Pharmacology: Characteristiccs of Drug classes, Part 2
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Adrenergic bronchodilators and phosphodiesterase inhibitors may both be classified as _______.
Adrenergic bronchodilators treat asthma how? By what mechanism?
- By Increasing the intracellular levels of cAMP.
- By increasing production of cAMP
Phosphodiesterase inhibitors treat asthma how? By what mechanism?
- By increasing intracellular levels of cAMP
- By decreasing breakdown of cAMP
How are corticosteroids used in the treatment of asthma?
Decrease airway inflammation
_____ produce bronchodilation by decreasing intracellular levels of cGMP
How are leukotriene receptor antagonists and mast cell stabilizers used in the treatment of asthma?
They both decrease the release of substances that can contribute to bronchospasm
What classes of drugs fall under the category of antiasthmatics?
- Leukotriene receptor antagonists
- Mast Cell Stabilizers
- Phosphodiesterase inhibitors
- Adrenergic Bronchodilators
During what time frame should a rapid acting bronchodilator be administered in anticipation of exercise?
10-15 minutes before: no earlier than 60 minutes before.
An asthma patient is switching from oral to inhaled corticosteroids. What assessments are important for the Nurse to make?
- Asess for signs of adrenal insufficiency ( anorexia, nausea, weakness, fatigue, hypotension, hypoglycemia)
- Monitor for withdrawl symptoms from corticosteroids.
What are the general, primary uses of the anticoagulant class of drugs?
- Prevention and treatment of thromboembolic disorders including:
- Deep vein thrombosis
- Pulmonary Embolism
- Atrial fibrillation with embolization
True or False: Anticoagulants are used in the management of MI sequentially or in combination with thrombolytics and/or antiplatelet agents.
True or False: Anticoagulants dissolve clots
- Anticoagulants are used to prevent clot extension and formation.
- Thrombolytics dissolve clots
What are the two most commonly used anticoagulants? (route and drug name)
- Parentaral Heparins
- Oral Warfarin
In pharmacotherapy involving anticoagulants, therapy is often started with ______ because of its rapid onset of action, while maintenance therapy consists of ______.
- heparin or heparin-like agent
_____ are mostly used to prevent deep vein thrombosis after certain surgical situations in which there is an increased risk of thromboembolism.
What common post-surgical situation puts the patient at risk for thromboembolism and requires prophylactic treatment with the drug above?
Low doses of heparin or heparin-like compounds
_____, an anticoagulant, takes several days to produce therapeutic effects.
In serious or severe thromboembolytic events, what sort of therapy will proceed therapy with anticoagulants?
True or False: Anticoagulants are contraindicated in patients with active bleeding.
True or False: Hypertension is a common side effect of the anticoagulants.
A patient on anticoagulant therapy notices they have black, tarry stools. What should the nurse do?
Notify the health care provider; the patient may have internal bleeding.
____ are used in the treatment of various forms of endogenous depression, often in conjunction with psychotherapy.
Other than treatment of depression, what other uses might drugs in the antidepressant have? (what other conditions might they treat?)
- Anxiety, including OCD and GAD
- Chronic pain syndromes
- Smoking cessation
In general, what mechanism of action do antidepressant most likely have?
They prevent the reuptake of dopamine, norepinephrine, and/or serotonin by presynaptic neurons, resulting in accumulation of these neurotransmitters.
What are the two major antidepressants?
- TCAs (Tricyclic Antidepressants)
- SSRIs (Selective Serotonin Reuptake inhibitors
In regards to antidepressants: most _____ agents possess significant anticholinergic and sedative properties, which explains many of their side effects.
True or False: Systemic side effects may occur with both oral and topical use of antidepressants.
How many days should patients be off other antidepressants before they begin MAOI therapy? How many days must they be off MAOI therapy before they begin therapy with other antidepressants?
Some antidepressants may cause ____ side effects, such as dystonia, akathisia, and psuedoparkinsonism. How should these side effects be dealt with?
- Dose reduction or discontinuation of therapy may be necessary.
- Muscarinic blockers (anticholinergics) used to treat Parkinsonism may be used to deal with these side effects.
____ is used in the management of type 1 DM.
____ may be used in type 2 diabetes mellitus when diet and/or oral medications fail to adequately control blood sugar.
How does the healthcare provider go about choosing what sort of insulin to prescribe (rapid acting, intermediate acting, long acting)?
It depends on the degree of control desired, daily blood glucose fluctuations, and history of previous reactions.
