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Pharmacology Basics Adapted from for Ambercare Corporation Education Department, 2014.

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1 Pharmacology Basics Adapted from for Ambercare Corporation Education Department, 2014

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 OBJECTIVES

3 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 mg of active drug can relieve a headache or ease the inflammation from a strained muscle or tendon in a 185 pound athlete? DID YOU EVER WONDER…?

4 Basic principles of pharmacology includes…
Pharmacokinetic Process: Absorption Distribution Metabolism Excretion Basic principles of pharmacology includes…

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 Patient safety is paramount!

6 Medications are distributed throughout the body by the blood and other fluids of distribution
Once they (the med) arrives at it’s 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 Receptors – function?

7 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 These “peripherally-acting” (act outside of the CNS) analgesics may also decrease the sensitivity of the local pain nerves, causing few pain impulses to be sensed and transmitted to the brain for appreciation. Receptors

8 Receptors Food for thought!
In some instances – a drug’s “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! PPI’s (Protonix) and H2 blockers – are other examples Receptors

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 Receptors – another example

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 Pharmacologist discoveries

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…. Receptors – common drugs

12 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…. NT in the sympathetic system include: Dopamine, NE, Epinephrine (alpha 1,2 and beta 1,2) NT in the parasympathetic system include: acetylcholine (nicotinic and muscarinic) Neurotransmitters

13 Pharmacokinetics – what is it
Pharmacokinetics – what is it? – a branch of pharmacology which deals with determining the movement (kinetics) of drugs into and out of the body Pharmacokinetics - “movement of drug through the body”…. Experimentally, this is done by administering a drug to a group of volunteer subjects or patients and obtaining blood and urine specimens for subsequent quantitative (how much) analysis. When the results of these analyses are plotted on graph paper with blood levels or urinary excretion on the vertical axis and time on the horizontal axis, a blood level-time or urinary excretion patter is obtained. These graphs are utilized to calculate the rates of appearance and elimination of the drug in the bloodstream, the rates of formation of the compounds into which the drugs are transformed in the liver (metabolized) and finally the rates of elimination or excretion of the metabolities – thus ½ life; first-pass effect; excretion times are identified. Pharmacokinetics

14 Four scientific or pharmacokinetic processes…..
Absorption Distribution Metabolism Excretion Four scientific or pharmacokinetic processes….. These four processes occur simultaneously until, first, the entire drug is absorbed from the GI tract, the muscle or subcutaneous tissue site into which it was injected, and there is no more absorption phase; and secondly, all of the drug has been metabolized, and there is no more “parent” drug and it is no longer detectable in the blood.

15 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…. The aqueous humor is a transparent, gelatinous fluid similar to plasma, but containing low protein concentrations. It is secreted from the ciliary epithelium, ... Absorption

16 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 don’t 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) Rate of Absorption -

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.. Rate of Absorption – key factors

18 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 flow…this 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… Distribution

19 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 Many drugs are bound to plasma proteins such as albumin. Why is this factor important? Since only drugs that are NOT bound are FREE to exert a pharmacologic effect – the ratio of “free” to “bound” drug is important in determining the onset and duration of action of drugs. Highly bound drugs are distributed less extensively throughout the body and are slower to act. By virtue of their high binding to plasma proteins, they also stay in the body for longer periods of time because the binding sites act as “reservoir” for the drug, releasing drug molecules more slowly. Example: is commonly used extended release meds such as Effexor XR (an antidepressant med). Most extended release meds will have XR, ER or XL in their name. Distribution effects

20 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 Drugs in the blood and tissues must be inactivated and excreted from the body. This process is initiated by altering the chemical structure of the drug in such a way as to promote its excretion. There are thousands of possible drug to drug and drug to food interactions and many medications and supplements are contraindicated under certain conditions or in patients with specific diseases and disorders. This is why it is imperative that patients keeps their PCP fully informed about all drugs and dietary supplements (including herbal remedies) Metabolism

