Drugs Flashcards
Trade name for Versed
Action List
Midazolam
- make sure we have a bag mask (review emergency response stuff)
- for Ketorolac ask patients if they have any renal issues or if they have ever been told that they can’t take NsAIDS. Also if they are on blood thinners
- order SOCKIT, use 3-4 times per day (but they can use it as much as they want), Gina gets it from “sedationkit.com”
- mylohyoid injection (can be used if the IAN is not providing complete anesthesia)
- ask patients how they respond to benedryl
- when gina is doing a longer case, she will often titrate to effect with Versed then give about 25 mg of benedryl to help keep them sedated
- steroids (dexamethasone, medrol dose pack) suppress the immune system, so not recommended for immune compromised patients (diabetic…)
- we are supposed to have a pharmacutical waste container for extra anesthetic and sedation liquids
- for OSHA you are supposed to have some sort of monthly safety meeting and it has to be documented. It can be a really short, but it has to be done.
- If you use any schedule II drugs (Fentanyl) you are required by the DEA to have a wall mounted cabinet with two keys so no one person can access the drugs
- Check our emergency kit, she keeps a list of the drugs and when they expire, by OSHA standards the kit should be checked every month. She also has the dosages listed and syringes marked so she doesn’t have to actually think about how much of what to give.
- we also are not supposed to reuse the saline bags
Trade name for Halcion
Triazolam
Trade name for Valium
Diazepam
Reversal agent for Benzos
Flumazenil
Flumazenil
benzodiazepine receptor antagonist, used for diagnosis, not true reversal
tramadol brand name
Ultram
tramadol uses and contra indications
treatment of moderate to severe pain
You should not take tramadol if you have used alcohol, sedatives, tranquilizers, or narcotic medications within the past few hours.
Tramadol can slow or stop your breathing
Bioavailability
The degree to which a drug or other substance becomes available to the target tissue after administration
Peak Plasma Concentration
The highest level of drug that occurs in the plasma portion of the blood after administration of the drug
How many Half-lives does it take until a drug is considered to be “eliminated” from the body?
5
Signs of Sedation
Verbal – the pt will actually tell you they are very relaxed if you ask them
• Drifting into relaxation when un-stimulated
– Closing eyes and wanting to sleep when no one is
talking directly to the patient
• Body limbs relaxing – arms falling to side of chair, weight of head bobbing,
• Body temperature – pt will begin to feel cold
• Verrill’s sign–eyelids at“half-mast”,half ptosis
effects of Benzodiazepines
-Anxiolytics (Antianxiety agent)
• Anterograde (from the time of admin) amnesia
• Anticonvulsant
• Muscle relaxing effects
-make sure their airway muscles don’t get too relaxed
• The Sedative of Choice for most General Dental Practitioners
examples of Benzodiazepines (3)
-both names
- diazepam (Valium)
- midazolam (Versed)
- trazolam (Halcion)
Reversal agent of Benzodiazepines (both names)
flumazenil (Romazicon)
ptosis
drooping of the eyelids
Fentanyl
a potent, synthetic opioid pain medication with a rapid onset and short duration of action
Phases 1 of IV administration of Diazepam
Phase 1: 0 to 15 Minutes (do injections during this time)
– During phase 1 of IV conscious sedation with diazepam, the cerebral blood level of diazepam is at its peak and the patient is sedated to the maximum degree.
– The patient remains responsive to verbal and physical stimulation, but response time is increased, speech is slurred, and the patient may have difficulty enunciating words.
– The patient may not appear to be aware of the presence of the doctor or the assistant during this phase.
– Anterograde amnesia, if it is to occur, usually involves procedures occurring at this time.
should you use topical when doing IV sedation?
No
- it’s a waste of time
- it will cause salivation
- decrease the gag reflex increasing risk of laryngospasm(?)
