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207 Cards in this Set

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what are the 3 primary mechanisms of axn for Antiepileptic drugs?
1. Enhance inhibitory neurotransmission via GABA stimulation
2. Stabilize cell membranes & surrounding cells (Na/Ca/K channels)
3. Reduce excitatory neruotransmission via antagonism of Glutamate
According to AAN guidelines, what "new" AED drugs are recommended as initial therapy for newly diagnosed Epilepsy?
Lamotrigine (LAMICTAL), Gabapentin (Neurontin), Oxcarbazepine (Trileptal)& Topiramate (TOPAMAX)
La Neu Tri Top
Which old AED's are recommended for intial use of newly diagnosed Epilepsy?
Cabamazepine (TEGRETOL), Phenytoin (DILANTIN), Valproic Acid (DEPAKOTE)& Phenobarbital
Which new AED's are used primarily as adjunct therapies & why?
Tiagibine (GABITRIL), Zonisamide (ZONEGRAN), Levetiracetam (KEPPRA); b/c insufficient evidence to be used as primary tx for new pts.
What steps should be taken before changing to a 2nd AED choice when pt has failure with 1st AED therapy?
Check diagnosis, Check compliance, Check for drug &/or alcohol abuse, check for underlying neoplasm (eg. CA or brain tumor)
What were all "new" AEDs originally approved for?
As adjunct treatment of partial or General Tonic Clonic (GTC) seizues.
_____ &_____ Can be used as monotherapy for refractory partial epilepsy according to AAN guidelines (HINT: New)
Oxcarbazepine (TRILEPTAL) & Topiramate (TOPAMAX); Went back and got approved as monotherapies
What drugs can be used as adjuncts in CHILDREN with refractory partial seizures?
Gabapentin (NEURONTIN), Lamotrigine (LAMICTAL), Oxcarbazemine (TRILEPTAL) & Topiramate (TOPAMAX)
What pregnancy category are the NEW AEDs?
Pregnancy Category C
What pregnancy category are the OLD AEDs?
Pregnancy Category D
What drugs should be used w/ Lennox- Gastaut Syndrome?
Topiramate (TOPAMAX) & Lamotrigine (LAMICTAL)
Which AEDs do not markedly increase metabolism of birth control pills?
VPA (DEPAKOTE), Topiramate (TOPAMAX) & Oxcarbazepine (TRILEPTAL)
What is the drug of choice for treatment of neonatal seizures?
What is Phenobarbitals Mechanism of Axn?
It increases seizure threshold & stimultes GABA
What is a unique feature of Carbamazepine?
It is an autoinducer; Hepatic enzyme inducer of its own metabolism.
What are the CONCENTRATION related adverse effects of Carbamazepine?
Diploplia, nausea, sedation, ataxia & dizziness
What are the IDIOSYNCRATIC adverse effects of Carbamazepine?
HYPOnatremia, blood dyscrasias, aplastic anemia & rash--> Stevens Johnson Syndrome
What is Carbamazepine's MOA?
Modulates Na+ ion channels
What is Phenytoins MOA?
Modulates Na/ Ca ion channels-- Has nonlinear pharmacokinetics!!
Estrogen is considered to be seizure ______, while Progestrin is considered to be seizure ______.
Activating, Protective.
What was the first treatment for Epilepsy?
Potassium Bromide (1857)
What AED was discovered accidentally as an effective treatment in the 1960's?
Valproic Acid-- originally used as a solvent to clean floors.
What are the 3 major electrolytes that are involved w/ seizure activity?
Na, Ca, & K
Which are inhibitory & which are excitatory?
GABA, Glutamate, Aspartate
Inhibitory, Excitatory, Excitatory
What is the name of the receptor where Glutamate binds?
NMDA receptor; when constantly exposed to glutamate can "burn" out.
What are the 2 major classifications of seizures?
Partial & Generalized
Name the types of partial seizures and how they differ.
Partial originates in 1 hemisphere--
*Simple partial: Consciousness is NOT impaired
*Complex partial: Consciousness IS impaired
What type of seizure involves both hemispheres of the brain and where consciousness is ALWAYS impaired?
