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week 9
Asthma GI
129
Pharmacology
Graduate
04/04/2013

Additional Pharmacology Flashcards

 


 

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Term
THEOPHYLLINE
Definition
Methylxanthine drug that increase cGMP concentration by inhibiting breakdown, which results in bronchodilation. Effects multiple body systems (CNS-excitation, insomnia; CV-positive chronotropic and iontropic effects; GI-stimulated gastric acid secretion; Renal-weak diureses; Smooth muscle-bronchodilation without tolerance; Skeletal muscle-strengthen contraction (diaphragm-reverse fatigue for COPD patients)). Narrow therapeutic index (10-20 mg/L), so monitoring is important. Many drug-drug interaction as it is metabolized by CYP 450.
Term
Psyllium
Definition
Bulk forming laxative that causes colonic distention and increased peristalsis.
Term
Sucralfate MOA
Definition
Ulcer-adherent complex at the ulcer site, protecting it against further acid attack, forms a viscous, adhesive barrier on the surface of intact mucosa of the stomach and duodenum, also inhibits pepsin activity.
Term
Sucralfate Kinetics & Dosing
Definition
Give on an empty stomach, as drug interferes with food. Excreted feces. Antacids should not be taken within one-half hour before or after administration. Do not take cimetidine, ciprofloxacin, digoxin, norfloxacin, ofloxacin, and ranitidine within 2 h before administration. Dosed 3-4 times a day prior to meals and bed in oral pill or suspension.
Term
Sucralfate Monitoring & ADR
Definition
Signs and symptoms or endoscopic improvement is indicative of efficacy, blood glucose levels in diabetic patients, renal function in elderly patients. Common side effect constipation.
Term
Montelukast
Definition
Type of leukotriene antagonist. Blocks leukotriene D4 receptors to inhibit leukotriene pathway. Block response to exercise and antigen challenge. Minimal side effects.
Term
Montelukast uses
Definition
Been shown to improve asthma control and to reduce the frequency of asthma exacerbations in outpatient clinical trials. Taken orally. Approved for children as young as 6 years of age. Also used in aspirin-induced asthma.
Term
Omeprazole
Definition
MOA: Proton pump inhibitor, binds to H+/K+ exchanging ATPase in gastric parietal cells which blocks acid secretion. Uses: duodenal ulcer, H. Pylori, Gastric ulcer, GERD, Erosive Esophagitis, Hypersecretory condition. ADR: Due to med being metabolized in the liver, patients with impairment need dose adjustments. MANY drug intxns, cough, URI, abd pain, acid regurge, constipation, D/N/V, gas, rash, taste perversion.
Term
Ipatropium
Definition
Muscarinic anatgonist, blocks receptors in bronchi to promote bronchodilation, best results when used in combo with beta-2 adrenergic agonists.
Term
Ipatropium
Definition
approved for bronchospasm associated with COPD but often used for excercise induced or allergen induced asthma. Needs frequent q 4 hour dosing via MDI or TID with neb.
Term
Ipatropium
Definition
ADRs- (Combivent) contraindicated with peanut allergy (soys lethicin, family of peanut, used as carrier). Dry mouth, irritation of the pharynx. Very little to no systemic absorption through the lungs.
Term
Cromolyn
Definition
A mast cell stabilizer given in anticipation of an exposure to an allergen. NOT FOR ACUTE EPISODES. Works on three different pathways: Mast cells-inhibits their early response. Eosinophils-Inhibits inflammation. Airway nerves- Inhibits cough. Cromolyn and other mast cell stabilizers do not cause bronchodilation. Must be administered locally (inhalers, eye drops) as they are insoluble and have no absorption. ADR: cough, airway and nasal irritation, nausea, and unpleasant taste. Needs frequent dosing and monitoring which contributes to a poorer compliance.
Term
Albuterol
Definition
A Beta-2 specific sympatomimetic used in the treatment of asthma. Available as an inhaler and PO. MOA= relaxation of bronchial smooth muscle and inhibition of mast cell mediator release due to stimulation of B2 receptors. Typically used to provide short-term relief in asthma attacks. ADRs= tachycardia, tremors, nervousness.
