Professional Documents
Culture Documents
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Learning Objectives
Mucoactiveagents
Cough suppressants
(antitussives)
Bronchodilator
Tuberculosis drugs
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Types of cough
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The physiology of mucus and sputum
production in the respiratory system
cilia trap large pieces of debris and waft them out of the airways
This results in the urge to cough and expectorate this mucus as sputum. Sputum
expectoration is not normal and there is always an underlying pathological cause.
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SPUTUM PRODUCTION
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SPUTUM PRODUCTION
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Mucoactive agents
Expectorants Mucolytic or
mucoregulators mucokinetics
Carbocysteine :
antioxidant classic mucolytics
restore the depolymerise mucin
viscoelastic glycoproteins
properties of mucous
peptides mucolytics
:depolymerise DNA
and F-actin polymer
networks
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Classic mucolytics
has significant
The prototype antioxidant
antioxidant
agent : N- and anti-
and anti-
acetyl cysteine inflammatory
inflammatory
(NAC) properties
properties.
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N-acetyl cysteine (NAC)
as an aerosol
dissociates
mucin
disulphide
bonds and can also
NAC decreased
other protect against
airway
disulphide free radical
inflammation
bond crossed damage
linked gel
component to
reduce
viscosity
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NAC decreased airway inflammation
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N-acetyl cysteine (NAC)
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N-acetyl cysteine (NAC)
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N-acetyl cysteine (NAC)
Rapidly
Deacetylated
absorbed into
and
various
metabolized in
tissues
the intestines
following an
and liver
oral dose
Peak plasma
Its levels:
metabolites approx.1 hour
incorporated after an oral
into proteins dose.
and peptides Biovailability
only 4-10%
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N-acetyl cysteine (NAC)
Side effects :
GIT irritation (oral)
Burning sensation in airways
(inhalation)
Bronchospasm (inhalation)
Sulphorous taste & odor (inhalation)
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N-acetyl cysteine (NAC)
NAC inhibits
cytotoxicity of
NAC might
Warning and the cancer
reduce thc
chemotherapy
Contraindicati drug cisplatin
action of
ons: doxorubicine
(Roller et al.,
antineoplastic
1998; Miyajima
et al., 1999)
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Other Mucolytics (Classic )
Erdosteine and fudosteine :
Erdosteine :
an antioxidant with mucolytic properties and
also reduces bacterial adhesiveness
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Other Mucolytics (Classic )
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Peptide Mucolytic
Dornase alpha :
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PULMOZYME
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Current Recommendations for Clinical
Use of Mucolytic Drugs
Hypertonic Saline :
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Current Recommendations for Clinical
Use of Mucolytic Drugs
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GG
Mekanisme kerjanya
GG memiliki aktivitas sebagai ekspektoran dengan
meningkatkan volume dan mengurangi kekentalan
sputum yang terdapat di trakhea dan bronki. Dapat
meningkatkan reflek batuk dan memudahkan untuk
membuang sputum.
Akan tetapi bukti objektif masih sedikit.
Dose : Oral 200400 mg/4 hours, max dose
2400 mg/d
adult : 3 x12 tab
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Mucokinetics
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Mucokinetics
salmeterol could restore secretory
functions in CF airway sub-mucosal
glands serous cells
Bronchodilators
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Mucokinetics
Ambroxol
Dosis:
Dewasa: sehari 3 kali 1 tablet.
Anak-anak 5 - 12 tahun : sehari 3
kali 1/2 tablet.
Anak-anak 2 - 5 tahun : sehari 3
kali 7,5 mg
Anak-anak di bawah 2 tahun :
sehari 2 kali 7,5 mg
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Mucoactive drugs and their potential
mechanisms of action
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Carbosystein:
Nama dagang di Indonesia: Rhinathiol
Bentuk sediaan:
Capsul 375 mg
Adult syr 250 mg/5 mL
Infants syr 100 mg/mL
Dosis : awal 3x2 caps per hari, dan
bila gejala membaik menjadi 4 x 1
caps perhari
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Mucoactive drugs and their potential
mechanisms of action
Mucoactive drugs Potential mechanism of action
Mucolytics: Breaks disulphide bonds linking
N-Acetylcysteine mucin polymers
N-Acystelyn Antioxidant and anti-inflammatory
Erdosteine
effects.
