4 “Tolal ce Moles ont Phavmaaceulical Chen by structures: — Sap fp Lnporland functional. grav | a Stiradare. Guroup olraclure pt as o | Mitriie. —C=N Cilla (Gyano) ° | Aldelyjde a Uther AG -0-c~ I Alcohol eee Fsler -G-0-¢- am - ° mine =¢- NH, | C pyimary ) eae {2 sO. MH-R | | fe de | fare Ge N=R Amino_acid 1 (CTertrary ) Bo eee | UNS, eta Dona ii ; coo | R Qualernary es fe K* amine saul Carbryjlic acd | - gol = 2 | {ZI ne 5 *Comformalion of orgame molecules in most commenly defer nrived 4 HE WNR ( Nuclear mragnel ic resenanice .) 1 fee gt Siaeetaat ave_divided inla_ three tain pe fe : pom isomers ane Gonformalioval (somers. Qo ohcal | awier’s,4 Dale (1) Qlicabtsamers’: Coulann at least one chal Casymmich ie) Carbon — + Chiral cevbem = Carbo atom Unt uv covalenlly bonded lo four different substitoends, oH CHls Lrample «2 hydtronybetonte + Wee wH Ho ef H'Cr CHs Ho They are. mirror imoges of each other ard aan not be supeviniposed , ar: 15: ave oplical tsomers lhot are mirror images of cach olher ar ul have iclentical chemical. and physital_praperlies except U Int one volales the plane of polarized light ina clockiyise diveclion and sol wm Galled C4) ar dertrarolalory (D).ard. the olher ina cauviler clackinse direction and called (—). or levoralatery a +fure erontioney either O’ar Lis oplically acl » Kacennic. mixtore Equal proportion of .D and L. mixture of a canpaund anid is aluinys aplically inaclive. cy dope (LS hyospmnnse) Examples 1) Levorphanol C1) has polent narcolic, analgesic. “and. ante tussive properlics whereas its mitror image dexlicorphangl has only conli-lussive actly. e Ze D propery plane in anabeste while L to autedussr = e02) (pinephvine Cts. £o_times more. polent Uhr sls -)enantiomers_ Deseo Irene tleastzctive two Chinl. corbiats where Me és.) ond_the other ia (Js Sop they Camt be mirror tmages of each olheror_superimposed.. Thus, they ano rave ante Chival Culer _that ia tcentical “ond the other ne ia. opposite. (nike, eneniliomers, chastereomers onc differcut in physicochemical properles suchas ee and aut point, = = — Of NHCts ~ plete eee hao luo assy mie chic Hie a on ie We ice NW- Cis, Sacer a2) Hy ee, ea —Wtrt_the other fino are cranliomers called pseadoephach ine (4) 82) = wale: Pseudoephedrine. ee vasopressar..aclivily —thon ephedrine... z eels pa cis Bis Ole er) lee Ho e= Ww —Hiceta=C =i fae Dee ee tF a NH-ciy Cee ee CMs 4) * Peeudaephedcine Gea) There, a) ephedrine. ore.cnanliomers.., CEC) _psendoephedrint_are_ Abies but, —-€pheelrine_8_pseudoephedrime, are. diastercamers.not Date (T) or CF): WEphedvine & pseudoephedrivie avec optical cher 5) CED) () (AKO) Pseudo ephedrine. are Diostereamers, diestercomers CF) enantiomers + tpimers + are special typeof diaskercomers where lwo impers are. shructurally édertical in all respecls excepl for (he slerco- ~ Chemisty of one Chiral cenler: (where irs inverled ). Example: 4 epix tetracycline Ho. sth’ NUCH), - ie ck ee rer ee ee” ee ‘ c- NH, — \ : on = -N¥2 HO" O voy o & Woo aye tees Telrageline am A epitelracgetine Wole.’ Gimerizalicn la. omparlant in diup_clepradalicn I ¢nactivation. @)Geomeliricisamers.