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4q Pharm Test2 > Tx of Asthma And COPD, antihistamines > Flashcards

Tx of Asthma And COPD, antihistamines Flashcards

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1
Q

Asthma

A

narrowing of the airways, esp small airways

involves reversible airway obstruction, inflammation & increased airway responsiveness to a variety of stimuli

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2
Q

Inflammation in asthma contributors (4)

A

INFLAMMATORY CELLS: leukocytes, mast cells, EOSINOPHILS, neutrophils, alveolar mactophages & lymphocytes are seen in the airways

PROSTAGLANDINS: prostaglandin D2 is a potent bronchoconstricor

INTERLEUKINS-4,5 & 13: attract & activate eosinophils & stimulate IgE production by B lymphocytes
LEUKOTRIENES: liberated during inflammation in the lunch, cause bronkoconstriction & edema

PLATELET-ACTIVATING FACTOR: causes immediate bronchoconstriction & sustained airway hyperreactivity, edema & chemotaxis of eosinophils. selective antagonists are being developed
-also increased mucus production

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3
Q

often used to diagnose and characterize asthma

A

increased responsiveness to challenge with METHACHOLINE, HISTAMINE & EXERCISE are often used to dx and characterize asthma

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4
Q

B2-Adrenergic Agonists

A

MOST EFFECTIVE bronchodilators

B2 receptor stimulation ACTIVATES ADENLYATE CYCLASE & INCREASES cAMP, which causes RELAXATION OF SMOOTH MUSCLES IN THE BRONCHIOLES & STABILIZATION OF MAST CELLS

generally given by INHALATION, which restricts action to the lung & increases the speed of action, important in relieving bronchospasm

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5
Q

selective B2 agonists

A

are more effective at stimulating B2 receptors (of the lungs) than B1 (of the heart)

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6
Q

First line tx for asthma

A

selective B2 agonists

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7
Q

name the 3 fast-acting (immediate effect) beta 2 agonists

what is their duration of action

A

Albuterol (Ventolin)
Levalbuterol (Xopenex)
Pirbuterol (Maxair)

duration of action: 4-8 hours

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8
Q

Salmeterol (Servent)

A
  • lasts for 12 hours
  • very BRONCHOSELECTIVE & designed to have a long duration of action
  • decrease likelihood of bronchospasms & for nocturnal asthma
  • given PROPHYLACTICALLY on a CHRONIC BASES
  • a CORTICOSTEROID SHOULD ALWAYS BE GIVEN IN CONJUNCTION

effects take abt 20 mins to occur
so NOT EFFECTIVE FOR THE RELEIF OF ASTHMA ATTACK IN PROGRESS
pts need a fast acting bronchodilator (rescue inhaler)

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9
Q

Formoterol

A

long acting bronchodilator, like salmuterol

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10
Q

Advair (salmeterol/fluticasone)

A

intermediate acting bronchodilator & corticosteroid

salmeterol should always be given with a corticosteroid

pts will need a fast acting rescue inhaler too

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11
Q

Dulera (formoterol/mometasone)

A

long acting bronchodilator + a corticosteroid

-pts should be given a fast acting rescue inhaler (-buterol) in addition to this

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12
Q

Inhaled selective B2 agonists SEs

A

the have very few

tachycardia
nervousness & dizziness
tremor

generally ppl become tolerant to these effects & they are often short-lived

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13
Q

B2 agonist controversies

A

TOLERACE TO B2 agonists could occur w/long-term tx, but this is more of a prob in places other than the lungs

CONCOMITANT use of CORTICOSTEROIDS can prevent & in fact reverse, the phenomenon of tolerance & prevent loss of B receptors

so, unless B agonists are used only on an as-needed basis, standard practice is to combine them with an inhaled steroid

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14
Q

Ipratropium (Atrovent)
class

absorption

activity

USE

A
  • Muscarinic antagonist
  • QUATENARY compounds, not absorbed systemically but STAY IN THE LUNG

bronchodilation develops more SLOWLY than with the B2 agonists

USE:

  1. widely for COPD or emphysema
  2. used in conjunction with a B2 agonists when B2 alone is not sufficient to tx sxs or if pt cannot tolerate B-agonists
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15
Q

Combivent

A

Iptratroprium (muscarinic antagonist) combined w/ Albuterol in one spray

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16
Q

Tiotropium (Spiriva): what is it?

