NAME: CANSAS, Michael E.

SCORE:
DATE: 04112024 RESPHARM
ACTIVITY NO 01
DRUG STUDY
Create a drug study for the following drugs:
Short acting Beta Agonists:
● Albuterol
● Levalbuterol
● Pirbuterol
● Terbutaline
● Metaproterenol
Long acting Beta Agonists
● Arformoterol
● Bambuterol
● Clenbuterol
● Formoterol
● Salmeterol
● Protokylol
Ultralong acting Beta Agonists
● Indacaterol
● Olodaterol
● Vilanterol
Anticholinergics
● Ipratropium Bromide
● Tiotropium Bromide
Corticosteroids
● Beclomethasone
● Budesonide
● Ciclesonide
● Fluticasone
● Mometasone
● Triamcinolone Acetonide
Leukotriene Modifiers
1. Montelukast
2. Zafirlukast
3. Zileuton
Mast Cell Stabilizers
● Cromolyn Sodium
● Nedocromil Sodium
Methylxanthines
● Aminophylline
● Theophylline
NAME: PINAY-AN, Enid Hope Maxigne SCORE:
DATE: 04112024 RESPHARM
ACTIVITY NO 01
DRUG STUDY
Create a drug study for the following drugs:
Short acting Beta Agonists:
Albuterol
Levalbuterol
Pirbuterol
Terbutaline
Metaproterenol
Long acting Beta Agonists
Arformoterol
Bambuterol
Clenbuterol
Formoterol
Salmeterol
Protokylol
Ultralong acting Beta Agonists
Indacaterol
Olodaterol
Vilanterol
Anticholinergics
Ipratropium Bromide
Tiotropium Bromide
Corticosteroids
Beclomethasone
Budesonide
Ciclesonide
Fluticasone
Mometasone
Triamcinolone Acetonide
Leukotriene Modifiers
Montelukast
Zafirlukast
Zileuton
Mast Cell Stabilizers
Cromolyn Sodium
Nedocromil Sodium
Methylxanthines
Aminophylline
Theophylline
SHORT ACTING BETA AGONISTS
01. Albuterol
● Definition:
○ Albuterol is a beta 2 adrenergic receptor agonist which is used in the treatment or
prevention of bronchospasm due to reversible obstructive airway disease, prevention of
exercise-induced bronchospasm. It may also be used in the treatment of asthma in
children under 4 yrs of age (off-label).
● Brand Names:
○ Airomir, ProAir HFA, ProAir RespiClick, Proventil HFA, Ventolin HFA, VoSpire ER)
● Generic Name:
○ albuterol sulfate
● Indications:
○ To prevent and relieve bronchospasm in patients with reversible obstructive airway
disease
● Pharmacodynamics:
○ Albuterol acts on β2-adrenergic receptors, inducing bronchial smooth muscle relaxation
and inhibiting immediate hypersensitivity mediator release, particularly from mast cells.
● Pharmacokinetics:
Route Onset Peak Duration

Per Orem 15–30 min 2–3 hrs 4–6 hrs

Per Orem 30 min 2–4 hrs 12 hrs

(Extended Release)

Inhalation 5–15 min 0.5–2 hrs 2–5 hrs

○ rapidly, well absorbed from GI tract
○ rapidly absorbed from bronchi after inhalation
○ metabolized in the liver
○ primarily excreted in urine
○ half-life: 3.8–6 hrs
● Mechanism of Action:
○ Stimulates beta2-adrenergic receptors in lungs, resulting in relaxation of bronchial
smooth muscle (little effect on HR).
○ Therapeutic Effect: Relieves bronchospasm and reduces airway resistance.
● Dosage:
○ Acute Bronchospasm, Exacerbation of Asthma
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS:
○ Acute, Severe: 4–8 puffs q 20 min up to 4 hrs, then q1–4h as
needed
● CHILDREN 12 YRS AND YOUNGER:
○ Acute, Severe: 4–8 puffs q 20 min for 3 doses, then q1–4h as
needed.
■ Nebulization:
● ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS:
○ Acute, Severe: 2.5–5 mg q20min for 3 doses, then 2.5–10 mg q1–
4h or 10–15 mg/hr continuously.
 ● CHILDREN 12 YRS AND YOUNGER:
○ 0.15 mg/kg q 20 min for 3 doses (minimum: 2.5 mg), then 0.15–
0.3 mg/kg q1–4h as needed.
○ Maximum: 10 mg q1–4h as needed or 0.5 mg/kg/hr by continuous
inhalation.
○ Bronchospasm
■ PO:
● ADULTS, CHILDREN OLDER THAN 12 YRS:
○ 2–4 mg 3–4 times/day. Maximum: 8 mg 4 times/day.
● ELDERLY:
○ 2 mg 3–4 times/day. Maximum: 8 mg 4 times/day.
● CHILDREN 6–12 YRS:
○ 2 mg 3–4 times/day. Maximum: 24 mg/day.
● CHILDREN 2–5 YRS:
○ 0.1–0.2 mg/kg/dose 3 times/day. Maximum: 4 mg 3 times/day.
■ PO: (Extended-Release):
● ADULTS, CHILDREN OLDER THAN 12 YRS:
○ 4–8 mg q12h. Maximum: 32 mg/day.
● CHILDREN 6–12 YRS:
○ 4 mg q12h. Maximum: 24 mg/day.
■ Nebulization:
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 2.5 mg 3–4 times/day as needed.
● CHILDREN 2–11 YRS:
○ (Greater than 15 kg):
■ 0.63–2.5 mg 3 to 4 times/day. Maximum: 10 mg/day.
○ (10–15 kg):
■ 0.63–1.25 mg 3–4 times/day as needed. Maximum: 10
mg/day.
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN:
○ 2 puffs q4–6h as needed.
○ Exercise-Induced Bronchospasm
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN 5 YRS AND OLDER:
○ 2 puffs 5 min before exercise.
● CHILDREN 4 YRS AND YOUNGER:
○ 1–2 puffs 5 min before exercise.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ hyperactivity, insomnia
○ CV: hypertension, palpitations, tachycardia, chest pain
○ EENT: conjunctivitis, dry and irritated throat, pharyngitis
○ GI: nausea, vomiting, anorexia, heartburn, GI distress, dry mouth
○ Metabolic: hypokalemia
○ Musculoskeletal: muscle cramps
 ○ Respiratory: cough, dyspnea, wheezing, paradoxical bronchospasm
○ Skin: pallor, urticaria, rash, angioedema, flushing, sweating
○ Other: tooth discoloration, increased appetite, hypersensitivity reaction
02. Levalbuterol
● Definition:
○ Levalbuterol is a beta2 agonist which is used in the treatment and prevention of
bronchospasm due to reversible obstructive airway disease (e.g., asthma, bronchitis,
emphysema). OFF-LABEL: Treatment of asthma in children younger than 4 yrs of age.
● Brand Names:
○ Xopenex, Xopenex HFA, Xopenex Concentrate
● Generic Name:
○ Levalbuterol
● Indications:
○ Levalbuterol is indicated for the treatment, prevention of bronchospasm due to reversible
obstructive airway disease (e.g., asthma, bronchitis, emphysema). It is also indicated for
the treatment of asthma in children younger than 4 yrs of age.
● Pharmacodynamics:
○ Binds to beta2-adrenergic receptors on bronchial cell membrane, stimulating the
intracellular enzyme adenylate cyclase to convert adenosine triphosphate to cyclic-3,5-
adenosine monophosphate. This action relaxes smooth muscles, dilates bronchioles,
and increases diuresis.
● Pharmacokinetics:
Route Onset Peak Duration

