Neuro - FA Pharm p532 - 539 Flashcards
DOC in status epilepticus & MoA
Benzos, !nc GABAA action
MoA of Carbamazepine
Blocks Na+ channels
1st and 2nd line treatment for eclampsia seizures
- MgSO4
- Benzos
DOC for trigeminal neuralgia
Carbamazepine
SE of Carbamazepine
Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis (cleft lip/palate, spina bifida), induction of cytochrome P-450, SIADH, SJS
Tx and MoA of Rx that treats absence seizures
Ethosuximide
Blocks thalamic T-type Ca2+ channels
(-) high voltage activated Ca channels
Gabapentin
SE of Ethosuximide
EFGHIJ—Ethosuximide causes Fatigue, GI distress, Headache, Itching (and urticaria), SJS
Other uses of Gabapentin other than seizures
Also used for peripheral neuropathy, postherpetic neuralgi
What epileptic drug needs to be titrated slowly bc of SJS
Lamotrigine
(Carbamazepine also, and rarely, Phenytoin)
Lamotrigine has a black box warning for what?
causing hemophagocytic lymphohistiocytosis
MoA of Lamotrigine
Blocks voltage gated Na channels - (-) Glu release
Which epileptic drug has personality changes as a SE?
Levetiracetam
He’s on another level
Which epileptic drugs (+) p450?
Phenobarbital
Carbamazepine
Phenytoin
Which 3 drugs are used for status epilepticus
Benzo - 1st line
Phenobarbital
Phenytoin - 1st line for recurrent seizure
1st line for neonatal seizures
phenobarbital
PhenoBabytal
Which epileptic drug has zero order kinetics
Phenytoin
List Ca2+ blockers for antiseizures
EGL
Ethosuximide
Gabapentin
Levetiracetam
Antiepileptic causing SIADH
carbamazepine
tonic-clonic DOC
valproic acid
patient with tonic clonic and absence seizures
valproic
gingival hyperplasia is caused by
phenytoin
Also Cyclosporin, CCB (verapamil)
baby with cleft palate, cardiac
defects, phalanx/fingernail hypoplasia
fetal phenytoin syndrome
kidney stones are caused by
topiramate
Sedation, slow cognition,
kidney stones, skinny (weight
loss), sight threatened
(glaucoma), speech
2 drugs that are used for migraine prophylaxis
Valproic acid
Topiramate
Also: TCAs, and BBs/CCBs (CCB only in VC phase)
What drug group is contraindicated in porphyria?
Barbituates
SE of Phenytoin
PHENYTOIN:
P-450 induction,
Hirsutism,
Enlarged gums,
Nystagmus,
Yellow-brown skin,
Teratogenicity (fetal hydantoin syndrome),
Osteopenia,
Inhibited folate absorption,
Neuropathy.
For which epileptic rx do you need to monitor LFTs
Valproic acid - rare but fatal hepatotox
CI in pregnancy
valproic acid
black box warning with vigabatrin?
permanent vision loss
Vision gone all bad with Vigabatrin
Which two drugs block GABA transaminase?
Valproic acid
Vigabatrin
The Vs block the enzyme
MoA of Barbituates
Facilitate GABAA action by INC duration of Cl− channel opening, thus dec neuron firing (barbidurates INC duration)
Which barb is used to induse anesthesia?
thiopental
MoA of Benzo?
Facilitate GABAA action by INC frequency of Cl– channel opening (“frenzodiazepines” inc frequency).
How does benzo affect sleep?
Dec REM sleep, dec N3 stage of sleep (delta )
Which benzos are short acting? what does that mean for addiction?
Which benzos are safe for those with liver problems
Lorazepam, Oxazepam, and Temazepam can be used for those with liver disease who drink a LOT due to minimal first-pass metabolism.
Which 3 benzos are used in status epilepticus?
lorazepam, diazepam, midazolam
How to tx Benzo OD? MoA? What is the potential post tx issue?
Treat overdose with flumazenil (competitive antagonist at GABA benzodiazepine receptor). Can precipitate seizures by causing acute benzodiazepine withdrawal.
Nonbenzo hypnotics?
Zolpidem, Zaleplon, esZopiclone. “These ZZZs put you to sleep.”
MoA of non benzo hypnotics
Act via the BZ1 subtype of the GABA receptor.
