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Cell-to-cell communication occurs via what compounds?
Peptides
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Name 3 examples of Kinins (vasodilator).
- 1. Bradykinins
- 2. Natriuretic peptides
- 3. Vasoactive
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Name 4 examples of Intestinal Peptides (Vasodilators).
- 1. Substance P
- 2. Neurotensin
- 3. Calcitonin gene related peptide
- 4. Adrenomedullin
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Name 5 vasoconstricting peptides.
- 1. Angio II
- 2. Vasopressin
- 3. Endothelins
- 4. Neuropeptides Y
- 5. Urotensin
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T or F. The activation of renin is usually caused by vasoconstriction of the blood vessels.
FALSE (renin is stimulated by vasodilation and then causes vasoconstriction)
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What is an example of renin release inhibitor?
Angio II (negative feedback cycle)
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What are 4 stimulators of renin?
- 1. Decrease Na+ delivery
- 2. Decrease renal arteriole pressure
- 3. Sympathetic Nerve stimulation (B1)
- 4. cAMP
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Where is vasopressin produced?
Vasopressin--> produced in hypothalamus & supraoptic nucleus
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What stimulates vasopressin production?
Reductions in plasma volume
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What is the main result of vasopressin simulation?
-Increase WATER reabsorption
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T or F. Vasopressin is an arterial vasoconstrictor in times of physiologic stress, like shock.
True (improves BP)
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What are the 3 types of functions of vasopressin?
- 1. V1a--> mediates vasoconstriction
- 2. V1b--> potentiates release of adrenocorticotropic hormones
- 3. V2 --> mediate ADH hormones
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Vasopressin is a V1 & V2 agonist or antagonist?
Vasopressin is a V1/V2 agonist
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What are 3 examples of synthetic vasopressin and the name of a brand drug?
- -Terlipressin, relcovaptan, Conivaptan
- -BRAND- Pitressin
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What are 2 adverse effects of vasopressin?
- 1. Severe vasoconstriction
- 2. Water intoxication
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What are the 3 forms of endothelin and where do they come from?
- ET-1--> MAIN ONE, vascular endothelium
- ET-2--> kidneys & intestine
- ET-3--> brain, GI, kidneys
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Are ET-1 dose-dependent or time-dependent?
ET-1--> dose dependent
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What are some physiologic action T-1? (5)
- 1. rapid ⇓ in BP (nitric oxide) followed by prolonged ⇑
- 2. ⇑ BP as result of vascular smooth muscle contraction
- 3. Positive inotropic/chronotropic actions on the heart
- 4. Renal vasoconstriction (⇓ GFR,⇓ excretion)
- 5. Proliferation of vasc. smooth m, cardiac cells, glomerular cells
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Where are ETa receptors located?
smooth muscle cells (affinity for ET1&3)
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Where is ETb receptors located?
Vascular endothelial cells (affinity for ET1&3)
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What is an example of a nonselective endothelin receptor blocker and what is it's physiological result?
Bosentan--> causes vasodilation & decrease arterial pressure
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Kinins are a vasoconstrictor or vasodilator?
Vasodilator
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What are 2 significant roles of kinins?
In inflammation & pain
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What is the MOA of kinins?
-Vasodilation of vasculature in heart, skeletal muscle, & liver
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What is the respiratory effect of kinins?
Bronchoconstriction--> contraction of smooth muscles
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What is bradykinin found in the body?
Plasma
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Describe the 2 active roles of bradykinin?
- -Symptoms of inflammation
- - Eliciting pain in nociceptive afferents of skin & viscera
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What HTN medication can also stop circulation of bradykinin?
ACE-Inhibitor
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What does natriuretic mean?
Excretion of sodium into the urine
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What stimulates ANP production?
- Stretch of the aorta
- --> like in CHF, renal failure, SIADH
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What is the major effect of ANP?
Vasodilation and decrease arterial blood flow
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Where are BNP mainly synthesized?
HEART (released in response to atrial blood volumes)
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What is an adverse effect of BNP?
fatal renal failure (avoid BNP synthetics in patients with comorbidities_
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Where are C-type peptides mainly located?
CNS
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Which of the natriuretic peptides is a potent vasodilator?
