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Pharmacology Fundamentals and Drug Effects

Jun 4, 2025

Pharmacology Lecture Notes

Key Terms

  • Pharmacotherapeutics: Use of drugs to treat diseases.
  • Pharmacokinetics: What the body does to the drug, involving:
    • Absorption
    • Distribution
    • Metabolism
    • Excretion
  • Pharmacodynamics: What the drug does to the body, focusing on effects & mechanisms.

ADME (Absorption, Distribution, Metabolism, Excretion)

  • Absorption: Entry of drug into the bloodstream, influenced by route and gastrointestinal health.
  • Distribution: Spread of drug through the body, dependent on blood flow and protein binding.
  • Metabolism: Liver’s transformation of the drug, which can activate or deactivate the compound.
  • Excretion: Removal by kidneys, primarily through urine or feces.

Impact of Renal & Liver Issues on Elimination

  • Renal Impairment: Decreased excretion leads to risk of toxicity.
  • Liver Impairment: Decreased metabolism results in drug buildup and increased half-life.

Definitions

  • Adverse effects: Harmful, unintended drug effects.
  • Side effects: Expected but often mild effects.
  • Overdose: Excessive drug amount causing toxicity.
  • Drug allergy: Immune reactions like rash or hives.
  • Anaphylaxis: Severe allergic reaction causing swelling and difficulty breathing.

Pharmacokinetic Concepts

  • Half-life (t½): Time for drug concentration to reduce by half.
  • Loading dose: Large initial dose to quickly achieve therapeutic level.
  • Peak dose: Maximum drug concentration in the blood.
  • Therapeutic effect: Desired drug effect.
  • Critical concentration: Minimum blood level required for efficacy.

Agonist vs Antagonist

  • Agonist: Activates receptor to produce a response (e.g., Morphine).
  • Antagonist: Blocks receptor to prevent a response (e.g., Naloxone).

Routes of Administration & Absorption Speed

  • Oral: Slow, affected by stomach pH.
  • Mucosal/sublingual: Rapid absorption under the tongue.
  • Injection (IM, IV, SubQ): Fastest absorption with IV being the fastest.
  • Rectal: Moderate absorption, bypasses some liver metabolism.
  • Topical/patch: Local or systemic slow absorption.
  • Extended-release: Slow release for longer effect and less frequent dosing.

FDA Drug Trial Phases

  • Phase 1-3: Testing drug safety and efficacy.
  • Phase 4: Post-marketing surveillance.

Controlled Substance Schedules

  • Schedule I: Highest abuse potential, no medical use.
  • Schedule V: Lowest abuse potential.

Pregnancy Categories

  • Category A: Safest.
  • Category X: Contraindicated in pregnancy.

Black Box Warning

  • Strongest FDA warning for serious side effects, e.g., Isotretinoin causing severe birth defects.

Brand vs Generic Names

  • Brand: Trademarked, e.g., Tylenol.
  • Generic: Chemical name, e.g., acetaminophen.

OTC & Herbal Concerns

  • Risk of interactions and overdosing.
  • Importance of patient education on all medication and herbal use.

Nurse’s Role in Medication Safety

  • Three Checks:
    1. Before pulling medication.
    2. After pulling medication.
    3. At bedside before administration.
  • Patient Rights: Ensuring correct patient, drug, dose, route, time, reason, documentation, response, and education.
  • Common Errors: Incorrect dose, patient, or route.
  • If Error Occurs: Assess patient, notify provider, document, and complete an incident report (not in chart).

Adrenergic & Cholinergic Agents

Sympathetic Nervous System (Adrenergic)

  • Adrenergic Agonists (Sympathomimetics): Stimulate alpha/beta receptors → "fight or flight" effects.
    • Alpha Receptors: Cause vasoconstriction, raise BP.
    • Beta 1 Receptors: Increase heart rate/contractility.
    • Beta 2 Receptors: Cause bronchodilation.
    • Examples: Epinephrine, Norepinephrine, Dopamine.
  • Adrenergic Antagonists (Sympatholytics): Block receptors → opposite effect.
    • Example: Tamsulosin lowers BP by blocking alpha-1 receptors.

Cholinergic System (Parasympathetic)

  • Cholinergic Agonists (Parasympathomimetics): Stimulate nicotinic/muscarinic receptors → "rest & digest" effects.
    • Effects: Increased secretions, bradycardia, GI motility.
    • Examples: Bethanechol, Pilocarpine.
  • Cholinergic Antagonists (Anticholinergics): Block muscarinic receptors → "dry" effects.
    • Examples: Atropine, Scopolamine, Oxybutynin.
    • "Wet Drugs": Cholinergic agonists that increase secretions like saliva, tears.
    • "Dry Drugs": Anticholinergics that decrease secretions, causing dry mouth.

Cholinergic Crisis

  • Excessive cholinergic activity leading to SLUDGE:
    • Salivation, Lacrimation, Urination, Diaphoresis/Diarrhea, GI Cramps, Emesis.
  • Can result in respiratory failure.

Side Effects

  • Cholinergic Agonists: Cause excessive salivation, diarrhea.
  • Anticholinergics: Cause dry mouth, urinary retention, blurred vision, tachycardia.

Specific Drugs to Know

DrugClassIndicationKey Side EffectsNursing/Teaching Tips
PhenylephrineAlpha-1 agonistNasal congestion, hypertensionHypertension, rebound congestionMonitor BP, avoid with hypertension
EpinephrineAlpha & Beta agonistAnaphylaxis, cardiac arrestTachycardia, hypertensionMonitor heart, use in emergencies only
DopamineDopaminergic/AdrenergicShock, heart failureTachyarrhythmiasMonitor cardiac status closely
ClonidineAlpha-2 agonistHypertensionHypotension, dry mouthDo not stop abruptly to avoid rebound HTN
PhentolamineAlpha blockerHypertensive crisisHypotensionMonitor BP after administration
BethanecholCholinergic agonistUrinary retentionAbdominal cramps, diarrheaMonitor bladder function, avoid in asthma
TamsulosinAlpha-1 blockerBPHHypotension, dizzinessMonitor BP, teach about orthostatic hypotension
MetoprololBeta-1 blockerHTN, angina, heart failureBradycardia, fatigueMonitor HR, do not stop suddenly
PropranololNon-selective Beta blockerHTN, arrhythmiasBronchospasm, fatigueCaution in asthma patients
TimololBeta blockerGlaucomaEye irritationTeach eye drop administration
AtenololBeta-1 blockerHTN, anginaBradycardia, fatigueMonitor HR
PilocarpineCholinergic agonistGlaucoma, dry mouthSweating, nauseaAvoid in asthma, monitor vision
Donepezil (Aricept)Acetylcholinesterase inhibitorAlzheimer’s diseaseNausea, diarrheaTake at bedtime, monitor cognition
PyridostigmineAcetylcholinesterase inhibitorMyasthenia gravisSLUDGE symptomsMonitor muscle strength, watch for cholinergic crisis
OxybutyninAnticholinergicOveractive bladderDry mouth, constipationEncourage fluids, monitor for urinary retention
ScopolamineAnticholinergicMotion sicknessDry mouth, drowsinessApply patch behind ear, avoid alcohol
TiotropiumAnticholinergicCOPDDry mouthTeach inhaler technique
AtropineAnticholinergicBradycardia, pre-opTachycardia, dry mouthMonitor HR, avoid in glaucoma
DicyclomineAnticholinergicIBSDry mouth, blurred visionAvoid driving, monitor bowel function