Kuliah farmakologi blok THT

1. Pharmacology of ENT
M. Fadhol Romdhoni
Medical Faculty
University of Muhammadiyah of Purwokerto

2. ENT cases
• Swimmer’s ear / Otitis externa
• Otitis media
• Rinitis alergic
• Sinusitis
• Cold
• Inflamation
• Oral yeast infectioan
• Cough

3. Pharmacoterapy in ENT
1. Decongestan t
2. Antihistamin
3. Mast cell stabilizer
4. Corticosteroid  Blok Endokrin
5. Anti yeast  Blok Imuninfeksi
6. Antibiotic  Blok Imuninfeksi
7. Antitusif  Blok Respirasi
8. Analgesik  Blok Muskuloskeletal
9. Ceruminolitic

4. Decongestant

5. Nasal Decongestant:
Nasal decongestants are vasoconstrictive
drugs extremely useful as
nonprescription medication. Both oral
and topical dosage forms are often
chosen as therapy in the common cold.

6. Mechanism of action:
Nasal decongestants belong to the
pharmacological class of
sympathomimetic amines. Decongestant
stimulates alpha-adrenergic agonist, by
constriction of blood vessels, reducing
its supply to the nose, decrease the
amount of blood in sinusoid vessels and
decrease mucosal edema.

7. Types of nasal decongestant:
• Internally or systemic decongestant:
(e.g. pseudoephedrine,
phenylpropanolamine (PPA) and
phenylephrine).
• Topical decongestant: drops or sprays
(e.g. xylometazoline, phenylephrine,
oxymetazoline, naphazoline).
• Inhaler: (1-desoxyephedrine and
propylhexedrine).

8. Systemic nasal decongestant:
Mechanism of action:
Potent direct acting alpha-adrenergic
stimulator with weak beta-Adrenergic
activity, causes vasoconstriction of the
arterioles of the nasal mucosa and
conjunctive, activates the dilator muscle
of the pupil to causes contraction, and
produce systemic arterial
vasoconstriction.

9. Side effect of systemic decongestant:
• CNS effect: Nervousness, restlessness,
headach and insomnia.
• CV effect: increase blood pressure and
increase heart rate.
• Urinary sphincter constriction

10. Examples of systemic decongestant:
– Pseudoephedrine
– Phenylpropanolamine (PPA)
– phenylephrine

11. Topical Nasal Decongestant:
Include:
sprays,
drops,
inhalers

12. 1- sprays:
Its advantages:
• Have fast onset of action.
• Cover large surface area.
• Simple to use.
• Inexpensive.
Its disadvantage:
• Imprecise dosage
• Tendency for tip the bottle to become
clogged.

13. 2- drops:
It preferred for small children.
Its disadvantage:
– High risk of contamination.
– Limited coverage into nasal mucosa.
– Easy passage into larynx.

14. 3- inhaler:
Easy to be handle and carry.

15. Side effect of topical decongestant:
• Local irritation.
• Rebound congestion

16. Example of topical decongestant:
Ephedrine HCL, Xylometazoline HCL,
Oxymetazoline HCL, Ipratropium bromide
(antimuscarinic).

17. Antihistamin
General Mechanism of Action of Antihistamines
• Blocks action of histamine at receptor
• Competes with histamine for binding
• Displaces histamine from receptor
• Most beneficial when given early

18. Example of antihistamin
• First generation
– Alkylamines 
Chlorpheniramine
maleate
– Ethanolamines 
Diphenhydramine HCl
– Ethylenediamines 
Tripelennamine
– Piperazines 
Azatadine
– Phenothiazines 
Promethazine HCl
– Piperadines 
Hydroxyzine HCl
• Second generation
– Terfenadine
– Fexofenadine HCl
– Loratadine
– Cetirizine

19. Toxic Reactions & Side Effects of H1 Blockers
1. CNS depression (mainly in first generation agents).
2. Allergic reactions (topical application).
3. Appetite loss, nausea and vomiting, constipation or
diarrhea.
4. Insomnia, tremors, nervousness, irritability,
tachycardia, dry mouth, blurred vision, urinary
retention, constipation (1st generation).
5. CNS stimulation with hallucinations, motor
disturbances (tremors and convulsions), and death.
6. Secreted in breast milk and can cross the placenta.