Inhalation 5–10 min 1.5 hrs 5–6 hrs

Nebulization 10–17 min 1.5 hrs 5–8 hrs

○ Half-life: 3.3–4 hrs.
● Mechanism of Action:
○ Stimulates beta2-adrenergic receptors in lungs, resulting in relaxation of bronchial
smooth muscle.
○ Therapeutic Effect: Relieves bronchospasm, reduces airway resistance.
● Dosage:
○ Treatment/Prevention of Bronchospasm
■ Nebulization:
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ Initially, 0.63 mg 3 times/day 6–8 hrs apart. May increase to 1.25
mg 3 times/day with close monitoring.
● CHILDREN 5–11 YRS:
○ Initially, 0.31 mg 3 times/day. Maximum:! 0.63 mg 3 times/day
● CHILDREN 4 YRS OR YOUNGER:
○ 0.31–1.25 mg q4–6h as needed.
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN 4 YRS AND OLDER:
○ 1–2 inhalations q4–6h.
○ Acute Asthma Exacerbation
■ Nebulization:
 ● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 1.25–2.5 mg q20min for 3 doses, then 1.25–5 mg q1–4h as
needed.
● CHILDREN YOUNGER THAN 12 YRS:
○ 0.075 mg/kg (minimum dose: 1.25 mg) q20min for 3 doses, then
0.075–0.15 mg/kg (Maximum: 5 mg dose) q1–4h as needed.
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 4–8 puffs q20min for up to 4 hrs, then q1–4h.
● CHILDREN YOUNGER THAN 12 YRS:
○ 4–8 puffs q20min for 3 doses, then q1–4h.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ Excessive sympathomimetic stimulation may produce palpitations, premature heart
contraction, tachycardia, chest pain, slight increase in B/P followed by substantial
decrease, chills, diaphoresis, blanching of skin. Too-frequent or excessive use may
decrease bronchodilating effectiveness, leading to severe, paradoxical
bronchoconstriction.
03. Pirbuterol
● Definition:
○ Pirbuterol is a beta 2 adrenergic bronchodilators which is used alone or together with
other medicines, to prevent bronchospasm in patients 12 years of age and older with
asthma, bronchitis, emphysema, and other lung diseases
● Brand Names:
○ Maxair, Maxair Autohaler
● Generic Name:
○ pirbuterol acetate
● Indications:
○ Pirbuterol is indicated for the prevention and reversal of bronchospasm in patients 12
years of age and older with reversible bronchospasm including asthma.
● Pharmacodynamics:
○ Binds to beta2-adrenergic receptors on bronchial cell membrane, stimulating the
intracellular enzyme adenylate cyclase to convert adenosine triphosphate to cyclic-3,5-
adenosine monophosphate. This action relaxes smooth muscles, dilates bronchioles,
and increases diuresis.
● Pharmacokinetics:
○ Half-Life: 2 hrs
○ Onset: <5 min; 0.5-1 hr (peak effect)
○ Duration: 5 hrs
○ Metabolism: Hepatic
○ Excretion: Urine (10%)
● Mechanism of Action:
○ Stimulates beta2-adrenergic receptors in lungs, resulting in relaxation of bronchial
smooth muscle.
● Dosage:
○ Adult:
 ■ Dosage Forms & Strengths
● metered dose inhaler
○ 200mcg/actuation (14g canister; ~400 actuations)
■ Asthma Maintenance Treatment
● 1-2 actuations q4-6hr PRN; not to exceed 12 actuations/day
○ Pediatric:
■ Dosage Forms & Strengths
● metered dose inhaler
○ 200mcg/actuation (14g canister; ~400 actuations)
■ Asthma Maintenance Treatment
● <12 years: Safety and efficacy not established
● >12 years: As adults; 1-2 actuations q4-6hr PRN; not to exceed 12
actuations/day
● Adverse Effect:
○ Nervousness ○ CoughHeadache
○ Restlessness ○ Dizziness
○ Serum glucose increased ○ Lightheadedness
○ Serum potassium decreased ○ Taste changes
○ Trembling ○ Vomiting
○ Palpitations ○ Nausea
○ Tachycardia ○ Paradoxical bronchospasm
04. Terbutaline
● Definition:
○ Terbutaline is a beta-2 adrenergic agonist used as a bronchodilator and to prevent
premature labor.
● Brand Names:
○ Bricanyl
● Generic Name:
○ Terbutaline
● Indications:
○ Terbutaline is indicated for prevention and reversal of bronchospasm in patients at least
12 years old, with asthma and reversible bronchospasm associated with bronchitis and
emphysema.
● Pharmacodynamics:
○ Terbutaline is a beta-2 adrenergic receptor agonist indicated to treat reversibly
bronchospasm in asthmatic patients with bronchitis and emphysema.16,17 It has a short
duration as the inhaled form is taken up to three times daily, and the therapeutic window
is wide.
● Pharmacokinetics:
○ Onset: 30-45 min (PO); 6-15 min (SC)
○ Duration: 90 min-4 hr
○ Peak plasma time: 30-60 min
○ Half-life: 11-16 hr
○ Protein binding: 25%
○ Absorption: 33-50%
○ Metabolism: Partially metabolized in liver, mainly to inactive sulfate conjugate
 ○ Excretion: 60% urine unchanged, up to 3% feces via bile; remainder in urine as the
conjugate (w/ parenteral admin)
● Mechanism of Action:
○ Terbutaline is a selective beta-2 adrenergic receptor agonist. Agonism of these
receptors in bronchioles activates adenylyl cyclase, increasing intracellular cyclic
adenosine monophosphate (cAMP).Increased cAMP decreases intracellular calcium,
activating protein kinase A, inactivating myosin light-chain kinase, activating myosin
light-chain phosphatase, and finally relaxing smooth muscle in the bronchiole.
● Dosage:
○ Adult:
■ Dosage Forms & Strengths
● Tablet
○ 2.5mg/5mg
● injectable solution
○ 1 mg/mL
■ Bronchospasm
● PO
○ Initiate at 2.5 mg three/four times daily PO
○ Maintenance: 5 mg three times daily PO q6hr while patient is
awake; reduce dose to 2.5 mg q6hr
○ Not to exceed 15 mg/Day
● SC
○ 0.25 mg q15-30min x 3 doses PRN in lateral deltoid
○ Not to exceed 0.5 mg/4 hr
■ Preterm Labor (Off-label)
● Initiate at 2.5-5 mcg/min IV
● Increase gradually as tolerated at 20-30 minute intervals
● Typical effective dose ranges between 17.5-30 mcg/min IV; some require
doses up to 70-80 mcg/min
● Continue infusion for 12 hr following cessation of uterine contractions; not
to exceed 48-72 hr
● PO use or prolonged IV use not recommended (see Black Box Warnings)
■ Renal Impairment
● GFR <50 mL/min: reduce dose by 50%
● GFR >50mL/min: Dose adjustment not necessary
○ Pediatric:
■ Dosage Forms & Strengths
● Tablet
○ 2.5mg
○ 5mg
● injectable solution
○ 1mg/mL
■ Bronchospasm
● PO
○ <12 years: 0.05 mg/kg three times daily initially; increase PRN, not
to exceed 5 mg/day
 ○ 12-15 years: 2.5 mg PO q6hr 3 times daily; not to exceed 7.5
mg/day
○ >15 years: 5 mg/dose PO q8hr three times daily; reduce dose to
2.5 mg q6hr; not to exceed 15 mg/24hr
● SC (in lateral deltoid)
○ <12 years: 0.005-0.01 mg/kg (no more than 0.4 mg) q15-20min x
3; THEN q2-6hour PRN
○ >12 years: 0.25 mg q15-30min x 3 doses PRN in lateral deltoid;
not to exceed 0.5 mg/4 hr
● Adverse Effect:
○ Nervousness ○ Nausea
○ Restlessness ○ Vomiting
○ Transient hyperglycemia ○ Bad taste in mouth
○ Transient hypokalemia ○ Muscle cramps
○ Trembling ○ Weakness
○ Tachycardia ○ Diaphoresis
○ HTN ○ Cardiac arrhythmias
○ Pounding heartbeat ○ Pulmonary edema
○ Dizziness ○ Myocardial ischemia
○ Lightheadedness ○ Myocardial infarction
○ Drowsiness ○ Increased fetal heart rate
○ Headache ○ Hypoglycemia in some neonates
○ Insomnia born to women who received
○ Dry mouth drug during labor
05. Metaproterenol
● Definition:
○ Metaproterenol is a beta-2 adrenergic agonist used in the treatment of asthma and
bronchospasm.
● Brand Names:
○ Alupent
● Generic Name:
○ metaproterenol sulfate
● Indications:
○ Metaproterenol is used to prevent and treat wheezing, shortness of breath, coughing,
and chest tightness caused by asthma, chronic bronchitis, emphysema, and other lung
diseases. It relaxes and opens air passages in the lungs, making it easier to breathe.
● Pharmacodynamics:
○ stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature
supplying skeletal muscle
● Pharmacokinetics:
○ Onset: 30 min (oral)
○ Peak effect: 1 hr
○ Duration: 2-6 hr
○ Metabolism: Liver
○ Metabolites: Metaproterenol-O-sulfate
○ Excretion: Uurine (40%)
● Mechanism of Action:
 ○ Beta-2 receptor agonist with some beta-1 activity; stimulation of beta2 receptors may
result in bronchial smooth muscle relaxation
● Dosage:
○ Adult:
■ Dosage Forms & Strengths
● Tablet
○ 10mg
○ 20mg
● Syrup
● 10mg/5mL
■ Asthma, Reversible Bronchospasm
● 20 mg PO three/four times daily
○ Pediatric:
■ Dosage Forms & Strengths
● tablet
○ 10mg
○ 20mg
● syrup
○ 10mg/5mL
■ Asthma
● PO
○ <2 years old: 0.4 mg/kg PO q8-12hr
○ 2-6 years old: 1-3.5 mg/kg/day divided q6-8hr PO; not to exceed
10 mg/dose
○ 6-9 years old: 10 mg PO three/four times daily
○ >12 years old: 20 mg PO three times daily
● Adverse Effect:
○ >10% ■ Insomnia (2%)
■ Tremor (2-17%) ■ Weakness (1%)
■ Tachycardia (6-17%) ■ Nausea (1-4%)
■ Nervousness (5-20%) ■ Exacerbation of
○ 1-10% asthma (2%)
