antitussive and expectorants, respiratory stimulation

1. ANTITUSSIVE AND EXPECTORENTS
RESPIRATORY STIMULATION
SOS IN PHARMACEUTICAL SCIENCES
JIWAJI UNVERSITY
SUBMITTED BY:- Maneesha Kushwaha
SUBMITTED TO:-Manoj Sharma

2. ANTITUSSIVE
• Antitussives are drugs that suppress coughing
,possibly by reducing the activity of the cough
center in the brain.
• Antitussive agents are used to relieve dry
cough
COUGH
• Cough is protective reflex, its purpose being
• expulsion of respiratory secretions or foreign
• particles from the lungs and upper airway
• passages.

3. MACHANISM OF COUGH

5. CLASSIFICATION
ANTITUSSIVE/ COUGH SUPPRESSANTS
a) Opioids and related drug
 Codeine
 Pholcodeine
 Morphine
b) Non opioids
 Dextromethorphan
 Noscapine
c) Antihistamine
 Chlorpheniramine
 Diphenhydramine
 promethazine

6. COMMON COUGH SYRUP AND
CODEINE

7. CODEINE
• Codeine is an opioid (methylmorphine) with a
relatively limited analgesic effect; it does not cause
significant respiratory depressions but has good
antitussive properties.
• Codeine raises the stimulus threshold of the cough
center and thus has a cough suppressing effect.
• In most humans 10% of a codeine dose is
transformed to morphine through demethylation in
the liver. This explains the analgesic effect that is
absent in individuals with the respective genetic
traits.

8. MECHANISM OF ACTION
• Codeine sulfate is an opioid analgesic, related
to morphine, but with less potent analgesic
properties.
Codeine is selective for the mu receptor, but
with a much weaker affinity than morphine.
The analgesic properties of codeine have been
speculated to come from its conversion to
morphine, although the exact mechanism of
analgesic action remains unknown.

9. PHARMACOKINETICS AND ADVERSE
REACTION OF CODEINE
Pharmacokinetics
Bioavailability: 50%
Peak plasma level: 1 hour
Plasma half-life: 3 to 4 hours
Active metabolites: several
Elimination: predominantly
extrarenal
Adverse Reaction
• Retention of urine
• itching
• vertigo
• palpitations or bradycardia
• sweating
• mild central nervous effects

10. INTERACTION

11. EXPECTORANTS

12. EXPECTORANTS

13. CLASSIFICATION OF EXPECTOTANTS
a) Directly acting:
 Sodium and potassium salt of iodine , citrate and
acetic acid, guaicol, tolu balsam,
hydrate,guaiphenesin
b) Mucolytics:
 Bromhexine
 Acetylcysteine
 Carbocisteine
c) Pharyngdemulcents:
lozenges, cough drops ,linctuses containing syrup,
glycerine, liquorice

14. GUAIPHENESIN
• Guaifenesin is an expectorant, the action of
which promotes or facilitates the removal of
secretions from the respiratory tract.
MACHANISM OF ACTION
• By increasing sputum volume and making
sputum less viscous, guaifenesin facilitates
expectoration of retained secretions.

15. PHARMACOKINETICS AND ADVERSE
REACTION
PHARMACOKINETICS
• Absorption
Readily absorbed.
• Elimination The half-life
is 1 h; renal excretion;
major urinary
metabolite is beta-2-
(methoxyphenoxy)
lactic acid
ADVERSE REACTION
• Dizziness,
• Headache and rash
(including urticaria).
• Rare drowsiness or mild
gastrointestinal
• disturbances are the only
side effects associated with
extromethorphan in clinical
use.

17. MUCOLYTICS
• Mucolytics are administered by inhalation to liquefy
mucus in the respiratory tract. Solutions of mucolytic
drugs may be nebulized into a face mask or
mouthpiece or instilled directly into the respiratory
tract through a tracheostomy.
• Sodium chloride solution and acetylcysteine
(Mucomyst) are the only agent recommende for use
as mucolytics.

18. ACETYLCYSTEINE
• Acetylcysteine is
effective within 1 minute
after inhalation, and
maximal effects occur
within 5 to 10 minutes. It
is effective immediately
after direct instillation.
• Oral acetylcysteine is
widely used in the
treatment of
acetaminophen
overdosage

19. OTHER EXPECTORANT
Expectorants like bromhexine or ambroxole
may effectively decrease viscosity of bronchial
secretions

20. RESPIRATORY STIMULATION OR
ANALEPTICS
Introduction:
A respiratory stimulant is primarily used in addition
to noninvasive ventilation (Noninvasive ventilation
support to a patient through the upper airways) as a
means to help increase the urge to breath. It work by
stimulating the central nervous system, resulting in
an increase in respiration rate and tidal volume,
which is the amount of air that is inhaled or exhaled
during a normal breath
• Respiratory stimulate and have resuscitative value in
coma or fainting.

21. RESPIRATORY STIMULATION OR
ANALEPTICS
• Situations in which analeptics are used:
 Respiratory depression due to hypnotic drug
poisoning
 Suffocation on drowning
 Apnoea in premature infants
 Failure to ventilate spontaneously after general
anesthesia

22. RESPIRATORY STIMULANTS/
ANALEPTICS DRUG
Doxapram
Prethcamide
Modafinil
Reflex stimulant: Ammonia,
alcohol,
vapours

23. DOXAPRAM
Doxapram, also known as dopram, is a respiratory
stimulant and as such, help stimulate the respiratory
drive in patients who are recovering from surgery,
who have overdosed on certain drug or, who have
high carbon dioxide levels in their blood, which can
occur copd (cronic obstractive pulmonary)

24. MACHANISM OF ACTION
Doxapram stimulates respiration by an action on
peripheral carotid chemoreceptors. As the dosage is
increased, the medulla are stimulated with
progressive stimulation of other parts of the brain
and spinal cord

25. COMMON RESPIRATORY STIMULANTS

26. PHARMACOLOGICAL EFFECT
• Direct (respiratory centre) and indirect (reflex via
chemoreceptor)
CLINICAL USES
• Respiratory failure
ADVERSE EFFECTS
Nausea, coughing, restlesness.
DOSE
40 -80 mg I.V. Or I.M
Use
Treats acute respiratory failure