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PHARMACOLOGY NOTES

(NCM 106)

➢ Four dominant methods:


PHARMACOLOGY
○ By therapeutic use, types of
➢ Derived from two Greek words: condition they are used to treat.
-PHARMAKON (MEDECINE) ○ By the mechanics of action, specific
-LOGOS (STUDY) biochemical reaction that occurs
 Related to pharmacokinetics & when you take a drug
pharmacodynamics ○ By their mode of action, specific
 Therapeutic (intended) way in which the body respond to
 Potential side effects drug
(unintended/unavoidable) ○ By their chemical source
 Classification:
> Analgesic: decreases body pain ➢ The purpose of drug classification:
> Antipyretic: lowers body temp ○ To ensure that you use a drug
safely to achieve outmost benefit
PHARMACOKINETICS ○ Ultimately, every time you take a
drug, your body chemistry is
➢ Medicine- through mouth (takes up to altered
30 mins to see effect) ○ This effects is meant to be
Ex. therapeutic, it can also cause side
Caplet: neozep effects that are harmful.
Enteric coated: enervon ○ Moreover, if you take multiple
Dragee: size of nips drugs, your body chemistry
may be changed in such a way that
DISINTEGRATION a drug is far less effective or the
- Breakdown of tablet into smaller pieces side effects are far more severe.

DISSOLUTION ➢ Drug-Drug Interactions


- Dissolving smaller particles in GI fluid The effectiveness of a drug can often be
before absorption reduced if the action of one drug
diminishes the action of another.
RATE LIMITING
- Time it takes for the drugs to •antacids invariably work by blocking
disintegrate and dissolve to become stomach acid but, by doing so, deplete
available the stomach of the acids needed to
break down and absorb a class of HIV
• Nephrotoxic- affects your kidneys drug known as protease inhibitors. If the
• Hepatotoxic- affects your liver medications are taken together, the HIV
drug will be less able to control the viral
infection
DRUG CLASSIFICATION
- Term used to describe medication that Drug Resistance
are group together because of their
similarity • Medications used to treat chronic
infections do so in a specific way.
1. Chronic: lasts longer than six months
and can continue when the injury or • If used incorrectly or for a long period
illness has been treated. of time, a drug may lose its potency as
the infection becomes resistant to its
2. Acute: happens quickly and goes away effects.
when there is no cause.

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➢ Drug Resistance ➢ Drug Approval Drug Names
• Medications used to treat chronic infections Each drug may have several names
do so in a specific way.
• Chemical Name
• If used incorrectly or for a long period of - Describes the drugs chemical structure
time, a drug may lose its potency as the (most meaningful to the chemist)
infection becomes resistant to its effects.
• Generic Name
• If this occurs, other drugs of the same class - Official name for the drug
may also fail or not work as well. - Not owned by any drug company
• e.g. Antibiotics - Universally accepted

➢ Parts of the prescription • Brand Trade Name


- A registered trademark of a drug
The superscription or heading with the company, easier to spell pronounce
symbol "R" or "Rx", which stands for the - Cardizem (brand) diltiazem HCL (generic)
word recipe (meaning, in Latin, to take)
➢ Drug Approval Pregnancy
The inscription, which contains the names
and quantities of the ingredients; • FDA developed a classification system
related to the effects of drugs on unborn
The subscription or directions for child (fetus) In drug books and literature,
compounding the drug, and pregnancy category is indicated for most
drugs
The signature which is often preceded by the
- A- No risk to fetus based on studies
sign's standing for signa (Latin for mark).
- B-Little to no risk based on animal studies,
giving the directions to be marked on the
some human studies
container
-C-Risk indicated based on animal studies,
Risk vs. benefit
➢ Essentials of medication order
-D- Risk to fetus proved Risk vs. benefit to
mother
The drug order, written by the physician, it
-X-Risk proved Avoid during pregnancy
has 7 essential parts for administration of
drugs safely. The nurse should know how to
➢ Prescription & over-the-counter drugs
read a drug order.
• Legal drugs are obtained either by a
It should have the following components:
prescription(Rx)or over the counter (OTC)
1- Patients full name.
2- Date and time.
There are major differences between the
3- Drug name.
two methods of dispensing drugs.
4- Dosage.
- To obtain prescription drugs, the
5- Route of administration.
person must receive a written order
6- Time and frequency of administration.
from a person with the legal authority
7- Signature of physician.
to write such a prescription.
➢ Forms of Oral Medications
Pharmacokinetics
-The process of drug movement to achieve
❖ Capsules drug action
-Cannot be broken or divided
❖ Tablets 4 processes: Absorption, distribution,
-Only divided if scored metabolism (Biotransformation), and
-Coated tablets are not to be broken excretion (elimination) - ADME
❖ Liquids
-May be measured in a medication cup, The nurse must be alert to any adverse drug
syringe or calibrated dropper effects and to report such findings promptly.

