PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024, Exams of Nursing

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PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Bioequivalence Definition - CORRECT ANSWERS Pharmaceutical equivalents that display the SAME RATE and EXTENT OF ABSORPTION Means delivering the SAME AMOUNT of ACTIVE DRUG moiety to SITE OF ACTION when GENERIC or INNOVATOR drugs are administered at the same molar dose under SIMILAR CONDITIONS Therapeutic Equivalents Definition - CORRECT ANSWERS Considered equivalent when the GENERIC drugs are PHARMACEUTICAL EQUILVALENTS and show SAME EFFICACY, SAFETY PROFILE as product whose efficacy and safety has been established Pharmaceutical Equivalents Definition - CORRECT ANSWERS Considered equivalents when BOTH AGENTS contain IDENTICAL AMOUNTS of ACTIVE ingredients in the same SALT or ESTER form, ROUTE of administration and possess IDENTICAL disintegration TIMES, and DISSOLUTION rates. Clinical Judgement in Prescribing - 7 Characteristics - CORRECT ANSWERS 1. Clear Indication for drug? 2. Drug effective in treating this disorder? 3. What are the goals of taking drug? 4. What conditions determine drug IS NOT meeting goal and different therapy should be tried? 5. Duplications with other drugs patient already taking? 6. Would over-the-counter drug be as useful? 7. What about cost? Pre-Clinical - Drug Development Phases: - CORRECT ANSWERS Studies in lab (performed on cells, isolated tissues/organs, animals) Designed to provide basic safety, bioavailability, pharmacokinetic, and initial efficacy data Development of suitable formulation for clinical use Reproductive toxicology Long-term carcinogenic testing PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Phase I - Drug Development Phases: - CORRECT ANSWERS Healthy people - Volunteers: used to establish: 1. Biological effects 2. Safe Doses and tolerability 3. Pharmacokinetics 4. Pharmacodynamic effect (B/P, HR, ECG) Phase I Drug Development - How Stopped - CORRECT ANSWERS 1. Trial stopped if half-life too short or too long 2. Trial stopped with significant ECG changes, severe adverse effects 3. Trials START with sub-pharmacological doses that are escalated following multiple doses (if safe) 4. Pre-clinical data available 5. Costs: $500,000-1.5M / drug tested Phase II - Drug Development Phases: - CORRECT ANSWERS 1. Used to treat disease in a SMALL NUMBER of patients. 2. Establish the ability to IMPROVE patient outcomes Test Efficacy and Safety Phase IIa: Drug limited to single/maximal tolerated dose level. 10-100 patients Phase IIb: Follows proof of concept (Phase IIa) - Several dose levels are tested on target population (dose ranging studies) How Progresses to Phase III - Drug Development - CORRECT ANSWERS Depends on: 1. Drug efficacy relative to competitors 2. Safety profile 3. Probability of technical success and regulatory success 4. Remaining patent life of drug 5. Costs to produce 6. Market share 7 Price PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS 3. Glutamate G-Protein Receptors - CORRECT ANSWERS 1. Guanine nucleotide regulator proteins 2. Share similar structure (seven regions) of protein span. 3. Create a POCKET where drugs bind 4. End with "TAIL" inside the cell 5. Individual [x]-proteins have general structure and DIFFER in their BINDING site and the intracellular portions that [x] proteins CONTROL after the drug is bound. G-Protein (2nd Messenger) Examples - CORRECT ANSWERS 1. cAMP - cyclic adenosine monophosphate 2. Ca++ phosphoinositide Diacylglycerols G-Protein Phosphorylate - CORRECT ANSWERS [x]-Protein receptor makes INTRACELLULAR parts of receptor AVAILABLE for phosphorylate G-Protein Sub-Units (3 Total) - CORRECT ANSWERS 1. Alpha 2. Beta 3. Gamma Transmembrane Receptors Definition and Action - CORRECT ANSWERS 1. Consist of Extracellular hormone-binding domain AND an Intracellular ENZYME domain that phosphorylates the amino acid TYROSINE 2. Hormone binds to receptor == enzyme activation sustains effect Transmembrane Receptors for: - CORRECT ANSWERS 1. Insulin 2. Epidermal growth factor 3. Platelet-derived growth factor Intracellular Receptors Definition - CORRECT ANSWERS 1. Regulate gene expressions 2. Lipid-soluble hormones pass through the cell membrane and bind to intracellular receptors PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Intracellular Receptors - Action once Bound - CORRECT ANSWERS 1. Displaces stabilizing protein 2. Permits receptor to FOLD into it's ACTIVE conformation 3. Receptor MOVES to nucleus 4. In nucleus controls CONSCRIPTION of GENES by binding specific DNA Hormone Receptor Types DNA Hormone Receptors Five Types - CORRECT ANSWERS 1. Corticosteroids 2. Mineralocorticoids 3. Sex steroids 4. Vitamin D 5. Thyroid hormones Role of Enzymes at Receptor Sites - CORRECT ANSWERS 1. Bind to substrates 2. Speed up biochemical reactions 3. Drugs can act to stimulate OR inhibit specific [xx] Agonist Definition - CORRECT ANSWERS Drugs that produce RECEPTOR STIMULATION and a CONFORMATIONAL change EVERY TIME they bind Have affinity and efficacy May demonstrate downregulation or desensitization. **Know what the receptor normally does Antagonist Definition - CORRECT ANSWERS 1. Drugs that OCCUPY receptors WITHOUT stimulating them. 2. They produce NO DIRECT response 3. The response occurs from INHIBITING receptor stimulation (e.g., Beta-Blockers at beta- adrenoceptor) Affinity to BIND, no Efficacy (don't create effect) PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS **Know what the receptor normally does Types of Antagonists - CORRECT ANSWERS 1. Competitive Reversible 2. Irreversible 3. Partial Agonists (part agonist - part antagonists) - they stimulate only SOME of the receptors Phase I Metabolism Definition - CORRECT ANSWERS 1. Results in metabolites with Greater or Lesser pharmacological activity 2. Many are Rapidly Eliminated 3. Others go on to next phase reactions Are non-synthetic reactions (CYP-450) 1. Oxidation 2. Reduction 3. Hydrolysis Phase II Metabolism Definition - CORRECT ANSWERS 1. Called synthetic or conjugated reactions because drug molecules metabolized 2. Leads to something being Added to the drug to Synthesize New Compound 3. Metabolites are LINKED to highly charged (Polar) molecules 4. Conjugation to charged molecules MAKES metabolites MORE Water Soluble and EASIER to be Excreted by kidneys Are Synthetic reactions - Glucuronidation CYP P450 Enzyme Metabolism - CORRECT ANSWERS 1. Responsible for metabolism of the largest number of drugs. 