Term
| What are the three MAIN properties of an ideal drug |
|
Definition
1. Effectiveness
2. Safety
3. Selectivity |
|
|
Term
| Name 6 additional properties that an ideal drug should have |
|
Definition
1. Reversible action
2. Predictability
3. Ease of administration
4. Freedom from drug interactions
5. Chemical stability
6. A simple generic name |
|
|
Term
| Why should a study be randomized? |
|
Definition
| To eliminate allocation bias |
|
|
Term
| What are the stages of drug development? What defines them? |
|
Definition
A. Preclinical testing - toxicities, pharmacokinetic properties, and potentially useful effects - Not on Humans
B. Clinical testing
1. Phase 1 - conducted with healthy volunteers unless side effects are too severe
Phase 2 & 3 - Tested in patients to determine therapeutic range, dosage range, safety, and effectiveness
Phase 4 - Post marketing surveillance |
|
|
Term
| What are some limitations to drug development and clinical trials? |
|
Definition
1. Data for women and children is limited
2. It's likely that new drugs will have undetected side-effects |
|
|
Term
| What are the three types of drug names? |
|
Definition
1. Chemical name
2. Generic name
3. Trade names |
|
|
Term
| Why is it better to use a generic drug name? |
|
Definition
| A drug generic named drug can have multiple trade names, and some OTC trade names can have different active ingredients. |
|
|
Term
| Who assigns non-proprietary names? Who assigns proprietary (trade) names? |
|
Definition
| The United States Adopted Names Council assigns nonproprietary names. The drug developer assigns trade names. |
|
|
Term
| What are the 4 pharmacokinetic processes? |
|
Definition
Absorption - Movement of a drug from administered site to blood
Distribution - Movement of drug throughout the body. Blood flow determines delivery rate
Metabolism - The enzymation alteration of drug structure (usually in liver)
Excretion - The removal of drugs from the body |
|
|
Term
| What are the barriers a drug molecule must pass through, and what organs does the drug usually reach? |
|
Definition
Cytoplasmic membrane is the major barrier. The three ways it can pass are:
1. channels and pores
2. transport systems
3. Direct penetration of the membrane itself (lipid only)
Kidneys and liver |
|
|
Term
|
Definition
| a Mixture of a drug plus binders and fillers, compressed together. The manufacturer can change the rate of disintegration and dissolution |
|
|
Term
| What is an enteric coated tablet? |
|
Definition
| Drugs that are covered with a material designed to dissolve in intestine but not the stomach. This protects the drug from acid and pepsin in the stomach and prevents gastric discomfort |
|
|
Term
| What is a sustained release tablet? |
|
Definition
| Capsules filled with tiny spheres that contain the drug. Each sphere has a coating that dissolves at variable rates. |
|
|
Term
| What is the first pass effect? How can it be avoided? |
|
Definition
| It is rapid hepatic inactivation of certain oral drugs, where one pass through the liver will inactivate the drug. Parenteral administration is avoids this. |
|
|
Term
| What is special about the blood brain barrier (BBB)? Which drugs can cross it? |
|
Definition
| Capillaries at the BBB have tight junctions, preventing drug passage. Drugs must be lipid soluble or utilize transport systems. |
|
|
Term
What is "protein-binding?"?
What happens to free drug levels when another highly protein bound drug is introduced? |
|
Definition
When a drug binds with a protein, albumin being the most common
One drug can displace albumin, increasing the free concentration of the displaced drug to increase. |
|
|
Term
What is a drug "half-life"?
How many half-lives does it take for a drug to reach plateau? |
|
Definition
Half life is the time required for the amount of drug in the body to decrease 50%
It takes 4 half-lives to reach plateau |
|
|
Term
What is therapeutic range?
What is toxicity?
What type of monitoring is done for a drug with low therapeutic index? |
|
Definition
Therapeutic range is the drug plasma level between minimum effectiveness and toxic concentration.
Toxicity is an adverse drug reaction from excessive dosing
Low therapeutic index doses are monitored more closely |
|
|
Term
What is a loading dose?