■ Diaphoresis ○ <1%
increased (4%) ■ Chest pain
■ Headache (4%) ■ Hypertension
■ Heartburn (4%) ■ Weakness
■ Palpation (4%) ■ Syncope
■ Pharyngitis (4%) ■ Spasms
■ Dizziness (1-4%)
LONG ACTING BETA AGONISTS
01. Arformoterol
● Definition:
○ Arformoterol is a long acting beta agonist and bronchodilator used for long-term,
symptomatic treatment of reversible bronchoconstriction in patients with chronic
obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema.
● Brand Names:
○ Brovana
● Generic Name:
○ Arformoterol
● Indications:
○ Long acting beta agonists, such as Arformoterol is indicated for maintenance
bronchodilation, control of bronchospasm, and the treatment of nocturnal symptoms in
asthma or other obstructive diseases, such as chronic obstructive pulmonary disease
(COPD).
● Pharmacodynamics:
○ Arformoterol, the active (R,R)-enantiomer of formoterol, is a selective long-acting β2-
adrenergic receptor agonist (beta2-agonist) that has two-fold greater potency than
racemic formoterol (which contains both the (S,S) and (R,R)-enantiomers). The (S,S)-
enantiomer is about 1,000-fold less potent as a β2-agonist than the (R,R)-enantiomer.
Arformoterol seems to have little or no effect on β1-adrenergic receptors.
● Pharmacokinetics:
○ Onset: 15 min
○ Peak: 30–60 min
○ Duration: 12 h
● Mechanism of Action:
○ stimulates the G protein–linked β receptor to cause smooth muscle relaxation.
Adrenergic agonists, such as albuterol or epinephrine, attach to β receptors, which are
polypeptide chains traversing the cell membrane seven times. This causes activation of
the stimulatory G protein, designated GS, linked to the receptor. When stimulated, the
receptor undergoes a conformational change, and the α subunit of the G protein
attaches to adenyl cyclase. Activation of adenyl cyclase by the GS protein causes an
increased synthesis of the second messenger, cyclic adenosine monophosphate
(cAMP). This ultimately causes smooth muscle relaxation and bronchodilation. ATP,
Adenosine triphosphate; COOH, carboxy terminus; GDP, guanosine diphosphate; GTP,
guanosine triphosphate.
● Dosage:
○ SVN: 15 mcg/2 mL unit dose, bid
● Adverse Effect:
○ Dizziness
○ Hypokalemia
○ Loss of bronchoprotection
○ Nausea
○ Tolerance (tachyphylaxis)
○ Worsening ventilation/perfusion (V̇ /Q̇ ) ratio (decrease in PaO2/SpO2)
02. Bambuterol
● Definition:
 ○ a long acting beta2-adrenoceptor agonist for the management of lung diseases
associated with bronchospasm.
● Brand Names:
○ Bambec and Oxeol
● Generic Name:
○ Bambuterol
● Indications:
○ For the prevention and reversal of bronchospasm in patients 12 years of age and older
with asthma and reversible bronchospasm associated with bronchitis and emphysema.
● Pharmacodynamics:
○ Bambuterol is a long acting beta2-adrenoceptor agonist used in the treatment of asthma.
It is a prodrug of terbutaline. Bambuterol causes smooth muscle relaxation, resulting in
dilation of bronchial passages.
● Pharmacokinetics:
○ Absorption: Absorbed from the GI tract (approx 20%). Bioavailability: Approx 10%. Time
to peak plasma concentration: Approx 4-7 hr (terbutaline).
○ Distribution: Plasma protein binding: 40-50%.
○ Metabolism: Slowly metabolized in the liver to its active metabolite, terbutaline via
hydrolysis and oxidation.
○ Excretion: Terminal half-life: 9-17 hr.
● Mechanism of Action:
○ Bambuterol is a prodrug of terbutaline. It relaxes bronchial smooth muscle by selectively
acting on β2-receptors.
● Dosage:
○ Adult: 10-20 mg once daily at bedtime.
● Adverse Effect:
○ Behavioral disturbances (e.g. restlessness, agitation), tremor, headache, sleep
disturbances, palpitations, muscle cramps, hypersensitivity reactions, hypokalaemia,
hyperglycaemia, dizziness, hyperactivity, tachycardia, cardiac arrhythmias, myocardial
ischaemia, paradoxical bronchospasm, nausea.
03. Clenbuterol
● Definition:
○ Clenbuterol is a beta-2-adrenergic agonist which acts as both a bronchodilator and a
decongestant. Variants of this may be used for animals. It is banned in some countries
due its controversial effects in bodybuilding and weight loss programs.
● Brand Names:
○ Dilaterol, Spiropent, Ventipulmin
● Generic Name:
○ Clenbuterol
● Indications:
○ Used as a bronchodilator in the treatment of asthma patients.
● Pharmacodynamics:
○ Clenbuterol is a substituted phenylaminoethanol that has beta-2 adrenomimetic
properties at very low doses. It is used as a bronchodilator in asthma. Although
approved for use in some countries, as of fall, 2006, clenbuterol is not an ingredient of
any therapeutic drug approved by the U.S. Food and Drug Administration.
● Pharmacokinetics:
 ○ Onset: 30 mins
○ Peak: 3hrs
● Mechanism of Action:
○ Clenbuterol is a Beta(2) agonist similar in some structural respects to salbutamol.
Agonism of the beta(2) receptor stimulates adenylyl cyclase activity which ultimately
leads to downstream effects of smooth muscle relaxation in the bronchioles.
● Dosage:
○ 0.02–0.03 milligrams daily
● Adverse Effect:
○ heart palpitations
○ atrial fibrillation, which is an irregular and often fast heartbeat
○ problems with blood pressure
04. Formoterol
● Definition:
○ Formoterol is an inhaled long-acting beta2-adrenergic receptor agonist used as a
bronchodilator in the management of asthma and COPD.
● Brand Names:
○ Bevespi, Breyna, Breztri, Duaklir, Duaklir Genuair, Dulera, Foradil, Oxeze, Perforomist,
Symbicort, Zenhale
● Generic Name:
○ Formoterol
● Indications:
○ Long acting beta agonists, such as Formoterol is indicated for maintenance
bronchodilation, control of bronchospasm, and the treatment of nocturnal symptoms in
asthma or other obstructive diseases, such as chronic obstructive pulmonary disease
(COPD).
● Pharmacodynamics:
○ Formoterol works locally in the lungs as a bronchodilator, relaxing smooth muscle and
opening up the airways. It possesses both a rapid onset of action (approximately 2-3
minutes) and a long duration of action (up to 12 hours). The use of long-acting beta-
agonists (LABAs), such as formoterol, without concomitant inhaled corticosteroids in
asthmatic patients should be avoided, as LABA monotherapy has been associated with
an increased risk of asthma-related death.
● Pharmacokinetics:
○ Onset: 15 min
○ Peak: 30–60 min
○ Duration: 12 h
● Mechanism of Action:
○ Formoterol is a relatively selective long-acting agonist of beta2-adrenergic receptors,
although it does carry some degree of activity at beta1 and beta3 receptors. Beta2
receptors are found predominantly in bronchial smooth muscle (with a relatively minor
amount found in cardiac tissue) whereas beta1 receptors are the predominant
adrenergic receptors found in the heart - for this reason, selectivity for beta2 receptors is
desirable in the treatment of pulmonary diseases such as COPD and asthma.
Formoterol has demonstrated an approximately 200-fold greater activity at beta2
receptors over beta1 receptors.
● Dosage:
 ○ SVN: 20 mcg/2 mL unit dose bid
● Adverse Effect:
○ Dizziness
○ Hypokalemia
○ Loss of bronchoprotection
○ Nausea
○ Tolerance (tachyphylaxis)
○ Worsening ventilation/perfusion (V̇ /Q̇ ) ratio (decrease in PaO2/SpO2)
05. Salmeterol
● Definition:
○ Salmeterol is a long-acting beta-2 adrenergic receptor agonist used to treat asthma and
COPD.
● Brand Names:
○ Advair, Airduo, Airduo Respiclick, Serevent, Serevent Diskus, Wixela
● Generic Name:
○ Salmeterol
● Indications:
○ Long acting beta agonists, such as Salmeterol is indicated for maintenance
bronchodilation, control of bronchospasm, and the treatment of nocturnal symptoms in
asthma or other obstructive diseases, such as chronic obstructive pulmonary disease
(COPD).
● Pharmacodynamics:
○ Salmeterol is a long-acting beta-2 adrenergic receptor agonist that binds to both the
active and exo sites of the beta-2 adrenergic receptor. Salmeterol has a longer duration
of action than other beta-2 agonists like salbutamol. Patients should be counseled
regarding the risks of long acting beta agonist (LABA) monotherapy, hypokalemia,
hypoglycemia, and not to take this drug with another LABA.
● Pharmacokinetics:
○ Onset: 20 min
○ Peak: 3–5 h
○ Duration: 12 h
● Mechanism of Action:
○ Beta-2 adrenoceptor stimulation causes relaxation of bronchial smooth muscle,
bronchodilation, and increased airflow.
○ Salmeterol is hypothesized to bind to 2 sites on the beta-2 adrenoceptor. The saligenin
moiety binds to the active site of the beta-2 adrenoceptor.1 The hydrophilic tail of
