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Pharmacology Basics Adapted from NurseCE4less.com for Ambercare Corporation Education Department, 2014 Slide 2 OBJECTIVES Describe the role of receptors related to medications Discuss the four components of pharmacokinetics Describe how medications are classified Identify medication classifications, actions, uses, adverse reactions, side effects, contraindications and implications Slide 3 DID YOU EVER WONDER? HOW Tylenol knows to go to your head when you have a headache and to your elbow when you have tennis elbow? OR how one or two small tablets containing only 500- 1000 mg of active drug can relieve a headache or ease the inflammation from a strained muscle or tendon in a 185 pound athlete? Slide 4 Basic principles of pharmacology includes Pharmacokinetic Process: Absorption Distribution Metabolism Excretion Slide 5 Patient safety is paramount! Medication management help patients by: Curing disease or infection, relieving symptoms such as pain or nausea Can also have the reverse effect: In terms of: Allergic reaction Overdose Adverse reaction Administering wrong medication Slide 6 Receptors function? Medications are distributed throughout the body by the blood and other fluids of distribution Once they (the med) arrives at its proper site of action, they act by binding to receptors, usually located on the outer membrane of cells or enzymes located within the cell Receptors are like biological light switches which turn on and off when stimulated by a drug which binds to the receptor and activates it Slide 7 Receptors Narcotics (Opioids) like Morphine bind to receptors in the brain that sense pain and decrease the intensity of that perception Antiplatelets (ASA); NSAIDs (Advil) or Antipyretics (Tylenol) bind to an enzyme located in the cells outside the brain close to where the pain is localized (e.g., hand, foot, low back, BUT NOT IN THE BRAIN) thereby decreasing the formation of biologically-active substances known as prostaglandins, which cause pain and inflammation Slide 8 Receptors Food for thought! In some instances a drugs site of action or receptor may actually be something that resides within the body but is not anatomically part of the body i.e., Tums the site of action is the acid in the stomach that is chemically neutralized However, if you take an OTC (Tagamet, Pepcid) that INHIBITS stomach acid production instead of neutralization of acid, these compounds BIND to and INHIBIT receptors in the stomach wall responsible for producing acid! Slide 9 Receptors another example Antibiotic therapy is another example of a drug that binds to a receptor that is not part of your body. Abx bind to portions of the bacterium that is living in the body which is causing illness. Most Abx inhibit an enzyme inside the bacteria that causes the bacteria to either stop reproducing or to die from inhibition of a vital biochemical process Slide 10 Pharmacologist discoveries As medical science has learned more about how drugs at, pharmacologists have discovered that the body is full of different types of receptors that respond to many different types of drugs. Some receptors are very selective and specific, while others lack such specificity and respond to several different types of drug molecules Slide 11 Receptors common drugs To date, receptors have been identified for the following common drugs, or neurotransmitters found in the body: Narcotics (opioids) Morphine Benzodiazepines (Valium, Xanax) Acetylcholine (nicotinic and muscarinic cholinergic receptors) found in the parasympathetic system (resting/digesting) Dopamine, serotonin (sympathetic system) Epinephrine (adrenalin) and NE (alpha and beta receptors) found in the sympathetic system (fight/flight) of the CNS and many others. Slide 12 Neurotransmitters Neurotransmitters are chemicals released from the END of ONE NEURON (nerve cell) which diffuse across the space between neurons called the synaptic cleft and stimulate an adjacent neuron to signal the transmission of information. Slide 13 Pharmacokinetics Pharmacokinetics what is it? a branch of pharmacology which deals with determining the movement (kinetics) of drugs into and out of the body Slide 14 Four scientific or pharmacokinetic processes.. Absorption Distribution Metabolism Excretion Slide 15 Absorption Is the process by which a drug is made available to the fluids of distribution of the body (e.g., blood, plasma, serum, aqueous humor, lymph, etc.). In the fasting state, most orally-administered drugs (PO) reach maximum or peak blood concentration within one to two hours IV is the most rapid route of administration, then Intra-nasal Inhalation SL IM SC or SQ (in the above order) route of administration. Slide 