Pharm II Exam 3
Terms
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- AD potential factors
-
Inflammatory mediators
MAO-B
Glutamate and other excitatory mediators
NMDA
decrease in concentraion of certain NTs - AD DDX
-
D- Drugs and EtOH
E- Ears and Eyes
M- Metabolic, endocrine, nutritional
E- Emotional disorders
N- Neurologic Disease
T- Tumors and Trauma
I- Infection
A- Arteriosclerosis - Tacrine(Cognex) SE
- Cholinergic
- Donepezil(Aricept)SE
- Cholinergic
- Rivastigmine(Exelon) SE
- Cholinergic, especially GI
- Galantamine (Reminyl) SE
- Cholinergic, especially GI
- Drugs to Tx AD
-
Tacrine(Cognex)
Donepezil(Aricept)
Rivastigmine(Exelon)
Glantamine(Reminyl)
Vit E
Memantine (Namenda) - Vitamin E
-
Delayed institutionalization and delayed deline in ADLs
No significant change in cognition - Memantine (Namenda)
-
NMDA receptor antagonist
Indicated in mod to severe AD - Antianxiety Meds
-
Benzos
Buspirone
SSRI and SNRI - Benzos
-
Alprazolam (Xanax)
Chlordiazepoxise (Librium)
Clorazepate (Tranxene)
Diazepam (Valium)
Lorazepam (Ativan)
Oxazepam (Serax) - Buspirone
-
delayed onset of activity
doesn't work well on pts that have already taken benzos
start buspirone before ending the benzos - SSRI and SNRI
- LT therapy
- OCD
-
SSRI
TCA- Clomipramine - Estimated adherance to LT therapy
- 50%
- Insomnia RX
-
OTC:
H1 aantagonists (diphenhydramine or doxylamine found in Unisom)
L-tryptophan
valerian
melatonin
EtOH - H1 antagonists SE
- anticholinergic
- MOA of Benzos and Benzo Receptor Agonists
-
bind to GABA receptors in the brain
stimulating GABAergic transmission and hyperpolarization of neuronal mb - Effects of Benzos
-
sedative
anxiolytic
muscle relaxant
anticonvulsant - Non Benzos
-
Zaleplon (Sonata)
Zolpidem (ambien)
Eszopiclone (Lunesta) - Ambien CR
- slightly longer activity
- Rx meds used for sleep that shouldn't be
-
Antidepressants (trazodone, mirtazapine, doxepine, amitriptyline)
Antipsychotics (Seroquel and Zyprexa) - Ramelteon (Rozerem)
-
sleeper
melatonin-receptor agonist with activity at MT1 and MT2
not a controlled substance - How long do we treat for sleep...
- with the exception of the newest benzo receptor agonist (Eszopliclone)- all of these are indicated for Short term use
- Triazolam SE
-
anterograde amnesiacognitive imparedment
motor incoordination
dependance
rebound insomnia -
Sleep aid drug interactions
Triazolam
eszopiclone
zolpidem
zaleplon -
use with caution if using drugs that inhibit CYP3A4
like
ketoconazole
nefazodone
protease inhibitors fluvoxamine
grapefruit -
Half Lives
Fluazepam (Dalmane)
Temazepam (Restoril)
Esstazolam (ProSom)
Triazolam (Halcion) -
Fluazepam (Dalmane)- long
Temazepam (Restoril)- slow
Esstazolam (ProSom)- fast
Triazolam (Halcion)- fast -
Half Lives
Zaleplon (Sonata)
Zolpidem (ambien)
Eszopiclone (Lunesta) -
Zaleplon (Sonata)- ultrashort
Zolpidem (ambien)- short
Eszopiclone (Lunesta)- intermed - Azaspirodecanediones
- Busirone
- Benzo SE
-
tiredness
memory deficits
amnesia
diff concentrating
problems with balance and incoordination - Antidote to benzo OD
- Flumazenil IV
- SSRI, TCA and MAOi
- all considered int e tx of various anxiety d/o: esp OCD and Panic d/o
- Drug interactions with anxiolytics
-
additive effect of sedation or psychomotor imparment with EtOH
Cimentidine increases levels of benzos
high doses and clozapina= death
BCP increase the levels - Hypnotics with short half lives
- lead to rebound insomnia
