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171 Cards in this Set
- Front
- Back
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What are the 3 excitatory amino acids?
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Glutamate
Aspartate Homocysteate |
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Lamotrigine
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Inhibits glutamate release
- new anti seizure drug |
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NMDA receptor blockers
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Decrease neuronal necrosis and apoptosis following stroke
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Ketamine
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IV anesthetics
Blocks NMDA receptors |
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AMPA sensitizers
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Useful in treatment of dementia
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Acamprosate
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NMDA blocker useful TX of alcohol withdrawl
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Anxiolytic drugs act as enhancers of (1) ex (2), (3)
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GABAa transmission
2 benzos 3 barbiturates |
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Main inhibitory nt in spinal cord
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Glycine
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Strychine
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Blocks glycine receptors in spinal cord - causes convulsions, increases spinal reflexes and muscle tonus
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3 main functions of serotonin
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Modulation of pain perception
Mood regulation Food intake |
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Serotonin cell bodies located in
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Rap he nucleus
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Fluoxetine
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SSRI
- strong anti depressant action |
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Buspirone
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5HT1a-R agonist
New anxiolytic drug |
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Sumatriptan
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5HT1d-R agonist
Migraine TX |
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Metoclopromide
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5HT4-R agonist
GI pro kinetic drug |
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Ondansetron
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5HT3-R antagonist
Anti emetic |
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Ergotamine
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5HT1b-R agonist
Constrict meningeal vessels TX of migraine |
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Inhibitors of serotonin uptake (1) appetite
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Decrease
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4 main actions of dopamine and pathways
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Inhibits prolactin release - tuberohypophyseal
Movement control - nigrostriatal Psychotic reactions - mesolimbic/ mesocortical Addiction |
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4 main classes of drugs used in Parkinson's
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Dopamine precursor - levodopa
Dopamine releaser - amantadine MAOb inhibitor - selegiline DA-R antagonists - bromocryptine, ropinirole |
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Apomorphine
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Drug that stimulates emesis
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2 main functions of NE
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Arousal and mood regulation
Modulation of SNS outflow ESP reg of BP |
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Amitryptiline
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TCA
Blocks NE reuptake 1 Enhances synaptic NE tranmission |
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MAOa inhibitors
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Phenylzine
Moclobemide |
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Main functions of Ach in CNS
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Movement control - striatum ( to much Ach causes tremor)
Cognate function - septohippocampal and nucleus basalis |
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Cholinolytics used in early or secondary parkinsonism
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Benzatropine
Trihexyphenidyl |
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CB1 receptor is located in (1)
9 actions |
1- CNS
Euphoria Impairment of memry/ learning Analgesic Anti emetic Influence on vision Decreased fertility Stimulates appetite Inhibits proliferation of cancer cells |
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CB2 receptor is located in (2)
3 functions |
Immune cells
Anti inflammatory Anti allergenic Immunosuppressive |
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Positive symptoms of schizophrenia 3
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Hallucinations- auditory
Delusions Unusual behavior - stereotypes, mannerisms |
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Negative symptoms of schizophrenia 5
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Reduced emotional range
Loss of interest Loss of initiative/ drive Indecisiveness Poverty of speech |
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Cognitive symptoms of schizophrenia 5
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Poor attention
Working memory impairment Formal thought disorder Impaired abstraction Executive function deficits |
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Bleuler's criteria of schizophrenia (4)
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Autism- mental isolation
Flattened affect Loose associations Ambivalence |
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Type 1 schizophrenia
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Patients w/ predominantly positive symptoms
- respond to antipsychotic drugs |
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Type 2 schizophrenia
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Patients w/ predominantly negative symptoms
- poor response to antipsychotic drugs |
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Main biochemical change in schizophrenia
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Excessive dopaminergic activity
- increase in DA receptor density in several brain regions |
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Potency of antipsychotic drugs correlates with blockage of which dopamine receptors?
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D2
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Dopamine hypothesis of schizophrenia
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Excessive dopamine transmission in mesolimbic-mesocortical pathway
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Main mechanism of action of antipsychotic medication? (1)
Which other receptors do they block and effect? (4) |
1 - block of dopamine receptors
1- alpha1 R - vasodilation 2- 5HT2a R - sedative 3- H1 R - sedative, anti emetic 4- M1 R - antimuscarinic symptoms |
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Effects of neuroleptics in normal ppl
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Impair performance
Cause sleepiness w/ restlessness |
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Antipsychotics typically treat which symptoms in pts?
