Drugs for Chronic Obstructive
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Transcript of Drugs for Chronic Obstructive
Drugs for Chronic Obstructive Drugs for Chronic Obstructive Pulmonary DiseasePulmonary Disease
Chronic obstructive Pulmonary disease
Syndromes•Asthma - acute episodes of reversible
bronchoconstriction cause by underlying
airway inflammation.
• Chronic bronchitis- excessive mucus
production due to hyperplasia and hyper
functioning of mucus secreting goblet cells.
• Emphysema - abnormal and permanent
enlargement of respiratory air spaces of their
walls with fibrosis.
Number of non-institutionalized adults who currently have asthma: 15.7 million
· Number of children who currently have asthma: 6.5 million
· Number of hospital emergency department visits: 1.8 million
· Number of deaths: 3,780
Asthma statistics
Genetic predisposition
Airway responsiveness
Asthma symptoms
Airway limitation
Enviromental exposure
Airway inflammation
inhaled allergens are ingested by a type of cell known as antigen presenting cells, or APCs. APCs then "present" pieces of the allergen to other immune system . In
asthmatics, IMMUNE CELLS ARE FORMED -(TH2), The resultant TH2 cells activate the humoral immune system which produces antibodies against the inhaled allergen. Later,
when an asthmatic inhales the same allergen, these antibodies "recognize" it and activate a humoral response. Inflammation results: chemicals are produced that cause
the airways to constrict and release more mucus, and the cell-mediated arm of the immune system is activated.
THE FOLLOWING DRUGS ARE KNOWN TO CAUSE THE FOLLOWING DRUGS ARE KNOWN TO CAUSE REACTION AMONG ASTHMATICS:REACTION AMONG ASTHMATICS:
1.1. ASPIRINASPIRIN aspirin sensitivity – 9 to 44%aspirin sensitivity – 9 to 44%2. NSAIDS2. NSAIDS3. ACETAMINOPHEN3. ACETAMINOPHEN 6 – 8% 6 – 8% 4. BETA-BLOCKERS4. BETA-BLOCKERS Can exacerbateCan exacerbate5. ACE – INHIBITORS5. ACE – INHIBITORS Develop coughDevelop cough
Agents Used to treat Agents Used to treat COPDCOPD
I – Bronchodilators
A. Methylxanthines
B.Adrenergic agonists
(Sympathomimetics)
C. Muscarinic antagonist
(Anticholinergics)
II – Mediator Release Inhibitors
A. Cromolyn Sodium (Intal)
B. Corticosteroids
C. IgE BLOCKER
D. Antieukotriene drugs
A. RELIEVERS
1. SHORT ACTING B2 AGONIST
- SALBUTAMOL
- TERBUTALINE
2. ANTICHOLINERGIC
- IPRATROPUIM
-ATROPINE
B. CONTROLLERS (MAINTENANCE)
1. MEDIATOR RELEASE INHIBITORS
- CROMOLYN
- INHALED GLUCOCORTICOIDS
- LEUKOTRIENE MODIFIERS
- MONTELUKAST
-ZILEUTON
5.ORAL
GLUCOCORTICOSTEROIDS
4. LONG ACTING B2 AGONIST
-SALMETEROL
-FORMETEROL
5. SUSTAINED RELEASE THEOPHYLLINE
DRUGS FOR ASTHMA MANAGEMENT
MethylxanthinesMethylxanthinesDegree of Degree of
BronchodilationsBronchodilations
EnprofyllineEnprofylline ++++ ++++
CaffeineCaffeine ++
TheobromineTheobromine ++
TheophyllineTheophylline +++ +++
(Prototype : Theophylline)(Prototype : Theophylline)
MethylxanthinesMethylxanthines
1. Inhibits cAMP phosphodiesterase which leads 1. Inhibits cAMP phosphodiesterase which leads to to cAMP – smooth muscle relaxation cAMP – smooth muscle relaxation bronchodilation.bronchodilation.