16 Rate of Absorption - Dependent on (PO drugs) and the subsequent appearance of the drug in the blood on the following factors: Rate of disintegration and dissolution of the pill or capsule in the stomach or GI tract Solubility of the drug (the more soluble, the faster absorption rate) The molecular charge of the drug molecule (charged substances are soluble, but dont pass through lipid (fat) soluble biologic membranes well) Aqueous (water) solubility vs. lipid (fat) solubility The presence or absence of food in the stomach (food delays the absorption of some drugs and enhances the absorption of others) Slide 17 Rate of Absorption key factors The presence of any concomitant medication(s) that can interfere with GI motility (e.g., Reglan increase GI motility, Aluminum antacids slow motility, atropine or scopolamine used for ulcers or nausea also slow GI motility (anticholinergic) keeping some drugs in the stomach longer slowing absorption rate; on the flip side: Tagamet, Zantac and Prilosec (Pepcid-AC) DECREASE gastric acid production thereby INCREASING the rate of gastric emptying and increasing the rate of absorption.. Slide 18 Distribution Once the drug has been absorbed from the stomach and/or intestines (GI tract) into the blood, it is circulated to some degree to all areas of the body to which there is blood flowthis process is distribution (the choo-choo so to speak) Organs with high blood flow (brain, heart, liver, etc.) are the first to accumulate drugs, while connective tissue and lesser-perfused organs are last Slide 19 Distribution effects The pattern of distribution of drug molecules by different tissues after the chemical enters the circulatory system varies. Why? Because of differences in pH, lipid content, cell membrane function and other individual tissue factors, most drugs are NOT equally distributed in all parts of the body E.g., ASA acidity influences a distribution patter that is different from that of an alkaline product such as amphetamine Slide 20 Metabolism Is the transformation of the drug molecule into a chemically related substance that is more easily excreted from the body (also know as: biotransformation, or detoxification) Drug metabolism is the process by which the body breaks down and converts medication into active chemical substances. Drugs can interact with other drugs, food and beverages. Interactions can lessen or magnify the desired therapeutic effect of a drug, or may cause unwanted or unexpected side effects Slide 21 Metabolism primary site The primary site of drug metabolism is the liverplays a major role in digestion, detoxification, and elimination of substances from the body (ponder of this statement for momentconsider disease processes such as ES liver disease what do you need to consider when administering drugs that are metabolized in the liver)? Slide 22 Metabolism Enzymes in the liver are responsible for chemically changing drug components into substances known as metabolites Metabolites are then bound to other substances for excretion through the lungs, or bodily fluids such as saliva, sweat, breast milk and urine, or through reabsorption by the intestines Slide 23 Metabolic Rate Can vary from individual to individual and drug dosages that work quickly and effectively in one individual may not work well for another Factors such as genetic disposition, environment, nutrition and age can influence drug metabolism Infants and elderly patients may have a reduced capacity to metabolize certain drugs and can be at risk for drug toxicity Slide 24 Metabolism Therapeutic agents like antibiotics and drugs used for the treatment of high blood pressure, epilepsy (phenobarbital, Dilantin) pain (morphine, codeine), anxiety (valium Xanax) are also metabolized to chemically-related compounds called metabolites which are excreted in the urine Slide 25 Drugs that commonly interact with other meds: Diuretics (such as HCTZ) can reduce serum K+ and Na+ electrolyte levels when taken with digoxin and lithium respectively MAOIs antidepressants can cause convulsions and other serious side effects when used with tricyclic antidepressants (nortriptyline), SSRIs or sympathomimetic drugs (amphetamines) Antibiotics may reduce the efficiency or oral contraceptives Slide 26 Drugs that commonly interact with other meds: Medications containing metals, such as antacids with aluminum additives and iron supplements can reduce the absorption of tetracycline's and fluoroquinolones Drugs that inhibit liver enzyme function thereby slowing metabolism include; ciprofloxacin, erythromycin, fluoxetine, paroxetine and ritonavir. The therapeutic effect of other medications taken with these drugs may be amplified Coumadin should be used with GREAT