acting beta adrenergic agonists and only then, if don't respond, think of long acting adrenergic agonists such as formeterol and salmeterol because of increased risk of acute asthma attacks and death reported associated with them |
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muscarinic antagonists in asthma
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ipratropium
triatropium |
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attn: if soy allergy
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ipratropium
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longer lasting
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triatropium
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Risks associated with inhalation of triotropium and ipratropium
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cardiovascular related death!
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Advantage of leukotriene pathway inhibitors in asthma
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oral administration
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zeleuton mao
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inhibits 5-lipooxygenase
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montelukast and zafirlukast
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blockade of LT1 receptor
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leukotriene modifier therapy is associated with what risks?
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neuropsychiatric: mood and behavior, suicide
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omalizumab
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anti IgE
cardiovasc and embolic side effects!!!! not for acute tx |
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Side effects of heparin
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thrombocytopenia
fever rash hemorrhage |
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What should you do at the excessive results with heparin use?
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1st. STOP Heparin
2nd. Use Protamine Sulphate |
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MOA of Heparin
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indirect
binds to ATIII and increases its affinity for thrombin, which inactivates it |
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MOA of LMWH
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bind factor Xa, which is needed in complex with factor Va to activate thrombin
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How should you administer Heparin
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not intramuscularly because it can result in a large hematom
for slow release do SQ or intrafat deep for fast, IV |
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How is Heparin metabolized
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heparinase in the liver
inactive mets excreted in liver so watch out for pts with renal and hepatic failure, since t/2 will be higher |
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What is heparin's effecton triglycerides
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Heparin induces LPL, so it lowers triglycerides in plasma
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moa of fondaparinux
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fondaparinux binds to atIII and increases its affinity to factor Xa
fondaparinux is a synthetic analogue of binding site of heparin to atIII |
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uses of fondaparinux
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dvt tx and prevention
surgery (hip replacement, etc) pulmonary embolism tx and prevention remember: no laboratory monitoring needed and no antidote available a single molecule of fondaparinux is recycled and rebinds to at3 |
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list direct thrombin inhibitors and what is their advantage over the indirect thrombin (through atIII) inhibitors?
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hirudin
lepirudin bivalirudin argatroban advantage: can inhibit trapped thrombin |
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LEPIRUDIN was approved for?
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patients who experienced HIT with use of heparin
Lepirudin reduces risk of serious new thromboembolic complications in pts with hit |
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what are antagonists to Lepirudin?
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no known antagonists
unlike heparin, it is not inhibited by factor IV |
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clearance of Lepirudin
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proportional to GFR
25% lower in women 20% lower in elderly 1st order process t/2 is 1.3 hours in young adults and up to 2 days in pts with renal failure |
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What would you use bivalrudin for?
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tx of unstable angina so prophylaxis of mi in pts undergoing ptca
For this use bivalirudin is given with aspirin also as prophylaxis of dvt in pts undergoing major surgeries (hip, knee) |
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Bivalirudin is more effective than Unfractionated heparin in producing early patency in pts treated with aspirin and streptokinase without increasing the risk of major bleeding. True of false?
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true
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How is bivalirudin eliminated?
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renal and proteolytic
related to gfr |
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what is the second thrombin inhibitor to be indicated for hit after lepirudin?
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argotraban (der of arginine)
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what advantage does argotraban have over lepivirudin?
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unlike lepivirudin, argotraban is hepatically eliminated so we can use in pts with end stage renal disease!
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what does abrupt discontinuation of arogtraban lead to?
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hypercoagulable state which could be detrimental for pts with angina or coronary heart disease
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lepirudin vs argotroban binding to thrombin
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lepirudin irreversible
argotroban reversible |
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discuss argotraban distribution
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most in extracellular
about 50 percent bound to albumin about 34 percent bound to alfa acid glycoprotein |
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Coumarin. Onset of action
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Coumarin inhibits blood clotting by interfering with the hepatic post-transltional modification of the vitamin K dependent clotting factors. It takes 8-12 h but usually about 2-3 days. It depends on the relative amounts of four protein clotting factors which have half lives from 6-60hr
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Antagonist of Coumarin
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vit. K
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With Coumarin, what substance cannot be produced
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prothrombin
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Factors that potentiate coumarin
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decrease in body's vit K
hepatic disease which decreases production of clotting factors hypermetabolic states as in fever and hyperthyroidism in which increase in catabolism of vit K dep. factors occurs |
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Does Heparin cross placenta?