2. May vary based on genetics, and age (levels of enzymes different in children based on age) PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Metabolizes: 1. Theophylline CYP2D6 - CORRECT ANSWERS 1. Primarily in liver 2. Required to convert opioids (e.g., codeine) into morphine (ProDrug example) Beta-Blockers are substrate Example of Inhibitor (metabolizes faster): Cimetidine, Amiodarone, Labetalol Example of Inducers (more drug available): Carbamazepine, Phenytoin, Phenobarbital, Rifampin If an Alpha 1 Receptors is STIMULATED, what happens? Use G1 protein - CORRECT ANSWERS Vascular & GU smooth muscle contraction (excite or stimulate) Arterioles = vasoconstriction Eyes = dilate Bladder = contraction, urinary retention Liver = Glycogenolysis (glycogen to glucose-1) Kidneys = Decreased Renin Block Receptor = Orthostatic Hypotension, reflex tachycardia (blood vessel relationship) Catecholamines (Adrenergic Agonists) - CORRECT ANSWERS Oral route = ineffective Duration of Action = short CNS penetration = poor Noncatecholamines (Adrenergic Agonists) - CORRECT ANSWERS Oral route = effective Duration of action = long PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS CNS penetration = good Epinephrine (Direct Acting Non-Selective Agonist) - CORRECT ANSWERS Stimulates all four types of receptors (Alpha 1, Alpha 2, Beta 1, Beta 2) Sympathetic system neurotransmitter What is Epinephrine used to treat? - CORRECT ANSWERS Treat: 1. Cardiac arrest, cardiogenic shock, severe hypotension How does Epinephrine work (mechanism of action)? - CORRECT ANSWERS Direct acting, non- selective (many receptors) Mechanism of action: A1 = vascular smooth muscle contraction A2 (dec. cAMP) = feedback inhibition of neurotransmitter release B1 (inc. cAMP) = Increase HR & inotropy (contractions) = Cardiac output Increase B/P, HR, contractility, and Cardiac Output Bronchodilation B2 (inc. cAMP) = smooth muscle relaxation: bronchial, vascular What are the side effects of Epinephrine? - CORRECT ANSWERS Precipitate myocardial ischemia or infarction (inc. cardiac work), arrhythmias What are the contraindications of Epinephrine - CORRECT ANSWERS Narrow angle glaucoma. Use with caution in pts with coronary disease What is patient education for Epinephrine (Epi-Pens)? - CORRECT ANSWERS Do not inject in hands or feet, or digits or in vein Injection in buttocks may not provide relief Norepinephrine (NE) - CORRECT ANSWERS Stimulate Alpha 1, Alpha 2, and Beta 1 receptors PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Sympathetic system neurotransmitter What is Norepinephrine used to treat? - CORRECT ANSWERS 1. Blood pressure control - acute hypotensive states 2. Adjunct treatment for cardiac arrest with profound hypotension How does Norepinephrine work? (Mechanism of Action) - CORRECT ANSWERS Stimulate Alpha 1, Alpha 2, and Beta 1 receptors Direct acting; Non-selective Mechanism of action: Amine derived from tyrosine. Lacks methyl group Low doses = Beta 1 effect more pronounced (increased cardiac output) High doses = Alpha 1 effects dominate (vasoconstriction, systemic vascular resistance) What are the side effects of Norepinephrine? - CORRECT ANSWERS Excessive vasoconstriction decreased end-organ perfusion decreased hepatic blood flow pulmonary vascular resistance reflex bradycardia decreased cardiac output. Alpha 1 Receptor locations - CORRECT ANSWERS 1. Radial muscle (eyes) = dilate 2. Salivary glands = secrete K+ and water 3. Arterioles (coronary, skin/mucosa, skeletal muscles, cerebral, pulmonary, renal) = constriction 4. Veins (systemic) = constriction 5. Bronchial muscles = relaxation 6. Bronchial glands increase secretions 7. GI Motility = decrease 8. GI Sphincters = contraction PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS What do you treat with Alpha-1 Antagonist (Blocker) (-osin or -sin suffix) - CORRECT ANSWERS 1. Benign prostate hypertrophy (BPH) 2. Hypertension 3. Raynaud phenomenon (vasospasm can lead to digital ischemia) What is the mechanism of action of Alpha-1 Antagonists (selective) (-osin or -sin suffix) What happens when and Alpha-1 receptor is blocked from being stimulated? - CORRECT ANSWERS 1. Arteriolar and venous vasodilation 2. Inhibits smooth muscle contraction in prostate What are the side effects of a selective Alpha-1 Antagonist (blocker)? (-osin or -sin suffix) What happens when the Alpha-1 Antagonist action EXCEEDS the therapeutic threshold and causes a side effect? - CORRECT ANSWERS Side Effects: Orthostatic hypotension, syncope, dry mouth, nightmares, sexual disfunction, lethargy Cautions: If B/P is less than 120/80 - skip the dose 1st dose phenomenon (orthostatic hypotension) Drug-Drug Interactions: - Alcholol (many of the -osin, -sin drugs) Prozosin = Beta-adrenergic blockers, Clonidine, Indomethacin Tamsulosin = cimetidine Terazosin = NSAIDs, sympathomimetics, estrogens, verapramil How should you educate patients regarding A1 Antagonists PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS (-osin or -sin suffix) - CORRECT ANSWERS - Take as exactly as prescribed, same time of day - Avoid NSAIDs - If for BPH, teach s/s of BPH to monitor for - Lifestyle factors if for HTN (weight, diet) How do Alpha 2 Receptors (G1 protein) work on the body? (think