caution in patients taking these drugs! Slide 27 Foods and beverages / drug interactions Grapefruit juice inhibits metabolism of many meds; including: cyclosporines, felodipine, nifedipine, triazolam and midazolam (to name a few) Foods and beverages with tyramines (red wine, malted beers, smoked foods, dried fruits and aged cheeses) can cause severe and dangerous elevation in blood pressure when taken with MAOI inhibitors (antidepressants emsam; marplan; nardil; parnate) Slide 28 Foods and beverages / drug interactions Dairy products (milk, cream) and products containing calcium can prevent the absorption of antibiotics such as tetracycline, doxycycline, and ciprofloxacin Whole milk with Vitamin D can cause milk-alkali syndrome in patients taking aluminum hydroxide antacids Caffeinated beverages can influence drug metabolism Alcohol is a CNS depressant should not be combined with other CNS depressants (antipsychotics, antihistamines) Slide 29 Excretion Is the process by which a drug is eliminated from the body by various organs such as the kidney and lungs and found in many biological fluids like: bile, sweat, hair, breast milk, or tears. However, the most common is the urine (excretion of drug) In order to determine the rate of excretion of any drug from the blood, one must first be certain that the entire drug in the patients GI tract has been absorbed (consider GI patients whos absorption rate is impaired via their disease process) Slide 30 Excretion The amount of time required to eliminate half of the drug from the body is called the half-life Generally, it takes six half-lives to rid the body of 98% of drug and 10 half-lives to completely eliminate the drug from the body Using these mathematical relationships allows pharmacologists to determine how often a therapeutic drug should be administered to a patient or toxicologist to determine a time interval within which one would test positive for drugs of abuse Slide 31 Drug Nomenclature A medication will have a generic name and one or more trade names the generic name usually signifies the medication's chemical derivation. The trade name is a name chosen by the pharmaceutical company for purposes of marketing. Trade names usually begin with a capital letter and followed by a trademark Generic names generally begin with a lower case letter Slide 32 Examples GenericTrade ibuprofenMotrin acetaminophenTylenol benzoyl peroxideOxy10 Slide 33 Drug Classifications Drugs are classified into different groups according to their chemical characteristics, structure and how they are used to treat specific diseases Example: Controlled versus Non-controlled; Non- controlled med is not considered to be a depressant or a stimulant and is not considered addictive or with a potential for abuse (OTCs or prescription drug) Slide 34 Controlled Meds Are divided into five schedules based on their potential for abuse and physical and psychological dependence Slide 35 Controlled meds Schedule I: drugs that currently do not have accepted medical use, have a high potential for abuse, and lack accepted safety measures for use (LSD, peyote, heroin) Schedule II: drugs that have medical use and a high potential for abuse; may cause severe dependence (morphine, secobarbital, amphetamines (Ritalin), methadone) Slide 36 Controlled Meds Schedule III: drugs used in medical practice with less potential for abuse than Schedule II drugs; may cause moderate to low physical dependence or high-psychological dependence (T3s Tylenol with codeine; stimulants, depressants, other classes ketamine is another example) Schedule IV: drugs that have medical use and lower abuse potential than CIII drugs; tend to cause limited physical or psychological dependence (diazepam) Schedule V: drugs that have medical use and lower potential for abuse than CIV drugs (cough syrups containing Codeine) Slide 37 Drug Classifications Enable us to readily identify the similarities and differences among a large number of medications; one of the best ways to master pharmacology is to become familiar with medication classifications.lets review some. Slide 38 Alpha-Adrenergic Blockers ActionsThey bind to a-adrenergic receptors leading to dilation of peripheral blood vessels; lowering peripheral resistance and BP UsesHTN, BPH, Raynauds short/long- acting agents (Cardura, Minipress) Adverse reactions /side effectsHypotension, nasal congestion, tachycardia, diarrhea, N/V ContraindicationsMI, CAD, including angina ImplicationsK+, Na+, carbon dioxide lab monitoring - daily #s; intake/output data orthostatic BPs Slide 39 Antacids ActionsContain magnesium, aluminum, calcium and a combination of these compounds. They slow down the rate of gastric emptying and neutralize gastric acidity