Copy and Edit

Sedatives

Description

Doctorate Anaesthesia Mind Map on Sedatives, created by melian.yates on 14/10/2013.
melian.yates
Mind Map by melian.yates, updated more than 1 year ago
melian.yates
Created by melian.yates about 11 years ago
35
0
0

Resource summary

Sedatives
  1. Phenothiazines
    1. Mechanism
      1. Dopamine Antagonism
      2. CNS
        1. Anxiolytic
          1. Neuroleptic
            1. Tranquiliser
              1. Antiemetic
            2. Mild sedative, if dose is increased, will just prolong level of sedation & increase side effects
          2. NO Analgesic properties
            1. Except Methotrimeprazine (small animal immobilon)
            2. Side Effects/ Toxicity
              1. Basal Ganglia
                1. Movement disorders (Chronic use - humans)
                2. Pituitary Gland
                  1. Increases Prolactin release (Chronic use - humans)
                3. CVS
                  1. Blocks alpha 1 - adrenoreceptors
                    1. Vasodilation & Hypotension
                      1. Can promote hypothermia
                        1. Anti-arrhythmic action
                    2. GIT
                      1. Antispasmodic action on gut
                      2. AntiHistamine (receptor blockade)
                        1. AntiMuscarinic (receptor blockade)
                          1. 5 - HT blockade
                        2. Potency of action dependent on the type of side chain attached to the N atom of the Phenothiazide ring
                          1. R1 = Propylamine
                            1. Increases Sedation
                            2. R1 = Piperadine
                              1. Anticholinergic activity
                              2. R1 = Piperazine
                                1. Less Sedative and Less Anticholinergic
                              3. Drugs
                                1. Acepromazine (ACP)
                                  1. Used extensively (Pre-anaesthetic)
                                    1. Oral tablet (Dogs & Cats), Injection (Small & Large animals), Gel (Horses)
                                      1. Absorption
                                        1. Oral bioavailabilty: 20 - 55%
                                          1. Onset: IM: 20 min, I/V: 5 min
                                            1. Lower end of dose range used I/V
                                              1. Combined w/ Opiods (Boxers and small animals w/ CV compromise)
                                              2. IM Preferred
                                                1. I/V: Given slowly to avoid vasodilaton and hypotension
                                              3. Metabolism
                                                1. Liver
                                                2. Distribution
                                                  1. t 1/2 = 4 - 6hrs
                                                  2. Excretion
                                                    1. Conjugated & Non-conjugated metabolites => Urine
                                                    2. Low dose: Behavior; High dose: sedation
                                                      1. Effective on young, anxious animals
                                                      2. Potentiates action of other drugs
                                                        1. Opiods
                                                          1. General Anaesthetics (Barbituates)
                                                            1. Local Anaesthetics
                                                        2. May lower the threshold for epileptiform sezures
                                                          1. Anticonvulsant properties
                                                            1. Potent Spasmolytic
                                                              1. Tx of Laminitis in Horses
                                                        3. Propionylpromazine
                                                          1. Chlorpromazine
                                                            1. Less potent, longer duration, unreliable in horses (excitement)
                                                            2. Promazine
                                                              1. Better sedation, fewer side effects than Chlorpromazine
                                                              2. Methotrimeprazine
                                                                1. Small animal Immobilin
                                                                  1. Potent Analgesic
                                                                2. Promethazine
                                                                  1. Irritant, Deep IM, Potent Antihistamine
                                                              3. Butyrophenoenes
                                                                1. CNS
                                                                  1. Dopamine Antagonism
                                                                    1. Sedative Action
                                                                      1. Potent Antiemetic
                                                                    2. Side Effects
                                                                      1. Hallucinations, Agitation (Humans)
                                                                    3. CVS
                                                                      1. Vasodilation
                                                                        1. Hypotension
                                                                      2. Drugs
                                                                        1. Azaperone
                                                                          1. Sedate/ modify behavior
                                                                            1. Pigs (Licensed)
                                                                              1. Tx of aggression
                                                                                1. Transport stress
                                                                                  1. Obsteric conditions
                                                                                    1. Premed for local and General Anaesthesia
                                                                              2. Potentiates Anaesthetic Agents
                                                                                1. Slight fall in BP
                                                                                2. Absoprtion
                                                                                  1. Deep IM injection
                                                                                    1. Behind ear (Pigs)
                                                                                      1. Leave undisturbed for 20 min
                                                                                    2. Distribution
                                                                                      1. t 1/2: 2-3 hrs
                                                                                    3. Fluanisone
                                                                                      1. Hypnorm: Used in combination w/ Fentanyl
                                                                                        1. Neurolept Anaesthesia
                                                                                          1. Mice, rats, rabbits & guinea pigs
                                                                                      2. Droperidol
                                                                                        1. Potent Neuroleptic
                                                                                          1. t 1/2: 6 - 8 hrs
                                                                                            1. Potent Antiemetic
                                                                                            2. Used in combination w/ Fentanyl
                                                                                              1. Neuroleptanalgesia
                                                                                        2. Benzodiazepines
                                                                                          1. Mechanism
                                                                                            1. Potentiation of GABA mediated Inhibition
                                                                                            2. CNS
                                                                                              1. Primarily Anxiolytic action
                                                                                                1. Muscle relaxation
                                                                                                  1. Anticonvulsant
                                                                                                    1. Little sedation in young, healthy animals
                                                                                                    2. CVS/ Resp.
                                                                                                      1. Minimal depression
                                                                                                      2. Drug interactions
                                                                                                        1. Synergistic effects with other central depressants
                                                                                                          1. Ex. Barbituates, Antihistamines and alcohol
                                                                                                        2. Metabolism
                                                                                                          1. Liver => Active metabolites
                                                                                                          2. Toxicity (Chronic use)
                                                                                                            1. Cognitive impairment
                                                                                                              1. Tolerance
                                                                                                                1. Dependence
                                                                                                                2. Drugs
                                                                                                                  1. Diazepam (Valium)
                                                                                                                    1. Absorption
                                                                                                                      1. Insoluble in H2O
                                                                                                                        1. Dissolved in propylene glycol
                                                                                                                        2. IV or Oral
                                                                                                                          1. Rapid Onset
                                                                                                                            1. Long acting
                                                                                                                            2. Metabolism
                                                                                                                              1. Liver
                                                                                                                                1. Does not induce hepatic enzyme systems
                                                                                                                                  1. Severe hepatic dysfunction, prolonged duration of action possible
                                                                                                                              2. Distribution
                                                                                                                                1. t 1/2: 20 - 40hrs
                                                                                                                                  1. 95% Protein bound
                                                                                                                                  2. Side Effects
                                                                                                                                    1. Pain on injection
                                                                                                                                      1. Thrombophlebitis
                                                                                                                                        1. Cardiac Arrhythmias
                                                                                                                                        2. Uses
                                                                                                                                          1. To control status epilepticus
                                                                                                                                            1. Stimulate appetite
                                                                                                                                              1. + Ketamine (Horses and Small animals): Induce and Maintain Anaesthesia
                                                                                                                                                1. + Hypnorm (small mammals): Anaesthesia w/ muscle relaxation
                                                                                                                                              2. Midazolam
                                                                                                                                                1. Does NOT cause Thrmbophlebitis
                                                                                                                                                  1. Absorption
                                                                                                                                                    1. H2O soluble
