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130 Cards in this Set

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agents used for inflammation (3)
glucocorticoids - chronic use limited by toxicity
SAARDs - slow acting antirheumatic drugs
DMARDs - disease modifying antirheumatic drugs
NSAIDs are excreted by the _________

must decrease dose in ________ disease
kidney

renal
NSAIDs Indications (4)
Rheumatoid arthritis
osteoarthritis
local MS sydromes (sprains)
gout - execept tolmentin
Aspirin inhibits __________ synthesis and inhibits _________ aggregation
prostaglandin

platelet
Aspirin indications (5)
TIA
MI
Unstable angina
coronary artery thrombosis
to decrease incidence of colon cancer
Aspirin adverse effects:
GI ___________
__________________
____________
renal toxicity
______
asthma
bleeding

gastric & duodenal ulcers

hepatotoxicity

rashes
High doses of aspirin causes salicylism - _________,________,_________,_________
vomititng, vertigo, tinnitus, decreased hearing
Aspirin toxicity tx:
__________ within 4 hrs
NaHCO3 infusions to alkaline urine
__________ assistance as needed
gastric lavage

ventilatory assistance
NSAIDs - Non Acetylated Salicylates

Mg choline salicylate and Na salicylate

_____________ agent
less effective analgesic
less effective cycloogenase inhibitor
used for _________ and _________
anti-inflammatory

asthma and blood dyscrasias
NSAIDs - Cox 2 selective inhibitors

MOA: inhibits _________ synthesis

Effects: analgesic, antipyretic, anti-inflammatory

do not offer ______________ effects of traditional NSAIDs
prostacyclin

cardioprotective
NSAIDs - Cox 2 selective inhibitor indications (6)
OA
RA
gouty arthritis
famililial adenomatous polyposis
acute MS syndromes
ankylosing spondylitis
NSAIDs - Cox 2 selective inhibitors: Celecoxib (________)

effective against ___ and ___
fewer _______ than most NSAIDs
it's a __________ - may cause rash

dose - ____/____ mg PO bid
Celebrex

RA and OA

ulcers

sulfonamide

100/200
NSAIDs - Cox 2 selective inhibitors: Valdecoxib (_________)

indications - primary dysmenorrhea, OA, RA

dosages
dysmenorrhea - ____ mg PO qd prn
OA/RA - _____ mg PO qd

serious rxns reported in _____________ sensitive pts
Bextra

20

10-20

sulfonamide
NSAIDs - Cox 2 selective inhibitors: Rofecoxib (_______)

indications - RA, OA, dysmenorrhea

dosages
dysmenorrhea - ____ mg PO qd x5 days
OA/RA - _____ PO qd

withdrawn b/c of strokes
Vioxx

50

12.5-25
NSAIDs - Cox 2 selective inhibitors: Etoricoxib (Arcoxia)

newest cox 2 inhibitor

dosages
OA/MS pain - _____ mg PO bid prn
RA - _____ mg PO qd
Gouty arthritis - ______ mg qd
60

90

120
NSAIDs - Cox 2 selective inhibitors: Meloxicam (_________)

popular in Europe, approved in the US for _____

fewer ___ symptoms & complications

not as selective as other Cox 2 inhibitors
Mobitz

OA

GI
NSAIDs - Nonselective Cox 2 inhibitors: Diclofenac
(________, _________)

diclofenac + _________ or _________ = < GI effects

dose - _____ mg qd

0.1% opthalmic soluntion - prevent post op ___________
3% topical gel - ____________
Cataflam, Voltaren

misoprostol or omeprazole

150

inflammation

solar keratosis
NSAIDs - Nonselective Cox 2 inhibitors: Etodolac (________)

indicated for post op pain after ________
causes less ___ toxicity

dose - ______ mg q6-8hrs
XL formulation - _______ mg PO qd
Lodine

CABG

GI

200-400

400-1000
NSAIDs - Nonselective Cox 2 inhibitors: Fenoprofen (________)

most associated with ____________

adverse effects:
_______, dyspepsia, perpheral edema, _____, puritis, ________
Nalfon

interstitial nephritis

nausea

rash

tinnitus
NSAIDs - Nonselective Cox 2 inhibitors: Flurbiprofen (_________)

dose - _______ mg qd

rarely can cause:
_________,__________,________
Anasaid

200-400

cogwheel rigidity, ataxia, tremor
NSAIDs - Nonselective Cox 2 inhibitors: Ibuprofen (________)