Term
Ranitidine
Definition
histamine
H2-receptor antagonist that inhibits stomach acid production.
Term
Ranitidine use
Definition
treatment
of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD).
Term
Cromolyn: MOA
Definition
Alters the function of delayed chloride channels, inhibiting inflammatory cell activation. This prophylactically prevents acute
bronchospasm.
Term
Cromolyn: ADR
Definition
Poorly absorbed, resulting in minimal ADRs. Cough, throat irritation, and mouth dryness may occur.
Term
Cromolyn: Clinical Uses
Definition
Prophylaxis for asthma induced by both exercise and antigens (inhaled); other routes useful for ocular, nasal, and GI allergies
Term
Omeprazole MOA
Definition
Irreversible blocking of H+, K+-ATPase inhibitors in actve parietal cells of the stomach, leading to a decrease in gastric secretion of up to 98%
Term
Omeprazole Pharmacokinetics
Definition
administered as an inactive prodrug, to protect the acid labile prodrug from rapid destruction when given orally it is formulated for delayed release as an acid-resistent, enteric coated capsule or tablet; the coating is dissolved after passing through the alkaline intestine lumen and the prodrug is released. It is available as a capsule or in a powder formation
Term
Omeprazole Clinical Uses
Definition
GERD, Peptic Ulcer Disease, treatment of H Pylori associated ulcers, NSAID associated ulcers and prevention of stress related bleeding in critcally ill patients
Term
Omeprazole Adverse Effects
Definition
Very well tolerated. Diarrhea, headache, abdominal pain in 1-5% of patients.
Term
Ipratropium MOA
Definition
competative, nonselective antagonist at M receptors
Term
Ipratropium Clinical Uses
Definition
Inhilation is used for Prevention or relief of acute episodes of bronchospasm. Can be used intranasal which is a local application that inhibits secretions from glands lining the nasal mucosa which decreases rhinorrhea
Term
Ipratropium ADR
Definition
Xerostomia, cough, dizziniess, HA
Term
Bisacodyl
Definition
Treats constipation, a bowel prep, bowel care, is a stimulant laxative that works by stimulating sensory nerve endings to create parasympathetic reflexes producing peristaltic movement of the colon. Evacuation usually occurs 15min to 1 hr with suppository and 6-12 hour with oral dose and is effective in parapalegia and poliomyelitis patients.
Term
Bisacodyl Pharm.
Definition
Bioavailable - do not take within 1 hour of milk ingestion to prevent rapid dissolution of enteric coating, is hydrolyzed to produce laxative effects, excreted in feces
Term
Bisacodyl Adverse Effects
Definition
Abd. cramping, colic, diarrhea with prolonged use that can produce water and potassium loss, rectal irritation, laxative abuse that can create abd. pain, weakness, fatigue, thirst, vomiting, nausea, fluid and electrolyte balance, and edema.
Term
Ranitidine MOA
Definition
H2 receptor antagonist. Competitive inhibition at the parietal H2 receptor and suppresses basal and-stimulated acid secretion. Reduces acid secretion by two mechanisms: 1) Histamine is blocked from binding to the parietal cell H2 receptor. 2) direct stimulation of the parietal cell by gastrin or acetylcholine has a diminished effect on acid secretion in the presence of H2 receptor blockade.
Term
Ranitidine Clinical Uses
Definition
GERD, Peptic Ulcer Disease, Non-Ulcer Dyspepsia, Prevention of bleeding from stress-related gastritis. H2 antagonists are heavily used by the public and continue to be prescribed, but they are becoming less favored than proton pump inhibitors.
Term
Ranitidine ADR
Definition
Extremely safe with ADR occurring in less than 3% of patients and consisting of diarrhea, headache, fatigue, myalgias, and constipation. Mental status changes include: confusion, hallucinations, and agitation.
Term
Psyllium
Definition
Natural plant product that acts as a bulk-forming laxative. It is an indigestible, hydrophilic colloid that absorbs water and forms a bulky, emollient gel that distends the colon and promotes peristalsis
Term
Psyllium adverse effects
Definition
Increased bloating and flatus
Term
Sucralfate MOA
Definition
Sucralfate has a negative charge and it binds to the positively charged proteins at the base of GI ulcers. This forms a barrier, protecting the ulcer and also stimulates mucosal prostaglandin and bicarbonate secretion.