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Positive symptoms
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Effect of antipsychotics on EEG
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Slowing of waves w/ increase in synchronization
-- elevates risk of seizures in epileptics |
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Endocrine effects of neuroleptics
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Increased prolactin secretion
Increased peripheral conversion of androgens to estrogens |
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Cardiovascular effects of neuroleptics
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Orthostatic hypotension
Prolongation of QT interval on ECG |
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Antimuscarinic actions of neuroleptics
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Constipation
Urinary retention Dry mouth |
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Tar dive dyskinesia
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Buccolingualmasticatory syndrome
Permanent movement of lips, tongue, chewing, blinking, trembling of lips and tongue; rarely abnormal mvts of hands and trunk |
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Main side effect of clozapine
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Agranulocytosis - have to monitor WBC count
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Main side effect of thioridazine
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ST segment abnormalities
Arrhythmia Retinal deposits - brown vision |
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Main side effect of chlorpromazine
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Corneal and lens deposit
Cholestatic jaundice |
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Agents used to TX extrapyramidal effects of neuroleptics (2)
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Antimuscarinic agents - benztropine, biperiden. Trihexyphenidyl
Antihistamine diphenhydramine |
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Neuroleptic malignant syndrome
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Muslce rigidity
Fever Leukocytosis Autonomic instability Muslce damage - increased CK levels |
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TX of neuroleptic malignant syndrome
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Physical cooling
Cholinolytics Muscle relaxants Dantrolene Dopamine agonists |
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Typical classical neuroleptic drugs (4)
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Phenothiazines
Thioxantene derivatives Butyrophenone derivatives Dibenzodiazepine derivatives |
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4 main phenothiazines
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Chlorpromazine
Thioridazine Promazine Trifluperazine |
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Chlorpromazine and prometazine are occasionally used for TX of
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Pain/ anxiety in myocardial infarction
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4 main thioxanthene derivatives
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Thiotixene
Chlorprotixene Zuclopenthixol Flupenthixol |
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3 main butyrophenone derivatives
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Haloperidol
Trifluperidol Droperidol |
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Droperidol - main uses (4)
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Anesthesia and internal disease emergencies
Premedictation before surgery - antiemetic and sedative W/ fentanyl in neuroleptic analgesia TX of pulmonary HTN |
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Example of dibenzodiazepine derivative
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Clozapine
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5 main atypical neuroleptics
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Risperidone
Ziprasidone Olanzepine Quetiapine Sertindole |
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Nicotinic agents and schizophrenia
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Possible role for agonists of alpha-7 nicotinic receptor ( bc schizo due to deficit in nAchR function)
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Amine hypothesis of depression
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Depression is associated w/ decreased NE and/ or 5HT synaptic transmission in limbic system structures
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Depression has what effect on receptor density?
Which receptors does it effect? |
Increases receptor density
Affects: Beta adrenergic POST Alpha adrenergic PRE 5HT2a POSt M1 POST |
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What's so special about tianeptin and amineptin?
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Clinically efficiency anti depressant drugs that INCREASE reuptake of serotonin
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Mechanism of action of TCAs
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Mixed serotonin / NE reuptake inhibitors
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Clinical uses of imipramine
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Depression
Bed wetting ADHD Panic attacks |
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Contraindications of TCAs
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Mania
Myocardial infarction Arrhythmia Liver insufficiency |
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Be careful using TCAs with
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Prostatic hypertrophy
Glaucoma Hyperthyreosis Epilepsy |
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Classical MAO inhibitors
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Phenylzine
Tranylcypromine Selegeline |
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Mechanism of action of MAO inhibitors
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Irreversible inhibitors of MAO a which is responsible for NE, serotonin and tyramine metabolism
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Indications for Mao inhibitors
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Rarely used bc of toxicity
Only in atypical depressions |
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Adverse effects of Mao inhibitors (4)
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Cheese reaction
Sleep disturbances Weight gain Poetical hypotension |
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Cheese reaction
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Accumulation of tyramine after eating certain foods I.e. Cheese, red wine, smoked meats
Causes hypertensive crisis bc tyramine causes release of NE from nerve terminals |
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Drug interactions of Mao inhibitors
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TCAs -2 week interval
SSRIs - serotonin syndrome All sympathomimetics drugs |
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Example of reversible inhibitor of Mao
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Moclobemide
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Moclobemide
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Minimal risk of cheese reaction but still affects sleep, weight gain, dizziness, vertigo and interacts with other drugs
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Examples of SSRIs (5)
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Fluoxetine
Paroxetine Sertraline Fluvoxamine Citalopram |
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Indications of SSRIs 5)
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Depression
Neurosis Bulimia Premenstrual syndrome Menopausal hot flashes and mood swings |
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Adverse effects of SSRIs
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Anxiety - rapid onset at beg of TX
Insomnia GI symptoms Tremor Decreased libido and sexual dysfunction |
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Serotonin syndrome
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Hyperthermia
Muscle rigidity Myoclonus Diarrhea Confusion -- potentially fatal interaction w/ TCAs and MAO-I s |
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Amoxapine
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Metabolite of loxapine
Blocks reuptake of NE Weak DA receptor blocker TX: psychotic patients w/ depression |
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VenlafaxIne
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Blocks reuptake of 5HT in low doses
Blocks both serotonin and NE at high doses Lacks antimuscarinic and antihistamine actions |
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Mechanism of action of mianserin / mirtazapine
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Antagonist at presynaptic a2 receptors causing disinhibition of 5Ht and NE relesse
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Adverse effects of mianserin
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Agranulocytosis!!!
