PHARMACOLOGY potency of an agonist. Ex.

Epinephrine and Phenoxybenzamine

Sources of drugs 2. Enzymes and pumps
 Animals = insulin ---- pancreas of cows and pigs (Drug-Enzyme Interaction)
 Plants = St. John’s Wort ---- for depression  Example: Cholinesterase(ASE=enzyme)
 Inorganic compounds Inhibitors
 Synthetic = E. coli (Inhibiting Pumps)
 Example: Reuptake Inhibitors - impulse
Branches of Pharmacology 3. Chemical Interaction
 Pharmacodynamics – Drug binding to receptor 4. Altering metabolic Process
 Pharmacokinetics – Body reactions to the drugs
Liberation Pharmacokinetics
Absorption 1. Liberation – release of active ingredients
Distribution 2. Absorption – Blood
Metabolism 3. Distribution
Excretion 4. Metabolism(Biotransformation) – ex. 500mg
Oral – going to liver- from liver release new
Rights of Drug Administration drug 400mg less active also called First Pass
 Right Drug Effect
 Right Dose 5. Excretion – kidneys, feces, lungs, Skin
 Right Patient Routes of Drug Absorption
 Right Time 1. Enteral Route - GIT
 Right Route Oral, Rectal (fastest route), Nasogastric
2. Parenteral – IV, SQ, IM, ID
 Right Documentation
3. Transmucosal – Sublingual, Inhalation, Topical
 Right education
 Right to refuse
Dose
 Right assessment
 Amount of drug to be administer
 Right Evaluation
Schedule
 Frequency, how many doses per day
Pharmacodynamics
Recommended dose
 Actions of drug
 Right amount + Right schedule
 Replacement a missing substance – Insulin,
Critical Concertation
Cortisol. T4, T3.
 level of drug in the blood which produces a
 Increase Cellular activities – Epinephrine
therapeutic effect.
 Depress cellular activities – Beta blockers
Therapeutic Effect
 Interfere with growth of a foreign cell -
 favorable response after a treatment of any
Antibiotic
kind
 Drug actions maybe through
Loading Dose
1. Receptors (Drug-Receptors Interaction)
 Initial dose, immediate response
 Example: Autonomic Drugs
 Agonist – stimulate  High than recommended dose
 Antagonist:  Giving during emergency cases.
 Competitive antagonist – Binds to a Half life
same Receptor, Potency of an agonist  Time it takes for a drug to become half of its
is reduced. Ex. Diazepam and previously peaked level.
Flumazenil.
 Non Competitive antagonist – Binds
to a different receptor, prevent
Dosage forms of Drugs Neurotransmitters
A. Solid  Chemicals in the body acting as “Messengers”
1. Tablets:  Acetylcholine (ACH)
 Scored  Muscle contraction
 Layered (2 or more chemicals tablet)  Memory
 Enteric-Coated (tablets not dissolved in Bipolar. Alzheimer’s Disease
stomach but in ab alkaline environment)  Norepinephrine and Epinephrine (NE/E)
 Chewable – liquid forms are better  Catecholamine (NE, E, D) released by
absorbed. nerves in the SNS
 Sustained-Release – liberation and  Depression
absorption is delayed and not at the same Schizophrenia, Mania.
time. Depression, ADHD
2. Capsule:  Dopamine (DOPA)
 Hard gel  Coordination of impulses and responses
 Soft gel  Cognitive behavior (thinking, learning,
3. Lozenges reasoning)
Antiseptic action – Destroy the bacteria Schizophrenia, Mania.
Anesthetic action – Relieve pain Depression, Parkinson’s, ADHD
B. Liquid  Serotonin (5HT)
1) Syrup  For arousal and sleep
 Sugar and clear and flavor  In preventing depression
 For kids  Promotes motivation
2) Suspension  Chocolate, Banana
 Shake before use Schizophrenia, Depression
3) Elixir
 Contains alcohol  Gamma-aminobutyric Acid (GABA)
 Cause drowsiness  Inhibitory nerve activity
 Avoid driving and operating machine  Prevents over excitability or stimulation
C. Topical such as seizure activity
I. Ointment  Treat Seizures, anti-convulsant drug
 Oil based
 For dry lesion Cholinergic Nerves
II. Cream  A nerve produces, stores and releases
 Water based Acetylcholine (ACH)
 Wet lesion Adrenergic Nerves
III. Lotion  A nerve producing epinephrine, norepinephrine
 Used if the lesion is extensive  Produce in the adrenal medulla.
IV. Patch Dopaminergic Nerves
 Apply over dry and none  a nerve producing dopamine.
irritation areas
 Rotate sites – irritation Autonomic Nervous System
 Includes two neurotransmitters:
Nervous System
Norepinephrine and Acetylcholine
 Two Branches:
1. Sympathetic – Adrenergic Nervous System.
Ex. NE=Adrenaline
2. Parasympathetic – Cholinergic
Ex. Acetylcholine
 ANS Sympathetic Parasympathetic Cholinergic agonist to BV = vasodilation
Response to: + HR, - HR, Contractility Adrenergic antagonist to GIT = diarrhea
Heart Contractility
Lungs, Bronchus RR – Bronchoconstriction OR: Atropine – Anticholinergic drug
Bronchodilation
 Lessen the secretion
Pupils Dilate: Mydrasis Constrict: Meiosis  Decrease risk of aspiration
GIT (blood flow, Constipation Diarrhea
motility, ADRENERGIC
secretions) (receptor)
Kidney - Urine formed + urine formed Alpha (a) Beta (B)
 Blood flow
Urinary Bladder Relax Contract A1 A2 B1 B2
 Sphincter Contract Relax
 Detrusor Urinary CNS Nerve Heart Lungs
muscle Retention of Emptying of bladder Bladder Membrane +HR, bronchodilati
Urine Sphincter – decrease NE +contractility on
Blood Vessels Vasoconstriction Vasodilation Closes: Release
Retention Potassium
( smooth
Weakens Enters Cell -
muscle)
SNS antiarrhythm
ic
PSNS
Sympathetic = SNS = Adrenergic Blood Vessels Pancreas Kidney Uterus -
Agonist = stimulate - decrease +Renin relaxation
Vasoconstricti insulin Release,
Mimetic = copy on release. increase BP

