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PHARM EXAM 1 > OXID/RED TO MECH. OF ANESTHESIA > Flashcards

OXID/RED TO MECH. OF ANESTHESIA Flashcards

1
Q

OXIDATION-REDUCTION PROCESS

A

AN ELECTRON DONOR (FROM NAD-COENZYME FORMED FROM NIACIN) AND MOLECULE O2 FOR ACTIVITY
THE O2 IS SPLIT WITH ONE ATOM OXIDIZING A MOLECULE OF DRUG AND THE OTHER INCORPORATED INTO H2O

LOSS OF ELECTRONS= OXIDATION

GAIN OF ELECTRONS= REDUCTION

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2
Q

WHAT OCCURS UNDER CONDITIONS OF LOW ppO2?

A

ENZYMES TRANSFERS ELECTRONS TO A SUBSTRATE RATHER THAN TO OXYGEN (INSUFFICIENT AMOUNT OF O2 TO COMPETE FOR ELECTRON).
THIS CAN LEAD TO TOXIC BUILD UP

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3
Q

CONJUGATION

A

INVOLVES CP-450

SUBSTANCES RENDERED INACTIVE AND WATER SOLUBLE THEREFORE AVAILABLE FOR ELIMINATION

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4
Q

HYDOLYSIS

A

INVOLVES NON- MICROSOMAL ENZYMES

HYDROLYSIS OFTEN AT ESTER BOND

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5
Q

NON-MICROSMOAL ENZYMES

A

CATALYZE REACTIONS FOR METABOLISM BY CONJUGATION AND HYDROLYSIS AND TO A LESSER EXTENT OXIDATION AND REDUCTION

MAINLY IN LIVER BUT ALSO PLASMA & GI TRACT

EX. ESTER HYDROLYSIS OF SUCCINYLCHOLINE, REMIFENTANIL, ESTER LOCALS

ENZYME INDUCT DOES NOT OCCUR BUT ACTIVITY IS GENETICALLY DETERMINED

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6
Q

ELIMINATION HALF “LIFE”

A

1ST HALF LIFE- 50% OF THE DRUG IS ELIMINATED FROM THE BODY
2ND HALF LIFE-50% OF THE REMAINING IS ELIMINATED; SO 75% IS TOTALLY REMOVED ALL TOGETHER
4TH HALF LIFE- 93.75% OF THE DRUG IS GONE
(4-5 HALF LIVES EQUAL TOTAL ELIMINATION)

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7
Q

ELIMINATION HALF “TIME”

A

TIME NEEDED FOR THE ELIMINATION OF 50% OF THE DRUG FROM THE PLASMA
A SIGNIFICANT CONCEPT WHEN CONSIDERING TIME OF AWAKENING

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8
Q

CONTEXT SENSITIVE HALF TIME

A

TIME NEEDED FOR PLASMA CONCENTRATION OF THE DRUG TO REACH 50% AFTER DISCONTINUATION OF A CONTINUOUS IV INFUSION

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9
Q

HALF LIFE OF EFFECT

A

INCLUDES ACTIVE METABOLITES EFFECTS

IN THIS WAY THE “HALF-LIFE” CAN DECEIVE YOU SINCE THE EFFECTS MAY OUTLAST THE PARENT COMPOUND SIGNIFICANTLY

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10
Q

RECOVERY TIME

A

TIME REQUIRED FOR THE PLASMA CONCENTRATION TO REACH A LEVEL COMPATIBLE WITH AWAKENING/RECOVERY OF EFFECTS
ELIMINATION AND CONTEXT SENSITIVE HALF TIME ARE REFLECTED IN RECOVERY TIME

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11
Q

ACCUMULATION

A

OCCURS WHENEVER SUBSEQUENT DOSES ARE GIVEN

IF THE DOSING INTERVAL IS SHORTER THAN 4 HALF LIVES ACCUMULATION WILL BE DETECTABLE

RATE OF ACCUMULATION IS INVERSELY PROPORTIONAL TO THAT FRACTION OF DRUG LOST DURING THE DOSING INTERVAL

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12
Q

CLEARANCE

A

IT IS THE VOLUME OF DRUG CLEARED FROM PLASMA BY EXCRETION AND METABOLISM

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13
Q

WHERE DOES METABOLISM OCCUR?

