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93 Cards in this Set
- Front
- Back
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Which phase of trials for a new drug are randomized, placebo controlled, double blind, crossover studies?
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III
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What phase of trials are done to determine toxicity, best ROA, and dosage range? Who participates?
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Phase I, 20-100 healthy volunteers over several months
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How many people participate in phase II trials and for how long? What are the two main purposes?
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up to several hundred
several months to two years effectiveness and short-term safety of the drug |
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How long does review for "fast track" status take and what treatments can it be used for?
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Products that fill unmet needs in serious or life-threatening diseases
Review takes 6mo (as opposed to 10-12 mo) |
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What are orphan drugs?
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Drugs developed for orphan diseases which affect less than 200,000 people in the U.S.
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When was the orphan drug act passed?
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1983
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What are compassionate use protocols?
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need to get investigational drug approval before general approval
mush show preliminary efficacy patient likely to die without treatment no comparable therapy available |
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What needs to be submitted by companies wanting to put out a generic drug after patents have expired on a brand-name drug?
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ANDA (Abbreviated New Drug Application) as per the Act of 1984 (must be bioequivalent, will have exclusive marketing for 180 days)
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What surfaces in phase IV trials?
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Rare adverse events (often need very large number of subjects before see this that phase III trials don't reach)
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What is the difference between drug recall and drug withdrawals?
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Drug recall is temporary while withdrawal is permanent
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What is a class I recall vs a class II recall?
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Class I recall is when a serious or life-threatening consequence of ingestion is reasonably worried about (e.g. microbial contamination of injectable drug)
Class III is when health consequences probably would not result e.g. quantity packaging error |
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What is off-label use of drugs?
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When physicians prescribe the drug differently than recommended or for other conditions (may be beneficial but they are legally accountable if an adverse reaction happens)
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What law put the FDA in charge of determining which drugs could be sold OTC to treat symptoms (often lower dosages)?
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1951 Durhan-Humphrey
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What is the role of the FDA in dietary supplements?
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Approves them for safety but not efficacy (1994 Act)
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What are two of the key factors in determining appropriate dosage of a drug?
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Patients weight and body surface area
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What standards are used in estimating the dosages for adults?
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An adult that is 150lbs/70kg and 1.73m^2 in size (underestimate!)
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How does the recommended dosage change for the elderly?
Why? |
Usually decreases
May have less ability to inactivate or excrete drugs due to liver or kidney disease, respectfully |
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What is Clark's Rule for dosing drugs for children 2yo or younger?
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Weight of pt in lb/150lb * adult dose
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What is Young's Rule for dosing drugs for children 2yo or older?
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Age of pt in years/(pt age + 12) * adult dose
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What is the body surface area method of dosing for children?
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pt body surface area in m^2/1.73m^2 * adult dose
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Who is the surface area formula for drug dosage used for?
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FT infants (non-neonates), frail elderly, chemotherapy patients (or usage of other very toxic drugs)
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What are the categories for drugs based on safety during pregnancy?
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Category A means it is safe
Category D means there is possible fetal risk so the benefit vs. risk must be weighed Category X means that fetal abnormalities have been reported |
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What are two classes of drugs in which drug resistance is seen?
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Antibiotics
Chemotherapy |
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What are the three ways in which DNA may be transferred that alters cells in a way that makes them resistant to the therapy?
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Transformation
Transduction Conjugation* |
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What are some genetic abnormalities that alter drug responses?
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Plasma cholinesterase
Acetylation Microsomal oxidation Intrinsic factor |
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What is summation in terms of drug interaction?
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When two or more drugs act on the same receptor to produce an effect of the magnitude of the sum of each's individual effect
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What is synergism in terms of drug interaction?
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When two drugs that when given together produce an effect greater than the sum of each's individual effect
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What is the difference between dispositional and functional tolerance?
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Dispositional tolerance is the result of a lower concentration of the drug at the site of action while functional tolerance is when there are less receptors but the same concentration of drug
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What is the difference between tachyphylaxis and chronic tolerance?
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Tachyphylaxis or acute tolerance is low order and due to a depletion of response mechanism.
Chronic tolerance is high order specificity and is less responsiveness despite adequate levels that should elicit a response |
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What is drug resistance?
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Decreased sensitivity to drugs
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What is idiosyncrancy?
