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Setyawati S Karyono
-atypical
Antipsychotic conventional
1.Phenothiazine
(Phenothiazine, Haloperidol)
Pharmacological Effects
Behavioral quieting of agitated Px, hallucinations , sedation, spontaneous activity cataleptic state (in high doses)
Seizure threshold precipitate epilepsi Ekstrapyramidal effects
Antiemetic effect Autonomic effects (-blocker, anticholinergic) Antihistaminic, antiserotonergic CVS qunidin-like effect Endocrine prolactin , gynecomastia, menstruation disturbances & ovulation
Side Effects
CNS drowsiness,parkinsonism etc Autonomics Endocrine Hypersensitivity allergy rash, photosensitivity, agranulocyitosis Toxic retinopathy BW gain Neuroleptic malignant syndrome (fever, musc. rigidity, stupor, respiratory & autonomic dysfungtion, leukocytosis) stop drug, supportive therapy, bromocriptine
Drug Interaction
Potentiation of CNS depressant & opioids Inhibition alcohol metab., phenitoin Effectiveness of levodopa in therapy parkinson
Additive anticholinergic & -blocker With antiarrythmia drug
2.Haloperidol
Mechanism and effect similar to the phenothiazines, but prefered in certain type of disorders Anticholinergic effect (-) Autonomic effect << hypotensive (+)
Atypical Antipsychotic
Receptor binding Antipsychotic D1 D2 5-HT2 -1 khol hist Clozapine ++ + +++ +++ +++ ++ Olanzepine ++ ++ +++ ++ +++ ++ Ouetiapine (+) + + ++ ++ Risperidone +++ +++ +++ Sertindole + +++ ++ Ziprasidone + +++ +++ ++
Haloperidol
Fluphenazine
4
4
1
1
4
3
4
4
Thiothixene
Trifluoperazine Perphenazine Molindone Loxapine Chlorpromazine
3
3 3 4 3 1
2
2 2 3 3 3
3
3 3 4 3 2
4
4 4 4 3 1
Thioridazine Clozapine
Risperidone
1 1
4
4 4
4
1 1
4
1 1
3
ANTIDEPRESSANT
Dysthymia
Persistent (2 + years) of: -depressed mood -poor appetite/ overeating -insomnia/hypersomnia -low energy, fatigue -poor self esteem -poor concentration -hopelessness
Mixed Disorder
Bipolar Disorder
Intermittent bouts of depression with mania or hypomania Depressive Phase: Varying degrees of depressed mood Mania Phase:
Inflated Self Esteem, decreased need for sleep, very talkative, flight of ideas, distractible, psychomotor agitation, excessive preoccupation with pleasurable activities
TREATMENT ANTIDEPRESSANT
Unipolar Depression/ Dysthymia
1.MAO Inhibitors monoamine (NE, dopamine) in synaps , improve mood response after several weeks
Side effects CVS, BW , intoxication brain, hepar Drug Interaction potentiation with sympatetic drug, tyramine, others antidepressant, inhibits drug metbolism Tranylcypromine- irreversible inhibitor of MAO-A,B uncommon use
2.Tricyclic Antidepressants:
(2nd Generation)
Inhibition uptake NE, 5-HT, DA Sedationantihistamine Anticholinergic effect CVS palpitation, tachycardi, arrythmia, hypotension down regulation 5-HT1A, D, & -2 receptors time delay in therapeutic action Metabolism : Imipramine Desipramine Amitriptylene Nortriptylene Parent Drug Active Metabolite
Tricyclic Antidepressants
Drug Interactions
Inhibition of P-450 Enzymes Reduction of Antihypertensive Actions Reduction of Seizure Threshold Additive Sedative Effects with Alcohol and other Depressants Enhancement of Anticholinergics
Tricyclic Antidepressants
Toxicity/Overdose
Narrow therapeutic window Restrict Rx amount Overdose may result in: Hypotension, shock, renal failure Grand mal seizures Hyperpyrexia Conduction disturbancesArrhythmias
Misc. Antidepressants
HeterocyclicsAmoxipine- nonselective Maprotiline- NE selective Trazodone-5-HT selective atypical , sedating no antichol. actions Buproprion- DA selective smoking cessation, ADHD
Tx Bipolar Disorder
Valproate (anticonvulsant) Carbamazepine (anticonvulsant)
Haloperidol (antipyschotic)