salmeterol binds to leucine residues in the exo-site of the beta-2 adrenoceptor almost
irreversibly, allowing salmeterol to persist in the active site, which is responsible for it's
long duration of action.
○ Another hypothesis is that the lipophilic drug diffuses into lipid bilayer of smooth muscle
cells and provides a depot of drug to the cells over a longer period of time.
● Dosage:
○ 1 inh bid
○ Available Preparations:
■ DPI 50 mcg/blister
■ 28, 60 inh/unit
● Adverse Effect:
 ○ Dizziness
○ Hypokalemia
○ Loss of bronchoprotection
○ Nausea
○ Tolerance (tachyphylaxis)
○ Worsening ventilation/perfusion (V̇ /Q̇ ) ratio (decrease in PaO2/SpO2)
06. Protokylol
● Definition:
○ Protokylol is a β-adrenergic receptor agonist used as a bronchodilator in Europe and the
United States.
● Brand Names:
○
● Generic Name:
○ Protokylol
● Indications:
● Pharmacodynamics:
● Pharmacokinetics:
● Mechanism of Action:
● Dosage:
● Adverse Effect:
ULTRALONG ACTING BETA AGONIST
01. Indacaterol
● Definition:
○ Indacaterol is an inhaled long-acting beta-2 adrenergic agonist used to relax bronchial
smooth muscle and improve symptoms and airflow obstruction caused by Chronic
Obstructive Pulmonary Disease (COPD) and moderate to severe asthma.
● Brand Names:
○ Arcapta Neohaler
● Generic Name:
○ Indacaterol
● Indications:
○ Long acting beta agonists, such as Salmeterol is indicated for maintenance
bronchodilation, control of bronchospasm, and the treatment of nocturnal symptoms in
asthma or other obstructive diseases, such as chronic obstructive pulmonary disease
(COPD).
● Pharmacodynamics:
○ Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of
the airways. This causes relaxation of the muscle, thereby increasing the diameter of the
airways, which become constricted in asthma and COPD. It is also long acting due to its
high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from
the receptors. Indacaterol also has a high intrinsic efficacy so it is also very rapid acting -
onset of action occurs within 5 minutes.
● Pharmacokinetics:
○ Onset: 5 min
○ Peak: 30 min
○ Duration: 24 h
● Mechanism of Action:
○ Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of
the airways. This causes relaxation of the muscle, thereby increasing the diameter of the
airways, which become constricted in asthma and COPD. It is also long acting due to its
high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from
the receptors. Indacaterol also has a high intrinsic efficacy so it is also very rapid acting -
onset of action occurs within 5 minutes.
● Dosage:
○ Adult: DPI: 75 mcg/inhalation, qd
○ COPD: 1 inh/day
● Adverse Effect:
○ Dizziness
○ Hypokalemia
○ Loss of bronchoprotection
○ Nausea
○ Tolerance (tachyphylaxis)
○ Worsening ventilation/perfusion (V̇ /Q̇ ) ratio (decrease in PaO2/SpO2)
02. Olodaterol
● Definition:
○ Olodaterol is a long-acting beta2-adrenergic agonist used in the management of chronic
obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.
 ● Brand Names:
○ Stiverdi Respimat
● Generic Name:
○ Olodaterol
● Indications:
○ Maintenance therapy in chronic obstructive pulmonary disease
○ Adult: As metered-dose aerosol inhaler (2.5 mcg/actuation): 2 inhalations once daily.
● Pharmacodynamics:
○ Olodaterol is a potent agonist of the human beta2-adrenergic receptor in vitro, and is
highly selective for this receptor, with much lower levels of activity at the b1- and b3-
adrenergic receptors that are commonly expressed on cardiac smooth muscle and
adipose tissue, respectively. Binding to the receptor causes smooth muscle relaxation in
the lungs and bronchodilation. It has also been shown to potently reverse active
bronchoconstriction.
● Pharmacokinetics:
○ Onset: 15 min
○ Peak: 30–60 min
○ Duration: 12 h
● Mechanism of Action:
○ Olodaterol is a long acting beta2-receptor agonist. It stimulates intracellular adenyl
cyclase, thereby increasing cyclic-3′, 5′-adenosine monophosphate (cAMP) levels,
resulting in bronchodilation by relaxation of airway smooth muscle.
● Dosage:
○ SMI: 2.5 mcg/actuation, 2 actuations qd
● Adverse Effect:
○ Significant: Hypersensitivity (e.g. angioedema), increased serum glucose, decreased
serum K, CNS stimulation/excitation, thyroid activity stimulation; CV effects (e.g.
increased pulse rate, and blood pressure, ECG changes), hypokalaemia,
hyperglycaemia.
○ Infections and infestations: UTI.
○ Musculoskeletal and connective tissue disorders: Arthralgia, back pain.
○ Nervous system disorders: Dizziness.
○ Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, bronchitis.
○ Skin and subcutaneous tissue disorders: Rash.
○ Potentially Fatal: Paradoxical bronchospasm.
03. Vilanterol
● Definition:
○ Vilanterol is a long-acting beta2-adrenergic agonist used in combination with other
bronchodilators for the management of chronic obstructive pulmonary disease (COPD),
including chronic bronchitis and/or emphysema.
● Brand Names:
○ Anoro, Anoro Ellipta, Breo Ellipta, Trelegy Ellipta
● Generic Name:
○ Vilanterol
● Indications:
○ Vilanterol is approved for use in several combination products such as with fluticasone
furoate under the trade name Breo Ellipta, in combination with umeclidinium bromide as
 Anoro Ellipta, and in combination with both fluticasone furoate and umeclidinium under
the trade name Trelegy Ellipta
● Pharmacodynamics:
○ Vilanterol is a selective long-acting beta2-adrenergic agonist. Its pharmacological effect
is attributable to stimulation of intracellular adenylyl cyclase which catalyzes the
conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate
(cAMP). Increases in cyclic AMP are associated with relaxation of bronchial smooth
muscle and inhibition of release of hypersensitivity mediators from mast cells in the
lungs.
● Pharmacokinetics:
○ Onset: 16 min
○ Peak: 1 min
● Mechanism of Action:
○ Vilanterol is a selective long-acting beta2-adrenergic agonist. Its pharmacological effect
is attributable to stimulation of intracellular adenylyl cyclase which catalyzes the
conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate
(cAMP). Increases in cyclic AMP are associated with relaxation of bronchial smooth
muscle and inhibition of release of hypersensitivity mediators from mast cells in the
lungs.
● Dosage:
○ For inhalation dosage form (powder):
■ For treatment of asthma:
● Adults—One inhalation once a day. Each inhalation contains 100 or 200
micrograms (mcg) of fluticasone and 25 mcg of vilanterol.
● Children 12 to 17 years of age—One inhalation once a day. Each
inhalation contains 100 mcg of fluticasone and 25 mcg of vilanterol.
● Children 5 to 11 years of age—One inhalation once a day. Each
inhalation contains 50 mcg of fluticasone and 25 mcg of vilanterol.
● Children younger than 5 years of age—Use and dose must be
determined by your doctor.
○ For treatment and prevention of worsening attacks of COPD:
■ Adults—One inhalation once a day. Each inhalation contains 100 micrograms
(mcg) of fluticasone and 25 mcg of vilanterol.
■ Children—Use is not recommended.
● Adverse Effect:
○ Significant: Hypersensitivity (e.g. angioedema), increased serum glucose, decreased
serum K, CNS stimulation/excitation, thyroid activity stimulation; CV effects (e.g.
increased pulse rate, and blood pressure, ECG changes), hypokalaemia,
hyperglycaemia.
○ Infections and infestations: UTI.
○ Musculoskeletal and connective tissue disorders: Arthralgia, back pain.
○ Nervous system disorders: Dizziness.
○ Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, bronchitis.
○ Skin and subcutaneous tissue disorders: Rash.
○ Potentially Fatal: Paradoxical bronchospasm.
ANTICHOLINERGICS
01. Ipratropium Bromide
● Definition:
○ Ipratropium is an anticholinergic bronchodilator which is used for the maintenance
treatment of bronchospasm due to COPD, bronchitis, emphysema, asthma. It is also
used for the symptomatic relief of rhinorrhea associated with the common cold and
allergic/nonallergic rhinitis.
● Brand Names:
○ Atrovent HFA, Apo-Ipratropium
● Generic Name:
○ Ipratropium bromide
● Indications:
○ Maintenance treatment of bronchospasm due to COPD, bronchitis, emphysema,
asthma.
○ Symptomatic relief of rhinorrhea associated with the common cold and
allergic/nonallergic rhinitis
● Pharmacodynamics:
○ Ipratropium is an anticholinergic bronchodilator that blocks action of acetylcholine at
parasympathetic sites in bronchial smooth muscle resulting in bronchodilation and the
inhibition of nasal secretions.
● Pharmacokinetics:
Route Onset Peak Duration