- Hypnotics with long half lives
- associated with sedative effects and cognitive or motor imparment the next day
- Barbituates
-
amobarbital
pentobarbital
secobarbital - Nonbarb/Nonbenzo
-
ethchlorvynol
glutethimide
methyprylon
chloral hydrate- used in peds - L-tryptophan
-
involved in non-REM sleep stages
fatalities: eosinophilia myalgia syndrome - Melatonin
- pineal gland and secreted during the nighttime adn ot environmental darkness
- CI to hypnotic use
-
sleep apnea syndromes
excessive EtOH consumption
pregnancy
need for alert fxn during NL sleep period - Cautions for hypnotic use
-
Pts who are elderly
have a h/o heavy snoring
renal, hepatic or pulmonary dz
other medications concomittantly
suicidal tendencies
hazardous occupations - Antidepressants Drug Therapy
-
SSRI
SNRI
TCA
MAOI
heterocyclics - SSRI are as effective as
- TCA
- SSRI
-
Fluoxetine (Prozac)
Paroxetine (Paxil)
Fluoxamine (Luvox)
Citalopram (Celexa)
Escitalopram (Levapro)
Sertaline (Zoloft) - TCA
-
Amitriptyline (Elavil or Endep)
Nortriptyline (Pamelor or Aventyl)
Imipramine (Tofranil)
Desipramine (Norpramin or Pertofrane)
Doxepin (Sinequin)
Trimipramide (Surmontil
Amoxapine (Asendin)
Protryptyline (Vivactil) - Meds that can precipitate depression
-
methyldopa
resepine
hydralazine
clonidine
propanolol
amantadine
levodopa
barbs
benzos
EtOH
amphetamine
corticosteroids
estrogen
progesterone - SE of SSRI
-
GI
N/V
sedation/stimulation
sexual dysfunction
anorgasmia
tremor
insomnia
nervousness -
Proxetine (Paxil)
Fluoxetine (Prozac)
Sertaline (Zoloft) - GI upset with every increase in dosage
- Drugs that can casue seratonin syndrome
-
MAOI
Meperidine
St Johns Wart
Cold Remedies
Dextromethorphan
Sympathomimetics
Diet Pills - SE of TCA
-
Anticholinergic
sedation
dec cardiovascular
dec seizure threshold
orthosttic hypotn
wt gain
narrow angle glaucoma
sinus tach
dry mouth
constipation
blurred vision
urinary retention and hesitency - 4 major problems with TCAS
-
slow onset
efficacy only 60-70%
AE
Lethargy - TCA dosing
- start low and titrate slow
- SNRI
-
same SE as SSRI
slight inc in diastolic BP - Remeron (mirtazapine)
-
alt to SSRI
dec sex SE at inc doses - Nefazadone (Serzone)
-
related to Trazodone
inhibits neuronal uptake of seratonin and NE and has anticholinergic activity - TCA drug interaction
-
Cimentidine
MAOI - MAOI
-
do not alter cardiac conduction
little effect on HR
No tyramine containing food - MAOI Se
-
orthostatic hypotn
mild anticholinergic
delayed ejaculation - MAOI Drug Interactions
-
epinephrine
pseudoephrine
stimulants
amphetanmines
Levodopa
Meperidine - Heterocyclics
-
Amoxapine
Trazodone
Maprotiline
Buproprion - Associated with seizures
-
Maprotiline
Buproprion - Buproprion
-
dopamine agonist effect
Zyban- antismoking form - Fluoxetine
-
Prozac
Only agent approved for the tx of depression in children - Tetracyclic
-
Maprotiline (Ludiomil)
Mirtazapine (Remeron) - Triazalopyridine
-
Trazodone (Desyrel)
Nefazodone (Serzone) - Aminoketone
- Wellbutrin (Buproprion)
- SSNRI
-
Effexor
Cymbalta - Ts for Bipoloar d/o
-
Mood Stabilizers
Antipsychotics - Mood Stabilizers
-
Mainstay of therapy
Lithium
Valproate
Lamotrigine
Carbamazepine
Oxcarbazepine - Aptypical Antipsychotics
-
Olanzapine
queriapine - Tx of Bipolar d/o
- response may be seen in 7-10 days but you can add the use of an antipsychotic and get results in 3-5 days
- SE of Lithium
-
death
stupor
coma
CV collapse
seizure
