Anti Tussive, Mucolytics, and Expectorant

ANTITUSSIVE,
EXPECTORANT, AND
MUCOLYTICS
SISTIM RESPIRATORIK
SALURAN NAFAS ATAS.

Udara melalui lubang hidung / mulut
ke pharynx larynx trakhea untuk selanjutnya ke paru.
Penyakit yang tersering Infeksi Saluran Nafas Atas

Batuk, Pilek
SISTIM RESPIRATORIK
SALURAN NAFAS BAWAH

udara melalui trakhea bronkhus bronkhioli alveoli
Penyakit yang sering :
PPOM
Asma bronkhiale
Bronkhitis kronis
Emfisema
CLINICAL MANIFESTATION
 Upper Respiratory Tract  Lower Respiratory Tract

: :
 Common cold  Acute bronchitis
 Sinusitis  Pneumonia
 Epiglottis  Acute exacerbation of
 Laringitis COPD
 Acute exacerbation of
bronchiectasis
 Runny nose, nasal
congesti, sneezing, cough
& sputum  Fever
 Fever  Severe cough
 Headache  Difficulty breathing
 Pain during swallowing  Wheezing
 Wheezing  Chest pain
 Causative : based on causa
 Simptomatics :
- dekongestan
- antitusif
- ekspektoran
- mukolitik
- antihistamin
Agonis adrenergik , OTC Mechanism of action
products, a single or
Aktivasi reseptor
combination with other postjunctional
products adrenergik 
vasokonstriksi
Efffects : congesti nasal Penurunan aliran darah
Examples : ke mukosa hidung
Ephedrin
hidung longgar
Pseudoephedrin
Phenylpropanolamin (PPA)
Phenylephrin
 Indikasi :
 Nasal congesti
 Sinus congesti
 Eustachian tube congesti
 Vasomotor rhinitis
 Adjunct to other agents for allergic rhinitis,
sinusitis, otitis, etc
 Pharmacokinetics :
 Absorption : mostly from GIT
 Metabolism : Hepatic
 Half-life : 9-16 hours
 Adverse effects :
 Insomnia
 Nervousness
 Rare : dizzziness, palpitation, headache
 Indikasi :
 Nasal congestion
 Control of urinary incontinence
 Priapism
 Obesity
 Use :
 In cough and cold combination (with
Guaifenesinin)
 Appetite suppressant formulations
 Absorption : GIT (38%)
 Half-life : 2 – 3 hours
 Adverse effects : induce extrasystoles and
ventricular tachycardia
 Interaction :
 Limit caffeine intake
 Take without regard to meals
 Indikasi :
 Nasal congestion
 Hypotension & shock (during anaesthesia)
 Hemorrhoids
 Increase blood pressure
 Absorption : completely absorbed after oral
administration
 Metabolism : intestinal and liver
 Ekskretion : urine
 Half-life : 2 – 3 hours
Suppress coughing / cough
suppressant
 Inhiting a coordinating region for coughing located

in brainstem, disrupting the cough reflex arc
 Controversy , FOR => dry and irritating cough
 Types :
▪ Dextrometorphan
▪ Codeine
▪ Levopropoxyphene
▪ Noscapine
 Wide used, is an opioid-like drug
 Non-competitive channel blocker
 Indication : treatment and relief of dry cough
 Absorption : rapidly via GIT
 Half-life : 3-6 jam
 Opioid agonist related to morphine
 Use : less potent analgesic, mild sedative
effects
 Indication :
 Treatment and management of pain (systemic)
 Antidiarrheal
 Cough suppressant
 Absorption : 90% via oral administration
 Metabolism : hepatic
 Excretion : 90% via urine
 Half-life : 3 hours
 Adverse effects :
 Respiratory depression
 Sedation
 Nausea, vomiting
 Bradycardia
 Removed from the market in US
 Name : Levopropoxyphene Napsylate Anhidrous
 Indication :
 Treatment of cough
 Respiratory tract disorders
 Adverse effect :
 Sakit kepala
 Ruam kulit
 Mulut kering
 Mual, muntah
 From opium poppy Papaver somniverum
 Use :
 Mild analgesic
 Antitussive
 Antineoplastic activities
 Indication : dry cough
 Headache
 Nausea
 Vasomotor rhinitis
As medications that improve the
ability to expectorate purulent
secretion.
 How it works : thins the mucus, breaking up