C-type natriuretic peptide
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T or F. Histatmines are inflammation modulators
True (stored as basophils/mast cells)
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Quick review of the immunologic release.
- -IgE binds w/ mast cell on membrane
- -Cell degranulates--> release histamines
- -Cause immediate Type I rxn
- -Negative feedback loop mediated by H2 receptor
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What are 5 effects of H1 stimulation?
- 1. Increased venular permeability
- 2. Increased bronchial/intestinal smooth m contraction
- 3. Increase nasal mucous production
- 4. Widened pulse pressure
- 5. Increased HR/CO
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What are 3 responses to H2 stimulation? (GI)
- 1. Increased venular permeability
- 2. Increased gastric acid secretion & airway mucous
- 3. Inhibition of neutrophil/eosinophil influx
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What are the 2 effects of histamine of the nervous system (H1 receptor)
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What are the 4 effects of histamine of the Cardio system
- 1. Decreased BP (vasodilation of arterioles
- 2. Reflex tachy
- 3. Flushing, H/A (vasodilation)
- 4. Edema--> leading to urticaria
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What is the bronchial smooth muscle effect of histamine?
Bronchoconstriction
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What is the GI effect of histamine?
contraction of intestinal smooth muscle
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Which H receptor plays the major role in stimulating gastric acid secretion?
H2 receptor
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What is the "triple response" of histamines?
- 1. erythema at site
- 2. Edema
- 3. Pruritis
- (4. flare)
- ***Primarily H2 effects
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Which anti-histamine generation has anti-cholinergic side effects?
First generation (very sedating too)
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Which histamine generation is used most for allergic rhinitis?
2nd generation
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Which Anti-histamine generation are mostly metabolized by CYP3A4 therefore having more drug interactions?
2nd generation
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T or F. 2nd generation have little or no sedation effects
True
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Which anti-H1 generation is useful in preventing nausea, motion sickness.
1st generation
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What are 6 pharmacodynamics of anti-histamines (mostly 1st).
- 1. Sedation
- 2. Anti-nausea/anti-emetic
- 3. Anti-parkinson effects (treat dystonia)
- 4. anticholinergic actions (dry secretions, blurred vision, constipation)
- 5. alpha blocking actions (orthostatic hypotension)
- 6. Local anesthesia
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What are 3 side effects of Anti-H 1st generation.
- 1. CNS depression
- 2. Urinary retention
- 3. Difficulty urinating
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What body functions does serotonin have an impact (4)?
- 1. mood
- 2. sleep
- 3. appetite
- 4. temperature regulation
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T or F. The effects of serotonin are similar to Histamines.
True (stimulant of pain/itch & role in symptoms from insect/plant stings)
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T or F. Serotonin can can tachycardia and hypertension.
True (activates chemoreceptor reflex)
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What the effects of serotonin on the respiratory system?
- -Bronchoconstriction (with cancer patients)
- -Hyperventilation during chemoreceptor reflex
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What are some effects of serotonin on the cardio system?
- -Contraction of vascular smooth m
- -Constricts veins
- -causes platelet aggregation
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What are the effects of serotonin on the GI tract?
- -promotes peristalsis
- -Cisapride--> enhances motility at 5-HT4 receptors
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What are the 2 serotonin receptors in the brain that are responsible for migraines?
**activation causes vasoconstriction and pain diminishes
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Which drugs are 5HT1D/1B agonists?
Triptans
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What is the peak concentration time and half life of Triptans?
peak in 15min, half-life 2-4hrs
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What are some adverse effects of Triptans (4)?
- 1. altered sensation (warm/tingly)
- 2. muscle weakness
- 3. dizziness,
- 4. coronary vasospasm
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What patients should NOT receive Imitrex (triptan)?
-Patients w/ known CAD, uncontrolled HTN, or PVD because can cause coronary vasospasm
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What are 3 adverse reactions of Sumatriptan (imitrex)?
- 1. Dizziness/hot sensation
- 2. burning, heaviness, flushing
- 3. N/V
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What type of meds should not be taken concurrently with a sumatriptan?
SSRIs--> can cause serotonin syndrome
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What are common symptoms associated with asthma?
- History--> wheezing (esp at night), chest tightness, difficulty breathing
- **symptoms at night are key
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When mast cells degranulate, what mediators are released?
