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143 Cards in this Set
- Front
- Back
Pharmacokinetics |
the study of drug movement through the body. The effect of the body on the drug.
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Absorption
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the movement of a drug from its administration site into the circulation
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Rate of Absorption
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how soon the effects of a drug will begin
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Amount of Absorption
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intensity of the drugs effects
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Factors affecting absorption
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rate of dissolution, surface area, blood flow, lipid solubility, pH partitioning,
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Rate of dissolution
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drugs in formulations that have rapid dissolution have a faster onset than drugs with slower rate of dissolution
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Surface Area
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the larger the surface area the faster the absorption. Small intestine has fastest absorption of oral administered drugs
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Blood Flow
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the more vascular a site the quicker the absorption. Works on concentration gradient, blood containing newly absorbed drug will be replaced rapidly by drug free blood.
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Lipid Solubility
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Highly lipid soluble drugs absorb more rapidly.
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pH partitioning
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drug absorption and elimination ca be affected by acid/base concepts. Also works on concentration gradient. Acid drugs are drawn toward alkaline and vice versa. Important in treatment of overdoses.
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Routes of administration
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enteral and parenteral and less commonly topical etc.
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Enteral Administration
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via the gastrointestinal tract
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Parenteral Administration
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drugs given by penetration of the skin and entry into the underlying tissue
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IV
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rapid effect maximal degree of control over circulating drug. Usually aqueous. Not reversible.
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Drawbacks of IV
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Infection, repeat dosage requires patent iv line.
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IM
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May be used for drugs that are aqueous and non-aqueous. Deltoid and Vastus lateralis quicker than dorso-gluteal or ventro-gluteal admin. Related to blood flow to tissue
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Subcutaneous
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Dependent on blood flow to the tissue. Slow and constant absorption, non-irritating requires absorption into capillaries.
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Oral
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most common. Variable in terms of availability. Efficacy may be limited by metabolism. Food in system may affect efficacy/action or delay gastric emptying leading to destruction of drugs.
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Distribution
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The movement of drugs throughout the body. Dependent upon blood flow to tissues, the availability of the drug to exit the vascular system and to a lesser extent, the ability of the drug to enter the cells.
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Speed of Blood flow
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Well perfused organs such as brain, heart, kidney and liver receive most of the drug in the first few minutes. Muscle, most viscera, skin and fat are slower to receive drug, from minutes to hours.
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Diffusion into Interstitial Compartments
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rapid diffusion occurs in most areas because of permeable capillaries. E.g.. Liver capillaries have much of basement membrane exposed by slit junctions which enables rapid diffusion including large plasma proteins.
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Blood brain Barrier
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no slit junctions in brain so drugs must either pass directly through (lipid soluble) or via active transport.
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Biotransformation
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Drug metabolism. The most important consequence of metabolism is promotion of renal excretion.
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Most important factor in biotransformation
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Renal excretion
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Factors affecting biotransformation
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Induction, first pass effect, extremes of age, nutritional status, competition among drugs.
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Induction
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Some drugs, acting on the liver, can increase the rate of their own or another drug's metabolism. E.G.. Phenobarbital the classic enzyme inducer
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First Pass
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rapid inactivation of oral drugs due to liver metabolism.
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Metabolism relating to lipophilic drugs
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Lipophilic properties that promote a drug's passage through biologic membranes and subsequent access to their sites of action also hinders elimination of the drug.
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Usual biotransformation of drugs
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usually biotransformed into more polar, inactive metabolites that are easily excreted by body.
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Hepatic Metabolism
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Metabolites with increased biologic activity or even toxic properties may be created through metabolism E.G.: Tylenol has a hepatotoxic metabolite.
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Hepatotoxic definition
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chemical-driven liver damage. It is a possible side-effect of certain medications
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Excretion
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Renal, billiary, fecal, breast milk, lungs, saliva, sweat
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Renal Excretion
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glomerular filtration, proximal tubule secretion, distal tubular secretion, renal excretion
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Plasma Drug Levels
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there is a direct relationship between therapeutic and toxic responses and the amount of drug present in plasma
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MEC
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Minimum effective concentration
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MEC definition
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the plasma drug level below which therapeutic effects will not occur
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Toxic Concentration
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the plasma drug level at which toxic effects occur
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Therapeutic Window
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the range of plama drug levels falling between the MEC and the toxic concentration. Drugs with narrow range of therapeutic window are more apt to cause toxicity. Digoxin is the classic example
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Drug Half life
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the time required for the amount of drug in the body to decrease(eliminated) by 50%. Drugs with a short half-life but a long dosing interval will lose the MEC
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Plateau
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when the amount of drug eliminated between doses equals the dose administered. Average drug levels will remain constant and plateau will have been reached.