What is a maintenance dose? |
|
Definition
A loading dose is an initial large dose to rapidly plateau the drug in serum.
a maintenance dose is a smaller dose to maintain plateau |
|
|
Term
What is an agonist?
What is a partial agonist? |
|
Definition
Molecule that activates receptor
An agonist that only has moderate intrinsic activity. |
|
|
Term
|
Definition
| Molecule that prevent receptor activation |
|
|
Term
| Can a drug cause a cell to perform "a new function?" |
|
Definition
|
|
Term
Define therapeutic index
Is an index of 10 safer than 2? |
|
Definition
The ratio between the LD50 (lethal response dose for 50% of population) over the ED50 (dose required for response for 50% of population)
10 is a much safer index than 5 |
|
|
Term
What, when continually exposed, can desensitize a cell?
What, when continually exposed, can cause a cell to become super sensitive |
|
Definition
A cell can be desensitized by continual exposure to an agonist.
A cell can become super sensitive with antagonists by more receptor synthesis |
|
|
Term
What two drugs together cause an increased therapeutic effect?
What is that effect? |
|
Definition
Ampicillin and Sulbactam
kill more bacteria together |
|
|
Term
What two drugs together cause an increased adverse effect?
What is that effect? |
|
Definition
| Aspirin and warfarin decreases warfarin's anti-coagulant properties and increases bleeding risk |
|
|
Term
What two drugs together cause an reduced therapeutic effect?
What is that effect? |
|
Definition
| Propranolol blocks albuterol's ability to dilate the bronchi |
|
|
Term
What two drugs together cause a reduced adverse effect?
What is that effect? |
|
Definition
| Naloxone blocks dangerous respiratory depression from morphine |
|
|
Term
| What does it mean to have a "potentiative interaction" |
|
Definition
a potentiative interaction can intensify therapeutic effects or intensify adverse effects
An enhancement of the effect of one agent by another to create an effect greater than their parts. |
|
|
Term
What is an inducing agent?
What is an inhibiting agent? |
|
Definition
Inducing agents are promoting.
Inhibiting agents reduce. |
|
|
Term
| How does grapefruit juice affect drug levels? |
|
Definition
| Grapefruit juice inhibits an isozyme of p450 (CYP3a4) in the liver and intestinal wall. This inhibition decreases intestinal metabolism of many drugs, making them more available for absorption, increasing drug levels is blood |
|
|
Term
| When considering meals, when should and PO drug be given? |
|
Definition
| 1 hour before or 2 hours after |
|
|
Term
| Can some foods impact drug action? |
|
Definition
Yes.
Warfarin inhibits vit K clotting factors.
Over consumption of vitamin K will diminish warfarin's therapeutic effect |
|
|
Term
What is an adverse effect?
How does it compare to toxicity? |
|
Definition
Any noxious, unintending, and undesired effect at normal doses.
Toxicity is adverse drug reaction from excessive dosing. |
|
|
Term
|
Definition
| An uncommon drug response resulting frm a genetic predisposition |
|
|
Term
| Define iatrogenic disease |
|
Definition
| Disease originating from healthcare |
|
|
Term
|
Definition
| An immune response that is determined by degree of sensitization to the immune system, not from drug dosage. |
|
|
Term
|
Definition
| Decreased responsiveness to a drug from repeated drug dosages |
|
|
Term
|
Definition
| State where a long term exposure to drugs will result in an abstinence syndrome if drug is discontinued. |
|
|
Term
| Describe an unusually long reaction to anesthetic because of deficiency of succinylcholinesterase |
|
Definition
|
|
Term
| What reaction is a patient with urticaria, wheezing, and low blood pressure experiencing? |
|
Definition
|
|
Term
| Classify parkinson's syndrome symptoms caused by an antipsychotic medication |
|
Definition
|
|
Term
| What is abstinence syndrome? |
|
Definition
| Abrupt withdrawl from a drug that one has physical dependance |
|
|
Term
Is the placenta a barrier to drug distribution?
What kind of drugs cross the placenta? |
|
Definition
Placenta is essentially the same as a cell membrane. Clinically, it's considered that all drugs can reach the fetus.
Lipid soluble drugs will cross the placenta more readily that polar and ionized. |
|
|
Term
Are drugs in pregnancy well-studied?
