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Dr. RAGHU PRASADA M S
MBBS,MD
ASSISTANT PROFESSOR
DEPT. OF PHARMACOLOGY
SSIMS & RC.
 Cough is a useful physiological mechanism that
serves to clear the respiratory passages of foreign
material and excess secretions.
 Cough reflex is complex, involving the central and
peripheral nervous systems as well as the smooth
muscle of the bronchial tree.
 It should not be suppressed discriminately.
 Chronic cough can contribute to fatigue, especially in
elderly patients, in such situations the physicians
should use a drug that will reduce the frequency or
intensity of the coughing.
 It has been suggested that irritation of the bronchial
mucosa causes bronchoconstriction, which in turn,
stimulates cough receptors (which probably
represent a specialized type of stretch receptor)
located in the tracheobronchial passages.
Stimulation of mechano-or chemoreceptors (throat,
respiratory passages or stretch receptors in lungs)
Afferent impulses to cough centre (medulla)
Efferent impulses via parasympathetic & motor
nerves to diaphragm, intercostal muscles & lung
Increased contraction of diaphragmatic, abdominal
& intercostal (ribs) muscles noisy expiration
(cough)
PRODUCTIVE COUGH
NON-PRODUCTIVE COUGH
Expectorants- increase the volume and decrease the
viscosity of secretions to enhance the propulsion of
these secretions upward and outward by ciliary
movement and coughing
Opioids –codeine, pholcodeine
Non-opioids-Dextromethorphan, noscapine and
pipazethate
Codeine –Semisynthetic opioid analgesic
-potent cough suppressant action
-10mg BD/TDS-lesser
addiction/constipation
Overdose-Resp. depression, convulsion, postural
hypotension, tachycardia
Structurally related to codeine
More potent, longer acting and better tolerated
than codeine
Causes lesser constipation and drowsiness than
codeine
Given orally 10-15mg BD
It is methyl ester of dextroisomer of levorphanol
MOA-NMDA receptor antagonist
It has least addiction, no analgesic action
(unlike levorphanol) least constipating effects and minimal
drowsiness
As potent as codeine -10mg TDS
Uses: Cough suppressant, used for temporary relief of
cough caused by minor throat & bronchial irritation
(accompanies with flu & cold), pain relief
Adverse Effects
 Nausea, vomiting, drowsiness, dizziness, blurred vision
Naturally occurring opium alkaloid belonging to
benzylisoquinoline group
Devoid of analgesic activity, drowsiness and liability
Has minimal constipating effects and popular cough
suppressant
Given orally-15mg TDS-produce headache and tremors
 Phenothiazine group of antitussive occasionally used
in cough mixtures
 Negligible CNS depressants –orally 40mg-TDS
Morphine-powerful cough suppressant, but long term
use constipation
BENZONATATE
It is an antitussive structurally related to the local
anaesthetic tetracaine
Inhibits the afferent cough impulses to suppress the
central cough centre, but also inhibits the pulmonary
stretch receptors has central as well as peripheral
mechanism of action
It possesses mild local anaesthetic action
Orally 100-200mg TDS
S/E- drowsiness, Nausea, Headache
 Indirect peripherally acting cough suppressant
 Provide protective coating over sensory receptors on
pharynx
 Honey, liquorice, syp tolu, syp Vasaka
PRENOXDIAZINE
-acts by inhibiting pulmonary stretch receptors to
relieve bronchospasm
It has moderate antitussive action
Orally 100-200mg TDS
Local anaesthetic-
Xylocaine, Bupivaciane- applied on pharynx and larynx
and decrease sensitivity of receptors
Antitussive –not to be used in cough associated with
bronchial asthma or chronic bronchitis or
bronchiectasis harmful retention and thickening of
sputum
Drugs either increase or decrease the viscosity of
respiratory secretions and facilitate their removal by
ciliary action and coughing by mucolytic and mucokinetic
action
Mucolytic expectorants
They alter the chemical charecteristics of mucous to
decrease its viscosity and to facilitate its removal by ciliary
action or coughing. Commonly used mucolytics- acetyl
cysteine, carbocysteine, Bromexine, Ambroxol and
Dornase-alfa
BROMHEXINE-Synthetic derivative of vasicine (alkaloid=
Adhatoda vasica)
MOA of Bromhexine
a) Thinning & fragmentation of mucopolysaccaride fibers
b) ↑ volume & ↓ viscosity of sputum
ACETLYL CYSTEINE
Mucolytic, that decreases viscosity of mucous by
splitting the disulfide (-S-S-) bonds of mucoproteins↓
viscosity
This action facilitated by Alkaline pH-7-9
Acetyl cysteine (cont..)