Term
Sucralfate Clinical Uses
Definition
Prevention of GI bleeding in critically ill patients. It is slightly less effective than H2 antagonists and proton pump inhibitors, but does not increase the risk of nosocomial pneumonia.
Term
Sucralfate Adverse Effects
Definition
Constipation in 2% of patients because of aluminum salt. No systemic effects because it is not absorbed.
Term
Sucralfate Drug Interactions
Definition
It can bind to other medications, which impairs their absorption.
Term
Sucralfate Pharm.
Definition
Only small amounts of aluminium salt is absorbed. For this reason prolonged use should be avoided in patients with renal impairment. Most of the medication is not absorbed in the GI tract.
Term
Theophylline MOA
Definition
Methylxanthine; Uncertain of exact MOA. Phosphodiesterase inhibition. Adenosine receptor antagoinst
Term
Theophylline Effects
Definition
Bronchodilation; cardiac stimulation; increased skeletal muscle strength (diaphragm)
Term
Theophylline Clinical Applications
Definition
Asthma; COPD
Term
Theophylline ADR
Definition
Narrow therapeutic window; its therapeutic and toxic effects are related to its blood level; Anorexia; N/V; abd. discomfort; HA; anxiety; seizures; arrhythmias;watch in pts with liver disease since it is metabolized by the liver
Term
Montelukast (Singulair) MOA
Definition
Blocks the leukotriene LTD4 receptors
Term
Montelukast Clinical Use
Definition
Shown to improve asthma control and to reduce the frequency of asthma exacerbations. Approved for use in children as young as 6 years old. Used for aspirin-induced asthma.
Term
Montelukast Effects
Definition
Blocks airway response to exercise and antigen challenge
Term
Montelucast adverse effects
Definition
minimal. Little toxicity. Nausea, diarrhea, abdominal pain, HA, dizziness, neuropsychiatric events. Pregnancy Category Class B
Term
Albuterol
Definition
sympathomimetic-beta specific
Term
Albuterol MOA
Definition
beta 2 receptor agonist that causes relaxation of bronchial smooth muscle resulting in bronchodilation
Term
Albuterol Clinical Use
Definition
Treatment for bronchoconstriction of Asthma, used for acute episodes of bronchospasms, not for prophylaxis
Term
Albuterol Adverse Effects
Definition
skeletal muscle tremors, nervousness, occassional weakness, tachycardia, arrhythmias, and LOC
Term
Cromolyn
(MOA)
Definition
Anti-inflammatory
-Inhibits chloride channels in cell membrane
-prevents mast cell degradation in the lung... which prevents bronchoconstriction
-prevents release of histamine (aka antihistamine)
Term
Cromolyn
(clinical uses)
Definition
Prophylactic treatment of ASTHMA-
-drug is Inhaled
(does NOT work during asthma attack)

Allergic Rhinoconjuctivitis= perennial allergies
-drug is given nasally or via eye drops
(prevents runny nose, itchy, watering eyes)
Term
Cromolyn
(ADR)
Definition
Very little toxicity since drug is very poorly absorbed
(which is why it isn't given orally):

Minor S/E:
-throat irritation
-cough
-dry mouth
-chest tightness/wheezing (rare)

SAFE for use in CHILDREN
Term
Montelukast (MOA)
Definition
Selective and active leukotriene receptor antagonist, binds to cysteinyl leukotrienes (CysLT) type-1 receptors
found in human airway (smooth muscle cells and macrophages),preventing airway edema, smooth muscle contraction and other respiratory
inflammation.
Term
Montelukast (Clinical Uses)
Definition
asthma and exercise induced asthma, seasonal and perennial allergy rhinitis; approved for use in children as young as 6 years old (per Micromedex, other sources stated use in children as young as a year.).
