Pharmacology

Pharmacology z z z z the branch of science that deals with the action of drugs on the biological systems Specifically those that are used in medicine for diagnostic and therapeutic purposes Used to achieve definite outcomes that improve quality of life Various drugs and other substances are being used widely for performance enhancement or mood alteration What is a drug? z Chemical agent used in prevention, treatment, & diagnosis of disease z Ancient practice dating back to the Egyptians z Many are derived from natural sources z Drugs which have, in the past, come from nature are now produced synthetically Administration of Drugs Must first enter the system and reach receptor tissue to be effective Internal administration z z z z z Inhalation (medication through respiratory tract) Intradermal (into the skin) Intramuscular (medication directly into muscle) Intranasal Intrathecal (medication injected into the spine) z z z z Oral (most common form) Rectal (limited due to dosage regulation) Sublingual/buccal (dissolvable agents placed under tongue Intravaginal (placing drug device inside vagina) Administration of Drugs Must first enter the system and reach receptor tissue to be effective External administration z Inunctions (oil based medication rubbed into skin) z Plasters (thick ointment, counterirritant for pain & inflammation relief, increasing circulation) z Ointments (long lasting topical medication z Transdermal patches (patch with slow release mechanism) z Pastes (ointments with nonfat base z Solutions administered externally) Pharmacokinetics z Method by which drugs are absorbed, distributed, metabolized and eliminated from the body z Pharmacodynamics is the actions or effects of drugs on the body Absorption of Drugs z Rate and extent determined by chemical characteristics of drug, dosage, and gastric emptying z Drug must dissolve before absorption. Bioavailability z How completely a drug is absorbed by the system is dependent on characteristics not dosage z Absorption rate dependent on dosage form Distribution z Once absorbed, drug is transported through blood to target tissue z Volume of distribution: volume of fluid/plasma in which drug is dissolved and indicates extent of distribution of that drug z Efficacy: capability of producing therapeutic effect z Potency: dose of the drug required to produce a desired therapeutic effect Metabolism z Biotransformation of drug to water soluble compounds that can be excreted z Most takes place in liver, rest in blood and kidneys z Liver detoxifies active agents z Metabolites may be active or could be toxic. Excretion z Excretion of drug or its metabolites is controlled by kidneys z Filtered through kidneys and usually excreted in the urine (some is reabsorbed) z May also be excreted in saliva, sweat and feces Drug Half-Life z The amount of time required for the plasma drug level to be reduced by one half measured in minutes, hours, or days depending on the drug z Drug steady state z The amount taken is equal to the amount excreted z Drugs with long half-lives may take days or weeks to reach steady state Effects of Physical Activity on Pharmokinetics Exercise influences the amount of a drug that reaches the receptor site z Exercise decreases the absorption after oral administration z Exercise increases absorption after intramuscular or subcutaneous administration due to the increased rate of blood flow Legal Concerns in Administering Versus Dispensing Drugs Administering is defined as a single dose of medication to be used by a patient z Dispensing constitutes providing a sufficient quantity to be used for multiple doses z z z By law, only licensed persons may prescribe or dispense prescription drugs for an athlete ATC’s are not allowed to dispense medication unless allowed by state licensure Administering Over the Counter Drugs ATC may be allowed to administer a single dose of nonprescription medication Rules relative to Secondary School z Oral medications vs. wound medication z z Rules relative to College and Professional Athletes ATC must still use reasonable care and be prudent about types of medication provided In all cases, actions should be performed under the supervision of a physician Record keeping Establish Protocols that Address the legal And safety Issues of your Athletes Log should Contain