What is another name for partial seizures?
FOCAL seizures
What is the most important predictor of remission in epilepsy?
Number of seizures within the first 6 months of treatment
What percentage of seizure patients are started on AED after their 2nd seizure?
80-90% b/c seizure reoccurence is only about 30-60% after 1st seizure.
What is the goal of treatment for epilepsy?
No Seizures and No side effects.
Which AED is a potent enzyme INHIBITOR & can double the half-life of Lamotrigine (LAMICTAL)?
Valproic Acid/ Divalproex Sodium (DEPAKOTE)
What is Lamotrigine's (LAMICTAL) MOA?
Modulates Na/ Ca channels, aspartate/ glutamate activity (excitatory neurotransmitters)
What is Levetiracetam's (KEPPRA) MOA?
Modulates Ca & K channels & GABA (Inhibitory neurotransmitter)
Which AED is considered relatively non-toxic and has virtually no side effects?
Levetiracetam (KEPPRA)
What is the advantage or using Oxcarbazepine (TRILEPTAL) over Carbazepine (TEGRETOL)?
Oxcarbazepine is not an autoinducer as Carbazepine is.
HYPOnatremia is reported more with Oxcarbazepine or Carbazepine?
Oxcarbazepine-- especially in at risk patients eg. Elderly
Which "new" AED causes the most cognitive impairment?
Topiramate (TOPAMAX)
What are the 4 common Concentration- related side effects of Phenytoin (DILANTIN)?
Nystagmus, Ataxia, Confusion & DEATH
What does GCSE stand for?
Generalized Convulsive Status Epilepticus
What is the number one cause of GCSE?
Non compliance or abrupt withdrawal from drugs-- esp Antiepileptic drugs.
What are the 4 immediate goals of treatment of GCSE?
1. Stabilize pt & maintain ABC's
2. Make dx & identify te precipitating factors
3. Terminate seizure ASAP
4. Prevent seizure recurrence
What are some nonpharmacological treatments for GCSE?
Air (O2) administration, correct metabolic acidosis if necessary, Check EEG for electrical disturbances, Give 100 mg Thiamine then glucose (50cc dextrose to adults)
What are the most commonly used drug classes for treatment of GCSE?
Hydantoins (Phenytoin), Benzodiazepines & Barbituates
What is the benzodiazepine of choice according to the Epilepsy Foundation of America?
Lorazepam (ATIVAN)-- not as lipophilic as diazepam but has longer duration of axn!
What is a major consideration when utilizing Diazepam (VALIUM) & Lorazepam (ATIVAN) in IV form?
Both contain propylene glycol-- a cardiac depressant; can cause cardiac arrythmias & hypotn is used too rapidly
Why is the history of the seizure important when diagnosing GCSEs?
Gives nature & duration of seizure
What are the major pathophysiological markers of Phase I GCSEs?
*Increse in Epinephrine, NorEpi, cortisol
*Metabolic demands are increased
*HTN, tachycardia, arrythmias
*Cerebral perfusion & blood flow preserved
*Increased secretions/ airway obstruxn
What are the major pathophyiological markers of Phase II GCSEs?
*Glucose is low- normal
*Hyperthermia, Hypoxia & possible respiratory failure developemt
*Increase in sweating, salivation, prolactin, GH & ACTH
*Motor activity may cease but electrical activity will persist
With regard to Status Epilepticus patients, what drug do some recommend as first line out of hospital treatment? And why?
Midazolam (VERSED)b/c well tolerated, doesn't need to be diluted, causes minimal changes in BP, RR & has no cardiac depressant effects
Why must Phenytoin (DILANTIN) be diluted in normal saline?
b/c it precipitates in glucose containing solutions.
What are some advantages of Fosphenytoin (CELEBYX) over Phenytoin (DILANTIN)? (3)
1.Is water soluble ester form of phenytoin, more compatible w/ IV fluids
2. NO propylene glycol,less likely to cause arrythmias & Hypotn
3. Can administer more rapidly & is rapidly converted to Phenytoin after IM/IV administration.
What population is Phenobarbital typically used in?
