© 2006 the mcgraw hill companies pharmacology. © 2006 the mcgraw hill companies introduction
TRANSCRIPT
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© 2006 The McGraw Hill Companies
Pharmacology
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© 2006 The McGraw Hill Companies
Introduction
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Introduction
• Drugs are chemical agents used in the diagnosis, treatment, and prevention of disease
What is pharmacology?
Why is it important?
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Introduction
• Written records of drug use date back to the ancient Egyptians
• Hippocrates wrote extensively about drugs
• During his time, a more scientific approach was used in treating specific diseases with drugs
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Introduction
• Subspecialties of Pharmacology
–Pharmacokinetics
–Pharmacodynamics
–Pharmacogenetics
–Pharmacogenomics
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Introduction
• Pharmacokinetics is dependent upon the body’s ability to move substances within the body– Active transport– Facilitated diffusion– Passive transport
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Pharmacology Basics
• Pharmacokinetics considerations– Molecule size and shape– Solubility in water and lipids– Ability to bind to tissue proteins– Ionization
Solubility Exercise
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Introduction
• Pharmacodynamics – Study of the
mechanisms by which specific drug dosages act to produce biochemical or physiological changes
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Introduction
• Pharmacodynamics – Drugs may act in four different ways:
• Bind to a receptor site• Change the physical properties of the cell• Chemically combine with other chemicals• Alter a normal metabolic pathway
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Introduction
• Pharmacogenetics and pharmacogenomics– Study unique genetic processes linked to
DNA coding and genetics
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Pharmacogenosy
• The study of natural drug sources– Plants– Animals– Minerals
• What are some common examples of each drug source?
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Pharmacogenosy
– Researchers can now manipulate the molecular structure of substances to create synthetic drugs
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Plant Sources of Drugs
• Oldest source of medications
• Drugs may consist of using the entire plant, leaves, roots, bulbs, stems, seeds, buds, or blossoms
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Animal Sources of Drugs
• Body fluids or glands from animals can act as sources for drugs
• Hormones• Oils and fats• Enzymes
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Mineral Sources of Drugs
• Metallic and nonmetallic minerals provide various inorganic materials
• Occur naturally or are combined to form acids, bases, or salts
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Introduction
• Laboratory-produced drug sources – New drugs may be a
more pure form of a naturally occurring drug or they may be a synthetic form
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Routes
• Routes of Administration– Enteral Route– Parenteral Route– Topical Route
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Introduction
• Subroutes of administration– Ingestion– Injection– Absorption– Inhalation
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Route of Administration
• Depends of many factors– Accessibility– Rate of absorption– Deactivation by enzymes or acids– Toxicity to tissues
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Drug Absorption
• Drug’s progress from its pharmaceutical dosage form to a biologically available substance
• Several factors affect drug absorption
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Factors
1. Solubility
2. Concentration
3. pH
4. Site of absorption
5. Blood supply
6. Bioavailability
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RouteOral (PO)
Subcutaneous (SQ)
Topical
Intramuscular (IM)
Rectal (PR)
Sublingual (SL)
Endotracheal (ET)
Inhalation
Intraosseous (IO)
Intavenous (IV)
Rate of AbsorptionSlow
Slow
Moderate
Moderate
Rapid
Rapid
Rapid
Rapid
Immediate
Immediate
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Drug Forms
• Usually consist of a powder dissolved in a liquid– Solute: drug– Solvent: liquid in which it is dissolved
• Primary difference between one preparation and another is the solvent
• What is a solution?
