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ANTIPSYCHOTICS (AP): Comparison Chart B Jensen BSP © www.RxFiles.ca Nov 2018 Name: Generic/TRADE GROUP Clinical ADVERSE EVENTS -AE (%) ANTI- DOSE: INITIAL/d; USUAL DOSE $ (& receptor activity) g =generic Equivalency-mg Anticholinergic Sedation Hypotension EPS EMETIC MAX/d; Elderly Dosing RANGE /Month ChlorproMAZINE LARGACTIL, g Pregnancy 25-75mg; 1000mg po 100mg po BID 12 (25 ,50 ,100 mg tab)(liquid made by some pharmacies) 100 >30 >30 >30 >10 category Aliphatic 50mg/2ml amp: D/C 2016) D2, 1, 5-HT2A Intractable: may help P L 1200mg Retinal pigmentosa 200mg po BID 14 Cholestatic jaundice <1%, Weight gain ~3-5kg, Seizures <1%, Photosensitivity <3%. Hiccups ; schizo ≥6mos ++++ Methotrimeprazine NOZINAN, g Phenothiazine 70 >30 >30 >30 >10 Mild: 5-25mg; 25mg po BID 28 (2, 5, 25, 50mg tab) + P L 1000mg po 50mg po BID 37 ⌂ (5mg/ml soln, 25mg/ml amp) H1,5HT2A Periciazine(Pericyazine) NEULEPTIL 15 >30 >30 >10 >2 ++++ 5-20mg AM + 5mg po AM + 42 (5,10,20mg cap; 10mg/ml liquid) D2 Phenothiazine 10-40mg PM po 10mg po PM FluPHENAzine MODECATE,MODITEN, g 5 >2 >2 >2 >30 + 2.5-10mg; 20mg po 1-5mg po daily 17-23 (DEPOT with preservative 125mg/5ml Vial & 15mg IM P L 2.5-12.5mg; 100mg 12.5-50mg IM/SC 35 /5ml vial 100mg/1ml amp; 1, 2 , 5mg tab) D2, 5-HT2A, 5-HT7 q4week IM/SC q2-3w q2-4w ~20mg/dCATIE Perphenazine TRILAFON, g Piperazine 4-16mg; 64mg po 8mg po BID 17 8 >10 >10 >10 >10 ++++ (2,4,8,16mg tab); (5mg/ml amp ) D2, 5-HT2A, H1 P L Trifluoperazine STELAZINE, g 6 >2 >2 >10 >30 ++++ 4-10mg; 40mg po 5mg po TID 34 P L (1,2,5,10, 20 mg tab; 10mg/ml soln) D2, 5-HT2A 10mg BID 29 Flupentixol FLUANXOL 10 >10 >2 >2 >30 ++ 3mg; 12mg po 3mg po BID 47 (DEPOT 20mg/1ml amp, 100mg/1ml amp; P L 0.5,3mg tab) D2, 5-HT2A 24mg IM q4week 5-20mg;100mg IM q2-3w 20-40mg IM q2-3w 27-42 Zuclopenthixol CLOPIXOL Thioxanthene 50 >10 >30 >2 >30 ++ 10-50mg; 100mg po 10mg po BID 36 (10,25mg tabs), D1-2, 5HT2A, 1 120mg IM q4week (LESS with 100-200mg IM q2w; 150-300mg IM 28-44 P L Acuphase (50mg/1 ml amp)DEPOT200mg/1 ml amp) DEPOT) 400mg q2-3w Not Interchangable Dibenzodiazepine P L CloZAPine CLOZARIL, g 50 6.25-25mg (25-50mg/d) 100mg po TID 268 {patients must register with specific monitoring program!} >30 >30 >30 >2 + Tx: Atropine eye drop/Atrovent nasal spray nocturnal 1% Max: 200mg po BID (25 , 50 , 100 , 200 mg tab) AE:Dizzy,constipation, N/V,HA, fever, nightmares,sweat,HR,BP,salivation , enuresis , seizure(5%-dose related),agranulocytosis CBC qweek(q24week if stable), weight ,ECG 's, 347 D1-5,5HT1&2,7 1-2,H1,M1-5 37% >10% hypomotility 1A2,3A4,2D6,2C19 level level cardiomyopathy; ALT , diabetes, lipids, akathisia , GI . DI: clozapine : CBZ (& neutropenia) & smoking; Cipro, fluvoxamine, caffeine & eryc clozapine ; benzodiazepines -rare resp. arrest. prolactin effect. Level: 1050 - 1650 nmol / L 900mg FDA: suicide risk in schizophrenics Haloperidol HALDOL, g 2 - 6 1.5-3mg; 100mg po 2mg po BID 28 >2 >2 >2 >30 +++ (0.5 ,1 ,2 ,5 ,10 mg tab; 2mg/ml soln ; 40mg IM q4week or Butyrophenone (LESS with with preservative 