also effective in closing a _____________ - ______ mg IV at
12-24hr intervals

dose - max of _____ mg/day
Motrin

patent ductus arteriosus

0.1-0.25

2400
NSAIDs - Nonselective Cox 2 inhibitors: Ibuprofen

adverse effects:
GI irriation & bleeding (< than with aspirin)
_______,__________
acute renal failure
________ retention
interstitial nephritis
________ syndrome
hepatitis
aseptic meningitis in pts with SLE
rarely, agranulocytosis & aplastic anemia
Rash, Pruritis

fluid

nephrotic

meningitis
Ibuprofen contraindications (3)
bronchospams rxn w/ aspirin
nasal polyps
angioedema
NSAIDs - Nonselective Cox 2 inhibitors: Indomethacin (________)

indications:
rheumatic conditions including JRA
gout
____________
PDA - given IV
________
nephrotic syndrome
__________ inflammation
Indocin

ankylosing spondylitis

pleurisy

conjunctiva
NSAIDs - Nonselective Cox 2 inhibitors: Indomethacin

Adverse effects:
GI - __________, ______, ________
CNS - _________, ________
Hematologic - ____________, __________
Renal failure

Contraindications (2)
hemorrhage, pain, diarrhea

headache, dizziness

thrombocytopenia, aplastic anemia

nasal polyps & angioedema
NSAIDs - Nonselective Cox 2 inhibitors: Ketorolac (________)

not an __________ like other NSAIDs
has replaced _________ in some situations

dosages
PO - ____ mg PO q6hrs (max 40mg/day)
IM - ____ mg x1, then 30mg q6hrs (max 120mg/day)
IV - ____ mg x1, then 30mg q6hrs x5days (max 120mg/day)

reduce dose in renal dz
Toradol

anti-inflammatory

morphine

10

60

30
NSAIDs - Nonselective Cox 2 inhibitors: Naproxen (__________)

available OTC as ________
ADR - ___________ incidence is low but twice that of ibuprofen

dose - ____ mg PO bid or tid (max 1500mg/day)
Naprosyn

Aleve

GI hemorrhage

500
NSAIDs - Nonselective Cox 2 inhibitors: Nabumentone (________)

half life doubles in _______ impairment
may cause ___________ is some pts

dose - ______ mg qd
Relafen

renal

photosensitivity

1500-2000
drugs used in gout (4)
cochicine
NSAIDs
Uricosuric agents
Allopurinol
Gout Therapy: Colchicine

Dosages
Prophylatic: ___ mg PO bid or tid
Tx of attack: ___ or ___ mg followed by 0.6mg PO q2hrs
___ mg in 24hrs could be fatal
treatment and prevention

0.6

0.6 or 1.2

8
Colchicine adverse effects:
_______ - most common SE
_____ & abdominal pain
peripheral _________
myopathy
may cause _________ and __________
diarrhea

N/V

neuritis

hair loss and bone marrow depression
Colchicine intoxication:
bloody ________
burning
______ pain
_________
oliguria
fatal _________

TX - _________
diarrhea

throat

hematuria

CNS depression

supportive
Gout Therapy: NSAIDs

_________ is used in place of colchicine

dose - ____ mg PO q6hrs x3 doses or until response occurs, then 25mg PO q6hrs x5days

treats acute attack but not for prevention b/c of ___________
indomethacin

50

renal toxicity
Gout Therapy: Uricosuric Agents - Probenecid (________)

not used as 1st line tx, only used when attacks are not controlled by other agents

dose - ____ mg PO bid (max 2-3 g/day)

Also Sulfinpyrazone

don't start therapy till ____ wks after an attack
Benemid

250

2-3
Uricosuric agents adverse effects:
_____ irritation
Allergic _________
__________ w/ probencid use
aplastic anemia - rare
GI

dermatitis

nephrotic syndrome
Gout Therapy: Allopurinol (________)

dose - ____ mg qd but depends on serum uric acid level

use in acute attack in combo w/ something else
Zyloprim

100-300
Allpurinol Indications:
chronic _____________
when 24 urine exceeds ____ mg
when there are ADRs to other uricosuric agents
recurrent __________
serum urate levels grossly elevated
goal < ___ mg/dL
tophaceous gout

600-700

renal stones

6.5
Allopurinol adverse effects:
GI effects - _______, _______, _______
peripheral neuritis
allergic skin rxns - ___________
rarely - exfoliate dermatitis, necrotizing vasculitis, bone marrow depression
nausea, vomiting, diarrhea

maculopapular rash
Allopurinol drug interactions:
inhibits metabolism of ___________ and oral ___________
may increase effects of _______________
reduce dose by 75% if also taking _____________
Probenecid

anticoagulants

cyclophosphamide

mercaptopurine
Rheumatoid Arthritis Agents

________ - Offer symptomatic relief & decrease inflammation
Have little effect on progression of bone & cartilage destruction

