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Showing posts with the label CENTRAL NERVOUS SYSTEM DRUGS

CNS STIMULANT - BASIC NEUROPHARMACOLOGY

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  Methylxanthines Theophylline, Caffeine, Cocaine... MOA  Inhibit PhosphodiEsterase enzymes..Increase cAMP ....Block Adenosine  receptor...Alter intracellular Ca++..Increase Ca++ in Brain..decrease Ca++ in smooth  muscles Actions increased mental alertness. +Ve ionotropic & chronotropic effect on heart.. .. Diuretic action...Stimulate secretions... contraindicated in Peptic ulcer.. T.E in Asthma.... in Headache... S.E  Insomnia.... cardiac arrhythmia... Nicotine  second most abused drug. MOA  cause ganglionic stimulation by depolarization..At high dose blockade of ganglia Actions  Euphoria...arousal...respiratory paralysis...Vasoconstriction....  increaase B.P....Appetite suppressant S.E  Diarrhea, tachycardia, withdrawal characterized by irritability, anxiety, difficulty in  conc. Headache, insomnia... Bupropion used to reduce craving for smoking Varencilline  Partial agonist at neural nicotinic Ach receptor in CNS...used ...

ANAESTHETICS : General Anesthetics | Basic Concepts in Pharmacology

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  Reversible state of CNS depression, resulting in loss of response to & perception of External stimuli. Pre-anaesthetics medicines calm the patient , relieve pain & protected against undesirable effects of anaesthetics or surgical procedure STAGES & DEPTH OF ANAESTHESIA 1) Induction=Period of time from onset of Administration to development of surgical  anaesthesia. Propofol produce induction in 30-40sec...For Childern Halothane or  Sevoflurane induce general anaesthesia 2) Maintenance=Sustained surgical anaesthesia 3) Recovery= Time from discontinuation of anaesthesia until consciousness & protective  physiological reflexes. Depth of Anaesthesia= Four stages ...each stage characterized by CNS depression Stage l-Analgesia= Loss of pain sensation Stage ll-Excitement= Dilirium....increase BP...increase risk of Laryngospasm Stage lll-Surgical Anaesthesia= Loss of muscle tone...decrease CNS reflexes  ...Regular respiration Stage IV-Medullary paralys...

ANTIPSYCHOTIC DRUGS -Typical and Atypical Antipsychotic Drugs

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Called NEUROLEPTICS/MAJOR TANQUILIZER Schizophrenia delusion,hallucination, thinking or speech disturbance First –Generation Antipsychotics/Conventional/typical/Traditional Antipsychotics Competitive inhibitor of various receptor....Block D2 receptor.. Second-Generation Antipsychotics/Atypical Antipsychotics Have less Extra-Pyramidal effects than First-generation...more Efficacious.. MOA block Dopamine receptor in the Brain..Block Serotonin receptor 5-HT in brain.. Refractory Patients= 20% patients do not responds First & Sec generation drugs. .Clozapine effective but have side effect of Bone marrow suppression & CVS side effect Actions Antipsychotic actions; reduce hallucination & delusions with Schizophrenia(+Vesymptoms).... -Ve symptoms; Anhedolia (not getting pleasure from normal stimuli), Apathy, Impaired attention Extra-Pyramidal Effects  Dystonia (Sustained contraction of muscles), Akathisia (motor restlessness), Tardive Dyskinesia(involuntary movement of tongue,...

OPIOIDS - Opiate Education: Key Points for the Pharmacist

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  Pain =unpleasant sensation acute or chronic consequence of neurochemical processin the peripheral and CNS. Opioids are natural or synthetic compounds that prodce Morphine-like effect Opioids Receptors= Protein receptors in CNS ,periphery and GIT..μ(mu), k(kappa), δ(delta) .. Morphine= Prototype, high affinity for μ receptor MOA= inhibit Adenylyl cyclase..increase K+ ion ..hyperpolarization..decrease Ca++influx ..Morphine act at k receptor in spinal cord & decrease Substance P..modulate pain ACTIONS= Analgesic by rising pain threshold in spinal cord & altering pain perception in brain...Euphoria..Respiratory Depression..Depression of Cough reflexes..Miosis(pin point pupil)....Emesis by stimulating CTZ..decrease GIT movement..Dilate CSF so contra in Brain injury..Histamine release..increase Growth hormone.. Prolong Labor T.E= induce Sleep...treatment of Diarrhea...Relief of Cough...treatment of Acute Pulmonary Edema P.K= linear P.K..First pass met..Morphine-6-Glucuronide p...

