Nasal decongestants and Respiratory Stimulants.pdf

3,474 views 29 slides Jan 14, 2023
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About This Presentation

At the end of this e-learning session you are able to…
A. Discuss definition and therapeutic uses, limitation, classification and pharmacology of nasal decongestant.
B. Explain definition and uses, limitation, classification and pharmacology of respiratory stimulants.

I am happy to share lec...


Slide Content

Prof. Shaikh Abusufiyan
Assistant Professor,
AIKTC-School of Pharmacy,
New Panvel-410206
Nasal Decongestant and
Respiratory Stimulants
Pharma Learning Forever

At the end of this e-learning session you are able to…
A.Discuss definitionandtherapeutic uses,
limitation, classification andpharmacology
of nasal decongestant.
B.Explain definitionanduses, limitation,
classification andpharmacology of
respiratory stimulants.
Copyright @shaikhabusufiyan2021

Definition:
•Thesearealphaagonist
thatproduceslocalvasoconstrictionontopical
application.
Reducescongestionofnasalpassage
Opencloggednasalpassageandenhances
drainageofthesinuses
https://www.britannica.com/science/nose, archived
on 7thJan 2023

•TherapeuticUse
•Patientwithallergicorvasomotor
rhinitis
•Acuterhinitisinpatientwithupper
respiratoryinfection

Limitation of chronic use of nasal decongestant or withdrawal
•Lossofefficacy
•Reboundhyperemia
•Worseningofsymptoms
Duetoreceptordesensitizationandmucosal
damage

1. Alpha1agonists
Eg.Phenylephrine
2.Alpha2Agonists/
Imidazoline compounds
Eg. Clonidine,
Xylometazoline
Oxymetazoline
Naphazoline
1. Short Acting (Topically
administered)
Eg. Phenylpropanolamine,
Phenylephrine
2. Long acting (Orally
administered
Eg.Naphazoline
Ephedrine
Pseudoephedrine
3. Long acting (Topically
administered)
Eg.Xylometazoline
Oxymetazoline
Classification of nasal decongestant:
Depending on duration actionDepending on alpha receptor agonism
Use with great caution
in patients with
hypertension and in
patients with prostatic
enlargement

•Alpha1agonists:
•ActivateAlpha1receptors
Vasoconstriction
Decreaseinresistancetoairflowby
decreaseinvolumeofnasalmucosa

•Advantage:
•NegligibleBetaactionevenathighdose
•Lesslikelytoinducedmucosaldamage
•OnlyonIVinfusion
itinducesmarkedarterialvasoconstrictionand
increaseinbloodpressure.

•Phenylephrinelack–oHgroupatposition4
ofbenzenering
Phenylephrine and epinephrine
EpinephrinePhenylephrine

Ephedrineisa
mixed-acting
sympathomimetic
amine
whereas
Pseudoephedrineis
anindirectly-acting
sympathomimetic
amine
Pseudoephedrineis
lesspotentthan
ephedrinein
producing
tachycardia,increase
inBP,andCNS
stimulationArchived on 5thJan 2023 https://www.differencebetween.com/what-is-the-difference-between-ephedrine-and-pseudoephedrine/

•TherapeuticUsesofAlpha1agonist
•Nasaldecongestantinacuterhinitis
•Topicallyusedasmydriatic
•Reducesintraoculartensionby
constrictingbodybloodvassals

ACTIVITY I
Q.1 Nasal decongestants are -------agonists?
Q.2 Enlist therapeutic uses of nasal decongestants
Q.3 Give example of long acting topically administered
nasal decongestants.
Copyright @shaikhabusufiyan2021

Activity II: Self learning of e-content

Alpha2receptor agonist/ Imidazoline compounds
•Alpha2receptorsmediate:
contractionofarteriolesthatsupplynutrition'stothe
nasalmucosa
•Thisintensecontractioncausesstructuraldamageto
themucosaandimpairedmucosalciliaryfunctions
Atrophicrhinitisandanosmiacanoccur
Regularuseshouldbeavoided