UsesGastritis, peptic ulcer, hiatal hernia and GERD (aluminum carbonate, calcium carbonate tums) Adverse Reactions & Side EffectsConstipation, diarrhea, flatus, abdominal distention, alkaluria ContraindicationsAllergy and sensitivity ImplicationsAssess epigastric pain, GI symptoms and renal problems and electrolytes Slide 40 Antianginals ActionsNitrates dilate coronary arteries, decrease preload/afterload; CCB dilate CA, decrease SA/AV node conduction; BB decrease HR, thus decreasing oxygen use UsesAngina. CCBs, BBs HTN and dysrhythmias (ols, nitro, verapamil) Adverse Reactions & Side EffectPostural Hypotension, fatigue, dysrhythmias, HTN, edema, dizziness ContraindicationsIncrease ICP, cerebral hemorrhage and sensitivity ImplicationsMonitor for SE / Orthostatic BP; assess for angina pain Slide 41 Anticholinergics ActionsInhibit acetylcholine (autonomic NS) UsesMany. Some decrease GI, urinary and biliary motility; GI secretions, decrease involuntary movement and relieve N/V; decrease secretions at EOL; increase HR in emergent situation; COPD (atropine, scopolamine) Adverse Reactions/Side EffectsDryness of mouth; paralytic ileus, constipation, urinary retention/hesitancy) dizziness and Ha ContraindicationsGI or urinary obstruction; narrow- angle glaucoma, and myasthenia gravis ImplicationsMonitor urinary and bowel function as well as vital signs; Slide 42 Anticoagulants ActionPrevent clot formation UsesMI; PE; DVT; DIC; Afib; and HD patients (Coumadin, heparin) Adverse Reactions & Side EffectsHemorrhage, diarrhea, fever, rash and blood disorders (leukopenia, thrombocytopenia) ContraindicationsBleeding disorders, such as hemophilia, and leukemia, ulcers, blood dyscrasias, nephritis, endocarditis and thrombocytopenia purpura ImplicationsObserve for bleeding (black stools, ecchymosis); monitor hgb/hct; PT/INR; PTT; vital signs Slide 43 Anticonvulsants ActionsTo prevent seizures UsesPrevent tonic-clonic seizures, psychomotor seizures, status epilepticus, petit mal and cortical focal seizures (Phenytoin, Diazepam) Adverse reactions & side effectsBone marrow suppression (can be life- threatening) GI problems; CNS effects like confusion, ataxia and slurring of speech ContraindicationsAllergy or sensitivity to drug class ImplicationsMonitor hepatic and renal function, blood, mental status, blood dyscrasias, and toxicity especially Stevens- Johnson syndrome Slide 44 Antidepressants Actions MAOIs inhibit MAO and thus increase epinephrine, NE, serotonin and dopamine; Tricyclic's - block the reuptake of serotonin and NE in the nerve endings, thus increasing the actions of both in the nerve Uses Depression, nocturnal enuresis in children; (Sertraline; amitriptyline; bupropion; lithium) Adverse Reactions & Side Effects Orthostatic hypotension; dry mouth; dizziness, drowsiness; urinary retention, HTN, renal failure and paralytic ileus Contraindications BPH; seizure disorders, renal, hepatic and cardiac disease Implications Monitor BPs; mental status; renal/hepatic function; extrapyramidal symptoms; urinary retention; withdrawal s/sx with abrupt cessation Slide 45 Anti-Diabetic Meds ActionsLowers blood sugar, K+ and P04; oral med stimulates B-cells of pancreas to release insulin UsesDiabetes and ketoacidosis; (Insulin, Glyburide) Adverse Reactions & Side EffectsHypoglycemia, hepatotoxicity, allergic responses ContraindicationsOral agents are contraindicated for juvenile diabetes and ketoacidosis ImplicationsMonitor CBGs; assess for hypoglycemia, rotate insulin injection sites and use human insulin when pork or beef sensitivity Slide 46 Antidiarrheal ActionsVarying. Some decrease water content in stool, some slow GI peristalsis UsesDiarrhea; (bismuth, kaolin pectin; loperamide) Adverse Reactions & Side EffectsConstipation, paralytic ileus, abdominal pain ContraindicationsColitis ImplicationsUsed for short term therapy (48 hours or less) monitor electrolytes and bowel response Slide 47 Antidysrhythmics Actions Class I: - decreases any disparity in the refractory period; increases duration of AP Class II: slows rate of SA node discharge and conduction through AV node; decreases HR decreasing oxygen demand in myocardium Class III: increases effective refractory period and AP duration Class IV: decreases SA nod discharge; slows conduction through AV node; inhibits Ca++ across cell Uses Atrial and Ventricular arrhythmias (afib, PVCs and tachycardia, HTN, angina) Digoxin, procainamide, acebutolol, amiodarone Adverse Reactions and Side Effects Hypotension, bradycardia, pro-arrhythmic effects Contraindications Various can be numerous Implications Monitor rate and rhythm, BP, K+ dependent edema, I/Os; eyesight, lung function; kidney function Slide 48 Antifungals Actions Decreases Na+, K+ and