HISTORICAL DEVELOPMENT
PHARMACOLOGY                                     1. HIPPOCRATES (460-325BC)
Introduction to Pharmacology:                       -Father of Medicine
                                                    -Develop aspirin
Pharmacology is the study of the actions,
mechanisms, uses and adverse effects of
drugs.                                           2. THEOPHRASTUS (380 BC)
                                                    -“Father of Pharmacology”
“Pharma”- drugs , “logos”
Pharmacology is the study of the actions,        3. AVICENNA (980-1027)
mechanisms, uses and adverse effects of             -“Canon of Medicine”
drugs                                               -Galenic Medicine
History of Pharmacology
                                                    “Poisons in Small doses are the
From the beginnings of time, pharmacology
                                                    best medicine” – William
has had a place in human history in all
                                                    Withering (1759)
cultures. The initial primitive pharmacology
knowledge developed from experiences on
which plants when eaten were safe and               Drug Evaluation & Regulation
which were toxic. In such a fashion a               The sale and use of drugs are
catalogue of good and bad evolved and was           regulated in almost all countries by
passed down through oral traditions. The            governmental agencies. In the United
story of pharmacology is an evolution from          States, regulation is by the Food and
the historic herbal traditions of many              Drug Administration (FDA). New
cultures through to definition of active            drugs are developed in industrial or
principles and refinement of action based on        academic laboratories. Before a new
chemical     synthesis    and     a   strong        drug can be approved for regular
understanding of physiology and protein             therapeutic use in humans, a series
structure. The pharmacology story is played         of animal and experimental human
at many levels but has as its underpinning          studies must be carried out.
the definition of pharmacology as a science         Before receiving the approval of the
with theories and principles discovered and         FDA< drugs must pass the several
accepted by rigorous investigation.                 stages, Preclinical trials and stages
                                                    1,2,3 studies,
  :All drugs derived from plant
  :All drugs are plant based                         Preclinical trials
  :ancient discovere that extracts from                -tested on laboratory animals
  plants and animals had medicinal effect.             for a main purpose
  :Kuhaon ang enzyme and make it synthetic
                                                       1. determine whether they
  to become effective                                  have the presumed effects in
                                                       living tissue
                                                       2. evaluate any adverse
                                                       effects
                                                        10. Drug misuse- improper use of
                                                            medications
         Phase1                                        11. Drug Abuse- inappropriate intake of
          -use human volunteer to test                      substance ex. Cocaine- local anesthesia
                                                        12. Drug Dependence- persons reliance on
            the drug, might be paid                         or need to take a drug
                                                            2 types
         Phase 2                                           1. Physiological Dependence- due to
          -to try the drug in patients                             biochemical changes in the body
                                                            2. Psychological              Dependence-
          who have the disease that the
                                                                   emotional reliance on a drug
          drug is meant to treat                        13. Drug Habituation- mild form of
          - patient are informed of the                     psychological dependence
          risks and fully monitored                     14. Illicit Drug- Street drug that are those
                                                            sold illegally
                                                        15. Dose- aim to give a patient a dose of the
         Phase 3                                           drug without causing harmful side
            - Use of drug in a vast                         effects
              clinical market                           16. Therapeutic Index- measure tha danger
         Phase 4                                           of poisoning
                                                        17. Bioavailability- a drug dose that reach
          -prescribers are obligated to
                                                            the peak of the serum, depending on the
          report to the FDA any                             drug route
          unexpected adverse effects                    18. Tolerance- decreasing response to a
                                                            repetitive drug disease
FDA Approval process can take 5-6 years
                                                             CONCEPTS OF PHARMACOLOGY
TERMINOLOGIES                                       PHARMACOKINETICS- the study of the time
                                                    course of drug absorption, distribution,
   1.   Pharmacology- studies the effect of the     metabolism, and excretion. The movement of the
        drugs on the body                           drug through the body
   2.   Pharmacopeias- total of authorized
                                                    PHARMACODYNAMICS- effect of drug on the
        drugs within the country
                                                    body
   3.   Medication- substance administered for
