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OBAT PADA GANGGUAN SISTEM PERNAFASAN dan Astma. Infeksi saluran pernafasan atas (ISPA) termasuk flu, rinitis akut, sinusitis, tonsillitis akut dan laryngitis.

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Presentasi berjudul: "OBAT PADA GANGGUAN SISTEM PERNAFASAN dan Astma. Infeksi saluran pernafasan atas (ISPA) termasuk flu, rinitis akut, sinusitis, tonsillitis akut dan laryngitis."— Transcript presentasi:

1 OBAT PADA GANGGUAN SISTEM PERNAFASAN dan Astma

2 Infeksi saluran pernafasan atas (ISPA) termasuk flu, rinitis akut, sinusitis, tonsillitis akut dan laryngitis akut. Pilek adalah tipe infeksi saluran nafas atas yang paling sering ditemukan.

3 Saluran Pernapasan Saluran pernapasan dibagi dalam 2 golongan utama: 1. saluran pernapasan atas, terdiri dari lobang hidung, rongga hidung, faring, laring 2. saluran pernafasan bawah terdiri dari trachea, bronchi, bronchioles, alveoli dan membran alveouler – kapiler

4 Gangguan Saluran pernafasan () : Saluran pernafasan atas Jenis-jenis infeksi saluran pernafasan atas : batuk pilek, faringitis, sinusitis, dan tonsilitis. Saluran pernafasan bawah Jenis infeksi saluran pernafasan bawah : asma, bronchitis kronik, emfizema, bronkioklialis.

5 Obat Saluran Pernafasan. Antihistaminika. Semua antihistamin memberi manfaat potensial pada terapi alergi nasal, rhinitis alergik. Antihistamin mengurangi rasa gatal pada hidung yang menyebabkan penderita bersin banyak obat-obat flu yang dapat dibeli bebas mengandung antihistamin, yang dapat menimbulkan rasa mengantuk. Antikolinergik Sifat antikolinergik pada kebanyakan antihistamin menyebabkan mulut kering dan pengurangan sekresi, membuat zat ini berguna untuk mengobati rhinitis yang ditimbulkan oleh flu.

6 Bronchial Asthma Therapeutic management: -Allergic control to prevent attacks. -Drug therapy: B- adrenergic, Theophyllin, & corticosteroids preparations + chest physiotherapy (only in between attacks).

7 Difenhidramin ( Benadryl ) D : PO : mg, setiap 4-6 jam D : PO, IM, IV : 5 mg/kg/h dalam 4 dosis terbagi, tidak lebih dari 300 mg/hari D : IM:IV: mg dosis tunggalIM:IV Batuk Karena Alergi

8 Klorfenilamin maleat (CTM) DWS: PO : 2-4 mg, setiap 4-6 jam Anak: 6-12 thn: 2 mg, setiap 4-6 jam Anak: 2-6 thn: PO, 1 mg, setiap 4-6 jam

9 Antihistamin lain Fenotiasin Prometazine Timeprazine Turunan piperazine hydroxyzine

10 Mukolitik Mukolitik berkerja dengan mencairkan dan mengencerkan secret mukosa yang kental sehingga dapat dikeluarkan. Efek samping yang paling sering terjadi adalah mual dan muntah, maka penderita tukak lambung perlu waspada. Wanita hamil dan selama laktasi boleh menggunakan obat ini. Contoh obat : ambroxol, bromheksin. Dosis: * ambroksol: dewasa dan anak-anak >12 thn, sehari 3 x 30 mg untuk 2-3 hari pertama. Kemudian sehari 3 x 15 mg. Anak-anak 5-12 thn, sehari 2-3 x 15 mg Anak 2-5 thn, sehari 3 x 7,5 mg (2,5 ml sirop) Anak * bromheksin: oral 3-4 dd 8-16 mg (klorida) anak-anak 3 dd 1,6-8 mg.

