increased # of enzymes, increased intrinsic? activity increased rate of metabolism = increase metabolic rate decrease amount of purest? drug 4. IV drug 1st order kinetic Q 3hrs. 9 hrs later Cp (plasma conc) = 3mcg/L. What was initial Cp of drug? = 9 hrs = 3 (t1/2 – half life) x 2=6; 6 x2=12 (2nd half life); 12×2=24 (1st half life) 5. Drug A 80% plasma protein bound w/ very low therapeutic index, Drug B 99% plasma protein = the risk of ADReaction will be more/increased w/ Drug A. So lower the % the higher the ADR risk 6. Basic (alkalinic) Drug Z pKa (pH) 8.0. not metabolized, undergoes renal elimination = True statement – acidification of urine will increase renal elimination/excretion of Drug Z 7. Presence of good slows reabsorption of Antibiotic Tab = a &b (decreases rate of absorption of Antibiotic; Takes longer to reach Therapeutic plasma levels of Antibiotics 8. BEST measure of Total amount of oral drug in plasma over time = AUC (area under the curve) 9. 10mg LOWOUCH IV for pain f=0.2, PO amount needed = 10/0.2= 50mg ****PO amt always IV amt for same drug 10. Renal clearance of 4 days: 0.90, 0.03, 0.62, 0.18, shortest t1/2(half life) = 0.90 L/hr/kg 11. EXAM 2 Notes Module/Exam 2 Weeks 4-6 ANS Quiz NURS 531 Pharm Endocrine/Autonomics: stion 1 0.2 out of 0.2 points Among the regimens listed below using various insulin preparations delivered subcutaneously by injection but not by pump, which would be the most logical? Selected Answer: b. Glargine to provide basal insulin coverage and aspart given before each meal. Answers: a. Lispro to provide basal insulin coverage and detimir given before each meal. b. Glargine to provide basal insulin coverage and aspart given before each meal. c. Detemir to provide basal insulin coverage and NPH insulin before each meal. d. Lispro or glargine injected every 3 hours and NPH given at bedtime. Question 2 0.2 out of 0.2 points Mr. P self-medicates with an aluminum hydroxide antacid before every meal to reduce symptoms of hyperacidity. However he tends to overeat and drink. As a result, he ends up taking a couple of aspirin every day. Which of the following is likely to be TRUE with regard to Mr. Ps self-medication with these over-the-counter medications? Selected Answer: c. Mr. P. will experience reduced therapeutic effects from the antacid because he is not taking it at the optimal time. Answers: a. More aspirin will be absorbed in the presence of the antacid. b. Mr P. is likely to experience diarrhea. c. Mr. P. will experience reduced therapeutic effects from the antacid because he is not taking it at the optimal time. d. Mr. P. sometimes takes other types of antacids because one antacid is the same as another with regard to adverse effects. Question 3 0.2 out of 0.2 points Which of the following statement(s) is/are TRUE about treatment of erectile dysfunction with a phosphodiesterase type 5 inhibitors? (Hint:You may choose more than one answer.) b. Phosphodiesterase type 5 inhibitors decrease the degradation of cyclicGMP. c. Among the phosphodiesterase type 5 inhibitors, tadalafil has the longest half-life. d. Use of phosphodiesterase type 5 inhibitors can result in visual disturbances and hypotension because these inhibitors are not absolutely selective for the phosphodiesterase type 5 isoform. Answers: a. Phosphodiesterase type 5 inhibitors stimulate nitric oxide synthase. b. Phosphodiesterase type 5 inhibitors decrease the degradation of cyclicGMP. c. Among the phosphodiesterase type 5 inhibitors, tadalafil has the longest half-life. d. Use of phosphodiesterase type 5 inhibitors can result in visual disturbances and hypotension because these inhibitors are not absolutely selective for the phosphodiesterase type 5 isoform. e. Only sildenafil can be taken with an organic nitrate. Question 4 0.2 out of 0.2 points Anna is an APN is treating a 58 year-old postmenopausal patient for severe osteoporosis. Consider the following and select one answer. e. All of the above actions are incorrect. Answers: a. Anna prescribes 2 drugs. She prescribes alendronate and raloxifene because the mechanism of alendronate is anabolic and the mechanism of raloxifene is anti-resorptive. b. Anna suggests that her patient should eat a large meal before taking alendronate to reduce potential gastrointestinal side effects of the drug. c. Anna orders liver function test for 6 months and 12 months after initiating therapy to treat osteoporosis because bisphosphonates are metabolized in the liver where they form a reactive metabolite that can injure liver cells. d. Because bisphosphonates can cause hypercalcemia, Anna suggests that her patient should refrain from drinking milk or