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Medications Used in
ENT Disorders
Group 08 1
30.11.2020
Introduction
• Otolaryngology, or ENT (ears, nose and throat) , is the branch of medicine
that specializes in the diagnosis and treatment of conditions of the ears,
nose, sinuses, larynx (voice box), mouth, and throat, as well as structures of
the neck and face.
2
• These are often common organ which directly entouched with outer
environment. In summer or winter session, ear, nose and throat are
more often get infected.
• ENT drugs commonly assemble as topical delivery and it has a
number of advantages over systemic delivery. A vastly higher
concentration of drug can be delivered to the site of infection.
• Medications delivered topically have no systemic effects.
3
• Ear infection like Chronic suppurative otitis media, Acute suppurative
otitis media , otosclerosis , Tinnitus are more common.
• Nose infection like Allergic rhinitis, Sinusitis, nasal polyps,running
nose are mostly common.
• Pharyingits / tonsillitis are common infection throat. These are
disease become sever when environment changed suddenly.
4
Ear drugs
• Antibiotics – To reduce the inflammation.
• Local analgesics – To reduce pain in the ear
• Steroids – To treat inflammation of the skin of the ear canel.
• Wax emulsifiers – Loosen and remove ear wax.
• Combination of Ear drops – To treat multiple aspects of Otitis media
or Otitis externa (Anti inflammatory, anti-pruritis, anti-allergic)
• Ear drops – Solution or suspension forms are common. Ointments
less.
5
Nose Drugs
• Nasal sprays for local effect are quite common. Steroids, antiasthma
medications such as salbutamol, ipratropium, montelukast and a large
number of inhalational anaesthetic agents are being used commonly.
• Nasal applications of topical decongestants or anti-inflammatory drugs
are the most popular topical nasal drug deliveries. For some compounds,
delivery of drugs via the nasal route provides direct access to systemic
absorption.
6
Drugs for throat
• Throat drugs are mainly use to stop cough reflex when the cough is non
productive or harmful. It reduce runny nose and postnasal drip.
Eg: Codeine (Opoid Antitussive)
• Oral thrush or a sore throat can be treated easily with over-the-counter
medicines.
• Mouth wash, Throat lozenges and pastilles are commonly used.
• Demulcents: sooth the throat and reduce afferent impulses from the
inflamed and irritated pharyngeal mucosa.
• Expectorants: drugs that increase bronchial secretion or reduce its
viscosity, facilitating its removal by coughing.
7
• ENT medications can be broken down into the following
categories
Corticosteroids
Antihistamines
Decongestants
Antibiotics
Antifungals
8
Corticosteroids Drugs
• Corticosteroids are frequently used in a wide range of ear-nose-throat
(ENT) conditions due to their anti-inflammatory properties.
Mechanism of Action:
• Steroid acts on transcription proteins found inside the cytoplasm and
causes a reduction in the amount of inflammatory cytokines secreted
by the cell. Reduces the cells response to inflammation.
• Due to this complex mechanism of action there is a time delay between
the administration of the drug and its clinical activity.
• They decrease inflammation and edema of the mucous membranes.
9
Corticosteroid Drug for the Nose
Intranasal (IN): (Spray or Drop) or Inhalation
• Intranasally administered steroid should be lipophilic; First pass
metabolism is avoided.
• Very low dose is enough for local effect – reduced systemic toxicity.
• Administered intranasally to treat allergic and nonallergic rhinitis.
Example
• Fluticasone
• Beclomethasone
• Beconase
• Mometasone
10
Topical:
• Applied topically as a solution in the external
ear canal to decrease inflammation associated
with allergies or infections.
Example
• Betamethasone
• Dexamethasone
11
Corticosteroid Drug for the Ears
Ear drops:
• Used to treat eczematous conditions of the skin lining of external canal,
Myringitis granulosa, to reduce middle ear mucosal edema in active
middle ear infections with central perforation.
Indications
• Acute allergic rhinitis
• Acute sinusitis
• Acute epiglottitis
• Otitis externa – to reduce external canal
inflammatory oedema
• Sinonasal inflammatory polyposis
• Acute sensorineural hearing loss (sudden
deafness)
• Nasal sarcoidosis
• Acute stridor before tracheostomy
• Chronic otitis media
12
Common Side effects
Complications Associated with
• Short-term Use of Steroids
• Long-term Use of Steroids
Short-term Use of Steroids:
• Hypothalamic-pituitary-adrenal
axis suppression
• Hyperglycemia
• Gastrointestinal Disturbances
• Psychiatric effects
13
Long-term Use of Steroids:
• Osteoporosis
• Cushingn Syndrome
• Accelerated atherosclerosis
• Early cataract
• Skin thinning
• Pupura
Decongestant Drugs
• Congestion in the nose, sinuses, and chest is due to swollen,
expanded, or dilated blood vessels in the membranes of the
nose and air passages.
