Pharmacology Exam Chapter 1 Study Notes: Key Concepts and Principles, Study Guides, Projects, Research of Pharmacology

Comprehensive study notes for chapter 1 of a pharmacology exam. It covers essential concepts like drug effectiveness, safety, selectivity, and pharmacokinetics. The notes delve into the importance of drug absorption, distribution, metabolism, and excretion, highlighting key factors influencing these processes. Additionally, it discusses the different routes of administration, dosage considerations, and the nursing process in drug therapy. The document also touches upon drug development, off-label use, and the distinction between prescription and over-the-counter medications.

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PHARM EXAM Chapter 1 STUDY NOTES
What is an Ideal drug?
oDrugs have to be effective, safe, selectivity
Effectiveness: Most important property a drug can have. Elicits the responses
for which it is given. Does what we want it to do and doesn't cause a lot of side
effects, also should be reversible (if side effects need to be able to stop them) US law
requires that all new drugs be proved effective prior to release.
Has to be affordable and easy to take, easy name to remember
Safety: safe drug cannot produce harmful effects even when administered in
high doses and for long time. All drugs have ability to cause injury (esp. with high
doses and prolonged use.) Chances of adverse effects can be reduced by proper
drug selection and proper dosing.
Certain anti-cancer drugs at usual dosage can increase risk of
serious infection
Opioid analgesics at high doses can cause fatal respiratory depression.
Aspirin and other related drugs in high doses can cause potentially
fatal gastric ulceration, perforation and bleeding.
Selectivity: drug that elicits only the response for which it is given. No such
thing as a wholly selective drug because all drugs have side effects.
Reversible action: important that effects be reversible. Important for all but antibiotics
because we want toxicity to microbes to endure
Predictability: Can't always know how drug and patient will interact because each patient
is unique. Maximize chances of desires responses by tailoring therapy to individual.
Ease of Administration: Convenient route and number of doses per day should be low.
oEase can enhance patient adherence and can decrease risk.
Freedom from Drug Interaction: because of potential for drug interaction, it must be
monitored when a patient is taking several drugs.
Low cost: idea drug is ideally easy to afford.
Chemically stability: some drugs lose effectiveness during storage or lose effectiveness when
put in solution.
Possession of simple generic name: makes it easy to recall and pronounce for the
common person.
The idea: maximum benefit, minimal harm.
Nurse's Responsibility (Pre-administration Assessment)
oCollecting baseline data
Needed to evaluate therapeutic responses and adverse effects
oIdentifying high-risk patients
Liver and kidney impairment
Genetic factors
Drug allergies
Pregnancy
Older adult/pediatric age group
Tools: Patient history, physical exam, and lab results
oAssessing Patient's Capacity for Self-care
oContraindication (you can't have that drug---allergy)
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PHARM EXAM Chapter 1 STUDY NOTES