method Of administration And dose of Medication given Obtain legal counsel Work with Board Of Pharmacy, SHC Physicians, to Avoid law Violations. Be aware of Laws Concerning prescribing Ordering, Storage Distribution, and Dispensing. Must maintain Adequate and Up to date Medical Information Record Keeping ATC’s must maintain accurate and up to date medical records for each Athlete/Patient Name z Complaint z Current medications z Any known drug allergies z Name of medication z Lot number z Expiration Date z Quantity given z Method of administration z Date and time of administration z Federally Mandated Labeling Requirements z z z z Name of product Name and address of manufacturer, packer or distributor Net contents of package Name of active ingredients and quantity of certain other ingredients z z z z Name of any habit forming drug contained Cautions and warnings to protect consumer Adequate directions for safe, effective use Expiration date and lot number Legal Considerations z All drugs dispensed from the athletic training room must be properly labeled according to Federally mandated criteria z ATC will have legal liability if drugs removed from original packaging and dispensed. Drug Safety Safety in Use of Pharmaceuticals 1. 2. 3. No drug is completely safe and harmless. Any drug can be potent and dangerous, with every individual reacting differently. Athletes must be instructed on specific information regarding their medications (i.e. Frequency, with or without food,) Individual Responses ATC must know their athlete’s in order to avoid potential adverse reactions z z z z z Individuals react differently to the same medications. different conditions cause altered effects of drugs. Drugs can change with improper storage or relative to how they are administered. Alcohol ingestion with medications should be avoided. Some medications can cause fluid depletion, further complicating illness, or make individuals sensitive to sunlight increasing risk of sunburn and allergic reactions z z z z Alcohol is a CNS depressant and can increase or decrease effects of other drugs. Alcohol is used in many liquid preparations. Medication can potentially effect certain physiologic functions related to dehydration (sweating, urination, and the ability to control and regulate body temperature. Different diets may impact absorption rate Medications for the Athletic Training Area Proper Storage Buying Medication Pharmacist is a vital resource. z z z assisting in selection of nonprescription drugs. suggesting less expensive generic drugs acting as a general advisor. Proper storage of medication is critical. z z z It must be kept in a locked cabinet. maintained in the original container. stored away from direct light, heat, damp places and extreme cold. Athletes Traveling with Medications z z z z z z Medication should not be stored in a bag/luggage but carried by the athlete taking it Sufficient supply should be packaged in case of emergency Make sure there is a source of medication while traveling Take copies of written prescriptions Keep medication in original container If traveling internationally, understand restrictions of individual boundaries Selected Therapeutic Drugs to Treat the Athlete z Widespread use in athletics and general society z Pharmaceutical labs develop compounds in vitro and then test, retest, and refine drugs in vivo before submitting it to the Food and Drug Administration (FDA) z Number of texts and databases are available for reference to determine appropriateness and effectiveness of medications for different conditions INFECTION PREVENTION Local Antiseptics and Disinfectants „ Antiseptics are substances that can be placed on living tissue for killing bacteria or inhibiting growth „ Disinfectants are used to combat microorganisms but should be applied to non-living objects „ Germicides (generic name) designed to destroy bacteria, fungicides, sporicides and sanitizers Antiseptics and Disinfectants Alcohol z z z z z Most widely used skin antiseptic Ethyl alcohol and isopropyl alcohol are equally effective Inexpensive and nonirritating, kill bacteria immediately with the exception of spores No long lasting germicidal action, can be used as an antiseptic or astringent 70% solution can be used to disinfect instruments z z z z Phenol Early antiseptic and disinfectant in