(.cis=trans isomers) This. occurs as. a_result of restricted rotation aramd double bonds or igi ing-syslemas., = : Very amporlant naless ae E (O_Gs E lions_tsomers_ove NOT mirveyumogesand. Le have DIFFERENT. Physicochensioal _ayre pharmacological — Propenlies. an (2). Since the funclronal _grenps are Separaled...by different —distances.ia_the Cis and frans_ssomer, So they dort fit_the Sante receplors equally well. Lf_thene jroups “are Phew wacephore. ,No 5 __Date. iene biee (ew tsommers have ae bialogwal aclivily « ~ pharmacophore gpaup rncans.: Ue ee the molecule which interact E with the veceplor (SAR) . +. Lramaples of cis & trans. isomers: F p oO ) Gee diel ylstibedrol has nly Tt the ‘iii actinty of brans = DES. fee ESE i ves Jeg 5 The aishve eae hema 8 ee i ACO) groups. ¢5_the same sleig Poies ¥6 ~ E as Thal n_estradial E Estradiol ~*2) Gleic acid & its tvansisomer,, elaidic acid. CHs CCH, He CCH, cH 3, a), Gh CHs, ay . Hooe (eit, 3,04 RC Coz) Coot Oleic. acid (cis == Elatdic aciel Cray 3). Cissvelinarc-acid (CIsotretinain Yam ols: trons isemer Ctrelinoin) Olly = ois Gil grains Sc Noy seq Taken orally ( sepenson GH, of drug in oi) formalabedl fone as soft gelatin capsule —.__ Lsolictinoin Lt tabreat severe resistant’ CCis- elmore acid) gptic acne. ‘ coonNo. 6 Pa otis tts Cl, Athy S @o, il tapyeally cs : Sabon ON ye bo y/ A Applet tapionlty Pe Ms in Che frcatinend of acne Trekinoin (Relin- A®) (Trans ~ rebmeic ocd) G3) Baberanetioned -somevisnane Cmformational isomers or conformers ave narisaperimpasoble orrentalions of a nolecule duc (o Kolaliow of atoms around Single bonds. ( Simple bonds) w Han chugs aan exist in marc than one conformal 4, givay them obilily “lo bind. to maaney receptors, and receplor oly pen Lxanyples of Color mational fsomers () Tans conformations ‘ol vocelylchalevie binds bo grvscer ie veceplor's whale gauche conformation binds be the sicolnic receplors. Bolh catormalions occur as a result of Yolation araurnd the carbat= carbon single bond. (Cl Jy W®. (Cll), : é EH aie A et cae Ic | : H Oke Trans nisie —___Gauth (0 > to 1 casters are: rrolseulea_conlaininy groups thal are. spalially and eleclrochennically equivalent” 0:9 “amide bend and ester bond irr procera and procaine respectively » éNo. iG Date *(2) Galarrwdion of “SOMBRE CH CH, MB: The favored.conformation.is the avie tr which the ln ger frtups. are separrted fram ne another by as peat adistuie as. ee j cv By ae: Single C-C Tond WE C= = egos _ Ethane. —Slaggertd. Eclipsed . Aloms are sepmaled Moms lend to posiben by-as great a distance Yronselves im space with as _passible. a no lwo atans otrveclly 7 ace er facing , ie, nol eclipsed . (5) Gastar malin of Gyelahexane i é pec rete sitoheeaialeas Fake ow —_Yelohexane is prebent ta what in called..chair colormation hich may be axial or egiatorial —stording LS. the positions of h paie fal —__ wat — Equatorial Mphogens ove pnalel « lyropens. ave. aypronmalely — with thie ovis. of the ting.» an the plane of the ring»No 13 Dete ct (a Phuglalenine z —— Hear be cawverled. to lyrosine_as_follaes: Phenylalanine Aydhorplase oO Cih~ GH coo -CHy — CH- Coon = 1 —— oho \ ue Ny CT Niky i Phevwlalanine - Tebralydro- Ditydro- Tyrosine biopteyin biopler in (DNB) DNB reducl } wpe Ht J NADPT i = of phenylalanine hydroxylase. or DHB reduckue® leads Sa fo on Of phenylalanine. This diene it Called : 2131 Wrosine 3s the preausaof + _ * cay Calecholamines : GOH S * cool Tyrosme, ' Home pec yeni EUUeSMs ce _ Gly = CHAU oct © Tydroxylase iG Lp fad - Tyrosine a Ho Cn witechondria) Dopa Get — ‘ pLP Dopa decarboryhse Flaaglttaalanaivas (Ty gtoplaswn We mel bl Crans erase ia Dopamine B= wo nin Ho: CHy ~Cly = Wy CSA 5 2 io. i Tn-adeunal’) lorgpnaepharine. waive Cre : i oll Hs mcg af Wo4Y—bn= CH NTNa 44 >, Struclare- activily relat cvtshyp of sprnephnine + ae pl Gils a) Hele all grap wv a 2H a ee S essential for activity Ho (Helo) desta fy sotap) @) Removal of Para-al gives Compounds. with a-adhenoceplor activily only. *¢3) Addilion of mel hy! group on A- Corban improves oral aclivily, (4) Javger N- substitulions ( than a mel yl group) gives comipanrds wilh” B- adnenoceplor selectivity. “ dobielansine lerbulalinre, .