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Pharmacology PP note

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Define Drugs: foreign substances placed into body. Medications: drugs or chemicals used to diagnose, treat, prevent disease. Pharmacology: study of drugs and their actions on body.
Names of Drugs Chemical Name – Ethyl -1- Methyl - 2 – Bad-1- stuff. Generic Name – the name that is usually suggested by the manufacturer. Official Name – the generic name with the initials “USP” behind the name. Brand Name – This is the trade name
Components of Drug Profiles Name –generic, trade, chemical Classification- the group which the drug belongs to. Mechanism of Action- the way the drug causes its effects Indications- when is it appropriate to use the drug Contraindications- when not to use the drug
Components of Drug Profiles (Cont.) Pharmacokinetics-how the drug is absorbed, distributed, and eliminated. Route of administration-how is the drug given Dosage- the amount given How supplied-concentrations Side effects
Main sources of drugs plants, animals, minerals, laboratory (synthetic) Reference Materials EMS guides United States Pharmacopeia (U S P) Physician's Desk Reference Drug inserts AMA Drug Evaluation WebMD eMedicine
Drug Sources Plants:MS, Heroin, Codeine, Atropine, Digoxin Animals: Insulin, Pitocin Minerals: Bicarb, Ca, Mag. Laboratory: Lidocaine, Valium, Humulin
Plants Night Shade - Atropine Fox Glove - Digitalis
Affect Affect –(verb) to act, an action, or influence. Clue – Affect and Action both start with “A.” And many times affect is associated with a behavior.
Effect Effect – (noun) an outcome, consequence, or influence. Clue - If there is “a / an / the” in front of the word, you should use “effect.”
Narcotic/Drug Control Pure Food and Drug Act – 1906 Improved drug quality and labeling AKA U.S. Pharmacopeia Federal Food Drug & Cosmetic Act – 1938 Gave the FDA the power to enforce safety standards
Narcotic/Drug Control Government recognized the need to control widely abused narcotics. In 1914 the Harrison Narcotic Act passed. Originally penned the name “narcotic.”
Narcotic/Drug Control 1970 Controlled Substance Act - Replaced the Harrison Narcotic Act and classified medications into 5 schedules
Human Studies Human studies: four phases. Phase 1: drug's pharmacokinetics, toxicity, safe dose. Phase 2: test on limited population. Phase 3: refine therapeutic dose; collect data on side effects. Phase 4: post marketing analysis during conditional approval.
Special Considerations - Pregnancy Geriatrics don’t metabolize medications quickly (decreased GI motility, decreased blood plasma proteins concentrations, increased fat, decreased liver and kidney function etc.) and the drug may build up in their system.
Special Considerations - Pediatrics Pediatric patients have diminished plasma proteins for some drugs to bind with, therefore, some medications will be available to the body causing an undesirable eff
Medications Medications do not create new properties on cells or tissues Medications modify/exploit existing functions. What affects medication’s effects? Age, Gender, & Genetics Weight Total Body Water/Fat Health Liver & Kidney Function Concentration Time
Drug Absorption is affected by Solubility of the drug Concentration pH Route of administration Body size Patient’s health Blood supply to the site of administration Bioavailability – the amount of drug that is still active after it reaches its target tissues
Patho Review Passive transport: movement of substance without use of energy. Diffusion: movement of solute in solution. Osmosis: movement of solvent. Filtration: movement of molecules across membrane down pressure gradient; area of high pressure to lower pressure.
Patho Review (cont.) Changing bloodstream's pH can affect protein-binding action of drug. Presence of serum protein-binding drugs can affect drug-protein binding. Albumins: chief proteins in blood for binding with drugs. Certain organs exclude some drugs from distribution.
The Basics Pharmacokinetics – absorption, distribution, metabolism and excretion of the drug Pharmacodynamics – the chemical and physical effects / drug actions Pharmacotherapeutics – drug use to prevent and treat diseases
Pharmacokinetics This is the science of how drugs are transported into, through, and then out of the body. Absorption Distribution Biotransformation Elimination
Pharmacodynamics This is effect the drug has on the body.