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Techniques for reducing fluctuations in plasma drug levels
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Continuous infusion (plasma levels kept constant), constant daily dose reduce size and interval of dosage.
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Loading Dose
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Large initial dose which achieve plateau rapidly
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Maintenance Dose
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small doses to maintain plateau
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Pharmacodynamics
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the study of the biochemical and physiologic effects of drugs and the molecular mechanisms by which those effects are produced. In short, what the drug does to the body.
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Dose Response Relationship
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Graded relationships. As the dosage increases the response becomes greater
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Maximal Efficacy
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the largest effect a drug can produce
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Potency
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the amount of drug that must be given to elicit a response
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Drug Receptor
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any functional macromolecule in a cell to which a drug binds to produce its effect
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Receptor Compatibility
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the ability of a drug to bind to it's receptor depends on the size and shape of the drug and it’s receptor, a single receptor can be responsible for regulating several physiologic activities. Drugs mimic or block the actions of the body's own regulatory mechanisms.
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Intrinsic Activity
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the ability of a drug to activate a receptor following binding and is linked to efficacy.
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Agonist
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drugs that bind with and activate receptors.
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Antagonists
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drugs with affinity for receptors but no intrinsic activity
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Tachyphylaxis
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reduction in responsiveness brought on by repeated doses in short period of time. Rapid tolerance. The MEC is elevated can occur from days to weeks of administration. Metabolic tolerance is caused by the effects of the enzyme induction on drugs. Accelerated metabolism can occur after days or weeks.
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Additive Effect
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2 drugs with similar properties are taken together.1+1=2 E.G. aspirin and codeine boost analgesic properties if taken together
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Synergistic Effect
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The response of two drugs taken together is greater than the response of the same drugs taken alone. 1+1=3 E.G. lasix and beta-blockers. Lasix removes fluid and b-blockers block vasoconstriction causing a sharp decrease in bp
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Antagonism
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One drug inhibits the effect of another. 1+1=0 Vitimin K given to inhibit bleeding from warfarin or Nalazone to antagonize morphine induced respiratory depression
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Lipophillic Drug Metabolism
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Lipophilic properties that promote a drug's passage through biologic membranes and subsequent access to their sites of action also hinders elimination of the drug.
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Penicillin Types
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Many Variations Penicillin G: IV or IV only aqueous preparations may be given IV, Penicllin V only Oral.
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Penicillin Action
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Bactericidal: inhibits synthesis of cell wall, indicated in infections caused by susceptible organizms, treatment for respiratory, genitourinary and gastrointestinal infections
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Antibiotic Commonalities
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All antibiotics have potential for renal toxicity, diarrhea and hypersensitivity
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Bacteriostatic
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Inhibits growth but does not kill
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Penicillin Contraindications
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hypersensitivity, drug interactions, can decrease effectiveness of oral contraceptives
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Penicillin: Nursing Implications
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Hypersensitivity reactions: risk for injury, Renal impairment: risk for, Knowledge deficit: home care administration
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Penicillin Patient Teaching
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Do not take any penicillin or derivative (cephalosporin) if allergic, complete full course of drug for greater effectiveness, follow dosing instructions very carefully. Take most PCN on empty stomach, take each dose w/ full glass of water, shake liquids well, report s&s of allergic reactions immediately and do not take w/ fruit juices.
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Peak and Trough Values
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Determine dose and time drug is to be given based on therapeutic levels
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Cultures
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Usually taken 30 mins after dose and then 30 mins before next scheduled dose. Help to determine dosage. Temp at which to take cultures varies from facility to facility
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Antibiotics-Renal Toxicity
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If BUN and creatinine levels are outside of normal range then the kidney ability to excrete wastes may be impaired.
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(Lanoxin)Digoxin Classification/Action
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Cardiac glycoside. Digitalis is naturally occuring. Increases the force of contractions and decreases hr. Increases CO and blood flow to kidneys and promotes diuresis.