-- (b) Thyroid hormones : Th vroglabulin és the precursor of 13 and Ta. and it conlains man: Iposne residues ,.ahich are todinaled la form the “inachve Preaursars : diiodot hyrasche (DIT) and mmoiodo lL wrasine CNILT), Ho Gilg Cll Hy 2 boot pleiele a ee Clly-Cll= NH = coo Fea Diet R nyo Then, HITs O17 panne Woo LY ce gay Zi 1 S TOOH 1a or, DIT+ DIT ed rT Peyaxidase. Wo Y-0-F Nc sith : : I i GooH (14)No 15 Date (6) Melanin opnlheais : “Tyrosine ial comerled fo dopa (as belore), Chen dopa va converted fo melanin by series of complicated steps. ay. Tiyplopha (a). Serafanin & melabmin + 2s the _precursar_of : ae 7 wile ya Clly- Cll- Goal) — Gi~ Cool? a gary i Tryptophan hydrorykse HOS —~ cleo ane SE ee eine om iL, \ 7 ws am Teyplophan ’ ¥ w D> hydraxyb yplophah (PLP) Decorboxylase y cog CON acetyl transfers. hoy PEL via 2 Helly Wrasse THs 0 oft aaa NH (aay) Gly ~ Oly -NMp ¢ E=0\ 5-lydrasy lryplamine. chs ) (5. HY) Nelataninn : ‘Serolanm Csecreledt by pineal gland én {he brain cid mney ado __role_m sleep cycle J. cb) Nicolinic oad ( niacin) : Mubrilional deficrenay » fellégra 5 16 thas treated auth bath tryplophon and the vilamias (Bs) Ce). Some pulrefoctive substances thal are produced by Un action of bacteria on, proteins a1 large mlestine , Samples + iNdaf and sKalal. - id a zoor coolt Dall “(63 Glulamic ‘acid thn dit Ct Cty —cooH ca) Gilulamale,tself, acts as an exeitalary rewrolransmitter in all CNS neurems. suds be ole OF 2 (bh) Glutathione syulhesis.. ( See page an dhis reviews) c) Jolie acid synthesis 9 cool 7 onl ees ; ae N-GH— CHCl, _ Cool) ee HN y eee > ane ; ee oe ““Pamivabenzoic — Gilulanic aciel Ppleridine PABA) - base - t Di hydrofalt C. acicl : #4) Synthesis of GABA : GABA ( Gamme. anunobulyric acid). (s an ae neurolransmitler in Ife. brains & spinal Carel. s Hv-cl- Coot L fle cae earbayha lbw El, poate ach CHe PLP as [coenzyme a Ne CooH coon [ Glakamic acid ] [GABA ] Va proic aciel Nv: GABA, def sctency may bedue_to. clefrcrency of cilher 1 7 (GAD or { PLP) and “can “lead to convulsions i Chilsien.No AT a Date \ “T61 Arginine : _ @ Urea : vine is involved in urca Cycle in the liver, » 0b) Creatine: (See page 12.0.thin. rewire) ©) Nilete Oxide__CNO ) Argnuine No syntrase a. Cilrulline +. NO wote: Citrallime is also invalved on area cycle. ms Ee. Aspartate: ilus the. precursor of or inwolved in: » ©) Purine synthesis and pyrinicine synth = (b) Asparagine: Asparagine. cnlers in’ the structure of Orylacin. co) tea” cycle on the liver,[B] Carbohydrate : Car bohydroles are polyhydroxy aldehydes or Ketones art arc classified as: CO) Noviosaccharicled : Gmsisls of poly bychroxy Kelme (c- fruclse)) or pabyhychoxy aletelycte (eg glucose) cunt : * Nolo: Aldehydic monoscccharices are ‘edticing agents. This properly wos ned in the pasts lo estimate glucase level en the avine by rectucin’ Benedicl’s solution, but il ia apparently non-specific and inaccurale, Te mechanism a5 follows’ ~ Beng a vecdacing agent , glucose can reduce cupric. ions (att) toy Cuprus. ( Gul¥) oxide. which in Insoluble and reddish orange im Calar. Since ascorbic aciel (Vil. C) in alsy a reducing agent , Se, it can give false positive resalls. Therehre, in order To be move spectic , reagent sh eps inaperqualed with : (1) Glucose oxidare ehey inte 7 (2) Peroxidase enzymic ie 03) Ortho taldine (dye) Vv are used where glucose ia. specitically oxidized lo glucovantc acld by glucose oxitane and H,02. Then, Hy Op in the presence of peroxidase (on the srep) ,conr ts