  • (^) What is an Ideal drug? o (^) Drugs have to be effective, safe, selectivity - (^) Effectiveness: Most important property a drug can have. Elicits the responses for which it is given. Does what we want it to do and doesn't cause a lot of side effects, also should be reversible (if side effects need to be able to stop them) US law requires that all new drugs be proved effective prior to release. - (^) Has to be affordable and easy to take, easy name to remember - (^) Safety: safe drug cannot produce harmful effects even when administered in high doses and for long time. All drugs have ability to cause injury (esp. with high doses and prolonged use.) Chances of adverse effects can be reduced by proper drug selection and proper dosing. ▪ (^) Certain anti-cancer drugs at usual dosage can increase risk of serious infection ▪ (^) Opioid analgesics at high doses can cause fatal respiratory depression. ▪ (^) Aspirin and other related drugs in high doses can cause potentially fatal gastric ulceration, perforation and bleeding. - (^) Selectivity: drug that elicits only the response for which it is given. No such thing as a wholly selective drug because all drugs have side effects.
  • (^) Reversible action: important that effects be reversible. Important for all but antibiotics because we want toxicity to microbes to endure
  • (^) Predictability: Can't always know how drug and patient will interact because each patient is unique. Maximize chances of desires responses by tailoring therapy to individual.
  • (^) Ease of Administration: Convenient route and number of doses per day should be low. o (^) Ease can enhance patient adherence and can decrease risk.
  • (^) Freedom from Drug Interaction: because of potential for drug interaction, it must be monitored when a patient is taking several drugs.
  • (^) Low cost: idea drug is ideally easy to afford.
  • (^) Chemically stability: some drugs lose effectiveness during storage or lose effectiveness when put in solution.
  • (^) Possession of simple generic name: makes it easy to recall and pronounce for the common person. The idea: maximum benefit, minimal harm.
  • (^) Nurse's Responsibility (Pre-administration Assessment) o (^) Collecting baseline data
  • (^) Needed to evaluate therapeutic responses and adverse effects o (^) Identifying high-risk patients
  • (^) Liver and kidney impairment
  • (^) Genetic factors
  • (^) Drug allergies
  • (^) Pregnancy
  • (^) Older adult/pediatric age group
  • (^) Tools: Patient history, physical exam, and lab results o (^) Assessing Patient's Capacity for Self-care o (^) Contraindication (you can't have that drug---allergy)
  • (^) Pre-existing condition the precluded the use of a drug in all but most critical condition
  • (^) ie if you have asthma you may have greater risk of drug allergy b/c both are linked to immune system o (^) Precaution
  • (^) Pre-existing condition that significantly increases the risk of an adverse reaction to a particular drug. o (^) Dosage and Administration
  • (^) Certain drugs may have more than one indication (use) ▪ (^) ie Codine can be used for pain but also for very bad cough)
  • (^) Dosage may differ depending on indication for which the drug is being used
  • (^) Many drugs can be administered through more than one route
  • (^) Dosage may differ depending on route selected ▪ (^) Route dependent
  • (^) Dilaudid IV- 1.5 mg
  • (^) PO (mouth)-7.5 mg
  • (^) Certain intravenous agents can cause severe local injury if extravasation (seeps into local tissues) occurs
  • (^) MS (Morphine) vs Mg (Magnesium) o (^) Maternal problems o (^) Morphine crosses plancental barrier o (^) Magnesium strengthens muscle contractions o (^) Baby doesn't breathe while born with morphine
  • (^) Dosage and Admin cont. o (^) Read medication order carefully o (^) Verify ID of patient (bracelet) o (^) Read medication label carefully o (^) Verify dosage calculations o (^) Don't give drug if you don't understand reason for its use o (^) Implement special handling for drug if required
  • (^) Therapeutic effects o (^) Evaluating: to make evaluation must know rationale for treatment and nature/time course of intended response
  • (^) If desired responses don't happen within timespan must quickly figure out why o (^) Promoting Patient Adherence