A

IN THE LIVER AS WELL AS OTHE MECHANISMS (HOFFMAN ELIMINATION, ESTER HYDROLYSIS)

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14
Q

WHY IS RATE OF CLEARANCE CRUCIAL?

A

TO DETERMINE INFUSION RATES AND DOSING

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15
Q

WHAT IS THE CLEARANCE (CL) OF A DRUG?

A

THE VOLUME OF PLASMA FROM WHICH THE DRUG IS COMPLETELY REMOVED PER UNIT TIME

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16
Q

WHAT IS ELIMINATION CONSTANT?

A

DETERMINES THE FRACTION OF THE DRUG IN THE BODY ELIMINATED PER UNIT TIME

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17
Q

WHAT IS THE STRATEGY FOR TREATING PATIENTS WITH DRUGS?

A

TO GIVE SUFFICIENT AMOUNTS THAT THE REQUIRED THERAPEUTIC EFFECT OCCURS WITHOUT TOXICITY

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18
Q

WHAT ABOUT MAINTENANCE DOSE?

A

ITS EQUAL TO THE RATE OF ELIMINATION AT STEADY STATE (I.E. AT STEADY STATE, RATE OF ELIMINATION=RATE OF ADMINISTRATION)

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19
Q

DOSING RATE EQUATION

A

CLEARANCE X DESIRED PLASMA CONCENTRATION

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20
Q

LOADING DOSE EQUATION

A

THE VOLUME OF DISTRIBUTION X THE DESIRED CONCENTRATION (I.E. THE CONCENTRATION AT STEADY STATE)

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21
Q

WHAT IS HEPATIC CLEARANCE

A

THE PRODUCT OF HEPATIC BLOOD FLOW AND THE HEPATIC EXTRACTION RATIO OF THE DRUG (A LOW ER= SMALL AMOUT OF DRUG REMOVED)

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22
Q

HOW ARE HIGH ER DRUGS PERFUSED?

A

PERFUSION IS DEPENDENT FOR ELIMINATION

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23
Q

HOW ARE LOW ER DRUGS PERFUSED

A

DEPENDS ON PROTEIN BINDING & ENZYME ACTIVITY (CAPACITY DEPENDENT)

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24
Q

ENZYME INDUCTION IS EQUIVALENT TO….

A

INCREASED HEPATIC CLEARANCE OF DRUGS WITH LOW ER= INCREASED DRUG NEEDED FOR EFFECT

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25
Q

WHAT DOES BILIARY EXCRETION INTO GI TRACT ACCOUNTS FOR WHAT?

A

MANY DRUG METABOLITES

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26
Q

WHAT OCCURS TO SOME OF THE DRUG METABOLITES THAT ARE CAUSED VIA BILIARY EXCRETION INTO GI TRACT?

A

SOME ARE REABSORBED FROM GI AND UNDERGO RENAL CLEARANCE (ENTEROHEPATIC CYCLING)

27
Q

WHICH ORGAN IS MOST IMPORTANT ORGANS FOR ELIMINATION OF DRUGS/METABOLITES?

A

KIDNEYS

28
Q

WHAT DOES RENAL EXCRETION ENTAIL?

A

GLOMERULAR INFILTRATION, ACTIVE TUBULAR SECRETION, PASSIVE TUBULAR REABSORPTION

29
Q

NO ____1___CURRENTLY AVAILABLE CAN PRODUCE ALL RESPONSES THUS COMBINATIONS OF _____2_____ ARE USED TO PRODUCE A BALANCED ANESTHESIA.

A

DRUG

DRUGS

30
Q

WHEN COMBINATION DRUGS REDUCE THE REQUIREMENT FOR INHALED ANESTHETICS WHAT IS MINIMIZED AND WHAT IS INCREASED?

A

MINIMIZED THEIR SIDE EFFECTS

INCREASING THEIR SAFETY

31
Q

WHEN SOME INHALED ANESTHETICS PRODUCE ONE OR MORE RESPONSES REQUIRED FOR GENERAL ANESTHESIA WHAT OCCURS TO THE DOSES OF BARBITURATES, OPIODS, AND NMB AGENTS?

A

THEY CAN BE REDUCED, ALSO INCREASING SAFETY.

32
Q

WHAT TISSUE DOES ALL ANESTHETICS HAVE AN AFFINITY FOR?

ARE ACTIONS IRREVERSIBLE OR REVERSIBLE?