orthotaldine dye tnlo (rnlense Lue Color) which can be measured by the instrament’ ov lo a seb of previous slondards. Tir's method jo called zs ae Note: Benedict and Climlest methols ae bared on Lapper Yeduclion while Aeelale_teblls and Kelastix methods arc uned to detect ketone badieo in the urine .J 8 Kreb’s CTCA) cycle : imp a gee © Se ae oe renee = A Batol lu = Galucose-6— f° Es : ea = 0} = GH)-0- ° W 4 rer ee a : 3 ie HHO SoH —~ 2 : n z : aoe | eo 2 e : 3 p \ Fruclase — 6~ P y | i) = Stee s : — aoe cat AA (Lack of energy (ATP)) sem | ae, sO es Sleps C Krebrs. cycle fall capocity ) — S tg a CHg ‘ oils boo : hcl «_ dehydragenase Wo-C-¥ Ries coon Anaerobic} Cool Ky, a py ruvic_ acid : oe 2 hydroxy propionic CAerobic — HS~Go spyruvale. del drojenase. Complex acid { Lachic acid) __Goditions] Coy rr 5 : i Hp CO*S=CoAS “Cheats a eat? =e ———}> Senthase Ace GA ea He ote ae iis ‘c-—Caol _ sic — coon cyede : Lotalecabiti Sly COOH... Cy =-cao (TCA) Gitric act20 mea Gmsist of shart chains of monosaccharides Jorned covalently by glycosidic bond ashich can be hydrolyzed by acids. U bases ). Examples : C1) Sucrose DUC SSACR ES me Glucose + Fruclase © the intestine. (2) Mallose, __“a tase & moleader of (ilucose ————_» 3) hacloge Laclase [in large tnkestine J Glucose + Galactase (Aik sugar) R= galactosidase ) *c4) Lactulose : és a synthelic disaccharide (hal is rol absarbed or aflected by disaccharidases Mp Uses and! onechaniain of ach of. haclulose : 'Maclulose és broker clawni by bacleria iar the Cheol Colm énlo acelic acid. and lactic acid , Uhis leads lo chop ti th ee the pH and Chus The Gonversion of (oxic and absorbable NHs inlo nont-loxienen- absorbable Ni¢* tan _ahich » a Complexes wilh fallly acids in the colons Reduction - of Nilg level in the Colon creales & concentration gradient favouriv, diffusion of Nits Fram the bload to Ue Colom _and soon. This. ts ubhized __(/-actulose) s clinically in treatment of (hepatic. _entepbalpally ce & Ayperammaner nic / (Blood ammanta tevel ) due to liver dys friction , i¢. 410 urta cycle. Another use: of: Lactulose is being an.asmalic loxative- “ cS Hon oO hae ekioll Ho. Hf OH Gralactopyranosyl- D> FructefrarvseNo. 41 Date —_ ; (3) Polysaccharides : (Also called glycans) are long chatir polyiners “i of carbaly drales and ving “be linear ov Liarihed. They can be clossitied.as hono~ or helero~ polysacchorided : (ay Homapalynechovides. Conteuv only one Uype of mapomeric esse Flew : unil. Examples : (i) Stench Pancreatic or Nallose colivary amylase sbrony orci Glucose wole: Slarth is insaluble in water duc to presence of highty branched chain, in its.sbructure. Ci) Gilycogem. Hight branched chains. of glucose. Jt server as —— Ue main starage cof polysaccharides 01 oniinade ethide. strats jan_planls, os *ciij) Deklvan_ -branched pp ccharicle cansishog af abeut 200°000 glucose unils and wed ad a plismm expander” an palrenls who have experrenced loss of blood Cb) allelevaypalysccclamcides + Conlain_ two ar mare lypes of monomeric sunils ae Examples (i) Mepari (on_acid mucopolysaccharéde) + Consist of_sulphale of N= aceyl glucosamine and Kiduronate) Jlrs. -Sepataled From ang tinue and CS used to treat’_blood_clats. cli) stn Vi lreous humor and Beition synovial fluid, fl_nsists..of allering unils of = eacelyl glacasamine and. bl acaly-muramio acid.Nn 22 Gd Jatly acids + They are lang chain carboxylic ocrds which may be saturated or ‘unsaturated . Oxidation of double bands in unsaluraled FAs io called rancedity. Mole: Fally acids con form esler with gy ceral [lo voduce triacylglycerol C161) whith ie sloved om (he