nutrients in the cell and increases cell permeability Uses Fungal infections such as cryptococcosis, aspergillsis, histoplasmosis, coccidiomycosis and candidiasis (Nystatin, Amphotericin B) Adverse Reactions & Side Effects Renal, liver damage and failure, gastroenteritis, hypoK+, anorexia, N/V Contraindications Sensitivity and bone marrow depression Implications For IV administration, use a filter, check for extravasation and protect from light (cover with foil). Monitor VS, I/O, weight, renal and hepatic function, HypoK+ and ototoxicity Slide 49 Antihistamines ActionsAntagonists of Histamine UsesAllergies, pruritus and rhinitis; decrease N/V; (Benadryl, Allegra, Claritin, Alavert, Tavist, Zyrtec, Chlor-trimeton); Adverse Reactions & Side EffectsDrowsiness, Ha, urinary retention, blood dyscrasias, thickened bronchial secretions and GI effects ContraindicationsSensitivity, asthma, PUD, narrow angle Glaucoma ImplicationsMonitor urinary frequency, respiratory and cardiac status and for blood dyscrasias Slide 50 Antihypertensives Actions ACEI dilate arterial and venous system; suppression of RA I to RA II; CA Adrenergic: inhibits impulses in CNS (SNS); decrease in CO, BP and HR Peripherally Adrenergics: inhibits release of NE; decreasing sympathetic vasoconstriction Vasodilators: decrease BP, HR/CO dilate smooth muscle of the arteries; BB/CCB/Diuretics discussed later Uses HTN, HF, angina and some dysrhythmias Adverse Reactions & Side Effects Hypotension, tachycardia, bradycardia, N/V/Ha Contraindications Heart block, hypersensitivity Implications Edema, monitor renal function, and HF Slide 51 Anti-Infectives ActionsInhibit the growth and/or replication of susceptible bacteria UsesInfection(s) (PCN, Tetracycline) Adverse Reactions & Side EffectsD/N/V, bone marrow depression and anaphylaxis ContraindicationsHypersensitivity; most ppl allergic to PCNs are also allergic to cephalosporin's ImplicationsObserve bowel pattern and urinary output. Monitor renal function, blood cultures and for signs of super infection and bleeding; along with WBCs Slide 52 Antineoplastics Actions Alkylating agents interfere with DNA; Antimetabolites inhibit DNA synthesis Antibiotics: - inhibit RNA delay or inhibiting mitosis Hormones: - change the effects of androgens, estrogen, luteinizing hormone and FSH Uses Tumors, lymphoma, leukemia and Hodgkins disease (fluorouracil; cisplatin) Adverse Reactions & Side Effects Anemia, thrombocytopenia, leukopenia, N/V; hair loss, hepatotoxicity, cardiotoxicity Contraindications Sensitivity, liver and renal damage Implications Monitor CBC with diff; renal and liver function tests; I/O; observe for bleeding, jaundice, dependent edema, breaks in skin and mucosal inflammation, irritation, phlebitis with IV route Slide 53 Antiparkinson Agents ActionsCholinergic-block acetylcholine receptors (blocks PSS) UsesParkinsons Disease (Levodopa) Adverse Reactions & Side EffectsInvoluntary movement, insomnia, N/V; orthostatic Hypotension; dry mouth; numbness and Ha ContraindicationsSensitivity and narrow angle glaucoma ImplicationsMonitor respirations, BP and changes in mentation Slide 54 Antipsychotics / Neuroleptic agents Actions Block dopamine receptors in the brain that involves psychotic behavior Uses Schizophrenia, mania, paranoia, and anxiety; can be used for unrelieved hiccups, N/V and pedi behavioral problems and pre-op relaxation (haldol, lithium) Adverse Reactions & Side Effects Extrapyramidal symptoms (dystonia, EPS< akathisia, and tardive dyskinesia); dry mouth, photosensitivity, agranulocytosis, hypotension and life threatening cardiac problems and laryngospasm Contraindications CAD, severe HTN, depression, bone marrow depression; blood dyscrasias, parkinsonism, cerebral arteriosclerosis, narrow angle glaucoma and children less than 12; caution in elderly Implications Monitor CBC, LFTs I/O; BP; dizziness; palpations, tachycardia; LOC, gait and sleep patterns Slide 55 Antituberulars ActionsDecreases the replication of the offending bacillus through the inhibition of RNA or DNA UsesPulmonary TB (Rifampin, Isoniazid, Rifabutin) Adverse Reactions & Side EffectsAnorexia, N/V; rash, renal, hepatic and ototoxic effects ContraindicationsSensitivity, renal disease; caution with hepatic disease, pregnancy and lactation ImplicationsCheck renal and hepatic status and s/sx of anemia Slide 56 Antitussives and Expectorants ActionsAntitussives suppression of the cough reflect; Expectorants decrease in the viscosity of thick, tenacious secretions UsesCough bronchitis, TB, pneumonia, CF; COPD; (antitussives are used for non-productive coughs) Guaifenesin, codeine) Adverse Reactions & Side EffectsDizziness, drowsiness and nausea ContraindicationsIodine sensitivity, pregnancy, lactation