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Respiratory Pharmacology Week 6

Respiratory Pharmacology Week 6. Inhaled Steroids. Mode of action at the tissue level Restoration of epithelium Reduction of thickening of basement membrane Reduction of mucosal edema Reduction of leukocyte infiltrate Reduction of mast cell number. Inhaled Steroids.

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Respiratory Pharmacology Week 6

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  1. Respiratory PharmacologyWeek 6

  2. Inhaled Steroids • Mode of action at the tissue level • Restoration of epithelium • Reduction of thickening of basement membrane • Reduction of mucosal edema • Reduction of leukocyte infiltrate • Reduction of mast cell number

  3. Inhaled Steroids • Mode of action at the molecular level: • Blockage of active sites of pro-inflammatory genes • Mode of action at the cellular level: • Inhibition of release of pro-inflammatory molecules

  4. Inhaled Corticosteroids • Mode of action • Modify response of the cell in order to inhibit inflammatory response of the airway • May require hours to days to gain full benefits • Daily compliance is essential to maximizing effects

  5. Inhaled Corticosteroids • Indications • Anti-inflammatory maintenance therapy of persistent asthma and COPD • Control of seasonal allergic or non-allergic rhinitis • May be administered as orally inhaled aerosol or intranasal aerosol • http://www.youtube.com/watch?v=LcM7f1iwOGo

  6. Aerobid is now Aerospan Flovent: DPI/MDI. 3 doses. Asmanex: twisthaler, grey or pink depending on dose Qvar: 40/80 ug dose

  7. Advair: MDI or DPI, 3 doses, combo drug Symbicort: 2 doses, combo drug Pulmicort: turbahaler or respules

  8. Inhaled Corticosteroids • Adverse effects • Decrease type and severity of side effects compared to systemic administration • Adrenal insufficiency • Acute asthma

  9. Inhaled Corticosteroids • Adverse effects (systemic mostly) • Osteoporosis • Growth suppression • Oropharyngeal infections

  10. Inhaled Corticosteroids • Adverse effects • Dysphonia • Cough • Bronchoconstriction

  11. Corticosteroids Used in Aerosol Administration

  12. Corticosteroids Used in Aerosol Administration

  13. Corticosteroids Used in Aerosol Administration

  14. Advair • AdvairDiskus combines an inhaled corticosteroid and an inhaled long-acting bronchodilator in one easy-to-use device. AdvairDiskus does not replace fast-acting inhalers for sudden symptoms. AdvairDiskus effectively treats the two main components of asthma at the same time: constriction, the tightening of the muscles around the airways, and inflammation, the swelling and irritation of the airways. Constriction and inflammation cause the airways to narrow and reduce airflow into the lungs, which may result in symptoms such as wheezing, coughing, chest tightness, or shortness of breath. The combination of fluticasone (Flovent-steroid) and salmeterol (Serevent-bronchodilator) is used to prevent wheezing, shortness of breath, and breathing difficulties caused by asthma, but also be prescribed for COPD.

  15. Advair • Generic Name: fluticasone propionate and salmeterolxinafoate • Trade Name: Advair (AdvairDiskus) • How should Advair Asthma Medication be Used?1. OPEN Hold the DISKUS in one hand and put the thumb of your other hand on the thumbgrip. Push your thumb away from you as far as it will go until the mouthpiece appears and snaps into position. 2. CLICK Hold the DISKUS in a level, horizontal position with the mouthpiece towards you. Slide the lever away from you as far as it will go until it clicks. The DISKUS is now ready to use. Every time the lever is pushed back, a dose is ready to be inhaled. This is shown by a decrease in numbers on the dose counter.

  16. Advair • To avoid releasing or wasting doses: • Do not close the DISKUS. • Do not tilt the DISKUS. • Do not play with the lever. • Do not advance the lever more than once. 3. INHALE Before inhaling your dose of AdvairDiskus, breathe out as far as is comfortable, holding the DISKUS level and away from your mouth. Remember, never breathe out into the DISKUS mouthpiece. Put the mouthpiece to your lips. Breathe in quickly and deeply through the AdvairDiskus, not through your nose.