________ - Arrest or slow progression of bone & cartilage destruction
Effects may take 6wks to 6 months to be evident
NSAIDs

DMARDs
Methotrexate
Azathioprine
Penicillamine
Hydroxychloroquinolone
Chloroquine
Organic gold compounds
Sulfasalazine
Leflunomide
Tumor Necrosis Factor blocking agents
Immunoadsorption apheresis
DMARDs
DMARDs: Methotrexate

1st DMARD of choice in treatment of ____

dose - _______ mg weekly PO
Increased effects seen with doses up to 30 or 35mg weekly
RA

7.5 - 15
DMARDs: Methotrexate Adverse Effects

Nausea & ___________
Progressive dose related __________ - enzyme elevation
Liver cirrhosis (<1%) rare
Myelosuppression
______________ reaction- rare hypersensitivity lung reaction with SOB
mucosal ulcers

hepatotoxicity

Pseudolymphomatous
DMARDs : Methotrexate Adverse Effects

Prevention - GI & liver function test abnormalities decreased with use of _________ 24hrs post each dose

Contraindicated - __________
leucovorin

Pregnancy
DMARDs: Chlorambucil (________)

Indications: _____ and ________ disease

Adverse Effects:
_________ suppression
_________
Amenorrhea
Risk of ________ increased 10 fold after 3yrs
Leukeran

SLE and Behcet’s disease

Marrow

Infertility

leukemia
DMARDs: Cyclophosphamide(__________)

______ suppression correlates with clinical response

Indications:
RA
Vasculitis
SLE
Wegener’s granulomatosis
Other Rheumatic conditions
Cytoxan

T cell
DMARDs: Cyclophosphamide

Adverse Effects
________ in both men & women
__________ suppression
Alopecia
Hemorrhagic ________
_________ Ca (rare)
Infertility

Bone marrow

cystitis

Bladder
DMARDs: Cyclosporine (_________, _________)

Indications:
_____
Maybe used in SLE, Dermatomycosis, Wegener’s gramulomatosis etc

Dose:
___ mg/kg/day divided into 2 doses
Available in 25mg, 100mg caps
Solution ___ mg/ml (Neoral)
Neoral, Sandimmune

RA

3-5

100
DMARDs: Azathioprine (_______)

Indications:
_____
Studies show efficacy in _________ arthritis, polymyositis, SLE

Dose: __ mg/kg/day
Available in 50mg,75mg, 100mg
Imuran

RA


psoriatic

2
DMARDs: Azathioprine

Adverse Effects:
___ disturbances
Bone marrow suppression
Increase in _________ risk
Increased risk for _________
Rarely, rash
Rarely hepatotoxicity
GI

infection

lymphoma
DMARDs: Myophenolate (________, _________)

Indications:
Tx of _______ disease due to SLE
___________________
RA (few controlled studies exist)

Dose: __ gm/day in 2 divided doses
Tabs, caps- 250mg, 500mg

Adverse Effects:
____ Effects
_________ effects
_________ toxicity
Cellcept, Myorfortic

Wegener’s granulomatosis

renal

2

GI

Hematologic

Hepatic
DMARDs: Chloroquine & Hydroxychloroquine

mainly for _______

Indications
____ - not considered efficacious DMARD
_________
Joint Pain of _____
malaria

RA

Serositis

SLE
DMARDs: Choroquine & Hydroxychloroquine

Dose:
___ mg/day for chloroquine
___ mg/kg/day for hydroxychloroquine

Adverse Effects:
_______ toxicity for doses >250 mg/day of chloroquine or doses >6.4 mg/kg/day of hydroxychloroquine
GI- __________
_________
________
200

6.4

Ocular

Abdominal pain

Nightmares

Rashes
DMARDs: Gold Compounds (_________)

Adverse Effects:
Hematologic abnormalities - __________, leukopenia, even pancytopenia & aplastic anemia
__________
Neuropathy
Rash
_________ Syndrome

Dose: __ mg PO bid or __ mg PO qd
Auranofin

thrombocytopenia

Jaundice

Nephrotic

3

6
DMARDs: Penicillamine

A metabolite of __________ & analogue of amino acid ________

Rarely used today because of toxicity
penicillin

cysteine
DMARDs: Sulfasalazine

Metabolized to sulfapyridine

Indications:
___ - reduces rate of appearance of new bone damage
_______
_______________

Dose: ___ gm/day
RA

JRA

Ankylosing spondylitis

2-3
DMARDs: Sulfasalazine

Adverse Effects:
____________
__________
Rash
_________ anemia
Neutropenia
Methyglobinemia
Drug induced jaundice (rare)
Reversible infertility in _____
Nausea/vomiting

Headache

Hemolytic

men
DMARDs: TNF α Blocking Agents

TNF α blocking agents combine with TNF to inhibit effect of endogenous __________

3 TNF agents approved by the FDA:
Adalimumab
Infliximab
Etanercept
cytokines
DMARDs: TNF α Blocking Agents - Adalimumab (________)

Indications:
RA – Can use as monotherapy or in combination with ___________
_________,__________

Dose: __ mg SQ once weekly
Humira

methotrexate

Juvenile RA , Psoriasis

40
DMARDs: TNF α Blocking Agents - Adalimumab

Adverse Effects:
Risk of macrophage dependent infection - usually ___ & other opportunistic infections
Screen for latent or active TB prior to adm.