11 Inhalasi Inhalasi adalah suatu cara penggunaan adrenergika dan kortikosteroida yang memberikan beberapa keuntungan. Efeknya lebih cepat, dosisnya jauh lebih rendah dan tidak diresorpsi ke dalam darah sehingga resiko efek sampingnya ringan sekali. Dalam sediaan inhalasi, obat dihisap sebagai aerosol (nebuhaler) atau sebagai serbuk halus (turbuhaler). Inhalasi dilakukan 3-4 kali sehari 2 semprotan, sebaiknya pada saat-saat tertentu, seperti sebelum atau sesudah mengelularkan ternaga, setelah bersentuhan dengan zat- zat yang merangsang (asap rokok, kabut, alergan, dan saat sesak napas). Contoh obat : minyak angin (aromatis), Metaproterenol dosis: isoproterenol atau isuprel: mg setiap 6-8 jam (dewasa) mg setiap 6-8 jam.

12 Kromoglikat Kromoglikat sangat efektif sebagai obat pencegah serangan asma dan bronchitis yang bersifat alergis, serta konjungtivitis atau rhinitis alergik dan alergi akibat bahan makanan. ] Efek samping berupa rangsangan lokal pada selaput lender tenggorok dan trachea, dengan gejala perasaan kering, batuk-batuk, kadang- kadang kejang bronchi dan serangan asma selewat. Wanita hamil dapat menggunakan obat ini. Contoh obat : Natrium kromoglikat dipakai untuk pengobatan, pencegahan pada asma bronchial dan tidak dipakai untuk serangan asma akut. Metode pemberiannya adalah secara inhalasi dan obat ini dapat dipakai bersama dengan adrenergic beta dan derivat santin. Obai ini tidak boleh dihentikan secara mendadak karena dapat menimbulkan serangan asma.,

13 Kortikosteroid Kortikosteroid berkhasiat meniadakan efek mediator, seperti peradangan dan gatal-gatal. Penggunaannya terutama bermanfaat pada serangan asma akibat infeksi virus, selain itu juga pada infeksi bakteri untuk melawan reaksi peradangan. Untuk mengurangi hiper reaktivitas bronchi, zat-zat ini dapat diberikan per inhalasi atau peroral. Penggunaan oral untuk jangka waktu lama hendaknya dihindari, karena menekan fungsi anak ginjal dan dapat mengakibatkan osteoporosis. Contoh obat : hidrokortison, deksamethason, beklometason, budesonid.

14 Antiasma dan Bronkodilator Teofilin Terdapat bersama kofein pada daun the dan memiliki sejumlah khasiat antara lain spamolitis terhadap otot polos khususnya pada bronchi, menstimuli jantung dan mendilatasinya serta menstimulasi SSP dan pernapasan. Reabsorpsi nya di usus tidak teratur. Efek sampingnya yang terpenting berupa mual dan muntah baik pada penggunaan oral maupun parienteral. Pada overdosis terjadi efek sentral (sukar tidur, tremor, dan kompulsi) serta gangguan pernapasan juga efek kardiovaskuler. Dosis: 3-4 dd mg microfine (retard) Teofilin dapat diberikan dengan cara injeksi dalam bentuk aminofilin, suatu campuran teofilin dengan etilendiamin. Stimulan adrenoseptor, contoh obat salbutamol, terbutalin sulfat, efedrin hidroklorida.

15 Obat-obat batuk Antitussiva (L. tussis = batuk) digunakan untuk pengobatan batuk sebagai gejala dan dapat di bagi dalam sejumlah kelompok dengan mekanisme kerja yang sangat beraneka ragam, yaitu : Zat pelunak batuk (emolliensia, L. mollis = lunak ), yang memperlunak rangsangan batuk, melumasi tenggorokan agar tidak kering, dan melunakkan mukosa yang teriritasi. Banyak digunakan syrup (thyme dan althea), zat-zat lender (infus carrageen) Ekspektoransia (L. ex = keluar, pectus = dada) : minyak terbang, guajakol, radix ipeca (dalam tablet / pelvis doveri) dan ammonium klorida (dalam obat batuk hitam, Sehingga mempermudah pengeluarannya ketika batuk. Mukolotika : asetilsistein, bromheksin, dan ambroksol, zat-zat ini berdaya merombak dan melarutkan dahak ( L. mucus = lender, lysis = melarutkan),

16 Zat pereda : kodein, noskapin, dekstometorfan, dan pentoksiferin, obat-obat dengan kerja sentral ini ampuh pada batuk kering yang mengelitik. Antihistaminika : prometazin, difenhidramin, dan klorfeniramin. Obat ini dapat menekan perasaan mengelitik di tenggorokan. Anastetika lokal : pentoksiferin. Obat ini menghambat penerusan rangsangan batuk ke pusat batuk.

