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Pharmacology
Lecture 3
51
Other
Graduate
02/01/2009

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Term
Catecholamines are...? And what part of the N.S. are they released from?
Definition
norepinephrine and epinephrine...and they are released from the sympathetic N.S. ganglion's
Term
Parasympathetic post-ganglionic fibers release?
Definition
acetylcholine
Term
What 2 substances inactivate the catecholamines?
Definition
monoamine oxidase (MAO) and catechol-o-methyl transferase (COMT)
Term
If you use a drug to inhibit MAO or COMT, what are you essentially doing? And what disorders are these drugs used for?
Definition
Since MAO & COMT are used in the body to break down catecholamines, if you take a drug that inhibits these enzymes, you will have more epinephrine & norepinephrine...Depression & Parkinson's disease are 2 disorders treated with MAO & COMT inhibitors
Term
Alpha 1 receptor stimulation causes:
Definition
vasoconstriction
Term
Stimulation of Dopaminergic receptors causes:
Definition
Vasoconstriction (these receptors are predominantly located in the renal and coronary vessels)
Term
Beta 2 receptors are located primarily where? And what does their stimulation cause?
Definition
In the lungs...And it causes vasodilation & increased HR & contractility
Term
What are the steps in the Enzymatic Synthesis of Catecholamines?
Definition
Tyrosine > Dopa > Dopamine > Norepinephrine > Epinephrine
Term
Name 2 alpha receptor agonists (stimulants):
Definition
Used for vasoconstriction (hypotensive shock) or as a nasal decongestant (the vasocontriction helps to dry up the blood vessels in the nasal cavity): phenylephrine (Neo-Synephrine®), & norepinephrine or levarterenol (Levophed®)
Term
Stimulation of ß-receptors leads to the activation of...?
Definition
adenylcyclase and to an increase in the intracellular concentration of cyclic AMP
Term
Name some clinical uses ß-agonists?
Definition
Bronchodilation for asthma and COPD (ß2); Cardiac stimulant (ß1); Tocolytic (uterine relaxant) – classic off-label use (torbutaline)
Term
Name the 4 main sympathetic N.S. receptors:
Definition
Alpha 1, Dopaminergic, Beta 1, and Beta 2
Term
Name the 2 main parasympathetic N.S. receptors:
Definition
Muscarinic & Nicotinic
Term
Antiadrenergic Drugs:
Definition
alpha blockers, and beta blockers
Term
Uses of ß-Blockers (8):
Definition
Cardiac arrhythmias,
Angina pectoris,
Hypertension,
Migraine headache prophylaxis,
Acute anxiety reaction,
Prevent recurrent M.I.,
Glaucoma (topically applied agents only),
Chronic (Congestive) heart failure;
Note: Not all Beta-blockers are approved for all these uses. The oldest, propranolol, is
approved for the first six of these indications
Term
Side Effects of ß-blockers:
Definition
Prolongs hypoglycemia, Bradycardia
Mental dullness, fatigue, decreased HDL cholesterol, Bronchospasms...use with caution in persons with diabetes b/c some B-blockers cause an increase in blood glucose, Not for Asthmatics or people with COPD, Not for people with peripheral vascular disease
Term
Uses of Cholinergic Agents:
Definition
Neurological diseases such as Alzheimer's and myasthenia gravis; Glaucoma—due to miotic effect; Dry mouth associated with Sjögren’s syndrome; To stimulate GIT and GUT (urinary retention)
Term
Side Effects of Cholinergic Agents (2):
Definition
Abdominal cramping and diarrhea (contraindicated in ulcers), & secretions (perspiration, saliva, etc.)
Term
Drugs that have anticholinergic effects are derived from natural sources such as the:
Definition
Atropa belladonna or “Deadly Night Shade”
Term
Uses of Anticholinergic Agents (8):
Definition
(1) Decreases glandular secretions, (2) “common cold” (to prevent rhinorrhea), (3) “drooling”
(in clients with cerebral palsy or other disabilities), (4) To dilate pupils for optical examinations, (5) Treatment of Parkinsonism, (6) To stimulate the heart for bradyarrhythmias, (7) To cause a bronchodilation effect in asthma and COPD, (8) To decrease gastrointestinal and genitourinary tract actions: (Diarrhea, Enuresis - involuntary urination, "Nervous Stomach" and "Spastic Colon", Overactive Bladder (OAB) and urinary incontinence)
Term
Anticholinergics cause both mydriasis and cycloplegia, what does this mean?
Definition
Mydriasis is dilation of the pupil,
Cycloplegia is paralysis of the ability for “accommodation” or focusing mechanism in the eye (also blurring of eye)
Term
“hot as a hare, blind as a bat, dry as a bone”...these side effects point to what type of drug usage?
Definition
anticholinergic drugs...Other adverse reactions include tachycardia, constipation, confusion, and urinary retention, which is especially important in older male patients.