21 Metabolism – primary site
The primary site of drug metabolism is the liver…plays a major role in digestion, detoxification, and elimination of substances from the body (ponder of this statement for moment…consider disease processes such as ES liver disease – what do you need to consider when administering drugs that are metabolized in the liver)? The family of liver isoenzymes known as cytochrome P-450 are crucial to drug metabolism. These enzymes have a catabolic action on substances, breaking them down into metabolites. Consequently, they also act to lower the concentration of medication in the bloodstream. Drug interactions can occur when one drug inhibits or induces P-450 that acts on another drug. Example: Nicotine, a drug contained in tobacco, is known to induce P-450s. Individuals with liver disease such as cirrhosis may also have insufficient levels of P-450 enzymes. As a result, the concentration of drugs metabolized by these enzymes remains high and can build up to toxic levels in the bloodstream. In addition, certain meds and foods such as grapefruit juice, can inactivate or lessen the metabolic activity of P-450s. Changing the drug dosage can alleviate the problem in some cases Metabolism – primary site

22 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 Metabolism

23 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 Interesting fact: in the case of ethanol, the alcohol molecule is metabolized in the liver by the enzyme alcohol dehydrogenase, to acetaldehyde that causes dilation of the blood vessels and after accumulation is responsible for the subsequent hangover that ensues. Metabolic Rate

24 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… Metabolism

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 Drugs that commonly interact with other meds:

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! Drugs that commonly interact with other meds:

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) Foods and beverages / drug interactions

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) This list is obviously not all-inclusive. Anyone who experiences a serious reaction to a drug that is not consistent with its product labeling should report the event to their doctor and/or MedWatch or FDA Foods and beverages / drug interactions

29 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 patient’s GI tract has been absorbed (consider GI patients who’s absorption rate is impaired via their disease process…) Excretion

30 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 Consider if your patient has kidney disease or ESRD? How will your half-lives be affected? Excretion

31 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 Drug Nomenclature

32 Examples ibuprofen Motrin® acetaminophen Tylenol® benzoyl peroxide
Generic Trade ibuprofen Motrin® acetaminophen Tylenol® benzoyl peroxide Oxy10® Examples

33 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) Drug Classifications

34 Are divided into five schedules based on their potential for abuse and physical and psychological dependence Controlled Meds

35 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) Controlled meds

36 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) Controlled Meds

37 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….let’s review some…. Drug Classifications

38 Alpha-Adrenergic Blockers
Actions They bind to a-adrenergic receptors – leading to dilation of peripheral blood vessels; lowering peripheral resistance and BP Uses HTN, BPH, Raynaud’s – short/long-acting agents –(Cardura, Minipress) Adverse reactions /side effects Hypotension, nasal congestion, tachycardia, diarrhea, N/V Contraindications MI, CAD, including angina Implications K+, Na+, carbon dioxide lab monitoring - daily #’s; intake/output data – orthostatic BP’s Hand-out sympathetic and parasympathic – pictorials Alpha-Adrenergic Blockers

39 Actions Contain magnesium, aluminum, calcium and a combination of these compounds. They slow down the rate of gastric emptying and neutralize gastric acidity Uses Gastritis, peptic ulcer, hiatal hernia and GERD (aluminum carbonate, calcium carbonate – tums) Adverse Reactions & Side Effects Constipation, diarrhea, flatus, abdominal distention, alkaluria Contraindications Allergy and sensitivity Implications Assess epigastric pain, GI symptoms and renal problems and electrolytes Antacids

40 Actions Nitrates – dilate coronary arteries, decrease preload/afterload; CCB – dilate CA, decrease SA/AV node conduction; BB – decrease HR, thus decreasing oxygen use Uses Angina. CCBs, BBs – HTN and dysrhythmias (ol’s, nitro, verapamil) Adverse Reactions & Side Effect Postural Hypotension, fatigue, dysrhythmias, HTN, edema, dizziness Contraindications Increase ICP, cerebral hemorrhage and sensitivity Implications Monitor for SE / Orthostatic BP; assess for angina pain Antianginals

