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23 Cards in this Set
- Front
- Back
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What drugs are classified as thioxanthenes?
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Flupenthixol ,Flupenthixol decanoate
Zuclopenthixol ,Zuclopenthixol decanoate Chlorprothixene Thiothixene |
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What drugs are considered to be Butyrophenones?
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Haloperidol - prototype
Droperidol |
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What drug's a Dibenzoxazepine?
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Loxapine
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What drugs are apart of the Phenethiazines ?
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Chlorpromazine - prototype
Trifluoperazine Thioridazine Fluphenazine Perphenazine |
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Name the atypical antipsychotics
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Clozapine- prototype
Risperidone Quetiapine Aripiprazole Olanzapine Ziprasidone Sulpiride Sertindole Paliperidone Asenapin |
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What are the main tracks of the Dopamine system ?
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Mesolimbic
Mesocortical Nigrostiatal Tuberoinfundibular |
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what tract is blocked by all antipsychotic drugs?
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Meso imbic
* blockade of remaining dopamine tracts causes adverse effects rather than therapeutic benefit This is major point of distinction between antipsychotics |
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What causes negative symptoms of schizophrenia ?
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Dopamine HYPO FUNCTIONING
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What 'a tie difference between typical and atypical antipsychotics?
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Typical antipsychotics affect all 4 dopamine tracts w varying degrees of potency. In contrast atypical antipsychotics primarily affect dopamine tracts in limbic system & are limbic specific
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What are The clinical uses of chloropromazine
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Schizophrenia - ↓ hyperactivity , ↓hallucinations, ↓ delusions
Mania Schizoaffective disorders Tourette’s syndrome Antiemetic Antipruritic for intractable itching (due → H 1 blockade) |
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What are the adverse effects of Chlorpromazine?
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Cholinergic blockade → dry mouth, constipation, urinary retention, blurred vision
α adrenergic blockade → postural hypotension Histamine blockade → sedation Epileptogenic Dopamine blockade (nigrostriatal) → Extrapyramidal dysfunction : Parkinsonism, akathisia, dystonia , tardive dyskinesia (perioral tremor, choreoathetosis ) , neuroleptic malignant syndrome : hyperpyrexia, catatonia, rigidity Dopamine blockade ( tuberoinfundibular ) → ↑ prolactin → amenorrhoea, galactorrhoea , infertility |
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How is chlorpromazine metabolised?
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Hepatic metabolism
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What are 1k benefits of Haloperidol ?
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High potency dopamine blocker
Exhibits minimal cross reactivity @ other receptors ( compare w chlorpromazine ) |
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What are the clinical boy Haloperidol?
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Schizophrenia - ↓ hyperactivity ,↓ hallucinations ↓ delusions
Mania Schizoaffective disorders Tourette’s syndrome |
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what are the adverse effects of Haloperidol?
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Relatively free of cholinergic , α adrenergic , histamine blocking side effects caused by dopamine blockade
Dopamine blockade ( nigrostriatal ) → Extrapyramidal dysfunction : Parkinsonism , akathisia , dystonia , tardive dyskinesia ( perioral tremor, choreoathetosis ) neuroleptic malignant syndrome : hyperpyrexia, catatonia, rigidity Dopamine blockade ( tuberoinfundibular ) → ↑ prolactin → amenorrhoea, galactorrhoea , infertility |
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What is the mechanism of the atypical antipsychotics?
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Low affinity for D2 receptors
antagonist action at 5 HT 2 receptor or antagonist action at both 5 HT 2 & D2 receptors critical for antipsychotic action of ATA Hypothesis suggests that selective D4 receptor antagonism or a combination of D2 & D4 antagonism is critical to the MOA of the ATA (quetiapine is not a D4 receptor antagonist so this cannot account for MOA of all ATA) |
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What is clozapine effective in treating and what are its adverse effects?
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Potent blockade of 5 HT 2 receptors along w dopamine blockade and hence is effective in treating negative symptoms of schizophrenia
ADR- Most Frequent: Constipation, Dizziness, Drowsiness, Fever, Headache , Nausea, Orthostatic hypotension, Sialorrhea, Tachyarrhythmia, Vomiting, Weight Gain Less frequent agranulocytosis, seizures |
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What lgpy symptoms are Risperidone effective in treating and what are the adverse effects
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Effective for both positive & negative symptoms Prolong QT interval – used w caution in patients w abnormal QT intervals
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What drugs are used to treat Parkinsonism and Akathisia ?
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Anticholinergic:
Benztropine Trihexyphenidyl Diphenhydramine Procyclidine Biperiden Dopaminergic: Amantadine Gabaminergic: Diazepam Clonazepam Lorazepam Noradrenergic blockers: Propranolol |
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What drugs are used to treat bipolar affective disorder?
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Lithium
Valproic acid Carbamazepine Oxcarbazepine Lamotrigine Gabapentin Topiramate Anti-psychotics: Olanzapine Aripriprazole Chloropromazine Quetiapine Risperidone Ziprasidone |
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What is the MOA of lithium?
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Not clearly understood. Inhibits recycling of neuronal membrane phosphoinositides involved in generation of 2 nd messengers in both α adrenergic receptors & muscarinic neurotransmission blunting hyperactive neurotransmission using these pathways
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How is lithium metabolised and what are its interactions?
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Well absorbed orally
Metabolism: Renal excretion Half life 20 – 24 hrs Teratogen Interactions: Thiazides & NSAIDS interfere w renal clearance → ↑ serum lithium level Antipsychotics ↑ EPSE (extra pyramidal symptoms) |
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What are the ADR of lithium?
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Tremor
Hyperactivity Seizures @ toxic levels- confusion Mild ↓ thyroid function (monitor for lithium induced hypothyroidism) Weight gain Vomiting Abdominal cramps Diarrhoea Reversible nephrogenic diabetes insipidus ( blocks effect of ADH on kidney ) Leukocytosis |
