ANESTHETICS

GENERAL ANESTHETICS
Action: analgesia, amnesia, loss of consciousness, inhibit autonomic & sensory reflexes, skeletal
muscle relaxation
Ideal anesthetic:
• Induces Rapid and smooth loss of consciousness then prompt recovery after its
discontinued
• Wide margin of safety
• No adverse effects
Depth of Anesthesia
1. Analgesia - initially produces analgesia
- development of amnesia
2. Excitement - delirium with or without vocalization
- irregular respiration
- retching and vomiting may occur
- regular breathing is re-established
3. Surgical anesthesia - from regular breathing to apnea
- changes in ocular movement, reflex and pupil size
4. Medullary depression - severe CNS depression: includes the vasomotor center
&respiratory center causing cessation of circulatory and respiratory
support and death occurs

Stages of Anesthesia
Induction - use of rapid acting agents e.g. Thiopental (IV)
- Halothane &Sevoflurane (Inh)
Maintenance - period of surgical anesthesia
- vital signs &response to stimuli are monitored to adjust IV - Inh dose to
obtain "balanced anesthesia"
Recovery - withdrawal/discontinuation of anesthesia
- anesthesia is redistributed from site of action

PATIENT FACTORS IN SELECTING AN ANESTHESIA

A. Status of organ system
Liver and kidney - influences distribution &clearance
- targets organs for toxic effects
- F-, Br-and other metabolites of halogenated hydrocarbons can
accumulate with repeated administration
Respiratory system - asthma &abnormal ventilation/perfusion can complicate control of
inhalation anesthetics
- respiratory depression
- bronchodilation
Cardiovascular system - hypotension
- sometimes favorable but may cause ischemia in some tissues
- halothane sensitized heart to sympathomimetics - arrhythmia
Nervous system - neurological disorder (epilepsy and MG)
- sensitivity to halogenated hydrocarbons which induces malignant
Hyperthermia
 Pregnancy - nitrous oxide - aplastic anemia
-Benzodiazepine - temporary hypotonia &altered thermoregulation in
the newborn
CI: labor and pregnant women

B. Concomitant use of drugs

Multiple Adjunct Agents/ - facilitates Induction of anesthesia
Preanesthetic meds - lower the dose of anesthesia
- may also cause undesirable effects ex. Hypoventilation
Concomitant use of additional - agents used to treat underlying disease
- drugs of abuse
Ex. Alcoholics have elevated hepatic enzymes involved in the
non-anesthetics metabolism of barbiturates &may develop tolerance of opioids

Preanesthetic Medications
Anticholinergics(Atropine)
Antiemetics(Ondansetron)
Antihistamine (Diphenhydramine)
Muscle relaxants(neuromuscular blockers)
Opioid analgesics
- decrease oral &airway secretion
- prevent/treat bradycardia
- prevents aspiration of stomach content
- prevents allergic reactions (Ranitidine)
- reduces gastric acidity
- facilitate intubation
- decrease muscle tone and prevent movements
- exert respiratory depression &decrease HR

A. Inhaled Anesthetics (most are used for maintenance of anesthesia)

NITROUS OXIDE
SEVOFLURANE - Rapid onset & recovery
HALOTHANE
ISOFLURANE
ENFLURANE - Moderate onset & recovery
DESFLURANE - poor induction but rapid recovery
METHOXYFLURANE - very slow onset and recovery

Advantage : Readily excreted by exhalation

Easy to change concentration to control depth
Potency : measured by Median Alveolar Concentration - the concentration needed to eliminate
movement on 50% of patients -- the lower the MAC the higher the potency
Absorption : Alveolar wash in : refers to the replacement of normal lung gases with anesthetics
Excretion : Wash out: the blood drives the anesthetic to the alveoli;
the faster they are absorbed, the faster they are excreted
MOA : Increase sensitivity of GABAA receptors prolonging the opening of channels
Increase activity of Glycine receptors
Block excitatory postsynaptic action of Nicotinic Receptors
HALOTHANE Use : Potent anesthetic and weak analgesic
Administered with Nitrous oxide, opioids, local anesthetics
AE : Hypotension, bradycardia Tx: PHENYLEPHRINE
Malignant hyperthermia Tx: DANTROLENE
Hepatitis (adults)
Used in children especially for its pleasant odor
NITROUS OXIDE Use : Potent analgesic
Weak anesthetic
Dental surgery (30% N2O with oxygen)
→ no respiratory depression
→ no muscle relaxation
Adv : least hepatotoxic of all inhaled anesthetics
Safest anesthetic but must be used with 20% oxygen
Popular anesthetic for outpatient surgery
AE : Vasodilation → hypotension
DESFLURANE Laryngospasm, coughing and excessive secretions
SEVOFLURANE Adv : rapid uptake without irritating the airway
(suitable for children) replaced Halothane
Recovery is faster than others
CI : Kidney failure (release of F-ions)
ENFLURANE Adv : less arrhythmia and sensitivity to catecholamines
Greater muscle relaxant effect
D/A : CNS excitation
CI : Seizures
Kidney failure (release of F-ions)
ISOFLURANE Adv : less F-; no arrhythmia and sensitization
AE : Hypotension due to peripheral vasodilation
Coronary vasodilation inc blood flow
B. Intravenous Anesthetics (most are used for induction of anesthesia)
Barbiturates (rapid)
Benzodiazepines (slow)
Etomidate - rapid
Propofol - rapid
Ketamine - moderate

BARBITURATES (Thiopental) Use : Potent anesthetic

Weak analgesic
Depresses the CNS in less than 1min
AE : Hypotension in hypovolemic patients
Laryngospasm, coughing, bronchospasm
Apnea, chest wall spasm
CI : Asthma
Acute intermittent porphyria
BENZODIAZEPINE Midazolam (fast acting), Diazepam, Lorazepam
Use : sedation of patient to facilitate amnesia
ETOMIDATE Use : Hypnotic agent but no analgesic activity
Formulated with Propylene glycol to increase solubility
AE : Decrease cortisol and aldosterone levels
Should not be used for long perfusions
No Heart and Circulation AE → used for px with Coronary
Artery Disease &Cardiovascular Dysfunction
PROFOPOL Use : Induction (onset at 40 sec)
– replaced thiopental as Maintenance
1stchoice for induction AE : Depression of the CNS
because it causes euphoria Muscle twitch, spontaneous movement, hiccups
and no NV Decrease BP and intracranial pressure
KETAMINE Use : Sedation, anesthesia, immobility
(dissociative anesthesia) – Employed in children and young adults for short surgery
patient is unconscious but
appears awake AE : •Heart stimulation (inc BP) used for hypovolemia,
cardiogenic shock, and asthma
•Increase cerebral blood flow, causes hallucinations and
nightmares in adults
CI : HTN and stroke

LOAL ANESTHETICS

ESTERS AMIDES
Cocaine Lidocaine
Procaine Mepivacaine
Tetracaine Bupivacaine
Benzocaine Ropivacaine

MOA: Interacts with protein receptors of Na+ channel to inhibit its function
Blocks nerve conduction of sensory impulses from the periphery to the CNS
USE: Abolish sensation or sometimes movement without altering the consciousness of the patient
AE: Bupivacaine → cardiotoxicity (arrhythmia) Mepivacaine → teratogenic
Procaine → allergies (metabolized to p-aminobenzoic acid)