Therapeutics 5 top 300 drugs: WEEK 6

Levetiracetam brand names

Keppra, Keppra XR, Roweepra, Spritam

Levetiracetam Class

Anticonvulsant

Levetiractam Indication + Dosing

Myoclonic Seizure adjunct: (initial) 500 mg bid, titrate to targe 3000 mg/d

Partial Seizure adjunct: IR— (initial) 500 mg bid max 3000 mg/d ER— (initial) 1000 mg/d max 3000 mg/d

Tonic-Clonic seizure, primary generalized, adjunct: (initial) 500 mg bid titrate to 3000 mg/d

Levetiracetam MOA

Pyrrolidine derivatitve

MOA is unclear not related to any known mechs

unique action from other AEDs

Levetiracetam BBW

none

Levetiracetam contraindications

hypersensitivity

Levetiracetam Common AEs

Asthenia

Abnormal behaviors

Fatigue

HA

Somnolence

Vomiting

Increased BP

Levetiracetam Rare AEs

Pancytopenia

Hepatotoxicity

Suicidal thoughts

Suicide

SJS

Levetiracetam counseling

swallow ER tabs whole; do not break/chew

avoid mental alertness activities until effects are realized

report mood swings, agitation, hostile behavior…

avoid sudden discontinuation of drug: increases seizure activity

Divalproex brand

Depakote

Divalproex Class

Anticonvulsant

Divalproex Indication + Dosing

Absence seizure simple and complex: 15 mg/kg/d titrate to 50 mg/kg/d

Complex partial epileptic seizure: 10-15 mg/kg/d titrate to 60 mg/kg/d

Manic bipolar disorder: 25 mg/kg/d titrate to 60 mg/kg/d

Migraine prophyl: ER—500 mg/d up to 250 mg/d, DR—250 mg bid up to 250 mg/d every 3 days to 500 mg bid

Divalproex MOA

Sodium valproate and valproic acid. Divalproex dissociates to valproate in stomach.

This increases GABA levels by inhibiting GABA metabolism or enhancing postsynaptic GABA activity.

Limits repetitive neuronal firing through voltage and usage Na+ channels.

Divalproex BBW

Hepatotox.

Mitochondrial disease

Teratogenicity

Pancreatitis

Divalproex contraindications

hypersensitivity

hepatic disease

urea cycle disorders

Divalproex common AEs

Abdominal pain

alopecia

asthenia

diarrhea

diplopia

dizziness

HA

infection

insomnia

nausea

somnolence

tremor

vomiting

Divalproex rare AEs

Hepatitis

palpitation

pancreatitis

tachycardia

thrombocytopenia

suicidal ideation or behavior

Divalproex counselling

avoid mental alertness activities

seek medical help for signs of liver dysfunction

take with food minimize GI

do not discontinue drug abruptly may precipitate seizures

avoid alcohol

sprinkle capsules

hazardous USP 800

Carbamazepine brands

Tegretol

Carbatrol

Carbamazepine class

anticonvulsant

carbamazepine indication + dosing

Focal-onset and generalized-onset seizures: 200 mg bid up to 1200 mg/d

neuropathic pain: 100-200 mg q12h

bipolar disease acute treatment of mania, hypomania, mixed eps: 100-400 mg in 2-4 divided doses up to 200 mg/d

Carbamazepine MOA

presynaptic: blocks firing of action potentials

postsynaptic: blocks high-frequency repetitive discharge at cell bodies.

Carbamazepine BBW

Agranulocytosis

aplastic anemia

dermatological reactions (asians)

screen for HLA-B 15:02

Carbamazepine contraindications

hypersensitivity

history of BM depression

MAOIs

nefazodone

Carbamazepine common AEs

Ataxia

drowsiness

dizziness

nausea

Carbamazepine rare AEs

cardiac dysrhythmia

hepatitis

nephrotoxicity

pancreatitis

pancytopenia

SJS

syncope

toxic epidermal necrolysis

suicidal thoughts

Carbamazepine counseling

may decrease oral contraceptive efficacy

avoid mental alertness activities

take with food

no alcohol, grapefruit

avoid abrupt discontinuation

Lacosamide brand

Vimpat

Motpoly XR

Lacosamide Class

anticonvulsant miscellaneous C5

Lacosamide indications + dosing

partial onset seizure: IR—100 mg bid, ER—200 mg/d

primary tonic-clonic seizure: IR—50 mg bid, ER—100 mg/d

Benztropine brand

Cogentin

benztropine class

antiparkinsonian anticholinergic

benztropine indication + dosing

EPS med-induced movement disorder: 1-2 mg/d titrate by 0.5 mg at 3 day intervals

parkinsonism: 1mg/d in divided doses titrate by 0.5 mg at 5 day intervals to 4 mg/d

