Respiratory drugs
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Transcript of Respiratory drugs
RESPIRATORY DRUGS-DR.AKIF A.B
STEP TO PG-MD/MS-DR.AKIF A.B
BRONCHIAL ASTHMABeta 2 agonists Salbutamol, Salmeterol,terbutaline,
formoterol
Anticholinergics Ipratropium, Tiotropium
Methylxanthines Theophylline (Deriphylline)
Corticosteroids
Leukotriene pathway inhibitors Monteleukast, Zafirleukast
Mast cell stabilisers Cromolyn sodium, nedocromil sodium, Ketotifen
Anti Ig E monoclonal antibody Omalizumab
STEP TO PG-MD/MS-DR.AKIF A.B
BRONCHIAL ASTHMA
Histamine
Activates T helper-2 cells to release IL-4
IL-4 induces IgE production by plasma cells
IgE binds to Mast cells
Mast cell degranulation releases
Inflammatory mediators
Arachidonic acid
Allergen
LT-C4/D4/E4
Bronchoconstriction
LOXChronic
InflammationSTEP TO PG-MD/MS-DR.AKIF A.B
RESPIRATORY DRUGS1) Long acting β2 adrenoreceptor agonist: (AIIMS Nov. 2009)
A Salmeterol
B Orciprenaline
C Penoterol
D Pexbaterol
STEP TO PG-MD/MS-DR.AKIF A.B
Ans. A Salmeterol
Salmeterol: It is the long acting selective β2 agonist with a slow onset of action;
used by inhalation on a twice-daily schedule for maintenance therapy and for nocturnal asthma, but not for acute symptoms.
STEP TO PG-MD/MS-DR.AKIF A.B
BRONCHODILATORSBeta 2 Agonists + Beta 2 receptor M3 receptor
Anticholinergics(-)
Increase C-AMP
Decrease Ca++
Increase Ca++
Bronchoconstriction
Bronchodilation
PDE5’AMP
Methylxanthines(-)
STEP TO PG-MD/MS-DR.AKIF A.B
BETA 2 AGONISTSShort acting Beta Agonists(SABA)
Features Long acting Beta Agonists(LABA)
Salbutamol Given by inhalational route
Salmeterol
Terbutaline Given by subcutaneous route
Formoterol
Levalbuterol Most potent SABA
STEP TO PG-MD/MS-DR.AKIF A.B
BETA 2 AGONISTSSIDE EFFECTS
1) Tremors : MC Side effect
2) Hypokalemia
3) Hyperglycemia
4) QT Prolongation
STEP TO PG-MD/MS-DR.AKIF A.B
ANTI CHOLINERGICS1)Ipratropium= Short acting
2) Tiotropium = Longest acting
-Acts by inhibiting M3 receptors
-Bronchodilator of choice in COPD
-Side effects : Dry mouth(MC), Urinary retention
STEP TO PG-MD/MS-DR.AKIF A.B
METHYLXANTHINES-Theophylline
-Inhibits Phophodiesterase 3 and 4 and thus prevents conversion of cAMP to 5’AMP and thus leads to Increase cAMP
-Dose : 8mg/kg for oral route
6mg/kg for I.V route
-Low therapeutic index
-Normal therepautic range : 5-15mg/L
STEP TO PG-MD/MS-DR.AKIF A.B
Thereupatic Drug Monitoring is done
for-Low =Lithium
-Thereupatic =Theophylline
-Index = Immunosuppressants (Cyclosporine and tacrolimus)
-Thereupatic = TCAs
-Drug = Digitalis
-Administration = Aminoglycosides/AntiepilepticsSTEP TO PG-MD/MS-DR.AKIF A.B
METHYLXANTHINES S/E1)Cardiac Arrhythmias (MC)
2)Seizures
3)Hypokalemia
4)Hyperglycemia
STEP TO PG-MD/MS-DR.AKIF A.B
RECENT ADVANCES1) Magnesium is used as bronchodilator since it causes inhibition of calcium transport into smooth muscle cell.
2) Cromakalin is a potassium channel opener under trial for asthma.