  • (^) Compliance or concordance ▪ (^) Extent to which patient behavior coincides with medical advice ▪ (^) Must completely inform patient for max adherence.
  • (^) Implementing Drug measures ▪ (^) Drug therapy can be enhanced by nondrug measures
  • (^) Ie becoming more healthy through diet and exercise
  • (^) All drugs have potential to produce undesired effects
  • (^) Minimize Adverse Effects by:
  • (^) Always know the following: o (^) Major adverse effects that drug can produce o (^) Times when reactions are likely to occur
  1. Phases II and III: tested in Patients. To determine therapeutic effects, dosage range, safety, and effectiveness.
  2. Phase IV: Postmarketing surveillance
  • (^) Drug Names o (^3) types of drug names
  1. Chemical
  2. Generic (need to know for exams)
  3. Trade o (^) Generic or Trade?
  4. Are they therapeutically equivalent?
  5. Would difference between brand-name and generic product justify use of trade names?
  6. Are chemically/molecularly different sometimes, different absorption
  • (^) Extra molecules can make your body stress more because more to break down o (^) Over the Counter drugs (OTC)
  1. Americans spend ~$20 bil annually on OTC
  2. Account for 60% of all doses administered
  3. 40% of Americans take at least 1 OTC drug every 2 days
  4. 4x as many illnesses are treated by consumer using an OTC drug as by consumer visiting a physician o (^) Prescription and OTC drugs
  5. Prescription Advantages: Get to see licenced human, can regulate the amount
  6. Prescription Disadvantages: Drugs can be more potent (higher risk), expensive, insurance
  7. OTC Advantages: Convenient, don't have to see Dr.,
  8. OTC Disadvantages: Self treating, can take as many as they want
  • (^) Term Pharmacokinetics- study of drug movement through body
  • (^) Also includes drug metabolism and drug excretion
  • (^4) basic pharmacokinetic processes o (^) Absorption o (^) Distribution o (^) Metabolism o (^) Excretion
  • (^) How we get it into the body depends on how it works
  • (^) Passage of Drugs across membranes o (^3) ways
  • (^) Channels and pores
  • (^) Transport system (P-glycoprotein: gets drug out of cell. Present in cells in liver, kidney, placenta, intestine, and brain capillaries)
  • (^) Direction penetration of membrane (lipid soluble goes through faster, protein binding)
  • (^) Most drugs: movement in body is dependent on drug ability to penetrate membranes directly
  • (^) Most drugs too large to pass through channels or pores
  • (^) Most drugs lack transport systems to help them cross membranes that separate them from sites of action, metabolism, and excretion (P-glycoprotein transport out of cell) o (^) Brain-blood barrier is why it is hard to treat dementia, Alzheimer's
  • (^) Polar molecules o (^) Uneven distribution of a charge o (^) No net charge o (^) Can't dissolve in lipid bilayer of cell membrane
  • (^) Ions o (^) Molecules that have net electrical charge o (^) Unless very small cannot cross membranes
  • (^) Quarternary Ammonium Compounds o (^) Molecules with at least 1 atom of nitrogen and constant positive charge o (^) Usually only have 3 chemical bonds on nitrogen but this has 4 o (^) Cannot cross most membranes
  • (^) Absorption o (^) Factors that affect drug absorption - (^) Rate of Dissolution - (^) Surface Area - (^) Blood Flow - (^) Lipid Solubility - (^) pH partitioning o (^) Route of Administration Enteral and Parenteral (injection- intravenous, subcutaneous and intramuscular) - (^) Oral route ▪ (^) Drugs to GI tract ▪ (^) Oral or through NG or gastrostomy tubes ▪ (^) Tablets and capsules - (^) Most patients prefer capsules - (^) Must dissolve before drug is available for absorption - (^) Slow onset time - (^) Oral liquid absorbed faster - (^) Enteral route ▪ (^) Tablets and capsule - (^) Enteric-coated - (^) Hard waxy coating to resist stomach acid - (^) Extended release - (^) Designed to dissolve slowly for longer duration of action - (^) Recent developments- dissolve in 30 seconds - (^) Orally disintegrating tablets (ODT) - (^) Oral soluble films ▪ (^) Nasogastric and gastrostomy tubes - (^) Medications administered through devices - (^) Usually liquid form - (^) Solid drugs that are crushed tend to clog tubes - (^) Don't use sustained release meds - (^) Drugs exposed to same processes as those given orally ▪ (^) Sublingual and buccal routes - (^) Meds kept in mouth