Sympathomimetic to bronchus = increase HR Hyperglycem

ia
Sympathomimetic to GIT = bronchodilation
Iris – Dilation: BV of heart,
Sympathomimetic to bladder = retention Mydriasis Lung &
Sympathomimetic to BV = vasoconstriction Skeletal
Sympathomimetic to blood flow = decrease muscle -
vasodilation
Liver –
Parasympathomimetic to GIT = Diarrhea Glycogenolysi
Parasympathomimetic to BV = vasodilation s
Hyperglycemi
Parasympathomimetic to pupils = meiosis a
Parasympathomimetic to bronchus =
bronchoconstriction AGONIST

Parasympathetic = PSNS = Cholinergic Alpha 1 Adrenergic Agonist

Antagonist = Block
Lytic = block, Destroy, Dissolve Phenylephrine
 Decongestant
Sympatholytic to pupils = meiosis  Allergic rhinitis – vasoconstriction – blood flow
Sympatholytic to BV = vasodilation decrease – reduce o2 and nutrients to cells –
Sympatholytic to bladder = emptying Shrink
Sympatholytic to heart = decrease HR  Eye exam
Sympatholytic to bronchus = bronchoconstriction Midodrine
 DOC for orthostatic hypotension
Parasympatholytic to pupils = mydriasis
 Vasoconstriction – increases TPR – Increase BP
Parasympatholytic to GIT = constipation

