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99 Cards in this Set

  • Front
  • Back
Therapy for pain and ___ effects often go hand in hand.
anti-inflammatory
Nonsteroidal Anti-inflammatory drugs (NSAIDS) work by inhabitation of ___ synthesis
prostanoid
Prostanoids , such as prostaglandins, prostacyclins, and thromboxanes, are products of the metabolism of a fatty acid found in cell membranes, called ___ acid.
arachidonic
NSAIDS inhibit the first step in this metabolism, by inhibiting an enzyme called ___(COX).
cyclooxygenase
Thromboxanes (thromboxane A_2 or TXA_2) are found in the platelet and facilitate ___, which eventually leads to clot formation. Thromboxanes also cause vessels to ___.
platelet aggregation
constrict
Prostacyclins are found in the cells lining blood vessels (vascular endothelial cells) and ___ platelet aggregation. They also cause vasodilation.
inhibit
Prostanoids in the bronchioles of the lung have a protective function, and keep the airways open. They are ___.
bronchodilatory
Prostanoids in the cells liking the stomach are ___ – they protect the stomach lining from gastric acid.
cytoprotective
There are two isoenzymes of cyclooxygenase, Cox-1 and Cox2. Although both are anti-imflammatory, only ___ is responsible for platelet aggregation and the cytoprotective effect in the stomach.
COX-1
Different drugs have different selectivies for the two isoenzymes. Those that affect COX-1 will promote ulcers and have an antithrombotic (inhibitory action toward ___) action, and will prolong bleeding time.
platelets
___ – inhibitory action toward platelets
Antithrombotic
Narcotic analgesics act at the level of the ___ to relieve pain. These agents also act at sites in the central nervous system to reduce the perception of pain
spinal cord
Drugs that affect the cardiovascular system are the most frequently prescribed group of drugs. These drugs modify heart rate, blood pressure, and cardiac conduction, as well as work to increase perfusion to organs by increasing ___ flow
blood
Drugs that affect the autonomic nervous sytem (ANS) – these drugs are useful in the therapy of hypertension, hypotension, angina, and arrhythmias. Most of the drugs prescribed are inhibitors of the ___ portion of the ANS, either directly or indirectly.
sympathetic
Calcium channel blockers – these drugs have a variety of actions and are useful in the therapy of hypertension, angina, arrhythmias, and congestive heart failure. Depending on the class of calcium channel blocker, these drugs may increase cardiac ___ and or decrease the work of the heart.
output
___ inhibitors and angiotensin II receptor blockers – decrease levels or activity of the potent vasoconstrictor angiotensin II, and are useful in congestive heart failure and hypertension.
ACE
___ – dilate arteries and are useful in the therapy of hypertension, congestive heart failure (CHF), and angina.
Vasodialators
___ – dialate veins and increase nyocardial perfusion. They are useful in the therapy of angina.
Venodilators
___ agents – increase the strength of contraction of the heart muscle and are used in congestive heart failure (CHF)
Inotropic
___ – are agents that act at the level of the kidney to lower plasma (fluid) volume. They are useful in the therapy of hypertension, CHF, and angina.
Diuretics
___ – targeted to block the B_1 receptor, which functions to increase heart rate and force contraction of the heart muscle.
Beta receptor Antagonists (Beta Blockers)
By blocking the Beta receptor, heart rate and cardiac output are ___. This results in decreased blood pressure and increased tissue perfusion
Cardiac conduction rate is slowed, decreasing the possibility of arrhythmias.