41 Anticholinergics Actions Inhibit acetylcholine (autonomic NS) Uses
Many. 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 Effects Dryness of mouth; paralytic ileus, constipation, urinary retention/hesitancy) dizziness and Ha Contraindications GI or urinary obstruction; narrow-angle glaucoma, and myasthenia gravis Implications Monitor urinary and bowel function as well as vital signs; There are 2 types of anticholinergic: short and long acting; short acting – relieves symptoms (stable - intermittent COPD processes) and long-acting helps prevent breathing problems (COPD patients) whose symptoms are ongoing; Anticholinergic dilate (relax and enlarge) the airways in the lungs (bronchodilator); they also may protect the airway from spasms that can cause bronchospasms – they also reduce mucus production. Anticholinergics are against acetylcholine (parasympathetic system) bringing in the sympathetic system Anticholinergics

42 Anticoagulants Action Prevent clot formation Uses
MI; PE; DVT; DIC; Afib; and HD patients (Coumadin, heparin) Adverse Reactions & Side Effects Hemorrhage, diarrhea, fever, rash and blood disorders (leukopenia, thrombocytopenia) Contraindications Bleeding disorders, such as hemophilia, and leukemia, ulcers, blood dyscrasias, nephritis, endocarditis and thrombocytopenia purpura Implications Observe for bleeding (black stools, ecchymosis); monitor hgb/hct; PT/INR; PTT; vital signs Often called “blood thinners” first line following stroke or MI and PE. They reduce the ability of the blood clot, thereby reducing the likelihood of a coronary, vascular emboli…Afib patients at high risk for micro-emboli to the brain (stroke) from stagnant pooling blood in RA – anticoagulation a must for this patient’s – decrease in CO by 20% with Afib. Anticoagulants

43 Anticonvulsants Actions To prevent seizures Uses
Prevent tonic-clonic seizures, psychomotor seizures, status epilepticus, petit mal and cortical focal seizures (Phenytoin, Diazepam) Adverse reactions & side effects Bone marrow suppression (can be life-threatening) GI problems; CNS effects like confusion, ataxia and slurring of speech Contraindications Allergy or sensitivity to drug class Implications Monitor hepatic and renal function, blood, mental status, blood dyscrasias, and toxicity – especially Stevens-Johnson syndrome Anticonvulsants are drugs that prevent or reduce the severity and frequency of seizures. The different types of anticonvulsants may act on different receptors in the brain and have different modes of action. This classification is further divided into barbiturates, hydantoins, succinimdes, benzodiazepines and others.. Anticonvulsants

44 Antidepressants Actions Uses Adverse Reactions & Side Effects
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 Antidepressants

45 Anti-Diabetic Meds Actions
Lowers blood sugar, K+ and P04; oral med stimulates B-cells of pancreas to release insulin Uses Diabetes and ketoacidosis; (Insulin, Glyburide) Adverse Reactions & Side Effects Hypoglycemia, hepatotoxicity, allergic responses Contraindications Oral agents are contraindicated for juvenile diabetes and ketoacidosis Implications Monitor CBGs; assess for hypoglycemia, rotate insulin injection sites and use human insulin when pork or beef sensitivity Antidiabetic drugs are medicines developed to stabilize and control blood glucose levels among diabetics. Numerous formulations exist, have varying onset of action, peak, duration and ½ life. Anti-Diabetic Meds

46 Antidiarrheal Actions
Varying. Some decrease water content in stool, some slow GI peristalsis Uses Diarrhea; (bismuth, kaolin pectin; loperamide) Adverse Reactions & Side Effects Constipation, paralytic ileus, abdominal pain Contraindications Colitis Implications Used for short term therapy (48 hours or less) monitor electrolytes and bowel response Antidiarrheal, such as Loperamide is also used to reduce the amount of discharge in patients who have undergone ileostomy; also used to treat on-going diarrhea in people with IBD. Antidiarrheal