Adrenergic agonist to heart = increase HR

Alpha 2 Adrenergic Agonist Alfuzosin
 Urinary bladder Emptying bladder BPH
Clonidine (Catapres) Tamsulosin
 Decrease BP  For BPH
Methyldopa
Beta Adrenergic Blockers Drugs
Beta 1 Adrenergic Agonist Indications:
 Use for HPNde. HRdec. BP
Dobutamine  Use for ANGINA: -O2 supply, +O2 demand,
 Synthetic dopamine Goal: +O2 suppy, -O2 demand
 CHF (congested heart failure) Decrease HR workload of heart decreaseO2
 Sympathomimetic drug demand decreaseO2 supply increase
 Side effects: palpitation, hypertension  MI
 Supraventricular Arrhythmia, Atrial FIB
Beta 2 Adrenergic Agonists  CHF (cautious)
Decrease HRdecrease workload of
Albuterol/Salbutamol heartincrease of contraction
 Bronchodilation  Anxiety (Propranolol)
 used for Asthma, COPD Tremors and palpitationdecrease HR
 Side effect: Palpitation, tremors (B2> B1)  Migraine
 Open-Angle Glaucoma (Betaxol, Timolol)
Terbutaline Side Effects Contraindication Nursing M.
 Used in asthma and COPD Bradycardia Monitor HR Hold if HR
 Used in premature labor: Tocolytic <60/min
Hypotension Monitor BP Hold if BP
Isosuxprine <90/60
 Tocolytic mmHg
Bronchoconstriction Monitor BS Avoid
asthma,
ANTAGONIST
COPD
Hypoglycemia Monitor BS Caution in
Alpha Adrenergic Antagonist
DM
Impotence
Phentolamine
 Use for hypertensive crisis due to: Beta 1-Selective Adrenergic Blockers Drugs
Pheochromocytoma (tumor in adrenal medulla,  Bisoprolol, Betaxolol
increase NE cause Hypertension) and MAOI’s  Esmolol
(MAO break down NE)
 Acebutolol, Atenolol
 Metoprolol
Alpha 1 Adrenergic Antagonist
Propanolol
Prazosin
 Use for tachycardia and tremors in
 Blood vessels  vasodilation  decrease TPR
hypertyroidism
 Hypertension
Doxazosin & Terazosin
CHOLINERGIC receptors
 Blood Vessel  Vasodilation  decrease TPR
 HPN
Muscarinic Agonist to Pupils = Meiosis
 Urinary Bladder  Emptying bladder  BPH Antinicotinic to Bladder = retention
(Benign Prostatic hypertrophy)
 CHOLINERGIC (Receptors)
Muscarinic Nicotinic
M1 M2 M3 M4 M5 N1 or N2 or Nn
Nm
CNS Heart Smooth CNS CNS NMJ Autonomic
Muscle Ganglia
Gastric
Parietal CNS
Cells
Adrenal
Autono Medulla
mic
Ganglia

Myasthenia Gravis
 Autoimmune  Antibody  Antigen (foreign
body)
 Attacking receptors
 Paralysis – descending paralysis
 Sign & Symptoms
Ptosis = initial sign. Check palpebral fissure
Diplopia – Double vision
Mask like facial expression
Dysphagia - Risk for aspiration
Weakening of Laryngeal Muscles
Respiratory Muscle Weakness - lead to
respiratory arrest. Prepare at bedside
tracheostomy set
 Nursing Priorities
Airway, Dysphagia (aspiration), Immobility
 Treatment:
Neostigmine
Pyridostigmine
Edrophonium – Chloride (tensilon) for
diagnostic
 Diagnostic Test:
Tensilon Test: Edrophonium Chloride
(Cholinergic drug), IV

MYASTHENIC CHOLINERGIC
CRISIS CRISIS
S/Sx Weakness, Weakness,
paralysis Paralysis
Cause Under dose of Overdose of
cholinergic drug cholinergic drug
Tx Cholinergic Anticholinergic
drugs drugs (
Atropine)