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Defense reactions cause tissue injury during conditions of inflammation. Inflammation diminishes at the completion of the healing process. Chemical mediators like histamines and prostaglandins trigger inflammation in response to trauma, toxins, or microbes. Nonsteroidal anti-inflammatory drugs (NSAIDs) have analgesic, anti-inflammatory, and antipyretic effects and are used to treat inflammatory musculoskeletal conditions like rheumatoid arthritis and pain. NSAIDs inhibit cyclooxygenase enzymes and thereby inhibit the synthesis of prostaglandins from arachidonic acid.
Defense reactions cause tissue injury during conditions of inflammation. Inflammation diminishes at the completion of the healing process. Chemical mediators like histamines and prostaglandins trigger inflammation in response to trauma, toxins, or microbes. Nonsteroidal anti-inflammatory drugs (NSAIDs) have analgesic, anti-inflammatory, and antipyretic effects and are used to treat inflammatory musculoskeletal conditions like rheumatoid arthritis and pain. NSAIDs inhibit cyclooxygenase enzymes and thereby inhibit the synthesis of prostaglandins from arachidonic acid.
Defense reactions cause tissue injury during conditions of inflammation. Inflammation diminishes at the completion of the healing process. Chemical mediators like histamines and prostaglandins trigger inflammation in response to trauma, toxins, or microbes. Nonsteroidal anti-inflammatory drugs (NSAIDs) have analgesic, anti-inflammatory, and antipyretic effects and are used to treat inflammatory musculoskeletal conditions like rheumatoid arthritis and pain. NSAIDs inhibit cyclooxygenase enzymes and thereby inhibit the synthesis of prostaglandins from arachidonic acid.
reactions cause tissue injury? Rheumatoid arthritis & asthma What point of the healing process does inflammation diiminish? Completion What can cause inflammation? Trauma, toxic chemicals, & microbial agents Name some chemical mediators that trigger inflammation? Histamines, lipids like prostaglandins & small/ large peptides, interleukin-1, & bradykinin When does rheumatoid arthritis occur? When WBCs attack the synovium and initiate an inflammatory attack What drugs have analgesic, anti-inflammatory & antipyretic effects on the body are used for inflammatory musculoskeletal conditions? NSAIDs COX-2 Inhibitors are used to treat what? Rheumatoid arthritis, osteoarthritis & pain What drug inhibits prostaglandin synthesis in the CNS & has antipyretic & analgesic properties? Acetaminophen What condition is a metabolic disorder characterized by high level of uric acid in the blood? Gout Acute gouty attacks are treated with what? Indomethacin, NSAIDs, glucocorticoids & prophylactic therapy What agents are used in treatment of rheumatoid arthritis & have been shown to slow the course of the disease? Disease-Modifying Anti Rheumatic Name some NSAIDs? Aspirin, Ibuprofen, Indomethacin, nabumetone, Naproxen, Oxaprozin, Celecoxib, Meloxicam & Sumatriptan What's the only NSAID that irreversibly inhibits COX-1 & 2? Aspirin Which drug is used to treat migrain headaches that is a serotonin agonist? Sumatriptan NSAIDs inhibit which set of enzymes that catalyze the first step in prostanoid biosynthesis? Cycloxygenase Prostaglandins are synthesized from what through the cycloxygenase pathway? Arachidonic acid Prostaglandin F2a, leukotrienes and thromboxanes activate what? Phosphatidyl inositol metabolism, causing increase in Ca2+ Adverse effects of aspirin and salicylic acid derivatives? Inc gastric secretion, reduced platelet aggregation, Na+ & H2O retention, which causes edema & hyperkalemia What types of drugs have the same effects as aspirin but with less intense GI effects? Propionic acid derivates like ibuprofen, fenoprofen What NSAIDS are typically not used to reduce fever? Acetic acid derivatives like etodolac, & incomethacin Adverse effects of NSAIDs? GI effects like n & v, ulcers, skin irritations, Na+ & H2O retention leading to edema & hyperkalemia, interstitial nephritis (except aspirin), prolonged bleeding times Which NSAID can cause MI and CVA but has less GI irritation than aspirin? Celecoxib (COX-2 inhibitor) Safest NSAID? Naproxen Which has low cost and long history of safety? Aspirin Which NSAID is very potent & can cause CNS disturbances? Indomethacin Old DMARDs? Methotreate, hydroxychloroquine Newer DMARDs? TNF- inhibitors, leflunomide, &anakinra What's Reye's syndrome? Acute encephalopathy, fat depositions in liver & other visceral organs What drugs treat gout? Allupiinol, probenecid, & colchine Which anti-gout drug inhibits xanthine oxidase activity? Allopurinol Which anti-gout drug decreases the reabsorption of uric acid? Probenecid Which anti-gout drug is anti-inflammatory that decreases leukocyte activity? Colchine NSAIDs inhibit the synthesis of what compound? Prostaglandin When are prostaglandins released? Allergic & inflammatory process What can cause platelet aggregation & smooth muscle contraction? TXA2 (thromboxane A2) What prostaglandins increase intracellular Ca2+? PGE2, PGF2a, leukotrienes thromboxane A2 Actions of prostaglandins? Vasodilation, bronchoconstriction, vessel permeability, enhance pain effects of bradykinin, directly cause pain, induce fever, increase or decrease cAMP Actions of histamines? Increases gap junction space, cause tissue congestion, swelling, bronchoconstriction, causes sneezing, watery eyes, itching, cause pressure & pain Actions of thromboxanes? Cause platelet aggregation, vasoconstriction, smooth muscle contraction, enhance function of inflammatory cells, increase intracellular Ca2+ Actions of leukotrienes? Inc vessel permeability, platelet aggregation, stimulate neutrophils, increase intracellular calcium, causes bronchoconstriction What sensitizes nerves to the action of bradykinin & histamine & causes pain, fever & inflammation? PGE2 What system is not inhibited by NSAIDs but is inhibited by colchine? Lipooxygenase Which joint disorder involves bone ends rubbing together? Osteoarthritis Which joint disorder involves swollen inflamed synovial membrane? Rheumatoid arthritis Arachidonic acid leads to the production of 5-lipoxygenase, cyclooxygenases (COX-1, and COX-2) what two enzymes? What activates the production of Phospholipase A2, which leads to the production of arachidonic acid? Bradykinin & angiotensin What inhibits the production of Phospholipase A2, which leads to the production of arachidonic acid? Corticosteroids What increases protective mucous? PGE2 What is the immediate precursor of leukotrienes? 5-HETE Prostaglandins leads to physiological responses? Platelet aggregation, smooth muscle contraction, and allergic reactions What happens to after prostaglandins bind to G proteins? Formation of diacylglycerol & IP3 is enhanced Uses of aspirin? Prevent heart attacks, arthritis, headache, other pains, & body aches How proinflammatory cytokines lead to RA? Cause inc cellular filtration into endothelium, inc production & release of proteolytic enzymes leading to degradation of cartilage/joint space narrowing, inc osteoclast activity -> bone erosion, demineralization What happens during initiation of pathogenesis of Rheumatoid Synovitis? Vascular injury causes influx of immune cells & plasma causing synoviocyte hyperplasia What happens during immune response of pathogenesis of Rheumatoid Synovitis? Cellular reactivation & proliferation of cytokines e.g Tumor Necrotic factor & interleukines. Neutrophils attracted and activated What happens during inflammation of pathogenesis of Rheumatoid Synovitis? Phagocytosis of immune complex and release of prostaglandins and lysosomal enzymes occur What happens during destruction of pathogenesis of Rheumatoid Synovitis? Collegenase (destroys cartilage); and prostaglandins secreted by synoviocytes What triggers release of COX-2? Oxidative stress, injury, ischemia, seizures & neurodegenerative diseases Name a selective COX-2 inhibitor? Celecoxib COX-2 inhibitors are NOT used for what? Analgesia, like headache, or to decrease platelet