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121 Cards in this Set
- Front
- Back
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drugs of 1st choice for:
Partial Seizures |
Carbamazepine
->Primidone/Phenobarbital Phenytoin (adjunct) Valproic Acid Oxcarbazepine Lamotrigine |
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drugs of 1st choice for:
Generalized Tonic Clonic |
Phenytoin
Carbamazepine/Oxcarb Valproic Acid |
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drugs of 1st choice for:
Absence |
Ethosuximide
Valproic Acid |
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drugs of 1st choice for:
Myoclonic and Atonic |
Valproic Acid
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what are the 4 ways that anti-epileptic drugs reduce excitation?
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•BLOCKING sodium channels
•BLOCKING calcium channels •PROMOTING activity of GABA •BLOCKING excitatory amino acid activity (glutamate, AMPA, NMDA) |
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drug for AED?
antagonizes transmission through AMPA receptor and enhance Cl- flux mediated by GABA |
Topiramate
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drug used to tx AED
MOA: may inhibit breakdown and promote production of GABA -calcium channel blockade (T-type) |
Valproic acid
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where do the following drugs act?
Carbamazepine Oxcarbazepine Phenytoin VPA Topiramate Lamotrigine Zonisamide |
Na channel blocker
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what drugs inhibit the breakdown of GABA
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VPA
Vigabatrin |
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what 2 drugs used to tx AED act directly on Cl ion channels?
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•Benzodiazepines- bind to specific subunit of receptor
•Barbiturates- bind to specific subunit of receptor |
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what AED drug needs to be closely monitered due to being highly bound to albumnin?
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Phenytoin – highly bound to albumin (>90%)
• “free” conc obtained which represents activity of drug • Conc (mcg/ml) = total (10-20); free (1-2) |
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what clinical situations will alter protien binding of phenytoin?
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• Acute illnesses (burns, trauma)
• Drug interactions (valproic acid) • Renal or hepatic impairment |
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what drug for AED has a non-linear kinetics and should not be increase in large doses?
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Phenytoin -> undergoes capacity-limited metabolism
• Non-linear kinetics • Clearance NOT proportional to concentration Do NOT make large dose increases when titrating phenytoin daily dose |
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What AED drug undergoes auto-induction?
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Carbamazepine undergoes “auto-induction”
• Hepatic enzymatic activity of carbamazepine enhanced -Typically starts the 1st week of therapy and lasts up to approx. 1 month. -May need to increase dosage several weeks into therapy |
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What AED drugs are known to be drug inducers?
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Carbamazepine, phenytoin,
phenobarbital |
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What AED drugs are known to be drug inhibitors?
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Valproic acid, felbamate
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what are general ae for AED?
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1. CNS toxicities- especially at initiation, so start low and go slow
2. blood discrasias and other serious toxicities (CHECK BASELINE LABS) 3. osteomalacia and osteoporosis |
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what 2 drugs used to tx AED can cause serious skin rashes?
what severe rxn can result? |
lamotrigine + valproic acid
Hypersensitivity reactions • Stevens-Johnson |
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What AED has the risk of aplastic anemia?
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Felbamate
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What AED is associated with does dependent thrombocytopenia?
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Valproic acid
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what 5 general areas in the body can ae develop from AED?
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skin, liver, blood, bone
also most AED inc weight |
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what one AED is known to cause weight loss?
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Topiramate
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What AED cause metabolic bone abnormalities?
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Carbamazepine, phenytoin,
phenobarbital, valproic acid |
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What drugs put pt at risk of fractures during seizures?
what is the MOA? |
Carbamazepine, phenytoin,
phenobarbital, valproic acid • Impaired calcium absorption • Increased catabolism of vitamin D • Impaired bone resorption and formation |
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What supplement should be give to pt on the following drugs?
Carbamazepine, phenytoin, phenobarbital, valproic acid and why? |
Consider supplemental vitamin D and calcium
-Metabolic bone abnormalities common -Mechanism • Impaired calcium absorption • Increased catabolism of vitamin D • Impaired bone resorption and formation |
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What AED causes:
• Nystagmus • Gingival hyperplasia |
Phenytoin
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What AED causes:
• Hyponatremia (SIADH) • May increase ADH or sensitivity |
Carbamazepine/Oxcarbazepine
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What AED causes:
• Kidney stones – Carbonic anhydrase inhibition in kidney |
Topiramate/Zonisamide
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how should women who are thinking of pregnancy or who are pregnant and epileptic be treated?