What can alter medication distribution Ionized drugs do not absorb across membranes of cells; most drugs do not fully ionize. pH Rate of absorption directly related to amount of surface area available for absorption. Greater the area, faster the absorption.
What can alter medication distribution (Cont.) Drug's concentration affects absorption higher concentration, more rapidly body will absorb them. Loading dose larger dose of same concentration of drug. Bioavailability measure of amount of drug still active after it reaches target tissue.
Drug Absorption & Excretion is Affected by… Some drugs have a narrow window of therapeutic effectiveness. Pregnancy – two patients to consider Increased blood volume Decreased protein binding Decreased liver function Decreased BP Side effects/Birth defects
Drug Absorption & Excretion is Affected by…(Cont.) Geriatrics – Poor health CHF Liver (filters out) Kidneys (excretes out in urine) ETC… Pediatrics – drug dosage based on child’s BSA or weight especially in neonates. Remember less body fat and immature kidneys. Use Broselow Tape or field guide
Meds Bound to Blood Protein As the drug travels through the body, it comes into contact plasma proteins (albumin). The portion of the drug bound to proteins are not capable of producing a therapeutic effect. Only the free drug is capable of working.
IONIZED + Facilitated Diffusion Using special channels that allow ion to pass, or by using a helper protein to help it pass. Electrically Charged Water Soluble Most drugs do not fully ionize Harder to diffuse
NON IONIZED + Simple Diffusion Neutral / Uncharged Lipid Soluble Easier to diffuse into cell
Ionization of table salt (NaCl) When a particle is put into water, it dissolves / breaks apart into its simpler parts creating ions. Some of these ions have a positive charge (more protons), such as sodium (Na+) and some a negative charge (more electrons), such as chloride (Cl-).
Lipid Soluble Drugs Lipid Soluble = NON-ionized (NaCl). The more lipid soluble a drug is, the more it will absorb.
Water Soluble Drugs Water Soluble or Hydrophilic = Ionized (Na+, Cl-). The more water soluble a drug is, the less it will absorb.
Ionized Ionized - An ionized drug is not lipid soluble generally does not passively cross the cell membrane. Ionized Ca++ has a charge and tends to want to bind with proteins such as albumin. Drugs and electrolytes, which are bound to proteins.
Nonionized Nonionized (neutral or uncharged) – are able to penetrate the cell’s outside lipid membrane. Therefore, lipid soluble drugs more easily diffuse across the cell membrane.
IONIZATION Most medications/electrolytes are either acids or bases. The ionized portion is charged, which attracts water molecules, thus forming larger complexes.
pH and its role in ionization / non-ionization The pH environment that the ion is in, dictates if the ion will become ionized or non-ionized. Therefore, based on the pH, drugs can be neutralized or become charged.
Water Soluble Drugs Water-soluble drugs (C & B vitamins are ingested, then dissolved by the body’s water, put into circulation, used, with the excess being excreted /eliminated from the body via urination.
Lipid Soluble Drugs Lipid-soluble drugs are ingested then dissolved in fat what we need is used and the rest is stored in fat for use later. This also means it’s easier to build up toxic levels faster with fat soluble substances.
Blood-Brain Barrier consists of a single layer of capillary endothelial cells. permits only lipid-soluble drugs to be distributed into the brain and cerebrospinal fluid. Examples of such drugs are general anesthetics and barbiturates.
Drug Class PROTOTYPE – a drug that best demonstrates the class’s common properties and illustrates its particular characteristics…It is the lead drug or first form of a drug that is used to create off-shoots of that medication.
Drug Forms
Agonist a chemical that binds to a receptor and activates the receptor to produce a response. Example: Opiates / Stimulants /Narcotics (binds with the brain’s receptors to make the pain disappear.)
Antagonist a chemical that binds to a receptor site but doesn’t produce a response. It simply blocks the agonist from working.