xanthinxanthinee
5’ AMP5’ AMP
Cyclic AMP Cyclic AMP phosphodiesterasephosphodiesterase
Cyclic 3’5 AMP Cyclic 3’5 AMP
Mechanism of action
2. Inhibits the re-uptake of catecholamines 2. Inhibits the re-uptake of catecholamines which can elevate cyclic AMP. Theophylline is an which can elevate cyclic AMP. Theophylline is an adenosine receptor antagonist adenosine receptor antagonist
Membrane Membrane receptorsreceptors
Membrane Membrane receptorsreceptors
Theophylline Theophylline antagonizes antagonizes AdenosineAdenosine
Theophylline Theophylline antagonizes antagonizes AdenosineAdenosine
AdenosineAdenosine(endogenous (endogenous
mediator)mediator)
AdenosineAdenosine(endogenous (endogenous
mediator)mediator)
Pharmacologic Effects:Pharmacologic Effects:A. Respiratory
system1. Rapid relaxation of bronchial sm.
Muscle – bronchodilation
2.Decrease histamine release
3.Stimulate ciliary transport of mucus
4. Improve respiratory performances by
improving contractility of the diaphragm
and by stimulating the medullary
respiratory center.
Pharmacologic Effects:Pharmacologic Effects:B.Effects on other
systems
Caffeine - (+)
1. Heart (+) chronotropic and inotropic effect cardiac stimulation
Theobromine - (++)
Theophylline -
(+++)Enprofylline - (++
++)
Pharmacologic Effects:Pharmacologic Effects:B.Effects on other
systems1. Pulmonary and peripheral vasodilatation ( B.P)
3.Stimulation of gastric acid and pepsinogen release.
2. alertness and cortical arousal medullary stimulation – can cause severe nervousness and seizures.
4. Diuresis
Pharmacokinetics : Prototype drug Pharmacokinetics : Prototype drug TheophyllineTheophylline
• rapidly and completely absorb from GIT
• metabolize in the liver by oxidation and demethylation
• half life – children – 3.5 hrs ; Adult – 8-9 hrsBronchodilator effect is achieve at bld levels of 10-20 mg/ml
(above this is associated with greater toxicity)
* Aminophylline – is a theophylline – ethylene diamine complex
Drug Drug Interactions Interactions
A. Drugs that theophylline effects1. Cimetidine2. Erythromycin , troleandomycin3. Oral contraceptives
B. Drugs that effectiveness of theophylline1. Lithium2. blockers3. Barbiturates4. Beta 5. Phenytoin
HalothaneHalothane - given with theophylline may result - given with theophylline may result to cardiac dysrhythmiasto cardiac dysrhythmias
Adverse EffectsAdverse Effects
1. Vomiting and GI bleeding 2. Cardiac arrhythmais 3. Nervousness , seizures , behavioral problems in children
Clinical Uses1. COPD2.Apnea in pre-term infants
* Initial loading dose – 5mg/kg – by infusion drip over 30 min.* Maintenance- 0.6 to 0.7 mg/kg/h* Pnts with heart or liver disease – 0.3 mg/kg/h
Beta Receptor AgonistBeta Receptor Agonist (Sympathomimetics)(Sympathomimetics)
- relaxes smooth muscle by cAMP as a
result of activation of adenylate cyclase.
