anesthetic drugs 1 notes

VT131 - Anesthetic Drugs I - Premedication

Terminology

  • Anesthetic agent: Any drug used to induce a loss of sensation, with or without unconsciousness.
  • Adjunct agent: A drug that is not a true anesthetic but is used during anesthesia to produce other desired effects.
  • Balanced Anesthesia: The practice of using a combination of drugs at lower doses to provide a safer anesthetic compared to a single agent at higher doses.
  • Pharmacokinetics: The effect that the body has on a drug.
  • Pharmacodynamics: The effect that the drug has on the body.
  • Agonists: Drugs that bind to and stimulate tissue receptors.
  • Antagonists: Drugs that bind to receptors but do not stimulate them, often displacing the agonist; commonly used as reversals.
  • Partial agonists: Drugs that bind to and partially stimulate receptors.
  • Agonist-Antagonists: Drugs that bind to more than one receptor type, simultaneously stimulating at least one receptor and blocking at least one other receptor.

Classification of Anesthetic Drugs

  • Based on route of administration
  • Based on the time period that they are used
  • Based on principal effect: Many drugs used have multiple effects.
  • Based on chemistry or drug class.

Regulations for Controlled Substances

  • Anesthetic drugs that are at risk for theft and abuse are regulated by the Drug Enforcement Agency (DEA) under the Controlled Substances Act (CSA).
  • Regulations require strict handling, record-keeping, and storage.
  • Consequences of misuse: Theft, illegal use, or diversion of a controlled substance are criminal acts punishable by imprisonment and/or fines, which may impact professional licensure eligibility.

Controlled Substance Schedules

  • The CSA assigns drugs into five drug schedules according to their potential for abuse:
    • Schedule I: Highest abuse potential; none in veterinary medicine.
    • Schedule II: High abuse potential; examples include fentanyl, morphine, and hydromorphone.
    • Schedule III: Medium abuse potential; examples include ketamine, telazol, buprenorphine, and pentobarbital.
    • Schedule IV: Low abuse potential; examples include diazepam, midazolam, alfaxalone, butorphanol, phenobarbital, alprazolam.
    • Schedule V: Lowest abuse potential; example includes Lomotil.

Record-keeping Requirements

  • General inventory of controlled drugs must be performed every 2 years.
  • Daily accounting of drug use is documented in controlled drug logs.
  • Controlled substance logs:
    • Must be official documents in a bound booklet with numbered pages filled out in indelible ink.
    • Kept for a minimum of 2 years.
    • Schedule II drug logs should be kept separate from other records.

Storage Requirements for Controlled Substances

  • Controlled substances must be securely locked in a substantially constructed cabinet.
  • Containers of controlled substances should not be left unattended on countertops or in public areas.
  • In cases of unexplained significant loss or suspected theft, registrants must notify the DEA and local police within one business day, and complete DEA Form 106.

Preanesthetic Medications

  • Premedications are given alone or with other drugs as part of balanced anesthesia.
  • Common premedications include:
    • Anticholinergics
    • Phenothiazines
    • Benzodiazepines
    • Alpha2-adrenoceptor agonists (alpha2-agonists)
    • Opioids.

Reasons for Using Preanesthetic Medications

  • Calm or sedate an excited, frightened, or aggressive animal.
  • Minimize adverse effects of concurrently administered drugs.
  • Reduce the required dose of concurrently administered agents.
  • Produce smoother anesthetic inductions and recoveries.
  • Decrease pain and discomfort before, during, and after surgery.
  • Produce muscle relaxation.

Administration of Preanesthetic Medications

  • The administration route can be IV, IM, or SQ.
  • After medicating, patients should remain in a quiet area for observation for 20-30 minutes to allow drug effects to take place.

Combining Drugs in a Syringe

  • Two or more anesthetic agents can be combined as premedications, typically mixed in the same syringe.
  • Most anesthetic drugs, except for diazepam, are water-soluble and can be combined safely.
  • Note: Diazepam is non-water-soluble and cannot be mixed with other drugs, except for ketamine (can be safely mixed).

