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17 Cards in this Set
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- Back
Ketamine(Ketanest, Ketaset, and Ketalar )
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Analgesia, Amnesia, Unconsciousness
Structural similarities to phencyclidine pKa 7.5, formulated pH 3.5 – 5, IV and IM Prepared as racemate NMDA non-competitive Antagonist Binds to PCP site Possible opioid - mosly kappa though weakly binds others, muscarinic, voltage gated, etc. Suppress neutrophil production of inflammatory mediators Improve blood flow, Inhibit cytokines |
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Ketamine MOA?
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Amnesia is dissociative. Dissociates thalamus (responsible for relaying impulse from RAS) to limbic cortex (responsible for awareness of sensation).
How it is does: NMDA is a glutamate (excitatory) receptor. Blocks the excitatory effects. Could interact with other receptors Analgesic effect could come from neutrophil supression – if inhibit cytokines, do not get inflammation and pain. |
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ketamine facts
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Structure: Structural similarities to PCP – hallucinogenic and nuerotoxic
Racemic mixture but S is more active which indicates must interact with receptors Formulated as salt-conjugate acid, so should not be mixed with any basic solution otherwise will precipitate. |
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Ketamine ADME
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A: rapid like thiopental, highly non-ionized, peak 1 min IV 5-10 min IM, not highly bound to plasma proteins.
D: quickly to highly perfused tissues (brain), redistribution leads to awaken, large VD. M: high hepatic clearance with high extraction ratio, some active and inactive metabolites E: elim t1/2 2-3 h, <4% recovered unchanged in urine< 5% in fecal material (so mostly renal), can cause induction |
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other Ketamine ADME facts
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Actually more lipid soluble than thiopental (5 to 10 times) , highly non-ionized ~60%
Because highly liphophilic, quickly distributed, also since ketamine does increase CBF this facilitates even more entry to brain. Volume of distribution 3L/Kg Extraction ration 0.9 Can see tolerance develop |
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Ketamin side effects
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Cardio: Increased HR, art. BP, CO
Can help with hypovolemic shock Catecholamine stores exhausted will see depression Resp: Minimal depression (the least of all options), **Bronchodilation, increased airway secretions Cereb: vascular dilator, increased O2 consump., CBF, ICP Emergence Delirium: terrible dreams, illusions, hallucination, nausea, vomiting Hypertonus (muscle spasm) Nystagmus (involuntary eye movement) |
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other Ketamine facts
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Do not use in case of ICP, use other options
Secretions may cause more laryngospasm and coughing Secreations may be descreased by using an antimuscarinic (glycopyrrolate) Because of emergence delirium, can give a benzodiazepine |
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Other etomidate facts
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Good for higher risk patients
with theophylline may cause seizures With Diazepam increase cardio stimulatory effects and increase elimintation t1/2. Sympathetic antagonists will unmask cardio stimulatory effects Inhaled anesthetics will minimally increase myocardial depression (negative inotrope) Lithium increased duration |
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With Ketamine, avoid the following...
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Cardiac Patients (cardio effects)
Coronary heart disease Hypertension Heart failure Arterial aneurysms Glaucoma Patients (eye pressure) Patients with increase ICP |
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Etomidate (Amidate)
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Anesthesia, Amnesia (low), no analgesia
Structure has imidazole,gives H2O solubility pKa 4.2, Formulated pH 7 fat emulsion, IV Prepared as racemate GABA Modulator Binds to alpha, increases affinity for GABA Depresses RAS Disinhibition of control of extrapyramidal motor activity 30 – 60% myoclonus |
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etomidate ADME
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A: rapid, highly non-ionized (99%), peak 1 min IV, 76% bound,.
D: quickly to highly perfused tissues (brain), redistribution leads to awaken, large VD. M: fast with hepatic and plasma esterase giving biotransformation, high extraction ratio, inactive metabolites E: elim t1/2 2-5 h, context sensitive less than thiopental |
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etomidate S/A's
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Cardio: minimal effect – Best stability of all options
Mild decrease peripheral vascular resistance At clinical conc. No negative inotropic effect. Resp: Minimal, Cereb: vasoconstriction, decrease O2 consump., CBF, ICP same as thiopental Emergence: nausea, vomiting (mixed data) Endocrine: Adrenocortical suppression Inhibits cortisol and aldosterol synthesis (4-8 hrs) Immune: Depresses immune system(lowers plasma cortisol) |
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Other etomidate facts
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Fentanyl, Alfentanil increase plasma levels and decrease elimination t1/2
Opioids decrease myoclonus |
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Propofol
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Anesthesia, Amnesia , Anti-convulsant, no analgesia
Induction drug of choice Structure is alkylated phenol, insoluble in H2O Formulation: 1% in (10% soybean, 2.2% glycerol, 1.2% lecithin) GABA Modulator, decreases rate of release of GABA Anti-pruritic effects Anti-emetic, acts on chemoreceptor trigger zone and vomiting center Waken faster than methylhexital/thiopental/etomidate – and waken more complete. The major advantage Antiemetic also makes induction agent of choice |
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propofol ADME
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A: rapid almost as fast as thiopental, non-ionized
D: quickly to highly perfused tissues (brain), may be taken into lungs, large VD. M: fast with hepatic and extrahepatic giving biotransformation, hydroxylation, glucoronidation, sulfonation, 4-hydroxy weakly active, E: clearance exceeds hepatic blood flow. elim t1/2 0.5-1.5 h, context sensitive less than 40 min., mostly urinary excretion Though clearance is high and very dependent upon liver, cirrhosis does not slow elimination Renal failure not affect clearance |
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propofol S/A's
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Cardio: decrease vascular resistance (vasodilation) venodilation, decreased contractractility, decreased BP, CO, more hypotension than thiopental.
Usually no change in heart rate, impairs baroreflex Usually not a concern Resp: Profound Respiratory depressant Apnea, Conscious sedation decreases ventilatory drive, Decreases upper airway reflexes, bronchodilatation Cereb: Decrease O2 consump., CBF, ICP Can still be used with patients with space occupying lesions Histamine Release: minor No change in heart rate indicates sympatholytic/parasympathomimetic action |
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Propofol other
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Increase dose needed for elderly with lower VD.
Increased dose needed for women. Causes some muscle twitching and hiccups Reduces intraocular pressure Fentanyl and alfentanil increase concentration Versed is synergistic but not sure this is a valuable mixture |