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422 Cards in this Set

  • Front
  • Back
What are the two major types of ion channels?
1. Voltage Gated
2. Ligand Gated
Where are voltage gated channels concentrated?
They are concentrated on the axons of nerve cells.
Voltage gated ion channels include what channels?
They include the sodium channels responsible for action potential propagation.
Cell bodies and dendrites also have voltage sensitive ion channels for what?
Potassium and calcium.
Ligand gated ion channels are also called what?
ionotropic receptors
Ionotropic receptors respond to what?
Chemical neurotransmitters that bind to receptor subunits present in their macromolecular structure.
Neuturtansmitters also bind to G protein coupled receptors. What are these called?
Metabotropic receptors.
Metabotropic receptors (G-Protein coupled receptors) can do what?
Modulate volatage gated ion channels.
What is a "Global but reversible depression of CNS function" called?
Anesthetized state
General Anesthesia includes what four things?
1. Amnesia
2. Immobility
3. Inhibition of reflexes
4. Skeletal Muscle Relaxation
How many stages of anesthesia are there?
Four
Stage 1 of Anesthesia is?
Analgeisa with or without amnesia
Stage 2 of Anesthesia is?
Excitement (Delirium)
Stage 3 of Anesthesia is?
Surgical Anesthesia
How many planes does stage 3 of anesthesia have?
Four
What two ways are general anesthetics administered?
IV and Inhalation
What are the two types of inhaled general anesthetics?
Nitrous Oxide and Volatile Liquids
Can Nitrous Oxide produce stage III anesthesia on its own?
NO!!!
Why is it that Nitrous oxide can not produce stage three anesthesia on its own?
Low potency
What is the maximal safe concentration of Nitrous Oxide?
70%
What are the four types of Volatile Liquid Inhaled Anesthetics?
Isoflurane, halothane, desflurane, and sevolfurane
How are volatile liquids administered?
They are vaporized with air; or oxygen as a carrier gas.
There are six categories of IV general anesthetics. What are they? HINT: BBOPKM
Barbiturates, Benzodiazepines, Opiods, Propofol, Ketamine and Misc.
What is the method of action for the general anesthetics?
Involves suppression of neuronal communication in critical brain areas.
Since the MOA for general anesthetics involves suppression of neuronal communication in critical brain ares, what are the two ways this occurs?
By either increasing Action Potential Threshold or By interfering with synaptic transmission.
General Anesthetics bind to the ________ receptor and potentiate _______ transmission?
GABAa
GABA
When GABA transmission is potentiated what does this cause to happen?
An increase in Cl- influx, which in turn increases membrane hyperpolarization, ultimately inhibiting neuronal activity.
What happens when you have a low concentration of a general anesthetic?
Indirect effect on GABAa receptor
What does this indirect effect of low concentration general anesthetics do to GABA?
It enhances the efficacy of the endogenous GABA
High concentrations of general anesthetics do what?
Directly activate GABAa channels.
What other methods of action might general anesthetics have involving K+ and Nicotinic Na+ channels?
An increase of K+ efflux can occur which would cause hyperpolarization. There can also be a decrease in the duration of opening of nicotinic Na+.
What three general anesthetics function by inhibiting NMDA receptors?
HINT: K,NO,X
Ketamine, nitrous oxide and xenon.
Potency of Inhalational general anesthetics is directly proportional to?
Lipid Solubility.
Increased Lipophilicity =
Increased Potency
The potency of an inhaled general anesthetic is measured by?
Minimum alveolar concetration of anesthetic or the MAC
If you have a high Oil/gas partition coefficient?
You have a high potency.
If you have a low MAC you have?
A high potency due to a higher lipid solubility.
The alveolar concentration of an anesthetic that is required to prevent a response to a standarized painful stimulus in 50% of patients.
MAC
MAC =
ED50
What is the usual effective MAC range?
0.5-1.5 MAC
When are MAC values lowered?
In the elderly and hypothermia
With inhaled anesthetic, brain anesthetic concentration is directly correlated to?
Blood anesthetic concentration.
During Induction:

Highly _______ (2)exert the greatest influence?
Perfused Organs
Highly perfused organs are?
The brain, heart, liver, kidneys, lungs, and spleen
During Maintenance: The rate of drug transfer is dependent on? (two things)
Drug tissue Solubility
Blood Flow
What is the major route of elimination for all inhalational anesthetics?
Lungs
What is the most important thing regarding elimination of an inhaled anesthetic?
Blood:Gas partition coeffecient
Which is eliminated faster? Blood insoluble agents, or blood soluble agents.
Blood insoluble agents are eliminated faster.
All inhaled anesthetics ____ MAP in direct proportion to their ______?
Decrease
Alveolar Concentration
What inhaled anesthetics decrease BP by decreasing CO?
HINT: H, E
Halothane and Enflurane
Isoflurane, desflurane, and sevoflurane do what to the cardiovascular system?
Decrease BP and PVR
What inhaled anesthetic decreases SA node firing leading to bradycardia?
HINT: Hal
Halothane
What two inhaled anesthetics cause sympathetic activation leading to tachycardia?
HINT: D, I
Desflurane and Isoflurane
How do inhalation anesthetics, except Nitrous Oxide, affect the respiratory system?
They decrease tidal volume and increase respiration rate. They decrase ventilatory response to low 02 so must ventilate mechanically until breathing restored. Pooling of mucus leads to atelectasis/pneumonia. Suctioning/early ambulation are required.
How do inhalation anesthetics affect the brain?
They decrease metabolic rate, they increase cerebral blood flow due to a decrease in vascular resistance.
In what brain condition should inhaled anesthetics be used with caution?
Increased Inter-Cranial Pressure, caution also in head trauma.
________ seen on EEG (CNS depressent effect) up to 1-1.5 MAC but higher may predispose to _______.
Burst Firing
Seizures
How do inhaled anesthetics affect the kidneys?
They decreased glomerular filtration rate and decrease renal blood flow.
In the liver, inhaled anesthetics decreased _______ to 15-45% normal.
Hepatic blood flow.
This inhaled anesthetic causes liver damage at low 02 levels, and usually after repeat exposure. What is the name of this toxicity?
Halothane
Halothane Hepatitis
What types of proteins are created in the process of halothane metabolism and what does this lead to?
Trifuoroacetylated proteins are generated, this leads to antibody formation, autoimmune hepatitis which results in liver transplant.
Sevoflurane degradation by CO2 absorbents release ___________ which causes ____________.
HINT: VE, PTN
Vinyl Ether
Proximal Tubular Necrosis
What is a genetic disorder of skeletal muscle where mutations on ryanodine receptors (L-type voltage gated Ca2+ channel) or SR leads to increase in free Ca2+?
Malignant Hyperthermia Syndrome
In patients that this occurs in what are they receiving when this occurs?
Muscle relaxants and inhaled anesthetics (especially halogenated).
Malignant Hyperthermia involves what symptoms?