frally Irssue and hed as on energy clre. & Calabolism of Tors: (See a text book fur detak) Crat 1G e FAS Glyceral © Lnsulinr B-opidalion | Styeolyors pyruvate Acelyl co Krebrs cycle mp ATP 4 6% +10 HsL : Hormone Sensitive Lipase Samples of falty acids and relaied Compounds “Cy Thao carbons: Akelic acid Cy Cool *(2) One Carbo: formic acid H=Cood (wot fall acid) *3) 18 Carbons + Sleavic_acid CHy (CH), Coo a) 18. Carbons 65 wnsafuded *(5) 16 Carbons © hydroxyl grey substilubions¢ Kicinoleic acid : y J I fiaA No_ 23 = Ban Date * Cl - (cll), - cil “Cll CH= cll = CCH) 3 OH - cool 7 ome Mole: The_ester_ of vicinsleic acid with glycerol ia Calle oF ricinglein_or_ Castoroil., ~The preserice. of Colt) grup in the — acid the ail” some polarity making 1b meses : le willy alcohol ——Ond “imuuscible with amimerti siband ather hylrocarton avenls. —*06) While woxs dt 1 mol’ a fally acid but an ester of hegh Molecular aucight alcohols end acids , (24-34 a Carb alomsy. white Wax in dey ived by leo bing » beesulax. Cyelln> war). C1) _ Garnauba, wax: has higher molecular yyej ME than while ying ancl 0 thi given i herrhaedy ashich makes : —_-it_woelal in. polishing mixtures for Coaled tablets, é *8)_ Cb pabmilale + s L he wy Se ablained Fram ae thehead of sperm ai hale o.. ale: Hineral oil po om xture of liquid frychocarbons ablained fram pelraleurn:. Bein aml- polar, it in immiscible ~—with_waler, alcahal.ar Gastar_dil because Lhoy have ————palar (OH) ormups. ffs. specilic. qravith ia. les tran 1 (lighter — them aby a i p / ~M-B ¢ 10. ppm Yet. (licopheral)., antioxidant, 1 added th ——— prevent oxictation of ansatiraded Chains in mineral oi! ——— fo. peroxides which give ant__tndesiyable odoy anf laole * a Olalam usa mixtine « "Lagu olplaic ydrocarbens with Solid. lydia carbons..(Cx5— Ceo) (hats. they sare _Hon-Polar- ered immiscille Ealeodol. >No Re Frat cg) Prostaglandins (Gis) and leukotrienes (Ts) + are related ror lo fally acidss They are sylhesized from archidmic acid , the main precarsor én humans. Archidenic acid ia a (29) aarbam alems with @)double bonds ie, palyunsatarated.— Jt & derived from smnembrone phospholipids by phospholipase. Ay. Archidonic acid Nrchidonic. acid io acted upon by cploowygerase (COX) enzymes 1k 2 Io produce proslaglandivs and by 5- loony gerare tnzyme to produce leukotrienes : # (A) Prostaglandins + They ave named in reference to the hrypolhel ical cenpound, Prodanotc. acid. They ave classified lo sever main classes..A, 8, C, O,E ,F & I. There Classes atc distinguished by the spatial arrangement of the functional — prays al Cy) and Cy of the. cyclo pentane ring. A further subclivision according tothe. number of: double bonds on. the side chains ia indicated by the.subscripl 1, 2,3. Archidmic acid derivatives always have [he subscript 2. p A a —— bramples. #c_ POEs Ho,No. 25 Dae aoe / Fai) Prostaglandin Ly ( Prostacyclin ) : fam 98 Shas asshivais ring allached to the Gpelopentanre ring so,il is referved la. as prostacyclin. Lees cool een = _ Prostanoic acid: Ho ieee 0 Cit) Aiprastedilio used to mainkxin patency of ditchus _. arteriosus in. vieonales, Glucocerticaids do if, opposite. Ch) Leukabrienes + are also derived from archidanic acid by O-lipoony genase... like. PGs, they. don't have a. cyelopentane. ring —~inthetr structure so, their synthesis is called. the linear pathuary | -of archidonic_acid metabolism. awhile PGs. synthesis 1s called the cyclic: palhusay licnce (he_name. oyclooxy gease Cramp: leabolriene Ag UE Ay a Ss ayeNn 86 bai EVI Saponificalion *Oelinilion : The reaction of fat (Triglycerides) ov oil wills a1 moryanic