Benztropine MOA

anticholinergic and antihistamine

may inhibit reuptake and storage of dopamine

Benztropine BBW

none

Benztropine Contraindications

hypersensitivity

use in patients < 3 years old

Benztropine common AEs

constipation

nausea

Benztropine rare AEs

anhidrosis

drug induced psychosis

eat stroke

increased body temp

tachycardia

visual hallucinations

Benztropine counselling

may impair heat regulation, use with caution in rigorous activities

avoid mental alertness

report any sudden muscle weaknesses

do not drink alcohol

Oxcarbazepine brand

Trileptal

Oxtellar XR

Oxcarbazepine class

Dibenzazepine caboxamide, anticonvulsant

Oxcarbazepine indication + dosing

Focal onset seizures: 300 mg BID, titrate to 1200-2400 mg/d

Oxcarbazepine MOA

analogue of carbamazepine, not known mech, involves blockage of sodium channels inhibiting repetitive neuronal firing

Oxcarbazepine BBW

none

Oxcarbazepine contraindications

hypersensitivity

Oxcarbazepine common AEs

Somnolence

abdominal pain

HA

diplopia

dizziness

Oxcarbazepine rare AEs

Anaphylaxia

angioedema

SJS

suicidal thoughts

pancytopenia

Oxcarbazepine counselling

suspension should be shaken well and dose prepped right away.

avoid mental alertness

report signs/symptoms of dermatologic rxns

take with food

avoid alcohol and grapefruit juice

avoid abrupt discontinuation

Phenytoin brand

dilantin

Phenytek

Phenytoin class

Hydantoin anticonvulsant

Phenytoin indication + dosing

Seizure, generalized: 100 mg tid up to 200 mg tid

Phenytoin MOA

Hydantoin suppresses spread of seizure activity by inhibiting synaptic post-tetanic potentiation and blocking propagation of electric discharge (may decrease sodium channels, or block calcium channels)

Phenytoin BBW

hypotension and arrhythmias with IV administration

Phenytoin contraindications

hypersensitivity

sinus bradycardia

AV block

concurrent delavirdine

history of phenytoin-related hepatotoxicity

Phenytoin common AEs

gingival hyperplasia

Phenytoin rare AEs

Hepatotoxicity

pancytopenia

systemic lupus

SJS

suicide behavior

withdrawal seizures

Phenytoin counselling

shake suspension

do not crush ER capsules

avoid mentla alertness activities

report signs of pancytopenia, hepatotoxicity, systemic lupus

do not drink alcohol

check with HCP

Phenobarbital brand

Luminal

Sezaby

Phenobarbital class

long acting barbiturate C 4

Phenobarbital indication + dosing

seizures: 50-100 mg bid-tid

sedation: 30-120 mg in 2-3 doses

Phenobarbital MOA

Produces different degrees of depression in CNS. works on decreasing postsynaptic resistance.

Phenobarbital BBW

Concomitant use with opioids

dependence and withdrawal

abuse (IV only)

Phenobarbital contraindications

hypersensitivity

liver function impairment

respiratory disease with dyspnea or obstruction

history of sedative of hypnotic addiction

personal/ family history of acute intermittent porphyria

Phenobarbital common AEs

hypotension

appetite changes

hypoventilation

Phenobarbital rare AEs

barbiturate withdrawal

bradyarrhythmias

megaloblastic anemia

respiratory depression

SJS

Phenobarbital counselling points

avoid mental alertness activities

advise against sudden discontinuation

do not drink alcohol

many drug interactions

Memantine brand

Namenda

Memantine class

NMDA antagonist

Memantine indication + dosing

Alzheimer disease: IR—5 mg daily ER—7 mg daily

Memantine MOA

binds to NMDA instead of glutamate causing less symptoms associated with AD

Memantine BBW

none

Memantine contraindications

hyeprsensitivity

Memantine common AEs

none

Memantine rare AEs

SJS

DVT

liver failure

hepatitis

cerebrovascular accident

grand mal seizures

transient ischemic attack

acute renal failure

Memantine counselling

may be taken with or without food

oral solution is packaged w/ dosing device used to administer med.