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An unexplainable abnormal response to a drug
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What is hypersensitivity?
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Altered reactivity to a drug which produces antibodies (acts as a hapten) -- exaggerated response next time
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What is hyper-reactivity?
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When the effect of a drug is more than expected for that dose.
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What is super-sensitivity?
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Then denervation or blockade of NT uptake result in hyper-reactivity to a drug or due to up-regulation of receptors (e.g. cocaine-induced supersensitivity to NE)
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What is drug dependence?
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When the CNS adapts so that tissue cannot function normally in the absence of the drug.
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Which schedule for controlled substance has the highest potential for abuse?
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C-I
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What is the dispensing requirements for C-II controlled substances?
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Must have written prescription
No refills allowed Container must have warning label ((may lead to severe physical or psychologic dependence)) |
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Which classes of controlled substances do not necessarily require a warning label?
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C-V
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What is type I injury mediated by?
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IgE, which stimulates mast cells to degranulate
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What are the symptoms of allergic rhinitis?
Signs? |
Arhinorrhea (thin, clear nasal discharge)
Nasal congestion Postnasal discharge Repeated sneezing Pruritis Pale or edematous nasal mucosa Transverse nasal creaes Allergic shiner |
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What are three chemicals related to allergies?
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Histamine (increases IP3 and DAG)
Leukotrienes C4, D2, E4 ECF (attracts eosinophils) |
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What are the differences in the roles of histamine and leukotrienes in allergic rhinitis?
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Histamine acts immediately and produces localized inflammation, lasts about an hour
Leukotrienes start to act as histamine is wearing off, produces persistent inflammation |
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What are three targets of allergy drugs? What acts at each?
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H1 receptors (antagonized by diphenhydramine, loratadine, fexofenadine)
PLA2 (inhibited by fluticasone) Degranulation of mast cells (inhibited by cromolyn sodium) |
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What is rhinitis medicamentosa?
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Rebound effect that results from overuse of nasal sprays
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What is the brand name for Claritin?
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Loratadine
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What is a side effect of diphenhydramine?
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Antimuscarinic activity since H1 receptor is related to muscarinic receptor
Marked sedation |
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Loratadine and Fexofenadine are active metabolites of which other H1-antagonists?
What are the advantages of the first two? |
Terfenadine
No prolonged QT Not inactivated by enzyme inhibitors as easily Does not cause drowsiness |
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What drugs can have interactions with Loratadine or fexofenadine?
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MAO-inhibitors
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How are corticosteroids anti-inflammatory?
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Block eicosinoid synthesis by stimulating production of PLA2 inhibitory proteins (lipocortins/annexins) which inhibit the release of arachidonic acid
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What is the chemical name of Flonase?
How is it taken for asthma? |
Fluticasone propionate
Orally |
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What is the best use for cromolyn sodium?
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Prophylactic use (needs to be used for a few weeks before it works) as an aerosol or sometimes eye drops
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What is one method of long term relief for allergies?
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Desensitization from intradermal injections --- induce formation of IgG
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What are three bronchoconstrictors in asthma?
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histamine
leukotrienes ECF |
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Is inspiration or expiration affected more in an acute asthma attack?
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Both are affected but expiration is harder than inspiration (due to overinflation)
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What is heard on auscultation in an asthmatic having an attack?
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Hyper resonant lung sounds
Diminished breath sounds Wheezes Rhonchi NO RALES |
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What causes death in asthma attacks most often?
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Asphyxiation due to mucous plug formation because of leukotrienes in the lungs
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What are two beta-2 receptor agonists?
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Albuterol (proventil) --rescue (((increases cAMP)))
Salmeterol (Serevent, Advair) -- prophylactic used in asthma |
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What do beclamethasone (flovent) and prednisone do?
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inhibit PLA2
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What is theophylline? What does it do?
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oral xanthine derivative that causes bronchodilation so helps with asthma
increases cAMP by inhibiting PDE which mediates cAMP-->AMP |
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What is beclamethasone (beclovent, vancenase)?
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A synthetic inhaled glucocorticoid
May result in hoarseness or thrush |
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What is prednisone?
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Oral corticosteroid that inhibits PLA2 and is metabolized by the liver and shows very little mineralocorticoid activity
May cause peptic ulcers or redistribution of fat into moon face |
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What do category B drugs Zafirlukast (Accolate) and Montelukast (singulair) do?
