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Flashcards in Pharm 1 Deck (99)
1

Pharmacokinetics

movement and alteration of the drug inside the body. absorption, distribution, metabolism, excretion

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Pharmacodynamics

action of the drug inside the body

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Therapeutics

to care for, tend to, or nurse

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ex. Of phototherapy

hyperbiliureinemia in neonates and skin diseases

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Chemotheraphy

treat infections, parasitic infestations, and malignancy with specific drugs that have selective toxicity for infecting organsims/malignant cells with not/minimal effects on the host cell

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Toxicology

study of poisonous effect of drugs and other chemicals and also includes the study of adverse effects of drugs

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clinical pharmacology

study of drugs in human

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pharmacogenetics/pharmacogenomics

study of genetic basis for variations in drug response

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plant

Plant _ Morphine, Atropine

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animal

Animal _ Heparin, Insulin

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human

Human _ GH, hCG

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mineral

Mineral _ Iron, Al(OH)3

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microbes

Microbes - Penicillin

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synthetic

Synthetic _Aspirin, Acetaminophen

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genetic engineering

Genetic Engineering - Insulin

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Ditoxin and digitoxin

from fox clove plant. Woman had edema used plant to decrease edema and doc studied it to from digitoxin

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generic name vs brand

acetaminophin vs tylenol

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chemical name vs generic name

acetylsalicylic acid vs asprin

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proprietary name

brand

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Routes of administration (7)

oral, sublingual, parenteral (IV/IM/SC/intraarterial/intraarticular/intrathecal/intraperitoneal/intradermal), rectal, inhalation, topical (vaginal/opthalmic), transdermal

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Sublingual

bypass portal system and first pass metabolism eg. Nitroglycerine

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parenteral

avoids mouth and intestines

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intraarterial

effect in local area

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intravenous

go to the whole body, not local actin

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intra thecal

injectioninto subarachnoid space in spinal cord. Used for spinal anestesia or brain conditions especially for drugs that don't cross the blood brain barrier

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topical

administere and action on the same site

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transdermal

action desiered is systeing--drug is absorbed from the skin

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oral pros

most common, convenient, noninvasive, self-medication possible, economical

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oral cons

cannot be used for uncooperative/vomiting patiens, certain drugs are not absorbed or destroyed by the gastric juices, cannot be given in emergencies, drugs are more likely to undergo first pass metabolism

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sublingual

no first pass metabolism, fast onset of action compared to oral route. Ex GTN (trinitorglycerine used for hypertension, heart failure), nifedipine (ca channel blocker)

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parenteral-intravenous pros

immediate action, useful in emergencies, avoids gastric juices/first pass metabolism, can be used in unconcious patients, irritant drugs can be given

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intravenous cons

painful, rusk of thrombophlebitis, expertise required, aseptic condition needs to be maintained, costly, attains high concentration in plasma and tissues and can cause toxicity

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intramuscular

mild irritant drugs can be given, absorption is quick, volume injected is max 10ml, no first pass metabolism

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subcutaneous

absorption is slow and constan, produce sustaned effect, mas 2 ml can be injected, self administration possible (insulin) pellet implantation (drug released over weeks--testosterone), silastic implants (drug released over months--contraception)

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intradermal

bcg vaccination, drug sensitivity testing

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intraarticular

steroids in rheumatoid arthritis

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intrathecal

used where durgs (lipid insoluble/highly polar) do not corss blood brain barrier but require action in brain or spinal space, strict aseptic precautions should be taken, eg. Amphotericin B in cryptococcal meningitis (poor penetration of BBB), spinal anesthesia, opiod analgesics (fentanyl)

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rectal

relatively little first pass metabolism, used in patients with vomiting or where drugs induces vomiting, larger amount and drugs with unpleasant taste can be administered, ex. Diazepam, acetaminophen, asprin (not given to children w/ fever bc they can develop reyes)

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topical

application of drugs to skin or to the mucus membrane like eye, ear, mouth, airway, rectum and vagina for local actions only, usually no systemic adverse effects

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transdermal delivery system

administration of drugs to skin for systemic effects, provides uniform plasma concentration, less inter-indificual variations, no first pass metabolism, convenient--better compliance, eg estradiol, gtn, scopolamine

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inhalation

delivery of drug to respiratory tract, alveolar epithelium offers good surface area for lipid soluble drugs, (fastes) very rapid onset of action due to large surface area and more vascualrity, drugs administered in gases or aerosol form, fapid action, no/less systemic toxicity, dose required is less, eg. inhalational anesthetics (nitrous oxide, ether, halothane), albuterol, steroids-beclomethasone in asthma

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inhalation cons

training for use (difficult for children and geriatrics), expensive, cannot be given to unconsious patients

