Neuro Block 2 Drugs

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Parkinsons Drugs

"BALSA" --bromocriptine, amantadine, levodopa (carbidopa), selegiline, antimuscarinics

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Benzotropine/Trihexyphenidyl
Diphenhydramine (benadryl)
L-Dopa
Carbidopa
Bromocriptine
Ropinirole
Pramipexole
Selegiline
Rasagiline
Tolcapone/Entacapone
Amantidine

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Benzotropine/Trihexyphenidyl

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"Park my M1-Benz"
-M1 muscarinic agonist w/ mild dopamine reuptake blocking properties (HIGH DOSES)
-Used when CIs exist for dopaminergic stimulation, or when other tx fails
SE: parasympathetic excess (DUMBBELLS)
CI: can't use w/ glaucoma pts, elderly, BPH

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Diphenhydramine (Benadryl)

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H1 partial agonist (inverse agonist?)--antihistamine
-Injectable for DA block-induced acute dystonias (eyeballs roll up in socket and lock)

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L-Dopa (levadopa)

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-readily crosses BBB and is rapidly converted to dopamine
-Start dose low to prevent vomiting and reduce bouts of hypotension; must titrate individual doses
SEs: Hypotension, N/V, affective disturbance (w/ high doses), increased sexual activity, DYSKINESIA (abnormal movements after 1 yr)
Interaxns: DO NOT USE w/ antipsychotics, nonspecific MAOIs(LETHAL!!!),

* Anti-ACh drugs potentiate effects*
CI: Melanoma, glaucoma

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Carbidopa

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-Used w/ L-DOPA to reduce dosage
-Carbidopa can't cross BBB thus only the dopamine that crosses can get converted-
-inhibits peripheral aromatic AA decarboxylase
CIs: Anti-psychotics, Nonspecific MAOIs (HTN crisis)
**use w/ anticholinergic to to potentiate effects

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DA Agonists:
Bromocriptine, Ropinirole, Carbergoline, Pramipexole

"Add the Bros, ropes, and prams IMPULSIVELY when CONTROL(ling) things get rough"

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**THESE ARE OFTEN USED AS ADDITIONS TO THERAPY**
DA Agonists
Bromo- D2
Ropinirole- D3 >D2
Pramipexole- D3/D4; Alpha 2
***Pramipexole is an Alpha2 agonist too-- causes sedation
--can be used as first lines, but usually as supplements when Carbidopa and L-dopa starts to fail
--Bromocriptine is very expensive-- therefore later use is preferred

Ropinirole and Pramipexole produce LESS dyskinesias than others;
SEs: somnolence and impulse control disorders

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Monoamine Oxidase B Inhibitors (MAOBIs):
Selegiline, Rasagiline

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-Used in Early Parkinson's
-Rasagiline is IRREVERSIBLE
-potentiate L-dopa and help stabilize levels
-beginning to be 1st line
Selegiline--->amphetamine
*MAO(B) is selective for dopamine
"Sel(l) amphetamines; Rasagiline is iRReversible

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Catechol-O-methyltransferase (COMT) Inhibitors:
Tolcapone and Entacapone

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-Use w/ L-DOPA
-Same SEs as DA agonist; potentiates L-Dopa side effects, nausea, anorexia, diarrhea, hallucinations
**TOLCAPONE- hepatotoxic
Don't use with nonspecific MAOIs

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Indirect Dopamine Agonists:
Amantidine

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-weakly blocks glutamate receptors to increase dopamine release
-prophylaxis for A2 flu
-SEs less severe than dopamine
used LATE in TX

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Anti-spasmodics:

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Cyclobenzaprine/Mataloxone/carisoprodol/methocarmanol; benzodiazepines/diazepam/clonazepam; baclofen; tizanidine; dantrolene; carbamazepine, oxcarbazepine, gabapentin

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Cyclobenzaprine/Mataloxone/carisoprodol/methocarmanol

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MOA: Muscle relaxants w/ sedation effects
Anticholinergic effects (Blocks DUMBBELLS)
Indications: musculoskeletal issues (sprains/strains)
"The CYCLe of Benz's MAToxALONE (the CARiSoPROdol); can make METHoCarMANOL"
^^lots of car names; muscle relax

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GABA-A Agonists
"Ben and his clonez' a pain-- they GABA-(A) all ZA time; let's sedate 'em"
"Oh you'll tolerate them quickly"

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benzodiazepines/diazepam/clonazepam
--Indications: muscle relaxant, anti-anxiety, tx of spinal transections; muscle trauma
-sedating effects
---TOLERANCE develops quickly

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Baclofen
"Bac off-- you're hyperpolarizing me; Ca2+ can't get near me; but not too fast; i'll go crazy!"