10-15x po daily dose. P L 50mg; 450mg IM q4w 5mg po BID 42 DEPOT 250mg/5ml, 500mg/5ml Vial, DEPOT) 100mg/1ml Amp ; 5mg/ml amp) D2>D1 QT interval esp. with IV dosing, May mortality, ALT 16%, Weight gain 1 kg; schizo/Tourette’s >3yrs approved 0.25-2mg/d 50-200mg IMq2-4w 57-87 Loxapine LOXAPAC IM, XYLAC Dibenzoxapine 10-20mg; 250mg po 10mg po BID 31 (5,10,25,50 mg tab); (2.5mg tab) 15 >10 >30 >10 10-30 + D/C Weight gain minimal P L (25mg/ml soln ; 50mg/ml amp ) D2, 5HT2A -inhaled powder ADASUVE 25mg po BID 42 USA OLANZapine ZYPREXA, g Reg + Zydis, g Thienobenzodiazepine 5-10mg; 20mg po 10mg daily 33 2.5 - 5 >10 >30 >2 >2 + $ CATIE (2.5,5,7.5,10,15mg tab) (ZYDIS 5,10,15mg tab )(20mg ) P L AE:somnolence, dry mouth, dizzy, headache, asthenia, constipation, nightmares, blurred vision, urinary incontinence, dyspepsia, ALT 6%, diabetes, weight , BP, 2.5-5mg/d 15-20mg po daily 54-75 ; , , , , & ( ) >10% postural 0.9% DRESS 1A2,2D6,P-gp smoking by fluvoxamine FDA FDA 10mg IM D1-4 5HT2A,C 1 H1 M1-3 5 approved 1996 akathisia , hypotension , Sz’s , ?stroke/death, triglycerides/cholesterol; skin . DI: olanzapine by: ; ; prolactin BPAD 1: acute tx of manic & mixed episodes13yr ; Schizophrenia Age 13yr AE: esp weight,TG,diabetes Pimozide ORAP, g Diphenylbutyl 2-4mg; 20mg po 6mg po daily 45 2 >2 >10 >2 >30 + 2D6 P L (2,4mg tab) D2, 5-HT7 piperidine QTc with >8mg/d or DI: azole antifungals, diltiazem, fluvoxamine, macrolides, sertraline, paroxetine, PI’sHIV& verapamil. FDA: for kids >12yr QUEtiapine SEROQUEL, g DI: 3A4 Dibenzothiazepine + 50mg; 800mg po 200mg po TID 35 (25, 50, 100, 200, 300mg tab),(150mg ); 60 - 75 10-30 >10-30 >10 >2 P L ~540mg/d CATIE 600mg hs 35 12.5-200mg/d (XR g: 50,150,200,300,400mg) AE : somnolence , dizzy, drowsy, nightmares, constipation, dry mouth, lens changes beagles-annual slit lamp exam, BP, wt, seizures 0.8%, dyspepsia, headache, abuse, urinary, DRESS, BPAD: acute tx of manic, depressive & mixed 10yr FDA 300mg po BID 35 D1-2, 5HT1A&2A,1,H1 (avail. 1997) failure n=3 17% 11% 0.4% effect incontinence, diabetes,ALT 9% ,akathisia >2%,?stroke/death,triglyceride ,cholesterol ,hypothyroidism ,?pancreatitis/platelet, low EPS , prolactin effect Schizo: 13yr FDA ; 600-800mg XR od $75 g - $98 g ODT=$44 RisperiDONE RISPERDAL, g Benzisoxazole + P L 1-2mg; 8mg po 1mg po BID 25 2 >2 >2-10 >10-30 >10 CATIE ODT=$77 0.25-2mg/d 2mg po BID 41 (0.25,0.5 ,1,2 ,3 ,4 mg tab;DEPOT 12.5,25,37.5,50mg vial ; CONSTA M-TAB , g melts 0.5,1,2,3,4 mg tab; 1mg/ml soln) 25mg; 50mg IM q2w 25-50mg IM q2w 368-708 FDA D1-4, 5HT1A&2A,1,2,H1 -little M1(approved 1993) AE: sedation, headache, dry mouth, constipation, blurred vision, urinary incontinence, insomnia, agitation, asthenia, BP, akathisia >10%, appetite, TTP, IFIS, BPSD; BPAD: acute manic & mixed tx 10yr ; FDA FDA FDA Jul’18 3A4,2D6,P-gp Autism:irritability Age 5-16yr ; Schizophrenia Age 13yr (Perseris: 90-120mg SC monthly) seizures 0.3%, photosensitive, ?stroke/death, weight . Oral liquid not mix with cola/tea. DI: ?furosemide. EPS dose >2-4mg/day & prolactin/TG. ARIPiprazole ABILIFY, g