Escolar Documentos
Profissional Documentos
Cultura Documentos
GPCR
Ach
nAchR
mAchR
GABA
GABAA
GABAB
Glutamate
NMDA
Metabotropic
Serotonin
5HT3
5HT1, 5HT2
Cannabinoids
TRPV1/TRPA1
CB1, CB2
What receptor do
barbiturates act
on? What type of
effect do they
have?
Barbs
PHENOBARBITAL,
PENTOBARBITAL, THIOPENTAL
Acts GABAA ligand gated chloride channel
latency
Respiratory
Benzos
Long-acting: DIAZEPAM,
CHLORDIAZEPOXIDE, CLONAZEPAM
Medium-acting: LORAZEPAM
Short-acting: OXAZEPAM,
ALPRAZOLAM, MIDAZOLAM
GABAA receptor
Lorazepam
(ATIVAN)
You would also load them
with phenytoin
Midazolam
Non-benzo benzo
BZ1 receptors
Short half-life
For insomnia, rapid onset, less potential for
tolerance and addiction, less withdrawal
ETHOSUXIMIDE
acid)
Blocks T-type Ca channels
Absence seizures: 3 Hz spike and wave
Risk of Stevens-Johnson
PHENYTOIN
Inhibit sodium channels
Adverse effects
Gingival hyperplasia
Hirsutism
LAD
Folate deficiency (interferes with
metabolism)
Hyperglycemia
Fetal hyantoin syndrome
rash
Weight
VALPROIC ACID
gain
HA
GI
upset
Hair loss
Hepatotoxicity (elevated LFTs)
Pancreatitis
Thrombocytopenia
Neural tube defects
diabetes
insipidus
Hypothyroidism
loss
EBSTEINS HEART ANOMALY
Li
WHICH CLASS?
Fluoxetine
Paroxetine
Sertraline
Citalopram
SSRIs
First
Hydrocephalus, intracranial
calcifications, chorioretinitis
Classic
Trigeminal
neuralgia
Carbamazepine
Non-depolarizing
Tubocurarine, pancuronium
Compete with Ach for postjunctional receptors (just
blocking endogenous agonist) > competitive anatonist
Large margin of safety because 75% Rs must be
blocked before inhibition
Not metabolized by cholinesterases
Readily antagonized and reversed by
anticholinesterase agents (neostigmine,
physostigmine, edrophonium)
Give atropine before (mAchR inhibitor) because
increased Ach would give PS sxs (salivation,
lacrimation, defection, emesis)
Depolarizing agents
Decamethonium,
succinylcholine
NAchR agonists that initially depolarize
muscle but prevent repolarization
Anticholinesterases of no benefit in
reversing (may even prolong it)
Side effects of
succinylcholine?
Increased
intraocular pressure
Muscle soreness
Hyperkalemia (possible arrhythmias)
Contraindicated in burn injury, massive
trauma, severe infection
Dissociative anesthesia
Conscious
PCP derivative
Increase
BP & HR
Definition of MAC?
Partial
Inversely
agent
Hyperthermia
Hypothermia
Chronic etOH
Acute etOH
Redheads
Age
Pregnancy
Sepsis
Alpha2 agonists (clonidine)
Opioids, benzos, barbs,
propofol, local anesthetics,
N2O
Risk of priapism?
TRAZODONE
(trazabone)
Blocks 5HT2a; 5HT1a partial agonist;
blocks 5HT reuptake
Sevoflurane
Nitrous
oxide
B12 dependent
Neuropathy
Muscle weakness
Ataxia
Megaloblastic anemia
Others:
Why is carbidopa
administered with L-dopa?
Carbidopa reduces peripheral metabolism
of L-dopa and improves brain delivery
Another note: vit B6 supplementation
should not be taken with levodopa
because increases peripheral metabolism
and decreases effectiveness
ACID
Because ethosuximide is only going to
be effective against absence
Remember that VPA is a 2nd line for
absence!
inhibitor
Prevents de-amination of dopamine
(prevents breakdown)
MAO-B preferentially metabolizes DA
over NE/5HT
WHICH CLASS?
Amitriptyline
Imipramine
Desipramine
TCAs
acid
WHICH CLASS?
Phenelzine
Tranylcypromine
Selegeline
MAO
inhibitor
NE/5HT accumulate in presynaptic
stores
crisis
Indirect pressor amine tyramine (found
in beer/cheese/wine/etc) can precipitate
severe HTN with used with MAO-I
syndrome
TCAs + SSRIs + dextromethorphan +
meperidine [IN COMBO WITH ] MAO-I
Akathisia
Movement
disorder characterized by
inner restlessness and inability to
sit/stand
Sometimes it is missed because the
movement/restlessness if
misinterpreted as worsening psychotic
behaviorthen a doc increases the dose
and exacerbates symptoms
Treat with BB
dyskinesia
Often irreversible
Other effects
EPS
(nigrostriatal pathway)
Dystonia
Parkinsonism
Akathesia
TD
Endocrine
Galactorrhea
Gynecomastia
Sexual dysfunction
NMS
Retinitis pigmentosa
Thioridazine
Corneal deposits
Chlorpromazine
HIGH
POTENCY
Haloperidol
Fluphenazine
Trifluoperazine
LOW
Chlorpromazine
Thioridazine
Atypical antipsychotics
MAJOR
RISK WITH
CLOZAPINE?
Agranulocytosis
malignant syndrome
Dopamine
agonist (bromocriptine)
and/or direct muscle relaxants
(dantrolene) have been used to
decrease mortality rates
Hyperthermia, extreme generalized
rigidity, autonomic instability, altered
mental status, myoglobinuria
of local anesthetic
necessary for nerve block increases as
pH decreases
Inflammation
produces DECREASED pH
and therefore decreases effectiveness of
local anesthetics
toxicity first
Cardiovascular
and sulfadiazine