and hypothyroidism; caution in elderly and asthma patients ImplicationsMonitor cough and sputum, increase fluid intake and humidification to thin secretions Slide 57 Antivirals ActionsInterferes with the DNA needed for viral replication UsesHIV, herpes, encephalitis, varicella zoster encephomyelitis, influenza (acyclovir, tamiflu) Adverse Reactions & Side EffectsN/V/D/Ha, anorexia, vaginitis, renal failure and metabolic encephalopathy which could be fatal ContraindicationsCaution in pregnancy and lactation; renal and liver disease and dehydration ImplicationsAssess renal and liver functions; observes for s/sx of infection and allergic reactions (itching, rash, urticaria); monitor for blood dysrasias Slide 58 Barbiturates ActionsDecrease impulse transmission to the cerebral cortex UsesEpilepsy, sedation, insomnia, anesthesia, (phenobarbital and secobarbital) Adverse Reactions & Side EffectsDrowsiness, Nausea, blood dyscrasias and Steven-Johnson syndrome ContraindicationsAllergy, poor liver function, pregnancy (cat D). Caution in elderly ImplicationsMonitor seizure control, BMP, LFTs; observe for toxicity insomnia, hallucinations, hypotension, pulmonary constrictions, cold clammy skin, cyanosis of lips (circumoral) N/V delirium, weakness) Slide 59 Benzodiazepines Actions Decreases anxiety by potentiating g- aminobutyric acid and other CNS inhibitory transmitters Uses Anxiety secondary to phobic disorders and other conditions, acute ETOH withdrawal and pre-op (Diazepam, Clonazepam) Adverse Reactions & Side Effects Physical dependence and abuse, dizziness, drowsiness, OHTN, and blurred vision Contraindications Narrow angle glaucoma, infants less than 6 months, lactation (diazepam) and liver disease (clonazepam); caution in elderly Implications Monitor OHTN; HR, LFTs BMP and signs of dependency; administer with milk or food to prevent GI upset Slide 60 Beta-Adrenergic Blockers BB (ols) Actions Selective: block stimulation of B1 receptors (one heart) in the cardiac smooth muscle with chronotropic and inotropic effects; Non-selective: lowers BP (plasma renins are reduced) w/o reduction in HR or reflex tachycardia Uses HTN, angina and ventricular dysrhythmias (atenolol, metoprolol, propranolol,) Adverse Reactions & Side Effects Ohtn, N/V/D, bradycardia, blood dyscrasias, CHF and bronchospasm Contraindications Hblock, cardiogenic shock and HF; caution in elderly, COPD an asthma patients; CAD, renal and thyroid disease patients Implications Monitor VS; I/O, Daily #s; renal function, edema, apical and radial pulse Slide 61 Bronchodilators Actions Anticholinergics inhibit the interaction of acetylcholine at receptor sites on bronchial smooth muscle Uses Asthma, bronchospasm, COPD, Cheyne- Stokes respirations (albuterol, aminophylline) Adverse Reactions & Side Effects Dyspnea, bronchospasm, anxiety, tremors, throat irritation, N/V Contraindications Narrow angle glaucoma, severe cardiac disease, tachydysrhythmias and sensitivity; use caution with HTN, seizure disorders, pregnancy and lactation, hyperthyroidism and BPH Implications Assess for a therapeutic response (absence of dyspnea and/or wheezing) and patient/family education about use of inhaler Slide 62 Calcium Channel Blockers Actions Inhibits the flow of calcium ions across the cell membrane of cardiac and vascular smooth muscle, thus relaxing the coronary vascular smooth muscle, dilating the CA, slowing SA/AV node conduction, and dilating peripheral arteries Uses Angina, HTN, and dysrhythmias (verapamil, felodipine) Adverse Reactions & Side Effects Dysrhythmias, edema, fatigue, HA and drowsiness Contraindications SBP of less than 90 mmHg; Wolff-Parkinson White Syndrome; 2/3 rd degree HB; SSS; and cardiogenic shock; HF may get worse in the presence of edema; caution with renal and hepatic disease Implications Monitor BP, HR, RR; administer at bedtime and before meals Slide 63 Cardiac Glycosides Actions Cardiac output and cardiac contractility are enhanced by making more calcium available Uses HF and tachycardia (digitoxin, digoxin) Adverse Reactions & Side Effects Cardiac changes, hypotension, GI blurred vision, yellowish-green halos and Ha Contraindications Hypersensitivity, Vfib, Vtach and carotid sinus syndrome; caution with electrolytes imbalance; acute MI; severe respiratory disease, AV block, renal or liver disease, hypothyroid and the elderly Implications Assess VS, check apical rate for one full minute if less 60 hold and notify physician; monitor BMP; I/O Slide 64 Cholinergics Actions These medications prevent the destruction of acetylcholine, thus increasing its concentration, which enhances the transmission of impulses Uses Myasthenia gravis, bladder distention, urinary distention, and post