Neuropharmacology Drug Cards

pregnancy category A

no problems for fetus

pregnancy category B

humans = no good studies

animals = no effect on babies

OR

animals = some babies affected

humans = NO babies affected

pregnancy category C

humans = no good studies

animal = some babies have problems

BUT... benefits outweigh risk

NO animal studies and NO good studies in preggo women

pregnancy category D

babies born with birth defects

still some benefits outweigh risk

pregnancy category X

absolutely not... benefits will never outweigh risks

Levodopa (Sinemet) classification

dopamine replacement

Levodopa (Sinemet) MOA

levodopa converted to dopamine, which then activates dopamine receptors

Levodopa (Sinemet) DOC

given to reduce movement disorders

first line drug

always combined w/ carbidopa, may also supplement to a dopamine agonist

Levodopa (Sinemet) dose/ route

PO, only given with carbidopa and entacapone

Levodopa (Sinemet) A/E

dose dependent (bad drug test, trippin, OD on dope)

dyskinesias

dark urine/ sweat (normal)

insomnia

nightmares

dysrhythmias

psychosis

early tx: n/v

postural hypotension

Levodopa (Sinemet) drug interactions

carbidopa and entacapone inc effects

1st gen antipsychotics decrease effects

MAO-inhibitors (inc toxicity, rx for HTN crisis)

Levodopa (Sinemet) contraindications

giving without carbidopa

use caution in renal failure

avoid in narrow-angle glaucoma

Levodopa (Sinemet) pt counseling

avoid high protein meals

eat consistent amount of protein throughout the day

may "wear off" between doses

noticeable difference may take weeks

give with food

Levodopa (Sinemet) NI

dyskinesias

other A/E

treatment may seem effective initially, but not as effective as disease progresses

Carbidopa (Sinemet) classification

dopamine agonist

Carbidopa (Sinemet) MOA

inhibits decarboxylation of levadopa in intestines/ peripheral tissues

Carbidopa (Sinemet) dose/ route

give without food

-can interfere with absorption

Carbidopa (Sinemet) DOC

combined with levodopa to increase therapeutic effects so that lower doses of levodopa can be used

Carbidopa (Sinemet) A/E

none

a/e are better absorption of levodopa

Carbidopa (Sinemet) drug interactions

inc beneficial effects of levodopa

Carbidopa (Sinemet) pt edu

avoid high protein meals (consistent amount of protein throughout the day)

may "wear off" between doses

may cause hallucinations

check CV assessment

Carbidopa (Sinemet) contraindications

should be given w levodopa

Carbidopa (Sinemet) NI

dyskinesias

other a/e

treatment may seem effective intially but not as effective as disease progresses

Pramipexole (Miraprex) classification

nonergot dopamine receptor agonsit

Pramipexole (Miraprex) MOA

selectively binds to dopamine receptor D2 and D3 receptors activating dopamine receptors midley blocks serotonergic and alpha-adrenergic receptors

Pramipexole (Miraprex) DOC

in monotherapy -> produces significant motor performance improvement

used for RLS

w levodopa, reduces motor control fluctuations

may reduce levodopa doses

Pramipexole (Miraprex) A/E

n/ c

dizziness

daytime somnolence

insomnia

weakness

hallucinations

sleep attacks

impulse control disorders

when combined with levodopa (hallucinations, daytime sleepiness, postural hypotension)

Pramipexole (Miraprex) drug interactions

cimetidine

Pramipexole (Miraprex) contraindications

compulsive behaviors

reduce dosage with significant renal impairment

Pramipexole (Miraprex) pt edu

may take several weeks to see maximum benefits

Pramipexole (Miraprex) NI

screen for compulsive behaviors prior to prescribing

assess renal fx (BUN/Cr)

Entacapone (Comtan) classification

catechol-O-methyltransferase (COMT) inhibitor

Entacapone (Comtan) MOA

selectively inhibits enzyme COMT, resulting decreased metabolism of levodopa in intestines and peripheral tissues`

Entacapone (Comtan) DOC

prolongs half life of levodopa/ carbidopa

to help w weaning off process

Entacapone (Comtan) A/E

n/v/d/c

yellow-orange discolored urine

increased levodopa levels may lead to dyskinesias

orthostatic hypotension

hallucinations

sleep disturbances

impulse control disorders

Entacapone (Comtan) drug interactions

potentially increases drug levels of other drugs metabolized by COMT (methyldopa, dobutamine, isoproterenol)

