1	Introduction to Pharmacology Mark Branon, BS, NREMT-P
2	Objectives After completing this chapter, the student should be able to: List four drug sources and give examples of each source Define the terms pharmacology, pharmacologists, and pharmacognosy Identify drugs by their chemical name, generic name, trade name, and official name List four sources of drug information and demonstrate how to find a medication in one of these references List several examples of both liquid and solid drugs
3	Legislative acts controlling drug use and abuse in the United States Purpose is to protect the public and patients Pure Food & Drug Act of 1906 – improved quality and labeling of drugs. Created the USP. Harrison Narcotic Act of 1914 – regulated the manufacture, sale, and use of opium, cocaine, and their derivatives Federal Food, Drug, & Cosmetic Act of 1938 gave the FDA its regulatory power
4	Legislative acts controlling drug use and abuse in the United States Durham-Humphrey Amendments of 1951 differentiated between prescription and OTC drugs Comprehensive Drug Abuse Prevention & Control Act (Controlled Substances Act) of 1970 in effect replaced the Harrison Narcotic Act and created the five “schedules” of controlled substances
5	Introduction Historical consideration Harrison Narcotic Act Pure Food and Drug Act Federal Food, Drug, and Cosmetic Act Drug Sources Plant sources of drugs Animal sources of drugs Mineral sources of drugs Laboratory sources of drugs
6	Drug Sources
7	Sources of Drug Information
8	Drug Research and Bringing a Drug to Market The pharmaceutical industry is highly motivated to bring profitable new drugs to market. Proving safety and reliability of these new drugs requires extensive research. Drugs can become “generic” when original company’s patent expires.
9	New Drug Development Timeline
10	How drugs are classified By body system affected cardiovascular Mechanism of action vasopressor Class of agent Benzodiazapine Indications anti-infective
11	Common Pharmacological Abbreviations
12	Common Abbreviations
13	Common Abbreviations (cont.)
14	FDA Classification of Newly Approved Drugs Numerical classification (chemical) Letter classification (treatment or therapeutic potential) Other classifications
15	New Drug Development Phase I: Determine pharmacokinetics and toxicity Phase II: Determine therapeutic drug level Phase III: Refine usual dose and study side effects Phase IV: Post-market analysis Expedited drug approval Orphan drugs
16	Black Box Warning FDA requires manufacturer to prominently display warning in “black box.” This can minimize risks by assuring practitioners are familiar with side effects.
17	Unlabeled Uses of Drugs
18	Medical Oversight The Medical Director Medical control Direct (on-line) medical control Indirect (off-line) medical control Medical control protocols and guidelines
19	Medical Oversight (cont.) Legal regulations, standards, and legislation International controls Controls in the United States Narcotics The Controlled Substances Act
20	Schedule of Controlled Drugs
21	Schedule I Very high abuse potential May lead to severe dependence No currently accepted medical use For research, analysis, or instruction Examples Heroin LSD Mescaline
22	Schedule II High abuse potential Has accepted medical uses May lead to severe physical and/or psychological dependence Examples Opium Morphine Codeine Oxycodone Cocaine Secobarbital
23	Schedule III Less abuse potential than Schedule II Accepted medical uses May lead to moderate/low physical dependence or high psychological dependence Examples are preparations with limited opiods such as Tylenol or ASA with codeine
24	Schedule IV Lower abuse potential than Schedule III Accepted medical uses May lead to limited physical or psychological dependence Examples Phenobarbital Diazepam Lorazepam
25	Schedule V Lowest abuse potential Accepted medical uses May lead to limited physical or psychological dependence Examples are medications for cough or diarrhea with limited quantities of opoids such as Lomotil
26	Drug Names Chemical names Generic names Trade names Official names
27	Drug Names (cont.) Chemical name A precise description of a drug’s chemical composition and molecular structure. ethyl 1-methyl-4phenylisonipectorate hydrochloride
28	Drug Names (cont.) Generic name A markedly abbreviated form of the chemical name of the drug. Generic medications usually have the same therapeutic efficacy as the nongeneric and are generally less expensive. meperidine hydrochloride
29	Drug Names (cont.) Trade name A copyrighted name designated by the drug company that sells the medication. Trade names are proper nouns. The first letter is capitalized. Demerol^® hydrochloride
30	Drug Names (cont.) Official name Followed by the initials USP or NF, denoting a listing in one of the official publications. Usually the same as the generic name. meperidine hydrochloride, USP
31	Components of a Drug Profile Names (generic and trade) Classification Mechanism of action Indications Pharmacokinetics Side effects/adverse reactions Contraindications Dosage How supplied Special considerations
32	Drug Forms Liquid forms Solid drugs Suppositories Inhalants
33	Drug Forms (cont.) Liquid forms Solutions Tinctures Suspensions Spirits Emulsions Elixirs Syrups
34	Drug Forms (cont.) Solid drugs Pills Powders Capsules Tablets
35	Drug Forms (cont.) Suppositories
36	Drug Forms (cont.) Inhalers Metered-dose Small-volume nebulizer
37	Ampules
38	Prefilled Syringes
39	Tubex Syringes Often used for controlled substances Require Tubex adaptor
40	Multidose Vials Dosage and volume vary by drug and manufacturer Often less expensive than other preparations
41	Single-Dose Vials Common in emergency medicine Usually contain standard dose (but can vary by manufacturer)
42	Mechanism of Action The way in which a drug causes its effects Pharmacodynamics
43	Pharmaceutical Phase of Drug Activity During this phase the drug dissolves so it can be made available for absorption Drugs given by the intravenous, transtracheal, and intraosseous routes bypass the pharmaceutical phase of drug activity.
