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Pharm > Quiz 2 > Flashcards

Quiz 2 Flashcards

1
Q

Agonism

A
  • ligand binds and stimulates R
  • drug on R activates
  • mol/cel resp
  • intrinsic activity = 1
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2
Q

Partial Agonism

A
  • drug on R activates
  • partial efficacy
  • intrinsic activity 0-1 or <1
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3
Q

Antagonism

A
  • drug on R prevents agonist binding
  • no resp to agonist
  • Also blocks baseline stim, so can take below baseline
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4
Q

Irreversible Antagonism

A
  • stays bound to R
  • high conc agonist may overcome
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5
Q

Competitive Antagonism

A
  • ag/ant both act on same R
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6
Q

Noncompetetive Antagonism

A
  • ant binds to one R preventing ag binding to different R
  • ag must not be bound for ant to bind
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7
Q

Opioid example of degrees of R activation

A
  • Methodone = full ag
    • high R activation
  • Buprenorphine = partial ag
    • medium activation
    • partial efficacy
  • Naloxone = antagonist
    • higher affinity
    • blocks/prevents ag activity
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8
Q

Pharmacologic Antagonism

A
  • antagonism at the R level
  • competetive and noncompetetive
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9
Q

Effect Antagonism

A
  • system level antagonism
  • ex: one drug works in brain to incr BP, a different one works in the heart to decr BP
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10
Q

Drugable Targets

A
  • places in proc we can aim to intervene with drug to effect system
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11
Q

Ligand-Gated Ion Channels

A
  • R binding causes ion channel to open
  • ions flow down a pre-established gradient to produce effect
  • ex: ACH opens channel, Na+ flows in depolarizing memb

-> initiates action potential

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12
Q

Voltage-gated Ion Channel

A
  • nearby memb pot changes conformation of channel
    • open/closed
  • Sz drugs stabilize hyper-exitable membranes
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13
Q

Na/K pump

A
  • Pump -> energy consuming
    1. E required
    2. moves ions against gradient
  • ex Dig inhibits NaKATPase
    • Na out/K in against gradient/establishing gradient
    • inh causes >Na inside, slowing export of Ca out
    • >Ca inside >contractility (force of contraction)
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14
Q

Enzymes

A
  • Catalyze rxn: A(substrate) + B(substrate) <=>C(product)
  • enz inhibitors
    • inh substrate from entering enz active site
    • ex AChE inhibitor: slows cleavage of ACH inc amt in syn cleft
  • also activators
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15
Q

RAAS

A
  • angiotensinogen —renin–> angiotensin I —ACE–> ang II
  • need quick response from system so gen is available to be converted rather than having to start from scratch
  • 3 targets
  1. renin inhibitor = tecterna
  2. ACEi’s
  3. ARB’s
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16
Q

Pharmaceutics

A
  • Science of dosage form design
  • preparing drugs for administration
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17
Q

Absorption

A
  1. moving drug from outside to inside of body
  2. across a bio memb
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18
Q

Enteral Absorption

A
  • Gut is most convenient
  • mouth to rectum
  1. mouth
  2. stomach
  3. SI
  4. rectum
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19
Q

Enteral: mouth

A
  • thin lining, rich blood supply -> rapid action
  • sublingual/buccal routes
  • swallowing not req
    • antiemetics
    • >compliance
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20
Q

Enteral: stomach

A
  • medium SA, rich blood supply, acidic pH
    • most drugs dis better in base
  • drugs don’t stay here long
    • variable with food in stomach/empty stomach
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21
Q

Enteral: small intestine

A
  • huge SA
  • rich blood supply
  • basic pH
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22
Q

Enteral: rectal

A
  • small SA, rich blood supply, basic pH
  • uses:
  1. N/V
  2. local effect to rectum/colon (ulcerative colitis)
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23
Q

Parenteral Administration

A
  • Bypasses membranes
    • IV
    • IA (artery)
    • IM
    • IT (inside thecal sac/spinal canal, also bypass BBB)
    • SQ
    • Epidural (next to thecal memb)
    • Intra-articular
      • low blood supply so little circulating drug gets there
      • ex: lubricant to knee
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24
Q

Topical Administration (sites)

A
  • Skin
  • Eyes
  • Ears
  • Intranasal
  • Inhalation
  • Vaginal
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25
Q