Nebulizn- 3-5ml of 20% soln
Onset of action quick---used 2-8 hourly
Uses
Cystic fibrosis (to viscosity of sputum)
Chronic bronchitis
Treatment of paracetamol poisoning
Unlabelled use includes the treatment of dry eyes
(keratoconjunctivitis sicca as 5% acetyl cysteine with
hyperomellose
Adverse effects
Nausea, vomiting, bronchospasm in bronchial asthma
CARBOCYSTEINE-has protected –SH group therefore
cannot work through SH group and –S-S- interchange
It cannot split the disulphide bonds of mucus
AMBROXOL-metabolite of bromexine
- mechanism similar to bromexine
- more useful in mucus plugs
- 30mg TDS
 These expectorants stimulate the flow of respiratory
tract secretions by stimulating the bronchial
secretory cells (to increase the volume) and ciliary
movements (to facilitate their removal
 Can also stimulate GI mucosa increase resp. sectrn
 Ammonium chloride, Sodium citrate Guaiacol,
Guiaifenesin
Essential oils- oil anize, oil eucalyptus
 Provide mild exp. By directly stimulating the
bronchial secretory cells
Ammonium chloride –cough expectorant in various
cough mixtures
-gastric irritant reflex bronchial sectrn
Sodium citrate-conventionally used in several cough
mixtures.
After absorption, citrates get converted to
bicarbonates invivo and mucous becomes less viscous
Obtained from creosate wood
Safe expectorants with proven efficacy
GUAIFENESIN -Less irritating derivative of guaiacol
After absorption-secreted into bronchial glands-
increase airway secretion and mucosal ciliary activity
Oral-100-200mg TDS
Class drugs used in cough

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Class drugs used in cough

  • 1. Dr. RAGHU PRASADA M S MBBS,MD ASSISTANT PROFESSOR DEPT. OF PHARMACOLOGY SSIMS & RC.
  • 2.  Cough is a useful physiological mechanism that serves to clear the respiratory passages of foreign material and excess secretions.  Cough reflex is complex, involving the central and peripheral nervous systems as well as the smooth muscle of the bronchial tree.  It should not be suppressed discriminately.  Chronic cough can contribute to fatigue, especially in elderly patients, in such situations the physicians should use a drug that will reduce the frequency or intensity of the coughing.
  • 3.  It has been suggested that irritation of the bronchial mucosa causes bronchoconstriction, which in turn, stimulates cough receptors (which probably represent a specialized type of stretch receptor) located in the tracheobronchial passages.