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➢ Absorption Medication
Passage of drug from its site of Is a substance administered for the diagnosis,
administration into the blood circulating sure, treatment, or relief of a symptom of for
body fluids preservation of disease.

• Rate of absorption depends on the route Pharmacology- study of the effect of drugs
of administration Enteral. Parenteral and Prescription- written direction for the
percutaneous. preparation and administration of a drug.

Purpose of medication:
• Passive, active, and pinocytosis are
different types of absorption
Drugs can BE ADMINISTERED For these Purposes:
- the ingestion of liquid into a cell by
the budding of small vesicles from ✓ Diagnostic Purpose:
the cell membrane. to identify any disease.

• Bioavailability is a subcategory of ✓ Prophylaxis


absorption - the percentage of the drug to prevent the occurrence of disease.
dose that reaches the systemic circulation
• Occurs after absorption and hepatic drug EX. Heparin po prevent Thrombosis or antibiotics
• Oral route is always less than 100% to prevent infection.
• Intravenous route is usually 100%
✓ Therapeutic purpose: To cure the Disease
➢ Distribution
The ways in which drugs are transported Uses of Drugs
by the circulating body fluids to the sites of
action • Prevention - used as RH prophylaxis to prevent
Diseases (EG. vaccines, Fluoride - Prevents Tooth
• Influenced by blood flow, affinity to the Decay)
tissue, and protein binding effect drugs are
distributed in the plasma (liquid part of the • Diagnosis - establishing patient's disease or
lymph and blood) and are bound to varying problem (e-6. Radio contrast dye, Tuberculosis
degrees w/ protein (albumin) (Mantoux Testing)

• Suppression- suppresses the Signs and


• Portion of drug bound is inactive - not
symptoms and prevents the disease process from
available to receptors
Progressing.
• Portion of drug unbound is free, active
- only free drugs can cause a • Treatment- alleviate the symptoms for patients
pharmacologic response with Chronic Disease (e.g. Anti-Asthmatic Drugs)
- some circulating drugs
(anticonvulsants, aminoglycosides) • Cure- complete eradication of diseases (e.g.
are checked for drug blood levels Antibiotics, Anti-Helminthic)

• Need to be aware of the condition of


your client - liver or kidney disease = low Storage medication:
serum albumin level less protein-binding - medications are disposed by the pharmacy
sites = excess free drug = drug toxicity to nursing units. Once delivered, proper
storage becomes the responsibility of the
✓ Remember - The amount of drug that nurse. All medications must be store in a
actually reaches the receptor sites cool dry place (usually in cabinets, medicine,
determines the extent of cart or fridge).
pharmacologic.

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PRINCIPIES OF MEDICATION 5. ASAP
ADMINISTRATION -not as urgent as stat
-as soon as possible
Principles include 3 Checks and 10 RIGHTS: -should be available for administration
to the patient with 30 mins of the
➢ 3 CHECKS ARE: written order

1) CHECK when obtaining the container of 6. ROUTINE ORDER


medicine. -orders not written as stat, asap, now
or prn
1) CHECK when removing the medicine from -usually carried out within 2 hrs. of the
The container. time the order is written by the
physician
3) CHECK when replacing the container.