Inhalation 1–3 min 1.5–2 hrs Up to 4 hrs

Nasal 5 min 1–4 hrs 4–8 hrs

○ Minimal systemic absorption after inhalation.
○ Metabolized in liver (systemic absorption). Primarily excreted in feces.
○ Half-life: 1.5–4 hrs (nasal).
● Mechanism of Action:
○ Blocks action of acetylcholine at parasympathetic sites in bronchial smooth muscle.
Application to nasal mucosa inhibits serous/seromucous gland secretions.
○ Therapeutic Effect: Causes bronchodilation, inhibits nasal secretions.
● Dosage:
○ Bronchodilator for COPD
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS:
○ 2 inhalations 4 times/ day. Maximum: 12 inhalations per 24 hrs.
■ Nebulization:
● ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS:
○ 500 mcg (1 unit dose vial) 3–4 times/day (doses 6–8 hrs apart).
○ Asthma Exacerbation
■ Note: Should be given in combination with a short-acting beta-adrenergic
agonist.
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS:
○ 8 inhalations q20min as needed for up to 3 hrs.
 ● CHILDREN 6–12 YRS:
○ 4–8 inhalations q20min as needed for up to 3 hrs.
● CHILDREN 5 YRS OR YOUNGER:
● 2 inhalations q20 min for 1 hr.
■ Nebulization:
● ADULTS, ELDERLY, CHILDREN OLDER THAN 12 YRS:
○ 500 mcg q20min for 3 doses, then as needed.
● CHILDREN 6–12 YRS:
○ 250–500 mcg q20min for 3 doses, then as needed.
● CHILDREN 5 YRS OR YOUNGER: 250 mcg q20 min for 1 hr.
○ Rhinorrhea (Perennial Allergic/Nonallergic Rhinitis)
■ Intranasal: (0.03%):
● ADULTS, ELDERLY, CHILDREN 6 YRS AND OLDER:
○ 2 sprays per nostril 2–3 times/day.
○ Rhinorrhea (Common Cold)
■ Intranasal: (0.06%):
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 2 sprays per nostril 3–4 times/day for up to 4 days.
● CHILDREN 5–11 YRS:! 2 sprays per nostril 3 times/day for up to 4 days.
○ Rhinorrhea (Seasonal Allergy)
■ Intranasal: (0.06%):
● ADULTS, ELDERLY, CHILDREN 5 YRS AND OLDER:
○ 2 sprays per nostril 4 times/day for up to 3 wks.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ Worsening of angle-closure glaucoma, acute eye pain, hypotension occur rarely.
02. Tiotropium Bromide
● Definition:
○ Tiotropium Bromide is an anticholinergic (long-acting) bronchodilator used in the long-
term maintenance treatment of bronchospasm associated with COPD, including chronic
bronchitis, emphysema, and for reducing COPD exacerbations.
○ Spiriva Respimat is used in the maintenance treatment of asthma in pts 6 yrs and older.
● Brand Names:
○ (Spiriva HandiHaler, Spiriva Respimat)
● Generic Name:
○ Tiotropium Bromide
● Indications:
○ Tiotropium Bromide is indicated for the following:
■ COPD (Maintenance Treatment, Reduction of COPD Exacerbations)
■ Asthma
● Pharmacodynamics:
○ Tiotropium bromide is an anticholinergic bronchodilator which competitively and
reversibly inhibits action of acetylcholine at muscarinic receptors in bronchial smooth
muscle resulting in bronchodilation.
● Pharmacokinetics:
○ Binds extensively to tissue.
 ○ Protein binding: 72%.
○ Metabolized by oxidation.
○ Excreted in urine.
○ Half-life: 5–6 days.
● Mechanism of Action:
○ Competitively and reversibly inhibits action of acetylcholine at muscarinic receptors in
bronchial smooth muscle.
○ Therapeutic Effect: Causes bronchodilation.
● Dosage:
○ COPD (Maintenance Treatment, Reduction of COPD Exacerbations)
■ Inhalation:
● ADULTS, ELDERLY:
○ (Spiriva): 18 mcg (1 capsule)/day via HandiHaler inhalation
device.
○ (Spiriva Respimat [2.5mcg/actuation]): 2 inhalations (2.5
mg/inhalation) once daily.
○ Asthma
■ Inhalation:
● ADULTS, ELDERLY, CHILDREN 6 YRS AND OLDER:
○ (Spiriva Respimat [1.25 mcg/actuation]): 2 inhalations of 1.25 mcg
once daily. Maximum benefit may take up to 4–8 wks.
○ Dosage in Renal Impairment
■ CrCl 60 mL/min or less:
■ Use caution in moderate to severe impairment.
○ Dosage in Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ Angina pectoris, depression, flu-like symptoms, glaucoma, increased intraocular
pressure occur rarely.
CORTICOSTEROIDS
01. Beclomethasone
● Definition:
○ Beclomethasone is an adrenocorticosteroid that is used for maintenance and
prophylactic treatment of asthma in pts 5 yrs and older.
● Brand Names:
○ Beconase AQ, QNASL, QVAR RediHaler)
● Generic Name:
○ Beclomethasone
● Indications:
○ Beclomethasone is indicated for:
■ Asthma
■ Rhinitis, Prevention of Recurrence of Nasal Polyps
■ Allergic Rhinitis
● Pharmacodynamics:
○ Beclomethasone is an adrenocorticosteroid which controls or prevents inflammation by
altering rate of protein synthesis; depresses migration of polymorphonuclear leukocytes,
fibroblasts; reverses capillary permeability which results in the inhibition of
bronchoconstriction, produces smooth muscle relaxation, decreases mucus secretion,
and decreases response to seasonal, perennial rhinitis.
● Pharmacokinetics:
○ Rapidly absorbed from pulmonary, nasal, GI tissue.
○ Metabolized in liver.
○ Protein binding: 87%.
○ Excreted in feces (60%), urine (12%). Half-life:! 2–4.5 hrs.
● Mechanism of Action:
○ Controls or prevents inflammation by altering rate of protein synthesis; depresses
migration of polymorphonuclear leukocytes, fibroblasts; reverses capillary permeability.
○ Therapeutic Effect:
■ Inhalation:
● Inhibits bronchoconstriction, produces smooth muscle relaxation,
decreases mucus secretion.
■ Intranasal:
● Decreases response to seasonal, perennial rhinitis.
● Dosage:
○ Asthma
■ Oral inhalation:
● (QVAR):
○ ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
■ (Pts not on inhaled corticosteroids):
● Initially 40–80 mcg twice daily.
■ (Previously on inhaled corticosteroids):
● Initially, 40–320 mcg twice daily. Maximum:! 320
mcg twice daily.
○ CHILDREN 5–11 YRS:
■ Initially, 40 mcg twice daily. Maximum:! 80 mcg twice daily.
○ Rhinitis, Prevention of Recurrence of Nasal Polyps
 ■ Nasal inhalation:
● (Beconase AQ):
○ ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
■ 1–2 sprays (42 or 84 mcg) in each nostril twice daily.
Maximum: 336 mcg/day.
○ CHILDREN 6–11 YRS:
■ 1 spray (42 mcg) each nostril twice daily (total dose: 168
mcg daily). May increase to 2 sprays (84 mcg) 2 times/day
(total dose 336 mcg daily). Once adequate control
achieved, decrease to 1 spray (42 mcg) in each nostril
twice daily (total dose: 168 mcg daily).
○ Allergic Rhinitis
■ Nasal inhalation:
● (QNASL): ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 80 mcg/spray: 2 sprays in each nostril daily. Maximum:! 320 mcg
(4 sprays/day).
● CHILDREN, 4–11 YRS OF AGE:
○ 40 mcg/ spray: 1 spray each nostril once daily. Maximum:! 80
mcg/day.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ Acute hypersensitivity reaction (urticaria, angioedema, severe bronchospasm) occurs
rarely. Change from systemic to local steroid therapy may unmask previously
suppressed bronchial asthma condition.
02. Budesonide
● Definition:
○ Budesonide is a glucocorticosteroid used in the management of seasonal or perennial
allergic rhinitis in adults and children 6 yrs and older.
● Brand Names:
○ Entocort EC, Pulmicort Flexhaler, Pulmicort, Rhinocort Allergy, Uceris
● Generic Name:
○ Budesonide
● Indications:
○ Budesonide is indicated for:
■ Rhinitis
■ Bronchial Asthma
■ Crohn’s Disease
■ Ulcerative Colitis
● Pharmacodynamics:
○ Budesonide is a glucocorticosteroid that inhibits the accumulation of inflammatory cells;
controls rate of protein synthesis; decreases migration of polymorphonuclear leukocytes
(reverses capillary permeability and lysosomal stabilization at cellular level) which
relieves symptoms of allergic rhinitis, asthma, Crohn’s disease.
● Pharmacokinetics:
○ Minimally absorbed from nasal tissue; moderately absorbed from inhalation.
○ Protein binding: 88%.
 ○ Primarily metabolized in liver.
○ Half-life: 2–3 hrs.
Form Onset Peak Duration

