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Pharm1 Test3 Barbiturates Barry

Oxygen is what percentage of air? 21%.
Increasing altitude decreases O2. How does this affect diffusion into tissues? It decreases.
How do hyperbaric chambers work? Increasing PO2 increases O2 delivery into tissues.
Normally hemoglobin is how saturated? 98%.
What are the four causes of oxygen deficiency? 1. low inspired fraction (FIO2), 2. increased diffusional barrier 3. hypoventilation 4. ventilation – perfusion mismatch
What are the five effects of hypoxia? 1. Increased ventilation 2. sympathetic stimulation 3. pulmonary vasoconstriction to optimize V/Q 4. impaired CNS function 5. anerobic metabolism
Hypoxia causes sympathetic stimulation. What results from this stimulation? Tachycardia, but decreased peripheral vascular resistance. This is a local effect.
Hypoxia causes anerobic metabolism. What results from prolonged anerobic metabolism? Increased lactic acid, decreased ionic gradients – increased cell H+, Ca++, Na+ leading to cell death.
What is the main use of oxygen? To reverse or prevent hypoxia.
True or false: due to dissociation curve, increased inspired O2 concentration does not greatly increase blood O2. True.
Overexposure to oxygen can cause toxicity, probably due to formation of... Peroxide.
Carbon dioxide is part of what buffer system? Bicarbonate buffer system.
Increasing PCO2 leads to... Respiratory acidosis.
Decreasing PCO2 leads to... Respiratory alkalosis.
What is another word for hypocarbia? Respiratory alkalosis.
When would you use hypocarbia to decrease cerebral vessels and decrease brain size somewhat? Neurosurgery.
When would we use carbon dioxide during cardiac surgery? To reduce air (insoluble N2) around heart.
True or false: sudden high calcium levels is an indicator for cell death? True.
True or false: CO2 therapy is frequently used to stimulate respirations. False.
Nitric oxide is used in the cells as a... Signaling molecule.
What is the main driving mechanism for the dilation of many arterioles? Nitric oxide.
Nitric Oxide can cause large pulmonary dilation with minimal systemic effects dsfj
Helium is an inert gas. What are its three main uses? Pulmonary function testing, laser airway surgery, and diving.
What are sedative? Agents which cause mild suppression of arousal and behavior, and a slight decrease in alertness and response to stimuli.
What are hypnotics? Agents which cause pronounced sedative effects including the induction of sleep.
True or false: patients receiving hypnotics are usually arousable to painful stimuli. True.
Most hypnotics are simply sedatives... Given in larger doses.
Nitric oxide has minimal systemic side effects. The main systemic side effect is... Binds to and inactivates oxyhemoglobin.
Normal sleep has at least two phases, which are? Slow wave sleep(SWS) and rapid eye movement sleep(REM).
What happens in slow wave sleep? EEG shows mainly high-voltage synchronous activity.
Describe rapid eye movement sleep: Skeletal muscles are relaxed (inhibited) and the eyes move back and forth rapidly. Accounts for ~ 25% of sleep.
What are the three effects of hypnotics on sleep? 1. SWS patterns are altered and shortened. 2. REM sleep is depressed 3. Total sleep time is prolonged.
True or false: Benzodiazepines bind to the GABA-a receptor complex at the same site as the Barbiturates. False. Benzodiazepines bind to the GABA-a receptor complex at a different site as the Barbiturates.
How do the Barbiturates act on GABA? Decreases the dissociation rate of GABA from its binding site, thus increasing the duration of action of GABA at the receptor, and increasing chloride conductance.
True or false: Barbiturates have been reported to be able to mimic the action of GABA at the GABA-a receptor, this is a strong effect. False. While Barbiturates have been reported to be able to mimic the action of GABA at the GABA-a receptor, this is minimal, and major effects require GABA.
In addition to decreasing the dissociating rate of GABA, Barbiturates also inhibit... Excitatory glutamate AMPA receptors.
The parent compound of Barbiturates is Barbituric Acid. What are its sedative qualities? It has none.
What forms does Barbituric Acid take? Keto and enol (tautomers)
You can affect the sedative/hypnotic qualities of a Barbiturate by adding functional groups onto what position? Position 5.