Phenylpiperazine 10-15mg; 30mg po 10-15mg po AM 45-52 7.5 <2 >10 >2 >2 + P L (2,5,10,15,20,30mg tab) DEPOT 300, 400mg IM vial 400mg IM q4w ≤400mg IM q4w MAINTENA behavior FDA minimal 3A4/2D6 483 AE: suicidal ;wt , sexual AE,anxiety, tremor;gamble; compulsive behavior, stimulate, akathisia, EPS, SJS,QT, BP; DI: : CBZ, eryc, fluox & parox-etine. VAST-D autistic /Tourette 6-17yr D2-D4, 5HT1A,2A/C, 5HT7 Schizo ≥15yr; BPAD ≥13yr;MDD ; & for adult BPAD I of these may need ↓dose than ♂ disorders withdrawal General: Onset 7day; good trial is ≤4-6wk. 25% of pts respond poorly to Tx, yet 30% respond to clozapine. ♀ Positive S&Sx: hallucinations, delusions, thought ; Negative S&Sx: social , isolation & apathy. = dose-renal dysfx =scored Neuroleptic Malignant Syndrome-upto 1%, often within 30day;esp. younger males,high potency depot; mortality of 10%,S/SX: >39oC, muscle rigidity, delirium, autonomic instability (i.e. BP),CPK,HR, arrhythmias, tremors, seizures & coma.Tx: D/C neuroleptic, cooling blanket, hydrate, dantrolene, bromocriptine & benzodiazepines. Tardive dyskinesia-after months to yrs of neuroleptics, in elderly.S&Sx: fly catching/protruding motions of tongue, tics of the face, chewing motions or excessive blinking.Tx: D/C/change/ neuroleptic,anticholinergics, tetrabenazine, donepezil, Vit E 400-1600iu/d. Depot Meds-after 3-6 months many accumulate; thereby, requiring dose, onset of action for most are 2-3 days (Peak 4-7day), except Clopixol ACUPHASE with onset: 2-4hr,duration: 2-3days and max. sedation at 8hr. (see pg 155) Pregnancy: Consider risk vs benefit! Use lowest possible dose, if possible try to D/C before delivery; neonate EPS risk & withdrawl sx. Avoid if possible esp. during 1st trimester. Phenothiazines are not thought to be teratogenic most data with chlorpromazine. Atypicals: not routinely recommended (assoc. with ‘large for gestational age’ babies), but benefits may outweigh risk. No known congential malformations? risperidone. Recommend folic acid ≤5mg/day & monitor blood sugars developmental toxicity. Level by: antacid, cholestyramine, carbamazepine, phenobarbital, phenytoin, rifampin & smoking. Level by: amitripyline, amiodarone, cimetidine, ciprofloxacin, diltiazem, erythromycin, fluoxetine, fluvoxamine, grapefruit juice, isoniazid, ketoconazole, nefazodone, paroxetine, propranolol, quinidine, ranolazine & ritonavir. EPS Acute dystonia-spasm of face,neck&back-like seizure(Onset 1-5day esp. young male,Tx:benztropine) Akathisia-motor restless-not verbal,pacing,fidgety(Onset 5-60day,esp. old female;Tx:dose/ low potency,lorazepam,propranolol,diphenhydramine) Parkinsonism-rigid,bradykinesia,shuffling gait,tremor (Onset 5-30day esp. old female;Tx:benztropine, amantadine) Rabbit Syndrome-rapid chewing movements (Onset after months esp. old females; Tx: benztropine). =EDS = Non-formulary Sask $105 BPAD (FDA BPAD1 age 10-17yr) interval 1A2 Asenapine SAPHRIS: 5,10mg SL tab BID Wait 10min after SL tab, before eat/drink. D2 & 5HT2A. MayQT ,EPS, akathisia, somnolence, allergic rx, minimal wt; mouth numbness,poor taste.