medical profession Used to control disease organisms Found in various concentrations and emollients Derivatives include, resorcinol, thymol, and common house cleaner Lysol Antiseptics and Disinfectants Oxidizing agent Halogens z z z Chlorine, bromine, fluoride (used for antiseptic effect) Iodophor or halogenated compounds create a much less irritating solution than tincture of iodine Betadine solution- excellent germicide, very effective for skin lesions, abrasions and lacerations z z z z Hydrogen peroxide is commonly used in the athletic training room. Readily decomposes in the presence of organic substances and has little use as an antiseptic. Cleanses infected cutaneous and mucous membranes. Dilute solution can be used to treat inflammatory mouth and throat conditions. Antifungal Agents Medicine used to treat fungi (epidermophyton, trichophyton, and candida albicans) 1. Topical antifungals may be Over the counter medications or Prescription. 2. Oral Antifungals are by prescription only and must be ordered by a physician. 3. Vaginal antifungals are available as Over the counter medications or by Prescription. 4. All prescription antifungals must be carefully monitored. Antibiotics 1. Mechanism of Action: Interferes with the necessary metabolic processes of pathogenic microorganisms. Chemical agents that are produced by microorganisms. 2. Used topically or as systemic medication. 3. Indiscriminate use can produce hypersensitivity and prevent development of natural immunity or resistance to subsequent infections. 4. Must be prescribed and monitored by physician Antibiotics 1. 2. 3. 4. 5. 6. Bacitracin -topical antibacterial agent used alone or as a part of double or triple antibacterial ointment. Erythromycin -Broad spectrum antibiotic that includes mycoplasm and streptococcus as well as similar spectrum to Penicillin. May be used in patients allergic to Penicillin. Penicillins and Cephalosporins -Most commonly prescribed broad spectrum antibiotic class used for URI, skin infections (does not cover MRSA) Sulfonamides -Systemic antibiotic that can be used for UTI’s, ear infections, topically for eye infections, and persistent URI’s. Tetracyclines -Broad spectrum systemic antibiotic that treat a variety of URI, Chlamydia, lymes disease. Quinolones - Newer broad spectrum antibiotic that treats more severe infections. MRSA •What is MRSA? •Does your Athletic Department have a protocol for MRSA? Asthma z z z z Used to treat chronic inflammatory lung disorder or exercise induced asthma. National Asthma Education and Prevention Program has established guidelines for diagnosis and treatment Goals of asthma therapy are to prevent chronic and troublesome symptoms, maintain normal lung function, prevent exacerbation and provide adequate pharmacotherapy with minimal adverse effects Treatment should not just be drug based -monitor lung function with peak flow meter -eliminate asthma triggers -maintain healthy lifestyle with plenty of rest, exercise, and good eating habits, and hydration. Pain Relief and Antiinflammatory 1. Excitatory effect on an individual impulse is depressed 2. Individual impulse is inhibited 3. Perceived impulse is decreased. 4. Anxiety created by pain or impending pain is decreased. 5. Anti-prostaglandin effects. Counterirritants and Local Anesthetics Analgesics give relief by causing systemic and topical analgesia. Application causes local increases in circulation, redness, rise in skin temperature. 1. 2. Mild pain can often be reduced with counterirritants. Examples 3. z z z z z z z Liniments (usually counterirritant or alcohol based) Analgesic balms (often counterirritant) Spray coolants (topical anesthetic-rapid freezing) Alcohol (coolness causes temporary analgesia) Menthol (analgesic counterirritant) Cold (constricts blood vessels to numb nerve endings) Local anesthetics (injected by physician) Non-narcotic Analgesics and Antipyretics Designed to suppress mild to moderate pain without drowsiness. Acetaminophen Tylenol - effective analgesic and antipyretic but has minimal anti-inflammatory activity z Does not irritate GI system and is often replacement for aspirin in non-inflammatory conditions z Over-ingestion can lead to liver damage z Aspirin z Effective analgesic and antipyretic with antiinflammatory activity but may cause GI irritation and other