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OBAT PADA GANGGUAN SISTEMPERNAFASAN dan Astma
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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.
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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
alveoulerkapiler
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Gangguan Saluran pernafasan () :
Saluran pernafasan atas
Jenis-jenis infeksi saluran pernafasan atas :batuk pilek, faringitis, sinusitis, dan toksilitis.
Saluran pernafasan bawahJenis infeksi saluran pernafasan bawah : asma,
bronchitis kronik, emfizema, bronkioklialis.
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Obat Saluran Pernafasan. Antihistaminika.
Semua antihistamin memberikan manfaat potensial pada terapi alerginasal, rhinitis alergik.
Antihistamin
mengurangi rasa gatal pada hidung yang menyebabkan penderitabersin banyak obat-obat flu yang dapat dibeli bebas mengandungantihistamin, yang dapat menimbulkan rasa mengantuk.
Antikolinergik
Sifat antikolinergik pada kebanyakan antihistamin menyebabkan mulutkering dan pengurangan sekresi, membuat zat ini berguna untukmengobati rhinitis yang ditimbulkan oleh flu.
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Bronchial Asthma
Therapeutic management:
- Allergic control to prevent attacks.
- Drug therapy:
B- adrenergic, Theophyllin, & corticosteroids
preparations + chest physiotherapy (only in
between attacks).
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Difenhidramin( Benadryl )
D : PO : 25-50 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: 10-50 mg dosis tunggal
Batuk Karena Alergi
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Klorfenilamin maleat
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
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Antihistamin lain
Fenotiasin
Prometazine
Timeprazine
Turunan piperazine
hydroxyzine
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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.
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InhalasiInhalasi adalah suatu cara penggunaan adrenergika dan
kortikosteroida yang memberikan beberapa keuntungan.Efeknya lebih cepat, dosisnya jauh lebih rendah dan tidakdiresorpsi ke dalam darah sehingga resiko efek sampingnyaringan sekali. Dalam sediaan inhalasi, obat dihisap sebagaiaerosol (nebuhaler) atau sebagai serbuk halus (turbuhaler).
Inhalasi dilakukan 3-4 kali sehari 2 semprotan, sebaiknya padasaat-saat tertentu, seperti sebelum atau sesudahmengelularkan ternaga, setelah bersentuhan dengan zat-zat yang merangsang (asap rokok, kabut, alergan, dan saatsesak napas).
Contoh obat : minyak angin (aromatis), Metaproterenol
dosis: isoproterenol atau isuprel: 10-20 mg setiap 6-8 jam(dewasa). 5-10 mg setiap 6-8 jam.
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Kromoglikat
Kromoglikat sangat efektif sebagai obat pencegah serangan asmadan bronchitis yang bersifat alergis, serta konjungtivitis atau rhinitisalergik dan alergi akibat bahan makanan. ]
Efek samping berupa rangsangan lokal pada selaput lender tenggorokdan trachea, dengan gejala perasaan kering, batuk-batuk, kadang-
kadang kejang bronchi dan serangan asma selewat. Wanita hamildapat menggunakan obat ini.
Contoh obat :
Natrium kromoglikat dipakai untuk pengobatan, pencegahan padaasma bronchial dan tidak dipakai untuk serangan asma akut.
Metode pemberiannya adalah secara inhalasi dan obat ini dapatdipakai bersama dengan adrenergic beta dan derivat santin. Obai initidak boleh dihentikan secara mendadak karena dapatmenimbulkan serangan asma.,
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Kortikosteroid
Kortikosteroid berkhasiat meniadakan efek mediator, sepertiperadangan dan gatal-gatal.
Penggunaannya terutama bermanfaat pada serangan asma
akibat infeksi virus, selain itu juga pada infeksi bakteri untukmelawan reaksi peradangan. Untuk mengurangi hiperreaktivitas bronchi, zat-zat ini dapat diberikan per inhalasi atauperoral.
Penggunaan oral untuk jangka waktu lama hendaknya
dihindari, karena menekan fungsi anak ginjal dan dapatmengakibatkan osteoporosis.
Contoh obat : hidrokortison, deksamethason, beklometason,budesonid.
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Antiasma dan BronkodilatorTeofilin
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. Padaoverdosis terjadi efek sentral (sukar tidur, tremor, dan kompulsi)
serta gangguan pernapasan juga efek kardiovaskuler.
Dosis: 3-4 dd 125-250 mg microfine (retard)
Teofilin dapat diberikan dengan cara injeksi dalam bentukaminofilin, suatu campuran teofilin dengan etilendiamin.