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Drug Forms
• Liquids
• Solids
• Suppositories
• Inhalants
• Sprays
• Creams/lotions
• Patches
• Lozenges
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Liquid Drugs
– Solutions
– Tinctures
– Suspensions
– Spirits
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Liquid Drugs
–Emulsions
–Elixirs
–Syrups
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Routes of Administration
–Enteral• Orally (PO)
–Parenteral• Intramuscular (IM)
• Subcutaneous (SC or SQ)
• Intravenous (IV)
• Inhalation
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Packaging
• Packaging and preparations – Vials
– Ampules
– Self-contained systems or syringes
– Nebules
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Solid Drugs
– Administered orally or rectally
• Pills
• Powders
• Capsules
• Tablets
• Suppositories
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Inhalants
–Nebulizers
–Metered-dose aerosols
–Turbo inhalers
–Vaporizers
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Distribution
• Several factors affect distribution:
• Cardiovascular function
• Regional blood flow
• Drug storage reservoirs
• Physiological barriers
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Biotransformation
• Biotransformation has two effects:– It can transform the drug into a more or less
active metabolite– It can make the drug more water soluble (or
less lipid-soluble) to facilitate elimination
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Biotransformation
• Can activate metabolites to make the drug active (prodrugs)
• Many processes occur in the liver– First-pass effect– Body detoxifies and disposes of
toxins and excess drug by increasing water solubility
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Basics
• Drugs are eliminated in either their original form or as metabolites– Drug excretion is the movement of a drug or
its metabolites from the tissues back into circulation and from secretion into organs of excretion
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Elimination
• Can be affected by– Drug half-life– Accumulation– Clearance– Onset, peak, and
duration
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Therapeutic Index
• Medication must reach a certain concentration at the target tissue to be effective
• Medication must reach a certain concentration at the target tissue to be effective
Therapeutic index
Therapeutic threshold
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Therapeutic Index
• Dose calculation• ED50
• LD50
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Receptors
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Receptors
• Mechanism of Action: how a drug works– Drug action
– Drug effect
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Receptors
• Drug receptors: proteins present on cell membrane to which a drug must bind in order to elicit a desired response
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Receptors
• Receptors are classified based on effects – Agonist– Antagonist
• Competitive antagonist• Noncompetitive antagonist
• A drug attached to a receptor site displays affinity
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Receptors
• Efficacy: the power of a drug to produce a therapeutic effect– Agonists have affinity and
efficacy– Antagonists have affinity but not
efficacy
• Drug potency: relative amount of drug required to produce the desired response
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Receptors
• How do drugs bind to receptor sites?– Ionic bonds– Hydrogen bonds– Hydrophobic bonds– Van der Waals forces– Covalent bonds
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Receptors
• Receptor sites– Several drugs may bind to the same receptor
site, thus creating different responses by the cells
– Two main functions• Ligand binding• Message propagation
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Neurotransmitters
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Neurotransmitters
• The nervous system is the body’s control system, regulating all bodily function via electrical impulses
• What are the two main parts of the central nervous system that drugs can affect?
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Neurotransmitters
• Two divisions:– Central Nervous System (CNS)– Peripheral Nervous System (PNS)
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Neurotransmitters
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NeurotransmittersOrgan Sympathetic stimulation Parasympathetic stimulation
Heart Increased rate, force
Decreased rate, force
Lungs Bronchodilation Bronchoconstriction
Kidneys Decreased output None
Systemic blood vessels
Constricted – dilated –
None
Liver Glucose release Glycogen synthesis
Blood glucose Increased None
Pupils Dilated Constricted
Basal metabolism Increased up to 100%
None
Skeletal muscle Increased strength None
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Neurotransmitters
• Nerves of the autonomic nervous system exit the CNS and enter autonomic ganglia
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Neurotransmitters
• No connection exists between two nerve cells or a nerve cell and its target organ; instead there is a space called a synapse
• Neurotransmitters are specialized chemicals that conduct impulses between nerve cells or between a nerve cell and an organ
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Neurotransmitters
• Neurotransmitters of ANS:– Acetylcholine (Ach)– Norepinephrine (NE)
• Synapses:– Cholinergic synapses: use acetylcholine– Adrenergic synapses: use norepinephrine
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Neurotransmitters
• What is the action of an adrenergic drugs?
• What is the action of a cholinergic drug?
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Neurotransmitters
• Sympathetic Nervous System– Arises from the thoracic and lumbar
regions of the spinal cord– Results in direct stimulation of adrenal
medulla and release of norepinephrine (noradrenaline) and epinephrine (adrenaline)
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Neurotransmitters
• Sympathetic Nervous System– Stimulation ultimately results in release of
norepinephrine from postganglionic nerves– Sympathetic stimulation also results in
release of epinephrine and norepinephrine from the adrenal medulla
– What is/are the chemical mediators of the SNS?
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Neurotransmitters
• Types of sympathetic receptors– What is the action of adrenergic receptors?