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- CDC recommends preconceptual folate
supplementation (minimum 0.4 mg/d) in all females of childbearing age, with or without epilepsy to avoid neural tube defects -In females with epilepsy on AEDs, it is common practice to supplement with folic acid 1-5 mg/day |
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type of headache?
Associated with parasympathetic overdrive: -lacrimation -nasal stuffiness -rhinorrhea -periorbital swelling |
Cluster Headache
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HA Type?
severity: mod / severe location: FT / periorbital duration: 4 to 72 hrs pain type: throbbing assoc. s/s: aura n/y photo |
Migraine
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HA Type?
severity: severe location: periorbital duration: 15 to 180 min pain type: sharp assoc. s/s: autonomic **always unilateral |
cluster
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HA Type?
severity: mild / mod location: diffuse duration: variable pain type: dull assoc. s/s: stiffness |
tension
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what is the cause of Chronic Daily Headache (CDH)
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Many CDH are a result of analgesic overuse (analgesic rebound headache/drug-induced headache)
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type of HA?
pts have headache >15 day/mon -> can be secondary to tension-type, migraine |
Chronic Daily Headache
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what serotonin receptors are involved with trigeminal nerve?
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5HT-1D receptors on trigeminal nerve
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what serotonin receptors are involved with cranial vessels?
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5HT-1B receptors on cranial vessel
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a network of nerve fibers that innervate cranial vessels which provide sensation of vesses likely to produce headaches
what is this? |
trigeminovascular system
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what is the order of cranial pain associated with HA?
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stimuli, neural activation, degranulation of inflammatory chemicals, bv dilation, ha pain, sensitization and more refractory pain
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type of ha therapy?
used during individual attacks to treat the intensity of pain and its associated symptoms ->Treat early in the attack |
Acute therapy
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when should preventive (prophylacitc) therapy be used?
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1. Attacks of headache occur at a frequency greater than 2 per week (except cluster)
2. Despite infrequency of attacks, the devastating nature of headaches make prevention worthwhile |
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when are parenteral dosage forms used in HA therapy?
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Parenteral dosage forms used if there is severe pain or nausea/vomiting
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when are Rectal/nasal dosage forms used in HA therapy?
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Rectal/nasal forms used if nausea/vomiting
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what is first line for aborting a mild migraine HA?
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Acetaminophen or NSAIDS are 1st line (if moderate pain)
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what is first line for aborting a sever migraine HA?
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Triptans 1st line (severe)
Sumatriptan (Imitrex) Zolmitriptan (Zomig®) Naratriptan (Amerge®) |
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first line tx for migrane HA prophylaxis?
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Beta-Blockers OR Topiramate are 1st line
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first line tx for migrane HA prophylaxis for a pt that is also depressed?
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Tricyclic antidepressant (1st line if also hx depression)
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first line tx for migrane propholaxis for pt with history of HTN
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Verapamil (2nd line after B-blockers if hx HTN )
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first line txmt for migraine HA prophylaxis and hx of seizures or bipolar dx
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Valproate or Topiramate (1st line if hx of seizures or bipolar dx-VPA)
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what is the key relationship between mentrual migrane and hormones?
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key issue is RAPID CHANGE in estrogen levels bc these types of HA occur less duing late pregnancy and menopause
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tx for menstrual migrane
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1. Standard therapy
2. “Miniprophylaxis” NSAIDS, ergots or triptans perimenstrually 3. Increase prophylactic medication dose 4. Extended regimen estrogen 5. Lower dose estrogen |
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what drugs should be avoided in tx pt with migraines during pregnancy?
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AVOID TRIPTANS AND ERGOTS
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in what situation is migraines treated as follows?
->Tylenol +/- codeine - caution 3rd trimester w/codeine (use sparingly) - NSAIDS - caution in 3rd trimester -Caffeine less than 300mg/day minimal risk to fetus -Prochlorperazine or metoclopramide |
Migraine in Pregnancy
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what HA is treated with Oxygen 7L/min x 7 min standard acute therapy 1st line?
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Cluster Headache - abortive tx
can also use -Ergot alkaloids (DHE or ergotamine) -Sumatriptan subcutaneously -NSAIDS (Indomethacin or Ketorolac) -Topical anesthetics (lidocaine, cocaine) -Steroids (dexamethasone) |
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what is the first line prophylactic therapy for cluster headache?
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Prednisone or Verapamil or Lithium are 1st line agents
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what type of HA has the following acute tx regimen?
Acetaminophen or NSAIDS are 1st line agents Butalbital +Caffeine + 1st line agent Opiod analgesic + 1st line agent Anxiolytics/Skeletal Muscle relaxants + 1st line |
Tension-Type Headache
Acute treatment |
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txmt for drug-induced ha?