• These membranes, with a great capacity for expansion, have an
abundant supply of blood vessels.
• Once the membranes swell, you start to feel congested.
14
• Decongestants help to shrink the blood vessels in the nasal membranes
and allow the air passages to open up.
15
Mechanism of Action of Decongestants Drugs
• Produce vasoconstriction by stimulating alpha receptors in
the smooth muscle around the blood vessels.
• Decrease swelling of mucous membranes in the nose,
sinuses, and pharynx,
• Alleviate nasal stuffiness and sinus congestion
• Allow secretions to drain
• Help open up Eustachian tubes to the ears
• Can be administered topically as nose drops or nasal sprays
or orally.
16
Example
• Oxymetazoline
• Terahydrolozine
• Phenylephrine
• Pseudoephedrine
Indications
• Nasal and eustachian tube congestion
• Nasal stuffiness
• Acute or chronic rhinitis
• Sinusitis, allergic conditions
• Before nasal diagnostic examination to improve visualization.
17
Side Effect
• Cardiac arrhythmias
• Headache
• Insomnia
Contraindications
• Severe hypertension
• Coronary artery disease
• Narrow angle glaucoma
• Use with Nasal steroids
• Pregnancy and lactation
18
Antihistamine Drugs
• Histamine is an important body chemical that is responsible for the
congestion, sneezing, runny nose, and itching that a patient suffers
with an allergic attack or an infection.
• Antihistamine drugs block the action of histamine, therefore reducing
these symptoms.
• For the best result, antihistamines should be taken before allergic
symptoms get well established, but they can also be very effective if
taken after the onset of symptoms.
19
20
Mechanisms of Action
• Histamine released from mast cells in the tissues when an allergic
reaction.
• Causes vasodilation in which the blood vessels and mucous membranes
become swollen and red. Irritates the tissue directly, causing pain and
itching.
• Antihistamines acts by blocking H1 histamine receptor sites, thereby
blocking the effects of histamine on H1-receptors on the Nose and
Throat.
• So block the action of histamine at H1 receptors to:
• Dry up secretion.
• Shrink edematous mucous membranes
• And Decrease itching and redness
21
Example:
• 1st Generation: Chlorpheniramine, Diphenhydramine, Brompheniramine
• 2nd Generation: Cetirizine, Levocetirizine, Loratadine, Desloratadine
Dosage form
• Intranasal, Topical, and Oral preparations are available
22
Indications
• Allergic Rhinitis
• Sneezing
• Stuffiness
• Itchy nose, and throat
• Runny nose.
Side Effects
• Sedation (by 1st Generation drugs)
• Dry Mouth
• Drowsiness
• Dizziness
• Nausea and Vomiting
23
Antibiotics Drugs
Antibiotics for Ear
Framycetin sulfate
• Framycetin is a broad spectrum aminoglycoside
antibiotic
• framycetin appears to inhibit protein synthesis
in susceptible bacteria by binding to ribosomal
subunits.
• Framycetin is not active against most anaerobic
bacteria
24
Gentamicin
• Gentamicin is a protein synthesis inhibitor.
• It binds the 30S bacterial ribosomal subunit and acts to inhibit the
formation of the initiation complex, causes mRNA misreading leading to
non-functional proteins.
• It also induces the dissolution of polyribosomes during protein synthesis.
• Aminoglycosides require oxygen for uptake into the bacterial cell. Thus,
they are only active against aerobes.
25
Antibiotics for Nose
Chlorhexidine with neomycin
• Chlorhexidine-neomycin is an antibiotic available in nasal topical form
only.
• It is used to treat minor nasal infection with, and carriage of,
Staphylococci bacteria.
• Chlorhexidine gluconate is an antiseptic that kills a wide range of
bacteria and yeasts, and some fungi and viruses.
• Neomycin sulphate is an antibiotic of the aminoglycoside type. It
rapidly kills bacteria by interfering with the production of proteins
that the bacteria need to divide and multiply.
26
Mupirocin
• Mupirocin is an antibiotic.
• It is used inside the nose to treat infections that are caused by certain
bacteria.
• This helps prevent the spread of infection to patients and health care
workers during outbreaks at institutions.
27
Antibiotics for Oropharyngeal
Doxycycline
• Doxycycline is a tetracycline antibiotic that fights bacteria in the body.