Phases 2 of IV administration of Diazepam
Phase 2: 16 to 30 Minutes
– The Level of sedation is somewhat lessened (the patient becomes more aware of the surroundings than in phase 1; however, he or she is definitely still sedated
– Because the cerebral blood level of diazepam begins to decrease as the drug undergoes redistribution: [α-half- life] to those organs and parts of the body that are less vessel rich than the brain
– Patient response to stimulation (verbal and physical) is more rapid, the slowing of responses in phase 1 having diminished or disappeared.
– Patients can usually recall event occurring during this phase, although in isolated cases amnesia may occur in this phase too.
Phases 3 of IV administration of Diazepam
Phase 3: 31 to 45 Minutes
– During this period the typical patient will state that he or she feels “normal” again; in others words, the feeling of sedation has dissipated.
– It may be tempting to administer additional diazepam to the patient; however, this is normally not necessary.
– Although no longer feeling sedated, the patient is also no longer apprehensive.
– The now decreasing cerebral blood level of diazepam is no longer adequate to maintain the earlier depth of sedation, but it is sufficient to provide an anxiolytic state (similar to the desired actions of oral diazepam).
– With treatment nearing completion and the patient free of pain, there is usually no need for the readministration of diazepam at this time.
Phases 4 of IV administration of Diazepam
Phase 4: 46 to 60 Minutes
– At this time after receiving diazepam, virtually all patients will feel, and in fact look, recovered. This is not a result of the β-half-life of the drug (30+ hours) but because of redistribution: α-half-life
– The blood level of diazepam at 60 minutes after IV administration of 20mg is 0.25 μg/ml.
– The patient is not recovered at this time. Under no circumstances should the doctor ever believe that this patient is capable of operating a car or leaving the dental or surgical office unescorted.
– As redistribution of diazepam continues during this first hour after IV administration, the level of the drug increases in several storage sites: the fat, the walls of the intestines, and the gallbladder.
– Diazepam stored in fat will usually remain there because diazepam is quite lipid soluble and the blood supply of fat is relatively poor.
– This is a significant phenomenon called: The Rebound effect or second-peak effect
The Rebound effect or second-peak effect
It involves a recurrence of symptoms of sedation and drowsiness approximately 1 hour after the first meal taken after the patient leaves the treatment site.
– In most cases this will be about 4 to 6 hours following the start of the procedure.
– After a meal, particularly one rich in lipids, the gallbladder constricts, releasing its contents of bile and un-metabolized diazepam into the small intestine
– Over the next hour or so diazepam is reabsorbed back into the cardiovascular system.
– In some patients the diazepam blood level may reach a level at which clinical signs and symptoms of sedation recur;
– The patient feels quite tired and will want to lie down for a few minutes.
– It becomes absolutely essential, therefore, advise the patient and their escort of the possibility before their discharge.
– The rebound effect is less likely to be observed in a patient whose gallbladder has been removed.
– Because diazepam is extremely lipophilic, it cannot be excreted through the kidneys and therefore must undergo biotransformation in the liver.
Diazepam Onset:
• 1-5 min (IV sedative action)
diazepam duration of action (PO and IV)
- PO (hypnotic action): 7-8hr
* IV (sedative action); 15-60min
half life of diazepam
• 20-70hr (Active metabolite)
-in the body for about 6 days (pump and dump)
pharmacology of diazepam
– Mechanism of Action: Modulates postsynaptic effects of GABA-A transmission,
– resulting in an increase in presynaptic inhibition.
– Appears to act on part of the limbic system, the thalamus, and hypothalamus, to induce a calming effect
metabolism of diazepam
• Metabolism
– Metabolized by hepatic P450 enzymes CYP2C19,
CYP3A4
• Excretion: – Urine
Interactions with Diazepam
– Serious: • Cimetidine • Clarithromycin • St. John’s Wort • Ect. – Significant: • Grapefruit • Ect.