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Treatment is removal of the agent
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drug for ha?
MOA is by vasoconstriction of cranial arteries or by stimulating 5HT-1 receptors (NON-SELECTIVE) |
abortive therapy
Ergot Alkaloids |
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Structurally related to amines (DA, EPI,NE) and can cause potent vasoconstriction or vasodilation
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Abortive therapy
Ergot Alkaloids |
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ae for what drug?
-Peripheral vasoconstriction is most serious adverse event -numbness/tingling in -extremities -muscle pain -gangrene Nausea/vomiting occur in up to 10% of pts -use lowest dose possible -use with metoclopramide (antiemetic) -Rebound headache/dependence |
Ergotamine-Adverse events
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when are ergotamines contraindicated?
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peripheral vascular disease
hepatic impairment renal impairment coronary artery disease pregnancy concomitant triptan use |
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what 2 types of HA are triptans effective at txmt?
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migranes and cluster HA
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which triptan is the gold stardard?
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sumatriptan (Imitrex)
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ae for sumatriptan?
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Most severe adverse events are coronary vasospasm, MI, arrhythmias, stroke
“Triptan” symptoms ->chest tightness, tingling, numbness ->neurologic- drowsiness, lethargy Most common AE with SQ is injection site reactions |
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all triptans have the same efficacy, similar se and indicated for abortive therapy.
T or F |
T
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which 5HT-1 receptor agonist is in the form of a rapidly degraded tablet and more bioavailable?
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Zolmitriptan & Rizatriptan
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which 5HT-1 receptor agonist is NOT contrindicated with MAO-I?
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Almotriptan
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which 5HT-1 receptor agonist show superior efficacy vs. sumatriptan?
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Eletriptan
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what drug used to tx ha has the following contraindications?
-peripheral vascular disease -uncontrolled HTN -coronary artery disease or significant cardiovascular disease -concomitant MAO-A inhibitor within 2 weeks - Except Almotriptan -concomitant ergot use within 24hrs -significant hepatic disease |
Triptans
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what is the concern in using acetominophen, asa or nsaids to tx HA?
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Major concern is rebound in combinations
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what is the drug with the following combination?
isometheptene + dichloralphenazone + acetaminophen |
Midrin - a simple analgesic
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drug of choice for nausea in migrane
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Metoclopramide
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what category are these drugs?
Metoclopramide Prochlorperazine Chlorpromazine |
Abortive Agents
Dopamine Antagonists |
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drugs of choice for tension-type prophylaxis and are also effective in migraine prophylaxis
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Tricyclics like amitriptyline (Elavil®)
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when should Tricyclics like amitriptyline (Elavil®) not be used to tx ha/migranes?
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Do not use in pregnant women, glaucoma, urinary retention, with MAO-I
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most common se for Tricyclics like amitriptyline (Elavil®) - antidepressants?
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Most common side effects are ANTICHOLINERGIC in nature
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txmt of choice to prevent migraines
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B-Blockers: Propranalol, atenolol, metoprolol effective
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se of using b-blockers in tx of migranes?
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-Side effects include fatigue, hypotension, bradycardia
-Caution in asthma, diabetes |
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txmt of choice for prevention of both cluster and migraine headaches
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CA channel blocker
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se of ccb with prophylactic tx of migraines and ha
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Side effects include hypotension, edema, constipation
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what prophylactic tx for migraines and ha also causes weight loss?
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Topiramate
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Treatment of choice for prophylaxis of chronic cluster headache
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Lithium
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what drug can precipitate a headache as well as lethargy and abdominal discomfort
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Lithium
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Ergots interact with what drugs?
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-with P450 3A4 inhibitors
-with macrolide antibiotics -propranolol |
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Triptans rx with what drugs?
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-MAO-I (eg phenelzene)
-triptans metabolized by MAO, increase effect -with ergots - may cause extreme vasoconstriction |
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what drugs do MAO-I react with?
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-isometheptene (Midrin®) -
excessive release of catecholamine -antidepressants |
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pain initiated or caused by a
primary lesion or dysfunction in the nervous system |
Neuropathic pain
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type of pain?
– aching, throbbing, sharp – trauma, arthritis – responds to NSAIDS, opioids |
Nociceptive Pain
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type of pain?
– burning, “electric”, shooting – difficult to treat with conventional analgesics – other sensory symptoms present – negative sx |
Neuropathic pain
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Diabetic Neuropathy - Treatment Strategies, what drugs are first line/.
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Gabapentin, pregabalin, tramadol, opioids, tricyclic
antidepressants or duloxetine , 1st line |
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what type of pain is caused by the follow?
