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    Pharmacology and

    Therapeutics

    Lecturer:Isaac Amankwaa

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    COURSE OBJECTIVES

    By the end of the course the student will:

    Discuss the various sources of drugs

    Explain the principles of pharmacology: pharmacokinetics and

    pharmacodynamics

    Explain the indications, dosages, actions, side effects,

    contraindications, drug interactions and nursing implications of

    drugs on the various systems of the body

    Identify the nursing responsibilities in administering the various

    drugs

    Apply current drug policies in the country.

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    COURSE CONTENT

    1. Sources of drugs

    2. General drug metabolism

    3. Analgesics4. Anaesthesics

    5. Tranquilizers: major and minor

    6. Antidepressants7. Anticholinergics

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    Course content CTD

    8. Drugs acting on the cardio-vascular system

    9. Haematinics

    10.Drugs acting on the respiratory system11.Drugs acting on the digestive system

    12.Drugs acting on the urinary system

    13.Drugs used in infections14.Miscellaneous drugs

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    Course content CTD

    Antimetabolites

    Eye preparations

    Ear preparations Drugs acting on the endocrine system

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    TERMINOLOGIES

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    Application of Pharm to Nursing

    Class to be divided into 4 groups to discuss1. Role of the nurse in drug therapy

    2. Drug administration practices students

    observed (good & bad) during their lastclinical placement

    3. Why you think nurses must learn pharm in

    nursing.4. The nurse, pharmacist and doctor who plays a

    central role in drug therapy and why?

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    TERMINOLOGIES

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    PHARMACOLOGY

    The study of the interaction ofsubstances(drugs), other than foods, with

    living systems

    or

    It is the study of effect of drugs on living

    organisms.

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    THERAPEUTICS

    The use of drug to diagnose,

    prevent or treat diseases or to

    prevent pregnancy

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    Clinical Pharmacology

    The study of drugs in humans-

    includes the study of drugs in

    patients as well as healthyvolunteers

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    A drug/Medication:

    A chemical used in the diagnosis,

    treatment, or prevention of disease.

    They are used interchangeably.

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    Sources of drugs

    Two main sources:1. Natural

    2. Synthetic

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    Synthetic Sources

    Prepared by chemical reactions in thelaboratory.

    Majority of drugs prepared by this

    method.

    One such area is Biotechnology:

    manipulation of proteins to permit the large-

    scale industrial production of complex

    natural substances (e.g. hormones).

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    Drug names

    A drug may have about four names:.

    1. Chemical name

    2. Generic name (nonproprietary)

    3. Official name

    4. Trade name

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    Types of drug names Examples

    Chemical name N-Acetyl-para-aminophenol

    Generic name acetaminophen

    Trade names Paracetamol, Tylenol, EFPAC

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    Which name to use? Generic or trade?

    Disadvantages of using generic names

    They are long and complicated

    They are difficult to remember

    Disadvantages of trade names:

    unlimited trade names which create confusion.

    Can result in double medication

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    Controlled substances

    Can cause physical or psychologicaldependence or both.

    Its use is subject to considerablecontrol.

    The nurse has both legal and ethical

    responsibilities when administeringthese drugs.

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    Nonprescription or Over-the-counter

    drugs (OTCs)

    These are drugs that can be purchased

    without prescription.

    Considered relatively safe for the layperson to

    use when taken according to directions

    provided by the manufacturer

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    Medication orders

    Patient medications must have an order from

    the physician, nurse practitioner or medical

    assistant.

    Medication orders are written in the form of

    PRECRIPTION

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    Types of Medication orders

    1. A standing order: carried out as specified until it iscancelled by another order. E.g. Caps amoxicillin 500mgtds for 7 days

    2. As needed (p.r.n.) order3. Single order

    Directive is carried out only once at the timespecified by the physician.eg atropine given to

    preoperative patients4. Stat order

    Also a single order

    Carried out at once

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    Science

    of Pharma-cology

    Pharmacognosy

    Pharmacokinetics

    Pharmacodynamics

    PharmacotherapeuticsToxicology

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    EFFECTS OF DRUGS

    Drugs are given for two effects:

    Local effects

    Systemic effect

    Both can further be grouped into

    desirable and

    Undesirable effects

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    PRINCIPLES OF PHARMACOLOGY

    Chapter Two

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    1. Pharmacokinetics

    2. Pharmacodynamics

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    Pharmacokinetics

    Processes that affect a drug from the time it

    enters the body until it leaves the body

    It answers the question: how does the body

    handles medications.

