Neuro Final 2 Drugs (eis)

induce dorsal horn & STT analgesia

This stage involves depression of inhibitory pathways - HYPERACTIVITY- this stage is skipped!

This stage involves the depression of ARAS pathways & spinal reflexes-

This stage ends with depression of the medulla (too deep! death)

•Disadvantages and limitations
»may cause cough, laryngospasm, bronchospasm, cardiovascular depression
»acute intermittent porphyria in some individuals
•Advantages and uses
»rapid and pleasant induction
»fast recovery, little post-anesthetic excitement or vomiting
•Widely used for induction

This drug will save your ass in Malignant Hyperthermia!

•Similar to thiopental
-rapid induction and recovery
-more hypotension is produced (because of histamine release causing vasodilation)
-esp. good recovery - upbeat mood
-little incidence of nausea, vomiting (useful antiemetic action)
- some reports of dreaming

a "dissociative anesthetic"
•Blockade of glutamic acid effects at NMDA receptors (excitatory NT)
•Disadvantages and limitations
-emergence excitement - disorientation, sensory & perceptual illusions, vivid dreams
-increased ICP
-poor muscle relaxation
-marked stimulation of secretions
Advantages and uses
profound analgesia
respiration and protective reflexes are well maintained
stimulates the cardiovascular system
Current status- trauma and emergency surgery, dressing changes, radiological procedures in children, combined with propofol
useful in high-risk patients (elderly)

•Naloxone reversal is available
•Fentanyl or a congener is combined with droperidol (a butyrophenone antipsychotic)
-neuroleptanesthesia is produced
–produces amnesia and analgesia
–sometimes combined with N2O
-used for diagnostic exams or minor surgical/radiological procedures

This is the coolest drug we’ve seen all year, it’s useful as an anti-szr rx (esp. status epilepticus) and is excreted mainly via the lungs! (spares the kidney/liver)

How did the administration of amphetamines and anticholinergerics give two clues about the cause of Parkinson Dx?

Why is Grandpa Al a classic case of PD risk factors?

Alleged negative PD risk factors?

Chlorpromazine, Haloperidol & Reserpine (anti-psychotics) all induce PD-like effects, Why?

Pramipexole, Ropinirole, Rotigotine & Bromocriptine are effective PD Rx's because they are __________

Anticholinergic can be used as adjunctive tx to PD, where would these drugs need to work in order to be effective? Where are the ACh neuronal cell bodies located

Why is L-DOPA used for PD tx?

Is L-DOPA useful in pts with MPTP exposure? Why or why not?

Why is carbidopa administered with L-DOPA?

Two major side effects of L-DOPA tx are:

About 90% of PD pts get _______ years of relief w/L-DOPA tx

Some PD pts experience _______ problems and about 15% experience psychiatric problems with reports of __________

What is the DIS advantage to administering L-DOPA w/carbidopa? (The advantage being a lower, more freq. dose)

What prevents the conversion of L-DOPA to 3OMD peripherally?

________ prevents the conversion of L-DOPA to 3OMD peripherally & in CNS (reserved for pts that don't respond to COMTAN-hepatotoxic)

How do MAOI's help treat PD?

_____ (MIRAPEX) and ________ (REQUIP) are ___&____
agonists used to tx PD

3 Benefits of D2/D3 rec. agonists?

This ergot derivative is a D2 agonist and has been replaced by Pramipexole/Ropinirole

What is the treatment for drug induced Parkinson Dx? (think: atropine+diphenhydramine)

2 requirements for microstimulator surgery tx of PD?

1st line tx for PD?

2nd line tx for PD?

This partial seizure has a complex symptomatology:
a) Alterations in perception/behavior/affect
b) Pts go thru a routine prior to szr onset- can be violent, cause legal problems

This partial seizure has an elementary symptomatology:
a "Jacksonian March" is one of them

Seizure with a bird like cry, loss bowel/bladder, tonus then clonus

What normally ends a TC szr?

Seizure (kids only!) shows altered consciousness for only few sec. & has a 3Hz EEG spike

Name two ways to induce an Absence szr:

Name 3 different ways anti-szr drugs work:

Whats the only drug that can be used for Tonic Clonic, Myoclonic, & Absence szrs?

This Rx reduces Na+ conductance (membrane excitability), is used more in kids, and is NOT useful for Myoclonic/Absence szrs

What are 4 ugly side effects of Phenytoin?

Elderly pts will complain of chest pain if given too much of this anti-convulsant

Two drugs that increase Phenytoin catabolism?

This drug is used in i.v. prep for STATUS EPILEPTICUS

3 drugs that pre-synaptically inhibit Na+ conductance:

Carbamazepine is used for TC-szrs, neuropathic pain, and what else?

Generally speaking, many ABtx will inhibit anti-convulsants. Conversely, _______ is an anti-convulsant that inhibits benzos, barbs, and other anti-convulsants (phenytoin/valpropic acid)

Side fx of Carbamazepine?

This drug is similar to carbabmazepine, but has fewer Rx interactions. Side fx incl somnolence

Rx used for generalized tonic/clonic and others seizures; historically for febrile seizures in children

Anti-szr Rx that:
-Potentiates GABA
-Reduces Ca+ dependent NT release
-REDUCES glutamate excitation

This is the drug of choice for uncomplicated* Absence szrs

This anti-convulsant potentiates GABA; reduces Ca-dependent NT release; antagonizes glutamate excitatory pathways

Two things that happen when you potentiate GABA:

This drug prevents GABA catabolism AND blocks Na+conductance (and blocks NMDA rec?)