47 Antidysrhythmics Actions Uses Adverse Reactions and Side Effects
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 Antidysrhythmics are used for the treatment of cardiac dysrhythmias, which is any change from the normal heartbeat rhythm. Includes bradycardia and tachycardia; Antidysrhythmics

48 Antifungals Actions Uses Adverse Reactions & Side Effects
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 Antifungals work by either killing fungal cells (cell wall, causing substance to leak out and die) or prevent the fungal cells from growing and reproducing. Antifungals

49 Antihistamines Actions Antagonists of Histamine Uses
Allergies, pruritus and rhinitis; decrease N/V; (Benadryl, Allegra, Claritin, Alavert, Tavist, Zyrtec, Chlor-trimeton); Adverse Reactions & Side Effects Drowsiness, Ha, urinary retention, blood dyscrasias, thickened bronchial secretions and GI effects Contraindications Sensitivity, asthma, PUD, narrow angle Glaucoma Implications Monitor urinary frequency, respiratory and cardiac status and for blood dyscrasias Come in many forms, including tablets, capsules, liquids, nasal sprays and eye drops; Antihistamines

50 Antihypertensives Actions Uses Adverse Reactions & Side Effects
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 Further divided into: ACE Inhibitors (prils) Beta-Adrenergic Blockers (BB) – ol’s CCB (amlodipine) Centrally acting adrenergics (catapres, clonidine) – inhibits stimulation of the CNS (alpha receptors) Diuretics (loop – furosemide; K+ sparing Aldactone) Peripherally acting antiadrenergics (cardura) Vasodilators (nitro) Antihypertensives

51 Anti-Infectives Actions
Inhibit the growth and/or replication of susceptible bacteria Uses Infection(s) – (PCN, Tetracycline) Adverse Reactions & Side Effects D/N/V, bone marrow depression and anaphylaxis Contraindications Hypersensitivity; most ppl allergic to PCNs are also allergic to cephalosporin's Implications Observe bowel pattern and urinary output. Monitor renal function, blood cultures and for signs of super infection and bleeding; along with WBCs Anti-infective meds are used to treat a wide variety of bacterial infections. They inhibit the growth of bacteria by interfering with the production of certain biochemical necessary to sustain the bacteria’s life or by interfering with the bacteria’s ability to use nutrients.; must be taken a specific time and must complete entire regimen! Broken down further: PCNs Cephalosporin's (ancef, keflex, kefzol) Aminoglycosides (gentamicin, neomycin) Sulfonamides (bactrim, septra) Tetracyclines Monbactam Erythromycins Quinolones (cipro, avelox, levaquin) Anti-Infectives

52 Antineoplastics Actions Uses Adverse Reactions & Side Effects
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 Hodgkin’s 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 Antineoplastics or anticancer drugs prevent or inhibit the maturation and proliferation of neoplasms. The agents (meds) travel the body and destroy cancer cells – both abnormal and normal cells: Divided into: Alkylating agents Antimetabolites Antibiotic agents Hormonal agents others Antineoplastics

53 Antiparkinson Agents Actions
Cholinergic-block acetylcholine receptors (blocks PSS) Uses Parkinson’s Disease (Levodopa) Adverse Reactions & Side Effects Involuntary movement, insomnia, N/V; orthostatic Hypotension; dry mouth; numbness and Ha Contraindications Sensitivity and narrow angle glaucoma Implications Monitor respirations, BP and changes in mentation Relieves Parkinson's symptoms and other forms of parkinsonism. It is a group of disorders that share four main symptoms: tremor or trembling in the hands, legs, jaw and face; stiffness or rigidity of arms, legs, and trunk, slowness of movement (bradykinesia) and poor balance and coordination; Parkinson’s disease is the most common form of parkinsonism; All types of parkinsonism occur when nerve cells in a particular part of the brain die or lose the ability to function. These cells normally produce a chemical called dopamine which helps relay signals to different partos of the brain. This process is important for producing smooth, coordinated movement throughout the body. When dopamine-producing cells are lost, normal movement becomes impossible. Further classified into: Cholinergics and Dopamine antagonists Antiparkinson Agents

