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56 Cards in this Set

  • Front
  • Back
What are examples of inhaled, short acting beta 2 agonists?
Albuterol, Terbutaline, Bitolterol, Pirbuterol
What are adverse effects of beta 2 agonists?
Arrhythmias, tremors,
muscle cramps, metabolic disturbances,
and loss of effectiveness with chronic use.
What is an example of a muscarinic antagonist?
Ipratropium

-Use it with a beta 2 agonist inhaler drug.
What are examples of corticosteroids?

What do they accomplish?
Prednisone, Methylprednisolone and Prednisolone

Systemic short-course burst to establish control when initiating bronchodilator therapy. Basically by sensitizing the beta 2 receptors.
Do muscarinic antagonists work better for asthma ir COPD?
For COPD, because the PS nervous system plays a bigger role in COPD.
How do beta 2 agonists cause bronchodilation?
By stimulating adenyl cyclase.
How does Theophilline cause bronchodilation?
By inhibiting PDE and inhibiting adenosine.
What are the most effective available preventive therapy drugs, for asthma?
Anti-inflammatory steriods. (Nasal preparations are also used for rhinitis).
What are adverse effects of systemic corticosteriods?
Oral candidiasis, possible bone resorption (Inhalation). Adrenal suppression, metabolism, growth retardation (Oral)
How do corticosteriods cause bronchodilation?
Inhibits PLA2 causing a decrease in arachidonic acid. Then decreases gene-expression of inflammatory mediators
What do cromolyin and neocromil accomplish?

When are the used?
They stop the secretion of the chemical mediators that are released from eosinophils and basophils.

For mild persistent asthma. But not for ongoing attacks. They take weeks to show improvements.
How soon are histamine, proteases, heparin, and TNF released.
Immediately because they are preformed.
How soon are prostaglandins, PAF, and leukotrienes released?
Over minutes--they are lipid derived.
How soon are interleukins released?
Over hours. This requires new mRNA and protein synthesis.
Which drugs are leukotriene modifiers?
Zafirlukast, Montelukast, and Ziluton.
How does Ziluton work?
It inhibits lipooxygenase.
How do Zafirlukast and Montelukast work?
They block LTD-4 receptors on bronchial smooth muscle.
When are leukotriene modifiers used?
May substitute for Cromolyn etc. in “Responders” to treat mild persistent asthma. Oral preparations better for children. Very effective in 10% of asthmatics who are aspirin-sensitive.
What does lipooxygenase do?
What does COX 1/II do?
secretes leukotrienes.
secretes prostaglandins and thromboxanes.
When are Theophylline/Aminophylline used?
Used orally for long-term control of mild - moderate persistent asthma. Adjuvant to steroids for nocturnal symptoms.
What are the adverse effects of Theophylline and Aminophylline?
CNS Stimulation (Nervousness, anxiety), Arrhythmias, Nausea, Vomiting. Narrow therapeutic interval and wide interpatient variability in clearance requires serum monitoring of drug levels. Thus, long-acting beta-2 agonists are preferred.
What are two examples of long-active beta 2 agonists (LABA)?
Salmeterol (Inhaled) and Sustained Release Albuterol tablets - 12 hr bronchodilation (prophylaxis)

-Used in combination with inhaled steroids for moderate-severe persistent asthma.
What are the three roles of histamine?
1. mediates immediate allergic/inflammatory reactions
2. regulates gastric acid secretion
3. functions as a neurotransmitter/neuromodulator
When is histamine released?
Type I Immediate Allergic Reaction. IgE antibody sensitized cells exposed to antigen degranulate (Ca2+-dependent)

-d-tubocurarine and opioids displace histamine without degranulation
What can occur when a person takes aspirin?
Because it blocks the COX pathway, the lipooxygenase pathway will be used more and release leukotrienes.
Where are H1 receptors found?
Smooth muscle, e.g. blood vessels, bronchi, GI tract; endothelium & sensory nerve endings – Gq- coupled to elevation in IP3, Ca2+ and diacylglycerol.
Where are H2 receptors found?
Gastric parietal cells, cardiac and some vascular smooth muscle – Gs- coupled to elevation in cAMP.
Where are H3 receptors found?
Presynaptic nerves in brain & myenteric plexus – Gi- coupled to N-type calcium channels.
Where are H4 receptors found?
Blood cells in bone marrow and circulating blood, e.g. eosinophils & neutrophils - Gi- coupled to reduction of cAMP and intracellular Ca2+.