• Alpha1 (1)
• Alpha2 (2)
• Beta1 (1)
• Beta2 (2)
– Of dopaminergic receptors?
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NeurotransmittersReceptor Actions
alpha1 (1) Peripheral vasoconstriction, increased contractile force, decreased rate
alpha2 (2) Peripheral vasoconstriction
beta1 (1) Increased heart rate, contractile force and automaticity
beta2 (2) Peripheral vasodilation, bronchodilation, uterine smooth muscle relaxation
dopaminergic Renal vasodilation and mesenteric vasodilation
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Neurotransmitters
• Sympathomimetics: medications that stimulate the sympathetic nervous system
• Sympatholytics: medications that inhibit the sympathetic nervous system
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Neurotransmitters
• The Parasympathetic Nervous System– Arises from the brain stem and sacral
segments of the spinal cord– Synapse in parasympathetic ganglia
– What is/are the chemical mediators of the PNS?
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Neurotransmitters
• Stimulation of the parasympathetic nervous system results in:– Pupillary constriction
– Secretion by digestive glands
– Increased smooth muscle activity along GI tract
– Bronchoconstriction
– Reduction in heart rate and contractile force
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Neurotransmitters
• Parasympatholytics: medications that block the actions of the parasympathetic nervous system
• Parasympathomimetics: medications that stimulate the parasympathetic nervous system
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Homeostasis and Balance
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Homeostasis and Balance
• Our bodies require constant regulation in order to maintain balance and control
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Drug Names and
References
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Drug Names and References
• Drug Classification– Prescription (Rx)
– Over-the-counter (OTC)• Herbal
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Drug Names and References
• Drug Names– Official: generally same as generic name
• meperidine hydrochloride, USP
– Chemical: anatomic and molecular structure• Ethyl 1-methyl-4-phenylisonipecotate
hydrochloride
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Drug Names and References
• Drug Names– Generic: abbreviated version of chemical
name• meperidine hydrochloride
– Trade: name based on chemical name or problem used to treat
• Demerol hydrochloride• What is another term for a drug’s trade name?
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Sources of Drug Information
• Using multiple sources may provide the best information
• United States Pharmacopia (USP)• National Formulary (NF)• American Hospital Formulary Service• Physician’s Desk Reference (PDR)• Packaging inserts, as required by law
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Drug Names and References
• A process must be approved by the FDA
• Studies take place in four phases– Preclinical testing, research, and development– Clinical research and development– NDA Review– Postmarketing surveillance
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Drug Names and References
• Bringing a drug to market is a process that takes several years and must be approved by the U.S. Food and Drug Administration (FDA)
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Drug Names and References
• Studies take place in four phases– Preclinical testing, research and development– Clinical research and development– NDA Review– Postmarketing surveillance
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Drug Names and References
• New Drug Development
–Phase I
–Phase II
–Phase III
–Phase IV
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Drug Names and References
• New Drug Development – Orphan Drugs
• Drugs not developed or adopted
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Unlabeled Uses of Drugs
• FDA only accepts a new drug for the indications in which phase II and III clinical studies have shown it to be effective.
• Indications approved (labeled)• Not approved (unlabeled)
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Drug Names and References
• Unlabeled uses of drugs– FDA recognizes that a drug’s labeling does
not always contain the most current information on usage
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© 2006 The McGraw Hill Companies
Patient Medication Rights
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Patient Medication Rights
• What are the six “rights” of patient medication administration that ensure safe, proper, and effective administration?
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Patient Medication Rights
1. Right patient
2. Right medication
3. Right dose
4. Right route
5. Right time
6. Right documentation
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© 2006 The McGraw Hill Companies
Classifying Medications
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AHA Classes of Recommendations for Drug Therapies
• Class I
Benefit >>> Risk
– Procedure/treatment or diagnostic test/assessment should be performed/administered
Table 15-7
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AHA Classes of Recommendations for Drug Therapies
• Class IIaBenefit >>RiskIt is reasonable to perform procedure/administer treatment or perform diagnostic test/assessment.
Table 15-7
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AHA Classes of Recommendations for Drug Therapies
• Class IIbBenefit RiskProcedure/treatment or diagnostic test/assessment may be considered.
Table 15-7
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AHA Classes of Recommendations for Drug Therapies
• Class IIIRisk Benefit Procedure/treatment or diagnostic test/assessment should not be performed/administered. It is not helpful and may be harmful.