Dosage Calculations
RIGHTS OF MEDICATION ADMINISTRATION
Basic drug calculation:
1) RIGHT to patient
2) RIGHT medication desired dose quantity (v) vehicle form
3) RIGHT time stock on hand & amount which the drug
4) RIGHT dose come
5) RIGHT route
6) RIGHT to information on drug/client
education
7) RIGHT to refuse medication
8 ) RIGHT assessment e.g. order, Ampicillin (Himox) 350 mg
Stock: Ampicillin (Himax) 500 mg in 5 ml
9) RIGHT documentation
vial
10) RIGHT evaluation
D
➢ Types of medication orders
V = A
H
1. STAT ORDER
-indicates that the medication is to be given D= Desired drug dose
immediately and only once. H= Dose on hand
-often associated with emergency V= Vehicle (the drug form)
medications that are needed for life- A= Amount to be given to patient
threatening situation.
-should be administered within 5 mins or less
► How to calculate drug dosage?
of receiving the written order.
Common Conversions:
2. SINGLE ORDER,
-or known As one -time order indicates that ✓1 Liter = 1000 Milliliters
the medications are to be to be given once at
a specific time. ✓1 Gram= 1000 Milligrams

3. STANDING ORDER, is written in advance


✓1Milligram = 1000 Micrograms
carried out under specific circumstances.
✓1 Kilogram = 2.2 pounds
4. PRN ORDER, "PRN" larin word FOR "pro re
nata", WHICH means "As the thing is need" A
✓1 ounce = 30 mL
PRN order or as needed order, permits the
nurse to give a medication when the client Remember! Before doing the calculation, convert
requires it. units of measurement to one system.

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Example: Example #03:
Amount desired (D)= 10,000 UNITS
The ordered dose is Ceftriaxone 750 Amount on hand (H)=5000 UNITS/mL
mg IV. the container contain 1g in a Quantity (V) = 1ml
10 ml vial. How many mL should be given?

How to calculate? 10, 000units /5000unitsX 1ml = 2mL


You should convert first g to mg,
then:
How to Read Drug Labels
(D) 750 mg
X (V) 10 ml= 7.5 ml LEARNING OBJECTIVES
(H) 1000 mg On completion of the materials provided in this
chapter, you will be able to identify the following
parts of each drug label:
Example #1:
1 Trade name of the medication
2 Generic name of the medication
Dilantin 125 mg is available as 125
3 Strength of the medication dosage
mg/5ml. Dilantin 0.3 g is ordered. How
4 Form in which the medication is provided
much should the nurse administer to
5 Route of administration
the patient?
6 Total amount or volume of the medication
provided in the container
Step 1: Determine your givens.
7 Directions for mixing or preparation of the
medication if required
Amount desired (D)=0.3g
Amount on hand (H)=125mg
The safe administration of medications to patients
Quantity (V) = 5ml
begins with the nurse accurately reading and
Step 2: Convert 0.3g to mg (since the interpreting the drug label. Thus, it is important for
ordered dose is in grams but the drug is the nurse to be familiar and comfortable with the
available on hand in milligrams) information that is found on the drug label.

PARTS OF A DRUG LABEL


0.3g X 1,000 mg/g = 300mg

Step 3: Plug in what you know into the 1. TRADE NAME. The trade name (also known as
formula and simplify. brand or proprietary name) is usually capitalized
and written in bold print. It is the first name
written on the label. The trade name is always
300mg/125mgX 5ml = 12ml
followed by the ® registration symbol. Different
manufacturers market the same medication
under different trade names.
Example #02:
2. GENERIC NAME. The generic name is the official
Amount desired (D)= 150mg
name of the drug. Each drug has only one generic
Amount on hand (H)=300mg/mL
name. This name appears directly under the trade
Quantity (V) = 1ml
name, usually in smaller or different type letters.
How many tablets should be given?
Physicians may order a patient’s medication by
generic or trade name. Nurses need to be familiar
with both names and cross-check references as
150mg /300mgX 1ml = 0.5 tabs
needed. Occasionally, only the generic name will
appear on the label.