cAMP cAMP cAMP cAMP
Activated by Activated by Beta agonistBeta agonist
Activated by Activated by Beta agonistBeta agonist
ATPATPATPATP
Adenylate Adenylate cyclasecyclase
Adenylate Adenylate cyclasecyclase
AgentAgentss 1. Epinephrine- given subcutaneously / 1. Epinephrine- given subcutaneously /
aerosolaerosol2. Ephedrine2. Ephedrine
3. Isoproterenol3. Isoproterenol
4. B4. B22 Selective Selectivea.Metaproterenol (Alupent)a.Metaproterenol (Alupent)b.Terbutaline (Bricanyl)b.Terbutaline (Bricanyl)c.Fenoterol (Berotec)c.Fenoterol (Berotec)d.Pirbuterol d.Pirbuterol e.Procasterol (Meptin)e.Procasterol (Meptin)f.Bambuterol (Bambec)f.Bambuterol (Bambec)g.Salmeterol g.Salmeterol (Serevent) (Serevent)
1. Albuterol1. Albuterol(Ventolin)(Ventolin)
Comparison of Beta – Receptor agonist Comparison of Beta – Receptor agonist on Selectivityon Selectivity
Beta Beta 11
Beta Beta 22
RemarksRemarks
- highly potent - highly potent - orally active- orally active- safe- safe- less cardiac - less cardiac - - stimulationstimulation
++++++++++
2.2.TerbutalineTerbutaline(Bricanyl)(Bricanyl)
- more side - more side - effects than - effects than -- albuterolalbuterol
++++++++
3. Procaterol3. Procaterol (Meptin) (Meptin)
- more potent, - more potent, - more effective - more effective -- than albuterolthan albuterol
++++++++++
4. Fenoterol4. Fenoterol (Berotec) (Berotec)
Comparison of Beta – Receptor agonist Comparison of Beta – Receptor agonist on Selectivityon Selectivity
Beta Beta 11
Beta Beta 22
RemarksRemarks
- - more selective more selective - for lung tissue 2x - for lung tissue 2x - potent than - potent than - albuterol by - albuterol by aerosol aerosol -long acting -long acting
++++++++++
5. Pirbuterol5. Pirbuterol (Exirel) (Exirel)
- - improve cardiac improve cardiac performances performances
- more selective on - more selective on
lung tissuelung tissue
++++++++++
6.Epirephrine6.Epirephrine
-rapid onset more rapid onset more cardiac side cardiac side effects effects activity +++activity +++
++++++++
++++++++
Comparison of Beta – Receptor agonist Comparison of Beta – Receptor agonist on Selectivityon Selectivity
Beta Beta 11
Beta Beta 22
RemarksRemarks
7.Isoproterenol7.Isoproterenol - - cardiac side cardiac side effects effects
++++++++
++++++++
8.Metaproterenol 8.Metaproterenol // Alupent Alupent
-less effective -less effective than albuterolthan albuterol
++++
++++
Long acting beta – receptor agonist , are analogs of albuterol and are long acting(12 hrs) , more affinity to the beta 2 receptor , has slow onset of action .
1. salmeterol
2. formeterol
Adverse Adverse EffectsEffects
1. Cardiac effects – arrhythmias 2.CNS effect – stimulation3.Skeletal muscle tremor
Anticholinergics:Anticholinergics:
Mech. of Action – competitively inhibit the effects of acetylcholine at muscarinic receptors
- block the contraction of airway sm. muscle-block in secretion of mucus in response to vagal activity.- Very effective in achieving bronchodilation in patients with hyperreactive airway disease due to vagal stimulation.
Ipratropium bromide (AtroventIpratropium bromide (Atrovent))
- is a quarternary ammonium deriv of
atropine that is given by aerosol. It does
not cross Bld-Brain barrier and is poorly
absorb from GIT , thus minimizing Anti-
cholinergic side effects.
- useful in chronic bronchitis , emphysema
and in pnts who cannot tolerate Beta
receptors agonist.
Combivent – combination of albuterol + ipratropium bromide
Mediator Release InhibitorsMediator Release Inhibitors : : (MRI)(MRI)
• Cromolyn Na (Intal) – Mech. of action – it
stabilizes Mast cell membranes and prevent
release of mediators in response to various
stimuli.
• It inhibits both early and late Phase rxn to
antigen exposure.