        diagnostic cure                             PHARMACOTHERAPEUTICS- clinical using of a
   4.   Prescription- written description for the   drug/use of drug/ purpose of drug
        preparation of and the administration of    PHARMACOGNOSY-study of natural (plant or
        the drug                                    animal)
   5.   Therapeutic effect- primary effect
        intended that is the reason the drug is     Ex: serpentina for diabetes side effect depression
        prescribed                                  Synthetic drug- gisundog ang compound para
   6.   Side effect- secondary effect of the drug   makuha ang same effect
   7.   Drug toxicity- harmful effect of the drug
        on an organism                              TOXICOLOGY- side effect of the drug
   8.   Drug Allergy- immunological reaction to
        a drug *provide skin test
   9.   Drug Interaction- administration of one
        drug before or after or both drug
                                              DRUG CLASSIFICATION
NAME OF DRUGS                                 Pharmacologic Classification- group of
Generic Name- given for the drug to being     active moieties that share scientifically
official name                                 documented properties and is defined on
                                              the basis of any combination of three
Ex:
         PARACETAMOL                          attributes of the active moiety:
           (Ibuprofen)
                             -Generic name           Mechanism of Action (MOA)
Official Name- name under which it is under          Physiologic Effect (PE)
publication                                          Chemical Structure (CS)
Chemical Name- Name by which the chemists
                                              The pharmacological effect is the lowering of
knows it                                      the blood pressure.
Trademark/Brandname- name given by the drug   Ex: Penicillins, Beta blockers, antibiotics
manufacturer
                                              Therapeutic Classification- may not have
NDC Number- National Drug code number used    similar chemical makeup.
to identify a specific drug
                                              They help protect you from severe side
                                              effects and drug interactions.
                                              Generic- barato      Branded- mahal
                                              Parkinson’s Disease- lack of dopamine
READ A DRUG LABEL                             Teratogenesis- congenital malformations
                                              produced in an embryo or fetus
                                                 ROUTE ADMINISTRATION
                                                  1. Oral - Administration to or by
                                                      way of the mouth, most
                                                      common, convenient route
                                                  2. Sublingual- drug placed under the
                                                     tongue -not swallow but kept in
                                                     mouth-
                                                  3. Buccal- drug placed to the cheeks
                                                     – drug kept in mouth not swallow-
Soure of Drug
                                                  4. Rectal- suppository,
Plants- such as digitalis                             Administration to the rectum
                                                     PARENTERAL ROUTES- Drugs w/
Human and Animals- such as
                                                     needles
epinephrine,insulin
                                                  5. Subcutaneous (SQ)- below the
                                                     skin - 45 °
                                                  6. Intramuscular (IM)- into the
                                                     muscle - 90 °
   7. Intradermal (ID)- into the dermal         6. Right Documentation - Make sure
      layer of the skin -shallow (10-15 °)         to write the time and any remarks on
   8. Intravenous(IV)- directly into the           the chart correctly
      bloodstream through the vein              7. Right History and Assessment-
   9. Inhalation- apply drug directly              Secure a copy of the client’s history
      unto lungs                                   to drug interactions and allergies
      Topical Route-drops applied               8. Drug approach and Right to
      locally to the skin                          Refuse - Give the client enough
                                                      autonomy to refuse the medication
      Opthalmic route- loal conditions
                                                      after thoroughly explaining the
      of the eye
                                                      effects
                                                9. Right Drug-Drug Interaction and
                                                   Evaluation- Review any medications
                                                   previously given or the diet of the
                                                   patient that can yield a bad
                                                   interaction to the drug to be given.
                                                   Check also the expiry date of the
                                                   medication being given.
                                                10.    Right Education and
                                                      Information.- Provide enough
                                                      knowledge to the patient of what drug
10 Rights of Drug Administration                      he/she would be taking and what are the
                                                      expected therapeutic and side effects.
   1. Right Drug.- check and verify if it’s
        the right name and form. Beware of            PHARMACOLOGY BASICS
        look-alike and sound-alike
        medication names.