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    Components of PK.

    Absorption (A)

    Distribution (D)

    Metabolism (M)

    Excretion (E)

    ADME

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    Absorption

    Passage of medication from administrative site till its

    entry into the systemic circulation.

    Determines how soon a drug becomes available to

    exert its action

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    Factors that influence absorption

    1. Route of administration: IM, Oral, IV

    2. Drug form e.g. tablet coating, liquid form,

    3. Surface area

    4. Blood flow

    5. Lipid solubility

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    Absorption of oral drugs

    The amount of drug reaching the systemic

    circulation is considerably less than the

    amount absorbed due to the extraction and

    metabolism of the drug by a process called

    first pass effect.

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    32

    Some of the drug is inactivated and not all will

    be available for use at its intended site of

    action.

    Drugs are therefore formulated to account for

    this difference in availability to the tissues.

    This is why different forms of drugs are not

    equal

    Bi il bili

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    Bioavailability

    The portion of a dose that reaches

    the systemic circulation and is

    available to act on body cells.

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    IV drugs- 100% bioavailability

    Absorption is rapid and 100% bioavailable.

    Avoids problems with stomach acid andintestinal absorption issues.

    IM drugs

    Not as rapid as IV.

    Better absorption if there is a good bloodsupply.

    Oral drugs

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    Routes that avoid 1stpass effect

    Sublingual and Bucal routes

    Absorbed into the highly vascularized tissue under

    the tongue or between the cheek and the gum-

    the oral mucosa

    Bypass the liver

    Rapidly absorbed.

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    Distribution

    After a drug is absorbed, the transportation of

    that drug from the bloodstream to the body

    tissues and intended site of action is called

    distribution.

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    Factors Affecting Distribution

    Blood supply to site of action: drug is distributed inthis order:

    a. Extensive blood supply: heart liver, kidney

    b. Areas of slower distribution: skin, fat

    c. Bones and brain

    Protein binding

    Degree of first pass effect.

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    Metabolism

    Series of chemical reactions that inactivates a

    drug by converting it into watersoluble

    compound so that it can be excreted by the

    body.

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    It takes place mainly in the liver and produces:

    1. An inactive metabolite

    2. A more soluble compound

    3. A more potent metabolite e.g. prodrugs.

    Levodopa is a prodrug of dopamine

    hydrochloride

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    Other organs or body tissues responsible for metabolism

    Liver (mainly)

    Skeletal muscle

    Kidneys

    Lungs

    Plasma

    Intestinal mucosa

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    Factors that decrease (delay) metabolism

    Cardiovascular dysfunction

    Renal insufficiency

    Starvation

    Obstructive jaundice

    Erythromycin or ketoconazole drug therapy

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    Excretion

    Removal of drugs from the body.

    Drugs and their metabolites can exit the body

    in urine, bile, sweat, saliva, breast milk, and

    expired air.

    The most important organ for drug excretion

    is the kidney.

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    Drug excretion

    Some drugs are excreted unchanged

    Patients who may require dosage

    reduction: Patients with kidney disease

    Children

    older adults

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    Half-life of a drug

    Time required for the serum

    concentration of a drug to decrease by

    50% or half of its original concentration.

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    Half-life of a drug

    Knowledge about drug half-life help in

    determining dosing interval

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    Pharmacodynamics

    Study of what drugs do to the body and how

    they do it.

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    Drug actions

    Drugs usually work in one of four ways:

    1. To increase cellular activities.

    2. To replace missing chemical3. To slow cellular activities

    4. To interfere with the functioning of

    foreign cells.

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    Receptor theory of drug action

    A drug will not act unless it is bound

    Most drugs cause their effects by interacting

    with specific drug receptors

    What are receptors

    Structures on a cell

    Have chemical structure that matches the shape

    and charge of the drug.

    Like the relationship btnx a key and lock

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    Types of drug-receptor interactions

    1. Agonist drug

    Able to interact and activate receptors

    Have two properties

    Affinity: ability of a drug to bind to a receptor

    Efficacy: tendency of a drug to activate a

    receptor once it is bound

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    A t i t d

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    Antagonist drug

    Able to interact with receptor but do not change

    the receptor

    Properties

    Have affinity

    Have no efficacy

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    Types of antagonist drugs

    Competitive antagonist

    Compete with the agonist drug for the same

    receptor site.