aggregation What COX inhibitors cause no gastric damage? COX-2 inhibitors What happens the acetyl group on aspirin? It irreversibly (covalently) inhibits cyclooxygenase. Acetylated cyclooxygenase What decreases synthesis of mucous? PGE2 & PGF2alpha How does the antipyretic action of aspirin work? It causes peripheral vasodilation, therefore, heat dissipation, increases respiration, high doses hyperventilation Side effects of aspirin? Increased gastric acid secretion, decreases mucous protection, therefore causes epigastric distress, ulceration and hemorrhage What increases platelet aggregation? TXA2 What decreases platelet aggregation? PGI2 How does aspirin cause anticoagulation? It decreases TXA2 How can aspirin cause edema & hyperkalemia? It decreases renal flow & increases retention of Na+ & H2O by affecting the actions of PGE2 & PGI2, which maintains renal blood flow Side effect of acetaminophen at high doses? Hepatoxicity How does aspirin affect the synthesis of PGE2 and PGI2? It decreases their synthesis How do NSAIDs affect prostaglandin synthesis? They inhibit prostaglandins that inhibit vasoconstrictors Examples of vasoconstrictors? Angiotensin II, Catecholamines, & Vasopressin What results from aspirin overdose? Vasomotor collapse, coma & dehydration High dose of aspirin causes what? Anti-inflammation, tinnitus, & central hyperventilation How much aspirin is needed to decrease myocardial infarctions? 150-300mg/day How much aspirin is considered low dose? 600 mg/day What's considered high dose of aspirin? 4000 mg/day Low dose aspirin follows what kind of elimination kinetics? 1st order High dose aspirin follows what kind of elimination kinetics? Zero order 1/2 life of low dose (600 mg) aspirin? 3 hrs 1/2 life of high dose (4000 mg) aspirin? 15 hrs Salicylates interact with what drugs to cause a reduced rate of aspirin absorption? Antacids Salicylates interact with what drugs to cause hemorrhage? Heparin or anticoagulants Acetaminophen's action are more prominent where? The CNS In what patients is acetaminophen used to as substitute for aspirin? Patients who have gastric complaints and need antpyretic & analgesic Side effects of therapeutic doses acetaminophen? Skin rash, minor allergic rxns, minor alterations in leukocyte count, renal tubular necrosis, & hypoglycemic coma What used in case of acetaminophen overdose? N-acetylcysteine What causes Reye's syndrome? Aspirin Does acetaminophen cause Reye's syndrome? No Which drug has no anti-inflammatory action? Acetaminophen Acetaminophen has little effect in what region of the body? Peripherally What is contraindicated in gout and why? Aspirin becauses it competes with uric acid Colchine decreases the release of what enzymes? Lipoxygenase, & leukotrienes and other mediators inflammation Allopurinol inhibit what enzyme? Xanthine oxidase Colchine decreases the mobility of what? Neutrophils How does colchine affect cell division of granulocytes? It binds to mitotic spindles and decreases cell division How does colchine affect mobility of neutrophils? It causes depolymerization of microtubular proteins and it binds to tubulin What disorder results from high levels of uric acid in the blood? Gout How does uric acid cause tissue damage? Granolocytes phagocytize the urate crystals which causes oxygen metabolites and lactate in synovial tissues What can aggravate gouty attacks? Purines, excessive alcohol consumption, a rich diet or kidney disease What's used to treat acute gout attacks? NSAIDs besides aspirin, indomethacin, What causes chronic gout? Genetics resulting in increase in the rate of purine synthesis, renal deficiency, Lesch-Nyhan syndrome, or excessive production or uric acid associated with cancer chemotherapy Treatment of chronic gout ? Uricosuric drugs that increase excretion of uric acid, & use of allopurinol Examples of uricosuric agents? Probenacid & Sulfinpyrazone What promotes renal clearance of uric acid by inhibiting the urate-anion exchanger in the proximal tubule? Uricosuric agents What disrupts mobility