The production of rennin is decreased, resulting in reduced production of the ___ angiotension II.
decreased
vasoconstrictor
___ - regulates one's (mean arterial) blood pressure
renin
Adverse effects of beta Blockers – the blockade of B_1 and B_2 receptors may interfere with the regulation of blood sugar (this is a ___ contraindication)
diabetic
The blockade of B_2 receptors may cause bronchoconstriction (___ contraindication)
asthmatic
Many adverse effects are caused by the blockade of ___ receptors so most drugs on the market are selective for the B_1 receptor. Unfortunately, none are completely without B_2 blockade. (i.e. very small amounts of B_2 blockade are present, which are considered negligible)
B_2
Beta Receptor Agonists – these drugs are useful in increasing the force of ___ of the heart, which raises blood pressure and cardiac output. These may be useful in cases of hypovolemia, severe hypotension, etc. These agents can also increase blood sugar.
contraction
Selective ___ receptor agonists are useful in the therapy of asthma.
B_2
___ – mechanism of action – blockade of Alpha_1 receptors results in a decrease in peripheral vasoconstriction, and lowering of blood pressure and cardiac afterload.
Alpha Receptor Antagonists
___ – a drop in blood pressure due to a change in body position when a person moves to a more vertical position.
Postural hypotension
___ – in emergency situations, these drugs are used intravenously in the therapy of shock. They are also used intravenously as decongestants.
Alpha receptor agonist
Adverse effects of Alpha_1 agonists are related to ___ in blood pressure.
increases
___ – these agents decrease the release of norepinephrine by binding to the regulatory Alpha_2 receptor on the sympathetic neuronal ending and nucleus tractus solitaries (NTS). Useful in the therapy of ___
Alpha_2 receptor agonists
hypertension
___ – these drugs act at the level of the muscarinic receptor to block parasympathetic effects
Muscarinic Antagonists
___ system – control smooth muscle contraction, regulate cardiac muscle, or stimulate or inhibit glandular secretion.
Parasympathetic
Calcium channel blockers block type “L” membrane channels for calcium, resulting in decreased calcium entry into the ___, in a dose-dependent manner.
cells
Vascular smooth muscle – calcium channel blockers can relax the smooth muscle of arteries and cause ___. They are therefore useful as antihypertensive and antianginal drugs.
vasodilation
Cardiac muscle – certain calcium channel blockers decrease conduction rate in cardiac tissue, resulting in a decrease in ___ and cardiac excitability. These drugs are thus useful as antiarrhythmics and antihypertensives, as well as the therapy of angina.
heart rate
Calcium channel blockers can also affect neuronal tissue in high therapeutic doses. Calcium is required for the release of ___, and calcium channel blockers can actually have sympatholytic effects.
neurotransmitter
PHYSIOLOGY REVIEW
Skeletal muscle obtains the calcium needed for contraction from intercellular stores, whereas cardiac muscle and smooth muscle obtain calcium from ___ the cell. Thus skeletal muscle is not effected by calcium channel blockers, while vascular and cardiac muscles are.
outside
The adverse effects of calcium channel blockers include flushing, ___, constipation, and nausea.
dizziness
___ - Inhibitors of Angiotension-Converting Enzyme
(ACE inhibitors)
___ is a potent vasoconstrictor that is produced through a cascade of events in the plasma.
Angiotensin II
___ – released from the kidney, acts on a blood protein, angiotensionogen, to form angiotension I, which is then acted upon by ACE to form angiotensin II. Ace also breaks down bradykinin, a potent vasodilatior. The net result is vasoconstriction and an ___ in blood pressure.
Renlin
increase
ACE inhibitors are competitive antagonists of ACE – they bind to angiotension I and complete with ACE for ___.
binding sites
ACE Inhibitors are useful in the therapy of hypertension, particularly in persons who are ___ and those with existing cardiac problems.
obese
___ have been shown to be less effective in populations of African descent, due to certain genetic differences.
ACE inhibitors
The inhibition of angiotension II formation results not only in less ___, but less release of aldosterone, as well. This results in less fluid and sodium retention.
vasoconstriction
ACE inhibitors may increase renal blood flow, so they are ___ in renal patients.
constraindicated
ACE inhibitors are constraindicated in pregnancy: when used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing ___.
fetus
ACE inhibitors generic names usually end in “___” or “___” so you can recognize them easily.
pril
prat
Angiotension II receptor Blockers - These agents are simply competitive antagonists of angiotension II at its ___.
receptor
Less adverse effects are seen with angiotension II receptor blockers than with ___, due to less bradykinin available, but the total blood-pressure-lowering effect is also less.