Are drugs in lactation well studied? |
|
Definition
Drugs in pregnancy are not well studied in their effects on mother and fetus.
Drugs may be excreted in breast milk, and possibly passed to the infant. Many of these drugs are unknown, so a protocol to mitigate risk is in place |
|
|
Term
| Should all drugs be withheld during pregnancy? |
|
Definition
| No, leaving asthma and epilepsy untreated puts the mother's health in danger and could result in injury to the fetus as well. |
|
|
Term
| During which period are most teratogenic effects likely to occur? |
|
Definition
The most sensitive period is the embryotic period. First trimester. Fetal periods are less sensitive.
The two weeks after conception are not susceptible to teratogenesis |
|
|
Term
| Do drugs used at, or near term, affect the baby? How about Opiates? |
|
Definition
| Yes, all drugs during pregnancy affect the baby. Opiate addiction during pregnancy will pass it on to the neonate. |
|
|
Term
| What happens when narcotics are given to the mother just prior to delivery? |
|
Definition
| It can depress the respiratory rate of the newborn |
|
|
Term
| How does pregnancy affect drug absorption? |
|
Definition
| Absorption may increase because tone and mobility of bowels decrease, causing drugs to spend longer in the intestine. |
|
|
Term
| How does pregnancy affect drug distribution? |
|
Definition
| Distribution increases for some drugs because the plasma volume soubles |
|
|
Term
| How does pregnancy affect drug metabolism? |
|
Definition
| Drug metabolism is increased for some drugs like antiepileptics. |
|
|
Term
| What is the effect of absorption, distribution, and metabolism on kidney function during pregnancy? |
|
Definition
| Renal blood flow is doubled by the third trimester, resulting in a large increase in GFR. Drugs are eliminated at an accelerated rate. |
|
|
Term
| What happens to plasma volume during pregnancy? |
|
Definition
|
|
Term
| What advice would be recommended for a nursing mother. |
|
Definition
| Take drugs immediately after breast feeding, choose drugs with a short half life, choose drugs that tend to be excluded from milk, and avoid drugs that are known to be hazardous |
|
|
Term
| Why are children so sensitive to drug effects? |
|
Definition
| Kidneys and liver are immature and the blood brain barrier isn't completely formed. All five pharmacokinetic processes are immature. |
|
|
Term
| Why are children sensitive to drug effects? (kidneys, liver, blood brain barrier) |
|
Definition
The kidneys are immature and the blood brain barrier isn't completely formed.
All five pharmacokinetic processes are immature. |
|
|
Term
| What are the four pharmacokinetic processes? |
|
Definition
1. Drug absorption
2. Drug distribution
3. Drug metabolism
4. Drug excretion |
|
|
Term
| What is pharmacodynamics? |
|
Definition
| The nature and intensity of the response once the drug has reached the site of action. |
|
|
Term
| How is drug ABSORPTION different in newborns (first 30 days of life) and infants (first year of life)? |
|
Definition
PO administration is unpredictable beause of delayed gastric emptying due to a higher pH in the stomach.
IM is slow and erratic for the first few days of life
subQ can increase toxicity because of thin skin |
|
|
Term
| How is drug DISTRIBUTION different in newborns (first 30 days of life) and infants (first year of life)? |
|
Definition
Protein binding is affected as albumin concentration is low and other substances compete to bind it.
Blood brain barrier is immature, causing drugs to reach the brain in higher doses than adults |
|
|
Term
| How is drug METABOLISM different in newborns (first 30 days of life) and infants (first year of life)? |
|
Definition
| Metabolism is affected by a low hepatic metabolism, becoming normal at the 1 YOA. |
|
|
Term
| How is drug EXCRETION different in newborns (first 30 days of life) and infants (first year of life)? |
|
Definition
| Excretion is low due to low poorly developed kidneys until the 1 YOA |
|
|
Term
| What are considerations with topical drugs in infants compared to older children and adults? |
|
Definition
| Infant's skin is thinner, greater risk for toxicity |
|
|
Term
How is gastric pH different between a 1 year old and a 4 year old?
