ent pharmacology

ENT disorders

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

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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