Topical: skin

A
  • ointments, creams, patches
  • local and systemic
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26
Q

Patches

A
  1. doesn’t rub/wash off
  2. ~occlusive dressing - changes skin properties >abs
  3. control dose, preloaded in patch
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27
Q

Topical: eyes

A
  • drops, ointments
  • local
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28
Q

Topical: ears

A
  • local
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29
Q

Topical: intranasal

A
  • sprays and drops
  • local
    • steroid
  • systemic - when it allows to bypass injection
    • narcan
    • migrane med
    • vaccines
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30
Q

Topical: inhalation

A
  • local
    • asthma drugs
  • systemic - difficult to predict absorption
    • inhaled insulin
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31
Q

Topical: vaginal

A
  • Local primarily
  • Systemic (contraceptives, primarily local w/systemic effects)
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32
Q

Pharmaceutical Phase

A
  • Disintegration
    • tablet to particles
    • >SA -> dissolves faster
  • Dissolution
    • particles to molecules in solution
    • Must be in solution to cross memb
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33
Q

Oral dosage forms - fastest to slowest

A
  1. dissolved liquid (elixer, syrup)
  2. suspension
  3. powder
  4. capsule
  5. tablet
  6. coated tablet/caplet
  7. enteric coated tablet
  8. sustained release
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34
Q

Dissolved liquid

A
  1. inconvenient
  2. tastes bad
  3. patient controls dose
  4. abs faster
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35
Q

Suspensions

A
  • chunks of drug floating in liquid
  • drug settles
  • may be more conc toward end if not always mixed properly before use
  • taste bad/bad mouth feel
  • patient controls dosage
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36
Q

Powders

A
  • in powder papers
  • unit dose
  • tear corner and pour into water
  • not really used any more
37
Q

Capsules

A
  • powder inside
  • modern “powder paper”
38
Q

Tablets

A
  • compressed powder
  • with exipients
39
Q

Coated tablets/Caplets

A
  • slower dissolving, <bad>
    </bad><li>easier to swallow</li>

</bad>

40
Q

Enteric-coated Tablets

A
  • don’t dis in acid
    • protects dosage (panc enz: act in duo, destroyed in stom)
      • else 50x dosage and hope some gets to duo
      • else enz w/antacid (inconvenient)
    • for drugs that upset stomach (ASA)
41
Q

Sustained Release

A
  • slow abs/time
  • short duration drugs -> long duration (ex procardia q6h or XL daily)
    1. allergy capsule w/colored beads
      1. red = IR
      2. blue = 4-8 hr coverage
      3. green = 8-12 hr coverage
    2. layered tablets - outer, inner, center layers
    3. GI transport system - procardia/nifedipine
    • water absorbing matrix - water in a constant rate
    • pushed memb up at constant rate, pushing drug out hole
  • Theo-24: dose dumping->arrhythmias, sz, death
42
Q

Pharmacokinetics

A
  • what body does to drug
  • mathematical models to make predictions
  • pharmacokinetic phase = absorption
43
Q

Diffusion: passive v. facilitated

A
  • most are passive diffusion
  • facilitated
    • membrane carrier molecule binds outside and releases inside
    • not against gradient
    • no energy expenditure
44
Q

Rate of absorption determines…(3)

A
  1. onset of action - faster abs -> faster onset
  2. duration of action - slower -> extended duration
  3. Intensity of response - faster -> inc levels, same dose >intense resp
    • ex: beer over 1/2h, 5min, beer bong
45
Q

Variables affecting absorption (4)

A
  1. nature of absorbing surface - skin v intestinal mucosa
  2. SA - small v large intestine
  3. blood flow (PIV not so good for patients in shock)
  4. pH as site
46
Q

Bioavailability

A
  • % of dose that reaches systemic circ (F or f in dec form)
  • First Pass Effect
47
Q

First Pass Effect

A
  • Factors affecting dose before it reaches sys circ
  1. stomach acid
  2. stomach enz
  3. slow/poor diffusion across memb
  4. liver met
  • ex:
    • ganciclovir poorly abs f=0.09 => 10x dose
    • propanolol hepatic met f=0.26 => ~75% removed first pass
48
Q

