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85 Cards in this Set

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What are the 7 tips for studying pharmacology?
1. Focus on classifications and prototypes
2. Compare newly encountered drugs with prototypes
3. Try to understand how the drug acts in the body (indications, side effects, contraindications)
4. Study major characteristics
5. Use your resources!
6. Write out drug info cards using your own words
7. Think about clinical application of the information
What are 6 general questions we should ask about medications we are administering?
1. What does the med do?
2 Why is the pt needing it?
3. What are the benefits?
4. What are the pt's primary problems?
5. What are the signs of the pt's issues that the medication is required?
6. Double check for ALLERGIES!!
What are the 6 areas of clinical info we need to know concerning medications?
1. Indication
2. Route (IV meds we need to know dilution, rate, and compatibility)
3. Adverse effects (side effects)
4. Contraindications (includes allergies)
5. Nursing considerations (implications) regarding administration info and assessment/monitoring
6. Action - what does the med do physically?
What is pharmacodynamics?
The study of Drug Action or the Mechanism of Action (which is mostly on receptors). These are three interchangeable names.
What is efficacy?
The ability of a drug to cause a desired effect or biological activity - drugs can't create a new function, they act on normal body chemicals.
What are the 4 considerations regarding receptors and medications?
1. Receptors bind with the natural body chemicals or drugs only if it is compatible with the receptor
2. Drugs bind with receptors on the cell surface or within the cell
3. Receptor specificity is the ability to bind only with compounds that have specific features
4. Receptor affinity is the strength with which the drug binds to the receptor
How is high affinity and low affinity clinically important in drugs?
High affinity drugs bind strongly with the receptors and can have affects even in low doses. Low affinity drugs are more likely to dissociate with the receptor or be bumped off by a high affinity drug.
What are the two major drug actions when attaching to receptors and any subcategories or actions?
A. They act like natural body chemicals to:
1. Open or close ion channels
2. Activate 2nd messengers within the cell
3. Stimulate usual cell function as an agonist
B. They block natural body chemicals by attaching to cell receptors so normal chemicals cannot attach - Antagonist
What action within the cell do water-soluble hormones produce within the cell?
The activate the 2nd messenger system
What is the general explanation of undesirable responses to drugs?
These are effects we don't want! Drugs have more than one action and attach to many receptors that have affinity for that drug, regardless of intended attachment to that receptor. This results in multiple actions that result in one of two actions - predictable and unpredictable responses.
What are 7 categories of predictable responses of drugs?
1. Side effects - unintended action, secondary effects
2. Adverse effects - undesirable side effect, may be harmful
3. Cumulative effects - the drug is not metabolized and excreted, so it accumulates in the body
4. Toxic effects - the drug dose increases in excess of the therapeutic range with adverse effects - can cause organ damage
5. Dependence - the drug is required or the person will feel physical symptoms of withdrawal - is predictable
6. Psychological dependence - the pt has a craving for the effects of the drug, but no physical dependence
7. Withdrawal - when the drug is no longer available and there is a physical dependence - Sx of withdrawal are usually the OPPOSITE from the drug effect
What are the 3 categories of unpredictable responses to drugs?
1. Drug allergy - can range from skin responses to anaphylaxis - drug needs to be d/c'd and not be given again. Prior to medicating, get a drug hx including sx related to perceived allergy
2. Idiosyncratic reaction - unpredictable, unintended rxn seen in the elderly and children that have no obvious cause
3. Iatrogenic reaction - condition caused by the drug therapy - ex. acne from the therapy
What are drug interactions?
A drug's effects on other drugs.
What are the 3 types of antagonistic effects of drug-drug interactions?
1. Drug #1 blocks the receptor drug #2 would use, causing drug #2 to have no action. Ex. Narcan (naloxone) for opioid overdose
2. Drug #1 can increase the metabolism of drug #2 - large amounts of alcohol makes microenzymes that metabolize narcotics and decrease sensitivity
3. Drug #1 can block absorption of drug #2 - ex. antacids increase stomach pH and some meds aren't absorbed - loss of therapeutic effects
What are 3 general categories of drug-drug interactions?