o (^) Entering cells o (^) Blood flow to Tissues

  • (^) Drugs are carried by the blood tissues and organs of body
  • (^) Blood flow determines rate of delivery
  • (^) Abscesses of tumor ▪ (^) Low regional blood flow affects therapy ▪ (^) Pus-filled pockets rather than internal blood vessels (have to drain so medicine can treat) ▪ (^) Solid tumors have limited blood supply ▪ (^) Capillary beds
  • (^) Drugs pass between capillary bed rather than through ▪ (^) Special barrier to drug distribution
  • (^) Blood-brain barrier ▪ (^) Doesn't contain pores ▪ (^) Protects brain from toxins and pathogens ▪ (^) Lipid-soluble drugs can cross ▪ (^) Not fully developed in neonates- heightened sensitivity to CNS toxicity ▪ (^) Placental Drug Transfer
  • (^) Movement determined for same way as other membranes
  • (^) Risks with drug transfer: ▪ (^) Birth defects: mental retardation, gross malfunctions, low birth weight - (^) Mother's use of habitual opioids ▪ (^) Birth of dependent baby
  • (^) Drug-protein complexes cannot cross capillary membranes (plasma albumin is more important most abundant protein in plasma)
  • (^) Only unbound drugs can reach target tissues- only ones used by body
  • (^) Competition of protein binding sites
  • (^) Each drug has protein binding percentage
  • (^) Some drugs must enter cells to reach site of action
  • (^) Most drugs must enter cells to undergo metabolism and excretion
  • (^) Many drugs produce their effects by binding with receptors on the external surface of the membrane o (^) Do not have to cross the cell membrane to act
  • (^) This repeated system doesn't make too much of a difference on cell levels
  • (^) Biotransformation o (^) Enzymatic alteration of drug structure o (^) Most often takes place in liver o (^) Most drug metabolism takes place in liver performed by hepatic microsomal enzyme system (P450 system)
  • (^) Hepatic microsomal enzymes o (^) Cytochrome p450 (CYP) o (^) An enzyme metabolizes many drugs o (^) Many isoenzymes systems within CYP
  • (^) Determine speed at which drug is metabolized
  • (^) Contributes largely to drug-drug interactions
  • (^) Drug Metabolism o (^6) possible consequences 1. Accelerated renal excretion of drugs (convert lipid solution to hydrophilic (water soluble) 2. Drug inactivation (active to inactive) 3. Increased therapeutic action (increase the effect) 4. Activation of "prodrugs" (drugs that need metabolism to activate) 5. Increased toxicity 6. Decreased toxicity o (^) Things to consider with drug metabolism: age, (liver function, heart function, can't chew as well, saliva decrease, GI motility decreases, kidney function goes downhill) induction/inhibition of drug-metabolizing enzymes (drugs affected by P450 inducers or inhibitors) o (^) First-pass effect (how many times goes through liver- doesn't make much of a difference) o (^) Nutritional status (if you don't take in as much protein or nutrients)
  • (^) Excretion o (^) Removal of drugs from the body (affect different parts of kidney) o (^) If patient's kidneys don't work well change drug to something that works on a different part of kidney) 1. Can excrete in urine, bile, sweat, saliva, breast milk, and expired air. o (^) Renal drug excretion is most important 1. Glomular filtration 2. Passive tubular reabsorption 3. Active tubular secretion o (^) Factors that modify renal drug excretion 1. pH-dependent ionization 2. Competition for active tubular transport 3. Age (very old and babies at risk) o (^) Other routes of excretion 1. Lungs 2. Glandular secretion ▪ (^) Sweat saliva, breast milk ▪ (^) Taste and smell some drugs ▪ (^) Excretion in breastmilk 3. Fecal and biliary excretion ▪ (^) Feces, bile 4. Enterohepatic recirculation ▪ (^) May recirculate drugs, metabolites, and prolong action - (^) Time course of drug responses o (^) Plasma drug levels 1. Minimum effective concentration (MEC) 2. Toxic concentration 3. Therapeutic range o (^) Single-dose time course o (^) Drug half-life 1. Time required for drug to be 50% decreased