Seizure termination most likely involves _______.
_______ controls Cl Channels & causes post synaptic hyperpolarization while______ (pre & post synaptic) inhibits release of excitatory amino acids
GABA-a receptor
GABA-b receptors
Define Chorea
Ongoing, rapid & irregular flitting movements that appear willful but are involuntary & dancelike.
What is a festinating gait?
Involuntary acceleration of ones gait (walk)
Handwritting that decreases in size
Substantia Nigra
Dopamine producing nerve cells located in the brain stem that control voluntary movement.
Mass of gray matter that includes the putamen & caudet
A mask-like face with little expression
Abnormal involuntary movements that typically are medication induced.
What are thought to be the environmental contributing factors in the development of Parkinson disease?
Rural living, drinking well water, heavy metal & hydrocarbon exposure
What are thought to be protective factors in the development of Parkinson disease?
Cigarette smoking, caffeine consumption & NSAID use.
MTPT is broken down by this enzyme producing this damaging ion.
Monamineoxidase B & MPP ion
MPP ion is damaging because...?
It interferes with Mitochondrial Metabolism of neurons in the Substantia Nigra.
What are the hallmark signs of Parkinson disease?
TRAP= Tremor (at rest) Rigidity, Akinesia & Postural Changes.
What is the difference between Essential tremor and tremor at rest?
Essential tremor occurs when not at rest.
GABA is a/an_________ neurotransmitter.
Glutamates is a/an __________ neurotransmitter.
Loss of D2 receptor function in the brain is responsible for loss of this type of muscle control.
Caudate Nucleus
Affects coordinated movement
Putamen & Caudate Nucleus
(Both responsible for movement) Comprise the Striatum
Substantia Nigra
Generates DOPAMINE which regulates reward and movement
Basal Ganglia
Comprised of Striatum, putamen, caudate nucleus, globus pallidus, subthalmic nucleus & substantia nigra
Responsible for relaying auditory, sensory, visual signals & movements into cerebral cortex
Cerebral Cortex
Manages higher brain function such as voluntary movements, sensation, reasoning and memory
Globidus Pallidus
group of nerves deep in the brain affecting movement, balance and walking
regulates movements; adrenaline is a derivative of dopamine. Decreased dopamine is assoc'd w/ PD; lose ihibitory effect--> Tremor at rest.
functions as INHIBITORY neurotransmitter; regulates sleep and anxiety
functions as EXCITATORY neurotransmitter
Substance P
Transmits pain impulses from body to CNS
Hormones release from the brain that bind certain receptors to supress pain and effect emotion.
manufactured in CNS & parasympathetic nervous system & is important for memory and learning
With a decrease in Dopamine, Acetylcholine has a ________ effect.
GREATER effect--> Tremor at rest.
What is Allodynia?
Painful response to what is normally nonpainful stimuli, eg. light touch, change in temp. etc.
List 3 examples of Neuropathic pain.
1.Post herpetic neuralgia
2. Phantom limb pain
3. Diabetic neuropathy
Neuropathic pain is generally less responsive to ______ alone.
With acute pain, its intesity is usually_____ to the degree of damage.
What are the beneficial effects of the acute injury response? (4)
1. Maintain perfusion
2. Enhanced energy produxn
3. Immobilization; minimizing further tissue injury
4. Learned avoidance
What are the adverse effects of acute injury response? (7)
2.Cardiac Issues
3.Hypercoagulable state
5.Reduxn in respiration volumes & rates
6.Mental/ Emotional
7. Prolonged convalescence
What are some agents used in the treatment of Chronic pain & their mechanism of axn?
Capsaicin- depletes substance P
TCAs- block serotonin/ NorEpi Uptake
Other antidepressants- may decrease neuronal excitation
What is considered to be the hallmark of Multiple Sclerosis? (Hint: MRI)
Plaques of scar tissue in multiple areas of CNS
What are the possible contributing factors of MS
*Genetic predisposition
*Environmental Triggers
*Vitamin D deficiency
What are the two "major" theories of etiology for MS?