Term
Montelukast (ADR)
Definition
Headache, Allergic granulomatosis angiitis, Stevens-Johnson syndrome, Toxic epidermal necrolysis, Aggressive behavior, Altered behavior, Suicidal thoughts
Term
Ranitidine (MOA)
Definition
Antagonist that competitively blocks the H2 receptor of the parietal cell in the stomach, leading to a decrease in acid production. Used in the treatment of:
-Gastroesophageal Reflux Disease (GERD)
-Peptic Ulcer Disease
-Dyspepsia (non-ulcer)
-Prevention of stress related gastritis
Term
Ranitidine (ADR)
Definition
few ADR, but can include diarrhea, headach, fatigue, myalgias, and constipation. With IV preps can cause mental status changes esp. those that are elderly, or renal or hepatic impairment
Term
psyllium (MOA)
Definition
Bulk forming laxatives made from indigestible parts of fruits, vegetables, and seed
Used to absorb water causing a bulky emollient gel that distends the colon, induces peristalsis, and stimulates evacuation
Term
psyllium (ADR and nursing considerations)
Definition
Increased bloating and flatus. Need adequate amount of water to prevent obstruction.
Term
Sucralfate (Clinical Uses
Definition
Short term treatment of duodenal ulcers
Term
Sucralfate (MOA)
Definition
Negatively charged sucralfate ions bond to high numbers of positively charged protiens of duodenal ulcer craters.
Term
Bisacodyl (MOA)
Definition
Bisacodyl is hydrolyzed to bis(p-hydroxyphenyl)pyridyl-2-methane, which is responsible for its laxative effects.
Term
Bisacodyl (Clinical Use)
Definition
Treatment of acute and chronic constipation. BM within 6-12 hours when given po and 15-60 minutes when given rectally. Available in tablet and suppository.
Term
Bisacodyl (ADR)
Definition
Abdominal discomfort, abdominal cramps or colic, diarrhea, proctitis, atony of colon
Term
Omeprazole (MOA)
Definition
Proton Pump Inhibior that irreversibly blockades the H+, K+ ATPase pump in active parietal cells of the stomach
Term
Omeprazole Clinical Uses
Definition
Peptic ulcer, GERD, erosive gastritis
Term
Omeprazole ADR
Definition
-One daily dose can stope about 98% of daily gastric acid secretion BUT cause GI intolerance due to loss of bacteria barrier
-Reduction of acid can reduce absorption of some drugs and increases others
-Pregnancy category C
Term
Theophylline MOA
Definition
Several proposed but none are firmly established. Possibly PDE inhibitor, possibly inhibits adenosine receptors on the cells surface, and possibly from the enhancement of histone deacetylation. The most directly involved is as a PDE4 inhibitor: In inflammatory cells it reduces the release of cytokines and chemokines which in turn results in a decreased immune cell activation and migration
Term
Theophylline Effects
Definition
Major therapeutic use is the effect on smooth muscle, which causes bronchodilation especially helpful in patients with asthma. CNS: In low and moderate doses causes increased alertness and deferral of fatigue. In higher doses may cause nervousness, insomnia, and bronchodilation in sensitive individuals. CV: Positive chronotropic and inotropic effects (increased rate and force of contraction of hte heart). In low to moderate doses may cause increased cardiac output, tachycardia, increased PVR, slight increase in BP.
Term
Theophylline clinical uses
Definition
Effective bronchodilator; relieves airflow obstruction in acute asthma exacerbations and reduces severity of symptoms in chronic asthma.
Term
Theophylline class
Definition
Methylxanthine: Others in this class include theobromine and caffeine
Term
Theophylline monitoring
Definition
Narrow therapeutic window; plasma concentration goal of 5-20 mg/L associated with an increase in pulmonary function. Routine monitoring of plasma levels ESSENTIAL
Term
Theophyline S/E
Definition
May occur in plasma concntration of 15 mg/L in some patients: Anorexia, nausea, vomiting, abdominal discomfort, headache, anxiety, then seizures or arrhythmias are associated with plasma levels >40 mg/L
Term
Theophylline Toxicity
Definition
Associated with plasma levels >40 mg/L: Tachycardia, tremors, vomiting, hypotension, hypokalemia, hyperglycemia. In severe poisoning (plasma level >100 mg/L seizures often occur and are resistant to anticonvulsants. Hemodialysis indicated in levels >100 mg/L and in patients with lower levels experiencing intractable seizures.