  • 4. Stimulation of mechano-or chemoreceptors (throat, respiratory passages or stretch receptors in lungs) Afferent impulses to cough centre (medulla) Efferent impulses via parasympathetic & motor nerves to diaphragm, intercostal muscles & lung Increased contraction of diaphragmatic, abdominal & intercostal (ribs) muscles noisy expiration (cough)
  • 5. PRODUCTIVE COUGH NON-PRODUCTIVE COUGH Expectorants- increase the volume and decrease the viscosity of secretions to enhance the propulsion of these secretions upward and outward by ciliary movement and coughing
  • 6. Opioids –codeine, pholcodeine Non-opioids-Dextromethorphan, noscapine and pipazethate Codeine –Semisynthetic opioid analgesic -potent cough suppressant action -10mg BD/TDS-lesser addiction/constipation Overdose-Resp. depression, convulsion, postural hypotension, tachycardia
  • 7. Structurally related to codeine More potent, longer acting and better tolerated than codeine Causes lesser constipation and drowsiness than codeine Given orally 10-15mg BD
  • 8. It is methyl ester of dextroisomer of levorphanol MOA-NMDA receptor antagonist It has least addiction, no analgesic action (unlike levorphanol) least constipating effects and minimal drowsiness As potent as codeine -10mg TDS Uses: Cough suppressant, used for temporary relief of cough caused by minor throat & bronchial irritation (accompanies with flu & cold), pain relief Adverse Effects  Nausea, vomiting, drowsiness, dizziness, blurred vision
  • 9. Naturally occurring opium alkaloid belonging to benzylisoquinoline group Devoid of analgesic activity, drowsiness and liability Has minimal constipating effects and popular cough suppressant Given orally-15mg TDS-produce headache and tremors
  • 10.  Phenothiazine group of antitussive occasionally used in cough mixtures  Negligible CNS depressants –orally 40mg-TDS Morphine-powerful cough suppressant, but long term use constipation
  • 11. BENZONATATE It is an antitussive structurally related to the local anaesthetic tetracaine Inhibits the afferent cough impulses to suppress the central cough centre, but also inhibits the pulmonary stretch receptors has central as well as peripheral mechanism of action It possesses mild local anaesthetic action Orally 100-200mg TDS S/E- drowsiness, Nausea, Headache
  • 12.  Indirect peripherally acting cough suppressant  Provide protective coating over sensory receptors on pharynx  Honey, liquorice, syp tolu, syp Vasaka PRENOXDIAZINE -acts by inhibiting pulmonary stretch receptors to relieve bronchospasm It has moderate antitussive action Orally 100-200mg TDS
  • 13. Local anaesthetic- Xylocaine, Bupivaciane- applied on pharynx and larynx and decrease sensitivity of receptors Antitussive –not to be used in cough associated with bronchial asthma or chronic bronchitis or bronchiectasis harmful retention and thickening of sputum
  • 14. Drugs either increase or decrease the viscosity of respiratory secretions and facilitate their removal by ciliary action and coughing by mucolytic and mucokinetic action Mucolytic expectorants They alter the chemical charecteristics of mucous to decrease its viscosity and to facilitate its removal by ciliary action or coughing. Commonly used mucolytics- acetyl cysteine, carbocysteine, Bromexine, Ambroxol and Dornase-alfa
  • 15. BROMHEXINE-Synthetic derivative of vasicine (alkaloid= Adhatoda vasica) MOA of Bromhexine a) Thinning & fragmentation of mucopolysaccaride fibers b) ↑ volume & ↓ viscosity of sputum ACETLYL CYSTEINE Mucolytic, that decreases viscosity of mucous by splitting the disulfide (-S-S-) bonds of mucoproteins↓ viscosity This action facilitated by Alkaline pH-7-9
  • 16. Acetyl cysteine (cont..) Nebulizn- 3-5ml of 20% soln Onset of action quick---used 2-8 hourly Uses Cystic fibrosis (to viscosity of sputum) Chronic bronchitis Treatment of paracetamol poisoning Unlabelled use includes the treatment of dry eyes (keratoconjunctivitis sicca as 5% acetyl cysteine with hyperomellose Adverse effects Nausea, vomiting, bronchospasm in bronchial asthma
  • 17. CARBOCYSTEINE-has protected –SH group therefore cannot work through SH group and –S-S- interchange It cannot split the disulphide bonds of mucus AMBROXOL-metabolite of bromexine - mechanism similar to bromexine - more useful in mucus plugs - 30mg TDS
  • 18.  These expectorants stimulate the flow of respiratory tract secretions by stimulating the bronchial secretory cells (to increase the volume) and ciliary movements (to facilitate their removal  Can also stimulate GI mucosa increase resp. sectrn  Ammonium chloride, Sodium citrate Guaiacol, Guiaifenesin
  • 19. Essential oils- oil anize, oil eucalyptus  Provide mild exp. By directly stimulating the bronchial secretory cells Ammonium chloride –cough expectorant in various cough mixtures -gastric irritant reflex bronchial sectrn Sodium citrate-conventionally used in several cough mixtures. After absorption, citrates get converted to bicarbonates invivo and mucous becomes less viscous
  • 20. Obtained from creosate wood Safe expectorants with proven efficacy GUAIFENESIN -Less irritating derivative of guaiacol After absorption-secreted into bronchial glands- increase airway secretion and mucosal ciliary activity Oral-100-200mg TDS