1. Autoimmune theory-immune attack vs 1 or more self mylen/oligodentrocyte antigens

2. Antimicrobial theory- virus/infexn
T Cells are involved with cell- mediated immunity.
Type 1 are_________, while Type 2 are_________.
PRO-Inflammatory-- produce interferon gamma, implicated in MS.
ANTI- Inflammatory.
B- Cells are responsible for _________ Immunity & are also known as?
Humoral immunity and are also known as ANTIBODIES eg. IgG, IgM, IgA, etc.
These proteins act as signally molecules that modulate the inflammatory response.
What do cytokines trigger?
Expression of adhesion molecules on endothelial cells & leukocytes & Migration of WBS's across the endothelial wall of brain & spinal cord.
_________ are a family of adhesion molecules that mediate attachment and signal transduction.
Interferons are naturally occuring proteins produced by ________ & ________.
Fibroblasts & Macrophages
Interferons largely act in these 3 ways.
1. Immunomodulatory
2. Antiviral
3. Antiproliferative
What cells appear to initiate myelin destruction?
T-helper cells (CD4)-- activated in the periphery following Antigen processing and presentation by macrophage or APC
According to the Autoimmune theory of MS, activated T- cells are responsible for these 2 actions.
1. Express adhesion molecules
2. Produce matrix metalloproteinases that chew up and poke holes in the BBB allowing for entry of T-cells.
There is a(n) INCREASE or DECREASE in T-supressor cells reported in patients with active and progressive MS.
What are the 2 primary ways that microbial infexn may cause or contribute to MS?
1. Infection itself triggers the autoimmune response
2. Bacteria/ virus directly attacks myelin sheath
Which virus is implicated 20x's more than others to the development of MS?
Epstein Barr Virus-- elevated Ab titers are measured
Demyelination & Inflammation lead to the ______?
Characteristic lesions found in CNS, spinal cord &/or optic nerves
What are some primary symptoms of Multiple Sclerosis? Remember Primary symptoms are directly caused by the disease.
Fatigue, Sensitivity to heat, bladder & bowel dysfn, gait problems, visual disturbances, abnormal sensations, cognitive dysfn, dizziness, spasticity and pain, impaired speech and swallowing & emotional disturbances
What are some secondary symptoms of MS? Secondary symptoms are classified as complications brought on by the primary symptoms of the disease.
UTI, bed sores, muscle contractures, Respiratory tract infexns.
What are some tertiary symptoms of MS? Remember that these symptoms affect the Quality of Life for the patient
Social withdrawal, Personal life issues, Emotional disturbances & financial problems.
How much higher is the rate of suicide among MS patients compaired to the general population?
7 times higher in MS patients
What does KEDSS stand for and what does it represent?
Kurtzke Expanded Diability Status Scale-- it's a common assessment tool used to assess MS disease severity.
The 1st attack in MS is commonly called the __________?
CIS= Clinically Isolated Syndrome
This type of MS is associated w/ period of disease remission and little or no progression of the disease. It accounts for approximately 85% of MS cases.
Relapsing Remitting MS (RRMS)
After the 2nd attack, this form of MS just become progressively worse due to little or no remission.
Secondary Progressive MS (SPMS)
This form of MS is progressive from the onset. More males initially present with this form and there are NO drugs labelled to treat this form of the disease.
Primary Progressive MS (PPMS)
This form of MS is know to be steadily worsening from onset with acute 'flare-ups'. It accounts for a low percentage of patients but they have a worse long term prognosis than RRMS patients do.
Progressive Relapsing MS
After 2 or more attacks and 2 or more objective lesions have been identified, what additional data is needed to obtain a clinical MS diagnosis?
NONE= clincal diagnosis.
With 1 attack & 2 or more objective lesions what else is needed to obtain a clinical MS diagnosis?
DISSEMINATION IN TIME demonstrated by MRI or 2nd Clinical attack
With 1 attack and 1 objective lesion what is needed to obtain a clinical MS diagnosis?