Anticholinergics

  • Anticholinergics are noncontrolled drugs used to prevent bradycardia and decrease salivary secretions.
  • Examples:
    • Atropine
    • Glycopyrrolate.

Mode of Action of Anticholinergics

  • Anticholinergics block the parasympathetic nervous system, hence considered parasympatholytic.
  • Most parasympathetic effects are mediated by the Vagus nerve; stimulation during intubation and surgery can lead to bradycardia and bronchoconstriction.
  • Anticholinergics effectively prevent bradycardia and decrease salivary secretions.

Anticholinergic Administration

  • Routes: IV, IM, SC, or IT.
  • Atropine: Faster onset, shorter peak, shorter duration; preferred in emergencies.
  • Glycopyrrolate: Slower onset, longer peak and duration; minimally crosses the placenta; preferred in cesarean sections.

Effects of Anticholinergics

  • Central Nervous System Effects:
    • Anticholinergics do not act as sedatives and lack CNS effects.
  • Cardiovascular Effects:
    • Prevent bradycardia; avoid use in animals with preexisting tachycardia or heart disease.
  • Respiratory Effects:
    • Decrease and thicken respiratory and salivary secretions, and induce bronchodilation.
  • Other Effects:
    • May cause mydriasis (pupil dilation) and decreased lacrimal secretions
    • Decreased gut motility.

Tranquilizers and Sedatives

  • Tranquilizers: Drugs that reduce anxiety without necessarily decreasing wakefulness.
  • Sedatives: Drugs that cause reduced mental activity and induce sleepiness.
  • The effects of these drugs often overlap and are interchanged.
  • Tranquilizer/Sedatives:
    • Phenothiazines
    • Benzodiazepines
    • Alpha2-adrenoceptor agonists (alpha2-agonists).

Phenothiazines: Acepromazine

  • Use of Acepromazine ("Ace") includes:
    • Lower dose requirement for general anesthetic.
    • Smooth induction and recovery.
    • Provides sedation/tranquilization for minor procedures.
  • Approved for dogs, cats, and horses and administered via IV or IM.
  • Responses to the drug vary based on species and breed; doses should be reduced in collies and Australian shepherds to minimize prolonged sedation.

Effects of Phenothiazines

  • Central Nervous System Effects:
    • Causes sedation but does not provide pain control, decreases anxiety, and may lower seizure threshold.
    • Occasionally might induce excitement or aggression.
  • Cardiovascular Effects:
    • Possess antiarrhythmic properties; cause hypotension and hypothermia.
  • Other Effects:
    • Anti-emetic effects, may lead to prolapse of the penis in horses, reduced PCV due to spleen uptake of RBCs, and prevents release of histamine.

Benzodiazepines

  • Benzodiazepines are tranquilizers used with other agents for muscle relaxant and anticonvulsant properties.
  • Alone, they produce unreliable sedation and may cause dysphoria.
  • Examples:
    • Midazolam – IV or IM
    • Zolazepam – IV or IM
    • Diazepam – IV (irritating IM)
    • Flumazenil – Reversal drug for benzodiazepines.
  • Diazepam and midazolam are light-sensitive and stored in brown glass vials; Zolazepam is available only mixed with tiletamine.

Effects of Benzodiazepines

  • Central Nervous System Effects:
    • Produce unreliable sedation unless used with other drugs, have anticonvulsant activity, and have no analgesic properties.
  • Cardiovascular and Respiratory Effects:
    • Minimal effects on cardiovascular and respiratory systems, leading to a high margin of safety; diazepam or midazolam are used for active seizures.
  • Other Effects:
    • Excellent muscle relaxants; decrease anesthetic requirements; cross the placenta and may cause CNS depression in neonates following cesarean.