ANXIOLYTIC & HYPNOTIC DRUGS - BENZODIAZEPENS, BENZODIAZEPENS ANTAGONIST, OTHER ANXIOLYTIC, BARBITURATE, ZOLPIDEM, DRUGS TO TREAT ETHANOL POISONING

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  Anxiety: unpleasant state of tension, apprehension, uneasiness, Classification  Benzodiazepens Bezodiazepene=composed of α , β , γ..BZD binds to GABA receptor at specific site located at the interface of α & γ2 subunit...influx of Cl- ions...hyperpolarization... Θ action potential Two BZD receptors BZ1 & BZ2 Actions  reduction of anxiety....sedation...Anticonvulsant....Muscle relaxant. .Anterograde Amnesia.. T.E  used in GAD(Generalized Anxiety Disorder),  PTSD (Post Traumatic Stress Disorder),  OCD(Obsessive Compulsive Disorder),  Phobia, Social Anxiety,  for Panic disorder Alprazolam is effective In Muscular Disorder Diazepam used.  Midazolam induce Anaesthesia Diazepam & Lorazepam DOC in Grand-Mal Epileptic disorder.. Clonazepam in Seizure Flurazepam (85hr t1/2) , Temazepam used in REM(Rapid Eye Movement) Triazolam used in induction of sleep S.E  drowsiness & confusion, Ataxia, weight gain, sexual dysfunction Contrai...

ANTI-DEPRESSENTS

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 Depression : intense feeling of sadness, hopelessness, despair symptoms that shows you are depressed SELECTIVE SEROTONIN REUPTAKE INHIBITORS MOA: inhibit serotonin reuptake...have little ability to block Dopamine Actions:  Citalopram & Fuloxetine are Racemic mixture..Escitalopram is S-enantiomer of Citalopram...Fuloxetine has 50hr t1/2. T.E:  treat Depression, Bulimia Nervosa, GAD, PTSD S.E: Sexual dysfunction, Suicidal ideation in Adults...Sleep disturbance.. Serotonin syndrome: Hyperthermia, muscle rigidity, Myoclonus muscle on withdrawl SEROTONIN/NOREPINEPHRINE REUPTAKE INHIBITOR Inhibit reuptake of both Serotonin & NorEpinephrine Venlafaxine & Desvenlafaxine= Desvenlafaxine is metabolite of Venlafaxine.. Duloxetine=Contraindicated in kidney impair.. T.E: used in Depression, Backache, MuscleAche, Diabetic peripheral neuropathy ATYPICAL ANTIDEPRESSENTS Mixed group of agents have action at different sites Bupropion : weak dopamine & norepinephrine reupt...

NEURODEGENRATIVE DISEASES - ANTI-PARKINSON DRUGS, ALZHEIMER DISEASE,MULTIPLE SCLEROSIS, AMYOTROPHIC LATERAL SCLEROSIS

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ALSO WATCH PRECISE VIDEOS OF ANTIMICROBIAL Parkinsonism Neurological disorder of muscle movement, characterized by Tremor, Muscular rigidity, Bradykinesia(slowness ininitiating & carrying voluntary  movement) , Postural and gait abnormalities. Etiology: imbalance b/w Substantia nigra & Neostriatum...Loss of DOPAMINE results in increased production of Ach in NEOSTRIATUM & decrease Inhibitory effect of DOPAMINE(produce in SUBSTANTIA NIGRA) on Ach... Levodopa  metabolic precursor of DOPAMINE...only provide Symptomatic relief MOA Dopamine does not cross B.B.B..Levodopa actively transported into CNS .converted into Dopamine in Brain... Carbidopa  DOPA decarboxylase inhibitor...Θ metabolism of Levodopa in GIT & Peripheral tissue...increasing availability of DOPA in brain T.E  2/3rd of Patient in Parkinson disase reduce severity of disease.. P.K levodopa 1-2 hr t1/2..ingestion of high protein(Amino ACIDS) may interfere in the transport of Levodopa...should b...