op paralytic ileus (neostigmine, bethanechol) Adverse Reactions & Side Effects Bronchospasm, laryngospasm, respiratory depression, convulsion, paralysis, respiratory arrest, N/V/D Contraindications Renal or intestinal obstruction, cautious with children, lactation, bradycardia, hypotension, seizure disorders, bronchial asthma, coronary occlusion and hyperthyroidism Implications Monitor VS, I/O; assess for urinary retention, bradycardia, bronchospasm, hypotension, respiratory depression Slide 65 Cholinergic Blockers Actions Blocks the ANS acetylcholine Uses Prevention of surgical secretions, - (at EOL also) decrease motility of the urinary, biliary and GI tracts; reverses NM blockage; parkinsonism symptoms secondary to the use of neuroleptic medications (atropine, scopolamine) Adverse Reactions & Side Effects Constipation and dryness of the mouth Contraindications GI and GU obstruction, angle closure glaucoma, myasthenia gravis, and hypersensitivity; caution with elderly, BPH and tachycardia patients Implications Monitor urinary status; I/O monitor dysuria, frequency or retention; observe constipation, LOC; administer with milk or food Slide 66 Corticosteroids Actions Glucocorticoids increase capillary permeability and suppress the movement of fibroblas and leukocytes, thereby decreasing inflammation Uses Glucocorticoids decrease inflammation some are used for adrenal insufficiency, allergies and cerebral edema (cortisone, dexamethasone, hydrocortisone, prednisone) Mineralocorticoids adrenal insufficiency Adverse Reactions & Side Effects Insomnia, euphoria, behavioral changes, PUD, sodium and fluid retention, hypokalemia, hyperglycemia, and carbohydrate intolerance (metabolic reactions) Contraindications Fungal infections, amebiasis, hypersensitivity, and lactation. Caution in elderly, children and pregnant women, diabetes, seizures, PUD, glaucoma, HF, HTN, impaired renal function,myasthenia gravis and ulcerative colitis Implications Give with food; monitor CBG, K+; Weight; I/O; plasma cortisol levels, adrenal insufficiency and for any signs of infection; mood changes, particular depression Slide 67 Diuretics Actions Thiazides and thiazide-like diuretics slow reabsorption n the distal tubule, thus increasing the excretion of sodium and water; Loop diuretics inhibit the reabsorption of Na+ and Chloride in the loop of Henle Carbonic anhydrase inhibitors decrease the sodium-hydrogen ion exchange in the tubule, thus increasing sodium excretion Uses HTN with edema and HF (lasix, HCTZ, aldactone) Adverse Reactions & Side Effects HypoK+; hyperglycemia and hyperuricemia (mostly with thiazides) blood dyscrasias, aplastic anemia, volume depletion, and dehydration Contraindications Electrolyte imbalances, anuria, dehydration; caution in elderly and renal or hepatic patients Implications K+ supplement may be needed with loop diuretic; observe for signs of hypokalemia and metabolic alkalosis; given in am Slide 68 Histamine H2 Antagonists Actions Inhibits histamine in the parietal cells, thereby inhibiting the secretion of gastric acid secretion Uses Gastric and duodenal ulcers, GERD; (cimetidine, ranitidine) Adverse Reactions & Side Effects Thrombocytopenia, neutropenia, aranulocytosis, aplastic anemia, confusion, diarrhea and Ha Contraindications Hypersensitivity, cautious in children less than 16 years of age, hepatic or renal disease, organic brain syndrome, lactation and pregnancy Implications Monitor I/O; creatinine, BUN and gastric pH; (maintain above 5); give slowly IV over 30 minutes to avoid bradycardia and administer oral with meals Slide 69 Immunosuppressant's ActionsInhibits lymphocytes UsesPrevention of organ transplant rejection; cyclosporine, azathioprine) Adverse Reactions & Side EffectsProteinuria, renal failure, albuminuria, hematuria, hepatotoxicity, oral candida, gum hyperplasia, HA and tremors ContraindicationsHypersensitivity; caution in severe hepatic or renal disease and pregnancy ImplicationsMonitor LFTs and BMP, drug blood levels; observe for hepatotoxicity, which can include itching, light colored stools, jaundice and dark urine; administer with meals Slide 70 Laxatives Actions Used to treat and prevent constipation; bulk laxatives absorb water thus adding bulk to stool; Lubricants: increase water retention in stool Stimulants: speed up peristalsis Saline laxatives pull water from intestines Osmotic enhance peristalsis and increase distention Stool softeners reduce surface tension of liquids within the bowel Uses Constipation, bowel prep; (psyllium, colace, mag citrate; mineral oil, bisacodyl) Adverse Reactions & Side Effects Cramping, D/N Contraindications Megacolon, abdominal pain, N/V, impaction, GI obstruction or perforation, gastric retention