Why do non benzo hypnotics have a short duration of action?
Short duration because of rapid metabolism by liver enzymes
orexin receptor antagonist?
Suvorexant
Orexin - antagonist
CI of Suvorexant
Can’t be used with narcolepsy, combination with strong CYP3A4 inhibitors. Not recommended in patients with liver disease
melatonin receptor agonist?
Ramelteon
Ramelteon binds to which rec’r in what nucleus?
MT1 & MT2
suprachiasmatic nucleus
Triptans have what MoA?
5-HT1B/1D agonists.
Inhibit trigeminal nerve activation,
prevent vasoactive peptide release,
induce vasoconstrition
Triptans are used for what type of headaches
Migraines and cluster headache attacks
Triptans CI in which patients
Peole with CAD/ vasospastic angina, bc causes coronary vasospasm
Which rx should not be mixed with triptans
Any serotonin agonists, bc could lead to serotonin syndrome
Psychiatric drugs: MAO
inhibitors, SSRIs, SNRIs,
TCAs,
vilazodone - (-) 5HT reuptake, 5HT1A partial agonist
vortioxetine - (-) 5HT reuptake, 5HT1A agonist, 5HT3 antagonist
Nonpsychiatric drugs:
tramadol, ondansetron,
triptans, linezolid, MDMA,
dextromethorphan,
meperidine, St. John’s wort
Name 2 Non-ergot (preferred) Tx for Parkinson?
pramipexole (restless leg syn Tx), ropinirole
Which drug incr dopamine release and decr reuptake?
Amantadine
Which agent blocks DOPA decarboxylase?
Carbidopa
Which drugs prevent peripheral l-dopa degradation to 3-O-methyldopa (3‑OMD) by inhibiting COMT?
Entacapone, tolcapone
Drug that blocks conversion of dopamine into 3-MT by selectively inhibiting MAO-B?
Selegiline
2 MOA of Tolcapone
—blocks conversion of dopamine to 3-MT (3 - methoxytyramine) by inhibiting central COMT
—prevent peripheral l-dopa degradation to 3-O-methyldopa (3‑OMD) by inhibiting COMT.
BALSA mneumonic stands for what? It treats what?
Parkinsons
Bromocriptine
Amantadine
Levodopa (with carbidopa)
Selegiline (and COMT inhibitors)
Antimuscarinics
How to curb excess cholinergic activity?
Benztropine, trihexyphenidyl (Antimuscarinic; improves tremor and rigidity but has little effect on bradykinesia in Parkinson disease). Park your Mercedes-Benz.
What enzyme converts L- Dopa to dopamine?
dopa decarboxylase
long termSE of L-Dopa
With progressive disease, l-DOPA can lead to “onoff” phenomenon with improved mobility during “on” periods, then impaired motor function during “off” times when patient responds poorly to l-DOPA or medication wears off.
Name a NMDA receptor antagonist that helps prevent excitotoxicity (mediated by Ca2+)?
Memantine used for Alzheimer
Rx used in ALS ?
Riluzole
Rilouzole - for Lou Gehrig
dec neuron glutamate
Huntington disease Rx and MoA
Tetrabenazine
Inhibit vesicular monoamine transporter (VMAT) –> dec dopamine vesicle packaging and release
Tetra = 4 , Huntington on Chr 4
high potency –> lipid or blood solubility
potency–> think lipid! want high solubility in lipid for high potency
rapid induction, want B/G ratio to be?
low–> increased free fraction
Side effect of Halothane
Hepatotoxicity
Methyoxyflurane SE
nephrotox
Proconvulsant
Enflurane
Pathomech of Malignant hyperthermia
Mutations in voltage-sensitive ryanodine receptor (RYR1 gene) cause Ca2+ release from sarcoplasmic reticulum.
List 4 IV anesthetics
Thiopental, Midazolam, Propofol, Ketamine
How do the IV anesthetics affect GABA
Thiopental - barb - inc duration of Cl’ channel opening - faciliate GABAa
Midazolam - inc freq of Cl channel opening - facilitate GABAa
Propofol - potentiates GABAa
MoA of Ketamine
NMDA -R antagonist
Which IV anesthetic causes anterograde amnesia, and which causes hallucinations
Midazolam ; Ketamine
Why are local anesthetics given with epinephrine
Can be given with vasoconstrictors (usually epinephrine) to enhance local action—dec bleeding, inc anesthesia by dec systemic concentration.
