Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm Exam I > Non-Barb Induction Agents > Flashcards

Non-Barb Induction Agents Flashcards

1
Q

At room temp what is the solubility of Propofol?

A

Highly lipid soluble, oil @ room temp

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What preservatives are in Propofol? Why do we care?

A

Sodium metabisulfite & EDTA (ethylenediamine tetraacetic acid) –

  • Na Metabisulfite = BRONCHOSPASMS!!
  • EDTA = inhibits phagocytosis & killing of S.aureus (infection control- single pt use, no more than 6 hrs)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Propofol MOA

A
  • Mimics GABA at the receptor, directly activating chloride channels (B1 subunit), which hyperpolarizes the postsynaptic membrane making it more resistant to excitation.
  • Produces a sedative and hypnotic effect.
  • No analgesia.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Pharmakokinetics of Propofol:

  • Redistribution
  • Vd
  • PB
A

Redistribution = RAPID– rapid awakening w/distribution half life 2-8min

Large Vd = 3.5-4.5 L/kg

Highly PB = 98%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Propofol Metabolism

A
  • Conjugated in liver to water soluble compunds
  • CP450; liver function does not effect rate of metabolism
  • Inactive metabolites

***Clearance exceeds hepatic blood flow = dep on hepatic enzymes instead of BF
2-3 compartment model

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Propofol: CNS EFFECTS

A

↓ IOP, CBF, ICP and CMRO2.
• Cerebroprotective- antioxidant effects resemble Vit E
• EEG burst suppression & decrease in BIS value. Age effects ED95 (highest in toddlers, decreases w/age so elderly must reduce dose)
• Hallucinations, opisthotonos
• ↓CPP due to dec BP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Propofol: CV EFFECTS

A

Dose-dep myocard depression & vasodilation = ↓SV, CO & SVR.

• ↓BP(25-40%; greater than w/STP & TPL), CO. No change in HR (blunted baroreceptor response).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Propofol: RESP EFFECTS

A
  • ↓Vt, variable RR. Bronchodilation in COPD (bronchospasm w/preservatives)
  • Apnea with induction dose.
    • ↓ventilatory response to CO2 & hyoxia
    • ↑Co2 & ↓pH. HPV remains intact.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Propofol: Rena/hepatic & GI EFFECTS

A
  • Green urine (phenols); cloudy urine

- Treats PONV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Propofol: MUSCLE EFFECTS

A
  • Does not potentiate NMB (unlike Etomidate)

- Muscle twitching can occur. (Myoclonus higher than w/TPL but less than w/etomidate & brevital)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Does propofol cross the placenta?

A

YES, & rapidly removed from fetal circulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

CI to propofol

A
  • Allergy (egg, soy).
  • Reduce dose in elderly, hypovolemic, high-risk surgical pt and concomitant use of sedatives and other narcotics.
  • Asthma and COPD
  • Incr ICP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

DOA & E1/2t of Propofol

A

DOA: 10-15 min

E1/2t: 0.5-1.5 hr

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Derivative for Ketamine

A

Phencyclidine derivative (PCP)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Detamine Solubility

A
  • H2O soluble in solution

- @ physio pH, becomes lipid soluble (HIGHLY lipid soluble; more than TPL)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

How is Ketamine prepared?

A
  • Prepared in acidic solution
  • Racemic mixture of equal parts R- & S- enantiomer (S enantiomer more potent analgesic, undergoes faster metabolism & has lower incidence of delirium).
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Ketamine MOA

A

Interacts with the following receptors:

1) NMDA = N-methyl d-asparte; an ionotropic receptor for glutamate; S isomer has high affinity for excitatory NMDA receptor in dorsal horn),
• Non-competitive antagonist at NMDA receptor ion channels.
• Activation of NMDA results in opening of an ion channel which is nonselective to cations allowing Na+ & sm amts of Ca2+ ions INTO & K OUT of the cell.
• Ca++ = play critical role in synaptic plasticicity; cellular mechanism for learning & memory
• NMDA receptors= ligand gated & voltage dep

2) Opiod receptors: Mu (S enantiomer has some mu activity), Delta, Kappa, Sigma,
3) Monoaminergic = involves descending inhibitory pathways for antinociception
4) Muscarinic = antagonist at this receptor; anticholinergic s/sx except inc salivation

5) Ca++ channels
* **NO effect on GABA!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Ketamine Metabolism

A

Extensive via liver CYP-450 (hepatic microsomal enzymes).
- N-demethylation followed by hydroxylation:
• Norketamine (Active metabolite): 20-25% activity of parent compound
• Hydroxylated to hydroxynorketamine

  • First pass effect
  • Changes in liver BF affect clearance (perfusion dependent elim; high extraction ratio).
  • 2 Compartment Model.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Ketamine Vd & PB

A

Vd: Large 3L/kg
PB: poorly 12%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Ketamine: CNS EFFECTS