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increases K+ conductance in terminals; reduces Ca2+ influx after an AP
indications: spinal cord injury, MS, movement disorder, ALS
SEs: Sedation/weakness/lassitude/WITHDRAWAL IS BAD; MUST WEAN; OD is very dangerous

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Tizanidine

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Alpha-2 agonists; presynaptic for Motor neurons;
decreases NE release
indications: MS, stroke, spinal cord damage
SEs: sedation, dry mouth, dizziness

**less hypotension problems than clonidine
"Taz needs to relax"

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Dantrolene

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causes decreased Ca2+ release from SR;
SEs: muscle weakness, dizziness, fatigue
HEPATOTOXIC
Uses: malignant hyperthermia; neuroleptic malignant syndrome
"Dan'z weak muscles are makin' him dizzy; he couldn't get enough Ca2+ from his SR so now his liver's failing"

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Anti-convulsants:
carbamazepine, oxcarbazepine, gabapentin

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Off-label use for those not responding to other tx

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Non-opioid pain analgesics:

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Aspirin/NSAIDs; corticosteroids; capsacin; ketamine; duloxetine/tricyclic antidepressants/milnacipran/venlafaxine; gabapentin/pregabalin

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Aspirin/NSAIDs

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Decrease synthesis of prostaglandins by inhibiting COX analgesia, inflammation
GI upset/ulcers
Aspirin: don't use in Pts under 12 yrs

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Corticosteroids

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Inhibits synthesis of prostaglandins, leukotrienes by inhibition of phospholipase A2
Analgesia, inflammation
SEs: causes adrenal suppression, altered carb metabolism, glaucoma/cataract risk, etc ----MUST WEAN OFF of this

CIs: Peptic ulcer, HD, HTN w/ HF, psychoses, DM, osteoporosis, glaucoma

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Capsaicin

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derived from hot peppers, releases substance P in periphery, inhibits accumulation of substance P---> depletion and causes local analgesic effect
topical tx for herpes zoster/arthritis/HIV neuropathy/shingles

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Ketamine

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Blocks NMDA type receptors to prevent a post-synaptic response;
widely used for vet med but only for brief procedures in humans
blocks CNS sensitization to pain
potential for hallucinations

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Duloxetine, tri-cyclic antidepressants, milnacipran, venlafaxine

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Block reuptake of NE and 5-HT in tx of chronic pain
relief from chronic pain more rapid and at lower doses than tricyclics;

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Anticonvulsants: gabapentin/pregabalin

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Tx for pain from neuralgias
MOA involves ability to prolong inactivated state of Na+ channels; and blocks subunit of Ca2+ channel; can use w/ morphine to potentiate effects
**neuropathic pain/allodynia**
"pre gab, a pen blocks my Na+ channels"

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Endogenous Opiods/Receptors:

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Enkephalins; Beta endorphins; dynorphan

*have very large precursor molecules; very laborious/E intensive to produce
-use for special circumstances

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Enkephalins

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MET/LEU pentapeptides-- NT like; localized in interneurons; rapidly degraded by enkephalinases

-concentrate in GP/caudate/SN

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Beta Endorphins

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31 AA peptide chain; enkephalinase resistant;
HORMONE and NT type actions; derived from proopiomelanocortin
found in pituitary---> hormonal fn; long axoned neurons in hypothalamus
**Mu opioid receptor**

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Dynorphan

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derived from prodynorphan; 8/9 AA sequence or 13/17--- peptidase resistant

has both NT and hormone like actions
posterior pituitary, brainstem, hypothalamus, cortex, hippocampus, spinal cord

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Opiod Analgesics

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morphine, methadone, codeine, propoxyphene, fentanyl, oxycodone/oxcontin, hydrocodone, tramacol, tapentadol, meperidine, buprenorphine

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Morphine

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MOP (mu opiod receptor) agonist; opiod prototype;
classic effects: miosis, respiratory depression, hypothermia, indifference to pain/euphoria, GI and physical dependence
**gets converted to M-6-glucaronide (more potent/longer lasting)
-Indicated for analgesia at multiple levels
-SEs: drowsiness, mental clouding, miosis, constipation, biliary constriction, dose-dependent euphoria, reduced resp due to decreased sensitivity to CO2, N/V, suppression of baroreceptor reflex, mild CV effects, increased ICP

CI: obesity, asthma, cor pulmonale, emphysema

*use scheduled lower doses to prevent recurrence of pain rather than repeatedly suppressing pain when it occurs, pt controlled analgesia gives better relief w/ lower dose;
OD sxs: resp depression, coma pinpoint pupil

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Methadone

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Synthetic drug, very similar to morphine
longer acting b/c it is highly bound to plasma proteins and is better absorbed orally
*useful in heroin abuse
SEs: CY3A4 metabolite, renal failure and neuropathic pain
*age is imp for dosage

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Codeine

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MOA: biotransformation to morphine via CYP2D6;
Indications: cough, mild pain, diarrhea
SEs: resp depression, constipation, low possibility of addiction
good oral drug

**being phased out**

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Propoxyphene
"Props, oxypene, you a WEAKER clone of methadone"

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Congener of methadone; no superiority over codeine and ASA when toxicity is considered
SEs: toxic psychosis

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Fentanyl
"Vent, fent!" but quick, pop, spray, or patch?

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-pure MU agonist; synthetic
-EXTREMELY potent; short acting
-used for neuroleptic anesthesia (when pt needs to be aware and cooperative)
-patch, lozenge, or nasal spray
SEs: resp depression, constipation, addiction

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Oxycodone/oxycontin

"The oxyMOPS are more available than morphine"

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better oral availability than morphine;
use w/ naloxone to reduce constipating effects
Indication: analgesic
sustained release form: oxycontin

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Hydrocodone

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partial mu agonist; high oral availability; common in outpatient use

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Tramadol

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Synthetic drug; good for moderate pain
weak opioid; MOA= block reuptake of NE and 5-HT
2D6 metabolism--
SEs: N/constipation/drowsiness;

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Tapentadol

"Tap on the tram"

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MOP agonist; NE uptake inhibitor
more efficacious than tramadol but less than morphine; greater safety than morphine
no biactivation necessary

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Meperidine

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Anticholinergic properties
Synthetic;less biliary spasms seen
WIDELY ABUSED
Indications: biliary colic
CIs: cardiovascular dysfunction; elderly (seizures/delirium)
TOXIC; renally cleared metabolite
DO NOT USE w/ nonspecific MAOIs---LETHAL

--derivates- lomotil= good for tx of diarrhea
loperamide- antidiarrheal effects and less abuse potential than diphenoxylate bc it doesnt cross BBB; causes increased anal sphincter tone
POORLY SOLUBLE IN WATER (spastic colon indications)

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Buprenorphine

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highly lipophilic; 25-50x more potent than morphine; MOP partial agonist; high doses ppt withdrawal
allyl substitution at pos 17
respiration depression reaches a ceiling at low doses
used to tx opioid dependence
binds extensively to protein

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Opioid Mixed Agonists/Antagonists

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Pentazocine
Nalbuphine
Butorphanol

**KOP agonists**

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Pentazocine

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Used for analgesics; weak MOP block; ceiling on respiratory depression; high doses are stimulatory/ppt withdrawal; lower abuse potential, antagonizes certain effects of morphine;

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Nalbuphine

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KOP and MOP antagonist; used for analgesia; SEs: resp depression, pentazocine-like cardiovascular effects

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Butorphanol

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increase in cardiac work load--- limiting factor
almost pure KOP; little mu binding; ceiling on resp depression due to kappa effects

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Opiod Antagonists--- pure MOP antagonists

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Naloxone
Naltrexone
Methylnaltrexone

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Naloxone

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very short acting;
significant 1st pass metabolism

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Naltrexone

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LONG acting; orally effective, survives 1st pass; adjunct in opioid/alcohol abuse

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Methylnaltrexone

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used for constipation; doesn't cross BBB