Table 15-7
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AHA Classes of Recommendations for Drug Therapies
• Class Indeterminate– Research is just getting started– Continuing area of research– No recommendation until further research
(e.g., cannot recommend for or against)
Table 15-7
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Classifying Medications
• Classified with other similar medications with the same effects– Body system/disease used to treat– Chemical group– Receptor binding site
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© 2006 The McGraw Hill Companies
What Paramedics Need to Know About Drugs
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What Paramedics Need to Know About Drugs
• Comprehensive drug list based on protocol– Be familiar with AHA Guidelines for
treating cardiac patients– Know local protocol and drugs used in
your region
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Need to Know
• Components of a drug
profile
– Names
– Classification
– Mechanism of action
– Indications
– Pharmacokinetics
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What Paramedics Need to Know About Drugs
• Components of a drug profile– Side effects/adverse reactions
– Contraindications
– Dosage
– How supplied
– Special considerations
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Need to Know
• Special considerations in drug therapy– Pediatric patients– Geriatric patients– Pregnant and lactating
patients
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Need to Know
• Use care administering medications
• Follow the medication order
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What Paramedics Need to Know About Drugs
• Preparation involves selecting the appropriate sized needle and syringe
• No compensation for dead space is necessary when drawing up medications
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What Paramedics Need to Know About Drugs
• Use different needles when reconstituting medication to be drawn up
• Use caution when mixing drugs in one syringe
• ALWAYS use sterile technique
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Need to Know
• Medical control– As a paramedic, you operate under the
licensure of a medical director who is responsible for all of your actions
– The medical director determines which drugs you will administer and the routes by which they are given
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Need to Know
• Reduce the potential for contamination
• Identify allergies prior to contacting hospital
• Obtain vital signs
• Obtain and confirm/repeat order
• Write the order and the time
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Need to Know
• Select the proper medication
• Inspect the medication
• Confirm the order and medication
• Six rights of administration
• Record drug, dose, volume, route, and time, and obtain vital signs and effects
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What Paramedics Need to Know About Drugs
• Storage and handling considerations– USP28-NF23, PF30 (6), p. 2118
• “Storage of Drugs in Emergency Medical Services (EMS) Vehicles”
• Narcotics and controlled substances should be secured according to local protocols
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What Paramedics Need to Know About Drugs
• Legal regulations, standards, and legislation– International controls
• United Nations World Health Organization provides technical assistance and encourages new research for drug use
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Need to Know
• Legal regulations, standards, and legislation– Controls in the U.S.
• Testing (animals studies and clinical patient trials)
• Legislative control
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Need to Know
• Legal regulations, standards, and legislation– “Truth in labeling”
• Why might “truth in labeling” be important?
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Need to Know
• Legal regulations, standards, and legislation– Narcotics
• Harrison Narcotic Act, 1914• Comprehensive Drug Abuse Prevention and Control
Act, 1970
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Schedule of Controlled DrugsCategory Examples
Schedule INo recognized medical use;
high abuse potential
Opiates (heroin), hallucinogens (LSD), depressants (methaqualone)
Schedule IIWritten prescriptions required;
no telephone renewals
Opiates (codeine, morphine, meperidine), stimulants (amphetamines), depressants
Schedule IIIPrescriptions rewritten after six months or five refills
Opiates (codeine <1.8 g/dl), stimulants, depressants, anabolic steroids
Schedule IVPrescriptions rewritten after six months or five refills
Opiates (propoxyphene), stimulants, depressants (chloral hydrate)
Schedule VAny nonnarcotic medication, OTC
Small amounts of opiates when uses as antitussives or antidiarrheals
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Need to Know
• Legal regulations, standards, and legislation– Controlled Substances Act, 1970
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Need to Know
• Legal regulations, standards, and legislation– Canadian drug legislation
• Under direct control of Department of National Health and Welfare
• Food and Drug Act, 1941• Canadian Food and Drugs Act, 1953
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Need to Know
• Legal regulations, standards, and legislation– Canadian Narcotic Control Act and Regulations
• Canadian Narcotic Control Act, 1965– Restricts sale, possession, and use of narcotics– Restricts narcotic distribution to authorized personnel
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Need to Know
• Legal regulations, standards, and legislation– Drug Standards
• United States Pharmacopeia (USP) is official standard to maintain uniformity
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Need to Know
• Important pharmacological terminology
– What is antagonism?