Oral antidiabetics are used primarily in _____ DM, when diet therapy alone fails to control blood glucose or symptoms or when patients are not amenable to using insulin.
- Type 2
- May also be administered concurrently with insulin.
Describe how insulin acts to treat both type 1 and type 2 Diabetes Mellitus.
It lowers blood glucose by increasing the transport of glucose into cells and promotes the conversion of glucose to glycogen.
This hormone produced in the pancreas promotes the conversion of amino acids to proteins in muscle, stimulates triglyceride formation, and inhibits the release of free fatty acids.
In what situations would patients who are stabilized on a diabetic program require the administration of insulin?
- Exposure to stress
True or False: Mixed insulins should never be used in a pump or for IV infusion.
What insulins may be administered via IV?
insulin asparte or insulin glulisine
What should the nurse advise the DM patient to do if they become hypoglycemic?
Take a form of oral glucose, such as tablets or liquid gel glucose, rather than sugar, and notify health care provider.
What two tests should be performed often on DM patients during periods of stress or illness?
- Blood glucose
- Urine Ketones
What are the possible mechanisms by which antidiarrheals act?
- Slow intestinal motility and propulsion
- Alter the fluid content of the stool (reabsorb more water)
______ acts to decrease blood glucose levels while _____ acts to increase blood glucose levels. Both are secreted by what?
- The Pancreas
Name 3 drug classes that have a hyperglycemic affect on the blood.
Name 4 drugs that have a hypoglycemic effect on the blood.
- ACE inhibitors
- Beta Blockers
______ results from the autoimmune destruction of pancreatic beta cells, resulting in a lack of insulin secretion.
Type 1 Diabetes Mellitus
Type 1 diabetes mellitus is also referred to as _______ DM.
What are the typical signs and symptoms of type 1 DM (7)?
- Hyperglycemia-- fasting glucose > 126 mg/dL
- Glucosuria-- high levels of glucose in the urine
- Weight loss
Untreated diabetes mellitus can cause long term damage to the arteries, which can lead to what diseases?
- Heart disease
- Kidney Disease
Is insulin always, sometimes, or never used to treat type 1 DM?
In what case would a patient suffering from type 2 diabetes mellitus need insulin?
When they are unable to manage their blood glucose levels with diet, exercise, and oral antidiabetic agents.
Why is it important for nurses to know the time of peak action of any insulin?
That is when the risk for hypoglycemic adverse effects is the greatest.
When might hypoglycemia occur in the type 1 DM patient?
- When the insulin level peaks
- During Exercise
- When the patient receives too much insulin due to medication error
- If the patient skips a meal
How should patients who participate in competitive sports keep their blood glucose levels normal?
By consuming food or sports drinks just prior to or during the activity
_____ is the more common form of diabetes mellitus, accounting for 90-95% of people with the disorder.
Type 2 DM
What is the primary physiologic characteristic of type 2 Diabetes Mellitus?
Insulin Resistance: Target cells become unresponsive to insulin due to a defect in insulin receptor function.
True or False: In Type 2 Diabetes Mellitus, the pancrease does not produce enough insulin for the body to make use of the glucose in the blood stream.
False. In type 2 DM, the pancreas produces sufficient amounts of insulin, but the target cells do not recognize it because they have become insulin resistant.
True or False: Patients with poorly managed type 1 and type 2 DM both have the same complications, including retinopathy, neuropathy, and nephropathy.
What causes type 2 diabetes mellitus?
Lack of physical activity paired with obesity are associated with the development of Type 2 DM
Oral hypoglycemics are mainly used to treat _____. At what point in the disease process are they usually prescribed?
- Type 2 Diabetes Mellitus
- When diet and exercise have failed to reduce blood glucose to normal levels
At what point is insulin added to the regimen for a Type 2 diabetic?
- When there has been a failure to achieve glycemic control with two oral hypoglycemic agents
- Periodically, a third oral drug will be added at the same time as insulin
The oral hypoglycemic ______ acts by stimulating the release of insulin from pancreatic islet cells and by increasing the sensitivity of insulin receptors on target cells.
_____ are oral hypoglycemics that decrease the hepatic production of glucose (gluconeogenesis) and reduce insulin resistance (it does not promote insulin release from the pancreas).
The oral hypoglycemics ____ act by blocking enzymes in the small intestine that are responsible for breaking down complex carbohydrates into monosaccharides, thus delaying the digestion of glucose.
