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111 Cards in this Set
- Front
- Back
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four sources of drugs
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plants, animals, minerals, and synthetic/semi-sythetic
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Pure Food and Drug Act- 1906
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*Passed to protect the public from adulterated or mislabeled drugs
*Drug company required to list if 1 of 11 dangerous and perhaps addicting drugs *false and misleading claims are not allowed on the package *only drugs sold in interstate commerce were covered |
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Food and Drug Act of 1909
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*designated the United States Pharmacopedia and the National Formulary as official standards
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Food Drug Cosmetic Act of 1938
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*drug manufactures must test for harmful effects and drug labels must be accurate and complete
*durham-humphrey ammendment- specified how drugs can b ordered and dispended *Kefauver-Harris Ammendment- require proof of safety and efficacy prior to approval and permitted generic versions of drugs initially marketed 1938-1962 |
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Generic Drug Criteria
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*Pharmaceutical Equivelence
*Bioequivalence |
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Pharmaceutical Equivalence
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same active ingredients, dosage form, strength, and route
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Bioequivalence
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rate and extent of absorption are not significantly different than pioneer
*AUC, Cmax, Tmax |
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controlled substances:
Schedule 1 |
high abuse potential
no accepted medical use research protocol only may lead to severe dependence Ex: herion, LSD |
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Controlled Substances:
Schedule 2 |
high abuse potential
accepted medical uses may lead to severe dependence written prescription, no refills Ex: opium, morphine, cocaine |
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Controlled Substances;
Schedule 3 |
less abuse potential than 1 &2
accepted medical uses low/moderate physical dependence, high psychological dependence written or oral prescription, up to 6 months of refills Ex: acetaminophen with codeine paregoric anabolic steroids |
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Controlled Substances:
Schedule 4 |
lower abuse potential than 3
accepted medical uses limited dependence writen or oral prescription, 6 months of refills Ex:phenobarbital diazepam chloral hydrate |
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Controlled Substances:
Schedule 5 |
lower abuse potential than 4
accepted medical uses limited dependence may or may not require a prescription terpin hydrate with codeine codeine in limited quantities |
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FDA Approval process
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1.Investigational new drug
2.New Drug application 3.Abbreviated New Drug Application |
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Molecular Targets of Drugs
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receptors, enzymes, carrier molecules, ion channels
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Receptor Binding- Agonism
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production of a molecular/cellular response to an interaction between a drug and a receptor that activates the receptor
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Receptor Binding- Competitive Antagonism
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agonsit and antagonist both trying to bind to the same receptor
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Receptor Binding- Non competitive Antagonism
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binding of antagonist to one receptor prevents agonist from binding to/activating another receptor
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Pharmocologic antagonism vs. Effect antagonism
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Effect Antagonism
If you have 2 different drugs: one reacts with blood vessels to cause BP to drop and the 2nd reacts with receptors on the heart to cause BP to go up |
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Pharmaceutical phase
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disnintegration and dissolution: in order for something to enter your body, it has to cross a biological membrane
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Phamacokinetic phase
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absorption- movement of drug molecules in the body
rate of absorption can determine the onset of action, duration of action, intensity of response |
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Subcutaneous
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inject into space under skin with small needle
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Intramuscular
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deep into muscle
DEPO injection- slow absorption |
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Intravenous
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directly into the vein- most common
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Intrathecal
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into the spine- spinal chord
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Epidural
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Close to spinal chord
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Hepatic biotransformation
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inactivation or removal from body
drug is changed into something else and peed out |
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Object Drug
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the drug whose action or kinetics is altered by a druf interaction
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Precipitant Drug
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the druf which causes the change to occur
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Pharmacokinetic drug interaction
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those in which one drug alters the rate or extent of absorption, distribution, metabolism or excretion of another drug
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Pharmacodynamic drug interaction
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those in which onee drug induces a change in a patient's response to a drug without altering the object drug's kinetics
-pharmacological interactions |
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Pharmaceutical drug interactions
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includes physical and chemical incompatibilities
-falling out of solution |
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Characteristics of important object drugs
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-narrow therapeutic range
-are metabolized by hepatic mixed function oxidases -are used chronically |
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Variables that affect absorption
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-nature of absorbing surface
-blood flow to site of administration -solubility of the drug -dosage form |
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Absorption of Dosage Forms
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-liquids, elixirs, syrups
-suspensions -powders -capsules -tablets -coated tablets -enteric coated tablets -substained release |
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pharmacokinetic drug interaction
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those which one drug alters the rate or extent of absorption, distribution, metabolism or excretion of another drug
-one drug causes a change in the plasma concentrations of another drug ex: draw blood and see how much drug is in it |