17 Penggolongan lain dari antitussiva menurut tempat kerja: Zat-zat sentral SSP Menekan rangsangan batuk di pusat batuk (medula), dan mungkin juga bekerja terhadap pusat saraf lebih tinggi (di otak) dengan efek menenangkan. – Zat adiktif : Doveri, kodein, hidrokodon dan normetadon. – Zat nonadiktif : noskapin, dekstrometorfan, pentoksiferin. Zat-zat perifer di luar SSP Emolionsia, ekspektoransia, mukolitika, anestetika local dan zat-zat pereda.

18 Beta1,2 selekstif pada pengobatan astma

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20

21 Obat Gangguan Saluran Nafas GENERIC:Albuterol BRAND:Proventil, Ventolin CLASS:Sympathomimetic

22 Albuterol Actions 1.Agonist for Beta 2 adrenergic receptors; relaxing bronchial smooth muscle which results in bronchodilation 2.Minimal cardiac side effects

23 Albuterol Indications: 1.Treatment of bronchospasm associated with asthma, chronic bronchitis and emphysema 2.Prevention of exercise-induced bronchospasm

24 Albuterol Contraindications: 1.Hypersensitivity to sympathomimetics 2.Cardiac dysrhythmia 3.Tachycardia and tachydysrhythmias

25 Albuterol Adverse Reactions: 1.Excessive use may cause paradoxical bronchospasm and arrhythmias 2.Tachycardia, palpitations, angina, PVCs, hypotension, and hypertension 3.Tremors 4.Hyperglycemia 5.Peripheral vasodilation 6.Nervousness 7.Nausea/Vomiting

26 Albuterol Precautions: 1.Diabetes 2.Hyperthyroidism 3.Cerebrovascular disease 4.Seizure disorders

27 Albuterol Dose: 1.2 inhalations with metered-dose inhaler, q 4-6 hours 2.3 ml premixed bullet in nebulizer

28 Albuterol Incompatible/Reactions: 1.Tricyclic antidepressants/monoamine oxidase inhibitors (MAOIs), may increase the effect of this drug 2.Other sympathomimetics 3.Beta blockers inhibit the effects

29 Albuterol Notes: Onset:5-15 minutes Peak:30 minutes – 2 hours Duration:3-4 hours 1.Can be delivered by inhaler and nebulizer 2.Metabolized in the liver and excreted in the urine

30 Epinephrine BRAND:Adrenalin CLASS:Sympathomimetic/Catecholamine

31 Epinephrine Kerja: 1.Direct effect on alpha and beta adrenergic receptor sites 2.Effects include: Alpha: bronchial, cutaneous, renal and visceral arteriolar constriction Beta 1: positive inotropic and chronotropic actions, increases automaticity Beta 2: bronchial smooth muscle relaxation and dilation of skeletal vasculature 3. Inhibits the release of histamine

32 Epinephrine Indikasi: 1.Cardiac arrest in general 2.Ventricular fibrillation 3.Asystole 4.Pulseless electrical activity 5.Infusion for profound hypotension associated with bradycardias, in combination with other pressors 6.Bronchospasm and bronchoconstriction of bronchial asthma and some forms of COPD 7.Anaphylaxis

33 Epinephrine kontraindikasi: 1.Uncorrected tachydysrhythmias 2.Underlying cardiovascular disease or hypertension 3.Glaucoma 4.Hypersensitivity to catecholamines 5.Hypothermia

34 Epinephrine/Adverse Reactions Hypertension Ventricular arrhythmias Pulmonary edema Tachycardia Palpitations Anxiety Psychomotor agitation Nausea/Vomiting Pupil dilation Angina Nervousness Headache Dizziness Tremors Hallucinations Cerebral hemorrhage Anorexia