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Block Leukotriene D4 and E4 receptors
Zafirlukast inhibit bronchoconstriction in this way which is caused by sulfur dioxide, cold air, and attenuates reactions cauesd by grass, cat dander, ragweed, and possibly aspirin-induced asthma |
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What does cromolyn sodium treat?
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Allergies and is prophylactic for asthma (but not useful in treatment of acute extrinsic asthma)
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What does histamine binding to H1 receptors in the lungs cause in acute asthma attacks and/or anaphylaxis?
What does histamine binding to H2 receptors in the upper respiratory tract cause? |
H1---bronchospasm
H2---vasodilation, inflammation |
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What happens in hypovolemic shock?
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Histamine binds to vascular H2 receptors causing smooth muscle relaxation-->dilation, and increased vascular permeability-->reduced blood volume
Congestion and edema in liver, spleen, kidney Histamine binds to H1 receptors in the GI tract causing constriction and abdominal cramping |
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What treatments are used to alleviate the CV symptoms of anaphylaxis?
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Aqueous epinephrine (IM or subcutaneously)
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What treatments are used to alleviate the cutaneous and GI symptoms of anaphylaxis?
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Antihistamines, diphenhydramine
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What treatments are sued to alleviate the pulmonary symptoms of anaphylaxis?
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Bronchodilators: Albuterol, Epinephrine
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What is an example of delayed hypersensitivity?
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Contact dermatitis
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What is an example of delayed hypersensitivity?
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Contact dermatitis
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What is an example of delayed hypersensitivity?
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Contact dermatitis
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What is the treatment for contact dermatitis?
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Topical application of cortisone creams
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What is the treatment for contact dermatitis?
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Topical application of cortisone creams
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What is the treatment for contact dermatitis?
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Topical application of cortisone creams
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What i the most important and most common mechanism of drug permeation?
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Passive transfer
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What types of drugs can do passive transfer?
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Non-ionized, lipid soluble
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What is different between capillaries, the glomeruli of the kidney, and capillaries of the pituitary and pineal glands, median eminence, choroid plexus, and area postrema (which causes you to vomit when toxic substance ingested) and the epithelial lining of the cornea, gut, and bladder in terms of drug absorption?
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large pores between cells, larger molecules can pass through but not if bound to protein
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What determines the rate of facilitated diffusion?
What is the driving force? |
The binding capacity of the solute and carrier
Driven by concentration gradient |
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What are some examples of carriers for facilitated diffusion?
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AA carriers in blood brain barrier
Weak acids in PCT of kidney Glucose |
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Where in the body are most drugs absorbed?
What affects the rate of absorption here? |
GI tract
Lipid solubility |
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Where are acidic drugs absorbed? Basic drugs?
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Acidic drugs in the stomach
Basic drugs in the intestine |
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What is the beginning point and endpoint of duration of drug effect?
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Onset to termination
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Why is the pulmonary system a good place for biotherapeutic administration?
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Large alveloar surface area, think tissue lining, limited proteolytic enzymes
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Which concentration would you want to know if you are worried about toxicity?
What about if you are worried about resistance? |
Peak concentration
Trough concentration (look at package insert to time when you will measure the amount in their blood) |
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What are 3 things that make the skin more permeable to drugs?
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Lipid solubility of drug
Damaged epidermis Wetting skin or applying drug in DMSO |
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What is a good way to compare the bioavailability of various drugs?
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Measure the area under the curve of each
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A drug staying in what part of the intestine longer will result in increased absorption?
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Proximal 1/4 small intestine
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Are ionized or nonionized drugs better absorbed?
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Nonionized
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When will 50% of a drug be absorbed?
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When drug is in place with a pH equal to its pKa, because then half ionized...if a weak acid drug put in pH higher than its pKa, will not be absorbed
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Where are the TJs in the BBB? In the choroid plexus?
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Endothelium
Epithelium |
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What are 4 most highly perfused organs in terms of blood flow and weight?
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Liver
Kidney CNS Myocardium |
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What order are most drugs eliminated by?
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First order (rate of elimination is proportional to amount of drug in the compartment)
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What is the formula for volume of distribution?
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amount of drug in body/concentration in plasma
dose/concentration in plasma MAKE SURE UNITS MATCH |
