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NEUROSCIENCE OF PAIN > LECTURE 5 > Flashcards

LECTURE 5 Flashcards

1
Q

PHARMACODYNAMICS

A

WHAT DRUG IS DOING W/IN FUNCTIONAL SYSTEM

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2
Q

PHARMACOKINETICS

A

HOW DRUG GETS METABOLIZED W/IN SYSTEM

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3
Q

PHARMACOLOGY

A

STUDY OF PRECISE CONTROL OF BIOLOGICAL FUNCTIONS OF EXOGENOUS APPLICATIONS OF CHEMICALS
CENTRAL PRINCIPLE - FUNCTIONAL RELATIONSHIP BETWEEN DRUG CONCENTRATION AND BIOLOGICAL RESPONSE = THE DOSE RESPONSE FUNCTION

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4
Q

LIGAND

A

BINDS TO A BIOMOLECULE (I.E. PROTEIN RECEPTOR/CHANNEL)

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5
Q

BIOMOLECULE

A

LIPIDS, CARBOHYDRATES, PROTEINS, NUCLEIC ACIDS (RECEPTORS - BIOMOLECULES THAT INITIATE A BIOLOGICAL FUNCTION WHEN A LIGAND BINDS TO IT)

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6
Q

AGONIST

A

(TYPE OF LIGAND) STIMULATES A BIOLOGICAL RESPONSE (CAN BE INHIBITORY OR EXCITATORY)

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7
Q

4 MAJOR CATEGORIES OF PROTEIN RECEPTORS

A
  1. ) CELL-SURFACE RECEPTORS
  2. ) TRANSPORTERS AND PUMPS
  3. ) ENZYMES - CAN INHIBIT OR PROMOTE
  4. ) KINASES - REGULATE ACTIVITY OF OTHER PROTEINS IN THE CELL
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8
Q

CELL-SURFACE RECEPTORS

A

(GPCRs, ION CHANNELS) TRANSLATE INFO ON OUTSIDE OF CELL TO BIOLOGICAL MEANINGFUL RESPONSE ON THE INSIDE

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9
Q

TRANSPORTERS AND PUMPS

A

MOVE IONS/MOLECULES ACROSS MEMBRANES (EFFLUX PUMPS)

*PARTICIPATE IN MAINTAINING THE CHEMICAL GRADIENT AND REUPTAKE NEUROTRANSMITTERS IN CLEFT BACK INTO THE CELL

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10
Q

ENZYMES

A

CONVERT STARTING MATERIAL INTO NEW USABLE PRODUCTS

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11
Q

KINASES

A

REGULATE ACTIVITY OF OTHER PROTEINS THROUGHOUT CELL BY PHOSPHORYLATION (REMOVE PHOSPHATE FROM ATP AND RE-LIGATING IT TO A PROTEIN IN NEED)

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12
Q

AFFINITY

A

ABILITY OF A DRUG TO GET TO A RECEPTOR
AT EQUILIBRIUM (BINDS AND DISASSOCIATES), A SPECIFIC AMOUNT OF DRUG WILL OCCUPY A FIXED PERCENTAGE OF RECEPTORS AT ANY GIVEN MOMENT IN TIME
DRUGS THAT ENGAGE W/ A RECEPTOR FOR > PERIODS OF TIME => > AFFINITY
BASED ON THE 3D STRUCTURE OF MOLECULE AND ITS ABILITY TO BIND TO THE ENZYME/RECEPTOR
(Kd) - DRUG CONCENTRATION AT WHICH 50% OF RECEPTORS ARE OCCUPIED
K2/K1 = Kd (RATE OF DISSOCIATION/RATE OF ASSOCIATION)
DRIVES PHARMACOLOGICAL ACTION - IF DRUG CAN’T GET TO RECEPTOR NOTHING WILL HAPPEN

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13
Q

AGONIST

A

BIND TO RECEPTORS VIA A WEAK, REVERSIBLE BOND (A + R –> AR –> EFFECT)
EFFICACY -
EFFECT IS COMPLETELY RELATED TO DOSE
RESPONSE TO AGONIST IS NOT ALWAYS LINEARLY PROPORTIONAL TO THE NUMBER OF RECEPTORS OCCUPIED

BOTH EFFICACY AND AFFINITY ARE BASED ON 3D STRUCTURE

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14
Q

EFFECT RESPONSE

A

SUPERAGONIST/HIGH EFFICACY AGONIST (FEW RECEPTORS OCCUPIED => FULL EFFECT) > PARTIAL AGONIST (100% RECEPTORS OCCUPIED) > ANTAGONISTS (NO INTRINSIC EFFICACY)