44	Pharmacokinetic Phase of Drug Activity Pharmacokinetics is the study of the processes that determine the duration and intensity of a drug’s effect. Absorption Distribution Biotransformation Elimination
45	Types of Transport Active transport – requires energy to move or cause action Facilitated diffusion – requires “help” but no real energy Passive transport – requires no energy Diffusion – movement of a solute from an area of higher concentration to an area of lower concentration Osmosis – movement of solvent from an area of lower solute concentration to and area of higher solute concentration
46	Absorption Absorption is the process by which a drug gets into the blood stream. IV drugs don’t require this step since they are introduced directly into the bloodstream Shock and hypothermia will slow absorption while fever and hyperthermia will increase it
47	Bioavailability The amount of a drug that is still available when it reaches its target tissue The drug must have survived the absorption process and have maintained its integrity long enough to be effective Examples: insulin can’t survive GI absorption and adenosine has a very short half-life
48	Distribution Once absorbed, the drug must be distributed throughout the body The blood-brain barrier prevents drugs except those that are non-protein bound and highly lipid soluble from making it to the brain The placental barrier restricts movement to the baby from the mother as well
49	Biotransformation Simply means the metabolism of a drug Some “prodrugs” aren’t active when administered and absorbed, but are active only after metabolism by the body.
50	Elimination Most drugs are eliminated from the body in urine Some are also excreted in feces or in exhaled air
51	Pharmacodynamic Phase of Drug Activity Binding to a receptor site Changing the physical properties of the cells Chemical combining with other chemicals Altering a normal metabolic pathway
52	Receptor Sites A receptor site is a specialized protein that combines with a drug resulting in a biochemical effect Affinity is the force of attraction between a drug and a receptor Efficacy is a drug’s ability to cause the expected response.
53	Types of Regulation Down regulation – binding a drug to receptors and decreasing the number of available receptors Up regulation – a drug causes the formation of more receptors
54	Agonist/Antagonist An agonist is a drug that binds to a receptor and causes it to initiate the expected response (causes action) An antagonist is a drug that binds to a drug but does not cause it to initiate the expected response (prevents action) Agonist-antagonists are drugs that bind to a receptor and stimulates some of its effects while blocking others
55	Types of Antagonism Competitive antagonism – one drug binds to a receptor and causes the expected effect while also blocking another drug from triggering the same receptor Noncompetitive antagonism – the binding of an antagonist causes a deformity of the binding site that prevents an agonist from fitting and binding Irreversible antagonism – a competitive antagonist permanently binds with a receptor site
56	Terminology
57	Capsule a special container might have gelatin, sized for single dose of the drug
58	Suppositories a semisolid substance for introduction into the rectum, vagina, or urethra, where it dissolves.
59	Pills medicine in the form of a tiny solid mass or pellet to be swallowed or chewed.
60	Spirits any distilled or volatile liquid.
61	Lozenge a small, dry, medicinal solid to be held in mouth until it dissolves.
62	Ampule a small glass container that can be sealed and its contents sterilized
63	Vial A small glass bottle for medicine or chemicals.
64	Powder an aggregation of fine particles of one or more substances that may be passed through fine meshes.
65	Tincture an alcoholic extract of vegetable or animal substances
66	Ointment a soft, medicated, fatty substance for external application to the body, having antiseptic, cosmetic, or healing properties.
67	Tablet a small, disk like mass of medicinal powder.
68	Suspension the state of a solid when it’s particles were mixed with, but not dissolved in, a fluid or another solid
69	Solution a liquid containing a dissolve substance.
70	Depression the decrease of a function such as respiration
71	Physiological concerning body function.
72	Therapeutic having medicinal or healing properties.
73	Untoward effect a side effect that proves harmful to the patient
74	Initiation the start of chemical or enzymatic reaction
75	Antagonism mutual opposition or contrary action, as between muscle or medicines.
76	Idiosyncrasy an unusual response to a drug.
77	Indication a sign or circumstance that indicates the proper treatment of the disease.
78	Side effect an action or effect of a drug other than that desired.
79	Cumulative effect an increasing in effect by successive additions; the total is usually greater than the sum of all the additions. Cumulative drug action: the action of small but repeated doses of drugs that are not immediately eliminated from the body.