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Ionotroph
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force of contraction
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Chronotroph
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heart rate
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Lanoxin indications
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Heart failure, atrial arrhythmias,
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Lanoxin Administration
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Oral or IV
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Lanoxin Toxicity
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rapid loading or digitalization (in order to reach plateau), impaired renal function, age extremes, electrolyte imbalance especially hypokalemia and also hypomagnesemia and hypercalemia
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Lanoxin S&S of toxicity
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nausea, diarrhea vomiting, visual changes (colored halo), arrhythmias.
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Lanoxin related labs
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digoxin level, BUN, creatinine, electrolytes.
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Digoxin Toxicity
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therapeutic range 0.8-2.0 ng/ml.
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Digoxin Antagonist
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Digibind. Digoxin immune fab.
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Digoxin Patient Teaching
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Pulse, consult health care provider before taking any other meds, avoid taking missed dose, therapeutic effect is decreased with antacids.
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Captopril/Capoten Classification
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Antihypertensive/ACE inhibitor
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Captopril/Capoten Action
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reduces the levels of angiotensin II thereby dilating blood vessels and lowering bp
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Captopril/Capoten Indication
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For mild to severe hypertension. More effective in young caucasians than in young African Americans (fare better with combo therapy of diruetics and ace inhibitors).
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Captopril Side Effects
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dry hacking cough (sensitivity in cough center), first dose syncope (bp decreases and fainting after 1st dose or rapid increase in dose), hyperkalemia
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Captopril Toxic Effects
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Angioedema- swelling of mucosa and submucosa in face, lips, tongue and potentially hands.
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Captopril Nursing Implications
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Administer 1 hr before meals, monitor bp for first dose syncope, intruct pt to lie down after first dose or after rapid increase in dose, adequate hydration, monitor K levels.
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Metoprolol (Lopressor) classification
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Beta-Adrenergic blocker. Prevents B-adrenergic receptors from responding to sympathetic nerve impulses. Meta analyst may prevent MI
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Metoprolol (Lopressor) Action
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Decreses hr, decreases force of contraction, cardiac output, conduction and bp. May cause bronchoconstriction and may decrease glucose metabolism
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Metoprolol Indications
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Angina, hypertension, arrhythmias, MI
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Metoprolol Side Effects
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hypoglycemia, severe bradycardia, airway resistance/pulmonary edema, headache, flush dizziness, severe bradycardia, bronchoconstriction, nausea, vomiting diarrhea
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CMP
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Complete metabolic profile. Blood glucose, BUN, creatinine, lytes.
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Metoprolol Nursing Implications
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Monitor hr/bp and report significant changes. Instruct pt to report dizziness, fainting, edema, respiratory problems. Take before meals. Diabetic pt can expect insulin changes, Abrupt withdrawal can lead to rebound sympathetic overactivity (rebound htn), monitor labs cbc, cmp.
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Furosemide (Lasix) Classification
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Loop diuretic
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Furosemide (lasix) Action
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reduces the body's total water and salt by increasing urinary secretion
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Lasix Indications
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Fluid volume excess
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Lasix Contraindications
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electrolyte depletion, allergy (sulfonamide)
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Lasix Side Effects
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Ototoxicity (ringing), hypokalemia, hypotension, photosensitivity, diarrhea, muscle spasms
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Lasix Nursing Implications
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Monitor I&O, weight and vitals. Teach pt to report s&s of ototoxicity. Monitor cmp. Sunscreen.
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Nitroglycerine Classification
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Organic Nitrate, Oral (Iserdil), IV, sublingual, transdermal
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Nitroglycerine action
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Acts directly on smooth muscle to promote venous dilation, decreases venous return, decreases oxygen demand by decreasing workload
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NTG side effects
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headache, hypotension, tachycardia (rare), tolerance
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NTG Nursing Implications
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Observe for relief of acute chest pain, teaching regarding diet, weight, lifestyle factors related to angina, teaching regarding compliance with drug therapy
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Heparin Classification
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anticoagulant. IV or sub q. First Pass drug. One and 1/2 to 2 times control is usualy considered therapeutic
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Heparin Action
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disrupts production of fibrin thereby disrupting the coagulation cascade. Inhibits formation of clots but does not bust old ones up. Immediate after IV and w/in 20 minutes of sub-q
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Heparin Indications
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prevention of DVT, and pulmonary embolism in susceptible pt. Prevention of clotting during cardiac surgery, dialysis.
