Transcript Drugs affecting the Central-Nervous

Drugs affecting the Central-NervousSystem (CNS) & PAIN medications
Chapters 12 and 13
MR160
Central Nervous System (the CNS)
• Stimulants – increase brain & spinal cord
activity
• Depressants – decrease CNS activity, either
specifically or generally (ANESTHESIA)
• Anti-convulsants (epilepsy) – goal is to
depress the Motor Cortex
• Anti-parkinsonian – physical therapy used in
early stages, then medication
CNS Stimulants
ADD & ADHD therapy
• Adderall (amphetamine salts) - oral
• Concerta (E/R methylphenidate) – oral
• Daytrana (methylphenidate) – skin patch!
• Ritalin (methylphenidate) – oral
• Strattera (atomoxetine) – not controlled!
Narcolepsy – Provigil promotes wakefulness
CNS Depressants (page 1)
the STAGES of General ANESTHESIA are
characterized by the level, or ‘depth’
• Stage I – Analgesia: euphoria, amnesia
• Stage II – Delirium: increase involuntary muscle
activity, irregular breathing, HTN, tachycardia
• Stage III – Surgical Anesthesia: until spontaneous
respiration ceases, watch eyes & reflexes
• Stage IV – Medullary Depression: pupils fixed &
dilated … no lid or corneal reflexes
CNS Depressants (page 2)
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HYPNOTICS and SEDATIVES
Daytime sedation – small doses
Sleep induction – larger doses
CAUTION: mixing w/ alcohol, antihistamines
morning ‘Hangover’ effect - greatly reduced
by use of short-acting agent or lower doses
• Barbiturates – phenobarbital, secobarbital
• Non-barbiturates – Ambien, flurazepam
--- Restless Leg Syndrome --• DOPAMINE RECEPTOR AGONISTS to treat
Restless Leg Syndrome (RLS)
• technically –NOT- CNS-depressants !
• Mirapex (pramipexole) – also sometimes
effective in Parkinsonism
• Requip (ropinirole) – Parkinsonism also, but
may cause patient to fall asleep during daily
activities!
Narcotic Analgesics
• OPIATES – derived from Opium (morphine,
codeine)
• OPIOIDS – synthetic drugs with actions similar
to opium/opiates
• The term ‘Narcotic’ includes both opiates &
opioids (all are Controlled-substances)
• Most effective, but most ADDICTIVE analgesics
• CAUTION: tolerance, physical dependence
------ OPIATES -----• MORPHINE SULFATE
MS Contin – controlled release
MSIR – immediate release
Roxanol – oral solution & concentrate
• CODEINE
* opiate or opioid OVERDOSE treatment =
Narcan (naloxone) … ‘antidote’
----- OPIOIDS ----•
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hydrocodone (Vicodin, Lortab, Norco)
oxycodone (OxyContin, OxyIR)
meperidine (Demerol)
methadone – some history
--- alternate dosage-forms --• fentanyl (Duragesic) – skin patches
• butorphanol (Stadol) – nasal spray
non-Narcotic analgesics
• acetaminophen (APAP) – Tylenol
• aspirin (ASA)
--- chewable (Bayer, St. Joseph’s)
--- buffered (Bufferin)
--- enteric-coated (Ecotrin)
• tramadol (Ultram) – abuse potential !
• propoxyphene (Darvon) – no longer on the
market --abuse potential !
Drugs for MIGRAINE
• The TRIPTAN’s – not related to other
analgesics
• ‘selective Serotonin Agonists’
• Primarily effective on headaches that are
vascular in nature …(not tension, cluster)
• MOA = constricts vessels, blocks nerves
• Imitrex (sumatriptan)-oral, injectable, nasal
• Axert (almotriptan)
EPILEPSY
• SEIZURE TYPES
• Tonic-Clonic (Grand Mal) – last 2 – 5 minutes,
often followed by deep sleep
• Absence (Petit Mal) – 1 to 30 seconds
• Complex Partial – brief period of confusion
• Epileptic ‘equivalents’ – these episodes
‘resemble’ seizures … causes?
---tetanus ---hypoglycemia ---drug-withdrawal
Drugs for Epilepsy (Seizures)
pg 113-115
• ANTICONVULSANTS
--Dilantin(phenytoin) --Tegretol(carbamazepine)
• BENZODIAZEPINES
--Klonopin(clonazepam) – Ativan (lorazepam) -Valium(diazepam) …others …
• Neurontin(gabapentin) – also for ‘neuralgia’
• Lamictal(lamotrigine) – stabilizes neuronal
membranes
PARKINSON agents
• PARKINSON’S DISEASE has no known cause,
but seems to be related to depletion of
dopamine in the brain
• “Secondary parkinsonism” may be caused by
drugs (antipsychotic meds), toxins, or
degenerative diseases (Alzheimer’s Disease)
• DOPAMINERGIC drugs
--- levodopa/carbidopa (Sinemet)
*see Table 12-4 for non-dopaminergic agents
Chapter 13
Analgesics/Antipyretics
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Analgesics & Pain
• What does “pain” look like?