    Prevents the agonist from binding and therefore

    prevents the agonist from causing effect

    Effect of competitive antagonist can be overcome

    by giving greater dose of the agonist

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    Types of antagonist drugs

    Non-competitive antagonist

    Permanently occupy or change the receptor so

    that the agonist cant interact with it.

    The effect of non-competitive antagonist cannot

    be overcome by increasing the dose of the

    agonist.

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    The Dose-response relationship

    The bigger the dose of a given drug, the

    greater the effect

    Dose response relationship is dependent on

    A. Affinity

    B. Efficacy

    C. Potency

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    Efficacy

    The maximum effect produced by a drug.

    E.g. if 1 gm of drug A and B are administered to

    reduce patients pain and drug A does it at 80%

    and drug B does it at 50%, then drug A is said to

    be more efficacious than drug B.

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    Potency

    Amount of drug that is given to elicit an effect.

    A potent drug produces its effect at low doses.

    E.g. if 10 mg of drug A is administered and the

    effect is 60% and 20mg of drug B produces

    same 60% effect, then drug A is said to bemore potent than B.

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    Pain

    Definition

    Pain is an unpleasant sensory or emotionalexperience related to actual or potential tissue

    damage Stimulus for pain

    Chemical

    Mechanical electrical

    thermal

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    Classification of Pain

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    Classification of Pain

    Based on duration

    Acute pain: a sharp, intense pain of rapid onset

    occurring over a short period.

    Chronic pain: persistent or intermittent usuallydefined as lasting at least 6 months.

    Base on location

    Somatic pain: pain arising from body walls Visceral pain:pain arising from organs in the

    abdominal and thoracic cavities

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    Classification of pain

    Referred pain:pain that occurs at the site distant

    from the source of the disease or injury, usually of

    visceral source.

    Phantom limb pain:pain associated with a

    missing limb

    Emotional or psychogenic pain

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    Pathophysiology of pain

    1.Transduction

    2.Transmission

    3.Modulation

    4.Perception

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    Transduction

    Nociceptorsdetect pain stimuli;

    convert them into electrical

    impulse .

    Histamine, bradykinin,

    acetylcholine & serotonin

    increase the transmission of

    pain. Prostaglandins: increase the

    sensitivity of pain receptors.

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    Transmission

    Movement of pain stimulus from site of injury

    to the spinal cord.

    This signal travels along:

    1. A-delta fibers:

    smaller, myelinated & transmit pain signals rapidly

    produces the first fast or acute pain

    2. Type C fibres

    are larger, unmyelinated

    transmit the second pain that is normally dull, aching

    and burning in quality.

    The pain also last longer

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    Modulation

    In the spinal cord, the signal

    Produce a reflex

    gets sent the CNS to be

    perceived.

    Endogenous opioids (endorphins

    and encephalin) modulate intensity

    of the signal sent up to the brain.

    Perception

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    Perception

    Final stop

    Occurs in the brain

    It is also conscious subjective and emotional.

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    Analgesics

    Drugs that relieve or reduce pain

    without producing

    unconsciousness.

    2 types

    Non-narcotic/NSAIDs

    Narcotic analgesics

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    Non-narcotic analgesics

    AKA Cyclooxygenase inhibitors

    Group of drugs that relieve pain, fever, and/or

    inflammation

    E.g. include:

    Salicylates

    NSAIDs

    Acetaminophen

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    Classification of non-narcotic

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    Classification of non-narcotic

    analgesics

    1. Nonsteroidal anti-inflammatory drugs

    Have anti-inflammatory properties

    E.g. aspirin, ibuprofen, naproxen, diclofenac

    2. Acetaminophen

    Reduce pain and fever but cant suppress

    inflammation

    E.g. Tylenol or paracetamol

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    Mechanism of action

    Inactivates cyclooxygenases (enzyme required

    for prostaglandin formation)

    Two forms of cyclooxygenases

    COX-1

    COX-2

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    Cox-1

    Present in all tissues/cells

    Functions:

    blood clotting

    protect stomach lining,

    Decrease gastric secretion,

    increase mucus secretion.