Does it affect drug absorption? |
|
Definition
| Gastric pH is much higher in a one year old vs a four year old. Drug absorption via PO will be altered due to delayed gastric emptying |
|
|
Term
| When does the kidney function of a child mature to adult level? |
|
Definition
|
|
Term
| How are albumin levels different in newborns/infants compared to older children? |
|
Definition
Albumin levels are lower in newborns and infants than older children.
Drug dosages must account for lower albumin binding |
|
|
Term
| What can aspirin cause in children? |
|
Definition
| Severe intoxication from overdose. Reye's syndrome if they have chickenpox |
|
|
Term
| What can glucocorticoids (i.e. prednisone) cause in children? |
|
Definition
| High glucocorticoid doses can cause growth supression |
|
|
Term
| What can sulfonamide antibiotics cause in children? |
|
Definition
| A buildup of bilirubin levels that causes Kenicterus |
|
|
Term
| How do you most accurately determine dose for a pediatric patient? how accurate is this? |
|
Definition
| Body surface forumla. Initial dose is at best an approximation. |
|
|
Term
| How is drug ABSORPTION different in elderly patients? |
|
Definition
| Total absorption does not change. Rate of absorption may be slower due to delayed gastric emptying and reduced splanchnic blood flow |
|
|
Term
| How is drug DISTRIBUTION different in elderly patients? |
|
Definition
An increased % body fat makes a storage depot for lipid soluble drugs
A decrease in total body water results in water soluble drugs being more concentrated
Reduced serum albumin |
|
|
Term
| How is drug METABOLISM different in elderly patients? |
|
Definition
Hepatic metabolism decreases with age.
Half life of some drugs may increase
First pass may be diminished |
|
|
Term
| How is drug EXCRETION different in elderly patients? |
|
Definition
Renal function decreases
Drug acculturation is secondary to reduced renal excretion and is the most important cause of adverse drug effects in elderly.
Creatine clearance is ideal to measure elderly kidney function |
|
|
Term
| Is absorption changed in the elderly? |
|
Definition
| The rate of absorption becomes slower. |
|
|
Term
| Which organ almost universally declines in function in the elderly? |
|
Definition
|
|
Term
| Why is creatinine clearance used to measure kidney function in the elderly? |
|
Definition
| Lean muscle mass declines in parallel with kidney function. |
|
|
Term
| What happens to body composition as a patient becomes elderly? |
|
Definition
| Increased body fat % and decrease lean muscle mass |
|
|
Term
| Are serum albumin levels higher or lower in the elderly? |
|
Definition
| Serum albumin is lower in the elderly. |
|
|
Term
| What happens to plasma volume in the elderly? |
|
Definition
| Total body water decreases, resulting in decreased plasma volume |
|
|
Term
| What considerations are there for administering morphine PO to an elderly pt? |
|
Definition
Reduced liver mass, reduced hepatic blood flow, and decreased hepatic enzymes will reduce the effect of first pass.
A lower dose should be considered |
|
|
Term
| Why are adverse drug reactions and drug-drug reactions much more common in the elderly? |
|
Definition
Adverse reactions are 7x more likely.
Drug accumulation secondary to renal failure, poly pharmacy, greater use of drugs with low therapeutic index, inadequate supervision, poor pt adherence.
The blood brain barrier becomes leaky in the elderly. |
|
|
Term
| What should the interval and dose be like in the elderly, compared to normal adults. |
|
Definition
| Doses should be lower, the intervals longer. |
|
|
Term
What receptor(s) are on the HEART?
What do they do? |
|
Definition
β1
- increased heart rate
- increased contractile force
- increased electrical conduction
- decreased delay of AV node
ONE BIG heart! |
|
|
Term
What receptor(s)are on the LUNGS?
What do they do? |
|
Definition
β2 - Bronchi Dilation
Muscarinic - Bronchi Constriction |
|
|
Term
What receptor(s)are on the KIDNEYS?
What do they do? |
|
Definition
Dopamine - Increases renal blood flow
β1 - Activates RAAs cycle |
|
|
Term
What receptor(s)are on LIVER and SKELETAL MUSCLE?