– What is cumulative action?
– What is potentiation?
– What is synergism?
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Need to Know
• Important pharmacological terminology
– Contraindications
– Hypersensitivity
– Idiosyncrasy
– Side effects
– Untoward effects
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Need to Know
• Important pharmacological terminology
– Bolus
– Indication
– Therapeutic action
– Tolerance
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Need to Know
• Important pharmacological terminology
– Depressant
– Habituation
– Refractory
– Stimulant
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© 2006 The McGraw Hill Companies
Pre- and Postmedication Administration
Procedures
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Pre- and Postmedication Administration Procedures
• Premedication procedures– Obtain a complete SAMPLE history– Obtain a full set of vital signs– Complete a detailed exam– Contact medical control for authorization
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Pre- and Postmedication Administration Procedures
• Postmedication procedures– Document– Obtain a full set of vital signs– Complete a detailed exam– Ongoing assessment
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Summary
• In order to deliver exceptional patient care, the paramedic must have a basic understanding of the responsibilities and scope of management prior to administration of any drug
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© 2006 The McGraw Hill Companies
Classifications
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Street Secret
• Most drugs within the same class have the same suffix; this name generally only applies to the generic name– Beta blockers: –olol– Antihyperlipidemics: –statin– ACE inhibitors: –pril– Calcium channel blocker: –ipines– Opiods: –ine, –one
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Street Secret
• Shortcut for remembering what types of doses cardiac drugs have (works for all ACLS drugs)– If the drug begins with a consonant, it is a
two-part dose for normal administration:• Lidocaine—mg/kg• Cardizem—mg/kg• Procainamide—mg/min
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Street Secret
• Shortcut for remembering what types of doses cardiac drugs have (works for all ACLS drugs)– If the drug begins with a vowel, it is a one-part
dose:• Epinephrine—mg• Adenosine—mg• Atropine—mg
– Note: This does not work for drips
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Street Secret
• A key to remembering the doses on ACLS drugs is as easy as taking a pulse– The dose for a patient with a pulse is half that
of a patient without a pulse
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• Antiarrhythmics• Adenosine
• Amiodarone
• Lidocaine
• Procainamide
ACLS Medications
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• Catecholamine-sympathomimetic
• Epinephrine 1:10,000
• Isoproterenol
ACLS Medications
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• Inotrope• Digoxin
• Epinephrine 1:10,000
ACLS Medications
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• Vasopressors• Dopamine
• Dobutamine
• Epinephrine 1:1 000
• Norepinephrine
• Vasopressin
ACLS Medications
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• Calcium channel blockers
• Diltiazem
• Verapamil
ACLS Medications
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• Parasympatholytics• Atropine
ACLS Medications
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• Mineral/electrolyte• Calcium chloride
• Magnesium sulfate
• Sodium bicarbonate
ACLS Medications
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• Endocrine/metabolic enhancing agent
• Vasopressin
ACLS Medications
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Classifying Medications
• Analgesics–Nonsteroidal anti-inflammatory
agents (NSAID)• Ibuprofen
• Ketorolac
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Classifying Medications
• Analgesics–Narcotics
• Butorphanol
• Fentanyl
• Meperdine
• Morphine sulfate
• Nalbuphine
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Classifying Medications
• Analgesics–Other analgesics
• Acetaminophen
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Classifying Medications
• Anaphylaxis–Antianaphylactic agents
• Epinephrine 1:1 000
• Diphenhydramine
• Hydroxyzine
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Classifying Medications
• Anesthetics– Topical anesthetics
• Benzocaine• Cetacaine• Lidocaine topical gel• Procaine• Proparacaine• Tetracaine
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Classifying Medications
• Anesthetics–Local anesthetics
• Procaine
• Proparacaine
• Tetracaine
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Classifying Medications
• Anesthetics–Inhaled agents
• Nitrous oxide
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Classifying Medications
• Antianginal agents–Nitroglycerine
–Nitroprusside
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Classifying Medications
• Anticoagulants– Heparin– Warfarin sodium
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Classifying Medications
• Anticonvulsants–Anticonvulsants
• Fosphenytoin
• Phenobarbital
• Phenytoin