    Inhibition: adverse effects of NSAIDs

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    Cox-2

    Active at sites of trauma, or injury and is

    associated with pain and other signs of

    inflammation.

    Inhibition of COX-2 results in therapeutic

    effects

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    Non-steroidal anti-inflammatory

    drugs (NSAIDs)

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    Introduction

    A non-narcotic analgesic

    So named because they dont belong to the

    steroids group

    Yet have anti-inflammatory & analgesic

    properties

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    Classification of NSAIDs

    First-generation NSAIDs

    Inhibit COX-1 and COX-2

    E.g. aspirin, ibuprofen and naproxen.

    Second Generation NSAIDs:

    Inhibit COX-2 only.

    Inhibit pain and inflammation with minimal risk

    of serious side effects. E.g. celecoxib.

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    Examples of NSAIDs

    Salicylates

    Ibuprofen

    Naproxen

    Diclofenac sodium

    Indometacin

    Celecoxib perixicam

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    Salicylates

    Pharmacologic Effects

    1. Analgesic

    2. Antipyretic

    3. Anti-inflammatory

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    f

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    Types of Salicylates

    Aspirin (acetylsalicylic acid)

    Magnesium salicylate

    Sodium salicylate

    All have similar in pharmacologic activity ( aspirin

    has greater anti- inflammatory effect

    Aspirin (acetylsalicylic acid): a

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    Aspirin (acetylsalicylic acid): a

    prototype

    Generic name:aspirin

    Trade names:Ecotrin,

    Classification:Antipyretic, Analgesic (non-

    opioid), anti-inflammatory, anitrheumatic,

    antiplatelet, salicylate and NSAID

    h i i

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    Therapeutic actions

    1. Suppression of inflammation:rheumatoid arthritis and

    osteoarthritis.

    2. Analgesia:mild to moderate pain e.g. headache &

    dysmenorrhea

    3. Reduction of fever: Inhibits pyrogen-induced synthesis

    of prostaglandins.

    h i i

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    Therapeutic actions

    4. Dysmenorrhea:Inhibits prostaglandin

    synthesis in the uterine smooth muscles.

    5. Suppression of platelet aggregation

    Synthesis of thromboxane A2 (TXA2) in the

    platelet promotes aggregation.

    Aspirin causes an irreversible inhibition of COX-1,

    the enzyme that makes TXA2.

    D

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    Dosages

    Aches and pains; fever: 325-650mg q 4 hrs.

    Acute rheumatic fever: 5-6gm/day/ divided doses

    Rheumatoid arthritis: 3.6-5.4mg /day/divided doses

    Acute MI: 160mg once a day

    Ischemic stroke/TIAs 50-325mg once a day

    Routes: Oral and Rectal

    Ad ff

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    Adverse effects

    GIT disturbances: e.g. dyspepsia andvomiting.

    Bleeding: due to inhibition of platelet

    aggregation. Renal impairment: inhibits synthesis of

    prostaglandins that cause vasodilation. Theresultant vasoconstriction decreases renal

    blood flow to the kidneys

    Allergy:

    Ad ff

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    Adverse effects

    Salicylism

    A syndrome: occurs when aspirin levels climb just

    slightly above therapeutic levels.The symptoms

    include:Dizziness& Tinnitus Reyes syndrome (rare but serious)

    Characterized by encephalopathy and fatty liver

    degeneration. Observed in children with influenza or chickenpox

    & taking aspirin.

    C t i di ti

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    Contraindication

    1. Hemophilia

    2. Children under 12 years

    3. GIT ulceration

    4. aspirin intolerance

    5. breastfeeding

    Ad ff t

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    Adverse effects GIT disturbances

    Salicylate toxicity produces a condition calledsalicylism. The symptoms include:

    Dizziness

    Tinnitus

    Impaired hearing

    Nausea

    Vomiting Mental confusion.

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    t i di ti

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    contraindication

    Heamophillics

    Chdn under 12 yrs

    GIT ulceration

    Breastfeeding

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    Ib f

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    Ibuprofen

    Generic Name: ibuprofen

    Trade/brand name: ????