Stimulan adrenoseptor, contoh obat salbutamol, terbutalin sulfat,
efedrin hidroklorida.
b b b k
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Obat-obat batukAntitussiva (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),
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Zat pereda : kodein, noskapin, dekstometorfan,dan pentoksiferin , obat-obat dengan kerjasentral ini ampuh pada batuk kering yang
mengelitik. Antihistaminika : prometazin, difenhidramin, dan
klorfeniramin. Obat ini dapat menekan perasaanmengelitik di tenggorokan.
Anastetika lokal : pentoksiferin. Obat inimenghambat penerusan rangsangan batuk kepusat batuk.
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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 lebihtinggi (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 localdan zat-zat pereda.
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Beta1,2 selekstif pada pengobatan
astma
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Obat Gangguan Saluran Nafas
GENERIC: Albuterol
BRAND: Proventil, Ventolin
CLASS: Sympathomimetic
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Albuterol
Actions
1. Agonist for Beta 2 adrenergic receptors; relaxing bronchial
smooth muscle which results in bronchodilation
2. Minimal cardiac side effects
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Albuterol
Indications:
1. Treatment of bronchospasm associated with asthma,
chronic bronchitis and emphysema
2. Prevention of exercise-induced bronchospasm
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Albuterol
Contraindications:
1. Hypersensitivity to sympathomimetics
2. Cardiac dysrhythmia
3. Tachycardia and tachydysrhythmias
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Albuterol
Adverse Reactions:
1. Excessive use may cause paradoxical bronchospasm and
arrhythmias
2. Tachycardia, palpitations, angina, PVCs, hypotension, andhypertension
3. Tremors
4. Hyperglycemia
5. Peripheral vasodilation6. Nervousness
7. Nausea/Vomiting
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Albuterol
Precautions:
1. Diabetes
2. Hyperthyroidism
3. Cerebrovascular disease
4. Seizure disorders
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Albuterol
Dose:
1. 2 inhalations with metered-dose inhaler, q 4-6 hours
2. 3 ml premixed bullet in nebulizer
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Albuterol
Incompatible/Reactions:
1. Tricyclic antidepressants/monoamine oxidase inhibitors
(MAOIs), may increase the effect of this drug
2. Other sympathomimetics3. Beta blockers inhibit the effects
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Albuterol
Notes:
Onset: 5-15 minutes
Peak: 30 minutes2 hoursDuration: 3-4 hours
1. Can be delivered by inhaler and nebulizer
2. Metabolized in the liver and excreted in the urine
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Epinephrine
BRAND: Adrenalin
CLASS: Sympathomimetic/Catecholamine
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Epinephrine
Action:
1. Direct effect on alphaand betaadrenergic receptor sites
2. Effects include:
Alpha: bronchial, cutaneous, renal and visceral arteriolarconstriction
Beta 1: positive inotropic and chronotropic actions,
increases automaticity
Beta 2: bronchial smooth muscle relaxation and dilation ofskeletal vasculature
3. Inhibits the release of histamine
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Epinephrine
Indications:
1. Cardiac arrest in general
2. Ventricular fibrillation
3. Asystole4. Pulseless electrical activity
5. Infusion for profound hypotension associated with
bradycardias, in combination with other pressors
6. Bronchospasm and bronchoconstriction of bronchialasthma and some forms of COPD
7. Anaphylaxis
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Epinephrine
Contraindications:
1. Uncorrected tachydysrhythmias
2. Underlying cardiovascular disease or hypertension3. Glaucoma
4. Hypersensitivity to catecholamines
5. Hypothermia
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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
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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
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Epinephrine
Precautions:
4. Hypovolemia (replenish volume first)
5. Diabetes mellitus
6. Hyperthyroidism7. 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
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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 minutesc. Escalating: 1 mg3 mg5 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
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Epinephrine
Incompatible/Reactions:
1. Potentiates other sympathomimetics
2. Patients on MAOIs, antihistamines, and tricyclicantidepressants may have heightened effects
3. Sodium bicarbonatedeactivates epinephrine
4. Nitrates
5. Lidocaine
6. Aminophylline
7. Dont mix the above drugs in the same syringe with epi; butcan use in the same IV linejust flush between meds
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Epinephrine
Notes:
ONSET: Immediate
PEAK: Minutes
DURATION: Several minutes
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Isoetharine
BRAND: Bronkosol, Bronkometer
CLASS: Sympathomimetic
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Isoetharine
Actions:
1. Beta 2 agonist (slight specificity); relaxes smooth muscle of
bronchioles, vasculature, uterus
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Isoetharine
Indications:
1. Relieve bronchospasm associated with asthma, chronic
bronchitis, and emphysema
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Isoetharine
Contraindications:
1. Hypersensitivity to sympathomimetics
2. Cardiac dysrhythmias3. Tachycardia and tachydysrhythmias
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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
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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