alkali ( KOH) to produce soap and glycerol. oO Che OG. Ry R, Cook Cty oH bH-0- OR + 8 KOH_Sepmibication. R, cook’ 4 CH-oH eas. cos R3 Ry Cook’ Cy-oH Fat or. oil folassiam hydroxide Soap Glyceral ( Triagl glycerol ) i Inorganic base.) Bwole: for idenlifying a frxed oil or judging ils quality, the Saponification value io used which és“ delermined by the number of milligrams of KOH required lo saponify the esters or neutralize the free acids present in one gram of the oi. © The difference between (esters) and foaps) GE * Esters: formed by reaclini~of org anie—acred and alcohol , where the OH) of the acid ral alKory (Ro) group of the alcohal : ae ZY R- CHOW + R= Qe R-G-0- RR + HO wt oe ti One H O Carboyylic acid Alcohol Gsler uielir “he * Example : Chylocalale Ose. oy -¢ -6%& eu; * -@S 2°? Inorganic acids also farm. soaps with alcohols. ae Soaps: Are the sails, of organic. fall Meee cirenaien melals such as Na and_k* ( baller pelily) » Soaps have or Rx of, ygonic. bd omppnic. LooeNo. auf Date. detergent properties ond mild anliseplic action. Soaps render agueaus solutions alkaline. : efi Exanipls of. soops : (1) Sodium slearale : ‘6 = (2) Polassiamoleale «9, 4 oi . y memes * Fxanipks of related Compounds: ~ (4) Zinc Slearale +o water _repellent pauder Chat wos used_as_o_tablel lubricant but was a divalent found to Gawe palin nl laagaal i o anal dot lp bons es = ee (2)\ Trielhandamine oleate’: ts an amine salt, used as the Es emulsifying agent in benzyl benzoale lolion, t Bester (Thor (A+ £thglacelate is a soap (f). SP ~-*NB: Soaps arc caisidertd : Anionic surface active agen >So Usey Can inaclivale calimic one. peas ees S Secineior isles = tomate i as e-g benealtoniann chilariceNe. 28 EVI] Opioids : The prololype is Morphine: WB: There are 5 (NG nS (EB Nole; Morphine has Bassymetric centers and ; occurs naturally a Lhe Le) cnemtiomer. He *olher morphine analogues and related compounds: rings in i shuclure; A, _*O) Codeine + mellybmorphine q ¥¢2) Ilevoin : dhacely! morphene ¥#(3) Numorphant : Oxymor phonic * (4) Dilaudid : | lydromorphone #5) Dion ; Ethyhnor phite ¥(6) Penlazocine + is a (antixed agonist ant jonist )opiaid used for analgesic . Naloxone “Can oproid alagonist) is added lo penlazocine lablels. mainly te raduce_ils abuse alential and secondarily to decrease respiratory clepressive ed in case_of overdose . a pe Aibetlon added tale b abuse Pabr ¥c7) Dipherouylete 2 i an agent useful_in_cliarrhea and ils straclure 's similar to thal of meperidine. ft yet has some of the addicting properties of meperidine. lapsamide ia also anil Opiotd an disehcal Walith fa depp of any of the cential optoid effects. Neperidine has a Gommen riame :\ Demerol,No 29 Date ; : CVIE1 Alkaloids : ee AlKaloids ave rnalevally occuring compounds that ave derived Maily from planls and “some from aninuls. * Camm properlies of alkaloids : C1) They ave weak bane (hawe. pka more than presence” of abasic ~N- in_their structures. They salls wilh acids eg.morphine sulphale. %(2)_ Sleveoisomerism ia common. én_alkalaid so large clifferevices In therapeutic activily can be expected. g 7) due to can form a (3) Insoluble in_waler and + soluble in alcohol. —* beamples.. Atropine , pilacarpine , hyoscine.,... ele, (1) or (61:01). Altaloids have pha ess Uan 1 (F) on —aaave than 2) Morphine iad acdeeria line. are sdansidlexeduta HewrIka hast CT) Nole: Alkaloids alwys have the suffix. (inc) in thety_ names.No. 3p CVIL} Antibiotics : ee TA} Penecillins : Y bw * They have Common slructwe containing : a Belaclom 5 thiozotdine ‘ring fased tayeler * . Rnecitlins differ Chemically in the acyl side chain ®. Unt of penecilliny actively s defined a5 the antibsolic aclivily af 0.6 My of Sodium penecillin Gi reference standard , > * Nos! penecillins are markeled as sodium or polessiant salts The polassianr content af perrecitin Gr ts Ad am by per million amils. 