side effects. Non-steroidal Anti-inflammatory Drugs z Anti-inflammatory, antipyretic and analgesic properties. z Inhibit prostaglandin synthesis and effective or osteo and rheumatoid arthritis. z Used primarily to reduce pain, stiffness, swelling, redness, fever associated with localized inflammation. Non-Steroidal Anti-inflammatory Drugs Other Considerations z Should not be used in place of acetaminophen or aspirin for headaches or increased temperature. z Individuals with nasal polyps, associated bronchospasm or history of anaphylaxis should not receive NSAID’s. z Can cause GI reactions, headache, dizziness, depression, or tinnitus. z Taken in conjunction with increased alcohol use may produce stomach irritation or GI ulceration. Nonsteroidal Anti-inflammatory Drugs Acetylsalicylic Acid (Aspirin) \ z z z z z z z Widely used analgesic, anti-inflammatory, antipyretic and may be overused thus an abused drug. Helps reduce pain, fever and inflammation. Adverse reactions generally GI related. Over-ingestion can lead to tinnitus and dizziness. .Reye’s syndrome can develop if given to adolescents. Allergic reactions result in anaphylaxis -- asthmatics may be at risk for reactions. Should be avoided within 12 hours of contact sports as it prolongs clotting time. Non Steroidal Anti-inflammatory Drug Over the Counter z Aspirin Advil z Aleve z Ketoprofen z Prescription Motrin z Anaprox z Naprosyn z Feldene z Mobic z Orudus z Celebrex z Corticosteroids z Used primarily for chronic inflammation of musculoskeletal and joint problems z Prolonged use can create complications z z z z z z z Fluid and electrolyte disturbances Musculoskeletal and joint impairment Dermatological problems Neurological impairment Endocrine dysfunction Ophthalmic conditions Metabolic impairment z Cortisone is primarily injected z Also administered through iontophoresis and phonophoresis z Can have negative effect on ligaments and tendons Drugs that Produce Skeletal Muscle Relaxation z Used to eliminate muscle guarding and spasm z cause drowsiness z Do not appear to be superior analgesics or sedatives in either acute or chronic conditions z Examples: Methocarbamol (Robaxin) , Carisoprodol (Soma), Cyclopentolate (Flexeril) Narcotic Analgesics Most derived from opium or are synthetic opiates z Depress pain impulse and respiratory center z Examples include: z Codeine z Hydrocodone (Vicodin) z Propoxyphene (Darvon) z Meperidine (Demerol) z Morphine Gastrointestinal Disorders z stomach z z z z upset flu gas formation acute or chronic hyperacidity diarrhea or constipation Drugs used to treat Gastrointestinal Disorders Relief of acid indigestion, heart burn, peptic ulcers Antacids Histamine-2 Blockers Sodium bicarbonate or z baking soda are popular Antacids with magnesium tend to z have laxative effect Those with aluminum and calcium cause constipation z Overuse can cause electrolyte imbalance z z z z Reduce stomach acid output by blocking histamine on certain stomach cells Used to treat peptic and gastric ulcers and GI hypersecretory conditions Drug examples include Cimetidine (Tagamet) and ranitidine (Zantac) Drugs used to treat Gastrointestinal Disorders z Anti-emetics z Used to treat nausea and vomiting z Working Locally z z Work on mucosal lining of stomach (may be more placebo) Pepto Bismol Working Centrally (require Rx) Affect brain, making it less sensitive to nerve impulses from inner ear and stomach z Variety of medications available, but may cause drowsiness. Phenergan, Tigan, Compazine z Drugs used to treat Gastrointestinal Disorders z Anti-flatulents Simethicone z z z Cathartics (laxatives) z z z z Provide relief from flatulence (gas) Inhibit gas formation and aid in expulsion Must be under direct supervision of physician z Constipation may be symptomatic of serious disease Indiscriminate use may render athlete unable to have normal bowel movements May cause electrolyte imbalance Anti-diarrheal Imodium z z Diarrhea tends to be a symptom, not a disease Result of emotional stress, allergies, adverse drug reactions, o different intestinal problems Colds and Allergies Symptomatic Treatment Nasal Decongestants z z Topical Oral Antihistamines z z Topical (Rx only) Oral (OTC and Rx) Antitussives Expectorants z z Water is a natural expectorant. Guaifenesin z z Non narcotic is DM Narcotic contains codeine or hydrocodone. Drugs to Control Bleeding z Vasoconstrictors z z z administered externally at sites of profuse bleeding Epinephrine commonly used Immediate acting. Often used in instances of epistaxis (nosebleed) z Hemostatic Agents z Drugs that immediately inhibit bleeding (under investigation) z Thrombin Anticoagulants z Heparin z z z Prolongs clotting time but will not dissolve clot once formed Controls extension of a thrombus already present Coumadin z Given orally, they can be used to slow clotting time in certain vascular disorders Drugs that Affect the Rate of Heat Illness Some drugs may alter the body’s ability to thermoregulate 1. 