inhibition) - CORRECT ANSWERS Inhibition NE (norepinephrine) release (primarily a CNS response) Presynaptic nerve terminals of smooth muscles Decrease heart rate, blood flow, peripheral resistance, Renal vascular resistance. Platelets = aggregation Lipocytes = inhibit lipolysis Pancreas = decrease insulin Alpha 2 Receptors - Organ Locations (all) - CORRECT ANSWERS 1. Skin/mucosa arterioles = constriction 2. Platelets = aggregation 3. Liver = glycogenolysis, and gluconeogenesis 4· Pancreas (islet cells) = decrease secretions (insulin) 5. Fat cells = inhibition lipolysis What are examples of Centrally Acting Alpha-2 Agonists? - CORRECT ANSWERS Clonidine (Catapress) Methyldopa Others mentioned in Chpt 11: Guanabenz PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Guanfacine What patient education should you give for centrally acting A2 Agonists? - CORRECT ANSWERS - Take as prescribed - Take missed doses ASAP - Do not double doses - These drugs to be withdrawn slowly over 2-3 days (rebound hypertension) - Proper patch placement - Lifestyle management for HTN control Methyldopa - interactions with herbs (ask about herbal use) What is Clonidine (Catapress) used to treat? - CORRECT ANSWERS 1. Antihypertensive 2. Opioid withdrawal 3. Antidiarrheal in patients with autonomic neuropathy (increases NaCl and decreases bicarb (HCO3-) 4. ADHD How does Clonidine (Catapress) work? - CORRECT ANSWERS Downregulates norepinephrine release. Binds to receptors in CNS (imidazoline receptors) = antihypertensive effect IV dose = vasoconstriction & hypertension followed by hypotension (pre-synaptic response) Oral dose = accumulates in CNS (CV control center) = suppresses sympathetic outflow What are the side effects of Clonidine (Catapress)? What happens when the inhibitory actions (A2-central agonist) exceed the therapeutic threshold and cause a reaction? - CORRECT ANSWERS Abrupt stop = rebound hypertension (taper drug gradually). Dry mouth, sedation, sexual dysfunction. Drug-Drug Interaction: PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Is a Prodrug - converted to morphine by CYP2D6 enzyme What is cocaine used to treat? - CORRECT ANSWERS Local anesthetic How does cocaine work on the body? - CORRECT ANSWERS Blocks reuptake of catecholamines - CNS: general stimulation - CV small doses (Bradycardia); - CV moderate doses (tachycardia, vasoconstriction, arrhythmia, MI) - Local Anesthetic: Blocks Na+ ion channels - reduces nerve fiber conduction -Thermoregulation = pyrogenic What are side effects of cocaine? - CORRECT ANSWERS CV: myocardial ischemia, coronary vasospasm, fatal arrhythmias. High potential for abuse What drug is an example of an indirect acting agonist that is an MOA inhibitor? - CORRECT ANSWERS Selegiline (Deprenyl) What is Selegiline (Deprenyl) used to treat? - CORRECT ANSWERS 1. Parkinsons Disease 2. Major depressive disorder (transdermal patch) 3. ADHD (off-label) How does Selegiline (Deprenyl) work? - CORRECT ANSWERS Selectively metabolizes dopamine. Irreversible inhibitor. What are the side effects of Selegiline (Deprenyl)? - CORRECT ANSWERS Severe: Hypertensive crisis, if eats with food/drink rich in tyramine (smoked or processed meats, fermented foods, soy products). Orthostatic hypotension, arrhythmias, hallucinations, extrapyramidal symptoms, sudden sleep episodes, mental status changes PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Common: xerostomia (dry mouth), constipation (anticholinergic effects). Headaches, dizziness, insomnia, nausea Caution: Do not stop abruptly (antidepressant, anti-parkinsonian discontinuation syndromes) What are the contraindications for Selegiline (Deprenyl)? - CORRECT ANSWERS Do not give within 10 days of elective surgery (blood pressure effects) What education should you give to someone taking Selegiline (Deprenyl) - CORRECT ANSWERS Do not stop abruptly (antidepressant, anti-parkinsonian discontinuation syndromes) Foods rich in thramine (avoid) What is an example drug for a COMT Inhibitor (indirect acting)? - CORRECT ANSWERS Entacapone (Comtan) (used in combination with Levodopa and Sinemet) What is Entacapone (Comtan) used to treat? - CORRECT ANSWERS Parkinsons Disease How does Entacapone (Comtan) work? - CORRECT ANSWERS Inhibitor of catechol o-methyl transferase (COMT), an important enzyme for degradation of Dopamine (biogenic amines) Route: oral What are the side effects of Entacapone (Comtan)? - CORRECT ANSWERS Severe: Dyskinesia Orthostatic hypotension Syncope Hallucinations, psychosis Rhabdomyolysis Fibrotic complications Colitis PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS NMS-like symptoms if rapidly discontinued Common: Dyskinesia, Hypo/hyperkinesia N&V and diarrhea, Dyspepsia, flatulence, Constipation Discolored urine Dizziness, Fatigue Hallucinations Back pain Dry mouth Dyspnea Anxiety, agitation, mood changes, confusion, compulsive behaviors Purpura What are two examples of drugs that are non-selective Alpha receptor Antagonists? - CORRECT ANSWERS Phentolamine (Regitine) - Reversible Phenoxybenzamine (Dibenzyline) - Irreversible What is Phenoxybenzamine (Dibenzyline) used to treat and how does it work? - CORRECT ANSWERS Pheochromocytomas Action: Inhibits neuronal and extraneuronal norepinephrine reuptake. Prevents catecholamines from overcoming blockade, last for days until new receptors are generated. What is Phentolamine (Regitine) used for? - CORRECT ANSWERS 1. Antihypertensive (particularly in patients with pheochromocytoma) 2. (less) sympathomimetic amine overdose; including extravasation into soft tissue PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Receptor effect: B1 = increase cAMP (increases HR and contractions) B2 = increase cAMP (vascular smooth muscle relaxant) A1 = PIP2 Cascade = vascular smooth muscle contraction (minor) Note: After 24-72 hrs = downregulation of receptors and decreasing efficacy of drug) Other: Inactivated by COMT and MAO enzymes What are the side effects of Dobutamine (Dobutrex)? - CORRECT ANSWERS Arrythmias, possible hypotension What are the contraindications of Dobutamine (Dobutrex)? - CORRECT ANSWERS Hypotension, hypertrophic cardiomyopathy What is a drug example of a non-selective Beta Agonist? - CORRECT ANSWERS Isoproterenol (Isuprel) What is Isoproterenol (Isuprel) used for? - CORRECT ANSWERS 1. Increase sinus rate, shorten QT interval (hemodynamically stable). 