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CCEMTP Pharmacology
SEDATIVES AND ANALGESICS
46
Medical
Professional
02/27/2008

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Term

Pharmacology

Sedatives and Analgesics

AGITATION

Definition

Etiology

Hypoxia, Pain, withdrawl, Sleep alterations,

  • ICU psychosis-"cluster" of psychotic symptoms in the form of delrium; acute brain failure
  • WIthdrawl to alcohol, benzodiazepines, opiates, street drugs
Term

SEDATIVES

ICU PSYCHOSIS

Definition

Diagnosis of exclusion-when they don't know what else to call it

10-15% of patients over 65 yrs old in ICU-"sundowners" sensory deprivation-unfamiliar surroundings

MANIFESTATIONS: hallucinations, combativeness, disorientation

can occur as a result of some antibiotics, heart failure

Term

ANALGESICS

Therapeutic Goals

Definition

To prevent harm to patient and oters

Avoid toxicity

alleviate discomfort

increase oxygenation

Term

Sedatives

(Properties)

Definition
  •  
    •  
      • Onset and DUration
      • Reversibility
      • Accumulation
      • Toxicity
      • Withdrawal
      • Tolerance
      • Drug Interactions
Term

Sedatives

Routes of Administration

Definition
  • Oral
  • Intramuscular
  • Intravenous
  • Bolus
  • Continuous
Term
Therapeutic Classes of Sedatives
Definition
  • Butyrophenones (eg Haloperidol)
  • Benzodiazepines
  • Propofol (diprovan)
Term
Haloperidol (Haldol)
Definition