fine hand tremor
GI upset (N, d, metal taste)
T wave flattening widening of QRS
DI
wt gain
hypothyroid
leukocytosis
teratogen
mild polyuria
polydipsia
muscle weakness
coarse tremor
confusion
sedation
lethargy
hyperreflexia
slurred speech
vertigo - Lithium
-
oldest
low thereputic index
Acute 0.7-1.2
Maint 0.6-1.0
laseline labs
Na balance is important
Multiple effects on NT
similar to cation
may take 10d-2 weeeks to lyse manic attack - Lithium drug interactions
-
NSAIDS
ACEi
diurectics - Meds that precipitate Mania
-
all antidepressants- switch phenomenon
stimulatants
cocaine
amphetamines
methylphenidate
OTC drugs
pseudephedrine
phenylpropanolamide
caffeine
corticosteroids
thyroid
androgens - Valproate (Depakote)
-
BPD
safer than Lithium
1st line agent
LFTs tested
Loading dose for acute pts
check blood concentration after 4 days
when using antidepressants tx for a shorter time - Lamictal (Lamotrigine)
-
maint of BPD I
can be initial or primary therapy
or adjuvant to valproate - Tegretol (Carbamezepine)
-
BPD
Inc toxic to blood cells - Topramax (Topiramate)
-
BPD
wt loss - Antipsychotics
-
Olanzapine (Zyprexa)
1st line agent to tx acute BPD and maint
should be used for least amount of time - Implanon
-
implant
etonogestrel
effective x 3yrs
inhibits ovulation - Nuva Ring
- EE
- Mirena
-
IUD
levonorestrel
effective x5yrs
high efficacy - OrthoEvra
-
Pathc
norelgestromin (NGMN)
plus EE - Estrogens
-
EE
Mestranol - How estrogens work
-
endometrial proliferation
effects on ovulation (FSH/)
cycle control - Estrogen considerations
-
dose is the primary concern
20-50mcg
fixed doses
incrimental estrogen doses
most of the formulations have 35mcg or less
rx the least ptoent formulation - Estrogen SE
-
Nausea
Breast Tenderness
h/a
thromboembolic effect - Progestins
-
Estranes
Gonanes - Estranes
-
norethindrone
norethindrone acetate - Gonane
-
Levonorestrel
norgestrel - How progestins work
-
prevents ovulation (LH)
thickens cervial mucus
endometrial transformation
cycle control - Progestin considerations
-
1st generations- noresthindrone
2nd gen- levonorgestrel
3rd gen- desogestrel and norgestimate - Progestin SE
-
oily skin- acne may worsen or get better
h/a
breast tenderness
mood changes
wt gain
BTB
hirsuitism - Hormaonal considerations
-
mood changes
wt gain
dec libido
h/a
androgenic SE - BCP interaction with Antibiotics
-
PCN, tet, griseo
use backup protection - BCP interaction with Acitretin (soratane)
- use alternative or additional method
- BCP interaction with Anticonvulsants (phenytoin, carbanezepine, phenobarb, primidone)
- use alt method or use 2nd method
- BCP interaction with Ascorbic Acid
-
Vit C
Avoid high doses of Vit C
use dec doses of estrogen - BCP interaction with Rifamycin
- use nonhormonal contraception during therapy and for 1 cycle after tx ends or inc estrogen
- BCP interaction with Antivirals protease inhibitors
-
inc estrogen
use 2nd method
use alt method - BCP interaction with benzos
- may need to dec benzo dose if CNS sx occur
- BCP interaction with hypoglycemics
-
pioglitazone (Actos)
rosiglitazone (Avandia)
use alt methods
use second method - COC as ECP uses
-
1st dose less than 72 hrs
2nd dose 12 hrs after 1st
repeat dose if vomitting within 3 hours
meclizine/diphenhydramine may be admin to dec N/V
no period in 2-3 weeks--> preg test - CI for COC as ECP
-
thromboembolism
DVT
CV dz or CAD
estrogen dependant neoplasm - COC is a category???