Term
Ipratropium Bromide
Definition
Selective antimuscarinic bronchodilator; derivative of atropine; clinical uses include COPD, nasal discharge, and adjunct therapy to asthma exacerbation; aerosol administration limits systemic anticholinergic activity
Term
Ipratropium bromide drug class
Definition
antimuscarinic (a derivative of atropine)
Term
Which route is ipratropium bromide administered?
Definition
Inhalation (can be given in large doses as is poorly absorbed and does not readily enter the CNS)
Term
Ipratropium bromide drug class
Definition
albuterol (enhances the bronchodilation produced by nebulized albuterol)
Term
Ipratropium bromide MOA
Definition
Competitive antagonist of smooth muscle muscarinic receptors of the PSNS
Term
Clinical effects of Ipratropium bromide (antimuscarinics)
Definition
Prevents cholinergic medicated bronchoconstriction, prevents vagally mediated mucous production
Term
Uses of Ipatropium bromide
Definition
COPD, beta blocker induced bronchospasm
Term
ADR of Ipatropium bromide
Definition
Very few ADR d/t no absorption from the lung and poor CNS entry which minimizes systemic effects
Term
albuterol class
Definition
sympathomimetic bronchodilator; beta-specific agonist; short acting
Term
albuterol : monitor
Definition
respiratory status; BP; CV status; use (more than one Rx fill per month means not controlled)
Term
albuterol
Definition
most widely used sympathomimetics for treatment of bronchoconstriction of asthma
Term
albuterol MOA
Definition
stimulate beta-2 receptors to relax airway smooth muscles; inhibit mediator release; and cause skeletal muscle tremor & tachycardia as s/e
Term
albuterol administration
Definition
best delivered by inhalation (MDI, neb) to gain the greatest local effect on airway smooth muscle with the least systemic toxicity; also available PO & parenteral
Term
albuterol ADR
Definition
sketetal muscle tremor; tachycardia; nervousness; arrhythmias
Term
albuterol clinical uses
Definition
asthma; COPD; drug of choice in acute asthmatic bronchospasm
Term
albuterol kinetics
Definition
short onset, max levels 15-30"; duration 3-4 hrs
Term
albuterol
Definition
use for acute episodes of bronchospasm not for prophylaxis (except exercise-induced asthma, may be useful before exercise to prevent bronchospasm)
Term
levalbuterol
Definition
purified preparation of R-isomer of albuterol, since only the R-isomer activates the beta agonist receptor
Term
albuterol (bronchodilator) emergency asthma action plan
Definition
Instruct all patients with asthma: for a severe attack, take up to four puffs every 20 minutes over 1 hour. If no clear improvement after the first four puffs, take the additional treatments while on the way to an ER.
Term
Psyllium pharmacologic Category
Definition
Bulk-Producing laxative
Term
How should psyllium be administered?
Definition
Drink at least 8 ounces of liquid with each dose. Mix powder in water or juice.
Term
Psyllium Adverse Reactions
Definition
GI-abdominal cramps, constipation, diarrhea, esophageal or bowel obstruction
Term
Psyllium MOA
Definition
Soluble fiber. Absorbs water in the intestine to form a viscous liquid which promote peristalsis and reduces transit time
Term
Sucralfate Class
Definition
Mucosal protective agent
Term
Sucralfate MOA
Definition
Protects gastroduodenal mucosa - a salt of sucrose complexed to sulfated aluminum hydroxide, which in water or acidic solutions forms a viscous, tenatious paste that binds selectively to ulcers or erosions to act as a barrier. The (-) charged sucrose sulfate is believed to bind with (+) charged proteins in the base of ulcers or erosion creating a viscous protective barrier, protecting from caustic damage and stimulating mucosal prostaglandin and bicarbonate secretion.
Term
Sucralfate ADR
Definition
Not signifcantly absorbed, thus no systemic adverse effects. Small amount Aluminum absorbed: Not to be used long-term in those with renal insufficiency. Constipation rare: 2%
Term
Sucralfate - To give or not to give with food
Definition
Give on an empty stomach (1g four times daily).