What do they do? |
|
Definition
| β2 - Upregulates gluconeogenesis |
|
|
Term
What receptor(s)are on the EYES?
What receptor(s) are on the LENS OF THE EYE?
What do they do? |
|
Definition
Eye
α1 - dilates pupils
Muscarinic - constricts pupils
Lens
α and βs - Far field vision
Musarinic - short field vision |
|
|
Term
What receptor(s)are on the SALIVARY GLANDS?
What do they do? |
|
Definition
| Muscarinic - if blocked causes dry mouth |
|
|
Term
| What receptor(s)are on the BLADDER? What do they do? |
|
Definition
α1 - cause bladder sphincter contraction
muscarinic - if activated, voiding occurs |
|
|
Term
Of the following: α1, β1, β2, muscarinic, and dopamine;
are they in the sympathetic or parasympathetic branch? |
|
Definition
α1 - Sympathetic
β1 - Sympathetic
β2 - Sympathetic branch
dopamine - sympathetic branch
muscarinic - Parasympathetic |
|
|
Term
Of the following: α1, β1, β2, and dopamine;
What transmitters bind to these? |
|
Definition
Epinephrine activates all α's and β's
Norepinephrine activates all α's and β1
Dopamine activates α1, β1, and dopamine receptors |
|
|
Term
| What transmitter binds to muscarinic receptors? |
|
Definition
|
|
Term
| Define a sympathomimetic drug |
|
Definition
| A drug that mimics the effect of the sympathetic nervous system |
|
|
Term
| Define a parasympathomimetic drug |
|
Definition
| A drug that mimics the effects of the parasympathetic nervous system |
|
|
Term
What are baroreceptors responsible for?
Where are they located? |
|
Definition
They regulate the blood pressure
They are located in the carotid sinus and aortic arch |
|
|
Term
For Bethanechol, What is it's:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects
5) Important drug interactions |
|
Definition
1) Mechanism - Direct-acting muscarinic agonist. The drug reversibly binds to receptor
2) Urinary retention, gastrointestinal uses
3) Increased U/O
4) Cardivascular system, alimentary system, urinary tract, exacerbation of asthma, dysrhythmias in hyperthyroid pt
5) N/A |
|
|
Term
For Atrophine, What is it's:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects
5) Important drug interactions |
|
Definition
1) Muscarinic antagonist that blocks muscarinic receptors, preventing activation
2) Used for preanesthetic medication, eye disorders, bradycardia, intestinal hypertonicity and hypermotility, muscarinic agonist poisoning, peptic ulcer disease, asthma, biliary colic.
3) Xerostomia (dry mouth), blurred vision and photophobia, elevation of intraocular pressure, urinary retention, constipation, anhidrosis, tachycardia, asthma
4) Reduced muscarinic activation
5) Avoid atropine with other drugs capable of causing muscarinic blockade |
|
|
Term
|
Definition
A muscarinic agonist
Used to treat glaucoma by increasing outflow of aqueous humor |
|
|
Term
| What are symptoms of muscarinic toxicity |
|
Definition
| Profuse saliva production, lacrimation, visual disturbances, bronchospasm, diarrhea, bradycardia, and hypotension |
|
|
Term
| What agent would relieve the symptoms of muscarinic toxicity |
|
Definition
| Atropine, a muscarinic antagonist |
|
|
Term
| Why are anticholinergic drugs effective in treating urge incontinence and OAB? |
|
Definition
| They prevent breakdown of acetycholine (which activates muscarinic receptors) |
|
|
Term
| What does anticholinergic poisoning look like? |
|
Definition
| Can't see, Can't spit, Can't pee, Can't shit. |
|
|
Term
What drug treats anticholinergic poisoning?
