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Pharmacology > Sedatives/Induction Agents > Flashcards

Sedatives/Induction Agents Flashcards

1
Q

Barbs MOA

A
  • Binds to GABAa (A/B)

- Glu inhibition @ AMPA

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2
Q

Barbs Pharmacokinetics

A
  • Absorption: IV/ Barbies in the butt for kids
  • *displays context sensitivity (infusion dose depends on elimination bc peripheral tissue is saturated)
  • Metabolism by CYP
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3
Q

Barbs Pharmacodynamics

A

CV: ↓BP; tachycardia
Resp: ↓RR Cerebral: constricts cerebral vasculature
↓CBF ↓ICP, ↓oxygen consumption
Histamine release (ex. methohexital)

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4
Q

Barbs Interactions/Contraindications

A
  • Contraindications: acute intermittent porphyria
  • Avoid in hypovolemic pts, beta blocker therapy, CHF , asthma pts
  • Consider dose reduction: interactions w/ opioid, alpha 2 adrenergic agonist, benzos, acute ethanol
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5
Q

Benzos MOA

A
  • increased GABA affinity by binding to GABAa @ alpha 1 and gamma 2
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6
Q

Benzos Pharmacokinetics

A 
A: IV/IM/PO
D:Lipid solubility: M>D>L
Half Life: D>L>M
Duration: L/D>M
-D: large Vd
-L: large affinity to receptor
M: D and M have active metabolites
--D: desmethyldiazepam --> Oxazepam --> CONJUGATION --> Urine excretion
--M: alpha hydroxymidazolam -->CONJUGATION --> Urine excretion
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7
Q

Benzos Pharmacodynamics

A 
CV: some ↓BP, minimal HR (some increase with midazolam)
Resp: some ↓RR 
Thrombophlebitis: D>M>>L
Cerebral: ↓CBF ↓ICP, ↓oxygen consumption
*anterograde amnesia*
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8
Q

Benzos Interactions/Contraindications

A
  • Drugs that induce or inhibit metabolizing CYP P450
  • Opioids + BZ = decrease in SVR (hypotension)
  • Allow decreased MAC
  • Additive sedative and RR depressants
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9
Q

Ketamine MOA

A
  • *inhibit NMDA

* nACh

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10
Q

Ketamine Pharmacokinetics

A

A: IV/IM
D: lipophilic w/ rapid brain uptake
M: hepatic extraction

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11
Q

Ketamine Pharmacodynamics

A 
*CV: increases BP, HR, CO, CBF, ICP 
Resp: ↓RR 
*analgesia
*Hallucinations
*inhibits NE reuptake
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12
Q

Ketamine Interactions/Contraindications

A

Alpha and Beta adrenergic antagonists block the symp response wanted by Ketamine.

Avoid in pts that have catecholamine depletion.

Additive effect: inhaled anesthetics, Propofol, BZ, GABA agents

Contraindications: CAD, HTN

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13
Q

Etomidate MOA

A

Binds to GABAa receptor and increases receptor affinity for GABA

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14
Q

Etomidate Pharmacokinetics

A

A: IV only
D: High protein binding/high lipid solubility (rapid onset)
M: by plasma esterases/hepatic CYP enzymes

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15
Q

Etomidate Pharmacodynamics

A

*CV: minimal to no CV depression
Cerebral perfusion well maintained

Preferred use in pts w/ high risk CV problems

  • -LV impairment
  • -cardiac tamponade
  • -hypovolemia

Respiratory drive maintained unless combined w/ opioids.

Endocrine: Adrenal suppression (inhibits 11-beta hydroxylase)

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16
Q

Etomidate Interactions/Contraindications

A
  • Not used in ICU sedation bc adrenal steroidogenesis (stress response)
  • Used for CV risk or neuro cases ( along with BZ for induction)
17
Q

Propofol MOA

A

-GABAa; likely bind Beta subunit

18
Q

Propofol Pharmacokinetics

A

A: IV only
D: rapid onset/awakening
M: hepatic breakdown and renally cleared

19
Q

Propofol Pharmacodynamics

A
  • decreases cerebral BF/BP/BV/ICP
  • antiemetic/antipruritic prop
  • NO analgesic
  • inhibits baroreceptor responses
20
Q

Propofol Interactions/Contraindications

A
  • Additive w/ BZ and opioids
  • Egg allergy (yolk)
  • smaller induction dose for elderly pts and TIVA
21
Q

Dexmedetomidine Uses

A
  • ICU sedation
  • Alcohol & cocaine with drawl treatment
  • epidural
  • opioid refusal
  • HTN patients
  • Hypotension perferred for surgery
  • Ophthalmic surgery
  • Premed for counter CV effect of Ketamine
  • post op shivers
22
Q

Dexmedetomidine MOA

A

Alpha 2 adrenergic agonist

opioid sparing

23
Q

Dexmedetomidine Pharmacokinetics

A 
A: IV ?
D: 
M: hepatic
E: renal
-Dose reduction in renal and hepatic insufficiency
24
Q

Dex Pharmacodynamics

A

Decrease SVR
Little effect on ventilation
Hypotension (25-50%)
Anxiolysis/Sedation/Analgesia

25
Q

Dex Interactions/Contraindications

A

Caution with vasodilators, cardiac depressants, drugs that decrease heart rate

Can we used prolonged dose? No, potentially cause withdrawal/ rebound hypertension

26
Q

Doxapram MOA

A

Medulla or carotid chemoreceptor stimulation (Stimulates respiration through action on respiratory center medulla or indirectly on peripheral carotid chemoreceptors)

27
Q

Doxapram Pharmacokinetics

28
Q

Doxapram Pharmacodynamics

A
  • CV: Tachycardia, arrhythmia

- Increases TV/RR

29
Q

Doxapram Interactions/Contraindications

A

CNS stim: seizures/muscle fasciculations/spasm

Nausea and vomiting

Avoid: epileptic/ cerebrovascular and CAD/ acute head injuries/ HT/ asthma

Pharmacology (9 decks)

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