A

similar to ipratropium (muscarinic antagonist)
has a longer duration of action & only needs once a day administration
-may work in some patients who do not respond as well to ipratroprium

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17
Q

Theophylline (Theo-Dur)

class

2 main actions (contributing to therapeutic effect)

therapeutic effect

therapeutic index

A

CNS stimulant acts like caffeine-decreases fatigue, elevates mood

  1. BLOCKS ADENOSINE RECEPTORS, which normally cause bronchoconstriction & inflammation
  2. inhibits PHOSPHODIESTERASE, increases amt of cAMP, similar to beta2 stimulation

very effective bronchodilator, RELAXES SMOOTH MUSCLE< ESP BRONCHIOLES, stimulates cardiac muscle & acts as a diuretic in the kidney
-used in pts who don’t respond sufficiently to B2 agonists alone in COPD

VERY LOW THERPEUTIC INDEX

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18
Q

Theophiline (The-Dur) pharmokinetics: administration, elimination, affected by

A

given ORALLY in sustained release prep
rate of absorption varies, so ONCE A DOSE IS ESTABLISED, IT IS BETTER NOT TO SWITCH BETWEEN BRANDS (prob. w/ generic prescribing)

eliminated by liver

  • clearance increased 2x by phenytoin
  • smoking, rifampin, & oral contraceptives also increase clearance of theophylline

cimetidine DECREASES clearance

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19
Q

Theophylline: side effects & toxicity

A

CNS: NERVOUSNESS, INSOMNIA, similar to caffeine, anxiety & tremors can occur

Cardiac: increases rate & force of contraction; in higher doses, can cause tachycardia & may predispose to ARRHYTHMIAS

MUSCLE: increases contractility of diaphragm & decreases fatigue

weak diuretic effect

Toxicity: overdose can be fatal (U) due to arrhythmias & seizures

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20
Q

Corticosteroids: use in asthma

A

-used to DECREASE INFLAMMATION in airways

should ALWAYS be included with long acting B2 agonists

IMPROVE SYMPTOMS & DECREASE THE REQUIREMENTS FOR BETA-AGONISTS

beneficial effects begin in 1 wk, improvement can continue for months

oral steroids used in severe cases of asthma, when other things are not enough;

oral steroids often used for SHORT PERIODS of EXACERBATION to BRING SYMPTOMS INTO CONTROL, may be used prophylactically (U) do not cause serious SEs when used short term

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21
Q

5 inhaled steroids

A 
Beclomethasone
Flunisolide
Triamcinolone
Fluticasone
Budesonide
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22
Q

Inhaled steroids: side effects

A

oropharyngeal candidiasis (THRUSH)
HOARSENESS is common
modest decrease in BONE DENSITY in women

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23
Q

Oral Steroids (2)

A

Methylprednisone

Prednisone

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24
Q

Oral steroids: side effects
long term?
short term?

Study These Flashcards
A

Long term: SEs can be significant
osteoporosis
thinning of skin, hyperglycemia
truncal obesity

short term: hyperactivity, insomnia, restlessness, possibly psychotic txns, increase appetite, GI disturbances
-these all decrease as dose is decreased, drug is stopped