• It inhibit release of histamine & leukotriene Dose – 20 mg inhaled 4x a day
ANTILEUKOTRIENE DRUGS
1. ZAFIRLUEKAST , MONTELEUKAST 1. ZAFIRLUEKAST , MONTELEUKAST (singulair)(singulair)
-are selective reversible inhibitor of the cysteinyl -are selective reversible inhibitor of the cysteinyl leukotriene 1 receptor ,thereby blocking the effects of leukotriene 1 receptor ,thereby blocking the effects of cysteinyl leukotrienescysteinyl leukotrienesdose : ADULT -10mgs , children -5 mgs Once a day at 6 pmdose : ADULT -10mgs , children -5 mgs Once a day at 6 pm
2. ZILEUTON- is a selective and specific inhibitor of 5 2. ZILEUTON- is a selective and specific inhibitor of 5 lipoxygenase ,preventing the formation of LTB4 and the lipoxygenase ,preventing the formation of LTB4 and the cysteinyl leukotrienecysteinyl leukotriene
Adverse effects :Adverse effects :1.1. Elevation of hepatic enzymes Elevation of hepatic enzymes zileuton and zafirlukast are inhibitors of cytochrome P450zileuton and zafirlukast are inhibitors of cytochrome P450 both drugs increases levels of warfarinboth drugs increases levels of warfarin2. Headache and dyspepsia 2. Headache and dyspepsia 3 . Eosinophilic vasculitis ( CHURG- STRAUSS SYNDROME )3 . Eosinophilic vasculitis ( CHURG- STRAUSS SYNDROME )
(SEE FIG 27.6 pg 319 LIPPINCOT )
CorticosteroidsCorticosteroids
MECHANISM OF ACTION:MECHANISM OF ACTION: -REDUCE THE SYNTHESIS OF ARACHIDONIC ACID BY -REDUCE THE SYNTHESIS OF ARACHIDONIC ACID BY
PHOSPHOLIPASE A2 AND INHIBIT THE EXPERSSION OFPHOSPHOLIPASE A2 AND INHIBIT THE EXPERSSION OF CYCLOOXEGENASE 2 ( COX 2)CYCLOOXEGENASE 2 ( COX 2)
- no direct effect on airway - no direct effect on airway -decreases the number and activity of inflammatory cells .-decreases the number and activity of inflammatory cells . Inhaled corticosteroids Inhaled corticosteroids 1.1. BudesonideBudesonide 3. flunisolide 3. flunisolide 2.2. Fluticasone Fluticasone 4. beclomethasone4. beclomethasone
SIDE EFFECTS : CANDIDIASIS ; SORE THROAT SIDE EFFECTS : CANDIDIASIS ; SORE THROAT
Systemic corticosteroidSystemic corticosteroid - prednisone - prednisone -methylprednisone -methylprednisone
Action of steroids on lungs Action of steroids on lungs 1. reduces hyperresposiveness of airways to a 1. reduces hyperresposiveness of airways to a
variety of bronchoconstrictor stimuli ( such as variety of bronchoconstrictor stimuli ( such as allergens , cold air , and exercise ) allergens , cold air , and exercise )
2 . Reverses mucosal edema 2 . Reverses mucosal edema 3. decreases the permeability of capillaries 3. decreases the permeability of capillaries 4. inhibit the release of leukotrienes 4. inhibit the release of leukotrienes
Advantages of using inhaled steroids Advantages of using inhaled steroids 1.1. Better asthma control ( fewer symptoms and Better asthma control ( fewer symptoms and
flare –ups )flare –ups )2.2. Decrease use of beta agonist and systemic Decrease use of beta agonist and systemic
steroids steroids 3.3. Improve lung function Improve lung function 4.4. Reduce the need for hospitalizationReduce the need for hospitalization
Monoclonal antibodies
OMALIZUMAB - - IS A RECOMBINANT DNA – IS A RECOMBINANT DNA – DERIVED MONOCLONAL ANTIBODIES THAT DERIVED MONOCLONAL ANTIBODIES THAT SELECTIVELY BINDS TO HUMAN IgE .SELECTIVELY BINDS TO HUMAN IgE .