1. Antagonistic effects
2. Additive effects
3. Synergistic effects
What are additive effects of drug-drug interactions?
2 drugs that have different actions will have an additive effect when given together - gives a predictive therapeutic effect with extra effects and better effects - ex. diuretic and ACE inhibitor for HTN
What are synergistic effects of drug-drug interactions?
2 drugs given together create a greater-than-additive effect - one drug may have a minimal effect, but when combined with another, both will have greater effects
What are the 3 reasons for seeking a synergistic effect from 2 drugs?
1. It helps to displace a drug from protein binding sites to make it available
2. It can inhibit metabolic inactivation
3. It can create a decreased elimination of one of the meds
What are possible consequences of a synergistic drug-drug interaction?
It can result in unpredictable effects and make it so the therapeutic goal is not reached - ex. all CNS depressants when given with alcohol increase the depressant effect and can result in cessation of breathing and death
What are the drug effects of antacids, ASA, diuretics, and mineral oil on nutrients?
Antacids - increase gastric pH and chelates minerals so they are not available
ASA - damages gastric lining and inhibits brush border enzymes, like cyclooxygenase (COX), and decreases prostaglandin synthesis.
Diuretics - increase the excretion of nutrients
Mineral oil - inhibits the absorption of Vitamin D, K, and beta-carotene
What does chelate mean?
Any of a class of coordination or complex compounds consisting of a central metal atom attached to a large molecule, called a ligand, in a cyclic or ring structure.
What is cyclooxygenase (COX)?
An enzyme (EC 1.14.99.1) that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain. Non-steroidal anti-inflammatory drugs, such as aspirin and ibuprofen, exert their effects through inhibition of COX. The names "prostaglandin synthase (PHS)" and "prostaglandin endoperoxide synthetase (PES)" are still used to refer to COX.
What are prostaglandins?
They are mediators and have a variety of strong physiological effects, such as regulating the contraction and relaxation of smooth muscle tissue.[1] Prostaglandins are not hormones, but autocrine or paracrine, which are locally acting messenger molecules. They differ from hormones in that they are not produced at a discrete site but in many places throughout the human body. Also, their target cells are present in the immediate vicinity of the site of their excretion (of which there are many).
What are 2 effects food can have on drugs?
1. Drug absorption is reduced or delayed by food, so the drug is absorbed best if given on an empty stomach - ex. ASA, digoxin, ibuprofen, PCN G&K - although food may be recommended TO reduce the action and inhibit destruction of mucosa
2. Drug absorption is enhanced by food - ex. erythromycin, diazepam, and chlorothiazide
What is Pharmacokinetics?
The study of 1. How drugs enter the body 2. How drugs are distributed to the intended site of action 3. How drugs are metabolized 4. How drugs are eliminated from the body
What are the three routes of absorption of a drug?
1. Enteral route - PO - preferred route
2. Parenteral route - using a needle to perforate the skin - IV, IM, SC (SQ)
3. Topical - absorbed through the skin or mucus membranes of the mouth or rectum
What 3 things must be present in order to be able to give a drug PO?
1. Pt must be able to swallow without aspiration
2. Pt must not be vomiting or have a significant risk of vomiting
3. GI tract must be able to absorb the drug - the villi must be intact
What is dissolution?
The breakdown of a drug in body fluid so it is dissolved and can get into circulation.
What is bioavailability?
The proportion of a drug that is available for systemic effects after being dissolved in the body or with water, alcohol, or oil.
What does food do for bioavailability?
It decreases dissolution and absorption
What 4 things affect stomach acid and bioavailabilty?
1. Some drugs are not stable in acid and are destroyed
2. People have differing amounts of stomach acid - the very old and very young have less
3. Acid degrades the strength of drugs
4. With less acid, less drug is degraded and more is available, so a lower dose is needed
What makes ionic drug forms absorbable by cells?
The pH in the stomach changes the charged particle to uncharged so it can be absorbed.
Why can't some meds be given through the GI tract?
Some are destroyed by pancreatic enzymes.
What are the 4 forms of oral meds?
1. Liquids - ready for absorption
2. Capsules - almost as fast as liquids
3. Sustained release tablets - SR, XR, CR - absorbed over 8-12 hours as various coatings come off
4. Enteric coated - protects capsule/tablets from stomach acid and comes off in the duodenum where the pH is increased
Describe the 3 parenteral routes of drug administration?