-These are not targeted clinically.
How does Histamine affect the cardiovascular system, mainly BP?
Decreases BP directly. And if it acts with nitric oxide, it causes vasodilation. Mainly H1 does this but there is some dependency on H2. H1 moves from the endothelium to the smooth muscle.
What does the vasodilation from histamine do?
Causes flushing, warmth, and headache.
What does Histamine do to contraction of the heart?
Increases rate and force. This is H2 dependent.
Which receptors cause leaky blood vessels?
H1--the endothelial cells contract and cause an increase in capillary permeability.
Which histamine receptors are responsible for the sensation of pain and itching?
H1. It also has a component of the urticarial response and reactions to insect bites.
Which histamine is involved in the axon reflex/triple response?
H1
What occurs in the triple response?
A sensory nerve is activated by histamine and depolarizes. Then an efferent nerve innervates a blood vessel, dilating it. This results in a flare.
What causes the cutaneous triple response?
Injection of histamine or morphine, or skin exposed to an allergen or insect bite.
What are the characteristics of the triple response?
1. Local reddening.
2. Edema from endothelial contraction.
3. Irregular flare from the axon reflex.
What does histamine do to bronchioles?
Bronchoconstriction from H1. This is not marked in non-asthmatics, but in asthmatics the effects are 100-1000 fold.
What happens to respiratory secretions from histamine?
Watery secretion from submucosal glands of the nasal cavity. It is mostly H1 mediated.
What does histamine do to the intestines?
It mediates its contraction, by H1 receptors.
What does histamine do to the stomach?
The H2 receptors mediate parietal cell acid production in gastric mucosa.
What are the 2nd generation anti-histamine drugs?
Fexofenadine, loraditdine, and cetrizine.
What do 1st generation drugs do, that 2nd generation drugs don't do?
They also block muscarinic receptors and cross the BBB (thus 2nd generation drugs do not cause sedation).
Lastly, 1st generation drugs have a shorter duration of action (4-6 hrs), while duration in 2nd generation is 12-24 hrs.
What are effects of antihistamines on the CNS?
the respiratory tract?
Sedation (if anti-cholinergic)
Decreased but thickened secretions (partly from anti-cholinergic), and bronchoconstriction
What are the effects of antihistamines on the blood vessels?
the heart?
Reversal of vasodilation, permeability, and the triple response.
Increased heart rate from anitcholinergic actions.
Do anithistamines work to treat asthma?
No.
What are two additional uses for antihistamines?
For motion sickness, from anticholinergic ability (Diphenhydramine).
And for sleep aids, from anticholinergic ability.
What are adverse effects of antihistamines?
sedation, dry mouth, blurred vision, urinary retention, and decreased GI motility.
What occurs when antihistamines are given to children?
paradoxical CNS stimulation--insomnia, nervousness and tremors.
What is the mechanism for allergies?
allergens bind to IgE antibodies on mast cells in the nose, and basophils in the blood, resulting in the release of preformed mediators.
Why are antihistamines not good decongestants?
Because there are multiple receptor types involved in congestion, and multiple mediators involved. Antihistamines target only H1 receptors.
What are good decongestants and how do they work?
Phenylephrine, pseudophedrine, and oxymetazoline. The cause vasoconstriction by acting as alpha-1 agonists.
Which drugs are antitussives?
Dextromethorphan, condeine, and hydrocodone.
What is an expectorant? What do they do?
A medication that helps bring up mucus and other material from the lungs, bronchi, and trachea. An example of an expectorant is guaifenesin. It thins the mucus and also lubricates the irritated respiratory tract.
What is special about anti-tussives?
They can be used for "skittling," causing hallucinogen effects. They do not contain antihistamine.