Biological Therapies. SSRIs Fluoxetine Fluvoxamine Paroxetine Citalopram Sertraline escitalopram.
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Transcript of Biological Therapies. SSRIs Fluoxetine Fluvoxamine Paroxetine Citalopram Sertraline escitalopram.
SSRIs
Share no molecular featuresHalf life:20 hours&3daysHepatic metabolismSpecific activity in the inhibition of serotonin
reuptakeNo activity on other receptorsOccurring 90% of clinical response at the
starting dose
SSRIsTherapeutic Indications
DepressionAnxiety dis.Eating dis.PMSPremature
ejaculation
ParaphiliasADHDAutistic dis.chronic pain
syndromes.Psychosomatic
conditions
SSRIs Adverse Effects
Sexual dysfunctionGI effectsHeadacheCNS effectsAntichoinergic effectsHematologic effectsElectrolyte and glucose disturbancesEndocrine and allergic reactions
Serotonin syndrome
HyperthermiashiveringDiarrheaAgitationHyperreflexia
MyoclonusSeizuresRigidityDeliriumcoma
TCAs
Tertiary amines:
Imipramine
Amitriptyline
Trimipramine
Doxepine
Clomipramine
Secondary amines:
Desipramine
Nortriptyline
ProtriptylineTetracyclic drugs:
Maprotiline
Amoxapine
TCAs:
Half life :10-70h(longer HL in Nortriptyline,Maprotiline)
Hepatic metabolismBlocking of reuptake of serotonin and NEAntagonism of muscarinic,H1,alfa1,2Type A antiarrhytmic effects40-fold difference in plasma concentrations in
different persons
TCAsAdverse Effects
Psychiatric effectsAnticholinergic effectsSedationAutonomic effectsCardiac effectsNeurological effectsAllergic and hematological effectsWeight gain
TCAsDrug – Drug Interactions
AntihypertensivesAntipsychoticsCNS depressantsSympathomimeticsOCPsSSRIsLithiumPrimidonAscorbic Acid
MAOIsTherapeutic Indications
Panic disorder with agoraphobiaSocial phobiaPTSDAtypical depressionEating dis.Pain dis.
MAOIsAdverse Reactions
Or HTNInsomniaWeight gainEdemaSexual dysfunctionHypertensive crisisparesthesia.,myoclonus,muscle pain
drugs to be avoided
AntiasthmaticsAntihypertensivesBuspironeLevodopaOpioidsSympathomimeticsSSRIsClomipramine
Mood Stabilizers
LithiumSodium ValproateCarbamazepineLamotrigineTopiramateGabapentinCalcium Channel Inhibitors
lithium
No binding to plasma proteinsNo metabolismSlow crossing BBBHalf- life : 20 hoursDecreasing of renal clearance in renal
insufficiency and puerperium / increasing during pregnancy
Lithiumtherapeutic indications
Bipolar mood disorderSchizophrenia/schizoaffective disordersMDDAggressionPMSBulimiaBinge drinkingBPDOCDPTSDTrichotilomania
Lithiummaintenance treatment
After the second episode of BMD1 After the first episode in :
1. Adolescents
2. High suicide risk
3. Poor support systems
4. No percipitating factors
5. Sudden onset
6. First episode of mania
7. FH of BMD1
LITHIUMAdverse effects
Gastrointestinal effectsNeurological effectsRenal effectsCardiac effectsThyroid effectsDermatological effects
Lithium toxicityCoarse tremorDysarthriaAtaxiaGI symptomsCardiovascular changesRenal dysfunctionFasciculationsMyoclonusSeizurescoma
LITHIUMDrug interactions
DAsAnticonvulsantsThiazidsPotassium sparing
diureticsNSAIDsACEIsCalcium channel
inhibitors
Osmotic diureticsLoop diureticsXantinsCarbonic anhydrase
inhibitors
LithiumClinical Guidelines
Initial medical work upDosageSerum concentrationsDiscontinuationPatient education
Sodium valproate
Effects on GABA neurotransmitter system.Therapeutically effective at serum
concentrations above 50 -100 microgr/mlHalf-life : 8-17 hoursMaintaining effective plasma concentrations
with dosing 1 to 4 times a day
Sodium ValproateTherapeutic Indications
Bipolar 1Disorder (acute – prophylaxis )Schizoaffective DisorderBehavioral dyscontrol syndromesDementiaOrganic brain diseasesTBIOther mental disorders
Sodium Valproate Adverse Reactions
GI effectsSedationAtaxiaDysarthriaTremorWeight gainHair loss
Elevation of liver transaminases
ThrombocytopeniaPlatelet dysfunctionHyponatremiaHepatotoxicityPancratitisPCO
Sodium ValproateDrug interactions
Lithium CarbamazepinAntidepressantsSDAsDAsPhenytoinPhenobarbitalBZDs
Sodium ValproateAdministration
R/O liver and pancreatic diseaseDose on the first day : 250 mgplasma concentrations : 50-100 mg/mlDaily dose : 1200-1500mgMood-stabilizing effects appear between 5-15
days after initiation
Carbamazepine
Steady-state levels in 2-4 days on a steady dosage
Half-life : 12-17 h after 1 month of administration
Metabolized in liverdecreasing synoptic transmission Reduction of currents through NMDA
channelsAntagonism of adenosine A1 receptors
Carbamazepine Therapeutic Indications
Bipolar disorder (manic-depressive episodes)Schizophrenia and schizoaffective disorderImpulse-control dis.PTSDAlcohol and BZD withdrawal
CarbamazepineAdverse Reactions
Blood DyscrasiasHepatitisExfoliative dermatitisGI EffectsCNS EffectsCardiac EffectsHyponatremia
CarbamazepineDrug Interactions
SSRIsAnti psychoticsCimetidineErythromycinIsoniazideKetoconazoleVerapamilallopurinol
OCPTCAsNa-valproateBupropionMAOIsClomipraminePrimidonePhenytoin
CarbamazepineTreatment
CBC,LFT,ECG,Serum ElectrolytesInitiate with 200mg to 600-1200mgAnticonvulsant Blood Concentration : 4-
12microgr/mlLaboratory
Monitoring :CBC ,Billirubin,LFT,CBZ Level