ACE inhibitors
Angiotension II receptor blockers reduce the ___(not levels) of angiotension II (e.g. vasoconstriction and increased secretion of aldosterone, a hormone that retains sodium and water from the renal tubules).
effects
___ – act at the level of arteriolar smooth muscle to relax it, resulting in dilation of the arteriole. Useful in the therapy of congestive heart failure, hypertension, and angina
Direct vasodilators
Venodilators (___) – act a the level of the vein to relax the venous smooth muscles and increase capacitance.
Nitrates
___ are not useful in the therapy of hypertension, as they do not significantly effect anteriolar smooth muscle.
Venodilators
Cardiac muscle is composed of contractile filaments made of actin and myosin, which overlap. The end (head) of the myosin molecule is an enzyme, which cleaves a phosphate group off the body’s energy source: ATP. This results in the release of energy and ___(cAMP), which regulates the contractile process.
cyclic AMP
In cardiac muscle, the contractile process starts with the binding of ___ to proteins surrounding the actin and ends with the degradation of cAMP by phosphodiesterase. By increasing the amount of calcium present or inhibiting phosphodiesterase (which allows the cAMP to stay around longer), we increase the number of active contractile filaments and increase the force of contraction.
calcium
___ agents increase the strength of contraction of cardiac muscle.
Inotropic
There are three classes of drugs presently used to increase contractile force.
The ___, which increase the amount of calcium available and thus increase the force of contraction.
The ___, which decrease the activity of phosphodiesterase and therefore increase levels of cAMP
The ___, which inhibit phosphodiesterase and increase levels of cAMP.
cardiac glycosides
bipyridines
methylxanthines
___ inhibit the actions of the cellular pump that pumps sodium out of the cell and potassium back in, after the action potential has occurred. This result is a bildup of sodium in the cell that can then exchange for calcium.
Cardiac glycosides
heart cells depend on calcium from the outside, the trapping of calcium in the cell and the additional pumping of calcium in from outside causes a large amount of calcium to be available for ___ and increases the number of contracting muscle fibers.
contraction
At the same time that sodium levels are building up within the cell and activating the sodium/calcium exchange, the potassium is building up outside of the cell. This can cause ___ in heart conduction.
abnormalities
___ levels are thus critical in a patient on cardiac glycosides and must be monitored closely.
Potassium
Phosphodiesterase inhibitors presently consist of two classes of drugs: the methylxanthines and bipyridines. These drugs increase levels of ___, resulting in longer and stronger contraction of cardiac muscle.
cAMP
___ – used as local anesthetics. They decrease excitation of conductive tissue. As agents used to block pain, they decrease the firing of pain neurons.
Sodium channel blockers
___ - Drugs used to decrease fluid volume
(Diuretics)
___ act on the nephron to increase retention of sodium in the urine, decrease the concentrating ability of the renal medulla, or increase the excretion of water and salt.
Diuretics
___ – act by disrupting the concentration mechanism in the kidney. As a result the urine is very dilute, which means that more water is iliminated. As water is eliminated, the plasma becomes more concentrated, drawing water out of tissues and decreasing edema.
Loop Diuretics
___ – act at the distal end of the nephron and impair the ability of the kidney to reabsorb chloride (and thus sodium) into the body.
Thiazide diuretics
___ – inhibit the conversion of carbon dioxide to carbonic acid, a process that utilizes water and brings it back into the body. The result is a slight loss of water and large loss of bicarbonate
Carbonic Anhydrase inhibitors
___ – these are very poor diuretics, They are used in combination with a potassium-wasting diuretic (e.g. thiazides)
Potassium-Sparing Diuretics
___– used intravenously, under supervised conditions. They are sugar polymers that bind to water and are filtered into the urine. As a result, they prevent the reabsorption of water and cause dieresis.