Alpha2-Adrenoceptor Agonists

  • Also referred to as alpha2-agonists, they are used alone or in combination for sedation, analgesia, and muscle relaxation; administered IV or IM.
  • Safe for young, healthy patients but should be avoided in geriatric, diabetic, pregnant, pediatric, or sick patients.
  • Examples:
    • Xylazine
    • Dexmedetomidine
    • Detomidine.

Effects of Alpha2-Adrenoceptor Agonists

  • Central Nervous System Effects:
    • Potent sedatives that provide short-lived analgesia and may alter behavior; horses may tremble or kick; cattle may frequently lie down or fall over.
  • Cardiovascular effects:
    • Initial vasoconstriction, hypertension, reflex bradycardia (pale mucous membranes); dramatic bradycardia (30 to 50 bpm in dogs) and possible hypotension with decreased cardiac output may occur, alongside cardiac arrhythmias.
  • Respiratory Effects:
    • Respiratory depression, especially in cattle.
  • Other Effects:
    • Muscle relaxation; increased effects of other anesthetics; vomiting; transient hyperglycemia; hypothermia; potentially induces abortion in cattle during last trimester; horses may sweat.

Monitoring and Reversal of Alpha2-Adrenoceptor Agonists

  • Vital signs should be carefully monitored in patients receiving alpha2-agonists.
  • Administration of anticholinergics to mitigate bradycardia is ineffective and may strain the heart.
  • Effective management: If excessive bradycardia occurs, the superior approach is to reverse the alpha2-agonist using specific antagonists.
    • Reversals:
      • Yohimbine and tolazoline can reverse xylazine effects.
      • Atipamezole reverses dexmedetomidine effects; administer IM only in cats, IM in dogs or IV slowly in emergencies.

Opioids

  • Opioids are used for analgesia, sedation, and to reduce the dosage required for other anesthetics.
  • They possess a wide margin of safety and can be used in debilitated patients.
  • Examples:
    • Agonists: morphine, hydromorphone, oxymorphone, fentanyl, meperidine
    • Partial Agonist: buprenorphine
    • Agonist–Antagonists: butorphanol and nalbuphine
    • Antagonist (reversal): naloxone.

Opioid Mode of Action and Pharmacology

  • Opioids act on receptors located in the brain and spinal cord.
  • Types of opioid receptors:
    • Mu (μ) agonism: causes analgesia, bradycardia, hypothermia, hypoventilation, vomiting, constipation.
    • Kappa (κ) agonism: induces minor analgesia, sedation, dysphoria.
    • Delta agonism: leads to hypoventilation, constipation, urinary retention.

Effects of Opioids

  • Central Nervous System Effects:
    • Opioids are strong analgesics that may induce CNS depression (sedation) or excitement; cats, horses, and ruminants might show CNS stimulation.
    • Can elevate intraocular and intracranial pressures; use cautiously in head trauma and CNS disorders.
  • Cardiovascular System Effects:
    • May result in vagus-induced bradycardia.
  • Respiratory System Effects:
    • Dose-dependent respiratory depression; panting commonly seen in dogs.
  • Other Effects and Adverse Effects:
    • Hypothermia in dogs; hyperthermia in cats; increased salivation, vomiting, diarrhea, gastrointestinal stasis, constipation; noise sensitivity; miosis in dogs; mydriasis in cats, ruminants, and horses; increased sweating in horses; decreased urine production and retention.
    • Morphine and meperidine can cause facial swelling and hypotension due to histamine release.

Neuroleptanalgesia

  • Definition: Neuroleptanalgesia is defined as a state of sedation and analgesia induced by simultaneous administration of an opioid and a tranquilizer.
  • Example: Combination of dexdomitor and butorphanol primarily used for minor procedures.
  • Preparedness: Anesthetists should be ready to intubate and ventilate patients as required during procedures where neuroleptanalgesia is applied.

Opioid Antagonists (Reversals)

  • Reversal: Opioids can be reversed with an antagonist, such as naloxone.
  • These antagonists will reverse both desirable and undesirable effects of the opioid.
  • An agonist–antagonists, such as butorphanol, can be employed to partially reverse effects of pure agonists.