Pharmacology Final Exam

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What are the three most important properties of an ideal drug?

safe, effective, selective

Define effective.

produces the anticipated response

Define safe.

can't produce harmful effects even in high doses

Define selective

only produces the desired effect

What are some important properties of an ideal drug other than safe, effective, and selective? (7)

reversible action, predictable, easy administration, free of interaction, affordable, chemically stable, simple generic name

What are the three names that every drug has?

chemical, generic, brand or trade

What is a chemical name?

precise description of the chemical composition and molecular structure of the drug

What is a generic name?

nonproprietary name assigned by the US Adopted Names Council

What is a trade name?

proprietary name selected and marketed by a pharmaceutical company

Are generic and brand name medications the same?

yes

What drugs would we be concerned about switching for a generic to a brand name?

low therapeutic indexes (warfarin)

What are the six rights of medication administration?

medication, patient, dose, route, time, documentation

What information should you give the patient about their prescription?

drug name, therapeutic category, dosage size, dosing schedule, route of adminisration, technique of administration, non-pharmacologic measures, expected response, duration of treatment, method of storage, major adverse side effects, drug-drug interaction, drug-food interaction, contact person

What is a randomized controlled trial?

RCTs are the most reliable way to objectively assess drug therapies. Subjects in an RCT are either given a experimental drug or a control (standard or placebo) for comparison.

Why is randomization important?

to prevent allocation bias which results when subjects in the experimental group are different from those in the control group

What is a blinded study?

one in which the people involved do not know to which group - control or experiment - individual subjects have been randomized

What is a double blind study?

the researchers as well as the subjects do not know to which group - control or experiment - subjects have been placed

What is the order of new drug development? (5)

preclinical testing, clinical testing phase I, II, III, and IV

Which phase of new drug development is drug metabolism, pharmacokinetics, and biologic effects assessed?

phase I

Which phase(s) of new drug development assess(es) therapeutic effects, dosage range, safety, and effectiveness?

phase II and III

Which stage of new drug development involves animals?

preclinical testing

Which phase of new drug development involves healthy subjects?

phase I

Which phase of new drug development is postmarketing surveillance?

phase IV

Drug development has historically excluded which groups of people?

women, children, those with co-morbidities

What are the three phases of drug activity?

pharmaceutical, pharmacokinetic, pharmacodynamic

What are the two main components of the pharmaceutical phase of drug activity?

disintegration of dosage form, dissolution of drug

What are the four main components of the the pharmacokinetic phase of drug activity?

absorption, distribution, metabolism, excretion

What is the pharmacodynamic phase of drug activity?

drug-receptor interaction

Arrange the following oral dosage forms from slowest to fastest absorbing. (powders, tablets/capsules, liquids/elixirs/syrups, EC tablets, suspension solutions, coated tablets)

EC tablets, coated tablets, tablets/capsules, powders, suspension solutions, liquids/elixirs/syrups

What is a p-glycoprotein?

transport system that moves drugs form one side of a cell membrane to another

Where are p-glycoproteins found? (4)

liver, kidney, placenta, intestine, brain

What kinds of drugs can directly penetrate cell membranes?

lipid soluble (lipophilic)

What drugs cannot directly penetrate cell membranes? (3)

polar molecules, ions, those that are too large to pass through channels or pores

What is absorption?

process involving the movement of drug molecules from the site of entry into the body to the circulating fluids

What is distribution?

the transport of drug from the bloodstream to various tissues

Distribution is most affected by this drug characteristic.

protein binding

Is a drug that is bound to protein pharmacologically active?

no

What is Vd?

volume of distribution; relates the amount of drug in the body to the concentration of drug in the blood

Where is most of a drug located when it has a high Vd?

extravascular tissue

Where is most of a drug located when it has a low Vd?

vascular compartment

What is metabolism?

the process of chemically inactivating a drug by converting it into a more water-soluble compound or metabolite that can be excreted from the body

Biotransformation is another term for _____.

metabolism

Where are a majority of drug metabolized?

liver

What is the cytochrome P450 system?

hepatic enzyme system responsible for drug metabolism

What is a CYP substrate?

a drug that is metabolized by P450

What is a CYP inducer?

a drug that induces the metabolism of another drug

What is a CYP inhibitor?

a drug that inhibits the metabolism of another drug

A CYP inhibitor does what to the inhibited drug's half-life?

increases it

What is a prodrug?

a compound that is pharmacologically inactive as administered and then undergoes conversion to its active form within the body

Describe the process of Tylenol poisoning.