- X-
- Progestin Pill ONLY
-
levonorestrel
Ovrette
Micronor
750 mcg within 72 hrs of unprotected sex
repeat 12hrs later
Failure rate <24hrs- 0.4%
24-72hrs- 2.7%
N/V in 6% of users - Danazol
-
sythetic androgen
2 regimines- 2-400 or 2-400 12 hrs apart - Danazol Considerations
-
women with Ci to estrogen
women who can't tolerate SE of COC
TERATOGEN--> MUST ABORT - Post Coital IUD Insertion
-
Failure rate 0.1%
must be inserted by professional
Cu T380A - Cu T380A MOA
-
sperm: immobilizes, interferes with migration
Ovum: inc speed of transport
Uterus: mechanical distention of endometrium - Cu T380A CI
-
women at risk for STDs
Women allergic to Cu - Problems with Cu T380A
-
insertion cna be difficult
bacteremia--> 13% abx prophylaxis - Benefits of Cu T380A
-
women withCI to hormones
left in place x 10yrs
insertion up to 5 days poist coital - High dose estrogen Administration
-
"standard method"- 60s and 70s
increase SE but equal in effectiveness as Yuzpe
bid x 5 days - Regimines of High dose estrogen
-
2.5 EE
10 esterified or conjugated estrogens
5mg estrone
25 DES - Problems with High dose estrogen
-
Estrogen CI
regimine is more complex
SE
no benefit of this over regular COC - Mifepristone
-
EC
potent anti-progesterone
pregnancy wasting
"abortion pill"
inc incidence of menstrual irregularities - Candidates for OCP
-
menstrual hx
contraceptive hx
PE exam
premenopausal women
risk for thromboembolism is increased after 35 in women who are obese and smoke
over 40- better complicance - CI for OCP
-
pregnancy
malignancy
thromboembolism
major surgery with expected prolonged immobilization
smoker >35yo
heavy smokers of any age
CAD
uncontrolled HTN
undx vag bleeding - Causes of BTB
-
missed pills
smoking
infection
formulation adjustment needed
drug interactions- mechanism CYP3A4 induction with intestinal flora - Progestin only over 40
-
lower efficacy
lower fertility
do not alleviate menopausal sx - Risks of OCP
-
N/V
abd cramping
h./a
migraines
BTB
bloating
breast tenderness
emotional lability
acne rash
edema
thromboembolism
MI
storke
sever HTN
cholestatic jaundice
depression
hepatic adenoma
breast CA - Benefits of OCP
-
improves dysfxnal uterine bleeding
LT benefits
protection against gyn Ca
protection against colorectal Ca
dec risk of RA
dec PID related hospitalizations
improvements in acne
preservation in bone mass
cycle regulation - EC effectiveness
- effectiveness is 75%
- Factors effecting efficacy of EC
-
age
underlying dz state
exposure to drug/toxins
preious rad or surgery
dec body fat - EC Options
-
ECP
Progestin Only pills
Danazol
Postcoital IUD insertion
high dose estrogen administration
Mifepristone (RU 486)
Early Identification and Abortion - Preven
-
EC Kit approved by the FDA
YUZPE method
estrogen (EE) plus progestin (norgestrel)
1st dose within 72 hrs of unprotected sex and then 2nd dose 12 hours later - COC as ECP
-
inhibit ovulation
Estrogens:
accelerate ovum transport
degenerates CL
change in secretions within the uterus
Progestins:
thick cervial mucus
inhibit capacitation
inhibit implantation
slow ovum transport - Drug induced Parkinsons