DISSEMINATION IN SPACE & TIME demonstrated by MRI or + CSF or 2 or more lesions consistant w/ MS or MRI or 2nd clinical attack
With 2 or more attacks and objective lesion what is needed to obtain a clinical MS diagnosis?
DISSEMINATION IN SPACE demonstrated by MRI or + CSF & 2 or more MRI lesions or Clinical attack involving different site.
What does the ABCR TM stand for in the treatment of MS?
They are the disease modifying therapies; stands for Avonex, Betaseron, Copaxone, Rebif & Tysabri & Mitoxantrone.
________ are naturally occurring cytokines that exhibit antiviral, anti-proliferative & anti-inflammatory effects. They are also indicated in relapsing forms of MS
Beta Interferons
What are the 4 points of efficacy for Beta Interferons?
1. Reduce relapse rate in patients w/ MS; ~30%
2. Reduce T2 MRI lesion burden; ~50-80%
3. Slow sustained disability progression.
4. Improve measures of QOL & cognitive function.
What MS patient populations should be treated with Beta Interferons?
Any patient w/ Relapsing Remitting MS OR patients with Secondary Progressive MS that are still experiencing relapses & those at high risk for developing MS
What is the most recognizable post-injection side effect of Beta Interferons?
FLU-LIKE SYMPTOMS; fatigue, muscle aches, fever, chills etc. Occurs in ~ 50% of pts; can be avoided/ reduced by premedicating w APAP or NSAIDS prior to injection.
When using Beta Interferons what side effects should the health care provider monitor for?
Depression or psyche worsening, Injection site reaxn, Worsening spasticity, Thrombocytopenia (reduced blood counts), hepatotoxicity & seizures.
In the EVIDENCE trial, which group had a greater percentage relapse- free patients after 24 weeks? Rebif or Avonex
Rebif- 75%- had fewer MRI lesions also-- but also had injexn site reaxns & more leukocyte abnormalities!
Avonex- 63%
What is Interferon Beta- 1a (Avonex) indicated for?
Relapsing forms of MS to slow accumulation of physical disability & decrease frequency of exacerations.
What is unique about Avonex?
Only Interferon given IM; injexns may be painful!
What pregnancy category are the Interferons?
Pregnancy category C
How is Interferon Beta 1b given?
SubQ injexn 3 times per weeks; if dose skipped doses should be given at least 48hrs apart!
Name the oldest Interferon Beta 1b.
What is Betaseron indicated for?
Indicated in treatment of relapsing forms of MS.
What is Glatiramer (COPAXONE) Mechanism of action?
NOT CLEARLY DEFINED; was designed to mimic & compete w/ myelin basic protein but may induce t-supressor cells in periphery.
How is Copaxone administered?
SUBQ injexn of 20mg ONCE DAILY.
What 3 things is Copaxone shown to do in treatment of MS?
*Reduce clinical attack rate in RRMS
*Reduce MS lesion burden on MRI
*Slow time to sustained disability progression in pts w/ RRMS
Unlike Beta Interferons, Glatiramer (COPAXONE) is not associted with this side effect.
Flu like symptoms; don't have to pretreat
What pregnancy category is Copaxone?
Pregnancy category B
What is Copaxone's place in therapy?
Should be considered for treatment of ANY patient with RRMS; it may be helpful in those w/ progressive disease as well-- only small trials so far.
What is Mitoxantrone (NOVANTRONE)?
Anti-neoplastic & immunosuppressive; shown to reduce clinical attack rate and MRI lesion burden in Relapsing MS
This drug is indicated for use in Secondary Progressive MS & clinically worsening Relapsing Remitting MS.
Mitoxantrone (NOVANTRONE); 1st and only drug w/ this approval in US.
What is the main adverse side effect associated with use of Novantrone?
Cumulative dose-related cardiotoxicity; manifests as cardiomyopathy, reduced EF or irreversible CHF; Limits total use to 2-4 years.
Generic name Mitoxantrone
What pregnancy category is Mitoxantrone (NOVANTRONE)?
pregnancy category X
What is a unique feature of Natalizumab (TYSABRI)?