A

NERVOUS TISSUE

REVERSIBLE

33
Q

WHAT ARE ANESTHETICS MOA?

A

ITS NOT WELL UNDERSTOOD BUT INCLUDES INHIBITION FO THE ACTIONS OF EXCITATORY NEUROTRANSMITTERS (ACh & Glutamate)

POTENTIATION OF THE INHIBITOR ACTIONS GABAergic AND GLYCINERGIC NERVES

CHANGES IN MEMBRANE LIPIDS (FLUIDITY-THINK VEG. OIL VS VEG. SHORTENING) THAT ALTER NA+ MOVEMENT ACROSS THE MEMBRANE

INTERACTION AT RECEPTORS

34
Q

IV ANESTHESIA CHARACTERISTICS

A

USED PRIMARILY AS ADJUNCTS TO INHALATION AGENTS AND POSSIBLY AS PRIMARY ANESTHETICS
USED FOR RAPID INDUCTION (BARBITURATES)
PRODUCE AMNESIA (BARBITURATES/BENZODIAZEPINES
CONTROL INTRA-OPERATIVE PAIN (OPIOIDS)
INTRAOPERATIVE NM BLOCKADE

35
Q

LOCAL AND REGIONAL ANESTHESIA CHARACTERISTICS

A

TO RENDER A PORTION OF THE BODY INSENSITIVE TO PAIN BY BLOCKING NERVE CONDUCTION
LAs REDUCE NA+ PERMEABILITY, RAISING THE THRESHOLD FOR ACTION POTENTIAL FIRING

36
Q

PHARMACOKINETCS OF INHALED ANESTHETICS INCLUDES…

A

ABSORPTION- UPTAKE FROM ALVEOLI TO CAPILLARY

DISTRIBUTION- SPREAD FROM CAPILLARY TO ORGAN

METABOLISM- MINIMAL HEPATIC VARIES BY AGENT

ELIMINATION- PRIMARILY BY LUNGS

37
Q

DEFINE UPTAKE.

A

EVENTUALLY THE PARTIAL PRESSURE OF THE GAS EQUILIBRATES BTW LUNGS, BLOOD, AND BRAIN

38
Q

PA MEANS

A

ALVEOLAR PARTIAL PRESSURE

39
Q

Pbr MEANS

A

BRAIN PARTIAL PRESSURE

40
Q

WHAT IS USED TO INFER DEPTH OF ANESTHESIA, RECOVERY FROM ANESTHESIA AND POTENCY COMPARISONS?

A

PA= ALVEOLAR PARTIAL PRESSURE ( AT EQUILIBRATION)

41
Q

WHAT EQUATION DETERMINES PA?

A

DELIVERY - UPTAKE

42
Q

WHAT IS DELIVERY AFFECTED BY?

A

INHALED PARTIAL PRESSURE (PI)
ALVEOLAR VENTILATION
BREATHING SYSTEM
FRC

43
Q

WHAT IS UPTAKE AFFECTED BY?

A

ANESTHESIA SOLUBILITY
CARDIAC OUTPUT
ALVEOLAR TO VENOUS PRESSURE GRADIENT

44
Q

IN REGARDS TO CONCENTRATION EFFECT, INTIAL ADMINISTRATION (INDUCTION) REQUIRES A ______ PI TO OFFSET THE UPTAKE. (HI OR LOW???)

A

HI

45
Q

IN REGARDS TO SECOND GAS EFFECT, WHAT DOES HIGH VOLUME UPTAKE OF 1 GAS DO TO THE PA OF ANOTHER GAS (N2O AND VOLATILE AGENT)?

A

ACCELERATES AN INCREASE

46
Q

AN INCREASE IN THE ALVEOLAR VENTILATION CAUSES THE RATE OF RISE OF PA TO DO WHAT?

A

INCREASE

> ALVEOLAR VENT= >RATE OF RISE OF PA

> ALVEOLAR VENT:FRC RATIO= >RATE OF RISE OF PA

47
Q

WHAT IS PA EFFECTED BY IN REGARDS TO DELIVERY?

A

VOLUME OF SYSTEMS, RUBBER COMPONENTS, GAS FLOW

48
Q

IN RELATIONSHIP TO BLOOD THE GAS COEFFICIENT OF N2O CAN IS HOW MUCH GREATER THAN THAT OF NITROGEN?