and colitis; Implications Monitor I/O, electrolytes; Slide 71 NM blocking agents ActionsInhibition of nerve impulse transmission UsesThe facilitation of endotracheal intubation and skeletal muscle relaxation (surgery/general) (gallamine, pancuronium) Adverse Reactions & Side EffectsApnea, respiratory depression, bronchospasm, and bradycardia ContraindicationsHypersensitivity; cautious use with collagen, thyroid and cardiac disease, lactation, pregnancy, children < 2; dehydration, electrolyte imbalances and myasthenia gravis ImplicationsMonitor K+ and Mag+; VS q 15 until recovery; I/O; IV doses may be given over 1-2 min Slide 72 NSAIDs ActionsDecreases prostaglandin synthesis UsesMild to moderate pain, arthritis and dysmenorrhea (Ibuprofen, Naproxen) Adverse Reactions & Side EffectsBlood dyscrasias, nephrotoxicity (oliguria, azotemia, hematuria and dysuria) abdominal pain, cholestasis hepatitis, anorexia, dizziness and drowsiness ContraindicationsAsthma, severe liver and/or renal disease, hypersensitivity. Caution in elderly, children, lactation, pregnancy and for patients with GI, cardiac and/or bleeding disorders ImplicationsMonitor renal and hepatic function. Obtain baseline hearing and eye exams; toxicity may include: tinnitus and or blurred vision Slide 73 Opioid analgesics ActionsDepression of the pain impulse transmission at the level of the spinal cord UsesModerate to severe pain (Codeine, fentanyl, morphine, oxycodone) Adverse Reactions & Side EffectsGI (constipation, n/v; anorexia, cramps); sedation, respiratory depression; circulatory depression and increased ICP ContraindicationsUpper airway obstruction, bronchial asthma, addiction, hypersensitivity. Caution with: renal, hepatic, respiratory and cardiac disease ImplicationsMonitor RR; urinary/GI output; LOC; can be used as antiemetic for N/V; continue to monitor/assess for pain Slide 74 Salicylates Actions Antipyretic (inhibits the heat regulation center in the hypothalamus), anti-inflammatory, analgesic (inhibits prostaglandin), Uses Mild to moderate pain, inflammation (arthritis), fever, and thromboembolic disorders (ASA, salsalate) Adverse Reactions & Side Effects Rash, GI symptoms, hepatotoxicity, blood dyscrasias, hearing problems (tinnitus) a sign of possible toxicity Contraindications Hypersensitivity; contraindicated with Vit K deficiency, GI bleed; bleeding disorders; children with Reyes syndrome; caution: Hodgkin's; hepatic/renal failure, anemia Implications Monitor renal/hepatic function; observe for hepatotoxicity (clay colored stools, dark urine, diarrhea, yellow sclera, itching, fever, abd. Pain tinnitus Slide 75 Thrombolytics Actions Convert plasminogen into plasmin to break down the fibrin of clots Uses PE, DV and arterial thrombosis; MI, AV cannula occlusion (Streptokinase, urokinase) Adverse Reactions & Side Effects Anaphylaxis, GI, GU, IC retroperitoneal bleeding; most common are decreased HCT, urticaria, Ha and N Contraindications Hypersensitivity; CNS neoplasms, bleeding, renal or hepatic disease, HTN, COPD, subacute bacterial endocarditis, rheumatic VHD, cerebral embolism or thrombosis or hemorrhage and recent surgery Implications Monitor VS and LOC; monitor bleeding (temp >104); arrhythmias, retro bleed; allergic response; ecchymosis, hematuria, hematemesis, epistaxis; not effective if thrombi are more than 1 wk old. Use 0.8 mm filter with IV administration Slide 76 Thyroid medications ActionsIncrease metabolism, C/O, blood volume, 02 consumption and RR UsesThyroid replacement (thyroid, levothyroxine) Adverse Reactions & Side EffectsPalpitations, tachycardia, insomnia, tremors, angina, #loss, dysrhythmias, thyroid storm ContraindicationsMI, adrenal insufficiency and thyrotoxicosis; caution in elderly, pregnant and lactating moms; DM, HTN, angina and cardiac disease ImplicationsAdminister at same time every day; monitor BP; I/O; #; cardiac status, irritability, excitability and nervousness Slide 77 Vasodilators ActionsVarious decreases vascular resistance and increases blood flow UsesHTN, angina, intermittent claudication, vasospasm, arteriosclerosis Imdur, Ismo (isosorbide mononitrate), Hydralazine, Isosorbide Dinitrate (SR); minoxidil; Nipride, Nitro-bid Adverse Reactions & Side EffectsHypotension, HTN, changes in EKG, Nausea, Ha ContraindicationsTachycardia, acute MI, thyrotoxicosis; PUD, uncompensated heart disease ImplicationsAdminister with meals to reduce GI s/sx; monitor bleeding times and cardiac status Slide 78 SUMMARY The topic of pharmacology is an important one for all involved in the filed of healthcare. Medications have great power to help patients, but can also harm them. Having an understanding of the basics of will allow clinicians to better serve their patients