In which conditions may you have to give a larger dose of anesthetic
In infected (acidic) tissue, alkaline anesthetics are charged and cannot penetrate membrane effectively = need more anesthetic
Which local anesthetic leads to cardiovasc tox and which leads to methemoglobinemia?
Cardio tox - Bupivacaine
BuPumpacaine
Methemoglobinemia - Benzocaine
BenZO MetheMO
Succinyl choline - MoA
strong Ach-R agonist
How to reverse blockade of Succinyl choline
Phase I (prolonged depolarization)—no antidote. Block potentiated by cholinesterase inhibitors.
Phase II (repolarized but blocked; ACh receptors are available, but desensitized)—may be reversed with cholinesterase inhibitors
Ex of nondepolarizing neuromuscular blocking drugs - MoA
Atracurium, cisatracurium, pancuronium, rocuronium, tubocurarine, vecuronium - competitive ACh antagonist
How to reverse nondepolarizing neuromuscular blocking drugs?
neostigmine
edrophonium
(cholinesterase blockers)
What must be given with neostigmine to (-) bradycardia
atropine + glycopyrrolate
a GABAB-R agonist in spinal cord
Baclofen
B- for back and GABAB
CNS acting spasmolytic
Cyclobenzaprine, mainly at the brain stem
Dantrolene MoA
(-) release of Ca2+ from SR of skeletal musc by (-)’d ryanodine receptor
Use of Dantrolene
Malignant hyperthermia (toxicity of inhaled anesthetics and succinylcholine) and neuroleptic malignant syndrome (toxicity of antipsychotic drugs)
centrally acting α2 agonist?
Tizanidine
Which channels do opiods affect and how?
close presynaptic Ca2+ channels, open postsynaptic K+ channels
Opoids stop the release of ?
ACh, norepinephrine, 5-HT, glutamate, substance P.
Partial opiod agonist
Buprenorphine
Mixed opiod agonist/antagonist
nalbuphine, pentazocine, butorphanol
Opiod antagonist
naloxone, naltrexone, methylnaltrexone
Opiods used for diarrhea
loperamide, diphenoxylate
Which opiod causes mydriasis instead of miosis
Meperidine
What is the risk with mixing pentazocine or Butorphanol with other opiods?
Can ppt withdrawal if a patient is taking a full agonist too
Tramadol, along with being a weak opiod agonist also acts on what other nt?
also inhibits the reuptake of norepinephrine and serotonin.
List 3 drugs that dec aq humor synthesis
BB
α-agonists
Acetazolamide
2 drugs that inc outflow of aq humor
Prostaglandins - Bimatoprost, latanoprost
Cholinomimetics - pilocarpine, carbachol, physiostigmine, echothiophate
Which two glaucoma drugs cause no vision or pupillary changes
BB
Acetazolamide
Diff between epinephrine and apraclonidine in terms of glaucoma tx
Epinephrine dec aq humor synthesis via VC, Apraclonidine (Brimondine) will dec synthesis directly
Which glaucoma drug should not be used in closed angle glaucoma
Epinephrine - will cause mydriasis
Which glaucoma drug causes miosis and cyclospasm
cholinomimetics (M3R)
Rx for acute angle closure glaucoma?
Pilocarpine (very effective at opening meshwork into canal of Schlemm)
SE of PGF2α
latanoprost, bimatoprost
darkens irises, and eyelash growth
what 2 drugs are used for maintenance programs for heroin addicts?
methadone, buprenorphine + naloxone
What do you use for Spasticity in MS
Baclofen (GABAb agonist)
list Muscarinic antagonist to treat neurogenic bladder
oxybutynin
Tolterodine
treatment for
- malignant hyperthermia
- Neuroepileptic syndrome
- serotonin syndrome
- extrapyramidal systems SE of antipyschotics
- dantrolene (fever+severe muscle contractions) (SSRI+inhaled anesthetics except N2O)
- dantrolene and D2 agonists (bromocriptine) (myoglobinuria + ridigity)
- cyproheptadine - 5hT2-R (-)’r (myoclonus + diarrhea)
- benztropine (anti muscuranic) or diphenhydramine
for endoscopy, what anesthetics are used?
Midazolam