Hyperthermia, Tachycardia, HTN, Muscle Rigidity and Contractions, and Metabolic Acidosis
What is the suggested Rx for metabolic hyperthermia syndrome?
Dantrolene, cooling, restore pH to 7.4
How does dantrolene work against this syndrome?
It blocks ryanodine.
This inhaled anesthetic sensititizes the heart to catecholamines by increasing automaticity leading to cardiac arrhythmias.
Halothane
When using halothane what are two drugs you must use with extreme caution?
HINT: EPI and Cat
Use EPI and other catechomalines with extreme caution.
This drug causes seizures, especially at higher concentrations?
HINT: En
Enflurane
In what kind of patients should enflurane be avoided?
Epileptics
Nitrous oxide can decrease methionine synthase activity leading to what?
Megaloblastic anemia.
Intravenous anesthetics are combined with what to increase cardiovascular stability?
Opiods
The short acting barbiturate, Thiopental is used for ______ and ___________?
Induction and Short Surgeries
If you have a large dose of the short acting barbiturate thiopental, what can occur?
Myocardial depression
In what situation is thiopental, a short acting barbiturate, used for specifically in large doses?
Brain Trauma. Due to the decrease in cerebral blood flow it can help lower blood loss.
What are three benzodiazepenes that are used as pre-op medications?
Diazepam, lorazepam, and midazolam
Midazolam, a benzodiazepene, is the ______ and it is placed in a ___________ so it results in __________?
Most common
water soluble preparation
less irritation
What reverses the effects of Midazolam, a benzodiazepene?
HINT: Flu
Flumazenil
Flumazenil is a ________, that reverses ________.
Benzodiazepene antagonist
Midazolam
Flumazenil has a _________ meaing that ___________.
Short t1/2
multiple doses may be required for desired affect
With the opiods _____ and _____, N20 and Benzodiazepenes are used. This is especially useful in high risk patients.
Morphine and Fentanyl
Increased _______ and Increased _______ are used in patients undergoing cardiac surgery or if patients have cardiac problems.
Increased doses of opiods with increased doses of Benzodiazepenes
What is one of the complications that can occur from using increased opiods?
Chest wall rigidity during surgery which leads to impaired breathing.
What is a opiod agonist that reverses respiratory depression?
Naloxone
What opiods have a very fast induction?
HINT: Alf, Rem
Alfentanil and remifentanil
What causes remifentanil to have a very fast recover
Remifentanil is metabolized by esterases, which leads to fast recovery
When you give fentanyl (an opiod) with droperidol (like haldol) and N20, neuroleptanesthesia occurs. What is this?
It is a dissociative anesthesia
What is a drug that has a very fast onset and recovery, quicker ambulation, less nausea and vomiting, and patient feels better overall. This drug is also used in conscious sedation.
Propofol
Propofol causes what problems in kids?
Acidosis, especially in kids with respiratory infections
Etomidate is best for patients with compromised _______ function?
cardiac
Etomidated causes minimal _____ and _______ depression.
CV and respiratory
This drug is not ______, so you must use with _______?
analgesic
opioids
What drug causes dissociative anesthesia, related to PCP, it is an NMDA receptor blocker so it effects glutamate and it is lipophilic so it has a very fast distribution?
Ketamine
Ketamine should be avoided in patients with ?
Head Trauma
Ketamine acts as a ______. It is good in _______ patients.
Cardiac Stimulant
Increased Risk Elderly
Ketamine can cause Emergence Phenomenon which leads to illusions, disorientation, excitation and hallucinations in PACU. How do you combat this?
Combine the drug with Benzodiazepenes.
What was the first local anesthetic?
Cocaine
Local anesthetics prevent ______ from generating leading to no _____ release further leading to the prevention of nerve conduction.
Action Potential
Neurotransmitter
What are the first neurons to be affected by local anesthetics?
small, unmyelinated neurons
MOA of Local Anesthetics are all the same.

Local anesthetics bind to the ________, decreasing _______ into the neuron, which inhibits ________ and ________ generation.
voltage gated Na channels
Na influx
depolarization
action potential
In order to gain entrance into the neuron, the local anesthetic must be in its ______ form?
Un-ionized form
In order to bind to its site of action, and block the Na channel, the local anesthetic must be in its ______ form?
Ionized
What are the routes of administration for local anesthetics?
Topical, Infiltration, or Regional Block
What type of formulations should always be used with spinal and epidural anesthesia?
Those that contain no preservatives and also those that contain vasoconstrictors
Avoid using spinal or epidural anesthesia in patients that are on ____?
LMWH = Low Molecular Weight Heparin
Local anesthetics are weak bases with pKa's between ______. Buffering the local anesthetic solution by increasing the _______ increases penetration to the site of action.
8.0-9.0
Unionized Aspect
Local Blood Flow can affect the _____ of local anesthetics.
absorption
Vasoconstriction of the local blood vessels __ drug removal, __ duration of action, and __ systemic toxicity.
Decreases
Increases
Decreases
Local anesthetics are often mixed with ____ as a vasoconstrictor?
EPI
What conditions do you not use vasoconstrictors with local anesthetic?
PVD, Raynauds, "end artery areas" such as fingers and toes, also spinal/epidural sites. Also, caution should be taken with patients with pre-existing cardiovascular diseases.
The local anesthetic esters contain the suffix _____ .
-caine
The ester local anesthetics are? (5 of them) Hint: C, B, P(N), Ch, T
Cocaine, Benzocaine, Procaine, Chloroprocaine, and Tetracaine
The amide local anesthetics contain the suffix ______, plus an extra _ in the rest of their name.
- caine
- i
The amide local anesthetics are?
Hint: L, M, D, B, R, P
Lidocaine, Mepivacaine, Dibucaine, Bupivacaine, Ropivacaine, Prilocaine
How are the ester local anesthetics metabolized?
They are rapidly hydrolyzed by plasma and tissue esterases.
A special caution with ester is that some patients have atypical plasma cholinesterase enzyme with leads to an
increase duration of action.
Hydrolysis of ester type local anesthetics results in the formation of _____.
PABA
PABA hypersensitivity can occur in patients who are given?
Ester type local anesthetics
PABA can inhibit the actions of _____, therefore you should avoid using _____ on patients taking sulfonamide antibiotics.
Antibiotics
ester local anesthetics
Amide local anesthetics are metabolized via ____ and ____ by liver microsomal enzymes.
Dealkylation
Hydrolysis
If a patient has liver impairment, caution should be taken with amide local anesthetics because?
The liver microsomal enzymes are what metabolize amide local anesthetics. Also, in the process of metabolism, active metabolites can be formed.
Cocaine is isolated from?
The leaves of the Erythroxylon coca tree.
When is cocaine actually used as a local anesthetic?
It is used topically in eye and nose surgeries.
What causes cocaine to have intrinsic vasoconstrictor properties?
Its ability to block NE uptake.