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No
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Does Coumarin cross placenta?
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Yes
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What state decreases activity of coumarin?
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Pregnancy.
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List factors that increase Coumarin efficacy:
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Vit.K deficiency
Age, increased sensitivity Aspirin Heparin Cimetidine, Furosemide, alcohol (acute displacement) |
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Factors that decrease activity of Coumarin
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Pregnancy (contraindicated also)
Genetic (resistance) Barbiturates Cholestyramine Vit. K |
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Since aspirin is contraindicated with Coumarin, what should we use as an analgesic?
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acetomenophen
sodium salicylate |
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Discuss phenylbutazone and oxyphenbutazone in regards to anticoagulants? (non steroidal analgesics)
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can cause severe hemorrhage by imp. platelet aggregation
induce peptic ulcer augment effects of anticoagulants |
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Barbiturates in regards to anticoags?
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Barbiturates increase their clearance
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Rifampin in regards to anticoags?
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Reduces their plasma concentration
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Cholestyramine in regards to anticoags?
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Reduces its plasma concentration
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On warfarin (coumadin), what should you monitor?
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PT time
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Agents that lead to an increased response to coumarin
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aspirin
oxyphenbutazone phenylbutazone |
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Agents that lead to a decreased response to coumarin
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barbiturates
rifampin cholestyramine |
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Aspirin MOA
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antithrombotic for arterial
acetylates cycooxygenase and suppresses TX A2 and prostacyclin formation by platelets effects last for several days (platelets life time) |
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Uses of Dipyridamol
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antithrombotic
used with warfarin for 1 prophylaxis of thromboemboli in pats with prosthetic heart disease used with aspirin to prolong survival of platelets in pts with thrombotic ds it's a vasodilator, little clinical effect by itself |
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advantages of TPA
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second generation thrombolytic
administered iv induces local fibrinolysis but very little systemic unlike reteplase, streptokinase and urokinase |
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Thrombolysis inhibitors
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Aminocarproic acid
tranexamic acid |
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TICLOPIDINE MOA ETC
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binds to P2Y2 coupled to Gi receptors and blocks ADP
takes 8-11 days to achieve effects requires conversion to an active metabolite by P450 SE: N, V, d, neutropenia 1%, thrombocytopenia |
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Ticlopidine uses
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secondary prevention of stroke
reduce cardiac events in pts with unstable angina |
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What is the drug of choice in pts who cannot tolerate aspirin?
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CLOPIDOGREL!!!!!
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What other drug may be superior to clopidogrel in reducing recurrent cardiovascular events?
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prasugrel
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Glycoprotein IIB/IIIA inhibitors
MOA |
GP IIB/IIIA is a surface receptor on pt to bind fibrinogen and willebrand factor
but first they must be activated by collagen, tx a2 or thrombin so these drugs bind the receptor and prevent activation |
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Abciximab
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fab fragment of humanized monoclonal antibody against GPIIb/iiia
used in conjunction with aspirin and heparin in percutaneous angioplasty bound for 18-24 hours unbound clearns in 30 min SE: major hemorrhage or thrombocytopenia may need pltelet transfusion |
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eptifibatide and tirofiban
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tx for unstable angina and mi
short action pltlet f is restored in 6-12 hours after cessation |
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tirofiban
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short duration
efficacy in nonQ wave myo infarction and ustable angina se like eptifibatide |
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Amrinone or Milrinone with CG?
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Milrinone not additive toxicity to CG
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MOA of Amrinone
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PDE inhibitor so increase cAMP
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Dobutamine acts on what receptor?
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B1
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Dopamine effects at dose gradation
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low - vasodilaton at DP1 renal receptor, increased renal flow
medium- b receptor- inotropic chronotropic high- spills into alfa receptors so vasoconstrictive |
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What potentiates CG toxicity
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low serum K and Mg
high serum Ca antacids increase aborption of digoxin p450 activation flushes it out |
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What's bidil and how is it used
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hydralazine+nitrate
used for African American population specifically |
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If you want to add a CCB to beta blockers, should you use verapamil, diltiazem or nifedipine
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do not use verapamil. It adds to the myodepression. It decreases contractility and heart rate. NIfedipine on the other hand does not. It mostly vasodilates smooth muscle.
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