Competitive antagonist binds to the same site as the agonist but does not activate it, thus it blocks the agonist. However, this process is reversible; if you give enough agonist, then it will overpower the antagonist.
binds to the same site as the agonist but does not activate it, thus it blocks the agonist. And, this process is irreversible… if you give enough agonist, it will NOT overpower the antagonist. Example – Beta blocker medications
Opiate Agonist-Antagonist Opiate medications such as Talwin and Nubain which stimulate some receptors and block others As a matter of fact, people who are addicted to full strength opiates and switch to Talwin or Nubain may actually begin to have withdrawal symptoms.
Drug Classifications Drugs can be classified by the following: Body systems they affect Nervous system, cardiovascular, lungs, etc Mechanism of action Indications Drug source Chemical class
Drug Classifications: Drugs Used to Affect Nervous System Central nervous system: brain and spinal cord; all nerves that originate and terminate within brain or spinal cord Peripheral nervous system: everything else
Drugs Used to Affect Nervous System Analgesics: medications that relieve sensation of pain. Analgesia: absence of sensation of pain. Anesthesia: absence of all sensation. Opioid antagonists: reverse effects of opioid analgesics. Nonopioid analgesics: NSAID
Table 13-4 Common Opioids Morphine, Duramorph Hydromorphone, Dilaudid Fentanyl, Sublimaze Meperidine, Demerol
Table 13-7 Opioid Agonists–Antagonists Nalbuphine, Nubian Butorphanol, Stadol
Drugs Used to Affect Nervous System Anesthetics: cause respiratory, central nervous system (C N S), cardiovascular depression. Given by inhalation or injection. Most anesthetics used outside operating room given intravenously. Given locally to block sensation.
Antianxiety and sedative-hypnotic drugs: decrease anxiety, induce amnesia, assist sleeping, part of balanced approach to anesthesia. Sedation: state of decreased anxiety and inhibitions. Hypnosis: instigation of sleep.
Antianxiety/Sedative-Hypnotic Drugs Benzodiazepines, barbiturates: decrease response to stimuli; dose dependent. Benzodiazepines antagonist: flumazenil.
Common Sedatives/Hypnotics Diazepam, Valium Midazolam, Versed Lorazepam, Ativan
Antiseizure or Antiepileptic Drugs Seizures: state of hyperactivity of section of brain (partial); all of brain (generalized). May or may not be accompanied by convulsions. Goal of seizure management: balance eliminating seizures against side effects of medications used to treat them.
Antiseizure or Antiepileptic Drugs Seizures treated through several general mechanisms. Most common: direct action on sodium and calcium ion channels in neural membra
Drugs Used to Affect Nervous System Central Nervous System Stimulants Increasing release or effectiveness of excitatory neurotransmitters. Decreasing release or effectiveness of inhibitory neurotransmitters. Amphetamines, methylphenidates, methylxanthines.
Psychotherapeutic Medications
Drugs Used to Affect Nervous System Psychotherapeutic Medications Chief pharmaceutical classes of antipsychotics and neuroleptics: phenothiazines and butyrophenones. Block dopamine, muscarinic acetylcholine, histamine, alpha1 adrenergic receptors.
Table 13-12 Antipsychotics Haloperidol, Haldol Chlorpromazine, Thorazine Ziprasidone, Geodon
Drugs Used to Affect Nervous System Psychotherapeutic Medications Antidepressants: psychotherapeutic medications. Tricyclic antidepressants (T C A s), selective serotonin reuptake inhibitors (S S R I s), monoamine oxidase inhibitors (M A O I s
Autonomic Nervous System Medications Part of nervous system that controls involuntary (automatic) actions. Sympathetic nervous system: allows body to function under stress; fight-or-flight. Parasympathetic nervous system: controls vegetative functions; feed-or-breed or rest-and-repose.
Drug Classifications Autonomic ganglia: nerve fibers from C N S interact with nerve fibers from ganglia to target organs.
Drug Classifications Preganglionic: autonomic nerve fibers exit C N S; terminate in autonomic ganglia. Postganglionic: autonomic nerve fibers exit ganglia; terminate in target tissues.