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Heparin Lab
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PTT
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Heparin Antagonist
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protamine sulfate
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Heparin Contraindications
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bleeding, high risk for bleeding, vitamin k deficiency, severe hypertension, advanced kidney or liver disease.
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Warfarin Classification
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anticoagulant.
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Warfarin Action
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acts in liver to prevent synthesis of vitamin K dependent factors. Onset is 3-5 days after administration
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Warfarin Antagonist
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Aqua-Mephyton (vitamin K)
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Warfarin Indications
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long term prevention of thromboembolic disorders
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Warfarin Contraindications
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bleeding, high risk for bleeding, vitamin k deficiency, severe hypertension, advanced kidney or liver disease.
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Warfarin Labs
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PT and INR (weekly for the first month) dose adjustment highly individual, Range of 2:3 is acceptable
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Enoxaparin (Lovenox)
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Low molecular weight heparin sq admin.
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Lovenox Antagonist
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protamine sulfate
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Lovenox Lab
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Does not require lab monitoring
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Anticoagulants Nursing Implications
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Monitor I&O, monitor labs, monitor for bleeding, instruct pt to report bleeding
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Phenytoin (dilantin) Classification
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Anticonvulsant or antiepileptic drug
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Dilantin Action
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Stabilization of neuronal membranes thereby limiting spread of seizure activity.
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Dilantin Indication
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Prophylaxis and Rx of grand mal seizures
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Dilantin Administration
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Oral or IV (can cause hypotension IV), Long half life. Not compatible with anything in IV line only saline. Mixing causes chalky precipitate.
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Dilantin Contraindications
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Heart block, dilantin slows blood flow/ hr. May increase blood glucose caution in diabetics, concurrent use of antacids may decrease efficacy.
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Dilantin Nursing Implications
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Adverse effects (GI, CNS) most likely to occur in geriatric population
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Dilantin Labs
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Dilantin level, hepatic profile (highly metabolized in liver), cbc. Flush IV before admin.
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Dilantin Patient Teaching
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proper dose, compliance with therapy, if dose is missed do not double up, avoid abrupt discontinuation, avoid alcohol. Take immediately after meals.
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Sodium Bicarbonate Special Note
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Not compatible with other drugs IV
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Zofran (Ondansetron) Classification
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Antiemetic
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Zofran Action
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blocks central serotonin receptors thus blocking the vomiting center.
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Zofran Indications
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Emetogenic cancer therapy as well as other causes of NV (used pre-op and/or post-op)
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Zofran Nursing Indications
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Management of possible headache, management of constipation, report cv symptoms
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Zofran Side Effects
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constipation, headache common, cardiovascular changes
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Insulin Classifications
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Parenteral antidiabetic agent/ hormone
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Insulin Action
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promotes the uptake of glucose by cells as well as other functions related to carbohydrate metabolism
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Insulin Types (examples)
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regular (rapid onset short duration), Lispro (humalog) rapid shorter acting analog of regular, Neutral Protamine Hagedorn (NPH) intermediate acting, Ultralente: long acting, Glargine (Lantus) long acting
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Insulin
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100 units per ml. Regular only insulin given IV. Rotate sites, monitor blood glucose levels.
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Insulin Nursing Implications
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Most serious consequence of insulin therapy is overdose manifested by: profuse diaphoresis, confusion, irritability, incoherent speech, hunger, headache, palpitations, tachycardia, blurred vision, convulsions and coma
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Insulin Patient Teaching
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administration, diet, carry quick form of carbohydrate, Sx hypoglycemia, identification
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Albuterol (Ventolin)
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Beta 2 Agonist, stimulates the Beta 2 receptors to relax smooth muscle in bronchioles.
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Albuterol Adverse
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tremors, tachycardia
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Prednisone Classification
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Glucocorticoid
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Prednisone Action
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Increases synthesis of glucose, suppresses immune response
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Prednisone Indications
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RA, asthma
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Prednisone Adverse affects
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Poor wound healing, hyperglycemia, electrolyte imbalances.
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Prednisone Nursing Implications
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monitor for hyperglycemia
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