– Cancer chemotherapy (taxanes, platinum, vinca alkaloids, thalidomide) – Antiretrovirals (ddI, ddC, d4T) – Isoniazid – CANCER AND HIV THEMSELVES CAN CAUSE NEUROPATHY |
Drug-induced Peripheral Neuropathy (DIPN)
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what categories of drugs cause Drug-induced Peripheral Neuropathy (DIPN)?
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Antiretrovirals
Cancer chemotherapy Anti-infectives |
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how do antineoplastic drugs cause Drug-induced Peripheral Neuropathy (DIPN)?
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• Disruption of axonal transport via microtubular
dysfunction • Increase in inlf mediators (Il-1, Il-6) causing cellular apoptosis and decrease in myelin generation |
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how do antiretroviral drugs cause Drug-induced Peripheral Neuropathy (DIPN)?
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– Inhibition of mitochondrial DNA polymerase
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what is “Dying-Back” (Wallerian Degeneration)?
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– Interruption of transport affects distal axons first then neurons more proximal are effected over time
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what are the risk factors for developing Drug-induced Peripheral Neuropathy (DIPN)?
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type of pain?
Caused by damage of neurons in spinal cord or the trigeminal nerve |
Post-herpetic neuralgia
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gabapentin, pregabalin, tramadol, opioids, lidocaine patch
used to tx what type of pain? |
Post-herpetic neuralgia
Drug Induced Peripheral Neuropathy diabetic neuropathy |
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type of pain?
Compression of 5th cranial nerve |
Trigeminal neuralgia
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what is the first line tx for Trigeminal neuralgia?
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Carbamazepine (CBZ) is 1st line agent
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drug treating pain?
Works by blocking Na+ channels reducing excitatory transmission |
Anticonvulsants -
Carbamazepine |
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what are the se for carbamazepine?
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• drowsiness
• nausea (take with food) • dizziness • confusion • unsteadiness on feet |
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what are the drug interactions for carbamazepine?
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Inducer of P450 enzymes
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drug for pain?
Generally less toxic than carbamazepine because it is not metabolized to toxic intermediate |
Anticonvulsants - Oxcarbazepine
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drug for pain?
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Anticonvulsants - Pregabalin
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drug for pain?
– Shows recovery rate of voltage-gated NA+ channels, Limits repetitive firing. – Increases GABA levels through effects on various enzymes |
Anticonvulsants - Valproate
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drug used for pain?
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Tricyclic Antidepressants
– Secondary amines: desipramine, nortriptyline – tertiary amines: amitriptyline, imipramine, clomipramine |
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what are common ae for tca?
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constipation, dry mouth, blurred vision, cognitive changes, tachycardia urinary retention
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most worrisome ae of tca?
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Alteration of cardiac conduction: most worrisome
– caution with erythromycin, SSRI’s |
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what drug used for pain has the following contraindications?
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closed-angle glaucoma,
benign prostatic hypertrophy, acute myocardial infarction |
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what drug used for pain can NOT BE USED WITH MAO-I?
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tca
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drug?
SSNRI FDA approved for diabetic neuropathy -Significantly reduced avg pain scores |
Duloxetine (Cymbalta®)
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drug for pain?
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Capsaicin
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drug used for pain?
– NE and 5HT reuptake inhibitor – metabolite which is an opioid agonist Most frequent side effects nausea/vomiting constipation -DO NOT USE in patients with seizures or in combination with other agents which can lower seizure threshold (TCA’s, SSRI’s) |
Tramadol
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what class of drugs are used to tx parkinson's disease
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anit-cholinergic agents
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what is the site of action for anticholinergic agents?
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muscarinic receptors in striatum
-block over-stimulated muscarinic receptors |
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key se of sinemet?
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dyskinesia, response fluctuation (motor complication), psychiatric complications (hallucinations)
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what are drug or food interactions that occur with sinemet?
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1. drugs that possess dopamine antagonist activity
2. ferrous sulfate 3. anticholinergics may alter gi absorption of levadopa 4. protien containing foods dec abs |
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what are the 2 dopamine agonist used to tx parkinson's disease?
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1. ergot dopamine agonist
-bromocriptine 2. non-ergot dopamine agonist -ropinirol (requip) -> used more and often used early in the disese then add levadopa later |
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drug for parkinson's disease?
prevents degredation of dopamine in the brain through MAO-B inhibition |
Selegiline
metabolites L-amp and L-methamp are thought to inhibit presynaptic reuptake of dopamine |
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se of mao-b inhibitors?
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orthostatic hypotension, hallucination, dyskinesias
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