                                                      1. Pharmacokinetics- The activity
   2.   Right Patient- Ask the name of the
                                                         of drugs in the body over a
        client and check his/her ID band
                                                         period of time, including the
        before giving the medication. Even if
                                                         processes by which drugs are
        you know that patient’s name, you
                                                         absorbed, distributed in the
        still need to ask just to verify.
                                                         body, localized in the tissues, and
   3.   Right Dose- Check the medication                 excreted.
        sheet and the doctor’s order before
                                                      2. Pharmacodynamics- study of
        medicating. Be aware of the
                                                         the effect of the drugs in the
        difference between an adult and a
                                                         body
        pediatric dose.
                                                      3. Pharmacognosy- study of the
   4.   Right Route- Check the order if it’s             origin. the study of medicines or
        oral, IV, SQ, IM, etc..                          crude drugs produced from
   5.    Right Time and Frequency - Check                natural sources such as plants,
        the order for when it would be given             microbes, and animals.
        and when was the last time it was             4. Pharmacotherapeutics- the
        given.                                           use of drugs for the prevention,
          treatment, diagnosis, and          *by binding to receptors on or within
          modification of normal functions   body cells drugs can:
       5. Toxicology- side effect
                                             -mimic or block the action of chemical
                                             messengers
           LIFE CYCLE OF A DRUG
           Absorption- movement of a         AGONIST DRUGS- mimic or support the
           substance                         drug
           Distribution- transport           ANTAGONIST DRUG- compete to block
           Digestion/metabolism-             the action of endogenous messengers
           biotransformation/converting
                                             COMMON DRUG RELATIONSHIP
           drug to
           Excretion- removed from the       Addition- the combined effect of two
           body                              drugs equals the sum of effect e
Slow Absorption- oral, sublingual,           Of each drug taken alone
transdermal, rectal                          Antagonism- the action of one drug
Fast Absorption- Parenterally, inhalation    negates the action of a second drug
         Drug Actions                        Potentiation- effect occurs within a drug
                                             increases or prolongs their action of
*Drugs work by a variety chemical
                                             another drug and the total effect is
mechanism
                                             greater than the sum of each drug used
*Drugs can be used to restore and            alone
maintain homeostasis
                                             Synergism- joint action of drugs in w/c
MESSENGERS AND RECEPTORS                     their combined effect is more intense or
-messengers communicate through the          longer in duration
action of chemical messengers, which
they produce and send into extracellular
                                             BIOAVAILABILITY- a drug dose that reach
fluids.
                                             the peak of your serum depending on the
Chemical Messengers: Histamine,              drug route
prostaglandin
                                             High bioavailability- fast absorption, no
Messengers- recognize and communicate        liver metabolism
with target cell via receptor
                                             Why do we need to know bioavailability?
Receptors- receptor site may have
                                             -to determine correct route of
specifity, respond only to certain
                                             administration
messengers
                                             -to determine correct dosage
MECHANISM OF DRUG ACTION
                                             DRUG CALCULATION
-Drugs act like chemical messengers to
perform their specific actions in the body   D/H x Q = x
EX: 750 MG ( Doctors order) X1tab= 1.5 TAB        Beta1- cardio, heart, -INC. heartrate
  500 MG – STOCK                                  Beta2- pulmonary,lungs, Bronchodilation,
                                                  (salbutamol-asthma)
PREVENTING MEDICATION ERROR
                                                  Alpha and beta adrenergic Agonist- they
*careful calculations,double checking             mimic or support the neurotransmitter
math and checking with other registered
                                                  -stimulates alpha1,beta1,beta 2
nurse may prevent medication error
                                                  *epi- shock,bronchospasm,glaucoma,cardiac
*infants and young children may receive
                                                  arrest
small dosage of calculations
                                                  *norepi- shock and cardiac arrest
                                                  *Dopamine- drug of choice for shock
                                                  *If hypertensive, do not drink neozepsince it
                                                  causes increase BP.