35 Epinephrine Precautions: 1.Due to the possibility of cardiovascular disease, epinephrine should be administered with caution in patients over 35 years of age (with respiratory problems or if they are conscious) 2.The patient should be carefully monitored for changes in pulse, blood pressure, and ECG after administration of epinephrine. 3.Because of its strong inotropic and chronotropic effects, epinephrine causes an increased myocardial O2 demand

36 Epinephrine Precautions: 4.Hypovolemia (replenish volume first) 5.Diabetes mellitus 6.Hyperthyroidism 7.Prostatic hypertrophy 8.Must be protected from light 9.Tends to be deactivated by alkaline solutions (sodium bicarbonate) 10.Do not use with MAOIs or tricyclic antidepressants due to the danger of hypertensive crisis

37 Epinephrine Dose: 1.Cardiac dosage: 1:10,000 a. 1 mg q 3-5 minutes (until the heart restarts) b. Intermediate: 2-5 mg q 3-5 minutes c. Escalating: 1 mg – 3 mg – 5 mg; 3 minutes apart d. High: 0.1 mg/kg q 3-5 minutes 2.Infusion: Mix 1 mg in 250 ml and run at 2-10 mcg/min 3.Anaphylaxis and Asthma:.1-.5 mg (1:1,000) SQ or IM

38 Epinephrine Incompatible/Reactions: 1.Potentiates other sympathomimetics 2.Patients on MAOIs, antihistamines, and tricyclic antidepressants may have heightened effects 3.Sodium bicarbonate – deactivates epinephrine 4.Nitrates 5.Lidocaine 6.Aminophylline 7.Don’t mix the above drugs in the same syringe with epi; but can use in the same IV line – just flush between meds

39 Epinephrine Notes: ONSET:Immediate PEAK:Minutes DURATION:Several minutes

40 Isoetharine BRAND:Bronkosol, Bronkometer CLASS:Sympathomimetic

41 Isoetharine Actions: 1. Beta 2 agonist (slight specificity); relaxes smooth muscle of bronchioles, vasculature, uterus

42 Isoetharine Indications: 1. Relieve bronchospasm associated with asthma, chronic bronchitis, and emphysema

43 Isoetharine Contraindications: 1.Hypersensitivity to sympathomimetics 2.Cardiac dysrhythmias 3.Tachycardia and tachydysrhythmias

44 Isoetharine Adverse Reactions: 1.Dose-related tachycardia, palpitations, tremors, nervousness, peripheral vasodilation, nausea/vomiting, transient hyperglycemia, life-threatening arrhythmias; multiple excessive doses can cause paradoxical bronchoconstriction 2.Angina 3.Hypertension 4.Headache, dizziness, anxiety, restlessness, hallucinations

45 Isoetharine Precautions: 1.Use with caution in patients with diabetes, hyperthyroidism, cardiovascular and cerebrovascular disease 2.Seizure disorders 3.Isoetharine contains acetone sodium bisulfite; a sulfite that may cause allergic-type reactions, including anaphylactic symptoms in certain susceptible individuals

46 Isoetharine Dose: ADULT 1-2 inhalations with metered-dose inhaler 3-7 inhalations, via hand nebulizer q 4 hours PEDIATRIC Not recommended in children less than 12 years

47 Isoetharine Incompatible/Reactions: 1. Additive adverse effects with other beta agonists

48 Isoetharine Notes: ONSET:Immediate PEAK:5-15 minutes DURATION:1-4 hours

49 Metaproterenol Sulfate BRAND:Alupent, Metaprel CLASS:Sympathomimetic

50 Metaproterenol Sulfate Actions: 1. Agonist for Beta 2 adrenergic receptors – acts directly on smooth muscle

51 Metaproterenol Sulfate Indications: 1. Relieve bronchospasm of COPD and Asthma

52 Metaproterenol Sulfate Contraindications: 1.Hypersensitivity to sympathomimetics 2.Hyperthyroidism 3.Cerebrovascular or cardiovascular disorders 4.Tachycardia and tachydysrhythmias

53 Metaproterenol Sulfate Adverse Reactions Dose-related tachycardia Palpitations Nervousness Peripheral vasodilation Excessive use – lethal arrhythmias, paradoxical bronchospasm Hypertension Tremors, headache, dizziness, anxiety, hallucinations Nausea/vomiting