    Classification: NSAID, Analgesic (non-opioid),

    priopionic acid derivative

    Dosage

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    Therapeutic action

    Exhibits anti-inflammatory, analgesic and

    antipyretic properties

    Has both central and peripheral effects

    Indications

    Relief S/S of rheumatoid arthritis

    Relief of mild to moderate pain Fever reduction

    Sid ff t

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    Side effects Dyspepsia

    vomiting,

    abdominal pains,

    heartburns,

    nausea,

    Diarrhoea Severe GI bleeding and Unceration

    C t i di ti

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    Contraindications

    1. Peptic Ulcer disease

    2. Hypersensitivity

    3. Neonates with congenital heart disease

    4. Active bleeding

    Acetaminophen

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    Acetaminophen

    Generic name acetaminophen

    Trade/Brand name Paracetamol, Tylenol,

    Panadol

    Mechanism of action

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    Mechanism of action

    Inhibition of prostaglandins by Paracetamol

    occurs ONLY IN THE CNS.

    Has no effect on prostaglandin synthesis in the

    peripheral sites.

    This may explain the absence of anti-inflammatory effects and gastric ulceration.

    Indications

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    Indications

    Relief of pain and fever

    It is preferred to NSAIDs for use in children

    suspected of having chicken pox and influenza

    Good replacement for patients with aspirin

    toxicity

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    Dosages:

    Adult and children over 12 yrs325mg to 650mg q 4 to 6 hrs.

    Pediatric patients

    0-3 months 62.5mg 4-11 months 125mg

    12-23 months 187.5mg

    2-3 years 250mg

    4-5yrs 375mg

    6-7 yrs 500mg

    Metabolism of acetaminophen

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    Acetaminophen can be metabolized in two ways;1. Major pathway:

    Acetaminophen undergoes conjugation with glucuronic acid to form nontoxic metabolites.

    At therapeutic doses, practically the entire drug is converted to nontoxic compounds via themajor pathway.

    2. Minor pathway : Acetaminophen is oxidized by P450-containing enzyme into highly reactive and toxic

    compound. Only a small fraction is converted into toxic metabolite via the minor pathway.

    Under normal conditions, the toxic metabolite undergoes rapid conversion to a nontoxicform; glutathione is required for the conversion.

    When an overdose of acetaminophen is taken, a larger than normal amount is processed viathe minor pathway; hence, a large quantity of toxic metabolite is produced.

    As the liver attempts to detoxify the metabolite, glutathione is rapidly depleted, and furtherdetoxification stops. As a result, the toxic metabolite accumulates, causing damage to the

    liver.

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    Opioids (Narcotic) Analgesics

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    Opioids (Narcotic) Analgesics

    Two classes:

    Narcotic analgesics obtained from raw opium

    Synthetic narcotic analgesics

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    Narcotic Analgesics

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    Narcotic Analgesics Terminologies

    Opiates: compounds extracted from the opium

    poppy flower

    opioids: chemical compounds that are wholly

    synthesized, but which resemble the opiates in

    their actions e.g. meperidine

    Other Examples: morphine and codeine.

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    General properties of narcotic analgesics

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    General properties of narcotic analgesics

    They have capacity to reduce pain and painperception

    Able to alter ones reaction to the pain

    They have sedative properties

    They cause profound feeling well-being

    (euphoria)

    Addictive properties (physical and

    psychological dependence)

    Examples of Narcotic Analgesics

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    (Opiates & Opioids)

    Strong opioid

    Morphine sulfate

    Pethidine Hydrocloride (meperidine)

    Fentanyl

    butorphanol,

    Levophanol

    Mild opioid

    Tramadol HCL

    Codeine phosphate101

    Prototype: Morphine sulfate

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    Prototype: Morphine sulfate

    Generic name

    Morphine sulfate

    Trade name:

    ???

    Classification:

    Opioid agonist analgesic

    Dosage and route

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    Dosage and route

    Oral 15mg PO daily, as a single dose in the evening

    IM or Subcutaneous

    5-20mg/70kg as directed by physician

    IV

    2.5-15/70kg of body weight

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    Effects of morphine

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    analgesia,

    sedation,

    euphoria,

    respiratory depression, cough suppression and

    suppression of bowel motility.

    105

    Indication

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    Severe acute pain or severe chronic pain.

    Preoperative sedation and adjunct to anesthesia

    control of pain associated with acute myocardial

    infarction

    Relieve of severe, persistent cough

    Treatment of severe diarrhea and intestinal cramping.