The ______ reduce blood glucose by decreasing insulin resistance and inhibiting hepatic gluconeogenesis. Hypoglycemia is not a side effect of this class, and they may take months to have an effect.
A class of hypoglycemics that act by stimulating the release of insulin from pancreatic cells in a manner similar to that of the sulfonylureas.
What are the six classes of drugs that fall under the category of oral hypoglycemics/ antidiabetics?
- Alpha-Glucosidase inhibitors
_____ are hormones that signal the pancreas to increase insulin secretion and the liver to stop producing glucagon. Several new oral hypoglycemics act by effecting this hormone.
Glucagon is released by the _____ and has what action?
Glycogen is produced by the ____ and performs what role?
Glucagon is released by the pancreas to increase blood glucose levels
Glycogen is produced by the liver and responds to glucagon: glucagon promotes the breakdown of glycogen, then increasing blood glucose.
____ is the stopping of blood flow, and is an essential mechanism that protects the body from both external and internal injury.
What are the basic steps in the process of blood clotting?
- Vessel spasms and constricts
- Platelets become sticky, adhereing to each other and to the damaged vessel-- aggragation is facilitated by ADP and thrombin
- Bound platelets break releasing substances that attract more platelets to the area.
When collagen is exposed a the site of injury, the damaged cells initiate a series of complex reactions called the ______.
___ occurs when fibrin threads create a meshwork that traps blood constituents so that they develop a clot.
Normal blood clotting occurs in about _____ minutes.
Finish filling in this flow chart about blood clotting:
Prothrombinase converts ______ to _______ -----> converts fibrinogen to ________, which provides a framework for the clot.
- prothrombin to thrombin
The process of clot removal is called _____. It is initiated within how long of clot formation? How long does it continue?
Finish filling in this flow chart about blood clot removal:
Fibrin clot is formed, nearby blood vessels secrete ______ ---> converts plasminogen to ______ -----> digests the fibrin strands to remove the clot
- Tissue Plasminogen Activator (TPA)
____ disorders occur when the body forms undesirable clots.
A thrombus in an arterial vessel often grows larger as more _____ is added, and are particularly problematic why? What can they cause?
- They deprive an area of adequate blood flow
- They can cause tissue ischemia ---> MI and many CVA
Pieces of thrombi may break off and travel through the blood stream to other vessels. A traveling clot is called a(n) ______.
Thrombi in the venous system usually form in the veins of the _____ in susceptible patients die to sluggish blood flow. What is this condition called?
Bleeding disorders are commonly characterized by abnormal clot formation. What is the is the most common nonhereditary bleeding disorder? What does it involve?
- A deficiency of platelets resulting form any condition that suppresses bone marrow function (immunosuppression, chemotherapy)
_____ are bleeding disorders caused by a genetic deficiency is specific clotting factors. They are typified by prolonged ____ which result in persistent bleeding that can be acute.
The classic form of Hemophilia, ______, accounts for 80% of cases of hemophilia and is caused by a lack of what clotting factor?
How is hemophilia treated?
By administering the absent clotting factor and, in acute situations, by transfusing fresh frozen plasma.
______ is the most common inherited bleeding disease.
von Willebrand's disease
How is von Willebrand's disease treated?
With factor VIII concentrate as well as desmopressin, which promores the release of stored vWF (von Willebrand Factor)
_____ work by either inhibiting specific clotting factors in the coagulation cascade or diminishing the clotting action of platelets.
____ are used to prevent the formation of clots, while _____ are used to dissolve clots that have already formed.
_____ promote the formation of clots by inhibiting the normal removal of fibrin, thus keeping the clot in place for a longer period. What are they commonly used for?
- To speed clot formation at a surgical site, thus limiting bleeding.
______ are used to prolong bleeding time, and thereby prevent blood clots from forming. Chemically speaking, how do they exert their effects?
- They impart a negative charge to the surface of the platelets which inhibits the clumping action or aggregation of these cells.
What is the traditional drug of choice for parenteral anticoagulation?
What is the mechanism of action of Heparin?
It enhances the actions of antithrombin III, a protein in plasma that inactivates thrombin and other procoagulant enzymes.
The heparin molecule has been shortened and modifed to create a newer class of drugs called ________. What is the mechanism of action of these drugs?
- Similiar to that of heparin except that their inhibition is more specific to active factor X (activates prothrombinase)
What are the advantages to using LMWHs (low molecular weight heparins)
- They posses the same degree of anticoagulant activity as Heparin but
- their duration of action is two to four times longer
- they produce a more stable response (requiring fewer follow-up labs)
- Caregivers can be trained in necessary SC injections at home
- Less likely than heparin to cause thrombocytopenia
What is the drug of choice for the prevention of DVT following surgery?