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    (19) & (11) EP 2 114 406 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/496 (2006.01) A61P 31/04 (2006.01) 25.05.2011 Bulletin 2011/21 A61P 33/00 (2006.01) (21) Application number: 08700129.3 (86) International application number: PCT/DK2008/000005 (22) Date of filing: 07.01.2008 (87) International publication number: WO 2008/080408 (10.07.2008 Gazette 2008/28) (54) THIOXANTHENE DERIVATESAS SOLEANTI- INFECTIVEAGENTS FORUSE INT HE TREATMENT OF INFECTIOUS DISEASES THIOXANTHEN-DERIVATE ALS ALLEINVERTRETER DER ANTIINFEKTIVA ZUR VERWENDUNG IN DER BEHANDLUNG VON INFEKTIONSKRANKHEITEN DÉRIVÉS DE THIOXANTHÈNE COMME SEULS AGENTS ANTIINFECTIEUX POUR LEUR UTILISATION DANS LE TRAITEMENT DES MALADIES INFECTIEUSES (84) Designated Contracting States: • MORTENSEN I ET AL: "THE ANTIBACTERIAL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR ACTIVITY OF THE HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT PSYCHOPHARMACOLOGICAL AGENT RO SE SI SK TR CLOPENTHIXOL AND ITS TWO MAIN METABOLITES" ACTA PATHOLOGICA (30) Priority: 05.01.2007 PCT/DK2007/000006 MICROBIOLOGICASCANDINAVICA, SECTION B, XX, XX, vol. 95B, no. 6, 1987, pages 355-359, (43) Date of publication of application: XP008066133 ISSN: 0108-0180 11.11.2009 Bulletin 2009/46 • KOCISKO ET AL: "Comparison of protease- resistant prion protein inhibitors in cell cultures (60) Divisional application: infected with two strains of mouse and sheep 10181816.9 / 2 301 545 scrapie" NEUROSCIENCE LETTERS, LIMERICK, IE, vol. 388, no. 2, 11 November 2005 (2005-11-11), (73) Proprietor: BKG Pharma ApS pages 106-111, XP005042190 ISSN: 0304-3940 2920 Charlottenlund (DK) • KAISER C ET AL: "Analogs of phenothiazines.
  • A Straightforward Route to Enantiopure Pyrrolizidines And

    A Straightforward Route to Enantiopure Pyrrolizidines And

    Molecules 2001, 6, 784-795 molecules ISSN 1420-3049 http://www.mdpi.org Biologically Active 1-Arylpiperazines. Synthesis of New N-(4- Aryl-1-piperazinyl)alkyl Derivatives of Quinazolidin-4(3H)-one, 2,3-Dihydrophthalazine-1,4-dione and 1,2-Dihydropyridazine- 3,6-dione as Potential Serotonin Receptor Ligands Piotr Kowalski1,*, Teresa Kowalska1, Maria J. Mokrosz2, Andrzej J. Bojarski2 and Sijka Charakchieva-Minol2 1 Institute of Organic Chemistry and Technology, Cracow University of Technology, 24 Warszawska str., 31-155 Cracow, Poland; 2 Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna str., 31-343 Cracow, Poland * Author to whom correspondence should be addressed; e-mail: [email protected] Received: 26 February 2001; in revised form: 28 August 2001 / Accepted: 28 August 2001 / Published: 31 August 2001 Abstract: The synthesis of a series of new n-propyl and n-butyl chain containing 1-aryl- piperazine derivatives of quinazolidin-4(3H)-one (7) 2-phenyl-2,3-dihydrophthalazine-1,4- dione (8) and 1-phenyl-1,2-dihydropyridazine-3,6-dione (9) as potential serotonin receptor ligands is described. Keywords: Arylpiperazines, lactams, serotonin receptor ligands. Introduction Early studies by Hibert et al. have shown that there are two basic pharmacophore groups common to all five classes of 5-HT1A receptor ligands: a basic nitrogen atom and an aromatic ring with its centre positioned at a distance of 5.2-5.7 Å [1]. Since then several attempts have been made to extend that model, but the large diversity of ligand structures made definition of general interaction modes Molecules 2001, 6 785 impossible.