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Basic Pharmacology Review I. Pharmacokinetics: What the body does to the drug A. Absorption 1. Time the drug enters the body until it gets into the bloodstream 2. Affected by dosage form, route, GI motility B. Distribution 1. Drug distributed to site of action 2. Protein binding 3. Blood brain barrier C. Metabolism 1. Liver 2. Hepatic First Pass Effect 3. Infants and Elderly have a decreased ability to metabolize drugs D. Excretion 1. Drugs eliminated from body primarily by kidneys but also intestines, lungs, and mammary, sweat, and salivary glands 2. Half-life: the time required for total amount of drug to decrease by 50% II. Pharmacodynamics: What the drug does to the body 1. Receptor Interactions Agonist Antagonist 2. Enzyme Interactions 3. Non-specific Interactions III. Major Drug Classification Facts A. Non-Narcotic Analgesics 1. Acetaminophen (Tylenol, APAP) non-narcotic analgesic 2. NOT an NSAID—no anti-inflammatory properties 3. Hepatoxicity with acute OD 4. Antidote for OD: acetylcysteine (Mucomyst) B. NSAIDS (Non-Steroidal Anti-inflammatory Drugs) 1. Drug Profiles Acetylsalicylic Acid (Aspirin, ASA) NSAID Ibuprofen (Motrin, Advil) NSAID 2. Antiplatelet properties with daily dosing: typically 81-325 mg 3. Inhibits prostaglandin synthesis and thromboxane 4. SE: Tinnitus, dizziness, confusion, epistaxis, GI bleeding, bruising, gastritis, N/V, edema C. Narcotic Analgesics 1. Drug Profiles: 2. 3. 4. 5. Morphine Sulfate Meperidine Methadone MOA: Binds to opioid receptors to decrease pain perception SE: Sedation, confusion, euphoria, impaired coordination, urinary retention, constipation, RESPIRATORY DEPRESSION, N/V, pupil constriction, and physical and psychological dependence Nursing Considerations for Narcotic Analgesics Always assess respiratory rate before giving Always assess patient’s pain perception Always evaluate effectiveness of medication Antagonist: naloxone hydrochloride (Narcan) D. CNS agents 1. Barbiturates-barbital MOA: Potentiates GABA Phenobarbital most frequently prescribed 2. Benzodiazepines-lams and pams Suppresses CNS activity Clonazepam (Klonopin) also used as a mood stabilizer 3. Antiepileptics Phenytoin (Dilantin)-Prototype Monitor therapeutic levels 10-20 Must be given IV—only in NS and administered slowly 4. Antiepileptics/Mood Stabilizers Carbamazepine (Tegretol) Valproic Acid (Depakote) Gabapentin (Neurontin) 5. Antipsychotics-azine E. Antidiabetic Agents 1. Drug Profiles: Insulin, Sulfonylureas, Biguanides, Thiazolidinediones, AlphaGlucosidase Inhibitors, Meglitinides 2. MOA: Insulin binds to receptor sites on cells and allows glucose to enter the cell for energy 3. SE: hypoglycemia, know onset, peak and duration, ketoacidosis 4. Nursing Considerations: Roll gently, Rapid first only IV, monitor BS Always listen to patient; errors with this drug can cause death F. Cardiac Glycosides 1. Digoxin (Lanoxin) 2. Used for CHF (Congestive Heart Failure) and/or Atrial fibrillation 3. Positive inotrope, negative chronotrope 4. SE: Anorexia, N/V, visual disturbances, arrhythmias, bradycardia, dig. toxicity with hypokalemia 5. Nursing Considerations: AP 60-100, nl level 0.5-2.0 mg/ml 6. Antidotes: Digoxin Immune Fab (Digibind) G. Beta Blockers – lol, olol 1. MOA: blocks the effects of SNS at beta receptor sites 2. SE: heart block, bradycardia, insomnia, dizziness, drowsiness, hypotension, and rash 3. Nursing Considerations: monitor HR & BP, I & O, and weight 4. Glucagon—antidote for beta-blocker OD 5. Contraindications