- REDUCES BINDING OF IgE TO RECEPTORS IN - REDUCES BINDING OF IgE TO RECEPTORS IN MAST CELLS AND BASOPHILS MAST CELLS AND BASOPHILS
- GIVEN PARENTERALY TWICE WEEKLY - GIVEN PARENTERALY TWICE WEEKLY
EXPOSURE TO ANTIGEN
ANTIGEN AND IgE on MAST CELLS
MEDIATORS
( LEUKOTRIENES , CYTOKINES,etc )
EARLY RESPONSE
BRONCHOCONSTICTIONLATE RESPONSE
INFLAMMATION
ACUTE SYMPTOMS BRONCHIAL HYREPREACTIVITY
AVOIDANCE
CROMOLYN, STEROIDS ZILEUTON
STEROIDS , CROMOLYN,
LEUKOTRIENE
ANTAGONIST BRONCHODILATORS
phrasesphrases
wheezeswheezes
CyanosisCyanosis
More than 45 More than 45 mmHgmmHg
breathless
mild moderate severeRespiratory arrest
Walking, can lie down
talking ,prefers sitting
At rest , hunched forward
talksentences
words
alertness agitated agitated agitated
Use of accessory muscle
none usually
usuallyParadoxical breathing
Moderate ,end expiratory loud loud absent
paO2 Normal Less than 60mmHg
More than 60 mm Hg
paCO2 less than 45 mm Hg
Less than 45 mmHg
More than 45 mm Hg
Severity of asthma exacerbations
More than More than once a week once a week Daily
Nighttime Nighttime symptomsymptom
More than 2x a month
Less than Less than once a week once a week
More than More than once a week once a week
intermittentmild moderate
severe
Exacerbationbrief
Affects daily activity and sleep
Limits activity/ sleep
Daytime symptom
night
Once a week
Daily
Less than 2x a month
PEFR MORE THAN 80%
MORE THAN 80% 60- 80 % LESS
THAN 60%
CLASSIFICATION OF ASTHMA BASED ON SEVERITY
Clinical (Mngt) PharmacologyClinical (Mngt) PharmacologyHome or OPD Mngt of Asthma
A. Mild asthma ( attacks less than 2 per week) – inhaled Beta agonist (e.g albuteral) on an “as needed basis”
1. Acute attacks Inhaled short Beta agonist 3- 4x2.
B. M ILD PERSISTENCE (more than two attacks per week)
Long term control inhaled antiflammatory – Cromolyn or inhaled Corticosteroid – 200 – 400 mcg/day.
May use a combination of inhaled long actging beta 2 agonist + corticosteroid . SERETIDE 250 DISKUS ONCE A DAY
Seretide 250 diskus –contains salmeterol xinafoate Seretide 250 diskus –contains salmeterol xinafoate 50mcgs and fluticasone propionate 250mcgs50mcgs and fluticasone propionate 250mcgs
C. Moderate persistence ( daily attacks , PF =60- 80 % of C. Moderate persistence ( daily attacks , PF =60- 80 % of normal )normal )
1. acute attacks – short acting beta2 agonist 1. acute attacks – short acting beta2 agonist
2. long term control 2. long term control
medium dose corticosteroid 400-800mcgs /day+ long acting medium dose corticosteroid 400-800mcgs /day+ long acting beta2 agonist combination OR beta2 agonist combination OR
Seretide 250 diskus twice a day Seretide 250 diskus twice a day
D. SEVERE PERSISTENCE ( CONTIUOUS ATTACK AND PF of less D. SEVERE PERSISTENCE ( CONTIUOUS ATTACK AND PF of less than 60% of normal )than 60% of normal )
1. acute attacks – short acting beta 2 agonist 1. acute attacks – short acting beta 2 agonist
2. long term control 2. long term control
high dose corticosteroid 800mcg to 1,600 mcg per day high dose corticosteroid 800mcg to 1,600 mcg per day
+ long acting beta2 agonist combination + long acting beta2 agonist combination
Seretide 500 diskus –contains salmeterol xinafoate 50mcgs Seretide 500 diskus –contains salmeterol xinafoate 50mcgs
and fluticasone propionate 500mcgsand fluticasone propionate 500mcgs
3. sustained release theophylline 3. sustained release theophylline
Theophylline should be reserved for patients in whom symptoms remain poorly controlled despite combination treatment.