Rarely __________
TB

leukopenia
DMARDs: TNF α Blocking Agents - Infliximab (_________)

Dose: ____ mg/kg IV infusion
typical 3-5mg/kg Q 8weeks

Indications:
RA
_____________
___________
Giant cell arteritis
__________ arthritis
Juvenile chronic arthritis - Should be used with _____
Can be used with other DMARDS – cyclosporine, Azathioprine
Remicade

3-10

Ulcerative Colitis

Sarcodosis

Psoriatic

MTX
DMARDs: TNF α Blocking Agents - Infliximab

Adverse Effects:
GI- _____
HA/___________
Rash
_______
Could be associated with latent ____- screen
Other opportunistic infections
N/V

sinusitis

Cough

TB
DMARDs: TNF α Blocking Agents - Etanercept (_______)

Dose: ___ mg SQ 2x/weekly (50mg/wkly)

Indications:
RA
Juvenile chronic arthritis
Psoriatic arthritis
Ankylosing spondylitis - Use as monotherapy or w/ ____
Enbrel

25

MTX
DMARDs: Leflunomide (______)

Indications: ____

Adverse Effects:
______ - 25%
Increase liver enzymes
Alopecia
Wt gain

Dose: LD ___ mg PO qd x3 days, then ______ mg PO qd
Tab 10mg, 20mg,100mg
Arava

RA

Diarrhea

100

10-20
Immunoabsorption Apheresis

Apheresis of _____ ml of plasma wkly x3 months
Recommended for patients who have failed numerous other therapies

Indications: _____

Adverse Effects:
_______ Pain & Swelling
____________
Nausea, rash, Pruritis (1-6%)
1200

RA

Joint

Hypotension
Skeletal Muscle Relaxants:
Drugs that affect skeletal muscle - 2 categories

Used during surgical procedures (adjunct to general anesthesia) or in ICU setting to cause paralysis - ________________

Used to reduce spasticity in a variety of neurological conditions
Referred to as central muscle relaxants (except dantrolene) - _______________
Neuromuscular Blockers

Spasmolytics
Skeletal Muscle Relaxants: Neuromuscular Blockers

All have structural resemblance to ____________

Two categories exist:
________________ and ________________
acetylcholine

Non Depolarizing Agents and Depolarizing Agents
________________ agents:
Includes all NMBAs in US except Succinylcholine

_____________ - considered the prototype

Rate of elimination correlates with duration of action:
________ elimination – long t1/2, longer duration
________ elimination- shorter t1/2, shorter duration
Non Depolarizing

Tubocurarine

Renal

Hepatic
__________ Derivatives
Atracurium (Tracrium)
Cistracurium (Nimbex)
Doxacurium (Nuromax)
Metocurine
Mivacurium (Mivacron)
Tubocurarine
Isoquinolone
_____________ derivatives:
Pancuronium (Pavulon)
Pipecuroniun (Arduan)
Rapacuronium
Rocuronium (Zemuron)
Vercuronium (Norcuron)
Depolarizing agent - Succinylcholine
Steroid
Skeletal Muscle Relaxants: NMBAs: Non Depolarizing Agents - Rapacurium

Fastest onset of action than any non depolarizing agent
Shortest duration of action
Expected to be alternative to ___________ for rapid intubation
High incidence of ___________ - withdrawal from market
Succinylcholine

bronchospasm
Skeletal Muscle Relaxants: NMBAs: Non Depolarizing Agents - Atracurium (_________)

Inactivated spontaneously- _________ elimination/less hepatic metabolism
By product - _________ crosses Blood brain barrier to cause ____________
Tracrium

hoffman

landanosine

seizures
Skeletal Muscle Relaxants: NMBAs: Non Depolarizing Agents - Cisatracurium (________)

Forms less landanosine & releases less ___________
Has all the advantages of atracurium with less side effects
Has largely replace atracurium in clinical practice
Nimbex

histamine
Skeletal Muscle Relaxants: NMBAs: Non Depolarizing Agents - Mivacurium (__________)