eating foods like yogurt and ice cream. e. All of the above actions are incorrect. Question 5 0.2 out of 0.2 points Match the mechanism of action with the drug o Question Correct Match Selected Match Glyburide e. Stimulates insulin secretion by binding to beta-cell sulfonylurea receptor e. Stimulates insulin secretion by binding to beta-cell sulfonylurea receptor Pioglitazone a. Act as a PPAR-gamma agonists to reduce insulin resistance a. Act as a PPAR-gamma agonists to reduce insulin resistance Metformin d. Delays glucose absorption from gut, reduces gluconeogenesis, reduces glycogenolysis, facilitates insulin-mediated glucose utilization d. Delays glucose absorption from gut, reduces gluconeogenesis, reduces glycogenolysis, facilitates insulin-mediated glucose utilization Exenatide b. Synthetic GLP-1 mimetic – enhances glucose-dependent insulin secretion, suppresses inappropriately elevated serum glucose concentrations, and delays gastric emptying b. Synthetic GLP-1 mimetic – enhances glucose-dependent insulin secretion, suppresses inappropriately elevated serum glucose concentrations, and delays gastric emptying Acarbose c. Delays the absorption of glucose from the intestines by inhibiting glucosidase in the wall of the intestines c. Delays the absorption of glucose from the intestines by inhibiting glucosidase in the wall of the intestines o o All Answer Choices a. Act as a PPAR-gamma agonists to reduce insulin resistance b. Synthetic GLP-1 mimetic – enhances glucose-dependent insulin secretion, suppresses inappropriately elevated serum glucose concentrations, and delays gastric emptying c. Delays the absorption of glucose from the intestines by inhibiting glucosidase in the wall of the intestines d. Delays glucose absorption from gut, reduces gluconeogenesis, reduces glycogenolysis, facilitates insulin-mediated glucose utilization e. Stimulates insulin secretion by binding to beta-cell sulfonylurea receptor Question 6 0.2 out of 0.2 points Which of the following statements are TRUE about histamine2-receptor antagonists in the treatment of hyperactivity and uncomplicated gastroesophageal reflux disease (GERD)? Selected Answer: c. For optimal response, H2 antagonists should be taken in the evening. Answers: a. Blocking the H2 receptor blocks the final common pathway of acid production in parietal cells. b. H2 receptor antagonists protect the stomach lining by increasing mucus production. c. For optimal response, H2 antagonists should be taken in the evening. d. Among the H2 antagonists, cimetidine has the least number of adverse effects. Question 7 0.2 out of 0.2 points Which of the following statements is TRUE with regard the ideal anti-muscarinic drug to treating overactive bladder (OAB)? Selected Answer: d. The ideal anti-muscarinic drug would be highly selective for the M3 receptor and would not cross the blood brain barrier. Answers: a. The ideal anti-muscarinic drug would be highly selective for the M2 receptor subtype. b. The ideal anti-muscarinic drug would be a tertiary amine. c. The ideal drug already exists. Current anti-muscarinics on the market are very effective. d. The ideal anti-muscarinic drug would be highly selective for the M3 receptor and would not cross the blood brain barrier. Question 8 0.2 out of 0.2 points Methimazole and propylthiouracil (PTU) are two drugs that are used to treat patients with Graves disease. What extra mechanism of action of PTU (compared to methimazole) explains the beneficial effects of PTU on patients who are experiencing severe hyperthyroidism or thyroid storm? Selected Answer: c. Only PTU inhibits conversion of T4 to T3 in periphery Answers: a. Only PTU inhibits peroxidase (oxidation of iodide to iodine) b. Only PTU inhibits coupling of iodine to tyrosine c. Only PTU inhibits conversion of T4 to T3 in periphery Question 9 0.2 out of 0.2 points RANKL (receptor activator of nuclear factor KappaB ligand) is a cell-attached ligand that is important in regulating bone remodeling. Which of the following statement is TRUE about drugs used to treat osteoporosis by decreasing RANKL action? Selected Answers: a. Osteoblasts-associated RANKL binds to the RANK receptor on osteoclasts. Answers: a. Osteoblasts-associated RANKL binds to the RANK receptor on osteoclasts. b. Bisphosphonates act as a transcription factor to increase the expression of RANKL. c. r-OPG (recombinant osterprotegrin) and denosumab bind to RANK and inhibit maturation of osteoclasts and thereby inhibit degradation of bone. d. Based on the mechanism of action of denosumab, a predicted effect of this drug would be an increase in serum calcium Question 10 0.2 out of 0.2 points Your