Low molecular weight heparins
What four drug classes encompass the parenteral anticoagulants?
- Low molecular weight heparin
- Direct Thrombin Inhibitors
- Antithrombin (in a class by itself)
_____ are parenteral anticoagulants that act on circulating thrombin as well as on thrombin that has already bound to a clot. They have limited therapeutic uses.
Direct Thrombin Inhibitors
__a__ is an unusual drug used as a parenteral anticoagulant that is obtained from genetically engineered goats that secrete human ____a____ in their milk.
___a___ is indicated for the prevention of peri-operative and peri-partum thromboembolytic events in hereditary __a___ deficient patients.
What is the most commonly prescribed oral anticoagulant?
Warfarin acts by inhibiting the hepatic synthesis of what coagulation factors?
Often, patients begin anticoagulation therapy with ____ and are switched to ____ when their condition stabilizes. Explain how the transition between these drugs is accomplished.
- warfarin (Coumadin)
When transitioning, these two drugs are administered concurrently for 2 to 3 days because warfarin takes several days to achieve optimum effect.
What is the most frequent and potentially serious adverse effect of all the anticoagulants? What patients should not take anticoagulants?
- Patients who have recently experienced a traumatic injury or surgery are especially at risk for bleeding associated with use of anticoagulants.
Pentoxifylline (Trental) is a _______. By what mechanism does it work?
- Oral anticoagulant
- Reduces the viscosity of red blood cells and increases their flexibility. It is given to increase microcirculation in patients with intermittent claudication (too little blood flow during exercise like walking).
_____ can cause an anticoagulant effect by interfereing with platelet aggregation. How do these differ from the anticoagulants?
- Antiplatelet drugs
- Anticoagulants are primarily used to prevent thrombosis in veins while antiplatelets are agents used to prevent clot formation in arteries.
____ prevent thrombosis in arteries while _____ prevent thrombosis in veins.
What four types of drugs are classified as antiplatelet drugs?
- ADP receptor blockers
- Glcyoprotein IIb/IIIa receptor antagonists
- Agents for intermittent claudification
Desrcibe Aspirin's antiplatelet activity.
It acs by binding irreversibly to the enzyme cyclooxygenase in platelets, inhibiting the formation of Thromboxane A2, a powerful inducer of platelet aggrevation.
What are the uses of Aspirin?
- Prevention of Stroke and MI (due to Antiplatelet activity)
_____ irreversibly alter the plasma membane of latelets, changing the binding of ADP to its receptor on platelets so that they are unable to recieve the chemical signals telling them to aggregate.
ADP receptor blockers
Endogenous __a__ is an enzyme necessary for platelet aggregation. ____a____ receptor agonists are the most effective antiplatelet agents, but also the most expensive and can only be given via IV.
These antiplatelets are the most effective and are used to prevent thrombi in patients experiencing a recent MI, stroke, or percutaneous transluminal coronary angioplasty (PTCA).
Glycoprotein IIb/IIIa receptor agonists
_____ is a condition caused by lack of sufficient blood flow to skeletal muscles in the lower limbs. This ischemia causes severe pain on walking, particularly in the calf muscles.
What do thrombolytics do?
digest and remove existing clots (induce fibrinolysis) by converting plasminogen to plasmin, which digests fibrin and breaks down fibrinogen, prothrombin, and other plasma proteins and clotting factors.
_____ promote fibrinolysis by converting plasminogen to plasmin.
These medications are administered for disorders in which an intravascular clot has already formed, such as in acute MI, pulmonary embolism, acute ischemic CVA, and deep vein thrombosis.
The therapeutic effects of thrombolytics are greatest when they are administered as soon as possible after clot formation occurs, preferably within _____ hours.
Do thrombolytics have a narrow or wide margin of safety? Explain.
They have a narrow margin of safety between dissolving "normal" and "abnormal"clots.
True or False: When a patient is receiving thrombolytic pharmacotherapy, vital signs must be monitored continuously and sign of bleeding should be recorded and the time noted.
- Vital signs must be monitored continuously, but signs of bleeding all for discontinuation of the therapy.
Hemostatics, also called ________ have what sort of affect on the body?
- They have an effect opposite to that of anticoagulants-- they shorten bleeding time.
What are patients who experience excessive bleeding after surgery treated with?
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