• If above regimen is not enough to control symptoms – add an oral conticosteroid – PREDNISONE 40-50 mgs /day for 5 days - Or methylprednisolone 16 mgs every other day
Hopitalized patients if :
1. No improvement within 2-6 hrs after corticosteroid treatment
2. High risk patient (hospitalization within one year)
3. Exacerbation is severe
4. There is further deterioration despite all medications
Treatment of STABLE COPD Treatment of STABLE COPD
MILD COPDMILD COPD - SHORT ACTING BRONCHODILATORSHORT ACTING BRONCHODILATOR
MODERATE COPDMODERATE COPD --REGULAR USE OF MORE THAN ONE BRONCHODILATOR REGULAR USE OF MORE THAN ONE BRONCHODILATOR - INHALED GLUCOCORTICOSTEROIDS- INHALED GLUCOCORTICOSTEROIDS
SEVERE COPDSEVERE COPD
-REGULAR USE OF MORE THAN ONE BRONCHODILATOR -REGULAR USE OF MORE THAN ONE BRONCHODILATOR INHALED GLUCOCORTICOSTEROIDS INHALED GLUCOCORTICOSTEROIDS -ANTIBIOTICS-ANTIBIOTICS-LONG TERM OXYGEN THERAPY-LONG TERM OXYGEN THERAPY
Other drugs for COPD
Alpha1 – proteinase inhibitors (Prolastine) –
use to treat emphysema caused by a
deficiency in alpha1 – proteinase a peptide
that inhibits elastase, in patients with the deficiency, elastase destroys lung parenchyma.Other Agents affecting the Respiratory
Tract Drugs Used to treat Rhinitis
1. Antihistaminics (Hi- receptors antagonist)
a. chlorpheniramine
b. diphenhydraminec.loratidine
secretion and parasympathetic activity
Drugs Used to treat Rhinitis (alpha) receptor agonist
A. Nasal aerosols 1.Epinephrine 2.Oxymetazoline 3.Phenylephrine
Constrictdilated arterials in nasal mucosa
3. Topical corticosteroids1 .Beclomethasone (Beconase)2. Fluticasone (Flixotide)3. Flunisolide (Nasalide)
4. Cromolyn Na
B. Administered orally 1.Phenylpropanolamine 2.Pseudoephedrine
3.Xylometazoline 4.Phenylephrine
EXPECTORANTSEXPECTORANTSA.A. VAGAL STIMULANTSVAGAL STIMULANTS
1.1. GLYCERYL GUIACOLATEGLYCERYL GUIACOLATE
2.2. SALT SOLUTIONSSALT SOLUTIONS
B. DIRECT STIMULANTSB. DIRECT STIMULANTS
1. POTASSIUM IODIDE1. POTASSIUM IODIDE
SATURATED SOLUTION (KISS)SATURATED SOLUTION (KISS)
2. BROMHEXINE2. BROMHEXINE
3. CARBOCISTEINE3. CARBOCISTEINE
4. AMBROXOL4. AMBROXOL
ANTITUSIVESANTITUSIVES
I. I. NARCOTIC ANTITUSSIVESNARCOTIC ANTITUSSIVES• HEROIN / MORPHINEHEROIN / MORPHINE• CODEINECODEINE
II. NON-NARCOTIC ANTITUSSIVESII. NON-NARCOTIC ANTITUSSIVES
A. MORPHINAN DERIVATIVES A. MORPHINAN DERIVATIVES
DEXTROMETHORPHANDEXTROMETHORPHAN
B. BENZYLISOQUINOLINESB. BENZYLISOQUINOLINES
NOSCAPINE/ NORCEINENOSCAPINE/ NORCEINE
HYDRASTINE / HOMARYLAMINEHYDRASTINE / HOMARYLAMINE
ANTITUSIVESANTITUSIVES
II. NON-NARCOTIC ANTITUSSIVESII. NON-NARCOTIC ANTITUSSIVESC. DIPHENYLAKYLAMINESC. DIPHENYLAKYLAMINES
CHLOPHENDIANOLCHLOPHENDIANOLLEVOPROPXYPHENELEVOPROPXYPHENE
D. PHENYLCYCLOPENTALKYLAMINESD. PHENYLCYCLOPENTALKYLAMINESCARAMIPHENCARAMIPHENCARBETAPENTANECARBETAPENTANE