• Doxycysline reversiably bind to 30s subunit at A site. And Block the
binding of aminoacyl t-RNA to m-RNA.
• Inhibit the addition of new aminoacid to growing peptide chain. And
Stop the translation process, new protein cannot be made.
28
Antifungal Drugs
• Fungal infections of the mouth are usually caused by Candida spp.
(candidiasis or candidosis).
• Different types of oropharyngeal candidiasis are managed as follows:
• Thrush
• Acute erythematous candidiasis
• Denture stomatitis
• Chronic hyperplastic candidiasis
• Angular cheilitis
29
Drugs used in oropharyngeal candidiasis
Miconazole
• Miconazole inhibits the fungal enzyme 14α-sterol demethylase,
resulting in a reduced production of ergosterol.
• In addition to its antifungal actions, miconazole, similarly
to ketoconazole, is known to act as an antagonist of
the glucocorticoid receptor
30
Nystatin
• nystatin is an ionophore. It binds to ergosterol, a major component of
the fungal cell membrane.
• When present in sufficient concentrations, it forms pores in the
membrane that lead to K+ leakage, acidification, and death of the
fungus.
• Nystatin when taken by mouth is used to treat yeast infections in the
mouth or stomach.
• Oral nystatin is not absorbed into your bloodstream and will not treat
fungal infections in other parts of the body or on the skin.
• Too toxic for synthetic use, Used only topically
31
References
• Abbasi, A. Al. (2017). Hand book of otolaryngology. September.
• Bade, D., K. G., S., L. J., K., M. S., R., V. S., H., & A. N., P. (2020). A cross sectional study on
prescription pattern of drugs in upper respiratory tract infections in a tertiary care hospital.
International Journal of Basic & Clinical Pharmacology, 9(2), 271.
• Daniel, M., Bharathi, D. R., Nataraj, G. R., & Jinil, A. L. (2018). Drug Utilization Trends in ENT
Outpatients. 3(December), 166–171.
• Klein, J. O. (1980). Principles and Practice of Infectious Disease. Annals of Internal Medicine,
92(5), 728.
• Paterson, S. (2016). Topical ear treatment – options, indications and limitations of current
therapy. Journal of Small Animal Practice, 57(12), 668–678.
• World Health Organization. (2004). The global burden of disease 2004. Update, World Health
Organization, 146.
32

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ent pharmacology

  • 1. Medications Used in ENT Disorders Group 08 1 30.11.2020
  • 2. Introduction • Otolaryngology, or ENT (ears, nose and throat) , is the branch of medicine that specializes in the diagnosis and treatment of conditions of the ears, nose, sinuses, larynx (voice box), mouth, and throat, as well as structures of the neck and face. 2
  • 3. • These are often common organ which directly entouched with outer environment. In summer or winter session, ear, nose and throat are more often get infected. • ENT drugs commonly assemble as topical delivery and it has a number of advantages over systemic delivery. A vastly higher concentration of drug can be delivered to the site of infection. • Medications delivered topically have no systemic effects. 3
  • 4. • Ear infection like Chronic suppurative otitis media, Acute suppurative otitis media , otosclerosis , Tinnitus are more common. • Nose infection like Allergic rhinitis, Sinusitis, nasal polyps,running nose are mostly common. • Pharyingits / tonsillitis are common infection throat. These are disease become sever when environment changed suddenly. 4
  • 5. Ear drugs • Antibiotics – To reduce the inflammation. • Local analgesics – To reduce pain in the ear • Steroids – To treat inflammation of the skin of the ear canel. • Wax emulsifiers – Loosen and remove ear wax. • Combination of Ear drops – To treat multiple aspects of Otitis media or Otitis externa (Anti inflammatory, anti-pruritis, anti-allergic) • Ear drops – Solution or suspension forms are common. Ointments less. 5
  • 6. Nose Drugs • Nasal sprays for local effect are quite common. Steroids, antiasthma medications such as salbutamol, ipratropium, montelukast and a large number of inhalational anaesthetic agents are being used commonly. • Nasal applications of topical decongestants or anti-inflammatory drugs are the most popular topical nasal drug deliveries. For some compounds, delivery of drugs via the nasal route provides direct access to systemic absorption. 6
  • 7. Drugs for throat • Throat drugs are mainly use to stop cough reflex when the cough is non productive or harmful. It reduce runny nose and postnasal drip. Eg: Codeine (Opoid Antitussive) • Oral thrush or a sore throat can be treated easily with over-the-counter medicines. • Mouth wash, Throat lozenges and pastilles are commonly used. • Demulcents: sooth the throat and reduce afferent impulses from the inflamed and irritated pharyngeal mucosa. • Expectorants: drugs that increase bronchial secretion or reduce its viscosity, facilitating its removal by coughing. 7