Distribution

A
  • ka = rate abs (drug in)
  • ke = rate elimination (drug out)
  • ka = ke => constant levels
  • One compartment model
    • one central compartment = blood
  • Two compartment model
    • administered to central compartment = blood
    • redistributes to second “tissue” compartment
      • skel m, fat, etc <=> in equilibrium
    • conc proportional between 2 compartments at a certain time
      • Dig @ 3-4h blood conc~heart tissue conc
        • earlier would give false high
        • not toxic in blood, toxic in heart
49
Q

Drug Elimination

A
  • “Removal of activity of drug”
    • biotransformation
    • excretion
50
Q

Biotransformation

A
  1. inactivating drug (active to inactive = eliminating)
    • hepatic met
      • cytochrome P-450
      • Ox/Red
      • Conjugation
    • Tissue enz
      • GI tract
      • Lungs
      • Kidneys
  2. activating drug also
51
Q

Excretion

A
  • Removal of still active drug
  1. kidneys
  2. Gi tract
  3. lungs (exhaled as in breathalyzer)
  4. sweat glands
  5. salivary glands
  6. mammary glands - active form?.. to baby
52
Q

Clearance

A
  • clearance is abstract
  • half-life is more common
    • time to reduce circulating amount by 50%
    • short half-life = more frequent dose
    • sometimes misleading -
      • emeprozole
        • short half-life, long duration of action
        • enters cell and remains active
      • propanolol - irreversible blocker, effects last longer
53
Q

Creatinine Clearance

A
  • change dose of renally excreted drugs based on renal fx
  • assess renal fx
    • serum Cr most commonly used
      • not nec accurate
    • CRCL
      • Cr constant rate of prod, removed through Glom filt
      • GF estimated by CRCL
      • >80 unlikely impairment
      • 50-80 mild impairment (narrow tx range req change)
      • <50 moderate impairment (many may req dosage change)
      • <10 severe impairment (look up drugs)
54
Q

Formula for CRCL

A

CRCL in ml/min

CLcr =

(140-age)IBW

——————- x (*.85 for females)

(Scr)(72)

IBW

  • male 50kg + (2.3 x inches over 5ft)
  • female 45kg + (2.3 x inches over 5ft)
55
Q

When would you use actual BW v IBW?

A
  • actual BW when excess wt is muscle, body builder
    • Cr=1.2, CrCl=109
  • IBW when excess wt is fat - doesn’t give credit for fat towards renal fx
    • Cr=1.2, Crcl=38 = moderate impairment
56
Q

MDRD

A
  • Modification of Diet in Renal Disease
  • valid for GFR<90ml/min
  • not accurate for emaciated or cirrhotic pts
  • more accurate but less common/less drug info provided
    • so use CrCl
  • GFR = (175)(Cr)-1.154(Age)-0.203(0.742females)(1.1212blacks)
    • 175cr1154age02030742f11212b
    • tickle cr to tell her age so name sake ron toten don
57
Q

Time-Concentration Curve

A
  • Concentration over time after dose is administered
58
Q

Absorption Phase

A
  • Drug is being absorbed faster than it is being eliminated
59
Q

Cmax

A
  • Maximum concentration
  • End of abs phase
  • Beginning of elim phase
60
Q

Elimination Phase

A
  • Drug is being eliminated faster than it is being absorbed
61
Q

Minimum Effective Concentration

A
  • MEC
  • must be above this to get measurable effect of drug
62
Q

Toxic Level

A
  • concentration level where increased risk of toxicity is seen
63
Q

Therapeutic Range

A
  • between MEC and toxic level
  • unimportant/unknown for many drugs
  1. drug has such a wide range
  2. blood level doesn’t correlate to effect
64
Q

Onset of Action

A
  • Time when MEC is achieved
65
Q

Duration of Action

A
  • [Time when conc falls below MEC] minus [Onset of Action]
66
Q

Drug-Drug Interactions

A
  • give 2 drugs and something different happens then giving the 2 drugs alone
    • antagonism - one offsets the activity of the other
    • synergism - one enhances the other
    • idiosyncratic - unpredictable
67
Q

Drug-Food Interactions

A
  • oral phenetoin + enteral feedings
    • head injury, sz
    • enteral feedings
    • 300mg normal, 2g required to overcome interaction
    • then enteral feeding stops or decreases -> overdose
68
Q

Drug-herbal interactions

A
  • herbal medication interacts with prescription drug
69
Q

Drug-laboratory Interactions

A
  • Drug interferes with results of a particular assay
70
Q

Pharmacokinetic Drug Interaction

A
  • levels
  • one drug causes the blood level of another drug to change +/-
  • alters rate or extent of absorption, dist or met of other drug
71
Q