Dornase alfa
Increases chloride secretion and
Gelsolin
Thymosin 4 breaks disulphide bonds
Dextran Modulates mucus production and
Heparin increases mucociliary transport
Hydrolyses the DNA in mucus and
reduces viscosity in the lungs
Severs actin filament cross-links
Severs actin filament cross-links
Breaks hydrogen bonds and
increases secretion hydration
Breaks both hydrogen and ionic
bonds
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Mucoactive drugs and their potential
mechanisms of action
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BRONCHODILATOR
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INTRODUCTION
beta-agonists
Anticholinergic
Phosphodiesterase (PDE)inhibitors : Theophylline
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INDICATION
Asthma
Bronchiectasis
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BETA-AGONISTS
Short-acting :
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SHORT-ACTING
Albuterol/salbutamol
Bambuterol
Fenoterol
Isoetherine
Isoproterenol
Levalbuterol
Metaproterenol
Terbutaline
Tornalate
Pirbuterol
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LONG-ACTING
Formoterol
Salmeterol
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EPINEPHRINE
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ISOPROTERENOL
A potent bronchodilator
Inhalation : 80-120 mcg maximal
bronchodilation within 5 minutes
Duration of action : 60-90 minutes
United Kingdom, 1960 an increase in the
asthma mortality use of high dose oh inhaled
isoproterenol
Now rarely used for asthma
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BETA-2 SELECTIVE DRUGS
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BETA-2-SELECTIVE DRUGS
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BETA-2-SELECTIVE DRUGS
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BETA-2-SELECTIVE DRUGS
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BETA-2-SELECTIVE DRUGS
Toxicities:
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METHYLXANTHINE DRUGS
Is metabolized by liver
Inexpensive
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ANTIMUSCARINIC AGENTS
Effective bronchodilators
Protype : atropine
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TUBERCULOSIS DRUGS
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INTRODUCTORY
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BIG PROBLEM
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The chemotherapy of tuberculosis started with
the introduction of streptomycin in 1946
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TB TREATMENT
The aims of TB treatment are:
To cure the patient and restore quality of life
and productivity;
To prevent relapse of TB;
To reduce the transmission of TB to others;
To prevent the development and transmission
of drug resistant TB.
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RCOMMENDED DOSES OF FIRST LINE
ANTI-TB DRUGS FOR ADULTS
Drug Daily 3 times per week
Dose & range Maximum (mg) Dose & range Daily maximum
(mg/kg BW) (mg/kg BW) (mg)
Patients aged over 60 years may not be able to tolerate more than 500750 mg daily, so
some guidelines recommend reduction of the dose to 10 mg/kg per day in patients in this
age group (2). Patients weighing less than 50 kg may not tolerate doses above 500750
mg daily (WHO Model Formulary 2008, www.who.int/selection_medicines/list/en/)
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New patients with pulmonary TB
WHO no longer recommends omission of ethambutol during the intensive phase of treatment for
patients with non-cavitary, smear-negative PTB or EPTB who are known to be HIV-negative. In
tuberculous meningitis, ethambutol should be replaced by streptomycin.
H = isoniazid, R= rifampicin, Z = pyrazinamide, E= ethambutol, S = streptomycin
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Dosing frequency for new TB
patients
Dosing frequency Comment
Note: Daily (rather than three times weekly) intensive-phase dosing may help to prevent
acquired drug resistance in TB patients starting treatment with isoniazid resistance
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Second-line agents
Amikacin (15 mg/kg/d)
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ISONIAZID
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ISONIAZID
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ISONIAZID
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ISONIAZID
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ISONIAZID
Adverse reaction:
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RIFAMPIN
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ETHAMBUTOL
A synthetic, water-soluble, heat-soluble compound, the dextro-
isomer
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ETHAMBUTOL
Most common :
TB meningitis retrobulbar neuritis loss
the higher visual acuity and red-
dose green blindness dose-
related at dosages : 25
mg/kg/d continued for
several months
Contra indicated in
children
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PIRAZYNAMIDE (PZA)
Inactive at neutral pH
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PZA
T12 : 8- 11 hours
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PZA
Adverse Effects:
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STREPTOMYCIN
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STREPTOMYCIN
IM well absorbed IM or IV
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STREPTOMYCIN
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STREPTOMYCIN
Adverse Effects:
Fever, skin rashes, and other allergic
manifestations
Pain at the injection site
Disturbance of vestibular function-
vertigo and loss of balance
Vestibular toxicity irreversible
During pregnancy deafness in the
newborn
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