patient is complaining that she has frequent spotting or break through bleeding since she started an oral contraceptive (OC). A common reason for this occurrence is related to: Selected Answer: taking an OC pill at different times. Answers: having multiple sexual partners. taking an OC pill at different times. the clinical and therapeutic efficacy of the drug. taking an OC pill with food. ANS Quiz module 2 ion 1 0.2 out of 0.2 points Nerve pathways from the autonomic nervous system (ANS) normally have a preganglionic and a postganglionic fiber. Which of the following properties is characteristic of ONLY the parasympathetic nervous system (PNS) but not the sympathetic nervous system (SNS)? Selected Answer: c. Acetylcholine is the primary neurotransmitter at the postganglionic fiber. Answers: a. Acetylcholine is the neurotransmitter of the preganglionic fiber. b. ATP and neuropeptide Y are co-transmitters at the postganglionic fiber. c. Acetylcholine is the primary neurotransmitter at the postganglionic fiber. d. Stimulation mediates stress, fright, flight and fright. e. Innervation of the eye, heart and lungs. Response Feedback: a) Acetylcholine is the neurotransmitter at the ganglion of both the PNS and SNS. b) ATP and neuropeptide Y are co-transmitters at adrenergic nerve terminals in the SNS. Co-transmitters ofcholinergic nerves are nitric oxide and vasoactive intestinal peptide. c) Acetylcholine is the primary neurotransmitter of PNS postganglionic fibers. Norepinephrine is the primary neurotransmitter of the ANS postganglionic fiber. d) Stimulation of the SNS mediates stress, fright, flight and fight. PNS stimulation is usually associated with relaxing or moderating activity e) Both the PNS and the SNS innervate the eye, heart and lungs. Question 2 0.2 out of 0.2 points What would be the outcome of blocking depolarization-induced influx of calcium through calcium channels in a preganglionic nerve terminal of the parasympathetic or sympathetic nervous system? Selected Answer: b. Release of neurotransmitter from the nerve terminal would be inhibited. Answers: a. Uptake of neurotransmitter from the synapse would be inhibited. b. Release of neurotransmitter from the nerve terminal would be inhibited. c. Synthesis of neurotransmitter in the nerve terminal would be inhibited. d. Binding of the neurotransmitter on the target cell/organ receptor would be facilitated. e. Neurotransmitter would be released from the presynaptic terminal by exocytosis. Response Feedback: a) Uptake may require ions to facilitate uptake but calcium is not one of the ions. * Note that inhibited does not necessarily infer that a process is totally reduced to zero or ablated. It means that the process is reduced or decreased to a varying degree. b) Release of neurotransmitter would be inhibited because depolarization induced opening of calcium channels mediates calcium influx. The influx of calcium mediates fusion of vesicles containing neurotransmitter (NT) to the cell surface membrane and exocytosis of the NT into the synapse. Without the Ca influx the NT would not be released. c) Calcium is not involved in synthesis of neurotransmitter in these nerve terminals d) Decreased calcium influx into the presynaptic membrane would have no effect on target organ receptor binding. e) If the influx of calcium were interrupted exocytosis of neurotransmitter would be inhibited. Question 3 0.2 out of 0.2 points Binding of acetylcholine to nicotinic receptors: Selected Answer: e. Results in the opening of sodium channels and the influx of sodium into the cell. Answers: a. Stimulates totally different signal transduction mechanisms at neuronal and skeletal muscle receptor sites b. Results in the inhibition of adenylate cyclase with subsequent decreased production of cAMP. c. Results in the activation of phospholipase C (PLC) with the subsequent production of inositol trisphosphate(IP3) and diacylglycerol (DAG). d. Leads to hyperpolarization of the cell membrane potential. e. Results in the opening of sodium channels and the influx of sodium into the cell. Response Feedback: a) Regardless of the location of the nicotinic receptor, binding of acetylcholine results in opening of sodium channels b) Neither activation or inhibition of adenylate cyclase is the signal transduction mechanism associated with nicotinic receptors. c) The contribution of PLC activation to nicotinic receptor signal transduction is very minimal if at all and certainly not the rule. d) Binding of acetylcholine to nicotinic receptors will result in depolarization of the cell membrane. e) Binding of acetylcholine to nicotinic receptors results in opening of Na+ channels