Benzocaine is for _____ use only. It is poorly absorbed due to its low _______, this also means that it has low systemic toxicity.
Topical
water solubility
What is the prototype of the ester local anesthetics?
Procaine
Procaine does not work ______.
Topically
Procaine has a _____ onset of action, and a _____ duration of action.
Short
Short
Chloroprocaine is structurally similar to ______. Chloroprocaine is _____ potent than ______, but _____ toxic.
Procaine
More
Procaine
Less
What ester local anesthetic is used in obstetrics because of its short duration of action and margin of safety?
Chloroprocaine
What drug is more potent than Procaine, but also more toxic?
Tetracaine
Tetracaine is commonly used in _____ anesthesia. It has a ____ onset of action and a _____ duration of action.
Spinal
Slow
Long
What is the most commonly used amide local anesthetic?
Lidocaine
Lidocaine, apart from being used as a local anesthetic, can also be used as an ?
Anti-Arrhythmic
Compared to procaine, lidocaine is ______ potent, ______ onset, and ______ duration of action.
More
Faster
Longer
Lidocaine works in what ways?
HINT: Routes of Administration
Topically, infiltration, and by spinal and epidural routes of administration
When lidocaine is given as an anti-arrhythmic how is it administered?
Via IV
Mepivacaine is similar to _____, but has a ______ onset, and a _______ duration of action.
Lidocaine
Quicker
Prolonged
Mepivicaine is not used _____.
Topically
Dibucaine is used ?
Topically
This drug is commonly used epidurally during labor because it alleviates pain, but it does not affect the motor function of the abdominal muscles?
Bupivacaine
Bupivacaine can sometimes have a rare incidence of?
Cardiotoxicity
This drug has a decreased cardiovascular toxicity compared to Bupivacaine? This drug is also less potent than Bupivacaine, so you need a higher drug concentration.
Ropivacaine
This drug has a longer onset of action than lidocaine, but has a similar duration of action. IT is 40% less toxic than lidocaine.
Prilocaine
Prilocaine is metabolized by the liver and yields _______ . Accumulation of this metabolite can lead to _______?
Orthotoluidine
Methemoglobinemia (Hb3+)
What is the rare occasion that local anesthetics become toxic?
When given in very high doses and administered systemically.
CNS effects of local anesthetic toxicity include agitation, anxiety, shaking, and seizures. This is treated with?
IV diazepam
Systemic toxicities of local anesthetics lead to?
Depression: Sleepiness, respiratory depression, myocardial insufficiency, and systemic hypotension (effects due to medullary depression), Decreased cardiac conduction, pacemaker activity, and strength of contraction, hypotension due to the effects on vascular smooth muscle, and if given via the spinal epidural route, then hypotension is due to inhibition of sympathetic output.
The skeletal muscle relaxants are made up of two dissimilar drug groups, what are they?
Neuromuscular blockers and spasmolytic (antispasmotic) drugs
Neuromuscular blockers are used as?
Paralytic agents during surgery for muscle relaxation and intubation. This allows for a "lighter" general anesthesia.
Neuromuscular blockers do not enter the ______, and they act on the ________.
CNS
Motor end plate
Most of the spasmolytic drugs act in the ______.
CNS
Spasmolytic drugs decrease _______ caused by neurological or moter end plate disease.
excessive muscle tone
Neuromuscular blockers produce blockade of the __________ causing paralysis of ________.
Neuromuscular junction
skeletal muscle
All neuromuscular blockers are given ______.
IV
What is the prototype for the non-depolarizing neuromuscular blockers?
Tubocurarine
What is the only depolarizing neuromuscular blocker in the United States?
Succinylcholine
The MOA for succinylcholine, a depolarizing NMB = succinylcholine (anectine) is an ______ at the _______ receptor.
Agonist
Nicotinic
Succinycholine, depolarizing NMB, initially causes _____ and ______. Normal sustained muscle contraction requires cycles of ______/_______.
Twitches
Fasciculations
Depolarization/Repolarization
Succinylcholine, depolarizing NMB, is given by continuous _______.
Infusion
Succinycholine, depolarizing NMB, causes continous depolarization "flickering" of ______ receptors. This leads to Phase I Block also known as ______.
Nicotinic
Flaccid paralysis
Succinlycholine, depolarizing NMB, Phase I is followed by Phase II which is gradual _______, and desensitization.
Repolarization
What is considered a kind of secondary MOA for succinylcholine, a depolarizing NMB?
It can also "plug up" the Na+ channel
What is the MOA for a non depolarizing NMB?
They block the nicotinic receptor at the end plate.
When a non-depolarizing NMB blocks the nicotinic receptor at the end plate what happens?
Competitive inhibitors prevent opening of the Na channel.
Some non-depolarizing NMB cause _____ of the channel pore at ______ concentrations.
Blocking
Higher
What is a way to overcome non-depolarizing NMB?
Increasing ACh in the synapse by administering AChEIs
What determines the t1/2 life for a non-depolarizing NMB?
The route of metabolism
If a Non-Depolarizing NMB has a short duration it is metabolized by ______.
Plasma Esterases
There is a caution for Non-depolarizing NMB for patients in ____ and ____ failure because these patients have low ____ levels/activity.
Renal and Hepatic
Esterase
With non-depolarizing NMB, one breakdown product can accumulate, enter the _____, and cause ______.
CNS
Convulsions
The short duration non-depolarizing NMB, that are metabolized by Plasma Esterases, are? Hint: 3 of them, A, C, M
Atracurium - can have spontaneous chemical degredation
Cistracurium (Nimbex)
Mivacurium (Mivacron)
What are the two intermediate duration non-depolarizing agents?
HINT: Two of them, R, and V
Rocuronium (Zemuron)
Vecuronium (Norcuron)
Rocuronium (Zemuron) and Vecuronium (Norcuron), the two intermediate duration non-depolarizing NMB, are metabolized in the _____ and excreted in the ______.
Liver
Bile
Long duration non-depolarizing NMB, include these four drugs.
HINT: D-T, D, Pan, Pip
D-Tubocurarine
Doxacurium (Nuromax)
Pancuronium (Pavulon)
Pipecuronium (Arduan)
Most of the long duration non-depolarizing NMB are _____ eliminated.
Renally
What Non-depolarizing NMB agents have a steroid nucleus?
HINT: 2 Intermediate and 2 Long Duration = R, V, Pan, Pipe
Rocuronium (Zemuron)
Vecuronium (Norcuron)
Pancuronium (Pavulon)
Pipercuronium (Arduan)
There is a caution with the non-depolarizing NMB with a steroid nucleus. They can metabolize to a _______ metabolite that can accumulate over several days.
3-Hydroxy
Succinylcholine, a depolarizing NMB = ______ molecules attached. Very rapidly metabolized by ___________. Inactivation by diffusion away from _______. Duration is less than _____.
2 Ach
Plasma Cholinesterase
End Plate
8 Minutes
Succinylcholine, a depolarizing NMB, Phase I blockade is ?
