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This comprehensive study guide provides a detailed overview of key pharmacology concepts, including pharmacokinetics, pharmacodynamics, drug administration routes, and specific drug mechanisms of action. it features numerous questions and answers covering various aspects of drug metabolism, bioavailability, and therapeutic applications, making it an excellent resource for students preparing for exams. The guide also includes information on important clinical considerations and drug interactions.
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Prodrug - ANSWER-An inactive drug dosage form that is converted to an active metabolite by various biochemical reactions once it is inside the body. -Cytochrome P -Ex. Aspirin, psilocybin, heroin Bioavailability - ANSWER-the rate at and the extent to which a nutrient is absorbed and used -Affected by route of administration and drug dosage -Drug clearance (rate drug leaves circulation) -Steady state concentration -Affected by chemical stability, solubility, and first pass Steady state (of a drug) - ANSWER-stable level of drug in the body, occurs in 5 half lives of the drug -rate of drug being added to system is equal to amount being eliminated from system Pharmacokinetics - ANSWER-The process by which drugs are absorbed, distributed within the body, metabolized, and excreted. -what the body does to the drug First pass - ANSWER-the fact that a medication in the GI tract passes through the liver before entering other organs does not - ANSWER-bioequivalence does/does not affect bioavailability Bioequivalence - ANSWER-relative therapeutic effectiveness of chemically equivalent drugs. Bioavailability (is affected by) - ANSWER--chemical instability -solubility -first pass metabolism Cytochrome P450 - ANSWER--enzymes that function to metabolize potentially toxic compounds, including drugs and products of endogenous metabolism such as bilirubin, principally in the liver. -genetics influence presence of enzymes -affects metabolism of warfarin, antidepressants, antiepileptics, and statins. -the levels of these drugs are higher when taken with certain drugs that are
inhibitors (ex. warfarin with omeprazole) because there is competition for enzyme metabolism. -inducers lead to decreased plasma concentration of drug. cytochrome p450 inducer - ANSWER-An inducer increases the metabolism of a substrate resulting in a decreased level or effect of the substrate
inhalation - ANSWER--drug effects as rapid as IV bolus -minimizes systemic side effects of respiratory drugs
oral - ANSWER--antidotes may be provided -most common, convenient, and economical method of drug administration -most complicated drug pathway -low gastric pH inactivates some drugs -20-60 minutes for effects -enteric, extended-release enteric-coated - ANSWER--protects the drug from stomach acid -delivers to less acidic intestine -useful for drugs that are acid labile or irritating to stomach (ex. omeprazole, aspirin) extended-release - ANSWER--control drug release -maintain therapeutic range over longer period -good for drugs with short half-life (i.e. morphine with half-life of 2-4 hours) aPTT - ANSWER-activated partial thromboplastin time 30-40 seconds - ANSWER-Normal activated partial thromboplastin time (APTT) 1.5-2.5 - ANSWER-therapeutic aPTT is x more than normal aPTT low dose heparin - ANSWER--5000 units BID -does not require aPTT monitoring INR - ANSWER-international normalized ratio 2-3 (INR) - ANSWER-therapeutic INR for warfarin <1.1 - ANSWER-normal INR Dabigatran (Pradaxa) - ANSWER--direct thrombin inhibitor -anticoagulant -blood factor IIa inhibitor idarucizumab - ANSWER-antidote for dabigatran factor xa inhibitors - ANSWER-apixaban, edoxaban, rivarozaban, fondaparinux apixiban (MOA) - ANSWER--Factor Xa inhibitor -Eliquis Edoxaban (MOA) - ANSWER--Factor Xa inhibitor
Fondaparinux (MOA) - ANSWER--factor Xa inhibitor -Arixtra Pulmonary Embolism - ANSWER--usually a clot from the leg that blocks the pulmonary vasculature -affects right ventricle d/t backing up of blood -can cause pulmonary hypertension -risk factors: immobility, obesity, hormonal birth control, smoking, HTN pulmonary hypertension - ANSWER--elevated pulmonary pressure resulting from an increase in pulmonary vascular resistance to blood flow through small arteries and arterioles. -increased afterload causes increase in RV size as contractility cannot overcome the resistance CVA (risk factors) - ANSWER-HTN, HLD, DM, Smoking, FHx CVA, Hx TIA/CVA, AFib action potential - ANSWER--sodium moves into cell (depolarization) -threshold potential must be reached -potassium moves out of cell (repolarization) -returns to resting potential by pumping sodium out of cell and potassium back into cell threshold potential - ANSWER-The minimum membrane potential that must be reached in order for an action potential to be generated. absolute refractory period - ANSWER-The minimum length of time after an action potential during which another action potential cannot begin. relative refractory period - ANSWER-A period after firing when a neuron is returning to its normal polarized state and will fire again only if the incoming message is much stronger than usual caseous necrosis - ANSWER--degeneration and death of tissue with a cheese-like appearance -associated with TB tuberculosis - ANSWER--An infectious disease that may affect almost all tissues of the body, especially the lungs -airborne -caseous necrosis -1/4 of world population infected -> leading cause of death d/t infectious disease