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, LFT’s I/O; BP; dizziness; palpations, tachycardia; LOC, gait and sleep patterns These meds have the ability to sedate, tranquilize, blunt emotional expression, attenuate aggressive and impulsive behavior, and cause disinterest in the environment and lack of initiative. Unique features of the drugs are that higher intellectual functions are left relatively intact and yet they act to specifically ameliorate the agitation and bizarre behavior and thinking of psychotic patients. Virtually all have anticholinergic side effects and produce a wide variety of dystonia's and EPS; they can also cause tardive dyskinesia (movement disorder – that is generally irreversible); Subdivided into: Phenothiazine's Thioxanthenes Butyrophenones Dibenzoxazepines Dibenzodiazepines Indolones Antipsychotics / Neuroleptic agents

55 Antituberulars Actions
Decreases the replication of the offending bacillus through the inhibition of RNA or DNA Uses Pulmonary TB (Rifampin, Isoniazid, Rifabutin) Adverse Reactions & Side Effects Anorexia, N/V; rash, renal, hepatic and ototoxic effects Contraindications Sensitivity, renal disease; caution with hepatic disease, pregnancy and lactation Implications Check renal and hepatic status and s/sx of anemia Used in the treatment and prevention of TB; Antituberulars

56 Antitussives and Expectorants
Actions Antitussives – suppression of the cough reflect; Expectorants – decrease in the viscosity of thick, tenacious secretions Uses Cough – bronchitis, TB, pneumonia, CF; COPD; (antitussives are used for non-productive coughs) – Guaifenesin, codeine) Adverse Reactions & Side Effects Dizziness, drowsiness and nausea Contraindications Iodine sensitivity, pregnancy, lactation and hypothyroidism; caution in elderly and asthma patients Implications Monitor cough and sputum, increase fluid intake and humidification to thin secretions Antitussives and Expectorants

57 Actions Interferes with the DNA needed for viral replication Uses HIV, herpes, encephalitis, varicella zoster encephomyelitis, influenza (acyclovir, tamiflu) Adverse Reactions & Side Effects N/V/D/Ha, anorexia, vaginitis, renal failure and metabolic encephalopathy which could be fatal Contraindications Caution in pregnancy and lactation; renal and liver disease and dehydration Implications Assess renal and liver functions; observes for s/sx of infection and allergic reactions (itching, rash, urticaria); monitor for blood dysrasias Blood dysrasias – diseased state of the blood Antivirals

58 Actions Decrease impulse transmission to the cerebral cortex Uses Epilepsy, sedation, insomnia, anesthesia, (phenobarbital and secobarbital) Adverse Reactions & Side Effects Drowsiness, Nausea, blood dyscrasias and Steven-Johnson syndrome Contraindications Allergy, poor liver function, pregnancy (cat D). Caution in elderly Implications Monitor seizure control, BMP, LFTs; observe for toxicity – insomnia, hallucinations, hypotension, pulmonary constrictions, cold clammy skin, cyanosis of lips (circumoral) N/V delirium, weakness) Phenobarbital and Secobarbital are the drugs of choice with Aid to Dying patients, now legal in NM Barbiturates

59 Benzodiazepines Actions Uses Adverse Reactions & Side Effects
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, LFT’s BMP and signs of dependency; administer with milk or food to prevent GI upset All benzos affect gamma-aminobutyric acid (GABA), a NT chemical that nerves use to communicate with one another. Since scientists believe that excessive activity of nerves in the brain may be the cause of anxiety and other psychological disorders, and GABA reduces the activity of nerves in the brain, benzos may be working by increasing the effects of GABA in the brain and spinal cord (CNS). Benzodiazepines

60 Beta-Adrenergic Blockers – BB (ol’s)
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 BB’s are meds that reduce BP. They work by blocking the effects of the hormone epinephrine. BB help blood vessels open up to improve blood flow; Categories: Selective and Nonselective Also come in long and short acting formulas Beta-Adrenergic Blockers – BB (ol’s)