- 1. Histamine
- 2. Tryptase
- 3. Leukotrienes
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What PFT level is usually diagnostic for asthma?
FEV1 <80% based on age/height
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What are the 5 pathways that drugs work on to treat asthma?
- 1. Reduce amt of IgE bound to mast cells
- 2. Prevent mast cell degranulation
- 3. block actions of mediators (histamine/leukotrienes)
- 4. Inhibit effects of Ach
- 5. Directly relax smooth muscle
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What 2 drugs are acute relief meds for asthmas?
- 1. short acting beta agonists
- 2. short acting corticosteriods (usually PO)
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What 3 drugs help "control" asthma?
- 1. Long acting corticosteroids (ICS)
- 2. Long acting beta agonist (LABA)
- 3. Leukotriene pathway inhibitors
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Where are alpha 1 receptors primarily found?
- Smooth muscles of arterioles, eye, gut, skin, veins
- **so stim usually cause contraction of smooth muscle cells
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What are 3 effects of stimulation of Beta2?
- 1. Decrease GI motility
- 2. Bronchodilation
- 3. Vasodilation in skeletal/cardiac muscles
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Sympathomimetics delivered by inhalation have a direct effect on:
Pulmonary smooth muscle
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T or F. Epi stimulates which receptors?
alpha 1 & beta 1
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Name 4 drugs that are B2 selective drugs, short acting.
- 1. albuterol
- 2. terbutaline
- 3. metaproterenol
- 4. pibuterol
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Which B2 selective drugs can be given PO?
- 1. Albuterol
- 2. terbutaline
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What 2 drugs are Long-acting beta agonists?
1. Salmeterol & formoterol
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Why are LABAs not used as monotherapy?
-Have no anti-inflammatory effects and can make it worse by itself because it opens airways but has no effects on increase mucous
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T or F. LABAs should NOT be initiated in patients with significantly worsening/acutely deteriorating asthma
True
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When would Theophylline (a methylxanthine) be used for treatment?
Resistant COPD (a phosphodiesterase inhibitor--> ⇑cAMP--> smooth muscle relax, decreaes inflammation, stimulate cardio fxn)
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What are 4 side effects of methylxanthines?
- 1. Nervousness, insominia
- 2. tachy (increased CO)
- 3. Stimulates gastric acid and digestive enzymes
- 4. weak diuretic
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What is the therapeutic level of methylxanthines? What level does cardiac arrythmias occur?
- Therapeutic--> 5-20
- Arrhythmias--> >40
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What are the effects of Anti-muscarinic agents and when are the normally used in respiratory cases?
- 1. Inhibit Ach--> blocks contraction of airway smooth muscle and increases the secretion of mucous (not good?)
- 2. Frequently used for COPD, occassionally for acute asthma
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T or F. Anti-muscarinic agents may be used in combo with albuterol for enhancement effects.
True
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What 5 things are Inhaled corticosteriods shown to improve?
- 1. severity of symptoms
- 2. Airway size
- 3. Airway reactivity
- 4. frequency of exacerbations
- 5. Quality of life
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What asthma med is the "cornerstone" of long term asthma therapy?
ICS
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What are 4 side effects of ICS with long-term use?
- 1. cataracts
- 2. osteoporosis
- 3. thrush
- 4. reduction in bone marrow density (flovent)
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What hygiene teaching should be given to patients taking ICS?
Rinse mouth out after use--> can cause thrush
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T or F. ICS can take weeks to achieve maximal effect.
True
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After how many days of use should oral corticosteroids be tapered off of?
if used > 5days to avoid adrenal insufficiency
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What are the effects of Leukotrienes in the airway?
- 1. Bronchoconstriction
- 2. increases reactivity
- 3. mucosal edema
- 4. mucus hypersecretion
- 5. hypersensitivity to histamine
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Which leukotriene inhibitor prevents SYNTHESIS of leukotrienes?
Zileuton (Zyflo)
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Which leukotriene inhibitors prevent leukotriene BINDING to cell receptors?
- 1. Zafirlukast (Accolate)
- 2. Montelukast (SIngulair)
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What are the effects of Leukotriene Pathway Inhibitors (3)?
- 1. Increase airway size
- 2. Decrease airway reactivity
- 3. Decrease airway inflammation
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