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66 Cards in this Set

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What type of synapses are most neural connections? How does this effect pharmacology?
Chemical
Neurons using distinct NTs are organized functionally in CNS
Some drugs may only affect one pathway
Other drugs may cause a more general response (ie. overall excitability of CNS)
What is the BBB?
A function of CNS capillaries; tight junctions btw endothelial cells, as well as astrocytes and bsmt membrane make it difficult for substances to diffuse into CNS
The BBB isn't something physical that you can see under a microscope - it is a function of the selective tight junctions of the capillaries
9 ways a drug may modify snaptic transmission?
1. Pre-snyaptic potential
2. Synthesis of NT
3. Storage of NT
4. Release
5. Reuptake
6. Degradation
7. Postsyaptic receptor
8. presynaptic autoreceptors
9. Membrane effects
Explain how a drug may modify snypatic transmission via. presynaptic AP (AKA presynaptic inhibition)
Drug blocks propoagation along neural axons so AP fails to reach snyapse
Explain how a drug may modify snypatic transmission via Synthesis of NT
Drugs can block synthesis of NT
Explain how a drug may exert its effects via Storage of NT
Usually a certain amt of NT is stored in presynaptic vesicles
Drugs dec this storage dec the ability of the synapse to continue to transmit info
Explain how a drug may exert its effects via Release
Drugs inc synaptic activity by directly increasing release of NT from presynaptic terminal
Can also impair the release by directly decreasing the amt of NT released during each AP
Explain how a drug may exert its effects via Reuptake
Reuptake = send NT back to presynaptic terminal
Block this and NT is allowed to remain in cleft and exert its effect
Explain how a drug may exert its effects via Degradation
Inhibit the enzyme that causes degradation of the NT (ie. cholinesterase inhibitors for MG or MAO inhibtors for depression)
Explain how a drug may exert its effects via Postsynaptic receptor?
Antagonist can block receptor
Allosteric modulators can bind to receptor and inc effect of NT (ie. valium)
Explain how a drug may exert its effects via Presynaptic autoreceptors
During high levels of synaptic activity, the accumulation of NT in the cleft may allow binding to the presynaptic receptors and limit futher release of NT
This a form of negative feedback
Certain drugs appear to be able to bind to these presynaptic autoreceptors and dec NT release.. or you could block these autoreceptors which would result in more NT
Explain how a drug may exert its effects via Membrane effects
Drugs can alter transmission by affecting membrane organization and fluidity
Allow vesicles to dock
Change presynaptic poential
What is epilepsy?
Chronic neurological d/o characterized by recurrent seizuers
What is a seizure?
Episode of sudden, transient disturbances in cerebral excitation
Sufficient # of neurons begin to fire rapidly in synchronized bursts
A group of hyperexcitable nerves intitiate the seizure
Causes of seizure
Incident: CVA, TBI, brain tumor
Genetic or birth trauma
We dunno
What is the Goal of epilepsy pharm?
Inhibit firing of cerebral neurons thru...
Inc inhibitor effects of GABA
Dec effects of excitatory NTs (glutamate)
Alter Na and Ca movt across membranes
If seizures end spontaneously that why do we need to treat them?
Seizure recurrence causes more damage to already injured nerves, and may also injure healhty ones
3 types of seizures and subtype
1. Partial
2. Generalized (absence, myoclonic, clonic, tonic, tonic-tonic)
3. Status epilepticus
Dif btw partial and genralized seizure?
Only part of brain is involved vs. whole brain involvement
What is an absence seziure?
Petit mal: sudden, brief LOC, may or may not have mo. signs
What is a myoclonic seizure
General seizure: mm contraction in part of the body, may or may not LOC
What is a clonic, tonic, tonic-clonic seizure?
Grand mal: mm contraction t/o body and LOC
What is Status epilepticus? What causes it?
Series of seizures without recover of conscioussness bw attacks: life-threatning
May stem from numerous factors: ischemic CVA, systemic or intracranial infection, drug/alcohol withdrawl?
Name 7 anti seizure drugs and what types of seizures they tx
1. Barbiturates (phenobarbital {Solfoton}): back up/adjunct drug
2. Benzodiazepines (diazepam {valium} and Lorazepam {ativan}): Status epilepticus
3. Carboxlic acids (Valproic acid {Depakote}): partial, tonic-clonic, absence, and myoclonic
4. Hydantoins (phenytoin {Dilantin}): tonic-clonic and partial
5. Iminostilbenes (carbamazepine {Tegretol}): Tonic-clonic and partial
6. Succinimides (ethosuximide {Zarontin}): absence
7. Neurontin (gabapentin): parital
Barbiturates:
Use/indication
Prototype
Mechanism
Adverse effects
Drug of choice for controlling seizures in infants, may be used in adults (particularly for hard-to-control seizures)
Phenobarbital (Solfoton)
Inc inhibition of GABA and inhibit Ca entry into presynaptic terminal = dec release of Glutamate
Drowsiness and sedation
Benzodiazepines:
Use
Drugs
Mechanism
Side effects
Tx status epilepticus, Klonotin treats absence seizures
Diazepam (valium), lorazepam (Ativan), Clonazepam, Klonotin
Inc Gaba inhibition
Sedation and behavioral changes
Short term vs. long term use of Benzodiazepines?
Short term: diazepam (valium) or Lorazepam (Ativan) via IV for acute problem
Long term: Clonazepam or Klonotin used for absence seizures
Carboxylic Acids:
Drug
Mechanism
Side effects
Other conditions it treats
Valproic acid (Depakote)
Unclear, likely multiple
GI distress
Bipolar
Two main drugs used to tx tonic-clonic and partial seizures
Hydantoins: phenytoin (Dilantin)
Iminostilbenes: carbamazepine (Tegretol)
Mechanism and side effect for Hydantoins and Iminostilbenes?
Stabilize neuronal membrane so it is less likely to be excited
Hydantoins: Confusion and ataxia
Iminostilbenes: Dizzy, water retention, anemia.. but NO SEDATION
Succinimides
Primary indication
Drug
Mechanism
Side effects
Absence seizures
Ethosuximide (Zarontin)
Reduce Ca currents, which limits spontaneous neuronal firing (so vesicle can't bind to the membrane)
GI deistress and other membrane effects
What is gabapentin (Neurontin) used to treat?
Partial seizures
Also a spasmolytic and usedful for treating neuropathic pain
What type of drug is neurontin? Mechanism? Side effects?
Second-generation which is used an adjunct therapy or alternative to first line drugs
Unclear, but may inc GABA release
Sedation, ataxia, dizziness
Antiseizures and pregnancy
Mothers on antiseizure drugs have inc risk of fetal malformations
Don't know if it the disease or the meds
How are antiseizure meds withdrawn?
Tapered to avoide inc seizure frequeny or severeity
Prevention level that includes health promotion, wellness education programs, immunizations, hearing protection in occupational settings, training to develop good body mechanics, health screening for prostate, breast, colon cancer. Before illness occurs
Primary prevention
2 general ways drugss can affect the CNS?
Alter quantity of NT released
Affect stimulation of postsynaptic receptors
What does drug tx do for Parkinson's?
Does not cure underlying pathology
Can alleviate the mo. s/s and dementia to improve quality of life
PD causes what imbalance?
Dec dopamine
Inc Ach
Main types of PD drugs
Levodopa
Dopamine agonist
Anticholinergics
Amantidine
Monoamine oxidase inhibitors (MOA)
COMT inhibitors
Primary drug tx for PD? MOA?
Levodopa. Converted to dopamine after crossing BBB
PROs vs. CONs of Levadopa
PROs: effective
CONs: vast majority converted to dopamine outside CNS
What drug is often administered with levadopa?
Peripheral Decarboxylase Inhbitor (Carbadopa) to inhbit premature conversion - Called Sinemet
ORALLY for this and levadopa
Side effects of Levodopa
Gi (espec if given without carbidopa)
CV (Postural hypotension) - careful with pts with hx or CVD
Dyskinesisas
Behavioral changes (especially when given with carbadopa)
Diminished response over years
Fluctuations in response (on-off phenomenon)
Who should not be taking Sinemet?
Phychoses pt... maybe jsut levadopa by itself
Why are drug holidays for levidopa not used much anymore?
Pose inc risk of immobility and associated conditions b/c back to PD's s/s
Dopamine agoinst: MOA and side effects
Directly stimulate dopamine in BG
N/V, postural hypotension
List 4 dopamine agonists. Which 2 are now often the first used drugs for early PD?
Bromocriptin (Parlodel)
Pergolide (Permax)
Ropinorle (Requip)
Pramipexole (Mirapex)
Last two are being used early
PROs of dopamine agonists?
Fewer side effecs than levodopa
Effective in early PD
Possible neuroprotective (dx-slowing)
Special use dopamine agoinst? Adverse effects?
Apomorphine (Apokyn) used for temporarily relief of Off periods from levadopa tx
Number of side effects/complications: severe N/V and potential complications
MOA for anticholinergics?
Block AcH receptors
Dec the ACh influence, to more closely match the dec dopamine influence
TREMORS
List 3 anticholinergic drugs
Benztropine mesylate (Cogentin)
Procyclidine (Kemadrin)
Trihexyphenidyl (Artane)
Anitcholinergics:
Pros
Cons
Side effects
Useful if used in comb with other drugs
CONS: nonselective, not as effective as other drugs when used alone
Side effects: mood changes, GI disturbances, dry mouth , urinary retention, others
Can also be used to tx dementia associated with PD
Amantidine (Symmetrel) MOA
Anti-viral drug taht blocks glutamate receptor (NMDA) and may have other neuro-transmitter effects
Research is on-going; may be antichilinergic and may enhance dopamine's effects
Symmetrel
Pros
Cons
Side effects
PROs: milder side effects than some PD drugs
CONs: Effective for short term (several wks)
Side effects: orthostatic hypotension, CNS/mood disturbances
MOA inhibitors:
Drugs and mechanism
Selegiline (Deprenyl) and Rasagline (Azilect)
Inhibit MAO enzyme that breaks down dopamine
MOA inhibitors:
Pros
Cons
Side effects
Pros minor side effects at low doses, seems to help in early PD
Cons: unclear if effective long term, drug-drug interactions
MINOR side effects
COMT inhibitors:
MOA and Drugs
Prevents breakdown of levadopa in periphery to an inactive metabolite
Tolcapone (Tasmar)
Entacapone (Comtan)
Stalevo
Sinemet plus entacapone
= levadopa, carbadopa, entacapone in one preparation
COMT inhibiotrs:
Pros
Cons
Side effects
Pros: can use lower levels of levadopa, may reduce fluctuations in levadopa response
Cons: side effects
Side effects: Iniital inc in dyskinesias, Gi disturbances, mm cramps
Tasmar - liver toxicity
What other neuroprotective agent may be used in PD?
Conezyme Q10... levels seem to be low in PD, but not clear if inc' these levels helps s/s
What drugs treat partial and tonic clonic seizures?
Hydantoins (Phenytoin)
Iminostilbenes (Tegretol)
Valproic acid (Depakote)
What drugs treat absence sizures?
Succinimides (Zarontin)
Valproic acid (depakote)
Klonotin
What drugs treat myoclonic seizures?
Valproic acid
What drugs treat tonic-clonic seizures?
Hydantoins and iminiostilbenes
What should PT be concerned with regarding the side effects of Anti-seizure drugs
1. Sedation-- need to find a balance bt one and off meds so pt wont be too tired for treatment but also wont get a seizure

2. Fall risk secondary to ataxia

3. Withdrawal sx's

4. GI disturbances can affect PT

5. When pts hx and what brings on seizure when treating

6. Low light environment

7. Modalities often bring on seizure