25
Leukotriene Inhibitors: what do they do? what are their benefits in asthma (3) what can't they do? (1) SEs (3)
leukotrienes are involved in the inflammation of asthma interfere w/the synthesis or receptor binding of leukotrienes benefits: -decrease the asthmatic response to exercise or cold air - decrease the need for inhaled oral steroids - may decrease need for inhaled steroids cannot stop and asthma attack in progress, inhaled B-agonists still needed SEs: slight increase in URIs, SORE THROAT, SLEEPINESS
26
3 drugs which block the leukotriene receptor
"-leukast"s Zafirlukast (Accolate) Montelukast (Singulair) Pranlukast (Ultaire)
27
Zileuton (Zyflo): what does it do how is it used what may it do
blocks 5-lipoxygenase & decreases synthesis of leukotrienes effective orally, must be taken CHRONICALLY may decrease asthmatic rxn to ASA & NSAIDS
28
``` Cromolyn sodium (Intal) Nedcromil (Tilade) ```
NOT a bronchodilator; INHIBITS RELEASE OF HISTAMINE FROM THE MAST CELLS used to tx asthma, esp in KIDS, but may work in some adults (U) inhaled, use SEVERAL TIMES A DAY CHRONICALLY to be effective PROPHYLAXIS -takes 2-3 months for effects to be seen can prevent development of asthma in response to allergens & induced by exercise few SEs: BAD TASTE is most common complaint
29
Omalizumab (Xolair): what is it use admin SEs
- monoclonal antibody targeted to IgE, prevents it from binding to mast cells & basophils - used to prevent allergic rxns in patients with moderate to severe asthma - may decrease need for steroids & reduce exacerbations subQ injection q 2-4 weeks may cause SERIOUS ALLERGIC & skin rxns
30
Histamine: involved in? stomach? highest concentration? central role in what?
neurotransmitter in brain, involved in arousal, neuroendocrine control & weight & temp regulation ENTOCHROMAFFIN-LIKE CELLS in stomach fundus release H->inc. gastric acid production highest cnctrtn in tissues that contain MAST CELLS, as well as in BASIPHILS in the blood -mast cells: prominent in nose, mouth feed, near pressure pts & bifurcations of blood vessels central role in IMMEDIATE HYPERSENSTIVITY & ALLERGIC RXNS
31
Histamine release from mast cells can be triggered by: (5)
1. intrxn of IgE & antigen- antibodies bind to mast cells & basophils via high affinity Fc receptors specific for IgE=the classic ALLERGIC RESPONSE 2. DRUGS, esp organic bases given IV: MORPHINE & CODEINE, RADIOCONTRAST DYES 3. VENOMS 4. scratching, cold, sun damage 5. certain cancers may increase mast cells resulting in increased histamine release
32
H1 receptor: what kind of receptor is it? what dose it do in 3 places? what drugs block it?
coupled to Gq stimulation inc. production of IP3 & DAG in CNS: produce wakefulness & inhibit appetitie in endothelium & blood vessels releases NO & causes vasodilation in other smooth muscles cause inc. calcium, leading to contraction classical "antihistamines" block the H1 receptor
33
H2 receptor
Gs, increases cAMP significant in secretion of gastric acid, heart, brain & on smooth muscles in blood vessels: leads to vasodilation
34
H3 receptor
Gi-linked, decreases cAMP found in brain, mostly presynaptically
35
H4 receptor
on leukocytes inbone marrow & circulating blood
36
histamine: cardiovascular effects
H1 stim causes vasodilation of small blood vessels (via NO): rapid short effects higher amts of histamine cause H2 receptor med. vasodlation: slower onset, longer duration dilation of blood vessels-> DECREASE BP w/ REFLEX TACHYCARDIA, FLUSHING of skin, feeling of WARMTH, & HA capillary permeability increased & endothelial cells separate in response to H1 stimulation-> HIVES & EDEMA LARGE DOSES of HISTAMINE->SHOCK due to decreased BP
37
histamine in respiratory system
BRONCHOSPASM (H1) due to inc. Ca2+, histamine stimulates secretory activity in the lung & inc. prostaglandin formation, small H2 bronchodilator effect too, bronchospasm is (U) mild in most ppl ASTHMATICS ARE VERY SENSITIVE TO THE EFFECTS OF HISTAMINE & likely to experience bronchospasm, may also involve irritation of vagal nerve endings
38
histamine effect on glandular tissue
INCREASED SECRETION OF GASTRIC ACID & pepsin from gastric mucosa (H2)
39
histamine: intradermal effects
LEWIS TRIPLE RESPONSE (wheal & flare) occurs after intradermal injection of histamine FLUSH: seconds, max w/in 1 min, due to dilation of capillaries FLARE: dilation of arterioles causing redness over a wider area, (response develops more slowly, due to stim of axon reflexes) WHEAL: swelling in the area of capillary dilation; appreas after 1-2mins & the result of edema due to increase capillary permeability pain & itching due to stimulation of nerve endings, transmitted to CNS
40
Manifestations of histamine release tx?