  • 8. • ENT medications can be broken down into the following categories Corticosteroids Antihistamines Decongestants Antibiotics Antifungals 8
  • 9. Corticosteroids Drugs • Corticosteroids are frequently used in a wide range of ear-nose-throat (ENT) conditions due to their anti-inflammatory properties. Mechanism of Action: • Steroid acts on transcription proteins found inside the cytoplasm and causes a reduction in the amount of inflammatory cytokines secreted by the cell. Reduces the cells response to inflammation. • Due to this complex mechanism of action there is a time delay between the administration of the drug and its clinical activity. • They decrease inflammation and edema of the mucous membranes. 9
  • 10. Corticosteroid Drug for the Nose Intranasal (IN): (Spray or Drop) or Inhalation • Intranasally administered steroid should be lipophilic; First pass metabolism is avoided. • Very low dose is enough for local effect – reduced systemic toxicity. • Administered intranasally to treat allergic and nonallergic rhinitis. Example • Fluticasone • Beclomethasone • Beconase • Mometasone 10
  • 11. Topical: • Applied topically as a solution in the external ear canal to decrease inflammation associated with allergies or infections. Example • Betamethasone • Dexamethasone 11 Corticosteroid Drug for the Ears Ear drops: • Used to treat eczematous conditions of the skin lining of external canal, Myringitis granulosa, to reduce middle ear mucosal edema in active middle ear infections with central perforation.
  • 12. Indications • Acute allergic rhinitis • Acute sinusitis • Acute epiglottitis • Otitis externa – to reduce external canal inflammatory oedema • Sinonasal inflammatory polyposis • Acute sensorineural hearing loss (sudden deafness) • Nasal sarcoidosis • Acute stridor before tracheostomy • Chronic otitis media 12
  • 13. Common Side effects Complications Associated with • Short-term Use of Steroids • Long-term Use of Steroids Short-term Use of Steroids: • Hypothalamic-pituitary-adrenal axis suppression • Hyperglycemia • Gastrointestinal Disturbances • Psychiatric effects 13 Long-term Use of Steroids: • Osteoporosis • Cushingn Syndrome • Accelerated atherosclerosis • Early cataract • Skin thinning • Pupura
  • 14. Decongestant Drugs • Congestion in the nose, sinuses, and chest is due to swollen, expanded, or dilated blood vessels in the membranes of the nose and air passages. • These membranes, with a great capacity for expansion, have an abundant supply of blood vessels. • Once the membranes swell, you start to feel congested. 14
  • 15. • Decongestants help to shrink the blood vessels in the nasal membranes and allow the air passages to open up. 15
  • 16. Mechanism of Action of Decongestants Drugs • Produce vasoconstriction by stimulating alpha receptors in the smooth muscle around the blood vessels. • Decrease swelling of mucous membranes in the nose, sinuses, and pharynx, • Alleviate nasal stuffiness and sinus congestion • Allow secretions to drain • Help open up Eustachian tubes to the ears • Can be administered topically as nose drops or nasal sprays or orally. 16
  • 17. Example • Oxymetazoline • Terahydrolozine • Phenylephrine • Pseudoephedrine Indications • Nasal and eustachian tube congestion • Nasal stuffiness • Acute or chronic rhinitis • Sinusitis, allergic conditions • Before nasal diagnostic examination to improve visualization. 17
  • 18. Side Effect • Cardiac arrhythmias • Headache • Insomnia Contraindications • Severe hypertension • Coronary artery disease • Narrow angle glaucoma • Use with Nasal steroids • Pregnancy and lactation 18
  • 19. Antihistamine Drugs • Histamine is an important body chemical that is responsible for the congestion, sneezing, runny nose, and itching that a patient suffers with an allergic attack or an infection. • Antihistamine drugs block the action of histamine, therefore reducing these symptoms. • For the best result, antihistamines should be taken before allergic symptoms get well established, but they can also be very effective if taken after the onset of symptoms. 19
  • 20. 20