of granulocytes, and inhibits the synthesis and release of the leukotrienes? Colchine What is effective in the treatment of primary hyperuricemia of gout & hyperuricemia secondary to other conditions? Allopurinol What gout treatment has the side effect of nausea, vomiting, abdominal pain, diarrhea, myopathy, neutropenia, aplastic anemia & alopecia? Colchine What gout treatment has the side effect of skin rashes in ~ 3 % of patients along with nausea & diarrhea? Allopurinol Adverse effect of chronic NSAID use? Analgesic nephropathy What can causes susceptibility to acute renal insufficiency? NSAIDs 2nd most unwanted effects of NSAIDs? Skin reactions like urticaria and Stevens-Johnson syndrome How do gold salts treat gout? They inhibit phagocytosis and lysosomal enzymes What drug is used for arthritis? Infliximab What drug is used for migraine headache? Sumatriptan
Terms Definitions COPD = chronic obstructive pulmonary disease 1. Emphysema 2. Asthma 3. Bronchiectasis 4. chronic bronchitis **COPD = IRREVERSIBLE airway obstruction Emphysema alveolar destruction with airspace enlargement & Airway collapse drugs used: Bronchodilator: theophyline Adrenergic Agonist -combivent - a combination of a B adrenergic agonist + an anticholinergic = a bronchodilatory for the treatment of COPD Atrovent the drug of choice for long term management of COPD causes - Xerostomia Asthma most common respiratory disease - REVERSIBLE airway obstruction - reduced expiratory airflow - clinical signs: wheezing, shortness of breath Asthma is triggered by allergens exercise stress pollution 2nd hand smoke infections Asthma medications 1. corticosteroids - nasonex & flovent HFA & nasacort 2. mast cell stabilizers -cromelyn - Intal 3. anticholinergics -comnivent 4. beta agonists -albuterol 5. xanthines -theophylline 6. leukotriene receptor agonists -Singulair Use of Singulair prevent of asthma; is NOT used for an asthma attack. - psychiatric problems have been reported: agitation, suicide, depression, insomnia & irritability Dental concerns of asthma medications: pulmonary hypertension minimize stress extra steriods What do you do to prevent Acute respiratory failure from asthma? avoid aspirin & NSAIDS and erythromycin keep emergency equipment available Etiology: giving oxygen w/ nitrous oxide or CNS depressant Bronchodilators 1. adrenergic agonists 2. xanthines 3. anticholinergic drugs
**Bronchodilators is REVERSIBLE airway obstruction Adrenergic agonists Ex: proventil HFA/PRO AIR HFA (bronchodilators) -albuterol uses: txt of asthma and COPD Advair Diskus A combination of a B adrenergic agonist + a corticosteroid = improves pulmonary function. Pharmacological effect of Adrenergic agonists drugs stimulate B2 receptor in the lungs...relaxing the smooth muscles Adverse effects of Adrenergic agonists nervousness, tachycardia and insomnia Xanthines (bronchodilators) uses: chronic asthma & COPD -MAJOR drug - caffeine, theophylline Bronchodilators in reversible airway obstruction What is the pharmacological effect of Xanthines? Bronchodilation What are the adverse effects of Xanthines? CNS stimulant Insomnia Nervousness Diuresis (increased secretion of urine) What is a drug interaction of Xanthines? Erythromycin can increase the serum levels of Theophylline and toxicity may result What is the 3rd Bronchodilator? Anticholinergics It is an Ihalation agent for COPD clients & asthmatics who cannot tolerate adrenergic agonists What are the side effects of anticholinergic drugs? They are minimal but include dry mouth What is cromolyn sodium or Intal used for and it's pharmacological effect? It's only effect is to PREVENT asthma...it has NO bronchodilator action. It's pharm. effect is that it prevents release of histamine from sensitized mast cells. What is the least toxic of all Asthma meds? Intal (cromolyn sodium). It's advantage is safety & available in metered doses What are corticosteroid nasal sprays used for? They are used to treat asthmatics who are refractory to (others don't work) asrenergic agonists. CANNOT be used