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Non-Barb Induction Agents Flashcards

1
Q

At room temp what is the solubility of Propofol?

A

Highly lipid soluble, oil @ room temp

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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)
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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.
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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%

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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

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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

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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).

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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.
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9
Q

Propofol: Rena/hepatic & GI EFFECTS

A
  • Green urine (phenols); cloudy urine

- Treats PONV

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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)

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11
Q

Does propofol cross the placenta?

A

YES, & rapidly removed from fetal circulation

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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
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13
Q

DOA & E1/2t of Propofol

A

DOA: 10-15 min

E1/2t: 0.5-1.5 hr

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14
Q

Derivative for Ketamine

A

Phencyclidine derivative (PCP)

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15
Q

Detamine Solubility

A
  • H2O soluble in solution

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

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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).
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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!

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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.
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19
Q

Ketamine Vd & PB

A

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

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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

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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.

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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
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23
Q

Ketamine: MUSCLE EFFECTS

A

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

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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.

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25
Although ketamine antagonizes muscarinic receptors what symptoms occur that are not anticholinergic?
Salivation & Lacrimation
26
Describe emergence reactions. | **What inc & dec incidence
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.
27
Ketamine CI
- Allergy - ↑IOP and ICP (open eye injury) - CAD (as sole anesthetic) - Vascular aneurysm - Uncontrolled systemic or pulm HTN - Psychiatric dz.
28
Ketamine DOSES Sedation Induction Infusion
Sedation: 0.2-0.5mg/kg IV Induction: 0.5-2mg/kg IV Infusion: 1-2mg/kg/min
29
Ketamine DOA & E1/2t
DOA: 10-15min | E1/2t: 2-3hrs
30
Etomidate Derivative
Carboxylated imidazole derivative
31
Etomidate pharmakokinetics: Redistribution Vd PB
Redistribution = Rapid from brain to other tissues Vd =Large 2.5-4.5 L/kg PB = Highly 75%
32
Etomidate: CNS EFFECTS
(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
Etomidate: CV EFFECTS
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
Etomidate: RESP EFFECTS
↓CO2 response (minimally). | Hiccups or coughing.
35
Etomidate: GI EFFECTS
High incidence of N/V (30-40%)
36
Etomidate: MUSCLE EFFECTS
Myoclonus (30-60% due to disinhibition of extrapyramidal system) **Potentiates NMB!! (opposite of proposal)
37
Etomidate solubility
H2O soluble in solution (Propylene glycol solvent; pH 6.9) & @ physio pH, becomes lipid soluble. Pain at IV site (propylene glycol; 80%). Thrombophebitis.
38
Etomidate Excretion
* 85% Renal * 13% Biliary * 2% unchanged
39
Does Etomidate have histamine release? analgesic properties?
NO
40
Etomidate CI
Allergy | Seizure Hx
41
Etomidate DOA & E1/2t
``` DOA = 5-15min E1/2t = 3-5hrs ```
42
Etomidate DOSES Induction Sedation Infusion
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
Etomidate is a great drug for what types of patients?
Great drug for CV disease pts!! Cardiac, aneurysms, IC HTN, RAD (NO histamine release), trauma
44
Propofol DOSES Induction Sedation Infusion Maintenance
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
Dexmedetomidine (precedex) MOA/Class
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
Precedex: Solubility & PB
Water soluble | 90% PB
47
Precedex antagonist
Atipamezole
48
Precedex Metabolism & Excretion
``` Metabolism: Rapid • Conjugation • N-methylation • Hydroxylation Excretion: Metabolites cleared in urine & bile ```
49
Precedex: CNS EFFECTS
* ↓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
Precedex: CV EFFECTS
↓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
Precedex: RESP EFFECTS
* Minimal change in RR, moderate↓ in TV * No change CO2 responsiveness * Upper airway obstruction possible
52
Precedex DOSES | Adjunct to GA & TIVA
- 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
Precedex E1/2t
2-3 hrs
54
Fospropofol structure
* 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
Fospropofol Advantages & Disadvantages
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
Fospropofol Metabolism
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
Fospropofol compared to proposal
o More potent | o Higher VD
58
Which drug reduces BP the most (even more than TPL)?
Propofol
59
Which non-barb also has analgesic activity (only one in its class)?
Ketamine
60
Which non-barb is most useful in CV population?
Etomidate = CV stable due to lack of effect on SNS & baroreceptors. Drug of choice for severe CV disease.
61
Which non-barb increases N/V? | Which non-barb treats N/V?
Etomidate = Causes N/V Propofol = Treats N/V
62
Which drug affects the conversion of cholesterol to cortisol? (therefore decreasing cortisol production)
Etomidate
63
Which non-barb potentiates NMB? Which don't potentiate NMB?
Etomidate potentiate NMB | Propofol does NOT potentiate NMB
64
Which non-barbs are cerebroprotective?
Propofol *Etomidate also decreases CBF, ICP, CRMO2 BUT has increase EEG activity in epileptic foci = CI in seizures
65
Which non-barb increases HR?
Ketamine only = INCREASES HR due to SNS activity * Etomidate & propofol = non change * Precedex = decrease
66
Which non-barb causes bronchodilation & is good in asthma patients?
Ketamine (Propofol naturally produces bronchodilation but due to preservatives also causes bronchospasm therefore not used in asthmatics/COPD)
67
Which non-barb has the longest E1/2t? Shortest?
``` Etomidate = 3-5hrs LONGEST Propofol = 2-3hrs Precedex = 2-3 hrs Propofol = 0.5-1.5hrs SHORTEST ```
68
Which non-barb crosses the BBB?
All of them!
69
Which non-barb causes direct myocardial depression?
Ketamine & Propofol Etomidate & precedex = minimal
70
Which non-barb INCREASES CO? Which DECREASES CO?
``` Ketamine = Increases CO Propofol = Decreases CO ``` *No change in Etomidate or Precedex
71
Which non-barbs have a high hepatic extraction ratio (therefore perfusion dependent elimination)?
Ketamine & Etomidate

Pharm Exam I (4 decks)

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