IV Anesthetics 2.

Depress RAS (reticular activating

system)
- If with overdose has antidote
3. Depress transmission in the
Dissipation of effect depends in sympathetic nervous system ganglia

Redistribution CNS effect

Biotransformation
Mild sedation to Coma
Excretion
Respiratory effect
Anesthetic vapors and gases
Respiratory depression
Partial pressure in blood can be altered
by varying the concentration of agent in Circulatory effect
the inspired mixture
If overdose turn off Direct myocardial depression

Characteristics of ideal IV anesthetic advantage Disadvantage

Rapid induction Respiratory
Rapid degradation depression
No secretion Little analgesia
Short elimination half life
Non-emetic Poor muscle relaxation
Barbiturates

Urea + Malonic acid + Barbituric acid Contraindication

Phenobarbital anticonvulsant
Porphyria marked increase in
o Phenol group confers
porphyria synthesis
anticonvulsant activity
Status asthmaticus thiopental and
Methohexital
thiomylal increases histamine release
o Methyl group confers
o Substitute methohexital and
convulsant activity
pentobarbital
Thiopental
o Sulfur group fast onset Benzodiazepines
Thiamylal
- Diazepam, lorazepam, midazolam
Mode of action
Favourable pharmacologic characteristics
1. Depress polysynaptic responses in
1. Amnesia
CNS via
2. Minimal depression of vent
o Presynaptic decrease release
3. Anticonvulsant
of AH
4. Rare development of tolerance or
o Postsynaptic-
physical dependant
Inhibition of polysynaptic neuron
Mode of action same as barbiturates
Indication Patient is non-communicative

Induction of anes Mode of action

Supplement to regional anes
Interruption of cerebral associative
Provide hypnosis
pathway
Control of convulsive condition
Relative sparing of RAS and limbic
ECT treatment
system
Long duration of action Depression of thalamo neocortical
system
Diazepam Suppression of lamina specific SC
Insoluble in water activity
Propylene glycol Na benzoate Disadvantage
Longest duration of action ( 21-37hrs)
venoirritating Increase BP and Intraocular pressure
Desmethyl diazepam Diplopia movement and nystagmus
Metabolized more slowly
Side effect hallucination prevents by giving
Lorazepam BZD

Insoluble in water Contraindication

Glycol OH solution
Eye surgery
venoirritating
History of increased intraocular
Midazolam pressure
CVA /stroke, psych prob
Water soluble HPN
Non-venoirritating
Shortest half life

Antagonist NEUROLEPTIC ANALGESIA

Physostigmine nonspecific and Properidol

inconsistent
Fentanyl synthetic narcotic analgesia
Aminophylline nonspecific
Flumazenil (anexate) specific Innovar mixture of dnoperidol
benzodiazepine antagonist
*A neuroleptic drug and a narcotic analgesia
Tretamine given together to:

- Phencyclidine derivatives Somnolence without total

- Product dissociatives anes consciousness
o Cataleptic state eyes remain Psychological indifference to
open, slow nystagmus gaze environment
 No voluntary movement Agonist meperidine, Demerol,
Analgesia fentanyl
Satisfactory amnesia Antagonist nalbuphine

Dnoperidol Delta receptor

Advantage: Effect modulate mu receptor activity

Agonist leu-enkephalin
- sleepiness and mental detachment
Antagonist naloxone
- Antiemetic
- Weak blocking effect of a-adrenergic Kappa receptor
receptor
Effect analgesia and sedation
Disadvantage: Agonist nalbuphine
Antagonist naloxone
- No antagonist
- Peripheral vasodilation Sigma receptor
- Most common extrapyramidal effects
- Cerebral vasoconstrictor Effect tachycardia, tachypnea
Agonist ketamine
Fentanyl Antagonist naloxone
advantage Disadvantage SUMMARY:
Antagonist- naloxone Respiratory
depression Naloxone pure opioid antagonist except mu-2
No histamine release Bradycardia receptor
Causes euphoria Bronchoconstriction
No direct myocardial Emetic Nalbuphine antagonist to mu-2 receptor
depression effect
Produce analgesia Miosis - Agonist of kappa receptor
Muscle rigidity, nuchal
rigidity Naloxone uses:
Patient awareness
- For tx of opioid induced depression of
ventilation
Class of opoids receptor - For tx of deliberate opioid overdose
- Detects suspected physical dependence
Mu-1
Side effects:
Effect supraspinal analgesia
Agonist morphine - Nausea and vomiting
Antagonist naloxone - Cardiovascular stimulation

Mu-2

Effect respiratory depression,

decreased heart rate