What is its mechanism? |
|
Definition
Physostigmine
Inhibits actylcholinesterase, preventing the breakdown of actylcholine. |
|
|
Term
For the catecholamine Epinephrine, What is it's:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects
5) Important drug interactions |
|
Definition
1)αs and βs
2) Delay absorption of local anesthetics, control superficial bleeding, elevate blood pressure, bronchodilation in allergic reaction, mydriasis,
3)vasoconstriction, bronchodilation
4)HTN, dysrhytmias, angina pectoris, necrosis following extravasation, hyperglycemia in diabetics
5) MAO inhibitors, Tricyclic antidepressants, α and β blockers, general anesthetics |
|
|
Term
For the catecholamine Norepinephrine, What is it's:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects
5) Important drug interactions |
|
Definition
1) αs and β1 agonist
2) Hypotensive states and cardiac arrest
3) Same as all epi, except β2 mediated
4) Tachydysrhytmias, angina, HTN, local necrosis on extravasation
5) MAO inhibitors, tricyclic antidepressants, general anesthetics, and α and β blockers
DOES NOT CAUSE HYPERGLYCEMIA in diabetics |
|
|
Term
For the catecholamine Isoproterenol, What is it's:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects
5) Important drug interactions |
|
Definition
1) β1 and β2 agonist
2) Cardiovascular disorders, Asthma (no longer used, β2 only is better), Bronchospasms
3)
4) Tachydysrhytmia, angina pectoralis, hyperglycemia in diabetics
5) MAO inhibitors, Tricyclic antidepressants, α and β blockers, general anesthetics |
|
|
Term
For the catecholamine Dopamine, What is it's:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects
5) Important drug interactions |
|
Definition
1) Dopamine, β1, and α1 at high doses agonist
2) Shock, Heart failure, acute renal failure
3) increased cardiac output, Increased renal bloodflow and u/o
4) Tachycardia, dysrhytmia, and anginal pain
5) MAO inhibitors, Tricyclic antidepressants, general anesthetics |
|
|
Term
What receptors are resposible for Epinephrine, Norepinephrine, Isoproterenol, and Dopamine actions:
1) BP
2) HR
3) Contractile force (positive inotropic effect) |
|
Definition
1) α1 caused vasoconstriction, increasing BP
2) β1 increases HR
3) β1 increases contractile force |
|
|
Term
| What do Epinephrine, Norepinephrine, Isoproterenol, and Dopamine do to the bronchi? |
|
Definition
| All that activate β2 receptors cause bronchodilation; Epinephrine and Isoproterenol |
|
|
Term
| Which of Epinephrine, Norepinephrine, Isoproterenol, and Dopamine increase U/O? |
|
Definition
| Dopamine receptor activation increases u/o |
|
|
Term
What are symptoms of anaphylactic shock?
How long does epinephrine's effects last when administered to one with anaphylaxis? |
|
Definition
Hypotension, bronchoconstriction, and edema the glottis.
Effects of epinephrine last 10-20 minutes |
|
|
Term
How are catecholamines metabolized?
Can catecholamines be administered orally? |
|
Definition
They are metabolized by MAO (monoamine oxidase) and COMT (Catechol-O-methyl transferase), enzymes found in the liver/intestinal walls
Orally, catecholamines are broken down before they can reach systemic circulation |
|
|
Term
| If a solution of catecholamines is discolored brown, what does it mean? |
|
Definition
| Oxidation has occurred and it should be discolored. Dobutamine is the exception, but must be used within 24 hrs of the appearance of discoloration. |
|
|
Term
| What does dose-dependant effects with dopamine and albuterol mean? |
|
Definition
Different doses, different receptors can be activated.
Dopamine:
low dose, only dopamine receptors
medium dose, dopamine and α1
High dose, dopamine, α1, and β1
Albuterol:
When dose is increased, it loses β2 specificity and activates β1 as well |
|
|
Term
| What does concerning about edema at an IV site when administering catecholamines? |
|
Definition
| The IV is leaking into the surrounding tissue. The catecholamines won't break down in the skin and can cause extravasation and local necrosis. |
|
|
Term
| Are non-catecholamines metabolized by MAO and COMT? |
|
Definition
| They are not readily metabolized by MAO and COMT |
|
|
Term
| Do catecholamines or non-catecholamines cross the BBB more readily? |
|
Definition
| Non-catecholamines are less polar, allowing them to cross the BBB easier than catecholamines |
|
|
Term
| What is the typical use for the non-catecholamine ephedrine? |
|
Definition
Ephedrine, a mixed drug, improves hemodynamic status of patients in shock.
phenylephrine |
|
|
Term
| What is the typical use for the non-catecholamine phenylephrine? |
|
Definition
| phenylephrine, common in cold medications, is used as a nasal decongestant |
|
|
Term
| What is the typical use for the non-catecholamine Terbutaline? |
|
Definition
| Asthma treatment via β2 bronchodilation |
|
|
Term
What is albuterol used for?
How does it work?
What are its side effects?
Dose dependancy? |
|
Definition
Albuterol treats asthma
Activates β2 receptors to cause bronchodilation
minimal side effects at small doses, tremors and tachycardia rare
At high doses, albuterol activates β1 as well |
|
|
Term
What is prazosin (minipress)?
What does it do?
What is it used for? |
|
Definition
A α blocker, competitive antagonist.
Causes dilation of the arterioles and veins and relaxation of bladder neck.
Approved for HTN only. |
|
|
Term
What is phentolamine?
What is it used for? |
|
Definition
A α blocker competitive antagonist
Pheochromocytoma (tumor of adrenal gland tissue), prevention of necrosis following extravasation, reversal of soft tissue anesthesia |
|
|
Term
| After administration of prazosin (minipress) or phentolamine, why should pt be cautious standing up? |
|
Definition
| Orthostatic hypotension is an adverse effect of α blocking. |
|
|
Term
| After administration of prazosin (minipress) or phentolamine, how is male sexual function affected? |
|
Definition
| α blocking can inhibit ejaculation. |
|
|
Term
For general betablockers, define:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects |
|
Definition
1) β antagonist
2) Angina pectoris, HTN, cardiac dysrhytmias, MI, heart failure, hyperthyroidism, migraine, stage fright, pheochromocytoma, glaucoma
3) Reduced HR, reduced force of contraction, Reduced velocity of AV impulse conduction
4)β1 - Bradycardia, Reduced cardiac output, precipitation of heart failure, AV heart block, rebound cardiac excitation
β2 - Bronchoconstriction, glycogenolysis inhibition |
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Term
| For Propranolol, define: 1) Mechanism 2) Medical indication 3) Expected Response 4) Adverse Effects 5) Drug interactions |
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Definition
1) β1 and β2 blocker
2) Angina pectoris, HTN, cardiac dysrhytmias, MI, heart failure, hyperthyroidism, migraine, stage fright, pheochromocytoma, glaucoma
3) β1 - reduces HR, reduces heart contraction force, AV impulse suppression, Can block RAAs from kidneys
β2 - Bronchoconstriction, vasoconstriction, and reduced glycogenolysis
4) β1 - Bradycardia, AV heart block, heart failure, rebound cardiac excitation β2 - Bronchoconstriction, inhibition of glycogenolysis, CNS effects, HTN effects
5) Do not use with Ca++ channel blockers. Do not use with insulin, Obscures insulin induced hypoglycemia symptoms |
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Term
For Metoprolol, define:
1) Mechanism
2) Medical indication
3) Expected Response
4) Adverse Effects
5) Drug interactions |
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Definition
1) β1 blocker
2) HTN, but can be used for angina pectoralis, heart failure, MI. Useful with a pt with asthma/COPD
3) β1 - reduces HR, reduces heart contraction force, AV impulse suppression, Can block RAAs from kidneys
4) Bradycardia, reduced C/O, AV heart block, rebound cardiac excitation following abrupt withdrawl
5) Do not use with Ca++ channel blockers. Do not use with insulin, Obscures insulin induced hypoglycemia symptoms |
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Term
| Why is heart disease a consideration with beta blockers? |
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Definition
The adverse effects could be fatal.
They prevent the heart from excessive sympathetic stimulation and protect against dysrhythmias. They can make heart block worse. |
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Term
| What are some cautions when giving a diabetic beta blockers? |
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Definition
β2 blocking can inhibit glycogenolysis, eliminating a corrective measure for hypoglycemia.
They can also mask tachycardia associated with hypertension |
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Term
| Should beta blockers be tapered? |
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Definition
If they are not tapered, rebound excitation can occur, increasing cardiac activity.
This can cause anginal pain or ventricular dysrhythmias. |
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