**Describe onset, max effect & termination effect of Ketamine in CNS

A

↑CBF (potent), ICP, IOP and CRMO2 (can be offset by TPL or diazepam)
• Crosses BBB (unlike glyco); Depresses neuronal function in association areas of cerebral cortex & thalamus while stimulating the hippocampus (limbic)
• Dose related depression of LOC.
• “Dissociative state” (Amnesia NOT as prominent as benzos)
•Nystagmus, Pupil dilation

• Onset 30sec→ Max effect 1min→ Termination of effect is RAPID after single bolus (15min) due to redistribution

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Ketamine: CV EFFECTS

A

↑SNS, HR, BP, CO, myocard work and O2 consumption. Direct myocardial depressant in catecholamine depleted pt (shock)
• Inhibits reuptake of NE
• Sympathomimetic-NMDA effect is NOT a peripheral effect. Probably occurs bc of NMDA receptor activity in nucleus tractus solitarius.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Ketamine: RESP EFFECTS

A

MINIMAL:

  • Bronchodilator (result of SNS activity).
  • CO2 response unchanged. ↑ PVR.
  • Induction dose can cause transient apnea.
  • Accumulation of excess secretions/saliva can contribute to the risk of laryngospasm
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Ketamine: MUSCLE EFFECTS

A

↑ skeletal muscle tone, non-purposeful movements, myoclonic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Describe the dissociative state that happens when giving Ketamine.

A

Depression of association areas functionally “dissociates” thalamus (relays sensory input from RAS to cortex) from the Limbic System (awareness of sensation).

Produces a cataleptic, functionally disorganized state. Appears csc., eyes open with slow nystagmic gaze but does not process info.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Although ketamine antagonizes muscarinic receptors what symptoms occur that are not anticholinergic?

A

Salivation & Lacrimation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Describe emergence reactions.

**What inc & dec incidence

A

Dreaming, out of body sense of floating, excitement, illusions, euphoria, fear (relatively common 10-30%)

  • ↑ = more common in females, higher doses attribute to incidence
  • ↓ = least common in peds; Bnzs most effective at decreasing the incidence.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Ketamine CI

A
  • Allergy
  • ↑IOP and ICP (open eye injury)
  • CAD (as sole anesthetic)
  • Vascular aneurysm
  • Uncontrolled systemic or pulm HTN
  • Psychiatric dz.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Ketamine DOSES

Sedation
Induction
Infusion

A

Sedation: 0.2-0.5mg/kg IV

Induction: 0.5-2mg/kg IV

Infusion: 1-2mg/kg/min

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Ketamine DOA & E1/2t

A

DOA: 10-15min

E1/2t: 2-3hrs

30
Q

Etomidate Derivative

A

Carboxylated imidazole derivative

31
Q

Etomidate pharmakokinetics:
Redistribution
Vd
PB

A

Redistribution = Rapid from brain to other tissues

Vd =Large 2.5-4.5 L/kg

PB = Highly 75%

32
Q

Etomidate: CNS EFFECTS

A

(Direct cerebrovasoconstriction) ↓CBF, ICP, IOP and CRMO2.
• Rapid loss of consciousness after single dose. No analgesia.
• Increases EEG activity in epileptogenic foci, has rare association with Grand Mal Sz and produces myoclonic movement

33
Q

Etomidate: CV EFFECTS

A

MINIMAL effects on CV function due to lack of effect on SNS & baroreceptors
• NO CHANGE: HR, ABP, PAP, CO, SVR, PVR *what sets this drug apart

34
Q

Etomidate: RESP EFFECTS

A

↓CO2 response (minimally).

Hiccups or coughing.

35
Q

Etomidate: GI EFFECTS

A

High incidence of N/V (30-40%)

36
Q

Etomidate: MUSCLE EFFECTS

A

Myoclonus (30-60% due to disinhibition of extrapyramidal system)
**Potentiates NMB!! (opposite of proposal)

37
Q

Etomidate solubility

A

H2O soluble in solution (Propylene glycol solvent; pH 6.9) & @ physio pH, becomes lipid soluble.

Pain at IV site (propylene glycol; 80%). Thrombophebitis.

38
Q

Etomidate Excretion

A
  • 85% Renal
  • 13% Biliary
  • 2% unchanged
39
Q

Does Etomidate have histamine release? analgesic properties?

A

NO

40
Q

Etomidate CI

A

Allergy

Seizure Hx

41
Q

Etomidate DOA & E1/2t

A 
DOA = 5-15min
E1/2t = 3-5hrs
42
Q

Etomidate DOSES
Induction
Sedation
Infusion

A

Induction = 0.2 - 0.6 mg/kg IV (0.3 mg/kg)

Sedation = 5 - 8 mcg/kg/min

Infusion = 10 mcg/kg/min with N2O & opiods
Rectal 6.5 mg/kg has been used in Peds

43
Q

Etomidate is a great drug for what types of patients?

A

Great drug for CV disease pts!! Cardiac, aneurysms, IC HTN, RAD (NO histamine release), trauma

44
Q

Propofol DOSES
Induction
Sedation Infusion
Maintenance

A

Induction = 1 - 2.5 mg/kg IV (APNEA)
*As high as 3mg/kg in toddlers due to pharmacokinetic dif

Sedation Infusion = 20 -100 mcg/kg/min
*Bolus doses of 10-20mg may be used for sedation-infusion better technique.

