benzodiazepines Flashcards
trade name of midazolam
versed
how is midazolam supplied
5mg/mL
1mg/mL
MOA of midazolam
binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system
limbic system
reticular formation
enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions
this shift in chloride ions results in hyper polarization (less excitable state)
stabilization
uses of midazolam
preoperative sedation
moderate sedation prior to iagnostic or radiographic procedures
ICU sedation
induction and maintenance of general anesthesia
what receptor does midazolam bind to?
GABA
where does midazolam work?
CNS
limbic system
reticular formation
what type of receptor is GABA
inhibitory
what ion is affected by midazolam?
Cl
what does the chloride shift due to midazolam result in?
hyperpolarization
less excitable state
stabilization
dose of midazolam IM
0.07 - 0.08 mg/kg 30-60 minues prior to surgery
what is a typical IM dose of midazolam?
5 mg
IV dose of midazolam
0.01-0.03 mg/kg
q5 minues
to affect
max dose of IV midazolam
0.1-0.2 mg/kg
7 mg-14 mg for a 70 kg pt
how is dosage affected for midazolam if the patient is unpremeditated vs. premedicated
premeditated dose much smaller
pre- 0.05-0.2
non-pre 0.3-0.35 mg/kg
dose of maintenance of midazolam
0.05 mg/kg as needed
continuous infusion of midazolam dose
- 015-0.06 mg/kg/hour
0. 25-1 mcg/kg/minute
who gets oral midazolam
peds
oral, rectal, intranasal
onset of IM midazolam
~15 minutes
onset of IV midazolam
3-5 minutes
onset of of oral midazolam
10-20 minutes
onset of intranasal midazolam
4-8 minutes peds
peak of IM midazolam
0.5-1 hour
duration of IM midazolam
6 hours
mean 2 hours
IV single dose of midazolam duration
less than 2 hours
dose dependent
how long is midazolam’s duration with cirrhosis
6 hours
metabolism of midazolam
extensively hepatic
CYP3A4
how much of midazolam is transformed to its active metabolite
60-70%
what is midazolam’s active metabolite
1-hydrozymidazolam
half life or midazolam
2-6 hours
what conditions prolong midazolam’s half life
cirrhosis CHF obesity renal failure- accumulation of active metabolites = prolonged sedation elderly
excretion of IV midazolam
urine
excretion of oral midazolam
urine 90%
feces 2-10 % over 5 days
adverse reactions with midazolam Pulmonary
: Decreased tidal volumes and/or respiratory rate decrease
Apnea
cough
adverse reactions with midazolam CV:
hypotension
adverse reactions with midazolam CNS:
drowsiness, oversdeation, HA, seizure,
adverse reactions with midazolam GI
N/V
adverse reactions with midazolam MSK:
pain at injection site myoclonic jerks (infants)
adverse reactions with midazolam misc.
Nystagmus
Dependence
Hiccups
Paradoxical reaction
contraindications with midazolam
Hypersentivitity
NO intrathecal or epidural of parenteral forms containing preservatives- benzyl alcohol
Acute narrow-angle glaucoma
Concurrent use of potent inhibitors of CYP3A4 (amprenavir, atazanavir, ritonavir)
trade name for diazepam
valium
how is diazepam supplied
5mg/mL
MOA for diazepam
Binds to stereospecific benzodiazepine receptors on the post-synaptic GABA neuron at several sites within the central nervous system
Including the limbic system reticular formation
Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions
The shift of chloride ions results in hyperpolarization (LESS excitable state) and stabilization
what drug does diazepam have the same MOA as?
midazolam and lorazipam
uses of diazepam?
Anxiety disorders
ETOH withdrawal
Skeletal muscle relaxant
Convulsant disorders
Pre-opertive sedation
Moderate sedation for procedures or radiographic procedures
ICU sedation
*same MOA as Midazolam
dose of diazepam- anxiety
oral, IM IV
2-10 mg
2-4 times per day
dose of diazepam- muscle spasm
IV IM
5-10 mg initially
5-10 mg in 3-4 hours
*if tetanus larger doses may be required
dose of diazepam sedation
5-10 mg loading dose
maintenance dose of diazepam sedation
0.03-0.1 mg/kg every 30 minutes to 6 hours
dose of diazepam skeletal muscle relaxant
oral 2-20 3-4 times/day
onset of diazepam
IV and oral
IV immediate
oral rapid
duration of IV diazepam
20-30 minutes
duration of oral diazepam
variable
metabolism of diazepam
hepatic
half-life elimination of diazepam
parent drug 20-50 hours in adults of
what conditions increase half life of diazepam
INCREASED with neonates, elderly, hepatic disorders
what is the major metabolite of diazepam? is it active? how long is the half-life
Major metabolite: active- desmethyldiazepam 50-100 hours
peak of diazepam
oral 15 minutes to 2 hours
adverse reactions with diazepam
MANY Hypotension, Vasodilation Amnesia, Ataxia, Confusion, Depression Drowsiness, Fatigue Headache, Slurred speech, Vertigo Paradoxical reactions
Rash, Jaundice, Phlebitis, Pain at injection
Constipation, Diarrhea, Nausea
Salivation changes
Incontinence, Urinary retention
Dysarthria, Tremor, Weakness, Diplopia
Apnea, Asthma, Decreased RR
Contraindications with Diazepam
Hypersentivitity
MG
Resp Insufficiency
Severe hepatic insuff
Sleep apnea
Acute narrow-angle glaucoma
trade name of lorazepam
ativan
how is lorazepam supplied
2mg/mL
4mg/mL
uses for lorazepam
Anxiety management
Short-term relief of anxiety
MOA of lorazepam
Binds to stereospecific benzodiazepine receptors on the post-synaptic GABA neuron at several sites within the central nervous system
Including the limbic system reticular formation
Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions
The shift of chloride ions results in hyperpolarization (LESS excitable state) and stabilization
dose of lorazepam IM
0.05 mg/kg 2 hours before surgery
max dose or IM lorazepam
4 mg
dose of lorazepam IV
0.044 mg/kg 15-20 minutes before surgery
what is the typical dose of IV lorazepam
2mg
what is the max dose of IV lorazepam
4 mg
how much should you not exceed of lorazepam in older than 50
2mg
onset of lorazepam
2-3 minutes
duration of lorazepam
8 hours
metabolism of lorazepam
hepatic
rapid conjugation to inactive compounds
half life elimination of lorazepam
14 hours adults
18 hours ESRD
42 hours neonates
18 hours 2-12 years
peak of lorazepam
IM and oral
less than 3 hours IM
2 hours oral
excretion of lorazepam
urine 88 %
predominately as inactive metabolites
feces 7 %
adverse reaction with lorazepam
Hypotension
contraindications with lorazepam
Hypersentivitity
Resp Insufficiency
*ok if vented
Sleep apnea
Acute narrow-angle glaucoma