Depolarizing
The succinylcholine, a depolarizing NMB, has a spreading, sustained depolarization leading to _______. This cannot be overcome by AChEIs. AChEIs actually augment the blockade.
Flaccid Paralysis
Phase II blockade, for Succinylcholine, a depolarizing NMB, is ________.
Desensitizing
Phase II blockase, for succinylcholine, a depolarizing NMB, can be overcome by?
AChEIs
With NMB, full respiratory paraylsis occurs so the patient must be?
Ventilated
Non depolarizing NMB, cause motor weakness leading to _______. Larger muscles are affected _____, recover _____. This muscle is the last of all to be affected?
Paralysis
later
faster
Diaphragm
The depolarizing NMB, succinylcholine, has evident _______, paralysis occurs in the ______ leading to the _______. There is very rapid paralysis, less than ____.
Fasciculations
Extremities
Trunk
One Minute
Tubocurarine, a non-depolarizing NMB, has partial autonomic ganglia blockade. This has a cardiovascular effect leading to _____ and _____
Hypotension
Tachycardia
Succinylcholine, a depolarizing NMB, can cause what cardiovascular affects?
First bradycardia (stimulates vagal ganglia) and then tachycardia and hypertension (stimulates sympathetic ganglia)
What non-depolarizing NMB can cause histamine release? This can cause bronchospasm, hypotension, and excessive bronchial secretions.
Tubocurarine
What dangerous effect can succinylcholine, depolarizing NMB, cause? HINT: Potassium
Hyperkalemia, succinylcholine can release K from inside the cells. K is normally situated inside the cells.
This drug is conraindicated in patients with Burns, spinal cord injuries, peripheral nerve dysfunction, muscular dystrophy, heart failure, cardiac arrhythmias and Increased interoptic pressure - especially narrow angle glaucoma?
Succinylcholine
Succinylcholine and Tubocurarine, when combined with general anesthetic can cause what life threatening problem?
Malignant Hyperthermia
Drug interactions for NMB, that cause prolonged NMB, involve what drugs?
HINT: Antibiotics, Heart, Anesthesia
Aminoglycoside antibiotics, antiarrhythmic agents, and inhaled anesthetics (especially isoflurane)
Reversing the non-depolarizing NMB, you use _____, because they compete with NMB.
AchEI (neostigmine, pyridostigmine)
With reversal of NMB, patients must _______ before leaving the O.R., and show a sufficient response to a _____ before extubation. Train of four: ____ impulses over ____ seconds.
breathe independently
peripheral nerve stimulator
Four
Two
What is given in pre-reversal of NMB and why?
Atropine is given to counter act any negative effces of AChEIs, such as bradycardia and salivation.
Spasmolytic drugs are effective in ____ excitatory or enhancing _____ synapse actions.
Decreasing
Inhibitory
Spasmolytic drugs affect the 1A motorneurons which are _____ neurons, that go from _____ to _____.
Afferent
Muscle
Spinal Cord
Diazepam, a benzodiazepene, augments _____ activity at ______ chloride channels.
GABA
GABAa
Diazepam produces presynaptic inhibition of _______? What is the major problem with this?
1A motorneurons
Sedation
Baclofen (Lioresal), a spasmolytic drug, is an _____ at _____ receptors. It Hyperpolarizes via increased ____ efflux. This can decrease sedation.
agonist
GABAb
K+
What is a problem, and a concern, with Baclofen (Lioresal), a muscle relaxant?
Problem: Can increase seizures
Concern: Taper down when discontinuing the drug
What is a spasmolytic drug, that is an a2 agonist, but works via imidazoline receptors? HINT: T
Tizanidine (Zanaflex)
Tizanidine, a spasmolytic drug, causes an increase in both ___ and ___________ in spinal cord.
Pre and Post synaptic inhibition
What are the problems with Tizanidine, a spasmolytic.
Drowsiness, hypotension, and dry mouth
Dantrolene, a spasmolytic drug, acts in ______ to decrease the release of ____ from the ____.
Skeletal muscle
Ca
Sarcoplasmic Reticulum
Botulinum toxin (Botox), used sometimes as a spasmolytic drug, types __, ___, and ___, prevent release of ______ vesicles. The effects of these injections can last up to ____ months.
A,B, and F
Cholinergic
Six
What is the prototype for acute local muscle spasm?
Cyclobenzaprine (Flexaril)
Acute local muscle spasm drugs, such as cyclobenzaprine (flexaril), are ____ that act in the brain stem/cord. They have ____ and _____ actions. These drugs are similar to ______.
Sedatives
Sedative and Antimuscarinic
Tricyclic Antidepressants
What is the most important class of sedative hypnotics and anxiolytics?
Benzodiazepines
Benzodiazepenes can also be used for the treatment of _____ and _____?
Seizures and Anxiety
What is the mechanism of action for benzodiazapenes and Barbiturates?
They potentiate the action of GABA at GABAa receptors.
BDZs bind specifically to their own recognition site on the ______ receptor/Cl- ______ complex.
GABAa
Ionophore
BDZs bind specifically to their own recognition site on the GABAa receptor/Cl-ionophore complex. This leads to an increase in the ________ of Cl- channel opening (increased Cl- influx) by promoting the binding of _______
Frequency
GABA
Increased GABA binding = increased ______ influx = _______ leading to increased inhibitory transmission. GABAa receptor has __ subunits from __ classes.
Cl-
Hyperpolarization
5
8
You need a minimum of alpha-2, Beta-2, and gamma subunites for what?
So chloride channels can function.
BDZ drugs in the brain are classified as either ?
BZ1 or BZ2
Zalepon and Zolpidem, newer drugs, not BDZs, they are a part of the Misc. class, they bind to what selectively?
BZ1
Barbiturates prolong the ______ of opening of the ___ channel by binding to their specific site on the _____ receptor.
Duration
Cl-
GABAa
Barbiturates at increased concentration can block _____ receptors and _____ channels.
Glutamate
Na+
What is a major inhibitor NT in the brain? HINT: G
GABA
GABA is the boss. It controls the __ channel?
Cl-
BDZs are ineffective without ____ present?
GABA
BDZs increase the ______ of channel opening?
Frequency
Barbiturates increase the _______ of openness.
Duration
Advantages of BDZs:
Relatively high __
Low incidence of ___
Slow elimination, active metabolites lead to long _____ __ _____, and better compliance
Low risk of ________, minor withdrawal symptoms.
TI
DDIs
Duration of Action
dependence
Disadvantages of BDZs:
__________ dependence
______ metabolites
Amnesia
Cost
Additive ___ depression
Psychological
Active
CNS
Absorption of BDZs:
P.O. is _______
IM absorption of BDZ is ______
Variable
Erratic
All BDZs cross the _____?
Placenta
Metabolism for BDZs?
Hepatic, extensive metabolism. No induction of liver microsomal enzymes.
Which BDZ has the longest t1/2?
HINT: D
Diazepam (20-90) hours
What BDZ has the shortest t1/2?
HINT: T
Triazolam (1-5) hours
Due to its long t1/2, Diazepam, a BDZ, should not be given to ?
The elderly and liver patients
Many BDZ phase I metabolites are active: Some metabolites have longer ___ than parent.
t1/2
There are nine BDZ, what is the most common suffix, what are the three BDZs that don't have this suffix named?
-epam, Triazolam, Alprazolam, Chlordiazepoxide
Barbiturates are given orally for _______ use?
Hypnotic
IV administration of barbiturates is given for control of __________ or to induce ________?
Seizures
Anesthesia
What is the one barbiturate that is partially excreted unchanged?
Phenobarbital
What are the ultra-short acting barbiturates? HINT: T, Meth
Thiopental
Methohexital
What are the short acting 1-4 hour barbiturates? HINT: S, H, Pent
Secobarbital
Hexobarbital
Pentobarbital
What are the intermediate acting 6-8 hour barbiturates? HINT: Amo, But
Amobarbital
Butabarbital
What are the long acting 10-12 hour barbiturates?
HINT: Bar, Phe, Metha
Barbital
Phenobarbital
Methabarbital
In the elderly and patients with liver disease two things can happen, what are they?
Drug Accumulation
CNS depression
In chronic barbiturate users:
Induction of liver microsomal enzymes leads to an increase in _______ metabolism, and development of _______.
Hepatic
Tolerance
Barbiturate elimination is via the ______, much drug may be reabsorbed from the _____ ______.
Kidney
Renal Tubule
You can alkalinate the urine of a patient to enhance elimination of barbiturates by using what?
NaHCO3
What is the only barbiturate that doesn't accumulate in the body when given daily? HINT: HEX
Hexobarbital
Sedatives are ____ dependent?
Dose
Pharmalogical Effects: Hypnosis:
Essentially no psychomotor ______, good if _____ ______. These produce _____ at a somewhat higher dose. Patients fall asleep faster. _ ___ sleep for insomniacs, tolerance with over two weeks use unless you are treating _____.
Depression
giving everyday
Sleep
Decreased REM
Anxiety
What two barbiturates are used for anesthesia, are highly lipophilic and are short acting due to rapid redistribution? HINT: Thi, Met
Thiophental
Methohexital
What two BDZs act as anesthesia adjuncts, have longer lasting effects, and are reversed with flumazenil? HINT: D, M
Diazepam
Midazolam
Most of the sedative/hypnotic drugs can decrease the spread of _______ activity in the brain?
Seizure
What BDZs are good for treating seizures? HINT: 4 of them, N, L, Cl, and D
Nitrazepam
Lorazepam
Clonazepam
Diazepam
What two barbiturates are good in treating seizures? HINT: P, Meth
Phenobarbital
Methabarbital
What is a prodrug of phenobarbital, a barbiturate?
Methabarbital
What drugs in combination are good for muscle relaxation? HINT: Car, Benz
Carbamates
BDZs
What is the method of action for the combination of Carbamates and BDZs?
Decrease neuronal transmission, believe to inhibit 1A activity
What drugs are primarily responsible for overdose deaths in the sedative-hypnotic/anxiolytic drugs?
Barbiturates, due to respiratory arrest. This is due to effects on the medullary respiratory center.
What problems can result cardiovascular from the sedative-hypnotic/anxiolytic drugs?
Hypovolemia, CHF, and decreased cardiac contractility
______ is common with both BZDs and Barbiturates? You can increase dose if necessary.
Tolerance
Cross tolerance with other sedative/hypnotic drugs can occur, also can occur with ____.
ETOH
Cause of tolerance in these drugs is unknown?
Barbiturates
Abrupt D/C, of sedative/hypnotic drugs, leads to generalized ____ withdrawal symptoms. These withdrawal symptoms may include what?
CNS
REM rebound, insomnia, agitation, excitation, tremulousness, weakness, delierium, high risk of seizure and death.
What is one of the most important reasons that you have to withdrawal a patient slowly from sedative/hypnotic drugs?
The high risk of seizures.
What are the four newer sedative-hypnotic drugs?
HINT: Bus, Zol, Zal, Esz
Buspirone (Buspar)
Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)
What is Buspirone used for?
Anti-Anxiety
Buspirone has no strong sedative effets, it is not hypnotic, anticonvulsant, or a muscle relaxant. it is a partial agonist at _____ receptors. It has no effect on ___ or ___ binding sites. it is not useful in ____ _____.
5HT1a
GABA
BDZ
Panic Attacks
Zolpidam (Ambien), is not structurally related to ___.
BDZs
Zolpidem (Ambien) is a hypnotic (___-________) that facilitates ____ inhibition.
BZ1-selective
GABA
Zolpidem (Ambien) is used for the treatment of ______. it decreases ____ sleep. It is not a muscle relaxant or an anticonvulsant. Respiratory depression is seen with an increased dose, especially with ____?
Insomnia
REM
ETOH
Zolepidem (Ambien) is less likely to produce tolerance than BDZs, you have to decrease the dose for _____, _______, and patients taking _______.
Elderly
Liver Disease
Cimetidine
Zaleplon (Sonata) is like _____ but has a t1/2 of _______. it is rapidly metabolized by _____ _____ and ______.
Ambien
1 Hour
Aldehyde Oxidase
CYP450
Zaleplon (Sonata) decreases _____ _____, which makes it good for patients with difficulty _____ _____, but may not be useful in maintaining _____.
Sleep latency
Falling Asleep
Sleep
Eszopiclone (Lunesta) is the newest non-___ hypnotic believed to act at the ___-___ receptor.
BDZ
GABA-BDZ
Eszopiclone (Lunesta) has a rapid onset (peak levels _ __ after dose) and a t1/2 of _ __.
1 hr
6 hrs
Eszopiclone (Lunesta) is used for the treatment of ______, and its pharmalogial effects and side-effects are similar to ____.
Insomnia
BDZs
Older, Hardly ever used drugs:
Alcohols:
Chloral hydrate (Noctec): Is metabolized by the ____ to _________ ____ (a toxic metabolite that accumulates)
Liver
Trichloracetic Acid
Piperidinediones:
Glutethimide (Doriden): Now a schedule II drug due to _______/________
High abuse/addiction potential
What are the carbamates?
Meprobamate (Miltown, Equanil)
What are the most commonly used drugs for anxiety states?
BDZ of intermediate/long t1/2
When diagnosing anxiety you have to determine if anxiety state is _______ or ______.
Secondary
Situational
What is a good drug for panic/phobic attacks? HINT: A(X)
Alprazolam (Xanax)
Buspirone is a great drug for anxiety, but it takes what? And it is not good for what?
It takes a week for the effect to begin.
It is not good for panic attacks.
when treating anxiety you have to use ____ doses for ____ periods. Caution patients about addictive effects with ____, and other _____ ____, ex. antihistamines.
Low
Short
Alcohol
Sedative Drugs
What drugs are best for sleep disorders, and what do you have to do on D/C? HINT: Est, Tri, Zol, Zal
BDZs with short t1/2 estazolam (pro-som), triazolam (halcion), Zolpidem (ambien) and zelplon (sonata)
Taper drugs on D/C or pt. can get rebound insomnia.
What is a barbiturate, used as a pre-anesthetic agent?
Thiopental
What two BDZs are used as components of anesthetic mixtures?
Diazepam (Valium), Midazolam (Versed)
What are two drugs, BDZ and Barbiturate, used as anticonvulsants?
Clonazepam (Klonopin), Phenobarbital
Diazepam lorazepm (Ativan) is used for ____ _______.
Status Epilepticus
Diazepam et al. can be used as?
Muscle relaxants.
Chlordiazepoxide (Librium), diazepam can be used for ______ ________/________.
Alcohol withrdawal/detoxification
Flumazenil (Romazicon) is a competitve antagonist of what?
BDZs and Zolpidem
Decrease doses of hypnotic/sedatives in what patients?
Cardiovascular
Respiratory
Liver Disease
Sleep Apnea
Higher doses of hypnotic/sedatives can cause what?
Lethargy, drunkeness, and behavioral problems (aggression)
What is a major problem with Flumazenil if given to patients who are long term users of BZDs, and have developed a dependence on BZDs?
It will precipitate withdrawal syndrome.
Is there a direct antidote for barbiturates?
NO!
What is the DSM-IV Criteria for diagnosing depression?
5 or more symptoms for at least 2 weeks and represent a change from previous functioning.
How long does it take for improvement to be seen with tricyclic antidepressants or MAOIs?
Even they they act fairly quickly, it takes like 2-3 weeks for these drugs to show signs of clinical improvement.
What are the four classes of anti-depressants?
Tricyclic antidepressants
Heterocyclics: 2nd and 3rd Gen.
SSRIs
MAOIs
All four classes of the antidepressants ptentiate the central action of __, __ or both?
NE
5-HT = Seratonin
What types of antidepressants have three rings and a similar strucure as phenothiazines (antipsychotics)?
Tricyclic Antidepressants
What are the two prototypes of tricyclic antidepressants?
HINT: IMI, AMI
Imipramine (IMI; Tofranil)
Amitryptiline (AMI; Elavil)
Imipramine and Amitriptyline, tricyclic antidepressants, are second favorite drugs to use compared to what other type of antidepressant?
2nd Favorite to SSRIs
Tricyclic antidepressants, MOA, block the re-uptake of __ and ___ by presynaptic nerve terminals. This increases __ and ___ available to interact with post synaptic receptors.
NE
5-HT
NE
5-HT
What are one of the dangers when using TCAs compared to SSRIs?
TCAs are very toxic and can be used successfully to perform suicide. If concerned for a patient it is best to give them a week's worth of an SSRI and then re-evaluate the patient.
TCAs are well absorbed __, they have widespread distribution and are highly bound to plasma proteins.
PO
TCAs have long half lives and can be problematic in overdose. They are highly toxic at higher blood levels. An example of this is ______ that has a t1/2 of ____.
Protriptyline
80 Hours
TCAs are metabolized via ______ (demethylation), then glucuronidation. Many have active _______.
CYP450
Metabolites
The CNS effects of TCAs:
In _________ individuals, feelings of dysphoria, anxiety and sedation, and difficulty concentrating and thinking. ____ ________ are corrected, and some _____ can be experienced.
Non Depressed
Sleep Disturbances
Sedation
Dry mouth, blurred vision, constipation, and urinary retention (due to blockade of muscarinic cholinergic receptors) are the results of what types of effects caused by TCAs?
Anticholinergic Effects
TCAs can cause what kind of cardiovascular effects?
Postural (orthostatic) Hypotension (due to peripheral a blockade)
Tachycardia (due to cardiac muscarinic receptor blockade and inhibition of NE reuptake)
What type of serious toxicity can occur because of TCAs, and should be avoided in such patients?
Cardiotoxicity
Cardiac patients
TCAs can also cause excessive sweating, weight gain, transition to manic excitement, can precipatate glaucoma, esp. in elderly with ____ _____ _____.
Narrow Angle Glaucoma
TCA is a common drug used in suicide attempts. It can cause SEVERE ________ _____.
Anticholinergic effects
What is the treatment for overdose of TCAs
Gastric lavage, activated charcoal, NaHCO3, diazepam and/or physostigmine (AChEI)
What are a few other indications for the use of TCAs?
Enuresis
Agorophobia
OCD
Neurogenic Pain
What drug must you never use with TCAs?
MAOIs, this leads to hyperpyrexia, convulsions, and death. Also Seratonin Syndrome
What syndrome, a rare but fatal drug interaction, is due to excessive 5-HT and results in HTN, Tachycardia, Hyperthermia, and Myoclonus
Serotonin Syndrome
Is there a specific antidote for Serotonin Syndrome?
No
What is the only treatment for serotonin syndrome?
Supportive treatment and discontinuing precipitating drugs. May also give cyproheptadine. Cyproheptadine is an antihistamine that blocks some serotonin receptors. BDZs can help control symptoms.
What are the second generation Heterocyclics or atypical antidepressants. HINT: Amo, Mapro, Traz, Bupro
Amoxapine (Asendin):NE reuptake blocker
Maprotiline (Ludiomil):NE reuptake blocker
Trazodone (Desyrel):5-HT reuptake blocker
Bupropion (Wellbutrin):???
What is Trazodone (Desyrel), a second generation heterocyclic/atypical antidepressant is used for what by exploiting its side effect?
It is used for insomnia, due to the fact that it causes drowsiness.
What are the third generation Heterocyclic/Atypical antidepressants?
HINT: Ven, Mir, Nefaz
Venlafaxine (Effexor): Blocks reuptake both of NE and 5-HT, but 5-HT more
Mirtazapine (Remerol):5-HT reuptake
blocker plus it increases amine release (a2 blocker)
Nefazodone (Serzone):5-HT reuptake blocker
Amoxapine (Asendin), a second generation heterocyclic antidepressant, has a __ antagonist effect which means it has a _________ effect?
DA = Dopamine
Antipsychotic
Amoxapine (Asendin), a second generation heterocyclic antidepressant, can cause what types of symptoms?
Akathisia, parkinsonism, tardive dyskinesia, and amenorrhea-galactorrhea syndrome can occur.
Maprotiline (Ludiomil), a second generation heterocyclic antidepressant, is a strong __ reptake blocker. It causes decreased sedation, antimuscarinic effects vs. older TCAs.