2. Bradycardia or heart block (emergency) while waiting for pacemaker Route: IV (metabolized in liver and other tissues by COMT) What are the side effect of Isoproterenol (Isuprel)? - CORRECT ANSWERS precipitate tachyarrhythmias, myocardial ischemia or infarction (due to increased cardiac work) What are the contraindications of Isoproterenol (Isuprel)? - CORRECT ANSWERS Patients at risk for tachyarrhythmias, those with ischemic heart disease How does Isoproterenol (Isuprel) work? - CORRECT ANSWERS Selectively stimulates Beta receptors. PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS B1 = increase HR and inotropy B2 = Vascular smooth muscle relaxation Net effect: Increase HR, increase contractility increasing cardiac output, decrease diastolic B/P Beta 2 Adrenergic Receptors - CORRECT ANSWERS 1. Increase cAMP and activate cardiac G1 under certain conditions Smooth muscles: Lungs = bronchodilation, increase secretions Arterioles/Venules = vasodilation GI/GU = decrease motility Uterus = inhibit labor Pancreas = increase insulin Beta 2 Receptor Locations (all) - CORRECT ANSWERS 1. Ciliary muscle (eye) = relaxation (far vision) 2. Arterioles (coronary, skeletal muscles, pulmonary, renal) = dilation 3. Systemic veins = dilatation 4. Bronchial muscles = relaxation 5. Bronchial glands = increase secretions 6. GI Motility = decrease 7. Liver = glycogenolysis, gluconeogenesis 8. Pancreas (Islet cells), = increase secretion 9. Ureter - detrusor muscle = relaxation 10. Uterus = smooth muscle relaxation What drugs (suffix/class) are used as Beta 2 Agonists? - CORRECT ANSWERS -terol suffix = Bronchodilators Examples: Albuterol (Proventil, Ventolin) PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Metaproterenol (Alupent) Arformoterol (Brovana) Formoterol (Foradil) Levabuterol (Xopenex) Salmeterol (Serevent) What is Albuterol (Proventil, Ventolin) and other -terol drugs used for? - CORRECT ANSWERS Bronchodilators (class) Treat: 1. Bronchospasms (asthma, bronchitis, COPD) How does Albuterol (Proventil, Ventolin) and other -terol drugs work? - CORRECT ANSWERS Stimulates adenylate cyclase, increases cAMP = relaxation of smooth muscles and bronchodilation What are the side effects of Albuterol (Proventil, Ventolin) and other -terol drugs? - CORRECT ANSWERS Skeletal muscle tremor, restlessness, apprehension, sinus tachycardia, other arrhythmias What are the contraindications of Albuterol (Proventil, Ventolin) and other -terol drugs? - CORRECT ANSWERS Caution in patients with CV disease, hyperthyroidism. Avoid concomitant use of MOA inhibitors & TCAs. Beta Blockers and diabetics - CORRECT ANSWERS Can block the common signs of hypoglycemia such as shaking or elevated heart rate. Will not block diaphoresis. Must educate patients. No Beta 2 drugs for clinical use -olol or -lol suffix - CORRECT ANSWERS Beta 1 Blocker class of medications (ANTAGONIST) How do beta-blockers work on the body? - CORRECT ANSWERS Opposite effect of stimulation (B1 receptor) 1. Heart: - SA Node = decrease heart rate; and PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Severe Asthma or COPD Prinzmetal and cocaine-induced angina (inhibits B2 vasodilation = coronary vasospasm) What patient education should be given for Beta-2 Blockers - CORRECT ANSWERS - Take drug exactly as prescribed - Do not skip doses Atenolol, metoprolol, nadolol - can take up to 8 hrs before next dose Pindolol, propranolol, timolol = up to 4 hrs before next dose Food may enhance bioavailability (propranolol, metoprolol) - take consistently with or w/o food Propranolol - can be crushed Consult doctor before taking OTC drugs; especially cold medicines (cause HTN and excessive bradycardia) If for angina and acute chest pain continues, call 911 What are examples of 1st Generation Beta Blockers? - CORRECT ANSWERS Propranolol (Inderol) -- also used for migraines Pindolol (Visken) Nadolol (Corgard) - excreted in urine unchanged Sotalol (Betapace) **Also used to treat portal hypertension What are examples of 2nd Generation Beta Blockers? - CORRECT ANSWERS Metoprolol (Lopressor) Atenolol (Tenormin) Bisoprolol (Zebeta) - longer acting Esmolol (Brevibloc) - short half-life (~10 mins); IV route Timolol (Betimil, Timoptic) - also used for glaucoma (selective, longer acting) PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Acebutolot (Sectral) - less likely to cause bradycardia; less suited for Angina What is an example of a 3rd generation Beta-Blocker? - CORRECT ANSWERS Carvedilol (Coreg) Others: Labetalol (Trandate) What is Carvedilol (Coreg) used for? - CORRECT ANSWERS Compensated Heart Failure What is Carvedilol mechanism of action? - CORRECT ANSWERS Vasodilatory effects caused by A1 and Ca++ entry blockade. Reverses increased HR, cardiac output, increased afterload, myocardial oxygen demand and ischemia What are the side effects for Carvedilol (Coreg)? - CORRECT ANSWERS Hypotension, bradycardia, bronchospasm. Can initially exacerbate heart failure symptoms if patient not compensated or if dose escalated too aggressively What are the contraindications of Carvedilol (Coreg)? - CORRECT ANSWERS Decompensated heart failure. Cholinergic Receptors - What are they? What do they do to the body? - CORRECT ANSWERS Muscarinic and Nicotinic Activated by acetylcholine When stimulated: 1. GI - motility increased 2. Cardiac - Slow heart rate; SA node firing decreased and AV node conduction/contractility decreased 