Short duration of action; similar to Rapacurium
Large doses- signifcant release of _________, causing ________, __________, __________
Clearance - by plasma cholinesterase
Duration of action longer with impaired ________ function
Mivacron

histamine

hypotensionm, flushing, bronchospasm

renal
Skeletal Muscle Relaxants: NMBAs: Non Depolarizing Agents - Tubocurarine

cause motor weakness followed by skeletal muscle becoming placid & inexcitable
Large muscle (abdomen, diaphragm) resistant to blockade, but recover quickly

Dose - _______ mg/kg IV
Duration: ______ mins
0.1-0.5

45-60
NON Depolarizing Agents:
Longer duration of action
Longer onset of action
___________ - fastest onset followed by Rocuronium

Depolarizing Agents:
Short duration of action
Shorter onset of action
____________ only
Rapacurium

Succinylcholine
Skeletal Muscle Relaxants: NMBA: Depolarizing Agent - Succinylcholine

Charaterized by 2 phases:
Phase 1 - depolarization
Phase 2 - desentization

Short onset - < ____ secs
Short Duration - _____ mins
Dose - _____ mg/kg IV
60

5-10

0.75-1.5
Skeletal Muscle Relaxants: NMBA Adverse Effeects

_________ CV effect:
Vercuronium
Doxacurium
Cistracurium
Rocuronium

__________ CV effect:
Pancuronium –tachycardia by release of norepinephrine
Mivacurium produces hypotension (less)
Atracurium -produces hypotension (less)
Minimal

Moderate
Skeletal Muscle Relaxants: NMBA Cardiovascular Adverse Effects

Tubocurarine - produces ___________

Succinylcholine -
__________ if given with halothane anesthesia
__________ if 2nd dose given <5 min later (transient)
___________ causing cardiac arrest in burn, trauma & closed head injury pts
hypotension

Arryhthmias

Bradycardia

hyperkalemia
Skeletal Muscle Relaxants: NMBA Other Adverse Effects

Succinylcholine -
increased __________ & __________ pressure
__________ pain in large doses

_________,_________,_________ all cause bronchospasm
Intra-occular & Intragastric

Muscle

Tubocurarine, Mivacurium, Rapacurium
Skeletal Muscle Relaxants: NMBA: Effects on Disease

Myasthenia gravis - strongly _________ NMB effect

Advanced Age - Prolonged duration for ___________ agents due to poor renal & hepatic clearance

Severe Burns - __________ dose requirements for non depolarizing NMBA to block sufficient receptors
enhances

non depolarizing

Increased
Reversal of Non Depolarizing Agents

Neostigmine, Pyridostigmine - Antagonize Non depolarizing NMBA by increasing the availability of __________ at the motor end plate

Eduphronium - antagonizes neuromuscular blockade by inhibition of acetylcholinesterase. May be _____ effective than neostigmine in more pronounced blockade
acetycholine

less
Muscle relaxants maybe divided into two groups - _________ and __________ agents

_________ - only agent with direct action at the level of the nerve-muscle connection
Centrally acting agents and Peripherally acting agents

Dantrolene
Skeletal Muscle Relaxants Indications

To relieve the _________ of neuromuscular disease such as:
Multiple sclerosis
Spinal Cord Injury
Stroke
Pain relief of minor strain injuries
Control of muscle symptoms of tetanus
Prevent or treat ____________ in surgery (Dantrolene)
spasticity

malignant hyperthermia
Carisoprodol (Soma®)
Chlorphenesin (Maolate®)
Chlorzoxazone (Paraflex®)
Metaxalone (Skelaxin®)
Methocarbamol (Robaxin®)
Cyclobenzaprine (Flexeril®)
Dantrolene (Dantrium®)
Diazepam (Valium®)
Ophenadrine (Norflex®)
Baclofen (Lioresal®)
Skeletal Muscle Relaxants
Skeletal Muscle Relaxants - Diazepam (_________)

Spasmolytic Agent
Adverse Effects- ________, _______

Dose: ____ mg/day given in 2-4 doses
may increase to 60 mg/day
Available- 2mg, 5mg, 10mg tabs
Valium

sedation, apnea

2-10
Skeletal Muscle Relaxants - Baclofen (_________)

As effective as diazepam in reducing spasticity, but produces less _________

Dosages:
Spasticity - ____ mg PO tid (Max 100 mg/day)
Hiccups - ____ mg 2-3x/day
Dosage Form: tabs 10mg, 20mg