•Alpha2receptoragonistsabsorbfromnose
Producessystemiceffect(CNSdepressionand
riseinBP)
Usewithcautionincaseofhypertensiveand
inpatientwithtreatmentofMAOInhibitors

Clonidine:
•Itisimidazolinederivative
•ActonperipheralAlpha2receptors.
•Duringclinicaltrialastopicalnasal
decongestant
Clonidinecauseshypotension,sedationand
bradycardia
•IVinfusionofclonidinecausesacuterisein
abloodpressure

Side effects of alpha2agonists:
•Hypertension through vasoconstriction
•Sleeplessness
•Anxiety
•Dizziness
•Excitability and nervousness
•Topical nasal decongestant quickly develop tachyphylaxis to
drug after repeated dose in short period
Long term use is not recommended

Activity III: Self learning assessment
https://forms.gle/9Ef1t7EVEF9vbTQ46
Do literature survey and name leading nasal decongestant brand in the market

Definition:
Thesearethedrugs
Whichstimulaterespiration
Andcanhaveresuscitationvalue(Abilityto
restoreconsciousness)incaseofcommaor
fainting.
Respiratorystimulants
human lungs; Image, EncyclopædiaBritannica. Encyclopædia
Britannica, Urlhttps://www.britannica.com/science/human-
respiratory-system#/media/1/499530/99769
•Access Date8 January 2023

•Relativelylittleeffectonmentalfunction
•Actmainlyonthebrainstem&spinalcord
•Atlowdoseitproducesincreaseinactivityof
the:
•Respiratory
•Vasomotorcenters
•Withhigherdosage--->convulsions.
Respiratorystimulants:
Archived from https://in.pinterest.com/pin/648870258809384846/on
8thJan 2023. Photo byLeggerondreamstime
·Illustration about Drawing of the brain and brainstem, shwoing
areas of the pons that control respiration. Illustration of science,
medulla, brain -14221213

•Synonyms:Sometimescalled
analeptics
•Usedtotreatpatientsinterminal
comaorwithsevererespiratory
failure.

Benefits
•Temporaryrestorationoffunctioncouldbeachieved
•Mortality-notreduced
•Treatmentcarriedaconsiderablerisk
•ofcausingconvulsions(Patientmoredeeplycomatose
thanbefore).
•Usedmainlytogivetheimpressionthatsomethingwas
beingdoneforapatientinextremis.

TherapeuticusesofAnaleptics:
•Itisverylimitedinconditionslike
•Overdosewithsedativeandhypnoticsuntil
mechanicalventilationisinitiated
•Acuterespiratoryinsufficiency
•Suffocationondrowning
•Postanaestheticrespiratorydepression
•Apneainprematureinfant
•Failuretoventilatespontaneouslyafter
generalanesthesia
•Idiopathichypoventilation

3. Drugs with mixed action
Eg.Nikethamide, Carbogen
1. Drugs acting directly on
respiratory centre
Eg. Caffeine, Bemegride,
Etimizole
2. Drugs acting by
reflex action
Eg.Cytiton, Lobeline
Classification of Respiratory Stimulants:

Doxapram
•Act by promoting --> excitationof central neurons.
•At low dose --> it is more selectivefor respiratory
center than other analeptics.
•In addition, it stimulate--> respiration through
carotidand aortic body chemoreceptors
•Carry less risk of causing convulsions than other
compounds --->Most commonlyused
•But itcauses nausea, coughing and restlessness -limit its
usefulness.

•Continuous IV infusion of Doxapram --->
Abolish episode of apnoea in premature
infants not responding to theophylline
•Dose: 40 to 80 mg, im or iv;
•0.5 to 2 mg/kg/hriv infusion

ACTIVITY III
Q.1 ------is the part of CNS where respiratory stimulant
acts.
Q.2 Enlist therapeutic uses of analeptics
Q.3 Name respiratory stimulant with mixed action.
Copyright @shaikhabusufiyan2021

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