1. SC - subcutaneous - small amount is injected just under the skin - absorbs slowly
2. IM - intramuscular - larger amount is given and has faster absorption due to an increased blood supply
3. IV - intravenous - There is NO ABSORPTION here as it is already in circulation - allows blood levels to stay high and therapeutic, however there is a risk for bacterial infections or damage to the veins - there must be no particles in the solute injected
What is chemical phlebitis?
Some drugs irritate the vein and a clot forms - the long-term result is hardening of the vein.
What creates the persistence of drugs in the blood?
Drugs are either free in the plasma and available for use, or are bound to proteins, mostly albumin, and are released as drug concentrations in the blood are lowered. The longer the drug will bind, the longer DURATION OF ACTION.
What are the 6 factors controlling the distribution of drugs in the body?
1. High lipid solubility and low protein binding readily diffuse across the cell membrane - ex. anesthetics
2. Water-soluble drugs pass along the cell membrane with difficulty
3. High drug concentrations favor diffusion into tissues
4. High binding proteins creates less free drug in the plasma and slows diffusion into the tissues
5. Non-specific binding - ex. many drugs bind to albumin
6. Competitive binding can cause a drug with lower affinity to be bumped off of albumin - ex. warfan has a weaker affinity and is bumped off by ASA, thus creating more availability of free warfan
What are the parts of the dose response curve?
Administration, absorption, time for absorption to reach minimal effective concentration (threshold), absorption during therapeutic range, peak, elimination through therapeutic range, elimination through time of termination of action.
What is half-life?
The time it takes for plasma levels of a drug to decrease to half the concentration.
What is the therapeutic index?
The ratio between desired effects and lethal dose - given as a ratio indicating how close the therapeutic dose and lethal dose are - ex. digoxin
What is a steady state concerning drug levels?
You administer a drug 4 times in order to reach the therapeutic range and get the trough at the therapeutic minimum; then administer the drug to keep levels in the therapeutic range - ex. antibiotics, they need high levels
What is a loading dose?
Administering a large dose when you can't wait for the concentration to get to a therapeutic range due to a long amount of time required - ex. some meds take 7-50 days to reach therapeutic levels - ex. digoxin, heparin.
What are the barriers to distribution?
1. Blood-brain barrier prevents water soluble drugs from passing into the CNS due to tight endothelial cells covered by fatty glial cells - lipid solubles can pass
2. Placental barrier - Some drugs can cross this barrier, so care is needed when selecting drugs
What is biotransformation?
The primary organ is the LIVER, although the kidney and bacteria in the colon help out. This is where drugs are made water soluble to be excreted by the kidney. The liver adjusts the synthesis of enzymes according to how much drug is needed - ex. excessive alcohol makes microenzymes that metabolize narcotics
Some drugs are also converted to active metabolites in the liver so they can be used.
Liver disease decreases this availability and drugs can accumulate to toxic levels.
What is the First Pass?
Drugs absorbed in the small intestine are absorbed into the blood and travel to the portal vein and into the liver where they are metabolized, which decreases the amount available.
What administration methods bypass the First Pass?
IV, IM, rectal, and SL because they go directly to the target organ and not through the liver first.
What is enterohepatic recycling?
Drugs released in bile move into feces but are reabsorbed in the intestine - this keeps drugs in the body more and levels can become toxic
Why is serum creatinine measured?
Creatinine builds up from muscle breakdown at a constant rate, so it is used to evaluate renal clearance. If GFR is low, that would mean passive glomerular diffusion and active secretion into the renal tubules is down and the drug may accumulate in the body.
What are special considerations concerning gastric issues and drug absorption with perinatal pharmacotherapeutics?
The mother will have slow gastric emptying and slow intestinal transit, which would increase the absorption of lipid soluble drugs and increase their effect.
How does N/V affect perinatal pharmacotherapeutics? What are the best ways to try to treat N/V when a mother is pregnant?