7 *. Wathicllina the most acid sensilive porecillin. *, Ofacillin és uselal ov treatinent of slaphylococci resistant bo penecillin G. ( fencillinase ~ producing slrains) . Oxocilhin 's abo acid lable , he, oxacitlin is bith’ resislant ts peuccille ay and acid hydroyors. ® Penccillin 6 benzathine provided a prolonged duration of action. oe Bacampicillin cower ils activity lo coiversia to ampicillin wluch 1S camsidered an extended spectrum pencallin. Amaxacilhn , —helacithn and cyclacillin fall inky the same.class. Tiey have an antino group in the side chair thal enables them to ois cell vial thal wx (nape meable to other. penecillins. (thal of Gim-Vve ongantsnt)No. 3t Date «The rast oylended spechum penecillns are reproveniled by The —atylureido penecillins such as mezocillin and piperacillin and azlocillin Acyluveide derivabves af ampicillin) _* macy io gguismmmaceasally b,c tnidonyl arbenecilli ts. x, > ke side_chaines = — penecill n& (Benzyl penecilln) OCH; _—Lhenayret by! pencil ce are 4 Penecilin_G_ ( benzyl penccillin) tsa natural penecillin. liable fo acids cand 3 lech naaed Gieneral formula of fenecillins Oe S Nw cng -Oxacillin Aid & fencaillinase~ sable rec. og —_Cleyacillin- OFA ae WL Ampicillin 1 Aad -stable_ (Extended specliun) es leita ae Ho > Gl Nile iz Amogacillin WH \ c=o i) cib=e Azlocillin Oren oe x S25 Pipers MintNo Ba, Dat i X — CH a) Cc=0 I oe z Carbenecillin + Garbenecillin ts a dicarboxylic com pound. Disodiom carbenecillin és given by injection becmae rs acid-—sensilive adhe. tndengl ester om be given oval _ *c8) Tetragyclines ‘ neg are oclalydro analogue of raph hacene 1 2 He op WE sy CMs 8 ae ey pao" aSeny a a ge Nl ORaeoOlee Op xy? « They orc amphoteric ,i-c, Canam sal with both acids ~ and = bare. 6 the hydrochloride salt io_lormet by. prokimalicn of N- atom om ‘carb 4. Anathersall wilh ascorbic acid w sed. fo prowenl preciptlation of. the tetracycline base in anyechons as they pecipilate above pll4. » Out of. dale. telracyclines copeci those. stud in high 2 humidity and. fempetalure. produce” toxic compounds that 7 Jaa ted ye prodiag of epinephrine thal ¢s _ dg pa J. less polar Lhan the porent drug and thus can penelrale (he Cornea in treatment of glaucoma + leyasterenol $b norepinephrunsNo = 35. bate CBJ Porsympathelic system + % 2 Ult Acclfcholintes Cig S CHCHy- N etl, Clg SS Acelyl ~~ ~choline Clle-Coot} —£tly~ COON » Succinyl chaline.s Cle E Clg Cly ~ Hn P succinic aciel - Chee CliyClle. t= Lcih jy 6 ” AL Tsoflurophate ges Gen ig eee * 02) Malathione. : (son arganophes phate. aut - ean auned as _pediculicide .No 36 (C1 Anaesthetics: : (1) Greneral anaesthelics\ : We or euie is AN CH, s \ ie cH, Pro pofol Cots —O- Cy Hs eh Hey) ethan = chereh Keto Z - thiePentel Sod Exomples i : ol NO Hpac! 1 a Nilrous *chlora farm : im oxide the presence of air, sumlght or open Momes ies oxidized to phagen: (0=C cl) gas which highly Ciel hy! elher Yeaclive and hydrolyzes in the lung to hyétvegen chloride = He-CH-al- ee gas hat causes pumona Mat 2 = i Nol cdema. Ethandl ycadls Milo Ee We? we wills phosgen (> form i “ meritoxic diethyl car borate. Kelamine * Thiopenlal Sodium Se, 1h alcahd is added to C2) Local anaesthetics: 2 Lidocaine: ~ CHy 0. cHy Lpophilic Amide aramalic en ieee anoeily eeu bond. Helps cress the ce membrane (uncharged / { Calls “NH-C— Ciys N. \ a \ Hyetrophitie amin 4) Nelabolized im liver p> 2). Comsidered o biotsosteric. yeplacement. of ester Chloroform and. stored in air-lighl light restslant cailainers ol lemperatuc al. above. 