Asthma & Copd Pharm

Front 1

Short-acting β2-specific agonists

Back 1

albuterol, terbutaline (IV)

Front 2

Long-acting β2-specific agonists

Back 2

salmeterol, formoterol

Front 3

Non-selective β2-agonists

Back 3

Epinephrine: β1, β2, α2
Ephedrine: β1, β2, some α
Isoproterenol: β1, β2

Front 4

ANS control of the lungs

Back 4

SNS: bronchodilation - β2 receptors activated by epinephrine from adrenal gland - no direct sympathetic innervation
PSNS: bronchoconstriction - M2 & M3 receptors on SMCs, M1 & M3 receptors on submucosal glands

Front 5

When should LABAs be used?

Back 5

ONLY in combination with inhaled corticosteroids

Front 6

Effects of β2-agonists

Back 6

Acts on Gs GPCR.
Increased levels of cAMP - relaxation of SMCs and decreased proliferation.
Efflux of K+ - hyperpolarization of the cell - reduction in [Ca2+] - SMC relaxation
Can also cause inflammation through Gq/PLC and β-arrestin-2.

Front 7

Adverse effects of sympathomimetics

Back 7

N/V, HA.
Increased HR, reflex hypotension, cardiac arrhythmias. Hypokalemia, QT-prolongation. CNS toxicity (agitation, convulsions, coma, respiratory collapse).

Front 8

Adverse effects of antimuscarinics

Back 8

Pupil dilation, loss of accomodation.
Ipratropium is poorly absorbed, no systemic effects.

Front 9

Antimuscarinic agents

Back 9

Atropine, ipratropium

Front 10

Mechanism of Combivent & indication

Back 10

Ipratropium + albuterol
Indicated for COPD

Front 11

Methylxanthine agents

Back 11

Aminophylline, theophylline

Front 12

Mechanism of methylxanthine agents

Back 12

Increased cAMP by inhibiting PDE.
Blockage of muscle adenosine receptors.
Decreased release of mediators from mast cells.
Bronchodilation.
Anti-inflammation (inhibition of txn of histone deacetylase).
Increased CNS activity, gastric acid secretion, skeletal muscle strength. Weak diuretic.

Front 13

Adverse effects of methylxanthines

Back 13

Narrow therapeutic index. THINK COFFEE.
N/V, nervousness, HA, insomnia.
Higher serum levels: vomiting, hypokalemia, hyperglycemia, tachycardia, arrhythmias, tremor, neuromuscular irritability, seizures.

Front 14

Mechanism of cromolyns

Back 14

Alters chloride channel activity.
Inhibits degranulation of mast cells & eosinophils.
Inhibits cough by acting on nerves.
Reduces bronchial hyperactivity for exercise induced & antigen-inhaled asthma.
Prophylactic treatment.

Front 15

Adverse effecst of cromolyns

Back 15

Taste. Irritation of trachea.
Rare: chest pain, restlessness, hypotension, arrhythmias, N/V, CNS depression, seizures, anorexia.

Front 16

Anti-inflammatory agents

Back 16

Ciclesonide - best PK & PD
"onides" & "asones"

Front 17

Cushingoid Syndrome

Back 17

Central weight gain, thinning of extremities, thin skin, increased acne, facial hair growth, scalp hair loss in women, ruddy complexion, acanthosis, child obesity, HTN

Front 18

Leukotriene receptor blockers

Back 18

Monteleukast, zafirlukast

Front 19

Leukotriene synthesis inhibitors

Back 19

Zileuton
Blocks 5-lipooxygenase.

Front 20

Anti-IgE Ab

Back 20

Omalizumab

Front 21

Actions of LTEs in asthma

Back 21

LTB4 - neutrophil chemoattractant
Bronchial hyper-reactivity, bronchoconstriction, mucosal edema, increased mucus secretion

Front 22

Adverse effecs of LTE antagonists

Back 22

Zafirlukast - GI disturbance, HA, elevation of liver enzymse, tumors in rodents
Monteleukast - GI disturbances, laryngitis, pharyngitis, nausea, otitis, sinusitis, viral infections

Front 23

Adverse effects of zileuton

Back 23

Liver enzyme elevation. CYP1A2 substrate & inhibitor - INTERACTION WITH THEOPHYLLINE

Front 24

Adverse effects of omalizumab

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Serious allergic rxns. Redness, bruising, warmth, burning, stinging, itching, or pain at injection site. Increase in CV complications.

Front 25

Preferred therapies for asthma

Back 25

SABA as needed for attacks. Omalizumab for allergies
Step 2: low-dose ICS
Step 3: Low dose ICS + LABA
Step 4: medium-dose ICS + LABA
Step 5: high-dose ICS + LABA
Step 6: high-dose ICS + LABA + oral corticosteroid

Front 26

Drugs contraindicated in airway disease

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Sedatives, beta-blockers (β1 okay), aspirin & COX inhibitors, ACEI, local anesthetics containing EPI

Front 27

Mechanism of doxapram

Back 27

Respiratory stimulant for post-anesthesia/drug-induced respiratory depression/acute hypercapnia in COPD.
Activates peripheral carotid receptors. Short-acting.