Osmotic Diuretics
___ – bind bile salts in the intestine. This prevents them from being absorbed and reused. Since bile salts are necessary for the digestion of fats, the body must then use cholesterol stores to make new bile salts. This lowers cholesterol stores (particularly LDL)
Bile Binding resins
___ - Drugs that interfere with triglyceride synthesis
(Fibrates)
The enzyme lipoprotein lipase breaks down VLDL. ___ increase the synthesis of this enzyme, resulting in decreased levels of VLDL.
Fibrates
Inhibitors of ___ – these drugs inhibit the first step in cholesterol biosynthesis
HMG CoA Reductase
___ – interfere with the clotting cascade
Anticoagulants
___ agents – interfere with platelet aggregation
Antithrombolytic
___ agents – break down an existing clot
Throbolytic
Anticoagulants interfere with various stages of the clotting cascade in blood plasma. They do not have a major effect on platelets. There are two main anticoagulant drugs, ___(which is used intravenously) and ___, which is taken orally.
heparin
warfarin
Heparin is a carbohydrate polymer that potentiates a natural anticoagulant called antithrombin III. This substance interferes with the formation of ___, which is required for clot formation.
thrombin
Because ___ is essentially a sugar, it would be digested if given orally.
heparin
Warfarin is an oral anticoagulant, that inhibits the recycling of ___
vitamin K
Since vitamin K is required for the action of several clotting factors that are necessary for the clotting cascade , and ___ effectively decreases liver stores of vitamin K, these clotting factors no longer function and clotting decreases in a dose-dependent manner.
warfarin
___ – these drugs interfere with the actions of the platelet plug and decrease platelet aggregation. This may result in a decrease in the number of small clots (thrombi) that routinely form in the course of normal blood flow, due to random platelet activation.
Antithrombotic agents
___ – break up formed clots. They act from within the clot to lyse (break up) the clot. The dangers of thrombolytic drugs lie in the formation of smaller clot pieces that can block small vessels and cause myocardial infarction or stroke. These are administered intravenously.
Thrombolytic drugs
The most common lung disorder treated pharmacologically is ___.
asthma
The objective in the treatment of asthma is to increase ___ diameter.
bronchiolar
___ – drugs that stimulate the Beta_2 receptor will cause bronchodilation, due to an increase in cyclic AMP. Those that block the receptor will inhibit this bronchodilation, and may cause ___.
Sympathetic agonists
bronchoconstriction
___ – since acetylcholine can cause bronchoconstriction, blocking receptors for acetycholine may cause bronchodilation.
Muscarinie antagonists
Methylxanthines – these are ___ inhibitors and raise the level of cAMP, resulting in dilation of bronchioles
phosphodiesterase
___ – these drugs will decrease the inflammatory response in the lung, which may be initiated by airborne pollutants, stress responses, or similar factors. These drugs decrease the inflammatory response by stabilizing mast cells, which secrete histamine, as well as stabilizing intracellular lysosomes, which release toxic substances.
Steroids and other anti-inflammatory drugs
___ – thise is the newest class of therapy for asthma. Leukotrienes are prostanoid derivatives that may be released in response to irritation, and which cause constriction of smooth muscle – in this case bronchiolar smooth muscle. By antagonizing these inflammatory agents, bronchioles remain dilated.
Leukotriene antagonists
Drugs that are useful in asthma are selective agonists at the ___ adrenergic receptor.
Beta_2
___ - These drugs are glucocorticoids. They decrease inflammation, resulting in decreased swelling of bronchiolar tissue and increased airway space.
Corticosteroids
Taken systematically, steroids cause inhibitory effects on the ___ gland and require gradual withdrawal in order to allow the ___ gland to resume normal functioning
adrenal
adrenal
Corticosteroids also inhibit the ___ system and may decrease production of certain hormones. These are metabolized in the liver and may affect liver function.
immune