Drug Classifications Synapse: space between nerve cells. Neuroeffector junction: space between nerve cell and target organ. Neurotransmitters: conduct nervous impulse between nerve cells or between nerve cell and target organ. Acetylcholine (ACh) and Norepinephrine
Drug Classifications Cholinergic: synapses that use acetylcholine as neurotransmitter. Adrenergic: synapses that use norepinephrine as neurotransmitter. Oculomotor nerve (III) Facial nerve (VII) Glossopharyngeal nerve (IX) Vagus nerve (X)
Stimulation of parasympathetic nervous system results in: Pupillary constriction (miosis) Secretion by digestive glands Reduction in heart rate; cardiac contractile force = possible low BP Bronchoconstriction (wheezing) Increased smooth muscle activity along digestive tract
Nervous System - Parasympathetic Cholinergic pertains to neurotransmitter ACh Adrenergic pertains to neurotransmitter norepinephrine. Cholinesterase – enzyme responsible for breaking down ACh.
Nervous System - Parasympathetic Parasympathomimetic (AKA cholinergic) – mimics the parasympathetic nervous system Parasympatholytic (AKA anticholinergic) – blocks the parasympathetic system.
Parasympathetic / Cholinergic Effects S – Salivation L - Lacrimation U - Urination D - Defecation G – Gastric motility E - Emesis
Atropine Contraindications High degree blocks (2nd type II and 3rd ) with wide QRS complexes Bradycardia 0.5 mg IV (Max of 3mg) Doses less than 0.5mg may cause paradoxical slowing Organophosphate 2 mg initial then 2-5mg subsequent every 5-15 minutes.
Atropine O.D. Hot as Hell Blind as a bat Dry as a bone Red as a beet Mad as a hatter
Atropine is a: Competitive Antagonist is a receptor antagonist that binds to a receptor but does not activate the receptor. The antagonist will compete with available agonist for receptor binding sites on the same receptor.
Atropine O.D. Signs/Symptoms a competitive antagonist of the muscarinic receptors Atropine dilates the pupils, increases heart rate, and reduces salivation and other secretions (Dry as a bone).
Ach Receptor Types in the Autonomic Nervous System: Muscarinic receptors were named as such because they are more sensitive to muscarine than to nicotine. Causes: decreased heart rate, constricted pupils, SLUDGE
Nicotinic ACh Receptors Low dose – excites autonomic nervous system which stimulates both the parasympathetic & sympathetic nervous system. initiates muscle contractions (increased heart rate, cardiac contraction, vasoconstriction)
Catecholamines Sympathetic Nervous System Natural: Epi Norepi Dopamine Synthetic: Isuprel Dobutamin
Sympathetic Nervous System Sympatholytic – blocks the sympathetic effects Stimulates alpha1 receptors = PVC = increased afterload from arteriole constriction and increased preload from venule constriction = increased diastolic and systolic pressures
Sympathetic Nervous System Sympathomimetic – mimics the sympathetic effects Alpha 1 stimulation can cause paradoxical bradycardia because the baroreceptors detect a rise in BP so the heart rate will decrease t
Sympathetic Nervous System
Beta 2 agonists medications used to treat asthma by stimulating beta 2 in the lungs causing the smooth bronchial muscles to relax. They may also work on other smooth muscles ( dilates blood vessels in the skeletal muscle, brain, and heart).
Beta 2 agonists also stimulate beta 1 which will cause tachycardia. Induces glycogenolysis (breaking down glycogen turning it into glucose)
ADH Antidiuretic hormone (ADH) Released from posterior pituitary AKA vasopressin ADH = fluid retention to combat dehydration
ADH The Hypothalamus senses low blood volume and increased serum osmolatity and signals the pituitary gland Pituitary gland secretes ADH into the bloodstream ADH causes kidneys to retain water Water retention boosts blood volume and decreases osmolality
Aldosterone Aldosterone = fluid retention Works alongside ADH to fight dehydration Aldosterone initiates active transport of sodium from the kidney’s nephrons to the blood stream… and remember, water follows salt.
Aldosterone Production Blood flow to the glomerulus drops. juxtaglomerular cells secrete renin into the bloodstream. Renin travels to the liver. Renin converts angiotensinogen in the liver to angiotensinogen 1 Angiotensinogen 1 travels to the lungs.
