1

Pharmacology Introduction
Gina Maiocco, PhD, RN, CCRN, CCNS
Key Terms
 Agonist
– A drug that has an affinity for the cellular receptors of another drug or natural substance that
produces an physiological effect
 Antagonist
– A drug that binds to a cellular receptor for a hormone, neurotransmitter, or another drug
blocking the action of that substance without producing any physiologic effect itself.
“Blocking Agent”

Key Terms
 Adrenergic
– Sympathetic NS
 Cholenergic
– Parasympathiometic application
 Dopaminergic
– Dopamine involvement in CNS regulation
Key Terms
 Alpha = vasoconstriction
 Beta = muscle activity
– B1 = myocardium = contraction, HR
– B2 = bronchial & vascular smooth muscles = bronchial relaxation and arterial dilation to
skeletal muscles
 Chronotrope
– Affects rate
 Inotrope
– Affects force of muscular contraction by activating beta cells
Cardiovascular Applications

Adrenergic Effects
 Sympathetic NS - agent that acts like epinephrine
 Produces:
– Vasoconstriction
–  HR, BP, CO
 Blocking agents
– peripheral vasodilation
–  HR, B/P
 2

Specific Drugs Imparting Adrenergic Effects

Alpha Agents
 Alpha = vasoconstriction
 Alpha adrenergic agonist
– Norepinephrine (levophed)
– Action =  B/P, work of heart
 Blocking agent - competes with catecholamines at peripheral autonomic receptor sites
– Regitine = dilation of arteries and veins
– Treat dopamine infiltration sites (see tissue necrosis)
– Side effect = orthostatic hypotension
Beta Adrenergic Agents
 Dobutamine or Dopamine (5 –10 mcg)
–  force of contraction,  heart rate
– Conditions: shock, CHF, sepsis
 Beta adrenergic antagonist - beta blockers (propanolol, labetalol)
–  HR, force of contraction
– Conditions: AMI, HPT
Calcium Channel Blockers
 Calcium enhances muscle depolarization ( resting potential)
 calcium =  b/p, arrhythmias, angina, migraines
  Ca+ = B/P,  rest
 Example:
– Verapamil
– Cardiazem
Ace Inhibitors
 Reduce arterial pressure by preventing generation of angiotensin II from angiotensin I
 Angiotensin II = potent vasoconstrictor
 Causes: B/P, water retention (aldosterone)
 Ace Inhibitors: (I.e. captopril, enalapril, lisinopril)
– B/P
– renal perfusion
Angiotensin II Inhibitors
 Block the binding of angiotensin II to specific tissue receptors in vascular smooth muscle &
adrenal glands
 Produces:
–  B/P
 3

 Example
– Losartin (cozaar)

CNS & Drugs

Cholinergic Effects
 Parasympathetic nervous system
– Acetylcholine (ACh) is primary neurotransmitter
– Nicotinic receptors: HR, B/P, peripheral vasoconstriction
– Muscarinic receptors: gastric motility, gastric acid & salivary secretion
 Conditions treated
– Alzheimers, Parkinson’s dx, motion sickness, PUD, IBS, visual disorders, urinary retention
Direct Acting Cholinergics
 Structurally similar to Ach
 Example:
– Urecholine
– Treats postoperative or postpartum urine retention
– Causes contraction and emptying of bladder
– Side effects
 Abdominal cramps
 Salivation
 N/v & diarrhea

Cholinesterase Inhibitor (colinergic)

 Elevates acetycholine concentrations in cerebral cortex by slowing degradation by
cholinesterase
 Elevated levels of ACh slows the neuronal degradation seen in Alzhiemer’s.
 Example:
– Aricept (donepezil)
– Side effects: abdominal pain, diarrhea, GI bleed

Anticholinergics
 Reverse cholinergic (parasympathetic) effects
 Blocks ACh at receptor sites in smooth muscles, secretory glands, SA & AV nodes & cardiac
muscle
 Example
– Scopolamine – motion sickness
– Atropine
– Treatment for bradycardia, excess secretions (preop)