61 Bronchodilators Actions Uses Adverse Reactions & Side Effects
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 Alpha/Beta adrenergic agonists – increase the diameter of nasal passages and relax bronchial smooth muscle B-adrenergic agonists – relax smooth muscle of the bronchi Phosphodiesterase inhibitors – increase smooth muscle relaxation in the respiratory system Bronchodilators

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; 2/3rd 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 Calcium Channel Blockers

63 Cardiac Glycosides Actions Uses Adverse Reactions & Side Effects
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 Cardiac Glycosides

64 Cholinergics Actions Uses Adverse Reactions & Side Effects
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 Cholinergics

65 Cholinergic Blockers Actions Uses Adverse Reactions & Side Effects
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 Cholinergic drugs are any various drugs that inhibit, enhance, or mimic the action of the NT acetylcholine, the primary transmitter of nerve impulses within the parasympathetic nervous system – ANS- that contracts smooth muscles, dilates blood vessels, increases bodily secretions and slows the heart rate. Cholinergic Blockers

66 Corticosteroids Actions Uses Adverse Reactions & Side Effects
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 Corticosteroids

67 Diuretics Actions Uses Adverse Reactions & Side Effects
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 Osmotic diuretics – decrease the absorption of Na+ by increasing osmotic pressure of GFR. K+ sparing diuretics – decrease K+ excretion by interfering with Na+ reabsorption at the distal tubule; Diuretics main action is to rid the body of sodium and water; they work by making the kidneys put more sodium into the urine; the sodium in turn takes water with it from the blood; that decreases the amount of fluid flowing through the blood vessels, which reduces pressure on the walls of the arteries. Classes include: Thiazides and thiazide-like (HCTZ) Loops (Lasix) Carbonic anhydrase inhibitors (Diamox, Azopt) Osmotic diuretics (mannitol) K+ sparing (aldactone) Diuretics

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 H2 blockers work by decreasing the amount of acid produced by the stomach and are available both OTC and with a doctor’s prescription. Histamine H2 Antagonists

69 Immunosuppressant's Actions Inhibits lymphocytes Uses
Prevention of organ transplant rejection; cyclosporine, azathioprine) Adverse Reactions & Side Effects Proteinuria, renal failure, albuminuria, hematuria, hepatotoxicity, oral candida, gum hyperplasia, HA and tremors Contraindications Hypersensitivity; caution in severe hepatic or renal disease and pregnancy Implications Monitor LFTs and BMP, drug blood levels; observe for hepatotoxicity, which can include itching, light colored stools, jaundice and dark urine; administer with meals Immunosuppressant's

70 Laxatives Actions Uses Adverse Reactions & Side Effects
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; Do not administer within one hour of taking an antacid, cimetidine or drinking milk Laxatives

71 NM blocking agents Actions Inhibition of nerve impulse transmission
Uses The facilitation of endotracheal intubation and skeletal muscle relaxation (surgery/general) (gallamine, pancuronium) Adverse Reactions & Side Effects Apnea, respiratory depression, bronchospasm, and bradycardia Contraindications Hypersensitivity; cautious use with collagen, thyroid and cardiac disease, lactation, pregnancy, children < 2; dehydration, electrolyte imbalances and myasthenia gravis Implications Monitor K+ and Mag+; VS q 15’ until recovery; I/O; IV doses may be given over 1-2 min NM blocking agents bind to AcH receptors post-synaptically and inhibit the action of AcH. This blocks NM transmission and causes paralysis of the muscle. NM blocking agents are used as adjunct to anesthesia, only when artificial ventilation is available, to produce muscle relaxation in order to prevent movement of muscle during surgery or for certain critically ill patients; Classifications: Depolarizing blockers AND Nondepolarizing blockers NM blocking agents