Maintenance = 100-300mcg/kg/min

45
Q

Dexmedetomidine (precedex) MOA/Class

A

Selective Alpha-2 adrenergic agonist
(1620:1 alpha 2: alpha 1)
(7-10x more selective for alpha 2 w/shorter DOA compared to clonidine)

46
Q

Precedex: Solubility & PB

A

Water soluble

90% PB

47
Q

Precedex antagonist

A

Atipamezole

48
Q

Precedex Metabolism & Excretion

A 
Metabolism: Rapid 
•	Conjugation
•	N-methylation
•	Hydroxylation
Excretion: Metabolites cleared in urine & bile
49
Q

Precedex: CNS EFFECTS

A
  • ↓CBF without changing ICP or CMRO2 significantly
  • ↓MAC of volatile agents and opioid requirement
  • Depresses thermoregulation (hypothermia, depresses shivering)
  • Can build tolerance and dependence.
50
Q

Precedex: CV EFFECTS

A

↓HR,SVR,BP
• Bolus can cause transient ↑BP, ↓HR
• Potential for severe bradycardia, heart block, systole
• Attenuates CV responses to noxious stimuli - decreases catecholamine levels during GA

51
Q

Precedex: RESP EFFECTS

A
  • Minimal change in RR, moderate↓ in TV
  • No change CO2 responsiveness
  • Upper airway obstruction possible
52
Q

Precedex DOSES

Adjunct to GA & TIVA

A
  • Adjunct to GA: 1mcg/kg bolus over 10-15 minutes followed by 0.2- 1 mcg/kg/hr infusion
  • TIVA: 1mcg/kg loading dose
    followed by 5-10mcg/kg/hr
53
Q

Precedex E1/2t

A

2-3 hrs

54
Q

Fospropofol structure

A
  • H2O soluble prodrug of propofol (eliminates the need for lipid formulation- responsible for the risk of pain on injection, infection, hypertriglycerides, PE etc)
  • Hydrolized after injection to propofol via endothelial cell alkaline phosphatases
55
Q

Fospropofol Advantages & Disadvantages

A

ADVANTAGES:
o Avoiding lipid formulation related complications
o If using low doses less episodes of apnea (slower onset of peak effect)

DISADVANTAGES:
o Slower peak effect, longer duration; may be more difficult to titrate
o Short period of tachycardia
o Transient paresthesias and pruritis
o Patients appear to differ in their individual reactions to a standard dose

56
Q

Fospropofol Metabolism

A

Non-linear metabolism to active drug:
o The higher the dose = the more hydrolyzed
o The lower the dose = the less hydrolyzed (less of the active metabolite propofol released)

57
Q

Fospropofol compared to proposal

A

o More potent

o Higher VD

58
Q

Which drug reduces BP the most (even more than TPL)?

A

Propofol

59
Q

Which non-barb also has analgesic activity (only one in its class)?

A

Ketamine

60
Q

Which non-barb is most useful in CV population?

A

Etomidate = CV stable due to lack of effect on SNS & baroreceptors. Drug of choice for severe CV disease.

61
Q

Which non-barb increases N/V?

Which non-barb treats N/V?

A

Etomidate = Causes N/V

Propofol = Treats N/V

62
Q

Which drug affects the conversion of cholesterol to cortisol? (therefore decreasing cortisol production)

A

Etomidate

63
Q

Which non-barb potentiates NMB? Which don’t potentiate NMB?

A

Etomidate potentiate NMB

Propofol does NOT potentiate NMB

64
Q

Which non-barbs are cerebroprotective?

A

Propofol

*Etomidate also decreases CBF, ICP, CRMO2 BUT has increase EEG activity in epileptic foci = CI in seizures

65
Q

Which non-barb increases HR?

A

Ketamine only = INCREASES HR due to SNS activity

  • Etomidate & propofol = non change
  • Precedex = decrease
66
Q

Which non-barb causes bronchodilation & is good in asthma patients?

A

Ketamine

(Propofol naturally produces bronchodilation but due to preservatives also causes bronchospasm therefore not used in asthmatics/COPD)

67
Q

Which non-barb has the longest E1/2t? Shortest?

A 
Etomidate = 3-5hrs LONGEST 
Propofol = 2-3hrs
Precedex = 2-3 hrs
Propofol = 0.5-1.5hrs SHORTEST
68
Q

Which non-barb crosses the BBB?

A

All of them!

69
Q

Which non-barb causes direct myocardial depression?

A

Ketamine & Propofol

Etomidate & precedex = minimal

70
Q

Which non-barb INCREASES CO? Which DECREASES CO?

A 
Ketamine = Increases CO
Propofol = Decreases CO

*No change in Etomidate or Precedex

71
Q

Which non-barbs have a high hepatic extraction ratio (therefore perfusion dependent elimination)?

A

Ketamine & Etomidate

Pharm Exam I (4 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions