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Pharmacology - Neuro
neuroscience system pharm
27
Medical
Graduate
09/02/2009

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Term
Carbidopa/Levodopa (Sinemet)
Definition
MOA: Carbidopa inhibits the decarboxylation of peripheral levodopa (which normally does not cross the blood-brain barrier). When levels are elevated, enough Levodopa crosses the blood-brain barrier and is decarboxylated into dopamine.
Side effects: drug-induced dyskinesias, nausea, vomiting, orthostatic hypertension
DOC in older pts, often withheld early on for younger pts
Term
Drugs that increase dopamine levels:
Definition
Carbidopa/Levodopa (Sinemet) = dopamine precursor
Amantadine releases as much L-dopa from intact SN cells as possible.
Dopamine receptor agonists
COMT inhibitors
Term
Dopamine receptor agonists
Definition
fewer dyskinesias but less efficacy than L-dopa
(may be used as early monotherapy in young patients):
Pramipexole (Mirapex): use of this agent is expected to increase as it may have neuroprotective properties
Ropinirole (Requip).
Side effects: postural hypotension, hallucinations, drowsiness
Term
COMT inhibitors
Definition
MOA: inhibit the metabolism of dopamine, thereby increasing levels of this neurotransmitter- see details in Clinical Resource Sheet.
Entacapone (Comtan) is the most important agent here. A related agent,
tolcopone (Tasmar)…may cause elevations of liver enzymes so serial LFTs must be monitored; consequently this agent is seldom used now.
Term
OPIOIDS
Definition
MOA: Act as agonists at the mu, delta and kappa opioid receptors; work primarily through Gi/Go proteins to hyperpolarize neurons and inhibit neurotransmitter release.
IND: Relief of moderate to severe pain, preoperative medication, and as adjuncts during anesthesia. Some agents are used for their antitussive (eg codeine) and antidiarrheal effects (see below).
Term
Opioid overdose
Definition
coma with marked respiratory depression and pinpoint pupils (miosis). Hypotension and decreased bowel sounds are also commonly observed. The Dx can be confirmed by giving IV naloxone (Narcan), a general opioid antagonist.
Term
Opioid side effects
Definition
Constipation is very common & occurs through decreased intestinal peristalsis.
Term
Agonists related to morphine/codeine
Definition
Morphine (MS Contin, MSIR)
Codeine/APAP (Tylenol #3)
Hydrocodone/APAP (Vicodin)
Oxycodone, Oxycodone/APAP (Oxycontin, Percocet)
Heroin
Term
Synthetic opioid agonists
Definition
Fentanyl (Duragesic)
Meperidine (Demerol)
Propoxyphene/APAP (Darvocet)
Tramadol (Ultram)
Methadone (Dolophine)
Remifentanil (Ultiva)
Term
Partial Agonists and Mixed Agonists/Antagonists
Definition
Buprenorphine (Buprenex)
Nalbuphine (Nubain)
Term
Synthetic Opioid antagonists
Definition
Naloxone (Narcan) MOA: Displaces opioid narcotics from receptor sites.
IND: Reverses the CNS and respiratory depression in suspected overdose
Naltrexone (Revia): longer acting orally bioavailable opioid antagonist used for the treatment of opioid addiction and alcoholism. This agent is also covered in the Psych System- in the Rx of alcoholism
Term
LOCAL ANESTHETICS
Definition
MOA: Block sodium channels preventing generation and conduction of nerve impulses
IND: Are used for local anesthesia (e.g. dental extraction, suturing)
Examples of drugs in this class include:
Lidocaine (Xylocaine)
Procaine (Novocaine)
Bupivacaine (Marcaine)
Cocaine (Used still as a local anesthetic in some ENT procedures)
Term
akinesia
Definition
delay in initiating movement, or slowness it its execution
Term
bradykinesia
Definition
slowness and "poverty" of movement
Term
dyskinesias
Definition
involuntary limb or trunk movements
Term
"freezing" (Parkinson's symptom)
Definition
temporary inability to move, usually with gait
Term
"on-off" phenomenon
Definition
rapid, unpredictable change in Parkinson's symptoms
Term
"wearing-off" phenomenon
Definition
waning of the effect of the last dose of levodopa, maybe associated with abrupt changes in performance
Term
Amantadine (Symmetrel)
Definition
Amantadine (Symmetrel) MOA: Releases dopamine from intact dopaminergic terminals that remain in the substantia nigra. ( May see used for early mild Parkinson’s disease and L-dopa dyskinesias.)
Term
Trihexyphenidyl (Artane)
Definition
MOA: antimuscarinic (inhibits cholinergic CNS receptors) and thus decreases over-firing of key neurons.
Use: effective for treating tremor, but only in young pts w/ mild dx (see side effects)
Side effects: cognitive changes, and many others
Term
Phenytoin (Dilantin)
Definition

Used in Tonic-Clonic and Partial seizures

MOA: decreases Na and Ca conductance, blocks reuptake of adenosine, enhances GABA (inhibitory)

Pharmacokinetics: slow GI (2-6 HRS) absorption, maybe used IV for status epilepticus. bound to plasma proteins.

SideEffects: hyperplasia of gingiva, hypertrichosis,

Term
Carbamazepine (Tegretol)
Definition

MOA:

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Term
Valproic Acid (Depakote)
Definition

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Term
Levetiracetam (Keppra)
Definition

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Term
Ethosuximide (Zarontin)
Definition

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Term
Gabapentin (Neurontin)
Definition

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Term
Lamotrigine (Lamictal)
Definition

MOA:

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