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dose

amout/quantity ex 5mg (strength of drug)

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dosage form

the physical form in shich drug is taken ex. Tablet

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dosage form examples

solid, liquid, gaseous, semi-solid

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Absorption

passage of drugs from the site of administration to the system circulation/plasma (not seen w/ IV)

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process of obsorption

simple/passive diffusion, carrier-mediated facilitated diffusion, active transport, filtration, pinocytosis

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simple/passive diffusion

majority of drugs, high conc. To low conc., no energy, not satruable, not inhibited, lipid soluble drugs pass through lipid bilayer by this process, driving force is concentration gradient

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carrier-mediated facilitated diffusion

move along conc. Gradient but need carrier, no energy, highly selective, competitive, and sturable, ex. Vit B12, glucose

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active transport

against concentration gradient, req both carrier and energy, selective, competitive, and saturable, ex. Iron, levodopa

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filtration

passage of some water soluble substanses through aqueous channels in the tight junctions btw adjacent epithelial cells, minor role in drug absorption

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pinocytosis

ability of cells to enguf small droplets, important in unicellular organisms like ameba, not in multicellular organsims

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c max

maximal drug level obtained with the does

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t max

time at chich c max occurs

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lag time

time from administration to appearance in the blood

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onset of activity

time from administration to blood level reaching minimal effective concentration

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duration of action

time plasma concentration remains grater that minimum effective concentration (MEC)

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time to peak

time from administration to c max

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bioavailability

the proportion of the dose administered that is available at the systemic circulation, rate and extent of drugs reaching the systemic circulation in unchanged form (F)

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IV route bioavailability

100%, F = 1

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Bioavailability formula

F oral = auc oral / auc iv; change oral to whatever form of administration you want

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chemically equivalent

satisfy the chemical and physical standards in parmacopeia; dos not necessary mean biologically equivalent and therapeutically equivalent, differnet brands have different responses

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bioavailability - drug related - physical properties of the drug

physical state (liquids better than solids), lipid or water solubility (lipophillic drugs absorbed faster than hydrophillic drugs)

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bioavailability - drug related - nature of the dosage form

particle size, disintegration time and dissolution rate, formulation

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particle size

small are better absorbed bc inc surface area, inc abs, inc BA

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disintegration time

rate of breakup of tablets into particles, higher means lower abs and BA

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dissolution rate

rate at which drug goes into solution, higher means inc abs and inc BA

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formulation

binding agent/excipient_.incompatible formulation can slow abs and BA ex. Tetracylines w/ ca of mg as excipients slow abs and BA

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bioavailability - patient related - physicological factors

pH and ionization constant, gastric emptying, surface area and its vascularity, presence of food, first pass metabolism/pre-systemic elimination

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pH and ionization constant

non ionized (lipophillic) efficiently cross membranes

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acidic drugs are better absorbed in the

stomach

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henderson hasselbalch for acid

ph - pka = log ionized/nonionized

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henderson hasselbalch for base

ph - pka = log nonionized/ionized

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basic drugs are better absorbed in the

intestine

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pka

drug in and eqm of ionized and non ionized (50/50)

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ph > pka

good basic abs, more acid ionization (i.e. ph - pka = positive numbers)

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ph < pka

good acidic abs, more basic ionization (i.e. ph - pka = negative numbers)

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ionized drug - renal clearance, reabsorbtion

more renal clearance, less reabsorbtion

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non ionized drug vs renal clearance

inverse relationship

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gastric emptying time

lower means more abs more BA (exception - diarrhea)

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gastric emptying time accelerated by

metoclopramide

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gastric emptying time prolonged by

fatty meal, acid drinks, drugs w/ antimotility effects

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surface area and its vascularity

increase means inc abs, inc BA ex. More abs in intestine vs stomach due to inc SA, inc blood flow

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presence of food

can facilitate or hamper abs

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milk w/ tetracyline

dec abs

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food w/ ampicillin

dec abs

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fatty diets w/ griseofulvin

inc abs

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first pass metabolism

inc means dec BA

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Distribution

process by which drug reversibly leaves the blood stream and enters the interstitium represented by Vd

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Vd

apparent volume of distribution required to accommodate all the drug if the concentration of the drug throughout the body were the same as that in the plasma

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if plasma concentration is less

more drug is distributed to the tissues

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Vd formula

Vd = D / C

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Vd of Chloroquine

15000L, well distributed throught body

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Vd of Warfarin

8L, mostly remains in blood

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Vd of 4 L

restricted to vascular compartment

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Vd fo 14 L

distrbuted in extracellular fluid but not into cells

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Vd of 42

pass most biological barriers distributed in intra and extra cellular fluid

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Vd > 42

drugs are extensively stored within specific cells or tissues

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Vd vs Plasma concentration

inverse relationship