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195 Cards in this Set

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  • Back
What two groups of alcaloids does opium resin contain?
Phenanthrenes and Isoquinolines
What is an opiate?
A drug delivered from opium poppy
What are opioids?
Includes opiates, opiopeptines, synthetic, and semisynthetic drugs
What are opiopeptines?
Endogenous peptides meaning they are produced in the body naturally
How much more potent are opiopeptines than morphine?
200
What are the four types of endogenous opioids?
Enkephalines, dynorphins, endorphins, and endomorphins
How many amino-acid peptides do enkephalines have?
5. They are pentapeptides
What are they two types of dynorphins?
A and B
How many amino-acid peptides do dynorphins have?
17
How many amino-acid peptides do endorphins have?
31
How many amino-acid peptides do endomorphins have?
4
Where are opioid receptors found?
The limbic system, the medial and lateral thalamus, the hypothalamus, the medulla oblongata, and the spinal cord
How many subtypes of opioid receptors are there?
4
What type of receptors are opioid receptors?
G-protein family
What is the main effect of opioid receptors on the cell membrane?
Inhibition
What is the process of opioid receptor inhibition?
Phospholipase C is activated which inhibits adenylate cyclase which inhibits cAMP. This opens K channels causing repolarization and closes Ca channels causing the inhibition of neurotransmitter release.
What are the four types of receptors?
Mu, Kappa, Sigma, Delta
What symptoms is Mu responsible for?
Analgesia, supraspinal analgesia, respiratory depression, euphoria, and physical dependence
What effects is Kappa responsible for?
Spinal analgesia, miosis, and sedation
What symptoms is Sigma responsible for?
Hallucinations, respiratory stimulation, and vasomotor stimulation
What symptoms is Delta responsible for?
Periphery
What is the molecular weight of Morphine?
285
What are the Morphine-like agonists?
Morphine Sulphate, Hydromorphone, Oxymorphone, and Heroin
What are the Codeine-like agonists?
Codeine, Tramadol, Hydrocodone, and Oxycodone
What are the synthetic opioid agonists?
Meperidine, Fentanyl, Methadone, Levophanol
What are the Agonists/Antagonists?
Pentazocine (Talwin), Butorphanol (Stadol), and Nalbuphine (Nubain)
What are the antagonists?
Naloxone (Narcan) and Naltrexone (Deprade, ReVia)
What are the CNS effects of Morphine?
Dose-related analgesia, sedation and euphoria, stimulation of chemoreceptor trigger zone (CTZ), N/V, miosis, small permeability of blood brain barrier, hypothermia, and convulsions at high doses
What are the respiratory/digestive side effects of Morphine?
Respiratory depression, chest wall rigidity, bronchoconstriction, decreased peristalsis, stomach motility, and biliary/pancreatic secretion. Also constricts the sphincter of Oddi in pancreas
What are the urogenital side effects of Morphine?
Urinary bladder contraction, uterine tone reduction, and crosses the placental barrier.
What are the skin effects of Morphine?
Allergic skin rashes and dilation of cutaneous vessels
Where is Morphine well absorbed?
GI Tract
Is first pass metabolism present when taken orally?
Yes
How much Morphine is protein-bound when in the body?
30%
Where is Morphine metabolized?
Liver
What is Morphine metabolized to?
Morphine 6-glucuronide
What are the clinical uses of Morphine?
Analgesia, pulmonary edema, severe diarrhea, cough suppression, and anesthesia
If Morphine is abruptly discontinued, when do withdrawal symptoms begin to occur?
8-10 hours after last dose
How long do withdrawal symptoms of Morphine last?
10 days
What are the symptoms of withdrawal?
Lacrimation, violent coughing/sneezing, insomnia, hypertension, tachycardia, depression, vomiting, diarrhea, and dehydration
What segment of Morphine comprises codeine?
3-methylether of morphine
What is the potency of codeine?
1/12th of morphine
What does 30mg of codeine equal to in relation to aspirin?
600mg
What are the benefits of codeine over morphine?
Less sedation, decreased respiratory depression, less GI effects, decreased rate of addiction, it is a good oral analgesic for mild pain
What is heroin converted to in the body?
Morphine
What is the other name for heroin?
Diacetylmorphine
What is the equivalent dosage of heroin to morphine?
3mg heroin = 10mg morphine
What is the molecular weight of methadone?
309.45
Methadone is orally more effective than morphine. True or False.
True
What happens to methadone in the tissues?
It gradually accumulates
What is the danger of methadone?
Cumulative toxicity
What is the molecular weight of Meperidine?
247.3
What is the analgesic potency of meperidine?