Pulmicort 2–8 days 4–6 wks -

Respules

Rhinocort 10 hrs 2 wks -

Aqua
● Mechanism of Action:
○ Inhibits accumulation of inflammatory cells; controls rate of protein synthesis; decreases
migration of polymorphonuclear leukocytes (reverses capillary permeability and
lysosomal stabilization at cellular level).
○ Therapeutic Effect: Relieves symptoms of allergic rhinitis, asthma, Crohn’s disease.
● Dosage:
○ Rhinitis
■ Intranasal: (Rx):
● ADULTS, ELDERLY, CHILDREN 6 YRS AND OLDER:
○ 1 spray (32 mcg) in each nostril once daily. Maximum: 4 sprays in
each nostril once daily for adults and children 12 yrs and older; 2
sprays in each nostril once daily for children 6–11 yrs.
■ Intranasal: (OTC):
● ADULTS, ELDERLY, CHILDREN 6 YRS AND OLDER:
○ 2 sprays in each nostril once daily. May decrease to 1 spray in
each nostril once daily.
○ Bronchial Asthma
■ Nebulization:
● CHILDREN 12 MOS–8 YRS:
○ (Previous therapy with bronchodilators alone):
■ 0.5 mg/day as single dose or 2 divided doses. Maximum:!
0.5 mg/ day.
○ (Previous therapy with inhaled corticosteroids):
■ 0.5 mg/day as single dose or 2 divided doses. Maximum: 1
mg/day.
○ (Previous therapy of oral corticosteroids):
■ 1 mg/day as single dose in 2 divided doses. Maximum:! 1
mg/day.
■ Oral inhalation:
● Pulmicort Flexhaler)
○ ADULTS, ELDERLY:
■ Initially, 360 mcg 2 times/day. Maximum:! 720 mcg 2
times/day.
○ CHILDREN, 6 YRS AND OLDER:
■ 180 mcg 2 times/day. Maximum: 360 mcg 2 times/day.
○ Crohn’s Disease
■ PO (capsule):
● ADULTS, ELDERLY:
○ 9 mg once daily for up to 8 wks.
 ○ Recurring episodes may be treated with a repeat 8-wk course of
treatment.
○ Maintenance of remission:
■ 6 mg once daily for up to 3 mos.
○ Ulcerative Colitis
■ PO (tablet):
● ADULTS, ELDERLY: 9 mg once daily in morning for up to 8 wks.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ Acute hypersensitivity reaction (urticaria, angioedema, severe bronchospasm) occurs
rarely.
03. Fluticasone
● Definition: Fluticasone is a corticosteroid used in the management of nasal symptoms of
perennial nonallergic rhinitis in adults and children 4 yrs and older, management of seasonal
and perennial allergic rhinitis in adults, children 2 yrs and older, treatment of nasal polyps in pts
18 yrs and older, relief of hayfever/other upper respiratory allergies, relief of
inflammation/pruritus associated with steroid-responsive disorders (e.g., contact dermatitis,
eczema), atopic dermatitis, maintenance treatment of bronchial asthma as prophylactic therapy.
● Brand Names: Arnuity Ellipta, Cutivate, Flonase, Flonase Allergy Relief, Flovent Diskus,
Xhance, Flonase Sensimist
● Generic Name: Fluticasone
● Indications:
○ Nonallergic Rhinitis
○ Allergic Rhinitis
○ Nasal Polyps
○ Maintenance Treatment of Asthma
● Pharmacodynamics:
○ Fluticasone is a corticosteroid used in the management of nasal symptoms of perennial
nonallergic rhinitis in adults and children 4 yrs and older, management of seasonal and
perennial allergic rhinitis in adults, children 2 yrs and older, treatment of nasal polyps in
pts 18 yrs and older, relief of hayfever/other upper respiratory allergies, relief of
inflammation/pruritus associated with steroid-responsive disorders (e.g., contact
dermatitis, eczema), atopic dermatitis, maintenance treatment of bronchial asthma as
prophylactic therapy. It acts as a potent vasoconstrictor, anti-inflammatory, thus
preventing, and controlling inflammation.
● Pharmacokinetics:
○ Inhalation/intranasal:
■ Protein binding: 91%.
■ Metabolized in liver.
■ Excreted in urine.
■ Half-life:! 3–7.8 hrs.
○ Topical:
■ Amount absorbed depends on affected area and skin condition (absorption
increased with fever, hydration, inflamed or denuded skin).
● Mechanism of Action:
○ Direct local effect as potent vasoconstrictor, anti-inflammatory.
 ○ Therapeutic Effect: Prevents, controls inflammation.
● Dosage:
○ Nonallergic Rhinitis
■ Intranasal:
● Flonase:
● ADULTS, ELDERLY:
○ Initially, 200 mcg (2 sprays in each nostril once daily or 1 spray in
each nostril q12h).
○ Maintenance: 1 spray in each nostril once daily. May increase to
100 mcg (2 sprays) in each nostril. Maximum: ! 200 mcg/day.
○ CHILDREN 4 YRS AND OLDER:
■ Initially, 100 mcg (1 spray in each nostril once daily).
Maximum:! 200 mcg/day (2 sprays each nostril).
● Flonase Sensimist:
○ ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
■ 110 mcg (2 sprays in each nostril) once daily.
■ Maintenance: ! 55 mcg (1 spray in each nostril) once daily.
○ CHILDREN 2–11 YRS:
■ 55 mcg (1 spray in each nostril) once daily.
○ Allergic Rhinitis
■ (Flonase Sensimist):
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 110 mcg (2 sprays in each nostril) once daily.
○ Maintenance: 55 mcg (1 spray in each nostril) once daily.
● CHILDREN 2–11 YRS:
○ 55 mcg (1 spray in each nostril) once daily.
○ Usual Topical Dosage
■ Note: Ointment for adults only.
■ Topical:
● ADULTS, ELDERLY, CHILDREN 3 MOS AND OLDER:
○ Apply sparingly to affected area once or twice daily.
○ Nasal Polyps
■ (Xhance):
■ ADULTS, ELDERLY:
● 93 mcg (1 spray) per nostril twice daily. May increase to 2 sprays twice
daily.
○ Maintenance Treatment of Asthma
■ Inhalation powder: (Arnuity Ellipta):
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 100–200 mcg once daily. Maximum:! 200 mcg/day.
● CHILDREN 5–11 YRS: 50 mcg once daily.
■ (Flovent Diskus):
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:!
○ Initially, 100 mcg twice daily. Maximum:! 500 mcg twice daily.
■ (Flovent HFA):
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:!
○ 88 mcg twice daily. Maximum:! 440 mcg twice daily.
 ● USUAL PEDIATRIC DOSE (4–11 YRS):
○ (Flovent Diskus):!
■ Initially, 50 mcg twice daily. May increase to 100 mcg twice
daily.
○ (Flovent HFA):! 88 mcg twice daily.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment. (Arnuity Ellipta):
■ Use caution in hepatic impairment.
● Adverse Effect:
○ None known.
04. Ciclesonide
● Definition: Ciclesonide is a glucocorticoid used in the symptomatic relief of nasal symptoms
associated with seasonal and perennial allergic rhinitis in adults and adolescents.
● Brand Names:
○ Alvesco, Omnaris, Zetonna
● Generic Name: ciclesonide
● Indications:
○ For the treatment of nasal symptoms associated with seasonal and perennial allergic
rhinitis in adults and adolescents 12 years of age and older.
● Pharmacodynamics:
○ Ciclesonide is a pro-drug that is enzymatically hydrolyzed to a pharmacologically active
metabolite, C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1) following intranasal
application. Des-ciclesonide has anti-inflammatory activity with affinity for the
glucocorticoid receptor that is 120 times higher than the parent compound. The precise
mechanism through which ciclesonide affects allergic rhinitis symptoms is not known.
Corticosteroids have been shown to have a wide range of effects on multiple cell types
(e.g., mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and
mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic
inflammation.
● Pharmacokinetics:
○ Clearance: 152 L/hr [Following IV administration of 800 mcg of ciclesonide
● Mechanism of Action:
○ Glucocorticoids such as ciclesonide can inhibit leukocyte infiltration at the site of
inflammation, interfere with mediators of inflammatory response, and suppress humoral
immune responses. The antiinflammatory actions of glucocorticoids are thought to
involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis
of potent mediators of inflammation such as prostaglandins and leukotrienes.
Ciclesonide reduces inflammatory reaction by limiting the capillary dilatation and
permeability of the vascular structures. These compounds restrict the accumulation of
polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive
kinins. Recent research suggests that corticosteroids may inhibit the release of
arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins.
Ciclesonide is a glucocorticoid receptor agonist. On binding, the corticoreceptor-ligand
complex translocates itself into the cell nucleus, where it binds to many glucocorticoid
response elements (GRE) in the promoter region of the target genes. The DNA bound
receptor then interacts with basic transcription factors, causing an increase or decrease
 in expression of specific target genes, including suppression of IL2 (interleukin 2)
expression.
● Dosage: one or two puffs two times a day
● Adverse Effect:
○ Significant: Oral candidiasis (thrush), dysphonia, cough, bronchospasm, systemic effects
with high doses.
○ Cardiac disorders: Not typically associated.
○ Gastrointestinal disorders: Not typically associated.
○ General disorders and administration site conditions: Not typically associated.
○ Metabolism and nutrition disorders: Not typically associated.
○ Musculoskeletal and connective tissue disorders: Not typically associated.
05. Mometasone
● Definition: Mometasone is an adrenocorticosteroid used in the treatment of nasal symptoms of
seasonal/perennial allergic rhinitis in adults, children 2 yrs and older.
● Brand Names:
○ Asmanex, Asmanex HFA, Elocon, Nasonex, Apo-Mometasone
● Generic Name: Mometasone
● Indications:
○ Allergic Rhinitis
○ Asthma
○ Nasal Polyp
● Pharmacodynamics:
○ Mometasone is an adrenocorticosteroid used in the treatment of nasal symptoms of
seasonal/perennial allergic rhinitis in adults, children 2 yrs and older. It acts by inhibiting
formation, release, and activity of mediators of inflammation (e.g., histamine, kinins) and
reversing the dilation and increased nasal permeability of inflammation which improves
symptoms of asthma, rhinitis.
● Pharmacokinetics:
○ Undetectable in plasma.
○ Protein binding: 98%–99%.
○ Swallowed portion undergoes extensive metabolism.
○ Excreted in bile (74%), urine (8%).
○ Half-life: 5 hrs.
● Mechanism of Action:
○ Inhibits formation, release, and activity of mediators of inflammation (e.g., histamine,
kinins). Reverses the dilation and increased nasal permeability of inflammation.
○ Therapeutic Effect:! Improves symptoms of asthma, rhinitis.
● Dosage:
○ Allergic Rhinitis
■ Nasal Spray:
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ 2 sprays (100 mcg) in each nostril once daily. Total daily dose:
200 mcg.
○ When used to prevent nasal rhinitis, begin 2–4 wks before start of
pollen season.
● CHILDREN 2–11 YRS:
 ○ 1 spray (50 mcg) in each nostril once daily. Total daily dose: 100
mcg.
○ Asthma
■ Inhalation:
■ ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER
● (Previous therapy with bronchodilators):