to Beta-blockers: _______________________________ ____________________________________________________________ H. Sodium Channel Blockers 1. Lidocaine (Xylocaine) 2. SE: Drowsiness, V-tach, heart block, HTN, Bradycardia 3. Nursing Considerations: Monitor ECG I. Calcium Channel Blockers (-dipine) 1. Diltiazem (Cardizem), Verapamil (Calan) 2. SE: hypotension, bradycardia, peripheral edema 3. Nursing Consideration: monitor pulse and BP 4. Antidote: Glucagon J. Nitrates-Vasodilators 1. Nitroglycerin 2. SE: postural hypotension, headache, tachycardia 3. Nursing Considerations: Large first pass effect, teach to take one ¼ grain tablet when chest pain occurs. Lie down and rest. Take 1 tablet every 5 minutes up to 3 tablets. Call 911 if no relief after first tablet K. Centrally Acting Agents1. Binds to alpha 2 receptor sites and decreases outflow of the SNS from the brain. 2. clonidine (Catapres) L. Alpha 1 Blockers (-zosin) 1. Blocks the effects of the SNS by binding to alpha 1 receptor sites 2. Antihypertensive/BPH M. ACE inhibitors (-prils) 1. Inhibits the ACE in the lungs and prevents the formation of angiotensin II, this stops vasoconstriction and aldosterone 2. SE: cough, angioedema, proteinuria, taste changes, orthostatic hypotension, pruritus, renal failure, rash, hyperkalemia N. Angiotensin II Blockers (-sartans) 1. Binds to angiotensin II receptor sites O. Diuretics 1. MOA: Inhibit the reabsorption of Na+ and H2O 2. Nursing Consideration: Monitor K+ 3. Loop Diuretics (-amide)—furosemide (Lasix) 4. Potassium-Sparing diuretics-Spirolactone (Aldactone) 5. Thiazide Diuretics- HCTZ P. Drugs affecting coagulation 1. Anticoagulants Heparin o Monitor PTT o Antidote: Protamine Sulfate Enoxaparin (Lovenox) Warfarin Sodium (Coumadin) o Monitor PT/INR o Antidote: Vitamin K SE: Hemorrhage 2. Antiplatelets-ASA, Dipyridamole (Persantine), Ticlopidine (Ticlid) 3. Antifibrinolytics-Aminocaproic Acid (Amicar) 4. Thrombolytics-Streptokinase (Streptase), Alteplase (Activase) Q. Anti-infectives 1. Culture and Sensitivity: Identifying organisms and the drugs that kill the bugs 2. Normal flora—bacteria, fungi, or protozoa in the oropharynx, upper and lower intestine, lower GU tract, conjunctiva and skin. These microbial agents prevent pathogens from causing infection when normal flora are killed during broad spectrum antibiotic therapy. 3. Superinfection 4. Drug Resistant organisms—MRSA, VRE 5. Antidote for allergic reaction: _________________________ 6. Antibiotics Penicillins (-cillin) Cephalosporins (-Cef) Misc- Vancomycin (Vancocin) Tetracyclines (-cycline) Aminoglycosides-KNOW Nephrotoxicity and Ototoxicity Macrolides (-romycin) Quinolones (-floxacin) Sulfonamides (-Sul) 7. Anti-Tuberculars Isoniazid (INH)- Pyridoxine (Vit B6) to prevent peripheral neuritis Ethambutol (Myambutol), Pyrazinamide, Rifampin, Streptomycin 8. Antiviral Agents Amantadine and rimantadine (Influenza A) Acyclovir (Zovirax) HSV Cidofovir, Ganciclovir, Foscarnet, CMV 9. AIDS NRTI-Zidovudine (AZT) NNRT-Delavirdine, Nevirapine PI- Saquinavir, Ritonavir, Indinavir 10. Antifungal Agents (-azole) Griseofulvin Amphotericin B Diflucan (Fluconazole) Nystatin R. GI Drugs 1. Antacids-neutralizes gastric acid; Mg—diarrhea; avoid in renal pts.; Ca & aluminum—constipation 2. H2 Antagonist (-tidine)—binds to H2 receptor sites to decrease HCL acid production 3. Proton Pump Inhibitors (-prazole)—blocks all HCL acid production 4. Antiflatulents 5. Antidiarrheals—contraindicated in AAC 6. Laxatives—bulk forming are safest and most natural 7. Antiemetics