adverse effects of diazepam
1-10% – Ataxia Adverse Effects: – Euphoria – Incoordination – Somnolence – Rash (3%, rectal gel) – Diarrhea (4%, rectal gel) • Frequency Not Defined: – Hypotension – Fatigue – MuscleWeakness – RespiratoryDepression – Neutropenia – Local effects: Pain, swelling, thrombophlebitis, carpel tunnel syndrome, tissue necrosis – Phlebitis if too rapid IV push
Gina’s clinical experience with Diazepam
– Not water soluble and cannot be diluted
– Inconvenient for smaller dosing of patients
– Diazepam causes pain and irritation to the injection site for most patients
Gina’s personal opinions on Diazepam
– Diazepam is not favorable due to the long half life
– There are newer, better, and safer medications
– Dentists who use this on a routine basis have outdated training.
When to consider using diazepam:
- Pre-op sedation (anxiolytic)
- I would recommend this for extremely anxious patients who may not come into your office for their apt without some assistance.
- I personally would prefer alprazolam (Xanax) over diazepam because it has a shorter half life. - If midazolam (Versed) is unobtainable
- Occasionally drugs will be difficult to order due to shortages.
Pre-op Anxiolytic diazepam
2-10mg PO 1 hour prior to dental
appointment.
- Lower spectrum of dosage for patients with no hx of benzodiazepine usage
- Higher spectrum of dosage for patients with 1+ yr hx of benzodiazepine usage
protocol for IV administration of diazepam (valium)
– Administer slowly via IV no more than 5mg/min
– Monitor respiration q5 min and before each IV dose
– Have airway support ready until effects of IV administration are known.
– Titrate to effect
Midazolam
Pharmacology:
– Mechanism of Action:
– Mechanism of Action:
– Effects may be mediated through GABA receptor system
– Binds receptors at several sites within the CNS, including the limbic system and reticular formation;
– Increase in neuronal membrane permeability to chloride ions enhances the inhibitory effects of GABA; the shift in chloride ions causes hyperpolarization = (less excitability) and stabilization of the neuronal membrane
GABA receptor
- GABA & glycine are believed to be the major inhibitory neurotransmitters in the CNS.
- GABA is found in high concentrations in the mammalian brain and spinal cord.
- When GABA receptor is activated, it results in hyperpolarization of the postsynaptic neuron, mediated by the inward flow of Cl-
- Benzodiazepines are thought to increase the affinity of GABA for its receptor and by increasing effective coupling of the GABA receptor to the Cl- channel
onset of Midazolam (Versed)
Onset:
• 2-3 min (IV)
• 15-20min (IM, PO)
Midazolam (Versed) duration of anxiolytic action
1-6 hour (IM)
midazolam duration of anterograde amnesia:
20-40 min (IV) 1 hr (IM)
midazolam peak sedation
30-60 minutes
midazolam Metabolism
– Metabolized by liver via CYP3A
midazolam Elimination
– Half-life: 2-6 hr (IV is closer to 2)
– Excretion: Urine (90%); feces (2%)
the recipe for administration of midazolam
- Initial: Usually 0.5-1 mg given over 2 minutes (not to exceed 2.5 mg/dose);
- wait 2-3 minutes to evaluate sedative effect after each dose adjustment; total dose >5 mg usually not necessary to reach desired sedation;
- use 30% less midazolam if patient pre-medicated with narcotics or other CNS depressants (valium, xanax) or if they are 65+ years old
midazolam Dosing Considerations
– Because it is water soluble, takes approximately 3 times longer than diazepam to peak EEG effects; thus, clinician must wait 2-3 minutes to fully evaluate sedative effects before initiating procedure or repeating dose
– Has twice the affinity for benzodiazepine receptors that diazepam has
– May be administered IM if unable to obtain vascular access
midazolam Adverse Effects:
– >10%: • Decreased Respiratory Rate (23%) • Apnea – 1-10%: • Drowsiness(1-5%) • Seizure-likeactivity(1%) • Nausea/Vomiting(3%) • Cough(1%) • Pain at injection site (4-5%) – Frequency Not Defined: • Headache • Sedation • Hiccoughs • Delirium • Euphoria
ketorlac
?ketamine
Midazolam Black Box Warnings:
– Respiratory depression/arrest has been associated with use, especially when used for sedation in noncritical care settings
– Use lower end of dosing range in debilitated patients, including elderly
– Do not administer by rapid IV injection in neonates (hypotension and seizures reported, especially when used concomitantly with fentanyl)
– Respiratory depression, airway obstruction, desaturation, hypoxia, and apnea, particularly when used with concomitant CNS depressants (eg opioids) have been reported.