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Classifying Medications
• Anticonvulsants–Benzodiazepine
• Diazepam
• Lorazepam
• Midazolam
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Classifying Medications
• Antiemetics–Droperidol
–Prochlorperazine
–Promethazine–Hydroxyzine
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Classifying Medications
• Antihypertensives–Antihypertensive
• Clonidine
• Diazoxide
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Classifying Medications
• Antihypertensives–ACE Inhibitor (acetylcholinesterase)
• Enalapril
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Classifying Medications
• Antihypertensives–Calcium channel blocker
• Nifedipine
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Classifying Medications
• Antihypertensives–Vasodilator
• Nitroprusside
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Classifying Medications
• Antihypoglycemics–Dextrose
–Glucagon
–Insulin
–Oral glucose paste
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Classifying Medications
• Antiplatelet agents–Acetylsalicylic
acid (ASA) or aspirin
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Classifying Medications
• Antitoxicologics–Anticholinergic
• Atropine
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Classifying Medications
• Antitoxicologics–Antidote
• Cyanide antidote kit
• Methylene blue
• Physostigmine
• Pralidoxime auto injector
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Classifying Medications
• Beta blockers–Esmolol
–Labetalol
–Metoprolol
–Propranolol
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Classifying Medications
• Diuretics–Diuretic
• Mannitol
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Classifying Medications
• Diuretics–Loop diuretics
• Bumetanide
• Furosemide
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Classifying Medications
• Fibrinolytics– Alteplase
– Antithrombin III
– Heparin
– Reteplase
– Tenectplase
– Urokinase
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Classifying Medications
• Gastric decontaminants– Toxicological agents
• Activated charcoal• Ipecac
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Classifying Medications
• Induction agents–Analgesic
• Ketamine
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Classifying Medications
• Induction agents–Barbiturate
• Methohexital
• Thiopental
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Classifying Medications
• Induction agents–Benzodiazepine
• Midazolam
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Classifying Medications
• Induction agents–Hypnotic
• Etomidate
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Classifying Medications
• Induction agents–Opiate
• Fentanyl
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Classifying Medications
• Narcotic and benzodiazepine antagonists–Flumazenil
–Naloxone
–Nalmefene
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Classifying Medications
• Nasal decongestants– Oxymetazoline
nasal – Phenylephrine
nasal
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Classifying Medications
• Neuroleptics–Antipsychotics
• Chlorpromazine
• Haloperidol
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Classifying Medications
• Neuroleptics–Antiemetic
• Droperidol
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Classifying Medications
• Paralytics– Neuromuscular blocking agents (NMBA)
• Depolarizing– Succinylcholine
• Nondepolarizing– Mivacurium– Pancuronium– Vecuronium
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Classifying Medications
• Postpartum agents–Oxytocin
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Classifying Medications
• Respiratory agents–Bronchodilators
• Sympathomimetic (adrenergic)– Beta2 selective
» Albuterol» Isoetharine» Terbutaline
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Classifying Medications
• Respiratory agents–Bronchodilators
• Sympathomimetic (adrenergic)– Nonselective
» Epinephrine » Epinephrine (inhaled)» EpiPen Autoinjector/EpiPen Jr» Metaproterenol» Racemic epinephrine
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Classifying Medications
• Respiratory agents–Bronchodilators
• Combination agents– Albuterol/ipratoprium
combination
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Classifying Medications
• Respiratory agents–Bronchodilators
• Methylxanthine (xanthine) derivative– Aminophylline
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Classifying Medications
• Respiratory agents– Bronchodilators
• Parasympatholytic (anticholinergic)
– Ipratoprium
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Classifying Medications
• Steroids–Dexamethasone
–Hydrocortisone
–Prednisone
–Methylprednisolone sodium succinate
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Classifying Medications
• Tocolytics–Magnesium sulfate
–Terbutaline
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Classifying Medications
• Vasopressors–Adrenergics
–Sympathomimetics
–Catecholamines
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Classifying Medications
• Vitamins and electrolytes– Calcium chloride
– Calcium gluconate
– Magnesium sulfate
– Potassium chloride
– Sodium bicarbonate
– Thiamine