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3. DOSAGE STRENGTH. The strength indicates 1. Trade name: Keflex
the amount or weight of the medication that is 2. Generic name: cephalexin
supplied in the specific unit of measure. This 3. Dosage strength: 250 mg
amount may be per capsule, tablet, milliliter, 4. Form: Capsules
and 5. Amount: 100
so on. 6. Directions: Keep tightly closed.
Store at controlled room temperature
4. FORM. The form indicates how the drug is 59° to 86° F (15° to 30° C).
supplied. Examples of various forms are tablets, 7. NDC number: 0777-0869-02
capsules, liquids, suppositories, and ointments. 8. Manufacturer: DISTA
9. Expiration date: (Yellow highlight)
5. ROUTE. The label will indicate how the drug is
to be administered. The route can be oral,
topical, injection (subcutaneous, intradermal, Anti-Infective Agents
intramuscular), or intravenous.
Antibiotics:
6. AMOUNT. The total amount or volume of the
medication may be indicated. Some examples ▪ Sulfonamides
are 250 mL of oral suspension and a bottle that ▪ Penicillins
contains 50 capsules. ▪ Cephalosporins
▪ Tetracyclines
7. DIRECTIONS. Some medications must be ▪ Aminoglycosides
mixed before use. The amounts and types of ▪ Quinolones
diluents required will be listed along with the ▪ Macrolides
resulting strengths of the medication. This
information may also be found on package
inserts. Antibiotics
Medications used to treat bacterial
infections Ideally, before beginning
antibiotic therapy, the suspected
areas of infection should be cultured
(bld. culture & sensitivity)to identify
the causative organism and potential
antibiotic susceptibilities.

➢ Empiric therapy: treatment of


Other information may be found on drug labels: the name an infection before specific
of the manufacturer, expiration date, special instructions culture information has been
for storage, a National Drug Code (NDC) number, and
reported or obtained
contraindications.
➢ Prophylactic therapy: treatment
with antibiotics to prevent an
EXAMPLES FOR PRACTICE IN READING DRUG infection, as in intra-abdominal
LABELS surgery Bactericidal: kill bacteria

•Bacteriostatic: inhibit growth of


susceptible bacteria, rather than
killing them immediately; will
eventually lead to bacterial death

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➢ Antibiotics: Sulfonamides Body System: Integumentary
EFFECT: Photosensitivity, exfoliative
One of the first groups of antibiotics dermatitis, Stevens-Johnson syndrome,
epidermal necrolysis
sulfadiazine

• sulfamethizole ➢ Antibiotics: Penicillins


•sulfamethoxazole
•sulfisoxazole •Natural penicillins
•Penicillinase-resistant penicillins
•Aminopenicillins
➢ Sulfonamides: Mechanism of Action •Extended-spectrum penicillins

Bacteriostatic action
-Prevent synthesis of folic acid required for Natural penicillins
synthesis of purines and nucleic acid penicillin G, penicillin V potassium
-Does not affect human cells or certain
bacteria-they can use preformed folic acid Penicillinase-resistant penicillins
cloxacillin, dicloxacillin, methicillin, nafcillin,
oxacillin
➢ Sulfonamides: sulfamethoxazole
Therapeutic Uses Aminopenicillins
amoxicillin, ampicillin, bacampicillin
Azo-Gantanol
•Combined with phenazopyridine (an Extended-spectrum penicillins
analgesic-anesthetic that affects the mucosa of piperacillin, ticarcillin, carbenicillin, mezlocillin
the urinary tract).
•Used to treat urinary tract infections (UTIs)
and to reduce the pain associated with UTIs. ➢ Antibiotics: Penicillins

Bactrim •First introduced in the 1940s


• Combined with trimethoprim. •Bactericidal: inhibit cell wall synthesis • Kill a
• Used to treat UTIs, Pneumocystis carinii wide variety of bacteria
pneumonia, ear infections, bronchitis, • Also called "beta-lactams"
gonorrhea, etc. •Bacteria produce enzymes capable of
destroying penicillins.
Azo-Gantrisin •These enzymes are known as beta-
•Combined with phenazopyridine lactamases.
•Used for UTIs •As a result, the medication is not effective.
Chemicals have been developed to inhibit
Pediazole these enzymes:
•Combined with erythromycin
•Used to treat otitis media - clavulanic acid
- tazobactam
- sulbactam
➢ Sulfonamides: Side Effects
•These chemicals bind with beta lactamase
Body System: Blood and prevent the enzyme from breaking down
EFFECT: Hemolytic and aplastic anemia, the penicillin
thrombocytopenia •Penicillin-beta-lactamase inhibitor
combination drugs:

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•These chemicals bind with beta ➢ Penicillins: Side Effects
lactamase and prevent the enzyme from
breaking down the penicillin  Common side effects:
✓ nausea, vomiting, diarrhea,
•Penicillin-beta-lactamase inhibitor abdominal pain
combination drugs: ✓ Other side effects are less
- ampicillin + sulbactam = Unasyn common
- amoxicillin + clavulanic acid =
Augmentin
- ticarcillin + clavulanic acid = ➢ Antibiotics: Cephalosporins
Timentin
- piperacillin +tazobactam = Zosyn, ▪ First Generation
Tazocin ▪ Second Generation
▪ Third Generation
▪ Fourth Generation
➢ Penicillins: Mechanism of Action

-Penicillins enter the bacteria via the cell ➢ Antibiotics: Cephalosporins


wall.
• Inside the cell, they bind to penicillin- -Semisynthetic derivatives from a
binding protein. fungus
• Once bound, normal cell wall synthesis -Structurally and pharmacologically
is disrupted. related to penicillins
• Result: bacteria cells die from cell lysis. -Bactericidal action
• Penicillins do not kill other cells in the
body.
 Broad spectrum

➢ Penicillins: Therapeutic Uses - Divided into groups according to


their antimicrobial activity
-Prevention and treatment of infections
caused by susceptible bacteria, such as:
- gram-positive bacteria  Broad-spectrum antibiotic
- Streptococcus, Enterococcus,
Staphylococcus species - The term broad-spectrum refers
to an antibiotic that acts against a
wide range of disease-causing
➢ Penicillins: Adverse Effects bacteria.

- Allergic reactions occur in 0.7% - - A broad-spectrum antibiotic acts


8% of treatments against both Gram-positive and
- urticaria, pruritus, angioedema Gram-negative bacteria,in
- 10% of allergic reactions are life contrast to a narrow-spectrum
threatening and antibiotic, which is effective
- of these are fatal against specific families of
bacteria.

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➢ Cephalosporins: First Generation •ceftriaxone
• ceftazidime
• cefadroxil • cefoperazone
•cephalexin • cefotaxime
•cephradine • moxalactam
• cefazolin
•cephalothin - Most potent group against gram-negative -
•cephapirin Less active against gram-positive
- Good gram-positive coverage
- Poor gram-negative coverage
- used for surgical prophylaxis. URTI otitis media ➢ Cephalosporins: Third Generation

➢ Cephalosporins: Second Generation cefixime (Suprax)


-Only oral third-generation agent
• cefaclor Best of available oral cephalosporins against
• cefonicid gram-negative
•cefprozil • Tablet and suspension
• ceforanide
• cefamandole ceftriaxone (Rocephin)
•cefmetazole -IV and IM, long half-life, once-a-day dosing
•cefoxitin Easily passes meninges and diffused into CSF
•cefotetan to treat CNS infections
• cefuroxime
- Good gram-positive coverage
Better gram-negative coverage than first ➢ Cephalosporins: Third Generation
generation
ceftazidime (Ceptaz, Fortaz, Tazidime, Tazicef)

➢ Cephalosporins: Second Generation •IV and IM


• Excellent gram-negative coverage
✓Cefoxitin • Used for difficult-to-treat organisms such as
Pseudomonas spp.
- (Mefoxin) IV and IM •Eliminated renally instead of biliary route
•Used prophylactically for abdominal or •Excellent spectrum of coverage
colorectal surgeries
•Also kills anaerobes
➢ Cephalosporins: Fourth Generation
√cefuroxime

-(Kefurox and Ceftin) PO cefepime (Maxipime)


•Surgical prophylaxis •Newest cephalosporin agents.
•Does not kill anaerobes
- Broader spectrum of antibacterial
activity than third generation, especially
➢ Cephalosporins: Third Generation against gram-positive bacteria.