Intrathecal dose: ______ mcg/24hrs
Injection: For intrathecal use 50mcg/ml,500mcg/ml 5ml, 2000mcg/ml 5ml
Lioresal

sedation

5-10

10-20

50-100
Skeletal Muscle Relaxants - Baclofen Adverse Effects

PO admin: __________ - tolerance develops

Intrathecal admin:
can control severe spasticity & muscle pain in pts, unresponsive to meds given by other routes
Tolerance may develop after months
Excessive _________
_________ depression
_______
Challenges - maintenance of delivery catheter in __________ space
Advantages - improved quality of life in pts with spastic disorders
Drowsiness

somnolence

Respiratory

Coma

subarachnoid
Skeletal Muscle Relaxants - Tizanidine (________)

Reduces spasticity at doses that cause < ___ effects than clonidine

Adverse effects:
_________ (48%)
hypotension
Bradycardia
Dry mouth
Asthenia

Dose: ___ mg tid
Capsules: 2mg, 4mg, 6mg
Tablets: 2mg, 4mg
Hepatic/renal insufficiency- may need to dose adjust
Zanaflex

CVS

Somnolence

2-4
Skeletal Muscle Relaxants - Dantrolene (_________)

Treats spasticity & _____________

Dosages:
Spasticity - ___ mg PO qd, increased to 2-4x/day up to max of 100mg PO qid

Adverse Effect:
___________________
________,__________
Occasional hepatitis
Dantrium

malignant hyperthermia

25

generalized muscle weakness

Sedation, Dizziness
Skeletal Muscle Relaxants - Dantrolene (Dantrium)

Malignant hyperthermia - rare heritable disorder triggered by stimuli like ____________ and _________

MOA: Sudden & prolonged release of ________, with massive muscle contraction & lactic acid production increased body temperature

Dose - __ mg/kg IV
Repeat PRN to a maximum of 10 mg/kg
Prophylaxis - ____ mg/kg IV 1.5hrs prior to anesthesia
Dosage Forms -
Caps: 25mg, 50mg, 100mg
Inj: 20mg vials
general anesthetics and NMBA

calcium

1

2.5
Skeletal Muscle Relaxants - Botulinum Toxin

Has become popular for the TX of generalized spastic disorders e.g. ___________
cerebral palsy
Skeletal Muscle Relaxants - Agents for Acute Local Spasms (spasmolytics)

Relief acute muscle spasm caused by local tissue trauma or muscle strain

___________ (Flexeril)- regarded as prototype for group
Cyclobenzaprine
Cyclobenzaprine (Flexeril)

Structurally related to TCAs
Not effective for Tx of muscle spasm due to ___________ or ____________

Dose: _____ mg/day in 3 divided doses

Adverse Effects:
________
________
Transient Visual ___________
cerebral palsy or spinal cord injury

20-40

Sedation

Confusion

Hallucination
Relaxants - Agents for Acute Local Spasms (spasmolytics)-for relaxing stiff, sore muscles

Carisoprodol (Soma®)
Dose - ____ mg PO qid
Children (6-12yr) - 6.25 mg/kg PO qid
Tabs 350mg

Chlorphenesin (Maolate®)
Dose: ____ mg PO tid
Tabs 400mg

Chlorzoxazone (Paraflex®)
Dose: ____ mg PO 3-4x/day
Tabs 250,500mg

Metaxalone (Skelaxin®)
Dose: ____ mg PO 3-4x/day
Tabs 400mg
350

800

500

800
Relaxants-Agents for Acute Local Spasms (spasmolytics)-for relaxing stiff, sore muscles

Methocarbamol (Robaxin®)
Dose: ____ mg PO qid
IV __ gm q8hrs
Max duration of therapy for IV=3days
Children (tetanus only) 15 mg/kg/dose q6hrs (Max 1.8 gm/mg x 3days)

Orphenadrine (Norflex®)
Dose: ____ mg PO bid
IM/IV 60 mg q12h
Inj. 30 mg/ml 2ml
Tabs- 100mg
1500

1

100
Discrete time limited alterations in brain function
including changes in motor activity, autonomic function, consciousness or sensation
that result from an abnormal & excessive electrical discharge of a group of neurons within the brain
Seizures
__________ - Specific type of seizures where the attack is primarily manifested by involuntary muscular contractions

____________ - A condition characterized by recurrent (2 or more) seizures unprovoked by any immediately identifiable cause
Convulsions

Epilepsy
Seizure Etiology:

60-70% of patients- no specific cause of seizures can be identified

___________ - congenital malformations, perinatal injuries, neurologic disorders, metabolic, infections

___________ - head trauma, brain tumors, infections- common causes

__________ - cerebrovascular diseases, brain tumor

________ - 2-3times increased risk in persons with first degree relatives with epilepsy
Infants/Children

Young adults

Elderly

Genetic
Sleep deprivation
Fever emotional stress
Lack of food, alcohol withdrawal
Pregnancy, Menses
Sensory stimuli-television, reading

Pseudo seizures - psychogenic basis
Predisposing factors to seizures
Classification of Seizure Type

Generalized Seizures:
Generalized __________ (grand mal seizures)
_________ (Petit mal seizures)
Tonic/Atonic Seizures
Clonic & Myoclonic seizures
__________ spasms
tonic clonic

Absence

Infantile
Classification of Seizure Type

Partial Seizures:
________ partial seizures
________ partial seizures
Partial seizures ________________
Simple

Complex

secondarily generalized
localized onset of attack ascertained by clinical observation or electroencephalogram (EEG)

3 types exist- determined by the degree of brain involvement by the abnormal discharge
Simple
Complex
Secondarily Generalized
Partial seizures
Least complicated, characterized by minimal spread of the abnormal discharge.
normal consciousness and awareness present

e.g. patient may have sudden onset of clonic jerking of an extremity lasting 60-90secs

Residual weakness may last 15-30mins after attack
Simple partial Seizure
Has a localized onset but discharge becomes more widespread (usually bilateral and almost always involving the limbic system

Arise from temporal lobe -hypoxia, infection

Presentation-pt may have brief warning, followed by alteration of consciousness during which pt may stare or stagger or fall
Automatism may be present-swallowing, fumbling, walking

Lasts 30-120sec, after which pt recovers, but may feel tired or ill after attack
Complex Partial seizure
Partial seizure immediately precedes generalized tonic clonic (grand mal seizure)
Secondarily generalized partial seizure
No evidence of localized onset of seizure

5 Types:
Generalized tonic clonic (grand mal seizures)
Absence (Petit mal seizures)
Tonic/Atonic Seizures
Clonic & Myoclonic seizures
Infantile spasms
Generalized seizures
Most dramatic of epileptic seizures

Characterized by tonic rigidity of all extremities followed in 15-30sec by a tremor
then excessive jerking of the body lasting 60-120sec (clonic phase)

Pt usually left in a stuporous phase; tongue or cheek maybe bitten; urinary incontinence common
Generalized tonic–clonic (grand mal seizures)
Characterized by sudden onset & abrupt cessation

Duration- < 10sec; rarely>45sec

Consciousness is altered; mild clonic jerking of eyelids or extremities may occur

Attacks begin in childhood or adolescence; may occur up to 100x/day
Absence (Petit mal) seizure
Seen in a wide variety of seizures-generalized tonic clonic seizures, partial seizures, partial seizures, absence seizures & infantile spasm

Tx should be directed at the primary seizure type, rather than at the myoclonus
Myoclonic Seizure
Pt has sudden loss of postural tone
If standing, falls suddenly to the floor
If sitting head & torso fall forward
Seizure type found in children
Atonic Seizures
An epileptic syndrome, not a seizure type
Characterized by brief myoclonic jerks of the body with sudden flexion or extension the body & limbs

90% of pts have first attack before age of 1 yr
Most are mentally retarded

Cause unknown - infection, kernicterus, tuberous sclerosis, hypoglycemia
Infantile Spasms
MANAGEMENT OF EPILEPSY: PARTIAL SEIZURES & GENERALIZED TONIC-CLONIC SEIZURES

Till recently choice of drug limited to Phenytoin, carbamazepine, barbiturates

Tendency in recent decades to limit sedative antiseizure drugs like barbiturates & benzodiazepine to pts unable to tolerate other meds

Choice now between ___________ & ___________
carbamazepine & phenytoin
MANAGEMENT OF EPILEPSY: GENERALIZED SEIZURES

Drugs used for generalized tonic clonic seizures are same as for partial seizures; plus ___________
valproic acid
Drugs effective against absence seizures: Two are non sedative, therefore preferred

____________
____________
___________ - sedative effective but has dose related adverse effects, plus tolerance
Ethosuximide (Zarontin)

Valproic Acid (Depakene, Depakote)

Clonazepam
TX of Myoclonic Syndromes:

Use _________ - can use IV in acute phase
non sedating & effective

Alternatives:
_________, or other Benzodiazepines
______________ & _____________could be useful
Valproate

Clonazepam

Zonisamide (Zonegran) & Levetiracetam
Tx of Juvenile myoclonic epilepsy:

__________ is drug of choice,
followed by __________,___________

aggravated by __________, ___________
Valproate

lamotrigine, topiramate


phenytoin, carbamezapine
Rx of Atonic Seizures:
Often refractory to all available medications

__________& ___________ maybe beneficial

____________ - may improve control in some & worsen attacks in others

___________ - effective in some; limited by toxicity
Valproate & lamotrigine

Benzodiazepines

Felbamate
Rx of Infantile Spasms:
Meant to control seizures - no effect on mental retardation

Most pts get one course of IM ____________
____________ maybe equally effective
_______________ also used
Corticotropin

Prednisone

Benzodiazepines (clonazepam)
Rx of Status Epilepticus:

___________ - most effective
Adult Dose: ______ mg IV q10-20 mins up to 30mg in 8hrs

may cause ____________; effect not lasting
Diazepam

5-10

resp. depression
Rx of Status Epilepticus:

____________ - alternative to diazepam

Dosages:
Infants - ____ mg/kg IV slow over 2-5 mins (max 4 mg/dose) may repeat 2nd dose of 0.05 mg/kg in 10-15 mins PRN
Adults: __ mg/dose slow IV over 2-5mins. May repeat in 10-15 mins (Max dose 8mg)

Start long acting agent like ____________
Lorazepam (Adovan)

0.1

4

phenytoin
Tx of Status Epilepticus (SE):

IV _________ - was mainstay for continuing therapy for SE
Effective & non sedating

LD = ____ mg/kg IV at a maximum rate of 50mg/min

Monitor cardiac rhythm & BP especially in elderly
_________ toxicity from propylene glycol
Phenytoin

13-18

Cardiac
Tx of Status Epilepticus (SE):

IV ____________ - better parenteral agent
Prodrug of phenytoin

Dose: LD ______ mg PE/kg IV given at 150 mg PE/min
Maint.D = 4-6 mg PE/kg/day
Fosphenytoin

15-20
Rx of Status Epilepticus (SE):

For pts not responding to Phenytoin, __________ given in large doses of _______ mg IV to a total dose of 400-800mg

________________ - common complication
General anesthesia may be necessary in highly resistant cases

For pts in absence status, _________________ still drug of choice
Phenobarbital

100-200

Respiratory depression

benzodiazepines
ANTSEIZURE MEDICATIONS - PHENYTOIN (DILANTIN)

Indications:
__________ or __________ partial seizures
primary or secondarily generalized seizures
convulsive status epileticus

Adverse Effects: (concentration dependent)
________
_________ or ________ vision
__________

Idiosyncratic:
hepatoxicity
rash, exfoliative dermatitis
_____________ syndrome
Lupus like reaction
Simple or complex

Nystagmus

double or blurred

drowsiness

Steven-Johnson
ANTSEIZURE MEDICATIONS - DILANTIN

Adverse Effects: (Chronic)
______ hypertrophy
____________ neuropathy
Chronic ____________
__________
_____________ anemia
Osteoporosis
Acne

Dose (maintenance):
Adults - ____ mg/kg/day (300-500 mg/day)
Children ____ mg/kg/day
Steady state achieved in 1-3 wks if initiated at maintenance dose

Dosage Forms:
30mg, 100mg caps
30 mg/5ml, 125 mg/5ml(susp)
50 mg/ml phenytoin Na inj
Gum

Peripheral

cerebral damage

Hirsutism

Megalobasltic

4-6

4-10
ANTSEIZURE MEDICATIONS - DILANTIN

___ mg phenytoin Na equivalents/ml fosphenytoin sodium inject able solution for IV and IM use

Advantages:
first line agent for _________ seizures
inexpensive
IV form available

Disadvantages:
Dose dependent kinetics
drug interactions
chronic neurologic & connective tissue effect
50

partial
ANTSEIZURE MEDICATIONS - Levetiracetam (KEPPRA)

IV/PO

Indication: Adjunctive therapy in the treatment of ________ seizures in children & adults 4yrs of age & older

Time peak = 20-120 mins
Excreted 91% ________
Partial

renally
ANTSEIZURE MEDICATIONS - KEPPRA

Adverse Effect:
CVS - _________
CNS - _____________, _____________, ___________
Skin – ________, __________
GI - N/V, ____________, ____________, ____________, __________
MS – _____________, ____________
chest pain

Somnolence, asthenia, coordination difficulties

rash, ecchymosis

abdominal pain, constipation, diarrhea, gingivitis

arthralgia, back pain
ANTSEIZURE MEDICATIONS - KEPPRA

Dosages:
Adults - ____ mg IV/PO bid
Increase by 1000 mg q2wks to 3000 mg/day in 2 divided doses

Pediatric (4-<16yrs) - ___ mg/kg IV/PO bid or ___ mg/kg qd
May increase 20 mg/kg/day q2wks to a maximum of 60 mg/kg/day in 2 divided doses

Levetiracetam injection (500 mg/5mL) must be diluted in 100 mL of a compatible diluent and administered IV as a __-minute IV infusion
500

10

20

15