-high risk countries include Mexico, Phillippines, Gautamala, China, Haiti, India -congregate settings such as homeless shelters are high risk, including for employees -increased in the mid 90s d/t AIDS but have decreased since 2000s
exotoxic bacteria - ANSWER--gram positive bacteria that stain purple -released from bacteria invasion period - ANSWER--when immune and inflammatory responses are initiated
pneumonia - ANSWER--infection of lower respiratory tract -sixth leading cause of death in U.S. -CAP, HCAP, HAP, VAP -HAP has 20-50% mortality -VAP occurs in up to 25% of ventilated patients -aspiration of oropharyngeal secretions is most common route of lower respiratory tract infection -most important guardian of lower respiratory tract is alveolar macrophage (Toll- like receptors) -pneumonococcus is most common and lethal cause of out/inpatient pneumonias -viral pneumonia is seasonal and usually mild and self limiting; however, pandemics... -mostly preceded by URI -pulmonary consolidation pulmonary consolidation - ANSWER-In pneumonia, the process by which the lungs become solidified as they fill with exudates. -CXR for pneumonia will show this and infiltrates. Acute bronchitis will not Upper respiratory tract (infections) - ANSWER-Sinusitis - blockage of sinuses Otitis media - infection of the middle ear Tonsillitis - inflammation of the tonsils Laryngitis - infection of the larynx that leads to loss of voice Pharyngitis - Sore throat (Antibiotics that should be) Avoided in Children - ANSWER--Tetracyclines -> teeth staining -Fluoroquinolones -> arthrotoxicity Antibodies in newborns - ANSWER--IgG passed to fetus through placenta in third trimester -colostrum and breastmilk contain IgA -passive immunity from mother -starts making own antibodies (IgM) 3-6 months after birth. There is a period when maternal antibodies are tapering off and newborn is only secreting minimal amounts of antibodies at about 3 months. -IgG levels start to rise again at around 1 year B cell (maturation) - ANSWER--Directed by bone marrow sites that harbor stromal cells, which nurture the lymphocyte stem cells and provide hormonal signals -Millions of distinct B cells develop and "home" to specific sites in the lymph nodes, spleen, and GALT -Come into contact with antigens throughout life
(types of) T cells - ANSWER-Helper T cells (CD4+): stimulates cytotoxic t cells, B cells, and macrophages to develop immune response Cytotoxic T cells (CD8+): simulates cell apopotosis Memory T cells: antigen specific t cells that retain a memory of prior infections ABO (compatibility) - ANSWER-O is universal donor; AB universal receiver respiratory acidosis (causes) - ANSWER-• Depression of the respiratory center. (1) Head injuries. (2) Oversedation with sedatives and/or narcotics.
potassium sparing diuretics (MOA) - ANSWER-Aldosterone antagonist in the distal convoluted tubule
atrial netriuretic peptide - ANSWER-acts acutely to reduce plasma volume by at least 3 mechanisms: increased renal excretion of salt and water, vasodilation, and increased vascular permeability. edema (oncotoic pressure) - ANSWER-Edema occurs when there is a decrease in plasma oncotic pressure, an increase in hydrostatic pressure, an increase in capillary permeability, or a combination of these factors. Edema also can be present when lymphatic flow is obstructed. angiotensin - ANSWER-a peptide hormone that constricts blood vessels, causes the retention of sodium and water, and produces thirst and a salt appetite amiodarone (pharmacokinetics) - ANSWER-Onset: 2-3 days (oral) Within minutes (IV) Peak Effect: 3-7 days (oral) Duration: varies Half-life: 40-55 days heart failure (patients) - ANSWER-have more than just heart failure. look for underlying angina, HTN... digoxin (and electrolytes) - ANSWER-hypomagnesemia, hypercalcemia, and hypokalemia hyperkalemia (renal failure) - ANSWER-renal failure results in elevated potassium levels because the body cannot clear the excess potassium from the blood stream through the kidneys like it normally does. hyperkalemia (addison's disease) - ANSWER-deficiency of aldosterone will result in decreased excretion of potassium hypercalcemia (treatment) - ANSWER--calcitonin, pamidronate (nitrogen containing biphosphonate compensatory hyperplasia - ANSWER-an adaptive mechanism that enables certain organs to regenerate; occurs significantly in epidermal and intestinal epithelia, hepatocytes, bone marrow cells, fibroblasts, and some bone, cartilage, and smooth muscle. naproxen - ANSWER-NSAID said for use in CAD patient NSAIDs (MOA) - ANSWER-Reversibly inhibit COX-1 & COX- Block prostaglandin synthesis
NSAID alternative - ANSWER-COX 2 inhibitors; given with risk of GI bleed (indicated by darkening stool and epigastric pain) diphenhydramine (side effects) - ANSWER-Cardiovascular: tachycardia, hypotension, palpitations Neurological: drowsiness, seizures Respiratory: mucus plugs, wheezing lortadine - ANSWER-lack of sedation and impairment of performance, longer duration of action, and absence of anticholinergic side effects. dimenhydrinate (onset of action) - ANSWER-within 15 minutes; lasts 3-6 hours (patients with history of kidney stones should) avoid - ANSWER-calcium tendon rupture - ANSWER-Fluoroquinolones have a black box warning for or tendonitis. There is an increased risk in elderly patients. Pseudomembranous colitis - ANSWER-Clindamycin, ampicillin, cephalosporins (C. diff) chronic pain - ANSWER-episode of pain that lasts for 6 months or longer; may be intermittent or continuous. NOT cancer pain