1/8th of morphine
What are some significant side effects of meperidine?
Smooth muscle spasm (bronchospasm), atropine-like activity (dry mouth, blurring of vision), hyperthermia, and convulsions with MAO
Why is meperidine preferred to morphine during labor?
Shorter duration of action
What happens with large doses of Meperidine?
CNS excitation
What is the analgesic potency of Fentanyl?
80/1 of morphine
What happens when high doses of Fentanyl are given?
Muscular rigidity
What was the first pure opioid antagonist?
Naloxone
What does Naloxone do?
It reverses respiratory depression, reverses cardiovascular effects, and precipitates withdrawal
Naloxone is rapidly metabolized. True or False?
True
When is Naltrexone contraindicated?
Anytime the liver is impaired.
What adverse effects does Naltrexone have?
Anxiety, cramps, and joint pain
What are the three major classes of sedative-hypnotics?
Barbiturates, benzodiazepines, and miscellaneous
What is the parent compound of barbiturates?
Barbituric acid
Does barbituric acid depress the CNS?
No
What does the efficacy of barbiturates depend on?
Lipid solubility
What is the ultra-short barbiturate, what is its time of action, and what is it typically used for?
Thiopental, 0-30s, adjuvant to anesthesia
What are the short-acting barbiturates, what is their time of action, and what are they classified as?
Hexobarbital, pentobarbital, secobarbital, 2 hours, hypnotics
What are the intermediate barbiturates, what is their time of action, and what is their classification?
Amobarbital, butabarbital, 3-5 hours, hypnotics
What are the long-acting barbiturates, what is their time of action, and what is their classification?
Barbital, phenobarbital, >6hours, hypnotics/sedatives/antiepileptics
Where are the barbiturates absorbed?
Stomach, small intestine, rectum, intramuscular
What two barriers are crossed by barbiturates?
Blood-brain barrier and placental barrier
What receptors do barbiturates and benzodiazepines act on?
GABA
Both barbiturates and benzodiazepines potentiate the binding of GABA to GABA receptors. True or False?
True
What do barbiturates stimulate physiologically?
Hepatic microsomal system
What are the clinical effects of barbiturates?
Low selectivity, narrow therapeutic index, tolerance, suppress REM sleep, high potential for dependence/abuse, oversedation, drowsiness, withdrawal (seizures, tremors, hallucinations)
What was the first benzodiazepine?
Valium (Diazepam)
How do barbiturates act on GABA receptors?
GABA binds to GABAa receptor. Barbiturates binding to receptor potentiates this binding. Chloride rushes into the cell making the membrane stable and making depolarization difficult.
What are the therapeutic uses of Valium?
Treatment of anxiety, anesthetic premedication, sedative-hypnotic, seizures, treatment of alcohol withdrawal, treatment of night terrors, treatment of panic attacks, obstetrics during labor
What are the pharmacodynamics of benzodiazepines?
They potentiate the binding of inhibitory GABA to GABA receptors, benzodiazepine receptors are in the thalamus, the limbic system, and cortex; and they bind to GABAa to increase the frequency of calcium channel opening
What is the difference between the pharmacodynamics between barbiturates and benzodiazepines?
Cloride channels open more frequently in benzodiazepines and channel opening is prolonged in barbiturates
What drug interactions should be avoided in benzodiazepines?
Alcohol, opioids, anesthetics, antidepressants, and MAO inhibitors
What is the action and 1/2 life of Midazolam?
Short acting and 2.5 hours
What is the action and 1/2 life of Lorazepam?
Intermediate acting and 14 hours
What is the action and half-life of Diazepam?
Long-acting and 2-4 days
What can chronic benzodiazepine use cause?
Cognitive impairment, tolerance, and dependence
How does Flumazenil work?
It is a competitive antagonist for benzodiazepine site on GABAa complex
What is the molecular weight of chloral hydrate?
165.5
Chloral hydrate suppresses REM. True or False?
False
Does chloral hydrate have an effect on RR/HR?
No
What does a sudden break in chloral hydrate tolerance lead to?
Acute intoxication
How does one determine cardiac output?
CO = HR x SV
What two systems control heart rate?
Parasympathetic and Sympathetic nervous systems
What two factors determine stroke volume?
SNS and venous return
What factors control the return of venous blood to the heart?
Low pressure in right atrium, low pressure in thoracic cage, valves provide unidirectional flow, and muscle pumps
What three factors control BP?
Resistance, HR, volume
What does sympathetic stimulation have upon the heart?
Norepinephrine increases permeability of fibers to sodium and calcium. Increases heart rate. Increases contractility
What are the parasympathetic effects on the heart?