3) Aprepitant : It is an NK1 antagonist under trial for treatment for cough associated with Bronchial cancer
4) Baclofen : GABA-B agonist is also known to have Antitussive effect
STEP TO PG-MD/MS-DR.AKIF A.B
2. Which of the following acts as a leukotriene receptor antoagonist? (AIIMS May 2011)
A Zafirlukast
B Zileuton
C Cromolyn sodium
D Deriphylline
STEP TO PG-MD/MS-DR.AKIF A.B
Ans. A Zafirlukast
a. Used for mild to moderate asthma
f. Short duration of action and hepatotoxic potential limit it's use.
STEP TO PG-MD/MS-DR.AKIF A.B
LEUKOTRIENE RECEPTORANTAGONISTS
-Monteleukast
-Zafirlukast
-5-LOX (5 Lipo-oxygenase) inhibitor: Zileuton
-S/E :Churg Strauss Sx
STEP TO PG-MD/MS-DR.AKIF A.B
Zileuton:Lipooxygenase Inhibitor
Leukotriene receptor antagonists
STEP TO PG-MD/MS-DR.AKIF A.B
3. Which one of the following is a side effect of beta2 agonist? (AIIMS May 2010)
A Hypoglycemia
B Hypomagnesemia
C Hypophosphatemia
D Hypokalemia
STEP TO PG-MD/MS-DR.AKIF A.B
Ans. D Hypokalemia Beta2 agonists like salbutamol and terbutaline can cause several adverse effects like :
a. Tachycardia due to stimulation of chronotropic Βeta2 receptors and at high dose due to stimulation of Βeta1 receptors also.
b. Tremors may result due to stimulation of muscle spindles.
c. Tolerance may develop due to densensitization of receptors.
d. Transient hyperkalemia followed by prolonged hypokalemia is seen on continued use.
e. Hyperglycemia may develop due to release of glucagon and stimulation of glycogenolysis and gluconeogenesis.
STEP TO PG-MD/MS-DR.AKIF A.B
BETA 2 AGONISTSSIDE EFFECTS
1) Tremors : MC Side effect
2) Hypokalemia
3) Hyperglycemia
4) QT Prolongation
STEP TO PG-MD/MS-DR.AKIF A.B
4. A predictably dangerous side effect of nadolol that constitutes a contraindication to its clinical use in susceptible patients is the induction of
A Hypertension
B Cardiac arrhythmia
C Asthmatic attacks
D Respiratory depression
STEP TO PG-MD/MS-DR.AKIF A.B
Ans. C Asthmatic attacks
The chief danger of therapy with beta -adrenergic blocking agents, such as nadolol and propranolol, is associated with the blockade itself.
Beta adrenergic blockade results in an increase in airway resistance that can be fatal in asthmatic patients.
Hypersensitivity reactions such as rash, fever, and purpura are rare and necessitate discontinuation of therapy
STEP TO PG-MD/MS-DR.AKIF A.B
SABA (DOC)
Acute attack Persistent Prophylaxis
Asthma
ICS (DOC) LABA (DOC)
Systemic corticosteroids
Oranticholinergics
I.V Aminophylline
Add LABA Cromolyn
NR
NR
NR NR
NR –No ResponseSTEP TO PG-MD/MS-DR.AKIF A.B
CORTICOSTEROIDS-Decreases chronic inflammation by their anti inflammatory effect
-DOC in :1) persistent bronchial asthma
2) Prophylaxis of Exercise Induced Asthma
INHALATIONAL CORTICOSTEROIDS
1) Beclomethasone
2) Ciclesonide
3) Triamcinolone
4) Fluticasone
STEP TO PG-MD/MS-DR.AKIF A.B
CORTICOSTEROIDS-All inhalational corticosteroids except Beclomethasone and Triamcinolone undergoes extensive first pass metabolism and hence produces less systemic toxicity.
-Most potent Inhalational Cortiocosteroid : Fluticasone
-MC S/E of ICS : Hoarseness of voice > Oropharyngeal candidiuasis
Soft Steroids-Prodrugs which are activated by acetylation in Lungs
-E.g: Beclomethasone
- Ciclesonide
STEP TO PG-MD/MS-DR.AKIF A.B
DRUGS FOR PULMONARY HYPERTENSION
Calcium channel blockers
Endothelin antagonists
PGI2 Analogs Phosphodiesterase-5 Inhibitors
Bosentan
Ambrisentan
Epoprostenol
Ileoprost
Teprostinil
Sildenafil
Tadafil
Best antihypertensive for treatment of PAH.