                                                                                                                                                      1. IV, IM, Oral
                                                                                                                                                      2. Distribution
                                                                                                                                                        1. Short duration
                                                                                                                                                          1. t 1/2: Cats: 2 hr
                                                                                                                                                      3. Climazolam
                                                                                                                                                        1. Horses: Maintain Anaesthesia + Ketamine
                                                                                                                                                        2. Tolezepam
                                                                                                                                                          1. + Tiletamine (Dissociative Anaesthetic
                                                                                                                                                        3. Benzodiazepine Antagonists
                                                                                                                                                          1. No intrinsic efficacy; Competetive Anatagonist
                                                                                                                                                            1. Flumazenil
                                                                                                                                                              1. Humans
                                                                                                                                                                1. Dogs, Cattle, Sheep: Antagonism of Diazepam/Midazolam sedation
                                                                                                                                                                  1. Has some Inverse Agonist Activity
                                                                                                                                                                  2. Sarmazenil
                                                                                                                                                                    1. Antagonize Midazolam, when used in combination w/ Ketamine to maintain Anaesthesia in Horses
                                                                                                                                                                    2. Inverse Agonists
                                                                                                                                                                      1. Act @ GABA receptor
                                                                                                                                                                        1. CLOSE the Cl- channel
                                                                                                                                                                          1. Causes the neuron to become vulnerable to excitation
                                                                                                                                                                            1. May promote convulsions
                                                                                                                                                                  3. Alpha 2 - Agonists
                                                                                                                                                                    1. Vary in Selectivity for Alpha 1 and Alpha 2 receptors
                                                                                                                                                                      1. Some also bind Nonadrenergic Imidazoline receptors
                                                                                                                                                                        1. Stimulation = Hypotension and Anti-arrhythmic action
                                                                                                                                                                          1. Imidazoles
                                                                                                                                                                            1. Detomidine
                                                                                                                                                                              1. Really expensive
                                                                                                                                                                                1. Really potent
                                                                                                                                                                                  1. Equipotent in Horses and Cattle
                                                                                                                                                                                  2. Absorption
                                                                                                                                                                                    1. IV or IM
                                                                                                                                                                                    2. Distribution
                                                                                                                                                                                      1. Longer duration
                                                                                                                                                                                        1. t 1/2: 1 - 2 hrs (Horses)
                                                                                                                                                                                      2. Urogenital
                                                                                                                                                                                        1. Slows uterine electrical activity
                                                                                                                                                                                          1. Better for pregnant cows
                                                                                                                                                                                      3. Romifidine
                                                                                                                                                                                        1. Distribution
                                                                                                                                                                                          1. Longer duration
                                                                                                                                                                                            1. t 1/2: up to 3 hrs
                                                                                                                                                                                          2. CNS
                                                                                                                                                                                            1. Causes less ataxia in horses
                                                                                                                                                                                          3. Medetomidine
                                                                                                                                                                                            1. Dogs, Cats, Exotics & Horses
                                                                                                                                                                                              1. Absorption
                                                                                                                                                                                                1. IM, IV or S/C
                                                                                                                                                                                                2. Distribution
                                                                                                                                                                                                  1. t 1/2: 3 hrs
                                                                                                                                                                                                  2. Very potent & very selective for Aplha 2 receptors
                                                                                                                                                                                                    1. Profound ANaesthetic sparing effect
                                                                                                                                                                                                      1. Max effect on BP w/ low doses
                                                                                                                                                                                                        1. Equal mixtture of 2 enantiomers
                                                                                                                                                                                                          1. Dexmedetomidine
                                                                                                                                                                                                            1. Levomedetomidine
                                                                                                                                                                                                              1. Pharmacologically inactive
                                                                                                                                                                                                          2. Dexmedetomidine (Dogs)
                                                                                                                                                                                                            1. Very potent
                                                                                                                                                                                                              1. Greater slectivity for Alpha 2 receptors than Alpha 1
                                                                                                                                                                                                                1. CVS
                                                                                                                                                                                                                  1. Antiarrhythmic
                                                                                                                                                                                                                    1. Depresses HR
                                                                                                                                                                                                                      1. Hypotension
                                                                                                                                                                                                                        1. Pale/ blue tinged mucous membranes
                                                                                                                                                                                                                      2. Distribution
                                                                                                                                                                                                                        1. Highly protein bound: 94%
                                                                                                                                                                                                                          1. Doses based on body surface area
                                                                                                                                                                                                                          2. Anaesthetic sparing
                                                                                                                                                                                                                            1. Reduce dose of induction by 30-60%
                                                                                                                                                                                                                            2. Should only be used for procedures < 20 min
                                                                                                                                                                                                                            3. Clodine
                                                                                                                                                                                                                            4. Oxazolines