Acetylcholine increases permeability of fibers to potassium and increases negativity. Decreases HR. No effect on contractility
Where is the majority of blood in CVS?
Veins
How much blood is in the veins?
64%
How much blood is in the arteries?
13%
How much blood is in the pulmonary circulation?
9%
How much blood is in the heart and arterioles/capillaries?
7%
What is Ohm's Law?
Q(flow in the system) = P(pressure in the system)/R(resistance in the system)
The sum of all resistances = total resistance in series or parallel?
Series
Total resistance is less than the sum of all resistances in series or parallel?
Parallel
What is Poiseulles Law?
The physical law that concerns the voluminal flow of an incompressible viscous liquid through a cylindrical tube
What are the three major factors affecting blood flow?
Radius, viscosity, and length
Small changes in the radius of a vessel may significantly affect the resistance to blood flow. True or False?
True
What is blood viscosity determined by?
Hematocrit
What is the viscosity of plasma?
1.8
What is the viscosity range of whole blood?
3-5
What is the viscosity of water?
One
What are the three factors in blood flow control?
Local, humoral, and nervous
What products comprise local blood flow control?
Carbon dioxide, lactic acid, adenosine, histamine, K+ ions, H+ ions, and nitric oxide
What products comprise humoral blood flow?
Vasoconstrictor = epinephrine, norepinephrine, angiotensin, endothelian, and vasopressin
Vasodilatory = epinephrine, bradykinin, serotonin, histamine, prostaglandins, and nitric oxide
What two factors comprise nervous system blood flow control?
Innervation of all blood vessels except capillaries and precapillaries. Vasoconstrictor and vasodilatory fibers
Which system is the most important in blood flow control?
Nervous
What is solubility?
The ability for a given solute to dissolve in a solvent. During equilibrium, dissolved gas molecules leave liquid at the same rate as other molecules that are dissolving
What is Henry's Law?
At a constant temperature, the amount of a given gas dissolved in a liquid is directly proportional to the partial pressure of that gas in equilibrium with that liquid
At higher temperatures, less gas dissolves. True or false?
True
Why do bubbles of air form in infusion lines passing through warming coils?
At higher temperatures, less gas dissolves
What is the solubility of nitrogen at temp 37 and partial pressure of 100kPa?
0.014L
What is the solubility of nitrous oxide at temp 37 and partial pressure of 100pKa?
0.39
Do gases have different solubilities?
Yes
At 21% O2 and 1 ATM, what is the amount of O2 in the blood?
0.3m/O2
Anesthetics with high solubilities are more powerful. True or false?
True
What is the solubility of nitrous oxide in blood at a temp 37 and partial pressure of 100kPa?
0.47L
What four factors determine the solubility of a gas?
Partial pressure, temperature, gas, liquid
What is a solubility coefficient?
A measure of how easily gas dissolves in liquid
What is the Bunsen Solubility Coefficient?
The volume of gas in milliliters at standard temperature and pressure that is dissolved in one milliliter of liquid
What is the Oswald Solubility Coefficient?
The volume of gas which dissolves in one unit volume of liquid at a known temperature
What is the partition coefficient?
The ratio of a substancein one phase compared with the other. The two phases are of equal volume and are in equilibrium
At a temp of 37, what is the nitrous oxide blood-gas partition coefficient?
0.47
At a temp of 37, what is the nitrous oxide gas-blood partition coefficient?
2.1
How much nitrous oxide dissolves in 1 L of oil?
1.47
How much nitrous oxide dissolves in 1 L of blood?
0.47
Do anesthetics have receptor sites?
No
Do anesthetics have pharmacologic antagonists?
No
What is at the foundation of anesthesia?
Overton-Meyer correlation
What are the principles of the Overton-Meyer correlation?
Anesthetic potency is proportional to lipid solubility; there is a linear relationship b/t oil/gas partition coefficient and potency; olive oil is used to measure lipid solubility
How far apart are alveoli from capillaries?
0.1-0.5micrometers
What is the surface area of alveoli?
60-100m2
What three factors affect alveolar stability?
Alveolar interdependence, pulmonary surfactant, residual volume
What is surfactant?
Phospholipids that reduce surface tension of the alveoli
What alveolar cells produce surfactant?
Type II
What is LaPlace's Law?
P(collapsing pressure) = 2T(surface tension)/R(alveolar radius)
What is the range of negative pressure in the pleural cavity?
-4 to -9
What is a pneumothorax?
A life-threatening condition in which pressure within the pleural cavity is equivalent to atmospheric pressure
What is tidal volume and what does it equal?
