MT115 MT TERM SUM LECTURE \ CESAR UNIT 10: ANESTHESIA I GENERAL ANESTHETICS: INTRAVENOUS OUTLINE Anesthesia A General Anesthesia B Local Anesthesia Barbiturates Benzodiazepines Dexmedetomidine Etomidate Ketamine Opioids Propofol OBJECTIVES At the end of the unit, the student is able to: • Identify accurately the drug and the adverse effects and toxicities of commonly used medications. Anesthesia à is a medical treatment that prevents patients from feeling pain during surgery (National Institute of General Medical Sciences, 2020). Local anesthesia à is an anesthetic agent given to temporarily stop the sense of pain in a particular area of the body. Regional anesthesia à is used to numb only the portion of the body that will undergo the surgery. General anesthesia à is an anesthetic used to induce unconsciousness during surgery (John Hopkins Medicine, 2020). In other books, local and regional anesthesia are grouped into local anesthetic agents. • • • • • STAGES OF ANESTHESIA 1 2 3 Inhaled gases are primarily used for maintenance of anesthesia after administration of an IV agent. Volatile anesthetics delivered to the patient are absorbed via the lungs into the systemic circulation causing dosedependent CNS depression. Induction Maintenance Recovery • INDUCTION • DIPRIVAN INHALED GENERAL ANESTHESIA • ANESTHESIA PRECEDEX AMIDATE KETALAR Induction is the time from administration of a potent anesthetic to development of effective anesthesia. • No specific receptor has been identified as the locus of general anesthetic action. The fact that chemically unrelated compounds produce anesthesia argues against the existence of a single receptor. HALOTHANE • • MAINTENANCE • • • After administering the anesthetic, vital signs and response to stimuli are monitored continuously to balance the amount of drug inhaled and/or infused with the depth of anesthesia. Maintenance provides sustained anesthesia. We need to continuously infuse or let the patient inhale the anesthetic agent so that he/she will not wake up in the middle of the procedure or feel pain. • ISOFLURANE • Postoperatively, the anesthetic admixture is withdrawn, and the patient is monitored for return of consciousness. Recovery à is essentially the reverse of induction and depends on how fast the anesthetic diffuses from the brain. It is the final stage. • • • GENERAL ANESTHETICS: INHALED • SUPRANE FLUOTHANE FORANE NITROUS OXIDE ULTANE Desflurane provides very rapid onset and recovery due to low blood solubility. This makes it a popular anesthetic for outpatient procedures. SEVOFLURANE GENERAL ANESTHESIA Desflurane Halothane Isoflurane Nitrous oxide Sevoflurane This agent undergoes little metabolism and is, therefore, not toxic to the liver or kidney. DESFLURANE RECOVERY • • Halothane à is the prototype to which newer inhalation anesthetics are compared. When halothane was introduced, its rapid induction and quick recovery made it an anesthetic of choice. Due to adverse effects and the availability of other anesthetics with fewer complications, halothane has been replaced in most countries. Sevoflurane has low pungency, allowing rapid induction without irritating the airways. This makes it suitable for inhalation induction in pediatric patients. NITROUS OXIDE • Nitrous oxide (“laughing gas”) is a non-irritating potent analgesic (removes pain) but a weak general anesthetic. TRANS BY: PABATAO | 1D-MT 1 TRANS: Anesthesia • It is commonly known as laughing gas due to the exhilarating effects of inhaling it. OPIOID • • • INTRAVENOUS GENERAL ANESTHESIA • • • IV anesthetics cause rapid induction. Anesthesia may then be maintained with an inhalation agent. IV anesthetics may be used as sole agents for short procedures or administered as infusions to help maintain anesthesia during longer cases. PROPOFOL • Propofol à is an IV sedative/hypnotic used for induction and/or maintenance of anesthesia. Because of their analgesic property, opioids are commonly combined with other anesthetics. The most commonly used opioids are fentanyl, sufentanil, and remifentanil, because they induce analgesia more rapidly than morphine. Morphine à usually given PO (post-operative) ETOMIDATE • Etomidate à is a hypnotic agent used to induce anesthesia, but it lacks analgesic activity. KETAMINE • • Ketamine, a short-acting, nonbarbiturate anesthetic, induces a dissociated state in which the patient is unconscious (but may appear to be awake) and does not feel pain. This dissociative anesthesia provides sedation, amnesia, and immobility. DEXMEDETOMIDINE • Dexmedetomidine à is a sedative used in intensive care settings and surgery. • Local anesthetics block nerve conduction of sensory impulses and, in higher concentration, motor impulses from the periphery to the CNS. Unlike general anesthetics, local anesthetics have specific receptors. Na+ ions channels are blocked to prevent the transient increase in permeability of the nerve membrane to Na+ that is required for an action potential. o Remember that human action potential happens when sodium rushes into the nerve. When propagation of action potentials is prevented, sensation cannot be transmitted from the source of stimulation to the brain. BARBITURATES • • It is a potent anesthetic but a weak analgesic. Barbiturates require supplementary analgesic administration during anesthesia. Amobarbital Pentobarbital Phenobarbital Secobarbital Thiopental BARBITURATES AMYTAL NEMBUTAL LUMINAL SODIUM SECONAL PENTOTHAL The benzodiazepines are used in conjunction with anesthetics for sedation (so that the patient will be asleep or unconscious during the procedure). Alprazolam Chlordiazepoxide Clonazepam Clorazepate Diazepam Estazolam Flurazepam Lorazepam Midazolam Oxazepam Quazepam Temazepam Triazolam • • • BENZODIAZEPINES • LOCAL ANESTHESIA BENZODIAZEPINES XANAX LIBRIUM KLONOPIN TRANXENE VALIUM, DIASTAT DALMANE ATIVAN VERSED DORAL RESTORIL HALCION TRANS BY: PABATAO | 1D-MT 2 TRANS: Anesthesia SUMMARY: DRUGS USED FOR LOCAL ANESTHESIA SUBCLASS, DRUG AMIDES • Lidocaine • Bupivacaine MECHANISM OF ACTION • • Blockade of sodium channels Same lidocaine as CLINICAL APPLICATIONS EFFECTS • • Slows, then blocks, action potential propagation Same lidocaine as • • • PHARMACOKINETICS, TOXICITIES Short-duration procedures topical (mucosal), intravenous, infiltration, spinal, epidural, minor and major peripheral blocks • Longer-duration procedures (but not used topically or intravenously) • • • • Prilocaine, mepivacaine: Like lidocaine (but also risk of methemoglobinemia with prilocaine) Articaine: popular dental anesthetic Ropivacaine, levobupivacaine: Like bupivacaine ESTERS • Chloroprocaine • Like lidocaine • Like lidocaine • Very short procedures (not generally used topically or intravenously) • • • Parenteral (eg, peripheral block, but varies significantly based on specific site) Duration 1-2 h 2-4 h with epinephrine Toxicity: Central nervous system (CNS) excitation (high-volume blocks) and local neurotoxicity Parenteral Duration 3-6 h Toxicity: CNS excitation Cardiovascular collapse (high-volume blocks) • • • • Cocaine • • Same as above Also has sympathomimetic effects • Same as above • Procedures requiring high surface activity and vasoconstriction • • • • • • • Parenteral Duration 30-60 min 60-90 min with epinephrine Toxicity: Like lidocaine Topical or parenteral Duration 1-2 h Toxicity: CNS excitation, convulsions, cardiac arrhythmias, hypertension, stroke Procaine: Like chloroprocaine (but not used epidurally) Tetracaine: Used primarily for spinal anesthesia; duration 2-3 h Benzocaine: used exclusively for topical anesthesia Note: Read the Subclass, Mechanism of Action and Clinical Applications only • • • REFERENCE Lecture and PPT of Jan Harmony A. Cesar, MSPh, MATh, Assistant Professor IV, OIC Dean Whallen, K. (2015). Lippincott Illustrated review: Pharmacology (6th ed.). Philadelphia: Wolters Kluwer. Katzung B.G. (2018). Basic & Clinical Pharmacology (14th ed.). New York: McGraw-Hill Education. Michigan Pain Consultants. (2020). Nociceptive vs neuropathic pain. Retrieved from: https://michiganpain.com/nociceptive-vs-neuropathicpain/. National Institute of General Medical Sciences. (2020). Anesthesia. Retrieved from: https://www.nigms.nih.gov/education/factsheets/Pages/anesthesia.aspx. TRANS BY: PABATAO | 1D-MT 3