and the influx of Na+ into the cell. Question 4 0.2 out of 0.2 points Which of the following statements best describes the consequence of norepinephrine (NE) binding to alpha2-adrenergic receptors (alpha2-AR) in the autonomic nervous system? Selected Answer: d. NE binds to presynaptic alpha2-AR, inhibits adenylase cyclase activity and diminishes the release of NE from the nerve terminal. Answers: a. NE binds to post-synaptic alpha2-AR, stimulates activation of adenylate cyclase and elicits a response in the target cell b. NE binds to post-synaptic alpha2-AR, inhibits activation of adenylate cyclase and mitigates the target cell response to other adrenergic agonists. c. NE binds to presynaptic alpha2-AR, stimulates adenylase cyclase activity and facilitates further release of NE from the nerve terminal. d. NE binds to presynaptic alpha2-AR, inhibits adenylase cyclase activity and diminishes the release of NE from the nerve terminal. e. NE binds to presynaptic alpha2-AR and stimulates the release of co-transmitters Response Feedback: It is true that NE binds to alpha2-AR. However, alpha2-AR are located on the pre-synaptic nerve terminal, inhibitsadenylate cyclase and diminishes the release of NE from the nerve terminal. This is a feedback mechanism. Question 5 0.2 out of 0.2 points Fill in the blanks of the following statements with either the word increase or decrease. Blocking reuptake of NE in an adrenergic nerve terminal would (1) ___________ the response to NE. Inhibiting acetylcholinesterase activity in cholinergic nerve terminals would (2) __________ the response to acetylcholine. Selected Answer: c. 1 = increase 2 = increase Answers: a. 1 = increase 2 = decrease b. 1 = decrease 2 = increase c. 1 = increase 2 = increase d. 1 = decrease 2 = decrease Response Feedback: Adrenergic: The main mechanism for termination of NE neurotransmission is reuptake of the neurotransmitter into the presynaptic nerve cell (reuptake 1). Blocking the reuptake of NE at the nerve terminal will result in a higher concentration of NE to bind to receptors. Therefore, the response to stimulation of an adrenergic neuron would be greater because more receptors would be bound in the target cell. Cholinergic : The main mechanism by which cholinergic transmission is terminated is by degradation ofacetylcholine into acetate and choline by acetylcholinesterase that is found in the cleft. If acetylcholinesterase were inhibited, the rate of acetylcholine degradation would be slower. Because of the slower degradation of acetylcholine, the neurotransmitter would accumulate and there would be more to bind to receptors. The greater the fraction of receptors bound the greater the response. Question 6 0.08 out of 0.2 points Match the response with stimulation of the appropriate receptor. Choose the best match. o Question Correct Match Selected Match Positive chronotropic effect on the heart b. Beta1-AR b. Beta1-AR Endothelial cell-mediated vasodilation of healthy, intact vascular a. Muscarinic (M3) e. Muscarinic (M2) Vasoconstriction of healthy, intact vasculature d. Alpha1-AR b. Beta1-AR Relaxation of bronchial smooth muscle c. Beta2-AR c. Beta2-AR Negative chronotropic effect on the heart e. Muscarinic (M2) a. Muscarinic (M3) o o All Answer Choices a. Muscarinic (M3) b. Beta1-AR c. Beta2-AR d. Alpha1-AR e. Muscarinic (M2) Response Feedback: It’s necessary to know the location and normal physiologic anticipated response when a receptor is activated. B1 + chrontropic effect on Heart; M3 Endothelial cell-mediated vasodilation of healthy, intact vascular; Alpha1-AR Vasoconstriction of healthy, intact vasculature; Beta2-AR Relaxation of bronchial smooth muscle; M2 Negative chronotropic effect on the heart. I want to point out that if the endothelium in an arteriole is injured or ablated then direct muscarinic stimulation of a vascular smooth muscle cell will cause contraction (vasoconstriction). It is also important to point out that beta2-adrenergic stimulation (by epinephrine) in skeletal muscle arterioles will cause vascular smooth muscle relaxation and vasodilation. Question 7 0.2 out of 0.2 points Early symptoms of nerve gas exposure include excessive salivation, lacrimation, urination, diarrhea/defecation, miosis (small pupil size), and fasciculation or tremors. Which of the following would best explain these symptoms? Selected Answer: b. Inhibition of degradation of acetylcholine released from cholinergic nerve terminals. Answers: a. Increased release of norepinephrine (NE) from adrenergic nerve terminals. b. Inhibition of degradation of acetylcholine released from cholinergic nerve terminals. c. Decreased depolarization