  • (^) Can be important if lack of potency forces huge doses
  • (^) Implies nothing about maximal efficacy - refers to dosage needed to produce effects
  • (^) Drug-Receptors Interaction o (^) Drugs - chemicals that produce effects by interaction with other chemicals
  • (^) Receptors macromolecule in a cell to which a drug binds to produce effect o (^) Normal points of control of physiologic processes o (^) Under conditions receptor regulated by molecules supplied by body o (^) Drugs can only mimic or block body's regulator molecules o (^) Drugs help by making body use pre-existing capabilities
  • (^) Receptors and selectivity of Drug Action o (^) More selective a drug is few side effects it will produce to some extent o (^) Receptors make selectivity possible o (^) Each type of receptor participates in regulation of just few processes
  • (^) Drug responses that don't involve receptors o (^) Simple physical or chemical interactions with other small molecules o (^) Examples of receptorless drugs: tums, etc.
  • (^) Interpatient Variability in Drug Responses o (^) Dose required to produce therapeutic response can vary substantially among patients o (^) Clinical implications of interpatient variability
  • (^) Initial dose of a drug is necessarily an approximation
  • (^) Subsequent doses must be "fine tuned" based of patient's response.
  • (^) Drug-drug interactions o (^) Intensifications of effects
  • (^) Increased therapeutic effects
  • (^) Sulbactam and ampicillin
  • (^) Increased adverse effects
  • (^) Aspirin and warfarin o (^) Reduction of effects
  • (^) Inhibitory: interactions that result in reduced drug effects
  • (^) Reduced therapeautic effects
  • (^) Propranolol and albuterol
  • (^) Reduced adverse effects
  • (^) Naloxone to treat morphine overdose
  • (^) Creation of unique response
  • (^) Alcohol with disulfiram (makes sick if drink alcohol)
  • (^) Basic mechanisms of drug-drug interactions o (^) Drugs can interact through four basic mechanisms
  1. Direct chemical or physical interaction
  2. Pharmacokinetic interaction
  3. Pharmacodynamics interaction
  4. Combined toxicity
  • (^) Direct Chemical or Physical Interaction o (^) Never combine drugs in same container without establishing compatibility
  • (^) Most common in intravenous solution (err on the side of caution, safer than figuring out all of compatability) o (^) Precipitate: don't administer
  • (^) Pharmacokinetic interactions o (^) Altered absorption 1. Elevated gastric pH (antacids) 2. Laxatives 3. Drugs that depress peristalsis (morphine) 4. Drugs that induce vomiting 5. Absorbent drugs 6. Drugs that reduce regional blood flow o (^) Altered distribution 1. Competition for protein binding 2. Altercation of extracellular pH o (^) Altered Renal excretion 1. Can alter: filtration, absorption, active secretion o (^) Altered metabolism 1. Most important and most complex mechanism in which drugs interact o (^) Interactions that involve P-plycoproteins (PCGPs) 1. Transmembrane protein transports a wide variety of drugs out of cells 2. Reduced or increased PGP ▪ (^) Intestinal epithelium: affects absorption ▪ (^) Placenta: affects drug export from placental cells to maternal blood ▪ (^) Blood-brain barrier o (^) Pharmacodynamics interactions 1. At same receptor ▪ (^) Almost always inhibitory 2. At separate sites ▪ (^) May be potentiative ▪ (^) Or inhibitory 3. Combined toxicity - (^) Minimizing Adverse Drug-Drug interactions - (^) Nursing actions help minimize this o (^) Take a history (med reconciliation) o (^) Timing of drugs (spread out when given) o (^) Be careful with low dose therapeutic drug
  • (^) Drug-Food Interactions o (^) Impact of food on:
  1. Drug absoprtion ▪ (^) Decreased absorption
  • (^) Rate
  • (^) Extent of absorption (occasionally)
  • (^) Milk and tetracycline
  • (^) Fiber and digoxin ▪ (^) Increased absorption
  • (^) High calorie meal and saquinavir (antiretroviral drug for AIDS)