Fully humanized monoclonal antibody vs. Alpha-4 integrins
What is Bacolofen's (LIORESAL) mechanism of action?
GABA Analog; for treatment of reversible spasticity associated with MS or spinal cord lesions
What is Tizanidine's (ZANAFLEX) mechanism of action?
Short acting a-agonist; enhances presynaptic inhibition of motor neurons. Has compararble efficacy vs Baclofen (LIORESAL)
What class of drugs is largely used for treatment of Urinary incontinence in MS pts?
Anticholinergics; Oxybutynin, tolterodine, probantheline, dicyclomine & amitriptyline
What type of drugs are used to treat fatigue in MS patients?
Stimulants; Amantidine, Pemoline (CYCLERT), Methylphenidate (CONCERTA) & dextroamphetamine (DEXEDRINE) & Modafanil (PROVIGIL)
What type of drugs is commonly used to treat the tremor in MS patients?
Beta Blockers-- Propranolol; Non selective B-blocker
What type of drugs are used to treat the sensory symptoms of MS?
TCA's, antidepressants, anticonvulsants.
What is the enzyme responsible for the conversion of tyrosine to levadopa?
Tyrosine Hydroxylase
What is the enzyme responsible for the conversion of Levadopa to Dopamine?
Dopa decarboxylase
What is the name of the enzyme found throughout the body and can metabolize dopamine?
COMT; catechole methyltransferase
Symptoms of PD appear only after 60-80% of dopamine neurons in the substantia nigra have died or have been impaired. True or False?
What is the catalyst that converts Tyrosine into Levodopa?
Tyrosine Hydroxylase
What are the 4 core symptoms of PD?
TRAP: tremor, rigidity, akinesia & postural changes
What is a clinical sign of PD that appears in 75% of patients?
Dyskinesia may be induced by the use of antiparkinsonism medications. True or False?
A response to _______ may help confirm Parkinson Disease diagnosis.
L-Dopa (Levo/carbidopa)
Psychiatric disorders such as depression, bipolar disorders addiction and schitzophrenia can cause PD. True or False?
Dopamine production peripheral to the brain can cause...?
Nausea & low blood pressure
In regards to dose failures, a patient's "delayed ons" or the time in which a medication seems to "kick in" can be exacerbated by...?
Consumption of high protein foods
A common side effect of Amantadine (SYMMETREL) is...?
Insomnia, swelling legs and SPLOTCHY SKIN a.k.a LIVEDO RETICULARIS
LIVEDO RETICULARIS is associated with what PD treatment drug?
Amantadine (SYMMETREL)
Name the present preferred surgery for treatment of moderate to advanced Parkinson Disease.
Subthalmic Surgery; can stimulate the cerebral cortex to work again.
The lack of which neurotransmitter is thought to be primarily responsible for Parkinson Disease?
A physician prescribed Amantadine for PD-- what does it effectively treat?
In the __________ researchers discovered an association between PD and low levels of dopamine in the striaum of the brain.
Some evidence exists that suggest that the onset of PD before the age of 40 may be cause by genetic factors. True or False
Parkinson disease is associated with a loss of dopaminergic neurons in the _______.
Substantia Nigra
The most common treatment for Parkinson disease is?
Transplants of fetal cells into the brains of humans w/ PD have been consistently successful in treating PD. True or False?
Falls commonly occure early in the course of Parkinson disease. True or False?
What drugs are substrates for CYP2C9?
Phenobarbital, Phenytoin, Valproic Acid, Carbamazepine, Warfarin, Diazepam & Tricyclic Antidepressants.
What drugs are inducers of CYP2C9?
Carbamazepine (AUTOINDUCER), Phenobarbital, Rifampin
What drugs are inhibitors of CYP2C9?
Valproic Acid, Cimetidine, Tamoxifen, Verapamil
What drugs are substrates for CYP2C19?
Phenobarbital, Phenytoin, Valproic Acid, SSRIs, Diazepam and Tricyclic Antidepressants
What drugs are inducers of CYP2C19?
Phenytoin, Phenobarbital and Rifampin.