-
Antipsychotics
Metoclopramide (Reglan) - DOPA decarboxylase Inhibitors
-
Carbidopa (Lodosyn)
Carb + Levo= Sinemet
provides smoother, faster titration of levodopa
dec SE of peripheral metabolism of Levodopa - Nonpharm tx for Parkinsons
-
Exercise
PT
OT
Hollistic
Palliative
Surgical
Individualized - Goal for Pharm therapy of Parkinsons
-
inc availability of dopamine inthe brain
maintain existing levels of dopamine by preventing metabolism of DOPA
inhibit the effects of increased Ach - Levodopa (Dopa, Larodopa)
-
precurser to dopamine
crosses BBB
converted in basal ganglia
rapid absorption
w/d: taper to avoid neuroleptic malignant syndrome - Levodopa/Carbidopa
-
Sinemet
immediate release- food decreases absorption
controlled release- food increases absorption - Levodopa/Carbidopa dosing
- individulaized dosing
- Levodopa/Carbidopa SE
-
orthostatic hypotn
dizziness
urinediscoloration - MAO-B Inhibitors
-
Selegiline(Eldepryl)
mild sx relief of PD
may delay the need for Levodopa by 9mo-1yr
use with Levo in advanced dz - Nonergotamine Dopamine Agonist
-
Pramipexole (mirapex)
Ropinirole (requip)
bind D3>D2 and 4
Does not bind D1 and 5
onset is in weeks
used in early PD
used in late PD with Levodopa to manage motor fluctuations - Nonergotamine Dopamine Agonist SE
- generalized edema
- Amantadine (symmetrel)
-
antiviral agent
may inc dopa release
block dopa reuptake
stimulate dopa receptors - Amantadine (symmetrel) uses
-
bradykinesia
rigidity
tremor
short term monotherapy early in dz - Amantadine (symmetrel) SE
- livedo reticularis
- Ergotamine Dopamine Agonist
-
Bromocriptine (Parlodel)
Perglide (Permax)
used in early PD to avoid high doses of Levadopa
used in advanced PD with Levodopa to managemotor fluctuation
WEEKS for onset - Ergotamine Dopamine Agonist SE
-
dyskinesia
retroperitoneal fibrosis
cardiac fibrosisi
valvulopathy - Injectable Dopamine agonist
-
Apomorphine (Apokyn)
for acute intermittent tx of mypomobility
"off" episodes ass with advanced parkinsons - Injectable Dopamine Agonist SE
- N/V
- Catechol-O-methyltransferase inhibitors (COMT inh)
-
Tolcapone (Tasmar)
Entacapone (Comtar)
adjuvant therapy to leva/carb
significantly increased "on" time and dec "off" time when used with levopdopa
Carb/.Lev/Entacapone (Stlevo)- indicated for wearing off - COMT inh SE
- urinary discoloration
- Anticholinergics
-
Benztropine (Congentin)
Trihexyphenidyl(Artane)
Diphenhydramine (Benadryl)
used to control tremor caused y excessive unopposed Ach in neostriatum
less effective for bradykinesia and rigidity than other agents - Anticholinergics SE:
- Anticholinergic
- Dopamine Agonists
- Must be slowly titrated
- Dopamine Agonists SE
-
orthostasis
dizziness
somnolence
hallucinations
dyskinesias
h/a
confusion - COMT inhibitors beware of...
-
Liver toxicity
esp with tolcapone - Specific Drugs indicated for AD Pharmacotherapy
-
Tacrine HCl (Cognex)
Donepezil HCl (Aricept)
Rivastigmine tartrate (Exelon)
Glantamine NBr (Reminyl)
Memantine HCl (Namenda ) - Antipsychotics to use cautiously in older pts
-
Clozapine
Haldol
Olanzapine
Risperidone