20. Drug Interactions of H1 Blockers
• Antihistamines that produce sedation can
potentiate CNS depressants (e.g., barbiturates,
opiates, general anesthetics, and alcohol)
• Antihistamines that possess anticholinergic
actions can produce manifestations of
excessive blockade if given with anticholinergic
drugs (e.g., dry mouth, constipation, or blurred
vision)

21. Second Generation Antihistamines
• Generally do not cause the sedation
• Do not cross the blood-brain barrier as readily
as First Generation compounds
• Lipophobicity
• Large molecular size

22. Mast Cell Stabilizers
• β2-adrenergic agonists
• Cromoglicic acid
• Ketotifen
• Methylxanthines
• Olopatadine
• Omalizumab
• Pemirolast
• Quercetin

23. Corticosteroid
• Act by inhibiting the body's immune
response. They decrease inflammation
and edema of the mucous membranes.
Have no decongestant or antihistamine
effect. Not used to treat the common
cold.

24. Example of Corticosteroid Drugs
• Beclomethasone  for nasal
• Mometasone  for nasal
• Dexamethasone  for ear

25. Antiyeast
• Yeasts, which are one-celled organisms that
are closely related to fungi, grow easily in the
warm, moist, dark environment of the mouth.
This is especially true in patients whose
immune systems are compromised by disease.
Candida albicans yeast infections of the mouth
are also known as oral candidiasis (thrush) or
monilia.

26. Example of Antiyeast Drug
• Nystatin
• Mycostatin

27. Antitusive
• Decrease coughing by suppressing the cough
center in brain or anesthetizing stretch
receptors in respiratory tract. Main purpose is
to control dry, nonproductive coughs. Not
prescribed to treat a productive cough.

28. Example of Antitusive Drug
• Detromethorphan
• Codein

29. Ceruminolytic
Hidrogen peroksida 3 %
Fenolgliserin

30. Obat tetes telinga
Dibuat dalam bentuk sediaan khusus untuk
telinga dgn pembawa yang mudah menyebar
ke dalam liang telinga.
Obat telinga tidak boleh digunakan untuk
jangka panjang karena bisa menimbulkan
ototoksik dan superinfeksi.
Bila infeksi disebabkan oleh jamur/virus tidak
boleh menggunakan obat telinga yang
mengandung antibiotika karena bisa
menimbulkan superinfeksi.
Supplement

31. Cara menggunakan obat tetes telinga
1. Cuci tangan dengan air dan sabun.

32. 2. Pastikan kondisi ujung botol atau pipet
tetes tidak rusak.

33. 3. Bersihkan telinga bagian luar dengan
menggunakan air hangat atau kain
lembab dengan hati-hati, kemudian
dikeringkan

34. 4. Hangatkan obat tetes telinga dengan
memegang botolnya menggunakan tangan
selama bbrp menit.Kocok botol obat tetes.

35. 5. Miringkan kepala sehingga telinga yang
akan diberikan obat menghadap ke
atas

36. 6.Teteskan obat sesuai dosis pd lubang telinga.
Pertahankan posisi kepala 2-3 menit. Tekan
tragus agar obat mencapai dasar saluran
telinga.

37. 7. Pasang kembali tutup botol tetes telinga
dengan rapat, jangan menyeka atau
membilas ujung botol tetes.

38. • 8.Cuci tangan dengan air dan sabun
untuk membersihkan sisa obat yang
mungkin menempel.

39. OBAT OTOTOKSIK
• Aminoglikosida
• Anti malaria
• Anti rematik
• Tuberkulostatik
• Anti kanker

40. Penggunaan Tetes Hidung
• 1. Blow the nose.
• 2. Sit down and tilt head backward strongly or lie
down with a pillow under the shoulders; keep head
straight.
• 3. Insert the dropper one centimeter into the
nostril.
• 4. Apply the amount of drops prescribed.

41. • 5. Immediately afterward tilt head forward strongly
(head between knees).
• 6. Sit up after a few seconds, the drops will then
drip into the pharynx.
• 7. Repeat the procedure for the other nostril, if
necessary.
• 8. Rinse the dropper with boiled water.

42. Penggunaan Nasal Spray
• 1. Blow the nose.
• 2. Sit with the head slightly tilted forward.
• 3. Shake the spray.
• 4. Insert the tip in one nostril.
• 5. Close the other nostril and mouth.
• 6. Spray by squeezing the vial (flask, container) and
sniff slowly

43. • 7. Remove the tip from the nose and bend the
head forward strongly (head between the knees).
• 8. Sit up after a few seconds; the spray will drip
down the pharynx.
• 9. Breathe through the mouth.
• 10. Repeat the procedure for the other nostril, if
necessary.
• 11. Rinse the tip with boiled water

44. Contoh preparat

45. Wassalam…
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