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Pharmacodynamic drug interactions
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those in which one drug induces a change in a patient's response to a drug without altering the object drug's kinetics
-pharmocological interactions -no change in concentration effecting intensity of effect |
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Pharmaceutical drug interactions
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physical and chemical incompatabilities like falling out of a solution
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Mechanism of Altered Absorption
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-drug binding (two drugs binding together because of taking them too close together)
-altered gut motility (speed at which speed moves through the gut) -altered Gut pH -altered gut flora |
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Altered Absorption Interactions of Highest Clinical Significance
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-cholestyramine/ many drugs (lower cholesterol, can bind to other drugs, absorption based interaction)
-ketoconazole/drugs or food which decrease gastric acid -tetracycline/ divalent or trivalent cations (loves to bind to Ca and not get absorbed) -flouroquinlones/ antacids, sucralfate, divalent or trivalent cations -oral contraceptives/ antibiotics |
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Enzyme Induction
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certain drugs are capable of increasing metabolic enzymes in the liver- enzymes can change drugs and make them inactive
-dose related -increase in levels of inducing drugs, increase in enzyme induction -body can only process so much drug at a time |
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Important enzyme inducing precipitant drugs
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anti-seizure drugs:
barbiturates carbamazepine *rifampin- treat TB most popular enzyme induction |
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Time Course of Induction Effects
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onset 5 days, maximal effect 2 weeks
offset 3 or more weeks slow onset, slow offset rifampin- onset 2-4 days, offset 2-3 weeks |
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Enzyme Inhibition
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-The most reported mechanism for interaction between two drugs
-A number of drugs are capable of decreasing the activity of Cytochrome P450 enzymes -drug concentrations goes up, toxity |
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Important Enzyme Inhibitors
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Erythromycin
*Antibiotics *Antifungals |
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Time Course of Inhibition
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fast onset, fast offset
more dangerous usually within 24 hours |
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Tubular Secretion
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from the blood to tubular system
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Tubular Reabsorption
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from tubular system into blood
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How nephron handles sodium and water
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proximal tube- 60-70% is reabsorbed
Ascending loop of henle- 20-25% absorbed water is reabsorbed in the collecting duct if ADH is present |
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MOA and primary use of acetazolamide
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-prevents reabsorption of bicarbonate
-increases osmotic pressure -causes osmotic diuresis -produces alkaline urine -eliminates more drugs for overdose |
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Generic Thiazides
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chlorothiazide
hydrochlorothiazide metolazone indapamide |
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Adverse effects of thiazides
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-hypokalemia
-hyperuricemia -hyperglycemia -hypercholesteremia |
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Conditions to use cation with thiazides
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-severe renal impairment
-diabetes mellitus -electrolyte imbalance -pregnant women -elderly -gout |
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Consequences of hypokalemia in using thiazides
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-arrhythmias
-orthostatic hypotension -muscle weakness/cramps |
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Generic names of loop diuretics
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-bumetanide
-ethancrynic acid -furosemide * |
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Adverse drug reactions for loop diuretics
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-hypokalemia
-hypomagnesemia -hyperuricemia -hypercholesterolemia -hypovolemia (decreased blood volume) -ototoxicity (hearing loss) -dematologic -gastrointestinal |
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Potassium- Sparing diuretics
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amiloride*
triamterene* spironolactone *similar |
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Risk groups for potassium sparing hyperkalemia
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-renal impairment
-diabetics -elderly |
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signs and symptoms of hyperkalemia
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parasthesias
muscle weakness flaccid paralysis bradycardia schock ecg abnormalities |
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MOA for spironolactone
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aldosterone receptor antagonist
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MOA for osmotic diuretics
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increase intravascular osmotic pressure
-keeps water and sodium in the tubule |
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Calculation of creatinine clearance
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IBW(male)= 50kg + (2.3 x in over 5ft tall)
IBW(female)= 45 kg + (2.3 in over 5 ft tall) CLcr= [140-age] BW ------------ (x 0.85 for females) [Scr][72kg] |
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Grading of renal impairment
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normal >80 ml/min
mild 50-80 ml/min moderate 10-50 ml/min severe <10 ml/min |
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Depressive Symptoms
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Must meet 5 with one being depressed mood or anhedonia
-weight loss/gain -insomnia/ hypersomnia -psychomotor agitation -fatigue or decreased energy -feelings of worthlessness -decreased concentration -recurrent thoughts of death -symptoms persist for at least 2 weeks |
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Neurotransmitters involved in depression
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serotonin
norepinephrine dopamine |
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Targets of medications
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-metabolic enzymes (MAO)
-reuptake transporter -receptors |
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Targets for treatment
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-serotonin transporter
-norepinephrine transporter -dopamine transporter -NE and 5-HT receptors -monoamine oxidase |
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Selective Serotonin Reuptake inhibitors
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-most commonly used
-safe, can't OD -prozac, zoloft |
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SSRI side effects
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-activation or sedation
-sleep distrurbances -nausea -sexual side effects -weight gain |
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SNRI side effects
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-nausea
-GI complaints -insomnia -sexual side effects -increased BP -sweating -agitation |
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Tricyclic antidepressants