Tylenol (acetaminophen) is converted into a hepatoxic metabolite following metabolism in the liver; it is this product of metabolism, and not acetaminophen itself, that causes toxicity

Would you except to see increased or decreased metabolism in a malnourished patient? Why?

decreased; not as many CYPs due to insufficient protein intake

What is excretion?

The process by which drugs and metabolites are eliminated from the body

What organ is most important in excretion?

kidneys

List common excretion sites. (6)

urine, bile - feces, expiration, sweat, saliva, lactation

What is the most convenient route of drug administration?

oral

What are the two major disadvantages of enteral drug administration?

variability, inactivation

Where are sublingual drugs administered?

under the tongue

Name a SL drug.

nitroglycerin

Where are buccal drugs administered?

between the gums and mucous membranes of the cheek

What drugs are administered in a buccal route?

hormone preparations

The following parenteral routes are ordered from fastest to slowest or from slowest to fastest absorptive rate? SC, IM, IV

slowest to fastest

Where is SC injection administered?

connective tissue or fat

What are the barrier(s) to absorption for IV administration?

none

What are the barrier(s) to absorption for IM administration?

capillary wall

Where are intrathecal drugs administered?

spinal subarachnoid space

Where are epidural drugs administered?

epidural space of spinal column

Why is the pulmonary route of drug administration great for absorption? (2)

large surface area, rich capillary network

Where are topical preparations used? (5)

eyes, ears, nasal mucosa, mouth, vagina

Do rectal preparations have local or systemic effects?

may be local or systemic

How are transdermal drugs prepared?

patches

What is the hepatic first-pass effect?

a significant amount of drug is metabolized by the liver before reaching systemic circulation

Why is the dosage of morphine PO so much higher than the dosage IV?

hepatic first-pass effect

What is half-life?

time for the amount of drug in the body to decrease by 50%

If the dosage of PO morphine was doubled, would its half-life increase, decrease, or stay the same?

stay the same

If a patient has hepatic or renal dysfunction, you should expect the half-life to be longer or shorter?

longer

How many half-lives does it take for a drug to reach plateau (a steady level)?

3-5

How many half-lives does it take for a drug to be eliminated?

3-5

What is the therapeutic index?

measure of the relative safety of a drug; LD50/ED50

What is the lethal dose (LD)?

dose that is lethal in 50% of lab animals tested

What is the effective dose (ED)?

dose required to produce therapeutic effect in 50% of a similar population

A safe drug would have a high or low therapeutic index?

high

What is a toxic adverse reaction?

adverse drug reaction by excessive dosing

What is an idiosyncratic effect?

uncommon drug response resulting from a genetic predisposition

What is physical dependence?

a stage in which the body has adapted to drug exposure in such a way that an abstinence syndrome will result if the drug use is discontinued

What drugs high physical dependence rates? (3)

opioids, barbiturates, amphetamines

What is iatrogenic disease?

disease produced by a health-care professional

Drug-induced PD is an example of what type of adverse reaction?

iatrogenic

What is a teratogenic effect?

drug-induced birth defect

What is tolerance?

educed physiological response occurring after repeated drug administration

What is tachyphylaxis?

developing tolerance quickly after repeated administration

What is the cumulative effect?

additive effect of repeated dosing that can cause harm

If a drug is supposed to be given "with food," when do you give it in relation to meal time?

with or shortly after meals

If a drug is supposed to be given "on an empty stomach," when do you given it in relation to meal time?

1 hour before or 2 hours after

Do drugs generally cause upset in conjunction with food?

no

What are the two components of the CNS?

brain, spinal cord

What are the two major components of the peripheral nervous system? Which is voluntary? Which is involuntary?

somatic (voluntary) and autonomic nervous system (involuntary)

What are the two divisions of the ANS?

parasympathetic nervous system (PNS) and sympathetic nervous system (SNS)

Which division of the ANS has cholinergic effects?

PNS

Which division of the ANS has adrenergic effects?

SNS

During parasympathetic activity, the heart rate is increased or decreased?

decreased

During parasympathetic activity, pupils should be constricted or dilated?

constricted

What is innervated by both the PNS and SNS and produces complementary effects?

male reproductive function; PNS erection, SNS ejaculation

What are the four subtypes of adrenergic receptors?

alpha1, alpha2, beta1, beta2, dopamine

What is the result of alpha2 activation?

in the CNS, reduced sympathetic outflow to heart and blood vessels and relief of severe pain

Blood vessels are innervated by what division of the ANS?

SNS

What is the most important feedback loop of the ANS?

baroreceptor reflex

What does the baroreceptor reflex regulate?

blood pressure

Where are baroreceptors located?

carotid sinus and aortic arch

Adrenergic receptors are mediated by what neurotransmitter(s)?

