Anti-inflammatory drugs Flashcards
Anti-inflammatory drugs
Mast cell stabilizers
Leukotriene receptor antagonists
Corticosteroids
Prednisone
Mast Cell stabilizers
cromolyn sodium (intal, inhaler), nedocromil (Tilade, inhaler), omalizumab (Xolair, SQ)
Kinetics of Mast Cell stabilizers
Low oral absorption, good resp absorption (inhaler/SQ)
Excreted unchanged in feces
2-4 weeks for therapeutic effect
MOA of Mast Cell stabilizers
Exact mechanisms unknown Inhibits mast cells from rupture Inhibits release of inflammtory mediators from mast cells - histamines and leukotrines Not a bronchodilator Never use as a rescue drug
Cautions with Mast Cell stabilizers
Do not use for acute brochospasm or status asthmaticus - Use only for prophylaxis
CV patienrs
Lactose intolerant patients
Adverse effect with Mast Cell stabilizers
Cough, bad taste, irritation of oropharnx
Headache, dizziness, nausea, rhinitis, eosinophilic pneumonia
Brochospasms (Rebound effect with increase use or abrupt d/c)
Education with Mast Cell stabilizers
Not used for managing acute symptoms - prophylaxis only
Must take daily if have symptoms or not
Take 15-20 min before activity that will induce bronchospasms or exposure to antigens
Leukotreine receptor antagonists
Most effective for long term control of asthma
zafirlukast (Accolate): take orally on empty stomach (best absorption)
montelukast (Singulair): chewable and regular tablets (take at night for best absorption)
zileuton (Zyflo): oral (BID, TID, QID d/t short halflife)
MOA of a Leukotreine receptor antagonists
NOT A BRONCHODILATOR
Zafirlukast and montelukast
- Block receptors for leukotreines bound to amino acid cysteine (Bronchoconstrictor)
zileutron
- inhibit first enzyme in lipoxygense pathway = Decrease production of leukotrienes = decrease inflammation
Cautions with Leukotreine receptor antagonists
Liver disease patients (montelukast is the best choice)
Psych hx
Adverse effects with Leukotreine receptor antagonists
Increased LFT’s (zafirlukast and zileuton), increased psych events (BB warning)
Fever, rash, anaphylaxis, headache, and dizziness (zafirlukast)
Drug interactions with Leukotreine receptor antagonists
zafirlukast
- increased effects of warfarin
- Theophyline and erythromycin decrease levels of zafirlukast
Zileuton
- Increase effects of warfarin, theophylline and propranolol
montelukast
- decreased effectiveness when taken w/ phenobarbital and rifampin
Corticosteroids
last resort tx d/t side effects
flunisolide: MDI
fluticasone: MDI
beclomethasone (Vanceril): MDI and nasal inhaler
prednisone: oral
methylprednisone (Solu-Medrol, Medrol): IV or oral
Kinetics of Corticosteroids
Good absorption thru GI and resp tract Highly protein bound Liver metabolism, some renal clearance Need to be continuously used to maintain effect NOT DILATORS, NOT USED FOR ACUTE ATTACKS
MOA of Corticosteroids
Suppresion of cytokine, leukotriene and prostoglandin production
Suppression of airway eosinophil recruitment
Suppression of release of inflammatory mediators
- All lead to decreased capillary dilation = decreased migration/activation of WBC’s = decreased inflammation
Increases number of beta receptors (Increased sensitivity to beta meds)
Cautions with Corticosteroids
Live vaccine admin d/t immunocompromised Systemic fungal infections HTN DM Osteoporosis Renal insuff Resp tract infections Ocular herpes simplex CHF GI. peptic ulcers
Adverse effects with Corticosteroids
Inhaled - Oral fungal infections (thrush) Oral, laryngeal, pharyngeal irritation - Dry mouth, hoarseness - Resp infections - LT use in kid could delay growth Oral: (w/increased doses of long-term use) - moon face - weight gain - edema (Increased Na and H2O retention) Peptic ulcer (Increase HCl production in stomach) Infections, Hyperglycemia LT use in kids could delay growth Most side effects occur within first 2 weeks but are reversible when d/c'd
Education with Corticosteroids
Good oral hygeine
s/s oropharyngeal candidiasis (Thrush)
rinse mouth after each time to decrease fungal infections
do not abruptly d/c meds - must taper gradually
Prednisone
Used for anti-inflammatory and immunosuppressive effects
Indications for Prednisone
Asthma, allergies, RA, inflammatory bowel disease, skin disorders, tendonitis or bursitis, prevent organ transplant rejection
MOA of Prednisone
Causes Na and H20 retention = edema and HTN
Anti-inflammatory retards leukocyte migration, suppresses tissue repair and decreased c-reactive protein
Does not affect antibody-antigen reactions
Immunosuppressive suppresses phagocytes, decreased eosinophils, lymphocytes, and immunoglobins
Cautions of Prednisone
Systemic fungal infections Administration of live viruses d/t immunocompromised HTN GI disorders DM Osteoporosis Renal insuff
Adverse effects of Prednisone
Anxiety, seizure, insomnia
Glucose intolerance, hyperglycemia, hyperlipidemia
Hirutism, obesisty, amenorrhea
HTN, CHF, pancreatitis
Ulcerative colitis, N/V, peptic ulcer with perforation or hemorrhage
Fluid/lyte imbalance, osteoporosis
Glaucoma, cataracts, acne, stiae
Drug interactions with Prednisone
Azole antifungal (prednisome clearnace possibly decreased) Barbituates Oral anticoagulants Contraceptives Diuretics Salicylates (ASA) Theopylline Warfarin
Education with Prednisone
Do not abruptly stop = adrenal insuff
must be gradually tapered so body can resume secretions of cortisol at normal level and rate
