2 OMFS Exam 3: Key Terms & Definitions for Oral Sedation

Airway affected

Which of the following is FALSE about minimal sedation:

- A minimally depressed level of consciousness

- Responsive to normally to verbal and tactile stimulation

- Thinking and coordination may be affected

- Airway affected

- Unaffected respiration

- Cardiovascular function are NOT affected

One medications

Which of the following is is TRUE about minimal sedation with oral medication techniques:

- Typically a benzodiazepine plus anti-histamine

- One medications

- Dose: within minimum recommended dose

- Administered during the appointment

maximum

MRD stands for the _____ FDA recommended dose of a drug, printed in FDA approved labeling for unmonitored home use

moderate

The administration of enteral drugs exceeding the maximum recommended dose during a single appointment is considered to be ____ sedation and those guidelines apply

moderate

If more than one enteral drug is administered to achieve the desired sedation effect, with or without the concomitant use of nitrous oxide, the guideline of ________ sedation must apply

unpredictable

Titration of oral medication for the purposes of sedation is _____.

moderate

The administration of enteral drugs exceeding the maximum recommended dose during a single appointment is considered to be moderate sedation and the ______ sedation guidelines apply.

analgesic effect

Which of the following is FALSE about enteral route of administration of drugs:

- cost effective

- no needles

- amnesic effect

- analgesic effect

- inability to titrate to effect

- ineffective (unreliable)

Mildly anxious and apprehensive adult patient that is cooperative and compliant

What type of patients are enteral sedative medications indicated for?

Mild dental anxiety

Enteral sedative medications are contraindicated in all of the following patients, EXCEPT:

- Mild dental anxiety

- Lack of cooperation to take oral medications

- Convinced they wish to be "asleep" for treatment

- Poor past experiences with the oral medication

- Lack of effect (hypo-responders)

- Paradoxical effect

- Allergy to enteral sedative medications

pharmacokinetics

What the body does to the drug:

- absorption

- metabolism

- distribution

- excretion

What 4 factors go into pharmacokinetics:

pharmacodynamics

The effect of the drug on the body:

absorption

The process of a drug from its site of administration to the systemic circulation:

prolong

Any factors that _______ gastric emptying time delays absorption

- Presence of food in stomach

- Fatty food

- Constipation

- Anxiety,fear, pain

- Diabetes

What are 5 factors that delays absorption:

faster

the more lipid soluble a drug is, the _____ it is absorbed

slower

the larger a drug is, the _____ it is absorbed

faster

the more aqueous a drug is, the _____ it is absorbed

drug is metabolized in the liver before entering systemic circulation

How does 1st pass metabolism decrease bioavailability of a drug?

oral medication, intestines, portal vein, liver, hepatic vein, systemic circulation

Describe 1st pass metabolism, the route oral medications take to reach circulation

bioavailability

The fraction absorbed medication into the systemic circulation is the drug's _______

100

Bioavailability = ____% with IV administration of a medication

toxic effects

most serious/life threatening effects of a medication:

adverse effects

unwanted side effects of a medication:

allergic effects

hypersensitivity effects of a medication:

idiosyncratic effects

unusual response (hyperalgesia, dysphoria) to a medication:

paradoxical effects

opposite of intended effect of a medication:

- age

- DDI

- diet

- BMI/liver mass

- medical condition

- gender

- genetics

- race

What are 8 factors that can influence the clinical effects of a medication:

analgesics

Benzodiazepines provide all of the following effects, EXCEPT:

- anxiolysis

- analgesics

- amnesia

- sedation

Benzodiazepines

Most frequently used class of drugs for sedation and anxiolysis in dentistry and medicine:

GABA Receptor Agonist: Enhance the binding of GABA molecules to the GABA receptor facilitating Cl- influx causing cell hyper-polarization = CNS depression

MOA for Benzodiazepines :

anxiolysis

If Benzodiazepines occupy 20% of its binding site as a GABA agonist, you can expect clinical __________ in your patient

sedation

If Benzodiazepines occupy 30-50% of its binding site as a GABA agonist, you can expect clinical __________ in your patient

hypnosis or unconsciousness

If Benzodiazepines occupy >60% of its binding site as a GABA agonist, you can expect clinical __________ in your patient

Myasthenia Gravis

All of the following are indications for the clinical use of Benzodiazepines, EXCEPT:

- Insomnia

- Alcohol withdrawal

- Seizure

- Myasthenia Gravis

- Anxiolysis

- Sedation

- Muscle relaxant

Seizures

All of the following are contraindications for the clinical use of Benzodiazepines, EXCEPT:

- Known allergy

- Myasthenia Gravis

- Severe liver impairment

- Severe respiratory insufficiency

- Sleep apnea syndrome

- Untreated glaucoma

- Pregnancy/nursing mothers

- Seizures

- pediatrics

- elderly

- impaired kidney/liver

- psych. patients taking Anti-depressants Anti-anxiety Pain meds, alcohol, cannabis

What patient populations should you be cautious with the administration of Benzodiazepines:

- Anxiolytic (for mild to moderate anxiety)

- Anti-convulsant activity

- Increase seizure threshold for local anesthetic induced seizure

- Mild muscle relaxing property

- Produce anterograde amnesia

What are the physiologic effects of Benzodiazepines on the CNS:

- Minimal depression when given alone and within the recommended dose

- Depression of respiratory drive at high doses and when combined with other sedatives/opioids