A

34 TIMES

MEANS THAT N20 CAN MOVE FROM BLOOD TO A CLOSED SPACE 34X FASTER THAN N CAN LEAVE IT

49
Q

SOLUBILITY IS INDICATED BY???

A

AGENTS PARTITION COEFFICIENT

50
Q

PARTITION COEFFICIENT EQUATION

A

PARTITION COEFFICIENT= DISTRIBUTION RATIO BTW PHASES AT EQUILIBRIUM (=PARTIAL PRESSURES) I.E. BLOOD:GAS, BLOOD:BRAIN, OIL:GAS( LIPID SOLUBILITY)

51
Q

WHAT DOES BLOOD:GAS PARTITION COEFFICIENT OF 0.5 MEANS?

A

THAT CONCENTRATION OF AGENT (MOLECULES) IN BLOOD IS HALF THAT CONCENTRATION IN ALVEOLAR GAS WHEN PRESSURES ARE EQUAL

52
Q

WHAT IS SLOW INDUCTION PROCESS?

A

PULMONARY BLOOD FLOW CARRIES AWAY ANESTHETIC > CARDIAC OUTPUT > RAPID UPTAKE < RATE OF RISE OF PA

53
Q

DOES HIGHLY PERFUSED TISSUES EQUILIBRATE MORE RAPIDLY OR SLOWLY DURING UPTAKE?

A

RAPIDLY

54
Q

WHAT OCCURS TO ANESTHETIC WHEN THERE IS A CONTINUED UPTAKE AFTER VESSEL RICH GROUP SATURATION?

A

THE ANESTHETIC IS ENTERING THE SKELETAL MUSCLE

55
Q

RECOVERY IS A DECREASE OR INCREASE IN Pbr RATE?

A

DECREASE

56
Q

DURING THE RECOVERY STAGE WHAT HAPPEN TO THE RATE OF WASHOUT?

A

IT IS RAPID DUE TO LOW SOLUBILITY IN BRAIN AND HIGH PERCENT OF CO TO BRAIN

57
Q

WHY DOESN’T RECOVERY MIRROR INDUCTION?

A

B/C THERE IS NO 2ND GAS EFFECT AND Pa IN MUSCLE AND FAT WHICH NEVER EQUILIBRATED

58
Q

DIFFUSION HYPOXIA IS A RESULT OF? AND HOW DOES THIS OCCUR?

A

ABRUPT DISCONTINUATION OF N2O

PARTIAL PRESSURE GRADIENTS REVERSE SO THAT N2O LEAVES BLOOD AND ENTERS ALVEOLI RAPIDLY DILUTING PAo2 AND THEREFORE PaO2

ALSO DILUTES PACO2 THEREFORE < STIMULUS TO BREATHE AND FURTHER < PaO2

59
Q

DEFINE MAC?

A

THE INSPIRED CONCENTRATION % AT 1 ATM THAT PREVENTS SKELETAL MUSCLE MOVEMENT IN RESPONSE TO PAINFUL STIMULI (I.E. INCISION) IN 50% OF SUBJECTS

60
Q

WHAT IS MAC EFFECTED BY?

A

VARIOUS PHYSIOLOGIC AND PHARMACOLOGIC FACTORS

61
Q

ARE MAC VALUES ADDITIVE OR SUBTRACTIVE?

A

ADDITIVE

62
Q

HOW IS MAC DESCRIBED IN 30-55 YEAR OLD HEALTHY INDIVIDUALS?

A

AS A PERCENTAGE AT 37 DEGREES AND 1 ATM

63
Q

MECHANISMS OF ANESTHESIA

A

MOA IS UNCERTAIN

LIKELY THE RESULT OF MORE THAN ONE THEORY (MORE THAN ONE SITE OF ACTION)

MOLECULAR CELULAR ACTION (BIND TO PROTEINS)

INTERACTION WITH RECEPTORS ON CELL MEMBRANES

LIGAND GATED CHANNELS LIKELY IMPORTANT SITES

STEREOSELECTIVITY INDICATES DIRECT PROTEIN BINDING EFFECT

POTENTIATION OF INHIBITORY RECEPTORS SUCH AS GAB

MEYER-OVERTON THEORY LESS LIKELY

64
Q

WHAT IS MEYER-OVERTON THEORY?

A

DISRUPTION OF BILIPID LAYER MEMBRANE BY ANESTHETICS

PHARM EXAM 1 (1 decks)

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