3 Side effects of Valproic Acid (DEPAKOTE) (also rx interactions)

This anti-convulsant is approved for myoclonic szrs but is 2º used for complicated Absence szrs & general TC szrs

Benzos used for febrile seizures & STATUS EPILEPTICUS

DEPAKOTE Rx interactions:

Benzos used for myoCLONic / Absence seizures

Two GABA analogs used to treat neuropathic pain (fibromyalgia) can also be used as partial szr adjuncts or for gen. TC szrs

Generally speaking, GABAergic agents are best used for ______ seizures

Monotherapy for partial seizures, assuming a more 1º role in gen./absence seizures; acts through Na+ channels

_______ is assoc with spina bifida

_______ is assoc with "FAS-like syndrome"

______ is listed as a second line rx for EVERY seizure dx!

1st line for gen. TC szr (adult)?

1st line for Myoclonic (adult)?

1st line rx for (almost) every childhood seizure?

The BZ1 receptor is responsible for the ________ effects of benzos while the BZ2 receptor is responsible for the ________ effects of benzos

What is the significance of the bimodal BZ rec & ß carboline excitation?

Benzos increase ________ sleep and ______ sleep BUT decrease _______ sleep and ______ sleep

Compared to the anxiety curve, the dose response curve for benzo SLEEP induction is shifted left or right?

Useful benzo for producing a full night's sleep (for pts who can stay asleep once started) paradoxical excitement sometimes occurs

This benzo is more useful for pts who have trouble falling asleep but not staying asleep (side fx include memory problems, abnormal thinking/behavior)

This benzo is poorly absorbed & therefore has a more intermediate onset/duration

3 non-benzo hypnotics that act on BZ1 rec

This rapid acting, less potent hypnotic does not have any of the morning after/memory side effects assoc. zolpidem

This drug will save your ass in a benzo OD, because it is a BZ antagonist.

Side effects of this hypnotic inlcude:
-Retrograde Amnesia
-Somnolent Food Foraging
- Wt. gain
-

Side effects for this hypnotic include:
- Retrograde amnesia
- Bad taste in the mouth

This melatonin agonist works on MT1/MT2 receptors and does not have the abuse potential/withdrawl/rebound insomnia that other hypnotics have.

MT1 regulates sleepiness
MT2 regulates ___________

This old school anti-depr. is a useful hypnotic, but can cause priapism &/or orthostatic hypotension

2 MAJOR conclusions about benzos & GABA:

The GABA receptor is a _____ channel and it's ___ component is the attachement site for benzos/barbs/hypnotics/EtOH/picrotoxin.

What is the MOA for benzos?

Mix benzos with this drug to induce psychosis: _________

T/F Benzos do NOT cross the placenta barrier

Barbiturates increase the ________ of Cl- channel openings. (compared to benzos)

In addition to potentiating GABA rec/Cl- channels, barbiturates also work to blockade ________ resulting in reduced ________ excitation

Adding methyl/thio groups to these carbons will result ing shorter acting barbs:

Adding a long side chain on this barb carbon will create a more effective anti-szr rx

How can you modify C5 to make a more effective sedative barb?

What's sole molecular difference between Pentobarbital and Thiopental? (Hint: think about their most common uses)

Phenobarbital is a ______ acting drug useful for szrs and what else? (Hint: think about it's structure)

Redistribution from CNS tissue to peripheral tissue to fat is an essential trait for this barb:

Barbiturates are weak acids. Name two MAJOR conclusions about absorption using this fact.

T/F The more LIPOPHYLLIC an rx is, the SHORTER onset time.

T/F Shorter acting barbs are often excreted unchanged (un-metaboliszed)

3 Drugs you may want to reconsider when taking BARBITURATES

Why should pts w/porphyria avoid barbiturates?

What is choral hydrate?

What is paraldehyde?

Deadly Fact: An ED99 barbiturate user can be an LD2, which can lead to ________

T/F Melatonin has been clincially proven to be an effective sleep aid and cure jet lag

Valerian root appears to be an effective hypnotic because...

Drugs of choice for insomnia? (Two benzos, one non-)
What is the Rx dose regimen?

Adjunct Rx for anxiety,partial agonist at 5HT1A receptor, little abuse potential:

Underlying neuronal cause thought to cause depression? What cellular cofactors are in play?

Withdrawl from this drug is like wearing a "static suit": ________

Category of anti-depressants that show profound anti-muscarinic effects

Anti-depressant that inhibits DA re-uptake?

Anti-depressant that may be more useful in elderly to stimulate appetite & as a sedative?

Which anti-depressant is infamous for causing liver damage?

First order treatment for mania?

What's the problem with using Li+ for tx of mania?

Two Anti-psychotics that are not assoc. with wt gain?

Name two SNRIs:
1. __________
2. __________

Opioids don't always work for severe MUSCLE SPASM pain, what could give a pt to help with pain?

Flurazepam, Oxazepam, Lorazepam, & Temazepam all have WHAT in common? (hint: think metabolites)