Sedation, weight gain, orthoststic hypotension |
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Tianeptin/ amineptin
- action - adverse effects |
Increase reuptake of 5Ht and NE
Headaches, tremor, abdominal pain |
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Bupropion
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Useful in TX of nicotine addiction and some types of depressiom
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Mechanism of action of amphetamine like drugs
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Release catecholamines
Inhibit catecholamines uptake |
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Effects of amphetamine-like drugs
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Locomotion stimulation
Euphoria and excitement Stereotyped behavior Anorexia |
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Amphetamine, methylphenidate and dextroamphetamine used clinically to TX
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ADHD in children
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ADHD can be TX with?
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Amphetamines
Atomexitine Imipramine Clonidine Bupropion |
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Phenmetrazine used to TX (1) but withdrawn due to (2)
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Appetite suppressant
Pulmonary hypertension |
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Cocaine
- mechanism (1) - clinical use (2) - risks (3) |
1 inhibitor of catecholamines uptake
2 local anesthetic in opthalmology and nasal procedures 3 risk of fetal damage |
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Gamma hydroxy butyric acid
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Activates GABA b receptors
Euphoria Amnesia Enhanced sensory perceptions Aka. Date rape drug, liquid ecstacy |
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Respiratory stimulants with weak convulsants actions
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Methylxanthines I.e. Caffiene, theophylline
Doxapram Almitrine * above 2 TX respiratory insufficiency |
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Respiratory stimulants with strong convulsants actions
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Pentylenetetrazol
Amiphenazole |
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Mechanism of action of methyxanthines (3)
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Inhibition of PDE
Antagonism of adenosine A2 receptors Inhibition of histone acetylation in inflammatory cells |
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Clinical use of theophylline
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Bronchodilator
- respiratory stimulant and anti asthmatic drug |
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TX strategy for dementia
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Increase cholinergic transmission
Decrease of excitotoxicity and anti-inflammatory actions |
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Cholinesterase inhibitors used in TX of dementia
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Tacrine
Donepizil Galantamine Rivastigmine |
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Reminyl
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Cholinesterase inhibitor
Also stimulates nAchR in brain to release more Ach |
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Memantine
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NMDA blocker used in TX of Alzheimer's
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Which drug classes induce physical dependence? (6)
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Opiates
Amphetamines Benzodiazepines Barbiturates Alcohol Nicotine |
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Melatonin
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Synthesis stimulated by darkness and regulated by NE
Affects ML1/2 receptors Shortens time to sleep induction |
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Ramelteon
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Shortens time to sleep induction
First pass metabolism BUT metabolite is long lasting |
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Toxicity of melatonin and ramelteon
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Dizziness
Fatigue Fall in testosterone Rise in prolactin |
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Barbiturates
- effects on REM sleep - mechanism of action - example |
Strongly diminishes REM sleep, w/ rebound increase
Increases activity of GABA receptor leads to hyper polarization of neurons Thiopentone |
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Uses of phenobarbital (barbiturate)
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Anti epileptic
Glucoronic transferase deficiency |
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Uses of thiopentone
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Premedication / induction of anesthesia
Neuroprotectiom - coma, cerebral swelling, brain trauma |
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Short acting barbiturates
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Hexobarbital
Thiopentone Methohexylate |
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Intermediat acting barbiturates
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Barbital
Cyclobarbital |
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Long acting barbiturates
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Phenobarbital
Methyl Phenobarbital Diarylobarbital Penthobarbital |
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Main actions of benzos (4)
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Anxiolytic/ hypnotic action
Sedative Anti epileptic Spasmolytic activity |
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Short acting benzodiazepines (6)
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Triazolam
Midazolam Alprazolam Lorazepam Diazepam Temazepam |
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Long acting benzodiazepines (5)
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Nitrazepam
Flunitrazepam Flurazepam Estazolam Chlordiazepoxide |
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Zaleplon
Zopiclone Zolpidem |
Increase GABA s receptor
Less anti epileptic and muscle relaxant effect Less affinity to receptors in spinal cord Ordered in increasing duration |
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Chloralhydrate
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Metabolized to trichloroethanol