54 Metaproterenol Sulfate Precautions: 1.History of cardiovascular disease or hypertension 2.Seizures

55 Metaproterenol Sulfate Dose: ADULT: 2-3 inhalations, q 3-4 hours Metered-dose inhaler or nebulizer PEDIATRICS: Not recommended in children under 12 years

56 Metaproterenol Sulfate Incompatible/Reactions: 1.Beta blockers 2.MAOIs, tricyclic antidepressants 3.Potentiates other beta agonists

57 Metaproterenol Sulfate Notes: ONSET:1 minute PEAK:1 hour DURATION:1-5 hours with single dose 2-5 hours with repeated dose

58 GENERIC:Terbutaline Sulfate BRAND:Bricanyl, Brethine CLASS:Sympathomimetic

59 Terbutaline Sulfate Actions: 1.Beta 2 agonist – has an affinity for beta 2 receptors of bronchial, vascular, and uterine smooth muscle 2.At increased doses, beta 1 effects may occur

60 Terbutaline Sulfate Indications: 1.Relieve bronchospasm associated with asthma, chronic bronchitis and emphysema (prevalent in patients over the age of 40 or with coronary artery disease) 2.Used in-hospital to stop pre-term labor

61 Terbutaline Sulfate Contraindications: 1.Hypersensitivity to sympathomimetics 2.Cardiac dysrhythmias 3.Tachycardia and tachydysrhythmias 4.Glaucoma

62 Terbutaline Sulfate Adverse Reactions: 1.Tachycardia, tremors, palpitations, nervousness and dizziness 2.Angina, PVCs, hypotension, and hypertension 3.Headache, anxiety, hallucinations 4.Nausea, vomiting 5.Bronchospasm

63 Terbutaline Sulfate Precautions: 1.Used with caution to patients with a history of cardiovascular disease or hypertension 2.Seizure disorders 3.Thyroid disease 4.Diabetes

64 Terbutaline Sulfate Dose: ADULT: 0.25 mg SQ; repeat in minutes 2 inhalations separated by a 60 second interval with a metered dose inhaler 4mg/7ml nebulizer mix

65 Terbutaline Sulfate Incompatible/Reactions: 1.Alkaline solutions 2.Degrades when exposed to light for long periods of time

66 Terbutaline Sulfate Notes: ONSET:15 minutes PEAK:30-60 minutes DURATION:90 minutes – 4 hours

67 Theophylline Ethylenediamine BRAND:Aminophylline CLASS:Methylxanthine Spasmolytic

68 Theophylline Actions: 1.Beta 2 agonist; directly relaxes bronchial smooth muscle 2.Dilates pulmonary and coronary arterioles, decreasing pulmonary hypertension and increasing coronary blood flow 3.Slight positive chronotropic and inotropic effects 4.Strengthens diaphragmatic contractions by affecting intracellular calcium 5.Mild diuretic

69 Theophylline Actions: 6.Stimulates CNS vomiting centers 7.Respiratory center stimulant 8.Stimulates vagal and vasomotor centers in the brain – can lead to decreased heart rate, vasoconstriction in the brain – depends on CNS or peripheral predominance

70 Theophylline Indications: 1.Relieve bronchospasm associated with asthma, chronic bronchitis, emphysema, and pulmonary edema 2.Management of CHF and pulmonary edema

71 Theophylline Contraindications: 1.Hypersensitivity to xanthene compounds (e.g. caffeine) 2.Cardiac dysrhythmias 3.Tachycardia and tachydysrhythmias

72 Theophylline Adverse Reactions Nausea/vomiting Hypotension Irritability Tachycardia Angina Flushing Diarrhea Increased respiratory rate Cardiac arrhythmias Tremors Seizures Palpitations Hypertension Anorexia

73 Theophylline Precautions: 1.Caution if patient is already taking theophylline-containing medications 2.Caution to patients with a history of cardiovascular disease or hypertension 3.Thyroid disease 4.Active peptic ulcer 5.Hypotension may occur following rapid administration 6.May oppose the effects of beta blockers