Treatment with antacids for N/V will increase gastric pH so weakly basic drugs have increased absorption - ex. opioids. It is best to eat small, frequent meals, don't eat and then lay down, avoid tight clothing, and avoid antacids if possible. Treat N/V with a few crackers before arising in the am and avoid spicy or gas forming foods. Try to avoid antiemetics - only take them if nutrition and fluid balance are compromised.
How does pregnancy affect the absorption of IM drugs? What happens with albumin during pregnancy?
They are absorbed more quickly due to increased tissue perfusion and vasodilation.
During pregnancy, there is decreased albumin, thus creating more free drug available.
How does pregnancy affect lipid soluble drugs? How does increased water weight affect drug action?
Increased body fat means increased storage of lipid soluble drugs, which could lead to toxicity.
Increased total body water decreases peak concentration, thus decreasing the available drug for action.
How does increased progesterone affect drug metabolism during pregnancy? What happens with GFR during pregnancy, and how does this affect drug concentrations?
Increased progesterone increases liver enzymes which increase drug metabolism. This causes liver clearance to increase and reduces half-life of the drug.
GFR is increased during pregnancy, which causes excretion of drugs to increase.
Does the placenta interfere with lipid soluble drugs crossing the barrier? What happens to the drugs?
Lipid soluble drugs easily cross the placental barrier and will accumulate in the fetus - ex. opioids cross the barrier and can cause respiratory depression when the baby is born.
Does the placenta interfere with water soluble drugs crossing the barrier? What happens with these drugs?
Water soluble drugs cross the placental barrier, but are excreted in the urine of the fetus. However, the urine goes into the amniotic fluid and the fetus swallows it creating continued exposure to the drug.
How does the mother having more total body water affect the fetus?
More total body water in the mother allows for more free drugs in circulation that are able to cross the placental barrier.
Does the fetal liver have any effect on drugs?
What happens with some drugs, such as tetracycline, concerning fetal tissues?
The fetal liver has some ability to inactivate drugs and at birth the neonate's liver has to clear what drugs were given to the mother.
Some drugs bind permanently to fetal tissue. An example is tetracycline binding to the teeth and permanently staining un-erupted teeth.
What is teratogenicity?
This refers to drugs that interfere with embryonic/fetal development. 15-60 days after conception the major organs are being formed and it is the most critical phase for malformation. After the first trimester, drugs don't affect fetal structure, but can have toxic effects.
How is lactated milk affected by some drugs and how should it be handled?
Some drugs can end up in breast milk, so if the drug can harm the infant, breast feeding should be stopped during the administration of the drug.
What are the consequences regarding sustained release drugs and breast feeding?
If a drug is given and the baby is breast feeding, how should this affect scheduling?
Sustained released drugs should be avoided as they can get into breast milk and are not easily eliminated by the baby.
Schedule the mother to get the medication after breast feeding in order to minimize the infant's exposure.
Regarding fat soluble drugs, what changes should be made in the infant's feeding schedule and why?
The infant should be given formula at mid day since this is the time when breast milk contains the most fat.
Always watch for infant drug reactions!
How are dosage calculations different in children?
Body weight varies a lot in children, so dosages are calculated based on body surface area (BSA).
How do dosages need to be changed in reference to the high water content in neonates?
Neonates are around 80% water, so dosages may need to be relatively higher for some drugs to reach therapeutic levels.
How is the newborn's GI system and liver different than others and what is the consequence?
How is pH different in a newborn and how does this effect drug absorption?
A newborn's GI system and liver are immature and have less enzymes. Therefore, the drugs have a longer half-life and it takes longer for them to be metabolized.
A newborn's pH is higher, so acidic drugs are not absorbed as well.
How is absorption via the skin different in newborns and why?
What response might babies and children have to medications?
The skin more readily absorbs drugs because it is immature and permeable.
Infants and children may have paradoxical responses to medications.
In regards to renal function, how is the structure and function different in neonates up to 6 months, and how does this affect drug excretion?
The neonate has decreased amounts of renal tubules, shorter tubules, and decreased tubular blood flow. This creates an increased risk of toxicity due to decreased excretion.
What happens to ICF in the elderly?
How are receptors affected in the elderly and how does this affect drug responsiveness?
ICF in the elderly decreases due to a fluid volume deficit.
Receptors decrease with aging, resulting in a decreased cellular responsiveness to drugs.
How are heart contractility and peripheral blood flow affected by aging and what is the result?
How are baroreceptors affected by age?
Myocardial contractility decreases around 1% each year. Peripheral blood flow is decreased in the older adult due to decreased elasticity of the arteries, which results in increased systolic and diastolic BP. Baroreceptors are less sensitive, so there is an increase in orthostatic hypotension.
How is GI motility, gastric pH, gag reflex, and esophageal emptying affected by aging? What are some consequences?
GI motility is decreased, gastric pH is increased (decreased absorption of Vitamins B1 and B12, calcium, and iron), gag reflex is decreased and esophageal emptying is slowed (leads to a higher risk of aspiration and pneumonia).
How are the liver and intestines affected as we age and what are the consequences?
Blood flow to the liver and intestines is decreased. This results in a reduction in microsomal enzymes in the liver. Peristalsis in the intestines is slowed and nutrient absorption is decreased.
How much is renal blood flow affected in the elderly and what is the result?
What happens to albumin levels?
By the age of 90, renal blood flow has decreased by 50%! This results in decreased tubular resorption, which results in a decreased ability to concentrate urine.
Albumin levels can drop in the elderly (or anyone), which leads to increased free drug - watch the lab work!
How is biotransformation, liver mass, muscle mass, GFR, and creatinine production affected by aging and what are the results?
Biotransformation decreases 50% between the ages of 60 and 100 as liver mass decreases. Muscle mass also decreases, GFR decreases, and creatinine production decreases. The serum creatinine concentration does not go up as GFR decreases, which means drugs stay in the body longer with increased side-effects.
What happens to CV compensatory mechanisms in the elderly and what are the consequences?
CV compensatory mechanisms are less effective in the elderly. Drugs designed to increase BP are more profound due to the vagal reflex that decreases the HR are less effecient.
What happens regarding K+ sparing diuretics and renal function in the elderly?
Renal function is decreased, which causes the effects of K+ sparing diuretics to become enhanced. This can result in hyperkalemia.
Why is hyperkalemia so dangerous?
K+ plays a large role in maintaining membrane potentials in muscles and electrical potentials in nerve cells. If it is altered, one main effect is a change in the heart's rhythm that can progress to cardiac arrest and death.
What happens to a neuromuscular blockade in the elderly?
How about autonomic adrenergic responses?
Neuromuscular blockade is increased in the elderly.
Autonomic adrenergic responses are decreased in the elderly, so beta blockers increase toxicity.
What is a neuromuscular blockade?
It is the administration of a paralytic agent which acts of the neuromuscular junction in order to create temporary paralysis for surgery or other medical needs - ex. anesthesia
What is the autonomic adrenergic response?
?
What happens with the neurotransmitters dopamine and acetylcholine in the elderly and what are the effects?
Dopa and ACH decrease in the elderly, therefore extrapyramidal (Parkinson-type effects) effects of neuroleptics and Reglan (increased peristalsis)
What kinds of responses can be seen in the elderly regarding sedatives/hypnotics/antianxiety drugs?
Paradoxical responses can happen with these drugs and the result can be restlessness, disorientation, confusion, and balance disturbances.
Poly pharmacy usually occurs as a result of multiple diseases. Then, side effects have to be treated, also. What three negative consequences (and sub information) result from poly pharmacy?
1. Increased risk of adverse drug effects
2. Drug interactions:
a. Take 2 drugs, there is a 5-6% chance of interactions
b. Take 5 drugs, there is a 50% chance of interactions
c. Take 8 drugs, there is a 100% chance of interactions!
3. Decreased compliance by pt due to low funds, confusion, etc.
What age and weight is the average dose based on?
What happens as body size/weight increases?
The average dose is based on a person (usually male) of 150 pounds and age 20-60.
As body weight/size increases, drug concentration decreases - dosages may need adjustment.
What is the termination of action regarding drugs?
No drug effects are seen, but the plasma may still contain the drug.
What is the trough level?
It is the lowest plasma concentration just prior to the next dose. Trough blood draws need to take place 5 minutes before the next administration of a drug.