30°F (-1"C) . —e Tonized =» Acie er clurationog Pole __Gonld- local onagsthelicss ot _| Frocaive) eg ae C=0= ctl, — NI CH filet ie alls "ap te esterase > ; =f Bite es Ae tne) _ . ook: aan daible loond 15 - = “OY¥idized to the nd ie Zar eek de which 3) Chamazcpine— Sat 7 ge —8)Gar is toxic to (I er = J ee rar 3b A ren ely rare aaetteetah ‘ KA 4 an ‘2Note s_In the si“No BF Date _ ay. “Wrajanthuaics y. Considered ani pm ab ee ae —— phenalhiozines we ae a __cH s, -N ON a sa cake SN Wh CH ay St eee Sta ia Sas ae Sy 24 UH) Malapesidal sed Used ta _conteal_ Guiles dela Teutclle_ayndrame. vi eo Ech chy Cy or oa . ead cl © _ *ap__Dro CHg— clig~ NH NHe #xessential_for Alt. ( Phery| cyclopropy| —fhenelzine __aclivily in amine)cs Chee cy Hy Imij __ Desiptomin — ae a prnmine Note: Inthe side chain, W-alam. Note: In the side chain, No. ats 5 aioe oe = leas anbicholinegic effects. Ei juoxeline Z =O. CH= CH CH, — AMICI aSMR (0 EBiyLand.phery emp —p_longec Fie) a elena hae pao py a 8 ml — Rp LS sth ae lc any ag, 13 Japa sium 121 choral hyn ik clcht Mwy C= ues Ci Lal, ae f ————¢ een “ay. SS a ee oe cei 3 Ee - es 4? (hc acting) aoe g. oh Otay Ay orelee ? chlorbe Ze? 0 Ke. /D “Nea spirodtca nediane geen BEEBE SR wertausng LS CON Berzaiccapn BES SRGaT TG Ue Drea esas ic_esley of nitric acid @Dxehe ~ atin. digil eee rei ——qly.came_(_digilexese)_ Digoxin -in_soll capsule form haa g rcaler _oral lycone.{ shevai (lero id cucleus + ether bond I bioavailabikly —No 43 _ Date. a #) Benzothiacepine, aNy cH 5 7 fa [ne delete eet hos close shruclwal a aa sinner tochtabaide bal mana test rave any darth. effect the __#* Diazoxide _! Ln Mate M20 retention due toils ee ache. Ho on eis chs 7 ( {_\-0- C= COO, Hs O- (ct) C~ Coo}! : CH. eo cut I Clofi brate emfi brnzi~ salivalion ef potenay lipophilic. subslitution __* Diazoxidehas_mo_sul mami “eau Pane is _mg_diurelic_actim, ___* Note: Thiazides enhante [he aclian of amphelamine becouse ee they change the pit of the urine so thal anrphelamare which is “a, weak bape isin the reabsorbed form.No 46 Date. a eae ANA “Palihistaminic.ayents + Blosynlhesisof ide of the cer ea . ee om + a) Re Side chain ea) may bea — maple ache a vileo lye or Ee #. Str imelidine (_lg~ Pep nate wil=¢= Niece N= CNoy Gere formate No 47 Date. 01 Sleroidal_harmaes.« __ Testosterone. (19.6) ie —Carlisel (lc) tram Leydeg cells of the testis _ Foam _achrenal cortex Ha eee ee _ a2 aseT a larger Ry substitution et lipid -solubilily pole ———Such_aa_secend genera’ cain —Gily buride., eS : 7 ar pe tater oeNo 4B Date. 5A Alt-A lly Dees 41) Aspyin Acely ester af sal icylic_ocid : a mete (zest sali : lopicall ee ees Fea) Diflunisal tal ela halized ta slice E ——Aeeblsalicgic ocd _Methglsalighade. Dalat ‘ #( Insoluble in He) piers iz EN.B: Sodium_aminosalicylate + __ __& t wtal_action —__ ek - i + - ee = ___ ler ens i CNS eek oat hs ee ae toyictly el tench | a active — OREN Gh ae ee ee - Indomethacin Salindae Cre le - #9 Tepe cat deol beanpl Ltt ; leah te TS oh. Coot _ ‘S — es be a= 3No__50_ Date. FLAVA Impordant” sfruehures: * Sarbue adlare_agenb, (SAR) = musk have a—utaler solubilizing ond fal So lubiliceng gnouups in_the some Bie — ee ee pe tl pum: a “ - thi eof adenine LE ar a ~ + Chink Metabolite) 03) wlan mic. c.g Sorbilan iene aleale 5 Tal o_o / aa Ela deteesto: That Mba 8 6 2 oye Sw 7 ieee ae He. ou Theophylline a ~ Citi aathwnalic) |, Allopurinal (Anti-gaul)