Pharmacology

-Butyrophenone

-Post-synaptic dopamine antagonist

-high potency neuroleptic

-allows the patient to process incoming stimuli

Term

Haloperidol

Parmokinetics

Definition

-Onset: 10-30 min

-Duration: 2-6 hours

-Half life: 10-19hours

DOSING

  • Mild agitation:  0.5-2.0 mg
  • Moderate agitation: 2.0-5.0mg
  • Severe agitation: 10-20mg
Term
Haloperidol (haldol)
Neuroleptization
Definition
-used for severely agitated patients
-Give initial dose IV and repeat q30min
-Double dose every 30 min until agitation is controlled
-give 1/2 total dose daily in divided doses
-taper over 2-3 days
Term
Haloperidol (haldol)
Adverse Effects
Definition
-QT prolongation
-Acute dystonic reaction
-Neuroleptic malignant syndrome
-hypotension
-sedation
Term
Droperidol (Inapsine)
Definition
Pharmocology
-Similar to haloperidol
-Post ganglionic alpha adrenergic blocker
-can be used as an anti-emetic
ADVERSE EFFECTS
-hypotension
-Sedation
Term
Droperidol (Inapsine)
Pharmokinetics
Definition
Onset-3-10 min
Duration 2-4 hours
1/2 life 2-3 hours
Term
BENZODIAZEPINES
Definition
Pharmocology
-Gaba mediated inhibition of pre and post synaptic dopamine
-EFFECTS
-anxiolysis
-Sedation
-Amnesia
-Skeletal muscle relaxation
Term
Midazolam (Versed)
Definition
Pharmokinetics
ONSET 1-5 min
DURATION 2-6 hours
1/2 life 1.5-3hrs
-prolonged up to 12 hrs in critically ill patients
-Active metabolite
Term
Midazolam (Versed)
DOSING
Definition
Mild agitation: 1-2 mg--2mg/hr
Moderate agitation: 5mg--3-5 mg/hr
Severe agitation: 7-10mg--5-7 mg/hr
Continuous infusion compatible with D5W, NS--Dosage range 1-10 mg/hr
Term
Lorazepam (ativan)
Definition
Pharmokinetics
ONSET: 1-5min
DURATION: 6-8hrs
1/2 life: 15-20hrs
-no active metabolites
Term
Lorazepam (Ativan)
DOSING
Definition
Mild agitation 0.5-1mg
Moderate Agitation 1-2 mg
Severe Agitation 2-4mg
Maximum rate 2mg/min
DILUTE BEFORE ADMINSTERING
-may be given by continuous infusion
Term
Lorazepam (Ativan)
Continuous infusion
Definition
-Compatable with D5W, NS
-Maximum concentration dependent on preparation
-DOSE: titrate to desired response
-Watch for precipitation
Term
Diazepam (Valium)
Definition
Pharmokinetics
-ONSET: 1-5 minutes
-DURATION: 20-30 min
-1/2 LIFE: 20-80hrs
-active metabolite
Term
Diazepam (valium)
DOSING
Definition
Moderate Agitation: 2-5mg
Severe agitation: 5-10mg
Maximum rate: 5mg/min
Term
Benzodiazepines
ADVERSE EFFECTS
Definition
-Hypotension
-Respiratory depression
-Bradycardia
-Excessive sedation
Term
Benzodiazepines
RISK FACTORS
Definition
-Elderly
-hypovolemia
-increased dose
-Liver impairment
Term
Flumazenil (Romazicon)
Definition
Benzodiazepine antagonist
PHARMOKINETICS
ONSET: 1-2 min
DURATION: <1hr
1/2 LIFE: 40-80 min
Term
Flumazenil (Romazicon)
DOSING
Definition
-0.2mg over 15seconds
-repeat 0.2 mg every minute
-total dose 1mg
OVERDOSE TREATMENT
0.2mg over 30seconds
-0.5mg every minute
-total dose 5mg
Term
Flumazenil (Romazicon)
DOSING-resedation
Definition
Repeat dosing for resedation
-1mg (0.5mg/min)
-every 20min
-no more than 3mg/hr
CONTINUOUS INFUSION
-compatable with D5W, NS
-Rate: 0.5-1.0 mg/hr
Term
Flumazenil (Romazicon)
ADVERSE EFFECTS
Definition
-Withdrawal
-Seizures
--TCA overdose (unknown effects of bicarbonate)
-Resedation
Term
PROPOFOL (DIPROVAN)
Definition
Pharmocology
-Sedative hypnotic for induction and maintenance of anesthesia or sedation
-mechanism of action unknown
Term
PROPOFOL (Diprovan)
Pharmokinetics
Definition
ONSET: 40sec-1min
DURATION: 5-10min
1/2 LIFE: 1-3min
-no active metabolite
Term
PRPOPFOL (Diprovan)
DOSING BY CONTINUOUS INFUSION
Definition
Initiate @ 5mcg/kg/min
-increase in 5-10 mcg/kg/min increments
-adjust every 5-10min
-usual max 50mcg/kg/min
--higher doses have been used
Term
PROPOFOL (Diprovan)
ADMINISTRATION CONSIDERATIONS
Definition
-Strict aseptic technique
-use vented tubing
-discard after 12 hours
--if dispensed in manufacturer vial
--discard in 6hrs if removed
-DO NOT FILTER
Term
PROPOFOL (DIPROVAN)
ADVERSE EFFECTS AND DRUG INTERACTIONS
Definition
ADVERSE EFFECTS
-Hypotension-up to 30%
-bradycardia
-hyperlipidemia
DRUG INTERACTIONS
-sedatives
-analgesics
-Intralipids
Term
ETOMIDATE
Definition
-a short acting, non barbituate intravenous anesthetic agent with hypnotic effects, etomidate is used to facilitate endotracheal intubation and advanced airway management
Term
ETOMIDATE
ACTION
Definition
ACTION
-main effect in the CNS is the production of hypnosis
-Mechanism(s) of CNS hypnosis
-not known for certain
-may enhance GABA inhibitory pathways in CNS
Term
ETOMIDATE
Onset and Duration
Definition
-after initial IV administration, onset occurs within 30-60 seconds
-patients awake from the induction dose within 3-10 minutes
-0.1 mg/kg bolus will provide approximately 100 seconds of sleep; 0.2 mg/kg will provide 200 seconds; 0.3mg/kg--300seconds
Term
ETOMIDATE
SIDE EFFECTS
Definition
-most frequent side effects are transient skeletal muscle movements, eye movement, tonic movement, etc.
-Transient apnea may occur as will transient hypotension
Term
ETOMIDATE
Side EFFECTS (cont)
Definition
GI-nausea, vomiting
RESPIRATORY-apnea, hyperventilation, hypoventilation, hiccuping, laryngospasm
Term
ETOMIDATE-SIDE EFFECTS (cont)
Definition
CNS-Myoclonic movements, Averting movements
CV-Hypertension, Hypotension, Tachycardia, Bradycardia, pain at injection site
Term
ETOMIDATE
DOSE and ROUTE
Definition
INITIAL DOSE: 0.3 mg/kg rapid IVP
2nd DOSE: 0.3 mg/kg rapid IVP 60 SECONDS AFTER INITIAL DOSE*
*the 2nd dose is only given if the patient's jaw is clenched or a bite reflex is present-may be given IV or IM
Term
ANALGESIA--effects of pain
Definition
-increased sympathetic outflow
-catecholemine release
-tachycardia
-tachypnea
-hypertension
Term
OPIOIDS
Definition
Pharmacology
-bind to opiate receptors in the CNS
-Alter perception of pain
-alter response to pain
Term
Morphine Sulfate
Definition
Pharmokinetics
ONSET: 15-60min
DURATION: 3-7hrs
1/2 LIFE: 2-4 hrs
Term
MORPHINE SULFATE
ADVERSE EFFECTS
Definition
-respiratory depression, sedation, constipation, vomiting, addiction
Term
NALOXONE (NARCAN)
Definition
-opioid antagonist
-pharmokinetics
ONSET: 2 min
DURATION: 20-60min
-1/2 life: 1-1.5hrs
-will reverse opioid effects; including pain control
Term
NARCAN
Dosing
Definition
-reversal of sedation: 0.1-0.2 mg every 2-3 minutes
OVERDOSE: 0.4-2mg every 2-3 minutes up to 10mg
-may use continuous infusion
Term
NARCAN
continuous infusion
Definition
-compatable with D5W, NS
-use 2/3 initial dose x 10
-add to 1 liter
-run at 100ml/hr
-give 1/2 initial dose 15min into infusion
Term
NARCAN
Adverse Effects
Definition
-secondary to narcotic reversal
--hypertension, tachycardia
--diaphoresis
--nausea, vomiting
-Pulmonary edema
-arrhythmias
-Excitation
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