Entacapone (Comtan) contraindications

give in combination with levodopa

Entacapone (Comtan) pt edu

a/e

importance of taking with levodopa carbidopa

Entacapone (Comtan) NI

for a/e to determine if levodopa should be adjusted

Selegiline (Eldepryl, Zelapar) classification

monoamine oxidase-B (MAO-B) inhibitor

Selegiline (Eldepryl, Zelapar) MOA

selectively and irreversibly inhibits MAO-B which is an enzyme that inactivates dopamine

Selegiline (Eldepryl, Zelapar) DOC

improves motor function

may delay neurodegeneration

can prolong effects of levodopa

using in new diagnosis

Selegiline (Eldepryl, Zelapar) dose/ route

orally disintegrating tablets (ODT) - avoid taking liquids

-take b4 breakfast and wait 5 min before drinking/ eating

Selegiline (Eldepryl, Zelapar) A/E

insomnia

orthostatic hypotension

dizziness

GI symptoms

hypertensive crisis buccal mucosa irritatioin if taking ODT

Selegiline (Eldepryl, Zelapar) drug interactions

tyramine

sympathomimetics

intensifies a/e of levodopa

meperidine

SSRI's

Selegiline (Eldepryl, Zelapar) contraindications

meperidine

SSRI's

Selegiline (Eldepryl, Zelapar) Pt edu

benefits may decline after 12-24 months

administer last dose before noon to avoid insomnia

avoid foods containing tyramine and sympathomimetics

avoid liquids with ODT

Selegiline (Eldepryl, Zelapar) NI

BP

effectiveness of drug

Donepezil (Aricept) Classification

cholinesterase inhibitor

Donepezil (Aricept) MOA

inhibits breakdown of acetylcholine by acetylcholinesterase, inc acetylcholine available at cholinergic synapses

Donepezil (Aricept) DOC

for mild, moderate, and severe AD

Donepezil (Aricept) AE

most common:

-HA

-dizziness

-vertigo

-insomnia

-n/v/d

most serious:

-bronchoconstriction

-bradycardia

-sinus sick syndrome

Donepezil (Aricept) drug interactions

first generation anti-histamines

tricyclic antidepressants

conventional antipsychotics

Donepezil (Aricept) contraindications

use caution w

-asthma

-copd

-liver and heart dx

-avoid administering with other agents that block cholinergic receptors

Donepezil (Aricept) pt edu

will not cure AD, can briefly slow progression

rx of a/e inc w high doses

take with food

Donepezil (Aricept) NI

monitor for effectiveness

ex benefits 1 in 12

bronchoconstriction

hr

titrate carefully, go slow and low

1-3 mo initial dose, don't change

Memantine (Namenda) classification

NMDA receptor antagonist

Memantine (Namenda) MOA

regulates ca uptake into cells

preventing toxic levels of ca from blocking memory formation

Memantine (Namenda) DOC

moderate to severe AD

better tolerated than cholinesterase inhibitors

Memantine (Namenda) a/e

dizziness

ha

confusion

constipation

diarrhea

htn

hypotension

Memantine (Namenda) drug interactions

other NMDA antagonists (amantadine, ketamine)

sodium bicarbonate

Memantine (Namenda) contraindications

use caution with drugs that alkalinize urine

use caution with renal/ hepatic impairment

Memantine (Namenda) pt edu

may see improvement in s/sx

Memantine (Namenda) NI

BUN, Cr

Phenytoin (Dilantin) classification

traditional AED

Phenytoin (Dilantin) MOA

blocking sodium entry into neurons decreases activity of neurons that produce seizures

Phenytoin (Dilantin) DOC

partial seziures

generalized tonic-clonic seizures

can be used for dysrhythmias

Phenytoin (Dilantin) a/e

nystagmus

sedation

ataxia

diplopia

cognitive impairment

gingival hyperplasia

measles like rash

bleeding tendencies in nb

dysrhythmias and hypotension with IV

Phenytoin (Dilantin) drug interactions

oral contraceptives

warfarin

glucocorticoids

diazepam

isoniazoid

cimetidine

alcohol

valproic acid

carbamazepine

phenobarbital

barbituates

CNS depressants

Phenytoin (Dilantin) contraindications

pregnancy category rx D

HLA-B* 1502 genetic mutation

Phenytoin (Dilantin) pt edu

good oral hygiene

take 0.5 mg folic acid daily

birth control

avoid alc and other CNS depressing drugs

Phenytoin (Dilantin) NI

screen for suicide rx

LFT's

a/e may indicate excessive drug levels (should be 10-20 mcg/ mL)

Carbamazepine (Tegretol) classification

traditional aed

Carbamazepine (Tegretol) MOA

suppresses high-frequency neuronal discharge in and around seizure focus

Carbamazepine (Tegretol) DOC

partial and tonic-clonic seizures

symptomatic control for bipolar disorders

trigeminal and glossopharyngeal neuralgias

Carbamazepine (Tegretol) a/e

nystagmus

blurred vision

diplopooa

ataqxia

vertigo

unsteadiness

ha

bone marrow suppression

leukopenia

anemia

thrombocytopenia

hypo-osmolarity

measles like rash

SJS

Carbamazepine (Tegretol) drug interactions

oral contraceptives

warfarin

phenytoin

phenobarbitual

grapefruit juice

Carbamazepine (Tegretol) contraindications

preexisiting hematologic abnormalities

preg cat rx d

screen pts of asian descent for HLA-B* 1502

Carbamazepine (Tegretol) pt counseling

tolerance to drug will inc a/e after a feew weeks

take largest dose at bedtime

avoid grapefruit juice take with meals

screen for suicide rx

LFT's

CBC

BMP

Valproic acid (Depakote) classification

traditional aed

Valproic acid (Depakote) MOA

suppresses high-frequency neurons targeting sodium channels

prevents ca from entering ca channels

may enhance inhibitory influence of GABA

Valproic acid (Depakote) DOC

seizure disorders

bipolar disorders

migraine ha

Valproic acid (Depakote) a/e

n/v

indigestion

hepatoxicity

pancreatitis

hypermmonemia

rash

weight gain

hair loss

tremor

blood dyscrasia

generally well tolerated

Valproic acid (Depakote) drug interactions

phenobarbital

phenytoin

topiramate

carbapenem abx

avoid administration with meropenem and imipenem/cliastatin

Valproic acid (Depakote) contraindications

preg cat d

avoid in combination w other drugs in children under 2

preexisiting liver dysfunction

Valproic acid (Depakote) pt edu

take with food

s/sx of liver failure and pancreatitis

BC

women of childbearing age should take folic acid

do not crush or chew tablets/ capsules

Valproic acid (Depakote) NI

screen for suicide rx

LFT's

lipase

amylase

therapeutic effects

switch iv to po as quickly as possible

Phenobarbital classification

anticonvulsant barbiturate

Phenobarbital MOA

binds to GABA receptors, leading to receptors to respond to GABA more

Phenobarbital uses

partial and general tonic-clonic seizures

IV form can be used to treat generalized convulsive status epilepticus

sedation

sleep aid

Phenobarbital a/e

lethargy

depression

learning impairment

paradoxical response in children

agitation and confusion in elderly

dependence

acute intermittent porphyria

bleeding tendencies in nb

rickets

osteomalacia

nystagmus respiratory depression leading to death

Phenobarbital drug interactions

oral contraceptives

warfarin

other CNS depressants including alcohol

valproic acid

Phenobarbital contraindications

hx of intermittent porphyria

suicidal tendencies

pregnancy category rx d

Phenobarbital pt counseling

doses used for seizures are not usually high enough to result in addiction

as tolerance buuilds up drowsiness will decrease, limit or avoid alcohol

do not discontinue abruptly

may take weeks to reach therapeutic levels

Phenobarbital NI

screen for suicide rx

monitor for nnystagmus and ataxia

CNS depression

plasma drug levels

15-40 mcg/ mL

LFT's

BUN

Cr

Gabapentin (Neurotin) classification

newer aed

Gabapentin (Neurotin) MOA

may enhance GABA release

precise MOA unknown

Gabapentin (Neurotin) DOC

fda approved

adjunctive therapy in partial seizures

post herpetic neuralgia

off label uses:

-monotherapy of partial seizures

-neuropathic pain

-migraine prophylaxis

-fibromyalgia

-postmentopausal hot flashes

Gabapentin (Neurotin) a/e

somnolence

dizziness

ataxia

fatigue

nystagmus

peripheral edema

Gabapentin (Neurotin) drug interactions

no significant drug interactions