3. Lung: bronchoconstriction and increased secretions 4. Bladder: contraction with relaxation of internal sphincter Drug-Drug interactions for Alpha-Beta Blockers - CORRECT ANSWERS Carvidilol = Inhibitors of CYP2D6 (cimetidine, ciprofloxacin, other quinolones, quinidine, fluoxetine, paroxetine, propafenone); Rifampin, Diphenhydramine PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Labetolol = Beta agonists, theophylline Epinephrine = Cardiac glycosides or diuretics, TCAs, MOA inhibitors, levothyroxine, antihistamines, beta-adrenergic blocking agents, alpha-adrenergic blocking agents, Ergot alkaloids Acetylcholine (Cholinergic) - CORRECT ANSWERS Parasympathetic Nervous System (PNS) Neurotransmitter Muscarinic Receptor Locations - CORRECT ANSWERS M receptors (global): Male sex organs = erection M1 receptor's location: GI (motility) = increases. M2 locations: Heart 1. SA Node = decreased heart rate, vagus arrest 2. Atria = decreased contractility; action potential duration is shortened. M3 locations: 1. Eye (radial muscle) = no effect 2. Eye (ciliary muscle) = contraction (near vision) 3. Arterioles - skeletal = dilation 4. Bronchial muscle = contraction 5. Sphincters (GI) = relaxation 6. Secretion (GI) = stimulation and increased secretions 7. Adrenal Medulla = secretion of epinephrine 8. Bladder (trigone and sphincter) = relaxes. 9. Endothelium = releases endothelium-derived relaxing factor. -chol suffix - CORRECT ANSWERS Muscarinic Agonist = stimulates muscarinic receptors **only exception suffix is pilocarpine PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Heart = increased HR Saliva = decreased Lungs = decreased secretions Sweat glands = decreased Eyes = dilation What are the side effects of Atropine? - CORRECT ANSWERS Red as a beet, blind as a bat, dry as a bone, hot as a hare, mad as a hatter = atropine flush, blurred vision, decreased secretions, hyperthermia, delirium, hallucinations What are the contraindications of Atropine? - CORRECT ANSWERS Narrow-angle glaucoma Benztropine (Antimuscarinic) overview - CORRECT ANSWERS Is lipophillic (cross BBB) Treats: Parkinson's disease (2nd or 3rd line therapy). Mechanism: Tertiary amine alkaloid - Antagonist of receptors in CNA Side Effect - Hyperthermia Contraindicated: Narrow-angle glaucoma Oxybutynin (Ditropan, Oxytrol) - Antimuscarinic Overview - CORRECT ANSWERS Competitive muscarinic acetylcholine receptor antagonist (relaxes smooth muscles of walls) Treats: Urinary incontinence Side Effects: parasympathetic blockade, pupil dilation, tachycardia, decreased GI motility and secretions Contraindications: Pyloric obstruction, retentive bladder Narrow-angle glaucoma PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Patient Education for Cholinergic Blockers - CORRECT ANSWERS - Take med as prescribed If missed dose, take ASAP unless almost time for next dose Do not double doses Benztropine - give with food Atropine, dicyclomine, propantheline - give 30-60 mins before food Lifestyle modifications (bladder training, kegal exercises, etc.) Toxicity and Muscarinic Poisoning - CORRECT ANSWERS Can occur from overdose and from ingestion of certain poisonous mushrooms S/S = abdominal cramps, salivation, flushing, N&V. Atropine = antidote SQ Muscarinic and Drug-Drug interactions - CORRECT ANSWERS Additive drug interactions w/cholinesterase inhibitors Quinidine, procainamide, and other phenothiazines (chorpromazine, thioridazine), histamine blockers... may antagonize the effects to bethanechol. AVOID concurrent dose administration Patient Education and Muscarinic Drugs - CORRECT ANSWERS To avoid nausea; take 1 hour before or 2 hours after a meal SQ only, never IM or IV. IF IM or IV = severe toxicity Notify healthcare provider if abdominal discomfort, salivation, sweating, or flushing occur. Report wheezing or breathing difficulties (Bethanechol specifically) May get dizzy if standing up quickly (hypotension). Arise slowly. Avoid exercising in hot weather; adequate intake of noncaffeinated liquids to reduce these problems. PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Nicotinic Receptor Location - CORRECT ANSWERS Adrenal Medulla = secretion of epinephrine and norepinephrine What are drug examples for direct acting nicotinic alkaloids? - CORRECT ANSWERS Nicotine Succinylcholine (Anectine) What is Nicotine used for? - CORRECT ANSWERS Smoking cessation Use orally or dermal patch What is Nicotine's mechanism of action? - CORRECT ANSWERS Prototypical agonist for nicotinic acetylcholine receptors which are ligand-gated Na+ and K+ channels. Stimulate both sympathetic and parasympathetic postganglionic neuros - releases Epinephrine (adrenal medulla) - Increases HR - Peripheral vasoconstriction - GI - increased motility and secretion - Increased respiratory rate - N&V What is the side effect from Nicotine? - CORRECT ANSWERS Dependence What is Succinylcholine (Anectine) used for? - CORRECT ANSWERS Paralysis, for brief surgical procedures How does Succinylcholine (Anectine) work? - CORRECT ANSWERS Binds nicotinic receptors; causes channels to open and the neuromuscular membrane to depolarize. IS NOT inactivated by acetylcholinesterase = prolonged depolarization What are the side effects of Succinylcholine (Anectine)? - CORRECT ANSWERS Malignant hyperthermia, hypotension, arrhythmias, respiratory collapse, increased intraocular pressure. Carbachol (Topical) - CORRECT ANSWERS Cholinergic agonist PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS GI/GU smooth muscle - increase tone, motility, sphincters relax Heart: decrease HR, contractility, and velocity thru AV node What are the side effects of Neostigmine (Prostigmin)? - CORRECT ANSWERS Precipitate tachyarrhythmias, myocardial ischemia or infarction (due to increased cardiac work) What are the contraindications of Neostigmine (Prostigmin) - CORRECT ANSWERS Patients at risk for tachyarrhythmias, those