Local Anesthetics

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NSAIDs: Salicylates: aspirin, sodium salicylate. Paraaminofenol Derivatives: Acetaminophen. Pyrazolones and pirazolindionas: Dipyrone, phenylbutazone. Ac derivatives. Acetic: indomethacin, diclofenac, ketorolac, etodolac, tolmetin, sulindac. Der. Propionic Ac: Ibuprofen, naproxen, ketoprofen, flurbiprofen. Oxicams: Piroxicam. Ders, antralílicos: mefenamic acid, flufenamic, Meclofenamic. Alcañón: Nabumetone. Ders. Sulfonic (coxibs): Celecoxib Etoricoxib. MECHANISM OF ACTION: Inhibits the enzyme cyclooxygenase, thus inhibiting the biosynthesis of PG in cells undergoing inflammation. Isoenzinas There are two COX: COX1: constitutive enzyme. Cox2: inducible enzyme. SELECTIVITY FOR COX: Relatively selective COX 1: AAS. Less selective for COX1: Ibuprofen and paracetamol. Preference for Cox-2: Naproxen, diclofenac and piroxicam. Cox2 inhibition exclusive: coxibs. AC. Pharmacodynamic: Analgesic: pain less intense and moderate. Less opioid analgesics but without the ram. ANTI-INFLAMMATORY: All except paracetamol. ANTIPYRETICS. EI: GI: gastrodudenales ulcers, bleeding and perforation risk of GI mucosa. A renal level: Insuf. acute renal edema by H20 retention, increased reabsorption of Cl, and the action of ADH, analgesic nephropathy. Salicylates: ASS q anaslgesico sodium salicylate. DTerapeútica: T ª elevated body decrease, increase O2 consumption and metabolic rate. DToxica: increase the T th body, profuse sweating and risk of dehydration. DTerapeuticas high: stimulate the respiratory center to increase ventilation, PCO2 and decrease favoring the presence of respiratory alkalosis. As compensation increases renal elimination of HCO3. If sustained DA, stimulation of the respiratory center is followed by depression, therefore it prevents the removal of CO2 and acidosis box appears mixed. A sample DB ASA antiplatelet activity, this activity is indicated for the prevention of thrombosis. A DA has a beneficial effect on rheumatic and inflammatory processes by two mechanisms: inhibition of PG synthesis, suppression of Ag-Ab reactions and modification of connective tissue metabolism. THERAPEUTIC USES: Antipyretic, Analgesic, acute rheumatic fever, rheumatoid arthritis, prophylaxis diseases that present with increased platelet aggregation. EI: GI: nausea and vomiting. GI bleeding. Reye Syndrome (children with chickenpox). POISONING: In chronic mild box appears: Salicas (tinnitus, diarrhea, mental confusion, headache). In severe acute CNS is affected, moving from excitement to a central depression, high fever, and altered acid-base balance and electrolytes. TTO OF POISONING:Gastric lavage, activated charcoal Admin for drug adsorption. Correct hyperthermia, acid-base and electrolyte solutions with appropriate IV. Tto symptomatic hypoglycemia, bleeding and vomiting. Not be used barbiturates or opiates to treat hyperventilation risk of respiratory acidosis and coma. PARACETAMOL: Alternative to the ASA. Good tolerance and bioavailability. No anti-inflammatory. Nephrotoxic: if it causes an acute severe attack can be deadly. RAM: hepatic necrosis dose dependent (fixes Flumil), methemoglobinemia, thrombocytopenia, hypoglycemic coma and renal tubular necrosis. THERAPEUTIC USES: Analgesic-antipyretic. Substitute if ASA contraindicated. Phenylbutazone: Anti-inflammatory ttos q in limited long x its high toxicity. It penetrates very well in healthy joints / swollen. RAM: GI intolerance, bleeding, rash, edema, aplastic anemia and agranulocytosis. Responsible for many deaths, limited as an antiinflammatory in: Phases acute gout exacerbation of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis



ANTIDEPRESSANT DRUGS: MECHANISM ACTION: NA reuptake inhibition, serotonin and dopamine. After exercising his 95% share of the amines are Recaptive in the presynaptic neuron, and 5% will be metabolized by the enzyme MAO (monoamine oxidase). Metabolites are active and that the antidepressant efficacy = original fco. ANTIDEPRESSANT CLASSIFICATION: Antidrepresivos antidepressants: Imipramine, Amitriptyline, Nortriptyline, Desipramine, Doxepin. Mec. Action: They block the reuptake of NA, 5-HT and DA. Pharmacological actions: improve mood, promote sleep and improve appetite. Indications: depression, bedwetting, Sindre. the hyperactive child and agoraphobia. RAM: Dry mouth, blurred vision, drowsiness, tachycardia, urinary retention, confusion, delusions, decreased libido. Interactions: potentiate the effects of alcohol, sedative, antiparkinsonian and antipsychotic drugs. SSRIs (Selective Inhibitors Serotonin reuptake): Paroxetine, Sertraline, Citalopram, Fluoxetine: A selective inhibitor of serotonin reuptake and is indicated for depression, obsessive compulsive disorder, panic disorder and bulimia nervosa. Contraindicated with MAOIs as they lead to increased serotonin, which can lead to serotonin syndrome. RAM: Same as tricyclic antidepressants. MAO inhibitors: Tranylcypromine, Phenelzine. Mec. Action: increase the levels of NA and 5-HT by inhibiting its metabolism. RAM: Headaches, ostostática hypotension, weight gain, decreased libido.
Antipsychotics or neuroleptics: They produce sedation and relaxation, tto Effective in acute and chronic psychosis, fear and aggression disappears, Dan extrapyramidal reactions, not physical or psychic dependence. RANKING: Phenothiazines: Chlorpromazine: Poco powerful. Thioridazine: Something more potent with fewer extrapyramidal effects . Perphenazine: It's more powerful, with more extrapyramidal side effects and less sedative. Actions: Sedation, reacting to external stimuli decreases, decrease emotional displays, agitation and aggression disappears
Indications: Schizophrenia, opiate withdrawal syndrome and alcoholic psychosis. RAM: sedation, dry mouth, blurred vision, orthostatic hypotension, neuroleptic malignant syndrome and gynecomastia. Butyrophenones: Haloperidol: Indicated in the psychoses. Droperidol: used in neuroleptanalgesia. Pimozide Good antipsychotic with few side effects. ttos chronic and prolonged action. lithium salts: Suitable manic-depressive psychosis. RAM: GI, trembling hands, memory loss, reactions. CUTA. Poisoning: lethargy, disorientation, convulsions and coma.
ANXIOLYTICS: FCOS that relieve anxiety or selectively removed without causing sedation or sleep. BENZODIAZEPINES. RATED LONG (> 30h): Diazepam, Clorazepate, flurazepam, clobazam, chlordiazepoxide, Quacepam. INTERMEDIATE (25-30h): Bromazepam, flunitrazepam, nitrazepam, Ketazolam. SHORT (6-24h): Alprazolam, Lorazepam, Lormetacepam, Oxazepam, Clotiazepam, Temazepam. Ultrashort (<6h) and Midazolam Triazolam. BENZODIAZEPINE ANALOGUES A: Zopiclone, Zolpidem And Zaleplom. PHARMACOLOGICAL ACTIONS: anxiolysis, anticonvulsant, antiepileptic, hypnotic, muscle relaxant and mild central antiarrhythmic action. MECHANISM OF ACTION: Facilitate the action of the neurotransmitter GABA by binding to a GABA receptor subunit that is associated a Cl channel, causing the entry of Cl into the cell is in a state being refractory to stimuli. GABA receptors act on central and peripheral. EI: Tolerance, Dependence: Physics (4 weeks) and mental (4 months). CLINICAL USES: Anxiety, alcohol addiction, epilepsy, muscle spasms and dystonia.

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