What drugs are inhibitors of CYP2C19?
Topiramate, Azoles, Omeprazole
What drugs are substrates for CYP3A4?
Carbamazepine, Tiagibine, Zonisamide, Statins, Amkio, CCBs, Theophylline, Macrolides
What drugs are inducers of CYP3A4?
Carbamazepine, Phenobarbital, Phenytoin,
Felbamate (FELBATOL), Rifampin
What drugs are inhibitors or CYP3A4?
Azoles, Cimetidine, Amiodarone, Macrolides, CCBs, SSRIs
What drugs are substrates of UDP glucuronyl transferase?
Lamotrigine, Carbamazepine
What drugs are Inducers of UDP glucuronyl transferase?
Lamotrigine, Phenobarbital and Phenytoin
What drugs are Inhibitors of UDP glucuronyl transferase?
Valproic Acid
To ameliorate pain is to....?
Make it more tolerable.
Many cancer patients are undermedicated for pain because... (9)
*Fear of addiction
*Fear of possibly hastening death
*Lack of knowledge
*Poor pain assessment
*Fear of DEA
*Pt reluctance to report pain
*Compliance issues
*Reimbursement schedules
What are the principles of therapy for MILD pain??
1. Assess the frequency/ duration/ etiology of pain routinely
2. If bone present, use of NSAID should be routine
3. Always dose a med to max before reverting to next step unless pain is out of control
4. If pain is constant or recurring always dose ATC
When treating chronic pain what is the maximum dosage for Carbamazepine (TEGRETOL)?
Titrated slowly up to max of 1000mg/qd
What is the mechanism of action for Oxcarbazepine (TRILEPTAL)?
Inhibits voltage-dependent Na+ channels & inhibits high-threshold N-Type Ca++ channels
What is the mechanism of action or Carbamazepine (TEGRETOL)?
Enhances inactivation of voltage-gated Na+ channels, increases release of serotonin & enhances dopaminergic transmission.
The FDA has approved Carbamazepine (TEGRETOL) for ____ (HINT: treatment of chronic pain)
Treatment of Trigeminal Neuralgia
How does modulation of Na+ decrease pain?
Prevents spontaneous ectopic discharges at concentrations lower than needed to block or inhibit impulse generation eg. w/ pain due to injury of the peripheral nervous system (Diabetes, severe accident)
What is the MDD for Oxcarbazepine (TRILEPTAL)?
Typically 600-1200 mg/day up to a max of 2400mg/day
How does Gabapentin work?
Does not influence synthesis or uptake of GABA--binds to voltage gated Ca++ channels presynaptically;may modulate release of excitatory neurotransmitters.
What is the MDD for Gabapentin (NEURONTIN)?
3600mg/day; above 3600, it inhibits its own absorption.
What is Lamotrigine's (LAMICTAL)mechanism of action?
*Stabilizes Na channels
*Inhibits release of glutamate
*Modulated high-threshold N-Type Ca channels
What is the max daily dose for Lamotrigine (LAMICTAL)?
25 mg/ day w/ a max daily dose of 400mg/day
What are the major adverse effects of Opioid analgesics?
Mood changes, somnolence, respiratory depression, decreased GI motility, stimulation of chemoreceptor trigger zone (N/V) Histamine release, tolerance & dependence
What are some common drug interactions of NSAIDS?
*Increases [warfarin]
*Increases nephrotoxicity risk; esp if on Diuretics or ACEI
*Hyperkalemia; esp if on K-sparing diuretics or K supplements
According to the WHO, what are the STEP I agents for pain treatment
*+/- adjuvants
According to the WHO, what are the adjuvants used for treatment of neuropathic pain?
TCAs & Anticonvulsants
When treating a person suspected for abusing opioids for pain what type of agent should never be used?
Mixed agonist-antagonist
Which pure agonist primarily activates the mu receptor in treatment of pain?
Which agent for pain should NEVER be used in end stage renal patients due to its harmful metabolite that are renally excreted?
Meperidine (DEMEROL) should never be given and Normederidine, it's metabolite can accumulate or be cleared via the kidneys