72 NSAIDs Actions Decreases prostaglandin synthesis Uses
Mild to moderate pain, arthritis and dysmenorrhea (Ibuprofen, Naproxen) Adverse Reactions & Side Effects Blood dyscrasias, nephrotoxicity (oliguria, azotemia, hematuria and dysuria) abdominal pain, cholestasis hepatitis, anorexia, dizziness and drowsiness Contraindications Asthma, severe liver and/or renal disease, hypersensitivity. Caution in elderly, children, lactation, pregnancy and for patients with GI, cardiac and/or bleeding disorders Implications Monitor renal and hepatic function. Obtain baseline hearing and eye exams; toxicity may include: tinnitus and or blurred vision NSAIDs work by reducing the production of prostaglandins. Prostaglandins are chemicals that promote inflammation, pain, and fever. They also protect the lining of the stomach and intestines from the damaging effects of acid, and promote blood clotting by activating blood platelets. Prostaglandins also affect kidney function. The enzymes that produce prostaglandins are called cyclooxygenase (COX). There are two types (COX-1 and COX-2). Both enzymes produces prostaglandins that promote inflammation, pain and fever; however, only COX-1 produces prostaglandins that activate platelets and protect the stomach and intestinal lining. NSAIDs block COX enzymes and reduce production of prostaglandins. NSAIDs can cause ulcers in the stomach and intestines and increase the risk of bleeding NSAIDs

73 Opioid analgesics Actions
Depression of the pain impulse transmission at the level of the spinal cord Uses Moderate to severe pain (Codeine, fentanyl, morphine, oxycodone) Adverse Reactions & Side Effects GI (constipation, n/v; anorexia, cramps); sedation, respiratory depression; circulatory depression and increased ICP Contraindications Upper airway obstruction, bronchial asthma, addiction, hypersensitivity. Caution with: renal, hepatic, respiratory and cardiac disease Implications Monitor RR; urinary/GI output; LOC; can be used as antiemetic for N/V; continue to monitor/assess for pain Opioid analgesics

74 Salicylates Actions Uses Adverse Reactions & Side Effects
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 Reye’s 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 Salicylates may be used to lessen the change of heart attack, stroke, or other problems that may occur when a blood vessel is blocked by blood clots. Salicylates

75 Thrombolytics Actions Uses Adverse Reactions & Side Effects
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 Dissolve or break up clots (clot busters) Thrombolytics

76 Thyroid medications Actions
Increase metabolism, C/O, blood volume, 02 consumption and RR Uses Thyroid replacement (thyroid, levothyroxine) Adverse Reactions & Side Effects Palpitations, tachycardia, insomnia, tremors, angina, #loss, dysrhythmias, thyroid storm Contraindications MI, adrenal insufficiency and thyrotoxicosis; caution in elderly, pregnant and lactating moms; DM, HTN, angina and cardiac disease Implications Administer at same time every day; monitor BP; I/O; #; cardiac status, irritability, excitability and nervousness Thyroid drugs are thyroid hormones used to treat hypothyroidism. They supplement the natural thyroid hormones in the body. Given for LOW thyroid activity – suppress goiters… Thyroid medications

77 Actions Various – decreases vascular resistance and increases blood flow Uses HTN, angina, intermittent claudication, vasospasm, arteriosclerosis Imdur, Ismo (isosorbide mononitrate), Hydralazine, Isosorbide Dinitrate (SR); minoxidil; Nipride, Nitro-bid Adverse Reactions & Side Effects Hypotension, HTN, changes in EKG, Nausea, Ha Contraindications Tachycardia, acute MI, thyrotoxicosis; PUD, uncompensated heart disease Implications Administer with meals to reduce GI s/sx; monitor bleeding times and cardiac status Vasodilators are agents that widen blood vessels thereby decreasing vascular resistance and increase blood flow. May activate vasomotor center in the brain, relaxing smooth muscle in the blood vessel walls or act locally on blood vessel smooth muscle walls. Short acting and long acting formulations Vasodilators

78 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 SUMMARY

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