80	Tolerance capacity for enduring a large amount of the substance without an adverse effect and showing a decreased sensitivity to subsequent doses of the same substance.
81	Synergism the harmonious action of two agents; such as drugs or organs, producing an effect that neither could produce alone or one that is greater than the total effects of each agent operating itself.
82	Potentiation the synergistic action of two substances in which the total effects are greater than the sum of the independent effects of the two substances.
83	Additive in pharmacology, the effect that one drug or substance contributes to the action of another drug or substance.
84	Habituation the act of becoming accustomed to anything from frequent use or exposure. In drug addiction, the mental equivalent of physical tolerance and dependence on drugs.
85	Hypersensitivity an abnormal sensitivity to a stimulus of any kind.
86	Contraindication any symptom or circumstance indicating the appropriateness of an otherwise advisable treatment.
87	Dose the amount of medicine or radiation to be administered at one time.
88	Dilution The process of attenuating or weakening of substance. A diluted substance.
89	Action performance of a function or process
90	Antidote a substance that neutralizes poisons or other effects.
91	Indications and use conditions in which a particular medication is utilized
92	Precautions conditions in which a drug may be used, but should be done so cautiously due to potential complications
93	Incompatibility the condition of not being in harmony with one’s surroundings or associates
94	Drug any substance that, when taken into a living organism, may modify one or more of its functions.
95	Therapeutics that branch of medicine concerned with the application of remedies and the treatment of disease.
96	Toxicology division of medical and biological science concerned with toxic substances, detecting them, studying their chemistry and pharmacological actions, and establishing antidotes and treatment of toxic manifestations, prevention of poisoning, and other methods for controlling exposure to harmful substances.
97	Antiarrhythmic The drug or physical force that acts to control or prevent cardiac arrhythmias
98	Vagolytic agent an agent, surgical or chemical, that prevents function of the vagus nerve.
99	Chronotropic agent influencing influencing the right of occurrence of an event, such as the heartbeat.
100	Dromotropic agent affecting the connectivity of nerve or muscle fibers.
101	Inotropic agent influencing the force of muscular contractility.
102	Analgesic a drug that relieves pain.
103	Alkalizing agent an agent that makes a substance alkaline, as through the addition of a base.
104	Antiemetic an agent that prevents or relieves nausea and vomiting.
105	Antihypertensive agent an agent that prevents or controls high blood pressure.
106	Antidiuretic agent a drug that decreases urine secretion.
107	Antitussive agent an agent that prevents or relieves coughing.
108	Antispasmodic agent an agent that prevents or relieves spasm.
109	Tranquilizer a drug that acts to reduce metal tension and anxiety without interfering with normal mental activity.
110	Orphan Drug A useful drug that does not ever reach the market for various reasons. Money is the most common reason a drug is orphaned.
111	Double Blind Study Medical study in which half of the test group receives a medication and the other half a placebo. This removes bias because neither the patient, nor the physician knows who has received the drug until the end of the study.
112	Placebo A medically inert substance
113	Pharmacology Affects On Pregnancy, Pediatrics, and the Aged
114	Medications and Pregnancy All women of childbearing age must be considered pregnant unless they or a pregnancy test indicate otherwise. Treating a pregnant patient is actually treating two patients, both must be considered. Benefits to the mother of a drug must be considered and clearly outweigh the dangers to the fetus.
115	Two pharmacological problems in pregnancy Changes in the mother’s anatomy and physiology Can affect onset and duration of action of many medications Potential for drugs to harm the fetus In the first trimester, some drugs may deform, injure, or kill the fetus. These are called teratogenic drugs. In the last trimester, drugs may pass through the placenta to affect the fetus Drugs given to the breastfeeding mother may also cross over to the baby and cause harm
116	FDA Pregnancy Categories
117	Pediatric Pharmacology Considerations Children are not simply “small adults” Absorption of oral medications is less than in adults Newborn’s skin is thinner and more permeable to topical medications Up to one year old, diminished plasma protein concentration leads to higher free drug availability Water distribution in the newborn (more extracellular fluid) may require higher doses Body surface area and weight are commonly used to dose pediatric medications (Broselow tape)
118	Geriatric Pharmacology Geriatric here is defined as over 60 (sorry Chuck) Absorption of oral medication is slower due to decreased gastrointestinal motility Polypharmacy
119	Questions ????