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15
Q

ANTAGONISTS

A

BLOCK RECEPTORS TO PREVENT AGONSTS FROM BINDING
PRODUCE NO EFFECT
BLOCK ACTION OF AGONIST - ONLY HAVE TO BLOCK/ALTER OPENING TO FUNCTION
DOSE RELATED EFFECTS
ANTAGONISTS ARE EITHER COMPETITIVE OR NON-COMPETITIVE
BIND VIA WEAK, REVERSIBLE CHEMICAL BONDS

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16
Q

EC50

A

EFFECTIVE DRUG CONCENTRATION AT 50% EFFECTIVE = USED TO COMPARE POTENCY
AFFINITY OF PARTIAL AGONIST/FULL AGONIST = SAME; HOWEVER, EFFICACY IS DIFFERENT
HIGH POTENCY = HIGH EFFICACY

17
Q

NON-COMPETITIVE ANTAGONIST

A

BIND TO ALTERNATIVE SITE ON RECEPTORS WHICH CHANGES THE 3D SHAPE OF AGONST-BINDING SITE
DIFFERENT PHARMACOLOGICAL RESPONSE THAN COMPETITIVE ANTAGONIST
FULL EFFECT OF AGONIST IS NOT ACHIEVED
AGONIST CONCENTRATION DOES NOT MATTER B/C IT IS NOT COMPETING W/ THE SAME SITE
CAN’T COMPARE THE EC50 OF AGONIST

18
Q

COMPETITIVE ANTAGONIST

A

BIND TO THE SAME SITE AS AGONIST

19
Q

IC50

A

WHAT CONCENTRATION OF ANTAGONIST => 50% BLOCKADE

20
Q

PHARMACOKINETICS (ADME)

A

ABSORPTION - ACHIEVING SIGNIFICANT BLOOD CONCENTRATION OF A DRUG W/ A SPECIFIC ADMINISTRATION
DISTRIBUTION - GETTING DRUG TO THE TARGET
METABOLISM - PROCESSING OF THE DRUG ONCE IN THE BODY
ELIMINATION - GETTING RID OF THE DRUG
DRUG CONCENTRATION AT TARGET DETERMINED BY THESE FACTORS

21
Q

GRAPHING DRUG CONCENTRATION TO TIME

A

INCREASED DOSE TO CMAX = ABSORPTION
TMAX = TIME REQUIRED TO REACH MAX BLOOD CONCENTRATION FOR A SPECIFIC DOSE
CMAX = MAX BLOOD CONCENTRATION FOR A SPECIFIC DOSE
T1/2 = HALF LIFE OF A DRUG - IMPORTANT FOR DOSING A DRUG TO MAKE SURE THAT THE BODY ISN’T COMPLETELY DEPLETED OF A DRUG

ADME HELPS W/ DOSING

22
Q

BIOAVAILABILITY

A

AMOUNT OF A DRUG AVAILABLE FOR THERAPEUTIC ACTIVITY
IV = 100% > INTRAMUSCULAR > SUBCUTANEOUS > INHALATION > TRANSDERMAL > RECTAL (PARTIALLY BYPASSES 1ST PASS EFFECT (AS DOES IV ADMIN.)) > SUBLINGUAL > SPINAL/BRAIN > ORAL
IM/SC DELIVERY REQUIRES A LIPOPHILIC DRUG => LONG ONSET

IV = 100% JUST MEANS THAT 100% OF THE DRUG IS IN THE BLOOD DOESN’T MEAN AMOUNT AVAILABLE FOR ACTION

23
Q

ORAL ADMINISTRATION

A

ORAL = SUBJECT TO 1ST PASS EFFECT WHERE MOST DRUGS GET ABSORBED IN THE STOMACH/SM. INTESTINE

  • WHATEVER IS ABSORBED HERE –> LIVER => METABOLIZED DRUGS
  • METABOLIZED IN THE LIVER OR LUNGS (CYTOCHROME P450) => MORE HYDROPHILIC METABOLITE (FAVORS EXCRETION)
24
Q

TRANSDERMAL ADMINISTRATION

A

TD = GOOD FOR PPL W/ GI ISSUES (DRUG PERMEATES SC LAYER)