The Thiobarbiturates are more lipid-soluble. How are they made? Replacement of C-2 oxygen with sulfur.
Phenobarbitol is a Barbiturate with anticonvulsent properties. How is it made? Addition of a phenol group at C-5.
How can you change the chemical structure of a Barbuturate to shorten its duration of action? Addition of a methyl group to the ring N atom.
What is the long-duration Barbiturate? Phenobarbital (Luminal).
What are the intermediate-duration Barbiturates? Pentobarbital (Nembutal) and Secobarbital (Seconal).
What are the short-duration Barbiturates? Methohexital (Brevital) and Thiopental (Pentothal).
True or false: Barbiturates are weak bases. False. Barbiturates are weak acids.
The basic way to chemically package Barbiturates is as a... Sodium salt.
A solution of Barbiturate is bacteriostatic why? Because of its high pH(packaged as a basic sodium salt).
Why do Barbiturates only last for a few weeks after being opened? Because after exposure to air acid precipitates out because CO2 in air alters pH of solution.
True or false: More lipid soluble Barbiturates have shorter onset due to rapid increase in brain conc., followed by rapid redistribution to body tissues. True.
Most Barbiturates are metabolized to a large extent. What is the primary metabolic pathway? Hydroxylation to inactive metabolites.
What is the half-life of Phenobarbitol? 86 hours.
In addition to the hydroxylation pathway, Barbiturates are also metabolized (to a larger extent by Asians) by what pathway? N-glucosylation.
Barbiturates are potent inducers of what in the liver? The hepatic microsomal enzyme system.
What is the result of Barbiturates' induction of hepatic microsomal enzyme system? An increased metabolic rate of barbiturates as well as other drugs normally metabolized by this system(oral anticoagulants, phenytoin, TCA).
Why do we use Barbiturates? Induction of anesthesia, anticonvulsants, Neuropsychiatric exams(Wada Speech Test) prior to neurosurgery, cerebral edema and brain protection.
How do Barbiturates effect pregnancy? Fetal blood levels usually well under maternal levels, but placental transfer does occur. Fetal elimination much slower than mother.
Why has use of Barbiturates declined? 1. Benzodiazepine’s are safer and just as effective. 2. Drug interactions (due to enzyme induction) 3. Tolerance development 4. Greater abuse potential 5. Less CNS specificity than Benzodiazepines
How do we currently use Barbiturates? 1. Therapeutic/diagnostic aids in psychiatry 2. Reduction of cerebral edema following surgery, head injury or cerebral ischema 3. Antiepileptic use.
Thiopental(Pentothal) is an ultra-short acting, highly lipid soluble Barbituate. How long until induction? 10-15 seconds.
Thiopental(Pentothal) is rapidly distributed into the brain due to high blood flow. It is then quickly redistributed where? Fatty tissues. This accounts for its short effect.
Why do we use Thiopental(Pentothal)? Induction and short cases.
Thiopental has a half-life of 6 hours. Where is it metabolized? By the P-450 system in the liver.
How do repeated doses of Thiopental(Pentothal) increase the duration of action? Because the body's storage centers (fatty tissues) fill up.
True or false: Thiopental(Pentothal) reduces pain threshold, sensitizing the body to pain. True.
True or false: Thiopental(Pentothal) has muscle relaxant effects. False. This drug has very poor skeletal muscle effects.
True or false: Thiopental(Pentothal) is a respiratory depressant, leading to a period of apnea on induction. True.
How does Thiopental(Pentothal) decrease blood pressure? Depressing the myocardium and relaxing smooth muscle in the vasculature.
True or false: we are currently on a Thiopental(Pentothal) shortage. True.
How does Methohexatol(Brevitol) compare in potency to Thiopental(Pentothal)? It is three times as potent.
Both are metabolized by the P-450 system. Why is Methohexatol(Brevitol) metabolized more quickly than Thiopental(Pentothal)? Methohexitol(Brevitol) is less lipid-soluble than Thiopental(Pentothal)?
True or false: Methoxital(Brevitol) has a faster recovery than Thiopental after multiple doses? True.
Created by: 1592042303