    106

    Contraindication

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    Hypersensitivity

    Addiction

    Hemorrhage

    Bronchial asthma

    Increased intracranial pressure

    107

    Adverse Effects

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    Read from hand out

    108

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    DRUGS USED IN THE PERIOPERATIVE

    PERIOD

    109

    Introduction

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    Introduction

    These drugs are CNS depressants.

    Classified into:

    General anesthetic agents,

    Narcotic analgesics

    Sedative-Hypnotics.

    110

    Preoperative agents: Sedative-hypnotics

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    Preoperative agents: Sedative hypnotics

    Definitions

    Anxiolytics: drugs that prevent feeling of tension or fear.

    Sedatives: provide a calming effect on patients

    Hypnotics: induces sleep.

    Sedative-hypnotic:Produces calming effect at lower doses

    and induce sleep at higher doses.

    111

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    Sedative-hypnoticsare grouped as:

    barbiturates

    benzodiazepines

    Barbiturates

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    Barbiturates

    They are powerful CNS

    depressants

    Rarely used because of:

    side effects

    risk of psychological

    and physical

    dependence.

    Mechanism of action

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    Act on the brainstem in the reticular activating

    system (RAS) by:

    inhibiting nerve cell function

    reducing nerve impulse transmission to the

    cerebral cortex.

    Raising the seizure convulsive threshold.

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    Drug

    name

    Dosage/Route Adverse effects

    Pheno

    barbita

    l

    (lumin

    al)

    Sedative: oral; 30-120mg /day

    IV/IM; 100-200mg/day

    Drowsiness, vitamin

    deficiency (vit. D;

    folate, or B12)

    Pentob

    arbital

    Sedative: oral; 20-30mg bid or qid

    Hypnotic: oral; 120-200mg;IM,

    150-200mg

    Respiratory

    depression,

    laryngospasm

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    PRINCIPLES OF DRUG

    DMINISTR TION

    OVERVIEW

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    OVERVIEW

    Drugs given for therapeutic purposes arecalled medications.

    Administering medications-an important

    nursing responsibility The basic requirements for accurate drug

    administration are often called the five

    rights and the three checks

    THE THREE CHECKS

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    THE THREE CHECKS

    The label on the medication container shouldbe checked three times during medicationpreparation.

    The label should be read: when the nurse reach for the container

    Immediately before pouring or opening themedication

    When replacing the container to the drawer orshelf

    The five rights

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    The five rights

    The right medication to the

    Right patient in the

    Right dosage through the

    Right route at the

    Right time

    LEGAL RESPONSIBILTIES

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    LEGAL RESPONSIBILTIES

    Registered Nurses are legally empowered, togive medications ordered

    When giving medications, the nurse is legally

    responsible for safe and accurate administration. She may be held liable for not giving a drug or for

    giving a wrong drug or a wrong dose.

    she is expected to have sufficient drug knowledge

    to recognize and question erroneous orders.

    LEGAL RESPONSIBILTIES

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    LEGAL RESPONSIBILTIES

    The nurse also is legally responsible for actionsdelegated to people who are inadequately

    prepared for or legally barred from

    administering medications (such as nursingassistants).

    nurses are expected to

    monitor clients responses to drug therapy. to teach clients safe and effective self-

    administration of drugs when indicated

    All substances are poisons;

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    p ;

    there is none that is not apoison. The right dosedifferentiates a poison froma remedy.

    Paracelsus, 1493-1541

    Ideal Drug

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    g

    Effectiveness

    Safety

    Selectivity

    Reversible

    Predictability

    Ease of administration

    Freedom from drug interactions

    Ideal Drug

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    g

    Low cost

    Chemical Stability

    Possession of a simple generic name

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    PHARMACOKINETICS

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    Therapeutic Objective

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    p j

    Maximum benefit with minimum harm

    The intensity of the response to a drug is

    directly related to the concentration of the

    drug at its site of action

    Intensity of Drug responses

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    y g p

    Administrationdosage and route

    Pharmacokinetics

    Pharmacodynamics

    Individual variation

    Nursing Responsibilities

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    g p

    Last line of defense against errors!!!!!!!!!