E. MISCELLANEOUSE. MISCELLANEOUSBENZONATATEBENZONATATECLOBUTINOLCLOBUTINOLDIBUNATESDIBUNATES
CODEINECODEINE- PHENATHRENE DERIVATIVE OPIATE AGONISTPHENATHRENE DERIVATIVE OPIATE AGONIST- PPC: 1 TO 2 HOURS; DURATION: 4 HRSPPC: 1 TO 2 HOURS; DURATION: 4 HRS
ACTION:ACTION: DIRECT EFFECT ON THE CENTERDIRECT EFFECT ON THE CENTER DRYING EFFECTDRYING EFFECT DECREASE VISCOSITYDECREASE VISCOSITY ANALGESIC & SEDATIVE EFFECTANALGESIC & SEDATIVE EFFECT
ADVERSE EFFECT:ADVERSE EFFECT: NAUSEA & VOMITINGNAUSEA & VOMITING CONSTIPATIONCONSTIPATION DIZZINESSDIZZINESS PRURITUSPRURITUS TOLERANCE & PHYSICAL DEPENDENCETOLERANCE & PHYSICAL DEPENDENCE
DEXTROMETHORPHANDEXTROMETHORPHAN
- METHYL ETHER OR DEXTROROTATORY FORM OF METHYL ETHER OR DEXTROROTATORY FORM OF LEVORPHANOLLEVORPHANOL
- PPC: 15 – 30 MINS; DURATION: 6 - 8 HRSPPC: 15 – 30 MINS; DURATION: 6 - 8 HRS- USEFUL FOR CHRONIC NON-PRODUCTIVE COUGHUSEFUL FOR CHRONIC NON-PRODUCTIVE COUGH
SIDE EFFECTS:SIDE EFFECTS:
* NAUSEA* NAUSEA * DRYING EFFECT* DRYING EFFECT
* DIZZINESS* DIZZINESS
DRUG INTERACTIONS:DRUG INTERACTIONS:
* PENICILLIN* PENICILLIN *TETRACYCLINES*TETRACYCLINES
*SALICYLATES*SALICYLATES * PHENOBARBITAL* PHENOBARBITAL
* KISS* KISS
BROMHEXINEBROMHEXINE- SYSTEMICALLY ACTIVE MUCOLYTIC AGENT- SYSTEMICALLY ACTIVE MUCOLYTIC AGENT
ACTION:ACTION: Depolymerization of MucopolysaccharideDepolymerization of Mucopolysaccharide Direct Effect on Bronchial GlandsDirect Effect on Bronchial Glands Liberation of Lysosomal Enzymes producing cells Liberation of Lysosomal Enzymes producing cells
which digest mucopolysaccharide fiberswhich digest mucopolysaccharide fibers
INDICATIONS:INDICATIONS: ALL forms of TRACHEOBRONCHITISALL forms of TRACHEOBRONCHITIS Emphysema with BronchitisEmphysema with Bronchitis PneumoconiosisPneumoconiosis Chronic Inflammatory Pulmonary ConditionsChronic Inflammatory Pulmonary Conditions Bronchitis with BronchospasmBronchitis with Bronchospasm AsthmaAsthma
BROMHEXINEBROMHEXINE
SIDE EFFECT:SIDE EFFECT:
EPIGASTRIC DISTRESSEPIGASTRIC DISTRESS
DRUG INTERACTIONS: DRUG INTERACTIONS:
INCREASE ANTIBIOTIC INCREASE ANTIBIOTIC CONCENTRATIONCONCENTRATION
AMBROXOLAMBROXOL- MUCOKINETIC & SECRETOLYTIC- MUCOKINETIC & SECRETOLYTIC
ACTION:ACTION: INCREASE RESP. TRACT SECRETIONSINCREASE RESP. TRACT SECRETIONSENHANCE PULM. SURFACTANT ENHANCE PULM. SURFACTANT
PRODUCTIONPRODUCTIONSTIMULATES CILIA ACTIVITYSTIMULATES CILIA ACTIVITY
IMPROVED MUCUS FLOW & TRANSPORTIMPROVED MUCUS FLOW & TRANSPORT
(CILIARY CLEARANCE FACILITATES (CILIARY CLEARANCE FACILITATES EXPECTORATION)EXPECTORATION)
AMBROXOLAMBROXOLUSE:USE: SECRETOLYTIC THERAPHY IN ACUTE SECRETOLYTIC THERAPHY IN ACUTE
& CHRONIC BRONCHO-PULMONARY & CHRONIC BRONCHO-PULMONARY DISEASES ASSTD WITH ABNORMAL DISEASES ASSTD WITH ABNORMAL SECRETIONS & IMPAIRED MUCUS SECRETIONS & IMPAIRED MUCUS TRANSPORT.TRANSPORT.