                                                                                                                                                                                                                              1. Rilmenidine
                                                                                                                                                                                                                              2. (DO NOT BIND to imidazoline receptors) Phenylethylamines
                                                                                                                                                                                                                                1. Xylazine
                                                                                                                                                                                                                                  1. Absorption
                                                                                                                                                                                                                                    1. IM or IV
                                                                                                                                                                                                                                      1. Cows, Horses: 24 hr rule (before 2nd dose)
                                                                                                                                                                                                                                    2. Distribution
                                                                                                                                                                                                                                      1. t 1/2: Species, Route and Dose dependent
                                                                                                                                                                                                                                      2. Metabolism
                                                                                                                                                                                                                                        1. Metabolised to multiple products that are excreted in urine
                                                                                                                                                                                                                                        2. Low selectivity for Alpha 2 receptors
                                                                                                                                                                                                                                          1. Used in Small and Large animals
                                                                                                                                                                                                                                            1. CNS
                                                                                                                                                                                                                                              1. Species differences in sensitivity
                                                                                                                                                                                                                                                1. Ruminant > Horse/Dog > Pig
                                                                                                                                                                                                                                              2. CVS
                                                                                                                                                                                                                                                1. Arrhythmogenic
                                                                                                                                                                                                                                                  1. Unlike modern drugs
                                                                                                                                                                                                                                                2. Urogenital
                                                                                                                                                                                                                                                  1. Contraction of Uterine smooth muscle
                                                                                                                                                                                                                                                    1. Not licensed for Cows in 3rd trimester => Abortion
                                                                                                                                                                                                                                          2. CNS
                                                                                                                                                                                                                                            1. Sedation (Pre-synaptic)
                                                                                                                                                                                                                                              1. Analgesia
                                                                                                                                                                                                                                                1. Muscle Relaxation
                                                                                                                                                                                                                                                  1. + Ketamine
                                                                                                                                                                                                                                                  2. Given intrathecally or Extradurally
                                                                                                                                                                                                                                                2. CVS
                                                                                                                                                                                                                                                  1. Vasoconstriction
                                                                                                                                                                                                                                                    1. Hypertension
                                                                                                                                                                                                                                                      1. Bradycardia
                                                                                                                                                                                                                                                        1. Due to Vagal reflex (feeback mechansims)
                                                                                                                                                                                                                                                    2. Works well w/ Opiods
                                                                                                                                                                                                                                                      1. Anaesthetic sparing effects (50-95%)
                                                                                                                                                                                                                                                      2. RESP.
                                                                                                                                                                                                                                                        1. Respiratory depression
                                                                                                                                                                                                                                                          1. Reduction in airway resistance
                                                                                                                                                                                                                                                            1. Xylozene (Sheep)
                                                                                                                                                                                                                                                          2. GIT
                                                                                                                                                                                                                                                            1. Vomiting (Some species)
                                                                                                                                                                                                                                                              1. GI motility depressed
                                                                                                                                                                                                                                                              2. Endocrine
                                                                                                                                                                                                                                                                1. Inhibition of ADH
                                                                                                                                                                                                                                                                  1. Diuresis
                                                                                                                                                                                                                                                                  2. Inhibition of Insulin release
                                                                                                                                                                                                                                                                    1. Hyperglycemia
                                                                                                                                                                                                                                                                  3. Urogenital
                                                                                                                                                                                                                                                                    1. Uterine contraction (Cows)
                                                                                                                                                                                                                                                                    2. Alpha 2 - Anatagonists
                                                                                                                                                                                                                                                                      1. Atipamezole (Antisedan)
                                                                                                                                                                                                                                                                        1. "Reversal"
                                                                                                                                                                                                                                                                        2. Yohimbine
                                                                                                                                                                                                                                                                          1. Tolazoline
                                                                                                                                                                                                                                                                            1. Sedation induced by Alpha 2 - Agonists may be reversed by specific Alpha 2 - Antagonists
                                                                                                                                                                                                                                                                              1. Going to reverse Analgesic properties too!
                                                                                                                                                                                                                                                                              2. Absorption
                                                                                                                                                                                                                                                                                1. IM