    Patient education

    Utilize the nursing process

    Drug Legislation

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    g g

    1906drugs should be free of adulterants

    1938testing for toxicity

    1962proof of effectiveness

    1970Controlled Substance ActScheduled

    drugs

    1997Food and Drug Administration

    Modernization Act

    New Drug Development

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    g p

    Preclinical testingprior to testing on humans

    Clinical testing

    Inormal volunteersexcept maybe patients

    who have disease

    II and IIIpatients

    IVreleased for general use

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    Be neither the first to adopt the new nor thelast to abandon the old!

    Drug Names

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    Chemical Generic Name

    Trade Name

    OTC drugs

    Pharmacokinetics

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    Drug movement throughout the body

    Absorptionmovement of drug from its site ofadministration into blood

    Dissolvemust dissolve before being absorbed

    Surface areathe larger the faster

    Blood flowmost rapid where blood flow is high

    Lipid solubility - the higher the faster

    pH partitioning

    Absorption - Routes

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    IVno barriers to absorption Intramusculargood for poorly soluble drugs, time

    released

    Subcutaneousagain no significant barriers Oralmust pass through cells of epithelium, enteric

    coating

    Safer but highly variable absorptionenteric,

    sustained-release, tablets

    Distribution

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    Blood flow to tissues Exiting the vascular system once it has been

    deliveredpass through pores in capillary

    wall

    Protein - binding

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    Drugs can bind with proteins Parts of drugs will be bound during any given

    time period

    Impedes drugs ability to reach sites of action,metabolism, or excretion

    Metabolism

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    LIVER Enzymatic alteration of drug structure

    Consequences of metabolism

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    Accelerated renal excretionkidney cannotexcrete highly lipid soluble

    Drug inactivation

    Increased therapeutic action

    Activation of prodrugs

    Increased or decreased toxicity

    Considerations in Metabolism

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    Age Induction of drug metabolizing enzymes

    First-pass effectNitroglycerin

    Nutritional status

    Competition between drugs

    Excretion

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    KIDNEY Glomerular filtrationblood to tubular urine

    Tubular reabsorption

    Active tubular secretionpumps for organic

    acids and organic basesto urine

    Monitoring drug levels

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    Plasma drug levels

    Therapeutic range

    Drug Half-life

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    Time requires for the amount of drug in thebody to decrease by 50%

    Will determine dosing requirements

    Goal - plateau

    Dosing

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    Loading doseswhen plateau must beachieved quickly

    Routine smaller dosesmaintenance doses

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    Peak and trough levels

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    Maximal efficacylargest effect a drug canproduce

    Potencyone that produces its effects at

    lower dosages

    Receptors

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    Drugs bind to receptors to produce effects

    Reversible

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    All that drugs can do is mimic the physiologicalactivity of the bodys own molecules

    Block the physiological activity of the bodys

    own molecules

    Agonists

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    Mimic the bodys own regulatory molecules

    Antagonists

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    Drugs that block the actions of endogenousregulators

    Partial agonists

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    Mimic the actions but with reduced intensity

    Drug Interactions

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    Can have varying effects

    Direct chemical or physicalIV preparation

    DrugFood Interactions

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    Frequently decreased rate of absorption

    Grapefruit juice can inhibit metabolism

    with food with or shortly after meal

    empty stomach one hour prior to meal or

    two hours after

    Adverse drug reactions

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    Side effect Toxicity

    Allergic reaction

    Idiosyncratic effect

    Iatrogenic disease

    Physical dependence

    Carcinogenic effect

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    Teratogenic effectinduce birth defect

    Ways to minimize

    Variation in drug responses

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    Age Body composition

    Gender

    Pathophysiology

    Tolerance Placebo effect

    Genetics

    Variability in absorptionbioavailabilityoral

    ability to reach circulation Compliance

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    What does the term adverse reaction refer to?

    A. A life-threatening response to a responseto a drug

    B. A drug-induced allergy C. A harmful, undesirable response to a drug

    D. An unpredictable response to a drug

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    What is an idiosyncratic response? A. a toxic reaction

    B. an allergic reaction

    C. a reaction peculiar to the patient

    D. an anaphylactic reaction

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    Which statement accurately characterizes geriatricpatients compliance with prescribed drug regimens?

    A. compliance decreases with age

    B. compliance increases with age

    C. compliance increases with multiple healthproblems

    D. compliance decreases when more than threedrugs are prescribed

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