EPI, NE

Cholinergic receptors are mediated by what neurotransmitter(s)?

ACh

What is the response of alpha1 activation for the following? (eye, arterioles, veins, male sex organs, prostate capsule, bladder)

mydriasis (dilation), constriction, constriction, ejaculation, contraction, contraction (sphincter)

What are three clinically significant actions of alpha1 agonists?

mydriasis (dilation), increased BP, nasal decongestion

What are two clinically significant actions of alpha1 antagonists?

decreased BP, decreased urinary symptoms associated with enlarged prostate

Where to beta1 receptors act?

heart, kidney

What is the response of beta1 activation for the following? (heart, kidney)

increased HR, increased AV node conduction, increase force of contraction; renin release

What are three clinically significant actions of beta1 agonists?

increase HR, increase cardiac output; increased BP with renin release

What are two clinically significant actions of beta1 antagonists?

decreased HR, decreased BP

Where do beta2 receptors act? (4)

bronchi, uterus, liver, select arterioles (heart, lungs, skeletal muscle)

What is the response of beta2 activation for the following? (bronchi, uterus, liver, select arterioles)

dilation, relaxation (to avoid labor), glycogenolysis, dilation

What are two clinically signficant actions of beta2 agonists?

bronchial dilation; relaxation of uterine smooth muscle

What cholinergic receptor subtype is activated by the PNS?

muscarinic

Where do muscarinic receptors act? (6)

eye, heart, lung, bladder, GI tract, male sex organs, sweat glands

What is the response of muscarinic activation for the following? (eyes, heart, lung, bladder, GI tract, male sex organs)

miosis (near vision focus), decreased rate, bronchial constriction, voiding, salivation/increased motility/gastric secretions/defecation, erection

What does the ending "mimetic" mean? For example, sympathomimetic.

agonist; SNS agonist

What does the ending "lytic" mean? For example, parasympatholytic.

antagonist; PNS antagonist

Using the ending "mimetic" or "lytic" construct a term to describe beta-blockers.

sympatholytic

What drug would need to be avoided when using prazosin (Minipress), an alpha1 anatgonist?

PDE5 inhibitors like Viagra

Name a non-selective beta-blocker.

propranolol

What is a cardio-selective beta-blocker?

one that only acts on beta1 receptors

Name a cardio-selective beta-blocker.

metoprolol (Lopressor), atenolol (Tenormin)

What type of beta-blocker is carvedilol (Coreg) and labetalol (Trandate)?

beta1, beta2, and alpha1

What type of effects does atropine elicit?

anticholinergic

What are the adverse effects of atropine?

blurred vision, photophobia, urinary retention, xerostomia (dry mouth), constipation, elevation of intraocular pressure, anhidrosis (absence of sweat), tachycardia, asthma (plugging secretions)

Phenotalamine (Regitine) is an antagonist of what receptors of the ANS?

alpha1,2

What do laxatives do?

soften stool, increase stool volume, hasten fecal passage through the intestine, facilitate evacuation from the rectum

What are the actions of bulk-forming laxatives? What group are they? What is their response time?

swell in water to soften and increase the bulk of fecal mass; group III; 1-3 days

Which class of laxative(s) do you need to take with a full glass of water?

bulk-forming, surfactant

Name two examples of bulk-forming laxatives.

psyllium (Metamucil), methylcellulose (Citrucel)

What are the actions of surfactant laxatives? What group are they? What is their response time?

lower surface tension to facilitate the movement of water into the stool; group III; 1-3 days

Name an example of a surfactant laxative.

docusate sodium (Colace)

What are the actions of stimulant laxatives? What group are they? What is their response time?

stimulate intestinal motility and increase water and electrolytes within the intestine; group II; 6-12 hours

Name two examples of stimulant laxatives.

bisacodyl (Correctol, Dulcolax, Feen-a-mint), senna (Ex-Lax, Senokot)

What are the actions of osmotic laxatives? What group are they? What is their response time?

osmotic action draws water into the intestine to the poorly absorbed compounds; group I; 2-6 hours

Name three examples of osmotic laxatives.

milk of magnesia, polyethylene glycol (Miralax), sodium phosphate (Fleet Phospho-Soda)

What toxicities are observed with osmotic laxative use? (2)

K+, Mag

What class of drug can induce peptic ulcer disease?

non-steroidal anti-inflammatory drugs (NSAIDs)

Where are H2 receptors located? What is their function?

parietal cells; activation promotes gastric acid secretion

What is the function of H2 blockers?

suppress acid secretion by blocking the receptors that promote acid secretion

What is the common ending for H2 blocker drugs?

-tidine

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