2. 3. 4. Anticholinergics and antihistamines (decrease sweating mechanism) Sympathomimetic amines (may predispose athlete to heat stroke) Phenothiazines (impacts hot/cold temp. regulation) Diuretics (alters volume expansion and cutaneous vasodilation) ATC must be aware of potential risk of medications relative to heat illnesses Be Prepared for Anaphylaxis –When life is at risk and time is critical due to an allergic reaction. –Epipen Auto Injector stops an allergic reaction fast. –Gives you time to get your Athlete/Patient emergency care. Substance Abuse Has No Place In Athletics 1. Athletic trainer must be knowledgeable about substance abuse in athletic population and should be able to recognize signs that athlete may be engaged in substance abuse. 2. Drug use and performance enhancing agents in athletics. 3. Use and abuse of substances can have a profound effect on performance Ergogenic Aids Performance Enhancing Substances z Drugs, Devices, Substances, or Procedures intended to improve athletic performance. z Some are naturally occuring, easily available and legal z Some are manufactured, illegal, and/or banned by Sporting organizations Stimulants Amphetamines and Cocaine Increase alertness, self confidence, and a feeling of energy z z Most widely used for performance enhancement z Short term and long term side effects may be of concern. z z Sympathomimethics Mental stimulation, increased blood flow, and feeling of energy. Often found in cold, allergy, and asthma meds. Anabolic Steroids Take Steroids May have Deleterious and Irreversible Effects to Health z z z Increase muscle mass, weight, growth, and bone maturation. Available as oral and injectable dosage forms Methods of Dosing: -Cycling -Stacking -Pyramiding. Designer Steroids Andro, THG, Clen, and DHEA are some of the commonly known Designer Steroid Supplements z Each has potential serious health risks. z Minimal Scientific evidence to prove benefit. z Banned by most Sports Organizations Creatine z Research has shown some positive effects, however more study is needed for long term safety/benefits z Be aware of the Tips and Cautions z Creatine supplements are not regulated, what you buy is not necessarily what you get! Human Growth Hormone z Increased use by athletes because it is more difficult to detect in testing z Like anabolic steroids, it is associated with serious and irreversible side effects. Blood Doping Blood Reinjection z Can significantly improve performance z Unethical and Dangerous z Risks involve allergic reactions, kidney damage, fever, jaundice, metabolic shock due to overload. Caffeine and other legal Drugs to Monitor Caffeine z Found in coffee, tea, cocoa, and soft drinks and is a CNS stimulant, diuretic, and stimulates gastric secretions. Habitual user that ceases use may go through withdrawal z Believed to act as ergogenic aid during prolonged activity z Banned by USOC as stimulant in high doses (12 mcg/ml) z Caffeine and other legal Drugs to Monitor Narcotic Analgesic Drugs z z Used for management of moderate/severe pain Risk physical and psychological dependency Beta Blockers z Relax blood vessels, slows heart rate and decreases cardiac output and heart contractility z Used for variety of cardiovascular and respiratory conditions In sports, misused for weight loss and decreasing concentration in urine Diuretics z Recreational Substance Abuse Among Athletes It occurs among athletes z Desire to experiment, temporarily escape, be part of the group z Can be abused and habit forming z Drug used for non-medical reasons with the intent of getting high, or altering mood or behavior z Psychological vs. Physical Dependence z z z Psychological dependence is the