•cefixime - Cephalosporins S/E is similar to


•ceftizoxime penicillins
•cefpodoxime proxetil

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 Metabolism > Pharmacodynamics Peak. Onset, Duration

→ Major mechanism of the


termination/inactivation of drug action • Onset of action time it takes to reach the
minimum effective concentration
• Liver is primary site where drugs are - Peak action- When the drug reaches its
inactivated by liver enzymes, become inactive highest blood or plasma concentration
metabolites or H20 (soluble substances), for - Duration of action Length of time drug has
excretion an effect
• Liver disease alters drug metabolism - drug
toxicity dit a decrease rate of metabolism
> Pharmacodynamics: Therapeutic
❖ Half-life (112) - the time it takes for 1/2 Index/Range
of a drug to be eliminated
•Safety of drugs is a major concern

 DRUG HALF-LIFE (t₁/2) Therapeutic index - estimates the margin of


safety of a drug
Half-life is the time required to reduce the
plasma concentration to 50% of its original Low therapeutic index = narrow safety
value
•High therapeutic index wide safety margin, less
▪ Will determine dosing requirements / danger of toxic effects
how long a drug will remain in the body
▪ Used in determining dosing interval Therapeutic range = area between the minimum
▪ Goal - Plateau effective concentration & min toxic
concentration of a drug
Half-life

• The half-life of a given medication is how Principles of Drug Administration


long it takes for the body to get rid of half of
the dose.
• Nurses are accountable for the safe
administration of medications
 Excretion • Nurses are legally liable when giving prescribed
drugs - Even if the dosage is incorrect, or the drug
• Drug removal from the body is contraindicated
• Main route is through the urine - other • Nurses are liable for the predicted effects of a
routes = bile, feces, lungs, breast milk drug once it is given
• Urine pH influences excretion
•Kidney disease affects excretion
➢ A nocebo effect, is said to occur when
negative expectations of the patient
➢ Pharmacodynamics regarding a treatment cause the treatment
to have a more negative effect than it
Def: The drugs mechanism of action otherwise would have.
→ Drug response can cause a primary or
secondary physiologic effect, or both - e.g. when a patient anticipates a side effect
→ Primary effect desirable of a medication, they can suffer that effect
→ Secondary effect desirable or even if the "medication" is actually an inert
undesirable substance

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In chemistry, the term chemically inert is ➢ Potency and Efficacy
used to describe a substance that is not
chemically reactive. Most Group 8 or 18 • Potency is an expression of the
elements that appear in the last column of activity of a drug in terms of the
the periodic table (Helium, Neon, Argon, concentration or amount of the drug
Krypton, Xenon and Radon) are classified as required to produce a defined effect
inert (or unreactive) - the maximum response
achievable from a
pharmaceutical drug in research
> The placebo effect, is said to occur when settings, and to the capacity for
positive expectations improve an outcome. sufficient therapeutic effect or
beneficial change in clinical
- Both placebo and nocebo effects are settings.
presumably psychogenic

- Psychogenic (psychiatry) originating So therefore...


from or caused by state of mind;
having a psychological rather than a Potency is an expression of the activity
physiological cause of a drug, in terms of the
concentration or amount needed to
produce a defined effect."
Term Meaning
• Both Drug A and Drug B achieve
the same maximum effect, i.e.
ED Effective Dose
they have equal efficacy.
TD Toxic Dose However, drug A achieves this
effect at a lower dose. Thus,
LD Lethal Dose Drug A has higher potency than
TI Therapeutic Index Drug B

TR Therapeutic Ratio

➢ Agonists and antagonists

*Graded Dose Response Relationship &


Therapeutic Response •Agonists
- activate receptors to produce
Drug dose-response relationships are the desired response.
important in assessing the efficacy and
potency of drugs. •Antagonists
- prevent receptor activation.
- They are also useful for the - Antagonists decrease cellular
interpretation of drug and receptor function if they block the action
interactions. of a substance that normally
increases cellular function.
- There are two types of drug dose-
response relationships:

1. the graded dose-response


2. the quantal dose-response
relationships

PHARMACOLOGY NOTES Page 11

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