SIDE EFFECT:SIDE EFFECT: NAUSEA & VOMITINGNAUSEA & VOMITINGRASHESRASHESCAN INCREASE ANTIBIOTIC CONC.CAN INCREASE ANTIBIOTIC CONC.
CARBOCISTEINECARBOCISTEINE(S-CARBOXYMETHYLCYSTEINE)(S-CARBOXYMETHYLCYSTEINE)
- MUCOREGULATOR IN RESP. TRACT MUCOREGULATOR IN RESP. TRACT DISORDERS CHARS BY EXCESSIVE OR DISORDERS CHARS BY EXCESSIVE OR VISCOUS MUCUSVISCOUS MUCUS
- ACT BY REGULATING AND ACT BY REGULATING AND NORMALIZING THE VISCOSITY OF NORMALIZING THE VISCOSITY OF SECRETION FROM THE MUCUS CELLS SECRETION FROM THE MUCUS CELLS OF RESP. TRACTOF RESP. TRACT
- STIMULATES THE LESS VISCOUC STIMULATES THE LESS VISCOUC SIALOGLYCOPEPTIDES AND SIALOGLYCOPEPTIDES AND SULFOGLYCOPEPTIDESSULFOGLYCOPEPTIDES
CARBOCISTEINECARBOCISTEINE
- STIMULATES THE LESS VISCOUS NEUTRAL STIMULATES THE LESS VISCOUS NEUTRAL GLUCOPEPTIDES DUE TO ACTIVATION OF GLUCOPEPTIDES DUE TO ACTIVATION OF SIALYLTRANSFERASE OR INHIBITON OF SIALYLTRANSFERASE OR INHIBITON OF NEURAMIDASENEURAMIDASE
- DECREASE THE SIZE AND NUMBER OF DECREASE THE SIZE AND NUMBER OF MUCUS PRODUCING CELLS.MUCUS PRODUCING CELLS.
SIDE EFFECTSIDE EFFECT::
GIT BLEEDING, NAUSEA, DIARRHEA, RASH, GIT BLEEDING, NAUSEA, DIARRHEA, RASH, DIZZINESS, HEADACHE, PALPITATIONSDIZZINESS, HEADACHE, PALPITATIONS
MUCOLYTIC AGENTSMUCOLYTIC AGENTSACETYLCYSTEINE: (MUCOMYST)ACETYLCYSTEINE: (MUCOMYST) REDUCES THE THICKNESS & STICKINESS OF REDUCES THE THICKNESS & STICKINESS OF
PURULENT & NONPURULENT PULMONARY PURULENT & NONPURULENT PULMONARY SECRETIONSSECRETIONS
BREAKS DISULFIDE LINDAGES OR BONDS OF BREAKS DISULFIDE LINDAGES OR BONDS OF MUCOPROTEIN MOLECULES OF RESP. MUCOPROTEIN MOLECULES OF RESP. SECRETIONS INTO SMALLER, MORE SOLUBLE SECRETIONS INTO SMALLER, MORE SOLUBLE & LESS VISCOUS STRANDS& LESS VISCOUS STRANDS
ANTIDOTE FOR PARACETAMOL POISONING ANTIDOTE FOR PARACETAMOL POISONING
MUCOLYTIC AGENTSMUCOLYTIC AGENTSACETYLCYSTEINE (con’t..)ACETYLCYSTEINE (con’t..) BRONCHOPULMONARY DSES.BRONCHOPULMONARY DSES.
i.e. CYSTIC FIBROSISi.e. CYSTIC FIBROSIS DXs AID IN BRONCHIAL STUDIESDXs AID IN BRONCHIAL STUDIES
(bronchospirometry/ bronchograms)(bronchospirometry/ bronchograms)GIVEN: GIVEN:
INHALATION/ INSTILLATIONINHALATION/ INSTILLATIONADVERSE EFFECTS:ADVERSE EFFECTS:
Hemoptysis, resp. irritation & difficultyHemoptysis, resp. irritation & difficultyN & V, inc temp, throat irritationN & V, inc temp, throat irritation
Clinical case scenario
Two year ago , a 31 year old female came to your clinic complaining of paroxysmal cough accommpanied by chest tightness and shortness of breath . This occur when her family moved into a new house 4 weeks PTC. This happened 2-3 x per week and affected her sleep .