Aldosterone Production (Cont.) Angiotensinogen 1 in the lungs is converted to angiotensinogen 2. Angiotensinogen 2 travels to the adrenal glands. angiotensinogen 2 stimulates the adrenal glands to produce aldosterone
Cardiac Antidysrhythmics Sodium Channel Blockers Procainamide Lidocaine Dilantin Beta Blockers All of the “LOL’s” Potassium Channel Blockers Amiodarone Calcium Channel Blockers Verapamil Misc. Adenosine Digoxin Mag
Sodium Channel Blockers Affect Na+ influx in phases 0 of fast action potentials. This slows the impulses down in the cardiac cells of the atria and ventricles… it doesn’t affect the SA or AV nodes.
Beta Blockers Beta 1 receptors are attached to the calcium channels, therefore blocking the beta receptors also blocks the calcium channels blocking influx of Ca+ of the slow action potential.
Calcium Channel Blockers Decrease SA and AV node automaticity, but most of their effectiveness occurs at the AV node. They effectively slow the impulse coming from an out of control rapid atrial fib at the AV node which slows ventricular response.
HTN HTN is a major cause of cardiac disease, blindness, renal failure and stroke. B/P = cardiac output x PVR C/O = HR x SV
Antihypertensive Meds. MOST COMMONLY USED Diuretics Beta Blockers USED AFTER THE OTHERS DIDN’T WORK: ACE inhibitors Calcium Channel Blockers Vasodilators
Diuretics in HTN Reduce circulating blood volume by increasing the urine O/P, therefore it reduces preload >>> C/O reduces BP
ACE Inhibitors in HTN Angiotensin Converting Enzyme Vasotec Zestril Captopril Prevents the conversion of angiotensin I to angiotensin II. Angiotensin II is a potent vasoconstrictor. So, if you block it, the vessels relax and your BP goes down
Cardiac Glycosides Occur naturally in the foxglove plant Increases intracellular levels of Na+ which also results in increased intracellular Ca+. It’s the Ca+ which causes an increase in contractile force of the heart. Digoxin (Lanoxin)
Thrombi Meds. Antiplatelets ASA Persantine (vasodilator and antiplatelet…used in a chemical induced “treadmill” stress test. Amiphylline reverses persantine’s effect) Ticlid Anticoagulants Coumadin (Warfarin) Heparin Thrombolytics Streptase tPA
Cholesterol Meds. LDL’s = CAD HDL’s = good cholesterol Zocor Mevacor Anything that ends in a “statin”
Decongestants / Antihistamines Expectorant – increases the productive cough. Mucolytic – waters down the mucous Antitussive – suppresses the cough Affrin Benadryl Don’t use benadryl in asthmatic patien
Prep Needed Before Med. Administration BSI Practice aseptic techniques Fill syringe Reconstitute powdered meds with fluid Be cautious when snapping the ampule’s neck Skin prep Betadine or alcohol Circular motion from center outward
Speed in Routes of Administration Oral – slow SC – slow Topical – Moderate IM – Moderate Intralingual – rapid Rectal – rapid
Speed in Routes of Administration (cont.) SL – rapid ET – rapid Inhalation – Rapid IO – immediate IV – immediate Intracardiac (Pulp Fiction style) - immediate
Pharm. Terms to Know BSI / PPE Sterile – free of all forms of life Medically clean – keeping it clean Disinfectant – cleansing agent that is toxic to living tissue (Bleach) Asepsis – free of pathogens (alcohol preps “pop” bacteria making it harmless)
Injections Intradermal Under the skin 10 – 15 degree angle Slow rate of absorption 1CC syringe Used for allergy and TB tests
Injections Subcutaneous – Adipose layer 45 degree angle No more than 0.5cc Upper arm, abdomen, thighs Epi and insulin
Injections Intramuscular – 90 degree angle Deltoid Up to 1ml Dorsal gluteal Up to 5ml Rectus Femoris Up to 5ml
IV Cannulation Tourniquet (stop venous flow, not arterial) Look and feel for a peripheral vein (AC best for full arrests) Aseptic (circular, alcohol prep) Approximately 10-15 degree angle Look for blood flash If new attempt needed, start second more proximal.
Created by: Sheamiles1995
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