Does not affect REM Used as hypnotic, sedative and anti epileptic Used in children |
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Toxicity of chloralhydrate
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Bitter taste and local mucus irritation
Allergic reaction Disorientation Risk of heart sensitization to NE Risk of accumulation in liver/ renal damage |
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Actions of anxiolytics (7)
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Decrease fear and aggression
Decrease mm tonus Anti epileptic Sedative/ hypnotic Autonomic reactions Analgesia w/ increased dose Anti depressant (alprazolam) |
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Side effects of anxiolytics (6)
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CNS depression w/ fatigue
Paradoxical rxn ESP in elderly Muscle relaxation Increased appetite Decreased libido Menstrual cycle disturbance |
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Anxiolytics that affect the 5HT system
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Buspirone
Gepirone Ipsapirone Tandospirone |
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Pain transmitted through A fibers
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Somatic
Sharp and well localized Strong mechanical stimulus |
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Pain transmitted through C fibers
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Visceral
Diffuse and dull Slower conduction - polymodal |
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Actions of opioids (2) specific to analgesia
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Increase pain threshold (spinal cord)
Increase pain tolerance ( limbic system) |
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Overall actions of opioids and receptors (5)
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Analgesia - mu, kappa and delta agonist effect
Sedation - kappa Euphoria - mu Respiratory depression - mu Miosis |
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Endorphins
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From proopiomelanocortin
Secreted during stress Involved in: Analgesia Hormonal regulation Immune rxns |
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Enkephalins
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Perception and conduction of pain
Regulation of Neuromediators and opioid secretion Seizures, motivation , EPS |
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Dynorphins
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Hallucinations
Dysphoria Miosis Antitussive Seizures, EPS |
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Actions of u opioid receptor
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Analgesia
Decrease ventilation Euphoria Dependency |
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Actions of delta receptor
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Dysphoria
Hallucinations Stimulation of vasomotor centre |
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Actions of kappa opioid receptor
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Spinal analgesia
Miosis Sedation Hallucinations |
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CNS actions of opioids (8)
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Analgesia
Respiratory depression Antitussive Miosis Nausea/vomiting Euphoria or dysphoria Sedation Seizures |
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Actions of opioids in periphery (5)
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Constipation
Vasodilation Uriticaria from H release Urinary retention Decreased uterine contractions |
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Uses of opioids (6)
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Analgesia
Pre Medication / anesthesia Pulmonary edema - morphine Delivery - petidine, pentazocine Diarrhea - codeine Antitussive - codeine |
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Contraindications of opioid use (9)
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Children, infants, elderly
Hypothyreosis Cor pulmonale Asthma Head trauma Undiagnosed abdominal or head pain Ppl w/ urinary retention Liver insufficiency Renal damage |
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Codeine
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Often combined w/ NSAIDs
Anittussive action Only for mild/ moderate pain Less addiction potential |
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Levorphanol/ oxycodone
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5-10x stronger than morphine
Greater oral bioavialability Similar addiction potential |
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Dextromethorphan
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Only anti tussive action
No CNS effects No addiction potential |
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Meperidine and pethydine
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Faster onset but shorter action than morphine
No anti tussive action No uterine relaxation - low placental diffusion No miosis Decreased constipation |
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Loperamide
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Only anti- diarrhea agents
Oral admin Very low CNS penetration Low addiction potential Do not use in diarrhea w. / fever |
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Methadone
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Increased oral bioavailabilty
TX of heroin addiction Strong CNS depressant and ventilatory depressant with potential for cardiotoxicity and pulmonary edema |
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Buprenophrine
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Delayed and weaker ventilatory response
Only partially reversed by naloxone Less euphoria Less abuse liability |
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Tramadol
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Less potent
Orally active Low abuse liability Also inhibits 5HT and NE uptake in CNS |
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Pentazocine
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Mixed antagonist/ agonist
Low placental penetration and increases oxytocin levels - good drug for delivery |
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Nalbuphine
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Partial u-R antagonist and k-R agonist
Used parenterally |
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Naloxone