the fluids that cause congestion and by clearing
thick mucus from the airway, making it easier
for the mucus to be coughed up
 Types :
 Guaifenesin
 Ipecac
 Ammonium chloride
 Potassium iodide
 Indication : to assist the expectoration of
phlegm from the airway in acute respiratory
tract infection
 Mechanism of action : increases the output of
phlegm (sputum) and bronchial secretion by
reducing adhesiveness and surface tension =>
increases the efficacy of the mucociliary
mechanism in removing accumulated secretions
from the upper and lower airway
 Absorption : rapidly from GIT
 Ekskretion : urine
 Half-life : 1 hour
 Interaction :
 Take with full glass of water
 From the plant Cephaelis ipecacuanha
 Indication :
 Low dose : an expectorant
 Other : induction of vomiting in poisoning victims
 Absorption : rapidly fro GIT
 Excretion : Feces
 Adverse effect : myopathy, muscle weakness
 In combination with other agents in
cough syrups
 Indication :
 expectorant
 Acid-base balance
 Mechanism of action :
 Irritative action on the bronchial mucosa
which causes the production of excess
respiratory tract fluid => easy to cough up
 Absorption : complete per oral
 Excretion : Urine
 Pallor
 Sweating
 Irregular breathing
 Bradycardia
 Mechanism of action : change the
biophysical properties of secretions by
degrading the mucin polymers, DNA,
fibrin, or F-actin in airway secretions
 Drugs :
 Bromheksin
 Ambroxol
 Asetilcystein
 Indication : expectorant/mucolytic agent
 Absorption : rapidly via oral
 Excretion : urine and bile
 GI
 Headache
 Dizziness
 Sweating
 Skin rashes
 A secretolytic agent
 Indication : bronchopulmonary diseases
 Mechanism of action : inhibit the NO-
dependent activation of soluble guanylate
cyclase => suppress the excessive mucus
secretion => lowers the phlegm viscosity
=> improves mucociliary transport of
bronchial secretion
 Absorption : rapid and almost complete
 Adverse effect : mild GI symptoms
 Use in nebulization
 Indication :
 Mucolytic in chronic bronchopulmonary diseases
 Management of Acetaminophen overdose
 Side effect :
 Stomatitis
 Nausea, vomiting
 Fever
 Rhinorrhea
 Sedative
 First Generation => sedation
 Chlorpheniramin maleat (chlortrimeton=ctm)
 Diphenhydramin (delladryl, benadryl)
 Prometazine (Phenergan)
 Second Generation :
 Loratadine
 Cetirizine
 First Generation
 Indication : rhinitis, urticaria, allergy, common cold, asthma,
hay fever
 Mechanism of action : blocks the action of endogenous
histamine => relief of negative symptoms of histamine
(vasodilatation, bronchoconstriction)
 Absorption : Well absorbed in GIT
 Metabolism :Hepatic
 Half life : 21-27 hours
 Drowsiness
 Dizziness, headache
 Upset stomach, constipation
 Interaction : Take with food
 First Generation
 OTC, “night time use”
 Indication :
 Allergic rhinitis
 Common cold
 Vertigo
 Mechanism of action : competes with free
histamine for binding at HA-receptor sites =>
antagonizes negative effect of histamine
 Absorption : quickly absorbed after 1 hour
 Metabolism : hepatic and renal
 Excretion : little in urine
 Half-life : 1-4 hour
 Myocardial infarc
 Coma => death (with LD50=500mg)
 Interaction :
 Take with food
 Indication : treatment of allergic disorders
 Mechanism of action : competes with free
histamine for binding at receptor
 Absorption : 88% via oral administration
 Excretion : urine
 Adverse effect : mild depression of CNS, KV
 Interaction : take with food
 Second generation of histamine
 Use alone or with combination with
pseudoephedrine sulfate => allergic rhinitis
 Mechanism of action : competes with
histamine => blocks endogenous histamine
=> temporary relief of negative symptoms
(nasal congestion, watery eyes)
 Absorption : rapidly with oral administration
 Half-life : 8 hours
 Adverse effect : somnolence, tachycardia,
headache
 Interaction : take on empty stomach
 2nd generation
 Indication : rhinitis (allergic, perennial)
 Mechanism of action : competes with
histamin for binding at the receptor =>
suppress histamine effects
 Low incidence of sedation
 Half-life : 8 hours
 Adverse effect : irritability, drowsiness
 Interaction : take with no regard to meals

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ANTITUSSIVE,

SALURAN NAFAS ATAS.

Penyakit yang tersering Infeksi Saluran Nafas Atas

SALURAN NAFAS BAWAH

 Upper Respiratory Tract  Lower Respiratory Tract

 Inhiting a coordinating region for coughing located

 How it works : thins the mucus, breaking up

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