hay fever/allergic rhinitis hives & skin rashes ANAPHYLAXIS: life threatening -drop in BP, shock, respiratory difficulty, abdominal cramps, edema, hives, throat swells TX w/: EPINEPHRINE, STEROIDS, INJECTED ANTIHISTAMINES (BOTH H1 & H2 blockers used together (diphenhydramine & cimetidine)
41
H1 receptor antagonists
ALL ANTIHISTAMINES BLOCK H1 RECEPTORS - compete w/histamine so effects dependent on amt of histamine present - in severe rxns, may not be sufficient to block effect 1st gen drugs have CNS effects & often block muscarinic receptors 2nd gen drugs are very selective for H1 receptor & have little or no CNS effect most are OTC
42
First Generation H1 antagonists
enter the brain & many of them are quite SEDATING
43
Diphenhydramine & dimenhydrainate (Dramamine) | characteristics
H1 antagonists HIGHLY SEDATING SIGNIFICANT ANTICHOLINERGIC ACTIVITY
44
Doxylmaine (Unisom) use
H1 antagonist | sleep aid
45
Brompheniramine (Dimetane) & chlorpheniramine (Chlor-Trimeton)
1st gen H1 antagonists w/little sedative effect
46
Promethazine (Phenergan)
1st gen H1 antagonist | a phenothiazine derivative w/significant ANTI-EMETIC effect & is VERY SEDATING
47
drugs used for motion sickness (3)
first gen H1 antagonists w/SIGNIFICANT ANTICHOLINERGIC ACTIVITY eg. diphenhydramine (Bendryl) dimenhydrate (Dramamine) promethazine (Phenergram)
48
2nd gen H1 antagonists features (4)
1. do not enter the brain well 2. primarily block peripheral receptors 3. NOT anticholinergic, so NON-SEDATING & have few SEs 4. may be better at preventing allergic rxns than tx the once they occur
49
2nd gen antihistamines: pharmokinetcs
given orally well absorbed in GI tract onset of activity 15-30 mins duration of actin: some 4-6 hrs, some 12-24 hrs also topical and injectable preps most are metabolized by the liver some metabolized by CYP3A4 & cncntrations can increase when tx w/drugs that inhibit metabolism
50
which 2nd gen antihistamines are eliminated only be the kidney (3) advantage
CETIRIZINE (Zyrtex) levocetirizine (Zyxal) & activastine (Semprex) in pts w/liver dz or where drug intrxns are a concern
51
Antihistamines: clinical applications (5)
allergic RHINITIS, seasonal rhinitis & conjunctivitis: response is best if used prophylactically (esp. tru for 2nd gen drugs) ITCHING & HIVES: inhibits inc. in capillary permeability that causes edema & wheal MOTION SICKNESS: diphenhydramine, dimenhydrinate & promethazine (b/c of anticholinergic effects) SEDATION: 1st gen H1 antagonists-diphenhydramine, doxylamine SECRETIONS: 1st get drugs w/anticholinergic effects decrease salivary & lacrimal secretions & frequently in cold preps for this not effective inasthma
52
1st gen antihistamines: side effects
SEDATION: potentiated by alcohol, CNS depressants; may impair motor skills, esp pronounced in ELDERLY CONTRAINDICATION IN KIDS ANTICHOLINERGIC: dry mouth & resp passages, dry, hot skin, urinary retention ro frequency, urinary retention, constipation, blurred vision other CNS EFFECTS: dizziness, tinnitus, lassitude, poor coordination, fatigue, blurred vision, diplopia, paradoxical excitement, nervousness, restlessness & insomnia ALLERGIC RXS: can occur w/topical preps may lower seizure threshold
53
Side effects of ALL ANTIHISTAMINES
GI: anorexia, N/V, epigastric distress, constipation, diarrhea, effect reduced if given w/food -some ppl have inc. appetite & weight gain TERATOGENIC EFFECTS are POSSIBLE, so avoid using in pregnant OTC preps combined w/cold meds a/w death in young kids so NOT recommended in kids under the age of 4
54
Antihistamines: drug intrxns
don't take w/other CNS depressants incl. alcohol, phenzothiazines, benzodiazepines, & barbiturates ERYTHROMYCIN & KETOCONAZOLE may inhibit metabolist of 2nd gen antihistamines, CIMETIDINE also decreases metabolism GRAPEFRUIT JUICE INHIBITS CYP3A4 and INCREASES CONCENTRATIONS OF MANY DRUGS
55
Antihistamines: acute poisoning 1st gen effects 2nd gen effects
fairly nontoxic, but kids are likely to take overdoses sxs of 1st gen antihistamine poisoning-sim to those of atropine: excitement, convulsions, ataxia, hallucinations, tremors, fixed dilated pupils, flushed, hot skin, coma, cardiorespiratory collapse others: SEDATION, & DRY OF SALIVARY & BRONCHIAL SECRETIONS 2nd gen OD-may cause CARDIAC ARRHYTHMIAS
56
Cromolyn sodium & nedcromil what do they do use? administration?
inhibit release of histamine from mast cells used to tx asthma INHALED, need to be taken chronically in order to be effective
57
Azelastine: admin? what is it? what is it good for?
applied NASALLY NON-COMPETATIVE H1 BLOCKER that also decrease release of histamine from mast cells used for allergic rhinitis
58
Ceterizine (Zyrtec)
may also inhibit release of histamine from mast cells

4q Pharm Test2 (7 decks)

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