drive to repeat the ingestion to produce pleasure or avoid discomfort Physical dependence is the state of drug adaptation that manifests self in form of tolerance When cease consumption abruptly unpleasant withdrawal occurs Tobacco Use Nicotine is the addictive chemical in tobacco one of the most toxic drugs z z z Cigarettes, cigars & pipes are increasingly rare in athletics, but Smokeless tobacco and passive exposure to others continues to be an ongoing problem Seriously impacts performance for those that are highly sensitive Smokeless Tobacco possesses serious health risk z More addictive habit w/out exposure to tar and carbon monoxide Alcohol Use Most widely used and abused substance with athletes z Absorption affected by quantity and rate of consumption, concentration and amount of food in stomach. z oxidized by liver at 2/3 ounce/ hour z If excess is in blood stream z z .1% - lose motor function .2%-.5% symptoms become more profound and Alcohol Use Athlete abusing alcohol may exhibit the following z Mood and attitude changes z Missed practices z Isolation z Fighting or inappropriate outburst of violence z Changes in appearance z Hostility z Complaints from family z Changes in peer group Drug Use Marijuana (carcinogenic drug) z z z z z Formerly most abused drug in Western society Can lead to respiratory disease, lowered sperm count and testosterone levels, limited immune functioning and cell metabolism Causes increased pulse rate and can cause decrease in strength Psychologically causes diminution of self-awareness and judgment, slower thinking and short attention span May remain in the body and brain for weeks and months resulting in cumulative deleterious effects Drug Use Cocaine z z z z CNS stimulant w/ short duration effects (intense) Produces immediate feeling of euphoria, excitement, etc. Long term use results in psychological tolerance and dependence Overdose can lead to: Tachycardia, hypertension, extra heartbeats, coronary vasoconstriction, strokes, pulmonary edema, aortic rupture and sudden death ƒ z z Sudden stimulation w/ crack can cause cardiac or respiratory failure Can be taken in many forms including snorted, intravenously or smoked (freebased) Be Prepared for a Drug Overdose „Call 911 „Call Poison Control „ Monitor Signs „Start Vital CPR if Necessary „ The following history would be helpful if it is possible to obtain: – – – – – – – – Is the patient conscious? Is the patient breathing? What is the age of the patient? What symptoms are the patient experiencing? What drug(s) were taken try to locate the drug's container? How much of the drug was taken? When was the drug taken? Was the drug taken with alcohol or any other drugs or chemicals? Drug Testing in Athletics Purpose: Identify individuals who have problems with drug abuse and ensure health and fair practices of athletes z Controversial topic z NCAA and USOC routinely test z z Began at the Olympics in 1968 and has since expanded nationally (USOC and NCAA) and internationally Mandatory and random testing occurs at both levels The Drug Test z NCAA requires all athletes to sign a consent form agreeing to participate in testing throughout the year. z USOC tests randomly throughout the year and before USOC sanctioned events. z During the test, the athlete provides identification, and 2 samples under direct supervision; One for testing and confirmation, second for reconfirmation. If positive… the athlete is subject to sanctions! Sanctions for Positive Tests NCAA USOC First time positive in NCAA results in minimum one year suspension; will undergo random testing throughout the year Must test negative prior to reinstatement However, additional positives can result in lifetime disqualification from NCAA z z z z Sanctions range from 3 months - 24 months depending on the drug for a first time offense z Lifetime ban for subsequent positive tests Banned Substances NCAA and USOC have a banned substance list for athletes Athletic trainers working with athletes who may be tested for drugs by NCAA or athletes governed by USOC should be familiar with the lists of banned drugs and substances. z 4600 medications including ergogenic drugs, recreational drugs, as well as OTC or prescribed medications are on the list of banned substances. z USOC is more extensive than NCAA because it is also subject to IOC rules