Dopaminergic Drugs
 Dopamine is a CNS neurotransmitter
 4

 Action
– Inhibits excitatory signals produced by ACh
  dopamine produces cholinergic activity
– Tremors (pill rolling)
– Rigidity (involuntary contraction of muscles)
– Bradykinesia – general slownes
– Akinesia – loss of voluntary movement
Parkinson’s Disease
 Extensive deterioration of neurons at basal ganglia – see dopamine levels
 Combo therapy
– Dopaminergic Drugs
– Levodopa
 Precursor to dopamine
– Anticholinergic Drugs
– Cogentin
– Artane

Pain and More Pain

Opioids - analgesics
 Tx moderate to severe pain by crossing blood brain barrier
 Effects:
– CNS - LOC
– Respiratory depression
– Cardiovascular
– Orthostatic hypotension
– GI - GI muscle tone
– GU – urinary retention
Opioid Terms
 Opioid agonist
– Produce maximal response (schedule II drugs)
– Examples: codeine, morphine, demerol, oxycodone
 Opioid agonist-antagonist
– Activate opioid receptor without causing respiratory depression
– Example: stadol, nubain, talwin
 Opioid antagonist
– Blocks or reverses opioid effect
– Example: naloxone (narcan)
 5

Cox 2 Inhibitors
 Blocks prostaglandins that arise from the cyclooxygenase (COX) metabolic pathway
 A non-steroidal drug to treat arthritic pain
 Cautions with Cox 2 & NSAIDS
– GI bleed
– Renal failure
– Asthma reaction
Blood and Drugs
“Coagulation” Terms
 Anticoagulation
– Hinder future clot formation by inhibiting conversion of prothrombin to thrombin (heparin or
lovenox) or reducing amount of vitamin K (coumadin)
 Antiplatelet
– Prevents production of TXA2 – causes platelet aggregation and vessel constriction (I.e.
ASA, plavix)
 Thrombolytic
– Dissolves thrombi after formation (I.e. TPA, retavase)
– Used in combo with anticoagulants
More COAG Terms
 Glycoprotein IIB/IIA Inhibitors
– Inhibits platelet aggregation
– Used as adjunct with ASA and heparin to decrease clot formation, especially during invasive
procedures (cath)
– Given IV – follow up via PO med (plavix) with similar action
– Example: Reopro, Integrilin, Aggrastatin
GI & Drugs
H-2 Blockers
 Blocks release of histamine, esp w/stress
 Histamine stimulates gastric acid secretion
 Use:
– Stress ulcers
– Allergic reactions
 Examples
– Ranitidine (zantac)
– Famotidine (pepcid)
 6

Proton Pump Inhibitors

 Suppress gastric acid secretion by irreversibly binding with proton-pump system that controls
hydrogen ion secretion
 Use on high risk patients (expensive in IV form!!)
– Vented patients >24 hours
– Thrombocytopenic
 Example
– Prevacid
– Prolosec
Drugs Influencing
the Respiratory System
Corticosteroids
 Anti-inflammatory effect – reduced mucus secretion in respiratory conditions
 Uses:
– Asthma, COPD, SCI
 Example: flovent, solumedrol, azmacort, decadron
 Side Effects
– Mask Infections
– Hyperglycemia
– Slow wound healing
Beta Agonists
 Relieve bronchoconstriction
 Uses
– Short term – tx acute exacerbations
– Long term – control symptoms, especially nocturnal
 Examples: alupent, serevent, proventil
 Side effects
– Tachycardia, headache, angina, muscle tremors
This material is based upon work supported by the Ohio Learning Network.
Any opinions, findings, and conclusions or recommendations in this material
are those of the author and do no necessarily reflect the views of the Ohio
Learning Network.

This material was developed by Dr. Gina Maiocco while employed on the faculty
of the Wright State University-Miami Valley College of Nursing and Health
during the 2004-2005 academic year.