Term
Sucralfate USE
Definition
Limited to use in ICU settings for critically ill patients as a slurry through NG tube for stress related bleeding.
Term
Cromolyn
Definition
Once a very popular medication used for asthma, it is no longer available in the US
Term
Cromolyn Route of Administration
Definition
Microfine powder or microfine suspension
Term
Cromolyn MOA
Definition
Alters the function of chloride channels and inhibits inflammatory cell activation therefore blocking bronchoconstriction before exposure to allergen that causes asthma symptoms
Term
Cromolyn Clinical Uses
Definition
In addition to being used for asthma, this medication has also been used for allergic rhinoconjunctivis as a nasal spray/eye drops
Term
Cromolyn ADRs
Definition
Minimal ADRs, only localized effects such as dryness or irritation with nasal spray or eye drops
Term
Theophylline MOA
Definition
Methylxanthine drug with MOA: phosphodiesterase inhibition, adenosine receptor agonist. Of note: several mechanisms have been proposed for the actions of methylxanthines, but none have been firmly established.
Term
Theophylline effects
Definition
Bronchodilation, cardiac stimulation, increased skeletal muscle strength (diaphram)
Term
Theophylline applications
Definition
Asthma, COPD
Term
Theophylline ADR
Definition
Insomnia, anorexia, nausea, vomiting, abdominal discomfort, headache & anxiety
Term
Theophylline advantages
Definition
Improves long-term control of asthma, is inexpensive (important advantage for economically disadvantaged patients in societies in which heatlh care resources are limited), and it can be taken orally.
Term
Ranitidine class of drug
Definition
H2 receptor antagonist
Term
Ranitidine clincial use
Definition
GERD, PUD, prevention of bleeding from stress related gastritis
Term
Ranitidine adverse effects
Definition
very minimal, possibly diarrhea, headache, fatigue
Term
Ranitidine's effects on acid secretion
Definition
Marked reduction in nocturnal acid secretion, modest reduction in meal time acid secretion
Term
Omeprazole MOA
Definition
A selective and irreversible proton pump inhibitor. Suppresses gastric acid secretion by antagonism of the H+/K+-ATPase enzyme system on the secretory surface of parietal cells.
Term
Omeprazole- Metabolism
Definition
Hepatic metabolism with extensive first-pass effect. Dose adjustment is recommended for patients with hepatic impairment.
Term
Omeprazole- common adverse effects
Definition
Abdominal pain, nausea, flatulence, vomitting, diarrhea, and headache
Term
Omeprazole- serious side effects
Definition
Stevens-Johnson syndrome, Toxic epidermal necrolysis, C. Diff diarrhea, fracture of bone (hip fracture), rhabdomyolysis, liver failure.
Term
Omeprazole has antimicrobial activity against which organism?
Definition
Helicobacter pylori; via selective inhibition of H. pylori urease, which is necessary for gastric colonization.
Term
Montelukast Classification
Definition
Bronchodilator, Leukotriene Receptor Antagonist
Term
Montelukast MOA
Definition
Inhibits leukotriene formation; leukotrienes exert their effects by increasing neutrophil, eosinophil migration. These actions further lead to bronchoconstriction, inflammation, and edema. This medication blocks the effects of leukotriene's
Term
Montelukast Uses
Definition
Chronic Asthma, seasonal allergic rhinitis, bronchospasm prophylaxis
Term
Montelukast Contraindications
Definition
Class B Pregnancy, alcohol consumption, severe hepatic disease, corticosteroid withdrawal
Term
Montelukast ADR
Definition
Dizziness, fatigue headache, seizures, suicidal ideation, pancreatitis, abdominal pain, influenza, cough, pancreatitis
Term
Montelukast Pharmacokinetics
Definition
Rapidly absorbed; peak 3-4 hours; half life of 2.7-5.5 hours; 99% protein binding; metabolized in the liver and excreted via bile.
Term
Montelukast Interactions
Definition
Commonly used medications: Barbiturates, Carbamazepine, Phenytoin. May increase AST and ALT labratories
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