                                                  Clonidine(Catapres)- stimulates alpha2 agonist
                                                  *antihypertensive
                                                  INCREASED IN HR= INCREASED IN OXYGEN
NERVOUS SYSTEM                                    DEMAND
                                                  Adrenergic- drugs that stimulate the sympathetic
    CNS          PERIPHERAL NS                    NS
                                                  -they mimic the sympathetic neurotransmitter
                                                  PARASYMPATHETIC/cholinergic- they mimic the
              SOMATIC          AUTONOMIC          neurotransmitter acetylcholine
               (voluntary)     (involuntary)      Cholinergic Receptors
                               SYMPATHETIC
                              (adrenergic)        Muscurinic       Nicotinic
                             *neurotransmitter    M1-eyes          neuromuscular
                         (give signal and bind)   M2-cardiac
                          -epinephrine            M3-lacrimation
                          - norepinephrine        M4&M5-cognition(IQ)
                          -dopamine               Direct Acting:
                         PARASYMPATHETIC          Decrease HR,BP, Increase Peristalsis
                          (cholinergic)           Acetylcholine-dec. HR,BP meiosis
                             -acetylcholine       Carbachol- miotics(naay glaucoma,eyedrop)
SYMPATHETIC                                       Pilocarpine- constrict ang pupil, inc outflow
Alpha1- vasoconstriction to increase BP           Bethanicol-para makaihi,bladder contraction
Alpha2- vasodilation to decrease BP
Indirect acting-increase acetylcholine by blocking   pancreas is a long, slender organ located near the
acetylcholinesterase                                 stomachPancreatic islets, clusters of cells
                                                     formerly known as the islets of Langerhans,
Edrophonium- given for myasthenia gravis-muscle
                                                     secrete glucagon and insulin. Glucagon plays an
weakness
                                                     important role in blood glucose regulation
Physostigmine- maintenance for Myastenia G.          because low blood glucose levels stimulate its
Neostigmine                                          release. elevated blood glucose levels stimulate
                                                     the release of insulin.
Pyridostigmine-given for POST OR
                                                     Insulin facilitates the uptake of glucose into
Drugs for Alzheimers                                 skeletal and adipose body cells.
Bonepezil,Rivastigmine,Galantimine                   Type 1 diabetes is an autoimmune disease
CHOLINERGIC ADVERSE EFFECT                           affecting the beta cells of the pancreas. Does not
                                                     release insulin. synthetic insulin must be
Diarrhea, Urination, Miosis/Muscle weakness,         administered by injection or infusion
Bronchorrhea,Bradycardia,Emisis,Lacrimation,Sali
vation&sweating                                      Types of Insulin
Trihexyphenidyl&Benztropine- drug given for          Rapid Acting: Lispro, Aspart,Glulisine
Parkinson’s disease                                  -mealtime insulin, act very quickly
OTHER DRUGS:                                         Short Acting- taken before meals
Food poisoning-muscarine                             Intermediate Acting- Absorbed most slowly and
Pilocarpine, dry mouth, eye rdop for glaucoma        last longer.Often combined with rapid/short
                                                     insulin
Edrophonium-drug for tensilon test(myasthenia
gravis)                                              Long Acting-absorbed slowly,used to control
                                                     blood sugar overnight, while fasting and between
DRUGS AFFECTING REPRODUCTIVE SYSTEM                  meals- -Glargine&Detemir- SC only
Female sex hormones both can be used to              Adverse Reaction To Insulin
replace missing hormones or to decrease the
release of endogenous hormones. The female sex       Lipodystrophy at the site of the injection.When
hormones include estrogen and progesterone.          often injecting the same site, the skin may shrink
                                                     or thicken
Estrogens- Used for hormone replacement
therapy (HRT) in small doses when ovarian            Type 2 Diabetes- cells donot response to the
activity is blocked or absent.                       insulin produce
Antiestrogen-unovulontary infertility                ORAL Agents- Metformin, sulfonylureas,
                                                     Meglitinides ,Acarbose, Thiazolidinediones
PCOS- given estrogen
Progestins- Prevent follicle maturation and
ovulation as well as uterine contraction.
Mifepristone& misoprostol- drug for abortion,
abort by bleeding
Estrogen- hormone replacement
Progesterone-support pregnancy
ANTIDIABETIC DRUGS
Arrythmic Drugs- for irregular rhythms
JEAHAN JAYNE ABALO BSN2A
ST JOHNPAUL II COLLEGE OF DAVAO
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