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Inhibition of u-R and k-R
TX of opioid overdose Increases BP in various form of shock Use IV - multiple doses bc short duration of action |
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Naltrexone
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Longer duration of action and more potent than naloxone
Can be used orally |
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Uses of naltrexone
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Overdosing of opioids
Infant apnea Rett syndrome Enhances seizure control of anti epileptics |
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Meptazinol
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Selective u2-R agonist - precipitates withdrawal symptoms
Causes nausea/vomiting |
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Mechanism of action of cocaine as local anesthetic
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Inhibits VG Na+ channels
Decreases membrane activity Decreases AP |
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Four ester local anesthetics
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Cocaine
Procaine Tetracaine Benzocaine |
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Examples of amide local anesthetics
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Lignocaine
Lidocaine Prilocaine Bipuvicaine Levobupivacaine Atricaine |
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Local anesthetic use contraindicated in (4)
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Increased thyroid states
Hypertension O'berst anesthesia Penile anesthesia |
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Use dependent property of local anesthetics
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The more Na+ channels open, the greater the block is
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5 types of anesthesia
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Surface - n.endings of skin/ mucous mbs
Infiltration - subcutaneous n..ending Conductive(regional) - mixed n.trunk SAA - spinal roots Epidural - epidural space |
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Hogine syndrome
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Caused by procaine
Micro thrombosis in lungs and CNS Increased HR / BP , increased ventilation, fear, disorientation and nausea |
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Tetrodotoxin
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Inhibits Na + channels causing weakness, paralysis and respiratory death
Toxin found in liver/ ovaries of puffer fish |
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Saxitoxin
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Marine organism - red tide phenomenon
LA that acts exclusively on outside of mb - independent of whether channel is open or closed |
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General anesthetics cause ... (5)
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Unconsciousness
Analgesia Loss of motor reflexes Amnesia Loss of autonomic reflexes |
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Lipid theory of anesthesia
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Direct action on lipids leads to indirect action on proteins
- affects the: thickness/volume, fluidity, dielectric properties etc of the mb |
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Effects of general anesthetics on CNS (5)
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Decrease synaptic transmission
Decrease postsynaptic action of nt Decrease excitability post synaptic cells Decrease transmitter release Decreasen conduction of AP |
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Main places of action of GA (2)
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Reticular formation - LOC
Hippocampus - short term amnesia |
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Effects of GA on cardiovascular system (4)
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Decrease heart contractility
Decrease SNS = decreased CO and BP Ventricular dysrhythmias Decreased ventilation |
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Stages of anesthesia (4)
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1. Analgesia
- conscious but drowsy, decreased pain 2. Excitement - LOC - reflexes increase (cough, pain) - irregular ventilation 3. Surgical anesthesia - pain decreases - reflexes decrease - diaphragm function decreases 4. Medullary paralysis - no ventilation |
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Inhaled GAs (6)
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N2O
Halothane Enflurane Isoflurane Sevflurane Desflurane |
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IV GAs (5)
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Barbiturates - thiopental
BDZs - diazepam, midazolam, ethomidate Opioids Propofol Ketamine |
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Minimum alveolar concentration
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Conc of inhalational anesthetic required to blunt muscular response to surgical incision in 50% of patients
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Blood:gas partition coefficient
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The lower the solubility in blood, the faster the process of equilibration and thus faster induction and recovery
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Oil:gas partition coefficient
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Related to GA potency
Depends on body fat Responsible for 'hangover' Action closely correlated w/ ventilation and CO |
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N2O
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Adjuvant for other GA - reduces MAC for them
- no hangover - does not produce muscle relaxation - increases CO and BP |
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N2O inhibits which receptors ?
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Glutamate receptors
ESP. NMDA |
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Side effects of N2O (5)
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Nausea/vomiting
Long term exposure = inactivation of vit b12 dep enzyme methionine synthase causing bone marrow depression Mild CNS depression Hypoxia during recovery Accumulation in body cavities |
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Steal phenomenon
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Isoflurane
Causes contraction of coronary vessels in regions of ischemia -> precipitates MI |