                                                                                                                                                                                                                                                                            Media attachments

                                                                                                                                                                                                                                                                            Show full summary Hide full summary

                                                                                                                                                                                                                                                                            Want to create your own Mind Maps for free with GoConqr? Learn more.

                                                                                                                                                                                                                                                                            Similar

                                                                                                                                                                                                                                                                            ANZCA Part 2 MCQs - 2015
                                                                                                                                                                                                                                                                            Branden Emmerson
                                                                                                                                                                                                                                                                            Tissue engineering: Case 6
                                                                                                                                                                                                                                                                            Bhavi Mistry
                                                                                                                                                                                                                                                                            ANZCA Part 2 2016
                                                                                                                                                                                                                                                                            Branden Emmerson
                                                                                                                                                                                                                                                                            General Anaesthetic Agents
                                                                                                                                                                                                                                                                            melian.yates
                                                                                                                                                                                                                                                                            Peri-operative Accidents & Emergencies
                                                                                                                                                                                                                                                                            melian.yates
                                                                                                                                                                                                                                                                            Conditions for Surgical Anaesthesia
                                                                                                                                                                                                                                                                            melian.yates
                                                                                                                                                                                                                                                                            Inhalation Anaesthetics
                                                                                                                                                                                                                                                                            melian.yates
                                                                                                                                                                                                                                                                            Analgesics
                                                                                                                                                                                                                                                                            melian.yates
                                                                                                                                                                                                                                                                            Surgical Muscle Relaxation
                                                                                                                                                                                                                                                                            melian.yates
                                                                                                                                                                                                                                                                            NS 43 - anaesthesia
                                                                                                                                                                                                                                                                            Erica Lai
                                                                                                                                                                                                                                                                            PSBD TEST # 3_1
                                                                                                                                                                                                                                                                            Suleman Shah
                                                                                                                                                                                                                                                                            Browse Library