25
Q

LIVER METABOLISM

A

50% OF ALL DRUGS METABOLIZED BY CYP-3A (DRUG COMBINATIONS CAN EXCITE OR INHIBIT CYP-3A ACTIVITY)
SMOKING INHIBITS CYP-3A ENZYMATIC ABILITY - DOSE OF DRUG DECREASES
DRUG:DRUG INTERACTIONS

26
Q

FACTORS THAT MODIFY DRUG METABOLISM

A

GENETIC POLYMORPHISM
DOSE OVERLOAD OF ENZYME CAPACITY
AGE - ENZYME MAKEUP - OLD AND YOUNG AT RISK FOR DRUG METABOLISM ISSUES
DISEASE (DOSE-ADJUSTMENT COMMON) - I.E. LIVER DISEASE, RENAL DISEASE
SEX - M/F SEX DIFFERENCES
SMOKING
DIET - VEGANS HAVE LESS ENZYMES

27
Q

SPECIAL PROPERTIES OF A DRUG TO PAY ATTENTION TO:

A
  1. ) TARGET
  2. ) WHAT ENZYMES METABOLIZE IT
  3. ) EXCRETION
28
Q

ENZYME-INDUCED DRUG

A

DRUG:DRUG INTERACTION -
WHEN A DRUG IS ONBOARD, METABOLISM OF WHATEVER IS BEING BROKEN DOWN BY PARTICULAR ENZYME WILL INCREASE (CYP2D6)
ASPIRIN = ENZYME-INDUCED (CAUSES AN INCREASE IN METABOLISM OF THE DRUG IN COMBINATION - GRAPE FRUIT JUICE AS WELL)
INCREASED METABOLISM => DECREASED EFFICACY/POTENCY

29
Q

ENZYME-INHIBITING DRUG

A

DRUG:DRUG INTERACTION -
WHEN A DRUG IS ONBOARD, METABOLISM OF WHATEVER IS BEING BROKEN DOWN BY PARTICULAR ENZYMES WILL DECREASE (CYP2D6)
INCREASED POTENCY AND POSSIBILITY OF OVERDOSING

30
Q

POLYMORPHISMS IN LIVER

A

CAUSE DIFFERENTIATION BETWEEN PEOPLE AND THEIR METABOLISM OF THE SAME DRUG (PHARMACOGENOMICS)
PERSON:DRUG INTERACTIONS
RAPID METABOLIZERS - DECREASED DRUG POTENCY/EFFICACY
SLOW METABOLIZERS - INCREASED DRUG POTENCY/EFFICACY (CAUSES TOXICITY)

31
Q

DOSE RESPONSE CURVE

A 
CONCENTRATION = EXOGENEOUS FLUID (MG/ML)
DOSE = EXOGENEOUS FLUID ADMINISTERED TO A PATIENT (MGML^-1KG^-1)

SHOWS EFFICACY AND AFFINITY
AFFINITY AND POTENCY ARE VERY CLOSELY RELATED
COMPARE DRUGS @ EC50
W/ ADDED ANTAGONIST, AGONIST CURVE WILL SHOW PARALLEL SHIFTS TO THE RIGHT (COMPETITIVE - DOESN’T MATTER FOR NON-COMPETITIVE) - CAN OVERWHELM ANTAGONIST W/ HIGHER CONCENTRATIONS OF AGONIST
W/NON-COMPETITIVE ANTAGONIST - SHIFT = TO THE RIGHT AND DOWN B/C AGONIST CAN NEVER GET TO FULL EFFECT B/C IT CAN’T BIND

32
Q

NON-SURMOUNTABLE ANTAGONIST

A

BINDS JUST LIKE THE COMPETITIVE ANTAGONIST AND DOESN’T DISASSOCIATE - SEE THE SAME PATTERN OF ANTAGONISM AS A NON-COMPETITIVE ANTAGONIST

33
Q

PORTAL SYSTEM

A

UPPER 1/3 OF INTESTINE SYSTEM THAT ABSORBS THE MEDICINE TO THE LIVER

SOME METABOLISM OCCURS IN LUNGS AS WELL

34
Q

METABOLITES

A

WHEN METABOLIZED - PARENT DRUG BREAKS DOWN INTO METABOLITES
LESS POTENT B/C THEY ARE MORE HYDROPHILIC AND THIS PROMOTES EXCRETION
THEY ARE LESS ACTIVE THAN PARENT DRUG - EXCEPT PRO-DRUGS

NEUROSCIENCE OF PAIN (8 decks)

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