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Isoetharine
Dose:
ADULT
1-2 inhalations with metered-dose inhaler3-7 inhalations, via hand nebulizer q 4 hours
PEDIATRIC
Not recommended in children less than 12 years
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Isoetharine
Incompatible/Reactions:
1. Additive adverse effects with other beta agonists
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Isoetharine
Notes:
ONSET: Immediate
PEAK: 5-15 minutes
DURATION: 1-4 hours
M l S lf
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Metaproterenol Sulfate
BRAND: Alupent, Metaprel
CLASS: Sympathomimetic
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Metaproterenol Sulfate
Actions:
1. Agonist for Beta 2 adrenergic receptorsacts directly on
smooth muscle
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Metaproterenol Sulfate
Indications:
1. Relieve bronchospasm of COPD and Asthma
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Metaproterenol Sulfate
Contraindications:
1. Hypersensitivity to sympathomimetics
2. Hyperthyroidism3. Cerebrovascular or cardiovascular disorders
4. Tachycardia and tachydysrhythmias
M t t l S lf t
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Metaproterenol Sulfate
Adverse Reactions
Dose-related tachycardia
Palpitations
Nervousness
Peripheral vasodilation
Excessive uselethal
arrhythmias, paradoxical
bronchospasm
Hypertension
Tremors, headache,
dizziness, anxiety,
hallucinations
Nausea/vomiting
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Metaproterenol Sulfate
Precautions:
1. History of cardiovascular disease or hypertension
2. Seizures
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Metaproterenol Sulfate
Dose:
ADULT:
2-3 inhalations, q 3-4 hoursMetered-dose inhaler or nebulizer
PEDIATRICS:
Not recommended in children under 12 years
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Metaproterenol Sulfate
Incompatible/Reactions:
1. Beta blockers
2. MAOIs, tricyclic antidepressants3. Potentiates other beta agonists
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Metaproterenol Sulfate
Notes:
ONSET: 1 minute
PEAK: 1 hour
DURATION: 1-5 hours with single dose
2-5 hours with repeated dose
GENERIC Terbutaline Sulfate
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GENERIC: Terbutaline Sulfate
BRAND: Bricanyl, Brethine
CLASS: Sympathomimetic
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Terbutaline Sulfate
Actions:
1. Beta 2 agonisthas an affinity for beta 2 receptors of
bronchial, vascular, and uterine smooth muscle
2. At increased doses, beta 1 effects may occur
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Terbutaline Sulfate
Indications:
1. Relieve bronchospasm associated with asthma, chronic
bronchitis and emphysema (prevalent in patients over theage of 40 or with coronary artery disease)
2. Used in-hospital to stop pre-term labor
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Terbutaline Sulfate
Contraindications:
1. Hypersensitivity to sympathomimetics
2. Cardiac dysrhythmias3. Tachycardia and tachydysrhythmias
4. Glaucoma
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Terbutaline Sulfate
Adverse Reactions:
1. Tachycardia, tremors, palpitations, nervousness and
dizziness2. Angina, PVCs, hypotension, and hypertension
3. Headache, anxiety, hallucinations
4. Nausea, vomiting
5. Bronchospasm
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Terbutaline Sulfate
Precautions:
1. Used with caution to patients with a history of
cardiovascular disease or hypertension2. Seizure disorders
3. Thyroid disease
4. Diabetes
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Terbutaline Sulfate
Dose:
ADULT:
0.25 mg SQ; repeat in 15-20 minutes2 inhalations separated by a 60 second interval with a metered
dose inhaler
4mg/7ml nebulizer mix
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Terbutaline Sulfate
Incompatible/Reactions:
1. Alkaline solutions
2. Degrades when exposed to light for long periods of time
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Terbutaline Sulfate
Notes:
ONSET: 15 minutes
PEAK: 30-60 minutes
DURATION: 90 minutes4 hours
Theophylline Ethylenediamine
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Theophylline Ethylenediamine
BRAND: Aminophylline
CLASS: Methylxanthine Spasmolytic
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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
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Theophylline
Actions:
6. Stimulates CNS vomiting centers
7. Respiratory center stimulant
8. Stimulates vagal and vasomotor centers in the braincanlead to decreased heart rate, vasoconstriction in the brain
depends on CNS or peripheral predominance
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Theophylline
Indications:
1. Relieve bronchospasm associated with asthma, chronic
bronchitis, emphysema, and pulmonary edema2. Management of CHF and pulmonary edema
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Theophylline
Contraindications:
1. Hypersensitivity to xanthene compounds (e.g. caffeine)
2. Cardiac dysrhythmias3. Tachycardia and tachydysrhythmias
Theophylline
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Theophylline
Adverse Reactions
Nausea/vomiting
Hypotension
Irritability
Tachycardia
Angina
Flushing
Diarrhea
Increased respiratory rate
Cardiac arrhythmias
Tremors
Seizures
Palpitations
Hypertension
Anorexia
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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 administration6. May oppose the effects of beta blockers
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Theophylline
Dose:
ADULT:
Loading dose of 6 mg/kg IV infusion over 20 minutesLoading dose of 1 mg/kg IV infusion over 20 minutes if the
patient has had theophylline products in the last 35 hours
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Theophylline
Incompatible/Reactions:
1. Incompatible with most drugs
2. Simetidine, propranolol, erythromycin, and troleandomycinmay increase the effects of the drug
3. Barbiturates, phenytoin, and smoking may decrease blood
levels
4. May increase the effects of anticoagulants
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Theophylline
Notes:ONSET: 15 minutes:
PEAK: 30 minutes1 hour
DURATION: Averages 5 hours
1. Common forms or oral aminophylline include:
* Marax * Primatene
* Quibron * Slo-Phyllin
* Slobid * Somophyllin
* Tedral * Theo-Dur
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Respiratory Medications
Respiratory meds are used for several purposes, themost obvious is the treatment of asthma. Class
includes:
1. Cough suppressants
2. Nasal decongestants
3. Antihistamines
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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 2selective sympathomimetics, nonselectivesympathomimetics, methylxanthines,anticholinergics, glucocorticoids and leukotrieneantagonists.
f
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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.
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Nonselective Sympathomimetics
Stimulate both beta 1 and beta 2 receptors, as well as alphareceptors.
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.
h l hi
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Methylxanthines
CNS stimulants that have additional bronchodilatoryproperties.
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
A i h li i
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Anticholinergics
Ipratropium (Atrovent) is an atropine derivative given bynebulizer.
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
Gl i id
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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.
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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 ofmethylprednisolone in emergencies are not likely
Long periods of administration can lead to adrenal
suppression and hyperglycemia.
Another anti-inflammatory agent used is cromolyn (Intal), aninhaled powder.
Gl ti id
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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.
L k t i A t i t
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Leukotriene Antagonists
Leukotrienes are mediators released from mast cells uponcontact with allergens.
Contribute powerfully to both inflammation and
bronchoconstriction
Can either block the synthesis of leukotrienes or block theirreceptors.
Zileuton (Zyflo) is the prototype of those that block the
synthesis of leukotrienes
Zafirlukast (Accolate) is the prototype of those that block theirreceptors
DRUGS USED FOR RHINITIS AND
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COUGH
Rhinitis: (inflammation of the nasal lining) comprisesa group of symptoms including nasal congestion,itching, redness, sneezing, and rhinorrhea (runnynose).
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 coughsuppressants are available in prescriptionmedications.
N l D t t
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Nasal Decongestants
Nasal congestion is caused by dilated and engorged nasalcapillaries.
Drugs that constrict these capillaries are effective nasal
decongestants.
Main pharmacologic classification in this functional category isalpha 1 agonists
Alpha 1 agonists may be given either topically or orally
Examples of agents: phenylephrine, pseudoephedrine, and
phenylpropanolamine, (administered in drops or mist)
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Antihistamines
Arrest the effects of histamine by blocking its receptors.
Histamineis 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.
A tihi t i
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Antihistamines
Histamine is synthesized and stored in two types ofgranulocytes; 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 theirspecific allergen.
A tihi t i
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Antihistamines
Secretory granules then migrate towards the cells exteriorand 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 hayfever 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
Antihistamines
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Antihistamines
Antihistamines are at best only a secondary drug for treatinganaphylaxis.
Just as there are H1 and H2 histamine receptors, there are H1
and H2 histamine receptor antagonists.
Most old antihistamines were H1 receptor antagonists, newerantihistamines 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])
Antihistamines
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Antihistamines
Other first generation antihistamines: clemastine (Tavist), andphenothiazines (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 andtherefore do not cause sedation.
Cough Suppressants
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Cough Suppressants
Coughing is a complex reflex that depends on functions in theCNS, 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 itis performing a useful function.
An unproductive cough, usually results from an irritated
oropharynx and can be troublesome.
The three classifications of cough suppressants include onethat is supported by evidence and two that are not.
Cough Suppressants
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Cough Suppressants
Antitussives1. 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
Cough Suppressants
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Cough Suppressants
5. The nonopioid antitussives do not have the potential forabuse.
a. Dextromethoraphan
b. Diphenhydramine
c. Benzonatate (Tessalon) Expectorants: intended to increase the productivity of
cough
Mucolytics:make mucus more watery and easier to coughup
Little data supports the effectiveness of either of theseapproaches to cough suppression