Object Drug

A
  • drug whose level is changed by another, precipitant drug
  • the victim
72
Q

Precipitant Drug

A
  • Causes a change in the levels of the object drug
73
Q

Pharmacodynamic Interaction

A
  • actions
  • one drug causes a change in patient response to another drug without altering the object drug’s kinetics
  • Pharmacological interaction
  • 2 drugs for BP cause greater drop than expected, no change in blood concentration = synergistic pharmacodynamic interaction
74
Q

Pharmaceutical Interactions

A
  • physical and chemical incompatibilities
  • IV admixtures -> precipitates
75
Q

Potential for Interactions

A
  • 4,000 drugs available in U.S.
  • 25% of pop on 5+ products
  • Possible combinations… too big to say
  • So identify patients and drugs at greatest risk
76
Q

Patients at Greatest Risk

A
  • multiple meds #1-more drugs, more risk
  • multiple docs
  • multiple pharmacies
  • elderly - more meds, worse response to rxn
  • obese - generally less healthy, multiple diseases, more meds
  • critically ill - more susceptible, less tolerance to rxn
77
Q

Object drug characteristics

A
  • narrow therapeutic range, ex coumadin
  • steep dose response curve - 2x dose -> 4x response
  • hepatically met drugs
  • chronic use drugs
    • interactions are usually slow to develop so chronic use drugs increase that risk
78
Q

Clinical Significance

A
  1. level goes from sub-therapeutic to therapeutic, could be clinically sig in a good way
  2. level goes from low therapeutic to mid therapeutic, probably not clinically sig
  3. level goes from low therapeutic to toxic, clinically sig, bad

*therapeutic range based on averages of thousands, so a particular pt may need “toxic” levels to be therapeutic, etc.

79
Q

Points of Caution in Assessing Patient Risk

A
  • over/under-estimation of clinical importance based on personal clinical experience
    • ex 1/10,000 rxn seen, withold proper tx for 9,999
    • ex clinician who says ‘I use those drugs together all the time’
  • clinical outcomes are highly situational
80
Q

Predicting Clinical Relevance

A
  • wide therapeutic range object, small change caused by precipitant
    • unconcerned
  • narrow range object, small change
    • medium caution
  • wide range, big change
    • more caution
  • narrow range, big change
    • worst case
81
Q

Absorption Interactions

A
  • primary site of abs is small intestine, but interactions can occur anywhere in the bowel
  • result of interaction
  1. changes in extent of abs
  2. changes in rate of abs
82
Q

Mechanisms of Altered Absorption

A
  • complexation
  • pH changes
  • GI motility changes
  • altered drug transport
  • enzymatic metabolism
83
Q

Complexation

A
  • drugs that form chemical complexes with other agents may lower the rate and extent of absorption - keeps obj drug from abs
  • Bile acid resins
    • Cholestyramine
    • Colestipol
  • divalent and trivalent metal ions
    • Mg, Ca, Zn, Fe, Al - ex Ca decr tetracycline abs
    • in many antacids and multivitamins
  • Give at different times could solve problem
84
Q

Changes in pH

A
  • Drugs that change gastric pH
    • H2 R blockers - cimetidine, ranitidine
    • PPI’s - omeprazole, lansoprazole
    • Antacids
  • Drugs that need acid pH for dissolution
    • ketoconazole, itraconazole
      • AID’s pt on ketoconazole for fungal infection starts taking antacid and ends up dying
    • Fe suppliments
85
Q

Changes in GI motility

A
  • Drugs that slow GI motility
    • narcotics
    • anticholinergics - antihistamines, tricyclic antidepressants, phenothiazines
  • Drugs that speed up GI motility
    • laxatives
    • metoclopramide
    • erythromycin
  • More time in gut may mean more destroyed by bact, so not nec more absorbed d/t time
  • One predictable example: less time in gut for time released=less absorption
86
Q

Altered Drug Transport

A
  • Transport systems in gut wall can be influenced
  • not practical… yet
87
Q

Enzymatic Metabolism

A
  • contribute to drug metabolism and the first pass effect
  • highest concentration in duodenum
  • effect metabolism moreso than absorption
88
Q

MEC

A
  • min eff conc

Pharm (7 decks)

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