NE
Trazodone (Desyrel), a second generation heterocyclic antidepressant, is a selective blocker of ________ uptake with only weak effects on catecholamine uptake. It is a good hypnotic but has a side effect in men which is _______. This drug may be best given to women
Serotonin
Priaprism
Bupropion (Wellbutrin, or Zyban), a second generation heterocyclic antidepressant. What is Wellbutrin used for? What is Zyban used for? What is there a high risk of when using this drug, especially in increased doses?
Wellbutrin = Depression tx
Zyban = Smoking tx
Seizures
Nefazodone (Serzone), a third generation heterocyclic antidepressant, Is like trazodone but less sedating. There are fewer _____ _____ _____ vs. other SSRIs, but this drug is a ____ inhibitor so there are a lot of DDIs.
Sexual side effects
CYP450
Venlafaxine, a third generation heterocyclic antidepressant, is like ____ at low doses. At higher doses it can _ pulse, and BP. So it is sympathomimetic.
SSRIs
Increase
Mirtazapine (Remerol), a third generation heterocyclic antidepressant, has strong __________ effects: It is more sedating than other heterocyclics. It can cause what physical change?
antihistamine
weight gain
SSRIs = She flew plains to central florida every day.
She = Sertraline (Zoloft)
Flew = Fluoxetine (Prozac)
Planes = Paroxetine (Paxil)
to
Central = Citalopram (Celexa)
Florida = Flovoxamine (Luvox)
Every = Escitalopram (Lexapro)
Day = Duloxetine (Cymbalta) = an SNRI
What was the first SSRI? It had minimal autonomic toxicity.
Fluoxetine (Prozac)
SSRIs have fewer side effects than ___, and ________?
TCAs
Heterocyclics
Fluoxetine (prozac), an SSRI, has a t1/2 of ______, and also has _____ metabolites. Fluoxetine is a ______ inhibitor causing many DDIs.
2-9 days
Active
CYP450
What are other indications for SSRI?
HINT: PA, SP, Bul, WL
Panic Attacks
Social Phobias
Bulimia
Weight Loss
Adverse reactions and DDIs of SSRIs include nausea, decreased libido, sexual dysfunction, Seratonin syndrome with ____? This combination is a deadly one.
MAOIs
SSRIs are very safe in comparison to ___ and ____, it is the drug of choice for ________.
TCA
MAOIs
Depression
MAOIs = TIP
Tranylcypromine (Parnate)
Isocarboxazid (Marplan)
Phenelzine (Nardil)
All of the MAOIs have a long duration of action. What is the DOA for Tranylcypromine, Isocarboxazid, and Phenelzine?
7 days
2-3 weeks
2-3 weeks
MAOIs are irreversible ______.
Inhibitors
All of the MAOIs have ________ effects.
Sympathomimetic
The MOA for MAOIs is that they block _______ ________ of ________ and 5-HT by MAO (A and B isoforms; non-selective)
Oxidative Deanimation
Catecholamines
Type A MAOIs typically block reuptake of what three things?
NE, 5-HT, Tyramine
Type B MAOIs typically block reuptake of what?
Dopamine
What type of MAOI, A or B, is known for having an antidepressant effect?
MAOa, Type A
Inhibition of MAOa, prevents _______ of NE, 5HT in neuronal cytoplasm which leads to an _ in molecules surviving to enter vesicles leading to _ molecules being released into the synapse
degradation
increase
increase
Adverse reactions of MAOIs
Postural hypotension
Liver toxicity
DDIs with TCA and SSRIs which can cause Serotonin syndrome
What is something that must be done in order to avoid problems with TCA, SSRI or Meperidine?
You have to allow for at least a 2 week wash out period. If this is disregarded death can result.
MAOIs can cause dangerous drug-food interactions. What specific problem can result?
Tyramine hypertensive crisis
PTs on MAOIs should avoid eating what foods?
Aged cheeses, red wine, beer, pickled herring, chicken liver, snails, yeast, chocolate, coffee, canned figs, fava beans, avocados and bananas
With this type of seizure the patient doesn't lose consciousness when the seizure starts.
Partial Seizures
What type of seizures occur when a patient loses consciousness instantaneously at the start of the seizure?
Generalized Seizures
Simple Partial Seizures, Complex Partial Seizures, and Partial Seizures secondarily generalized are examples of what type of seizures?
Partial Seizures
The etiology of seizures is usually ______. Although, seizures can be considered to be ______ due to channelopathies.
Idiopathic
Genetic
Causes of seizures can stem from ______ _______ _____ : Head trauma (acute), or CNS infections/tumors. Post Traumatic Epilepsy can occur after ____ years. Neurochemical/Metabolic disorders can cause epilepsy, such as ____ ____ ____. Also _________ diseases.
Elevated Intercranial Pressure
3-5 years
Low Blood Sugar
Neurogenitive
SEIZURE MECHANISMS:
"____ ____" by neurons occurs. An influx of _____ causes an opening of voltage dependent __ channels. There are bursts of action potentials. This causes a hypersynchronization and recruitment of neighboring ______.
Burst Firing
Ca
Na
Neurons
The key to preventing seizures is to prevent ________.
Hypersynchronization
Primary generalized seizures start in the _____ and then spread out.
Thalamus
Partial Seizures:
Pt is not _______, at least at outset. Localized onset that is determined by symptoms or EEG. The focus is in the brain; often the temporal lobe. It may spread or not.
Unconscious
What are the three types of partial seizures?
Simple Partial
Complex Partial
Partial with secondary generalization
Simple partial seizures are characterized by?
Patient remains conscious, has sensory, autonomic, motor or psychic symptoms.
Complex partial seizures are characterized by?
Patient is conscious initially, may become confused. Motor symptoms start regionally, may spread unilaterally or bilaterally. Automatisms and Aura.
What is Aura?
Smelling something, bright flashes, etc. This gives a patient an indication to find a safe place to lay down.
Generalized Seizures
Generalized Tonic-Clonic (Grand Mal)
Absence Seizures (Petit Mal)
Lennox-Gastaut Syndrome (variant absence)
Myoclonic Seizures
Atonic Seizures
Unclasssified
Infantile Spasms
GTC: Gran Mal is characterized by?
Ca 2+ channel blockers, tonic = rigid, clonic = jerking motions; urinary incontinence.
Characteristics of Absence Seizure (Petit Mal)?
Brief 10-45 seconds, with a loss of conscious. Staring, pause in converation. Minor motor symptoms. More common in children. Characteristic 2.5-3.5 Hz spike and wave pattern on EEG. These are seen a lot in the elderly.
Lennox-Gastaut Syndrome is characterized by?
Triad of seizure types - GTC, atonic and absence. Slow wave on EEG, Poor prognosis: due to brain abnormality. This is usually seen with children who have brain malformations.
Myoclonic Seizures are characterized by?
Jerking (single or repetive), Often seen in combination with other seizure types. Early Adolescence (JME), In AM, good prognosis with drugs.
Atonic seizures are characterized by what?
Sudden loss of postural tone. Dropping/falling down. Dangerous: Head injury/wear helmets.
Status Epilepticus is characterized by?