o (^) Risk increased by severe illness

  • (^) Terms related to adverse drug reactions o (^) Side effect:
  1. Nearly unavoidable secondary drug effect produced at therapeutic doses
  2. May develop soon after drug is initiated or not until drug has been taken for weeks or months o (^) Toxicity
  3. Formal definition: adverse drug reactions caused by excessive dosing
  4. May occur even with normal dosing ▪ (^) Neutropenia (risk for infection) and anticancer medication o (^) Allergic reactions
  5. Immune response
  6. Determined preliminary by the degree of sensitization of the immune system rather than by drug dosage
  7. Patient's sensitivity of a drug can change over time
  8. Very few drug reactions cause severe allergic reactions ▪ (^) Penicillin are most common ▪ (^) Allergies may also be induced by sulfonamides (diuretics, antibiotics, and oral hypoglycemic agents) o (^) Idiosyncratic effect
  9. Uncommon drug response resulting from genetic predisposition
  10. Succinylcholine-induced paralysis ▪ (^) Usually brief but may last for hours in genetically predisposed patients
  11. Paradoxical effect ▪ (^) The opposite of intended drug response ▪ (^) For example, when using benzodiazepines for sedation to treat insomnia, excitement may occur instead (especially in kids and older adults)
  12. Carcinogenic effect
  13. Iatrogenic disease ▪ (^) Iatrogenic: literally disease produced by physician- used to refer to a disease produced by drugs (for example, drugs for antipsychotic disorders can cause Parkinson's-like symptoms( ▪ (^) Sometimes also called drug-induced disease ▪ (^) Essentially identical to naturally occurring pathology
  14. Teratogenic effect ▪ (^) Drug-induced birth defect o (^) Boxed Warnings
  15. Aka black box warnings
  16. Strongest safety warning drug can carry and still remain on the market o (^) Physical dependence
  17. Develops during long-term use of certain rugs (opioids, alcohol, barbiturates, and amphetamines(
  18. State in which body has adapted to drug exposure in such a way that an abstinence syndrome will result if drug use is discontinued
  19. Important to warn patients against abrupt discontinuation of any medication without first consulting knowledgeable health profession

o (^) Organ-specific drugs o (^) Many drugs are toxic to specific organs o (^) Common examples include:

  1. Kidneys: Amphotericin B (antifungal)
  2. Heart: Doxorubicin (anticancer)
  3. Lungs: Amiodarone (antidysrhythmic)
  4. Inner ear: Aminoglycoside (antibiotic) o (^) Hepatotoxic drugs
  5. Leading cause of liver failure in US
  6. More than 50 drugs are hepatotoxic
  7. As some drugs undergo metabolism, converted to toxic products that can injure liver cells
  8. Combining hepatotoxic drugs may increase risk for liver damage (acetaminophen and alcohol)
  • (^) Identifying Adverse Drug Reactions o (^) Can be difficult to determine whether a specific drug is responsible for an observed adverse event o (^) Other factors to consider
  1. Underlying illness
  2. Other drugs o (^) How is reaction identified? When did this happen, are you ok, how do you feel?
  • (^) Burden of Medical Errors o (^) 98,000 people die every year from preventable medical errors
  • (^) Medication Errors o (^) The risk for errors in hospitals is high because each medication order processed by several people
  1. Nurse is last person in sequence
  2. Last line of defense against mistakes
  3. Heavy responsibility on nurse to ensure patient safety o (^) Causes of medication errors
  4. Skipping important steps (right patient, drug, room, time)
  5. Being tired
  6. Discounting what the patient says
  7. Being in a hurry
  8. Improper medication labeling o (^) Reporting Medication Errors
  9. Facilities have policies and procedures for reporting medication errors
  10. Documentation should be factual
  11. Include specific intervention implemented to protect patient safety
  12. Failure to document could be interpreted as negligence
  13. Record all names of individuals notified of error
  14. MAR (Medication Administration Record) should contain information on given/omitted medications
  15. Written incident report must be completed ▪ (^) Identifies factors contributing to error
  16. Incident report is not included in patient's medical record o (^) Ways Reduce Medication Errors

o (^) Most cases (75%) of nonadherance are intentional o (^) Reasons include the following

  1. High cost of drugs, side effects, and patient's belief that drug dose is too high or unnecessary o (^) Nursing actions?
  2. Simplify meds and times
  3. Make things clearly labeled
  4. Easy open lids
  5. Support systems in place
  6. Easy instructions
  7. List on fridge of meds, times, etc.
  8. Visiting Nurse
  9. Assess safety of house (falls risk)