diluting 5mg/mL midazolam to 1mg/mL
Put 1 mL of midazolam in a 5 mL syring, then add 4 mL of saline
What drug class does Midazolam (Versed) belong to?
Benzodiazepines
When/why do we use Midazolam (Versed)?
– To treat Anxiety
– To sedate and create amnesia
– To treat seizures
What should our initial dose be in 95% + of cases?
1mg
What should the maximum initial dose be for Midazolam (Versed)?
2.5mg
How long should we wait in between doses of
ANY medication, including Midazolam (Versed)?
2-3 mins minimum
What should our maximum dose of Midazolam (Versed) be regardless of the case length?
Unknown (Dose is based on patient response to medication and level of sedation)
Triazolam other name
Halcion
Reverses Benzodiazepines
Flumazenil
procedure for administering Flumazenil
– 0.2mg IV inj over 15-30 secs (administer slowly)
– If no response: then 0.3mg over 15-30 seconds 1 min later.
– If no response then again 0.5mg IV over 15-30 sec to max cumulative dose of 3mg/hr
half life of Flumazenil
53 minutes
onset of Flumazenil
rapid: 30-60 minute duration
- first order elimination
mechanism of action of flumazenil
Competitive benzodiazepine receptor antagonist
half life of the main Benzodiazepines and reversal agent
- Versed: 2-6hrs
- Valium: 20-70hrs
- Triazolam: 1.5-5.5hrs
- Flumazenil: 53mins
if you have a patient that states they typically vomit after sedation, what should you not give them?
Fentanyl, or give them very little
If you add fentanyl to versed, what happens
1+1 does not equal 2, it will increase the depth of sedation. If Gina has a patient that is having a hard time getting sedated with Versed, she may just add a little Fentanyl to help them get more sedated.
use for fentanyl
Intra operative pain, it’s not good for post op pain because the half life is so short. So if they are moving and wincing during extractions or something (and if they have had the max dose of anesthetic) give a little fentanyl
half life of fentanyl
2-4 hours
patient with a history of seizures, you can make them more likely to have a seizure by giving them…
a narcotic (?)
Respiratory depression occurs with what medications
-Fentanyl
-
Ketorolac (Toradol)
Gina prefers to use this over narcotics for post operative pain. • Class: – NSAID • Dosing Forms: – Patients >50 kg and/or <65 years of age – Moderate / Severe Pain: – IV Administration: 30mg single dose – PO: 30mg q6hr; not to exceed 120mg/day
Dosing Considerations for Ketorolac (Toradol)
– Always begin with parenteral therapy
– Oral administration indicated only as continuation of IV/IM dosing, if necessary
– Duration of therapy should not exceed 5 days
– Dosage beyond maximum or labeled doses will not provide better efficacy but will increase risk of serious adverse events
Contra Indications for Ketorolac (Toradol)
– Renal Impairment:
• Severe contraindications
– Contraindications
• not to be used more than 5 days.
Serious interactions with Ketorolac (Toradol)
aspirin ibuprofen naproxen meloxicam salicylates (non-asa) celecoxib (celebrex)
black box warning for Ketorolac
• Cardiovascular Risk
– NSAIDS may increase risk of serious cardiovascular
thrombotic events, MI, and stroke
– Risk may increase with duration of use
• Gastrointestinal Risk
– NSAIDs increase risk of serious GI adverse events, including bleeding, ulceration, and gastric or intestinal perforation
– Elderly patients are at greater risk for serious GI events (especially with extended use)