for an asthma attack What is the pharmacological effect of corticosteroid nasal sprays? It's an ANTIINFLAMMATORY nasal spray to increase pulmonary function by a decrease in wheezing, tightness & coughing What are some examples of corticosteroids? Nasacort (triamcinolone) Flovent HFA inhaler (fluticasone) Nasonex (no sig. effects of dental treatment) What are some adverse effects of corticosteroids? Adrenal suppression Poor wound healing Immunosuppression What are clients who use oral corticosteriod inhalers advised to do? Rinse their mouth after using the inhaler to minimize the chance of candidiasis. What are two nasal decongestants or agents for respiratory conditions? Sudafed Allegra D What are the effects and uses of Constrict respiratory mucosa & stimulate B adrenergic receptors nasal decongestants? causing bronchial relaxation. Reduce nasal stuffiness. What is an adverse effect of a nasal decongestants? Pseudoephedrine is a sympathomimetic amine which could interact with epinephrine to cause a pressor response. (use epi with caution) What is an expectorant? They are drugs that promote the REMOVAL & RELEASE of mucus from the respiratory passages EX. Mucinex DM Why is Mucinex different from Mucinex DM The Mucinex DM has dextromethorphan added to control the cough What is a Mucolytics? A drug that DESTROYS OR DISSOLVES mucus. What is an antitussives? An agent which prevents or inhibits coughing like Delsym.
Opiods are most effective BUT are addicting What is the mechanism of action of antitussives? They are chemically related to mrophine but lacking in narcotic properties except for overdose. It controls the cough by depressing the medullary cough center. What is a drug used for smoking cessation? Chantix (varenicline) a patial nicotine agonist due to stimulating dopamine activity to a lesser degree than actual nicotine. Xerostomia is noted
Terms Definitions What are the contraindications for taking Birth Control Pills? Pregnancy Breast feeding if under 6 weeks postpartum HTN 160/100 Vascular disease Heavy smoking over 35 History of DVT, pulmonary embolism, stroke (Multi- Cardio risk factors) Endometrial cancer Ischemic, heart valve defect Breast cancer less than 5 years ago Liver tumors Cirrohosis Active viral hepatitis Diabetic nephropathy, retinopathy, neuropathy Diabetes more than 20 years duration (BCP's increase glucose) Mono-phasic pills Most common Fixed ratio of estrogen and progestin throughout cycle 1 tab daily at the same time 21 and 28 tablets 7 placebo counters Bi-phasic pills Fixed estrogen Progesterone varies which mimics the normal cycle Mini-pills Progestin only birth control pill Alters cervical mucus altering the endometrium to inhibit implantation Designed to reduce circulatroy side effects Increased risk pregnancy and BREAD THRU bleeding If pill taken more than 3 hours late - need back - up contraception for 48 hours. All 28 pills are active. Extended cycle BCP's 4 periods a year May have break through bleeding Always SUNDAY start e.g. Seasonale (Ethinyl Estradiol / Levonorgestrel) Seasonique Continuous dose Lybrel - taken continuously without interruption for withdrawl menses FDA Pregnancy Category A Studies show no fetal risk FDA Pregnancy Category B No fetal risk in animal studies No risk assumed in humans FDA Pregnancy Category C Fetal risk in animal studies weight risk vs. benefit FDA Pregnancy Category D Proven fetal risk weigh risk vs. benefit if life-threatening FDA Pregnancy Category X Proven fetal risk Risk more than benefit - AVOID in pregnancy Teratogenic effects of drugs Teratogen: Substance that causes developmental abnormalities Exposure may result in death of embryo or minor cellular damage without congenital birth defects. Results in malformations exerts effects at a particular stage of fetal development depends on dose Teratogen = Smoking Includes intrauterine growth restriction Still birth - primary and secondary smoke Teratogen - Alcohol Miscarriage Neurocognitive delay in child Teratogen drugs ACE Inhibitors Tetrocyclins Warfarin Androgens - male hormones How to oral contraceptive exert their therapeutic effects? 