74 Theophylline Dose: ADULT: Loading dose of 6 mg/kg IV infusion over 20 minutes Loading dose of 1 mg/kg IV infusion over 20 minutes if the patient has had theophylline products in the last 35 hours

75 Theophylline Incompatible/Reactions: 1.Incompatible with most drugs 2.Simetidine, propranolol, erythromycin, and troleandomycin may increase the effects of the drug 3.Barbiturates, phenytoin, and smoking may decrease blood levels 4.May increase the effects of anticoagulants

76 Theophylline Notes: ONSET:15 minutes: PEAK:30 minutes – 1 hour DURATION:Averages 5 hours 1.Common forms or oral aminophylline include: * Marax* Primatene * Quibron* Slo-Phyllin * Slobid* Somophyllin * Tedral* Theo-Dur

77 Respiratory Medications Respiratory meds are used for several purposes, the most obvious is the treatment of asthma. Class includes: 1.Cough suppressants 2.Nasal decongestants 3.Antihistamines

78 Antiasthmatic Medications Asthma has two basic pathophysiologies: 1.Bronchoconstriction 2.Inflammation Treatment is aimed to relieve bronchospasm and decrease inflammation. Specific approaches are categorized as beta 2 selective sympathomimetics, nonselective sympathomimetics, methylxanthines, anticholinergics, glucocorticoids and leukotriene antagonists.

79 Beta 2 Specific Agents Albuterol (Proventil, Ventolin) is the prototype of this class. 1.These agents relax bronchial smooth muscle, resulting in bronchodilation and relief from bronchospasm. 2.These agents are first line therapy for acute shortness of breath. 3.Administered via metered dose inhaler or nebulizer. 4.Overall, these agents are very safe.

80 Nonselective Sympathomimetics Stimulate both beta 1 and beta 2 receptors, as well as alpha receptors. Rarely used to treat asthma because they have the undesired effects of increased peripheral vascular resistance and increased risks for tachycardias and other dysrhythmias. Agents include: epinephrine, ephedrine, and isoproterenol Epinephrine is the only nonselective sympathomimetic in common use today.

81 Methylxanthines CNS stimulants that have additional bronchodilatory properties. Used only when other drugs such as beta 2 specific agents are ineffective. Possibly block adenosine receptors. Prototype is theophylline, taken orally. Aminophylline, an IV medication, is rapidly metabolized into theophylline and, therefore, has identical effects. Chief side effects: nausea/vomiting, insomnia, restlessness, and dysrhythmias

82 Anticholinergics Ipratropium (Atrovent) is an atropine derivative given by nebulizer. Because stimulating the muscarinic receptors in the lungs results in constriction of bronchial smooth muscle, ipratropium, a muscarinic antagonist, causes bronchodilation. Ipratropium is inhaled, and has no systemic effects. Has an additive effect when used with beta 2 agonists. Most common side effect is dry mouth

83 Glucocorticoids Anti-inflammatory properties. Lower the production and release of inflammatory substances such as histamine, prostaglandins, and leukotrienes, and reduce mucus and edema secondary to decreasing vascular permeability. May be inhaled or taken orally, as well as IV. Prototype of inhaled glucocorticoid is beclomethasone. Prototype of oral glucocorticoid is prednisone. Administered as preventative care.

84 Glucocorticoids When inhaled they cause few side effects. Side effects are due mostly to direct exposure on the oropharynx, and gargling after taking the drug can decrease the side effects. Side effects from the IV administrations of methylprednisolone in emergencies are not likely Long periods of administration can lead to adrenal suppression and hyperglycemia. Another anti-inflammatory agent used is cromolyn (Intal), an inhaled powder.

85 Glucocorticoids Cromolyn is the safest of all antiasthma agents. Only side effects are coughing or wheezing due to local irritation caused by the powder. Often used for preventing asthma in adults and children.