○ Asmanex):
■ Initially, inhale 220 mcg (1 puff) once daily. Maximum: 440
mcg/day as single or 2 divided doses.
● Previous therapy with inhaled corticosteroids):
○ Asmanex HFA):
■ Initially, 200 mcg twice daily. Maximum: 400 mcg twice
daily.
● (Previous therapy with oral corticosteroids):
○ (Asmanex): 440 mcg (2 puffs) twice daily.
○ (Asmanex HFA): 400 mcg twice daily. Reduce predniSONE no
faster than 2.5 mg/day beginning after at least 1 wk of
mometasone.
■ CHILDREN 4–11 YRS:
● (Asmanex): 110 mcg once daily in evening.
○ Skin Disease
■ Topical:
● ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
○ Apply cream, lotion, or ointment sparingly to affected area once
daily.
○ Nasal Polyp
■ Nasal Spray:
● ADULTS, ELDERLY:
○ 2 sprays (100 mcg) in each nostril once or twice daily. Total daily
dose: 400 mcg.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ Acute hypersensitivity reaction (urticaria, angioedema, severe bronchospasm) occurs
rarely. Transfer from systemic to local steroid therapy may unmask previously
suppressed bronchial asthma condition.
06. Triamcinolone Acetonide
● Definition:
● Brand Names:
● Generic Name:
● Indications:
● Pharmacodynamics:
● Pharmacokinetics:
● Mechanism of Action:
● Dosage:
● Adverse Effect:
LEUKOTRIENE MODIFIERS
01. Montelukast
● Definition: Montelukast is a leukotriene receptor inhibitor used for prophylaxis, chronic treatment
of asthma, prevention of exercise-induced bronchoconstriction. Relief of symptoms of seasonal
allergic rhinitis (hay fever), perennial allergic rhinitis.
● Brand Names: Singulair
● Generic Name: Montelukast
● Indications:
○ Bronchial Asthma
○ Seasonal Allergic Rhinitis
○ Perennial allergic rhinitis
○ Exercise-Induced Bronchoconstriction Prevention
● Pharmacodynamics:
○ Montelukast is a leukotriene receptor inhibitor used for prophylaxis, chronic treatment of
asthma, prevention of exercise-induced bronchoconstriction. Relief of symptoms of
seasonal allergic rhinitis (hay fever), perennial allergic rhinitis. It binds to cysteinyl
leukotriene receptors, inhibiting effects of leukotrienes on bronchial smooth muscle
which decreases bronchoconstriction, vascular permeability, mucosal edema, mucus
production
● Pharmacokinetics:
○ Duration: 24 hrs
○ Rapidly absorbed from GI tract.
○ Protein binding: 99%.
○ Extensively metabolized in liver.
○ Excreted almost exclusively in feces.
○ Half-life: 2.7–5.5 hrs (slightly longer in elderly).
● Mechanism of Action:
○ Binds to cysteinyl leukotriene receptors, inhibiting effects of leukotrienes on bronchial
smooth muscle.
○ Therapeutic Effect: Decreases bronchoconstriction, vascular permeability, mucosal
edema, mucus production
● Dosage:
○ Bronchial Asthma
■ PO:
● ADULTS, ELDERLY, CHILDREN 15 YRS AND OLDER:
○ One 10-mg tablet daily, taken in the evening.
● CHILDREN 6–14 YRS:
○ One 5-mg chewable tablet daily, taken in the evening.
● CHILDREN 2–5 YRS:
○ One 4-mg chewable tablet or oral granules daily, taken in the
evening.
● CHILDREN 6–23 MOS:
○ 4 mg (oral granules) once daily in the evening.
○ Seasonal Allergic Rhinitis
■ PO: ADULTS, ELDERLY, CHILDREN 15 YRS AND OLDER:
● One 10-mg tablet, taken in the evening.
■ CHILDREN 6–14 YRS:
 ● One 5-mg chewable tablet, taken in the evening.
■ CHILDREN 2–5 YRS:
● One 4-mg chewable tablet, or oral granules taken in the evening.
○ Perennial Allergic Rhinitis
■ PO:
● ADULTS, ELDERLY, CHILDREN 15 YRS AND OLDER:
○ One 10-mg tablet, taken in the evening.
● CHILDREN 6–14 YRS:
○ One 5-mg chewable tablet, taken in the evening.
● CHILDREN 2–5 YRS:
○ One 4-mg chewable tablet or oral granules, taken in the evening.
● CHILDREN 6–23 MOS:
○ 4 mg oral granules, taken in the evening.
○ Exercise-Induced Bronchoconstriction Prevention
■ PO:
● ADULTS, ELDERLY, CHILDREN 15 YRS AND OLDER:
○ 10 mg 2 or more hrs before exercise. No additional doses within
24 hrs.
● CHILDREN 6–14 YRS:
○ 5 mg (chew tab) 2 or more hrs prior to exercise. No additional
doses within 24 hrs.
○ Dosage in Renal/Hepatic Impairment
■ No dose adjustment.
● Adverse Effect:
○ Suicidal ideation and behavior, depression have been noted.
02. Zafirlukast
● Definition: Leukotriene receptor antagonist which is used for prophylaxis, chronic treatment of
bronchial asthma in adults and children 5 yrs and older
● Brand Names: Accolate
● Generic Name: Zafirlukast
● Indications:
○ Bronchial Asthma prophylaxis
● Pharmacodynamics:
○ Leukotriene receptor antagonist which is used for prophylaxis, chronic treatment of
bronchial asthma in adults and children 5 yrs and older. It binds to cysteinyl leukotriene
receptors, inhibiting effects of leukotrienes on bronchial smooth muscle and decreases
bronchoconstriction, vascular permeability, mucosal edema, mucus production
● Pharmacokinetics:
○ Rapidly absorbed after PO administration (food reduces absorption).
○ Protein binding: 99%.
○ Metabolized in liver.
○ Primarily excreted in feces.
○ Unknown if removed by hemodialysis.
○ Half-life: 10 hrs.
● Mechanism of Action:
○ Binds to cysteinyl leukotriene receptors, inhibiting effects of leukotrienes on bronchial
smooth muscle.
 ○ Therapeutic Effect: Decreases bronchoconstriction, vascular permeability, mucosal
edema, mucus production
● Dosage:
○ Bronchial Asthma
■ PO: ADULTS, ELDERLY, CHILDREN 12 YRS AND OLDER:
● 20 mg twice daily.
■ CHILDREN 5–11 YRS:
● 10 mg twice daily
● Adverse Effect:
○ Concurrent administration of inhaled corticosteroids increases risk of upper respiratory
tract infection.
03. Zileuton
● Definition: Zileuton is a leukotriene synthesis inhibitor used in the prophylaxis and treatment of
chronic asthma.
● Brand Names: Zyflo
● Generic Name: Zileuton
● Indications:
○ For the prophylaxis and chronic treatment of asthma in adults and children 12
years of age and older.
● Pharmacodynamics:
○ Zileuton is an asthma drug that differs chemically and pharmacologically from other
antiasthmatic agents. It blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an
enzyme of the eicosanoid synthesis pathway. Current data indicates that asthma is a
chronic inflammatory disorder of the airways involving the production and activity of
several endogenous inflammatory mediators, including leukotrienes. Sulfido-peptide
leukotrienes (LTC4, LTD4, LTE4, also known as the slow-releasing substances of
anaphylaxis) and LTB4, a chemoattractant for neutrophils and eosinophils, are derived
from the initial unstable product of arachidonic acid metabolism, leukotriene A4 (LTA4),
and can be measured in a number of biological fluids including bronchoalveolar lavage
fluid (BALF) from asthmatic patients. In humans, pretreatment with zileuton attenuated
bronchoconstriction caused by cold air challenge in patients with asthma.
● Pharmacokinetics:
○ Half-life: 2.5 hrs
○ Protein binding: 93% bound to plasma proteins, primarily to albumin.
○ Metabolism: Hepatic
● Mechanism of Action:
○ Leukotrienes are substances that induce numerous biological effects including
augmentation of neutrophil and eosinophil migration, neutrophil and monocyte
aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle
contraction. These effects contribute to inflammation, edema, mucus secretion, and
bronchoconstriction in the airways of asthmatic patients. Zileuton relieves such
symptoms through its selective inhibition of 5-lipoxygenase, the enzyme that catalyzes
the formation of leukotrienes from arachidonic acid. Specifically, it inhibits leukotriene
LTB4, LTC4, LTD4, and LTE4 formation. Both the R(+) and S(-) enantiomers are
pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems. Due to the role
of leukotrienes in the pathogenesis of asthma, modulation of leukotriene formation by
 interruption of 5-lipoxygenase activity may reduce airway symptoms, decrease bronchial
smooth muscle tone, and improve asthma control.
● Dosage:
○ Oral
■ Chronic asthma
● Adult: 600 mg 4 times daily (immediate-release); 1200 mg bid (controlled-
release).
● Elderly: No dosage adjustment needed.
● Child: ≥12 yr Same as adult dose.
○ Renal Impairment
■ No dosage adjustment needed.
○ Hepatic Impairment
■ Contraindicated.
● Adverse Effect:
○ Headache, dizziness, pain including pharyngolaryngeal pain, GI disturbances, myalgia,
arthralgia, sinusitis, conjunctivitis, fever, hypertonia, lymphadenopathy, malaise,
neuropsychiatric events (e.g. sleep disorders, behaviour changes), UTI, vaginitis,
hypersensitivity, urticaria, rash, leucopenia, jaundice, hyperbilirubinaemia and elevated
liver enzymes.
○ Potentially Fatal: Severe hepatic injury.
MAST CELL STABILIZERS
01. Cromolyn Sodium
● Definition: Cromolyn is a medication that manages symptoms of mastocytosis. This condition
causes your body to produce too many mast cells. Mast cells are immune cells that build up
under your skin and/or in your bones, intestines and other organs.
● Brand Names: Gastrocrom
● Generic Name: Cromolyn Sodium
● Indications:
○ Mastocytosis
● Pharmacodynamics:
○ Cromolyn sodium is a mast cell stabilizer that prevents the subsequent release of
inflammatory mediators, including histamine and leukotrienes, which cause allergic
symptoms and bronchoconstriction
● Pharmacokinetics:
○ Bioavailability: 0.5-2%
○ Peak plasma time: 15 min
○ Peak plasma concentration: 9 ng/mL
○ Half-life: 80-90 min
○ Onset: 2-6 weeks (PO)
○ Duration: 6 hr
○ Excretion: Feces (98%, unabsorbed drugs); urine (<0.5%)
● Mechanism of Action:
○ Mast cell stabilizer; inhibits release of histamine, leukotrienes, and slow-reacting
substance of anaphylaxis from mast cell by inhibiting degranulation following exposure
to reactive antigens
● Dosage:
○ Dosage Forms & Strengths
■ oral concentrate
● 100mg/5mL
● Adverse Effect:
○ Diarrhea
○ Headache
○ Angioedema
○ Premature ventricular contractions
○ Hypoesthesia
○ Lightheadedness
○ Flushing
○ Palpitation
○ Erythema
○ Postprandial
○ Photosensitivity
○ Behavior changes
○ Psychosis
○ Esophagospasm
○ Nausea
○ Abdominal pain
○ Pancytopenia
 ○ Polycythemia
○ Stomatitis
○ Neutropenia
○ Rash
○ Pruritus
02. Nedocromil Sodium
● Definition: Nedocromil is a pyrano quinoline used to treat allergic conjunctivitis.
● Brand Names: Alocril
● Generic Name: Nedocromil Sodium
● Indications:
○ For the treatment of mild to moderate asthma
● Pharmacodynamics:
○ Nedocromil is an anti-inflammatory agent and can be administered directly to the
bronchial mucosa. It has significant inhibitory effect on allergen-induced early and late
asthmatic reactions and on bronchial hyperresponsiveness.
● Pharmacokinetics:
○ Protein binding - approximately 89% protein bound in human plasma over a