• Pain evaluation is based on:
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Location of pain
Duration
Intensity (1-10 scale)
Precipitating factors
• Pain may be Acute or Chronic:
– Acute-short duration, responds to analgesics
– Chronic-over time, less responsive to analgesics, tolerance
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Types of Analgesics
3 Classes
Opioid
Non-opioid
Adjuvant
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Opioids & Opiates (Narcotics)
• OPIOID – a derivative of opium
• OPIATE – a synthetic chemical that produces an
analgesic effect similar to opium.
• Examples: codeine, morphine (opioids) &
oxycodone, fentanyl, meperidine (opiates)
• Reduces pain from any origin
• CAUTION: Tolerance and physical dependence
• Many are Schedule II controlled substances
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Narcotic Analgesics Side Effects
• Euphoria, Sedation, Confusion
• Slowed reaction time
• Respiratory depression (in major overdose
situations)
• Nausea, stomach upset
• Constipation
• “Idiosyncratic” (restlessness & agitation)
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Drug Interactions with Narcotics
• Alcohol & other CNS depressants can lead to
Respiratory depression
*Sedatives
*Antihistamines
* benzodiazepines
• What drug is used to treat narcotic overdose?
--- naloxone (Narcan)
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Non-opioid Analgesics
• For mild to moderate pain
1. Not related to morphine
2. Work on peripheral nervous system,
not the CNS (outside brain, spinal cord)
3. Do not produce physical dependency
and tolerance
4. Do not alter consciousness or mental
function
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Non-opioid Analgesics
• low-intensity pain of inflammation and dull
aches and vague pain
• Fever reduction
• Used as
-analgesic
-antipyretic, and/or
- anti-inflammatory
• Not every drug in this class has all 3 effects
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more info on Non-opioid Analgesics
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Typically the first step in pain control
OTC or Rx
Less expensive that Narcotics
combined with narcotics to become Rx items:
* Hydrocodone+APAP *Hydrocodone+ibuprofen *Oxycodone+APAP
• May be combined with non-narcotics to
become Rx or OTC items:
– ASA+caffeine -APAP+caffeine+butalbital (Fiorocet)
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Salicylate Analgesics (aspirin”ASA”)
• Oldest non-opioid analgesics; not for children
• Four distinct therapeutic actions of ASA:
– 1. Analgesic – inhibits prostaglandin release from damaged
tissues
– 2. Anti-inflammatory—reducing prostaglandin synthesis
– 3. Anti-pyretic—reduces fever by causing vasodilation
– 4. Anti-coagulant—prevents platelets from aggregating (clump)
to decrease clot formation
• Beware GI effects, bleeding out
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Acetaminophen (APAP)
• Analgesic & Antipyretic actions ONLY
• why use APAP over ASA?
– Can be used in all ages (including children)
– Rarely causes GI upset and bleeding
– ok with anticoagulation medications
• Main disadvantage –liver damage w/ long term
use, high dosages, or heavy alcohol use
• NMT (no more than) 3 grams (3000-mg) in 24
hours for adults with normal liver function!
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Non-steroidal Anti-inflammatory
(NSAID’s)
• ibuprofen (Advil®, Motrin®), naproxen (Aleve®)
• for mild to moderate pain
• for inflammatory conditions, dysmenorrhea,
dental pain
• S/E- GI … stomach upset, bleeding
• Do not take with ASA, APAP or other NSAID’s.
• Time limits: 10 days for pain, 3 days for fever or
as directed by MD
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World Health Organization (WHO) Pain Ladder
•Mild Pain- take APAP, ASA, or NSAIDS
around the clock
•Moderate Pain- add mild opioid (codeine or
hydrocodone)
•Severe Pain-D/C mild Opioid, give strong
opioid (hydromorphone or morphine), while
continuing the non-opioid. [a word about
meperidine (Demerol)]
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Adjuvant Analgesic
• Used to enhance analgesic efficiency and prolong effects of opioid
medications
• Typically not prescribed alone for pain
• Goal = Decreasing amount of pain medication while increasing pain
control
• to reduce side effects of analgesics (ex: nausea)
• Examples:
– Tricyclic Antidepressants (amitriptyline) *treat dull aches
– Corticosteroids (prednisone) *treat inflammation
– Anti-Convulsants (lorazepam, phenytoin, gabapentin) *treat sharp,
shooting, or burning pain
– Antihistamines (hydroxyzine) *treat anxiety/nausea
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------ THANKS ------
Have a great week!
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