with ischemic heart disease Sarin - What is it used for? - CORRECT ANSWERS Acute poisoning - CNS: coma, respiratory depression, seizures - Muscarinic: Bradycardia, N&V, diarrhea, blurred vision, sweating, salivation Nicotinic: muscle twitching, fasciculations, weakness, flaccid paralysis Antidote: Atropine PNS Drugs - CORRECT ANSWERS Increase acetylcholine (stimulate) or BLOCK cholinesterase so that acetylcholine works better (not broken down) PNS Drugs - Stimulate Receptors - CORRECT ANSWERS 1. Glaucoma 2. Alzheimer's 3. Irritable bowel syndrome 4. Urinary retention 5. Parkinson's Muscarinic Agonist - CORRECT ANSWERS Examples: Bethanechol, Pilocarpine Increases muscle tone in the bladder to help empty Muscarinic Antagonist Actions - CORRECT ANSWERS Decreases secretions PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Decreases urination Decreases GI motility Increases heart rate Sympathetic Nervous System (SNS) Neurotransmitters - CORRECT ANSWERS Epinephrine Norepinephrine Dopamine Organs Resting Capacity - CORRECT ANSWERS 1. Maintained by opposing influences from the parasympathetic and sympathetic nervous system 2. Changes in Resting Activity a. Increase activity of PNS or SNS b. Decrease activity of opposing system (PNS or SNS) Adverse Drug Effects - CORRECT ANSWERS Target Organ: Therapeutic Effect Ancillary Organs: May have adverse effect (e.g. damage to liver, kidneys as drugs excreted) Criteria for Drug Prescribing Seven Criteria or Factors - CORRECT ANSWERS 1. Pharmacodynamic factors 2. Pharmacokinetics 3. Therapeutic Factors 4. Safety 5. Cost 6. Patient factors (e.g., previous ADRs, beliefs, current drug therapy, age, pregnancy) 7. Provider factors (ease of prescribing, monitoring, formularies) The "I Can PresCribE A Drug" Mnemonic - CORRECT ANSWERS I = Indication C = Contraindications P = Precautions PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS C = Cost/Compliance E = Efficacy A = Adverse Effects D = Drug/Duration/Direction WHO Process for Rationale Prescribing Six Steps - CORRECT ANSWERS 1. Accurate diagnosis 2. Determine therapeutic objective 3. Choose appropriate treatment - collaborate w/patient 4. Start treatment 5. Educate patient re: therapy 6. Monitor effectiveness Food, Drug, and Cosmetic Act 1906 - CORRECT ANSWERS 1. Restricts manufacturing and distribution of drugs 2. Standards for labeling and branding 3. Standards for strength and purity Food, Drug, and Cosmetic Act 1938 - CORRECT ANSWERS 1. Restricts drug alteration, misbranding 2. Restricts interstate commerce of unapproved drug 3. Created the FDA Kefauver-Harris Amendments - 1962 - CORRECT ANSWERS 1. Safety and efficacy proved BEFORE marketing 2. All drugs produced between 1938-1962 to be evaluated for safety Orphan Drug Act - 1983 - CORRECT ANSWERS Fosters orphan drug development for drugs targeting rare diseases Drug Price Competition and Patent Term Restoration Act - 1984 - CORRECT ANSWERS 1. Expands # of generic drugs for abbreviated new drug application 2. Markets drugs through bioequivalence PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Clinical Manifestations: Urticaria, Wheezing, Rhinitis, Anaphylaxis (systemic or localized) - hay ve Management = give epi, antihistamines, and corticosteroids Type II - Adverse Drug Reactions - CORRECT ANSWERS Antibody-dependent cytotoxicity (rare response) - Occurs when drug binds to cells (RBCs) and is recognized by an antibody (usually IgG) - Complement and cytotoxic T-Cells are activated Example: Heparin-induced thrombocytopenia Clinical Manifestations: Blood transfusion reactions, erythroblastosis fetalis, and autoimmune hemolytic anemia Type III Adverse Drug Reaction - CORRECT ANSWERS Immune complex hypersensitivity Occur when antibodies (IgG & IgM) are formed against soluble antigens. The antigen-antibody complexes are deposited in tissues such as joints and lungs Drug Example: Ceclor. Note that still can take PCNs and cefalosporins Example: Arthus reaction to tetanus vaccine Clinical Manifestations: Localized Arthus reactions and generalized reactions such as serum sickness, necrotizing vasculitis, glomerulonephritis, RA, and systemic lupus erythematosus Type IV Adverse Drug Reaction - CORRECT ANSWERS Cell-mediated or Delayed hypersensitivity - cytotoxic, T-cells are activated Example drug rash, eosinophilia, and systemic syndrome (DRESS) PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS - Poison Ivy, latex - With repeated exposure to drugs, a "cytokine storm" can be triggered Clinical Manifestations: Contact dermatitis, tubercular lesions, and graft rejection Treatment: Corticosteroids and other immunosuppressive agents Idosyncratic Reaction - CORRECT ANSWERS Unpredictable and may be more likely to result in mortality Intrinsic Reaction - CORRECT ANSWERS 1. Pharmacological 2. Often predictable based on the drug's mechanism of action 3. Is typically dose related Genetic Polymorphism - CORRECT ANSWERS Multiple differences of a DNA sequence found in at least 1% of the population Genetics - CORRECT ANSWERS The study of heredity and its variation Genomics - CORRECT ANSWERS The study of the complete set of genetic information present in a cell, an organism, or species Pharmacogenetics - CORRECT ANSWERS The study of the influence of HEREDITARY FACTORS on the response of individual organisms to drugs Single Nucleotide Polymorphisms (SNP) - CORRECT ANSWERS Are alterations in DNA sometimes associated with population groups Explains why certain groups of patients are MORE or LESS sensitive to certain drugs Polymorphic Variation - CORRECT ANSWERS Expressed IF the variant copy of a gene is expressed in the equivalent of 1% or more of the population PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Such as is common for genes encoding drug metabolizing enzymes (DMEs) Poor Metabolizers - Phenotype - CORRECT ANSWERS Lack a working enzyme Intermediate