  • 21. Mechanisms of Action • Histamine released from mast cells in the tissues when an allergic reaction. • Causes vasodilation in which the blood vessels and mucous membranes become swollen and red. Irritates the tissue directly, causing pain and itching. • Antihistamines acts by blocking H1 histamine receptor sites, thereby blocking the effects of histamine on H1-receptors on the Nose and Throat. • So block the action of histamine at H1 receptors to: • Dry up secretion. • Shrink edematous mucous membranes • And Decrease itching and redness 21
  • 22. Example: • 1st Generation: Chlorpheniramine, Diphenhydramine, Brompheniramine • 2nd Generation: Cetirizine, Levocetirizine, Loratadine, Desloratadine Dosage form • Intranasal, Topical, and Oral preparations are available 22
  • 23. Indications • Allergic Rhinitis • Sneezing • Stuffiness • Itchy nose, and throat • Runny nose. Side Effects • Sedation (by 1st Generation drugs) • Dry Mouth • Drowsiness • Dizziness • Nausea and Vomiting 23
  • 24. Antibiotics Drugs Antibiotics for Ear Framycetin sulfate • Framycetin is a broad spectrum aminoglycoside antibiotic • framycetin appears to inhibit protein synthesis in susceptible bacteria by binding to ribosomal subunits. • Framycetin is not active against most anaerobic bacteria 24
  • 25. Gentamicin • Gentamicin is a protein synthesis inhibitor. • It binds the 30S bacterial ribosomal subunit and acts to inhibit the formation of the initiation complex, causes mRNA misreading leading to non-functional proteins. • It also induces the dissolution of polyribosomes during protein synthesis. • Aminoglycosides require oxygen for uptake into the bacterial cell. Thus, they are only active against aerobes. 25
  • 26. Antibiotics for Nose Chlorhexidine with neomycin • Chlorhexidine-neomycin is an antibiotic available in nasal topical form only. • It is used to treat minor nasal infection with, and carriage of, Staphylococci bacteria. • Chlorhexidine gluconate is an antiseptic that kills a wide range of bacteria and yeasts, and some fungi and viruses. • Neomycin sulphate is an antibiotic of the aminoglycoside type. It rapidly kills bacteria by interfering with the production of proteins that the bacteria need to divide and multiply. 26
  • 27. Mupirocin • Mupirocin is an antibiotic. • It is used inside the nose to treat infections that are caused by certain bacteria. • This helps prevent the spread of infection to patients and health care workers during outbreaks at institutions. 27
  • 28. Antibiotics for Oropharyngeal Doxycycline • Doxycycline is a tetracycline antibiotic that fights bacteria in the body. • Doxycysline reversiably bind to 30s subunit at A site. And Block the binding of aminoacyl t-RNA to m-RNA. • Inhibit the addition of new aminoacid to growing peptide chain. And Stop the translation process, new protein cannot be made. 28
  • 29. Antifungal Drugs • Fungal infections of the mouth are usually caused by Candida spp. (candidiasis or candidosis). • Different types of oropharyngeal candidiasis are managed as follows: • Thrush • Acute erythematous candidiasis • Denture stomatitis • Chronic hyperplastic candidiasis • Angular cheilitis 29
  • 30. Drugs used in oropharyngeal candidiasis Miconazole • Miconazole inhibits the fungal enzyme 14α-sterol demethylase, resulting in a reduced production of ergosterol. • In addition to its antifungal actions, miconazole, similarly to ketoconazole, is known to act as an antagonist of the glucocorticoid receptor 30
  • 31. Nystatin • nystatin is an ionophore. It binds to ergosterol, a major component of the fungal cell membrane. • When present in sufficient concentrations, it forms pores in the membrane that lead to K+ leakage, acidification, and death of the fungus. • Nystatin when taken by mouth is used to treat yeast infections in the mouth or stomach. • Oral nystatin is not absorbed into your bloodstream and will not treat fungal infections in other parts of the body or on the skin. • Too toxic for synthetic use, Used only topically 31
  • 32. References • Abbasi, A. Al. (2017). Hand book of otolaryngology. September. • Bade, D., K. G., S., L. J., K., M. S., R., V. S., H., & A. N., P. (2020). A cross sectional study on prescription pattern of drugs in upper respiratory tract infections in a tertiary care hospital. International Journal of Basic & Clinical Pharmacology, 9(2), 271. • Daniel, M., Bharathi, D. R., Nataraj, G. R., & Jinil, A. L. (2018). Drug Utilization Trends in ENT Outpatients. 3(December), 166–171. • Klein, J. O. (1980). Principles and Practice of Infectious Disease. Annals of Internal Medicine, 92(5), 728. • Paterson, S. (2016). Topical ear treatment – options, indications and limitations of current therapy. Journal of Small Animal Practice, 57(12), 668–678. • World Health Organization. (2004). The global burden of disease 2004. Update, World Health Organization, 146. 32