concentration range of 0.5 to 50 µg/mL
○ Metabolism: Nedocromil is not metabolized after IV administration and is excreted
unchanged.
○ Route of elimination: It is not metabolized and is eliminated primarily unchanged in urine
(70%) and feces (30%).
○ Half-life: ~3.3 hours
● Mechanism of Action:
○ Nedocromil has been shown to inhibit the in vitro activation of, and mediator release
from, a variety of inflammatory cell types associated with asthma, including eosinophils,
neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil inhibits
activation and release of inflammatory mediators such as histamine, prostaglandin D2
and leukotrienes c4 from different types of cells in the lumen and mucosa of the
bronchial tree. These mediators are derived from arachidonic acid metabolism through
the lipoxygenase and cyclo-oxygenase pathways. The mechanism of action of
nedocromil may be due partly to inhibition of axon reflexes and release of sensory
neuropeptides, such as substance P, neurokinin A, and calcitonin-geneñrelated
peptides. The result is inhibition of bradykinin-induced bronchoconstriction. Nedocromil
does not posess any bronchodilator, antihistamine, or corticosteroid activity.
● Dosage:
○ Inhalation/Respiratory
■ Chronic asthma
● Adult: As metered-dose inhaler (2 mg/dose): Initially, 2 actuations 4 times
daily. Dose may be reduced to bid, according to patient’s response.
● Child: ≥6 yr Same as adult dose.
○ Ophthalmic
■ Vernal keratoconjunctivitis
● Adult: As 2% soln: Instill 1 drop into each eye 4 times daily.
● Child: ≥6 yr Same as adult dose.
○ Ophthalmic
■ Allergic conjunctivitis
 ● Adult: As 2% soln: Instill 1-2 drop into each eye bid, may be increased to
4 times daily, if necessary. Max treatment duration: 12 wk.
● Child: ≥6 yr Same as adult dose.
● Adverse Effect:
○ Nervous: Headache.
○ GI: Nausea, vomiting, abdominal pain, dysgeusia, dyspepsia.
○ Resp: Cough, throat irritation, transient bronchospasm, pharyngitis, nasal congestion,
rhinitis.
○ Ophthalmologic: Burning, irritation, stinging, conjunctivitis, eye redness, photophobia.
METHYLXANTHINES
01. Aminophylline
● Definition:
○ Aminophylline is a bronchodilator consisting of theophylline that is used for the treatment
of bronchospasm due to asthma, emphysema and chronic bronchitis.
● Brand Names: Norphyl, Phyllocontin, Quibron-T.
● Generic Name: Aminophylline
● Indications:
○ For the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
● Pharmacodynamics:
○ Aminophylline is the ethylenediamine salt of theophylline. Theophylline stimulates the
CNS, skeletal muscles, and cardiac muscle. It relaxes certain smooth muscles in the
bronchi, produces diuresis, and causes an increase in gastric secretion.
● Pharmacokinetics:
○ Half-life: 7-9 Hours
○ Protein binding: 60%
● Mechanism of Action:
○ Aminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is
released from aminophylline, and theophylline relaxes the smooth muscle of the
bronchial airways and pulmonary blood vessels and reduces airway responsiveness to
histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits
type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking
down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation.
Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated
bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase
to prevent transcription of inflammatory genes that require the acetylation of histones for
transcription to begin.
● Dosage:
○ 15.2 to 17.7 milligrams (mg) per kg of body weight per day, divided and given every 4 to
6 hours
● Adverse Effect
○ Nausea.
○ Vomiting.
○ Headache.
○ Insomnia.
○ Seizures.
○ Irregular heartbeat.:
02. Theophylline
● Definition:
○ Theophylline is a xanthine used to manage the symptoms of asthma, COPD, and other
lung conditions caused by reversible airflow obstruction.
● Brand Names:
○ Elixophyllin, Elixophylline, Pulmophylline, Quibron-T, Theo-24, Theolair, Uniphyl
● Generic Name:
○ Theophylline
● Indications:
 ○ For the treatment of the symptoms and reversible airflow obstruction associated with
chronic asthma and other chronic lung diseases, such as emphysema and chronic
bronchitis.
● Pharmacodynamics:
○ Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is
used to treat asthma and bronchospasm. Theophylline has two distinct actions in the
airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation
(i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e.,
non-bronchodilator prophylactic effects).
● Pharmacokinetics:
○ Volume of distribution: 0.3 to 0.7 L/kg
○ Protein binding: 40%, primarily to albumin.
○ Metabolism: Hepatic
● Mechanism of Action:
○ Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood
vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and
allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase
(PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells,
possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B
receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states,
theophylline activates histone deacetylase to prevent transcription of inflammatory genes
that require the acetylation of histones for transcription to begin.
● Dosage:
○ Intravenous
○ Acute severe bronchospasm
■ Adult: Individualise dosing based on serum theophylline levels; use ideal body
weight to calculate dose. As adjunct to inhaled β2-agonists and systemic
corticosteroids for the treatment of acute exacerbations of symptoms and
reversible airflow obstruction associated with asthma and other chronic lung
diseases: As theophylline (anhydrous) in dextrose 5%: In patients who have not
received theophylline or other xanthine agents in the previous 24 hours: Loading
dose: 4.6 mg/kg via infusion over 30 minutes. Maintenance dose: Initially, 0.4
mg/kg/hour. Dosing recommendations are designed to achieve approx 10
mcg/mL serum levels. Dosage requirement must be guided by the patient’s
serum theophylline concentrations, clinical response, lifestyle, and co-morbidities
(refer to detailed product guideline).
■ Elderly: Dose reduction may be necessary.
■ Child: Individualise dosing based on serum theophylline levels; use ideal body
weight to calculate dose. In patients who have not received theophylline or other
xanthine agents in the previous 24 hours: Loading dose: 4.6 mg/kg via infusion
over 30 minutes. Maintenance dose: 1-<9 years Initially, 0.8 mg/kg/hour; 9-<12
years Initially, 0.7 mg/kg/hour. Dosing recommendations are designed to achieve
approx 10 mcg/mL serum levels. Dosage requirement must be guided by the
patient’s serum theophylline concentrations, clinical response, lifestyle, and co-
morbidities (refer to detailed product guideline).
○ Oral
■ Acute bronchospasm
 ● Adult: Individualise dosing based on serum theophylline levels; use ideal
body weight to calculate dose. As theophylline (anhydrous) immediate-
release solution: In patients who have not received theophylline or other
xanthine agents in the previous 24 hours: Loading dose: 5 mg/kg to
achieve an average of approx 10 mcg/mL peak serum levels. Dosage
requirement must be guided by the patient’s serum theophylline
concentrations, safety, and tolerability (refer to detailed product
guideline).
● Elderly: Dose reduction may be necessary.
○ Oral
■ Chronic bronchospasm
● Adult: Individualise dosing based on serum theophylline levels; use ideal
body weight to calculate dose. For the prophylaxis and treatment of
bronchospasm and reversible bronchoconstriction associated with
asthma, COPD, and chronic bronchitis: As theophylline (anhydrous)
modified-release tab/cap: 250-500 mg bid. Alternatively, 400 or 600 mg
once daily. As theophylline monohydrate modified-release tab: Usual
maintenance dose: 200 mg 12 hourly, may be adjusted to 300 mg or 400
mg 12 hourly based on clinical response. Dosage requirement must be
guided by the patient’s serum theophylline concentrations, safety, and
tolerability (refer to detailed product guideline).
■ Elderly: Dose reduction may be necessary.
■ Child: Individualise dosing based on serum theophylline levels; use
ideal body weight to calculate dose. As theophylline monohydrate
modified-release tab: ≥6 years Usual maintenance dose: 9 mg/kg bid.
As theophylline (anhydrous) modified-release tab/cap: 6-12 years 20-
35 kg: 125-250 mg bid; >12 years Same as adult dose. Dosage
requirement must be guided by the patient’s serum theophylline
concentrations, safety, and tolerability (refer to detailed product
guideline).
● Adverse Effect:
○ Significant: Exacerbated cardiac arrhythmias, urinary retention (particularly in elderly
males), exacerbated seizures, status epilepticus, exacerbated peptic ulcer.
○ Cardiac disorders: Atrial or sinus tachycardia, palpitations.
○ Gastrointestinal disorders: Abdominal pain, diarrhoea, gastric irritation, GERD, nausea,
vomiting.
○ Immune system disorders: Hypersensitivity (e.g. anaphylactic reaction, urticaria,
bronchospasm).
○ Investigations: Increased serum calcium, increased blood creatinine.
○ Metabolism and nutrition disorders: Hyperuricaemia, hypokalaemia, hyperglycaemia,
electrolyte imbalance.
○ Nervous system disorders: Dizziness, headache, tremor.
○ Psychiatric disorders: Agitation, anxiety, insomnia, sleep disorder, restlessness.
○ Renal and urinary disorders: Diuresis.
○ Skin and subcutaneous tissue disorders: Rash, pruritus.
○ Vascular disorders: Hypotension.
○ Potentially Fatal: Theophylline toxicity (with reduced clearance).
REFERENCES:
●
● Johnson, D.B., Merrel, B.J. & Bounds, C.G. (2024). Albuterol. National Library of Medicine. Retrieved
from [Link]
● Pirbuterol (Inhalation Route). (2024). Retrieved from
[Link]
● Pirbuterol (discontinued). (n.d.) Medscape. Retrieved from
[Link]
● Terbutaline (Rx). (n.d.). Medscape. Retrieved from [Link]
terbutaline-343135#0
● Terbutaline. (2024). Drugbank. Retrieved from [Link]
● Metaproterenol (Inhalation route). (2024). Mayo Clinic. Retrieved from
[Link]
20073605
● Cunha, J.P. (2022). Alupent. Rx List. Retrieved from [Link]
[Link]#description
● Metaproterenol. (2017). Medline Plus. Retrieved from
[Link]
%20prevent,making%20it%20easier%20to%20breathe.
● Arformoterol. (n.d.). Drugbank. Retrieved from [Link]
● Bambuterol (n.d.). Drugbank. Retrieved from [Link]
● Bambuterol. (n.d.). MIMS Philippines. Retrieved from
[Link]
● Clenbuterol. (2021). Drugbank. Retrieved from [Link]
● Salmeterol. (2024). Drugbank. Retrieved from [Link]
● Olodaterol. (n.d.). MIMS Philippines. Retrieved from
[Link]
● Vilanterol. (2023). Drugbank. Retrieved from [Link]