  17. Combos • Symbicort(Contains formoterol, a long-acting beta2-adrenergic agonist (LABA) and budesonide (steroid); given BID, two doses 160/4.5 mcg, 80/4.5 mcg; MDI) • Dulera(mometasonefuroate/ formoterolfumaratedihydrate, BID, 100/5 or 200/5 mcg dose MDI)

  18. Non-Steroidal Anti-Asthma Drugs • Mast cell stabilizers • Indicated for prophylactic control of mild to moderate asthma • Inhibits degranulation of mast cells in response to allergic and non-allergic stimuli • Used typically as alternatives to inhaled corticosteroids, especially in children

  19. Non-Steroidal Anti-Asthma Drugs • Leukotriene inhibitors • Indicated for prophylactic control of mild to moderate asthma • Used in combination with inhaled steroids to reduce the dose of the steroid

  20. Non-Steroidal Anti-Asthma Drugs

  21. Non-Steroidal Anti-Asthma Drugs

  22. Aerosolized Anti-Infective Agents • Pentamidineisethionate (Nebupent) • Indicated for the prevention of Pneumocystis carinii pneumonia (PCP) • Not recommended for use in treatment of PCP (however typically given)

  23. PentamidineIsethionate (Nebupent) • Action: The drug interferes with protozoal nuclear metabolism inhibitionofDNA, RNA, phospholipid and protein synthesis. It is known to have activity against pneumocystis carinii. • Indication: Prevention of Pneumocystis carinii pneumonia (PCP) in high risk, HIV-infected patients. • Dosage: 300mg once every 4 weeks (nebulized)

  24. Pneumocystis pneumonia (PCP) • Pneumocystis pneumonia (PCP) form of pneumonia, caused by the yeast-like fungus (which had previously been erroneously classified as a protozoan) Pneumocystis jirovecii • Pneumocystisis commonly found in the lungs of healthy people, but being a source of opportunistic infection it can cause a lung infection in people with a weak immune system. • Pneumocystis pneumonia is especially seen in people with cancer, HIV/AIDS and the use of medications that affect the immune system. • also known as Pneumocystis jiroveci[i] pneumonia

  25. PentamidineIsethionate • Adverse effects • Cough • Bronchial irritation, bronchospasm • Shortness of breath • Given using a scavenger nebulizer/SPAG

  26. PentamidineIsethionate • Adverse effects • Fatigue • Pharyngitis • Chest Pain

  27. Aerosolized Anti-Infective Agents • Ribavirin (Virazole) • Indicated as anti-viral agent to treat respiratory syncytial virus (RSV) • Administered via small particle aerosol generator (SPAG)

  28. Ribavirin-injection • Ribavirin is also used with an interferon medication to treat hepatitis C in people who have not been treated with an interferon before. • Ribavirin is in a class of antiviral medications called nucleoside analogues. It works by stopping the virus that causes hepatitis C from spreading inside the body. It is not known if treatment that includes ribavirin and another medication cures hepatitis C infection, prevents liver damage that may be caused by hepatitis C, or prevents the spread of hepatitis C to other people.

  29. Ribavirin • Adverse effects • Skin rash • Eyelid erythema • Occlusion of endotracheal tube • Deterioration of pulmonary function

  30. Aerosolized Anti-Infective Agents • Tobramycin (Tobi) • Indicated for management of chronic infection with Pseudomonas aeruginosa; typically seen with CF and immune suppressed patients • Treat or prevent colonization

  31. Tobi • Action: Aminoglycoside antibiotic disrupts protein synthesis eventually resulting in cell death (gram negative organisms). • Dosage: One 5 mL ampule contains 300mg of tobramycin. Given B.I.D. / Q12 with recommended nebulizer (Pari type neb)

  32. Tobramycin • Adverse effects • Ototoxicity and tinnitus • Bronchospasm • Fetal harm (deafness)

  33. Aerosolized Anti-Infective Agents • Zanamivir (Relenza) • Indicated for treatment of uncomplicated illness due to influenza virus

  34. Relenza • used in the treatment and prophylaxis of influenza caused by influenza A virus and influenza B virus. • The bioavailability of zanamivir is 2%. After inhalation, zanamivir is concentrated in the lungs and oropharynx, where up to 15% of the dose is absorbed and excreted in urine. • Dosing is limited to the inhaled route. This restricts its usage, as treating asthmatics could induce bronchospasms

  35. Zanamivir • Adverse effects • Bronchospasm • Under treatment of bacterial infection appearing as viral infection

  36. Aerosolized Anti-Infective Agents • Amphotericin B • Indicated for the treatment of fungal infections, especially in lung transplants

  37. amphotericin B • amphotericin B binds the main component of fungal cell membranes, forming a transmembrane channel that leads to monovalent ion (K+, Na+, H+ and Cl−) leakage, which is the primary effect leading to fungal cell death.

  38. Amphotericin B • Adverse effects • Nausea • Vomiting • Bronchoconstriction

  39. Aerosolized Anti-Infective Agents

  40. Nitric Oxide • Indicated for the treatment of pulmonary hypertension in neonates • Causes relaxation of vascular smooth muscle, producing pulmonary vasodilation

  41. Nitric Oxide • Contraindicated in neonates with right to left shunts

  42. Nitric Oxide • Adverse effects • Hypotension • Formation of Methemoglobinia • Withdrawal

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