Metabolizers - Phenotype - CORRECT ANSWERS Are Heterogeneous for ONE working, wild-type allele (or TWO reduced function alleles) Extensive Metabolizers - Phenotype - CORRECT ANSWERS Have two normally functioning alleles Ultra-Rapid Metabolizers - CORRECT ANSWERS Have more than one functioning copy of a certain enzyme Phase I Metabolism - CORRECT ANSWERS Oxidation, Reduction, Hydrolysis (typically in the liver) with ORAL medications Phase II Metabolism - CORRECT ANSWERS Conjugate reactions that occur post Phase I metabolism Drug Effect for Poor and Intermediate Metabolizers - CORRECT ANSWERS Slow effect on metabolism Clinical Implications: 1. ProDrug will be slowly metabolized into active drug metabolite 2. May have accumulation of ProDrug 3. Active drug will be slowly metabolized into INACTIVE metabolite = potential for accumulation of ACTIVE drug Dosing: Requires lower dose of medication Drug Effect for Ultrarapid Metabolizers - CORRECT ANSWERS Prodrug rapidly metabolized into active drug. No drug adjustment needed. OR PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Steady State - CORRECT ANSWERS Reached when the concentration of the drug given routinely stays at the same level Prescription Writing - Legal Requirements - CORRECT ANSWERS All prescriptions shall conform to ALL applicable State and Federal statues, rules, and regulations Scope of Practice and Prescribing - CORRECT ANSWERS 1. Methods of treatment AND 2. Authority to ADMINISTER, DISPENSE, or PRESCRIBE are within SCOPE OF PRACTICE, of 3. Skills, Training, Education, and Competence of professional Writing a Prescription - Key Elements - CORRECT ANSWERS 1. Date 2. Legal Name 3. Address 4. Date of Birth 5. Rx (prescription abbreviation) 6. Inscription (drug name and strength) 7. Signa (patient directions) 8. Optional to include diagnosis (why giving) Provider Info 1 . Provider Legal Name, address, phone # 2. Prescribers signature and license # Drug Info 2. Generic Name of Drug; trade name in parenthesis) 3. Dosage, Dosage Regimen (written in numerals, no fractions, no decimal after whole number) 4. Route 5. Allowable substitutions Pharmacokinetics Definition - CORRECT ANSWERS dealing with the absorption, distribution through the body, metabolism, and excretion of drugs PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS WHAT the body DOES to the drug Absorption - CORRECT ANSWERS Transfer of a drug from its site of administration to the blood stream Occurs mostly through passive diffusion Factors Affecting Absorption - CORRECT ANSWERS 1. Route of administration IV - Fastest Oral - Slowest (less predictable, first pass metabolism) Sublingual/buccal = no first pass effect 2. Drug properties (lipid-solubility, pH, polority, solubility, drug formulation (tab, solution, suspension) 3. Total surface area available for absorption 4. Contact time with absorption surface **remember first pass metabolism and bioavailability Influence of pH and pKa - CORRECT ANSWERS 1. Most drugs are weak acids or weak bases 2. pKa - characteristics; determines how readily drug can cross membrane 3. The ionization of drugs MAY REDUCE their ability to permeate membranes (pH of environment & drugs pKa) 4. The ionization of drugs IS DETERMINED by dealing with the absorption, distribution through the body, metabolism, and excretion of drugs By controlling the pH of the solution drug is in OR the pKa = we can control the rate of drug transferred across the cell membrane Example: Stomach is more acidic Intestines are more basic PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS pKa of aspirin is 4.5 (weak acid) - most is absorbed in the stomach AND is pH sensitive in the small intestine per StatPearls [Internet], National Library of Medicine, 2023. pKa Definition - CORRECT ANSWERS pH at which one-half of molecules are ionized while the other half remain un-ionized Determines how readily a drug can cross membranes Henderson-Hasleback equation Distribution - CORRECT ANSWERS Passage of a drug from the circulation to the tissue and its site of action Drugs cannot create action IF not distributed to site of action in adequate concentrations. Factors Affecting Distribution - CORRECT ANSWERS Factors that are the Same as Absorption 1. Lipid-Solubility 2. Drug pH (pKa) Factors that are unique to Distribution 3. Blood flow to tissues 4. Plasma protein binding 5. Specialized barriers 6. Disease States Note: Movement continues until equalibrium achieved Active Transport - CORRECT ANSWERS Moves AGAINST the concentration gradient. Requires energy Note: Carrier proteins are specific to each molecule PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Renal Excretion and Reabsorption - CORRECT ANSWERS 1. Most common method 2. Usually removes drug that is UNBOUND and free in the plasma 3. Glomerular filtration 4. Tubular secretion and reabsorption Biliary Excretion and Reabsorption - CORRECT ANSWERS Transported by liver cells from blood to bile then enters GI tract and is excreted through feces Enterohepatic reabsorption Pharmcodynamics - CORRECT ANSWERS The action of the DRUG on the BODY 1. Receptor interactions 2. Dose response phenomena 3. Mechanism of therapeutic and toxic action Types of Drug Receptors - CORRECT ANSWERS 1. Ligand-gated ion channels Example: (e.g. cholinergic nicotinic receptors). Changes in membrane potential or ionic concentration within cell. 2. G-protein-coupled receptors Example: alpha and beta adrenoceptors. Protein Phsophorylation 3. Enzyme-linked receptors Examples: Insulin receptors. Protein AND receptor phosphrylation 4. Intracellular Receptors Example: Steroid Receptors. Protein phosphorylation AND altered gene expression Drug Response Curve - CORRECT ANSWERS Show differences in potency and efficacy PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Biological Effect = Y axis (vertical) EFFECT Log drug concentration = X axis (horizontal)... OVER