Motor or "absence continuing", medical emergency, antiseizure drugs include anesthetics and ventilator.
AEDs are usually taken for ____. Thus toxicity and DDIs are a major concern.
Years
AED MOAs = Repress repetitive firing in _____ ___, or block the _____ of abnormal electrical activity to adjacent neurons.
epileptic foci
spread
Phenytoin (Dipehnylhydantoin; Dilantin) Very effective for ______ and _____. MOA = Voltage-dependent __channel blocker. Blocks high frequency repetitive firing by stablizing the inactive state of the Na channel. Does not block normal firing.
Partial
GTC
Ca
Phenytoin PK is _____! Zero order elimination in the therapeutic range. It is non-linear, oral bioavailability variable, undergoes ___-____ metabolism, 97-98% _____ bound.
Horrid
First-Pass
Protein
Phenytoin has DDIs with drugs that compete for ___ ____ binding sites.
Plasma Protein
Phenytoin is metabolized by CYP___ and ___, so inducers therof cause increased elimination and therapeutic failure. Inhibitors thereof cause slowing of elimination and toxicity.
2C9
3A4
The adverse reactions of Phenytoin include ______, ataxia, _______ hyperplasia. Idiosyncratic reactions include rash, lymphadenopathy, and in rare cases agranulocytosis.
Diplopia
gingival
What is a water soluble pro-drug of Phenytoin? It is expensive but worth it.
Fosphenytoin (Cerebyx)
Carbamazepine (CBZ; Tegretol) is very effective for _____ and ______ seizures?
Partial
Generalized TC
Carbamazepine (CBZ; Tegretol) blocks voltage dependent __ channels. It is an inducer of CYP___. It causes many drug interactions. It is also used for trigeminal neuralgia and bipolar disorder
Na
3A4
The adverse reactions of Carbamazepine (CBZ; Tegretol) includes Diplopia, _____, idiosyncratic agranulocytosis, and _____ anemia.
Ataxia
Aplastic
Oxcarbazine (Tileptal), is similar to _____, but less ____.
Carbamazepine
Potent
Oxcarbazine (Trileptal) blocks voltage dependent __ channels. It is safer and has fewer idiosyncratic reations. It has less CYP___ induction.
Na
450
This is the oldest anti-epileptic drug; it is effective but highly sedative?
Phenobarbital (Pb)
Phenobarbital is a _____ enhancer.
GABA
What seizures might be worsened by the use of Phenobarbital?
HINT: A, A
Absence and Atonic
What anti-epileptic drug is metabolically converted to phenobarbital? This drug has a voltage dependent __ channel blockade.
Primidone
Na
Diazepam (Valium), is used for ____ _____ rectally.
Status Epilepticus
Lorazepam (Ativan) is used for ____ ____ and has a longer duration than ______.
Status Epilepticus
Diazepam
What benzodiazepam is useful in combating absence and myoclonic seizures? It is potent and has a long acting effect. Although it can be sedative.
Clonazepam
Clorazepate dipotassium (Tranxene) has an adjunctive use for complex _____ seizures.
Partial
Lamotrigine (Lamictal) is for ____, ____ and ______ seizures.
Partial
Absence
Myoclonic
Lamotrigine (Lamictal) blocks voltage dependant __ channels. It may act on Ca channels. The ARs are the usual CNS effects that include what?
Na
Ataxia, Droginess
Lamotrigine can cause rashes, especially in ______.
Children
Topirimate (Topamax) has _ possible MOAs.
3
Topirimate (Topamax) is bested for partial and GTC seizures, as well as ______ and _____-_____.
Absence
Lennox-Gastaut
What are the three MOAs for Topirimate (Topamax)?
Blocks voltage dependent Na channels
May enhance GABA action
Decreased effect of Kainate (excitatory amino acid analog) on AMPA receptor.
What are the ARs for Topiramate (Topamax)?
The usual CNS effects, plus nephrolithiasis.
Zonisamide (Zonegran), is a sulfonamide. This means that there is a danger of this causing a ____ that could lead to _____-______ syndrome
Rash
Steven's-Johnson's
What is Zonisamide (Zonegran) used for?
Partial and GTC seizures, myoclonic and infantile spasms
What is the MOA for Zonisamide (Zonegran)?
Blocks voltage dependent Na channels.
Levetiracetam (Keppra) has an unknown MOA. It is an adjunct for ____ seizures. It is not metabolized by CYP___, so it means there are fewer DDIs with its use.
Partial
450
Felbamate (Felbatrol), is a very ____ drug.
risky
Felbamate is toxic and can cause ___ _____. It is reserved for refractory cases and has restricted prescribing.
aplastic anemia.
Gabapentin (Neurontin), considered an ___ __ ___ is an amino acid like GABA itself. Its MOA is unknown. It is a adjunctive drug for ___ and ___ seizures, it is also used for ______ pain. It has minor side effects that include sleepiness, dizziness and ataxia.
Add on Drug
Partial and GTC
Neuropathic
Tiagabine (Gabatril) is a _____ uptake inhibitor. It is adjunctive for ____ seizures. It has minor ARs and idiosynycratic rash.
GABA
Partial
Vigabatrin (Sabril), is an irreversible ___-_ inhibitor. It is for ____ seizures. It has renal elimination which means that it less likely to have ___. It can cause drowsiness, etx. psychosis.
GABA-T
Partial
DDIs
What is a major AR of Vigabatrin (Sabril)?
It can cause irreversible visual field damage.
Who should you never give Vigabatrin to?
Someone who is a Psych patient.
Ethosuximide (Zarontin) is the DOC for what kind of seizures?
Absence
What is the MOA for Ethosuximide (Zarontin)?
It decreases T-currents (calcium); pacemaker in thalamus
What is a DDI for Ethosuximide (Zarontin)?
Valproate inhibits ethosuximide metabolism
ARs for Ethosuximide (Zarontin) include GI pain, the usual rash, and in rare cases ____-_____ ______.
Steven's-Johnson's Syndrome
Valproic acid/Valproate (Depakene; Depakote [SR]) is the DOC for _____ in combination, ___, and ______ seizures.
Absence
GTC
Myoclonic
What is the MOA for Valproic acid/Valproate?
It isn't fully known but it may be a calcium channel blockade.
The DDI's for Valproic acid/Valproate include what?
it inhibits metabolism of PHT, CBZ, PB, LTG, also displaces PHT from plasma proteins.
The ARs of Valproic acid/Valproate are usual, plus idiosyncratic ______.
Hepatotoxicity.
The formation of toxic metabolites occur, you have to monitor the LFTs of this anti-epileptic drug. The rule of thumb for administering this drug is "start low, go slow".
Valproic acid/Valproate.
Valproic acid/Valproate can cause what tetratogenic problem?
Fetal Hydration Syndrome
What are the other three treatments for epilepsy?
Ketogenic Diet
Surgery
Vagal Nerve Stimulation.