86 Leukotriene Antagonists Leukotrienes are mediators released from mast cells upon contact with allergens. Contribute powerfully to both inflammation and bronchoconstriction Can either block the synthesis of leukotrienes or block their receptors. Zileuton (Zyflo) is the prototype of those that block the synthesis of leukotrienes Zafirlukast (Accolate) is the prototype of those that block their receptors

87 DRUGS USED FOR RHINITIS AND COUGH Rhinitis: (inflammation of the nasal lining) comprises a group of symptoms including nasal congestion, itching, redness, sneezing, and rhinorrhea (runny nose). Allergic reactions or viral infections may cause it Drugs that treat the symptoms of rhinitis and cold are commonly found in over-the-counter remedies. Nasal decongestants, antihistamines, and cough suppressants are available in prescription medications.

88 Nasal Decongestants Nasal congestion is caused by dilated and engorged nasal capillaries. Drugs that constrict these capillaries are effective nasal decongestants. Main pharmacologic classification in this functional category is alpha 1 agonists Alpha 1 agonists may be given either topically or orally Examples of agents: phenylephrine, pseudoephedrine, and phenylpropanolamine, (administered in drops or mist)

89 Antihistamines Arrest the effects of histamine by blocking its receptors. Histamine is an endogenous substance that affects a wide variety of organs systems. Noted for its role in allergic reaction. Histamine binds with H1 receptors to cause vasodilation and increased capillary permeability (vasculature) In the lungs, H1 receptors cause bronchoconstriction In the gut, H2 receptors cause an increase in gastric acid release Histamine also acts as a neurotransmitter in the CNS.

90 Antihistamines Histamine is synthesized and stored in two types of granulocytes; tissue-bound mast cells and plasma-bound basophils Both types are full of secretory granules, which are vesicles containing inflammatory mediators such as histamine, leukotrienes, and prostaglandins, among others. When cells are exposed to allergens, they develop antibodies on their surfaces. On subsequent exposures, the antibodies bind with their specific allergen.

91 Antihistamines Secretory granules then migrate towards the cell’s exterior and fuse with the cell membrane. Causing them to release their contents. Histamines are useful in our immune systems. When our immune systems overreact do allergies such as hay fever or cedar fever send us running for the antihistamines Typical symptoms of allergic reaction include most of those associated with rhinitis. Severe allergic reactions (anaphylaxis) may cause hypotension

92 Antihistamines Antihistamines are at best only a secondary drug for treating anaphylaxis. Just as there are H1 and H2 histamine receptors, there are H1 and H2 histamine receptor antagonists. Most old antihistamines were H1 receptor antagonists, newer antihistamines are H2 receptor antagonists. Chief side effect is sedation (H1), newer generation do not cause this sedation effect (H2). First generation medications: alkylamines (chlorpheniramine [Chlor-Trimeton]), ethanolamines (diphenhydramine [Benadryl])

93 Antihistamines Other first generation antihistamines: clemastine (Tavist), and phenothiazines (promethazine [Phenergan]). Some antihistamines also have significant anticholinergic properties: promethazine and dimenhydrinate (Dramamine), used for motion sickness. Second generation antihistamines include: terfenadine (Seldane), loratadine (Claritine), cetirizine (Zyrtec, and fexofenadine (Allegra). These agents do not cross the blood-brain barrier and therefore do not cause sedation.

94 Cough Suppressants Coughing is a complex reflex that depends on functions in the CNS, the PNS, and the respiratory muscles. It is a defense mechanism that aids the removal of foreign particles like smoke and dust. In general, treating a productive cough is not appropriate, as it is performing a useful function. An unproductive cough, usually results from an irritated oropharynx and can be troublesome. The three classifications of cough suppressants include one that is supported by evidence and two that are not.

95 Cough Suppressants Antitussives 1.Suppress the stimulus to cough in the CNS. 2.This functional class includes two specific pharmacologic types: a. Opioids b. Nonopioids 3.Two most common opioid antitussives are codeine and hydrocodone 4.Both inhibit the stimulus for coughing in the brain but also produce varying degrees of euphoria

96 Penekan Batuk 5. antitussives nonopioid tidak memilki potensi untuk disalahgunakan. a. Dextromethoraphan b. Diphenhydramine c. Benzonatate (Tessalon) EKspektoran: dimaksud untuk mengurangi produksi batuk Mucolytics: membuat dahak lebih encer dan mudah dikeluarkan Masih sedikit data-data penekan batuk


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