Induction Drugs Flashcards
Gold standard for IV anesthetics
Barbs
barbituric acid is composed of
urea + malonic acid
Barbs: sedative & hypnotic properties are determined by alterations in which carbon atoms?
2 & #5
Name the oxybarbiturates
Methohexital
Phenobarbital
Pentobarbital
Secobarbital
The characteristic effect of methohexital due to methyl group on the nitrogen
Increased risk of excitatory phenomenon, seizures, and hiccoughs
The phenyl group at the #5 position for Phenobarbital leads to what drug effect?
increased anticonvulsant properties
How do pentobarbital and secobarbital differ in chemical structure from the other oxybarbiturates?
O2 atom at the #2 carbon atom
Name the two Thiobarbiturates.
Thiopental
Thiamylal
How does the chemical structure of thiobarbiturates differ, and what does this mean for the drug characteristics?
There is sulfur at the #2 carbon atom. This leads to increased lipid solubility and hypnotic potency.
Barbs MOA
Increase affinity for GABA. Barbs can also mimic GABA and activate chloride channels even with no GABA present.
How does the metabolism of oxybarbs and thiobarbs differ?
Oxybarbs = Liver
Thiobarbs = Liver, Kidney, Brain
Intra-arterial injection of which barb can lead to cyanosis and gangrene?
Thiobarb
What effect does sustained delivery of barbs have on liver enzymes, and which medication is the biggest culprit?
Liver enzymes are induced leading to increased metabolism of drugs. Phenobartibal is the most potent liver enzyme inducer.
Liver enzyme induction accelerates the metabolism of which drugs?
oral anticoagulants
phenytoin
TCA
corticosteroids
bile salts
vitamin K
What is Porphyria, and what drug class is avoided by patients presenting with it?
The autosomal dominant disease leads to defective heme metabolism. This leads to neurological damage, peripheral and autonomic neuropathies, and psychiatric manifestations.
Barbiturates should be avoided.
Why are barbiturates bad for patients with AIP?
Barbiturates accelerate heme production. AIP presents as a defect in heme metabolism which leads to excessive accumulation of heme, eventually leading to acute attacks and death.
Categorize the BZ by their elimination half-life.
Short: Midazolam
Intermediate: Lorazepam
Long: diazepam
T 1/2 of Midazolam?
<6 hours
T 1/2 of Lorazepam?
6-24 hours
T 1/2 of Diazepam?
24-37 hours
BZ MOA
BZ bind to GABBA-A receptors and modulates their activity (enhances affinity). GABA is required as BZ are unable to open chloride channels without them.
The imidazole ring found in BZ requires what state to increase lipid solubility, and under what circumstances does this occur?
Closed state, and occurs at physiological pH.
Which BZ are preferred for increased age and liver disease, and why?
Lorazepam, oxazepam, temazepam.
These are metabolized by glucuronidation, which is not effected by age or liver disease.
A symptom of BZ withdrawal in the elderly presents as what?
Confusion
Long-term use of BZ leads to two significant things in the patient population.
Tolerance & cognitive decline
BZ produce more _____ than sedation.
amnesia
PO administration of which drug has a high first-pass hepatic extraction.
Midazolam
Drugs that inhibit CYP450 enzymes and prolong metabolism include (5).
Fentanyl
Erythromycin
CCB
Antifungals
Cimetidine
CNS effects include anterograde amnesia.
Midazolam
Respiratory effects of Midazolam
decreased TV
increased RR
May increase cardiac output in CHF patients.
Midazolam
Modest CV effects include decreased ABP and increased HR.
Midazolam
Most common preoperative sedative in adults and children.
Midazolam
Used prophylactically to raise seizure threshold when performing regional blocks
BZ
Avoid this bz medication in pregnant patients
Midazolam
Po administration results in 100% bioavailability.
Diazepam
Mixing with NS or water for dilution results in cloudiness.
Diazepam
This medication crosses the placenta, resulting in fetal concentrations equal to or greater than the mother
Diazepam
Which active metabolite of a BZ contributes to sustained drug effects and return of drowsiness 6-8 hours after administration?
Desmethyldiazepam
Which drug can decrease LVED pressure with small doses?
Diazepam
Minimal CV effects with this drug. They equate to natural sleep.
Diazepam
Used to produce skeletal muscle relaxation in lumbar disc disease.
Diazepam