TIME Therapeutic Index - CORRECT ANSWERS Graph 1. Y-Axis (vertical) = Plama concentrations 2. X-axis (horizontal) = Duration of Action Factors: 1. Onset 2. Duration of Action 3. Peak of Effect 4. Side-Effects - Sub-therapeutic - Desired response - Therapeutic window - Adverse response Pediatric Prescribing - Issues - CORRECT ANSWERS 1. Potential for ADR for hospitalized patients is 3x as high as hospitalized adults - Formulated and packaged for adults - not tested - Off label use - Less able to physiologically manage (e.g., renal, hepatic, immune functions still developing) - 12% of all prescriptions written for children < 9 years old Differences in Pediatrics from Adults - CORRECT ANSWERS 1. Drug absorption 2. Distribution 3. Biotransformation 4. Excretion/Elimination Pharmacokinetics in Children - CORRECT ANSWERS 1. Doses based on weight (mg/kg) PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS 2. Physiologic Differences - Infants have more water, less fat - Immature liver = makes fewer serum proteins, less able to metabolize drugs - Renal function not fully developed unto 30 months 3. Phase of development important 4. Drugs known to be dangerous to children ARE NOT given Pediatric Absorption - CORRECT ANSWERS 1. Gastric pH - not to adult levels until age 1 year IF acidic environment needed to absorb = less medication will be absorbed by infants 2. Children have GREATER body surface area = greater absorption of topical medications. 3. Skin MORE permeable leading to greater topical absorption. 4. Immature peripheral circulation will PREVENT absorption of IM or SQ meds Pediatric Distribution - CORRECT ANSWERS 1. Differences in Body Water and Fat 2. Immature Liver Function - Age 0-6 months: Less albumin, few plasma proteins - Fewer binding sites = higher blood concentrations of tow or more drugs OR less affinity for one of the drugs 3. Immature Blood Brain Barrier Birth: Blood brain barrier is NOT developed = greater risk of CNS toxicity; drug enters CNS Pediatrics and Phase I Metabolism (P450s) - CORRECT ANSWERS 1. CYP3A - major role in drug metabolism - CYP3A7: is present in utero, declines rapidly after birth - The rate of decline of CYP3A7 decrease through FIRST SIX months with an INCREASE in CYP3A4 and CYP3A5 - Adult levels of these isoenzymes (above) will not be reached for several years (age 2-5) PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS D - Positive evidence of human fetal risk based on adverse reaction data from investigational or market experience or studies in humans. Potential benefits may warrant use of drug in pregnant women despite risks. X - Studies in animals and humans demonstrated fetal abnormalities.... DO NOT use in pregnant woman Will still see old categories Infants and Drugs - CORRECT ANSWERS 1. Fewer protein binding sites 2. Less albumin 3. Immature liver function 4. Stomach acid less acidic 5. Immature kidney function/urine output 6. Significantly higher risk for toxicity even with topical drugs To increase drug compliance, improve taste of drugs Drug Therapy and Geriatrics - Aging Changes - CORRECT ANSWERS Start to notice at age 45 1. Blood brain barrier (Benzos, opioids) 2. Baroreceptor responsiveness (orthostatic hypotension) 3. Decreased renal/hepatic blood flow 4. Immunosenescence (reason for pneumonia and increased mortality) 5. Pharmacodynamics (changes in receptors/responsiveness) aging changes Geriatric Drug Absorption - CORRECT ANSWERS 1. Decreased gastric acid - drugs needing acidic environment = Will take longer to dissolve - Decreases systemic availability of drug 2. Reduced blood flow to organs - decreasing blood absorption 3. Decreased drug absorption with IM or SQ due to decreased blood flow at administration site - Overall SLOWED drug absorption related to DECREASED GI motility, decreased Gastric acidity, AND reduced Blood Flow PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS Geriatrics and Drug Distribution - CORRECT ANSWERS 1. Decreased body mass 2. Reduced albumin 3. Less effective blood-brain barrier 4. Decreased cardiac output 5. Changes in body weight 6. Poor nutrition 7. Dehydration 8. Inactivity 9. Bedrest 10. Increased body fat (lipophilic drugs WILL have GREATER time to excretion) 11. Less water in body (MIGHT have increased levels of hydrophilic meds Three most problematic drugs: Warfarin, Dilantin, SSRIs (decreased albumin and body mass) Particular problem with Benzodiazepines (decreased retention, significant side effects) Geriatric Drug Excretion - CORRECT ANSWERS 1. Decrease glomerular filtration and renal tubule excretion - If GFR < 60 = be cautious; if sick GFR is likely LOWER - 2/3 of elderly populations - GFR = asymptomatic until < 35 2. Creatinine levels may remain NORMAL despite GFR changes 3. Muscle mass decreases and less overall creatinine exists ** Must monitor creatinine clearance Medication Safety - Older Adults - CORRECT ANSWERS Take 34% of all drugs prescribed; 30% of all OTC Most prescriptions are for: PHARMACOLOGY EXAM 1 STUDY SET (WEEKS 1 - 3) QUESTIONS AND ANSWERS LATEST UPDATE 2023/2024 ALL ANSWERS 100% CORRECT ELABORATED TO SCORE A+ FOR SUCCESS 1. HTN 2. CADS 3. Analgesic/anti-inflammatory 4. Sedatives 5. GI meds Geriatrics and ADRs - CORRECT ANSWERS 1. Accidental overdose often related to pain meds 2. Four medications cause 2/3 of hospitalizations - Warfarin - Insulin - Oral antiplatelets - Oral hypoglycemics Geriatrics and ADR Causes - CORRECT ANSWERS 1. Medication factors 2. Physiologic aging changes 3. Patient errors 4. System errors (multiple pharmacies) 5. Provider errors (overprescribing) ** pay attention to sight and hearing problems Geriatrics and ADRs - Patient Attributes - CORRECT ANSWERS 1. Age > 85 2. Low BMI < 22 3. Creatine Clearance < 50 mL/min 4. More than 6 co-morbid disorders 5. More than 9 meds, more than 12 doses a day 6. Previous ADR ** sensory deficit, arthritis, etc.