Lecture 5 Flashcards by David Gorenz

Oral Sedation Advantages

Well accepted
Easy
Cost Effective
Low Adverse Reaction
No needles

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Oral Sedation Disadvantages

Compliance
Latent Period
Erratic
Difficult to titrate
Difficult to alter
Prolonged duration- may need escort home
1st Pass Metabolism

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Enteral Absorption

Oral, Sublingual, Rectal

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Parenteral

IV, IM, IN, inhalation, Transdermal, Transmucosal

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Bioavailability

The fraction of drug that reaches the central circulation

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Proteins that drugs bind to

Most common: Albumin

2nd most common: a-acid glycoprotein

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Where is the drug metabolized?

Most often in LIVER

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CYP 450

Cleaves prodrug into active drug or further metabolizes drug

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Common Ways of Metabolizing Drugs

CYP 450 and Glucoronidation

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Acidic drugs better absorbed in _______ environment, like the _________

acidic; stomach

Basic better metabolize in more basic places like small intestine

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Rationale for oral sedation

Good nights sleep, decrease pre-op anxiety, decrease intraoperative anxiety/pain
NOT for making uncooperative patients cooperative

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Oral agents rules in Ohio

All agents must be administered concomitantly- and can only prescribe ONE dose

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Sublingual Advantages

Enters systemic circulation
Cost
Low adverse rxn
No 1st pass effect

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Sublingual Disadvantages

Cooperation needed
Difficult to titrate
Difficult to alter

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Sublingual

Considered Enteral

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Sublingual Characteristics

Deeper level of sedation
Higher peak plasma levels
Decreased time to sedation

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Examples of Sublingual Meds

Nitroglycerin, Nifedipine, Fentanyl lollipop

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Intranasal

Rapid onset, goes directly into systemic circulation

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IM advantages

Quick onset
Max effect at 30 min
Reliable and predictable
Cooperation not essential

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IM Disadvantages

Not titratable
Not very reversible
Prolonged
Injection--> painful
Injury--> nerve damage
Have to use needle!

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Sites for IM

Gluteal, Ventrogluteal, Vastus Lateralis, Deltoid

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Gluteal IM

Least well perfused
Can cause damage to Sciatic N
Don’t do in little kids!
Do in Gluteus Medius, NOT gluteus maximus

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Deltoid IM

Best perfused, best absorption, holds 4mL

Don’t do in little kids

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Vastus Lateralis IM

Study These Flashcards

Do for kids!!

Holds 15 mL, quicker uptake than Deltoid

IM Complications

``` Nerve damage Periostitis Hematoma Abscess Sloughing of tissue ```

Clark's Rule of Dosing

Weight/150 * Adult dose

Young's Rule of Dosing

Age/Age+12 * Adult dose

Most accurate dosing for children

Age related body surface area as a percent of average adult body surface area

Rectal Advantages

Relatively rapid Less SE's and lower intensity SE's Cost and Ease - higher acceptance Less hepatic 1st pass effect (only 1/3)

Rectal Disadvantages

``` Inconvenient Intestinal irritation Difficult to titrate Difficult to alter Prolonged Duration Erratic- variable absorption ```

Superior vs Middle vs Inferior Rectal veins

Superior enters portal system/Liver via inf mesenteric | Middle and Inferior empty into circulation w/ internal iliac V

Drugs to use with Rectal

Midazolam or Diazepam

IV advantages

``` Rapid onset Highly effective Shorter recovery ABILITY TO REDOSE Ability to reverse Titratable ```

IV disadvantages

``` Venipuncture Inc monitoring Pain from needle Potential catheter injury Most cannot be reversed Pt cooperation ```

Drugs that reverse benzodiazepines

Miloxam and Flumazenil

Benzodiazepines: Site of Action

GABA and how Cl is transferred into cell

Benzodiazepines Physio effects

Reduction of hostile and aggressive behavior, reduces fear, relaxes skeletal muscles, anticonvulsant, sedation, and hypnosis

Contraindications to Benzodiazepines

Allergy to them | Acute Narrow angle glaucoma

Benzodiazepines: Uses

Sedative Anxiolysis Anticonvulsant Amnesia

Benzodiazepines effects on Respiration

Little when used alone and orally Mild when used alone and slowly titrated IV Unconsciousness and loss of airway in high or bolus dose

Benzodiazepines effects on CV

Minimal

Benzodiazepines Adverse Effects

Disinhibition Ataxia Prolonged drowsiness or amnesia

Benzodiazepines drug interactions

Opioids- additive resp depression Other CNS sedatives - barbiturates, antidepressants, clonidine- synnergistic Cimetidine- Inc T1/2 of Diazepam

Half life of Midazolam

1-4 hrs

Half life of Diazepam

Pt's age

Oral Benzo drugs

Diazepam, Midazolam, Flumazenil, Lorazepam

Flow of Benzodiazepines throughout body

Go first (75%) to vessel rich tissues like brain, then (19%) to muscles, then (6%) to far, and finally (1%) to vessel-poor group

Diazepam Characteristics

Dissolved in organic solvent- propylene glycol Sodium Benzoate Burns on injection 5-15 mg for 1 hr appointment

Midazolam

Rapid absorption orally 50% lost to 1st pass effect Slow effect-site equilibration time Short duration of action

Midazolam risk

Greater risk of early respiratory depression

Titrate how much Diazepam or Midazolam

2.5mg Diazepam or 1 mg Midazolam

Diazepam Oral Dosing

2-10 mg tabs for adults | 1-2 mg for children > 6mo

Midazolam Oral Dosing

250-500 mcg/kg (

Lorazepam

For pts w/ impaired liver fxn because does not require hepatic oxidation 0.05 mg/kg IM/IV so

Triazolam

``` Transient anterograde amnesia Cat X May cause higher freq of psychiatric SE's 0.125-0.25 mg orally Long half life ```

Zaleplon

10 mg orally NOT a benzodiazepine Metabolized by Aldehyde Oxidase

Zolpidem

10 mg orally NOT a benzodiazepine Short T1/2, potentiates GABA

Temazapam

For sleeping | 7.5-15mg orally

Lecture 5 Flashcards

(58 cards)