of postsynaptic parasympathetic nerve fibers. d. Decreased reuptake of NE into presynaptic adrenergic nerve terminals. e. Increased acetylcholinesterase activity. Response Feedback: a) If you increase the release of NE you would be likely to observe symptoms that are the opposite of those described. b) Inhibition of degradation of acetylcholine that has been released from cholinergic nerves would result in increased Acetylcholine levels and increased occupancy of muscarinic receptors mediating symptoms characteristic of activations of the parasympathetic nervous system similar to those described in the question. In addition there would be more acetylcholine to bind to nicotinic receptors in skeletal muscle motor end plates leading to fasciculation and/or tremors. c) If depolarization of postsynaptic parasympathetic cholinergic nerves were decreased less acetylcholine neurotransmitter would be released and receptors that mediate the symptoms described in the question would not be observed. d) Decreased uptake into presynaptic adrenergic nerve terminals would result in more NE-induced stimulation of alpha- and beta-adrenergic receptors on target organs/cell. Norepinephrine does not mediate the described symptoms. e) Increased acetylcholinesterase activity would result in increased degradation of acetylcholine and thereby less acetylcholine to bind muscarinic and nicotinic receptors (see answer b) Question 8 0.2 out of 0.2 points Some target organs or cells are more influenced by either the sympathetic or parasympathetic nervous system (i.e., the target organ receives higher sympathetic or parasympathetic tone). Given this fact, if transmission at all autonomic nervous system ganglion were blocked, what change would you expect to see on the production of saliva by salivary glands? Selected Answer: c. A decrease in salivation Answers: a. No change in salivation b. An increase in salivation c. A decrease in salivation Response Feedback: General rationale: Most organs controlled by the autonomic nervous system have input from both the parasympathetic nervous system (PNS) and the sympathetic nervous system (SNS).Because ganglionic blockers block the PNS and the SNS, the effect of these drugs is influenced by the dominant tone in the organ system. Salivary glands have higher parasympathetic tone (or input) than sympathetic tone. Therefore if you blocked stimulation of both divisions of the ANS, the greatest effect you will observe will be the loss of PNS stimulation. PNS stimulation mediates increased salivation. Thus you would observe this loss or a decrease in salivation or dry mouth. Question 9 0.2 out of 0.2 points Binding of acetylcholine to muscarinic receptors on the adrenal gland results in the release of epinephrine into the bloodstream. Select the statement which correctly identifies a way in which epinephrine differs from norepinephrine. Selected Answer: e. Epinephrine has a higher affinity for the beta2-adrenergic receptor subtype than norepinephrine. Answers: a. Epinephrine has higher affinity for alpha1-adrenergic receptors than norepinephrine. b. Epinephrine is lacking a methyl group on its amine (nitrogen molecule) whereas norepinephrine has a methyl group at this position. c. Epinephrine is degraded by catechol-O-methyltransferase and monoamine oxidase whereas these enzymes do not degrade norepinephrine. d. Epinephrine crosses the blood-brain barrier whereas norepinephrine does not. e. Epinephrine has a higher affinity for the beta2-adrenergic receptor subtype than norepinephrine. Response Feedback: This is essentially a true/false question. Of the 5 statements e is true. a. Epinephrine has higher affinity for alpha 1-adrenergic receptors than norepinephrine. b. These catecholamines are structurally similar with the exception that epinephrine has a methyl group on itsamine side (nitrogen molecule) whereas norepinephrine has a hydrogen ion at this position. c. Epinephrine is degraded by catechol-O-methyltransferase and monoamine oxidase. The same enzymes degradenorepinephrine. d. Epinephrine does not cross the blood-brain barrier whereas norepinephrine acts as a neurotransmitter in the brain (important at the end of the course too). e. Epinephrine has a higher affinity for the beta2-adrenergic receptor subtype than norepinephrine. The ranked order of the drug affinity for the beta2-adrenergic receptor is IsoprotenolEpinephrineNorepinephrine. See the dose response curve for B2 receptor. Question 10 0.2 out of 0.2 points Which of the following statements correctly describes the circulatory reflex initiated by the baroreceptors in response to an episodic elevation in blood pressure? Selected Answer: c. Excitation of the baroreceptors causes a drop in blood pressure because of a decrease in peripheral vascular resistance and a decrease in cardiac output. Answers: a. Increased sympathetic stimulation causes vasodilation bringing elevated blood pressure back to normal. b. Stimulating the vagal parasympathetic center in the medulla causes an increased heart rate and strength of contraction. c. Excitation of the baroreceptors causes a drop in blood pressure because of a decrease in peripheral vascular resistance and a decrease in cardiac output. d. Heart rate increases and stroke volume increases resulting in a higher cardiac output. Response Feedback: Increased blood pressure in the carotid and aortic artery stretches the baroreceptors and initiates an increased rate of depolarization of the vagal and glossopharyngeal nerves that synapse in the cardiovascular center of the medulla. This results in activation of nerves that inhibit the vasoconstrictor center of the medulla and excite thevagal parasympathetic center. In turn this causes: (1) vasodilation of the veins and arterioles in the periphery (2) decrease in heart rate and (3) decreased strength of contraction. As a result arterial pressure is reduced by decreasing heart rate, stroke volume (thereby cardiac output) and peripheral resistance. a) Increased sympathetic stimulation would cause vasoconstriction and increase blood pressure. b) Parasympathetic stimulation decreases heart rate and strength of contraction via the vagus nerve. c) Excitation of the baroreceptors causes a drop in blood pressure because of a decrease in peripheral vascular resistance and a decrease in cardiac output. d) Heart rate increases and stroke volume increases resulting in a higher cardiac output. This sequence describes what happens with a drop in blood pressure. Quiz 1 9/18/17 This is a multiple choice quiz with 10 questions. Each correct answer is worth 1 point. This is an open book quiz with forced completion (must answer all questions at one time). You may use any resources to help you answer the questions. You may take 2 attempts to take the quiz. However, you must submit your final answers before the deadline. The submission site for this quiz will close at that time. After the deadline passes, you will have no other opportunity to submit your quiz. Question 1 0.2 out of 0.2 points An identical dose of medication was administered to a patient. The first time it was administered orally and the second time it was given intravenously. Plasma drug concentrations were measured at the same time intervals after administration of each drug. In the following Figure, the results were graphed as log of the plasma drug concentration (Cp) versus time after administration. AUCIV is the area under the curve when the drug was given intravenously and AUCPO is the area under the curve when the drug was given orally. What information can you obtain based on the Figure? Selected Answer: e. a and c Answers: a. oral bioavailability b. potency of the drug c. extent and rate of oral absorption the drug d. efficacy of the drug e. a and c Response Feedback: Bioavailability is defined as the fraction of the administered dose of a drug that reaches the systemic circulation in an active form. We define the bioavailability of a drug given intravenously as 1.0 (100%), because medications given via intravenously can avoid barriers which affect absorption. However, drugs given by routes other than IV must be absorbed and might undergo hepatic first-pass metabolism. Thus, they have a bioavailability of less than 1.0. The calculation of bioavailability is based on the ratio of the area under the concentration-time curve (AUC) for the administration route being considered (oral, IM, etc.) and the AUC obtained with IV administration. In other words – in this case the bioavailability would be AUCPO divided by AUCIV. The area under the curve also defines the extent of absorption. Question 2 0.2 out of 0.2 points A 55 year old female who has chronic renal failure due to a history of poorly controlled diabetes has a estimated glomerular filtration rate (eGFR) = 28 ml/min/ 1.73m2. Which of the following statement(s) describe pharmacokinetic issue(s) of special concern for this patient? Selected Answer: e. b and d Answers: a. The half-life of drugs cleared by glomerular filtration would be shorter. b. Plasma concentration of drugs eliminated by the kidney may be higher in this individual than those without chronic renal failure. c. Drugs cleared by biliary excretion will have a longer half-life. d. Drugs with a narrow therapeutic window that are eliminated by the kidney are more likely to cause adverse effects in this individual than in those without chronic renal failure. e. b and d Response Feedback: The clearance of drugs eliminated by the kidney are likely to be lower in a person with chronic renal failure. The glomerular filtration rate is very low as indicated by her creatinine clearance value. Half-life is the time it takes for half of the drug to be cleared from the body. Therefore if a drug is eliminated by the kidney – particularly by glomerular filtration – then the half-life will be longer. If a drug has a narrow therapeutic window then decreased elimination of the drug can result in higher plasma levels for a longer period of time and a higher probability of an adverse effect. If the drug is given chronically at a given dose and maintenance interval – it is likely that the drug will accumulate in the plasma and be even more likely to result in an adverse effect. Question 3 0.2 out of 0.2 points Ten (10) mg of Drug B is given to Mr. Anderson. Every hour, 0.5 mg of Drug B is eliminated. Therefore, drug B is eliminated by (1)_____order kinetics. However, if a constant proportion of Drug B were eliminated every hour, then Drug B would be eliminated by (2)_____order kinetics. Selected Answer: a. (1) zero; (2) first Answers: a. (1) zero; (2) first b. (1) first; (2) zero Response Feedback: In first order kinetics, the elimination of the drug is proportional to the plasma concentration. After one half-life, 50% of the drug will be eliminated. For example, if 100 mg of a drug is given, following one half-life, 50% of the drug will be eliminated, decreasing the plasma concentation to 50 mg. If 200 mg of the same drug is given, after one half-life, 50% of the drug will be eliminated, resulting in a plasma concentration of 100 mg. Regardless of the amount of drug given, after one half-life, 50% of the drug will be eliminated. In zero order kinetics, the amount of drug eliminated is the same and is independent of the drug concentration. For example, 0.5 mg of Drug B is eliminated every hour. If 10 mg of Drug B is given, after one hour, 9.5 mg of Drug B will remain in the body. If the dose is tripled and 30 mg of Drug B is given, the body still only eliminates 0.5 mg every hour. Therefore, after one hour, 29.5 mg of Drug B will remain in the body. You can see how this could lead to toxic drug levels since the body does not eliminate more of the drug when a larger dose is given. Question 4 0 out of 0.2 points Which of the following statements are FALSE regarding P-glycoprotein? Selected Answer: a. P-glycoprotein reduces transport of drugs from one side of a membrane to the other. Answers: a. P-glycoprotein reduces transport of drugs from one side of a membrane to the other. b. P-glycoprotein can be found in the brain and intestines. c. Increasing or decreasing the expression of P-glycoprotein can affect the absorption and plasma levels of drugs. d. P-glycoprotein allows for increased transportation of drugs across the intestines and blood brain barrier. Response Feedback: Recall that P-glycoproteins are efflux proteins and function as a protective barrier, which decrease transportation of drugs into intestinal cells and across blood brain barrier. They are found in multiple sites throughout the body. Changing the expression of theses transport proteins affects drugs levels. Question 5 0.2 out of 0.2 points Which are TRUE about cytochrome p450 (CYP450) enzymes? Selected Answer: e. All of the above. Answers: a. They are important for phase 1 drug metabolism. b. There is more than one isoform (isozyme) of CYP450 metabolizing enzymes and CYP3A4 & CYP2D6 are two examples CYP450 isoforms. c. CYP450 enzymes are found throughout the body, but are predominantly found in the liver and small intestine. d. CYP450 enzymes can activate pro-drugs. e. All of the above. Response Feedback: All are true statements. Pro-drugs need to be metabolized in order to be altered to their active form. Question 6 0.2 out of 0.2 points If Drug X is metabolized by the CYP3A4 enzyme and Drug Y inhibits the CYP3A4 enzyme, concomitant administration of drugs X and Y would likely cause which result? Selected Answer: a. Increase in Drug X plasma levels. Answers: a. Increase in Drug X plasma levels. b. Decrease in Drug X plasma levels. c. No change in Drug X or Drug Y plasma levels. Response Feedback: If Drug Y inhibits the enzyme required to metabolize Drug X, metabolism of Drug X will be hindered. Metabolism usually makes a drug more polar and more easily cleared from the body. If this process is inhibited the drug will be cleared more slowly
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