DOC for class II & III PAH (Low Risk)
Best drug for treatment of PAH
-DOC for class IV PAH (High risk)
Sildenafil is the DOC for Erectile Dysfunction
STEP TO PG-MD/MS-DR.AKIF A.B
ANTITUSSIVESCentrally acting drugs
Features Peripherally acting drugs
Features
OpioidsCodeinePholcodeineMorphine methadone
-acts by inhibiting mu receptors
Local anaesthetics
Lidocaine andBupivacaine is used topically
-Mexilitene by oral route
Dextromethorphan
-NMDA receptor Inhibitor- S/E: Hallucination & Addiction
Cromolyn Effective in ACEIs associated cough
Diphenylhydramine
S/E: SedationAnticholinergic effect
Moguistine
Caramiphen
OPIOIDS-Antitussive of choice = Codeine
-Mild to moderate cough = codeine and pholcodeine
-Severe persistent cough of bronchial cancer = Morphine and methadone
-MC S/E : Constipation
STEP TO PG-MD/MS-DR.AKIF A.B
MUCOLYTICS-These liquifies mucus in respiratory tract and facilitates removal.
-Acetylcysteine
-Bromhexine
-Ambroxol
-These 2 drugs acts by breaking the Disulfide bond
STEP TO PG-MD/MS-DR.AKIF A.B
EXPECTORANTS-These are drugs that increase removal of secretion from respiratory tract by due to reflex stimulation caused by Gastric irritation.
- Guaifenesin
STEP TO PG-MD/MS-DR.AKIF A.B
CONDITION DOCAllergic bronchopulmonary aspergillosis
Prednisolone
Cryptogenic organising Pneumonia Prednisolone
Sarcoidosis Prednisolone
Acute attack of asthma SalbutamolProphylaxis of asthma LABAExercise induced asthma Inhalational corticosteroids
Persistent asthma Inhalational corticosteroids
Brittle asthma Epinephrine
DRUG OF CHOICESTEP TO PG-MD/MS-DR.AKIF A.B
CONDITION DOCChylothorax Octreotide via chest tubeCOPD Anticholinergics(Tiotropium)
Non specific Cough CodeineBronchial cancer induced cough Morphine
Pleurodesis DoxycyclinePericardiodesis Doxycycline
Pulmonary edema (Diuretic of choice) Loop diuretics
Class II & III PAH BosentanClass IV PAH Epoprostenol
DRUG OF CHOICESTEP TO PG-MD/MS-DR.AKIF A.B
NEW DRUGSNEW DRUG
Pirfenedone Idiopathic pulmonary fibrosis
Nintedanib Idiopathic pulmonary fibrosis
Umeclidinium COPD
Oladetrol COPD
Ivacaflor Cystic fibrosis
Rufilomilast COPD
STEP TO PG-MD/MS-DR.AKIF A.B
INHALATIONAL DEVICES-Size of Drug particle appropriate for inhalational route is 2-5microns
1) Metered dose inhaler
2) Dry powder inhalers
3) Nebulisers
STEP TO PG-MD/MS-DR.AKIF A.B
METERED DOSE INHALER
STEP TO PG-MD/MS-DR.AKIF A.B
DRY POWDER INHALERS
STEP TO PG-MD/MS-DR.AKIF A.B
NEBULISERS
STEP TO PG-MD/MS-DR.AKIF A.B
STEP TO PG-MD/MS-DR.AKIF A.B
NASAL CANNULA
STEP TO PG-MD/MS-DR.AKIF A.B
SIMPLE OXYGEN MASK
STEP TO PG-MD/MS-DR.AKIF A.B
VENTURI MASK
STEP TO PG-MD/MS-DR.AKIF A.B
NON BREATHING MASK
STEP TO PG-MD/MS-DR.AKIF A.B
FACE TENT
STEP TO PG-MD/MS-DR.AKIF A.B
STEP TO PG-MD/MS-DR.AKIF A.B
STEP TO PG-MD/MS-DR.AKIF A.B