The volume of air that is breathed with normal respiration. It is typically 500ml
What is inspiratory reserve volume and what does it equal?
IRV is the additional volume of air that can be breathed in after normal respiration. It equals 3000ml.
What is expiratory reserve volume and what does it equal?
ERV is the additional volume of air that can be exhaled after normal respiration. It equals 1100ml.
What is residual volume and what does it equal?
The volume of air that remains in the lungs after maximal exhalation. It equals 1200ml.
What is inspiratory capacity?
This is the volume of air that can be inhaled after normal exhalation
What is vital capacity?
The volume of air that can be forced out of the lungs after maximal exhalation
What is functional residual capacity?
The volume of air that resides in the lungs after normal exhalation
What is total lung capacity?
The volume of air in the lungs after maximal inhalation
What is minute respiratory volume?
The volume of air that can be inhaled/exhaled in one minute
What is alveolar ventilation rate?
The volume of air that reaches the alveoli per unit time
What is anemic hypoxia?
When total O2 in blood is low but pO2 is normal
What is histotoxic hypoxia?
When cells are receiving enough O2 but they cannot utilize it well because they have impaired oxidative phosphorylated enzymes
What is circulatory hypoxia?
When organs and tissues do not receive enough oxygen
What is hypoxic hypoxia?
Generalized hypoxia
If pO2 decreases and/or pCO2 rises, what happens?
Peripheral chemoreceptors are triggered and ventilation increases to increase pO2 or decrease pCO2
What are the 3 categories of general anesthesia?
Inhalation, intravenous, and balanced
Why do we use premedications in anesthesia?
They reduce the amount of anesthesia needed
If you increase MAC, do you stimulate or depress the CNS?
You stimulate the CNS
What factors increase your MAC?
Alcoholism, CNS stimulants, hyperthermia, young age
What factors decrease your MAC?
Anemia, other anesthetics, CNS depressants/sedation, Lithium, Lidocaine, opioids, hypothermia, pregnancy, very young age, and alpha 2 agonists
What are the physiological effects of anesthesia on the CNS?
Decreased awareness, decreased cerebral metabolism, increased cerebral blood flow, increased CSF pressure, EEG changes, seizures, shivering
What are the physiological effects of anesthesia on the respiratory system?
Bronchodilation, increased RR, decreased minute volume, decreased alveolar ventilation, depressed cerebral chemoreceptors, depressed response to hypoxia
What are the physiological effects of anesthesia on the heart?
Decreased BP, decreased myocardial oxygen consumption, decreased sympathetic response, decreased AV conduction, increased arrhythmias, increased cutaneous blood flow
What are the physiological effects of anesthesia on the musculoskeletal system?
Skeletal muscle relaxation, uterine tone relaxation, malignent hyperthermia
Why was diethyl ether halted in use?
Flammable
What are the anesthetic properties of IV barbituates?
Rapid induction, rapid recovery, respiratory depression, cardiac depression
What are the anesthetic properties of benzodiazepines?
Rapid induction, rapid recovery, minimal respiratory depression
What are the anesthetic properties of ketamine?
Hallucinations, trance-like state
What are the anesthetic properties of opioids?
Analgesia, respiratory depression, constipation, N/V, prolongs awakening, wheezing, hypotension
How is Halothane biotransformed?
5% is biotransformed by P-450 by removal of bromide and chloride
Halothane is safe for children. True or false?
True
What does Halothane do to metals and rubber?
It corrodes metal and reacts with rubber
What is the major cardiac effect of halothane?
It increases sensitivity to catecholamines
What are the adverse effects of halothane?
Decreased liver function and malignent hyperthermia
When does halothane hepatitis occur?
2-5 days post-op evidenced by fever and vomiting
What populations are susceptible to halothane hepatitis?
Middle age, women, preexisting liver disease
Children are susceptible to halothane hepatitis. True or false
False
What anesthetic is characterized by free flouride in the system and nephrotoxicity?
Methoxyflurane
Methoxyflurane is characterized by what two side effects?
Free flouride in the body and nephrotoxicity
What anesthetic dissolves in rubber, stimulates salivation, and suppresses laryngeal reflexes?
Enflurane
Enflurane is characterized by what side effects?
Stimulates salivation, dissolves in rubber, and suppresses laryngeal reflexes
What anesthetic is used in day surgery and cannot be used in infants/children w/mask because of upper airway irritation?
Desflurane
Is nitrous oxide combustible?
Yes
What concentration of nitrous oxide maintains anesthesia?
75-80%
What organ is responsible for the elimination of nitrous oxide?
The lungs via respiration