What are the physiologic effects of Benzodiazepines on the Respiratory system:

- COPD

- Sleep Apnea

- Morbidly obese

You should be cautious of the respiratory depressive effects of Benzodiazepines in patients with what conditions:

- Minimal effect on the cardiovascular system

- Ideal for managing anxiety in patient with cardiac history

What are the physiologic effects of Benzodiazepines on the Cardiovascular:

Grapefruit juice

What is a food that is a CYP450 3A4 inhibitor:

Erythromycin

What is an antibiotic that is a CYP450 3A4 inhibitor:

Ketoconazole

What is an antifungal that is a CYP450 3A4 inhibitor:

Fluvoxamine

What is an antidepressant that is a CYP450 3A4 inhibitor:

Verapamil, Diltiazem, Amiodarone

What are 3 anti-arrhythmics that is a CYP450 3A4 inhibitors:

Rifampin

What is an antibiotic that is a CYP450 3A4 inducer:

Phenytoin, Carbamazepine

What are 2 anticonvulsants that is a CYP450 3A4 inducers:

Synergistic Effect

Increased effect of CNS and respiratory depression when used together, Can be potentially result in overdose events

Alcohol, Opioids, IV anesthetics

What are 3 substances that can have a synergistic effect with Benzodiazepines:

pharmacodynamics

Similarity among all types of benzodiazepines are related to its __________

pharmacokinetics

Differences among all types of benzodiazepines are related to its __________

- Triazolam

- Diazepam

- Lorazepam

What are the main 3 Benzodiazepines we use in dentistry?

Diazepam (Valium)

ID the Benzo:

- "Grandfather" of all benzodiazepines

- Long elimination half life (20-80 hours)

- Used for longer dental procedures (2-4 hours)

- Undergo metabolism through hepatic cytochrome P450 3A4 enzyme

- increased Drug drug interaction

- Affected by advanced age, hepatic disease

Lorazepam (Ativan)

ID the Benzo:

- Elimination half life is shorter than diazepam

- Does not undergo hepatic cytochrome P450 enzyme

- Duration of clinical effect is longer than diazepam

- Less lipid soluble slower redistribution away from CNS

- Used for longer dental procedures (3-6 hour)

Triazolam (Halcion)

ID the Benzo:

- Introduced in 1980s for short term treatment of insomnia

- Use for sedation in dental office (off label use)

- NOT FDA approved for sedation in children

- Undergo metabolism through the hepatic P450 system

- Difference from Diazepam: Faster onset Shorter clinical duration of action, Lack of active metabolites, Shorter elimination half life Ideal for short dental procedures

Diazepam (Valium)

Which Benzo is significantly metabolized by the CYP450 3A4 pathway in the liver:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Diazepam (Valium)

Which Benzo has the longest elimination half-life:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Triazolam (Halcion)

Which Benzo has the shortest elimination half-life:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Triazolam (Halcion)

Which Benzo has the shortest onset time:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Lorazepam (Ativan)

Which Benzo has the longest onset time:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Triazolam (Halcion)

Which Benzo has the shortest clinical effect:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Lorazepam (Ativan)

Which Benzo has the longest clinical effect:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Triazolam (Halcion)

Which Benzo has been associated with strong amnesic effect resulting in sleep driving and other complex behaviors (preparing food, making phone calls etc. while not fully awake/aware) even within the theraputic dose:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

Triazolam (Halcion)

Which Benzo can be administered enterally or sublingually -Sublingual dose has 28% greater bioavailability compared to oral:

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

- Midazolam (Versed)

Which Benzo is mainly used for pediatric sedation No pill form, only syrup formulation for oral administration. Onset: 15-30 minutes. Oral form is not commonly used for adults.

- Triazolam (Halcion)

- Diazepam (Valium)

- Lorazepam (Ativan)

- Midazolam (Versed)

- same GABA agonist effect

- sedative, anticonvulsant, and anxiolytic effects

- clinical effects can be reversed by flumazenil

- They all have high lipid solubility: Rapid onset (30 min) Short duration of action (<4 hours)

-

What are the benefits of using non-benzodiazepine hypnotics:

Zolpidem (Ambien)

ID the non-benzodiazepine hypnotic:

- Approved for short term management of insomnia

- Unlike benzodiazepines, muscle relaxation and anti-convulsant effects is only seen at a much higher dose

- Rapid onset (30 minutes)

- Short elimination half life (2.6 hours)

- No active metabolites

- Very little residual next day hang-over effect

Flumazenil (Romazicon)

ID the medication:

- Mechanism of Action: Competitive GABA receptor antagonist - Indication: Reverse the CNS depression effects of benzodiazepines

-- Reverse the paradoxical reaction (aggression, agitation, disorientation, tachycardia, delirium)

- Rapid onset with IV administration: 2-5 minutes

- Short duration of action (30-60 minutes)

- Monitor for signs of re-sedation

- May lower seizure threshold

What precautions do you have to take when administering Flumazenil (Romazicon)?

Medication should be taken with 8oz of water and with food

All of the following are best practices when administering/prescribing oral seditives, EXCEPT:

- Provide written instruction

- Make sure the prescription is marked with the same instruction

- Prescribe only the dose needed for the appointment

- Document instructions and doses prescribed to the patient

- Medication should be taken with 8oz of water and with food

- Remind the patient to not drive and no alcohol use for 12 hours after taking the medication.

- Informed consent must be obtained prior to taking the medication