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lethal in overdose as little as 3x daily dose
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Goal of treatment
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achieve remission
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Best antidepressant treatment
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all are equally effective
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MOA of antacids
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to neutralize stomach acidity
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Indications for antacid
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-peptic ulcer
-gastritis -gastric hyperacitity -heartburn |
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Drug interactions associated with antacids
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-tetracycline (binds to Ca
-methenamine -requires acidic urine -ketoconazole -increased gastric pH, decreases absorption |
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ADR of Aluminum hydroxide
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-constipation
-phosphate depletion -osteoporosis |
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ADR of Magnesium
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-diarrhea
-hypokalemia -hypermagnesemia |
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ADR Calcium carbonate
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-calcium stone formation
-acid rebound (body starts secreting more acid) |
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ADR of sodium bicarbonate
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-systemic alkalosis
-acid rebound -sodium overload |
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Patient tips for using antacids
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-take 1 and 3 hours after meals and at bedtime
-take 1 hour before and 2 hours after other meds -shake liquid preps -refrigerate liquids to taste better -no calcium antacids with milk or vitamins -chew tablets completely |
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MOA and indications for alginic acid
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forms a form that floats on the liquid present in stomach
-used for control of reflux symptoms |
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MOA and indications for simethicone
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defoaming agent used to relieve intestinal gas
-prevents the formation of large gas bubbles |
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Primary antiemetic use for scopolamine
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motion sickness
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primary antiemetic use for promethazine
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common in hospital drugs
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primary antiemetic use for ondansetron
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largest advances in treating cancer to prevent nausea in cancer drugs
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purpose of ipecac syrup
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home emergency treatment
-contraindicated for: unconscious caustic substances depressed gag reflex chronic use |
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Gastric Mucosal protection
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epithelial cells secrete mucus and bicarbonate to neutralize layer of cells in stomach
-blood flow to repair cells -prostaglandins |
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Heliobacter pylori in peptic ulcers
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bacteria that lives in the lumen of the stomach and can cause ulcers if other factors are present
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MOA of H2 Receptor antagonists
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partially block secretion of acid
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Indications for H2 blockers
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-treat and prevent duodenal ulcers
-treat gastric ulcers -GERD -hypersecretory states |
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Drug interactions with H2 blockers
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-anticoagulants
-antidepressants -antacids -ketoconazole |
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Common H2 blockers
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cimetidine
famotidine nizatidine ranitidine |
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MOA of Sucralfate
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forms a protective barrier at the ulcer site only in the intestine
-treatment, not prevention |
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Side effects of Sucralfate
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constipation, diarrhea, nausea
*caution in renal failure |
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MOA of Misoprostil
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prostoglandin analog
-prevents gastric ulcers while taking NSAIDS |
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Side effects of Misoprostil
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diarrhea, abdominal pain, gas, headache
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Cautions with Misoprostil
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contraindicated in pregnancy
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MOA of proton pump inhibitors
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completely blocks gastric acid pump
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Indications for proton pump inhibitors
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-severe erosive esophagitis
-hypersecretory gastric conditions -gastric and duodenal ulcers -GERD |
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MOA for bulk forming laxatives
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absorbs water to increase bulk and distension of bowls to initiate reflex action
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Indications for bulk forming laxatives
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regulatory
-psyllium (Metamucil) |
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MOA for stool softners
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wetting agent used to soften stool mass
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Indications for stool softners
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used in hospital preventativly
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MOA for stimulant laxatives
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increase peristalsis by iritating nerves in the colon
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indications for stimulant laxatives
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used for active constipation
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MOA for osmotic/saline laxatives
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increase water content of bowel stimulating peristalsis
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MOA for mineral oil
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coat feces easing passage of stool
-absorbs fat soluble vitamins, tends to leak from rectum, lipid pneumonia |
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MOA of glycerin
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used as a suppository in children
-osmotic action |
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MOA and side effects of diphenoxylate and atropine
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inhibits intestinal smooth muscle
-derivative of opium -dry mouth, dizziness, tachcardia, flushing |
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MOA and side effects of loperamide
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inhibits intestinal smooth muscle and firms up stool mass
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Purpose of atropine in diphenoxylate
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to reduce abuse associated with diphenoxylate's opium effects
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