1. Suppress pituitary secretion of FSH and LF 2. Creates changes in the endometrium to make it less favorable for implantation of fertilized ovum 3. Changes in quantity and viscosity of cervical mucous to make it hostile to sperm. Why are extended BCP's used? The active pill days or hormones in the pills are extended. Inert pills reduced which shortens the period of withdrawl bleeding for patient. The shorter period of hormone free tablets increases the contraceptives efficacy. What are non - contraceptive benefits of BCP's Suppressed pain at ovulation - Mittelschmerz Decreased dysmenorrhea Lighter, shorter menstrual flow Decreased iron deficiency anemia from decreased flow Reduced risk of functional ovarian cysts Protection against benign breast lesions Reduced risk of pelvic inflammatory disease Lower risk of ectoptic pregnancy Decreased menstrual migraines Decreased risk of ovarian and endometrial cancer. What are side effects of BCP's Nausea Weight gain Sore or swollen breasts Spotting btw periods lighter periods mood changes Adverse reactions to BCP's Adverse: Abdominal Pain Chest pain severe headaches Eye problems - blurred vision Swelling and aching in legs and thighs.
Higher doses of estrogen increase the risk for thromboembolism, stroke and MI Low dose combo oral BCP's reduce the risk Two arms of WHI study Estrogen and Progestin HT arm Estrogen only - ET arm Question - to see if either reduced incidence of heart, disease, breast and colorectal cancer and fractures in post-menopausal women - 16000 tested. HT study findings Estrogen and Progestin _ HT E nded after 5.2 years Risks outweighed benefits Increased risk of breast cancer heart attack stroke blood clots Decreased risk for Colon cancer spine and hip fractures ET Study findings Estrogen only Lasted 2 years Did not prevent Cardio vascular disease Increased risk of stroke Did not affect breast cancer risk Lowered risk for hip fracture If had hysterectomy - can't take estrogen alone - increases chance of endometrial cancer. Conclusions of HT and ET study HT increased risk of breast cancer Estrogen alone - DOES NOT increase risk Hormone therapy SHOULD be prescribed for menopausal symptoms SHOULD NOT be prescribed for long term prevention of disease such as CV (increases mortality with MI, stroke and DVT Ostroporosis Nursing implications for BCP's and Drospirenone Drospirenone is the only Progestin derived from Spironolactone (not testosterone) structurally similar to progesterone e.g. Yasmin, Yaz (monophasic - 24 days active) Take serum K levels Contraindications with Drospirenone Use increases serum potassium Contraindicated with kidney, liver or adrenal insufficiency and use of NSAIDS K+ sparing diuretics ACE Inhibitors Angiotensin II anatagonists Heparin ACHES A - Abdominal pain - blood clot in abdomen C = Chest pain - sign of embolism H - Headaches severe- dizziness, weakness, numbness, speech difficulties E - eye disorder - clot behind eye S = severe leg pain or calf swelling = DVT BCP's first time health education Risk Iron anemia Thromboembolism goes up No STD protection PE, MI, CVA and retinol thrombosis is rare To take the pill at the same time everyday and let them know about side effects Risk for uterine, ovarian and endometrial cancer goes UP What are the indications for Anabolic steroids Testosterone derivative INcreases strength and power Creates euphoria and enhanced sexual performance Side effects of anabolic steroids Dramatic increase in weight Body size changes in mood and behavior
Side effects - water retention cardiovascular damage cardiomyopathy stroke hepatic problems lower HDL cholesterol - good fat Physiologic and therapeutic uses of drugs of Erectile Dysfunction Medications Viagra - selective reuptake inhibitor of cGMP in corpus cavernosa (this helps relax smooth muscle which increases vasodilation and increases blood flow) Potentiates hypotensive effects of nitrates so is contraindicated with use of other NITRATES