Term
What are some of the Traditional Risk Factors for CVD?
Definition
Increasing age (male ≥ 45, female ≥ 55);
Having parents with heart disease (family history of premature cardiac heart disease: male < 55, female < 65);
Smoking and second-hand smoke;
HDL < 40 mg/dL;
High blood pressure - For every increase of 20/10 mmHg in blood pressure, there is a doubling in the risk of death from cardiovascular disease;
Lack of physical activity and/or being overweight;
Diabetes (insulin resistance)
Term
In a patient without renal insufficiency, what is the type of diuretic of choice?
Definition
Thiazide b/c it also has vasodilator action
Term
What is a normal range for C-reactive protein (indicative of inflammation)? And when this is high it is an indicator for what?
Definition
1-3 mg/L is normal...If this is high it indicates CVD
Term
C-reactive protein can be lowered by:
Definition
Diet, Exercise, Statins, Aspirin, Alcohol
Term
Hypertension is defined as an elevation of:
Definition
either the systolic blood pressure or the diastolic blood pressure or both
Term
The _____ pressure is the most important in people over age 50
Definition
Systolic
Term
Prehypertension:
Definition
120-139 &/0r 80-89
Term
Stage 1 hypertension:
Definition
140-159 &/or 90-99
Term
The mainstay of hypertension therapy is:
Definition
lifestyle interventions initiated prior to or in conjunction with pharmacologic therapy: smoking cessation, weight reduction, dietary sodium restriction to < 2.3 grams/day and low-saturated-fat diet, discontinuance (if appropriate) of caffeine and drugs that increase blood pressure: e.g., oral contraceptives, corticosteroids, sodium-containing antacids, NSAIDs, supplemental potassium, calcium and magnesium, regular aerobic activity
Term
What should be used in drug treatment for most patients with uncomplicated hypertension, either alone or combined with drugs from other classes?
Definition
Thiazide diuretics
Term
The ALLHAT Study showed what?
Definition
The study concluded that thiazide diuretics, specifically chlorthalidone, should be the initial drug of choice for the treatment of hypertension
Term
____ are no longer recommended for initial treatment of uncomplicated hypertension?
Definition
B-blockers
Term
Aim for a BP less than _____ for most patients and less than _____ for those with coronary artery disease, diabetes, or kidney disease.
Definition
140/90...130/80
Term
The ACCOMPLISH study found that:
Definition
It shows that some patients do better on an ACE inhibitor plus calcium channel blocker, than on an ACE inhibitor plus thiazide
Term
Thiazide-Type Diuretics are taken ____ daily, and preferably in the _____?
Definition
once daily...in the morning
Term
Side effects of thiazide treatment:
Definition
hypokalemia, their efficacy is diminished in patients with renal insufficiency, Use with caution in severe renal disease and severe hepatic disturbances
Term
A creatinine clearance of less than < 30 to 50 ml/min shows what? And in this case what kind of diuretic should you use if needed?
Definition
It shows impaired renal function, and in this case it would be better to use a loop diuretic
Term
Side Effects of Thiazides:
Definition
Hypokalemia,
Hyperuricemia (can precipitate gout),
Hyperglycemia,
Hyperlipidemia, and hypercholesterolemia
Term
Loop diuretics have basically the same side effects as thiazides plus the possibility of ______ from intravenous furosemide
Definition
ototoxicity
Term
Replacement of ____ is essential in patients taking either thiazide or loop diuretics. This is especially important in patients on Digoxin b/c _____ increases the potential for digoxin toxicity.
Definition
Potassium...hypokalemia
Term
Potassium Supplements are notoriously...?
Definition
irritating to the GI tract and also have a “bad” taste
Term
Spironolactone is an _____ receptor antagonist. Its side effects include:
Definition
aldosterone...Side effects: mastodynia, gynecomastia and menstrual abnormalities...It is also used for acne due to its anti-androgen (estrogenic) effects
Term
Name which drug is a Selective Aldosterone Receptor Antagonists (SARA)— for the treatment of high blood pressure?
Definition
Eplerenone (Inspra®)
Term
B-blocker agents reduce blood pressure not only by reducing adrenergic stimulation to the B-receptors, but also by...?
Definition
decreasing renin release from the kidney
Term
Patients who develop symptomatic bradycardia with other ß-blockers may want to switch to a B-blocker with what intrinic activity?
Definition
A B-blocker with intrinsic sympathomimetic activity (ISA), which does not cause a decrease in heart rate at rest
Term
B-blockers with ISA should not be used for...? (3)
Definition
angina pectoris, for cardiac protection during surgery, or after a MI
Term
Which B-blocker is better for diabetic patients since it doesn't increase blood glucose?
Definition
carvedilol (Coreg®)
Term
Taking a Central Alpha-Adrenergic Agonist causes what result?
Definition
Results in a peripheral drop in blood pressure
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